公开(公告)号：KR101494488B1

公开(公告)日：2015-02-24

申请号：KR1020107017557

申请日：2008-12-03

Applicant: (주)아모레퍼시픽

Inventor： 박미영 ,  김연준 ,  최진규 ,  이기화 ,  김선영 ,  고현주 ,  우병영 ,  이은경 ,  신동욱 ,  이형호 ,  이태룡 ,  임경민

IPC: A61K31/15 ,  A61P3/02 ,  A61P3/10

CPC classification number: A61K31/15

Abstract: 화학식 1로 나타내어지는 2-사이클로펜텐-1-온 옥심유도체를 포함하는 비만, 이상지질혈증, 당뇨 등과 같은 지방대사질환 예방 및 치료용 약학조성물이 개시된다. 구체적으로 상기 화합물은 분화된 지방세포 (3T3-L1)에서의 지방분해를 촉진시켜 결과적으로 체내 지방을 감소시킴으로써, 비만, 이상지질혈증, 당뇨 등과 같은 지방대사 질환의 예방 및 치료에 이용될 수 있다. 화학식 1에서 R
1 은 선형 또는 분지형 C
1 -C
6 알킬기, 또는 사이클로알킬기, 또는 치환기를 갖거나 갖지 않는 페닐기를 의미하고, R
2 는 치환기를 가지거나 가지지 않는 방향족기를 의미한다.

公开(公告)号：KR1020120025903A

公开(公告)日：2012-03-16

申请号：KR1020100088083

申请日：2010-09-08

Applicant: (주)아모레퍼시픽

Inventor： 백흥수 ,  우병영 ,  신송석 ,  이종석 ,  오미현 ,  주영협

IPC: C07D241/44 ,  A61K9/00 ,  A61K47/06 ,  A61L31/16

CPC classification number: C07D241/44 ,  A61K9/0056 ,  A61K47/06 ,  A61L31/16

Abstract: PURPOSE: A novel quinoxaline compound, isomer thereof, precursor drug thereof, or pharmaceutically acceptable salt thereof is provided to absorb UVA and UVB. CONSTITUTION: A quinoxaline compound is denoted by chemical formula 1. An UV absorber or pharmaceutical or cosmetic composition for antiaging contains the quinoxaline compound, isomer thereof, precursor drug thereof, or pharmaceutically acceptable salt, hydrate, or solvate thereof as an active ingredient.

Abstract translation: 目的：提供一种新的喹喔啉化合物，其异构体，其前体药物或其药学上可接受的盐以吸收UVA和UVB。 构成：喹喔啉化合物由化学式1表示。用于抗衰老的紫外线吸收剂或药物或化妆品组合物含有喹喔啉化合物，其异构体，其前体药物或其药学上可接受的盐，水合物或溶剂化物作为活性成分。

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：KR1020100103671A

公开(公告)日：2010-09-27

申请号：KR1020107017557

申请日：2008-12-03

Applicant: (주)아모레퍼시픽

Inventor： 박미영 ,  김연준 ,  최진규 ,  이기화 ,  김선영 ,  고현주 ,  우병영 ,  이은경 ,  신동욱 ,  이형호 ,  이태룡 ,  임경민

IPC: A61K31/15 ,  A61P3/02 ,  A61P3/10

CPC classification number: A61K31/15

Abstract: PURPOSE: A pharmaceutical composition containing 2-cyclopentene-1-one oxime derivative is provided to promote adipose lysis in adipocytes(3T3-L1) and to prevent and treat lipid metabolic diseases including obesity and diabetes. CONSTITUTION: A pharmaceutical composition for preventing and treating lipid metabolic diseases contains 2-cyclopenten-1-one oxime derivative compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. In chemical formula 1, R1 is linear or branched C1-C10 alkyl group or C3-C7 cycloalkyl group, or phenyl group with or without substituent. The phenyl group is denoted by chemical formula 2. The pharmaceutical composition is used for preventing and treating obesity, diabetes, or dyslipidemia.

Abstract translation: 目的：提供含有2-环戊烯-1-酮肟衍生物的药物组合物，以促进脂肪细胞（3T3-L1）中的脂肪裂解，并预防和治疗脂肪代谢疾病，包括肥胖和糖尿病。 构成：用于预防和治疗脂质代谢疾病的药物组合物含有化学式1的2-环戊烯-1-酮肟衍生物化合物或其药学上可接受的盐作为活性成分。 在化学式1中，R 1为直链或支链C 1 -C 10烷基或C 3 -C 7环烷基，或具有或不具有取代基的苯基。 苯基由化学式2表示。药物组合物用于预防和治疗肥胖症，糖尿病或血脂异常。

公开(公告)号：KR1020100061401A

公开(公告)日：2010-06-07

申请号：KR1020090115960

申请日：2009-11-27

Applicant: (주)아모레퍼시픽

Inventor： 이기화 ,  전재일 ,  홍덕기 ,  우병영 ,  이영란

IPC: C07D487/04 ,  A61K47/10 ,  A61K47/26 ,  A61K9/00

CPC classification number: A61K9/08 ,  A61K9/20 ,  C07D487/04 ,  A61K9/0019 ,  A61K47/10 ,  A61K47/26

Abstract: PURPOSE: A crystalline form of adefovir dipivoxil, and a virus infection prevention and treatment pharmaceutical composition containing thereof are provided to secure the excellent living-body safety, solubility and dissolution velocity. CONSTITUTION: A crystalline form of adefovir dipivoxil is in a form of an ethyl alcohol solvent containing 0.3~0.7 equivalent of ethyl alcohol within the crystal lattice. The crystalline form of the adefovir dipivoxil has peaks of when measuring by the X-ray powder diffraction method at the 2 theta diffraction angle. The melting point of the crystalline form of the adefovir dipivoxil is 64~68 deg C and 76~80 deg C. A virus infection prevention and treatment pharmaceutical composition includes the crystalline form of the adefovir dipivoxil.

Abstract translation: 目的：提供阿德福韦酯的结晶形式和含有其的病毒感染预防和治疗药物组合物，以确保优异的活体安全性，溶解度和溶解速度。 构成：阿德福韦酯的结晶形式是在晶格内含有0.3〜0.7当量乙醇的乙醇溶剂形式。 当通过X射线粉末衍射法在2θ衍射角测量时，阿德福韦酯的结晶形式具有峰值。 阿德福韦酯的结晶形式的熔点为64〜68℃，76〜80℃。病毒感染预防和治疗药物组合物包括阿德福韦酯的结晶形式。

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：KR1020080052024A

公开(公告)日：2008-06-11

申请号：KR1020060123982

申请日：2006-12-07

Applicant: (주)아모레퍼시픽 ,  크리스탈지노믹스(주) ,  연세대학교 산학협력단

Inventor： 홍용덕 ,  강승현 ,  김연준 ,  변경희 ,  우병영 ,  박미영 ,  주영협 ,  김정주 ,  장두옥 ,  태진성 ,  신동규 ,  김용은 ,  천영훈 ,  이재일 ,  현영란 ,  노성구 ,  조중명

IPC: C07D487/04 ,  A61K31/4162

CPC classification number: C07D487/04

Abstract: Triazolopyridazine derivatives are provided to inhibit acetyl-CoA carboxylase 2(ACC2), so that the compounds are useful for prevention and treatment of obesity, diabetes, hyperlipidemia and metabolic syndrome-related disease. Triazolopyridazine derivatives represented by the formula(1) have inhibitory effects on acetyl-CoA carboxylase 2, wherein X is hydrogen, pyridyl, thiophenyl, furanyl or phenyl optionally substituted by C1-5 alkyl, C1-5 alkoxy, hydroxy or halogen; Y is pyridine, thiophene or NHR2; Z is O, S, NH, methylene, ethylene or -CH(CH3)-; R1 is methyl, hydroxy or hydroxy methyl; R2 is hydrogen, C1-7 alkyl, C3-8 cycloalkyl optionally substituted by hydroxy or C1-7 alkyl, or phenyl optionally substituted by C1-5 alkyl; R3 is hydrogen, hydroxy, C1-5 alkyl, C1-5 alkoxy or halogen; R4 is hydrogen, hydroxy, C1-5 alkyl, C1-5 alkoxy, trifluoromethyl, C1-5 alkoxycarbonyl or halogen; and W is bond, C1-2 alkylene, alkenylene or alkynylene.

Abstract translation: 提供三唑并哒嗪衍生物以抑制乙酰辅酶A羧化酶2（ACC2），使得该化合物可用于预防和治疗肥胖症，糖尿病，高脂血症和代谢综合征相关疾病。 由式（1）表示的三唑并哒嗪衍生物对乙酰辅酶A羧化酶2具有抑制作用，其中X为氢，吡啶基，噻吩基，呋喃基或任选被C 1-5烷氧基，羟基或卤素取代的苯基; Y为吡啶，噻吩或NHR2; Z是O，S，NH，亚甲基，亚乙基或-CH（CH 3） - ; R1是甲基，羟基或羟基甲基; R 2为氢，C 1-7烷基，任选被羟基或C 1-7烷基取代的C 3-8环烷基，或任选被C 1-5烷基取代的苯基; R3是氢，羟基，C1-5烷基，C1-5烷氧基或卤素; R4是氢，羟基，C1-5烷基，C1-5烷氧基，三氟甲基，C1-5烷氧基羰基或卤素; W是键，C1-2亚烷基，亚烯基或亚炔基。

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。