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1. 发明授权

US09079858B2 Rock kinase inhibitors 有权
标题翻译：岩石激酶抑制剂
公开(公告)号：US09079858B2
公开(公告)日：2015-07-14
申请号：US14241092
申请日：2012-08-31
申请人： Jo Alen , Sandro Boland , Arnaud Pierre Jean Bourin , Olivier Defert , Dirk Leysen
发明人： Jo Alen , Sandro Boland , Arnaud Pierre Jean Bourin , Olivier Defert , Dirk Leysen
IPC分类号： C07D213/00 , C07D213/79 , C07D213/74 , A61K31/44 , A61K31/443 , C07D213/75 , C07D405/12 , C07D413/12 , C07D401/12 , C07D417/12 , C07D409/12
CPC分类号： C07D213/74 , A61K31/44 , A61K31/443 , C07D213/75 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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.
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。

2. 发明授权

US09067889B2 Biphenylcarboxamides as ROCK kinase inhibitors 有权
标题翻译：联苯甲酰胺作为ROCK激酶抑制剂
公开(公告)号：US09067889B2
公开(公告)日：2015-06-30
申请号：US14241093
申请日：2012-08-31
申请人： Jo Alen , Sandro Boland , Arnaud Pierre Jean Bourin , Olivier Defert , Dirk Leysen
发明人： Jo Alen , Sandro Boland , Arnaud Pierre Jean Bourin , Olivier Defert , Dirk Leysen
IPC分类号： A61K31/04 , C07D401/12 , C07D213/74 , A61K31/44 , A61K31/443 , C07D213/75 , C07D405/12 , C07D413/12 , C07D417/12 , C07D409/12
CPC分类号： C07D213/74 , A61K31/44 , A61K31/443 , C07D213/75 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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, gastrointestinal diseases and respiratory diseases.
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，胃肠道疾病和呼吸系统疾病）的药物中的方法。

3. 发明申请

US20070155836A1 Steroids having a mixed androgenic and progestagenic profile 失效
标题翻译：具有混合雄激素和孕激素特征的类固醇
公开(公告)号：US20070155836A1
公开(公告)日：2007-07-05
申请号：US10584006
申请日：2004-12-15
申请人： Jaap Van Der Louw , Dirk Leysen , Arii Grootenhuis , Marcel De Gooijer
发明人： Jaap Van Der Louw , Dirk Leysen , Arii Grootenhuis , Marcel De Gooijer
IPC分类号： A61K31/22 , A61K31/15 , A61K31/12 , C07C67/02
CPC分类号： C07J63/008
摘要： This invention provides 19-nor-D-homos-teroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R1 is O, or NOR, with R being hydrogen, (C1-6)alkyl or (C1-6)acyl, R2 is methyl or ethyl, and R3 is hydrogen or (C1-15)acyl.
摘要翻译：本发明提供具有口服活性的混合雄激素/孕激素分布的19-去甲基-D-同系物，预防小梁骨矿物质密度（BMD）损失，并且其缺乏肝毒性，具有根据式 I）其中R 1是O或NOR，其中R是氢，（C 1-6 - ）烷基或（C 1-6）烷基或 >）酰基，R 2是甲基或乙基，R 3是氢或（C 1-15）酰基。

4. 发明申请

US20060094698A1 Self-administered contraceptive injection of oily solution 审中-公开
标题翻译：自制避孕注射油性溶液
公开(公告)号：US20060094698A1
公开(公告)日：2006-05-04
申请号：US10515714
申请日：2003-05-23
申请人： Henrik De Nijs , Hendrikus Adrianus Van Der Voort , Dirk Leysen
发明人： Henrik De Nijs , Hendrikus Adrianus Van Der Voort , Dirk Leysen
IPC分类号： A61K31/56 , A61M31/00
CPC分类号： A61K9/0021 , A61K9/0019 , A61K31/569 , A61K45/06 , A61K47/14 , A61K47/44 , A61K2300/00
摘要： The subject invention provides a pharmaceutical formulation in the form of an oily solution for injection to a subject comprising a contraceptively and/or therapeutically effective amount of a long-acting progestogen and a contraceptively and/or therapeutically effective amount of a long-acting androgen dissolved in a pharmaceutically acceptable oily medium wherein the injection is administered by the subject itself with a needle-less device, a mini-needle device or a pre-filled subcutaneous syringe.
摘要翻译：本发明提供了一种用于注射给受试者的油性溶液形式的药物制剂，包括避孕和/或治疗有效量的长效孕激素和避孕和/或治疗有效量的长效雄激素溶解在药学上可接受的油性介质中，其中注射由受试者本身用无针装置，微型针装置或预填充的皮下注射器施用。

5. 发明授权

US06552011B1 (Androst-5-en-17beta -yl)alkyl sulfoxides and sulfones and their use for control of fertility 失效
标题翻译：（雄甾-5-en-17β-基）烷基亚砜和砜及其用于控制生育力的用途
公开(公告)号：US06552011B1
公开(公告)日：2003-04-22
申请号：US09913932
申请日：2001-08-20
申请人： Dirk Leysen , Jaap van der Louw , Anja Wiersma
发明人： Dirk Leysen , Jaap van der Louw , Anja Wiersma
IPC分类号： A61K3156
CPC分类号： A61K31/573 , Y10S514/841 , Y10S514/843
摘要： The invention relates to (androst-5-en-17beta-yl)alkylsulfoxides and sulfones having general formula (I), wherein R1, R2, R3, X and Y are defined in the specification. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.
摘要翻译：本发明涉及具有通式（I）的（雄甾-5-烯-17β-基）烷基亚砜和砜，其中R1，R2，R3，X和Y在本说明书中定义。本发明的化合物具有减数分裂抑制活性，可用于控制生育力。

6. 发明授权

US06313139B1 Benzylamine derivatives which are useful in treating psychiatric disorders 有权
标题翻译：可用于治疗精神疾病的苄胺衍生物
公开(公告)号：US06313139B1
公开(公告)日：2001-11-06
申请号：US09359284
申请日：1999-07-22
申请人： Fredericus Antonius Dijcks , Dirk Leysen , Joannes Theodorus Maria Linders , Gerardus Stephanus Franciscus Ruigt , Ian Craig Carlyle , Simon James Anthony Grove , Duncan Robertson Rae , Simon N. Thorn
发明人： Fredericus Antonius Dijcks , Dirk Leysen , Joannes Theodorus Maria Linders , Gerardus Stephanus Franciscus Ruigt , Ian Craig Carlyle , Simon James Anthony Grove , Duncan Robertson Rae , Simon N. Thorn
IPC分类号： A61K31437
CPC分类号： C07D413/04 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/137 , A61K31/15 , A61K31/381 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/437 , A61K31/472 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/58
摘要： The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
摘要翻译：本发明涉及某些新的苄胺衍生物，其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是治疗抑郁症。

7. 发明授权

US6080773A Benzylamine derivatives which are useful in treating psychiatric disorders 失效
标题翻译：可用于治疗精神疾病的苄胺衍生物
公开(公告)号：US6080773A
公开(公告)日：2000-06-27
申请号：US950359
申请日：1997-10-14
申请人： Fredericus Antonius Dijcks , Dirk Leysen , Joannes Theodorus Maria Linders , Gerardus Stephanus Franciscus Ruigt , Ian Craig Carlyle , Simon James Anthony Grove , Duncan Robertson Rae , Simon N. Thorn
发明人： Fredericus Antonius Dijcks , Dirk Leysen , Joannes Theodorus Maria Linders , Gerardus Stephanus Franciscus Ruigt , Ian Craig Carlyle , Simon James Anthony Grove , Duncan Robertson Rae , Simon N. Thorn
IPC分类号： G01N33/50 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/416 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/47 , A61K31/472 , A61K31/496 , A61K31/505 , A61K45/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07C47/55 , C07C47/575 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/48 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/56 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/56 , C07D333/58 , C07D413/04 , C07D498/04 , G01N33/15 , A61K31/415
CPC分类号： C07D413/04 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/137 , A61K31/15 , A61K31/381 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/437 , A61K31/472 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/58
摘要： The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
摘要翻译：本发明涉及某些新的苄胺衍生物，其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是治疗抑郁症。

8. 发明授权

US5190965A Phenoxyphenyl derivatives, compositions and methods of use thereof 失效
标题翻译：苯氧基苯基衍生物，组合物及其使用方法
公开(公告)号：US5190965A
公开(公告)日：1993-03-02
申请号：US891545
申请日：1992-05-29
申请人： Gerardus S. F. Ruigt , Dirk Leysen , Johannes H. Wieringa
发明人： Gerardus S. F. Ruigt , Dirk Leysen , Johannes H. Wieringa
IPC分类号： A61K31/135 , A61K31/415 , A61P25/24 , A61P25/26 , C07C213/00 , C07C217/58 , C07D233/22
CPC分类号： C07C217/58 , C07D233/22
摘要： The invention concerns a phenoxyphenyl derivative having the formula ##STR1## wherein R is one or two halogen atoms; andA is CH.sub.2 NR.sub.1 R.sub.2 or 4,5-dihydro-1H-imidazole, in which R.sub.1 and R.sub.2 are independently selected from hydrogen and lower alkyl; ora pharmaceutically acceptable salt thereof.The compounds have long half-lives and can be used against depression.
摘要翻译：本发明涉及具有下式的苯氧基苯基衍生物：其中R是一个或两个卤素原子; 并且A是CH2NR1R2或4,5-二氢-1H-咪唑，其中R 1和R 2独立地选自氢和低级烷基; 或其药学上可接受的盐。这些化合物具有较长的半衰期，可用于抵抗抑郁症。

9. 发明授权

US09073905B2 Rock inhibitors 有权
标题翻译：岩石抑制剂
公开(公告)号：US09073905B2
公开(公告)日：2015-07-07
申请号：US14113941
申请日：2012-04-27
申请人： Dirk Leysen , Olivier Defert , Sandro Boland , Jo Alen , Arnaud Pierre Jean Bourin
发明人： Dirk Leysen , Olivier Defert , Sandro Boland , Jo Alen , Arnaud Pierre Jean Bourin
IPC分类号： C07D409/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D451/04 , A61K31/4725 , A61K31/439 , A61K31/4468
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。

10. 发明申请

US20140371268A1 BIPHENYLCARBOXAMIDES AS ROCK KINASE INHIBITORS 有权
标题翻译：作为岩石激酶抑制剂的双嘧达莫
公开(公告)号：US20140371268A1
公开(公告)日：2014-12-18
申请号：US14241093
申请日：2012-08-31
申请人： Jo Alen , Sandro Boland , Arnaud Pierre Jean Bourin , Olivier Defert , Dirk Leysen
发明人： Jo Alen , Sandro Boland , Arnaud Pierre Jean Bourin , Olivier Defert , Dirk Leysen
IPC分类号： C07D213/74 , C07D401/12 , C07D409/12 , C07D405/12
CPC分类号： C07D213/74 , A61K31/44 , A61K31/443 , C07D213/75 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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, gastrointestinal diseases and respiratory diseases.
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，胃肠道疾病和呼吸系统疾病）的药物中的方法。

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