Pyrazolo [1, 5-a] pyridine derivatives for treatment of TRPM3-mediated disorders

Abstract

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

Description

Technical Field

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

[0002] The TRP superfamily consists of proteins with six transmembrane domains (6TM) that assemble into homo- or hetero-tetramers to form cation-permeable ion channels. The name TRP derives from the Drosophila trp (transient receptor potential) mutant, which characterizes Drosophila photoreceptors as having a transient receptor potential in response to sustained light. Over the past 15 years, trp-related channels have been identified in yeast, worms, insects, fish, and mammals, including 27 TRPs in humans. Based on sequence homology, TRP channels can be divided into seven subfamilies: TRPC, TRPV, TRPM, TRPA, TRPP, TRPML, and TRPN.

[0003] Members of the TRP superfamily are likely expressed in all mammalian organs and cell types, and much progress has been made in recent years in understanding their physiological roles. The specific selectivity of certain TRP channels enables them to 2+ Mg 2+ TRP channels play a key role in the cellular uptake and / or transepithelial transport of trace metal ions. In addition, the sensitivity of TRP channels to a variety of chemical and physical stimuli enables them to participate as dedicated biosensors in processes ranging from vision to taste and touch. In particular, several members of the TRP superfamily show very high sensitivity to temperature. These so-called thermal TRPs are highly expressed in sensory neurons and / or skin keratinocytes, where they act as the main thermal sensors for detecting both harmless and noxious (painful) temperatures.

[0004] It is becoming increasingly clear that TRP channel dysfunction is directly involved in the etiology of a variety of inherited and acquired diseases. In fact, loss-of-function and gain-of-function mutations in TRP channel genes have been identified as direct causes of inherited diseases including brachyolmia, hypomagnesemia with secondary hypocalcemia, polycystic kidney disease, mucolipidosis type IV, and familial focal segmental glomerulosclerosis. In addition, TRP channel function / dysfunction has been directly linked to a variety of pathological conditions including chronic pain, hypertension, cancer, and neurodegenerative disorders.

[0005] TRPM3 (transient receptor potential mestatin 3) represents a promising pharmacological target. TRPM3 is expressed in a large subpopulation of small diameter sensory neurons from dorsal root and trigeminal ganglion, and is involved in thermal induction. Neurosteroid pregnenolone sulfate is a known effective TRPM3 activator (Wagner et al., 2008). Neurosteroid pregnenolone sulfate induces pain in wild-type mice, but not in knockout TRPM3 mice. Recently, it has also been shown that CFA-induced inflammation and inflammatory pain are eliminated in TRPM3 knockout mice. Therefore, TRPM3 antagonists can be used as analgesics to combat pain, such as inflammatory pain (Vriens J. et al., Neuron, May 2011). The relationship between TRPM3 and epilepsy has also been confirmed (see, for example, Eur J Hum Genet. 2019 Oct;27(10):1611–1618; Elife 2020 May 19;9:e57190.doi:10.7554 / eLife.57190.DOI:10.7554 / eLife.57190; Channels (Austin). 2021;15(1):386–397. Therefore, TRPM3 is also a potential target for the treatment of epilepsy.

[0006] Some TRPM3 antagonists are known, but none of them point to the compounds of the present invention (Straub I et al., Mol Pharmacol, November 2013). For example, liquiritigenin (a putative TRPM3 blocker) has been described as reducing mechanical and cold hyperalgesia in a rat pain model (Chen L et al., Scientific reports, July 2014). There is still a huge medical need for new, alternative and / or better therapeutic agents for preventing or treating TRPM3-mediated disorders, more particularly pain such as inflammatory pain and epilepsy. There is a great need for therapeutic agents with good efficacy, low levels or no side effects (such as unlikely to be addictive, non-toxic like opioids) and / or good or better pharmacokinetic or pharmacodynamic properties for certain types of pain.

[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] The present invention provides pyrazolo[1,5-a]pyridine derivatives and pharmaceutical compositions comprising such pyrazolo[1,5-a]pyridine derivatives. The present invention also provides pyrazolo[1,5-a]pyridine derivatives for use as a medicament, more particularly for preventing and / or treating TRPM3-mediated disorders, in particular for preventing and / or treating pain and / or inflammatory hypersensitivity and / or epilepsy; and / or for combating pain and / or inflammatory hypersensitivity and / or for combating epilepsy.

[0009] The present invention also provides the use of pyrazolo[1,5-a]pyridine derivatives in the manufacture of pharmaceutical compositions or drugs for preventing and / or treating TRPM3-mediated disorders, especially for preventing and / or treating pain and / or inflammatory hypersensitivity and / or epilepsy; and / or for combating pain and / or inflammatory hypersensitivity and / or epilepsy.

[0010] The present invention also provides a method for preventing or treating a TRPM3-mediated disorder by administering a pyrazolo[1,5-a]pyridine derivative according to the present invention to a subject in need thereof. More particularly, the present invention relates to such a method for preventing and / or treating pain and / or inflammatory hypersensitivity and / or epilepsy; and / or for combating pain and / or inflammatory hypersensitivity and / or epilepsy.

[0011] The present invention further provides a method for preparing the pyrazolo[1,5-a]pyridine derivatives of the present invention. DETAILED DESCRIPTION

[0012] The present invention will be further described and in some cases described with respect to specific embodiments but the invention is not limited thereto.

[0013] The first aspect of the present invention is to provide a compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph

[0014]

[0015] Optionally for use in treating pain or epilepsy or in a method of treating pain or epilepsy;

[0016] in

[0017] R 1 Indicates -F, -Cl, -Br, -I, -CN, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W、-S(=O)R W 、-S(=O) 2 R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;

[0018] Q means -OR 2 or -NR 3 R 4 ;

[0019] R 2 Indicates -R Y ;

[0020] R 3 Indicates -OH or -R Y ;

[0021] R 4 Indicates -R Y or -S(=O) 2 R Y ;

[0022] or R 3 and R 4 together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S;

[0023] T stands for -O- and U stands for -CR 5 R 5 '-; or T means -CR 5 R 5 '- and U means -O-;

[0024] R 5 and R 5 'Independently represent -R Y ;

[0025] R 6 , R 7 and R 8 Independently represent -F, -Cl, -Br, -I, -CN, -NO 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 ;

[0026] V represents a saturated or unsaturated 3-14-membered heterocycloalkyl; a saturated or unsaturated 3-14-membered cycloalkyl; a 5-14-membered aryl; -C 1 -C 6 Alkyl, -C 1 -C 6 heteroalkyl; or 5-14 membered heteroaryl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are singly or polysubstituted;

[0027] in

[0028] R W and R X Independently of each other and in each case independently represent

[0029] -H;

[0030] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0031] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6-heteroalkyl;

[0032] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0033] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0034] R Y and R Z Independently of each other and in each case independently represent

[0035] -H;

[0036] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0037] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0038] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0039] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0040] unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl; wherein the 6-14 membered aryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0041] unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl; wherein the 5-14 membered heteroaryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0042] or R Y and R Z together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S;

[0043] and wherein "mono- or poly-substituted" in each case independently refers to substitution by one or more, e.g. 1, 2, 3, 4 or more substituents, said substituents being independently selected from the group consisting of: -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-O-CF 3 , -C 1-6 -Alkylene-O-CF 2 H, -C 1-6 -Alkylene-O-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 -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), -N(3-14 membered cycloalkyl)(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C 1-6 -alkylene-OH, -N(H)-C 1-6 -alkylene-OH, -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, -C1-6 -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 -C1-6 -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-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14-membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(=O)-(3- to 14-membered cycloalkyl), -C(=O)-(3- to 14-membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5- to 14-membered heteroaryl), -S(=O) 2 -(3-14 membered cycloalkyl), -S(=O) 2 -(3 to 14 membered heterocycloalkyl), -S(=O) 2 -phenyl, -S(=O) 2 -(5- to 14-membered heteroaryl).

[0044] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention

[0045] (a-1)Q represents -NR 3 R 4 ; R 1 Represents R W ; and R W Indicates -C 1 -C 6 -alkyl-, and / or

[0046] (a-2) Q represents -NR 3 R 4 ; and R 5 and R 5 ' represents -H; and / or

[0047] (a-3) Q represents -NR 3 R 4 ; and R 6 indicates -H; and / or

[0048] (a-4) Q represents -NR 3 R 4 ; and R 8 Indicates -H;

[0049] or

[0050] (b-1)

[0051] (b-1) Q represents -NR 3 R 4 ; and R 1 Indicates -CH 2 F, -CHF 2 , -CF 3 , -CN, -methyl, -ethyl, -propyl or -cyclopropyl; and / or

[0052] (b-2) Q represents -NR 3 R 4 ; and R 5 and R 5 ' does not represent -H; and / or

[0053] (b-3) Q represents -NR 3 R 4 ; and R 3 Indicates -H.

[0054] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, T represents -O- and U represents -CR 5 R 5 According to this embodiment, the pyrazolo[1,5-a]pyridine derivative according to the invention is a compound of formula (II), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph

[0055]

[0056] In another embodiment of the pyrazolo[1,5-a]pyridine derivative according to formula I, T represents -CR 5 R 5 '- and U means -O-.

[0057] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to formula I or II, R 1 Methyl, ethyl or other C 1 -C 6 In another preferred embodiment, R 1 It's methyl.

[0058] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, Q represents -NR3 R 4 .

[0059] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, Q represents -OR 2 .

[0060] In some embodiments of the pyrazolo[1,5-a]pyridine derivative according to the present invention, V represents a saturated or unsaturated 3-14-membered cycloalkyl group; a 3-14-membered heterocycloalkyl group, a saturated or unsaturated 5-14-membered aryl group; 1 -C 6 alkyl; or 5-14 membered heteroaryl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0062] In some embodiments, the 5-14 membered heteroaryl group within the definition of V is selected from benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, pyrazolo[1,5-a]pyridine, 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; each of which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF 3 , -CF2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0063] Preferably, the 5-14 membered heteroaryl within the definition of V is selected from the group consisting of furan, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, triazole, pyridine, isoquinoline, benzothiazole, pyridazine, pyrimidine, imidazopyridine; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0064] Preferably, the 5- to 14-membered heteroaryl within the definition of V is selected from the group consisting of furan-2-yl, furan-3-yl, thiophen-2-yl, thiophen-3-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, oxazol-5-yl, isoxazol-4-yl, thiazol-2-yl, thiazol-4-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; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0065] In some embodiments, the 5-14 membered heteroaryl group within the definition of V is selected from the group consisting of pyrazol-3-yl, pyrazol-4-yl, thiazol-4-yl, thiazol-5-yl, pyridin-2-yl, pyridin-3-yl and pyridin-4-yl; each of which is unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR YC(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0066] In one embodiment, the saturated or unsaturated 3-14 membered cycloalkyl within the definition of V is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl or cyclodecyl, including unfused or unbridged, fused or bridged cycloalkyl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0067] In one embodiment, the 5-14 membered aryl group within the definition of V is phenyl or another 5-14 membered aryl group which is unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y RZ 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0068] In other embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, V represents a 3-14 membered heterocycloalkyl group, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0069] In some embodiments, the 3-14 membered heterocycloalkyl group within the definition of V is selected from azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiazolin-cyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydro-cyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; in each case unsubstituted, independently of one another selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0070] In some embodiments, the 3-14 membered heterocycloalkyl group within the definition of V is oxane, oxane-4-yl, oxetane or oxetane-3-yl; each of which is unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5, -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0071] In another preferred embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, V represents C 1 -C 6 Alkyl or C 1 -C 6 Heteroalkyl, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0072] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, V is unsubstituted, monosubstituted or polysubstituted by substituents independently selected from the following:

[0073] -F, -Cl, -Br, -I, -CN, -C(=O)OH, -NH2 、-NO 2 、-OH、=O、-SF 5 ;

[0074] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl;

[0075] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 -alkyl;

[0076] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -NHC 1-6 -alkyl;

[0077] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C 1-6 -alkyl) 2 ;

[0078] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 -alkyl;

[0079] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O) 2 -C 1-6 -alkyl;

[0080] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0081] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0082] In some embodiments, V is unsubstituted, monosubstituted or polysubstituted with substituents independently selected from the following:

[0083] -OH, -F, -Cl, -Br, -I, -SH, -CF 3 , -CHF 2 、-CH2 F, -OCF 3 、-OCHF 2 、-OCH 2 F. SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 or -N(CH 3 ) 2 ;

[0084] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0085] -C 1-6 -heteroalkyl, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0086] -OC 1-6-alkyl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0087] -O(C=O)C 1-6 -alkyl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0088] -C(=O)OC 1-6 -alkyl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -SH, =S, -CN, -CF 3 , -CHF 2 、-CH 2 F, -OCF 3 、-OCHF 2 、-OCH 2 F. SF 5 、-NO2 , -C(=O)OH, -NH 2 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0089] 3-14 membered cycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; each of which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0090] 3-14 membered heterocycloalkyl selected from azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azooctane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolin, isoxazolidine, morpholine, oxazolidine, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, thiomorpholine, indoline, dihydrobenzofuran, the group consisting of: hexahydro-1H-pyrrolizine, hexahydro-cyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine, in each case unsubstituted, independently of one another, selected from the group consisting of -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono-substituted or poly-substituted.

[0091] In some embodiments, V is unsubstituted, independently selected from -F, -Cl, -CN, -OH, =O, -C 1-6 -alkyl, methyl, ethyl, -CHF 2 , -CF 3 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-NHC(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl) 2 、-OC 1-6 -alkyl, -OCF 3 、-OC 1-6 -alkylene-N(C 1-6 -alkyl) 2 、-S(=O) 2 -C 1-6 -alkyl, -azetidine, -C 1-6 -alkylene-O-tetrahydropyran or -C 1-6 The substituents of the -alkyl-substituted-piperazine are mono- or poly-substituted.

[0092] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, V is

[0093] (i) unsubstituted;

[0094] (ii) monosubstituted;

[0095] (iii) disubstituted;

[0096] (iv) trisubstituted; or

[0097] (v) Tetrasubstituted.

[0098] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, V is

[0099] (i) unsubstituted;

[0100] (ii) monosubstituted; or

[0101] (iii) Disubstituted.

[0102] In some embodiments, V represents a saturated or unsaturated 3-14-membered heterocycloalkyl (preferably a 3-5-membered heterocycloalkyl); a 5-14-membered heteroaryl (preferably a 5-6-membered heteroaryl); a saturated or unsaturated 3-14-membered cycloalkyl; a 5-14-membered aryl; or C 1 -C 6 Alkyl; in each case unsubstituted, monosubstituted or polysubstituted; preferably a residue selected from the group consisting of:

[0103]

[0104]

[0105] In one embodiment, V represents unsubstituted, monosubstituted or polysubstituted -oxetane; preferably

[0106] In some embodiments, V represents a residue according to formula (E)

[0107]

[0108] in

[0109] Y E1 Indicates -N=, -NR E2 -, S, O, or -CR E3 =; Y E2 Indicates -N=, -NR E3 -, S, O, or -CR E4 =; and Y E3 Indicates -N=, -NR E4 -, S, O, or -CR E5 =; condition is Y E1 , Y E2 and Y E3 At least one of them is not -CR E3 =, -CR E4 = and -CR E5 = In another preferred embodiment, V represents a residue according to the general formula (E)

[0110] Wherein YE1 represents -N=, -NRE2-, S or -CRE3=; YE2 represents -N=, -NRE3-, S or -CRE4=; and YE3 represents -N=, -NRE4-, S or -CRE5=; provided that at least one of YE1, YE2 and YE3 is not -CRE3=, -CRE4= and -CRE5=, respectively.

[0111] R E1 , R E2 , R E3 and R E4 Independently represent -H, -CH 3 、-CH 2 -cyclopropyl, -CH 2 CF 3 、-CH 2 CHF 2 or -CF 3 ; more particularly R E1 , R E2 , R E3 and R E4 Independently represent -H, -CH 3 or -CF 3 ; preferably the condition is R E1 , R E2 , R E3 and R E4 Only one of them represents a residue other than -H.

[0112] In some embodiments, V represents unsubstituted, monosubstituted or polysubstituted 2-pyridine. In some embodiments, V represents a residue selected from the group consisting of:

[0113]

[0114]

[0115] In some embodiments, V represents unsubstituted, monosubstituted or polysubstituted 3-pyridine. In a preferred embodiment, V represents a residue selected from the group consisting of:

[0116]

[0117] In some embodiments, V represents unsubstituted, monosubstituted or polysubstituted 4-pyridine. In a preferred embodiment, V represents a residue selected from the group consisting of:

[0118]

[0119] In some embodiments, optionally wherein U—CH 2, V represents a residue selected from the group consisting of:

[0120]

[0121]

[0122] In an alternative embodiment, V represents a residue selected from the group consisting of:

[0123]

[0124] In some embodiments, V represents an unsubstituted, monosubstituted or polysubstituted bicyclic heteroaryl, preferably selected from the group consisting of:

[0125]

[0126] In some embodiments, V represents a residue according to formula (F')

[0127]

[0128] in

[0129] Y F1 Indicates -N= or -CR F4 =; and Y F2 Indicates -N= or -CR F5 =; and Y F3 Indicates -N= or -CR F3 =; condition is Y F1 and Y F2 At least one of them is not -CR F4 = and -CR F5 =;

[0130] R F1 , R F2 , R F3 , R F4 and R F5 Independently represent -H, -CH 3 , -CF 3 、-OH、-OCH 3 、-OCH 2 CH 3 , -Cl or -azetidinyl; preferably, R F1 , R F2 , R F3 , R F4 and R F5 Only one of them represents a residue other than -H.

[0131] In another embodiment, V represents a residue according to formula (F)

[0132]

[0133] in

[0134] Y F1 Indicates -N= or -CR F4 =; and Y F2 Indicates -N= or -CR F5 =; condition is Y F1 and Y F2 At least one of them is not -CR F4 = and -CR F5 =;

[0135] R F1 , R F2 , R F3 , R F4 and R F5 Independently represent -H, -CH 3 , -CF 3 、-OH、-OCH 3 、-OCH 2 CH 3 , -Cl or -azetidinyl; preferably, R F1 , R F2 , R F3 , R F4 and R F5 Only one of them represents a residue other than -H.

[0136] In some embodiments, V represents a residue according to formula (G) or (H)

[0137]

[0138] Where R G1 and R H1 Selected from -H, -CH 3 , -CF 3 、-OH、-OCH 3 、-OCH 2 CH 3 , -Cl, azetidinyl, -cyclopropyl, -O-cyclopropyl, and -CHF 2 A group consisting of; or R G1 and R H1 Selected from -H, -CH 3 , -CF 3 、-OH、-OCH 3 、-OCH 2 CH 3 , -Cl and azetidinyl group.

[0139] In other embodiments, V represents a residue according to formula (G') or (H')

[0140]

[0141] Where R G1 and R H1 Selected from -H, -CH 3 , -CF 3 、-OH、-OCH 3 、-OCH 2 CH 3 , -Cl, azetidinyl, -cyclopropyl, -O-cyclopropyl, and -CHF 2 A group consisting of; or R G1 and R H1 Selected from -H, -CH 3 , -CF 3 、-OH、-OCH 3 、-OCH 2 CH 3 , -Cl and azetidinyl group;

[0142] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, R 1 represents -H, -F, -Cl, -Br, -I, -CN;

[0143] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl; saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 -alkyl;

[0144] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)C 1-6 -alkyl;

[0145] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 -alkyl;

[0146] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)NHC 1-6 -alkyl;

[0147] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)N(C 1-6 -alkyl) 2 ;

[0148] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)C 1-6 -alkyl;

[0149] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O) 2 -C 1-6 -alkyl;

[0150] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl; or

[0151] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0152] In some embodiments, R 1 Indicates -H, -F, -Cl, -Br, -I, -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 -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.

[0153] In some embodiments, R 1 Indicates -H, -C 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -CH 2 F, -CHF 2 , -CF 3 , unsubstituted -cyclopentyl or -cyclopropyl. Preferably, R 1 Indicates -H, -C 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -CH 2 F, -CHF 2 , -CF 3 In some embodiments, R 1 Indicates -CH 3 .

[0154] In some embodiments, R 1 Indicates -CH 2 F, -CHF 2 、-CH 3 Or -cyclopropyl. Preferably, R 1 Indicates -CH 2 F, -CHF 2 or -CH 3 In some embodiments, R 1 Represents -C(=O)NH 2 or -CHF 2 .

[0155] In some embodiments, R 1 Indicates -H, -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-CF2 H, -C 1-3 -Alkylene-CFH 2 or -cyclopropyl; preferably, R 1 Indicates -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 or -C 1-3 -Alkylene-CFH 2 ; For example -CH 3 .

[0156] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 2 Indicates -H;

[0157] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0158] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0159] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0160] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0161] In some embodiments, R 2 Indicates -H, -C 1-6 -alkyl, -C 1-6-Alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl) 2 , -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 .

[0162] In some embodiments, R 2 Indicates -H or -C 1-6 -alkyl.

[0163] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, R 3 Indicates -H;

[0164] -OH;

[0165] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl; or

[0166] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl.

[0167] In some embodiments, R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-NH 2 , -C 1-6 -alkylene-NH(C1-6 -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 .

[0168] In some embodiments, R 3 represents -H, -OH or saturated, unsubstituted or -C substituted by -OH 1-6 -alkyl. Preferably, R 3 Indicates -H.

[0169] In some embodiments, R 3 Indicates -H, and R 4 represents residues other than -H.

[0170] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, R 4 Indicates -H;

[0171] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)C 1-6 -alkyl;

[0172] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O) 2 -C 1-6 -alkyl;

[0173] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0174] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0175] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0176] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0177] unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl; wherein the 6-14 membered aryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0178] unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl; wherein the 5-14 membered heteroaryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0179] In some embodiments, R 4 express

[0180] -S(=O) 2 C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, independently selected from -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 - alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0181] -S(=O) 2 (3-14 membered cycloalkyl), wherein the 3-14 membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, each of which is saturated or unsaturated, unsubstituted, substituted independently of one another by -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 - alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0182] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, independently selected from -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, -C1-6 -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 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0183] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, in each case saturated or unsaturated, in each case unsubstituted, substituted independently of one another by -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)OC1-6 -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 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0184] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6-Alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from the group consisting of azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiazolidine, cyclopentane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothia-cyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolazine, hexahydro-cyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; in each case unsubstituted, independently of one another, selected from the group consisting of -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)OC1-6 -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 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0185] -phenyl, which is unsubstituted, independently selected from -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 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0186] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -Alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furan, imidazole, imidazopyridine, pyrazolo[1,5-a]pyridine, 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; in each case unsubstituted, independently selected from the group consisting of -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 The substituents from the group consisting of -alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl; and unsubstituted 5- to 14-membered heteroaryl are mono- or poly-substituted.

[0187] In some embodiments, R 4 express

[0188] -H;

[0189] Saturated, unsubstituted, mono- or poly-substituted by -F -S(=O) 2 C 1-6 -alkyl;

[0190] Saturated, unsubstituted -S(=O) 2 (3-14 membered cycloalkyl);

[0191] -C 1-6 -alkyl, which is saturated, unsubstituted, independently selected from -OH, =O, -NH 2 、-NHC 1-6 -alkyl, -N(C 1-6 -alkyl) 2 、-OC 1-6 -alkyl, -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 , unsubstituted -phenyl, mono-substituted or di-substituted;

[0192] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3-14 membered cycloalkyl is saturated, unsubstituted, substituted independently by -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 - The substituent group consisting of the alkyl group is mono-substituted or di-substituted;

[0193] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from azetidine, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole, octahydropyrrolo[1,2 -a] pyrazine, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiazolin-cyclohexane, in each case unsubstituted, independently selected from the group consisting of -F, -OH, =O, -C 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 - The substituents of the group consisting of alkylene-phenyl are mono- or poly-substituted;

[0194] unsubstituted-phenyl;

[0195] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, in each case unsubstituted, independently selected from the group consisting of -C 1-6 The substituent group consisting of -alkyl and -OH is mono- or di-substituted.

[0196] In one embodiment of the pyrazolo[1,5-a]pyridine derivative according to the present invention, R 3 and R 4 Together they form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S.

[0197] In some embodiments, R 3 and R 4 together to form a heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine and piperazine, each of which is unsubstituted, independently of one another, selected from the group consisting of -F, -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)OC 1-6 -alkyl, unsubstituted-pyridyl and unsubstituted or -C 1-6-alkyl monosubstituted 1,2,4-oxadiazole is monosubstituted or polysubstituted. 3 and R 4 Together, they do not form unsubstituted, monosubstituted or polysubstituted morpholines.

[0198] In some embodiments, R 3 and R 4 Together we form

[0199] Unsubstituted or -N(CH 3 ) 2 a monosubstituted pyrrolidine ring;

[0200] Not replaced or selected by -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 group consisting of a monosubstituted piperidine ring, and unsubstituted or -C 1-6 - alkyl monosubstituted 1,2,4-oxadiazole;

[0201] an unsubstituted morpholine ring; or

[0202] Not replaced or selected by -C 1-6 The substituents of the N-substituted piperazine ring are composed of -alkyl and unsubstituted -pyridyl.

[0203] In some embodiments, R 3 and R 4 Both do not represent -H. In some embodiments, R 3 and R 4 Together with the nitrogen atom to which they are attached, form a residue selected from the group consisting of:

[0204]

[0205]

[0206] In other embodiments, R 3 Indicates -H, and R 4 -H is not indicated.

[0207] In some embodiments, R 3 Indicates -H, and R 4 represents saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C6 -alkyl. In some embodiments, R 3 Indicates -H, and R 4 represents a residue selected from the group consisting of:

[0208]

[0209] In other embodiments, R 3 Indicates -H, and R 4 Represents the residue -CR'R"-(CH 2 ) m -OH, wherein m is an integer from 1 to 6, preferably from 1 to 3; and wherein R' and R" independently represent -H, -C 1-3 -alkyl, -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 or C(=O)-NH-C 1-3 -alkyl; preferably -H, -CH 3 , -C 1-3 -alkylene-OH, -C(=O)-NH 2 or C(=O)-NH-C 1-3 -alkyl. In one embodiment, at least R' or R" does not represent -H. In an alternative embodiment, neither R' or R" represents -H.

[0210] In other embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl group; or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered heterocycloalkyl group.

[0211] In other embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-membered cycloalkyl group; or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-membered heterocycloalkyl group. 3 Indicates -H, and R4 represents a residue selected from the group consisting of:

[0212]

[0213] In some embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 4-membered cycloalkyl group; or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered heterocycloalkyl group (preferably a 4-membered heterocycloalkyl group). 3 Indicates -H, and R 4 represents a residue selected from the group consisting of:

[0214]

[0215] In some embodiments, R 3 Indicates -H, and R 4 represents a residue according to the general formula (A),

[0216]

[0217] in

[0218] m A is 0 or 1;

[0219] Y A Selected from -O-, -NR A6 -and-CR A7 R A8 -;and

[0220] R A1 , R A2 , R A3 , R A4 , R A5 , R A6 , R A7 and R A8 Independently represent -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 ),-C1-3 -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 , -3-oxetane or -CHF 2 Preferably, R A1 , R A2 , R A3 , R A4 , R A5 , R A6 , R A7 and R A8 Independently represent -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 A8 Together with the carbon atoms to which they are attached, they form a ring and represent -CH 2 OCH 2 -、-CH 2 OCH 2 CH 2 -or-CH 2 CH 2 OCH 2 CH 2 -、-CH 2 NHCH 2 -、-CH2 NHCH 2 CH 2 -or-CH 2 CH 2 NHCH 2 CH 2 -.

[0221] In some embodiments, R 3 Indicates -H, and R 4 represents a residue according to the general formula (A) as defined above, wherein

[0222] m A is 0 or 1;

[0223] Y A Selected from -O- and -CR A7 R A8 -;and

[0224] R A1 , R A2 , R A3 , R A4 , R A5 , R A7 and R A8 Independently represent -H, -C 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C 1-3 -alkyl) 2 、-C(=O)NH 2 or -CHF 2 Preferably R A1 , R A2 , R A3 , R A4 , R A5 , R A7 and R A8 Independently represent -H, -C 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C 1-3 -alkyl) 2 or -C(=O)NH 2 ; preferably the condition is R A1 , R A2 , R A3 , R A4 , R A5 , R A7 and R A8 Only one of them represents a residue other than -H.

[0225] In some embodiments, R 3 Indicates -H, and R 4represents a residue according to the general formula (A) as defined above, wherein

[0226] m A is 0 or 1;

[0227] Y A Selected from -O- and -CR A7 R A8 -;and

[0228] R A1 Indicates -C 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C 1-3 -alkyl) 2 、-C(=O)NH 2 or -CHF 2 Preferably R A1 Indicates -C 1-3 -alkylene-OH, -C 1-3 -alkylene-N(C 1-3 -alkyl) 2 or -C(=O)NH 2 ;and

[0229] R A2 , R A3 , R A4 , R A5 , R A7 and R A8 Indicates -H.

[0230] In some embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl group (preferably a 5-membered cycloalkyl group); or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered heterocycloalkyl group (preferably a 5-membered heterocycloalkyl group); or an unsubstituted, monosubstituted or polysubstituted 5-14-membered heteroaryl group (preferably a 5-membered heteroaryl group). In a preferred embodiment, R 3 Indicates -H, and R 4 represents a residue selected from the group consisting of:

[0231]

[0232] In some embodiments, R 3 Indicates -H, and R 4 represents a residue according to the general formula (B),

[0233]

[0234] in

[0235] Y B Selected from -O-, -NR B8 -and-CR B9 R B10 -;and

[0236] R B1 , R B2 , R B3 , R B4 , R B5 , R B6 , R B7 , R B8 , R B9 and R B10 Independently represent -H, -F, -OH, -C 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, -C 1-3 -alkylene-C(=O)OC 1-3 -alkyl, -C(=O)NH 2 、-C(=O)NH-C 1-3 -alkyl or -C(=O)N(C 1-3 -alkyl) 2 ; or R B2 and R B3 Together they represent =O; or R B4 and R B5 Together they represent =O.

[0237] In some embodiments, R 3 Indicates -H, and R 4 represents a residue according to the general formula (B) as defined above, wherein

[0238] Y B Selected from -O- and -NR B8 -;and

[0239] R B1 , R B2 , R B3 , R B4 , R B5 , R B6 , R B7 , R B8 Independently represent -H, -F, -C 1-3 -alkyl, -C 1-3 -alkylene-OH, -C1-3 -Alkylene-CF 3 or -C(=O)NH 2 ; or R B2 and R B3 Together they represent =O; or R B4 and R B5 Together they represent =O; preferably the condition is R A1 , R A2 , R A3 , R A4 , R A5 , R A7 and R A8 Only 1, 2 or 3 of them represent residues other than -H; preferably, the condition is that R A1 , R A2 , R A3 , R A4 , R A5 , R A7 and R A8 At least one of represents a residue other than -H.

[0240] In some embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl group (preferably a 6-membered cycloalkyl group); or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered heterocycloalkyl group (preferably a 6-membered heterocycloalkyl group); or an unsubstituted, monosubstituted or polysubstituted 6-14-membered aryl group (preferably a 6-membered aryl group); or an unsubstituted, monosubstituted or polysubstituted 5-14-membered heteroaryl group (preferably a 6-membered heteroaryl group). In a preferred embodiment, R 3 Indicates -H, and R 4 represents a residue selected from the group consisting of:

[0241]

[0242]

[0243] In some embodiments, R 3 Indicates -H, and R 4 represents a residue according to the general formula (C),

[0244]

[0245] in

[0246] Y C1 Selected from -O-, -S(=O) 2 -、-NR C8 -and-CR C9 R C10-, and Y C2 Indicates -CR C11 R C12 -; or Y C1 Indicates -CR C9 R C10 -, and Y C2 Selected from -O-, -S(=O) 2 -and-NR C8 -;

[0247] R C1 , R C2 , R C3 , R C4 , R C5 , R C6 , R C7 , R C8 , R C9 , R C10 , R C11 and R C12 Independently express

[0248] 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-, -C(=O)NH 2 、-C(=O)NH-C 1-3 -alkyl or -C(=O)N(C 1-3 -alkyl) 2 : or R C2 and R C3 Together they represent =O; or R C4 and R C5 Together they represent =O; or R C9 and R C10 Together they represent =O; or R C11 and R C12 Together they represent =O.

[0249] In some embodiments, R 3 Indicates -H, and R 4 represents a residue according to the general formula (C) as defined above, wherein

[0250] Y C1 Selected from -O- or -NR C8 -, and Y C2 Indicates -CRC11 R C12 -; or Y C1 Indicates -CR C9 R C10 -, and Y C2 Selected from -O- and -NR C8 -;

[0251] R C1 , R C2 , R C3 , R C4 , R C5 , R C6 , R C7 , R C8 , R C9 , R C10 , R C11 and R C12 Independently represent -H, -F, -C 1-3 -alkyl, -C 1-3 -alkylene-OH or -C(=O)NH 2 ; preferably the condition is R C1 , R C2 , R C3 , R C4 , R C5 , R C6 , R C7 , R C8 , R C9 , R C10 , R C11 and R C12 Only 1, 2 or 3 of them represent residues other than -H; preferably, the condition is that R C1 , R C2 , R C3 , R C4 , R C5 , R C6 , R C7 , R C8 , R C9 , R C10 , R C11 and R C12 At least one of represents a residue other than -H.

[0252] In some embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 7-membered cycloalkyl group; or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 7-membered heterocycloalkyl group. 3 Indicates -H, and R 4 Residues:

[0253]

[0254] In some embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl group (preferably a 3-, 4-, 5- or 6-membered cycloalkyl group); wherein the 3-14-membered cycloalkyl group is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linked; or saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl (preferably 4, 5 or 6 membered heterocycloalkyl); wherein the 3-14 membered heterocycloalkyl is linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linked; or unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl (preferably 6-membered aryl); wherein the 6-14 membered aryl is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linked; or unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl (preferably 5- or 6-membered heteroaryl); wherein the 5-14 membered heteroaryl is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linkage. In a preferred embodiment, R 3 Indicates -H, and R 4 represents a residue selected from the group consisting of:

[0255]

[0256]

[0257] In some embodiments, R 3 Indicates -H, and R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 5-membered heterocycloalkyl group; wherein the 5-membered heterocycloalkyl group is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linked; or unsubstituted, monosubstituted or polysubstituted 5-membered heteroaryl; wherein the 5-membered heteroaryl is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linkage.

[0258] In some embodiments, R 3 Indicates -H, and R4 represents a residue selected from the group consisting of:

[0259]

[0260] In some embodiments, R 3 Indicates -H, and R 4 express

[0261] (i) Residue -CR'R"-(CH 2 ) m -OH, wherein m is an integer from 1 to 6, preferably from 1 to 3; and wherein R' and R" independently represent -H, -C 1-3 -alkyl, -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. In one embodiment, at least R' or R" does not represent -H. In one embodiment, neither R' or R" represents -H; or

[0262] (ii) a residue according to formula (D),

[0263]

[0264] in

[0265] m D and n D are independently 0, 1, 2 or 3; preferably, m D +n D ≤3;

[0266] Y D1 Selected from -O-, -S(=O) 2 -, -S(=O)(=NH)-, -NR D8 -and-CR D9 R D10 -, and Y D2 Indicates -CR D11 R D12 -; or Y D1Selected from -O-, -S(=O) 2 -、-NR D8 -and-CR D9 R D10 -, and Y D2 Indicates -CR D11 R D12 -; or Y D1 Indicates -CR D9 R D10 -, and Y D2 Selected from -O-, -S(=O) 2 -and-NR D8 -;

[0267] R D1 , R D2 , R D3 , R D4 , R D5 , R D6 , R D7 , R D8 , R D9 , R D10 , R D11 and R D12 Independently represent -H, -F, -OH, -C 1-3 -alkylene-OH, -C(=O)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 D3 Together they represent =O; or R D4 and R D5 Together they represent =O; or R D9 and R D10 Together they represent =O; or R D11 and R D12 Together they represent =O;

[0268] Preferably,

[0269] m D and n D are independently 0, 1, 2 or 3; preferably, m D +n D ≤3;

[0270] Y D1 Selected from -O-, -NR D8 -and-CR D9 R D10 -, and Y D2 Indicates -CR D11 R D12 -; or Y D1 Indicates -CR D9 R D10 -, and Y D2 Selected from -O- and -NR D8 -;

[0271] R D1 , R D2 , R D3 , R D4 , R D5 , R D6 , R D7 , R D8 , R D9 , R D10 , R D11 and R D12 Independently represent -H, -F, -OH, -C 1-3 -alkylene-OH, -C(=O)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 D3 Together they represent =O; or R D4 and R D5 Together they represent =O; or R D9 and R D10 Together they represent =O; or R D11 and R D12 Together they represent =O; preferably the condition is R D1 , R D2 , R D3 , R D4 , R D5, R D6 , R D7 , R D8 , R D9 , R D10 , R D11 and R D12 Only 1, 2 or 3 of them represent residues other than -H; preferably, the condition is that R D1 , R D2 , R D3 , R D4 , R D5 , R D6 , R D7 , R D8 , R D9 , R D10 , R D11 and R D12 At least one of represents a residue other than -H.

[0272] In some embodiments, R 3 Indicates -H, and R 4 represents a residue selected from the group consisting of:

[0273]

[0274]

[0275] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 5 and R 5 'Independently express

[0276] -H;

[0277] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0278] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0279] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0280] In some embodiments, R 5 and R5 ' represents -H, -C independently of each other 1 -C 6 -alkyl or -C 1 -C 6 -alkylene-N(C 1 -C 6 -alkyl) 2 .

[0281] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 5 and R 5 At least one of ' is not -H.

[0282] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 5 and R 5 'Both are -H.

[0283] In some embodiments, T represents -O-, and U represents -CR 5 R 5 '-, and the resulting part -O-CR 5 R 5 '- represents a residue selected from the group consisting of:

[0284]

[0285] In some embodiments, T represents -CR 5 R 5 '-, and U represents -O-, and the resulting part -CR 5 R 5 '-O- indicates residue:

[0286]

[0287] In some embodiments, R 5 Indicates -H, and R 5 ' means 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 and -C 1-3 -alkylene-OH group consisting of residues; preferably -H or C 1-3 -alkyl.

[0288] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 6 , R 7 and R 8 Independently express

[0289] -H;

[0290] -F, -Cl, -Br, -I, -OH, -SH, -SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 ;

[0291] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl;

[0292] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 -alkyl;

[0293] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -NHC 1-6 -alkyl;

[0294] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C 1-6 -alkyl) 2 ;

[0295] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 -alkyl;

[0296] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC(=O)C 1-6 -alkyl;

[0297] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -heteroalkyl.

[0298] In some embodiments, R 6 , R 7 and R 8 Independently express

[0299] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 ,

[0300] -C 1-6 -alkyl, -CF 3 , -CHF2 、-CH 2 F.

[0301] -OC 1-6 -alkyl, -OCF 3 、-OCHF 2 、-OCH 2 F.

[0302] -NHC 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 Substituents are substituted;

[0303] -N(C 1-6 -alkyl) 2 , which is unsubstituted or is substituted by one or more independently selected from -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 Substituents are substituted;

[0304] -C(=O)OC 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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, -NH2 and -C(=O)NH 2 Substituents are substituted;

[0305] -OC(=O)C 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 or

[0306] -C 1-6 -heteroalkyl, which is unsubstituted or substituted by one or more independently selected from -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 by a substituent.

[0307] In some embodiments, R 6 , R 7 and R 8 Each independently represents a group consisting of -H, -F, -Cl, -Br, -I, -CN, C 1-3 -alkyl, -CF 3 , -CF 2 H and -CFH 2 A residue from the group consisting of: -H or -F.

[0308] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 6 Indicates -H, -F, -Cl, -CN or -C 1 -C 6 -alkyl.

[0309] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 6 -H is not indicated.

[0310] In some embodiments, R 6 Indicates a group selected from -H, -F, -Cl, -CN or -CH 3 The residue of the group consisting of: -H, -F, -CN or -CH 3 .

[0311] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 7 Indicates -H, -F, -Cl, -CN or -C 1 -C 6 -alkyl.

[0312] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 7 -H is not indicated.

[0313] In some embodiments, especially when Q represents -NR 3 R 4 When R 7 Indicates a group selected from -H, -F, -Cl, -CN or CH 3 The residues that make up the group.

[0314] In some embodiments, especially when Q represents -OR 2 When R 7 represents a residue selected from the group consisting of: -H or

[0315]

[0316] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 8 Indicates -H, -F, -Cl, -CN or -C 1 -C 6 -alkyl.

[0317] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention, R 8 -H is not indicated.

[0318] In some embodiments, R 8 Indicates a group selected from -H, -F, -Cl, -CN or CH 3 The residue of the group consisting of: 。

[0319] In some embodiments of the pyrazolo[1,5-a]pyridine derivatives according to the present invention

[0320] (i)R 6 , R 7 and R 8 Each represents -H; or

[0321] (ii) R 6 , R 7 and R 8 The two in it represent -H, and R 6 , R 7 and R 8 The other one of the above represents -F, -Cl, -CN or -CH 3 ;or

[0322] (iii) R 6 , R 7 and R 8 One of them represents -H, and R 6 , R 7 and R 8 The other of each independently represents -F, -Cl, -CN or -CH 3 .

[0323] In some embodiments, the compound is according to formula (I), wherein

[0324] -R 1 Indicates -CH 3 ; and / or

[0325] -R 6 , R 7 and R 8 each represents -H; and / or

[0326] -T means -O-; and / or

[0327] -U means -CH 2 -; and / or

[0328] -V represents thiazolyl, pyridinyl or pyrazolyl; wherein the thiazolyl, pyridinyl and pyrazolyl are each independently unsubstituted, selected from -CH 3 ;-F;-CH 2 CHF 2 ; and -CF 3 The substituents of the group consisting of are mono- or di-substituted; and / or

[0329] -Q means NR 3 R 4 ; and / or

[0330] -R 3 means H; and / or

[0331] -R 4 express

[0332] In an exemplary embodiment of the present invention, the pyrazolo[1,5-a]pyridine derivative is selected from the group consisting of:

[0333] Cpd 001-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-2-(hydroxymethyl)butanamide;

[0334] Cpd 002-N-(1,3-dihydroxy-2-methylpropan-2-yl)-5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridine-3-carboxamide;

[0335] Cpd 003-(2S)-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxypropanamide;

[0336] Cpd 004-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-2-methylpropanamide;

[0337] Cpd 005-5-[(2-fluorophenyl)methoxy]-N-(2-methylsulfonamidoethyl)-2-methylpyrazolo[1,5-a]pyridine-3-carboxamide;

[0338] Cpd 006-N-(2,2-difluoroethyl)-5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridine-3-carboxamide;

[0339] Cpd 007-(2S,3R)-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxybutanamide;

[0340] Cpd 008-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide;

[0341] Cpd 009-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-N-methylpropanamide;

[0342] Cpd 010-(2S)-3-hydroxy-2-({2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]pyrazolo[1,5-a]pyridin-3-yl}carboxamido)propanamide;

[0343] Cpd 011-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-N,2-dimethylpropanamide;

[0344] Cpd 012-(2S)-2-({5-[(2-chlorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxypropanamide;

[0345] Cpd 013-2-({5-[(2-chlorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-2-methylpropanamide;

[0346] Cpd 014-5-[(2-chlorophenyl)methoxy]-N-(1,3-dihydroxy-2-methylpropan-2-yl)-2-methylpyrazolo[1,5-a]pyridine-3-carboxamide;

[0347] Cpd 015-2-{[5-(2,2-difluoroethoxy)-2-methylpyrazolo[1,5-a]pyridin-3-yl]formamido}-3-hydroxy-2-methylpropanamide;

[0348] Cpd 016-2-{[5-(Benzyloxy)-2-methylpyrazolo[1,5-a]pyridin-3-yl]formamido}-3-hydroxy-2-methylpropanamide;

[0349] Cpd 017-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-N,N,2-trimethylpropanamide;

[0350] Cpd 018-5-[(2-fluorophenyl)methoxy]-N-[3-(hydroxymethyl)-2-oxopyrrolidin-3-yl]-2-methylpyrazolo[1,5-a]pyridine-3-carboxamide;

[0351] Cpd 019-2-({5-[(2-chlorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0352] Cpd 020-2-({5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0353] Cpd 021-3-hydroxy-2-methyl-2-({2-methyl-5-[(6-methylpyridin-3-yl)methoxy]pyrazolo[1,5-a]pyridin-3-yl}carboxamido)propanamide;

[0354] Cpd 022-2-{[5-(cyclopropylmethoxy)-2-methylpyrazolo[1,5-a]pyridin-3-yl]formamido}-3-hydroxy-2-methylpropanamide;

[0355] Cpd 023-2-[(5-{[2-(difluoromethyl)phenyl]methoxy}-2-methylpyrazolo[1,5-a]pyridin-3-yl)formamido]-3-hydroxy-2-methylpropanamide;

[0356] Cpd 024-2-(1-{5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}-N-methylformamido)-3-hydroxy-2-methylpropanamide;

[0357] Cpd 025-N-(4,4-difluoro-1-hydroxy-2-methylbutan-2-yl)-5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridine-3-carboxamide;

[0358] Cpd 026-2-({5-[(2,4-difluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0359] Cpd 027-2-({5-[(2,3-difluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0360] Cpd 028-2-({5-[(2-fluoro-4-methylphenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0361] Cpd 029-2-({5-[(2-fluoro-3-methylphenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0362] Cpd 030-2-({5-[(2,5-difluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0363] Cpd 031-2-({5-[(2-fluoro-6-methylphenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0364] Cpd 032-2-({5-[(2,6-difluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridin-3-yl}carboxamido)-3-hydroxy-2-methylpropanamide;

[0365] Cpd 033-5-(Benzyloxy)-2-methylpyrazolo[1,5-a]pyridine-3-carboxylic acid;

[0366] Cpd 034-5-(Cyclopropylmethoxy)-2-methylpyrazolo[1,5-a]pyridine-3-carboxylic acid;

[0367] Cpd 035-5-[(2-fluorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridine-3-carboxylic acid;

[0368] Cpd 036-5-[(2-chlorophenyl)methoxy]-2-methylpyrazolo[1,5-a]pyridine-3-carboxylic acid;

[0369] Cpd 037-N-(4,4-difluoro-1-hydroxy-2-methylbutan-2-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide;

[0370] Cpd 038-N-(4,4-difluoro-1-hydroxy-2-methylbutan-2-yl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0371] Cpd 042-2-methyl-5-[(pyridin-2-yl)methoxy]-N-(2,2,2-trifluoroethyl)pyrazolo[1,5-a]pyridine-3-carboxamide,

[0372] Cpd 043-N-(2-hydroxyethyl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0373] Cpd 044-N-[(1H-imidazol-2-yl)methyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0374] Cpd 045-N-[3-(dimethylamino)-2,2-dimethylpropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0375] Cpd 046-N-(2,2-difluoro-2-phenylethyl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0376] Cpd 047-N-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0377] Cpd 048-N-{[3-(difluoromethoxy)phenyl]methyl}-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0378] Cpd 049-N-(4,4-difluoropiperidin-3-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0379] Cpd 050-N-(4,4-difluoropiperidin-3-yl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0380] Cpd 051-N-(5,5-difluoropiperidin-3-yl)-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0381] Cpd 052-N-(5,5-difluoropiperidin-3-yl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0382] Cpd 053-2-methyl-5-[(4-methyl-1,3-thiazol-5-yl)methoxy]-N-(pyrrolidin-3-yl)pyrazolo[1,5-a]pyridine-3-carboxamide,

[0383] Cpd 054-2-methyl-5-[(pyridin-2-yl)methoxy]-N-(pyrrolidin-3-yl)pyrazolo[1,5-a]pyridine-3-carboxamide,

[0384] Cpd 055-N-[3,3-difluoro-1-(hydroxymethyl)cyclobutyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0385] Cpd 056-N-[2-hydroxy-5-(trifluoromethyl)pyridin-3-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0386] Cpd 057-N-[5-(hydroxymethyl)-2,2-dimethyl-1,3-dioxane-5-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0387] Cpd 058-N-[1-(4-fluorophenyl)-2-hydroxyethyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0388] Cpd 059-N-[2-hydroxy-1-(pyridin-2-yl)ethyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0389] Cpd 061-N-[1-(4-fluorophenyl)-3-hydroxypropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0390] Cpd 062-2-methyl-5-[(pyridin-2-yl)methoxy]-N-(4,4,4-trifluoro-1-hydroxybutan-2-yl)pyrazolo[1,5-a]pyridine-3-carboxamide,

[0391] Cpd 063-2-methyl-5-[(pyridin-2-yl)methoxy]-N-[4,4,4-trifluoro-1-hydroxy-3-(trifluoromethyl)butan-2-yl]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0392] Cpd 064-N-(4,4-difluoro-1-hydroxybutan-2-yl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0393] Cpd 066-N-(4,4-difluoro-1-methoxy-2-methylbutan-2-yl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0394] Cpd 068-N-(1-hydroxy-2-methyl-3-oxobutan-2-yl)-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0395] Cpd 071-N-[2,2-difluoro-1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0396] Cpd 071A-N-[cis-2,2-difluoro-1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0397] Cpd 071B-N-[trans-2,2-difluoro-1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0398] Cpd 072-N-[cis-2-(difluoromethyl)-1-(hydroxymethyl)cyclopropyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0399] Cpd 074-N-[1-(1-cyclopropyl-1H-imidazol-2-yl)-2-hydroxyethyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0400] Cpd 075-N-[1-hydroxy-2-(1-methyl-1H-pyrazol-3-yl)propan-2-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0401] Cpd 076-(R)-4-hydroxy-3-({2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridin-3-yl}formamido)butanamide,

[0402] Cpd 077-N-[2-hydroxy-1-(oxan-4-yl)ethyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0403] Cpd 079-N-[1-hydroxy-3-(pyrimidin-2-yl)propan-2-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0404] Cpd 079A-(R)-N-[1-hydroxy-3-(pyrimidin-2-yl)propan-2-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0405] Cpd 079B-(S)-N-[1-hydroxy-3-(pyrimidin-2-yl)propan-2-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0406] Cpd 081-2-methyl-5-[(pyridin-2-yl)methoxy]-N-(4,4,4-trifluoro-2-hydroxybutyl)pyrazolo[1,5-a]pyridine-3-carboxamide,

[0407] Cpd 082-2-methyl-5-[(pyridin-2-yl)methoxy]-N-[4-(trifluoromethyl)pyrrolidin-3-yl]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0408] Cpd 082A-2-methyl-5-[(pyridin-2-yl)methoxy]-N-[cis-4-(trifluoromethyl)pyrrolidin-3-yl]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0409] Cpd 082B-2-methyl-5-[(pyridin-2-yl)methoxy]-N-[trans-4-(trifluoromethyl)pyrrolidin-3-yl]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0410] Cpd 084-N-[3-(2,2-difluoroethyl)piperidin-3-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0411] Cpd 087-N-[2-hydroxy-1-(1-methyl-1H-pyrazol-3-yl)ethyl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0412] Cpd 088-N-[1-hydroxy-3-(pyridin-2-yl)propan-2-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0413] Cpd 089-3-hydroxy-2-methyl-2-({2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridin-3-yl}carboxamido)propanamide,

[0414] Cpd 090-2-methyl-5-[(pyridin-2-yl)methoxy]-N-(1,1,1-trifluoro-3-hydroxypropan-2-yl)pyrazolo[1,5-a]pyridine-3-carboxamide,

[0415] Cpd 091-N-[3-(hydroxymethyl)-2-oxopyrrolidin-3-yl]-2-methyl-5-[(pyridin-2-yl)methoxy]pyrazolo[1,5-a]pyridine-3-carboxamide,

[0416] The pyrazolo[1,5-a]pyridine derivatives according to the present invention are used for treating pain, which is preferably selected from nociceptive pain, inflammatory pain and neuropathic pain. More preferably, the pain is postoperative pain. The pyrazolo[1,5-a]pyridine derivatives according to the present invention are used for treating epilepsy.

[0417] In some embodiments, the pyrazolo[1,5-a]pyridine derivative is selected from the group consisting of compounds 001-091 shown in Table 1 below, including stereoisomers and pharmaceutically acceptable salts thereof:

[0418] Table 1: Exemplary pyrazolo[1,5-a]pyridine derivatives

[0419]

[0420]

[0421] In some embodiments, the pyrazolo[1,5-a]pyridine derivative is selected from the group consisting of compounds 037-088 shown in Table 2 below, including stereoisomers and pharmaceutically acceptable salts thereof:

[0422] Table 2: Exemplary pyrazolo[1,5-a]pyridine derivatives

[0423]

[0424]

[0425]

[0426]

[0427]

[0428]

[0429] Q, T, U, V, R including the disclosed substituents 1 , R 2 , R 3 , R 4 , R 5 , R5 '、R 6 , R 7 and R 8 All definitions, embodiments and meanings of also apply similarly to the pyrazolo[1,5-a]pyridine derivatives according to the present invention, including but not limited to (a-1), (a-2), (a-3), (b-1), (b-2) and (b-3), which are not necessarily limited to use for the treatment of pain. Therefore, this aspect of the invention relates to pyrazolo[1,5-a]pyridine derivatives themselves, compositions comprising pyrazolo[1,5-a]pyridine derivatives, medicaments comprising pyrazolo[1,5-a]pyridine derivatives, and pyrazolo[1,5-a]pyridine derivatives for preventing and / or treating TRPM3-mediated conditions such as pain and / or inflammatory hypersensitivity and / or epilepsy; and / or pyrazolo[1,5-a]pyridine derivatives for combating pain and / or inflammatory hypersensitivity and / or epilepsy. Preferably, the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain. More preferably, the pain is postoperative pain.

[0430] In some embodiments of the present invention, the pyrazolo[1,5-a]pyridine derivative is selected from the group consisting of cpd001 to cpd 036 as described above and physiologically acceptable salts thereof.

[0431] In some embodiments of the present invention, the pyrazolo[1,5-a]pyridine derivative is selected from the group consisting of cpd037 to cpd091 as described above and physiologically acceptable salts thereof.

[0432] Another aspect of the present invention relates to a pharmaceutical composition or a medicament comprising a compound according to the invention as described above.

[0433] Mentioning "one embodiment" or "an embodiment" throughout the specification means that the specific features, structures or characteristics described in conjunction with the embodiment are included in at least one embodiment of the present invention. Therefore, the phrases "in one embodiment" or "in an embodiment" that appear in various places throughout the specification do not necessarily all refer to the same embodiment, but may refer to the same embodiment. In addition, in one or more embodiments, specific features, structures or characteristics may be combined in any suitable manner, which will be apparent to those of ordinary skill in the art from this disclosure. In addition, the embodiments described for one aspect of the present invention may be used for another aspect of the present invention, and may be combined. Indefinite or definite articles are used when referring to singular nouns, such as "a / an", "the", unless otherwise specifically stated, this includes the plural form of the noun.

[0434] Similarly, it should be appreciated that in the description of exemplary embodiments of the invention, various features of the invention are sometimes combined in a single embodiment, figure, or description thereof for the purpose of simplifying the disclosure and aiding in the understanding of one or more of the various inventive aspects.

[0435] In each of the following definitions, the number of carbon atoms represents the maximum number of carbon atoms that is generally optimally present in a substituent or linker; it is understood that where otherwise indicated in this application, the number of carbon atoms represents the optimal maximum number of carbon atoms for that particular substituent or linker.

[0436] As used herein, the term "leaving group" or "LG" means a chemical group that is easily displaced or cleaved or hydrolyzed by a nucleophile under basic or acidic conditions. In a specific embodiment, the leaving group is selected from a halogen atom (e.g., Cl, Br, I) or a sulfonate (e.g., mesylate, tosylate, triflate).

[0437] The term "protecting group" refers to a part of a compound that masks or changes the properties of a functional group or the properties of the compound as a whole. The chemical substructure of a protecting group varies greatly. One function of a protecting group is to act as an intermediate in the synthesis of a parent drug substance. Chemical protecting groups and protection / deprotection strategies 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 generally used to mask the reactivity of certain functional groups to aid in the efficiency of desired chemical reactions, such as forming and destroying chemical bonds in an orderly and planned manner. The protection of the functional groups of a compound changes other physical properties, such as polarity, lipophilicity (hydrophobicity), and other properties that can be measured by common analytical tools, in addition to the reactivity of the protected functional groups. The chemically protected intermediates themselves can be biologically active or inactive.

[0438] Protected compounds can also show changes in vitro and in vivo, and in some cases, show optimized properties, such as resistance to enzymatic degradation or chelation through cell membranes and. In this effect, protected compounds with expected therapeutic effects can be referred to as prodrugs. Another function of protecting groups is to convert the parent drug into prodrugs, thus releasing the parent drug when converting the prodrug in vivo. Because active prodrugs may be more effectively absorbed than parent drugs, prodrugs may have greater efficacy than parent drugs in vivo. In the case of chemical intermediates, protecting groups are removed in vitro, or in the case of prodrugs, protecting groups are removed in vivo. For chemical intermediates, it is not particularly important that the product (e.g., alcohol) obtained after deprotection is physiologically acceptable, although it is usually more desirable that the product is pharmacologically harmless.

[0439] As used herein, the term "heteroatom" means an atom selected from nitrogen, which may be quaternized or present as an oxide; oxygen; and sulfur, including oxidized sulfur, including sulfoxides and sulfones, and in some cases sulfonates. In some cases, compounds and / or synthetic intermediates may include heteroatoms such as boron, phosphorus and silicon.

[0440] As used herein, the term "saturated or unsaturated alkyl" includes saturated alkyl as well as unsaturated alkyl, such as alkenyl, alkynyl, etc. As used herein, the term "alkyl" means a normal, secondary or tertiary straight or branched chain hydrocarbon having no unsaturated sites. Examples are methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl (i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl and 3,3-dimethyl-2-butyl. As used herein, the term "alkenyl" means a normal, secondary or tertiary straight or branched chain hydrocarbon having at least one (usually 1 to 3, preferably 1) unsaturated site (i.e., carbon-carbon sp2 double bond). Examples include, but are not limited to, 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 can be in cis or trans configuration. As used herein, the term "alkynyl" means a normal, secondary or tertiary straight or branched chain hydrocarbon having at least one (usually 1 to 3, preferably 1) site of unsaturation (i.e., a carbon-carbon sp triple bond). Examples include, but are not limited to, ethynyl (-C≡CH) and 1-propynyl (propargyl, -CH 2 C≡CH).

[0441] As used herein, the term "saturated or unsaturated alkylene" includes saturated alkylene and unsaturated alkylene, such as alkenylene, alkynylene, alkenylene, etc. As used herein, the term "alkylene" means a saturated, straight-chain or branched hydrocarbon group having two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkane. Typical alkylene groups include, but are not limited to, methylene (-CH 2-), 1,2-ethyl (-CH 2 CH 2 -), 1,3-propyl (-CH 2 CH 2 CH 2 -), 1,4-butyl (-CH 2 CH 2 CH 2 CH 2 -) etc. As used herein, the term "alkenylene" means a straight or branched hydrocarbon group having at least one (usually 1 to 3, preferably 1) unsaturated site (i.e., carbon-carbon sp2 double bond) and two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkene. As used herein, the term "alkynylene" means a straight or branched hydrocarbon group having at least one (usually 1 to 3, preferably 1) unsaturated site (i.e., carbon-carbon sp2 triple bond) and two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkyne.

[0442] As used herein, the term "saturated or unsaturated heteroalkyl" includes saturated heteroalkyl and unsaturated heteroalkyl, such as heteroalkenyl, heteroalkynyl, heteroalkenynyl, etc. As used herein, the term "heteroalkyl" means a straight or branched chain alkyl in which one or more carbon atoms (usually 1, 2 or 3) are replaced by heteroatoms (i.e., oxygen, nitrogen or sulfur atoms), provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. This means that one or more -CH 3 Can be -NH 2 Replace and / or one or more -CH 2 - can be replaced by -NH-, -O- or -S-. The S atom in the chain can be optionally oxidized by one or two oxygen atoms to give sulfoxides and sulfones, respectively. In addition, the heteroalkyl group in the pyrazolo[1,5-a]pyridine derivatives of the present invention can contain an oxo group or a thio group on any carbon or heteroatom, which will produce a stable compound. Exemplary heteroalkyl groups include, but are not limited to, alcohols, alkyl ethers (e.g., -methoxy, -ethoxy, -butoxy...), primary, secondary and tertiary alkylamines, amides, ketones, esters, alkyl sulfides and alkyl sulfones. The term "heteroalkenyl" means a straight or branched alkenyl group in which one or more carbon atoms (usually 1, 2 or 3) are replaced by oxygen, nitrogen or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Therefore, the term heteroalkenyl includes imines, -O-alkenyls, -NH-alkenyls, -N(alkenyls) 2, -N(alkyl)(alkenyl) and -S-alkenyl. As used herein, the term "heteroalkynyl" means a straight or branched chain alkynyl group in which one or more carbon atoms (usually 1, 2 or 3) are replaced by oxygen, nitrogen or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Thus, the term heteroalkynyl includes -cyano, -O-alkynyl, -NH-alkynyl, -N(alkynyl) 2 , -N(alkyl)(alkynyl), -N(alkenyl)(alkynyl), and -S-alkynyl.

[0443] As used herein, the term "saturated or unsaturated heteroalkylene" includes saturated heteroalkylene and unsaturated heteroalkylene, such as heteroalkenylene, heteroalkynylene, heteroalkenylynylene, etc. As used herein, the term "heteroalkylene" means a straight or branched chain alkylene group in which one or more carbon atoms (usually 1, 2 or 3) are replaced by heteroatoms (i.e., oxygen, nitrogen or sulfur atoms), provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein, the term "heteroalkenylene" means a straight or branched chain alkenylene group in which one or more carbon atoms (usually 1, 2 or 3) are replaced by oxygen, nitrogen or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein, the term "heteroalkynylene" means a straight or branched chain alkynylene group in which one or more carbon atoms (usually 1, 2 or 3) are replaced by oxygen, nitrogen or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms.

[0444] As used herein, the term "saturated or unsaturated cycloalkyl" includes saturated cycloalkyl and unsaturated cycloalkyl, such as cycloalkenyl, cycloalkynyl, etc. As used herein and unless otherwise specified, the term "cycloalkyl" means a saturated cyclic hydrocarbon group, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, norbornyl, fenchyl, decalinyl, adamantyl, etc. As used herein, the term "cycloalkenyl" means a non-aromatic cyclic hydrocarbon group having at least one (usually 1 to 3, preferably 1) unsaturated site (i.e., carbon-carbon sp2 double bond). Examples include, but are not limited to, cyclopentenyl and cyclohexenyl. The double bond can be a cis or trans configuration. As used herein, the term "cycloalkynyl" means a non-aromatic cyclic hydrocarbon group having at least one (usually 1 to 3, preferably 1) unsaturated site (i.e., carbon-carbon sp triple bond). An example is cyclohept-1-yne. The fused system of a cycloalkyl ring and a heterocycloalkyl ring is considered to be a heterocycloalkyl, regardless of the ring attached to the core structure. The fused system of a cycloalkyl ring and an aryl ring is considered to be an aryl, regardless of the ring attached to the core structure. The fused system of a cycloalkyl ring and a heteroaryl ring is considered to be a heteroaryl, regardless of the ring attached to the core structure.

[0445] As used herein, the term "saturated or unsaturated heterocycloalkyl" includes saturated heterocycloalkyl and unsaturated non-aromatic heterocycloalkyl containing at least one heteroatom (i.e., N, O or S) as a ring member. As used herein and unless otherwise specified, the term "heterocycloalkyl" means a "cycloalkyl" in which one or more carbon atoms (usually 1, 2 or 3) are replaced by oxygen, nitrogen or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein and unless otherwise specified, the term "heterocycloalkenyl" means a "cycloalkenyl" in which one or more carbon atoms (usually 1, 2 or 3) are replaced by oxygen, nitrogen or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. As used herein and unless otherwise specified, the term "heterocycloalkynyl" means a "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 may not contain two adjacent O atoms or two adjacent S atoms. Examples of saturated and unsaturated heterocycloalkyl groups include, but are not limited to, azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiophene ... Heterocyclopropane, thiolane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothiananes, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine.Other heterocycloalkyl groups 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 date), in particular Volumes 13, 14, 16, 19 and 28; Katritzky, Alan R., Rees, CW and Scriven, E. "Comprehensive Heterocyclic Chemistry" (Pergamon Press, 1996); and J. Am. Chem. Soc. (1960) 82: 5566. When the heterocycloalkyl group does not contain nitrogen as a ring member, it is usually bonded via carbon. When the heterocycloalkyl group contains nitrogen as a ring member, it can be bonded via nitrogen or carbon. The fused system of a heterocycloalkyl ring with a cycloalkyl ring is considered to be a heterocycloalkyl, regardless of the ring attached to the core structure. The fused system of a heterocycloalkyl ring with an aryl ring is considered to be a heterocycloalkyl, regardless of the ring attached to the core structure. The fused system of a heterocycloalkyl ring with a heteroaryl ring is considered to be a heteroaryl, regardless of the ring attached to the core structure.

[0446] As used herein, the term "aryl" means an aromatic hydrocarbon. Typical aryl groups include, but are not limited to, one ring, or two or three rings fused together, derived from groups such as benzene, naphthalene, anthracene, biphenyl, etc. The fused system of an aryl ring and a cycloalkyl ring is considered to be an aryl group, regardless of the ring that is attached to the core structure. The fused system of an aryl ring and a heterocycloalkyl ring is considered to be a heterocycloalkyl group, regardless of the ring that is attached to the core structure. Therefore, indoline, dihydrobenzofuran, dihydrobenzothiophene, etc. are considered to be heterocycloalkyl groups according to the present invention. The fused system of an aryl ring and a heteroaryl ring is considered to be a heteroaryl group, regardless of the ring that is attached to the core structure.

[0447] As used herein, the term "heteroaryl" means an aromatic ring system comprising at least one heteroatom (i.e., N, O, or S) as a ring member of the aromatic ring system. Examples of heteroaryl groups include, but are not limited to, benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine.

[0448] As a further example, 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, pyrazole, 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.

[0449] Carbon-bonded heterocycles include 2-pyridyl, 3-pyridyl, 4-pyridyl, 5-pyridyl, 6-pyridyl, 3-pyridazinyl, 4-pyridazinyl, 5-pyridazinyl, 6-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 6-pyrimidinyl, 2-pyrazinyl, 3-pyrazinyl, 5-pyrazinyl, 6-pyrazinyl, 2-thiazolyl, 4-thiazolyl or 5-thiazolyl. For example, nitrogen-bonded heterocycles are bonded to the 1 position of aziridine, azetidine, pyrrole, pyrrolidine, 2-pyrroline, 3-pyrroline, imidazole, imidazoline, 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. Nitrogen-bonded heterocycles include 1-aziridine, 1-azetidinyl, 1-pyrrolyl, 1-imidazolyl, 1-pyrazolyl, and 1-piperidinyl. Other heteroaryl groups 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. W. and Scriven, E. "Comprehensive Heterocyclic Chemistry" (Pergamon Press, 1996); and J. Am. Chem. Soc. (1960) 82:5566.

[0450] As used herein with respect to substituents and unless otherwise indicated, the terms "monosubstituted", "disubstituted", "trisubstituted", "polysubstituted" and the like refer to chemical structures as defined herein in which the corresponding moiety is substituted with one or more substituents, meaning that one or more hydrogen atoms of the moiety are each independently replaced with a substituent. For example, -C 1-6 -alkyl groups include -CH 2 F, -CHF 2 , -CF 3 、-CH 2 CF 3 CF 2 CF 3 Likewise, -C may be polysubstituted by substituents independently selected from -F and -Cl.1-6 -alkyl groups include -CH 2 F, -CHF 2 , -CF 3 、-CH 2 CF 3 CF 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. The names of any substituents found in more than one position in a compound of the invention should be selected independently.

[0451] As used herein and unless otherwise specified, the term "solvate" includes any combination that may be formed by a derivative of the present invention and a suitable inorganic solvent (e.g., hydrate) or an organic solvent such as, but not limited to, alcohols, ketones, esters, ethers, nitriles, and the like.

[0452] As used herein, the term "subject" refers to an animal, including a human, preferably a mammal, and most preferably a human, that is the object of treatment, observation, or experiment.

[0453] As used herein, the term "therapeutically effective amount" means the amount of an active compound or agent that elicits a biological or medicinal response in a tissue system, animal or human that is sought by a researcher, veterinarian, medical doctor or other clinician, which includes alleviation or partial alleviation of the symptoms of the disease or condition being treated.

[0454] As used herein, the term "composition" is intended to encompass a product comprising the specified ingredients in therapeutically effective amounts, as well as any product which results, directly or indirectly, from combination of the specified ingredients in the specified amounts.

[0455] As used herein, the term "antagonist" or "inhibitor" refers to a compound that can produce a functional antagonism of the TRPM3 ion channel, including competitive antagonists, non-competitive antagonists, desensitizing agonists and partial agonists. Generally, "antagonists" and "inhibitors" can be understood as regulating TRPM3.

[0456] For the purposes of the present invention, the term "TRPM3-modulated" is used to refer to conditions that are affected by modulation of TRPM3 ion channels, including states that are modulated by TRPM3 ion channels.

[0457] As used herein, the term "TRPM3-mediated disorder" refers to a disorder or disease that uses an antagonist or modulator of TRPM3 to prevent, treat, (partially) alleviate or improve symptoms and is composed of pain, inflammatory hypersensitivity symptoms and epilepsy. According to the International Association for the Study of Pain and for the purposes of the present invention, pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or is described by such damage. Preferably, the TRPM3-mediated disorder is pain, which is preferably selected from nociceptive pain, inflammatory pain and neuropathic pain. More preferably, pain is postoperative pain. For the purposes of the present invention, the term "inflammatory hypersensitivity" is used to refer to a symptom characterized by one or more inflammatory markers (including edema, erythema, high fever and pain) and / or excessive physiological or pathophysiological reactions to one or more types of stimulation (including heat, mechanical and / or chemical stimulation).

[0458] The pyrazolo[1,5-a]pyridine derivatives of the present invention have been shown or understood to be antagonists or modulators of TRPM3, and therefore the present invention provides such compounds for use as drugs, more specifically as drugs for preventing or treating TRPM3-mediated disorders in a subject using a therapeutically effective amount of the pyrazolo[1,5-a]pyridine derivatives of the present invention.

[0459] In one embodiment of the present invention, the pyrazolo[1,5-a]pyridine derivative of the present invention is the only pharmacologically active compound for therapeutic administration. In another embodiment of the present invention, the pyrazolo[1,5-a]pyridine derivative of the present invention can be used in combination with other therapeutic agents for the treatment or prevention of TRPM3-mediated disorders. Therefore, the present invention also relates to the use of a composition comprising:

[0460] - one or more compounds of the formulae and embodiments herein, and

[0461] - One or more other therapeutic or prophylactic agents for preventing or treating TRPM3-mediated disorders, which are used simultaneously, separately or sequentially as biologically active agents in the form of a combined preparation.

[0462] The pharmaceutical composition or combined preparation according to the present invention may contain a wide range of content of the pyrazolo[1,5-a]pyridine derivative of the present invention, depending on the intended use and the intended effect of the preparation. Typically, the content of the pyrazolo[1,5-a]pyridine derivative of the present invention in the combined preparation is in the range of 0.1 to 99.9% by weight, preferably 1 to 99% by weight, and more preferably 5 to 95% by weight.

[0463] In view of the fact that when several active ingredients are used in combination, they do not necessarily exert their combined therapeutic effect directly in the mammal to be treated at the same time, the corresponding composition can also be in the form of a medical kit or package containing the two components in separate but adjacent containers or compartments. In the latter case, each active ingredient can therefore be formulated in a manner suitable for a route of administration different from that of the other ingredients, for example, one of them can be in the form of an oral or parenteral preparation, while the other is in the form of an ampoule or aerosol for intravenous injection.

[0464] Those skilled in the art will also recognize that the pyrazolo[1,5-a]pyridine derivatives of the present invention can exist in many different protonation states, depending on the pH of their environment, etc. Although the structural formulas provided herein only depict compounds in one of several possible protonation states, it should be understood that these structures are merely illustrative and the present invention is not limited to any particular protonation state - any and all protonated forms of the compounds are intended to fall within the scope of the present invention.

[0465] As used herein, the term "pharmaceutically acceptable salt" or "physiologically acceptable salt" refers to the therapeutically active non-toxic salt forms that the compounds of the formula herein are able to form. Therefore, the compounds of the present invention optionally include salts of the compounds herein, especially those containing, for example, Na + , Li + , K + , Ca 2+ and Mg 2+ Pharmaceutically acceptable non-toxic salts of. Such salts may include those derived by combining appropriate cations (such as alkali metal and alkaline earth metal ions or ammonium and quaternary ammonium ions) with acid anion moieties (usually carboxylic acids). The pyrazolo[1,5-a]pyridine derivatives of the present invention may carry multiple positive or negative charges. The net charge of the pyrazolo[1,5-a]pyridine derivatives of the present invention may be positive or negative. Any associated counterions are generally determined by the synthesis and / or separation methods used to obtain the compound. Typical counterions include, but are not limited to, ammonium, sodium, potassium, lithium, halides, acetates, trifluoroacetates, and the like and mixtures thereof. It should be understood that the identity of any associated counterions is not a critical feature of the present invention, and the present invention includes compounds associated with any type of counterions. In addition, since the compounds may exist in a variety of different forms, the present invention is intended to include not only compound forms associated with counterions (e.g., dry salts), but also forms not associated with counterions (e.g., aqueous solutions or organic solutions). Metal salts are generally prepared by reacting metal hydroxides with compounds of the present invention. Examples of metal salts prepared in this manner are those containing Li + 、Na + and K +Salt. By adding a suitable metal compound, a less soluble metal salt can be precipitated from a solution of a more soluble salt. In addition, salts can be formed by acid addition of certain organic and inorganic acids with a basic center (usually an amine) or an acidic group. Examples of such suitable acids include, for example, inorganic acids such as hydrohalic acids, such as hydrochloric acid or hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, etc.; or organic acids, such as acetic acid, propionic acid, glycolic acid, 2-hydroxypropionic acid, 2-oxopropionic acid, lactic acid, pyruvic acid, oxalic acid (i.e., ethylene glycol), malonic acid, succinic acid (i.e., succinic acid), maleic acid, fumaric acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, cyclohexanesulfonic acid, salicylic acid (i.e., 2-hydroxybenzoic acid), p-aminosalicylic acid, etc. In addition, the term also includes compounds of the formula herein and solvates that their salts can form, such as hydrates, alcoholates, etc. Finally, it is to be understood that the compositions herein comprise the pyrazolo[1,5-a]pyridine derivatives of the present invention in unionized and zwitterionic form, as well as in hydrated form in combination with a stoichiometric amount of water.

[0466] Also included within the scope of the invention are salts of the parent compound with one or more amino acids, especially naturally occurring amino acids found as protein components. The amino acids are typically amino acids with side chains having basic or acidic groups, such as lysine, arginine or glutamic acid, or neutral groups, such as glycine, serine, threonine, alanine, isoleucine or leucine.

[0467] The pyrazolo[1,5-a]pyridine derivatives of the present invention also include physiologically acceptable salts thereof. Examples of physiologically acceptable salts of the pyrazolo[1,5-a]pyridine derivatives of the present invention include salts derived from appropriate bases, such as alkali metals (e.g., sodium), alkaline earth metals (e.g., magnesium), ammonium and NX4. + (Where X is -C 1-6 Physiologically acceptable salts of compounds containing hydroxyl groups include salts of organic carboxylic acids such as acetic acid, benzoic acid, lactic acid, fumaric acid, tartaric acid, maleic acid, malonic acid, malic acid, isethionic acid, lactobionic acid and succinic acid; organic sulfonic acids such as methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid and p-toluenesulfonic acid; and inorganic acids such as hydrochloric acid, sulfuric acid, phosphoric acid and aminosulfonic acid. Physiologically acceptable salts of compounds containing hydroxyl groups include salts of the anion of the compound with a suitable cation such as Na + and NX4 + (wherein X is generally independently selected from -H or -C 1-4 -alkyl). However, salts of physiologically unacceptable acids or bases may also be used, for example, to prepare or purify physiologically acceptable compounds. All salts, whether or not derived from physiologically acceptable acids or bases, are within the scope of the present invention.

[0468] As used herein and unless otherwise indicated, the term "enantiomer" means each individual optically active form of a pyrazolo[1,5-a]pyridine derivative of the invention having an optical purity or enantiomeric excess (as determined by standard methods in the art) of at least 80% (i.e., at least 90% of one enantiomer and at most 10% of the other enantiomer), preferably at least 90%, and more preferably at least 98%.

[0469] As used herein, the term "isomer" means all possible isomeric forms, including tautomeric forms and stereochemical forms, which the compounds of the formula herein may have, but do not include positional isomers. Typically, the structures shown herein illustrate only one tautomeric form or resonance form of the compound, but corresponding alternative configurations are also contemplated. Unless otherwise indicated, the chemical name of the compound represents a mixture of all possible stereochemical isomeric forms, the mixture containing all diastereomers and enantiomers of the basic molecular structure (because the compounds of the formula herein can have at least one chiral center), as well as stereochemically pure or enriched compounds. More particularly, stereocenters can have R- or S- configurations, and multiple bonds can have cis or trans configurations.

[0470] Pure isomeric forms of the compounds are defined as isomers that are substantially free of other enantiomeric or diastereomeric forms of the same basic molecular structure. In particular, the terms "stereoisomerically pure" or "chirally pure" relate to compounds having a stereoisomeric excess of at least about 80% (i.e., at least 90% of one isomer and up to 10% of other possible isomers), preferably at least 90%, more preferably at least 94%, and most preferably at least 97%. The terms "enantiomerically pure" and "diastereomerically pure" should be understood in a similar manner, taking into account the enantiomeric excess and diastereomeric excess, respectively, of the mixture in question.

[0471] Separation of stereoisomers is accomplished by standard methods known to those skilled in the art. One enantiomer of the pyrazolo[1,5-a]pyridine derivative of the present invention can be separated by methods such as forming diastereomers using an optically active resolving agent, without substantially containing its opposite enantiomer (EL Elliel's "Stereochemistry of Carbon Compounds," (1962), McGraw Hill; Lochmuller, CH, (1975) J. Chromatogr., 113: (3) 283-302). Separation of isomers in a mixture can be accomplished by any suitable method, including: (1) forming ionic diastereomeric salts with chiral compounds and separating by fractional crystallization or other methods, (2) forming diastereomeric compounds with chiral derivatizing agents, separating diastereomers, and converting to pure enantiomers, or (3) enantiomers can be directly separated under chiral conditions. In method (1), diastereomeric salts can be formed by reacting enantiomerically pure chiral bases such as strychnine, quinine, ephedrine, strychnine, a-methyl-b-phenylethylamine (amphetamine), etc. with asymmetric compounds with acidic functional groups such as carboxylic acids and sulfonic acids. Diastereomeric salts can be induced to separate by fractional crystallization or ion chromatography. In order to separate the optical isomers of amino compounds, adding chiral carboxylic acids or sulfonic acids such as camphorsulfonic acid, tartaric acid, mandelic acid or lactic acid can lead to the formation of diastereomeric salts. Alternatively, by method (2), the substrate to be separated can react with one enantiomer of the chiral compound to form a diastereomeric pair (Eliel, E. and Wilen, S. (1994) Stereochemistry of Organic Compounds, John Wiley & Sons, Inc., p. 322). Diastereomeric compounds can be formed by reacting an asymmetric compound with an enantiomerically pure chiral derivatizing agent such as a menthyl derivative, followed by separation of the diastereomers and hydrolysis to produce the free, enantiomerically enriched compound. A method for determining optical purity involves preparing a chiral ester (such as menthyl) or Moschel ester of the racemic mixture, acetic acid a-methoxy-a-(trifluoromethyl)phenyl ester (Jacob III. (1982) J. Org. Chem. 47: 4165), and analyzing the NMR spectrum to determine the presence of two atropisomers. Stable diastereomers can be separated and isolated by normal and reverse phase chromatography according to the method for separating atropisomers naphthyl-isoquinolines (Hoye, T., WO96 / 15111). In method (3), the racemic mixture of two asymmetric enantiomers is separated by chromatography using a chiral stationary phase. Suitable chiral stationary phases are, for example, polysaccharides, particularly cellulose or amylose derivatives. Commercially available chiral stationary phases based on polysaccharides are CA, OA, OB5, OC5, OD, OF, OG, OJ, and OK, and AD, AS, OP(+) and OT(+). Suitable eluents or mobile phases used in combination with the polysaccharide chiral stationary phase are hexane or the like modified with alcohols such as ethanol, isopropanol, etc. ("Chiral Liquid Chromatography" (1989) WJ Lough, ed., Chapman and Hall, New York; Okamoto, (1990) "Optical resolution of dihydropyridine enantiomers by High-performance liquid chromatography using phenylcarbamates of polysaccharides as a chiral stationary phase", J. of Chromatogr. 513: 375-378).

[0472] The terms cis and trans are used herein according to Chemical Abstracts nomenclature and include reference to the position of substituents on a ring portion. The absolute stereochemical configuration of compounds of the formulae described herein can be readily determined by those skilled in the art using well-known methods such as X-ray diffraction.

[0473] When a compound is crystallized from a solution or slurry, it may crystallize in different spatially arranged lattices (a property known as "polymorphism") to form crystals having different crystalline forms, each of which is known as a "polymorph". Thus, as used herein, the term "polymorph" refers to a crystalline form of a compound of formula (I) in which the molecules are located in three-dimensional lattice positions. Different polymorphs of a compound of formula (I) may differ from one another in one or more physical properties, such as solubility and dissolution rate, true specific gravity, crystal form, accumulation pattern, flowability and / or solid state stability, etc.

[0474] The pyrazolo[1,5-a]pyridine derivatives and physiologically acceptable salts thereof (hereinafter collectively referred to as active ingredients) of the present invention can be administered by any route suitable for the condition to be treated, including oral, rectal, nasal, topical (including ocular, buccal and sublingual), vaginal and parenteral (including subcutaneous, intramuscular, intranasal, intravenous, intraarterial, intradermal, intrathecal and epidural). The preferred route of administration may vary, for example, depending on the condition of the recipient.

[0475] A therapeutically effective amount of a compound preparation, in particular for treating TRPM3-mediated disorders in humans and other mammals or animals, is preferably a TRPM3 ion channel inhibiting amount of the compound as defined herein and corresponds to an amount ensuring plasma levels between 1 μg / ml and 100 mg / ml.

[0476] Suitable doses of the compounds or compositions of the present invention are used to treat or prevent TRPM3-mediated disorders in a subject. Depending on the pathological condition to be treated and the condition of the patient, the effective amount may be divided into several subunits per day, or may be administered at intervals of more than one day.

[0477] The present invention further provides (pharmaceutical) compositions comprising one or more pyrazolo[1,5-a]pyridine derivatives of the present invention, more particularly all formula (I) and other formulas and embodiments described herein and more specific aspects or embodiments thereof. In addition, the present invention provides compounds or (pharmaceutical) compositions of the present invention, more particularly all formula (I) and other formulas and embodiments described herein and more specific aspects or embodiments thereof, for use as a medicament, more particularly for the treatment of pain. TRPM3-mediated conditions are selected from pain and inflammatory hypersensitivity conditions and epilepsy.

[0478] The pyrazolo[1,5-a]pyridine derivatives of the present invention can be formulated with conventional carriers and excipients, which will be selected according to conventional practice. Tablets will contain excipients, glidants, fillers, binders, etc. Aqueous preparations are prepared in sterile form and are generally isotonic when intended to be delivered by means other than oral administration. The preparations optionally contain excipients such as those described in "Handbook of Pharmaceutical Excipients" (1986).

[0479] Subsequently, as used herein, the term "pharmaceutically acceptable carrier" means any material or substance formulated with the active ingredient to facilitate its application or distribution to the site to be treated, for example by dissolving, dispersing or diffusing the composition, and / or facilitating its storage, transportation or handling without impairing its effectiveness. A pharmaceutically acceptable carrier may be a solid or a liquid or a gas compressed to form a liquid, i.e., the composition of the present invention may be suitably used as a concentrate, emulsion, solution, granule, powder, spray, aerosol, suspension, ointment, cream, tablet, pill or powder.

[0480] Suitable pharmaceutical carriers for the pharmaceutical composition and its preparation are well known to those skilled in the art, and there is no particular restriction on their selection in the present invention. They may also include additives, such as wetting agents, dispersants, adhesives, binders, emulsifiers, surfactants, solvents, coatings, antibacterial and antifungal agents, isotonic agents, etc., provided that they are consistent with pharmaceutical practice, i.e., carriers and additives will not cause permanent damage to mammals. The pharmaceutical composition of the present invention may be prepared in any known manner, such as by uniformly mixing, coating and / or grinding the active ingredient with selected carrier materials and suitable other additives (such as surfactants) in one or more step procedures. It may also be prepared by micronization, such as in order to obtain microspheres in the form of microspheres of about 1 to 10 grams in diameter, i.e., for the manufacture of microcapsules for controlling or sustained release of active ingredients.

[0481] Although the pyrazolo[1,5-a]pyridine derivatives can be administered alone, it is preferably provided as a pharmaceutical formulation. The veterinary and human formulations of the present invention contain at least one active ingredient as described above, as well as one or more pharmaceutically acceptable carriers and optional other therapeutic ingredients. The carrier is preferably "acceptable" in the sense that it is compatible with the other ingredients of the formulation and is harmless to the recipient thereof. The formulations include formulations suitable for oral, rectal, nasal, topical (including buccal and sublingual), vaginal or parenteral (including subcutaneous, intramuscular, intravenous, intradermal, intrathecal and epidural) administration. The formulations can be conveniently presented in unit dosage form and can be prepared by any method well known in the pharmaceutical art. Such methods include the step of combining the active ingredient with a carrier constituting one or more auxiliary ingredients. Typically, the formulation is prepared by uniformly and intimately combining the active ingredient with a liquid carrier or a finely divided solid carrier or both, and then molding the product if necessary.

[0482] Formulations of the present invention suitable for oral administration may be presented as discrete units such as capsules, cachets or tablets, each containing a predetermined amount of the active ingredient; as a powder or granules; as a solution or suspension in an aqueous liquid or a non-aqueous liquid; or as an oil-in-water liquid emulsion or a water-in-oil liquid emulsion. The active ingredient may also be presented as a bolus, electuary or paste.

[0483] Tablets can be made by compression or molding, optionally with one or more auxiliary ingredients. Compressed tablets can be prepared by compressing the active ingredient of a free-flowing form (such as a powder or granule) in a suitable machine, the active ingredient optionally mixed with a binding agent, lubricant, inert diluent, preservative, surfactant or dispersant. Molded tablets can be prepared by molding a mixture of a powdered compound moistened with an inert liquid diluent in a suitable machine. Tablets can be optionally coated or scored, and can be formulated to provide a slow or controlled release of the active ingredient therein. For infections of the eye or other external tissues (e.g., oral cavity and skin), the formulation is optionally applied as a topical ointment or cream containing, for example, 0.075 to 20% w / w (including active ingredients in the range of 0.1% to 20% in increments of 0.1% w / w, such as 0.6% w / w, 0.7% w / w, etc.), preferably 0.2 to 15% w / w, and most preferably 0.5 to 10% w / w of the amount of active ingredient. When formulated as an ointment, the active ingredient can be used with a paraffin or water-miscible ointment base. Alternatively, the active ingredient can be formulated into a cream with an oil-in-water cream base. If desired, the aqueous phase of the cream base may include, for example, at least 30% w / w of a polyol, i.e., an alcohol having two or more hydroxyl groups, such as propylene glycol, 1,3-butylene glycol, mannitol, sorbitol, glycerol, and polyethylene glycol (including PEG400) and mixtures thereof. Topical formulations may desirably include compounds that enhance the absorption or penetration of the active ingredient through the skin or other affected area. Examples of such dermal penetration enhancers include dimethyl sulfoxide and related analogs.

[0484] The oil phase of the emulsion of the present invention can be constituted by known ingredients in a known manner. Although this phase can only contain an emulsifier (emulsifier) ​​(also known as an emulsifier (emulgent)), it ideally comprises at least one emulsifier and a fat or oil or a mixture of both fat and oil. Optionally, a hydrophilic emulsifier is included together with a lipophilic emulsifier used as a stabilizer. It is also preferred to include oil and fat. The emulsifier and stabilizer or not together with the stabilizer constitute the so-called emulsifying wax, and the wax together with the oil and fat constitute the so-called emulsified ointment base, which forms the oily dispersed phase of the cream formulation.

[0485] Selecting suitable oil or fat for preparation is based on obtaining required cosmetic properties, because the solubility of active compound in most oils that may be used for pharmaceutical emulsion preparations is very low.Therefore, cream should optionally be non-greasy, non-dyed and washable product with suitable consistency, to avoid leakage from pipe or other containers.Linear or branched monobasic or dibasic alkyl esters can be used, such as propylene glycol diester of diisoadipate, isocetyl stearate, coconut fatty acid, isopropyl myristate, decyl oleate, isopropyl palmitate, butyl stearate, 2-ethylhexyl palmitate or the blend of the branched ester called Crodamol CAP, and the latter three kinds are preferred esters.According to required property, these can be used alone or in combination.Alternatively, high melting point lipids can be used, such as white soft paraffin and / or liquid paraffin or other mineral oils.

[0486] Formulations suitable for topical administration to the eye also include eye drops in which the active ingredient is dissolved or suspended in a suitable carrier, especially an aqueous solvent for the active ingredient. The active ingredient is optionally present in such formulations at a concentration of 0.5% to 20%, advantageously 0.5% to 10%, especially about 1.5% w / w. Formulations suitable for topical administration in the oral cavity include lozenges comprising the active ingredient in a flavored base (usually sucrose and gum arabic or tragacanth); pastilles comprising the active ingredient in an inert base (such as gelatin and glycerin, or sucrose and gum arabic); and mouthwashes comprising the active ingredient in a suitable liquid carrier.

[0487] Preparations for rectal administration may exist as suppositories with a suitable matrix, including, for example, cocoa butter or salicylates. Preparations suitable for nasal administration, in which the carrier is solid, include coarse powders of particle sizes, for example, in the range of 20 to 500 microns (including particle sizes in the range of 20 to 500 microns in increments of 5 microns, such as 30 microns, 35 microns, etc.), which are applied in the manner of snuff inhalation, i.e., by rapid inhalation through the nasal passages from a powder container near the nose. Suitable preparations for use as, for example, nasal sprays or nasal drops, in which the carrier is liquid, include aqueous or oily solutions of active ingredients. Preparations suitable for aerosol administration may be prepared according to conventional methods and may be delivered with other therapeutic agents.

[0488] Formulations suitable for vaginal administration may be presented as pessaries, tampons, creams, gels, pastes, foams or spray formulations containing in addition to the active ingredient such carriers as are known in the art to be appropriate.

[0489] Preparations suitable for parenteral administration include aqueous and non-aqueous sterile injection solutions, which may contain antioxidants, buffers, bacteriostats, and solutes that make the preparation isotonic with the blood of the intended recipient; and aqueous and non-aqueous sterile suspensions, which may include suspending agents and thickening agents. The preparation may be present in unit dose or multi-dose containers, such as sealed ampoules and vials, and may be stored under freeze-dried (lyophilized) conditions, requiring only the addition of a sterile liquid carrier, such as water for injection, immediately before use. Extemporaneous injection solutions and suspensions may be prepared from sterile powders, granules, and tablets of the aforementioned types.

[0490] Preferred unit dosage formulations are those containing a daily dose or unit daily dose, as herein above recited, or an appropriate fraction thereof, of the active ingredient.

[0491] It should be understood that in addition to the ingredients particularly mentioned above, the formulations of this invention may include other agents conventional in the art having regard to the type of formulation in question, for example those suitable for oral administration may include flavoring agents.

[0492] The pyrazolo[1,5-a]pyridine derivatives of the present invention can be used to provide controlled release pharmaceutical formulations ("controlled release formulations") containing one or more pyrazolo[1,5-a]pyridine derivatives of the present invention as active ingredients, wherein the release of the active ingredient can be controlled and regulated to allow for less frequent dosing or to improve the pharmacokinetic or toxicity profile of a given compound of the present invention. Controlled release formulations suitable for oral administration, wherein discrete units containing one or more pyrazolo[1,5-a]pyridine derivatives of the present invention can be prepared according to conventional methods.

[0493] Another embodiment of the present invention relates to various precursors or "prodrug" forms of the pyrazolo[1,5-a]pyridine derivatives of the present invention. It may be desirable to formulate the pyrazolo[1,5-a]pyridine derivatives of the present invention in the form of a chemical substance that itself has no significant biological activity, but when delivered to an animal, mammal or human, will undergo a chemical reaction catalyzed by the normal functions of the body, especially enzymes present in the stomach or serum, which has the effect of releasing the compound as defined herein. Therefore, the term "prodrug" refers to these substances that are converted into the active pharmaceutical ingredient in vivo.

[0494] The prodrugs of the pyrazolo[1,5-a]pyridine derivatives of the present invention may have any form suitable for formulators, for example, esters are common prodrug forms that are not limiting. However, in the present case, the prodrug may have to be in a form in which the covalent bonds therein are cleaved by the action of an enzyme present at the target site. For example, the CC covalent bond may be selectively cleaved by one or more enzymes at the target site, and therefore, prodrugs other than readily hydrolyzable proforms may be used, especially esters, amides, etc. The counterpart of the active pharmaceutical ingredient in the prodrug may have different structures, such as amino acid or peptide structures, alkyl chains, sugar moieties, and other structures known in the art.

[0495] For the purposes of the present invention, the term "therapeutically suitable prodrug" is defined herein as "a compound modified in such a way that, when in contact with the tissues of the animal, mammal or human to which the prodrug has been administered, the compound is converted in vivo by single or multiple biotransformations to a therapeutically active form without undue toxicity, irritation or allergic response and to achieve the desired therapeutic result."

[0496] More specifically, as used herein, the term "prodrug" refers to an inactive or significantly less active derivative of a compound such as a compound represented by a structural formula described herein, which undergoes spontaneous or enzymatic conversion in vivo to release a pharmacologically active form of the compound. For a comprehensive review, reference is made to Rautio J. et al. ("Prodrugs: design and clinical applications" Nature Reviews Drug Discovery, 2008, doi: 10.1038 / nrd2468).

[0497] Representative pyrazolo[1,5-a]pyridine derivatives of the present invention can be synthesized according to the general synthetic methods described below and illustrated in the following schemes. Since the schemes are illustrative, the present invention should not be construed as being limited to the specific chemical reactions and specific conditions described in the schemes and examples. The various starting materials used in the schemes are commercially available or can be prepared by methods well known to those skilled in the art. The variables are as defined herein and are within the skill of those skilled in the art.

[0498] Exemplary embodiments of the invention are summarized below as clauses 1 to 51:

[0499] 1. A compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph

[0500]

[0501] Preferably, the compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph, is optionally used in the treatment of pain or epilepsy or in a method for the treatment of pain or epilepsy;

[0502] in

[0503] R 1 Indicates -F, -Cl, -Br, -I, -CN, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O) 2 R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;

[0504] Q means -OR 2 or -NR 3 R 4 ;

[0505] R 2 Indicates -R Y ;

[0506] R 3 Indicates -OH or -R Y ;

[0507] R 4 Indicates -R Y or -S(=O) 2 R Y ;

[0508] or R 3 and R 4 together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S;

[0509] T stands for -O- and U stands for -CR 5 R 5 '-; or T means -CR 5 R 5 '- and U means -O-;

[0510] R 5 and R5 'Independently represent -R Y ;

[0511] R 6 , R 7 and R 8 Independently represent -F, -Cl, -Br, -I, -CN, -NO 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 ;

[0512] V represents a saturated or unsaturated 3-14-membered heterocycloalkyl; a saturated or unsaturated 3-14-membered cycloalkyl; a 5-14-membered aryl, a C 1 -C 6 alkyl; or 5-14 membered heteroaryl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are singly or polysubstituted;

[0513] in

[0514] R W and R X Independently of each other, in each case independently

[0515] -H;

[0516] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0517] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0518] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0519] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0520] R Y and R Z Independently of each other, in each case independently

[0521] -H;

[0522] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0523] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0524] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0525] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0526] unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl; wherein the 6-14 membered aryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0527] unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl; wherein the 5-14 membered heteroaryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0528] or R Y and R Z together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S;

[0529] and wherein "mono- or poly-substituted" in each case independently refers to substitution by one or more substituents which are independently selected from the group consisting of: -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-CFH2 , -C 1-6 -Alkylene-O-CF 3 , -C 1-6 -Alkylene-O-CF 2 H, -C 1-6 -Alkylene-O-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 -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), -N(3-14 membered cycloalkyl)(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C 1-6 -alkylene-OH, -N(H)-C 1-6-alkylene-OH, -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-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14-membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(=O)-(3- to 14-membered cycloalkyl), -C(=O)-(3- to 14-membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5- to 14-membered heteroaryl), -S(=O) 2 -(3-14 membered cycloalkyl), -S(=O) 2 -(3 to 14 membered heterocycloalkyl), -S(=O) 2 -phenyl, -S(=O) 2 -(5- to 14-membered heteroaryl).

[0530] 2. The compound according to item 1 itself or the compound for use, wherein T represents -O- and U represents -CR 5 R 5 '-.

[0531] 3. The compound according to item 1 itself or the compound for use, wherein T represents -CR 5 R 5 '-, and U means -O-.

[0532] 4. The compound according to any one of clauses 1 to 3, wherein Q represents -NR 3 R 4 .

[0533] 5. The compound according to any one of clauses 1 to 3, wherein Q represents -OR 2 .

[0534] 6. The compound according to any one of clauses 1 to 5, wherein V represents a saturated or unsaturated 3-14-membered heterocycloalkyl; a saturated or unsaturated 3-14-membered cycloalkyl; a 5-14-membered aryl; C 1 -C 6 alkyl; or 5-14 membered heteroaryl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0535] 7. The compound according to item 6, wherein the 5-14 membered heteroaryl group is mono- or poly-substituted.

[0536] 8. The compound according to clause 6 or 7, wherein the 5-14 membered heteroaryl is selected from benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furazan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthyridine, oxadiazole, oxazole, oxindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazole, thiadiazole, thiazole, thiophene, triazine, triazole and [1,2,4]triazolo[4,3-a]pyrimidine; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0537] 9. The compound according to any one of clauses 6 to 8, wherein the 5-14 membered heteroaryl is selected from the group consisting of furan, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, triazole, pyridine, isoquinoline, benzothiazole, pyridazine, pyrimidine, imidazopyridine; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NRY R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0538] 10. The compound according to any one of clauses 6 to 9, as such or for use, wherein the 5-14 membered heteroaryl is selected from the group consisting of furan-2-yl, furan-3-yl, thiophen-2-yl, thiophen-3-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, oxazol-5-yl, isoxazol-4-yl, thiazol-2-yl, thiazol-4-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; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0539] 11. The compound according to any one of clauses 1 to 5, wherein V represents a 3-14-membered heterocycloalkyl group, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0540] 12. The compound according to clause 11 itself or the compound for use, wherein the 3-14 membered heterocycloalkyl group is selected from azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiazolidine, cyclopentane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothia-cyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0541] 13. The compound according to clause 11 or 12, wherein the 3-14 membered heterocycloalkyl is oxane or oxetanyl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0542] 14. The compound according to any one of clauses 11 to 13, wherein the 3-14 membered heterocycloalkyl is oxan-4-yl or oxetane-3-yl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-ORY 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0543] 15. The compound according to any one of clauses 1 to 5, wherein the saturated or unsaturated 3-14 membered cycloalkyl is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl or cyclodecyl, including unfused or unbridged, fused or bridged cycloalkyl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0544] 16. The compound according to any one of clauses 1 to 5, wherein the 5-14 membered aryl is phenyl or another 5-14 membered aryl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0545] 17. The compound according to any one of clauses 1 to 6, wherein C represents V 1 -C 6 Alkyl or C 1 -C 6 Heteroalkyl is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[0546] 18. The compound according to any of the preceding clauses per se or the compound for use, wherein V is unsubstituted, monosubstituted or polysubstituted by substituents independently selected from the following:

[0547] -F, -Cl, -Br, -I, CF 3 , -CF 2 H, -CN, -C(=O)OH, -NH 2 、-NO 2 、-OH、=O、-SF 5 ;

[0548] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl;

[0549] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 -alkyl;

[0550] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -NHC 1-6 -alkyl;

[0551] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C 1-6 -alkyl) 2 ;

[0552] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 -alkyl;

[0553] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O) 2 -C 1-6 -alkyl;

[0554] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0555] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0556] 19. The compound according to any of the preceding clauses per se or the compound for use, wherein V is unsubstituted, monosubstituted or polysubstituted by substituents independently selected from the following:

[0557] -OH, -F, -Cl, -Br, -I, -SH, -CF 3 , -CHF 2 、-CH 2 F, -OCF 3 、-OCHF 2 、-OCH 2 F. SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 、-N(CH 3 ) 2 , -cyclopropyl or -O-cyclopropyl; preferably selected from -OH, -F, -Cl, -Br, -I, -SH, -CF 3 , -CHF 2 、-CH 2 F, -OCF 3 、-OCHF 2 、-OCH 2 F. SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 or -N(CH 3 ) 2 ;

[0558] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 、-C(=O)NH 2 The substituents of the group consisting of -cyclopropyl are monosubstituted or polysubstituted; preferably selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6-alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The group composed of;

[0559] -C 1-6 -heteroalkyl, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0560] -OC 1-6 -alkyl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2The substituents constituting the group are mono- or poly-substituted;

[0561] -O(C=O)C 1-6 -alkyl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0562] -C(=O)OC 1-6 -alkyl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0563] 3-14 membered cycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; each of which is unsubstituted, independently selected from -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -SH, =S, -CN, -CF 3 , -CHF 2 、-CH 2F, -OCF 3 、-OCHF 2 、-OCH 2 F. SF 5 、-NO 2 , -C(=O)OH, -NH 2 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono- or poly-substituted;

[0564] 3-14 membered heterocycloalkyl selected from azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, thiomorpholine, indoline, dihydrobenzo[1,2-dihydro- ... furan, dihydrobenzothiophene, 1,1-dioxothiananes, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopenta[c]pyrrole, octahydrocyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine, each unsubstituted, independently of one another, selected from the group consisting of -F, -Cl, -Br, -I, -C 1-6 -alkyl, C 2-6 -alkenyl, -C 2-6 -alkynyl, -OH, =O, -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 、C(=O)CHF 2 and -C(=O)NH 2 The substituents constituting the group are mono-substituted or poly-substituted.

[0565] 20. The compound according to any one of the preceding clauses, itself or the compound for use, wherein V is unsubstituted, independently selected from -F, -Cl, -CN, -OH, =O, -C 1-6 -alkyl, -CHF 2, -CF 3 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-NHC(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl) 2 、-OC 1-6 -alkyl, -OCF 3 、-OC 1-6 -alkylene-N(C 1-6 -alkyl) 2 、-S(=O) 2 -C 1-6 -alkyl, -azetidine, -C 1-6 -alkylene-O-tetrahydropyran or -C 1-6 The substituent of the -alkyl-substituted-piperazine is mono- or poly-substituted; or represents an unsubstituted, mono- or poly-substituted oxetanyl group.

[0566] 21. The compound according to any one of the preceding clauses, itself or for use, wherein V is

[0567] (i) unsubstituted;

[0568] (ii) monosubstituted;

[0569] (iii) disubstituted;

[0570] (iv) trisubstituted; or

[0571] (v) Tetrasubstituted.

[0572] 22. The compound according to any one of the preceding clauses, itself or for use, wherein R 1 express

[0573] -H, -F, -Cl, -Br, -I;

[0574] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl; saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 -alkyl;

[0575] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)C 1-6 -alkyl;

[0576] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 -alkyl;

[0577] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)NHC 1-6 -alkyl;

[0578] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)N(C 1-6 -alkyl) 2 ;

[0579] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)C 1-6 -alkyl;

[0580] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O) 2 -C 1-6 -alkyl;

[0581] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl; or

[0582] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0583] 23. The compound according to any one of the preceding clauses, itself or for use, wherein R 1 Indicates -H, -F, -Cl, -Br, -I, -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 -alkyl)-C 1-6 -Alkylene-CF 3 、-C(=O)C 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -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.

[0584] 24. The compound according to any one of the preceding clauses, itself or for use, wherein R 1 Indicates -H, -C 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -CH 2 F, -CHF 2 , -CF 3 , unsubstituted-cyclopentyl or -unsubstituted cyclopropyl; preferably wherein R 1 Indicates -H, -C 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -CH 2 F, -CHF 2 , -CF 3 or unsubstituted-cyclopentyl.

[0585] 25. The compound according to any one of the preceding clauses, itself or for use, wherein R 1 Indicates -CH 2 F, -CHF 2 、-CH 3 or unsubstituted-cyclopropyl; preferably wherein R 1 Indicates -CH2 F, -CHF 2 、-CH 3 or -CH 2 CH 3 .

[0586] 26. The compound according to any one of the preceding clauses, itself or for use, wherein R 2 express

[0587] -H;

[0588] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0589] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0590] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0591] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0592] 27. The compound according to any one of the preceding clauses, itself or for use, wherein R 2 Indicates -H, -C 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl) 2 , -CF 3 , -CF 2 H, -CFH 2 , -CF 2Cl, -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 .

[0593] 28. The compound according to any one of the preceding clauses, itself or for use, wherein R 2 Indicates -H or -C 1-6 -alkyl.

[0594] 29. The compound according to any one of the preceding clauses, itself or for use, wherein R 3 express

[0595] -H;

[0596] -OH;

[0597] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl; or

[0598] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl.

[0599] 30. The compound according to any one of the preceding clauses, itself or for use, wherein R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -Alkylene-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 .

[0600] 31. A compound according to any one of the preceding clauses, wherein R 3 represents -H, -OH or saturated, unsubstituted or -C substituted by -OH 1-6 -alkyl.

[0601] 32. The compound according to any one of the preceding clauses, itself or for use, wherein R 4 express

[0602] -H;

[0603] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)C 1-6 -alkyl;

[0604] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O) 2 -C 1-6 -alkyl;

[0605] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0606] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0607] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6-heteroalkylene-linkage;

[0608] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0609] unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl; wherein the 6-14 membered aryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0610] unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl; wherein the 5-14 membered heteroaryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0611] 33. The compound according to any one of the preceding clauses, itself or for use, wherein R 4 express

[0612] -S(=O) 2 C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, independently selected from -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 - alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0613] -S(=O) 2 (3-14 membered cycloalkyl), wherein the 3-14 membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, each of which is saturated or unsaturated, unsubstituted, substituted independently of one another by -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, -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(=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 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0614] -C 1-6 -alkyl, which is saturated or unsaturated, unsubstituted, independently selected from -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 - alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0615] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered cycloalkyl is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, in each case saturated or unsaturated, in each case unsubstituted, substituted independently of one another by -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 - alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0616] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6 -Alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from the group consisting of azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiazolidine, cyclopentane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothia-cyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolazine, hexahydro-cyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole and octahydropyrrolo[1,2-a]pyrazine; in each case unsubstituted, independently of one another, selected from the group consisting of -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 - alkylene-phenyl, saturated or unsaturated, unsubstituted 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0617] -phenyl, which is unsubstituted, independently selected from -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 3-14-membered heterocycloalkyl; and unsubstituted 5-14-membered heteroaryl are mono- or poly-substituted;

[0618] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -Alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of benzimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoindole, quinoline, 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; in each case unsubstituted, independently selected from the group consisting of -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 The substituents from the group consisting of -alkylene-phenyl, saturated or unsaturated, unsubstituted 3- to 14-membered heterocycloalkyl; and unsubstituted 5- to 14-membered heteroaryl are mono- or poly-substituted.

[0619] 34. A compound according to any one of the preceding clauses, wherein R 4 express

[0620] -H;

[0621] Saturated, unsubstituted, mono- or poly-substituted by -F -S(=O) 2 C1-6 -alkyl;

[0622] Saturated, unsubstituted -S(=O) 2 (3-14 membered cycloalkyl);

[0623] -C 1-6 -alkyl, which is saturated, unsubstituted, independently selected from -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 -alkyl, unsubstituted -phenyl, mono-substituted or di-substituted;

[0624] 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3-14 membered cycloalkyl is saturated, unsubstituted, substituted independently by -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 - The substituents of the group consisting of alkyl groups are mono-substituted or di-substituted;

[0625] 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl), wherein -C 1-6-alkylene- is unsubstituted or monosubstituted by -OH, wherein the 3- to 14-membered heterocycloalkyl is in each case selected from azetidine, 1,4-oxazepane, pyrrolidine, piperidine, azepane, diazepane, tetrahydrofuran, tetrahydropyran, oxetane, morpholine, piperazine, hexahydrocyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole, octahydro-pyrrolo[1,2 -a] pyrazine, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, quinuclidine, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiazolin-cyclohexane, in each case unsubstituted, independently selected from the group consisting of -F, -OH, =O, -C 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 - The substituents of the group consisting of alkylene-phenyl are mono- or poly-substituted;

[0626] unsubstituted-phenyl;

[0627] 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl), wherein -C 1-6 -alkylene- is unsubstituted or monosubstituted by -OH, wherein the 5- to 14-membered heteroaryl is in each case selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole and [1,2,4]triazolo[4,3-a]pyrimidine, in each case unsubstituted, independently selected from the group consisting of -C1-6 The substituent group consisting of -alkyl and -OH is mono- or di-substituted.

[0628] 35. The compound according to any one of the preceding clauses, itself or for use, wherein R 3 and R 4 Together they form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S.

[0629] 36. The compound according to any one of the preceding clauses, itself or for use, wherein R 3 and R 4 together to form a heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine and piperazine, each of which is unsubstituted, independently of one another, and selected from the group consisting of -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)OC 1-6 -alkyl, unsubstituted-pyridyl and unsubstituted or -C 1-6 The substituents of the group consisting of -alkyl mono-substituted 1,2,4-oxadiazole are mono- or poly-substituted.

[0630] 37. The compound according to any one of the preceding clauses, itself or for use, wherein R 3 and R 4 Together we form

[0631] Unsubstituted or -N(CH 3 ) 2 a monosubstituted pyrrolidine ring;

[0632] Not replaced or selected by -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 group consisting of a monosubstituted piperidine ring, and unsubstituted or -C 1-6 - alkyl monosubstituted 1,2,4-oxadiazole;

[0633] an unsubstituted morpholine ring; or

[0634] Not replaced or selected by -C 1-6 The substituents of the N-substituted piperazine ring are composed of -alkyl and unsubstituted -pyridyl.

[0635] 38. The compound according to any one of the preceding clauses, as such or for use, wherein R 5 and R 5 'Independently express

[0636] -H;

[0637] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0638] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0639] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[0640] 39. The compound according to any one of the preceding clauses, itself or for use, wherein R 5 and R 5 ' represents -H, -C independently of each other 1 -C 6 -alkyl or -C 1 -C 6 -alkylene-N(C 1 -C 6 -alkyl) 2 .

[0641] 40. A compound according to any one of the preceding clauses, wherein R 5 and R 5 At least one of ' does not represent -H.

[0642] 41. A compound according to any one of the preceding clauses, wherein R 6 , R 7 and R 8 Independently express

[0643] -H;

[0644] -F, -Cl, -Br, -I, -OH, -SH, -SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 ;

[0645] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl;

[0646] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 -alkyl;

[0647] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -NHC 1-6 -alkyl;

[0648] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C 1-6 -alkyl) 2 ;

[0649] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 -alkyl;

[0650] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC(=O)C 1-6 -alkyl;

[0651] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -heteroalkyl.

[0652] 42. A compound according to any one of the preceding clauses, itself or for use, wherein R 6 , R 7 and R 8 Independently express

[0653] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 ,

[0654] -C 1-6 -alkyl, -CF 3 , -CHF 2 、-CH 2 F.

[0655] -OC 1-6-alkyl, -OCF 3 、-OCHF 2 、-OCH 2 F.

[0656] -NHC 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 Substituents are substituted;

[0657] -N(C 1-6 -alkyl) 2 , which is unsubstituted or is substituted by one or more independently selected from -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 Substituents are substituted;

[0658] -C(=O)OC 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 Substituents are substituted;

[0659] -OC(=O)C1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 or

[0660] -C 1-6 -heteroalkyl, which is unsubstituted or substituted by one or more independently selected from -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 by a substituent.

[0661] 43. A compound according to any one of the preceding clauses, wherein R 6 Indicates -H, -F, -Cl, -CN or -C 1 -C 6 -alkyl.

[0662] 44. A compound according to any one of the preceding clauses, wherein R 6 -H is not indicated.

[0663] 45. A compound according to any one of the preceding clauses, itself or for use, wherein R 7 Indicates -H, -F, -Cl, -CN or -C 1 -C 6 -alkyl.

[0664] 46. ​​A compound according to any one of the preceding clauses, wherein R 7 -H is not indicated.

[0665] 47. A compound according to any one of the preceding clauses, wherein R 8 Indicates -H, -F, -Cl, -CN or -C 1 -C 6 -alkyl.

[0666] 48. A compound according to any one of the preceding clauses, wherein R 8 -H is not indicated.

[0667] 49. The compound according to any one of the preceding clauses, itself or the compound for use, wherein

[0668] (i)R 6 , R 7 and R 8 Each represents -H; or

[0669] (ii) R 6 , R 7 and R 8 The two in it represent -H, and R 6 , R 7 and R 8 The other one of the above represents -F, -Cl, -CN or -CH 3 ;or

[0670] (iii) R 6 , R 7 and R 8 One of them represents -H, and R 6 , R 7 and R 8 The other of each independently represents -F, -Cl, -CN or -CH 3 .

[0671] 50. A compound according to any of the preceding clauses as such or for use, which is selected from the group consisting of cpd 001 to cpd 036 or cpd 037 to 091 as described above and their physiologically acceptable salts.

[0672] 51. A compound per se or a compound for use according to any of the preceding clauses, wherein the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain.

[0673] 52. A compound per se or a compound for use according to any of the preceding clauses, wherein the pain is post-operative pain.

[0674] 53. A compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph, as defined in any of the preceding clauses, wherein

[0675] (a-1)Q represents -NR 3 R 4 ; R 1 Represents R W ; and R W Indicates -C 1 -C 6 -alkyl-, and / or

[0676] (a-2) Q represents -NR 3 R 4 ; and R 5 and R 5 ' represents -H; and / or

[0677] (a-3) Q represents -NR 3 R 4 ; and R 6 indicates -H; and / or

[0678] (a-4) Q represents -NR 3 R 4 ; and R 8 Indicates -H;

[0679] or

[0680] (b-1)

[0681] (b-1) Q represents -NR 3 R 4 ; and R 1 Indicates -CH 2 F, -CHF 2 , -CF 3 , -CN, -methyl, -ethyl, -propyl or -cyclopropyl; and / or

[0682] (b-2) Q represents -NR 3 R 4 ; and R 5 and R 5 ' does not represent -H; and / or

[0683] (b-3) Q represents -NR 3 R 4 ; and R 3 Indicates -H.

[0684] 54. A pharmaceutical composition or medicament comprising a compound according to any of the preceding clauses.

[0685] Further exemplary embodiments of the invention are summarized below as items 1 to 68:

[0686] 1. A compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph

[0687]

[0688] in

[0689] R 1 Indicates -F, -Cl, -Br, -I, -CN, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O) 2 R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ;

[0690] Q means -OR 2 or -NR 3 R 4 ;

[0691] R 2 Indicates -R Y ;

[0692] R 3 Indicates -OH or -R Y ;

[0693] R 4 Indicates -R Y or -S(=O) 2 R Y ;

[0694] or R 3 and R 4 together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S;

[0695] T stands for -O- and U stands for -CR 5 R 5 '-; or T means -CR 5 R 5 '- and U means -O-;

[0696] R 5 and R5 'Independently represent -R Y ;

[0697] R 6 , R 7 and R 8 Independently represent -F, -Cl, -Br, -I, -CN, -NO 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 ;

[0698] V represents a saturated or unsaturated 3-14-membered heterocycloalkyl group; a saturated or unsaturated 3-14-membered cycloalkyl group; a 5-14-membered aryl group; C 1 -C 6 alkyl or 5-14 membered heteroaryl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are singly or polysubstituted;

[0699] in

[0700] R W and R X Independently of each other and in each case independently represent

[0701] -H;

[0702] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0703] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0704] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0705] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0706] R Y and R Z Independently of each other and in each case independently represent

[0707] -H;

[0708] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[0709] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[0710] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0711] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl; wherein the 3-14 membered heterocycloalkyl is optionally substituted by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0712] unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl; wherein the 6-14 membered aryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linked; or

[0713] unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl; wherein the 5-14 membered heteroaryl is optionally substituted by in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage;

[0714] or R Y and R Z together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S;

[0715] and wherein "mono- or poly-substituted" in each case independently refers to substitution by one or more substituents which are independently selected from the group consisting of: -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-CFH2 , -C 1-6 -Alkylene-O-CF 3 , -C 1-6 -Alkylene-O-CF 2 H, -C 1-6 -Alkylene-O-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 -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), -N(3-14 membered cycloalkyl)(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C 1-6 -alkylene-OH, -N(H)-C 1-6-alkylene-OH, -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-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14-membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(=O)-(3- to 14-membered cycloalkyl), -C(=O)-(3- to 14-membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5- to 14-membered heteroaryl), -S(=O) 2 -(3-14 membered cycloalkyl), -S(=O) 2 -(3 to 14 membered heterocycloalkyl), -S(=O) 2 -phenyl, -S(=O) 2 -(5- to 14-membered heteroaryl).

[0716] 2. Preferably, the compound of formula (I) according to item 1, its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph,

[0717]

[0718] in

[0719] Q means -OR 2 or -NR 3 R 4;

[0720] T stands for -O-;

[0721] U stands for –CR 5 R 5 '-;

[0722] V means H or R 4

[0723] R 1 Indicates -H, R 9 、-OC 1-6 -alkyl, -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 ,-S(=O)-C 1-6 -alkyl, -S(=O) 2 -C 1-6 -alkyl, unsubstituted cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl;

[0724] R 2 Represents hydrogen or R 9 ;

[0725] R 3 Indicates -H, R 9 、-OH、-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 ;

[0726] R 4 Represents R 4 'or-SO 2-R 4 ',in

[0727] R 4 ' indicates -R 9 , -R cycl or -R 10 -R cycl ;and

[0728] R cycl express

[0729] Saturated or unsaturated 3-14 membered cycloalkyl

[0730] Saturated or unsaturated 4-14 membered heterocycloalkyl having one or more N, O or S atoms in the heterocycloalkyl ring

[0731] 6-14 membered aryl, or

[0732] 5-14 membered heteroaryl having one or more N, O or S in the heteroaryl ring;

[0733] R 1 and R 3 Can together form the group -R 10 -;or

[0734] R 3 and R 4 Can together form the group -R 10 -;

[0735] R 5 , R 5 '、R 6 , R 7 and R 8 independently of each other represent hydrogen or R 9 ;and

[0736] R cycl Can be R 9 Replace, and R cycl The cycloalkyl ring and the heterocycloalkyl ring of are independently capable of being substituted by =O or =S; and

[0737] R 9 Indicates -C 1-6 -alkyl or -C having one or more N, O or S in the chain 1-6 -heteroalkyl; and

[0738] R 10 Indicates -C 1-6 -alkylene or -C having one or more N, O or S in the chain 1-6 -heteroalkylene; and

[0739] Where R 9and R 10 can be straight or branched chain, saturated or unsaturated; and

[0740] R 9 , R 10 and R cycl Can be R 11 replace; and

[0741] R 11 Selected from the list consisting of: -OR, -NR 2 , halogen, -CN, -COOR, -CO-NR 2 、-CONR(OR)、-O-CO-OC 1-6 -alkyl, -NR-C(=O)-R, -NR-C(=O)-OR, -NR-C(=O)-N(R) 2 、-OS(=O) 2 -NR 2 、-NR-SO 2 -R, -N(R)-S(=O) 2 OR, -N(R)-S(=O) 2 NR 2 ,-SR,-S(=O)-R,-S(=O) 2 -OR, -S(=O) 2 -NR 2 、-NO、-NO 2 , -C 1-6 -alkylene-OR, -C 1-6 -Alkylene-NR 2 , =O or =S or a saturated or unsaturated 3-7 membered cycloalkyl, wherein the residues R can be independently selected from the group consisting of: H or -C 1-6 -alkyl.

[0742] 3. The compound according to item 1, wherein R 1 represents a straight or branched alkyl group having 1 to 6 carbon atoms, which can be replaced by halogen, -OR, -CONR 2 or -NR 2 substituted, wherein the residues R independently represent H or C which can be substituted by halogen 1-6 -alkyl.

[0743] 4. A compound according to any one of the preceding clauses, wherein R 3 Represents hydrogen or R 9 .

[0744] 5. A compound according to any one of the preceding clauses, wherein

[0745] Q means OR 2 or -NR 3 R 4 ;

[0746] T stands for -O-;

[0747] U stands for –CR 5 R 5 '-;

[0748] V means H or R 4

[0749] R 1 represents a straight or branched alkyl group having 1 to 6 carbon atoms, which can be replaced by halogen, -OR, -CONR 2 or -NR 2 substituted, wherein the residues R independently represent H or C which can be substituted by halogen 1-6 -alkyl;

[0750] R 2 and R 3 Represents hydrogen or R 9 ;

[0751] or R 1 and R 3 Can together form the group -R 10 -;

[0752] R 4 Represents R 4 'or-SO 2 -R 4 ',in

[0753] R 4 ' indicates -R 9 , -R cycl or -R 10 -R cycl ;and

[0754] R cycl express

[0755] Saturated or unsaturated 3-14 membered cycloalkyl

[0756] a saturated or unsaturated 4-14 membered heterocycloalkyl radical having one or more N, O or S atoms in the heterocycloalkyl ring,

[0757] 6-14 membered aryl, or

[0758] 5-14 membered heteroaryl having one or more N, O or S in the heteroaryl ring;

[0759] R 5 , R 5 '、R6 , R 7 and R 8 independently of each other represent hydrogen or R 9 ;and

[0760] R cycl Can be R 9 Replace, and R cycl The cycloalkyl ring and the heterocycloalkyl ring of are independently capable of being substituted by =O or =S; and

[0761] R 9 Indicates -C 1-6 -alkyl or -C having one or more N, O or S in the chain 1-6 -heteroalkyl; and

[0762] R 10 Indicates -C 1-6 -alkylene or -C having one or more N, O or S in the chain 1-6 -heteroalkylene; and

[0763] Where R 9 and R 10 can be straight or branched chain, saturated or unsaturated; and

[0764] R 9 , R 10 and R cycl Can be R 11 replace; and

[0765] R 11 Selected from the list consisting of: -OR, -NR 2 , halogen, -CN, -COOR, -CO-NR 2 、-CONR(OR)、-O-CO-OC 1-6 -alkyl, -NR-C(=O)-R, -NR-C(=O)-OR, -NR-C(=O)-N(R) 2 、-OS(=O) 2 -NR 2 、-NR-SO 2 -R, -N(R)-S(=O) 2 OR, -N(R)-S(=O) 2 NR 2 ,-SR,-S(=O)-R,-S(=O) 2 -OR, -S(=O) 2 -NR 2 、-NO、-NO 2 , -C 1-6 -alkylene-OR, -C 1-6-Alkylene-NR 2 or a saturated or unsaturated 3-7 membered cycloalkyl radical, wherein the radicals R can independently be H or -C substituted by halogen 1-6 -alkyl.

[0766] 6. A compound according to any one of the preceding clauses, wherein V represents

[0767] H,

[0768] -R 9 ,

[0769] a saturated or unsaturated 3-14-membered cycloalkyl group,

[0770] a saturated or unsaturated 4-14 membered heterocycloalkyl radical having one or more N, O or S atoms in the heterocycloalkyl ring,

[0771] 6-14 membered aryl,

[0772] A 5-14 membered heteroaryl having one or more N, O or S atoms in the heteroaryl ring, wherein the cyclic group can be replaced by R 9 replace.

[0773] 7. A compound according to any one of the preceding clauses, wherein R 5 , R 5 '、R 6 , R 7 and R 8 independently of each other represent hydrogen or C 1-3 -alkyl.

[0774] 8. A compound according to any one of the preceding clauses, wherein R 5 , R 5 '、R 6 , R 7 and R 8 Independently of each other represent hydrogen or methyl.

[0775] 9. A compound according to any one of the preceding clauses, wherein

[0776] Q means OR 2 or -NR 3 R 4 ;

[0777] T stands for -O-;

[0778] U stands for –CR 5 R 5 '-;

[0779] V means H, -R 9 or -R cycl ;

[0780] R 1 Indicates -C 1-6 -alkyl, which can be replaced by halogen, -OH, OR, -CONR 2 or -NR 2 substituted, wherein the residues R independently represent H or -C which can be substituted by halogen 1-6 -alkyl;

[0781] R 2 and R 3 represents hydrogen or methyl;

[0782] or R 1 and R 3 Can together form the group -R 10 -;

[0783] R 4 Represents R 4 'or-SO 2 -R 4 ',in

[0784] R 4 ' indicates -R 9 , -R cycl or -R 10 -R cycl ;and

[0785] R cycl express

[0786] Saturated or unsaturated 3-14 membered cycloalkyl

[0787] Saturated or unsaturated 4-14 membered heterocycloalkyl having one or more N, O or S atoms in the heterocycloalkyl ring

[0788] 6-14 membered aryl, or

[0789] 5-14 membered heteroaryl having one or more N, O or S in the heteroaryl ring;

[0790] R 5 , R 5 '、R 6 , R 7 and R 8 independently of one another represent hydrogen or methyl; and

[0791] R cycl Can be R 9 Replace, and R cycl The cycloalkyl ring and the heterocycloalkyl ring of are independently capable of being substituted by =O or =S; and

[0792] R 9 Indicates -C1-6 -alkyl or -C having one or more N, O or S in the chain 1-6 -heteroalkyl; and

[0793] R 10 Indicates -C 1-6 -alkylene or -C having one or more N, O or S in the chain 1-6 -heteroalkylene; and

[0794] Where R 9 and R 10 can be straight or branched chain, saturated or unsaturated; and

[0795] R 9 , R 10 and R cycl Can be R 11 replace; and

[0796] R 11 Selected from the list consisting of: -OR, -NR 2 , halogen, -CN, -COOR, -CO-NR 2 、-CONR(OR)、-O-CO-OC 1-6 -alkyl, -NR-C(=O)-R, -NR-C(=O)-OR, -NR-C(=O)-N(R) 2 、-OS(=O) 2 -NR 2 、-NR-SO 2 -R, -N(R)-S(=O) 2 OR, -N(R)-S(=O) 2 NR 2 ,-SR,-S(=O)-R,-S(=O) 2 -OR, -S(=O) 2 -NR 2 、-NO、-NO 2 , -C 1-6 -alkylene-OR, -C 1-6 -Alkylene-NR 2 or a saturated or unsaturated 3-7 membered cycloalkyl radical, wherein the radicals R can independently be H or -C substituted by halogen 1-6 -alkyl.

[0797] 10. A compound according to any one of the preceding clauses, wherein R 5 and R 5 ' represents hydrogen.

[0798] 11. A compound according to any one of the preceding clauses, wherein R1 and R 3 Together they form the group -R 10 -.

[0799] 12. A compound according to any one of the preceding clauses, wherein R 1 and R 3 Together they form a straight-chain or branched alkanediyl or alkenediyl having 1 to 4 carbon atoms, which can be unsubstituted or can be substituted with halogen, C 1-6 -alkyl or CONR 2 substitution, wherein the residues R can independently be H or C 1-6 -alkyl.

[0800] 13. A compound according to any one of the preceding clauses, wherein R 1 and R 3 Together they form a straight-chain or branched alkanediyl or alkenediyl having 1 to 3 carbon atoms, which can be unsubstituted or substituted with halogen, C 1-6 -alkyl or CONR 2 substitution, wherein the residues R can independently be H or C 1-6 -alkyl.

[0801] 14. The compound according to any one of items 1 to 13, wherein R 1 and R 3 Not linked to form a heterocyclic ring.

[0802] 15. A compound according to any one of the preceding clauses, wherein R 4 Represents R 4 'or-SO 2 -C 1-6 -alkyl.

[0803] 16. A compound according to any one of the preceding clauses, wherein V represents H, C 1-6 -alkyl or -R cycl .

[0804] 17. A compound according to any one of the preceding clauses, wherein

[0805] Q means OR 2 or -NR 3 R 4 ;

[0806] T stands for -O-;

[0807] U stands for –CH 2 -;

[0808] V stands for H, C 1-6 -alkyl or -R cycl; and wherein the cyclic group in group V can be replaced by at least one selected from -COO-C 1-6 -alkyl, -CO-NR 2 , -CN, halogen or C 1-6 -alkyl, wherein R independently represents H or -C 1-6 - alkyl, and the alkyl group in the group V can be substituted by one or more halogen atoms;

[0809] R 1 Indicates -C 1-6 -alkyl, which can be replaced by halogen, -OH, -CONR 2 or -NR 2 substituted, wherein the residues R independently represent H or -C which can be substituted by halogen 1-6 -alkyl;

[0810] R 2 and R 3 represents hydrogen or methyl;

[0811] R 4 Indicates -SO 2 -C 1-6 -alkyl, -R 9 , -R cycl or -R 10 -R cycl ;and

[0812] R cycl express

[0813] Saturated or unsaturated 3-14 membered cycloalkyl

[0814] Saturated or unsaturated 4-14 membered heterocycloalkyl having one or more N, O or S atoms in the heterocycloalkyl ring

[0815] 6-14 membered aryl, or

[0816] A 5-14 membered heteroaryl having one or more N, O or S in the heteroaryl ring, and R 6 , R 7 and R 8 independently of one another represent hydrogen or methyl; and

[0817] R cycl Can be R 9 Replace, and R cycl The cycloalkyl ring and the heterocycloalkyl ring of are independently capable of being substituted by =O or =S; and

[0818] R 9 Indicates -C 1-6-alkyl or -C having one or more N, O or S in the chain 1-6 -heteroalkyl; and

[0819] R 10 Indicates -C 1-6 -alkylene or -C having one or more N, O or S in the chain 1-6 -heteroalkylene; and

[0820] Where R 9 and R 10 can be straight or branched chain, saturated or unsaturated; and

[0821] R 9 , R 10 and R 4 R cycl Can be R 11 replace; and

[0822] R 11 Selected from the list consisting of: -OR, -NR 2 , halogen, -CN, -COOR, -CO-NR 2 、-CONR(OR)、-O-CO-OC 1-6 -alkyl, -NR-C(=O)-R, -NR-C(=O)-OR, -NR-C(=O)-N(R) 2 、-OS(=O) 2 -NR 2 、-NR-SO 2 -R, -N(R)-S(=O) 2 OR, -N(R)-S(=O) 2 NR 2 ,-SR,-S(=O)-R,-S(=O) 2 -OR, -S(=O) 2 -NR 2 、-NO、-NO 2 , -C 1-6 -alkylene-OR, -C 1-6 -Alkylene-NR 2 or a saturated or unsaturated 3-7 membered cycloalkyl radical, wherein the radicals R can independently be H or -C substituted by halogen 1-6 -alkyl.

[0823] 18. A compound according to any one of the preceding clauses, wherein R 6 , R 7 and R 8 represent hydrogen independently of one another.

[0824] 19. A compound according to any one of the preceding clauses, wherein R 2 Represents hydrogen.

[0825] 20. A compound according to any one of the preceding clauses, wherein R 3 Represents hydrogen.

[0826] 21. A compound according to any one of the preceding clauses, wherein R 2 and R 3 Represents hydrogen.

[0827] 22. A compound according to any one of the preceding clauses, wherein R 2 , R 3 , R 5 , R 5 '、R 6 , R 7 and R 8 represent hydrogen independently of one another.

[0828] 23. A compound according to any one of the preceding clauses, wherein R 1 Indicates -C 1-6 -alkyl.

[0829] 24. A compound according to any one of the preceding clauses, wherein

[0830] Q means OR 2 or –NR 3 R 4 ;

[0831] T stands for -O-;

[0832] U stands for -CH 2 -;

[0833] V stands for H, C 1-6 -alkyl or -R cycl ; and wherein R in the group V cycl Can be at least one selected from -COO-C 1-6 -alkyl, -CO-NR 2 , -CN, halogen or C 1-6 -alkyl, wherein R independently represents H or -C 1-6 - alkyl, and the alkyl group in the group V can be substituted by one or more halogen atoms;

[0834] R 1 Indicates -C 1-6 -alkyl;

[0835] R 2 represents hydrogen;

[0836] R 3 represents hydrogen;

[0837] R 4 Indicates -SO 2 -C 1-6 -alkyl, -R 9 , -R cycl or -R 10 -R cycl ;and

[0838] R cycl express

[0839] Saturated or unsaturated 3-6 membered cycloalkyl

[0840] Saturated or unsaturated 4-7 membered heterocycloalkyl having one or more N, O or S atoms in the heterocycloalkyl ring

[0841] 6-membered aryl, or

[0842] 6-membered heteroaryl having one or more N, O or S in the heteroaryl ring; and

[0843] R 6 , R 7 and R 8 independently of one another represent hydrogen or methyl; and

[0844] R cycl Can be R 9 Replace, and R cycl The cycloalkyl ring and the heterocycloalkyl ring of are independently capable of being substituted by =O or =S; and

[0845] R 9 Indicates -C 1-6 -alkyl or -C having one or more N, O or S in the chain 1-6 -heteroalkyl; and

[0846] R 10 Indicates -C 1-6 -alkylene or -C having one or more N, O or S in the chain 1-6 -heteroalkylene; and

[0847] Where R 9 and R 10 can be straight or branched chain, saturated or unsaturated; and

[0848] R 9 , R 10 and R 4 R cycl Can be R 11 replace; and

[0849] R 11 Selected from the list consisting of: -OR, -NR 2 , halogen, -CN, -COOR, -CO-NR 2 、-CONR(OR)、-O-CO-OC 1-6 -alkyl, -NR-C(=O)-R, -NR-C(=O)-OR, -NR-C(=O)-N(R) 2 、-OS(=O) 2 -NR 2 、-NR-SO 2 -R, -N(R)-S(=O) 2 OR, -N(R)-S(=O) 2 NR 2 ,-SR,-S(=O)-R,-S(=O) 2 -OR, -S(=O) 2 -NR 2 、-NO、-NO 2 , -C 1-6 -alkylene-OR, -C 1-6 -Alkylene-NR 2 or a saturated or unsaturated 3-7 membered cycloalkyl radical, wherein the radicals R can independently be H or -C substituted by halogen 1-6 -alkyl.

[0850] 25. A compound according to any one of the preceding clauses, wherein R 9 -C indicates a straight or branched chain 1-6 -alkyl.

[0851] 26. A compound according to any one of the preceding clauses, wherein R 10 -C indicates a straight or branched chain 1-6 -alkylene-.

[0852] 27. A compound according to any one of the preceding clauses, wherein R 9 -C indicates a straight or branched chain 1-6 -alkyl, and R 10 -C indicates a straight or branched chain 1-6 -alkylene-.

[0853] 28. A compound according to any one of the preceding clauses, wherein R 9 -C indicates a straight or branched chain 1-3 -alkyl.

[0854] 29. A compound according to any one of the preceding clauses, wherein R 10 -C indicates a straight or branched chain1-3 -alkylene-.

[0855] 30. A compound according to any one of the preceding clauses, wherein R 9 -C indicates a straight or branched chain 1-3 -alkyl, and R 10 -C indicates a straight or branched chain 1-3 -alkylene-.

[0856] 31. A compound as described in any of the preceding clauses, wherein the residue R 4 The substituent of the cyclic group in is directly bonded to the cyclic group.

[0857] 32. A compound according to any one of the preceding clauses, wherein

[0858] Q means OR 2 or –NR 3 R 4 ;

[0859] T stands for -O-;

[0860] U stands for -CH 2 -;

[0861] V stands for H, C 1-6 -alkyl or -R cycl ; and wherein R in the group V cycl can be replaced by at least one selected from -CN, halogen or C 1-3 - substituted by a group consisting of a group consisting of -alkyl, and the alkyl group in the group V can be substituted by one or more halogen atoms;

[0862] R 1 Indicates -C 1-3 -alkyl;

[0863] R 2 represents hydrogen;

[0864] R 3 represents hydrogen;

[0865] R 4 Indicates -SO 2 -C 1-6 -alkyl, -R 9 , -R cycl or -R 10 -R cycl ;and

[0866] R cycl express

[0867] Saturated or unsaturated 3-6 membered cycloalkyl

[0868] Saturated or unsaturated 4-7 membered heterocycloalkyl having one or more N, O or S atoms in the heterocycloalkyl ring

[0869] 6-membered aryl, or

[0870] 5-6 membered heteroaryl having one or more N, O or S in the heteroaryl ring; and

[0871] R 6 , R 7 and R 8 represents hydrogen; and

[0872] R cycl Can be R 9 Replace, and R cycl The cycloalkyl ring and the heterocycloalkyl ring of are independently capable of being substituted by =O or =S; and

[0873] R 9 Represents C 1-6 Alkyl; and

[0874] R 10 Indicates -C 1-3 - alkylene; and

[0875] Where R 9 and R 10 can be straight or branched chain, saturated or unsaturated; and

[0876] R 9 , R 10 and R 4 R cycl Can be R 11 replace; and

[0877] R 11 Selected from OH, halogen, C 1-3 -alkyl, -NR-SO 2 -R or -CONR 2 A list of groups, wherein R can be independently H or C which can be substituted by halogen 1-3 -alkyl.

[0878] 33. A compound according to any one of the preceding clauses, wherein R cycl Contains 1, 2 or 3 heteroatoms.

[0879] 34. A compound according to any one of the preceding clauses, wherein R cycl Contains 1 or 2 heteroatoms.

[0880] 35. A compound according to any one of the preceding clauses, wherein R cycl Contains 1 heteroatom.

[0881] 36. A compound according to any one of the preceding clauses, wherein

[0882] Q means OR 2 or –NR 3 R 4 ;

[0883] T stands for -O-;

[0884] U stands for -CH 2 -;

[0885] V stands for

[0886] H;

[0887] C 1-3 - alkyl, which can be substituted by at least one halogen;

[0888] 3-6 membered cycloalkyl, which can be substituted by -CN groups;

[0889] 4-6 membered heterocycloalkyl containing one oxygen atom in the heterocycloalkyl ring;

[0890] 6-membered aryl group, which can be substituted by at least one halogen or by

[0891] C 1-3 -alkyl substituted, wherein the C 1-3 - The alkyl group can be substituted by at least one halogen atom;

[0892] A 5-6 membered heteroaryl having one or more N, O or S atoms in the heteroaryl ring, wherein the heteroaryl ring can be substituted by halogen or C 1-3 - alkyl substitution, the alkyl group may be substituted by at least one halogen atom;

[0893] R 1 Indicates -C 1-3 -alkyl;

[0894] R 2 represents hydrogen;

[0895] R 3 represents hydrogen;

[0896] R 4 express

[0897] -SO 2 -C 1-3 -alkyl;

[0898] C 1-6 Alkyl, which can be OH, F, -NR 2 、-NR-SO 2 -R or -CONR2 substituted, wherein the residues R are independently hydrogen or C 1-3 alkyl;

[0899] 3-6 membered cycloalkyl, which can be substituted by halogen, C 1-3 -alkyl or -OH, =O or -CONH 2 replace;

[0900] C 1-3 -alkylene-3-6 membered cycloalkyl, which can be C 1-3 -alkyl or -N(C 1-6 alkyl) 2 group substitution;

[0901] A 4-7 membered heterocycloalkyl having one or more N or O atoms in the heterocycloalkyl ring, and wherein the heterocycloalkyl ring can be substituted by =O, halogen or -CONR 2 wherein the residues R independently represent H or C 1-3 -alkyl, or the heterocycloalkyl ring can be replaced by C 1-3 Alkyl substitution, the alkyl group can be substituted by OH or halogen;

[0902] C with one or more N, O in the heterocycloalkyl ring 1-4 -alkylene-4-7 membered heterocycloalkyl, wherein the heterocycloalkyl can be replaced by a C 1-3 Alkyl or =O substituted;

[0903] 6-membered aromatic group, C 1-3 Alkyl or –OC 1-3 Alkyl, wherein the C 1-3 Alkyl and –OC 1-3 The alkyl group may be substituted with halogen; or

[0904] A 5-7 membered heteroaryl having one or more N, O or S in the heteroaryl ring, wherein the heteroaryl ring can be replaced by a C 1-3 Alkyl substitution, or the heteroaryl ring can be substituted by OH; or

[0905] A C having one or more N or O in a heteroaryl ring 1-3 -alkylene-5-6 membered heteroaryl, wherein the C 1-3 -alkylene groups can be substituted by halogen or OH, and the heteroaryl ring can be substituted by OH or a C 1-3 Alkyl group substitution;

[0906] And R 6 , R 7 and R 8Represents hydrogen.

[0907] 37. A compound according to any one of the preceding clauses, wherein

[0908] Q means OR 2 or –NR 3 R 4 ;

[0909] T stands for -O-;

[0910] U stands for -CH 2 -;

[0911] V stands for

[0912] H;

[0913] C 1-3 - alkyl, which can be linear or branched and can be substituted by at least one fluorine atom;

[0914] 3-6 membered cycloalkyl;

[0915] 4-6 membered heterocycloalkyl containing one oxygen atom in the heterocycloalkyl ring;

[0916] 6-membered aromatic group, which can be substituted by at least one fluorine atom, by at least one chlorine atom or by at least one C 1-3 -alkyl group, wherein the C 1-3 - the alkyl group can be substituted by at least one fluorine atom;

[0917] A 5-6 membered heteroaryl having one or more N, O or S atoms in the heteroaryl ring, wherein the heteroaryl ring can be replaced by C 1-3 - alkyl substitution, the alkyl group can be substituted by at least one fluorine atom;

[0918] R 1 Indicates -C 1-3 -alkyl;

[0919] R 2 represents hydrogen;

[0920] R 3 represents hydrogen;

[0921] R 4 express

[0922] C 1-6 Alkyl groups, which can be linear or branched and can be replaced by OH, F, =O, -NR 2 、-NR-SO 2 -Me or -CONR 2 substitution, wherein the residues R are independently hydrogen or methyl;

[0923] 3-5 membered cycloalkyl, which can be substituted by halogen, C 1-3 -alkyl or –OH substitution;

[0924] A 4-7 membered heterocycloalkyl having one or more N or O atoms in the heterocycloalkyl ring, wherein the heterocycloalkyl ring can be substituted by halogen, =O or -CONR 2 wherein the residues R independently represent H or C 1-3 -alkyl, or the heterocycloalkyl ring can be replaced by a C 1-3 Alkyl group substitution;

[0925] C with one or more N or O in the heterocycloalkyl ring 1-4 -alkylene-5-6 membered heterocycloalkyl, wherein the C 1-4 - an alkylene group which can be linear or branched and can be substituted by OH; or

[0926] 6-membered aryl, which can be substituted by halogen or a straight or branched C 1-3 Alkyl substitution; or

[0927] C 1-4 -alkylene-6-membered aryl, wherein the C 1-4 -Alkylene groups may be linear or branched and may be substituted by halogen or OH, and the aryl groups may be substituted by halogen C 1-3 -alkyl or -OC 1-3 -alkyl substituted, wherein the C 1-3 -alkyl and –OC 1-3 - the alkyl groups may independently of one another be substituted by halogen; or

[0928] A 5-7 membered heteroaryl having one or more N, O or S in the heteroaryl ring, wherein the heteroaryl ring can be replaced by a C 1-6 Alkyl substitution, or the heteroaryl ring can be substituted by OH; or

[0929] A C having one or more N or O in a heteroaryl ring 1-3 -alkylene-5-6 membered heteroaryl, wherein the C 1-3 The -alkylene group can be substituted by halogen or OH, and the heteroaryl ring can be substituted by OH, cyclopropyl, cyclobutyl or a C 1-3 Alkyl group substitution;

[0930] And R 6 , R 7 and R 8 Represents hydrogen.

[0931] 38. A compound according to any one of the preceding clauses, wherein

[0932] Q means OR 2 or –NR 3 R 4 ;

[0933] T stands for -O-;

[0934] U stands for -CH 2 -;

[0935] V stands for

[0936] A methyl group which can be substituted by at least one fluorine atom;

[0937] 3-5-membered cycloalkyl;

[0938] Phenyl which can be substituted by at least one fluorine atom, by at least one chlorine atom or by at least one methyl group which can be substituted by fluorine;

[0939] 1,3-thiazole, which can be substituted with a methyl group; or

[0940] Pyridine, which can be substituted with a methyl group which can be substituted with fluorine;

[0941] R 1 Indicates -C 1-3 -alkyl;

[0942] R 2 represents hydrogen;

[0943] R 3 represents hydrogen;

[0944] R 4 express

[0945] C 1-6 Alkyl groups which can be linear or branched and can be replaced by OH, F, =O, -NMe 2 、-NR-SO 2 -Me or -CONR 2 substitution, wherein the residues R are independently hydrogen or methyl;

[0946] 3-4 membered cycloalkyl, C which can be substituted by fluorine or -OH 1-3 - alkyl substitution;

[0947] A 4-6 membered heterocycloalkyl having one or two N or O atoms in the heterocycloalkyl ring, wherein the heterocycloalkyl ring can be substituted by halogen or =O or by OH or fluorine. 1-3 Alkyl group substitution;

[0948] C with one or two O atoms in the heterocycloalkyl ring 1-4-alkylene-5-6 membered heterocycloalkyl, wherein the C 1-4 -Alkylene groups can be substituted by OH;

[0949] C 1-4 -alkylene-6-membered aryl, wherein the C 1-4 - the alkylene group can be linear or branched and can be substituted by fluorine or OH, and the aryl group can be substituted by fluorine or methoxy, wherein the methoxy group can be substituted by fluorine; or

[0950] A 5-6 membered heteroaryl having one or two nitrogen atoms in the heteroaryl ring, wherein the heteroaryl ring can be substituted by OH or a C 1-3 Alkyl substitution; or

[0951] A C having one or two nitrogen atoms in the heteroaryl ring 1-3 -alkylene-5-6 membered heteroaryl, wherein the C 1-3 The -alkylene group can be substituted by fluorine or OH, and the heteroaryl ring can be substituted by OH, cyclopropyl, cyclobutyl or a C substituted by halogen. 1-3 Alkyl group substitution;

[0952] And R 6 , R 7 and R 8 Represents hydrogen.

[0953] 39. A compound according to any one of the preceding clauses, wherein

[0954] Q means OR 2 or –NR 3 R 4 ;

[0955] T stands for -O-;

[0956] U stands for -CH 2 -;

[0957] V stands for

[0958] a methyl group substituted with two fluorine atoms;

[0959] Cyclopropyl;

[0960] Phenyl which can be substituted by one or two fluorine atoms or chlorine atoms, or by a fluorine atom and a methyl group substituted by 1, 2 or 3 fluorine atoms;

[0961] 1,3-thiazole, which is substituted with a methyl group; or

[0962] pyridine, which is substituted with a methyl group;

[0963] R 1Indicates -C 1-3 -alkyl;

[0964] R 2 represents hydrogen;

[0965] R 3 represents hydrogen;

[0966] R 4 express

[0967] C 1-5 Alkyl, which can be substituted by up to two OH, up to two F, -CONR 2 or -NHS(=O) 2 -Me substitution, wherein the residues R are independently hydrogen or methyl; or

[0968] 3-4 membered cycloalkyl, which may be substituted by fluorine or by -OH 1-3 - alkyl substitution;

[0969] A 5-6 membered heterocycloalkyl having one or two N or O atoms in the heterocycloalkyl ring, wherein the heterocycloalkyl ring can be substituted by halogen, =O or by OH or fluorine. 1-2 Alkyl group substitution;

[0970] C 1-3 -alkylene-tetrahydropyran residue, wherein C 1-4 - alkylene groups are substituted by OH;

[0971] C 1-2 -alkylene-6-membered aryl, wherein the C 1-2 - the alkylene group can be linear or branched and can be substituted by fluorine or OH, and the aryl group can be substituted by fluorine, methyl or methoxy, wherein the methyl or methoxy group can be substituted by fluorine; or

[0972] a pyridine ring substituted with OH and trifluoromethyl; or

[0973] A C having one or two nitrogen atoms in the heteroaryl ring 1-3 -alkylene-5-6 membered heteroaryl, wherein the C 1-3 - the alkylene group can be substituted by fluorine or OH, and the heteroaryl ring can be substituted by OH, cyclopropyl, cyclobutyl or methyl which can be substituted by fluorine;

[0974] And R 6 , R 7 and R 8 Represents hydrogen.

[0975] 40. A compound according to any one of the preceding clauses, wherein

[0976] Q means OR 2 or –NR 3 R 4 ;

[0977] T stands for -O-;

[0978] U stands for -CH 2 -;

[0979] V stands for

[0980] H;

[0981] C 1-3 - alkyl, which can be substituted by at least one halogen;

[0982] 3-6 membered cycloalkyl, which can be substituted by -CN groups;

[0983] 4-6 membered heterocycloalkyl containing one oxygen atom in the heterocycloalkyl ring;

[0984] 6-membered aryl group, which can be substituted by at least one halogen or by

[0985] C 1-3 -alkyl substituted, wherein the C 1-3 - The alkyl group can be substituted by at least one halogen atom;

[0986] A 5-6 membered heteroaryl having one or more N, O or S atoms in the heteroaryl ring, wherein the heteroaryl ring can be substituted by halogen or C 1-3 - alkyl substitution, the alkyl group may be substituted by at least one halogen atom;

[0987] R 1 Indicates -C 1-3 -alkyl;

[0988] R 2 represents hydrogen;

[0989] R 3 represents hydrogen;

[0990] R 4 express

[0991] -SO 2 -C 1-3 -alkyl;

[0992] C 1-6 Alkyl groups, which can be substituted by OH, F, -NR-SO 2 -R or -CONR 2 substituted, wherein the residues R are independently hydrogen or C 1-3 alkyl;

[0993] 3-6 membered cycloalkyl, which can be substituted by halogen, C 1-3-alkylene-OH, =O or -CONH 2 replace;

[0994] C 1-3 -alkylene-3-6 membered cycloalkyl, which can be C 1-3 -alkyl or -N(C 1-6 alkyl) 2 group substitution;

[0995] A 4-7 membered heterocycloalkyl having one or more N or O atoms in the heterocycloalkyl ring, and wherein the heterocycloalkyl ring can be substituted by =O, halogen or -CONR 2 wherein the residues R independently represent H or C 1-3 -alkyl, or the cycloalkyl ring can be replaced by C 1-3 Alkyl substitution, wherein the alkyl group can be substituted by at least one of OH or halogen;

[0996] C with one or more N, O in the heterocycloalkyl ring 1-4 -alkylene-4-7 membered heterocycloalkyl, wherein the heterocycloalkyl can be C 1-3 Alkyl or =O substituted;

[0997] A 5-7 membered heteroaryl having one or more N, O or S in the heteroaryl ring, wherein the heteroaryl ring can be replaced by C 1-6 Alkyl or OH substituted; or

[0998] A C having one or more N, O or S in a heteroaryl ring 1-3 -alkylene-5-6 membered heteroaryl, wherein the heteroaryl ring can be substituted by OH;

[0999] And R 6 , R 7 and R 8 Represents hydrogen.

[1000] 41. A compound according to any one of the preceding clauses, wherein

[1001] Q means OR 2 or –NR 3 R 4 ;

[1002] T stands for -O-;

[1003] U stands for -CH 2 -;

[1004] V stands for

[1005] H;

[1006] C 1-3 - alkyl groups which may be substituted by at least one fluorine atom;

[1007] 3-6 membered cycloalkyl, which can be substituted by -CN groups;

[1008] 4-6 membered heterocycloalkyl containing one oxygen atom in the heterocycloalkyl ring;

[1009] 6-membered aromatic group, which can be substituted by at least one fluorine atom, by at least one chlorine atom or by at least one C 1-3 -alkyl group, wherein the C 1-3 - the alkyl group can be substituted by at least one fluorine atom;

[1010] A 5-6 membered heteroaryl having one or more N, O or S atoms in the heteroaryl ring, wherein the heteroaryl ring can be replaced by C 1-3 - alkyl substitution, the alkyl group can be substituted by at least one fluorine atom;

[1011] R 1 Indicates -C 1-3 -alkyl;

[1012] R 2 represents hydrogen;

[1013] R 3 represents hydrogen;

[1014] R 4 express

[1015] C 1-6 Alkyl groups, which can be substituted by OH, F, -NH-SO 2 -C 1-3 -alkyl or -CONR 2 substitution, wherein the residues R are independently hydrogen or methyl;

[1016] A 4-7 membered heterocycloalkyl having one or more N or O atoms in the heterocycloalkyl ring, wherein the heterocycloalkyl ring can be replaced by =O or by C 1-3 - alkylene-OH substitution;

[1017] And R 6 , R 7 and R 8 Represents hydrogen.

[1018] 42. A compound according to any one of the preceding clauses, wherein

[1019] Q means OR 2 or –NR 3 R 4 ;

[1020] T stands for -O-;

[1021] U stands for -CH2 -;

[1022] V stands for

[1023] A methyl group which can be substituted by at least one fluorine atom;

[1024] 3-5-membered cycloalkyl;

[1025] Phenyl, which can be substituted by at least one fluorine atom, by at least one chlorine atom or by at least one methyl group;

[1026] 1,3-thiazole, which can be substituted with a methyl group; or

[1027] Pyridine, which can be substituted with methyl groups;

[1028] R 1 Indicates -C 1-3 -alkyl;

[1029] R 2 represents hydrogen;

[1030] R 3 represents hydrogen;

[1031] R 4 express

[1032] C 1-5 Alkyl, which can be replaced by OH, F or -CONR 2 or –NH-S(=O) 2 -Me substitution, wherein the residues R are independently hydrogen or methyl;

[1033] A 4-6 membered heterocycloalkyl having one N atom in the heterocycloalkyl ring, the heterocycloalkyl ring being capable of being a lactam ring, and wherein the heterocycloalkyl ring is capable of being replaced by C 1-2 - alkylene-OH substitution;

[1034] And R 6 , R 7 and R 8 Represents hydrogen.

[1035] 43. A compound according to any one of the preceding clauses, wherein

[1036] Q means OR 2 or –NR 3 R 4 ;

[1037] T stands for -O-;

[1038] U stands for -CH 2 -;

[1039] V stands for

[1040] a methyl group substituted with two fluorine atoms;

[1041] 3-4-membered cycloalkyl;

[1042] Phenyl, which can be substituted by one or two fluorine atoms or by a fluorine atom and a methyl group;

[1043] 1,3-thiazole, which is substituted with a methyl group; or

[1044] pyridine, which is substituted with a methyl group;

[1045] R 1 Indicates -C 1-3 -alkyl;

[1046] R 2 represents hydrogen;

[1047] R 3 represents hydrogen;

[1048] R 4 express

[1049] C 1-5 Alkyl, which can be substituted by up to two OH, up to two F, -CONR 2 or -NHS(=O) 2 -Me substitution, wherein the residues R are independently hydrogen or methyl; or

[1050] With C 1-2 -2-pyrrolidone ring of alkylene-OH;

[1051] And R 6 , R 7 and R 8 Represents hydrogen.

[1052] 44. The compound according to item 1, wherein R 3 Indicates -H.

[1053] 45. The compound according to item 2, wherein R 4 represents residues other than -H.

[1054] 46. ​​The compound according to any one of items 44 to 45, wherein R 1 It represents -methyl or ethyl.

[1055] 47. The compound according to any one of items 44 to 46, wherein T represents -O-, and U represents -CR 5 R 5 '-.

[1056] 48. A compound according to any of the preceding clauses, wherein V represents (i) a benzoimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, 5-14 membered heteroaryl of 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; in each case unsubstituted, independently selected from -F, -Cl, -CN, -OH, =O, -C 1-6 -alkyl, -CHF 2 , -CF 3 , -C 1-6 -Alkylene-NH 2 , -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-CHF 2 , -C 1-6 -Alkylene-CF 3 , -C 1-6 -alkylene-cyclopropyl, -cyclopropyl, -O-cyclopropyl, -C 1-6 -Alkylene-NHC(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl) 2 、-OC 1-6 -alkyl, -OCF 3 、-OC 1-6 -alkylene-N(C 1-6 -alkyl) 2 、-S(=O) 2 -C 1-6 -alkyl, -azetidine, -C 1-6 -alkylene-O-tetrahydropyran or -C 1-6 The substituents of the -alkyl-substituted-piperazine are mono- or polysubstituted; in particular, in each case unsubstituted, independently of one another, selected from the group consisting of -F, -Cl, -CN, -OH, =O, -C 1-6 -alkyl, -CHF 2 , -CF 3 , -C 1-6 -Alkylene-NH 2 , -C 1-6-Alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-NHC(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl) 2 、-OC 1-6 -alkyl, -OCF 3 、-OC 1-6 -alkylene-N(C 1-6 -alkyl) 2 、-S(=O) 2 -C 1-6 -alkyl, -azetidine, -C 1-6 -alkylene-O-tetrahydropyran or -C 1-6 The substituent of the -alkyl-substituted-piperazine is mono- or poly-substituted; or represents (ii) an unsubstituted, mono- or poly-substituted-oxetanyl group.

[1057] 49. A compound according to any one of items 1 to 47, wherein the saturated or unsaturated 3-14 membered cycloalkyl within the definition of V is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl or cyclodecyl, including unfused or unbridged, fused or bridged cycloalkyl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[1058] 50. A compound according to any one of items 1 to 47, wherein the 5-14 membered aryl group within the definition of V is phenyl or another 5-14 membered aryl group, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[1059] 51. The compound according to any one of items 1 to 47, wherein the 3-14 membered heterocycloalkyl group within the definition of V is selected from azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiazolidine, cyclopentane, thiomorpholine, indoline, dihydrobenzofuran, dihydrobenzothiophene, 1,1-dioxothia-cyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydro-cyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole and octahydro-pyrrolo[1,2-a]pyrazine; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2, =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[1060] 52. The compound according to any one of items 1 to 47, wherein V represents C 1 -C 6 Alkyl or C 1 -C 6 Heteroalkyl, which is saturated or unsaturated, unsubstituted, independently selected from -F, -Cl, -Br, -I, CF 3 , -CF 2 H.C 1 -C 6 Alkyl, -CN, -NO, -NO 2 , =O, =S, -SF 5 , -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O) 2 R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

[1061] 53. The compound according to any one of items 1 to 47, wherein V is a residue selected from the group consisting of:

[1062]

[1063]

[1064] 54. A compound according to any one of the preceding clauses, wherein R 1 Indicates -H, -F, -Cl, -Br, -I, -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 -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.

[1065] 55. A compound according to any one of the preceding clauses, wherein R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C1-6 -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 .

[1066] 56. A compound according to any one of the preceding clauses, wherein R 4 express

[1067] -H;

[1068] Saturated, unsubstituted, mono- or poly-substituted by -F -S(=O) 2 C 1-6 -alkyl;

[1069] Saturated, unsubstituted -S(=O) 2 (3-14 membered cycloalkyl);

[1070] Saturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl;

[1071] each unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl);

[1072] unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl);

[1073] Each unsubstituted, monosubstituted or polysubstituted -phenyl or -C 1-6 -alkylene-phenyl; or

[1074] each unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl).

[1075] 57. A compound as described in any one of claims 1 to 55, wherein R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl group (preferably a 3-, 4-, 5- or 6-membered cycloalkyl group); wherein the 3-14-membered cycloalkyl group is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linked; or saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl (preferably 4, 5 or 6 membered heterocycloalkyl); wherein the 3-14 membered heterocycloalkyl is linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linked; or unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl (preferably 6-membered aryl); wherein the 6-14 membered aryl is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linked; or unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl (preferably 5- or 6-membered heteroaryl); wherein the 5-14 membered heteroaryl is connected by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene-linkage.

[1076] 58. A compound according to any one of the preceding clauses, wherein R 3 is H, and R 4 is a residue selected from the group consisting of:

[1077]

[1078]

[1079]

[1080] 59. A compound according to any one of the preceding clauses, wherein R 3 and R 4 together to form a heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine and piperazine, each of which is unsubstituted, independently of one another, selected from the group consisting of -F, -C 1-6 -alkyl, -NH 2 、-NHCH 3 、-N(CH3 ) 2 、-C(=O)NH-C 1-6 -alkyl, -C(=O)N(C 1-6 -alkyl) 2 、-C(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, unsubstituted-pyridyl and unsubstituted or -C 1-6 The substituents of the group consisting of -alkyl mono-substituted 1,2,4-oxadiazole are mono- or poly-substituted.

[1081] 60. A compound according to any one of the preceding clauses, wherein R 5 and R 5 'Independently express

[1082] -H;

[1083] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkyl;

[1084] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -heteroalkyl;

[1085] saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally substituted by in each case a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1 -C 6 -alkylene- or -C 1 -C 6 -heteroalkylene-linkage.

[1086] 61. A compound according to any one of the preceding clauses, wherein R 6 , R 7 and R 8 Independently express

[1087] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF 5 、-CN、-NO 2 , -C(=O)OH, -NH 2 ,

[1088] -C 1-6 -alkyl, -CF 3 , -CHF 2 、-CH 2 F.

[1089] -OC 1-6 -alkyl, -OCF 3 、-OCHF 2 、-OCH 2 F.

[1090] -NHC 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 Substituents are substituted;

[1091] -N(C 1-6 -alkyl) 2 , which is unsubstituted or is substituted by one or more independently selected from -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 Substituents are substituted;

[1092] -C(=O)OC 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 Substituents are substituted;

[1093] -OC(=O)C 1-6 -alkyl, which is unsubstituted or substituted by one or more independently selected from -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 or

[1094] -C 1-6 -heteroalkyl, which is unsubstituted or substituted by one or more independently selected from -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 by a substituent.

[1095] 62. The compound according to any one of the preceding clauses, which is selected from the group consisting of compounds 001-036 as shown in the following table:

[1096]

[1097]

[1098] 63. The compound according to any one of the preceding clauses, which is selected from the group consisting of compounds 037-091 as shown in the following table:

[1099]

[1100]

[1101]

[1102]

[1103]

[1104] 64. A pharmaceutical composition comprising a compound according to any one of the preceding clauses.

[1105] 65. A compound according to any one of items 1 to 63 or a pharmaceutical composition according to item 64 for use in the treatment of pain.

[1106] 66. The compound or pharmaceutical composition for use in the treatment of pain according to item 65, wherein the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain; preferably postoperative pain.

[1107] 67. A method of treating pain, comprising administering to a subject in need thereof a compound according to any one of items 1 to 63 or a pharmaceutical composition according to any one of items 64 to 66.

[1108] 68. The method according to item 67, wherein the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain; preferably post-operative pain.

[1109] 69. A compound according to any one of items 1 to 63 or a pharmaceutical composition according to claim 64 for use in the treatment of epilepsy.

[1110] 70. A method of treating epilepsy comprising administering to a subject in need thereof a compound according to any one of items 1 to 63 or a pharmaceutical composition according to any one of items 64 or 69.

[1111] Example

[1112] The following examples are provided for the purpose of illustrating the present invention and should in no way be construed as limiting the scope of the present invention.

[1113] Representative compounds of the present invention can be synthesized according to the general synthetic methods described below and illustrated in the following schemes. Since the schemes are illustrative, the present invention should not be construed as being limited to the specific chemical reactions and specific conditions described in the schemes and examples. The various starting materials used in the schemes are commercially available or can be prepared by methods well known to those skilled in the art. The variables are as defined herein and are within the technical scope of those skilled in the art.

[1114] In the present specification, the abbreviations used, in particular in the schemes and examples, are as follows: ABC—ammonium bicarbonate in water, ACN—acetonitrile, AcOH—acetic acid, ADDP—1,1'-(azodicarbonyl)dipiperidine, aq.—water solution, AIBN—azobisisobutyronitrile, CAN—cerium ammonium nitrate, COMU—(1-cyano-2-ethoxy-2-oxoethylideneaminooxy)dimethylamino-morpholinyl-carbonium hexafluorophosphate, D ABCO – 1,4-diazabicyclo[2.2.2]octane, DAST – diethylaminosulfur trifluoride, DBU – 1,8-diazabicyclo[5.4.0]undec-7-ene, DCC – N,N'-dicyclohexylcarbodiimide, DCM – dichloromethane, DEAD – diethyl azodicarboxylate, DIA – diastereomers, DIAD – diisopropyl azodicarboxylate, DEA – diethylamine, DIPEA – diisopropylethylamine , DME – 1,2-dimethoxyethane, DMF – N,N-dimethylformamide, DMSO – dimethyl sulfoxide, DPPA – diphenylphosphoryl azide, 2,4-DNPH-2,4-dinitrophenylhydrazine, DTBAD – tert-butyl azodicarboxylate, EDCI or EDC – 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide, En – enantiomer, Et2O – diethyl ether, EtOH – ethanol, EtOA c – ethyl acetate, Eq. – equivalent, FA – formic acid, FCC – flash column chromatography, h – hour, HATU – O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate, HPLC – high performance liquid chromatography, IPA – isopropanol, LAH – lithium aluminum hydride, LG – leaving group, MeOH – methanol, MgSO4 – magnesium sulfate, min. – minute, Ms – methanesulfonyl, Na 2 SO 4– sodium sulfate, NBS – N-bromosuccinimide, nBuLi – n-butyllithium, NMP – 1-methyl-2-pyrrolidone, Pd(PPh3)4 – tetrakis-(triphenylphosphine)-palladium(0), Pd2(dba)3 – tris(dibenzylideneacetone)dipalladium, Petether – petroleum ether, PPh3 – triphenylphosphine, PS-DIEA – polystyrene-supported diisopropylethylamine, PS-PPh3 – polystyrene-supported triphenylphosphine, PyBop – benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, PTSA – p-toluenesulfonic acid, RF: borderline Ratio, RM – reaction mixture, RP – reverse phase, RT – room temperature, sat. – saturated, SEM – [2-(trimethylsilyl)ethoxy]methyl acetal, SFC – supercritical fluid chromatography, SPE – solid phase extraction, TBDMS – tert-butyldimethylsilyl ether, TBAF – tetrabutylammonium fluoride hydrate, TBAI – tetrabutylammonium iodide, TEA – triethylamine, THF – tetrahydrofuran, TFA – trifluoroacetic acid, TLC – thin layer chromatography, TPP – triphenylphosphine, IPA – isopropanol, TMS – trimethylsilyl, T3P – propylphosphonic anhydride.

[1115] Compounds of interest having structures according to Formula (A) and all other formulae described herein and embodiments thereof can be prepared as outlined in General Chemical Scheme 1.

[1116]

[1117] Solution 1: All V, R 1 , R 2 , R 3 , R 4 and R 5 As described for the compounds of the present invention. 5 At each occurrence, up to two independent substituents (i.e., R 5 and R 5 ').

[1118] 4-(Benzyloxy)pyridine of Formula 1 can be reacted with a reagent bearing an electrophilic amine (e.g., 2,4-DNPH, O-(mesitylenesulfonyl)hydroxylamine, etc.) in a suitable solvent (e.g., MeCN, DMF, NMP, etc.) to give an N-aminopyridinium salt of Formula 2. The intermediate of Formula 2 can be condensed with an alkyne ester derivative 3 (commercially available or synthesized by procedures known to those skilled in the art) (wherein R2 is an ester protecting group (e.g., methyl, ethyl, tert-butyl, etc.) in the presence of a base (e.g., potassium carbonate, DBU, etc.) in a polar solvent (e.g., DMF, DCM, MeCN, etc.) at a temperature in the range of 0 to 100° C. to give a pyrazolo[1,5-a]pyridine of Formula 4. The ester derivative 4 can then be converted to an intermediate compound of Formula 5 via a hydrogenation reaction with a reducing agent (e.g., hydrogen, ammonium formate, cyclohexadiene, etc.) using a catalyst (more preferably Pd or Pt) in a solvent (e.g., THF, EtOH, etc.). The intermediate of Formula 5 can then be catalyzed at a temperature ranging from 0°C to 100°C in the presence or absence of a chelating agent (e.g., 18-crown-6, cis-trans-cis-bicyclohexano-18-crown-6, etc.) in a polar solvent (e.g., MeCN, DMF, NMP, etc.) in the presence of a base (e.g., DIPEA, DBU, triethylamine, Cs 2 CO 3 In the presence of 6a (e.g., 6a), an intermediate of formula 6a (commercially available or synthesized) is used to convert to the desired compound of formula 7 via nucleophilic substitution, wherein LG is a leaving group. Alternatively, the intermediate of formula 5 can be replaced by reacting with an intermediate of formula 6b (commercially available or synthesized) at a temperature ranging from 0°C to 100°C in a solvent (e.g., THF, toluene, etc.) in the presence of an azodicarboxylic acid reagent (e.g., DEAD, DIAD, ADDP, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.) to obtain the desired compound of formula 7. The ester derivative 7 can then be converted to the desired compound of formula 8 via a standard saponification reaction. Alternatively, the benzyl derivative 4 can then be converted to the desired compound of formula 8 via a standard saponification reaction. The desired compounds of Formula 10 can be obtained from acid derivatives of Formula 8 by reaction with amine derivatives of Formula 9 (commercially available or synthesized by procedures known in the art or as described in the Examples below) in polar aprotic solvents (e.g., DCM, DMF, etc.) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.). Alternatively, the formic acid derivatives of Formula 8 can be converted to acid chloride derivatives by procedures known to those skilled in the art or as described in the Examples below, and then reacted with amines of Formula 9 by procedures known to those skilled in the art or as described in the Examples below to obtain the desired pyrazolo[1,5-a]pyridines of Formula 10.

[1119] Compounds of interest having structures according to Formula (A) and all other formulae described herein and embodiments thereof can be prepared as outlined in General Chemical Scheme 2.

[1120]

[1121] Solution 2: All V, n, R 1 , R 2 R 3 , R 4 and R 5 As described for the compounds of the present invention. 5 At each occurrence, up to two independent substituents (i.e., R 5 and R 5 In some embodiments, the integer n may be in the range of 1 to 10.

[1122] 4-(Benzyloxy)pyridine of formula 11 can be reacted with a reagent bearing an electrophilic amine (e.g., 2,4-DNPH, O-(mesitylenesulfonyl)hydroxylamine, etc.) in a suitable solvent (e.g., MeCN, DMF, NMP, etc.) to give N-aminopyridinium salts of formula 12. Intermediates of formula 12 can be condensed with alkyne ester derivatives 13 (commercially available or synthesized by procedures known to those skilled in the art) (wherein R2 is an ester protecting group (e.g., methyl, ethyl, tert-butyl, etc.) in the presence of a base (e.g., potassium carbonate, DBU, etc.) in a polar solvent (e.g., DMF, DCM, MeCN, etc.) at a temperature in the range of 0 to 100° C. to give pyrazolo[1,5-a]pyridine of formula 14. The ester derivative 14 can then be converted to an intermediate compound of Formula 15 via a hydrogenation reaction with a reducing agent (e.g., hydrogen, ammonium formate, cyclohexadiene, etc.) using a catalyst (more preferably Pd or Pt) in a solvent (e.g., THF, EtOH, etc.). The intermediate of Formula 15 can then be converted to an intermediate compound of Formula 15 in a polar solvent (e.g., MeCN, DMF, NMP, etc.) in the presence or absence of a chelating agent (e.g., 18-crown-6, cis-trans-cis-bicyclohexano-18-crown-6, etc.) at a temperature ranging from 0°C to 100°C in the presence or absence of a chelating agent (e.g., 18-crown-6, cis-trans-cis-bicyclohexano-18-crown-6, etc.). 2 CO 3The intermediate of formula 16a (commercially available or synthesized) is converted to the desired compound of formula 17 via nucleophilic substitution in the presence of LG, wherein LG is a leaving group. Alternatively, the intermediate of formula 15 can be instead reacted with the intermediate of formula 16b (commercially available or synthesized) at a temperature ranging from 0°C to 100°C in a solvent (e.g., THF, toluene, etc.) in the presence of an azodicarboxylic acid reagent (e.g., DEAD, DIAD, ADDP, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.) to obtain the desired compound of formula 17. The ester derivative 17 can then be converted to the desired compound of formula 18 via a standard saponification reaction. Alternatively, the benzyl derivative 14 can then be converted to the desired compound of formula 18 via a standard saponification reaction. The desired compounds of Formula 20 can be obtained from acid derivatives of Formula 18 by reaction with amine derivatives of Formula 19 (commercially available or synthesized by procedures known in the art or as described in the Examples below) in polar aprotic solvents (e.g., DCM, DMF, etc.) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.). Alternatively, the formic acid derivatives of Formula 18 can be converted to acid chloride derivatives by procedures known to those skilled in the art or as described in the Examples below, and then reacted with amines of Formula 9 by procedures known to those skilled in the art or as described in the Examples below to obtain the desired pyrazolo[1,5-a]pyridines of Formula 20.

[1123] Table 3: Exemplary compounds

[1124]

[1125]

[1126] Table 4: Exemplary compounds

[1127]

[1128]

[1129]

[1130]

[1131]

[1132]

[1133] The following examples are provided for the purpose of illustrating the present invention and should in no way be construed as limiting the scope of the present invention.

[1134] Part A presents the preparation of compounds, while Part B presents the pharmacological examples.

[1135] Section A

[1136] All starting materials not explicitly described were commercially available (detailed information on suppliers, e.g., ABCR, ApolloScientific Combi-Blocks, Enamine, FluoroChem, MatrixScientific, Maybridge, Merck, TCI, etc. can be found in e.g. database) or its synthesis has been precisely described in the specialist literature (for example, the experimental instructions can be found in Database or database) or can be prepared using conventional methods known to those skilled in the art.

[1137] If necessary, the reaction was carried out under an inert atmosphere (mainly argon and N 2 ) are carried out under the conditions of . Between different reactions carried out by similar methods, the equivalent number of reagents and the amount of solvent used as well as the reaction temperature and time may vary slightly. Post-treatment and purification methods are adjusted according to the characteristic properties of each compound and may vary slightly for similar methods. The yield of the prepared compound is not optimized.

[1138] "Equivalent" ("eq." or "eq" or "equiv.") means molar equivalent, "RT" or "rt" means room temperature T (23±7°C), "M" means concentration in mol / l, "sol." means solution, and "conc." means concentrated. The mixing ratio of solvents is usually expressed in volume / volume ratio.

[1139] pass 1 H-NMR spectroscopy and / or mass spectrometry (MS, [M+H] + and / or [MH] – All exemplary compounds and selected intermediates were subjected to critical analytical characterization (m / z). In some cases, for example, regioisomers and / or diastereomers may be formed during the reaction, and additional analysis was performed in some cases, such as 13 C NMR and NOE (Nuclear Overhauser Effect) NMR experiments.

[1140] The analytical instrument used is, for example, a BRUKER 400MHz or BRUKER 500MHz machine (software Topspin) for NMR analysis, alternatively a BRUKER AVANCE 300MHz and 400Mhz is used. For LC / MS analysis, for example, an Agilent 1290infinity, Mass: 6150SQD (ESI / APCI) or Agilent 1200SERIES, Mass: 6130SQD (ESI / APCI) (software Chemistation) is used. Analytical HPLC is measured, for example, on Waters (software Empower), Agilent-1200-ELSD (software Chemistation) or Agilent-1260 (software OpenLAB). Analytical SFC is carried out, for example, on PIC solution (software: SFC PICLAB ONLINE), WATERS-X5 (software MASSLYNX) or WATERS-UPC2 (Empower).

[1141] Preparative HPLC is performed, for example, on Waters 2998 (software Empower) or YMC (software K-Prep). Preparative SFC is performed, for example, on Waters, SFC-200 (software Chromscope or Super chrome), Waters, SFC-80 (Superchrome) or PIC, PIC-175 (software S10-100).

[1142] The structures of exemplary compounds containing stereocenters are drawn and named with absolute stereochemistry, if known. In the case of unknown absolute stereochemistry, the compounds may be racemic, a mixture of diastereomers, pure diastereomers of unknown stereochemistry, or pure enantiomers of unknown stereochemistry. Dia 1 and Dia 2 mean that the diastereomers are separated, but the stereochemistry is unknown. En 1 and En 2 mean that both enantiomers are separated, but the absolute configuration is unknown. Unless the chemical name of the compound specifies the exact stereochemistry, no suffix is ​​given after the compound code, which means that the compound containing the stereocenter is obtained as a racemic mixture or a mixture of diastereomers, respectively.

[1143] Synthesis of ethyl 5-(benzyloxy)-2-methylpyrazolo[1,5-a]pyridine-3-carboxylate (Int-01).

[1144]

[1145] Step 1: To a stirred solution of 4-benzyloxy-pyridine (60 g, 324.3.961 mmol) in MeCN (600 mL) at room temperature was added 2,4-DNPH (64.5 g, 324.3 mmol). The reaction mixture was heated to 40 °C and stirred at 40 °C for 16 h. The reaction mixture was concentrated under reduced pressure, keeping the water bath temperature below 40 °C to give 1-amino-4-benzyloxy-pyridinium. To a solution of 1-amino-4-benzyloxy-pyridinium in DMF (600 mL) at room temperature was added potassium carbonate (447.5 g, 3243.2 mmol), followed by but-2-ynoic acid methyl ester (56.6 mL, 486.4 mmol). The reaction mixture was stirred at room temperature for 16 h. The reaction mixture was quenched with ice-cold water and extracted with EtOAc:MTBE (1:3, 3 L). The combined organic layers were washed with brine (900 mL×2) and purified by anhydrous Na 2 SO 4 The crude product was purified by column chromatography on silica gel (100-200 mesh) using 20% ​​to 25% EtOAc in Pet ether as eluent to afford ethyl 5-(benzyloxy)-2-methylpyrazolo[1,5-a]pyridine-3-carboxylate (Int-01) (20 g, 19.8% for two steps) as an off-white solid. 1 H-NMR(400MHz, CDCl3)d[ppm]:8.21-8.23(m,1H),7.26-7.47(m,7H),6.60-6.62(m,1H),5.15(s,2H),4.36(q,3H),2.62(s,3H),1.40(t,3H).

[1146] Synthesis of 2-amino-3-((tert-butyldimethylsilyl)oxy)-2-methylpropanamide (Int-02).

[1147]

[1148] Step 1: To a stirred solution of 1-(tert-butyl-dimethyl-silanyloxy)-propan-2-one (25 g, 132.7 mmol) in EtOH (250 ml) at room temperature, 4-methoxybenzylamine (19.08 ml, 146 mmol) was added. Trimethylsilyl cyanide (19.93 ml, 159.286 mmol) was then added to the reaction mixture at room temperature followed by ammonium chloride (2.13 g, 39.8 mmol). The reaction mixture was stirred at 80 °C for 16 h. The reaction mixture was concentrated. The crude product was distributed between EtOAc and a saturated sodium bicarbonate solution. The organic layer was washed with a saline solution, dried over sodium sulfate and concentrated. The crude was purified on FCC using 100-200 silica gel, eluting with 10% EtOAc-hexanes to give 3-(tert-butyl-dimethyl-silanyloxy)-2-(4-methoxy-benzylamino)-2-methyl-propionitrile (25 g, 57%) as a yellow liquid. 1 H-NMR(400MHz,DMSO)δ[ppm]:7.25-7.23(d,2H),6.68-6.86(d,2H),3.72-3.68(m,6H),3.51-3.48(m,1H),1.36(s,3H),0.87(s,9H),0.06(s,6H).

[1149] Step 2: To a stirred solution of 3-(tert-butyl-dimethyl-silanyloxy)-2-(4-methoxy-benzylamino)-2-methyl-propionitrile (10 g, 29.9 mmol) in DMSO (100 ml) was added potassium carbonate (28.92 g, 209.243 mmol) at room temperature. Hydrogen peroxide (14.03 ml, 298.92 mmol) was added dropwise to the reaction at 0°C. The reaction mixture was stirred at room temperature for 16 h. The reaction mixture was quenched with ice-cold water and extracted with MTBE. The organic portion was purified by Na 2 SO 4 The crude material was purified on FCC using 100-200 silica gel, eluting with 50% EtOAc-hexanes to give 3-(tert-butyl-dimethyl-silanyloxy)-2-(4-methoxy-benzylamino)-2-methyl-propionamide (3.4 g, 33%) as an oily liquid. 1H-NMR(400MHz,DMSO)δ[ppm]:7.26-7.24(d,3H),7.06(s,1H),6.87-6.85(d,2H),3.72(s,3H),3.70-3 .68(m,1H),3.58-3.56(m,1H),3.51-3.50(d,2H),2.04(m,1H),1.15(s,3H),0.85(s,9H),0.03(s,6H).

[1150] Step 3: To a stirred solution of -(tert-butyl-dimethyl-silanyloxy)-2-(4-methoxy-benzylamino)-2-methyl-propionamide (3 g, 8.509 mmol) in MeOH (60 ml) was added palladium hydroxide (1.5 g) at room temperature. The reaction mixture was stirred at room temperature under H 2 Stirred under balloon pressure for 4 h. The reaction mixture was filtered through a bed of celite and washed with 10% MeOH-DCM. The combined filtrate was concentrated to give 2-amino-3-((tert-butyldimethylsilyl)oxy)-2-methylpropanamide (Int-02) (1.5 g, 76%) as an off-white solid. 1 H-NMR(400MHz,DMSO)δ[ppm]:7.25(s,1H),6.95(s,1H),3.77-3.74(d,1H),3.70-3 .68(m,1H),3.27-3.24(d,1H),1.82(s,2H),1.04(s,3H),0.85(s,9H),0.02(s,6H).

[1151] Synthesis of ethyl 5-hydroxy-2-methylpyrazolo[1,5-a]pyridine-3-carboxylate (Int-03).

[1152]

[1153] Step 1 To a stirred solution of 5-benzyloxy-2-methyl-pyrazolo[1,5-a]pyridine-3-carboxylic acid ethyl ester (int-01) (10.0 g) in MeOH (650 mL) was added 10% Pd / C (2.5 g) at room temperature. The reaction mixture was heated to 40°C under balloon pressure. 2 The mixture was stirred for 4 h in 4% 4- (2-nitropropene)-2-nitropropene (Int-03) (5.0 g, 70%) under reduced pressure.The reaction mixture was filtered through a bed of diatomaceous earth, and the bed of diatomaceous earth was washed with 10% MeOH (50 mL) in dichloromethane. The combined filtrate was concentrated under reduced pressure. The crude product was ground with MTBE and n-pentane (1:9, 100 mL) to obtain 5-hydroxy-2-methylpyrazolo [1,5-a] pyridine-3-carboxylic acid ethyl ester (Int-03) (5.0 g, 70%), which was a pale solid. 1H-NMR(400MHz,DMSO-d6)d[ppm]:10.89(s,1H),8.49-8.51(m,1H),7.20(s,1H),6.59-6.62(m,1H),4.24(q,2H),2.47(s,3H),1.32(t,3H).

[1154] Synthesis of 2-amino-2-(hydroxymethyl)butanamide (Int-04).

[1155]

[1156] Step 1: A mixture of sodium cyanide (4.45 g, 90.90 mmol), ammonium chloride (4.9 g, 90.90 mmol) and ammonia solution (7 M in methanol, 120 mL) in methanol (65 ml) was stirred at room temperature and stirred for 10 min, then 1-hydroxybutan-2-one (4.0 g, 45.45 mmol) was added. The reaction mixture was stirred at room temperature for 24 h and filtered through a celite bed, which was washed with methanol (50 mL). The combined filtrate was concentrated under vacuum. Ethyl acetate (80 mL) was added to the residue, and the mixture was filtered. The filtrate was concentrated under vacuum. The residue was co-distilled with dichloromethane (2 x 50 mL) to give 2-amino-2-(hydroxymethyl)butyronitrile (4.2 g) as a light yellow residue. TLC system: 100% ethyl acetate; RF: 0.3.

[1157] Step 2: To a stirred solution of 2-amino-2-(hydroxymethyl)butyronitrile (2.0 g, 17.54 mmol) in ethanol (20 mL) cooled to 0 °C was added KOH (1.47 g, 26.31 mmol), followed by dropwise addition of 30% H 2 O 2 (2mL). The reaction mixture was stirred at room temperature for 1 h. The reaction progress was monitored by TLC and the reaction mixture was concentrated under vacuum. The crude product was diluted with 10% methanol in dichloromethane (2x 50ml), stirred for 20 minutes and filtered. The filtrate was concentrated under reduced pressure to give 2-amino-2-(hydroxymethyl)butanamide (Int-04) (1.8g) as a viscous residue. TLC system: 10% methanol / dichloromethane; RF: 0.1.

[1158] Synthesis of 2-amino-4,4-difluorobutan-1-ol (Int-05).

[1159]

[1160] Step 1: To a solution of t-BuOK (13.2 g, 117.836 mmol) in DMF (150 mL) at 0°C was added ethyl 2-((diphenylmethylene)amino)acetate (30 g, 112.225 mmol). After 30 min, 1,1-difluoro-2-iodoethane (24.9 g, 130.181 mmol) was added over 10 min, maintaining the temperature at -5°C to 5°C. The reaction mixture was stirred at 5°C for 1 h. Upon completion, the reaction mixture was washed with saturated NH 4 The mixture was diluted with 4% Cl solution (100 mL) and extracted with EtOAc (3×100 mL). The combined organic layers were washed with brine (100 mL) and purified by Na 2 SO 4 Dry, filter and concentrate under reduced pressure.The residue was purified by silica gel FCC using 5% EtOAc in pet ether as eluent to give ethyl 2-((diphenylmethylene)amino)-4,4-difluorobutanoate as a light yellow liquid (30 g, 80.67%). 1 H NMR (400 MHz, CDCl 3 )δppm:7.64(d,2H),7.42–7.48(m,4H),7.31–7.39(m,2H),7.18–7.25(m,2H),5.75– 5.91(tt,1H),4.27–4.30(m,1H),4.12–4.21(m,2H),2.45–2.53(m,2H),1.25(t,3H)

[1161] Step 2: To a solution of ethyl 2-((diphenylmethylene)amino)-4,4-difluorobutanoate (8.0 g, 24.143 mmol) in hexane (40 ml) was added 1N HCL (80 ml) at room temperature. The reaction mixture was stirred at room temperature for 4 h. Upon completion, the reaction mixture was washed with hexane (2×40 mL). The aqueous solution was washed with NaHCO 3 The mixture was basified (pH 8) and extracted with EtOAc (2×100 mL). The combined organic layers were purified by Na 2 SO 4 Drying and concentration under reduced pressure gave the desired product as a brown liquid (2.5 g). 1 H NMR (400 MHz, CDCl 3 )δppm:5.91–6.22(m,1H),4.20(q,2H),3.61–3.65(m,1H),2.24-2.36(m,1H),1.98–2.00(m,1H),1.27(t,3H).

[1162] Step 3: To a solution of ethyl 2-amino-4,4-difluorobutyrate (2.5 g, 14.956 mmol) in EtOH (30 mL) was added sodium borohydride (1.697 g, 44.868 mmol) at 0°C. The reaction mixture was stirred at room temperature for 6 h. The reaction mixture was washed with saturated NH 4 The combined organic layers were washed with brine (20.0 mL) and purified by anhydrous Na 2 SO 4 Drying, filtration and concentration under reduced pressure gave 2-amino-4,4-difluorobutan-1-ol (Int-05) as a yellow liquid (1.2 g, 64.13%).

[1163] Synthesis of 4,4-difluoro-1-methoxy-2-methylbutan-2-amine hydrochloride (Int-06).

[1164]

[1165] Step 1: To a solution of 2-amino-4,4-difluoro-2-methylbutan-1-ol (2.5 g, 17.96 mmol) in toluene (25 mL) was added phthalic anhydride (2.66 g, 17.96 mmol). The reaction mixture was stirred in a sealed tube at 120 °C for 24 h. After consumption, the reaction mixture was concentrated under reduced pressure. The residue was purified by silica gel FCC using 25% EtOAc in pet ether as eluent to give 2-(4,4-difluoro-1-hydroxy-2-methylbutan-2-yl)isoindoline-1,3-dione as a light yellow gum (2.0 1 H NMR (400 MHz, CDCl 3 )δppm:7.79–7.84(m,2H),7.71–7.75(m,2H),6.06–6.37(dt,1H),4.03–4.12(m,2H),3.62(t,1H),2.87–3.00(m,1H),2.29–2.43(m,1H),1.66(s,3H).g, yield: 41.34%).

[1166] Step 2: To a solution of 2-(4,4-difluoro-1-hydroxy-2-methylbutan-2-yl)isoindoline-1,3-dione (2.6 g, 9.657 mmol) in DMF (26 mL) at 0°C was added NaH (60% in mineral oil) (463.51 mg, 19.313 mmol), iodomethane (1.194 mL, 19.31 mmol). The reaction mixture was stirred at room temperature for 2 h. After consumption, the reaction mixture was quenched with ice-cold water (20 mL) and extracted with EtOAc (2 x 40 mL). The organic layer was purified by Na 2 SO 4 Dry, filter and concentrate under reduced pressure.The residue was purified by silica gel FCC using 25% EtOAc in pet ether as eluent to give 2-(4,4-difluoro-1-methoxy-2-methylbutan-2-yl)isoindoline-1,3-dione as a light yellow gum (1.1 g, yield: 40.21%). 1 HNMR (400MHz, CDCl 3 )δppm:7.76–7.81(m,2H),7.67–7.72(m,2H),5.87–6.17(dt,1H),3.99(d,1H) ,3.79(d,2H),3.36(d,3H),2.77–2.90(m,1H),2.40–2.53(m,1H),1.82(s,3H).

[1167] Step 3: To a solution of 2-(4,4-difluoro-1-methoxy-2-methylbutan-2-yl)isoindoline-1,3-dione (1.1 g, 3.883 mmol) in IPA (22 mL) and water (2.2 mL) was added NaBH at 0 °C. 4 (733.9 mg, 19.41 mmol). The reaction mixture was stirred at room temperature for 16 h. After completion, the reaction mixture was concentrated, and the resulting residue was quenched with cold water (30 mL) and extracted with EtOAc (2 × 30 mL). The organic layer was washed with brine (20 mL) and purified by anhydrous Na 2 SO 4 The product was stirred for 2 hours at 4 ℃ for 1 h.Then the mixture was stirred for 2 hours at 4 ℃ for 3 hours.The mixture was dried, filtered and concentrated under reduced pressure.The residue was treated with 6N HCl (22mL) and heated to 80 ° C and continued for 2h.The reaction mixture was concentrated under reduced pressure and the residue obtained was ground with ether (2x 30mL).The solid was filtered and dried under vacuum to obtain 4,4-difluoro-1-methoxy-2-methylbutan-2-amine hydrochloride (Int-06), which was a pale solid (650mg, yield: 88.27%). 1 HNMR (400 MHz, DMSO-d 6)δppm:8.40(s,3H),6.20–6.50(dt,1H),3.43(s,2H),3.33(s,3H),2.19–2.30(m,2H),1.29(s,3H).

[1168] Synthesis of methyl 1-amino-2,2-difluorocyclopropane-1-carboxylate hydrobromide (Int-07).

[1169]

[1170] Step 1: To a solution of methyl 2-(((benzyloxy)carbonyl)amino)acrylate (2.5 g, 10.627 mmol) in toluene (50 mL) was added NaF (44.61 mg, 1.063 mmol) at room temperature and heated to 110 °C. After 10 min, a solution of trimethylsilyl 2,2-difluoro-2-(fluorosulfonyl)acetate (5.236 mL, 26.56 mmol) in toluene (50 mL) was added dropwise to the RM over 4 h. The reaction mixture was stirred at 110 °C for 18 h. Upon completion, the reaction mixture was cooled to 0 °C and heated with saturated Na 2 CO 3 The solution was quenched with EtOAc (70 mL) and extracted with EtOAc (2×70 mL). The combined organic layers were washed with brine solution (50 mL) and purified by Na 2 SO 4 Dry, filter and concentrate under reduced pressure.The residue was purified by silica gel FCC using 15% EtOAc in pet ether as eluent to give methyl 1-(((benzyloxy)carbonyl)amino)-2,2-difluorocyclopropane-1-carboxylate as a light yellow liquid (1.4 g, yield: 46.18%). 1 H NMR (400 MHz, CDCl 3 )δppm:7.32–7.38(m,5H),5.57(s,1H),5.14(s,2H),3.77(s,3H),2.66–2.71(m,1H),1.75–1.95(m,1H).

[1171] Step 2: 1-(((benzyloxy)carbonyl)amino)-2,2-difluorocyclopropane-1-carboxylic acid methyl ester (1.4 g, 4.908 mmol) and HBr in acetic acid (33%) (7.5 mL) were stirred at room temperature for 2 h. After consumption, the reaction mixture was concentrated under reduced pressure and the obtained residue was ground with ether (2 x 30 mL). The obtained solid was filtered and dried under vacuum to give 1-amino-2,2-difluorocyclopropane-1-carboxylic acid methyl ester hydrobromide (Int-07) as a light brown solid (1.0 g, yield: 87.81%). 1H NMR (400 MHz, DMSO-d 6 )δppm:9.15(s,2H),3.82(s,3H),2.69–2.78(m,1H),2.43–2.51(m,1H).

[1172] Synthesis of (cis-1-amino-2-(difluoromethyl)cyclopropyl)methanol hydrochloride (Int-08).

[1173]

[1174] Step 1: at room temperature, to the solution of (cis-2-(difluoromethyl)-1-(hydroxymethyl)cyclopropyl)carbamic acid tert-butyl ester (880mg, 3.318mmol) in DCM (10mL), 4M HCl in dioxane (5.0mL) solution is added.The reaction mixture is stirred at room temperature for 1h.After consumption, the reaction mixture is concentrated under reduced pressure and the obtained residue is ground with ether (2x 20mL).The residue is dried under vacuum to obtain cis-1-amino-2-(difluoromethyl)cyclopropyl)methanol hydrochloride (Int-08), which is a light yellow jelly (700mg). 1 H NMR (400 MHz, CDCl 3 )δppm:9.19(s,2H),6.00–5.70(dt,1H),3.70(s,3H),2.80-2.70(m,1H),2.23-2.18(m,1H),1.90-1.86(m,1H).

[1175] Synthesis of 2-amino-2-(1-cyclopropyl-1H-imidazol-2-yl)ethan-1-ol hydrochloride (Int-09).

[1176]

[1177] Step 1: In N 2 Atmosphere, at room temperature, 2-methylpropane-2-sulfinamide (1.53g, 12.62mmol) and copper (II) sulfate (3.66g, 22.94mmol) were added to a solution of 2-((tert-butyldimethylsilyl)oxy)acetaldehyde (2g, 11.47mmol) in DCM (30mL). The reaction mixture was stirred at room temperature for 12h. After completion, the reaction mixture was filtered and rinsed with DCM (50mL). The filtrate was concentrated under reduced pressure. The residue was passed through silica gel FCC, using 10% EtOAc in Pet. ether as eluent to purify to obtain (E / Z)-N-(2-((tert-butyldimethylsilyl)oxy)ethylidene)-2-methylpropane-2-sulfinamide as a light yellow jelly (1.5g, yield: 47.11%).1 H NMR (400 MHz, CDCl 3 )δppm:7.96(s,1H),4.44(s,2H),1.10(s,9H).0.82(s,9H).

[1178] Step 2: At -78 ° C, a solution of 1-cyclopropyl-1H-imidazole (500 mg, 4.62 mmol) in THF (22 mL) was treated dropwise with nBuLi (5 mL, 2.5 M). The reaction mixture was stirred at -78 ° C for 2 h. After 2 h, a solution of (E)-N-(2-((tert-butyldimethylsilyl)oxy)ethylidene)-2-methylpropane-2-sulfinamide (1.54 g, 5.54 mmol) in THF (2 mL) was added dropwise to the reaction mixture. The reaction mixture was stirred for 1.5 h. After completion, the reaction mixture was heated at 0 ° C with saturated NH 4 The mixture was quenched with Cl (25 mL) and extracted with EtOAc (3×30 mL). The combined organic layers were washed with brine (30 mL) and concentrated to give the compound (1.5 g, 84%).

[1179] Step 3: To a solution of N-(2-((tert-butyldimethylsilyl)oxy)-1-(1-cyclopropyl-1H-imidazol-2-yl)ethyl)-2-methylpropane-2-sulfinamide (1.3 g, 3.37 mmol) in 1,4-dioxane (10 mL) was added 4M HCl in 1,4-dioxane (5 mL) at 0°C. The reaction mixture was stirred at room temperature for 16 h. After consumption, the reaction mixture was concentrated under reduced pressure. The residue was triturated with DCM (2 x 5 mL) and dried under vacuum to give 2-amino-2-(1-cyclopropyl-1H-imidazol-2-yl)ethan-1-ol hydrochloride (Int-09) as a brown gum (800 mg, 88%).

[1180] Synthesis of ethyl 2-amino-2-(1-methyl-1H-pyrazol-3-yl)propanoate (Int-10).

[1181]

[1182] Step 1: To a solution of ethyl 2-((diphenylmethylene)amino)acetate (5.0 g, 18.704 mmol), 3-bromo-1-methyl-1H-pyrazole (2.850 mL, 28.056 mmol) in toluene (50 mL in a 100 mL sealed tube) was added K 3 PO 4(11.907 g, 56.113 mmol). The reaction mixture was degassed with argon for 20 min. Pd(t-Bu3P)2 (955.87 mg, 1.870 mmol) was added at room temperature. The resulting reaction mixture was stirred at 100 °C for 16 h. After completion, the reaction mixture was diluted with cold water (100 mL) and extracted with EtOAc (2 x 100 mL). The combined organic layers were washed with brine (100 mL) and purified by Na 2 SO 4 The residue was purified by silica gel FCC using 12% EtOAc in pet ether as eluent to give ethyl 2-((diphenylmethylene)amino)-2-(1-methyl-1H-pyrazol-3-yl)acetate as a light yellow gum (2.5 g, yield: 38.47%). 1 H NMR (400 MHz, CDCl 3 )δppm:7.68-7.71(q,2H),7.42-7.44(m,3H),7.36-7.38(m,1H),7.30-7.33(m,3H),7.1 7-7.20(m,2H),6.45(d,1H),5.34(s,1H),4.15-4.19(m,2H),3.84(s,3H),1.22(t,3H).

[1183] Step 2: To a solution of ethyl 2-((diphenylmethylene)amino)-2-(1-methyl-1H-pyrazol-3-yl)acetate (1.8 g, 5.181 mmol) in DMF (20 mL, placed in a sealed tube) was added NaH (60%) (621 mg, 15.543 mmol) in portions at 0°C. The reaction mixture was stirred at 0°C for 30 min. After 30 min, iodomethane (1.613 mL, 25.90 mmol) was added. The reaction mixture was stirred at room temperature for 16 h. Upon completion, the reaction mixture was quenched with cold water (50 mL) and extracted with EtOAc (2 x 50 mL). The combined organic layers were washed with brine (50 mL) and purified by anhydrous Na 2 SO 4 Dry, filter and concentrate under reduced pressure. The residue was purified by silica gel FCC using 20% ​​EtOAc in pet ether as eluent to give ethyl 2-((diphenylmethylene)amino)-2-(1-methyl-1H-pyrazol-3-yl)propanoate as a light brown gum (1.0 g, yield: 53.40%). 1 H NMR (400 MHz, DMSO-d 6)δppm:7.48-7.52(m,3H),7.34-7.42(m,6H),6.34(d,2H),5.75(s,1H),3.63-3.75(m,5H),1.62(s,3H),1.00(t,3H).

[1184] Step 3: To a solution of ethyl 2-((diphenylmethylene)amino)-2-(1-methyl-1H-pyrazol-3-yl)propanoate (1.6 g, 4.427 mmol) in hexane (15 mL) was added 1N HCl (aq) (30 mL) at room temperature. The reaction mixture was stirred for 16 h. Upon completion, the reaction mixture was extracted with EtOAc (3 x 20 mL). The aqueous layer was washed with saturated NaHCO 3 The solution was basified (pH 0.8) and extracted with 10% MeOH in DCM (3 x 30 mL). The combined organic layers were purified by Na 2 SO 4 Drying, filtration and concentration under reduced pressure gave ethyl 2-amino-2-(1-methyl-1H-pyrazol-3-yl)propanoate (Int-10) as a brown liquid (630 mg, 72.24%). 1 H NMR (400 MHz, DMSO-d 6 )δppm:7.54(s,1H),6.18(s,1H),4.00-4.07(m,2H),3.99(s,3H),2.21(s,2H),1.50(s,3H),1.12(t,3H).

[1185] Synthesis of trans-tert-butyl 3-amino-4-(trifluoromethyl)pyrrolidine-1-carboxylate (Int-11).

[1186]

[1187] Step 1: To a solution of trans-1-(tert-butoxycarbonyl)-4-(trifluoromethyl)pyrrolidine-3-carboxylic acid (3 g, 10.591 mmol) in xylene (25 mL) was added TEA (1.771 mL, 12.710 mmol) and DPPA (2.505 mL, 11.651 mmol) dropwise at room temperature. The reaction mixture was heated to 130 °C and stirred for 1 h. After 1 h, benzyl alcohol (1.211 mL, 11.651 mmol) was added to the reaction mixture and stirred at 130 °C for 3 h. After cooling to room temperature, the reaction mixture was quenched with 1N NaOH solution (80.0 mL) and washed with EtOAc (2 x 50 mL). The aqueous layer was acidified by washing with aqueous citric acid solution (pH ~ 5) and extracted with DCM (2 x 80 mL). The organic layer was washed with brine (50 mL) and purified by Na 2SO 4 Dry, filter and concentrate under reduced pressure.The residue was purified by silica gel FCC using 15% EtOAc in pet ether as eluent to give trans-tert-butyl 3-(((benzyloxy)carbonyl)amino)-4-(trifluoromethyl)pyrrolidine-1-carboxylate as a yellow solid (2.2 g, 53.48%). 1 H NMR (400 MHz, DMSO-d 6 )δppm:7.32–7.38(m,7H),5.10(s,3H),4.69(d,1H),4.35-4.40(m,1H),3.77-3.82(m,1H),3.49(s,2H),2.94(s,2H),1.45(s,9H).

[1188] Step 2: To a solution of trans-tert-butyl 3-(((benzyloxy)carbonyl)amino)-4-(trifluoromethyl)pyrrolidine-1-carboxylate (2.4 g, 6.179 mmol) in EtOAc (20 mL) was added 10% Pd / C (1.315 g, 12.359 mmol). The reaction mixture was stirred at room temperature under hydrogen balloon pressure for 16 h. Upon completion, the reaction mixture was filtered through a pad of celite, washed with EtOAc (2x100 mL), and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel FCC using 45% EtOAc in pet ether as eluent to give trans-tert-butyl 3-amino-4-(trifluoromethyl)pyrrolidine-1-carboxylate (Int-11) as a colorless liquid (1.3 g, 82.74%). 1 H NMR (400 MHz, DMSO-d 6 )δppm:3.49-3.62(m,3H),3.26-3.31(m,2H),2.96(s,1H),2.85(s,1H),1.82-1.98(m,2H),1.39(s,9H).

[1189] Synthesis of benzyl 3-amino-3-(2,2-difluoroethyl)piperidine-1-carboxylate (Int-12).

[1190]

[1191] Step 1: To a solution of 1-((benzyloxy)carbonyl)-3-(2,2-difluoroethyl)piperidine-3-carboxylic acid (2.0 g, 6.114 mmol) in toluene (20 mL) was added TEA (1.704 mL, 12.228 mmol) and DPPA (1.446 mL, 6.725 mmol) dropwise at room temperature. The reaction mixture was heated at 100 °C for 2 h. After cooling to room temperature, the reaction mixture was diluted with water and extracted with EtOAc (2 x 100 mL). The combined organic layers were washed with brine (50 mL) and purified by Na 2 SO 4 Dry, filter and concentrate under reduced pressure to give benzyl 3-(2,2-difluoroethyl)-3-isocyanatopiperidine-1-carboxylate as a light yellow liquid (1.8 g, 90.78%).

[1192] Step 2: To a solution of 3-(2,2-difluoroethyl)-3-isocyanatopiperidine-1-carboxylic acid benzyl ester (1.8 g, 5.550 mmol) in 1,4-dioxane (18 mL) was added 6 M aqueous HCl (18 mL). The reaction mixture was heated to 45 ° C and continued for 16 h. After completion, the reaction mixture was concentrated. The residue was diluted with water (50 mL) and washed with EtOAc (100 mL). The aqueous layer was basified with 1N NaOH solution (50 mL) and extracted with DCM (2 x 100 mL). The combined organic layers were washed with brine (10 mL) and purified by Na 2 SO 4 Dry, filter and concentrate under reduced pressure to give benzyl 3-amino-3-(2,2-difluoroethyl)piperidine-1-carboxylate (Int-12) as a light yellow liquid (900 mg, 54.36%). 1 H NMR (400 MHz, DMSO d 6 )δppm:7.37–7.30(m,5H),6.37–6.07(m,1H),5.06(s,2H),3.56(s,4H),3. 38–3.16(m,3H),1.90–1.79(m,2H),1.65–1.55(m,4H),1.43–1.38(m,2H).

[1193] Synthesis of ethyl 2-amino-2-(1-methyl-1H-pyrazol-3-yl)acetate (Int-13).

[1194]

[1195] Step 1: To a solution of ethyl 2-((diphenylmethylene)amino)-2-(1-methyl-1H-pyrazol-3-yl)acetate (2.4 g, 6.908 mmol, 1.0 equiv) in hexanes (10 mL) was added 1N HCl(aq) (25 mL) at room temperature. The reaction mixture was stirred for 16 h. Upon completion, the reaction mixture was extracted with EtOAc (2 x 30 mL). The aqueous layer was washed with saturated NaHCO 3 The solution was basified (pH 0.8) and extracted with 10% MeOH in DCM (3 x 50 mL). The combined organic layers were purified by Na 2 SO 4 Dry, filter and concentrate under reduced pressure to give 2-amino-2-(1-methyl-1H-pyrazol-3-yl)ethyl 1 H NMR (400 MHz, DMSO-d 6 )δppm:7.57(d,1H),6.15(d,1H),4.43(s,1H),4.11-4.01(m,2H),3.70(s,3H),2.07(s,2H),1.14(t,3H). Ethyl acetate (Int-13) (900mg, 71.11%).

[1196] Synthesis of 2-amino-3-hydroxy-2-methylpropanamide (Int-14).

[1197]

[1198] Step 1: After 10 minutes, 1-hydroxyacetone (3.0 g, 40.54 mmol) was added to a mixture of sodium cyanide (3.97 g, 81.08 mmol), ammonium chloride (4.29 g, 81.08 mmol) and ammonia solution (7 M in methanol, 30 mL). The reaction mixture was stirred at room temperature for 23 hours under nitrogen and then concentrated in vacuo. EtOAc (200 mL) was added to the residue and the solid was filtered. The filtrate was concentrated in vacuo and DCM (1×50 mL) was added to the residue. The solution was cooled to -20°C and allowed to stand at room temperature for 60 h. The precipitate was collected by filtration, washed with cold DCM and dried in vacuo to give 2-amino-3-hydroxy-2-methylpropionitrile (2.0 g, 50%).

[1199] Step 2: To a stirred solution of amino-3-hydroxy-2-methylpropionitrile (2.0 g, 20 mmol) in ethanol (30 mL) at 0°C was added KOH (1.62 g, 30 mmol, 1.5 eq), followed by dropwise addition of H 2 O 2(2mL). The reaction mixture was stirred at room temperature for 18h. The reaction mixture was concentrated under reduced pressure. The residue was diluted with 10% MeOH in DCM (2×100ml), stirred for 20 minutes, then filtered, and the filtrate was concentrated under reduced pressure to give 2-amino-3-hydroxy-2-methylpropionamide (Int-14) (0.6g, 26%).

[1200] Synthesis of ethyl 3-amino-2-oxopyrrolidine-3-carboxylate hydrochloride (Int-15).

[1201]

[1202] Step 1: At 0°C, Boc anhydride (35.8 mL, 155.9 mmol) was added to a solution of diethyl 2-aminomalonate hydrochloride (30 g, 141.7 mmol) and TEA (60.18 mL, 425.25 mmol) in DCM (400 mL). The reaction mixture was stirred at room temperature for 16 h. The RM was diluted with ice water (500 mL) and the organic layer was separated. The organic layer was washed with brine (200 mL) and washed with Na 2 SO 4 Drying, filtration and concentration under reduced pressure gave colorless diethyl 2-((tert-butoxycarbonyl)amino)malonate (35.8 g).

[1203] Step 2: To a solution of diethyl 2-((tert-butoxycarbonyl)amino)malonate (10 g, 36.36 mmol) and sodium ethoxide (1.97 g, 29.08 mmol) in ethanol (300 mL) cooled to 0°C was added a solution of nitroethylene (6.64 g, 90.90 mmol) dissolved in ether (15 mL). The reaction mixture was allowed to slowly reach room temperature. The RM was stirred for 2 h. The RM was diluted with ice water (500 mL) and the organic layer was separated, washed with brine (100 mL), and filtered through Na 2 SO 4 The residue was dried, filtered and concentrated under reduced pressure to give a residue. The residue was purified by reverse phase GRACE flash chromatography using 0.1% FA in water and ACN as eluent. The fractions were collected and concentrated in vacuo to give diethyl 2-((tert-butoxycarbonyl)amino)-2-(2-nitroethyl)malonate (4.1 g).

[1204] Step 3: under inert atmosphere, in Parr hydrogenation vessel, Raney nickel (5.3g) is added to a solution of 2-((tert-butoxycarbonyl) amino)-2-(2-nitroethyl) diethyl malonate (4.0g, 11.49mmol) in ethanol (50mL). Reactant mixture is hydrogenated 16h at 70psi and room temperature. RM is filtered through diatomaceous earth pad, and diatomaceous earth pad is washed with ethanol. The filtrate combined is concentrated under reduced pressure, obtains 3-((tert-butoxycarbonyl) amino)-2-oxopyrrolidine-3-ethyl formate (1.6g), is colorless oil.

[1205] Step 4: HCl (4M in dioxane, 3.6 mL) was added to a stirred solution of ethyl 3-((tert-butoxycarbonyl)amino)-2-oxopyrrolidine-3-carboxylate (1.6 g, 5.9 mmol) in DCM (30 mL) at 0°C. The RM was stirred at room temperature for 2 h. The RM was concentrated in vacuo. The residue was triturated with ether (10 mL), filtered and dried in vacuo to give ethyl 3-amino-2-oxopyrrolidine-3-carboxylate hydrochloride (1.03 g) as an off-white solid.

[1206] Synthesis of 3-amino-3-(hydroxymethyl)pyrrolidin-2-one (Int-16-En1) and (Int-16–En2).

[1207]

[1208] Step 1: To a stirred solution of diethyl 2-(2-(1,3-dioxoisoindolin-2-yl)ethyl)malonate (60 g, 179.99 mmol) in 1,4-dioxane (600 mL) was added TEA (49.90 mL, 359.99 mmol) at 0 °C. After 15 min, formaldehyde (29.18 g, 359.99 mmol) was added at 0 °C. The RM was warmed to room temperature and stirred at 80 °C for 16 h. Upon completion, the reaction mixture was diluted with ice-cold water (200 mL) and extracted with EtOAc (2×300 mL). The combined organic layers were washed with brine (150 mL), purified by Na 2 SO 4 Dry, filter and concentrate under reduced pressure.The residue was purified by silica gel FCC using a gradient of 0-40% EtOAc in pet ether to give diethyl 2-(2-(1,3-dioxoisoindolin-2-yl)ethyl)-2-(hydroxymethyl)malonate (59 g, 90%) as a light yellow gum. 1 H NMR (400 MHz, CDCl 3)δppm:7.86–7.82(m,2H),7.74–7.69(m,2H),4.25–4.18(m,4H),4.07(d,2H),3.83–3.79(m,2H),2.79(t,1H),2.33–2.30(m,2H),1.28(t,6H).

[1209] Step 2: To a stirred solution of diethyl 2-(2-(1,3-dioxoisoindolin-2-yl)ethyl)-2-(hydroxymethyl)malonate (68 g, 187.13 mmol) in DCM (700 mL) at 0°C was added imidazole (25.48 g, 374.27 mmol) and stirred for 15 minutes. Tert-butyldimethylsilyl chloride (33.84 g, 224.56 mmol) was then added at 0°C. The reaction mixture was stirred at room temperature for 16 h. Upon completion, the reaction mixture was diluted with ice-cold water (300 mL) and extracted with DCM (2×500 mL). The combined organic layers were ...

Claims

1. A compound of formula (I), its stereoisomeric form, physiologically acceptable salt, solvate and / or polymorph in R 1 represents -F, -Cl, -Br, -I, -CN, -R W , -OR W , -OC(=O)R W , -NR W R X , - NR W C(=O)R X 、 -SR W 、 -S(=O)R W 、 -S(=O)2R W 、 -C(=O)R W 、 -C(=O)OR W or - C(=O)NR W R X ; Q means -OR 2 or -NR 3 R 4 ; R 2 Indicates -R Y ; R 3 Indicates -OH or -R Y ; R 4 Indicates -R Y or -S(=O)2R Y ; or R 3 and R 4 together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S; T stands for -O- and U stands for -CR 5 R 5 '-; or T means -CR 5 R 5 '- and U means -O-; R 5 and R 5 'Independently represent -R Y ; R 6 , R 7 and R 8 Independently represent -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -R W 、-OR W 、-OC(=O)R W 、-NR W R X 、-NR W C(=O)R X 、-SR W 、-S(=O)R W 、-S(=O)2R W 、-C(=O)R W 、-C(=O)OR W or -C(=O)NR W R X ; V represents a saturated or unsaturated 3-14-membered heterocycloalkyl group; a saturated or unsaturated 3-14-membered cycloalkyl group; a 5-14-membered aryl group; a C1-C6 alkyl group or a 5-14-membered heteroaryl group; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, -CF3, -CF2H, C1-C6 alkyl, -CN, -NO, -NO2, =O, =S, -SF5, -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O)2R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are singly or polysubstituted; in R W and R X Independently of each other and in each case independently represent -H； Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkyl; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-heteroalkyl; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl; wherein the 3-14 membered cycloalkyl is optionally linked via in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene- or -C1-C6-heteroalkylene-; or Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered heterocycloalkyl; wherein the 3-14-membered heterocycloalkyl is optionally linked via in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene- or -C1-C6-heteroalkylene-; R Y and R Z Independently of each other and in each case independently represent -H; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkyl; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-heteroalkyl; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl; wherein the 3-14-membered cycloalkyl is optionally linked via in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene- or -C1-C6-heteroalkylene-; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered heterocycloalkyl; wherein the 3-14-membered heterocycloalkyl is optionally linked via in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene- or -C1-C6-heteroalkylene-; unsubstituted, monosubstituted or polysubstituted 6- to 14-membered aryl; wherein the 6- to 14-membered aryl is optionally linked via in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene- or -C1-C6-heteroalkylene-; or unsubstituted, monosubstituted or polysubstituted 5- to 14-membered heteroaryl; wherein the 5- to 14-membered heteroaryl is optionally linked via in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene- or -C1-C6-heteroalkylene-; or R Y and R Z together form a saturated or unsaturated, unsubstituted or mono- or polysubstituted 4-, 5-, 6-, 7- or 8-membered heterocyclic ring containing 1 to 3 heteroatoms selected from N, O and S; and wherein "mono- or poly-substituted" in each case independently refers to substitution by one or more substituents which are independently selected from the group consisting of: -F, -Cl, -Br, -I, -CN, -C 1-6 -alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -alkylene-O-CF3, -C 1-6 -alkylene-O-CF2H, -C 1-6 -alkylene-O-CFH2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-C 1-6 -alkyl, -C(=O)OH, -C 1-6 -alkylene-C(=O)-OH, -C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-C(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkylene-CF3, -C(=O)-NH2, -C 1-6 -alkylene-C(=O)-NH2, -C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-C(=O)-NH(C 1-6 -alkyl), -C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-C(=O)-N(C 1-6 -alkyl)2, -C(=O)-NH(OH), -C 1-6 -alkylene-C(=O)-NH(OH), -OH, -C 1-6 -alkylene-OH, =O, -OCF3, -OCF2H, -OCFH2, -OCF2Cl, -OCFCl2, -OC 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -OC 1-6 -Alkylene-OC 1-6 -alkyl, -OC 1-6 -Alkylene-NH2, -OC 1-6 -Alkylene-NH-C 1-6 -alkyl, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -OC(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-C 1-6 -alkyl, -OC(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-OC(=O)-OC 1-6 -alkyl, -OC(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OC(=O)-NH(C 1-6 -alkyl), -OC(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OC(=O)-N(C 1-6 -alkyl)2, -OS(=O)2-NH2, -C 1-6 -alkylene-OS(=O)2-NH2, -OS(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-OS(=O)2-NH(C 1-6 -alkyl), -OS(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-OS(=O)2-N(C 1-6 -alkyl)2, -NH2, -NO, -NO2, -C 1-6 -alkylene-NH2, -NH(C 1-6 -alkyl), -N(3-14 membered cycloalkyl)(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C 1-6 -alkylene-OH, -N(H)-C 1-6 -alkylene-OH, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -NH-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-C 1-6 -alkyl, -NH-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-NH-C(=O)-OC 1-6 -alkyl, -NH-C(=O)-NH2, -C 1-6 -alkylene-NH-C(=O)-NH2, -NH-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-C(=O)-NH(C 1-6 -alkyl), -NH-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-C(=O)-N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-C 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-C(=O)-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH2, -N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C(=O)-N(C 1-6 -alkyl)2, -NH-S(=O)2OH, -C 1-6 -alkylene-NH-S(=O)2OH, -NH-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-NH-S(=O)2-C 1-6 -alkyl, -NH-S(=O)2-OC 1-6 -alkyl, -C 1-6 -Alkylene-NH-S(=O)2-OC 1-6 -alkyl, -NH-S(=O)2-NH2, -C 1-6 -alkylene-NH-S(=O)2-NH2, -NH-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-NH-S(=O)2-NH(C 1-6 -alkyl), -NH-S(=O)2N(C 1-6 -alkyl)2, -C 1-6 -alkylene-NH-S(=O)2N(C 1-6 -alkyl)2, -N(C 1-6 -alkyl)-S(=O)2-OH, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OH, -N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-C 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-OC 1-6 -alkyl, -N(C 1-6 -alkyl)-S(=O)2-NH2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH2, -N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-NH(C 1-6 -alkyl), -N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-N(C 1-6 -alkyl)-S(=O)2-N(C 1-6 -alkyl)2, -SH, =S, -SF5, -SCF3, -SCF2H, -SCFH2, -SC 1-6 -alkyl, -C 1-6 -Alkylene-SC 1-6 -alkyl, -S(=O)-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -C 1-6 -alkylene-S(=O)2-C 1-6 -alkyl, -S(=O)2-OH, -C 1-6 -alkylene-S(=O)2-OH, -S(=O)2-OC 1-6 -alkyl 、 -C 1-6 -Alkylene-S(=O)2-OC 1-6 -alkyl 、 -S(=O)2-NH2, -C 1-6 -alkylene-S(=O)2-NH2, -S(=O)2-NH(C 1-6 -alkyl), -C 1-6 -alkylene-S(=O)2-NH(C 1-6 -alkyl), -S(=O)2-N(C 1-6 -alkyl)2, -C 1-6 -alkylene-S(=O)2-N(C 1-6 -alkyl)2,3-14-membered cycloalkyl, -C 1-6 -alkylene-(3-14 membered cycloalkyl), 3 to 14 membered heterocycloalkyl, -C 1-6 -alkylene-(3 to 14-membered heterocycloalkyl), -phenyl, -C 1-6 -alkylene-phenyl, 5- to 14-membered heteroaryl, -C 1-6 -alkylene-(5- to 14-membered heteroaryl), -O-(3- to 14-membered cycloalkyl), -O-(3- to 14-membered heterocycloalkyl), -O-phenyl, -O-(5- to 14-membered heteroaryl), -C(=O)-(3- to 14-membered cycloalkyl), -C(=O)-(3- to 14-membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5- to 14-membered heteroaryl), -S(=O)2-(3- to 14-membered cycloalkyl), -S(=O)2-(3- to 14-membered heterocycloalkyl), -S(=O)2-phenyl, -S(=O)2-(5- to 14-membered heteroaryl).

2. The compound of claim 1, wherein R 3 Indicates -H.

3. The compound as claimed in claim 2, wherein R 4 represents residues other than -H.

4. The compound according to any one of claims 1 to 3, wherein R 1 It represents -methyl or ethyl.

5. A compound as claimed in any one of claims 1 to 3, wherein T represents -O-, and U represents -CR 5 R 5 '-.

6. The compound according to any one of claims 1 to 5, wherein R 5 and R 5’ The R of each of Y It's H.

7. A compound as claimed in any one of claims 1 to 6, wherein V represents (i) a benzoimidazole, benzisoxazole, benzoxazole, benzodioxole, benzofuran, benzothiadiazole, benzothiazole, benzothiophene, carbazole, cinnoline, dibenzofuran, furan, furan, imidazole, imidazopyridine, indazole, indole, indolizine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, 5-14 membered heteroaryl of 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; in each case unsubstituted, independently selected from -F, -Cl, -CN, -OH, =O, -C 1-6 -alkyl, -CHF2, -CF3, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -alkylene-CHF2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-cyclopropyl, -cyclopropyl, -O-cyclopropyl, -C 1-6 -Alkylene-NHC(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -OC 1-6 -alkyl, -OCF3, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -S(=O)2-C 1-6 -alkyl, -azetidine, -C 1-6 -alkylene-O-tetrahydropyran or -C 1-6 The substituents of the -alkyl-substituted-piperazine are mono- or polysubstituted; in particular, in each case unsubstituted, independently of one another, selected from the group consisting of -F, -Cl, -CN, -OH, =O, -C 1-6 -alkyl, -CHF2, -CF3, -C 1-6 -alkylene-NH2, -C 1-6 -Alkylene-NHC(=O)OC 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-NHC(=O)-OC 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -N(C 1-6 -alkyl)2, -OC 1-6 -alkyl, -OCF3, -OC 1-6 -alkylene-N(C 1-6 -alkyl)2, -S(=O)2-C 1-6 -alkyl, -azetidine, -C 1-6 -alkylene-O-tetrahydropyran or -C 1-6 The substituent of the -alkyl-substituted-piperazine is mono- or poly-substituted; or represents (ii) an unsubstituted, mono- or poly-substituted-oxetanyl group.

8. Compounds as described in any one of claims 1 to 6, wherein the saturated or unsaturated 3-14 membered cycloalkyl within the definition of V is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl or cyclodecyl, including unfused or unbridged, fused or bridged cycloalkyl; in each case unsubstituted, independently selected from -F, -Cl, -Br, -I, CF3, -CF2H, C1-C6 alkyl, -CN, -NO, -NO2, =O, =S, -SF5, -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O)2R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

9. The compound of any one of claims 1 to 6, wherein the 5-14 membered aryl within the definition of V is phenyl or another 5-14 membered aryl, which is unsubstituted, independently selected from -F, -Cl, -Br, -I, CF3, -CF2H, C1-C6 alkyl, -CN, -NO, -NO2, =O, =S, -SF5, -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O)2R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

10. The compound of any one of claims 1 to 6, wherein the 3-14 membered heterocycloalkyl group within the definition of V is selected from azepane, 1,4-oxazepane, azetidine, azetidine, aziridine, azocane, diazepane, dioxane, dioxolane, dithiane, dithiolane, imidazoline, isothiazolinone, isoxazolidine, morpholine, oxazolidine, oxane, oxane, oxetane, oxirane, piperazine, piperidine, pyrazolidine, pyrrolidine, quinuclidine, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolidine, thietane, thiirane, thiolane, thiomorpholine, indoline, dihydrobenzofuran, dihydro benzothiophene, 1,1-dioxothiazolin-cyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]-nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydro-cyclopenta[c]pyrrole, octahydro-cyclopenta[c]pyrrole and octahydro-pyrrolo[1,2-a]pyrazine; in each case unsubstituted, independently of one another selected from -F, -Cl, -Br, -I, CF3, -CF2H, C1-C6 alkyl, -CN, -NO, -NO2, =O, =S, -SF5, -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O)2R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

11. as claimed in any one of claims 1 to 6 compounds, wherein V represents C1-C6 alkyl or C1-C6 heteroalkyl, which is saturated or unsaturated, unsubstituted, selected independently from -F, -Cl, -Br, -I, CF3, -CF2H, C1-C6 alkyl, -CN, -NO, -NO2, =O, =S, -SF5, -R Y 、-OR Y 、-OC(=O)R Y 、-NR Y R Z 、-NR Y C(=O)R Z 、-SR Y 、-S(=O)R Y 、-S(=O)2R Y 、-C(=O)R Y 、-C(=O)OR Y or -C(=O)NR Y R Z The substituents are mono- or poly-substituted.

12. The compound of any one of claims 1 to 6, wherein V is a residue selected from the group consisting of:

13. The compound of claim 1, wherein R 1 Indicates -H, -F, -Cl, -Br, -I, -C 1-6 -alkyl, -OC 1-6 -alkyl, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3, -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -alkylene-CF3, -C(=O)C 1-6 -alkyl, -C(=O)OC 1-6 -alkyl, -C(=O)NH2, -C(=O)NHC 1-6 -alkyl, -C(=O)N(C 1-6 -alkyl)2, -S(=O)-C 1-6 -alkyl, -S(=O)2-C 1-6 -alkyl, -OC 1-6 -alkyl, unsubstituted-cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl or unsubstituted cyclohexyl.

14. The compound of claim 1, wherein R 3 Indicates -H, -OH, -C 1-6 -alkyl, -C 1-6 -alkylene-OH, -C 1-6 -Alkylene-OC 1-6 -alkyl, -C 1-6 -alkylene-NH2, -C 1-6 -alkylene-NH(C 1-6 -alkyl), -C 1-6 -alkylene-N(C 1-6 -alkyl)2, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 -alkylene-CF3, -C 1-6 -alkylene-CF2H, -C 1-6 -alkylene-CFH2, -C 1-6 -Alkylene-NH-C 1-6 -alkylene-CF3 or -C 1-6 -alkylene-N(C 1-6 -alkyl)-C 1-6 -Alkylene-CF3.

15. A compound as claimed in any one of claims 1 to 14, wherein R 4 Indicates -H; Saturated, unsubstituted, mono- or poly-substituted by -F -S(=O)2C 1-6 -alkyl; Saturated, unsubstituted -S(=O)2(3-14 membered cycloalkyl); Saturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 -alkyl; each unsubstituted, monosubstituted or polysubstituted 3-14 membered cycloalkyl or -C 1-6 -alkylene-(3-14 membered cycloalkyl); unsubstituted, monosubstituted or polysubstituted 3-14 membered heterocycloalkyl or -C 1-6 -alkylene-(3-14 membered heterocycloalkyl); Each unsubstituted, monosubstituted or polysubstituted -phenyl or -C 1-6 -alkylene-phenyl; or each unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl or -C 1-6 -alkylene-(5-14 membered heteroaryl).

16. A compound as claimed in any one of claims 1 to 14, wherein R 4 represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl (preferably a 3-, 4-, 5- or 6-membered cycloalkyl); wherein the 3-14-membered cycloalkyl is connected via a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene-; or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered heterocycloalkyl (preferably a 4-, 5- or 6-membered heterocycloalkyl); wherein the 3-14-membered heterocycloalkyl is connected via a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene-. or unsubstituted, monosubstituted or polysubstituted 6-14 membered aryl (preferably 6 membered aryl); wherein the 6-14 membered aryl is connected through a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene-; or unsubstituted, monosubstituted or polysubstituted 5-14 membered heteroaryl (preferably 5 or 6 membered heteroaryl); wherein the 5-14 membered heteroaryl is connected through a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene-.

17. A compound as claimed in any one of claims 1 to 16, wherein R 3 is H, and R 4 is a residue selected from the group consisting of:

18. The compound of claim 1, wherein R 3 and R 4 together to form a heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine and piperazine, each of which is unsubstituted, independently of one another, selected from the group consisting of -F, -C 1-6 -alkyl, -NH2, -NHCH3, -N(CH3)2, -C(=O)NH-C 1-6 -alkyl, -C(=O)N(C 1-6 -alkyl)2, -C(=O)OC 1-6 -alkyl, -NHC(=O)OC 1-6 -alkyl, unsubstituted-pyridyl and unsubstituted or -C 1-6 The substituents of the group consisting of -alkyl mono-substituted 1,2,4-oxadiazole are mono- or poly-substituted.

19. The compound of claim 1, wherein R 5 and R 5 'Independently express -H； Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkyl; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-heteroalkyl; Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3-14-membered cycloalkyl; wherein the 3-14-membered cycloalkyl is optionally linked via in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6-alkylene- or -C1-C6-heteroalkylene-.

20. A compound as claimed in any one of claims 1 to 19, wherein R 6 , R 7 and R 8 Independently express -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2, -C 1-6 -alkyl, -CF3, -CHF2, -CH2F, -OC 1-6 -alkyl, -OCF3, -OCHF2, -OCH2F, -NHC 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; -N(C 1-6 -alkyl)2, which is unsubstituted or substituted by one or more substituents independently selected from -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; -C(=O)OC 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; -OC(=O)C 1-6 -alkyl, which is unsubstituted or substituted by one or more substituents independently selected from -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; or -C 1-6 -heteroalkyl, which is unsubstituted or substituted by one or more substituents independently selected from -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2.

21. The compound of claim 1, which is selected from the group consisting of compounds 001-036 as shown in the following table:

22. The compound of claim 1, which is selected from the group consisting of compounds 037-091 as shown in the following table:

23. A pharmaceutical composition comprising a compound as claimed in any one of claims 1 to 22.

24. A compound as claimed in any one of claims 1 to 22 or a pharmaceutical composition as claimed in claim 23 for use in the treatment of pain.

25. The compound or pharmaceutical composition for use in the treatment of pain according to claim 24, wherein the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain; preferably postoperative pain.

26. A method of treating pain comprising administering to a subject in need thereof a compound as claimed in any one of claims 1 to 22 or a pharmaceutical composition as claimed in any one of claims 23 to 25.

27. The method of claim 26, wherein the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain; preferably post-operative pain.

28. A compound as claimed in any one of claims 1 to 22 or a pharmaceutical composition as claimed in claim 23 for use in the treatment of epilepsy.

29. A method for treating epilepsy, comprising administering to a subject in need thereof a compound as claimed in any one of claims 1 to 22 or a pharmaceutical composition as claimed in claim 23.

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