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11. 发明申请

WO2007042321A2 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2007042321A2
公开(公告)日：2007-04-19
申请号：PCT/EP2006/009923
申请日：2006-10-13
申请人： DEVGEN N.V. , VAN ROMPAEY, Philippe , ARZEL, Philippe , DEFERT, Olivier , LEYSEN, Dirk
发明人： VAN ROMPAEY, Philippe , ARZEL, Philippe , DEFERT, Olivier , LEYSEN, Dirk
IPC分类号： C07D213/40 , C07D401/12 , C07D407/12 , C07D409/12 , C07D471/04 , A61P11/06 , A61K31/4409
CPC分类号： C07D213/40 , C07D401/12 , C07D407/12 , C07D409/12 , C07D471/04
摘要： The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I, II, or III or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, I II III wherein X, R 1 , R 2 , R 3 , R 31 , n, and m have the meaning defined in the claims. In particular, the present invention relates more specifically to ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
摘要翻译：本发明涉及新的AGC激酶抑制剂，特别是涉及式I，II或III的化合物或其立体异构体，互变异构体，外消旋，代谢物，前体或前药，盐，水合物或溶剂合物，其中X R 1，R 2，R 3，R 31，n和m具有如下定义的含义：索赔。特别地，本发明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。

12. 发明申请

WO2008049919A2 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2008049919A2
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061542
申请日：2007-10-26
申请人： DEVGEN N.V. , DEFERT, Olivier , LEYSEN, Dirk , VAN ROMPAEY, Philippe
发明人： DEFERT, Olivier , LEYSEN, Dirk , VAN ROMPAEY, Philippe
IPC分类号： C07D217/02 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D217/02 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/08
摘要： The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein R 1 , R 2 , R 4 , R 5 , R 7 , R 8 , q s, L, and Y have the meaning defined in the claims. In particular, the present invention relates to ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
摘要翻译：本发明涉及新的AGC激酶抑制剂，特别是涉及式（I）或（II）的化合物或其立体异构体，互变异构体，外消旋，代谢物，前体或前药，盐，水合物或溶剂化物，其中R < R 1，R 2，R 4，R 5，R 7，R SUP， qS，L和Y具有权利要求中限定的含义。特别地，本发明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。

13. 发明申请

WO2007006547A1 AMIDE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：酰胺衍生物作为激酶抑制剂
公开(公告)号：WO2007006547A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/006765
申请日：2006-07-11
申请人： DEVGEN N.V. , DEFERT, Olivier , VAN ROMPAEY, Philippe , BLOM, Petra , LEYSEN, Dirk , DE WILDE, Gert , BROWN, Thomas
发明人： DEFERT, Olivier , VAN ROMPAEY, Philippe , BLOM, Petra , LEYSEN, Dirk , DE WILDE, Gert , BROWN, Thomas
IPC分类号： C07D213/75 , C07D401/12 , C07D407/12 , A61K31/4409 , A61K31/437 , A61P9/00 , A61P15/00 , A61P11/00 , A61P25/00 , A61P19/00 , A61P35/00 , C07D413/14 , C07D413/12 , C07D471/04 , C07D411/12
CPC分类号： C07D409/14 , C07D213/75 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar 1 , Ar 2 , R 1 , R 3 , p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
摘要翻译：本发明涉及新的AGC激酶抑制剂，特别是涉及式（I）或（II）的化合物或其立体异构体，互变异构体，外消旋，代谢物，前体或前药，盐，水合物或溶剂化物，其中Ar < > 1 ，2 ，R 1，R 3，p和n具有权利要求中限定的含义。特别地，本发明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。

14. 发明申请

WO2006058905A1 5-CARBOXAMIDO SUBSTITUTED THIAZOLE DERIVATIVES THAT INTERACT WITH ION CHANNELS, IN PARTICULAR WITH ION CHANNELS FROM THE Kv FAMILY 审中-公开
标题翻译： 5-CARBOXAMIDO取代与离子通道相互作用的噻唑衍生物，特别是来自Kv家族的离子通道
公开(公告)号：WO2006058905A1
公开(公告)日：2006-06-08
申请号：PCT/EP2005/056390
申请日：2005-12-01
申请人： DEVGEN NV , BLOM, Petra , DE KERPEL, Jan, Octaaf , FOURMAINTRAUX, Eric, Pierre, Paul, René , KALETTA, Titus, Jan , LEYSEN, Dirk
发明人： BLOM, Petra , DE KERPEL, Jan, Octaaf , FOURMAINTRAUX, Eric, Pierre, Paul, René , KALETTA, Titus, Jan , LEYSEN, Dirk
IPC分类号： A61K31/426 , A61P9/00 , C07D277/56 , C07D263/48 , C07D233/54 , C07D233/90
CPC分类号： C07D239/42 , C07D233/90 , C07D263/48 , C07D271/07 , C07D277/56 , C07D333/38 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula (I), (II), (III) or (IV), stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y 1 , Y 2 , R 1 , n, R 3 , R 8 , R 9 , R 10 , L 1 , L 2 , Ar 1 and Ar 2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.
摘要翻译：本发明涉及与离子通道相互作用的化合物。特别地，本发明涉及具有结构式（I），（II），（III）或（IV）的结构式的化合物，立体异构体，互变异构体，外消旋学，前药，其代谢物或其药学上可接受的盐和/ 或其溶剂合物，其中X，Y 1，Y 2，R 1，n，R 3，R R 9，R 9，R 10，L 1，L 2，Ar 2，本发明还涉及制备所述化合物的方法，包含所述化合物的药物组合物以及所述化合物在所述化合物中的用途。治疗人体和动物体的方法。

15. 发明申请

WO2014068035A1 NOVEL ROCK INHIBITORS 审中-公开
标题翻译：新型岩石抑制剂
公开(公告)号：WO2014068035A1
公开(公告)日：2014-05-08
申请号：PCT/EP2013/072774
申请日：2013-10-31
申请人： AMAKEM NV
发明人： BOURIN, Arnaud, Pierre, Jean , LEYSEN, Dirk , DEFERT, Olivier , BOLAND, Sandro
IPC分类号： C07D405/14 , C07D401/12 , A61K31/4725 , A61K31/454
CPC分类号： C07D405/14 , C07D217/04 , C07D401/12 , C07D405/12
摘要： The present invention relates to new kinase inhibitors, 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. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors.
摘要翻译：本发明涉及新的激酶抑制剂，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。本发明的化合物显示软的药物特征，即它们在进入体循环时迅速失活。因此，它们允许减少全身暴露于功能活性的ROCK抑制剂。

16. 发明申请

WO2006134167A1 STEROIDS HAVING A MIXED ANDROGENIC AND PROGESTAGENIC PROFILE 审中-公开
标题翻译：具有混合原始和原始性状的STEROIDS
公开(公告)号：WO2006134167A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/063282
申请日：2006-06-16
申请人： N.V. ORGANON , VAN DER LOUW, Jaap , LEYSEN, Dirk , DE GOOIJER, Marcel Evert , CALS, Joseph Maria, Gerardus Barbara
发明人： VAN DER LOUW, Jaap , LEYSEN, Dirk , DE GOOIJER, Marcel Evert , CALS, Joseph Maria, Gerardus Barbara
IPC分类号： C07J63/00 , A61K31/565 , A61P5/26
CPC分类号： C07J63/008
摘要： The invention provides for compounds having formula (1) wherein, R 1 is O, (H,H), (H,OH), or NOR, with R being hydrogen, (C 1-6 ) alkyl or (C 1-6 ) acyl; R 2 is hydrogen, methyl, ethyl, or ethenyl; R 3 is hydrogen, methyl, ethyl, ethenyl, fluoro, or chloro; R 4 is methyl, or ethyl; R 5 is hydrogen, methyl, or ethyl; R 6 is hydrogen, methyl, ethyl, (C 1-3 ) alkenyl, or (C 1-3 ) alkynyl; R 7 is hydrogen or (C 1-15 ) acyl; and at least one of R 5 or R 6 is hydrogen; or a pharmaceutically acceptable salt thereof, for use as medicine for a treatment to increase androgen levels, for androgen supplementation, for testosterone replacement and for benign prostate hypertrophy and in a method of male contraception, preferably as sole means to achieve both progestagenic sterilitant effect and androgen supplementation.
摘要翻译：本发明提供具有式（1）的化合物，其中R 1是O，（H，H），（H，OH）或NOR，其中R是氢，（C 1 -6 N）烷基或（C 1-6 - ）酰基; R 2是氢，甲基，乙基或乙烯基; R 3是氢，甲基，乙基，乙烯基，氟或氯; R 4是甲基或乙基; R 5是氢，甲基或乙基; R 6是氢，甲基，乙基，（C 1-3-3）烯基或（C 1-3-3）炔基; R 7是氢或（C 1-15）酰基; 并且R 5或R 6中的至少一个为氢; 用作治疗用于增加雄激素水平，用于雄激素补充，用于睾酮替代和良性前列腺肥大的药物的药物，以及用于男性避孕的方法中，优选作为实现孕激素相关性效应的唯一手段雄激素补充。

17. 发明授权

EP2542528B1 HETEROCYCLIC AMIDES AS ROCK INHIBITORS 有权转让
标题翻译：杂环酰胺作为岩石抑制剂
公开(公告)号：EP2542528B1
公开(公告)日：2013-06-19
申请号：EP11712789.4
申请日：2011-03-04
申请人： Amakem NV
发明人： LEYSEN, Dirk , DEFERT, Olivier , KAVAL, Nadzeya , BLOM, Petra , BOLAND, Sandro
IPC分类号： C07D213/75 , C07D239/42 , C07D471/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D493/04 , A61K31/437 , A61K31/4409 , A61K31/4433 , A61K31/443 , A61K31/4436 , A61K31/505 , A61P1/00 , A61P9/00
CPC分类号： C07D213/75 , C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D493/04

18. 发明申请

WO2003022864A1 17ALPHA-HYDROXY-14BETA-STEROIDS WITH HORMONAL EFFECT 审中-公开
公开(公告)号：WO2003022864A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/010041
申请日：2002-09-06
申请人： AKZO NOBEL N.V. , VAN DER LOUW, Jaap , LEYSEN, Dirk , DE GOOIJER, Marcel, Evert
发明人： VAN DER LOUW, Jaap , LEYSEN, Dirk , DE GOOIJER, Marcel, Evert
IPC分类号： C07J1/00
CPC分类号： C07J1/0062
摘要： This invention relates to steroidal compounds having the formula (I), wherein: R 1 is O, (H,H), (H,OH), NOH, whereby OH is optionally etherified or esterified; R 2 and R 3 are independently hydrogen or (C 1-4 ) alkyl and at least one of R 2 and R 3 is (C 1-4 ) alkyl; R 4 is hydrogen, or (C 1-15 ) acyl for use in androgen-related treatments, such as androgen insufficiency and male or female contraception.
摘要翻译：本发明涉及具有式（I）的甾体化合物，其中：R 1是O，（H，H），（H，OH），NOH，由此OH任选被醚化或酯化; R 2和R 3独立地是氢或（C 1-4）烷基，R 2和R 3中的至少一个是（C 1-4）烷基; R 4是氢或用于雄激素相关治疗的（C1-15）酰基，例如雄激素不足和雄性或雌性避孕。

19. 发明申请

WO2004069829A1 (2S)-2-((PYRIMIDIN-4-YL)AMINO)-4-METHYLPENTANOIC ACID AMINOETHYLAMID DERIVATIVES AS IL-8 RECEPTOR MODULATORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND RHEUMATOID ARTHRITIS 审中-公开
标题翻译：（2S）-2 - （（吡咯烷-4-基）氨基）-4-甲基戊酸氨基氨基甲酸酯衍生物作为治疗角质层坏死和炎症性角膜炎的IL-8受体调节剂
公开(公告)号：WO2004069829A1
公开(公告)日：2004-08-19
申请号：PCT/US2004/000437
申请日：2004-01-09
申请人： PHARMACOPEIA DRUG DISCOVERY, INC. , CONTI, Paolo, Giovanni, Martino , LEYSEN, Dirk , LOUNNAS, Valere, X., H. , OHLMEYER, Michael, H., J. , BOHNSTEDT, Adolph, C. , HO, Koc-Kan , KULTGEN, Steven, G. , ROUGHTON, Andrew, Laird , AULD, Douglas, S.
发明人： CONTI, Paolo, Giovanni, Martino , LEYSEN, Dirk , LOUNNAS, Valere, X., H. , OHLMEYER, Michael, H., J. , BOHNSTEDT, Adolph, C. , HO, Koc-Kan , KULTGEN, Steven, G. , ROUGHTON, Andrew, Laird , AULD, Douglas, S.
IPC分类号： C07D403/04
CPC分类号： C07D405/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/12 , C07D417/14 , C07D491/04
摘要： The invention relates to compounds of the formula: (I); wherein R1 is a basic moiety having the structure -NH(CH 2 ) 2 NR5R6, (Formula II) or (Formula II); wherein R5, R6 and R7 are independently selected from H, (1-6C)alkyl, (2-6C)alkenyl; (3-8C)cycloalkyl, and (1-6C)alkyl substituted with furanyl, (1-6C)alkoxy, (3-8C)cycloalkyl, trifluoromethyl or amido; or R5 and R6 together with N to which they are attached are a (4-8) membered heterocycle, which heterocycle may be substituted with (1-6C)alkoxy, trifluoromethyl or amido and which heterocycle may be fused with another (5-6) membered heterocycle; n is 1, 2 or 3; and the ring structure A represents a (4-6) membered heterocycle; R2 is (1-6C)alkyl, optionally substituted with (1-6C)alkoxy; R3 is aryl, heterocyclyl, -X-(CH 2 ) m aryl or -X-(CH 2 ) m -heterocyclyl, wherein X is O, S or NR8, R8 being H or (1-6C)alkyl, and m is 0, 1, 2 or 3; and R4 is H, (1-8C)akyl, (1-8C)alkoxy or (2-8C)alkenyl, the alkyl moiety of each optionally being substituted with hydroxy, halogen, cyano, nitro, oxo, amino, alkylamino, dialkylamino, amido, alkylamido, carboxy, (1-8C)alkoxy, (1-8C)alkylthio, perfluoro (1-4C)alkyl, (3-8C)cycloalky, aryl, aryloxy, heterocyclyl or-0-heterocyclyl; or a pharmaceutically acceptable salt thereof. The compounds of the invention are Il-8 receptor modulators, in particular inhibitors thereof, and can be used for treating or preventing Il-8 receptor mediated disorders, such as atherosclerosis, inflammation, rheumatoid arthritis and related disorders.
摘要翻译：本发明涉及下式的化合物：（I）; 其中R1是具有结构-NH（CH 2）2 NR 5 R 6，（式II）或（式II）的碱性部分; 其中R5，R6和R7独立地选自H，（1-6C）烷基，（2-6C）烯基; （3-8C）环烷基和被呋喃基，（1-6C）烷氧基，（3-8C）环烷基，三氟甲基或酰氨基取代的（1-6C）烷基; 或R 5和R 6与它们所连接的N一起为（4-8）元杂环，该杂环可以被（1-6C）烷氧基，三氟甲基或酰氨基取代，并且该杂环可以与另一个（5-6 ）元杂环 n为1,2或3; 环结构A表示（4-6）元杂环; R2是（1-6C）烷基，任选地被（1-6C）烷氧基取代; R3是芳基，杂环基，-X-（CH2）马来酰基或-X-（CH2）m-杂环基，其中X是O，S或NR8，R8是H或（1-6C）烷基，m是0,1 ，2或3; 并且R 4是H，（1-8C）烷基，（1-8C）烷氧基或（2-8C）烯基，其烷基部分任选被羟基，卤素，氰基，硝基，氧代，氨基，烷基氨基，二烷基氨基，（1-8C）烷氧基，（1-8C）烷硫基，全氟（1-4C）烷基，（3-8C）环烷基，芳基，芳氧基，杂环基或-O-杂环基; 或其药学上可接受的盐。本发明的化合物是II-8受体调节剂，特别是其抑制剂，并且可用于治疗或预防II-8受体介导的病症，例如动脉粥样硬化，炎症，类风湿性关节炎和相关疾病。

20. 发明申请

WO2003101374A3 USE OF NEW ETONOGESTREL ESTERS 审中-公开
公开(公告)号：WO2003101374A3
公开(公告)日：2003-12-11
申请号：PCT/EP2003/050188
申请日：2003-05-22
申请人： AKZO NOBEL N.V. , DE NIJS, Henrik , VAN DER VOORT, Hendrikus Adrianus Antonius , LEYSEN, Dirk , GROOTENHUIS, Arij Jan , VAN DER LOUW, Jaap
发明人： DE NIJS, Henrik , VAN DER VOORT, Hendrikus Adrianus Antonius , LEYSEN, Dirk , GROOTENHUIS, Arij Jan , VAN DER LOUW, Jaap
IPC分类号： A61P15/00
摘要： The subject invention provides a contraceptive and/or HRT kit comprising a contraceptively and/or therapeutically effective amount of a long-acting etonogestrel ester with a fatty-chain length of C7-C15.

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