WO2019110137A1

WO2019110137A1 - O-phenoxy and o-benzyloxypropylamino derivatives having activity against pain

Info

Publication number: WO2019110137A1
Application number: PCT/EP2018/000541
Authority: WO
Inventors: Carmen ALMANSA-ROSALES; Marina VIRGILI-BERNADÓ; Monica Alonso-Xalma
Original assignee: Esteve Pharmaceuticals, S.A.
Priority date: 2017-12-04
Filing date: 2018-12-03
Publication date: 2019-06-13
Also published as: TW201938154A; AR113910A1

Abstract

The present invention relates to o-phenoxy and o-benzyloxypropylamino derivatives (I) having pharmacological activity towards the α2δ subunit, in particular the a2S-1 subunit, of the voltage-gated calcium channel, 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

O-PHENOXY AND O-BENZYLOXYPROPYLAMINO DERIVATIVES HAVING

ACTIVITY AGAINST PAIN

FIELD OF THE INVENTION

The present invention relates to compounds having pharmacological activity towards both the a₂d subunit of the voltage-gated calcium channel, and more particularly to o- phenoxy and o-benzyloxypropylamino 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.; 201 1 ; 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.; 201 1 ; BMC Public Health ; 1 1 ; 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. 2015 67:821-70). The VGCC are assembled through interactions of different subunits, namely on (Ca_vai), b (Ca_vp) a₂d (Ca_vot₂5) and g (Ca_vy). The oti subunits are the key porous forming units of the channel complex, being responsible for the Ca²⁺ conduction and generation of Ca²⁺ influx. The a₂d, b, and g subunits are auxiliary, although very important for the regulation of the channel, since they increase the expression of the oti 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 (Ca_v3.1 , Ca_v3.2, and Ca_v3.3), and high voltage-activated L- (Ca_v1.1 through Ca_v1.4), N-(Ca_v2.2), P/Q-(Ca_v2.1), and R-(Ca_v2.3) types, depending on the channel forming Cava 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. 2009 6:679-92; 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. 2012 167:970-89.).

The Ca_v1 and Ca_v2 subfamilies contain an auxiliary a₂d 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 a₂d subunits, each encoded by a unique gene and all possessing splice variants. Each a₂d protein is encoded by a single messenger RNA and is post-translationally cleaved and then linked by disulfide bonds. Four genes encoding a₂d subunits have now been cloned. a₂d-1 was initially cloned from skeletal muscle and shows a fairly ubiquitous distribution. The a₂d-2 and a₂d-3 subunits were subsequently cloned from brain. The most recently identified subunit, a₂d-4, is largely non-neuronal. The human a₂d-4 protein sequence shares 30, 32 and 61 % identity with the human a₂d-1 , a₂d-2 and a₂d-3 subunits, respectively. The gene structure of all a₂d subunits is similar. All a₂d subunits show several splice variants (Davies et al., Trends Pharmacol Sci. 2007 28:220-8.; Dolphin AC, Nat Rev Neurosci. 2012 13:542-55., Biochim Biophys Acta. 2013 1828:1541-9.).

The Ca_va₂6-1 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_va₂6-1 , but not Ca_vct₂8-2, 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_va₂5-1 subunit to the central presynaptic terminals diminishes tactile allodynia in nerve injured animals, suggesting that elevated DRG Ca_v(¾28-1 subunit contributes to neuropathic allodynia.

The Ca_vcx₂6-1 subunit (and the Ca_va₂5-2, but not Ca_vcx₂5-3 and Ca_va₂5-4, subunits) is the binding site for gabapentin which has anti-allodynic/ hyperalgesic properties in patients and animal models. Because injury-induced Ca_vot₂5-1 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_va₂5-1 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_va₂5-1 subunit can block nerve injury-induced Ca_va₂5-1 upregulation and prevent the onset of allodynia and reserve established allodynia.

As mentioned above, the a_åd 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 Ca_vcc₂5 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).

Thus, the present application, relates to the advantages of having activity for the ct₂5-1 subunit of voltage-gated calcium channels to treat chronic pain.

In this way, the present invention relates to compounds having a mechanism of action (blocker of the 0₂6 subunit, in particular the a₂d-1 subunit, of voltage-gated calcium channels) which implies a beter efficacy and tolerability than gabapentinoids (pregabalin and gabapentin).

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 series of compounds that show pharmacological activity towards the a₂d subunit, in particular the a₂d-1 subunit, of the voltage-gated calcium channel, 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 relevant for the treatment of pain. This was mainly achieved by providing the compounds according to the invention that bind to the a₂d subunit, in particular the a₂d-1 subunit, of the voltage-gated calcium channel.

SUMMARY OF THE INVENTION

In this invention a family of structurally distinct o-phenoxy and o-benzyloxypropylamino derivatives, encompassed by formula (I), which have a pharmacological activity towards the a₂d subunit, in particular the a₂d-1 subunit, of the voltage-gated calcium channel, was identified, thus solving the above problem of identifying alternative or improved pain treatments by offering such compounds.

The main object of the invention is directed to a compound having an activity binding to the a₂d subunit, in particular the a₂d-1 subunit, of the voltage-gated calcium channel, 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 ligands of the a₂d subunit, in particular the a₂d-1 subunit, of the voltage-gated calcium channel, it is a very preferred embodiment if the compound has a binding expressed as K, responding to the following scales: K,(a₂d-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 Ri, R₂, R₃, R_3', R₄, R₄ , X, Ui, 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

As this invention is aimed at providing a compound or a chemically related series of compounds which act as ligands of the a₂d subunit, in particular the a₂d-1 subunit, of the voltage-gated calcium channel, it is a very preferred embodiment if the compound has a binding expressed as K, responding to the following scales:

Ki(a₂d-1 ) is preferably < 10000 nM, more preferably < 5000 nM, even more preferably

< 500 nM or even more preferably < 100 nM.

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

wherein X is selected from a bond, -[C(R_aRt_>)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_PC(0)N(R_z)[CH2]q-, - [CH₂]_pN(R_z)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-; R_a is selected from hydrogen, halogen, substituted or unsubstituted C1-6 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, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-e alkyl; p is 0, 1 , 2, 3, 4 or 5; q is O, 1 , 2, 3, 4 or 5;

Y 1 is— C(RioRio )-; 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 C2-6 alkynyl; alternatively, R₁₀ and R₁₀ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is— C(Rio' Rio ) ; 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 R₁₀ · may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; n is 0 or 1 ;

Ri is selected from, -NR5R5' and -NR₅ C(0)Rs;

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

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

R₃ is selected from hydrogen, substituted or unsubstituted C1 -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 , - NR₄I C(0)R₄I , -NR₄I S(0)₂R₄I , -S(0)₂NR4iR₄r, -NR₄I C(0)NR₄I R₄r , -SR41 , -S(0)R_4i, - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i , -C(0)NR₄I R₄I , -OCH2CH2OR41 , - NR4iS(0)₂NR4i'R4i and -C(CH₃)₂OR4i ; wherein R₄₁ , R₄₁ and R₄₁ are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Rs is selected from 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, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl , substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl;

R₅ is selected from hydrogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-6 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 particular embodiment, if X is selected from -[CH₂]pC(0)N(Rz)[CH₂]_q-, and - [CH2]pN(R_z)[CH₂]q-, q is 1 , 2, 3, 4 or 5.

In another particular embodiment if X is selected from a bond, -[C(R_aR_b)]_P-, - [CH₂]_pC(0)[CH₂]_q- and -[CH₂]pN(Rz)C(0)[CH₂]_q-, q is 0, 1 , 2, 3, 4 or 5; and if X is selected from -[CH₂]pC(0)N(Rz)[CH₂]_q- and -[CH₂]_PN(Rz)[CH₂]_q-, q is 1 , 2, 3, 4 or 5.

In a particular embodiment the following compounds are excluded:

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(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]pN(R_z)C(0)[CH₂]q- and -[CH₂]_pN(R_z)[CH₂]q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci.₆ alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2.6 alkynyl;

R_b is selected from hydrogen, halogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C₂.e alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted

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(0)-Ci-₆ alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;

Yi is— C(Rio io )-; 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 C2-6 alkynyl; alternatively, R₁₀ and R₁₀ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is— C(Rio"Rio’)-; wherein R₁₀ · and R₁₀ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2.6 alkynyl; alternatively, Rio- and R₁₀ · may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

n is 0 or 1 ;

R1 is selected from-NRsRs and -NR₅ C(0)R5;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, is substituted with one or more substituent/s selected from halogen, -R21 , -OR21, -NO2, -NR21R21 , -NR₂₁C(0)R₂₁ , -NR21S(0)₂R₂₁ , -S(0)₂NR_2iR2r, - NR₂IC(0)NR₂I R₂r , -SR21 , -S(0)R2i , -S(0)2R2i, -CN, haloalkyl, haloalkoxy, -C(0)0R2i, -

C(0)NR₂₁R₂₁ , -OCH2CH2OR21, -NR21S(0)₂NR₂₁ R21 and -C(CH₃)20R₂I ; wherein R21, R21' and R₂r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₃ 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 and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, is substituted with one or more substituent/s selected from -OR₃₁, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R₃₁, -OR31 , -NO2, -NR₃₁R31 , - NR₃IC(0)R₃I , -NR₃₁S(0)₂R₃₁ , -S(0)₂NR₃₁R₃₁ , - NR₃IC(0)NR₃I R₃r , -SR31 , -S(0)R₃I , -S(0)₂R₃I , -CN, haloalkyl, haloalkoxy, -C(0)0R_3i, -

C(0)NR₃₁R₃₁ , -OCH2CH2OR31 , -NR₃₁S(0)₂NR₃₁ R31 and -C(CH₃)₂OR3i ;

wherein 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;

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; the alkyl, alkenyl or alkynyl defined in R₃ , if substituted, 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, substituted or unsubstituted C alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C₂.e alkynyl;

R₄ and R₄ are independently selected from halogen, -R₄₁, -OR₄I , -NO₂, -NR₄I R₄I , - NR₄I C(0)R₄I , -NR₄I S(0)₂R₄I , -S(0)₂NR₄I R₄I , -NR₄IC(0)NR₄I R_4r, -SR₄I , -S(0)R_4i , - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i , -C(0)NR₄I R₄I , -OCH₂CH₂OR₄I , - NR₄I S(0)₂NR₄I R₄I · and -C(CH₃)₂OR₄I ; wherein R₄I , R_4r and R₄r are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂.6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Rs is selected from 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, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl , substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR₅₁, halogen, -CN, haloalkyl, haloalkoxy and -NR51R51 ; wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroarylor alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s selected from halogen, -R₅₁, -OR₅₁, -N0₂, -NR₅₁R₅₁ , - NR_5IC(0)R_5I\ -NR_5iS(0)₂R5i , -S(0)₂NR_5I R_5I , - NR_5iC(0)NR₅rR5r, -SR51 , - S(0)R_5I, -S(0)₂R_5I , -CN, haloalkyl, haloalkoxy, -C(0)0R_5i, -C(0)NR_5iR₅r, - OCH2CH2OR51, -NR_5iS(0)₂NR5i'R5i and -C(CH₃)20R_5I ; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

wherein R₅₁, R₅₁ and R₅r 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;

R₅ is 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 alkyl, alkenyl or alkynyl defined in R₅ , if substituted, is substituted with one or more substituent/s selected from -OR₅₂, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; wherein R₅₂ and R₅₂ are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

the alkyl, alkenyl or alkynyl, 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 =0, -OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13 ; wherein Rn and R13 are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C_2-e alkenyl, and unsubstituted C₂.e 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 =0, halogen, -R14, -ORu, -NO2, -NR14R14 , - NRi₄C(0)Ri4·, -NRi₄S(0)₂Ri4 , -S(0)₂NRi₄Ri4 , - NRi₄C(0)NRi₄ Ri4··, -SRM , -S(0)Ri₄, - S(0)₂Ri₄, -CN, haloalkyl, haloalkoxy, -C(0)0Ri₄, -C(0)NRi₄Ri4 , -OCH₂CH₂ORi4, - NRi₄S(0)₂NRi4 R14 and -C(CH₃)₂ORI₄; wherein Ru, R14 and R14 are independently selected from hydrogen, unsubstituted Ci.₆ alkyl, unsubstituted C₂-e 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.

wherein

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted C 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 Ci-e alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2-e alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-e alkenyl, substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-e alkyl; if X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]_pC(0)[CH₂]_q- and -

[CH₂]_pN(R_z)C(0)[CH₂]_q-, q is 0, 1 , 2, 3, 4 or 5; and if X is selected from -[CH₂]_pC(0)N(R_z)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-, q is 1 , 2, 3, 4 or 5;

p is 0, 1 , 2, 3, 4 or 5;

Yi is— C(RioRio )-; wherein Rio and Rio are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C₂-e alkynyl; alternatively, R₁₀ and R₁₀ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

wherein R₁₀ and R₁₀ are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R10 and Rio ·· may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

n is 0 or 1 ;

R1 is selected from-NRsRs and -NRsCfOJRs;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, -NR21R21 , -NR_2IC(0)R_2I , -NR2iS(0)2R2r, -S(0)2NR2iR2i', - NR_2iC(0)NR_2i R2r , -SR21 , -S(0)R_2I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, - C(0)NR₂₁R₂₁ , -OCH2CH2OR21, -NR₂₁S(0)₂NR₂₁ R21 and -C(CH₃)₂OR2i; wherein R21 , R21 and R₂r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl; R3 is selected from substituted or unsubstituted Ci-_b alkyl, substituted or unsubstituted C₂-6 alkenyl, substituted or unsubstituted C₂.e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, is substituted with one or more substituent/s selected from -OR₃₁, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R31, -OR31, -NO2, -NR31R31 , - NR₃₁C(0)R₃₁ , -NR₃₁S(0)₂R₃₁ , -S(0)₂NR₃IR₃I , - NR₃IC(0)NR₃I Rsr, -SR31 , -S(0)R_3i, -S(0)₂R3i, -CN, haloalkyl, haloalkoxy, -C(0)0R3i, -

C(0)NR₃IR₃I , -OCH₂CH₂OR_3i, -NR₃IS(0)₂NR₃I R31 and -C(CH₃)₂OR₃I,

wherein R₃₁, R₃₁ and R₃₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂.6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

R3 is selected from hydrogen, substituted or unsubstituted C1 -6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2.6 alkynyl; the alkyl, alkenyl or alkynyl defined in R3', if substituted, 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, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C₂.e alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₄ and R₄ are independently selected from halogen, -R₄₁, -OR₄₁, -N0₂, -NR41R41 , - NR_4iC(0)R₄r, -NR₄IS(0)₂R₄I , -S(0)₂NR₄I R₄I , -NR₄IC(0)NR₄I R₄r , -SR41 , -S(0)R_4i, - S(0)₂R_4i, -CN, haloalkyl, haloalkoxy, -C(0)OR_4I , -C(0)NR_4iR ₁ , -OCH₂CH₂OR_4I , - NR_4IS(0)₂NR_4I R₄r and -C(CH₃)₂OR _I ; wherein R _I , R₄r and R₄r are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₅ is selected from substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR₅₁, halogen, -CN, haloalkyl, haloalkoxy and -NR51R51 ; wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R5, if substituted, is substituted with one or more substituent/s selected from halogen, -R51, -OR51, -N0₂, -NR51R51 , - NR_5iC(0)R₅r, -NR_5iS(0)₂R5i , -S(0)₂NR_5IR_5I , - NR_5IC(0)NR_5I Rsr, -SR51 , - S(0)R_5I , -S(0)₂R_5I , -CN, haloalkyl, haloalkoxy, -C(0)0R_5i, -C(0)NR_5I RSI , - OCH2CH2OR51, -NR₅₁S(0)₂NR₅₁ Rsr and -C(CH₃)₂OR5i; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl; wherein R₅₁, Rsr and R₅₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂.e alkenyl and substituted or unsubstituted C_2.6 alkynyl;

R₅ is selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C₂-6 alkynyl; wherein the alkyl, alkenyl or alkynyl defined in R5 , if substituted, is substituted with one or more substituent/s selected from -OR₅₂, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; wherein R52 and R52 are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C₂-6 alkenyl and substituted or unsubstituted C_2-e alkynyl;

the alkyl, alkenyl or alkynyl, 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 =0, -OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13 ; wherein R₁₃ and R₁₃ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C_2.6 alkenyl, and unsubstituted C_2-e 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 =0, halogen, -R14, -OR14, -N0₂, -NR14R14 , - NRi₄C(0)Ri₄ , -NRI₄S(0)₂RI₄ , -S(0)₂NRI₄RI₄·, - NRI₄C(0)NRI₄ RI₄ , -SRI₄ , -S(0)Ri₄, - S(0)₂RI₄, -CN, haloalkyl, haloalkoxy, -C(0)ORI₄, -C(0)NRI₄RI₄ , -OCH₂CH₂ORI₄, - NR_I4S(0)₂NRI₄ RI₄ · and -C(CH₃)₂0RI₄; wherein Ri₄, R_I4 and R are independently selected from hydrogen, unsubstituted C_1-6 alkyl, unsubstituted C_2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

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

wherein Ri, 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.

wherein

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(0)[CH₂]q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e 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 alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C₂-e alkynyl; alternatively, R_a and R_P, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂.e alkenyl, substituted or unsubstituted C_2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-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 selected from-NRsRs and -NRs C(0)R₅;

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

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

R₄ and R₄ are independently selected from halogen, -R_4I , -OR_4I , -NO2, -NR_4IR_4I , - NR_4IC(0)R_4V, -NR_4IS(0)₂R_4I , -S(0)₂N

S(0)₂R_4I , -CN, haloa!kyl, haloalkoxy,

NR_4IS(0)₂NR_4I R₄r and -C(CH₃)₂OR_4I ; wherein R_4I , R r and R₄r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2.e alkenyl and substituted or unsubstituted C_2.6 alkynyl;

Rs is selected from substituted or unsubstituted Ci.₆ alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C_2.e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylary! and substituted or unsubstituted alkylheteroaryl;

R₅ is selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C₂-e 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.

wherein X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(Rz)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl; R_b is selected from hydrogen, halogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C_2-e alkenyl and substituted or unsubstituted C₂.e alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl; R_z is selected from hydrogen, substituted or unsubstituted Ci-e 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(0)-Ci-₆ alkyl; p is O, 1 , 2, 3, 4 or 5; q is O, 1 , 2, 3, 4 or 5; n is 0 or 1 ;

R1 is selected from-NRsRs and -NR₅ C(0)R5;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, is substituted with one or more substituent/s selected from halogen, -R21 , -OR21, -NO2, -NR21R21', -NR₂IC(0)R₂I , -NR_2iS(0)₂R2i , -S(0)₂NR_2iR2i , - NR₂IC(0)NR₂I R21 , -SR21 , -S(0)R₂I , -S(0)₂R₂I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, - C(0)NR₂₁R₂₁ , -OCH2CH2OR21, -NR₂₁S(0)₂NR₂₁ R21 and -C(CH₃)₂OR2i; wherein R₂₁, R_{21 '} 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;

R3 is selected from substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R₃, if substituted, is substituted with one or more substituent/s selected from -OR₃₁, halogen, -CN, haloalkyl, haloalkoxy and -NR₃₁R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R31 , -OR31, -NO2, -NR31 R31 , - NR_3iC(0)R₃r, -NR₃IS(0)₂R₃I , -S(0)₂NR_3i R3i', - NR₃IC(0)NR₃I Rsr, -SR31 , -S(0)R₃I , -S(0)₂R₃I , -CN, haloalkyl, haloalkoxy, -C(0)0R3i , - C(0)NR₃₁ R₃₁ , -OCH2CH2OR31 , -NR3iS(0)₂NR₃rR3i and -C(CH₃)₂OR3i ;

wherein R₃I , R₃₁ and R₃₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₃ is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; the alkyl, alkenyl or alkynyl defined in R₃ , if substituted, 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 C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₄ and R₄ are independently selected from halogen, -R41 , -OR₄I , -N0₂, -NR₄IR₄I , - NR₄IC(0)R₄I , -NR₄IS(0)₂R₄I , -S(0)₂NR₄I R₄V, -NR₄IC(0)NR₄I R_4r , -SR₄I , -S(0)R_4i, - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i , -C(0)NR_4iR_4r, -OCH₂CH₂OR₄I , - NR₄IS(0)2NR₄I R₄r and -C(CH3)20R₄I ; wherein R₄I , R₄r and R₄r are independently selected from hydrogen, substituted or unsubstituted C1 -6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; Rs is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroarylor alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR51 , halogen, -CN, haloalkyl, haloalkoxy and -NR51 R51 ; wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s selected from halogen, -R51 , -OR51 , -N0₂, -NR51R51 , - NR₅I C(0)R₅I , -NR₅₁S(0)₂R₅₁ , -S(0)₂NR₅₁R51 , - NR₅IC(0)NR₅I Rsr , -SR51 , - S(0)Rsi, -S(0)₂R₅I , -CN, haloalkyl, haloalkoxy, -C(0)OR₅I , -C(0)NR_5iR5i·, - OCH2CH2OR51, -NR5iS(0)₂NR₅rR5r and -C(CH₃)20R₅I ; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

wherein R51 , R51 and R₅r are independently selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R₅ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; wherein the alkyl, alkenyl or alkynyl defined in R₅ , if substituted, is substituted with one or more substituent/s selected from -OR₅₂, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; wherein R₅₂ and R₅₂ are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2-6 alkynyl;

the alkyl, alkenyl or alkynyl, 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 =0, -OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13 ; wherein R₁₃ and R₁₃ are independently selected from hydrogen, unsubstituted Ci-₆ alkyl, unsubstituted C_2-6 alkenyl, and unsubstituted C₂-e 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 =0, halogen, -R14, -OR14, -NO2, -NR14R14 , - NRi₄C(0)Ri4 , -NR₁₄S(0)₂Ri4·, -S(0)₂NRi₄Ri4·, - NRi₄C(0)NRi₄ Ri4 , -SR14 , -S(0)Ri₄, - S(0)2Ri4, -CN, haloalkyl, haloalkoxy, -C(0)0Ri4, -C(0)NRi4Ri4 , -OCH2CH2OR14, - NRi₄S(0)₂NRi4 R14 and -C(CH₃)20RI₄; wherein Ru, R₁₄ and RM- are independently selected from hydrogen, unsubstituted Ci-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 (l^a)

wherein Ri, R₂, R₃, R₃ , R₄, R₄ , Re, Re , X, Ui , 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 (l^a)

wherein

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]pC(0)N(R_z)[CH₂]_q-, - [CH₂]pN(R_z)C(0)[CH₂]q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C_2-e alkynyl;

Rp is selected from hydrogen, halogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C₂.e alkenyl and substituted or unsubstituted C_2-e alkynyl; alternatively, R_a and R_t>, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted Ci-e 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(0)-Ci-₆ alkyl; p is O, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;

Yi is— C(RioRio )-; wherein R10 and Rio 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 R10 may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is— C(Rio io· )-; 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, Rio · and R10 · may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; n is 0 or 1 ;

R1 is selected from -NR₅R₅ and -NR₅ C(0)R₅;

R3 is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂-6 alkenyl, 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.e alkenyl and substituted or unsubstituted C2.6 alkynyl;

R₄ and R₄ are independently selected from halogen, -R41, -OR41, -NO2, -NR₄₁R₄₁ , - NR_4iC(0)R₄r, -NR_4iS(0)₂R4i , -S(0)₂NR_4iR4i , -NR₄I C(0)NR₄I R₄r , -SR41 , -S(0)R_4i, - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR₄IR₄I , -OCH₂CH₂OR I , - NR_4iS(0)₂NR_4i'R₄r and -C(CH₃)₂OR₄I ; wherein R₄I , R₄r and R _r are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Rs is selected from 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, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl;

Rs· is 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 and R₆ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21', -NR₂IC(0)R₂I , -NR21 S(0)₂R2i ', -S(0)2NR2iR2r, - NR2iC(0)NR2i'R2i”, -SR21 , -S(0)R_2I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR₂I R₂I , - OCH2CH2OR21 , -NR2iS(0)2NR2i'R2i" and -C(CH3)20R2i; wherein R₂₁, R₂₁ and R₂₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

wherein

X is selected from a bond, -[C(R_aRb)]_P-, -[CH₂]_PC(0)[CH2]q-, -[CH2]_PC(0)N(R_z)[CH2]q-, - [CH₂]_pN(Rz)C(0)[CH₂]q- and -[CH₂]_PN(R_z)[CH₂]_q-;

R_a 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, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted Ci_-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(0)-Ci-e alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;

Yi is— C(RioRio )-; 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 Rio· may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is— C(Rio Rio )-; wherein R₁₀ and Rnr are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, Rio- and Rio - may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

n is 0 or 1 ;

R1 is selected from -NR5R5 and -NR₅ C(0)R5;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, is substituted with one or more substituent/s selected from halogen, -R₂₁, -OR21, -NO2, -NR21R21 , -NR2iC(0)R_2i , -NR₂₁S(0)₂R21·, -S(0)2NR2iR2i’, - NR_2iC(0)NR₂rR2r, -SR21 , -S(0)R₂I , -S(0)₂R_2i , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, - C(0)NR₂₁R₂₁ , -OCH2CH2OR21, -NR2iS(0)₂NR₂rR2i and -C(CH₃)20R₂I ; wherein R₂₁ , R₂₁ and R_21" are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₃ 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 and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, is substituted with one or more substituent/s selected from -OR₃₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR31R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R31 , -OR31 , -NO2, -NR31R31 , - NR₃IC(0)R₃I·, -NR₃IS(0)₂R₃I , -S(0)₂NR_3iR3i , - NR₃IC(0)NR₃I R₃r, -SR31 , -S(0)R_3i, -S(0)₂R3i, -CN, haloalkyl, haloalkoxy, -C(0)0R3i , -

C(0)NR₃₁R₃₁ , -OCH2CH2OR31, -NR₃₁S(0)₂NR₃₁ R31 and -C(CH₃)20R₃I ;

wherein R₃₁ , R₃₁ and R₃r are independently selected from hydrogen, substituted or unsubstituted Ci-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 C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; the alkyl, alkenyl or alkynyl defined in R₃ , if substituted, 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, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2.e alkenyl and substituted or unsubstituted C₂.6 alkynyl;

R₄ and R₄ are independently selected from halogen, -R_4I , -OR_4I , -NO2, -NR_4IR_4I , - NR_4IC(0)R_4I , -NR_4IS(0)₂R_4I , -S(0)₂NR₄₁R₄r, -NR_4IC(0)NR_4I R_4I , -SR_4I , -S(0)R_4i, - S(0)₂R _I , -CN, haloalkyl, haloalkoxy, -C(0)0R _i, -C(0)NR_4iR_4r, -OCH₂CH₂OR_4I , - NR_4IS(0)₂NR_4I R_4r and -C(CH₃)₂OR_4I ; wherein R_4I , R₄r and R₄r are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2.6 alkynyl;

R₅ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂-6 alkenyl, and substituted or unsubstituted C_2.e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR₅₁, halogen, -CN, haloalkyl, haloalkoxy and -NR₅₁R₅₁ ; wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s selected from halogen, -R₅₁, -OR₅₁, -N0₂, -NR₅₁R51 , - NR₅₁C(0)R₅₁ , -NR₅₁S(0)₂R₅₁ , -S(0)₂NR₅₁ R51 ·, - NR_5IC(0)NR_5I Rsr , -SR₅₁ , - S(0)Rsi, -S(0)₂RSI , -CN, haloalkyl, haloalkoxy, -C(0)0Rsi, -C(0)NR_6iR5i , - OCH2CH2OR51 , -NR_5IS(0)₂NR_5I Rsr and -C(CH₃)20R_5I; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

wherein R51, Rsr and Rsr 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;

Rs· 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 Rs , if substituted, is substituted with one or more substituent/s selected from -OR₅₂, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; wherein R₅₂ and R_52' are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

Re and Re are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21', -NR_2IC(0)R_2I , -NR2iS(0)2R2i’, -S(0)2NR2I R21 - NR2iC(0)NR_2i R₂r , -SR21 , -S(0)R_2i, -S(0)₂R_2i, -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2I R_2I , - OCH2CH2OR21, -NR21 S(0)₂NR2i 'R21” and -C(CH3)20R2i; wherein R₂₁, R₂₁ and R₂₁ are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

the alkyl, alkenyl or alkynyl, 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 =0, -OR13, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13 ; wherein R₁₃ and R₁₃ 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 =0, halogen, -R14, -ORu, -NO2, -NR14R14 , - NRi₄C(0)Ri4 , -NRi₄S(0)₂Ri4 , -S(0)₂NRi₄Ri4 , - NRI₄C(0)NRI₄ RH , -SR , -S(0)Ri₄, - S(0)₂Ri4, -CN, haloalkyl, haloalkoxy, -C(0)0Ri₄, -C(0)NRi₄Ri4 , -OCH₂CH₂ORI₄, - NRi₄S(0)₂NRi4 Ri4" and -C(CH₃)₂ORi4; wherein R , R₁₄ and Ru are independently selected from hydrogen, unsubstituted Ci_-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 (l^a’)

(P wherein Ri , R₂, R3, R3 , R₄, R₄ , Re, Re , 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.

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

(P wherein

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - (CH₂]_pN(R_z)C(0)[CH₂]_q- and -[CH₂]_pN(R₂)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2-e alkynyl;

R_b is selected from hydrogen, halogen, substituted or unsubstituted Ci.e 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, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂-e alkenyl, substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-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 ; Ri is selected from -NR5R5 and -NRs C(0)R5;

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

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 R₄ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R₄₁ , - NR_4iC(0)R4i , -NR4iS(0)₂R4v, -S(0)₂NR4iR4i·, -NR₄IC(0)NR₄I R41 ", -SR41 , -S(0)R₄I , - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR₄I R₄I , -OCH2CH2OR41 , - NR₄I S(0)₂NR₄I R41" and -C(CH₃)₂OR4i; wherein R₄₁ , R₄₁ and R₄₁ are independently selected from hydrogen, substituted or unsubstituted Ci.e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Rs is selected from 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, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl;

Rs 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;

R₆ and R₆ are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR21R21', -NR2iC(0)R₂r, -NR2iS(0)2R2i , -S(0)2NR2IR21", - NR_2iC(0)NR2i R₂r , -SR21 , -S(0)R₂I , -S(0)₂R₂I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR₂I R₂I , - OCH2CH2OR21 , -NR2iS(0)2NR2i’R2i'' and -C(CH3)20R2i; wherein R₂I , R₂r and R₂r are independently selected from hydrogen, substituted or unsubstituted Ci-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.

wherein X is selected from a bond, -[C(R_aRb)]_P-, -[CH₂]pC(0)[CH2]q-, -[CH₂]pC(0)N(Rz)[CH2]q-, - [CH₂]_pN(R_z)C(0)[CH₂]q- and -[CH₂]pN(R_z)[CH₂]q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C₂-e alkynyl; R_b 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, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted C1 -6 alkyl, substituted or unsubstituted C₂-e alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-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 selected from -NR5R5 and -NR₅ C(0)R5;

R2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R_å, if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, -NR21R21 ,

wherein R21, R21 and R₂r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; R₃ is selected from substituted or unsubstituted Ci.e alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2.6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R3, if substituted, is substituted with one or more substituent/s selected from -OR₃₁, halogen, -CN, haloalkyl, haloalkoxy and -NR₃₁R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R31, -OR₃₁ , -NO2, -NR31R31 , - NR₃IC(0)R₃I , -NR_3iS(0)₂R3i , -S(0)₂NR_3iR3i , - NR₃IC(0)NR₃I R₃r , -SR31 , -S(0)R_3i, -S(0)₂R3i , -CN, haloalkyl, haloalkoxy, -C(0)0R_3i , -

C(0)NR₃₁R₃₁ , -0CH₂CH₂0R₃₁, -NR₃IS(0)₂NR₃I R31 and -C(CH₃)₂OR3i ; wherein R31, R31 and R31 are independently selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C₂-e alkynyl;

R3 is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C₂.e alkynyl; the alkyl, alkenyl or alkynyl defined in R3 , if substituted, 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, substituted or unsubstituted Ci.₆ alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2.e alkynyl;

R₄ and R₄ are independently selected from halogen, -R₄₁, -OR41, -NO₂, -NR41R41 , - NR₄I C(0)R₄I , -NR_4iS(0)₂R_{4i '}, -S(0)₂NR₄I R41 , -NR₄IC(0)NR₄I R₄r , -SR41 , -S(0)R₄₁ , - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR₄I R₄I , -OCH₂CH₂OR₄I , - NR₄IS(0)₂NR₄I R41 and -C(CH₃)₂OR4i; wherein R₄₁ , R₄₁ and R₄r are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Rs is selected from 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, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR₅₁, halogen, -CN, haloalkyl, haloalkoxy and -NR51R51'; wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s selected from halogen, -R₅₁ , -OR51, -NO2, -NR51R51 , - NR_5iC(0)R₅r, -NR_5iS(0)₂R5i , -S(0)₂NR_5iR5r, - NR₅IC(0)NR₅I Rsr, -SR51 , - S(0)Rsi, -S(0)₂R_5i, -CN, haloalkyl, haloalkoxy, -C(0)OR5i , -C(0)NRsiRsi , - OCH2CH2OR51 , -NR51S(0)₂NR₅₁ Rsr and -C(CH₃)20R₅I ; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

wherein R₅I , Rsr and R₅₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₅ is 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 alkyl, alkenyl or alkynyl defined in Rs , if substituted, is substituted with one or more substituent/s selected from -OR₅₂, halogen, -CN, haloalkyl, haloalkoxy and -NR₅₂R52 ; wherein R₅₂ and R_52' are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Re and R_6’ are independently selected from hydrogen, halogen, -R21, -OR21, -N0₂, - NR21R21 , -NR_2iC(0)R2i , -NR2iS(0)2R2i·, -S(0)₂NR2iR₂r, - NR2iC(0)NR_2i R2r, -SR21 , -S(0)R_2i, -S(0)₂R_2i, -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2I R_2I , - OCH2CH2OR21 , -NR_2IS(0)₂NR_2I R21" and -C(CH₃)20R_2I ; wherein R₂₁, R₂₁ and R₂₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; the alkyl, alkenyl or alkynyl, 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 =0, -OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13 ; wherein R₁₃ and R₁₃ are independently selected from hydrogen, unsubstituted Ci-₆ alkyl, unsubstituted C_2-6 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 =0, halogen, -RI₄, -OR14, -NO2, -NR14R14 , - NRi₄C(0)Ri4 , -NR₁₄S(0)₂Ri4·, -S(0)₂NRi₄Ri4 , - NRi₄C(0)NRi₄ Ri4 , -SR14 , -S(0)Ri4, - S(0)₂Ri₄, -CN, haloalkyl, haloalkoxy, -C(0)0Ri₄, -C(0)NRi₄Ri4 , -OCH2CH2OR14, - NRi₄S(0)₂NRi4 RI4·· and -C(CH₃)₂ORi4; wherein Ru, R and Ru are independently selected from hydrogen, unsubstituted Ci.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 (l^b)

wherein Ri, R₂, R₃, R₃ , R₄, R₄ , Re, Re , X, Ui, 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 (l^b)

wherein

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]_q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]pN(R_z)C(0)[CH₂]q- and -[CH₂]_pN(R_z)[CH₂]q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci-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 Ci-₆ alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C₂-e alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C_2-e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-6 alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;

Yi is— C(RioRio )-; wherein R₁₀ and Ri₀ are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, R₁₀ and R₁₀ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is— C(Rio' Rio )-; wherein R₁₀ and Rio- are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, Rio- and R₁₀ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; n is 0 or 1 ;

R₁ is selected from -NR5R5 and -NRs C(0)R5;

R₃ 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 and substituted or unsubstituted alkylcycloalkyl; R₃ is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

R₄ and R₄ are independently selected from halogen, -R₄I , -OR₄I , -NO2, -NR₄IR₄I , - NR_4IC(0)R₄I , -NR_4iS(0)₂R₄r, -S(0)₂NR I R I , -NR_4iC(0)NR_4rR _i ·, -SR₄I , -S(0)R _i, - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR_4iR_4r, -OCH₂CH₂OR I , - NR₄IS(0)₂NR I R I and -C(CH₃)₂OR₄I ; wherein R₄I , R₄r and R r are independently selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C_2-e alkynyl;

R₅ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C₂.e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl;

R₅ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C₂-e alkynyl;

Re and R₆ are independently selected from hydrogen, halogen, -R_2I , -OR_2i, -N0₂, - NR_2I R_2I , -NR_2IC(0)R_2I , -NR_2iS(0)₂R₂r, -S(0)₂NR_2iR₂v, - NR₂-iC(0)NR_2i R_{2i "}, -SR_2I , -S(0)R_2I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2I R_2V, - 0CH₂CH₂0R₂₁ , -NR_2IS(0)₂NR_2I R₂1 and -C(CH₃)₂OR_2I ; wherein R_2I , R₂r and R₂r are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2.e 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 (l^b)

wherein X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl; R_b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C_å alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl; R_z is selected from hydrogen, substituted or unsubstituted 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(0)-Ci_-6 alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;

Y 1 is— C(RioRio )-; 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 Ri o· may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is— C(Rio"Rio'”)-; wherein R10 and Rio - are independently selected from hydrogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl; alternatively, Ri o- and R10 may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; n is 0 or 1 ;

R1 is selected from -NR5R5 and -NRs C(0)R5;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R2, if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, -NR21R21 , -NR₂₁C(0)R₂₁ , -NR2iS(0)₂R₂r, -S(0)₂NR_2IR_2I , - NR_2IC(0)NR_2I R21 , -SR21 , -S(0)R_2I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R2i, - C(0)NR₂₁R₂₁ , -OCH2CH2OR21 , -NR_2IS(0)₂NR_2I R21" and -C(CH₃)₂OR2i; wherein R21, R21 and R₂r are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R3 is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2.6 alkenyl, substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, is substituted with one or more substituent/s selected from -OR₃₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR31 R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R31 , -OR31 , -NO2, -NR31 R31 , - NR_3IC(0)R_3I , -NR_3iS(0)₂R3i , -S(0)₂NR_3IR_3I , - NR_3IC(0)NR_3I Rs , -SR31 , -S(0)R_3I , -S(0)₂R_3I , -CN, haloalkyl, haloalkoxy, -C(0)0R_3i , - C(0)NR₃₁ R₃₁ , -OCH2CH2OR31 , -NR₃₁ S(0)₂NR₃₁ R31 · and -C(CH₃)₂OR3i ; wherein R₃₁ , R₃₁· and R₃r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R3' is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; the alkyl, alkenyl or alkynyl defined in R3 , if substituted, 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, substituted or unsubstituted C1-6 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(0)R₄₁ , -NR₄₁S(0)₂R41 , -S(0)₂NR₄₁R41 , -NR_4IC(0)NR_4I R₄r, -SR41 , -S(0)R₄₁, - S(0)₂R_4I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR_4iR4i , -OCH₂CH₂OR_4I , - NR_4IS(0)₂NR_4I R41 and -C(CH3)20R4i; wherein R41 , R41 and R41 are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Rs is selected from substituted or unsubstituted Ci.₆ alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR₅₁, halogen, -CN, haloalkyl, haloalkoxy and -NR51R51 ; wherein the cycloalkyl, aryl or heterocyclyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R5, if substituted, is substituted with one or more substituent/s selected from halogen, -R51, -OR51, -NO2, -NR51R51 , - NRSI C(0)R_5I·, -NR_5IS(0)₂R_5I·, -S(0)₂NR_5iR5i , - NR5iC(0)NR₅vR₅r, -SR51 , - S(0)Rsi, -S(0)₂R_5I , -CN, haloalkyl, haloalkoxy, -C(0)0R_5i, -C(0)NR_5I R_5I , - OCH2CH2OR51, -NR_5iS(0)₂NR_{5i '}R5i" and -C(CH₃)₂OR5i; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

wherein R₅₁, R₅₁ and Rsr are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Rs is selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂.e alkynyl; wherein the alkyl, alkenyl or alkynyl defined in R₅ , if substituted, is substituted with one or more substituent/s selected from -OR₅₂, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; wherein R₅₂ and R₅₂· 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;

Re and Re are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21’, -NR₂IC(0)R₂I , -NR2iS(0)2R2i’, -S(0)2NR2I R21', - NR2iC(0)NR_2i-R2r , -SR21 , -S(0)R₂I , -S(0)₂R₂I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2iR2i , - OCH2CH2OR21, -NR_2iS(0)₂NR_2i R21 and -C(CH₃)₂OR2i; wherein R₂₁, R₂₁ and R₂₁ are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl; the alkyl, alkenyl or alkynyl, 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 =0, -OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13 ; wherein R13 and R13 are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C₂-e 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 =0, halogen, -R-u, -OR14, -NO2, -NR14R14 , - NRi₄C(0)Ri4 , -NRi₄S(0)₂Ri4 , -S(0)₂NRi₄Ri4 , - NR₁₄C(0)NRi₄ Ri4 , -SRu , -S(0)Ri₄, - S(0)₂Ri4, -CN, haloalkyl, haloalkoxy, -C(0)0Ri₄, -C(0)NRi₄Ri4·, -OCH₂CH₂ORI₄, - NRi₄S(0)₂NRi₄ Ri4 and -C(CH₃)₂ORI₄;

wherein R , R14 and R are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C_2.6 alkenyl, unsubstituted C_2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

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

(l^b ), wherein Ri, R₂, R₃, R₃ , R₄, R₄ , Re, Re , 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.

(l^b ). wherein

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]_q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

R_b is selected from hydrogen, halogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C₂-e 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, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2.6 alkenyl, substituted or unsubstituted C₂.e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-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 ;

Ri is selected from -NR5R5 and -NR₅ C(0)R5;

R3 is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C₂.e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; R₃ is selected from hydrogen, substituted or unsubstituted Ci-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(0)R₄₁ , -NR₄₁S(0)₂R41 , -S(0)₂NR₄₁ R41·, -NR_4IC(0)NR_4I R₄r , -SR41 , -S(0)R₄₁ , - S(0)₂R_4I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR_4I R_4I , -OCH2CH2OR41 , - NR_4IS(0)₂NR_4I R41 and -C(CH₃)20R_4I ; wherein R₄₁ , R₄₁ and R₄₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

R₅ is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl;

Rs' is selected from hydrogen, substituted or unsubstituted Ci_-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl;

Re and R₆ are independently selected from hydrogen, halogen, -R₂₁ , -OR₂₁ , -NO2, - NR21R2I’, -NR₂IC(0)R₂₁ , -NR21 S(0)2R21 ', -S(0)2NR2lR21', - NR2lC(0)NR₂rR21 ", -SR21 , -S(0)R₂I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2i R2r, - OCH2CH2OR21 , -NR2iS(0)2NR2rR2i’’ and -C(CH3)20R2i; 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; 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 (l^b’)

(l^b ). wherein

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]pN(R_z)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2.6 alkynyl;

R_b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂-e 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, may form a substituted or unsubstituted cycloalkyl;

R_z is selected from hydrogen, substituted or unsubstituted Ci.e alkyl, substituted or unsubstituted C_2.e alkenyl, substituted or unsubstituted C_2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-e 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 selected from -NR5R5 and -NR₅ C(0)R5;

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21 , -NO2, -NR21R21 , -NR_2iC(0)R₂r, -NR2iS(0)2R2v, -S(0)2NR2iR2r, - NR2iC(0)NR2rR2i", -SR21 , -S(0)R_2i , -S(0)₂R_2i, -CN, haloalkyl, haloalkoxy, -C(0)0R2i , - C(0)NR₂₁R₂₁ , -OCH2CH2OR21 , -NR₂₁S(0)₂NR21 R21" and -C(CH₃)₂OR2i; wherein R21, R21 and R21 are independently selected from hydrogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

R3 is selected from substituted or unsubstituted C1 -6 alkyl, substituted or unsubstituted C2-6 alkenyl, 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, is substituted with one or more substituent/s selected from -OR₃₁ , halogen, -CN, haloalkyl, haloalkoxy and -NR31 R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R₃₁, -OR₃₁ , -N0₂, -NR31R31 , - NR₃₁C(0)R₃₁ , -NR₃₁S(0)₂R₃₁ , -S(0)₂NR₃IR₃I , - NR₃IC(0)NR₃I Rsr , -SR31 , -S(0)R_3i, -S(0)₂R₃I , -CN, haloalkyl, haloalkoxy, -C(0)0R_3i , - C(0)NR₃IR₃I , -OCH₂CH₂OR₃I , -NR₃I S(0)₂NR₃I R31 and -C(CH₃)₂OR3i ;

wherein R₃₁ , R₃₁ and R₃₁ are independently selected from hydrogen, substituted or unsubstituted Ci-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 Ci_-6 alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C_2.6 alkynyl; the alkyl, alkenyl or alkynyl defined in R3 , if substituted, 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, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2.e alkynyl;

R₄ and R_4' are independently selected from halogen, -R I , -OR₄I , -N0₂, -NR IR₄I , - NR₄IS(0)₂R₄I , -S(0)₂NR_4iR_4r, -NR₄IC(0)NR₄I R_4r , -SR₄I , -S(0)R_4i, - haloalkyl, haloalkoxy, -C(0)0R_4i , -C(0)NR_4iR_4r, -OCH₂CH₂OR₄I , -

R₄I and -C(CH₃)₂OR ₁; wherein R₄I , R_4r and R _r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂.e alkenyl and substituted or unsubstituted C₂-e alkynyl; Rs is selected from substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR51 , halogen, -CN, haloalkyl, haloalkoxy and -NR51 R51 ; wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s selected from halogen, -R51, -OR51, -N0₂, -NR51R51 , - NR_5iC(0)R₅r, -NR_5IS(0)₂R_5I , -S(0)₂NR_5iR5r, - NR_5iC(0)NR_{5i '}R5r, -SR_5I , - S(0)R_5I , -S(0)₂R_5I , -CN, haloalkyl, haloalkoxy, -C(0)0R_5i, -C(0)NR_5I R_5I , - OCH2CH2OR51, -NR₅₁S(0)₂NR₅₁ Rsr and -C(CH₃)20R_5I; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

wherein R₅₁, R₅₁ and R₅₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C_2.6 alkynyl;

Rs is 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 alkyl, alkenyl or alkynyl defined in R₅ , if substituted, is substituted with one or more substituent/s selected from -OR52, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; wherein R52 and R52 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;

R₆ and R₆ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R2I·, -NR2lC(0)R₂₁ , -NR2lS(0)2R2V, -S(0)2NR2lR21', - NR₂IC(0)NR₂I R21", -SR21 , -S(0)R₂I , -S(0)₂R₂₁, -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR₂I R_2I , - OCH2CH2OR21, -NR2iS(0)2NR2i R2i" and -C(CH3)20R2i; 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;

the alkyl, alkenyl or alkynyl, 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 =0, -OR13, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13 ; wherein R13 and R13 are independently selected from hydrogen, unsubstituted Ci.e 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 =0, halogen, -R14, -OR14, -NO2, -NR14R14 , - NRi₄C(0)Ri4 , -NRi₄S(0)₂Ri4', -S(0)₂NRi4Ri4 , - NRI₄C(0)NRI₄ Rir, -SR , -S(0)Ri₄, - S(0)₂Ri4, -CN, haloalkyl, haloalkoxy, -C(0)0Ri₄, -C(0)NRi₄Ri4 , -OCH2CH2OR14, - NRi4S(0)₂NR_14'Ri4 ' and -C(CH₃)₂ORi4; wherein Ru, RI₄ and RI₄- are independently selected from hydrogen, unsubstituted Ci-₆ alkyl, unsubstituted C₂-e 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.

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 Formulae (G), (l^a), (l^a ), (l^b) and (l^b ), (where applicable), and to all intermediate of synthesis, when those groups are present in the mentioned general Markush formulae, since compounds of general Formulae (G), (l^a), (l^a ), (l^b) and (l^b ), are included within the scope of the larger definition of general 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), (G), (l^a), (l^a ), (l^b) and (l^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’), (l^a), (l^a ), (l^b) and (l^b ), and to all intermediates of synthesis.

For clarity purposes, the expression“the cycloalkyl in Rio-Rio“ means the cycloalkyl resulting when R₁₀ and R₁₀ form, together with the carbon to which they are attached, a cycloalkyl. This cycloalkyl can then be substituted or not. This definition is also generally applicable and can be also applied as a definition of any other cycle (like heterocyclyl, aryl or cycloalkyl) formed from two different functional groups like e.g.“the cycle in Rj-Rj*“ means the cycle resulting when R, and R, form a cycle together with the atom(s) to which they are attached. This cycle can then be substituted or not.

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, Ci-2-alkyl represents C1- or C2-alkyl, Ci-3-alkyl represents C1-, C2- or C3-alkyl, Ci-4-alkyl represents C1-, C2-, C3- or C4-alkyl, Ci.₅-alkyl represents C1-, C2-, C3-, C4-, or C5-alkyl, Ci-₆-alkyl represents C1-, C2-, C3-, C4-, C5- or C6-alkyl, Ci.₇-alkyl represents C1-, C2-, C3-, C4- , C5-, C6- or C7-alkyl, Ci-s-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7- or C8- alkyl, Ci-io-alkyl represents C1 -, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9- or C10-alkyl and Ci-18-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9-, C10-, C1 1 -, 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 Ci_-8alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, or octyl; preferably is Ci-ealkyl like methyl, ethyl, propyl, butyl, pentyl, or hexyl; more preferably is C^alkyl 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 C₂-io-alkenyl or C_2-8-alkenyl like ethylene, propylene, butylene, pentylene, hexylene, heptylene or octylene; or is C2-6- alkenyl like ethylene, propylene, butylene, pentylene, or hexylene; or is C₂-4-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 C2-10- alkynyl or C2-e-alkynyl like ethyne, propyne, butyene, pentyne, hexyne, heptyne, or octyne; or is C2-e-alkynyl like ethyne, propyne, butyene, pentyne, or hexyne; or is C2-4- 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), -NRKRK , -SRK, -S(0)RK, -S(0)2RK, -ORR, - C(0)R_k, -C(0)OR_k, -CN, -C(0)NR_kR_{k ,} haloalkyl, haloalkoxy, being R_k represented by Ri_3, R_{31 ,} R_32, R51 or R52 (being R_k represented by R13 , R31 , R32 , R51 or R₅₂·; being R_k represented by R₁₃ ·_, R_{31 ,} R_{32 ,} R₅₁ or R5_{2 ;} wherein R1 to R52 and R_z are as defined in the description, and wherein when different radicals R1 to R5₂ and R₂ 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), -NR_kR_k , -OR_k, -CN, -SR_k, haloalkyl, haloalkoxy, being R_k represented by R13, R31, R_32, R₅₁ or R₅₂, (being R_k represented by RI₃ R_{31 ,} R_{32 ,} R₅₁ or R52 ; being R_k - represented by Ri_3", R_{31 ",} R₃₂ \ Rsr or R₅₂ ); wherein R₁ to R₅₂ and R_z are as defined in the description, and wherein when different radicals R₁ to R₅₂ · and R_z 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. -CH₂CI, -CH₂F, -CHC , -CHF₂, -CCI₃, -CF₃ and -CH2-CHCI2. Preferably haloalkyl is understood in the context of this invention as halogen- substituted Ci-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 -CH₂CI, -CH₂F, -CHCb, -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. -OCH₂CI, -OCH2F, -OCHC , -OCHF₂, -OCCI3, -OCF₃ and - OCH2-CHCI2. Preferably haloalkyl is understood in the context of this invention as halogen-substituted -OC^-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 -OCH2CI, -OCH2F, -OCHCI2, - 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, C_3-4- 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, Cs-e-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-scycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; or is C₃-7cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; or is Cs-ecycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, especially cyclopentyl or cyclohexyl.

Aryl is understood as meaning 5 to 18 (preferably 6 to 14) 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, dihydroindene 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 - especially - 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.

A 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.

Examples include non-aromatic heterocyclyls such as tetrahydropyrane, oxazepane, morpholine, piperidine, pyrrolidine as well as heteroaryls such as furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, thiazole, benzothiazole, indole, benzotriazole, carbazole and quinazoline.

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

- the heteroaryl (being equivalent to heteroaromatic radicals or aromatic heterocyclyls, or also to “heterocyclyl containing at least one aromatic ring containing at least one heteroatom") 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.

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.

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 Ci-e-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. -Chh-phenyl).

In the context of this invention alkylheterocyclyl is understood as meaning an heterocyclyl group being connected to another atom through a Ci.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 Ci-e-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, -N0₂ , -NR_kR_k , -C(0)0R_k, NR_kC(0)R_k , -C(0)NR_kR_k· , - NR_kS(0)₂Rk , =0, -OCH₂CH₂OH, -NR_kC(0)NR_k Rk , -S(0)₂NR_kR_k , -NR_kS(0)₂NR_k Rk , haloalkyl, haloalkoxy, -SR_k, -S(0)R_k, -S(0)₂R_k or C(CH₃)ORk, or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, with R_k, R_k and R_k independently being either H or a saturated or unsaturated, linear or branched, substituted or unsubstituted Ci-e-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted Ci-e-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted -O-Ci-₆-alkyl (alkoxy); a saturated or unsaturated, linear or branched, substituted or unsubstituted - S-Ci-e-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted -C(0)-Ci-₆ alkyl-group; a saturated or unsaturated, linear or branched, substituted or unsubstituted -C(0)-0-Ci-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 Rn, RI₄. R21. R31 or Rsi, (being R_k one of Rn·_, R_{14 ,} R₂r_, R_{31 '} or R_{51 ,} being Rk- one of Rn , R_{14 ,} R₂r, R31" or R51„ wherein R₁ to R₅₂ and R_z are as defined in the description, and wherein when different radicals R₁ to R₅₂ 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(0)R_k , - NR_kS(0)₂Rk , -S(0)₂NR_kRk , -NR_kC(0)NR_k Rk_\ haloalkyl, haloalkoxy, -SR_k , -S(0)R_k or S(0)₂R_k, or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, being R_k one of Rn_, RI_4, R₂I _, R₃₁ or R₅₁, (being R_k one of Rn _, R₁₄ R₂I R_{31 '} or R_{51 ;} being Rk one of Rn-, R14 , R2r, R31" or R_{51 ";} wherein R₁ to R₅₂ and R_z are as defined in the description, and wherein when different radicals R₁ to Rs₂ 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 =0.

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 CI-, 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 Ή” 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(R_aR_b)]_P-, -[CH₂]pC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(Rz)C(0)[CH₂]q- and -[CH₂]_pN(R_z)[CH₂]_q-;

R_a is selected from hydrogen, halogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C_2.e alkynyl;

R_b is selected from hydrogen, halogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C₂.e 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, may 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.

X is selected from a bond, -[C(R_aR_b)]_P-, -[CH₂]_PC(0)[CH₂]q-, -[CH2]_PC(0)N(Rz)[CH₂]q-, - [CH₂]_PN(Rz)C(0)[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.

-X-R₁ is selected from -R1 , -[C(R_aRb)]_P-Ri, -[CH2] C(0)[CH2]_q-Ri, [CH₂]_PC(0)N(Rz)[CH₂]q-Ri, -[CH₂]_PN(R_z)C(0)[CH2]q-Ri and -[CH₂]_PN(R_z)[CH2]_q-Ri; 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.

R_a is selected from hydrogen, halogen, substituted or unsubstituted C1-6 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

Rp is selected from hydrogen, halogen, substituted or unsubstituted Ci-e 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 alternatively, R_a and Rt_>, taken together with the carbon atom to which they are attached, may 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.

X is selected from a bond,

[CH₂]pN(Rz)C(0)[CH₂]q- and -

R_z is selected from hydrogen, substituted or unsubstituted C1 -6 alkyl, substituted or unsubstituted C₂-e alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-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.

R_z 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 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.

Yi is— C(Rio io )-; wherein Rio and Rio are independently selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, R₁₀ and R₁₀ may 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.

Yi is— C(RioRio )-; 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.

Rio and Rio are independently selected from hydrogen, substituted or unsubstituted Ci- b alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R₁₀ and R₁₀ may 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

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.

Y2 is— C(Rio"Rio' )-; wherein R₁₀ and Rio - are independently selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R₁₀ and Rio- may 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.

Y₂ is— C(Rio”Rio )-; 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.

R₁₀ and Rio · are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂-6 alkenyl and substituted or unsubstituted C_2. e alkynyl; alternatively, R₁₀ - and R₁₀ · may 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.

Rio and Rio are independently selected from hydrogen, substituted or unsubstituted Ci-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂. e 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 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.

Ri is selected from -NR₅R₅ and -NRs CfOJRs; 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.

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.

R₃ 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 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.

R₃ is selected from substituted or unsubstituted Ci-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 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.

R_3' 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.

R₄ and R_4' are independently selected from halogen, -R_4I , -OR_4I , -N0₂, -NR_4iR₄r, - NR_4IC(0)R_4I , -NR_4IS(0)₂R_4I , -S(0)₂NR_4IR_4I , -NR _iC(0)NR_4VR₄r, -SR _I , -S(0)R_4i, - S(0)₂R_4I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR_4IR_4I , -0CH₂CH20R_4I , - NR_4iS(0)₂NR_4i'R r and -C(CH₃)₂OR_4I ; 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

Rs is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; 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.

Rs is selected from substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; 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 is selected from substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; 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.

Re and R₆ are independently selected from hydrogen, halogen, -R21 , -OR21 , -NO2, - NR21R21', -NR₂₁C(0)R₂₁ , -NR2iS(0)2R2i\ -S(0)2NR2iR2i\ - NR₂IC(0)NR₂VR21", -SR21 , -S(0)R₂I , -S(0)₂R₂I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR₂I R₂I , - OCH2CH2OR21 , -NR₂IS(0)₂NR₂I R21 and -C(CH₃)₂OR2i; 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.

R₁₀ and R₁₀ are independently selected from hydrogen, substituted or unsubstituted Ci- 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

R₁₀ and R₁₀ 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.

R₁₀ and R₁₀ may 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.

Rio and Rio- 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.

Rio- and R₁₀ 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.

R₂₁, R₂₁ and R_{21 "} are independently selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C₂.e 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.

R₂₁, R₂₁ and R₂₁ 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.

R₃₁ , R₃₁ and R₃₁ 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.

R₃₁, R₃₁ and R₃₁ 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.

R32 and R32 are independently selected from hydrogen, substituted or unsubstituted Ci. e 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.

R₃₂ and R₃₂ 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 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.

R₄I , R₄₁ and R₄₁ 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.

R₅₁, R₅₁ and R₅₁ 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

R₅₁, R₅₁ and R₅₁ 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.

R₅₂ and R_52' are independently selected from hydrogen, substituted or unsubstituted Ci. 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.

R₅₂ and R₅₂ 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

R₁₃ and R₁₃ are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C_2-6 alkenyl, and 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.

R₁₃ and R₁₃ are independently selected from hydrogen and unsubstituted Ci-e 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.

R_H, R and R are independently selected from hydrogen, unsubstituted Ci-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.

Ri₄, R and Ru 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.

R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R₂, if substituted, is substituted with one or more substituent/s selected from halogen, -R_2I , -OR_2I , -N0₂, -NR_2I R_2I , -NR_2iC(0)R₂r, -NR_2IS(0)₂R_2I , -S(0)₂NR_2iR₂r, - NR_2iC(0)NR₂rR_{2i "}, -SR_2I , -S(0)R_2I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, - C(0)NR_2I R_2I , -OCH₂CH₂OR_2I , -NR_2I S(0)₂NR_2I R_2r and -C(CH₃)₂OR_2I ; wherein R_2I , R₂r and R₂r are independently selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C_2-e 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.

R₃ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C₂-e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein, the alkyl, alkenyl or alkynyl defined in R₃, if substituted, is substituted with one or more substituent/s selected from -OR₃₁, halogen, -CN, haloalkyl, haloalkoxy and -NR31R31 ; wherein the cycloalkyl in R₃, if substituted, is substituted with one or more substituent/s selected from halogen, -R31, -OR31, -NO2, -NR31R31 , - NR₃₁C(0)R₃₁ , -NR₃₁S(0)₂R31 , -S(0)₂NR₃₁R₃₁ , - NR_3IC(0)NR_3I Rsr , -SR31 , -S(0)R_3i, -S(0)₂R₃₁, -CN, haloalkyl, haloalkoxy, -C(0)0R3i, - C(0)NR_3I R_3I , -OCH2CH2OR31, -NR_3I S(0)₂NR_3I R31 and -C(CH₃)₂OR_3I ;

wherein R₃₁, R₃₁ and R₃₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 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 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; the alkyl, alkenyl or alkynyl defined in R_3', if substituted, 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, substituted or unsubstituted Ci.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.

R₅ is selected from 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, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl, alkenyl or alkynyl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR₅₁, halogen, -CN, haloalkyl, haloalkoxy and -NR₅₁R₅₁ ; wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s selected from halogen, -R51, -OR51, -N0₂, -NR51R51 , - NR₅₁C(0)R₅₁ , -NR₅₁S(0)₂R51 , -S(0)₂NR₅₁R51 , - NR₅₁C(0)NR₅₁ Rsr , -SR51 , - S(0)Rsi, -S(0)₂R₅I , -CN, haloalkyl, haloalkoxy, -C(0)0R_5i, -C(0)NR_5iR5i·, - OCH2CH2OR51, -NR₅IS(0)₂NR₅I Rsr and -C(CH₃)₂OR5i; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

wherein R₅₁, R₅₁ and R₅₁ are independently selected from hydrogen, substituted or unsubstituted C_1-6 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.

Rs is 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 alkyl, alkenyl or alkynyl defined in R₅ , if substituted, is substituted with one or more substituent/s selected from -OR₅₂, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; wherein R₅₂ and R₅₂ 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.

R₆ and Re are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO2, -NR21R2I , -NR₂IC(0)R₂₁ , -NR2lS(0)2R21 , -S(0)2NR2lR21',

NR₂IC(0)NR₂I R_21", -SR₂₁ , -S(0)R₂₁, -S(0)₂R₂₁, -CN, haloalkyl, haloalkoxy, -C(0)0R_2i , -C(0)NR₂I R₂I , -OCH2CH2OR21 , NR2iS(0)2NR2rR2i" and -C(CH3)20R2ii 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. 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, 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 =0, -OR₁₃, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13'; wherein R₁₃ and R_13’ are independently selected from hydrogen, unsubstituted Ci-e alkyl, unsubstituted C_2-6 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 =0, halogen, -RI₄, -ORu, -NO2, -NR14R14 , - NRi₄C(0)Ri4 , -NRi₄S(0)₂Ri4 , -S(0)₂NRi₄Ri4 , - NRi₄C(0)NRi_4'Ri4 ', -SR , -S(0)Ri₄, - S(0)₂Ri4, -CN, haloalkyl, haloalkoxy, -C(0)0R₁₄, -C(0)NRi₄Ri4 , -OCH₂CH₂ORI₄, - NRi₄S(0)₂NRi4 R14 and -C(CH₃)₂ORi4;

wherein R14, R14 and Ru- are independently selected from hydrogen, unsubstituted C1-6 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 the aryl or heterocyclyl in R₂, if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, -NR21R21 , -NR_2iC(0)R2i , -NR_2iS(0)2R2i , - S(0)₂NR₂₁R₂₁ , - NR₂IC(0)NR₂I R21 , -SR21 , -S(0)R₂I , -S(0)₂R2i , -CN, haloalkyl, haloalkoxy, -C(0)0R2i, -C(0)NR2iR2r, -OCH2CH2OR21, -NR2iS(0)2NR2i'R2i" and - C(CH₃)20R₂I ; 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, 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 a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the cycloalkyl in R3, if substituted, is substituted with one or more substituent/s selected from halogen, -R31, -OR31, -NO2, -NR31R31 , -NR3iC(0)R3i , -NR_3iS(0)2R3i , - S(0)₂NR₃₁R31 , - NR₃IC(0)NR₃I R31 , -SR31 , -S(0)R_3i , -S(0)₂R_3i, -CN, haloalkyl, haloalkoxy, -C(0)0R_3i, -C(0)NR₃IR₃I , -OCH₂CH₂OR₃I , -NR₃IS(0)₂NR₃I R31 and - C(CH₃)₂OR_3I ; 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, is substituted with one or more substituent/s selected from -OR₃₂, halogen, -CN, haloalkyl, haloalkoxy and -NR32R32 ; 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, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, defined in R₅, if substituted, is substituted with one or more substituent/s selected from -OR51 , halogen, -CN, haloalkyl, haloalkoxy and -NRsiRsr; 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 cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroarylor alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s selected from halogen, -R51 , -OR51 , -NO2, -NR51R51 , - NR₅₁C(0)R₅₁ , -NR_5iS(0)₂R5r, -S(0)₂NR_5iR5r, - NR₅IC(0)NR₅I Rsr, -SR51 , - S(0)Rsi, -S(0)₂R₅I , -CN, haloalkyl, haloalkoxy, -C(0)OR₅I , -C(0)NR₅IR5V, - OCH2CH2OR51 , -NR₅I S(0)2NR₅I R51 and -C(CH3)20R5i; and/or is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl;

In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein the cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryll or alkylcycloalkyl, as defined in R5, if substituted, is substituted with one or more substituent/s selected from halogen, -R51, -OR51 , -NO2, -NR51R51 , -NR5iC(0)Rsi , -NR5iS(0)₂R5i , -S(0)2NR5iRsi , - NR5iC(0)NR_5i R5i· , -SR51 , -S(0)Rsi, -S(0)₂R_5i, -CN, haloalkyl, haloalkoxy, - C(0)0RS1 , -C(0)NR₅₁R₅₁ , -OCH2CH2OR51, -NR₅₁S(0)₂NR₅₁ Rsr and -C(CH₃)₂OR₅I ; 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 cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R5, if substituted, is substituted with one or more substituent/s selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheterocyclyl; 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 cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more -NR₅₁R₅₁ ; 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 cycloalkyl, aryl or heteroaryl, also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R₅, if substituted, is substituted with one or more substituent/s 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 the alkyl, alkenyl or alkynyl defined in Rs , if substituted, is substituted with one or more substituent/s selected from -OR52, halogen, -CN, haloalkyl, haloalkoxy and -NR52R52 ; 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, 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 =0, -OR13, halogen, -CN, haloalkyl, haloalkoxy and -NR13R13'; 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, 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 =0, halogen, -Ru, -OR14, -NO2, -NR14R14 , - NRi₄C(0)Ri4 , -NRi₄S(0)₂Ri4 , -S(0)₂NRi4Ri4·, - NRi₄C(0)NRi₄ Ri4 ·, -SR14 , -S(0)Ri₄, - S(0)₂Ri4, -CN, haloalkyl, haloalkoxy, -C(0)ORi4, -C(0)NRi4Ri4 , -OCH₂CH₂ORi4, - NRi₄S(0)₂NRi4 R14 and -C(CH₃)₂ORI₄; 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_aRb)]_P-, -[C(R_aRb)]pC(0)[C(R_cRd)]q-, -[C(RaRb)]pC(0)N(R_z)[C(R_cRd)]q- , -[C(R_aRb)]pN(R_z)C(0)[C(R_cRd)]q- or -[C(R_aRb)]_PN(R_z)[C(R_cRd)]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 and C(O)- C_1-6 alkyl;

R_a is selected from hydrogen, halogen, substituted or unsubstituted C₁.6 alkyl, substituted or unsubstituted C_2-6 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 C₂-6 alkynyl; alternatively, R_a and R_b, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;

R_c is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

Rq is selected from hydrogen, substituted or unsubstituted C1.6 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 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_aRb)]_P-, -[C(R_aRb)]pC(0)[C(R_cRd)]q-, -[C(R_aRb)]_PC(0)N(R_z)[C(RoRd)]q- , -[C(R_aR_b)]pN(Rz)C(0)[C(RcRd)]q- or -[C(R_aRb)]_pN(R_z)[C(R_cRd)]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.

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 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.

R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci_-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 another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

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; 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.

R_a and R_b, 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.

R_c 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

R_d is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C₂-e 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, -[CH₂]_P-, -[CH₂]_PC(0)[CH₂]q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(R_z)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-; and/or

R_z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2.6 alkenyl, substituted or unsubstituted C₂-e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-e alkyl; preferably R_z is selected from hydrogen and substituted or unsubstituted C1-6 alkyl; more preferably R_z is selected from hydrogen and substituted or unsubstituted methyl; 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 0, 1 or 2; and/or Yi is -C(RioRio·)-; preferably Y₁ is -CH2-; and/or

Y₂ is -C(RioRio)-; preferably Y₁ is -CH2-; and/or n is 0 or 1 ; and/or

Ri is selected from -NR₅R5 and -NR₅C(0)R5; and/or

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

R₃ 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 and substituted or unsubstituted alkylcycloalkyl; preferably R₃ is substituted or unsubstituted C_1-6 alkyl; more preferably R₃ is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; and/or

R₃ is selected from hydrogen, substituted or unsubstituted Ci.₆ alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-₆ alkynyl; preferably R_3' is hydrogen; and/or

R₄ and R₄ are independently selected from halogen, -R₄₁, -OR₄₁, -NO₂, -NR₄₁R₄₁ , - NR_4IC(0)R_4I , -NR_4IS(0)₂R₄₁·, -S(0)₂NR_4iR_4i , -NR_4IC(0)NR_4I R₄r , -SR₄₁ , -S(0)R_4i, - S(0)₂R_4i, -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR_4iR_4i , -OCH₂CH₂OR₄₁, - NR_4iS(0)₂NR_4i R₄₁ · and -C(CH₃)₂OR_4I ; and/or

R₅ is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C_2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; preferably R₅ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; and/or

Rs is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R5 is selected from hydrogen and substituted or unsubstituted C_1.6 alkyl, and/or

Re and R₆ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21_’, -NR_2iC(0)R₂r, -NR2iS(0)2R2v, -S(0)2NR2iR2i\ - NR2iC(0)NR2i R2r , -SR21 , -S(0)R_2I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2I R_2I , - OCH2CH2OR21, -NR_2iS(0)₂NR_2i R21 and -C(CH₃)₂0R_2i; preferably Re and Re are hydrogen, and/or

R₁₀ and R₁₀ are independently selected from hydrogen, substituted or unsubstituted Ci. e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂.e alkynyl; preferably R₁₀ and R₁₀ are independently selected from hydrogen; and/or

Rio- 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 C2- e alkynyl; preferably R10 and Rio· are independently selected from hydrogen; and/or Rio and Rio form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; and/or

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; and/or

R₃₁, R₃₁ and R₃₁ 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;

and/or

R₃₂ and R₃₂ are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-6 alkynyl; and/or

R₄₁, R₄₁ 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, R₄₁ and R₄₁ are all hydrogen;

and/or

R₅₁, R₅₁ and R₅₁ 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 R₅₁, R₅₁ and R₅₁ are substituted or unsubstituted C1-6 alkyl; and/or

R₅₂ and R₅₂ are independently selected from hydrogen, substituted or unsubstituted Ci- e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-6 alkynyl; and/or

R13 and R13 are independently selected from hydrogen, unsubstituted C1 -6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2.6 alkynyl; and/or

R14, R_M' and Ru- are independently selected from hydrogen, unsubstituted C1.6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

X is selected from a bond,

[CH2]_PN(R_z)C(0)[CH₂]q- and -

and if X is selected from a bond, -[CH2]_P-, -[CH₂]_PC(0)[CH2]q- and -[CH2]_PN(R_z)C(0)[CH2]_q-, q is 0, 1 , 2, 3, 4 or 5; preferably q is 0, 1 or 2; and if X is selected from -[CH₂]_PC(0)N(R_z)[CH₂]q- and -[CH₂]_PN(R_z)[CH₂]q-, q is 1 , 2, 3, 4 or 5; preferably q is 1 or 2; and/or

R_z 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(0)-Ci-6 alkyl; preferably R_z is selected from hydrogen and substituted or unsubstituted C1-6 alkyl; more preferably R_z is selected from hydrogen and substituted or unsubstituted methyl; and/or p is 0, 1 , 2, 3, 4 or 5; preferably p is 0, 1 or 2; and/or

Yi is -C(RioRio )-; preferably Yi is -CH₂-; and/or

Y₂ is -C(RioRio )-; preferably Yi is -CH₂-; and/or n is 0 or 1 ; and/or

Ri is selected from -NR5R5 and -NRs CfOJRs; and/or

R3 is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C_2.6 alkenyl, substituted or unsubstituted C₂-e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably R3 is substituted or unsubstituted C1-6 alkyl; more preferably R3 is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; and/or R_3' is selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2-6 alkynyl; preferably R₃ is hydrogen; and/or

R₄ and R₄ are independently selected from halogen, -R _I , -OR_4I , -NO₂, -NR_4IR_4I , - NR _iC(0)R r, -NR _IS(0)₂R_4I , -S(0)₂NR_4iR_4r, -NR_4iC(0)NR_4rR₄r, -SR_4I , -S(0)R_4i, - S(0)₂R_4I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR_4I R _I , -OCH₂CH₂OR_4I , - NR_4IS(0)₂NR_4I R_4V and -C(CH₃)₂OR_4I ; and/or

R₅ is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C_2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl;preferably R₅ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; and/or

R₅ 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 R₅ is selected from hydrogen and substituted or unsubstituted C_1-6 alkyl, and/or

Re and Re are independently selected from hydrogen, halogen, -R₂₁, -OR₂₁, -NO₂, - NR₂₁ R_21’, -NR₂₁C(0)R₂₁ , -NR2iS(0)₂R2i_\ -S(0)₂NR_2iR2v, - NR₂₁C(0)NR₂₁ R_21", -SR₂₁ , -S(0)R_2I , -S(0)₂R_2I , -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2I R_2I , - OCH₂CH₂OR₂₁ , -NR_2IS(0)₂NR_2I R₂₁ and -C(CH₃)20R_2I ; preferably Re and Re are hydrogen, and/or R₁₀ and R₁₀ are independently selected from hydrogen, substituted or unsubstituted Ci. ₆ alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R₁₀ and R₁₀ are independently selected from hydrogen; and/or 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- e alkynyl; preferably R10 and Ri o- are independently selected from hydrogen; and/or

R10 and Ri o- form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; and/or

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; and/or

R31 , R31 and R₃r 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 R32 and R32 are independently selected from hydrogen, substituted or unsubstituted Ci.

6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; and/or

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; preferably R41 , R41 and R41 are all hydrogen;

and/or R₅₁ , R₅₁ and R₅₁ 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 R₅₁, R₅₁ and R₅₁ are substituted or unsubstituted C_1-6 alkyl; and/or

R₅₂ and R_52' are independently selected from hydrogen, substituted or unsubstituted Ci- e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; and/or

R₁₃ and R₁₃ are independently selected from hydrogen, unsubstituted C1.6 alkyl, unsubstituted C_2-6 alkenyl, and unsubstituted C2-6 alkynyl; and/or

R₁₄, R₁₄ and R are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C₂-e alkenyl, unsubstituted C_2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

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,

[CH₂]_PN(Rz)C(0)[CH₂]_q- and -

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

Yi is— C(RioRio)-; and/or

Y₂ is— C(Rio'Rio )-; and/or

R_z 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(0)-Ci-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; preferably the Ci_-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; 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

R1 is selected from -NR5R5 and -NR₅ C(0)Rs;

and/or

R_å 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, 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; preferably the heterocyclyl is thiophen; and/or

R₃ is selected from substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; 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 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 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

R₃· is 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 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

R₄ and R₄ are independently selected from halogen, -R I , -OR₄I , -NO2, -NR₄I R₄I , - NR₄I C(0)R₄V, -NR₄I S(0)₂R₄I , -S(0)₂NR_4iR₄r, -NR₄I C(0)NR₄I R_4r, -SR₄I , -S(0)R_4i, - S(0)₂R₄I , -CN, haloalkyl, haloalkoxy, -C(0)0R _i, -C(0)NR₄I R₄I , -OCH₂CH₂OR I , - NR_4iS(0)₂NR_{4i '}R₄r and -C(CH₃)₂OR I ; wherein

the alkyl is Ci-e alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl;

and/or

R5 is selected from 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, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; wherein the alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the alkyl is methyl or ethyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the Ci-e alkyl is methyl, ethyl, isopropyl or isobutyl; 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 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; preferably the cycloalkyl is cyclohexyl or cyclopropyl; and/or the aryl is selected from phenyl, naphthyl, dihydroindene or anthracene; preferably is naphthyl, dihydroindene and phenyl; preferably the aryl is phenyl or dihydroindene; and/orthe heteroaryl 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 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; preferably the heteroaryl is pyridine, thiophen, quinoline or isoquinoline;

and/or

R₅ is selected from hydrogen, substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; wherein the C_1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably 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

Re and Re are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21 R21 -NR₂₁C(0)R₂₁ , -NR2iS(0)2R2r, -S(0)2NR2IR2T, - NR2iC(0)NR₂rR2r, -SR21 , -S(0)R_2I , -S(0)₂R2i, -CN, haloalkyl, haloalkoxy, -C(0)0R2i, -C(0)NR_2iR2i , - OCH2CH2OR21, -NR21 S(0)2NR_{2I '}R21 " and -C(CH3)20R2i;

wherein the alkyl is Ci-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 Ci. e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; wherein

the Ci_-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

R₁₀ and R₁₀ may form, with the carbon atom to which they are attached, 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

Rio · 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 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

R₁₀ and Rio- may form, with the carbon atom to which they are attached, 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

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; 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 C_2-6 -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 C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; wherein the Ci-₆alkyl 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

R32 and R32 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 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 Ci_-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;

and/or

R₅₁, Rsr and R₅₁ 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 Ci-ealkyl 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

R₅₂ and R_52' are independently selected from hydrogen, substituted or unsubstituted Ci- 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 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 R₁₃ and R₁₃ are independently selected from hydrogen, unsubstituted C1.6 alkyl, unsubstituted C_2-6 alkenyl, and 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

R14, R 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 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, 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; 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_z as defined in any of the embodiments of the present invention,

the alkyl is Ci-₆ alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the Ci-₆ alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the Ci-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 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, 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; 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 Ci_-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the Ci-ealkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the Ci-e 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; 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 Ci-ealkyl 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 C_1-6 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 as defined in any of the embodiments of the present invention, the alkyl is Ci_-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the alkyl is methyl or ethyl; 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, ethyl, isopropyl or isobutyl; 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; preferably the cycloalkyl is cyclohexyl or cyclopropyl; and/or the aryl is selected from phenyl, naphthyl, dihydroindene or anthracene; preferably is naphthyl, dihydroindene and phenyl; preferably the aryl is phenyl or dihydroindene; and/or

the heteroaryl 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 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; preferably the heteroaryl is pyridine, thiophen, quinoline or isoquinoline; 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 as defined in any of the embodiments of the present invention, the Ci-₆ alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the Ci-e 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;

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in Re and R₆ as defined in any of the embodiments of the present invention, the alkyl is Ci-e 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 R₁₀ as defined in any of the embodiments of the present invention, the Ci-ealkyl 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 Rio and Rio 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 Rnr and R10 as defined in any of the embodiments of the present invention, the Ci-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;

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

the Ci-₆alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the Ci_-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 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 R₃₁, R₃₁ and R₃₁ 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 R₃₂ and R₃₂ as defined in any of the embodiments of the present invention,

In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R₄₁ , R₄r and R₄r as defined in any of the embodiments of the present invention,

the Ci.₆alkyl 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 R₅₁, R₅₁ and R₅₁ 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; 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; 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 R₅₂ and R₅₂ as defined in any of the embodiments of the present invention,

the Ci-₆alkyl 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 R₁₃ and R_13' 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 R , R and R_M as defined in any of the embodiments of the present invention, the Ci-ealkyl 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 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 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, 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 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 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 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.

X is selected from a bond, -[CH₂]_P-, -[CH₂]pC(0)[CH₂]_q-, -[CH₂]_pC(0)N(R_z)[CH₂]_q-, - [CH₂]_pN(Rz)C(0)[CH₂]_q- and -[CH₂]_pN(R_z)[CH₂]_q-; preferably X is selected from a bond, -CH2-, -CH2CH2-, -C(O)-, -C(0)NH-, -C(0)NHCH2-,-C(0)NHCH2CH2-, -NHC(O)-, - NHC(0)CH2-, )-, -NHC(0)CH2CH2-, -N(CH3)C(0)CH2CH2-, -CH2NH-, -NHCH2-, - NHCH2CH2-, -N(CH3)CH2CH2- and -CH2NHCH2-; 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

Yi is -C(RioRio)-; 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.

Y2 is -C(Ri<rRio")-; 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.

R_z is selected from hydrogen, substituted or unsubstituted Ci-₆ alkyl, substituted or unsubstituted C₂-e alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-₆ alkyl; preferably R_z is selected from hydrogen and substituted or unsubstituted C1.6 alkyl; more preferably R_z 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

Ri is selected from-NRsRs and -NRs C(0)Rs; preferably Ri is a substituted or unsubstituted group selected from -N(CH3)(CH2CH3)-, -N(CH3)(cyclopropyl)-, -NH- cyclohexyl, -NH-pyridinyl, -NH-phenyl, -NH-CH2-pyridinyl, -NH-CH2-phenyl, -NH- CH2-CH(N[CH3]2)-phenyl, -NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2- quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2- dihydroindenyl, -N(CH3)2, -N(CH3)(isobutyl), -N(CH3)(CH2-phenyl), N(CH3)(CH2CH2-phenyl), -N(CH3)(CH2-thienyl), -NHC(0)-pyridinyl, -NHC(O)- isopropyl, -NHC(0)-phenyl, -NHC(0)-CH2-thienyl and -NHC(0)-CH2-phenyl.

Ri is selected from-NRsRs and -NR₅C(0)R₅; preferably Ri is a substituted or unsubstituted group selected from NH-cyclohexyl, -NH-pyridinyl, -NH-phenyl, -NH- CH2-pyridinyl, -NH-CH2-phenyl, -NH-CH2-CH(N[CH3]2)-phenyl, -NH-CH2CH2- phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-isoquinolinyl, -NH- CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2-dihydroindenyl, -N(CH3)2, N(CH3)(isobutyl), -N(CH3)(CH2-phenyl), -N(CH3)(CH2CH2-phenyl), -N(CH3)(CH2- thienyl), -NHC(0)-pyridinyl, -NHC(0)-isopropyl, -NHC(0)-phenyl, -NHC(0)-CH2- thienyl and -NHC(0)-CH2-phenyl.

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 selected from substituted or unsubstituted phenyl and substituted or unsubstituted 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.

R₃ is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, substituted or unsubstituted C₂-e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably R3 is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl; 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; preferably, R3 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.

R₄ and R₄ are independently selected from halogen, -R₄I , -OR₄I , -NO2, -NR₄I R I , - NR₄₁C(0)R₄₁ , -NR₄₁S(0)₂R₄₁ , -S(0)₂NR_4iR_4i , -NR₄IC(0)NR₄I R₄r, -SR₄I , -S(0)R_4i, - S(0)₂R_4I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, -C(0)NR₄I R₄I , -OCH₂CH₂OR₄I , - NR₄IS(0)₂NR₄I R₄r and -C(CH3)₂OR₄I ; wherein R I , R₄r and R₄r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C₂.6 alkenyl and substituted or unsubstituted C_2.6 alkynyl; 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 is selected from substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; preferably R5 is selected from substituted or unsubstituted C1 -6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryll; more preferably R5 is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2-pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2- quinolinyl, , -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, cyclopropyl and 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.

Rs is selected from substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryl; preferably R5 is selected from substituted or unsubstituted C1 -6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted alkylheteroaryll; more preferably R5 is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2-pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2- quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2-dihydroindenyl and 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.

Rs is 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 R5 is selected from hydrogen and substituted or unsubstituted Ci_-6 alkyl, more preferably R₅ 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.

Re and Re are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21', -NR2iC(0)R₂r, -NR2iS(0)2R2v, -S(0)2NR2iR2r, - NR2iC(0)NR2i R2i”, -SR21 , -S(0)R2i, -S(0)2R2i, -CN, haloalkyl, haloalkoxy, -C(0)0R_2i, -C(0)NR_2iR2r, - OCH2CH2OR21, -NR_2iS(0)₂NR_2i R21 and -C(CH₃)20R_2I ; preferably, Re and Re 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 are independently selected from hydrogen, substituted or unsubstituted Ci. 6 alkyl, substituted or unsubstituted C_2.6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably, R10 and Rio 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.

Rio- 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; preferably, Rio- and R10 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.

R21 , R21 and R21 are independently selected from hydrogen, substituted or unsubstituted Ci.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.

R₃₁, R₃₁ and R₃r 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.

R₃₂ and R₃₂ are independently selected from hydrogen, substituted or unsubstituted Ci. e 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.

R₄₁, R_{41 '} and R₄₁ are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C₂-e alkenyl and substituted or unsubstituted C_2-6 alkynyl; preferably, R₄₁ 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.

R₅₁, R₅₁ and R₅₁ 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 R₅₁ and R₅₁ are independently 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.

R₅₂ and R₅₂ are independently selected from hydrogen, substituted or unsubstituted Ci- e 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 another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein R₁₃ and R_13' are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C_2-6 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.

Ri4, R₁₄ and R₁₄ are independently selected from hydrogen, unsubstituted Ci_-6 alkyl, unsubstituted C_2-6 alkenyl, unsubstituted C₂-e alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; preferably R₁₄ 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 p is 0, 1 or 2; and q is 0, 1 or 2; and n is 0 or 1 ; and X is selected from a bond, -CH2-, -CH2CH2-, -C(O)-, -C(0)NH-, -C(0)NHCH2-,- C(0)NHCH2CH2-, -NHC(O)-, -NHC(0)CH2-, )-, -NHC(0)CH2CH2-,

N(CH3)C(0)CH2CH2-, -CH2NH-, -NHCH2-, -NHCH2CH2-, -N(CH3)CH2CH2- and - CH2NHCH2-; and

Yi is -CH2-; and

Y₂ is -CH2-; and

R_z is selected from hydrogen and substituted or unsubstituted Ci-e alkyl; more preferably R_z is selected from hydrogen and substituted or unsubstituted methyl; and

Ri is a substituted or unsubstituted group selected from -N(CH3)(CH2CH3)-, - N(CH3)(cyclopropyl)-, -NH-cyclohexyl, -NH-pyridinyl, -NH-phenyl, -NH-CH3-pyridinyl, - NH-CH2-phenyl, -NH-CH2-CH(N[CH3]2)-phenyl, -NH-CH2CH2-phenyl, -NH- CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2-thienyl, - NH-CH2CH2-thienyl, -NH-CH2-dihydroindenyl, -N(CH3)2, -N(CH3)(isobutyl), - N(CH3)(CH2-phenyl), -N(CH3)(CH2CH2-phenyl), -N(CH3)(CH2-thienyl), -NHC(O)- pyridinyl, -NHC(0)-isopropyl, -NHC(0)-phenyl, -NHC(0)-CH2-thienyl and -NHC(O)- CH2-phenyl; and

R₂ is selected from substituted or unsubstituted phenyl and substituted or unsubstituted thiophen; and

R3 is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl; and R3' is hydrogen; and

R₄ and R₄ are both hydrogen; and R₅ is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, , -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2- dihydroindenyl, cyclopropyl and cyclohexyl; and R₅ is selected from hydrogen and substituted or unsubstituted methyl; and

R₆ and R₆ are both hydrogen; and

R10 and Ri₀ are both hydrogen; and

R10 and R10 are both hydrogen; and

R₄I is hydrogen; and R₅₁ and R₅₁ are independently selected from hydrogen and substituted or unsubstituted methyl; and

RM 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 a preferred embodiment p is 0, 1 or 2;

In a preferred embodiment q is 0, 1 or 2;

In a preferred embodiment n is 0 or 1 ;

In a preferred embodiment

X is selected from a bond, -CH2-, -CH2CH2-, -C(O)-, -C(0)NH-, -C(0)NHCH2-, - C(0)NHCH2CH2-, -NHC(O)-, -NHC(0)CH2-, -NHC(0)CH2CH2-,

N(CH3)C(0)CH2CH2-, -CH2NH-, -NHCH2-, -NHCH2CH2-, -N(CH3)CH2CH2- and - CH2NHCH2-;

In a preferred embodiment

X is selected from a bond, -CH2-, -CH2CH2-, -C(O)-, -C(0)NHCH2-, - C(0)NHCH2CH2-, -NHC(O)-, -NHC(0)CH2-, -NHC(0)CH2CH2-,

N(CH3)C(0)CH2CH2-, -NHCH2-, -NHCH2CH2-, -N(CH3)CH2CH2- and -CH2NHCH2-

In a preferred embodiment

Yi is -CH2-; In a preferred embodiment

Y₂ is -CH2-;

In a preferred embodiment

R_z is selected from hydrogen and substituted or unsubstituted methyl;

In a preferred embodiment

Ri is a substituted or unsubstituted group selected from -NH-cyclohexyl, -NH-pyridinyl, -NH-phenyl_t -NH-CH3-pyridinyl, -NH-CH2-phenyl, -NH-CH2-CH(N[CH3]2)-phenyl, - NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2- isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2-dihydroindenyl, - N(CH3)2, -N(CH3)(isobutyl), -N(CH3)(CH2-phenyl), -N(CH3)(CH2CH2-phenyl), - N(CH3)(CH2-thienyl), -NHC(0)-pyridinyl, -NHC(0)-isopropyl, -NHC(0)-phenyl, NHC(0)-CH2-thienyl and -NHC(0)-CH2-phenyl.

In another preferred embodiment

Ri is a substituted or unsubstituted group selected from -N(CH3)(CH2CH3), - N(CH3)(CH2CH20CH3), -N(CH3)(CH2CH2-CN), -N(CH3)(cyclopropyl), -NH- cyclohexyl, -NH-pyridinyl, -NH-phenyl, -NH-CH3-pyridinyl, -NH-CH2-phenyl, -NH- CH2-CH(N[CH3]2)-phenyl, -NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2- quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2- dihydroindenyl, -N(CH3)2, -N(CH3)(isobutyl), -N(CH3)(CH2-phenyl), N(CH3)(CH2CH2-phenyl), -N(CH3)(CH2-thienyl), -NHC(0)-pyridinyl, -NHC(O)- isopropyl, -NHC(0)-phenyl, -NHC(0)-CH2-thienyl and -NHC(0)-CH2-phenyl.

In a preferred embodiment

R₂ is selected from substituted or unsubstituted phenyl and substituted or unsubstituted thiophen;

In a preferred embodiment

R3 is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl; In a preferred embodiment

R3 is hydrogen;

In a preferred embodiment R₄ and R₄ are both hydrogen; In a preferred embodiment

Rs is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl. In another preferred embodiment

Rs is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, CH2CH3, CH2CH20CH3, CH2CH2-CN, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, - CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, cyclopropyl and cyclohexyl.

In a preferred embodiment

Rs is selected from hydrogen and substituted or unsubstituted methyl; In a preferred embodiment R₆ and Rs are both hydrogen;

In a preferred embodiment R10 and R10 are both hydrogen; In a preferred embodiment R10 and R10 are both hydrogen; In a preferred embodiment

R₁₄ is hydrogen;

In a preferred embodiment R₄₁ is hydrogen; In a preferred embodiment

R₅₁ and R₅₁ are both substituted or unsubstituted methyl;

In a preferred embodiment

R₅₁ is substituted or unsubstituted methyl;

In a preferred embodiment

R₅₁ is hydrogen;

In a preferred embodiment

R₃ is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl, while R₃ is hydrogen;

In a preferred embodiment

Rs is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, , -CH2-isoquinolinyl, -CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl, while Rs is selected from hydrogen and substituted or unsubstituted methyl.

In another preferred embodiment

Rs is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, CH2CH3, CH2CH20CH3, CH2CH2-CN, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, , -CH2-isoquinolinyl, - CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, cyclopropyl and cyclohexyl, while R₅ is selected from hydrogen and substituted or unsubstituted methyl.

In a preferred embodiment R₅ is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2- dihydroindenyland cyclohexyl, while R5 is hydrogen.

In a preferred embodiment

R₅ is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2- dihydroindenyl, and cyclohexyl, while R5 is substituted or unsubstituted methyl. In a preferred embodiment

Rs is a substituted or unsubstituted group selected from methyl, isobutyl, benzyl, phenethyl and thienyl, while Rs· is substituted or unsubstituted methyl.

In another preferred embodiment

R₅ is a substituted or unsubstituted group selected from methyl, ethyl, isobutyl, CH2CH20CH3, CH2CH2-CN, cyclopropyl, benzyl, phenethyl and -CH2-thienyl, while R₅ is substituted or unsubstituted methyl

In a preferred embodiment

Rs is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2- pyridinyl, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, -CH2- quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl and cyclohexyl, while R5 is hydrogen; In an embodiment of the compound according to the invention of general Formula (I), the halogen is fluorine, chlorine, iodine or bromine; 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 compound is

In a preferred further embodiment, the compound is

In a preferred further embodiment, the compound is

As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the a2d subunit, particularly the a2d-1 subunit, of the voltage-gated calcium channel it is a very preferred embodiment in which the compounds are selected which act as ligands of the a2d subunit, particularly the a2d-1 subunit, of the voltage-gated calcium channel and especially compounds which have a binding expressed as Ki responding to the following scales:

Kί(a2d1) 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), (G), (l^a), (l^a’)_ (l^b), (l^b>) 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. Ri, R₂, R_3I R₃ , R₄, R₄ , X, Ui, 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 aspect of the invention is also a process for the production of a compound according to Formula (I), following scheme 1 , scheme 2, scheme 3, scheme 4, scheme 5, scheme 6 or scheme 7.

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 7. A preferred embodiment of the invention is a process for the production of a compound according to Formula (I), wherein, if not defined otherwise, Ri , R₂ R3, R3 , R₄, R₄ , X, Yi , Y₂ and n have the meanings defined in the description.

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

wherein -X is a bond and Ri represents -NR₅R₅ , Y1 and Y2 both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (I la)

wherein Q represents chloro, bromo, iodo or triflate, A represents -NR3R3' and R₂, R3, R₃·_, R_4I R₄ and n have the meanings as defined in the description, with an amine of formula III-2 ^R- NH

i

5'

III-2 wherein R₅ and R₅ have the meanings as defined in the description.

wherein -X is a bond and R1 represents -NRs C(0)R₅ , Y1 and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄· and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (I la)

lla wherein Q represents chloro, bromo, iodo or triflate, A represents -NR3R3 and R₂, R3, R₃·_, R_4I R₄ and n have the meanings as defined in the description, with an amine of formula III-3

111-3 wherein Rs and Rs have the meanings as defined in the description.

(0 wherein -X-Ri represents -[CH₂]p-NRsRs·, Yi and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (Mb)

wherein r is 1 , 2, 3 or 4, A represents -NR3R3' and R2, R3, R3' R₄, R₄· and n have the meanings as defined in the description, with an amine of formula III-2

wherein R₅ and R₅ have the meanings as defined in the description.

wherein -X-R₁ represents -[Ch^p-NRsRs·, Y1 and Y2 both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄· and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (lla)

lla wherein Q represents chloro, bromo, iodo or triflate, A represents -NR₃R3' and R₂, R3, R₃ R_4I R₄ and n have the meanings as defined in the description, with an organometallic reagent of formula III-4

111-4 wherein R₅ and R₅ and p have the meanings as defined in the description, and M represents a suitable organometallic group, preferably a boron or zinc reagent.

wherein -X is a bond and Ri represents -NR₅R₅ Y1 and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ , Rs, Rs and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (lie),

wherein A represents -NR₃R_3' and R2, R₃, R₃ , R₄, R₄ and n have the meanings as defined in the description, with an aldehyde of formula 111-5 under reductive amination conditions

Rs-CHO

Hl-5 or with an alkylating agent of formula III-6, under conventional alkylation conditions

Rs-LG

III-6 wherein R₅ has the meanings as defined in the description and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate.

wherein -X is a bond and Ri represents -NR₅C(0)Rs , Yi and Y₂ both represent -CH₂- _, and wherein R₂, R₃, R₃·, R₄, R₄ , Rs, Rs and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (le)

le wherein A represents -NR₃R₃· and R₂, R₃, R₃ , R₄, R₄ , Rs and n have the meanings as defined in the description, with an alkylating agent of formula III-6’

R .-LG

III-6^* wherein R₅ has the meaning as defined in the description but different from hydrogen, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate.

wherein -X is -[CH₂]p- and Ri represents -C(0)NR₅Rs , Yi and Y₂ both represent - CH_2-, and wherein R₂, R₃, R₃ , R₄, R₄ , Rs, Rs· and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (lid)

wherein A represents -NR₃R₃· and R₂, R₃, R₃ , R₄, R₄ and n and p have the meanings as defined in the description, with an amine of formula III-2 under amidation conditions

^R- NH

R₅'

MI-2 wherein Rs and Rs have the meanings as defined in the description.

wherein n is 0, Y1 and Y₂ both represent -CH_2-, and wherein Ri , R₂, R₃, R₃ , R₄, R₄· and X have the meanings as defined in the description, said process comprises reacting a compound of Formula (Via)

wherein G is OH, and R₄, R₄ have the meanings as defined in the description, with a compound of formula VII

wherein Z represents OH (in which case Mitsunobu type condictions apply) or a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate (in which case alkylation conditions apply), A represents -NR₃R_3' and R₂, R₃ and R₃ , have the meaning as defined in the description.

wherein n is 1 , Y1 and Y₂ both represent -CH₂- and wherein R1, R₂, R3, R3 , R₄, R₄ and X have the meaning as defined in the description, said process comprises reacting a compound of Formula (Vlb)

with a compound of formula VII

VII 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 and wherein R₄, R₄ have the meanings as defined in the description, A represents -NR₃R_3' and R₂, R₃ and R₃ , have 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 is a bond and R₁ represents -NR₅R₅ Y₁ and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R_4' and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (lla)

lla wherein Q represents chloro, bromo, iodo or triflate, A represents -NR₃R_3' and R₂, R3, R_{3 ,} R₄, R₄ and n have the meanings as defined in the description, with an amine of formula III-2

III-2 wherein Rs and Rs have the meanings as defined in the description; or

wherein -X is a bond and Ri represents -NRs C(0)Rs , Yi and Y₂ both represent -CH₂- _, and wherein R₂, R₃ R₃ , R₄, R₄ and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (lla)

wherein Q represents chloro, bromo, iodo or triflate, A represents -NR₃R₃· and R₂, R_3, R_{3 ,} R₄, R₄ and n have the meanings as defined in the description, with an amine of formula III-3

III-3 wherein Rs and Rs have the meanings as defined in the description;

or

wherein -X-Ri represents -[CH^p-NRsRs·, Yi and Y₂ both represent -CH₂- and wherein R₂, R3, R3 , R₄, R_4' and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (lib)

wherein r is 1 , 2, 3 or 4, A represents -NR₃R_3' and R2, R3, R3', R4, R₄ and n have the meanings as defined in the description, with an amine of formula III-2

wherein R₅ and R₅ have the meanings as defined in the description;

or

wherein -X-R₁ represents -[Chklp-NRsRs·, Y₁ and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R_4I R₄ and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (lla)

lla wherein Q represents chloro, bromo, iodo or triflate, A represents -NR₃R_3' and R₂, R3, R₃·_, R_4I R₄ and n have the meanings as defined in the description, with an organometallic reagent of formula 111-4

III-4 wherein R₅ and R₅ and p have the meanings as defined in the description, and M represents a suitable organometallic group, preferably a boron or zinc reagent;

or

wherein -X is a bond and R1 represents -NR₅R₅ Y1 and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ , Rs, Rs and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (lie),

lie wherein A represents -NR3R3' and R₂, R3, R3 , R₄, R₄ and n have the meanings as defined in the description, with an aldehyde of formula III-5 under the reductive amination

Rs-CHO

III-5 or with an alkylating agent of formula III-6, under conventional alkylation conditions

Rs-LG

ni-6 wherein Rs has the meanings as defined in the description and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or

wherein -X is a bond and Ri represents -NRsC(0)Rs , Yi and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ , Rs, Rs and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (le)

wherein A represents -NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ , Rs and n have the meanings as defined in the description, with an alkylating agent of formula III-6’

R₅-LG

III-6' wherein Rs· has the meanings as defined in the description but different from hydrogen, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or wherein -X is -[CH₂]p- and R₁ represents -C(0)NRsR₅ , Y1 and Y₂ both represent - CH₂- and wherein R₂, R₃, R_3\ R₄, R₄ , Rs, Rs and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (lid)

wherein A represents -NR3R3' and R_2l R3, R3 , R₄, R₄ and n and p have the meanings as defined in the description, with an amine of formula 111-2 under amidation conditions

111-2 wherein R₅ and R₅ have the meanings as defined in the description;

or

wherein n is 0, Y₁ and Y₂ both represent -CH₂- and wherein R1, R₂, R3, R3 , R₄, R₄ and X have the meanings as defined in the description, said process comprises reacting a compound of Formula (Via)

Via wherein G is OH, and R₄, R₄ have the meanings as defined in the description, with a compound of formula VII

VII wherein Z represents OH or a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, A represents -NR₃R_3' and R₂, R₃ and R₃ , have the meaning as defined in the description;

or

wherein n is 1 , Y1 and Y₂ both represent -CH₂- and wherein Ri, R₂ R₃, R₃ , R₄, R₄· and X have the meaning as defined in the description, said process comprises reacting a compound of Formula (Via)

with a compound of formula VII

VII 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 or a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, and wherein R₄, R₄ have the meanings as defined in the description, A represents -NR₃R_3' and R₂, R₃ and R₃ , have 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), 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 HCI 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 °C.

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 °C.

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

II

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, and Y represent suitable functional groups for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula

(Ha),

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n have the meaning 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, for the preparation of compounds of Formula (I).

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

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n and r have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, for the preparation of compounds of Formula (I).

(He),

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n have the meaning as defined in the description, 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 (lid),

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n and p have the meaning as defined in the description, 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 (H I),

Ri-W

HI

wherein Ri has the meaning as defined in the description and W represent suitable functional groups, for the preparation of compounds of Formula (I).

A particular embodiment of the invention refers to the use of a compound of Formula (MI-2),

wherein Rs and Rs’ 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 (MI-3)

III-3

A particular embodiment of the invention refers to the use of a compound of Formula (MI-4)

MI-4

wherein p, Rs and Rs’ 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).

5

A particular embodiment of the invention refers to the use of a compound of Formula (MI-5)

R₅-CHO

III-5

wherein Rs has the meaning as defined in the description, for the preparation of

10 compounds of Formula (I).

Rs-LG

,5 '"-⁶

wherein Rs has the meaning 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).

20

R₅-LG

III-6·

wherein Rs has the meaning as defined in the description, and LG represents a leaving 25 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 (IVb),

IVb wherein A=LG

wherein A is LG, R₂, R₄, R₄ , Rs, Rs’ and n have the meaning as defined in the description, 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 (IVc),

c w er n

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

IVd wherein A=LG wherein A is LG, R₂, R₄, R₄ , Rs, Rs’ and n and p have the meaning as defined in the description, 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 (IVe),

IVe wherein A=LG

wherein A is LG, R₂, R₄, R₄ , Rs and n have the meaning as defined in the description, 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 (IVf),

IVf wherein A=LG

wherein A is LG, R₂, R₄, R₄ , Rs, Rs’ and n and p have the meaning as defined in the description, 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 (IVg),

IVg wherein A=LG

wherein A is LG, Ri, R₂, R₄ and R₄ have the meaning as defined in the description, 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 (IVh),

IVh wherein A=LG

wherein A is LG, R1, R₂, R₄ and R₄ have the meaning as defined in the description, 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 (V)

HNR₃R₃.

v

wherein R3 and R₃ have the meaning as defined in the description, for the preparation of compounds of Formula (I). In a particular embodiment there is the use of a compound of Formula (VI)

VI

wherein G represents OH, halogen or a leaving group, Ri, R₄ and R₄ and n 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 (Via)

wherein G represents OH, halogen or a leaving group, Ri , R₄ and R₄· 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 (Vlb)

wherein G represents OH, halogen or a leaving group, Ri , R₄ and R₄ 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 (VII)

VII

wherein Z represents OH or a leaving group, A is LG or NR3R3 , R2, R3 and R3 have the meaning 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 (VIM)

VIII

Y represents a suitable functional group, G represents OH, halogen or a leaving group, R₄ and R₄ and n 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 (II),

II

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, and Y represent suitable functional groups; or of a compound of Formula (lla)

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n have the meaning 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;

or of a compound of Formula (lib),

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n and r have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (lie),

lie

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (lid),

lid wherein A is LG or NR3R3 and R₂, R3, R3 , R₄, R₄ and n and p have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (III),

wherein R1 has the meaning as defined in the description and W represent suitable functional groups; or of a compound of Formula (111-2),

wherein Rs and Rs’ have the meaning as defined in the description;

or of a compound of Formula (MI-3)

III-3

wherein Rs and Rs’ have the meaning as defined in the description; or of a compound of Formula (III-4)

IIM

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

or of a compound of Formula (III-5)

R5-CHO

III-5

wherein R₅ has the meaning as defined in the description;

or of a compound of Formula (MI-5) Rs-LG

III-6

wherein R5 has the meaning as defined in the description, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (III-5)

R₅-LG

III-6’

or of a compound of Formula

IVb wherein A=LG

wherein A is LG, R2, R₄, R₄·, Rs, Rs’ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula

O IVc wherein A=LG

wherein A is LG, R2, R₄, R₄ , Rs, Rs’ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula

IVd wherein A=LG wherein A is LG, R₂, R₄, R₄·, Rs, Rs’ and n and p have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula

IVe wherein A=LG

wherein A is LG, R₂, R , R₄ , Rs and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula

IVf wherein A=LG

wherein A is LG, R₂, R₄, R₄ , Rs, Rs’ and n and p have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula

IVg wherein A=LG

wherein A is LG, Ri, R₂, R₄ and R₄ have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (IVh),

IVh wherein A=LG

or of a compound of Formula (V)

HNR₃R₃.

v

wherein R₃ and R₃ have the meaning as defined in the description;

or of a compound of Formula (VI)

VI

wherein G represents OH, halogen or a leaving group, Ri , R₄ and R and n have the meaning as defined in the description;

or of a compound of Formula (Via)

Via

wherein G represents OH, halogen or a leaving group, Ri , R₄ and R have the meaning as defined in the description;

or of a compound of Formula (Vlb)

wherein G represents OH, halogen or a leaving group, Ri, R₄ and R₄ have the meaning as defined in the description;

or of a compound of Formula (VII)

VII

wherein Z represents OH or a leaving group, A is LG or NR₃R₃ , R_å, R3 and R3' have the meaning as defined in the description and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (VIII)

VIII

Y represents a suitable functional group, G represents OH, halogen or a leaving group, R₄ and R₄ and n have the meaning as defined in the description,

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 7.

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:

HNR₃R₃. V

Method A wherein Ri, R₂, R3, R3 , R₄, R_4\ X and n have the meanings as defined in claim 1 , LG represents a leaving group, and Y and W represent suitable functional groups to perform such transformation 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 in a microwave reactor. 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 ll-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 la, lb and lc starting from a compound of formula lla or lla-LG is represented in Scheme 1 :

wherein R₂ R₃, R₃ , R₄, R₄·, Rs, Rs and n have the meanings as defined in claim 1 , Q represents chloro, bromo, iodo or triflate, LG represents a leaving group (such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate). In turn, the preparation of a compound of formula lb from a compound of formula I la is carried out by treating a compound of formula lla with an amine of formula III-2 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 Af ./^-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.

Finally, the preparation of a compound of formula lc from a compound of formula lla is carried out by treating a compound of formula lla with an amide of formula III-3 under the same Ullmann arylation conditions described above for the preparation of a compound of formula lb.

Alternatively, the amino group NR₃R₃ present in a compound of formula lb, lc or lla can be incorporated later in the synthesis by reaction of a precursor compound of formula IVb, IVc or lla-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-Ri represents -[ChUlp-NRsRs , resulting in compounds of formula Id, starting from a compound of formula lib or llb-LG is represented in Scheme 2:

lla A=NR₃R₃. _

lla-LG A=LG J ^v wherein R₂, R3, R3 , R₄, R₄ , Rs, Rs , 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 Id from an aldehyde compound of formula lib can be carried out by treating a compound of formula Mb with an amine of formula III-2 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. Alternatively, a compound of formula Id can be prepared by reacting a compound of formula lla with an organometallic reagent of formula 111-4, preferably a boron or zinc reagent, under coupling conditions. 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).

In addition, the amino group NR3R3 present in a compound of formula Id, lla or Mb can be incorporated later in the synthesis by reaction of a precursor compound of formula IVd, lla-LG or llb-LG, respectively, with an amine of formula V following the conditions described above in Method A.

Scheme 3

An alternative synthetic route according to method A for preparing compounds of formula lb and lc starting from an amino compound of formula lie or llc-LG is represented in Scheme 3:

le A=NR₃R₃. lc A=NR₃R_r

IVe A=LG ^{J V} IVc-LG A=LG ^V wherein R₂, R3, R3 , R₄, R₄ , Rs, Rs and n 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 preparation of a compound of formula lb from an amino compound of formula lie can be carried out by treating a compound of formula lie with an aldehyde of formula III-5 under the reductive amination conditions described above in Scheme 2 or alternatively by treating a compound of formula lie with an alkylating agent of formula III-6, under conventional alkylation conditions such as described in Method A. Alternatively a compound of formula lc wherein R₅ is H (a compound of formula le) can be prepared by the amidation reaction between a compound of formula II and an acylating agent of formula MI-7. When Z is OH, the compound of formula MI-7 is a carboxylic acid and the reaction is carried out using a suitable coupling reagent such as A/-(3-dimethylaminopropyl)-/V-ethylcarbodiimide (EDC), dicyclohexylcarbodiimide (DCC), /V-[(dimethylamino)-1 H-1 ,2,3-triazolo-[4,5-/)]pyridin-1 -ylmethylene]-/\/- methylmethanaminium hexafluorophosphate N- oxide (HATU) or A/.A/.A/'.A/'-tetramethyl- 0-(1/-/-benzotriazol-1 -yl)uronium hexafluorophosphate (HBTU), optionally in the presence of 1-hydroxybenzotriazole, optionally in the presence of an organic base such as A/-methylmorpholine or A/,A/-diisopropylethylamine, in a suitable solvent such as dichloromethane or dimethylformamide, and at a suitable temperature, preferably at room temperature. When Z is halogen, the compound of formula 111-7 is an acyl halide and the reaction is carried out 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 A/,A/-diisopropylethylamine or an inorganic base such as K2CO3; and at a suitable temperature, preferably comprised between 0 °C and room temperature. Additionally, an activating agent such as 4-dimethylaminopyridine can be used. Finally, a compound of formula lc can be alternatively prepared by reacting a compound of formula le with an alkylating agent of formula MI-6’. This alkylation reaction is carried out in an aprotic solvent, preferably dimethylformamide, in the presence of an inorganic base such as NaH, at a suitable temperature, preferably at room temperature.

In addition, the amino group NR3R3 present in a compound of formula lb, lc, le, or lie can be incorporated later in the synthesis by reaction of a precursor compound of formula IVb, IVc, IVe or llc-LG, respectively, with an amine of formula V following the conditions described above in Method A.

Scheme 4 The general synthetic route according to method A for preparing compounds of formula (I) wherein -X-R1 represents -[CH₂]_P-C(0)NR₅R_5', resulting in compounds of formula If, starting from a compound of formula lid or lld-LG is represented in Scheme 4:

wherein R₂, R₃, R₃ , R₄, R₄ , Rs, Rs , 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 If from an acid compound of formula lid and an amine of formula III-2 can be carried out under the amidation conditions described above in Scheme 3.

METHOD B

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

Method B

wherein Ri, R₂, R₃, R₃ , R₄, R₄ , X 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 Ig, is represented in Scheme 5:

Via Ig A=NR₃R₃

IVg A=LG 3 V HNR3R3' wherein Ri, R₂, R₃, R₃ , R₄, R₄ and X 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 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 K₂C0₃, Cs₂C03, sodium hydride or potassium terf-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 Via with an alcohol of formula VII 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 VII with a compound of formula Via wherein G represents halogen (preferably fluoro), in the presence of a strong base such as sodium hydride or potassium terf-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 VII 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 Ih, is represented in Scheme 6:

IVh A=LG 3 V HNR₃R₃' wherein Ri, R₂, R₃, R₃ , R₄, R₄ and X 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 VI from a common precursor of formula VIII is summarized in Scheme 7 below:

VI wherein Ri, R₂, R3, R3 , R₄, R₄ , X and n have the meanings as defined in claim 1 , and G, W, Y and Z have the meanings as defined above in Schemes 1 to 6.

The preparation of a compound of formula VI from a compound of formula VIII 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 ll-LG from a compound of formula VIII and a compound of formula VII can be carried out under the reaction conditions described above in general Method B and further detailed in Schemes 5 and 6.

The compounds of formula III, III-2, III-3, III-4, MI-5, MI-6, MI-6’, MI-7, V, VII and VIII 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 (terf- 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

AcOH: acetic acid

ADDP: 1 , 1 '-(azodicarbonyl)dipiperidine

aq.: aqueous

BINAP: 2,2’-bis(diphenylphosphino)-1 , T-binaphthyl

Boc: terf-butoxycarbonyl

CH: cyclohexane

DCE: dichloroethane

DCM: dichloromethane

Deprot.: deprotection

DIAD: diisopropyl azodicarboxylate

DIBALH: diisobutylaluminum hydride DIPEA: A/,/V-diisopropylethylamine

DMF: A/,A/-dimethylformamide

DMSO: dimethylsulfoxide

EtOAc: ethyl acetate

EtOH: ethanol

EX: example

h: hour/s

HATU: 0-(7-azabenzotriazol-1-yl)-/\/,A/,A/',/\/'-tetramethyluronium hexafluorophosphate

HPLC: high performance liquid chromatography

INT: intermediate

MeOH: methanol

MS: mass spectrometry

Min: minutes

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

Quant: quantitative

Ret.: retention

r.t.: room temperature

Sat: saturated

Sol.: solution

Teoc: 2-(trimethylsilyl)ethoxycarbonyl

TFA: trifluoroacetic acid

THF: tetrahydrofuran

TMSI: trimethylsilyl iodide (or also named iodotrimethylsilane)

Wt: weight

The following methods were used to determine the HPLC-MS spectra: Method A

Column: Gemini-NX 30 x 4.6 mm, 3 um

Temperature: 40 °C

Flow: 2.0 mL/min

Gradient: NH₄HCO₃ pH 8 : ACN (95:5)— 0.5min— (95:5)— 6.5min— (0: 100)— 1 min— (0:100)

Sample dissolved approx. 1 mg/ml_ in NH₄HCO₃ PH 8/ ACN Method B

Column: Kinetex EVO 50 x 4.6 mm, 2.6 um

Temperature: 40 °C

Flow: 2.0 mL/min

Sample dissolved approx. 1 mg/mL in NH₄HCO₃ PH 8/ CAN Method C

Column: Kinetex EVO 50 x 4.6 mm, 2.6 um

Temperature: 40 °C

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. 1 mg/mL in NH₄HCO₃ PH 8/ CAN Method D

Column: Kromasil C18 250 x 4,6 mm 5um

Temperature: 40 °C

Flow: 1 mL/min

Gradient: H₂O-0.1 %HCOOH / ACN (100:0)— 30min— (0: 100)

Sample dissolved approx. 4mg/mL in ACN/H2O 1 : 1

Method E

Column: Luna C18 250 x 4,6 mm 5um

Temperature: 40 °C

Flow: 1 mL/min

Gradient: H₂O-0.1 %HCOOH /ACN (100:0)— 30min— (0: 100)— 10min— (0:100) Sample dissolved approx. 1 mg/mL in ACN Method F

Column: Gemini C18 30 x 4,6 mm 3um

Temperature: 40 °C

Flow: 1.5 mL/min

Gradient H₂O-0.1 %HCOOH / ACN (95:5)— 0.5min— (95:5)— 8.5min - (0:100)—

1 min— (0:100)

Sample dissolved approx. 1 mg/ml_ in ACN

Synthesis of Intermediates

Intermediate 1 : (ft)-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 (f?)-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 °C overnight. The solvent was evaporated, the residue was dissolved in DCM and it was washed with 1 N NaOH, dried over MgS0₄, filtered and concentrated to dryness. The crude product (7.74 g) was slurried in a mixture of methylcyclohexane-toluene (3:1 v/v, 22 mL) and heated at 60 °C 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 obtain the title compound (2.68 g, 36% yield).

Step 2. (/?)-3-(2-Bromophenoxy)-A/-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) under a N₂ atmosphere, potassium tert- butoxide (0.6 g, 5.3 mmol) was added and the reaction mixture was heated at 60 °C for 8 h. It was then cooled to r.t. and water was added. The aqueous phase was extracted twice with EtOAc. The combined organic phases were dried over MgS0₄, 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_), under a N₂ atmosphere, DIPEA (0.58 ml_, 3.3 mml) and a solution of 4-nitrophenyl (2-(trimethylsilyl)ethyl) carbonate (0.95 g, 3.3 mmol) in DCM (1.5 mL) were added. After stirring at r.t. overnight, NaHCOs sat. solution was added and it was extracted twice with DCM. The combined organic phases were washed with 2 N NaOH solution, dried over MgS0₄, 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 2-4 using suitable starting materials:

Intermediate 5: 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 °C, DIAD (11.5 mL, 58.3 mmol) was added dropwise. After stirring 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 give 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 mol) in toluene (40 mL), cooled at 0 °C, DIBALH (25 wt% solution in toluene, 13.5 mL, 20.2 mmol) was added dropwise and the reaction was stirred at 0-5 °C for 4 h. Then, 10% aq. HCI 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 Na₂S0₄ and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (4 g, 38% yield).

This method was used for the preparation of Intermediate 6 using suitable starting materials:

(1 ) 1 M DIBALH in DCM was used in Step 2 Intermediate 7. Lithium 2-(3-chloro-1-(thiophen-2-yl)propoxy)benzoate

Step 1. Methyl 2-(3-chloro-1-(thiophen-2-yl)propoxy)benzoate: To a solution of 3- chloro-1-(thiophen-2-yl)propan-1-ol (2 g, 11.3 mmol), tributylphosphine (3.4 mL, 13.6 mmol) and methyl 2-hydroxybenzoate (1.45 mL, 11.3 mmol) in dry THF (20 mL), ADDP (3.4 g, 13.6 mmol) was added. The mixture was stirred at r.t. overnight. The suspension was filtered through a pad of Celite, washed with THF, and the filtrate was concentrated under vacuum. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (1.27 g, 36% yield).

Step 2. Title compound: A solution of the compound obtained in Step 1 (1.05 g, 3.4 mmol) in THF (17 mL) and 1 M LiOH solution (17 mL, 17 mmol) was heated at 50 °C overnight. The solvent was evaporated, toluene was added and it was concentrated again to dryness to remove residual water. The crude product was used in the next step without further purification (1.76 g, quantitative).

Intermediate 8. terf-Butyl (3-(2-bromophenoxy)-3-(thiophen-2- yl)propyl)(methyl)carbamate

Step 1. 2-(1-(2-Bromophenoxy)-3-chloropropyl)thiophene: Following the experimental procedure described in Step 1 of Intermediate 7, but using 2-bromophenol instead of methyl 2-hydroxybenzoate, the title compound was obtained and used without further purification (3.85 g, quant yield). Step 2. 3-(2-Bromophenoxy)-A/-methyl-3-(thiophen-2-yl)propan-1 -amine: In a sealed tube, a mixture of the product obtained in Step 1 (3.75 g, 1 1.32 mmol) and methylamine (33 wt% in EtOH, 30 mL, 226 mmol) was heated at 100 °C overnight. Then, it was concentrated to dryness and the crude was used in the next step without further purification (3.72 g, quant yield).

Step 3. Title compound: To a solution of the product obtained in Step 2 (3.7 g, 1 1 .32 mmol) in ferf-butanol (10 mL), 2 M NaOH solution (10 mL) and di-te/Y-butyl dicarbonate (2.5 g, 1 1.3 mmol) were added and the reaction mixture was stirred at r.t. overnight. Brine and DCM were added, the phases were separated and the aqueous layer was extracted with DCM. The combined organic phases were washed with brine, dried over MgS0₄, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (1.34 g, 28% yield for the 3 steps).

Intermediate 9. Lithium 2-(3-(methyl((2-(trimethylsilyl)ethoxy)carbonyl)amino)-1 - (thiophen-2-yl)propoxy)benzoate

Step 1 . Methyl 2-(3-(benzyl(methyl)amino)-1 -(thiophen-2-yl)propoxy)benzoate: Following the experimental procedure described in Step 1 of Intermediate 7, starting from 3-(benzyl(methyl)amino)-1 -(thiophen-2-yl)propan-1-ol and methyl 2- hydroxybenzoate, the title compound was obtained (195 mg, 43% yield).

Step 2. Methyl 2-(3-(methyl((2-(trimethylsilyl)ethoxy)carbonyl)amino)-1-(thiophen-2- yl)propoxy)benzoate: To a solution of 2-(trimethylsilyl)ethanol (0.21 mL, 1.5 mmol) and K₂C0₃ (0.42 g, 3 mmol) in toluene (2 mL) at 0 °C, a solution of triphosgene (146 mg, 0.49 mmol) in toluene (1 mL) was added dropwise. The mixture was stirred at r.t. for 1 h and then cooled to 0 °C. To this mixture, a solution of the compound obtained in Step 1 (195 mg, 0.49 mmol) in toluene (2 mL) was added at 0 °C and the resultant mixture was stirred at r.t. overnight. The reaction mixture was poured into NaHCC>3 sat. sol. and it was extracted twice with EtOAc. The combined organic extracts were dried over MgS0₄, filtered and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (190 mg, 85% yield).

Step 3. Title compound: Following the experimental procedure described in Step 2 of Intermediate 7, starting from the product obtained in Step 2, the title compound was obtained as a crude product that was purified by eluting through a C18-cartridge, to give the title compound (49 mg, 26% yield).

Intermediate 10. tert-Butyl (3-(2-bromophenoxy)-3-phenylpropyl)(methyl)carbamate:

In a sealed tube, a mixture of terf-butyl (3-chloro-3-phenylpropyl)(methyl)carbamate (4 g, 14.1 mmol), K₂CO₃ (5.84 g, 42.3 mmol), Kl (234 mg, 1.41 mmol) and 2-bromophenol (2.4 g, 14.1 mmol) in ACN (92 mL) was heated at 60 °C overnight. Water was added to the reaction mixture, and it was extracted with EtOAc. The combined organic extracts were dried over MgS0₄, filtered and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (2.36 g, 40% yield).

This method was used for the preparation of Intermediate 1 1 using suitable starting materials:

Intermediate 12. 2-(3-((tert-Butoxycarbonyl)(methyl)amino)-1-phenylpropoxy)benzoic acid

Step 1. Methyl 2-(3-((tert-butoxycarbonyl)(methyl)amino)-1-phenylpropoxy)benzoate: Following the experimental procedure described in Intermediate 10, but using methyl 2-hydroxybenzoate instead of 2-bromophenol, the title compound was obtained (1.48 g, 63% yield).

Step 2. Title compound: To a solution of the compound obtained in Step 1 (1.48 g, 3.7 mmol) in a mixture of THF:water (1 :1 , 15 ml_), lithium hydroxide monohydrate (1.2 g, 30 mmol) was added and the reaction mixture was heated at 50 °C overnight. The solvent was concentrated, pH was adjusted to 3 with 6 M HCI and it was extracted with EtOAc. The combined organic extracts were dried over MgS0₄, filtered and concentrated to dryness to afford the title compound (1.1g, 78% yield).

Intermediate 13. ferf-Butyl (3-((2-bromobenzyl)oxy)-3-phenylpropyl)(methyl)carbamate

To a solution of tert-butyl (3-hydroxy-3-phenylpropyl)(methyl)carbamate (2 g, 7.5 mmol) and tetrabutylammonium iodide (2.8 g, 7.5 mmol) in DMF (10 ml_), cooled at 0 °C, NaH (60% dispersion in mineral oil, 603 mg, 15 mmol) was added portionwise under a N₂ atmosphere. The reaction was stirred at 0 °C for 30 min and then a solution of 1-bromo- 2-(bromomethyl)benzene (1.8 g, 7.5 mmol) in DMF (4 mL) was added. The reaction mixture was stirred at r.t. overnight. Water and EtOAc were added, the phases were separated and the aqueous phase was extracted with EtOAc. The combined organic extracts were washed with water and brine, dried over MgSCV filtered and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (2.34 g, 71 % yield).

Intermediate 14. te/f-Butyl (3-(2-aminophenoxy)-3-phenylpropyl)(methyl)carbamate

Step 1. tert-Butyl methyl(3-(2-nitrophenoxy)-3-phenylpropyl)carbamate: Following the experimental procedure described in Step 1 of Intermediate 5, starting from ferf-butyl (3-hydroxy-3-phenylpropyl)(methyl)carbamate and 2-nitrophenol, the title compound was obtained (1.55 g, 63% yield).

Step 2. Title compound: To a solution of the compound obtained in Step 1 (1.55 g, 4 mmol) in a mixture of EtOH:water (4:1 , 33 ml_), iron (2.2 g, 40 mmol) and ammonium chloride (107 mg, 2 mmol) were added. The mixture was heated at reflux temperature for 4 h. It was allowed to cool down and the suspension was filtered through a pad of Celite, washed with EtOH and concentrated to dryness to render the title compound that was used without further purification (1.24 g, 87% yield).

Intermediate 15. (/?)-2-(Trimethylsilyl)ethyl (3-(2-bromophenoxy)-3-(thiophen-3- yl)propyl)(methyl)carbamate

Following the experimental procedure described for the preparation of Intermediate 1 , using (f?)-3-chloro-1-(thiophen-3-yl)propan-1-ol and methylamine as starting materials, the title compound was obtained. Intermediate 16: (/?)-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 and the tube was inertized with argon. Then, a solution of Intermediate 1 (0.7 g, 1.45 mmol) in 1 ,4-dioxane (18 ml_) was added and the reaction was heated at 110 °C for 4 h under an argon atmosphere. The reaction mixture was filtered through a pad of Celite, that was washed with EtOAc. The filtrate was washed with brine, dried over MgS0₄, 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 Os0₄ (4 wt% aq. sol., 0.75 mL, 0.118 mmol) was added. It was stirred at r.t. for 10 min. and then Nal0₄ (573 mg, 2.68 mmol) was added and the reaction mixture was stirred at r.t. for 15 min. The solvent was evaporated and the aqueous phase was extracted with EtOAc. The combined organic extracts were dried over MgS0₄, filtered and concentrated to dryness to afford the title compound (448 mg, 93% yield).

This method was used for the preparation of Intermediates 17-19 using suitable starting materials:

Synthesis of Examples

General Deprotection Methods Method 1. Boc deprotection with TMSI. To a solution of the N- Boc protected compound

(1 mmol) in dry ACN (45 mL), TMSI (2 mmol) was added dropwise. After stirring for 15 min at r.t. , NaHC0₃ sat. solution and DCM were added and the mixture was stirred for additional 10 minutes. The phases were separated, the organic phase was dried over MgS0₄ and concentrated to dryness, to afford the crude compound, which was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1 :4).

Method 2. Boc deprotection with TFA. A solution of the A/-Boc protected compound (1 mmol) in a mixture of DCM (15 mL) and TFA (10 mmol) was stirred at r.t. until full conversion was achieved. The volatiles were evaporated and the residue was re- dissolved in DCM and washed with 1 M NaOH solution and brine, dried over MgS0₄ and concentrated. The crude compound was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1 :4). Method 3. Boc deprotection with HCI. To a solution of the A/-Boc protected compound (1 mmol) in dioxane (10 mL), HCI (4 N solution in dioxane, 10 mmol) was added under a N₂ atmosphere. The reaction was stirred at r.t. overnight. The solvent was evaporated and the residue was purified by eluting through an acidic ion exchange resin cartridge (SCX), to give the desired compound, which was further purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1 :4).

Method 4 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 MgS0₄ and concentrated. The crude compound was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1 :4).

Method 5. 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 °C for 1 h. The solvent was concentrated to dryness and the crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1 :4).

Example 1 : 2-(3-(Methylamino)-1-phenylpropoxy)-/V-(thiophen-2-ylmethyl)aniline

Step 1. terf-Butyl methyl(3-phenyl-3-(2-((thiophen-2- ylmethyl)amino)phenoxy)propyl)carbamate: In a sealed tube, a mixture of Intermediate 10 (100 mg, 0.238 mmol), thiophen-2-ylmethanamine (50 mg, 0.442 mmol), Pd2(dba)3 (22 mg, 0.024 mmol), BINAP (29 mg, 0.048 mmol) and sodium terf-butoxide (67 mg, 0.714 mmol) in dry toluene (4 ml_) was heated at 120 °C overnight under an argon atmosphere. The reaction mixture was filtered through a pad of Celite, washed with EtOAc and the filtrate was concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (90 mg, 83% yield).

Step 2. Title compound: Starting from the compound obtained in Step 1 (90 mg, 0.2 mmol) and following General Deprotection method 2, the title compound was obtained (48 mg, 68% yield).

HPLC retention time (method B): 4.44 min; MS: 353.1 (M+H).

This method was used for the preparation of Examples 2-7 using suitable starting materials:

Example 8: /V-Methyl-3-phenyl-3-(2-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2- yl)phenoxy)propan-1 -amine

Step 1. te/t-Butyl 2-(4,4,5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)-6,7- dihydrothieno[3,2-c]pyridine-5(4/-/)-carboxylate: To a solution of tert-butyl 2-bromo-6,7- dihydrothieno[3,2-c]pyridine-5(4/-/)-carboxylate (0.3 g, 0.943 mmol) in dry THF (7 mL), cooled at -78 °C, butyllithium (1.6 M solution in hexanes, 0.71 mL, 1.31 mmol) was added dropwise under a N_å atmosphere and the mixture was stirred at -78 °C for 30 min. Then, a solution of 2-isopropoxy-4,4,5,5-tetramethyl-1 ,3,2-dioxaborolane (0.29 mL, 1.41 mmol) in dry THF (2 ml_) was added dropwise. The reaction mixture was stirred at -78 °C for 20 min, then left to warm to r.t. gradually. NH₄CI sat. solution was added and the mixture extracted with EtOAc. The combined organic extracts were washed with brine, dried over MgS0₄ and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (78 mg, 22% yield).

Step 2. tert-Butyl 2-(2-(3-((tert-butoxycarbonyl)(methyl)amino)-1 - phenylpropoxy)phenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4/-/)-carboxylate: In a sealed tube, a mixture of Intermediate 10 (86 mg, 0.205 mmol), the compound obtained in Step 1 (75 mg, 0.205 mmol), tetrakis(triphenylphosphine)palladium(0) (24 mg, 0.021 mmol) and K₂C0₃ (57 mg, 0.41 1 mmol) in a mixture of dioxane:water (15: 1 , 2.7 mL) was heated at 100 °C overnight under an argon atmosphere. The reaction mixture was filtered through a pad of Celite, washed with EtOAc and the filtrate was concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (44 mg, 37% yield).

Step 3. Title compound: Starting from the compound obtained in Step 2 (44 mg, 0.076 mmol) and following General Deprotection method 2, the title compound was obtained (12 mg, 42% yield).

HPLC retention time (method B): 3.53 min; MS: 379.1 (M+H).

Example 9. /\/-(2-(3-(Methylamino)-1 -(thiophen-2-yl)propoxy)phenyl)-2- phenylacetamide

Step 1. 2-(Trimethylsilyl)ethyl methyl(3-(2-(2-phenylacetamido)phenoxy)-3-(thiophen- 2-yl)propyl)carbamate: In a sealed tube, a mixture of Intermediate 4 (150 mg, 0.319 mmol), 2-phenylacetamide (56 mg, 0.414 mmol), /V.A^-dimethylethane-l ,2-diamine (10 mί, 0.096 mmol), copper (I) iodide (18 mg, 0.096 mmol) and potassium phosphate (135 mg, 0.638 mmol) in 1 ,4-dioxane (4.5 ml_) was heated at 120 °C overnight under an argon atmosphere. Additional A^A^-dimethylethane-l , 2-diamine (10 mI_, 0.096 mmol) and copper (I) iodide (18 mg, 0.096 mmol) were added and the reaction mixture was again heated at 120 °C overnight. It was filtered through a pad of Celite, washed with DCM and the filtrate was concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (130 mg, 78% yield).

Step 2. Title compound: Starting from the compound obtained in Step 1 (130 mg, 0.248 mmol) and following the General Deprotection method 5, the title compound was obtained (83 mg, 88% yield).

HPLC retention time (method B): 3.84 min; MS: 381 .1 (M+H).

This method was used for the preparation of Examples 10-13 using suitable starting materials:

Example 14: /V-Methyl-3-(2-(2-(methyl(phenethyl)amino)ethyl)phenoxy)-3-(thiophen- 2-yl)propan-1 -amine

Step 1. /V-(2-(3-Chloro-1-(thiophen-2-yl)propoxy)phenethyl)-A/-methyl-2- phenylethanamine: A solution of Intermediate 6 (250 mg, 0.85 mmol), A/-methyl-2- phenylethanamine (0.12 ml_, 0.85 mmol) and AcOH (4.8 pL, 0.085 mmol) in DCE (3.54 mL) was stirred for 2 h under a N₂ atmosphere. Then, sodium triacetoxyborohydride (270 mg, 1.27 mmol) was added and the reaction mixture was stirred at r.t. overnight. NaHCOs sat. solution was added and the mixture extracted with DCM. The combined organic extracts were washed with brine, dried over MgS0₄ 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 (248 mg, 70% yield).

Step 2. Title compound: A solution of the compound obtained in Step 1 (103 mg, 0.25 mmol) and methylamine (33 wt% solution in EtOH, 1.6 mL, 12.44 mmol) was heated in a sealed tube at 50 °C for 20 h. The solvent was evaporated to dryness, the residue was dissolved in DCM and it was washed with 1 N NaOH, dried over MgS0₄ 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 (63 mg, 62% yield).

HPLC retention time (method C): 5.39 min; MS: 408.9 (M+H).

This method was used for the preparation of Examples 15-26 using suitable starting materials:

Example 27: A/-Methyl-3-phenyl-3-(2-(((2-(4-(pyridin-2-yl)tetrahydro-2H-pyran-4- yl)ethyl)amino)methyl)phenoxy)propan-1 -amine

Step 1. tert- Butyl methyl(3-phenyl-3-(2-(((2-(4-(pyridin-2-yl)tetrahydro-2/-/-pyran-4- yl)ethyl)amino)methyl)phenoxy)propyl)carbamate: Following the experimental procedure described in Step 1 of Example 14, starting from Intermediate 1 1 (100 mg, 0.27 mmol) and 2-(4-(pyridin-2-yl)tetrahydro-2H-pyran-4-yl)ethanamine (55 mg, 0.27 mmol), the title compound was obtained (83 mg, 54% yield. Step 2. Title compound: Starting from the compound obtained in Step 1 (83 mg, 0.15 mmol) and following General Deprotection method 2, the title compound was obtained (20 mg, 30% yield).

HPLC retention time (method B): 3.60 min; MS: 460.3 (M+H). This method was used for the preparation of Examples 28-32 using suitable starting materials:

Example 33: /V-(2-(3-(Methylamino)-1 -phenylpropoxy)benzyl)pyridin-4-amine

Step 1. te/t-Butyl methyl(3-phenyl-3-(2-((pyridin-4- ylamino)methyl)phenoxy)propyl)carbamate: A solution of Intermediate 11 (100 mg, 0.25 mmol) and pyridine-4-amine (23 mg, 0.25 mmol) in toluene (0.8 mL) was heated at 120 °C for 48 h. The solvent was concentrated, the residue was dissolved in MeOH (0.8 mL) and NaBhL (14 mg, 0.374 mmol) was added. The mixture was stirred for 4 h at r.t. and the solvent was evaporated. The crude product was diluted with water and DCM, the phases were separated and the aqueous layer was extracted with DCM. The combined organic extracts were dried over MgS0₄, 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 (31 mg, 28% yield).

Step 2. Title compound: Starting from the compound obtained in Step 1 (30 mg, 0.07 mmol) and following General Deprotection method 2, the title compound was obtained (19 mg, 83% yield).

HPLC retention time (method D): 10.34 min; MS: 348.2 (M+H). This method was used for the preparation of Example 34 using suitable starting materials:

Example 35: 2-(3-(Methylamino)-1 -(thiophen-2-yl)propoxy)-/\/-phenethylbenzamide

Step 1. 2-(3-Chloro-1 -(thiophen-2-yl)propoxy)-A/-phenethylbenzamide: To a solution of Intermediate 7 (235 mg, 57 wt%, 0.44 mmol) and 2-phenylethanamine (56 mI_, 0.44 mmol) in dry DMF (7 ml_), DIPEA (345 mI_, 2.0 mmol) and HATU (201 mg, 0.53 mmol) were added. The reaction mixture was stirred at r.t. overnight. NaHCOs sat. solution was added and the mixture extracted with EtOAc. The combined organic extracts were washed with water and brine, dried over MgS0₄ and concentrated to dryness. The crude product was used without further purification (188 mg, quant yield).

Step 2. Title compound: Following the experimental procedure described in Step 2 of Example 14, starting from the product obtained in Step 1 (188 mg, 0.44 mmol), the title compound was obtained (15 mg, 8% yield).

HPLC retention time (method C): 4.5 min; MS: 395.0 (M+H). Example 36: A/-Benzyl-2-(3-(methylamino)-1 -(thiophen-2-yl)propoxy)benzamide

Step 1. 2-(Trimethylsilyl)ethyl (3-(2-(benzylcarbamoyl)phenoxy)-3-(thiophen-2- yl)propyl)(methyl)carbamate: Following the procedure described in Step 1 of Example 35, starting from Intermediate 9 (49 mg, 0.1 1 mmol) and benzylamine (12 mI_, 0.1 1 mmol), the title compound was obtained (28 mg, 48% yield).

Step 2. Title compound: Following the General Deprotection method 5, starting from the compound obtained in Step 1 (28 mg, 0.053 mmol), the title compound was obtained (5.7 mg, 28% yield).

HPLC retention time (method B): 3.74 min; MS: 381 .1 (M+H).

This method was used for the preparation of Examples 37-50 using suitable starting materials:

Example 51 : A/-(2-(3-(Methylamino)-1-phenylpropoxy)phenyl)-2-(thiophen-2- yl)acetamide

Step 1. terf-Butyl methyl(3-phenyl-3-(2-(2-(thiophen-2- yl)acetamido)phenoxy)propyl)carbamate: Following the experimental procedure described in Step 1 of Example 35, starting from Intermediate 14 (100 mg, 0.28 mmol) and 2-(thiophen-2-yl)acetic acid (40 mg, 0.28 mmol), the title compound was obtained (84 mg, 56% yield). Step 2. Title compound: Following the General Deprotection method 2, starting from the compound obtained in Step 1 (84 mg, 0.158 mmol) the title compound was obtained (20 mg, 33% yield).

HPLC retention time (method B): 3.86 min; MS: 381 .1 (M+H).

Example 52: 3-(Benzyl(methyl)amino)-/V-(2-(3-(methylamino)-1- phenylpropoxy)phenyl)propanamide

Step 1 . ferf-Butyl (3-(2-(3-chloropropanamido)phenoxy)-3- phenylpropyl)(methyl)carbamate: To a solution of Intermediate 14 (200 mg, 0.56 mmol) in ACN (5 mL) under a N₂ atmosphere, DIPEA (0.244 ml_, 1.4 mmol) and 3- chloropropanoyl chloride (64 mI_, 0.67 mmol) were added dropwise. The mixture was stirred for 1 h at r.t. and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (167 mg, 67% yield).

Step 2. tert- Butyl (3-(2-(3-(benzyl(methyl)amino)propanamido)phenoxy)-3- phenylpropyl)(methyl)carbamate: A solution of the product obtained in Step 1 (167 mg, 0.37 mmol) and A/-methyl-1 -phenylmethanamine (42 mI_, 0.33 mmol) in EtOH (1 .6 mL) was heated in a sealed tube at 60 ⁰ C overnight. The solvent was evaporated and the residue dissolved in EtOAc. The mixture was washed with 1 N NaOH solution and the organic phase was dried over MgS0₄ and concentrated to dryness. The crude product thus obtained was used without further purification (194 mg, overweight, quant yield assumed).

Step 3. Title compound: Following the General Deprotection method 2, starting from the compound obtained in Step 2 (70 mg, 0.131 mmol), the title compound was obtained (46 mg, 82% yield).

HPLC retention time (method B): 4.58 min; MS: 432.2 (M+H). This method was used for the preparation of Examples 53-55 using suitable starting materials:

Example 56. 3-(Benzyl(methyl)amino)-A/-methyl-/\/-(2-(3-(methylamino)-1 - phenylpropoxy)phenyl)propanamide

Step 1. tert-Butyl (3-(2-(3-(benzyl(methyl)amino)-/\/-methylpropanamido)phenoxy)-3- phenylpropyl)(methyl)carbamate: To a solution of the product obtained in Step 2 of Example 52 (70 mg, 0.131 mmol) in dry DMF (2 mL), cooled at 0 °C, NaH (60% dispersion in mineral oil, 10 mg, 0.26 mmol) was added under a N₂ atmosphere. The reaction mixture was stirred for 30 min at r.t., then iodomethane (8 pL, 0.131 mmol) was added and it was stirred at r.t. overnightAdditional NaH (60% dispersion in mineral oil, 5 mg, 0.13 mmol) was added at 0 °C and the mixture was stirred for 30 min at r.t.. Additional iodomethane (4 pL, 0.7 mmol) was added and the reaction was stirred at r.t. overnight. Water and EtOAc were added, the phases were separated and the aqueous layer was extracted with EtOAc. The combined organic extracts were dried over MgS0₄ and concentrated. The crude was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (45 mg, 63% yield).

Step 2. Title compound: Following the General Deprotection method 2, starting from the compound obtained in Step 1 (45 mg, 0.082 mmol), the title compound was obtained (1 1 mg, 30% yield).

HPLC retention time (method B): 4.47 min; MS: 446.3 (M+H).

Example 57. 4-(Dimethylamino)-A/-(2-(3-(methylamino)-1- phenylpropoxy)phenyl)nicotinamide

Step 1. tert- Butyl (3-(2-(4-chloronicotinamido)phenoxy)-3- phenylpropyl)(methyl)carbamate: Following the experimental procedure described in Step 1 of Example 35, starting from Intermediate 14 (150 mg, 0.42 mmol) and 4- chloronicotinic acid (66 mg, 0.42 mmol), the title compound was obtained (175 mg, 84% yield).

Step 2. terf-Butyl (3-(2-(4-(dimethylamino)nicotinamido)phenoxy)-3- phenylpropyl)(methyl)carbamate: A mixture of the product obtained in Step 1 (175 mg, 0.35 mmol) and dimethylamine (2 M solution in THF, 1.7 mL, 3.4 mmol) was heated in a sealed tube at 70 °C overnight. The reaction mixture was diluted with water and it was extracted with EtOAc. The combined organic extracts were washed with brine, dried over MgS0₄ and concentrated. The crude product thus obtained was used without further purification (135 mg, 75% yield). Step 3. Title compound: Following the General Deprotection method 1 , starting from the compound obtained in Step 2 (45 mg, 0.082 mmol), the title compound was obtained (22 mg, 55% yield).

HPLC retention time (method A): 3.59 min; MS: 405.2 (M+H).

Example 58. /V-(2-(3-(Methylamino)-1 -phenylpropoxy)phenyl)benzamide

Step 1. terf-Butyl (3-(2-benzamidophenoxy)-3-phenylpropyl)(methyl)carbamate: To a solution of Intermediate 14 (200 mg, 0.56 mmol) in THF (8 mL), under a N₂ atmosphere, DIPEA (0.147 mL, 0.84 mmol) and benzoyl chloride (92 mί, 0.78 mmol) were added dropwise and the mixture was stirred at r.t. overnight. It was concentrated to dryness and the residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (203 mg, 80% yield).

Step 2. Title compound: Following the General Deprotection method 2, starting from the compound obtained in Step 1 (100 mg, 0.22 mmol), the title compound was obtained (35 mg, 45% yield).

HPLC retention time (method A): 3.87 min; MS: 361.1 (M+H).

This method was used for the preparation of Examples 59-62 using suitable starting materials:

Example 63. A/-Benzyl-2-(3-(methylamino)-1-phenylpropoxy)aniline

Step 1. tert- Butyl (3-(2-(benzylamino)phenoxy)-3-phenylpropyl)(methyl)carbamate: Following the experimental procedure described in Step 1 of Example 14, starting from Intermediate 14 (160 mg, 045 mmol) and benzaldehyde (48 mΐ_, 0.53 mmol), the title compound was obtained (83 mg, 41% yield).

Step 2. Title compound: Following the General Deprotection method 2, starting from the compound obtained in Step 1 (83 mg, 0.18 mmol) the title compound was obtained (53 mg, 82% yield).

HPLC retention time (method A): 4.84 min; MS: 347.1 (M+H). This method was used for the preparation of Examples 64-65 using suitable starting materials:

Following the method described in Step 1 of Example 1 using suitable starting materials, followed by the General Deprotection method 5, Examples 66-68 were obtained:

Following the method described in Step 1 of Example 14 using suitable starting materials, followed by the General Deprotection method 5, Examples 69-76 were obtained:

Table of Examples with binding to the a₂d-1 Subunit of the voltage-gated calcium channel;

BIOLOGICAL ACTIVITY

Pharmacological study

Human a2d-1 subunit of Ca_v2.2 calcium channel assay Human a₂d-1 enriched membranes (2.5 pg) 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 mM pregabalin. The binding of the test compound was measured at five different concentrations. After 60 min incubation at 27 °C, 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-HCI, pH 7.4. Filter plates were dried at 60 °C for 1 hour and 30 mI of scintillation cocktail were added to each well before radioactivity reading. Readings were performed in a Trilux 1450 Microbeta radioactive counter (Perkin Elmer).

Results:

As this invention is aimed at providing a compound or a chemically related series of compounds which act as ligands of the a2d subunit of voltage-gated calcium channels it is a very preferred embodiment in which the compounds are selected which act as ligands of the a₂d subunit of voltage-gated calcium channels and especially compounds which have a binding expressed as Ki responding to the following scales:

Kί(a2d-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 the a2d-1 subunit of voltage-gated calcium channels expressed as Ki:

+ Kί(a₂d-1) >= 5000 nM

++ 500nM <= Kί(a₂d-1) <5000 nM

+++ Kί(a₂d-1) <500 nM All compounds prepared in the present application exhibit binding to the a2d-1 subunit of voltage-gated calcium channels, 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(0)[CH2]_q-,

[CH₂]pC(0)N(R_z)[CH2]_q-, -[CH₂]pN(Rz)C(0)[CH₂]_q- and -[CH₂]pN(Rz)[CH₂]_q-; R_a is selected from hydrogen, halogen, substituted or unsubstituted Ci_₆ alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

R_b 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, may form a substituted or unsubstituted cycloalkyl;

R_z 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(0)-Ci.₆ alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;

Yi is— C(RioRio )-; 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 Rio· may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

Y2 is— C(Rio Rio’ )-; wherein Rio· and R₁₀ are independently selected from hydrogen, substituted or unsubstituted Ci_-6 alkyl, substituted or unsubstituted C₂-6 alkenyl and substituted or unsubstituted C_2-6 alkynyl; alternatively, Rio- and R₁₀- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

n is 0 or 1 ;

R1 is selected from-NRsRs and -NRs C(0)R5; R₂ is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl,

R₃ 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 and substituted or unsubstituted alkylcycloalkyl;

R₃ is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-6 alkynyl;

R₄ and R₄ are independently selected from halogen, -R_4I , -OR_4I , -NO2, - NR_4I R_4I , -NR_4IC(0)R_4I , -NR_4IS(0)₂R_4I , -S(0)₂NR_4I R_4I , -NR_4iC(0)NR_4rR₄r, - SR_4I , -S(0)R_4I , -S(0)₂R_4I , -CN, haloalkyl, haloalkoxy, -C(0)0R_4i, - C(0)NR_4iR₄r, -OCH₂CH₂OR_4I , -NR_4IS(0)₂NR_4I R_4r and -C(CH₃)₂OR_4I ; wherein R_4I , R₄r and R₄r are independently selected from hydrogen, substituted or unsubstituted C_1.6 alkyl, substituted or unsubstituted C_2-6 alkenyl and substituted or unsubstituted C₂-e alkynyl;

Rs is selected from substituted or unsubstituted C_1-6 alkyl, substituted or unsubstituted C_2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylary! and substituted or unsubstituted alkylheteroaryl; R₅ is selected from hydrogen, substituted or unsubstituted Ci_-6 alkyl, substituted or unsubstituted C_2.e 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;

the following compounds are further excluded:

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 (G), (l^a), (l^a’), (l^b) or (l^b ),

281 (P,

wherein R₆ and Re are independently selected from hydrogen, halogen, - R21, -OR21, -NO2, -NR21R21', -NR₂₁C(0)R₂₁ , -NR2iS(0)2R2v, -S(0)2NR2I R21 , - NR_2iC(0)NR₂rR2i , -SR21 , -S(0)R_2I , -S(0)₂R₂₁ , -CN, haloalkyl, haloalkoxy, -OCH2CH2OR21, NR2iS(0)2N

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.

4. Compound according to anyone of claims 1 to 3 wherein Ri is a substituted or unsubstituted group selected from -N(CH3)(CH2CH3), N(CH3)(CH2CH20CH3), -N(CH3)(CH2CH2-CN), -N(CH3)(cyclopropyl), -NH- cyclohexyl, -NH-pyridinyl, -NH-phenyl, -NH-CH3-pyridinyl, -NH-CH2-phenyl, - NH-CH2-CH(N[CH3]2)-phenyl, -NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2- thienyl, -NH-CH2-dihydroindenyl, -N(CH3)2, -N(CH3)(isobutyl), -N(CH3)(CH2- phenyl), -N(CH3)(CH2CH2-phenyl), -N(CH3)(CH2-thienyl), -NHC(0)-pyridinyl, -NHC(0)-isopropyl, -NHC(0)-phenyl, -NHC(0)-CH2-thienyl and -NHC(O)- CH2-phenyl.

5. Compound according to any one of claims 1 to 3 wherein Rs is a substituted or unsubstituted group selected from pyridinyl, phenyl, -CH2-pyridinyl, CH2CH3, CH2CH20CH3, CH2CH2-CN, benzyl, -CH2CH(N[CH3]2)-phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2- thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, cyclopropyl and cyclohexyl;

6. Compound according to anyone of claims 1 to 5 wherein X is a bond or a substituted or unsubstituted group selected from bond, -CH2-, -CH2CH2-, - C(O)-, -C(0)NH-, -C(0)NHCH2-,-C(0)NHCH2CH2-, -NHC(O)-, -NHC(0)CH2-, -NHC(0)CH2CH2-, -N(CH3)C(0)CH2CH2-, -CH2NH-, -NHCH2-,

NHCH2CH2-, -N(CH3)CH2CH2- and -CH2NHCH2-;.

7. Compound according to anyone of claims 1 to 6 wherein

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

8. Compound according to anyone of claims 1 to 7 wherein q is 0, 1 , 2, 3, 4 or 5; preferably 0, 1 or 2.

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

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

1 1. Compounds selected from

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

a) wherein -X is a bond and R₁ represents -NR₅R₅ Y₁ and Y2 both represent — CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (Ha)

wherein Q represents chloro, bromo, iodo or triflate, A represents -NR3R3· and

R₂, R_3, R₃·_, R₄, R₄ and n have the meanings as defined in the description, with an amine of formula III-2

^R- NH

i

Rs

in-2 wherein R5 and R5 have the meanings as defined in the description; or

b) wherein -X is a bond and Ri represents -NR₅ C(0)R5 , Yi and Y₂ both represent -CH₂- and wherein R₂, R₃, R_3\ R₄, R₄ and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (lla)

lla wherein Q represents chloro, bromo, iodo or triflate, A represents -NR₃R3' and R₂, R_3, R₃·_, R₄, R_4' and n have the meanings as defined in the description, with an amine of formula MI-3

III-3 wherein R5 and R5 have the meanings as defined in the description;

or

c) wherein -X-R1 represents -[CH₂]_P-NR₅R5', Y1 and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (lib)

wherein r is 1 , 2, 3 or 4, A represents -NR₃R_3' and R₂, R_3, R3·. R₄, R₄ and n have the meanings as defined in the description, with an amine of formula III-2

^R-NH

R_s'

111-2 wherein R₅ and R₅ have the meanings as defined in the description;

or

d) wherein -X-R₁ represents -[CH₂]_P-NR₅R₅ , Y1 and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (Ha)

lla wherein Q represents chloro, bromo, iodo or triflate, A represents -NR₃R_3' and R₂, R_3, R_3', R_4I R₄ and n have the meanings as defined in the description, with an organometallic reagent of formula III-4

MI-4 wherein R₅ and R₅ and p have the meanings as defined in the description, and M represents a suitable organometallic group, preferably a boron or zinc reagent;

or

e) wherein -X is a bond and Ri represents -NR₅R_5' Y₁ and Y₂ both represent -CH₂- and wherein R₂, R₃, R₃ , R₄, R₄ , Rs, Rs and n have the meanings as defined in the description, said process comprises reacting a compound of

Formula (lie),

lie wherein A represents -NR₃R₃ and R_å, R₃, R₃ , R₄, R₄· and n have the meanings as defined in the description, with an aldehyde of formula III-5 under the reductive amination

R5-CHO

III-5 or with an alkylating agent of formula MI-6, under conventional alkylation conditions

Rs-LG

III-6 wherein Rs has the meanings as defined in the description and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or

f) wherein -X is a bond and Ri represents -NR_5'C(0)Rs , Yi and Y₂ both represent -CH₂-, and wherein R₂, R3, R3 , R₄, R₄ , Rs, Rs and n have the meanings as defined in the description, said process comprises reacting a compound of Formula (le)

le wherein A represents -NR₃R_3' and R₂, R3, R3 , R₄, R₄ , Rs and n have the meanings as defined in the description, with an alkylating agent of formula III-6’

R5 -LG

III-6' wherein Rs has the meanings as defined in the description but different from hydrogen, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or g) wherein -X is -[CH₂]p- and Ri represents -C(0)NRsRs , Yi and Y₂ both represent -CH₂-, and wherein R₂, R₃, R₃ , R₄, R₄ , Rs, Rs and n and p have the meanings as defined in the description, said process comprises reacting a compound of Formula (lid)

III-2 wherein Rs and Rs have the meanings as defined in the description;

or

h) wherein n is 0, Yi and Y₂ both represent -CH₂- and wherein Ri, R₂, R₃, R₃ ,

R₄, R₄ and X have the meanings as defined in the description, said process comprises reacting a compound of Formula (Via)

VII wherein Z represents OH or a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, A represents -NR₃R_3' and R₂, R3 and R3·, have the meaning as defined in the description;

or

J) wherein n is 1 , Y1 and Y₂ both represent -CH₂- and wherein R1, R₂, R₃, R₃ , R₄, R and X have the meaning as defined in the description, said process comprises reacting a compound of Formula (Via)

with a compound of formula VII

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 or a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, and wherein R₄, R₄ have the meanings as defined in the description, A represents -NR3R3 and R2, R3 and R3 , have the meaning as defined in the description.

13. Use of a compound of Formula (II),

II

wherein A is LG or NR₃R₃ and R₂, R3, R3', R₄, R₄ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate, and Y represent suitable functional groups; or of a compound of Formula (lla),

lla

wherein A is LG or NR₃R₃ and R₂, R₃, R3 , R₄, R₄ and n have the meaning 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;

or of a compound of Formula (lib),

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R_4' and n and r have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (lie),

lie

wherein A is LG or NR₃R₃ and R₂, R₃, R_3', R₄, R_4' and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (lid),

wherein A is LG or NR₃R₃ and R₂, R₃, R₃ , R₄, R₄ and n and p have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (III),

wherein R₁ has the meaning as defined in the description and W represent suitable functional groups; or of a compound of Formula (III-2),

wherein R5 and Rs’ have the meaning as defined in the description;

or of a compound of Formula

III-3

wherein R5 and R5’ have the meaning as defined in the description; or of a compound of Formula

III-4

wherein p, R5 and R5’ have the meaning as defined in the description, and M represents a suitable organometallic group, preferably a boron or zinc reagent; or of a compound of Formula (MI-5)

R_S-CHO

MI-5

wherein R5 has the meaning as defined in the description;

or of a compound of Formula (MI-5)

R₅-LG

iii-b

or of a compound of Formula (MI-5)

R5-LG

III-6' wherein Rs has the meaning as defined in the description, and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (IVb),

IVb wherein A=LG

wherein A is LG, R₂, R₄, R₄·, Rs, Rs’ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (IVc),

c w ere n

wherein A is LG, R₂, R₄, R₄ , R₅, Rs’ and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (IVd),

IVd wherein A=LG

or of a compound of Formula (IVe),

IVe wherein A=LG

wherein A is LG, R₂, R₄, R₄ , Rs and n have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (IVf),

IVf wherein A=LG

or of a compound of Formula (IVg),

IVg wherein A=LG

or of a compound of Formula (IVh),

IVh wherein A=LG wherein A is LG, Ri, R₂, R₄ and R₄ have the meaning as defined in the description, LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate;

or of a compound of Formula (V)

HNR3R3.

V

wherein R₃ and R₃ have the meaning as defined in the description;

or of a compound of Formula

VI

wherein G represents OH, halogen or a leaving group, R₁, R₄ and R₄ and n have the meaning as defined in the description;

or of a compound of Formula

Via

or of a compound of Formula

Vlb

or of a compound of Formula

wherein Z represents OH or a leaving group, A is LG or NR3R3 , R2, R3 and R3 have the meaning as defined in the description and LG represents a leaving group such as chloro, bromo, iodo, mesylate, tosylate, nosylate or triflate; or of a compound of Formula

Y represents a suitable functional group, G represents OH, halogen or a leaving group, R₄ and R and n have the meaning as defined in the description, for the preparation of compounds of Formula (I) as defined in any one of claims 1 to 10.

14. A pharmaceutical composition which comprises a compound of Formula (I) as defined in any one of claims 1 to 10, or which comprises a compound as defined in claim 1 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

15. A compound of Formula (I) as defined in any one of claims 1 to 10, or a compound as defined in claim 11 , for use as a medicament.

16. A compound of Formula (I) as defined in any one of claims 1 to 10, or a compound as defined in claim 11 , 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.