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1. 发明申请

WO2005040210A2 NOVEL CXCL8 ANTAGONISTS 审中-公开
标题翻译：新的CXCL8 ANTAGONISTS
公开(公告)号：WO2005040210A2
公开(公告)日：2005-05-06
申请号：PCT/EP2004/052637
申请日：2004-10-22
申请人： Applied Research Systems ARS Holding N.V. , PROUDFOOT, Amanda , SHAW, Jeffrey
发明人： PROUDFOOT, Amanda , SHAW, Jeffrey
IPC分类号： C07K14/54
CPC分类号： C07K14/5421 , A61K38/00
摘要： Novel antagonists of the chemokine CXCL8 (also known as Interleukin-8) can be obtained by generating mutants having specific combinations of non-.conservative substitutions of basic amino acids located in the C-terminal region. Compounds prepared in accordance with the present invention can be used to block CXCL8 activity in vivo , thereby providing therapeutic compositions for use in the treatment or prevention of CXCL-8-related diseases.
摘要翻译：趋化因子CXCL8（也称为白细胞介素-8）的新型拮抗剂可以通过产生具有位于C末端区域中的碱性氨基酸的非保守取代的特异性组合的突变体获得。根据本发明制备的化合物可用于在体内阻断CXCL8活性，从而提供用于治疗或预防CXCL-8相关疾病的治疗组合物。

2. 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。

3. 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;

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