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：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。