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1. 发明授权

US5519138A Phenylalkyl derivatives, with pharmaceutical activity 失效
标题翻译：苯基烷基衍生物，具有药物活性
公开(公告)号：US5519138A
公开(公告)日：1996-05-21
申请号：US348650
申请日：1994-12-01
申请人： Uwe Ries , Manfred Reiffen , Wolfgang Grell , Norbert Hauel , Berthold Narr , Armin Heckel , Andreas Bomhard , Jacques van Meel , Wolfgang Wienen , Michael Entzeroth
发明人： Uwe Ries , Manfred Reiffen , Wolfgang Grell , Norbert Hauel , Berthold Narr , Armin Heckel , Andreas Bomhard , Jacques van Meel , Wolfgang Wienen , Michael Entzeroth
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/47 , A61K31/496 , A61K31/50 , A61K31/675 , A61P1/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P43/00 , C07D215/20 , C07D215/22 , C07D215/233 , C07D233/68 , C07D235/08 , C07D235/18 , C07D239/91 , C07D403/04 , C07D403/12 , C07D403/14 , C07D471/04 , C07D521/00 , C07F9/6506 , A61K31/41 , C07D401/14 , C07D405/14 , C07D487/04
CPC分类号： C07D215/233 , C07D231/12 , C07D233/56 , C07D233/68 , C07D235/08 , C07D235/18 , C07D239/91 , C07D249/08 , C07D403/04 , C07D403/12 , C07D403/14 , C07D471/04 , C07F9/65068
摘要： A phenylalkyl derivative of the formula ##STR1## wherein R.sub.a to R.sub.f, A and B are substituents and n is the number 0 or 1.These phenylalkyl derivatives possess angiotensin antagonist activity.
摘要翻译：式（I）的苯基烷基衍生物其中Ra至Rf，A和B为取代基，n为数字0或1.这些苯基烷基衍生物具有血管紧张素拮抗剂活性。

2. 发明申请

US20050065346A1 Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions 有权
标题翻译：羧酸酰胺，其制备及其作为药物组合物的用途
公开(公告)号：US20050065346A1
公开(公告)日：2005-03-24
申请号：US10938804
申请日：2004-09-10
申请人： Uwe Ries , Henning Priepke , Armin Heckel , Herbert Nar , Wolfgang Wienen , Jean Marie Stassen
发明人： Uwe Ries , Henning Priepke , Armin Heckel , Herbert Nar , Wolfgang Wienen , Jean Marie Stassen
IPC分类号： C07D295/18 , A61K31/167 , A61K31/18 , A61K31/40 , A61K31/4453 , A61P7/02 , A61P43/00 , C07C257/18 , C07C303/40 , C07C311/21 , C07C311/46 , C07D207/12 , C07D211/46 , C07D213/68 , C07D233/54 , C07D295/135 , C07D295/185 , C07D295/192 , C07D211/32
CPC分类号： C07D295/185 , C07C257/18 , C07C311/21 , C07C311/46 , C07C2601/08 , C07D207/12 , C07D211/46 , C07D213/68 , C07D295/135 , C07D295/192
摘要： The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.
摘要翻译：本发明涉及通式的羧酸酰胺，其中R 1至R 5，Ar，m和n如权利要求1所定义，其互变异构体，立体异构体，其混合物，其前药和其盐具有有价值的性质。其中R5表示氰基的上述通式I的化合物是制备其它通式I化合物的有价值的中间产物，其中R5表示权利要求1中提到的脒基之一的上述通式I的化合物具有有价值的药理学特性，特别是抗血栓形成活性和因子Xa抑制活性。

3. 发明授权

US07425641B2 Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions 有权
标题翻译：羧酸酰胺，其制备及其作为药物组合物的用途
公开(公告)号：US07425641B2
公开(公告)日：2008-09-16
申请号：US10938804
申请日：2004-09-10
申请人： Uwe Ries , Henning Priepke , Armin Heckel , Herbert Nar , Wolfgang Wienen , Jean Marie Stassen
发明人： Uwe Ries , Henning Priepke , Armin Heckel , Herbert Nar , Wolfgang Wienen , Jean Marie Stassen
IPC分类号： C07D272/02 , C07D211/06 , A61K31/40 , A61K31/445
CPC分类号： C07D295/185 , C07C257/18 , C07C311/21 , C07C311/46 , C07C2601/08 , C07D207/12 , C07D211/46 , C07D213/68 , C07D295/135 , C07D295/192
摘要： The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.
摘要翻译：本发明涉及通式其中R 1至R 5，Ar，m和n如权利要求1所定义的羧酸酰胺，互变异构体，立体异构体，混合物其前体药物及其盐具有有价值的性质。其中R 5表示氰基的上述通式I的化合物是制备其它通式I化合物的有价值的中间产物，以及上述通式I的化合物，其中R 1， 5 表示权利要求1中提及的脒基之一具有有价值的药理学性质，特别是抗血栓形成活性和因子Xa抑制活性。

4. 发明授权

US5008290A Sulphonamidoethyl compounds and pharmaceutical compositions comprising these compounds 失效
标题翻译：磺酰氨基乙基化合物和包含这些化合物的药物组合物
公开(公告)号：US5008290A
公开(公告)日：1991-04-16
申请号：US319397
申请日：1989-03-03
申请人： Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
发明人： Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
IPC分类号： A61K31/40 , A61P9/12 , C07D207/32 , C07D207/335 , C07D207/337 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24 , C07D405/04 , C07D409/04 , C07D409/12
CPC分类号： C07D207/335 , C07D207/337 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24 , C07D405/04 , C07D409/04
摘要： The invention relates to new sulphonamidoethyl compounds having valuable pharmacological properties, particularly anti-thrombotic properties, and which are also thromboxane antagonists.

5. 发明授权

US4820705A Benzenesulphonamidoindanyl compounds, medicaments thereof, and processes of preparation 失效
标题翻译：苯磺酰胺基茚满基化合物，其药物及其制备方法
公开(公告)号：US4820705A
公开(公告)日：1989-04-11
申请号：US73950
申请日：1987-07-16
申请人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
发明人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
IPC分类号： A61K31/195 , A61K31/215 , A61K31/235 , A61K31/50 , A61P7/02 , A61P43/00 , B01J23/44 , C07C311/21 , C07C311/29 , C07D237/04 , C07D237/14 , C07D237/24
CPC分类号： C07D237/04
摘要： The invention relates to new benzenesulphonamidoindanyl compounds having the following formula ##STR1## wherein the substituents are defined herein useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.
摘要翻译：本发明涉及具有下式的新的苯磺酰胺基茚满基化合物（Ⅰ），其中本文定义的取代基可用于治疗和预防血栓栓塞性疾病，动脉硬化和肿瘤转移。

6. 发明授权

US4714698A 8-alkylthio-2-piperazino-pyrimido[5,4-d]-pyrimidines 失效
标题翻译： 8-烷硫基-2-哌嗪基 - 嘧啶并[5,4-d] - 嘧啶
公开(公告)号：US4714698A
公开(公告)日：1987-12-22
申请号：US745095
申请日：1985-06-17
申请人： Josef Roch , Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Rainer Zimmermann , Johannes Weisenberger
发明人： Josef Roch , Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Rainer Zimmermann , Johannes Weisenberger
IPC分类号： A61K31/505 , A61K31/55 , A61P7/02 , A61P9/10 , A61P35/00 , C07D487/04 , C07D471/04
CPC分类号： C07D487/04
摘要： The invention relates to new compounds of general formula ##STR1## wherein R.sub.1 represents an alkyl group,R.sub.2 represents a hydrogen atom, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group or an allyl, phenyl or benzyl group,R.sub.3 represents an allyl group, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group orR.sub.2 and R.sub.3 together with the nitrogen atom between them represent a straight-chained alkyleneimino group,the acid addition salts thereof, particularly the acid addition salts thereof with physiologically acceptable inorganic or organic acids which have valuable pharmacological properties, particularly a metastasis-inhibiting effect based on their selective tumour-PDE inhibiting effect, and pharmaceutical compositions containing these compounds or the physiologically acceptable acid addition salts thereof.The new compounds may be prepared according to methods known for analogous compounds.
摘要翻译：本发明涉及通式（I）的新化合物，其中R 1表示烷基，R 2表示氢原子，任选被羟基取代的烷基（除了在α碳原子上），或表示环烷基基团或烯丙基，苯基或苄基，R 3表示烯丙基，任选被羟基取代的烷基（除了在α碳原子上），或表示环烷基或R 2和R 3以及它们之间的氮原子代表直链亚烷基亚氨基，其酸加成盐，特别是其酸加成盐与具有有价值的药理学性质的生理上可接受的无机或有机酸，特别是基于其选择性肿瘤-PDE抑制作用的转移抑制作用，以及含有这些化合物的药物组合物或其生理上可接受的酸加成盐。新化合物可以根据类似化合物已知的方法制备。

7. 发明授权

US4929754A Benzenesulphonamidoindanyl compounds 失效
标题翻译：苯磺酰胺基茚满基化合物
公开(公告)号：US4929754A
公开(公告)日：1990-05-29
申请号：US305255
申请日：1989-02-01
申请人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
发明人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
IPC分类号： A61K31/195 , A61K31/215 , A61K31/235 , A61K31/50 , A61P7/02 , A61P43/00 , B01J23/44 , C07C311/21 , C07C311/29 , C07D237/04
CPC分类号： C07D237/04
摘要： The invention relates to new benzenesulphonamidoindanyl compounds useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.

8. 发明授权

US4870076A Sulphonamidoethyl compounds, pharmaceutical compositions comprising these compounds and processes for preparing them 失效
标题翻译：磺酰氨基乙基化合物，包含这些化合物的药物组合物及其制备方法
公开(公告)号：US4870076A
公开(公告)日：1989-09-26
申请号：US92742
申请日：1987-09-03
申请人： Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
发明人： Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
IPC分类号： A61K31/40 , A61P9/12 , C07D207/32 , C07D207/335 , C07D207/337 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24 , C07D405/04 , C07D409/04 , C07D409/12
CPC分类号： C07D207/335 , C07D207/337 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24 , C07D405/04 , C07D409/04
摘要： The invention relates to new sulphonamido-ethyl compounds having the following structure: ##STR1## wherein R.sub.1 is substituted or unsubstituted phenyl, benzyl, nitrophenyl, acetamidophenyl or thienyl, R.sub.2 is hydroxycarbonyl or alkoxycarbonyl bonded via alkylene or alkenylene, or a 4,5-dihydro-pyridazin-3-one-6-yl or pyridazin-3-on-6-yl group optionally substituted on a ring carbon by C.sub.1 -C.sub.3 alkyl and X is substituted or unsubstituted imino, oxygen or sulphur, which compounds may be used to prevent arteriosclerosis or tumor metastasis, and are antitrombotic and thromboxane antagonists.
摘要翻译：本发明涉及具有以下结构的新型磺酰氨基乙基化合物：其中R1是取代或未取代的苯基，苄基，硝基苯基，乙酰氨基苯基或噻吩基，R2是通过亚烷基或亚烯基键合的羟基羰基或烷氧基羰基，二环哒嗪-3-酮-6-基或哒嗪-3-基-6-基，任选在环碳上被C 1 -C 3烷基取代，X是取代或未取代的亚氨基，氧或硫，可以使用该化合物以防止动脉硬化或肿瘤转移，并且是抗血栓形成和血栓素拮抗剂。

9. 发明授权

US06319918B1 Substituted indolinones with kinase inhibitory activity 有权
标题翻译：具有激酶抑制活性的取代的吲哚啉酮
公开(公告)号：US06319918B1
公开(公告)日：2001-11-20
申请号：US09323499
申请日：1999-06-01
申请人： Armin Heckel , Rainer Walter , Wolfgang Grell , Jacobus C. A. van Meel , Norbert Redemann
发明人： Armin Heckel , Rainer Walter , Wolfgang Grell , Jacobus C. A. van Meel , Norbert Redemann
IPC分类号： A61K3155
CPC分类号： C07D209/30 , C07D209/34
摘要： Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and 3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.
摘要翻译：通用结构式取代的吲哚酮对各种激酶和cyclin / CDK复合物的影响以及各种肿瘤细胞的增殖。示例性化合物是：3-Z- [1-（4-（N-苄基-N-甲基 - 氨基甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮和3-Z- [1- （4-（2,3,4,5-四氢 - 苯并（d）氮杂-3-基 - 甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮。

10. 发明授权

US06855710B2 Substituted indolines with an inhibitory effect on various kinases and complexes of CDKs 有权
标题翻译：取代的吲哚啉对CDK的各种激酶和复合物具有抑制作用
公开(公告)号：US06855710B2
公开(公告)日：2005-02-15
申请号：US10666643
申请日：2003-09-19
申请人： Rainer Walter , Wolfgang Grell , Armin Heckel , Frank Himmelsbach , Wolfgang Eberlein , Gerald Roth , Jacobus C.A. van Meel , Norbert Redemann , Walter Spevak , Ulrike Tontsch-Grunt , Thomas von Rueden
发明人： Rainer Walter , Wolfgang Grell , Armin Heckel , Frank Himmelsbach , Wolfgang Eberlein , Gerald Roth , Jacobus C.A. van Meel , Norbert Redemann , Walter Spevak , Ulrike Tontsch-Grunt , Thomas von Rueden
IPC分类号： C07D401/12 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P43/00 , C07D20060101 , C07D209/34 , C07D209/36 , C07D209/48 , C07D401/14 , C07D403/12
CPC分类号： C07D401/12 , C07D209/34 , C07D403/12
摘要： The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.
摘要翻译：本发明涉及新一代的取代的二氢吲哚酮，其通式为R，R 1至R 5如权利要求1所定义，其异构体及其盐具有有价值的性质。上述通式I的化合物，其中R 1表示氢原子， 3-烷基或前药基团具有有价值的药理学性质，特别是对各种激酶，对病毒细胞周期蛋白和受体酪氨酸激酶的抑制作用，以及上述通式I的其它化合物，其中R1不表示氢原子， C1-3烷基或前药基团是用于制备上述化合物的有价值的中间产物。

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