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1. 发明申请

WO1998015556A1 TRICYCLIC COMPOUNDS HAVING ACTIVITY AS Ras-FPT INHIBITORS 审中-公开
标题翻译：具有作为Ras-FPT抑制剂的活性的三元化合物
公开(公告)号：WO1998015556A1
公开(公告)日：1998-04-16
申请号：PCT/US1997017314
申请日：1997-10-07
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , AFONSO, Adriano , KELLY, Joseph, M. , ROSENBLUM, Stuart , WOLIN, Ronald, L. , WEINSTEIN, Jay
IPC分类号： C07D491/044
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： Compounds of formula (I), wherein: X is hydrogen, halogen, CF3, nitro, NH2 or lower alkyl; each X is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl; n is 1 or 2; Y is selected from the group consisting of S(O)p, O, and NR , wherein p is 0, 1 or 2, and R is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl; R and R , which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR ; A ..... is C=, CH- or N-; R is -CZ-Y -Y -R , wherein: Z is O, =CH-CN, or =N-CN; one of Y and Y is a bond, -CO-, O, S, or -NR -, and the other is (CH2)m, where m is 0 or an integer of 1 to 4, and R is H or alkyl, with the previso that when Z is O and m is 0 then Y or Y is selected form -CO-, O, S, or -NR ; R is aryl, heteroaryl or heterocycloalkyl, with proviso that R can also be lower alkyl when Z is =N-CN; and their pharmaceutically acceptable acid additions salts; have activity as Ras-FPT inhibitors. They can be used, e.g., in pharmaceutical compositions, for inhibiting the abnormal growth of cells and for inhibiting proliferative diseases. Processes for their preparation, and useful intermediates, are also disclosed.
摘要翻译：式（I）的化合物，其中：X 1是氢，卤素，CF 3，硝基，NH 2或低级烷基; 每个X 2独立地选自氢，卤素，低级烷氧基和低级烷基; n为1或2; Y选自S（O）p，O和NR 5，其中p为0,1或2，R 5为氢，烷基，芳基，环烷基，低级烷氧基羰基，氨基羰基或酰基 ; R 1和R 2可以相同或不同，选自氢和低级烷基，或者当Y是NR 5时可以一起形成氧原子; A 是C =，CH-或N-; R是-CZ-Y 1 -Y 2 -R 3，其中：Z是O，= CH-CN或= N-CN; Y 1和Y 2之一是键，-CO-，O，S或-NR 4 - ，另一个是（CH 2）m，其中m是0或1〜 4和R 4是H或烷基，其中当Z是O且m是0时，Y 1或Y 2选自-CO-，O，S或-NR 4 >; R 3是芳基，杂芳基或杂环烷基，条件是当Z = N-CN时，R 3也可以是低级烷基; 及其药学上可接受的酸加成盐; 具有作为Ras-FPT抑制剂的活性。它们可以用于例如药物组合物中，用于抑制细胞的异常生长和抑制增殖性疾病。还公开了它们的制备方法和有用的中间体。

2. 发明申请

WO2007084319A2 DIARYL PIPERIDINES AS CB1 MODULATORS 审中-公开
标题翻译： DIARYL PIPERIDINES作为CB1调节剂
公开(公告)号：WO2007084319A2
公开(公告)日：2007-07-26
申请号：PCT/US2007/000705
申请日：2007-01-11
申请人： SCHERING CORPORATION , SCOTT, Jack, D. , WEINSTEIN, Jay , MILLER, Michael, W. , STAMFORD, Andrew, W. , GILBERT, Eric, J. , XIA, Yan , GREENLEE, William, J. , LI, Wei
发明人： SCOTT, Jack, D. , WEINSTEIN, Jay , MILLER, Michael, W. , STAMFORD, Andrew, W. , GILBERT, Eric, J. , XIA, Yan , GREENLEE, William, J. , LI, Wei
CPC分类号： C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/58 , C07D211/60 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/10
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome (e.g., obesity, waist circumference, lipid profile, and insulin sensitivity), neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：具有通式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗疾病，病症或病症，例如代谢综合征（例如肥胖症，腰围，血脂分布和胰岛素敏感性），神经炎症疾病，认知障碍，精神病，成瘾行为，胃肠疾病和心血管疾病。

3. 发明申请

WO2006060461A1 SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 审中-公开
标题翻译：取代的PIPERAZINES作为CB1拮抗剂
公开(公告)号：WO2006060461A1
公开(公告)日：2006-06-08
申请号：PCT/US2005/043281
申请日：2005-12-01
申请人： SCHERING CORPORATION , GILBERT, Eric, J. , MILLER, Michael, W. , SCOTT, Jack, D. , STAMFORD, Andrew, W. , GREENLEE, William, J. , WEINSTEIN, Jay
发明人： GILBERT, Eric, J. , MILLER, Michael, W. , SCOTT, Jack, D. , STAMFORD, Andrew, W. , GREENLEE, William, J. , WEINSTEIN, Jay
IPC分类号： C07D241/04 , A61K31/495 , A61K31/496 , A61P3/00
CPC分类号： C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10
摘要： Compounds of Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物：化学式应在纸上以抽象形式出现。或其药学上可接受的盐，溶剂化物或酯可用于治疗由CB1受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如戒烟），胃肠道疾病和心血管病。

4. 发明公开

EP0989981A1 NOVEL PHENYL-SUBSTITUTED TRICYCLIC INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 失效
标题翻译：蛋白法尼基转移苯基取代的三环抑制剂
公开(公告)号：EP0989981A1
公开(公告)日：2000-04-05
申请号：EP98932719.2
申请日：1998-06-15
申请人： SCHERING CORPORATION
发明人： AFONSO, Adriano , KELLY, Joseph, M. , WEINSTEIN, Jay , WOLIN, Ronald, L. , ROSENBLUM, Stuart, B.
IPC分类号： C07D401/04 , C07D221/16 , A61K31/55 , A61K31/435
CPC分类号： C07D401/12 , C07D401/14
摘要： Novel phenyl-substituted tricyclic compounds of formula (1.0) and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.

5. 发明授权

EP0549729B1 ANTIVIRAL COMPOUNDS AND ANTIHYPERTENSIVE COMPOUNDS 失效
标题翻译：抗病毒和抗高血压CONNECTIONS
公开(公告)号：EP0549729B1
公开(公告)日：1997-12-17
申请号：EP91919340.9
申请日：1991-09-06
申请人： SCHERING CORPORATION
发明人： AFONSO, Adriano , WEINSTEIN, Jay , GENTLES, Margaret, Jevnik
IPC分类号： C07D215/22 , A61K31/47 , C07D311/16 , C07D335/06 , A61K31/37 , C07D409/12 , C07D405/12 , C07D417/04 , C07D401/06 , C07D405/04 , C07D407/12
CPC分类号： C07D215/22 , C07D311/16 , C07D401/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07F7/1856 , C07F9/60
摘要： Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by formula (1.0) and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by formula (1.0) are disclosed. Methods of treating a viral infection using compounds represented by formula (1.0) are disclosed. Also disclosed are methods of treating hypertension using compounds of formula (1.0) wherein R is selected from the group consisting of H, halogen and -C(O)OR?6; and R1¿ is selected from the group consisting of -OR14, -O(CH¿2?)aaC(H)3-iZi and -O(CH2)hN(R?15)¿2.

6. 发明公开

EP1819684A1 SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 有权
标题翻译：取代哌嗪CB1受体拮抗剂
公开(公告)号：EP1819684A1
公开(公告)日：2007-08-22
申请号：EP05852503.1
申请日：2005-12-01
申请人： SCHERING CORPORATION
发明人： GILBERT, Eric, J. , MILLER, Michael, W. , SCOTT, Jack, D. , STAMFORD, Andrew, W. , GREENLEE, William, J. , WEINSTEIN, Jay
IPC分类号： C07D241/04 , A61K31/495 , A61K31/496 , A61P3/00
CPC分类号： C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10
摘要： Compounds of Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

7. 发明公开

EP1987000A2 DIARYL PIPERIDINES AS CB1 MODULATORS 审中-公开
标题翻译：二芳基哌啶，CB1调节剂
公开(公告)号：EP1987000A2
公开(公告)日：2008-11-05
申请号：EP07716533.0
申请日：2007-01-11
申请人： Schering Corporation
发明人： SCOTT, Jack, D. , WEINSTEIN, Jay , MILLER, Michael, W. , STAMFORD, Andrew, W. , GILBERT, Eric, J. , XIA, Yan , GREENLEE, William, J. , LI, Wei
IPC分类号： C07D211/18 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
CPC分类号： C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/58 , C07D211/60 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/10
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome (e.g., obesity, waist circumference, lipid profile, and insulin sensitivity), neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.

8. 发明公开

EP0550464A1 ANTIVIRAL COMPOUNDS AND ANTIHYPERTENSIVE COMPOUNDS 失效
标题翻译：抗病毒和抗高血压CONNECTIONS。
公开(公告)号：EP0550464A1
公开(公告)日：1993-07-14
申请号：EP91915366.0
申请日：1991-09-06
申请人： SCHERING CORPORATION
发明人： AFONSO, Adriano , WEINSTEIN, Jay , GENTLES, Margaret, Jevnik , ROSENBLUM, Stuart, Barry
IPC分类号： A61K31 , A61P9 , A61P31 , C07C49 , C07C225 , C07C235 , C07C309 , C07C311 , C07C323 , C07D215 , C07D311 , C07D335 , C07D401 , C07D405 , C07D407 , C07D409 , C07D417 , C07F7 , C07F9
CPC分类号： C07D215/22 , C07D311/16 , C07D401/06 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07F7/1856 , C07F9/60
摘要： Composés utiles comme agents anti-viraux contre des virus contenant de l'ADN tels que des virus du groupe de l'herpès. Les composés ainsi que sels et solvates pharmaceutiquement acceptables sont représentés par des composés de la formule (1.0) L'invention concerne également des compositions pharmaceutiques contenant des composés représentés par la formule (1.0) ainsi que des procédés de traitement d'une infection virale utilisant des composés représentés par ladite formule (1.0). En outre l'invention concerne des composés utiles en tant qu'agents anti-hypertenseurs ainsi que des procédés de l'hypertension à l'aide desdits composés. Les agents anti-hypertenseurs sont des composés représentés par la formule (1.0) dans laquelle R4 est sélectionné dans le groupe constitué d'alkyle et d'aminoalkyle. R1 est de préférence H.

9. 发明公开

EP0547145A1 ANTIVIRAL COMPOUNDS 失效
标题翻译：抗病毒化合物。
公开(公告)号：EP0547145A1
公开(公告)日：1993-06-23
申请号：EP91916684.0
申请日：1991-09-06
申请人： SCHERING CORPORATION
发明人： AFONSO, Adriano , WEINSTEIN, Jay , GENTLES, Margaret, Jevnik
IPC分类号： A61K31 , A61P31 , C07C49 , C07D215 , C07D311 , C07D335
CPC分类号： C07D215/22 , C07D311/56 , C07D335/06
摘要： Composés utiles comme agents anti-viraux contre des virus contenant de l'ADN tels que des virus du groupe de l'herpès. Les composés ainsi que leurs sels et solvates pharmaceutiquement acceptables sont représentés par la formule (1.0) dans laquelle: (A) X est choisi dans le groupe constitué de N-R3, O, S et C(R3)2; (B) R3 est choisi parmi H ainsi qu'une gamme de substituants; (C) R1 représente un groupe d'étherification ou d'estérification; (D) R2 est choisi parmi une gamme de substituants; (E) m représente 0 ou un nombre entier compris entre 1 et 4; et (F) R4 et R5 sont identiques et sont choisis entre des groupes alkyle et axyle. L'invention concerne également des sels pharmaceutiquement acceptables des composés de la formule (1.0), lesquels sont acides ou basiques. De plus, l'invention concerne des compositions pharmaceutiques contenant des composés représentés par la formule (1.0). En outre, l'invention concerne des procédés de traitement d'infections virales à l'aide de composés représentés par la formule (1.0).

10. 发明授权

EP1021448B1 TRICYCLIC COMPOUNDS HAVING ACTIVITY AS Ras-FPT INHIBITORS 失效
标题翻译：三环化合物作为RAS抑制剂FPT
公开(公告)号：EP1021448B1
公开(公告)日：2003-05-02
申请号：EP97911596.1
申请日：1997-10-07
申请人： SCHERING CORPORATION
发明人： AFONSO, Adriano , KELLY, Joseph, M. , ROSENBLUM, Stuart , WOLIN, Ronald, L. , WEINSTEIN, Jay
IPC分类号： C07D491/044 , A61K31/435 , C07D495/04 , C07D471/04 , A61K31/55
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： Compounds of formula (I), wherein: X1 is hydrogen, halogen, CF¿3?, nitro, NH2 or lower alkyl; each X?2¿ is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl; n is 1 or 2; Y is selected from the group consisting of S(O)¿p?, O, and NR?5¿, wherein p is 0, 1 or 2, and R5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl; R?1 and R2¿, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR5; A..... is C=, CH- or N-; R is -CZ-Y1-Y2-R3, wherein: Z is O, =CH-CN, or =N-CN; one of Y?1 and Y2¿ is a bond, -CO-, O, S, or -NR4-, and the other is (CH¿2?)m, where m is 0 or an integer of 1 to 4, and R?4¿ is H or alkyl, with the previso that when Z is O and m is 0 then Y1 or Y2 is selected form -CO-, O, S, or -NR4; R3 is aryl, heteroaryl or heterocycloalkyl, with proviso that R3 can also be lower alkyl when Z is =N-CN; and their pharmaceutically acceptable acid additions salts; have activity as Ras-FPT inhibitors. They can be used, e.g., in pharmaceutical compositions, for inhibiting the abnormal growth of cells and for inhibiting proliferative diseases. Processes for their preparation, and useful intermediates, are also disclosed.

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