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1. 发明申请

WO2004096794A1 AZETIDINECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CB1 RECEPTOR MEDIATED DISORDRS 审中-公开
标题翻译： AZETIDINECARBOXAMIDE衍生物及其在治疗CB1受体介导的病症中的应用
公开(公告)号：WO2004096794A1
公开(公告)日：2004-11-11
申请号：PCT/GB2004/001884
申请日：2004-04-29
申请人： VERNALIS RESEARCH LIMITED , DAVIDSON, James, Edward, Paul , BENTLEY, Jonathan, Mark , DAWSON, Claire, Elizabeth , HARRISON, Kerry , MANSELL, Howard, Langham , PITHER, Alan, Leslie , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , RUSTON, Victoria, Jane
发明人： DAVIDSON, James, Edward, Paul , BENTLEY, Jonathan, Mark , DAWSON, Claire, Elizabeth , HARRISON, Kerry , MANSELL, Howard, Langham , PITHER, Alan, Leslie , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , RUSTON, Victoria, Jane
IPC分类号： C07D403/06
CPC分类号： C07D401/12 , C07D205/04 , C07D211/46 , C07D403/06 , C07D405/12 , C07D409/06 , C07D409/12
摘要： Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB 1 receptors, such as obesity, wherein: R 1 is aryl or heteroaryl; R 2 is alkyl, aryl or heteroaryl; R 3 is alkyl, aryl, heteroaryl, NR 9 R 10 , OR 15, or NR 16 C(O)R 17 ; Y is C=O, C=S, SO 2 , or (CR 7 R 8) p ; m = 1 or 2; n = 1 or 2; and p=1,2,3 or 4, R 7 to R 17 being as defined in the specification; wherein if -Y-R 3 is -C(O)NH(alkyl) then: R 1 and/or R 2 is selected from heteroary1; and/or m and/or n is 2; and/or R 11 and/or R 12 is lower alkyl, or a pharmaceutically acceptable salt or prodrug thereof.
摘要翻译：式（I）化合物及其在治疗中的用途，特别是用于治疗由CB1受体介导的障碍，例如肥胖症，其中：R 1是芳基或杂芳基; R 2是烷基，芳基或杂芳基; R 3是烷基，芳基，杂芳基，NR 9 R 10，OR 15或NR 16 C（O）R 17; Y是C = O，C = S ，SO 2或（CR 7 R 8）> p; m = 1或2; n = 1或2; 和p = 1,2,3或4，R 7至R 17如说明书中所定义; 其中如果-Y-R 3是-C（O）NH（烷基），那么：R 1和/或R 2选自杂芳基; 和/或m和/或n为2; 和/或R 11和/或R 12是低级烷基，或其药学上可接受的盐或前药。

2. 发明申请

WO2004096763A1 AZETIDINECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CB1 RECEPTOR MEDIATED DISORDERS 审中-公开
标题翻译： AZETIDINECARBOXAMIDE衍生物及其在治疗CB1受体介导的疾病中的应用
公开(公告)号：WO2004096763A1
公开(公告)日：2004-11-11
申请号：PCT/GB2004/001831
申请日：2004-04-29
申请人： VERNALIS RESEARCH LIMITED , DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , HARRISON, Kerry , MANSELL, Howard, Langham , PRATT, Robert, Mark , SOHAL, Suhkjit , RUSTON, Victoria, Jane
发明人： DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , HARRISON, Kerry , MANSELL, Howard, Langham , PRATT, Robert, Mark , SOHAL, Suhkjit , RUSTON, Victoria, Jane
IPC分类号： C07D205/04
CPC分类号： C07D405/12 , C07D205/04 , C07D409/12
摘要： Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB 1 receptors such as obesity: Formuila (I) wherein: R 1 and R 2 are independently selected from aryl; and R 3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R 1 and R 2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [-CH-0-] group.
摘要翻译：式（I）化合物及其在治疗中的用途，特别是用于治疗由CB1受体如肥胖症介导的病症：Formuila（I）其中：R 1和R 2独立地选自芳基; 和R 3是氢或烷基; 或其药学上可接受的盐或前药，其中R 1和R 2中的至少一个在其邻位的相邻位置具有非氢取代基，相对于[-CH- 0-]组。

3. 发明申请

WO2004096209A1 THE USE OF AZETIDINECARBOXAMIDE DERIVATIVES IN THERAPY 审中-公开
标题翻译：治疗方法中使用阿奇霉素酰胺衍生物
公开(公告)号：WO2004096209A1
公开(公告)日：2004-11-11
申请号：PCT/GB2004/001812
申请日：2004-04-29
申请人： VERNALIS RESEARCH LIMITED , DAVIDSON, James, Edward, Paul , ADAMS, David, Reginald , BICKERDIKE, Michael, John , FLETCHER, Allan
发明人： DAVIDSON, James, Edward, Paul , ADAMS, David, Reginald , BICKERDIKE, Michael, John , FLETCHER, Allan
IPC分类号： A61K31/397
CPC分类号： A61K31/397
摘要： The use of a compound of formula (I): wherein: R 1 is aryl; R 2 is H, alkyl or aryl; and R 3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for the treatment of a disorder mediated by CB 1 receptors.
摘要翻译：使用式（I）化合物：其中：R 1是芳基; R 2是H，烷基或芳基; 和R 3是氢或烷基; 或其药学上可接受的盐或前药在制备用于治疗由CB1受体介导的病症的药物中的用途。

4. 发明申请

WO2007057687A1 PIPERAZINE DERIVATIVES AND THEIR USE IN THERAPY 审中-公开
标题翻译：哌嗪衍生物及其治疗用途
公开(公告)号：WO2007057687A1
公开(公告)日：2007-05-24
申请号：PCT/GB2006/004300
申请日：2006-11-17
申请人： VERNALIS (R & D) LIMITED , MONCK, Nathaniel, Julius, Thomas , DAVIDSON, James, Edward, Paul , NUNNS, Claire, Louise , REEVES, Stephen, David
发明人： MONCK, Nathaniel, Julius, Thomas , DAVIDSON, James, Edward, Paul , NUNNS, Claire, Louise , REEVES, Stephen, David
IPC分类号： C07D403/10 , C07D241/04 , C07D401/10 , A61K31/506 , A61K31/496 , A61K31/495 , A61K31/551 , A61K31/4995 , A61P3/00 , A61P19/08 , A61P9/10 , A61P35/00
CPC分类号： C07D403/10 , C07D241/04 , C07D401/10
摘要： Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB 1 receptors wherein R 1 is a radical of formula -(Alk 1 ) m -(NH) p -(Alk 2 ) n -Q wherein m, n and p are independently 0 or 1, Alk 1 and Alk 2 are straight or branched chain divalent C 1 -C 6 alkylene or C 2 -C 6 alkenylene radicals, and Q is (i) hydrogen, except in the case where m, n and p are each 0, or (ii) an optionally substituted carbocyclic or heterocyclic group; R 2 is hydrogen, C 1 -C 3 alkyl, cyclopropyl, or -CF 3 ; Ring A is a phenyl or 5- or 6-membered heteroaryl ring either of which is optionally substituted; Ar is a phenyl or 5- or 6-membered heteroaryl ring either of which is optionally substituted; L is -CH 2 -, -C(=O)-, -NH-, -O-, -S-, -SO-, -SO 2 -, -(CH 2 ) 2 -, -CH=CH-, -OCH 2 -, -CH(CH 3 )-, or -NH-CH 2 -; s is 1 and W is an optionally substituted N-containing heterocyclic ring of 5 to 7 ring atoms; or s is O and W is an optionally substituted N-containing saturated heterocyclic ring of 5 to 7 ring atoms, or an N-containing heteroaryl ring of 5 or 6 ring atoms substituted by at least one substituent selected from amino, C 1 -C 6 alkylamino or cyano; or a pharmaceutically acceptable salt, hydrate or solvate thereof.
摘要翻译：式（I）化合物及其在治疗中的用途，特别是用于治疗CB 1受体介导的病症，其中R 1是式 - （Alk < SUP> 1 ）_{米 - （NH）_{p - （ALK ^{2 ）_{名词 -Q 其中m，n和p独立地为0或1，Alk 1和Alk 2是直链或支链二价C 1 -C 3 > 6个亚烷基或C 2 -C 6亚烯基，Q是（i）氢，除了在m，n和p各自的情况下 0，或（ii）任选取代的碳环或杂环基; R 2是氢，C 1 -C 3烷基，环丙基或-CF 3 N; 环A是任选被取代的苯基或5-或6-元杂芳基环; Ar是任选被取代的苯基或5-或6-元杂芳基环; L是-CH 2 - ， - C（= O） - ， - NH - ， - O - ， - S - ， - SO - ， - SO 2 - - （CH 2）2 - ， - CH = CH - ， - OCH 2 - ， - CH（CH 3）） - 或-NH-CH 2 - ; s为1，W为任选取代的5〜7个环原子的含氮杂环; 或s为O且W为任选取代的5至7个环原子的含N的饱和杂环，或5或6个环原子的含N杂芳基环被至少一个选自氨基， C 1 -C 6烷基氨基或氰基; 或其药学上可接受的盐，水合物或溶剂化物。}}}}

5. 发明申请

WO2002048124A3 PIPERAZINE DERIVATIVES 审中-公开
公开(公告)号：WO2002048124A3
公开(公告)日：2002-06-20
申请号：PCT/EP2001/014343
申请日：2001-12-06
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , GEORGE, Ashley, Roger , MANSELL, Howard, Langham , MATTEI, Patrizio , MIZRAHI, Jacques , NETTEKOVEN, Matthias, Heinrich , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , ROEVER, Stephan , SPECKLIN, Jean-Luc , STALDER, Henri , WILKINSON, Kerry
IPC分类号： C07D295/20
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R 1 to 4 4 , A 1 , A 2 m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

6. 发明公开

EP1109813A1 PYRROLOINDOLES, PYRIDOINDOLES AND AZEPINOINDOLES AS 5-HT2C AGONISTS 有权
标题翻译： PYRROLOINDOLE，并吲哚和AZEPINOINDOLE超过5-HT 2C受体激动剂
公开(公告)号：EP1109813A1
公开(公告)日：2001-06-27
申请号：EP99943091.1
申请日：1999-09-01
申请人： VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , ROFFEY, Jonathan, Richard, Anthony , HAMLYN, Richard, John , GAUR, Suneel , DUNCTON, Matthew, Alexander, James , DAVIDSON, James, Edward, Paul , BICKERDIKE, Michael, John , CLIFFE, Ian, Anthony , MANSELL, Howard, Langham
IPC分类号： C07D487/04 , C07D471/04 , C07D491/14 , A61K31/40
CPC分类号： C07D471/04 , C07D487/04 , C07D491/14
摘要： A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

7. 发明授权

EP1109813B1 PYRROLOINDOLES, PYRIDOINDOLES AND AZEPINOINDOLES AS 5-HT2C AGONISTS 有权
标题翻译： PYRROLOINDOLE，并吲哚和AZEPINOINDOLE超过5-HT 2C受体激动剂
公开(公告)号：EP1109813B1
公开(公告)日：2004-08-11
申请号：EP99943091.1
申请日：1999-09-01
申请人： VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , ROFFEY, Jonathan, Richard, Anthony , HAMLYN, Richard, John , GAUR, Suneel , DUNCTON, Matthew, Alexander, James , DAVIDSON, James, Edward, Paul , BICKERDIKE, Michael, John , CLIFFE, Ian, Anthony , MANSELL, Howard, Langham
IPC分类号： C07D487/04 , C07D471/04 , C07D491/14 , A61K31/40
CPC分类号： C07D471/04 , C07D487/04 , C07D491/14
摘要： A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

8. 发明公开

EP1343775A2 PIPERAZINE DERIVATIVES 有权
标题翻译：哌嗪衍生物
公开(公告)号：EP1343775A2
公开(公告)日：2003-09-17
申请号：EP01990522.3
申请日：2001-12-06
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , GEORGE, Ashley, Roger , MANSELL, Howard, Langham , MATTEI, Patrizio , MIZRAHI, Jacques , NETTEKOVEN, Matthias, Heinrich , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , ROEVER, Stephan , SPECKLIN, Jean-Luc , STALDER, Henri , WILKINSON, Kerry
IPC分类号： C07D295/20 , A61K31/495 , A61P3/04 , C07D261/08 , C07D213/30
CPC分类号： C07D207/325 , C07D213/30 , C07D213/64 , C07D213/643 , C07D261/08 , C07D277/24 , C07D285/14 , C07D295/205 , C07D295/21 , C07D307/12 , C07D307/42 , C07D333/16 , C07D413/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R?1 to 44, A1, A2¿ m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

9. 发明公开

EP1202965A1 INDOLE DERIVATIVES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR MEDICINAL APPLICATION 有权
标题翻译：吲哚化合物，METHOD FOR PRODUCING他们和他们的药物组合物含有医疗应用
公开(公告)号：EP1202965A1
公开(公告)日：2002-05-08
申请号：EP00951697.2
申请日：2000-08-04
申请人： VERNALIS RESEARCH LIMITED
发明人： BENTLEY, Jonathan, Mark , ROFFEY, Jonathan, Richard, Anthony , DAVIDSON, James, Edward, Paul , MANSELL,Howard, Langh am , HAMLYN, Richard, John , CLIFFE, Ian, Anthony , ADAMS, David, Reginald , MONCK, Nathaniel, Julius
IPC分类号： C07D209/80 , C07D495/04 , A61K31/403 , A61K31/407 , A61P25/28
CPC分类号： C07D495/04 , C07D209/94
摘要： A chemical compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4, R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5 is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4 to R7 is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT¿2C? receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

10. 发明授权

EP1343775B1 PIPERAZINE DERIVATIVES 有权
标题翻译：哌嗪衍生物
公开(公告)号：EP1343775B1
公开(公告)日：2008-06-04
申请号：EP01990522.3
申请日：2001-12-06
申请人： F. Hoffmann-La Roche AG , VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , GEORGE, Ashley, Roger , MANSELL, Howard, Langham , MATTEI, Patrizio , MIZRAHI, Jacques , NETTEKOVEN, Matthias, Heinrich , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , ROEVER, Stephan , SPECKLIN, Jean-Luc , STALDER, Henri , HARRISON, Kerry
IPC分类号： C07D295/20 , A61K31/495 , A61P3/04 , C07D261/08 , C07D213/30
CPC分类号： C07D207/325 , C07D213/30 , C07D213/64 , C07D213/643 , C07D261/08 , C07D277/24 , C07D285/14 , C07D295/205 , C07D295/21 , C07D307/12 , C07D307/42 , C07D333/16 , C07D413/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R?1 to 44, A1, A2¿ m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
摘要翻译：本发明涉及式（I）的化学化合物及其药学上可用的盐，溶剂合物和酯，其中R 1至44，A 1，A 2和m具有权利要求1中给出的含义。可以使用它们其为用于治疗或预防中枢神经系统疾病，心血管疾病，胃肠疾病，糖尿病，肥胖症和睡眠呼吸暂停的药物制剂形式。

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