New derivatives for treating TRPM3-mediated disorders

Abstract

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

Description

[Technical field]

[0001] The present invention relates to compounds useful for the prevention or treatment of TRPM3-mediated disorders, more particularly disorders selected from pain, epilepsy and inflammatory hypersensitivity. The present invention also relates to a method for the prevention or treatment of said TRPM3-mediated disorders. [Background technology]

[0002] The TRP superfamily consists of proteins with six transmembrane domains (6TM) that assemble as homo- or heterotetramers to form cation-permeable ion channels. The name TRP comes from the Drosophila trp (transient receptor potential) mutants that are characterized by a transient receptor potential in fly photoreceptors in response to sustained light. In the past 15 years, trp-related channels have been identified in yeast, parasites, 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 expressed in virtually all mammalian organs and cell types, and in recent years, great progress has been made in understanding their physiological roles. The customized selectivity of certain TRP channels is due to their ability to selectively bind Ca. 2+ , Mg 2+ , and trace metal ions. Moreover, the sensitivity of TRP channels to a wide range of chemical and physical stimuli allows them to function as dedicated biological sensors involved in processes from vision to taste to touch. Specifically, some members of the TRP superfamily show extremely high sensitivity to temperature. These so-called thermo-TRPs are highly expressed in sensory neurons and / or skin keratinocytes and function as the primary thermosensors for the detection of innocuous and noxious (painful) temperatures.

[0004] It is becoming increasingly clear that TRP channel dysfunction is directly involved in the pathogenesis of various genetic and acquired diseases. In fact, both loss-of-function and gain-of-function mutations in TRP channel genes have been identified as the direct cause of genetic diseases, including brachiolemia, hypomagnesemia with secondary hypocalcemia, polycystic kidney disease, mucolipidosis type IV, and familial focal segmental glomerulosclerosis. Furthermore, TRP channel function / dysfunction is directly related to a wide range of pathological conditions, including chronic pain, hypertension, cancer, epilepsy, and neurodegenerative disorders.

[0005] TRPM3 (Transient Receptor Potential Melastatin 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). The neurosteroid pregnenolone sulfate caused pain in wild-type mice but not in knockout TRPM3 mice. It was also recently shown that CFA-induced inflammation and inflammatory pain were eliminated in TRPM3 knockout mice. Thus, TRPM3 antagonists could be used as analgesics to counter pain, such as inflammatory pain (Vriens J. et al. Neuron, May 2011). TRPM3 is also expressed in several other tissues, including the brain; reports have shown that two mutations in TRPM3 are associated with developmental and epileptic encephalopathies (Zhao, S., et al. Channels (Austin). 2021).

[0006] Although several TRPM3 antagonists are known, none of them refer to the compounds of the present invention (Straub I et al. Mol Pharmacol, November 2013). For example, liquiritigenin, a putative TRPM3 blocker, has been described to reduce mechanical and cold hyperalgesia in a rat pain model (Chen L et al. Scientific reports, July 2014). There remains a great medical need for new, alternative, and / or better treatments for the prevention or treatment of TRPM3-mediated disorders such as pain and epilepsy, more specifically for inflammatory pain such as epileptic encephalopathy or pain such as epilepsy. Good efficacy against certain types of pain, low or no side effects (such as no addiction potential and no toxicity as with opiates) and / or good or better pharmacokinetic or -dynamic properties are highly needed.

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

[0008] A first aspect of the present invention relates to a compound of formula (I), its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs thereof, [ka] During the ceremony, R 1 -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) 2 R W , -C(=O)R W , -C(=O)ORW or -C(=O)NR W R X represents Q is -OR 2 or -NR 3 R 4 represents R 2 But -R Y5 represents R 3 is -OH or -R Y1 represents R 4 But -R Y2 or -S(=O) 2 R Y3 represents Or, R 3 and R 4 together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 4-, 5-, 6-, 7-, or 8-membered heterocycle containing 1 to 3 heteroatoms selected from N, O, and S; T represents -O- and U represents -(CR 5 R 5 ') n - or T represents -(CR 5 R 5 ') n -, U represents -O-, n is an integer selected from 1, 2, 3, 4, or 5; R 5 and R 5 ', but independently of each other, -R Y4 represents R 6 , R 7 , and R 8 are, independently of each other, -F, -Cl, -Br, -I, -CN, -NO 2 ,-SCIENCE FICTION 5 , -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) 2 RW , -C(=O)R W , -C(=O)OR W or -C(=O)NR W R X represents W, saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl; unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or In each case, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, During the ceremony, R W and R X but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl; A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered heterocycloalkyl, R Y1 , R Y2 , R Y3 , R Y4 , and R Y5 but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl; A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, "Mono- or polysubstituted" means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-NH 2 , -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 -NH 2 , -C 1-6 -Alkylene-OS(=O) 2 -NH 2 , -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 , -NH 2 , -NO, -NO 2 , -C 1-6 -Alkylene-NH 2 , -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)-NH 2 , -C 1-6 -Alkylene-NH-C(=O)-NH 2 , -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(C1-6 -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)-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-NH 2 , -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) 2 OH, -C 1-6 -Alkylene-NH-S(=O) 2 OH, -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 -NH 2, -C 1-6 -Alkylene-NH-S(=O) 2 -NH 2 , -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) 2 N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-S(=O) 2 N(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 -NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -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(C1-6 -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, -SF 5 , -SCF 3 , -SCF 2 H, -SCFH 2 , -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 -NH 2 , -C 1-6 -Alkylene-S(=O) 2 -NH 2 , -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(C1-6 -alkyl) 2 , 3-14 membered cycloalkyl, -C 1-6 -Alkylene-(3- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-14 membered heteroaryl, -C 1-6 -Alkylene-(5-14 membered heteroaryl), -O-(3-14 membered cycloalkyl), -O-(3-14 membered heterocycloalkyl), -O-phenyl, -O-(5-14 membered heteroaryl), -C(=O)-(3-14 membered cycloalkyl), -C(=O)-(3-14 membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5-14 membered heteroaryl), -S(=O) 2 -(3 to 14 membered cycloalkyl), -S(=O) 2 -(3-14 membered heterocycloalkyl), -S(=O) 2 -phenyl, or -S(=O) 2 -(5-14 membered heteroaryl), or the compound is ethyl 5-methoxy-2-methyl-1-benzothiophene-3-carboxylate, its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs thereof of formula (I). In particular, the present invention relates to compounds of formula (I), their stereoisomers, physiologically acceptable salts, solvates and / or polymorphs thereof, [ka] During the ceremony, R 1 -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)2 R W , -C(=O)R W , -C(=O)OR W or -C(=O)NR W R X represents Q is -OR 2 or -NR 3 R 4 represents R 2 But -R Y5 represents R 3 is -OH or -R Y1 represents R 4 But -R Y2 or -S(=O) 2 R Y3 represents Or, R 3 and R 4 together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 4-, 5-, 6-, 7-, or 8-membered heterocycle containing 1 to 3 heteroatoms selected from N, O, and S; T represents -O- and U represents -(CR 5 R 5 ') n - or T represents -(CR 5 R 5 ') n -, U represents -O-, n is an integer selected from 1, 2, 3, 4, or 5; R 5 and R 5 ', but independently of each other, -R Y4 represents R 6 , R 7 , and R 8 are, independently of each other, -F, -Cl, -Br, -I, -CN, -NO 2 ,-SCIENCE FICTION 5 , -R W , -OR W , -OC(=O)R W , -NR W R X , -NR W C(=O)R X , -SRW , -S(=O)R W , -S(=O) 2 R W , -C(=O)R W , -C(=O)OR W or -C(=O)NR W R X represents W, saturated or unsaturated 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or In each case, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, During the ceremony, R W and R X but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, or A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered heterocycloalkyl, R Y1 , R Y2 , R Y3 , R Y4 , and R Y5 but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, "Mono- or polysubstituted" means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -C 1-6 -Alkylene-C(=O)-NH 2 , -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 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-NH 2 , -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 -NH 2 , -C 1-6 -Alkylene-OS(=O) 2 -NH 2 , -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 , -NH 2 , -NO, -NO 2 , -C 1-6 -Alkylene-NH 2 , -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)-NH 2 , -C 1-6 -Alkylene-NH-C(=O)-NH 2 , -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(C1-6 -alkyl)-C(=O)-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-NH 2 , -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) 2 OH, -C 1-6 -Alkylene-NH-S(=O) 2 OH, -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 -NH 2 , -C 1-6 -Alkylene-NH-S(=O) 2 -NH 2 , -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) 2 N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-S(=O) 2 N(C1-6 -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 -NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -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, -SF 5 , -SCF 3 , -SCF 2 H, -SCFH 2 , -SC1-6 -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 -NH 2 , -C 1-6 -Alkylene-S(=O) 2 -NH 2 , -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- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-14 membered heteroaryl, -C 1-6-Alkylene-(5-14 membered heteroaryl), -O-(3-14 membered cycloalkyl), -O-(3-14 membered heterocycloalkyl), -O-phenyl, -O-(5-14 membered heteroaryl), -C(=O)-(3-14 membered cycloalkyl), -C(=O)-(3-14 membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5-14 membered heteroaryl), -S(=O) 2 -(3 to 14 membered cycloalkyl), -S(=O) 2 -(3-14 membered heterocycloalkyl), -S(=O) 2 -phenyl, or -S(=O) 2 -(5-14 membered heteroaryl), The compound is Provided is a compound of formula (I), its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs thereof, which is not 5-benzyloxybenzo[b]thiophene-3-carboxylic acid.

[0009] A second aspect of the invention encompasses a pharmaceutical composition comprising a compound of formula (I) according to the first aspect.

[0010] According to a third aspect, the present invention also provides a compound of formula (I) according to the first aspect or a pharmaceutical composition according to the second aspect for use as a medicament.

[0011] According to a fourth aspect, the present invention also encompasses a compound of formula (I) as defined in the first aspect or a pharmaceutical composition as defined in the second aspect for use in the prevention and / or treatment of a TRPM3 mediated disorder, in particular for use in the prevention and / or treatment of and / or against pain, epilepsy and / or inflammatory hypersensitivity, in particular for use in the prevention and / or treatment of and / or against pain, epilepsy and / or inflammatory hypersensitivity, in particular for use in the prevention and / or treatment of and / or against pain, epilepsy and / or inflammatory hypersensitivity.

[0012] The present invention also provides a method for preventing or treating a TRPM3-mediated disorder by administering a compound of formula (I) according to the first aspect to a subject in need thereof. More specifically, the present invention relates to such a method for preventing and / or treating pain, epilepsy and / or inflammatory hypersensitivity and / or combating pain, epilepsy and / or inflammatory hypersensitivity. More specifically, the present invention relates to such a method for preventing and / or treating pain, epileptic encephalopathy and / or inflammatory hypersensitivity and / or combating pain, epileptic encephalopathy and / or inflammatory hypersensitivity.

[0013] The present invention further provides a process for preparing a compound of formula (I) according to the first aspect, comprising the steps of: - converting benzothiophene to a 5-hydroxybenzothiophene-3-carboxylate ester derivative; - substitution of the previously obtained 5-hydroxybenzothiophene-3-carboxylate ester derivative with a suitable derivative or alcohol derivative bearing a leaving group under alkylation or Mitsunobu conditions to obtain a 5-O-substituted benzothiophene-3-carboxylate ester derivative, - converting the previously obtained 5-O-substituted benzothiophene-3-carboxylate ester derivative into a carboxylic acid to obtain a 5-O-substituted benzothiophene-3-carboxylic acid derivative; and - coupling the previously obtained 5-O-substituted benzothiophene-3-carboxylic acid derivative with a suitable amine to give the desired derivative of the invention. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0014] Before the invention is described, it is to be understood that this invention is not limited to the particular processes, methods, and compounds described, as such processes, methods, and compounds may, of course, vary. It is also to be understood that the terms used herein are not intended to be limiting, since the scope of the invention will be limited only by the appended claims.

[0015] When describing the compounds and processes of this invention, the terms used should be construed in accordance with the following definitions, unless the context dictates otherwise.

[0016] As used in this specification and the appended claims, the singular forms "a," "an," and "the" include both singular and plural referents unless the context clearly dictates otherwise. For example, "a compound" means one compound or more than one compound.

[0017] As used herein, the terms "comprising," "comprises," and "comprised of" are synonymous with "including," "includes," or "containing," "contains," and are inclusive or open-ended and do not exclude additional, unrecited components, elements, or method steps. The terms "comprising," "comprises," and "comprised of" include the term "consisting of."

[0018] As used herein, the term "about," when referring to a measurable value such as a parameter, amount, length of time, and the like, is meant to encompass variations of the specified value and therefrom of no more than + / - 10%, preferably no more than + / - 5%, more preferably no more than + / - 1%, and even more preferably no more than + / - 0.1%, provided that such variations are appropriate in the disclosed invention. It is to be understood that the value to which the modifier "about" refers is itself specifically and preferably disclosed.

[0019] As used herein, the term "and / or," when used in a list of two or more items, means that any one of the listed items may be taken alone, or any combination of two or more of the listed items may be taken. For example, if a list is described as including groups A, B, and / or C, the list may include A only, B only, C only, 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.

[0020] The recitation of numerical ranges by endpoints includes all integers and, where appropriate, fractions subsumed within that range (e.g., 1 to 5 can include 1, 2, 3, 4, for example, when referring to several elements, and can also include 1.5, 2, 2.75, and 3.80, for example, when referring to measurements). The recitation of endpoints also includes the endpoint values ​​themselves (e.g., 1.0 to 5.0 includes both 1.0 and 5.0). Any numerical ranges described herein are intended to include all sub-ranges subsumed therein.

[0021] References throughout this specification to "one embodiment" or "an embodiment" mean that a particular feature, structure, or characteristic described in connection with that embodiment is included in at least one embodiment of the invention. Thus, the phrases "in one embodiment" or "in an embodiment" appearing in various places in this specification do not necessarily all refer to the same embodiment, although they may. Furthermore, particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments, as would be apparent to one of ordinary skill in the art from this disclosure. Moreover, some embodiments described herein include some features but not other features included in other embodiments, and combinations of features of different embodiments are meant to be within the scope of the invention and form different embodiments, as would be understood by one of ordinary skill in the art. For example, in the following claims, any of the claimed embodiments may be used in any combination.

[0022] Similarly, in describing exemplary embodiments of the invention, it will be understood that various features of the invention may be grouped together in a single embodiment, figure, or description thereof in order to streamline the disclosure and to aid in understanding one or more of the various inventive aspects.

[0023] Unless otherwise defined, all terms used in disclosing the present invention, including technical and scientific terms, have the meanings commonly understood by those of ordinary skill in the art to which the present invention belongs. As a further guide, definitions of terms used in the description are included to better understand the teachings of the present invention.

[0024] When describing the present invention, the terms used should be construed in accordance with the following definitions, unless the context dictates otherwise.

[0025] The above terms and other terms used herein are well understood by those of ordinary skill in the art.

[0026] Whenever the term "substituted" is used herein, it is meant to indicate that one or more hydrogen atoms on the atom designated with the phrase "substituted" are replaced with a selection from a designated group, provided that the normal valence of the designated atom is not exceeded, and that the replacement results in a chemically stable compound, i.e., a compound that is robust enough to survive isolation from a reaction mixture.

[0027] In each of the following definitions, the number of carbon atoms represents the maximum number of carbon atoms that are generally optimally present in a substituent or linker. If otherwise indicated in this application, it is understood that the number of carbon atoms represents the optimal maximum number of carbon atoms for that particular substituent or linker.

[0028] The term "leaving group" or "LG" as used herein means a chemical group that is susceptible to displacement by a nucleophile or to cleavage or hydrolysis under basic or acidic conditions. In certain embodiments, the leaving group is selected from a halogen atom (e.g., Cl, Br, I) or a sulfonate (e.g., mesylate, tosylate, triflate).

[0029] The term "protecting group" refers to a moiety of a compound that masks or modifies the properties of a functional group or the overall compound. The chemical substructure of protecting groups varies widely. One function of a protecting group is to serve as an intermediate in the synthesis of a parent drug substance. Chemical protecting groups and strategies for protection / deprotection are well known in the art. See "Protective Groups in Organic Chemistry", Theodora W. Greene (John Wiley & Sons, Inc., New York, 1991). Protecting groups are often utilized to mask the reactivity of certain functional groups to aid in the efficiency of a desired chemical reaction, e.g., forming and breaking chemical bonds in an orderly and planned manner. Protection of a functional group of a compound alters other physical properties besides the reactivity of the protected functional group, such as polarity, lipophilicity (hydrophobicity), and other properties that can be measured by common analytical tools. Chemically protected intermediates may themselves be biologically active or inactive.

[0030] Protected compounds may also exhibit altered properties, and in some cases, optimized properties in vitro and in vivo (passing cell membranes and resistance to enzymatic degradation or capture). In this role, protected compounds with the intended therapeutic effect may be referred to as prodrugs. Another function of the protecting group is to convert the parent drug into a prodrug, whereby the parent drug is released upon conversion of the prodrug in vivo. Since the active prodrug may be absorbed more effectively than the parent drug, the prodrug may have greater potency in vivo than the parent drug. Protecting groups are removed either in vitro in the case of chemical intermediates, or in vivo in the case of prodrugs. For chemical intermediates, it is not particularly important that the resulting product (e.g., alcohol) after deprotection is physiologically acceptable, but it is generally more desirable if the product is pharmacologically harmless.

[0031] The term "heteroatom(s)" as used herein means atoms selected from nitrogen, oxygen, and sulfur, including sulfoxide and sulfone, which may be quaternized.

[0032] The term "saturated or unsaturated alkyl" as used herein includes saturated alkyl and unsaturated alkyl such as alkenyl, alkynyl, etc. Suitable examples of saturated or unsaturated alkyl include, but are not limited to, methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl (i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl, and 3,3-dimethyl-2-butyl. "C 1-6"Alkyl" includes all straight or branched chain alkyl groups having 1 to 6 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl, butyl and its isomers (e.g., n-butyl, i-butyl, and t-butyl), pentyl and its isomers, and hexyl and its isomers. For example, "C 1-5 "Alkyl" is inclusive of all straight or branched chain alkyl groups having from 1 to 5 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl, butyl and its isomers (e.g., n-butyl, i-butyl, and t-butyl), pentyl and its isomers, ethylene or vinyl (-CH=CH 2 ), allyl (-CH 2 CH=CH 2 ), 5-hexenyl (-CH 2 CH 2 CH 2 CH 2 CH=CH 2 ), 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.

[0033] The term "alkyl" as used herein means a normal, secondary or tertiary, straight or branched chain hydrocarbon having no sites of unsaturation. Examples are methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl (i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl, and 3,3-dimethyl-2-butyl. 1-6"Alkyl" includes all straight or branched chain alkyl groups having 1 to 6 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl, butyl and its isomers (e.g., n-butyl, i-butyl, and t-butyl), pentyl and its isomers, and hexyl and its isomers. For example, "C 1-5 "Alkyl" includes all straight or branched chain alkyl groups having from 1 to 5 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl, butyl and its isomers (e.g., n-butyl, i-butyl, and t-butyl), pentyl and its isomers. For example, "C 1-4 "Alkyl" includes all straight or branched chain alkyl groups having 1 to 4 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl, butyl and their isomers (e.g., n-butyl, i-butyl, and t-butyl). For example, "C 1-3 "Alkyl" includes all straight or branched chain alkyl groups having 1 to 3 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl. "Substituted C 1-6 "Alkyl" refers to a C alkyl group substituted with one or more substituents (e.g., 1 to 3 substituents, e.g., 1, 2, or 3 substituents) at any available point of attachment. 1-6 Refers to an alkyl group.

[0034] As used herein, the term "alkenyl" refers to a normal, secondary or tertiary, straight or branched chain hydrocarbon having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., a carbon-carbon, sp2 double bond. Examples include ethylene or vinyl (-CH=CH 2 ), allyl (-CH 2 CH=CH 2 ), and 5-hexenyl (-CH 2 CH 2 CH 2 CH 2 CH=CH 2) The double bond may be in the cis or trans configuration. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms the named group may contain. For example, "C 2-6 The term "alkenyl" refers to an unsaturated hydrocarbyl group that contains one or more carbon-carbon double bonds and that contains from 2 to 6 carbon atoms, and may be straight or branched. For example, C 2-4 Alkenyl includes all straight or branched alkenyl groups having 2 to 4 carbon atoms. 2-6 Examples of alkenyl groups are ethenyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl, and the like.

[0035] The term "alkynyl" as used herein means a normal, secondary, tertiary, straight or branched chain hydrocarbon having at least one site of unsaturation (usually one to three, preferably one), i.e., a carbon-carbon, sp triple bond. Examples include ethynyl (-C≡CH) and 1-propynyl (propargyl, -CH 2 C≡CH). When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms the named group may contain. For example, "C 2-6 The term "alkynyl" refers to an unsaturated hydrocarbyl group that contains one or more carbon-carbon triple bonds and that contains from 2 to 6 carbon atoms, and may be straight or branched. For example, C 2-4 Alkynyl includes all straight or branched chain alkynyl groups having 2 to 4 carbon atoms. 2-6 Non-limiting examples of alkynyl groups include ethynyl, 2-propynyl, 2-butynyl, 3-butynyl, 2-pentynyl and chain isomers thereof, 2-hexynyl and chain isomers thereof, and the like.

[0036] As used herein, the term "saturated or unsaturated alkylene" encompasses saturated alkylenes as well as unsaturated alkylenes such as alkenylene, alkynylene, etc. As used herein, the term "alkylene" refers to a saturated, straight-chain, or branched-chain hydrocarbon radical having two monovalent radical centers derived by the removal of two hydrogen atoms from the same or two different carbon atoms of a parent alkane. Exemplary alkylene radicals include methylene (-CH 2 -), ethylene (-CH 2 -CH 2 -), methylmethylene (-CH(CH 3 )-), 1-methyl-ethylene (-CH(CH 3 )-CH 2 -), n-propylene (-CH 2 -CH 2 -CH 2 -), 2-methylpropylene (-CH 2 -CH(CH 3 )-CH 2 -), 3-methylpropylene (-CH 2 -CH 2 -CH(CH 3 )-), n-butylene (-CH 2 -CH 2 -CH 2 -CH 2 -), 2-methylbutylene (-CH 2 -CH(CH 3 )-CH 2 -CH 2 -), 4-methylbutylene (-CH 2 -CH 2 -CH 2 -CH(CH 3 )-), pentylene and its chain isomers, and hexylene and its chain isomers.

[0037] The term "alkenylene" as used herein means a straight or branched chain hydrocarbon radical having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., a carbon-carbon, sp2 double bond, and having two monovalent radical centers obtained by the removal of two hydrogen atoms from the same or two different carbon atoms of a parent alkene. 2-6 "Alkenylene" by itself or as part of another substituent is a C alkyl group that is divalent, i.e., has two single bonds for attachment to two other groups. 2-6 Refers to an alkenyl group.

[0038] The term "alkynylene" as used herein means a straight or branched chain hydrocarbon radical having at least one site of unsaturation (usually one to three, preferably one), i.e., a carbon-carbon, sp triple bond, and having two monovalent radical centers obtained by removal of two hydrogen atoms from the same or two different carbon atoms of a parent alkene. 2-6 The term "alkynylene" by itself or as part of another substituent refers to a C alkyl group that is divalent, i.e., has two single bonds for attachment to two other groups. 2-6 Refers to an alkynyl group.

[0039] The term "alkenyl" as a group or part of a group refers to an unsaturated hydrocarbyl group that contains one or more carbon-carbon double bonds, and may be straight or branched. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms that the named group may contain. For example, "C 2-6 The term "alkenyl" refers to an unsaturated hydrocarbyl group that contains one or more carbon-carbon double bonds and that contains from 2 to 6 carbon atoms, and may be straight or branched. For example, C 2-4 Alkenyl includes all straight or branched alkenyl groups having 2 to 4 carbon atoms. 2-6 Examples of alkenyl groups are ethenyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl, and the like.

[0040] The term "alkynyl" by itself or as part of another substituent refers to an unsaturated hydrocarbyl group that contains one or more carbon-carbon triple bonds, and may be straight or branched. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms that the named group may contain. For example, "C 2-6 The term "alkynyl" refers to an unsaturated hydrocarbyl group that contains one or more carbon-carbon triple bonds and that contains from 2 to 6 carbon atoms, and may be straight or branched. For example, C 2-4 Alkynyl includes all straight or branched chain alkynyl groups having 2 to 4 carbon atoms. 2-6 Non-limiting examples of alkynyl groups include ethynyl, 2-propynyl, 2-butynyl, 3-butynyl, 2-pentynyl and chain isomers thereof, 2-hexynyl and chain isomers thereof, and the like.

[0041] "HaloC" as a group or part of a group 1-6 The term "alkyl" refers to a C alkyl group having the meaning defined above, in which one, two or three hydrogen atoms are each replaced by a halogen as defined herein. 1-6 Refers to an alkyl group. Such haloC 1-6 Non-limiting examples of alkyl groups include chloromethyl, 1-bromoethyl, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1,1-trifluoroethyl, and the like.

[0042] As used herein, the term "saturated or unsaturated heteroalkyl" encompasses saturated heteroalkyls as well as unsaturated heteroalkyls such as heteroalkenyls and heteroalkynyls. As used herein, the term "heteroalkyl" refers to straight or branched chain alkyls in which one or more carbon atoms (usually one, two or three) are replaced by heteroatoms, i.e., oxygen, nitrogen or sulfur atoms, provided that the chain cannot contain two adjacent O atoms or two adjacent S atoms. This means that one or more of the alkyls may have -CH 3 Ga-NH 2and / or one or more of the alkyl groups may be replaced by -CH 2 It means that - can be replaced by -NH-, -O-, or -S-. The S atom in the chain can be optionally oxidized with one or two oxygen atoms to give sulfoxides and sulfones, respectively. Furthermore, the heteroalkyl groups in the compounds of the present invention can contain oxo or thio groups at any carbon or heteroatom that results in a stable compound. Exemplary heteroalkyl groups include, but are not limited to, alcohols, alkyl ethers (e.g., -methoxy, -ethoxy, -butoxy, etc.), primary, secondary, and tertiary alkyl amines, amides, ketones, esters, alkyl sulfides, and alkyl sulfones. The term "heteroalkenyl" refers to straight or branched alkenyl, in which one or more carbon atoms (usually one, two, or three) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain cannot contain two adjacent O atoms or two adjacent S atoms. Thus, the term heteroalkenyl includes imines, -O-alkenyl, -NH-alkenyl, -N(alkenyl) 2 , -N(alkyl)(alkenyl), and -S-alkenyl. As used herein, the term "heteroalkynyl" means a straight or branched chain alkynyl in which one or more carbon atoms (usually one, two, or three) are replaced by an oxygen, nitrogen, or sulfur atom, provided that the chain cannot contain two adjacent O atoms or two adjacent S atoms. Thus, the term heteroalkynyl includes -cyano, -O-alkynyl, -NH-alkynyl, -N(alkynyl), -Cyano, ... 2 , -N(alkyl)(alkynyl), -N(alkenyl)(alkynyl), and -S-alkynyl.

[0043] The term "saturated or unsaturated heteroalkylene" as used herein includes saturated heteroalkylene as well as unsaturated heteroalkylene such as heteroalkenylene and heteroalkynylene. The term "heteroalkylene" as used herein means straight or branched chain alkylene, in which one or more carbon atoms (usually one, two or three) are replaced by heteroatoms, i.e., oxygen, nitrogen or sulfur atoms, with the proviso that the chain may not contain two adjacent O atoms or two adjacent S atoms. The term "heteroalkenylene" as used herein means straight or branched chain alkenylene, in which one or more carbon atoms (usually one, two or three) are replaced by oxygen, nitrogen or sulfur atoms, with the proviso that the chain may not contain two adjacent O atoms or two adjacent S atoms. The term "heteroalkynylene," as used herein, means a straight- or branched-chain alkynylene in which one or more carbon atoms (usually 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain cannot contain two adjacent O atoms or two adjacent S atoms.

[0044] The term "saturated or unsaturated cycloalkyl" as used herein includes saturated cycloalkyl and unsaturated cycloalkyl such as cycloalkenyl, cycloalkynyl. In particular, the term "saturated or unsaturated cycloalkyl" as used herein encompasses saturated cycloalkyl and unsaturated non-aromatic cycloalkyl such as cycloalkenyl and cycloalkynyl. In particular, the terms "saturated or unsaturated cycloalkyl" and "saturated or non-aromatic unsaturated cycloalkyl" are synonymous. The term "saturated or unsaturated cycloalkyl" also includes all saturated and unsaturated hydrocarbon groups containing one or more rings, including monocyclic or bicyclic groups. The additional rings of polycyclic cycloalkyls may be fused, bridged, and / or joined via one or more spiro atoms. Suitable examples of saturated or unsaturated cycloalkyl include cyclopropyl, cyclopropanyl, cyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenylcycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, 1,3-cyclohexadienyl, 1,4-cyclohexadienyl, 1,5-cyclooctadienyl, bicyclo[2.2.1]heptan-2-yl, (1S,4R)-norbornan-2-yl, and (1R,4R)-norbornan-3-yl. The term "cycloalkyl", as used herein, unless otherwise specified, includes, but is not limited to, (1S,4S)-norbornan-2-yl, (1R,4S)-norbornan-2-yl, decalinyl, adamantyl, spiro[3.3]heptan-2-yl, 3-bicyclo[3.1.0]hexanyl, and the like. Examples of cycloalkyl include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, norbornyl, fenchyl, decalinyl, adamantyl, spiro[3.3]heptan-2-yl, 3-bicyclo[3.1.0]hexanyl, and the like.The term "cycloalkenyl" as used herein means a non-aromatic cyclic hydrocarbon radical having at least one site of unsaturation (usually 1-3, preferably 1), i.e., a carbon-carbon, sp2 double bond. The term "cycloalkenyl" also includes monocyclic or bicyclic groups, where the additional rings of polycyclic cycloalkenyls may be fused, bridged, and / or joined through one or more spiro atoms. Examples include, but are not limited to, cyclopentenyl and cyclohexenyl. The double bond may be in a cis or trans configuration. The term "cycloalkynyl" as used herein means a non-aromatic cyclic hydrocarbon radical having at least one site of unsaturation (usually 1-3, preferably 1), i.e., a carbon-carbon, sp triplet. An example is cyclohept-1-ene. A fused system of cycloalkyl rings with a heterocycloalkyl ring is considered to be a heterocycloalkyl, regardless of the ring attached to the core structure. A fused system of cycloalkyl rings with an aryl ring is considered to be an aryl, regardless of the ring attached to the core structure. A fused system of a cycloalkyl ring with a heteroaryl ring is considered heteroaryl, regardless of which ring is attached to the core structure.

[0045] The term "saturated or unsaturated heterocycloalkyl" as used herein includes saturated heterocycloalkyl as well as unsaturated non-aromatic heterocycloalkyl containing at least one heteroatom, i.e., N, O, or S, as a ring member. In particular, the terms "saturated or unsaturated heterocycloalkyl" and "saturated or non-aromatic unsaturated heterocycloalkyl" are synonymous. The term "heterocycloalkyl" as used herein means "cycloalkyl" unless otherwise stated, with the proviso that one or more carbon atoms (usually one, two, or three) are replaced by oxygen, nitrogen, or sulfur atoms, and the chain may not contain two adjacent O atoms or two adjacent S atoms. The term "heterocycloalkenyl" as used herein means "cycloalkenyl" unless otherwise stated, with the proviso that one or more carbon atoms (usually one, two, or three) are replaced by oxygen, nitrogen, or sulfur atoms, and the chain may not contain two adjacent O atoms or two adjacent S atoms. The term "heterocycloalkynyl," as used herein, unless otherwise noted, means "cycloalkynyl" in which one or more carbon atoms (usually 1, 2 or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain cannot contain two adjacent O atoms or two adjacent S atoms.Examples of saturated and unsaturated heterocycloalkyls include azepane, 1,4-oxazepane, azetane, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxalidine, morpholine, oxazolidine, oxepane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, thiomol. These include, but are not limited to, folin, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiacylcyclohexane, 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-pyrrolidine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine. Further heterocycloalkyls in the sense of the present invention are described in Paquette, Leo A. "Principles of Modern Heterocyclic Chemistry" (WA Benjamin, New York, 1968), in particular chapters 1, 3, 4, 6, 7, and 9; "The Chemistry of Heterocyclic Compounds, A series of Monographs" (John Wiley & Sons, New York, 1950 to present), in particular volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, C. Wand Scriven, E. "Comprehensive Heterocyclic Chemistry" (Pergamon Press, 1996); and J. Am. Chem. Soc. (1960) 82:5566. If the heterocycloalkyl does not contain nitrogen as a ring member, it is typically bonded through carbon. If the heterocycloalkyl contains nitrogen as a ring member, it can be bonded through nitrogen or carbon.A fused system of a heterocycloalkyl ring with a cycloalkyl ring is considered to be a heterocycloalkyl, regardless of the ring that is attached to the core structure. A fused system of a heterocycloalkyl ring with an aryl ring is considered to be a heterocycloalkyl, regardless of the ring that is attached to the core structure. A fused system of a heterocycloalkyl ring with a heteroaryl ring is considered to be a heteroaryl, regardless of the ring that is attached to the core structure.

[0046] The term "aryl" as used herein means an aromatic hydrocarbon. Typical aryl groups include, but are not limited to, radicals derived from 1-membered, or 2- or 3-membered benzene, naphthalene, anthracene, biphenyl, and the like, fused together. A fused system of an aryl ring with a cycloalkyl ring is considered an aryl, regardless of the ring that is attached to the core structure. A fused system of an aryl ring with a heterocycloalkyl ring is considered a heterocycloalkyl, regardless of the ring that is attached to the core structure. Thus, indoline, dihydrobenzofuran, dihydrobenzothiophene, and the like are considered heterocycloalkyl according to the present invention. A fused system of an aryl ring with a heteroaryl ring is considered a heteroaryl, regardless of the ring that is attached to the core structure.

[0047] The term "heteroaryl" as used herein means an aromatic ring system containing at least one heteroatom, i.e., N, O, or S, as a ring member of the aromatic ring system. Examples of heteroaryl include, but are not limited to, benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine.

[0048] As further examples, the carbon-bonded heterocycle is bonded at the 2-, 3-, 4-, 5-, or 6-position of pyridine, the 3-, 4-, 5-, or 6-position of pyridazine, the 2-, 4-, 5-, or 6-position of pyrimidine, the 2-, 3-, 5-, or 6-position of pyrazine, the 2-, 3-, 4-, or 5-position of furan, tetrahydrofuran, thiophene, pyrrole, or tetrahydropyrrole, the 2-, 4-, or 5-position of oxazole, imidazole, or thiazole, the 3-, 4-, or 5-position of isoxazole, prazole, or isothiazole, the 2- or 3-position of aziridine, the 2-, 3-, or 4-position of azetidine, the 2-, 3-, 4-, 5-, 6-, 7-, or 8-position of quinoline, or the 1-, 3-, 4-, 5-, 6-, 7-, or 8-position of isoquinoline.

[0049] 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. By way of example, nitrogen-bonded heterocycles are bonded to the 1-position of aziridine, azetidine, pyrrole, pyrrolidine, 2-pyrroline, 3-pyrroline, imidazole, imidazolidine, 2-imidazoline, 3-imidazoline, pyrazole, pyrazoline, 2-pyrazoline, 3-pyrazoline, piperidine, piperazine, indole, indoline, 1H-indazole, the 2-position of isoindole or isoindoline, the 4-position of morpholine, and the 9-position of carbazole or β-carboline. Preferred nitrogen-bonded heterocycles include 1-aziridyl, 1-azetidyl, 1-pyrrolyl, 1-imidazolyl, 1-pyrazolyl, and 1-piperidinyl. Further heteroaryls within the meaning of the present invention are described in Paquette, Leo A. "Principles of Modern Heterocyclic Chemistry" (WA Benjamin, New York, 1968), in particular chapters 1, 3, 4, 6, 7, and 9, "The Chemistry of Heterocyclic Compounds, A series of Monographs" (John Wiley & Sons, New York, 1950 to present), in particular volumes 13, 14, 16, 19, and 28, Katritzky, Alan R., Rees, C. Wand Scriven, E. "Comprehensive Heterocyclic Chemistry" (Pergamon Press, 1996); and J. Am. Chem. Soc. (1960) 82:5566.

[0050] As used herein with respect to substituents, unless otherwise indicated, the terms "monosubstituted," "disubstituted," "trisubstituted," "polysubstituted," and the like refer to chemical structures as defined herein, each of which is substituted with one or more substituents, and each of which means that one or more hydrogen atoms of the moiety are each independently replaced by a substituent. For example, -C which can be polysubstituted with -F. 1-6 -Alkyl is -CH 2 F, -CHF 2 , -CF 3 , -CH 2 CF 3 , C.F. 2 CF 3 Similarly, -C, which may be polysubstituted with substituents selected from -F and -Cl, independently of each other, 1-6 -Alkyl is -CH 2 F, -CHF 2 , -CF 3 , -CH 2 CF 3 , C.F. 2 CF 3 , -CH 2 Cl, -CHCl 2 , -CCl 3 , -CH 2 CCl 3 , CCl 2 CCl 3 , -CHClF, -CClF 2 , -CCl 2 CF 3 , -CF 2 CCl 3 , -CClFCCl 2 F, etc. Any substituent designation found at more than one site in a compound of the invention is intended to be independently selected.

[0051] As used herein, and unless otherwise specified, the term "solvate" includes any combination that may be formed by the derivatives of the present invention with suitable inorganic solvents (e.g., hydrates) or organic solvents, such as, but not limited to, alcohols, ketones, esters, ethers, nitriles, and the like.

[0052] The term "subject" as used herein refers to an animal, including a human, preferably a mammal, most preferably a human, who has been the object of treatment, observation or experiment.

[0053] As used herein, the term "therapeutically effective amount" refers to that amount of an active compound or pharmaceutical agent that elicits the biological or medicinal response in a tissue system, animal, or human that is sought by a researcher, veterinarian, physician, or other clinician, including alleviation or partial alleviation of the symptoms of the disease or disorder being treated.

[0054] As used herein, "composition" is intended to encompass a product containing therapeutically effective amounts of the specified ingredients, as well as any product resulting directly or indirectly from combining the specified ingredients in the specified amounts.

[0055] The terms "antagonist" or "inhibitor" as used herein refer to compounds capable of producing functional antagonists of the TRPM3 ion channel, including competitive antagonists, non-competitive antagonists, desensitizing agonists, and partial agonists, depending on the context.

[0056] For purposes of the present invention, the term "TRPM3 modulated" is used to refer to conditions that are affected by modulation of the TRPM3 ion channel, including conditions mediated by the TRPM3 ion channel.

[0057] The term "TRPM3-mediated disorder" as used herein refers to disorders or diseases consisting of pain and inflammatory hypersensitivity states, the symptoms of which are prevented, treated, (partially) alleviated or ameliorated by the use of antagonists of TRPM3. According to the International Association for the Study of Pain, for the purposes of the present 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 disorder is pain or epilepsy. Preferably, the TRPM3-mediated disorder is epilepsy, preferably selected from epileptic encephalopathies. For the purposes of the present invention, the term "epileptic encephalopathies" refers to a group of severe epilepsies characterized by both seizures and encephalopathy. Preferably, the TRPM3-mediated disorder is pain, preferably selected from nociceptive pain, inflammatory pain, and neuropathic pain. More preferably, the pain is postoperative pain. For purposes of the present invention, the term "inflammatory hypersensitivity" is used to refer to a condition characterized by one or more hallmarks of inflammation, including edema, erythema, hyperpyrexia and pain, and / or by an exaggerated physiological or pathophysiological response to one or more types of stimuli, including thermal, mechanical, and / or chemical stimuli.

[0058] The present invention will occasionally be further described with reference to particular embodiments, but the present invention is not limited thereto.

[0059] Preferred statements (features) and embodiments of the compounds and methods of the present invention are now described. Each statement and embodiment of the invention so defined may be combined with any other statement and / or embodiment, unless expressly indicated to the contrary. In particular, any feature indicated as being preferred or advantageous may be combined with any other one or more features indicated as being preferred or advantageous.

[0060] The numbered statements of this invention are as follows: 1. Compounds of formula (I), their stereoisomers, physiologically acceptable salts, solvates and / or polymorphs, [ka] During the ceremony, R 1 -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) 2 R W , -C(=O)R W , -C(=O)OR W or -C(=O)NR W R X represents Q is -OR 2 or -NR 3 R 4 represents R 2 But -R Y5 represents R 3 is -OH or -R Y1 represents R 4 But -R Y2 or -S(=O) 2 R Y3 represents Or, R 3 and R 4 together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 4-, 5-, 6-, 7-, or 8-membered heterocycle containing 1 to 3 heteroatoms selected from N, O, and S; T represents -O- and U represents -(CR 5 R 5 ') n - or T represents -(CR 5 R 5 ') n -, U represents -O-, n is an integer selected from 1, 2, 3, 4, or 5; R 5 and R 5 ', but independently of each other, -R Y4 represents R 6 , R 7 , and R 8 are, independently of each other, -F, -Cl, -Br, -I, -CN, -NO 2 ,-SCIENCE FICTION 5 , -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) 2 R W , -C(=O)R W , -C(=O)OR W or -C(=O)NR W R X represents W, saturated or unsaturated 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or In each case, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, During the ceremony, R W and R X but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, or A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered heterocycloalkyl, R Y1 , R Y2 , R Y3 , R Y4 , and R Y5 but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, "Mono- or polysubstituted" means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -C 1-6 -Alkylene-C(=O)-NH 2 , -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-NH 2 , -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 -NH 2 , -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 , -NH 2 , -NO, -NO 2 , -C 1-6 -Alkylene-NH 2 , -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)-NH 2 , -C 1-6 -Alkylene-NH-C(=O)-NH 2 , -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, -C1-6 -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)-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-NH 2 , -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) 2 OH, -C 1-6 -Alkylene-NH-S(=O) 2 OH, -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 -NH 2 , -C 1-6 -Alkylene-NH-S(=O) 2 -NH 2 , -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) 2 N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-S(=O) 2 N(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 -NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -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, -SF 5 , -SCF 3 , -SCF 2 H, -SCFH 2 , -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 -NH 2 , -C 1-6 -Alkylene-S(=O) 2 -NH 2 , -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- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-14 membered heteroaryl, -C 1-6 -Alkylene-(5-14 membered heteroaryl), -O-(3-14 membered cycloalkyl), -O-(3-14 membered heterocycloalkyl), -O-phenyl, -O-(5-14 membered heteroaryl), -C(=O)-(3-14 membered cycloalkyl), -C(=O)-(3-14 membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5-14 membered heteroaryl), -S(=O) 2 -(3 to 14 membered cycloalkyl), -S(=O) 2 -(3-14 membered heterocycloalkyl), -S(=O) 2 -phenyl, or -S(=O) 2 -(5-14 membered heteroaryl), or the compound is ethyl 5-methoxy-2-methyl-1-benzothiophene-3-carboxylate; In particular, the compound Compounds of formula (I), stereoisomers, physiologically acceptable salts, solvates and / or polymorphs thereof which are not 5-benzyloxybenzo[b]thiophene-3-carboxylic acid. 2.Q is -NR 3 R 4 2. The compound of claim 1, wherein 3.Q is -OR 2 2. The compound of claim 1, wherein 4. T represents -O- and U represents -(CR 5 R 5 ') n -, wherein 5.R 1 but, -H, -F, -Cl, -Br, -I, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -OC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)OC 1-6 -alkyl, -C(=O)NH 2 , Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)NHC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C(=O)N(C 1-6 -alkyl) 2 , Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O) 2 -C 1 - 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, or A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each occurrence representing a saturated or unsaturated, unsubstituted, mono- or poly-substituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted, 3- to 14-membered cycloalkyl. 6.R 1 but, -H, -F, -Cl, -Br, -I, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -OC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)OC 1-6 -alkyl, -C(=O)NH 2 , Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)NHC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C(=O)N(C 1-6 -alkyl) 2 , Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O) 2 -C 1 - 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, or An unsubstituted, mono- or poly-substituted 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, or 8- to 14-membered cycloalkynyl, each of which is represented by -C1 -C 6 -Alkylene- or -C 1 -C 6 A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each case representing a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, 8- to 14-membered cycloalkynyl. 7.R 1 -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 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkylene)-C 1-6 -Alkylene-CF 3 , -C(=O)C 1-6 -Alkyl, -C(=O)OC 1-6 -Alkyl, C(=O)NH 2 , -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, -OC1-6 A compound according to any one of the preceding statements, wherein R represents -alkyl, unsubstituted -cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl, or unsubstituted cyclohexyl. 8.R 1 is -H, unsubstituted, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -CHF 2 , -CF 3 or -cyclopentyl, 9.R 2 but, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each case representing a saturated or unsaturated, unsubstituted, mono- or poly-substituted, 5- to 14-membered heteroaryl. 10.R 2 but, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, or Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl. 11.R 2 But, -H, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C 1-6-Alkylene-NH 2 , -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , or -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 20. The compound according to any one of the preceding statements, wherein 12.R 2 is -H or -C which is saturated, unsubstituted or monosubstituted with -OH 1-6 A compound according to any one of the preceding statements, wherein: 13.R 2 A compound according to any one of the preceding statements, wherein represents -H. 14.R 3 but, -H, -OH, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each case representing a saturated or unsaturated, unsubstituted, mono- or poly-substituted, 5- to 14-membered heteroaryl. 15.R 3 but, -H, -OH, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, or Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl. 16.R 3 But -H, -OH, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , or -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 20. The compound according to any one of the preceding statements, wherein 17.R 3 is -H, -OH, or -C which is saturated, unsubstituted or monosubstituted with -OH; 1-6 A compound according to any one of the preceding statements, wherein: 18.R 3 A compound according to any one of the preceding statements, wherein represents -H. 19.R 4 but, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O) 2 -C 1 - 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each case representing a saturated or unsaturated, unsubstituted, mono- or poly-substituted, 5- to 14-membered heteroaryl. 20.R 4 but, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O) 2 -C 1 - 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6-heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Unsubstituted, mono- or polysubstituted -C 1-6 -alkylene-phenyl, unsubstituted, mono- or polysubstituted -phenyl, or An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each case representing a saturated or unsaturated, unsubstituted, mono- or poly-substituted, 5- to 14-membered heteroaryl. 21.R 4 but, Saturated or unsaturated, unsubstituted, independently of each other, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6-S(=O) mono- or polysubstituted with a substituent selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 2 C 1-6 -alkyl, -S(=O) 2 (3 to 14 membered cycloalkyl), wherein the 3 to 14 membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each occurrence of which is saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6-alkyl), -C(=O)N(C 1-6 -alkyl) 2 , S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -S(=O) mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 2 (3 to 14 membered cycloalkyl), Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6-alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -C is mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkyl, Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -C is mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1 -C 6 -heteroalkyl, 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3- to 14-membered cycloalkyl) 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 3- to 14-membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, in each case saturated or unsaturated, in each case unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -3- to 14-membered cycloalkyl or -C 1-6 -alkylene-(3 to 14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl or -C 1-6 -alkylene-(3- to 14-membered heterocycloalkyl), 1-6-alkylene- is unsubstituted or monosubstituted by -OH and the 3 to 14 membered heterocycloalkyl is, in each occurrence, azepane, 1,4-oxazepane, azetane, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxalidine, morpholine, oxazolidine, oxepane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane. , thiolane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiacylcyclohexane, 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-pyrrolidine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine, in each case unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -3- to 14-membered heterocycloalkyl, each of which is mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), Unsubstituted, -F, -Cl, -CN, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -C is mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkylene-phenyl, Unsubstituted, -F, -Cl, -CN, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -phenyl, which is mono- or polysubstituted with substituents independently selected from the group consisting of: -alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 1-6 -alkylene- is unsubstituted or monosubstituted by -OH and the 5- to 14-membered heteroaryl is, in each occurrence, benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, iso selected from the group consisting of quinoline, isothiazole, isoxazole, naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, in each case unsubstituted, -F, -Cl, -CN, -C 1-6 -Alkyl, -C 1-6-Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl, each of which is mono- or polysubstituted with a substituent selected from the group consisting of: 1-6 -alkylene-(5-14 membered heteroaryl), 22.R 4 but, -H, Saturated, unsubstituted, -S(=O) mono- or polysubstituted with -F 2 C 1-6 -alkyl, Saturated, unsubstituted -S(=O) 2 (3 to 14 membered cycloalkyl), Saturated, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3- to 14-membered cycloalkyl, unsubstituted phenyl, oxetanyl, or pyrimidinyl, each of which is mono- or polysubstituted with a substituent selected from the group consisting of 1-6 -alkyl, 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3- to 14-membered cycloalkyl) 1-6 -Alkylene- is unsubstituted or mono- or polysubstituted with -F, -Cl, -Br, -I, or -OH, and the 3- to 14-membered cycloalkyl is saturated, unsubstituted, -F, -Cl, -Br, -I, or -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3- to 14-membered cycloalkyl, unsubstituted phenyl, oxetanyl, or pyrimidinyl, each of which is mono- or disubstituted with a substituent selected from the group consisting of 3- to 14-membered cycloalkyl, unsubstituted phenyl, oxetanyl, or pyrimidinyl; 1-6 -alkylene-(3 to 14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl or -C 1-6 -alkylene-(3- to 14-membered heterocycloalkyl), 1-6 -Alkylene- is unsubstituted or mono- or polysubstituted by -F, -Cl, -Br, -I, -OH, and the 3- to 14-membered heterocycloalkyl is, in each case, azetane, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, -azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolidine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiacylcyclohexane, in each case unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2, 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5-14 membered heteroaryl, or -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 1-6 -alkylene- is unsubstituted or monosubstituted with -F, -Cl, -Br, -I, or -OH, and the 5- to 14-membered heteroaryl, at each occurrence, is selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, at each occurrence, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC1-6 -Alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -Alkyl, -NHC(=O)OC 1-6 -Alkyl, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl, or -C 1-6 -alkylene-(5-14 membered heteroaryl), 23.R 4 but, -H, Saturated, unsubstituted, -S(=O) mono- or polysubstituted with -F 2 C 1-6 -alkyl, Saturated, unsubstituted -S(=O) 2 (3 to 14 membered cycloalkyl), Saturated, unsubstituted, -OH, -OC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -C is mono- or disubstituted with substituents independently selected from the group consisting of -alkyl, -phenyl, and unsubstituted -C 1-6 -alkyl, 3-14 membered cycloalkyl or -C 1-6-alkylene-(3- to 14-membered cycloalkyl) 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 3- to 14-membered cycloalkyl is saturated, unsubstituted, -C 1-6 -Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -N(C 1-6 -alkyl) 2 , -NHC(=O)OC 1-6 -C11, -C21, -C31, -C41, -C51, -C61, -C71, -C81, -C91, -C101, -C112, -C121, 1-6 -alkylene-(3 to 14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl or -C 1-6 -alkylene-(3- to 14-membered heterocycloalkyl), 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, and the 3- to 14-membered heterocycloalkyl is, in each occurrence, azetane, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octa ... 1,2-dioxothiacylcyclohexane, 4-azabicyclo[3.3]hexane, 5-azabicyclo[3.4]hexane, 6-azabicyclo[3.5]hexane, 7-azabicyclo[3.6]hexane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolidine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiacylcyclohexane, 4-azabicyclo[3.4]hexane, 5-azabicyclo[3.5]hexane, 6-azabicyclo[3.4]hexane, 7-azabicyclo[3.5]hexane, 8-azabicyclo[3.4]hexane, 9-azabicyclo[3.4]hexane, 1,2 ... 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -C1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -S(=O) 2 C 1-6 -Alkyl, oxetanyl, pyrimidinyl, -C 1-6 -3 to 14-membered heterocycloalkyl or -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), unsubstituted phenyl, 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 5 to 14 membered heteroaryl, at each occurrence, is selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, and at each occurrence, is unsubstituted, -C 1-6 -5 to 14-membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 24.R 3 represents -H, R 4 but, -H, Saturated, unsubstituted, -S(=O) mono- or polysubstituted with -F 2 C 1-6 -alkyl, Saturated, unsubstituted -S(=O) 2 (3 to 14 membered cycloalkyl), Saturated, unsubstituted, -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkyl, -C(=O)NH 2 , -C(=O)-NH-C 1-3 -Alkyl, -C(=O)-N(C 1-3 -alkyl) 2 or unsubstituted phenyl, 1-6 -alkyl, 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3- to 14-membered cycloalkyl) 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 3- to 14-membered cycloalkyl is saturated, unsubstituted, -C 1-6 -Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -N(C 1-6 -alkyl) 2 , -NHC(=O)OC 1-6-C11, -C21, -C31, -C41, -C51, -C61, -C71, -C81, -C91, -C101, -C112, -C121, 1-6 -alkylene-(3 to 14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl or -C 1-6 -alkylene-(3- to 14-membered heterocycloalkyl), 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, and the 3- to 14-membered heterocycloalkyl is, in each occurrence, azetane, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octa ... 1,2-dioxothiacylcyclohexane, 4-azabicyclo[3.3]hexane, 5-azabicyclo[3.4]hexane, 6-azabicyclo[3.5]hexane, 7-azabicyclo[3.6]hexane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolidine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiacylcyclohexane, 4-azabicyclo[3.4]hexane, 5-azabicyclo[3.5]hexane, 6-azabicyclo[3.4]hexane, 7-azabicyclo[3.5]hexane, 8-azabicyclo[3.4]hexane, 9-azabicyclo[3.4]hexane, 1,2 ... 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -S(=O) 2 C1-6 -Alkyl, oxetanyl, pyrimidinyl, -C 1-6 -3 to 14-membered heterocycloalkyl or -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), unsubstituted phenyl, 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 5 to 14 membered heteroaryl, at each occurrence, is selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, and at each occurrence, is unsubstituted, -C 1-6 -5 to 14-membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 25.R 3 and R 4 and R are independently selected from N, O, and S; and R are independently selected from N, O, and S; and R is independently selected from N, O, and S. 26.R 3 and R 4 taken together form a heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine, and piperazine, in each occurrence unsubstituted or -C 1-6 -Alkyl, -NH 2 , -NHCH 3 , -N(CH 3 ) 2 , -C(=O)NH-C 1-6 -Alkyl, -C(=O)N(C 1-6 -alkyl) 2 , -C(=O)OC 1-6 -Alkyl, -NHC(=O)OC1-6 -alkyl, unsubstituted-pyridyl, and unsubstituted or -C 1-6 -1,2,4-oxadiazole mono- or polysubstituted with substituents independently selected from the group consisting of: 27.R 3 and R 4 But together, Unsubstituted or -N(CH 3 ) 2 a pyrrolidine ring monosubstituted with Unsubstituted or -C 1-6 -Alkyl, -NH 2 , -N(CH 3 ) 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 a piperidine ring, an unsubstituted morpholine ring, or Unsubstituted or -C 1-6 A compound according to any one of the preceding statements, forming a piperidine ring, N-substituted with a substituent selected from the group consisting of -alkyl and unsubstituted -pyridyl. 28.R 3 and R 4 together with the nitrogen atom to which they are attached, [Table 1] A compound according to any one of the preceding statements, forming a residue selected from the group consisting of: 29. W, Saturated or unsaturated 3- to 14-membered cycloalkyl, unsubstituted, mono- or di-substituted, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or di-substituted 3- to 14-membered cycloalkyl, unsubstituted, mono- or di-substituted 6- to 14-membered aryl; saturated or unsaturated, unsubstituted, mono- or di-substituted 3- to 14-membered heterocycloalkyl; unsubstituted, mono- or di-substituted 5- to 14-membered heteroaryl; or In each case, unsubstituted, monosubstituted or disubstituted -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, 30.W is unsubstituted, mono- or di-substituted, 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, or 8- to 14-membered cycloalkynyl; preferably, unsubstituted, mono- or di-substituted, 3- to 12-membered saturated cycloalkyl, 5- to 12-membered cycloalkenyl, or 8- to 12-membered cycloalkynyl; preferably, unsubstituted, mono- or di-substituted, 3- to 10-membered saturated cycloalkyl, 5- to 10-membered cycloalkenyl, or 8- to 10-membered cycloalkynyl; preferably, unsubstituted, mono- or di-substituted, 3- to 8-membered saturated cycloalkyl, 5- to 8-membered cycloalkenyl, or 8-membered cycloalkynyl; unsubstituted, mono- or di-substituted 6- to 14-membered aryl; saturated or unsaturated, unsubstituted, mono- or di-substituted 3- to 14-membered heterocycloalkyl; unsubstituted, mono- or di-substituted 5- to 14-membered heteroaryl; or In each case, unsubstituted, monosubstituted or disubstituted -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, 31. W, Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2, 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl, mono- or polysubstituted with substituents independently selected from, in particular, saturated or aromatically unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2-NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, 5- to 14-membered heteroaryl, or a 3- to 14-membered cycloalkyl, which is mono- or polysubstituted with substituents independently selected from the group consisting of 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, and 5- to 14-membered heteroaryl; Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , a mono- or poly-substituted 6- to 14-membered aryl independently selected from 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, and 5- to 14-membered heteroaryl; Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C1-6 -Alkylene-NHC(=O)OC 1-6 -Alkyl, -NHC(=O)OC 1-6 -Alkyl, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , a mono- or poly-substituted 3- to 14-membered heterocycloalkyl selected from 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, and 5- to 14-membered heteroaryl; Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-C1-6 -Alkylene-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , a mono- or poly-substituted 5- to 14-membered heteroaryl independently selected from 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, and 5- to 14-membered heteroaryl; or In each case, unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , -C mono- or polysubstituted with substituents independently selected from 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted -phenyl, and 5- to 14-membered heteroaryl; 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, 32. W, Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3-14 membered heterocycloalkyl, unsubstituted -phenyl, 5-14 membered heteroaryl, mono- or polysubstituted with substituents independently selected from 3- to 10-membered cycloalkyl, in particular saturated or aromatically unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2, 3- to 14-membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl, or Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2, -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , a mono- or poly-substituted 6- to 12-membered aryl independently selected from 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, and 5- to 14-membered heteroaryl; Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6-Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , a mono- or poly-substituted 3- to 10-membered heterocycloalkyl independently selected from 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, and 5- to 14-membered heteroaryl; Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , a mono- or poly-substituted 5- to 10-membered heteroaryl independently selected from 3- to 14-membered cycloalkyl, 3- to 14-membered heterocycloalkyl, unsubstituted phenyl, and 5- to 14-membered heteroaryl; or Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3- to 14-membered heterocycloalkyl, unsubstituted -phenyl, 5- to 14-membered heteroaryl, mono- or polysubstituted with substituents independently selected from the group consisting of -C 1 -C 6 -alkyl. 33. W, Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 3- to 14-membered cycloalkyl, mono- or polysubstituted with substituents independently selected from, in particular, saturated or non-aromatically unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6-alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 3 to 14-membered cycloalkyl, mono- or polysubstituted with substituents independently selected from Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a mono- or polysubstituted 6- to 14-membered aryl independently selected from Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2, -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a mono- or polysubstituted 3- to 14-membered heterocycloalkyl independently selected from Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 or In each case, unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2-NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, 34. W, Saturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 23- to 10-membered cycloalkyl, mono- or disubstituted with substituents independently selected from Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a mono- or polysubstituted 6- to 14-membered aryl independently selected from Saturated, unsubstituted, -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6-Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a mono- or di-substituted 3- to 10-membered heterocycloalkyl selected from Unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2, -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 or In each case, unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-OH, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl)2 -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, 35.R 5 and R 5 ' but independently of each other, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each occurrence representing a saturated or unsaturated, unsubstituted, mono- or poly-substituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted, 3- to 14-membered cycloalkyl. 36. n is an integer selected from 1, 2, or 3; R 5 and R 5 ' but independently of each other, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 A compound according to any one of the preceding statements, optionally connected through -heteroalkylene-, in each occurrence representing a saturated or unsaturated, unsubstituted, mono- or poly-substituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted, 3- to 14-membered cycloalkyl. 37.R 5 and R 5 ', but independently of each other, -H, -C 1 -C 6 -alkyl or -C 1 -C 6 -Alkylene-N(C 1 -C 6 -alkyl) 2 20. The compound according to any one of the preceding statements, wherein 38.R 6 , R 7 , and R 8 But independently of each other, -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 , -CN, -NO 2 , -C(=O)OH, -NH 2 , Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -OC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -NHC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -N(C 1-6 -alkyl) 2 , Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)OC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -OC(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1-6 -heteroalkyl. 39.R 6 , R 7 , and R 8 But independently of each other, -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 , -CN, -NO 2 , -C(=O)OH, -NH 2 , -C 1-6 -Alkyl, -CF 3 , -CHF 2 , -CH 2 F, -OC 1-6 -Alkyl, -OCF 3 , -OCHF 2 , -OCH 2 F, unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3, -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -NHC 1-6 -alkyl, unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -N(C 1-6 -alkyl) 2 , unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -C(=O)OC 1-6 -alkyl, unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -OC(=O)C 1-6 -alkyl, or unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -C 1-6 -heteroalkyl. 40.R 6 is -H, -F, -Cl, -CN, or -C 1 -C 6 A compound according to any one of the preceding statements, wherein: 41.R 6 does not represent -H. 42.R 7 is -H, -F, -Cl, -CN, or -C 1 -C 6 A compound according to any one of the preceding statements, wherein: 43.R 7 does not represent -H. 44.R 8 is -H, -F, -Cl, -CN, or -C 1 -C 6 A compound according to any one of the preceding statements, wherein: 45.R 8 does not represent -H. 46.(i)R 6 , R 7, and R 8 each represents -H, or (ii)R 6 , R 7 , and R 8 Two of them represent -H, and R 6 , R 7 , and R 8 the other is -F, -Cl, -CN, or -CH 3 represents or (iii)R 6 , R 7 , and R 8 One of the groups represents -H, and R 6 , R 7 , and R 8 are each independently -F, -Cl, -CN, or -CH 3 20. The compound according to any one of the preceding statements, wherein 47. A compound according to any one of the preceding statements, selected from the group consisting of compounds 001 to 152 as described herein and physiologically acceptable salts thereof. 48.R 1 H, -CH 2 F, -CHF 2 , or -CF 3 represents R2 represents H; R 3 represents -H, R 4 but, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case optionally connected through -heteroalkylene-, saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, Or, R 3 and R4 together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 5- or 6-membered heterocycle containing 1 or 2 heteroatoms selected from N, O, and S, R 5 and R 5 ', but independently of each other, -H, -C 1 -C 6 -alkyl or -C 1 -C 6 -Alkylene-N(C 1 -C 6 -alkyl) 2 represents R 6 , R 7 , and R 8 are each independently -H, -F, -Cl, -CN, or -C 1 -C 6 -alkyl, W, saturated or unsaturated 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or Unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl. 49.R 1 H, -CH 2 F, -CHF 2 , or -CF 3 represents R2 represents H; R 3 represents -H, R 4 but, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, An unsubstituted, mono- or poly-substituted 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, or 8- to 14-membered cycloalkynyl, each of which is represented by -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, 8- to 14-membered cycloalkynyl; A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, Or, R 3 and R 4together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 5- or 6-membered heterocycle containing 1 or 2 heteroatoms selected from N, O, and S, R 5 and R 5 ', but independently of each other, -H, -C 1 -C 6 -alkyl or -C 1 -C 6 -Alkylene-N(C 1 -C 6 -alkyl) 2 represents R 6 , R 7 , and R 8 are each independently -H, -F, -Cl, -CN, or -C 1 -C 6 -alkyl, W, unsubstituted, mono- or polysubstituted 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, or 8- to 14-membered cycloalkynyl; unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or Unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl. 50.R 1 H, -CH 2 F, -CHF 2 , or -CF 3 represents R 3 represents -H, R 4 but, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case optionally connected through -heteroalkylene-, saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, Or, R 3 and R 4 together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 5- or 6-membered heterocycle containing 1 or 2 heteroatoms selected from N, O, and S, R 5 and R 5 ', but independently of each other, -H, -C 1 -C 6 -alkyl or -C 1 -C 6 -Alkylene-N(C 1 -C 6 -alkyl) 2 represents R 6 , R 7 , and R 8 are each independently -H, -F, -Cl, -CN, or -C 1 -C 6 -alkyl, W, saturated or unsaturated 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or Unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl. 51.R 1 H, -CH 2 F, -CHF 2 , or -CF 3 represents R 3 represents -H, R 4 but, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, An unsubstituted, mono- or poly-substituted 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, or 8- to 14-membered cycloalkynyl, each of which is represented by -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, 8- to 14-membered cycloalkynyl; A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, Or, R 3 and R 4 together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 5- or 6-membered heterocycle containing 1 or 2 heteroatoms selected from N, O, and S, R 5 and R 5 ', but independently of each other, -H, -C 1 -C 6 -alkyl or -C 1 -C 6 -Alkylene-N(C 1 -C 6 -alkyl) 2 represents R 6 , R 7 , and R 8 are each independently -H, -F, -Cl, -CN, or -C 1 -C 6 -alkyl, W, unsubstituted, mono- or polysubstituted 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, or 8- to 14-membered cycloalkynyl; unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or Unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl. 52. A pharmaceutical composition or medicament comprising a compound according to any one of the preceding statements. 53. A compound according to any one of the preceding statements or a pharmaceutical composition according to statement 52 for use as a medicament. 54. A compound according to any one of the preceding statements or a pharmaceutical composition according to statement 52, for use in the treatment of pain or epilepsy, preferably pain and epileptic encephalopathy. 55. The compound for use or pharmaceutical composition for use according to statement 54, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain. 56. The compound for use or pharmaceutical composition for use according to statement 55, wherein the pain is post-operative pain. 57. A method for the prevention and / or treatment of a TRPM3-mediated disorder, comprising administering to a subject an effective amount of a compound according to any one of the preceding statements 1 to 51, or a pharmaceutical composition according to claim 52. 58. A method for the prevention and / or treatment of pain, or epilepsy, such as epileptic encephalopathy, comprising administering to a subject an effective amount of a compound according to any one of the preceding statements 1 to 51, or a pharmaceutical composition according to claim 52. 59. The method of claim 58, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain.

[0061] A first aspect of the present invention provides a compound of formula (I), its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs, [ka] During the ceremony, R 1 -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) 2 R W , -C(=O)R W , -C(=O)OR W or -C(=O)NR W R X represents Q is -OR 2 or -NR 3 R 4 represents R 3 is -OH or -R Y1 represents R 4 But -R Y2 or -S(=O) 2 R Y3 represents Or, R 3 and R 4 together form a saturated or unsaturated, unsubstituted, mono- or polysubstituted 4-, 5-, 6-, 7-, or 8-membered heterocycle containing 1 to 3 heteroatoms selected from N, O, and S; T represents -O- and U represents -(CR 5 R 5 ') n - or T represents -(CR 5 R 5 ') n -, U represents -O-, n is an integer selected from 1, 2, 3, 4, or 5; R 5 and R 5 ', but independently of each other, -R Y4 represents R 6 , R 7 , and R 8 are, independently of each other, -F, -Cl, -Br, -I, -CN, -NO 2 ,-SCIENCE FICTION 5 , -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) 2 R W , -C(=O)R W , -C(=O)OR W or -C(=O)NR W R X represents W, saturated or unsaturated 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, unsubstituted, mono- or polysubstituted 6- to 14-membered aryl; saturated or unsaturated, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; Mono- or polysubstituted 5- to 14-membered heteroaryl, or In each case, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, During the ceremony, R W and R X but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, or A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered heterocycloalkyl, R Y1 , R Y2 , R Y3 , R Y4 , and R Y5 but independently of one another, and in each case independently, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl, "Mono- or polysubstituted" means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6-Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -C 1-6 -Alkylene-C(=O)-NH 2 , -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-NH 2 , -OC1-6 -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 -NH 2 , -C 1-6 -Alkylene-OS(=O) 2 -NH 2 , -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 , -NH 2 , -NO, -NO 2 , -C 1-6 -Alkylene-NH 2 , -NH(C 1-6 -alkyl), -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl) 2 , -C1-6 -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)-NH 2 , -C 1-6 -Alkylene-NH-C(=O)-NH 2 , -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)-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-NH 2 , -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) 2 OH, -C 1-6 -Alkylene-NH-S(=O) 2 OH, -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 -NH 2 , -C 1-6 -Alkylene-NH-S(=O) 2 -NH 2 , -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) 2 N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-S(=O) 2 N(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 -NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -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, -SF 5 , -SCF 3 , -SCF 2 H, -SCFH 2 , -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 -NH 2 , -C 1-6 -Alkylene-S(=O) 2 -NH 2 , -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- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-14 membered heteroaryl, -C 1-6 -Alkylene-(5-14 membered heteroaryl), -O-(3-14 membered cycloalkyl), -O-(3-14 membered heterocycloalkyl), -O-phenyl, -O-(5-14 membered heteroaryl), -C(=O)-(3-14 membered cycloalkyl), -C(=O)-(3-14 membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5-14 membered heteroaryl), -S(=O) 2 -(3 to 14 membered cycloalkyl), -S(=O) 2 -(3-14 membered heterocycloalkyl), -S(=O) 2 -phenyl, or -S(=O) 2-(5-14 membered heteroaryl), or the compound is ethyl 5-methoxy-2-methyl-1-benzothiophene-3-carboxylate; The compound is Not 5-benzyloxybenzo[b]thiophene-3-carboxylic acid.

[0062] In some embodiments, Q is -NR 3 R 4 Represents.

[0063] In some embodiments, Q is -OR 2 Represents.

[0064] In some embodiments, T represents -O- and U represents -(CR 5 R 5 ') n -, where n is an integer selected from 1, 2, or 3.

[0065] In some embodiments, R 1 teeth, -H, -F, -Cl, -Br, -I, -CN, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, -OH, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -OC 1-6 -alkyl, -NH 2 , Saturated or unsaturated, unsubstituted, mono- or poly-substituted -NHC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -N(C 1-6 -alkyl) 2 , Saturated or unsaturated, unsubstituted, mono- or polysubstituted -NHC(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -NC 1-6 -AlkylC(=O)C 1-6 -alkyl, -SH, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -SC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)OC 1-6 -alkyl, -C(=O)NH 2 , Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)NHC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C(=O)N(C 1-6 -alkyl) 2 , Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O) 2 -C 1 - 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, or A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, which in each case represents a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered heterocycloalkyl.

[0066] In some embodiments, R 1 teeth, -H, -F, -Cl, -Br, -I, -CN, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C 1-6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6-Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C 1 -C 6 -heteroalkyl, -OH, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2, -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -OC, each of which is mono- or polysubstituted with a substituent selected independently from the group consisting of: 1-6 -Alkyl, -OC 2 -C6 -Alkenyl, -OC 2 -C 6 -alkynyl, -NH 2 , Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O)2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -NHC, mono- or polysubstituted with substituents independently selected from the group consisting of: 1-6 -alkyl, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -N(C 1-6 -alkyl) 2 , Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6-Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -NHC(=O)C mono- or polysubstituted with substituents independently selected from the group consisting of 1-6 -alkyl, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -NC, mono- or polysubstituted with substituents independently selected from the group consisting of: 1-6 -AlkylC(=O)C 1-6 -alkyl, -SH, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -C1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -Alkyl, -NHC(=O)OC 1-6 -Alkyl, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -SC, each of which is mono- or polysubstituted with substituents independently selected from the group consisting of: 1-6 -Alkyl, -SC 2 -C 6 -Alkenyl, -SC 2 -C 6 -alkynyl, Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C(=O)C mono- or polysubstituted with substituents independently selected from the group consisting of 1-6 -alkyl, Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C(=O)OC, mono- or polysubstituted with substituents independently selected from the group consisting of: 1-6 -alkyl, -C(=O)NH 2 , Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C(=O)NHC, mono- or polysubstituted with substituents independently selected from the group consisting of: 1-6 -alkyl, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C(=O)N(C 1-6 -alkyl) 2 , Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -S(=O)C mono- or polysubstituted with substituents independently selected from the group consisting of 1-6 -alkyl, Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -S(=O) 2 -C 1-6-alkyl, Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl)2 -C 1 -C 6 -heteroalkyl, or Unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2, -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a 3- to 14-membered cycloalkyl group, which is mono- or polysubstituted with substituents independently selected from the group consisting of: A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 and represents a 3- to 14-membered cycloalkyl which is mono- or polysubstituted with substituents independently selected from the group consisting of:

[0067] In some embodiments, R 1 -H, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -Alkynyl, -OH, -OC 1-6 -Alkyl, -SH, -NH 2 , -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 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2, -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -C(=O)C 1-6 -Alkyl, -C(=O)OC 1-6 -Alkyl, -C(=O)NH 2 , -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- to 14-membered cycloalkyl, or unsubstituted 3- to 14-membered heterocycloalkyl. 1 -H, -F, -Cl, -Br, -I, CN, -C 1-6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -Alkynyl, -OH, -OC 1-6 -Alkyl, -SH, -NH 2 , -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 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3, -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -C(=O)C 1-6 -Alkyl, -C(=O)OC 1-6 -Alkyl, -C(=O)NH 2 , -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.

[0068] In some embodiments, R 1 are -H, CN, and -C 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -CH 2 F, -CHF 2 , -CF 3 , -C(=O)NH 2 , unsubstituted cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl, or unsubstituted cyclohexyl. 1 -H, -CH 2 F, -CHF 2 , -CF 3 , -C(=O)NH 2 , -CN, unsubstituted cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl, or unsubstituted cyclohexyl. 1 -H, -C 1-6 -Alkyl, -C(=O)NH 2, -CHF 2 , unsubstituted cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl, or unsubstituted cyclohexyl.

[0069] Preferably, R 1 -H, -CN, -C 1-3 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-3 -Alkylene-CF 3 , -C 1-3 -Alkylene-CF 2 H, -C(=O)NH 2 , or -C 1-3 -Alkylene-CFH 2 , more preferably -H, -CH 3 , or -CF 2 Represents H.

[0070] In some embodiments, R 2 teeth, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, which in each case represents a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl.

[0071] In some embodiments, R 2 teeth, -H, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3, -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1-C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, which in each case is unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 and in particular, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is selected from the group consisting of: 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a 3- to 14-membered cycloalkyl group, which is mono- or polysubstituted with substituents independently selected from the group consisting of: An unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a 3- to 14-membered heterocycloalkyl group, which is mono- or polysubstituted with substituents independently selected from the group consisting of An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2, -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 or a 6- to 14-membered aryl, each of which is mono- or polysubstituted with substituents independently selected from the group consisting of An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 and represents a 5- to 14-membered heteroaryl which is mono- or polysubstituted with substituents independently selected from the group consisting of:

[0072] In some embodiments, R2 teeth, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, or Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl.

[0073] In some embodiments, R 2 -H, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-C(=O)-NH 2 , -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , or -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 Preferably, R 2 -H, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6-Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , or -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 Preferably, R 2 is -H or -C which is saturated, unsubstituted or monosubstituted with -OH; 1-6 -alkyl. Preferably, R 2 represents -H.

[0074] In some embodiments, R 2 -H, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6-Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , or -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 Represents.

[0075] In some embodiments, R 2 is -H or -C 1-6 - represents alkyl.

[0076] In some embodiments, Q is -OR 2 R 1 -C 1-6 -Alkyl, -CH 2 F, -CHF 2 , or -CF 3 Represents.

[0077] In some embodiments, R 3 teeth, -H, -OH, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, which in each case represents a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl.

[0078] In some embodiments, R 3 teeth, -H, -OH, In each case, unsubstituted -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2-NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, Unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6-Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, which in each case is unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-C1-6 -Alkylene-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 and in particular, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is selected from the group consisting of: 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a 3- to 14-membered cycloalkyl group, which is mono- or polysubstituted with substituents independently selected from the group consisting of: An unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 a 3- to 14-membered heterocycloalkyl group, which is mono- or polysubstituted with substituents independently selected from the group consisting of An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 or a 6- to 14-membered aryl, each of which is mono- or polysubstituted with substituents independently selected from the group consisting of An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case, saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)OC1-6 -Alkyl, -C(=O)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 and represents a 5- to 14-membered heteroaryl which is mono- or polysubstituted with substituents independently selected from the group consisting of:

[0079] In some embodiments, R 3 teeth, -H, -OH, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, or Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl.

[0080] In some embodiments, R 3 -H, -OH, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-C(=O)-NH 2 , -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , or -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 Preferably, R 3 -H, -OH, -C 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH(C 1-6 -alkyl), -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , or -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 Preferably, R 3 is -H, -OH, or -C which is saturated, unsubstituted or monosubstituted with -OH; 1-6-alkyl. Preferably, R 3 represents -H.

[0081] In some embodiments, R 3 and R 4 do not both represent -H. In some embodiments, R 3 represents -H, R 4 does not represent -H.

[0082] In some embodiments, R 4 teeth, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -S(=O) 2 -C 1 - 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6-heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered heterocycloalkyl; An unsubstituted, mono- or polysubstituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 6- to 14-membered aryl; An unsubstituted, mono- or polysubstituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, which in each case represents a saturated or unsaturated, unsubstituted, mono- or polysubstituted, 5- to 14-membered heteroaryl.

[0083] Preferably, R 4 teeth, Unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -S(=O) mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 2 C 1-6 -alkyl, -S(=O) 2 (3 to 14 membered cycloalkyl), wherein the 3 to 14 membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each occurrence of which is saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3, -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -S(=O) mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 2 (3 to 14 membered cycloalkyl), Unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl, 1-6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, 3-14 membered cycloalkyl or -C 1-6-alkylene-(3- to 14-membered cycloalkyl) 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 3- to 14-membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, in each case saturated or unsaturated, in each case unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C1-6 -3- to 14-membered cycloalkyl or -C 1-6 -alkylene-(3 to 14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl or -C 1-6 -alkylene-(3- to 14-membered heterocycloalkyl), 1-6 -alkylene- is unsubstituted or monosubstituted by -OH and the 3 to 14 membered heterocycloalkyl is, in each occurrence, azepane, 1,4-oxazepane, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxalidine, morpholine, oxazolidine, oxepane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thio oran, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiacylcyclohexane, 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-pyrrolidine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine, in each case unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -3- to 14-membered heterocycloalkyl, each of which is mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), Unsubstituted, -F, -Cl, -CN, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -phenyl, which is mono- or polysubstituted with substituents independently selected from the group consisting of: -alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 1-6-alkylene- is unsubstituted or monosubstituted with -OH, and the 5- to 14-membered heteroaryl, at each occurrence, is selected from the group consisting of benzimidazole, benzisoxazole, benzoxazole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, at each occurrence unsubstituted, -F, -Cl, -CN, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6-Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl, each of which is mono- or polysubstituted with a substituent selected from the group consisting of: 1-6 -alkylene-(5- to 14-membered heteroaryl).

[0084] Preferably, R 4 teeth, -H, -S(=O) mono- or polysubstituted with -F 2 C 1-6 -alkyl, Unsubstituted -S(=O) 2 (3 to 14 membered cycloalkyl), -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkyl, -C(=O)NH 2 , -C(=O)-NH-C 1-3 -Alkyl, -C(=O)-N(C 1-3 -alkyl) 2 or unsubstituted phenyl, 1-6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C6 -alkynyl, 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3- to 14-membered cycloalkyl) 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 3- to 14-membered cycloalkyl is saturated, unsubstituted, -C 1-6 -Alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -Alkyl, -OH, -OC 1-6 -Alkyl, -NH 2 , -N(C 1-6 -alkyl) 2 , -NHC(=O)OC 1-6 -C11, -C21, -C31, -C41, -C51, -C61, -C71, -C81, -C91, -C101, -C112, -C121, 1-6 -alkylene-(3 to 14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl or -C 1-6 -alkylene-(3- to 14-membered heterocycloalkyl), 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, and the 3- to 14-membered heterocycloalkyl is, in each occurrence, azetane, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octa ... 1,2-dioxothiacylcyclohexane, 4-azabicyclo[3.3]hexane, 5-azabicyclo[3.4]hexane, 6-azabicyclo[3.5]hexane, 7-azabicyclo[3.6]hexane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolidine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiacylcyclohexane, 4-azabicyclo[3.4]hexane, 5-azabicyclo[3.5]hexane, 6-azabicyclo[3.4]hexane, 7-azabicyclo[3.5]hexane, 8-azabicyclo[3.4]hexane, 9-azabicyclo[3.4]hexane, 1,2 ...1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -S(=O) 2 C 1-6 -Alkyl, oxetanyl, pyrimidinyl, -C 1-6 -3 to 14-membered heterocycloalkyl or -C 1-6 -alkylene-(3 to 14 membered heterocycloalkyl), unsubstituted phenyl, 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), 1-6 -alkylene- is unsubstituted or monosubstituted with -OH, and the 5 to 14 membered heteroaryl, at each occurrence, is selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, and at each occurrence, is unsubstituted, -C 1-6 -5 to 14-membered heteroaryl or -C 1-6 -alkylene-(5- to 14-membered heteroaryl).

[0085] In some embodiments, R 4 teeth, The following: [Table 2] or Unsubstituted, mono- or polysubstituted C 1 -C 6 -alkyl, preferably the residue -CR'R"-(CH 2 ) m m is an integer selected from 1, 2, 3, 4, 5, or 6, preferably selected from 1, 2, or 3; R′ and R″ are each independently selected from —H, —C 1-3 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -C 1-3 -Alkylene-CF 3 , -C 1-3 -Alkylene-CF 2 H, -C 1-3 -Alkylene-CFH 2 , -C 1-3 -Alkylene-OC 1-3 -Alkyl, -C 1-3 -Alkylene-OH, -C(=O)-NH 2 , -C(=O)-NH-C 1-3 -Alkyl, or -C(=O)-N(C 1-3 -alkyl) 2 , preferably -H, -CH 3 , -C 1-3 -Alkylene-OH, C(=O)-NH 2 , -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, and preferably [Table 3] or represents a saturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 13-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 12-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 11-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 10-membered cycloalkyl, preferably the following: [Table 4] a cycloalkyl residue selected from the group consisting of A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 12-membered cycloalkyl, wherein the 3- to 12-membered cycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 10-membered cycloalkyl, wherein the 3- to 10-membered cycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 8-membered cycloalkyl, wherein the 3- to 8-membered cycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6-alkylene-, in particular, saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 12-membered cycloalkyl, wherein the 3- to 12-membered cycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 10-membered cycloalkyl, wherein the 3- to 10-membered cycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 8-membered cycloalkyl, wherein the 3- to 8-membered cycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-connected 3-8 membered cycloalkyl, preferably the following: [ka] or represents a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 13-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 11-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably the following: [Table 5-1] [Table 5-2] More preferably, selected from the group consisting of: [Table 6] or A saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 12-membered heterocycloalkyl, wherein the 3- to 12-membered heterocycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably a saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 10-membered heterocycloalkyl, wherein the 3- to 10-membered heterocycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6-alkylene-, preferably a saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 8-membered heterocycloalkyl, wherein the 3- to 8-membered heterocycloalkyl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-connected 3-8 membered heterocycloalkyl, preferably the following: [Table 7] or an unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 8-membered aryl, or An unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, wherein the 6- to 14-membered aryl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, wherein the 6- to 12-membered aryl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl, wherein the 6- to 10-membered aryl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-connected 6-10 membered aryl, preferably the following: [Table 8] or It represents an unsubstituted, mono-substituted or poly-substituted 5-14 membered heteroaryl, preferably an unsubstituted, mono-substituted or poly-substituted 5-12 membered heteroaryl, preferably an unsubstituted, mono-substituted or poly-substituted 5-10 membered heteroaryl, preferably an unsubstituted, mono-substituted or poly-substituted 5-9 membered heteroaryl, preferably the following: [Table 9-1] [Table 9-2] and more preferably represents a residue selected from the group consisting of: [Table 10] or An unsubstituted, mono- or poly-substituted 5- to 14-membered heteroaryl, wherein the 5- to 14-membered heteroaryl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, preferably an unsubstituted, mono- or poly-substituted 5- to 12-membered heteroaryl, wherein the 5- to 12-membered heteroaryl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, and an unsubstituted, mono- or poly-substituted 5- to 10-membered heteroaryl, wherein the 5- to 10-membered heteroaryl is a saturated or unsaturated, unsubstituted, mono- or poly-substituted -C 1 -C 6 -alkylene-, and the 5-8 membered heteroaryl is a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-bonded 5-8 membered heteroaryl, preferably a residue selected from the group consisting of: [Table 11]

[0086] In some embodiments, R 4 represents a residue according to general formula (A), [ka] During the ceremony, m A is 0 or 1, Y A -O-, -NR A6 - and -CR A7 R A8 - selected from R A1 , R A2 , R A3 , R A4 , R A5 , R A6 , R A7 , and R A8 are, independently of each other, -H, -F, -C 1-3 -Alkyl, -C 1-3 -Alkylene-OH, -C 1-3 -Alkylene-NH 2 , -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-CF 3 ), -C 1-3 -Alkylene-C(=O)NH 2 , -C 1-3 -Alkylene-NH-C(=O)OC 1-4 -Alkyl, -C(=O)NH 2 , -C(=O)-NH-C 1-3 -Alkyl, -C(=O)-N(C 1-3 -alkyl) 2 or -3-oxetanyl, or R A7 and R A8together with the carbon atoms to which they are attached form a ring, -CH 2 OCH 2 -, -CH 2 OCH 2 CH 2 -or-CH 2 CH 2 OCH 2 CH 2 -, -CH 2 NHCH 2 -, -CH 2 NHCH 2 CH 2 -or-CH 2 CH 2 NHCH 2 CH 2 - represents.

[0087] In some embodiments, R 4 represents a residue according to general formula (A) as defined above, m A is 0 or 1, Y A However, -O- and -CR A7 R A8 - selected from R A1 , R A2 , R A3 , R A4 , R A5 , R A7 , and R A8 are, independently of each other, -H, -C 1-3 -Alkylene-OH, -C 1-3 -Alkylene-N(C 1-3 -alkyl) 2 , or -C(=O)NH 2 Preferably, R A1 , R A2 , R A3 , R A4 , R A5 , R A7 , and R A8 represents a residue that is not -H.

[0088] In some embodiments, R 4represents a residue according to general formula (A) as defined above, m A is 0 or 1, Y A However, -O- and -CR A7 R A8 - selected from R A1 But -C 1-3 -Alkylene-OH, -C 1-3 -Alkylene-N(C 1-3 -alkyl) 2 , or -C(=O)NH 2 represents R A2 , R A3 , R A4 , R A5 , R A7 , and R A8 represents -H.

[0089] In some embodiments, R 4 represents a residue according to general formula (B), [ka] During the ceremony, Y B -O-, -NR B8 - and -CR B9 R B10 - selected from R B1 , R B2 , R B3 , R B4 , R B5 , R B6 , R B7 , R B8 , R B9 , and R B10 are independently -H, -F, -OH, -C(=O)-NH 2 , -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-CF 3 , -C 1-3 -Alkylene-CO 2 H or -C 1-3 -Alkylene-C(=O)OC 1-3 -alkyl or R B2 and R B3 taken together represent =O or R B4 and R B5 Together, they represent =O.

[0090] In some embodiments, R 4 represents a residue according to general formula (B) as defined above, Y B -O- and -NR B8 - selected from R B1 , R B2 , R B3 , R B4 , R B5 , R B6 , R B7 , R B8 However, independently of each other, -H, -F, -C 1-3 -Alkyl, -C 1-3 -Alkylene - OH, -C 1-3 -Alkylene-CF 3 or -C(=O)-NH 2 or R B2 and R B3 together represent =O or R B4 and R B5 taken together represent =O or preferably R A1 , R A2 , R A3 , R A4 , R A5 , R A7 , and R A8 represents a residue that is not -H, preferably A1 , R A2 , R A3 , R A4 , R A5 , R A7 , and RA8 represents a residue that is not -H.

[0091] In some embodiments, R 4 represents a residue according to general formula (C), [ka] During the ceremony, Y C1 But -O-, -S(=O) 2 -, -NR C8 - and -CR C9 R C10 - or Y C2 But -CR C11 R C12 - or Y C1 But -CR C9 R C10 - represents Y C2 But -O-, -S(=O) 2 - and -NR C8 - selected from 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 But independently of each other, -H, -F, -OH, -C(=O)OC 1-3 -Alkyl, -NH 2 , -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl) 2 , -C 1-3 -Alkyl, -C 1-3 -Alkylene-OH, -C 1-3 -Alkylene-CF 3 , -C(=O)-NH 2 , -C(=O)-NH-C 1-3 -Alkyl, or -C(=O)N-(C 1-3 -alkyl) 2or R C2 and R C3 together represent =O or R C4 and R C5 together represent =O or R C9 and R C10 together represent =O or R C11 and R C12 Together they represent =O.

[0092] In some embodiments, R 4 represents a residue according to general formula (C) as defined above, Y C1 is -O- or -NR C8 - selected from Y C2 But -CR C11 R C12 - or Y C1 But -CR C9 R C10 - represents Y C2 -O- and -NR C8 - selected from 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 However, independently of each other, -H, -F, -C 1-3 -Alkyl, -C 1-3 -Alkylene-OH or -C(=O)-NH 2 or preferably R C1 , R C2 , R C3 , R C4 , R C5 , R C6 , R C7 , R C8 , R C9 , R C10 , R C11 , and R C12represents a residue that is not -H, preferably C1 , R C2 , R C3 , R C4 , R C5 , R C6 , R C7 , R C8 , R C9 , R C10 , R C11 , and R C12 represents a residue that is not -H.

[0093] In some embodiments, R 4 teeth, (i) Residue -CR'R”-(CH 2 ) m -OH, in which m is an integer of 1 to 6, preferably an integer of 1 to 3; R' and R" are each independently -H, -C 1-3 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -C 1-3 -Alkylene-CF 3 , -C 1-3 -Alkylene-CF 2 H, -C 1-3 -Alkylene-CFH 2 , -C 1-3 -Alkylene-OC 1-3 -alkyl or -C 1-3 -alkylene-OH, preferably -H, -CH 3 , or -C 1-3 - alkylene-OH, the residue -CR'R"-(CH 2 ) m In a preferred embodiment, at least R' or R" does not represent -H. In a preferred embodiment, neither R' nor R" represents -H, or (ii) a residue according to general formula (D), [ka] During the ceremony, m D and nD are each independently 0, 1, 2 or 3, but preferably m D +n D Provided that ≦3, Y D1 But -O-, -S(=O) 2 -, -NR D8 - and -CR D9 R D10 - selected from Y D2 But -CR D11 R D12 - or Y D1 But -CR D9 R D10 - represents Y D2 But -O-, -S(=O) 2 - and -NR D8 - selected from 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 However, independently of each other, -H, -F, -OH, -C 1-3 -Alkylene-OH, -C(=O)NH 2 , -C 1-3 -Alkylene-C(O)NH 2 , -C(=O)OC 1-3 -Alkyl, -NH 2 , -C 1-3 -Alkylene-NH 2 , -NH(C 1-3 -alkyl), -N(C 1-3 -alkyl) 2 , -NH(C 1-3 -Alkylene-CF 3 ), -C 1-3 -Alkylene-OCH 3 , -C 1-3 -Alkyl, -C 1-3 -Alkylene-CF 3 or R D2 and R D3together represent =O or R D4 and R D5 together represent =O or R D9 and R D10 together represent =O or R D11 and R D12 together represent =O, Preferably, m D and n D are each independently 0, 1, 2 or 3, but preferably m D +n D Provided that ≦3, Y D1 -O-, -NR D8 - and -CR D9 R D10 - selected from Y D2 But -CR D11 R D12 - or Y D1 But -CR D9 R D10 - represents Y D2 -O- and -NR D8 - selected from 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 However, independently of each other, -H, -F, -OH, -C 1-3 -Alkylene-OH, -C(=O)NH 2 , -CH 2 NH 2 , -CH 2 N(CH 3 ) 2 , -NHCH 2 CF 3 , -CH 3 , or -CH 2 CF 3 or R D2 and R D3together represent =O or R D4 and R D5 together represent =O or R D9 and R D10 together represent =O or R D11 and R D12 taken together represent =O, preferably 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 represents a residue that is not -H, preferably D1 , R D2 , R D3 , R D4 , R D5 , R D6 , R D7 , R D8 , R D9 , R D10 , R D11 , and R D12 represents a residue that is not -H.

[0094] In some embodiments, R 4 is a residue according to the general formula (A), (B), (C), (D) or the formula -CR'R"-(CH 2 ) m Represents the residue of -OH.

[0095] In some embodiments, R 4 represents a residue selected from the group consisting of: -CH 3 , [Table 12]

[0096] In some embodiments, R 3is H and R 4 is any of the embodiments previously described herein.

[0097] In some embodiments, R 5 and R 5 ' are independent of each other, -H, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1 -C 6 -heteroalkyl, A saturated or unsaturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, in each case saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C 1 -C 6 -Alkylene- or -C 1 -C 6 -heteroalkylene-, optionally connected through, in each case representing a saturated or unsaturated, unsubstituted, mono- or polysubstituted, saturated or non-aromatic unsaturated, unsubstituted, mono- or polysubstituted, 3- to 14-membered cycloalkyl.

[0098] Preferably, R 5 and R 5 ' are, independently of each other, -H, -C 1 -C 6 -alkyl or -C 1 -C 6 -Alkylene-N(C 1 -C 6 -alkyl)2 Shows.

[0099] In some embodiments, R 5 and R 5 At least one of the ' is not -H.

[0100] In some embodiments, R 5 and R 5 ' are both -H.

[0101] In a preferred embodiment, T represents -O- and U represents -(CR 5 R 5 ') n represents the resulting moiety -O-(CR 5 R 5 ') n - represents a residue selected from the group consisting of: [Table 13]

[0102] In some embodiments, R 5 represents -H, R 5 ', -H, -C 1-3 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -C 1-3 -Alkylene-CF 3 , -C 1-3 -Alkylene-CF 2 H, -C 1-3 -Alkylene-CFH 2 , and -C 1-3 -Alkylene-OH, preferably -H or C 1-3 -alkyl.

[0103] In some embodiments, R 6 , R 7 , and R 8 are independent of each other, -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 , -CN, -NO 2 , -C(=O)OH, -NH 2 , Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -OC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -NHC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -N(C 1-6 -alkyl) 2 , Saturated or unsaturated, unsubstituted, mono- or poly-substituted -C(=O)OC 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or poly-substituted -OC(=O)C 1-6 -alkyl, Saturated or unsaturated, unsubstituted, mono- or polysubstituted -C 1-6 -heteroalkyl.

[0104] In some embodiments, R 6 , R 7 , and R 8 are independent of each other, -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 , -CN, -NO 2 , -C(=O)OH, -NH 2 , In each case, saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -C is mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C1-6 -Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -OC, mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkyl, Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6-Alkylene-OC 1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -NHC mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkyl, Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -N(C) mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkyl) 2 , Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC1-6 -Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -C(═O)OC mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl. 1-6 -alkyl, Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OH, -C 1-6 -Alkylene-OC 1-6-Alkyl, -NH 2 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -OC(═O)C mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -alkyl, Saturated or unsaturated, unsubstituted, -F, -Cl, -C 1-6 -Alkyl, -C 1-6 -Alkylene-CF 3 , -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-NH 2 , -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-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -C(=O)NH 2 , -C(=O)NH(C 1-6 -alkyl), -C(=O)N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -phenyl, -C 1-6 -C is mono- or polysubstituted with substituents independently selected from the group consisting of alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl, and unsubstituted 5- to 14-membered heteroaryl; 1-6 -heteroalkyl.

[0105] Preferably, R 6 , R 7 , and R 8 are independent of each other, -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 , -CN, -NO 2 , -C(=O)OH, -NH 2 , -C 1-6 -Alkyl, -CF 3 , -CHF 2 , -CH 2 F, -OC 1-6 -Alkyl, -OCF 3 , -OCHF 2 , -OCH 2 F, unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -NHC 1-6 -alkyl, unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -N(C 1-6 -alkyl) 2 , unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH2 , and -C(=O)NH 2 -C(=O)OC 1-6 -alkyl, unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -OC(=O)C 1-6 -alkyl, or unsubstituted or, independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF 3 , -CHF 2 , -CH 2 F, -OCF 3 , -OCHF 2 , -OCH 2 F, S.F. 5 , -NO 2 , -C(=O)OH, -NH 2 , and -C(=O)NH 2 -C 1-6 -heteroalkyl.

[0106] In some embodiments, R 6 , R 7 , and R 8 are, independently of each other, -H, -F, -Cl, -Br, -I, -CN, C 1-3 -Alkyl, -CF 3 , -CF 2 H, and -CFH 2 , preferably -H or -F.

[0107] In some embodiments, R 6is -H, -F, -Cl, -CN, or -C 1 -C 6 - represents alkyl.

[0108] In some embodiments, R 6 is -H, -F, -Cl, -CN, or -CH 3 , preferably -H, -F, -CN, or -CH 3 represents a residue selected from the group consisting of:

[0109] In some embodiments, R 6 does not represent -H.

[0110] In some embodiments, R 7 is -H, -F, -Cl, -CN, or -C 1 -C 6 - represents alkyl.

[0111] In some embodiments, R 7 does not represent -H.

[0112] In some embodiments, R 7 is -H, -F, -Cl, -CN, or -CH 3 , preferably -H, -F, -Cl, or -CH 3 represents a residue selected from the group consisting of:

[0113] In some embodiments, R 6 , R 7 , and R 8 represent, independently of each other, -H or a residue selected from the group consisting of: [Table 14]

[0114] In some embodiments, R 8 is -H, -F, -Cl, -CN, or -C 1 -C 6 - represents alkyl.

[0115] In some embodiments, R 8 does not represent -H.

[0116] In some embodiments, R 8 is -H, -F, -Cl, -CN, or CH 3 , preferably -F.

[0117] In some embodiments, (i)R 6 , R 7 , and R 8 each represents -H, or (ii)R 6 , R 7 , and R 8 Two of the represent -H, and R 6 , R 7 , and R 8 the other is -F, -Cl, -CN, or -CH 3 represents or (iii)R 6 , R 7 , and R 8 One of the groups represents -H, and R 6 , R 7 , and R 8 the other of which is independently -F, -Cl, -CN, or -CH 3 Represents.

[0118] In some embodiments, W is Saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 12-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 10-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 8-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 6-membered cycloalkyl, wherein the cycloalkyl is unsubstituted, mono- or tri-substituted, preferably the cycloalkyl is unsubstituted, mono- or di-substituted, in particular saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered cycloalkyl, preferably saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 12-membered cycloalkyl, preferably saturated or non-aromatic unsaturated, unsubstituted, Mono- or poly-substituted 3- to 10-membered cycloalkyl, preferably saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 8-membered cycloalkyl, preferably saturated or non-aromatic unsaturated, unsubstituted, mono- or poly-substituted 3- to 6-membered cycloalkyl, wherein the cycloalkyl is unsubstituted, mono- or tri-substituted, preferably the cycloalkyl is unsubstituted, mono- or di-substituted; saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 12-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 10-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 8-membered cycloalkyl, preferably saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 6-membered cycloalkyl; An unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl, wherein the aryl is unsubstituted, mono- or tri-substituted, preferably the aryl is unsubstituted, mono- or di-substituted; an unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl; A saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 8-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 6-membered heterocycloalkyl, wherein the heterocycloalkyl is unsubstituted, mono-substituted or tri-substituted, preferably Preferably, the heterocycloalkyl is an unsubstituted, mono-substituted or di-substituted, saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 8-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 6-membered heterocycloalkyl, unsubstituted, mono- or poly-substituted 5- to 14-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 12-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 10-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 9-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 8-membered heteroaryl, wherein the heteroaryl is unsubstituted, mono- or tri-substituted, preferably the heteroaryl is unsubstituted, mono- or di-substituted; unsubstituted, mono- or poly-substituted 5- to 14-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 12-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 10-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 9-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 8-membered heteroaryl; -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, wherein the alkyl, alkenyl, or alkynyl is unsubstituted, monosubstituted, or trisubstituted, preferably the alkyl, alkenyl, or alkynyl is unsubstituted, monosubstituted, or disubstituted; 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl.

[0119] In some embodiments, W is unsubstituted, mono- or poly-substituted 3- to 14-membered saturated cycloalkyl, 5- to 14-membered cycloalkenyl, 8- to 14-membered cycloalkynyl, preferably unsubstituted, mono- or poly-substituted 3- to 12-membered saturated cycloalkyl, 5- to 12-membered cycloalkenyl, 8- to 12-membered cycloalkynyl, preferably unsubstituted, mono- or poly-substituted 3- to 10-membered saturated cycloalkyl, 5- to 10-membered cycloalkenyl, 8- to 10-membered cycloalkynyl, preferably unsubstituted, mono- or poly-substituted 3- to 8-membered saturated cycloalkyl, 5- to 8-membered cycloalkenyl, 8 ...6-membered saturated cycloalkyl, 5- to 6-membered cycloalkenyl, wherein the cycloalkyl is unsubstituted, mono- or tri-substituted, Preferably, the cycloalkyl is unsubstituted, monosubstituted or trisubstituted, and is an unsubstituted, monosubstituted or polysubstituted 3-14 membered saturated cycloalkyl, 5-14 membered cycloalkenyl, or 8-14 membered cycloalkynyl, preferably an unsubstituted, monosubstituted or polysubstituted 3-12 membered saturated cycloalkyl, 5-12 membered cycloalkenyl, or 8-12 membered cycloalkynyl, preferably an unsubstituted, monosubstituted or polysubstituted 3-10 membered saturated cycloalkyl, 5-10 membered cycloalkenyl, or 8-10 membered cycloalkynyl, preferably an unsubstituted, monosubstituted or polysubstituted 3-8 membered saturated cycloalkyl, 5-8 membered cycloalkenyl, or 8 membered cycloalkynyl, preferably an unsubstituted, monosubstituted or polysubstituted 3-6 membered saturated cycloalkyl, 5-6 membered cycloalkenyl, An unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl, wherein the aryl is unsubstituted, mono- or tri-substituted, preferably the aryl is unsubstituted, mono- or di-substituted; an unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl; A saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 8-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 6-membered heterocycloalkyl, wherein the heterocycloalkyl is unsubstituted, mono-substituted or tri-substituted, preferably Preferably, the heterocycloalkyl is an unsubstituted, mono-substituted or di-substituted, saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 8-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 6-membered heterocycloalkyl, unsubstituted, mono- or poly-substituted 5- to 14-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 12-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 10-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 9-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 8-membered heteroaryl, wherein the heteroaryl is unsubstituted, mono- or tri-substituted, preferably the heteroaryl is unsubstituted, mono- or di-substituted; unsubstituted, mono- or poly-substituted 5- to 14-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 12-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 10-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 9-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 8-membered heteroaryl; -C 1 -C6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, wherein the alkyl, alkenyl, or alkynyl is unsubstituted, monosubstituted, or trisubstituted, preferably the alkyl, alkenyl, or alkynyl is unsubstituted, monosubstituted, or disubstituted; 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl.

[0120] In some embodiments, W is A saturated, unsubstituted, mono- or poly-substituted 3- to 14-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or poly-substituted 3- to 12-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or poly-substituted 3- to 10-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or poly-substituted 3- to 8-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or poly-substituted 3- to 6-membered cycloalkyl, wherein the cycloalkyl is unsubstituted, mono- or tri-substituted, preferably Preferably, the cycloalkyl is an unsubstituted, monosubstituted or disubstituted saturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl, preferably a saturated, unsubstituted, monosubstituted or polysubstituted 3- to 12-membered cycloalkyl, preferably a saturated, unsubstituted, monosubstituted or polysubstituted 3- to 10-membered cycloalkyl, preferably a saturated, unsubstituted, monosubstituted or polysubstituted 3- to 8-membered cycloalkyl, preferably a saturated, unsubstituted, monosubstituted or polysubstituted 3- to 6-membered cycloalkyl, An unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl, wherein the aryl is unsubstituted, mono- or tri-substituted, preferably the aryl is unsubstituted, mono- or di-substituted; an unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl; A saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 8-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 6-membered heterocycloalkyl, wherein the heterocycloalkyl is unsubstituted, mono-substituted or tri-substituted, preferably Preferably, the heterocycloalkyl is an unsubstituted, mono-substituted or di-substituted, saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 8-membered heterocycloalkyl, preferably a saturated or unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 6-membered heterocycloalkyl, unsubstituted, mono- or poly-substituted 5- to 14-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 12-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 10-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 9-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 8-membered heteroaryl, wherein the heteroaryl is unsubstituted, mono- or tri-substituted, preferably the heteroaryl is unsubstituted, mono- or di-substituted; unsubstituted, mono- or poly-substituted 5- to 14-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 12-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 10-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 9-membered heteroaryl, preferably unsubstituted, mono- or poly-substituted 5- to 8-membered heteroaryl; In each case, unsubstituted, monosubstituted or disubstituted -C 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, The substituents are -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -C1-6 -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C 1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3-14 membered heterocycloalkyl, unsubstituted -phenyl, and 5-14 membered heteroaryl.

[0121] In some embodiments, W is an unsubstituted, mono- or polysubstituted 3- to 10-membered cycloalkyl, an unsubstituted, mono- or polysubstituted 6- to 12-membered aryl, a saturated or unsaturated, mono- or polysubstituted 3- to 10-membered heterocycloalkyl, a mono- or polysubstituted 5- to 12-membered heteroaryl, -C 1 -C 6 -Alkyl, haloC 1-6 Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6-alkynyl, preferably W is unsubstituted, mono- or polysubstituted 3- to 10-membered cycloalkyl, unsubstituted, mono- or polysubstituted 6- to 12-membered aryl, saturated or unsaturated, mono- or polysubstituted 3- to 10-membered heterocycloalkyl, mono- or di-substituted 5- to 12-membered heteroaryl, or, in each case, unsubstituted, mono- or di-substituted -C 1 -C 6 -Alkyl, haloC 1-6 Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl, preferably W is unsubstituted, mono- or di-substituted 3- to 10-membered cycloalkyl, unsubstituted, mono- or di-substituted 6- to 12-membered aryl, saturated or unsaturated, mono- or di-substituted 3- to 10-membered heterocycloalkyl, mono- or di-substituted 5- to 12-membered heteroaryl, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl and t-butyl, pentyl, hexyl-CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -CCl 3 , -C 1-6 -Alkylene-CCl 3 , or -C 1-6 -Alkylene-CF 3 Represents.

[0122] In some embodiments, W is represents a saturated, unsubstituted, mono- or polysubstituted 3- to 14-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 13-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 12-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 11-membered cycloalkyl, preferably a saturated, unsubstituted, mono- or polysubstituted 3- to 10-membered cycloalkyl, preferably a cycloalkyl residue selected from the group consisting of: [Table 15] It represents an unsubstituted, mono- or poly-substituted 6- to 14-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 12-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 10-membered aryl, preferably an unsubstituted, mono- or poly-substituted 6- to 8-membered aryl, preferably the following: [Table 16] or represents a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 14-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 13-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 12-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 11-membered heterocycloalkyl, preferably a saturated, unsaturated, unsubstituted, mono-substituted or poly-substituted 3- to 10-membered heterocycloalkyl, preferably the following: [Table 17-1] [Table 17-2] More preferably, selected from the group consisting of: [Table 18] a heterocycloalkyl residue selected from the group consisting of It represents an unsubstituted, mono-substituted or poly-substituted 5-14 membered heteroaryl, preferably an unsubstituted, mono-substituted or poly-substituted 5-12 membered heteroaryl, preferably an unsubstituted, mono-substituted or poly-substituted 5-10 membered heteroaryl, preferably an unsubstituted, mono-substituted or poly-substituted 5-9 membered heteroaryl, more preferably the following: [Table 19-1] [Table 19-2] and more preferably represents a residue selected from the group consisting of: [Table 20] or In each case, unsubstituted -F, -Cl, -Br, -I, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C(=O)-C 1-6 -Alkyl, -C(=O)OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC 1-6 -Alkylene-CF 3 , -OH, =O, -OC 1-6 -Alkyl, -NH 2 , -NHC 1-6 -Alkyl, -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH 2 , -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-CF 3 , -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)NH 2 , -C(=O)-NH-C 1-6 -Alkyl, -C(=O)-N(C1-6 -alkyl) 2 , -S(=O) 2 C 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 -C, mono- or polysubstituted with substituents independently selected from the group consisting of 3- to 14-membered heterocycloalkyl, unsubstituted -phenyl, and 5- to 14-membered heteroaryl; 1 -C 6 -Alkyl, -C 2 -C 6 -alkenyl, -C 2 -C 6 -alkynyl.

[0123] In some embodiments, the 5-14 membered heteroaryl within the definition of W is selected from the group consisting of unsubstituted, mono- or polysubstituted benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, noline, isothiazole, isoxazole, naphthyridine, are selected from oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole, [1,2,4]triazolo[4,3-a]pyrimidine, preferably this definition includes in each case unsubstituted, mono- or polysubstituted benzimidazole, benzisoxazole, benzodioxole, benzofuran, benzothiazole, benzothiophene. , cinnoline, dibenzofuran, furan, thiophene, furazan, imidazole, imidazopyridine, indole, isobenzofuran, isoindole, isoquinoline, isoxazole, oxadiazole, oxazole, oxindole, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinoline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, preferably this definition is selected from unsubstituted, monosubstituted aryl, ... and preferably this definition includes in each case unsubstituted, mono- or polysubstituted furan-2-yl, furan-3-yl, thiophen-2-yl, thiophen-3-yl, pyrazol-5-yl, oxazol-5-yl, isoxazol-4-yl, thiazol-2-yl, thiazol-5-yl, 1,2,4-triazol-3-yl, 1,2,3-triazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, isoquinolin-1-yl, isoquinolin-5-yl, benzo[d]thiazol-2-yl, pyridazin-3-yl, pyrimidin-5-yl, and imidazo[1,2-a]pyridin-6-yl.

[0124] In some embodiments, 3 to 14 membered heterocycloalkyl within the definition of W is, at each occurrence, selected from the group consisting of unsubstituted, mono- or polysubstituted azepane, 1,4-oxazepane, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazolidine, isothiazolidine, isoxalidine, morpholine, oxazolidine, oxepane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiacylcyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabiscylcyclohexane, 1,1-dioxothiac ... cyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolidine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine, preferably this definition includes in each case mono- or polysubstituted azepanes, azetidines, aziridines, diazepanes, dioxanes, dioxolanes, dithianes, dithianes ... oran, imidazolidine, isoxalidine, morpholine, oxazolidine, oxepane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, thiazolidine, thiolane, indoline, dihydrobenzofuran, dihydrobenzothiophene, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, hexahydro-1H-pyrrolidine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine, preferably this definition also includes in each case mono- or polysubstituted azepanes, azetidines, aziridines, diazepanes, dioxanes, dioxolanes, dithiolanes, imidazolidines, isoxalidines, morpholines, oxazolidines, oxepanes, oxetanes, oxiranes, piperazines, piperidines, pyrazolidines, pyrrolidines, tetrahydrofurans, thiazolidines, thiolanes, indolines, dihydrides, Preferably, this definition is selected from mono- or polysubstituted azetidine, dioxane, imidazolidine, isoxalidine, morpholine, oxazolidine, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidin-1-yl, pyrrolidin-2-yl, tetrahydrofuran-1-yl, tetrahydrofuran-2-yl, tetrahydropyran-1-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, thiazolidine, thiolane and indoline.

[0125] In some embodiments, the 5-14 membered heteroaryl within the definition of W represents a residue according to general formula (E): [ka] During the ceremony, Y E1 -N=, -NR E2 -, S, O, or -CR E3 = Y E2 -N=, -NR E3 -, S, O, or -CR E4 = Y E3 -N=, -NR E4 -, S, O, or -CR E5 = represents Y E1 , Y E2 , and Y E3 At least one of the following is -CR E3 =, -CRE4 = and -CR E5 In another preferred embodiment, W represents a residue according to the general formula (E): In the formula, YE1 represents -N=, -NRE2-, S, or -CRE3=, YE2 represents -N=, -NRE3-, S, or -CRE4=, and YE3 represents -N=, -NRE4-, S, or -CRE5=, provided that at least one of YE1, YE2, and YE3 is not -CRE3=, -CRE4=, or -CRE5=, respectively. R E1 , R E2 , R E3 , and R E4 are, independently of each other, -H, -CH 3 , -CH 2 -Cyclopropyl, -CH 2 CF 3 , -CH 2 CHF 2 , or -CF 3 More specifically, R E1 , R E2 , R E3 , and R E4 are, independently of each other, -H, -CH 3 , or -CF 3 Preferably, R E1 , R E2 , R E3 , and R E4 represents a residue that is not -H.

[0126] In some embodiments, the 5-14 membered heteroaryl within the definition of W represents a residue according to the general formula (F'): [ka] During the ceremony, Y F1 -N= or -CR F4 = Y F2 -N= or -CR F5 = Y F3 -N= or -CR F3 = represents Y F1and Y F2 At least one of the following is -CR F4 = and -CR F5 Provided that it is not = R F1 , R F2 , R F3 , R F4 , and R F5 are, independently of each other, -H, -CH 3 , -CF 3 , -OH, -OCH 3 , -OCH 2 CH 3 , -Cl, or -azetidinyl, but preferably R F1 , R F2 , R F3 , R F4 , and R F5 represents a residue that is not -H.

[0127] In some embodiments, the 5-14 membered heteroaryl within the definition of W represents a residue according to the general formula (F): [ka] During the ceremony, Y F1 -N= or -CR F4 = Y F2 -N= or -CR F5 = represents Y F1 and Y F2 At least one of the following is -CR F4 = and -CR F5 Provided that it is not = R F1 , R F2 , R F3 , R F4 , and R F5 are, independently of each other, -H, -CH 3 , -CF 3 , -OH, -OCH 3 , -OCH 2 CH 3 , -Cl, or -azetidinyl, but preferably R F1 , R F2, R F3 , R F4 , and R F5 represents a residue that is not -H.

[0128] In some embodiments, the 5-14 membered heteroaryl within the definition of W represents a residue according to general formula (G) or (H): [ka] In the formula, R G1 and R H1 -H, -CH 3 , -CF 3 , -OH, -OCH 3 , -OCH 2 CH 3 , -Cl, azetidinyl, -cyclopropyl, -O-cyclopropyl, and -CHF 2 or R G1 and R H1 -H, -CH 3 , -CF 3 , -OH, -OCH 3 , -OCH 2 CH 3 , -Cl, and azetidinyl.

[0129] In some embodiments, the 5-14 membered heteroaryl within the definition of W represents a residue according to general formula (G') or (H'): [ka] In the formula, R G1 and R H1 -H, -CH 3 , -CF 3 , -OH, -OCH 3 , -OCH 2 CH 3 , -Cl, azetidinyl, -cyclopropyl, -O-cyclopropyl, and -CHF 2 or R G1 and R H1 -H, -CH 3 , -CF 3, -OH, -OCH 3 , -OCH 2 CH 3 , -Cl, and azetidinyl.

[0130] In some embodiments, the 5-14 membered heteroaryl within the definition of W represents a residue according to general formula (E), (F), (F'), (G), (H), (G'), or (H') as defined herein above.

[0131] In some embodiments, the term “mono- or poly-substituted” refers, at each occurrence, independently to —F, —Cl, —Br, —I, —CN, —C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -C 1-6 -Alkylene-C(=O)-NH 2 , -C(=O)-NH(C1-6 -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-6 -Alkyl, -C 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-OC 1-6 -Alkyl, -OC 1-6 -Alkylene-NH 2 , -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 -NH 2 , -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 , -NH 2 , -NO, -NO 2 , -C 1-6 -Alkylene-NH 2 , -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)-NH 2 , -C 1-6 -Alkylene-NH-C(=O)-NH 2 , -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)-NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-NH 2 , -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) 2 OH, -C 1-6 -Alkylene-NH-S(=O) 2 OH, -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 -NH 2 , -C 1-6 -Alkylene-NH-S(=O)2 -NH 2 , -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) 2 N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-NH-S(=O) 2 N(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 -NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -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, -SF 5 , -SCF 3 , -SCF 2 H, -SCFH 2 , -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 -NH 2 , -C 1-6 -Alkylene-S(=O) 2 -NH 2 , -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- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-14 membered heteroaryl, -C 1-6 -Alkylene-(5-14 membered heteroaryl), -O-(3-14 membered cycloalkyl), -O-(3-14 membered heterocycloalkyl), -O-phenyl, -O-(5-14 membered heteroaryl), -C(=O)-(3-14 membered cycloalkyl), -C(=O)-(3-14 membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5-14 membered heteroaryl), -S(=O) 2 -(3 to 14 membered cycloalkyl), -S(=O) 2 -(3-14 membered heterocycloalkyl), -S(=O) 2 -phenyl, or -S(=O) 2 -(5- to 14-membered heteroaryl), preferably this term means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Arki Ren-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -C 1-6 -Alkylene-C(=O)-NH 2 , -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -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), -NH 2 , -NO, -NO 2 , -C 1-6 -Alkylene-NH 2 , -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)-OC1-6 -Alkyl, -C 1-6 -Alkylene-NH-C(=O)-OC 1-6 -Alkyl, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -Alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -Alkyl, -N(C 1-6 -alkyl)-C(=O)-NH 2 , -NH-S(=O) 2 OH, -C 1-6 -Alkylene-NH-S(=O) 2 OH, -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(C1-6 -alkyl)-S(=O) 2 -OC 1-6 -Alkyl, -N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -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, -SF 5 , -SCF 3 , -SCF 2 H, -SCFH 2 , -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 -NH 2 , -C 1-6-Alkylene-S(=O) 2 -NH 2 , -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- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-14 membered heteroaryl, -C 1-6 -Alkylene-(5-14 membered heteroaryl), -O-(3-14 membered cycloalkyl), -O-(3-14 membered heterocycloalkyl), -O-phenyl, -O-(5-14 membered heteroaryl), -S(=O) 2 -(3 to 14 membered cycloalkyl), -S(=O) 2 -(3-14 membered heterocycloalkyl), -S(=O) 2 -phenyl, or -S(=O) 2 -(5- to 14-membered heteroaryl), preferably this term means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6-Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -C 1-6 -Alkylene-C(=O)-NH 2 , -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -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), -NH 2 , -NO, -NO 2 , -C 1-6 -Alkylene-NH 2 , -NH(C 1-6 -alkyl), -C 1-6 -Alkylene-NH(C 1-6-alkyl), -N(C 1-6 -alkyl) 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl) 2 , -NH-C(=O)-C 1-6 -Alkyl, -C 1-6 -Alkylene-NH-C(=O)-C 1-6 -Alkyl, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -OH, -N(C 1-6 -alkyl)-S(=O) 2 -C 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -C 1-6 -Alkyl, -N(C 1-6 -alkyl)-S(=O) 2 -OC 1-6 -Alkyl, -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -OC 1-6 -Alkyl, -N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-S(=O) 2 -NH 2 , -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 -NH 2 , -C 1-6 -Alkylene-S(=O) 2 -NH 2 , -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- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-14 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-14 membered heteroaryl, -C1-6 -Alkylene-(5-14 membered heteroaryl), -O-(3-14 membered cycloalkyl), -O-(3-14 membered heterocycloalkyl), -O-phenyl, -S(=O) 2 -(3 to 14 membered cycloalkyl), -S(=O) 2 -(3-14 membered heterocycloalkyl), -S(=O) 2 -phenyl, or -S(=O) 2 -(5- to 14-membered heteroaryl), preferably this term means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF 3 , -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-CF 3 , -C(=O)-NH 2 , -C 1-6 -Alkylene-C(=O)-NH 2 , -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -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), -NH 2 , -NO 2 , -C 1-6 -Alkylene-NH 2 , -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-SC1-6 -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 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3 to 12 membered cycloalkyl, -C 1-6 -Alkylene-(3- to 12-membered cycloalkyl), 3- to 12-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-12 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-12 membered heteroaryl, -C 1-6 -alkylene-(5- to 12-membered heteroaryl), preferably this term means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-6 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -Alkylene-CF 2 H, -C 1-6 -Alkylene-CFH 2 , -C 1-6 -Alkylene-NH-C 1-6 -Alkylene-CF 3 , -C(=O)OH, -C 1-6 -Alkylene-C(=O)-OH, -C(=O)-OC 1-6 -Alkyl, -C(=O)OC1-6 -Alkylene-CF 3 , -C(=O)-NH 2 , -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, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-6 -Alkyl, -OC(=O)-C 1-6 -Alkyl, -OC(=O)-NH(C 1-6 -alkyl), -NH 2 , -NO 2 , -C 1-6 -Alkylene-NH 2 , -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 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O)2 -N(C 1-6 -alkyl) 2 , 3 to 12 membered cycloalkyl, -C 1-6 -Alkylene-(3- to 12-membered cycloalkyl), 3- to 12-membered heterocycloalkyl, -C 1-6 -Alkylene-(3-12 membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5-12 membered heteroaryl, -C 1-6 -alkylene-(5- to 12-membered heteroaryl), preferably this term means, at each occurrence, independently, -F, -Cl, -Br, -I, -CN, -C 1-5 -Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-5 -Alkylene-CF 3 , -C 1-5 -Alkylene-NH-C 1-5 -Alkylene-CF 3 , -C(=O)OH, -C 1-5 -Alkylene-C(=O)-OH, -C(=O)-OC 1-5 -Alkyl, -C(=O)-NH 2 , -C(=O)-NH(C 1-5 -alkyl), C(=O)-N(C 1-5 -alkyl) 2 , -OH, -C 1-5 -Alkylene-OH, =O, -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-5 -Alkyl, -OC(=O)-C 1-5 -Alkyl, -OC(=O)-NH(C 1-6 -alkyl), -NH 2 , -NO 2 , -C 1-5 -Alkylene-NH 2 , -NH(C 1-5-alkyl), -C 1-5 -Alkylene-NH(C 1-5 -alkyl), -N(C 1-5 -alkyl) 2 , -C 1-5 -Alkylene-N(C 1-5 -alkyl) 2 , -N(C 1-5 -alkyl)-S(=O) 2 -C 1-5 -Alkyl, -N(C 1-5 -alkyl)-S(=O) 2 -OC 1-5 -Alkyl, -SH, -SC 1-5 Alkyl, -S(=O) 2 -C 1-5 Alkyl, -S(=O) 2 -OH, -S(=O) 2 -OC 1-6 -Alkyl, -S(=O) 2 -NH 2 , -S(=O) 2 -NH(C 1-6 -alkyl), -S(=O) 2 -N(C 1-6 -alkyl) 2 , 3 to 10 membered cycloalkyl, -C 1-5 -alkylene-(3- to 10-membered cycloalkyl), 3- to 10-membered heterocycloalkyl, -C 1-5 -Alkylene-(3 to 10 membered heterocycloalkyl), -phenyl, -C 1-5 -alkylene-phenyl, 5-10 membered heteroaryl, -C 1-5 -alkylene-(5-10 membered heteroaryl) is substituted with one or more substituents independently selected from the group consisting of aryl, aryl, aryl and heteroaryl.

[0132] In some embodiments, the 3- to 14-membered cycloalkyl within the definition of W is unsubstituted, —F, —Cl, —Br, —I, —CN, C 1-3- Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-3 -Alkylene-CF3 , -C 1-3 -Alkylene-CF 2 H, -C 1-3 -Alkylene-CFH 2 , -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-3 -Alkyl, -C 1-3 -Alkylene-OC 1-3 -alkyl, and -C 1-3 -Alkylene-OH, preferably -F, -Cl, -Br, -I, -CN, -CH 3 , -CF 3 , -CF 2 H, -CFH 2 , -OCF 3 , and -OCH 3 - or disubstituted with a substituent selected from the group consisting of:

[0133] In some embodiments, the 6-14 membered aryl within the definition of W is unsubstituted, -F, -Cl, -Br, -I, -CN, C 1-3- Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-3 -Alkylene-CF 3 , -C 1-3 -Alkylene-CF 2 H, -C 1-3 -Alkylene-CFH 2 , -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-3 -Alkyl, -C 1-3 -Alkylene-OC 1-3 -alkyl, and -C 1-3 -Alkylene-OH, preferably -F, -Cl, -Br, -I, -CN, -CH 3 , -CF3 , -CF 2 H, -CFH 2 , -OCF 3 , and -OCH 3 - or disubstituted with a substituent selected from the group consisting of:

[0134] In some embodiments, the 5-14 membered heteroaryl within the definition of W is unsubstituted, -F, -Cl, -Br, -I, -CN, C 1-3- Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-3 -Alkylene-CF 3 , -C 1-3 -Alkylene-CF 2 H, -C 1-3 -Alkylene-CFH 2 , -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-3 -Alkyl, -C 1-3 -Alkylene-OC 1-3 -alkyl, and -C 1-3 -Alkylene-OH, preferably -F, -Cl, -Br, -I, -CN, -CH 3 , -CF 3 , -CF 2 H, -CFH 2 , -OCF 3 , and -OCH 3 - or disubstituted with a substituent selected from the group consisting of:

[0135] In some embodiments, within the definition of W, 1 -C 6 -Alkyl is unsubstituted, -F, -Cl, -Br, -I, -CN, C 1-3- Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl2 , -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-3 -Alkyl and -OH, preferably -F, -Cl, -Br, -I, -CN, -CH 3 , -CF 3 , -CF 2 H, -CFH 2 , -OCF 3 , and -OCH 3 - or disubstituted with a substituent selected from the group consisting of:

[0136] In some embodiments, the 3- to 14-membered heterocycloalkyl within the definition of W is unsubstituted, —F, —Cl, —Br, —I, —CN, C 1-3- Alkyl, -CF 3 , -CF 2 H, -CFH 2 , -CF 2 Cl, -CFCl 2 , -C 1-3 -Alkylene-CF 3 , -C 1-3 -Alkylene-CF 2 H, -C 1-3 -Alkylene-CFH 2 , -OCF 3 , -OCF 2 H, -OCFH 2 , -OCF 2 Cl, -OCFCl 2 , -OC 1-3 -Alkyl, -C 1-3 -Alkylene-OC 1-3 -alkyl, and -C 1-3 -Alkylene-OH, preferably -F, -Cl, -Br, -I, -CN, -CH 3 , -CF 3 , -CF 2 H, -CFH 2 , -OCF 3 , and -OCH 3 - or disubstituted with a substituent selected from the group consisting of:

[0137] In some embodiments of the invention, the compound is selected from the group consisting of: Compound 001-(2R)-2-{[5-(benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamide}propanamide, Compound 00 2-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 003-(2R)-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 004-(2R)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 005-(2R)-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 006-(2R)-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 007-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide, Compound 008-(2S)-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 009-(2S)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 010-(2S)-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 011-(2S)-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 01 2-(2S)-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 013-5-(benzyloxy)-2-(difluoromethyl)-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide, Compound 014-5-(benzyloxy)-2-(difluoromethyl)-N-(2-hydroxy-2-methylpropyl)-1-benzothiophene-3-carboxamide, Compound 015-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-4-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 016-(2S)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 017-(2R)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 018-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 019-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 020-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amide}oxolane-3-carboxamide, Compound 021-4-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amide}oxane-4-carboxamide, Compound 022-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 023-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 024-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 025-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 026-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 027-(2S)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide, Compound 028-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 029-(2R)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide, Compound 030-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 031-2-methyl-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 032-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 033-4-{2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amide}oxane-4-carboxamide, Compound 034-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 035-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 036-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 037-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 038-3-{2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 039-N-(3,3-difluorocyclobutyl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 040-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide, Compound 041-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(2-oxopyrrolidin-3-yl)-1-benzothiophene-3-carboxamide, Compound 042-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 043-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide, Compound 044-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide, Compound 045-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 046-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[(5-oxopyrrolidin-2-yl)methyl]-1-benzothiophene-3-carboxamide, Compound 047-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 048-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-1-benzothiophene-3-carboxamide, Compound 049-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxylic acid, Compound 050-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamide}-3-hydroxypropanamide, Compound 051-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-3-hydroxypropanamide, Compound 05 2-(2S)-3-hydroxy-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 05 3-(2S)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 054-(2S)-3-hydroxy-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 055-5-[(2-fluorophenyl)methoxy]-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 056-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-3-hydroxypropanamide, Compound 057-(2R)-3-hydroxy-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamido)propanamide, Compound 058-(2R)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 059-5-[(2-fluorophenyl)methoxy]-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidin-3-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 060-5-(benzyloxy)-2-methyl-N-[(3S)-2-oxopyrrolidin-3-yl]-1-benzothiophene-3-carboxamide, Compound 061-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamide}-2-methylpropanamide, Compound 062-2-{[5-(benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamide}-2-methylpropanamide, Compound 063-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-2-methylpropanamide, Compound 064-2-methyl-2-({2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 065-2-methyl-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 066-2-({5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-2-methylpropanamide, Compound 067-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxan-4-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 068-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxetan-3-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 069-5-(cyclopropylmethoxy)-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-1-benzothiophene-3-carboxamide, Compound 070-4-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-amide}oxane-4-carboxamide, Compound 071-4-{2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-amide}oxane-4-carboxamide, Compound 072-4-{5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-amide}oxane-4-carboxylic acid, Compound 073-5-(benzyloxy)-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 074-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 075-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 076-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 077-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 078-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 079-N-[1-(hydroxymethyl)cyclobutyl]-5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 080-5-(benzyloxy)-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 081-5-[(2-fluorophenyl)methoxy]-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 082-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 083-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 084-N-[4-(hydroxymethyl)oxan-4-yl]-5-[(2-hydroxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 085-5-[(2-fluorophenyl)methoxy]-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 086-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 087-3-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 088-3-{2-methyl-5-[(pyridin-2-yl)methoxy]-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 089-5-(benzyloxy)-N-(3,3-difluorocyclobutyl)-2-methyl-1-benzothiophene-3-carboxamide, Compound 090-N-(3,3-difluorocyclobutyl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 091-5-(benzyloxy)-2-methyl-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide, Compound 092-2-methyl-N-(1-methyl-1H-pyrazol-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 093-5-[(2-fluorophenyl)methoxy]-2-methyl-N-(2-oxopyrrolidin-3-yl)-1-benzothiophene-3-carboxamide, Compound 094-2-methyl-N-(2-oxopyrrolidin-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 095-En1-N-(3,3-difluoropiperidin-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 095-En2-N-(3,3-difluoropiperidin-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 096-5-(benzyloxy)-2-methyl-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide, Compound 097-2-methyl-N-(oxolan-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 098-5-(benzyloxy)-2-methyl-N-[2-methyl-2-(morpholin-4-yl)propyl]-1-benzothiophene-3-carboxamide, Compound 099-2-methyl-N-[2-methyl-2-(morpholin-4-yl)propyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 100-5-(benzyloxy)-N-(2-hydroxy-2-methylpropyl)-2-methyl-1-benzothiophene-3-carboxamide, Compound 101-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 102-5-(benzyloxy)-2-methyl-N-[(5-oxopyrrolidin-2-yl)methyl]-1-benzothiophene-3-carboxamide, Compound 103-2-methyl-N-[(5-oxopyrrolidin-2-yl)methyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 104-5-(benzyloxy)-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 105-N-[(6-hydroxypyridin-2-yl)methyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 106-5-(benzyloxy)-2-methyl-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-1-benzothiophene-3-carboxamide, Compound 107-2-methyl-N-[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 108-5-(benzyloxy)-2-methyl-1-benzothiophene-3-carboxylic acid, Compound 109-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxylic acid, Compound 110-ethyl 5-methoxy-2-methyl-1-benzothiophene-3-carboxylate, Compound 111-5-(benzyloxy)-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-1-benzothiophene-3-carboxamide, Compound 112-5-(benzyloxy)-2-(difluoromethyl)-N-{[1-(dimethylamino)cyclopentyl]methyl}-1-benzothiophene-3-carboxamide, Compound 113-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 114-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 115-5-(benzyloxy)-N-[2-(dimethylamino)ethyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 116-5-(benzyloxy)-2-(difluoromethyl)-N-[2-(dimethylamino)ethyl]-1-benzothiophene-3-carboxamide, Compound 117-N-[2-(dimethylamino)ethyl]-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 118-N-[2-(dimethylamino)ethyl]-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 119-5-(benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-(difluoromethyl)-1-benzothiophene-3-carboxamide, Compound 120-5-(benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-1-benzothiophene-3-carboxamide, Compound 121-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 122-N-(4,4-difluoro-1-methylpyrrolidin-3-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 123-5-(benzyloxy)-2-methyl-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide, Compound 124-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide, Compound 125-2-methyl-N-(1-methylpyrrolidin-3-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 126-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methylpyrrolidin-3-yl)-1-benzothiophene-3-carboxamide, Compound 127-5-(benzyloxy)-2-methyl-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide, Compound 128-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide, Compound 129-2-methyl-N-(1-methylpiperidin-4-yl)-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 130-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(1-methylpiperidin-4-yl)-1-benzothiophene-3-carboxamide, Compound 131-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methyl-1H-pyrazol-3-yl)-1-benzothiophene-3-carboxamide, Compound 13 2-3-hydroxy-N,2-dimethyl-2-({2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 13 3-N-methyl-3-{2-methyl-5-[(2-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-amide}oxolane-3-carboxamide, Compound 134-5-(benzyloxy)-N,2-dimethyl-1-benzothiophene-3-carboxamide, Compound 135-5-(benzyloxy)-2-(difluoromethyl)-N-methyl-1-benzothiophene-3-carboxamide, Compound 136-N,2-dimethyl-5-{[2-(trifluoromethyl)pyridin-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 137-N,2-dimethyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 138-(2S)-2-({5-[(2-methoxypyridin-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamido)propanamide, Compound 13 9-(2S)-3-hydroxy-2-({5-[(2-methoxypyridin-3-yl)methoxy]-2-...

Claims

1. Equation (I): 【Chemistry 1】 [During the ceremony, R １ is selected from -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) ２ R Ｗ , -C(=O)R Ｗ , -C(=O)OR Ｗ , or -C(=O)NR Ｗ R Ｘ and represents Q is -OR ２ or -NR ３ R ４ This represents, R ２ is, -R Ｙ５ This represents, R ３ is -OH or -R Ｙ１ This represents, R ４ is, -R Ｙ２ or -S (=O) ２ R Ｙ３ This represents, Alternatively, R ３ and R ４ Together, they form a saturated or unsaturated, unsubstituted, or monosubstituted or polysubstituted 4, 5, 6, 7, or 8-membered heterocycle containing 1 to 3 heteroatoms selected from N, O, and S. T represents -O-, and U represents -(CR ５ R ５ ') ｎ - represents, or T is - (CR ５ R ５ ') ｎ - represents, and U represents -O-, n is an integer selected from 1, 2, 3, 4, or 5. R ５ and R ５ ' are independent of each other, -R Ｙ４ This represents, R ６ , R ７ , and R ８ These are -F, -Cl, -Br, -I, -CN, and -NO, which are independent of each other. ２ , -SF ５ , -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) ２ R Ｗ , -C(=O)R Ｗ , -C (=O) OR Ｗ , or -C(=O)NR Ｗ R Ｘ This represents, W is Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups, Unsubstituted, monosubstituted or polysubstituted 6- to 14-membered aryl compounds, Saturated or unsaturated, monosubstituted or polysubstituted 3- to 14-membered heterocycloalkyl groups, Monosubstituted or polysubstituted 5- to 14-membered heteroaryls, In each case, non-substitutive, mono-substitutive or multi-substitutive, -C １ -C ６ -Alkyl, -C ２ -C ６ -Alkenyl, -C ２ -C ６ - Represents Alkinnil, Here, R Ｗ and R Ｘ They are independent of each other, in each case, independently, -H, Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C １ -C ６ - Alkyl, Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C １ -C ６ - Heteroalkyl, A saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl, wherein the 3- to 14-membered cycloalkyl is -C １ -C ６ -Alkylene- or -C １ -C ６ -Heteroalkylene- is optionally connected, in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 3- to 14-membered cycloalkyl, or A saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C １ -C ６ -Alkylene- or -C １ -C ６ The heteroalkylene is optionally connected through a heteroalkylene, and in each case represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 3 to 14-membered heterocycloalkyl group. R Ｙ１ , R Ｙ２ , R Ｙ３ , R Ｙ４ , and R Ｙ５ They are independent of each other, in each case, independently, -H, Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C １ -C ６ - Alkyl, Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C １ -C ６ - Heteroalkyl, A saturated or unsaturated, unsubstituted, mono-substituted or multi-substituted 3- to 14-member cycloalkyl, wherein the 3- to 14-member cycloalkyl is -C １ -C ６ -alkylene- or -C １ -C ６ -heteroalkylene- optionally connected through, and in each case, a saturated or unsaturated, unsubstituted, mono-substituted or multi-substituted 3- to 14-member cycloalkyl, A saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocycloalkyl, wherein the 3- to 14-membered heterocycloalkyl is -C １ -C ６ -Alkylene- or -C １ -C ６ -Heteroalkylene- is optionally connected, and in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 3 to 14-membered heterocycloalkyl, Unsubstituted, mono-substituted or multi-substituted 6- to 14-member aryl, wherein the 6- to 14-member aryl is -C １ -C ６ -alkylene- or -C １ -C ６ -heteroalkylene- optionally connected through, and in each case, saturated or unsaturated, unsubstituted, mono-substituted or multi-substituted, 6- to 14-member aryl, or Unsubstituted, monosubstituted, or polysubstituted 5- to 14-membered heteroaryls, wherein the 5- to 14-membered heteroaryl is -C １ -C ６ -Alkylene- or -C １ -C ６ The heteroalkylene is optionally connected through a heteroalkylene, and in each case represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 5 to 14-membered heteroaryl. "Single substitution or multiple substitution" in each case independently refers to -F, -Cl, -Br, -I, -CN, and -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C １－６ -Alkilen-CF ２ H, -C １－６ -Alkilen-CFH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-N(C) １－６ -Alkyl)-C １－６ -Alkilen-CF ３ , -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)O-C １－６ -Alkilen-CF ３ , -C(=O)-NH ２ , -C １－６ -Alkylene-C(=O)-NH ２ , -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,-OCF ３ , -OCF ２ H, -OCFH ２ , -OCF ２ Cl, -OCFCl ２ , -O-C １－６ -Alkyl, -C １－６ -Alkylene-O-C １－６ -alkyl, -O-C １－６ -Alkylene-O-C １－６ -alkyl, -O-C １－６ -Alkilen-NH ２ , -O-C １－６ - Alkilen-NH-C １－６ -alkyl, -O-C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -OC(=O)-C １－６ -Alkyl, -C １－６ -Alkylene-O-C(=O)-C １－６ -Alkyl, -O-C (=O)-O-C １－６ -Alkyl, -C １－６ -Alkylene-O-C(=O)-O-C １－６ -alkyl, -O-C(=O)-NH(C １－６ -Alkyl), -C １－６ -Alkylene-O-C(=O)-NH(C) １－６ -alkyl), -O-C(=O)-N(C １－６ -Alkyl) ２ , -C １－６ -Alkylene-O-C(=O)-N(C) １－６ -Alkyl) ２ , -O-S (=O) ２ -NH ２ , -C １－６ -Alkilen-O-S (=O) ２ -NH ２ , -O-S (=O) ２ -NH(C) １－６ -Alkyl), -C １－６ -Alkilen-O-S (=O) ２ -NH(C) １－６ -alkyl), -O-S (=O) ２ -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-O-S (=O) ２ -N(C) １－６ -Alkyl) ２ , -NH ２ , -NO, -NO ２ , -C １－６ -Alkilen-NH ２ ,-NH(C １－６ -Alkyl), -C １－６ -Alkilen-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 -Alkilen-NH-C(=O)-C １－６ -Alkyl, -NH-C(=O)-O-C １－６ -Alkyl, -C １－６ -Alkilen-NH-C(=O)-O-C １－６ -alkyl, -NH-C(=O)-NH ２ , -C １－６ -Alkilen-NH-C(=O)-NH ２ , -NH-C(=O)-NH(C １－６ -Alkyl), -C １－６ -Alkilen-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)-O-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl)-C(=O)-O-C １－６ -alkyl, -N(C) １－６ -alkyl)-C(=O)-NH ２ , -C １－６ -Alkylene-N(C) １－６ -alkyl)-C(=O)-NH ２ , -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) ２ OH, -C １－６ -Alkilen-NH-S(=O) ２ OH, -NH-S (=O) ２ -C １－６ -Alkyl, -C １－６ -Alkilen-NH-S(=O) ２ -C １－６ -alkyl, -NH-S (=O) ２ -O-C １－６ -Alkyl, -C １－６ -Alkilen-NH-S(=O) ２ -O-C １－６ -alkyl, -NH-S (=O) ２ -NH ２ , -C １－６ -Alkilen-NH-S(=O) ２ -NH ２ , -NH-S (=O) ２ -NH(C) １－６ -Alkyl), -C １－６ -Alkilen-NH-S(=O) ２ -NH(C) １－６ -alkyl), -NH-S (=O) ２ N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH-S(=O) ２ N(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 -O-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -alkyl)-S(=O) ２ -O-C １－６ -alkyl, -N(C) １－６ -alkyl)-S(=O) ２ -NH ２ , -C １－６ -Alkylene-N(C) １－６ -alkyl)-S(=O) ２ -NH ２ , -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, -SF ５ , -SCF ３ , -SCF ２ H, -SCFH ２ , -S-C １－６ -Alkyl, -C １－６ -Alkilen-S-C 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 -Alkilen-S (=O) ２ -C １－６ -alkyl, -S (=O) ２ -OH, -C １－６ -Alkilen-S (=O) ２ -OH, -S (=O) ２ -O-C １－６ -Alkyl, -C １－６ -Alkilen-S (=O) ２ -O-C １－６ -alkyl, -S (=O) ２ -NH ２ , -C １－６ -Alkilen-S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -Alkyl), -C １－６ -Alkilen-S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-S (=O) ２ -N(C) １－６ -Alkyl) ２ , 3-14 member cycloalkyl, -C １－６ -Alkylene-(3-14 member cycloalkyl), 3-14 member heterocycloalkyl, -C １－６ -Alkylene-(3-14 member heterocycloalkyl), -phenyl, -C １－６ -alkylene-phenyl, 5-14 member heteroaryl, -C １－６ -alkylene-(5-14 member heteroaryl), -O-(3-14 member cycloalkyl), -O-(3-14 member heterocycloalkyl), -O-phenyl, -O-(5-14 member heteroaryl), -C(=O)-(3-14 member cycloalkyl), -C(=O)-(3-14 member heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5-14 member heteroaryl), -S(=O) ２ - (3-14 member cycloalkyl), -S (=O) ２ - (3-14 member heterocycloalkyl), -S (=O) ２ -phenyl, or -S (=O) ２ [This means that the molecule is substituted with one or more substituents independently selected from (5- to 14-membered heteroaryl groups)] Compounds of, or their stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs, The compound is not 5-benzyloxybenzo[b]thiophene-3-carboxylic acid. The compound of formula (I), or its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs.

2. Q is -NR ３ R ４ The compound described in claim 1 or its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs.

3. T represents -O-, and U represents -(CR ５ R ５ ') ｎ A compound according to claim 1 or its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs that represent -.

4. R ３ However, -H, -OH, -C １－６ -Alkyl, -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkilen-NH ２ , -C １－６ -Alkilen-NH(C) １－６ -Alkyl), -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C １－６ -Alkilen-CF ２ H, -C １－６ -Alkilen-CFH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , or -C １－６ -Alkylene-N(C) １－６ -Alkyl)-C １－６ -Alkilen-CF ３ The compound described in claim 1 or its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs.

5. R ４ but, -H, Saturated, unsubstituted, monosubstituted, or polysubstituted -S (=O) ２ C １－６ - Alkyl, Saturated, monosubstituted or polysubstituted -S (=O) ２ (3-14 member cycloalkyl), Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C １ -C ６ - Alkyl, Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C １ -C ６ - Heteroalkyl, A saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl group, wherein the 3- to 14-membered cycloalkyl group is -C １ -C ６ -Alkylene- or -C １ -C ６ - Heteroalkylene - is optionally connected, and in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 3 to 14-membered cycloalkyl, A saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocycloalkyl group, wherein the 3- to 14-membered heterocycloalkyl group is -C １ -C ６ -Alkylene- or -C １ -C ６ -Heteroalkylene- is optionally connected, and in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 3 to 14-membered heterocycloalkyl, Unsubstituted, monosubstituted, or polysubstituted -C １ -C ６ -Alkylene-phenyl, Unsubstituted, monosubstituted or polysubstituted -phenyl, or Unsubstituted, monosubstituted, or polysubstituted 5- to 14-membered heteroaryls, wherein the 5- to 14-membered heteroaryl is -C １ -C ６ -Alkylene- or -C １ -C ６ The compound according to claim 1 or its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs, optionally linked through a heteroalkylene, in each case representing a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 5- to 14-membered heteroaryl.

6. R ４ but, -H, Saturated, unsubstituted, monosubstituted or polysubstituted -S (=O) with -F ２ C １－６ - Alkyl, Saturated, unsubstituted -S (=O) ２ (3-14 member cycloalkyl), Saturated, unsubstituted, -F, -Cl, -Br, -I, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , a substituent independently selected from the group consisting of 3-14 membered cycloalkyl, unsubstituted -phenyl, oxetanyl, or pyrimidinyl, monosubstituted or polysubstituted, -C １－６ - Alkyl, 3-14 member cycloalkyl or -C １－６ -Alkylene- (3-14 member cycloalkyl), -C １－６ -Alkylene- is unsubstituted, or monosubstituted or polysubstituted with -F, -Cl, -Br, -I, -OH, and the 3- to 14-membered cycloalkyl group is saturated, unsubstituted, -F, -Cl, -Br, -I, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , a substituent independently selected from the group consisting of 3-14 member cycloalkyls, unsubstituted -phenyl, oxetanyl, or pyrimidinyl, which is monosubstituted or disubstituted, 3-14 member cycloalkyl or -C １－６ -Alkylene- (3-14 member cycloalkyl), 3-14 member heterocycloalkyl or -C １－６ -Alkylene- (3-14 member heterocycloalkyl), -C １－６ -Alkylene- is unsubstituted, or monosubstituted or polysubstituted with -F, -Cl, -Br, -I, -OH, and the 3- to 14-membered heterocycloalkyl is, in each case, azetane, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole Selected from 1,1-dioxotiacyclohexane, octahydropyrrolo[1,2-a]pyrazine, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolidine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, and 1,1-dioxotiacyclohexane, in each case unsubstituted, -F, -Cl, -Br, -I, -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , a substituent independently selected from the group consisting of 3-14 member heterocycloalkyls, unsubstituted -phenyls, and 5-14 member heteroaryls, which is monosubstituted or polysubstituted, 3-14 member heterocycloalkyls or -C １－６ -Alkylene- (3-14 member heterocycloalkyl), 5-14 member heteroaryl or -C １－６ -Alkilen- (5-14 member heteroaryl), -C １－６ -Alkylene- is unsubstituted or monosubstituted with -F, -Cl, -Br, -I, -OH, and the 5-14 member heteroaryl is selected in each case from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine, and in each case is unsubstituted, -F, -Cl, -Br, -I, -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , a substituent independently selected from the group consisting of 3-14 member cycloalkyl, 3-14 member heterocycloalkyl, unsubstituted -phenyl, and 5-14 member heteroaryl, which is monosubstituted or disubstituted, a 5-14 member heteroaryl or -C １－６ A compound according to claim 1, or a stereoisomer, physiologically acceptable salt, solvate, and / or polymorph thereof, representing an alkylene (5-14 member heteroaryl).

7. W is Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , 3-14 member cycloalkyl, 3-14 member heterocycloalkyl, unsubstituted -phenyl, 5-14 member heteroaryl, monosubstituted or polysubstituted 3-14 member cycloalkyl, Unsubstituted -F, -Cl, -Br, -I, -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , monosubstituted or polysubstituted 6-14 member aryls independently selected from 3-14 member cycloalkyls, 3-14 member heterocycloalkyls, unsubstituted -phenyls, and 5-14 member heteroaryls, Saturated or unsaturated, unsubstituted, -F, -Cl, -Br, -I, -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , monosubstituted or polysubstituted 3-14 member heterocycloalkyls independently selected from 3-14 member cycloalkyls, 3-14 member heterocycloalkyls, unsubstituted -phenyls, and 5-14 member heteroaryls, Unsubstituted -F, -Cl, -Br, -I, -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ , 3-14 member cycloalkyl, 3-14 member heterocycloalkyl, unsubstituted -phenyl, monosubstituted or polysubstituted 5-14 member heteroaryl, independently selected from 5-14 member heteroaryl, or In each case, the unsubstituted -F, -Cl, -Br, -I, -C １－６ -Alkyl, -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C (=O) -C １－６ -alkyl, -C(=O)OH, -C(=O)-OC １－６ -alkyl, -C(=O)O-C １－６ -Alkilen-CF ３ , -OH, =O, -OC １－６ -alkyl, -NH ２ , - NHC １－６ -alkyl, -N(C) １－６ -Alkyl) ２ , -C １－６ -Alkilen-NH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkyl, -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-OH, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkylene-NHC(=O)O-C １－６ -Alkyl, -NHC(=O)O-C １－６ -alkyl, -C(=O)NH ２ , -C(=O)-NH-C １－６ -alkyl, -C(=O)-N(C １－６ -Alkyl) ２ , -S (=O) ２ C １－６ -alkyl, -S (=O) ２ -NH ２ , -S (=O) ２ -NH(C) １－６ -alkyl), -S (=O) ２ -N(C) １－６ -Alkyl) ２ -C １ -C ６ -Alkyl, -C ２ -C ６ -Alkenyl, -C ２ -C ６ - The compound according to claim 1 or its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs, representing alkynyl.

8. R １ However, -H, -F, -Cl, -Br, -I, -CN, -C １－６ -alkyl, -O-C １－６ -Alkyl, -C １－６ -Alkylene-O-C １－６ -Alkyl, -C １－６ -Alkilen-NH(C) １－６ -Alkyl), -C １－６ -Alkylene-N(C) １－６ -Alkyl) ２ , -CF ３ , -CF ２ H, -CFH ２ , -CF ２ Cl, -CFCl ２ , -C １－６ -Alkilen-CF ３ , -C １－６ -Alkilen-CF ２ H, -C １－６ -Alkilen-CFH ２ , -C １－６ - Alkilen-NH-C １－６ -Alkilen-CF ３ , -C １－６ -Alkylene-N(C) １－６ -Alkyl)-C １－６ -Alkilen-CF ３ , -C(=O)C １－６ -alkyl, -C(=O)OC １－６ -alkyl, -C(=O)NHC １－６ -alkyl, -C(=O)NH ２ , -C(=O)N(C １－６ -Alkyl) ２ , -S(=O)-C １－６ -alkyl, -S (=O) ２ -C １－６ -alkyl, -O-C １－６ A compound according to claim 1, or a stereoisomer, physiologically acceptable salt, solvate and / or polymorph thereof, representing an alkyl, unsubstituted-cyclopropyl, unsubstituted-cyclobutyl, unsubstituted-cyclopentyl, or unsubstituted-cyclohexyl.

9. R ５ and R ５ 'But, independently of each other, -H, Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C １ -C ６ - Alkyl, Saturated or unsaturated, unsubstituted, mono-substituted or multi-substituted -C １ -C ６ -heteroalkyl, A saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl group, wherein the 3- to 14-membered cycloalkyl group is -C １ -C ６ -Alkylene- or -C １ -C ６ The compound according to claim 1 or its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs, optionally linked through a heteroalkylene, in each case representing a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, 3 to 14-membered cycloalkyl group.

10. R ６ , R ７ , and R ８ are, independently of each other, -H、-F、-Cl、-Br、-I、-OH、-SH、-SF ５ 、-CN、-NO ２ 、-C(=O)OH、-NH ２ 、 -C １－６ -Alkyl, -CF ３ ,-CHF ２ ien-CH ２ F, -O-C １－６ -Alkyl, -OCF ３ , -OCHF ２ , -OCH ２ F, Non-substituted, or independently of each other: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF ３ ,-CHF ２ ien-CH ２ F, -OCF ３ , -OCHF ２ , -OCH ２ F, SF ５ , -NO ２ , -C(=O)OH, -NH ２ , and -C(=O)NH ２ -NHC １－６ - Alkyl, Non-substituted, or independently of each other: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF ３ ,-CHF ２ ien-CH ２ F, -OCF ３ , -OCHF ２ , -OCH ２ F, SF ５ , -NO ２ , -C(=O)OH, -NH ２ , and -C(=O)NH ２ -N(C) is substituted with one or more substituents selected from １－６ -Alkyl) ２ , Non-substituted, or independently of each other: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF ３ ,-CHF ２ ien-CH ２ F, -OCF ３ , -OCHF ２ , -OCH ２ F, SF ５ , -NO ２ , -C(=O)OH, -NH ２ , and -C(=O)NH ２ -C(=O)OC which is substituted with one or more substituents selected from １－６ - Alkyl, Non-substituted, or independently of each other: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF ３ ,-CHF ２ ien-CH ２ F, -OCF ３ , -OCHF ２ , -OCH ２ F, SF ５ , -NO ２ , -C(=O)OH, -NH ２ , and -C(=O)NH ２ -OC(=O)C, which is substituted with one or more substituents selected from １－６ - Alkyl, or Non-replaced or independently of each other, -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF ３ , -CHF ２ , -CH ２ F, -OCF ３ , -OCHF ２ , -OCH ２ F, SF ５ , -NO ２ , -C(=O)OH, -NH ２ , and -C(=O)NH ２ substituted with one or more substituents selected from, -C １－６ -heteroalkyl, represents the compound according to claim 1 or a stereoisomer, a physiologically acceptable salt, solvate and / or polymorph thereof.

11. Compound 001-(2R)-2-{[5-(benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamide}propanamide, Compound 002-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 003-(2R)-2-({2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 004-(2R)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 005-(2R)-2-({2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 006-(2R)-2-({2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 007-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 008-(2S)-2-({2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 009-(2S)-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 010-(2S)-2-({5-[(2-hydroxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 011-(2S)-2-({2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 012-(2S)-2-({2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 013-5-(benzyloxy)-2-(difluoromethyl)-N-[2-methyl-2-(morpholine-4-yl)propyl]-1-benzothiophene-3-carboxamide, Compound 014-5-(benzyloxy)-2-(difluoromethyl)-N-(2-hydroxy-2-methylpropyl)-1-benzothiophene-3-carboxamide Compound 015-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazole-4-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 016-(2S)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 017-(2R)-3-hydroxy-2-({2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 018-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 019-3-hydroxy-2-methyl-2-({2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 020-3-{2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-amide}oxolan-3-carboxamide, Compound 021-4-{2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-amide}oxan-4-carboxamide, Compound 022-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 023-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 024-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 025-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 026-3-{2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 027-(2S)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 028-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 029-(2R)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 030-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 031-2-methyl-2-({2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 032-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 033-4-{2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-amide}oxan-4-carboxamide, Compound 034-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 035-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 036-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 037-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 038-3-{2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 039-N-(3,3-difluorocyclobutyl)-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 040-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-(1-methyl-1H-pyrazole-3-yl)-1-benzothiophene-3-carboxamide, Compound 041-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-(2-oxopyrrolidine-3-yl)-1-benzothiophene-3-carboxamide, Compound 042-N-(3,3-difluoropiperidine-4-yl)-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 043-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide, Compound 044-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-[2-methyl-2-(morpholine-4-yl)propyl]-1-benzothiophene-3-carboxamide, Compound 045-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 046-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-[(5-oxopyrrolidine-2-yl)methyl]-1-benzothiophene-3-carboxamide, Compound 047-N-[(6-hydroxypyridine-2-yl)methyl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 048-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-[2-(2-oxo-1,3-oxazolidine-3-yl)ethyl]-1-benzothiophene-3-carboxamide, Compound 049-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxylic acid, Compound 050-(2S)-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamide}-3-hydroxypropanamide, Compound 051-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-3-hydroxypropanamide, Compound 052-(2S)-3-hydroxy-2-({2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 053-(2S)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 054-(2S)-3-hydroxy-2-({5-[(2-hydroxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 055-5-[(2-fluorophenyl)methoxy]-N-[(3R)-1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 056-(2R)-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-3-hydroxypropanamide, Compound 057-(2R)-3-hydroxy-2-({2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 058-(2R)-3-hydroxy-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 059-5-[(2-fluorophenyl)methoxy]-N-[(3S)-1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 060-5-(benzyloxy)-2-methyl-N-[(3S)-2-oxopyrrolidine-3-yl]-1-benzothiophene-3-carboxamide, Compound 061-2-{[5-(cyclopropylmethoxy)-2-methyl-1-benzothiophen-3-yl]formamide}-2-methylpropanamide, Compound 062-2-{[5-(benzyloxy)-2-methyl-1-benzothiophen-3-yl]formamide}-2-methylpropanamide, Compound 063-2-({5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-2-methylpropanamide, Compound 064-2-methyl-2-({2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 065-2-methyl-2-[(2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophen-3-yl)formamide]propanamide, Compound 066-2-({5-[(2-hydroxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-2-methylpropanamide, Compound 067-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxan-4-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 068-3-hydroxy-2-methyl-2-({2-methyl-5-[(oxetan-3-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 069-5-(cyclopropylmethoxy)-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-1-benzothiophene-3-carboxamide, Compound 070-4-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-amide}oxan-4-carboxamide, Compound 071-4-{2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophene-3-amide}oxan-4-carboxamide, Compound 072-4-{5-[(2-hydroxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-amide}oxan-4-carboxylic acid, Compound 073-5-(benzyloxy)-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 074-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 075-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 076-N-[1-(hydroxymethyl)cyclopropyl]-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 077-5-[(2-fluorophenyl)methoxy]-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 078-N-[1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 079-N-[1-(hydroxymethyl)cyclobutyl]-5-[(2-hydroxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 080-5-(benzyloxy)-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 081-5-[(2-fluorophenyl)methoxy]-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 082-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 083-N-[4-(hydroxymethyl)oxan-4-yl]-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 084-N-[4-(hydroxymethyl)oxan-4-yl]-5-[(2-hydroxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 085-5-[(2-fluorophenyl)methoxy]-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 086-N-[3-(hydroxymethyl)oxetan-3-yl]-2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 087-3-{5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 088-3-{2-methyl-5-[(pyridine-2-yl)methoxy]-1-benzothiophene-3-amide}oxetane-3-carboxamide, Compound 089-5-(benzyloxy)-N-(3,3-difluorocyclobutyl)-2-methyl-1-benzothiophene-3-carboxamide Compound 090-N-(3,3-difluorocyclobutyl)-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 091-5-(benzyloxy)-2-methyl-N-(1-methyl-1H-pyrazole-3-yl)-1-benzothiophene-3-carboxamide, Compound 092-2-methyl-N-(1-methyl-1H-pyrazole-3-yl)-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 093-5-[(2-fluorophenyl)methoxy]-2-methyl-N-(2-oxopyrrolidine-3-yl)-1-benzothiophene-3-carboxamide, Compound 094-2-methyl-N-(2-oxopyrrolidine-3-yl)-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 095-En1-N-(3,3-difluoropiperidine-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 095-En2-N-(3,3-difluoropiperidine-4-yl)-5-[(2-fluorophenyl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 096-5-(benzyloxy)-2-methyl-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide, Compound 097-2-methyl-N-(oxolan-3-yl)-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 098-5-(benzyloxy)-2-methyl-N-[2-methyl-2-(morpholine-4-yl)propyl]-1-benzothiophene-3-carboxamide, Compound 099-2-methyl-N-[2-methyl-2-(morpholine-4-yl)propyl]-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 100-5-(benzyloxy)-N-(2-hydroxy-2-methylpropyl)-2-methyl-1-benzothiophene-3-carboxamide Compound 101-N-(2-hydroxy-2-methylpropyl)-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 102-5-(benzyloxy)-2-methyl-N-[(5-oxopyrrolidine-2-yl)methyl]-1-benzothiophene-3-carboxamide, Compound 103-2-methyl-N-[(5-oxopyrrolidine-2-yl)methyl]-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 104-5-(benzyloxy)-N-[(6-hydroxypyridine-2-yl)methyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 105-N-[(6-hydroxypyridine-2-yl)methyl]-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 106-5-(benzyloxy)-2-methyl-N-[2-(2-oxo-1,3-oxazolidine-3-yl)ethyl]-1-benzothiophene-3-carboxamide, Compound 107-2-methyl-N-[2-(2-oxo-1,3-oxazolidine-3-yl)ethyl]-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 108-5-(benzyloxy)-2-methyl-1-benzothiophene-3-carboxylic acid, Compound 109-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxylic acid, Compound 111-5-(benzyloxy)-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-1-benzothiophene-3-carboxamide, Compound 112-5-(benzyloxy)-2-(difluoromethyl)-N-{[1-(dimethylamino)cyclopentyl]methyl}-1-benzothiophene-3-carboxamide, Compound 113-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 114-N-{[1-(dimethylamino)cyclopentyl]methyl}-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 115-5-(benzyloxy)-N-[2-(dimethylamino)ethyl]-2-methyl-1-benzothiophene-3-carboxamide, Compound 116-5-(benzyloxy)-2-(difluoromethyl)-N-[2-(dimethylamino)ethyl]-1-benzothiophene-3-carboxamide, Compound 117-N-[2-(dimethylamino)ethyl]-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 118-N-[2-(dimethylamino)ethyl]-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 119-5-(benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidine-3-yl)-2-(difluoromethyl)-1-benzothiophene-3-carboxamide, Compound 120-5-(benzyloxy)-N-(4,4-difluoro-1-methylpyrrolidine-3-yl)-2-methyl-1-benzothiophene-3-carboxamide, Compound 121-N-(4,4-difluoro-1-methylpyrrolidine-3-yl)-2-methyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 122-N-(4,4-difluoro-1-methylpyrrolidine-3-yl)-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 123-5-(benzyloxy)-2-methyl-N-(1-methylpyrrolidine-3-yl)-1-benzothiophene-3-carboxamide, Compound 124-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methylpyrrolidine-3-yl)-1-benzothiophene-3-carboxamide, Compound 125-2-methyl-N-(1-methylpyrrolidine-3-yl)-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 126-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-(1-methylpyrrolidine-3-yl)-1-benzothiophene-3-carboxamide, Compound 127-5-(benzyloxy)-2-methyl-N-(1-methylpiperidine-4-yl)-1-benzothiophene-3-carboxamide, Compound 128-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methylpiperidine-4-yl)-1-benzothiophene-3-carboxamide, Compound 129-2-methyl-N-(1-methylpiperidine-4-yl)-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 130-2-methyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-N-(1-methylpiperidine-4-yl)-1-benzothiophene-3-carboxamide, Compound 131-5-(benzyloxy)-2-(difluoromethyl)-N-(1-methyl-1H-pyrazole-3-yl)-1-benzothiophene-3-carboxamide, Compound 132-3-hydroxy-N,2-dimethyl-2-({2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophen-3-yl}formamide)propanamide, Compound 133-N-methyl-3-{2-methyl-5-[(2-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-amide}oxolan-3-carboxamide, Compound 134-5-(benzyloxy)-N,2-dimethyl-1-benzothiophene-3-carboxamide, Compound 135-5-(benzyloxy)-2-(difluoromethyl)-N-methyl-1-benzothiophene-3-carboxamide Compound 136-N,2-dimethyl-5-{[2-(trifluoromethyl)pyridine-3-yl]methoxy}-1-benzothiophene-3-carboxamide, Compound 137-N,2-dimethyl-5-[(4-methyl-1,3-thiazole-5-yl)methoxy]-1-benzothiophene-3-carboxamide, Compound 138-(2S)-2-({5-[(2-methoxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 139-(2S)-3-hydroxy-2-({5-[(2-methoxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 140-(2R)-2-({5-[(2-methoxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)propanamide, Compound 141-2-({5-[(2-methoxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophen-3-yl}formamide)-2-methylpropanamide, Compound 142-N-[1-(hydroxymethyl)cyclopropyl]-5-[(2-methoxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 143-N-[1-(hydroxymethyl)cyclobutyl]-5-[(2-methoxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 144-N-[4-(hydroxymethyl)oxan-4-yl]-5-[(2-methoxypyridine-3-yl)methoxy]-2-methyl-1-benzothiophene-3-carboxamide, Compound 145-5-(benzyloxy)-N-(3,3-difluorocyclobutyl)-2-(difluoromethyl)-1-benzothiophene-3-carboxamide, Compound 146-5-(benzyloxy)-2-(difluoromethyl)-N-(2-oxopyrrolidine-3-yl)-1-benzothiophene-3-carboxamide, Compound 147-5-(benzyloxy)-2-(difluoromethyl)-N-(oxolan-3-yl)-1-benzothiophene-3-carboxamide, Compound 148-5-(benzyloxy)-2-(difluoromethyl)-N-[(5-oxopyrrolidine-2-yl)methyl]-1-benzothiophene-3-carboxamide, Compound 149-5-(benzyloxy)-2-(difluoromethyl)-N-[2-(2-oxo-1,3-oxazolidine-3-yl)ethyl]-1-benzothiophene-3-carboxamide, Compound 150-5-(benzyloxy)-2-(difluoromethyl)-1-benzothiophene-3-carboxylic acid, Compound 151-5-(benzyloxy)-2-(difluoromethyl)-N-[(6-hydroxypyridine-2-yl)methyl]-1-benzothiophene-3-carboxamide, and Compound 152-5-(benzyloxy)-2-(difluoromethyl)-N-[4-(hydroxymethyl)oxan-4-yl]-1-benzothiophene-3-carboxamide, The compound according to claim 1 or its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs, selected from the group consisting of the stereoisomers thereof, physiologically acceptable salts, solvates, and / or polymorphs.

12. A pharmaceutical composition comprising a compound according to any one of claims 1 to 11 or a stereoisomer thereof, a physiologically acceptable salt, solvate, and / or polymorph.

13. A pharmaceutical composition according to claim 12 for use as a medicine.

14. The pharmaceutical composition according to claim 12 for use in the treatment of pain or epilepsy.

15. The pharmaceutical composition according to claim 14, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain, and is preferably postoperative pain.

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