公开(公告)号：US07009053B2

公开(公告)日：2006-03-07

申请号：US10493706

申请日：2003-04-30

申请人： Sung-Gyu Kim ,  Yoon Sung Jung ,  Jae Yang Kong ,  Woo Kyu Park

发明人： Sung-Gyu Kim ,  Yoon Sung Jung ,  Jae Yang Kong ,  Woo Kyu Park

IPC分类号： C07D215/38 ,  C07D215/44 ,  A61K31/47

CPC分类号： C07D409/12 ,  C07D215/42 ,  C07D215/44 ,  C07D215/54 ,  C07D401/12 ,  C07D405/12

摘要： The present invention relates to new quinoline derivatives of formula (1) or their pharmaceutically acceptable salts with caspase-3 inhibitory activity and their preparation methods, wherein R2 is H; halogen; C1-6alkyl; C1-6 alkoxy; C1-6 alkoxyalkyl; or C3-6cycloalkyl; R1 is formula (a); —CN; or formula (b); R is H; C6-14aryl unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; 5–15 membered heterocyclic group unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; or —(CH2)n—CHR4R5. The present invention relates to a pharmaceutical composition for treating caspase-associated diseases by inhibiting the activity of caspase-3 which comprises the compound of formula (1) or its pharmaceutically acceptable salt.

摘要翻译： 本发明涉及式（1）的新喹啉衍生物或其与胱天蛋白酶-3抑制活性的药学上可接受的盐及其制备方法，其中R 2为H; 卤素; C 1-6烷基; C 1-6烷氧基; C 1-6烷氧基烷基; 或C 3-6环烷基; R 1是式（a）; -CN; 或式（b）; R为H; 未取代的或被卤素C 1-6烷基，C 1-6烷氧基或氨基取代的C 6-14芳基; 未取代或被卤素取代的5-15元杂环基，C 1-6烷基，C 1-6烷氧基或氨基; 或 - （CH 2）n-CHR 4 R 5 5。 本发明涉及通过抑制胱天蛋白酶-3的活性来治疗半胱氨酸蛋白酶相关疾病的药物组合物，其包含式（1）化合物或其药学上可接受的盐。

公开(公告)号：US08236806B2

公开(公告)日：2012-08-07

申请号：US12530312

申请日：2007-07-13

申请人： Jae Yang Kong ,  Woo-Kyu Park ,  Heeyeong Cho ,  Daeyoung Jeong ,  Gildon Choi ,  Hun Yeong Koh ,  Sang Hee Kim ,  Ae Nim Pae ,  Yong Seo Cho ,  Joo Hwan Cha ,  Hyunah Choo ,  Sang Eun Chae ,  Hee-Yoon Lee

发明人： Jae Yang Kong ,  Woo-Kyu Park ,  Heeyeong Cho ,  Daeyoung Jeong ,  Gildon Choi ,  Hun Yeong Koh ,  Sang Hee Kim ,  Ae Nim Pae ,  Yong Seo Cho ,  Joo Hwan Cha ,  Hyunah Choo ,  Sang Eun Chae ,  Hee-Yoon Lee

IPC分类号： A61K31/496 ,  C07D231/12 ,  C07D401/04 ,  C07D409/04

CPC分类号： C07D403/06

摘要： The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

摘要翻译： 本发明涉及一种新的哌嗪基 - 丙基 - 吡唑衍生物，其制备方法和包含其的药学上可接受的组合物。 本发明的新型哌嗪基 - 丙基 - 吡唑衍生物对多巴胺D4受体具有优异的选择性亲和力，可有效抑制阿扑吗啡诱导的精神病性行为（笼养），并在小鼠旋转试验中具有较低的不良反应。 因此，它可以被开发为用于治疗和预防中枢神经系统（CNS）障碍，特别是精神分裂症，注意缺陷多动障碍，抑郁症，压力疾病，恐慌症，恐惧症，强迫症，创伤后疼痛的治疗剂 压力障碍，认知障碍，阿尔茨海默病，帕金森病，焦虑症，过敏性反应，躁狂症，癫痫发作，人格障碍，偏头痛，药物成瘾，酒精成瘾，肥胖，进食障碍和睡眠障碍。

公开(公告)号：US08372844B2

公开(公告)日：2013-02-12

申请号：US13454817

申请日：2012-04-24

申请人： Jae Yang Kong ,  Woo-Kyu Park ,  Heeyeong Cho ,  Daeyoung Jeong ,  Gildon Choi ,  Hun Yeong Koh ,  Sang Hee Kim ,  Ae Nim Pae ,  Yong Seo Cho ,  Joo Hwan Cha ,  Hyunah Choo ,  Sang Eun Chae ,  Hee-Yoon Lee

发明人： Jae Yang Kong ,  Woo-Kyu Park ,  Heeyeong Cho ,  Daeyoung Jeong ,  Gildon Choi ,  Hun Yeong Koh ,  Sang Hee Kim ,  Ae Nim Pae ,  Yong Seo Cho ,  Joo Hwan Cha ,  Hyunah Choo ,  Sang Eun Chae ,  Hee-Yoon Lee

IPC分类号： A61K31/496 ,  C07D231/12 ,  C07D401/04 ,  C07D409/04

CPC分类号： C07D403/06

摘要： The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

摘要翻译： 本发明涉及一种新的哌嗪基 - 丙基 - 吡唑衍生物，其制备方法和包含其的药学上可接受的组合物。 本发明的新型哌嗪基 - 丙基 - 吡唑衍生物对多巴胺D4受体具有优异的选择性亲和力，可有效抑制阿扑吗啡诱导的精神病性行为（笼养），并在小鼠旋转试验中具有较低的不良反应。 因此，它可以被开发为用于治疗和预防中枢神经系统（CNS）障碍，特别是精神分裂症，注意缺陷多动障碍，抑郁症，压力疾病，恐慌症，恐惧症，强迫症，创伤后疼痛的治疗剂 压力障碍，认知障碍，阿尔茨海默病，帕金森病，焦虑症，过敏性反应，躁狂症，癫痫发作，人格障碍，偏头痛，药物成瘾，酒精成瘾，肥胖，进食障碍和睡眠障碍。

公开(公告)号：US20100063286A1

公开(公告)日：2010-03-11

申请号：US12530312

申请日：2007-07-13

申请人： Jae Yang Kong ,  Woo-Kyu Park ,  Heeyeong Cho ,  Daeyoung Jeong ,  Gildon Choi ,  Hun Yeong Koh ,  Sang Hee Kim ,  Ae Nim Pae ,  Yong Seo Cho ,  Joo Hwan Cha ,  Hyunah Choo ,  Sang Eun Chae ,  Hee-Yoon Lee

发明人： Jae Yang Kong ,  Woo-Kyu Park ,  Heeyeong Cho ,  Daeyoung Jeong ,  Gildon Choi ,  Hun Yeong Koh ,  Sang Hee Kim ,  Ae Nim Pae ,  Yong Seo Cho ,  Joo Hwan Cha ,  Hyunah Choo ,  Sang Eun Chae ,  Hee-Yoon Lee

IPC分类号： C07D403/06

CPC分类号： C07D403/06

摘要： The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

摘要翻译： 本发明涉及一种新的哌嗪基 - 丙基 - 吡唑衍生物，其制备方法和包含其的药学上可接受的组合物。 本发明的新型哌嗪基 - 丙基 - 吡唑衍生物对多巴胺D4受体具有优异的选择性亲和力，可有效抑制阿扑吗啡诱导的精神病性行为（笼养），并在小鼠旋转试验中具有较低的不良反应。 因此，它可以被开发为用于治疗和预防中枢神经系统（CNS）障碍，特别是精神分裂症，注意缺陷多动障碍，抑郁症，压力疾病，恐慌症，恐惧症，强迫症，创伤后疼痛的治疗剂 压力障碍，认知障碍，阿尔茨海默病，帕金森病，焦虑症，过敏性反应，躁狂症，癫痫发作，人格障碍，偏头痛，药物成瘾，酒精成瘾，肥胖，进食障碍和睡眠障碍。

公开(公告)号：US5990126A

公开(公告)日：1999-11-23

申请号：US52752

申请日：1998-03-31

申请人： No Sang Park ,  Churl Min Seong ,  Young Sik Jung ,  Jin Il Choi ,  Chang Woo Lee ,  Yong Jun Chung ,  Seung Won Choi ,  Jae Yang Kong ,  Woo Kyu Park

发明人： No Sang Park ,  Churl Min Seong ,  Young Sik Jung ,  Jin Il Choi ,  Chang Woo Lee ,  Yong Jun Chung ,  Seung Won Choi ,  Jae Yang Kong ,  Woo Kyu Park

IPC分类号： A61K31/47 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D215/22

CPC分类号： C07D401/12 ,  C07D215/36 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： A class of quinolinic sulfide derivatives of formula I are potent and specific antagonists at the strychnine insensitive glycine bitding site on the NMDA receptor complex with an pharmacological advantageous profile. They may be useful in treatment or prevention of neuro-degenerative disorders. Particularly, the compounds included in the present invention are especially useful for minimizing damage of the central nervous system arising as a consequence of ischemic or hypoxic condition such as stroke, hypoglycemia, cerebral ischemia, cardiac arrest, and physical trauma. They are also useful in prevention of chronic neurodegenerative disorders including epilepsy, Alzheimer's disease, Huntington's disease and Parkinsonism. By virtue of their NMDA receptor antagonist properties, the present compounds may also use as anticonvulsant, analgesic, antidepressant, anxiolytic, and antischizophrenic agent. Formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R are defined in specification.

摘要翻译： 一类式I的喹啉硫化物衍生物是具有药理学优点的NMDA受体复合物上的士的宁不敏感甘氨酸位点处的有效和特异性拮抗剂。 它们可用于治疗或预防神经退行性疾病。 特别地，本发明中包括的化合物特别可用于使由于中风，低血糖，脑缺血，心跳停止和身体创伤等缺血或缺氧状况而引起的中枢神经系统的损伤最小化。 它们也可用于预防慢性神经变性障碍，包括癫痫，阿尔茨海默病，亨廷顿病和帕金森综合征。 由于其NMDA受体拮抗剂性质，本发明化合物也可用作抗惊厥药，镇痛药，抗抑郁药，抗焦虑药和抗精神分裂剂。 其中R1，R2，R3，R4和R在说明书中定义。

公开(公告)号：US20100145043A1

公开(公告)日：2010-06-10

申请号：US12570492

申请日：2009-09-30

申请人： Young-Dae Gong ,  Taeho Lee ,  Moon-Kook Jeon ,  Heeyeong Cho ,  Jae Yang Kong ,  Gildon Choi ,  Dae Young Jeong ,  Soon-Hee Hwang

发明人： Young-Dae Gong ,  Taeho Lee ,  Moon-Kook Jeon ,  Heeyeong Cho ,  Jae Yang Kong ,  Gildon Choi ,  Dae Young Jeong ,  Soon-Hee Hwang

IPC分类号： C07D417/14 ,  C07D417/04 ,  C07D277/56

CPC分类号： C07D277/56 ,  C07D417/04 ,  C07D417/12

摘要： Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R1, R2, R3 and R4 are as defined in the specification.

摘要翻译： 本文公开了2,4-二取代-5-氨基羰基-1,3-噻唑衍生物，其制备方法和用于治疗由SPC诱导的炎症性疾病的治疗剂，其含有该衍生物作为活性成分。 通过使用人真皮细胞的试验和使用小鼠的动物试验分析2,4-二取代-5-氨基羰基-1,3-噻唑衍生物的抗炎作用，结果发现衍生物 与现有技术中已知的噻唑衍生物相比，对SPC受体显示出优异的抑制活性。 因此，2,4-二取代-5-氨基羰基-1,3-噻唑衍生物或其药学上可接受的盐可用作用于治疗炎性疾病如炎症，瘙痒和皮肤感染的治疗剂中的活性成分，其出现在特应性 皮炎和其他由SPC活动引起的疾病。 其中R1，R2，R3和R4如说明书中所定义。

公开(公告)号：US06716857B2

公开(公告)日：2004-04-06

申请号：US10273630

申请日：2002-10-18

申请人： Youseung Kim ,  Soon Bang Kang ,  Gyochang Keum ,  Min Seok Jang ,  Jae Yang Kong ,  Dae Young Jeong

发明人： Youseung Kim ,  Soon Bang Kang ,  Gyochang Keum ,  Min Seok Jang ,  Jae Yang Kong ,  Dae Young Jeong

IPC分类号： A61K3144

CPC分类号： C07D401/06

摘要： The present invention relates to novel tetrahydropyridine derivatives of formula 1 having an appropriately substituted pyrrolidinone and oxime, wherein m is 0 or 1, n is 1 or 2, R1 is hydrogen, C1-4alkyl, C2-4 alkynyl or aryl, R3 is C1-4 alkyl, which show high efficacy, low cholinergic adverse effects and high affinity for muscarinic acetylcholine receptor; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.

摘要翻译： 本发明涉及具有适当取代的吡咯烷酮和肟的式1的新的四氢吡啶衍生物，其中m为0或1，n为1或2，R 1为氢，C 1-4烷基，C 2-4炔基或芳基， R 3是C 1-4烷基，其显示出高效力，低胆碱能不良反应和对毒蕈碱性乙酰胆碱受体的高亲和力; 及其药学上可接受的盐; 制备方法; 和包含这些化合物或盐的药物组合物。

公开(公告)号：US20110135714A1

公开(公告)日：2011-06-09

申请号：US13016682

申请日：2011-01-28

申请人： Byung Cheol SHIN ,  Hasoo Seong ,  Aeri Lee ,  Jae Yang Kong ,  Hyae Gyeong Cheon ,  Young Sik Cho ,  Sung Soo Jun ,  Young Gwan Jo

发明人： Byung Cheol SHIN ,  Hasoo Seong ,  Aeri Lee ,  Jae Yang Kong ,  Hyae Gyeong Cheon ,  Young Sik Cho ,  Sung Soo Jun ,  Young Gwan Jo

IPC分类号： A61K31/714 ,  A61K9/127 ,  A61P17/00

CPC分类号： A61K31/714 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/127 ,  A61K9/7023 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to a composition for external application for improving a skin disease (e.g. psoriasis). The composition contains adenosyl cobalamin (coenzyme B12), optionally in admixture with other cobalamins. The composition can be present in the form of liposomal preparations, which are made of a phospholipid and cholesterol.

摘要翻译： 本发明涉及用于改善皮肤病（例如牛皮癣）的外用组合物。 该组合物含有腺苷钴胺素（辅酶B12），任选与其它钴胺素混合。 组合物可以以由磷脂和胆固醇制成的脂质体制剂的形式存在。

公开(公告)号：US06759419B2

公开(公告)日：2004-07-06

申请号：US10273643

申请日：2002-10-18

申请人： Youseung Kim ,  Soon Bang Kang ,  Gyochang Keum ,  Min Seok Jang ,  Jae Yang Kong ,  Dae Young Jeong ,  Taeg-Su Jang

发明人： Youseung Kim ,  Soon Bang Kang ,  Gyochang Keum ,  Min Seok Jang ,  Jae Yang Kong ,  Dae Young Jeong ,  Taeg-Su Jang

IPC分类号： A61K31445

CPC分类号： C07D413/14

摘要： The present invention relates to substituted pyrrolidinone compounds of formula 1, wherein n is 0 or 1; Aza is a heterocycle optionally substituted with C1-4 alkyl, or C1-4 alkyl substituted with a heterocycle, which represents a saturated or unsaturated five- or six-membered ring having nitrogen(s) as a heteroatom, which are muscarinic acetylcholine receptor agonists and useful as nootropics and therapeutic agents for cerebral neural diseases such as Alzheimer's disease; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.

摘要翻译： 本发明涉及式1的取代吡咯烷酮化合物，其中n为0或1; 氮杂是任选被C 1-4烷基取代的杂环，或被杂环取代的C 1-4烷基，其表示饱和或不饱和的具有氮（S）杂原子的五元或六元环，它们是毒蕈碱性乙酰胆碱受体激动剂 并且可用作脑神经疾病如阿尔茨海默病的神经调节剂和治疗剂; 及其药学上可接受的盐; 制备方法; 和包含这些化合物或盐的药物组合物。

公开(公告)号：US06673800B2

公开(公告)日：2004-01-06

申请号：US09838253

申请日：2001-04-20

申请人： Hun Yeong Koh ,  Kyung Il Choi ,  Yong Seo Cho ,  Ae Nim Pae ,  Jae Yang Kong ,  Dae Young Jeong ,  Sun Ho Jung ,  Ji Young Jung ,  Hee-Yoon Lee

发明人： Hun Yeong Koh ,  Kyung Il Choi ,  Yong Seo Cho ,  Ae Nim Pae ,  Jae Yang Kong ,  Dae Young Jeong ,  Sun Ho Jung ,  Ji Young Jung ,  Hee-Yoon Lee

IPC分类号： A61K31496

CPC分类号： C07D413/04 ,  C07D261/08

摘要： The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, X and n are the same as defined in the specification.

摘要翻译： 本发明涉及在下列通式（1）表示的多巴胺D3和D4受体中具有选择性生物活性的4,5-二氢异恶唑基烷基哌嗪衍生物及其还原胺还原胺化反应的制备方法，其中R1，R2， X和n与说明书中定义的相同。