Novel derivatives for treatment of TRPM3-mediated disorders

Abstract

The present invention relates to compounds useful in the prevention or treatment of TRPM3-mediated disorders, more particularly disorders selected from the group consisting of pain, epilepsy and inflammatory hypersensitivity. The invention also relates to a method for preventing or treating the TRPM3-mediated condition.

Description

Technical Field

[0001] This invention relates to compounds that can be used for the prevention or treatment of TRPM3-mediated conditions, more specifically selected from conditions of pain, epilepsy, and inflammatory hypersensitivity reactions. The invention also relates to a method for the prevention or treatment of said TRPM3-mediated conditions. Background Technology

[0002] The TRP superfamily consists of proteins with six transmembrane domains (6TM), which assemble as homotetramers or heterotetramers to form cation-permeable ion channels. The name TRP originates from a Drosophila trp (transient receptor potential) mutant, characterized by a transient receptor potential in the Drosophila photoreceptor's 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 significant progress has been made in understanding their physiological roles in recent years. Customized selectivity of certain TRP channels allows these channels to... 2+ Mg 2+ TRP channels play a crucial role in the cellular uptake and / or transepithelial transport of trace metal ions. Furthermore, the sensitivity of TRP channels to a wide range of chemical and physical stimuli allows them to function as dedicated biosensors involved in processes ranging from vision to taste and touch. Specifically, several members of the TRP superfamily exhibit very high sensitivity to temperature. These so-called thermal TRPs are highly expressed in sensory neurons and / or 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 etiology of a wide range of 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. Furthermore, TRP channel function / dysfunction has been directly associated with a broad range of pathological conditions, including chronic pain, hypertension, cancer, epilepsy, and neurodegenerative diseases.

[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 a potent known activator of TRPM3 (Wagner et al., 2008). Pregnenolone sulfate induces pain in wild-type mice but not in TRPM3 knockout mice. Recently, it has also been shown that CFA-induced inflammation and inflammatory pain are eliminated in TRPM3 knockout mice. Therefore, TRPM3 antagonists could 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; two mutations in TRPM3 have been reported to be associated with developmental and epileptic encephalopathy (Zhao et al., Channels, Austin, 2021).

[0006] Several TRPM3 antagonists are known, but none point to the compounds of this invention (Straub I et al., *Molecular Pharmacol*, November 2013). For example, liquiditigenin, a putative TRPM3 blocker, has been described as reducing mechanical and cold hyperalgesia in rat models of pain (Chen L et al., *Scientific Reports*, July 2014). There remains a significant medical need for novel, alternative, and / or better therapeutic agents for the prevention or treatment of 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 strong need for therapeutic agents that are potent for a particular type of pain, low in level or without side effects (e.g., unlikely to be addictive like opioids, non-toxic), and / or have good or better pharmacokinetic or kinetic properties.

[0007] This invention provides a novel class of compounds that are antagonists of TRPM3 and can be used as modulators of TRPM3-mediated diseases. Summary of the Invention

[0008] The first aspect of the present invention provides a compound of formula (I) (also referred to as a benzofuran derivative according to the invention), its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs.

[0009]

[0010] in

[0011] R1 This represents -F, -Cl, -Br, -I, -CN, and -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 indicates -NR 3 R 4 ;

[0013] R 3 Indicates -OH or -R Y1 ;

[0014] R 4 -R Y2 or -S(=O)2R Y3 ;

[0015] Or R 3 and R 4 Together they form 4, 5, 6, 7 or 8-membered heterocycles containing 1 to 3 heteroatoms selected from N, O and S, which are saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;

[0016] T represents -O-, and U represents -(CR) 5 R 5 ') n -; or T represents -(CR) 5 R 5 ') n - and U represents -O-;

[0017] n is an integer selected from 1, 2, 3, 4 or 5;

[0018] R 5 and R 5 'Represented independently of each other - R Y4 ;

[0019] R 6 R 7 and R 8 The following can be represented independently: -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 ;

[0020] W indicates

[0021] 3-14 membered cycloalkyl groups, which may be saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted; or

[0022] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, they are unsubstituted, monosubstituted, or polysubstituted;

[0023] in

[0024] R W and R X Represented independently of each other in each case.

[0025] -H;

[0026] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0027] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0028] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0029] 3-14 membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocyclic alkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0030] R Y1 R Y2 RY3 and R Y4 Represented independently of each other in each case.

[0031] -H;

[0032] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0033] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0034] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0035] 3-14 membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocyclic alkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0036] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0037] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0038] Furthermore, "monosubstituted or polysubstituted" in each case independently means substituted by one or more substituents independently selected from the following: -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-C1-6 -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 heterocyclic alkyl), -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).

[0039] Specifically, the present invention provides a compound of formula (I), its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs.

[0040]

[0041] in

[0042] R 1 This represents -F, -Cl, -Br, -I, -CN, and -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 ;

[0043] Q indicates -NR 3 R 4 ;

[0044] R 3 Indicates -OH or -R Y1 ;

[0045] R 4 -R Y2 or -S(=O)2R Y3;

[0046] Or R 3 and R 4 Together they form 4, 5, 6, 7 or 8-membered heterocycles containing 1 to 3 heteroatoms selected from N, O and S, which are saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;

[0047] T represents -O-, and U represents -(CR) 5 R 5 ') n -; or T represents -(CR) 5 R 5 ') n - and U represents -O-;

[0048] n is an integer selected from 1, 2, 3, 4 or 5;

[0049] R 5 and R 5 'Represented independently of each other - R Y4 ;

[0050] R 6 R 7 and R 8 The following can be represented independently: -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 ;

[0051] W indicates

[0052] 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; or

[0053] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, they are unsubstituted, monosubstituted, or polysubstituted;

[0054] in

[0055] R W and RX Represented independently of each other in each case.

[0056] -H;

[0057] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0058] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0059] 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein said 3-14 membered cycloalkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0060] 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0061] R Y1 R Y2 R Y3 and R Y4 Represented independently of each other in each case.

[0062] -H;

[0063] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0064] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0065] 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0066] 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0067] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0068] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0069] Furthermore, "monosubstituted or polysubstituted" in each case independently means substituted by one or more substituents independently selected from the following: -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), -C1-6 -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, -C1-6 -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 heterocyclic alkyl), -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).

[0070] A second aspect of the invention covers a pharmaceutical composition comprising a compound of formula (I) as described in the first aspect.

[0071] According to a third aspect, the present invention also provides compounds of formula (I) as described in the first aspect or pharmaceutical compositions as described in the second aspect, which are used as pharmaceuticals.

[0072] According to a fourth aspect, the present invention also covers compounds of formula (I) as described in the first aspect or pharmaceutical compositions as described in the second aspect, for the prevention and / or treatment of TRPM3-mediated conditions, particularly for the prevention and / or treatment of pain, epilepsy, and / or inflammatory hypersensitivity; and / or for the treatment of pain, epilepsy, and / or inflammatory hypersensitivity. Specifically, for the prevention and / or treatment of pain, epileptic encephalopathy, and / or inflammatory hypersensitivity; and / or for the treatment of pain, epileptic encephalopathy, and / or inflammatory hypersensitivity.

[0073] The present invention also provides a method for preventing or treating TRPM3-mediated conditions by administering a compound of formula (I) as described in the first aspect to a subject in need. More specifically, the present invention relates to such methods for preventing and / or treating pain, epilepsy, and / or inflammatory hypersensitivity reactions; and / or for combating pain, epilepsy, and / or inflammatory hypersensitivity reactions. More specifically, the present invention relates to such methods for preventing and / or treating pain, epileptic encephalopathy, and / or inflammatory hypersensitivity reactions; and / or for combating pain, epileptic encephalopathy, and / or inflammatory hypersensitivity reactions.

[0074] The present invention further provides a method for preparing a compound of formula (I) as described in the first aspect, the method comprising the following steps:

[0075] - Reaction of benzoquinone with a suitable β-keto ester or enamine derivative yields a 5-hydroxybenzofuran-3-carboxylate derivative.

[0076] - Under phototensive conditions, the previously obtained 5-hydroxybenzofuran-3-carboxylate derivative is replaced with a suitable derivative or alcohol derivative carrying a leaving group to obtain a 5-O-substituted benzofuran-3-carboxylate derivative.

[0077] - The previously obtained 5-O-substituted benzofuran-3-carboxylate derivative was converted to formic acid to obtain a 5-O-substituted benzofuran-3-carboxylic acid derivative, and

[0078] - The previously obtained 5-O substituted benzofuran-3-carboxylic acid derivative is coupled with a suitable amine to obtain the desired derivative of the present invention. Detailed Implementation

[0079] Before describing this invention, it should be understood that the invention is not limited to the specific processes, methods, and compounds described, as such processes, methods, and compounds can certainly be varied. It should also be understood that the terminology used herein is not intended to be limiting, as the scope of the invention will be limited only by the appended claims.

[0080] When describing the compounds or processes of the present invention, the terms used will be interpreted according to the following definitions unless the context otherwise indicates.

[0081] As used in the specification and appended claims, unless the context clearly indicates otherwise, the singular forms “a / an” and “the” include both the singular and plural indicators. For example, “compound” means one or more compounds.

[0082] 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, unlisted members, elements, or method steps. The terms “comprising, comprises, and comprised of” also include the terms “composed of”.

[0083] When referring to measurable values ​​such as parameters, quantities, time intervals, etc., as used herein, the term "about" is intended to cover variations of + / -10% or less, preferably + / -5% or less, more preferably + / -1% or less, and still more preferably + / -0.1% or less, provided such variations are suitable for implementation in the disclosed invention. It should be understood that the value referred to by the modifier "about" is itself specifically and preferably disclosed.

[0084] As used herein, when the term “and / or” is used in a list of two or more items, it means that any one of the listed items may be used alone, or any combination of two or more of the listed items may be used. For example, if the list is described as containing groups A, B, and / or C, then the list may 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.

[0085] The description of an endpoint to a numerical range includes all integers, as well as fractions included where appropriate within the range (e.g., when referring to multiple elements, 1 to 5 may include 1, 2, 3, 4, and when referring to measurements, it may also include 1.5, 2, 2.75, and 3.80). The description of an endpoint also includes the endpoint value itself (e.g., 1.0 to 5.0 includes both 1.0 and 5.0). Any numerical range described herein is intended to include all subranges included therein.

[0086] Throughout this specification, references to "an embodiment" or "one embodiment" mean that a specific feature, structure, or characteristic described in connection with an embodiment is included in at least one embodiment of the invention. Therefore, the appearance of the phrase "in one embodiment" or "in one embodiment" in various places throughout this specification does not necessarily refer to the same embodiment, but may refer to the same embodiment. Furthermore, in one or more embodiments, specific features, structures, or characteristics may be combined in any suitable manner, as will be apparent to those skilled in the art based on this disclosure. Moreover, while some embodiments described herein include some but not others of features included in other embodiments, 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 invention and form different embodiments. For example, in the following claims, any claimed embodiment may be used in any combination.

[0087] Similarly, it should be understood that in the description of exemplary embodiments of the invention, various features of the invention are sometimes grouped together in a single embodiment, drawing or description thereof for the purpose of simplifying the disclosure and aiding in the understanding of one or more of the various inventive aspects.

[0088] Unless otherwise defined, all terms (including technical and scientific terms) used in disclosing this invention have the meanings commonly understood by one of ordinary skill in the art to which this invention pertains. Further guidance, including definitions of the terms used in the specification, is provided to better understand the teachings of this invention.

[0089] When describing this invention, the terms used will be interpreted according to the following definitions unless the context otherwise requires.

[0090] Those skilled in the art will readily understand the terms described above, as well as other terms used in the specification.

[0091] Whenever the term “substituted” is used herein, it means that one or more hydrogen atoms on the atom indicated in the expression “substituted” are selectively substituted from the indicated group, provided that the substitution does not exceed the normal valence of the indicated atom, and that the substitution produces a chemically stable compound, i.e., a compound that is robust enough to survive separation from the reaction mixture.

[0092] In each of the following definitions, the number of carbon atoms represents the maximum number of carbon atoms that are generally best present in the substituent or linker; it should be understood that, where otherwise indicated in this application, the number of carbon atoms represents the optimal maximum number of carbon atoms for the particular substituent or linker.

[0093] As used herein, the term "leaving group" or "LG" means a chemical group that is readily replaced, cleaved, or hydrolyzed by a nucleophile under basic or acidic conditions. In a particular embodiment, the leaving group is selected from halogen atoms (e.g., Cl, Br, I) or sulfonates (e.g., methanesulfonates, toluenesulfonates, trifluoromethanesulfonates).

[0094] The term "protecting group" refers to a portion of a compound that masks or alters the properties of a functional group or the properties of the compound as a whole. The chemical substructure of protecting groups varies considerably. One function of protecting groups is as intermediates in the synthesis of parent drug substances. Chemical protecting groups and the strategies used 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 often used to mask the reactivity of certain functional groups to contribute to the efficiency of desired chemical reactions, such as the orderly and planned formation and breaking of chemical bonds. Protection of a compound's functional groups alters other physical properties besides the reactivity of the protected functional group, such as polarity, lipophilicity (hydrophobicity), and other properties measurable by common analytical tools. Chemically protected intermediates can themselves be biologically active or inactive.

[0095] Protected compounds can also exhibit altered, and in some cases optimized, in vitro and in vivo properties, such as resistance to cell membranes and to enzymatic degradation or chelation. In this role, the protected compound with the intended therapeutic effect can be referred to as a prodrug. Another function of the protecting group is to convert the parent drug into a prodrug, thereby releasing the parent drug during the conversion of the prodrug in vivo. Because the active prodrug can be absorbed more efficiently than the parent drug, the prodrug can have greater potency in vivo than the parent drug. In the case of chemical intermediates, the protecting group is removed in vitro, or in the case of prodrugs, the protecting group is removed in vivo. For chemical intermediates, whether the resulting product (e.g., an alcohol) after deprotection is physiologically acceptable is not particularly important, although it is generally more desirable for the product to be pharmacologically harmless.

[0096] As used herein, the term "heteroatom" means an atom selected from: nitrogen (which may be quaternized); oxygen; and sulfur (including sulfoxides and sulfones).

[0097] As used herein, the term "saturated or unsaturated alkyl" encompasses both saturated alkyl groups and unsaturated alkyl groups, such as alkenyl, ynyl, etc. 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. 1-6 "Alkyl" includes all straight-chain or branched alkyl groups having between 1 and 6 carbon atoms, and therefore includes methyl, ethyl, n-propyl, isopropyl, butyl and its isomers (e.g., n-butyl, isobutyl and tert-butyl); pentyl and its isomers; hexyl and its isomers. For example, "C 1-5 "Alkyl" includes all straight-chain or branched alkyl groups having between 1 and 5 carbon atoms, and therefore includes methyl, ethyl, n-propyl, isopropyl, butyl and its isomers (e.g., n-butyl, isobutyl and tert-butyl); pentyl and its isomers; ethylene or vinyl (-CH=CH2), allyl (-CH2CH=CH2), 5-hexenyl (-CH2CH2CH2CH2CH=CH2); 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl, ethynyl, 2-propynyl, 2-butynyl, 3-butynyl, 2-pentynyl and its chain isomers, 2-hexynyl and its chain isomers.

[0098] As used herein, the term "alkyl" means a straight-chain or branched n-, secondary, or tertiary hydrocarbon without unsaturated sites. 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-chain or branched alkyl groups having between 1 and 6 carbon atoms, and therefore includes methyl, ethyl, n-propyl, isopropyl, butyl and its isomers (e.g., n-butyl, isobutyl and tert-butyl); pentyl and its isomers; hexyl and its isomers. For example, "C 1-5 "Alkyl" includes all straight-chain or branched alkyl groups having between 1 and 5 carbon atoms, and therefore includes methyl, ethyl, n-propyl, isopropyl, butyl and its isomers (e.g., n-butyl, isobutyl and tert-butyl); pentyl and its isomers. For example, "C 1-4 "Alkyl" includes all straight-chain or branched alkyl groups having between 1 and 4 carbon atoms, and therefore includes methyl, ethyl, n-propyl, isopropyl, butyl, and their isomers (e.g., n-butyl, isobutyl, and tert-butyl). For example, "C 1-3 "Alkyl" includes all straight-chain or branched alkyl groups having between 1 and 3 carbon atoms, and therefore includes methyl, ethyl, n-propyl, and isopropyl. "Substituted C 1-6 "Alkyl" refers to a C14 alkyl group that is substituted at any available attachment point with one or more substituents (e.g., 1 to 3 substituents, such as 1, 2, or 3 substituents). 1-6 alkyl.

[0099] As used herein, the term "alkenyl" refers to a straight-chain or branched normal, secondary, or tertiary hydrocarbon having at least one unsaturated site (typically 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 cis or trans configuration. When a subscript is used after a carbon atom herein, the subscript indicates the number of carbon atoms that the nominate group may contain. For example, the term "C 2-6"Alkenyl" refers to an unsaturated hydrocarbon group, which can be straight-chain or branched, containing one or more carbon-carbon double bonds and comprising 2 to 6 carbon atoms. For example, C 2-4 Alkenyl groups include all straight-chain or branched alkenyl groups having 2 to 4 carbon atoms. C 2-6 Examples of alkenyl groups are vinyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl, etc.

[0100] As used herein, the term "alkynyl" refers to a straight-chain or branched normal, secondary, or tertiary hydrocarbon having at least one unsaturated site (typically 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 (propynyl, -CH2C≡CH). When a subscript is used after a carbon atom herein, the subscript indicates the number of carbon atoms that the nominate group may contain. For example, the term "C 2-6 "Alkyne" refers to an unsaturated hydrocarbon group, which can be straight-chain or branched, containing one or more carbon-carbon triple bonds and comprising 2 to 6 carbon atoms. For example, C 2-4 Alkynes include all straight-chain or branched alkynes 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 its chain isomers, 2-hexynyl and its chain isomers, etc.

[0101] As used herein, the term "saturated or unsaturated alkylene" encompasses both saturated and unsaturated alkylene, such as alkenylene, alkyneene, etc. As used herein, the term "alkylene" means a saturated, straight-chain or branched hydrocarbon group having two monovalent groups at the center derived by removing two hydrogen atoms from the same or two different carbon atoms of the 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, and hexylene and its chain isomers.

[0102] As used herein, the term "alkenyl" refers to a straight-chain or branched hydrocarbon group having at least one unsaturated site (typically 1 to 3, preferably 1), namely a carbon-carbon sp2 double bond, and having two monovalent groups at the center derived by removing two hydrogen atoms from the same or two different carbon atoms of the parent alkene. 2-6 "Ideenyl", whether it is itself or as part of another substituent, refers to a divalent C. 2-6 Alkenyl groups are those with two single bonds that can attach two other groups.

[0103] As used herein, the term "ethynyl" refers to a straight-chain or branched hydrocarbon group having at least one unsaturated site (typically 1 to 3, preferably 1), namely a carbon-carbon sp triple bond, and having two monovalent groups at the center derived by removing two hydrogen atoms from the same or two different carbon atoms of the parent alkyne. As used herein, the term "C 2-6 "Imyynyl", either on its own or as part of another substituent, refers to a divalent C- group. 2-6 The alkynyl group has two single bonds to attach two other groups.

[0104] The term "alkenyl," as a group or part of a group, refers to an unsaturated hydrocarbon group, which may be straight-chain or branched, containing one or more carbon-carbon double bonds. When a subscript is used after a carbon atom herein, the subscript indicates 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, which can be straight-chain or branched, containing one or more carbon-carbon double bonds and comprising 2 to 6 carbon atoms. For example, C 2-4 Alkenyl groups include all straight-chain or branched alkenyl groups having 2 to 4 carbon atoms. C 2-6 Examples of alkenyl groups are vinyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl, etc.

[0105] The term "alkynyl" itself, or as part of another substituent, refers to an unsaturated hydrocarbon group, which may be straight-chain or branched, containing one or more carbon-carbon triple bonds. When a subscript is used after a carbon atom herein, the subscript indicates the number of carbon atoms that the named group may contain. For example, the term "C 2-6 "Alkyne" refers to an unsaturated hydrocarbon group, which can be straight-chain or branched, containing one or more carbon-carbon triple bonds and comprising 2 to 6 carbon atoms. For example, C 2-4 Alkynes include all straight-chain or branched alkynes having 2 to 4 carbon atoms. 2-6Non-limiting examples of alkynyl groups include ethynyl, 2-propynyl, 2-butynyl, 3-butynyl, 2-pentynyl and its chain isomers, 2-hexynyl and its chain isomers, etc.

[0106] The term "halogenated C" 1-6 "Alkyl" as a group or part of a group refers to a C group having the meaning as defined above. 1-6 Alkyl groups, in which one, two, or three hydrogen atoms are each substituted with a 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, etc.

[0107] As used herein, the term "saturated or unsaturated heteroalkyl" encompasses both saturated and unsaturated heteroalkyl groups, such as heteroalkenyl, heteroynyl, etc. As used herein, the term "heteroalkyl" means a straight-chain or branched alkyl group in which one or more carbon atoms (typically 1, 2, or 3) are substituted with heteroatoms (i.e., oxygen, nitrogen, or sulfur atoms), provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. This means that one or more -CH3 groups of the alkyl group may be substituted with -NH2 and / or one or more -CH2- groups of the alkyl group may be substituted with -NH-, -O-, or -S-. The S atoms in the chain may optionally be oxidized with one or two oxygen atoms to provide sulfoxides and sulfones, respectively. Furthermore, the heteroalkyl groups in the benzofuran derivatives of the present invention may contain oxo or thio groups at any carbon or heteroatom, which will produce stable compounds. Exemplary heteroalkyl groups include, but are not limited to, alcohols, alkyl ethers (e.g., -methoxy, -ethoxy, -butoxy…), primary alkylamines, secondary alkylamines and tertiary alkylamines, amides, ketones, esters, alkyl sulfides, and alkyl sulfones. The term "heteroalkenyl" refers to a straight-chain or branched alkenyl group in which one or more carbon atoms (typically 1, 2, or 3) are substituted with oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Therefore, the term heteroalkenyl includes imine, -O-alkenyl, -NH-alkenyl, -N(alkenyl)2, -N(alkyl)(alkenyl), and -S-alkenyl. As used herein, the term "heteroyynyl" refers to a straight-chain or branched ynyl group in which one or more carbon atoms (typically 1, 2, or 3) are substituted with oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Therefore, the term heteroyynyl includes -cyano, -O-ynyl, -NH-ynyl, -N(ynyl)2, -N(alkyl)(ynyl), -N(alkenyl)(ynyl), and -S-ynyl.

[0108] As used herein, the term "saturated or unsaturated heteroalkylene" encompasses both saturated and unsaturated heteroalkylene, such as heteroalkylene, heteroalkylene, etc. As used herein, the term "heteroalkylene" means a straight-chain or branched alkylene where one or more carbon atoms (typically 1, 2, or 3) are substituted with heteroatoms (i.e., oxygen, nitrogen, or sulfur atoms), provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein, the term "heteroalkylene" means a straight-chain or branched alkenylene where one or more carbon atoms (typically 1, 2, or 3) are substituted with oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein, the term "heteroalkylene" means a straight-chain or branched alkyneylene where one or more carbon atoms (typically 1, 2, or 3) are substituted with oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms.

[0109] As used herein, the term "saturated or unsaturated cycloalkyl" encompasses both saturated cycloalkyl groups and unsaturated cycloalkyl groups, such as cycloalkenyl, cycloynyl, etc. Specifically, as used herein, the term "saturated or unsaturated cycloalkyl" encompasses both saturated cycloalkyl groups and unsaturated non-aromatic cycloalkyl groups, such as cycloalkenyl and cycloynyl. 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. Additional rings of polycyclic cycloalkyl groups may be fused, bridged, and / or joined by one or more spirochetes. 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, 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]hexyl, bicyclo[1.1.1]pentane, and cis-bicyclo[3.1.0]hexane. Unless otherwise stated, the term "cycloalkyl" as used herein means a saturated cyclic hydrocarbon group, including monocyclic or bicyclic groups; additional rings of a polycyclic cycloalkyl group may be fused, bridged, and / or joined by one or more spiro atoms. Examples of cycloalkyl groups include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, norbornel, fumarate, decahydronaphthyl, adamantyl, spiro[3.3]hept-2-yl, 3-bicyclo[3.1.0]hexyl, etc. As used herein, the term "cycloalkenyl" means a non-aromatic cyclic hydrocarbon group having at least one unsaturated site (typically 1 to 3, preferably 1), i.e., a carbon-carbon sp2 double bond. The term "cycloalkenyl" also includes monocyclic or bicyclic groups; additional rings of a polycyclic cycloalkenyl group may be fused, bridged, and / or joined by one or more spiro atoms. Examples include, but are not limited to, cyclopentenyl and cyclohexenyl. The double bond may be cis or trans configuration. As used herein, the term "cycloalkynyl" means a non-aromatic cycloalkyl group having at least one unsaturated site (typically 1 to 3, preferably 1), i.e., a carbon-carbon sp triple atom. An example is cyclohepta-1-yne. Fusion systems of cycloalkyl and heterocyclic alkyl rings are considered heterocyclic alkyl, regardless of the ring bonded to the core structure. Fusion systems of cycloalkyl and aryl rings are considered aryl, regardless of the ring bonded to the core structure. Fusion systems of cycloalkyl and heteroaryl rings are considered heteroaryl, regardless of the ring bonded to the core structure.

[0110] As used herein, the term "saturated or unsaturated heterocyclic alkyl" encompasses both saturated heterocyclic alkyl and unsaturated non-aromatic heterocyclic alkyl that includes at least one heteroatom, i.e., N, O, or S, as a ring member. Specifically, the terms "saturated or unsaturated heterocyclic alkyl" and "saturated or non-aromatic unsaturated heterocyclic alkyl" are synonymous. Unless otherwise stated, as used herein, the term "heterocyclic alkyl" means a "cycloalkyl" in which one or more carbon atoms (typically 1, 2, or 3) are substituted with oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Unless otherwise stated, as used herein, the term "heterocyclic alkenyl" means a "cycloalkenyl" in which one or more carbon atoms (typically 1, 2, or 3) are substituted with oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Unless otherwise stated, as used herein, the term "heterocyclic alkynyl" means a "cycloalkynyl" 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 heterocyclic alkyl groups include, but are not limited to, azetane, 1,4-oxaazetane, azetane, azetidine, azetane propane, azetane octane, diazetane, dioxane, dioxane, dioxane, dithiazolide, dithiopentane, imidazolide, isothiazolidine, isoxazolidine, morpholine, oxazolidine, hexane oxide, oxazolide, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyridine Flour, thiazolyl, thiazolylbutane, thiazolylpropane, thiazolylpentane, 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-pyrrolizine, hexahydrocyclopentan[c]pyrrole, octahydrocyclopentan[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine.Further descriptions of heterocyclic alkyl groups in the context of this invention are found in Paquette, Leo A., “Principles of Modern Heterocyclic Chemistry” (WA Benjamin, New York, 1968), particularly in Chapters 1, 3, 4, 6, 7, and 9; “The Chemistry of Heterocyclic Compounds, A series of Monographs” (John Wiley & Sons, New York, 1950–present), particularly Volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, CW, and Scriven, E., “Comprehensive Heterocyclic Chemistry” (Pergamon Press, 1996); and the Journal of the American Chemical Society (J. Am. Chem. Soc.) (1960) 82:5566. When a heterocyclic alkyl group does not contain nitrogen as a ring member, it is typically bonded via carbon. When a heterocyclic alkyl group contains nitrogen as a ring member, it can be bonded via nitrogen or carbon. Fused systems of heterocyclic alkyl rings with cycloalkyl rings are considered heterocyclic alkyl, regardless of the ring bonded to the core structure. Fused systems of heterocyclic alkyl rings with aryl rings are considered heterocyclic alkyl, regardless of the ring bonded to the core structure. Fused systems of heterocyclic alkyl rings with heteroaryl rings are considered heteroaryl, regardless of the ring bonded to the core structure.

[0111] As used herein, the term "aryl" refers to an aromatic hydrocarbon. Typical aryl groups include, but are not limited to, groups consisting of one ring or two or three rings fused together, derived from benzene, naphthalene, anthracene, biphenyl, etc. A fused system of an aryl ring with a cycloalkyl ring is considered aryl, regardless of the ring bonded to the core structure. A fused system of an aryl ring with a heterocyclic alkyl ring is considered heterocyclic alkyl, regardless of the ring bonded to the core structure. Therefore, indoline, dihydrobenzofuran, dihydrobenzothiophene, etc., are considered heterocyclic alkyl according to the present invention. A fused system of an aryl ring with a heteroaryl ring is considered heteroaryl, regardless of the ring bonded to the core structure.

[0112] 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, benzoxazole, benzoisoxazole, benzodioxane, benzofuran, benzothiadiazole, benzothiazol, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazon, imidazole, imidazopyridine, indazole, indole, inazine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthidine, oxadiazole, oxazole, hydroxyindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazolium, thiadiazole, thiazolium, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine.

[0113] For further examples, carbon-bonded heterocyclic compounds are bonded at positions 2, 3, 4, 5, or 6 of pyridine, positions 3, 4, 5, or 6 of pyridazine, positions 2, 4, 5, or 6 of pyrimidine, positions 2, 3, 5, or 6 of pyrazine, positions 2, 3, 4, or 5 of furan, tetrahydrofuran, thiophene, pyrrole, or tetrahydropyrrole, positions 2, 3, 4, or 5 of oxazole, imidazole, or thiazole, positions 3, 4, or 5 of isoxazole, pyrazole, or isothiazole, positions 2 or 3 of aziridine, positions 2, 3, or 4 of aziridine, positions 2, 3, 4, 5, 6, 7, or 8 of quinoline, or positions 1, 3, 4, 5, 6, 7, or 8 of isoquinoline.

[0114] 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, the nitrogen-bonded heterocycle is bonded at position 1 in aziridine, aziridine, pyrrole, pyrrolidine, 2-pyrrololine, 3-pyrroleoline, imidazole, imidazolidine, 2-imidazoline, 3-imidazoline, pyrazole, pyrazoline, 2-pyrazoline, 3-pyrazoline, piperidine, piperazine, indole, indoline, and 1H-indazole; position 2 in isoindole or isoindoline; position 4 in morpholine; and position 9 in carbazole or β-carbline. Preferred nitrogen-bonded heterocycles include 1-aziridinepropyl, 1-aziridinebutyl, 1-pyrroleyl, 1-imidazolyl, 1-pyrazolyl, and 1-piperidinyl. Further descriptions of heteroaryl groups in the sense of this invention are found in Paquette, Leo A., “Principles of Modern Heterocyclic Chemistry” (WA Benjamin Press, New York, 1968), particularly in Chapters 1, 3, 4, 6, 7, and 9; “Chemistry of Heterocyclic Compounds: A Series of Monographs” (John Wiley & Sons, New York, 1950–present), particularly Volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, CW, and Scriven, E., “Comprehensive Heterocyclic Chemistry” (Pergman Press, 1996); and the Journal of the American Chemical Society (1960) 82:5566.

[0115] As used herein with respect to substituents, and unless otherwise stated, the terms “monosubstituted,” “disubstituted,” “trisubstituted,” “polysubstituted,” etc., mean as defined herein a chemical structure in which the corresponding moiety is substituted by one or more substituents, meaning that one or more hydrogen atoms of the moiety are each independently substituted by a substituent. For example, -C can be polysubstituted by -F. 1-6 -alkyl groups cover -CH2F, -CHF2, -CF3, -CH2CF3, CF2CF3, etc. Similarly, -C groups can be multi-substituted by substituents selected independently from -F and -Cl. 1-6 -alkyl substituents include -CH2F, -CHF2, -CF3, -CH2CF3, CF2CF3, -CH2Cl, -CHCl2, -CCl3, -CH2CCl3, CCl2CCl3, -CHClF, -CClF2, -CCl2CF3, -CF2CCl3, -CClFCCl2F, etc. The name of any substituent found at more than one site in the compounds of this invention should be chosen independently.

[0116] Unless otherwise stated, as used herein, the term "solvent" includes any combination that can be formed from derivatives of the present invention with suitable inorganic solvents (e.g., hydrates) or organic solvents (e.g., but not limited to alcohols, ketones, esters, ethers, nitriles, etc.).

[0117] As used herein, the term “subject” means an animal, including humans, preferably mammals, and most preferably humans, that has been used as a subject of treatment, observation or experimentation.

[0118] As used herein, the term “therapeutic effective amount” means the amount of an active compound or agent that elicits a biological or medical response sought by a researcher, veterinarian, physician or other clinician in an tissue system, animal or human, including the reduction or partial reduction of symptoms of the disease or condition being treated.

[0119] As used herein, the term "composition" is intended to cover products containing a specific ingredient in a therapeutically effective amount, and any product directly or indirectly produced by a combination of specific ingredients in a specific amount.

[0120] As used herein, the terms “antagonist” or “inhibitor” refer to compounds that, depending on the circumstances, produce a functional antagonistic effect on the TRPM3 ion channel, including competitive antagonists, non-competitive antagonists, desensitizing agonists, and partial agonists.

[0121] For the purposes of this invention, the term "TRPM3-regulated" is used to refer to situations influenced by the regulation of TRPM3 ion channels, including states mediated by TRPM3 ion channels.

[0122] As used herein, the term "TRPM3-mediated condition" refers to a condition or disease whose symptoms, consisting of pain and inflammatory hypersensitivity, can be prevented, treated, (partially) alleviated, or improved by the use of TRPM3 antagonists. According to the International Association for the Study of Pain and for the purposes of this invention, pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage. Preferably, the TRPM3-mediated condition is pain or epilepsy. Preferably, the TRPM3-mediated condition is epilepsy, preferably selected from epileptic encephalopathy. For the purposes of this invention, the term "epilepsy encephalopathy" refers to a group of severe epilepsy characterized by seizures and encephalopathy. Preferably, the TRPM3-mediated condition is pain, preferably selected from nociceptive pain, inflammatory pain, and neuropathic pain. More preferably, the pain is postoperative pain. For the purposes of this invention, the term "inflammatory hypersensitivity reaction" is used to refer to a condition characterized by one or more inflammatory markers (including edema, erythema, hyperthermia, and pain) and / or an excessive physiological or pathophysiological response to one or more types of stimuli (including thermal, mechanical, and / or chemical stimuli).

[0123] The invention will be further described, and in some cases described with respect to specific embodiments, but the invention is not limited thereto.

[0124] Preferred claims (features) and embodiments of the compounds and methods of the present invention are now set forth. Each claim and embodiment of the invention as thus defined may be combined with any other claim and / or embodiment unless the contrary is expressly indicated. Specifically, any feature indicated as preferred or advantageous may be combined with any one or more other features indicated as preferred or advantageous.

[0125] The numbered declaration of this invention is:

[0126] 1. A compound of formula (I), its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs.

[0127]

[0128] in

[0129] R 1 This represents -F, -Cl, -Br, -I, -CN, and -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 ;

[0130] Q indicates -NR 3 R 4 ;

[0131] R 3 Indicates -OH or -R Y1 ;

[0132] R 4 Indicates -R Y2 or -S(=O)2R Y3 ;

[0133] Or R 3 and R 4 Together they form 4, 5, 6, 7 or 8-membered heterocycles containing 1 to 3 heteroatoms selected from N, O and S, which are saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;

[0134] T represents -O-, and U represents -(CR) 5 R 5 ') n -; or T represents -(CR) 5 R 5 ') n - and U represents -O-;

[0135] n is an integer selected from 1, 2, 3, 4 or 5;

[0136] R 5 and R 5 'Represented independently of each other - R Y4 ;

[0137] R 6 R 7 and R 8 The following can be represented independently: -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)RW -S(=O)2R W -C(=O)R W -C(=O)OR W or -C(=O)NR W R X ;

[0138] W indicates

[0139] 3-14 membered cycloalkyl groups, which are saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted; specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; or

[0140] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, they are unsubstituted, monosubstituted, or polysubstituted;

[0141] in

[0142] R W and R X Represented independently of each other in each case.

[0143] -H;

[0144] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0145] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0146] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically, the 3-14 membered cycloalkyl group is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0147] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0148] R Y1 R Y2 R Y3 and R Y4 Represented independently of each other in each case.

[0149] -H;

[0150] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0151] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0152] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0153] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0154] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0155] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0156] Furthermore, "monosubstituted or polysubstituted" in each case independently means substituted by one or more substituents independently selected from the following: -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), -C1-6 -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, -C1-6 -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 heterocyclic alkyl), -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).

[0157] 2. The compound according to Statement 1, wherein T represents -O- and U represents -(CR) 5 R 5 ') n -

[0158] 3. The compound according to any one of statements 1 or 2, wherein R 1 express

[0159] -H, -F, -Cl, -Br, -I;

[0160] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0161] -OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0162] -C(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0163] -C(=O)OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0164] -C(=O)NH2;

[0165] -C(=O)NHC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0166] -C(=O)N(C 1-6 -alkyl)2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0167] -S(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0168] -S(=O)2-C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0169] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0170] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked by -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 linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0171] 4. The compound according to any one of the foregoing statements, wherein R 1 express

[0172] -H, -F, -Cl, -Br, -I;

[0173] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0174] -OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0175] -C(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0176] -C(=O)OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0177] -C(=O)NH2;

[0178] -C(=O)NHC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0179] -C(=O)N(C 1-6 -alkyl)2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0180] -S(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0181] -S(=O)2-C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0182] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0183] The 3-14-membered saturated cycloalkyl, 5-14-membered cycloalkenyl, or 8-14-membered cycloynyl groups are unsubstituted, monosubstituted, polysubstituted, or polysubstituted; each of the 3-14-membered cycloalkyl, 5-14-membered cycloalkenyl, or 8-14-membered cycloynyl groups is optionally linked by a -C1-C6-alkylene- or C1-C6-heteroalkylene- group, and in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably, the 3-12-membered saturated cycloalkyl, 5-12-membered cycloalkenyl, or 8-12-membered cycloynyl groups are unsubstituted, monosubstituted, or polysubstituted, each of the 3-12-membered cycloalkyl, 5-12-membered cycloalkenyl, or 8-12-membered cycloynyl groups is optionally linked by a -C1-C6-alkylene- or C1-C6-heteroalkylene- group, and in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted. Preferably, the 3-10-membered saturated cycloalkyl, 5-10-membered cycloalkenyl, or 8-10-membered cycloynyl group is unsubstituted, monosubstituted, polysubstituted, or polysubstituted, wherein each of the 3-10-membered cycloalkyl, 5-10-membered cycloalkenyl, or 8-10-membered cycloynyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, and in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably, the 3-8-membered saturated cycloalkyl, 5-8-membered cycloalkenyl, or 8-membered cycloynyl group is unsubstituted, monosubstituted, polysubstituted, or polysubstituted, wherein each of the 3-8-membered cycloalkyl, 5-8-membered cycloalkenyl, or 8-membered cycloynyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, and in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0184] 5. The compound according to any one of the foregoing statements, wherein R 1 This represents -H, -F, -Cl, -Br, -I, -CN, and -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, -C1-6 -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 group, -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.

[0185] 6. The compound according to any one of the foregoing statements, wherein R 1 Indicates -H, -C 1-6 -alkyl, -C 1-6 -alkylene-OC 1-6 -alkyl, -CHF2, -CF3 or unsubstituted -cyclopentyl.

[0186] 7. The compound according to any one of the foregoing statements, wherein R 3 express

[0187] -H;

[0188] -OH;

[0189] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0190] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0191] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0192] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0193] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0194] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0195] 8. The compound according to any one of the foregoing statements, wherein R 3 express

[0196] -H;

[0197] -OH;

[0198] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0199] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0200] 9. The compound according to any one of the foregoing statements, wherein R 3 Represents -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.

[0201] 10. The compound according to any one of the foregoing statements, wherein R 3 It represents -H, -OH, or a saturated, unsubstituted, or monosubstituted -C. 1-6 -alkyl.

[0202] 11. The compound according to any one of the foregoing statements, wherein R 3 It represents -H.

[0203] 12. The compound according to any one of the foregoing statements, wherein R 4 express

[0204] -H;

[0205] -S(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0206] -S(=O)2-C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0207] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0208] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0209] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0210] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0211] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0212] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0213] 13. The compound according to any one of the foregoing statements, wherein R 4 express

[0214] -H;

[0215] -S(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0216] -S(=O)2-C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0217] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0218] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0219] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0220] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0221] -C 1-6 -alkylene-phenyl, which is unsubstituted, monosubstituted or polysubstituted;

[0222] -phenyl, which is unsubstituted, monosubstituted, or polysubstituted; or

[0223] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0224] 14. The compound according to any one of the foregoing statements, wherein R 4 express

[0225] -S(=O)2C 1-6-alkyl groups, which are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted groups: -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0226] -S(=O)2(3-14 membered cycloalkyl), wherein the 3-14 membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, which in each case is saturated or unsaturated, unsubstituted, and independently mono- or poly-substituted 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, -C1-6 -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0227] -C 1-6 -alkyl groups, which are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted groups: -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0228] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, and mono- or polysubstituted, independently 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)OC1-6 -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0229] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, which in each case is saturated or unsaturated, and which in each case is unsubstituted and independently monosubstituted or polysubstituted with 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0230] 3-14 membered heterocyclic alkyl or -C 1-6 -alkylene-(3-14 membered heterocyclic alkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered heterocyclic alkyl group is selected from the group consisting of: aziridine, 1,4-oxazacycloheptane, aziridine, aziridine, aziridine propane, aziridine octane, diazacycloheptane, dioxane, dioxane, dioxane, dithiopentane, dithiopentane, imidazoline, isothiazolidine, isoxazolidine, morpholine, oxazolidine, hexane oxide, oxazolidine, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, thiohexacyclobutane, thiohexacyclopropane, thiohexacyclo 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-pyrrolizine, hexahydrocyclopentano[c]pyrrole, octahydrocyclopentano[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; which in each case are unsubstituted, monosubstituted or polysubstituted by substituents selected independently 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0231] -C 1-6 -alkylene-phenyl, wherein the substituents are unsubstituted and independently selected from the group consisting of mono- or polysubstituted groups: -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(C1-6 -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0232] -Phenyl, which is an unsubstituted, mono- or polysubstituted substituent, independently 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0233] 5-14 heteroaryl or -C 1-6 -alkylene-(5-14-membered heteroaryl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted with -OH, wherein the 5-14-membered heteroaryl group is selected from the group consisting of: benzimidazole, benzisoxazole, benzoxazole, benzodioxane, benzofuran, benzothiadiazole, benzothiazolium, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazonium, imidazole, imidazopyridine, indazole, indole, inazine, isobenzofuran, isoindole, isoquinoline, isothiazazole Isoxazole, naphthidine, oxadiazole, oxazole, hydroxyindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazolium, thiadiazole, thiazolium, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine; which in each case are unsubstituted, and are independently selected from the group consisting of mono- or polysubstituted substituents 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl.

[0234] 15. The compound according to any one of the foregoing statements, wherein R 4 express

[0235] -H;

[0236] -S(=O)2C 1-6 -alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted with -F;

[0237] -S(=O)2 (3-14 membered cycloalkyl), which is saturated and unsubstituted;

[0238] -C 1-6 -alkyl groups, which are saturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted substituents: -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, oxetyl or pyrimidinyl;

[0239] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted or polysubstituted by -F, -Cl, -Br, -I, -OH, wherein the 3-14 membered cycloalkyl group is saturated, unsubstituted, and independently monosubstituted or disubstituted 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, oxetyl or pyrimidinyl;

[0240] 3-14 membered heterocyclic alkyl or -C 1-6 -alkylene-(3-14 membered heterocyclic alkyl), wherein -C1-6 -alkylene- is unsubstituted or monosubstituted or polysubstituted with -F, -Cl, -Br, -I, -OH, wherein the 3-14 membered heterocyclic alkyl group is selected in each case from aziridine, 1,4-oxazacycloheptane, pyrrolidine, piperidine, aziridine, diazacycloheptane, tetrahydrofuran, tetrahydropyran, oxazacyclobutane, morpholine, piperazine, hexahydrocyclopentanop[c]pyrrole, octahydrocyclopentanop[c]pyrrole, octahydropyrrolo[1,2-a]pyrrole. Azine, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinine ring, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, wherein in each case, the substituents are unsubstituted and independently selected from the group consisting of mono- or poly-substituted groups: -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl;

[0241] 5-14 heteroaryl or -C 1-6 -alkylene-(5-14-membered heteroaryl), wherein -C 1-6 The -alkylene group is unsubstituted or monosubstituted with -F, -Cl, -Br, -I, or -OH, wherein the 5-14 heteroaryl group is selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, which is unsubstituted and independently monosubstituted or disubstituted with substituents selected from the group consisting of -F, -Cl, -Br, -I, and -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl.

[0242] 16. The compound according to any one of the foregoing statements, wherein R 4 express

[0243] -H;

[0244] -S(=O)2C 1-6 -alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted with -F;

[0245] -S(=O)2 (3-14 membered cycloalkyl), which is saturated and unsubstituted;

[0246] -C 1-6 -alkyl groups, which are saturated, unsubstituted, and independently selected from the group consisting of mono- or disubstituted groups: 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;

[0247] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered cycloalkyl group is saturated, unsubstituted, and independently monosubstituted or disubstituted with 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;

[0248] 3-14 membered heterocyclic alkyl or -C 1-6 -alkylene-(3-14 membered heterocyclic alkyl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered heterocyclic alkyl group is selected in each case from aziridine, 1,4-oxazacycloheptane, pyrrolidine, piperidine, aziridine, diazacycloheptane, tetrahydrofuran, tetrahydropyran, oxazacyclobutane, morpholine, piperazine, hexahydrocyclopentanop[c]pyrrole, octahydrocyclopentanop[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabis(2-dimethylbenzene)pyrrole, 1,4-oxazacycloheptane, pyrrolo[1,2-a]pyrazine ... Cyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinine ring, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, wherein in each case, the substituents are unsubstituted and independently selected from the group consisting of mono- or poly-substituted groups: -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, oxetyl, pyrimidinyl, -C 1-6 -alkylene-phenyl;

[0249] Unsubstituted -phenyl;

[0250] 5-14 heteroaryl or -C 1-6 -alkylene-(5-14-membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 5-14-membered heteroaryl group is selected from the group consisting of: pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, which is unsubstituted and independently monosubstituted or disubstituted with substituents selected from the group consisting of: -C 1-6 -alkyl, -OH.

[0251] 17. The compound according to any one of the foregoing statements, wherein

[0252] R 3 It represents -H; and

[0253] R 4 express

[0254] -H;

[0255] -S(=O)2C 1-6 -alkyl, which is saturated, unsubstituted, monosubstituted or polysubstituted with -F;

[0256] -S(=O)2 (3-14 membered cycloalkyl), which is saturated and unsubstituted;

[0257] -C 1-6 -alkyl groups, which are saturated, unsubstituted, and independently selected from the group consisting of mono- or disubstituted substituents: -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;

[0258] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered cycloalkyl group is saturated, unsubstituted, and independently monosubstituted or disubstituted with 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;

[0259] 3-14 membered heterocyclic alkyl or -C 1-6-alkylene-(3-14 membered heterocyclic alkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered heterocyclic alkyl group is selected in each case from aziridine, 1,4-oxazacycloheptane, pyrrolidine, piperidine, aziridine, diazacycloheptane, tetrahydrofuran, tetrahydropyran, oxazacyclobutane, morpholine, piperazine, hexahydrocyclopentanop[c]pyrrole, octahydrocyclopentanop[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabis(2-dimethylbenzene)pyrrole, 1,4-oxazacycloheptane, pyrrolo[1,2-a]pyrazine ... Cyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinine ring, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, wherein in each case, the substituents are unsubstituted and independently selected from the group consisting of mono- or poly-substituted groups: -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, oxetyl, pyrimidinyl, -C 1-6 -alkylene-phenyl;

[0260] Unsubstituted -phenyl;

[0261] 5-14 heteroaryl or -C 1-6 -alkylene-(5-14-membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 5-14-membered heteroaryl group is selected from the group consisting of: pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, which is unsubstituted and independently monosubstituted or disubstituted with substituents selected from the group consisting of: -C 1-6 -alkyl, -OH.

[0262] 18. The compound according to any one of the foregoing statements, wherein R 3 and R 4 Together they form a 5- or 6-membered heterocycle containing one or two heteroatoms selected from N, O, and S, which may be saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0263] 19. The compound according to any one of the foregoing statements, wherein R 3 and R 4 Together they form heterocycles selected from the group consisting of: pyrrolidine, piperidine, morpholine, and piperazine, which in each case are unsubstituted and independently mono- 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 -C 1-6 -Alkyl monosubstituted 1,2,4-oxadiazole.

[0264] 20. The compound according to any one of the foregoing statements, wherein R 3 and R 4 Together

[0265] The pyrrolidine ring is either unsubstituted or monosubstituted with -N(CH3)2;

[0266] Piperidine ring, which is either 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 -C 1-6 -Alkyl monosubstituted 1,2,4-oxadiazole;

[0267] The morpholine ring, which is unsubstituted; or

[0268] Piperazine ring, which is unsubstituted or N-substituted by a substituent selected from the group consisting of: -C 1-6 -alkyl and unsubstituted -pyridyl.

[0269] 21. The compound according to any one of the foregoing statements, wherein R 3 and R4 Together with the nitrogen atom to which it is attached, it forms residues selected from the following group:

[0270]

[0271] 22. The compound according to any one of the foregoing statements, wherein W represents

[0272] 3-14 membered cycloalkyl groups, which may be saturated or unsaturated; unsubstituted, monosubstituted or disubstituted;

[0273] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, they are unsubstituted, monosubstituted, or disubstituted;

[0274] Specifically, W represents

[0275] 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or disubstituted;

[0276] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, they are unsubstituted, monosubstituted, or disubstituted.

[0277] 23. The compound according to any one of the foregoing statements, wherein W represents

[0278] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, and independently mono- or polysubstituted by substituents selected from the following: -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, -C1-6 -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl, specifically 3-14-membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, and independently mono- or poly-substituted by substituents selected from the following: -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl; or

[0279] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, it is unsubstituted and independently mono- or poly-substituted by a substituent selected from the following: -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl.

[0280] 24. The compound according to any one of the foregoing statements, wherein W represents

[0281] 3-10 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, and independently mono- or poly-substituted by substituents selected from the following: -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl, specifically 3-10-membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, and independently mono- or poly-substituted by substituents selected from the following: -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl; or

[0282] -C1-C6-alkyl groups, which are unsubstituted and independently mono- or poly-substituted by substituents selected from the following: -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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl.

[0283] 25. The compound according to any one of the foregoing statements, wherein W represents

[0284] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, and independently mono- or polysubstituted by substituents selected from the following: -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-aromatic unsaturated, unsubstituted, and independently mono- or poly-substituted by substituents selected from the following: -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

[0285] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, it is unsubstituted and independently mono- or poly-substituted by a substituent selected from the following: -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.

[0286] 26. The compound according to any one of the foregoing statements, wherein W represents

[0287] 3-14 membered saturated cycloalkyl groups, which are unsubstituted and independently mono- or polysubstituted by substituents selected from the following: -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

[0288] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, it is unsubstituted and independently mono- or poly-substituted by a substituent selected from the following: -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、-C1-6 -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.

[0289] 27. The compound according to any one of the foregoing statements, wherein R 5 and R 5 'represented independently of each other'

[0290] -H;

[0291] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0292] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0293] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked by -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 linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0294] 28. The compound according to any one of the foregoing statements, wherein n is an integer selected from 1, 2, or 3, and

[0295] R 5 and R 5 'represented independently of each other'

[0296] -H;

[0297] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0298] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0299] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked by -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 linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0300] 29. The compound according to any one of the foregoing statements, wherein R 5 and R 5 'Independently represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2.

[0301] 30. The compound according to any one of the foregoing statements, wherein R 6 R 7 and R 8 Representing each other independently

[0302] -H;

[0303] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;

[0304] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0305] -OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0306] -NHC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0307] -N(C 1-6 -alkyl)2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0308] -C(=O)OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0309] -OC(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0310] -C 1-6 - Heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0311] 31. The compound according to any one of the foregoing statements, wherein R 6 R 7 and R 8 Representing each other independently

[0312] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2,

[0313] -C 1-6 -alkyl, -CF3, -CHF2, -CH2F,

[0314] -OC 1-6 -alkyl, -OCF3, -OCHF2, -OCH2F,

[0315] -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;

[0316] -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;

[0317] -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;

[0318] -OC(=O)C 1-6-alkyl group, 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

[0319] -C 1-6 - Heteroalkyl groups, which are 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.

[0320] 32. The compound according to any one of the foregoing statements, wherein R 6 It represents -H, -F, -Cl, -CN or -C1-C6-alkyl.

[0321] 33. The compound according to any one of the foregoing statements, wherein R 6 It does not represent -H.

[0322] 34. The compound according to any one of the foregoing statements, wherein R 7 It represents -H, -F, -Cl, -CN or -C1-C6-alkyl.

[0323] 35. The compound according to any one of the foregoing statements, wherein R 7 It does not represent -H.

[0324] 36. The compound according to any one of the foregoing statements, wherein R 8 It represents -H, -F, -Cl, -CN or -C1-C6-alkyl.

[0325] 37. The compound according to any one of the foregoing statements, wherein R 8 It does not represent -H.

[0326] 38. The compound according to any one of the foregoing statements, wherein

[0327] (i)R 6 R 7 and R 8 Each represents -H; or

[0328] (ii)R 6 R 7 and R 8 Both in the text represent -H, and R6 R 7 and R 8 The other one represents -F, -Cl, -CN, or -CH3; or

[0329] (iii)R 6 R 7 and R 8 One of them represents -H, and R 6 R 7 and R 8 The other one in the series can be represented independently as -F, -Cl, -CN, or -CH3.

[0330] 39. The compound according to any one of the foregoing statements, which is selected from the group consisting of Cpd 001 to Cpd044 as mentioned herein and its physiologically acceptable salts.

[0331] 40. The compound according to any one of the foregoing statements is selected from the group consisting of Cpd 001 to Cpd062 as mentioned herein and its physiologically acceptable salts.

[0332] 41. The compound according to any one of the foregoing statements, wherein

[0333] R 1 Indicates H, -CH2F, -CHF2, or -CF3; and / or

[0334] R 3 Indicates -H;

[0335] R 4 express

[0336] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0337] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0338] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0339] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0340] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0341] Or R 3 and R 4 Together they form a 5- or 6-membered heterocycle containing one or two heteroatoms selected from N, O, and S, which may be saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted.

[0342] R 5 and R 5 'Independently representing -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2;

[0343] R 6 R 7 and R 8 Each can independently represent -H, -F, -Cl, -CN, or -C1-C6-alkyl;

[0344] W indicates

[0345] 3-14 membered cycloalkyl groups, which are saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted; specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; or

[0346] -C1-C6-alkyl; which is unsubstituted, monosubstituted or polysubstituted.

[0347] 42. A pharmaceutical composition or drug comprising a compound according to any one of the foregoing statements.

[0348] 43. The compound according to any one of the foregoing statements or the pharmaceutical composition according to statement 42, which is used as a medicine.

[0349] 44. The compound according to any one of the foregoing statements or the pharmaceutical composition according to statement 42, for the treatment of pain or epilepsy; preferably, pain and epileptic encephalopathy.

[0350] 45. The compound or pharmaceutical composition for use as described in statement 44, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain.

[0351] 46. ​​The compound or pharmaceutical composition for use as described in statement 44, wherein the pain is postoperative pain.

[0352] 47. A method for preventing and / or treating TRPM3-mediated conditions, the method comprising administering to a subject an effective amount of a compound according to any one of claims 1 to 41 or a pharmaceutical composition according to claim 42.

[0353] 48. A method for preventing and / or treating pain or epilepsy, such as epileptic encephalopathy, said method comprising administering to a subject an effective amount of a compound according to any one of claims 1 to 41 or a pharmaceutical composition according to claim 42.

[0354] 49. The method according to statement 48, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain.

[0355] The first aspect of the present invention provides a compound of formula (I) (also referred to as a benzofuran derivative according to the invention), its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs.

[0356]

[0357] in

[0358] R 1 This represents -F, -Cl, -Br, -I, -CN, and -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 ;

[0359] Q indicates -NR 3 R 4 ;

[0360] R 3 Indicates -OH or -R Y1 ;

[0361] R 4 -R Y2 or -S(=O)2R Y3 ;

[0362] Or R 3 and R 4 Together they form 4, 5, 6, 7 or 8-membered heterocycles containing 1 to 3 heteroatoms selected from N, O and S, which are saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;

[0363] T represents -O-, and U represents -(CR) 5 R 5 ') n -; or T represents -(CR) 5 R 5 ') n - and U represents -O-;

[0364] n is an integer selected from 1, 2, 3, 4 or 5;

[0365] R 5 and R 5 'Represented independently of each other - R Y4 ;

[0366] R 6 R 7 and R 8 The following can be represented independently: -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 ;

[0367] W indicates

[0368] 3-14 membered cycloalkyl groups, which are saturated or unsaturated; unsubstituted, monosubstituted or polysubstituted; specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; or

[0369] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, they are unsubstituted, monosubstituted, or polysubstituted;

[0370] in

[0371] R W and R X Represented independently of each other in each case.

[0372] -H;

[0373] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0374] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0375] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically, the 3-14 membered cycloalkyl group is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0376] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0377] R Y1 R Y2 R Y3 and R Y4 Represented independently of each other in each case.

[0378] -H;

[0379] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0380] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0381] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0382] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0383] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0384] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0385] Furthermore, "monosubstituted or polysubstituted" in each case independently means substituted by one or more substituents independently selected from the following: -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), -C1-6 -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, -C1-6 -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 heterocyclic alkyl), -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).

[0386] In some embodiments, T represents -O-, and U represents -(CR) 5 R 5 ') n -; and n is an integer selected from 1, 2 or 3.

[0387] In some embodiments, R 1 express

[0388] -H, -F, -Cl, -Br, -I, CN;

[0389] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0390] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0391] -OH;

[0392] -OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0393] -NH2;

[0394] NHC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0395] -N(C 1-6 -alkyl)2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0396] -NHC(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0397] -NC 1-6 -alkyl C(=O)C 1-6 -alkyl groups, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0398] -SH;

[0399] -SC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0400] -C(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0401] -C(=O)OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0402] -C(=O)NH2;

[0403] -C(=O)NHC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0404] -C(=O)N(C 1-6 -alkyl)2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0405] -S(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0406] -S(=O)2-C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0407] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0408] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0409] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0410] In some embodiments, R 1 express

[0411] -H, -F, -Cl, -Br, -I, CN;

[0412] -C 1-6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, wherein in each case they are unsubstituted and independently mono- or polysubstituted 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;

[0413] -C1-C6-heteroalkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0414] -OH;

[0415] -OC 1-6 -alkyl, -O-C2-C6-alkenyl, -O-C2-C6-ynyl, wherein in each case they are unsubstituted and independently mono- or polysubstituted 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;

[0416] -NH2;

[0417] -NHC 1-6 -alkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0418] -N(C 1-6 -alkyl)2, wherein in each case the substituents are unsubstituted and independently selected from the group consisting of mono- or polysubstituted groups: -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;

[0419] -NHC(=O)C 1-6-alkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0420] -NC 1-6 -alkyl C(=O)C 1-6 -alkyl groups, which in each case are unsubstituted and independently monosubstituted or polysubstituted 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;

[0421] -SH;

[0422] -SC 1-6 -alkyl, -S-C2-C6-alkenyl, -S-C2-C6-ynyl, wherein in each case they are unsubstituted and independently mono- or polysubstituted 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;

[0423] -C(=O)C 1-6 -alkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0424] -C(=O)OC 1-6 -alkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0425] -C(=O)NH2;

[0426] -C(=O)NHC 1-6 -alkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0427] -C(=O)N(C 1-6 -alkyl)2, wherein in each case the substituents are unsubstituted and independently selected from the group consisting of mono- or polysubstituted groups: -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;

[0428] -S(=O)C 1-6 -alkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0429] -S(=O)2-C 1-6 -alkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0430] -C1-C6-heteroalkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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

[0431] 3-14 membered cycloalkyl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, and monosubstituted or polysubstituted with substituents independently 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;

[0432] 3-14 membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; specifically, 3-14 membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein said 3-14 membered heterocyclic alkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, unsubstituted, and monosubstituted or polysubstituted by substituents independently 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.

[0433] In some embodiments, R 1 This represents -H, -F, -Cl, -Br, -I, -CN, and -C. 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, -OH, -OC1-6 -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. Preferably, R 1 This represents -H, -F, -Cl, -Br, -I, CN, and -C. 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, -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 -cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl, or unsubstituted cyclohexyl.

[0434] 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 This 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.

[0435] 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.

[0436] In some embodiments, R 3 express

[0437] -H;

[0438] -OH;

[0439] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0440] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0441] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0442] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0443] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0444] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0445] In some embodiments, R 3 express

[0446] -H;

[0447] -OH;

[0448] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, wherein in each case they are unsubstituted and independently mono- or polysubstituted 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;

[0449] -C1-C6-heteroalkyl groups, which are unsubstituted, mono- or polysubstituted, independently 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;

[0450] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein said 3-14 membered cycloalkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are unsubstituted and independently monosubstituted or polysubstituted 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, specifically 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein said 3-14 membered cycloalkyl is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is unsubstituted and monosubstituted or polysubstituted independently of 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;

[0451] 3-14 membered heterocyclic alkyl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein said 3-14 membered heterocyclic alkyl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, and monosubstituted or polysubstituted with substituents independently 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;;

[0452] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are unsubstituted and independently monosubstituted or polysubstituted 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

[0453] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein said 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, and monosubstituted or polysubstituted by substituents independently 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.

[0454] In some embodiments, R 3 express

[0455] -H;

[0456] -OH;

[0457] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0458] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0459] Preferably, R 3 Represents -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. More preferably, R 3 Represents -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. Preferably, R 3It represents -H, -OH, or a saturated, unsubstituted, or monosubstituted -C. 1-6 -alkyl. Preferably, R 3 It represents -H.

[0460] In some embodiments, R 3 and R 4 Neither of them indicates -H. In some embodiments, R 3 It represents -H, and R 4 It does not represent -H.

[0461] In some embodiments, R 4 express

[0462] -H;

[0463] -S(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0464] -S(=O)2-C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0465] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0466] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0467] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0468] 3-14-membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, specifically 3-14-membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14-membered heterocyclic alkyl group is optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0469] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl group is optionally linked by a -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0470] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 5-14-membered heteroaryl groups are optionally linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0471] Preferably, R 4 express

[0472] -S(=O)2C 1-6 -alkyl groups, which are unsubstituted, mono- or polysubstituted groups independently 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0473] -S(=O)2(3-14 membered cycloalkyl), wherein the 3-14 membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, which in each case is saturated or unsaturated, unsubstituted, and independently mono- or poly-substituted 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)OC1-6 -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0474] -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, wherein the substituents are unsubstituted and independently selected from the group consisting of mono- or polysubstituted groups: -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0475] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, which in each case is saturated or unsaturated, and which in each case is unsubstituted and independently monosubstituted or polysubstituted with 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl; specifically 3-14-membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, which in each case is saturated or non-aromatic unsaturated, and which in each case is unsubstituted and independently monosubstituted or polysubstituted with 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0476] 3-14 membered heterocyclic alkyl or -C 1-6 -alkylene-(3-14 membered heterocyclic alkyl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered heterocyclic alkyl group is selected from the group consisting of: aziridine, 1,4-oxazacycloheptane, aziridine, aziridine, aziridine, aziridine, diazacycloheptane, dioxane, dioxane, dithiazoline, imidazoline, isothiazidine, isoxazidine, morpholine, oxazidine, hexane oxide, oxazidine, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, thiohexacyclobutane, thiohexacyclopropane, thiohexacyclopentane, thiomorpholine Indoline, dihydrobenzofuran, benzodioxane, 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-pyrrolizine, hexahydrocyclopentano[c]pyrrole, octahydrocyclopentano[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; in each case, they are unsubstituted, monosubstituted or polysubstituted by substituents selected independently 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0477] -Phenyl, which is an unsubstituted, mono- or polysubstituted substituent, independently 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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0478] 5-14 heteroaryl or -C 1-6 -alkylene-(5-14-membered heteroaryl), wherein -C 1-6The -alkylene group is either unsubstituted or monosubstituted with -OH, wherein the 5-14 heteroaryl group is selected from the group consisting of: benzimidazole, benzisoxazole, benzoxazole, benzofuran, benzothiadiazole, benzothiazazole, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazon, imidazole, imidazopyridine, indazole, indole, indazine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole Naphthylidine, oxadiazole, oxazole, hydroxyindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazolium, thiadiazole, thiazolium, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine; which in each case are unsubstituted, and are independently selected from the group consisting of mono- or polysubstituted substituents: -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl.

[0479] Preferably, R 4 express

[0480] -H;

[0481] -S(=O)2C 1-6 -alkyl group, which is mono- or poly-substituted with -F;

[0482] -S(=O)2 (3-14 membered cycloalkyl), which is unsubstituted;

[0483] -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, which are mono- or di-substituted groups independently 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;

[0484] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered cycloalkyl group is saturated, unsubstituted, and independently monosubstituted or disubstituted with 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;

[0485] 3-14 membered heterocyclic alkyl or -C 1-6 -alkylene-(3-14 membered heterocyclic alkyl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted with -OH, wherein the 3-14 membered heterocyclic alkyl group is selected in each case from aziridine, 1,4-oxazacycloheptane, pyrrolidine, piperidine, aziridine, diazacycloheptane, tetrahydrofuran, tetrahydropyran, oxazacyclobutane, morpholine, piperazine, hexahydrocyclopentanop[c]pyrrole, octahydrocyclopentanop[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabis(2-dimethylbenzene)pyrrole, 1,4-oxazacycloheptane, pyrrolo[1,2-a]pyrazine ... Cyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinine ring, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiocyclohexane, wherein in each case, the substituents are unsubstituted and independently selected from the group consisting of mono- or poly-substituted groups: -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, oxetyl, pyrimidinyl, -C 1-6 -alkylene-phenyl;

[0486] Unsubstituted -phenyl;

[0487] 5-14 heteroaryl or -C 1-6 -alkylene-(5-14-membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, wherein the 5-14-membered heteroaryl group is selected from the group consisting of: pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, which is unsubstituted and independently monosubstituted or disubstituted with substituents selected from the group consisting of: -C 1-6 -alkyl, -OH.

[0488] In some embodiments, R 4 express

[0489] Residues selected from the following groups:

[0490]

[0491] or

[0492] C1-C6-alkyl, which is unsubstituted, monosubstituted or polysubstituted; preferably representing residue -CR'R”-(CH2). m -OH, where m is an integer selected from 1, 2, 3, 4, 5 or 6, preferably selected from 1, 2 or 3; and where 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, -C 1-3 -alkylene-OH, -C(=O)-NH2, -C(=O)-NH-C 1-3 -alkyl or -C(=O)-N(C) 1-3 -alkyl)2; -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, -C 1-3 -alkyl group, -C substituted with OH 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; -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, -C 1-3 -alkyl group, -C substituted with OH 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 1-3 -alkylene(CF3)-NH2, -C(=O)-NH2, -C(=O)-NH-C 1-3 -alkyl or -C(=O)-N(C) 1-3 -alkyl)2; -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 -H, -CH3, -CH3CH2(OH)- substituted with OH, -C 1-3 -alkylene-OH, -C(CF3)-NH2, -C 1-3 -alkylene-CF3, -C 1-3-alkylene-CFH2, -C 1-3 -alkylene-O-CH3, 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' nor R” represents -H; preferably, it represents residues selected from the group consisting of:

[0493]

[0494]

[0495] or;

[0496] 3-14 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-13 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-12 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-11 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-10 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably representing cycloalkyl residues selected from the group consisting of:

[0497]

[0498] or;

[0499] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl group is linked by a -C1-C6-alkylene group, and is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-12 membered cycloalkyl group is linked by a -C1-C6-alkylene group, and is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered cycloalkyl groups. The 3-10 membered cycloalkyl group is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-10 membered cycloalkyl group is linked by a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered cycloalkyl group is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-8 membered cycloalkyl group is linked by a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; specifically 3-14 membered cycloalkyl group is saturated or non-aromatic. Aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted compounds; wherein the 3-14 membered cycloalkyl group is linked by a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-12 membered cycloalkyl group, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted; wherein the 3-12 membered cycloalkyl group is linked by a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-10 membered cycloalkyl group, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted. Non-aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted residues; wherein the 3-10 membered cycloalkyl group is linked by a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted residues; preferably 3-8 membered cycloalkyl group, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted residues; wherein the 3-8 membered cycloalkyl group is linked by a -C1-C6-alkylene group and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted residues; preferably residues selected from the group consisting of:

[0500]

[0501] 3-14 membered heterocyclic alkyl groups, which are saturated, unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-13 membered heterocyclic alkyl groups, which are saturated, unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-12 membered heterocyclic alkyl groups, which are saturated, unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-11 membered heterocyclic alkyl groups, which are saturated, unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-10 membered heterocyclic alkyl groups, which are saturated, unsaturated, unsubstituted, monosubstituted, or polysubstituted; specifically, 3-14 membered heterocyclic alkyl groups, which are saturated and non-aromatic. The heterocyclic alkyl group is unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-13 membered heterocyclic alkyl, which is saturated, non-aromatic, unsubstituted, monosubstituted, or polysubstituted; preferably 3-12 membered heterocyclic alkyl, which is saturated, non-aromatic, unsubstituted, monosubstituted, or polysubstituted; preferably 3-11 membered heterocyclic alkyl, which is saturated, non-aromatic, unsubstituted, monosubstituted, or polysubstituted; preferably 3-10 membered heterocyclic alkyl, which is saturated, non-aromatic, unsubstituted, monosubstituted, or polysubstituted; preferably, it represents a heterocyclic alkyl residue selected from the group consisting of:

[0502]

[0503]

[0504] or

[0505] 3-14 membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered heterocyclic alkyl groups are linked by -C1-C6-alkylene groups, and are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-12 membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-12 membered heterocyclic alkyl groups are linked by -C1-C6-alkylene groups, and are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-10 membered heterocyclic alkyl groups. Alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-10 membered heterocyclic alkyl groups are linked by -C1-C6-alkylene- and are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably 3-8 membered heterocyclic alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-8 membered heterocyclic alkyl groups are linked by -C1-C6-alkylene- and are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; specifically 3-14 membered heterocyclic alkyl groups, which are saturated or unsubstituted... Aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted heterocyclic alkyl groups; wherein the 3-14 membered heterocyclic alkyl groups are linked by -C1-C6-alkylene groups and are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-12 membered heterocyclic alkyl groups, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted; wherein the 3-12 membered heterocyclic alkyl groups are linked by -C1-C6-alkylene groups and are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-10 membered heterocyclic alkyl groups, which are saturated Or non-aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted; wherein the 3-10 membered heterocyclic alkyl group is linked by -C1-C6-alkylene- and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-8 membered heterocyclic alkyl group, which is saturated or non-aromatic unsaturated, unsubstituted, monosubstituted, or polysubstituted; wherein the 3-8 membered heterocyclic alkyl group is linked by -C1-C6-alkylene- and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably representing residues selected from the group consisting of:

[0506]

[0507] or

[0508] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; preferably 6-12 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; preferably 6-10 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; preferably 6-8 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; or

[0509] 6-14 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-14 aryl groups are linked by -C1-C6-alkylene groups, and are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 6-12 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-12 aryl groups are linked by -C1-C6-alkylene groups, and are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 6-10 aryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 6-10 aryl groups are linked by -C1-C6-alkylene groups, and are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably, residues selected from the group consisting of:

[0510]

[0511] or

[0512] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; preferably 5-12-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; preferably 5-10-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; preferably 5-9-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; preferably representing residues selected from the group consisting of:

[0513]

[0514]

[0515]

[0516] More preferably, residues selected from the group consisting of:

[0517]

[0518] or

[0519] 5-14-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 5-14-membered heteroaryl groups are linked by -C1-C6-alkylene groups, and are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably 5-12-membered heteroaryl groups, which are unsubstituted, monosubstituted, or polysubstituted; wherein the 5-12-membered heteroaryl groups are linked by -C1-C6-alkylene groups, and are saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; 5-10-membered heteroaryl groups aryl group, which is unsubstituted, monosubstituted, or polysubstituted; wherein the 5-10-membered heteroaryl group is linked by a -C1-C6-alkylene group, and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; 5-8-membered heteroaryl group, which is unsubstituted, monosubstituted, or polysubstituted; wherein the 5-8-membered heteroaryl group is linked by a -C1-C6-alkylene group, and is saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; preferably, it represents residues selected from the group consisting of:

[0520]

[0521] In some embodiments, R 4 This indicates the residues according to general formula (A).

[0522]

[0523] in

[0524] m A It is 0 or 1;

[0525] Y A Selected from -O-, -NR A6 -and-CR A7 R A8 -;and

[0526] R A1 R A2 R A3 R A4 R A5 R A6 R A7 and R A8 -H, -F, and -C can be represented 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-oxetanebutyl; or R A7 and R A8 It forms a ring with the carbon atom to which it is attached and is represented as -CH2OCH2-, -CH2OCH2CH2-, or -CH2CH2OCH2CH2-, -CH2NHCH2-, -CH2NHCH2CH2-, or -CH2CH2NHCH2CH2-.

[0527] In some embodiments, R 4 Represents residues according to the general formula (A) as defined above, wherein

[0528] m A It is 0 or 1;

[0529] Y A Selected from -O- and -CR A7 R A8 -;and

[0530] R A1 R A2 R A3 R A4 R A5 R A7 and R A8 -H and -C are represented independently of each other. 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C) 1-3 -alkyl)2 or -C(=O)NH2; preferably, the condition is R A1 R A2 R A3 R A4 R A5 R A7 and R A8 Only one of them indicates that it is not a -H residue.

[0531] In some embodiments, R 4 Represents residues according to the general formula (A) as defined above, wherein

[0532] m A It is 0 or 1;

[0533] Y A Selected from -O- and -CR A7R A8 -;and

[0534] R A1 Indicates -C 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C) 1-3 -alkyl)2 or -C(=O)NH2; and

[0535] R A2 R A3 R A4 R A5 R A7 and R A8 It represents -H.

[0536] In some embodiments, R 4 This indicates the residues according to general formula (B).

[0537]

[0538] in

[0539] Y B Selected from -O-, -NR B8 -and-CR B9 R B10 -;and

[0540] R B1 R B2 R B3 R B4 R B5 R B6 R B7 R B8 R B9 and R B10 They can be represented independently as -H, -F, -OH, -C(=O)-NH2, and -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 means =O; or R B4 and R B5 Together they represent = O.

[0541] In some embodiments, R 4 Represents residues according to the general formula (B) as defined above, wherein

[0542] Y B Selected from -O- and -NR B8 -;and

[0543] R B1 R B2 R B3 R B4 R B5 R B6 R B7 R B8 -H, -F, and -C can be represented 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 means =O; or R B4 and R B5 Together means = 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 residues in the R group represent residues that are not -H; the preferred condition is R. A1 R A2 R A3 R A4 R A5 R A7 and R A8 At least one of them indicates a residue that is not -H.

[0544] In some embodiments, R 4 This indicates the residues according to the general formula (C).

[0545]

[0546] in

[0547] 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 -;

[0548] 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 They can be represented independently as -H, -F, -OH, and -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 means =O; or R C4 and R C5 Together means =O; or R C9 and R C10 Together means =O; or R C11 and R C12 Together they represent = O.

[0549] In some embodiments, R 4 Represents residues according to the general formula (C) as defined above, where

[0550] 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 -;

[0551] R C1 R C2 R C3 RC4 R C5 R C6 R C7 R C8 R C9 R C10 R C11 and R C12 -H, -F, and -C can be represented independently of each other. 1-3 -alkyl, -C 1-3 -alkylene-OH or -C(=O)-NH2; preferably, the condition is 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 residues in the R group represent residues that are not -H; the preferred condition is 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 them indicates a residue that is not -H.

[0552] In some embodiments, R 4 express

[0553] (i) residue -CR'R”-(CH2) m -OH, where m is an integer from 1 to 6, preferably from 1 to 3; and where 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, neither R' nor R” represents -H; or

[0554] (ii) Based on the residues of general formula (D),

[0555]

[0556] in

[0557] m D and n D Each of the following is independent of the other: 0, 1, 2, or 3; the preferred condition is m. D +n D ≤3;

[0558] 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 -;

[0559] 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 They can be represented independently of each other: -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 means =O; or R D4 and R D5 Together means =O; or R D9 and R D10 Together means =O; or R D11 and R D12 Together means = 0;

[0560] Preferably, wherein

[0561] m D and n D Each of the following is independent of the other: 0, 1, 2, or 3; the preferred condition is m. D +n D ≤3;

[0562] 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 -;

[0563] 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 They can be represented independently of each other: -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 means =O; or R D4 and R D5 Together means =O; or R D9 and R D10 Together means =O; or R D11 and R D12 Together means = 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 residues in the R group represent residues that are not -H; the preferred condition is 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 them indicates a residue that is not -H.

[0564] In some embodiments, R 4 Represents residues according to general formulas (A), (B), (C), and (D), or as described herein, formula -CR'R”-(CH2). m -OH residues.

[0565] In some embodiments, R 4 Residues selected from the following group: -CH3,

[0566]

[0567]

[0568] In some embodiments, R 3 It is H, and R 4 This refers to any of the embodiments described above.

[0569] In some embodiments, R 5 and R 5 'represented independently of each other'

[0570] -H;

[0571] -C1-C6-alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0572] -C1-C6-heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0573] 3-14 membered cycloalkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked by -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 linked by -C1-C6-alkylene- or -C1-C6-heteroalkylene-, which in each case is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0574] Preferably, R 5 and R 5 'Independently represent -H, -C1-C6-alkyl or -C1-C6-alkylene-N(C1-C6-alkyl)2.

[0575] In some embodiments, R 5 and R 5 At least one of them is not -H.

[0576] In some embodiments, R 5 and R 5 Both are -H.

[0577] In a preferred embodiment, T represents -O-, and U represents -(CR) 5 R 5 ') n And the obtained part -O-(CR 5 R 5 ') n - Residues selected from the following groups:

[0578]

[0579]

[0580] In some embodiments, R 5 It represents -H, and R 5 'Indicates residues selected from the following groups: -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.

[0581] In some embodiments, R6 R 7 and R 8 Representing each other independently

[0582] -H;

[0583] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;

[0584] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0585] -OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0586] -NHC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0587] -N(C 1-6 -alkyl)2, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0588] -C(=O)OC 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0589] -OC(=O)C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0590] -C 1-6 - Heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0591] In some embodiments, R 6 R 7 and R 8 Representing each other independently

[0592] -H;

[0593] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;

[0594] -C 1-6 -alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, wherein in each case they are saturated or unsaturated, unsubstituted, and mono- or polysubstituted with substituents selected independently from the group consisting of: -F, -Cl, -C 1-6 -alkyl, -C1-6 -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0595] -OC 1-6 -alkyl groups, which are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted groups: -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0596] -NHC 1-6 -alkyl groups, which are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted groups: -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、-C1-6 -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0597] -N(C 1-6 -alkyl)2, wherein the substituents are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted groups: -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0598] -C(=O)OC 1-6 -alkyl groups, which are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted groups: -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 heterocyclic alkyl; and unsubstituted 5-14-membered heteroaryl;

[0599] -OC(=O)C 1-6-alkyl groups, which are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted groups: -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 heterocyclic alkyl groups; and unsubstituted 5-14-membered heteroaryl groups.

[0600] -C 1-6 -Heteroalkyl groups, which are saturated or unsaturated, unsubstituted, and independently selected from the group consisting of mono- or polysubstituted substituents: -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, -NHC1-6 -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 heterocyclic alkyl groups; and unsubstituted 5-14-membered heteroaryl groups.

[0601] Preferably, R 6 R 7 and R 8 Representing each other independently

[0602] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2,

[0603] -C 1-6 -alkyl, -CF3, -CHF2, -CH2F,

[0604] -OC 1-6 -alkyl, -OCF3, -OCHF2, -OCH2F,

[0605] -NHC1-6-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;

[0606] -N(C1-6-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;

[0607] -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;

[0608] -OC(=O)C 1-6 -alkyl group, 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

[0609] -C 1-6 - Heteroalkyl groups, which are 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.

[0610] In some embodiments, R 6 R 7 and R 8 Residues selected independently from the following groups: -H, -F, -Cl, -Br, -I, -CN, C 1-3-alkyl, -CF3, -CF2H and -CFH2; preferably -H or -F.

[0611] In some embodiments, R 6 It represents -H, -F, -Cl, -CN or -C1-C6-alkyl.

[0612] In some embodiments, R 6 The residues selected from the group consisting of -H, -F, -Cl, -CN or -CH3 are preferred.

[0613] In some embodiments, R 6 It does not represent -H.

[0614] In some embodiments, R 7 It represents -H, -F, -Cl, -CN or -C1-C6-alkyl.

[0615] In a preferred embodiment of the benzofuran derivative according to the present invention, R 7 It does not represent -H.

[0616] In some embodiments, R 7 The residues selected from the group consisting of: -H, -F, -Cl, -CN or CH3; preferably -H, -F, -Cl or -CH3.

[0617] In some embodiments, R 6 R 7 and R 8 The residues that represent the groups selected independently from the following groups are: -H, -F, -Cl, -Br, -I, -CN, C 1-6 -alkyl, -CF3, -CF2H, -CFH2; or

[0618]

[0619] In some embodiments of the benzofuran derivative according to the present invention, R 8 It represents -H, -F, -Cl, -CN or -C1-C6-alkyl.

[0620] In some embodiments of the benzofuran derivative according to the present invention, R 8 It does not represent -H.

[0621] In some embodiments, R 8 The residues selected from the group consisting of: -H, -F, -Cl, -CN or CH3; preferably -F.

[0622] In some embodiments of the benzofuran derivatives according to the present invention

[0623] (i)R 6 R 7 and R 8 Each represents -H; or

[0624] (ii)R 6 R 7 and R 8 Both in the text represent -H, and R 6 R 7 and R 8 The other one represents -F, -Cl, -CN, or -CH3; or

[0625] (iii)R 6 R 7 and R 8 One of them represents -H, and R 6 R 7 and R 8 The other one in the series can be represented independently as -F, -Cl, -CN, or -CH3.

[0626] In some embodiments, W represents

[0627] 3-14 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; specifically 3-14 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; or

[0628] 3-12 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; specifically 3-12 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; or

[0629] 3-10 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; specifically 3-10 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; or

[0630] 3-8 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; specifically 3-8 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; or

[0631] 3-6 membered cycloalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or tetrasubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted; specifically 3-6 membered cycloalkyl groups, which are saturated or non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; preferably unsubstituted, monosubstituted or tetrasubstituted; preferably unsubstituted, monosubstituted or trisubstituted; preferably unsubstituted, monosubstituted or disubstituted.

[0632] The substituents thereon 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、-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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14 membered heteroaryl; or

[0633] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, the substituents are unsubstituted and independently monosubstituted or disubstituted 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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl.

[0634] In some embodiments, W represents a 3-10 membered cycloalkyl group, which is saturated or unsaturated, unsubstituted, monosubstituted or disubstituted, or -C1-C6-alkyl, halo-C 1-6 Alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, which are unsubstituted, monosubstituted or disubstituted, specifically 3-10 membered cycloalkyl, which are saturated or non-aromatic unsaturated, unsubstituted, monosubstituted or disubstituted, or -C1-C6-alkyl, halogenated C 1-6 Alkyl, -C2-C6-enyl, -C2-C6-ynyl, which are unsubstituted, monosubstituted, or disubstituted; preferably W represents a 3- to 10-membered cycloalkyl group, which is saturated or unsaturated, selected from the group consisting of: cyclopropyl, cyclopropenyl, cyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, 1,3-cyclohexadienyl, 1,4-cyclohexadienyl, 1,5-cyclooctadienyl alkyl, 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, decahydronaphthyl, adamantyl, spiro[3.3]hept-2-yl, 3-bicyclo[3.1.0]hexyl, which in each case are unsubstituted, monosubstituted or disubstituted; or -C1-C6-alkyl, halogenated C 1-6 Alkyl, -C2-C6-enyl, -C2-C6-ynyl, which in each case are unsubstituted, monosubstituted or disubstituted; preferably W represents a 3-10 membered cycloalkyl group, which is saturated or non-aromatic unsaturated, selected from the group consisting of: cyclopropyl, cyclopropenyl, cyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, 1,3-cyclohexadienyl, 1,4-cyclohexadienyl, 1,5-cyclooctadienyl, bicyclo[2.2] [3.1] Hept-2-yl, (1S,4R)-norborn-2-yl, (1R,4R)-norborn-3-yl, (1S,4S)-norborn-2-yl, (1R,4S)-norborn-2-yl, decahydronaphthyl, adamantyl, spiro[3.3]hept-2-yl, 3-bicyclo[3.1.0]hexyl, bicyclo[1.1.1]pentane, cis-bicyclo[3.1.0]hexane, which in each case are unsubstituted, monosubstituted or disubstituted; or -C1-C6-alkyl, halogenated C 1-6Alkyl, -C2-C6-alkenyl, -C2-C6-ynyl, which in each case are unsubstituted, monosubstituted, or disubstituted; preferably W represents a 3-10 membered cycloalkyl group, which is saturated or unsaturated, unsubstituted, 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; preferably W represents a 3-10 membered cycloalkyl group, which is saturated or unsaturated, selected from the group consisting of: 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)-norbornane-2-yl, (1R,4R)-norbornane Alkyl-3-yl, (1S,4S)-norbornan-2-yl, (1R,4S)-norbornan-2-yl, decahydronaphthyl, adamantyl, spiro[3.3]hept-2-yl, 3-bicyclo[3.1.0]hexyl, which in each case are unsubstituted, 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; preferably W represents a 3-10 membered cycloalkyl group, which is saturated or unsaturated, selected from the group consisting of: 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)-norbornen-2-yl, decalinyl, adamantyl, spiro[3.3]hept-2-yl, 3-bicyclo[3.1.0]hexyl, bicyclo[1.1.1]pentane, cis-bicyclo[3.1.0]hexane, which in each case are unsubstituted, 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.

[0635] In some embodiments, W represents

[0636] 3-14 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-13 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-12 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-11 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably 3-10 membered cycloalkyl groups, which are saturated, unsubstituted, monosubstituted, or polysubstituted; preferably representing cycloalkyl residues selected from the group consisting of:

[0637]

[0638]

[0639] or

[0640] -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-ynyl; in each case, the substituents are unsubstituted and independently mono- or polysubstituted 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 heterocyclic alkyl, unsubstituted -phenyl, 5 to 14-membered heteroaryl.

[0641] In some embodiments, the term "monosubstituted or polysubstituted" independently means, in each case, substitution by one or more substituents independently selected from the following: -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, -C1-6 -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 heterocyclic alkyl), -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 term in each case independently means substituted by one or more substituents independently selected from the following: -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, -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)-OC1-6 -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(C1-6 -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), -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 heterocyclic alkyl), -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 term in each case independently means substituted by one or more substituents independently selected from the following: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C1-6 -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, -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)-C1-6 -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(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, -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(C1-6 -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 heterocyclic alkyl), -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 term in each case independently means substituted by one or more substituents independently selected from the following: -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, -C1-6 -alkylene-(3-12 membered cycloalkyl), 3- to 12 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 12-membered heterocyclic alkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5 to 12-membered heteroaryl, -C 1-6 -alkylene- (5 to 12-membered heteroaryl); preferably, the term in each case independently means substituted by one or more substituents independently selected from the following: -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 heterocyclic alkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5 to 12-membered heteroaryl, -C 1-6 -alkylene- (5 to 12-membered heteroaryl); preferably, the term in each case independently means substituted by one or more substituents independently selected from the following: -F, -Cl, -Br, -I, -CN, -C 1-5 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-5 -alkylene-CF3, -C 1-5 -alkylene-NH-C 1-5 -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 group, -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 heterocyclic alkyl), -phenyl, -C 1-5 -alkylene-phenyl, 5 to 10-membered heteroaryl, -C 1-5 -alkylene-(5 to 10-membered heteroaryl).

[0642] In a preferred embodiment of the invention, the benzofuran derivative is selected from the group consisting of:

[0643] Cpd 001-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropionamide;

[0644] Cpd 002-(2S)-2-({5-[(2,2-difluorocyclopropyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxypropionamide;

[0645] Cpd 003-(2S)-2-[(5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-yl)formamido]-3-hydroxypropionamide;

[0646] Cpd 004-(2S)-2-{[2-cyclopropyl-5-(cyclopropylmethoxy)-1-benzofuran-3-yl]formamido}-3-hydroxypropionamide;

[0647] Cpd 005-(2S)-2-{[5-(2-cyclopropylethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropionamide;

[0648] Cpd 006-(2S)-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropionamide;

[0649] Cpd 007-(2S)-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}propionamide;

[0650] Cpd 008-(2S)-2-{[5-(cyclopropylmethoxy)-2-(difluoromethyl)-1-benzofuran-3-yl]formamido}-3-hydroxypropionamide;

[0651] Cpd 009-(2R)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropionamide;

[0652] Cpd 010-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}propionamide;

[0653] Cpd 011-(2S,3R)-2-[(5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-yl)formamido]-3-hydroxybutyramide;

[0654] Cpd 012-(2S,3R)-2-{[5-(2-cyclopropylethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxybutyramide;

[0655] Cpd 013-2-({5-[(2,2-difluorocyclopentyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxypropionamide;

[0656] Cpd 014-2-[(5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-yl)formamido]-3-hydroxy-2-methylpropionamide;

[0657] Cpd 015-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-2-methylpropionamide;

[0658] Cpd 016-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-2-methylpropionamide;

[0659] Cpd 017-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropionamide;

[0660] Cpd 018-5-(cyclobutylmethoxy)-N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-1-benzofuran-3-carboxamide;

[0661] Cpd 019-5-(cyclobutylmethoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methyl-1-benzofuran-3-carboxamide;

[0662] Cpd 020-5-(cyclohexylmethoxy)-2-methyl-N-(1-methylpiperidin-4-yl)-1-benzofuran-3-carboxamide;

[0663] Cpd 021-5-(cyclopropylmethoxy)-2-methyl-N-(1-methylpiperidin-4-yl)-1-benzofuran-3-carboxamide;

[0664] Cpd 022-5-(cyclopropylmethoxy)-2-methyl-N-(oxan-4-yl)-1-benzofuran-3-carboxamide;

[0665] Cpd 023-5-(cyclopropylmethoxy)-N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-1-benzofuran-3-carboxamide;

[0666] Cpd 024-5-(cyclopropylmethoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methyl-1-benzofuran-3-carboxamide;

[0667] Cpd 025-5-(cyclopropylmethoxy)-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-1-benzofuran-3-carboxamide;

[0668] Cpd 026-5-(cyclopropylmethoxy)-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzofuran-3-carboxamide;

[0669] Cpd 027-5-(cyclopropylmethoxy)-N-[3-(hydroxymethyl)-2-oxopiperidin-3-yl]-2-methyl-1-benzofuran-3-carboxamide;

[0670] Cpd 028-5-(cyclopropylmethoxy)-N-[3-(hydroxymethyl)-2-oxopyrrolidone-3-yl]-2-methyl-1-benzofuran-3-carboxamide;

[0671] Cpd 029-5-(cyclopropylmethoxy)-N-[3-(hydroxymethyl)oxetane-3-yl]-2-methyl-1-benzofuran-3-carboxamide;

[0672] Cpd 030-5-(cyclopropylmethoxy)-N-[4-(hydroxymethyl)oxane-4-yl]-2-methyl-1-benzofuran-3-carboxamide;

[0673] Cpd 031-5-[(2,2-difluorocyclopropyl)methoxy]-N-(3,3-difluoropiperidin-4-yl)-2-methyl-1-benzofuran-3-carboxamide;

[0674] Cpd 032-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-[(1-methylcyclopropyl)methoxy]-1-benzofuran-3-carboxamide;

[0675] Cpd 033-N-(3,3-difluoropiperidin-4-yl)-5-[(2,2-dimethylcyclopropyl)methoxy]-2-methyl-1-benzofuran-3-carboxamide;

[0676] Cpd 034-N-(3-carbamoyloxetane-3-yl)-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide;

[0677] Cpd 035-N-(3-carbamoyloxacyclopentan-3-yl)-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide;

[0678] Cpd 036-N-(3-carbamoyloxacyclopentan-3-yl)-5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-carboxamide;

[0679] Cpd 037-N-(4-carbamoyloxane-4-yl)-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide;

[0680] Cpd 038-(2S)-2-{[5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropionamide;

[0681] Cpd 039-(2S)-2-{[5-(2,2-dimethylpropoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropamide;

[0682] Cpd 040-(2S,3R)-2-{[5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxybutyramide;

[0683] Cpd 041-2-{[5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropionamide;

[0684] Cpd 042-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(2-methylpropoxy)-1-benzofuran-3-carboxamide;

[0685] Cpd 043-N-(3,3-difluoropiperidin-4-yl)-5-(2,2-dimethylpropoxy)-2-methyl-1-benzofuran-3-carboxamide;

[0686] Cpd 044-N-(3-carbamoyloxetane-3-yl)-5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-carboxamide;

[0687] Cpd 045-2-{[5-(cyclopropylmethoxy)-6-fluoro-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropionamide;

[0688] Cpd 046-5-(cyclopropylmethoxy)-N-(4,4-difluoro-1-hydroxy-2-methylbut-2-yl)-2-methyl-1-benzofuran-3-carboxamide;

[0689] Cpd 047-3-hydroxy-2-methyl-2-{[2-methyl-5-(2,2,2-trifluoroethoxy)-1-benzofuran-3-yl]formamido}acrylamide;

[0690] Cpd 048-3-Hydroxy-2-methyl-2-[(2-methyl-5-{[1-(trifluoromethyl)cyclopropyl]methoxy}-1-benzofuran-3-yl)formamido]acrylamide;

[0691] Cpd 049-2-({5-[(2,2-dimethylcyclopropyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxy-2-methylpropionamide;

[0692] Cpd 050-cis-2-{[5-({bicyclo[3.1.0]hex-3-yl}methoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropionamide

[0693] Cpd 051-trans-2-{[5-({bicyclo[3.1.0]hex-3-yl}methoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropionamide;

[0694] Cpd 052-3-hydroxy-2-methyl-2-{[2-methyl-5-({3-methylbicyclo[1.1.1]pent-1-yl}methoxy)-1-benzofuran-3-yl]formamido}acrylamide;

[0695] Cpd 053-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropionamide;

[0696] Cpd 054-2-({5-[(3,3-difluorocyclobutyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxy-2-methylpropionamide;

[0697] Cpd 055-5-(cyclopropylmethoxy)-2-methyl-N-(2-oxopiperidin-3-yl)-1-benzofuran-3-carboxamide;

[0698] Cpd 056-N-[(2)-3-amino-4,4,4-trifluoro-1-hydroxybut-2-yl]-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide;

[0699] Cpd 057-5-[(2,2-difluorocyclopropyl)methoxy]-2-methyl-N-(4,4,4-trifluoro-1-hydroxybut-2-yl)-1-benzofuran-3-carboxamide;

[0700] Cpd 058-cis-3-hydroxy-2-methyl-2-({2-methyl-5-[(3-methylcyclobutyl)methoxy]-1-benzofuran-3-yl}formamido)acrylamide;

[0701] Cpd 059-trans-3-hydroxy-2-methyl-2-({2-methyl-5-[(3-methylcyclobutyl)methoxy]-1-benzofuran-3-yl}formamido)acrylamide;

[0702] Cpd 060-N-(1-hydroxy-3-methoxy-2-methylpropyl-2-yl)-2-methyl-5-{[1-(trifluoromethyl)cyclopropyl]methoxy}-1-benzofuran-3-carboxamide;

[0703] Cpd 061-2-Methyl-N-(3-methyl-2-oxopiridine-3-yl)-5-{[1-(trifluoromethyl)cyclopropyl]methoxy}-1-benzofuran-3-carboxamide;

[0704] Cpd 062-2-{[5-(cyclopentylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropionamide;

[0705] And its physiologically acceptable salt content.

[0706] This invention also covers pharmaceutical compositions comprising at least one compound of the present invention. Furthermore, this invention covers a pharmaceutical composition comprising at least one compound of the present invention and at least one acceptable carrier, excipient, or diluent for pharmaceutical purposes.

[0707] In some embodiments, the present invention relates to the use of at least one compound of formula (I) or any subgroup thereof in the prevention and / or treatment of pain or epilepsy; preferably in the treatment of pain or epileptic encephalopathy (for the preparation of compositions thereof).

[0708] In some embodiments, the present invention relates to a method for preventing and / or treating metabolic pain, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain; preferably postoperative pain.

[0709] Q, T, U, W, R 1 R 3 R 4 R 5 R 5 '、n、R 6 R 7 R 8 All definitions, preferred embodiments, and preferred meanings, including preferred substituents, are similarly applied to the benzofuran derivatives according to the invention, which are not necessarily limited to the treatment of pain or epilepsy. Therefore, this aspect of the invention relates to the benzofuran derivatives themselves, compositions comprising benzofuran derivatives, pharmaceuticals comprising benzofuran derivatives, and benzofuran derivatives for the prevention and / or treatment of TRPM3-mediated conditions such as pain, epilepsy, and / or inflammatory hypersensitivity; and / or for the treatment of pain, epilepsy, and / or inflammatory hypersensitivity. Preferably, the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain. More preferably, the pain is postoperative pain.

[0710] In a preferred embodiment of the invention, the benzofuran derivative is selected from the group consisting of Cpd 001 to Cpd 044 mentioned above and their physiologically acceptable salts. In a preferred embodiment of the invention, the benzofuran derivative is selected from the group consisting of Cpd 001 to Cpd 062 mentioned above and their physiologically acceptable salts.

[0711] Another aspect of the present invention relates to pharmaceutical compositions or drugs comprising benzofuran derivatives according to the present invention as described above.

[0712] The benzofuran derivatives of the present invention have been shown to be antagonists of TRPM3, and therefore the present invention provides compounds themselves that are used as medicines, more specifically medicines that prevent or treat TRPM3-mediated conditions in subjects by acting in an effective amount of the benzofuran derivatives of the present invention.

[0713] In a preferred embodiment of the invention, the benzofuran derivative of the invention is the only pharmacologically active compound in the administration therapy. In another preferred embodiment of the invention, the benzofuran derivative of the invention can be combined with other therapeutic agents for the treatment or prevention of TRPM3-mediated conditions. Therefore, the invention also relates to the use of compositions comprising:

[0714] - One or more compounds of the formulas and embodiments herein, and

[0715] - One or more additional therapeutic or preventive agents for the prevention or treatment of TRPM3-mediated conditions, wherein the one or more additional therapeutic or preventive agents are bioactive agents in the form of a combination formulation for simultaneous, separate or sequential use.

[0716] Pharmaceutical compositions or formulations according to the invention may contain the benzofuran derivatives of the invention in a wide range of contents, depending on the intended use and expected effect of the formulation. Typically, the content of the benzofuran derivatives of the invention in the formulation is in the range of 0.1 to 99.9% by weight, preferably 1 to 99% by weight, and more preferably 5 to 95% by weight.

[0717] Given the aforementioned facts, when several active ingredients are used in combination, these active ingredients do not necessarily produce their combined therapeutic effect simultaneously and directly in the mammal to be treated. The corresponding composition may also be in the form of a medical kit or package containing two ingredients in separate but adjacent reservoirs or compartments. In the latter case, each active ingredient can therefore be formulated in a manner suitable for a different route of administration than the other ingredients; for example, one of the active ingredients may be in the form of an oral or parenteral formulation, while the other active ingredient may be in the form of an ampoule or aerosol for intravenous injection.

[0718] Those skilled in the art will also recognize that the benzofuran derivatives of the present invention can exist in many different protonated states, depending in particular on the pH and other environmental conditions. While the structural formulas provided herein depict compounds in only one of several possible protonated states, it should be understood that these structures are illustrative only, and the invention is not limited to any particular protonated state—any and all protonated forms of the compounds are intended to fall within the scope of the invention.

[0719] As used herein, the term "pharmaceutically acceptable salt" means a therapeutically active, non-toxic salt form that compounds of the formulas herein can form. Therefore, the compounds of the present invention optionally comprise salts of the compounds herein, particularly containing, for example, Na. + Li + K + Ca 2+ and Mg2+ Pharmaceutically acceptable non-toxic salts. Such salts may comprise salts derived by combination of a suitable cation (such as an alkali and alkaline earth metal ion or an ammonium and quaternary ammonium ion) with an acid anionic moiety (typically a carboxylic acid). The benzofuran derivatives of the present invention may carry multiple positive or negative charges. The net charge of the benzofuran derivatives of the present invention may be positive or negative. Any associated counterions are generally determined by the synthetic and / or isolated methods used to obtain the compound. Typical counterions include, but are not limited to, ammonium, sodium, potassium, lithium, halides, acetates, trifluoroacetates, etc., and mixtures thereof. It should be understood that the identity of any associated counterion is not a key feature of the present invention, and the present invention covers compounds associated with any type of counterion. Furthermore, since compounds can exist in a variety of different forms, the present invention is intended to cover not only forms of compounds associated with counterions (e.g., dry salts) but also forms that do not associate with counterions (e.g., aqueous solutions or organic solutions). Metal salts are generally prepared by reacting a metal hydroxide with the compounds of the present invention. Examples of metal salts prepared in this manner are those containing Li + Na + and K + Salts. Metal salts with low solubility can be precipitated from solutions of salts with higher solubility by adding a suitable metal compound. Additionally, salts can be formed by the addition of certain organic and inorganic acids to a basic center (usually an amine) or an acidic group. Examples of such suitable acids include, for example, inorganic acids (such as hydrohalic acids), such as hydrochloric acid or hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, etc.; or organic acids, such as acetic acid, propionic acid, glycolic acid, 2-hydroxypropionic acid, 2-oxopropionic acid, lactic acid, pyruvic acid, oxalic acid (i.e., oxalic acid), malonic acid, succinic acid (i.e., succinic acid), maleic acid, fumaric acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, cyclohexylaminosulfonic acid, salicylic acid (i.e., 2-hydroxybenzoic acid), p-aminosalicylic acid, etc. Furthermore, this term also includes solvates, such as hydrates, alcohols, etc., that compounds of the formulas herein and their salts can form. Finally, it should be understood that the compositions herein comprise the benzofuran derivatives of the invention in their unionized and zwitterionic forms, and in their hydrated form in combination with a stoichiometric amount of water.

[0720] The scope of this invention also includes salts of parent compounds and one or more amino acids, particularly salts of naturally occurring amino acids found as protein components. Amino acids are typically those carrying side chains with basic or acidic groups (e.g., lysine, arginine, or glutamic acid) or neutral groups (e.g., glycine, serine, threonine, alanine, isoleucine, or leucine).

[0721] The benzofuran derivatives of the present invention also include their physiologically acceptable salts. Examples of physiologically acceptable salts of the benzofuran derivatives of the present invention include salts derived from suitable bases such as alkali metals (e.g., sodium), alkaline earth metals (e.g., magnesium), ammonium, and Nx4. + (where X is -C) 1-6 -alkyl). Physiologically acceptable salts of compounds containing hydrogen atoms or amino groups include salts of organic carboxylic acids (such as acetic acid, benzoic acid, lactic acid, fumaric acid, tartaric acid, maleic acid, malonic acid, malic acid, hydroxyethanesulfonic acid, lactobionic acid, and succinic acid); organic sulfonic acids (such as methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, and p-toluenesulfonic acid); and inorganic acids (such as hydrochloric acid, sulfuric acid, phosphoric acid, and aminosulfonic acid). Physiologically acceptable salts of compounds containing hydroxyl groups include salts of the anion of the compound with a suitable cation (such as Na+). + and NX4 + (where X is usually selected independently from -H or -C) 1-4 Combinations of alkyl groups. However, salts that are not physiologically acceptable acids or bases may also be used, for example, to prepare or purify physiologically acceptable compounds. All salts, whether or not derived from physiologically acceptable acids or bases, are within the scope of this invention.

[0722] Unless otherwise stated, as used herein, the term “enantiomer” means each individual optically active form of the benzofuran derivative of the present invention having an optical purity or enantiomer excess (determined by standard methods in the art) of at least 80% (i.e. at least 90% of one enantiomer and at most 10% of another enantiomer), preferably at least 90%, and more preferably at least 98%.

[0723] As used herein, the term "isomer" means all possible isomeric forms that a compound of the formula herein may have, including tautomers and stereochemical forms, but excluding positional isomers. Generally, the structures shown herein illustrate only one tautomer or resonance form of the compound, but corresponding alternative configurations are also contemplated. Unless otherwise stated, the chemical name of a compound represents a mixture of all possible stereochemical isomeric forms, containing all diastereomers and enantiomers of the basic molecular structure (because compounds of the formula herein may have at least one chiral center), as well as stereochemically pure or enriched compounds. More specifically, the stereocenter may have an R or S configuration, and multiple bonds may have cis or trans configurations.

[0724] The pure isomer form of the compound is defined as an isomer that substantially does not contain other enantiomers or diastereomers of the same basic molecular structure. Specifically, the terms "stereoisomerically pure" or "chirally pure" refer to a compound in which the stereoisomer excess is at least about 80% (i.e., at least 90% of one isomer and at most 10% of other possible isomers), preferably at least 90%, more preferably at least 94%, and most preferably at least 97%. The terms "enantiomerically pure" and "diastereomerically pure" should be understood in a similar manner, taking into account the enantiomeric excess and diastereomeric excess of the mixture, respectively.

[0725] The separation of stereoisomers is accomplished by standard methods known to those skilled in the art. One enantiomer of the benzofuran derivative of the present invention can be separated by methods such as forming diastereomers using optically active resolving agents (“Stereochemistry of Carbon Compounds”, (1962) L. Eliel, McGraw Hill; Lochmuller, CH, (1975) J. Chromatogr., 113:(3)283-302), substantially free of its opposite enantiomers. The separation of isomers in a mixture can be achieved by any suitable method, including: (1) forming ionic diastereomer salts with a chiral compound and separating by fractional crystallization or other methods; (2) forming diastereomer compounds with a chiral derivatizing agent, separating the diastereomers and converting them to pure enantiomers; or (3) the enantiomers can be directly separated under chiral conditions. In method (1), diastereomer salts can be formed by reacting an enantiomerically pure chiral base (such as brucine, quinine, ephedrine, strychnine, α-methyl-β-phenylethylamine) with an asymmetric compound carrying an acidic functional group (such as carboxylic acid and sulfonic acid). The diastereomer salts can be separated by fractional crystallization or ion chromatography. To separate the optical isomers of amino compounds, the addition of a chiral carboxylic acid or sulfonic acid (such as camphorsulfonic acid, tartaric acid, mandelic acid, or lactic acid) can lead to the formation of diastereomer salts. Alternatively, by method (2), the substrate to be separated can react with one enantiomer of a chiral compound to form a diastereomer pair (Eliel, E. and Wilen, S. (1994), *Stereochemistry of Organic Compounds*). (Compounds), John Wiley & Sons, Inc., p. 322). Diasteremeric compounds can be formed by reacting an asymmetric compound with an enantiomerically pure chiral derivatizing agent (such as a menthyl derivative), followed by separation of the diastereomer and hydrolysis to produce a free enantiomer-enriched compound. Methods for determining optical purity involve preparing a racemic mixture of chiral esters, such as menthyl ester or mosher ester, α-methoxy-α-(trifluoromethyl)phenylacetate (Jacob III. (1982) J. Org. Chem. 47:4165), and analyzing the presence of two diastereomers of the blocked transisomers in the NMR spectrum.According to the method used for separating the transisomer naphthyl-isoquinoline (Hoye, T., WO 96 / 15111), stable diastereomers can be separated and isolated by normal-phase chromatography and reversed-phase chromatography. In method (3), a racemic mixture of two asymmetric enantiomers is separated chromatographically using a chiral stationary phase. Suitable chiral stationary phases are, for example, polysaccharides, particularly cellulose or amylose derivatives. Commercially available polysaccharide-based chiral stationary phases are... CA, OA, OB5, OC5, OD, OF, OG, OJ, and OK, and AD, AS, OP(+), and OT(+). A suitable eluent or mobile phase used in combination with the chiral stationary phase of the polysaccharide is hexane modified with an alcohol (such as ethanol, isopropanol, etc.). (“Chiral Liquid Chromatography” (1989), edited by W.J. Lough, Chapman and Hall, New York; Okamoto Co., Ltd., (1990), “Optical resolution of dihydropyridine enantiomers by High-performance liquid chromatography using phenylcarbamates of polysaccharides as achiralstationary phase”, *Journal of Chromatography*, 513:375-378).

[0726] The terms cis and trans are used herein according to Chemical Abstracts nomenclature and include reference to the position of the substituent on the ring moiety. Those skilled in the art can readily determine the absolute stereochemical configuration of compounds of the formulas described herein using well-known methods such as X-ray diffraction.

[0727] When a compound crystallizes from a solution or slurry, it can crystallize in different spatially arranged lattice sites (this property is called "polymorphism") to form crystals with different crystalline forms, each of which is called a "polymorph". Therefore, as used herein, the term "polymorph" refers to the crystalline form of a compound of formula (I) in which the molecules are located in three-dimensional lattice sites. Different polymorphs of a compound of formula (I) can differ from each other in one or more physical properties, such as solubility and dissolution rate, true specific gravity, crystal form, accumulation mode, flowability, and / or solid-state stability.

[0728] The benzofuran derivatives of the present invention and their physiologically acceptable salts (hereinafter collectively referred to as the active ingredients) may be administered via any route suitable for the condition to be treated, including oral, rectal, nasal, topical (including ocular, buccal, and sublingual), vaginal, and parenteral (including subcutaneous, intramuscular, intranasal, intravenous, intraarterial, intradermal, intrathecal, and epidural). Preferred routes of administration may vary depending on, for example, the recipient's condition.

[0729] The therapeutically effective amount of the compound formulation, particularly for the treatment of TRPM3-mediated conditions in humans and other mammals or animals, is preferably the amount of TRPM3 ion channel inhibition of the compound as defined herein, and corresponds to an amount that ensures plasma levels are between 1 μg / ml and 100 mg / ml, optionally 10 mg / ml.

[0730] Appropriate doses of the compounds or compositions of the present invention are applied to treat or prevent TRPM3-mediated conditions in subjects. Depending on the pathological condition to be treated and the patient's condition, the effective dose may be divided into several subunits per day or may be administered at intervals of more than one day.

[0731] The present invention further provides (pharmaceutical) compositions comprising one or more benzofuran derivatives of the present invention, more specifically all formulas (I) and other formulas and embodiments described herein, and benzofuran derivatives of more specific aspects or embodiments thereof. Furthermore, the present invention provides compounds or (pharmaceutical) compositions of the present invention, more specifically all formulas (I) and other formulas and embodiments described herein, and compounds or (pharmaceutical) compositions of more specific aspects or embodiments thereof, said compounds or (pharmaceutical) compositions for use as medicines, more specifically, for treating pain or epilepsy. TRPM3-mediated conditions are selected from pain, epilepsy, and inflammatory hypersensitivity symptoms.

[0732] The benzofuran derivatives of the present invention can be formulated with conventional carriers and excipients, which will be selected according to conventional practice. The tablets will contain excipients, flow aids, fillers, binders, etc. The aqueous formulation is prepared aseptically and will generally be isotonic when intended for delivery by means other than oral administration. The formulation optionally contains excipients, such as those described in the "Handbook of Pharmaceutical Excipients" (1986).

[0733] Subsequently, as used herein, the term "pharmaceutically acceptable carrier" means any material or substance formulated with the active ingredient to facilitate its application or dispersal to the site of treatment, for example by dissolving, dispersing, or diffusing the composition, and / or facilitating its storage, transport, or handling without impairing its effectiveness. A pharmaceutically acceptable carrier can be a solid or liquid or a gas that has been compressed to form a liquid; that is, the compositions of the present invention can be suitably used as concentrates, emulsions, solutions, granules, powders, sprays, aerosols, suspensions, ointments, creams, tablets, pills, or powders.

[0734] Suitable pharmaceutical carriers for the pharmaceutical compositions and formulations thereof are well known to those skilled in the art, and there are no particular limitations on their selection within the present invention. They may also include additives such as wetting agents, dispersants, adhesives, binders, emulsifiers, surfactants, solvents, coatings, antibacterial and antifungal agents, isotonic agents, etc., provided that they are consistent with pharmaceutical practice, i.e., that the carrier and additives do not cause permanent harm to mammals. The pharmaceutical compositions of the present invention can be prepared in any known manner, for example by uniformly mixing, coating, and / or grinding the active ingredient with a selected carrier material and, where appropriate, other additives (such as surfactants) in one or more steps. They can also be prepared by micronization, for example, to obtain the pharmaceutical compositions in the form of microspheres typically having a diameter of about 1 to 10 μm, i.e., for the preparation of microcapsules for controlled or sustained release of the active ingredient.

[0735] While benzofuran derivatives can be administered alone, they are preferably present as pharmaceutical formulations. The formulations of the present invention for both veterinary and human use comprise at least one active ingredient as described above, and thus one or more pharmaceutically acceptable carriers and optionally other therapeutic ingredients. The carrier is preferably “acceptable” in the sense of compatibility with the other components of the formulation and harmlessness to the recipient. Formulations include those suitable for oral, rectal, nasal, topical (including buccal and sublingual), vaginal, or parenteral (including subcutaneous, intramuscular, intravenous, intradermal, intrathecal, and epidural) administration. Formulations can be conveniently presented in unit dosage forms and can be prepared by any method well known in the pharmaceutical industry. Such methods include the step of associating the active ingredient with a carrier constituting one or more auxiliary ingredients. Typically, formulations are prepared by homogeneously and tightly associating the active ingredient with a liquid carrier or a finely dispersed solid carrier, or both, and then shaping the product if necessary.

[0736] The formulations of the present invention suitable for oral administration can be presented as discrete units, such as capsules, sachets, or tablets each containing a predetermined amount of the active ingredient; as powders or granules; as solutions or suspensions in aqueous or non-aqueous liquids; or as oil-in-water or water-in-oil liquid emulsions. The active ingredient can also be presented as pellets, syrups, or pastes.

[0737] Tablets can be prepared by compression or molding, optionally with one or more excipients. Compressed tablets can be prepared by compressing an active ingredient in a free-flowing form (such as powder or granules) optionally mixed with a binder, lubricant, inert diluent, preservative, surfactant, or dispersant in a suitable machine. Molded tablets can be prepared by molding a mixture of powdered compounds wetted with an inert liquid diluent in a suitable machine. Tablets can optionally be coated or scored and can be formulated to provide a slow or controlled release of the active ingredient therein. For infections of the eyes or other external tissues (e.g., mouth and skin), the formulation is optionally applied as a topical ointment or cream containing, for example, 0.075 to 20% w / w (including the active ingredient in the range of 0.1% to 20%, in increments of 0.1% w / w, such as 0.6% w / w, 0.7% w / w, etc.), preferably 0.2 to 15% w / w, and most preferably 0.5 to 10% w / w. When formulated as an ointment, the active ingredient can be used with a paraffin or water-miscible ointment base. Alternatively, the active ingredient can be formulated into a cream using an oil-in-water cream base. If desired, the aqueous phase of the cream base may include, for example, at least 30% w / w of a polyol, i.e., an alcohol having two or more hydroxyl groups, such as propylene glycol, 1,3-diol, mannitol, sorbitol, glycerin, and polyethylene glycol (including PEG400) and mixtures thereof. Topical formulations may desiccately include compounds that enhance the absorption or penetration of the active ingredient across the skin or other affected areas. Examples of such transdermal penetration enhancers include dimethyl sulfoxide and related analogues.

[0738] The oil phase of the emulsion of the present invention can be composed of known ingredients in a known manner. Although the phase may contain only emulsifiers (also known as laxatives), it desirably includes at least one emulsifier with fats or oils, or with a mixture of both fats and oils. Optionally, hydrophilic emulsifiers are included together with lipophilic emulsifiers that act as stabilizers. Both oils and fats are also preferred. Emulsifiers, with or without stabilizers, together constitute a so-called emulsified wax, and the wax, together with the oils and fats, constitutes a so-called emulsified ointment matrix, which forms the oily dispersed phase of the ointment formulation.

[0739] The selection of a suitable oil or fat for the formulation is based on achieving the desired cosmetic properties, as the active compounds have very low solubility in most oils that may be used in pharmaceutical emulsion formulations. Therefore, the cream should optionally be a non-greasy, non-staining, and washable product with a suitable consistency to prevent leakage from tubes or other containers. Straight-chain or branched, mono- or dialkyl esters, such as diisoadipate, isocetyl stearate, coconut fatty acid propylene glycol diester, isopropyl myristate, decyl oleate, isopropyl palmitate, butyl stearate, 2-ethylhexyl palmitate, or blends of branched esters known as CrodamolCAP, the latter three being preferred, can be used. These can be used alone or in combination, depending on the desired properties. Alternatively, high-melting-point lipids or other mineral oils, such as white soft paraffin and / or liquid paraffin, can be used.

[0740] Formulations suitable for topical application to the eyes also include eye drops, wherein the active ingredient is dissolved or suspended in a suitable carrier, particularly in an aqueous solvent of the active ingredient. The active ingredient is optionally present in such formulations at a concentration of 0.5% to 20%, advantageously 0.5% to 10%, specifically about 1.5% w / w. Formulations suitable for topical application in the mouth include lozenges containing the active ingredient in a flavoring matrix (typically sucrose and gum arabic or tragacanth); soft lozenges containing the active ingredient in an inert matrix (such as gelatin and glycerin or sucrose and gum arabic); and mouthwashes containing the active ingredient in a suitable liquid carrier.

[0741] Formulations for rectal administration can be presented as suppositories containing a suitable matrix, such as cocoa butter or salicylates. Formulations suitable for nasal administration, wherein the carrier is solid, include coarse powder with a particle size, for example, in the range of 20 to 500 micrometers (including particle sizes between 20 and 500 micrometers, in increments of 5 micrometers, such as 30 micrometers, 35 micrometers, etc.), which are administered by nasal inhalation, i.e., rapid inhalation through the nasal passages from a powder container near the nose. Suitable formulations for administration as, for example, nasal sprays or drops, wherein the carrier is liquid, include aqueous or oily solutions of the active ingredient. Formulations suitable for aerosol administration can be prepared according to conventional methods and can be delivered together with other therapeutic agents.

[0742] Formulas suitable for vaginal application may be presented as vaginal suppositories, tampons, creams, gels, pastes, foams or sprays, wherein, in addition to the active ingredient, the formula contains a suitable carrier as known in the art.

[0743] Formulas suitable for parenteral administration include aqueous and non-aqueous sterile injectable solutions, which may contain antioxidants, buffers, antibacterial agents, and solutes that make the formula isotonic with the blood of the intended recipient; and aqueous and non-aqueous sterile suspensions, which may include suspending agents and thickeners. Formulas may be available in single-dose or multi-dose containers (e.g., sealed ampoules and vials) and may be stored under lyophilized (freeze-dried) conditions where a sterile liquid carrier (e.g., water for injection) needs to be added only immediately before subsequent use. Temporary injectable solutions and suspensions can be prepared from sterile powders, granules, and tablets of the types previously described.

[0744] Preferred unit dose formulations are formulations containing the active ingredient at the daily dose or unit daily sub-dose as described above, or appropriate portions thereof.

[0745] It should be understood that, in addition to the ingredients specifically mentioned above, the formulations of the present invention may include other conventional pharmaceutical agents in the art related to the type of formulation discussed, such as flavoring agents suitable for oral administration.

[0746] The benzofuran derivatives of the present invention can be used to provide controlled-release pharmaceutical formulations (“controlled-release formulations”) containing one or more of the benzofuran derivatives of the present invention as active ingredients, wherein the release of the active ingredient can be controlled and modulated to allow administration at a lower frequency or to improve the pharmacokinetic or toxicological characteristics of a given compound of the present invention. Controlled-release formulations containing discrete units of one or more benzofuran derivatives of the present invention suitable for oral administration can be prepared according to conventional methods.

[0747] Another embodiment of the invention relates to various prodrug or "prodrug" forms of the benzofuran derivatives of the invention. It may be desirable to formulate the benzofuran derivatives of the invention into chemical species that are not inherently biologically active, but which, when delivered to an animal, mammal, or human, undergo a chemical reaction catalyzed by normal bodily functions, particularly by enzymes present in the stomach or serum, releasing compounds as defined herein. Therefore, the term "prodrug" refers to these species that are converted into an active pharmaceutical ingredient in vivo.

[0748] The benzofuran derivative prodrugs of the present invention can have any form suitable for the formulation user; for example, esters are a common, non-limiting form of prodrug. However, in the present case, the prodrug may necessarily be present in a form in which the covalent bond is cleaved by the action of an enzyme present at the target locus. For example, the C-C covalent bond can be selectively cleaved at the target locus by one or more enzymes; therefore, prodrugs in forms other than readily hydrolyzable precursors, especially esters, amides, etc., can be used. The counterparts of the active pharmaceutical ingredient in the prodrug can have different structures, such as amino acid or peptide structures, alkyl chains, sugar moieties, and other structures known in the art.

[0749] For the purposes of this invention, the term "therapeutically suitable prodrug" is defined herein as "a compound modified in vivo to a therapeutically active form, whether by a single biotransformation or by multiple biotransformations, upon contact with tissues of an animal, mammal, or human to which a prodrug has been administered, without undue toxicity, irritation, or allergic response, and achieving the desired therapeutic outcome."

[0750] More specifically, as used herein, the term "prodrug" refers to an inactive or significantly reduced-activity derivative of a compound represented by a structural formula as described herein, which undergoes spontaneous or enzymatic conversion in vivo to release the pharmacologically active form of the compound. For a full review, see Rautio J. et al., ("Prodrugs: design and clinical applications," *Nature Reviews Drug Discovery*, 2008, doi:10.1038 / nrd2468).

[0751] Representative benzofuran derivatives of the present invention were synthesized according to the general synthetic methods described below and illustrated in the following embodiments. Since the embodiments are illustrative, the invention should not be construed as being limited to the specific chemical reactions and conditions described in the embodiments and examples. Various starting materials used in the embodiments are commercially available or can be prepared by methods well known to those skilled in the art. Variables are as defined herein and are within the skill of those skilled in the art.

[0752] Example

[0753] The following examples are provided for the purpose of illustrating the invention and should not in any way be construed as limiting the scope of the invention.

[0754] Representative compounds of the present invention can be synthesized according to the general synthetic methods described below and illustrated in the following embodiments. Since the embodiments are illustrative, the invention should not be construed as being limited to the specific chemical reactions and conditions described in the embodiments and examples. Various starting materials used in the embodiments are commercially available or can be prepared by methods well known to those skilled in the art. Variables are as defined herein and are within the skill of those skilled in the art.

[0755] The abbreviations used in this specification, specifically in the schemes and examples, are as follows: ABC – ammonium bicarbonate aqueous solution, ACN – acetonitrile, AcOH – acetic acid, ADDP-1,1'-(azodicarbonyl)piperidine, aq. – aqueous solution, AIBN – azobisisobutyronitrile, CAN – cerium ammonium nitrate, COMU – (1-cyano-2-ethoxy-2-oxoethyleneaminooxy)dimethylamino-morpholino-carbocation, hexafluorophosphate, DABCO – 1,4-diazabicyclo[2.2.2]octane, DAST – diethylaminosulfur trifluoride, DB U-1,8-diazabicyclo[5.4.0]undec-7-ene, DCC-N,N'-dicyclohexylcarbodiimide, DCM-dichloromethane, DEAD-diethyl azodicarboxylate, DIA-diastereomer, DIAD-diisopropyl azodicarboxylate, DEA-diethylamine, DIPEA-diisopropyl-ethylamine, DME-1,2-dimethoxyethane, DMF-N,N-dimethylformamide, DMSO-dimethyl sulfoxide, DTBAD-tert-butyl azodicarboxylate, EDCI or EDC-1-ethyl-3-(3-dimethylaminopropyl) Carbodiimide, En – enantiomer, Et2O – diethyl ether, EtOH – ethanol, EtOAc – ethyl acetate, Eq. – equivalent, FA – formic acid, FCC – rapid column chromatography, h – hours, HATU – O-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethylurea hexafluorophosphate, HPLC – high performance liquid chromatography, IPA – isopropanol, LAH – lithium aluminum hydride, LG – leaving group, MeOH – methanol, MgSO4 – magnesium sulfate, min. – minutes, Na2SO4 – sodium sulfate, NBS – N-bromosuccinimide, NMP – 1-methyl-2-pyrrolidone, Pd(PPh3)4-tetra-(triphenylphosphine)-palladium(O), Pd2(dba)3-tris(dibenzylideneacetone)dipalladium, Pet ether – petroleum ether, PPh3 – triphenylphosphine, P S-DIEA - diisopropylethylamine supported on polystyrene, PS-PPh3 - triphenylphosphine supported on polystyrene, PyBop - benzotriazol-1-yl-hexafluorophosphate oxytripyrrolidinephosphonium, PTSA - p-toluenesulfonic acid, RF - front ratio, RM - reaction mixture, RP - reversed phase, RT - room temperature, sat. - saturation, SEM - [2-(trimethylsilyl)ethoxy]methyl acetal, SFC - supercritical fluid chromatography, SPE - solid phase extraction, TBDMS - tert-butyldimethylsilyl, TBAF - tetrabutylammonium fluoride, TBAI - tetrabutylammonium iodide, TEA - triethylamine, THF - tetrahydrofuran, TFA - trifluoroacetic acid, TLC - thin layer chromatography, TPP - triphenylphosphine, IPA - isopropanol, TMS - trimethylsilyl, T3P - propylphosphonic anhydride.

[0756] The compounds of interest have structures according to general formula (I), and all other formulas and their embodiments described herein can be prepared as outlined in General Chemical Scheme 1.

[0757]

[0758] Option 1: All W, R1, R3, R4 and R5 are as described in the compounds of this invention.

[0759] At temperatures ranging from 0 to 100°C, in the presence of a polar solvent (e.g., DCM, MeOH, EtOH, etc.) containing a Lewis acid (e.g., titanium(IV) chloride, zinc(II) chloride, etc.), the p-benzoquinone of Formula 1 can be condensed with a ketone ester of Formula 2 (commercially available or synthesized by procedures known to those skilled in the art), wherein R2 is an ester protecting group (e.g., methyl, ethyl, t-Bu, etc.) to provide an intermediate of Formula 4. More detailed information can be found in the following references (Bioorg. Med. Chem. 2012, 20, 4237-4244 and FR 1319594). Alternatively, the p-benzoquinone of Formula 1 can be reacted with an enamine of Formula 3 (commercially available or synthesized by procedures known to those skilled in the art) at a temperature in the range of 0 to 100 °C in the presence of a polar solvent (e.g., DCM, MeOH, EtOH, etc.) containing a protic acid (e.g., trifluoroacetic acid, p-toluenesulfonic acid, etc.) to provide an intermediate of Formula 4. More detailed information can be found in the following reference (J. Heterocyclic Chem., 2006, 43, 873). Then, at a temperature in the range of 0 to 100 °C, with or without a chelating agent (e.g., 18-crown-6, cis-anti-cis-dicyclohexyl-18-crown-6, etc.), and in the presence of a polar solvent (e.g., acetonitrile, DMF, NMP, etc.) containing a base (e.g., DIPEA, DBU, triethylamine, Cs₂CO₃, etc.), the intermediate of Formula 4 can be converted into the desired compound of Formula 7 by nucleophilic substitution using the intermediate of Formula 5 (commercially available or synthetically synthesized). LG is the leaving group. Alternatively, at a temperature in the range of 0 to 100 °C, in the presence of a solvent (e.g., THF, toluene, etc.) containing an azodicarboxylic acid reagent (e.g., DEAD, DIAD, ADDP, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.), the intermediate of Formula 4 can also be reacted with the intermediate of Formula 6 (commercially available or synthetically synthesized) to provide the desired compound of Formula 7. The ester derivative 7 can then be converted into the desired compound of formula 8 by a standard saponification reaction. The desired compound of formula 10 can be obtained from the acid derivative of formula 8 by reacting it with the amine derivative of formula 9 (commercially available or synthesized by procedures known in the art or as shown in the examples below) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.) in a polar aprotic solvent (e.g., DCM, DMF, etc.). Alternatively, the carboxylic acid derivative of formula 8 can be converted into an acyl chloride derivative by procedures known to those skilled in the art or as shown in the examples below, and then reacted with the amine of formula 9 by procedures known to those skilled in the art or as shown in the examples below to obtain the desired compound of formula 10.

[0760] In a more specific embodiment, the compounds of the present invention can be synthesized as described in Scheme 2.

[0761]

[0762] Option 2: All W, R1, R3, R4 and R5 are as described in the compounds of this invention.

[0763] Under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.), a 5-hydroxy-benzofuran-3-carboxylic acid derivative 11 (commercially available or synthesized by procedures known in the art or as illustrated in the following examples) can be reacted with an amine derivative of Formula 9 (commercially available or synthesized by procedures known in the art or as shown in the following examples) in a polar aprotic solvent (e.g., DCM, DMF, etc.) to provide an intermediate of Formula 12. Alternatively, the compound of Formula 13 (as described in Scheme 1) can be converted into an intermediate of Formula 12 by hydrogenation reaction with a reducing agent (e.g., hydrogen, ammonium formate, cyclohexadiene, etc.) using a catalyst (more preferably Pd or Pt) in a solvent (e.g., THF, EtOH, etc.). Then, at a temperature in the range of 0 to 100 °C, with or without a chelating agent (e.g., 18-crown-6, cis-anti-cis-dicyclohexyl-18-crown-6, etc.), and in the presence of a polar solvent (e.g., acetonitrile, DMF, NMP, etc.) containing a base (e.g., DIPEA, DBU, triethylamine, Cs2CO3, etc.), the intermediate of Formula 5 (commercially available or synthesized) can be used to convert the intermediate of Formula 12 into the desired compound of Formula 10 by nucleophilic substitution, wherein LG is the leaving group. Alternatively, the compound of Formula 12 can be reacted with an intermediate of Formula 6 (commercially available or synthesized) at a temperature in the range of 0 to 100°C in the presence of a solvent (e.g., THF, toluene, etc.) containing an azodicarboxylic acid reagent (e.g., DEAD, ADDP, DIAD, tert-butylazodicarboxylate, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.) to provide the desired compound of Formula 10.

[0764] In a more specific embodiment, the compounds of the present invention can be synthesized as described in embodiment 3.

[0765]

[0766] Option 3: All W, R1, R3, R4 and R5 are as described in the compounds of this invention.

[0767] The intermediate of Formula 4 can be halogenated in a solvent (e.g., chloroform, water, etc.) with a suitable halogenating agent (e.g., bromine, N-bromosuccinimide, etc.) to provide the desired intermediate 23. The desired compound of Formula 26 can be obtained by a Ullmann-type reaction with CuCN, followed by a Mitsunobu-type reaction with the intermediate of Formula 6 (commercially available or synthetically). Alternatively, the desired compound of Formula 26 can be obtained by a Mitsunobu-type reaction with the intermediate of Formula 6 (commercially available or synthetically) followed by a Suzuki reaction. The ester derivative 26 can then be converted to the desired compound of Formula 27 by a standard saponification reaction. The desired compound of formula 28 can be obtained by reacting an acid derivative of formula 27 with an amine derivative of formula 9 (which may be commercially available or synthesized by procedures known in the art or as shown in the examples below) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.) in a polar aprotic solvent (e.g., DCM, DMF, etc.).

[0768] Example

[0769]

[0770]

[0771]

[0772] The examples described above are provided for the purpose of illustrating the invention and should in no way be construed as limiting the scope of the invention.

[0773] Part A represents the preparation of the compound, while part A represents a pharmacological example.

[0774] Part A

[0775] All starting materials not explicitly described are commercially available (details of suppliers, such as ABCR, Apollo Scientific, Combi-Blocks, Enamine, FluoroChem, MatrixScientific, Maybridge, Merck, TCI, etc., can be found at [link to supplier information]). (Found in a database) or its synthesis has been precisely described in professional literature (experimental guidelines can be found in, for example...). database or (Found in a database) or can be prepared using conventional methods known to those skilled in the art.

[0776] If necessary, the reaction is carried out under an inert atmosphere (primarily argon and N2). The equivalence of reagents and the amount of solvent used, as well as the reaction temperature and time, can be slightly varied between different reactions carried out using similar methods. Post-treatment and purification methods are adjusted according to the characteristic properties of each compound and can be slightly varied for similar methods. The yields of the prepared compounds have not been optimized.

[0777] The terms "equivalent" ("eq." or "eq" or "equiv.") refer to molar equivalents, "RT" or "rt" refers to room temperature (T, 23±7℃), "M" is the concentration in mol / L, "sol." means solution, and "conc." means concentration. The mixing ratio of solvents is usually expressed as a volume / volume ratio.

[0778] pass 1 H-NMR spectroscopy and / or mass spectrometry (MS, m / z represents [M+H]) + And / or indicates [MH] – Key analytical characterization was performed on all exemplary compounds and selected intermediates. In some cases, such as when positional isomers and / or diastereomers may be formed, additional analyses were performed in other cases, for example... 13 C NMR and NOE (nuclear overhauser effect) NMR experiments.

[0779] The analytical instruments used were, for example, a Bruker 400MHz or 500MHz instrument (Topspin software) for NMR analysis, or a Bruker Avance 300MHz and 400MHz instrument. For LC / MS analysis, instruments such as an Agilent 1290 Infinity, Mass:6150SQD (ESI / APCI) or an Agilent 1200 Series, Mass:6130SQD (ESI / APCI) (Chemistation software) were used. Analytical HPLC was performed, for example, on a Waters instrument (Empower software), an Agilent-1200-ELSD (Chemistation software), or an Agilent-1260 (OpenLAB software). Analytical SFC was performed, for example, on a PIC solution instrument (software: SFC PICLAB ONLINE), a Waters-X5 (MASSLYNX software), or a Waters-UPC2 (Empower).

[0780] Preparative HPLC was performed, for example, on a Waters 2998 (Empower software) or YMC (K-Prep software). Preparative SFC was performed, for example, on a Waters SFC-200 (Chromscope or Superchrome software), Waters SFC-80 (Superchrome), or PIC PIC-175 (S10-100 software).

[0781] If the stereochemistry is known, draw the structure of the example compound containing the stereocenter and name it with its absolute stereochemistry. In cases where the absolute stereochemistry is unknown, the compound may be a mixture of racemic diastereomers, a pure diastereomer with unknown stereochemistry, or a pure enantiomer with unknown stereochemistry. Dia 1 and Dia 2 indicate that the diastereomers have been isolated, but their stereochemistry is unknown. En 1 and En 2 indicate that both enantiomers have been isolated, but their absolute configuration is unknown. The absence of a suffix after the compound code indicates that the compound cont...

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 stands for -NR 3 R 4 ; 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 non-aromatic unsaturated; unsubstituted, monosubstituted or polysubstituted; 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 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 3-14 membered heterocycloalkyl, which is saturated or non-aromatic 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 and R Y4 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 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; 3-14 membered heterocycloalkyl, which is saturated or non-aromatic 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).

2. The compound according to claim 1, wherein T represents -O-, and U represents -(CR 5 R 5 ') n -.

3. The compound according to any one of claims 1 or 2, 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.

4. A compound according to any one of claims 1 to 3, 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 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 is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; 3-14 membered heterocycloalkyl, which is saturated or non-aromatic 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.

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 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 cycloalkyl, 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 heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl.

6. A compound according to any one of claims 1 to 5, wherein R 3 indicates -H; and 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 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; 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 3-14 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; 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 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 ... 1,4-oxazepane, pyrrolidine, 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, oxetanyl, pyrimidinyl, -C 1-6 -alkylene-phenyl; unsubstituted-phenyl; 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.

7. A compound according to any one of claims 1 to 6, wherein W represents 3-14 membered cycloalkyl, which is saturated or non-aromatic unsaturated, unsubstituted, mono-substituted or poly-substituted 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; 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 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 non-aromatic unsaturated, unsubstituted, monosubstituted or polysubstituted; wherein the 3-14 membered cycloalkyl is optionally linked via -C1-C6-alkylene- or -C1-C6-heteroalkylene-, It is in each case 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 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; -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; -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; -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 -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.

11. A compound according to any one of claims 1 to 10, selected from the group consisting of: Cpd 001-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 002-(2S)-2-({5-[(2,2-difluorocyclopropyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxypropanamide; Cpd 003-(2S)-2-[(5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-yl)formamido]-3-hydroxypropanamide; Cpd 004-(2S)-2-{[2-cyclopropyl-5-(cyclopropylmethoxy)-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 005-(2S)-2-{[5-(2-cyclopropylethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 006-(2S)-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 007-(2S)-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}propanamide; Cpd 008-(2S)-2-{[5-(cyclopropylmethoxy)-2-(difluoromethyl)-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 009-(2R)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 010-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}propanamide; Cpd 011-(2S,3R)-2-[(5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-yl)formamido]-3-hydroxybutanamide; Cpd 012-(2S,3R)-2-{[5-(2-cyclopropylethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxybutanamide; Cpd 013-2-({5-[(2,2-difluorocyclopentyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxypropanamide; Cpd 014-2-[(5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-yl)formamido]-3-hydroxy-2-methylpropanamide; Cpd 015-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-2-methylpropanamide; Cpd 016-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-2-methylpropanamide; Cpd 017-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropanamide; Cpd 018-5-(cyclobutylmethoxy)-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-1-benzofuran-3-carboxamide; Cpd 019-5-(cyclobutylmethoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methyl-1-benzofuran-3-carboxamide; Cpd 020-5-(cyclohexylmethoxy)-2-methyl-N-(1-methylpiperidin-4-yl)-1-benzofuran-3-carboxamide; Cpd 021-5-(cyclopropylmethoxy)-2-methyl-N-(1-methylpiperidin-4-yl)-1-benzofuran-3-carboxamide; Cpd 022-5-(Cyclopropylmethoxy)-2-methyl-N-(oxan-4-yl)-1-benzofuran-3-carboxamide; Cpd 023-5-(Cyclopropylmethoxy)-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-1-benzofuran-3-carboxamide; Cpd 024-5-(cyclopropylmethoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methyl-1-benzofuran-3-carboxamide; Cpd 025-5-(Cyclopropylmethoxy)-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-1-benzofuran-3-carboxamide; Cpd 026-5-(Cyclopropylmethoxy)-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzofuran-3-carboxamide; Cpd 027-5-(cyclopropylmethoxy)-N-[3-(hydroxymethyl)-2-oxopiperidin-3-yl]-2-methyl-1-benzofuran-3-carboxamide; Cpd 028-5-(Cyclopropylmethoxy)-N-[3-(hydroxymethyl)-2-oxopyrrolidin-3-yl]-2-methyl-1-benzofuran-3-carboxamide; Cpd 029-5-(Cyclopropylmethoxy)-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-1-benzofuran-3-carboxamide; Cpd 030-5-(Cyclopropylmethoxy)-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzofuran-3-carboxamide; Cpd 031-5-[(2,2-difluorocyclopropyl)methoxy]-N-(3,3-difluoropiperidin-4-yl)-2-methyl-1-benzofuran-3-carboxamide; Cpd 032-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-[(1-methylcyclopropyl)methoxy]-1-benzofuran-3-carboxamide; Cpd 033-N-(3,3-difluoropiperidin-4-yl)-5-[(2,2-dimethylcyclopropyl)methoxy]-2-methyl-1-benzofuran-3-carboxamide; Cpd 034-N-(3-carbamoyloxetane-3-yl)-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide; Cpd 035-N-(3-carbamoyloxolan-3-yl)-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide; Cpd 036-N-(3-carbamoyloxolan-3-yl)-5-{[1-(difluoromethyl)cyclopropyl]methoxy}-2-methyl-1-benzofuran-3-carboxamide; Cpd 037-N-(4-carbamoyloxan-4-yl)-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide; Cpd 038-(2S)-2-{[5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 039-(2S)-2-{[5-(2,2-dimethylpropoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxypropanamide; Cpd 040-(2S,3R)-2-{[5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxybutanamide; Cpd 041-2-{[5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropanamide; Cpd 042-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(2-methylpropoxy)-1-benzofuran-3-carboxamide; Cpd 043-N-(3,3-difluoropiperidin-4-yl)-5-(2,2-dimethylpropoxy)-2-methyl-1-benzofuran-3-carboxamide; Cpd 044-N-(3-carbamoyloxolan-3-yl)-5-(2,2-difluoroethoxy)-2-methyl-1-benzofuran-3-carboxamide; Cpd 045-2-{[5-(cyclopropylmethoxy)-6-fluoro-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropanamide; Cpd 046-5-(Cyclopropylmethoxy)-N-(4,4-difluoro-1-hydroxy-2-methylbutan-2-yl)-2-methyl-1-benzofuran-3-carboxamide; Cpd 047-3-hydroxy-2-methyl-2-{[2-methyl-5-(2,2,2-trifluoroethoxy)-1-benzofuran-3-yl]formamido}acrylamide; Cpd 048-3-hydroxy-2-methyl-2-[(2-methyl-5-{[1-(trifluoromethyl)cyclopropyl]methoxy}-1-benzofuran-3-yl)formamido]acrylamide; Cpd 049-2-({5-[(2,2-dimethylcyclopropyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxy-2-methylpropanamide; Cpd 050-cis-2-{[5-({bicyclo[3.1.0]hex-3-yl}methoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropanamide Cpd 051-trans-2-{[5-({bicyclo[3.1.0]hex-3-yl}methoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropanamide; Cpd 052-3-hydroxy-2-methyl-2-{[2-methyl-5-({3-methylbicyclo[1.1.1]pentan-1-yl}methoxy)-1-benzofuran-3-yl]formamido}acrylamide; Cpd 053-2-{[5-(cyclobutylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropanamide; Cpd 054-2-({5-[(3,3-difluorocyclobutyl)methoxy]-2-methyl-1-benzofuran-3-yl}formamido)-3-hydroxy-2-methylpropanamide; Cpd 055-5-(cyclopropylmethoxy)-2-methyl-N-(2-oxopiperidin-3-yl)-1-benzofuran-3-carboxamide; Cpd 056-N-[(2)-3-amino-4,4,4-trifluoro-1-hydroxybutan-2-yl]-5-(cyclopropylmethoxy)-2-methyl-1-benzofuran-3-carboxamide; Cpd 057-5-[(2,2-difluorocyclopropyl)methoxy]-2-methyl-N-(4,4,4-trifluoro-1-hydroxybutan-2-yl)-1-benzofuran-3-carboxamide; Cpd 058-cis-3-hydroxy-2-methyl-2-({2-methyl-5-[(3-methylcyclobutyl)methoxy]-1-benzofuran-3-yl}formamido)acrylamide; Cpd 059-trans-3-hydroxy-2-methyl-2-({2-methyl-5-[(3-methylcyclobutyl)methoxy]-1-benzofuran-3-yl}formamido)acrylamide; Cpd 060-N-(1-hydroxy-3-methoxy-2-methylpropan-2-yl)-2-methyl-5-{[1-(trifluoromethyl)cyclopropyl]methoxy}-1-benzofuran-3-carboxamide; Cpd 061-2-methyl-N-(3-methyl-2-oxopiperidin-3-yl)-5-{[1-(trifluoromethyl)cyclopropyl]methoxy}-1-benzofuran-3-carboxamide; Cpd 062-2-{[5-(cyclopentylmethoxy)-2-methyl-1-benzofuran-3-yl]formamido}-3-hydroxy-2-methylpropanamide; 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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