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：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。

公开(公告)号：KR1020170081315A

公开(公告)日：2017-07-12

申请号：KR1020160000212

申请日：2016-01-04

Applicant: (주)아모레퍼시픽

Inventor： 우병영 ,  이기화 ,  노종화 ,  박제홍 ,  박미영 ,  박영호

IPC: C07C303/36 ,  C07C311/08 ,  C07D213/26 ,  C07D213/61

CPC classification number: C07C303/36 ,  C07C311/08 ,  C07D213/26 ,  C07D213/61

Abstract: 본명세서는비대칭탄소원자에아민기가결합된화합물의입체이성질체혼합물을카이랄보조체와혼합시키는단계를포함하는입체이성질체혼합물의카이랄분할방법에관한것이다. 이때, 카이랄보조체는 2,3-디벤조일-타르타르산또는-디--톨루오일타르타르산이고, 이러한방법에의하면높은수준의광학순도를가지는광학이성질체를얻는것이가능하다. 또한, 이러한방법에의하면광학이성질체를회수하여모액에포함된입체이성질체혼합물의비율을조절하는것이가능하다. 따라서, 본발명의일 측면에따른방법은약학또는제약분야에서단일한형태의광학이성질체를가지는화합물을높은순도로수득하고자하는경우에유용하게사용될수 있으며, 다른반응에서사용된모액을라세미화하는데유용하게사용될수 있다.

Abstract translation: [0011]本申请公开了胺基团键合到的不对称碳原子以立体异构体混合物的手性拆分方法，包括手性辅助体和混合的步骤的化合物的立体异构混合物。 在这种情况下，手性辅助体是2,3-二苯甲酰基 - 它能够获得甲苯甲酰酒石酸，根据该方法具有高度的光学纯度的光学异构体 - 酒石酸或α-d。 另外，根据该方法，可以回收光学异构体以控制母液中所含立体异构体混合物的比例。 因此，根据本发明的一方面，该方法可有效地，如果期望得到具有单一hanhyeongtae在药物或药物与高纯度的光学异构体，对母液中的不同反应中使用的外消旋化有用的化合物采用 它可以被使用。

公开(公告)号：KR101567571B1

公开(公告)日：2015-11-11

申请号：KR1020107017553

申请日：2008-12-03

Applicant: (주)아모레퍼시픽

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

IPC: A61K8/40 ,  A61K8/30 ,  A61K8/34 ,  A61Q19/00

CPC classification number: A61K31/15

Abstract: 화학식 1로나타내어지는 2-사이클로펜텐-1-온옥심유도체를포함하는슬리밍화장료조성물이개시된다. 구체적으로상기화합물은분화된지방세포 (3T3-L1)에서의지방분해를촉진시켜결과적으로체내지방을감소시킴으로써, 슬리밍과같은미용목적으로이용될수 있다. 화학식 1에서 R은선형또는분지형 C-C알킬기, 또는사이클로알킬기, 또는치환기를갖거나갖지않는페닐기를의미하고, R는치환기를갖거나갖지않는방향족기를의미한다.