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1. 发明申请

WO2015130444A1 QUINOLINE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS 审中-公开
标题翻译：喹啉衍生物作为CB-1反相激动剂有用
公开(公告)号：WO2015130444A1
公开(公告)日：2015-09-03
申请号：PCT/US2015/014712
申请日：2015-02-06
申请人： JANSSEN PHARMACEUTICA NV , DECORTE, Bart , MACIELAG, Mark , GRECO, Michael , ZHANG, Yue-Mei , TELEHA, Christopher
发明人： DECORTE, Bart , MACIELAG, Mark , GRECO, Michael , ZHANG, Yue-Mei , TELEHA, Christopher
IPC分类号： C07D401/14 , C07D215/42 , C07D215/44 , C07D401/12 , C07D409/14 , C07D417/06 , C07D417/14 , C07D405/14 , C07D215/06 , C07D401/04 , C07D409/06 , A61K31/47 , A61K31/4706 , A61P3/04 , A61P3/10
CPC分类号： C07D215/44 , C07D215/06 , C07D215/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.
摘要翻译：本发明涉及喹啉衍生物，含有所述衍生物的药物组合物及其在治疗由CB-1受体介导的病症和病症中的用途; 更具体地，涉及治疗响应于CB-1受体反向激动作用的病症和病症。例如，本发明的化合物可用于治疗代谢紊乱。

2. 发明申请

WO2012047580A1 ALPHA-KETOAMIDE DERIVATIVES USEFUL ENDOTHELIAL LIPASE INHIBITORS 审中-公开
标题翻译： ALPHA-KETAAMIDE衍生物有用的内皮脂肪酶抑制剂
公开(公告)号：WO2012047580A1
公开(公告)日：2012-04-12
申请号：PCT/US2011/053236
申请日：2011-09-26
申请人： JANSSEN PHARMACEUTICA NV , GRECO, Michael, N. , CONNELLY, Margery, A. , GHOSH, Shyamali , HLASTA, Dennis, J. , LAWSON, Edward, C. , STROBEL, Eric , WEIDNER-WELLS, Michele, A. , YE, Hong
发明人： GRECO, Michael, N. , CONNELLY, Margery, A. , GHOSH, Shyamali , HLASTA, Dennis, J. , LAWSON, Edward, C. , STROBEL, Eric , WEIDNER-WELLS, Michele, A. , YE, Hong
IPC分类号： A01N43/64 , A61K31/41
CPC分类号： C07D271/10 , C07D249/08 , C07D285/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention is directed to α-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
摘要翻译：本发明涉及α-酮酰胺衍生物，含有它们的药物组合物及其在治疗由内皮脂肪酶（例如心血管疾病）调节的病症和状况中的用途。

3. 发明申请

WO2015130445A1 QUINOLINE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS 审中-公开
标题翻译：喹啉衍生物可用作CB-1反义激动剂
公开(公告)号：WO2015130445A1
公开(公告)日：2015-09-03
申请号：PCT/US2015/014713
申请日：2015-02-06
申请人： JANSSEN PHARMACEUTICA NV , DECORTE, Bart , MACIELAG, Mark , GRECO, Michael , ZHANG, Yue-Mei , TELEHA, Christopher
发明人： DECORTE, Bart , MACIELAG, Mark , GRECO, Michael , ZHANG, Yue-Mei , TELEHA, Christopher
IPC分类号： C07D401/14 , C07D405/14 , C07D215/04 , C07D215/42 , C07D215/44 , C07D401/04 , C07D401/12 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , A61P3/04 , A61P3/10 , A61K31/47 , A61K31/4706
CPC分类号： C07D215/44 , C07D215/04 , C07D215/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C09B11/02
摘要： The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.
摘要翻译：本发明涉及喹啉衍生物，含有所述衍生物的药物组合物及其在治疗由CB-1受体介导的病症和病症中的用途; 更具体地说，用于治疗对CB-1受体的反向激动作用有响应的病症和病症。例如，本发明的化合物可用于治疗代谢紊乱。

4. 发明申请

WO2008048668A2 NOVEL INHIBITORS OF CHYMASE 审中-公开
标题翻译： CHYMASE的新型抑制剂
公开(公告)号：WO2008048668A2
公开(公告)日：2008-04-24
申请号：PCT/US2007/022244
申请日：2007-10-18
申请人： JANSSEN PHARMACEUTICA, N.V. , GRECO, Michael, N. , HAWKINS, Michael, J. , POWELL, Eugene , DE GARAVILLA, Lawrence , MARYANOFF, Bruce, E.
发明人： GRECO, Michael, N. , HAWKINS, Michael, J. , POWELL, Eugene , DE GARAVILLA, Lawrence , MARYANOFF, Bruce, E.
IPC分类号： A61K31/665 , A61P11/00 , C07F9/02
CPC分类号： C07F9/65517
摘要： The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates and derivatives thereof, and methods for treating inflammatory or serine protease mediated disorders.
摘要翻译：本发明涉及式（I）化合物或其对映异构体，非对映异构体，多晶型物或药学上可接受的盐以及制备所述化合物和组合物，其中间体及衍生物和方法的方法用于治疗炎性或丝氨酸蛋白酶介导的病症。

5. 发明申请

WO2004094441A2 NOVEL PHOSPHONIC ACID COMPOUNDS AS INHIBITORS OF SERINE PROTEASES 审中-公开
标题翻译：新型磷酸化合物作为丝氨酸蛋白酶的抑制剂
公开(公告)号：WO2004094441A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/011490
申请日：2004-04-14
申请人： ORTHO-MCNEIL PHARMACEUTICAL, INC. , GRECO, Michael, N. , ALMOND, Harold, R. , POWELL, Eugene , DE GARAVILLA, Lawrence
发明人： GRECO, Michael, N. , ALMOND, Harold, R. , POWELL, Eugene , DE GARAVILLA, Lawrence
IPC分类号： C07F9/6509
CPC分类号： C07F9/65586 , C07F9/3882 , C07F9/5721 , C07F9/5727 , C07F9/591 , C07F9/598 , C07F9/650958 , C07F9/65517 , C07F9/65583 , C07F9/6561
摘要： The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
摘要翻译：本发明涉及可用作丝氨酸蛋白酶抑制剂的膦酸化合物，其组合物和用于治疗炎性和丝氨酸蛋白酶介导的病症的方法。

6. 发明申请

WO1993015079A1 PYRROLOIMIDAZOLYL AND IMIDAZOPYRIDINYL SUBSTITUTED 1H-BENZIMIDAZOLE DERIVATIVES AS AROMATASE INHIBITORS 审中-公开
标题翻译：吡咯并咪唑并咪唑并吡啶将取代的1H-苯并咪唑衍生物作为芳香酶抑制剂
公开(公告)号：WO1993015079A1
公开(公告)日：1993-08-05
申请号：PCT/EP1993000129
申请日：1993-01-20
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSEN, Marcel, August, Constant , RAEYMAEKERS, Alfons, Herman, Margaretha , FREYNE, Eddy, Jean, Edgard , GRECO, Michael, Nicholas
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Pyrroloimidazolyl and imidazopyridinyl substituted 1H &cir& _-benzimidazole derivatives having formula (I) wherein n is 0 or 1; R is hydrogen, nitro, amino, mono- or diC1-6alkyl)amino, halo, C1-6alkyl, hydroxy or C1-6alkyloxy; R is hydrogen; C1-10alkyl; C3-6alkenyl; C3-6alkynyl; C3-7cycloalkyl; phenyl; substituted phenyl; C1-4alkyl substituted with phenyl, substituted phenyl, naphthalenyl, thienyl, furanyl, C1-4alkylfuranyl, C3-7cycloalkyl; and R is hydrogen, C1-8alkyl; C3-7cycloalkyl; hydroxy, amino; C1-6alkyloxy; C1-6alkyloxycarbonylamino; phenyl; C1-4alkyl substituted with phenyl, piperazinyl, 4-(C1-4alkyl)piperazinyl or morpholinyl; each substituted phenyl independently is phenyl substituted with a substituent independently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C1-6alkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, formyl, (hydroxyimino)methyl, cyano, amino, mono- and di(C1-6alkyl)amino and nitro, having sex hormone synthesis inhibiting properties. Compositions containing said compounds of formula (I). Preparations of said compounds and compositions, and use thereof for treating mammals suffering from sex hormone disorders.
摘要翻译：具有式（I）的吡咯并咪唑基和咪唑并吡啶基取代的1H和苯并咪唑衍生物，其中n为0或1; R 1是氢，硝基，氨基，单或二C 1-6烷基）氨基，卤素，C 1-6烷基，羟基或C 1-6烷氧基; R 2是氢; C 1-10烷基; C3-6alkenyl; C 3-6炔基; 3-7环烷基; 苯基; 取代的苯基; 被苯基，取代的苯基，萘基，噻吩基，呋喃基，C1-4烷基呋喃基，C3-7环烷基取代的C1-4烷基; 和R 3是氢，C 1-8烷基; 3-7环烷基; 羟基，氨基; C1-6烷; C1-6alkyloxycarbonylamino; 苯基; 被苯基，哌嗪基，4-（C 1-4烷基）哌嗪基或吗啉基取代的C 1-4烷基; 每个取代的苯基独立地是被独立地选自卤素，羟基，羟甲基，三氟甲基，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，甲酰基，（羟基亚氨基）甲基，氰基，氨基，单和二（C 1-6烷基）氨基和硝基，具有性激素合成抑制性质。含有所述式（I）化合物的组合物。所述化合物和组合物的制备及其用于治疗患有性激素障碍的哺乳动物的用途。

7. 发明申请

WO2005073214A2 NOVEL INHIBITORS OF CHYMASE 审中-公开
标题翻译： CHYMASE的新型抑制剂
公开(公告)号：WO2005073214A2
公开(公告)日：2005-08-11
申请号：PCT/US2005/001659
申请日：2005-01-18
申请人： JANSSEN PHARMACEUTICA, N.V. , HAWKINS, Michael, J. , GRECO, Michael, N. , POWELL, Eugene , DE GARAVILLA, Lawrence , MARYANOFF, Bruce, E.
发明人： HAWKINS, Michael, J. , GRECO, Michael, N. , POWELL, Eugene , DE GARAVILLA, Lawrence , MARYANOFF, Bruce, E.
IPC分类号： C07D333/00
CPC分类号： C07F9/6561 , C07F9/4006 , C07F9/5721 , C07F9/5728 , C07F9/598 , C07F9/60 , C07F9/62 , C07F9/65517 , C07F9/655354 , C07F9/65583 , C07F9/65586 , C07F9/657181
摘要： The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
摘要翻译：本发明涉及式（I）化合物，这些化合物的制备方法，组合物，中间体及其衍生物，以及治疗炎性和丝氨酸蛋白酶介导的病症的方法。

8. 发明申请

WO2012162409A1 BIPHENYL DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS 审中-公开
标题翻译：二苯乙烯衍生物作为GLUCAGON受体拮抗剂有用
公开(公告)号：WO2012162409A1
公开(公告)日：2012-11-29
申请号：PCT/US2012/039173
申请日：2012-05-23
申请人： JANSSEN PHARMACEUTICA NV , CHAKRAVARTY, Devraj , GRECO, Michael, N. , SHOOK, Brian , XU, Guozhang , ZHANG, Rui
发明人： CHAKRAVARTY, Devraj , GRECO, Michael, N. , SHOOK, Brian , XU, Guozhang , ZHANG, Rui
IPC分类号： C07C231/12 , C07C233/83 , A61P3/08 , A61P5/50 , A61K31/166 , A61K31/195
CPC分类号： C07C237/36
摘要： The present invention is directed to biphenyl derivatives of Formula (I), pharmaceutical compositions containing them and their use in the treatment and / or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity. (I)
摘要翻译：本发明涉及式（I）的联苯衍生物，含有它们的药物组合物及其在治疗和/或预防通过拮抗一种或多种胰高血糖素受体而改善的病症和病症中的用途，包括例如II型代谢疾病糖尿病和肥胖。（一世）

9. 发明申请

WO2005073214A3 NOVEL INHIBITORS OF CHYMASE 审中-公开
标题翻译： CHYMASE的新型抑制剂
公开(公告)号：WO2005073214A3
公开(公告)日：2005-10-20
申请号：PCT/US2005001659
申请日：2005-01-18
申请人： JANSSEN PHARMACEUTICA NV , HAWKINS MICHAEL J , GRECO MICHAEL N , POWELL EUGENE , DE GARAVILLA LAWRENCE , MARYANOFF BRUCE E
发明人： HAWKINS MICHAEL J , GRECO MICHAEL N , POWELL EUGENE , DE GARAVILLA LAWRENCE , MARYANOFF BRUCE E
IPC分类号： A61K31/165 , A61K31/381 , A61K31/4436 , A61K31/453 , A61K31/662 , C07F9/30 , C07F9/32 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/59 , C07F9/60 , C07F9/62 , C07F9/655 , C07F9/6553 , C07F9/6558 , C07F9/6561 , C07F9/6571
CPC分类号： C07F9/6561 , C07F9/4006 , C07F9/5721 , C07F9/5728 , C07F9/598 , C07F9/60 , C07F9/62 , C07F9/65517 , C07F9/655354 , C07F9/65583 , C07F9/65586 , C07F9/657181
摘要： The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
摘要翻译：本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体和衍生物，以及治疗炎性和丝氨酸蛋白酶介导的病症的方法。

10. 发明申请

WO2004094441A3 PIPERAZINE CONTAINING PHOSPHONIC ACID COMPOUNDS AS INHIBITORS OF SERINE PROTEASES 审中-公开
标题翻译：含有磷酸化合物的哌嗪作为丝氨酸蛋白酶的抑制剂
公开(公告)号：WO2004094441A3
公开(公告)日：2005-10-13
申请号：PCT/US2004011490
申请日：2004-04-14
申请人： ORTHO MCNEIL PHARM INC , GRECO MICHAEL N , ALMOND HAROLD R , POWELL EUGENE , DE GARAVILLA LAWRENCE
发明人： GRECO MICHAEL N , ALMOND HAROLD R , POWELL EUGENE , DE GARAVILLA LAWRENCE
IPC分类号： C07F9/38 , C07F9/572 , C07F9/59 , C07F9/6509 , C07F9/655 , C07F9/6558 , C07F9/6561 , A61K31/675
CPC分类号： C07F9/65586 , C07F9/3882 , C07F9/5721 , C07F9/5727 , C07F9/591 , C07F9/598 , C07F9/650958 , C07F9/65517 , C07F9/65583 , C07F9/6561
摘要： The present invention is directed to phosphonic acid compounds of Formula (II): useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
摘要翻译：本发明涉及式（II）的膦酸化合物：可用作丝氨酸蛋白酶抑制剂，其组合物和用于治疗炎性和丝氨酸蛋白酶介导的病症的方法。

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