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1. 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。

2. 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。

3. 发明申请

WO2008148849A2 PIPERIDINE/PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌啶/哌嗪衍生物
公开(公告)号：WO2008148849A2
公开(公告)日：2008-12-11
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 , 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 , 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 (II), (III) 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（II），（III）; 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。

4. 发明申请

WO2007090836A3 PIPERIDINE DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为CXCR3受体拮抗剂的哌啶衍生物
公开(公告)号：WO2007090836A3
公开(公告)日：2007-11-29
申请号：PCT/EP2007051123
申请日：2007-02-06
申请人： JANSSEN PHARMACEUTICA NV , COESEMANS ERWIN , BONGARTZ JEAN-PIERRE ANDRE MAR , VAN LOMMEN GUY ROSALIA EUGEEN
发明人： COESEMANS ERWIN , BONGARTZ JEAN-PIERRE ANDRE MAR , VAN LOMMEN GUY ROSALIA EUGEEN
IPC分类号： A61K31/4545 , A61P29/00 , C07D211/26 , C07D211/96 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： C07D211/96 , C07D211/26 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to a compound of formula (I),a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y represents a direct bond, CH 2 -C(=O) wherein the CH 2 is attached to the N of the piperidine ring, C(=O) or S(=O) p ; p represents an integer of value 1 or 2; R 1 represents CH(R 4 )-aryl or CH(R 4 )-heteroaryl; R 2 represents aryl 2 or heteroaryl; R 3 represents hydrogen, C 1-6 alkyl, polyhaloC 1 -6 alkyl, C 1-6 alkyloxy, aryl 1 , aryl 1 -NH-, heteroaryl, heteroaryl-NH-, C 3-7 cycloalkyl, amino or mono or di(C 1 -4 alkyl)amino. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）化合物，其N-氧化物，其药学上可接受的盐，其立体化学异构形式或其溶剂合物，其中X表示N或CH; Y表示直接键合CH 2，其中CH 2 N连接到哌啶环的N，C（= O）或S（= O） = O）_{p ; p表示1或2的整数; R 1表示CH（R 4） - 芳基或CH（R 4 H 4） - 杂芳基; R 2表示芳基2或杂芳基; R 3表示氢，C 1-6烷基，多卤C 1-6烷基，C 1-6烷氧基，芳基1，芳基-NH-，杂芳基，杂芳基-NH-，C 3-7环烷基，氨基或单或二（ C 1-4烷基）氨基。本发明还涉及式（I）化合物在制备用于预防或治疗通过活化CXCR3受体介导的疾病的药物中的用途; 制备式（I）化合物的方法和包含它们的药物组合物。}

5. 发明专利

CA2687912C PIPERIDINE/PIPERAZINE DERIVATIVES 未知
公开(公告)号：CA2687912C
公开(公告)日：2015-11-03
申请号：CA2687912
申请日：2008-06-05
申请人： JANSSEN PHARMACEUTICA NV
发明人： BONGARTZ JEAN-PIERRE ANDRE MARC , MEERPOEL LIEVEN , BOECKX GUSTAAF MARIA , VAN LOMMEN GUY ROSALIA EUGEEN , BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR , OBRECHT DANIEL , ERMERT PHILIPP , LUTHER ANATOL
IPC分类号： C07D487/04 , A61K31/40 , A61K31/4188 , A61K31/4196 , A61K31/4245 , A61P1/16 , A61P3/00 , A61P3/08 , C07D231/12 , C07D249/08
摘要： The invention further 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 -NRx -C(=O)-; -Z-C(=O)-; -Z-NRx -C(=O)-; -S(=O)p-; C(=S)-; -NRx -C(=S)-; -Z-C(=S)-; -Z-NRx -C(=S)-; -O-C(=O)-; -C(=O)-C(=O)-; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 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-benzo- dioxinyl, 1,3-benzodioxolyl,2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; 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.

6. 发明专利

AU2008258560C1 Piperidine/piperazine derivatives 未知
公开(公告)号：AU2008258560C1
公开(公告)日：2014-04-10
申请号：AU2008258560
申请日：2008-06-05
申请人： JANSSEN PHARMACEUTICA NV
发明人： BONGARTZ JEAN-PIERRE ANDRE MARC , BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR , COESEMANS ERWIN , VAN LOMMEN GUY ROSALIA EUGEEN
IPC分类号： C07D295/20 , A61K31/4965
摘要： The invention relates to a DGAT inhibitor of formula (I) including any stereochemically isomeric form thereof, wherein A represents CH or N; X represents O or NR

7. 发明专利

AU2008258549B2 Piperidine/piperazine derivatives 未知
公开(公告)号：AU2008258549B2
公开(公告)日：2013-11-14
申请号：AU2008258549
申请日：2008-06-05
申请人： JANSSEN PHARMACEUTICA NV
发明人： OBRECHT DANIEL , LUTHER ANATOL , MEERPOEL LIEVEN , VAN LOMMEN GUY ROSALIA EUGEEN , BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR , ERMERT PHILIPP , BOECKX GUSTAAF MARIA , BONGARTZ JEAN-PIERRE ANDRE MARC
IPC分类号： C07D239/26 , A61K31/497 , A61K31/506 , A61P3/08 , C07D239/42 , C07D249/08 , C07D249/12 , C07D487/04
摘要： The invention further 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 -NR

8. 发明专利

BRPI0707629A2 未知
公开(公告)号：BRPI0707629A2
公开(公告)日：2011-05-10
申请号：BRPI0707629
申请日：2007-02-06
申请人： JANSSEN PHARMACEUTICA NV
发明人： COESEMANS ERWIN , VAN LOMMEN GUY ROSALIA EUGEEN , BONGARTZ JEAN-PIERRE ANDRE MARC
IPC分类号： A61K31/4545 , A61P29/00 , C07D211/26 , C07D211/96 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to a compound of formula (I),a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y represents a direct bond, CH 2 -C(=O) wherein the CH 2 is attached to the N of the piperidine ring, C(=O) or S(=O) p ; p represents an integer of value 1 or 2; R 1 represents CH(R 4 )-aryl or CH(R 4 )-heteroaryl; R 2 represents aryl 2 or heteroaryl; R 3 represents hydrogen, C 1-6 alkyl, polyhaloC 1 -6 alkyl, C 1-6 alkyloxy, aryl 1 , aryl 1 -NH-, heteroaryl, heteroaryl-NH-, C 3-7 cycloalkyl, amino or mono or di(C 1 -4 alkyl)amino. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.

9. 发明专利

CL2008001669A1 Compuestos derivados de piperidina/piperazina inhibidora de dgat-1; procedimiento de preparacion; composicion farmaceutica que comprende a dicho compuesto; y uso en el tratamiento de la obesidad, dislipidemia, fibrosis hepatica y diabetes tipo ii, entre otras. 未知
公开(公告)号：CL2008001669A1
公开(公告)日：2009-07-17
申请号：CL2008001669
申请日：2008-06-06
申请人： JANSSEN PHARMACEUTICA NV
发明人： MEERPOEL LIEVEN , BONGARTZ JEAN PIERRE ANDRE MARC , VAN LOMMEN GUY ROSALIA EUGEEN , BOECKX GUSTAAF MARIA , BUYCK CHRITOPHE FRANCIS ROBET NESTOR , OBRECHT DANIEL , ERMERT PHILLIPP , LUTHER ANATOL
IPC分类号： A61K31/496 , A61P3/00 , A61P3/06 , A61P3/10 , C07D231/00 , C07D233/00 , C07D487/04
摘要： COMPUESTO INHIBIDOR DE DGAT DE FÓRMULA QUE INCLUYE CUALQUIER FORMA ESTEREOQUÍMICAMENTE ISOMÉRICA DEL MISMO, DONDE A, LA LÍNEA PUNTEADA, X, R, R2 Y R 8 SON COMO SE DEFINEN EN LA MEMORIA DESCRIPTIVA, N-ÓXIDO DE LOS MISMOS, UNA SAL ACEPTABLE PARA USO FARMACÉUTICO DE LOS MISMOS O UN SOLVATO DE LOS MISMOS. ADEMÁS, LA INVENCIÓN SE REFIERE A PROCESOS PARA PREPARAR TALES COMPUESTOS, COMPOSICIONES FARMACÉUTICAS QUE COMPRENDE A DICHOS COMPUESTOS ASÍ COMO AL USO COMO MEDICAMENTO DE DICHOS COMPUESTOS.

10. 发明专利

ES2317247T3 MERCAPTOIMIDAZOLES COMO ANTAGONISTAS DEL RECEPTOR CCR2. 未知
公开(公告)号：ES2317247T3
公开(公告)日：2009-04-16
申请号：ES05749653
申请日：2005-05-24
申请人： JANSSEN PHARMACEUTICA NV
发明人： BOECKX GUSTAAF MARIA , VAN LOMMEN GUY ROSALIA EUGEEN , DOYON JULIEN GEORGES PIERRE-OLIVIER , COESEMANS ERWIN
IPC分类号： C07D403/04 , A61K31/4164 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/506 , C07D233/84 , C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04
摘要： Un compuesto de fórmula (I)** ver fórmula** un N-óxido, una sal de adición farmacéuticamente aceptable, una amina cuaternaria o una forma estereoquímicamente isómera del mismo, en la que R1 representa alquilo C1-6; cada R2 representa independientemente halo o polihalo-alquilo C1-6; R3 representa hidrógeno, ciano, alquilo C1-6 opcionalmente sustituido con hidroxi o alquil C1-6-oxi, C(=O)-O- R5, C(=O)-NR6aR6b, C(=S)-NR6aR6b, S(=O)2-NR6aR6b o C(=O)-R7; R4 representa hidrógeno; R5 representa hidrógeno, alquilo C1-6, hidroxi-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, polihalo-alquilo C1-6, alquil C1-6-oxi-alquilo C1-6, amino-alquilo C1-6, mono- o di(alquil C1-4)amino-alquilo C1-6, aminocarbonilalquilo C 1-6, mono- o di(alquil C 1-4)-aminocarbonil-alquilo C 1-6, o arilo; R 6a y R 6b representan cada uno independientemente hidrógeno, alquilo C 1-6, amino, mono- o di(alquil C 1-4)amino, arilNH-, amino-alquilo C 1-6, mono- o di(alquil C 1-4)amino-alquilo C 1-6, alquil C 1-6-carbonilamino, aminocarbonilamino, alquil C1-6-oxi, carbonilamino o hidroxi-alquilo C1-6; o R6a y R6b, tomados junto con el nitrógeno al que están unidos, forman pirrolidinilo, imidazolidinilo, pirazolidinilo, piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo o piperazinilo sustituido con alquilo C1-6; R7 representa hidrógeno, alquilo C1-6, hidroxi-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, polihalo-alquilo C1-6, alquil C1-6-oxi-alquilo C1-6, amino-alquilo C1-6, mono- o di(alquil C1-4)amino-alquilo C1-6, aminocarbonilalquilo C 1-6, mono- o di(alquil C 1-4)aminocarbonil-alquilo C 1-6, arilo o heteroarilo; Z representa un sistema anular cíclico seleccionado de ** ver fórmula** cada R 8 representa independientemente hidrógeno, halo, alquilo C 1-6, alquil C 1-6-oxi, polihalo-alquilo C 1-6, polihalo-alquil C 1-6-oxi, ciano, aminocarbonilo, mono- o di(alquil C 1-4)-aminocarbonilo, amino, mono- o di (alquil C1-4)-amino, hidroxi-alquil C1-6-amino, arilo, ariloxi, piperidinilo, piperidinilamino, morfolinilo, piperazinilo o nitro; cada R9 representa independientemente hidrógeno, halo o alquilo C1-6; n es 1, 2, 3, 4 ó 5; arilo representa fenilo o fenilo sustituido con uno, dos, tres, cuatro o cinco sustituyentes seleccionados cada uno independientemente de halo, alquilo C1-6, alquil C1-6-oxi, polihalo-alquilo C1-6, polihalo-alquil C1-6-oxi, ciano, aminocarbonilo, mono- o di(alquil C 1-4)-aminocarbonilo, amino, mono- o di(alquil C 1-4)-amino, feniloxi o nitro; heteroarilo representa furanilo, tienilo, pirrolilo, oxazolilo, tiazolilo, imidazolilo, pirazolilo, isoxazolilo, isotiazolilo, oxadiazolilo, triazolilo, tiadiazolilo, piridilo, piridazinilo, pirimidinilo, pirazinilo, estando cada uno de dichos heterociclos opcionalmente sustituido con uno o dos sustituyentes seleccionados cada uno independientemente de halo, alquilo C1-6, alquil C1-6-oxi, polihalo-alquilo C1-6, polihalo-alquil C1-6-oxi, ciano, aminocarbonilo, mono- o di(alquil C 1-4)-aminocarbonilo, amino, mono- o di(alquil C 1-4)amino o nitro.

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