公开(公告)号：KR1020130103461A

公开(公告)日：2013-09-23

申请号：KR1020130092770

申请日：2013-08-05

Applicant: 한국과학기술연구원

Inventor： 노은주 ,  신계정 ,  이창준 ,  오수진 ,  박정은 ,  양정은 ,  황은미 ,  우동호 ,  이순혁 ,  김동규 ,  전희정 ,  지완근 ,  나윤수

IPC: C07D403/06 ,  C07D403/12 ,  A61K31/497 ,  A61P25/00

Abstract: PURPOSE: A phenoxypropanol derivative is provided to effectively suppress T-type calcium channel or TWIK-related K+ (TREK)-1 channel, thereby treating various diseases caused by the activation of the channels. CONSTITUTION: A phenoxypropanol derivative of chemical formula I or a racemic body, a pharmaceutically acceptable salt, a solvate, or a hydrate thereof is provided. A pharmaceutical composition for preventing or treating diseases related to T-type calcium channel or TREK-1 channel, selected among Parkinson's disease, Alzheimer's disease, schizophrenia, sleep disorder, epilepsy, pain, hypertension, arrhythmia, ventricular hypertrophy, angina pectoris, heart failure, myocardial infarction, cancer, hypoxia, cerebral ischemia, alkalemia, and depression contains the phenoxypropanol derivative, the racemic body, the pharmaceutically acceptable salt, the solvate, or the hydrate as an active ingredient. A method for suppressing T-type calcium channel or TREK-1 channel comprises the steps of: preparing a biological sample from an organ; and applying the phenoxypropanol derivative, the racemic body, the pharmaceutically acceptable salt, the solvate, or the hydrate to the biological sample.

Abstract translation: 目的：提供苯氧基丙醇衍生物，有效抑制T型钙通道或TWIK相关K +（TREK）-1通道，从而治疗由通道激活引起的各种疾病。 构成：提供化学式I的苯氧基丙醇衍生物或外消旋体，其药学上可接受的盐，溶剂化物或其水合物。 用于预防或治疗与帕金森病，阿尔茨海默病，精神分裂症，睡眠障碍，癫痫，疼痛，高血压，心律失常，心室肥大，心绞痛，心力衰竭有关的T型钙通道或TREK-1通道相关疾病的药物组合物 ，心肌梗死，癌症，缺氧，脑缺血，碱血症和抑郁症含有苯氧基丙醇衍生物，外消旋体，药学上可接受的盐，溶剂合物或水合物作为活性成分。 抑制T型钙通道或TREK-1通道的方法包括以下步骤：从器官制备生物样品; 以及将所述苯氧基丙醇衍生物，外消旋体，药学上可接受的盐，溶剂合物或水合物施用于生物样品。

公开(公告)号：KR1020130088988A

公开(公告)日：2013-08-09

申请号：KR1020120010286

申请日：2012-02-01

Applicant: 한국과학기술연구원

Inventor： 노은주 ,  박정은 ,  송치만 ,  한호규 ,  정찬성 ,  남기달 ,  심태보

IPC: C07D209/08 ,  C07D207/18 ,  A61K31/403 ,  A61P25/00

Abstract: PURPOSE: A novel compound is provided to suppress triple reuptake by blocking serotonin, norepinephrine, and dopamine. CONSTITUTION: A compound selected among (1S,3aR,9bS)-1-phenyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole derivatives and pharmaceutically acceptable salts thereof is denoted by chemical formula 1. The compound is selected among (1S,3aR,9bS)-9-chloro-1-phenyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole, (1S,3aR,9bS)-8-chloro-1-phenyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole, (1S,3aR,9bS)-7-chloro-1-phenyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole, (1S,3aR,9bS)-7,8-dichloro-1-phenyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole, and pharmaceutically acceptable salts thereof. A pharmaceutical composition for preventing and treating depression contains the compound as an active ingredient.

Abstract translation: 目的：通过阻断5-羟色胺，去甲肾上腺素和多巴胺来提供新的化合物来抑制三重再摄取。 构成：选自（1S，3aR，9bS）-1-苯基-2,3,3a，4,5,9b-六氢-1H-苯并[e]吲哚衍生物及其药学上可接受的盐的化合物由化学式 该化合物选自（1S，3aR，9bS）-9-氯-1-苯基-2,3,3a，4,5,9b-六氢-1H-苯并[e]吲哚，（1S，3aR， 9bS）-8-氯-1-苯基-2,3,3a，4,5,9b-六氢-1H-苯并[e]吲哚，（1S，3aR，9bS）-7-氯-1-苯基-2 ，3,3a，4,5,9b-六氢-1H-苯并[e]吲哚，（1S，3aR，9bS）-7,8-二氯-1-苯基-2,3,3a，4,5,9b 六氢-1H-苯并[e]吲哚及其药学上可接受的盐。 用于预防和治疗抑郁症的药物组合物含有作为活性成分的化合物。

公开(公告)号：KR1020130060799A

公开(公告)日：2013-06-10

申请号：KR1020110127053

申请日：2011-11-30

Applicant: 한국과학기술연구원

Inventor： 노은주 ,  신계정 ,  이창준 ,  오수진 ,  박정은 ,  양정은 ,  황은미 ,  우동호 ,  이순혁 ,  김동규 ,  전희정 ,  지완근 ,  나윤수

IPC: C07D403/06 ,  A61K31/496 ,  A61P25/00

CPC classification number: C07D295/15 ,  C07D211/22 ,  C07D211/38 ,  C07D211/52 ,  C07D211/58 ,  C07D231/40 ,  C07D233/64 ,  C07D295/088 ,  C12N5/0686 ,  C12N2501/999

Abstract: PURPOSE: A phenoxy propanol derivative is provided to effectively suppress T-type calcium channel or TREK(TWIK-related K+)-1 channel and to treat various diseases. CONSTITUTION: A pharmaceutical composition for preventing or treating diseases related to T-type calcium channel or TREK-1 channel contains a phenoxy propanol derivative with a structure of chemical formula I or a racemic body, a pharmaceutically acceptable salt, solvent, or hydrate thereof as an active ingredient. A method for suppressing the T-type calcium channel or TREK-1 channel comprises: a step of preparing a biological sample from organism; and a step of applying the phenoxy propanol derivative, or a racemic body, a pharmaceutically acceptable salt, solvate, or hydrate thereof.

Abstract translation: 目的：提供苯氧丙醇衍生物，有效抑制T型钙通道或TREK（TWIK相关K +）-1通道，治疗各种疾病。 构成：用于预防或治疗与T型钙通道或TREK-1通道有关的疾病的药物组合物含有具有化学式I结构的苯氧基丙醇衍生物或其外消旋体，其药学上可接受的盐，溶剂或水合物作为 活性成分。 抑制T型钙通道或TREK-1通道的方法包括：从生物体制备生物样品的步骤; 以及施用苯氧基丙醇衍生物或外消旋体，其药学上可接受的盐，溶剂合物或水合物的步骤。