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1. 发明申请

WO2004005249A1 PYRROLIDINE DERIVATIVES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：吡咯烷衍生物作为氧化物拮抗剂
公开(公告)号：WO2004005249A1
公开(公告)日：2004-01-15
申请号：PCT/EP2003/050286
申请日：2003-07-04
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , JORAND-LEBRUN, Catherine , DORBAIS, Jérôme , QUATTROPANI, Anna , SCHWARZ, Matthias , VALOGNES, Delphine
发明人： JORAND-LEBRUN, Catherine , DORBAIS, Jérôme , QUATTROPANI, Anna , SCHWARZ, Matthias , VALOGNES, Delphine
IPC分类号： C07D207/22
CPC分类号： C07D231/12 , C07D207/22 , C07D233/56 , C07D249/08 , C07D403/06
摘要： The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R 1 is selected from the group comprising or consisting of H and C 1 -C 6 -alkyl, for the prevention and/or treatment of preterm labor, premature birth or dysmenorrhea.
摘要翻译：本发明涉及式（I）的新型吡咯烷衍生物，其几何异构体，其作为对映异构体的光学活性形式，非对映异构体，这些及其外消旋体形式的混合物，以及其盐，其中R 1选自由H和C 1 -C 6烷基组成或组成的组，用于预防和/或治疗早产，早产或痛经。

2. 发明申请

WO2004076407A2 PYRROLIDINE DERIVATIVES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为氧化物拮抗剂
公开(公告)号：WO2004076407A2
公开(公告)日：2004-09-10
申请号：PCT/EP2004/050142
申请日：2004-02-16
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SCHWARZ, Matthias , JORAND-LEBRUN, Catherine , VALOGNES, Delphine
发明人： SCHWARZ, Matthias , JORAND-LEBRUN, Catherine , VALOGNES, Delphine
IPC分类号： C07D
CPC分类号： C07D413/06 , C07D207/22
摘要： The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate forms, as well as salts thereof, wherein: R 1i s selected from the group comprising or consisting of H and C 1 -C 6 -alkyl; R 2 is selected from the group comprising or consisting of hydrogen, C I -C 6 -alkyl, C I -C 6 alkyl aryl, heteroaryl, C I -C 6 alkyl heteroaryl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyl aryl, C 2 -C 6 alkenyl heteroaryl, C 2 -C 6 -alkynyl, C 2 -C 6 -alkynyl aryl, C 2 C 6 -alkynyl heteroaryl, C 3 -C 8 cycloalkyl, heterocycloalkyl, CI-C6-alkyl cycloallcyl, CI-C6-alkyI heterocycloalkyl, CIC6 alkyl carboxy, acyl, C I -C 6 -alkyl acyl, C I -C 6 -alkyl acyloxy, C I -C 6 -alkyl alkoxy, alkoxycarbonyl, C I -C 6 -alkyI alkoxycarbonyl, aminocarbonyl, C I -C 6 -alkyl aminocarbonyl, C I -C 6 -alkyl acylarnino, C I -C 6 -alkyl ureido, amino, C I -C 6 alkyl amino, sulfonyloxy, C I -C 6 alkyl sulfonyloxy, sulfonyl, C I -C 6 -alkyl sulfonyl, sulfinyl, C I -C 6 -alkyl sulfinyl, C I -C 6 alkyl sulfanyl, C I -C 6 -alkyl sulfonylamino;
摘要翻译：本发明涉及式（I）的新型吡咯烷衍生物，其几何异构体，其作为对映体的光学活性形式，diastercomers，它们的混合物及其外消旋体形式，以及其盐，其中：R 1选自由H和C 1 -C 6烷基组成或由其组成的基团; R 2选自氢，C 1 -C 6 - 烷基，C 1 -C 6烷基芳基，杂芳基，C 1 -C 6烷基杂芳基，C 2 -C 6 - 烯基，C 2 -C 6 - 链烯基芳基， C 1 -C 6烷基杂芳基，C 2 -C 6炔基，C 2 -C 6炔基芳基，C 2 -C 6炔基杂芳基，C 3 -C 8环烷基，杂环烷基， C 1-6烷基酰氧基，C 1 -C 6烷基烷氧基，烷氧基羰基，C 1 -C 6烷基烷氧基羰基，氨基羰基，C 1 -C 6烷基氨基羰基，C 1 -C 6烷基酰基氨基，C 1 -C 6烷基脲基，氨基，C1-C6烷基氨基，磺酰氧基，C1-C6烷基磺酰氧基，磺酰基，C1-C6烷基磺酰基，亚磺酰基，C1-C6烷基亚磺酰基，C1-C6烷基硫烷基，C1-C6烷基磺酰基氨基;

3. 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。

4. 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.

5. 发明申请

WO2005068444A2 THIAZOLE DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：噻唑衍生物及其用途
公开(公告)号：WO2005068444A2
公开(公告)日：2005-07-28
申请号：PCT/EP2005/050102
申请日：2005-01-11
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , QUATTROPANI, Anna , RUECKLE, Thomas , SCHWARZ, Matthias , DORBAIS, Jerôme , SAUER, Wolfgang , CLEVA, Christophe , DESFORGES, Gwénaëlle
发明人： QUATTROPANI, Anna , RUECKLE, Thomas , SCHWARZ, Matthias , DORBAIS, Jerôme , SAUER, Wolfgang , CLEVA, Christophe , DESFORGES, Gwénaëlle
IPC分类号： C07D277/46
CPC分类号： C07D417/04 , C07D277/46 , C07D417/14
摘要： The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
摘要翻译：本发明涉及式（I）的噻唑衍生物，特别是用于治疗和/或预防自身免疫性疾病和/或炎性疾病，心血管疾病，神经退行性疾病，细菌或病毒感染，肾脏疾病，血小板聚集，癌症，移植，移植排斥或肺损伤。

6. 发明申请

WO2003053437A1 TRIAZOLES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：三唑作为氧化物拮抗剂
公开(公告)号：WO2003053437A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/014594
申请日：2002-12-19
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , QUATTROPANI, Anna , SCHWARZ, Matthias , THOMAS, Russell, J. , COULTER, Thomas
发明人： QUATTROPANI, Anna , SCHWARZ, Matthias , THOMAS, Russell, J. , COULTER, Thomas
IPC分类号： A61K31/4196
CPC分类号： C07D403/12 , C07D249/10 , C07D249/12 , C07D249/14 , C07D405/06 , C07D405/12
摘要： The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole deriva-tives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.
摘要翻译：本发明涉及特别用作药物活性化合物的式（I）的三唑衍生物以及含有这种三唑衍生物的药物制剂。所述三唑可用于治疗和/或预防早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。特别地，本发明涉及显示催产素和/或加压素受体的显着调节，特别是拮抗活性的三唑衍生物。更优选地，所述化合物可用于治疗和/或预防催产素和/或加压素介导的疾病状态。本发明还涉及新的三唑衍生物及其制备方法。

7. 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。

8. 发明申请

WO2002074741A1 PYRROLIDINE ESTER DERIVATIVES WITH OXYTOCIN MODULATING ACITVITY 审中-公开
标题翻译：具有氧化调节作用的吡咯烷酮衍生物
公开(公告)号：WO2002074741A1
公开(公告)日：2002-09-26
申请号：PCT/EP2002/003005
申请日：2002-03-19
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING NV , SCHWARZ, Matthias , QUATTROPANI, Anna , SCHEER, Alexander , DORBAIS, Jérôme , POMEL, Vincent
发明人： SCHWARZ, Matthias , QUATTROPANI, Anna , SCHEER, Alexander , DORBAIS, Jérôme , POMEL, Vincent
IPC分类号： C07D207/20
CPC分类号： C07D401/10 , A61K31/401 , C07D207/22 , C07D403/10
摘要： The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonise the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR 6 R 7 , NOR 6 , NNR 6 R 7 ;R is selected from the group comprising or consisting of C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, saturated or unsaturated 3-8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl. R 1 is selected from the group comprising or consisting of C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, aryl, heteroaryl, 3-8-membered cycloalkyl, acyl, C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1-2 further cycloalkyl or aryl or heteroaryl group.
摘要翻译：本发明涉及式（I）的吡咯烷酯用于治疗和/或预防早产，早产和痛经的用途。特别地，本发明涉及式（I）的吡咯烷酯的用途，特别是拮抗催产素受体。本发明还涉及新的吡咯烷酯。 X选自CR 6 R 7，NOR 6，NNR 6 R 7; R选自C 1 -C 6烷基，C 2 -C 6烯基 C 2 -C 6炔基，饱和或不饱和的3-8元环烷基，其可以含有1-3个选自N，O，S，芳基，杂芳基，C 1 -C 6烷基芳基，C 1 -C 6烷基杂芳基的杂原子。 R 1选自由C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，芳基，杂芳基，3-8元环烷基，酰基，C 1 -C 6 - 烷基芳基，C 1 -C 6烷基杂芳基，所述环烷基或芳基或杂芳基可与1-2个其它环烷基或芳基或杂芳基稠合。

9. 发明申请

WO2007065940A1 ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES 审中-公开
标题翻译：抗生素PYRIMIDYL，FUSED PYRIMIDYL和PYRIMIDYL HYDRAZONES
公开(公告)号：WO2007065940A1
公开(公告)日：2007-06-14
申请号：PCT/EP2006/069460
申请日：2006-12-08
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , HEALEY, Brian , ZHAO, Zhong , SUTTON, Amanda , SCHWARZ, Matthias
发明人： HEALEY, Brian , ZHAO, Zhong , SUTTON, Amanda , SCHWARZ, Matthias
IPC分类号： C07D239/94 , C07D239/42 , C07D239/46 , C07D239/48 , C07D413/04 , C07D401/04 , A61K31/505 , A61K31/506 , A61P35/00
CPC分类号： C07D239/94 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D413/04
摘要： The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.
摘要翻译：本发明涉及一系列新的嘧啶基或稠合嘧啶基腙系列。其中A选自式（A1），（A2），（A3），（A4），（A5）的式（I）化合物可用于治疗和/或预防增殖性疾病。

10. 发明申请

WO2006056427A1 NOVEL 4-ARYLAMINO PYRIDONE DERIVATIVES AS MEK INHIBITORS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS 审中-公开
标题翻译：新型4-亚氨基吡啶酮衍生物作为治疗高脂血症的MEK抑制剂
公开(公告)号：WO2006056427A1
公开(公告)日：2006-06-01
申请号：PCT/EP2005/012546
申请日：2005-11-23
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , ABEL, Ulrich , DEPPE, Holger , FEURER, Achim , GRÄDLER, Ulrich , GOUTOPOULOS, Andreas , SCHWARZ, Matthias
发明人： ABEL, Ulrich , DEPPE, Holger , FEURER, Achim , GRÄDLER, Ulrich , GOUTOPOULOS, Andreas , SCHWARZ, Matthias
IPC分类号： C07D213/82 , C07D413/04 , A61K31/4412 , A61K31/4439 , A61P35/00 , C07D213/80
CPC分类号： C07D213/78 , C07D213/80 , C07D213/82 , C07D413/04
摘要： The invention provides novel, substituted 4-arylamino pyridone compounds (formula (I)), pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R 1, R2, R9, R 10, R 11, R 12, R 13, R 14 and L are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
摘要翻译：本发明提供新的取代的4-芳基氨基吡啶酮化合物（式（I）），其药学上可接受的盐，溶剂合物和前药化合物，其中W，R 1，R 2，R 9，R 10，R 11，R 12，R 13， R 14和L如说明书中所定义。这些化合物是MEK抑制剂，可用于治疗过度增殖性疾病，如癌症，再狭窄和炎症。还公开了这样的化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗和含有这些化合物的药物组合物中的应用。

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