公开(公告)号：KR1020100119757A

公开(公告)日：2010-11-10

申请号：KR1020107016895

申请日：2009-01-28

Applicant: (주)아모레퍼시픽

Inventor： 신송석 ,  김진관 ,  김선영 ,  이기화 ,  우병영 ,  모주현 ,  정연수 ,  임경민 ,  최진규 ,  고현주 ,  박영호

IPC: C07C311/45 ,  C07C311/13 ,  A61K31/18 ,  A61P29/00

CPC classification number: C07C311/08 ,  C07C2601/14 ,  C07D295/145 ,  C07C311/45 ,  A61K31/18 ,  C07C311/13

Abstract: PURPOSE: A compound as a vinilloid receptor antagonist, an isomer thereof, and a pharmaceutical composition containing thereof are provided to secure the remarkably improved balance of the vinilloid receptor 1 activity and the PK properties. CONSTITUTION: A compound, an isomer thereof, and pharmaceutically acceptable salt thereof has the structure marked with chemical formula 1. In the chemical formula 1, R1 is hydrogen, methyl, or ethyl. R2 and R3 are independently, the hydrogen, halogen, cyano, the methyl, the ethyl, methoxy, trifluoromethyl, vinyl, or acetylenyl. R4 is either the trifluoromethyl or fluoro.

Abstract translation: 目的：提供作为维生素受体拮抗剂的化合物，其异构体和含有其的药物组合物，以确保维生素受体1活性和PK性质的显着改善的平衡。 构成：化合物及其药学上可接受的盐具有化学式1的结构。在化学式1中，R 1是氢，甲基或乙基。 R2和R3独立地为氢，卤素，氰基，甲基，乙基，甲氧基，三氟甲基，乙烯基或乙炔基。 R4是三氟甲基或氟。

公开(公告)号：KR1020100053470A

公开(公告)日：2010-05-20

申请号：KR1020090108632

申请日：2009-11-11

Applicant: (주)아모레퍼시픽

Inventor： 김선영 ,  김연준 ,  남미희 ,  이기화 ,  신송석 ,  우병영 ,  임경민 ,  정연수 ,  모주현 ,  최진규 ,  고현주 ,  이정오 ,  김혁 ,  윤정훈

IPC: C07D323/04 ,  A61K31/357

Abstract: PURPOSE: A novel compound which functions as a vanilloid receptor 1(VR1) antagonist is provided to prevent or treat disease related to hair growth, rhinitis, and pancreatitis. CONSTITUTION: A vanilloid receptor antagonist compound is denoted by chemical formula I. A pharmaceutical composition contains the compound, isomer, or pharmaceutically acceptable salt thereof. The composition is used for preventing or treating arthritis disease, neuropathy, HIV related neuropathy, nerve injury, neurodegeneration, cerebral apoplexy, urinary incontinence, cough, neuropathy/allergy/inflammation skin disease, atopic dermatitis, psoriasis, pruritus, the prurigo, acouesthesia, aliasing, bregma anaphylaxis, effluvium, or alopecia.

Abstract translation: 目的：提供作为香草素受体1（VR1）拮抗剂起作用的新型化合物，以预防或治疗与毛发生长，鼻炎和胰腺炎有关的疾病。 构成：香草素受体拮抗剂化合物由化学式I表示。药物组合物含有化合物，异构体或其药学上可接受的盐。 该组合物用于预防或治疗关节炎疾病，神经病，HIV相关神经病，神经损伤，神经变性，脑中风，尿失禁，咳嗽，神经病变/过敏/炎症皮肤病，特应性皮炎，牛皮癣，瘙痒，瘙痒症，麻醉， 混叠，原发性过敏性反应，流出或脱发。

公开(公告)号：KR1020080007329A

公开(公告)日：2008-01-18

申请号：KR1020077024002

申请日：2006-03-15

Applicant: (주)아모레퍼시픽

Inventor： 김희두 ,  서영거 ,  박형근 ,  오우택 ,  박설린 ,  김주현 ,  장미정 ,  박영호 ,  신송석 ,  김선영 ,  김진관 ,  정연수 ,  이기화 ,  최진규 ,  임경민 ,  고현주 ,  모주현 ,  김성일 ,  우병영

IPC: C07C275/24 ,  C07C275/18 ,  A61K31/17

CPC classification number: C07C275/24 ,  C07C311/08 ,  C07C311/11 ,  C07C323/62 ,  C07D211/46 ,  C07D295/088 ,  C07D295/155 ,  C07D309/12 ,  C07F7/0818

Abstract: A compound as a vanilloid receptor antagonist is provided to obtain a pharmaceutical composition effective for preventing or treating pain, migraine, arthralgia, nerve injury, skin diseases, overactive bladder, irritable bowel syndrome, or the like. A compound as a vanilloid receptor antagonist, an isomer or a pharmaceutically acceptable salt thereof is represented by the following formula I. In formula I, X is NHCH2, CR11=CR12, NH, CHR11CHR12 or C=C, wherein each of R11 and R12 represents H, halogen, C1-C5 alkyl, C1-C5 alkoxy, halo(C1-C5)alkyl or phenyl; R1 is a C2-C5 alkenyl or C2-C5 alkynyl; R2 is H, halogen, nitro, cyano, C1-C5 alkyl, C1-C5 alkoxy, halo(C1-C5)alkyl, C2-C5 alkenyl, or C2-C5 alkynyl; R2 is H, halogen, nitro, cyano, C1-C5 alkyl, C1-C5 alkoxy, halo(C1-C5)alkyl, C2-C5 alkenyl, C2-C5 alkynyl, carboxyl, C1-C5 alkoxycarbonyl, C1-C5 alkylthio, phenyl or phenyl(C1-C3)alkyl, wherein is each phenyl group is non-substituted or substituted with at least one substituent; R3 is H, C1-C5 alkyl, C1-C5 alkoxy or halo(C1-C5)alkyl; each of R4, R5 R6, R7 and R8 independently represents H, carboxyl, C1-C5 alkyl, nitro, C2-C5 alkenyl, C1-C5 alkoxy, C2-C5 alkynyl, halo(C1-C5)alkyl, C1-C5 alkylthio, C1-C5 alkylsulfonyl, C1-C5 alkylcarbonyl, C1-C5 alkoxycarbonyl, hydroxy, C2-C5 alkenyloxy, C1-C5 alkoxy(C1-C5)alkoxy, C1-C5 alkoxy(C1-C5)alkoxy(C1-C5)alkyl, C1-C3 alkylpiperazinyl, piperazinyl(C1-C5)alkoxy, piperidinyl(C1-C5)alkoxy, C1-C5 alkoxy (C1-C5)alkylamino, C1-C7 alkylamino, morpholinyl, morpholinyl(C1-C5)alkyloxy, tetrahydropyranyloxy, phenyl or halogen, wherein each phenyl group is non-substituted or substituted with at least one substituent; each of R9 and R10 independently represents H, -SO2R13, -SOR13, C1-C5 alkyl, C1-C5 alkoxy, halo (C1-C5)alkyl, C2-C5 alkenyl, C1-C5 alkoxycarbonyl, C1-C5 alkylthio, phenyl or phenyl (C1-C3)alkyl, wherein each phenyl group is non-substituted or substituted with at least one substituent, and R13 is H, amino, C1-C5 alkyl, C2-C5 alkenyl, C1-C5 alkoxy, halo(C1-C5)alkyl, trifluoromethyl, phenyl or phenyl(C1-C3)alkyl.

Abstract translation: 提供作为香草素受体拮抗剂的化合物以获得有效预防或治疗疼痛，偏头痛，关节痛，神经损伤，皮肤疾病，膀胱过度活动症，肠易激综合征等的药物组合物。 作为香草酸受体拮抗剂的化合物，其异构体或其药学上可接受的盐由下式I表示。在式I中，X为NHCH 2，CR 11 = CR 12，NH，CHR 11 CHR 12或C = C，其中R 11和R 12 表示H，卤素，C 1 -C 5烷基，C 1 -C 5烷氧基，卤代（C 1 -C 5）烷基或苯基; R1是C2-C5烯基或C2-C5炔基; R2是H，卤素，硝基，氰基，C1-C5烷基，C1-C5烷氧基，卤代（C1-C5）烷基，C2-C5烯基或C2-C5炔基; R2是H，卤素，硝基，氰基，C1-C5烷基，C1-C5烷氧基，卤代（C1-C5）烷基，C2-C5烯基，C2-C5炔基，羧基，C1-C5烷氧羰基，C1-C5烷硫基， 苯基或苯基（C1-C3）烷基，其中每个苯基是未取代的或被至少一个取代基取代; R3是H，C1-C5烷基，C1-C5烷氧基或卤代（C1-C5）烷基; R 4，R 5，R 6，R 7和R 8各自独立地表示H，羧基，C 1 -C 5烷基，硝基，C 2 -C 5烯基，C 1 -C 5烷氧基，C 2 -C 5炔基，卤代（C 1 -C 5）烷基，C 1 -C 5烷硫基 ，C1-C5烷基磺酰基，C1-C5烷基羰基，C1-C5烷氧基羰基，羟基，C2-C5链烯氧基，C1-C5烷氧基（C1-C5）烷氧基，C1-C5烷氧基（C1-C5）烷氧基（C1-C5）烷基 （C1-C5）烷氧基，C1-C5烷氧基（C1-C5）烷基氨基，C1-C7烷基氨基，吗啉基，吗啉基（C1-C5）烷氧基，四氢吡喃基氧基， 苯基或卤素，其中每个苯基未被取代或被至少一个取代基取代; R 9和R 10各自独立地表示H，-SO 2 R 13，-SOR 13，C 1 -C 5烷基，C 1 -C 5烷氧基，卤代（C 1 -C 5）烷基，C 2 -C 5烯基，C 1 -C 5烷氧基羰基，C 1 -C 5烷硫基，苯基或 苯基（C1-C3）烷基，其中每个苯基未被取代或被至少一个取代基取代，R 13是H，氨基，C 1 -C 5烷基，C 2 -C 5烯基，C 1 -C 5烷氧基，卤代（C1- C5）烷基，三氟甲基，苯基或苯基（C1-C3）烷基。

公开(公告)号：KR1020070114821A

公开(公告)日：2007-12-04

申请号：KR1020077024004

申请日：2006-03-17

Applicant: (주)아모레퍼시픽

Inventor： 서영거 ,  김희두 ,  박형근 ,  오우택 ,  이용실 ,  박설린 ,  유정현 ,  박영호 ,  신송석 ,  김선영 ,  김진관 ,  정연수 ,  이기화 ,  최진규 ,  임경민 ,  고현주 ,  모주현 ,  김성일 ,  배준호

IPC: C07C275/24 ,  C07C275/18 ,  A61K31/17

CPC classification number: C07C275/24 ,  C07C311/08 ,  C07C311/11 ,  C07C323/62 ,  C07D211/46 ,  C07D295/088 ,  C07D295/155 ,  C07D309/12 ,  C07F7/0818

Abstract: A compound as a vanilloid receptor antagonist is provided to obtain a high activity in preventing or treating pain, migraine, arthralgia, neuralgia, neural diseases, neural injury, skin diseases, irritable bowel syndrome, inflammatory diseases, cardiac diseases, etc. A compound as a vanilloid receptor antagonist is a compound represented by the following formula Ia or an isomer and/or pharmaceutically acceptable salt thereof. In formula Ia, X is CR11=CR12 or C=C, wherein each of R11 and R12 independently represents H, a halogen atom, C1-C5 alkyl or phenyl; each of R1 and R2 independently represents H, carboxyl, C1-C5 alkyl, halogen, nitro, C1-C5 alkoxy, halo(C1-C5)alkyl, C1-C5 alkylcarbonyl, C1-C5 alkylcarbonylamino, C1-C5 alkylsulfonylamino, phenylsulfonylamino, C1-C5 alkylthio, C1-C5 alkylsulfonyl or C1-C5 alkoxycarbonyl; R3 is H, C1-C5 alkyl, C1-C5 alkoxy or halo(C1-C5)alkyl; each of R4, R5, R6, R7 and R8 independently represents H, carboxyl, C1-C5 alkyl, nitro, C2-C5 alkenyl, C1-C5 alkoxy, C2-C5 alkynyl, halo(C1-C5)alkyl, C1-C5 alkylthio, C1-C5 alkylsulfonyl, C1-C5 alkylcarbonyl, C1-C5 alkoxycarbonyl, phenyl or halogen, wherein the phenyl is non-substituted or substituted with at least one substituent selected from carboxyl, C1-C5 alkyl, halogen, nitro, C2-C5 alkenyl, C1-C5 alkoxy, halo(C1-C5)alkyl, C1-C5 alkylcarbonyl, C1-C5 alkylthio, C1-C5 alkylsulfonyl and C1-C5 alkoxycarbonyl; R9 is C1-C5 alkylsulfonyl or C2-C5 alkenylsulfonyl; and R10 is H, with the proviso that when R3 is not H, R11 and R13 cannot represent H at the same time.

Abstract translation: 提供了一种作为香草素受体拮抗剂的化合物，用于预防或治疗疼痛，偏头痛，关节痛，神经痛，神经疾病，神经损伤，皮肤病，肠易激综合征，炎性疾病，心脏病等中的高活性。 香草酸受体拮抗剂是由下式Ia表示的化合物或其异构体和/或其药学上可接受的盐。 在式Ia中，X是CR 11 = CR 12或C = C，其中R 11和R 12各自独立地表示H，卤素原子，C 1 -C 5烷基或苯基; R1和R2各自独立地表示H，羧基，C1-C5烷基，卤素，硝基，C1-C5烷氧基，卤代（C1-C5）烷基，C1-C5烷基羰基，C1-C5烷基羰基氨基，C1-C5烷基磺酰基氨基，苯基磺酰基氨基， C1-C5烷硫基，C1-C5烷基磺酰基或C1-C5烷氧基羰基; R3是H，C1-C5烷基，C1-C5烷氧基或卤代（C1-C5）烷基; R4，R5，R6，R7和R8各自独立地表示H，羧基，C1-C5烷基，硝基，C2-C5烯基，C1-C5烷氧基，C2-C5炔基，卤代（C1-C5）烷基，C1-C5 烷基硫代，C 1 -C 5烷基磺酰基，C 1 -C 5烷基羰基，C 1 -C 5烷氧基羰基，苯基或卤素，其中苯基是未取代的或被至少一个选自羧基，C 1 -C 5烷基，卤素，硝基， C5链烯基，C1-C5烷氧基，卤代（C1-C5）烷基，C1-C5烷基羰基，C1-C5烷硫基，C1-C5烷基磺酰基和C1-C5烷氧基羰基; R9为C1-C5烷基磺酰基或C2-C5链烯基磺酰基; R 10为H，条件是当R3不为H时，R11和R13不能同时表示H。