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1. 发明申请

WO2009147170A2 DRUG COMBINATIONS COMPRISING A DGAT INHIBITOR AND A PPAR-AGONIST 审中-公开
标题翻译：包含DGAT抑制剂和PPAR-AGONIST的药物组合
公开(公告)号：WO2009147170A2
公开(公告)日：2009-12-10
申请号：PCT/EP2009/056800
申请日：2009-06-03
申请人： JANSSEN PHARMACEUTICA NV , LINDERS, Joannes, Theodorus, Maria , ROEVENS, Peter, Walter, Maria , HRUPKA, Brian, Joel
发明人： LINDERS, Joannes, Theodorus, Maria , ROEVENS, Peter, Walter, Maria , HRUPKA, Brian, Joel
IPC分类号： A61K31/4965
CPC分类号： A61K45/06 , A61K31/216 , A61K31/496 , C07D295/192 , A61K2300/00
摘要： The present invention relates to combinations of a DGAT inhibitor and a peroxisome proliferator-activator receptor (PPAR) agonist or a prodrug thereof. The invention further relates to methods for preparing such combinations, pharmaceutical compositions comprising said combinations as well as the use as a medicament of said combinations. The present invention also relates to novel DGAT inhibitors. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicament of said compounds.
摘要翻译：本发明涉及DGAT抑制剂和过氧化物酶体增殖物激活受体（PPAR）激动剂或其前药的组合。本发明还涉及制备这种组合的方法，包含所述组合的药物组合物以及作为所述组合的药物的用途。本发明还涉及新型DGAT抑制剂。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物的用途。

2. 发明申请

WO2008148868A1 PIPERIDINE/PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌啶/哌嗪衍生物
公开(公告)号：WO2008148868A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057060
申请日：2008-06-06
申请人： JANSSEN PHARMACEUTICA N.V. , BONGARTZ, Jean-Pierre, André, Marc , LINDERS, Joannes, Theodorus, Maria , MEERPOEL, Lieven , VAN LOMMEN, Guy, Rosalia, Eugeen , COESEMANS, Erwin , BRAEKEN, Mirielle , BUYCK, Christophe, Francis, Robert, Nestor , BERWAER, Monique, Jenny, Marie , DE WAEPENAERT, Katharina, Antonia, Germania, J.M. , ROEVENS, Peter, Walter, Maria , BOECKX, Gustaaf, Maria , DAVIDENKO, Petr, Vladimirivich
发明人： BONGARTZ, Jean-Pierre, André, Marc , LINDERS, Joannes, Theodorus, Maria , MEERPOEL, Lieven , VAN LOMMEN, Guy, Rosalia, Eugeen , COESEMANS, Erwin , BRAEKEN, Mirielle , BUYCK, Christophe, Francis, Robert, Nestor , BERWAER, Monique, Jenny, Marie , DE WAEPENAERT, Katharina, Antonia, Germania, J.M. , ROEVENS, Peter, Walter, Maria , BOECKX, Gustaaf, Maria , DAVIDENKO, Petr, Vladimirivich
IPC分类号： A61K31/4965 , C07D295/20 , A61P3/08
CPC分类号： C07D295/205 , C07D207/09 , C07D211/26 , C07D211/38 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/18 , C07D295/192 , C07D295/21 , C07D295/215 , C07D295/24 , C07D295/26 , C07D307/52 , C07D307/79 , C07D309/04 , C07D317/58 , C07D333/24
摘要： The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NR x -C(=O)-; -Z 1 -C(O)-; -Z 1 -NR x -C(=O)-; -C(=O)-Z 1 -; -NR x -C(=O)-Z 1 -; -S(=O)p-; -C(=S)-; -NR x -C(=S)-; -Z 1 -C(=S)-; -Z 1 -NR X -C(=S)-; -C(=S)-Z1-; -NR x -C(=S)-Z 1 -; Y represents NR x -C(=0)- Z 2 -; -NR x -C(=0)-Z 2 -NR y -; -NR x -C(=0)-Z 2 -NR y -C(=0)-; -NR x -C(=0)-Z 2 -NR y -C(=0)- O-; -NR x -C(=0)-Z 2 -0-; -NR x -C(=0)-Z 2 -0-C(=0)-; -NR x -C(=0)-Z 2 -C(=0)-; -NR x -C(=0)-Z 2 -C(=0)-0-; -NR x -C(=0)-0-Z 2 -C(=0)-; -NR x -C(=0)-0-Z 2 -C(=0)-0-; -NR x -C(=O)-O-Z 2 -O-C(=O)-; -NR x -C(=O)-Z 2 -C(=O)-NR y -; -NR x -C(=O)-Z 2 -NR y - C(=0)-NR y -; -C(=O)-Z 2 -; -C(=O)-Z 2 -O-; -C(=0)-NR x -Z 2 -; -C(=0)-NR x -Z 2 -0-; -C(=0)-NR x -Z 2 -C(=0)-0-; -C(=0)-NR x -Z 2 -0-C(=0)-; -C(=0)-NR x -0-Z 2 -; -C(=O)- NR x -Z 2 -NR y -; -C(=0)-NR x -Z 2 -NR y -C(=0)-; -C(=0)-NR x -Z 2 -NR y -C(=0)-0-; R 1 represents C 1-12 alkyl optionally substituted with cyano, C 1-4 alkyloxy, C 1-4 alkyl-oxyC 1-4 alkyloxy, C 3-6 Cy cloalkyl or aryl; C 2-6 alkenyl; C 2-6 alkynyl; C 3-6 cycloalkyl; adamantanyl; aryl 1 ; aryl 1 C 1-6 alkyl; Het 1 ; or Het 1 C 1-6 alkyl; provided that when Y represents -NR X -C(=O)-Z 2 -; -NR x -C(=0)-Z 2 -NR y ; -NR X -C(=O)-Z 2 -C(=O)- NR y -; -C(=O)-Z 2 -; -NR x -C(=0)-Z 2 -NR y -C(=0)-NR y -; -C(=O)-NR X -Z 2 -; -C(=O)-NR X - O-Z 2 -; or -C(=0)-NR x -Z 2 -NR y -; then R 1 may also represent hydrogen; R 2 represents hydrogen, C 1-12 alkyl, C 2-6 alkenyl or R 3 ; provided that if X represents -O-C(=O)-, then R 2 represents R 3 ; and provided that is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
摘要翻译：本发明涉及式（I）的DGAT抑制剂：包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-C（= O） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; -NRx-C（= O） - ; -Z1-C（O） - ; -Z1-NRX-C（= O） - ; -C（= O）-Z 1 - ; -NRx-C（= O）-Z 1 - ; -S（= O）p - ; -C（= S） - ; -NRx-C（= S） - ; -Z1-C（= S） - ; -Z1-NRX-C（= S） - ; -C（= S）-Z 1 - ; -NRx-C（= S）-Z 1 - ; Y表示NR x -C（= O）-Z 2 - ; -NRx-C（= O）-Z 2 -NR Y - ; -NRx-C（= O）-Z 2-NRY-C（= O） - ; -NR x -C（= O）-Z 2 -NR y -C（= O）-O-; -NRx-C（= O）-Z2-0-; -NRx-C（= O）-Z2-0-C（= O） - ; -NRx-C（= O）-Z 2-C（= O） - ; -NRx-C（= O）-Z 2-C（= O）-O-; -NRx-C（= O）-O-Z2-C（= O） - ; -NRx-C（= O）-O-Z2-C（= O）-O-; -NRx-C（= O）-O-Z2-O-C（= O） - ; -NRx-C（= O）-Z 2-C（= O）-NRy-; -NR x -C（= O）-Z 2 -NR y -C（= O）-NR y - ; -C（= O）-Z 2 - ; -C（= O）-Z 2-O-; -C（= O）-NRx-Z2-; -C（= O）-NRx-Z2-0-; -C（= O）-NRx-Z2-C（= O）-O-; -C（= O）-NRx-Z2-0-C（= O） - ; -C（= O）-NRx-0-Z2-; -C（= O）-NR x-Z 2 -NR y - ; -C（= O）-NRx-Z2-NRY-C（= O） - ; -C（= O）-NRx-Z2-NRY-C（= O）-O-; R 1表示任选被氰基，C 1-4烷氧基，C 1-4烷基 - 氧基C 1-4烷氧基，C 3-6环烷基或芳基取代的C 1-12烷基; 2-6链烯基; C 2-6炔基; 3-6环; 金刚烷基; aryl1; aryl1C1-6alkyl; 的Het1; 或Het1C 1-6烷基; 条件是当Y表示-NR X-C（= O）-Z 2; -NRx-C（= O）-Z 2-NRY; -NR X-C（= O）-Z 2 -C（= O）-NR y - ; -C（= O）-Z 2 - ; -NRx-C（= O）-Z 2-NRY-C（= O）-NRy-; -C（= O）-NRX-Z2-; -C（= O）-NRX-O-Z 2 - ; 或-C（= O）-NR x-Z 2 -NR y - ; 那么R1也可以代表氢; R2代表氢，C1-12烷基，C2-6烯基或R3; 条件是如果X表示-O-C（= O） - ，则R2表示R3; 并且排除在外; 其N-氧化物，其药学上可接受的盐或其溶剂合物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。

3. 发明申请

WO2008068265A1 NOVEL SUBSTITUTED DIAZA SPIRO PYRIDINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES 审中-公开
标题翻译：新一代采用DIAZA SPIRO PYRIDINONE衍生物用于MCH-1介导的疾病
公开(公告)号：WO2008068265A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/063310
申请日：2007-12-04
申请人： JANSSEN PHARMACEUTICA N.V. , ANDRÉS-GIL, José, Ignacio , ALCÁZAR-VACA, Manuel, Jesús , DAUTZENBERG, Frank, Matthias , LINDERS, Joannes, Theodorus, Maria
发明人： ANDRÉS-GIL, José, Ignacio , ALCÁZAR-VACA, Manuel, Jesús , DAUTZENBERG, Frank, Matthias , LINDERS, Joannes, Theodorus, Maria
IPC分类号： C07D471/10 , C07D498/10 , A61K31/4427 , A61K31/5386 , A61P3/04 , A61P3/06 , A61P25/22 , A61P25/24
CPC分类号： C07D471/10 , C07D498/10
摘要： The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.
摘要翻译：本发明涉及具有拮抗性黑色素浓缩激素（MCH）活性，特别是根据通式（I）的MCH-1活性的芳基和杂芳基取代的二氮杂 - 螺 - 吡啶酮衍生物，其药学上可接受的酸或碱加成盐，其N-氧化物形式或其季铵盐，其中变量在权利要求1中定义。它还涉及它们的制备方法，包含它们的组合物及其作为药物的用途。根据本发明的化合物可用于预防和/或治疗精神病学障碍，包括但不限于焦虑，进食障碍，情绪障碍，例如双相性精神障碍和抑郁症，精神病如精神分裂症和睡眠障碍; 肥胖; 糖尿病; 性障碍和神经障碍。

4. 发明申请

WO2005108360A1 PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译：吡咯烷-2-酮和哌啶-2-酮衍生物作为11-羟基甾醇脱氢酶抑制剂
公开(公告)号：WO2005108360A1
公开(公告)日：2005-11-17
申请号：PCT/EP2005/051968
申请日：2005-04-29
申请人： JANSSEN PHARMACEUTICA N.V. , JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , BUYCK, Christophe, Francis, Robert, Nestor , VAN DER VEKEN, Louis Jozef Elisabeth , DIMITROV, Vladimir, Dimtchev , NIKIFOROV, Theo, Teofanov
发明人： JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , BUYCK, Christophe, Francis, Robert, Nestor , VAN DER VEKEN, Louis Jozef Elisabeth , DIMITROV, Vladimir, Dimtchev , NIKIFOROV, Theo, Teofanov
IPC分类号： C07D207/26
CPC分类号： C07D211/76 , C07D207/26 , C07D207/267 , C07D405/06
摘要： Formula (I), the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C 1-3 alkyl linker optionally substituted with one or two substituents selected from C 1-4 alkyl, C 1-3 alkyloxy-C 1-4 alkyl-, hydroxy-C 1-4 alkyl, hydroxy, C 1-3 alkyloxy- or phenyl-C 1-4 alkyl; M represents a direct bond or a C 1-3 alkyl linker optionally substituted with one or two substituents selected from hydroxy, C 1-4 alkyl or C 1-4 alkyloxy; R 1 and R 2 each independently represent hydrogen, halo, cyano, hydroxy, C 1-4 alkyl optionally substituted with halo, C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar 1 and halo; or R 1 and R 2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R 3 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyloxy-, cyano or hydroxy; R 4 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyloxy-, cyano or hydroxy; R 5 represents hydrogen, C 1-4 alkyl or Ar 2 -C 1-4 alky-; R 6 represents hydrogen, halo, C 1-4 alkyl Or C 1-4 alkyoxy-; Ar 1 and Ar 2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C 1-4 alkyl, C 1-4 alkyloxy-, or phenyl-C 1-4 alkyl; for use as a medicine.
摘要翻译：式（I），N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n为1或2; L表示任选被一个或两个选自C 1-4烷基，C 1-3烷氧基-C 1-4烷基 - ，羟基-C 1-4烷基，羟基，C 1-3烷氧基或苯基-C 1-4烷基的取代基取代的C 1-3烷基接头。 M表示直接键或任选被一个或两个选自羟基，C 1-4烷基或C 1-4烷氧基的取代基取代的C 1-3烷基接头; R 1和R 2各自独立地表示氢，卤素，氰基，羟基，任选被卤素取代的C 1-4烷基，C 1-4烷氧基 - 任选被一个或任选被两个或三个选自羟基，Ar 1 >和光环; 或R 1和R 2与它们所连接的苯环一起形成萘基或1,3-苯并二恶唑基，其中所述萘基或1,3-苯并二恶唑基任选被卤素取代; R 3表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R 4表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R 5表示氢，C 1-4烷基或Ar 2 -C 1-4烷基; R 6表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; Ar 1和Ar 2各自独立地表示苯基或萘基，其中所述苯基和萘基任选被C 1-4烷基，C 1-4烷氧基 - 或苯基-C 1-4烷基取代; 用作药物。

5. 发明申请

WO2005058824A3 N-ARYL PIPERIDINE SUBSTITUTED BIPHENYLCARBOXAMIDES AS INHIBITORS OF APOLIPOPROTE IN B 审中-公开
公开(公告)号：WO2005058824A3
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053280
申请日：2004-12-06
申请人： JANSSEN PHARMACEUTICA N.V. , MEERPOEL, Lieven , VIELLEVOYE, Marcel , LINDERS, Joannes, Theodorus, Maria
发明人： MEERPOEL, Lieven , VIELLEVOYE, Marcel , LINDERS, Joannes, Theodorus, Maria
IPC分类号： C07D211/60
摘要： N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I), methods for preparing compounds, pharmaceutical compositions comprising said compounds as wee as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.

6. 发明申请

WO2009133052A1 BENZOCYCLOHEPTANE AND BENZOXEPINE DERIVATIVES 审中-公开
标题翻译：苯并噻吩和苯并吡喃衍生物
公开(公告)号：WO2009133052A1
公开(公告)日：2009-11-05
申请号：PCT/EP2009/055034
申请日：2009-04-27
申请人： JANSSEN PHARMACEUTICA NV , SCHOENTJES, Bruno , PONCELET, Alain, Philippe , DOYON, Julien, Georges, Pierre-Olivier , LINDERS, Joannes, Theodorus, Maria , MEERPOEL, Lieven , VER DONCK, Luc, August, Laurentius
发明人： SCHOENTJES, Bruno , PONCELET, Alain, Philippe , DOYON, Julien, Georges, Pierre-Olivier , LINDERS, Joannes, Theodorus, Maria , MEERPOEL, Lieven , VER DONCK, Luc, August, Laurentius
IPC分类号： C07C215/44 , C07C217/52 , C07C313/08 , C07C213/02 , C07C213/08 , A61K31/135 , A61K31/335
CPC分类号： C07C215/42 , C07C35/52 , C07C43/192 , C07C215/64 , C07C217/08 , C07C217/74 , C07C2602/12 , C07D207/06 , C07D213/53 , C07D213/65 , C07D215/14 , C07D239/26 , C07D295/092 , C07D295/096 , C07D295/16 , C07D313/08 , C07D317/58 , C07D405/04 , C07D407/04
摘要： The present invention relates to a compound of formula (I), including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N -oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than formula (B) or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
摘要翻译：本发明涉及式（I）化合物，包括其任何立体化学异构形式，其中取代基如说明书和权利要求书中所定义; 其N-氧化物，其药学上可接受的盐或其溶剂合物; 条件是该化合物不是式（B）化合物或其药学上可接受的盐。要求保护的化合物可用于治疗通过激活GHS1A-r受体而影响，介导或促进的疾病的治疗。本发明还涉及其药物组合物及其制备方法。

7. 发明申请

WO2008148849A8 PIPERIDINE/PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌啶/哌嗪衍生物
公开(公告)号：WO2008148849A8
公开(公告)日：2009-07-09
申请号：PCT/EP2008057008
申请日：2008-06-05
申请人： JANSSEN PHARMACEUTICA NV , BONGARTZ JEAN-PIERRE ANDRE MARC , LINDERS JOANNES THEODORUS MARIA , MEERPOEL LIEVEN , VAN LOMMEN GUY ROSALIA EUGEEN , COESEMANS ERWIN , BRAEKEN MIRIELLE , BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR , BERWAER MONIQUE JENNY MARIE , DE WAEPENAERT KATHARINA ANTONIA GERMANIA J M , ROEVENS PETER WALTER MARIA , DAVIDENKO PETR VLADIMIRIVICH
发明人： BONGARTZ JEAN-PIERRE ANDRE MARC , LINDERS JOANNES THEODORUS MARIA , MEERPOEL LIEVEN , VAN LOMMEN GUY ROSALIA EUGEEN , COESEMANS ERWIN , BRAEKEN MIRIELLE , BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR , BERWAER MONIQUE JENNY MARIE , DE WAEPENAERT KATHARINA ANTONIA GERMANIA J M , ROEVENS PETER WALTER MARIA , DAVIDENKO PETR VLADIMIRIVICH
IPC分类号： A61K31/451 , A61K31/495 , A61P3/06 , A61P9/00 , A61P35/00 , C07D295/135
CPC分类号： A61K31/4523 , A61K31/451 , A61K31/454 , A61K31/495 , A61K31/496 , C07D207/277 , C07D207/323 , C07D211/26 , C07D211/60 , C07D231/12 , C07D233/54 , C07D233/64 , C07D235/18 , C07D249/08 , C07D257/04 , C07D263/34 , C07D277/56 , C07D279/02 , C07D279/12 , C07D295/20 , C07D295/205 , C07D295/21 , C07D295/215 , C07D307/54 , C07D319/18 , C07D401/12 , C07D417/12 , C07D417/14
摘要： The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C(=O)-; -C(=O)-C(=O)-; -NRX-C(=O)-; -Z-C(=O)-; -Z-NRX-C(=O)-; -C(=O)-Z-; -NRX-C(=O)-Z-; -C(=S)-; -NRX-C(=S)-; -Z-C(=S)-; -Z-NRX-C(=S)-; - C(=S)-Z-; -NRX-C(=S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C(=O)-NRX- or -NRX-C(=O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3- dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (A), (B) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
摘要翻译：本发明涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-O-C（= O） - ; -C（= O）-C（= O） - ; -NRX-C（= O） - ; -Z-C（= O） - ; -Z-NRX-C（= O） - ; -C（= O）-Z-; -NRX-C（= O）-Z-; -C（= S） - ; -NRX-C（= S） - ; -Z-C（= S） - ; -Z-NRX-C（= S） - ; -C（= S）-Z-; -NRX-C（= S）-Z-; Z表示选自C 1-6烷二基，C 2-6亚烯基或C 2-6炔二基的二价基团; 其中所述C 1-6烷二基，C 2-6亚烯基或C 2-6炔二基中的每一个可任选被取代; 并且其中连接在C 1-6烷二基中的相同碳原子上的两个氢原子可任选地被C 1-6烷二基取代; Y表示-C（= O）-NRX-或-NRX-C（= O） - ; R1表示金刚烷基，C3-6环烷基; 芳基1或Het1; R2代表C3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含有1或2个N原子的6元芳族杂环，其中所述C3 -6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶英，1,3-苯并二恶唑基或杂环可以任选被取代; R 7表示氢，卤素，C 1-4烷基，被羟基取代的C 1-4烷基; 条件是排除以下化合物（A），（B）; 其N-氧化物，其药学上可接受的盐或其溶剂合物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及作为所述化合物的DGAT抑制剂的药物用途。

8. 发明申请

WO2008148868A8 PIPERIDINE/PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌啶/哌嗪衍生物
公开(公告)号：WO2008148868A8
公开(公告)日：2009-03-05
申请号：PCT/EP2008057060
申请日：2008-06-06
申请人： JANSSEN PHARMACEUTICA NV , BONGARTZ JEAN-PIERRE ANDRE MARC , LINDERS JOANNES THEODORUS MARIA , MEERPOEL LIEVEN , VAN LOMMEN GUY ROSALIA EUGEEN , COESEMANS ERWIN , BRAEKEN MIRIELLE , BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR , BERWAER MONIQUE JENNY MARIE , DE WAEPENAERT KATHARINA ANTONIA GERMANIA J M , ROEVENS PETER WALTER MARIA , BOECKX GUSTAAF MARIA , DAVIDENKO PETR VLADIMIRIVICH
发明人： BONGARTZ JEAN-PIERRE ANDRE MARC , LINDERS JOANNES THEODORUS MARIA , MEERPOEL LIEVEN , VAN LOMMEN GUY ROSALIA EUGEEN , COESEMANS ERWIN , BRAEKEN MIRIELLE , BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR , BERWAER MONIQUE JENNY MARIE , DE WAEPENAERT KATHARINA ANTONIA GERMANIA J M , ROEVENS PETER WALTER MARIA , BOECKX GUSTAAF MARIA , DAVIDENKO PETR VLADIMIRIVICH
IPC分类号： A61K31/4965 , A61P3/08 , C07D295/20
CPC分类号： C07D295/205 , C07D207/09 , C07D211/26 , C07D211/38 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/18 , C07D295/192 , C07D295/21 , C07D295/215 , C07D295/24 , C07D295/26 , C07D307/52 , C07D307/79 , C07D309/04 , C07D317/58 , C07D333/24
摘要： The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NRx-C(=O)-; -Z1-C(O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(=O)-Z1-; -S(=O)p-; -C(=S)-; -NRx-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(=S)-Z1-; Y represents NRx-C(=0)- Z2-; -NRx-C(=0)-Z2-NRy-; -NRx-C(=0)-Z2-NRy-C(=0)-; -NRx-C(=0)-Z2-NRy-C(=0)- O-; -NRx-C(=0)-Z2-0-; -NRx-C(=0)-Z2-0-C(=0)-; -NRx-C(=0)-Z2-C(=0)-; -NRx-C(=0)-Z2-C(=0)-0-; -NRx-C(=0)-0-Z2-C(=0)-; -NRx-C(=0)-0-Z2-C(=0)-0-; -NRx-C(=O)-O-Z2-O-C(=O)-; -NRx-C(=O)-Z2-C(=O)-NRy-; -NRx-C(=O)-Z2-NRy- C(=0)-NRy-; -C(=O)-Z2-; -C(=O)-Z2-O-; -C(=0)-NRx-Z2-; -C(=0)-NRx-Z2-0-; -C(=0)-NRx-Z2-C(=0)-0-; -C(=0)-NRx-Z2-0-C(=0)-; -C(=0)-NRx-0-Z2-; -C(=O)- NRx-Z2-NRy-; -C(=0)-NRx-Z2-NRy-C(=0)-; -C(=0)-NRx-Z2-NRy-C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cy cloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents -NRX-C(=O)-Z2-; -NRx-C(=0)-Z2-NRy; -NRX-C(=O)-Z2-C(=O)- NRy-; -C(=O)-Z2-; -NRx-C(=0)-Z2-NRy-C(=0)-NRy-; -C(=O)-NRX-Z2-; -C(=O)-NRX- O-Z2-; or -C(=0)-NRx-Z2-NRy-; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents -O-C(=O)-, then R2 represents R3; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
摘要翻译：本发明涉及式（I）的DGAT抑制剂：包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-C（= O） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; -NRx-C（= O） - ; -Z1-C（O） - ; -Z1-NRX-C（= O） - ; -C（= O）-Z 1 - ; -NRx-C（= O）-Z 1 - ; -S（= O）p - ; -C（= S） - ; -NRx-C（= S） - ; -Z1-C（= S） - ; -Z1-NRX-C（= S） - ; -C（= S）-Z 1 - ; -NRx-C（= S）-Z 1 - ; Y表示NR x -C（= O）-Z 2 - ; -NRx-C（= O）-Z 2 -NR Y - ; -NRx-C（= O）-Z 2-NRY-C（= O） - ; -NR x -C（= O）-Z 2 -NR y -C（= O）-O-; -NRx-C（= O）-Z2-0-; -NRx-C（= O）-Z2-0-C（= O） - ; -NRx-C（= O）-Z 2-C（= O） - ; -NRx-C（= O）-Z 2-C（= O）-O-; -NRx-C（= O）-O-Z2-C（= O） - ; -NRx-C（= O）-O-Z2-C（= O）-O-; -NRx-C（= O）-O-Z2-O-C（= O） - ; -NRx-C（= O）-Z 2-C（= O）-NRy-; -NR x -C（= O）-Z 2 -NR y -C（= O）-NR y - ; -C（= O）-Z 2 - ; -C（= O）-Z 2-O-; -C（= O）-NRx-Z2-; -C（= O）-NRx-Z2-0-; -C（= O）-NRx-Z2-C（= O）-O-; -C（= O）-NRx-Z2-0-C（= O） - ; -C（= O）-NRx-0-Z2-; -C（= O）-NR x-Z 2 -NR y - ; -C（= O）-NRx-Z2-NRY-C（= O） - ; -C（= O）-NRx-Z2-NRY-C（= O）-O-; R 1表示任选被氰基，C 1-4烷氧基，C 1-4烷基 - 氧基C 1-4烷氧基，C 3-6环烷基或芳基取代的C 1-12烷基; 2-6链烯基; C 2-6炔基; 3-6环; 金刚烷基; aryl1; aryl1C1-6alkyl; 的Het1; 或Het1C 1-6烷基; 条件是当Y表示-NR X-C（= O）-Z 2; -NRx-C（= O）-Z 2-NRY; -NR X-C（= O）-Z 2 -C（= O）-NR y - ; -C（= O）-Z 2 - ; -NRx-C（= O）-Z 2-NRY-C（= O）-NRy-; -C（= O）-NRX-Z2-; -C（= O）-NR X-O-Z 2 - ; 或-C（= O）-NR x-Z 2 -NR y - ; 那么R1也可以代表氢; R2代表氢，C1-12烷基，C2-6烯基或R3; 条件是如果X表示-O-C（= O） - ，则R2表示R3; 并且（A）被排除在外; 其N-氧化物，其药学上可接受的盐或其溶剂合物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。

9. 发明申请

WO2008092862A1 BICYCLIC DERIVATIVES AS EP4 AGONISTS 审中-公开
标题翻译：双酚A衍生物作为EP4 AGONISTS
公开(公告)号：WO2008092862A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051045
申请日：2008-01-29
申请人： JANSSEN PHARMACEUTICA N.V. , LINDERS, Joannes, Theodorus, Maria , VAN LOMMEN, Guy, Rosalia, Eugeen , VAN DER VEKEN, Louis, Jozef, Elisabeth , HENDRICKX, Robert, Jozef, Maria , VAN WAUWE, Jean, Pierre, Frans , AERSSENS, Jeroen, Marcel, Maria, Roger , D'LAVARI, Mansoor , FILIP, Sorin-Vasile , LOWERSON, Kenneth, Andrew , DAVIDENKO, Petr, Vladimirivich , REYNOV, Mikhail, Viktorovich
发明人： LINDERS, Joannes, Theodorus, Maria , VAN LOMMEN, Guy, Rosalia, Eugeen , VAN DER VEKEN, Louis, Jozef, Elisabeth , HENDRICKX, Robert, Jozef, Maria , VAN WAUWE, Jean, Pierre, Frans , AERSSENS, Jeroen, Marcel, Maria, Roger , D'LAVARI, Mansoor , FILIP, Sorin-Vasile , LOWERSON, Kenneth, Andrew , DAVIDENKO, Petr, Vladimirivich , REYNOV, Mikhail, Viktorovich
IPC分类号： C07D495/04 , A61P43/00 , A61K31/519
CPC分类号： C07D495/04
摘要： The present invention relates to a compound of formula (I) including any stereochemical isomeric form thereof, wherein A represents a 5 or 6-membered aromatic optionally substituted heterocycle containing 1, 2 or 3 heteroatoms; ring E represents a partially saturated or aromatic 5-membered heterocycle wherein the dotted lines represent an optional double bond and wherein B, C and D each independently represent CH 2 , CH, N, NH, S or O and F represents N or C, provided that the 5-membered ring contains 1, 2 or 3 heteroatoms; X represents a direct bond or C 1-4 alkanediyl; Y represents N or CH; R 1 represents hydrogen or fluoro; R 2 represents hydrogen, halo, cyano, C 1-6 alkyl, C 1-6 alkyloxy, C 1-6 alkylcarbonyl or C 1-6 alkylcarbonylamino; R 3 represents hydrogen, halo, C 1-6 alkyl, C 1-6 alkyloxy, cyano, nitro, amino or mono-or di(C 1-6 alkyl)amino; n represents an integer of value 1, 2 or 3; a N -oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a disease by activating the EP4 receptor.
摘要翻译：本发明涉及包括其任何立体化学异构形式的式（I）化合物，其中A表示含有1,2或3个杂原子的5或6元芳族任选取代的杂环; 环E表示部分饱和或芳族5元杂环，其中虚线表示任选的双键，并且其中B，C和D各自独立地表示CH 2，CH，N，NH，S或O 并且F表示N或C，条件是5元环含有1,2或3个杂原子; X表示直接键或C 1-4烷二基; Y表示N或CH; R 1表示氢或氟; R 2表示氢，卤素，氰基，C 1-6烷基，C 1-6烷基氧基，C 1-6烷基，烷基羰基或C 1-6烷基羰基氨基; R 3表示氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，硝基，氨基或单 - 或二 - （C _{1-6 烷基）氨基; n表示数值1,2或3的整数; 其N-氧化物，其药学上可接受的盐或其溶剂合物。所要求保护的化合物可用于通过激活EP4受体来治疗疾病。}

10. 发明申请

WO2006117307A2 BENZOTRIAZOLE DERIVATIVES AS CANNABINOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯并噻唑衍生物作为CANNABINOID受体拮抗剂
公开(公告)号：WO2006117307A2
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061787
申请日：2006-04-24
申请人： JANSSEN PHARMACEUTICA N.V. , BERWAER, Monique Jenny Marie , LINDERS, Joannes Theodorus Maria , KING, Peter John , VAN HECKE, Geert Maria Robert
发明人： BERWAER, Monique Jenny Marie , LINDERS, Joannes Theodorus Maria , KING, Peter John , VAN HECKE, Geert Maria Robert
CPC分类号： A61K31/4192 , C07D249/18 , C07D403/06 , C07D417/06
摘要： The present invention relates to a group of benzotriazole derivatives, infra that are potent cannabinoid-CB i modulators (known as antagonists or inverse agonists), useful in the treatment obesity, psychiatric and neurological disorders, as well as other diseases involving cannabinoid-CB 1 neurotransmission (Current Opinion in Drug Discovery & Development 2004 7(4):498-506) the pharmaceutically acceptable acid addition salts and stereoisomeric forms thereof, wherein R I is hydrogen, halo, trifluoromethyl, C 1-4 alkyl, C 1-4 alkyloxy- or C 1-4 alkyloxycarbonyl; R 2 is hydrogen, phenyl, C 3-7 cycloalkyl or C 1-6 alkyl optionally substituted with Ar 1 ; R 3 is hydrogen, hydroxyl or C 1-6 alkyl; Ar 1 is phenyl or phenyl substituted with up to three halo substituents; and Het represents a monocyclic 5 or 6 membered partially saturated or aromatic heterocycle selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, pyrimidinyl, pyridinyl, pyrazinyl, triazinyl, pyridazinyl, 2H-pyranyl or 4H-pyranyl wherein said heterocycle is optionally substituted with C 1-6 alkyl.
摘要翻译：本发明涉及以下一组苯并三唑衍生物，以下是可用于治疗肥胖症，精神病学和神经障碍的有效大麻素-CBI调节剂（称为拮抗剂或反向激动剂），以及涉及大麻素CB 1神经传递（Current Opinion in Drug Discovery＆Development 2004,7（4）：498-506）的其它疾病，其药学上可接受的酸加成盐和立体异构形式，其中R I 氢，卤素，三氟甲基，C 1-4烷基，C 1-4烷基氧基或C 1-4烷基氧基羰基 ; R 2是氢，苯基，C 3-7环烷基或任选被Ar 1或O 2取代的C 1-6烷基 >; R 3是氢，羟基或C 1-6烷基; Ar 1是苯基或被至多3个卤素取代基取代的苯基; 并且Het表示选自呋喃基，噻吩基，吡咯基，恶唑基，噻唑基，咪唑基，吡唑基，异唑基，异噻唑基，恶二唑基，三唑基，噻二唑基，嘧啶基，吡啶基，吡嗪基，三嗪基，哒嗪基，吡嗪基等的单环5或6元部分饱和或芳族杂环。其中所述杂环任选被C 1-6烷基取代。

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