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1. 发明申请

WO2011107608A8 HETEROCYCLIC AMIDES AS ROCK INHIBITORS 审中-公开
标题翻译：杂环化合物作为岩石抑制剂
公开(公告)号：WO2011107608A8
公开(公告)日：2012-05-03
申请号：PCT/EP2011053343
申请日：2011-03-04
申请人： AMAKEM NV , LEYSEN DIRK , DEFERT OLIVIER , KAVAL NADZEYA , BLOM PETRA , BOLAND SANDRO
发明人： LEYSEN DIRK , DEFERT OLIVIER , KAVAL NADZEYA , BLOM PETRA , BOLAND SANDRO
IPC分类号： C07D213/75 , A61K31/437 , A61K31/4409 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/505 , A61P1/00 , A61P9/00 , C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D493/04
CPC分类号： C07D213/75 , C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D493/04
摘要： The present invention relates to new kinase inhibitors of formula (I), more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
摘要翻译：本发明涉及式（I）的新的激酶抑制剂，更具体地涉及包含这种抑制剂的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病和呼吸系统疾病）的药物中的方法。

2. 发明申请

WO2012146724A3 NOVEL ROCK INHIBITORS 审中-公开
标题翻译：新型岩石抑制剂
公开(公告)号：WO2012146724A3
公开(公告)日：2013-01-17
申请号：PCT/EP2012057785
申请日：2012-04-27
申请人： AMAKEM NV , LEYSEN DIRK , DEFERT OLIVIER , BOLAND SANDRO , ALEN JO , BOURIN ARNAUD PIERRE JEAN
发明人： LEYSEN DIRK , DEFERT OLIVIER , BOLAND SANDRO , ALEN JO , BOURIN ARNAUD PIERRE JEAN
IPC分类号： C07D401/12 , A61K31/439 , A61K31/4468 , A61K31/4725 , A61P9/00 , A61P11/00 , A61P15/00 , A61P25/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D451/04
CPC分类号： C07D409/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D451/04
摘要： The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, -NH-, or a direct bond; Y is -NH- or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of:Formula (II), Ar is selected from the group comprising: Formula (III), R2 is hydrogen or methyl; R8 is hydrogen, methyl, halogen, or alkynyl; R1 is an aryl or heteroaryl more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
摘要翻译：本发明涉及式（I）的新的激酶抑制剂，其中X是氧，-NH-或直接键; Y是-NH-或直接键; n为0〜4的整数; m为0〜4的整数; Cy表示由包括稠合，双，螺或桥连的碳环和杂环的一个（多）周期组成的二价基团; 特别是选自由式（II）组成的组，Ar选自：式（III），R 2是氢或甲基; R8是氢，甲基，卤素或炔基; R1是芳基或杂芳基更具体地是ROCK抑制剂，组合物，特别是药物，包含这种抑制剂，以及这些抑制剂在治疗和预防疾病中的用途。特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病和呼吸系统疾病）的药物中的方法。

3. 发明申请

WO2005028442A3 2-PYRIDINONE DERIVATIVES, HAVING HIV INHIBITING PROPERTIES 审中-公开
标题翻译：具有HIV抑制特性的2-吡啶酮衍生物
公开(公告)号：WO2005028442A3
公开(公告)日：2005-09-09
申请号：PCT/BE2004000134
申请日：2004-09-22
申请人： UNIV NOTRE DAME DE LA PAIX , UNIV BRUXELLES , LE VAN KIET , GEORGES BENOIT , HEVESI LASZLO , CAUVIN CHRISTINE , BOLAND SANDRO , DURANT FRANCOIS , DEMONTE DOMINIQUE , VAN LINT CARINE , BURNY ARSENE , BOLLEN ALEX , JACQUET ALAIN , DE WALQUE STEPHANE
发明人： LE VAN KIET , GEORGES BENOIT , HEVESI LASZLO , CAUVIN CHRISTINE , BOLAND SANDRO , DURANT FRANCOIS , DEMONTE DOMINIQUE , VAN LINT CARINE , BURNY ARSENE , BOLLEN ALEX , JACQUET ALAIN , DE WALQUE STEPHANE
IPC分类号： A61P31/18 , C07D213/69 , C07D213/80 , A61K31/4412
CPC分类号： C07D213/69 , C07D213/80
摘要： The present invention relates to 2-Pyridinone derivatives, more specifically 5-ethyl-6-methyl-2-pyridinone derivatives, according to general formula I that inhibit human immunodeficiency virus type 1 (HIV-1) replication and are therefore of interest in the treatment of Acquired Immune Deficiency Syndrome (AIDS). The present invention further relates to the synthesis of said compounds and their use, with or without other pharmaceutical agents, in the treatment of AIDS and viral infections by HIV-1.
摘要翻译：本发明涉及抑制人免疫缺陷病毒1型（HIV-1）复制物的通式I的2-吡啶酮衍生物，更具体地说是5-乙基-6-甲基-2-吡啶酮衍生物，因此在治疗获得性免疫缺陷综合征（AIDS）。本发明还涉及所述化合物的合成及其用于或不用其它药剂用于治疗HIV-1的AIDS和病毒感染的用途。

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