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1. 发明申请

WO2004071390A3 PIPERAZINE-2-CARBOXAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2004071390A3
公开(公告)日：2004-08-26
申请号：PCT/EP2004/050093
申请日：2004-02-06
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , PAGE, Patrick , JORAND-LEBRUN, Catherine , THOMAS, Russel J. , SCHWARZ, Matthias
发明人： PAGE, Patrick , JORAND-LEBRUN, Catherine , THOMAS, Russel J. , SCHWARZ, Matthias
IPC分类号： A61K31/495
摘要： The present invention is related to piperazine -2-carboxamide derivatives of formula (I) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. Wherein A, X, Y, R 1 and R 2 are as defined in the description.

2. 发明申请

WO2003082278A1 THIAZOLIDINE CARBOXAMIDE DERIVATIVES AS MODULATORS OF THE PROSTAGLANDIN F RECEPTOR 审中-公开
标题翻译：作为PROSTAGLANDIN F受体的调节剂的噻唑烷羧酰胺衍生物
公开(公告)号：WO2003082278A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/050083
申请日：2003-03-27
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , PAGE, Patrick , JORAND-LEBRUN, Catherine , QUATTROPANI, Anna , POMEL, Vincent , SCHWARZ, Matthias , HAMELIN, Estelle , THOMAS, Russell J.
发明人： PAGE, Patrick , JORAND-LEBRUN, Catherine , QUATTROPANI, Anna , POMEL, Vincent , SCHWARZ, Matthias , HAMELIN, Estelle , THOMAS, Russell J.
IPC分类号： A61K31/426
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , C07D277/06 , C07D417/14 , Y02P20/582
摘要： The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. G is selected from the group consisting of C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl, C 1 -C 6 Alkyl cycloalkyl, C 1 -C 6 -alkyl heteroaryl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl or -heterocycloalkyl, said cycloalkyl or aryl or heteroaryl groups may be fused with cycloalkyl or aryl or heteroaryl groups. R 1 is selected from the group consisting of aryl, heteroaryl, C 3 -C 8 -cycloalkyl or - heterocyclo-alkyl, said (hetero)cycloalkyl or aryl or heteroaryl groups may be fused with (hetero)cycloalkyl or aryl or heteroaryl groups. R 2 is selected from the group consisting of H, carboxy, acyl, alkoxycarbonyl, aminocarbonyl, C 1 -C 5 -alkyl carboxy, C 1 -C 5 -alkyl acyl, C 1 -C 5 -alkyl alkoxycarbonyl, C 1 -C 5 -alkyl aminocarbonyl, C 1 -C 5 -alkyl acyloxy, C 1 -C 5 -alkyl acylamino, C 1 -C 5 -alkyl ureido, C 1 -C 5 alkyl amino, C 1 -C 5 -alkyl alkoxy, C 1 -C 5 -alkyl sulfanyl, C 1 -C 5 -alkyl sulfinyl, C 1 -C 5 -alkyl sulfonyl, C 1 -C 5 -alkyl sulfonylamino, C 1 -C 5 -alkyl sulfonyloxy, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl, heterocycloalkyl, C 1 -C 6 -alkyl aryl, C 2 -C 6 -alkyl heteroaryl, C 1 -C 6 -alkyl cycloalkyl, C 1 -C 6 -alkyl heterocycloalkyl, C 2 -C 6 -alkenyl aryl, C 2 -C 6 -alkenyl heteroaryl, C 2 -C 6 -alkynyl aryl, or C 2 -C 6 -alkynyl heteroaryl.
摘要翻译：本发明涉及式（II）的噻唑烷羧酰胺衍生物，其用于治疗和/或预防早产，早产，痛经和用于在剖宫产分娩前停止劳动。 G选自C1-C6-烷基芳基，C1-C6-烷基杂芳基，C1-C6烷基环烷基，C1-C6-烷基杂芳基，芳基，杂芳基，C3-C8-环烷基或 - 杂环烷基，所述环烷基或芳基或杂芳基可与环烷基或芳基或杂芳基稠合。 R 1选自芳基，杂芳基，C 3 -C 8 - 环烷基或 - - 杂环烷基，所述（杂）环烷基或芳基或杂芳基可与（杂）环烷基或芳基或杂芳基稠合。 R 2选自H，羧基，酰基，烷氧基羰基，氨基羰基，C 1 -C 5 - 烷基羧基，C 1 -C 5 - 烷基酰基，C 1 -C 5 - 烷基烷氧基羰基，C 1 -C 5 - 烷基氨基羰基，C 1 C 1 -C 5烷基酰氧基，C 1 -C 5烷基酰氨基，C 1 -C 5烷基脲基，C 1 -C 5烷基氨基，C 1 -C 5烷基烷氧基，C 1 -C 5烷基硫烷基，C 1 -C 5烷基亚磺酰基，烷基磺酰基，C 1 -C 5 - 烷基磺酰基氨基，C 1 -C 5 - 烷基磺酰氧基，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，芳基，杂芳基，C 3 -C 8 - 环烷基，杂环烷基，C 1 -C 6 烷基芳基，C 2 -C 6烷基杂芳基，C 1 -C 6烷基环烷基，C 1 -C 6烷基杂环烷基，C 2 -C 6烯基芳基，C 2 -C 6链烯基杂芳基，C 2 -C 6炔基芳基或C 2 -C 6 - 炔基杂芳基。

3. 发明申请

WO2005026159A1 BENZOXAZOLE ACETONITRILES 审中-公开
标题翻译：苯并噻唑乙酸酯
公开(公告)号：WO2005026159A1
公开(公告)日：2005-03-24
申请号：PCT/EP2004/052141
申请日：2004-09-10
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SCHWARZ, Matthias , GAILLARD, Pascale , PAGE, Patrick , GOTTELAND, Jean-Pierre , THOMAS, Russell, J.
发明人： SCHWARZ, Matthias , GAILLARD, Pascale , PAGE, Patrick , GOTTELAND, Jean-Pierre , THOMAS, Russell, J.
IPC分类号： C07D413/06
CPC分类号： C07D491/10 , C07D413/06 , C07D413/14
摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylarnino moiety.R 1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C i C 6 -alkYl, C 2 -C 6 -alkenYl, C 2 -C 6 -alkynyl or C l -C 6 -alkoxy, aryl, halogen, carboxy,aminocarbonyl, cyano or hydroxy.
摘要翻译：本发明涉及苯并恶唑乙腈和含有该苯并恶唑乙腈的配方（I）的药物制剂。所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高血糖调节的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）。本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基，L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。选自N，O，S或L是酰基氨基部分.R 1选自氢，磺酰基，氨基，C 1 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 烯基，炔基或C 1 -C 6 - 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。

4. 发明申请

WO2006125784A1 TRICYCLIC SPIRO DERIVATIVES AS CRTH2 MODULATORS 审中-公开
标题翻译：作为CRTH2调节剂的TRICYCLIC SPIRO衍生物
公开(公告)号：WO2006125784A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/062545
申请日：2006-05-23
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SCHWARZ, Matthias , SEBILLE, Eric , CLEVA, Christophe , MERLOT, Cedric , CHURCH, Dennis , PAGE, Patrick , MACRITCHIE, Jacqueline A. , ATHERALL, John Frederick , CROSIGNANI, Stefano , PUPOWICZ, Doris
发明人： SCHWARZ, Matthias , SEBILLE, Eric , CLEVA, Christophe , MERLOT, Cedric , CHURCH, Dennis , PAGE, Patrick , MACRITCHIE, Jacqueline A. , ATHERALL, John Frederick , CROSIGNANI, Stefano , PUPOWICZ, Doris
IPC分类号： C07D487/10 , A61K31/407 , A61P29/00 , A61P37/08
CPC分类号： C07D487/10
摘要： The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.
摘要翻译：本发明涉及式（I）的螺衍生物用于治疗和/或预防具有炎性成分的过敏性疾病，炎性皮肤病和其它疾病的用途。具体地说，本发明涉及螺衍生物用于调节CRTH2活性的用途。

5. 发明申请

WO2006111560A2 2,3 SUBSTITUTED PYRAZINE SULFONAMIDES 审中-公开
标题翻译： 2,3取代的吡嗪磺酰胺
公开(公告)号：WO2006111560A2
公开(公告)日：2006-10-26
申请号：PCT/EP2006/061706
申请日：2006-04-20
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , PAGE, Patrick , SCHWARZ, Matthias , SEBILLE, Eric , CLEVA, Christophe , MERLOT, Cedric , MAIO, Maurizio
发明人： PAGE, Patrick , SCHWARZ, Matthias , SEBILLE, Eric , CLEVA, Christophe , MERLOT, Cedric , MAIO, Maurizio
IPC分类号： A61K31/4965 , A61K31/497 , A61P11/06 , C07D401/12
CPC分类号： C07D241/22 , C07D241/20 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.
摘要翻译：本发明涉及式（I）的2,3-取代吡嗪磺酰胺在治疗和/或预防过敏性疾病，炎性皮肤病和其它具有炎性成分的疾病中的应用。具体地说，本发明涉及2,3取代吡嗪磺酰胺用于调节，特别是抑制CRTH2活性的用途。

6. 发明申请

WO2002102799A2 PYRROLIDINE OXADIAZOLE- AND THIADIAZOLE DERIVATIVES 审中-公开
标题翻译：吡咯烷氧基噻唑和噻唑并吡啶衍生物
公开(公告)号：WO2002102799A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006629
申请日：2002-06-14
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SCHWARZ, Matthias , PAGE, Patrick , POMEL, Vincent , QUATTROPANI, Anna , THOMAS, Russell, J.
发明人： SCHWARZ, Matthias , PAGE, Patrick , POMEL, Vincent , QUATTROPANI, Anna , THOMAS, Russell, J.
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. (I) B is a oxadiazole or thiadiazole group.
摘要翻译：本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物，以及含有这种吡咯烷恶二唑衍生物的药物制剂。所述吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法。（I）B是恶二唑或噻二唑基。

7. 发明申请

WO2005026155A1 BENZIMIDAZOLE ACETONITRILES 审中-公开
标题翻译：苯并咪唑乙酸酯
公开(公告)号：WO2005026155A1
公开(公告)日：2005-03-24
申请号：PCT/EP2004/052137
申请日：2004-09-10
申请人： Applied Research Systems ARS Holding N.V. , SCHWARZ, Mattias , GAILLARD, Pascale , PAGE, Patrick , GOTTELAND, Jean-Pierre , THOMAS, Russell J.
发明人： SCHWARZ, Mattias , GAILLARD, Pascale , PAGE, Patrick , GOTTELAND, Jean-Pierre , THOMAS, Russell J.
IPC分类号： C07D403/06
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucosetolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing ben7.oxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatorn selected from N, O, S or L is an acylamino moiety; R 1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C I -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl or C l -C 6 -alkoxy, aryl,halogen, cyano or hydroxy;R 2 is selected from the group comprising or consisting of hydrogen, C I -C 6 -alkyl, C 2 -C 6 alkenyl, C 2 -C 6 -alkynyl, or C I -C 6 -alkoxy.
摘要翻译：本发明涉及苯并咪唑乙腈和含有式（I）的苯并咪唑乙腈的药物制剂。所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合症（PCOS）（I））。本发明还涉及制备ben7.oxazole乙腈的方法。 G是嘧啶基; L是氨基或含有至少一个选自N，O，S或L的杂化子的3-8元杂环烷基是酰氨基部分; R 1选自氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基或C 1 -C 6 - 烷氧基，芳基，卤素氰基或羟基; R 2选自由氢，C 1 -C 6 - 烷基，C 2 -C 6烯基，C 2 -C 6 - 炔基或C 1 -C 6 - 烷氧基组成或组成的组。

8. 发明公开

EP1633363A1 PYRIDINYL ACETONITRILES 有权
标题翻译：吡啶衍生物
公开(公告)号：EP1633363A1
公开(公告)日：2006-03-15
申请号：EP04730871.3
申请日：2004-05-03
申请人： Applied Research Systems ARS Holding N.V.
发明人： SCHWARZ, Matthias , GAILLARD, Pascale Domaine de la Prasle , GOTTELAND, Jean-Pierre , THOMAS, Russell, J. , PAGE, Patrick
IPC分类号： A61K31/505 , A61K31/53 , A61P37/02 , A61P25/16 , C07D401/06
CPC分类号： C07D401/06 , A61K31/505 , A61K31/53
摘要： The present invention is related to pyridinyl acetonitriles as well as to pharmaceutical formulations containing such pyridinyl acetonitriles. Said pyridinyl acetonitriles are modulators of the protein kinase signalling pathways, particularly the one involving Glycogen Kinase Synthase 3 or JNK. The present invention is furthermore related to methods of preparing pyridinyl acetonitriles. X is a substituted or unsubstituted pyridinyl. G is an unsubstituted or substituted pyrimidinyl or triazinyl.

9. 发明公开

EP1668004A1 BENZOXAZOLE ACETONITRILES 审中-公开
标题翻译：苯并恶唑乙腈
公开(公告)号：EP1668004A1
公开(公告)日：2006-06-14
申请号：EP04766769.6
申请日：2004-09-10
申请人： Applied Research Systems ARS Holding N.V.
发明人： SCHWARZ, Matthias , GAILLARD, Pascale , PAGE, Patrick , GOTTELAND, Jean-Pierre , THOMAS, Russel, J.
IPC分类号： C07D413/06 , C07D413/14 , A61K31/423 , A61P3/10
CPC分类号： C07D491/10 , C07D413/06 , C07D413/14
摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylarnino moiety.R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, CiC6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or Cl-C6-alkoxy, aryl, halogen, carboxy,aminocarbonyl, cyano or hydroxy.
摘要翻译：本发明涉及苯并恶唑乙腈以及含有这样的式（I）的苯并恶唑乙腈的药物制剂。所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高甘油三酯介导的代谢疾病，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖症，多囊卵巢综合征（PCOS）。本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基.L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。选自N，O，S或L的化合物是酰基氨基部分。R 1选自包括氢，磺酰基，氨基，C 1 -C 6 - 烷基，C 2 -C 6 - 链烯基，C 2 -C 6炔基或C 1 -C 6 - 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。

10. 发明公开

EP1667995A1 BENZIMIDAZOLE ACETONITRILES 审中-公开
标题翻译：苯并咪唑ACETONITRILES
公开(公告)号：EP1667995A1
公开(公告)日：2006-06-14
申请号：EP04766767.0
申请日：2004-09-10
申请人： Applied Research Systems ARS Holding N.V.
发明人： SCHWARZ, Mattias , GAILLARD, Pascale , PAGE, Patrick , GOTTELAND, Jean-Pierre , THOMAS, Russel J.
IPC分类号： C07D403/06 , C07D403/14 , C07D401/14
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucosetolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing ben7.oxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatorn selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, CI-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or Cl-C6-alkoxy, aryl,halogen, cyano or hydroxy;R2 is selected from the group comprising or consisting of hydrogen, CI -C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or CI -C6-alkoxy.
摘要翻译：本发明涉及苯并咪唑乙腈以及含有这种式（I）的苯并咪唑乙腈的药物制剂。所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢疾病，包括II型糖尿病，不充分的葡萄糖耐受性，胰岛素抵抗，肥胖症，多囊卵巢综合征（PCOS）（I）。本发明还涉及制备苯并恶唑乙腈的方法。 G是嘧啶基; L为含有至少一个选自N，O，S或L的杂芳基的氨基或3-8元杂环烷基，为酰氨基部分; R 1选自包括氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或C 1 -C 6烷氧基，芳基，卤素，氰基或羟基; R 2选自包括氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或C 1 -C 6烷氧基或由其组成的组。

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