WO2019149919A1

WO2019149919A1 - Aminopropoxypiperidinylamido derivatives having multimodal activity against pain

Info

Publication number: WO2019149919A1
Application number: PCT/EP2019/052568
Authority: WO
Inventors: Marina VIRGILI-BERNADO; Carmen ALMANSA-ROSALES; Monica Alonso-Xalma; Laura OSORIO-PLANES
Original assignee: Esteve Pharmaceuticals, S.A.
Priority date: 2018-02-05
Filing date: 2019-02-04
Publication date: 2019-08-08

Abstract

The present invention relates to aminopropoxyphenylpiperidinylamidoderivatives 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

AMINOPROPOXYPIPERIDINYLAMIDO DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN FIELD OF THE INVENTION The present invention relates to compounds having dual pharmacological activity towards both the α₂ δ ^ ^subunit of the voltage-gated calcium channel, and the µ-opioid receptor (MOR or mu-opioid receptor) and more particularly to aminopropoxyphenylpiperidinylamido derivatives having this pharmacological activity, 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. BACKGROUND OF THE INVENTION The adequate management of pain constitutes an important challenge, since currently available treatments provide in many cases only modest improvements, leaving many patients unrelieved (Turk, D.C., Wilson, H.D., Cahana, A.; 2011; Lancet; 377; 2226- 2235). Pain affects a big portion of the population with an estimated prevalence of 20 % and its incidence, particularly in the case of chronic pain, is increasing due to the population ageing. Additionally, pain is clearly related to comorbidities, such as depression, anxiety and insomnia, which leads to important productivity losses and socio-economical burden (Goldberg, D.S., McGee, S.J.; 2011; BMC Public Health; 11; 770). Existing pain therapies include non-steroidal anti-inflammatory drugs (NSAIDs), opioid agonists, calcium channel blockers and antidepressants, but they are much less than optimal regarding their safety ratio. All of them show limited efficacy and a range of secondary effects that preclude their use, especially in chronic settings. Voltage-gated calcium channels (VGCC) are required for many key functions in the body. Different subtypes of voltage-gated calcium channels have been described (Zamponi et al., Pharmacol Rev.201567:821-70). The VGCC are assembled through interactions of different subunits, namely α1 (Cav α1), β (Cav β) α2 δ (Cavα₂δ) and γ (Cav γ). The α1 subunits are the key porous forming units of the channel complex, being responsible for the Ca²⁺ conduction and generation of Ca²⁺ influx. The α₂ δ, ^, and ^ subunits are auxiliary, although very important for the regulation of the channel, since they increase the expression of the α1 subunits in the plasma membrane as well as modulate their function, resulting in functional diversity in different cell types. Based on their physiological and pharmacological properties, VGCC can be subdivided into low voltage-activated T-type (Cav3.1, Cav3.2, and Cav3.3), and high voltage-activated L- (Cav1.1 through Cav1.4), N-(Cav2.2), P/Q-(Cav2.1), and R-(Cav2.3) types, depending on the channel forming Ca_V α subunits. All of these five subclasses are found in the central and peripheral nervous systems. Regulation of intracellular calcium through activation of these VGCC plays obligatory roles in: 1) neurotransmitter release, 2) membrane depolarization and hyperpolarization, 3) enzyme activation and inactivation, and 4) gene regulation (Perret and Luo, Neurotherapeutics. 20096:679-92; Zamponi et al., 2015 supra; Neumaier et al., Prog Neurobiol.2015 129:1-36.). A large body of data has clearly indicated that VGCC are implicated in mediating various disease states including pain processing. Drugs interacting with the different calcium channel subtypes and subunits have been developed. Current therapeutic agents include drugs targeting L-type Ca_v1.2 calcium channels, particularly 1,4-dihydropyridines, which are widely used in the treatment of hypertension. T-type (Ca_v3) channels are the target of ethosuximide, widely used in absence epilepsy. Ziconotide, a peptide blocker of N-type (Ca_v2.2) calcium channels, has been approved as a treatment of intractable pain. (Perret and Luo, 2009, supra; Vink and Alewood, Br J Pharmacol.2012167:970-89.). The Ca_v1 and Ca_v2 subfamilies contain an auxiliary α₂δ subunit, which is the therapeutic target of the gabapentinoid drugs of value in certain epilepsies and chronic neuropathic pain. To date, there are four known α₂δ subunits, each encoded by a unique gene and all possessing splice variants. Eachα₂δ protein is encoded by a single messenger RNA and is post-translationally cleaved and then linked by disulfide bonds. Four genes encoding α₂δ subunits have now been cloned. α₂δ-1 was initially cloned from skeletal muscle and shows a fairly ubiquitous distribution. The α₂δ-2 and α₂δ-3 subunits were subsequently cloned from brain. The most recently identified subunit, α₂δ-4, is largely non-neuronal. The human α₂δ-4 protein sequence shares 30, 32 and 61% identity with the human α₂δ-1, α₂δ-2 and α₂δ-3 subunits, respectively. The gene structure of all α₂δ subunits is similar. All α₂δ subunits show several splice variants (Davies et al., Trends Pharmacol Sci.200728:220-8.; Dolphin AC, Nat Rev Neurosci. 201213:542-55., Biochim Biophys Acta.20131828:1541-9.). The Cavα₂δ-1 subunit may play an important role in neuropathic pain development (Perret and Luo, 2009, supra; Vink and Alewood, 2012, supra). Biochemical data have indicated a significant Ca_v α₂ δ-1, but not Ca_v α₂ δ-2, subunit upregulation in the spinal dorsal horn, and DRG (dorsal root ganglia) after nerve injury that correlates with neuropathic pain development. In addition, blocking axonal transport of injury-induced DRG Ca_v α₂ δ-1 subunit to the central presynaptic terminals diminishes tactile allodynia in nerve injured animals, suggesting that elevated DRG Ca_v α₂ δ-1 subunit contributes to neuropathic allodynia. The Ca_v α₂ δ-1 subunit (and the Ca_v α₂ δ-2, but not Cavα₂δ-3 and Cavα₂δ-4, subunits) is the binding site for gabapentin which has anti-allodynic/ hyperalgesic properties in patients and animal models. Because injury-induced Ca_v α₂ δ-1 expression correlates with neuropathic pain development and maintenance, and various calcium channels are known to contribute to spinal synaptic neurotransmission and DRG neuron excitability, injury-induced Ca_v α₂ δ-1 subunit upregulation may contribute to the initiation and maintenance of neuropathic pain by altering the properties and/or distribution of VGCC in the subpopulation of DRG neurons and their central terminals, therefore modulating excitability and/or synaptic neuroplasticity in the dorsal horn. Intrathecal antisense oligonucleotides against the Ca_v α₂ δ-1 subunit can block nerve injury-induced Ca_v α₂ δ-1 upregulation and prevent the onset of allodynia and reserve established allodynia. As mentioned above, the α₂δ subunits of VGCC form the binding site for gabapentin and pregabalin, which are structural derivatives of the inhibitory neurotransmitter GABA although they do not bind to GABAA, GABAB, or benzodiazepine receptors, or alter GABA regulation in animal brain preparations. The binding of gabapentin and pregabalin to the Cavα₂δ subunit results in a reduction in the calcium-dependent release of multiple neurotransmitters, leading to efficacy and tolerability for neuropathic pain management. Gabapentinoids may also reduce excitability by inhibiting synaptogenesis (Perret and Luo, 2009, supra; Vink and Alewood, 2012, supra, Zamponi et al., 2015, supra). As mentioned before, there are few available therapeutic classes for the treatment of pain, and opioids are among the most effective, especially when addressing severe pain states. They act through three different types of opioid receptors (mu, kappa and gamma) which are transmembrane G-protein coupled receptors (GPCRs). Still, the main analgesic action is attributed to the activation of the 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, emesis and physical dependence [Meldrum, M.L. (Ed.). Opioids and Pain Relief: A Historical Perspective. Progress in Pain Research and Management, Vol 25. IASP Press, Seattle, 2003]. Additionally, MOR agonists are not optimal for the treatment of chronic pain as indicated by the diminished effectiveness of morphine against chronic pain conditions. This is especially proven for the chronic pain conditions of neuropathic or inflammatory origin, in comparison to its high potency against acute pain. The finding that chronic pain can lead to MOR down-regulation may offer a molecular basis for the relative lack of efficacy of morphine in long-term treatment settings [Dickenson, A.H., Suzuki, R. Opioids in neuropathic pain: Clues from animal studies. Eur J Pain 9, 113-6 (2005)]. Moreover, prolonged treatment with morphine may result in tolerance to its analgesic effects, most likely due to treatment-induced MOR down-regulation, internalization and other regulatory mechanisms. As a consequence, long-term treatment can result in substantial increases in dosing in order to maintain a clinically satisfactory pain relief, but the narrow therapeutic window of MOR agonists finally results in unacceptable side effects and poor patient compliance. Polypharmacology is a phenomenon in which a drug binds multiple rather than a single target with significant affinity. The effect of polypharmacology 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 subsets of targets; binding to some targets may have no effect. Multi-component drugs or multi-targeting drugs can overcome toxicity and other side effects associated with high doses of single drugs by countering biological compensation, allowing reduced dosage of each compound or accessing context-specific multitarget mechanisms. Because multitarget mechanisms require their targets to be available for coordinated action, one would expect synergies to occur in a narrower range of cellular phenotypes given differential expression of the drug targets than would the activities of single agents. In fact, it has been experimentally demonstrated that synergistic drug combinations are generally more specific to particular cellular contexts than are single agent activities, such selectivity is achieved through differential expression of the drugs’ targets in cell types associated with therapeutic, but not toxic, effects (Lehar et al., Nat Biotechnol 2009; 27: 659–666.). In the case of chronic pain, which is a multifactorial disease, multi-targeting drugs may produce concerted pharmacological intervention of multiple targets and signaling pathways that drive pain. Because they actually make use of biological complexity, multi-targeting (or multi-component drugs) approaches are among the most promising avenues toward treating multifactorial diseases such as pain (Gilron et al., Lancet Neurol.2013 Nov;12(11):1084-95.). In fact, positive synergistic interaction for several compounds, including analgesics, has been described (Schröder et al., J Pharmacol Exp Ther.2011; 337:312-20. Erratum in: J Pharmacol Exp Ther.2012; 342:232.; Zhang et al., Cell Death Dis.2014; 5:e1138.; Gilron et al., 2013, supra). Given the significant differences in pharmacokinetics, metabolisms and bioavailability, reformulation of drug combinations (multi-component drugs) is challenging. Further, two drugs that are generally safe when dosed individually cannot be assumed to be safe in combination. In addition to the possibility of adverse drug-drug interactions, if the theory of network pharmacology indicates that an effect on phenotype may derive from hitting multiple targets, then that combined phenotypic perturbation may be efficacious or deleterious. The major challenge to both drug combination strategies is the regulatory requirement for each individual drug to be shown to be safe as an individual agent and in combination (Hopkins, Nat Chem Biol.2008; 4:682-90.). An alternative strategy for multitarget therapy is to design a single compound with selective polypharmacology (multi-targeting drug). It has been shown that many approved drugs act on multiple targets. Dosing with a single compound may have advantages over a drug combination in terms of equitable pharmacokinetics and biodistribution. Indeed, troughs in drug exposure due to incompatible pharmacokinetics between components of a combination therapy may create a low-dose window of opportunity where a reduced selection pressure can lead to drug resistance. In terms of drug registration, approval of a single compound acting on multiple targets faces significantly lower regulatory barriers than approval of a combination of new drugs (Hopkins, 2008, supra). Thus, the present application, relates to the advantages of having dual activity, for μ- receptor and the ^2 ^-1 subunit of voltage-gated calcium channels, in the same molecule to treat chronic pain. In this way, the present invention relates to compounds having a complementary dual mechanism of action ( μ-receptor agonist and blocker of the α₂δ subunit, in particular the α₂δ-1 subunit, of voltage-gated calcium channels) which implies a better profile of tolerability than the strong opioids (morphine, oxycodone, fentanyl etc) and/or better efficacy and tolerability than gabapentinoids (pregabalin and gabapentin). Pain is multimodal in nature, since in nearly all pain states several mediators, signaling pathways and molecular mechanisms are implicated. Consequently, monomodal therapies fail to provide complete pain relief. Currently, combining existing therapies is a common clinical practice and many efforts are directed to assess the best combination of available drugs in clinical studies (Mao, J., Gold, M.S., Backonja, M.; 2011; J. Pain; 12; 157-166). Accordingly, there is still a need to find compounds that have an alternative or improved pharmacological activity in the treatment of pain, being both effective and showing the desired selectivity, and having good“drugability” properties, i.e. good pharmaceutical properties related to administration, distribution, metabolism and excretion. The authors of the present invention, have found a serie of compounds that show dual pharmacological activity towards both the α₂δ subunits, in particular the α₂δ-1 subunit, of the voltage-gated calcium channel, and the µ-opioid receptor (MOR or mu-opioid receptor) resulting in an innovative, effective and alternative solution for the treatment of pain. In view of the existing results of the currently available therapies and clinical practices, the present invention offers a solution by combining in a single compound binding to two different targets relevant for the treatment of pain. This was mainly achieved by providing the compounds according to the invention that bind both to the µ-opioid receptor and to the α₂δ subunits, in particular the α₂δ-1 subunit, of the voltage-gated calcium channel.

SUMMARY OF THE INVENTION In this invention a family of structurally distinct aminopropoxyphenylpiperidinylamidoderivatives, encompassed by formula (I), which have a dual pharmacological activity towards both theα₂δ subunits, in particular theα₂δ- 1 subunit, of the voltage-gated calcium channel, and the µ-opioid receptor, was identified thus solving the above problem of identifying alternative or improved pain treatments by offering such dual compounds. The main object of the invention is directed to a compound having a dual activity binding to the α₂δ subunit, in particular the α₂δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor for use in the treatment of pain.

As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of theα₂δ subunits, in particular theα₂δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor it is a very preferred embodiment if the compound has a binding expressed as Ki responding to the following scales:

K_i(µ) is preferably < 1000 nM, more preferably < 500 nM, even more preferably < 100 nM.

K_i(α₂δ-1) is preferably < 10000 nM, more preferably < 5000 nM, even more preferably < 500 nM or even more preferably < 100 nM.

The invention is directed in a main aspect to a compound of general Formula (I),

wherein R1, R2, R3, R3’, R4, R4’, X, Y1, Y2 and n are as defined below in the detailed description. A further object of the invention refers to the processes for preparation of compounds of general formula (I). A still further object of the invention refers to the use of intermediate compounds for the preparation of a compound of general formula (I). It is also an object of the invention a pharmaceutical composition comprising a compound of formula (I). Finally, it is an object of the invention the use of compound as a medicament and more particularly for the treatment of pain and pain related conditions.

DETAILED DESCRIPTION OF THE INVENTION In this invention a family of structurally distinct aminopropoxyphenylpiperidinylamido derivatives, encompassed by formula (I), which have a dual pharmacological activity towards both the α₂δ subunits, in particular the α₂δ-1 subunit, of the voltage-gated calcium channel, and the µ-opioid receptor was identified, thus solving the above problem of identifying alternative or improved pain treatments by offering such dual compounds. The main object of the invention is directed to a compound having a dual activity binding to the α₂δ subunit, in particular the α₂δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor, for use in the treatment of pain.

As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of theα₂δ subunits, in particular theα₂δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor, it is a very preferred embodiment if the compound has a binding expressed as K_i responding to the following scales:

Ki(α₂δ-1) is preferably < 10000 nM, more preferably < 5000 nM, even more preferably < 500 nM or even more preferably < 100 nM.

The applicant has surprisingly found that the problem of providing a new effective and alternative for treating pain and pain related disorders can be solved by using a multimodal balanced analgesic approach combining two different synergistic activities in a single drug (i.e., dual ligands which are bifunctional and bind to µ-opioid receptor and to α₂δ subunit, in particular the α₂δ-1 subunit, of the voltage-gated calcium channel), thereby enhancing through the α₂δ blockade without increasing the undesirable side effects. This supports the therapeutic value of a dual agent, whereby the ^2 ^ binding component acts as an intrinsic adjuvant of the MOR binding component. A dual compound that possess binding to both the µ-opioid receptor and to the ^2 ^ subunit of the voltage-gated calcium channel shows a highly valuable therapeutic potential by achieving an outstanding analgesia (enhanced in respect to the potency of the opioid component alone) with a reduced side-effect profile (safety margin increased compared to that of the opioid component alone) versus existing opioid therapies. Advantageously, the dual compounds according to the present invention would in addition show one or more the following functionalities: blockade of the ^2 ^ subunit, in particular the ^2 ^-1 subunit, of the voltage-gated calcium channel and µ-opioid receptor agonism It has to be noted, though, that functionalities“antagonism” and“agonism” are also sub- divided in their effect into subfunctionalities like partial agonism or inverse agonism. Accordingly, the functionalities of the compound should be considered within a relatively broad bandwidth. An antagonist blocks or dampens agonist-mediated responses. Known subfunctionalities are neutral antagonists or inverse agonists. An agonist increases the activity of the receptor above its basal level. Known subfunctionalities are full agonists, or partial agonists. In addition, the two mechanisms complement each other since MOR agonists are only marginally effective in the treatment of neuropathic pain, while the blockers of the α₂δ subunit, in particular the α₂δ-1 subunit, of voltage-gated calcium channels show outstanding effects in preclinical neuropathic pain models. Thus, the α₂δ component, in particular the ^2 ^-1 component, adds unique analgesic actions in opioid-resistant pain. Finally, the dual approach has clear advantages over MOR agonists in the treatment of chronic pain as lower and better tolerated doses would be needed based on the potentiation of analgesia but not of the adverse events of MOR agonists. A further advantage of using designed multiple ligands is a lower risk of drug-drug interactions compared to cocktails or multi-component drugs, thus involving simpler pharmacokinetics and less variability among patients. Additionally, this approach may improve patient compliance and broaden the therapeutic application in relation to monomechanistic drugs, by addressing more complex aetiologies. It is also seen as a way of improving the R&D output obtained using the“one drug-one target” approach, which has been questioned over the last 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)].

In its broader aspect, the present invention is directed to compounds of general Formula (I):

wherein

X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-; R_a is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R_b is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Ra and Rb, taken 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; Y₁ is–C(R₁₀R_10’)-; wherein R₁₀ and R_10’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R10 and R10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y₂ is–C(R_10’’R_10’’’)-; wherein R10’’ and R10’’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R_10’’ and R_10’’’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

R1 is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R₅, R_5’, R_5’’ and R_5’’’ are independently 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, R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

R₆, R_6’, R_6’’ and R_6’’’ are independently 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, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; R₇ is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR71; wherein R₇₁ 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;

R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, - NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein R82 and R82’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

alternatively, R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea;

R2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; R3’ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR₄₁S(O)₂NR_41’R_41’’ and -C(CH₃)₂OR₄₁; wherein R₄₁, R_41’ and R_41’’ 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; These compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another embodiment, these compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof.

In a further embodiment the compound according to the invention is a compound of general Formula (I)

wherein X is selected from a bond, -[C(RaRb)]p-, -[CH2]pC(O)[CH2]q-, -[CH2]pC(O)N(Rz)[CH2]q-, - [CH2]pN(Rz)C(O)[CH2]q- and -[CH2]pN(Rz)[CH2]q-; Ra is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 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, taken 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; Y1 is–C(R10R10’)-; wherein R10 and R10’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R₁₀ and R_10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y₂ 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’’’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

R₁ is

wherein m is 0, 1 or 2; r is 0, 1 or 2; R5, R5’, R5’’ and R5’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R5 and R5’ and/or R5’’ and R5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

wherein the alkyl, alkenyl or alkynyl defined in R₅, R_5’ R_5’’ and R_5’’’, if substituted, it is substituted with one or more substituent/s selected from–OR₅₁, halogen, - CN, haloalkyl, haloalkoxy and–NR₅₁R_51’;

wherein the cycloalkyl, as defined in R₅-R_5’ and/or R_5’’-R_5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₅₁, -OR₅₁, -NO₂, -NR₅₁R_51’, -NR₅₁C(O)R_51’, -NR₅₁S(O)₂R_51’, -S(O)₂NR₅₁R_51’, - NR₅₁C(O)NR_51’R_51’’, -SR₅₁, -S(O)R₅₁, -S(O)₂R₅₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₅₁, -C(O)NR₅₁R_51’, -OCH₂CH₂OR₅₁, - NR₅₁S(O)₂NR_51’R_51’’ and -C(CH₃)₂OR₅₁; preferably selected from halogen, - R₅₁, -OR₅₁, -NR₅₁R_51’, -CN, haloalkyl and haloalkoxy;

wherein R₅₁, R_51’ and R_51’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R6, R6’, R6’’ and R6’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R6, R6’ R6’’ and R6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR₆₁, halogen, - CN, haloalkyl, haloalkoxy and–NR₆₁R_61’;

wherein the cycloalkyl, as defined in R₆-R_6’ and/or R_6’’-R_6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₆₁, -OR₆₁, -NO₂, -NR₆₁R_61’, -NR₆₁C(O)R_61’, -NR₆₁S(O)₂R_61’, -S(O)₂NR₆₁R_61’, - NR₆₁C(O)NR_61’R_61’’, -SR₆₁, -S(O)R₆₁, -S(O)₂R₆₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₆₁, -C(O)NR₆₁R_61’, -OCH₂CH₂OR₆₁, - NR₆₁S(O)₂NR_61’R_61’’ and -C(CH₃)₂OR₆₁; preferably selected from halogen, - R₆₁, -OR₆₁, -NR₆₁R_61’, -CN, haloalkyl and haloalkoxy; wherein R₆₁, 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;

R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR71; wherein the alkyl, alkenyl or alkynyl defined in R₇, if substituted, it is substituted with one or more substituent/s selected from–OR71, halogen, -CN, haloalkyl, haloalkoxy and–NR71R71’; the aryl, heterocyclyl or cycloalkyl in R₇, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₇₁, -OR₇₁, -NO₂, - NR₇₁R_71’, -NR₇₁C(O)R_71’, -NR₇₁S(O)₂R_71’, -S(O)₂NR₇₁R_71’, - NR₇₁C(O)NR_71’R_71’’, -SR₇₁, -S(O)R₇₁, -S(O)₂R₇₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₇₁, -C(O)NR₇₁R_71’, -OCH₂CH₂OR₇₁, -NR₇₁S(O)₂NR_71’R_71’’ and - C(CH₃)₂OR₇₁; wherein R₇₁, 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;

R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; wherein the aryl and heterocyclyl, as defined in R₈, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R81, -OR81, -NO2, -NR81R81’, -NR81C(O)R81’, - NR81S(O)2R81’, -S(O)2NR81R81’, - NR81C(O)NR81’R81’’, -SR81, -S(O)R81, - S(O)2R81, –CN, haloalkyl, haloalkoxy, -C(O)OR81, -C(O)NR81R81’, - OCH2CH2OR81, -NR81S(O)2NR81’R81’’ and -C(CH3)2OR81; wherein R81, R81’ and R81’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, - NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the alkyl, alkenyl or alkynyl defined in R8’, if substituted, it is substituted with one or more substituent/s selected from–OR₈₂, halogen, -CN, haloalkyl, haloalkoxy and–NR₈₂R_82’;

wherein the cycloalkyl, aryl and heterocyclyl, as defined in R_8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₂, -OR₈₂, -NO₂, -NR₈₂R_82’, -NR₈₂C(O)R_82’, - NR₈₂S(O)₂R_82’, -S(O)₂NR₈₂R_82’, - NR₈₂C(O)NR_82’R_82’’, -SR₈₂, -S(O)R₈₂, - S(O)₂R₈₂, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₂, -C(O)NR₈₂R_82’, - OCH₂CH₂OR₈₂, -NR₈₂S(O)₂NR_82’R_82’’ and -C(CH₃)₂OR₈₂; wherein R₈₂, R_82’ and R_82’’ 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, R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; wherein the cyclic amide or cyclic urea, as defined in R8-R8’ when taken together with the–N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R83, -OR83, -NO2, -NR83R83’, -NR83C(O)R83’, -NR83S(O)2R83’, -S(O)2NR83R83’, - NR83C(O)NR83’R83’’, -SR83, -S(O)R83, -S(O)2R83,–CN, haloalkyl, haloalkoxy, -C(O)OR83, -C(O)NR83R83’, -OCH2CH2OR83, -NR83S(O)2NR83’R83’’ and - C(CH3)2OR83; wherein R₈₃, R_83’ and R_83’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁, -S(O)R₂₁, -S(O)₂R₂₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, -OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and - C(CH₃)₂OR₂₁; wherein R₂₁, 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;

R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, it is substituted with one or more substituent/s selected from–OR31, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31’; wherein the cycloalkyl in R3, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R31, -OR31, -NO2, -NR31R31’, -NR31C(O)R31’, -NR31S(O)2R31’, -S(O)2NR31R31’, - NR31C(O)NR31’R31’’, -SR31, -S(O)R31, -S(O)2R31,–CN, haloalkyl, haloalkoxy, -C(O)OR₃₁, -C(O)NR₃₁R_31’, -OCH₂CH₂OR₃₁, -NR₃₁S(O)₂NR_31’R_31’’ and - C(CH3)2OR31; preferably selected from halogen, -R31, -OR31, -NR31R31’, - CN, haloalkyl and haloalkoxy;

wherein R₃₁, 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 substituted or unsubstituted C_2-6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R_3’, if substituted, it is substituted with one or more substituent/s selected from–OR₃₂, halogen, -CN, haloalkyl, haloalkoxy and -NR₃₂R_32’; wherein R₃₂ 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;

R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)2R41,–CN, haloalkyl, haloalkoxy, -C(O)OR41, -C(O)NR41R41’, -OCH2CH2OR41, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; the alkyl, alkenyl or alkynyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from–OR13, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13’; wherein R₁₃ and R_13’ are independently selected from hydrogen, unsubstituted C_1-6 alkyl, unsubstituted C_2-6 alkenyl, and unsubstituted C_2-6 alkynyl;

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R₁₄, -OR₁₄, -NO₂, -NR₁₄R_14’, - NR₁₄C(O)R_14’, -NR₁₄S(O)₂R_14’, -S(O)₂NR₁₄R_14’, - NR₁₄C(O)NR_14’R_14’’, -SR₁₄, -S(O)R₁₄, - S(O)₂R₁₄,–CN, haloalkyl, haloalkoxy, -C(O)OR₁₄, -C(O)NR₁₄R_14’, -OCH₂CH₂OR₁₄, - NR₁₄S(O)₂NR_14’R_14’’ and -C(CH₃)₂OR₁₄; wherein R₁₄, 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;

optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^’)

(I’) wherein R1, R2, R3, R3’, R4, R4’, X and n are as defined in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

(I’) wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-; R_a is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; Rb is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl;

n is 0 or 1;

R₁ is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R5, R5’, R5’’ and R5’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

R₆, R_6’, R_6’’ and R_6’’’ are independently 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, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR71; wherein wherein R₇₁ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl;

R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, - NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;

R2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl,

R₃ 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, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;

R3’ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)2R41,–CN, haloalkyl, haloalkoxy, -C(O)OR41, -C(O)NR41R41’, -OCH2CH2OR41, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R₄₁, R_41’ and R_41’’ 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;

(I’) wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH2]pN(Rz)C(O)[CH2]q- and -[CH2]pN(Rz)[CH2]q-; Ra is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 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, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl;

n is 0 or 1;

R₁ is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R5, R5’, R5’’ and R5’’’ are independently 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, R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

wherein the cycloalkyl, as defined in R₅-R_5’ and/or R_5’’-R_5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₅₁, -OR₅₁, -NO₂, -NR₅₁R_51’, -NR₅₁C(O)R_51’, -NR₅₁S(O)₂R_51’, -S(O)₂NR₅₁R_51’, - NR₅₁C(O)NR_51’R_51’’, -SR₅₁ , -S(O)R₅₁, -S(O)₂R₅₁, –CN, haloalkyl, haloalkoxy, -C(O)OR51, -C(O)NR51R51’, -OCH2CH2OR51, - NR51S(O)2NR51’R51’’ and -C(CH3)2OR51; preferably selected from halogen, - R51, -OR51, -NR51R51’, -CN, haloalkyl and haloalkoxy;

wherein R51, R51’ and R51’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; R6, R6’, R6’’ and R6’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R6 and R6’ and/or R6’’ and R6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R₆, R_6’ R_6’’ and R_6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR₆₁, halogen, - CN, haloalkyl, haloalkoxy and–NR₆₁R_61’;

wherein the cycloalkyl, as defined in R₆-R_6’ and/or R_6’’-R_6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₆₁, -OR₆₁, -NO₂, -NR₆₁R_61’, -NR₆₁C(O)R_61’, -NR₆₁S(O)₂R_61’, -S(O)₂NR₆₁R_61’, - NR₆₁C(O)NR_61’R_61’’, -SR₆₁ , -S(O)R₆₁, -S(O)₂R₆₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₆₁, -C(O)NR₆₁R_61’, -OCH₂CH₂OR₆₁, - NR₆₁S(O)₂NR_61’R_61’’ and -C(CH₃)₂OR₆₁; preferably selected from halogen, - R₆₁, -OR₆₁, -NR₆₁R_61’, -CN, haloalkyl and haloalkoxy; wherein R₆₁, R_61’ and R_61’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR71; wherein the alkyl, alkenyl or alkynyl defined in R7, if substituted, it is substituted with one or more substituent/s selected from–OR71, halogen, -CN, haloalkyl, haloalkoxy and–NR₇₁R_71’; the aryl, heterocyclyl or cycloalkyl in R₇, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₇₁, -OR₇₁, -NO₂, - NR₇₁R_71’, -NR₇₁C(O)R_71’, -NR₇₁S(O)₂R_71’, -S(O)₂NR₇₁R_71’, - NR₇₁C(O)NR_71’R_71’’, -SR₇₁ , -S(O)R₇₁, -S(O)₂R₇₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₇₁, -C(O)NR₇₁R_71’, -OCH₂CH₂OR₇₁, - NR₇₁S(O)₂NR_71’R_71’’ and -C(CH₃)₂OR₇₁; wherein R₇₁, 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;

R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; wherein the aryl and heterocyclyl, as defined in R8, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R81, -OR81, -NO2, -NR81R81’, -NR81C(O)R81’, - NR81S(O)2R81’, -S(O)2NR81R81’, - NR81C(O)NR81’R81’’, -SR81 , -S(O)R81, - S(O)2R81, –CN, haloalkyl, haloalkoxy, -C(O)OR81, -C(O)NR81R81’, - OCH2CH2OR81, -NR81S(O)2NR81’R81’’ and -C(CH3)2OR81; wherein R81, R81’ and R81’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, - NR82R82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein

the alkyl, alkenyl or alkynyl defined in R_8’, if substituted, it is substituted with one or more substituent/s selected from–OR₈₂, halogen, -CN, haloalkyl, haloalkoxy and–NR₈₂R_82’;

wherein the cycloalkyl, aryl and heterocyclyl, as defined in R_8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₂, -OR₈₂, -NO₂, -NR₈₂R_82’, -NR₈₂C(O)R_82’, - NR₈₂S(O)₂R_82’, -S(O)₂NR₈₂R_82’, - NR₈₂C(O)NR_82’R_82’’, -SR₈₂ , -S(O)R₈₂, - S(O)₂R₈₂, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₂, -C(O)NR₈₂R_82’, - OCH₂CH₂OR₈₂, -NR₈₂S(O)₂NR_82’R_82’’ and -C(CH₃)₂OR₈₂; wherein R₈₂, R_82’ and R_82’’ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

alternatively, R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; wherein the cyclic amide or cyclic urea, as defined in R8-R8’ when taken together with the–N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R83, -OR₈₃, -NO₂, -NR₈₃R_83’, -NR₈₃C(O)R_83’, -NR₈₃S(O)₂R_83’, -S(O)₂NR₈₃R_83’, - NR83C(O)NR83’R83’’, -SR83 , -S(O)R83, -S(O)2R83, –CN, haloalkyl, haloalkoxy, -C(O)OR83, -C(O)NR83R83’, -OCH2CH2OR83, - NR83S(O)2NR83’R83’’ and -C(CH3)2OR83; wherein R83, R83’ and R83’’ 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;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, -OCH₂CH₂OR₂₁, - NR21S(O)2NR21’R21’’ and -C(CH3)2OR21; wherein R21, R21’ and R21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R3, if substituted, it is substituted with one or more substituent/s selected from–OR31, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31’; wherein the cycloalkyl in R₃, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R31, -OR31, -NO2, -NR31R31’, -NR31C(O)R31’, -NR31S(O)2R31’, -S(O)2NR31R31’, - NR31C(O)NR31’R31’’, -SR31 , -S(O)R31, -S(O)2R31, –CN, haloalkyl, haloalkoxy, -C(O)OR31, -C(O)NR31R31’, -OCH2CH2OR31, - NR₃₁S(O)₂NR_31’R_31’’ and -C(CH₃)₂OR₃₁; preferably selected from halogen, - R₃₁, -OR₃₁, -NR₃₁R_31’, -CN, haloalkyl and haloalkoxy;

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 alkyl, alkenyl or alkynyl defined in R_3’, if substituted, it is substituted with one or more substituent/s selected from–OR₃₂, halogen, -CN, haloalkyl, haloalkoxy and -NR₃₂R_32’; wherein R₃₂ 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 C2-6 alkynyl;

R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)2R41,–CN, haloalkyl, haloalkoxy, -C(O)OR41, -C(O)NR41R41’, -OCH2CH2OR41, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R₄₁, R_41’ and R_41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

the alkyl, alkenyl or alkynyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from–OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR₁₃R_13’; wherein R₁₃ and R_13’ are independently selected from hydrogen, unsubstituted C_1-6 alkyl, unsubstituted C_2-6 alkenyl, and unsubstituted C_2-6 alkynyl;

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R₁₄, -OR₁₄, -NO₂, -NR₁₄R_14’, - NR₁₄C(O)R_14’, -NR₁₄S(O)₂R_14’, -S(O)₂NR₁₄R_14’, - NR₁₄C(O)NR_14’R_14’’, -SR₁₄ , -S(O)R₁₄, - S(O)₂R₁₄,–CN, haloalkyl, haloalkoxy, -C(O)OR₁₄, -C(O)NR₁₄R_14’, -OCH₂CH₂OR₁₄, - NR₁₄S(O)₂NR_14’R_14’’ and -C(CH₃)₂OR₁₄;

wherein R14, R14’ and R14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^a)

wherein R₁, R₃, R_3’, R₄, R_4’, R₉, R_9’, X, Y₁, Y₂ and n are as defined in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^a)

wherein

X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_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, Ra and Rb, taken 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)-C1-6 alkyl; p is 0, 1, 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5;

n is 0 or 1; Y1 is–C(R10R10’)-; wherein R10 and R10’ 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, R₁₀ and R_10’ may, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

R₁ is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR₇₁; wherein R71 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, - NR82R82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; alternatively, R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea;

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;

R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)2R41,–CN, haloalkyl, haloalkoxy, -C(O)OR41, -C(O)NR41R41’, -OCH2CH2OR41, - NR₄₁S(O)₂NR_41’R_41’’ and -C(CH₃)₂OR₄₁; wherein R₄₁, R_41’ and R_41’’ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R9 and R9’ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21’, -NR21C(O)R21’, -NR21S(O)2R21’, -S(O)2NR21R21’, - NR21C(O)NR21’R21’’, -SR21 , -S(O)R21, -S(O)2R21, –CN, haloalkyl, haloalkoxy, -C(O)OR21, -C(O)NR21R21’, - OCH2CH2OR21, -NR21S(O)2NR21’R21’’ and -C(CH3)2OR21; wherein R₂₁, R_21’ and R_21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

wherein

R1 is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

wherein the alkyl, alkenyl or alkynyl defined in R₅, R_5’ R_5’’ and R_5’’’, if substituted, it is substituted with one or more substituent/s selected from–OR₅₁, halogen, - CN, haloalkyl, haloalkoxy and–NR₅₁R_51’; wherein the cycloalkyl, as defined in R₅-R_5’ and/or R_5’’-R_5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R51, -OR51, -NO2, -NR51R51’, -NR51C(O)R51’, -NR51S(O)2R51’, -S(O)2NR51R51’, - NR51C(O)NR51’R51’’, -SR51 , -S(O)R51, -S(O)2R51, –CN, haloalkyl, haloalkoxy, -C(O)OR51, -C(O)NR51R51’, -OCH2CH2OR51, - NR₅₁S(O)₂NR_51’R_51’’ and -C(CH₃)₂OR₅₁; preferably selected from halogen, - R₅₁, -OR₅₁, -NR₅₁R_51’, -CN, haloalkyl and haloalkoxy;

wherein R₅₁, 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;

R₆, R_6’, R_6’’ and R_6’’’ are independently 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, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R6, R6’ R6’’ and R6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR61, halogen, - CN, haloalkyl, haloalkoxy and–NR61R61’;

wherein the cycloalkyl, as defined in R6-R6’ and/or R6’’-R6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R61, -OR61, -NO2, -NR61R61’, -NR61C(O)R61’, -NR61S(O)2R61’, -S(O)2NR61R61’, - NR61C(O)NR61’R61’’, -SR61 , -S(O)R61, -S(O)2R61, –CN, haloalkyl, haloalkoxy, -C(O)OR61, -C(O)NR61R61’, -OCH2CH2OR61, - NR₆₁S(O)₂NR_61’R_61’’ and -C(CH₃)₂OR₆₁; preferably selected from halogen, - R61, -OR61, -NR61R61’, -CN, haloalkyl and haloalkoxy; wherein R61, R61’ and R61’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR₇₁; wherein the alkyl, alkenyl or alkynyl defined in R₇, if substituted, it is substituted with one or more substituent/s selected from–OR₇₁, halogen, -CN, haloalkyl, haloalkoxy and–NR₇₁R_71’; the aryl, heterocyclyl or cycloalkyl in R₇, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₇₁, -OR₇₁, -NO₂, - NR₇₁R_71’, -NR₇₁C(O)R_71’, -NR₇₁S(O)₂R_71’, -S(O)₂NR₇₁R_71’, - NR71C(O)NR71’R71’’, -SR71 , -S(O)R71, -S(O)2R71, –CN, haloalkyl, haloalkoxy, -C(O)OR71, -C(O)NR71R71’, -OCH2CH2OR71, - NR71S(O)2NR71’R71’’ and -C(CH3)2OR71; wherein R71, R71’ and R71’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; wherein the aryl and heterocyclyl, as defined in R₈, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R81, -OR81, -NO2, -NR81R81’, -NR81C(O)R81’, - NR81S(O)2R81’, -S(O)2NR81R81’, - NR81C(O)NR81’R81’’, -SR81 , -S(O)R81, - S(O)₂R₈₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₁, -C(O)NR₈₁R_81’, - OCH₂CH₂OR₈₁, -NR₈₁S(O)₂NR_81’R_81’’ and -C(CH₃)₂OR₈₁; wherein R₈₁, 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_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, - NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein

the alkyl, alkenyl or alkynyl defined in R8’, if substituted, it is substituted with one or more substituent/s selected from–OR₈₂, halogen, -CN, haloalkyl, haloalkoxy and–NR₈₂R_82’;

wherein the cycloalkyl, aryl and heterocyclyl, as defined in R8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R82, -OR82, -NO2, -NR82R82’, -NR82C(O)R82’, - NR82S(O)2R82’, -S(O)2NR82R82’, - NR82C(O)NR82’R82’’, -SR82 , -S(O)R82, - S(O)2R82, –CN, haloalkyl, haloalkoxy, -C(O)OR82, -C(O)NR82R82’, - OCH2CH2OR82, -NR82S(O)2NR82’R82’’ and -C(CH3)2OR82; wherein R₈₂, R_82’ and R_82’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

alternatively, R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; wherein the cyclic amide or cyclic urea, as defined in R₈-R_8’ when taken together with the–N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₃, -OR₈₃, -NO₂, -NR₈₃R_83’, -NR₈₃C(O)R_83’, -NR₈₃S(O)₂R_83’, -S(O)₂NR₈₃R_83’, - NR₈₃C(O)NR_83’R_83’’, -SR₈₃ , -S(O)R₈₃, -S(O)₂R₈₃, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₃, -C(O)NR₈₃R_83’, -OCH₂CH₂OR₈₃, - NR₈₃S(O)₂NR_83’R_83’’ and -C(CH₃)₂OR₈₃; wherein R₈₃, R_83’ and R_83’’ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R3, if substituted, it is substituted with one or more substituent/s selected from–OR31, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31’; wherein the cycloalkyl in R3, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R31, -OR31, -NO2, -NR31R31’, -NR31C(O)R31’, -NR31S(O)2R31’, -S(O)2NR31R31’, - NR31C(O)NR31’R31’’, -SR31 , -S(O)R31, -S(O)2R31, –CN, haloalkyl, haloalkoxy, -C(O)OR₃₁, -C(O)NR₃₁R_31’, -OCH₂CH₂OR₃₁, - NR31S(O)2NR31’R31’’ and -C(CH3)2OR31; preferably selected from halogen, - R31, -OR31, -NR31R31’, -CN, haloalkyl and haloalkoxy;

R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)2R41,–CN, haloalkyl, haloalkoxy, -C(O)OR41, -C(O)NR41R41’, -OCH2CH2OR41, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR21R21’, -NR21C(O)R21’, -NR21S(O)2R21’, -S(O)2NR21R21’, - NR21C(O)NR21’R21’’, -SR21 , -S(O)R21, -S(O)2R21, –CN, haloalkyl, haloalkoxy, -C(O)OR21, -C(O)NR21R21’, - OCH2CH2OR21, -NR21S(O)2NR21’R21’’ and -C(CH3)2OR21; wherein R21, R21’ and R21’’ 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 aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R₁₄, -OR₁₄, -NO₂, -NR₁₄R_14’, - NR14C(O)R14’, -NR14S(O)2R14’, -S(O)2NR14R14’, - NR14C(O)NR14’R14’’, -SR14 , -S(O)R14, - S(O)2R14,–CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14’, -OCH2CH2OR14, - NR14S(O)2NR14’R14’’ and -C(CH3)2OR14;

wherein R14, R14’ and R14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^a’)

wherein R₁, R₃, R_3’, R₄, R_4’, R₉, R_9’, X and n are as defined in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_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, taken 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;

R1 is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR₇₁; wherein R₇₁ 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;

R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl;

R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, - NR82R82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; alternatively, R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea;

R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 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 C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR₄₁S(O)₂NR_41’R_41’’ and -C(CH₃)₂OR₄₁; wherein R₄₁, R_41’ and R_41’’ 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;

R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, - OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; wherein R₂₁, R_21’ and R_21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

R1 is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R₁₄, -OR₁₄, -NO₂, -NR₁₄R_14’, - NR₁₄C(O)R_14’, -NR₁₄S(O)₂R_14’, -S(O)₂NR₁₄R_14’, - NR₁₄C(O)NR_14’R_14’’, -SR₁₄ , -S(O)R₁₄, - S(O)2R14,–CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14’, -OCH2CH2OR14, - NR14S(O)2NR14’R14’’ and -C(CH3)2OR14;

wherein R14, R14’ and R14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^b)

wherein R₁, R₃, R_3’, R₄, R_4’, R₉, R_9’, X, Y₁, Y₂ and n are as defined below in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^b)

Rz is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 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; Y1 is–C(R10R10’)-; wherein R10 and R10’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, R₁₀ and R_10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

R₁ is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R5, R5’, R5’’ and R5’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR₇₁; wherein R₇₁ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, - NR82R82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; alternatively, R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea;

R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR₄₁S(O)₂NR_41’R_41’’ and -C(CH₃)₂OR₄₁; wherein R₄₁, R_41’ and R_41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R9 and R9’ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21’, -NR21C(O)R21’, -NR21S(O)2R21’, -S(O)2NR21R21’, - NR21C(O)NR21’R21’’, -SR21 , -S(O)R21, -S(O)2R21, –CN, haloalkyl, haloalkoxy, -C(O)OR21, -C(O)NR21R21’, - OCH2CH2OR21, -NR21S(O)2NR21’R21’’ and -C(CH3)2OR21; wherein R₂₁, R_21’ and R_21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH2]pN(Rz)C(O)[CH2]q- and -[CH2]pN(Rz)[CH2]q-; R_a is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; Rb is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl;

n is 0 or 1; Y1 is–C(R10R10’)-; wherein R10 and R10’ 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, R₁₀ and R_10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is–C(R10’’R10’’’)-; wherein R_10’’ and R_10’’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R10’’ and R10’’’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

R1 is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

wherein the alkyl, alkenyl or alkynyl defined in R₅, R_5’ R_5’’ and R_5’’’, if substituted, it is substituted with one or more substituent/s selected from–OR51, halogen, - CN, haloalkyl, haloalkoxy and–NR51R51’;

wherein the cycloalkyl, as defined in R₅-R_5’ and/or R_5’’-R_5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₅₁, -OR₅₁, -NO₂, -NR₅₁R_51’, -NR₅₁C(O)R_51’, -NR₅₁S(O)₂R_51’, -S(O)₂NR₅₁R_51’, - NR₅₁C(O)NR_51’R_51’’, -SR₅₁ , -S(O)R₅₁, -S(O)₂R₅₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₅₁, -C(O)NR₅₁R_51’, -OCH₂CH₂OR₅₁, - NR₅₁S(O)₂NR_51’R_51’’ and -C(CH₃)₂OR₅₁; preferably selected from halogen, - R₅₁, -OR₅₁, -NR₅₁R_51’, -CN, haloalkyl and haloalkoxy;

R6, R6’, R6’’ and R6’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R6, R6’ R6’’ and R6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR61, halogen, - CN, haloalkyl, haloalkoxy and–NR61R61’; wherein the cycloalkyl, as defined in R₆-R_6’ and/or R_6’’-R_6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R61, -OR61, -NO2, -NR61R61’, -NR61C(O)R61’, -NR61S(O)2R61’, -S(O)2NR61R61’, - NR61C(O)NR61’R61’’, -SR61 , -S(O)R61, -S(O)2R61, –CN, haloalkyl, haloalkoxy, -C(O)OR61, -C(O)NR61R61’, -OCH2CH2OR61, - NR₆₁S(O)₂NR_61’R_61’’ and -C(CH₃)₂OR₆₁; preferably selected from halogen, - R₆₁, -OR₆₁, -NR₆₁R_61’, -CN, haloalkyl and haloalkoxy; wherein R₆₁, 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;

R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR71; wherein the alkyl, alkenyl or alkynyl defined in R7, if substituted, it is substituted with one or more substituent/s selected from–OR₇₁, halogen, -CN, haloalkyl, haloalkoxy and–NR₇₁R_71’; the aryl, heterocyclyl or cycloalkyl in R7, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R71, -OR71, -NO2, - NR71R71’, -NR71C(O)R71’, R71’, - NR71C(O)NR71’R71’’, -SR71 ,

haloalkyl, haloalkoxy, -C(O)OR71, -C(O)NR71R71’, -OCH2CH2OR71, - NR71S(O)2NR71’R71’’ and -C(CH3)2OR71; wherein R₇₁, R_71’ and R_71’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; wherein the aryl and heterocyclyl, as defined in R₈, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R₈₁, -OR₈₁, -NO₂, -NR₈₁R_81’, -NR₈₁C(O)R_81’, - NR₈₁S(O)₂R_81’, -S(O)₂NR₈₁R_81’, - NR₈₁C(O)NR_81’R_81’’, -SR₈₁ , -S(O)R₈₁, - S(O)₂R₈₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₁, -C(O)NR₈₁R_81’, - OCH₂CH₂OR₈₁, -NR₈₁S(O)₂NR_81’R_81’’ and -C(CH₃)₂OR₈₁; wherein R₈₁, 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 C2-6 alkynyl;

R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, - NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein

the alkyl, alkenyl or alkynyl defined in R8’, if substituted, it is substituted with one or more substituent/s selected from–OR82, halogen, -CN, haloalkyl, haloalkoxy and–NR82R82’; wherein the cycloalkyl, aryl and heterocyclyl, as defined in R_8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₂, -OR₈₂, -NO₂, -NR₈₂R_82’, -NR₈₂C(O)R_82’, - NR₈₂S(O)₂R_82’, -S(O)₂NR₈₂R_82’, - NR₈₂C(O)NR_82’R_82’’, -SR₈₂ , -S(O)R₈₂, - S(O)₂R₈₂, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₂, -C(O)NR₈₂R_82’, - OCH₂CH₂OR₈₂, -NR₈₂S(O)₂NR_82’R_82’’ and -C(CH₃)₂OR₈₂; wherein R₈₂, R_82’ and R_82’’ 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, R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; wherein the cyclic amide or cyclic urea, as defined in R₈-R_8’ when taken together with the–N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₃, -OR₈₃, -NO₂, -NR₈₃R_83’, -NR₈₃C(O)R_83’, -NR₈₃S(O)₂R_83’, -S(O)₂NR₈₃R_83’, - NR83C(O)NR83’R83’’, -SR83 , -S(O)R83, -S(O)2R83, –CN, haloalkyl, haloalkoxy, -C(O)OR83, -C(O)NR83R83’, -OCH2CH2OR83, - NR83S(O)2NR83’R83’’ and -C(CH3)2OR83; wherein R83, R83’ and R83’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, it is substituted with one or more substituent/s selected from–OR31, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31’; wherein the cycloalkyl in R₃, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₃₁, -OR₃₁, -NO₂, -NR₃₁R_31’, -NR₃₁C(O)R_31’, -NR₃₁S(O)₂R_31’, -S(O)₂NR₃₁R_31’, - NR₃₁C(O)NR_31’R_31’’, -SR₃₁ , -S(O)R₃₁, -S(O)₂R₃₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₃₁, -C(O)NR₃₁R_31’, -OCH₂CH₂OR₃₁, - NR₃₁S(O)₂NR_31’R_31’’ and -C(CH₃)₂OR₃₁; preferably selected from halogen, - R₃₁, -OR₃₁, -NR₃₁R_31’, -CN, haloalkyl and haloalkoxy;

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 alkyl, alkenyl or alkynyl defined in R_3’, if substituted, it is substituted with one or more substituent/s selected from–OR₃₂, halogen, -CN, haloalkyl, haloalkoxy and -NR32R32’; wherein R₃₂ and R_32’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, - OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; wherein R₂₁, 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 aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R14, -OR14, -NO2, -NR14R14’, - NR14C(O)R14’, -NR14S(O)2R14’, -S(O)2NR14R14’, - NR14C(O)NR14’R14’’, -SR14 , -S(O)R14, - S(O)2R14,–CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14’, -OCH2CH2OR14, - NR14S(O)2NR14’R14’’ and -C(CH3)2OR14; wherein R14, R14’ and R14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^b’)

wherein R₁, R₃, R_3’, R₄, R_4’, R₉, R_9’, X and n are as defined below in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_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, Ra and Rb, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl;

Rz is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(O)-C1-6 alkyl; p is 0, 1, 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5;

n is 0 or 1;

R1 is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, - NR82R82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;

alternatively, R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;

R3’ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR₄₁S(O)₂NR_41’R_41’’ and -C(CH₃)₂OR₄₁; wherein R₄₁, R_41’ and R_41’’ 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;

R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR21R21’, -NR21C(O)R21’, -NR21S(O)2R21’, -S(O)2NR21R21’, - NR21C(O)NR21’R21’’, -SR21 , -S(O)R21, -S(O)2R21, –CN, haloalkyl, haloalkoxy, -C(O)OR21, -C(O)NR21R21’, - OCH2CH2OR21, -NR21S(O)2NR21’R21’’ and -C(CH3)2OR21; wherein R₂₁, 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I^b’)

wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_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; Rb is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Ra and Rb, taken 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 C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(O)-C1-6 alkyl; p is 0, 1, 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5;

n is 0 or 1;

R₁ is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R₅, R_5’, R_5’’ and R_5’’’ are independently 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, R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R5, R5’ R5’’ and R5’’’, if substituted, it is substituted with one or more substituent/s selected from–OR51, halogen, - CN, haloalkyl, haloalkoxy and–NR51R51’;

wherein R₅₁, 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 C2-6 alkynyl;

R6, R6’, R6’’ and R6’’’ are independently 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, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R6, R6’ R6’’ and R6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR61, halogen, - CN, haloalkyl, haloalkoxy and–NR61R61’; wherein the cycloalkyl, as defined in R₆-R_6’ and/or R_6’’-R_6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₆₁, -OR₆₁, -NO₂, -NR₆₁R_61’, -NR₆₁C(O)R_61’, -NR₆₁S(O)₂R_61’, -S(O)₂NR₆₁R_61’, - NR₆₁C(O)NR_61’R_61’’, -SR₆₁ , -S(O)R₆₁, -S(O)₂R₆₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₆₁, -C(O)NR₆₁R_61’, -OCH₂CH₂OR₆₁, - NR₆₁S(O)₂NR_61’R_61’’ and -C(CH₃)₂OR₆₁; preferably selected from halogen, - R₆₁, -OR₆₁, -NR₆₁R_61’, -CN, haloalkyl and haloalkoxy; wherein R₆₁, 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;

R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR₇₁; wherein the alkyl, alkenyl or alkynyl defined in R7, if substituted, it is substituted with one or more substituent/s selected from–OR71, halogen, -CN, haloalkyl, haloalkoxy and–NR71R71’; the aryl, heterocyclyl or cycloalkyl in R7, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R71, -OR71, -NO2, - NR71R71’, -NR71C(O)R71’, -NR71S(O)2R71’, -S(O)2NR71R71’, - NR71C(O)NR71’R71’’, -SR71 , -S(O)R71, -S(O)2R71, –CN, haloalkyl, haloalkoxy, -C(O)OR71, -C(O)NR71R71’, -OCH2CH2OR71, - NR71S(O)2NR71’R71’’ and -C(CH3)2OR71; wherein R₇₁, R_71’ and R_71’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;

R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, - OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; wherein R₂₁, 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 alkyl, alkenyl or alkynyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from–OR13, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13’; wherein R13 and R13’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl;

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R14, -OR14, -NO2, -NR14R14’, - NR14C(O)R14’, -NR14S(O)2R14’, -S(O)2NR14R14’, - NR14C(O)NR14’R14’’, -SR14 , -S(O)R14, - S(O)2R14,–CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14’, -OCH2CH2OR14, - NR14S(O)2NR14’R14’’ and -C(CH3)2OR14; wherein R₁₄, R_14’ and R_14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

For clarity purposes, all groups and definitions described in the present description and referring to compounds of general Formula (I), also apply to compounds of general Markush Formulae (I’), (I^a), (I^a’), (I^b) and (I^b’), (where applicable), and to all intermediate of synthesis, when those groups are present in the mentioned general Markush formulae, since compounds of general Markush Formulae (I’), (I^a), (I^a’), (I^b) and (I^b’), are included within the scope of the larger definition of general Markush Formula (I).

For clarity purposes, the general Markush Formula (I)

is equivalent to

wherein only– CH2- is included into the brackets, and n means the number of times that–CH2- is repeated. The same would apply, when applicable, to general Markush Formulae (I), (I’), (I^a), (I^a’), (I^b) and (I^b’), and to all intermediates of synthesis. In addition, and for clarity purposes, it should further be understood that naturally if n is 0, the oxygen atom and/or the phenyl group are still present, when applicable, in general Markush Formulae (I), (I’), (I^a), (I^a’), (I^b) and (I^b’), and to all intermediates of synthesis.

For clarity purposes, the expression e.g.“the cycle in R₈-R_8’“, means the cycle resulting when R₈ and R_8’ form, together with the atom(s) to which they are attached. This cycle can then be substituted or not. This definition is also generally applicable and can be also applied as a definition of any other cycle (preferably cycloalkyls, heterocycls or aryls) formed from two different functional groups like e.g.“the cycle in Ri-Ri’“ means the cycle resulting when Ri and Ri’ form a cycle together with the atom(s) to which they are attached. This cycle can then be substituted or not. For clarity purposes, reference is also made to the following statements below in the definitions of substitutions on alkyl etc. or aryl etc. that“wherein when different radicals R1 to R83’’ are present simultaneously in Formula (I) they may be identical or different”. This statement is reflected in the below general Formula (I^3’) being derived from and falling into the definition of R1 within Formula (I),

wherein R5, R5’, R5’’, R5’’’, R6, R6’, R6’’, R6’’’, R7, R8, R8’ and t are as defined in the description. In addition, R6a, R6b, R6c, R6d, m’ and r’ are added. As said above, this statement is thus reflected in that R6a, R6b are or could be different from R6 and R6’ or not. In the same way, R6c and R6d are or could be different from R6’’ and R6’’’ or not. m’ being 0 or 1 and r’ being 0 or 1 naturally resulting from m being o, 1 or 2 or r being 0, 1 or 2. The same would be applicable mutatis mutandis for general Formulas like general Formula (I) as well as the other general Formulas (I), (I’), (I^a), (I^a’), (I^b) and (I^b’), above and to all intermediates of synthesis.

In the context of this invention, alkyl is understood as meaning saturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses e.g. -CH3 and -CH2-CH3. In these radicals, C1-2-alkyl represents C1- or C2-alkyl, C1-3-alkyl represents C1-, C2- or C3-alkyl, C1-4-alkyl represents C1-, C2-, C3- or C4-alkyl, C1-5-alkyl represents C1-, C2-, C3-, C4-, or C5-alkyl, C1-6-alkyl represents C1-, C2-, C3-, C4-, C5- or C6-alkyl, C1-7-alkyl represents C1-, C2-, C3-, C4- , C5-, C6- or C7-alkyl, C1-8-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7- or C8- alkyl, C1-10-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9- or C10-alkyl and C1-18-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9-, C10-, C11-, C12-, C13-, C14-, C15-, C16-, C17- or C18-alkyl. The alkyl radicals are 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 also CHF₂, CF₃ or CH₂OH etc. Preferably alkyl is understood in the context of this invention as C1-8alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, or octyl; preferably is C1-6alkyl like methyl, ethyl, propyl, butyl, pentyl, or hexyl; more preferably is C1-4alkyl like methyl, ethyl, propyl or butyl. Alkenyl is understood as meaning unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses groups like e.g. -CH=CH-CH₃. The alkenyl radicals are preferably vinyl (ethenyl), allyl (2-propenyl). Preferably in the context of this invention alkenyl is C_2-10-alkenyl or C_2-8-alkenyl like ethylene, propylene, butylene, pentylene, hexylene, heptylene or octylene; or is C_2-6- alkenyl like ethylene, propylene, butylene, pentylene, or hexylene; or is C_2-4-alkenyl, like ethylene, propylene, or butylenes. Alkynyl is understood as meaning unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses groups like e.g. -C=C-CH₃ (1-propinyl). Preferably alkynyl in the context of this invention is C_2-10- alkynyl or C_2-8-alkynyl like ethyne, propyne, butyene, pentyne, hexyne, heptyne, or octyne; or is C_2-6-alkynyl like ethyne, propyne, butyene, pentyne, or hexyne; or is C_2-4- alkynyl like ethyne, propyne, butyene, pentyne, or hexyne. In connection with alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl and O-alkyl - unless defined otherwise - the term substituted in the context of this invention is understood as meaning replacement of at least one hydrogen radical on a carbon atom by halogen (F, Cl, Br, I), -NR_kR_k’, -SR_k, -S(O)R_k, -S(O)₂R_k, -OR_k, - C(O)R_k, -C(O)OR_k, -CN, -C(O)NR_kR_k’, haloalkyl, haloalkoxy, being R_k represented by R13, R31, R32, R51, R61, R71 or R82 (being Rk’ represented by R13’, R31’, R32’, R51’, R61’, R71’ or R82’; being Rk’’ represented by R13’’, R31’’, R32’’, R51’’, R61’’, R71’’ or R82’’); wherein R1 to R83’’ andRz are as defined in the description, and wherein when different radicals R1 to R83’’ andRz are present simultaneously in Formula I they may be identical or different. Most preferably in connection with alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl, substituted is understood in the context of this invention that any alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl which is substituted with one or more of halogen (F, Cl, Br, I), -NRkRk’, -ORk, -CN,–SRk, haloalkyl, haloalkoxy, being Rk represented by R13, R31, R32, R51, R61, R71 or R82, (being Rk’ represented by R13’, R31’, R32’, R51’, R61’, R71’ or R82’; being R_k’’ represented by R_13’’, R_31’’, R_32’’, R_51’’, R_61’’, R_71’’ or R_82’’)_; wherein R₁ to R_83’’ andR_z are as defined in the description, and wherein when different radicals R1 to R83’’ and Rz are present simultaneously in Formula I they may be identical or different. More than one replacement on the same molecule and also on the same carbon atom is possible with the same or different substituents. This includes for example 3 hydrogens being replaced on the same C atom, as in the case of CF₃, or at different places of the same molecule, as in the case of e.g. -CH(OH)-CH=CH-CHCl₂. In the context of this invention haloalkyl is understood as meaning an alkyl being substituted once or several times by a halogen (selected from F, Cl, Br, I). It encompasses e.g.–CH₂Cl,–CH₂F,–CHCl₂,–CHF₂,–CCl₃,–CF₃ and -CH₂-CHCI₂. Preferably haloalkyl is understood in the context of this invention as halogen- substituted C_1-4-alkyl representing halogen substituted C1-, C2-, C3- or C4-alkyl. The halogen-substituted alkyl radicals are thus preferably methyl, ethyl, propyl, and butyl. Preferred examples include–CH₂Cl,–CH₂F,–CHCl₂,–CHF₂, and–CF₃. In the context of this invention haloalkoxy is understood as meaning an–O-alkyl being substituted once or several times by a halogen (selected from F, Cl, Br, I). It encompasses e.g.–OCH2Cl,–OCH2F,–OCHCl2,–OCHF2,–OCCl3,–OCF3 and - OCH2-CHCI2. Preferably haloalkoxy is understood in the context of this invention as halogen-substituted -OC_1-4-alkyl representing halogen substituted C1-, C2-, C3- or C4- alkoxy. The halogen-substituted alkyl radicals are thus preferably O-methyl, O-ethyl, O-propyl, and O-butyl. Preferred examples include–OCH₂Cl,–OCH₂F,–OCHCl₂,– OCHF2, and–OCF3. In the context of this invention cycloalkyl is understood as meaning saturated and unsaturated (but not aromatic) cyclic hydrocarbons (without a heteroatom in the ring), which can be unsubstituted or once or several times substituted. Furthermore, C3-4- cycloalkyl represents C3- or C4-cycloalkyl, C3-5-cycloalkyl represents C3-, C4- or C5- cycloalkyl, C3-6-cycloalkyl represents C3-, C4-, C5- or C6-cycloalkyl, C3-7-cycloalkyl represents C3-, C4-, C5-, C6- or C7-cycloalkyl, C3-8-cycloalkyl represents C3-, C4-, C5- , C6-, C7- or C8-cycloalkyl, C4-5-cycloalkyl represents C4- or C5-cycloalkyl, C4-6- cycloalkyl represents C4-, C5- or C6-cycloalkyl, C4-7-cycloalkyl represents C4-, C5-, C6- or C7-cycloalkyl, C5-6-cycloalkyl represents C5- or C6-cycloalkyl and C5-7-cycloalkyl represents 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 this invention cycloalkyl is C3-8cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; or is C3-7cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; or is C_3-6cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, especially cyclopentyl or cyclohexyl. Aryl is understood as meaning 5 to 18 membered mono or polycyclic ring systems with at least one aromatic ring but without heteroatoms even in only one of the rings. Examples are phenyl, naphthyl, fluoranthenyl, fluorenyl, tetralinyl or indanyl, 9H- fluorenyl or anthracenyl radicals, which can be unsubstituted or once or several times substituted. Most preferably aryl is understood in the context of this invention as phenyl, naphthyl or anthracenyl, preferably is phenyl. A heterocyclyl radical or group (also called heterocyclyl hereinafter) is understood as meaning 5 to 18 membered mono or polycyclic heterocyclic ring systems, with at least one saturated or unsaturated ring which contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring. A heterocyclic group can also be substituted once or several times.

Subgroups inside the heterocyclyls as understood herein include heteroaryls and non- aromatic heterocyclyls.

- the heteroaryl (being equivalent to heteroaromatic radicals or aromatic heterocyclyls) is an aromatic 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more rings of which at least one aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a 5 to 18 membered mono or polycyclic aromatic heterocyclic ring system of one or two rings of which at least one aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is 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;

- the non-aromatic heterocyclyl is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more rings of which at least one ring– with this (or these) ring(s) then not being aromatic - contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or two rings of which one or both rings– with this one or two rings then not being aromatic– contain/s one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepam, pyrrolidine, piperidine, piperazine, tetrahydropyran, morpholine, indoline, oxopyrrolidine, benzodioxane, especially is benzodioxane, morpholine, tetrahydropyran, piperidine, oxopyrrolidine and pyrrolidine.

Preferably in the context of this invention heterocyclyl is defined as a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring. Preferably it is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring. An heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, quinolone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, benzodioxolane, benzodioxane, carbazole, oxaspirodecan or thiazole; In general, such a heterocyclyl may contain between 3 and 32 atoms in the rings (preferably 4 to 20 atoms in the rings, or most preferably 5 to 18 atoms in the rings). Thus, a heterocyclyl may contain between 3 and 12 atoms in the ring (preferably 4 to 10 atoms in the ring, or 5 to 8 atoms in the ring, or 5 to 6 atoms in the ring) in case of a heterocyclyl of one saturated or unsaturated ring. Such a heterocyclyl may also contain between 5 and 22 atoms in both rings together (preferably 6 to 16 atoms in both rings together, or 7 to 12 atoms in both rings together or 8 to 10 atoms in both rings together) in case of a heterocyclyl of two saturated or unsaturated rings. Such a heterocyclyl may also contain between 7 and 32 atoms in the 3 rings together (preferably 10 to 22 atoms in the three rings together, or 12 to 20 atoms in the three rings together or 10 to 18 atoms in the three rings together) in case of a heterocyclyl of three saturated or unsaturated rings.

Preferred examples of heterocyclyls include oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, , benzofuran, benzimidazole, indazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline, especially is pyridine, pyrazine, indazole, benzodioxane, thiazole, benzothiazole, morpholine, tetrahydropyrane, pyrazole, imidazole, piperidine, thiophene, indole, benzimidazole, pyrrolo[2,3b]pyridine, benzoxazole, oxopyrrolidine, pyrimidine, oxazepane and pyrrolidine. In the context of this invention oxopyrrolidine is understood as meaning pyrrolidin-2- one. An N-containing heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains a nitrogen and optionally one or more further heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains a nitrogen and optionally one or more further heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepam, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzimidazole, indazole, benzothiazole, benzodiazole, morpholine, indoline, triazole, isoxazole, pyrazole, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, quinolone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, carbazole or thiazole. In the context of this invention, a cyclic amide is defined as a subgroup of a heterocyclyl (as defined above) formed through the cyclization of a carbon sequence, containing at least the sequence

forming part of the cycle. Said cyclic amide may optionally be fused to a ring system. Preferably the cyclic amide is an“indoline-2-one”. A cyclic amide may be substituted or unsubstituted as defined for heterocyclyl above.

In the context of this invention, a cyclic urea is defined as a subgroup of a heterocyclyl (as defined above) formed through the cyclization of a carbon sequence containing at least the sequence

forming part of the cycle. Said cyclic urea may optionally be fused to a ring system. Preferably the cyclic urea is“1H-benzo[d]imidazol-2(3H)-one”. A cyclic urea may be substituted or unsubstituted as defined for heterocyclyl above. In connection with aromatic heterocyclyls (heteroaryls), non-aromatic heterocyclyls, aryls and cycloalkyls, when a ring system falls within two or more of the above cycle definitions simultaneously, then the ring system is defined first as an aromatic heterocyclyl (heteroaryl) if at least one aromatic ring contains a heteroatom. If no aromatic ring contains a heteroatom, then the ring system is defined as a non-aromatic heterocyclyl if at least one non-aromatic ring contains a heteroatom. If no non-aromatic ring contains a heteroatom, then the ring system is defined as an aryl if it contains at least one aryl cycle. If no aryl is present, then the ring system is defined as a cycloalkyl if at least one non-aromatic cyclic hydrocarbon is present. In the context of this invention alkylaryl is understood as meaning an aryl group (see above) being connected to another atom through a C_1-6-alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times. Preferably alkylaryl is understood as meaning an aryl group (see above) being connected to another atom through 1 to 4 (-CH₂-) groups. Most preferably alkylaryl is benzyl (i.e.–CH₂-phenyl). In the context of this invention alkylheterocyclyl is understood as meaning an heterocyclyl group being connected to another atom through a C1-6-alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times. Preferably alkylheterocyclyl is understood as meaning an heterocyclyl group (see above) being connected to another atom through 1 to 4 (-CH₂-) groups. Most preferably alkylheterocyclyl is–CH₂-pyridine. In the context of this invention alkylcycloalkyl is understood as meaning an cycloalkyl group being connected to another atom through a C1-6-alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times. Preferably alkylcycloalkyl is understood as meaning a cycloalkyl group (see above) being connected to another atom through 1 to 4 (-CH2-) groups. Most preferably alkylcycloalkyl is–CH2-cyclopropyl. Preferably, the aryl is a monocyclic aryl. More preferably the aryl is a 5, 6 or 7 membered monocyclic aryl. Even more preferably the aryl is a 5 or 6 membered monocyclic aryl. Preferably, the heteroaryl is a monocyclic heteroaryl. More preferably the heteroaryl is a 5, 6 or 7 membered monocyclic heteroaryl. Even more preferably the heteroaryl is a 5 or 6 membered monocyclic heteroaryl. Preferably, the non-aromatic heterocyclyl is a monocyclic non-aromatic heterocyclyl. More preferably the non-aromatic heterocyclyl is a 4, 5, 6 or 7 membered monocyclic non-aromatic heterocyclyl. Even more preferably the non-aromatic heterocyclyl is a 5 or 6 membered monocyclic non-aromatic heterocyclyl. Preferably, the cycloalkyl is a monocyclic cycloalkyl. More preferably the cycloalkyl is a 3, 4, 5, 6, 7 or 8 membered monocyclic cycloalkyl. Even more preferably the cycloalkyl is a 3, 4, 5 or 6 membered monocyclic cycloalkyl.

In connection with aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), substituted is understood - unless defined otherwise - as meaning substitution of the ring-system of the aryl or alkyl-aryl, cycloalkyl or alkyl-cycloalkyl; heterocyclyl or alkyl-heterocyclyl with one or more of halogen (F, Cl, Br, I), -Rk ,-ORk, -CN, -NO2 , -NRkRk’, -C(O)ORk, NRkC(O)Rk’ , -C(O)NRkRk’ , - NR_kS(O)₂R_k’ , =O, -OCH₂CH₂OH, -NR_kC(O)NR_k’R_k’’, -S(O)₂NR_kR_k’, -NR_kS(O)₂NR_k’R_k’’, haloalkyl, haloalkoxy, -SR_k, -S(O)R_k, -S(O)₂R_k or C(CH₃)OR_k, or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, with Rk, Rk’ and Rk’’ independently being either H or a saturated or unsaturated, linear or branched, substituted or unsubstituted C1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted C1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted–O-C1-6-alkyl (alkoxy); a saturated or unsaturated, linear or branched, substituted or unsubstituted– S-C1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted -C(O)-C1-6-alkyl-group; a saturated or unsaturated, linear or branched, substituted or unsubstituted -C(O)-O-C1-6-alkyl-group; a substituted or unsubstituted aryl or alkyl-aryl; a substituted or unsubstituted cycloalkyl or alkyl-cycloalkyl; a substituted or unsubstituted heterocyclyl or alkyl-heterocyclyl, being Rk one of R14, R21, R31, R51, R61, R71, R81, R82 or R83,(being Rk’ one of R14’, R21’, R31’, R51’, R61’, R71’, R81’, R82’ or R83’, being Rk’’ one of R14’’, R21’’, R31’’, R51’’, R61’’, R71’’, R81’’, R82’’ or R83’’; wherein R1 to R83’’ and Rz are as defined in the description, and wherein when different radicals R₁ to R_83’’ and R_z are present simultaneously in Formula I they may be identical or different. Most preferably in connection with aryl (including alkyl-aryl), cycloalkyl (including alkyl- cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), substituted is understood in the context of this invention that any aryl, cycloalkyl and heterocyclyl which is substituted is substituted (also in an alyklaryl, alkylcycloalkyl or alkylheterocyclyl) with one or more of halogen (F, Cl, Br, I), -R_k ,-OR_k, -CN , -NO₂ , -NR_kR_k’’’ , NR_kC(O)R_k’, - NR_kS(O)₂R_k’ , -S(O)₂NR_kR_k’, -NR_kC(O)NR_k’R_k’’, haloalkyl, haloalkoxy,–SR_k , -S(O)R_k or S(O)₂R_k, or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, being R_k one of R_14, R_21, R_31, R_51, R_61, R_71, R_81, R_{82 or} R₈₃, (being R_k’ one of R_14’, R_21’, R_31’, R_51’, R_61’, R_71’, R_81’, R_{82’ or} R_83’; being R_k’’ one of R_14’’, R_21’’, R_31’’, R_51’’, R_61’’, R_71’’, R_81’’, R_{82’’ or} R_83’’; wherein R₁ to R_83’’ andR_z are as defined in the description, and wherein when different radicals R₁ to R_83’’ and R_z are present simultaneously in Formula I they may be identical or different. In connection with cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkylheterocyclyl) namely non-aromatic heterocyclyl (including non-aromatic alkyl- heterocyclyl), substituted is also understood - unless defined otherwise - as meaning substitution of the ring-system of the cycloalkyl or alkyl-cycloalkyl; non-aromatic heterocyclyl or non aromatic alkyl-heterocyclyl with

(leading to a spiro structure) and/or with =O. Moreover, in connection with cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkylheterocyclyl) namely non-aromatic heterocyclyl (including non-aromatic alkyl-heterocyclyl), substituted is also understood - unless defined otherwise - as meaning substitution of the ring-system of the cycloalkyl or alkyl-cycloalkyl; non- aromatic heterocyclyl or non aromatic alkyl-heterocyclyl is spirosubstituted or substituted with =O.

Moreover, in connection with cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkylheterocyclyl) namely non-aromatic heterocyclyl (including non-aromatic alkyl-heterocyclyl), substituted is also understood - unless defined otherwise - as meaning substitution of the ring-system of the cycloalkyl or alkyl-cycloalkyl; non- aromatic heterocyclyl or non aromatic alkyl-heterocyclyl with =O.

A ring system is a system consisting of at least one ring of connected atoms but including also systems in which two or more rings of connected atoms are joined with “joined” meaning that the respective rings are sharing one (like a spiro structure), two or more atoms being a member or members of both joined rings.

The term“leaving group” means a molecular fragment that departs with a pair of electrons in heterolytic bond cleavage. Leaving groups can be anions or neutral molecules. Common anionic leaving groups are halides such as Cl−, Br−, and I−, and sulfonate esters, such as tosylate (TsO−) or mesylate. The term“salt” is to be understood as meaning any form of the active compound used according to the invention in which it assumes an ionic form or is charged and is coupled with a counter-ion (a cation or anion) or is in solution. By this are also to be understood complexes of the active compound with other molecules and ions, in particular complexes via ionic interactions. The term“physiologically acceptable salt” means in the context of this invention any salt that is physiologically tolerated (most of the time meaning not being toxic- especially not caused by the counter-ion) if used appropriately for a treatment especially if used on or applied to humans and/or mammals. These physiologically acceptable salts can be formed with cations or bases and in the context of this invention is understood as meaning salts of at least one of the compounds used according to the invention - usually a (deprotonated) acid - as an anion with at least one, preferably inorganic, cation which is physiologically tolerated - especially if used on humans and/or mammals. The salts of the alkali metals and alkaline earth metals are particularly preferred, and also those with NH4, but in particular (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 this invention is understood as meaning salts of at least one of the compounds used according to the invention as the cation with at least one anion which are physiologically tolerated - especially if used on humans and/or mammals. By this is understood in particular, in the context of this invention, the salt formed with a physiologically tolerated acid, that is to say salts of the particular active compound with inorganic or organic acids which are physiologically tolerated - especially if used on humans and/or mammals. Examples of physiologically tolerated salts of particular acids are salts of: hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, formic acid, acetic acid, oxalic acid, succinic acid, malic acid, tartaric acid, mandelic acid, fumaric acid, lactic acid or citric acid. The compounds of the invention may be present in crystalline form or in the form of free compounds like a free base or acid. Any compound that is a solvate of a compound according to the invention like a compound according to general formula I defined above is understood to be also covered by the scope of the invention. Methods of solvation are generally known within the art. Suitable solvates are pharmaceutically acceptable solvates. The term“solvate” according to this invention is to be understood as meaning any form of the active compound according to the invention in which this compound has attached to it via non- covalent binding another molecule (most likely a polar solvent). Especially preferred examples include hydrates and alcoholates, like methanolates or ethanolates. Any compound that is a prodrug of a compound according to the invention like a compound according to general formula I defined above is understood to be also covered by the scope of the invention. The term“prodrug” is used in its broadest sense and encompasses those derivatives that are converted in vivo to the compounds of the invention. Such derivatives would readily occur to those skilled in the art, and include, depending on the functional groups present in the molecule and without limitation, the following derivatives of the present compounds: esters, amino acid esters, phosphate esters, metal salts sulfonate esters, carbamates, and amides. Examples of well known methods of producing a prodrug of a given acting compound are known to those skilled in the art and can be found e.g. in Krogsgaard-Larsen et al.“Textbook of Drug design and Discovery” Taylor & Francis (April 2002). Any compound that is a N-oxide of a compound according to the invention like a compound according to general formula I defined above is understood to be also covered by the scope of the invention.

Unless otherwise stated, the compounds of the invention are also meant to include compounds which differ only in the presence of one or more isotopically enriched atoms. For example, compounds having the present structures except for the replacement of a hydrogen by a deuterium or tritium, or the replacement of a carbon by ¹³C- or ¹⁴C-enriched carbon or of a nitrogen by ¹⁵N-enriched nitrogen are within the scope of this invention. This would especially also apply to the provisos described above so that any mentioning of hydrogen or any“H” in a formula would also cover deuterium or tritium. The compounds of formula (I) as well as their salts or solvates of the compounds are preferably in pharmaceutically acceptable or substantially pure form. By pharmaceutically acceptable form is meant, inter alia, having a pharmaceutically acceptable level of purity excluding normal pharmaceutical additives such as diluents and carriers, and including no material considered toxic at normal dosage levels. Purity levels for the drug substance are preferably above 50%, more preferably above 70%, most preferably above 90%. In a preferred embodiment it is above 95% of the compound of formula (I), or of its salts. This applies also to its solvates or prodrugs.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein X is selected from a bond, -[C(RaRb)]p-, -[CH2]pC(O)[CH2]q-, -[CH2]pC(O)N(Rz)[CH2]q-, - [CH2]pN(Rz)C(O)[CH2]q- and -[CH2]pN(Rz)[CH2]q-; Ra is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R_b is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Ra and Rb, taken 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; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein X is selected from a bond, -[C(RaRb)]p-, -[CH2]pC(O)[CH2]q-, -[CH2]pC(O)N(Rz)[CH2]q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein X is selected from a bond, -[CH₂]_p- , -[CH(CH₃)]_p- and -[CH₂]_pN(R_z)C(O)[CH₂]_q-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further 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 C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Ra is selected from hydrogen, halogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Ra is selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further 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 C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Rb is selected from hydrogen, halogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Ra and Rb, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Rz is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(O)-C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein p is 0, 1, 2, 3, 4 or 5; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein q is 0, 1, 2, 3, 4 or 5; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein n is 0 or 1; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein m is 0, 1 or 2; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein r is 0, 1 or 2; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Y₁ is–C(R₁₀R_10’)-; wherein R10 and R10’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R₁₀ and R_10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Y1 is–C(R10R10’)-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein Y₂ is–C(R_10’’R_10’’’)-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R₁ is

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl and substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃ is selected from substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R3’ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_3’ is selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR₄₁S(O)₂NR_41’R_41’’ and -C(CH₃)₂OR₄₁; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R5, R5’, R5’’ and R5’’’ are independently 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; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₅, R_5’, R_5’’ and R_5’’’ are independently selected from hydrogen, halogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R6, R6’, R6’’ and R6’’’ are independently 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; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R6, R6’, R6’’ and R6’’’ are independently selected from hydrogen, halogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and–C(O)OR71; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and–C(O)OR₇₁; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted aromatic heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, -NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R8’ is selected from substituted or unsubstituted C1-6 alkyl, -NR82R82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_8’ is selected from substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_8’ 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 and substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic urea; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R9 and R9’ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21’, -NR21C(O)R21’, -NR21S(O)2R21’, -S(O)2NR21R21’, - NR21C(O)NR21’R21’’, -SR21 , -S(O)R21, -S(O)2R21, –CN, haloalkyl, haloalkoxy, -C(O)OR21, -C(O)NR21R21’, - OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₁₀ 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R10 and R10’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₁₀ and R_10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R10’’ and R10’’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_10’’ and R_10’’’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R13 and R13’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R13 and R13’ are independently selected from hydrogen and unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₁₄, 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; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R14, R14’ and R14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₂₁, R_21’ and R_21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₂₁, R_21’ and R_21’’ are independently selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃₁, 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃₁, R_31’ and R_31’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃₂ 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃₂ and R_32’ are independently selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₄₁, R_41’ and R_41’’ are independently selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₅₁, R_51’ and R_51’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R51, R51’ and R51’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₆₁, 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R61, R61’ and R61’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₇₁, 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₇₁, R_71’ and R_71’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R81, R81’ and R81’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈₁, R_81’ and R_81’’ are independently selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R82, R82’ and R82’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈₂, R_82’ and R_82’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈₃, R_83’ and R_83’’ 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈₃, R_83’ and R_83’’ are independently selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, -OCH₂CH₂OR₂₁, - NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; wherein R₂₁, 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R3, if substituted, it is substituted with one or more substituent/s selected from–OR31, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31’; wherein the cycloalkyl in R₃, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R31, -OR31, -NO2, -NR31R31’, -NR31C(O)R31’, -NR31S(O)2R31’, -S(O)2NR31R31’, - NR31C(O)NR31’R31’’, -SR31 , -S(O)R31, -S(O)2R31, –CN, haloalkyl, haloalkoxy, -C(O)OR31, -C(O)NR31R31’, -OCH2CH2OR31, - NR₃₁S(O)₂NR_31’R_31’’ and -C(CH₃)₂OR₃₁; preferably selected from halogen, - R₃₁, -OR₃₁, -NR₃₁R_31’, -CN, haloalkyl and haloalkoxy;

wherein R₃₁, 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R3, if substituted, it is substituted with one or more substituent/s selected from–OR31, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31’; wherein the cycloalkyl in R3, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R31, -OR31, -NO2, -NR31R31’, -NR31C(O)R31’, -NR31S(O)2R31’, -S(O)2NR31R31’, - NR31C(O)NR31’R31’’, -SR31 , -S(O)R31, -S(O)2R31, –CN, haloalkyl, haloalkoxy, -C(O)OR31, -C(O)NR31R31’, -OCH2CH2OR31, - NR31S(O)2NR31’R31’’ and -C(CH3)2OR31; preferably selected from halogen, - R31, -OR31, -NR31R31’, -CN, haloalkyl and haloalkoxy; wherein R₃₁, R_31’ and R_31’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted cycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, it is substituted with one or more substituent/s selected from–OR₃₁, halogen, -CN, haloalkyl, haloalkoxy and -NR₃₁R_31’; wherein the cycloalkyl in R₃, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₃₁, -OR₃₁, -NO₂, -NR₃₁R_31’, -NR₃₁C(O)R_31’, -NR₃₁S(O)₂R_31’, -S(O)₂NR₃₁R_31’, - NR31C(O)NR31’R31’’, -SR31 , -S(O)R31, -S(O)2R31, –CN, haloalkyl, haloalkoxy, -C(O)OR31, -C(O)NR31R31’, -OCH2CH2OR31, - NR31S(O)2NR31’R31’’ and -C(CH3)2OR31; preferably selected from halogen, - R31, -OR31, -NR31R31’, -CN, haloalkyl and haloalkoxy;

wherein R31, R31’ and R31’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R3’ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R_3’, if substituted, it is substituted with one or more substituent/s selected from–OR₃₂, halogen, -CN, haloalkyl, haloalkoxy and -NR₃₂R_32’; wherein R₃₂ 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R3’ is selected from hydrogen and substituted or unsubstituted C1-6 alkyl; wherein, the alkyl, alkenyl or alkynyl defined in R3’, if substituted, it is substituted with one or more substituent/s selected from–OR32, halogen, -CN, haloalkyl, haloalkoxy and -NR32R32’; wherein R32 and R32’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₅, R_5’, R_5’’ and R_5’’’ are independently 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, R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

wherein the cycloalkyl, as defined in R₅-R_5’ and/or R_5’’-R_5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R51, -OR51, -NO2, -NR51R51’, -NR51C(O)R51’, -NR51S(O)2R51’, -S(O)2NR51R51’, - NR51C(O)NR51’R51’’, -SR51 , -S(O)R51, -S(O)2R51, –CN, haloalkyl, haloalkoxy, -C(O)OR51, -C(O)NR51R51’, -OCH2CH2OR51, - NR51S(O)2NR51’R51’’ and -C(CH3)2OR51; preferably selected from halogen, - R51, -OR51, -NR51R51’, -CN, haloalkyl and haloalkoxy; wherein R₅₁, R_51’ and R_51’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₅, R_5’, R_5’’ and R_5’’’ are independently selected from hydrogen, halogen and substituted or unsubstituted C_1-6 alkyl; alternatively, R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R5, R5’ R5’’ and R5’’’, if substituted, it is substituted with one or more substituent/s selected from–OR51, halogen, - CN, haloalkyl, haloalkoxy and–NR51R51’;

wherein the cycloalkyl, as defined in R5-R5’ and/or R5’’-R5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R51, -OR51, -NO2, -NR51R51’, -NR51C(O)R51’, -NR51S(O)2R51’, -S(O)2NR51R51’, - NR51C(O)NR51’R51’’, -SR51 , -S(O)R51, -S(O)2R51, –CN, haloalkyl, haloalkoxy, -C(O)OR51, -C(O)NR51R51’, -OCH2CH2OR51, - NR51S(O)2NR51’R51’’ and -C(CH3)2OR51; preferably selected from halogen, - R51, -OR51, -NR51R51’, -CN, haloalkyl and haloalkoxy; wherein R₅₁, R_51’ and R_51’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₆, R_6’, R_6’’ and R_6’’’ are independently 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, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R6, R6’ R6’’ and R6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR61, halogen, - CN, haloalkyl, haloalkoxy and–NR61R61’;

wherein the cycloalkyl, as defined in R6-R6’ and/or R6’’-R6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R61, -OR61, -NO2, -NR61R61’, -NR61C(O)R61’, -NR61S(O)2R61’, -S(O)2NR61R61’, - NR61C(O)NR61’R61’’, -SR61 , -S(O)R61, -S(O)2R61, –CN, haloalkyl, haloalkoxy, -C(O)OR61, -C(O)NR61R61’, -OCH2CH2OR61, - NR61S(O)2NR61’R61’’ and -C(CH3)2OR61; preferably selected from halogen, - R61, -OR61, -NR61R61’, -CN, haloalkyl and haloalkoxy; wherein R₆₁, R_61’ and R_61’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₆, R_6’, R_6’’ and R_6’’’ are independently selected from hydrogen, halogen and substituted or unsubstituted C_1-6 alkyl; alternatively, R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R6, R6’ R6’’ and R6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR61, halogen, - CN, haloalkyl, haloalkoxy and–NR61R61’;

wherein the cycloalkyl, as defined in R6-R6’ and/or R6’’-R6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R61, -OR61, -NO2, -NR61R61’, -NR61C(O)R61’, -NR61S(O)2R61’, -S(O)2NR61R61’, - NR61C(O)NR61’R61’’, -SR61 , -S(O)R61, -S(O)2R61, –CN, haloalkyl, haloalkoxy, -C(O)OR61, -C(O)NR61R61’, -OCH2CH2OR61, - NR61S(O)2NR61’R61’’ and -C(CH3)2OR61; preferably selected from halogen, - R61, -OR61, -NR61R61’, -CN, haloalkyl and haloalkoxy; wherein R₆₁, R_61’ and R_61’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR₇₁; wherein the alkyl, alkenyl or alkynyl defined in R₇, if substituted, it is substituted with one or more substituent/s selected from–OR71, halogen, -CN, haloalkyl, haloalkoxy and–NR71R71’; the aryl, heterocyclyl or cycloalkyl in R7, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R71, -OR71, -NO2, - NR71R71’, -NR71C(O)R71’, -NR71S(O)2R71’, -S(O)2NR71R71’, - NR71C(O)NR71’R71’’, -SR71 , -S(O)R71, -S(O)2R71, –CN, haloalkyl, haloalkoxy, -C(O)OR71, -C(O)NR71R71’, -OCH2CH2OR71, - NR71S(O)2NR71’R71’’ and -C(CH3)2OR71; wherein R71, R71’ and R71’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₇ is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and–C(O)OR₇₁; wherein the alkyl, alkenyl or alkynyl defined in R₇, if substituted, it is substituted with one or more substituent/s selected from–OR₇₁, halogen, -CN, haloalkyl, haloalkoxy and–NR₇₁R_71’; the aryl, heterocyclyl or cycloalkyl in R₇, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₇₁, -OR₇₁, -NO₂, - NR₇₁R_71’, -NR₇₁C(O)R_71’, -NR₇₁S(O)₂R_71’, -S(O)₂NR₇₁R_71’, - NR₇₁C(O)NR_71’R_71’’, -SR₇₁ , -S(O)R₇₁, -S(O)₂R₇₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₇₁, -C(O)NR₇₁R_71’, -OCH₂CH₂OR₇₁, - NR₇₁S(O)₂NR_71’R_71’’ and -C(CH₃)₂OR₇₁; wherein R71, R71’ and R71’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; wherein the aryl and heterocyclyl, as defined in R8, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R₈₁, -OR₈₁, -NO₂, -NR₈₁R_81’, -NR₈₁C(O)R_81’, - NR₈₁S(O)₂R_81’, -S(O)₂NR₈₁R_81’, - NR₈₁C(O)NR_81’R_81’’, -SR₈₁ , -S(O)R₈₁, - S(O)₂R₈₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₁, -C(O)NR₈₁R_81’, - OCH₂CH₂OR₈₁, -NR₈₁S(O)₂NR_81’R_81’’ and -C(CH₃)₂OR₈₁; wherein R₈₁, 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;

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; wherein the aryl and heterocyclyl, as defined in R8, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R81, -OR81, -NO2, -NR81R81’, -NR81C(O)R81’, - NR₈₁S(O)₂R_81’, -S(O)₂NR₈₁R_81’, - NR₈₁C(O)NR_81’R_81’’, -SR₈₁ , -S(O)R₈₁, - S(O)2R81, –CN, haloalkyl, haloalkoxy, -C(O)OR81, -C(O)NR81R81’, - OCH2CH2OR81, -NR81S(O)2NR81’R81’’ and -C(CH3)2OR81; wherein R81, R81’ and R81’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, - NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the alkyl, alkenyl or alkynyl defined in R8’, if substituted, it is substituted with one or more substituent/s selected from–OR₈₂, halogen, -CN, haloalkyl, haloalkoxy and–NR₈₂R_82’;

wherein the cycloalkyl, aryl and heterocyclyl, as defined in R8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R82, -OR82, -NO2, -NR82R82’, -NR82C(O)R82’, - NR82S(O)2R82’, -S(O)2NR82R82’, - NR82C(O)NR82’R82’’, -SR82 , -S(O)R82, - S(O)2R82, –CN, haloalkyl, haloalkoxy, -C(O)OR82, -C(O)NR82R82’, - OCH2CH2OR82, -NR82S(O)2NR82’R82’’ and -C(CH3)2OR82; wherein R₈₂, R_82’ and R_82’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, -NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the alkyl, alkenyl or alkynyl defined in R_8’, if substituted, it is substituted with one or more substituent/s selected from–OR82, halogen, -CN, haloalkyl, haloalkoxy and–NR82R82’;

wherein the cycloalkyl, aryl and heterocyclyl, as defined in R_8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R82, -OR82, -NO2, -NR82R82’, -NR82C(O)R82’, - NR82S(O)2R82’, -S(O)2NR82R82’, - NR82C(O)NR82’R82’’, -SR82 , -S(O)R82, - S(O)2R82, –CN, haloalkyl, haloalkoxy, -C(O)OR82, -C(O)NR82R82’, - OCH2CH2OR82, -NR82S(O)2NR82’R82’’ and -C(CH3)2OR82; wherein R82, R82’ and R82’’ are independently selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; wherein the cyclic amide or cyclic urea, as defined in R₈-R_8’ when taken together with the–N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₃, -OR₈₃, -NO₂, -NR₈₃R_83’, -NR₈₃C(O)R_83’, -NR₈₃S(O)₂R_83’, -S(O)₂NR₈₃R_83’, - NR₈₃C(O)NR_83’R_83’’, -SR₈₃ , -S(O)R₈₃, -S(O)₂R₈₃, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₃, -C(O)NR₈₃R_83’, -OCH₂CH₂OR₈₃, - NR83S(O)2NR83’R83’’ and -C(CH3)2OR83; wherein R83, R83’ and R83’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; wherein the cyclic amide or cyclic urea, as defined in R8-R8’ when taken together with the–N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₃, -OR₈₃, -NO₂, -NR₈₃R_83’, -NR₈₃C(O)R_83’, -NR₈₃S(O)₂R_83’, -S(O)₂NR₈₃R_83’, - NR₈₃C(O)NR_83’R_83’’, -SR₈₃ , -S(O)R₈₃, -S(O)₂R₈₃, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₃, -C(O)NR₈₃R_83’, -OCH₂CH₂OR₈₃, - NR₈₃S(O)₂NR_83’R_83’’ and -C(CH₃)₂OR₈₃; wherein R₈₃, R_83’ and R_83’’ are independently selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, -NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR21, -C(O)NR21R21’, -OCH2CH2OR21, - NR21S(O)2NR21’R21’’ and -C(CH3)2OR21; wherein R21, R21’ and R21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, -NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, -OCH₂CH₂OR₂₁, - NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; wherein R₂₁, R_21’ and R_21’’ are independently selected from hydrogen and substituted or unsubstituted C_1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from–OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13’; wherein R13 and R13’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R₁₄, -OR₁₄, -NO₂, -NR₁₄R_14’, - NR₁₄C(O)R_14’, -NR₁₄S(O)₂R_14’, -S(O)₂NR₁₄R_14’, - NR₁₄C(O)NR_14’R_14’’, -SR₁₄ , -S(O)R₁₄, - S(O)₂R₁₄,–CN, haloalkyl, haloalkoxy, -C(O)OR₁₄, -C(O)NR₁₄R_14’, -OCH₂CH₂OR₁₄, - NR₁₄S(O)₂NR_14’R_14’’ and -C(CH₃)₂OR₁₄; wherein R₁₄, 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; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein wherein the aryl or heterocyclyl in R₂, if substituted, it is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, - NR21R21’, -NR21C(O)R21’, -NR21S(O)2R21’, -S(O)2NR21R21’, - NR21C(O)NR21’R21’’, -SR21 , -S(O)R21, -S(O)2R21, –CN, haloalkyl, haloalkoxy, -C(O)OR21, -C(O)NR21R21’, -OCH2CH2OR21, - NR21S(O)2NR21’R21’’ and -C(CH3)2OR21; wherein R₂₁, R_21’ and R_21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R₃, if substituted, it is substituted with one or more substituent/s selected from–OR₃₁, halogen, -CN, haloalkyl, haloalkoxy and -NR₃₁R_31’; wherein the cycloalkyl in R₃, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₃₁, -OR₃₁, -NO₂, -NR₃₁R_31’, -NR₃₁C(O)R_31’, -NR₃₁S(O)₂R_31’, -S(O)₂NR₃₁R_31’, - NR₃₁C(O)NR_31’R_31’’, -SR₃₁ , -S(O)R₃₁, -S(O)₂R₃₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₃₁, -C(O)NR₃₁R_31’, -OCH₂CH₂OR₃₁, - NR31S(O)2NR31’R31’’ and -C(CH3)2OR31; preferably selected from halogen, - R31, -OR31, -NR31R31’, -CN, haloalkyl and haloalkoxy;

wherein R₃₁, 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 C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R3’, if substituted, it is substituted with one or more substituent/s selected from–OR32, halogen, -CN, haloalkyl, haloalkoxy and -NR32R32’; wherein R₃₂ 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R₅, R_5’ R_5’’ and R_5’’’, if substituted, it is substituted with one or more substituent/s selected from–OR₅₁, halogen, - CN, haloalkyl, haloalkoxy and–NR₅₁R_51’;

wherein the cycloalkyl, as defined in R₅-R_5’ and/or R_5’’-R_5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₅₁, -OR₅₁, -NO₂, -NR₅₁R_51’, -NR₅₁C(O)R_51’, -NR₅₁S(O)₂R_51’, -S(O)₂NR₅₁R_51’, - NR51C(O)NR51’R51’’, -SR51 , -S(O)R51, -S(O)2R51, –CN, haloalkyl, haloalkoxy, -C(O)OR51, -C(O)NR51R51’, -OCH2CH2OR51, - NR51S(O)2NR51’R51’’ and -C(CH3)2OR51; preferably selected from halogen, - R51, -OR51, -NR51R51’, -CN, haloalkyl and haloalkoxy; wherein R51, R51’ and R51’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R₆,

R_6’’ and R_6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR₆₁, halogen, - CN, haloalkyl, haloalkoxy and–NR₆₁R_61’;

wherein the cycloalkyl, as defined in R₆-R_6’ and/or R_6’’-R_6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, - R₆₁, -OR₆₁, -NO₂, -NR₆₁R_61’, -NR₆₁C(O)R_61’, -NR₆₁S(O)₂R_61’, -S(O)₂NR₆₁R_61’, - NR₆₁C(O)NR_61’R_61’’, -SR₆₁ , -S(O)R₆₁, -S(O)₂R₆₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₆₁, -C(O)NR₆₁R_61’, -OCH₂CH₂OR₆₁, - NR₆₁S(O)₂NR_61’R_61’’ and -C(CH₃)₂OR₆₁; preferably selected from halogen, - R₆₁, -OR₆₁, -NR₆₁R_61’, -CN, haloalkyl and haloalkoxy; wherein R₆₁, 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 C2-6 alkynyl;

optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R7, if substituted, it is substituted with one or more substituent/s selected from–OR71, halogen, -CN, haloalkyl, haloalkoxy and–NR71R71’; the aryl, heterocyclyl or cycloalkyl in R₇, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₇₁, -OR₇₁, -NO₂, - NR₇₁R_71’, -NR₇₁C(O)R_71’, -NR₇₁S(O)₂R_71’, -S(O)₂NR₇₁R_71’, - NR₇₁C(O)NR_71’R_71’’, -SR₇₁ , -S(O)R₇₁, -S(O)₂R₇₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₇₁, -C(O)NR₇₁R_71’, -OCH₂CH₂OR₇₁, - NR₇₁S(O)₂NR_71’R_71’’ and -C(CH₃)₂OR₇₁; wherein R₇₁, 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the aryl and heterocyclyl, as defined in R8, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R81, -OR81, -NO2, -NR81R81’, -NR81C(O)R81’, - NR81S(O)2R81’, -S(O)2NR81R81’, - NR81C(O)NR81’R81’’, -SR81 , -S(O)R81, - S(O)2R81, –CN, haloalkyl, haloalkoxy, -C(O)OR81, -C(O)NR81R81’, - OCH2CH2OR81, -NR81S(O)2NR81’R81’’ and -C(CH3)2OR81; wherein R₈₁, R_81’ and R_81’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R_8’, if substituted, it is substituted with one or more substituent/s selected from–OR₈₂, halogen, -CN, haloalkyl, haloalkoxy and–NR₈₂R_82’; wherein the cycloalkyl, aryl and heterocyclyl, as defined in R_8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₂, -OR₈₂, -NO₂, -NR₈₂R_82’, -NR₈₂C(O)R_82’, - NR₈₂S(O)₂R_82’, -S(O)₂NR₈₂R_82’, - NR₈₂C(O)NR_82’R_82’’, -SR₈₂ , -S(O)R₈₂, - S(O)₂R₈₂, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₂, -C(O)NR₈₂R_82’, - OCH2CH2OR82, -NR82S(O)2NR82’R82’’ and -C(CH3)2OR82; wherein R82, R82’ and R82’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the cyclic amide or cyclic urea, as defined in R₈-R_8’ when taken together with the–N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R83, - OR83, -NO2, -NR83R83’, -NR83C(O)R83’, -NR83S(O)2R83’, -S(O)2NR83R83’, - NR83C(O)NR83’R83’’, -SR83 , -S(O)R83, -S(O)2R83, –CN, haloalkyl, haloalkoxy, -C(O)OR₈₃, -C(O)NR₈₃R_83’, -OCH₂CH₂OR₈₃, - NR₈₃S(O)₂NR_83’R_83’’ and -C(CH₃)₂OR₈₃; wherein R₈₃, R_83’ and R_83’’ 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from–OR13, halogen, -CN, haloalkyl, haloalkoxy and -NR₁₃R_13’; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from =O, halogen, -R₁₄, -OR₁₄, -NO₂, -NR₁₄R_14’, - NR14C(O)R14’, -NR14S(O)2R14’, -S(O)2NR14R14’, - NR14C(O)NR14’R14’’, -SR14 , -S(O)R14, - S(O)2R14,–CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14’, -OCH2CH2OR14, - NR14S(O)2NR14’R14’’ and -C(CH3)2OR14; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the aryl or heterocyclyl in R₂, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₂₁, -OR₂₁, -NO₂, -NR₂₁R_21’, -NR₂₁C(O)R_21’, - NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, -OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH3)2OR21; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R3, if substituted, it is substituted with one or more substituent/s selected from–OR31, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31’; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl in R₃, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R₃₁, -OR₃₁, -NO₂, -NR₃₁R_31’, - NR₃₁C(O)R_31’, -NR₃₁S(O)₂R_31’, -S(O)₂NR₃₁R_31’, - NR₃₁C(O)NR_31’R_31’’, -SR₃₁ , -S(O)R₃₁, - S(O)₂R₃₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₃₁, -C(O)NR₃₁R_31’, -OCH₂CH₂OR₃₁, - NR₃₁S(O)₂NR_31’R_31’’ and -C(CH₃)₂OR₃₁; preferably selected from halogen, -R₃₁, -OR₃₁, -NR₃₁R_31’, -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl in R₃, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₃₁, -OR₃₁, -NR₃₁R_31’, -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R3’, if substituted, it is substituted with one or more substituent/s selected from–OR32, halogen, -CN, haloalkyl, haloalkoxy and - NR₃₂R_32’; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R₅, R_5’ R_5’’ and R_5’’’, if substituted, it is substituted with one or more substituent/s selected from–OR₅₁, halogen, -CN, haloalkyl, haloalkoxy and–NR₅₁R_51’; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl, as defined in R5-R5’ and/or R5’’-R5’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R51, -OR51, -NO2, -NR51R51’, - NR51C(O)R51’, -NR51S(O)2R51’, -S(O)2NR51R51’, - NR51C(O)NR51’R51’’, -SR51 , -S(O)R51, - S(O)2R51,–CN, haloalkyl, haloalkoxy, -C(O)OR51, -C(O)NR51R51’, -OCH2CH2OR51, - NR51S(O)2NR51’R51’’ and -C(CH3)2OR51; preferably selected from halogen, -R51, -OR51, -NR51R51’, -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl, as defined in R₅-R_5’ and/or R_5’’-R_5’’’, if substituted, is substituted with one or more substituent/s selected from selected from halogen, -R₅₁, -OR₅₁, -NR₅₁R_51’, -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R6, R6’ R6’’ and R6’’’, if substituted, it is substituted with one or more substituent/s selected from–OR61, halogen, -CN, haloalkyl, haloalkoxy and–NR₆₁R_61’; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl, as defined in R₆-R_6’ and/or R_6’’-R_6’’’, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R61, -OR61, -NO2, -NR61R61’, - NR61C(O)R61’, -NR61S(O)2R61’, -S(O)2NR61R61’, - NR61C(O)NR61’R61’’, -SR61 , -S(O)R61, - S(O)2R61,–CN, haloalkyl, haloalkoxy, -C(O)OR61, -C(O)NR61R61’, -OCH2CH2OR61, - NR61S(O)2NR61’R61’’ and -C(CH3)2OR61; preferably selected from halogen, -R61, -OR61, -NR₆₁R_61’, -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl, as defined in R₆-R_6’ and/or R_6’’-R_6’’’, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₆₁, -OR₆₁, -NR₆₁R_61’, -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R7, if substituted, it is substituted with one or more substituent/s selected from–OR71, halogen, -CN, haloalkyl, haloalkoxy and–NR71R71’; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the aryl, heterocyclyl or cycloalkyl in R7, if substituted, it is substituted with one or more substituent/s selected from =O, halogen, -R71, -OR71, -NO2, -NR71R71’, -NR71C(O)R71’, - NR₇₁S(O)₂R_71’, -S(O)₂NR₇₁R_71’, - NR₇₁C(O)NR_71’R_71’’, -SR₇₁ , -S(O)R₇₁, -S(O)₂R₇₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₇₁, -C(O)NR₇₁R_71’, -OCH₂CH₂OR₇₁, -NR₇₁S(O)₂NR_71’R_71’’ and -C(CH₃)₂OR₇₁; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the aryl and heterocyclyl, as defined in R₈, if substituted, it is substituted with one or more substituent/s selected from substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted cycloalkyl, halogen, -R81, - OR81, -NO2, -NR81R81’, -NR81C(O)R81’, -NR81S(O)2R81’, -S(O)2NR81R81’, - NR₈₁C(O)NR_81’R_81’’, -SR₈₁ , -S(O)R₈₁, -S(O)₂R₈₁, –CN, haloalkyl, haloalkoxy, - C(O)OR₈₁, -C(O)NR₈₁R_81’, -OCH₂CH₂OR₈₁, -NR₈₁S(O)₂NR_81’R_81’’ and -C(CH₃)₂OR₈₁; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R_8’, if substituted, it is substituted with one or more substituent/s selected from–OR82, halogen, -CN, haloalkyl, haloalkoxy and– NR82R82’; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl, aryl and heterocyclyl, as defined in R_8’, also in alkylcycloalkyl, if substituted, it is substituted with one or more substituent/s selected from halogen, -R₈₂, -OR₈₂, -NO₂, -NR₈₂R_82’, -NR₈₂C(O)R_82’, -NR₈₂S(O)₂R_82’, -S(O)₂NR₈₂R_82’, - NR₈₂C(O)NR_82’R_82’’, -SR₈₂ , -S(O)R₈₂, -S(O)₂R₈₂, –CN, haloalkyl, haloalkoxy, - C(O)OR₈₂, -C(O)NR₈₂R_82’, -OCH₂CH₂OR₈₂, -NR₈₂S(O)₂NR_82’R_82’’ and -C(CH₃)₂OR₈₂; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein the cyclic amide or cyclic urea, as defined in R8-R8’ when taken together with the– N(CO)- atoms to which they are attached, if substituted, it is substituted with one or more substituent/s selected from halogen, -R83, -OR83, -NO2, -NR83R83’, -NR83C(O)R83’, -NR83S(O)2R83’, -S(O)2NR83R83’, - NR83C(O)NR83’R83’’, -SR83 , -S(O)R83, -S(O)2R83,–CN, haloalkyl, haloalkoxy, -C(O)OR₈₃, -C(O)NR₈₃R_83’, -OCH₂CH₂OR₈₃, -NR₈₃S(O)₂NR_83’R_83’’ and -C(CH3)2OR83; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein X is a bond, -[C(R_aR_b)]_p-, -[C(R_aR_b)]_pC(O)[C(R_cR_d)]_q-, -[C(R_aR_b)]_pC(O)N(R_z)[C(R_cR_d)]_q- , [C(R_aR_b)]_pN(R_z)C(O)[C(R_cR_d)]_q- or -[C(R_aR_b)]_pN(R_z)[C(R_cR_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 alkylcycloalkyl and - C(O)-C_1-6 alkyl; R_a is selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; Rb is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl;

Rc is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R_d is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein X is a bond, -[C(R_aR_b)]_p-, -[C(R_aR_b)]_pC(O)[C(R_cR_d)]_q-, -[C(R_aR_b)]_pC(O)N(R_z)[C(R_cR_d)]_q- , [C(R_aR_b)]_pN(R_z)C(O)[C(R_cR_d)]_q- or -[C(R_aR_b)]_pN(R_z)[C(R_cR_d)]_q-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein Rz is selected from hydrogen, substituted or unsubstituted C1-6 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein Ra is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the 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 C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein Ra and Rb, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein Rc is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein R_d 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH2]pN(Rz)C(O)[CH2]q- and -[CH2]pN(Rz)[CH2]q-; preferably X is selected from a bond, -[C(RaRb)]p- and -[CH2]pN(Rz)C(O)[CH2]q- ; more preferably selected from a bond, -CH2- , -CH(CH3)-, -CH2CH2- and -NHC(O)CH2-; and/or R1 is

and/or Rz is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(O)-C1-6 alkyl;preferably Rz is selected from hydrogen; 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 q is 1; and/or Y₁ is–C(R₁₀R_10’)-; preferably Y₁ is–CH₂-; and/or Y₂ is–C(R₁₀R_10’)-; preferably Y₂ is–CH₂-; and/or n is 0 or 1; preferably n is 0; and/or R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, preferably R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, more preferably R₂ is a substituted or unsubstituted group selected from phenyl and thiophen; and/or R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;preferably R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted cycloalkyl; more preferably R₃ is hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl or substituted or unsubstituted cyclopropyl; 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; preferably R_3’ is hydrogen; and/or R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)2R41,–CN, haloalkyl, haloalkoxy, -C(O)OR41, -C(O)NR41R41’, -OCH2CH2OR41, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; preferably R4 and R4’ are both hydrogen; and/or R₅, R_5’, R_5’’ and R_5’’’ are independently 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 R₅, R_5’, R_5’’ and R_5’’’ are all hydrogen; alternatively, R5 and R5’ and/or R5’’ and R5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; and/or R₆, R_6’, R_6’’ and R_6’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R6, R6’, R6’’ and R6’’’ are all hydrogen; alternatively, R6 and R6’ and/or R6’’ and R6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; and/or

R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and–C(O)OR₇₁; preferably R₇ is hydrogen;

and/or R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; preferably R₈ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; more preferably R₈ is selected from substituted or unsubstituted phenyl, substituted or unsubstituted pyridine and pyrazole; and/or R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, -NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; preferably R_8’ is selected from substituted or unsubstituted C1-6 alkyl and substituted or unsubstituted heterocyclyl; more preferably, R8’ is selected from substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted thiophen and substituted or unsubstituted furan; and/or R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; preferably R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted indoline-2-one or substituted or unsubstituted 1H- benzo[d]imidazol-2(3H)-one; and/or R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, - OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; preferably R₉ and R_9’ are both hydrogen; and/or R₁₀ 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 R₁₀ and R_10’ are both hydrogen; alternatively, R₁₀ and R_10’ form, with the carbon atom to which they are attached, 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 R_10’’ and R_10’’’ are both hydrogen; alternatively, R10’’ and R10’’’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

and/or R₁₃ and R_13’ are independently selected from hydrogen, unsubstituted C_1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl; and/or R14, R14’ and R14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; and/or R₂₁, 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 R₃₁, 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; and/or R₃₂ and R_32’ are independently selected from hydrogen, substituted or unsubstituted C_1- 6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; and/or R₄₁, R_41’ and R_41’’ 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 R₄₁ is hydrogen or substituted or unsubstituted methyl; and/or R51, R51’ and R51’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; and/or R61, R61’ and R61’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; and/or R₇₁, 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 R₈₁, 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; and/or R₈₂, R_82’ and R_82’’ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R82 is substituted or unsubstituted methyl; and/or R83, R83’ and R83’’ 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 R₈₃ is substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein X is selected from a bond, -[C(RaRb)]p-, -[CH2]pC(O)[CH2]q-, -[CH2]pC(O)N(Rz)[CH2]q-, - [CH2]pN(Rz)C(O)[CH2]q- and -[CH2]pN(Rz)[CH2]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 is 0 or 1; and/or Y₁ is–C(R₁₀R_10’)-; and/or Y₂ is–C(R_10’’R_10’’’)-; and/or

R₁ is

and/or m is 0, 1 or 2; and/or r is 0, 1 or 2; and/or Ra is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; wherein 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; and/or the C_2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

and/or

Rb is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; wherein the C1-6 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

or R_a and R_b, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;

and/or Rz is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(O)-C_1-6 alkyl; wherein the alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably the heterocyclyl is thiophen; and/or

R₃ 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, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein the alkyl is C_1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl or ethyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; ; more preferably the cycloalkyl is cyclopropyl;

and/or

R_3’ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

wherein the C_1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or R4 and R4’ are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR₄₁S(O)₂NR_41’R_41’’ and -C(CH₃)₂OR₄₁; wherein the alkyl is C_1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl;

and/or

R₅, R_5’, R_5’’ and R_5’’’ are independently 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 C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; or

R5 and R5’ and/or R5’’ and R5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;

and/or R₆, R_6’, R_6’’ and R_6’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; wherein the C_1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl;

wherein

the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;

and/or R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and–C(O)OR71; wherein the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; and/or

R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; wherein the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; more preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably the heterocyclyl is pyridine or pyrazole;

and/or

R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, -NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl or ethyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably the heterocyclyl is thiophen or furan;

or R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; wherein the cyclic amide is formed through the cyclization of a carbon sequence, containing at least the sequence

forming part of the cycle, said cyclic amide being optionally fused to a ring system; preferably the cyclic amide is indoline-2-one; and/or

the cyclic urea is formed through the cyclization of a carbon sequence containing at least the sequence

forming part of the cycle, said cyclic urea being optionally fused to a ring system; preferably the cyclic urea is 1H-benzo[d]imidazol-2(3H)-one; and/or

R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, - OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; wherein the alkyl is C_1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl; and/or

R10 and R10’ 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; 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

or R10 and R10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; or

R10’’ and R10’’’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; wherein

the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or R₁₃ and R_13’ are independently selected from hydrogen, unsubstituted 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, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C_2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or R14, R14’ and R14’’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; wherein

the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; and/or R₂₁, 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

and/or R31, R31’ and R31’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

and/or

R₃₂ 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 C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 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; preferably the C_1- ₆ alkyl is methyl; and/or the C_2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

and/or

R51, R51’ and R51’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; wherein the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

and/or

R₆₁, 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, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C1-6 alkyl is methyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or R₇₁, 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 C2-6 alkynyl; wherein

the C_1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or

R81, R81’ and R81’’ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; wherein

the C_1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or R₈₂, R_82’ and R_82’’ 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; more preferably the C_1-6 alkyl is methyl; wherein

the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or R83, R83’ and R83’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; more preferably the C1-6 alkyl is methyl;

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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R_a as defined in any of the embodiments of the present invention, the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in Rb as defined in any of the embodiments of the present invention, the C1-6 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in Ra-Rb as defined in any of the embodiments of the present invention, the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in Rz as defined in any of the embodiments of the present invention, the alkyl is C_1-6 alkyl like 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₂ as defined in any of the embodiments of the present invention, the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably the heterocyclyl is thiophen;

optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R3 as defined in any of the embodiments of the present invention, the alkyl is C1-6 alkyl like 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; ; more preferably the cycloalkyl is cyclopropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R3’ as defined in any of the embodiments of the present invention, the C1-6 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R4 and R4’as defined in any of the embodiments of the present invention, the alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₅, R_5’, R_5’’ and R_5’’’ as defined in any of the embodiments of the present invention, 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R5 and R5’ and/or R5’’ and R5’’’ as defined in any of the embodiments of the present invention, the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R6, R6’, R6’’ and R6’’’ as defined in any of the embodiments of the present invention, 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R6 and R6’ and/or R6’’ and R6’’’ as defined in any of the embodiments of the present invention, the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₇ as defined in any of the embodiments of the present invention, 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₈ as defined in any of the embodiments of the present invention, the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; more preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably the heterocyclyl is pyridine or pyrazole; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the 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 alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl or ethyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline; preferably the heterocyclyl is thiophen or furan; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₈ and R_8’ as defined in any of the embodiments of the present invention, the cyclic amide is formed through the cyclization of a carbon sequence, containing at least the sequence

forming part of the cycle, said cyclic urea being optionally fused to a ring system; preferably the cyclic urea is 1H-benzo[d]imidazol-2(3H)-one; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R9 and R9’ as defined in any of the embodiments of the present invention, the alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2- methylpropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₁₀ and R_10’ as defined in any of the embodiments of the present invention, 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R10 and R10’ as defined in any of the embodiments of the present invention, the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the 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 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R10’’ and R10’’’ as defined in any of the embodiments of the present invention, the cycloalkyl is C_3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C_3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C_3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R13 and R13’ as defined in any of the embodiments of the present invention, the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₁₄, R_14’ and R_14’’ as defined in any of the embodiments of the present invention, 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which 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 is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, 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 oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole, indoline-2-one and quinazoline;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R21, R21’ and R21’’ as defined in any of the embodiments of the present invention,

the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C1-6 alkyl is methyl, ethyl or propyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₃₁, R_31’ and R_31’’ as defined in any of the embodiments of the present invention,

the C_1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R32 and R32’ as defined in any of the embodiments of the present invention,

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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R41, R41’ and R41’’ as defined in any of the embodiments of the present invention,

the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C1-6 alkyl is methyl; preferably the C1- 6 alkyl is methyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₅₁, R_51’ and R_51’’ as defined in any of the embodiments of the present invention,

the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₆₁, R_61’ and R_61’’ as defined in any of the embodiments of the present invention,

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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R71, R71’ and R71’’ as defined in any of the embodiments of the present invention, 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R81, R81’ and R81’’ as defined in any of the embodiments of the present invention,

the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl,pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₈₂, R_82’ and R_82’’ as defined in any of the embodiments of the present invention,

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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R83, R83’ and R83’’ as defined in any of the embodiments of the present invention,

the C1-6 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 ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C_2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein p is 0, 1, 2, 3, 4 or 5; preferably p is 0, 1 or 2; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein q is 0, 1, 2, 3, 4 or 5; preferably q is 1; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein n is 0 or 1; preferably n is 0; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-; preferably X is selected from a bond, -[C(R_aR_b)]_p- and -[CH₂]_pN(R_z)C(O)[CH₂]_q- ; more preferably selected from a bond, -CH₂- , -CH(CH3)-, -CH2CH2- and -NHC(O)CH2-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein Ra is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably, R_a is selected from hydrogen and substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein Y₁ is–C(R₁₀R_10’)-; preferably Y₁ is–CH₂-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein Y₂ is–C(R₁₀R_10’)-; preferably Y₂ is–CH₂-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein Rz is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(O)-C1-6 alkyl;preferably R_z is selected from hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, preferably R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, more preferably R₂ is a substituted or unsubstituted group selected from phenyl and thiophen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;preferably R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl and substituted or unsubstituted cycloalkyl; more preferably R₃ is hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl or substituted or unsubstituted cyclopropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the 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 C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; preferably R_3’ is hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR₄₁C(O)R_41’, -NR₄₁S(O)₂R_41’, -S(O)₂NR₄₁R_41’, -NR₄₁C(O)NR_41’R_41’’, -SR₄₁ , -S(O)R₄₁, - S(O)₂R₄₁,–CN, haloalkyl, haloalkoxy, -C(O)OR₄₁, -C(O)NR₄₁R_41’, -OCH₂CH₂OR₄₁, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; preferably R4 is fluorine or methyl while R4’ is hydrogen, more preferably R4 and R4’ are both hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R5, R5’, R5’’ and R5’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; preferably R₅, R_5’, R_5’’ and R_5’’’ are all hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₅ and R_5’ and/or R_5’’ and R_5’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R6, R6’, R6’’ and R6’’’ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R6, R6’, R6’’ and R6’’’ are all hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₆ and R_6’ and/or R_6’’ and R_6’’’ taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₇ 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, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and–C(O)OR71; preferably R7 is hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; preferably R8 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; more preferably R₈ is selected from substituted or unsubstituted phenyl, substituted or unsubstituted pyridine and pyrazole; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R_8’ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, -NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; preferably R_8’ is selected from substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted heterocyclyl; more preferably, R_8’ is selected from substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted thiophen and substituted or unsubstituted furan; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or a substituted or unsubstituted cyclic urea; preferably R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted indoline-2-one or a substituted or unsubstituted 1H- benzo[d]imidazol-2(3H)-one; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₉ and R_9’ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, - OCH₂CH₂OR₂₁, -NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; preferably R₉ and R_9’ are both hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₁₀ 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 R₁₀ and R_10’ are both hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R10 and R10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the 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 R_10’’ and R_10’’’ are both hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R_10’’ and R_10’’’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R13 and R13’ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₁₄, 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; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R21, R21’ and R21’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₃₁, 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₃₂ and R_32’ are independently selected from hydrogen, substituted or unsubstituted C_1- 6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R41, R41’ and R41’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; preferably R₄₁ is hydrogen or substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₅₁, 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 in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₆₁, 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R71, R71’ and R71’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₈₁, 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R82, R82’ and R82’’ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R82 is substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R83, R83’ and R83’’ 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 R₈₃ is substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein p is 0, 1 or 2; and/or q is 1; and/or n is 0; and/or m is 1; and/or r is 1; and/or X is selected from a a bond, -CH2-, -CH(CH3)-, -CH2CH2- and -NHC(O)CH2-; and/or Y₁ is–CH₂-; and/or Y2 is–CH2- ; and/or R_a is hydrogen or substituted or unsubstituted methyl; and/or R_b is hydrogen and/or R_z is hydrogen; and/or

R₁ is

and/or R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, more preferably R₂ is a substituted or unsubstituted group selected from phenyl and thiophen; and/or R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted cycloalkyl; more preferably R₃ is hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl or substituted or unsubstituted cyclopropyl; and/or R_3’ is hydrogen; and/or R₄ is hydrogen; and/or R₄ is substituted or unsubstituted C_1-6 alkyl; preferably R₄ is substituted or unsubstituted methyl; and/or R₄ is halogen, preferably fluorine; and/or R_4’ is hydrogen; and/or R₄ is substituted or unsubstituted C_1-6 alkyl; preferably R₄ is substituted or unsubstituted methyl, while R_4’ is hydrogen; and/or R₄ is halogen, preferably fluorine, while R_4’ is hydrogen; and/or R₄ and R_4’ are both hydrogen; and/or R₅ is selected from halogen and hydrogen; preferably from fluorine and hydrogen; and/or

R5’, R5’’ and R5’’’ are all hydrogen; and/or R₆, R_6’, R_6’’ and R_6’’’ are all hydrogen; and/or R₇ is hydrogen; and/or R₈ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; more preferably R₈ is selected from substituted or unsubstituted phenyl, substituted or unsubstituted pyridine and substituted or unsubstituted pyrazole; and/or R_8’ is selected from substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted heterocyclyl; more preferably, R_8’ is selected from substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted thiophen and substituted or unsubstituted furan; and/or R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted indoline-2-one or substituted or unsubstituted 1H- benzo[d]imidazol-2(3H)-one; and/or R₉ and R_9’ are selected from halogen and hydrogen; preferably from fluorine and hydrogen; and/or R10 and R10’ are both hydrogen; and/or R10’’ and R10’’’ are both hydrogen; and/or R₄₁ is selected from substituted or unsubstituted C_1-6 alkyl and hydrogen; preferably from from substituted or unsubstituted methyl and hydrogen; and/or R₈₂ is substituted or unsubstituted C_1-6 alkyl; preferably substituted or unsubstituted methyl; and/or R₈₃ is substituted or unsubstituted C_1-6 alkyl; preferably substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In a preferred embodiment p is 0, 1 or 2. In a preferred embodiment q is 1. In a preferred embodiment n is 0. In a preferred embodiment m is 1. In a preferred embodiment r is 1. In a preferred embodiment

m is 1 and r is 1.

In a preferred embodiment

X is selected from a a bond, -CH2-, -CH(CH3)-, -CH2CH2- and -NHC(O)CH2-. In a preferred embodiment

R_a is hydrogen or substituted or unsubstituted methyl.

In a preferred embodiment

R_b is hydrogen.

In a preferred embodiment

R_a is hydrogen or substituted or unsubstituted methyl, while R_b is hydrogen. In a preferred embodiment

R_a is substituted or unsubstituted methyl, while R_b is hydrogen. In a preferred embodiment

R_a and R_b are both hydrogen. In a preferred embodiment

In a preferred embodiment

In a preferred embodiment Y₁ is–CH₂-. In a preferred embodiment Y₂ is–CH₂-.

In a preferred embodiment Y1 and Y2 are both–CH2-. In a preferred embodiment R_z is hydrogen. In a preferred embodiment R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, more preferably R₂ is a substituted or unsubstituted group selected from phenyl and thiophen. In a preferred embodiment R3 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl and substituted or unsubstituted cycloalkyl; more preferably R3 is hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl or substituted or unsubstituted cyclopropyl. In a preferred embodiment R₃ is selected from substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted cycloalkyl; more preferably R₃ is substituted or unsubstituted methyl, substituted or unsubstituted ethyl or substituted or unsubstituted cyclopropyl.

In a preferred embodiment R_3’ is hydrogen. In a preferred embodiment R₃ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted cycloalkyl; more preferably R₃ is hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl or substituted or unsubstituted cyclopropyl, while R_3’ is hydrogen. In a preferred embodiment R3 is substituted or unsubstituted C1-6 alkyl; more preferably R3 is substituted or unsubstituted methyl, while R3’ is hydrogen. In a preferred embodiment R₃ is substituted or unsubstituted C_1-6 alkyl; more preferably R₃ is substituted or unsubstituted ethyl, while R_3’ is hydrogen. In a preferred embodiment R3 is substituted or unsubstituted cycloalkyl; more preferably R3 is substituted or unsubstituted cyclopropyl, while R3’ is hydrogen. In a preferred embodiment R3 and R3’ are both hydrogen. In a preferred embodiment R4 is hydrogen. In a preferred embodiment R₄ is substituted or unsubstituted C_1-6 alkyl; preferably R₄ is substituted or unsubstituted methyl. In a preferred embodiment R₄ is halogen, preferably fluorine. In a preferred embodiment R_4’ is hydrogen. In a preferred embodiment R₄ is substituted or unsubstituted C_1-6 alkyl; preferably R₄ is substituted or unsubstituted methyl, while R_4’ is hydrogen. In a preferred embodiment R₄ is halogen, preferably fluorine, while R_4’ is hydrogen. In a preferred embodiment R₄ and R_4’ are both hydrogen. In a preferred embodiment R5 is selected from fluorine and hydrogen. In a preferred embodiment R_5’, R_5’’ and R_5’’’ are all hydrogen. In a preferred embodiment R5 is fluorine, while R5’, R5’’ and R5’’’ are all hydrogen. In a preferred embodiment R5, R5’, R5’’ and R5’’’ are all hydrogen. In a preferred embodiment R₆, R_6’, R_6’’ and R_6’’’ are all hydrogen. In a preferred embodiment R₇ is hydrogen. In a preferred embodiment R₈ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; more preferably R₈ is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; even more preferably R₈ is selected from substituted or unsubstituted phenyl, substituted or unsubstituted pyridine and substituted or unsubstituted pyrazole. In a preferred embodiment R_8’ is selected from substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted heterocyclyl; more preferably, R_8’ is selected from substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted thiophen and substituted or unsubstituted furan.

In a preferred embodiment R8 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; more preferably R8 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; even more preferably R8 is selected from substituted or unsubstituted phenyl, substituted or unsubstituted pyridine and substituted or unsubstituted pyrazole, while R8’ is selected from substituted or unsubstituted C1-6 alkyl and substituted or unsubstituted heterocyclyl; more preferably, R8’ is selected from substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted thiophen and substituted or unsubstituted furan.

In a preferred embodiment R₈ is substituted or unsubstituted aryl; more preferably R₈ is substituted or unsubstituted phenyl, while R_8’ is selected from substituted or unsubstituted C_1-6 alkyl and substituted or unsubstituted heterocyclyl; more preferably, while R_8’ is selected from substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted thiophen and substituted or unsubstituted furan.

In a preferred embodiment R₈ is substituted or unsubstituted heterocyclyl; preferably R₈ is substituted or unsubstituted aromatic heterocyclyl; more preferably R₈ is selected from substituted or unsubstituted pyridine and substituted or unsubstituted pyrazole, while R8’ is substituted or unsubstituted C1-6 alkyl; more preferably, R8’ is substituted or unsubstituted ethyl.

In a preferred embodiment R₈ is substituted or unsubstituted aryl; more preferably R₈ is substituted or unsubstituted phenyl, while R_8’ is substituted or unsubstituted C_1-6 alkyl; more preferably, R8’ is substituted or unsubstituted methyl.

In a preferred embodiment R₈ is substituted or unsubstituted aryl; more preferably R₈ is substituted or unsubstituted phenyl, while R8’ is substituted or unsubstituted C1-6 alkyl; more preferably, R8’ is substituted or unsubstituted ethyl.

In a preferred embodiment R₈ is substituted or unsubstituted aryl; more preferably R₈ is substituted or unsubstituted phenyl, while R_8’ is substituted or unsubstituted heterocyclyl; more preferably, R_8’ is substituted or unsubstituted thiophen. In a preferred embodiment R₈ is substituted or unsubstituted aryl; more preferably R₈ is substituted or unsubstituted phenyl, while R_8’ is substituted or unsubstituted heterocyclyl; more preferably, R_8’ is substituted or unsubstituted furan.

In a preferred embodiment R₈ is substituted or unsubstituted heterocyclyl; preferably R₈ is substituted or unsubstituted aromatic heterocyclyl; more preferably R₈ is substituted or unsubstituted pyridine, while R8’ is substituted or unsubstituted C1-6 alkyl; more preferably, R8’ is substituted or unsubstituted ethyl. In a preferred embodiment R₈ is substituted or unsubstituted heterocyclyl; preferably R₈ is substituted or unsubstituted aromatic heterocyclyl; more preferably R₈ is substituted or unsubstituted pyrazole, while R_8’ is substituted or unsubstituted C_1-6 alkyl; more preferably, R_8’ is substituted or unsubstituted ethyl.

In a preferred embodiment R₈ and R_8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted indolin-2-one or substituted or unsubstituted 1H- benzo[d]imidazol-2(3H)-one. In a preferred embodiment R9 is selected from fluorine and hydrogen. In a preferred embodiment R₉’ is hydrogen. In a preferred embodiment R₉ is fluorine while R₉’ is hydrogen. In a preferred embodiment R₉ and R_9’ are both hydrogen. In a preferred embodiment R₁₀ and R_10’ are both hydrogen. In a preferred embodiment R_10’’ and R_10’’’ are both hydrogen. In a preferred embodiment R10, R10’, R10’’ and R10’’’ are all hydrogen.

In a preferred embodiment R₄₁ is selected from hydrogen and substituted or unsubstituted methyl. In a preferred embodiment R₈₂ is substituted or unsubstituted methyl. In a preferred embodiment R83 is substituted or unsubstituted methyl.

In an embodiment of the compound according to the invention of general Formula (I), the halogen is fluorine, chlorine, iodine or bromine; preferably fluorine, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In an embodiment of the compound according to the invention of general Formula (I), the haloalkyl is–CF₃ ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

In another embodiment of the compound according to the invention of general Formula (I), the haloalkoxy is–OCF₃; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. In a preferred further embodiment, the compounds of the general Formula (I) are selected from

In a preferred further embodiment, the compounds of the general Formula (I) are selected from

As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the ^ ^ ^ ^subunit, particularly the ^ ^ ^ ^ ^ ^ subunit, of the voltage-gated calcium channel and the µ-opioid receptor it is a very preferred embodiment in which the compounds are selected which act as dual ligands of the ^ ^ ^ ^subunit, particularly the ^ ^ ^ ^ ^ ^subunit, of the voltage-gated calcium channel and the µ-opioid receptor and especially compounds which have a binding expressed as Ki responding to the following scales:

Ki(µ) is preferably < 1000 nM, more preferably < 500 nM, even more preferably < 100 nM.

Ki( ^ ^ ^1) is preferably < 10000 nM, more preferably < 5000 nM, even more preferably < 500 nM.

In the following the phrase“compound of the invention” is used. This is to be understood as any compound according to the invention as described above according to general Formula (I), (I’), (I^a), (I^a’), (I^b), (I^b’), (I^3’) and (IZ).

The compounds of the invention represented by the above described Formula (I) may include enantiomers depending on the presence of chiral centres or isomers depending on the presence of multiple bonds (e.g. Z, E). The single isomers, enantiomers or diastereoisomers and mixtures thereof fall within the scope of the present invention.

For the sake of clarity the expression“a compound according to Formula (I), wherein e.g. R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁, Y₂ and n are as defined below in the detailed description” would (just like the expression“a compound of Formula (I) as defined in any one of claims e.g.1 to 8” found in the claims) refer to“a compound according to Formula (I)”, wherein the definitions of the respective substituents R₁ etc. (also from the cited claims) are applied. In addition, this would also mean, though (especially in regards to the claims) that also one or more disclaimers defined in the description (or used in any of the cited claims like e.g. claim 1) would be applicable to define the respective compound. Thus, a disclaimer found in e.g. claim 1 would be also used to define the compound“of Formula (I) as defined in any one of the corresponding related claims e.g.1 to 8”. In general the processes are described below in the experimental part. The starting materials are commercially available or can be prepared by conventional methods. A preferred embodiment of the invention is a process for the production of a compound according to Formula (I), wherein, if not defined otherwise, R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁, Y₂ and n have the meanings defined in the description. LG represents a leaving group (such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate).

In a particular embodiment there is a process for the production of a compound according to Formula (I),

wherein X represents a bond, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ and n have the meanings as defined in the description, said process comprises treating a compound of formula (IIa),

wherein Q represents chloro, bromo, iodo or triflate, with a suitable N-containing cyclic reagent of formula (III-1)

under standard Buchwald-Hartwig or Ullmann arylation conditions.

wherein -X- represents -[C(RaRb)]p-, and wherein Ra, Rb, R1, R2, R3, R3’, R4, R4’, Y1, Y2 and n and p have the meanings as defined in the description, said process comprises treating a compound of formula (IIb’)

wherein r represents 0 to 4, with a N-containing cyclic reagent of formula (III-1)

under standard reductive amination conditions.

wherein -X- represents -[C(RaRb)]p-, and wherein Ra, Rb, R1, R2, R3, R3’, R4, R4’, Y1, Y2 and n and p have the meanings as defined in the description, said process comprises treating a compound of formula (IIa),

wherein Q represents chloro, bromo, iodo or triflate, with an organometallic reagent of formula (III-2’)

wherein M represents a suitable organometallic group, preferably a boron or zinc reagent, and p has the meaning as defined in the description. In a particular embodiment there is a process for the production of a compound according to Formula (I),

wherein -X- represents -[CRaRb]pC(O)[CH2]q- and q is 0, and wherein Ra and Rb are hydrogen and R1, R2, R3, R3’, R4, R4’, Y1, Y2, n, p and q have the meanings as defined in the description, said process comprises treating a compound of formula (IIc’)

with a N-containing cyclic reagent of formula (III-1)

under conventional amidation conditions.

wherein -X- represents -[CRaRb]pN(Rz)C(O)[CH2]q-, and wherein Ra and Rb are hydrogen and R1, R2, R3, R3’, R4, R4’, Y1, Y2 , n, p and q have the meanings as defined in the description, said process comprises treating a compound of formula (VI’)

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, p, q and Rz have the meanings as defined in the description, with a N-containing cyclic reagent of formula (III-1)

under conventional alkylation conditions.

wherein -X- represents -[CRaRb]pN(Rz)C(O)[CH2]q-, and wherein Ra and Rb are hydrogen and R1, R2, R3, R3’, R4, R4’, Y1, Y2, n, p and q have the meanings as defined in the description, said process comprises treating an amino compound of formula (IId’)

wherein p and Rz have the meanings as defined in the description, with an acyl reagent of formula (III-3),

under amidation conditions, wherein Z represents OH or halogen and q has the meaning as defined in the description.

wherein -X- represents -[CR_aR_b]_pN(R_z)C(O)[CH₂]_q-, p is 0, and wherein R_a and R_b are hydrogen and R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ , n, p and q have the meanings as defined in the description, said process comprises reacting a compound of formula (IIa)

wherein Q represents chloro, bromo, iodo or triflate, with a carboxamido compound of formula (III-5)

under Ullmann arylation conditions, wherein q and Rz have the meanings as defined in the description.

wherein n is 0, and wherein R1, R2, R3, R3’, R4, R4’, X, Y1 and Y2 have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIa) wherein G is OH,

with an alkylating agent of formula (VIII)

wherein Z represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate.

wherein n is 0, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIa) wherein G is OH,

with an alcohol of formula (VIII) wherein Z represents OH,

in the presence of a suitable azo compound.

wherein n is 0, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIa) wherein G is halogen,

with an alcohol of formula (VIII) wherein Z represents OH,

in the presence of a strong base.

wherein n is 1, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIb)

with an agent of formula (VIII),

wherein either Z represents OH and G represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, or alternatively Z represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate and G represents OH.

a) wherein X represents a bond, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ and n have the meanings as defined in the description, said process comprises treating a compound of formula (IIa),

under standard Buchwald-Hartwig or Ullmann arylation conditions;

or

b) wherein -X- represents -[C(RaRb)]p-, and wherein Ra, Rb, R1, R2, R3, R3’, R4, R4’, Y1, Y2 and n and p have the meanings as defined in the description, said process comprises treating a compound of formula (IIb’)

under standard reductive amination conditions; or

c) wherein -X- represents -[C(R_aR_b)]_p-, and wherein R_a, R_b, R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ and n and p have the meanings as defined in the description, said process comprises treating a compound of formula (IIa),

wherein M represents a suitable organometallic group, preferably a boron or zinc reagent, and p has the meaning as defined in the description;

or d) wherein -X- represents -[CR_aR_b]_pC(O)[CH₂]_q- and q is 0, and wherein R_a and R_b are hydrogen and R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n, p and q have the meanings as defined in the description, said process comprises treating a compound of formula (IIc’)

with a N-containing cyclic reagent of formula (III-1) under conventional amidation conditions;

or

e) wherein -X- represents -[CR_aR_b]_pN(R_z)C(O)[CH₂]_q-, and wherein R_a and R_b are hydrogen and R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ , n, p and q have the meanings as defined in the description, said process comprises treating a compound of formula (VI’)

under conventional alkylation conditions;

or f) wherein -X- represents -[CR_aR_b]_pN(R_z)C(O)[CH₂]_q-, and wherein R_a and R_b are hydrogen and R1, R2, R3, R3’, R4, R4’, Y1, Y2, n, p and q have the meanings as defined in the description, said process comprises treating an amino compound of formula (IId’)

under amidation conditions, wherein Z represents OH or halogen and q has the meaning as defined in the description;

or g) wherein -X- represents -[CR_aR_b]_pN(R_z)C(O)[CH₂]_q-, p is 0, and wherein R_a and R_b are hydrogen and R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ , n, p and q have the meanings as defined in the description, said process comprises reacting a compound of formula (IIa)

under Ullmann arylation conditions, wherein q and Rz have the meanings as defined in the description;

or

h) wherein n is 0, and wherein R1, R2, R3, R3’, R4, R4’, X, Y1 and Y2 have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIa) wherein G is OH,

with an alkylating agent of formula (VIII)

wherein Z represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or i) wherein n is 0, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIa) wherein G is OH,

with an alcohol of formula (VIII) wherein Z represents OH,

in the presence of a suitable azo compound;

or

j) wherein n is 0, and wherein R1, R2, R3, R3’, R4, R4’, X, Y1 and Y2 have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIa) wherein G is halogen,

with an alcohol of formula (VIII) wherein Z represents OH,

in the presence of a strong base; or

k) wherein n is 1, and wherein R1, R2, R3, R3’, R4, R4’, X, Y1 and Y2 have the meanings as defined in the description, said process comprises reacting a compound of formula (VIIb)

with an agent of formula (VIII),

In a particular embodiment there is a process for the production of a compound according to Formula (I), by the reduction reaction of a carbonyl derivative with a suitable reductive reagent, preferably sodium borohydride, in an organic solvent, preferably MeOH, to afford a hydroxyl compound.

In a particular embodiment there is a process for the production of a compound according to Formula (I), by deprotection reaction of a compound of formula I that contains an amine protecting group such as a carbamate, preferably tert-butoxy carbonyl, by any suitable method, such as treatment with an acid, preferably HCl or trifluoroacetic acid in an appropriate solvent such as 1,4-dioxane, DCM, ethyl acetate or a mixture of an organic solvent and water. In a particular embodiment there is a process for the production of a compound according to Formula (I), by reductive amination reaction of a compound of formula I that contains an amino group with an aldehyde, preferably carried out with a reductive reagent, preferably sodium triacetoxyborohydride, in an organic solvent, preferably DCE, in the presence of an organic base, preferably DIPEA or TEA. Alternatively, the reaction can be carried out in the presence of an acid, preferably acetic acid. In a particular embodiment there is a process for the production of a compound according to Formula (I), by reaction of a compound of formula I that contains an amino group with an alkylating reagent, in the presence of a base, preferably DIPEA or K₂CO₃, in an organic solvent, preferably acetonitrile, at suitable temperature, such as in the range of 0-120 ºC. In a particular embodiment there is a process for the production of a compound according to Formula (I), by reaction of a compound of formula I that contains an amino group with a vinyl derivative, in an organic solvent, preferably 2-methoxyethanol, at suitable temperature, such as in the range of 20-140 ºC.

A particular embodiment of the invention refers to the use of a compound of Formula (II),

wherein Z represents OH or halogen, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ and n have the meanings as defined in the description, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (IIa),

wherein Q represents chloro, bromo, iodo or triflate, R2, R3, R3’, R4, R4’, Y1, Y2 and n have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IIa-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, Q represents chloro, bromo, iodo or triflate, R₂, R₄, R_4’, Y₁, Y₂ and n have the meanings as defined in the description, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (IIb),

wherein R2, R3, R3’, R4, R4’, Y1, Y2, n and r have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IIb’),

wherein R_a, R_b, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n and r have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IIb-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R₂, R₄, R_4’, Y₁, Y₂, n and r have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IIb’-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, Ra, Rb, R2, R4, R4’, Y1, Y2, n and r have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IIc),

wherein R2, R3, R3’, R4, R4’, Y1, Y2, n and p have the meanings as defined in the description, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (IIc’),

wherein R_a, R_b, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n and p have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IIc-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R₂, R₄, R_4’, Y₁, Y₂, n and p have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IIc’-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R_a, R_b, R2, R₄, R_4’, Y₁, Y₂, n and p have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IId),

wherein R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n, p and R_z have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IId’),

wherein R_a, R_b, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n, p and R_z have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IId’-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R_a, R_b, R₂, R₄, R_4’, Y₁, Y₂, n, p and R_z have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IId’-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, Ra, Rb, R2, R4, R4’, Y1, Y2, n, p and Rz have the meanings as defined in the description, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (III-1),

wherein R1 has the meaning as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (III-2),

wherein p and R₁ have the meaning as defined in the description, and M represents a suitable organometallic group, preferably a boron or zinc reagent, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (III’-2),

wherein p and R_a, R_b, R₁ have the meaning as defined in the description, and M represents a suitable organometallic group, preferably a boron or zinc reagent, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (III-3),

wherein q and R₁ have the meaning as defined in the description, and Z represents OH or halogen, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (III-4),

wherein q has the meaning as defined in the description, Z represents OH or halogen, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (III-5),

wherein q, Rz and R1 have the meaning as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IVa),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R₁, R₂, R₄, R_4’, Y₁, Y₂ and n have the meanings as defined in the description, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (IVb),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R₁, R₂, R₄, R_4’, Y₁, Y_2, p and n have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IVb’),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R_a, R_b, R₁, R₂, R₄, R_4’, Y₁, Y_2, p and n have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IVc),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R₁, R₂, R₄, R_4’, Y₁, Y_2, p and n have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IVc’),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, Ra, Rb, R1, R2, R4, R4’, Y1, Y2, p and n have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IVd),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, Rz, R1, R2, R4, R4’, Y1, Y2, p and n have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IVd’),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R_a, R_b, R_z, R₁, R₂, R₄, R_4’, Y₁, Y_2, p and n have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IVe),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R1, R2, R4, R4’, Y1 and Y2 have the meanings as defined in the description, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (IVf),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R₁, R₂, R₄, R_4’, Y₁ and Y₂ have the meanings as defined in the description, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (V),

wherein R₃ and R_3’ have the meaning as defined in the description, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (VI),

wherein R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n, p, q and R_z have the meanings as defined in the description, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (VI’),

wherein R_a, R_b, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n, p, q and R_z have the meanings as defined in the description, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (VII),

wherein n, R1, R4, R4’ and X have the meanings as defined in the description, and G is OH or halogen, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (VIIa),

wherein R₁, R₄, R_4’ and X have the meanings as defined in the description, and G is OH or halogen, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (VIIb),

wherein R₁, R₄, R_4’ and X have the meanings as defined in the description, and G is OH or a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (VIII),

wherein R2, R3, R3’, Y1 and Y2 have the meaning as defined in the description, and Z represents OH or halogen, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (VIII-LG),

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, R2, Y1, and Y2 have the meaning as defined in the description, and Z represents OH or halogen, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (IX),

wherein n, R4, R4’ have the meanings as defined in the description, and Z represents OH or halogen and G is OH or halogen, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (X),

wherein R₃, R_3’, R₄, R_4’, n, Y₁ and Y₂ have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (X’),

wherein Ra, Rb, R3, R3’, R4, R4’, n, Y1 and Y2 have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (X-LG),

wherein R3, R3’, R4, R4’, n, Y1 and Y2 have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (X’-LG),

wherein R_a, R_b, R₃, R_3’, R₄, R_4’, n, Y₁ and Y₂ have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (XI),

wherein R₃, R_3’, R₄, R_4’, n, Y₁ and Y₂ have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (XI-LG),

wherein R₃, R_3’, R₄, R_4’, n, Y₁ and Y₂ have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (XI’-LG),

wherein R_a, R_b, R₃, R_3’, R₄, R_4’, n, Y₁ and Y₂ have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula (XI’-LG),

wherein R_a, R_b, R₃, R_3’, R₄, R_4’, n, Y₁ and Y₂ have the meaning as defined in the description, and r represents 0 to 4, for the preparation of compounds of Formula (I). A particular embodiment of the invention refers to the use of a compound of Formula 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’-LG

wherein R_a, R_b, R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ , n, p, q, r and R_z have the meanings as defined in the description, Q represents chloro, bromo, iodo or triflate, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, have the meanings as defined in the description, M represents a suitable organometallic group, Z represents OH or halogen, and G is OH, halogen or a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, for the preparation of compounds of Formula (I). The obtained reaction products may, if desired, be purified by conventional methods, such as crystallisation and chromatography. Where the above described processes for the preparation of compounds of the invention give rise to mixtures of stereoisomers, these isomers may be separated by conventional techniques such as preparative chromatography. If there are chiral centers the compounds may be prepared in racemic form, or individual enantiomers may be prepared either by enantiospecific synthesis or by resolution.

One preferred pharmaceutically acceptable form of a compound of the invention is the crystalline form, including such form in pharmaceutical composition. In the case of salts and also solvates of the compounds of the invention the additional ionic and solvent moieties must also be non-toxic. The compounds of the invention may present different polymorphic forms, it is intended that the invention encompasses all such forms. Another aspect of the invention refers to a pharmaceutical composition which comprises a compound according to the invention as described above according to general formula I or a pharmaceutically acceptable salt or steroisomer thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle. The present invention thus provides pharmaceutical compositions comprising a compound of this invention, or a pharmaceutically acceptable salt or stereoisomers thereof together with a pharmaceutically acceptable carrier, adjuvant, or vehicle, for administration to a patient. Examples of pharmaceutical compositions include any solid (tablets, pills, capsules, granules etc.) or liquid (solutions, suspensions or emulsions) composition for oral, topical or parenteral administration. In a preferred embodiment the pharmaceutical compositions are in oral form, either solid or liquid. Suitable dose forms for oral administration may be tablets, capsules, syrops or solutions and may contain conventional excipients known in the art such as binding agents, for example syrup, acacia, gelatin, sorbitol, tragacanth, or polyvinylpyrrolidone; fillers, for example lactose, sugar, maize starch, calcium phosphate, sorbitol or glycine; tabletting lubricants, for example magnesium stearate; disintegrants, for example starch, polyvinylpyrrolidone, sodium starch glycollate or microcrystalline cellulose; or pharmaceutically acceptable wetting agents such as sodium lauryl sulfate. The solid oral compositions may be prepared by conventional methods of blending, filling or tabletting. Repeated blending operations may be used to distribute the active agent throughout those compositions employing large quantities of fillers. Such operations are conventional in the art. The tablets may for example be prepared by wet or dry granulation and optionally coated according to methods well known in normal pharmaceutical practice, in particular with an enteric coating. The pharmaceutical compositions may also be adapted for parenteral administration, such as sterile solutions, suspensions or lyophilized products in the apropriate unit dosage form. Adequate excipients can be used, such as bulking agents, buffering agents or surfactants. The mentioned formulations will be prepared using standard methods such as those described or referred to in the Spanish and US Pharmacopoeias and similar reference texts. Administration of the compounds or compositions of the present invention may be by any suitable method, such as intravenous infusion, oral preparations, and intraperitoneal and intravenous administration. Oral administration is preferred because of the convenience for the patient and the chronic character of the diseases to be treated. Generally an effective administered amount of a compound of the invention will depend on the relative efficacy of the compound chosen, the severity of the disorder being treated and the weight of the sufferer. However, active compounds will typically be administered once or more times a day for example 1, 2, 3 or 4 times daily, with typical total daily doses in the range of from 0.1 to 1000 mg/kg/day. The compounds and compositions of this invention may be used with other drugs to provide a combination therapy. The other drugs may form part of the same composition, or be provided as a separate composition for administration at the same time or at different time. Another aspect of the invention refers to the use of a compound of the invention or a pharmaceutically acceptable salt or isomer thereof in the manufacture of a medicament. Another aspect of the invention refers to a compound of the invention according as described above according to general formula I, or a pharmaceutically acceptable salt or isomer thereof, for use as a medicament for the treatment of pain. Preferably the pain is medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia or hyperalgesia. This may include mechanical allodynia or thermal hyperalgesia. Another aspect of the invention refers to the use of a compound of the invention in the manufacture of a medicament for the treatment or prophylaxis of pain. In a preferred embodiment the pain is selected from medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia or hyperalgesia, also preferably including mechanical allodynia or thermal hyperalgesia. Another aspect of this invention relates to a method of treating or preventing pain which method comprises administering to a patient in need of such a treatment a therapeutically effective amount of a compound as above defined or a pharmaceutical composition thereof. Among the pain syndromes that can be treated are medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia or hyperalgesia, whereas this could also include mechanical allodynia or thermal hyperalgesia.

The present invention is illustrated below with the aid of examples. These illustrations are given solely by way of example and do not limit the general spirit of the present invention.

General Experimental Part (Methods and Equipment of the synthesis and analysis

SYNTHESIS DESCRIPTION Two different general methods have been developed for obtaining the compounds of the invention, as described below in methods A and B, and further detailed in Schemes 1 to 8.

METHOD A A one-step process is described for the preparation of compounds of general formula (I) starting from a compound of formula (II), as shown in the following scheme:

Method A

wherein R1, R2, R3, R3’, R4, R4’, X, Y1, Y2 and n have the meanings as defined in claim 1, LG represents a leaving group, Z represents a suitable functional group to perform such transformation, and R¹-W represents a compound of formula III-1, III-2, III-3 or III- 5, as it is detailed below in Schemes 1 to 4.

In addition, the amino group NR3R3’ present in a compound of formula (I) can be incorporated later in the synthesis by reaction of a compound of formula (IV) wherein LG represents a leaving group (such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate) with an amine of formula (V) to render a compound of formula (I) 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 in the presence of a base such as K2CO3, N,N-diisopropylethylamine or triethylamine; at a suitable temperature comprised between room temperature and the reflux temperature, preferably heating, or alternatively, the reactions can be carried out under microwave heating. Additionally, an activating agent such as sodium iodide or potassium iodide can be used. Such transformation can also be performed starting from a compound of formula (II-LG) to prepare a compound of formula (II).

Scheme 1 The general synthetic route according to method A for preparing compounds of formula (I) wherein X represents a bond, resulting in compounds of formula (Ia) starting from a compound of formula (IIa) is represented in Scheme 1:

wherein R1, R2, R3, R3’, R4, R4’, Y1, Y2 and n have the meanings as defined in claim 1, Q represents chloro, bromo, iodo or triflate and LG represents a leaving group (such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate). The preparation of a compound of formula (Ia) from a compound of formula (IIa) is carried out by treating a compound of formula (IIa) with a suitable N-containing cyclic reagent of formula (III-1) under standard Buchwald-Hartwig conditions, using a Pd catalyst such as tris(dibenzylideneacetone)dipalladium(0) or palladium acetate, and a suitable ligand, preferably a phosphine ligand such as BINAP or XPhos, using a suitable base such as sodium tert-butoxide or cesium carbonate, in a suitable solvent such as toluene or 1,4-dioxane, at a suitable temperature, preferably heating. Alternatively, the reaction can be carried out under Ullmann arylation conditions, using a Cu catalyst such as copper iodide and a suitable ligand, preferably an amino ligand such as N¹,N²-dimethylethane-1,2-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 heating.

Alternatively, the amino group NR3R3’ present in a compound of formula (Ia) or (IIa) can be incorporated later in the synthesis by reaction of a precursor compound of formula (IVa) or (IIa-LG), respectively, with an amine of formula (V) following the conditions described above in Method A.

Scheme 2 The general synthetic route according to method A for preparing compounds of formula (I) wherein -X- represents -[CH₂]_p-, resulting in compounds of formula (Ib), starting from a compound of formula (IIa) or (IIb), is represented in Scheme 2:

wherein R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n and p have the meanings as defined in claim 1, LG represents a leaving group (such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate), Q represents chloro, bromo, iodo or triflate, M represents a suitable organometallic group (preferably a boron or zinc reagent) and r represents 0 to 4. The preparation of a compound of formula (Ib) from an aldehyde compound of formula (IIb) can be carried out by treating a compound of formula (IIb) with a N-containing cyclic reagent of formula (III-1) under standard reductive amination conditions. The reaction is carried out in the presence of a reductive reagent, such as sodium triacetoxyborohydride, sodium borohydride or sodium cyanoborohydride, in a suitable solvent, preferably tetrahydrofuran, dichloroethane or methanol, optionally in the presence of an acid (preferably acetic acid) or a base (preferably N,N- diisopropylethylamine). Alternatively, a compound of formula (Ib) can be prepared by reacting a compound of formula (IIa) with an organometallic reagent of formula (III-2), preferably a boron or zinc reagent. The coupling reaction is carried out under conventional coupling procedures described in the literature, using a suitable catalyst (preferably a Pd catalyst) and a suitable ligand (preferably a phosphine ligand), such as for example 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 mixtures thereof with water. In addition, the amino group NR₃R_3’ present in a compound of formula (Ib), (IIa) or (IIb) can be incorporated later in the synthesis by reaction of a precursor compound of formula (IVb), (IIa-LG) or (IIb-LG), respectively, with an amine of formula (V), following the conditions described above in Method A. This process can easily be adapted wherein -X- represents -[CRaRb]p-, by choosing the corresponding reagents.

Scheme 3 The general synthetic route according to method A for preparing compounds of formula (I) wherein -X- represents -[CH2]pC(O)[CH2]q- and q is 0, resulting in compounds of formula (Ic), starting from a compound of formula (IIc) is represented in Scheme 3:

wherein R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n and p have the meanings as defined in claim 1 and LG represents a leaving group (such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate). The preparation of a compound of formula (Ic) from an acid compound of formula (IIc) and a N-containing cyclic reagent of formula (III-1) can be carried out under conventional amidation conditions. As a way of example, the reaction is carried out using a suitable coupling reagent such as N-(3-dimethylaminopropyl)-N′- ethylcarbodiimide (EDC), dicyclohexylcarbodiimide (DCC), N-[(dimethylamino)-1H- 1,2,3-triazolo-[4,5-b]pyridin-1-ylmethylene]-N-methylmethanaminium

hexafluorophosphate N-oxide (HATU) or N,N,N′,N′-tetramethyl-O-(1H-benzotriazol-1- yl)uronium hexafluorophosphate (HBTU), optionally in the presence of 1- hydroxybenzotriazole, optionally in the presence of an organic base such as N- methylmorpholine or N,N-diisopropylethylamine, in a suitable solvent such as dichloromethane or dimethylformamide, and at a suitable temperature, preferably at room temperature. Alternatively, the amidation can be performed in two steps by first converting an acid of formula (IIc) into its corresponding acyl halide following standard conditions described in the literature, and then reacting it with a compound of formula (III-1) in a suitable solvent, such as dichloromethane, tetrahydrofuran, ethyl acetate or ethyl acetate-water mixtures; in the presence of an organic base such as triethylamine or N,N-diisopropylethylamine or an inorganic base such as K2CO3; and at a suitable temperature, preferably comprised between 0 ºC and room temperature. Additionally, an activating agent such as 4-dimethylaminopyridine can be used. In addition, the amino group NR3R3’ present in a compound of formula (Ic) or (IIc) can be incorporated later in the synthesis by reaction of a precursor compound of formula (IVc) or (IIc-LG), respectively, with an amine of formula (V) following the conditions described above in Method A. This process can easily be adapted wherein -X- represents -[CRaRb]pC(O)[CH2]q-, by choosing the corresponding reagents.

Scheme 4 The general synthetic route according to method A for preparing compounds of formula (I) wherein -X- represents -[CH₂]_pN(R_z)C(O)[CH₂]_q-, resulting in compounds of formula (Id), starting from a compound of formula (IId) or (IIa), is represented in Scheme 4:

wherein R1, R2, R3, R3’, R4, R4’, Rz, Y1, Y2, n, p and q have the meanings as defined in claim 1, LG represents a leaving group (such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate) and Z represents OH or halogen (preferably bromo or chloro). The reaction between an amino compound of formula (IId) with an acyl reagent of formula (III-3) to render a compound of formula (Id) can be carried out under the amidation conditions described above in Scheme 3 for the preparation of compounds of formula (Ic). Alternatively, the compounds of formula (Id) can be prepared in 2 steps by treating a compound of formula (IId) with an acylating agent of formula (III-4) under the same amidation conditions to obtain a compound of formula (VI), followed by reaction with a N-containing cyclic reagent of formula (III-1), 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). Finally, a compound of formula (Id) wherein p is 0 can be alternatively prepared by reacting a compound of formula (IIa) with a carboxamido compound of formula (III-5). The reaction can be carried out under Ullmann arylation conditions, using a Cu catalyst such as copper iodide and a suitable ligand, preferably an amino ligand such as N¹,N²- dimethylethane-1,2-diamine, in the presence of a suitable base such as potassium phosphate, in a suitable solvent such as 1,4-dioxane or dimethylformamide, at a suitable temperature, preferably heating. Alternatively, the coupling reaction can be performed under standard Buchwald-Hartwig arylation conditions, using a suitable Pd catalyst and a suitable ligand (preferably a phosphine ligand). In addition, the amino group NR3R3’ present in a compound of formula (Id), (IIa) or (IId) can be incorporated later in the synthesis by reaction of a precursor compound of formula (IVd), (IIa-LG) or (IId-LG), respectively, with an amine of formula (V) following the conditions described above in Method A. This process can easily be adapted wherein -X- represents -[CRaRb]pN(Rz)C(O)[CH2]q- , by choosing the corresponding reagents.

METHOD B An alternative one-step process is described for the preparation of compounds of general formula (I) starting from a compound of formula (VII), as shown in the following scheme:

Method B

wherein R1, R2, R3, R3’, R4, R4’, X, Y1, Y2 and n have the meanings as defined in claim 1, Z represents OH or a leaving group, and G represents OH, halogen or a leaving group depending on the meaning of n. Specific reaction conditions are detailed below in Schemes 5 and 6. As it has been mentioned before, alternatively the amino group NR3R3’ present in a compound of formula (I) can be incorporated later in the synthesis by reaction of a precursor compound of formula (IV) with an amine of formula (V) following the conditions described above in Method A.

Scheme 5 The general synthetic route according to method B for preparing compounds of formula (I) wherein n is 0, resulting in compounds of formula (Ie), is represented in Scheme 5:

wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in claim 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 chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, the alkylation reaction between a phenol of formula (VIIa) and an alkylating agent of formula (VIII) is carried out in a suitable solvent, such as dimethylformamide, dimethylacetamide, dimethylsulfoxide, acetonitrile, dichloromethane or 1,4-dioxane; in the presence of a base such as K₂CO₃, Cs₂CO₃, sodium hydride or potassium tert-butoxide; at a suitable temperature comprised between room temperature and the reflux temperature, or alternatively, the reactions can be carried out in a microwave reactor. Additionally, an activating agent 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 treating a phenol of formula (VIIa) with an alcohol of formula (VIII) in the presence of an azo compound such as 1,1'- (azodicarbonyl)dipiperidine (ADDP), diisopropylazodicarboxylate (DIAD) or diethyl azodicarboxylate (DEAD) and a phosphine such as tributylphosphine or triphenylphoshine. The Mitsunobu reaction is carried out in a suitable solvent, such as toluene or tetrahydrofuran; at a suitable temperature comprised between room temperature and the reflux temperature. c) When G is halogen and Z represents OH, the reaction is carried out under conventional aromatic nucleophilic substitution conditions by treating an alcohol of formula (VIII) with a compound of formula (VIIa) wherein G represents halogen (preferably fluoro), in the presence of a strong base such as sodium hydride or potassium tert-butoxide. The reaction is carried out in a suitable solvent, such as a polar aprotic solvent, preferably dimethylformamide, dimethylacetamide or dimethylsulfoxide; at a suitable temperature comprised between room temperature and the reflux temperature, preferably heating, or alternatively, the reactions can be carried out in a microwave reactor. Alternatively, when G is bromo or iodo, the compound of formula (VIII) can be introduced under cross-coupling conditions, using a Pd or Cu catalyst and a suitable ligand.

Scheme 6 The general synthetic route according to method B for preparing compounds of formula (I) wherein n is 1, resulting in compounds of formula (If), is represented in Scheme 6:

wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in claim 1, n is 1, and either Z represents OH and G represents a leaving group or alternatively Z represents a leaving group and G represents OH. The reaction is carried out under standard alkylation reaction conditions such as those described in Scheme 5 above.

Scheme 7 The preparation of key compounds of formula (II) and (VII) from a common precursor of formula (IX) is summarized in Scheme 7 below:

wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁, Y₂ and n have the meanings as defined in claim 1, and G and Z have the meanings as defined above in Schemes 1 to 6, and R1-W represents a compound of formula III-1, III-2, III-3 or III-5 as defined above in

Schemes 1 to 6..

The preparation of a compound of formula (VII) from a compound of formula (IX) and a compound of formula (III) can be carried out under the reaction conditions described above in general Method A and further detailed in Schemes 1 to 4. The preparation of a compound of formula (II) or (II-LG) from a compound of formula (IX) and a compound of formula (VIII) can be carried out under the reaction conditions described above in general Method B and further detailed in Schemes 5 and 6.

Scheme 8 In addition, a compound of formula (IIb) can be prepared from a compound of formula (IIa) following several methods described in the literature. As a way of example, two routes of synthesis are described in Scheme 8 below:

wherein R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ and n have the meanings as defined in claim 1, Q represents chloro, bromo, iodo or triflate and and r represents 0 to 4. Following Route A, a compound of formula (IIa) is converted into a nitrile compound of formula (X) (under standard conditions described in the literature depending on the nature of r), followed by reduction with a suitable hydride source such as diisobutylaluminum hydride, to render a compound of formula IIb. Alternatively and following Route B, a compound of formula (IIa) is converted into an alkenyl compound of formula (XI) via a cross-coupling reaction using conventional reaction conditions, preferably a Suzuki coupling, followed by oxidative cleavage by treatment with a reagent such as osmium tetroxide followed by treatment with an oxidant such as sodium periodate, to render a compound of formula IIb. By choosing the corresponding reagents, this process can easily be adapted to prepare compounds of formula IIb’ or IIb’-LG, that can be used according to Scheme 2 for the preparation of compounds of formula Ib or IVb wherein -X- represents -[CR_aR_b]_p-, The compounds of formula (III), (III-1), (III-2), (III-3), (III-4), (III-5), (V), (VIII) and (IX) used in the methods and schemes disclosed above are commercially available or can be synthesized following common procedures described in the literature. Moreover, certain compounds of the present invention can also be obtained starting from other compounds of formula (I) by appropriate conversion reactions of functional groups, in one or several steps, using well-known reactions in organic chemistry under standard experimental conditions. In some of the processes described above it may be necessary to protect the reactive or labile groups present with suitable protecting groups, such as for example Boc (tert- butoxycarbonyl), Teoc (2-(trimethylsilyl)ethoxycarbonyl) or benzyl for the protection of amino groups, and common silyl protecting groups for the protection of the hydroxyl group. The procedures for the introduction and removal of these protecting groups are well known in the art and can be found thoroughly described in the literature. In addition, a compound of formula (I) can be obtained in enantiopure form by resolution of a racemic compound of formula (I) either by chiral preparative HPLC or by crystallization of a diastereomeric salt or co-crystal. Alternatively, the resolution step can be carried out at a 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'-binaphthyl Boc: tert-butoxycarbonyl

tBuOH: tert-butanol

CH: cyclohexane

DCE: dichloroethane

DCM: dichloromethane

DEA: diethylamine

Deprot.: deprotection

DIAD: diisopropyl azodicarboxylate

DIBAL-H: diisobutylaluminum hydride

DIPEA: N,N-diisopropylethylamine

DMA: N,N-dimethylacetamide

DMF: N,N-dimethylformamide

DMSO: dimethylsulfoxide

EtOAc: ethyl acetate

EtOH: ethanol

EX: example

h: hour/s

HPLC: high performance liquid chromatography INT: intermediate

MeOH: methanol

MS: mass spectrometry Min: minutes

Pd(OAc)2: palladium(II) acetate

Pd2(dba)3: tris(dibenzylideneacetone)dipalladium(0)

Pd(PPh3)4: tetrakis(triphenylphosphine)palladium(0)

Quant: quantitative

Ret.: retention

r.t.: room temperature

Sat.: saturated

Sol.: solution

SPhos: 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl

Teoc: 2-(trimethylsilyl)ethoxycarbonyl

THF: tetrahydrofuran

Ti(OⁱPr)₄: titanium(IV) propan-2-olate

Wt: weight

XPhos: 2-dicyclohexylphosphino-2′,4′,6′-triisopropylbiphenyl

The following method was used to determine the HPLC-MS spectra:

Column: Kinetex EVO 50 x 4.6 mm, 2.6 um

Temperature: 40 ºC

Flow: 1.5 mL/min

Gradient: NH₄HCO₃ pH 8 : ACN (95:5)---0.5min---(95:5)---6.5min---(0:100)---2min--- (0:100)

Sample dissolved approx.1mg/mL in NH4HCO3 pH 8/ ACN Synthesis of Intermediates Intermediate 1: (R)-2-(Trimethylsilyl)ethyl (3-(2-bromophenoxy)-3-(thiophen-2- yl)propyl)(ethyl)carbamate

Step 1. (R)-3-(Ethylamino)-1-(thiophen-2-yl)propan-1-ol: A solution of (R)-3-chloro-1- (thiophen-2-yl)propan-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 ºC overnight. The solvent was evaporated, the residue was dissolved in DCM and it was washed with 1 N NaOH, dried over MgSO₄, filtered and concentrated to dryness. The crude product (7.74 g) was slurried in methylcyclohexane (44 mL) and heated at 60 ºC for 1 h. Then, it was allowed to cool down and it was stirred at r.t. for 1 h. The solids were 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: To a solution of the product obtained in Step 1 (0.98 g, 5.3 mmol) and 1-bromo-2- fluorobenzene (2.29 mL, 21.1 mmol) in DMSO (1.6 mL), potassium tert-butoxide (0.6 g, 5.3 mmol) was added under a N₂ atmosphere and the reaction mixture was heated at 60 ºC for 8 h. It was then cooled to r.t., water was added and the aqueous phase was extracted twice with EtOAc. The combined organic phases were dried over MgSO₄, 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. Title compound: To a solution of the product obtained in Step 2 (1.14 g, 3.3 mmol) in DCM (1.5 mL), DIPEA (0.58 mL, 3.3 mmol) and a solution of 4-nitrophenyl (2- (trimethylsilyl)ethyl) carbonate (0.95 g, 3.3 mmol) in DCM (1.5 mL) were added under a N2 atmosphere and the mixture was stirred at r.t. overnight. NaHCO3 sat. solution was added and it was extracted twice with DCM. The combined organic phases were washed with 2 N NaOH aq. solution, dried over MgSO4, 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).

This method was used for the preparation of Intermediates 2-5 using suitable starting materials:

Intermediate 6: 2-(Trimethylsilyl)ethyl (3-(2-bromophenoxy)-3-(3- fluorophenyl)propyl)(methyl)carbamate

Step 1. 1-(3-Fluorophenyl)-3-(methylamino)propan-1-one hydrochloride: In a sealed tube, 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 ºC overnight. The solvent was partially evaporated, and the precipitated solids were filtered off. The filtrate was evaporated to dryness and the residue was slurried in EtOAc (150 mL). The solids were filtered, washed with EtOAc and dried under vacuum, to afford the title compound (6.35 g, 40% yield). Step 2. 1-(3-Fluorophenyl)-3-(methylamino)propan-1-ol: To a cooled solution of the product obtained in Step 1 (6.35 g, 21.9 mmol) in MeOH (140 mL), NaBH₄ (2.48 g, 65.6 mmol) was added portionwise and the mixture was stirred at 0-5 ºC for 1 h. NH₄Cl sat. solution was then added (25 mL) and MeOH was distilled off. The aqueous phase was extracted with CHCl₃ and finally with CHCl₃/MeOH (9:1). The combined organic extracts were dried over MgSO₄, filtered and concentrated to dryness to afford the title compound (2 g, 50% yield).

Step 3. 3-(2-Bromophenoxy)-3-(3-fluorophenyl)-N-methylpropan-1-amine: Following the experimental procedure described in Step 2 of Intermediate 1, using the compound obtained in Step 2, the title compound was obtained (2.96 g, 80% yield)

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

Intermediate 7: 2-(3-Chloro-1-(thiophen-2-yl)propoxy)benzaldehyde

Step 1.2-(3-Chloro-1-(thiophen-2-yl)propoxy)benzonitrile: To a solution of 3-chloro-1- (thiophen-2-yl)propan-1-ol (10 g, 52 mmol), triphenylphosphine (15 g, 57.2 mmol) and 2-hydroxybenzonitrile (6.8 g, 57.2 mmol) in dry THF (252 mL), cooled at 0 ºC, DIAD (11.5 mL, 58.3 mmol) was added dropwise and the mixture was stirred at r.t. overnight. The solvent was concentrated under vacuum and the residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to afford the title compound (13.9 g, 96% yield). Step 2. Title compound: To a solution of the product obtained in Step 1 (4 g, 14.4 mmol) in toluene (40 mL), cooled at 0 ºC, DIBAL-H (25 wt% solution in toluene, 13.5 mL, 20.2 mmol) was added dropwise and the reaction mixture was stirred at 0-5 ºC for 4 h. Then, 10% aq. HCl solution was slowly added to quench the reaction and the mixture was stirred at r.t. for 10 min. It was extracted with EtOAc and the combined organic phases were washed with water and brine, dried over Na₂SO₄, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc, to afford the title compound (1.54 g, 38% yield). This method was used for the preparation of Intermediate 8 using suitable starting materials:

(1) 1 M DIBAL-H in DCM at -78 ºC was used in Step 2 Intermediate 9: tert-Butyl (3-(2-formylphenoxy)-3-phenylpropyl)(methyl)carbamate:

In a sealed tube, a mixture of tert-butyl (3-chloro-3-phenylpropyl)(methyl)carbamate (1 g, 3.52 mmol), K2CO3 (1.46 g, 10.57 mmol), KI (58 mg, 0.352 mmol) and 2- hydroxybenzaldehyde (0.38 mL, 3.52 mmol) in DMF (23 mL) was heated at 60 ºC overnight. After cooling down to r.t., water was added to the reaction mixture and it was extracted with EtOAc. The combined organic phases were washed with 1 N NaOH aq. solution and brine, dried over MgSO₄, filtered and concentrated to dryness to afford the title compound (1.21 g, 93% yield).

Intermediate 10: 2-(Trimethylsilyl)ethyl (3-(2-bromo-4-fluorophenoxy)-3-(thiophen-2- yl)propyl)(methyl)carbamate

Step 1. 2-(1-(2-Bromo-4-fluorophenoxy)-3-chloropropyl)thiophene: Following the experimental procedure described in Step 1 of Intermediate 7, using 2-bromo-4- fluorophenol instead of 2-hydrozybenzonitrile, the title compound was obtained (373 mg, 63% yield). Step 2. 3-(2-Bromo-4-fluorophenoxy)-N-methyl-3-(thiophen-2-yl)propan-1-amine: In a sealed tube, a solution of the compound obtained in Step 1 (373 mg, 1.07 mmol) and methylamine (33 wt% solution in EtOH, 6.6 mL, 53.3 mmol) was heated at 100 ºC overnight. The solvent was evaporated, the crude product was partitioned between DCM and 1 N NaOH aq. solution. The phases were separated and the aqueous phase was extracted with DCM. The combined organic phases were dried over Na2SO4, filtered and concentrated. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4), to give the title compound (204 mg, 55% yield). Step 3. Title compound: Following the experimental procedure described in Step 3 of Intermediate 1, using the compound obtained in Step 2, the title compound was obtained (224 mg, quant. yield). This method was used for the preparation of Intermediate 11 using suitable starting materials:

Intermediate 12: (R)-2-(Trimethylsilyl)ethyl methyl(3-(2-(2-oxoethyl)phenoxy)-3- (thiophen-2-yl)propyl)carbamate

Step 1. (R)-2-(Trimethylsilyl)ethyl (3-(2-(cyanomethyl)phenoxy)-3-(thiophen-2- yl)propyl)(methyl)carbamate: In a sealed tube, Pd2(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. 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 ºC overnight under argon. 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. Title compound: To a solution of the product obtained in Step 1 (0.5 g, 1.08 mmol) in DCM (8 mL), cooled at -78 ºC, DIBAL-H (1 M solution in DCM, 3.25 mL, 3.25 mmol) was added dropwise and the reaction mixture was stirred at -78 ºC for 1.5 h. Then, it was poured into a sat. solution of potassium tartrate, cooled at -78 ºC, and the mixture was allowed to reach r.t. under stirring. It was extracted with DCM and the combined organic phases were washed with brine, dried over MgSO4, filtered and concentrated to dryness to afford the title compound (406 mg, 81% yield).

Intermediate 13: (R)-2-(Trimethylsilyl)ethyl ethyl(3-(2-(2-oxoethyl)phenoxy)-3- (thiophen-2-yl)propyl)carbamate

Step 1. (R)-2-(Trimethylsilyl)ethyl (3-(2-allylphenoxy)-3-(thiophen-2- yl)propyl)(ethyl)carbamate: In a sealed tube Pd(PPh3)4 (137 mg, 0.145 mmol), 2-allyl- 4,4,5,5-tetramethyl-1,3,2-dioxaborolane (0.73 g, 4.3 mmol) and potassium carbonate (0.3 g, 2.17 mmol) were charged. 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 ºC for 4 h. The reaction mixture was filtered through a pad of Celite, that was washed with EtOAc. The filtrate was washed with brine, dried over MgSO₄, 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. Title compound: To a solution of the product obtained in Step 1 (478 mg, 1.07 mmol) in a mixture of THF-water (2:1, 22.5 mL), a solution of OsO4 (4 wt% aq. sol., 0.75 mL, 0.118 mmol) was added. The reaction was stirred at r.t. for 10 min. and then NaIO₄ (573 mg, 2.68 mmol) was added. The mixture was stirred at r.t. for 15 min. The solvent was concentrated and the aqueous phase was extracted with EtOAc. The combined organic extracts were dried over MgSO₄, filtered and concentrated to dryness to afford the title compound (448 mg, 93% yield). This method was used for the preparation of Intermediate 14 using suitable starting materials:

Intermediate 15: (S)-2-(Trimethylsilyl)ethyl (3-(2-acetylphenoxy)-3-(thiophen-2- yl)propyl)(methyl)carbamate

Step 1. (S)-1-(2-(3-(Methylamino)-1-(thiophen-2-yl)propoxy)phenyl)ethanone: To a solution of (S)-3-(methylamino)-1-(thiophen-2-yl)propan-1-ol (300 mg, 1.75 mmol) in anhydrous DMA (3 mL), cooled at 0 ºC under a N₂ atmosphere, NaH (60 wt% dispersion in mineral oil, 175 mg, 4.38 mmol) was added portionwise. After stirring at 0 ºC for 30 min, a solution of 1-(2-fluorophenyl)ethan-1-one (0.21 mL, 1.75 mmol) in anhydrous DMA (3 mL) was added and the reaction mixture was stirred at 50 ºC for 2 h. It was cooled to 0 ºC and then NH₄Cl sat. sol. was carefully added. The aqueous phase was extracted with EtOAc and the combined organic phases were dried over MgSO₄, 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 (166 mg, 33% yield). Step 2. Title compound: Following the experimental procedure described in Step 3 of Intermediate 1, starting from the compound obtained in Step 1 (166 mg, 0.574 mmol), the title compound was obtained (157 mg, 63% yield).

This method was used for the preparation of Intermediate 16 using suitable starting materials:

Intermediate 17 was prepared following the experimental procedure described for the synthesis of Intermediate 10, using suitable starting materials:

Intermediates 18-19 were prepared following the experimental procedure described for the synthesis of Intermediate 1, using suitable starting materials:

Intermediates 20-22 were prepared following the experimental procedure described for the synthesis of Intermediate 13, using 4,4,5,5-tetramethyl-2-vinyl-1,3,2-dioxaborolane in Step 1 and suitable starting materials:

Intermediate 23: (R)-2-(Trimethylsilyl)ethyl (3-(2-(2-oxoethyl)phenoxy)-3-(thiophen-2- yl)propyl)carbamate.

Step 1. (R)-2-(3-Hydroxy-3-(thiophen-2-yl)propyl)isoindoline-1,3-dione: To a solution of (R)-3-chloro-1-(thiophen-2-yl)propan-1-ol (2 g, 11.3 mmol) in anhydrous DMF (10 mL), potassium phthalimide (3.98 g, 21.5 mmol) and potassium iodide (56 mg, 0.34 mmol) were added and the mixture was heated at 100 ºC for 3 h. Water and NaHCO₃ sat. were added and the mixture was stirred at r.t. for 30 min. The phases were separated and the aqueous phase was extracted with EtOAc. The combined organic extacts were washed with water and brine, dried over MgSO₄, 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-(thiophen-2-yl)propan-1-ol: A solution of the compound obtained in Step 1 (2.5 g, 8.74 mmol) and ) and hydrazine hydrate (4.25 mL, 43.7 mmol) in MeOH (200 mL) was stirred at r.t. overnight. The resulting suspension was filtered and the solids were washed with MeOH. The filtrate was concentrated to dryness, resuspended in MeOH and eluted through a C₁₈ cartridge. The solvent was concentrated, and the resulting solid residue was suspended in CHCl₃ (50 mL) and stirred at r.t. for 1 h. The solids were removed by filtration and the filtrate was concentrated to dryness to afford the title compound (1.02 g, 75% yield).

Step 3. (R)-3-(2-Bromophenoxy)-3-(thiophen-2-yl)propan-1-amine: Following the experimental procedure described in Step 2 of Intermediate 1, starting from the product obtained in Step 2, the title compound was obtained (1.75 g, 86% yield).

Step 4. (R)-2-(Trimethylsilyl)ethyl (3-(2-bromophenoxy)-3-(thiophen-2- yl)propyl)carbamate: Following the experimental procedure described in Step 3 of Intermediate 1, starting from the product obtained in Step 3, the title compound was obtained (1.6 g, 68% yield).

Step 5. (R)-2-(Trimethylsilyl)ethyl (3-(2-allylphenoxy)-3-(thiophen-2- yl)propyl)carbamate: Following the experimental procedure described in Step 1 of Intermediate 13, starting from the product obtained in Step 4, the title compound was obtained (463 mg, 52% yield).

Step 6. Title compound: Following the experimental procedure described in Step 2 of Intermediate 13, starting from the product obtained in Step 5, the title compound was obtained (321 mg, 81% yield).

Synthesis of Examples General Deprotection Methods Method 1. Teoc deprotection with CsF. A solution of the N-Teoc protected compound (1 mmol) and cesium fluoride (5 mmol) in DMF (26 mL) was heated at 90 ºC 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). Method 2. Boc deprotection with ZnBr₂. A solution of the N-Boc protected compound (1 mmol) in DCM (5 mL) was added to a stirred suspension of ZnBr₂ (5.7 mmol) in DCM (50 mL) under a N₂ atmosphere. After stirring the mixture at r.t. overnight, water was added and it was stirred for 5 min. The layers were separated and the aqueous phase was extracted with DCM. The combined organic extracts were dried over MgSO₄ and concentrated. The crude compound was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4).

Example 1: N-(1-(2-(3-(Methylamino)-1-(thiophen-2-yl)propoxy)phenyl)piperidin-4-yl)- N-phenylpropionamide

Step 1. 2-(Trimethylsilyl)ethyl methyl(3-(2-(4-(N-phenylpropionamido)piperidin-1- yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate: In a sealed tube, a mixture of Intermediate 4 (80 mg, 0.170 mmol), N-phenyl-N-(piperidin-4-yl)propionamide (46 mg, 0.201 mmol), Pd₂(dba)₃ (15.5 mg, 0.017 mmol), BINAP (21 mg, 0.034 mmol) and sodium tert-butoxide (49 mg, 0.51 mmol) in dry toluene (3.2 mL) was heated at 130 ºC overnight under an argon atmosphere. The reaction mixture was filtered through a pad of Celite that was washed with EtOAc. The filtrate was concentrated to dryness and the residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (88 mg, 83% yield). Step 2. Title compound: Starting from the compound obtained in Step 1 (88 mg, 0.141 mmol) and following General Deprotection Method 1, the title compound was obtained (45 mg, 67% yield).

HPLC retention time: 5.54 min; MS: 478.2 (M+H).

Example 2: (R)-N-(1-(2-((2-(3-(Methylamino)-1-(thiophen-2-yl)propoxy)phenyl)amino)- 2-oxoethyl)piperidin-4-yl)-N-phenylpropionamide

Step 1. N-(1-(2-Amino-2-oxoethyl)piperidin-4-yl)-N-phenylpropionamide: A mixture of N-phenyl-N-(piperidin-4-yl)propionamide (150 mg, 0.646 mmol), 2-bromoacetamide (95 mg, 0.691 mmol), KI (11 mg, 0.065 mmol) and K2CO3 (98 mg, 0.710 mmol) in ACN (6.5 mL) was heated at 50 ºC overnight. The suspension was filtered, the collected solids were washed with ACN and discarded, and the filtrate was concentrated to dryness to afford the title compound (225 mg, overweight, quant. yield assumed), which was used without further purification.

Step 2. (R)-2-(Trimethylsilyl)ethyl methyl(3-(2-(2-(4-(N-phenylpropionamido)piperidin- 1-yl)acetamido)phenoxy)-3-(thiophen-2-yl)propyl)carbamate: In a sealed tube, a mixture of Intermediate 3 (116 mg, 0.247 mmol), the product obtained in Step 1 (112 mg, 83 wt%, 0.321 mmol), N¹,N²-dimethylethane-1,2-diamine (8 ^L, 0.074 mmol), copper(I) iodide (14 mg, 0.074 mmol) and potassium phosphate (105 mg, 0.494 mmol) in 1,4-dioxane (3.5 mL) was heated at 120 ºC overnight under an argon atmosphere. Additional N¹,N²-dimethylethane-1,2-diamine (8 ^L, 0.074 mmol) and copper(I) iodide (14 mg, 0.074 mmol) were added and the reaction mixture was again heated at 120 ºC overnight. The mixture was then filtered through a pad of Celite that washed with DCM. 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 (105 mg, 63% yield). Step 3. Title compound: Starting from the compound obtained in Step 2 (105 mg, 0.155 mmol) and following General Deprotection Method 1, the title compound was obtained (65 mg, 79% yield).

HPLC retention time: 4.94 min; MS: 535.2 (M+H). This method was used for the preparation of Examples 3-4 using suitable starting materials:

Example 5: N-(1-(2-(3-(Methylamino)-1-(thiophen-2-yl)propoxy)phenethyl)piperidin-4- yl)-N-phenylpropionamide

Step 1. N-(1-(2-(3-Chloro-1-(thiophen-2-yl)propoxy)phenethyl)piperidin-4-yl)-N- phenylpropionamide: A solution of Intermediate 8 (1.37 g, 4.65 mmol), N-phenyl-N- (piperidin-4-yl)propionamide (0.756 g, 3.25 mmol) and DIPEA (0.971 mL, 5.58 mmol) in DCE (13.7 mL) was stirred for 30 min at r.t. under a N2 atmosphere. Then, sodium triacetoxyborohydride (1.97 g, 9.29 mmol) was added and the reaction mixture was stirred at r.t. overnight. NaHCO₃ sat. solution was added and it was extracted with DCM. The combined organic phases were washed with brine, dried over MgSO₄ 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 (567 mg, 24% yield).

Step 2. Title compound: A solution of the compound obtained in Step 1 (0.567 g, 1.1 mmol) and methylamine (33 wt% solution in EtOH, 8.3 mL, 66.6 mmol) was heated in a sealed tube at 50 ºC overnight. The solvent was evaporated to dryness, the residue was redissolved in DCM and it was washed with 1 N NaOH aq. solution. The organic phase was dried over MgSO₄, 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 (273 mg, 48% yield).

HPLC retention time: 5.28 min; MS: 506.2 (M+H). This method was used for the preparation of Examples 6-28 using suitable starting materials:

Example 29: (R)-N-(1-(2-(3-(Methylamino)-1-(thiophen-2- yl)propoxy)phenethyl)piperidin-4-yl)-N-(pyridin-3-yl)propionamide

Step 1. (R)-2-(Trimethylsilyl)ethyl methyl(3-(2-(2-(4-(N-(pyridin-3- yl)propionamido)piperidin-1-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate: Following the experimental procedure described in Step 1 of Example 5, starting from Intermediate 12 (203 mg, 0.437 mmol) and N-(piperidin-4-yl)-N-(pyridin-3- yl)propionamide trifluoroacetate (202 mg, 0.437 mmol), the title compound was obtained (86 mg, 30% yield).

Step 2. Title compound: Starting from the compound obtained in Step 1 (86 mg, 0.132 mmol) and following General Deprotection Method 1, the title compound was obtained (30 mg, 45% yield).

HPLC retention time: 4.31 min; MS: 506.9 (M+H). This method was used for the preparation of Examples 30-34 using suitable starting materials:

Example 35: N-(1-(2-(3-Amino-1-(thiophen-2-yl)propoxy)benzyl)piperidin-4-yl)-N- phenylpropionamide

Step 1. N-(1-(2-(3-Chloro-1-(thiophen-2-yl)propoxy)benzyl)piperidin-4-yl)-N- phenylpropionamide: Following the experimental procedure described in Step 1 of Example 5, but starting from Intermediate 7 (164 mg, 0.584 mmol) instead of Intermediate 8, the title compound was obtained (203 mg, 70% yield). Step 2. N-(1-(2-(3-(1,3-Dioxoisoindolin-2-yl)-1-(thiophen-2-yl)propoxy)benzyl)piperidin- 4-yl)-N-phenylpropionamide: A solution of the compound obtained in Step 1 (155 mg, 0.312 mmol), potassium phthalimide (220 mg, 1.18 mmol) and KI (3 mg, 0.02 mmol) in DMF (1.6 mL) was heated at 100 ºC for 4 h. After cooling down to r.t., water was added and the mixture was stirred for 30 min. It was diluted with additional water and DCM, the phases were separated and the aqueous layer was extracted with DCM. The combined organic extracts were dried over MgSO₄, filtered and concentrated to dryness to give the title compound (133 mg, 70% yield).

Step 3. Title compound: A solution of the product obtained in Step 2 (133 mg, 0.219 mmol) and hydrazine hydrate (0.09 mL, 1.92 mmol) in MeOH (1.3 mL) was heated at 65 ºC for 1 h. The resulting suspension was filtered and the solids were washed with DCM. Water was added to the filtrate and it was extracted with DCM. The combined organic phases were washed with brine, dried over Na₂SO₄, filtered and concentrated. The crude product was purified by flash chromatography, C₁₈, gradient NH₄HCO₃ pH 8 to ACN to give the title compound (14 mg, 13% yield).

HPLC retention time: 5.21 min; MS: 478.2 (M+H).

Example 36: (R)-N-(1-(2-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)piperidin- 4-yl)-N-phenylpropionamide

Step 1. N-Phenyl-N-(1-((trifluoro- ^⁴-boranyl)methyl)piperidin-4-yl)propionamide, potassium salt: A schlenk flask was loaded with N-phenyl-N-(piperidin-4- yl)propionamide (220 mg, 0.95 mmol) and potassium (bromomethyl)trifluoroborate (228 mg, 1.13 mmol) and then it was evacuated and backfilled with argon three times. A mixture of THF-^tBuOH 2:1 (5 mL, previously degassed by bubbling argon through it) was added, the reaction mixture was purged with argon and it was heated at 85 ºC overnight. The solvent 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 (254 mg, 76% yield).

Step 2. (R)-2-(Trimethylsilyl)ethyl methyl(3-(2-((4-(N-phenylpropionamido)piperidin-1- yl)methyl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate: In a sealed tube, a mixture of Intermediate 3 (165 mg, 0.35 mmol), the product obtained in Step 1 (124 mg, 0.35 mmol), Pd(OAc)₂ (14 mg, 0.063 mmol), XPhos (60 mg, 0.126 mmol) and Cs₂CO₃ (343 mg, 1.05 mmol) in a mixture of 1,4-dioxane-water (10:1, 2.5 mL) was heated at 110 ºC overnight under an argon atmosphere. The solvent was concentrated to dryness and the residue was partitioned between EtOAc and NaHCO₃ sat. solution. The phases were separated and the aqueous phase was extracted with EtOAc. The combined organic phases were washed with brine, dried over MgSO₄, 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 (173 mg, 78% yield).

Step 3. Title compound: Starting from the compound obtained in Step 2 (173 mg, 0.272 mmol) and following General Deprotection Method 1, the title compound was obtained (86 mg, 64% yield).

HPLC retention time: 5.26 min; MS: 492.2 (M+H).

This method was used for the preparation of Examples 37-42 using suitable starting materials:

Examples 43 and 44: N-(1-((S)-1-(2-((S)-3-(Methylamino)-1-(thiophen-2- yl)propoxy)phenyl)ethyl)piperidin-4-yl)-N-phenylpropionamide and N-(1-((R)-1-(2-((S)- 3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)ethyl)piperidin-4-yl)-N- phenylpropionamide

Step 1a and 1b. 2-(Trimethylsilyl)ethyl methyl((S)-3-(2-((S)-1-(4-(N- phenylpropionamido)piperidin-1-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate and 2-(Trimethylsilyl)ethyl methyl((S)-3-(2-((R)-1-(4-(N-phenylpropionamido)piperidin- 1-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate: A mixture of Intermediate 15 (133 mg, 0.2 mmol) and Ti(OⁱPr)₄ (0.59 mL, 2.0 mmol) was heated at 65 ºC for 6 h. Then a solution of sodium cyanoborohydride (110 mg, 1.75 mmol) in EtOH (4 mL) was added dropwise and the reaction mixture was stirred at 60 ºC overnight. The solvent was evaporated and the residue was partitioned between NaHCO3 sat. sol. and DCM. The aqueous phase was extracted with DCM and the combined organic extracts were washed with brine, dried over MgSO4 and concentrated to dryness to afford a 1:1 mixture of the two diastereomers which were separated by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compounds Step 1a (12 mg, 9% yield) and Step 1b (6 mg, 4% yield).

Step 2a and 2b. Title compounds: Starting from the compound obtained in Step 1a (12 mg, 0.018 mmol) and following General Deprotection Method 1, Example 43 was obtained (4 mg, 42% yield).

HPLC retention time: 5.38 min; MS: 506.3 (M+H). Following an analogous procedure but starting from Step 1b, Example 44 was obtained. HPLC retention time: 5.17 min; MS: 506.3 (M+H).

Examples 45 and 46: (S)-N-(1-(2-(3-(Methylamino)-1-(thiophen-2- yl)propoxy)phenethyl)piperidin-4-yl)-N-phenylpropionamide and (R)-N-(1-(2-(3- (methylamino)-1-(thiophen-2-yl)propoxy)phenethyl)piperidin-4-yl)-N- phenylpropionamide

Starting from Example 5, a chiral preparative HPLC separation (column: Chiralpak IA; temperature: ambient; flow: 13 mL/min; eluent: n-Heptane/(EtOH + 0.33% DEA) 85/15 v/v) was carried out to give the title compounds.

Examples 47 and 48: N-(1-((R)-1-(2-((R)-3-(Methylamino)-1-(thiophen-2- yl)propoxy)phenyl)ethyl)piperidin-4-yl)-N-phenylpropionamide and N-(1-((S)-1-(2-((R)- 3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)ethyl)piperidin-4-yl)-N- phenylpropionamide

Following the procedure described for the preparation of Examples 43 and 44 butstarting from Intermediate 16, the title compounds were obtained. HPLC retention time: 5.10 min; MS: 506.3 (M+H) and 5.14 min; MS: 506.3 (M+H). Following the method described for the synthesis of Example 29, using suitable starting materials, Examples 49-54 were prepared:

Examples 55 and 56: N-((3S,4R)-1-(2-((R)-3-(Ethylamino)-1-(thiophen-2- yl)propoxy)phenethyl)-3-fluoropiperidin-4-yl)-N-(pyridin-3-yl)propionamide and N- ((3R,4S)-1-(2-((R)-3-(ethylamino)-1-(thiophen-2-yl)propoxy)phenethyl)-3- fluoropiperidin-4-yl)-N-(pyridin-3-yl)propionamide

Step 1. 2-(Trimethylsilyl)ethyl ethyl((R)-3-(2-(2-((3R,4S)-3-fluoro-4-(N-(pyridin-3- yl)propionamido)piperidin-1-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate and 2-(trimethylsilyl)ethyl ethyl((R)-3-(2-(2-((3S,4R)-3-fluoro-4-(N-(pyridin-3- yl)propionamido)piperidin-1-yl)ethyl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate: Following the experimental procedure described in Step 1 of Example 5, starting from Intermediate 13 (142 mg, 0.317 mmol) and cis-N-(3-fluoropiperidin-4-yl)-N-(pyridin-3- yl)propionamide trifluoroacetate (111 mg, 0.317 mmol), the title compounds were obtained as a 1:1 mixture of stereoisomers (104 mg, 48% yield). Step 2. N-((3S,4R)-1-(2-((R)-3-(Ethylamino)-1-(thiophen-2-yl)propoxy)phenethyl)-3- fluoropiperidin-4-yl)-N-(pyridin-3-yl)propionamide and N-((3R,4S)-1-(2-((R)-3- (ethylamino)-1-(thiophen-2-yl)propoxy)phenethyl)-3-fluoropiperidin-4-yl)-N-(pyridin-3- yl)propionamide: Starting from the mixture of compounds obtained in Step 1 (104 mg, 0.152 mmol) and following General Deprotection Method 1, the title compounds were obtained as a 1:1 mixture of stereoisomers (43 mg, 52% yield). Step 3. Starting from the mixture of products obtained in Step 2, a chiral preparative HPLC separation (column: Chiralpak IC; temperature: ambient; flow: 10 mL/min; eluent: n-Heptane/(EtOH + 0.2% DEA) 70/30 v/v) was carried out to give the title compounds. HPLC retention time: 4.65 min; MS: 539.3 (M+H).

Table of Examples with binding to the µ-opioid Receptor and the ^2 ^-1 Subunit of the voltage-gated calcium channel: BIOLOGICAL ACTIVITY

Pharmacological study Human ^₂ ^ ^ ^ subunit of Ca_v2.2 calcium channel ^assay

Human ^ ^ ^ ^ ^ enriched membranes (2.5 µg) were incubated with 15 nM of radiolabeled [3H]-Gabapentin in assay buffer containing Hepes-KOH 10mM, pH 7.4. NSB (non specific binding) was measured by adding 10 µM pregabalin. The binding of the test compound was measured at five different concentrations. After 60 min incubation at 27 ºC, binding reaction was terminated by filtering through Multiscreen GF/C (Millipore) presoaked in 0.5 % polyethyleneimine in Vacuum Manifold Station, followed by 3 washes with ice-cold filtration buffer containing 50 mM Tris-HCl, pH 7.4. Filter plates were dried at 60 ºC for 1 hour and 30 µl of scintillation cocktail were added to each well before radioactivity reading. Readings were performed in a Trilux 1450 Microbeta radioactive counter (Perkin Elmer).

Human μ-opioid receptor radioligand assay Transfected CHO-K1 cell membranes (20 μg) were incubated with [³H]-DAMGO (1 nM) in assay buffer containing Tris-HCl 50 mM, MgCl2 5 mM at pH 7.4. NBS (non-specific binding) was measured by adding 10 μM Naloxone. The binding of the test compound was measured at five different concentrations. Plates were 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 plates were washed 3 times with ice-cold 10 mM Tris–HCl (pH 7.4). Filters were dried and counted at approximately 40% efficiency in a MicroBeta scintillation counter (Perkin-Elmer) using EcoScint liquid scintillation cocktail.

Results:

As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the ^₂^^ subunit of voltage-gated calcium channels and the µ-opioid receptor it is a very preferred embodiment in which the compounds are selected which act as dual ligands of the ^_^^^ subunit of voltage- gated calcium channels and the µ-opioid receptor and especially compounds which have a binding expressed as Ki responding to the following scales:

Ki(^2^-1) is preferably < 10000 nM, more preferably < 5000 nM, or even more preferably < 500 nM.

The following scale has been adopted for representing the binding to µ-opioid receptor 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 for representing the binding to the ^₂^^^ subunit of voltage-gated calcium channels expressed as K_i: + K_i(^₂^-1) >= 5000 nM

++ 500nM <= K_i(^₂^-1) <5000 nM

+++ K_i(^₂^-1) <500 nM All compounds prepared in the present application exhibit binding to the ^₂^^^ subunit of voltage-gated calcium channels and the µ-opioid receptor, in particular the following binding results are shown:

Claims

CLAIMS: 1. Compound of general formula (I),

wherein X is selected from a bond, -[C(R_aR_b)]_p-, -[CH₂]_pC(O)[CH₂]_q-, -[CH₂]_pC(O)N(R_z)[CH₂]_q- , -[CH₂]_pN(R_z)C(O)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_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, taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl;

n is 0 or 1; Y1 is–C(R10R10’)-; wherein R₁₀ 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, R₁₀ and R_10’ form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

R1 is

wherein m is 0, 1 or 2; r is 0, 1 or 2;

R7 is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl and – C(O)OR71; wherein R71 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; R₈ is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl;

R8’ is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, - NR₈₂R_82’, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein R₈₂ and R_82’ 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;

R3’ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R₄ and R_4’ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R_41’, - NR41C(O)R41’, -NR41S(O)2R41’, -S(O)2NR41R41’, -NR41C(O)NR41’R41’’, -SR41 , -S(O)R41, - S(O)2R41,–CN, haloalkyl, haloalkoxy, -C(O)OR41, -C(O)NR41R41’, -OCH2CH2OR41, - NR41S(O)2NR41’R41’’ and -C(CH3)2OR41; wherein R41, R41’ and R41’’ 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 form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

2. Compound according to claim 1 wherein R₂ is a substituted or unsubstituted group selected from phenyl and thienyl.

3. Compound according to any one of claims 1 or 2 wherein the compound of Formula (I) is a compound of Formula (I’), (I^a), (I^a’), (I^b) or (I^b’),

(I^b),

(I^b’), wherein R₉ and R_9’ are independently selected from hydrogen, halogen, - R₂₁, -OR₂₁, -NO₂, -NR₂₁R_21’, -NR₂₁C(O)R_21’, -NR₂₁S(O)₂R_21’, -S(O)₂NR₂₁R_21’, - NR₂₁C(O)NR_21’R_21’’, -SR₂₁ , -S(O)R₂₁, -S(O)₂R₂₁, –CN, haloalkyl, haloalkoxy, -C(O)OR₂₁, -C(O)NR₂₁R_21’, -OCH₂CH₂OR₂₁, - NR₂₁S(O)₂NR_21’R_21’’ and -C(CH₃)₂OR₂₁; wherein R₂₁, 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;

4. Compound according to any one of claims 1 to 3 wherein R8 is selected from substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; preferably R8 is a substituted or unsubstituted group selected from phenyl, pyridinyl and pyrazolyl, whereas R8’ is selected from substituted or unsubstituted C1-6 alkyl and substituted or unsubstituted heterocyclyl; preferably R_8’ is a substituted or unsubstituted group selected from methyl, ethyl, thienyl and furanyl.

5. Compound according to any one of claims 1 to 3 wherein R8 and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted cyclic amide or substituted or unsubstituted cyclic urea; preferably R₈ and R8’, taken together with the–N(CO)- atoms to which they are attached form a substituted or unsubstituted indolin-2-one or substituted or unsubstituted 1H- benzo[d]imidazol-2(3H)-one.

6. Compound according to any one of claims 1 to 5 wherein X is a bond or a group selected from -CH₂-, -CH(CH₃)-, -CH₂CH₂- and -NHC(O)CH₂-; preferably selected from -CH₂- and -CH₂CH₂-.

7. Compound according to any one of claims 1 to 6 wherein

p is 0, 1, 2, 3, 4 or 5; preferably p is 0, 1 or 2; more preferably p is 1 or 2.

8. Compound according to any one of claims 1 to 7 wherein

q is 0, 1, 2, 3, 4 or 5; preferably q is 1.

9. Compound according to any one of claims 1 to 8 wherein the compound is selected from

(

(

( (

( ( (

(

( ( (

(

( (

(

( (

and/or

10. Process for the preparation of compounds of Formula (I) as defined in any one of claims 1 to 9,

(I) a) wherein X represents a bond, and wherein R1, R2, R3, R3’, R4, R4’, Y1, Y2 and n have the meanings as defined in the preceding claims, said process comprises treating a compound of formula (IIa),

under standard Buchwald-Hartwig or Ullmann arylation conditions;

or

b) wherein -X- represents -[C(R_aR_b)]_p-, and wherein R_a, R_b, R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ and n and p have the meanings as defined in the preceding claims, said process comprises treating a compound of formula (IIb’)

under standard reductive amination conditions;

or

c) wherein -X- represents -[C(R_aR_b)]_p-, and wherein R_a, R_b, R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ and n and p have the meanings as defined in the preceding claims, said process comprises treating a compound of formula (IIa),

wherein M represents a suitable organometallic group, preferably a boron or zinc reagent, and p has the meaning as defined in the preceding claims;

or d) wherein -X- represents -[CRaRb]pC(O)[CH2]q- and q is 0, and wherein Ra and Rb are hydrogen and R1, R2, R3, R3’, R4, R4’, Y1, Y2, n, p and q have the meanings as defined in the preceding claims, said process comprises treating a compound of formula (IIc’)

with a N-containing cyclic reagent of formula (III-1)

under conventional amidation conditions;

or

e) wherein -X- represents -[CRaRb]pN(Rz)C(O)[CH2]q-, and wherein Ra and Rb are hydrogen and R1, R2, R3, R3’, R4, R4’, Y1, Y2 , n, p and q have the meanings as defined in the preceding claims, said process comprises treating a compound of formula (VI’)

wherein LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, p, q and Rz have the meanings as defined in the preceding claims, with a N-containing cyclic reagent of formula (III-1)

under conventional alkylation conditions;

or

f) wherein -X- represents -[CR_aR_b]_pN(R_z)C(O)[CH₂]_q-, and wherein R_a and R_b are hydrogen and R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂, n, p and q have the meanings as defined in the preceding claims, said process comprises treating an amino compound of formula (IId’)

wherein p and Rz have the meanings as defined in the preceding claims, with an acyl reagent of formula (III-3),

under amidation conditions, wherein Z represents OH or halogen and q has the meaning as defined in the preceding claims;

or g) wherein -X- represents -[CR_aR_b]_pN(R_z)C(O)[CH₂]_q-, p is 0, and wherein R_a and R_b are hydrogen and R₁, R₂, R₃, R_3’, R₄, R_4’, Y₁, Y₂ , n, p and q have the meanings as defined in the preceding claims, said process comprises reacting a compound of formula (IIa)

under Ullmann arylation conditions, wherein q and Rz have the meanings as defined in the preceding claims;

or

h) wherein n is 0, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in the preceding claims, said process comprises reacting a compound of formula (VIIa) wherein G is OH,

with an alkylating agent of formul

or

i) wherein n is 0, and wherein R1, R2, R3, R3’, R4, R4’, X, Y1 and Y2 have the meanings as defined in the preceding claims, said process comprises reacting a compound of formula (VIIa) wherein G is OH,

with an alcoholof formula (VIII) wherein Z represents OH,

in the presence of a suitable azo compound;

or

j) wherein n is 0, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in the preceding claims, said process comprises reacting a compound of formula (VIIa) wherein G is halogen,

with an alcoholof formula (VIII) wherein Z represents OH,

in the presence of a strong base;

or

k) wherein n is 1, and wherein R₁, R₂, R₃, R_3’, R₄, R_4’, X, Y₁ and Y₂ have the meanings as defined in the preceding claims, said process comprises reacting a compound of formula (VIIb)

with an agent of formula (VIII),

11. Use of the compounds of Formula 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’-LG

,

,

for the preparation of compounds of Formula (I) as defined in any one of claims 1 to 9.

12. A pharmaceutical composition which comprises a compound of Formula (I) as defined in any one of claims 1 to 9 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

13. A compound of Formula (I) as defined in any one of claims 1 to 9 for use as a medicament.

14. A compound of Formula (I) as defined in any one of claims 1 to 9 for use as a medicament; preferably for use as a medicament for the treatment of pain, especially medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia or hyperalgesia.