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1. 发明公开

EP2509981A1 INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE 有权
标题翻译：抑制剂二酰甘油酰基转移酶
公开(公告)号：EP2509981A1
公开(公告)日：2012-10-17
申请号：EP10799154.9
申请日：2010-12-07
申请人： Eli Lilly and Company
发明人： ARNOLD, Macklin, Brian , BEAUCHAMP, Thomas, James , CANADA, Emily, Jane , HEMBRE, Erik, James , LU, Jianliang , RIZZO, John, Robert , SCHAUS, John, Mehnert , SHI, Qing
IPC分类号： C07D487/04 , A61K31/5517 , A61P3/00
CPC分类号： C07D487/04
摘要： This invention provides compounds of formula (I) : or a pharmaceutically acceptable salt thereof as inhibitors of diacylglycerol acyltransferase 1 (DGAT-1); as well as a method for treating obesity, a method for treating diabetes, and a pharmaceutical composition.

2. 发明授权

EP1341777B1 1-(2-M-METHANESULFONAMIDOPHENYLETHYL)-4-(M-TRIFLUOROMETHYLPHENYL)PIPERAZINE AND PHARMACEUTICALLY ACCEPTABLE SALTS AND SOLVATES THEREOF AND THEIR USE IN THE TREATEMENT OF INCONTINENCE 有权
标题翻译： 1-（2-M-methanesulfonamidophenylethyl）-4-（间三氟甲基苯基）哌嗪和其药物上可接受的盐和溶剂合物及其用于失禁处理
公开(公告)号：EP1341777B1
公开(公告)日：2007-09-26
申请号：EP01990644.5
申请日：2001-11-16
申请人： ELI LILLY AND COMPANY
发明人： SCHAUS, John, Mehnert , THOMPSON, Dennis, Charles , THOR, Karl, Bruce
IPC分类号： C07D295/00
CPC分类号： C07D295/135 , A61K31/495 , A61K45/06 , A61K2300/00
摘要： The present invention provides a compound of the formula (I), and the pharmaceutically acceptable salts and solvates thereof, which is useful for treating bladder over-activity or urinary incontinence.

3. 发明授权

EP2509981B1 INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE 有权
标题翻译：抑制剂二酰甘油酰基转移酶
公开(公告)号：EP2509981B1
公开(公告)日：2014-08-06
申请号：EP10799154.9
申请日：2010-12-07
申请人： Eli Lilly and Company
发明人： ARNOLD, Macklin, Brian , BEAUCHAMP, Thomas, James , CANADA, Emily, Jane , HEMBRE, Erik, James , LU, Jianliang , RIZZO, John, Robert , SCHAUS, John, Mehnert , SHI, Qing
IPC分类号： C07D487/04 , A61K31/5517 , A61P3/00
CPC分类号： C07D487/04

4. 发明授权

EP1379239B1 N-(2-ARYLETHYL) BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR 有权
标题翻译： N-（2-芳基乙基）苯甲酰胺ALS 5-HT6抗体拮抗剂
公开(公告)号：EP1379239B1
公开(公告)日：2007-09-12
申请号：EP02731094.5
申请日：2002-03-15
申请人： ELI LILLY AND COMPANY
发明人： CHEN, Zhaogen , COHEN, Michael, Philip , FISHER, Matthew, Joseph , GIETHLEN, Bruno, Prestwick Chemical, Inc. , GILLIG, James, Ronald , MCCOWAN, Jefferson, Ray , MILLER, Shawn, Christopher , SCHAUS, John, Mehnert
IPC分类号： A61K31/4045 , C07D209/16 , A61P25/18 , A61P25/28 , C07D403/12 , C07D401/12 , A61K31/4406 , A61K31/4409 , A61K31/506 , A61K31/4402 , C07C217/54 , C07C323/01 , C07C317/14 , C07D213/64 , C07D277/34 , C07D239/34 , C07D233/24 , C07D333/20 , C07D307/91 , C07D209/14
CPC分类号： C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要： The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
摘要翻译：本发明提供式I化合物其药学上可接受的盐及其药物组合物，它们是5-HT 6受体的拮抗剂。本发明进一步提供了一种治疗与5-HT 6受体相关的疾病的方法，包括精神分裂症，焦虑，阿尔茨海默病和认知障碍，其选自年龄相关的认知衰退，轻度认知损伤和痴呆，包括：向有需要的患者施用有效量的式I化合物。

5. 发明公开

EP1664063A1 SUBSTITUTED PIPERAZINES OF AZEPINES, OXAZEPINES, AND THIAZEPINES 审中-公开
标题翻译：作者氮杂，氧氮杂和THIAZEPINEN取代的哌嗪
公开(公告)号：EP1664063A1
公开(公告)日：2006-06-07
申请号：EP04780445.5
申请日：2004-09-07
申请人： ELI LILLY AND COMPANY
发明人： HE, John, Xiaoqiang , ROCCO, Vincent, Patrick , SCHAUS, John, Mehnert , MARTIN, Fionna, Mitchell, Eli Lilly and Company , OWTON, William, Martin, Eli Lilly and Company , TUPPER, David, Edward, Eli Lilly and Company
IPC分类号： C07D513/04 , C07D495/04 , A61K31/55 , A61K31/554 , C07D417/04 , A61P25/24
CPC分类号： C07D417/04 , C07D495/04 , C07D513/04
摘要： Described herein are antipyschotic compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, -CN, imidazolidin-2-one, phenyl, or tetrazole wherein tetrazole is unsubstituted or substituted with (C1-4) alkyl; R2 is H, halogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, OR6, SR6, NO2, CN, COR6, C(O)OR6, C(OH)R6, CONR7R8, phenyl or (C1-6) alkyl, wherein the (C1-6) alkyl is unsubstituted or substituted with a hydroxy; R3 is hydrogen, (C 1-6)fluoroalkyl , (C3-6) cycloalkyl, (C 2-6) alkenyl, phenyl, monocyclic heteroaromatic, bicyclic heteroaromatic, or (C1-4)alkyl wherein (C1-4) alkyl is unsubstituted or substituted with a phenyl; R4 and R5 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR9, SR9, NO2, CN, or COR9; R6 is hydrogen, (C1-6) fluoroalkyl, or (C1-6) alkyl; R7 and R8 are independently hydrogen, or (C1-6) alkyl; R9 is hydrogen, (C1-6) fluoroalkyl, (C1-6) alkyl; Alk is (C1-4) alkylene unsubstituted or substituted with a hydroxy; Y is oxygen, sulfur, SO2, or a bond; X is CH2, C=O, S, O, or SO2; Z is hydrogen, halogen, (C1-6) alkyl, (C1-6)fluoroalkyl, -OH, (C1-6) alkoxy, (C1-6) fluoroalkoxy, (C1-6) alkylthio, (C1-6) acyl, (C1-4)alkylsulfonyl, -OCF3, -NO2, - CN, carboxamido which may be substituted on the nitrogen by one or two (C1-4) alkyl groups, and -NH2 in which one of the hydrogens may be replaced by a (C1-4) alkyl group and the other hydrogen may be replaced by either a (C1-4) alkyl group, a (C1-6) acyl group, or a (C1-4) alkylsulfonyl group; the phenyl of R1, R2 or R3 is independently unsubstituted or substituted with one to three substituents independently selected from Z; the monocyclic heteroaromatic of R3 is unsubstituted or substituted with one to three substituents independently selected from Z; the bicyclic heteroaromatic of R3 is unsubstituted or substituted with one to three substituents independently selected from Z; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).

6. 发明授权

EP2280961B1 1,5-DIPHENYL-PYRROLIDIN-2-ONE COMPOUNDS AS CB-1 LIGANDS 有权
标题翻译： 1,5-二苯基-2-吡咯烷ON化合物作为CB-1配体
公开(公告)号：EP2280961B1
公开(公告)日：2012-07-25
申请号：EP09734415.4
申请日：2009-04-02
申请人： ELI LILLY AND COMPANY
发明人： SCHAUS, John, Mehnert
IPC分类号： C07D403/12 , A61K31/506 , A61P25/18
CPC分类号： C07D403/12
摘要： CB-1 receptor inverse agonist compounds of Formula (I) and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.

7. 发明公开

EP2280961A1 1,5-DIPHENYL-PYRROLIDIN-2-ONE COMPOUNDS AS CB-1 LIGANDS 有权
标题翻译： 1,5-二苯基-2-吡咯烷ON化合物作为CB-1配体
公开(公告)号：EP2280961A1
公开(公告)日：2011-02-09
申请号：EP09734415.4
申请日：2009-04-02
申请人： ELI LILLY AND COMPANY
发明人： SCHAUS, John, Mehnert
IPC分类号： C07D403/12 , A61K31/506 , A61P25/18
CPC分类号： C07D403/12
摘要： CB-1 receptor inverse agonist compounds of Formula (I) and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.

8. 发明授权

EP1492794B1 PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES AND THEIR USE AS DOPAMINE RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PSYCHOTIC DISORDERS 有权
标题翻译：哌嗪取代的芳基 - 苯二氮及其作为多巴胺受体拮抗剂治疗PSYCHOSE使用
公开(公告)号：EP1492794B1
公开(公告)日：2007-12-12
申请号：EP03713911.0
申请日：2003-03-17
申请人： ELI LILLY AND COMPANY
发明人： AICHER, Thomas, Daniel , CHEN, Zhaogen , CHEN, Ying , FAUL, Margaret, Mary , KRUSHINSKI, Joseph, Herman, Jr. , LE HUEROU, Yvan , PINEIRO-NUNEZ, Marta, Maria , ROCCO, Vincent, Patrick , RULEY, Kevin, Michael , SCHAUS, John, Mehnert , THOMPSON, Dennis, Charles , TUPPER, David, Edward, Eli Lilly and Company Ltd
IPC分类号： C07D495/04 , C07D513/04 , C07D403/04 , C07D487/04 , C07D241/04 , C07D401/06 , C07D407/06 , C07D409/06
CPC分类号： C07D487/04 , C07D243/38 , C07D495/04 , C07D513/04
摘要： Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl,wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, benzyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R7, NR8R9, or optionally substituted phenyl, wherein R7 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, benzyl, or optionally substituted phenyl, R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I). Also described are compounds useful as intermediates for the synthesis of the compounds of formula (I).

9. 发明授权

EP1546134B1 PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES 有权
标题翻译：哌嗪取代的芳基苯并二氮杂
公开(公告)号：EP1546134B1
公开(公告)日：2007-05-02
申请号：EP03784411.5
申请日：2003-07-28
申请人： ELI LILLY AND COMPANY
发明人： AICHER, Thomas, Daniel , CHEN, Zhaogen House 10A, Phase V. Green Villa , LE HUEROU, Yvan , MARTIN, Fionna Mitchell Eli Lilly and Company Ltd. , PINEIRO-NUNEZ, Marta, Maria , ROCCO, Vincent, Patrick , RULEY, Kevin, Michael , SCHAUS, John, Mehnert , SPINAZZE, Patrick, Gianpietro , TUPPER, David Edward Eli Lilly and Company
IPC分类号： C07D403/04 , C07D495/04 , C07D513/04 , A61K31/55 , A61P25/18
CPC分类号： C07D403/04 , C07D495/04 , C07D513/04
摘要： Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or -CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, N02, CN, COR4, C(O)OR4, CONR5R6 , NR5R6, S02NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen, (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyl is unsubsituted or substituted with a phenyl; R4 is hydrogen, (C1-6 alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treament of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).
摘要翻译：本文描述的是式（I）的化合物，其中：是任选苯并稠合的五元或六元芳族环，其具有0至3个独立地选自N，S和O的杂原子; Alk是（C1-4）亚烷基或羟基取代的（C1-4）亚烷基; X是氧或硫; （C 1-4）烷基是未取代的或被羟基，甲氧基，乙氧基，OCH 2 CH 2 OH或-CN取代的（C 1-4）烷基，（C 1-6）氟代烷基， ; （C1-6）氟代烷基，（C1-6）环烷基，OR4，SR4，NO2，CN，COR4，C（O）OR4，CONR5R6，NR5R6，SO2NR5R6，NR5COR4，NR5SO2R4，任选取代的芳族，或（C 1-6）烷基，其中（C 1-6）烷基未被取代或被羟基取代; （C1-4）氟烷基，（C2-6）链烯基，Ar，（C1-4）烷基-Ar或（C1-4）烷基未被取代或被苯基取代的（C1-4） ; （C 1-6烷基，（C 1-6）氟烷基或任选取代的芳族基; R 5和R 6独立地为氢，（C 1-6）烷基或任选取代的芳族基团，R 7为氢，（C 1-6）烷基，（C 1-6）氟烷基或任选取代的芳族基团; R 8和R 9独立地为氢，（C 1-6）烷基或任选取代的芳族基团; Ar为任选取代的苯基，萘基，单环杂芳族或双环杂芳族; Z 1和Z 2 （C 1-6）烷基，（C 1-6）氟烷基，OR 7，SR 7，NO 2，CN，COR 7，CONR 8 R 9，NR 8 R 9和任选取代的芳族基团;以及所有的盐，溶剂合物，（I）化合物作为多巴胺D2受体的拮抗剂的用途，以及作为治疗精神病和双相性精神障碍的药剂的用途，以及式（I）化合物的药物制剂）。

10. 发明公开

EP1379239A2 N-(2-ARYLETHYL) BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR 有权
标题翻译： N-（2-芳基乙基）苄胺ALS 5-HT6受体antagoniste
公开(公告)号：EP1379239A2
公开(公告)日：2004-01-14
申请号：EP02731094.5
申请日：2002-03-15
申请人： ELI LILLY AND COMPANY
发明人： CHEN, Zhaogen , COHEN, Michael, Philip , FISHER, Matthew, Joseph , GIETHLEN, Bruno,Prestwick Chemical, Inc. , GILLIG, James, Ronald , MCCOWAN, Jefferson, Ray , MILLER, Shawn, Christopher , SCHAUS, John, Mehnert
IPC分类号： A61K31/4045 , C07D209/16 , A61P25/18 , A61P25/28 , C07D403/12 , C07D401/12 , A61K31/4406 , A61K31/4409 , A61K31/506 , A61K31/4402 , C07C217/54 , C07C323/01 , C07C317/14 , C07D213/64 , C07D277/34 , C07D239/34 , C07D233/24 , C07D333/20 , C07D307/91 , C07D209/14
CPC分类号： C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要： The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.

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