Novel derivatives for treatment of TRPM3-mediated disorders
By providing a novel compound that acts as a TRPM3 antagonist, it solves the problem of the lack of effective TRPM3 antagonists in the prior art, and achieves effective treatment of TRPM3-mediated disorders, especially pain, epilepsy and inflammatory hypersensitivity reaction.
Patent Information
- Application Number
- CN202380047494.6
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2022-05-25
- Filing Date
- 2023-05-25
- Publication Date
- 2025-02-11
AI Technical Summary
The prior art lacks effective TRPM3 antagonists to prevent or treat TRPM3-mediated conditions such as pain, epilepsy, and inflammatory hypersensitivity reactions.
A novel compound is provided as an antagonist of TRPM3 for modulating TRPM3-mediated disorders. The structure of the compound includes a specific heterocyclic system and substituent combination, which is capable of effectively antagonizing the TRPM3 channel.
The compound is able to effectively antagonize the TRPM3 channel, providing a new therapeutic approach to prevent or treat TRPM3-mediated conditions, especially pain, epilepsy and inflammatory hypersensitivity, and has good pharmacokinetic properties.
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Abstract
Description
Technical Field
[0001] The present invention relates to compounds that can be used to prevent or treat TRPM3-mediated disorders, more particularly disorders selected from pain, epilepsy and inflammatory hypersensitivity reactions. The present invention also relates to a method for preventing or treating said TRPM3-mediated disorders. Background Art
[0002] The TRP superfamily consists of proteins with six transmembrane domains (6TM) that assemble as homo- or heterotetramers to form cation-permeable ion channels. The name TRP is derived from the Drosophila trp (transient receptor potential) mutant, which characterizes Drosophila photoreceptors as having a transient receptor potential in response to sustained light. Over the past 15 years, trp-related channels have been identified in yeast, worms, insects, fish, and mammals, including 27 TRPs in humans. Based on sequence homology, TRP channels can be divided into seven subfamilies: TRPC, TRPV, TRPM, TRPA, TRPP, TRPML, and TRPN.
[0003] Members of the TRP superfamily are likely expressed in all mammalian organs and cell types, and great progress has been made in recent years in understanding their physiological roles. The tailored selectivity of certain TRP channels enables them to be expressed in the presence of Ca 2+ Mg 2+ The TRPs play a key role in the cellular uptake and / or transepithelial transport of trace metal ions. In addition, the sensitivity of TRP channels to a wide range of chemical and physical stimuli allows them to act as specialized biosensors, participating in processes from vision to taste and touch. Specifically, several members of the TRP superfamily show very high sensitivity to temperature. These so-called thermal TRPs are highly expressed in sensory neurons and / or skin keratinocytes, where they act as primary thermal sensors for detecting harmless and harmful (painful) temperatures.
[0004] It is becoming increasingly clear that TRP channel dysfunction is directly involved in the cause of disease of various hereditary and acquired diseases. In fact, both loss of function and gain of function mutations in TRP channel genes have been identified as direct causes of hereditary diseases, including brachyolmia, hypomagnesemia with secondary hypocalcemia, polycystic kidney disease, mucopolysaccharidosis type IV, and familial focal segmental glomerulosclerosis. In addition, TRP channel function / dysfunction has been directly related to a wide range of pathological conditions, including chronic pain, hypertension, cancer, epilepsy, and neurodegenerative disorders.
[0005] TRPM3 (transient receptor potential M-type 3) represents a promising pharmacological target. TRPM3 is expressed in a large subset of small-diameter sensory neurons from the dorsal root and trigeminal ganglion and is involved in heat sensing. The neurosteroid pregnenolone sulfate is an effective known activator of TRPM3 (Wagner et al., 2008). The neurosteroid pregnenolone sulfate induces pain in wild-type mice, but not in TRPM3 knockout mice. It has also been recently shown that CFA-induced inflammation and inflammatory pain are eliminated in TRPM3 knockout mice. Therefore, TRPM3 antagonists can be used as analgesics to combat pain, such as inflammatory pain (Vriens J. et al., Neuron, May 2011). TRPM3 is also expressed in many other tissues including the brain; reports show that two mutations in TRPM3 are associated with developmental and epileptic encephalopathy (Zhao, S. et al., Channels (Austin). 2021).
[0006] Some TRPM3 antagonists are known, but none of them point to the compounds of the present invention (Straub I et al., Mol Pharmacol, November 2013). For example, liquiritigenin, a putative TRPM3 blocker, has been described as reducing mechanical hyperalgesia and cold hyperalgesia in a rat pain model (Chen L et al., Scientific Reports, July 2014). There is still a huge medical need for novel, alternative and / or better therapeutic agents for preventing or treating TRPM3-mediated conditions (such as pain and epilepsy), more specifically for pain, such as inflammatory pain or epilepsy (such as epileptic encephalopathy). There is a great need for therapeutic agents with good efficacy, low levels or no side effects (such as the impossibility of addiction, non-toxicity like opioids) and / or good or better pharmacokinetic or kinetic properties for certain types of pain.
[0007] The present invention provides a novel class of compounds that are antagonists of TRPM3 and are useful as modulators of TRPM3-mediated disorders. Summary of the Invention
[0008] The first aspect of the present invention provides a compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph
[0009]
[0010] in
[0011] R 1Indicates -F, -Cl, -Br, -I, -CN, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;
[0012] Q means -OR 2 or -NR 3 R 4 ;
[0013] R 2 Indicates -R Y5 ;
[0014] R 3 Indicates -OH or -R Y1 ;
[0015] R 4 Indicates -R Y2 or -S(=O)2R Y3 ;
[0016] or R 3 and R 4 together forming a 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0017] T represents -O-, and U represents -(CR 5 R 5 ') n -; or T represents -(CR 5 R 5 ') n -, and U represents -O-;
[0018] n is an integer selected from 1, 2, 3, 4 or 5;
[0019] R 5 and R 5 'Independently represent -R Y4 ;
[0020] R 6 、R 7and R 8 independently represent -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;
[0021] W stands for
[0022] 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted;
[0023] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0024] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0025] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0026] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted;
[0027] in
[0028] R W and R X Independently of each other, expressed independently in each case
[0029] -H;
[0030] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0031] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0032] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0033] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0034] R Y1 、R Y2 、R Y3 、R Y4 and R Y5 Independently of each other, expressed independently in each case
[0035] -H;
[0036] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0037] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0038] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0039] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0040] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0041] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0042] and wherein "mono- or polysubstituted" independently in each case means substituted by one or more substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-C 1-6 -alkyl, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -C(=O)-NH(OH), -C 1-6 -alkylene-C(=O)-NH(OH), -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6-alkyl, -OC 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-NH2, -OC 1-6 -alkylene-NH-C 1-6 -alkyl, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-OC 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OC(=O)-NH(C 1-6 -alkyl), -OC(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OC(=O)-N(C 1-6 -alkyl)2, -OS(=O)2-NH2, -C 1-6 -alkylene-OS(=O)2-NH2, -OS(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OS(=O)2-NH(C 1-6 -alkyl), -OS(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OS(=O)2-N(C 1-6 -alkyl)2, -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6-alkyl, -NH-C(=O)-NH2, -C 1-6 -alkylene-NH-C(=O)-NH2, -NH-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-C(=O)-NH(C 1-6 -alkyl), -NH-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C(=O)-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH2, -N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-OC 1-6 -alkyl, -NH-S(=O)2-NH2, -C 1-6-alkylene-NH-S(=O)2-NH2, -NH-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-S(=O)2-NH(C 1-6 -alkyl), -NH-S(=O)2N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-S(=O)2N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)-C 1-6 -alkyl, -S(=O)2-C1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(═O)-(3- to 14-membered cycloalkyl), -C(═O)-(3- to 14-membered heterocycloalkyl), -C(═O)-phenyl, -C(═O)-(5- to 14-membered heteroaryl), -S(═O)2-(3- to 14-membered cycloalkyl), -S(═O)2-(3- to 14-membered heterocycloalkyl), -S(═O)2-phenyl, or -S(═O)2-(5- to 14-membered heteroaryl);
[0043] Alternatively, the compound is ethyl 5-methoxy-2-methyl-1-benzothiophene-3-carboxylate.
[0044] Specifically, the present invention provides a compound of formula (I), its stereoisomeric forms, physiologically acceptable salts, solvates and / or polymorphs
[0045]
[0046] in
[0047] R 1 Indicates -F, -Cl, -Br, -I, -CN, -R W 、-OR W、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;
[0048] Q means -OR 2 or -NR 3 R 4 ;
[0049] R 2 Indicates -R Y5 ;
[0050] R 3 Indicates -OH or -R Y1 ;
[0051] R 4 Indicates -R Y2 or -S(=O)2R Y3 ;
[0052] or R 3 and R 4 together forming a 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0053] T represents -O-, and U represents -(CR 5 R 5 ') n -; or T represents -(CR 5 R 5 ') n -, and U represents -O-;
[0054] n is an integer selected from 1, 2, 3, 4 or 5;
[0055] R 5 and R 5 'Independently represent -R Y4 ;
[0056] R 6 、R 7 and R 8 independently represent -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -RW 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;
[0057] W stands for
[0058] 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted;
[0059] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0060] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0061] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0062] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted;
[0063] in
[0064] R W and R X Independently of each other, expressed independently in each case
[0065] -H;
[0066] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0067] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0068] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0069] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0070] R Y1 、R Y2 、R Y3 、R Y4 and R Y5 Independently of each other, expressed independently in each case
[0071] -H;
[0072] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0073] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0074] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0075] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0076] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0077] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0078] and wherein "mono- or polysubstituted" independently in each case means substituted by one or more substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-C 1-6 -alkyl, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -C(=O)-NH(OH), -C 1-6 -alkylene-C(=O)-NH(OH), -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-NH2, -OC 1-6 -alkylene-NH-C 1-6 -alkyl, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-OC 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OC(=O)-NH(C 1-6 -alkyl), -OC(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OC(=O)-N(C 1-6 -alkyl)2, -OS(=O)2-NH2, -C 1-6 -alkylene-OS(=O)2-NH2, -OS(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OS(=O)2-NH(C 1-6 -alkyl), -OS(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OS(=O)2-N(C 1-6 -alkyl)2, -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6-alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6 -alkyl, -NH-C(=O)-NH2, -C 1-6 -alkylene-NH-C(=O)-NH2, -NH-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-C(=O)-NH(C 1-6 -alkyl), -NH-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C(=O)-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH2, -N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6-alkyl)-C(=O)-N(C 1-6 -alkyl)2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-OC 1-6 -alkyl, -NH-S(=O)2-NH2, -C 1-6 -alkylene-NH-S(=O)2-NH2, -NH-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-S(=O)2-NH(C 1-6 -alkyl), -NH-S(=O)2N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-S(=O)2N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6-alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(═O)-(3- to 14-membered cycloalkyl), -C(═O)-(3- to 14-membered heterocycloalkyl), -C(═O)-phenyl, -C(═O)-(5- to 14-membered heteroaryl), -S(═O)2-(3- to 14-membered cycloalkyl), -S(═O)2-(3- to 14-membered heterocycloalkyl), -S(═O)2-phenyl or -S(═O)2-(5- to 14-membered heteroaryl),
[0079] wherein the compound is not:
[0080] 5-Benzyloxybenzo[b]thiophene-3-carboxylic acid.
[0081] A second aspect of the present invention encompasses a pharmaceutical composition comprising a compound of formula (I) as described in the first aspect.
[0082] According to a third aspect, the present invention also provides a compound of formula (I) as described in the first aspect or a pharmaceutical composition as described in the second aspect for use as a medicament.
[0083] According to a fourth aspect, the present invention also encompasses a compound of formula (I) as described in the first aspect or a pharmaceutical composition as described in the second aspect for use in preventing and / or treating a TRPM3-mediated disorder, in particular for preventing and / or treating pain, epilepsy and / or inflammatory hypersensitivity; and / or for combating pain, epilepsy and / or inflammatory hypersensitivity. Specifically for preventing and / or treating pain, epileptic encephalopathy and / or inflammatory hypersensitivity; and / or for combating pain, epileptic encephalopathy and / or inflammatory hypersensitivity.
[0084] The present invention also provides a method for preventing or treating a TRPM3-mediated disorder by administering a compound of formula (I) as described in the first aspect to a subject in need thereof. More specifically, the present invention relates to methods for preventing and / or treating pain, epilepsy, and / or inflammatory hypersensitivity; and / or for combating pain, epilepsy, and / or inflammatory hypersensitivity. More specifically, the present invention relates to methods for preventing and / or treating pain, epileptic encephalopathy, and / or inflammatory hypersensitivity; and / or for combating pain, epileptic encephalopathy, and / or inflammatory hypersensitivity.
[0085] The present invention further provides a method for preparing the compound of formula (I) as described in the first aspect, the method comprising the following steps:
[0086] - converting benzothiophene into a 5-hydroxybenzothiophene-3-carboxylate derivative,
[0087] - Substitution of the previously obtained 5-hydroxybenzothiophene-3-carboxylate derivative with a suitable derivative or alcohol derivative carrying a leaving group under alkylation or Mitsunobu conditions to obtain a 5-O-substituted benzothiophene-3-carboxylate derivative
[0088] - converting the previously obtained 5-O-substituted benzothiophene-3-carboxylate derivative into formic acid to obtain a 5-O-substituted benzothiophene-3-carboxylic acid derivative, and
[0089] - The previously obtained 5-O substituted benzothiophene-3-carboxylic acid derivatives are coupled with suitable amines to obtain the desired derivatives of the present invention. DETAILED DESCRIPTION
[0090] Before describing the present invention, it should be understood that this invention is not limited to the particular processes, methods and compounds described, as such processes, methods and compounds may, of course, vary. It should also be understood that the terminology used herein is not intended to be limiting, as the scope of the present invention will be limited only by the appended claims.
[0091] When describing the compounds or processes of the present invention, the terms used are to be interpreted in accordance with the following definitions, unless the context indicates otherwise.
[0092] As used in the specification and the appended claims, the singular forms "a," "an," and "the" include both singular and plural referents unless the context clearly dictates otherwise. For example, "a compound" means one compound or more than one compound.
[0093] As used herein, the terms "comprising, comprises, and comprised of" are synonymous with "including, includes, or "containing, contains," and are inclusive or open-ended and do not exclude additional, unrecited members, elements, or method steps. The terms "comprising, comprises, and comprised of" also include the term "consisting of."
[0094] As used herein, the term "about" when referring to a measurable value such as a parameter, amount, time interval, etc., is intended to encompass variations of + / -10% or less, preferably + / -5% or less, more preferably + / -1% or less, and still more preferably + / -0.1% or less of the specified value, so long as such variations are suitable for performing the disclosed invention. It should be understood that the value to which the modifier "about" refers is itself also specifically and preferably disclosed.
[0095] As used herein, when the term "and / or" is used in conjunction with a list of two or more items, it means that any one of the listed items can be taken alone, or any combination of two or more of the listed items can be taken. For example, if a list is described as containing the group A, B, and / or C, the list can contain A alone; B alone; C alone; a combination of A and B; a combination of A and C; a combination of B and C; or a combination of A, B, and C.
[0096] The recitation of numerical ranges by endpoints includes all integers and, where appropriate, fractions within the range (e.g., 1 to 5 when referring to, for example, a plurality of elements, may include 1, 2, 3, 4, and when referring to, for example, a measurement, may also include 1.5, 2, 2.75, and 3.80). The recitation of endpoints also includes the endpoint values themselves (e.g., 1.0 to 5.0 includes both 1.0 and 5.0). Any numerical range recited herein is intended to include all subranges subsumed therein.
[0097] References throughout this specification to "one embodiment" or "an embodiment" mean that a particular feature, structure, or characteristic described in connection with the embodiment is included in at least one embodiment of the present invention. Thus, the appearances of the phrases "in one embodiment" or "in an embodiment" in various places throughout this specification do not necessarily all refer to the same embodiment, but may. Furthermore, in one or more embodiments, the particular features, structures, or characteristics may be combined in any suitable manner, as will be apparent to those skilled in the art from this disclosure. Furthermore, while some embodiments described herein include some features included in other embodiments but not others, as will be understood by those skilled in the art, combinations of features from different embodiments are intended to be within the scope of the present invention and to form different embodiments. For example, in the following claims, any of the claimed embodiments may be used in any combination.
[0098] Similarly, it should be appreciated that in the description of exemplary embodiments of the invention, various features of the invention are sometimes grouped together in a single embodiment, figure, or description thereof for the purpose of simplifying the disclosure and aiding in understanding one or more of the various inventive aspects.
[0099] Unless otherwise defined, all terms (including technical and scientific terms) used in disclosing the present invention have the meaning commonly understood by one of ordinary skill in the art to which the present invention belongs. For further guidance, definitions of terms used in the specification are included to better understand the teachings of the present invention.
[0100] When describing the present invention, the terms used are to be interpreted in accordance with the following definitions, unless the context indicates otherwise.
[0101] The terms described above and other terms used in the specification can be well understood by those skilled in the art.
[0102] Whenever the term "substituted" is used herein, it is meant to indicate that one or more hydrogen atoms on the indicated atom in the expression using "substituted" is replaced with a selection from the indicated group, provided that the normal valency of the indicated atom is not exceeded and that the substitution results in a chemically stable compound, i.e., a compound sufficiently robust to survive isolation from a reaction mixture.
[0103] In each of the following definitions, the number of carbon atoms represents the maximum number of carbon atoms that is generally optimally present in a substituent or linker; it is understood that where otherwise indicated in this application, the number of carbon atoms represents the optimal maximum number of carbon atoms for that particular substituent or linker.
[0104] As used herein, the term "leaving group" or "LG" refers to a chemical group that is easily displaced or cleaved or hydrolyzed by a nucleophile under basic or acidic conditions. In a specific embodiment, the leaving group is selected from a halogen atom (e.g., Cl, Br, I) or a sulfonate (e.g., methanesulfonate, tosylate, triflate).
[0105] The term "protecting group" refers to a compound portion that masks or changes the properties of a functional group or the properties of the entire compound. The chemical substructure of a protecting group varies greatly. One function of a protecting group is to act as an intermediate in the synthesis of the parent drug substance. Chemical protecting groups and strategies for protection / deprotection are well known in the art. See: "Protective Groups in Organic Chemistry", Theodora W. Greene (John Wiley & Sons, Inc., New York), 1991. Protecting groups are typically used to mask the reactivity of certain functional groups to aid in the efficiency of desired chemical reactions, such as forming and breaking chemical bonds in an orderly and planned manner. Protection of a compound's functional groups changes other physical properties besides the reactivity of the protected functional group, such as polarity, lipophilicity (hydrophobicity), and other properties that can be measured by conventional analytical tools. Chemically protected intermediates themselves can be biologically active or inactive.
[0106] Protected compounds can also show changed, and in some cases optimized external and internal properties, such as by cell membrane and resistance to enzymatic degradation or chelation. In this effect, the protected compound with expected therapeutic effect can be referred to as prodrug. Another function of blocking group is that the parent drug is converted into prodrug, thus releasing the parent drug when converting the prodrug in vivo. Because active prodrug can be more effectively absorbed than the parent drug, prodrug can have a larger effect than the parent drug in vivo. In the case of chemical intermediates, blocking group is removed in vitro, or in the case of prodrug, blocking group is removed in vivo. For chemical intermediates, whether the resulting product (for example, alcohol) after deprotection is physiologically acceptable is not particularly important, although it is usually more desirable whether the product is pharmacologically harmless.
[0107] As used herein, the term "heteroatom" means an atom selected from the group consisting of nitrogen (which may be quaternized); oxygen; and sulfur (including sulfoxides and sulfones).
[0108] As used herein, the term "saturated or unsaturated alkyl" encompasses saturated alkyl groups as well as unsaturated alkyl groups such as alkenyl, alkynyl, and the like. Suitable examples of saturated or unsaturated alkyl groups include, but are not limited to, methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl (i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl, and 3,3-dimethyl-2-butyl. "C 1-6 "Alkyl" includes all straight or branched chain alkyl groups having between 1 and 6 carbon atoms, and thus includes methyl, ethyl, n-propyl, isopropyl, butyl and isomers thereof (e.g., n-butyl, isobutyl and tert-butyl); pentyl and isomers thereof, hexyl and isomers thereof. For example, "C 1-5 "Alkyl" includes all straight or branched chain alkyl groups having between 1 and 5 carbon atoms, and thus includes methyl, ethyl, n-propyl, isopropyl, butyl and isomers thereof (e.g., n-butyl, isobutyl and tert-butyl); pentyl and isomers thereof; ethylene or vinyl (-CH=CH2), allyl (-CH2CH=CH2), 5-hexenyl (-CH2CH2CH2CH2CH=CH2); 2-butenyl, 3-butenyl, 2-pentenyl and isomers thereof, 2-hexenyl and isomers thereof, 2,4-pentadienyl, ethynyl, 2-propynyl, 2-butynyl, 3-butynyl, 2-pentynyl and chain isomers thereof, 2-hexynyl and chain isomers thereof.
[0109] As used herein, the term "alkyl" means a straight or branched normal, secondary or tertiary hydrocarbon with no sites of unsaturation. Examples are methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl (i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl and 3,3-dimethyl-2-butyl. "C 1-6 "Alkyl" includes all straight or branched chain alkyl groups having between 1 and 6 carbon atoms, and thus includes methyl, ethyl, n-propyl, isopropyl, butyl and isomers thereof (e.g., n-butyl, isobutyl and tert-butyl); pentyl and isomers thereof, hexyl and isomers thereof. For example, "C 1-5 "Alkyl" includes all straight or branched chain alkyl groups having between 1 and 5 carbon atoms, and thus includes methyl, ethyl, n-propyl, isopropyl, butyl and isomers thereof (e.g., n-butyl, isobutyl and tert-butyl); pentyl and isomers thereof. For example, "C 1-4 "Alkyl" includes all straight or branched chain alkyl groups having between 1 and 4 carbon atoms, and thus includes methyl, ethyl, n-propyl, isopropyl, butyl, and isomers thereof (e.g., n-butyl, isobutyl, and tert-butyl). For example, "C 1-3 "Alkyl" includes all straight or branched chain alkyl groups having between 1 and 3 carbon atoms, and thus includes methyl, ethyl, n-propyl, isopropyl. "Substituted C 1-6 "Alkyl" refers to a C substituted with one or more substituents (e.g., 1 to 3 substituents, e.g., 1, 2, or 3 substituents) at any available point of attachment. 1-6 alkyl.
[0110] As used herein, the term "alkenyl" means a straight or branched normal hydrocarbon, secondary hydrocarbon, or tertiary hydrocarbon having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp2 double bond. Examples include, but are not limited to, ethylene or vinyl (-CH=CH2), allyl (-CH2CH=CH2), and 5-hexenyl (-CH2CH2CH2CH2CH=CH2). The double bond can be in cis or trans configuration. When a subscript is used after a carbon atom herein, the subscript refers to the number of carbon atoms that the named group may contain. For example, the term "C 2-6"Alkenyl" refers to an unsaturated hydrocarbon group that may be straight or branched, containing one or more carbon-carbon double bonds and containing 2 to 6 carbon atoms. For example, C 2-4 Alkenyl includes all straight-chain or branched alkenyl groups having 2 to 4 carbon atoms. 2-6 Examples of alkenyl groups are ethenyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl and the like.
[0111] As used herein, the term "alkynyl" means a straight or branched normal hydrocarbon, secondary hydrocarbon, or tertiary hydrocarbon having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp triple bond. Examples include, but are not limited to, ethynyl (-C≡CH) and 1-propynyl (propargyl, -CH2C≡CH). When a subscript is used after a carbon atom, the subscript refers to the number of carbon atoms that the named group may contain. For example, the term "C 2-6 "Alkynyl" refers to an unsaturated hydrocarbon group that may be straight or branched, containing one or more carbon-carbon triple bonds and containing 2 to 6 carbon atoms. For example, C 2-4 Alkynyl includes all straight-chain or branched alkynyl groups having 2 to 4 carbon atoms. 2-6 Non-limiting examples of alkynyl groups include ethynyl, 2-propynyl, 2-butynyl, 3-butynyl, 2-pentynyl and chain isomers thereof, 2-hexynyl and chain isomers thereof, and the like.
[0112] As used herein, the term "saturated or unsaturated alkylene" encompasses saturated alkylene as well as unsaturated alkylene, such as alkenylene, alkynylene, etc. As used herein, the term "alkylene" means a saturated, straight-chain or branched hydrocarbon radical having two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkane. Typical alkylene groups include, but are not limited to, methylene (-CH2-), ethylene (-CH2-CH2-), methylmethylene (-CH(CH3)-), 1-methyl-ethylene (-CH(CH3)-CH2-), n-propylene (-CH2-CH2-CH2-), 2-methylpropylene (-CH2-CH(CH3)-CH2-), 3-methylpropylene (-CH2-CH2-CH(CH3)-), n-butylene (-CH2-CH2-CH2-CH2-), 2-methylbutylene (-CH2-CH(CH3)-CH2-CH2-), 4-methylbutylene (-CH2-CH2-CH2-CH(CH3)-), pentylene and its chain isomers, hexylene and its chain isomers.
[0113] As used herein, the term "alkenylene" means a straight or branched chain hydrocarbon radical having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp2 double bond, and having two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkene. 2-6 "Alkenylene" by itself or as part of another substituent refers to a divalent C 2-6 An alkenyl group, that is, has two single bonds to attach two other groups.
[0114] As used herein, the term "alkynylene" means a straight or branched chain hydrocarbon radical having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp triple bond, and having two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkyne. As used herein, the term "C 2-6 "Alkynylidene" by itself or as part of another substituent refers to a divalent C 2-6 Alkynyl groups, that is, have two single bonds to attach two other groups.
[0115] The term "alkenyl" as a group or part of a group refers to an unsaturated hydrocarbon group that may be straight or branched chain containing one or more carbon-carbon double bonds. When a subscript is used after a carbon atom herein, the subscript refers to the number of carbon atoms that the named group may contain. For example, the term "C 2-6 "Alkenyl" refers to an unsaturated hydrocarbon group that may be straight or branched, containing one or more carbon-carbon double bonds and containing 2 to 6 carbon atoms. For example, C 2-4 Alkenyl includes all straight-chain or branched alkenyl groups having 2 to 4 carbon atoms. 2-6 Examples of alkenyl groups are ethenyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl and the like.
[0116] The term "alkynyl" by itself or as part of another substituent refers to an unsaturated hydrocarbon radical which may be straight or branched chain containing one or more carbon-carbon triple bonds. When a subscript is used herein after a carbon atom, the subscript refers to the number of carbon atoms the named group may contain. For example, the term "C 2-6 "Alkynyl" refers to an unsaturated hydrocarbon group that may be straight or branched, containing one or more carbon-carbon triple bonds and containing 2 to 6 carbon atoms. For example, C 2-4 Alkynyl includes all straight-chain or branched alkynyl groups having 2 to 4 carbon atoms. 2-6Non-limiting examples of alkynyl groups include ethynyl, 2-propynyl, 2-butynyl, 3-butynyl, 2-pentynyl and chain isomers thereof, 2-hexynyl and chain isomers thereof, and the like.
[0117] The term "halogenated C 1-6 "Alkyl" as a group or part of a group refers to a C 1-6 Alkyl wherein one, two or three hydrogen atoms are each substituted by halogen as defined herein. Such halogenated C 1-6 Non-limiting examples of alkyl groups include chloromethyl, 1-bromoethyl, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1,1-trifluoroethyl, and the like.
[0118] As used herein, term " saturated or unsaturated heteroalkyl " covers saturated heteroalkyl and unsaturated heteroalkyl, such as heteroalkenyl, heteroalkynyl etc.As used herein, term " heteroalkyl " means straight or branched chain alkyl, wherein one or more carbon atoms (typically 1,2 or 3) are replaced by heteroatoms (that is, oxygen, nitrogen or sulphur atom), and condition is that the chain can be free of two adjacent O atoms or two adjacent S atoms.This means that one or more -CH of the alkyl can be replaced by -NH2 and / or one or more -CH of the alkyl - can be replaced by -NH-, -O- or -S-. The S atom in the chain can optionally be oxidized by one or two oxygen atoms to provide sulfoxide and sulfone respectively. In addition, the heteroalkyl in the compound of the present invention can contain oxo or thio group at any carbon or heteroatom, which will produce stable compound. Exemplary heteroalkyl includes but is not limited to alcohol, alkyl ether (such as -methoxy, -ethoxy, -butoxy ...), primary alkylamine, secondary alkylamine and tertiary alkylamine, amides, ketones, esters, alkyl sulfide and alkyl sulfone. The term "heteroalkenyl" means a straight or branched chain alkenyl group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Thus, the term heteroalkenyl includes imine, -O-alkenyl, -NH-alkenyl, -N(alkenyl), -N(alkyl)(alkenyl), and -S-alkenyl. As used herein, the term "heteroalkynyl" means a straight or branched chain alkynyl group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Thus, the term heteroalkynyl includes -cyano, -O-alkynyl, -NH-alkynyl, -N(alkynyl), -N(alkyl)(alkynyl), -N(alkenyl)(alkynyl), and -S-alkynyl.
[0119] As used herein, the term "saturated or unsaturated heteroalkylene" encompasses saturated heteroalkylene and unsaturated heteroalkylene, such as heteroalkenylene, heteroalkynylene, etc. As used herein, the term "heteroalkylene" means a straight or branched chain alkylene group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by a heteroatom (i.e., an oxygen, nitrogen, or sulfur atom), provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein, the term "heteroalkenylene" means a straight or branched chain alkenylene group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by an oxygen, nitrogen, or sulfur atom, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein, the term "heteroalkynylene" means a straight or branched chain alkynylene group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by an oxygen, nitrogen, or sulfur atom, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms.
[0120] As used herein, the term "saturated or unsaturated cycloalkyl" encompasses saturated cycloalkyl and unsaturated cycloalkyl, such as cycloalkenyl, cycloalkynyl, etc. Specifically, as used herein, the term "saturated or unsaturated cycloalkyl" encompasses saturated cycloalkyl and unsaturated non-aromatic cycloalkyl, such as cycloalkenyl and cycloalkynyl. Specifically, the terms "saturated or unsaturated cycloalkyl" and "saturated or non-aromatic unsaturated cycloalkyl" are synonymous. The term "saturated or unsaturated cycloalkyl" also includes all saturated and unsaturated hydrocarbon groups containing one or more rings, including monocyclic or bicyclic groups. The additional rings of the polycyclic cycloalkyl can be fused, bridged and / or joined by one or more spiro atoms. Suitable examples of saturated or unsaturated cycloalkyl groups include, but are not limited to, cyclopropyl, cyclopropenyl, cyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, 1,3-cyclohexadienyl, 1,4-cyclohexadienyl, 1,5-cyclooctadienyl, bicyclo[2.2.1]hept-2-yl, (1S,4R)-norbornan-2-yl, (1R,4R)-norbornan-3-yl, (1S,4S)-norbornan-2-yl, (1R,4S)-norbornan-2-yl, decalinyl, adamantyl, spiro[3.3]hept-2-yl, 3-bicyclo[3.1.0]hexanyl. Unless otherwise indicated, as used herein, the term "cycloalkyl" means a saturated cyclic hydrocarbon group, including monocyclic or bicyclic groups; the other rings of polycyclic cycloalkyl groups can be fused, bridged and / or connected by one or more spiro atoms. Examples of cycloalkyl groups include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, norbornyl, fenchyl, decalinyl, adamantyl, spiro [3.3] hept-2-yl, 3-bicyclo [3.1.0] hexane, etc. As used herein, the term "cycloalkenyl" means a non-aromatic cyclic hydrocarbon group having at least one unsaturated site (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp2 double bond. The term "cycloalkenyl" also includes monocyclic or bicyclic groups; the other rings of polycyclic cycloalkenyl groups can be fused, bridged and / or connected by one or more spiro atoms. Examples include, but are not limited to, cyclopentenyl and cyclohexenyl. The double bond can be a cis or trans configuration. As used herein, the term "cycloalkynyl" means a non-aromatic cyclic hydrocarbon radical having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp triplet. An example is cyclohept-1-yne. A fused system of a cycloalkyl ring and a heterocycloalkyl ring is considered to be a heterocycloalkyl, regardless of the ring bound to the core structure. A fused system of a cycloalkyl ring and an aryl ring is considered to be an aryl, regardless of the ring bound to the core structure. A fused system of a cycloalkyl ring and a heteroaryl ring is considered to be a heteroaryl, regardless of the ring bound to the core structure.
[0121] As used herein, the term "saturated or unsaturated heterocycloalkyl" encompasses saturated heterocycloalkyl and unsaturated non-aromatic heterocycloalkyl groups comprising at least one heteroatom, i.e., N, O, or S as a ring member. Specifically, the terms "saturated or unsaturated heterocycloalkyl" and "saturated or non-aromatic unsaturated heterocycloalkyl" are synonymous. Unless otherwise indicated, as used herein, the term "heterocycloalkyl" means a "cycloalkyl" in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Unless otherwise indicated, as used herein, the term "heterocycloalkenyl" means a "cycloalkenyl" in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Unless otherwise indicated, as used herein, the term "heterocycloalkynyl" means a "cycloalkynyl" group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Examples of saturated and unsaturated heterocycloalkyl groups include, but are not limited to, azepane, 1,4-oxazepane, azetane, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxazolidine, morpholine, oxazolidine, oxetane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran,
[0015] In some embodiments, the present invention includes but is not limited to thiophene, thiazolyl thiophene, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolidine, thiapyrrolAdditional heterocycloalkyl groups within the meaning of the present invention are described in Paquette, Leo A., Principles of Modern Heterocyclic Chemistry (WA Benjamin, New York, 1968), in particular Chapters 1, 3, 4, 6, 7, and 9; The Chemistry of Heterocyclic Compounds, A series of Monographs (John Wiley & Sons, New York, 1950 to present), in particular Volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, CW, and Scriven, E., Comprehensive Heterocyclic Chemistry (Pergamon Press, 1996); and J. Am. Chem. Soc. (1960) 82:5566. When a heterocycloalkyl group does not contain nitrogen as a ring member, it is typically bonded through a carbon. When a heterocycloalkyl group contains nitrogen as a ring member, it may be bonded through either nitrogen or carbon. A system of a heterocycloalkyl ring fused to a cycloalkyl ring is considered a heterocycloalkyl group, regardless of the ring to which it is attached. A system of a heterocycloalkyl ring fused to an aryl ring is considered a heterocycloalkyl group, regardless of the ring to which it is attached. A system of a heterocycloalkyl ring fused to a heteroaryl ring is considered a heteroaryl group, regardless of the ring to which it is attached.
[0122] As used herein, the term "aryl" means an aromatic hydrocarbon. Typical aryl groups include, but are not limited to, one ring or two or three rings fused together, groups derived from benzene, naphthalene, anthracene, biphenyl, etc. The fused system of an aryl ring and a cycloalkyl ring is considered to be an aryl group, regardless of the ring that is combined with the core structure. The fused system of an aryl ring and a heterocycloalkyl ring is considered to be a heterocycloalkyl group, regardless of the ring that is combined with the core structure. Therefore, indoline, dihydrobenzofuran, dihydrobenzothiophene, etc. are considered to be heterocycloalkyl groups according to the present invention. The fused system of an aryl ring and a heteroaryl ring is considered to be a heteroaryl group, regardless of the ring that is combined with the core structure.
[0123] As used herein, the term "heteroaryl" means an aromatic ring system that includes at least one heteroatom (i.e., N, O, or S) as a ring member of the aromatic ring system. Examples of heteroaryl groups include, but are not limited to, benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine.
[0124] By way of further example, the carbon-bonded heterocycle is bonded at position 2, 3, 4, 5, or 6 of a pyridine, at position 3, 4, 5, or 6 of a pyridazine, at position 2, 4, 5, or 6 of a pyrimidine, at position 2, 3, 5, or 6 of a pyrazine, at position 2, 3, 4, or 5 of a furan, tetrahydrofuran, thiophene, pyrrole, or tetrahydropyrrole, at position 2, 4, or 5 of an oxazole, imidazole, or thiazole, at position 3, 4, or 5 of an isoxazole, pyrazole, or isothiazole, at position 2 or 3 of an aziridine, at position 2, 3, or 4 of an azetidine, at position 2, 3, 4, 5, 6, 7, or 8 of a quinoline, or at position 1, 3, 4, 5, 6, 7, or 8 of an isoquinoline.
[0125] Preferred carbon-bonded heterocycles include 2-pyridyl, 3-pyridyl, 4-pyridyl, 5-pyridyl, 6-pyridyl, 3-pyridazinyl, 4-pyridazinyl, 5-pyridazinyl, 6-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 6-pyrimidinyl, 2-pyrazinyl, 3-pyrazinyl, 5-pyrazinyl, 6-pyrazinyl, 2-thiazolyl, 4-thiazolyl, or 5-thiazolyl. For example, nitrogen-bonded heterocycles are bonded to aziridine, azetidine, pyrrole, pyrrolidine, 2-pyrroline, 3-pyrroline, imidazole, imidazolidine, 2-imidazoline, 3-imidazoline, pyrazole, pyrazoline, 2-pyrazoline, 3-pyrazoline, piperidine, piperazine, indole, indoline, 1H-indazole at position 1, isoindole or isoindoline at position 2, morpholine at position 4, and carbazole or β-carboline at position 9. Preferred nitrogen-bonded heterocycles include 1-aziridine, 1-azetidinyl, 1-pyrrolyl, 1-imidazolyl, 1-pyrazolyl, and 1-piperidinyl. Additional heteroaryl groups within the meaning of the present invention are described in Paquette, Leo A., Principles of Modern Heterocyclic Chemistry (W.A. Benjamin Publishers, New York, 1968), in particular Chapters 1, 3, 4, 6, 7, and 9; in The Chemistry of Heterocyclic Compounds: A Series of Monographs (John Wiley & Sons, New York, 1950 to present), in particular Volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, C.W., and Scriven, E., Comprehensive Heterocyclic Chemistry (Pergamon Publishers, 1996); and in Journal of the American Chemical Society (1960) 82:5566.
[0126] As used herein with respect to substituents, and unless otherwise indicated, the terms "monosubstituted," "disubstituted," "trisubstituted," "polysubstituted," and the like refer to chemical structures as defined herein wherein the corresponding moiety is substituted with one or more substituents, meaning that one or more hydrogen atoms of the moiety are each independently replaced with a substituent. For example, -C 1-6 -alkyl covers -CH2F, -CHF2, -CF3, -CH2CF3, CF2CF3, etc. Likewise, -C may be polysubstituted with substituents independently selected from -F and -Cl. 1-6 -Alkyl covers -CH2F, -CHF2, -CF3, -CH2CF3, CF2CF3, -CH2Cl, -CHCl2, -CCl3, -CH2CCl3, CCl2CCl3, -CHClF, -CClF2, -CCl2CF3, -CF2CCl3, -CClFCCl2F, etc. The name of any substituent found in more than one site in the compounds of the invention should be selected independently.
[0127] Unless otherwise indicated, as used herein, the term "solvate" includes any combination that can be formed between a derivative of the present invention and a suitable inorganic solvent (e.g., hydrate) or an organic solvent (such as, but not limited to, alcohols, ketones, esters, ethers, nitriles, etc.).
[0128] As used herein, the term "subject" refers to an animal, including a human, preferably a mammal, most preferably a human, that has been the object of treatment, observation or experiment.
[0129] As used herein, the term "therapeutically effective amount" means that amount of an active compound or agent that elicits the biological or medical response in a tissue system, animal or human that is being sought by the researcher, veterinarian, medical doctor or other clinician, including alleviation or partial alleviation of the symptoms of the disease or condition being treated.
[0130] As used herein, the term "composition" is intended to encompass a product comprising the specified ingredients in therapeutically effective amounts, as well as any product which results, directly or indirectly, from combination of the specified ingredients in the specified amounts.
[0131] As used herein, the term "antagonist" or "inhibitor" refers to a compound that can produce a functional antagonistic effect on the TRPM3 ion channel, including competitive antagonists, non-competitive antagonists, desensitizing agonists and partial agonists.
[0132] For the purposes of the present invention, the term "TRPM3-modulated" is used to refer to conditions that are affected by modulation of the TRPM3 ion channel, including states mediated by the TRPM3 ion channel.
[0133] As used herein, the term "TRPM3-mediated disorder" refers to a disorder or disease that can be prevented, treated, (partially) alleviated or improved using an antagonist of TRPM3, as well as symptoms and pain and inflammatory hypersensitivity symptoms. According to the International Association for the Study of Pain and for the purposes of the present invention, pain is an unpleasant sensation and emotional experience associated with actual or potential tissue damage, or is described in terms of such damage. Preferably, the disorder mediated by TRPM3 is pain or epilepsy. Preferably, the disorder mediated by TRPM3 is epilepsy, and the epilepsy is preferably selected from epileptic encephalopathy. For the purposes of the present invention, the term "epileptic encephalopathy" refers to a group of severe epilepsy characterized by epileptic seizures and encephalopathy. Preferably, the disorder mediated by TRPM3 is pain, and the pain is preferably selected from nociceptive pain, inflammatory pain and neuropathic pain. More preferably, pain is postoperative pain. For the purposes of the present invention, the term "inflammatory hypersensitivity" is used to refer to a condition characterized by one or more hallmarks of inflammation (including edema, erythema, hyperthermia, and pain) and / or an exaggerated physiological or pathophysiological response to one or more types of stimuli (including thermal, mechanical, and / or chemical stimuli).
[0134] The invention will be further described and in some cases with respect to specific embodiments but the invention is not limited thereto.
[0135] Preferred claims (features) and embodiments of the compounds and methods of the present invention are now set forth. Each claim and embodiment of the present invention, as so defined, may be combined with any other claim and / or embodiment, unless expressly indicated to the contrary. Specifically, any feature indicated as preferred or advantageous may be combined with any one or more other features indicated as preferred or advantageous.
[0136] The numbered claims of this invention are:
[0137] 1. A compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph
[0138]
[0139] in
[0140] R 1 Indicates -F, -Cl, -Br, -I, -CN, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)RX 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;
[0141] Q means -OR 2 or -NR 3 R 4 ;
[0142] R 2 Indicates -R Y5 ;
[0143] R 3 Indicates -OH or -R Y1 ;
[0144] R 4 Indicates -R Y2 or -S(=O)2R Y3 ;
[0145] or R 3 and R 4 together forming a 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0146] T represents -O-, and U represents -(CR 5 R 5 ') n -; or T represents -(CR 5 R 5 ') n -, and U represents -O-;
[0147] n is an integer selected from 1, 2, 3, 4 or 5;
[0148] R 5 and R 5 'Independently represent -R Y4 ;
[0149] R 6 、R 7 and R 8 independently represent -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -R W 、-OR W 、-OC(=O)R W 、-NR W RX 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;
[0150] W stands for
[0151] 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted;
[0152] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0153] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0154] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0155] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted;
[0156] in
[0157] R W and R X Independently of each other, expressed independently in each case
[0158] -H;
[0159] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0160] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0161] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0162] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0163] R Y1 、R Y2 、R Y3 、R Y4 and R Y5 Independently of each other, expressed independently in each case
[0164] -H;
[0165] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0166] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0167] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0168] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0169] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0170] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0171] and wherein "mono- or polysubstituted" independently in each case means substituted by one or more substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-C 1-6 -alkyl, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -C(=O)-NH(OH), -C 1-6 -alkylene-C(=O)-NH(OH), -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-NH2, -OC 1-6 -alkylene-NH-C 1-6 -alkyl, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-OC 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OC(=O)-NH(C 1-6 -alkyl), -OC(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OC(=O)-N(C 1-6 -alkyl)2, -OS(=O)2-NH2, -C 1-6 -alkylene-OS(=O)2-NH2, -OS(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OS(=O)2-NH(C 1-6 -alkyl), -OS(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OS(=O)2-N(C 1-6 -alkyl)2, -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6-alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6 -alkyl, -NH-C(=O)-NH2, -C 1-6 -alkylene-NH-C(=O)-NH2, -NH-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-C(=O)-NH(C 1-6 -alkyl), -NH-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C(=O)-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH2, -N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6-alkyl)-C(=O)-N(C 1-6 -alkyl)2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-OC 1-6 -alkyl, -NH-S(=O)2-NH2, -C 1-6 -alkylene-NH-S(=O)2-NH2, -NH-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-S(=O)2-NH(C 1-6 -alkyl), -NH-S(=O)2N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-S(=O)2N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6-alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(═O)-(3- to 14-membered cycloalkyl), -C(═O)-(3- to 14-membered heterocycloalkyl), -C(═O)-phenyl, -C(═O)-(5- to 14-membered heteroaryl), -S(═O)2-(3- to 14-membered cycloalkyl), -S(═O)2-(3- to 14-membered heterocycloalkyl), -S(═O)2-phenyl, or -S(═O)2-(5- to 14-membered heteroaryl);
[0172] or the compound is ethyl 5-methoxy-2-methyl-1-benzothiophene-3-carboxylate;
[0173] Specifically wherein the compound is not:
[0174] 5-Benzyloxybenzo[b]thiophene-3-carboxylic acid.
[0175] 2. The compound according to claim 1, wherein Q represents -NR 3 R 4 .
[0176] 3. The compound according to statement 1, wherein Q represents -OR 2 .
[0177] 4. A compound according to any one of the preceding statements, wherein T represents -O-, and U represents -(CR 5 R 5 ') n -.
[0178] 5. A compound according to any one of the preceding statements, wherein R 1 express
[0179] -H, -F, -Cl, -Br, -I;
[0180] -C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0181] -OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0182] -C(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0183] -C(=O)OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0184] -C(=O)NH2;
[0185] -C(=O)NHC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0186] -C(=O)N(C 1-6 -alkyl) 2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0187] -S(=O)C1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0188] -S(=O)2-C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0189] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0190] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0191] 6. A compound according to any one of the preceding statements, wherein R 1 express
[0192] -H, -F, -Cl, -Br, -I;
[0193] -C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0194] -OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0195] -C(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0196] -C(=O)OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0197] -C(=O)NH2;
[0198] -C(=O)NHC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0199] -C(=O)N(C 1-6-alkyl) 2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0200] -S(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0201] -S(=O)2-C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0202] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0203] 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted; wherein each of the 3-14 membered cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl is optionally linked through -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0204] 7. A compound according to any one of the preceding statements, wherein R 1 Indicates -H, -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)C 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -C(=O)NH2; -C(=O)NHC 1-6 -alkyl, -C(=O)N(C 1-6 -alkyl)2, -S(=O)-C1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -OC 1-6 -alkyl, unsubstituted-cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl.
[0205] 8. A compound according to any one of the preceding statements, wherein R 1 Indicates -H, -C 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -CHF2, -CF3 or unsubstituted-cyclopentyl.
[0206] 9. A compound according to any one of the preceding statements, wherein R 2 express
[0207] -H;
[0208] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0209] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0210] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0211] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0212] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0213] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0214] 10. A compound according to any one of the preceding statements, wherein R 2 express
[0215] -H;
[0216] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0217] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0218] 11. A compound according to any one of the preceding statements, wherein R 2 Indicates -H, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3.
[0219] 12. A compound according to any one of the preceding statements, wherein R 2 represents -H or saturated, unsubstituted or monosubstituted -C 1-6 -alkyl.
[0220] 13. A compound according to any one of the preceding statements, wherein R 2 Indicates -H.
[0221] 14. A compound according to any of the preceding statements, wherein R 3 express
[0222] -H;
[0223] -OH;
[0224] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0225] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0226] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0227] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0228] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0229] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0230] 15. A compound according to any one of the preceding statements, wherein R 3 express
[0231] -H;
[0232] -OH;
[0233] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0234] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0235] 16. A compound according to any of the preceding statements, wherein R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3.
[0236] 17. A compound according to any of the preceding statements, wherein R 3 represents -H, -OH or saturated, unsubstituted or monosubstituted -C 1-6 -alkyl.
[0237] 18. A compound according to any of the preceding statements, wherein R 3 Indicates -H.
[0238] 19. A compound according to any of the preceding statements, wherein R 4 express
[0239] -H;
[0240] -S(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0241] -S(=O)2-C 1-6- alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0242] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0243] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0244] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0245] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0246] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0247] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0248] 20. A compound according to any of the preceding statements, wherein R 4 express
[0249] -H;
[0250] -S(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0251] -S(=O)2-C1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0252] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0253] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0254] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0255] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0256] -C 1-6 -alkylene-phenyl, which is unsubstituted, monosubstituted or polysubstituted;
[0257] -phenyl, which is unsubstituted, monosubstituted or polysubstituted; or
[0258] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0259] 21. A compound according to any of the preceding statements, wherein R 4 express
[0260] -S(=O)2C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6-alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0261] -S(=O)2(3-14 membered cycloalkyl), wherein the 3-14 membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which are in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6-alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0262] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0263] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6-alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0264] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which are in each case saturated or unsaturated, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6-alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0265] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from the group consisting of azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxazolidine, morpholine, oxazolidine, oxetane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiocyclohexane, ... pentane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; which are in each case unsubstituted, monosubstituted or polysubstituted, independently of one another, by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6-alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0266] -C 1-6 -alkylene-phenyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -CN, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0267] -phenyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -CN, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0268] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole , isoxazole, naphthidine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole and [1,2,4]triazolo[4,3-a]pyrimidine; which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -CN, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl.
[0269] 22. A compound according to any one of the preceding statements, wherein R 4 express
[0270] -H;
[0271] -S(=O)2C 1-6 -alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted by -F;
[0272] -S(=O)2(3-14 membered cycloalkyl), which is saturated and unsubstituted;
[0273] -C 1-6 -alkyl, which is saturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6-alkyl) 2, 3-14 membered cycloalkyl, unsubstituted -phenyl, oxetanyl or pyrimidinyl;
[0274] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or mono- or polysubstituted by -F, -Cl, -Br, -I, -OH, wherein the 3- to 14-membered cycloalkyl is saturated, unsubstituted, mono- or disubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, unsubstituted -phenyl, oxetanyl or pyrimidinyl;
[0275] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C1-6 -alkylene- is unsubstituted or mono- or polysubstituted by -F, -Cl, -Br, -I, -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from azetidine, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, octahydropyrrolo[1,2-a]pyrrole, oxazine, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C1-6 -alkyl)2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl;
[0276] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -F, -Cl, -Br, -I, -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, which are in each case unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6-alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl.
[0277] 23. A compound according to any of the preceding statements, wherein R 4 express
[0278] -H;
[0279] -S(=O)2C 1-6 -alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted by -F;
[0280] -S(=O)2(3-14 membered cycloalkyl), which is saturated and unsubstituted;
[0281] -C 1-6 -alkyl, which is saturated, unsubstituted, mono- or di-substituted independently of one another by substituents selected from the group consisting of OH, -OC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, unsubstituted-phenyl;
[0282] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered cycloalkyl is saturated, unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of: C 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl;
[0283] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is selected in each case from azetidine, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabis[c]pyrrole ...pyrrolo[1,2-a]pyrazine, 8-azabis[c]pyrrole, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, cyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolazine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -OH, =O, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -S(=O)2C 1-6 -alkyl, oxetane, pyrimidinyl, -C 1-6 -alkylene-phenyl;
[0284] unsubstituted-phenyl;
[0285] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, which are in each case unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of: -C 1-6 -alkyl, -OH.
[0286] 24. A compound according to any of the preceding statements, wherein
[0287] R 3 represents -H; and
[0288] R 4 express
[0289] -H;
[0290] -S(=O)2C 1-6 -alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted by -F;
[0291] -S(=O)2(3-14 membered cycloalkyl), which is saturated and unsubstituted;
[0292] -C 1-6 -alkyl, which is saturated, unsubstituted, mono- or di-substituted independently of one another by substituents selected from the group consisting of: -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-3 -alkyl, -C(=O)-N(C 1-3 -alkyl)2 or unsubstituted-phenyl;
[0293] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered cycloalkyl is saturated, unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of: C 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl;
[0294] 3-14 membered heterocycloalkyl or -C 1-6-alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is selected in each case from azetidine, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabis[c]pyrrole ...pyrrolo[1,2-a]pyrazine, 8-azabis[c]pyrrole, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, cyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolazine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -OH, =O, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -S(=O)2C 1-6 -alkyl, oxetane, pyrimidinyl, -C 1-6 -alkylene-phenyl;
[0295] unsubstituted-phenyl;
[0296] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, which are in each case unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of: -C 1-6 -alkyl, -OH.
[0297] 25. A compound according to any of the preceding statements, wherein R 3 and R 4 Together they form a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted.
[0298] 26. A compound according to any of the preceding statements, wherein R 3 and R 4 together form a heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine and piperazine, which are in each case unsubstituted, independently of one another, monosubstituted or polysubstituted by substituents selected from the group consisting of: C 1-6 -alkyl, -NH2, -NHCH3, -N(CH3)2, -C(=O)NH-C 1-6 -alkyl, -C(=O)N(C 1-6 -alkyl)2, -C(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, unsubstituted-pyridyl and unsubstituted or substituted-C 1-6 -alkyl monosubstituted 1,2,4-oxadiazole.
[0299] 27. A compound according to any of the preceding statements, wherein R 3 and R 4 Together
[0300] a pyrrolidine ring, which is unsubstituted or monosubstituted with -N(CH3)2;
[0301] a piperidine ring which is unsubstituted or monosubstituted with a substituent selected from the group consisting of: -C 1-6 -alkyl, -NH2, -N(CH3)2, -C(=O)NH-C 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl and unsubstituted or substituted-C 1-6 -alkyl monosubstituted 1,2,4-oxadiazole;
[0302] a morpholine ring, which is unsubstituted; or
[0303] A piperazine ring which is unsubstituted or N-substituted with a substituent selected from the group consisting of: -C 1-6 -alkyl and unsubstituted-pyridyl.
[0304] 28. A compound according to any of the preceding statements, wherein R 3 and R4 Together with the nitrogen atom to which it is attached, it forms a residue selected from the group consisting of:
[0305]
[0306] 29. A compound according to any one of the preceding statements, wherein W represents
[0307] 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or disubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or disubstituted;
[0308] 6-14 membered aryl, which is unsubstituted, monosubstituted or disubstituted;
[0309] 3-14 membered heterocycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or disubstituted;
[0310] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or disubstituted; or
[0311] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or disubstituted.
[0312] 30. A compound according to any one of the preceding statements, wherein W represents
[0313] 3-14-membered saturated cycloalkyl, 5-14-membered cycloalkenyl, 8-14-membered cycloalkynyl, which are unsubstituted, monosubstituted or disubstituted; preferably 3-12-membered saturated cycloalkyl, 5-12-membered cycloalkenyl, 8-12-membered cycloalkynyl, which are unsubstituted, monosubstituted or disubstituted; preferably 3-10-membered saturated cycloalkyl, 5-10-membered cycloalkenyl, 8-10-membered cycloalkynyl, which are unsubstituted, monosubstituted or disubstituted; preferably 3-8-membered saturated cycloalkyl, 5-8-membered cycloalkenyl, 8-membered cycloalkynyl, which are unsubstituted, monosubstituted or disubstituted;
[0314] 6-14 membered aryl, which is unsubstituted, monosubstituted or disubstituted;
[0315] 3-14 membered heterocycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or disubstituted;
[0316] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or disubstituted; or
[0317] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or disubstituted.
[0318] 31. A compound according to any one of the preceding statements, wherein W represents
[0319] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatically unsaturated, unsubstituted, monosubstituted or polysubstituted by substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6-alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl;
[0320] 6-14 membered aryl, which is unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6-alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl;
[0321] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl;
[0322] 5-14 membered heteroaryl, which is unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6-alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl; or
[0323] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl.
[0324] 32. A compound according to any one of the preceding statements, wherein W represents
[0325] 3-10 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl, specifically 3-10 membered cycloalkyl, which is saturated or non-aromatically unsaturated, unsubstituted, mono- or poly-substituted by substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6-alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl; or
[0326] 6-12 membered aryl, which is unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl;
[0327] 3-10 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6-alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl;
[0328] 5-10 membered heteroaryl, which is unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6-alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl; or
[0329] -C1-C6-alkyl, which is unsubstituted, monosubstituted or polysubstituted by substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl.
[0330] 33. A compound according to any one of the preceding statements, wherein W represents
[0331] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatically unsaturated, unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2,
[0332] 6-14 membered aryl, which is unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0333] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6-alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0334] 5-14 membered heteroaryl, which is unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2; or
[0335] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2.
[0336] 34. A compound according to any one of the preceding statements, wherein W represents
[0337] 3-10 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or disubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2,
[0338] 6-14 membered aryl, which is unsubstituted, independently selected from the following mono- or polysubstituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6-alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0339] 3-10 membered heterocycloalkyl, which is saturated, unsubstituted, mono- or di-substituted independently selected from: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0340] 5-10 membered heteroaryl, which is unsubstituted, independently selected from the following mono- or di-substituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6-alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2; or
[0341] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or disubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OH, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2.
[0342] 35. A compound according to any of the preceding statements, wherein R 5 and R 5 'Independently express
[0343] -H;
[0344] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0345] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0346] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0347] 36. A compound according to any of the preceding statements, wherein n is an integer selected from 1, 2 or 3, and
[0348] R 5 and R 5 'Independently express
[0349] -H;
[0350] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0351] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0352] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0353] 37. A compound according to any of the preceding statements, wherein R 5 and R 5 ' independently of one another represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2.
[0354] 38. A compound according to any of the preceding statements, wherein R 6 、R 7 and R 8 Independently express
[0355] -H;
[0356] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;
[0357] -C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0358] -OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0359] -NHC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0360] -N(C 1-6 -alkyl) 2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0361] -C(=O)OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0362] -OC(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0363] -C 1-6 - heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0364] 39. A compound according to any of the preceding statements, wherein R 6 、R 7 and R 8 Independently express
[0365] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2,
[0366] -C 1-6 -alkyl, -CF3, -CHF2, -CH2F,
[0367] -OC 1-6 -alkyl, -OCF3, -OCHF2, -OCH2F,
[0368] -NHC 1-6-alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;
[0369] -N(C 1-6 -alkyl)2, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;
[0370] -C(=O)OC 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;
[0371] -OC(=O)C 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; or
[0372] -C 1-6 -heteroalkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2.
[0373] 40. A compound according to any of the preceding statements, wherein R 6 represents -H, -F, -Cl, -CN or -C1-C6-alkyl.
[0374] 41. A compound according to any of the preceding statements, wherein R 6 -H is not indicated.
[0375] 42. A compound according to any of the preceding statements, wherein R 7 represents -H, -F, -Cl, -CN or -C1-C6-alkyl.
[0376] 43. A compound according to any of the preceding statements, wherein R 7 -H is not indicated.
[0377] 44. A compound according to any of the preceding statements, wherein R 8 represents -H, -F, -Cl, -CN or -C1-C6-alkyl.
[0378] 45. A compound according to any of the preceding statements, wherein R 8 -H is not indicated.
[0379] 46. A compound according to any of the preceding statements, wherein
[0380] (i)R 6 、R 7 and R 8 each represents -H; or
[0381] (ii)R 6 、R 7 and R 8 The two in the table represent -H, and R 6 、R 7 and R 8 The other of represents -F, -Cl, -CN or -CH3; or
[0382] (iii)R 6 、R 7 and R 8 One of them represents -H, and R 6 、R 7 and R 8 The other of them independently represent -F, -Cl, -CN or -CH3.
[0383] 47. A compound according to any of the preceding statements, selected from the group consisting of Cpd 001 to Cpd 152 as mentioned herein and physiologically acceptable salts thereof.
[0384] 48. A compound according to any of the preceding statements, wherein
[0385] R 1 represents H, -CH2F, -CHF2 or -CF3;
[0386] R2 represents H;
[0387] R 3 Indicates -H;
[0388] R 4 express
[0389] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0390] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0391] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0392] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0393] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0394] or R 3 and R 4 together forming a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0395] R 5 and R 5'Independently represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2;
[0396] R 6 、R 7 and R 8 independently of one another represent -H, -F, -Cl, -CN or -C1-C6-alkyl;
[0397] W stands for
[0398] 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted;
[0399] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0400] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0401] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0402] -C1-C6-alkyl; which is unsubstituted, monosubstituted or polysubstituted.
[0403] 49. A compound according to any of the preceding statements, wherein
[0404] R 1 represents H, -CH2F, -CHF2 or -CF3;
[0405] R2 represents H;
[0406] R 3 Indicates -H;
[0407] R 4 express
[0408] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0409] 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted; wherein each of the 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl is optionally linked through -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0410] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0411] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0412] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0413] or R 3 and R 4 together forming a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0414] R 5 and R 5 'Independently represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2;
[0415] R 6 、R 7 and R 8 independently of one another represent -H, -F, -Cl, -CN or -C1-C6-alkyl;
[0416] W stands for
[0417] 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted;
[0418] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0419] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0420] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0421] -C1-C6-alkyl; which is unsubstituted, monosubstituted or polysubstituted.
[0422] 50. A compound according to any of the preceding statements, wherein
[0423] R 1 represents H, -CH2F, -CHF2 or -CF3;
[0424] R 3 Indicates -H;
[0425] R 4 express
[0426] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0427] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0428] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0429] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0430] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0431] or R 3 and R 4 together forming a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0432] R 5 and R 5 'Independently represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2;
[0433] R 6 、R 7 and R 8 independently of one another represent -H, -F, -Cl, -CN or -C1-C6-alkyl;
[0434] W stands for
[0435] 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted;
[0436] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0437] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0438] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0439] -C1-C6-alkyl; which is unsubstituted, monosubstituted or polysubstituted.
[0440] 51. A compound according to any of the preceding statements, wherein
[0441] R 1 represents H, -CH2F, -CHF2 or -CF3;
[0442] R 3 Indicates -H;
[0443] R 4 express
[0444] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0445] 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted; wherein each of the 3-14 membered cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl is optionally linked through -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0446] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0447] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0448] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0449] or R 3 and R 4 together forming a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0450] R 5 and R 5 'Independently represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2;
[0451] R 6 、R 7 and R 8 independently of one another represent -H, -F, -Cl, -CN or -C1-C6-alkyl;
[0452] W stands for
[0453] 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted;
[0454] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0455] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0456] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0457] -C1-C6-alkyl; which is unsubstituted, monosubstituted or polysubstituted.
[0458] 52. A pharmaceutical composition or medicament comprising a compound according to any one of the preceding statements.
[0459] 53. A compound according to any of the preceding statements or a pharmaceutical composition according to statement 52 for use as a medicament.
[0460] 54. A compound according to any preceding statement or a pharmaceutical composition according to statement 52 for use in the treatment of pain or epilepsy; preferably, pain and epileptic encephalopathy.
[0461] 55. The compound for use or pharmaceutical composition for use of statement 54, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain.
[0462] 56. The compound for use or pharmaceutical composition for use of statement 55, wherein the pain is postoperative pain.
[0463] 57. A method for preventing and / or treating a TRPM3-mediated disorder, the method comprising administering to a subject an effective amount of a compound according to any one of statements 1 to 51 or a pharmaceutical composition according to claim 52.
[0464] 58. A method for preventing and / or treating pain or epilepsy; such as epileptic encephalopathy, comprising administering to a subject an effective amount of a compound according to any one of statements 1 to 51 or a pharmaceutical composition according to claim 52.
[0465] 59. The method of statement 58 wherein the pain is selected from the group consisting of nociceptive pain, inflammatory pain, and neuropathic pain.
[0466] The first aspect of the present invention is to provide a compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph
[0467]
[0468] in
[0469] R 1 Indicates -F, -Cl, -Br, -I, -CN, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2RW 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;
[0470] Q means -OR 2 or -NR 3 R 4 ;
[0471] R 3 Indicates -OH or -R Y1 ;
[0472] R 4 Indicates -R Y2 or -S(=O)2R Y3 ;
[0473] or R 3 and R 4 together forming a 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted;
[0474] T represents -O-, and U represents -(CR 5 R 5 ') n -; or T represents -(CR 5 R 5 ') n -, and U represents -O-;
[0475] n is an integer selected from 1, 2, 3, 4 or 5;
[0476] R 5 and R 5 'Independently represent -R Y4 ;
[0477] R 6 、R 7 and R 8 Independently represent -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)RW 、-C(=O)OR W or -C(=O)NR W R X ;
[0478] W stands for
[0479] 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted;
[0480] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted;
[0481] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted;
[0482] 5-14 membered heteroaryl, which is mono- or polysubstituted; or
[0483] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted;
[0484] in
[0485] R W and R X Independently of each other, expressed independently in each case
[0486] -H;
[0487] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0488] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0489] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0490] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0491] R Y1 、R Y2 、R Y3 、R Y4 and R Y5 Independently of each other, expressed independently in each case
[0492] -H;
[0493] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0494] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0495] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0496] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0497] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0498] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0499] and wherein "mono- or polysubstituted" independently in each case means substituted by one or more substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-C 1-6 -alkyl, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -C(=O)-NH(OH), -C 1-6 -alkylene-C(=O)-NH(OH), -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6-alkyl, -OC 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-NH2, -OC 1-6 -alkylene-NH-C 1-6 -alkyl, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-OC 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OC(=O)-NH(C 1-6 -alkyl), -OC(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OC(=O)-N(C 1-6 -alkyl)2, -OS(=O)2-NH2, -C 1-6 -alkylene-OS(=O)2-NH2, -OS(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OS(=O)2-NH(C 1-6 -alkyl), -OS(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OS(=O)2-N(C 1-6 -alkyl)2, -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6-alkyl, -NH-C(=O)-NH2, -C 1-6 -alkylene-NH-C(=O)-NH2, -NH-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-C(=O)-NH(C 1-6 -alkyl), -NH-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C(=O)-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH2, -N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-OC 1-6 -alkyl, -NH-S(=O)2-NH2, -C 1-6-alkylene-NH-S(=O)2-NH2, -NH-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-S(=O)2-NH(C 1-6 -alkyl), -NH-S(=O)2N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-S(=O)2N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)-C 1-6 -alkyl, -S(=O)2-C1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(═O)-(3- to 14-membered cycloalkyl), -C(═O)-(3- to 14-membered heterocycloalkyl), -C(═O)-phenyl, -C(═O)-(5- to 14-membered heteroaryl), -S(═O)2-(3- to 14-membered cycloalkyl), -S(═O)2-(3- to 14-membered heterocycloalkyl), -S(═O)2-phenyl, or -S(═O)2-(5- to 14-membered heteroaryl);
[0500] or the compound is ethyl 5-methoxy-2-methyl-1-benzothiophene-3-carboxylate;
[0501] wherein the compound is not:
[0502] 5-Benzyloxybenzo[b]thiophene-3-carboxylic acid.
[0503] In some embodiments, Q represents -NR 3 R 4 .
[0504] In some embodiments, Q represents -OR 2 .
[0505] In some embodiments, T represents -O-, U represents -(CR 5 R 5 ') n -; and n is an integer selected from 1, 2 or 3.
[0506] In some embodiments, R 1 express
[0507] -H, -F, -Cl, -Br, -I, CN;
[0508] -C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0509] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0510] -OH;
[0511] -OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0512] -NH2;
[0513] NHC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0514] -N(C 1-6 -alkyl) 2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0515] -NHC(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0516] -NC 1-6 -alkylC(=O)C 1-6 - alkyl, which is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0517] -SH;
[0518] -SC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0519] -C(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0520] -C(=O)OC 1-6- alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0521] -C(=O)NH2;
[0522] -C(=O)NHC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0523] -C(=O)N(C 1-6 -alkyl) 2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0524] -S(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0525] -S(=O)2-C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0526] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0527] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0528] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0529] In some embodiments, R 1 express
[0530] -H, -F, -Cl, -Br, -I, CN;
[0531] -C 1-6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0532] -C1-C6-heteroalkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0533] -OH;
[0534] -OC 1-6 -alkyl, -O-C2-C6-alkenyl, -O-C2-C6-alkynyl, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6-alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0535] -NH2;
[0536] -NHC 1-6 -alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6-alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0537] -N(C 1-6 -alkyl) 2, which is in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0538] -NHC(=O)C 1-6-alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0539] -NC 1-6 -alkylC(=O)C 1-6 -alkyl, which is in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6-alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0540] -SH;
[0541] -SC 1-6 -alkyl, -S-C2-C6-alkenyl, -S-C2-C6-alkynyl, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6-alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0542] -C(=O)C 1-6 -alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6-alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0543] -C(=O)OC 1-6 -alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0544] -C(=O)NH2;
[0545] -C(=O)NHC 1-6 -alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0546] -C(=O)N(C 1-6 -alkyl) 2, which is in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0547] -S(=O)C 1-6 -alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6-alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0548] -S(=O)2-C 1-6 -alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0549] -C1-C6-heteroalkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;; or
[0550] 3-14 membered cycloalkyl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0551] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2.
[0552] In some embodiments, R 1 Indicates -H, -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, -OH, -OC 1-6 -alkyl, -SH, -NH2, -C 1-6-alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)C 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)NHC 1-6 -alkyl, -C(=O)N(C 1-6 -alkyl)2, -S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -OC 1-6 -alkyl, unsubstituted 3-14 membered cycloalkyl or unsubstituted 3-14 membered heterocycloalkyl. 1 Indicates -H, -F, -Cl, -Br, -I, CN, -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, -OH, -OC 1-6 -alkyl, -SH, -NH2, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)C1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)NHC 1-6 -alkyl, -C(=O)N(C 1-6 -alkyl)2, -S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -OC 1-6 -alkyl, unsubstituted-cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl.
[0553] In some embodiments, R 1 Indicates -H, CN, -C 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -CH2F, -CHF2, -CF3, -C(=O)NH2, unsubstituted-cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl. Preferably, R 1 represents -H, -CH2F, -CHF2, -CF3, -C(=O)NH2, -CN, unsubstituted-cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl. Preferably, R 1 Indicates H, -C 1-6 -alkyl, -C(=O)NH2, -CHF2, unsubstituted-cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl.
[0554] Preferably, R 1 Indicates -H, -CN, -C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C(=O)NH2 or -C 1-3 -alkylene-CFH2; more specifically -H, -CH3 or -CF2H,.
[0555] In some embodiments, R 2 express
[0556] -H;
[0557] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0558] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0559] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0560] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0561] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0562] In some embodiments, R 2 express
[0563] -H;
[0564] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6-alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0565] -C1-C6-heteroalkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0566] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6-alkyl) 2, in particular 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0567] 3-14 membered heterocycloalkyl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0568] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2; or
[0569] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6-alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2.
[0570] In some embodiments, R 2 express
[0571] -H;
[0572] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0573] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0574] In some embodiments, R 2 Indicates -H, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-C(=O)-NH2, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3. Preferably, R 2 Indicates -H, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3. Preferably, R 2 represents -H or saturated, unsubstituted or monosubstituted -C 1-6 -alkyl. Preferably, R 2 Indicates -H.
[0575] In some embodiments, R 2 Indicates -H, -C 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C1-6 -alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3.
[0576] In some embodiments, R 2 Indicates -H or -C 1-6 -alkyl.
[0577] In some embodiments, Q represents -OR 2 ; and R 1 Indicates -C 1-6 -alkyl, -CH2F, -CHF2 or -CF3.
[0578] In some embodiments, R 3 express
[0579] -H;
[0580] -OH;
[0581] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0582] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0583] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0584] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0585] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0586] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0587] In some embodiments, R 3 express
[0588] -H;
[0589] -OH;
[0590] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6-alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0591] -C1-C6-heteroalkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0592] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, in particular 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6-alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0593] 3-14 membered heterocycloalkyl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2;
[0594] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2; or
[0595] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2.
[0596] In some embodiments, R 3 express
[0597] -H;
[0598] -OH;
[0599] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0600] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0601] In some embodiments, R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-C(=O)-NH2, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3. Preferably, R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3. Preferably, R 3 represents -H, -OH or saturated, unsubstituted or monosubstituted -C 1-6 -alkyl. Preferably, R 3 Indicates -H.
[0602] In some embodiments, R 3 and R 4 Neither represents -H. In some embodiments, R 3 Indicates -H, and R 4 -H is not indicated.
[0603] In some embodiments, R 4 express
[0604] -H;
[0605] -S(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0606] -S(=O)2-C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0607] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0608] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0609] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0610] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0611] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or
[0612] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0613] Preferably, R 4 express
[0614] -S(=O)2C 1-6 -alkyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0615] -S(=O)2(3-14 membered cycloalkyl), wherein the 3-14 membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which are in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0616] -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, which are unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6-alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0617] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which are in each case saturated or unsaturated, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6-alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0618] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from the group consisting of azepane, 1,4-oxazepane, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxazolidine, morpholine, oxazolidine, oxetane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, Thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; which are in each case unsubstituted, monosubstituted or polysubstituted, independently of one another, by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6-alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0619] -phenyl, which is unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -CN, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6-alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0620] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of benzimidazole, benzisoxazole, benzoxazole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole , naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole and [1,2,4]triazolo[4,3-a]pyrimidine; which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -CN, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6-alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl.
[0621] Preferably, R 4 express
[0622] -H;
[0623] -S(=O)2C 1-6 -alkyl, which is mono- or polysubstituted by -F;
[0624] -S(=O)2(3-14 membered cycloalkyl), which is unsubstituted;
[0625] -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, which are each independently mono- or disubstituted by substituents selected from the group consisting of: -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-3 -alkyl, -C(=O)-N(C 1-3 -alkyl)2 or unsubstituted-phenyl;
[0626] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered cycloalkyl is saturated, unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of: C 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -OH, -OC 1-6 -alkyl, -NH2, -N(C 1-6-alkyl)2, -NHC(=O)OC 1-6 -alkyl;
[0627] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is selected in each case from azetidine, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabis[c]pyrrole ...pyrrolo[1,2-a]pyrazine, 8-azabis[c]pyrrole, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, cyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -OH, =O, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -S(=O)2C 1-6 -alkyl, oxetane, pyrimidinyl, -C 1-6 -alkylene-phenyl;
[0628] unsubstituted-phenyl;
[0629] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, which are in each case unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of: -C 1-6 -alkyl, -OH.
[0630] In some embodiments, R 4 express
[0631] A residue selected from the group consisting of:
[0632]
[0633] or
[0634] C1-C6-alkyl, which is unsubstituted, monosubstituted or polysubstituted; preferably represents the residue -CR'R"-(CH2) m -OH, wherein m is an integer selected from 1, 2, 3, 4, 5 or 6, preferably selected from 1, 2 or 3; and wherein R' and R" independently of each other represent -H, -C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C 1-3 -alkylene-CFH2, -C 1-3 -alkylene-OC 1-3 -alkyl, -C 1-3 -alkylene-OH, -C(=O)-NH2, -C(=O)-NH-C 1-3 -alkyl or -C(=O)-N(C 1-3 -alkyl) 2; preferably -H, -CH3, -C 1-3 -alkylene-OH, C(=O)-NH2, -C(=O)-NH-C 1-3 -alkyl or -C(=O)-N(C 1-3 -alkyl) 2. Preferably, at least R' or R" does not represent -H; preferably, neither R' or R" represents -H; preferably represents a residue selected from the group consisting of:
[0635]
[0636] or
[0637] 3-14 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-13 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-11 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably represents a cycloalkyl residue selected from the group consisting of:
[0638]
[0639]
[0640] or
[0641] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is linked via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-12 membered cycloalkyl is linked via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl wherein the 3-10 membered cycloalkyl is linked via a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably a 3-8 membered cycloalkyl is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-8 membered cycloalkyl is linked via a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; specifically a 3-14 membered cycloalkyl is saturated or non-aromatic aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is linked by -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-12 membered cycloalkyl is linked by -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl, which is saturated or non-aromatic, unsaturated, unsubstituted, mono- or polysubstituted; wherein the 3- to 10-membered cycloalkyl is linked via a -C1-C6-alkylene-group, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted; preferably a 3- to 8-membered cycloalkyl group, which is saturated or non-aromatic, unsaturated, unsubstituted, mono- or polysubstituted; wherein the 3- to 8-membered cycloalkyl is linked via a -C1-C6-alkylene-group, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted; preferably represents a residue selected from the group consisting of:
[0642] or
[0643] 3-14 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-13 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-11 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably represents a heterocycloalkyl residue selected from the group consisting of:
[0644]
[0645]
[0646] More preferably selected from the group consisting of:
[0647]
[0648]
[0649] or
[0650] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is linked through a -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably a 3-12 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-12 membered heterocycloalkyl is linked through a -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably a 3-10 membered heterocycloalkyl Cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-10 membered heterocycloalkyl is linked via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-8 membered heterocycloalkyl is linked via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably represents a residue selected from the group consisting of:
[0651]
[0652] or
[0653] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 6-12 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 6-10 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 6-8 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; or
[0654] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is attached via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 6-12 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-12 membered aryl is attached via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 6-10 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-10 membered aryl is attached via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably represents a residue selected from the group consisting of:
[0655]
[0656] or
[0657] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-12 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-10 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-9 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably represents a residue selected from the group consisting of:
[0658]
[0659]
[0660] More preferably represents a residue selected from the group consisting of:
[0661]
[0662] or
[0663] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is linked via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 5-12 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-12 membered heteroaryl is linked via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 5-10 membered heteroaryl Aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-10 membered heteroaryl is attached via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 5-8 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-8 membered heteroaryl is attached via -C1-C6-alkylene-, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably represents a residue selected from the group consisting of:
[0664]
[0665] In some embodiments, R 4 represents a residue according to formula (A),
[0666]
[0667] in
[0668] m A is 0 or 1;
[0669] Y A Selected from -O-, -NR A6 -and-CR A7 R A8 -;and
[0670] R A1 、R A2 、R A3 、R A4 、R A5 、R A6 、R A7 and R A8 represents -H, -F, -C independently of each other 1-3 -alkyl, -C 1-3 -alkylene-OH, -C 1-3 -alkylene-NH2, -C 1-3 -alkylene-NH(C 1-3 -alkyl), -C 1-3 -alkylene-N(C 1-3 -alkyl)2, -C 1-3 -alkylene-NH(C 1-3-alkylene-CF3), -C 1-3 -alkylene-C(=O)NH2, -C 1-3 -alkylene-NH-C(=O)OC 1-4 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-3 -alkyl, -C(=O)-N(C 1-3 -alkyl) 2 or -3-oxetane; or R A7 and R A8 Together with the carbon atom to which it is attached, it forms a ring and represents -CH2OCH2-, -CH2OCH2CH2-, or -CH2CH2OCH2CH2-, -CH2NHCH2-, -CH2NHCH2CH2-, or -CH2CH2NHCH2CH2-.
[0671] In some embodiments, R 4 represents a residue according to general formula (A) as defined above, wherein
[0672] m A is 0 or 1;
[0673] Y A Selected from -O- and -CR A7 R A8 -;and
[0674] R A1 、R A2 、R A3 、R A4 、R A5 、R A7 and R A8 represent -H, -C independently of each other 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C 1-3 -alkyl)2 or -C(=O)NH2; preferably with the condition that R A1 、R A2 、R A3 、R A4 、R A5 、R A7 and R A8 Only one of represents a residue other than -H.
[0675] In some embodiments, R 4 represents a residue according to general formula (A) as defined above, wherein
[0676] m A is 0 or 1;
[0677] Y A Selected from -O- and -CR A7R A8 -;and
[0678] R A1 Indicates -C 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C 1-3 -alkyl)2 or -C(=O)NH2; and
[0679] R A2 、R A3 、R A4 、R A5 、R A7 and R A8 Indicates -H.
[0680] In some embodiments, R 4 represents a residue according to formula (B),
[0681]
[0682] in
[0683] Y B Selected from -O-, -NR B8 -and-CR B9 R B10 -;and
[0684] R B1 、R B2 、R B3 、R B4 、R B5 、R B6 、R B7 、R B8 、R B9 and R B10 independently represent -H, -F, -OH, -C(=O)-NH2, -C(=O)-NH-C 1-3 -alkyl, -C(=O)-N(C 1-3 -alkyl)2, -C 1-3 -alkyl, -C 1-3 -alkylene-OH, -C 1-3 -alkylene-OC 1-3 -alkyl, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CO2H or -C 1-3 -alkylene-C(=O)OC 1-3 -alkyl; or R B2 and R B3 Together they represent =O; or R B4 and R B5 Together they represent =O.
[0685] In some embodiments, R 4 represents a residue according to general formula (B) as defined above, wherein
[0686] Y B Selected from -O- and -NR B8 -;and
[0687] R B1 、R B2 、R B3 、R B4 、R B5 、R B6 、R B7 、R B8 represents -H, -F, -C independently of each other 1-3 -alkyl, -C 1-3 -alkylene-OH, -C 1-3 -alkylene-CF3 or -C(=O)-NH2; or R B2 and R B3 Together they represent =O; or R B4 and R B5 Together they represent =O; preferably, the condition is R A1 、R A2 、R A3 、R A4 、R A5 、R A7 and R A8 Only 1, 2 or 3 of them represent residues other than -H; preferably with the proviso that R A1 、R A2 、R A3 、R A4 、R A5 、R A7 and R A8 At least one of represents a residue other than -H.
[0688] In some embodiments, R 4 represents a residue according to formula (C),
[0689]
[0690] in
[0691] Y C1 Selected from -O-, -S(=O)2-, -NR C8 -and-CR C9 R C10 -, and Y C2 Indicates -CR C11 R C12 -; or Y C1 Indicates -CRC9 R C10 -, and Y C2 Selected from -O-, -S(=O)2- and -NR C8 -;
[0692] R C1 、R C2 、R C3 、R C4 、R C5 、R C6 、R C7 、R C8 、R C9 、R C10 、R C11 and R C12 Independently express
[0693] -H, -F, -OH, -C(=O)OC 1-3 -alkyl, -NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2, -C 1-3 -alkyl, -C 1-3 -alkylene-OH, -C 1-3 -alkylene-CF3, -C(=O)-NH2, -C(=O)-NH-C 1-3 -alkyl or -C(=O)N-(C 1-3 -alkyl)2; or R C2 and R C3 Together they represent =O; or R C4 and R C5 Together they represent =O; or R C9 and R C10 Together they represent =O; or R C11 and R C12 Together they represent =O.
[0694] In some embodiments, R 4 represents a residue according to general formula (C) as defined above, wherein
[0695] Y C1 Selected from -O- or -NR C8 -, and Y C2 Indicates -CR C11 R C12 -; or Y C1 Indicates -CR C9 R C10 -, and Y C2 Selected from -O- and -NR C8 -;
[0696] R C1 、RC2 、R C3 、R C4 、R C5 、R C6 、R C7 、R C8 、R C9 、R C10 、R C11 and R C12 represents -H, -F, -C independently of each other 1-3 -alkyl, -C 1-3 -alkylene-OH or -C(=O)-NH2; preferably with the condition that R C1 、R C2 、R C3 、R C4 、R C5 、R C6 、R C7 、R C8 、R C9 、R C10 、R C11 and R C12 Only 1, 2 or 3 of them represent residues other than -H; preferably with the proviso that R C1 、R C2 、R C3 、R C4 、R C5 、R C6 、R C7 、R C8 、R C9 、R C10 、R C11 and R C12 At least one of represents a residue other than -H.
[0697] In some embodiments, R 4 express
[0698] (i) Residue -CR'R"-(CH2) m -OH, wherein m is an integer from 1 to 6, preferably from 1 to 3; and wherein R' and R" independently represent -H, -C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C 1-3 -alkylene-CFH2, -C 1-3 -alkylene-OC 1-3 -alkyl or -C 1-3 -alkylene-OH, preferably -H, -CH3 or -C 1-3-alkylene-OH. In a preferred embodiment, at least R' or R" does not represent -H. In a preferred embodiment, both R' and R" do not represent -H; or
[0699] (ii) a residue according to formula (D),
[0700]
[0701] in
[0702] m D and n D are independently 0, 1, 2 or 3; preferably with the condition that m D +n D ≤3;
[0703] Y D1 Selected from -O-, -S(=O)2-, -NR D8 -and-CR D9 R D10 -, and Y D2 Indicates -CR D11 R D12 -; or Y D1 Indicates -CR D9 R D10 -, and Y D2 Selected from -O-, -S(=O)2- and -NR D8 -;
[0704] R D1 、R D2 、R D3 、R D4 、R D5 、R D6 、R D7 、R D8 、R D9 、R D10 、R D11 and R D12 independently represent -H, -F, -OH, -C 1-3 -alkylene-OH, -C(=O)NH2, -C 1-3 -alkylene-C(O)NH2, -C(=O)OC 1-3 -alkyl, -NH2, -C 1-3 -alkylene-NH2, -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl)2, -NH(C 1-3 -alkylene-CF3), -C 1-3 -alkylene-OCH3, -C 1-3 -alkyl, -C 1-3-alkylene-CF3: or R D2 and R D3 Together they represent =O; or R D4 and R D5 Together they represent =O; or R D9 and R D10 Together they represent =O; or R D11 and R D12 Together they represent =O;
[0705] Preferably,
[0706] m D and n D are independently 0, 1, 2 or 3; preferably with the condition that m D +n D ≤3;
[0707] Y D1 Selected from -O-, -NR D8 -and-CR D9 R D10 -, and Y D2 Indicates -CR D11 R D12 -; or Y D1 Indicates -CR D9 R D10 -, and Y D2 Selected from -O- and -NR D8 -;
[0708] R D1 、R D2 、R D3 、R D4 、R D5 、R D6 、R D7 、R D8 、R D9 、R D10 、R D11 and R D12 independently represent -H, -F, -OH, -C 1-3 -alkylene-OH, -C(=O)NH2, -CH2NH2, -CH2N(CH3)2, -NHCH2CF3, -CH3 or -CH2CF3: or R D2 and R D3 Together they represent =O; or R D4 and R D5 Together they represent =O; or R D9 and R D10 Together they represent =O; or R D11 and R D12 Together they represent =O; preferably, the condition is R D1 、RD2 、R D3 、R D4 、R D5 、R D6 、R D7 、R D8 、R D9 、R D10 、R D11 and R D12 Only 1, 2 or 3 of them represent residues other than -H; preferably with the proviso that R D1 、R D2 、R D3 、R D4 、R D5 、R D6 、R D7 、R D8 、R D9 、R D10 、R D11 and R D12 At least one of represents a residue other than -H.
[0709] In some embodiments, R 4 represents a residue according to formula (A), (B), (C), (D) or a residue of formula -CR'R"-(CH2) as described herein m -OH residue.
[0710] In some embodiments, R 4 represents a residue selected from the group consisting of: -CH3,
[0711]
[0712] In some embodiments, R 3 is H, and R 4 Any embodiment described above.
[0713] In some embodiments, R 5 and R 5 'Independently express
[0714] -H;
[0715] - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0716] -C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0717] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0718] Preferably, R 5 and R 5 ' independently of one another represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2.
[0719] In some embodiments, R 5 and R 5 At least one of ' is not -H.
[0720] In some embodiments, R 5 and R 5 'Both are -H.
[0721] In a preferred embodiment, T represents -O-, and U represents -(CR 5 R 5 ') n , and the resulting portion -O-(CR 5 R 5 ') n - represents a residue selected from the group consisting of:
[0722]
[0723] In some embodiments, R 5 Indicates -H, and R 5 ' represents a residue selected from the group consisting of: -H, -C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C 1-3 -alkylene-CFH2 and -C 1-3 -alkylene-OH; preferably -H or C 1-3 -alkyl.
[0724] In some embodiments, R 6 、R 7 and R 8Independently express
[0725] -H;
[0726] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;
[0727] -C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0728] -OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0729] -NHC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0730] -N(C 1-6 -alkyl) 2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0731] -C(=O)OC 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0732] -OC(=O)C 1-6 - alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;
[0733] -C 1-6 - heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
[0734] In some embodiments, R 6 、R 7 and R 8 Independently express
[0735] -H;
[0736] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;
[0737] -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, which are in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6-alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0738] -OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0739] -NHC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6-alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0740] -N(C 1-6 -alkyl) 2, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0741] -C(=O)OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl;
[0742] -OC(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6-alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl
[0743] -C 1-6 -heteroalkyl, which is saturated or unsaturated, unsubstituted, mono- or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -NHC(=O)OC 1-6 -alkyl, -N(C 1-6-alkyl)C(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)NH2, -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14 membered heterocycloalkyl; and unsubstituted 5-14 membered heteroaryl.
[0744] Preferably, R 6 、R 7 and R 8 Independently express
[0745] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2,
[0746] -C 1-6 -alkyl, -CF3, -CHF2, -CH2F,
[0747] -OC 1-6 -alkyl, -OCF3, -OCHF2, -OCH2F,
[0748] -NHC 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;
[0749] -N(C 1-6-alkyl)2, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;
[0750] -C(=O)OC 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;
[0751] -OC(=O)C 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; or
[0752] -C 1-6 -heteroalkyl, which is unsubstituted or substituted by one or more substituents independently selected from the group consisting of: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2.
[0753] In some embodiments, R 6 、R 7 and R 8 represent, independently of one another, a residue selected from the group consisting of: -H, -F, -Cl, -Br, -I, -CN, C 1-3 -alkyl, -CF3, -CF2H and -CFH2; preferably -H or -F.
[0754] In some embodiments, R 6 represents -H, -F, -Cl, -CN or -C1-C6-alkyl.
[0755] In some embodiments, R 6represents a residue selected from the group consisting of: -H, -F, -Cl, -CN or -CH3; preferably -H, -F, -CN or -CH3.
[0756] In some embodiments, R 6 -H is not indicated.
[0757] In some embodiments, R 7 represents -H, -F, -Cl, -CN or -C1-C6-alkyl.
[0758] In some embodiments, R 7 -H is not indicated.
[0759] In some embodiments, R 7 represents a residue selected from the group consisting of: -H, -F, -Cl, -CN or CH3; preferably -H, -F, -Cl or -CH3.
[0760] In some embodiments, R 6 、R 7 and R 8 independently of one another represent a residue selected from the group consisting of -H; or
[0761]
[0762] In some embodiments, R 8 represents -H, -F, -Cl, -CN or -C1-C6-alkyl.
[0763] In some embodiments, R 8 -H is not indicated.
[0764] In some embodiments, R 8 represents a residue selected from the group consisting of: -H, -F, -Cl, -CN or CH3; preferably -F.
[0765] In some embodiments
[0766] (i)R 6 、R 7 and R 8 each represents -H; or
[0767] (ii)R 6 、R 7 and R 8 The two in the table represent -H, and R 6 、R 7 and R 8 The other of represents -F, -Cl, -CN or -CH3; or
[0768] (iii)R 6、R 7 and R 8 One of them represents -H, and R 6 、R 7 and R 8 The other of each independently represents -F, -Cl, -CN or -CH3.
[0769] In some embodiments, W represents
[0770] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-6 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the cycloalkyl is unsubstituted, monosubstituted or trisubstituted; preferably the cycloalkyl is unsubstituted, monosubstituted or disubstituted, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-6 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the cycloalkyl is unsubstituted, monosubstituted or trisubstituted; preferably the cycloalkyl is unsubstituted, monosubstituted or disubstituted;
[0771] 6-14 membered aryl which is unsubstituted, monosubstituted or polysubstituted; preferably 6-12 membered aryl which is unsubstituted, monosubstituted or polysubstituted; preferably 6-10 membered aryl which is unsubstituted, monosubstituted or polysubstituted; wherein the aryl is unsubstituted, monosubstituted or trisubstituted; preferably the aryl is unsubstituted, monosubstituted or disubstituted; or
[0772] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-6 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the heterocycloalkyl is unsubstituted, monosubstituted or trisubstituted; preferably the heterocycloalkyl is unsubstituted, monosubstituted or disubstituted;
[0773] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-12 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-10 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-9 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-8 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the heteroaryl is unsubstituted, monosubstituted or trisubstituted; preferably the heteroaryl is unsubstituted, monosubstituted or disubstituted;
[0774] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; wherein the alkyl, alkenyl or alkynyl is unsubstituted, monosubstituted or trisubstituted; preferably the alkyl, alkenyl or alkynyl is unsubstituted, monosubstituted or disubstituted.
[0775] In some embodiments, W represents
[0776] 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, 8-14 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered saturated cycloalkyl, 5-12 membered cycloalkenyl, 8-12 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered saturated cycloalkyl, 5-10 membered cycloalkenyl, 8-10 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered saturated cycloalkyl, 5-8 membered cycloalkenyl, 8 membered cycloalkynyl, which are unsubstituted, monosubstituted or polysubstituted; preferably 3-6 membered saturated cycloalkyl, 5-6 membered cycloalkenyl, which are unsubstituted, monosubstituted or polysubstituted; wherein the cycloalkyl is unsubstituted, monosubstituted or trisubstituted; preferably the cycloalkyl is unsubstituted, monosubstituted or disubstituted;
[0777] 6-14 membered aryl which is unsubstituted, monosubstituted or polysubstituted; preferably 6-12 membered aryl which is unsubstituted, monosubstituted or polysubstituted; preferably 6-10 membered aryl which is unsubstituted, monosubstituted or polysubstituted; wherein the aryl is unsubstituted, monosubstituted or trisubstituted; preferably the aryl is unsubstituted, monosubstituted or disubstituted; or
[0778] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-6 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the heterocycloalkyl is unsubstituted, monosubstituted or trisubstituted; preferably the heterocycloalkyl is unsubstituted, monosubstituted or disubstituted;
[0779] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-12 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-10 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-9 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-8 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the heteroaryl is unsubstituted, monosubstituted or trisubstituted; preferably the heteroaryl is unsubstituted, monosubstituted or disubstituted;
[0780] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; wherein the alkyl, alkenyl or alkynyl is unsubstituted, monosubstituted or trisubstituted; preferably the alkyl, alkenyl or alkynyl is unsubstituted, monosubstituted or disubstituted.
[0781] In some embodiments, W represents
[0782] 3-14 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-6 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; wherein the cycloalkyl is unsubstituted, monosubstituted or trisubstituted; preferably the cycloalkyl is unsubstituted, monosubstituted or disubstituted;
[0783] 6-14 membered aryl which is unsubstituted, monosubstituted or polysubstituted; preferably 6-12 membered aryl which is unsubstituted, monosubstituted or polysubstituted; preferably 6-10 membered aryl which is unsubstituted, monosubstituted or polysubstituted; wherein the aryl is unsubstituted, monosubstituted or trisubstituted; preferably the aryl is unsubstituted, monosubstituted or disubstituted; or
[0784] 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-6 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the heterocycloalkyl is unsubstituted, monosubstituted or trisubstituted; preferably the heterocycloalkyl is unsubstituted, monosubstituted or disubstituted;
[0785] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-12 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-10 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-9 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-8 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the heteroaryl is unsubstituted, monosubstituted or trisubstituted; preferably the heteroaryl is unsubstituted, monosubstituted or disubstituted;
[0786] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or disubstituted
[0787] wherein the substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl.
[0788] In some embodiments, W represents a 3-10 membered cycloalkyl group which is unsubstituted, monosubstituted or polysubstituted, a 6-12 membered aryl group which is unsubstituted, monosubstituted or polysubstituted, a 3-10 membered heterocycloalkyl group which is saturated or unsaturated, monosubstituted or polysubstituted, a 5-12 membered heteroaryl group which is monosubstituted or polysubstituted, a -C1-C6-alkyl group, a halo-C 1-6 alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; preferably W represents a 3-10 membered cycloalkyl group which is unsubstituted, monosubstituted or disubstituted, a 6-12 membered aryl group which is unsubstituted, monosubstituted or disubstituted, a 3-10 membered heterocycloalkyl group which is saturated or unsaturated, monosubstituted or disubstituted, a 5-12 membered heteroaryl group which is monosubstituted or disubstituted or -C1-C6-alkyl, a halogenated C 1-6alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, which are in each case unsubstituted, monosubstituted or disubstituted; preferably W represents 3-10 membered cycloalkyl, which is unsubstituted, monosubstituted or disubstituted, 6-12 membered aryl, which is unsubstituted, monosubstituted or disubstituted, 3-10 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or disubstituted, 5-12 membered heteroaryl, which is monosubstituted or disubstituted, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl and tert-butyl; pentyl, hexyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -CCl3, -C 1-6 -alkylene-CCl3 or -C 1-6 -alkylene-CF3.
[0789] In some embodiments, W represents
[0790] 3-14 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-13 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-11 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; preferably represents a cycloalkyl residue selected from the group consisting of:
[0791]
[0792]
[0793] 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 6-12 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 6-10 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 6-8 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; preferably represents a phenyl residue selected from the group consisting of:
[0794]
[0795] or
[0796] 3-14 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-13 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-11 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered heterocycloalkyl, which is saturated, unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably represents a heterocycloalkyl residue selected from the group consisting of:
[0797]
[0798]
[0799] More preferably selected from the group consisting of:
[0800]
[0801]
[0802] or
[0803] 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-12 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-10 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; preferably 5-9 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; more preferably represents a residue selected from the group consisting of:
[0804]
[0805]
[0806] More preferably represents a residue selected from the group consisting of:
[0807]
[0808] or
[0809] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6-alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl.
[0810] In some embodiments, the 5-14 membered heteroaryl group within the definition of W is selected from benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, pyrimidine, benzoimidazole, benzoisoxazole, benzodioxole, benzofuran, benzothiazole, benzothiophene, cinnoline, dibenzofuran, furan, thiophene, furazan, imidazole, imidazopyridine, indole, isobenzofuran, isoindole, isoquinoline, isoxazole, oxadiazole, oxazole, oxindole, pyrazine, pyrazole, pyridazine, pyridine , pyrimidine, pyrrole, quinoline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole and [1,2,4]triazolo[4,3-a]pyrimidine; which are in each case unsubstituted, monosubstituted or polysubstituted; preferably defined in the group consisting of furan, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, triazole, pyridine, isoquinoline, benzothiazole, pyridazine, pyrimidine, imidazopyridine; which are in each case unsubstituted, monosubstituted or polysubstituted; preferably defined in the group consisting of furan-2-yl, furan-3-yl, thiophene- 2-yl, thien-3-yl, pyrazol-5-yl, oxazol-5-yl, isoxazol-4-yl, thiazol-2-yl, thiazol-5-yl, 1,2,4-triazol-3-yl, 1,2,3-triazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, isoquinolin-1-yl, isoquinolin-5-yl, benzo[d]thiazol-2-yl, pyridazin-3-yl, pyrimidin-5-yl and imidazo[1,2-a]pyridin-6-yl, which are in each case unsubstituted, monosubstituted or polysubstituted.
[0811] In some embodiments, the 3-14 membered heterocycloalkyl group within the definition of W is selected from azepane, 1,4-oxazepane, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxazolidine, morpholine, oxazolidine, oxetane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2 -oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; which are in each case unsubstituted, monosubstituted or polysubstituted; preferably defined from the group consisting of azepane, azetidine, aziridine, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isoxazolidine, morpholine, oxazolidine, oxetane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetracycline substituted benzophenone, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; which are in each case unsubstituted, monosubstituted or polysubstituted; preferably defined as azepane, azetidine, aziridine, diazepane, dioxane, dioxolane, dithiolane, imidazolidine, isoxazolidine, morpholine, oxazolidine, oxetane, oxetane, oxirane, piperazine, piperazine, 1-yl, tetrahydrofuran-2-yl, tetrahydropyran-1-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, thiazolidine, thiolane and indoline, which are each unsubstituted, monosubstituted or polysubstituted.
[0812] In some embodiments, the 5-14 membered heteroaryl group within the definition of W represents a residue according to formula (E)
[0813]
[0814] in
[0815] Y E1 Indicates -N=, -NR E2 -, S, O, or -CR E3 =;Y E2 Indicates -N=, -NR E3 -, S, O, or -CR E4 =, and Y E3 Indicates -N=, -NR E4 -, S, O, or -CR E5 =; condition is Y E1 、Y E2 and Y E3 At least one of them is not -CR E3 =, -CR E4 = and -CR E5 = In another preferred embodiment, W represents a residue according to formula (E)
[0816] wherein YE1 represents -N=, -NRE2-, S or -CRE3=; YE2 represents -N=, -NRE3-, S or -CRE4=; and YE3 represents -N=, -NRE4-, S or -CRE5=; provided that at least one of YE1, YE2 and YE3 is not -CRE3=, -CRE4= and -CRE5=, respectively.
[0817] R E1 、R E2 、R E3 and R E4 independently of one another represent -H, -CH3, -CH2-cyclopropyl, -CH2CF3, -CH2CHF2 or -CF3; more specifically R E1 、R E2 、R E3 and R E4 independently represent -H, -CH3 or -CF3; preferably with the proviso that R E1 、R E2 、R E3 and R E4 Only one of represents a residue other than -H.
[0818] In some embodiments, the 5-14 membered heteroaryl group within the definition of W represents a residue according to the general formula (F')
[0819]
[0820] in
[0821] YF1 Indicates -N= or -CR F4 =; and Y F2 Indicates -N= or -CR F5 =; and Y F3 Indicates -N= or -CR F3 =; condition is Y F1 and Y F2 At least one of them is not -CR F4 = and -CR F5 =;
[0822] R F1 、R F2 、R F3 、R F4 and R F5 independently of one another represent -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl or -azetidinyl; preferably with the proviso that R F1 、R F2 、R F3 、R F4 and R F5 Only one of represents a residue other than -H.
[0823] In some embodiments, the 5-14 membered heteroaryl group within the definition of W represents a residue according to formula (F)
[0824]
[0825] in
[0826] Y F1 Indicates -N= or -CR F4 =; and Y F2 Indicates -N= or -CR F5 =; condition is Y F1 and Y F2 At least one of them is not -CR F4 = and -CR F5 =;
[0827] R F1 、R F2 、R F3 、R F4 and R F5 independently of one another represent -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl or -azetidinyl; preferably with the proviso that R F1 、R F2 、R F3 、R F4 and R F5 Only one of represents a residue other than -H.
[0828] In some embodiments, the 5-14 membered heteroaryl group within the definition of W represents a residue according to formula (G) or (H)
[0829]
[0830] where R G1 and R H1 is selected from the group consisting of: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, azetidinyl, -cyclopropyl, -O-cyclopropyl, and -CHF2; or wherein R G1 and R H1 Selected from the group consisting of: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl and azetidinyl.
[0831] In some embodiments, the 5-14 membered heteroaryl group within the definition of W represents a residue according to formula (G') or (H')
[0832]
[0833] where R G1 and R H1 is selected from the group consisting of: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, azetidinyl, -cyclopropyl, -O-cyclopropyl, and -CHF2; or wherein R G1 and R H1 Selected from the group consisting of: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl and azetidinyl;
[0834] In some embodiments, 5-14 membered heteroaryl within the definition of W represents a residue according to formula (E), (F), (F'), (G), (H), (G'), or (H') as defined above.
[0835] In some embodiments, the term "mono- or poly-substituted" independently in each instance means substituted with one or more substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-C 1-6 -alkyl, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -C(=O)-NH(OH), -C 1-6 -alkylene-C(=O)-NH(OH), -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-OC 1-6 -alkyl, -OC 1-6 -alkylene-NH2, -OC 1-6 -alkylene-NH-C 1-6 -alkyl, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-OC 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -C 1-6-alkylene-OC(=O)-NH(C 1-6 -alkyl), -OC(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OC(=O)-N(C 1-6 -alkyl)2, -OS(=O)2-NH2, -C 1-6 -alkylene-OS(=O)2-NH2, -OS(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OS(=O)2-NH(C 1-6 -alkyl), -OS(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OS(=O)2-N(C 1-6 -alkyl)2, -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6 -alkyl, -NH-C(=O)-NH2, -C 1-6 -alkylene-NH-C(=O)-NH2, -NH-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-C(=O)-NH(C 1-6 -alkyl), -NH-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C(=O)-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6-alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH2, -N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-OC 1-6 -alkyl, -NH-S(=O)2-NH2, -C 1-6 -alkylene-NH-S(=O)2-NH2, -NH-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-S(=O)2-NH(C 1-6 -alkyl), -NH-S(=O)2N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-S(=O)2N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6-alkylene-S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(═O)-(3- to 14-membered cycloalkyl), -C(═O)-(3- to 14-membered heterocycloalkyl), -C(═O)-phenyl, -C(═O)-(5- to 14-membered heteroaryl), -S(═O)2-(3- to 14-membered cycloalkyl), -S(═O)2-(3- to 14-membered heterocycloalkyl), -S(═O)2-phenyl or -S(═O)2-(5- to 14-membered heteroaryl); preferably the terms independently in each case mean substituted by one or more substituents independently of one another selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -OH, -C1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-OC 1-6-alkyl, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -S(=O)2-(3- to 14-membered cycloalkyl), -S(=O)2-(3- to 14-membered heterocycloalkyl), -S(=O)2-phenyl or -S(=O)2-(5- to 14-membered heteroaryl); preferably, the terms independently in each case mean substituted by one or more substituents independently of one another selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C1-6 -alkyl)2, -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -S(=O)2-(3- to 14-membered cycloalkyl), -S(=O)2-(3- to 14-membered heterocycloalkyl), -S(=O)2-phenyl or -S(=O)2-(5- to 14-membered heteroaryl); preferably, the terms independently in each case mean substituted by one or more substituents independently of one another selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6-alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -NH2, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6-alkylene-NH-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -SH, -SC 1-6 -alkyl, -C 1-6 -alkylene-SC 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-12 membered cycloalkyl, -C 1-6 -alkylene-(3-12 membered cycloalkyl), 3 to 12 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 12 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 12-membered heteroaryl, -C 1-6 -alkylene-(5- to 12-membered heteroaryl); preferably the term independently in each case means substituted by one or more substituents independently of one another selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-NH-C 1-6 -alkylene-CF3, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6-alkylene-CF3, -C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -OC(=O)-C 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -NH2, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -SH, -SC 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-12 membered cycloalkyl, -C 1-6 -alkylene-(3-12 membered cycloalkyl), 3 to 12 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 12 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 12-membered heteroaryl, -C 1-6 -alkylene-(5- to 12-membered heteroaryl); preferably the term independently in each case means substituted by one or more substituents independently of one another selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-5 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-5 -alkylene-CF3, -C 1-5 -alkylene-NH-C1-5 -alkylene-CF3, -C(=O)OH, -C 1-5 -alkylene-C(=O)-OH, -C(=O)-OC 1-5 -alkyl, -C(=O)-NH2, -C(=O)-NH(C 1-5 -alkyl), C(=O)-N(C 1-5 -alkyl)2, -OH, -C 1-5 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-5 -alkyl, -OC(=O)-C 1-5 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -NH2, -NO2, -C 1-5 -alkylene-NH2, -NH(C 1-5 -alkyl), -C 1-5 -alkylene-NH(C 1-5 -alkyl), -N(C 1-5 -alkyl)2, -C 1-5 -alkylene-N(C 1-5 -alkyl)2, -N(C 1-5 -alkyl)-S(=O)2-C 1-5 -alkyl, -N(C 1-5 -alkyl)-S(=O)2-OC 1-5 -alkyl, -SH, -SC 1-5 Alkyl, -S(=O)2-C 1-5 Alkyl, -S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-10 membered cycloalkyl, -C 1-5 -alkylene-(3-10 membered cycloalkyl), 3 to 10 membered heterocycloalkyl, -C 1-5 -alkylene-(3 to 10 membered heterocycloalkyl), -phenyl, -C 1-5 -alkylene-phenyl, 5- to 10-membered heteroaryl, -C 1-5 -alkylene-(5- to 10-membered heteroaryl).
[0836] In some embodiments, the 3-14 membered cycloalkyl group within the definition of W is unsubstituted, monosubstituted, or disubstituted with a substituent selected from the group consisting of: -F, -Cl, -Br, -I, -CN, C 1-3-alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C 1-3 -alkylene-CFH 2、 -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-3 -alkyl, -C 1-3 -alkylene-OC 1-3 -alkyl and -C 1-3 -Alkylene-OH; preferably -F, -Cl, -Br, -I, -CN, -CH3, -CF3, -CF2H, -CFH2, -OCF3 and -OCH3.
[0837] In some embodiments, the 6-14 membered aryl group within the definition of W is unsubstituted, monosubstituted, or disubstituted with a substituent selected from the group consisting of: -F, -Cl, -Br, -I, -CN, C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C 1-3 -alkylene-CFH 2、 -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-3 -alkyl, -C 1-3 -alkylene-OC 1-3 -alkyl and -C 1-3 -Alkylene-OH; preferably -F, -Cl, -Br, -I, -CN, -CH3, -CF3, -CF2H, -CFH2, -OCF3 and -OCH3.
[0838] In some embodiments, the 5-14 membered heteroaryl group within the definition of W is unsubstituted, monosubstituted, or disubstituted with a substituent selected from the group consisting of: -F, -Cl, -Br, -I, -CN, C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C 1-3 -alkylene-CFH 2、 -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-3 -alkyl, -C 1-3-alkylene-OC 1-3 -alkyl and -C 1-3 -Alkylene-OH; preferably -F, -Cl, -Br, -I, -CN, -CH3, -CF3, -CF2H, -CFH2, -OCF3 and -OCH3.
[0839] In some embodiments, the -C1-C6-alkyl group within the definition of W is unsubstituted, monosubstituted, or disubstituted with a substituent selected from the group consisting of: -F, -Cl, -Br, -I, -CN, C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-3 -alkyl and -OH; preferably -F, -Cl, -Br, -I, -CN, -CH3, -CF3, -CF2H, -CFH2, -OCF3 and -OCH3.
[0840] In some embodiments, the 3-14 membered heterocycloalkyl group within the definition of W is unsubstituted, monosubstituted, or disubstituted with a substituent selected from the group consisting of: -F, -Cl, -Br, -I, -CN, C 1-3 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-3 -alkylene-CF3, -C 1-3 -alkylene-CF2H, -C 1-3 -alkylene-CFH 2、 -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-3 -alkyl, -C 1-3 -alkylene-OC 1-3 -alkyl and -C 1-3 -Alkylene-OH; preferably -F, -Cl, -Br, -I, -CN, -CH3, -CF3, -CF2H, -CFH2, -OCF3 and -OCH3.
[0841] In some embodiments of the invention, the compound is selected from the group consisting of:
[0842] Cpd 001-(2R)-2-{[5-(benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamido}propionamide;
[0843] Cpd 002-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propionamide;
[0844] Cpd 003-(2R)-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propionamide;
[0845] Cpd 004-(2R)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propionamide;
[0846] Cpd 005-(2R)-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propionamide;
[0847] Cpd 006-(2R)-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propionamide;
[0848] Cpd 007-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propionamide;
[0849] Cpd 008-(2S)-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0850] Cpd 009-(2S)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propanamide;
[0851] Cpd 010-(2S)-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide;
[0852] Cpd 011-(2S)-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0853] Cpd 012-(2S)-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0854] Cpd 013-5-(Benzyloxy)-2-(difluoromethyl)-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide;
[0855] Cpd 014-5-(Benzyloxy)-2-(difluoromethyl)-N-(2-hydroxy-2-methylpropyl)-1-benzothiophene-3-carboxamide;
[0856] Cpd 015-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-4-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0857] Cpd 016-(2S)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0858] Cpd 017-(2R)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0859] Cpd 018-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0860] Cpd 019-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0861] Cpd 020-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amino}oxolane-3-carboxamide;
[0862] Cpd 021-4-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-amino}oxane-4-carboxamide;
[0863] Cpd 022-N-[1-(Hydroxymethyl)cyclopropyl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0864] Cpd 023-N-[1-(Hydroxymethyl)cyclobutyl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0865] Cpd 024-N-[4-(Hydroxymethyl)oxan-4-yl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0866] Cpd 025-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0867] Cpd 026-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-amino}oxetane-3-carboxamide;
[0868] Cpd 027-(2S)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0869] Cpd 028-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0870] Cpd 029-(2R)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propionamide;
[0871] Cpd 030-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0872] Cpd 031-2-methyl-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0873] Cpd 032-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0874] Cpd 033-4-{2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-amino}oxane-4-carboxamide;
[0875] Cpd 034-N-[1-(Hydroxymethyl)cyclopropyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0876] Cpd 035-N-[1-(Hydroxymethyl)cyclobutyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0877] Cpd 036-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0878] Cpd 037-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0879] Cpd 038-3-{2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-amino}oxetane-3-carboxamide;
[0880] Cpd 039-N-(3,3-difluorocyclobutyl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0881] Cpd 040-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide;
[0882] Cpd 041-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(2-oxopyrrolidin-3-yl)-1-benzothiophene-3-carboxamide;
[0883] Cpd 042-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0884] Cpd 043-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide;
[0885] Cpd 044-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide;
[0886] Cpd 045-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0887] Cpd 046-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[(5-oxopyrrolidin-2-yl)methyl]-1-benzothiophene-3-carboxamide;
[0888] Cpd 047-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0889] Cpd 048-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-1-benzothiophene-3-carboxamide;
[0890] Cpd 049-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxylic acid;
[0891] Cpd 050-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamido}-3-hydroxypropionamide;
[0892] Cpd 051-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-3-hydroxypropionamide;
[0893] Cpd 052-(2S)-3-hydroxy-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0894] Cpd 053-(2S)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propionamide;
[0895] Cpd 054-(2S)-3-hydroxy-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide;
[0896] Cpd 055-5-[(2-fluorophenyl)methoxy]-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-1-benzothiophene-3-carboxamide;
[0897] Cpd 056-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-3-hydroxypropionamide;
[0898] Cpd 057-(2R)-3-hydroxy-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0899] Cpd 058-(2R)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propionamide;
[0900] Cpd 059-5-[(2-fluorophenyl)methoxy]-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-1-benzothiophene-3-carboxamide;
[0901] Cpd 060-5-(Benzyloxy)-2-methyl-N-[(3S)-2-oxopyrrolidin-3-yl]-1-benzothiophene-3-carboxamide;
[0902] Cpd 061-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamido}-2-methylpropanamide;
[0903] Cpd 062-2-{[5-(Benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamido}-2-methylpropionamide;
[0904] Cpd 063-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-2-methylpropanamide;
[0905] Cpd 064-2-methyl-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0906] Cpd 065-2-methyl-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propionamide;
[0907] Cpd 066-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-2-methylpropanamide;
[0908] Cpd 067-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxan-4-yl)methoxy]-1-benzothiophen-3-yl}formamido)propionamide;
[0909] Cpd 068-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxetan-3-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide;
[0910] Cpd 069-5-(cyclopropylmethoxy)-N-(1,3-dihydroxy-2-methylprop-2-yl)-2-methyl-1-benzothiophene-3-carboxamide;
[0911] Cpd 070-4-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-amino}oxane-4-carboxamide;
[0912] Cpd 071-4-{2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-amino}oxane-4-carboxamide;
[0913] Cpd 072-4-{5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-amino}oxane-4-carboxylic acid;
[0914] Cpd 073-5-(Benzyloxy)-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide;
[0915] Cpd 074-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide;
[0916] Cpd 075-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0917] Cpd 076-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0918] Cpd 077-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-1-benzothiophene-3-carboxamide;
[0919] Cpd 078-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0920] Cpd 079-N-[1-(Hydroxymethyl)cyclobutyl]-5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide;
[0921] Cpd 080-5-(Benzyloxy)-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide;
[0922] Cpd 081-5-[(2-fluorophenyl)methoxy]-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide;
[0923] Cpd 082-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0924] Cpd 083-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0925] Cpd 084-N-[4-(hydroxymethyl)oxan-4-yl]-5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide;
[0926] Cpd 085-5-[(2-fluorophenyl)methoxy]-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-1-benzothiophene-3-carboxamide;
[0927] Cpd 086-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0928] Cpd 087-3-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-amino}oxetane-3-carboxamide;
[0929] Cpd 088-3-{2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-amino}oxetane-3-carboxamide;
[0930] Cpd 089-5-(Benzyloxy)-N-(3,3-difluorocyclobutyl)-2-methyl-1-benzothiophene-3-carboxamide;
[0931] Cpd 090-N-(3,3-difluorocyclobutyl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0932] Cpd 091-5-(Benzyloxy)-2-methyl-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide;
[0933] Cpd 092-2-methyl-N-(1-methyl-1H-pyrazol-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0934] Cpd 093-5-[(2-fluorophenyl)methoxy]-2-methyl-N-(2-oxopyrrolidin-3-yl)-1-benzothiophene-3-carboxamide;
[0935] Cpd 094-2-methyl-N-(2-oxopyrrolidin-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0936] Cpd 095-En1-N-(3,3-difluoropiperidin-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide;
[0937] Cpd 095-En2-N-(3,3-difluoropiperidin-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide;
[0938] Cpd 096-5-(Benzyloxy)-2-methyl-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide;
[0939] Cpd 097-2-methyl-N-(oxolan-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0940] Cpd 098-5-(Benzyloxy)-2-methyl-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide;
[0941] Cpd 099-2-methyl-N-[2-methyl-2-(morpholin-4-yl)propyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0942] Cpd 100-5-(Benzyloxy)-N-(2-hydroxy-2-methylpropyl)-2-methyl-1-benzothiophene-3-carboxamide;
[0943] Cpd 101-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0944] Cpd 102-5-(Benzyloxy)-2-methyl-N-[(5-oxopyrrolidin-2-yl)methyl]-1-benzothiophene-3-carboxamide;
[0945] Cpd 103-2-methyl-N-[(5-oxopyrrolidin-2-yl)methyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0946] Cpd 104-5-(Benzyloxy)-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-1-benzothiophene-3-carboxamide;
[0947] Cpd 105-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0948] pd 106-5-(Benzyloxy)-2-methyl-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-1-benzothiophene-3-carboxamide;
[0949] Cpd 107-2-methyl-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0950] Cpd 108-5-(Benzyloxy)-2-methyl-1-benzothiophene-3-carboxylic acid;
[0951] Cpd 109-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxylic acid;
[0952] Cpd 110-5-methoxy-2-methyl-1-benzothiophene-3-carboxylic acid ethyl ester;
[0953] Cpd 111-5-(Benzyloxy)-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-1-benzothiophene-3-carboxamide;
[0954] Cpd 112-5-(Benzyloxy)-2-(difluoromethyl)-N-{[1-(dimethylamino)cyclopentyl]methyl}-1-benzothiophene-3-carboxamide;
[0955] Cpd 113-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0956] Cpd 114-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0957] Cpd 115-5-(Benzyloxy)-N-[2-(dimethylamino)ethyl]-2-methyl-1-benzothiophene-3-carboxamide;
[0958] Cpd 116-5-(benzyloxy)-2-(difluoromethyl)-N-[2-(dimethylamino)ethyl]-1-benzothiophene-3-carboxamide;
[0959] Cpd 117-N-[2-(dimethylamino)ethyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0960] Cpd 118-N-[2-(dimethylamino)ethyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0961] Cpd 119-5-(Benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-(difluoromethyl)-1-benzothiophene-3-carboxamide;
[0962] Cpd 120-5-(Benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-1-benzothiophene-3-carboxamide;
[0963] Cpd 121-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0964] Cpd 122-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide;
[0965] Cpd 123-5-(Benzyloxy)-2-methyl-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide;
[0966] Cpd 124-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide;
[0967] Cpd 125-2-methyl-N-(1-methylpyrrolidin-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0968] Cpd 126-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide;
[0969] Cpd 127-5-(Benzyloxy)-2-methyl-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide;
[0970] Cpd 128-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide;
[0971] Cpd 129-2-methyl-N-(1-methylpiperidin-4-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide;
[0972] Cpd 130-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide;
[0973] Cpd 131-5-(Benzyloxy)-2-(difluoromethyl)-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide;
[0974] Cpd 132-3-hydroxy-N,2-dimethyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propionamide;
[0975] Cpd 133-N-methyl-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-amino}oxolane-3-carboxamide;
[0976] Cpd 134-5-(Benzyloxy)-N,2-dimethy...
Claims
1. A compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph in R 1 represents -F, -Cl, -Br, -I, -CN, -R W , -OR W , -OC(=O)R W , -NR W R X , -NR W C(=O)R X , -SR W 、 -S(=O)R W 、 -S(=O)2R W 、 -C(=O)R W 、 -C(=O)OR W or -C(=O)NR W R X ; Q means -OR 2 or -NR 3 R 4 ; R 2 Indicates -R Y5 ; R 3 Indicates -OH or -R Y1 ; R 4 Indicates -R Y2 or -S(=O)2R Y3 ; or R 3 and R 4 together form a 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S, which is saturated or unsaturated, unsubstituted or mono- or polysubstituted; T stands for -O-, and U stands for -(CR 5 R 5 ') n -; or T means -(CR 5 R 5 ') n -, and U represents -O-; n is an integer selected from 1, 2, 3, 4 or 5; R 5 and R 5 'Independently represent -R Y4 ; R 6 , R 7 and R 8 Independently represent -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ; W stands for 3-14 membered cycloalkyl, which is saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted; 6-14 membered aryl which is unsubstituted, monosubstituted or polysubstituted; 3-14 membered heterocycloalkyl, which is saturated or unsaturated, monosubstituted or polysubstituted; 5-14 membered heteroaryl, which is mono- or poly-substituted; or -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted; in R W and R X Independently of each other, in each case independently -H; - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; - C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; R Y1 , R Y2 , R Y3 , R Y4 and R Y5 Independently of each other, in each case independently -H; - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; - C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 6-14 membered aryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 6-14 membered aryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; and wherein "mono- or polysubstituted" in each case independently means substitution by one or more substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-C 1-6 -alkyl, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -C(=O)-NH(OH), -C 1-6 -alkylene-C(=O)-NH(OH), -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -OC 1-6 -Alkylene-OC 1-6 -alkyl, -OC 1-6 -Alkylene-NH2, -OC 1-6 -Alkylene-NH-C 1-6 -alkyl, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-OC 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OC(=O)-NH(C 1-6 -alkyl), -OC(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OC(=O)-N(C 1-6 -alkyl)2, -OS(=O)2-NH2, -C 1-6 -alkylene-OS(=O)2-NH2, -OS(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OS(=O)2-NH(C 1-6 -alkyl), -OS(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OS(=O)2-N(C 1-6 -alkyl)2, -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6 -alkyl, -NH-C(=O)-NH2, -C 1-6 -alkylene-NH-C(=O)-NH2, -NH-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-C(=O)-NH(C 1-6 -alkyl), -NH-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C(=O)-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH2, -N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -Alkylene-NH-S(=O)2-OC 1-6 -alkyl, -NH-S(=O)2-NH2, -C 1-6 -alkylene-NH-S(=O)2-NH2, -NH-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-S(=O)2-NH(C 1-6 -alkyl), -NH-S(=O)2N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-S(=O)2N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -Alkylene-SC 1-6 -alkyl, -S(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl, -C 1-6 -Alkylene-S(=O)2-OC 1-6 -alkyl, -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl)2,3-14-membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14-membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(═O)-(3- to 14-membered cycloalkyl), -C(═O)-(3- to 14-membered heterocycloalkyl), -C(═O)-phenyl, -C(═O)-(5- to 14-membered heteroaryl), -S(═O)2-(3- to 14-membered cycloalkyl), -S(═O)2-(3- to 14-membered heterocycloalkyl), -S(═O)2-phenyl or -S(═O)2-(5- to 14-membered heteroaryl), Wherein the compound is not: 5-Benzyloxybenzo[b]thiophene-3-carboxylic acid.
2. The compound according to claim 1, wherein Q represents -NR 3 R 4 .
3. A compound according to any one of claims 1 or 2, wherein T represents -O-, and U represents -(CR 5 R 5 ') n -.
4. A compound according to any one of claims 1 to 3, wherein R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF3.
5. A compound according to any one of claims 1 to 4, wherein R 4 express -H; -S(=O)2C 1-6 - alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted; -S(=O)2(3-14 membered cycloalkyl), which is saturated, monosubstituted or polysubstituted; - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; - C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein The 3-14 membered cycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; -C 1-6 - alkylene-phenyl which is unsubstituted, monosubstituted or polysubstituted; - phenyl, which is unsubstituted, monosubstituted or polysubstituted; or 5-14 membered heteroaryl, which is unsubstituted, monosubstituted or polysubstituted; wherein the 5-14 membered heteroaryl is optionally attached via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
6. A compound according to any one of claims 1 to 5, wherein R 4 express -H; -S(=O)2C 1-6 -alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted by -F; -S(=O)2(3-14 membered cycloalkyl), which is saturated and unsubstituted; -C 1-6 -alkyl, which is saturated, unsubstituted, mono- or poly-substituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene -NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene -NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl; -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, unsubstituted -phenyl, oxetanyl or pyrimidinyl; 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or mono- or poly-substituted by -F, -Cl, -Br, -I, -OH, wherein the 3- to 14-membered cycloalkyl is saturated, unsubstituted, mono- or di-substituted independently of one another by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl) 2, 3-14 membered cycloalkyl, unsubstituted -phenyl, oxetanyl or pyrimidinyl; 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or mono- or polysubstituted by -F, -Cl, -Br, -I, -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from azetidine, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, octahydropyrrolo[1,2-a]pyrrole, oxazine, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, which are in each case unsubstituted, monosubstituted or polysubstituted, independently of one another, by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl; 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -F, -Cl, -Br, -I, -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, which are in each case unsubstituted, monosubstituted or disubstituted independently of one another by substituents selected from the group consisting of -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl.
7. A compound according to any one of claims 1 to 6, wherein W represents 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl; 6-14 membered aryl, which is unsubstituted, independently selected from the following mono- or poly-substituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl; 3-14 membered heterocycloalkyl, which is saturated or unsaturated, unsubstituted, independently selected from the following mono- or poly-substituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl; 5-14 membered heteroaryl, which is unsubstituted, independently selected from the following mono- or poly-substituted: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl; or -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl; which are in each case unsubstituted, monosubstituted or polysubstituted independently by substituents selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C(=O)OH, -C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -OH, =O, -OC 1-6 -alkyl, -NH2, -NHC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NH-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 -alkyl, -C(=O)-N(C 1-6 -alkyl)2, -S(=O)2C 1-6 -alkyl, -S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, 3-14 membered cycloalkyl, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl.
8. A compound according to any one of claims 1 to 7, wherein R 1 Indicates -H, -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -OC 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)C 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -C(=O)NHC 1-6 -alkyl, -C(=O)NH2, -C(=O)N(C 1-6 -alkyl)2, -S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -OC 1-6 -alkyl, unsubstituted-cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl.
9. A compound according to any one of claims 1 to 8, wherein R 5 and R 5 'Independently express -H; - C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; - C1-C6-heteroalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein The 3- to 14-membered cycloalkyl radical is optionally linked via a -C1-C6-alkylene- or -C1-C6-heteroalkylene- radical, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.
10. A compound according to any one of claims 1 to 9, wherein R 6 , R 7 and R 8 Independently express -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2, -C 1-6 -alkyl, -CF3, -CHF2, -CH2F, -OC 1-6 -alkyl, -OCF3, -OCHF2, -OCH2F, -NHC 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; -N(C 1-6 -alkyl)2, which is unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; -C(=O)OC 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; -OC(=O)C 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; or -C 1-6 -heteroalkyl, which is unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2.
11. A compound according to any one of claims 1 to 10, selected from the group consisting of: Cpd 001-(2R)-2-{[5-(Benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamido}propanamide; Cpd 002-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide; Cpd 003-(2R)-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 004-(2R)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propanamide; Cpd 005-(2R)-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 006-(2R)-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 007-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide; Cpd 008-(2S)-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 009-(2S)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propanamide; Cpd 010-(2S)-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide; Cpd 011-(2S)-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 012-(2S)-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 013-5-(Benzyloxy)-2-(difluoromethyl)-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide; Cpd 014-5-(Benzyloxy)-2-(difluoromethyl)-N-(2-hydroxy-2-methylpropyl)-1-benzothiophene-3-carboxamide; Cpd 015-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-4-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 016-(2S)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 017-(2R)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 018-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 019-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 020-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amino}oxolane-3-carboxamide; Cpd 021-4-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amino}oxane-4-carboxamide; Cpd 022-N-[1-(Hydroxymethyl)cyclopropyl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 023-N-[1-(Hydroxymethyl)cyclobutyl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 024-N-[4-(Hydroxymethyl)oxan-4-yl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 025-N-[3-(Hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 026-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amino}oxetane-3-carboxamide; Cpd 027-(2S)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 028-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 029-(2R)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 030-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 031-2-methyl-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 032-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 033-4-{2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amino}oxane-4-carboxamide; Cpd 034-N-[1-(Hydroxymethyl)cyclopropyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 035-N-[1-(Hydroxymethyl)cyclobutyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 036-N-[4-(Hydroxymethyl)oxan-4-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 037-N-[3-(Hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 038-3-{2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amino}oxetane-3-carboxamide; Cpd 039-N-(3,3-difluorocyclobutyl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 040-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide; Cpd 041-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(2-oxopyrrolidin-3-yl)-1-benzothiophene-3-carboxamide; Cpd 042-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 043-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide; Cpd 044-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide; Cpd 045-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 046-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[(5-oxopyrrolidin-2-yl)methyl]-1-benzothiophene-3-carboxamide; Cpd 047-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 048-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-1-benzothiophene-3-carboxamide; Cpd 049-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxylic acid; Cpd 050-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamido}-3-hydroxypropanamide; Cpd 051-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-3-hydroxypropanamide; Cpd 05 2-(2S)-3-hydroxy-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 05 3-(2S)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propanamide; Cpd 054-(2S)-3-hydroxy-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide; Cpd 055-5-[(2-Fluorophenyl)methoxy]-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 056-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-3-hydroxypropanamide; Cpd 057-(2R)-3-hydroxy-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 058-(2R)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propanamide; Cpd 059-5-[(2-Fluorophenyl)methoxy]-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 060-5-(Benzyloxy)-2-methyl-N-[(3S)-2-oxopyrrolidin-3-yl]-1-benzothiophene-3-carboxamide; Cpd 061-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamido}-2-methylpropanamide; Cpd 062-2-{[5-(Benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamido}-2-methylpropanamide; Cpd 063-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-2-methylpropanamide; Cpd 064-2-methyl-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide; Cpd 065-2-methyl-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamido]propanamide; Cpd 066-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-2-methylpropanamide; Cpd 067-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxan-4-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 068-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxetan-3-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 069-5-(Cyclopropylmethoxy)-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-1-benzothiophene-3-carboxamide; Cpd 070-4-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-amino}oxane-4-carboxamide; Cpd 071-4-{2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-amino}oxane-4-carboxamide; Cpd 072-4-{5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-amino}oxane-4-carboxylic acid; Cpd 073-5-(Benzyloxy)-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 074-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 075-N-[1-(Hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 076-N-[1-(Hydroxymethyl)cyclopropyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 077-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 078-N-[1-(Hydroxymethyl)cyclobutyl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 079-N-[1-(Hydroxymethyl)cyclobutyl]-5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 080-5-(Benzyloxy)-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 081-5-[(2-fluorophenyl)methoxy]-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 082-N-[4-(Hydroxymethyl)oxan-4-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 083-N-[4-(Hydroxymethyl)oxan-4-yl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 084-N-[4-(Hydroxymethyl)oxan-4-yl]-5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 085-5-[(2-fluorophenyl)methoxy]-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 086-N-[3-(Hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 087-3-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-amino}oxetane-3-carboxamide; Cpd 088-3-{2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-amino}oxetane-3-carboxamide; Cpd 089-5-(Benzyloxy)-N-(3,3-difluorocyclobutyl)-2-methyl-1-benzothiophene-3-carboxamide; Cpd 090-N-(3,3-difluorocyclobutyl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 091-5-(Benzyloxy)-2-methyl-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide; Cpd 092-2-methyl-N-(1-methyl-1H-pyrazol-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 093-5-[(2-fluorophenyl)methoxy]-2-methyl-N-(2-oxopyrrolidin-3-yl)-1-benzothiophene-3-carboxamide; Cpd 094-2-methyl-N-(2-oxopyrrolidin-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 095-En1-N-(3,3-difluoropiperidin-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 095-En2-N-(3,3-difluoropiperidin-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 096-5-(Benzyloxy)-2-methyl-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide; Cpd 097-2-methyl-N-(oxolan-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 098-5-(Benzyloxy)-2-methyl-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide; Cpd 099-2-methyl-N-[2-methyl-2-(morpholin-4-yl)propyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 100-5-(Benzyloxy)-N-(2-hydroxy-2-methylpropyl)-2-methyl-1-benzothiophene-3-carboxamide; Cpd 101-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 102-5-(Benzyloxy)-2-methyl-N-[(5-oxopyrrolidin-2-yl)methyl]-1-benzothiophene-3-carboxamide; Cpd 103-2-methyl-N-[(5-oxopyrrolidin-2-yl)methyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 104-5-(Benzyloxy)-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 105-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 106-5-(Benzyloxy)-2-methyl-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-1-benzothiophene-3-carboxamide; Cpd 107-2-methyl-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 108-5-(Benzyloxy)-2-methyl-1-benzothiophene-3-carboxylic acid; Cpd 109-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxylic acid; Cpd 111-5-(Benzyloxy)-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-1-benzothiophene-3-carboxamide; Cpd 112-5-(Benzyloxy)-2-(difluoromethyl)-N-{[1-(dimethylamino)cyclopentyl]methyl}-1-benzothiophene-3-carboxamide; Cpd 113-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 114-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 115-5-(Benzyloxy)-N-[2-(dimethylamino)ethyl]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 116-5-(Benzyloxy)-2-(difluoromethyl)-N-[2-(dimethylamino)ethyl]-1-benzothiophene-3-carboxamide; Cpd 117-N-[2-(dimethylamino)ethyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 118-N-[2-(dimethylamino)ethyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 119-5-(Benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-(difluoromethyl)-1-benzothiophene-3-carboxamide; Cpd 120-5-(Benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-1-benzothiophene-3-carboxamide; Cpd 121-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 122-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 123-5-(Benzyloxy)-2-methyl-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide; Cpd 124-5-(Benzyloxy)-2-(difluoromethyl)-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide; Cpd 125-2-methyl-N-(1-methylpyrrolidin-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 126-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide; Cpd 127-5-(Benzyloxy)-2-methyl-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide; Cpd 128-5-(Benzyloxy)-2-(difluoromethyl)-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide; Cpd 129-2-methyl-N-(1-methylpiperidin-4-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 130-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide; Cpd 131-5-(Benzyloxy)-2-(difluoromethyl)-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide; Cpd 132-3-hydroxy-N,2-dimethyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}carboxamido)propanamide; Cpd 133-N-methyl-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amino}oxolane-3-carboxamide; Cpd 134-5-(Benzyloxy)-N,2-dimethyl-1-benzothiophene-3-carboxamide; Cpd 135-5-(Benzyloxy)-2-(difluoromethyl)-N-methyl-1-benzothiophene-3-carboxamide; Cpd 136-N,2-dimethyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide; Cpd 137-N,2-dimethyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide; Cpd 138-(2S)-2-({5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide; Cpd 139-(2S)-3-hydroxy-2-({5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide; Cpd 140-(2R)-2-({5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide; Cpd 141-2-({5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)-2-methylpropanamide; Cpd 142-N-[1-(Hydroxymethyl)cyclopropyl]-5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 143-N-[1-(Hydroxymethyl)cyclobutyl]-5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 144-N-[4-(Hydroxymethyl)oxan-4-yl]-5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide; Cpd 145-5-(Benzyloxy)-N-(3,3-difluorocyclobutyl)-2-(difluoromethyl)-1-benzothiophene-3-carboxamide; Cpd 146-5-(Benzyloxy)-2-(difluoromethyl)-N-(2-oxopyrrolidin-3-yl)-1-benzothiophene-3-carboxamide; Cpd 147-5-(Benzyloxy)-2-(difluoromethyl)-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide; Cpd 148-5-(Benzyloxy)-2-(difluoromethyl)-N-[(5-oxopyrrolidin-2-yl)methyl]-1-benzothiophene-3-carboxamide; Cpd 149-5-(Benzyloxy)-2-(difluoromethyl)-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-1-benzothiophene-3-carboxamide; Cpd 150-5-(Benzyloxy)-2-(difluoromethyl)-1-benzothiophene-3-carboxylic acid; Cpd 151 - 5-(Benzyloxy)-2-(difluoromethyl)-N-[(6-hydroxypyridin-2-yl)methyl]-1-benzothiophene-3-carboxamide; Cpd 152-5-(Benzyloxy)-2-(difluoromethyl)-N-[4-(hydroxymethyl)oxan-4-yl]-1-benzothiophene-3-carboxamide; and physiologically acceptable salts thereof.
12. A pharmaceutical composition comprising a compound according to any one of claims 1 to 11.
13. A compound according to any one of claims 1 to 11 or a pharmaceutical composition according to claim 12 for use as a medicament.
14. A compound according to any one of claims 1 to 11 or a pharmaceutical composition according to claim 12 for use in the treatment of pain or epilepsy.
15. The compound for use or pharmaceutical composition for use according to claim 14, wherein the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain; preferably postoperative pain.
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Benzofuran compounds and use thereof
WO2026067597A1