TW202003526A - Aminopropoxyphenyl and benzyl 1-oxa-4,9-diazaspiroundecane derivatives having multimodal activity against pain - Google Patents

Abstract

The present invention relates to aminopropoxyphenyl and benzyl 1-oxa-4,9-diazaspiroundecane derivatives having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the µ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Description

Aminopropoxyphenyl and benzyl 1-oxa-4,9-diazaspiroundecane derivatives with analgesic multimodal activity

The present invention relates to compounds having dual pharmacological activity on the α ₂ δ subunit of voltage-gated calcium channels and μ-opioid receptors (MOR or μ-opioid receptors), and more particularly on compounds having this pharmacological activity Aminopropoxyphenyl and benzyl 1-oxa-4,9-diazaspiroundecane derivatives, methods for preparing these compounds, pharmaceutical compositions containing them, and their treatment, special It is used to treat pain.

The adequate management of pain poses an important challenge, because currently available treatments provide only modest improvement in many situations, leaving many patients unrelieved (Turk, DC, Wilson, HD, Cahana, A.; 2011; Lancet ; 377; 2226-2235). Pain affects most groups, with an estimated prevalence rate of 20%, and especially in the case of chronic pain, its incidence increases due to an aging population. In addition, pain is clearly associated with comorbidities (such as depression, anxiety, and insomnia), which leads to important productivity losses and socioeconomic burdens (Goldberg, DS, McGee, SJ; 2011; BMC Public Health ; 11; 770). Existing pain therapies include non-steroidal anti-inflammatory drugs (NSAIDs), opioid agonists, calcium channel blockers, and antidepressants, but their safety ratios are far below optimal. They all show limited efficacy and multiple secondary effects, which hinders their use, especially in chronic environments.

Voltage-gated calcium channels (VGCC) are required for many critical functions in the body. Different subtypes of voltage-gated calcium channels have been described (Zamponi et al., Pharmacol Rev. 2015 67:821-70). VGCC is assembled through the interaction of different subunits (ie α ₁ (Ca _v α ₁ ), β (Ca _v β), α ₂ δ (Ca _v α ₂ δ) and γ (Ca _v γ)). The α ₁ subunit is the key porous forming unit of the channel complex, responsible for Ca ²⁺ conduction and the generation of Ca ²⁺ influx. The α ₂ δ, β, and γ subunits are assisted, but they are extremely important for the regulation of the channel. This is because it increases the performance of the α ₁ subunit in the plasma membrane and regulates its function, resulting in function in different cell types Diversity. According to the channels forming the Ca _V α subunit, VGCC can be subdivided into low-voltage activated T-type (Ca _v 3.1, Ca _v 3.2 and Ca _v 3.3) and high-voltage activated L-type (Ca _v based on its physiological and pharmacological properties 1.1 to Ca _v 1.4), N type (Ca _v 2.2), P/Q type (Ca _v 2.1) and R type (Ca _v 2.3). All five of these subcategories can be found in the central and peripheral nervous systems. The regulation of intracellular calcium through activation of these VGCCs plays a necessary role in the following aspects: 1) neurotransmitter release, 2) membrane depolarization and hyperpolarization, 3) enzyme activation and inactivation, and 4) gene regulation ( Perret and Luo, Neurotherapeutics. 2009 6:679-92; Zamponi et al., 2015, supra; Neumaier et al., Prog Neurobiol. 2015 129:1-36.). A large amount of data clearly indicates that VGCC is involved in mediating various disease states, including pain management. Drugs that interact with different calcium channel subtypes and subunits have been developed. Current therapeutic agents include drugs that target L-type Ca _v 1.2 calcium channels, particularly 1,4-dihydropyridine, which is widely used to treat hypertension. The T-type (Ca _v 3) channel is the target of ethylsuccinamide, which is widely used in the absence of epilepsy. Ziconotide (a peptide blocker of N-type (Ca _v 2.2) calcium channels) has been approved for the treatment of intractable pain. (Perret and Luo, 2009, supra; Vink and Alewood, Br J Pharmacol. 2012 167:970-89.).

Ca _v 1 and Ca _v 2 subfamilies contain auxiliary α ₂ δ subunit, which is based in certain chronic epilepsy and neuropathic pain valuable class of gabapentin (gabapentinoid) therapeutic drug targets. To date, there are four known α ₂ δ subunits, each of which is encoded by a unique gene and all have splice variants. Each α ₂ δ protein is encoded by a single messenger RNA, and is cleaved after translation, and then connected by disulfide bonds. Four genes encoding α ₂ δ subunits have been selected. α ₂ δ-1 was originally selected from skeletal muscle and showed a fairly ubiquitous distribution. Subsequently, α ₂ δ-2 and α ₂ δ-3 subunits were selected from the brain. The recently identified subunit α ₂ δ-4 is mainly non-neuronal. The human α ₂ δ-4 protein sequence shares 30, 32 and 61% identity with human α ₂ δ-1, α ₂ δ-2 and α ₂ δ-3 subunits, respectively. The genetic structure of all α ₂ δ subunits is similar. All α ₂ δ subunits show several splice variants (Davies et al., Trends Pharmacol Sci. 2007 28:220-8.; Dolphin AC, Nat Rev Neurosci. 2012 13:542-55., Biochim Biophys Acta. 2013 1828 :1541-9.).

The Ca _v α ₂ δ-1 subunit may play an important role in the development of neuropathic pain (Perret and Luo, 2009, supra; Vink and Alewood, 2012, supra). Biochemical data indicated that after nerve injury associated with neuropathic pain inflammation, the Ca _v α ₂ δ-1 subunit in the dorsal horn of the spinal cord and DRG (dorsal root ganglion) was significantly up-regulated, while the Ca _v α ₂ δ-2 subunit Units are not significantly raised. In addition, blocking the damage-induced DRG Ca _v α ₂ δ-1 subunit axon transport to the front of the central synapse reduces the tactile touch pain in nerve-damaged animals, indicating that increased DRG Ca _v α ₂ δ-1 subunit contributes to Neuropathic touch pain.

The Ca _v α ₂ δ-1 subunit (and Ca _v α ₂ δ-2, but not the Ca _v α ₂ δ-3 and Ca _v α ₂ δ-4 subunits) has anti-touch pain in patients and animal models /Gabapentin binding site for hyperalgesic properties. Since damage-induced Ca _v α ₂ δ-1 expression is related to the occurrence and maintenance of neuropathic pain, and various calcium channels are known to contribute to spinal cord synaptic nerve transmission and DRG neuronal excitability, damage-induced Ca _v α ₂ Up-regulation of the delta-1 subunit may help to initiate and maintain neuropathic pain by changing the nature and/or distribution of VGCC in the DRG neurons and their subgroups at the center end, thus regulating excitability in the dorsal horn and/or Or synaptic nerve plasticity. Intrathecal antisense oligonucleotides targeting the Cav _{v 2 2} delta-1 subunit can block nerve injury-induced Ca _v alpha ₂ delta-1 upregulation and prevent the onset of touch pain and retain established touch pain.

As mentioned above, the α ₂ δ subunit of VGCC forms the binding site of gabapentin and pregabalin. Gabapentin and pregabalin are structural derivatives of the inhibitory neurotransmitter GABA, but they are not related to GABAA, GABAB or benzodiazepine receptor binding, or alter GABA regulation in animal brain preparations. The combination of gabapentin and pregabalin with the Ca _v α ₂ δ subunit leads to a reduction in calcium-dependent release of various neurotransmitters, leading to the efficacy and tolerance of neuropathic pain management. Gabapentin can also reduce excitability by inhibiting the occurrence of synapses (Perret and Luo, 2009, supra; Vink and Alewood, 2012, supra, Zamponi et al., 2015, supra).

As mentioned above, there are very few treatment categories available for the treatment of pain, and opioids are the most effective, especially when addressing severe pain states. It acts via three different types of opioid receptors (μ, κ, and γ), which are transmembrane G protein-coupled receptors (GPCRs). However, the main analgesic effect is due to the activation of μ-opioid receptor (MOR). However, the general administration of MOR agonists is limited due to their important side effects (such as constipation, respiratory depression, tolerance, vomiting, and physical dependence) [Meldrum, ML (Editor), Opioids and Pain Relief: A Historical Perspective. Progress in Pain Research and Management, Volume 25, IASP Press, Seattle, 2003]. In addition, MOR agonists are not optimal for the treatment of chronic pain, as indicated by the reduced effectiveness of morphine against chronic pain conditions. Compared to its high efficacy against acute pain, this particularly proves chronic pain conditions of neuropathic or inflammatory origin. The finding that chronic pain can lead to a down-regulation of MOR may provide a molecular basis for the relative lack of efficacy of morphine in long-term treatment settings [Dickenson, AH, Suzuki, R. Opioids in neuropathic pain: Clues from animal studies . Eur J Pain 9, 113-6 (2005)]. In addition, long-term treatment with morphine may result in tolerance to its analgesic effects, which is most likely due to treatment-induced down-regulation of MOR, internalization, and other regulatory mechanisms. Therefore, long-term treatment can lead to a significant increase in dose to maintain clinically satisfactory pain relief, but the narrow therapeutic window of MOR agonists ultimately leads to unacceptable side effects and poor patient compliance.

Multi-target pharmacology is a phenomenon in which drugs bind multiple rather than a single target with significant affinity. The effect of multi-target pharmacology on therapy can be positive (effective therapy) and/or negative (side effects). Positive and/or negative effects can be caused by binding to the same or different target subsets; binding to some targets may be ineffective. Multi-component drugs or multi-targeted drugs can overcome the toxicity and other side effects associated with high-dose single drugs by counteracting biocompensation, thereby allowing the reduction of the dose of each compound or obtaining an environment-specific multi-target mechanism. Since the multi-target mechanism requires that its targets can be used for coordination, it is expected that the synergy will occur in a cell phenotype that gives a differential manifestation of drug targets with a narrower range than the activity of a single agent. In fact, it has been experimentally demonstrated that synergistic drug combinations are usually more specific to a specific cell environment than a single drug activity, and this selectivity is achieved through the differential performance of drug targets in cell types associated with therapeutic but non-toxic effects (Lehar et al., Nat Biotechnol 2009; 27: 659-666).

In the case of chronic pain as a multifactorial disease, multi-targeted drugs can produce multiple targets and coordinate pharmacological interventions that drive the signaling pathways of pain. Because it actually uses biological complexity, the multi-targeting (or multi-component drug) approach is one of the most promising ways to treat multifactorial diseases (such as pain) (Gilron et al., Lancet Neurol. November 2013; 12(11):1084-95). In fact, positive synergistic interactions of several compounds including analgesics have been described (Schröder et al., J Pharmacol Exp Ther. 2011; 337:312-20. Erratum, in the following: J Pharmacol Exp Ther. 2012; 342:232.; Zhang et al., Cell Death Dis. 2014; 5:e1138.; Gilron et al., 2013, supra).

In view of the significant differences in pharmacokinetics, metabolism and bioavailability, the redistribution of drug combinations (multi-component drugs) is challenging. In addition, two drugs that are generally safe when administered alone cannot be considered safe when combined. In addition to the possibility of undesirable drug-drug interactions, if the theory of network pharmacology indicates that the effect on the phenotype may result from hitting multiple targets, then the combined phenotype perturbation may be effective or harmful. The main challenge of the two-drug combination strategy is the regulatory requirement that each individual drug be shown to be safe in the form of individual agents and combinations (Hopkins, Nat Chem Biol. 2008; 4:682-90).

An alternative strategy for multi-target therapy is to design a single compound with selective multi-target pharmacology (multi-targeted drugs). Many approved drugs have been shown to act on multiple targets. In terms of fair pharmacokinetics and biodistribution, administration of a single compound may have advantages over drug combinations. In fact, due to the incompatible pharmacokinetics between the components of combination therapy, the trough of drug exposure can create a low-dose opportunity window in which the reduced selection pressure can lead to drug resistance. As far as drug registration is concerned, the regulatory barriers to approving a single compound acting on multiple targets are significantly lower than approving new drug combinations (Hopkins, 2008, supra).

Therefore, the present application relates to the advantage of having dual activity of the α ₂ δ-1 subunit of the μ-receptor and the voltage-gated calcium channel in the same molecule to treat chronic pain.

In this way, the present invention relates to compounds with complementary dual action mechanisms (μ-receptor agonists and α ₂ δ subunits of voltage-gated calcium channels, specifically α ₂ δ-1 subunit blockers) , Which means better tolerance characteristics than strong opioids (morphine, oxycodone, fentanyl, etc.), and/or more than gabapentin (pregabalin and gabapentin) Good performance and tolerance.

Pain is multimodal in nature, because in almost all pain states, it involves several mediators, signaling pathways, and molecular mechanisms. Therefore, monomodal therapy cannot provide complete pain relief. Currently, combining existing therapies is a common clinical practice and many efforts are aimed at evaluating the best combination of drugs available in clinical studies (Mao, J., Gold, MS, Backonja, M.; 2011; J. Pain; 12; 157-166 ).

Therefore, there is still a need to find compounds that have alternative or improved pharmacological activity in the treatment of pain, are both effective and show desired selectivity, and have good "pharmacological" properties, that is, good medicines related to administration, distribution, metabolism, and excretion nature.

The authors of the present invention have found that both the α ₂ δ subunit of the voltage-gated calcium channel (specifically the α ₂ δ-1 subunit) and the μ-opioid receptor (MOR or μ-opioid receptor) show A series of compounds with dual pharmacological activity, providing innovative, effective and alternative solutions for the treatment of pain.

In view of the current results of currently available therapies and clinical practice, the present invention provides a solution by combining in a single compound that is bound to two different targets related to pain treatment. This is mainly achieved by providing the compounds according to the invention, which bind both the μ-opioid receptor and the α ₂ δ subunit of the voltage-gated calcium channel (specifically the α ₂ δ-1 subunit ) Combine.

In the present invention, the family of structurally different aminopropoxyphenyl and benzyl 1-oxa-4,9-diazaspiroundecane derivatives covered by formula (I) is identified, which It has dual pharmacological activity on the α ₂ δ subunit (specifically α ₂ δ-1 subunit) and µ-opioid receptors of voltage-gated calcium channels, so by providing these dual compounds, the identification of substitution or improvement is solved The above problems of pain treatment.

The main object of the present invention is to provide a compound having dual activity bound to a voltage-gated calcium channel α ₂ δ subunit (specifically α ₂ δ-1 subunit) and a µ-opioid receptor for use in therapy pain.

Since the present invention aims to provide a compound or a chemically related compound which is used as a double ligand of α ₂ δ subunit (specifically, α ₂ δ-1 subunit) and µ-opioid receptor for voltage-gated calcium channels Series, so if the compound has a bond expressed as K _i corresponding to the following measure, it is an excellent embodiment: K _i (µ) is preferably <1000 nM, more preferably <500 nM, and even better <100 nM.

K _i (α ₂ δ-1) is preferably &lt; 10000 nM, more preferably &lt; 5000 nM, even more preferably &lt; 500 nM or even better &lt; 100 nM.

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 、Y₂ 及n係如下文詳細說明中所定義。The present invention relates to the compound of general formula (I) in the main aspect,

Wherein R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ , Y ₂ and n are as defined in the detailed description below.

A further object of the invention refers to a method for preparing compounds of general formula (I).

A further object of the invention refers to the use of intermediate compounds, which are used to prepare compounds of general formula (I).

The object of the present invention is also a pharmaceutical composition comprising a compound of formula (I).

Finally, the object of the present invention is the use of the compound as a medicament and more specifically for the treatment of pain and pain-related conditions.

In the present invention, the family of structurally different aminopropoxyphenyl and benzyl 1-oxa-4,9-diazaspiroundecane derivatives covered by formula (I) is identified, which It has dual pharmacological activity on the α ₂ δ subunit (specifically α ₂ δ-1 subunit) and µ-opioid receptors of voltage-gated calcium channels, so by providing these dual compounds, the identification of substitution or improvement is solved The above problems of pain treatment.

The main object of the present invention is to provide a compound having dual activity bound to a voltage-gated calcium channel α ₂ δ subunit (specifically α ₂ δ-1 subunit) and a µ-opioid receptor for use in therapy pain.

Since the present invention aims to provide a compound or a chemically related compound used as a dual ligand of α ₂ δ subunit (specifically α ₂ δ-1 subunit) and µ-opioid receptor for voltage-gated calcium channels Series, so if the compound has a bond expressed as K _i corresponding to the following measure, it is an excellent embodiment:

K _i (µ) is preferably <1000 nM, more preferably <500 nM, even better <100 nM.

K _i (α ₂ δ-1) is preferably &lt; 10000 nM, more preferably &lt; 5000 nM, even more preferably &lt; 500 nM or even better &lt; 100 nM.

The applicant was surprised to find that by using a multi-mode balanced analgesic method combining two different synergistic activities in a single drug (ie, dual ligands, which have dual functions and bind to μ-opioid receptors and voltage-gated calcium The α ₂ δ subunit of the channel, specifically the α ₂ δ-1 subunit), can solve the problem of providing new effective and alternative treatments for pain and pain-related diseases, thereby enhancing enhancement by α ₂ δ block without increasing undesirable Side effects. This supports the therapeutic value of dual agents, where the α ₂ δ binding component is used as an inherent adjuvant for the MOR binding component.

The dual compound with binding to the μ-opioid receptor and the α ₂ δ subunit of the voltage-gated calcium channel shows high therapeutic potential by achieving excellent analgesia (enhanced in the efficacy of the individual opioid component), and Relative to existing opioid therapies with reduced side-effect properties (increased safety margin compared to opioid components alone).

Advantageously, the dual compound according to the invention will additionally exhibit one or more of the following functions: blocking the α ₂ δ subunit of the voltage-gated calcium channel (specifically the α ₂ δ-1 subunit) and the μ-opioid receptor Excited.

However, it should be noted that the functions "antagonism" and "agonism" are also subdivided into sub-functions such as partial activation or inverse activation in their effects. Therefore, the function of the compound should be considered within a relatively wide bandwidth.

Antagonists block or buffer agonist-mediated responses. It is known that the sub-function is a neutral antagonist or inverse agonist.

Agonists increase the activity of the receptor above its basic level. It is known that sub-functions are full agonists or partial agonists.

In addition, the two mechanisms are complementary to each other, because MOR agonists are only minimally effective in the treatment of neuropathic pain, and the voltage-gated calcium channel α ₂ δ subunit (specifically the α ₂ δ-1 subunit ) Blockers show excellent effects in preclinical neuropathic pain models. Therefore, the α ₂ δ component, specifically the α ₂ δ-1 component, adds a unique analgesic effect in opioid-resistant pain. Finally, the dual approach has significant advantages over MOR agonists in the treatment of chronic pain. This is due to the enhanced analgesia without adverse events of MOR agonists, requiring a lower and better tolerated dose.

Another advantage of using multi-ligand design is a lower risk of drug-drug interactions compared to mixed or multi-component drugs, thus involving simpler pharmacokinetics and less variability between patients . In addition, by addressing more complex causes, this method can improve patient compliance and expand therapeutic applications related to single-mechanism drugs. It is also seen as a method of improving the R&D output obtained using the "one drug-one target" method, which has been questioned in the past few years [Bornot A, Bauer U, Brown A, Firth M, Hellawell C, Engkvist O. Systematic Exploration of Dual-Acting Modulators from a Combined Medicinal Chemistry and Biology Perspective. J. Med. Chem , 56, 1197-1210 (2013)].

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₂ 選自經取代或未經取代之芳基及經取代或未經取代之雜環基， R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； 根據本發明之該等化合物視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In its broadest form, the invention relates to compounds of general formula (I):

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O) -C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or Unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _{10 '''} )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10′′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclic, R _{3 is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkane Group and substituted or unsubstituted alkylcycloalkyl; R _3'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and Substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C( O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O ) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _{2 -6} alkynyl and substituted or unsubstituted cycloalkyl; these compounds according to the present invention are optionally stereoisomers, preferably mirror isomers or diastereomers, exo In the form of rotates, or in the form of mixtures of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates Thing.

Please note that "or its corresponding salt" also means "or its corresponding pharmaceutically acceptable salt". This applies to all the following examples and the use of "salts" is therefore equivalent to "pharmaceutically acceptable salts".

In another embodiment, the compounds according to the invention are optionally in the form of stereoisomers, preferably enantiomers or diastereomers, racemates, or in stereoisomeric forms At least two of the structure, preferably mirror image isomer and/or diastereomer are in the form of a mixture in any mixing ratio, or in the form of their corresponding salts.

In certain embodiments, the following premises apply: When Y is CO, then R _{6 is} not -C(O)R ₇ .

In certain embodiments, the following premises apply: When R ₆ is -C(O)R ₇ , then Y is not CO.

In certain embodiments, the following premises apply: When R ₆ is -C(O)R ₇ , then Y is -CH ₂ -.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₂ 選自經取代或未經取代之芳基及經取代或未經取代之雜環基， 其中R₂ 中之該芳基或雜環基若經取代則經一或多個選自以下之取代基取代：鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention is a compound of general formula (I)

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O) -C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or Unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _{10 '''} )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10′′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Or, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl, or alkynyl group defined in R ₅ and R _5′ is substituted by one or more Substituted by a substituent selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; wherein the ring is as defined in R ₅ or alkylcycloalkyl If the alkyl group is substituted, it is substituted with one or more substituents selected from: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O) R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S( O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' , -OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the (etc.) substituent is preferably selected from halogen, -R ₅₁ , -OR ₅₁ ,- NR ₅₁ R _51' , -CN, haloalkyl and haloalkoxy; wherein R ₅₁ , R _51' and R _{51'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the cycloalkyl group as defined in R ₅ -R _5′ is substituted by one or Substitution with multiple substituents selected from: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' , -NR ₅₂ S( O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O ) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -OCH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ , -OR ₅₂ , -NR ₅₂ R _52' , -CN, haloalkyl and haloalkoxy; wherein R ₅₂ , R _52' and R _{52'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkane Group, substituted or unsubstituted aryl group, substituted or unsubstituted alkyl aryl group, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group and -C (O) R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, haloalkyl , Haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic group as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups Substitution is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O)R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the substituent(s) are preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein _R61 , _R61' and _{R61'' are} independently selected from hydrogen, substituted or unsubstituted _C1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted Substituted aryl, substituted or unsubstituted alkylaryl, Substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by one or more selected from Substituted by the following substituents: -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₇₁ R _71' ; where as in R ₇ , also alkylcycloalkyl, alkylaryl and alkyl If the cycloalkyl group, aryl group and heterocyclic group defined in the radical heterocyclic group are substituted, they are substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ ,- NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C( O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ ; the (etc.) The substituent is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71'' are} independently selected From hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen , Halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR ₈₁ ; R _8'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _8, or as defined in the R _{8 'of} the alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkyl, haloalkoxy Radical and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and Substituted or unsubstituted C _2-6 alkynyl; R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocycle in R ₂ If the group is substituted, it is substituted with one or more substituents selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _{21 '} , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein, R If the alkyl, alkenyl or alkynyl group defined in ₃ is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also an alkylcycloalkyl group is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₃₁ ,- OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' ,- NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C( O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _31' R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; The substituent(s) is preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and haloalkoxy; wherein R ₃₁ , R _31' and R _31'' Independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _3'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein, R _{3 'is} defined of the alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _32, halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O ) NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' is} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl And substituted or unsubstituted cycloalkyl; also if the alkyl, alkenyl or alkynyl in alkylaryl, alkylheterocyclic or alkylcycloalkyl is substituted and the substitution has not been otherwise defined, Then it is substituted with one or more substituents selected from: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₁₃ R _13' ; where R ₁₃ and R _13' Independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also alkylaryl, alkylheterocyclyl Or if the aryl, heterocyclic group or cycloalkyl group in the alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, halogen,- R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S(O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S(O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy , -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S(O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl, and unsubstituted heterocycle Radical; optionally in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or At least two of the diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X及n係如詳細說明中所定義， 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^′ )

Where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X and n are as defined in the detailed description, stereo stereoisomers, preferably mirror image isomers or non-mirror One of the structures, in the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or Its corresponding salt, or its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₂ 選自經取代或未經取代之芳基及經取代或未經取代之雜環基， R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^′ )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Substituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclic, R _{3 is} selected from Hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted Cycloalkyl and substituted or unsubstituted alkylcycloalkyl; R _3'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR _{4 1} C(O)NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O ) OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or un Substituted C _2-6 alkynyl and substituted or unsubstituted cycloalkyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers, racemates In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₂ 選自經取代或未經取代之芳基及經取代或未經取代之雜環基， 其中R₂ 中之該芳基或雜環基若經取代則經一或多個選自以下之取代基取代：鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^′ )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O) -C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by One or more substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; where as in R ₅ or alkyl cycloalkyl If the defined cycloalkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' ,- OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ ,- _{oR 51, -NR 51 R 51 '} , -CN, haloalkyl and haloalkoxy; wherein R _51, R _51' and R _{51 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein such R ₅ -R _{5 'of} the defined substituted cycloalkyl group if Is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' ,- NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -O CH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ ,- _{oR 52, -NR 52 R 52 '} , -CN, haloalkyl and haloalkoxy; wherein R _52, R _52' and R _{52 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, halogen Alkyl, haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic ring as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups If the group is substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O ) R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted Alkylaryl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by a Or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; wherein as in R ₇ , alkylcycloalkyl, alkyl The cycloalkyl, aryl and heterocyclic groups defined in the arylaryl and alkyl heterocyclic groups are substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C (O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ The substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein R ₈ or R _{8 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkoxy Group, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein R ₂ If substituted, the aryl or heterocyclic group is substituted with one or more substituents selected from the group consisting of halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O )R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl; wherein , If the alkyl, alkenyl, or alkynyl group defined in R ₃ is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also an alkylcycloalkyl group is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy,- C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _31' R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) is preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' is} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl ; R _3'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; wherein, R _{3 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR ₃₂ , Halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ ,- C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; of which R ₄₁ , R _{41 '} And R _{41'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _{2- 6} Alkynyl and substituted or unsubstituted cycloalkyl; also the alkyl, alkenyl or alkynyl in alkylaryl, alkylheterocyclic or alkylcycloalkyl is substituted and the substitution has not been Otherwise defined, it is substituted with one or more substituents selected from: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₁₃ R _13' ; where R ₁₃ and R _{13' is} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also alkylaryl, alkyl If the aryl, heterocyclic or cycloalkyl group in the heterocyclic group or alkylcycloalkyl group is substituted and the substitution has not been otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, Halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S(O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S(O) ₂ R ₁₄ , -CN, haloalkyl, halo Alkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S(O) ₂ NR _14' R _14'' and -C( CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, Unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted Substituted heterocyclic groups; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in stereoisomers, preferably mirror isomers At least two of the compounds and/or diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

其中R₁ 、R₃ 、R_3’ 、R₄ 、R_4’ 、R₉ 、R_9’ 、X、Y₁ 、Y₂ 及n係如詳細說明中所定義， 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is ^a compound of the general formula (I ^a )

Where R ₁ , R ₃ , R _3' , R ₄ , R _4' , R ₉ , R _9' , X, Y ₁ , Y ₂ and n are as defined in the detailed description, and are stereoisomers as appropriate, One of the preferred enantiomers or diastereomers, racemates, or at least two of stereoisomers, preferred enantiomers and/or diastereomers In the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_{4 ’} 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is ^a compound of the general formula (I ^a )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O) -C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or Unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _{10 '''} )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10′′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R _{3′ is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _{4 ′ are} independently selected From halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S( O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; wherein R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or Unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is ^a compound of the general formula (I ^a )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O) -C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or Unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _{10 '''} )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10′′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by One or more substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; where as in R ₅ or alkyl cycloalkyl If the defined cycloalkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' ,- OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ ,- _{oR 51, -NR 51 R 51 '} , -CN, haloalkyl and haloalkoxy; wherein R _51, R _51' and R _{51 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein such R ₅ -R _{5 'of} the defined substituted cycloalkyl group if Is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' ,- NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -O CH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ ,- _{oR 52, -NR 52 R 52 '} , -CN, haloalkyl and haloalkoxy; wherein R _52, R _52' and R _{52 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, halogen Alkyl, haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic ring as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups If the group is substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O ) R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted Alkylaryl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by a Or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; wherein as in R ₇ , also alkylcycloalkyl, alkyl The cycloalkyl, aryl and heterocyclic groups defined in the arylaryl and alkyl heterocyclic groups are substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C (O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ The substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein R ₈ or R _{8 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkoxy Group, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl group as defined in R ₃ If a group, alkenyl group or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , Halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also alkylcycloalkyl is substituted by one or more selected from Substituted by the following substituents: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _{31 '} R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and Haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and A substituted or unsubstituted C _2-6 alkynyl group; wherein, if the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted, it is substituted with one or more substituents selected from: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O ) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkane Radicals; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O ) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; also the alkyl in alkylaryl, alkyl heterocyclic or alkylcycloalkyl If a group, alkenyl group or alkynyl group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkane Oxygen and -NR ₁₃ R _13' ; wherein R ₁₃ and R _{13' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also if the aryl, heterocyclyl or cycloalkyl in alkylaryl, alkylheterocyclyl or alkylcycloalkyl is substituted and the substitution has not been otherwise defined, Or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S (O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S( O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S( O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, Unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted ring Alkyl and unsubstituted heterocyclic groups; optionally in the form of stereoisomers, preferably mirror image isomers or diastereomers, racemates, or stereoisomers, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

其中R₁ 、R₃ 、R_3’ 、R₄ 、R_4’ 、R₉ 、R_9’ 、X及n係如詳細說明中所定義， 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^a ′)

Wherein R ₁ , R ₃ , R _3' , R ₄ , R _4' , R ₉ , R _9' , X and n are as defined in the detailed description, stereo stereoisomers, preferably mirror-image isomers, as the case may be Or one of the diastereomers, racemates, or a mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^a ′)

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R _{3′ is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _{4′ are} independently selected From halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S(O ) R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; wherein R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or unsubstituted Substituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _{21 '} R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted Or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; one of stereoisomers, preferably mirror isomers or diastereomers as the case may be , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^a ′)

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by One or more substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; where as in R ₅ or alkyl cycloalkyl If the defined cycloalkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' ,- OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ ,- _{oR 51, -NR 51 R 51 '} , -CN, haloalkyl and haloalkoxy; wherein R _51, R _51' and R _{51 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein such R ₅ -R _{5 'of} the defined substituted cycloalkyl group if Is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' ,- NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -O CH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ ,- _{oR 52, -NR 52 R 52 '} , -CN, haloalkyl and haloalkoxy; wherein R _52, R _52' and R _{52 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, halogen Alkyl, haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic ring as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups If the group is substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O ) R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted Alkylaryl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by a Or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; wherein as in R ₇ , also alkylcycloalkyl, alkyl The cycloalkyl, aryl and heterocyclic groups defined in the arylaryl and alkyl heterocyclic groups are substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C (O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ The substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein R ₈ or R _{8 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkoxy Group, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl group as defined in R ₃ If a group, alkenyl group or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , Halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also alkylcycloalkyl is substituted by one or more selected from Substituted by the following substituents: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _{31 '} R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and Haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and A substituted or unsubstituted C _2-6 alkynyl group; wherein, if the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted, it is substituted with one or more substituents selected from: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O ) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkane Radicals; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O ) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; also the alkyl in alkylaryl, alkyl heterocyclic or alkylcycloalkyl If a group, alkenyl group or alkynyl group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkane Oxygen and -NR ₁₃ R _13' ; wherein R ₁₃ and R _{13' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also if the aryl, heterocyclyl or cycloalkyl in alkylaryl, alkylheterocyclyl or alkylcycloalkyl is substituted and the substitution has not been otherwise defined, Or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S (O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S( O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S( O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, Unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted ring Alkyl and unsubstituted heterocyclic groups; optionally in the form of stereoisomers, preferably mirror image isomers or diastereomers, racemates, or stereoisomers, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

其中R₁ 、R₃ 、R_3’ 、R₄ 、R_4’ 、R₉ 、R_9’ 、X、Y₁ 、Y₂ 及n係如下文詳細說明中所定義， 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^b )

Where R ₁ , R ₃ , R _3' , R ₄ , R _4' , R ₉ , R _9' , X, Y ₁ , Y ₂ and n are as defined in the detailed description below, and are stereoisomers as appropriate , One of the preferred enantiomers or diastereomers, racemates, or at least two of the stereoisomers, preferred enantiomers and/or diastereomers They are in the form of mixtures of any mixing ratio, or their corresponding salts, or their corresponding solvates.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_{4 ’} 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^b )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted Or unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _10''' )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkene Group and substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10″′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R _{3′ is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _{4 ′ are} independently selected From halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S( O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; wherein R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or Unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^b )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted Or unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _10''' )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkene Group and substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10″′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by One or more substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; where as in R ₅ or alkyl cycloalkyl If the defined cycloalkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' ,- OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ ,- _{oR 51, -NR 51 R 51 '} , -CN, haloalkyl and haloalkoxy; wherein R _51, R _51' and R _{51 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein such R ₅ -R _{5 'of} the defined substituted cycloalkyl group if Is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' ,- NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -O CH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ ,- _{oR 52, -NR 52 R 52 '} , -CN, haloalkyl and haloalkoxy; wherein R _52, R _52' and R _{52 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, halogen Alkyl, haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic ring as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups If the group is substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O ) R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted Alkylaryl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by a Or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; wherein as in R ₇ , also alkylcycloalkyl, alkyl The cycloalkyl, aryl and heterocyclic groups defined in the arylaryl and alkyl heterocyclic groups are substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C (O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ The substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein R ₈ or R _{8 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkoxy Group, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl group as defined in R ₃ If a group, alkenyl group or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , Halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also alkylcycloalkyl is substituted by one or more selected from Substituted by the following substituents: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _{31 '} R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and Haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and A substituted or unsubstituted C _2-6 alkynyl group; wherein, if the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted, it is substituted with one or more substituents selected from: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O ) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkane Radicals; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O ) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; also the alkyl in alkylaryl, alkyl heterocyclic or alkylcycloalkyl If a group, alkenyl group or alkynyl group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkane Oxygen and -NR ₁₃ R _13' ; wherein R ₁₃ and R _{13' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also if the aryl, heterocyclyl or cycloalkyl in alkylaryl, alkylheterocyclyl or alkylcycloalkyl is substituted and the substitution has not been otherwise defined, Or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S (O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S( O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S( O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, Unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted ring Alkyl and unsubstituted heterocyclic groups; optionally in the form of stereoisomers, preferably mirror image isomers or diastereomers, racemates, or stereoisomers, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

其中R₁ 、R₃ 、R_3’ 、R₄ 、R_4’ 、R₉ 、R_9’ 、X及n係如下文詳細說明中所定義， 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^b ′)

Wherein R ₁ , R ₃ , R _3' , R ₄ , R _4' , R ₉ , R _9' , X and n are as defined in the detailed description below, stereo stereoisomers, preferably mirror image isomers, as the case may be One of the compounds or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

(I^b’ )， 其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^b ′)

(I ^b' ), where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C( O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _{a is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _{2- 6} alkynyl; R _{b is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _{2- 6} alkynyl; alternatively, R _a and R _b together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkane Group and -C(O)-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁ Series

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R _{3′ is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _{4′ are} independently selected From halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S(O ) R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; wherein R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or unsubstituted Substituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _{21 '} R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted Or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; one of stereoisomers, preferably mirror isomers or diastereomers as the case may be , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^b ′)

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by One or more substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; where as in R ₅ or alkyl cycloalkyl If the defined cycloalkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' ,- OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ ,- _{oR 51, -NR 51 R 51 '} , -CN, haloalkyl and haloalkoxy; wherein R _51, R _51' and R _{51 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein such R ₅ -R _{5 'of} the defined substituted cycloalkyl group if Is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' ,- NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -O CH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ ,- _{oR 52, -NR 52 R 52 '} , -CN, haloalkyl and haloalkoxy; wherein R _52, R _52' and R _{52 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, halogen Alkyl, haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic ring as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups If the group is substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O ) R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted Alkylaryl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by a Or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; wherein as in R ₇ , also alkylcycloalkyl, alkyl The cycloalkyl, aryl and heterocyclic groups defined in the arylaryl and alkyl heterocyclic groups are substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C (O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ The substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein R ₈ or R _{8 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkoxy Group, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl group as defined in R ₃ If a group, alkenyl group or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , Halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also alkylcycloalkyl is substituted by one or more selected from Substituted by the following substituents: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _{31 '} R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and Haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and A substituted or unsubstituted C _2-6 alkynyl group; wherein, if the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted, it is substituted with one or more substituents selected from: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O ) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkane Radicals; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O ) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; also the alkyl in alkylaryl, alkyl heterocyclic or alkylcycloalkyl If a group, alkenyl group or alkynyl group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkane Oxygen and -NR ₁₃ R _13' ; wherein R ₁₃ and R _{13' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also if the aryl, heterocyclyl or cycloalkyl in alkylaryl, alkylheterocyclyl or alkylcycloalkyl is substituted and the substitution has not been otherwise defined, Or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S (O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S( O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S( O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, Unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted ring Alkyl and unsubstituted heterocyclic groups; optionally in the form of stereoisomers, preferably mirror image isomers or diastereomers, racemates, or stereoisomers, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

(I^c )， 其中R₁ 、R₃ 、R_3’ 、R₄ 、R_4’ 、R₉ 、R_9’ 、X、Y₁ 、Y₂ 及n係如下文詳細說明中所定義， 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^c )

(I ^c ), where R ₁ , R ₃ , R _3' , R ₄ , R _4' , R ₉ , R _9' , X, Y ₁ , Y ₂ and n are as defined in the detailed description below, as appropriate In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_{4 ’} 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^c )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted Or unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _10''' )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkene Group and substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10″′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R _{3′ is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _{4 ′ are} independently selected From halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S( O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; wherein R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or Unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； Y₁ 係-C(R₁₀ R_10’ )-； 其中R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₁₀ 及R_10’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； Y₂ 係-C(R_10’’ R_10’’’ )-； 其中R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_10’’ 及R_10’’’ 可與其連接之碳原子一起形成經取代或未經取代之環烷基； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of the general formula (I) is a compound of the general formula (I ^c )

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted Or unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; Y ₂ is -C(R _10'' R _10''' )-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkene Group and substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10″′ may form a substituted or unsubstituted cycloalkyl together with the carbon atom to which they are attached; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by One or more substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; where as in R ₅ or alkyl cycloalkyl If the defined cycloalkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' ,- OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ ,- _{oR 51, -NR 51 R 51 '} , -CN, haloalkyl and haloalkoxy; wherein R _51, R _51' and R _{51 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein such R ₅ -R _{5 'of} the defined substituted cycloalkyl group if Is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' ,- NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -O CH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ ,- _{oR 52, -NR 52 R 52 '} , -CN, haloalkyl and haloalkoxy; wherein R _52, R _52' and R _{52 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, halogen Alkyl, haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic ring as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups If the group is substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O ) R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted Alkylaryl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by a Or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; wherein as in R ₇ , also alkylcycloalkyl, alkyl The cycloalkyl, aryl and heterocyclic groups defined in the arylaryl and alkyl heterocyclic groups are substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C (O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ The substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein R ₈ or R _{8 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkoxy Group, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl group as defined in R ₃ If a group, alkenyl group or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , Halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also alkylcycloalkyl is substituted by one or more selected from Substituted by the following substituents: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _{31 '} R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and Haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and A substituted or unsubstituted C _2-6 alkynyl group; wherein, if the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted, it is substituted with one or more substituents selected from: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O ) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkane Radicals; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O ) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; also the alkyl in alkylaryl, alkyl heterocyclic or alkylcycloalkyl If a group, alkenyl group or alkynyl group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkane Oxygen and -NR ₁₃ R _13' ; wherein R ₁₃ and R _{13' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also if the aryl, heterocyclyl or cycloalkyl in alkylaryl, alkylheterocyclyl or alkylcycloalkyl is substituted and the substitution has not been otherwise defined, Or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S (O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S( O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S( O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, Unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted ring Alkyl and unsubstituted heterocyclic groups; optionally in the form of stereoisomers, preferably mirror image isomers or diastereomers, racemates, or stereoisomers, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

其中R₁ 、R₃ 、R_3’ 、R₄ 、R_4’ 、R₉ 、R_9’ 、X及n係如下文詳細說明中所定義， 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^c ′)

Wherein R ₁ , R ₃ , R _3' , R ₄ , R _4' , R ₉ , R _9' , X and n are as defined in the detailed description below, stereo stereoisomers, preferably mirror image isomers, as the case may be One of the compounds or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中R₈₁ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_{4 ’} 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^c ′)

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R _{3′ is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _{4 ′ are} independently selected From halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S( O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; wherein R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or Unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

其中 X選自鍵、-[C(R_a R_b )]_p -、-[CH₂ ]_p C(O)[CH₂ ]_q -、-[CH₂ ]_p C(O)N(R_z )[CH₂ ]_q -、-[CH₂ ]_p N(R_z )C(O)[CH₂ ]_q -及-[CH₂ ]_p N(R_z )[CH₂ ]_q -； R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R_a 及R_b 與其連接之碳原子一起可形成經取代或未經取代之環烷基； R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； p係0、1、2、3、4或5； q係0、1、2、3、4或5； n係0或1； R₁ 係

； 其中 m係0、1或2； r係0、1或2； Y係-CH₂ -或C=O； R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 或者，R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 R₅ 及R_5’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₅₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₅₁ R_51’ ； 其中如R₅ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₁ 、-OR₅₁ 、-NO₂ 、-NR₅₁ R_51’ 、-NR₅₁ C(O)R_51’ 、-NR₅₁ S(O)₂ R_51’ 、-S(O)₂ NR₅₁ R_51’ 、-NR₅₁ C(O)NR_51’ R_51’’ 、-SR₅₁ 、-S(O)R₅₁ 、-S(O)₂ R₅₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₁ 、-C(O)NR₅₁ R_51’ 、-OCH₂ CH₂ OR₅₁ 、-NR₅₁ S(O)₂ NR_51’ R_51’’ 及-C(CH₃ )₂ OR₅₁ ；該(等)取代基較佳選自鹵素、-R₅₁ 、-OR₅₁ 、-NR₅₁ R_51’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中如R₅ -R_5’ 中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₅₂ 、-OR₅₂ 、-NO₂ 、-NR₅₂ R_52’ 、-NR₅₂ C(O)R_52’ 、-NR₅₂ S(O)₂ R_52’ 、-S(O)₂ NR₅₂ R_52’ 、-NR₅₂ C(O)NR_52’ R_52’’ 、-SR₅₂ 、-S(O)R₅₂ 、-S(O)₂ R₅₂ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₅₂ 、-C(O)NR₅₂ R_52’ 、-OCH₂ CH₂ OR₅₂ 、-NR₅₂ S(O)₂ NR_52’ R_52’’ 及-C(CH₃ )₂ OR₅₂ ；該(等)取代基較佳選自鹵素、-R₅₂ 、-OR₅₂ 、-NR₅₂ R_52’ 、-CN、鹵烷基及鹵烷氧基； 其中R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 R₆ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₆₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₆₁ R_61’ ； 其中 R₆ 中、亦烷基環烷基、烷基芳基及烷基雜環基中定義之該環烷基、芳基或雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₆₁ 、-OR₆₁ 、-NO₂ 、-NR₆₁ R_61’ 、-NR₆₁ C(O)R_61’ 、-NR₆₁ S(O)₂ R_61’ 、-S(O)₂ NR₆₁ R_61’ 、-NR₆₁ C(O)NR_61’ R_61’’ 、-SR₆₁ 、-S(O)R₆₁ 、-S(O)₂ R₆₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₆₁ 、-C(O)NR₆₁ R_61’ 、-OCH₂ CH₂ OR₆₁ 、-NR₆₁ S(O)₂ NR_61’ R_61’’ 及-C(CH₃ )₂ OR₆₁ ；該(等)取代基較佳選自鹵素、-R₆₁ 、-OR₆₁ 、-NR₆₁ R_61’ 、-CN、鹵烷基及鹵烷氧基； 其中R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 R₇ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₇₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₇₁ R_71’ ； 其中 如R₇ 中、亦烷基環烷基、烷基芳基及烷基雜環基中所定義之該環烷基、芳基及雜環基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₇₁ 、-OR₇₁ 、-NO₂ 、-NR₇₁ R_71’ 、-NR₇₁ C(O)R_71’ 、-NR₇₁ S(O)₂ R_71’ 、-S(O)₂ NR₇₁ R_71’ 、-NR₇₁ C(O)NR_71’ R_71’’ 、-SR₇₁ 、-S(O)R₇₁ 、-S(O)₂ R₇₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₇₁ 、-C(O)NR₇₁ R_71’ 、-OCH₂ CH₂ OR₇₁ 、-NR₇₁ S(O)₂ NR_71’ R_71’’ 及-C(CH₃ )₂ OR₇₁ ；該(等)取代基較佳選自鹵素、-R₇₁ 、-OR₇₁ 、-NR₇₁ R_71’ 、-CN、鹵烷基及鹵烷氧基； 其中R₇₁ 、R_71’ 及R_71’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 R₈ 或R_8’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₈₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₈₁ R_81’ ； 其中R₈₁ 及R_81’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中， R₃ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₁ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₁ R_31’ ； 其中R₃ 中、亦烷基環烷基中定義之該環烷基若經取代則經一或多個選自以下之取代基取代：=O、鹵素、-R₃₁ 、-OR₃₁ 、-NO₂ 、-NR₃₁ R_31’ 、-NR₃₁ C(O)R_31’ 、-NR₃₁ S(O)₂ R_31’ 、-S(O)₂ NR₃₁ R_31’ 、-NR₃₁ C(O)NR_31’ R_31’’ 、-SR₃₁ 、-S(O)R₃₁ 、-S(O)₂ R₃₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₃₁ 、-C(O)NR₃₁ R_31’ 、-OCH₂ CH₂ OR₃₁ 、-NR₃₁ S(O)₂ NR_31’ R_31’’ 及-C(CH₃ )₂ OR₃₁ ；該(等)取代基較佳選自鹵素、-R₃₁ 、-OR₃₁ 、-NR₃₁ R_31’ 、-CN、鹵烷基及鹵烷氧基； 其中R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中， R_3’ 中定義之該烷基、烯基或炔基若經取代則經一或多個選自以下之取代基取代：-OR₃₂ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₃₂ R_32’ ； 其中R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該烷基、烯基或炔基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、-OR₁₃ 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR₁₃ R_13’ ； 其中R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 亦烷基芳基、烷基雜環基或烷基環烷基中之該芳基、雜環基或環烷基若經取代且該取代尚未另外定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R₁₄ 、-OR₁₄ 、-NO₂ 、-NR₁₄ R_14’ 、-NR₁₄ C(O)R_14’ 、-NR₁₄ S(O)₂ R_14’ 、-S(O)₂ NR₁₄ R_14’ 、-NR₁₄ C(O)NR_14’ R_14’’ 、-SR₁₄ 、-S(O)R₁₄ 、-S(O)₂ R₁₄ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₁₄ 、-C(O)NR₁₄ R_14’ 、-OCH₂ CH₂ OR₁₄ 、-NR₁₄ S(O)₂ NR_14’ R_14’’ 及-C(CH₃ )₂ OR₁₄ ； 其中R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I ^c ′)

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached can form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O )-C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by One or more substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; where as in R ₅ or alkyl cycloalkyl If the defined cycloalkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' ,- OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ ,- _{oR 51, -NR 51 R 51 '} , -CN, haloalkyl and haloalkoxy; wherein R _51, R _51' and R _{51 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein such R ₅ -R _{5 'of} the defined substituted cycloalkyl group if Is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' ,- NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -O CH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ ,- _{oR 52, -NR 52 R 52 '} , -CN, haloalkyl and haloalkoxy; wherein R _52, R _52' and R _{52 ''} are independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, halogen Alkyl, haloalkoxy and -NR ₆₁ R _61' ; wherein the cycloalkyl, aryl or heterocyclic ring as defined in R ₆ and also alkylcycloalkyl, alkylaryl and alkylheterocyclic groups If the group is substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O ) R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted Alkylaryl, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by a Or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; wherein as in R ₇ , also alkylcycloalkyl, alkyl The cycloalkyl, aryl and heterocyclic groups defined in the arylaryl and alkyl heterocyclic groups are substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C (O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ The substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or unsubstituted C _2-6 alkenyl group and the substituted or non-substituted C _2-6 alkynyl; wherein R ₈ or R _{8 'of} the defined alkyl, alkenyl or alkynyl group, if substituted is substituted with one or more substituents selected from the following group of substituents: -OR _81, halogen, -CN, haloalkoxy Group, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl group as defined in R ₃ If a group, alkenyl group or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , Halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also alkylcycloalkyl is substituted by one or more selected from Substituted by the following substituents: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _{31 '} R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and Haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and A substituted or unsubstituted C _2-6 alkynyl group; wherein, if the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted, it is substituted with one or more substituents selected from: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _4'are independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O ) NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkane Radicals; R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O ) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; also the alkyl in alkylaryl, alkyl heterocyclic or alkylcycloalkyl If a group, alkenyl group or alkynyl group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkane Oxygen and -NR ₁₃ R _13' ; wherein R ₁₃ and R _{13' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; also if the aryl, heterocyclyl or cycloalkyl in alkylaryl, alkylheterocyclyl or alkylcycloalkyl is substituted and the substitution has not been otherwise defined, Or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _14' , -NR ₁₄ C(O)R _14' , -NR ₁₄ S (O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S( O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S( O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; wherein R ₁₄ , R _14' and R _{14'' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, Unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted ring Alkyl and unsubstituted heterocyclic groups; optionally in the form of stereoisomers, preferably mirror image isomers or diastereomers, racemates, or stereoisomers, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

For clarity, all groups and definitions described and referred to in this description and in the compounds of general formula (I) also apply to general Markush formulas (I'), (I ^a ), (I ^a' ), (I ^b ), (I ^b' ), (I ^c ) and (I ^c' ) compounds (where applicable), and when their groups are present in the general maku mentioned When in the formula, it is applicable to all synthetic intermediates, this is because the general Markush formula (I'), (I ^a ), (I ^a' ), (I ^b ), (I ^b' ), (I ^c ) And (I ^c' ) compounds are included within the broader definition of the general Markush formula (I).

等價於

其中僅-CH₂ -包括於括號中，且n意味著-CH₂ -重複之次數。在適用時，同樣將適用於一般馬庫什式(I’)、(I^a )、(I^a’ )、(I^b )、(I^b’ )、(I^c )及(I^c’ )以及所有合成中間體。For clarity, the general Markush formula (I)

Equivalent to

Among them, only -CH ₂ -is included in parentheses, and n means the number of times -CH ₂ -is repeated. When applicable, the same applies to general Markush formulas (I'), (I ^a ), (I ^a' ), (I ^b ), (I ^b' ), (I ^c ) and (I ^c' ) And all synthetic intermediates.

In addition, and for the sake of clarity, it should be further understood that, of course, if n is 0, the oxygen atom and/or phenyl group still exists in the general Markush formula (I'), (I ^a ), (I ^{a '} ), (I ^b ), (I ^b' ), (I ^c ) and (I ^c' ), and applicable to all synthetic intermediates.

For clarity, such as "R ₅ -R _{5 'in} the ring" means that when R ₅ and R _5' form a ring together with the atoms generated at the time of connection thereto. Then, the ring may be substituted or unsubstituted. This definition is also generally available and can also be applied as the definition of any other ring (preferably cycloalkyl, heterocyclyl or aryl) formed from two different functional groups, for example, "R _i -R _i' ring "means that when R _i and R _{i 'generated} when the ring with the atom to form a ring together with the connector. Then, the ring may be substituted or unsubstituted.

In the context of the present invention, alkyl is understood to mean a saturated, linear or branched hydrocarbon, which may be unsubstituted or substituted once or several times. It covers, for example, -CH ₃ and -CH ₂ -CH ₃ . In these groups, C _1-2 -alkyl represents C1- or C2-alkyl, C _1-3 -alkyl represents C1-, C2- or C3-alkyl, and C _1-4 -alkyl represents C1-, C2-, C3- or C4-alkyl, C _1-5 -alkyl means C1-, C2-, C3-, C4- or C5-alkyl, C _1-6 -alkyl means C1-, C2-, C3-, C4-, C5- or C6-alkyl, C _1-7 -alkyl means C1-, C2-, C3-, C4-, C5-, C6- or C7-alkyl, C _{1 -8} -alkyl means C1-, C2-, C3-, C4-, C5-, C6-, C7- or C8-alkyl, C _1-10 -alkyl means C1-, C2-, C3-, C4 -, C5-, C6-, C7-, C8-, C9- or C10-alkyl, and C _1-18 -alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7 -, C8-, C9-, C10-, C11-, C12-, C13-, C14-, C15-, C16-, C17- or C18-alkyl. Alkyl is preferably methyl, ethyl, propyl, methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, pentyl, 1 ,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, hexyl, 1-methylpentyl, if substituted, it is also CHF ₂ , CF ₃ or CH ₂ OH etc. Preferred alkyl in the context of the present invention is understood to be C _1-8 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl or octyl; preferably C _{1- 6} alkyl groups such as methyl, ethyl, propyl, butyl, pentyl or hexyl; more preferably C _1-4 alkyl groups such as methyl, ethyl, propyl or butyl.

Alkenyl is understood to mean unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It covers groups such as -CH=CH-CH ₃ and the like. The alkenyl group is preferably vinyl (ethenyl) or allyl (2-propenyl). Preferably, in the context of the present invention, alkenyl is C _2-10 -alkenyl or C _2-8 -alkenyl, such as vinyl, propenyl, butenyl, pentenyl, hexenyl, heptyl Alkenyl or octenyl; or C _2-6 -alkenyl, such as vinyl, propenyl, butenyl, pentenyl, or hexenyl; or C _2-4 -alkenyl, such as vinyl, Propylene or butenyl.

Alkynyl is understood to mean unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It covers groups such as -C = C-CH ₃ (1-propynyl). Preferably, in the context of the present invention, alkynyl is C _2-10 -alkynyl or C _2-8 -alkynyl, such as ethynyl, propynyl, butynyl, pentynyl, hexynyl, Heptynyl or octynyl; or C _2-6 -alkynyl, such as ethynyl, propynyl, butynyl, pentynyl, or hexynyl; or C _2-4 -alkynyl, such as acetylene Group, propynyl, butynyl, pentynyl or hexynyl.

With regard to alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl and O-alkyl-, unless otherwise defined, in the context of the present invention The term substituted should be understood as that at least one hydrogen group on the carbon atom is composed of halogen (F, Cl, Br, I), -NR _k R _k' , -SR _k , -S(O)R _k , -S( O) ₂ R _k , -OR _k , -C(O)R _k , -C(O)OR _k , -CN, -C(O)NR _k R _k' , haloalkyl, haloalkoxy substitution, R _{k is} represented by R ₁₃ , R ₃₁ , R ₃₂ , R ₅₁ , R ₆₁ , R ₇₁ or R ₈₁ (R _k′ is represented by R _13′ , R _31′ , R _32′ , R _51′ , R _61′ , R _71' or R _81' ; R _{k'' is} represented by R _13'' , R _31'' , R _32'' , R _51'' , R _61'' , R _71'' or R _81'' ); Wherein R ₁ to R _81'' and R _z and R _a and R _b are as defined in the specification, and wherein when different groups R ₁ to R _81'' and R _z are present in formula I at the same time, they can Same or different.

Most preferably, with regard to alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl, substitutions are understood in the context of the present invention Any alkyl group substituted with one or more of halogen (F, Cl, Br, I), -NR _k R _k' , -OR _k , -CN, -SR _k , haloalkyl, haloalkoxy (Also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl, R _k consists of R ₁₃ , R ₃₁ , R ₃₂ , R ₅₁ , R ₆₁ , R ₇₁ or R ₈₁ represents, (R _{k 'by} the _{R 13', R 31 ',} R 32', R 51 ', R 61', R 71 ' or R _81' represents; R _{k ''} the R _{13 ''} , R _31'' , R _32'' , R _51'' , R _61'' , R _71'' or R _81'' means); where R ₁ to R _81'' and R _z are as described in the specification Definition, and wherein when different groups R ₁ to R _{81 ″} and R _z and R _a and R _b are present in formula I at the same time, they may be the same or different.

The same molecule and the same carbon atom may be replaced more than once by the same or different substituents. This includes (for example) the replacement of 3 hydrogens on the same C atom (as in the case of CF ₃ ), or on different positions on the same molecule (as in eg -CH(OH)-CH=CH-CHCl ₂ ).

In the context of the present invention, haloalkyl is understood to mean that the alkyl is substituted once or several times by halogen (selected from F, Cl, Br, I). It covers, for example, —CH ₂ Cl, —CH ₂ F, —CHCl ₂ , —CHF ₂ , —CCl ₃ , —CF ₃ and —CH ₂ —CHCI ₂ . Preferably, in the context of the present invention, haloalkyl is understood to be halogen substituted C _1-4 -alkyl, which means halogen substituted C1-, C2-, C3- or C4-alkyl. Therefore, the halogen-substituted alkyl is preferably methyl, ethyl, propyl and butyl. Preferred examples include -CH ₂ Cl, -CH ₂ F, -CHCl ₂ , -CHF ₂ and -CF ₃ .

In the context of the present invention, haloalkoxy is understood to mean that -O-alkyl is substituted once or several times by halogen (selected from F, Cl, Br, I). It covers, for example, -OCH ₂ Cl, -OCH ₂ F, -OCHCl ₂ , -OCHF ₂ , -OCCl ₃ , -OCF ₃ and -OCH ₂ -CHCI ₂ . Preferably, in the context of the present invention, haloalkoxy is understood to be -OC _1-4 -alkyl substituted by halogen, which means C1-, C2-, C3- or C4-alkoxy substituted by halogen. Therefore, the halogen-substituted alkyl groups are preferably O-methyl, O-ethyl, O-propyl and O-butyl. Preferred examples include -OCH ₂ Cl, -OCH ₂ F, -OCHCl ₂ , -OCHF ₂ and -OCF ₃ .

In the context of the present invention, cycloalkyl is understood to mean saturated and unsaturated (but not aromatic) cyclic hydrocarbons (no heteroatoms in the ring), which may be unsubstituted or substituted once or several times. In addition, C _3-4 -cycloalkyl means C3- or C4-cycloalkyl, C _3-5 -cycloalkyl means C3-, C4- or C5-cycloalkyl, and C _3-6 -cycloalkyl means C3-, C4-, C5- or C6-cycloalkyl, C _3-7 -cycloalkyl means C3-, C4-, C5-, C6- or C7-cycloalkyl, C _3-8 -cycloalkyl Means C3-, C4-, C5-, C6-, C7- or C8-cycloalkyl, C _4-5 -cycloalkyl means C4- or C5-cycloalkyl, C _4-6 -cycloalkyl means C4 -, C5- or C6-cycloalkyl, C _4-7 -cycloalkyl means C4-, C5-, C6- or C7-cycloalkyl, C _5-6 -cycloalkyl means C5- or C6-cyclo Alkyl, and C _5-7 -cycloalkyl means C5-, C6- or C7-cycloalkyl. Examples are cyclopropyl, 2-methylcyclopropyl, cyclopropylmethyl, cyclobutyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cycloheptyl, cyclooctyl and also adamantyl. Preferably, in the context of the present invention, cycloalkyl is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; or is C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; or C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or Cyclohexyl, especially cyclopentyl or cyclohexyl.

Aryl is understood to mean a 5- to 18-membered monocyclic or polycyclic ring system having at least one aromatic ring but no heteroatoms even in only one of the rings. Examples are phenyl, naphthyl, propadienyl, fluoranthenyl, fluorenyl, tetrahydronaphthyl or indanyl, 9H-fluorenyl or anthracenyl, which may be unsubstituted or substituted once Or several times. Optimally, in the context of the present invention, aryl is understood to be phenyl, naphthyl or anthracenyl, preferably phenyl.

Heterocyclic group (radical or group) (hereinafter also referred to as heterocyclic group) is understood to mean a 5- to 18-membered monocyclic or polycyclic heterocyclic ring system having at least one saturated or unsaturated ring in which Contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur. The heterocyclic group may also be substituted once or several times.

Subunits within heterocyclic groups as understood herein include heteroaryl and non-aromatic heterocyclic groups.

-Heteroaryl (equivalent to heteroaromatic group or aromatic heterocyclic group) is an aromatic 5- to 18-membered monocyclic or polycyclic heterocyclic ring system with one or more rings in which at least one aromatic ring is in the ring Contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur; preferably one or two rings of 5 to 18 membered monocyclic or polycyclic aromatic heterocyclic ring systems, at least one of which is aromatic The family ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably selected from furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine , Quinoline, isoquinoline, phthalazine, benzothiazole, indole, benzotriazole, carbazole, quinazoline, thiazole, imidazole, pyrazole, oxazole, thiophene and benzimidazole;

-A non-aromatic heterocyclic group is a 5- to 18-membered monocyclic or polycyclic heterocyclic ring system with one or more rings in which at least one ring (with this ring or rings) is not aromatic) Contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur; preferably a 5- to 18-membered monocyclic or polycyclic heterocyclic ring system (having one or two rings) of one or two rings , It is not aromatic) contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably selected from norhydroxyazepam, pyrrolidine, hexahydropyridine, hexahydropyridine Azine, tetrahydropyran, morpholine, indoline, pendant pyrrolidine, benzodioxane, especially benzodioxane, morpholine, tetrahydropyran, hexahydropyridine, pendant pyrrole Pyridine and pyrrolidine.

Preferably, in the context of the present invention, heterocyclyl is defined as one or more saturated or unsaturated 5 to 18 membered monocyclic or polycyclic heterocyclic ring systems in which at least one ring contains one or more in the ring A heteroatom selected from the group consisting of nitrogen, oxygen and/or sulfur. Preferably, it is a 5- to 18-membered monocyclic or polycyclic heterocyclic ring system of one or two saturated or unsaturated rings, wherein at least one ring contains one or more selected from nitrogen, oxygen and/or sulfur in the ring Heterogenous atoms in groups.

Preferred examples of heterocyclic groups include oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benfuran, benzimidazole, indazole , Benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[ 2,3b]pyridine, quinoline, isoquinoline, tetrahydroisoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, lateral oxygen Pyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline, especially pyridine, pyrazine, indazole, benzodioxane, thiazole, benzothiazole, morpholine , Tetrahydropyran, pyrazole, imidazole, hexahydropyridine, thiophene, indole, benzimidazole, pyrrolo[2,3b]pyridine, benzoxazole, pendant pyrrolidine, pyrimidine, oxygen nitrogen heterocycle Heptane and pyrrolidine.

In the context of the present invention, pendant pyrrolidine is understood to mean pyrrolidin-2-one.

N -containing heterocyclic group is a heterocyclic system of one or more saturated or unsaturated rings, wherein at least one ring contains nitrogen in the ring and optionally one or more others selected from the group consisting of nitrogen, oxygen and/or sulfur Heteroatom; preferably a heterocyclic ring system with one or two saturated or unsaturated rings, wherein at least one ring contains nitrogen in the ring and optionally one or more others selected from the group consisting of nitrogen, oxygen and/or sulfur Heteroatoms, more preferably selected from noroxyrazine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzimidazole, indazole, Benzothiazole, benzodiazole, morpholine, indoline, triazole, isoxazole, pyrazole, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, quinolinone, isoquinoline , Tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, carbazole or thiazole.

之碳序列而形成的雜環基(如上文所定義)之亞基。該環狀醯胺可視情況稠合至環系統。較佳地，環狀醯胺係「吲哚啉-2-酮」。環狀醯胺可如針對上文雜環基所定義經取代或未經取代。In the context of the present invention, cyclic amides are defined as sequences containing at least part forming a ring via cyclization

The subunit of the heterocyclic group (as defined above) formed by the carbon sequence. The cyclic amide is fused to the ring system as the case may be. Preferably, the cyclic amide group is "indolin-2-one". The cyclic amide can be substituted or unsubstituted as defined for the heterocyclic group above.

之碳序列而形成的雜環基(如上文所定義)之亞基。該環狀脲可視情況稠合至環系統。較佳地，環狀脲係「1H-苯并[d]咪唑-2(3H)-酮」。環狀脲可如針對上文雜環基所定義經取代或未經取代。In the context of the present invention, cyclic urea is defined as a sequence containing at least a ring-forming part via cyclization

The subunit of the heterocyclic group (as defined above) formed by the carbon sequence. The cyclic urea is fused to the ring system as the case may be. Preferably, the cyclic urea system is "1H-benzo[d]imidazol-2(3H)-one". The cyclic urea may be substituted or unsubstituted as defined for the heterocyclic group above.

Combining aromatic heterocyclic groups (heteroaryl), non-aromatic heterocyclic groups, aryl groups and cycloalkyl groups, when the ring system is in two or more of the above ring definitions at the same time, the ring system is defined first It is an aromatic heterocyclic group (heteroaryl), provided that at least one aromatic ring contains a heteroatom. If the aromatic ring does not contain heteroatoms, the ring system is defined as a non-aromatic heterocyclic group, provided that at least one non-aromatic ring contains heteroatoms. If the non-aromatic ring contains no heteroatoms, the ring system is defined as an aryl group, provided that it contains at least one aryl ring. If no aryl group is present, the ring system is defined as cycloalkyl, provided that at least one non-aromatic cyclic hydrocarbon is present.

In the context of the present invention, alkylaryl is understood to mean that an aryl group (see above) is connected to another atom via a C _1-6 -alkyl (see above), the C _1-6 -alkyl It may be branched or linear and unsubstituted or substituted once or several times. Preferably, alkylaryl is understood to mean that the aryl group (see above) is connected to another atom via 1 to 4 (-CH ₂ -) groups. Best alkylaryl benzyl-based (i.e., -CH ₂ - phenyl).

In the context of the present invention, alkylheterocyclyl is understood to mean that the heterocyclyl is connected to another atom via C _1-6 -alkyl (see above), which C _1-6 -alkyl may have a branch The chain may be linear and unsubstituted or substituted once or several times. Preferably, alkylheterocyclyl is understood to mean that the heterocyclyl (see above) is connected to another atom via 1 to 4 (-CH ₂ -) groups. Most preferably, the alkyl heterocyclic group is -CH ₂ -pyridine.

In the context of the present invention, alkylcycloalkyl is understood to mean that cycloalkyl is connected to another atom via a C _1-6 -alkyl (see above), which C _1-6 -alkyl may have a branch Or it is linear and unsubstituted or substituted once or several times. Preferably, alkylcycloalkyl is understood to mean that cycloalkyl (see above) is connected to another atom via 1 to 4 (-CH ₂ -) groups. Most preferably, the alkylcycloalkyl group is -CH ₂ -cyclopropyl.

Heterocyclyl is a heterocyclic ring system with one or more saturated or unsaturated rings, where at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur in the ring; preferably one Or a heterocyclic ring system of two saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably selected from oxazepine Alkane, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzothiazole, benzo Diazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b ]Pyridine, quinoline, quinolinone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, side Oxypyrrolidine, benzodioxolane, benzodioxane, carbazole, oxaspirodecane or thiazole;

In general, the heterocyclic group may contain between 3 and 32 atoms in the ring (preferably 4 to 20 atoms in the ring, or 5 to 18 atoms in the best ring). Therefore, in the case of a saturated or unsaturated ring heterocyclic group, the heterocyclic group may contain between 3 and 12 atoms in the ring (preferably 4 to 10 atoms in the ring, or in the ring 5 to 8 atoms, or 5 to 6 atoms in the ring). In the case of a heterocyclic group of two saturated or unsaturated rings, the heterocyclic group may also contain between 5 and 22 atoms in both rings together (preferably 6 to 16 atoms, or 7 to 12 atoms in two rings together, or 8 to 10 atoms in two rings together). In the case of heterocyclic groups of three saturated or unsaturated rings, the heterocyclic group may also contain between 7 and 32 atoms in 3 rings together (preferably 10 to 22 atoms, or 12 to 20 atoms in 3 rings together, or 10 to 18 atoms in 3 rings together).

Preferably, the aryl group is a monocyclic aryl group. More preferably, the aryl group is a 5, 6 or 7 membered monocyclic aryl group. Even better, the aryl group is a 5 or 6 membered monocyclic aryl group.

Preferably, the heteroaryl group is a monocyclic heteroaryl group. More preferably, the heteroaryl group is a 5, 6 or 7 membered monocyclic heteroaryl group. Even better, the heteroaryl group is a 5 or 6 membered monocyclic heteroaryl group.

Preferably, the non-aromatic heterocyclic group is a monocyclic non-aromatic heterocyclic group. More preferably, the non-aromatic heterocyclic group is a 4, 5, 6 or 7-membered monocyclic non-aromatic heterocyclic group. Even more preferably, the non-aromatic heterocyclic group is a 5- or 6-membered monocyclic non-aromatic heterocyclic group.

Preferably, cycloalkyl is a monocyclic cycloalkyl. More preferably, the cycloalkyl group is a 3, 4, 5, 6, 7 or 8-membered monocyclic cycloalkyl group. Even more preferably, the cycloalkyl group is a 3, 4, 5, or 6-membered monocyclic cycloalkyl group.

With regard to aryl groups (including alkyl-aryl groups), cycloalkyl groups (including alkyl-cycloalkyl groups) or heterocyclic groups (including alkyl-heterocyclic groups), unless otherwise defined, substituted is understood to mean The ring system of aryl or alkyl-aryl, cycloalkyl or alkyl-cycloalkyl, heterocyclyl or alkyl-heterocyclyl is substituted by one or more of the following: halogen (F, Cl, Br , I), -R _k , -OR _k , -CN, -NO ₂ , -NR _k R _k' , -C(O)OR _k , NR _k C(O)R _k' , -C(O)NR _{k R k ', -NR k S} (O) 2 R k', = O, -OCH 2 CH 2 OH, -NR k C (O) NR k 'R k'', -S (O) 2 NR k R _k' , -NR _k S(O) ₂ NR k'R _{k' '} , haloalkyl, haloalkoxy, -SR _k , -S(O)R _k , -S(O) ₂ R _k or C(CH ₃ )OR _k , or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, where R _k , R _k'and R _{k'' are} independently H or saturated or unsaturated, linear or branched, substituted or unsubstituted C _1-6 -alkyl; saturated or unsaturated, linear or Branched, substituted or unsubstituted C _1-6 -alkyl; saturated or unsaturated, linear or branched, substituted or unsubstituted -OC _1-6- alkyl (alkoxy) ; Saturated or unsaturated, linear or branched, substituted or unsubstituted -SC _1-6- alkyl; saturated or unsaturated, linear or branched, substituted or unsubstituted -C (O)-C _1-6- alkyl-group; saturated or unsaturated, linear or branched, substituted or unsubstituted -C(O)-OC _1-6- alkyl- group ; Substituted or unsubstituted aryl or alkyl-aryl; substituted or unsubstituted cycloalkyl or alkyl-cycloalkyl; substituted or unsubstituted heterocyclyl or alkyl-hetero Cyclic group, R _k is one of R ₁₄ , R ₂₁ , R ₃₁ , R ₄₁ , R ₅₁ , R ₅₂ , R ₆₁ or R ₇₁ , (where R _k′ is R _14′ , R _21′ , R _{One of 31'} , R _41' , R _51' , R _52' , R _61' or R _71' is R _k'' is R _14'' , R _21'' , R _31'' , R _{41 ''} , R _51'' , R _52'' , R _61'' or R _71'' ; where R ₁ to R _81'' and R _z and R _a and R _b are as defined in the specification , And wherein when different groups R ₁ to R _{81 ″} and R _z and R _a and R _{b are} simultaneously present in Formula I, they may be the same or different.

Most preferably, regarding aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl), or heterocyclic group (including alkyl-heterocyclic), in the present invention, substituted It should be understood that any substituted aryl, cycloalkyl, and heterocyclic groups (also in alkylaryl, alkylcycloalkyl, or alkylheterocyclic groups) are substituted with one or more of the following: halogen ( F, Cl, Br, I), -R _k , -OR _k , -CN, -NO ₂ , -NR _k R _k''' , NR _k C(O)R _k' , -NR _k S(O) _{2 R k ', -S (O} ) 2 NR k R k', -NR k C (O) NR k 'R k'', haloalkyl, haloalkoxy, -SR _k, -S (O) R _k or S(O) ₂ R _k , or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, R _k is one of R ₁₄ , R ₂₁ , R ₃₁ , R ₄₁ , R ₅₁ , R ₅₂ , R ₆₁ or R ₇₁ , (where R _k′ is R _14′ , R _21′ , R _31′ , One of R _41' , R _51' , R _52' , R _61' or R _71' ; R _k'' is R _14'' , R _21'' , R _31'' , R _41'' , One of R _51'' , R _52'' , R _61'' or R _71'' ; wherein R ₁ to R _81'' and R _z and R _a and R _b are as defined in the specification, and wherein When different groups R ₁ to R _{81 ″} and R _z and R _a and R _b are present in formula I at the same time, they may be the same or different.

(導致螺結構)及/或=O的取代。Binding cycloalkyl (including alkyl-cycloalkyl), or heterocyclic group (including alkyl heterocyclic group), ie non-aromatic heterocyclic group (including non-aromatic alkyl-heterocyclic group), unless otherwise Definition, otherwise substituted should be understood to mean the ring system of cycloalkyl or alkyl-cycloalkyl, non-aromatic heterocyclic group or non-aromatic alkyl-heterocyclic group

(Resulting in a spiro structure) and/or =O substitution.

In addition, in combination with cycloalkyl (including alkyl-cycloalkyl), or heterocyclic group (including alkyl heterocyclic group), that is, non-aromatic heterocyclic group (including non-aromatic alkyl-heterocyclic group), unless Otherwise defined, otherwise substituted should be understood to mean that the ring system of cycloalkyl or alkyl-cycloalkyl, non-aromatic heterocyclic group or non-aromatic alkyl-heterocyclic group is substituted by spiro or =0.

In addition, in combination with cycloalkyl (including alkyl-cycloalkyl), or heterocyclic group (including alkyl heterocyclic group), that is, non-aromatic heterocyclic group (including non-aromatic alkyl-heterocyclic group), unless Otherwise defined, otherwise substituted is understood to mean the substitution of the ring system of cycloalkyl or alkyl-cycloalkyl, non-aromatic heterocyclic group or non-aromatic alkyl-heterocyclic group by =O.

，其中R_a 、R_b 及p係如說明書中所定義。For clarity, also refer to the following description in the definition of substitution on alkyl etc. or aryl etc., "when different groups R ₁ to R _81" and R _z and R _a and R _b are present in formula I at the same time In medium time, it may be the same or different". This description is reflected in the definition of X= -[C(R _a R _b )] _p -in the general formula (I): X=

, Where R _a , R _b and p are as defined in the specification.

其中R_a 、R_b 及p係如說明書中所定義。另外，添加R_a’ 及R_b’ 。正如上文所述，此說明由此反映：R_a’ 及R_b’ 不同於或可不同於R_a 及R_b 或相同。X can also be expressed as:

Where R _a , R _b and p are as defined in the specification. In addition, R _a'and R _{b'are added} . As mentioned above, this description reflects whereby: R _{a 'and} R _b' may be different or different from R _a and R _b are the same or.

The necessary amendments to the details are also applicable to general formulae such as general formula (I) and other general formulae (I ^' ) to (Ic ^' ) and all synthetic intermediates.

A ring system is a system consisting of at least one ring connecting atoms, but also includes systems in which two or more rings connecting atoms are joined, where "joining" means that each other ring shares one (such as a spiro structure), two One or more atoms are one or more members of two bonding rings.

The term "breakaway group" means a molecular fragment that leaves with a pair of electrons in the cleavage of a heterocleft bond. The leaving group may be an anion or a neutral molecule. Common anionic leaving group based halide, e.g. Cl ^-, Br ^- and I ^-; and sulfonate, e.g. tosylate (TsO ^-) or mesylate.

The term "salt" is understood to mean any form of active compound used in accordance with the invention, wherein it takes the form of an ion or is charged and is coupled with a counter ion (cation or anion) or in solution. It should also be understood from this that the active compound recombines with other molecules and ions, specifically through ionic interaction.

The term "physiologically acceptable salt" in the context of the present invention means any physiologically tolerated salt (most of the time means if used appropriately in therapy, especially if used or applied to humans and/or mammals) Non-toxic-especially not caused by relative ions).

Such physiologically acceptable salts can be formed with cations or bases, and should be understood in the context of the present invention to mean salts of at least one compound used according to the present invention-usually (deprotonated) acids-in the form of anions and At least one, preferably inorganic cationic form, which is physiologically tolerated, especially if used in humans and/or mammals. Salts of alkali metals and alkaline earth metals are particularly preferred, and those having NH ₄ , but specifically (mono)- or (di)sodium, (mono)- or (di)potassium, magnesium or calcium salts.

Physiologically acceptable salts can also be formed with anions or acids, and in the context of the present invention it should be understood that salts of at least one compound used in accordance with the present invention mean cations and at least one anion, and these salts are particularly useful in Humans and/or mammals are physiologically tolerated. It should therefore be understood that in the context of the present invention, salts with physiologically tolerable acids, ie salts of specific active compounds with inorganic or organic acids, these salts are particularly useful in humans and/or mammals The time is physiologically tolerable. Examples of physiologically tolerable salts of specific acids are hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, formic acid, acetic acid, oxalic acid, succinic acid, malic acid, tartaric acid, amygdalic acid, fumaric acid, lactic acid or lemon acid.

The compounds of the present invention may exist in crystalline form or in the form of free compounds such as free bases or acids.

Any compound that is a solvate of a compound according to the invention (as defined above in Formula I) should be understood to be included within the scope of the invention. Solvation methods are generally known in the industry. Suitable solvates are pharmaceutically acceptable solvates. The term "solvate" according to the present invention is understood to mean any form of the active compound according to the present invention, wherein this compound is connected to it via a non-covalently bound another molecule (most likely a polar solvent). Particularly preferred examples include hydrates and alcoholates, such as methanolates or ethanolates.

Any compound that is a prodrug of a compound according to the present invention (as defined above in Formula I) should be understood to be included within the scope of the present invention. The term "prodrug" is used in its broadest sense and covers their derivatives that are converted into the compounds of the present invention in vivo. Such derivatives will be easily remembered by those skilled in the art, and based on the functional groups present in the molecule, including but not limited to the following derivatives of the compounds of the present invention: esters, amino esters, phosphate esters, metal salt sulfonates , Carbamate and amide. Examples of well-known methods for producing prodrugs of compounds with a given effect are known to those skilled in the art and can be found, for example, in Krogsgaard-Larsen et al., "Textbook of Drug design and Discovery" Taylor & Francis (April 2002 ).

Any compound that is an N-oxide of a compound according to the present invention (a compound of formula I as defined above) should be understood to be included within the scope of the present invention.

Unless otherwise stated, the compounds of the present invention are also intended to include compounds that differ only in the presence of one or more isotopically enriched atoms. For example, compounds having the structure of the present invention (where hydrogen is replaced by deuterium or tritium, or carbon is replaced by ¹³ C- or ¹⁴ C-rich carbon, or nitrogen is replaced by ¹⁵ N-rich nitrogen) belong to the present invention Within range. This will especially apply to the above prerequisites, so that references to hydrogen or any "H" in the formula will also cover deuterium or tritium.

The compound of formula (I) and the salt or solvate of the compound are preferably in pharmaceutically acceptable or substantially pure form. A pharmaceutically acceptable form especially means having a pharmaceutically acceptable degree of purity, excluding normal pharmaceutical additives (such as diluents and carriers), and excluding substances considered to be toxic at normal dosage values. The purity value of the API is preferably higher than 50%, more preferably higher than 70%, and most preferably higher than 90%. In a preferred embodiment, it is higher than 95% of the compound of formula (I) or its salt. This also applies to its solvates or prodrugs.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein X is selected from the group consisting of -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O )[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -And-[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _{a is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{b is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; R _{z is} selected from Hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted Cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O)-C _1-6 alkyl; stereoisomers, preferably mirror-isomers or diastereomers, as the case may be One of them, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture in any mixing ratio, or The corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein X is selected from the group consisting of bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O )[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -And-[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; depending on the situation, one of the stereoisomers, the preferred mirror isomers or the non-mirror isomers, the racemate In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein X is selected from the group consisting of -[C(R _a R _b )] _p -and -[CH ₂ ] _p C(O )[CH ₂ ] _q -; depending on the situation, it is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror images At least two of the isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{a is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or non-mirror isomers, extinction In the form of rotates, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates Thing.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{a is} selected from hydrogen, halogen, and substituted or unsubstituted C _1-6 alkyl; One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{a is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally stereoisomers , One of the preferred enantiomers or diastereomers, racemates, or at least two of the stereoisomers, preferred enantiomers and/or diastereomers They are in the form of mixtures of any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{b is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or non-mirror isomers, extinction In the form of rotates, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates Thing.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{b is} selected from hydrogen, halogen, and substituted or unsubstituted C _1-6 alkyl; One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the formula (I) of the compounds according to the present invention as follows based compound to form a cycloalkyl, substituted or non-substituted with wherein R _a and R _b carbon connected thereto of atoms; optionally a three-dimensional Isomers, one of the preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O) -C _1-6 alkyl; optionally in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror images At least two of the isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O)-C _1-6 alkyl; stereoisomers, preferably mirror-isomers or diastereomers, as the case may be One of them, in the form of a racemate, or in the form of a mixture of any mixture ratio of stereoisomers, preferably mirror isomers, and/or diastereoisomers, or its corresponding Salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is the following compound, wherein p is 0, 1, 2, 3, 4 or 5; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is the following compound, wherein q is 0, 1, 2, 3, 4 or 5; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is the following compound, wherein n is 0 or 1; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is the following compound, wherein m is 0, 1 or 2; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is the following compound, wherein r is 0, 1 or 2; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein Y is -CH ₂ -or C=O; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein Y ₁ is -C(R ₁₀ R _10′ )-; wherein R ₁₀ and R _{10′ are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; or, R ₁₀ and R _10′ Together with the carbon atom to which it is attached form a substituted or unsubstituted cycloalkyl; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates, Or at least two of the stereoisomers, preferably mirror image isomers and/or diastereomers in the form of a mixture at any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein Y ₂ is -C(R _10'' R _10''' )-; wherein R _10'' and R _10''' independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; Or, R _10'' and R _10''' together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; optionally stereoisomers, preferably mirror isomers or diastereomers One of them, in the form of a racemate, or in the form of a mixture of any mixture ratio of stereoisomers, preferably mirror isomers, and/or diastereoisomers, or its corresponding Salts, or their corresponding solvates.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein Y ₁ is -C(R ₁₀ R _10' )-; optionally stereoisomers, preferably mirror images One of the compounds or diastereomers, racemate, or at least two of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein Y ₂ is -C(R _10'' R _10′'' )-; One of the best enantiomers or diastereomers, in the form of racemates, or at least two of stereoisomers, preferably enantiomers and/or diastereomers In the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₁ is

; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or At least two of the mirror image isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of the general formula (I) is a compound wherein R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclic groups; as appropriate In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the present invention of general formula (I) is a compound wherein R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclic group, In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; depending on the situation One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereoisomers, racemates, or At least two of the stereoisomers, preferably mirror image isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R ₃ is hydrogen or a substituted or unsubstituted C _1-6 alkyl; optionally stereoisomers, One of the preferred enantiomers or diastereomers, racemate, or at least two of stereoisomers, preferred enantiomers, and/or diastereomers In the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₃ is a substituted or unsubstituted C _1-6 alkyl group; stereoisomers are preferred, preferably One of the enantiomers or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably enantiomers, and/or diastereomers, in any form The form of the mixture in the mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, racemic In the form of a mixture, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate .

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl; optionally stereoisomeric , One of the preferred enantiomers or diastereomers, the racemate, or at least one of the stereoisomers, preferred enantiomers and/or diastereomers The two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₄ and R _{4 ′ are} independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O) NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; where R ₄₁ , R _41' and R _{41 ''} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and Substituted or unsubstituted cycloalkyl; optionally in the form of a stereoisomer, preferably mirror image isomer or diastereomer, racemate, or as a stereoisomer, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₄ and R _{4 ′ are} independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O) NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; stereoisomers are preferred, preferably One of the enantiomers or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably enantiomers, and/or diastereomers, in any form The form of the mixture in the mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound in which both R ₄ and R _{4 ′} are -R ₄₁ ; stereoisomers, preferably mirror image isomers, as the case may be One of the compounds or diastereomers, racemate, or at least two of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound in which both R ₄ and R _{4 ′} are hydrogen; optionally stereoisomers, preferably mirror isomers or One of the diastereomers, racemate, or a mixture of stereoisomers, preferably mirror isomers, and/or at least two of the diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; depending on the situation One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in the form of one of stereoisomers, preferably enantiomers or diastereoisomers, racemates, or At least two of the stereoisomers, preferably mirror isomers and/or diastereoisomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{5 is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally stereoisomers , One of the preferred enantiomers or diastereomers, racemates, or at least two of the stereoisomers, preferred enantiomers and/or diastereomers They are in the form of mixtures of any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₅ is a substituted or unsubstituted C _1-6 alkyl group; stereoisomers are preferred, preferably One of the enantiomers or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably enantiomers, and/or diastereomers, in any form The form of the mixture in the mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{5′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, racemic In the form of a mixture, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate .

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{5′ is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally stereoisomeric , One of the preferred enantiomers or diastereomers, the racemate, or at least one of the stereoisomers, preferred enantiomers and/or diastereomers The two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound in which R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; One of the stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted Substituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, Substituted or unsubstituted alkyl heterocyclic group and -C(O)R ₇ ; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers, racemates In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{6 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted cycloalkane Group, substituted or unsubstituted aryl group, substituted or unsubstituted alkyl aryl group, substituted or unsubstituted heterocyclic group and -C(O)R ₇ ; stereoisomeric as appropriate , One of the preferred enantiomers or diastereomers, racemates, or at least two of the stereoisomers, preferred enantiomers and/or diastereomers They are in the form of mixtures of any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{6 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted alkyl Aryl and -C(O)R ₇ ; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereoisomers, racemates, or stereoisomers, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted Aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylheterocyclyl; stereoisomers, preferably mirror images, as appropriate One of the isomers or diastereomers, in the form of a racemate, or in any mixture of stereoisomers, preferably mirror isomers and/or diastereomers In the form of a mixture of ratios, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted cycloalkane Group, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic group, substituted Or an unsubstituted alkyl heterocyclic group; optionally in the form of a stereoisomer, preferably an enantiomer or diastereomer, a racemate, or as a stereoisomer, Preferably at least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₇ is a substituted or unsubstituted aryl group; stereoisomers, preferably mirror isomers, as the case may be Or one of the diastereomers, racemates, or a mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and -OR ₈₁ ; optionally one of stereoisomers, preferred mirror isomers, or non-mirror isomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, and -OR ₈₁ ; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{8′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, racemic In the form of a mixture, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate .

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{8′ is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally stereoisomeric , One of the preferred enantiomers or diastereomers, the racemate, or at least one of the stereoisomers, preferred enantiomers and/or diastereomers The two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O) NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; stereoisomers are preferred, preferably One of the enantiomers or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably enantiomers, and/or diastereomers, in any form The form of the mixture in the mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₉ and R _9'are independently selected from -R ₂₁ ; optionally stereoisomers, preferably mirror images One of the compounds or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₁₀ and R _{10′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; one of stereo isomers, preferably mirror isomers or diastereomers, as the case may be , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R ₁₀ and R _{10′ are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₁₀ and R _10′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; One of the stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _10″ and R _{10″′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or non-mirror isomers One of them, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture in any mixing ratio, or The corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _10″ and R _{10″′ are} independently selected from hydrogen and substituted or unsubstituted C _1-6 Alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or Or at least two of the diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _10″ and R _10″′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl ; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or At least two of the mirror image isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₁₃ and R _{13′ are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; optionally in the form of stereoisomers, preferably mirror isomers or diastereomers, racemates, Or at least two of stereoisomers, preferably mirror isomers and/or diastereoisomers in the form of a mixture in any mixing ratio, or a corresponding salt or a corresponding solvate thereof.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R ₁₃ and R _{13′ are} independently selected from hydrogen and unsubstituted C _1-6 alkyl; optionally stereo Isomers, one of the preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R ₁₄ , R _14′ and R _{14″ are} independently selected from hydrogen, unsubstituted C _1-6 alkyl , Unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group; stereoscopic as the case may be One of the isomers, preferred mirror isomers or diastereomers, racemate, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₁₄ , R _14′ and R _{14″ are} independently selected from hydrogen, unsubstituted C _1-6 alkyl , Unsubstituted aryl, unsubstituted cycloalkyl, and unsubstituted heterocyclic group; depending on the situation, one of stereoisomers, preferred mirror isomers, or non-mirror isomers, external In the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in any mixing ratio, or its corresponding salt, or its corresponding solvent Compound.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₂₁ , R _21′ and R _{21″ are} independently selected from hydrogen, substituted or unsubstituted C _{1- 6} Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror image isomers or non-mirror images, as the case may be One of the structures, the racemate, or a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in any mixture ratio, or Its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₂₁ , R _21′ and R _{21″ are} independently selected from hydrogen and substituted or unsubstituted C _{1- 6} alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the formula (I) of the present invention based compound according to the following compounds, wherein R _31, R _{31 'and} R _31''are independently selected from hydrogen, substituted or non-substituted C _{1- 6} Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror image isomers or non-mirror images, as the case may be One of the structures, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or Its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the present invention of general formula (I) is a compound wherein R ₃₁ , R _31′ and R _{31″ are} independently selected from hydrogen and substituted or unsubstituted C _{1- 6} alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₃₂ and R _{32′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; one of stereo isomers, preferably mirror isomers or diastereomers, as the case may be , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₃₂ and R _{32' are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₄₁ , R _{41 ′} and R _{41 ″ are} independently selected from hydrogen, substituted or unsubstituted C _{1- 6} Alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; optionally stereoisomers , One of the preferred enantiomers or diastereomers, racemates, or at least two of the stereoisomers, preferred enantiomers and/or diastereomers They are in the form of mixtures of any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₄₁ , R _{41 ′} and R _{41 ″ are} independently selected from hydrogen, substituted or unsubstituted C _{1- 6} Alkyl and substituted or unsubstituted cycloalkyl; optionally in the form of stereoisomers, preferably mirror isomers or diastereomers, racemates, or stereo At least two of the isomers, preferably mirror image isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the present invention of general formula (I) is a compound wherein R ₅₁ , R _51′ and R _{51″ are} independently selected from hydrogen, substituted or unsubstituted C _{1- 6} Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror image isomers or non-mirror images, as the case may be One of the structures, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or Its corresponding salt, or its corresponding solvate.

In another embodiment, the formula (I) of the present invention based compound according to the following compounds, wherein R _51, R _{51 'and} R _{51' 'are} independently selected from hydrogen and a substituted or non-substituted C _{1- 6} alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₅₂ , R _52′ and R _{52″ are} independently selected from hydrogen, substituted or unsubstituted C _{1- 6} Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror image isomers or non-mirror images, as the case may be One of the structures, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or Its corresponding salt, or its corresponding solvate.

In another embodiment, the formula (I) of the present invention based compound according to the following compounds, wherein R _52, R _{52 'and} R _{52' 'are} independently selected from hydrogen and a substituted or non-substituted C _{1- 6} alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the present invention of general formula (I) is a compound wherein R ₆₁ , R _61′ and R _{61″ are} independently selected from hydrogen, substituted or unsubstituted C _{1- 6} Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror image isomers or non-mirror images, as the case may be One of the structures, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or Its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the present invention of general formula (I) is a compound wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen and substituted or unsubstituted C _{1- 6} alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the present invention of general formula (I) is a compound wherein R ₇₁ , R _71′ and R _{71″ are} independently selected from hydrogen, substituted or unsubstituted C _{1- 6} Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror image isomers or non-mirror images, as the case may be One of the structures, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or Its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of the general formula (I) is a compound wherein R ₇₁ , R _71′ and R _{71″ are} independently selected from hydrogen and substituted or unsubstituted C _{1- 6} alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{81 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, racemates In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{81 is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally stereoisomers , One of the preferred enantiomers or diastereomers, racemates, or at least two of the stereoisomers, preferred enantiomers and/or diastereomers They are in the form of mixtures of any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{81′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, racemic In the form of a mixture, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate .

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{81′ is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally stereoisomeric , One of the preferred enantiomers or diastereomers, the racemate, or at least one of the stereoisomers, preferred enantiomers and/or diastereomers The two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₈₁ and R _{81′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R ₈₁ and R _{81′ are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein R If the aryl or heterocyclic group in ₂ is substituted, it is substituted by one or more substituents selected from the group consisting of: halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from Hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomeric as appropriate , One of the preferred enantiomers or diastereomers, the racemate, or at least one of the stereoisomers, preferred enantiomers and/or diastereomers The two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl; wherein, R ₃ If the defined alkyl, alkenyl or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also an alkylcycloalkyl group is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O) OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _31' R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the ( Etc.) The substituent is preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independent Selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; as appropriate One of the stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, if the alkyl group defined in R ₃ is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein the cycloalkyl group defined in R ₃ and also alkylcycloalkyl group is substituted by one or more selected from the following Substituent substitution: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ ,- CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _31' R _31" and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and haloalkane Oxygen; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally stereoisomers, preferably mirror isomers or One of the diastereomers, racemates, or a mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R ₃ is hydrogen or a substituted or unsubstituted C _1-6 alkyl; wherein, as defined in R ₃ If the alkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₃₁ R _31' ; wherein R ₃₁ and R _{31 '} Independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, racemates In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R ₃ is C _1-6 alkyl; wherein, if the alkyl group defined in R ₃ is substituted, it is substituted by one or Multiple substituents selected from the group consisting of -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₁ R _31' ; wherein R ₃₁ and R _{31' are} independently selected from hydrogen and substituted Or unsubstituted C _1-6 alkyl; optionally in the form of a stereoisomer, preferably mirror image isomer or diastereomer, racemate, or as a stereoisomer At least two of the preferred mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein, if the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted, one or more are selected from The following substituents are substituted: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers Or one of the diastereomers, the racemate, or a mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{3′ is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; wherein, R _3′ If the defined alkyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₃₂ R _32' ; where R ₃₂ And R _{32' is} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, external In the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding solvent Compound.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R _{5′ is} selected from Hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; or, R ₅ and R _5′ together with the carbon atom to which it is attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by one or more selected from Substituted by the following substituents: -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₅₁ R _51' ; wherein the cycloalkyl group is as defined in R ₅ and also alkylcycloalkyl If substituted, it is substituted by one or more substituents selected from: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _{51 '} , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O) R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' , -OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ , -OR ₅₁ , -NR ₅₁ R _51' , -CN, haloalkyl and haloalkoxy; wherein R ₅₁ , R _51' and R _{51'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted Or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the cycloalkyl group as defined in R ₅ -R _5′ is substituted by one or more Substitutions selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' , -NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -OCH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ , -OR ₅₂ , -NR ₅₂ R _52' , -CN, haloalkyl and haloalkoxy; wherein R ₅₂ , R _52' and R _{52'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl Group, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror isomers or diastereomers, as the case may be One of them, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture at any mixing ratio, or their corresponding Salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Cycloalkyl and substituted or unsubstituted alkyl cycloalkyl; R _{5′ is} selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; or, R ₅ and R _5′ are connected to the carbon The atoms together form a substituted or unsubstituted cycloalkyl group; wherein the alkyl groups defined in R ₅ and R _5′ are substituted by one or more substituents selected from the group consisting of —OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₅₁ R _51' ; wherein the cycloalkyl group as defined in R ₅ or alkylcycloalkyl group is substituted by one or more selected from the following Substituent substitution: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S(O) ₂ R _{51 '} , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' , -OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ , -OR ₅₁ , -NR ₅₁ R _51' , -CN, haloalkyl and halo Alkoxy; wherein R ₅₁ , R _51′ and R _{51″ are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; wherein the cycloalkane as defined in R ₅ -R _5′ If the group is substituted, it is substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' , -NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O ) R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -OCH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the (etc.) substituent is preferably selected from halogen, -R ₅₂ , -OR ₅₂ , -NR ₅₂ R _52' , -CN, halo Group and haloalkoxy; wherein R ₅₂ , R _52' and R _{52'' are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; stereoisomers, preferably mirror images, as the case may be One of the isomers or diastereomers, in the form of racemates, or in any mixture of stereoisomers, preferably mirror isomers and/or diastereomers In the form of a mixture of ratios, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted Substituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylheterocyclyl, and -C(O)R ₇ ; where If the alkyl, alkenyl, or alkynyl group defined in R ₆ is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₆₁ , halogen, -CN, haloalkyl, haloalkoxy, and- NR ₆₁ R _{61 ';} in which R _6, also alkylcycloalkyl, alkylaryl and heterocyclic group defined of the cycloalkyl group, an aryl group or a heterocyclic group, if substituted by one or more of the A substituent selected from the group consisting of: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O ) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O)R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the substituent(s) are preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, halogen Alkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally in the form of stereoisomers, preferably mirror isomers or diastereomers, racemates, Or at least two of the stereoisomers, preferably mirror image isomers and/or diastereomers in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of formula (I) according to the invention is a compound wherein R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, Substituted or unsubstituted alkyl heterocyclic group and -C(O)R ₇ ; wherein the alkyl group defined in R ₆ is substituted by one or more substituents selected from the following groups if substituted: -OR ₆₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₆₁ R _{61 '; 6} wherein R, also alkylcycloalkyl, alkylaryl groups and the heterocyclic groups defined in the cycloalkyl If a group, aryl group or heterocyclic group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' ,- NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' ,- SR ₆₁ , -S(O)R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'', and -C(CH ₃ ) ₂ OR ₆₁ ; the substituent(s) are preferably selected from halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferably mirror isomers At least two of the compounds and/or diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted Aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic; wherein the alkyl, alkene as defined in R ₇ If the group or alkynyl group is substituted, it is substituted with one or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₇₁ R _71' ; where R ₇ The cycloalkyl, aryl, and heterocyclic groups defined in the middle, also alkylcycloalkyl, alkylaryl, and alkylheterocyclic groups are substituted with one or more substituents selected from the following if substituted ：=O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S (O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, halogen Alkyl, haloalkoxy, -C(O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' And -C(CH ₃ ) ₂ OR ₇₁ ; the substituent(s) is preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; Where R ₇₁ , R _71' and R _{71'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted Substituted C _2-6 alkynyl; optionally in the form of a stereoisomer, preferably mirror image isomer or diastereomer, racemate, or in the form of a stereoisomer, At least two of the good mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted cycloalkane Group, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic group, substituted Or an unsubstituted alkyl heterocyclic group; wherein the alkyl group defined in R ₇ is substituted with one or more substituents selected from the group consisting of -OR ₇₁ , halogen, -CN, haloalkyl, Haloalkoxy and -NR ₇₁ R _71' ; wherein the cycloalkyl, aryl and heterocyclic group as defined in R ₇ and also alkylcycloalkyl, alkylaryl and alkyl heterocyclic group If substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _{71 '} , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O) R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ ; the substituent(s) are preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; best halogen; wherein R ₇₁ , R _71' and R _{71'' are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkane Radicals; optionally in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or At least two of the diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted the substituted C _2-6 alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted Or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the alkyl, alkenyl or alkynyl group defined in R ₈ or R _8′ is substituted by One or more substituents selected from the group consisting of -OR ₈₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, One of the preferred enantiomers or diastereomers, racemate, or at least two of stereoisomers, preferred enantiomers and/or diastereomers In the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, and -OR ₈₁ ; R _{8 'is} selected from hydrogen and a substituted or non-substituted C _1-6 alkyl; wherein R ₈ or R _8' is defined when the alkyl group of which is substituted by one or more substituents selected from the following group of substituents: -OR ₈₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₈₁ R _81' ; wherein R ₈₁ and R _{81' are} independently selected from hydrogen and substituted or unsubstituted C _1-6 alkane Radicals; optionally in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or At least two of the diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of the general formula (I) is a compound in which the alkyl, alkenyl or alkyne in the alkylaryl, alkylheterocyclyl or alkylcycloalkyl If the group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₁₃ R _13' ; wherein R ₁₃ and R _{13' are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of the general formula (I) is a compound wherein the aryl, heterocyclyl or alkylaryl, alkylheterocyclyl or alkylcycloalkyl If cycloalkyl is substituted and the substitution has not been otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _{14 '} , -NR ₁₄ C(O)R _14' , -NR ₁₄ S(O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S(O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S(O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; of which R ₁₄ , R _14' and R _14'' Independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted Cycloalkyl and unsubstituted heterocyclic groups; optionally in the form of stereoisomers, preferably mirror isomers or diastereoisomers, racemates, or stereoisomers At least two of the preferred mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the present invention is a compound wherein the aryl or heterocyclic group in R ₂ is substituted with one or more substituents selected from : Halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, Haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C (CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally in the form of stereoisomers, preferably mirror isomers or diastereomers, racemates, Or at least two of stereoisomers, preferably mirror isomers and/or diastereoisomers in the form of a mixture in any mixing ratio, or a corresponding salt or a corresponding solvate thereof.

In another embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₃ is substituted by one or more selected from the following Substituent substitution: -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₃₁ R _31' ; where the cycloalkyl group defined in R ₃ and also alkylcycloalkyl is substituted Then substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' ,- NR ₃₁ S(O) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _31' R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl and haloalkoxy; wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; one of stereoisomers, preferably mirror isomers or non-mirror isomers, extinction In the form of rotates, or in the form of mixtures of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates Thing.

In another embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted by one or more selected from the following Substituent substitution: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₃₂ R _32' ; wherein R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or One of the diastereomers, racemates, or a mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by one or more Substituted by a substituent selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₅₁ R _51' ; wherein the ring is as defined in R ₅ or alkylcycloalkyl If the alkyl group is substituted, it is substituted with one or more substituents selected from: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O) R _51' , -NR ₅₁ S(O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S( O)R ₅₁ , -S(O) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' , -OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the (etc.) substituent is preferably selected from halogen, -R ₅₁ , -OR ₅₁ ,- NR ₅₁ R _51' , -CN, haloalkyl and haloalkoxy; wherein R ₅₁ , R _51' and R _{51'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; in stereo isomers, preferably mirror isomers or diastereomers, as the case may be One, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, Or its corresponding solvate.

In another embodiment, the compound of the general formula (I) according to the present invention is a compound wherein the cycloalkyl group as defined in R ₅ -R _5′ is substituted by one or more selected from the following Substituent substitution: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' , -NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ ,- CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -OCH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _52' R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ , -OR ₅₂ , -NR ₅₂ R _52' , -CN, haloalkyl and haloalkanes Oxygen; wherein R ₅₂ , R _52' and R _{52'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and Substituted or unsubstituted C _2-6 alkynyl; optionally in the form of a stereoisomer, preferably mirror image isomer or diastereomer, racemate, or stereoisomer At least two of the compounds, the preferred mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another embodiment, the compound of general formula (I) according to the invention is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more selected from the following substituents: -OR _61, halogen, -CN, haloalkyl, haloalkoxy and -NR ₆₁ R _{61 ';} in R _6, also alkyl cycloalkyl, alkyl aryl and heterocyclyl group If the cycloalkyl, aryl or heterocyclic group defined in is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O)R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O ) NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the (etc.) substituent is preferably selected From halogen, -R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl and haloalkoxy; wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted Or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; stereoisomers are preferred, preferably One of the enantiomers or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably enantiomers, and/or diastereomers, in any form The form of the mixture in the mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by one or more selected from Substituent substitution: -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₇₁ R _71' ; as in R ₇ , also alkylcycloalkyl, alkylaryl and alkyl heterocycle If the cycloalkyl, aryl and heterocyclic group defined in the radical is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _71'' , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₇₁ , -C (O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ ; Preferably selected from halogen, -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; wherein R ₇₁ , R _71' and R _{71'' are} independently selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, One of the preferred enantiomers or diastereomers, racemate, or at least two of stereoisomers, preferred enantiomers and/or diastereomers In the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₈ or R _8′ is substituted by one or more Substitutions selected from the group consisting of -OR ₈₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₈₁ R _81' ; where R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted Substituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; stereoisomers, preferably mirror images, depending on the situation One of the structure or diastereomer, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of the general formula (I) is a compound in which the alkyl, alkenyl or alkyne in the alkylaryl, alkylheterocyclyl or alkylcycloalkyl If the group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, -OR ₁₃ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₁₃ R _13' ; in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment, the compound according to the invention of the general formula (I) is a compound wherein the aryl, heterocyclyl or alkylaryl, alkylheterocyclyl or alkylcycloalkyl If cycloalkyl is substituted and the substitution has not been otherwise defined, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₁₄ , -OR ₁₄ , -NO ₂ , -NR ₁₄ R _{14 '} , -NR ₁₄ C(O)R _14' , -NR ₁₄ S(O) ₂ R _14' , -S(O) ₂ NR ₁₄ R _14' , -NR ₁₄ C(O)NR _14' R _14'' , -SR ₁₄ , -S(O)R ₁₄ , -S(O) ₂ R ₁₄ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₁₄ , -C(O)NR ₁₄ R _14' , -OCH ₂ CH ₂ OR ₁₄ , -NR ₁₄ S(O) ₂ NR _14' R _14'' and -C(CH ₃ ) ₂ OR ₁₄ ; depending on the situation, stereoisomers, preferably mirror images One of the structure or diastereomer, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the aryl or heterocyclic group in R ₂ is substituted by one or more substitutions selected from Substitution: halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S( O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, halo Group, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; depending on the situation, it is in the form of one of stereoisomers, preferably enantiomers or diastereoisomers, racemates, or in the form of stereoisomers, At least two of the best mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₃ is substituted by one or more selected from Substituted by the following substituents: -OR ₃₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₃₁ R _31' One of them, in the form of a racemate, or in the form of a mixture of any mixture ratio of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, or The corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound in which the cycloalkyl group defined in R ₃ and also an alkylcycloalkyl group is substituted by one or more A substituent selected from the group consisting of: =O, halogen, -R ₃₁ , -OR ₃₁ , -NO ₂ , -NR ₃₁ R _31' , -NR ₃₁ C(O)R _31' , -NR ₃₁ S(O ) ₂ R _31' , -S(O) ₂ NR ₃₁ R _31' , -NR ₃₁ C(O)NR _31' R _31'' , -SR ₃₁ , -S(O)R ₃₁ , -S(O) ₂ R ₃₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₃₁ , -C(O)NR ₃₁ R _31' , -OCH ₂ CH ₂ OR ₃₁ , -NR ₃₁ S(O) ₂ NR _31' R _31'' and -C(CH ₃ ) ₂ OR ₃₁ ; the substituent(s) are preferably selected from halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, halogen Alkyl and haloalkoxy; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror images At least two of the isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound in which the cycloalkyl group defined in R ₃ and also an alkylcycloalkyl group is substituted by a Or more substituents selected from the group consisting of halogen, -R ₃₁ , -OR ₃₁ , -NR ₃₁ R _31' , -CN, haloalkyl, and haloalkoxy; stereoisomers are preferred, preferably One of the enantiomers or diastereomers, in the form of a racemate, or at least two of stereoisomers, preferably enantiomers, and/or diastereomers, in any form The form of the mixture in the mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R _3′ is substituted by one or more Substitute from the following substituents: -OR ₃₂ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₃₂ R _32' ; depending on the situation, stereoisomers, preferably mirror image isomers or non-mirror images One of the structures, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or Its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₅ and R _5′ is substituted by one or Multiple substituents selected from the group consisting of -OR ₅₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₅₁ R _51' ; optionally stereoisomers, preferably mirror isomers or One of the diastereomers, racemates, or a mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound of the general formula (I) according to the present invention is a compound in which the cycloalkyl group as defined in R ₅ and also an alkylcycloalkyl group is substituted by one or Multiple substituents selected from the group consisting of: =O, halogen, -R ₅₁ , -OR ₅₁ , -NO ₂ , -NR ₅₁ R _51' , -NR ₅₁ C(O)R _51' , -NR ₅₁ S( O) ₂ R _51' , -S(O) ₂ NR ₅₁ R _51' , -NR ₅₁ C(O)NR _51' R _51'' , -SR ₅₁ , -S(O)R ₅₁ , -S(O ) ₂ R ₅₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₁ , -C(O)NR ₅₁ R _51' , -OCH ₂ CH ₂ OR ₅₁ , -NR ₅₁ S(O ) ₂ NR _51' R _51'' and -C(CH ₃ ) ₂ OR ₅₁ ; the substituent(s) are preferably selected from halogen, -R ₅₁ , -OR ₅₁ , -NR ₅₁ R _51' , -CN, Haloalkyl and haloalkoxy; optionally in the form of stereoisomers, preferably mirror image isomers or diastereomers, racemates, or stereoisomers, preferably At least two of the enantiomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment, the compound of the general formula (I) according to the present invention is a compound in which the cycloalkyl group as defined in R ₅ -R _5′ is substituted by one or more selected from Substituted by the following substituents: =O, halogen, -R ₅₂ , -OR ₅₂ , -NO ₂ , -NR ₅₂ R _52' , -NR ₅₂ C(O)R _52' , -NR ₅₂ S(O) ₂ R _52' , -S(O) ₂ NR ₅₂ R _52' , -NR ₅₂ C(O)NR _52' R _52'' , -SR ₅₂ , -S(O)R ₅₂ , -S(O) ₂ R ₅₂ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₅₂ , -C(O)NR ₅₂ R _52' , -OCH ₂ CH ₂ OR ₅₂ , -NR ₅₂ S(O) ₂ NR _{52 '} R _52'' and -C(CH ₃ ) ₂ OR ₅₂ ; the substituent(s) are preferably selected from halogen, -R ₅₂ , -OR ₅₂ , -NR ₅₂ R _52' , -CN, haloalkyl and Haloalkoxy; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers At least two of the and/or diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₆ is substituted by one or more selected from Substituted by the following substituents: -OR ₆₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₆₁ R _61' ; stereoisomers, preferably mirror isomers or diastereomeric isomers as appropriate One of them, in the form of a racemate, or in the form of a mixture of any mixture ratio of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, or The corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound wherein R ₆ is also defined as alkylcycloalkyl, alkylaryl and alkylheterocyclic If the cycloalkyl, aryl or heterocyclic group is substituted, it is substituted with one or more substituents selected from the group consisting of: =O, halogen, -R ₆₁ , -OR ₆₁ , -NO ₂ , -NR ₆₁ R _61' , -NR ₆₁ C(O)R _61' , -NR ₆₁ S(O) ₂ R _61' , -S(O) ₂ NR ₆₁ R _61' , -NR ₆₁ C(O)NR _61' R _61'' , -SR ₆₁ , -S(O)R ₆₁ , -S(O) ₂ R ₆₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₆₁ , -C(O)NR ₆₁ R _61' , -OCH ₂ CH ₂ OR ₆₁ , -NR ₆₁ S(O) ₂ NR _61' R _61'' and -C(CH ₃ ) ₂ OR ₆₁ ; the substituent(s) are preferably selected from halogen,- R ₆₁ , -OR ₆₁ , -NR ₆₁ R _61' , -CN, haloalkyl, and haloalkoxy; one of stereoisomers, preferred mirror isomers, or non-mirror isomers, as the case may be , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Corresponding solvate.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₇ is substituted by one or more selected from Substitution with the following substituents: -OR ₇₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR ₇₁ R _71' One of them, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in the form of a mixture in any mixing ratio, or The corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the present invention of the general formula (I) is a compound as defined in R ₇ , also alkylcycloalkyl, alkylaryl and alkylheterocyclyl If the cycloalkyl, aryl and heterocyclic groups are substituted, they are substituted by one or more substituents selected from the group consisting of: =O, halogen, -R ₇₁ , -OR ₇₁ , -NO ₂ , -NR ₇₁ R _71' , -NR ₇₁ C(O)R _71' , -NR ₇₁ S(O) ₂ R _71' , -S(O) ₂ NR ₇₁ R _71' , -NR ₇₁ C(O)NR _71' R _{71 ''} , -SR ₇₁ , -S(O)R ₇₁ , -S(O) ₂ R ₇₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₇₁ , -C(O)NR ₇₁ R _71' , -OCH ₂ CH ₂ OR ₇₁ , -NR ₇₁ S(O) ₂ NR _71' R _71'' and -C(CH ₃ ) ₂ OR ₇₁ ; the substituent(s) are preferably selected from halogen , -R ₇₁ , -OR ₇₁ , -NR ₇₁ R _71' , -CN, haloalkyl and haloalkoxy; the best halogen; stereoisomers, preferably mirror isomers or non-mirror isomers depending on the situation One of the structures, the racemate, or a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in any mixture ratio, or Its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein the alkyl, alkenyl or alkynyl group defined in R ₈ or R _8′ is substituted by one or Multiple substituents selected from the group consisting of: -OR ₈₁ , halogen, -CN, haloalkyl, haloalkoxy, and -NR ₈₁ R _81' ; optionally stereoisomers, preferably mirror isomers or One of the diastereomers, racemate, or a mixture of stereoisomers, preferably mirror isomers, and/or at least two of the diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound of the general formula (I) according to the present invention is a compound wherein X is a bond, -[C(R _a R _b )] _p -, -[C(R _a R _b )] _p C(O)[C(R _c R _d )] _q -, -[C(R _a R _b )] _p C(O)N(R _z )[C(R _c R _d )] _q- , [C(R _a R _b )] _p N(R _z )C(O)[C(R _c R _d )] _q -or-[C(R _a R _b )] _p N(R _z )[C (R _c R _d )] _q -; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl and -C(O)-C _1-6 alkyl; R _{a is} selected from hydrogen , Halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{b is} selected from hydrogen , Halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which it is attached form a substituted or unsubstituted cycloalkyl; R _{c is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; _{Rd is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkene Radicals and substituted or unsubstituted C _2-6 alkynyl groups; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereoisomers, racemates, or At least two of the stereoisomers, preferably mirror isomers, and/or diastereoisomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment, the compound of the general formula (I) according to the present invention is a compound wherein X is a bond, -[C(R _a R _b )] _p -, -[C(R _a R _b )] _p C(O)[C(R _c R _d )] _q -, -[C(R _a R _b )] _p C(O)N(R _z )[C(R _c R _d )] _q- , [C(R _a R _b )] _p N(R _z )C(O)[C(R _c R _d )] _q -or-[C(R _a R _b )] _p N(R _z )[C (R _c R _d )] _q -; depending on the situation, it is in the form of one of stereoisomers, preferably mirror isomers or diastereoisomers, racemates, or stereoisomers, relatively At least two of the good mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C( O)-C _1-6 alkyl; optionally in the form of a stereoisomer, preferably an enantiomer or a non-image isomer, a racemate, or in the form of a stereoisomer, At least two of the good mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein R _{a is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers, In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding Solvate.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein R _{b is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or diastereomers, In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding Solvate.

In another preferred embodiment, formula (I) compound is the following compound according to the present invention, form a cycloalkyl substituted or non-substituted with wherein R _a and R _b carbon connected thereto of atoms; optionally In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein R _{c is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; as the case may be one of stereoisomers, preferably mirror isomers or non-mirror isomers, extinction In the form of rotates, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates Thing.

In another preferred embodiment, the compound according to the invention of the general formula (I) is a compound wherein _{Rd is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally one of stereoisomers, preferably mirror isomers or non-mirrors, exo In the form of rotates, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates Thing.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein X is selected from a bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C (O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; preferably, X is selected from a bond, -[C(R _a R _b )] _p -and -[CH ₂ ] _p C(O)[CH ₂ ] _q -; more preferably selected from bonds, -CH ₂ -, -CH ₂ CH ₂ -, -CH ₂ CH(methyl)- and -C(O)-; and/or R _{a is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; the best, R _a type hydrogen or substituted or non-substituted methyl; and / or R _b is selected from hydrogen, halo, a substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl group and the substituted or unsubstituted C _2-6 alkynyl; preferably, R _b based hydrogen; and / or R _a and R _b form a substituted or non-together with the carbon atom to which the Substituted cycloalkyl; and/or R ₁ is; and/or R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl , Substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O)-C _1-6 alkane Base; and/or p is 0, 1, 2, 3, 4 or 5; preferably, p is 0, 1 or 2; and/or q is 0, 1, 2, 3, 4 or 5; preferably Ground, q is 0; and/or Y ₁ is -C(R ₁₀ R _10' )-; preferably Y ₁ is -CH ₂ -; and/or Y ₂ is -C(R ₁₀ R _10' )-; Preferably Y ₂ -CH ₂ -; and/or n is 0 or 1; preferably n is 0; and/or m is 0, 1 or 2; preferably m is 1; and/or r is 0 , 1 or 2; preferably, r is 1; and/or Y is -CH ₂ -or C=O; and/or R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted Heterocyclic group; preferably, R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclic group, more preferably, R ₂ is selected from phenyl and thiophene Substituted or unsubstituted groups; and/or R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or Unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; preferably, R ₃ is hydrogen or substituted or unsubstituted C _1-6 alkyl; more preferably, R ₃ is hydrogen, substituted or unsubstituted methyl or substituted or unsubstituted ethyl; and/or R _3'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; the best, R _{3 'based} hydrogen; and / or R ₄ and R _4' are independently selected from _{halogen, -R 41, -OR 41, -NO} 2, -NR 41 R 41 ', -NR 41 C (O) R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S( O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; preferably, both R ₄ and R _{4 '} are -R ₄₁ , more preferably , R ₄ and R _{4 ′} are both hydrogen; and/or R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, Substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; preferably, R ₅ is substituted or unsubstituted Substituted C _1-6 alkyl; more preferably, R ₅ is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; and/or R _{5′ is} selected from hydrogen, substituted or unsubstituted Substituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, R _{5′ is} selected from hydrogen and Substituted or unsubstituted methyl; and/or R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; preferably substituted or unsubstituted cyclopropyl; and /Or R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Substituted heterocyclic group, substituted or unsubstituted alkyl heterocyclic group and -C(O)R ₇ ; preferably, R _{6 is} selected from substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic group, and -C(O) R ₇ ; more preferably, R _{6 is} selected from substituted or Unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted isopropyl, substituted or unsubstituted cyclopropyl, substituted or unsubstituted phenyl, Substituted or unsubstituted pyridine, substituted or unsubstituted benzyl and substituted or unsubstituted benzyl; and/or R _{7 is} selected from substituted or unsubstituted C _1-6 alkanes Group, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl Cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic; Preferably, R ₇ is substituted or unsubstituted aryl; more preferably, R ₇ is substituted or unsubstituted phenyl; and/or R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted Substituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR ₈₁ ; preferably, R ₈ is hydrogen; And/or R _8'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkyne Radical; preferably, R _8′ is hydrogen; and/or R ₉ and R _{9′ are} independently selected from halogen, —R ₂₁ , —OR ₂₁ , —NO ₂ , —NR ₂₁ R _21′ , —NR ₂₁ C (O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH _{2 CH 2 OR 21, -NR 21} S (O) 2 NR 21 'R 21'' and _{-C (CH 3) 2 OR 21} ; preferably, R ₉ and R _9' and Both lines -R _21; More preferably, R ₉ and R _{9 'and} Both-based hydrogen; and / or R ₁₀ and R _10' are independently selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non- Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, both R ₁₀ and R _10′ are hydrogen; and/or R ₁₀ and R _10′ are connected to Carbon atoms together form a substituted or unsubstituted cycloalkyl; and/or R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, both R _10″ and R _10′″ are hydrogen; and/or R _{10 ''} And R _10′'' together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; and/or R ₁₃ and R _{13′ are} independently selected from hydrogen, unsubstituted C _1-6 alkyl Group, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; and/or R ₁₄ , R _14′ and R _{14″ are} independently selected from hydrogen, unsubstituted C _{1 -6} alkyl, unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group; And/or R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted Or unsubstituted C _2-6 alkynyl; and/or R ₃₁ , R _31′ and R _{31″ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; and/or R ₃₂ and R _{32′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; and/or R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen , Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and substituted or unsubstituted Cycloalkyl; preferably, R ₄₁ is hydrogen; and/or R ₅₁ , R _51′ and R _{51″ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; and/or R ₅₂ , R _52′ and R _{52'' are} independently selected from hydrogen, substituted or unsubstituted Substituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; and/or R ₆₁ , R _61' and R _61'' Independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; and /Or R ₇₁ , R _71' and R _{71'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or Unsubstituted C _2-6 alkynyl; and/or R ₈₁ and R _{81′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally in the form of stereoisomers, preferably mirror isomers or diastereomers, racemates, Or in the form of a mixture of any mixture ratio of at least two of stereoisomers, preferably mirror isomers and/or diastereoisomers, Or its corresponding salt, or its corresponding solvate.

及/或 m係0、1或2； 及/或 r係0、1或2； 及/或 Y係-CH₂ -或C=O； 及/或 R_a 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；更佳甲基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R_b 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R_a 及R_b 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 R_z 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C_1-6 烷基； 其中 該烷基係C_1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 R₂ 選自經取代或未經取代之芳基及經取代或未經取代之雜環基， 其中 該芳基選自苯基、萘基或蒽；較佳係萘基及苯基；較佳地，該芳基係苯基； 及/或 該雜環基係一或多個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子；較佳係一個或兩個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、六氫吡啶、六氫吡嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫吡喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、異喹啉、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、嘧啶、苯并二氧戊環、苯并二噁烷、咔唑、吲哚啉-2-酮及喹唑啉；較佳地，雜環基係噻吩； 及/或 R₃ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中 該烷基係C_1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C_1-6 烷基係甲基或乙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 R_3’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₄ 及R_4’ 獨立地選自鹵素、-R₄₁ 、-OR₄₁ 、-NO₂ 、-NR₄₁ R_41’ 、-NR₄₁ C(O)R_41’ 、-NR₄₁ S(O)₂ R_41’ 、-S(O)₂ NR₄₁ R_41’ 、-NR₄₁ C(O)NR_41’ R_41’’ 、-SR₄₁ 、-S(O)R₄₁ 、-S(O)₂ R₄₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₄₁ 、-C(O)NR₄₁ R_41’ 、-OCH₂ CH₂ OR₄₁ 、-NR₄₁ S(O)₂ NR_41’ R_41’’ 及-C(CH₃ )₂ OR₄₁ ； 其中 該烷基係C_1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 R₅ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C_1-6 烷基係甲基或乙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R_5’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳甲基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₅ 及R_5’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基；較佳地，該環烷基係環丙基； 及/或 R₆ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基及-C(O)R₇ ； 其中 該烷基係C_1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該烷基係甲基； 及/或 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C_1-6 烷基係甲基、乙基或異丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基；較佳環丙基； 及/或 該芳基選自苯基、萘基或蒽；較佳係萘基及苯基；較佳地，該芳基係苯基； 及/或 該雜環基係一或多個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子；較佳係一個或兩個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、六氫吡啶、六氫吡嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫吡喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、異喹啉、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、嘧啶、苯并二氧戊環、苯并二噁烷、咔唑、吲哚啉-2-酮及喹唑啉；較佳地，雜環基係吡啶； 及/或 R₇ 選自經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基、經取代或未經取代之芳基、經取代或未經取代之烷基芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基雜環基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 該芳基選自苯基、萘基或蒽；較佳係萘基及苯基；較佳地，該芳基係苯基； 及/或 該雜環基係一或多個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子；較佳係一個或兩個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、六氫吡啶、六氫吡嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫吡喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、異喹啉、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、嘧啶、苯并二氧戊環、苯并二噁烷、咔唑、吲哚啉-2-酮及喹唑啉； 及/或 R₈ 選自氫、鹵素、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及-OR₈₁ ； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R_8’ 選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該烷基係C_1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 R₉ 及R_9’ 獨立地選自鹵素、-R₂₁ 、-OR₂₁ 、-NO₂ 、-NR₂₁ R_21’ 、-NR₂₁ C(O)R_21’ 、-NR₂₁ S(O)₂ R_21’ 、-S(O)₂ NR₂₁ R_21’ 、-NR₂₁ C(O)NR_21’ R_21’’ 、-SR₂₁ 、-S(O)R₂₁ 、-S(O)₂ R₂₁ 、-CN、鹵烷基、鹵烷氧基、-C(O)OR₂₁ 、-C(O)NR₂₁ R_21’ 、-OCH₂ CH₂ OR₂₁ 、-NR₂₁ S(O)₂ NR_21’ R_21’’ 及-C(CH₃ )₂ OR₂₁ ； 其中 該烷基係C_1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 R₁₀ 及R_10’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₁₀ 及R_10’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 R_10’’ 及R_10’’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R_10’’ 及R_10’’’ 與其連接之碳原子一起形成經取代或未經取代之環烷基； 其中 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 R₁₃ 及R_13’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基及未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₁₄ 、R_14’ 及R_14’’ 獨立地選自氫、未經取代之C_1-6 烷基、未經取代之C_2-6 烯基、未經取代之C_2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 該芳基選自苯基、萘基或蒽；較佳係萘基及苯基； 及/或 該雜環基係一或多個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子；較佳係一個或兩個飽和或不飽和環之雜環系統，其中至少一個環在環中含有一或多個選自由氮、氧及/或硫組成之群之雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、六氫吡啶、六氫吡嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫吡喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、異喹啉、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、嘧啶、苯并二氧戊環、苯并二噁烷、咔唑、吲哚啉-2-酮及喹唑啉； 及/或 R₂₁ 、R_21’ 及R_21’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，更佳地，該C_1-6 烷基係甲基、乙基或丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₃₁ 、R_31’ 及R_31’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₃₂ 及R_32’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₄₁ 、R_41’ 及R_41’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基、經取代或未經取代之C_2-6 炔基及經取代或未經取代之環烷基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，更佳地，該C_1-6 烷基係甲基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 該環烷基係C_3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳係C_3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C_3-6 環烷基，如環丙基、環丁基、環戊基或環己基； 及/或 R₅₁ 、R_51’ 及R_51’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₅₂ 、R_52’ 及R_52’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₆₁ 、R_61’ 及R_61’’ 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，更佳地，該C_1-6 烷基係甲基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₇₁ 、R_71’ 及R_{71 ’’} 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 及/或 R₈₁ 及R_{81 ’} 獨立地選自氫、經取代或未經取代之C_1-6 烷基、經取代或未經取代之C_2-6 烯基及經取代或未經取代之C_2-6 炔基； 其中 該C_1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基； 及/或 該C_2-6 -烯基較佳選自乙烯基、丙烯基、丁烯基、戊烯基、己烯基、異丙烯基及異丁烯基； 及/或 該C_2-6 -炔基較佳選自乙炔基、丙炔基、丁炔基、戊炔基、己炔基、異丙炔及異丁炔； 視情況呈立體異構物、較佳鏡像異構物或非鏡像異構物中之一者、外消旋物之形式，或呈立體異構物、較佳鏡像異構物及/或非鏡像異構物中之至少兩者呈任何混合比率之混合物的形式，或其相應鹽、或其相應溶劑合物。In another preferred embodiment, the compound of general formula (I) according to the present invention is a compound wherein X is selected from the group consisting of -[C(R _a R _b )] _p -, -[CH ₂ ] _p C (O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; and/or p is 0, 1, 2, 3, 4 or 5; and/or q is 0, 1, 2, 3, 4 or 5; and/or n series 0 or 1; and/or Y ₁ series-C(R ₁₀ R _10' )-; and/or Y ₂ series-C(R _10'' R _10''' )-; and/or R ₁ series

And / or 0, 1 or 2 m based; and / or lines r 0,1 or 2; and / or Y-based -CH ₂ - or C = O; and / or R _a is selected from hydrogen, halogen, substituted or Unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein C _1-6 alkyl is preferably selected from Methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; more preferably methyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl , Propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentyl Alkynyl, hexynyl, isopropyne and isobutyne; and/or R _{b is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl Or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl, and isobutenyl; and/ Or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutyne; and/or R _a and R _b are connected thereto The carbon atoms of together form a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is a C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or Cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl , Cyclobutyl, cyclopentyl or cyclohexyl; and/or R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, Substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C(O)-C _1-6 alkyl; Wherein the alkyl group is C _1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _1-6 alkyl The group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferably selected from vinyl , Propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentyl Alkynyl, hexynyl, isopropyne and isobutyne; and/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl Or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl Group, cyclobutyl, cyclopentyl or cyclohexyl; and/or R _{2 is} selected from substituted or unsubstituted Substituted aryl and substituted or unsubstituted heterocyclic, wherein the aryl is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl is phenyl ; And/or the heterocyclic group is one or more heterocyclic ring systems of saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring Preferably a heterocyclic ring system with one or two saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably selected from Oxazepane, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzene Thiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrole P[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, Pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably, heterocyclic group thiophene; and/or R _{3 is} selected from hydrogen, Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkane Group and substituted or unsubstituted alkylcycloalkyl; wherein the alkyl group is C _1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2 -Methylpropyl; and/or the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; Preferably, the C _1-6 alkyl is methyl or ethyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, iso Propenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutynyl; and/ Or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as Cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or R _3'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is It is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, propynyl, Butynyl, pentynyl, hexynyl, isopropyne and isobutyne; and/or R ₄ and R _4′ alone Site selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S( O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkane Group, haloalkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; wherein the alkyl group is C _1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl ; And/or R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkyne Group, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; wherein the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, Amyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C _1-6 alkyl is methyl or ethyl; and/or the C _2-6 -alkenyl is preferably selected from ethylene Group, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, Pentynyl, hexynyl, isopropyne and isobutyne; and/or R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl Or 2-methylpropyl; preferably methyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and Isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutynyl; and/or R ₅ And R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclo Hexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkane Group, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably, the cycloalkyl is cyclopropyl; and/or R _{6 is} selected from hydrogen, substituted or unsubstituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, Substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted Substituted alkyl heterocyclic group and -C(O)R ₇ ; wherein the alkyl group is a C _1-6 alkyl group, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the alkyl is methyl; and/or the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, iso Propyl or 2-methylpropyl; preferably, the C _1-6 alkyl is methyl, ethyl or isopropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, Propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl Group, hexynyl, isopropyne and isobutyne; and/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or Cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl , Cyclobutyl, cyclopentyl or cyclohexyl; preferably cyclopropyl; and/or the aryl group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl group Is a phenyl group; and/or the heterocyclic group is one or more heterocyclic ring systems of saturated or unsaturated rings, wherein at least one ring contains one or more rings selected from the group consisting of nitrogen, oxygen and/or sulfur Heteroatom; preferably a heterocyclic ring system with one or two saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more Preferably selected from oxaziridine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benfuran, benzimidazole, indole Azole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyridine Azine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant Pyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably, heterocyclyl pyridine; and/or R _{7 is} selected from Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted ring Alkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclyl, Substituted or unsubstituted alkyl heterocyclic group; wherein the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl Group; and/or the C _2-6 -alkenyl group is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, Isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutynyl; and /Or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or The aryl group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl is phenyl; and/or the heterocyclic group is one or more saturated or unsaturated rings Heterocyclic ring system, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur in the ring; preferably a heterocyclic ring system with one or two saturated or unsaturated rings, At least one of the rings contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably selected from oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole , Azetidine, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran , Morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, Benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, Indoline-2-one and quinazoline; and/or R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl , Substituted or unsubstituted C _2-6 alkynyl and -OR ₈₁ ; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl Or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl, and isobutenyl; and /Or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl, and isobutyne; and/or R _{8′ is} selected from hydrogen , Substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the alkyl is C _{1 -6} alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _1-6 alkyl is preferably selected from methyl , Ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl , Pentenyl, hexenyl, isopropenyl and isobutenyl; and/or R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O ) R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein the alkyl group is C _1-6 alkyl, such as methyl, ethyl, propyl, Butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or R ₁₀ and R _{10′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted Or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, Pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, iso Propenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutynyl; and/ Or R ₁₀ and R _10' together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is a C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentane Group, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _{3- 6} cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and / or R _{10 ''} and R _{10 '''are} independently selected from hydrogen, substituted or non-substituted C _{1- 6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, Propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl , Hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and Isobutyne; and/or R _10'' and R _10''' together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is a C _3-8 cycloalkyl, such as Cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or Cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl; and/or R ₁₃ and R _{13′ are} independently selected from hydrogen, not taken Substituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propylene Group, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferably selected from vinyl, propenyl, butenyl, pentenyl, Hexenyl, isopropenyl, and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl, and iso Butyne; and/or R ₁₄ , R _14′ and R _{14″ are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl, and unsubstituted heterocyclic group; wherein the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, Butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexene Group, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutynyl ; And/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl Groups such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl groups such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and /Or the aryl group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; and/or the heterocyclic group is one or more heterocyclic ring systems of saturated or unsaturated rings, at least one ring Contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur in the ring; preferably a heterocyclic ring system with one or two saturated or unsaturated rings, in which at least one ring contains a Or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur, more preferably selected from oxaziridine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, Pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan , Triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5- Thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinoline Oxazoline; and/or R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl And substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2- Methylpropyl, more preferably, the C _1-6 alkyl is methyl, ethyl Or propyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl, and isobutenyl; and/or the C _{2 -6} -alkynyl is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutyne; and/or R ₃₁ , R _31' and R _31'' Independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is It is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, propynyl, Butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; and/or R ₃₂ and R _{32' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl , Pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, Isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutynyl; and /Or R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or Unsubstituted C _2-6 alkynyl and substituted or unsubstituted cycloalkyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl , Isopropyl or 2-methylpropyl, more preferably, the C _1-6 alkyl is methyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butene Group, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl , Isopropyne and isobutyne; and/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; Preferred is C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, Cyclopentyl or cyclohexyl; and/or R ₅₁ , R _51' and R _{51'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2 -6} alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl Base or 2-methyl Propyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _{2- 6} -alkynyl is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutyne; and/or R ₅₂ , R _52' and R _52'' independently Selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _{The 1-6} alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferred Selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, propynyl, butylene Alkynyl, pentynyl, hexynyl, isopropyne and isobutyne; and/or R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 Alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propylene Group, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl, more preferably, the C _1-6 alkyl is methyl; and/or the C _2-6 -alkenyl is preferably selected From vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl Group, pentynyl, hexynyl, isopropyne and isobutyne; and/or R ₇₁ , R _71' and R _{71 '' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkane Group, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl , Butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexyl Alkenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutyl Alkyne; and/or R ₈₁ and R _{81 'are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, and substituted or unsubstituted Substituted C _2-6 alkynyl; wherein the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and /Or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl Preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutyne; optionally stereoisomers, preferably mirror isomers or non-mirrors Like one of the isomers, racemate, or as a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which, in R _a as defined in any of the embodiments of the present invention, the C _1-6 alkyl The group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; more preferably methyl; and/or the C _2-6 -alkenyl group It is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, propynyl, Butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; as the case may be, one of stereoisomers, preferably mirror isomers or diastereomers, racemates In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which, in R _b as defined in any of the embodiments of the present invention, the C _1-6 alkyl The group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferably selected from vinyl , Propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentyl Alkynyl, hexynyl, isopropyne and isobutyne; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates, or stereo At least two of the isomers, preferably mirror image isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which, in R _a -R _b as defined in any of the embodiments of the present invention, the cycloalkane The base is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, Cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; optionally stereoisomers, One of the preferred enantiomers or diastereomers, racemate, or at least two of stereoisomers, preferred enantiomers and/or diastereomers In the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein in R _z as defined in any of the embodiments of the present invention, the alkyl group is C _{1 -6} alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _1-6 alkyl is preferably selected from methyl , Ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl , Pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, Isopropyne and isobutyne; and/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably System C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclo Amyl or cyclohexyl; optionally in the form of one of stereoisomers, preferred mirror isomers or diastereoisomers, racemates, or stereoisomers, preferred mirror isomers At least two of the compounds and/or diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein in R ₂ as defined in any of the embodiments of the present invention, the aryl group is selected from benzene Group, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl group is phenyl; and/or the heterocyclic group is one or more heterocyclic ring systems of saturated or unsaturated rings, wherein At least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur; preferably a heterocyclic ring system with one or two saturated or unsaturated rings, wherein at least one ring is in the ring Contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur, more preferably selected from oxaziridine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine , Pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indole Porphyrin, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2 ,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2- Ketone and quinazoline; preferably, heterocyclic thiophene; optionally in the form of one of stereoisomers, preferably enantiomers or diastereomers, racemates, or At least two of the stereoisomers, preferably mirror isomers, and/or diastereoisomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which, in R ₃ as defined in any of the embodiments of the present invention, the alkyl group is C _{1 -6} alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _1-6 alkyl is preferably selected from methyl , Ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C _1-6 alkyl is methyl or ethyl; and/or the C _{2 -6} -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from acetylene Group, propynyl, butynyl, pentynyl, hexynyl, isopropyne and isobutyne; and/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl , Cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl; as the case may be, one of stereoisomers, preferably mirror isomers, or diastereomers, external In the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding solvent Compound.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein in R _3′ as defined in any of the embodiments of the present invention, the C _1-6 The alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferably selected from ethylene Group, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, Pentynyl, hexynyl, isopropyne, and isobutyne; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates, or At least two of the stereoisomers, preferably mirror isomers, and/or diastereoisomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to the general formula (I), the compound is a compound wherein in R ₄ and R _4′ as defined in any of the embodiments of the present invention, the alkane The base is C _1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; stereoisomers are preferred, mirror image is preferred One of the structure or diastereomer, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to the general formula (I), the compound is a compound wherein in R ₅ as defined in any of the embodiments of the present invention, the C _1-6 alkyl The group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C _1-6 alkyl is methyl or ethyl ; And/or the C _2-6 -alkenyl group is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6- The alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl and isobutyne; stereoisomers, preferably mirror image isomers or non-mirror images as appropriate One of the isomers, the racemate, or at least two of the stereoisomers, preferably the mirror isomers, and/or the diastereomers, in the form of a mixture in any mixing ratio, Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein in R _5′ as defined in any of the embodiments of the present invention, the C _1-6 The alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably methyl; and/or the C _2-6 -alkenyl It is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl and propynyl , Butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; as the case may be, stereoisomers, preferred mirror isomers or non-mirror isomers, racemates In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to the general formula (I), the compound is a compound wherein in R ₅ and R _5′ as defined in any of the embodiments of the present invention, the ring Alkyl is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl , Cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably, cycloalkyl Cyclopropyl; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers At least two of the and/or diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein in R ₆ as defined in any of the embodiments of the present invention, the alkyl group is C _{1 -6} alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the alkyl is methyl; and/or the C _1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C _1-6 alkyl is Group, ethyl or isopropyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and /Or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; and/or the cycloalkyl system C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl , Cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably cyclopropyl; and/or the aromatic The group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl is phenyl; and/or the heterocyclic group is one or more heterocyclic saturated or unsaturated rings Ring system, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably a heterocyclic ring system with one or two saturated or unsaturated rings, wherein at least A ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably selected from oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, nitrogen Heterocyclobutane, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, Porphyrin, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo -1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indole Quinolin-2-one and quinazoline; preferably, heterocyclyl pyridine; one of stereoisomers, preferably enantiomers or diastereomers, racemates as the case may be In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the present invention according to the general formula (I), the compound is a compound wherein in R ₇ as defined in any of the embodiments of the present invention, the C _1-6 alkyl The group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferably selected from vinyl , Propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentyl Alkynyl, hexynyl, isopropyne and isobutyne; and/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl Or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl Group, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl is phenyl; and /Or the heterocyclic group is a heterocyclic system of one or more saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; It is preferably a heterocyclic ring system with one or two saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably selected from oxygen and nitrogen Heterocycloheptane, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzothiazole , Benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[ 2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, pyrimidine, Benzodioxolane, benzodioxane, carbazole, indoline-2-one, and quinazoline; stereoisomers, preferably mirror-isomers or diastereomers, as the case may be One, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, Or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein in R ₈ as defined in any of the embodiments of the present invention, the C _1-6 alkyl The group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferably selected from vinyl , Propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentyl Alkynyl, hexynyl, isopropyne and isobutyne; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates, or stereo At least two of the isomers, preferably mirror image isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which, in R _8′ as defined in any of the embodiments of the present invention, the alkyl group is C _1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _1-6 alkyl is preferably selected from methyl Group, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferably selected from vinyl, propenyl, butene Radical, pentenyl, hexenyl, isopropenyl and isobutenyl; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates, or At least two of the stereoisomers, preferably mirror isomers and/or diastereoisomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which in R ₉ and R _9′ as defined in any of the embodiments of the present invention, the alkane The base is C _1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; stereoisomers are preferred, mirror image is preferred One of the structure or diastereomer, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which, in R ₁₀ and R _10′ as defined in any of the embodiments of the present invention, the C _{The 1-6} alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferred Selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, propynyl, butylene Alkynyl, pentynyl, hexynyl, isopropyne and isobutyne; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates , Or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein in R ₁₀ and R _10′ as defined in any of the embodiments of the present invention, the ring Alkyl is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl , Cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; stereoisomers as appropriate , One of the preferred enantiomers or diastereomers, racemates, or at least two of the stereoisomers, preferred enantiomers and/or diastereomers They are in the form of mixtures of any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R _10'' and R _10''' as defined in any of the embodiments of the present invention Among them, the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6- The alkenyl group is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propylene Alkynyl, butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; depending on the situation, one of stereoisomers, preferred mirror isomers, or non-mirror isomers, extinction In the form of rotates, or in the form of mixtures of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or their corresponding salts, or their corresponding solvates Thing.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R _10'' and R _10''' as defined in any of the embodiments of the present invention In this, the cycloalkyl group is a C _3-8 cycloalkyl group, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably C _3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; as appropriate One of the stereoisomers, preferred mirror isomers or diastereomers, racemate, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to the general formula (I), the compound is a compound wherein in R ₁₃ and R _13′ as defined in any of the embodiments of the present invention, the C _{The 1-6} alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferred Selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, propynyl, butylene Alkynyl, pentynyl, hexynyl, isopropyne and isobutyne; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates , Or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₁₄ , R _14′ and R _14′ as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -Alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, Propynyl, butynyl, pentynyl, hexynyl, isopropyne and isobutyne; and/or the cycloalkyl group is C _3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclo Amyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably from C _{3 -6} cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; and/or The heterocyclic group is a heterocyclic system of one or more saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur in the ring; preferably Heterocyclic system of one or two saturated or unsaturated rings, wherein at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and/or sulfur in the ring, more preferably selected from oxygen-nitrogen heterocycles Heptane, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, hexahydropyridine, hexahydropyrazine, benzofuran, benzimidazole, indazole, benzothiazole, benzene Pyridazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2, 3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant pyrrolidine, pyrimidine, benzo Dioxolane, benzodioxane, carbazole, indoline-2-one, and quinazoline; depending on the situation, one of stereoisomers, preferred mirror isomers, or diastereomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Corresponding solvate.

In another preferred embodiment of the present invention according to the general formula (I), the compound is a compound in which R ₂₁ , R _21′ and R _21′ as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl, more preferably, the C _{1- 6} alkyl is methyl, ethyl or propyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and Isobutenyl; and/or the C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropynyl, and isobutynyl; One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₃₁ , R _31′ and R _31′ as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -Alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, Propynyl, butynyl, pentynyl, hexynyl, isopropynyl, and isobutynyl; depending on the situation, one of stereoisomers, preferred mirror isomers, or non-mirror isomers , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Corresponding solvate.

In another preferred embodiment of the present invention according to the general formula (I), the compound is a compound in which, in R ₃₂ and R _32′ as defined in any of the embodiments of the present invention, the C _{The 1-6} alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -alkenyl group is preferred Selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, propynyl, butylene Alkynyl, pentynyl, hexynyl, isopropyne and isobutyne; optionally in the form of one of stereoisomers, preferably mirror isomers or diastereomers, racemates , Or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₄₁ , R _41' and R _41' as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl, more preferably, the C _{1- 6} alkyl methyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or The C _2-6 -alkynyl group is preferably selected from the group consisting of ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; and/or the cycloalkyl group C _{3- 8} cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C _3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclo Amyl, cyclohexyl, or cycloheptyl; more preferably from C _3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl; stereoisomers, preferably mirror image isomers, as appropriate One of the compounds or diastereomers, racemate, or at least two of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₅₁ , R _51′ and R _51′ as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -Alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, Propynyl, butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; depending on the situation, one of stereoisomers, preferred mirror isomers, or diastereomers, external In the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding solvent Compound.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₅₂ , R _52′ and R _52′ as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -Alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, Propynyl, butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; depending on the situation, one of stereoisomers, preferred mirror isomers, or diastereomers, external In the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding solvent Compound.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₆₁ , R _61′ and R _61′ as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl, more preferably, the C _{1- 6} alkyl methyl; and/or the C _2-6 -alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or The C _2-6 -alkynyl group is preferably selected from ethynyl, propynyl, butynyl, pentynyl, hexynyl, isopropyne and isobutyne; stereoisomers, preferably mirror images, as the case may be One of the isomers or diastereomers, racemates, or any mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixture In the form of a mixture of ratios, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₇₁ , R _{71 ′} and R _{71 ′} as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -Alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, Propynyl, butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; depending on the situation, one of stereoisomers, preferred mirror isomers, or diastereomers, external In the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers, in any mixing ratio, or its corresponding salt, or its corresponding solvent Compound.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₈₁ , R _{81 ′} and R _{81 ′} as defined in any of the embodiments of the present invention _' , the C _1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; and/or the C _2-6 -Alkenyl is preferably selected from vinyl, propenyl, butenyl, pentenyl, hexenyl, isopropenyl and isobutenyl; and/or the C _2-6 -alkynyl is preferably selected from ethynyl, Propynyl, butynyl, pentynyl, hexynyl, isopropyne, and isobutyne; depending on the situation, one of stereoisomers, preferred mirror isomers, or diastereomers, external In the form of a racemate, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding solvent Compound.

In another preferred embodiment of the present invention according to general formula (I), the compound is as follows, wherein p is 0, 1, 2, 3, 4 or 5; preferably, p is 0, 1 or 2; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is as follows, wherein q is 0, 1, 2, 3, 4 or 5; preferably, q is 0; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is as follows, wherein n is 0 or 1; preferably n is 0; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is as follows, wherein m is 0, 1 or 2; preferably, m is 1; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is as follows, wherein r is 0, 1 or 2; preferably, r is 1; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein X is selected from a bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C (O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; preferably, X is selected from a bond, -[C(R _a R _b )] _p -and -[CH ₂ ] _p C(O)[CH ₂ ] _q -; more preferably selected from bond, -CH ₂ -, -CH ₂ CH ₂ -, -CH ₂ CH(methyl)- and -C(O)-; stereoscopic as the case may be Isomers, one of the preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{a is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or the unsubstituted C _2-6 alkenyl group and the substituted or unsubstituted C _2-6 alkynyl; preferably, R _a type hydrogen or substituted or non-substituted methyl group; optionally stereoisomeric form , One of the preferred enantiomers or diastereomers, the racemate, or at least one of the stereoisomers, preferred enantiomers and/or diastereomers The two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{b is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, R _b is hydrogen; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixture ratio , Or its corresponding salt, or its corresponding solvate.

In accordance with another embodiment of formula (I) of the preferred embodiment of the invention, the compound is the following compound, which form a cycloalkyl substituted or unsubstituted together with the carbon atoms of R _a and R _b of connected thereto; optionally In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein Y is -CH ₂ -or C=O; optionally stereoisomers, preferably mirror isomers Or one of the diastereomers, racemates, or a mixture of stereoisomers, preferably mirror isomers and/or diastereomers in any mixing ratio Form, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which Y ₁ is -C(R ₁₀ R _10' )-; preferably Y ₁ is -CH ₂ -; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein Y ₂ is -C(R ₁₀ R _10' )-; preferably Y ₂ is -CH ₂ -; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, and -C( O)-C _1-6 alkyl; optionally in the form of a stereoisomer, preferably an enantiomer or a non-image isomer, a racemate, or in the form of a stereoisomer, At least two of the good mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclic group; Preferably, R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclic groups, more preferably, R ₂ is selected from phenyl and thiophene substituted or unsubstituted Substituted groups; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers At least two of the and/or diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{3 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; preferably , R ₃ is hydrogen or substituted or unsubstituted C _1-6 alkyl; more preferably, R ₃ is hydrogen, substituted or unsubstituted methyl or substituted or unsubstituted ethyl; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{3′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, R _3′ is hydrogen; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₄ and R _{4′ are} independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ ,- NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _{41 '} R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₄₁ , -C( O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C(CH ₃ ) ₂ OR ₄₁ ; preferably, R ₄ and R _{4 'Both} of these two lines -R _41, more preferably, R ₄ and R _4' hydrogen Both of these two lines; optionally form stereoisomers, preferably enantiomers or enantiomer of one of those , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; preferably , R ₅ is substituted or unsubstituted C _1-6 alkyl; more preferably, R ₅ is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; depending on the situation One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{5′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, R _{5′ is} selected from hydrogen and substituted or unsubstituted methyl; depending on the situation One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; Preferably substituted or unsubstituted cyclopropyl; optionally in the form of a stereoisomer, preferably an enantiomer or diastereomer, a racemate, or as a stereoisomer At least two of the preferred mirror isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkyl cycloalkyl, substituted or Unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; Preferably, R _{6 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Substituted heterocyclyl, substituted or unsubstituted cycloalkyl, and -C(O)R ₇ ; more preferably, R _{6 is} selected from substituted or unsubstituted methyl, substituted or unsubstituted Ethyl, substituted or unsubstituted isopropyl, substituted or unsubstituted cyclopropyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridine, substituted or unsubstituted Benzyl and substituted or unsubstituted benzyl; optionally in the form of stereoisomers, preferably enantiomers or diastereomers, racemates, or At least two of the stereoisomers, preferably mirror image isomers and/or diastereomers are in the form of a mixture in any mixing ratio, or their corresponding salts, or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted Substituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic; preferably, R ₇ is substituted Or an unsubstituted aryl group; more preferably, R ₇ is a substituted or unsubstituted phenyl group; one of stereoisomers, preferably mirror isomers or diastereomers, as the case may be, In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or its corresponding salt, or its corresponding Solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or Unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl and -OR ₈₁ ; preferably, R ₈ is hydrogen; depending on the situation, stereoisomers, preferably mirror images One of the structure or diastereomer, racemate, or at least two of stereoisomers, preferably mirror isomers, and/or diastereomers in any mixing ratio In the form of a mixture, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _{8′ is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, R _8′ is hydrogen; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₉ and R _{9′ are} independently selected from halogen, —R ₂₁ , —OR ₂₁ , —NO ₂ , − NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _{21 '} R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C( O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; preferably, R ₉ and R _{9 'Both} of these two lines -R _21; more preferably, R _9, and R & lt _9' Both of these two lines of hydrogen; optionally form stereoisomers, preferably enantiomers or enantiomer of one of those , In the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₁₀ and R _{10′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, both R ₁₀ and R _10′ are hydrogen; One of the structure, the preferred enantiomer or diastereomer, the racemate, or in the form of a stereoisomer, preferred enantiomer and/or diastereomer At least the two are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₁₀ and R _10′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; The situation is in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and/or non-mirrors At least two of the structures are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R _10″ and R _{10″′ are} independently selected from hydrogen, substituted or unsubstituted C _{1 -6} alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; preferably, both R _10″ and R _10′″ It is hydrogen; optionally in the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or Or at least two of the diastereomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R _10" and R _10"' together with the carbon atom to which they are attached form a substituted or unsubstituted ring Alkyl; optionally in the form of one of stereoisomers, preferred mirror isomers or diastereoisomers, racemates, or stereoisomers, preferred mirror isomers and/or Or at least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₁₃ and R _{13′ are} independently selected from hydrogen, unsubstituted C _1-6 alkyl, Substituted C _2-6 alkenyl and unsubstituted C _2-6 alkynyl; optionally one of stereoisomers, preferably mirror isomers or diastereomers, racemates In the form of, or in the form of a mixture of at least two of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₁₄ , R _14′ and R _{14″ are} independently selected from hydrogen, unsubstituted C _1-6 Alkyl, unsubstituted C _2-6 alkenyl, unsubstituted C _2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl, and unsubstituted heterocyclyl; as appropriate In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₂₁ , R _21′ and R _{21″ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₃₁ , R _31' and R _{31'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, the racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₃₂ and R _{32′ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereo stereoisomers, preferably mirror isomers or non-mirror isomers, as the case may be One of them, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof , Or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; preferably, R ₄₁ is hydrogen; optionally in the form of stereoisomers, preferred mirror isomers or diastereomers, racemates, or stereoisomers, preferred mirror isomers and At least two of the diastereoisomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound in which R ₅₁ , R _51′ and R _{51″ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixture ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₅₂ , R _52′ and R _{52″ are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₆₁ , R _61' and R _{61'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₇₁ , R _71' and R _{71'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; optionally stereoisomers, preferably mirror isomers or non- One of the enantiomers, a racemate, or a mixture of stereoisomers, preferably enantiomers, and/or diastereoisomers in any mixing ratio , Or its corresponding salt, or its corresponding solvate.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein R ₈₁ and R _{81' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl , Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; stereo stereoisomers, preferably mirror isomers or non-mirror isomers as appropriate One of them, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof , Or their corresponding solvates.

In another preferred embodiment of the present invention according to general formula (I), the compound is a compound wherein p is 0, 1 or 2; and/or q is 0; and/or n is 0; and/or m is 1; and/or r is 1; and/or X is selected from bonds, -CH ₂ -, -CH ₂ CH ₂ -, -CH ₂ CH(methyl)- and -C(O)-; and/ Y-based or -CH ₂ - or C = O; and / or lines Y ₁ -CH ₂ -; and / or lines Y ₂ -CH ₂ -; and / or R _a type hydrogen or substituted or unsubstituted armor Group; and/or R _b is hydrogen; and/or R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclic group, more preferably, R ₂ is selected from benzene Substituted and unsubstituted groups of thiol and thiophene; and/or R ₃ is a substituted or unsubstituted C _1-6 alkyl group; more preferably, R ₃ is hydrogen, substituted or unsubstituted methyl or substituted or non-substituted ethyl; and / or R _{3 'based} hydrogen; and / or R ₄ based hydrogen; and / or R ₄ and R _4' and Both lines -R _41, more preferably , R ₄ and R _4′ are both hydrogen; and/or R ₅ is a substituted or unsubstituted C _1-6 alkyl; more preferably, R ₅ is a substituted or unsubstituted methyl or Substituted or unsubstituted ethyl; and/or R _{5′ is} selected from hydrogen or substituted or unsubstituted methyl; and/or R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted Substituted cyclopropyl; and/or R _{6 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, Substituted or unsubstituted alkylaryl, substituted or unsubstituted heterocyclic group and -C(O)R ₇ ; more preferably, R _{6 is} selected from substituted or unsubstituted methyl, substituted Or unsubstituted ethyl, substituted or unsubstituted isopropyl, substituted or unsubstituted cyclopropyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridine, Substituted or unsubstituted benzyl and substituted or unsubstituted benzyl; and/or R ₇ is substituted or unsubstituted aryl; more preferably, R ₇ is substituted or unsubstituted Substituted phenyl; and/or R ₈ is hydrogen; and/or R _8′ is hydrogen; and/or R ₉ and R _9′ are both -R ₂₁ ; more preferably, R ₉ and R _{9′ are} Both are hydrogen; and/or R ₁₀ and R _10' are both hydrogen; and/or R _10'' and R _10''' are both hydrogen; and/or R ₄₁ are hydrogen; as appropriate One of the stereoisomers, preferred mirror isomers or diastereomers, racemates, or in the form of stereoisomers, preferred mirror isomers and/or diastereomers At least two of them are in the form of a mixture of any mixing ratio, or its corresponding salt, or its corresponding solvate.

In the preferred embodiment p is 0, 1, or 2.

In the preferred embodiment q is 0.

In the preferred embodiment n系0.

In the preferred embodiment m系1.

In the preferred embodiment r系1.

In the preferred embodiment Both m and r are 1.

In a preferred embodiment X is selected from the group consisting of bond, -CH ₂ -, -CH ₂ CH ₂ -, -CH ₂ CH(methyl)- and -C(O)-.

Based embodiment R _a hydrogen or a substituted or unsubstituted methyl group in the preferred embodiment.

In the preferred embodiment R _b is hydrogen.

Example R _a and R _b are hydrogen Both of these two lines in the preferred embodiment.

選自

及

。In the preferred embodiment

Select from

and

.

選自

及-C(O)-R₁ 。In the preferred embodiment

Select from

And -C(O)-R ₁ .

In a preferred embodiment, Y is -CH ₂ -or C=O.

In the preferred embodiment Y ₁ is -CH ₂ -.

In a preferred embodiment Y ₂ is -CH ₂ -.

In the preferred embodiment both Y ₁ and Y ₂ are -CH ₂ -.

In a preferred embodiment R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclic group, more preferably, R ₂ is selected from substituted or unsubstituted phenyl and thiophene Unsubstituted group.

In a preferred embodiment R ₃ is hydrogen or substituted or unsubstituted C _1-6 alkyl; more preferably, R ₃ is hydrogen, substituted or unsubstituted methyl or substituted or unsubstituted Of ethyl.

Example R _{3 'in} the preferred embodiment based hydrogen; In the preferred embodiment R ₃ lines of a substituted or unsubstituted C _1-6 alkyl; more preferably, R ₃ a substituted or unsubstituted based Armor group, and R _{3 'hydrogen} system.

In a preferred embodiment R ₃ is hydrogen or substituted or unsubstituted C _1-6 alkyl; more preferably, R ₃ is hydrogen, substituted or unsubstituted methyl or substituted or unsubstituted of ethyl and R _{3 'hydrogen} system.

In the preferred embodiment R ₄ is hydrogen.

In the preferred embodiment in Example ₄ R _{'hydrogen-based}

In the preferred embodiment, both R ₄ and R _{4 ′} are hydrogen.

In a preferred embodiment, R ₅ is substituted or unsubstituted C _1-6 alkyl; more preferably, R ₅ is substituted or unsubstituted methyl or substituted or unsubstituted ethyl.

In a preferred embodiment R _5'is selected from hydrogen or substituted or unsubstituted C _1-6 alkyl; preferably hydrogen or substituted or unsubstituted methyl.

In a preferred embodiment, R ₅ is a substituted or unsubstituted C _1-6 alkyl group; more preferably, R ₅ is a substituted or unsubstituted methyl group, and R _{5′ is} selected from hydrogen.

In a preferred embodiment, R ₅ is substituted or unsubstituted C _1-6 alkyl; more preferably, R ₅ is substituted or unsubstituted methyl or substituted or unsubstituted ethyl, R _{5′ is} selected from hydrogen or substituted or unsubstituted C _1-6 alkyl; preferably hydrogen or substituted or unsubstituted methyl.

In a preferred embodiment R ₅ is substituted or unsubstituted C _1-6 alkyl; more preferably, R ₅ is substituted or unsubstituted methyl or substituted or unsubstituted ethyl, and R _{5 'type} hydrogen.

In a preferred embodiment, both R ₅ and R _5′ are substituted or unsubstituted C _1-6 alkyl; more preferably, both R ₅ and R _5′ are substituted or unsubstituted Of methyl.

In a preferred embodiment R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cyclopropyl group.

In a preferred embodiment R _{6 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted alkylaryl and -C(O)R ₇ ; more preferably, R ₆ Selected from substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted isopropyl, substituted or unsubstituted benzyl, and substituted or unsubstituted The benzoyl group.

In a preferred embodiment R _{6 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted Substituted heterocyclyl, substituted or unsubstituted alkylaryl and -C(O)R ₇ ; more preferably, R _{6 is} selected from substituted or unsubstituted methyl, substituted or unsubstituted Ethyl, substituted or unsubstituted isopropyl, substituted or unsubstituted cyclopropyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridine, substituted or unsubstituted Substituted benzyl and substituted or unsubstituted benzyl.

In a preferred embodiment, R ₇ is a substituted or unsubstituted aryl group; more preferably, R ₇ is a substituted or unsubstituted phenyl group.

In the preferred embodiment R ₈ is hydrogen.

In the preferred embodiment embodiment R _{8 'based} hydrogen

Example R ₈ and R _{8 'Both} of these lines in the preferred embodiment hydrogen.

Example R ₉ and R ₉ in the preferred embodiment _'Both of these two lines -R _21; more preferably, R ₉ and R _{9' are} hydrogen Both of these two lines.

In the preferred embodiment, both R ₁₀ and R _10' are hydrogen.

In a preferred embodiment, both R _10" and R _10"' are hydrogen.

In a preferred embodiment, R ₁₀ , R _10′ , R _10″ and R _{10″′ are} all hydrogen.

In the preferred embodiment R ₄₁ is hydrogen.

In an embodiment of the compound according to the invention of general formula (I), Halogen is fluorine, chlorine, iodine or bromine; preferably fluorine, In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In an embodiment of the compound according to the invention of general formula (I), Haloalkyl-CF3; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In another embodiment of the compounds according to the invention of general formula (I), Haloalkoxy-OCF3; In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In a further preferred embodiment, the compound of formula (I) is selected from

In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In a further preferred embodiment, the compound of formula (I) is selected from

In the form of one of stereoisomers, preferred mirror isomers or diastereomers, racemates, or as stereoisomers, preferred mirror isomers and/or non-mirrors, as appropriate At least two of the isomers are in the form of a mixture in any mixing ratio, or its corresponding salt, or its corresponding solvate.

In an excellent embodiment, the compound selected as the α2δ subunit of the voltage-gated calcium channel, specifically the α2δ-1 subunit and the dual ligand of the µ-opioid receptor, and in particular the compound has a measure corresponding to the following the binding is expressed as the K _i: K _i (μ) preferably <1000 nM, more preferably <500 nM, and even more preferably <100 nM.

Ki(α2δ1) is preferably <10000 nM, more preferably <5000 nM, even more preferably <500 nM.

In the following, the phrase "the compound of the present invention" is used. This should be understood as according to the general formula (I), (I'), (I ^a ), (I ^a '), (I ^b ), (I ^b '), (I ^c ), (I ^c ') and (IZ) any compound according to the invention.

The compound of the present invention represented by the above formula (I) may include a mirror image isomer depending on the presence of a chiral center or may include isomers depending on the presence of multiple bonds (eg, Z, E). Single isomers, enantiomers or diastereomers and mixtures thereof are within the scope of the present invention.

For clarity, the expression "a compound according to formula (I), where, for example, R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ , Y ₂ and n are as follows "Defined in the description" will (only the expression "compound of formula (I) as defined in any one of technical solutions 1 to 8" as found in the scope of patent application) means "compound according to formula (I)", The definitions of the various substituents R ₁ etc. (also from the patent application) are used. In addition, this also means that although (especially with regard to the scope of patent application) one or more of the waiver statements defined in the specification (or used in any of the scope of patent applications as described in, for example, Technical Solution 1) will apply To define individual compounds. Therefore, for example, the waiver statement found in technical solution 1 will also be used to define the compound of "formula (I) as defined in the corresponding related technical solution such as any one of 1 to 8".

In general, the method is described in the experimental section below. The starting materials are commercially available or can be prepared by conventional methods.

A preferred embodiment of the present invention is a method of producing a compound according to formula (I), wherein R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ if not otherwise defined , Y ₂ and n have the meanings defined in the specification. LG means a leaving group (for example, chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate).

其中Q表示氯、溴、碘或三氟甲磺酸根；用式(III-1)之適宜含N 環狀試劑

在布赫瓦爾德-哈特維希(Buchwald-Hartwig)或烏耳曼(Ullmann)芳基化條件下處理。In certain embodiments, there is a method of producing a compound according to formula (I), wherein X represents a bond, and wherein R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , Y ₁ , Y ₂ And n have the meanings defined in the specification, the method includes the compound of formula (IIa),

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate; use a suitable N- containing cyclic reagent of formula (III-1)

Treatment under Buchwald-Hartwig or Ullmann arylation conditions.

其中r表示0至4；用式(III-1)之含N 環狀試劑

在標準還原胺化條件下處理。In a particular embodiment, there is a method of producing a compound according to formula (I), wherein -X- represents -[C(R _a R _b )] _p -, and wherein R _a , R _b , R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n and p have the meanings defined in the specification, the method includes the compound of formula (IIb')

Where r represents 0 to 4; use the N -containing ring reagent of formula (III-1)

Handle under standard reductive amination conditions.

其中Q表示氯、溴、碘或三氟甲磺酸根；用式(III-2’)之有機金屬試劑處理，

其中M表示適宜有機金屬基團、較佳硼或鋅試劑，且p具有如說明書中所定義之含義。In a particular embodiment, there is a method of producing a compound according to formula (I), wherein -X- represents -[C(R _a R _b )] _p -, and wherein R _a , R _b , R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n and p have the meanings defined in the specification, the method includes the compound of formula (IIa)

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate; treated with an organometallic reagent of formula (III-2'),

Where M represents a suitable organometallic group, preferably boron or zinc reagent, and p has the meaning as defined in the specification.

用式(III-1)之含N 環狀試劑

在習用醯胺化條件下處理。In a particular embodiment, there is a method of producing a compound according to formula (I), wherein -X- represents -[CR _a R _b ] _p C(O)[CH ₂ ] _q -and q is 0, and wherein R _a And R _b is hydrogen and wherein R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and q have the meanings defined in the specification, the method includes Compound of formula (IIc')

Use the N -containing ring reagent of formula (III-1)

Handle under conventional amidation conditions.

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，p、q及Rz具有說明書中所定義之含義；用式(III-1)之含N 環狀試劑

在習用烷基化條件下處理。In a particular embodiment, there is a method of producing a compound according to formula (I), wherein -X- represents -[CR _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -, and wherein R _a and R _b are hydrogen and R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and q have the meanings defined in the specification, the method includes The compound of formula (VI')

Where LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, p, q and Rz have the meanings defined in the specification; use formula ( III-1) N -containing ring reagent

Handle under conventional alkylation conditions.

其中p及Rz具有說明書中所定義之含義；用式(III-3)之醯基試劑，

在醯胺化條件下處理，其中Z表示OH或鹵素且q具有如說明書中所定義之含義。In a particular embodiment, there is a method of producing a compound according to formula (I), wherein -X- represents -[R _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -, and wherein R _a and R _b are hydrogen and R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and q have the meanings defined in the specification, the method includes The amine compound of formula (IId')

Where p and Rz have the meanings defined in the specification; using the amide reagent of formula (III-3),

Treatment under amidation conditions, where Z represents OH or halogen and q has the meaning as defined in the specification.

其中Q表示氯、溴、碘或三氟甲磺酸根；與式(III-5)之甲醯胺基化合物

在烏耳曼芳基化條件反應，其中q及Rz具有說明書中所定義之含義。In a particular embodiment, there is a method of producing a compound according to formula (I), wherein -X- represents -[CR _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -, p is 0 , And wherein R _a and R _b are hydrogen and wherein R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and q have the meanings defined in the specification , The method comprises using a compound of formula (IIa)

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate; and the compound of formula (III-5)

The reaction is carried out under Ulman arylation conditions, where q and Rz have the meanings defined in the specification.

與式(VIII)之烷基化劑反應

其中Z表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根。In particular embodiments, there are methods of producing compounds according to formula (I), wherein n is 0, and wherein R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ and Y ₂ has the meaning defined in the specification, the method comprises using a compound of formula (VIIa), wherein G is OH,

Reaction with alkylating agent of formula (VIII)

Where Z represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate.

與式(VIII)之醇，其中Z表示OH，

在適宜偶氮化合物存在下反應。In particular embodiments, there are methods of producing compounds according to formula (I), wherein n is 0, and wherein R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ and Y ₂ has the meaning defined in the specification, the method comprises using a compound of formula (VIIa), wherein G is OH,

With alcohol of formula (VIII), where Z represents OH,

Reaction in the presence of a suitable azo compound.

與式(VIII)之醇，其中Z表示OH，

在強鹼存在下反應。In particular embodiments, there are methods of producing compounds according to formula (I), wherein n is 0, and wherein R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ and Y ₂ has the meaning defined in the specification, the method comprises using a compound of formula (VIIa), wherein G is halogen,

With alcohol of formula (VIII), where Z represents OH,

React in the presence of strong base.

與式(VIII)之試劑反應，

其中Z表示OH且G表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，或另一選擇為，Z表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，且G表示OH。In certain embodiments, there are methods of producing compounds according to formula (I), wherein n is 1, and wherein R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ and Y ₂ has the meaning defined in the specification, the method comprises using a compound of formula (VIIb)

React with the reagent of formula (VIII),

Where Z represents OH and G represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, or alternatively, Z represents a leaving group, for example Chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, and G represents OH.

a) 其中X表示鍵，且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n具有說明書中所定義之含義，該方法包含將式(IIa)之化合物，

其中Q表示氯、溴、碘或三氟甲磺酸根；用適宜式(III-1)之含N 環狀試劑

在布赫瓦爾德-哈特維希或烏耳曼芳基化條件下處理； 或 b) 其中-X-表示-[C(R_a R_b )]_p -，且其中R_a 、R_b 、R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n及p具有說明書中所定義之含義，該方法包含將式(IIb’)之化合物

其中r表示0至4；用式(III-1)之含N 環狀試劑

在標準還原胺化條件下處理； 或 c) 其中-X-表示-[C(R_a R_b )]_p -，且其中R_a 、R_b 、R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n及p具有說明書中所定義之含義，該方法包含將式(IIa)之化合物

其中Q表示氯、溴、碘或三氟甲磺酸根；用式(III-2’)之有機金屬試劑處理，

其中M表示適宜有機金屬基團、較佳硼或鋅試劑，且p具有如說明書中所定義之含義； 或 d) 其中-X-表示-[CR_a R_b ]_p C(O)[CH₂ ]_q -且q係0，且其中R_a 及R_b 係氫且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及q具有說明書中所定義之含義，該方法包含將式(IIc’)之化合物

用式(III-1)之含N 環狀試劑

在習用醯胺化條件下處理； 或 e) 其中-X-表示-[CR_a R_b ]_p N(R_z )C(O)[CH₂ ]_q -，且其中R_a 及R_b 係氫且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及q具有說明書中所定義之含義，該方法包含將式(VI’)之化合物

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，p、q及Rz具有說明書中所定義之含義；用式(III-1)之含N 環狀試劑，

在習用烷基化條件下處理； 或 f) 其中-X-表示-[CR_a R_b ]_p N(R_z )C(O)[CH₂ ]_q -，且其中R_a 及R_b 係氫且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及q具有說明書中所定義之含義，該方法包含將式(IId’)之胺基化合物

其中p及Rz具有說明書中所定義之含義；用式(III-3)之醯基試劑，

在醯胺化條件下處理，其中Z表示OH或鹵素且q具有如說明書中所定義之含義； 或 g) 其中-X-表示-[CR_a R_b ]_p N(R_z )C(O)[CH₂ ]_q -，p係0，且其中R_a 及R_b 係氫且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及q具有說明書中所定義之含義，該方法包含使式(IIa)之化合物

其中Q表示氯、溴、碘或三氟甲磺酸根；與式(III-5)之甲醯胺基化合物

在烏耳曼芳基化條件下反應，其中q及Rz具有說明書中所定義之含義； 或 h) 其中n係0，且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 及Y₂ 具有說明書中所定義之含義，該方法包含使式(VIIa)之化合物，其中G係OH，

與式(VIII)之烷基化劑反應，

其中Z表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根； 或 i) 其中n係0，且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 及Y₂ 具有說明書中所定義之含義，該方法包含使式(VIIa)之化合物，其中G係OH，

與式(VIII)之醇，其中Z表示OH，

在適宜偶氮化合物存在下反應； 或 j) 其中n係0，且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 及Y₂ 具有說明書中所定義之含義，該方法包含使式(VIIa)之化合物，其中G係鹵素，

與式(VIII)之醇，其中Z表示OH，

在強鹼存在下反應； 或 k) 其中n係1，且其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 及Y₂ 具有說明書中所定義之含義，該方法包含使式(VIIb)之化合物，

與式(VIII)之試劑反應，

其中Z表示OH且G表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，或另一選擇為，Z表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，且G表示OH。In certain embodiments, there are methods of producing compounds according to formula (I),

a) where X represents a bond, and where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n have the meanings defined in the specification, the method includes the formula ( Compound IIa),

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate; use a suitable N -containing cyclic reagent of formula (III-1)

Treatment under Buchwald-Hartwig or Ulman arylation conditions; or b) where -X- represents -[C(R _a R _b )] _p -, and where R _a , R _b , R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n and p have the meanings defined in the specification, the method includes the compound of formula (IIb')

Where r represents 0 to 4; use the N -containing ring reagent of formula (III-1)

Treatment under standard reductive amination conditions; or c) where -X- represents -[C(R _a R _b )] _p -, and where R _a , R _b , R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n and p have the meanings defined in the specification, the method includes the compound of formula (IIa)

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate; treated with an organometallic reagent of formula (III-2'),

Where M represents a suitable organometallic group, preferably boron or zinc reagent, and p has the meaning as defined in the specification; or d) where -X- represents -[CR _a R _b ] _p C(O)[CH ₂ ] _q -and q is 0, and R _a and R _b are hydrogen and R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and q Has the meaning defined in the specification, the method includes the compound of formula (IIc')

Use the N -containing ring reagent of formula (III-1)

Treatment under conventional amidation conditions; or e) where -X- represents -[CR _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -, and where R _a and R _b are hydrogen And where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and q have the meanings defined in the specification, the method includes formula (VI') Compound

Where LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, p, q and Rz have the meanings defined in the specification; use formula ( III-1) N -containing ring reagent,

Treatment under conventional alkylation conditions; or f) where -X- represents -[CR _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -, and where R _a and R _b are hydrogen And where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p, and q have the meanings defined in the specification, the method includes formula (IId') Amine compound

Where p and Rz have the meanings defined in the specification; using the amide reagent of formula (III-3),

Treatment under amidation conditions, where Z represents OH or halogen and q has the meaning as defined in the specification; or g) where -X- represents -[CR _a R _b ] _p N(R _z )C(O) [CH ₂ ] _q -, p is 0, and R _a and R _b are hydrogen and R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , Y ₁ , Y ₂ , n, p and q have the meanings defined in the specification, and the method includes making the compound of formula (IIa)

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate; and the compound of formula (III-5)

Reaction under Ullmann arylation conditions, where q and Rz have the meanings defined in the specification; or h) where n is 0, and where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ and Y ₂ have the meanings defined in the specification, the method includes using a compound of formula (VIIa), wherein G is OH,

React with alkylating agent of formula (VIII),

Where Z represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate; or i) where n is 0, and where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ and Y ₂ have the meanings defined in the specification. The method includes using a compound of formula (VIIa), wherein G is OH,

With alcohol of formula (VIII), where Z represents OH,

React in the presence of a suitable azo compound; or j) wherein n is 0, and wherein R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ and Y ₂ have the The meaning of the definition, the method includes the use of compounds of formula (VIIa) wherein G is halogen,

With alcohol of formula (VIII), where Z represents OH,

React in the presence of a strong base; or k) where n is 1, and wherein R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ and Y ₂ have the definitions in the specification Meaning, the method comprises using a compound of formula (VIIb),

React with the reagent of formula (VIII),

Where Z represents OH and G represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, or alternatively, Z represents a leaving group, for example Chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, and G represents OH.

In a particular embodiment, there is a method of producing a compound according to formula (I) by generating a reduction reaction of a carbonyl derivative and a suitable reducing agent (preferably sodium borohydride) in an organic solvent (preferably MeOH) to The hydroxy compound is obtained.

In particular embodiments, there are methods for producing compounds according to formula (I) by: by any suitable method, for example in a suitable solvent (such as 1,4-dioxane, DCM, ethyl acetate or an organic solvent and The mixture of water) is treated with an acid (preferably HCl or trifluoroacetic acid), and the compound of formula I containing an amine protecting group (such as a carbamate, preferably a third butoxycarbonyl group) undergoes a deprotection reaction.

In a particular embodiment, there is a method of producing a compound according to formula (I) by: carrying out an amine group-containing compound of formula I in an organic solvent (preferably DCE) in the presence of an organic base (preferably DIPEA or TEA) The reductive amination reaction with aldehyde is preferably carried out using a reducing agent (preferably sodium triethoxyborohydride). Alternatively, the reaction can be carried out in the presence of acid (preferably acetic acid).

In a particular embodiment, there is a method of producing a compound according to formula (I) by: at a suitable temperature (eg, in the range of 0-120°C), in the presence of a base (preferably DIPEA or K ₂ CO ₃ ) 1. The compound of formula I containing an amine group in an organic solvent (preferably acetonitrile) is reacted with an alkylating agent.

In a particular embodiment, there is a method of producing a compound according to formula (I) as follows: a compound of formula I containing an amine group and a vinyl derivative in an organic solvent at a suitable temperature (eg, in the range of 20-140° C.) Preferably, the reaction is carried out in 2-methoxyethanol).

其中Z表示OH或鹵素，R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (II),

Where Z represents OH or halogen, R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n have the meanings defined in the specification, which are used to prepare the compound of formula (I).

其中Q表示氯、溴、碘或三氟甲磺酸根，R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIa),

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate, R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n have the meanings defined in the specification and are used for Preparation of compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，Q表示氯、溴、碘或三氟甲磺酸根，R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIa-LG),

Where LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, Q represents chlorine, bromine, iodine or triflate, R ₂ , R ₄ , R _4′ , Y ₁ , Y ₂ and n have the meanings defined in the specification, which are used to prepare the compound of formula (I).

其中R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及r具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIb),

Wherein R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , Y ₁ , Y ₂ , n and r have the meanings defined in the specification, which are used to prepare the compound of formula (I).

其中R_a 、R_b 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及r具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIb'),

Wherein _{R a, R b, R 2} , R 3, R 3 ', R 4, R 4', Y 1, Y 2, n and r have the meanings as defined in the specification, for the preparation of compounds of formula (I) .

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及r具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIb-LG),

Where LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, R ₂ , R ₄ , R _4' , Y ₁ , Y ₂ , n and r have the meanings defined in the specification and are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_a 、R_b 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及r具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIb'-LG),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R a, R b, R} 2, R 4, R 4 ', Y ₁ , Y ₂ , n, and r have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及p具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIc),

Wherein R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , Y ₁ , Y ₂ , n and p have the meanings defined in the specification, which are used to prepare the compound of formula (I).

其中R_a 、R_b 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及p具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIc'),

Wherein _{R a, R b, R 2} , R 3, R 3 ', R 4, R 4', Y 1, Y 2, n and p have the meanings defined in the specification, for the preparation of compounds of formula (I) .

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及p具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIc-LG),

Where LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, R ₂ , R ₄ , R _4' , Y ₁ , Y ₂ , n and p have the meanings defined in the specification and are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_a 、R_b 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及p具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IIc'-LG),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R a, R b, R} 2, R 4, R 4 ', Y ₁ , Y ₂ , n and p have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及R_z 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IId),

Wherein R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and R _z have the meanings defined in the specification, which are used to prepare the compound of formula (I).

其中R_a 、R_b 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及R_z 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IId'),

Wherein _{R a, R b, R 2} , R 3, R 3 ', R 4, R 4', Y 1, Y 2, n, p , and R _z have the meanings defined in the specification, for the preparation of formula ( I) Compound.

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_a 、R_b 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及R_z 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IId'-LG),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R a, R b, R} 2, R 4, R 4 ', Y ₁ , Y ₂ , n, p, and R _z have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_a 、R_b 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p及R_z 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IId'-LG),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R a, R b, R} 2, R 4, R 4 ', Y ₁ , Y ₂ , n, p, and R _z have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中R₁ 具有如說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (III-1),

Where R ₁ has the meaning as defined in the specification, which is used to prepare the compound of formula (I).

其中p及R₁ 具有說明書中所定義之含義，且M表示適宜有機金屬基團、較佳硼或鋅試劑，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (III-2),

Where p and R ₁ have the meanings defined in the specification, and M represents a suitable organometallic group, preferably boron or zinc reagent, which is used to prepare the compound of formula (I).

其中p及R_a 、R_b 、R₁ 具有說明書中所定義之含義，且M表示適宜有機金屬基團、較佳硼或鋅試劑，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (III'-2),

Wherein p and R _a, R _b, R ₁ has the meaning defined in the specification, and M represents a suitable organometallic groups, preferably boron or zinc reagent, for the preparation of compounds of formula (I).

其中q及R₁ 具有說明書中所定義之含義，且Z表示OH或鹵素，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (III-3),

Where q and R ₁ have the meanings defined in the specification, and Z represents OH or halogen, which is used to prepare the compound of formula (I).

其中q具有如說明書中所定義之含義，Z表示OH或鹵素，且LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (III-4),

Where q has the meaning as defined in the specification, Z represents OH or halogen, and LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate , Which is used to prepare compounds of formula (I).

其中q、R_z 及R₁ 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (III-5),

Where q, R _z and R ₁ have the meanings defined in the specification, which are used to prepare the compound of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVa),

Where LG represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, R ₁ , R ₂ , R ₄ , R _4' , Y ₁ , Y ₂ and n have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、p及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVb),

Where LG represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, R ₁ , R ₂ , R ₄ , R _4' , Y ₁ , Y ₂ , p and n have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_a 、R_b 、R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、p及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVb'),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R a, R b, R} 1, R 2, R 4, R _4' , Y ₁ , Y ₂ , p, and n have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、p及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVc),

Where LG represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, R ₁ , R ₂ , R ₄ , R _4' , Y ₁ , Y ₂ , p and n have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_a 、R_b 、R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、p及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVc'),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R a, R b, R} 1, R 2, R 4, R _4' , Y ₁ , Y ₂ , p, and n have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_z 、R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、p及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVd),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R z, R 1, R} 2, R 4, R 4 ', Y ₁ , Y ₂ , p and n have the meanings defined in the specification, which are used to prepare compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R_a 、R_b 、R_z 、R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、p及n具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVd'),

Wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, a sulfonate or triflate _{nitrophenyl, R a, R b, R} z, R 1, R 2, R _{4, R 4 ', Y 1} , Y 2, p and n have the meanings defined in the specification, for the preparation of compounds of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 及Y₂ 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVe),

Where LG represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, R ₁ , R ₂ , R ₄ , R _4' , Y ₁ and Y ₂ has the meaning defined in the specification, which is used to prepare the compound of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₁ 、R₂ 、R₄ 、R_4’ 、Y₁ 及Y₂ 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IVf),

Where LG represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, R ₁ , R ₂ , R ₄ , R _4' , Y ₁ and Y ₂ has the meaning defined in the specification, which is used to prepare the compound of formula (I).

其中R₃ 及R_3’ 具有說明書中所定義之含義，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (V),

Wherein R ₃ and R _{3 'has} the meaning defined in the specification, for the preparation of compounds of formula (I).

其中R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p、q及R_z 具有說明書中所定義之含義，且LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (VI),

Where R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p, q, and R _z have the meanings defined in the specification, and LG represents a leaving group, such as chlorine, bromine , Iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, which are used to prepare compounds of formula (I).

其中R_a 、R_b 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p、q及R_z 具有說明書中所定義之含義，且LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (VI'),

Wherein _{R a, R b, R 2} , R 3, R 3 ', R 4, R 4', Y 1, Y 2, n, p, q , and R _z have the meanings defined in the specification, the above and LG represents a leaving Radicals, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, which are used to prepare compounds of formula (I).

其中n、R₁ 、R₄ 、R_4’ 及X具有說明書中所定義之含義，且G係OH或鹵素，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (VII),

Where n, R ₁ , R ₄ , R _4′ and X have the meanings defined in the specification, and G is OH or halogen, which is used to prepare the compound of formula (I).

其中R₁ 、R₄ 、R_4’ 及X具有說明書中所定義之含義，且G係OH或鹵素，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (VIIa),

Where R ₁ , R ₄ , R _4′ and X have the meanings defined in the specification, and G is OH or halogen, which is used to prepare the compound of formula (I).

其中R₁ 、R₄ 、R_4’ 及X具有說明書中所定義之含義，且G係OH或脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (VIIb),

Where R ₁ , R ₄ , R _4'and X have the meanings defined in the specification, and G is OH or a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or Trifluoromethanesulfonate, which is used to prepare compounds of formula (I).

其中R₂ 、R₃ 、R_3’ 、Y₁ 及Y₂ 具有說明書中所定義之含義，且Z表示OH或鹵素，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (VIII),

Where R ₂ , R ₃ , R _3′ , Y ₁ and Y ₂ have the meanings defined in the specification, and Z represents OH or halogen, which is used to prepare the compound of formula (I).

其中LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，R₂ 、Y₁ 及Y₂ 具有說明書中所定義之含義，且Z表示OH或鹵素，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (VIII-LG),

Where LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, R ₂ , Y ₁ and Y ₂ have the meanings defined in the specification, And Z represents OH or halogen, which is used to prepare the compound of formula (I).

其中n、R₄ 、R_4’ 具有說明書中所定義之含義，且Z表示OH或鹵素且G係OH或鹵素，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (IX),

Where n, R ₄ and R _4′ have the meanings defined in the specification, and Z represents OH or halogen and G is OH or halogen, which is used to prepare the compound of formula (I).

其中R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (X),

Where R ₃ , R _3′ , R ₄ , R _4′ , n, Y ₁ and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, which is used to prepare the compound of formula (I).

其中R_a 、R_b 、R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (X'),

Wherein _{R a, R b, R 3} , R 3 ', R 4, R 4', n, Y 1 and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, for the preparation of formula (I ) Compounds.

其中R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (X-LG),

Where R ₃ , R _3′ , R ₄ , R _4′ , n, Y ₁ and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, which is used to prepare the compound of formula (I).

其中R_a 、R_b 、R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (X'-LG),

Wherein _{R a, R b, R 3} , R 3 ', R 4, R 4', n, Y 1 and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, for the preparation of formula (I ) Compounds.

其中R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (XI),

Where R ₃ , R _3′ , R ₄ , R _4′ , n, Y ₁ and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, which is used to prepare the compound of formula (I).

其中R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (XI-LG),

Where R ₃ , R _3′ , R ₄ , R _4′ , n, Y ₁ and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, which is used to prepare the compound of formula (I).

其中R_a 、R_b 、R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (XI'-LG),

Wherein _{R a, R b, R 3} , R 3 ', R 4, R 4', n, Y 1 and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, for the preparation of formula (I ) Compounds.

其中R_a 、R_b 、R₃ 、R_3’ 、R₄ 、R_4’ 、n、Y₁ 及Y₂ 具有說明書中所定義之含義，且r表示0至4，其用於製備式(I)化合物。The specific embodiment of the present invention refers to the use of the compound of formula (XI'-LG),

Wherein _{R a, R b, R 3} , R 3 ', R 4, R 4', n, Y 1 and Y ₂ have the meanings defined in the specification, and r represents 0 to 4, for the preparation of formula (I ) Compounds.

其中R_a 、R_b 、R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n、p、q、r及R_z 具有說明書中所定義之含義，Q表示氯、溴、碘或三氟甲磺酸根，LG表示脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，具有說明書中所定義之含義，M表示適宜有機金屬基團，Z表示OH或鹵素，且G係OH、鹵素或脫離基，例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根，該化合物用於製備式(I)化合物。A specific embodiment of the present invention refers to formulas II, IIa, IIa-LG, IIb, IIb', IIb-LG, IIb'-LG, IIc, IIc', IIc-LG, IIc'-LG, IId, IId', IId-LG, IId'-LG, III-1, III-2, III'-2, III-3, III-4, III-5, IVa, IVb, IVb', IVc, IVc', IVd, IVd' , IVe, IVf, V, VI, VI', VII, VIIa, VIIb, VIII, VIII-LG, IX, X, X', X-LG, X'-LG, XI, XI-LG, XI' or XI Uses of'-LG compounds

Wherein _{R a, R b, R 1} , R 2, R 3, R 3 ', R 4, R 4', Y 1, Y 2, n, p, q, r , and R _z have the meanings defined in the description of , Q represents chlorine, bromine, iodine or trifluoromethanesulfonate, LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, with instructions As defined in M, M represents a suitable organometallic group, Z represents OH or halogen, and G is OH, halogen or a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate Acid or triflate, this compound is used to prepare the compound of formula (I).

If desired, the reaction product obtained can be purified by conventional methods such as crystallization and chromatography. If the above method of preparing the compounds of the present invention produces a mixture of stereoisomers, the isomers can be separated by conventional techniques (eg, preparative chromatography). If a chiral center is present, the compound can be prepared in racemic form, or individual mirror isomers can be prepared by mirror-specific synthesis or by resolution.

A preferred pharmaceutically acceptable form of the compound of the present invention is the crystalline form, including this form in pharmaceutical compositions. In the case of salts and solvates of the compounds of the present invention, the additional ion and solvent portions must also be non-toxic. The compounds of the present invention may exhibit different polymorphic forms, and the present invention is intended to cover all such forms.

Another aspect of the present invention refers to a pharmaceutical composition comprising a compound according to the present invention as described above according to general formula I or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable Carrier, adjuvant or vehicle. Therefore, the present invention provides a pharmaceutical composition comprising the compound of the present invention, or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. These pharmaceutical compositions are used For administration to patients.

Examples of pharmaceutical compositions include any solid (lozenges, pills, capsules, granules, etc.) or liquid (solution, suspension or emulsion) composition for oral, topical or parenteral administration.

In a preferred embodiment, the pharmaceutical composition is in oral form, either solid or liquid. Suitable dosage forms for oral administration may be lozenges, capsules, syrops or solutions and may contain conventional excipients known in the industry, such as binding agents such as syrup, gum arabic, gelatin, sorbitol, tragacanth Or polyvinylpyrrolidone; fillers such as lactose, sugar, maize starch, calcium phosphate, sorbitol or glycine; tablet lubricants such as magnesium stearate; disintegrants such as starch, polyvinyl Pyrrolidone, sodium starch glycolate or microcrystalline cellulose; or a pharmaceutically acceptable wetting agent, such as sodium lauryl sulfate.

The solid oral composition can be prepared by conventional methods of blending, filling, or making ingots. Repeated blending operations can be used to distribute the active agent throughout those compositions employing large amounts of fillers. These operations are customary in the industry. Lozenges can be prepared, for example, by wet or dry granulation and are optionally applied according to methods well known in ordinary medical practice, specifically with an enteric coating.

The pharmaceutical composition may also be suitable for parenteral administration, such as sterile solutions, suspensions or lyophilized products in appropriate unit dosage forms. Sufficient excipients can be used, such as build-up agents, buffers or surfactants.

The formulations mentioned will be prepared using standard methods (such as those described or mentioned in the Spanish and US Pharmacopeias and similar references).

The compound or composition of the present invention can be administered by any suitable method, such as intravenous infusion, oral preparation, and intraperitoneal and intravenous administration. Due to the convenience of the patient and the chronic nature of the disease to be treated, oral administration is preferred.

In general, the effective dosage of a compound of this invention will depend on the relative potency of the selected compound, the severity of the condition being treated, and the weight of the victim. However, the active compound will usually be administered one or more times per day, for example once, twice, 3 times or 4 times a day, with a typical total daily dose in the range of 0.1 to 1000 mg/kg/day.

The compounds and compositions of the present invention can be used with other drugs to provide combination therapies. Other drugs may form part of the same composition, or be provided as separate compositions for administration at the same time or at different times.

Another aspect of the present invention refers to the use of the compound of the present invention or a pharmaceutically acceptable salt or isomer thereof for the manufacture of a medicament.

Another aspect of the present invention refers to the compound of the present invention or its pharmaceutically acceptable salt or isomer according to general formula I as described above, which is used as a medicament for treating pain. Preferably, the pain is moderate to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, touch pain or hyperalgesia. This may include mechanical touch pain or thermal hyperalgesia.

Another aspect of the invention refers to the use of the compound of the invention for the manufacture of a medicament for the treatment or prevention of pain.

In a preferred embodiment, the pain is selected from moderate to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, touch pain or hyperalgesia, preferably also including mechanical Allergy to touch pain or heat pain.

Another aspect of the invention relates to a method of treating or preventing pain, which method comprises administering to a patient in need of such treatment a therapeutically effective amount of a compound as defined above or a pharmaceutical composition thereof. Treatable pain syndromes are moderate to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, touch pain or hyperalgesia, and this may also include mechanical touch pain or Hot hyperalgesia.

The invention is explained below by means of examples. These descriptions are given by way of examples only, and do not limit the general spirit of the invention.

General Experimental Part Synthesis Description Two different general methods have been developed for obtaining compounds of the present invention, as described in Methods A and B below, and further detailed in Schemes 1-8.

方法A 其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 、Y₂ 及n具有如技術方案1中所定義之含義，LG表示脫離基，且Z表示適宜官能基以實施該轉變，且R₁ -W表示式III-1、III-2、III-3或III-5之化合物，如下文於方案1至4中所詳述。 Method A illustrates a one-step method for preparing compounds of general formula (I) starting from compounds of formula (II), as shown in the following scheme:

Method A where R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ , Y ₂ and n have the meanings as defined in technical scheme 1, LG represents a leaving group, and Z Represents a suitable functional group to carry out the transformation, and R ₁ -W represents a compound of formula III-1, III-2, III-3, or III-5, as detailed in Schemes 1 to 4 below.

In addition, the amine group NR ₃ R _3′ present in the compound of formula (I) can be represented by the compound of formula (IV) (where LG represents a leaving group (such as chlorine, bromine, iodine, mesylate, tosylate, p-nitro Benzenesulfonate or triflate)) is reacted with an amine of formula (V) to provide a compound of formula (I) and later incorporated into the synthesis, as shown in the scheme above. The alkylation reaction is carried out in a suitable solvent (such as ethanol, dimethylformamide, dimethylsulfoxide or acetonitrile, preferably ethanol), using an excess of amine (V), or optionally a base (such as K ₂ CO ₃ , N , N -diisopropylethylamine or triethylamine), preferably at a suitable temperature including between room temperature and reflux temperature, preferably by heating, or alternatively, these reactions may Implemented under microwave heating. In addition, activators such as sodium iodide or potassium iodide can be used. This transformation can also be carried out starting from the compound of formula (II-LG) to prepare the compound of formula (II).

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n具有如技術方案1中所定義之含義，Q表示氯、溴、碘或三氟甲磺酸根且LG表示脫離基(例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根)。 Scheme 1 The general synthetic route for preparing compounds of formula (I) (where X represents a bond) according to method A, thereby producing compounds of formula (Ia) starting from compounds of formula (IIa) is shown in Scheme 1:

Where R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , Y ₁ , Y ₂ and n have the meanings as defined in technical scheme 1, Q represents chlorine, bromine, iodine or trifluoromethyl Sulfonate and LG represent a leaving group (eg chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate).

The preparation of compounds of formula (Ia) from compounds of formula (IIa) is carried out by using Pd catalysts (eg ginseng (dibenzylideneacetone) dipalladium (0) under Buchwald-Hartwig conditions ) Or palladium acetate), and a suitable ligand (preferably a phosphine ligand, such as BINAP or XPhos), using a suitable base (such as sodium tributoxide or cesium carbonate) in a suitable solvent (such as toluene or 1,4-dioxane) Alkane), at a suitable temperature, preferably heated, and treating the compound of formula (IIa) with a suitable N -containing cyclic reagent of formula (III-1). Alternatively, the reaction may use a Cu catalyst (such as copper iodide) and a suitable ligand (preferably an amine-based ligand, such as N ¹ , N ² -dimethylethane-1 under Ulman arylation conditions ,2-diamine), in the presence of a suitable base (such as potassium phosphate or potassium carbonate), in a suitable solvent (such as 1,4-dioxane or dimethylformamide), at a suitable temperature, preferably Heat to implement.

Alternatively, the amine group NR ₃ R _3′ present in the compound of formula (Ia) or (IIa) can follow the above method A by the precursor compound of formula (IVa) or (IIa-LG) and the amine of formula (V), respectively The conditional reactions described in later are incorporated into the synthesis.

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及p具有如技術方案1中所定義之含義，LG表示脫離基(例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根)，Q表示氯、溴、碘或三氟甲磺酸根，M表示適宜有機金屬基團(較佳硼或鋅試劑)且r表示0至4。 Scheme 2 is used to prepare a compound of formula (I) (where -X- represents -[CH ₂ ] _p -) according to method A, so as to produce a compound of formula (Ib) starting from a compound of formula (IIa) or (IIb) The general synthetic route is shown in Scheme 2:

Where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n and p have the meanings as defined in technical scheme 1, LG represents a leaving group (eg chlorine, bromine , Iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate), Q represents chlorine, bromine, iodine or trifluoromethanesulfonate, M represents a suitable organometallic group (preferably boron Or zinc reagent) and r represents 0 to 4.

The preparation of the compound of formula (Ib) from the aldehyde compound of formula (IIb) can be carried out by treating the compound of formula (IIb) with an N -containing cyclic reagent of formula (III-1) under standard reductive amination conditions. The reaction is carried out in a suitable solvent (preferably tetrahydrofuran, dichloroethane or methanol) in the presence of a reducing agent (e.g. sodium triethoxyborohydride, sodium borohydride or sodium cyanoborohydride), as appropriate It is carried out in the presence of an acid (preferably acetic acid) or a base (preferably N , N -diisopropylethylamine).

Alternatively, the compound of formula (Ib) can be prepared by reacting the compound of formula (IIa) with an organometallic reagent (preferably boron or zinc reagent) of formula (III-2). The coupling reaction is under the conventional coupling procedure described in the literature, using a suitable catalyst (preferably a Pd catalyst) and a suitable ligand (preferably a phosphine ligand) (e.g. tetrakis(triphenylphosphine)palladium(0), Or palladium acetate and XPhos), in the presence of a suitable base (such as potassium carbonate or cesium carbonate), in a suitable solvent (such as tetrahydrofuran, 1,2-dimethoxyethane or 1,4-dioxane, or Water mixture).

In addition, the amine group NR ₃ R _3′ present in the compound of formula (Ib), (IIa) or (IIb) can be obtained by formula (IVb), (IIa-LG) or (IIb-LG) and formula (V) The amines follow the conditions described in Method A above and are later incorporated into the synthesis.

This process can be easily adapted by selecting the corresponding reagent, where -X- represents -[CR _a R _b ] _p -.

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 、n及p具有如技術方案1中所定義之含義且LG表示脫離基(例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根)。 Scheme 3 is used to prepare the compound of formula (I) (where -[CH ₂ ] _p C(O)[CH ₂ ] _q -and q is 0) according to method A, thus starting from the compound of formula (IIc) to produce formula (Ic) ) The general synthetic route of the compound is shown in Scheme 3:

Where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n and p have the meanings as defined in technical scheme 1 and LG represents a leaving group (e.g. chlorine, bromine , Iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate).

The preparation of the compound of formula (Ic) from the acid compound of formula (IIc) and the N -containing cyclic reagent of formula (III-1) can be carried out under conventional amidation conditions. For example, the reaction system using a suitable coupling agent (e.g., N - (3- dimethylaminopropyl) - N '- ethylcarbodiimide (the EDC), dicyclohexyl carbodiimide (DCC) , N -[(dimethylamino)-1 H -1,2,3-triazolo-[4,5- b ]pyridin-1-ylmethylene]- N -methylmethylammonium hexafluoro Phosphate N -oxide (HATU) or N , N , N ', N' -tetramethyl- O- ( 1H -benzotriazol-1-yl) ureonium hexafluorophosphate (HBTU)), depending on In the presence of 1-hydroxybenzotriazole, optionally in the presence of an organic base (e.g. N -methylmorpholine or N , N -diisopropylethylamine), in a suitable solvent (e.g. dichloromethane or di Methylformamide) and at a suitable temperature, preferably at room temperature. Alternatively, the amidation can be carried out in two steps by: first converting the acid of formula (IIc) to its corresponding acyl halide following the standard conditions described in the literature, and then allowing it to react with the compound of formula (III-1) In a suitable solvent (e.g. dichloromethane, tetrahydrofuran, ethyl acetate or ethyl acetate-water mixture), in an organic base (e.g. triethylamine or N , N -diisopropylethylamine) or an inorganic base (e.g. K ₂ CO ₃ ) in the presence and at a suitable temperature (preferably including between 0°C and room temperature). In addition, activators such as 4-dimethylaminopyridine can be used.

In addition, the amine group NR ₃ R _3′ present in the compound of formula (Ic) or (IIc) can follow the above method A by the precursor compound of formula (IVc) or (IIc-LG) and the amine of formula (V), respectively The conditional reactions described in later are incorporated into the synthesis.

This process can be easily adapted by selecting the corresponding reagent, where -X- means -[CR _a R _b ] _p C(O)[CH ₂ ] _q -or-[CR _a R _b ] _p C(O)[CR _c R _d ] _q -.

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、R_z 、Y₁ 、Y₂ 、n、p及q具有如技術方案1中所定義之含義，LG表示脫離基(例如氯、溴、碘、甲磺酸根、甲苯磺酸根、對硝基苯磺酸根或三氟甲磺酸根)且Z表示OH或鹵素(較佳溴或氯)。 Scheme 4 is used to prepare a compound of formula (I) according to Method A (where -X- represents -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -), thereby formula (IId) or ( The general synthetic route for compounds of formula IIa to start producing compounds of formula (Id) is shown in Scheme 4:

Where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , R _z , Y ₁ , Y ₂ , n, p, and q have the meanings as defined in technical solution 1, and LG stands for the radical (Eg chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate) and Z represents OH or halogen (preferably bromine or chlorine).

The reaction of the amine compound of formula (IId) with the amide reagent of formula (III-3) to provide the compound of formula (Id) can be carried out under the amidation conditions described above in Scheme 3 for the preparation of the compound of formula (Ic). Alternatively, the compound of formula (Id) can be prepared in 2 steps by treating the compound of formula (IId) with an amide of formula (III-4) under the same amidation conditions to obtain the compound of formula (VI), followed by Under conventional alkylation conditions (such as those described in Method A for the reaction of a compound of formula (IV) with an amine of formula (V)), they are reacted with the N -containing cyclic reagent of formula (III-1).

Finally, or alternatively, the compound of formula (Id) (where p is 0) can be prepared by reacting the compound of formula (IIa) with the formamide compound of formula (III-5). In this reaction, a Cu catalyst (such as copper iodide) and a suitable ligand (preferably an amine ligand, such as N ¹ , N ² -dimethylethane-1,2 -Diamine), in the presence of a suitable base (eg potassium phosphate), in a suitable solvent (eg 1,4-dioxane or dimethylformamide), at a suitable temperature, preferably by heating. Alternatively, the coupling reaction can be carried out under Buchwald-Hartwig conditions using a suitable Pd catalyst and a suitable ligand (preferably a phosphine ligand).

In addition, the amino group NR ₃ R _3′ present in the compound of formula (Id), (IIa) or (IId) can be obtained by formula (IVd), (IIa-LG) or (IId-LG) and formula (V) The amines follow the conditions described in Method A above and are later incorporated into the synthesis.

This process can be easily adapted by selecting the corresponding reagent, where -X- represents -[CR _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -.

方法B 其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 、Y₂ 及n具有如技術方案1中所定義之含義，Z表示OH或脫離基，且G表示OH、鹵素或脫離基，此取決於n之含義。具體反應條件詳述於下文方案5及6中。 Method B illustrates an alternative one-step method for preparing compounds of general formula (I) starting from compounds of formula (VII), as shown in the following scheme:

Method B where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ , Y ₂ and n have the meanings as defined in technical scheme 1, Z represents OH or a leaving group, And G represents OH, halogen, or leaving group, which depends on the meaning of n. The specific reaction conditions are detailed in Schemes 5 and 6 below.

As mentioned above, the amine group NR ₃ R _3′ present in the compound of formula (I) can be reacted by the precursor compound of formula (IV) and the amine of formula (V) following the conditions described in Method A above. Later included in the synthesis.

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 及Y₂ 具有如技術方案1中所定義之含義，n係0，Z表示OH或脫離基，且G表示OH或鹵素。 Scheme 5 The general synthetic route for the preparation of compounds of formula (I) (where n is 0) according to method B to produce compounds of formula (Ie) is shown in scheme 5:

Where R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ and Y ₂ have the meanings as defined in technical scheme 1, n is 0, Z represents OH or a leaving group, And G represents OH or halogen.

Depending on the meaning of G and Z, different reaction conditions will apply: a) When G is OH and Z represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or In the case of trifluoromethanesulfonate, the alkylation reaction between the phenol of formula (VIIa) and the alkylating agent of formula (VIII) is in a suitable solvent (such as dimethylformamide, dimethylacetamide, Dimethyl sulfoxide, acetonitrile, dichloromethane or 1,4-dioxane), in the presence of a base (e.g. K ₂ CO ₃ , Cs ₂ CO ₃ , sodium hydride or potassium tertiary butoxide) It is carried out at a suitable temperature between room temperature and reflux temperature, or alternatively, the reactions can be carried out in a microwave reactor. In addition, activators such as sodium iodide can be used. b) When G is OH and Z represents OH, the reaction is carried out under conventional Mitsunobu conditions by using azo compounds (such as 1,1'-(azodicarbonyl) dihexahydropyridine (ADDP), azobis Treatment of formula (VIIa) with an alcohol of formula (VIII) in the presence of diisopropyl formate (DIAD) or diethyl azodicarboxylate (DEAD)) and a phosphine (such as tributylphosphine or triphenylphosphine) Phenol to implement. The Mitsunobu reaction is carried out in a suitable solvent (such as toluene or tetrahydrofuran) at a suitable temperature including between room temperature and reflux temperature. c) When G is halogen and Z represents OH, the reaction is carried out by using a compound of formula (VIIa) in the presence of a strong base (such as sodium hydride or potassium tertiary butoxide) under conventional aromatic nucleophilic substitution conditions ( Where G represents halogen (preferably fluorine), the alcohol of formula (VIII) is treated by the treatment. The reaction is carried out in a suitable solvent (such as a polar aprotic solvent, preferably dimethylformamide, dimethylacetamide or dimethylsulfoxide) at a suitable temperature between room temperature and reflux temperature 1. Preferably, heating is carried out, or alternatively, the reactions can be carried out in a microwave reactor. Alternatively, when G is bromine or iodine, the compound of formula (VIII) can be introduced under cross-coupling conditions using a Pd or Cu catalyst and a suitable ligand.

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 及Y₂ 具有如技術方案1中所定義之含義，n係1，且Z表示OH且G表示脫離基，或另一選擇為，Z表示脫離基且G表示OH。 Scheme 6 The general synthetic route for the preparation of compounds of formula (I) (where n is 1) according to method B, to produce compounds of formula (If) is shown in scheme 6:

Where R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ and Y ₂ have the meanings as defined in technical solution 1, n is 1, and Z represents OH and G represents Leaving the group, or alternatively, Z represents the leaving group and G represents OH.

The reaction is carried out under standard alkylation reaction conditions (such as those described in Scheme 5 above).

其中R₁ 、R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、X、Y₁ 、Y₂ 及n具有如技術方案1中所定義之含義，且G及Z具有方案1至6中如上文所定義之含義，且及R₁ -W表示方案1至6中如上文所定義之式III-1、III-2、III-3或III-5之化合物。 Scheme 7 The preparation of key compounds of formula (II) and (VII) from common precursors of formula (IX) is outlined in scheme 7 below:

Where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ , Y ₂ and n have the meanings as defined in technical scheme 1, and G and Z have schemes 1 to 6 Has the meaning as defined above, and R ₁ -W represent the compounds of the formulae III-1, III-2, III-3 or III-5 in Schemes 1 to 6 as defined above.

The preparation of compounds of formula (VII) from compounds of formula (IX) and compounds of formula (III) can be carried out under the reaction conditions described in general method A above and further detailed in schemes 1 to 4.

The preparation of compounds of formula (II) or (II-LG) from compounds of formula (IX) and compounds of formula (VIII) can be carried out under the reaction conditions described in general method B above and further detailed in schemes 5 and 6.

其中R₂ 、R₃ 、R_3’ 、R₄ 、R_4’ 、Y₁ 、Y₂ 及n具有如技術方案1中所定義之含義，Q表示氯、溴、碘或三氟甲磺酸根且r表示0至4。 Scheme 8 In addition, compounds of formula (IIb) can be prepared from compounds of formula (IIa) following several methods described in the literature. For example, two synthetic routes are illustrated in Scheme 8 below:

Where R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n have the meanings as defined in technical scheme 1, Q represents chlorine, bromine, iodine or trifluoromethanesulfonate and r represents 0 to 4.

Following route A, the compound of formula (IIa) is converted to the nitrile compound of formula (X) (depending on the nature of r, under the standard conditions described in the literature), followed by a suitable source of hydride (eg diisobutyl) Aluminum hydride) to provide the compound of formula IIb.

Or and following route B, the compound of formula (IIa) is converted to the alkenyl compound of formula (XI) via a cross-coupling reaction, preferably Suzuki coupling, using conventional reaction conditions, followed by oxidation by treatment with reagents such as osmium tetroxide The cleavage is followed by treatment with an oxidizing agent (eg sodium periodate), optionally in the presence of additives (eg pyrimidine or 2,6-lutidine), to provide the compound of formula IIb.

By selecting the corresponding reagents, this process can be easily adapted to prepare compounds of formula IIb' or IIb'-LG, which can be used to prepare compounds of formula Ib or IVb according to Scheme 2, where -X- represents -[CR _a R _b ] _p -, formulas (III), (III-1), (III-2), (III-3), (III-4), (III-5), ( Compounds V), (VIII) and (IX) are commercially available or can be synthesized following common procedures described in the literature.

In addition, certain compounds of the present invention can also be obtained starting from other compounds of formula (I) by carrying out appropriate conversion reactions of functional groups in one or several steps under standard experimental conditions using well-known reactions in organic chemistry.

In some of the above processes, it may be necessary to protect and protect suitable amine groups (eg Boc (third butoxycarbonyl), Teoc (2-(trimethylsilyl)ethoxycarbonyl) Or benzyl group) and a common silicon-based protecting group used to protect the hydroxyl group together with a reactive or unstable group. The procedures for introducing and removing these protecting groups are well known in the industry and the findings can be thoroughly described in the literature.

In addition, the compound of formula (I) can be obtained by resolving the racemic compound of formula (I) by chiral preparative HPLC or by crystallization of diastereomeric salts or co-crystals in mirror-pure form. Alternatively, the resolution step can be performed at any previous stage using any suitable intermediate.

Examples The following abbreviations are used in the examples: ACN: acetonitrile aq.: aqueous BINAP: 2,2′-bis(diphenylphosphino)-1,1′-binaphthalene Boc: third butoxycarbonyl CH: cyclohexyl Alkane DCE: dichloroethane DCM: dichloromethane Deprot.: deprotection DIAD: diisopropyl azodicarboxylate; DIBAL-H: diisobutylaluminum hydride DIPEA: N,N -diisopropyl ethyl Amine DME: 1,2-dimethoxyethane DMF: N,N -dimethylformamide DMSO: dimethyl sulfoxide EtOAc: ethyl acetate EtOH: ethanol EX: Example h: hour HATU: O- ( 7-azabenzotriazol-1-yl) -N,N,N ′ ,N′ -tetramethylureonium hexafluorophosphate HPLC: high performance liquid chromatography INT: intermediate MeOH: methanol MS: mass spectrometry Min: minutes Pd ₂ (dba) ₃ : ginseng (dibenzylideneacetone) dipalladium (0) Pd (PPh ₃ ) ₄ : tetrakis (triphenylphosphine) palladium (0) Quant: quantitative Ret.: retention rt : Room temperature Sat: saturated Sol.: solution SPhos: 2-dicyclohexylphosphino-2',6'-dimethoxybiphenyl Teoc: 2-(trimethylsilyl)ethoxycarbonyl TFA: tri Fluoroacetic acid THF: tetrahydrofuran wt: weight

The HPLC-MS spectrum was measured using the following method: Method A column: Gemini-NX 30 × 4.6 mm, 3 um temperature: 40°C flow rate: 2.0 mL/min gradient: NH ₄ HCO ₃ pH 8: ACN (95:5)- --0.5min---(95:5)---6.5min---(0:100)---1min---(0:100) The sample is dissolved in NH ₄ HCO ₃ pH at about 1 mg/mL 8/ Method B column in ACN: Kinetex EVO 50 × 4.6 mm, 2.6 um Temperature: 40°C Flow rate: 1.5 mL/min Gradient: NH ₄ HCO ₃ pH 8: ACN (95:5)---0.5min-- -(95:5)---6.5min---(0:100)---2min---(0:100) The sample is dissolved in NH ₄ HCO ₃ pH 8/ ACN at about 1 mg/mL Method C Column: Luna C18 250 × 4,6 mm 5um Temperature: 40℃ Flow rate: 1 mL/min Gradient: H ₂ O-0.1% HCOOH /ACN (100:0)---30min---(0:100) ---10min---(0:100) The sample is dissolved in ACN at about 1 mg/mL Method D Column: Kromasil C18 250 x 4,6 mm 5um Temperature: 40°C Flow rate: 1 mL/min Gradient: H ₂ O-0.1%HCOOH / ACN (100:0)---30min---(0:100) The sample is dissolved in ACN/H ₂ O 1:1 at about 4mg/mL

Synthesis of Intermediate Intermediate 1: ( R )-(3-(2-Bromophenoxy)-3-(thiophen-2-yl)propyl)(ethyl)aminocarboxylic acid 2-(trimethylsilicone Group) ethyl ester

Step 1. ( R )-3-(ethylamino)-1-(thiophen-2-yl)propan-1-ol: convert ( R )-3-chloro-1-(thiophen-2-yl)propan A solution of -1-ol (7 g, 39.6 mmol) and ethylamine (70 wt% in water, 31 mL, 396 mmol) in EtOH (175 mL) was heated in a sealed flask at 90°C overnight. The solvent was evaporated, the residue was dissolved in DCM and it was washed with 1 N NaOH, dried over MgSO ₄ , filtered and concentrated to dryness. The crude product (7.74 g) was slurried in methylcyclohexane (44 mL) and heated at 60 °C for 1 h. Then, let it cool and stir it at rt for 1 h. The solid was filtered, washed with methylcyclohexane and dried under vacuum to provide the title compound (2.68 g, 36% yield).

Step 2. ( R )-3-(2-Bromophenoxy)- N -ethyl-3-(thiophen-2-yl)propan-1-amine: the product obtained in step 1 under N ₂ atmosphere (0.98 g, 5.3 mmol) and 1-bromo-2-fluorobenzene (2.29 mL, 21.1 mmol) in DMSO (1.6 mL) were added potassium tert-butoxide (0.6 g, 5.3 mmol) and the reaction mixture Heat at 60°C for 8 h. It was then cooled to rt, water was added and the aqueous phase was extracted twice with EtOAc. The combined organic phase was dried over MgSO ₄ , filtered and evaporated to dryness. The crude product was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)) to give the title compound (1.14 g, 63% yield).

Step 3. The title compound: To a solution of the product obtained in Step 2 (1.14 g, 3.3 mmol) in DCM (1.5 mL) under N ₂ atmosphere, add DIPEA (0.58 mL, 3.3 mmol) and 4-nitrocarbonate A solution of phenyl (2-(trimethylsilyl)ethyl) ester (0.95 g, 3.3 mmol) in DCM (1.5 mL), and the mixture was stirred at rt overnight. A saturated solution of NaHCO _{3 was} added and it was extracted twice with DCM. The combined organic phases were washed with 2N aqueous NaOH, dried over MgSO ₄ , filtered and concentrated to dryness. The residue was purified by flash chromatography (silica gel, gradient CH to EtOAc) to give the title compound (1.46 g, 90% yield).

Use appropriate starting materials to prepare intermediate 2-3 using this method:

Intermediate 4: (3-(2-bromophenoxy)-3-(3-fluorophenyl)propyl)(methyl)carbamic acid 2-(trimethylsilyl)ethyl ester

Step 1. 1-(3-fluorophenyl)-3-(methylamino)propan-1-one hydrochloride: In a sealed tube, place 1-(3-fluorophenyl)ethanone (7.5 g , 54.7 mmol), methylamine hydrochloride (4.43 g, 77 mmol) and paraformaldehyde (2.3 g, 65.6 mmol) were dissolved in EtOH (60 mL) and the mixture was heated at 100° C. overnight. The solvent was partially evaporated, and the precipitated solid was filtered off. The filtrate was evaporated to dryness, and the residue was slurried in EtOAc (150 mL). The solid was filtered, washed with EtOAc and dried under vacuum to give the title compound (6.35 g, 40% yield).

Step 2. 1-(3-fluorophenyl)-3-(methylamino)propan-1-ol: cooling the product obtained in Step 1 (6.35 g, 21.9 mmol) in MeOH (140 mL) NaBH ₄ (2.48 g, 65.6 mmol) was added portionwise to the solution and the mixture was stirred at 0-5°C for 1 h. Then a saturated solution of NH ₄ Cl (25 mL) was added and MeOH was distilled off. The aqueous phase was extracted with CHCl ₃ and finally with CHCl ₃ /MeOH (9:1). The combined organic extracts were dried over MgSO ₄ , filtered and concentrated to dryness to give the title compound (2 g, 50% yield).

Step 3. 3-(2-Bromophenoxy)-3-(3-fluorophenyl) -N -methylpropan-1-amine: follow the experimental procedures and use steps described in step 2 of intermediate 1 Compound obtained in 2 to obtain the title compound (2.96 g, 80% yield)

Step 4. The title compound: Following the experimental procedure described in Step 3 of Intermediate 1, starting from the product obtained in Step 3, the title compound (4 g, 96% yield) was obtained.

Intermediate 5: 2-(3-chloro-1-(thiophen-2-yl)propoxy)benzaldehyde

Step 1. 2-(3-chloro-1-(thiophen-2-yl)propoxy)benzonitrile: To 3-chloro-1-(thiophen-2-yl)propan-1 cooled at 0°C -A solution of alcohol (10 g, 52 mmol), triphenylphosphine (15 g, 57.2 mmol) and 2-hydroxybenzonitrile (6.8 g, 57.2 mmol) in anhydrous THF (252 mL) was added DIAD dropwise (11.5 mL, 58.3 mmol) and the mixture was stirred at rt overnight. The solvent was concentrated under vacuum and the residue was purified by flash chromatography (silica gel, gradient CH to EtOAc) to give the title compound (13.9 g, 96% yield).

Step 2. The title compound: DIBAL-H (25 wt% solution in toluene) was added dropwise to a solution of the product (4 g, 14.4 mmol) obtained in Step 1 cooled at 0°C in toluene (40 mL) , 13.5 mL, 20.2 mmol) and the reaction mixture was stirred at 0-5 °C for 4 h. Then, a 10% aqueous HCl solution was slowly added to quench the reaction and the mixture was stirred at rt for 10 min. It was extracted with EtOAc and the combined organic phases were washed with water and brine, dried over Na ₂ SO ₄ , filtered and concentrated to dryness. The residue was purified by flash chromatography (silica gel, gradient CH to EtOAc) to give the title compound (1.54 g, 38% yield).

(1) 在步驟2中使用-78℃下之DCM中之1 M DIBAL-HUse appropriate starting materials to prepare intermediate 6 using this method:

(1) Use 1 M DIBAL-H in DCM at -78℃ in step 2

在密封管中，將(3-氯-3-苯丙基)(甲基)胺基甲酸第三丁基酯(1 g, 3.52 mmol)、K₂ CO₃ (1.46 g, 10.57 mmol)、KI (58 mg, 0.352 mmol)及2-羥基苯甲醛(0.38 mL, 3.52 mmol)於DMF (23 mL)中之混合物於60℃下加熱過夜。在冷卻至r.t.後，向反應混合物中添加水且將其用EtOAc萃取。將合併之有機相用1 N NaOH水溶液及鹽水洗滌，經MgSO₄ 乾燥，過濾且濃縮至乾燥，以得到標題化合物(1.21 g, 93%產率)。Intermediate 7: (3-(2-Methylphenoxy)-3-phenylpropyl)(methyl)carbamic acid tert-butyl ester:

In a sealed tube, combine (3-chloro-3-phenylpropyl)(methyl)carbamic acid tert-butyl ester (1 g, 3.52 mmol), K ₂ CO ₃ (1.46 g, 10.57 mmol), KI A mixture of (58 mg, 0.352 mmol) and 2-hydroxybenzaldehyde (0.38 mL, 3.52 mmol) in DMF (23 mL) was heated at 60°C overnight. After cooling to rt, water was added to the reaction mixture and it was extracted with EtOAc. The combined organic phase was washed with 1 N aqueous NaOH solution and brine, dried over MgSO ₄ , filtered and concentrated to dryness to give the title compound (1.21 g, 93% yield).

Use appropriate starting materials to prepare intermediate 8 using this method:

Intermediate 9: ( R )-methyl(3-(2-(2-oxoethyl)phenoxy)-3-(thien-2-yl)propyl)aminocarboxylic acid 2-(trimethyl (Silysyl) ethyl ester

Step 1. ( R )-(3-(2-(cyanomethyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)aminocarboxylic acid 2-(trimethylsilicone Base) ethyl ester: Pd ₂ (dba) ₃ (91 mg, 0.1 mmol), SPhos (123 mg, 0.3 mmol) and potassium 2-cyanoacetate (0.79 g, 6.48 mmol) were charged in a sealed tube. The tube was purged with argon, and a solution of intermediate 3 (2.5 g, 4.98 mmol) in mesitylene (12.5 mL) was added. The reaction was heated at 140°C under argon overnight. The solvent was then concentrated and the residue was purified by flash chromatography (silica gel, gradient CH to EtOAc) to give the title compound (1.8 g, 78% yield).

Step 2. The title compound: DIBAL-H (1 M solution in DCM) was added dropwise to a solution of the product (0.5 g, 1.08 mmol) obtained in Step 1 cooled at -78°C in DCM (8 mL) , 3.25 mL, 3.25 mmol) and the reaction mixture was stirred at -78 °C for 1.5 h. Then, it was poured into a saturated solution of potassium tartrate cooled at -78°C, and the mixture was brought to rt with stirring. It was extracted with DCM and the combined organic phase was washed with brine, dried over MgSO ₄ , filtered and concentrated to dryness to give the title compound (406 mg, 81% yield).

Use appropriate starting materials to prepare intermediate 10 using this method:

Intermediate 11: ( R )-ethyl(3-(2-(2-oxoethyl)phenoxy)-3-(thien-2-yl)propyl)aminocarboxylic acid 2-(trimethyl (Silysyl) ethyl ester

Step 1. ( R )-(3-(2-allylphenoxy)-3-(thien-2-yl)propyl)(ethyl)carbamic acid 2-(trimethylsilyl)ethyl Base ester, in a sealed tube, filled with Pd(PPh ₃ ) ₄ (137 mg, 0.145 mmol), 2-allyl-4,4,5,5-tetramethyl-1,3,2-diox Heteroborolane (0.73 g, 4.3 mmol) and potassium carbonate (0.3 g, 2.17 mmol). The tube was purged with argon, and a solution of intermediate 1 (0.7 g, 1.45 mmol) in 1,4-dioxane (18 mL) was added. The reaction was heated at 110 °C under argon atmosphere for 4 h. The reaction mixture was filtered through a pad of celite, which was washed with EtOAc. The filtrate was washed with brine, dried over MgSO ₄ , filtered and concentrated to dryness. The residue was purified by flash chromatography (silica gel, gradient CH to EtOAc) to give the title compound (478 mg, 74% yield).

Step 2. The title compound: To a solution of the product obtained in Step 1 (478 mg, 1.07 mmol) in a THF-water mixture (2:1, 22.5 mL), add an OsO ₄ solution (4 wt% aq. sol. , 0.75 mL, 0.118 mmol). The reaction was stirred at rt for 10 min. and then NaIO ₄ (573 mg, 2.68 mmol) was added. The mixture was stirred at rt for 15 min. The solvent was concentrated and the aqueous phase was extracted with EtOAc. The combined organic extracts were dried over MgSO ₄ , filtered and concentrated to dryness to give the title compound (448 mg, 93% yield).

Use appropriate starting materials to prepare intermediate 12 using this method:

Intermediate 13: 2-(3-(((third butoxycarbonyl)(methyl)amino)-1-phenylpropoxy)benzoic acid

Step 1. Methyl 2-(3-((third butoxycarbonyl)(methyl)amino)-1-phenylpropoxy)benzoate: follow the experimental procedure described in Intermediate 7, But using methyl 2-hydroxybenzoate as the starting material, the title compound (1.48 g, 63% yield) was obtained.

Step 2. The title compound: To a solution of the compound obtained in Step 1 (1.48 g, 3.7 mmol) in a mixture of THF (7.5 mL) and water (7.5 mL) was added lithium hydroxide monohydrate (1.2 g, 30 mmol) and the reaction mixture was heated at 50 °C overnight. The solvent was concentrated, the pH was adjusted to 3 with 6 N HCl and it was extracted with EtOAc. The combined organic phase was dried over MgSO ₄ , filtered and concentrated to dryness to give the title compound (1.1 g, 78% yield).

Intermediate 14: ( R )-(3-(2-Bromophenoxy)-3-(thiophen-2-yl)propyl)aminocarboxylic acid 2-(trimethylsilyl)ethyl ester

Step 1. ( R )-2-(3-Hydroxy-3-(thien-2-yl)propyl)isoindoline-1,3-dione: To ( R )-3-chloro-1-( Thiphen-2-yl)propan-1-ol (2 g, 11.3 mmol) in anhydrous DMF (10 mL) was added potassium phthalimide (3.98 g, 21.5 mmol) and potassium iodide (56 mg, 0.34 mmol) ), and the mixture was heated at 100° C. for 3 h. Sol. Water and NaHCO ₃ sat. sol. were added and the mixture was stirred at rt for 30 min. The phases were separated and the aqueous phase was extracted with EtOAc. The combined organic extracts were washed with water and brine, dried over MgSO ₄ , filtered and evaporated to dryness. The crude product was purified by flash chromatography (silica gel, gradient CH to EtOAc) to give the title compound (2.7 g, 83% yield).

Step 2. ( R )-3-Amino-1-(thien-2-yl)propan-1-ol: The compound obtained in Step 1 (2.5 g, 8.74 mmol) and hydrazine hydrate (4.25 mL, 43.7 mmol ) The solution in MeOH (200 mL) was stirred at rt overnight. The resulting suspension was filtered and the solid was washed with MeOH. The filtrate was concentrated to dryness, resuspended in MeOH and leached through a _C18 column. The solvent was concentrated, and the resulting solid residue was suspended in DCM (50 mL) and stirred at rt for 1 h. The solid was removed by filtration and the filtrate was concentrated to dryness to obtain the title compound (1.02 g, 75% yield).

Step 3. ( R )-3-(2-Bromophenoxy)-3-(thiophen-2-yl)propan-1-amine: follow the experimental procedure described in Step 2 of Intermediate 1, from Step 2 The product obtained in the beginning starts to obtain the title compound (1.75 g, 86% yield).

Step 4. The title compound: Following the experimental procedure described in Step 3 of Intermediate 1, starting from the product obtained in Step 3, the title compound (1.6 g, 68% yield) was obtained.

遵循中間體1之步驟2及3中所述之實驗程序、自(R )-3-(甲基胺基)-1-(噻吩-3-基)丙-1-醇(根據WO2018115064中間體14製備)開始，獲得標題化合物。Intermediate 15: ( R )-(3-(2-Bromophenoxy)-3-(thiophen-3-yl)propyl)(methyl)aminocarboxylic acid 2-(trimethylsilyl)ethyl ester

Follow the experimental procedures described in steps 2 and 3 of intermediate 1, from ( R )-3-(methylamino)-1-(thiophen-3-yl)propan-1-ol (according to WO2018115064 intermediate 14 Preparation) begins to obtain the title compound.

Intermediates 16-17 were prepared following the experimental procedures described for the synthesis of Intermediate 11, using suitable starting materials:

將中間體3 (0.300 g, 0.64 mmol)、三丁基甲氧化錫(0.26 mL, 0.96 mmol)、乙酸異丙烯基酯(0.1 mL, 0.96 mmol)、乙酸鈀(II) (7.1 mg, 0.032 mmol)及三(鄰甲苯基)膦(19 mg, 0.064 mmol)於甲苯(2 mL)中之混合物於100℃下在氮氣氛下攪拌5 h。使反應混合物冷卻且然後將其用EtOAc (5 mL)及4 M氟化鉀水溶液(2 mL)稀釋且將混合物攪拌15 min。將其經由Celite^® 墊過濾且分離各相。將有機相用鹽水洗滌且蒸發至乾燥。藉由急速層析(矽膠，梯度CH至EtOAc)純化粗產物，從而產生標題化合物(267 mg, 93%產率)。Intermediate 18: ( R )-methyl(3-(2-(2-oxopropyl)phenoxy)-3-(thien-2-yl)propyl)aminocarboxylic acid 2-(trimethyl (Silysyl) ethyl ester

Intermediate 3 (0.300 g, 0.64 mmol), tributyltin methoxide (0.26 mL, 0.96 mmol), isopropenyl acetate (0.1 mL, 0.96 mmol), palladium(II) acetate (7.1 mg, 0.032 mmol) and A mixture of tri(o-tolyl)phosphine (19 mg, 0.064 mmol) in toluene (2 mL) was stirred at 100°C for 5 h under a nitrogen atmosphere. The reaction mixture was allowed to cool and then it was diluted with EtOAc (5 mL) and 4 M aqueous potassium fluoride solution (2 mL) and the mixture was stirred for 15 min. The phases were separated and filtered through a pad of Celite ^®. The organic phase was washed with brine and evaporated to dryness. The crude product was purified by flash chromatography (silica gel, gradient CH to EtOAc) to give the title compound (267 mg, 93% yield).

Intermediates 19 and 20: (2 R ,6 R ,7 S )-4-isopropyl-2,7-dimethyl-1-oxa-4,9-diazaspiro[5.5]undecane -3-one trifluoroacetate and (2 R ,6 S ,7 R )-4-isopropyl-2,7-dimethyl-1-oxa-4,9-diazaspiro[5.5 ]Undecane-3-one trifluoroacetate

Step 1. (3 R ,4 S )-4-methyl-1-oxa-6-azaspiro[2.5]octane-6-carboxylic acid tert-butyl ester and (3 S ,4 R )-4 -Methyl-1-oxa-6-azaspiro[2.5]octane-6-carboxylic acid tert-butyl ester: To potassium tert-butoxide (2 g, 18.3 mmol) in DMSO (16 mL) To the solution was added trimethyl sulfoxide (4 g, 18.3 mmol) in portions, keeping the internal temperature between 20-25°C, and then the mixture was stirred at rt for 1.5 h. DME (4.5 mL) was added and the solution was cooled to 0-5 °C. Then, 3-methyl-4-oxohexahydropyridine-1-carboxylic acid tert-butyl ester (3 g, 14 mmol) in a mixture of DME (4.5 mL) and DMSO (1.5 mL) was added dropwise The solution, keeping the internal temperature between 0-5 °C, and the reaction mixture was further stirred for 1 h. Water and EtOAc were added, the phases were separated and the aqueous phase was extracted twice with EtOAc. The organic phases were combined, washed with water (x4), dried over MgSO ₄ and concentrated under vacuum to give the title compound as a racemic mixture (2.88 g, 90% yield).

Step 2. (3 S ,4 R )-4-hydroxy-4-((isopropylamino)methyl)-3-methylhexahydropyridine-1-carboxylic acid tert-butyl ester and (3 R , 4 S )-4-hydroxy-4-((isopropylamino)methyl)-3-methylhexahydropyridine-1-carboxylic acid tert-butyl ester: to racemic mixture obtained in step 1 ( 2.88 g, 12.7 mmol) in a solution of ethanol-water 9:1 mixture (43 mL) was added isopropylamine (16.3 mL, 190 mmol) and the reaction mixture was stirred at rt overnight. The solvent was removed under vacuum to give the title compound (3.6 g, 99% yield) as a racemic mixture.

Step 3. (3 S ,4 R )-4-((( ( S )-2-chloro- N -isopropylpropenylamino)methyl)-4-hydroxy-3-methylhexahydropyridine-1- Tert-butyl formate and (3 R ,4 S )-4-((( ( S )-2-chloro- N -isopropylpropenylamino)methyl)-4-hydroxy-3-methylhexahydrogen Pyridine-1-carboxylic acid tert-butyl ester: To a solution of the racemic mixture obtained in step 2 (3.6 g, 12.6 mmol) in ethyl acetate (37 mL) was added K ₂ CO ₃ (4.86 g, 35 mmol) in water (40 mL). After cooling to 0 °C, a solution of ( S )-2-chloropropionyl chloride (2.17 g, 17.1 mmol) in EtOAc (18 mL) was added dropwise. The reaction mixture was stirred at 0 °C for 30 min, the layers were separated and the aqueous phase was extracted with EtOAc. The organic phases were combined, washed with 0.5 M aqueous HCl solution and then saturated NaHCO ₃ solution, dried over MgSO ₄ , filtered and concentrated to dryness to give the title compound (as a 1:1 mixture of diastereomers) without Further purification is used in the next step.

Steps 4a and 4b. (2 R ,6 R ,7 S )-4-isopropyl-2,7-dimethyl-3-oxo-1-oxa-4,9-diazaspiro[ 5.5] Undecane-9-carboxylic acid tert-butyl ester and (2 R ,6 S ,7 R )-4-isopropyl-2,7-dimethyl-3-oxo-1-oxa -4,9-Diazaspiro[5.5]undecane-9-carboxylic acid tert-butyl ester: Using a dry ice/acetone bath, the crude product mixture (4.7 g, 12.5 mmol) obtained in step 3 was dissolved in THF (70 The solution in mL) was cooled to -78°C. After adding a third potassium butoxide solution (13.8 mL, 1 M in THF, 13.8 mmol), the reaction mixture was stirred at -78°C for 30 min. Then a saturated solution of NH ₄ Cl was added, and the aqueous phase was extracted with EtOAc. The organic phases were combined, dried over MgSO ₄ , filtered and concentrated under vacuum. The crude product was purified by flash chromatography (C ₁₈ , gradient NH ₄ HCO ₃ pH 8 to ACN) to give the title compounds 4a (960 mg, 22% yield) and 4b (922 mg, 21% yield).

Steps 5a and 5b. The title compound: a solution of the product (4a) (264 mg, 0.76 mmol) and TFA (0.6 mL, 0.884 mmol) obtained in Step 4 in DCM was stirred at r.t. for 3 h. The volatile material was evaporated to dryness to obtain intermediate 19 (463 mg, 59 wt%, quantitative yield).

Following a similar procedure but starting with the product (4b) obtained in step 4, intermediate 20 (430 mg, 56 wt%, quantitative yield) was obtained.

Intermediates 21 and 22. (2 R ,6 R ,7 S )-7-fluoro-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]11 Alkane-3-one trifluoroacetate and (2 R ,6 S ,7 R )-7-fluoro-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro [5.5] Undecane-3-one trifluoroacetate

Steps 1a and 1b. (trans)-4-fluoro-1-oxa-6-azaspiro[2.5]octane-6-carboxylic acid tert-butyl ester and ( cis )-4-fluoro-1- Oxa-6-azaspiro[2.5]octane-6-carboxylic acid tert-butyl ester: follow the experimental procedure described for the synthesis of step 1 of intermediates 19 and 20, from 3-fluoro-4-oxo Starting with tert-butyl hexahydropyridine-1-carboxylate (3 g, 13.8 mmol), a mixture of cis and trans products was obtained. The mixture was purified by flash chromatography (silica gel, gradient CH to EtOAc) to yield the title compounds 1a (1.39 g, 43% yield) and 1b (397 mg, 12% yield) as racemates.

Step 2. (Trans)-3-fluoro-4-hydroxy-4-((isopropylamino)methyl)hexahydropyridine-1-carboxylic acid tert-butyl ester: starting from the product obtained in step 1a 3. Follow the experimental procedure described in Step 2 of Intermediates 19 and 20 to obtain the title compound (1.81 g, 96 wt%).

Step 3. (3 S ,4 R )-4-((( R )-2-chloro- N -isopropylpropenylamino)methyl)-3-fluoro-4-hydroxyhexahydropyridine-1-carboxylic acid Third butyl ester and (3 R ,4 S )-4-((( ( S )-2-chloro- N -isopropylpropenylamino)methyl)-3-fluoro-4-hydroxyhexahydropyridine- 1-Butyl formic acid: Starting from the product obtained in step 2 and following the experimental procedures described in step 3 of intermediates 19 and 20, the title compound (in the form of a 1:1 mixture of stereoisomers, 1.75 g, 77% yield).

Step 4. (2 R ,6 R ,7 S )-7-fluoro-4-isopropyl-2-methyl-3-oxo-1-oxa-4,9-diazaspiro[5.5 ] Undecane-9-carboxylic acid tert-butyl ester and (2 R ,6 S ,7 R )-7-fluoro-4-isopropyl-2-methyl-3-oxo-1-oxa -4,9-diazaspiro[5.5]undecane-9-carboxylic acid tert-butyl ester: starting from the product obtained in step 3 and following the experimental procedure described in step 4 of intermediates 19 and 20, The title compound was obtained (as a 1:1 mixture of stereoisomers, 0.775 g, 49% yield).

Step 5. The title compound: A solution of the product obtained in Step 4 (219 mg, 0.64 mmol) and TFA (0.5 mL, 0.725 mmol) in DCM was stirred at r.t. for 3 h. The volatile material was evaporated to dryness to obtain the title compound (as a 1:1 mixture of stereoisomers, 0.347 g, 63 wt%, quantitative yield).

Intermediates 23 and 24. (2 R ,6 R ,7 R )-7-fluoro-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]11 Alkane-3-one trifluoroacetate and (2 R ,6 S ,7 S )-7-fluoro-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro [5.5] Undecane-3-one trifluoroacetate

Following the procedure described in steps 2 to 5 of intermediates 21 and 22, starting from the product obtained in step 1b of intermediates 21 and 22, the title compound (in the form of a 1:1 mixture of stereoisomers, 0.208 g , 81 wt%, quantitative yield).

Synthesis of Examples General Deprotection Method Method 1. Deprotection with TMSI Boc. To a solution of N- Boc protected compound (1 mmol) in anhydrous ACN (45 mL) was added TMSI (2 mmol) dropwise. After stirring at rt for 15 min, a saturated solution of NaHCO ₃ and DCM were added and the mixture was stirred for another 10 minutes. The phases were separated and the organic phase was dried over MgSO ₄ and concentrated to dryness to give the crude compound, which was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)).

Method 2. Deprotect with Boc of TFA. A solution of the N- Boc protected compound (1 mmol) in a mixture of DCM (15 mL) and TFA (10 mmol) was stirred at rt until complete conversion was achieved. The volatile material was evaporated and the residue was redissolved in DCM and washed with 1 M NaOH solution and brine, dried over MgSO ₄ and concentrated. The compound was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)).

Method 3. Deprotection with Boc of HCl. To a solution of N- Boc protected compound (1 mmol) in dioxane (10 mL) was added HCl (4 N solution in dioxane under N ₂ atmosphere, 10 mmol). The reaction was stirred at rt overnight. The solvent was evaporated and the residue was purified by leaching through an acid ion exchange resin column (SCX) to produce the desired compound, which was further purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)) .

Method 4. Deprotect with CsF Teoc. A solution of N- Teoc protected compound (1 mmol) and cesium fluoride (5 mmol) in DMF (26 mL) was heated at 90°C for 1 h. The solvent was concentrated to dryness and the crude product was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)).

Example 1: N -methyl-3-(2-(12-methyl-4-oxa-8,12-diazabispiro[2.1.5.3]tridecane-8-yl)phenoxy) -3-phenylpropan-1-amine

Step 1. Methyl (3-(2-(12-methyl-4-oxa-8,12-diazabispiro[2.1.5.3]tridecane-8-yl)phenoxy)-3 -Phenylpropyl)carbamic acid tert-butyl ester: In a schlenk tube, the intermediate 8 (193 mg, 0.46 mmol), 12-methyl-4-oxa-8,12 -Diazabisspiro[2.1.5.3]tridecane (prepared according to WO2017084752, 82 mg, 0.42 mmol), Pd ₂ (dba) ₃ (19 mg, 0.021 mmol), BINAP (26 mg, 0.042 mmol) and Potassium tributoxide (84 mg, 0.75 mmol) was mixed in toluene (1.6 mL). The reaction was purged by bubbling argon through the solution for 5 min and heated at 100 °C overnight. However, it was filtered through a pad of diatomaceous earth, which was washed with EtOAc. The filtrate was concentrated to dryness and the residue was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)) to give the title compound (75 mg, 34% yield).

Step 2. The title compound: Starting from the compound obtained in Step 1 (75 mg, 0.14 mmol) and following the general deprotection method 1, the title compound (20 mg, 33% yield) was obtained.

HPLC residence time (Method A): 4.76 min; MS: 436.2 (M+H).

This method is used to prepare Examples 2-5 using suitable starting materials:

Example 6: 12-isopropyl-8-(2-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-4-oxa-8,12 -Diazabispiro[2.1.5.3]tridecane-13-one

Step 1. 8-(2-(3-chloro-1-(thien-2-yl)propoxy)benzyl)-12-isopropyl-4-oxa-8,12-diazepine spiro [2.1.5.3] tridecane-13-one: at rt under an atmosphere of N ₂ intermediate 5 (150 mg, 0.53 mmol) , 12- isopropyl-4-oxa-8,12-two A solution of azabispiro[2.1.5.3]tridecane-13-one (prepared according to WO2017084752, 127 mg, 0.50 mmol) and DIPEA (0.37 mL, 2.14 mmol) in DCE (1.5 mL) was stirred for 30 min. Then, sodium triethoxyborohydride (282 mg, 1.07 mmol) was added and the reaction mixture was stirred at rt overnight. A saturated solution of NaHCO _{3 was} added and it was extracted with DCM. The combined organic phase was washed with brine, dried over MgSO ₄ and concentrated to dryness to give the crude product, which was used without further purification (319 mg, overweight, assumed quantitative yield).

Step 2. The title compound: In a sealed tube, place a solution of the compound obtained in Step 1 (319 mg, 84 wt%, 0.53 mmol) and methylamine (33 wt% solution in EtOH, 1 mL, 26.7 mmol) in Heat at 100°C overnight. The solvent was evaporated to dryness, the residue was dissolved in DCM and it was washed with 1 N aqueous NaOH. The organic phase was dried over MgSO ₄ , filtered and concentrated to dryness. The crude product was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)) to give the title compound (64 mg, 24% yield).

HPLC residence time (Method B): 4.23 min; MS: 498.2 (M+H).

This method is used to prepare Example 7 using suitable starting materials:

Example 8: ( R )-4-isopropyl-2-methyl-9-(2-(( S )-3-(methylamino)-1-(thiophen-2-yl)propoxy) Phenethyl)-1-oxa-4,9-diazaspiro[5.5]undecane-3-one

Step 1. (( S )-3-(2-(2-((( R )-4-isopropyl-2-methyl-3- pendoxy-1-oxa-4,9-diaza Spiro[5.5]undec-9-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)aminocarboxylic acid 2-(trimethylsilyl)ethyl Ester: follow the experimental procedure described in Step 1 of Example 6, from Intermediate 10 (103 mg, 0.238 mmol) and ( R )-4-isopropyl-2-methyl-1-oxa-4,9 -Starting from diazaspiro[5.5]undec-3-one trifluoroacetate (prepared according to WO2017084752, 81 mg, 0.238 mmol), the title compound (45 mg, 29% yield) was obtained.

Step 2. The title compound: Starting from the compound obtained in Step 1 (45 mg, 0.07 mmol) and following general deprotection method 4, the title compound (13 mg, 37% yield) was obtained.

HPLC residence time (Method B): 4.46 min; MS: 499.9 (M+H).

This method is used to prepare Examples 9-22 using suitable starting materials:

Example 23: (12-isopropyl-4-oxa-8,12-diazabispiro[2.1.5.3]tridecane-8-yl)(2-(3-(methylamino)- 1-phenylpropoxy)phenyl)methanone

Step 1. (3-(2-(12-Isopropyl-4-oxa-8,12-diazabispiro[2.1.5 ⁵ .3 ³ ]tridecane-8-carbonyl)phenoxy )-3-phenylpropyl)(methyl)carbamic acid tert-butyl ester: intermediate 13 (150 mg, 0.39 mmol) and 12-isopropyl-4-oxa-8,12-diazepine Heterobispiro[2.1.5.3]tridecane (prepared according to WO2017084752, 87 mg, 0.39 mmol) in anhydrous DMF (5 mL) was added DIPEA (0.20 mL, 1.17 mmol) and HATU (148 mg, 0.39 mmol) ) And the reaction mixture was stirred at rt overnight. A saturated solution of NaHCO _{3 was} added and it was extracted with EtOAc. The combined organic phase was washed with water and brine, dried over MgSO ₄ and concentrated to dryness. The crude product was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)) to give the title compound (158 mg, 69% yield).

Step 2. The title compound: Starting from the compound obtained in Step 1 (158 mg, 0.27 mmol) and following general deprotection method 3, the title compound (55 mg, 42% yield) was obtained.

HPLC residence time (Method A): 4.38 min; MS: 492.3 (M+H).

This method is used to prepare examples 24-25 using suitable starting materials:

Follow for example 8 The method described in the synthesis, the use of suitable intermediates aldehydes and amines ( according to WO2017084752 , WO2015185209 , WO2015185208 and WO2015185207 preparation ) , Preparation Example 26-41 :

Examples 42 and 43: ( R )-4-isopropyl-2-methyl-9-(( S )-1-(2-(( R )-3-(methylamino)-1--1-thiophene -2-yl)propoxy)phenyl)prop-2-yl)-1-oxa-4,9-diazaspiro[5.5]undecane-3-one and ( R )-4-iso Propyl-2-methyl-9-(( R )-1-(2-(( R )-3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl) Propan-2-yl)-1-oxa-4,9-diazaspiro[5.5]undecane-3-one

Step 1. (( R )-3-(2-(( S )-2-(( R )-4-isopropyl-2-methyl-3-oxo-1-oxa-4,9 -Diazaspiro[5.5]undec-9-yl)propyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)aminocarboxylic acid 2-(trimethylsilicon Group) ethyl ester and (( R )-3-(2-(( R )-2-(( R )-4-isopropyl-2-methyl-3- pendoxy-1-oxa- 4,9-diazaspiro[5.5]undec-9-yl)propyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)aminocarboxylic acid 2-(tri Methylsilyl) ethyl ester: A mixture of intermediate 18 (139 mg, 0.3 mmol) and titanium(IV) isopropoxide (0.91 mL, 0.883 mmol) was heated at 65°C for 6 h. Then, a solution of sodium cyanoborohydride (171 mg, 2.72 mmol) in EtOH (3 mL) was added dropwise and the reaction mixture was stirred at 60 °C overnight. The solvent was evaporated and the residue was partitioned between saturated NaHCO ₃ solution and DCM. The aqueous phase was extracted with DCM and the combined organic extracts were washed with brine, dried over MgSO ₄ and concentrated to dryness. The residue was purified by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)) to give the title compound (128 mg, 63% yield) as a 1:1 mixture.

Step 2. The title compound: Starting from the compound obtained in Step 1 (128 mg, 0.195 mmol) and following the general deprotection method 4, the title compound was obtained as a 1:1 mixture (68 mg, 68% yield). Then perform chiral preparative HPLC separation (column: Chiralpak IA; temperature: ambient temperature; flow rate: 12 mL/min; eluent: n-heptane/(EtOH + 0.3% DEA) 80/20 v/v) to The title compound is produced.

Example 42 (35 mg) HPLC residence time (Method B): 4.61 min; MS: 514.3 (M+H).

Example 43 (23 mg) HPLC residence time (Method B): 4.71 min; MS: 514.3 (M+H).

Examples 44 and 45: (2 R ,6 R ,7 S )-7-fluoro-4-isopropyl-2-methyl-9-(2-(( R )-3-(methylamino)- 1-(thiophen-2-yl)propoxy)phenethyl)-1-oxa-4,9-diazaspiro[5.5]undecane-3-one and (2 R ,6 S ,7 R )-7-fluoro-4-isopropyl-2-methyl-9-(2-(( R )-3-(methylamino)-1-(thiophen-2-yl)propoxy) Phenethyl)-1-oxa-4,9-diazaspiro[5.5]undecane-3-one

Step 1. (( R )-3-(2-(2-((2 R ,6 R ,7 S )-7-fluoro-4-isopropyl-2-methyl-3-oxo-1 -Oxa-4,9-diazaspiro[5.5]undec-9-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)aminocarboxylic acid 2-(Trimethylsilyl) ethyl ester and (( R )-3-(2-(2-((2 R ,6 S ,7 R )-7-fluoro-4-isopropyl-2- Methyl-3-oxo-1-oxa-4,9-diazaspiro[5.5]undec-9-yl)ethyl)phenoxy)-3-(thiophen-2-yl) Propyl)(methyl)carbamic acid 2-(trimethylsilyl)ethyl ester: follow the experimental procedure described in step 1 of Example 8, intermediates 21 and 22 from intermediate 9 and 1:1 Starting with the mixture, the title compound was obtained as a 1:1 mixture (225 mg, 55% yield).

Step 2. The title compound: Starting from the compound obtained in Step 1 (255 mg, 0.340 mmol) and following general deprotection method 4, the title compound was obtained as a 1:1 mixture (104 mg, 98% yield). Then perform chiral preparative HPLC separation (column: Chiralpak IA; temperature: ambient temperature; flow rate: 12 mL/min; eluent: n-heptane/(EtOH + 0.3% DEA) 60/40 v/v) The title compound is produced.

Example 44 (39 mg) HPLC residence time (Method B): 4.75 min; MS: 518.2 (M+H).

Example 45 (28 mg) HPLC residence time (Method B): 4.67 min; MS: 518.2 (M+H).

Examples 46 and 47 : (2 R ,6 S ,7 S )-7- fluoro- 4- isopropyl- 2- methyl -9-(2-(( R )-3-( methylamino )- 1-( thiophen -2- yl ) propoxy ) phenethyl )-1 -oxa -4,9 -diazaspiro [5.5] undecane- 3 -one and (2 R ,6 R ,7 R )-7- fluoro- 4- isopropyl- 2- methyl -9-(2-(( R )-3-( methylamino )-1-( thiophen -2- yl ) propoxy ) Phenethyl )-1 -oxa -4,9 -diazaspiro [5.5] undecane- 3 -one

Step 1. (( R )-3-(2-(2-((2 R ,6 S ,7 S )-7-fluoro-4-isopropyl-2-methyl-3-oxo-1 -Oxa-4,9-diazaspiro[5.5]undec-9-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)aminocarboxylic acid 2-(Trimethylsilyl) ethyl ester and (( R )-3-(2-(2-((2 R ,6 R ,7 R )-7-fluoro-4-isopropyl-2- Methyl-3-oxo-1-oxa-4,9-diazaspiro[5.5]undec-9-yl)ethyl)phenoxy)-3-(thiophen-2-yl) Propyl)(methyl)aminocarboxylic acid 2-(trimethylsilyl)ethyl ester: follow the experimental procedure described in Step 1 of Example 8, from Intermediate 9 and Intermediate 23 and 24 from 1:1 Starting with the mixture, the title compound was obtained as a 1:1 mixture (136 mg, 58% yield).

Step 2. The title compound: starting from the compound obtained in Step 1 (135 mg, 0.205 mmol) and following general deprotection method 4, the title compound (68 mg, 64% yield) was obtained in the form of a 1:1 mixture. Then perform achiral preparative HPLC separation (column: Chiralpak IA; temperature: ambient temperature; flow rate; 18 mL/min; eluent: n-heptane/(EtOH + 0.3% DEA) 50/50 v/v) This gave the title compound.

Example 46 (3 mg) HPLC residence time (Method B): 4.68 min; MS: 518.2 (M+H).

Example 47 (18 mg) HPLC residence time (Method B): 4.81 min; MS: 518.2 (M+H).

Table of examples of α ₂ δ-1 subunits bound to µ -opioid receptors and voltage-gated calcium channels : biologically active pharmacokinetic studies Ca _v 2.2 human α ₂ δ-1 subunits for calcium channel analysis will Human α ₂ δ-1 enriched membrane (2.5 µg) was incubated with 15 nM radiolabeled [3H]-gabapentin in analysis buffer containing Hepes-KOH 10mM (pH 7.4). NSB (non-specific binding) was measured by adding 10 µM pregabalin. The combination of test compounds was measured at 5 different concentrations. After incubation at 27°C for 60 min, the binding reaction was terminated by filtration through Multiscreen GF/C (Millipore) pre-soaked in 0.5% polyethyleneimine in a vacuum manifold station, followed by a solution containing 50 mM Tris-HCl ( Wash with ice-cold filter buffer pH 7.4) 3 times. The filter plate was dried at 60°C for 1 hour and 30 µl of scintillation mix was added to each well, after which the radioactivity was read. The reading was carried out in a Trilux 1450 Microbeta radioactivity counter (Perkin Elmer).

Human μ - opioid receptor radioligand analysis Transfected CHO-K1 cell membrane (20 μg) together with [ ³ H]-DAMGO (1 nM) in assay buffer containing Tris-HCl 50 mM, MgCl ₂ 5 mM The solution was incubated at pH 7.4. NBS (non-specific binding) was measured by adding 10 μM Naloxone. The combination of test compounds was measured at 5 different concentrations. The plate was incubated at 27°C for 60 min. After the incubation period, the reaction mixture was then transferred to MultiScreen HTS, FC plates (Millipore), filtered and the plates were washed 3 times with ice-cold 10 mM Tris-HCl (pH 7.4). The filter was dried and counted at about 40% efficiency using EcoScint liquid scintillation mix on a MicroBeta scintillation counter (Perkin-Elmer).

Results : Since the present invention aims to provide a compound which is used as a double ligand of the voltage-gated calcium channel and a dual ligand of the α ₂ δ subunit and the µ-opioid receptor, or a series of chemically related compounds, it is an excellent embodiment to choose Compounds used as dual ligands of the α ₂ δ subunit of the voltage-gated calcium channel and the µ-opioid receptor and in particular compounds having a binding expressed as K _i corresponding to the following scale: K _i (µ) Best <1000 nM, better <500 nM, even better <100 nM. K _i (α ₂ δ-1) is preferably <10000 nM, more preferably <5000 nM, or even more preferably <500 nM. The following scale has been adopted to indicate binding to µ-opioid receptors, expressed as K _i : + K _i (µ) ＞= 500 nM ++ 100 nM ＜= K _i (µ) ＜ 500 nM +++ K _i (µ) ＜ 100 nM The following scale has been adopted to indicate the combination with the α ₂ δ-1 subunit of the voltage-gated calcium channel, expressed as K _i : + K _i (α ₂ δ-1) >= 5000 nM ++ 500nM ＜= K _i (α ₂ δ-1) ＜5000 nM +++ K _i (α ₂ δ-1) ＜500 nM All compounds prepared in this application exhibit voltage-gated calcium channels The binding of the α ₂ δ-1 subunit and the µ-opioid receptor specifically shows the following binding results:

Claims (13)

A compound of general formula (I),

Where X is selected from bond, -[C(R _a R _b )] _p -, -[CH ₂ ] _p C(O)[CH ₂ ] _q -, -[CH ₂ ] _p C(O)N(R _z )[CH ₂ ] _q -, -[CH ₂ ] _p N(R _z )C(O)[CH ₂ ] _q -and -[CH ₂ ] _p N(R _z )[CH ₂ ] _q -; R _a Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _b Selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; or, R _a and R _b together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{z is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C(O) -C _1-6 alkyl; p is 0, ₁ , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; n is 0 or 1; Y ₁ is -C(R ₁₀ R _10' )-; wherein R ₁₀ and R _{10' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or Unsubstituted C _2-6 alkynyl; alternatively, R ₁₀ and R _10' together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; Y ₂ is -C(R _10'' R _10''')-; wherein R _10'' and R _{10''' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and Substituted or unsubstituted C _2-6 alkynyl; alternatively, R _10″ and R _10″′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R ₁ is

; Where m is 0, 1 or 2; r is 0, 1 or 2; Y is -CH ₂ -or C=O; R _{5 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkyl cycloalkyl ; R _5'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; Alternatively, R ₅ and R _5′ together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R _{6 is} selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted Substituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted Or unsubstituted aryl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclic, substituted or unsubstituted alkyl heterocyclic and -C(O)R ₇ ; R _{7 is} selected from substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted Or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted Heterocyclic group, substituted or unsubstituted alkyl heterocyclic group; R _{8 is} selected from hydrogen, halogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _{2- 6} alkenyl group, a substituted or unsubstituted C _2-6 alkynyl group and the -OR _81; R _{8 'is} selected from hydrogen, substituted or unsubstituted alkyl group of C _1-6, substituted or non-substituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl; R _{2 is} selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclic; R _{3 is} selected from Hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 alkenyl, substituted or unsubstituted C _2-6 alkynyl, substituted or unsubstituted Cycloalkyl and substituted or unsubstituted alkylcycloalkyl; R _3'is selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl and substituted or unsubstituted C _2-6 alkynyl; R ₄ and R _{4 'are} independently selected from halogen, -R ₄₁ , -OR ₄₁ , -NO ₂ , -NR ₄₁ R _41' , -NR ₄₁ C(O)R _41' , -NR ₄₁ S(O) ₂ R _41' , -S(O) ₂ NR ₄₁ R _41' , -NR ₄₁ C(O)NR _41' R _41'' , -SR ₄₁ , -S(O)R ₄₁ , -S(O) ₂ R ₄₁ , -CN, haloalkyl, halo Alkoxy, -C(O)OR ₄₁ , -C(O)NR ₄₁ R _41' , -OCH ₂ CH ₂ OR ₄₁ , -NR ₄₁ S(O) ₂ NR _41' R _41'' and -C( CH ₃ ) ₂ OR ₄₁ ; wherein R ₄₁ , R _41' and R _{41'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, substituted or unsubstituted C _2-6 Alkenyl, substituted or unsubstituted C _2-6 alkynyl, and substituted or unsubstituted cycloalkyl; optionally in stereoisomers, preferably mirror isomers or diastereomers One, in the form of a racemate, or in the form of a mixture of stereoisomers, preferably mirror isomers, and/or diastereoisomers in any mixing ratio, or a corresponding salt thereof, or Its corresponding solvate. The compound according to claim 1, wherein R ₂ is a substituted or unsubstituted group selected from phenyl and thienyl. A compound according to any one of claims 1 or 2, wherein the compound of formula (I) is of formula (I'), (I ^a ), (I ^a '), (I ^b ), (I ^b' ), ( I ^c ) or (I ^c ') compounds,

Where R ₉ and R _9'are independently selected from halogen, -R ₂₁ , -OR ₂₁ , -NO ₂ , -NR ₂₁ R _21' , -NR ₂₁ C(O)R _21' , -NR ₂₁ S(O) ₂ R _21' , -S(O) ₂ NR ₂₁ R _21' , -NR ₂₁ C(O)NR _21' R _21'' , -SR ₂₁ , -S(O)R ₂₁ , -S(O) ₂ R ₂₁ , -CN, haloalkyl, haloalkoxy, -C(O)OR ₂₁ , -C(O)NR ₂₁ R _21' , -OCH ₂ CH ₂ OR ₂₁ , -NR ₂₁ S(O) ₂ NR _21' R _21'' and -C(CH ₃ ) ₂ OR ₂₁ ; wherein R ₂₁ , R _21' and R _{21'' are} independently selected from hydrogen, substituted or unsubstituted C _1-6 alkyl, Substituted or unsubstituted C _2-6 alkenyl and substituted or unsubstituted C _2-6 alkynyl. The compound according to any one of claims 1 to 3, wherein

Select from

and

; Where p is 0, 1, 2, 3, 4 or 5; q is 0, ₁ , 2, 3, 4 or 5; and R ₁ is as defined in the preceding claim. The compound according to any one of claims 1 to 4, wherein X is a bond, C(O),

-CH ₂ -or -CH ₂ CH ₂ -. The compound according to any one of claims 1 to 5, wherein p is 0, 1, 2, 3, 4 or 5; preferably, p is 0, 1 or 2. The compound according to any one of claims 1 to 5, wherein q is 0, 1, 2, 3, 4 or 5; preferably, q is 0. The compound according to any one of claims 1 to 7, wherein the compound is selected from

or

. A method for preparing a compound of formula (I) according to any one of claims 1 to 8,

a) where X represents a bond, and where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ and n have the meanings as defined in the preceding request, the method includes the formula The compound of (IIa),

Where Q represents chlorine, bromine, iodine or triflate; use the suitable N- containing cyclic reagent of formula (III-1)

Treatment under Buchwald-Hartwig or Ullmann arylation conditions; or b) where -X- represents -[C(R _a R _b )] _p -, and wherein _{R a, R b, R 1} , R 2, R 3, R 3 ', R 4, R 4', Y 1, Y 2 , and n and p have the preceding request meaning as defined in the item, the method comprising The compound of formula (IIb'),

Where r represents 0 to 4; use the N -containing ring reagent of formula (III-1)

Treatment under standard reductive amination conditions; or c) where -X- represents -[C(R _a R _b )] _p -, and where R _a , R _b , R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4′ , Y ₁ , Y ₂ and n and p have the meanings as defined in the preceding claim, the method includes the compound of formula (IIa),

Where Q represents chlorine, bromine, iodine or triflate; treated with organometallic reagent of formula (III-2')

Where M represents a suitable organometallic group, preferably boron or zinc reagent, and p has the meaning as defined in the preceding claim; or d) where -X- represents -[CR _a R _b ] _p C(O)[CH _{2] q} - and q lines 0, and wherein R _a and R _b based hydrogen and wherein _{R 1, R 2, R 3} , R 3 ', R 4, R 4', Y 1, Y 2, n, p , and q has the meaning as defined in the preceding claim, the method includes a compound of formula (IIc'),

Using the N -containing ring reagent of formula (III-1),

Treatment under conventional amidation conditions; or e) where -X- represents -[CR _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -, and where R _a and R _b are hydrogen And where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p and q have the meanings as defined in the preceding request, the method includes formula (VI' ) Compounds,

Where LG represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate (nosylate) or trifluoromethanesulfonate, p, q and Rz have the definitions as defined in the preceding request Meaning; with N -containing ring reagent of formula (III-1),

Treatment under conventional alkylation conditions; or f) where -X- represents -[CR _a R _b ] _p N(R _z )C(O)[CH ₂ ] _q -, and where R _a and R _b are hydrogen And where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , Y ₁ , Y ₂ , n, p, and q have the meanings as defined in the preceding request, the method includes formula (IId' ) Of the amine compound,

Where p and Rz have the meanings as defined in the preceding claim; use the amide-based reagent of formula (III-3)

Treatment under amidation conditions, where Z represents OH or halogen and q has the meaning as defined in the preceding claim; or g) where -X- represents -[CR _a R _b ] _p N(R _z )C(O )[CH ₂ ] _q -, p is 0, and R _a and R _b are hydrogen and R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , Y ₁ , Y ₂ , n , P and q have the meanings as defined in the preceding claim, the method comprises using a compound of formula (IIa),

Where Q represents chlorine, bromine, iodine or trifluoromethanesulfonate; and a carboxamido compound of formula (III-5),

Reaction under Ullmann arylation conditions, where q and Rz have the meanings as defined in the preceding claims; or h) where n is 0, and where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ and Y ₂ have the meanings as defined in the preceding claim, the method comprises using a compound of formula (VIIa), wherein G is OH,

Reaction with alkylating agent of formula (VIII)

Where Z represents a leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate; or i) where n is 0, and where R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ and Y ₂ have the meanings as defined in the preceding claims, the method comprises using a compound of formula (VIIa), wherein G is OH,

With alcohol of formula (VIII), where Z represents OH,

React in the presence of a suitable azo compound; or j) wherein n is 0, and wherein R ₁ , R ₂ , R ₃ , R _3′ , R ₄ , R _4′ , X, Y ₁ and Y ₂ have The meaning as defined in the item, the method comprises using a compound of formula (VIIa), wherein G is halogen,

Alcohol with formula (VIII), where Z represents OH

React in the presence of a strong base; or k) wherein n is 1, and wherein R ₁ , R ₂ , R ₃ , R _3' , R ₄ , R _4' , X, Y ₁ and Y ₂ have the The meaning of the definition, the method includes the use of compounds of formula (VIIb),

React with the agent of formula (VIII),

Where Z represents OH and G represents a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, or alternatively, Z represents a leaving group, such as chlorine , Bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or trifluoromethanesulfonate, and G represents OH. IIa, IIa-LG, IIb, IIb', IIb-LG, IIb'-LG, IIc, IIc', IIc-LG, IIc'-LG, IId, IId', IId-LG, IId'-LG, III- 1. III-2, III'-2, III-3, III-4, III-5, IVa, IVb, IVb', IVc, IVc', IVd, IVd', IVe, IVf, V, VI, VI' , VII, VIIa, VIIb, VIII, VIII-LG, IX, X, X', X-LG, X'-LG, XI, XI-LG, XI' or XI'-LG compounds,

Wherein _{R a, R b, R 1} , R 2, R 3, R 3 ', R 4, R 4', Y 1, Y 2, n, p, q, r , and R _z have the preceding claims, the terms defined Meaning, Q means chlorine, bromine, iodine or triflate, LG means leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, p-nitrobenzenesulfonate or triflate, Has the meaning defined in the specification, M represents a suitable organometallic group, Z represents OH or halogen, and G is OH, halogen or leaving group, such as chlorine, bromine, iodine, methanesulfonate, tosylate, p-nitro Benzenesulfonate or trifluoromethanesulfonate, this compound is used to prepare the compound of formula (I). A pharmaceutical composition comprising the compound of formula (I) according to any one of claims 1 to 8 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle. The compound of formula (I) according to any one of claims 1 to 8 for use as a medicament. The compound of formula (I) according to any one of claims 1 to 8 for use as a medicament; preferably for use in the treatment of pain, especially moderate to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammation Agents for sexual pain, acute pain or neuropathic pain, allodynia or hyperalgesia.