Heterocyclic derivatives for the treatment of trpm3-mediated disorders

Abstract

This invention relates to compounds for the prevention or treatment of TRPM3-mediated conditions, more specifically, conditions selected from pain and inflammatory hypersensitivity reactions. The invention also relates to a method for the prevention or treatment of said TRPM3-mediated conditions.

Description

Technical Field

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

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

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

[0004] It is becoming increasingly clear that TRP channel dysfunction is directly involved in the etiology of a wide range of hereditary and acquired diseases. In fact, loss-of-function and gain-of-function mutations in TRP channel genes have been identified as direct causes of hereditary diseases, including shortness of breath, hypomagnesemia with secondary hypocalcemia, polycystic kidney disease, mucopolysaccharidosis type IV, and familial focal segmental glomerulosclerosis. Furthermore, TRP channel function / dysfunction has been directly associated with a broad range of pathological symptoms, including chronic pain, hypertension, cancer, and neurodegenerative diseases.

[0005] TRPM3 (transient receptor potential M-type 3) represents a promising pharmacological target. TRPM3 is expressed in large sub-concentrations of small-diameter sensory neurons from the dorsal root and trigeminal ganglion and is involved in heat sensing. The neurosteroid pregnenolone sulfate is a known potent activator of TRPM3 (Wagner et al., 2008). Pregnenolone sulfate induces pain in wild-type mice but not in TRPM3 knockout mice. It has also recently been shown that CFA-induced inflammation and inflammatory pain are eliminated in TRPM3 knockout mice. Therefore, TRPM3 antagonists could be used as analgesics to combat pain, such as inflammatory pain (Vriens J. et al., *Neuron*, May 2011).

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

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

[0008] This invention provides benzofuran derivatives and pharmaceutical compositions comprising such benzofuran derivatives. The invention also provides benzofuran derivatives for use as pharmaceuticals, more specifically for the prevention and / or treatment of TRPM3-mediated conditions, particularly for the prevention and / or treatment of pain and / or inflammatory hypersensitivity reactions; and / or for combating pain and / or inflammatory hypersensitivity reactions.

[0009] The present invention also provides the use of benzofuran derivatives in the preparation of pharmaceutical compositions or medicaments for the prevention and / or treatment of TRPM3-mediated conditions, particularly for the prevention and / or treatment of pain and / or inflammatory hypersensitivity; and / or for the treatment of pain and / or inflammatory hypersensitivity.

[0010] The present invention also provides a method for preventing or treating TRPM3-mediated conditions by administering a benzofuran derivative according to the invention to a subject in need. More specifically, the present invention relates to methods for preventing and / or treating pain and / or inflammatory hypersensitivity reactions; and / or for combating pain and / or inflammatory hypersensitivity reactions.

[0011] The present invention further provides a method for preparing the benzofuran derivative of the present invention, the method comprising the following steps:

[0012] - Reaction of benzoquinone with a suitable β-keto ester or enamine derivative yields a 5-hydroxybenzofuran-3-carboxylic acid ester derivative.

[0013] - Under mitomobu conditions, the previously obtained 5-hydroxybenzofuran-3-carboxylic acid ester derivative is replaced with a suitable derivative or alcohol derivative containing a leaving group to obtain a 5-O-substituted benzofuran-3-carboxylic acid ester derivative.

[0014] - Convert the previously obtained 5-O-substituted benzofuran-3-carboxylic acid ester derivative into a carboxylic acid to obtain the desired benzofuran derivative of the present invention, and

[0015] - The previously obtained 5-O-substituted benzofuran-3-carboxylic acid derivative is coupled with a suitable amine to obtain the desired amide derivative of the present invention. Detailed Implementation

[0016] The invention will be further described, and in some cases described with respect to specific embodiments, but the invention is not limited thereto.

[0017] The first aspect of the present invention provides compounds of formula (I), their stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs.

[0018]

[0019] Preferably used for the treatment of pain;

[0020] in

[0021] R 1 This represents -F, -Cl, -Br, -I, -CN, and -R. W -OR W -OC(=O)R W -NR W R X -NR W C(=O)R X -SR W -S(=O)R W-S(=O)2R W -C(=O)R W -C(=O)OR W or -C(=O)NR W R X ;

[0022] Q means -OR 2 or -NR 3 R 4 ;

[0023] R 2 Indicates -R Y ;

[0024] R 3 Indicates -OH or -R Y ;

[0025] R 4 Indicates -R Y or -S(=O)2R Y ;

[0026] Or R 3 and R 4 Together they form saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted 4, 5, 6, 7 or 8-membered heterocycles containing 1 to 3 heteroatoms selected from N, O and S.

[0027] T represents -O- and U represents -CR 5 R 5 '-; or T represents -CR 5 R 5 '-and U represents -O-;

[0028] R 5 and R 5 'Represented independently of each other - R Y ;

[0029] R 6 R 7 and R 8 The following can be represented independently: -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -R W -OR W -OC(=O)R W -NR W R X -NR W C(=O)R X -SR W -S(=O)R W -S(=O)2R W -C(=O)R W -C(=O)ORW or -C(=O)NR W R X ;

[0030] V represents a saturated or unsaturated 3- to 14-membered heterocyclic alkyl group; or a 5- to 14-membered heteroaryl group; in each case, it is unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from -F, -Cl, -Br, -I, -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 ;

[0031] in

[0032] R W and R X Represented independently of each other in each case.

[0033] -H;

[0034] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[0035] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[0036] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl group is optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0037] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0038] R Y and RZ Represented independently of each other in each case.

[0039] -H;

[0040] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[0041] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[0042] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0043] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0044] Unsubstituted, monosubstituted, or polysubstituted 6- to 14-membered aryl groups; wherein the 6- to 14-membered aryl groups are optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0045] Unsubstituted, monosubstituted, or polysubstituted 5- to 14-membered heteroaryl groups; wherein the 5- to 14-membered heteroaryl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted;

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

[0047] Furthermore, "mono- or poly-substituted" in each case independently indicates substitution by one or more, such as 1, 2, 3, 4 or more substituents, which are independently selected from -F, -Cl, -Br, -I, -CN, -C 1-6 Alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-6 Alkylene-CF3, -C1-6 Alkylene -CF2H, -C 1-6 Alkylene -CFH2, -C 1-6 Alkylene -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 group, -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 Alkylenes -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 1-6Alkyl group, -OC (=O)-OC 1-6 Alkyl, -C 1-6 Alkylene-OC(=O)-OC 1-6 Alkyl group, -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 Alkylenes -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 group 2, -NH2, -NO, -NO2, -C 1-6 Alkylene -NH2, -NH(C 1-6 Alkyl), -N (3 to 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 group, -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 1-6Alkyl)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 Alkylenes -NH-S(=O)2OH, -NH-S(=O)2-C 1-6 Alkyl, -C 1-6 Alkylene-NH-S(=O)2-C 1-6 Alkyl group, -NH-S(=O)2-OC 1-6 Alkyl, -C 1-6 Alkylene-NH-S(=O)2-OC 1-6 Alkyl group, -NH-S(=O)2-NH2, -C 1-6 Alkylenes -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 1-6alkyl)-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 group 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 group, -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 Alkylenes -S(=O)2-OH, -S(=O)2-OC 1-6 Alkyl, -C 1-6 Alkylene-S(=O)2-OC 1-6 Alkyl group, -S(=O)2-NH2, -C 1-6 Alkylene -S(=O)2-NH2, -S(=O)2-NH(C 1-6Alkyl), -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 to 14-membered cycloalkyl, -C 1-6 Alkylene (3- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 alkylene-(3 to 14-membered heterocyclic alkyl), -phenyl, -C 1-6 alkylene-phenyl, 5 to 14-membered heteroaryl, -C 1-6 Alkylene-(5 to 14-membered heteroaryl), -O-(3 to 14-membered cycloalkyl), -O-(3 to 14-membered heterocycloalkyl), -O-phenyl, -O-(5 to 14-membered heteroaryl), -C(=O)-(3 to 14-membered cycloalkyl), -C(=O)-(3 to 14-membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5 to 14-membered heteroaryl), -S(=O)2-(3 to 14-membered cycloalkyl), -S(=O)2-(3 to 14-membered heterocycloalkyl), -S(=O)2-phenyl, -S(=O)2-(5 to 14-membered heteroaryl).

[0048] In a preferred embodiment of the benzofuran derivative according to the present invention,

[0049] (a-1)Q means -OR 2 And R 1 Indicates -CH2F, -CHF2, or -CF3; and / or

[0050] (a-2)Q means -OR 2 And R 5 and R 5 At least one of ' does not represent -H; and / or

[0051] (a-3)Q means -OR 2 And R 6 Not indicating -H; and / or

[0052] (a-4)Q means -OR 2 And R 8 It does not represent -H;

[0053] or

[0054] (b-1)Q represents -NR 3 R 4 The condition is that the following compounds and their salts are excluded.

[0055]

[0056] and / or

[0057] (b-2)Q represents -NR 3 R 4 And R 1 It represents -CH2F, -CHF2, -CF3, -CN, -propyl, or -cyclopropyl; and / or

[0058] (b-3)Q represents -NR 3 R 4 And R 5 and R 5 At least one of ' does not represent -H; and / or

[0059] (b-4)Q represents -NR 3 R 4 And R 3 It represents -H.

[0060] In a preferred embodiment of the benzofuran derivative according to the invention, T represents -O- and U represents -CR 5 R 5 According to this embodiment, the benzofuran derivative according to the invention is a compound of formula (II), its stereoisomer, a physiologically acceptable salt, a solvate, and / or a polymorph.

[0061]

[0062] In another preferred embodiment of the benzofuran derivative according to the invention, T represents -CR 5 R 5 '-and U represents -O-.

[0063] In a preferred embodiment of the benzofuran derivative according to the invention, Q represents -NR. 3 R 4 .

[0064] In another preferred embodiment of the benzofuran derivative according to the invention, Q represents -OR 2 .

[0065] In a preferred embodiment of the benzofuran derivative according to the invention, V represents a 5- to 14-membered heteroaryl group, which is unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from -F, -Cl, -Br, -I, -CN, -NO, -NO2, =O, =S, -SF5, -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)2R Y -C(=O)R Y -C(=O)OR Y or -C(=O)NR Y R Z .

[0066] Preferably, the 5 to 14 heteroaryl groups within the definition of V are not unsubstituted, monosubstituted, or polysubstituted benzofurans.

[0067] Preferably, the 5 to 14-membered heteroaryl group in the definition of V is selected from benzimidazole, benzisoxazole, benzoxazole, benzo-m-dioxane, benzofuran, benzothiadiazole, benzothiazol, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazon, imidazole, imidazopyridine, indazole, indole, inazine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthidine, oxadiazole, oxazole, hydroxyindole, phthalazine, purine, Pyrazines, pyrazoles, pyridazines, pyridines, pyrimidines, pyrroles, quinazolines, quinolines, quinoxalines, tetrazolium, thiadiazoles, thiazolium, thiophene, triazines, triazoles, and [1,2,4]triazolo[4,3-a]pyrimidines; in each case, they are unsubstituted, monosubstituted, or polysubstituted, with substituents selected independently from -F, -Cl, -Br, -I, -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 .

[0068] Preferably, the 5 to 14 heteroaryl groups within the definition of V are selected from the group consisting of: furan, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, triazole, pyridine, isoquinoline, benzothiazole, pyridazine, pyrimidine, and imidazopyridine; in each case, they are unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from -F, -Cl, -Br, -I, -CN, -NO, -NO2, =O, =S, -SF5, and -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 .

[0069] Preferably, the 5 to 14 heteroaryl groups within the definition of V are selected from the group consisting of: furan-2-yl, furan-3-yl, thiophene-2-yl, thiophene-3-yl, pyrazol-5-yl, oxazol-5-yl, isoxazol-4-yl, thiazolyl-2-yl, thiazolyl-5-yl, 1,2,4-triazol-3-yl, 1,2,3-triazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl The substituents are: 1-yl isoquinolino-5-yl, benzo[d]thiazolyl-2-yl, pyridazin-3-yl, pyrimidin-5-yl, and imidazo[1,2-a]pyridin-6-yl; in each case, they are unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[0070] In another preferred embodiment of the benzofuran derivative according to the invention, V represents a saturated or unsaturated, unsubstituted, mono- or poly-substituted 3- to 14-membered heterocyclic alkyl group, wherein these substituents are independently selected from -F, -Cl, -Br, -I, -CN, -NO, -NO2, =O, =S, -SF5, -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)2R Y -C(=O)R Y -C(=O)OR Y or -C(=O)NR Y R Z .

[0071] Preferably, the 3 to 14-membered heterocyclic alkyl group defined in V is selected from aziridine, 1,4-oxazacycloheptanidine, aziridine, aziridine, aziridine, aziridine propane, aziridine octane, diazacycloheptanidine, dioxacyclohexane, dioxapentane, dithiazide, dithiopentane, imidazolide, isothiazolidine, isoxazolidine, morpholine, oxazolidine, epoxide, oxazacyclohexane, oxazacyclohexane, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazolide, thiohexane, thiohexane propane, thiohexane pentane, thiomorpholine, indoline, benzodihydrofuran, dihydrobenzothiophene, 1, 1-Dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine; in each case unsubstituted, monosubstituted, or polysubstituted, the substituents being independently selected from -F, -Cl, -Br, -I, -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 .

[0072] Preferably, the 3- to 14-membered heterocyclic alkyl group defined in V is tetrahydropyran or pyrrolidine; in each case, it is unsubstituted, monosubstituted, or polysubstituted, with these substituents independently selected from -F, -Cl, -Br, -I, -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 .

[0073] Preferably, the 3- to 14-membered heterocyclic alkyl group defined in V is tetrahydropyran-4-yl or pyrrolidine-3-yl; in each case, it is unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[0074] In a preferred embodiment of the benzofuran derivative according to the invention, V is unsubstituted and mono- or polysubstituted, independently selected from the following substituents:

[0075] -F, -Cl, -Br, -I, -CN, -C(=O)OH, -NH2, -NO2, -OH, =O, -SF5;

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

[0077] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 alkyl;

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

[0079] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C) 1-6 Alkyl)2;

[0080] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 alkyl;

[0081] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)2-C 1-6 alkyl;

[0082] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl group is optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0083] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, and the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0084] Preferably, V is unsubstituted and is mono- or poly-substituted, independently selected from the following substituents:

[0085] -OH, -F, -Cl, -Br, -I, -SH, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -CN, -NO2, -C(=O)OH, -NH2 or -N(CH3)2;

[0086] -C 1-6 Alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, with the substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[0087] -C 1-6 Heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, with the substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[0088] -OC 1-6 Alkyl groups, which are unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[0089] -O(C=O)C 1-6 Alkyl groups, which are unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[0090] -C(=O)OC 1-6 Alkyl groups, which are unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[0091] 3 to 14-membered cycloalkyl groups selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl; in each case unsubstituted, monosubstituted, or polysubstituted, with substituents independently selected from the group consisting of -F, -Cl, -Br, -I, and -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[0092] 3 to 14-membered heterocyclic alkyl groups selected from the group consisting of: aziridine, 1,4-oxazacycloheptanidine, aziridine, aziridine, aziridine, aziridine, aziridine, aziridine, aziridine, diazacycloheptanidine, dioxacyclohexane, dioxacyclohexane, dithiazoline, dithiopentane, imidazoline, isothiazolidine, isoxazolidine, morpholine, oxazolidine, hexane oxide, oxazacycloheptanidine, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, thioheptanidine, thioheptanidine, thioheptanidine, thioheptanidine, thioheptanidine, thiomorpholine, indoline, benzodihydrofuran, dihydrobenzene Thiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, and octahydropyrrolo[1,2-a]pyrrazine, wherein the groups are in each case unsubstituted, monosubstituted, or polysubstituted by substituents selected independently from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2.

[0093] Preferably, V is unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from -F, -Cl, -CN, -OH, =O, and -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 group, -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, -azacyclobutane, -C 1-6 alkylene-O-tetrahydropyran or -C 1-6 Alkyl-substituted piperazine.

[0094] In a preferred embodiment of the benzofuran derivative according to the present invention, V is

[0095] (i) Unreplaced;

[0096] (ii) Monosubstituted;

[0097] (iii) Disubstituted;

[0098] (iv) Trisubstituted; or

[0099] (v) Tetrasubstituted.

[0100] In a preferred embodiment of the benzofuran derivative according to the present invention, V is

[0101] (i) Unreplaced;

[0102] (ii) Monosubstituted; or

[0103] (iii) Disubstituted.

[0104] In a preferred embodiment, V represents a saturated or unsaturated 3- to 14-membered heterocyclic alkyl group (preferably a 5-membered heterocyclic alkyl group); or a 5- to 14-membered heteroaryl group (preferably a 5-membered heteroaryl group); in each case it is unsubstituted, monosubstituted, or polysubstituted; preferably residues selected from the group consisting of:

[0105]

[0106]

[0107] In a preferred embodiment, V represents an unsubstituted, monosubstituted, or polysubstituted oxetane; preferably

[0108] In a preferred embodiment, V represents a residue according to general formula (E).

[0109]

[0110] in

[0111] 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 =; the 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 general formula (E).

[0112] Where YE1 represents -N=, -NRE2-, S or -CRE3=; YE2 represents -N=, -NRE3-, S or -CRE4=; and YE3 represents -N=, -NRE4-, S or -CRE5=; the condition is that at least one of YE1, YE2 and YE3 is not -CRE3=, -CRE4= and -CRE5= respectively.

[0113] R E1 R E2 R E3 and R E4 Each can independently represent -H, -CH3, -CH2-cyclopropyl, -CH2CF3, -CH2CHF2, or -CF3; more specifically, R E1 R E2 R E3 and R E4 Each can be independently represented as -H, -CH3, or -CF3; preferably, the condition is R. E1 R E2 R E3 and R E4 There is only one residue that is not -H.

[0114] In a preferred embodiment, V represents an unsubstituted, monosubstituted, or polysubstituted 2-pyridine. In a preferred embodiment, V represents a residue selected from the group consisting of:

[0115]

[0116] In a preferred embodiment, V represents an unsubstituted, monosubstituted, or polysubstituted 3-pyridine. In a preferred embodiment, V represents a residue selected from the group consisting of:

[0117]

[0118] In a preferred embodiment, V represents an unsubstituted, monosubstituted, or polysubstituted 4-pyridine. In a preferred embodiment, V represents a residue selected from the group consisting of:

[0119]

[0120] In a preferred embodiment, V represents residues selected from the group consisting of:

[0121]

[0122] In a preferred embodiment, V represents an unsubstituted, monosubstituted, or multisubstituted bicyclic heteroaryl group, preferably selected from the group consisting of:

[0123]

[0124] In a preferred embodiment, V represents a residue according to the general formula (F').

[0125]

[0126] in

[0127] Y F1 This indicates -N= or -CR F4 =; and Y F2 This indicates -N= or -CR F5 =; and Y F3 This indicates -N= or -CR F3 =; the condition is Y F1 and Y F2 At least one of them is not -CR F4 = and -CR F5 =;

[0128] R F1 R F2 R F3 R F4 and R F5Each of the following can independently represent -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, or -azacyclobutane; preferably, the condition is R. F1 R F2 R F3 R F4 and R F5 There is only one residue that is not -H.

[0129] In another preferred embodiment, V represents a residue according to general formula (F).

[0130]

[0131] in

[0132] Y F1 This indicates -N= or -CR F4 =; and Y F2 This indicates -N= or -CR F5 =; the condition is Y F1 and Y F2 At least one of them is not -CR F4 = and -CR F5 =;

[0133] R F1 R F2 R F3 R F4 and R F5 Each of the following can independently represent -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, or -azacyclobutane; preferably, the condition is R. F1 R F2 R F3 R F4 and R F5 There is only one residue that is not -H.

[0134] In a preferred embodiment, V represents a residue according to general formula (G) or (H).

[0135]

[0136] Where R G1 and R H1 Choose from the group consisting of: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, aziridine, -cyclopropyl, -O-cyclopropyl, and -CHF2; or R. G1 and R H1 Choose from the following groups: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, and aziridine.

[0137] In other preferred embodiments, V represents a residue according to the general formula (G') or (H').

[0138]

[0139] Where R G1 and R H1 Choose from the group consisting of: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, aziridine, -cyclopropyl, -O-cyclopropyl, and -CHF2; or R. G1 and R H1 Choose from the following groups: -H, -CH3, -CF3, -OH, -OCH3, -OCH2CH3, -Cl, and aziridine;

[0140] In a preferred embodiment of the benzofuran derivative according to the present invention, R 1 express

[0141] -H, -F, -Cl, -Br, -I, -CN;

[0142] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 Alkyl; saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 alkyl;

[0143] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)C 1-6 alkyl;

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

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

[0146] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)N(C 1-6 Alkyl)2;

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

[0148] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)2-C 1-6 alkyl;

[0149] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups; or

[0150] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0151] Preferably, R 1 Representing -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 groups: -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 group, -C(=O)OC 1-6 Alkyl group, -C(=O)NH2, -C(=O)NHC 1-6 Alkyl, -C(=O)N(C) 1-6 Alkyl)2、-S(=O)-C 1-6 Alkyl group, -S(=O)2-C 1-6 Alkyl, -OC 1-6 Alkyl, unsubstituted cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl, or unsubstituted cyclohexyl.

[0152] Preferably, R 1 Indicates -H, -C 1-6 Alkyl, -C 1-6 Alkylene-OC 1-6 Alkyl, -CH2F, -CHF2, -CF3, unsubstituted -cyclopentyl or -cyclopropyl. Preferably, R 1 Indicates -H, -C 1-6 Alkyl, -C 1-6Alkylene-OC 1-6 Alkyl, -CH2F, -CHF2, -CF3, or unsubstituted cyclopentyl. Preferably, R 1 It represents -CH3.

[0153] Preferably, R 1 It represents -CH2F, -CHF2, -CH3, or -cyclopropyl. Preferably, R 1 This indicates -CH2F, -CHF2, or -CH3. Preferably, R... 1 It represents -C(=O)NH2 or -CHF2.

[0154] Preferably, R 1 Indicates -H, -C 1-3 Alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-3 Alkylene-CF3, -C 1-3 Alkylene -CF2H, -C 1-3 alkylene-CFH2 or cyclopropyl; preferably, R 1 Indicates -H, -C 1-3 Alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C 1-3 Alkylene-CF3, -C 1-3 Alkylene -CF2H or -C 1-3 Alkylene-CFH2; more preferably -CH3.

[0155] In a preferred embodiment of the benzofuran derivative according to the present invention, R 2 express

[0156] -H;

[0157] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[0158] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[0159] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl group is optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[0160] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, and the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0161] Preferably, 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 groups: -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.

[0162] Preferably, R 2 Indicates -H or -C 1-6 alkyl.

[0163] In a preferred embodiment of the benzofuran derivative according to the present invention, R 3 express

[0164] -H;

[0165] -OH;

[0166] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups; or

[0167] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups.

[0168] Preferably, R 3 Represents -H, -OH, -C 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH(C) 1-6Alkyl), -C 1-6 Alkylene-N(C) 1-6 Alkyl groups: -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.

[0169] Preferably, R 3 It represents -H, -OH, or a saturated, unsubstituted, or monosubstituted -C. 1-6 Alkyl group. Preferably, R 3 It represents -H.

[0170] Preferably, R 3 Indicates -H and R 4 This indicates residues other than -H.

[0171] In a preferred embodiment of the benzofuran derivative according to the present invention, R 4 express

[0172] -H;

[0173] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)C 1-6 alkyl;

[0174] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)2-C 1-6 alkyl;

[0175] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[0176] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[0177] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0178] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[0179] Unsubstituted, monosubstituted, or polysubstituted 6- to 14-membered aryl groups; wherein the 6- to 14-membered aryl groups are optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[0180] Unsubstituted, monosubstituted, or polysubstituted 5- to 14-membered heteroaryl groups; wherein the 5- to 14-membered heteroaryl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0181] Preferably, R 4 express

[0182] -S(=O)2C 1-6 Alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, with the substituents independently chosen from the group consisting of: -F, -Cl, -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[0183] -S(=O)2 (3 to 14-membered cycloalkyl), wherein the 3 to 14-membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, wherein the group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, and the substituents are independently selected from the group consisting of -F, -Cl, and -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[0184] -C 1-6 Alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, with the substituents independently chosen from the group consisting of: -F, -Cl, -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[0185] 3 to 14-membered cycloalkyl or -C 1-6 Alkylene (3 to 14-membered cycloalkyl), wherein -C 1-6The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 3- to 14-membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, wherein the group is saturated or unsaturated in each case, and wherein the group is unsubstituted, monosubstituted, or polysubstituted by substituents, which are independently selected from the group consisting of -F, -Cl, and -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[0186] 3 to 14-membered heterocyclic alkyl groups or -C 1-6 Alkylene (3 to 14-membered heterocyclic alkyl), wherein -C 1-6The alkylene group is either unsubstituted or monosubstituted with -OH, wherein the 3 to 14-membered heterocyclic alkyl group is selected from the group consisting of: aziridine, 1,4-oxazacycloheptane, aziridine, aziridine, aziridine, aziridine propane, aziridine octane, diazacycloheptane, dioxacyclohexane, dioxapentane, dithiazide, dithiopentane, imidazoline, isothiazidine, isoxazidine, morpholine, oxazidine, hexane oxide, oxacyclobutane, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, thiohexacyclobutane, thiohexacyclopropane, thiohexacyclopentane. Thiomorpholine, indoline, benzodihydrofuran, dihydrobenzothiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine; in each case unsubstituted, monosubstituted, or polysubstituted by substituents selected independently from the group consisting of: -F, -Cl, -C 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[0187] Unsubstituted, mono- or poly-substituted -phenyl groups, wherein the substituents are independently selected from the group consisting of: -F, -Cl, -CN, -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[0188] 5 to 14 heteroaryl or -C 1-6 alkylene-(5 to 14-membered heteroaryl), wherein -C 1-6The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 5 to 14-membered heteroaryl group is selected from the group consisting of: benzimidazole, benzisoxazole, benzoxazole, benzo-m-dioxane, benzofuran, benzothiadiazole, benzothiazol, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazon, imidazole, imidazopyridine, indazole, indole, inazine, isobenzofuran, isoindole, isoquinoline, isothiazol, iso... Oxazole, naphthidine, oxadiazole, oxazole, hydroxyindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazolium, thiadiazole, thiazolium, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine; in each case unsubstituted, monosubstituted, or polysubstituted, the substituents being independently selected from the group consisting of: -F, -Cl, -CN, -C 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which is saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl.

[0189] Preferably, R 4 express

[0190] -H;

[0191] Saturated, unsubstituted, mono- or poly-substituted -S(=O)2C 1-6 alkyl;

[0192] Saturated, unsubstituted -S(=O)2 (3 to 14-membered cycloalkyl);

[0193] -C 1-6 Alkyl groups are saturated, unsubstituted, monosubstituted, or disubstituted, with the substituents independently chosen from the group consisting of: -OH, =O, -NH2, -NHC. 1-6 Alkyl, -N(C) 1-6 Alkyl)2, -OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl group, -C(=O)NH2, -C(=O)-NH-C 1-3 Alkyl, -C(=O)-N(C) 1-3 2. Alkyl group; unsubstituted -phenyl group;

[0194] 3 to 14-membered cycloalkyl or -C 1-6 Alkylene (3 to 14-membered cycloalkyl), wherein -C 1-6 The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 3 to 14-membered cycloalkyl group is saturated, unsubstituted, monosubstituted, or disubstituted, and these substituents are independently selected from the group consisting of: -C 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C 1-6 alkylene -OH, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -OH, -OC 1-6 Alkyl, -NH2, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 alkyl;

[0195] 3 to 14-membered heterocyclic alkyl groups or -C 1-6 Alkylene (3 to 14-membered heterocyclic alkyl), wherein -C 1-6The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 3 to 14-membered heterocyclic alkyl group is selected in each case from aziridine, 1,4-oxazacycloheptanane, pyrrolidine, piperidine, aziridine, diazacycloheptanane, tetrahydrofuran, tetrahydropyran, oxazacyclobutane, morpholine, piperazine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabicyclo[3]pyrrole, and 1,4-oxazacycloheptanane. .2.1] Octane, 9-azabicyclo[3.3.1]nonane, quinine ring, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiacyclohexane, wherein the groups are in each case unsubstituted, monosubstituted, or polysubstituted by substituents, which are independently selected from the group consisting of: -F, -OH, =O, -C 1-6 Alkyl, -C 1-6 Alkylene-CF3, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -N(C) 1-6 Alkyl)2, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2、-C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl group), -S(=O)2C 1-6 Alkyl, oxetane butyl, pyrimidinyl, -C 1-6 alkylene-phenyl;

[0196] Unsubstituted -phenyl;

[0197] 5 to 14 heteroaryl or -C 1-6 alkylene-(5 to 14-membered heteroaryl), wherein -C 1-6 The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 5 to 14-membered heteroaryl group is selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine in each case, and the group is unsubstituted and monosubstituted or disubstituted by substituents selected independently from the group consisting of -C 1-6 Alkyl group, -OH group.

[0198] In a preferred embodiment of the benzofuran derivative according to the present invention, R 3 and R4 Together they form a 5- or 6-membered heterocycle containing one or two heteroatoms selected from N, O, and S, which may be saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[0199] Preferably, R 3 and R 4 Together they form a heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine, and piperazine, wherein the heterocycle is in each case unsubstituted, monosubstituted, or polysubstituted by substituents selected independently from the group consisting of -F, -C. 1-6 Alkyl groups, -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 group, -NHC(=O)OC 1-6 Alkyl, unsubstituted pyridyl, and unsubstituted or -C 1-6 Alkyl monosubstituted 1,2,4-oxadiazole. In a preferred embodiment, R 3 and R 4 Together they do not form unsubstituted, monosubstituted, or polysubstituted morpholines.

[0200] Preferably, R 3 and R 4 Together

[0201] The pyrrolidine ring is either unsubstituted or monosubstituted with -N(CH3)2;

[0202] Piperidine ring, which is either unsubstituted or monosubstituted with a substituent selected from the group consisting of: -C 1-6 Alkyl groups, -NH2, -N(CH3)2, -C(=O)NH-C 1-6 Alkyl group, -C(=O)OC 1-6 Alkyl group, -NHC(=O)OC 1-6 Alkyl and unsubstituted or -C 1-6 Alkyl monosubstituted 1,2,4-oxadiazole;

[0203] The morpholine ring is unsubstituted; or

[0204] Piperazine ring, which is either unsubstituted or N-substituted with a substituent selected from the group consisting of: -C 1-6 Alkyl and unsubstituted pyridyl groups.

[0205] In a preferred embodiment, R 3 and R 4 Neither represents -H. In the preferred embodiment, R 3 and R 4Together with the nitrogen atoms to which they are attached, they form residues selected from the following group:

[0206]

[0207] In other preferred embodiments, R 3 Indicates -H and R 4 It does not represent -H.

[0208] In a preferred embodiment, R 3 Indicates -H and R 4 Represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl group. In a preferred embodiment, R 3 Indicates -H and R 4 Residues selected from the following groups:

[0209]

[0210] In a preferred embodiment, R 3 Indicates -H and R 4 This indicates the residue -CR'R”-(CH2). m -OH, where m is an integer from 1 to 6, preferably from 1 to 3; and where R' and R” independently represent -H and -C. 1-3 Alkyl, -CF3, -CF2H, -CFH2, -C 1-3 Alkylene-CF3, -C 1-3 Alkylene -CF2H, -C 1-3 Alkylene -CFH2, -C 1-3 Alkylene-OC 1-3 Alkyl, -C 1-3 Alkylene -OH, -C(=O)-NH2 or C(=O)-NH-C 1-3 Alkyl group; preferably -H, -CH3, -C 1-3 Alkylene -OH, -C(=O)-NH2 or C(=O)-NH-C 1-3 Alkyl group. In a preferred embodiment, at least R' or R” does not represent -H. In a preferred embodiment, neither R' nor R” represents -H.

[0211] In other preferred embodiments, R 3 Indicates -H and R 4 It refers to 3- to 14-membered cycloalkyl groups that are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or 3- to 14-membered heterocycloalkyl groups that are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0212] In a preferred embodiment, R 3 Indicates -H and R 4This refers to 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. In a preferred embodiment, R 3 Indicates -H and R 4 Residues selected from the following groups:

[0213]

[0214] In a preferred embodiment, R 3 Indicates -H and R 4 This refers to saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups (preferably 4-membered cycloalkyl groups); or saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocycloalkyl groups (preferably 4-membered heterocycloalkyl groups). In a preferred embodiment, R 3 Indicates -H and R 4 Residues selected from the following groups:

[0215]

[0216] In a preferred embodiment, R 3 Indicates -H and R 4 This represents the residues according to general formula (A).

[0217]

[0218] in

[0219] m A It is 0 or 1;

[0220] Y A Selected from -O-, -NR A6 -and-CR A7 R A8 -;as well as

[0221] R A1 R A2 R A3 R A4 R A5 R A6 R A7 and R A8 -H, F, and -C are represented independently of each other. 1-3 Alkyl, -C 1-3 alkylene -OH, -C 1-3 Alkylene -NH2, -C 1-3 Alkylene-NH(C) 1-3 Alkyl), -C 1-3 Alkylene-N(C) 1-3 Alkyl)2, -C1-3 Alkylene-NH(C) 1-3 Alkylene-CF3), -C 1-3 Alkylene -C(=O)NH2, -C 1-3 Alkylene-NH-C(=O)OC 1-4 Alkyl group, -C(=O)NH2, -C(=O)-NH-C 1-3 Alkyl, -C(=O)-N(C) 1-3 Alkyl)2, -3-oxetane butyl or -CHF2; preferably, R A1 R A2 R A3 R A4 R A5 R A6 R A7 and R A8 -H, F, and -C are represented independently of each other. 1-3 Alkyl, -C 1-3 alkylene -OH, -C 1-3 Alkylene -NH2, -C 1-3 Alkylene-NH(C) 1-3 Alkyl), -C 1-3 Alkylene-N(C) 1-3 Alkyl)2, -C 1-3 Alkylene-NH(C) 1-3 Alkylene-CF3), -C 1-3 Alkylene -C(=O)NH2, -C 1-3 Alkylene-NH-C(=O)OC 1-4 Alkyl group, -C(=O)NH2, -C(=O)-NH-C 1-3 Alkyl, -C(=O)-N(C) 1-3 alkyl)2 or 3-oxetane butyl; or R A7 and R A8 Together with the carbon atoms to which they are attached, they form a ring and are represented as -CH2OCH2-, -CH2OCH2CH2-, or -CH2CH2OCH2CH2-, -CH2NHCH2-, -CH2NHCH2CH2-, or -CH2CH2NHCH2CH2-.

[0222] In a preferred embodiment, R 3 Indicates -H and R 4 Represents the residues defined above according to general formula (A), where

[0223] m A It is 0 or 1;

[0224] Y A Selected from -O- and -CR A7 RA8 -;as well as

[0225] R A1 R A2 R A3 R A4 R A5 R A7 and R A8 -H and -C are represented independently of each other. 1-3 alkylene -OH, -C 1-3 Alkylene-N(C) 1-3 Alkyl group 2, -C(=O)NH2 or -CHF2; preferably, R A1 R A2 R A3 R A4 R A5 R A7 and R A8 -H and -C are represented independently of each other. 1-3 alkylene -OH, -C 1-3 Alkylene-N(C) 1-3 alkyl)2 or -C(=O)NH2; preferably, the condition is R A1 R A2 R A3 R A4 R A5 R A7 and R A8 There is only one residue that is not -H.

[0226] In a preferred embodiment, R 3 Indicates -H and R 4 Represents the residues defined above according to general formula (A), where

[0227] m A It is 0 or 1;

[0228] Y A Selected from -O- and -CR A7 R A8 -;as well as

[0229] R A1 Indicates -C 1-3 alkylene -OH, -C 1-3 Alkylene-N(C) 1-3 Alkyl group 2, -C(=O)NH2 or -CHF2; preferably, R A1 Indicates -C 1-3 alkylene -OH, -C 1-3 Alkylene-N(C) 1-3 Alkyl)2 or -C(=O)NH2; and

[0230] R A2 R A3 R A4 R A5 R A7 and R A8 It represents -H.

[0231] In a preferred embodiment, R 3 Indicates -H and R 4 This refers to a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl group (preferably a 5-membered cycloalkyl group); or a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocycloalkyl group (preferably a 5-membered heterocycloalkyl group); or an unsubstituted, monosubstituted or polysubstituted 5- to 14-membered heteroaryl group (preferably a 5-membered heteroaryl group). In a preferred embodiment, R 3 Indicates -H and R 4 Residues selected from the following groups:

[0232]

[0233]

[0234] In a preferred embodiment, R 3 Indicates -H and R 4 This indicates the residues according to general formula (B).

[0235]

[0236] in

[0237] Y B Selected from -O-, -NR B8 -and-CR B9 R B10 -;as well as

[0238] R B1 R B2 R B3 R B4 R B5 R B6 R B7 R B8 R B9 and R B10 They can be represented independently of each other: -H, -F, -OH, -C. 1-3 Alkyl, -C 1-3 alkylene -OH, -C 1-3 Alkylene-OC 1-3 Alkyl, -C 1-3 Alkylene-CF3, -C 1-3 Alkylene -CO2H, -C 1-3Alkylene-C(=O)OC 1-3 Alkyl group, -C(=O)NH2, -C(=O)NH-C 1-3 Alkyl or -C(=O)N(C 1-3 Alkyl)2; or R B2 and R B3 Together means =O; or R B4 and R B5 Together they represent = O.

[0239] In a preferred embodiment, R 3 Indicates -H and R 4 Represents the residues defined above according to general formula (B), where

[0240] Y B Selected from -O- and -NR B8 -;as well as

[0241] R B1 R B2 R B3 R B4 R B5 R B6 R B7 R B8 -H, -F, and -C can be represented independently of each other. 1-3 Alkyl, -C 1-3 alkylene -OH, -C 1-3 Alkylene -CF3 or -C(=O)NH2; or R B2 and R B3 Together means =O; or R B4 and R B5 Together means = 0; preferably, the condition is R. A1 R A2 R A3 R A4 R A5 R A7 and R A8 Only 1, 2, or 3 residues in the sample represent residues that are not -H; preferably, the condition is R A1 R A2 R A3 R A4 R A5 R A7 and R A8 At least one of them represents a residue that is not -H.

[0242] In a preferred embodiment, R 3 Indicates -H and R 4This refers to saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl (preferably 6-membered cycloalkyl); or saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocycloalkyl (preferably 6-membered heterocycloalkyl); or unsubstituted, monosubstituted or polysubstituted 6- to 14-membered aryl (preferably 6-membered aryl); or unsubstituted, monosubstituted or polysubstituted 5- to 14-membered heteroaryl (preferably 6-membered heteroaryl). In a preferred embodiment, R 3 Indicates -H and R 4 Residues selected from the following groups:

[0243]

[0244] In a preferred embodiment, R 3 Indicates -H and R 4 This indicates the residues according to the general formula (C).

[0245]

[0246]

[0247] in

[0248] 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 -;

[0249] 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 Representing each other independently

[0250] -H, -F, -OH, -C(=O)OC 1-3 Alkyl, -NH2, -NH(C) 1-3 alkyl), -N(C) 1-3Alkyl)2, -C 1-3 Alkyl, -C 1-3 alkylene -OH, -C 1-3 Alkylene -, -C(=O)NH2, -C(=O)NH-C 1-3 Alkyl or -C(=O)N(C 1-3 Alkyl)2: or R C2 and R C3 Together means =O; or R C4 and R C5 Together means =O; or R C9 and R C10 Together means =O; or R C11 and R C12 Together they represent = O.

[0251] In a preferred embodiment, R 3 Indicates -H and R 4 Represents residues as defined above according to general formula (C), where

[0252] Y C1 Selected from -O- or -NR C8 -and Y C2 Indicates -CR C11 R C12 -; or Y C1 Indicates -CR C9 R C10 -and Y C2 Selected from -O- and -NR C8 -;

[0253] 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 -H, -F, and -C can be represented independently of each other. 1-3 Alkyl, -C 1-3 Alkylene -OH or -C(=O)NH2; preferably, the condition is R C1 R C2 R C3 R C4 R C5 R C6 R C7 R C8 R C9 R C10 R C11and R C12 Only 1, 2, or 3 residues in the sample represent residues that are not -H; 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 At least one of them represents a residue that is not -H.

[0254] In a preferred embodiment, R 3 Indicates -H and R 4 This refers to 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. In a preferred embodiment, R 3 Indicates -H and R 4 Residues:

[0255]

[0256] In a preferred embodiment, R 3 Indicates -H and R 4 This refers to saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups (preferably 4, 5, or 6-membered cycloalkyl groups); wherein the 3- to 14-membered cycloalkyl group is linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkylene group; or saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups (preferably 4, 5, or 6-membered heterocyclic alkyl groups); wherein the 3- to 14-membered heterocyclic alkyl group is linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkylene group. The 36 to 14 aryl groups are linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkylene group; or unsubstituted, monosubstituted or polysubstituted 5 to 14 heteroaryl groups (preferably 5 or 6 heteroaryl groups); wherein the 5 to 14 heteroaryl groups are linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkylene group. In a preferred embodiment, R 3 Indicates -H and R 4 Residues selected from the following groups:

[0257]

[0258]

[0259] In a preferred embodiment, R 3 Indicates -H and R 4 The term represents a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 5-membered heterocyclic alkyl group; wherein the 5-membered heterocyclic alkyl group is linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkylene group; or an unsubstituted, monosubstituted or polysubstituted 5-membered heteroaryl group; wherein the 5-membered heteroaryl group is linked by a saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkylene group.

[0260] In a preferred embodiment, R 3 Indicates -H and R 4 Residues selected from the following groups:

[0261]

[0262] In a preferred embodiment, R 3 Indicates -H and R 4 express

[0263] (i) residue -CR'R”-(CH2) m -OH, where m is an integer from 1 to 6, preferably from 1 to 3; and where R' and R” independently represent -H and -C. 1-3 Alkyl, -CF3, -CF2H, -CFH2, -C 1-3 Alkylene-CF3, -C 1-3 Alkylene -CF2H, -C 1-3 Alkylene -CFH2, -C 1-3 Alkylene-OC 1-3 Alkyl or -C 1-3 Alkylene -OH; preferably -H, -CH3 or -C 1-3 Alkylene -OH. In a preferred embodiment, at least R' or R” does not represent -H. In a preferred embodiment, neither R' nor R” represents -H; or

[0264] (ii) Based on the residues of general formula (D),

[0265]

[0266] in

[0267] m D and n D Each is independently 0, 1, 2, or 3; preferably, the condition is m D +n D ≤3;

[0268] Y D1Selected 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 D1 Selected from -O-, -S(=O)2-, -NR D8 -and-CR D9 R D10 -and Y D2 Indicates -CR D11 R D12 -; or Y D1 Indicates -CR D9 R D10 -and Y D2 Selected from -O-, -S(=O)2- and -NR D8 -;

[0269] R D1 R D2 R D3 R D4 R D5 R D6 R D7 R D8 R D9 R D10 R D11 and R D12 They can be represented independently of each other: -H, -F, -OH, -C. 1-3 Alkylene -OH, -C(=O)NH2, -C 1-3 Alkylenes -C(O)NH2, -C(=O)OC 1-3 Alkyl, -NH2, -C 1-3 Alkylene -NH2, -NH(C 1-3 alkyl), -N(C) 1-3 alkyl)2、-NH(C 1-3 Alkylene-CF3), -C 1-3 Alkylene -OCH3, -C 1-3 Alkyl, -C 1-3 Alkylene-CF3: or R D2 and R D3 Together means =O; or R D4 and R D5 Together means =O; or R D9 and R D10 Together means =O; or R D11 and R D12 Together means = 0;

[0270] Preferably, wherein

[0271] m D and n D Each is independently 0, 1, 2, or 3; preferably, the condition is m D +n D ≤3;

[0272] 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 -;

[0273] R D1 R D2 R D3 R D4 R D5 R D6 R D7 R D8 R D9 R D10 R D11 and R D12 They can be represented independently of each other: -H, -F, -OH, -C. 1-3 Alkylene groups: -OH, -C(=O)NH2, -CH2NH2, -CH2N(CH3)2, -NHCH2CF3, -CH3 or -CH2CF3; or R D2 and R D3 Together means =O; or R D4 and R D5 Together means =O; or R D9 and R D10 Together means =O; or R D11 and R D12 Together means = 0; 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 residues in the sample represent residues that are not -H; preferably, the condition is RD1 R D2 R D3 R D4 R D5 R D6 R D7 R D8 R D9 R D10 R D11 and R D12 At least one of them represents a residue that is not -H.

[0274] In a preferred embodiment of the benzofuran derivative according to the present invention, R 5 and R 5 'represented independently of each other'

[0275] -H;

[0276] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[0277] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[0278] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[0279] Preferably, R 5 and R 5 'Independently represent -H, -C1-C6 alkyl or -C1-C6 alkylene-N(C1-C6 alkyl)2.

[0280] In a preferred embodiment of the benzofuran derivative according to the present invention, R 5 and R 5 At least one of them is not -H.

[0281] In a preferred embodiment of the benzofuran derivative according to the present invention, R 5 and R 5 'All are -H.'

[0282] In a preferred embodiment, T represents -O- and U represents -CR. 5 R 5 '-and the obtained part-O-CR 5 R 5 '-' indicates residues selected from the following groups:

[0283]

[0284] In a preferred embodiment, T represents -CR 5 R 5 '-and U represents -O-and the obtained part -CR 5 R 5 '-O-' indicates a residue:

[0285]

[0286] In a preferred embodiment, R 5 Indicates -H and R 5 'Indicates residues selected from the following groups: -H, -C 1-3 Alkyl, -CF3, -CF2H, -CFH2, -C 1-3 Alkylene-CF3, -C 1-3 Alkylene -CF2H, -C 1-3 Alkylene-CFH2 and -C 1-3 alkylene -OH; preferably -H or C 1-3 alkyl.

[0287] In a preferred embodiment of the benzofuran derivative according to the present invention, R 6 R 7 and R 8 Representing each other independently

[0288] -H;

[0289] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;

[0290] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 alkyl;

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

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

[0293] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C) 1-6 Alkyl)2;

[0294] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 alkyl;

[0295] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC (=O)C1-6 alkyl;

[0296] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 Heteroalkyl groups.

[0297] Preferably, R 6 R 7 and R 8 Representing each other independently

[0298] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2,

[0299] -C 1-6 Alkyl, -CF3, -CHF2, -CH2F,

[0300] -OC 1-6 Alkyl, -OCF3, -OCHF2, -OCH2F,

[0301] -NHC 1-6 Alkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;

[0302] -N(C 1-6 Alkyl)2, which is unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;

[0303] -C(=O)OC 1-6 Alkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;

[0304] -OC(=O)C 1-6Alkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; or

[0305] -C 1-6 Heteroalkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2.

[0306] In a preferred embodiment, R 6 R 7 and R 8 Residues selected independently from the following groups: -H, -F, -Cl, -Br, -I, -CN, C 1-3 Alkyl, -CF3, -CF2H and -CFH2; preferably -H or -F.

[0307] In a preferred embodiment of the benzofuran derivative according to the present invention, R 6 It represents -H, -F, -Cl, -CN or -C1-C6 alkyl.

[0308] In a preferred embodiment of the benzofuran derivative according to the present invention, R 6 It does not represent -H.

[0309] In a preferred embodiment, R 6 The residues selected from the group consisting of -H, -F, -Cl, -CN or -CH3 are preferred.

[0310] In a preferred embodiment of the benzofuran derivative according to the present invention, R 7 It represents -H, -F, -Cl, -CN or -C1-C6 alkyl.

[0311] In a preferred embodiment of the benzofuran derivative according to the present invention, R 7 It does not represent -H.

[0312] In a preferred embodiment, particularly when Q represents -NR 3 R 4 At that time, R 7The residues selected from the group consisting of: -H, -F, -Cl, -CN or CH3; preferably -H, -F, -Cl or -CH3.

[0313] In a preferred embodiment, particularly when Q represents -OR 2 At that time, R 7 Residues selected from the following groups: -H or

[0314]

[0315] In a preferred embodiment of the benzofuran derivative according to the present invention, R 8 It represents -H, -F, -Cl, -CN or -C1-C6 alkyl.

[0316] In a preferred embodiment of the benzofuran derivative according to the present invention, R 8 It does not represent -H.

[0317] In a preferred embodiment, R 8 The residues selected from the group consisting of: -H, -F, -Cl, -CN or CH3; preferably -F.

[0318] In a preferred embodiment of the benzofuran derivative according to the present invention,

[0319] (i)R 6 R 7 and R 8 Each represents -H; or

[0320] (ii)R 6 R 7 and R 8 The two characters in the text represent -H and R. 6 R 7 and R 8 Another representation of -F, -Cl, -CN, or -CH3; or

[0321] (iii)R 6 R 7 and R 8 One of them represents -H and R 6 R 7 and R 8 Another independent expression in the expression is -F, -Cl, -CN, or -CH3.

[0322] In a particularly preferred embodiment, the compound is according to general formula (I), wherein

[0323] -R 1 Indicates -CH3; and / or

[0324] -R6 R 7 and R 8 Each represents -H; and / or

[0325] -T indicates -O-; and / or

[0326] -U indicates -CH2-; and / or

[0327] -V represents a thiazolyl, pyridinyl, or pyrazolyl group; wherein the thiazolyl, pyridinyl, and pyrazolyl groups can each be independently unsubstituted, monosubstituted, or disubstituted by substituents selected from the group consisting of: -CH3; -F; -CH2CHF2; and -CF3; and / or

[0328] -Q indicates NR 3 R 4 ; and / or

[0329] -R 3 Indicates H; and / or

[0330] -R 4 express

[0331] In a preferred embodiment of the present invention, the benzofuran derivative is selected from the group consisting of:

[0332] cpd 001 5-(furan-3-ylmethoxy)-2-methylbenzofuran-3-carboxylic acid

[0333] cpd 002 2-Methyl-5-(oxazol-5-ylmethoxy)benzofuran-3-carboxylic acid

[0334] cpd 003 2-Methyl-5-(pyrrolidine-3-ylmethoxy)benzofuran-3-carboxylic acid

[0335] cpd 004 2-Methyl-5-(pyridin-4-ylmethoxy)benzofuran-3-carboxylic acid

[0336] cpd 005 2-Methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxylic acid

[0337] cpd 006 2-Methyl-5-(pyridin-3-ylmethoxy)benzofuran-3-carboxylic acid

[0338] cpd 007 2-Methyl-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxylic acid

[0339] cpd 008 2-Methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxylic acid

[0340] cpd 009 2-Methyl-5-((1-methyl-1H-pyrazol-3-yl)methoxy)benzofuran-3-carboxylic acid

[0341] cpd 010 2-Methyl-5-((1-methyl-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxylic acid

[0342] cpd 011 2-Methyl-5-(thiophen-3-ylmethoxy)benzofuran-3-carboxylic acid

[0343] cpd 012 2-Methyl-5-(thiophen-2-ylmethoxy)benzofuran-3-carboxylic acid

[0344] cpd 013 2-Methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxylic acid

[0345] cpd 014 2-Methyl-5-(thiazolyl-5-ylmethoxy)benzofuran-3-carboxylic acid

[0346] cpd 015 2-Methyl-5-((tetrahydro-2H-pyran-4-yl)methoxy)benzofuran-3-carboxylic acid

[0347] cpd 016 5-((3,5-dimethylisoxazol-4-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0348] cpd 017 5-(benzo[d]thiazolyl-2-ylmethoxy)-2-methylbenzofuran-3-carboxylic acid

[0349] cpd 018 2-Methyl-5-((5-(trifluoromethyl)furan-2-yl)methoxy)benzofuran-3-carboxylic acid

[0350] cpd 019 5-((1-(tert-butoxycarbonyl)pyrrolidine-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0351] cpd 020(S)-2-methyl-5-(oxazol-5-ylmethoxy)-N-(pyrrolidone-3-yl)benzofuran-3-carboxamide

[0352] cpd 021(S)-2-methyl-5-(pyridin-4-ylmethoxy)-N-(pyrrolidine-3-yl)benzofuran-3-carboxamide

[0353] cpd 022(S)-2-methyl-5-(pyridin-3-ylmethoxy)-N-(pyrrolidine-3-yl)benzofuran-3-carboxamide

[0354] cpd 023(S)-2-methyl-5-((1-methyl-1H-pyrazol-3-yl)methoxy)-N-(pyrrolidine-3-yl)benzofuran-3-carboxamide

[0355] cpd 024 (S)-2-methyl-N-(pyrrolidone-3-yl)-5-(thiazolyl-5-ylmethoxy)benzofuran-3-carboxamide

[0356] cpd 025 (S)-2-methyl-N-(pyrrolidone-3-yl)-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0357] CPD 026 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0358] CPD 027 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-(pyridin-3-ylmethoxy)benzofuran-3-carboxamide

[0359] cpd 028 (S)-2-methyl-5-((5-methylpyridin-3-yl)methoxy)-N-(pyrrolidine-3-yl)benzofuran-3-carboxamide

[0360] cpd 029 (S)-2-methyl-5-((6-methylpyridin-2-yl)methoxy)-N-(pyrrolidine-3-yl)benzofuran-3-carboxamide

[0361] CPD 030 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxamide

[0362] cpd 031 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-(pyrazin-2-ylmethoxy)benzofuran-3-carboxamide

[0363] cpd 032 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-(pyrimidin-5-ylmethoxy)benzofuran-3-carboxamide

[0364] cpd 033 2-Methyl-5-((6-methylpyridin-3-yl)methoxy)-N-(tetrahydrofuran-3-yl)benzofuran-3-carboxamide

[0365] cpd 034 2-Methyl-5-((4-methylpyridin-3-yl)methoxy)-N-(tetrahydrofuran-3-yl)benzofuran-3-carboxamide

[0366] CPD 035 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-(thiophene-3-ylmethoxy)benzofuran-3-carboxamide

[0367] CPD 036 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0368] cpd 037 2-Methyl-5-((4-methylpyridin-3-yl)methoxy)-N-(2-oxopyrrolidine-3-yl)benzofuran-3-carboxamide

[0369] cpd 038 2-Methyl-5-((5-methylpyridin-3-yl)methoxy)-N-(2-oxopyrrolidone-3-yl)benzofuran-3-carboxamide

[0370] cpd 039 2-Methyl-N-(1-methylpiperidin-4-yl)-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0371] cpd 040 5-((4-methoxypyridin-3-yl)methoxy)-2-methyl-N-(tetrahydrofuran-3-yl)benzofuran-3-carboxamide

[0372] cpd 041 2-Methyl-N-(1-methylpiperidin-4-yl)-5-(thiophen-2-ylmethoxy)benzofuran-3-carboxamide

[0373] CPD 042 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(2-oxopyrrolidine-3-yl)benzofuran-3-carboxamide

[0374] CPD 043 2-Methyl-5-((4-methylthiazolyl-2-yl)methoxy)-N-(2-oxopyrrolidine-3-yl)benzofuran-3-carboxamide

[0375] cpd 044 5-((2,6-dimethylpyridin-3-yl)methoxy)-2-methyl-N-(2-oxopyrrolidone-3-yl)benzofuran-3-carboxamide

[0376] cpd 045 2-Methyl-N-(1-methylpiperidin-4-yl)-5-(1-(pyridin-4-yl)ethoxy)benzofuran-3-carboxamide

[0377] cpd 046 5-((2-methoxypyridin-3-yl)methoxy)-2-methyl-N-(2-oxopyrrolidone-3-yl)benzofuran-3-carboxamide

[0378] cpd 047 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0379] cpd 048 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0380] cpd 049 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0381] cpd 050 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0382] cpd 051 5-((2-methoxypyridin-3-yl)methoxy)-2-methyl-N-(1-methylpiperidin-4-yl)benzofuran-3-carboxamide

[0383] cpd 052 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0384] cpd 053 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((3-methylpyridin-2-yl)methoxy)benzofuran-3-carboxamide

[0385] cpd 054 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0386] cpd 055(S)-2-methyl-N-(pyrrolidone-3-yl)-5-((5-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0387] cpd 056 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0388] CPD 057 2-Methyl-N-(tetrahydrofuran-3-yl)-5-((4-(trifluoromethyl)thiazolyl)methoxy)benzofuran-3-carboxamide

[0389] cpd 058 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0390] CPD 059 5-(isoquinoline-1-ylmethoxy)-2-methyl-N-(1-methylpiperidin-4-yl)benzofuran-3-carboxamide

[0391] CPD 060 5-(isoquinoline-5-ylmethoxy)-2-methyl-N-(1-methylpiperidin-4-yl)benzofuran-3-carboxamide

[0392] CPD 061 5-(isoquinoline-6-ylmethoxy)-2-methyl-N-(1-methylpiperidin-4-yl)benzofuran-3-carboxamide

[0393] cpd 062 N-(3,3-difluoropiperidin-4-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0394] cpd 063 N-(3,3-difluoropiperidin-4-yl)-5-((6-methoxypyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0395] cpd 064 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0396] CPD 065 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-((6-(trifluoromethyl)pyridin-2-yl)methoxy)benzofuran-3-carboxamide

[0397] cpd 066 2-Methyl-N-(2-oxopyrrolidone-3-yl)-5-((6-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0398] cpd 067 5-((2-chloropyridin-3-yl)methoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methylbenzofuran-3-carboxamide

[0399] cpd 068 5-((4-chloropyridin-3-yl)methoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methylbenzofuran-3-carboxamide

[0400] cpd 069 2-Methyl-N-(1-methylpiperidin-4-yl)-5-((5-(trifluoromethyl)furan-2-yl)methoxy)benzofuran-3-carboxamide

[0401] cpd 070 N-(3,3-difluoropiperidin-4-yl)-5-(imidazo[1,2-a]pyridin-6-ylmethoxy)-2-methylbenzofuran-3-carboxamide

[0402] cpd 071 N-(3,3-difluoropiperidin-4-yl)-5-((6-(dimethylamino)pyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0403] cpd 072 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0404] cpd 073(S)-3-(2-methyl-5-((5-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0405] cpd 074 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0406] cpd 075 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((5-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0407] cpd 076 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((3-(trifluoromethyl)pyridin-2-yl)methoxy)benzofuran-3-carboxamide

[0408] cpd 077(S)-3-(2-methyl-5-((5-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0409] cpd 078 4-(5-((6-(dimethylamino)pyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamido)-3,3-difluoropiperidine-1-carboxylic acid tert-butyl ester

[0410] cpd 079 3-(((3-(ethoxycarbonyl)-2-methylbenzofuran-5-yl)oxy)methyl)pyrrolidine-1-carboxylic acid tert-butyl ester

[0411] cpd 080(R)-3-(2-methyl-5-(oxazol-5-ylmethoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0412] cpd 081(R)-3-(2-methyl-5-(pyridin-4-ylmethoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0413] cpd 082(R)-3-(2-methyl-5-(pyridin-3-ylmethoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0414] cpd 083(R)-3-(2-methyl-5-((1-methyl-1H-pyrazol-3-yl)methoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0415] cpd 084(R)-3-(2-methyl-5-(thiazolyl-5-ylmethoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0416] cpd 085(R)-3-(2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0417] cpd 086(R)-3-(2-methyl-5-((6-methylpyridin-2-yl)methoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid tert-butyl ester

[0418] CPD 087 3,3-Difluoro-4-(2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0419] CPD 088 3,3-Difluoro-4-(2-methyl-5-((3-methylpyridin-2-yl)methoxy)benzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0420] CPD 089 3,3-Difluoro-4-(5-(((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0421] CPD 090 3,3-Difluoro-4-(2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0422] CPD 091 3,3-Difluoro-4-(5-(((6-methoxypyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0423] cpd 092 4-(5-((2-chloropyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamido)-3,3-difluoropiperidine-1-carboxylic acid tert-butyl ester

[0424] CPD 093 4-(5-((4-chloropyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamido)-3,3-difluoropiperidine-1-carboxylic acid tert-butyl ester

[0425] CPD 094 3,3-Difluoro-4-(5-(imidazo[1,2-a]pyridin-6-ylmethoxy)-2-methylbenzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0426] CPD 095 3,3-Difluoro-4-(2-methyl-5-((5-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0427] CPD 096 3,3-Difluoro-4-(2-methyl-5-((3-(trifluoromethyl)pyridin-2-yl)methoxy)benzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0428] CPD 097 3,3-Difluoro-4-(2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0429] CPD 098 3,3-Difluoro-4-(2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamido)piperidine-1-carboxylic acid tert-butyl ester

[0430] cpd 099 2-Methyl-5-((4-methylpyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0431] cpd 100 5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0432] cpd 101 2-Methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0433] cpd 102 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxylic acid

[0434] cpd 103 N-(4,4-difluoropiperidin-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0435] cpd 104 N-(1-hydroxy-2-methylpropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0436] cpd 105 N-(4,4-difluoropyrrolidone-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0437] cpd 106 N-(4,4-difluoropyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0438] cpd 107 N-(1-(hydroxymethyl)cyclobutyl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0439] cpd 108 N-(1-((dimethylamino)methyl)cyclobutyl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0440] cpd 109 N-(1-hydroxy-2-methylpropyl-2-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0441] cpd 110 N-(3,3-difluoro-1-methylpiperidin-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0442] cpd 111 N-(4,4-difluoropiperidin-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0443] cpd 112 N-(3,3-difluoropiperidin-4-yl)-4-fluoro-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0444] cpd 113 N-(3,3-difluoropiperidin-4-yl)-6-fluoro-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0445] cpd 114 N-(1-(2-hydroxyethyl)cyclobutyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0446] cpd 115 N-(5,5-difluoropiperidin-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0447] cpd 116 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(1-(2,2,2-trifluoroethyl)pyrrolidine-3-yl)benzofuran-3-carboxamide

[0448] cpd 117 N-(1-(hydroxymethyl)cyclobutyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0449] cpd 118 N-(4,4-difluoro-1-methylpiperidin-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0450] cpd 119 N-(3-carbamoyloxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0451] cpd 120 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0452] cpd 121 N-(3-(2-hydroxyethyl)tetrahydrofuran-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0453] cpd 122 7-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0454] cpd 123 N-(4,4-difluoro-1-methylpyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0455] cpd 124 N-(4,4-difluoro-1-methylpyrrolidone-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0456] cpd 125 N-(5,5-difluoropiperidin-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0457] cpd 126 N-(3-(2-hydroxyethyl)tetrahydrofuran-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0458] cpd 127 N-(1-(2-hydroxyethyl)cyclobutyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0459] cpd 128 N-(3-(2-hydroxyethyl)oxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0460] cpd 129 N-(3-(2-hydroxyethyl)oxetane-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0461] cpd 130 N-(3,3-difluoro-1-methylpiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0462] cpd 131 N-(4,4-difluoro-1-methylpiperidin-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0463] cpd 132 N-(3-(hydroxymethyl)tetrahydrofuran-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0464] cpd 133 N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0465] cpd 134 N-(4,4-difluoro-1-(2-hydroxyethyl)pyrrolidine-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0466] cpd 135 N-(3-(hydroxymethyl)tetrahydrofuran-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0467] cpd 136 N-(1-(aminomethyl)cyclobutyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0468] cpd 137 N-(1-(aminomethyl)cyclobutyl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0469] cpd 138 2-Methyl-N-(1H-pyrazol-3-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0470] cpd 139 N-(1-(hydroxymethyl)cyclopropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0471] cpd 140 N-(1-((dimethylamino)methyl)cyclobutyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0472] cpd 141 N-(5,5-difluoro-1-methylpiperidin-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0473] cpd 142 N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0474] cpd 143 2-Methyl-N-(1-Methyl-1H-pyrazol-4-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0475] cpd 144 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(1H-pyrazol-3-yl)benzofuran-3-carboxamide

[0476] cpd 145 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(1-(((2,2,2-trifluoroethyl)amino)methyl)cyclobutyl)benzofuran-3-carboxamide

[0477] cpd 146 2-Methyl-N-(1-Methyl-1H-pyrazol-3-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0478] cpd 147 N-(4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0479] cpd 148 2-Methyl-N-(tetrahydrofuran-3-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0480] cpd 149 2-Methyl-N-(1-(2,2,2-trifluoroethyl)pyrrolidine-3-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0481] cpd 150 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(1H-pyrazol-4-yl)benzofuran-3-carboxamide

[0482] cpd 151 N-(4,4-difluoro-1-(2-hydroxyethyl)pyrrolidine-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0483] cpd 152 2-Methyl-N-(1-methyl-1H-pyrazol-4-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0484] cpd 153 2-Methyl-N-(1-(((2,2,2-trifluoroethyl)amino)methyl)cyclobutyl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0485] cpd 154 2-Methyl-N-(1-Methyl-1H-pyrazol-5-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0486] cpd 155 N-(4,4-difluoro-1-(2,2,2-trifluoroethyl)pyrrolidine-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0487] cpd 156 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(2-oxaspiro[3.3]hept-6-yl)benzofuran-3-carboxamide

[0488] cpd 157 N-(4,4-difluoro-1-(2,2,2-trifluoroethyl)pyrrolidine-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0489] cpd 158 2-Methyl-N-(1H-pyrazol-4-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0490] cpd 159 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(tetrahydrofuran-3-yl)benzofuran-3-carboxamide

[0491] cpd 160 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0492] cpd 161 2-Methyl-N-(1-methyl-1H-pyrazol-3-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0493] cpd 162 N-(4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0494] cpd 163 N-(5,5-difluoro-1-methylpiperidin-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0495] cpd 164 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0496] cpd 165 6-Chloro-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0497] cpd 166 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)benzofuran-3-carboxamide

[0498] cpd 167 2-Methyl-N-(2-oxaspiro[3.3]hept-6-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0499] cpd 168 2-Methyl-N-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0500] cpd 169 N-(1-(2-methoxyethyl)-2-oxopyrrolidine-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0501] cpd 170 2-Methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxylic acid (3-aminotetrahydrofuran-3-yl)methyl ester

[0502] cpd 171 2-Methyl-N-(1-Methyl-1H-pyrazol-5-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0503] CPD 172 2,2,2-trifluoroethyl 3,3-difluoro-4-(2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid

[0504] cpd 173 2-Methyl-N-(2-azaspiro[3.3]hept-6-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0505] cpd 174 6-Chloro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0506] cpd 175(R)-3,3-difluoro-4-(2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamido)pyrrolidine-1-carboxylic acid 2,2,2-trifluoroethyl ester

[0507] cpd 176 N-(3,3-difluoropiperidin-4-yl)-7-fluoro-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0508] cpd 177 4-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0509] cpd 178(3-amino-1H-pyrazole-1-yl)(2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-yl)methyl ketone

[0510] cpd 179 N-(3,3-difluoropiperidin-4-yl)-2,6-dimethyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0511] cpd 180 N-(1-(2-hydroxyethyl)-5-oxopyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0512] cpd 181(4-amino-1H-pyrazole-1-yl)(2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-yl)methyl ketone

[0513] cpd 182 6-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0514] cpd 183 N-(3,3-difluoropiperidin-4-yl)-2,7-dimethyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0515] cpd 184 7-Chloro-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0516] cpd 185 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2,6-dimethyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0517] cpd 186 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2,7-dimethyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0518] cpd 187 7-Chloro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0519] cpd 188 7-Cyano-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0520] cpd 189 N-((3-aminooxetane-3-yl)methyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0521] cpd 190 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(2-azaspiro[3.3]hept-6-yl)benzofuran-3-carboxamide

[0522] cpd 191 4-Cyano-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0523] cpd 192(3-amino-1H-pyrazole-1-yl)(2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-yl) methyl ketone

[0524] cpd 193 4-Cyano-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0525] cpd 194 6-Cyano-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0526] cpd 195 6-Cyano-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0527] cpd 196 7-cyano-N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0528] cpd 197 2-(difluoromethyl)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0529] CPD 198 2-(difluoromethyl)-N-(1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0530] cpd 199 2-(difluoromethyl)-N-(3,3-difluoropiperidin-4-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0531] cpd 200 N-(1-(hydroxymethyl)cyclopropyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0532] cpd 201 N-(3-(hydroxymethyl)azacyclobutane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0533] cpd 202 N-(3-(hydroxymethyl)azacyclobutane-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0534] cpd 203 N-(4,4-difluorotetrahydrofuran-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0535] cpd 204 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0536] cpd 205 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0537] cpd 206 5-((2-ethoxypyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0538] cpd 207 N-(3,3-difluoropiperidin-4-yl)-5-((2-ethoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0539] Cpd 208 2-Methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxylic acid

[0540] Cpd 209 2-Methyl-5-((2-(trifluoromethyl)thiazolyl-5-yl)methoxy)benzofuran-3-carboxylic acid

[0541] Cpd 210 2-Methyl-5-((2-methyl-4-(trifluoromethyl)thiazo-5-yl)methoxy)benzofuran-3-carboxylic acid

[0542] Cpd 211 2-Methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxylic acid

[0543] Cpd 212 2-Methyl-5-((2-methylthiazo-4-yl)methoxy)benzofuran-3-carboxylic acid

[0544] Cpd 213 2-Methyl-5-((3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxylic acid

[0545] Cpd 214 2-Methyl-5-((4-methylpyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0546] Cpd 215 2-Methyl-5-((5-methylisoxazol-3-yl)methoxy)benzofuran-3-carboxylic acid

[0547] Cpd 216 2-Methyl-5-((5-methylthiazo-4-yl)methoxy)benzofuran-3-carboxylic acid

[0548] Cpd 217 2-Methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0549] Cpd 218 2-Methyl-5-(oxetane-3-ylmethoxy)benzofuran-3-carboxylic acid

[0550] Cpd 219 2-Methyl-5-(pyrimidin-4-ylmethoxy)benzofuran-3-carboxylic acid

[0551] Cpd 220 5-((1-(2,2-difluoroethyl)-1H-pyrazole-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0552] Cpd 221 5-((2-(difluoromethoxy)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0553] Cpd 222 5-((2-(dimethylamino)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0554] Cpd 223 5-((2,4-dimethylthiazolyl-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0555] Cpd 224 5-((2,5-dimethylthiazolyl-4-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0556] Cpd 225 5-((2-aminopyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0557] Cpd 226 5-((3-(difluoromethyl)pyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0558] Cpd 227 5-((6-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0559] Cpd 228 5-((4-fluoro-1-methyl-1H-pyrazole-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0560] Cpd 229 2-(difluoromethyl)-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxylic acid

[0561] Cpd 230 2-(difluoromethyl)-5-((2-methoxypyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0562] Cpd 231 2-Cyclopropyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0563] Cpd 232 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0564] Cpd 233 4-Fluoro-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxylic acid

[0565] Cpd 234 4-Fluoro-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0566] Cpd 235 5-((1-(2,2-difluoroethyl)-1H-imidazol-2-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0567] Cpd 236 5-((2-(azacyclobutane-1-yl)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0568] Cpd 237 5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0569] Cpd 238 5-((2-cyanopyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0570] Cpd 239 5-((2-ethoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0571] Cpd 240 5-((3-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0572] Cpd 241 5-((5-(2-hydroxyethoxy)pyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0573] Cpd 242 5-((5-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0574] Cpd 243 6-Fluoro-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxylic acid

[0575] Cpd 244 6-Fluoro-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0576] Cpd 245 7-Fluoro-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxylic acid

[0577] Cpd 246 7-Fluoro-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0578] Cpd 247 2-Methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0579] Cpd 248 2-Methyl-5-(1-(2-(trifluoromethyl)thiazolyl-5-yl)ethoxy)benzofuran-3-carboxylic acid

[0580] Cpd 249 2-Methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxylic acid

[0581] Cpd 250 2-Methyl-5-((1-methyl-2-oxo-1,2-dihydropyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0582] Cpd 251 2,4-Dimethyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0583] Cpd 252 2-Methyl-5-(((2-(trifluoromethyl)pyridin-3-yl)oxy)methyl)benzofuran-3-carboxylic acid

[0584] Cpd 253 2-Methyl-5-((1-methyl-1H-1,2,3-triazol-4-yl)methoxy)benzofuran-3-carboxylic acid

[0585] Cpd 254 2-Methyl-5-((1-methyl-1H-1,2,3-triazol-5-yl)methoxy)benzofuran-3-carboxylic acid

[0586] Cpd 255 2-Methyl-5-((1-methyl-1H-1,2,4-triazol-3-yl)methoxy)benzofuran-3-carboxylic acid

[0587] Cpd 256 2-Methyl-5-((1-methyl-6-oxo-1,6-dihydropyridin-2-yl)methoxy)benzofuran-3-carboxylic acid Cpd 257 2-Methyl-5-((2-methylpyrimidin-4-yl)methoxy)benzofuran-3-carboxylic acid

[0588] Cpd 258 2-Methyl-5-((3-methyloxetane-3-yl)methoxy)benzofuran-3-carboxylic acid

[0589] Cpd 259 2-Methyl-5-((4-methyloxazol-2-yl)methoxy)benzofuran-3-carboxylic acid

[0590] Cpd 260 2-Methyl-5-((4-methylthiazo-2-yl)methoxy)benzofuran-3-carboxylic acid

[0591] Cpd 261 2-Methyl-5-((5-methylpyrazin-2-yl)methoxy)benzofuran-3-carboxylic acid

[0592] Cpd 262 2-Methyl-5-((5-methylthiazolyl-2-yl)methoxy)benzofuran-3-carboxylic acid

[0593] Cpd 263 2-Methyl-5-((6-methylpyridazin-3-yl)methoxy)benzofuran-3-carboxylic acid

[0594] Cpd 264 2-Methyl-5-(pyrimidin-2-ylmethoxy)benzofuran-3-carboxylic acid

[0595] Cpd 265 2-Cyclopropyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxylic acid

[0596] Cpd 266 5-((6-methoxypyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0597] Cpd 267 5-(imidazo[1,2-a]pyridin-6-ylmethoxy)-2-methylbenzofuran-3-carboxylic acid

[0598] Cpd 268 2-Methyl-5-(1-(4-methylthiazo-5-yl)ethoxy)benzofuran-3-carboxylic acid

[0599] Cpd 269 5-((2-methoxypyridin-4-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0600] Cpd 270(2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carbonyl)serine

[0601] Cpd 271(R)-N-(1-amino-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0602] Cpd 272(R)-N-(1-amino-3-(methanesulfonyl)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0603] Cpd 273(R)-N-(1-amino-3-methyl-1-oxobut-2-yl)-2-methyl-5-((4-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0604] Cpd 274(R)-N-(1-hydroxy-3-(methanesulfonyl)propyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0605] Cpd 275(R)-N-(1-hydroxy-3-(methanesulfonyl)propyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0606] Cpd 276(R)-N-(3-hydroxy-1-(methylamino)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0607] Cpd 277(S)-N-(1-(3,3-difluoropyrrolidone-1-yl)-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0608] Cpd 278(S)-N-(1-(dimethylamino)-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0609] Cpd 279(S)-N-(1-amino-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0610] Cpd 280(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0611] Cpd 281(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-(trifluoromethyl)thiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0612] Cpd 282(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methyl-4-(trifluoromethyl)thiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0613] Cpd 283(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[0614] Cpd 284(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0615] Cpd 285(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-4-yl)methoxy)benzofuran-3-carboxamide

[0616] Cpd 286(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide

[0617] Cpd 287(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0618] Cpd 288(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0619] Cpd 289(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylisoxazol-3-yl)methoxy)benzofuran-3-carboxamide

[0620] Cpd 290(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylthiazolyl-4-yl)methoxy)benzofuran-3-carboxamide

[0621] Cpd 291(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0622] Cpd 292(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(oxetane-3-ylmethoxy)benzofuran-3-carboxamide

[0623] Cpd 293(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxamide

[0624] Cpd 294(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyrimidin-4-ylmethoxy)benzofuran-3-carboxamide

[0625] Cpd 295(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0626] Cpd 296(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-(difluoromethoxy)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0627] Cpd 297(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-(dimethylamino)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0628] Cpd 298(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,4-dimethylthiazo-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0629] Cpd 299(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,5-dimethylthiazo-4-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0630] Cpd 300(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-aminopyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0631] Cpd 301(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((3-(difluoromethyl)pyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0632] Cpd 302(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0633] Cpd 303(S)-N-(1-amino-3-methoxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0634] Cpd 304(S)-N-(1-amino-3-methyl-1-oxobut-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0635] Cpd 305(S)-N-(3-hydroxy-1-(methylamino)-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0636] Cpd 306(S)-N-(3-hydroxy-1-(methylamino)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0637] Cpd 307(S)-N-(3-hydroxy-1-oxo-1-(pyrrolidin-1-yl)propyl-2-yl)-2-methyl-5-((2-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0638] Cpd 308 2-(difluoromethyl)-N-(1-(hydroxymethyl)cyclopropyl)-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0639] Cpd 309 2-(difluoromethyl)-N-(3-(hydroxymethyl)oxetane-3-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0640] Cpd 310 2-(difluoromethyl)-N-(3,3-difluoropiperidin-4-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0641] Cpd 311 2-(difluoromethyl)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-hydroxypyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0642] Cpd 312 2-(difluoromethyl)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-methoxypyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0643] Cpd 313 2-Cyclopropyl-N-(3,3-Difluoropiperidin-4-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0644] Cpd 314 2-Cyclopropyl-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0645] Cpd 315 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(1-(oxazol-2-yl)ethyl)benzofuran-3-carboxamide

[0646] Cpd 316 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(1,1,1-trifluoro-3-hydroxypropyl-2-yl)benzofuran-3-carboxamide

[0647] Cpd 317 2-Methyl-5-((4-methylthiazo-5-yl)methoxy)-N-(5-oxo-1,4-oxazacycloheptane-6-yl)benzofuran-3-carboxamide

[0648] Cpd 318 2-Methyl-N-(1-(methylcarbamoyl)cyclobutyl)-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0649] Cpd 319 2-Methyl-N-(1-(methylcarbamoyl)cyclobutyl)-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0650] Cpd 320 2-Methyl-N-(1-(methylcarbamoyl)cyclobutyl)-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0651] Cpd 321 2-Methyl-N-(2-(methylamino)-2-oxoethyl)-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0652] Cpd 322 2-Methyl-N-(2-(methylsulfonylamino)ethyl)-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0653] Cpd 323 2-Methyl-N-(2-(methanesulfonyl)ethyl)-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0654] Cpd 324 2-Methyl-N-(3-(methylcarbamoyl)oxetane-3-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0655] Cpd 325 3-(((3-((4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)carbamoyl)-2-methylbenzofuran-5-yl)oxy)methyl)pyridineamide

[0656] Cpd 326 4-Fluoro-N-(1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0657] Cpd 327 4-Fluoro-N-(1-(hydroxymethyl)cyclopropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0658] Cpd 328 4-Fluoro-N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0659] Cpd 329 4-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0660] Cpd 330 4-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0661] Cpd 331 5-((1-(2,2-difluoroethyl)-1H-imidazol-2-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0662] Cpd 332 5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methylbenzofuran-3-carboxamide

[0663] Cpd 333 5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-N-(3-(hydroxymethyl)-2-oxopyrrolidine-3-yl)-2-methylbenzofuran-3-carboxamide

[0664] Cpd 334 5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0665] Cpd 335 5-((2-(azacyclobutane-1-yl)pyridin-3-yl)methoxy)-N-(1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl)-2-methylbenzofuran-3-carboxamide

[0666] Cpd 336 5-((2-(azacyclobutan-1-yl)pyridin-3-yl)methoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methylbenzofuran-3-carboxamide

[0667] Cpd 337 5-((2-(azacyclobutane-1-yl)pyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0668] Cpd 338 5-((2-(difluoromethoxy)pyridin-3-yl)methoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methylbenzofuran-3-carboxamide

[0669] Cpd 339 5-((2-(difluoromethoxy)pyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0670] Cpd 340 5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-N-(1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl)-2-methylbenzofuran-3-carboxamide

[0671] Cpd 341 5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-N-(3-(hydroxymethyl)oxetane-3-yl)-2-methylbenzofuran-3-carboxamide

[0672] Cpd 342 5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methylbenzofuran-3-carboxamide

[0673] Cpd 343 5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0674] Cpd 344 5-((2-(dimethylamino)pyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0675] Cpd 345 5-((2,4-dimethylthiazolyl-5-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0676] Cpd 346 5-((2-aminopyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0677] Cpd 347 5-((2-cyanopyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0678] Cpd 348 5-((2-ethoxypyridin-3-yl)methoxy)-N-(1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl)-2-methylbenzofuran-3-carboxamide

[0679] Cpd 349 5-((2-hydroxypyridin-3-yl)methoxy)-N-(cis-4-hydroxytetrahydrofuran-3-yl)-2-methylbenzofuran-3-carboxamide

[0680] Cpd 350 5-((2-hydroxypyridin-3-yl)methoxy)-N-(trans-4-hydroxytetrahydrofuran-3-yl)-2-methylbenzofuran-3-carboxamide

[0681] Cpd 351 5-((3-(difluoromethyl)pyridin-2-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0682] Cpd 352 5-((3-fluoropyridin-2-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0683] Cpd 355 5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-N-(3-(hydroxymethyl)-2-oxopiridine-3-yl)-2-methylbenzofuran-3-carboxamide

[0684] Cpd 356 5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-N-(3-(hydroxymethyl)-2-oxopyrrolidine-3-yl)-2-methylbenzofuran-3-carboxamide

[0685] Cpd 357 5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0686] Cpd 358 5-((5-(2-hydroxyethoxy)pyridin-2-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0687] Cpd 359 5-((5-fluoropyridin-2-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[0688] Cpd 360 6-Fluoro-N-(1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0689] Cpd 361 6-Fluoro-N-(1-(hydroxymethyl)cyclopropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0690] Cpd 362 6-Fluoro-N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0691] Cpd 363 6-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0692] Cpd 364 6-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0693] Cpd 365 7-Fluoro-N-(1-(2-hydroxyethyl)-2-oxopyrrolidine-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0694] Cpd 366 7-Fluoro-N-(1-(hydroxymethyl)cyclopropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0695] Cpd 367 7-Fluoro-N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0696] Cpd 368 7-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0697] Cpd 369 7-Fluoro-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0698] Cpd 370 N-((1-cyanocyclopropyl)methyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0699] Cpd 371 N-((1-cyanocyclopropyl)methyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0700] Cpd 372 N-((1-fluorocyclopropyl)methyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0701] Cpd 373 N-((1-fluorocyclopropyl)methyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0702] Cpd 374 N-((1H-pyrazol-3-yl)methyl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0703] Cpd 375 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[0704] Cpd 376 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0705] Cpd 377 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0706] Cpd 378 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0707] Cpd 379 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0708] Cpd 380 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0709] Cpd 381 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0710] Cpd 382 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-5-((2,4-dimethylthiazo-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0711] Cpd 383 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0712] Cpd 384 N-((3-fluorooxocyclobutane-3-yl)methyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0713] Cpd 385 N-((3-fluorooxocyclobutane-3-yl)methyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0714] Cpd 386 N-(cis-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0715] Cpd 387 N-(cis-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0716] Cpd 388 N-(trans-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((2-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0717] Cpd 389 N-(trans-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0718] Cpd 390 N-((3S,4R)-4-hydroxy-2-oxopyrrolidone-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0719] Cpd 391 N-((3S,4R)-4-hydroxy-2-oxopyrrolidone-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0720] Cpd 392 N-((3S,4R)-4-hydroxy-2-oxopyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0721] Cpd 393 N-((4-fluorotetrahydro-2H-pyran-4-yl)methyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0722] Cpd 394 N-((4-fluorotetrahydro-2H-pyran-4-yl)methyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0723] Cpd 395 N-((S)-1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(1-(2-methylthiazolyl-5-yl)ethoxy)benzofuran-3-carboxamide

[0724] Cpd 396 N-(1-((2-hydroxyethyl)(methyl)amino)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0725] Cpd 397 N-(1-((2-hydroxyethyl)amino)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0726] Cpd 398 N-(1-((2-hydroxyethyl)amino)-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0727] Cpd 399 N-(1-((difluoromethoxy)methyl)cyclopropyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0728] Cpd 400 N-(1-((difluoromethoxy)methyl)cyclopropyl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0729] Cpd 401 N-(1-(1H-benzo[d]imidazol-2-yl)-2-hydroxyethyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0730] Cpd 402 N-(1-(2-(2-hydroxyethoxy)ethyl)-2-oxopyrrolidine-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0731] Cpd 403 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0732] Cpd 404 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((1-methyl-1H-pyrazole-5-yl)methoxy)benzofuran-3-carboxamide

[0733] Cpd 405 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((1-methyl-2-oxo-1,2-dihydropyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0734] Cpd 406 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0735] Cpd 407 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0736] Cpd 408 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0737] Cpd 409 N-(1-(2-hydroxyethyl)-2-oxopyrrolidone-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0738] Cpd 410 N-(1-(2-hydroxyethyl)-3-methyl-2-oxopyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0739] Cpd 411 N-(1-(dimethylamino)-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0740] Cpd 412 N-(1-(dimethylamino)-3-hydroxypropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0741] Cpd 413 N-(1-(dimethylamino)-3-hydroxypropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0742] Cpd 414 N-(1-(hydroxymethyl)cyclobutyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0743] Cpd 415 N-(1-(hydroxymethyl)cyclobutyl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0744] Cpd 416 N-(1-(hydroxymethyl)cyclobutyl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0745] Cpd 417 N-(1-(hydroxymethyl)cyclobutyl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0746] Cpd 418 N-(1-(hydroxymethyl)cyclopropyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0747] Cpd 419 N-(1-(hydroxymethyl)cyclopropyl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0748] Cpd 420 N-(1-(hydroxymethyl)cyclopropyl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0749] Cpd 421 N-(1-(hydroxymethyl)cyclopropyl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0750] Cpd 422 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0751] Cpd 423 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0752] Cpd 424 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0753] Cpd 425 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0754] Cpd 426 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0755] Cpd 427 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxamide

[0756] Cpd 428 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0757] Cpd 429 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-2-methyl-5-(pyrimidin-4-ylmethoxy)benzofuran-3-carboxamide

[0758] Cpd 430 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0759] Cpd 431 N-(1,3-dihydroxy-2-methylpropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0760] Cpd 432 N-(1-amino-1-oxo-3-(1H-1,2,4-triazol-1-yl)propyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0761] Cpd 433 N-(1-amino-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0762] Cpd 434 N-(1-amino-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0763] Cpd 435 N-(1-amino-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0764] Cpd 436 N-(1-amino-1-oxopropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0765] Cpd 437 N-(1-amino-1-oxopropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0766] Cpd 438 N-(1-amino-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0767] Cpd 439 N-(1-amino-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0768] Cpd 440 N-(1-amino-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0769] Cpd 441 N-(1-amino-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxamide

[0770] Cpd 442 N-(1-amino-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0771] Cpd 443 N-(1-amino-2-methyl-1-oxopropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0772] Cpd 444 N-(1-amino-2-methyl-1-oxopropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0773] Cpd 445 N-(1-amino-3-(cyclopropyl(methyl)amino)-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0774] Cpd 446 N-(1-amino-3-(cyclopropyl(methyl)amino)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0775] Cpd 447 N-(1-amino-3-(difluoromethoxy)-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0776] Cpd 448 N-(1-amino-3-(difluoromethoxy)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0777] Cpd 449 N-(1-amino-3-(dimethylamino)-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0778] Cpd 450 N-(1-amino-3-(dimethylamino)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0779] Cpd 451 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0780] Cpd 452 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0781] Cpd 453 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0782] Cpd 454 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0783] Cpd 455 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0784] Cpd 456 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0785] Cpd 457 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0786] Cpd 458 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,4-dimethylthiazolyl-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0787] Cpd 459 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0788] Cpd 460 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0789] Cpd 461 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0790] Cpd 462 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0791] Cpd 463 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0792] Cpd 464 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0793] Cpd 465 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0794] Cpd 466 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0795] Cpd 467 N-(1-amino-3-methoxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0796] Cpd 468 N-(1-amino-3-methoxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0797] Cpd 469 N-(1-amino-4-hydroxy-1-oxobut-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0798] Cpd 470 N-(1-carbamoyl-3,3-difluorocyclobutyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0799] Cpd 471 N-(1-carbamoylcyclobutyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0800] Cpd 472 N-(1-carbamoylcyclobutyl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0801] Cpd 473 N-(1-carbamoylcyclobutyl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0802] Cpd 474 N-(1-carbamoylcyclobutyl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0803] Cpd 475 N-(1-carbamoylcyclopropyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0804] Cpd 476 N-(1-carbamoylcyclopropyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0805] Cpd 477 N-(1-carbamoylcyclopropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0806] Cpd 478 N-(1-carbamoylcyclopropyl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0807] Cpd 479 N-(1-carbamoylcyclopropyl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0808] Cpd 480 N-(1-carbamoylcyclopropyl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0809] Cpd 481 N-(1-hydroxy-2-methylpropyl-2-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0810] Cpd 482 N-(1-hydroxy-2-methylpropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0811] Cpd 483 N-(1-hydroxy-2-methylpropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0812] Cpd 484 N-(1-hydroxy-2-methylpropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0813] Cpd 485 N-(1-hydroxy-2-methylpropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0814] Cpd 486 N-(1-hydroxy-2-methylpropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0815] Cpd 487 N-(1-hydroxy-3-morpholinopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0816] Cpd 488 N-(1-hydroxy-3-morpholinopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0817] Cpd 489 N-(1-hydroxypropyl-2-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0818] Cpd 490 N-(1-hydroxypropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0819] Cpd 491 N-(1-hydroxypropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0820] Cpd 492(S)-N-(1-hydroxypropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0821] Cpd 493(R)-N-(1-hydroxypropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0822] Cpd 494(S)-N-(1-hydroxypropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0823] Cpd 495(R)-N-(1-hydroxypropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0824] Cpd 496(S)-N-(1-hydroxypropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0825] Cpd 497(R)-N-(1-hydroxypropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0826] Cpd 498 N-(2,2-difluoroethyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0827] Cpd 499 N-(2,2-difluoropropyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0828] Cpd 500 N-(2,2-difluoropropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0829] Cpd 501 N-(2-acetamidoethyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0830] Cpd 502 N-(2-amino-1-cyano-2-oxoethyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0831] Cpd 503 N-(2-amino-2-oxoethyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0832] Cpd 504 N-(2-fluoro-2-methylpropyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0833] Cpd 505 N-(2-fluoro-2-methylpropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0834] Cpd 506 N-(2-hydroxy-2-methylpropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0835] Cpd 507 N-(3-(aminomethyl)oxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0836] Cpd 508 N-(3-(dimethylamino)oxetane-3-carbonyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0837] Cpd 509 N-(3-(dimethylcarbamoyl)oxetane-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0838] Cpd 510 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0839] Cpd 511 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[0840] Cpd 512 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0841] Cpd 513 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0842] Cpd 514 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0843] Cpd 515 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[0844] Cpd 516 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0845] Cpd 517 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0846] Cpd 518 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0847] Cpd 519 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0848] Cpd 520 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0849] Cpd 521 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0850] Cpd 522 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0851] Cpd 523 N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0852] Cpd 524 N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0853] Cpd 525 N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0854] Cpd 526 N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0855] Cpd 527 N-(3-(hydroxymethyl)oxetane-3-yl)-2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0856] Cpd 528 N-(3-(hydroxymethyl)oxetane-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0857] Cpd 529 N-(3-(hydroxymethyl)oxetane-3-yl)-N,2-dimethyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0858] Cpd 530 N-(3-(hydroxymethyl)pyrrolidone-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0859] Cpd 531 N-(3-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0860] Cpd 532 N-(3-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0861] Cpd 533 N-(3-(hydroxymethyl)tetrahydrofuran-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0862] Cpd 534 N-(3-(hydroxymethyl)tetrahydrofuran-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0863] Cpd 535 N-(3-(hydroxymethyl)tetrahydrofuran-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0864] Cpd 536 N-(3-(hydroxymethyl)tetrahydrofuran-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0865] Cpd 537 N-(3,3-difluoro-1-(hydroxymethyl)cyclobutyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0866] Cpd 538 N-(3,3-difluoropiperidin-4-yl)-2,4-dimethyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0867] Cpd 539 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(((2-(trifluoromethyl)pyridin-3-yl)oxy)methyl)benzofuran-3-carboxamide

[0868] Cpd 540 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((1-methyl-1H-1,2,3-triazol-4-yl)methoxy)benzofuran-3-carboxamide

[0869] Cpd 541 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((1-methyl-1H-1,2,3-triazol-5-yl)methoxy)benzofuran-3-carboxamide

[0870] Cpd 542 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((1-methyl-1H-1,2,4-triazol-3-yl)methoxy)benzofuran-3-carboxamide

[0871] Cpd 543 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0872] Cpd 544 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((1-methyl-2-oxo-1,2-dihydropyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0873] Cpd 545 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((1-methyl-6-oxo-1,6-dihydropyridin-2-yl)methoxy)benzofuran-3-carboxamide

[0874] Cpd 546 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0875] Cpd 547 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0876] Cpd 548 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-methylpyrimidin-4-yl)methoxy)benzofuran-3-carboxamide

[0877] Cpd 549 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0878] Cpd 550 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((3-methyloxetane-3-yl)methoxy)benzofuran-3-carboxamide

[0879] Cpd 551 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((4-methyloxazol-2-yl)methoxy)benzofuran-3-carboxamide

[0880] Cpd 552 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((4-methylthiazolyl-2-yl)methoxy)benzofuran-3-carboxamide

[0881] Cpd 553 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((5-methylisoxazol-3-yl)methoxy)benzofuran-3-carboxamide

[0882] Cpd 554 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((5-methylpyrazin-2-yl)methoxy)benzofuran-3-carboxamide

[0883] Cpd 555 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((5-methylthiazolyl-2-yl)methoxy)benzofuran-3-carboxamide

[0884] Cpd 556 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-((6-methylpyridazin-3-yl)methoxy)benzofuran-3-carboxamide

[0885] Cpd 557 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxamide

[0886] Cpd 558 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(pyridin-3-ylmethoxy)benzofuran-3-carboxamide

[0887] Cpd 559 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(pyrimidin-2-ylmethoxy)benzofuran-3-carboxamide

[0888] Cpd 560 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0889] Cpd 561 N-(3,3-difluoropiperidin-4-yl)-2-methyl-5-(thiazolyl-5-ylmethoxy)benzofuran-3-carboxamide

[0890] Cpd 562 N-(3,3-difluoropiperidin-4-yl)-4-fluoro-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0891] Cpd 563 N-(3,3-difluoropiperidin-4-yl)-5-((2,4-dimethylthiazolyl-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0892] Cpd 564 N-(3,3-difluoropiperidin-4-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0893] Cpd 565 N-(3,3-difluoropiperidin-4-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0894] Cpd 566 N-(3,3-difluoropiperidin-4-yl)-5-((3-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0895] Cpd 567 N-(3,3-difluoropiperidin-4-yl)-5-((5-(2-hydroxyethoxy)pyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0896] Cpd 568 N-(3,3-difluoropiperidin-4-yl)-5-((5-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0897] Cpd 569 N-(3,3-difluoropiperidin-4-yl)-5-((6-hydroxypyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0898] Cpd 570 N-(3,3-difluoropiperidin-4-yl)-5-((6-methoxypyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0899] Cpd 571 N-(3,3-difluoropiperidin-4-yl)-5-(imidazo[1,2-a]pyridin-6-ylmethoxy)-2-methylbenzofuran-3-carboxamide

[0900] Cpd 572 N-(3,3-difluoropiperidin-4-yl)-6-fluoro-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0901] Cpd 573 N-(3,3-difluoropiperidin-4-yl)-7-fluoro-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0902] Cpd 574 N-(3,3-difluoropropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0903] Cpd 575 N-(3-amino-2-(dimethylamino)-3-oxopropyl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[0904] Cpd 576 N-(3-amino-2,2-dimethyl-3-oxopropyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0905] Cpd 577 N-(3-carbamoyloxetane-3-yl)-2-(difluoromethyl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0906] Cpd 578 N-(3-carbamoyloxetane-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0907] Cpd 579 N-(3-carbamoyloxetane-3-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0908] Cpd 580 N-(3-carbamoyloxetane-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0909] Cpd 581 N-(3-carbamoyloxetane-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0910] Cpd 582 N-(3-carbamoyloxetane-3-yl)-2-methyl-5-(thiazolyl-2-ylmethoxy)benzofuran-3-carboxamide

[0911] Cpd 583 N-(3-carbamoyloxetane-3-yl)-4-fluoro-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0912] Cpd 584 N-(3-carbamoyloxetane-3-yl)-5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0913] Cpd 585 N-(3-carbamoyloxetane-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0914] Cpd 586 N-(3-carbamoyloxetane-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0915] Cpd 587 N-(3-carbamoyloxetane-3-yl)-6-fluoro-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0916] Cpd 588 N-(3-carbamoyloxetane-3-yl)-7-fluoro-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0917] Cpd 589 N-(3-carbamoyloxetane-3-yl)-N,2-dimethyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0918] Cpd 590 N-(3-carbamoyltetrahydro-2H-pyran-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0919] Cpd 591 N-(3-carbamoyltetrahydrofuran-3-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0920] Cpd 592 N-(3-carbamoyltetrahydrofuran-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0921] Cpd 593 N-(3-carbamoyltetrahydrofuran-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0922] Cpd 594 N-(3-carbamoyltetrahydrofuran-3-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0923] Cpd 595 N-(3-carbamoyltetrahydrofuran-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0924] Cpd 596 N-(3-carbamoyltetrahydrofuran-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0925] Cpd 597 N-(3-carbamoyltetrahydrofuran-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0926] Cpd 598 N-(3-carbamoyltetrahydrofuran-3-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0927] Cpd 599 N-(3-cyanoxacyclobutane-3-yl)-N,2-dimethyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0928] Cpd 600 N-(3-hydroxy-1-(methylamino)-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0929] Cpd 601 N-(3-hydroxy-1-(methylamino)-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0930] Cpd 602 N-(3-hydroxy-2,2-dimethylpropyl)-2-methyl-5-((4-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0931] Cpd 603 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2,4-dimethyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0932] Cpd 604 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((1-methyl-1H-1,2,3-triazol-4-yl)methoxy)benzofuran-3-carboxamide

[0933] Cpd 605 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((1-methyl-1H-1,2,3-triazol-5-yl)methoxy)benzofuran-3-carboxamide

[0934] Cpd 606 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((1-methyl-1H-1,2,4-triazol-3-yl)methoxy)benzofuran-3-carboxamide

[0935] Cpd 607 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((1-methyl-1H-imidazol-5-yl)methoxy)benzofuran-3-carboxamide

[0936] Cpd 608 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0937] Cpd 609 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((1-methyl-2-oxo-1,2-dihydropyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0938] Cpd 610 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-6-methyl-5-((1-methyl-2-oxo-1,6-dihydropyridin-2-yl)methoxy)benzofuran-3-carboxamide

[0939] Cpd 611 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0940] Cpd 612 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((2-methylpyrimidin-4-yl)methoxy)benzofuran-3-carboxamide

[0941] Cpd 613 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0942] Cpd 614 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((2-oxo-1,2-dihydropyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0943] Cpd 615 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide

[0944] Cpd 616 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methyloxazol-2-yl)methoxy)benzofuran-3-carboxamide

[0945] Cpd 617 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-2-yl)methoxy)benzofuran-3-carboxamide

[0946] Cpd 618 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((5-methylisoxazol-3-yl)methoxy)benzofuran-3-carboxamide

[0947] Cpd 619 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((5-methylpyrazin-2-yl)methoxy)benzofuran-3-carboxamide

[0948] Cpd 620 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((5-methylthiazolyl-2-yl)methoxy)benzofuran-3-carboxamide

[0949] Cpd 621 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((6-methylpyridazin-3-yl)methoxy)benzofuran-3-carboxamide

[0950] Cpd 622 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0951] Cpd 623 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-(1-(4-methylthiazolyl-5-yl)ethoxy)benzofuran-3-carboxamide

[0952] Cpd 624 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxamide

[0953] Cpd 625 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-(pyridin-3-ylmethoxy)benzofuran-3-carboxamide

[0954] Cpd 626 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-(pyrimidin-2-ylmethoxy)benzofuran-3-carboxamide

[0955] Cpd 627 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methyl-5-(thiazolyl-5-ylmethoxy)benzofuran-3-carboxamide

[0956] Cpd 628 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-hydroxypyridin-4-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0957] Cpd 629 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((2-methoxypyridin-4-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0958] Cpd 630 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((6-hydroxypyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0959] Cpd 631 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((6-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0960] Cpd 632 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((6-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0961] Cpd 633 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-(imidazo[1,2-a]pyridin-6-ylmethoxy)-2-methylbenzofuran-3-carboxamide

[0962] Cpd 634 N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-N,2-dimethyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0963] Cpd 635 N-(4,4-difluoropiperidin-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0964] Cpd 636 N-(4,4-difluoropiperidin-3-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0965] Cpd 637 N-(4,4-difluoropiperidin-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0966] Cpd 638 N-(4,4-difluoropyrrolidone-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0967] Cpd 639 N-(4,4-difluoropyrrolidone-3-yl)-2-methyl-5-((1-methyl-1H-pyrazole-5-yl)methoxy)benzofuran-3-carboxamide

[0968] Cpd 640 N-(4,4-difluoropyrrolidone-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0969] Cpd 641 N-(4,4-difluorotetrahydrofuran-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0970] Cpd 642 N-(4,4-difluorotetrahydrofuran-3-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0971] Cpd 643 N-(4,4-difluorotetrahydrofuran-3-yl)-2-methyl-5-((2-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide

[0972] Cpd 646 N-(4,4-difluorotetrahydrofuran-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0973] Cpd 647 N-(4,4-difluorotetrahydrofuran-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[0974] Cpd 648 N-(4,4-difluorotetrahydrofuran-3-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0975] Cpd 649 N-(4-amino-2-methyl-4-oxobut-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0976] Cpd 650 N-(4-carbamoyltetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0977] Cpd 651 N-(4-hydroxy-2-methylbut-2-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0978] Cpd 652 N-(4-hydroxy-2-methylbut-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0979] Cpd 653 N-(cis-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0980] Cpd 654 N-(trans-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide

[0981] Cpd 655 N-(cis-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0982] Cpd 656 N-(trans-4-hydroxytetrahydrofuran-3-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[0983] Cpd 657 N3-(3,3-difluoropiperidin-4-yl)-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-2,3-dicarboxamide

[0984] Cpd 658 N3-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-2,3-dicarboxamide

[0985] Cpd 659 N-Cyclobutyl-N-(2-hydroxyethyl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0986] Cpd 660 N-Cyclobutyl-N-(2-hydroxyethyl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[0987] Cpd 661 2-Methyl-5-((4-methylthiazo-5-yl)methoxy)-N-(2-oxozyracycloheptane-3-yl)benzofuran-3-carboxamide

[0988] Cpd 662 N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-3-ylmethoxy)benzofuran-3-carboxamide

[0989] Cpd 663 N-(4,4-difluoropyrrolidone-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0990] Cpd 664 N-(4,4-difluorotetrahydrofuran-3-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide

[0991] Cpd 665 N-(4,4-difluorotetrahydrofuran-3-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0992] Cpd 666 2-Methyl-5-((4-methylthiazolyl-5-yl)methoxy)-N-(2,2,2-trifluoroethyl)benzofuran-3-carboxamide

[0993] Cpd 667 5-((1,4-dimethyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0994] Cpd 668(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1,4-dimethyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0995] Cpd 669 5-((4-chloro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0996] Cpd 670(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-chloro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0997] Cpd 671 5-((4-chloro-1-isopropyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[0998] Cpd 672(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-chloro-1-isopropyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[0999] Cpd 673 2-Methyl-5-((3-methylisoxazol-5-yl)methoxy)benzofuran-3-carboxylic acid

[1000] Cpd 674(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((3-methylisoxazol-5-yl)methyl)benzofuran-3-carboxamide

[1001] Cpd 675 5-((1-isopropyl-1H-pyrazole-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[1002] Cpd 676(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-isopropyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1003] Cpd 677 5-((2,4-dimethyloxazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[1004] Cpd 678(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,4-dimethyloxazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1005] Cpd 679 2-Methyl-5-((4-methyloxazol-5-yl)methoxy)benzofuran-3-carboxylic acid

[1006] Cpd 680(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[1007] Cpd 681 5-((2-isopropylthiazolyl-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[1008] Cpd 682(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-isopropylthiazolyl-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1009] Cpd 683 N-(1-(difluoromethyl)cyclobutyl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1010] Cpd 684(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylthiazolyl-2-yl)methoxy)benzofuran-3-carboxamide

[1011] Cpd 685 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-((3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide

[1012] Cpd 686(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-3-yl)methoxy)benzofuran-3-carboxamide

[1013] Cpd 687 2-Methyl-5-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxylic acid

[1014] Cpd 688(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[1015] Cpd 689 5-((1-(cyclopropylmethyl)-1H-pyrazole-5-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[1016] Cpd 690(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-(cyclopropylmethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1017] Cpd 691 2-Methyl-5-((1-Methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxylic acid

[1018] Cpd 692(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide

[1019] Cpd 693 2-Methyl-5-((4-(trifluoromethyl)thiazolyl-5-yl)methoxy)benzofuran-3-carboxylic acid

[1020] Cpd 694(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-(trifluoromethyl)thiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1021] Cpd 695(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(thiazo-2-ylmethoxy)benzofuran-3-carboxamide

[1022] Cpd 696 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-5-((5-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1023] Cpd 697(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(thiazolyl-5-ylmethoxy)benzofuran-3-carboxamide

[1024] Cpd 698(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide

[1025] Cpd 699 2-Methyl-5-((5-methylpyridin-2-yl)methoxy)benzofuran-3-carboxylic acid

[1026] Cpd 700(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylpyridin-2-yl)methoxy)benzofuran-3-carboxamide

[1027] Cpd 701 5-((2-cyclopropylpyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[1028] Cpd 702(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-cyclopropylpyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1029] Cpd 703 5-((3-cyclopropylpyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[1030] Cpd 704(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((3-cyclopropylpyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide;

[1031] Cpd 705 5-((3-cyclopropylpyridin-2-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[1032] Cpd 706(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-(azacyclobutan-1-yl)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1033] Cpd 707 2-Methyl-5-((2-methylpyrimidin-5-yl)methoxy)benzofuran-3-carboxylic acid

[1034] Cpd 708(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylpyrimidin-5-yl)methoxy)benzofuran-3-carboxamide

[1035] Cpd 709 5-((2-cyclopropoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxylic acid

[1036] Cpd 710(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-cyclopropoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1037] Cpd 711 5-((2-cyclopropoxypyridin-3-yl)methoxy)-N-(4-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)-2-methylbenzofuran-3-carboxamide

[1038] Cpd 712(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyrimidin-2-ylmethoxy)benzofuran-3-carboxamide

[1039] Cpd 713 2-Methyl-5-(pyrazin-2-ylmethoxy)benzofuran-3-carboxylic acid

[1040] Cpd 714(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyrazin-2-ylmethoxy)benzofuran-3-carboxamide

[1041] Cpd 715(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1042] Cpd 716(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-4-ylmethoxy)benzofuran-3-carboxamide

[1043] Cpd 717 5-((3-(difluoromethyl)pyridin-2-yl)methoxy)-N-(3,3-difluoropiperidin-4-yl)-2-methylbenzofuran-3-carboxamide

[1044] Cpd 718 N-((2S,3R)-1-amino-3-hydroxy-1-oxobut-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[1045] Cpd 719 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[1046] Cpd 720 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1047] Cpd 721 N-(1-(difluoromethyl)cyclobutyl)-2-methyl-5-((4-methylthiazolyl)methoxy)benzofuran-3-carboxamide

[1048] Cpd 722 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[1049] Cpd 723 N-(3,3-difluorotetrahydro-2H-pyran-4-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1050] Cpd 724 N-(3,3-difluorotetrahydro-2H-pyran-4-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1051] Cpd 725 N-(3-carbamoyltetrahydrofuran-3-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[1052] Cpd 726 N-(1-amino-3-(methanesulfonyl)-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1053] Cpd 727 N-(1-imino-1-oxotetrahydro-1H-1l6-thiophene-3-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1054] Cpd 728 N-(3-(hydroxymethyl)pyrrolidone-3-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1055] Cpd 729 N-(1-amino-1-oxo-3-(1H-1,2,4-triazol-1-yl)propyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1056] Cpd 730 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((3-(trifluoromethyl)-1H-pyrazole-4-yl)methoxy)benzofuran-3-carboxamide

[1057] Cpd 731 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-((3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide

[1058] Cpd 732 N-(3-(hydroxymethyl)-2-oxopiperidin-3-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide

[1059] Cpd 733 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-((1-methyl-1H-pyrazole-5-yl)methoxy)benzofuran-3-carboxamide

[1060] Cpd 734 N-(3-(hydroxymethyl)-2-oxopyrrolidone-3-yl)-2-methyl-5-(pyridazin-3-ylmethoxy)benzofuran-3-carboxamide

[1061] Cpd 735 5-((5-fluoropyridin-2-yl)methoxy)-N-(3-(hydroxymethyl)-2-oxopyrrolidine-3-yl)-2-methylbenzofuran-3-carboxamide

[1062] Cpd 736 5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-N-(3-(hydroxymethyl)-2-oxopyrrolidine-3-yl)-2-methylbenzofuran-3-carboxamide

[1063] Cpd 737 5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-N-(3-(hydroxymethyl)-2-oxopiridine-3-yl)-2-methylbenzofuran-3-carboxamide

[1064] Cpd 738 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[1065] Cpd 739 N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((5-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1066] Cpd 740 N-(3-carbamoyltetrahydrofuran-3-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1067] Cpd 741(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((5-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide

[1068] Cpd 742(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1069] Cpd 743(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[1070] Cpd 744(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[1071] Cpd 745(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1072] Cpd 746(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[1073] Cpd 747(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-cyclopropyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide

[1074] Cpd 748(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-cyclopropyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1075] Cpd 749(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-cyclopropyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide

[1076] Cpd 750(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-cyclopropyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide

[1077] Cpd 751(S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-cyclopropyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide

[1078] And its physiologically acceptable salts.

[1079] The benzofuran derivatives according to the invention are used to treat pain, preferably selected from nociceptive pain, inflammatory pain, and neuropathic pain. More preferably, the pain is postoperative pain.

[1080] Another aspect of the present invention relates to compounds of formula (I),

[1081]

[1082] As defined above, its stereoisomers, physiologically acceptable salts, solvates, and / or polymorphs; preferably, wherein

[1083] (a-1)Q means -OR 2 And R 1 Indicates -CH2F, -CHF2, or -CF3; and / or

[1084] (a-2)Q means -OR 2 And R 5 and R 5 At least one of ' does not represent -H; and / or

[1085] (a-3)Q means -OR 2 And R 6 Not indicating -H; and / or

[1086] (a-3)Q means -OR 2 And R 8 It does not represent -H;

[1087] or

[1088] (b-1)Q represents -NR 3 R 4 The condition is that the following compounds and their salts are excluded.

[1089]

[1090]

[1091] and / or

[1092] (b-2)Q represents -NR 3 R 4 And R 1 It represents -CH2F, -CHF2, -CF3 or -cyclopropyl; and / or

[1093] (b-3)Q represents -NR 3 R 4 And R 1 Indicates -CH2F, -CHF2, or -CF3; and / or

[1094] (b-4)Q represents -NR 3 R 4 And R 5 and R 5 At least one of ' does not represent -H; and / or

[1095] (b-5)Q represents -NR 3 R 4 And R 3 It represents -H.

[1096] In preferred embodiments of the benzofuran derivatives (a-1), (a-2), (a-3), (b-1), (b-2), (b-3), and (b-4) according to the present invention, T represents -O- and U represents -CR. 5 R 5 '-(i.e., benzofuran derivatives have formula (II)).

[1097] Q, T, U, V, R 1 R 2 R 3 R 4 R 5 R 5 '、R 6 R 7 and R8 All definitions, preferred embodiments, and preferred meanings (including preferred substituents) also apply similarly to the benzofuran derivatives according to the invention, including but not limited to (a-1), (a-2), (a-3), (b-1), (b-2), (b-3), and (b-4), which are not necessarily limited to the use in treating pain. Therefore, this aspect of the invention relates to the benzofuran derivatives themselves, compositions comprising benzofuran derivatives, pharmaceuticals comprising benzofuran derivatives, and benzofuran derivatives for the prevention and / or treatment of TRPM3-mediated conditions (such as pain and / or inflammatory hypersensitivity); and / or for the treatment of pain and / or inflammatory hypersensitivity. Preferably, the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain. More preferably, the pain is postoperative pain.

[1098] In a preferred embodiment of the invention, the benzofuran derivative is selected from the group consisting of: cpd001 to cpd207 as described above and their physiologically acceptable salts.

[1099] Another aspect of the present invention relates to pharmaceutical compositions or drugs comprising compounds according to the present invention as described above.

[1100] Throughout this specification, references to "an embodiment" or "an embodiment" mean that a particular feature, structure, or characteristic described in connection with that embodiment is included in at least one embodiment of the invention. Therefore, the phrases "in one embodiment" or "in an embodiment" appearing throughout this specification do not necessarily refer to the same embodiment, but may refer to the same embodiment. Furthermore, in one or more embodiments, specific features, structures, or characteristics can be combined in any suitable manner, as will be apparent to those skilled in the art from this disclosure. Moreover, embodiments described with respect to one aspect of the invention can be used in another aspect of the invention and can be combined. When referring to singular nouns, the use of indefinite or definite articles, such as "a" or "an," or "the," includes the plural form of the noun, unless otherwise specified.

[1101] Similarly, it should be understood that in the description of exemplary embodiments of the invention, various features of the invention are sometimes combined in a single embodiment, drawing or description thereof for the purpose of simplifying the disclosure and aiding in the understanding of one or more aspects of the invention.

[1102] In the following definitions, the number of carbon atoms represents the maximum number of carbon atoms that are typically best present in the substituent or linker; it should be understood that, where otherwise stated in this application, the number of carbon atoms represents the optimal maximum number of carbon atoms for that particular substituent or linker.

[1103] As used herein, the term "leaving group" or "LG" refers to a chemical group that is readily replaced, cleaved, or hydrolyzed by a nucleophile under basic or acidic conditions. In one specific embodiment, the leaving group is selected from halogen atoms (e.g., Cl, Br, I) or sulfonates (e.g., methanesulfonate, toluenesulfonate, trifluoromethanesulfonate).

[1104] The term "protecting group" refers to a part of a compound that masks or alters the properties of a functional group or the properties of the compound as a whole. The chemical substructure of protecting groups varies considerably. One function of protecting groups is as intermediates in the synthesis of parent drugs. Chemical protecting groups and protecting / deprotecting 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 often used to mask the reactivity of certain functional groups to contribute to the efficiency of desired chemical reactions, such as the orderly and planned formation and breaking of chemical bonds. Protection of a compound's functional groups alters other physical properties besides the reactivity of the protected functional group, such as polarity, lipophilicity (hydrophobicity), and other properties measurable by commonly used analytical tools. Chemically protected intermediates can themselves be biologically active or inactive.

[1105] Protected compounds can also exhibit altered, and in some cases optimized, in vitro and in vivo properties, such as resistance to cell membrane degradation or chelation. In this role, the protected compound with the intended therapeutic effect may be referred to as a prodrug. Another function of the protecting group is to convert the parent drug into a prodrug, thereby releasing the parent drug during prodrug conversion in vivo. Because the active prodrug can be absorbed more efficiently than the parent drug, it can have greater potency in vivo. In the case of chemical intermediates, the protecting group is removed in vitro, or in the case of prodrugs, the protecting group is removed in vivo. For chemical intermediates, whether the product obtained after deprotection (e.g., an alcohol) is physiologically acceptable is not particularly important, although it is generally desirable for the product to be pharmacologically harmless.

[1106] As used in this article, the term "heteroatom" refers to an atom selected from the following: nitrogen, which can be quaternized; oxygen; and sulfur, including sulfoxide and sulfone.

[1107] As used herein, the term "saturated or unsaturated alkyl" encompasses both saturated and unsaturated alkyl groups, such as alkenyl and ynyl groups. The term "alkyl" as used herein refers to a straight-chain or branched n-, secondary, or tertiary hydrocarbon without unsaturated sites. Examples are methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl (i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl, and 3,3-dimethyl-2-butyl. As used herein, the term "alkenyl" refers to a straight-chain or branched n-, secondary, or tertiary hydrocarbon having at least one unsaturated site (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp2 double bond. Examples include, but are not limited to, ethylene or vinyl (-CH=CH2), allyl (-CH2CH=CH2), and 5-hexenyl (-CH2CH2CH2CH2CH=CH2). The double bond can be cis or trans configuration. As used herein, the term "alkynyl" refers to a straight-chain or branched n-, secondary, or tertiary hydrocarbon having at least one unsaturated site (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp triple bond. Examples include, but are not limited to, ethynyl (-C≡CH) and 1-propynyl (propynyl, -CH2C≡CH).

[1108] As used herein, the term "saturated or unsaturated alkylene" encompasses both saturated and unsaturated alkylenes, such as alkenyl, alynyl, alynylynyl, etc. The term "alkylene" as used herein refers to a saturated, straight-chain, or branched hydrocarbon group having two monovalent groups derived from the same or two different carbon atoms of a parent alkane by removing two hydrogen atoms. Typical alkylenes include, but are not limited to, methylene (-CH2-), 1,2-ethyl (-CH2CH2-), 1,3-propyl (-CH2CH2CH2-), 1,4-butyl (-CH2CH2CH2CH2-), etc. The term "alkenyl" as used herein refers to a straight-chain or branched hydrocarbon group having at least one unsaturated site (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp2 double bond, and having two monovalent groups derived from the same or two different carbon atoms of a parent alkene by removing two hydrogen atoms. As used herein, the term "ethynyl" refers to a straight-chain or branched hydrocarbon group having at least one unsaturated site (usually 1 to 3, preferably 1), namely a carbon-carbon sp triple bond and having two monovalent groups at the center derived by removing two hydrogen atoms from the same or two different carbon atoms of the parent alkyne.

[1109] As used herein, the term "saturated or unsaturated heteroalkyl" encompasses both saturated and unsaturated heteroalkyl groups, such as heteroalkenyl, heteroynyl, heteroenynyl, etc. The term "heteroalkyl" as used herein refers to a straight-chain or branched alkyl group in which one or more carbon atoms (typically 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 -CH3 groups of the alkyl group may be replaced by -NH2 and / or one or more -CH2- groups of the alkyl group may be replaced by -NH-, -O-, or -S-. The S atoms in the chain may optionally be oxidized by one or two oxygen atoms to provide sulfoxides and sulfones, respectively. Furthermore, the heteroalkyl groups in the benzofuran derivatives of the present invention may contain oxo or thio groups on any carbon or heteroatom, which will produce stable compounds. Exemplary heteroalkyl groups include, but are not limited to, alcohols, alkyl ethers (e.g., -methoxy, -ethoxy, -butoxy…), primary, secondary, and tertiary alkylamines, amides, ketones, esters, alkyl sulfides, and alkyl sulfones. The term "heteroalkenyl" refers to a straight-chain or branched alkenyl group in which one or more carbon atoms (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 imine, -O-alkenyl, -NH-alkenyl, -N(alkenyl)2, -N(alkyl)(alkenyl), and -S-alkenyl. The term "heteroyynyl" as used herein refers to a straight-chain or branched ynyl 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 heteroyynyl includes -cyano, -O-ynyl, -NH-ynyl, -N(ynyl)2, -N(alkyl)(ynyl), -N(alkenyl)(ynyl), and -S-ynyl.

[1110] As used herein, the term "saturated or unsaturated heteroalkylene" encompasses both saturated and unsaturated heteroalkylene, such as heteroalkylene, heteroynylene, and heteroynylene. The term "heteroalkylene" as used herein refers to a straight-chain or branched alkylene group in which one or more carbon atoms (typically 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. The term "heteroalkylene" as used herein refers to a straight-chain or branched alkenylene group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. The term "heteroynylene" as used herein refers to a straight-chain or branched alynylene group in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms.

[1111] As used herein, the term "saturated or unsaturated cycloalkyl" encompasses both saturated and unsaturated cycloalkyl groups, such as cycloalkenyl and cycloynyl groups. Unless otherwise stated, the term "cycloalkyl" as used herein refers to a saturated cycloalkyl group, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, norbornyl, fampyl, decahydronaphthyl, adamantyl, etc. The term "cycloalkenyl" as used herein refers to a non-aromatic cyclic hydrocarbon group having at least one unsaturated site (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp2 double bond. Examples include, but are not limited to, cyclopentenyl and cyclohexenyl. The double bond can be cis or trans configuration. The term "cycloynyl" as used herein refers to a non-aromatic cyclic hydrocarbon group having at least one unsaturated site (usually 1 to 3, preferably 1), i.e., a carbon-carbon sp triple bond. An example is cyclohept-1-yne. Fusion systems of cycloalkyl and heterocyclic alkyl rings are considered heterocyclic alkyl groups, regardless of the ring bonded to the core structure. Fused systems of cycloalkyl and aryl rings are considered aryl, regardless of the ring bonded to the core structure. Fused systems of cycloalkyl and heteroaryl rings are considered heteroaryl, regardless of the ring bonded to the core structure.

[1112] As used herein, the term "saturated or unsaturated heterocyclic alkyl" encompasses both saturated heterocyclic alkyl and unsaturated non-aromatic heterocyclic alkyl that includes at least one heteroatom, i.e., N, O, or S, as a ring member. Unless otherwise stated, the term "heterocyclic alkyl" as used herein means a "cycloalkyl" in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Unless otherwise stated, the term "heterocyclic alkenyl" as used herein means a "cycloalkenyl" in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Unless otherwise stated, the term "heterocyclic alkynyl" as used herein means a "cycloalkynyl" in which one or more carbon atoms (typically 1, 2, or 3) are replaced by oxygen, nitrogen, or sulfur atoms, provided that the chain may not contain two adjacent O atoms or two adjacent S atoms. Examples of saturated and unsaturated heterocyclic alkyl groups include, but are not limited to, azacycloheptane, 1,4-oxazacycloheptane, azacyclobutane, azacyclobutane, azacyclopropane, azacyclooctane, diazacycloheptane, dioxacyclohexane, dioxapentane, dithiazoline, dithiopentane, imidazoline, isothiazolane, isoxazolane, morpholine, oxazolane, epoxide, oxacyclobutane, ethylene oxide, piperazine, piperidine, pyrazolane, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, and thiohexacyclobutane. Thionylpropane, thiocyclopentane, thiomorpholine, indoline, benzodihydrofuran, dihydrobenzothiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine.Other heterocyclic alkyl groups used in the sense of this invention are described in Paquette, Leo A., *Principles of Modern Heterocyclic Chemistry* (W.A. Benjamin, New York, 1968), particularly Chapters 1, 3, 4, 6, 7, and 9; *The Chemistry of Heterocyclic Compounds, A series of Monographs* (John Wiley & Sons, New York, 1950–present), particularly Volumes 13, 14, 16, 19, and 28; and Katritsky, Alan R., Rees, C.W., and Scriven, E., *Comprehensive Heterocyclic Chemistry* (Pergamon Press). Press), 1996; and Journal of the American Chemical Society (J. Am. Chem. Soc.) (1960) 82:5566. When heterocyclic alkyl groups do not contain nitrogen as a ring member, they are usually bonded by carbon. When heterocyclic alkyl groups contain nitrogen as a ring member, they can be bonded by nitrogen or carbon. Fused systems of heterocyclic alkyl rings with cycloalkyl rings are considered heterocyclic alkyl, regardless of the ring bonded to the core structure. Fused systems of heterocyclic alkyl rings with aryl rings are considered heterocyclic alkyl, regardless of the ring bonded to the core structure. Fused systems of heterocyclic alkyl rings with heteroaryl rings are considered heteroaryl, regardless of the ring bonded to the core structure.

[1113] As used herein, the term "aryl" refers to an aromatic hydrocarbon. Typical aryl groups include, but are not limited to, one-membered rings or fused two- or three-membered rings, derived from groups such as benzene, naphthalene, anthracene, and biphenyl. Fused systems of aromatic rings with cycloalkyl rings are considered aryl, regardless of the ring bonded to the core structure. Fused systems of aryl rings with heterocyclic alkyl rings are considered heterocyclic alkyl, regardless of the ring bonded to the core structure. Therefore, indoline, dihydrobenzofuran, dihydrobenzothiophene, etc., are considered heterocyclic alkyl groups of this invention. Fused systems of aryl rings with heteroaryl rings are considered heteroaryl, regardless of the ring bonded to the core structure.

[1114] As used herein, the term "heteroaryl" refers to an aromatic ring system that includes at least one heteroatom (i.e., N, O, or S) as a ring member of the aromatic ring system. Examples of heteroaryl groups include, but are not limited to, benzimidazole, benzisoxazole, benzoxoxazole, benzodioxane, benzofuran, benzothiadiazole, benzothiazol, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazon, imidazole, imidazopyridine, indazole, indole, inazine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthidine, oxadiazole, oxazole, hydroxyindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazolium, thiadiazole, thiazolium, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine.

[1115] For further examples, carbon-bonded heterocycles are bonded at positions 2, 3, 4, 5, or 6 of pyridine, positions 3, 4, 5, or 6 of pyridazine, positions 2, 4, 5, or 6 of pyrimidine, positions 2, 3, 5, or 6 of pyrazine, positions 2, 3, 4, or 5 of furan, tetrahydrofuran, thiophene, pyrrole, or tetrahydropyrrole, positions 2, 4, or 5 of oxazole, imidazole, or thiazole, positions 3, 4, or 5 of isoxazole, pyrazole, or isothiazole, positions 2 or 3 of aziridine, positions 2, 3, or 4 of aziridine, positions 2, 3, 4, 5, 6, 7, or 8 of quinoline, or positions 1, 3, 4, 5, 6, 7, or 8 of isoquinoline.

[1116] Preferred carbon-bonded heterocycles include 2-pyridyl, 3-pyridyl, 4-pyridyl, 5-pyridyl, 6-pyridyl, 3-pyridazinyl, 4-pyridazinyl, 5-pyridazinyl, 6-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 6-pyrimidinyl, 2-pyrazinyl, 3-pyrazinyl, 5-pyrazinyl, 6-pyrazinyl, 2-thiazolyl, 4-thiazolyl, or 5-thiazolyl. For example, the nitrogen-bonded heterocycle is bonded at the 1-position of aziridine, aziridine, pyrrole, pyrrolidine, 2-pyrrololine, 3-pyrroleoline, imidazole, imidazolidine, 2-imidazoline, 3-imidazoline, pyrazole, pyrazoline, 2-pyrazoline, 3-pyrazoline, piperidine, piperazine, indole, indoline, 1H-indazole, the 2-position of isoindole or isoindoline, the 4-position of morpholine, and the 9-position of carbazole or β-carbline. Preferred nitrogen-bonded heterocycles include 1-aziridinepropyl, 1-aziridinebutyl, 1-pyrroleyl, 1-imidazoyl, 1-pyrazolyl, and 1-piperidinyl. Other heteroaryl groups in the sense of this invention are described in Paquette, Leo A., *Principles of Modern Heterocyclic Chemistry* (Benjamin Press, New York, 1968), particularly Chapters 1, 3, 4, 6, 7, and 9; *A Series of Monographs on the Chemistry of Heterocyclic Compounds* (John Wiley International, New York, 1950–present), particularly Volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, CW, and Scriven, E., *Comprehensive Heterocyclic Chemistry* (Pergman Press, 1996); and *Journal of the American Chemical Society* (1960) 82:5566.

[1117] As used herein with respect to substituents, and unless otherwise stated, the terms “monosubstituted,” “disubstituted,” “trisubstituted,” “polysubstituted,” etc., mean as defined herein, a chemical structure in which each part is substituted by one or more substituents, meaning that one or more hydrogen atoms of said part are each independently substituted by a substituent. For example, -C can be polysubstituted by -F. 1-6 Alkyl groups include -CH2F, -CHF2, -CF3, -CH2CF3, CF2CF3, etc. Similarly, -C groups can be multisubstituted by substituents selected independently from -F and -Cl. 1-6 Alkyl groups include -CH2F, -CHF2, -CF3, -CH2CF3, CF2CF3, -CH2Cl, -CHCl2, -CCl3, -CH2CCl3, CCl2CCl3, -CHClF, -CClF2, -CCl2CF3, -CF2CCl3, -CClFCCl2F, etc. The name of any substituent found at more than one site in the compounds of this invention should be chosen independently.

[1118] Unless otherwise stated, the term "solvent" as used herein includes any combination that can be formed from derivatives of the present invention with suitable inorganic solvents (e.g., hydrates) or organic solvents (e.g., but not limited to alcohols, ketones, esters, ethers, nitriles, etc.).

[1119] As used in this article, the term "subject" refers to an animal, including humans, preferably mammals, and most preferably humans, that has been used as a subject of treatment, observation or experimentation.

[1120] As used herein, the term "therapeutic effective amount" refers to the amount of an active compound or agent that elicits a biological or medical response sought by researchers, veterinarians, physicians or other clinicians in an tissue system, animal or human, including the reduction or partial reduction of symptoms of the disease or condition being treated.

[1121] As used herein, the term "composition" is intended to cover products containing a specific amount of a therapeutically effective ingredient, and any product obtained directly or indirectly from a combination of specific amounts of a specific ingredient.

[1122] As used in this article, the terms "antagonist" or "inhibitor" refer to compounds that, depending on the circumstances, produce a functional antagonistic effect on the TRPM3 ion channel, including competitive antagonists, non-competitive antagonists, desensitizing agonists, and partial agonists.

[1123] For the purposes of this invention, the term "TRPM3-regulated" is used to refer to situations influenced by the regulation of TRPM3 ion channels, including states mediated by TRPM3 ion channels.

[1124] As used herein, the term "TRPM3-mediated condition" refers to a condition or disease whose symptoms can be prevented, treated, (partially) alleviated, or improved using a TRPM3 antagonist and consist of pain and inflammatory hypersensitivity symptoms. According to the International Association for the Study of Pain and for the purposes of this invention, pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage. Preferably, the TRPM3-mediated condition is pain, preferably selected from nociceptive pain, inflammatory pain, and neuropathic pain. More preferably, the pain is postoperative pain. For the purposes of this invention, the term "inflammatory hypersensitivity" is used to refer to a condition characterized by one or more inflammatory features (including edema, erythema, hyperthermia, and pain) and / or an excessive physiological or pathophysiological response to one or more types of stimuli (including thermal, mechanical, and / or chemical stimuli).

[1125] The benzofuran derivatives of the present invention have been shown to be antagonists of TRPM3, and therefore the present invention provides such compounds for use as medicines, and more specifically as medicines in the prevention or treatment of TRPM3-mediated conditions in a subject by using a therapeutically effective amount of the benzofuran derivatives of the present invention.

[1126] In a preferred embodiment of the invention, the benzofuran derivative of the invention is the only pharmacologically active compound for therapeutic application. In another preferred embodiment of the invention, the benzofuran derivative of the invention can be used in combination with other therapeutic agents to treat or prevent TRPM3-mediated conditions. Therefore, the invention also relates to the use of compositions comprising:

[1127] - One or more compounds of the formulas and embodiments herein, and

[1128] - One or more other therapeutic or preventive agents for the prevention or treatment of TRPM3-mediated conditions, which are bioactive agents used simultaneously, separately or sequentially in combination formulations.

[1129] Pharmaceutical compositions or combinations according to the invention may contain the benzofuran derivatives of the invention in a wide range of contents, depending on the intended use and expected effect of the formulation. Typically, the content of the benzofuran derivatives of the invention in the combination formulation is in the range of 0.1 to 99.9% by weight, preferably 1 to 99% by weight, and more preferably 5 to 95% by weight.

[1130] Given this fact, when several active ingredients are used in combination, they do not necessarily produce their combined therapeutic effect simultaneously and directly in the mammal to be treated. The corresponding composition may also be in the form of a medical kit or package containing two ingredients in separate but adjacent reservoirs or compartments. In the latter case, each active ingredient can therefore be formulated in a manner suitable for a different route of administration than the others; for example, one may be in the form of an oral or parenteral preparation, while the other may be in the form of an ampoule or aerosol for intravenous injection.

[1131] Those skilled in the art will also recognize that the benzofuran derivatives of the present invention can exist in many different protonated states, depending in particular on the pH and other conditions of their environment. While the structural formulas provided herein describe compounds in only one of several possible protonated states, it should be understood that these structures are illustrative only, and the invention is not limited to any particular protonated state—any and all protonated forms of the compounds are intended to fall within the scope of the invention.

[1132] As used herein, the term "pharmaceutically acceptable salt" refers to a therapeutically active, non-toxic salt form that the compounds of the chemical formulas herein can form. Therefore, the compounds of the present invention optionally comprise salts of the compounds herein, particularly containing, for example, Na. + Li + K + Ca 2+ and Mg 2+ Pharmaceutically acceptable non-toxic salts. Such salts may include those derived by combination of a suitable cation (such as alkali metal and alkaline earth metal ions or ammonium and quaternary ammonium ions) with an acid anionic moiety (typically a carboxylic acid). The benzofuran derivatives of the present invention may carry multiple positive or negative charges. The net charge of the benzofuran derivatives of the present invention may be positive or negative. Any associated counterions are generally determined by the synthetic and / or isolation methods used to obtain the compound. Typical counterions include, but are not limited to, ammonium, sodium, potassium, lithium, halides, acetates, trifluoroacetates, etc., and mixtures thereof. It should be understood that the identity of any associated counterion is not a key feature of the present invention, and the present invention covers compounds associated with any type of counterion. Furthermore, since compounds can exist in a variety of different forms, the present invention is intended to cover not only forms 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 a metal hydroxide with the compounds of the present invention. Examples of metal salts prepared in this manner are those containing Li + Na + and K + Salts. Less soluble metal salts can be precipitated from solutions of more soluble salts by adding a suitable metal compound. Additionally, salts can be formed by the addition of certain organic and inorganic acids to an acid 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., oxalic acid), malonic acid, succinic acid (i.e., succinic acid), maleic acid, fumaric acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, cyclohexylaminosulfonic acid, salicylic acid (i.e., 2-hydroxybenzoic acid), p-aminosalicylic acid, etc. Furthermore, the term also includes solvates, such as hydrates, alcohols, etc., that compounds of the chemical formulas herein and their salts can form. Finally, it should be understood that the compositions herein comprise the benzofuran derivatives of the invention in unionized and zwitterionic forms, and in hydrate form in combination with stoichiometric amounts of water.

[1133] The scope of this invention also includes salts of parent compounds and one or more amino acids, particularly salts of naturally occurring amino acids found as protein components. Amino acids are typically those with side chains having basic or acidic groups (e.g., lysine, arginine, or glutamic acid) or neutral groups (e.g., glycine, serine, threonine, alanine, isoleucine, or leucine).

[1134] The benzofuran derivatives of the present invention also include their physiologically acceptable salts. Examples of physiologically acceptable salts of the benzofuran derivatives of the present invention include salts derived from suitable bases, such as alkali metals (e.g., sodium), alkaline earth metals (e.g., magnesium), ammonium, and Nx4. + (where X is -C) 1-6 Alkyl groups. Physiologically acceptable salts of compounds containing hydrogen atoms or amino groups include salts of organic carboxylic acids (such as acetic acid, benzoic acid, lactic acid, fumaric acid, tartaric acid, maleic acid, malonic acid, malic acid, ethanesulfonic acid, lactobionic acid, and succinic acid); organic sulfonic acids (such as methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, and p-toluenesulfonic acid); and inorganic acids (such as hydrochloric acid, sulfuric acid, phosphoric acid, and aminosulfonic acid). Physiologically acceptable salts of compounds containing hydroxyl groups include salts of the anion of the compound with a suitable cation (such as Na+). + and NX4 + (where X is usually selected independently from -H or -C) 1-4 Combinations of alkyl groups. However, salts 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 this invention.

[1135] Unless otherwise stated, the term “enantiomer” as used herein refers to each individual optically active form of the benzofuran derivative of the present invention having an optical purity or enantiomer excess (determined by standard methods in the art) of at least 80% (i.e. at least 90% of one enantiomer and at most 10% of the other enantiomer), preferably at least 90%, more preferably at least 98%.

[1136] As used herein, the term "isomer" refers to all possible isomers that a compound of the formula herein may have, including tautomers and stereochemical forms, but excluding positional isomers. Generally, the structures shown herein illustrate only one tautomer or resonance form of the compound, but corresponding alternative configurations are also contemplated. Unless otherwise stated, the chemical name of a compound indicates a mixture of all possible stereochemical isomers, containing all diastereomers and enantiomers of the basic molecular structure (since compounds of the formula herein may have at least one chiral center), as well as stereochemically pure or enriched compounds. More specifically, the stereocenter may have an R- or S-configuration, and multiple bonds may have cis or trans configurations.

[1137] The pure isomer form of the compound is defined as an isomer that substantially does not contain other enantiomers or diastereomers of the same basic molecular structure. Specifically, the terms "stereoisomerically pure" or "chirally pure" refer to a compound with a stereoisomeric excess of at least about 80% (i.e., at least 90% of one isomer and at most 10% of other possible isomers), preferably at least 90%, more preferably at least 94%, and most preferably at least 97%. The terms "enantiomerically pure" and "diastereomerically pure" should be understood in a similar manner, taking into account the enantiomeric excess and diastereomeric excess of the mixture, respectively.

[1138] The separation of stereoisomers is accomplished by standard methods known to those skilled in the art. One enantiomer of the benzofuran derivative of the present invention can be separated, for example, by forming diastereomers using an optically active resolving agent (Stereochemistry of Carbon Compounds, (1962) by E.L. Leel, McGraw Hill; Lochmuller, CH, (1975) J. Chromatogr., 113:(3)283-302), substantially free of its opposite enantiomers. The separation of isomers in a mixture can be achieved by any suitable method, including: (1) forming ionic diastereomer salts with a chiral compound and separating by fractional crystallization or other methods; (2) forming diastereomer compounds with a chiral derivatizing agent, separating the diastereomers and converting them into pure enantiomers; or (3) the enantiomers can be directly separated under chiral conditions. In method (1), diastereomer salts can be formed by reacting an enantiomerically pure chiral base (such as strychnine, quinine, ephedrine, strychnine, α-methyl-β-phenylethylamine (amphetamine)) with an asymmetric compound containing an acidic functional group (such as carboxylic acid and sulfonic acid). The diastereomer salts can be separated by fractional crystallization or ion chromatography. To separate the optical isomers of amino compounds, the addition of a chiral carboxylic acid or sulfonic acid (such as camphorsulfonic acid, tartaric acid, mandelic acid, or lactic acid) can lead to the formation of diastereomer salts. Alternatively, by method (2), the substrate to be separated can react with one enantiomer of a chiral compound to form a diastereomer pair (Eliel, E. and Wilen, S. (1994), *Stereochemistry of Organic Compounds*). (Compounds), John Wiley & Sons, Inc., p. 322). Diasteremeric compounds can be formed by reacting an asymmetric compound with an enantiomerically pure chiral derivatizing agent (such as a menthyl derivative), followed by separation of the diastereomer and hydrolysis to produce a free enantiomer-enriched compound. Methods for determining optical purity include preparing a racemic mixture of chiral esters, such as menthyl ester or mosher ester, α-methoxy-α-(trifluoromethyl)phenylacetate (Jacob III. (1982) Journal of Organic Chemistry 47:4165), and analyzing the presence of two trans-restricted diastereomers in the NMR spectrum. According to the method for separating trans-restricted naphthyl-isoquinoline (Hoye, T., WO 96 / 15111), stable diastereomers can be separated and isolated by normal-phase chromatography and reversed-phase chromatography.In method (3), a racemic mixture of two asymmetric enantiomers is separated by chromatography using a chiral stationary phase. Suitable chiral stationary phases are, for example, polysaccharides, particularly cellulose or amylose derivatives. Commercially available polysaccharide-based chiral stationary phases are... CA, OA, OB5, OC5, OD, OF, OG, OJ, and OK, and AD, AS, OP(+), and OT(+). Suitable eluents or mobile phases used in combination with the chiral stationary phase of the polysaccharide are alcohols (such as ethanol, isopropanol, etc.) such as hexane. (Chiral Liquid Chromatography (1989), edited by W.J. Lough, 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, Journal of Chromatography 513:375-378).

[1139] The terms cis and trans are used herein according to Chemical Abstracts nomenclature and include reference to the position of the substituent on the ring moiety. Those skilled in the art can readily determine the absolute stereochemical configuration of compounds of the formulas described herein using known methods such as X-ray diffraction.

[1140] When a compound crystallizes from a solution or slurry, it can crystallize in different spatially arranged lattice sites (a property known as "polymorphism") to form crystals with different crystalline forms, each called a "polymorph". Therefore, the term "polymorph" as used herein refers to the crystalline form of a compound of formula (I), in which the molecules reside in three-dimensional lattice sites. Different polymorphs of a compound of formula (I) can differ from each other in one or more physical properties, such as solubility and dissolution rate, true specific gravity, crystal form, accumulation mode, fluidity, and / or solid-state stability, etc.

[1141] The benzofuran derivatives of the present invention and their physiologically acceptable salts (hereinafter collectively referred to as the active ingredients) may be administered via any route suitable for the condition to be treated, including oral, rectal, nasal, topical (including ocular, buccal, and sublingual), vaginal, and parenteral (including subcutaneous, intramuscular, intranasal, intravenous, intraarterial, intradermal, intrathecal, and epidural). Preferred routes of administration may vary depending on, for example, the recipient's condition.

[1142] The therapeutically effective amount of a compound formulation, particularly for the treatment of TRPM3-mediated conditions in humans and other mammals or animals, is preferably the amount of TRPM3 ion channel inhibition of the compound as defined herein, and corresponds to an amount that ensures a plasma level of 1 μg / ml to 100 mg / ml, optionally 10 mg / ml.

[1143] Appropriate doses of the compounds or compositions of the present invention are applied to treat or prevent TRPM3-mediated conditions in a subject. Depending on the pathological state to be treated and the patient's condition, the effective dose may be divided into several subunits per day or may be administered at intervals of more than one day.

[1144] The present invention further provides (pharmaceutical) compositions comprising one or more benzofuran derivatives of the present invention, more specifically all of formula (I) and other formulas and the embodiments described herein and their more specific aspects or embodiments. Furthermore, the present invention provides compounds or (pharmaceutical) compositions of the present invention for use as medicines, more particularly for the treatment of pain, more specifically having all of formula (I) and other chemical formulas and embodiments described herein and their more specific aspects or embodiments. TRPM3-mediated symptoms are selected from pain and inflammatory hypersensitivity symptoms.

[1145] The benzofuran 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, flow aids, fillers, binders, etc. Aqueous formulations are prepared aseptically and are typically isotonic when intended for delivery by means other than oral administration. Formulations optionally contain excipients, such as those described in the Handbook of Pharmaceutical Excipients (1986).

[1146] Subsequently, the term "pharmaceutically acceptable carrier" as used herein means any material or substance formulated with the active ingredient to facilitate its application or dispersal to the site of treatment, for example by dissolving, dispersing, or diffusing the composition, and / or facilitating its storage, transport, or handling without impairing its effectiveness. A pharmaceutically acceptable carrier can be a solid or liquid or a gas that has been compressed to form a liquid; that is, the compositions of the present invention can suitably be used as concentrates, emulsions, solutions, granules, powders, sprays, aerosols, suspensions, ointments, creams, tablets, pills, or powders.

[1147] Suitable pharmaceutical carriers for the pharmaceutical compositions and formulations thereof are well known to those skilled in the art, and there are no particular limitations on their selection in this invention. They may also include additives such as wetting agents, dispersants, adhesives, binders, emulsifiers, surfactants, solvents, coatings, antibacterial and antifungal agents, isotonic agents, etc., provided that they are consistent with pharmaceutical practice, i.e., that the carrier and additives do not cause permanent harm to mammals. The pharmaceutical compositions of this invention can be prepared in any known manner, for example by uniformly mixing, coating, and / or grinding the active ingredient with a selected carrier material and, where appropriate, other additives (such as surfactants) in one or more steps. They can also be prepared by micronization, for example, to obtain them in the form of microspheres typically having a diameter of about 1 to 10 μm, i.e., for the preparation of microcapsules for controlled or sustained release of the active ingredient.

[1148] While benzofuran derivatives can be administered alone, they are preferably present in the form of pharmaceutical formulations. The veterinary and human formulations of the present invention comprise 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 of compatibility with the other components of the formulation and harmlessness to the recipient. Formulations include those suitable for oral, rectal, nasal, topical (including oral and sublingual), vaginal, or parenteral (including subcutaneous, intramuscular, intravenous, intradermal, intrathecal, and epidural) administration. Formulations can be conveniently present in unit dosage forms and can be prepared by any method well known in the pharmaceutical field. These methods include the step of binding the active ingredient to a carrier constituting one or more auxiliary ingredients. Typically, formulations are prepared by uniformly and tightly binding the active ingredient to a liquid carrier or a finely dispersed solid carrier, or both, and then, if desired, shaping the product.

[1149] The formulations of the present invention suitable for oral administration can exist as discrete units, such as capsules, sachets, or tablets each containing a predetermined amount of the active ingredient; as powders or granules; as solutions or suspensions in aqueous or non-aqueous liquids; or as oil-in-water or water-in-oil emulsions. The active ingredient can also exist as pellets, syrups, or pastes.

[1150] Tablets can be prepared by compression or molding, optionally with one or more excipients. Compressed tablets can be prepared by compressing the active ingredient in a free-flowing form (such as powder or granules) optionally mixed with a binder, lubricant, inert diluent, preservative, surfactant, or dispersant in a suitable machine. Molded tablets can be prepared by molding a mixture of powdered compounds moistened with an inert liquid diluent in a suitable machine. Tablets can optionally be coated or scored and can be formulated to provide a slow or controlled release of the active ingredient therein. For infections of the eyes or other external tissues (e.g., the mouth and skin), the formulation is optionally applied as a topical ointment or cream containing, for example, 0.075 to 20% w / w (including the active ingredient in increments of 0.1% w / w, such as 0.6% w / w, 0.7% w / w, etc.), preferably 0.2 to 15% w / w, and most preferably 0.5 to 10% w / w. When formulated as an ointment, the active ingredient can be used with a paraffin-based or water-miscible ointment base. Alternatively, the active ingredient can be formulated into 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-butanediol, mannitol, sorbitol, glycerin, and polyethylene glycol (including PEG400) and mixtures thereof. Topical formulations may ideally include compounds that enhance the absorption or penetration of the active ingredient through the skin or other affected areas. Examples of such transdermal penetration enhancers include dimethyl sulfoxide and related analogues.

[1151] The oil phase of the emulsion of the present invention can be composed of known ingredients in a known manner. Although this phase may contain only emulsifiers (also known as laxatives), it ideally contains at least one emulsifier with fats or oils, or with a mixture of both fats and oils. Optionally, hydrophilic emulsifiers are included together with lipophilic emulsifiers that act as stabilizers. Both oils and fats are also preferred. The emulsifiers, with or without stabilizers, constitute so-called emulsified waxes, and the waxes, together with the oils and fats, constitute a so-called emulsified ointment matrix, which forms the oily dispersed phase of the ointment formulation.

[1152] The selection of a suitable oil or fat for the formulation is based on achieving the desired cosmetic performance, as the active compound has very low solubility in most oils that may be used in pharmaceutical emulsion formulations. Therefore, the cream should optionally be a non-greasy, non-coloring, and washable product with a suitable consistency to prevent leakage from tubes or other containers. Straight-chain or branched mono- or dialkyl esters, such as diisohexyl adipate, isohexadecanyl stearate, propylene glycol diester of coconut fatty acids, isopropyl myristate, decyl oleate, isopropyl palmitate, butyl stearate, 2-ethylhexyl palmitate, or blends of branched esters known as Crodamol CAP, the latter three being preferred esters, can be used. These can be used alone or in combination, depending on the desired performance. Alternatively, high-melting-point lipids, such as white soft paraffin and / or liquid paraffin or other mineral oils, can be used.

[1153] Formulations suitable for topical ocular application also include eye drops, wherein the active ingredient is dissolved or suspended in a suitable carrier, particularly in an aqueous solvent of the active ingredient. The active ingredient is optionally present in such formulations at a concentration of 0.5% to 20%, advantageously 0.5% to 10%, and particularly about 1.5% w / w. Formulations suitable for topical oral application include lozenges containing the active ingredient in a flavoring matrix (typically sucrose and gum arabic or tragacanth); soft lozenges containing the active ingredient in an inert matrix (such as gelatin and glycerin or sucrose and gum arabic); and mouthwashes containing the active ingredient in a suitable liquid carrier.

[1154] Formulations for rectal administration may exist as suppositories having a suitable matrix comprising, for example, cocoa butter or salicylates. Formulations suitable for nasal administration, wherein the carrier is solid, include coarse powder with a particle size, for example, in the range of 20 to 500 micrometers (including increments of 5 micrometers within the range of 20 to 500 micrometers, such as 30 micrometers, 35 micrometers, etc.), administered by nasal inhalation, i.e., rapid inhalation through the nasal passages from a powder container near the nose. Suitable formulations for administration as, for example, nasal sprays or drops, wherein the carrier is liquid, include aqueous or oily solutions of the active ingredient. Formulations suitable for aerosol administration can be prepared according to conventional methods and can be delivered together with other therapeutic agents.

[1155] Preparations suitable for vaginal application may exist as vaginal suppositories, tampons, creams, gels, pastes, foams or sprays, and in addition to the active ingredient, contain a carrier known in the art as suitable.

[1156] Formulations suitable for parenteral administration include aqueous and non-aqueous sterile injectable solutions, which may contain antioxidants, buffers, antibacterial agents, and solutes that make the formulation isotonic with the blood of the intended recipient; and aqueous and non-aqueous sterile suspensions, which may include suspending agents and thickeners. Formulations may be available in single-dose or multi-dose containers, such as sealed ampoules and vials, and may be stored under lyophilized (freeze-dried) conditions, requiring only the addition of a sterile liquid carrier, such as water for injection, just before use. Temporary injectable solutions and suspensions may be prepared from the aforementioned types of sterile powders, granules, and tablets.

[1157] Preferred unit-dose formulations are those containing the active ingredient at the daily dose or sub-daily dose or an appropriate fraction thereof as described above.

[1158] It should be understood that, in addition to the ingredients specifically mentioned above, the formulations of the present invention may include other agents conventional in the art related to the type of formulation discussed, such as flavoring agents, those suitable for oral administration.

[1159] The benzofuran derivatives of the present invention can be used to provide controlled-release pharmaceutical formulations (“controlled-release formulations”) containing one or more of the benzofuran derivatives of the present invention as active ingredients, wherein the release of the active ingredient can be controlled and modulated to allow for lower frequency of administration or to improve the pharmacokinetic or toxicological characteristics of a given compound of the present invention. Controlled-release formulations suitable for oral administration, comprising discrete units of one or more benzofuran derivatives of the present invention, can be prepared according to conventional methods.

[1160] Another embodiment of the invention relates to various precursor or "prodrug" forms of the benzofuran derivatives of the invention. It may be necessary to formulate the benzofuran derivatives of the invention into a form of chemicals that themselves do not possess significant biological activity, but when delivered to animals, mammals, or humans, they undergo a chemical reaction catalyzed by normal bodily functions, particularly enzymes present in the stomach or serum, which has the effect of releasing compounds as defined herein. Therefore, the term "prodrug" refers to these substances that are converted into an active pharmaceutical ingredient in vivo.

[1161] The benzofuran derivative prodrugs of the present invention can have any form suitable to the formulation user; for example, esters are a common, non-limiting prodrug form. However, in this case, the prodrug may necessarily be present in a form in which the covalent bonds are cleaved by the action of an enzyme present at the target locus. For example, the C-C covalent bonds can be selectively cleaved by one or more enzymes at the target locus; therefore, prodrugs in forms other than readily hydrolyzable precursors, especially esters, amides, etc., can be used. The counterparts of the active pharmaceutical ingredient in the prodrug can have different structures, such as amino acid or peptide structures, alkyl chains, sugar moieties, and other structures known in the art.

[1162] For the purposes of this invention, the term "therapeutically suitable prodrug" is defined herein as "a compound modified in vivo to a therapeutically active form when in contact with tissues of an animal, mammal, or human to which a prodrug has been administered, whether by a single biotransformation or by multiple biotransformations, without undue toxicity, irritation, or allergic reaction, and achieving the desired therapeutic outcome."

[1163] More specifically, the term "prodrug" as used herein refers to an inactive or significantly reduced-activity derivative of a compound represented by the structural formula described herein, which undergoes spontaneous or enzymatic conversion in vivo to release the pharmacologically active form of the compound. For a comprehensive review, please refer to Rautio J. et al. ("Prodrugs: design and clinical applications," *Nature Reviews Drug Discovery*, 2008, doi:10.1038 / nrd2468).

[1164] Representative benzofuran derivatives of the present invention can be synthesized according to the general synthetic methods described below and illustrated in the embodiments below. Since the embodiments are exemplary, the invention should not be construed as being limited to the specific chemical reactions and conditions described in the embodiments and examples. Various starting materials used in the embodiments are commercially available or can be prepared by methods well known to those skilled in the art. Variables are as defined herein and are within the skill of those skilled in the art.

[1165] Preferred embodiments of the present invention are summarized below as clauses 1 to 51:

[1166] 1. A compound of formula (I), its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs.

[1167]

[1168] Preferred are compounds of formula (I) used for the treatment of pain, their stereoisomers, physiologically acceptable salts, solvates and / or polymorphs;

[1169] in

[1170] R 1 This represents -F, -Cl, -Br, -I, -CN, and -R. W -OR W -OC(=O)R W -NR W R X -NR W C(=O)R X-SR W -S(=O)R W -S(=O)2R W -C(=O)R W -C(=O)OR W or -C(=O)NR W R X ;

[1171] Q means -OR 2 or -NR 3 R 4 ;

[1172] R 2 Indicates -R Y ;

[1173] R 3 Indicates -OH or -R Y ;

[1174] R 4 Indicates -R Y or -S(=O)2R Y ;

[1175] Or R 3 and R 4 Together they form saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted 4, 5, 6, 7 or 8-membered heterocycles containing 1 to 3 heteroatoms selected from N, O and S.

[1176] T represents -O- and U represents -CR 5 R 5 '-; or T represents -CR 5 R 5 '-and U represents -O-;

[1177] R 5 and R 5 'Represented independently of each other - R Y ;

[1178] R 6 R 7 and R 8 The following can be represented independently: -F, -Cl, -Br, -I, -CN, -NO2, -SF5, -R W -OR W -OC(=O)R W -NR W R X -NR W C(=O)R X -SR W -S(=O)R W -S(=O)2RW -C(=O)R W -C(=O)OR W or -C(=O)NR W R X ;

[1179] V represents a saturated or unsaturated 3- to 14-membered heterocyclic alkyl group; or a 5- to 14-membered heteroaryl group; in each case, it is unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from -F, -Cl, -Br, -I, -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 ;

[1180] in

[1181] R W and R X Represented independently of each other in each case.

[1182] -H;

[1183] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[1184] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[1185] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl group is optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[1186] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[1187] R Y and R Z Represented independently of each other in each case.

[1188] -H;

[1189] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[1190] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[1191] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[1192] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[1193] Unsubstituted, monosubstituted, or polysubstituted 6- to 14-membered aryl groups; wherein the 6- to 14-membered aryl groups are optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[1194] Unsubstituted, monosubstituted, or polysubstituted 5- to 14-membered heteroaryl groups; wherein the 5- to 14-membered heteroaryl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted;

[1195] Or R Y and R Z Together they form saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted 4, 5, 6, 7 or 8-membered heterocycles containing 1 to 3 heteroatoms selected from N, O and S.

[1196] Furthermore, "mono- or poly-substituted" in each case independently indicates substitution by one or more substituents, which are independently selected from -F, -Cl, -Br, -I, -CN, and -C. 1-6 Alkyl, -CF3, -CF2H, -CFH2, -CF2Cl, -CFCl2, -C1-6 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 group, -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 Alkylenes -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 1-6Alkylene-OC(=O)-C 1-6 Alkyl group, -OC (=O)-OC 1-6 Alkyl, -C 1-6 Alkylene-OC(=O)-OC 1-6 Alkyl group, -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 Alkylenes -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 group 2, -NH2, -NO, -NO2, -C 1-6 Alkylene -NH2, -NH(C 1-6 Alkyl), -N (3 to 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 group, -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) 1-6Alkyl), -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 Alkylenes -NH-S(=O)2OH, -NH-S(=O)2-C 1-6 Alkyl, -C 1-6 Alkylene-NH-S(=O)2-C 1-6 Alkyl group, -NH-S(=O)2-OC 1-6 Alkyl, -C 1-6 Alkylene-NH-S(=O)2-OC 1-6 Alkyl group, -NH-S(=O)2-NH2, -C 1-6 Alkylenes -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(C1-6 Alkyl)2, -N(C 1-6 alkyl)-S(=O)2-OH, -C 1-6 Alkylene-N(C) 1-6 alkyl)-S(=O)2-OH, -N(C 1-6 alkyl)-S(=O)2-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 alkyl)-S(=O)2-C 1-6 Alkyl, -N(C) 1-6 alkyl)-S(=O)2-OC 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 alkyl)-S(=O)2-OC 1-6 Alkyl, -N(C) 1-6 Alkyl)-S(=O)2-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 group 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 group, -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 Alkylenes -S(=O)2-OH, -S(=O)2-OC 1-6 Alkyl, -C 1-6 Alkylene-S(=O)2-OC 1-6 Alkyl group, -S(=O)2-NH2, -C 1-6Alkylene -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 to 14-membered cycloalkyl, -C 1-6 Alkylene (3- to 14-membered cycloalkyl), 3- to 14-membered heterocycloalkyl, -C 1-6 alkylene-(3 to 14-membered heterocyclic alkyl), -phenyl, -C 1-6 alkylene-phenyl, 5 to 14-membered heteroaryl, -C 1-6 Alkylene-(5 to 14-membered heteroaryl), -O-(3 to 14-membered cycloalkyl), -O-(3 to 14-membered heterocycloalkyl), -O-phenyl, -O-(5 to 14-membered heteroaryl), -C(=O)-(3 to 14-membered cycloalkyl), -C(=O)-(3 to 14-membered heterocycloalkyl), -C(=O)-phenyl, -C(=O)-(5 to 14-membered heteroaryl), -S(=O)2-(3 to 14-membered cycloalkyl), -S(=O)2-(3 to 14-membered heterocycloalkyl), -S(=O)2-phenyl, -S(=O)2-(5 to 14-membered heteroaryl).

[1197] 2. The compound itself or for the purpose described in Clause 1, wherein T represents -O- and U represents -CR 5 R 5 '-.

[1198] 3. The compound itself as described in Clause 1 or for the purpose described in Clause 1, wherein T represents -CR 5 R 5 '-and U represents -O-.

[1199] 4. The compound itself according to any one of clauses 1 to 3, or for use according to any one of clauses 1 to 3, wherein Q represents -NR. 3 R 4 .

[1200] 5. The compound itself according to any one of clauses 1 to 3, or for use according to any one of clauses 1 to 3, wherein Q represents -OR 2 .

[1201] 6. The compound for itself or for use in accordance with any one of the clauses 1 to 5, wherein V represents a 5- to 14-membered heteroaryl group that is unsubstituted, monosubstituted, or polysubstituted, the substituents being independently selected from -F, -Cl, -Br, -I, -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 .

[1202] 7. The compound described in Clause 6, either on its own or for the purpose described in Clause 6, wherein the 5 to 14 heteroaryl group is not a benzofuran.

[1203] 8. The compound itself or for the purpose described in Clause 6 or 7, wherein the 5 to 14 heteroaryl group is selected from benzimidazole, benzisoxazole, benzoxazole, benzom-dioxane, benzofuran, benzothiadiazole, benzothiazolium, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazonium, imidazole, imidazopyridine, indazole, indole, inazine, isobenzofuran, isoindole, isoquinoline, isothiazole, isoxazole, naphthidine, oxadiazole Oxazole, hydroxyindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazolium, thiadiazole, thiazole, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine; in each case, they are unsubstituted, monosubstituted, or polysubstituted, wherein the substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[1204] 9. The compound for its own use or for any of the claims 6 to 8, wherein the 5 to 14 heteroaryl groups are selected from the group consisting of: furan, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, triazole, pyridine, isoquinoline, benzothiazole, pyridazine, pyrimidine, imidazopyridine; and in each case, unsubstituted, monosubstituted, or polysubstituted, wherein the substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[1205] 10. The compound for itself or for use in accordance with any one of clauses 6 to 9, wherein the 5 to 14 heteroaryl groups are selected from the group consisting of: furan-2-yl, furan-3-yl, thiophene-2-yl, thiophene-3-yl, pyrazol-5-yl, oxazol-5-yl, isoxazol-4-yl, thiazolyl-2-yl, thiazolyl-5-yl, 1,2,4-triazol-3-yl, 1,2,3-triazol-4-yl, pyrazol-5-yl The substituents are 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 1-isoquinoline, 5-isoquinoline, 2-benzo[d]thiazolyl, 3-pyridazinyl, 5-pyrimidinyl, and 6-imidazo[1,2-a]pyridinyl; in each case they are unsubstituted, monosubstituted, or polysubstituted, wherein the substituents are independently selected from -F, -Cl, -Br, -I, -CN, -NO, -NO2, =O, =S, -SF5, and -R. Y -OR Y -OC(=O)R Y -NR Y R Z -NR Y C(=O)R Z -SRY -S(=O)R Y -S(=O)2R Y -C(=O)R Y -C(=O)OR Y or -C(=O)NR Y R Z .

[1206] 11. The compound for itself or for use in accordance with any one of the provisions of clauses 1 to 5, wherein V represents a 3- to 14-membered heterocyclic alkyl group that is saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, wherein the substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[1207] 12. The compound itself or for the purpose described in Clause 11, wherein the 3 to 14-membered heterocyclic alkyl group is selected from aziridine, 1,4-oxazacycloheptane, aziridine, aziridine, aziridine propane, aziridine octane, diazacycloheptane, dioxane, dioxane, dioxane, dithiazide, dithiopentane, imidazoline, isothiazolidine, isoxazolidine, morpholine, oxazolidine, hexane oxide, oxazacyclobutane, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, thiohexacyclobutane, thiohexacyclopropane, thiohexacyclopentane, thiomorpholine, indoline, benzo[a] Dihydrofuran, dihydrobenzothiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, and octahydropyrrolo[1,2-a]pyrrazine; in each case, the substituents are unsubstituted, monosubstituted, or polysubstituted, wherein the substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[1208] 13. The compound itself or for use as described in Clause 11 or 12, wherein the 3- to 14-membered heterocyclic alkyl group is tetrahydropyran or pyrrolidine; in each case, it is unsubstituted, monosubstituted, or polysubstituted, wherein the substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[1209] 14. The compound for itself or for use in any one of the provisions of 11 to 13, wherein the 3- to 14-membered heterocyclic alkyl group is tetrahydropyran-4-yl or pyrrolidine-3-yl; and in each case is unsubstituted, monosubstituted, or polysubstituted, wherein the substituents are independently selected from -F, -Cl, -Br, -I, -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 .

[1210] 15. The compound itself according to any one of the preceding clauses, or for use according to any one of the preceding clauses, wherein V is unsubstituted, monosubstituted, or polysubstituted, the substituents being independently selected from the group consisting of:

[1211] -F, -Cl, -Br, -I, -CN, -C(=O)OH, -NH2, -NO2, -OH, =O, -SF5;

[1212] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 alkyl;

[1213] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 alkyl;

[1214] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -NHC 1-6 alkyl;

[1215] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C)1-6 Alkyl)2;

[1216] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 alkyl;

[1217] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)2-C 1-6 alkyl;

[1218] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl group is optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[1219] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, and the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[1220] 16. The compound itself according to any one of the preceding clauses, or for use according to any one of the preceding clauses, wherein V is unsubstituted, monosubstituted, or polysubstituted, the substituents being independently selected from the group consisting of:

[1221] -OH, -F, -Cl, -Br, -I, -SH, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -CN, -NO2, -C(=O)OH, -NH2, -N(CH3)2, -cyclopropyl or -O-cyclopropyl; preferably, selected from -OH, -F, -Cl, -Br, -I, -SH, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -CN, -NO2, -C(=O)OH, -NH2 or -N(CH3)2;

[1222] -C 1-6 Alkyl groups, which are saturated or unsaturated, unsubstituted, mono- or poly-substituted, wherein the substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2, -C(=O)NH2 and -cyclopropyl; preferably, selected from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[1223] -C 1-6 Heteroalkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, with the substituents independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[1224] -OC 1-6 Alkyl groups, which are unsubstituted, monosubstituted, or polysubstituted, wherein the substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[1225] -O(C=O)C 1-6 Alkyl groups, which are unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[1226] -C(=O)OC 1-6 Alkyl groups, which are unsubstituted, monosubstituted, or polysubstituted, and these substituents are independently selected from the group consisting of: -F, -Cl, -Br, -I, -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[1227] 3 to 14-membered cycloalkyl groups selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl; in each case unsubstituted, monosubstituted, or polysubstituted, with substituents independently selected from the group consisting of -F, -Cl, -Br, -I, and -C. 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2;

[1228] 3 to 14-membered heterocyclic alkyl groups selected from the group consisting of: aziridine, 1,4-oxazacycloheptanidine, aziridine, aziridine, aziridine, aziridine, aziridine, aziridine, aziridine, diazacycloheptanidine, dioxacyclohexane, dioxacyclohexane, dithiazoline, dithiopentane, imidazoline, isothiazolidine, isoxazolidine, morpholine, oxazolidine, hexane oxide, oxazacycloheptanidine, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, thioheptanidine, thioheptanidine, thioheptanidine, thioheptanidine, thioheptanidine, thiomorpholine, indoline, benzodihydrofuran, dihydrobenzene Thiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, and octahydropyrrolo[1,2-a]pyrrazine, wherein the groups are in each case unsubstituted, monosubstituted, or polysubstituted by substituents selected independently from the group consisting of: -F, -Cl, -Br, -I, -C 1-6 Alkyl, C 2-6 alkenyl, -C 2-6 Alkyne, -OH, =O, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2, C(=O)CHF2 and -C(=O)NH2.

[1229] 17. The compound itself or for use in accordance with any one of the preceding clauses, wherein V is unsubstituted, monosubstituted, or polysubstituted, the substituents being 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-NHC(=O)-OC 1-6 Alkyl group, -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, -azacyclobutane, -C 1-6alkylene-O-tetrahydropyran or -C 1-6 Alkyl-substituted piperazine; or indicating unsubstituted, monosubstituted or polysubstituted oxobutyric.

[1230] 18. The compound itself or for use in accordance with any one of the preceding clauses, wherein V is

[1231] (i) Unreplaced;

[1232] (ii) Monosubstituted;

[1233] (iii) Disubstituted;

[1234] (iv) Trisubstituted; or

[1235] (v) Tetrasubstituted.

[1236] 19. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 1 express

[1237] -H, -F, -Cl, -Br, -I;

[1238] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 Alkyl; saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 alkyl;

[1239] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)C 1-6 alkyl;

[1240] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 alkyl;

[1241] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)NHC 1-6 alkyl;

[1242] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)N(C 1-6 Alkyl)2;

[1243] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)C 1-6 alkyl;

[1244] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)2-C 1-6 alkyl;

[1245] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups; or

[1246] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[1247] 20. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 1 Representing -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 groups: -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 group, -C(=O)OC 1-6 Alkyl group, -C(=O)NHC 1-6 Alkyl, -C(=O)N(C) 1-6 Alkyl)2、-S(=O)-C 1-6 Alkyl group, -S(=O)2-C 1-6 Alkyl, -OC 1-6 Alkyl, unsubstituted cyclopropyl, unsubstituted cyclobutyl, unsubstituted cyclopentyl, or unsubstituted cyclohexyl.

[1248] 21. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 1 Indicates -H, -C 1-6 Alkyl, -C 1-6 Alkylene-OC 1-6Alkyl, -CH2F, -CHF2, -CF3, unsubstituted -cyclopentyl or unsubstituted -cyclopropyl; preferably, wherein R 1 Indicates -H, -C 1-6 Alkyl, -C 1-6 Alkylene-OC 1-6 Alkyl, -CH2F, -CHF2, -CF3 or unsubstituted -cyclopentyl.

[1249] 22. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 1 Represents -CH2F, -CHF2, -CH3, or unsubstituted -cyclopropyl; preferably, wherein R 1 It represents -CH2F, -CHF2, or -CH3.

[1250] 23. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 2 express

[1251] -H;

[1252] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[1253] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[1254] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl group is optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted; or

[1255] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, and the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[1256] 24. The compound itself or for use in accordance with any one of the preceding clauses, 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 groups: -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.

[1257] 25. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 2 Indicates -H or -C 1-6 alkyl.

[1258] 26. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 3 express

[1259] -H;

[1260] -OH;

[1261] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups; or

[1262] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups.

[1263] 27. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 3 Represents -H, -OH, -C 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH(C) 1-6 Alkyl), -C 1-6 Alkylene-N(C) 1-6 Alkyl groups: -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 1-6Alkylene-CF3 or -C 1-6 Alkylene-N(C) 1-6 alkyl)-C 1-6 Alkylene-CF3.

[1264] 28. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 3 Indicates -H, -OH or -C 1-6 Alkyl, saturated, unsubstituted, or monosubstituted with -OH.

[1265] 29. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 4 express

[1266] -H;

[1267] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)C 1-6 alkyl;

[1268] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -S(=O)2-C 1-6 alkyl;

[1269] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[1270] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[1271] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[1272] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered heterocyclic alkyl groups; wherein the 3- to 14-membered heterocyclic alkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted;

[1273] Unsubstituted, monosubstituted, or polysubstituted 6- to 14-membered aryl groups; wherein the 6- to 14-membered aryl groups are optionally linked by a -C1-C6 alkylene group or a -C1-C6 heteroalkylene group, wherein the alkylene group or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted; or

[1274] Unsubstituted, monosubstituted, or polysubstituted 5- to 14-membered heteroaryl groups; wherein the 5- to 14-membered heteroaryl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted, or polysubstituted.

[1275] 30. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 4 express

[1276] -S(=O)2C 1-6 Alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, with the substituents independently chosen from the group consisting of: -F, -Cl, -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[1277] -S(=O)2 (3 to 14-membered cycloalkyl), wherein the 3 to 14-membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, wherein the group is, in each case, saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, and the substituents are independently selected from the group consisting of -F, -Cl, and -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[1278] -C 1-6 Alkyl groups, which are saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted, with the substituents independently chosen from the group consisting of: -F, -Cl, -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[1279] 3 to 14-membered cycloalkyl or -C 1-6 Alkylene (3 to 14-membered cycloalkyl), wherein -C 1-6 The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 3- to 14-membered cycloalkyl group is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, wherein the group is saturated or unsaturated in each case, and wherein the group is unsubstituted, monosubstituted, or polysubstituted by substituents, which are independently selected from the group consisting of -F, -Cl, and -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[1280] 3 to 14-membered heterocyclic alkyl groups or -C 1-6 Alkylene (3 to 14-membered heterocyclic alkyl), wherein -C 1-6 The alkylene group is either unsubstituted or monosubstituted with -OH, wherein the 3 to 14-membered heterocyclic alkyl group is selected from the group consisting of: aziridine, 1,4-oxazacycloheptane, aziridine, aziridine, aziridine, aziridine propane, aziridine octane, diazacycloheptane, dioxacyclohexane, dioxapentane, dithiazide, dithiopentane, imidazoline, isothiazidine, isoxazidine, morpholine, oxazidine, hexane oxide, oxacyclobutane, ethylene oxide, piperazine, piperidine, pyrazolidine, pyrrolidine, quinine ring, tetrahydrofuran, tetrahydropyran, tetrahydrothiopyran, thiazoline, thiohexacyclobutane, thiohexacyclopropane, thiohexacyclopentane. Thiomorpholine, indoline, benzodihydrofuran, dihydrobenzothiophene, 1,1-dioxothiocyclohexane, 2-azaspiro[3.3]heptane, 2-oxaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 8-azabicyclo[3.2.1]octane, 9-azabicyclo[3.3.1]nonane, hexahydro-1H-pyrrolizine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, and octahydropyrrolo[1,2-a]pyrazine; in each case unsubstituted, monosubstituted, or polysubstituted by substituents selected independently from the group consisting of: -F, -Cl, -C 1-6Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[1281] Unsubstituted, mono- or poly-substituted -phenyl groups, wherein the substituents are independently selected from the group consisting of: -F, -Cl, -CN, -C. 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C) 1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which are saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl;

[1282] 5 to 14 heteroaryl or -C 1-6 alkylene-(5 to 14-membered heteroaryl), wherein -C 1-6 The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 5 to 14-membered heteroaryl group is selected from the group consisting of: benzimidazole, benzisoxazole, benzoxazole, benzo-m-dioxane, benzofuran, benzothiadiazole, benzothiazol, benzothiophene, carbazole, zoline, dibenzofuran, furan, furazon, imidazole, imidazopyridine, indazole, indole, inazine, isobenzofuran, isoindole, isoquinoline, isothiazol, iso... Oxazole, naphthidine, oxadiazole, oxazole, hydroxyindole, phthalazine, purine, pyrazine, pyrazole, pyridazine, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, tetrazolium, thiadiazole, thiazolium, thiophene, triazine, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine; in each case unsubstituted, monosubstituted, or polysubstituted, the substituents being independently selected from the group consisting of: -F, -Cl, -CN, -C 1-6 Alkyl, -C 1-6 Alkylenes -CF3, -OH, =O, -OC 1-6 Alkyl, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -NHC 1-6 Alkyl, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 Alkyl, -N(C)1-6 Alkyl)C(=O)OC 1-6 Alkyl, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6 Alkyl), -C(=O)N(C 1-6 Alkyl)2、-S(=O)2C 1-6 Alkyl, -phenyl, -C 1-6 Alkylene-phenyl, 3 to 14-membered heterocyclic alkyl, which is saturated or unsaturated and unsubstituted; and unsubstituted 5 to 14-membered heteroaryl.

[1283] 31. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 4 express

[1284] -H;

[1285] Saturated, unsubstituted, mono- or poly-substituted -S(=O)2C 1-6 alkyl;

[1286] Saturated, unsubstituted -S(=O)2 (3 to 14-membered cycloalkyl);

[1287] Saturated, unsubstituted, monosubstituted, or disubstituted -C 1-6 Alkyl groups, wherein the substituents are independently selected from the group consisting of: -OH, -OC 1-6 Alkyl, -N(C) 1-6 Alkyl)2, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkyl groups, unsubstituted phenyl groups;

[1288] 3 to 14-membered cycloalkyl or -C 1-6 Alkylene (3 to 14-membered cycloalkyl), wherein -C 1-6The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 3 to 14-membered cycloalkyl group is saturated, unsubstituted, monosubstituted, or disubstituted, and these substituents are independently selected from the group consisting of: -C 1-6 Alkyl, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-NH-C 1-6 Alkylene-CF3, -C 1-6 alkylene -OH, -C 1-6 Alkylene-NHC(=O)OC 1-6 Alkyl, -OH, -OC 1-6 Alkyl, -NH2, -N(C) 1-6 Alkyl)2、-NHC(=O)OC 1-6 alkyl;

[1289] 3 to 14-membered heterocyclic alkyl groups or -C 1-6 Alkylene (3 to 14-membered heterocyclic alkyl), wherein -C 1-6 The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 3 to 14-membered heterocyclic alkyl group is selected in each case from aziridine, 1,4-oxazacycloheptanane, pyrrolidine, piperidine, aziridine, diazacycloheptanane, tetrahydrofuran, tetrahydropyran, oxazacyclobutane, morpholine, piperazine, hexahydrocyclopentadieno[c]pyrrole, octahydrocyclopentadieno[c]pyrrole, octahydropyrrolo[1,2-a]pyrazine, 8-azabicyclo[3]pyrrole, and 1,4-oxazacycloheptanane. .2.1] Octane, 9-azabicyclo[3.3.1]nonane, quinine ring, hexahydro-1H-pyrrolizine, 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, 7-azaspiro[3.5]nonane, 1,1-dioxothiacyclohexane, wherein the groups are in each case unsubstituted, monosubstituted, or polysubstituted by substituents, which are independently selected from the group consisting of: -F, -OH, =O, -C 1-6 Alkyl, -C 1-6 Alkylene-CF3, -C 1-6 alkylene -OH, -C 1-6 Alkylene-OC 1-6 Alkyl, -NH2, -N(C) 1-6 Alkyl)2, -C 1-6 Alkylene -NH2, -C 1-6 Alkylene-N(C) 1-6 Alkyl)2、-C(=O)-C 1-6 Alkyl, -C(=O)OH, -C(=O)OC 1-6 Alkyl group, -C(=O)OC 1-6 Alkylenes -CF3, -C(=O)NH2, -C(=O)NH(C 1-6Alkyl group), -S(=O)2C 1-6 Alkyl, oxetane butyl, pyrimidinyl, -C 1-6 alkylene-phenyl;

[1290] Unsubstituted -phenyl;

[1291] 5 to 14 heteroaryl or -C 1-6 alkylene-(5 to 14-membered heteroaryl), wherein -C 1-6 The alkylene group is unsubstituted or monosubstituted with -OH, wherein the 5 to 14-membered heteroaryl group is selected from the group consisting of pyridine, pyridazine, pyrazine, pyrazole, isoxazole, triazole, and [1,2,4]triazolo[4,3-a]pyrimidine in each case, and the group is unsubstituted and monosubstituted or disubstituted by substituents selected independently from the group consisting of -C 1-6 Alkyl group, -OH group.

[1292] 32. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 3 and R 4 Together they form saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted 5- or 6-membered heterocycles containing one or two heteroatoms selected from N, O and S.

[1293] 33. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 3 and R 4 Together they form heterocycles selected from the group consisting of: pyrrolidine, piperidine, morpholine, and piperazine, wherein in each case the heterocycle is unsubstituted and mono- or polysubstituted by substituents selected independently from the group consisting of: -C 1-6 Alkyl groups, -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 group, -NHC(=O)OC 1-6 Alkyl, unsubstituted pyridyl, and unsubstituted or -C 1-6 Alkyl monosubstituted 1,2,4-oxadiazole.

[1294] 34. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 3 and R 4 Together

[1295] The pyrrolidine ring is either unsubstituted or monosubstituted with -N(CH3)2;

[1296] Piperidine ring, which is either unsubstituted or monosubstituted with a substituent selected from the group consisting of: -C 1-6 Alkyl groups, -NH2, -N(CH3)2, -C(=O)NH-C 1-6 Alkyl group, -C(=O)OC 1-6 Alkyl group, -NHC(=O)OC 1-6 Alkyl and unsubstituted or -C 1-6 Alkyl monosubstituted 1,2,4-oxadiazole;

[1297] The morpholine ring is unsubstituted; or

[1298] Piperazine ring, which is either unsubstituted or N-substituted with a substituent selected from the group consisting of: -C 1-6 Alkyl and unsubstituted pyridyl groups.

[1299] 35. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 5 and R 5 'represented independently of each other'

[1300] -H;

[1301] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 alkyl groups;

[1302] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C1-C6 heteroalkyl groups;

[1303] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted 3- to 14-membered cycloalkyl groups; wherein the 3- to 14-membered cycloalkyl groups are optionally linked by -C1-C6 alkylene- or -C1-C6 heteroalkylene-, wherein the alkylene or heteroalkylene group is in each case saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted.

[1304] 36. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 5 and R 5 'Independently represent -H, -C1-C6 alkyl or -C1-C6 alkylene-N(C1-C6 alkyl)2.

[1305] 37. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 5 and R 5 At least one of the characters does not represent -H.

[1306] 38. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 6 R 7 and R 8 Representing each other independently

[1307] -H;

[1308] -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2;

[1309] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 alkyl;

[1310] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC 1-6 alkyl;

[1311] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -NHC 1-6 alkyl;

[1312] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -N(C) 1-6 Alkyl)2;

[1313] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C(=O)OC 1-6 alkyl;

[1314] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -OC (=O)C 1-6 alkyl;

[1315] Saturated or unsaturated, unsubstituted, monosubstituted or polysubstituted -C 1-6 Heteroalkyl groups.

[1316] 39. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 6 R 7 and R 8 Representing each other independently

[1317] -H, -F, -Cl, -Br, -I, -OH, -SH, -SF5, -CN, -NO2, -C(=O)OH, -NH2,

[1318] -C 1-6 Alkyl, -CF3, -CHF2, -CH2F,

[1319] -OC 1-6 Alkyl, -OCF3, -OCHF2, -OCH2F,

[1320] -NHC 1-6 Alkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;

[1321] -N(C 1-6 Alkyl)2, which is unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;

[1322] -C(=O)OC 1-6 Alkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2;

[1323] -OC(=O)C 1-6 Alkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2; or

[1324] -C 1-6 Heteroalkyl groups, which are unsubstituted or substituted by one or more substituents independently selected from the following: -OH, =O, -F, -Cl, -Br, -I, -SH, =S, -CN, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, SF5, -NO2, -C(=O)OH, -NH2 and -C(=O)NH2.

[1325] 40. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 6 It represents -H, -F, -Cl, -CN or -C1-C6 alkyl.

[1326] 41. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 6 It does not represent -H.

[1327] 42. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 7 It represents -H, -F, -Cl, -CN or -C1-C6 alkyl.

[1328] 43. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 7 It does not represent -H.

[1329] 44. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 8 It represents -H, -F, -Cl, -CN or -C1-C6 alkyl.

[1330] 45. The compound itself or for use in accordance with any one of the preceding clauses, wherein R 8 It does not represent -H.

[1331] 46. ​​The compound itself or for use in accordance with any one of the preceding clauses, wherein

[1332] (i)R 6 R 7 and R 8 Each represents -H; or

[1333] (ii)R 6 R 7 and R 8 The two characters in the text represent -H and R. 6 R 7 and R 8 Another representation of -F, -Cl, -CN, or -CH3; or

[1334] (iii)R 6 R 7 and R 8 One of them represents -H and R 6 R 7 and R 8 Another independent expression in the expression is -F, -Cl, -CN, or -CH3.

[1335] 47. The compound itself, or for use in accordance with any one of the preceding clauses, is selected from the group consisting of: cpd 001 to cpd 207 as described above and their physiologically acceptable salts.

[1336] 48. The compound itself or for use in accordance with any of the preceding clauses, wherein the pain is selected from nociceptive pain, inflammatory pain and neuropathic pain.

[1337] 49. The compound itself or for use in accordance with any of the preceding clauses, wherein the pain is postoperative pain.

[1338] 50. The compound of formula (I) according to any one of the preceding clauses, its stereoisomers, physiologically acceptable salts, solvates and / or polymorphs, wherein

[1339] (a) Q means -OR 2 ;as well as

[1340] (a-1)R 1 Indicates -CH2F, -CHF2, or -CF3; and / or

[1341] (a-2)R 5 and R 5 At least one of ' does not represent -H; and / or

[1342] (a-3)R 6 Not indicating -H; and / or

[1343] (a-4)R 8 It does not represent -H;

[1344] or

[1345] (b) Q represents -NR 3 R 4 ;as well as

[1346] (b-1) The condition is the exclusion of the following compounds and their salts.

[1347]

[1348] and / or

[1349] (b-2)R 1 It represents -CH2F, -CHF2 or -CF3, -CN, -propyl or -cyclopropyl; and / or

[1350] (b-3)R 5 and R 5At least one of ' does not represent -H; and / or

[1351] (b-4)R 3 It represents -H.

[1352] 51. A pharmaceutical composition or drug comprising a compound according to any one of the preceding clauses.

[1353] Example

[1354] The following examples are provided to illustrate the invention and should not be construed as limiting the scope of the invention.

[1355] Representative compounds of the present invention can be synthesized according to the general synthetic methods described below and illustrated in the following embodiments. Since the embodiments are exemplary, the invention should not be construed as being limited to the specific chemical reactions and conditions described in the embodiments and examples. Various starting materials used in the embodiments are commercially available or can be prepared by methods well known to those skilled in the art. Variables are as defined herein and are within the skill of those skilled in the art.

[1356] In this specification, the abbreviations used particularly in the schemes and examples are as follows: ACN - acetonitrile, AcOH - acetic acid, ADDP-1,1'-(azodicarbonyl)piperidine, aq. - aqueous, AIBN - azobisisobutyronitrile, CAN - cerium ammonium nitrate, COMU - (1-cyano-2-ethoxy-2-oxoethyleneaminooxy)dimethylamino-morpholino-carbomonium, hexafluorophosphate, DABCO-1,4-diazabicyclo[2.2.2]octyl Alkane, DAST-diethylaminosulfur trifluoride, DBU-1,8-diazabicyclo[5.4.0]undec-7-ene, DCC-N,N'-dicyclohexylcarbodiimide, DCM-dichloromethane, DEAD-diethyl azodicarboxylate, DIA-diastereomer, DIAD-diisopropyl azodicarboxylate, DEA-diethylamine, DIPEA-diisopropylethylamine, DME-1,2-dimethoxyethane, DMF-N,N-dimethylmethane Amide, DMSO (dimethyl sulfoxide), DTBAD (tert-butyl azodicarboxylate), EDCI or EDC (1-ethyl-3-(3-dimethylaminopropyl)carbodiimide), En (enantiomer), Et2O (diethyl ether), EtOH (ethanol), EtOAc (ethyl acetate), Eq. (equivalent), FA (formic acid), FCC (fast column chromatography), h (hours), HATU-O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyl Urea hexafluorophosphate, HPLC, IPA, LAH, LG, MeOH, MgSO4, Na2SO4, NBS, N-bromosuccinimide, NMP, Pd(PPh3)4-tetra-(triphenylphosphine)-palladium(O), Pd2(dba)3-tris(dibenzylacetone)dipalladium, Pet ether - petroleum ether, PPh3 - triphenylphosphine, PS-DIEA - polystyrene-supported diisopropylethylamine, PS-PPh3 - polystyrene-supported triphenylphosphine, PyBop - benzotriazol-1-yl-oxotripyrrolidine hexafluorophosphate, PTSA - p-toluenesulfonic acid, RF - front ratio, RM - reaction mixture, RP - reversed 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

[1357] Compounds of interest having structures according to general formula (A) and all other formulas and embodiments described herein can be prepared as outlined in General Chemical Scheme 1.

[1358]

[1359] Option 1: All R1, R2, R3, R4 and R5 are as described in the compounds of this invention.

[1360] In the presence of Lewis acids (e.g., titanium(IV) chloride, zinc(II) chloride, etc.), in polar solvents (e.g., DCM, MeOH, EtOH, etc.), at temperatures ranging from 0 to 100 °C, p-benzoquinone of Formula 1 can be condensed with a ketone ester of Formula 2 (commercially available or synthesized by procedures known to those skilled in the art), wherein R2 is an ester protecting group (e.g., methyl, ethyl, t-Bu, etc.) to provide an intermediate of Formula 4. More detailed information can be found in the following references (Bioorg. Med. Chem. 2012, 20, 4237-4244 and FR 1319594). Alternatively, the p-benzoquinone of Formula 1 can be reacted with an enamine of Formula 3 (commercially available or synthesized by procedures known to those skilled in the art) in the presence of a protic acid (e.g., trifluoroacetic acid, p-toluenesulfonic acid, etc.) in a polar solvent (e.g., DCM, MeOH, EtOH, etc.) at a temperature ranging from 0 to 100 °C to provide the intermediate of Formula 4. More detailed information can be found in the following reference (J. Heterocyclic Chem., 2006, 43, 873). The intermediate of Formula 5, in which LG is the leaving group (commercially available or synthetic), can then be converted to the desired Formula 7 compound via nucleophilic substitution in the presence of a base (e.g., DIPEA, DBU, triethylamine, Cs₂CO₃, etc.), in a polar solvent (e.g., acetonitrile, DMF, NMP, etc.), with or without a chelating agent (e.g., 18-crown ether-6, cis-trans-cis-dicyclohexyl-18-crown ether-6, etc.), at a temperature ranging from 0 to 100 °C. Alternatively, the intermediate of Formula 4 can also be reacted with the intermediate of Formula 6 (commercially available or synthetic) in a solvent (e.g., THF, toluene, etc.) in the presence of an azodicarboxylic acid ester reagent (e.g., DEAD, DIAD, ADDP, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.) at a temperature ranging from 0 to 100 °C to provide the desired Formula 7 compound. The ester derivative 7 can then be converted to the desired Formula 8 compound by a standard saponification reaction. The desired Formula 10 compound can be obtained by reacting an acid derivative of Formula 8 with an amine derivative of Formula 9 (commercially available or synthesized by methods known in the art or as described in the examples below) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.) in a polar aprotic solvent (e.g., DCM, DMF, etc.). Alternatively, the carboxylic acid derivative of Formula 8 can be converted into an acyl chloride derivative by methods known to those skilled in the art or as described in the examples below, and then reacted with an amine of Formula 9 by methods known to those skilled in the art or as described in the examples below to obtain the desired Formula 10 compound.

[1361] In a more specific embodiment, the compounds of the present invention may be synthesized as described in Scheme 2.

[1362]

[1363] Option 2: All R1, R2, R3, R4 and R5 are as described in the compounds of this invention.

[1364] A 5-hydroxy-benzofuran-3-carboxylic acid derivative 11 (commercially available or synthesized by procedures known in the art or as described in the examples below) can be reacted with an amine derivative of Formula 9 (commercially available or synthesized by procedures known in the art or as described in the examples below) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.) in a polar aprotic solvent (e.g., DCM, DMF, etc.) to provide an intermediate of Formula 12. Alternatively, a compound of Formula 13 (synthesized as described in Scheme 1) can be converted to an intermediate of Formula 12 by hydrogenation with a reducing agent (e.g., hydrogen, ammonium formate, cyclohexadiene, etc.) in a solvent (e.g., THF, EtOH, etc.) using a catalyst (more preferably Pd or Pt). The intermediate of Formula 12 can then be converted to the desired compound of Formula 10 via nucleophilic substitution in the presence of a base (e.g., DIPEA, DBU, triethylamine, Cs₂CO₃, etc.), in a polar solvent (e.g., acetonitrile, DMF, NMP, etc.), with or without a chelating agent (e.g., 18-crown ether-6, cis-trans-cis-dicyclohexyl-18-crown ether-6, etc.), at a temperature ranging from 0 to 100 °C. Alternatively, the compound of Formula 12 can also be reacted with the intermediate of Formula 6 (commercially available or synthetically produced) in the presence of an azodicarboxylic acid ester reagent (e.g., DEAD, ADDP, DIAD, tert-butyl azodicarboxylic acid, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.) in a solvent (e.g., THF, toluene, etc.) at a temperature ranging from 0 to 100 °C to provide the desired compound of Formula 10.

[1365] In a more specific embodiment, the compounds of the present invention may be synthesized as described in Scheme 3.

[1366]

[1367] Option 3: All R1, R2, R3, R4, R5, R7 and R8 are as described in the compounds of this invention.

[1368] In the presence of Lewis acids (e.g., titanium(IV) chloride, zinc(II) chloride, etc.), in polar solvents (e.g., DCM, MeOH, EtOH, etc.), at temperatures ranging from 0 to 100 °C, a substituted p-benzoquinone derivative of Formula 14 can be condensed with a ketone ester of Formula 2 (commercially available or synthesized by procedures known to those skilled in the art), wherein R2 is an ester protecting group (e.g., methyl, ethyl, t-Bu, etc.) to provide a mixture of substituted intermediates of Formulas 15 and 16. More detailed information can be found in the following references (Bioorg. Med. Chem. 2012, 20, 4237-4244 and FR1319594). The intermediates of Formula 15 and / or 16, in which LG is the leaving group (commercially available or synthetic), can then be converted into the desired compounds of Formula 17 and / or 18 via nucleophilic substitution in the presence of a base (e.g., DIPEA, DBU, triethylamine, Cs2CO3, etc.), in a polar solvent (e.g., acetonitrile, DMF, NMP, etc.), with or without a chelating agent (e.g., 18-crown ether-6, cis-trans-cis-dicyclohexyl-18-crown ether-6, etc.), at a temperature in the range of 0 to 100 °C. Alternatively, intermediates of formula 15 and / or 16 can also be reacted with intermediates of formula 6 (commercially available or synthetic) in the presence of an azodicarboxylic acid ester reagent (e.g., DEAD, DIAD, ADDP, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.) in a solvent (e.g., THF, toluene, etc.) at a temperature ranging from 0 to 100 °C to provide the desired compounds of formula 17 and / or 18. Ester derivatives 17 and / or 18 can then be converted to the desired carboxylic acids of formula 19 and / or 20 by a standard saponification reaction. The desired compounds of formula 21 and / or 22 can be obtained from acid derivatives of formula 19 and / or 20 by reacting with amine derivatives of formula 9 (commercially available or synthesized by methods known in the art or as described in the examples below) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.) in a polar aprotic solvent (e.g., DCM, DMF, etc.). A mixture of compounds 21 and 22 can be separated (e.g., by silica gel, HPLC, SFC, or preparative CFC) to provide the desired compound of formula 21 or 22.

[1369] In a more specific embodiment, the compounds of the present invention may be synthesized as described in Scheme 4.

[1370]

[1371] Option 4: All R1, R2, R3, R4, R5, R7 and R8 are as described in the compounds of this invention.

[1372] The intermediate of Formula 4 can be halogenated in a solvent (e.g., chloroform, water, etc.) with a suitable halogenating agent (e.g., bromine, N-bromosuccinimide, etc.) to provide the desired intermediate 23. The desired compound of Formula 26 can be obtained by reacting CuCN in a Ullmann-type reaction followed by a Mitsunobu-type reaction with the intermediate of Formula 6 (commercially available or synthetically produced). Alternatively, the desired compound of Formula 26 can be obtained by a Mitsunobu-type reaction with the intermediate of Formula 6 (commercially available or synthetically produced), followed by a Suzuki reaction. The ester derivative 26 can then be converted to the desired compound of Formula 27 by a standard saponification reaction. The desired compound of Formula 28 can be obtained from the acid derivative of Formula 27 by reacting it with the amine derivative of Formula 9 (commercially available or synthesized by methods known in the art or as described in the examples below) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.) in a polar aprotic solvent (e.g., DCM, DMF, etc.).

[1373] In a more specific embodiment, the compounds of the present invention may be synthesized as described in embodiment 5.

[1374]

[1375] Option 5: All R1, R2, R3 and R4 are as described in the compounds of this invention.

[1376] The intermediate of Formula 4 can be halogenated in a solvent (e.g., chloroform, acetonitrile, etc.) with a suitable halogenating agent (e.g., fluorine, etc.) to provide the desired intermediates 29 and 30. The intermediates of Formula 29 and / or 30 can be reacted with the intermediate of Formula 6 (commercially available or synthetic) in a solvent (e.g., THF, toluene, etc.) in the presence of an azodicarboxylic acid ester reagent (e.g., DEAD, DIAD, ADDP, etc.) and a phosphine (e.g., tributylphosphine, triphenylphosphine, etc.) at a temperature ranging from 0 to 100 °C to provide the desired compounds of Formula 31 and / or 32. The ester derivatives 31 and / or 32 can then be converted to the corresponding carboxylic acids of Formula 33 and / or 34 by a standard saponification reaction. The desired compounds of formula 35 and / or 36 can be obtained by reacting acid derivatives of formula 33 and / or 34 with amine derivatives of formula 9 (commercially available or synthesized by methods known in the art or as described in the examples below) under standard peptide coupling conditions (e.g., DCC, EDCI, HATU, PyBop, etc.) in a polar aprotic solvent (e.g., DCM, DMF, etc.). Mixtures of compounds 35 and 36 can be isolated (e.g., silica gel, HPLC, SFC, or preparative CFC) to provide the desired compound of formula 35 or 36.

[1377] Example

[1378]

[1379]

[1380]

[1381]

[1382]

[1383]

[1384]

[1385]

[1386]

[1387]

[1388]

[1389]

[1390]

[1391]

[1392]

[1393]

[1394]

[1395]

[1396]

[1397]

[1398]

[1399]

[1400]

[1401]

[1402]

[1403]

[1404]

[1405]

[1406]

[1407]

[1408]

[1409]

[1410]

[1411]

[1412]

[1413] The following examples are provided to illustrate the invention and should not be construed as limiting the scope of the invention.

[1414] Part A represents the preparation of the compound, while part B represents a pharmacological example.

[1415] Part A

[1416] All starting materials not explicitly described are commercially available (details of suppliers such as Acros, Avocado, Aldrich, Fluka, FluoroChem, Matrix Scientific, Maybridge, Merck, Sigma, etc. can be found at [link to supplier information]). (Found in the database) or its synthesis has been precisely described in professional literature (experimental guidelines can be found in, for example) database or (Found in a database) or can be prepared using conventional methods known to those skilled in the art.

[1417] If desired, the reaction is carried out under an inert atmosphere (primarily argon and N2). The equivalence of reagents and the amount of solvent used, as well as the reaction temperature and time, can be slightly varied between different reactions carried out using similar methods. Post-treatment and purification methods are adjusted according to the characteristic properties of each compound and can be slightly varied for similar methods. The yields of the prepared compounds were not optimized.

[1418] The terms "equivalent" ("eq." or "eq" or "equiv.") indicate molar equivalents, "RT" or "rt" indicates room temperature (T, 23±7℃), "M" is the concentration in mol / L, "sol." indicates a solution, and "conc." indicates a concentration. The mixing ratio of solvents is usually expressed as a volume / volume ratio.

[1419] pass 1 H-NMR spectroscopy and / or mass spectrometry (MS, m / z represents [M+H]) + and / or [MH] – Key analytical characterization was performed on all exemplary compounds and selected intermediates. In some cases, regioisomers and / or diastereomers may form during the reaction, and in others, additional analyses were performed, such as... 13 C NMR and NOE (nuclear overhauser effect) NMR experiments.

[1420] The analytical instruments used were, for example, a BRUKER 400MHz or BRUKER 500MHz instrument (Software Topspin) for NMR analysis, or a BRUKER AVANCE 300MHz and 400MHz instrument. For LC / MS analysis, instruments such as an Agilent 1290 Infinity, Mass:6150SQD (ESI / APCI) or an Agilent 1200 SERIES, Mass:6130SQD (ESI / APCI) (Software Chemistation) were used. Analytical HPLC was performed, for example, on Waters (Software Empower), an Agilent-1200-ELSD (Software Chemistation), or an Agilent-1260 (Software OpenLAB). Analytical SFC was performed, for example, on PIC solutions (Software: SFC PICLAB ONLINE), WATERS-X5 (Software MASSLYNX), or WATERS-UPC2 (Empower).

[1421] Preparative HPLC was performed, for example, on a Waters 2998 (Software Empower) or YMC (Software K-Prep). Preparative SFC was performed, for example, on a Waters SFC-200 (Software Chromscope or Super chrome), Waters SFC-80 (Super chrome), or PIC PIC-175 (Software S10-100).

[1422] If the stereochemistry is known, draw the structure of the example compound containing the stereocenter and name it with its absolute stereochemistry. In cases where the absolute stereochemistry is unknown, the compound may be a mixture of racemic diastereomers, a pure diastereomer with unknown stereochemistry, or a pure enantiomer with unknown stereochemistry. Dia 1 and Dia 2 indicate that the diastereomers have been isolated, but their stereochemistry is unknown. En 1 and En 2 indicate that both enantiomers have been isolated, but their absolute configuration is unknown. The absence of a suffix after the compound code indicates that the compound containing the stereocenter was obtained as either a racemic mixture or a mixture of diastereomers, unless the chemical name of the compound specifies the exact stereochemistry.

[1423] The LC / MS analyses mentioned in the experimental section were also performed on a Dionex Ultimate 3000 HPLC system (equipped with a PDA detector) connected to a Brucker Esquire 6000 mass spectrometer (equipped with a multi-mode source, ESI / APCI) (Method L in the table below). Alternatively, the LC / MS analyses mentioned in the experimental section were performed on a Waters system that incorporates an Acquity UPLC H-Class equipped with an Acquity UPLC PDA detector and an Acquity TQ detector (ESI) (Method U in the table below).

[1424] Conditions used for HPLC analysis in the experimental section. The LC / MS analyses mentioned in the experimental section were performed on a Dionex Ultimate 3000 HPLC system (equipped with a PDA detector) connected to a Brucker Esquire 6000 mass spectrometer (equipped with a multimode source, ESI / APCI). Separations were performed using a SunFire C18 3.5μm 3.0x100mm column equipped with a SunFire C18 3.5μm 3.0x20mm Guard column or an X-Bridge C18 100x3.0mm column equipped with an X-Bridge C18 3.5μm 3.0x20mm Guard column kept at 30°C, with the DAD acquisition wavelength set in the range of 190 to 420 nm (Method L in the table below). Elution was performed using the methods described in the table below. Solvent A: 0.1% formic acid (LC-MS grade) in milliQ water; Solvent B: 10 mmol NH4OAc (LC-MS grade) in milliQ water, adjusted to pH 10 with NH3 aqueous solution (LC-MS grade); Solvent C: Acetonitrile (LC-MS grade).

[1425]

[1426]

[1427] Conditions used for UPLC analysis in the experimental section. The LC / MS analyses mentioned in the experimental section were performed on a Waters system combining an Acquity UPLC H-Class equipped with an Acquity UPLC PDA detector and an Acquity TQ detector (ESI). Separation was performed using an Acquity UPLC HSS C18 column (2.1 x 50 mm, 1.8 μM) equipped with a pre-filter and kept at 40 °C, or an Acquity UPLC BEH C18 column (2.1 x 50 mm, 1.7 μM) equipped with a pre-filter and kept at 40 °C, with the PAD acquisition wavelength set in the range of 210 to 420 nm (Method U in the table below). Elution was performed using the method described in the table below. Solvent A: 0.1% formic acid (LC-MS grade) in milliQ water; Solvent B: 10 mmol NH4OAc (LC-MS grade) in milliQ water, adjusted to pH 10 with NH3 aqueous solution, LC-MS grade. Solvent C: Acetonitrile, LC-MS grade.

[1428]

[1429]

[1430] The preparative HPLC purifications mentioned in this experimental section were performed using the following system: a Waters 2489 UV / Visible detector, a Waters 2545 binary gradient module, a Waters fraction collector III, and a Waters Dual Flex syringe. Separation was performed using X-Bridge Prep C18 columns equipped with X-Bridge C18 guard columns (19x10 mm, 5 μm) or SunFire Prep C18 ODB columns equipped with SunFire C18 guard columns (5 μm; 19x100 mm) or (5 μm; 19x10 mm). Elution was performed using the methods described in the table below, with detection wavelengths fixed at 210 and 254 nm. Solvent A: 0.1% formic acid (LC-MS grade) in milliQ water; Solvent B: 10 mmol NH4OAc (LC-MS grade) in milliQ water, adjusted to pH 10 with NH3 aqueous solution, LC-MS grade. Solvent C: Acetonitrile, LC-MS grade.

[1431]

[1432] The synthesis of 2-methyl-5-((5-(trifluoromethyl)furan-2-yl)methoxy)benzofuran-3-carboxylic acid (cpd 018) become.

[1433]

[1434] Step 1: Cesium carbonate (0.444 g; 1.36 mmol) was added to a solution of ethyl 5-hydroxy-2-methylbenzofuran-3-carboxylate (0.100 g; 0.45 mmol) in THF (10 mL) and NMP (1 mL), and the mixture was stirred at room temperature for 25 minutes. Then, 2-(bromomethyl)-5-(trifluoromethyl)furan (0.104 mg; 0.45 mmol) was added, and the stirred solution was heated at 95 °C until the 5-hydroxy-2-methylbenzofuran-3-carboxylate was consumed. The mixture was cooled to room temperature, poured into water, and extracted twice with EtOAc. The combined organic layers were dried over sodium sulfate, filtered, and concentrated under reduced pressure. The residue was purified by a heptane gradient of EtOAc (0% to 80%) on silica gel via FC to give 0.167 g (100%) ethyl 2-methyl-5-((5-(trifluoromethyl)furan-2-yl)methoxy)benzofuran-3-carboxylic acid.

[1435] Step 2: Sodium hydroxide (0.102 g; 1.8 mmol) was added to a solution of ethyl 2-methyl-5-((5-(trifluoromethyl)furan-2-yl)methoxy)benzofuran-3-carboxylic acid (0.167 g; 0.45 mmol) in a mixture of water-EtOH-MeOH-THF (6:3:3:1, 12 mL), and the solution was heated under reflux until the ethyl 5-(benzyloxy)-2-methylbenzofuran-3-carboxylic acid was consumed. After cooling, the volatiles were removed under reduced pressure, and the remaining residue was dissolved in water and washed with DCM. The mixture was acidified to pH ~2 with aqueous hydrochloric acid (6N) and extracted with EtOAc. The resulting organic layer was washed with water and brine, dried over magnesium sulfate, and filtered to give 147.6 mg (89%) of 2-methyl-5-((5-(trifluoromethyl)furan-2-yl)methoxy)benzofuran-3-carboxylic acid (cpd 018).

[1436] Cpd 016 and cpd 017 were prepared in a similar manner to cpd 018 (using appropriate reagents and purification methods known to those skilled in the art).

[1437] Synthesis of 2-methyl-5-((2-(trifluoromethyl)benzyl)oxy)benzofuran-3-carboxylic acid (cpd 101).

[1438]

[1439] Step 1: Tributylphosphine (1.7 mL; 6.5 mmol) was added dropwise under argon atmosphere to a stirred mixture of methyl 5-hydroxy-2-methylbenzofuran-3-carboxylate (1 g; 4.6 mmol), 2-(trifluoromethyl)pyridin-3-yl)methanol (1.28 g; 6.9 mmol), and ADDP (1.66 g; 6.5 mmol) in dry THF (5 mL). The mixture was stirred for 2 hours and concentrated under reduced pressure. The residue was purified by FCC using a heptane gradient of EtOAc (0 to 20%) on silica gel to give 1.4 g (83%) of methyl 2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxylate. M / Z(+): 366 (M+H). M / Z(-): 364 (MH).

[1440] S...

Claims

1. A compound of formula (I) or a physiologically acceptable salt thereof （I） in R 1 CH3 can be arbitrarily replaced by F; Q is -NR 3 R 4 ; R 3 It is H; R 4 yes or ; T is -O- and U is -CH2-; R 6 R 7 and R 8 Each is H; and V is a 5-membered heteroaryl group selected from oxazolyl, isoxazolyl, thiazolyl, pyrazolyl, and imidazolyl, or a 6-membered heteroaryl group selected from pyridinyl, pyridazinyl, pyrimidinyl, and pyrazinyl, wherein the 5-membered heteroaryl or 6-membered heteroaryl group is optionally substituted with the following groups: -F, -Cl, C1-C3 alkyl optionally substituted with -F, or C1-C3 alkoxy optionally substituted with -F.

2. The compound of claim 1 or a physiologically acceptable salt thereof, wherein R 1 It is -CH3.

3. The compound of claim 1 or a physiologically acceptable salt thereof, wherein R 4 yes or .

4. The compound of claim 1 or a physiologically acceptable salt thereof, wherein R 4 yes .

5. The compound of claim 1 or a physiologically acceptable salt thereof, wherein R 4 yes .

6. The compound of claim 1 or a physiologically acceptable salt thereof, wherein V is a 5-membered heteroaryl group selected from oxazolyl, isoxazolyl, thiazolyl, pyrazolyl and imidazolyl, wherein the 5-membered heteroaryl group is optionally substituted with the following groups: -F, -Cl, C1-C3 alkyl optionally substituted with -F or C1-C3 alkoxy optionally substituted with -F.

7. The compound of claim 1 or a physiologically acceptable salt thereof, wherein V is a 6-membered heteroaryl group selected from pyridinyl, pyridinyl, pyrimidinyl and pyrazinyl, wherein the 6-membered heteroaryl group is optionally substituted with the following groups: -F, -Cl, C1-C3 alkyl optionally substituted with -F or C1-C3 alkoxy optionally substituted with -F.

8. A compound selected from the group consisting of: (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-(trifluoromethyl)pyridin-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-(trifluoromethyl)thiazo-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methyl-4-(trifluoromethyl)thiazo-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazo-4-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylisoxazol-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylthiazo-4-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridazine-3-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyrimidin-4-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-(difluoromethoxy)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,4-dimethylthiazo-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,5-dimethylthiazo-4-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((3-(difluoromethyl)pyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-imidazol-2-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide; N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide; N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-(difluoromethyl)pyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide; N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,4-dimethylthiazo-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-hydroxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide; N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((2-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((2-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((4-methylthiazolyl-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((1-(2,2-difluoroethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((4-fluoro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-3-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1,4-dimethyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-chloro-1-methyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((4-chloro-1-isopropyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((3-methylisoxazol-5-yl)methyl)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-isopropyl-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2,4-dimethyloxazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-isopropylthiazo-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylthiazo-2-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((1-(cyclopropylmethyl)-1H-pyrazol-5-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((4-(trifluoromethyl)thiazo-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(thiazo-2-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(thiazo-5-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((1-methyl-1H-pyrazol-4-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((5-methylpyridin-2-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-((2-methylpyrimidin-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyrimidin-2-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyrazin-2-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-4-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((2-methoxypyridin-3-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-2-methyl-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-2-methyl-1-oxopropyl-2-yl)-5-((5-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-5-((5-fluoropyridin-2-yl)methoxy)-2-methylbenzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((4-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((6-methylpyridin-3-yl)methoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-(pyridin-2-ylmethoxy)benzofuran-3-carboxamide; (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((2-methylthiazo-5-yl)methoxy)benzofuran-3-carboxamide; and (S)-N-(1-amino-3-hydroxy-1-oxopropyl-2-yl)-2-(difluoromethyl)-5-((2-methyloxazol-5-yl)methoxy)benzofuran-3-carboxamide, Or a physiologically acceptable salt.

9. A pharmaceutical composition comprising a compound according to any one of claims 1 to 8 or a physiologically acceptable salt thereof and a pharmaceutically acceptable carrier.

10. Use of the compound of any one of claims 1 to 8 or a physiologically acceptable salt thereof or the pharmaceutical composition of claim 9 in the preparation of a medicament for treating pain.

11. The use according to claim 10, wherein the pain is selected from nociceptive pain, inflammatory pain, and neuropathic pain.

12. The use according to claim 10, wherein the pain is postoperative pain.

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