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1. 发明申请

US20050137240A1 Selective NPY (Y5) antagonists 失效
标题翻译：选择性NPY（Y5）拮抗剂
公开(公告)号：US20050137240A1
公开(公告)日：2005-06-23
申请号：US11040328
申请日：2005-01-20
申请人： Mohammad Marzabadi , Wai Wong , Stewart Noble , Peter Buhlmayer , Heinrich Rueger , Yasuchika Yamaguchi , Walter Schilling
发明人： Mohammad Marzabadi , Wai Wong , Stewart Noble , Peter Buhlmayer , Heinrich Rueger , Yasuchika Yamaguchi , Walter Schilling
IPC分类号： C07D277/42 , C07D277/60 , C07D417/12 , C07D513/04 , A61K31/426 , C07D277/38
CPC分类号： C07D277/60 , C07D277/42 , C07D417/12 , C07D513/04
摘要： This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.
摘要翻译：本发明涉及作为NPY（Y5）受体的选择性拮抗剂的双环和三环化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。本发明提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了本发明化合物用于制备用于治疗异常的药物组合物的用途，其中所述异常通过降低人Y5受体的活性而减轻。

2. 发明授权

US4889869A Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
标题翻译：由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4889869A
公开(公告)日：1989-12-26
申请号：US341239
申请日：1989-04-19
申请人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
发明人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
IPC分类号： C07D233/54 , C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12
CPC分类号： C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulyhinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译：式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，磺酰基或磺酰基，R 6代表取代的氨基，具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

3. 发明授权

US4758584A Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
标题翻译：由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4758584A
公开(公告)日：1988-07-19
申请号：US011183
申请日：1987-02-05
申请人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
发明人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
IPC分类号： C07D233/54 , C07D401/12 , C07D417/12 , C07K5/02 , A61K37/64 , C07K5/08
CPC分类号： C07D233/64 , C07D401/12 , C07D417/12 , C07K5/0227 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译：式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，亚磺酰基或磺酰基，R 6代表取代的氨基，具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

4. 发明授权

US4914129A Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
标题翻译：由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4914129A
公开(公告)日：1990-04-03
申请号：US405372
申请日：1989-09-08
申请人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
发明人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
IPC分类号： C07D233/54 , C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12
CPC分类号： C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

5. 发明授权

US5719141A 2,9-diamino- and 2-amino-8-carbamoyl-4-hydroxy-alkanoic acid amide derivatives 失效
标题翻译： 2,9-二氨基 - 和2-氨基-8-氨基甲酰基-4-羟基 - 链烷酰胺衍生物
公开(公告)号：US5719141A
公开(公告)日：1998-02-17
申请号：US525254
申请日：1995-09-08
申请人： Vittorio Rasetti , Heinrich Rueger , Jurgen Klaus Maibaum , Robert Mah , Markus Grutter , Nissim Claude Cohen
发明人： Vittorio Rasetti , Heinrich Rueger , Jurgen Klaus Maibaum , Robert Mah , Markus Grutter , Nissim Claude Cohen
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/5355 , A61K31/538 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61P9/12 , C07C237/04 , C07C237/06 , C07C237/22 , C07C271/20 , C07C271/22 , C07D207/00 , C07D209/00 , C07D209/08 , C07D209/42 , C07D211/00 , C07D211/34 , C07D211/60 , C07D213/40 , C07D213/75 , C07D213/89 , C07D215/00 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/36 , C07D215/38 , C07D215/54 , C07D215/56 , C07D217/02 , C07D221/12 , C07D223/16 , C07D235/04 , C07D235/06 , C07D235/08 , C07D239/70 , C07D239/74 , C07D241/00 , C07D241/36 , C07D241/44 , C07D265/28 , C07D265/34 , C07D265/36 , C07D279/12 , C07D279/14 , C07D279/16 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D411/02 , C07D413/02
CPC分类号： C07D213/40 , C07C237/06 , C07C237/22 , C07C271/20 , C07D209/08 , C07D209/42 , C07D211/34 , C07D213/89 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/36 , C07D215/38 , C07D215/54 , C07D215/56 , C07D217/02 , C07D221/12 , C07D223/16 , C07D235/06 , C07D239/74 , C07D241/44 , C07D265/36 , C07D279/16 , C07D401/04 , C07D401/12 , C07D413/04
摘要： Compounds of the formula I ##STR1## in which R.sub.1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R.sub.4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R.sub.5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R.sub.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R.sub.7 is hydrogen or lower alkyl, or R.sub.6 and R.sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R.sub.8 denotes an aliphatic, cycloaliphatic-aliphatic or heteroarylaliphatic radical, and their salts can be used as active ingredients for medicaments for treatment of high blood pressure.
摘要翻译：其中R 1是芳基氨基，N-芳基-N-（低级烷氧基 - 低级烷基） - 氨基，N-芳基-N-芳基 - 低级烷基 - 氨基或杂环基的式I化合物（I）环碳原子，X是羰基或亚甲基，R2和R3彼此独立地是氢或低级烷基，或者与它们所键合的碳原子一起是亚环烷基，R4是氢，低级烷基，低级烷酰基或低级烷氧基羰基，R5是羟基，低级烷酰氧基或低级烷氧基羰基氧基，R6是氢，低级烷基，低级烯基，低级炔基，环烷基，环烷基 - 低级烷基，具有5-7个环原子的芳基 - 低级烷基或杂芳基 - 低级烷基在杂芳基环中，R 7为氢或低级烷基，或者R 6和R 7与它们所键合的碳原子一起为环亚烷基，R 8表示脂族，脂环族 - 脂族或杂芳基脂肪族基团，它们的盐可以是用作治疗药物的有效成分 t的高血压。

6. 发明申请

US20070142401A1 Indolyl-pyrroledione derivatives for the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation 审中-公开
标题翻译：用于治疗与β-淀粉样蛋白生成和/或聚集相关的神经和血管障碍的吲哚基 - 吡咯并二酮衍生物
公开(公告)号：US20070142401A1
公开(公告)日：2007-06-21
申请号：US10576176
申请日：2004-10-26
申请人： Yves Auberson , Graeme Bilbe , Rainer Kuhn , Peter Von Matt , Heinrich Rueger , Matthias Staufenbiel , Jurgen Wagner , Kaspar Zimmermann
发明人： Yves Auberson , Graeme Bilbe , Rainer Kuhn , Peter Von Matt , Heinrich Rueger , Matthias Staufenbiel , Jurgen Wagner , Kaspar Zimmermann
IPC分类号： A61K31/519 , A61K31/506 , A61K31/4709 , A61K31/404
CPC分类号： A61K31/00 , A61K31/496 , A61K31/517
摘要： The invention relates to the use of an inhibitor of formula (I), or a pharmaceutically acceptable salt thereof having an activity on protein kinases PKC alpha, PKC beta, PKC gamma, PKC epsilon, PKC theta, CDK-1, KDR, PKA, Flt-1, Flt-2, Flt-3 or Flt-4, or on a combination of the above enzymes, for the treatment and/or prevention of neurological and vascular disorders related to beta-amyloid generation and/or aggregation such as neurodegenerative diseases like Down's Syndrome, memory and cognitive impairment, dementia, amyloid neuropathies, brain inflammation, nerve and brain trauma, vascular amyloidosis, or cerebral hemorrhage with amyloidosis.
摘要翻译：本发明涉及对蛋白激酶PKCα，PKCβ，PKCγ，PKCε，PKCθ，CDK-1，KDR，PKA等具有活性的式（I）抑制剂或其药学上可接受的盐的用途， Flt-1，Flt-2，Flt-3或Flt-4，或上述酶的组合，用于治疗和/或预防与β-淀粉样蛋白产生和/或聚集相关的神经和血管障碍，例如神经变性疾病如唐氏综合征，记忆和认知障碍，痴呆，淀粉样蛋白神经病，脑炎症，神经和脑外伤，血管淀粉样变性或淀粉样变性脑出血。

7. 发明授权

US09550796B2 Pyrrolopyrrolone derivatives and their use as BET inhibitors 有权
标题翻译：吡咯并吡咯啉衍生物及其作为BET抑制剂的用途
公开(公告)号：US09550796B2
公开(公告)日：2017-01-24
申请号：US15037116
申请日：2014-11-20
申请人： Heinrich Rueger , Jutta Blank , Vincent Bordas , Simona Cotesta , Guido Bold , Vito Guagnano , Andrea Vaupel
发明人： Heinrich Rueger , Jutta Blank , Vincent Bordas , Simona Cotesta , Guido Bold , Vito Guagnano , Andrea Vaupel
IPC分类号： C07D487/04 , A61K31/407 , A61K31/44 , A61K31/5377 , A61K31/506 , A61K31/41 , A61K31/4439 , A61K45/06 , C07D519/00 , A61K31/437 , A61K31/444 , A61K31/4192 , A61K31/513 , A61K31/5025
CPC分类号： C07D519/00 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/506 , A61K31/513 , A61P35/00 , C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐; 制备本发明化合物的方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

8. 发明申请

US20110082227A1 FOAMED POLYESTERS AND METHODS FOR THEIR PRODUCTION 审中-公开
标题翻译：泡沫聚酯及其生产方法
公开(公告)号：US20110082227A1
公开(公告)日：2011-04-07
申请号：US12996648
申请日：2009-06-02
申请人： Heinrich Rueger , Michael Gisler , Linus Villiger , Cédric Muenger
发明人： Heinrich Rueger , Michael Gisler , Linus Villiger , Cédric Muenger
IPC分类号： C08G63/00 , C08G63/46
CPC分类号： C08J9/122 , C08J9/0023 , C08J9/0061 , C08J2201/022 , C08J2201/03 , C08J2203/06 , C08J2205/052 , C08J2367/02 , C08J2400/14 , C08J2467/00 , C08K5/092 , C08K5/1539 , C08L67/02 , C08L67/025 , C08L2666/18
摘要： Foam bodies made of thermoplastic polyesters with high homogeneity, a low open-cell factor and high elongation at break under shear stress, the polyester foam containing at least one thermoplastic elastomer such as a thermoplastic copolyester elastomer, in quantities of, for example, 0.5 to 15% by weight based on the weight of the foam body. The foam bodies can be obtained by foaming a starting polyester with low intrinsic viscosity in a mixture with a modification means in the form of a premix containing dianhydrides of tetracarboxylic acids and thermoplastic copolyester elastomers.
摘要翻译：由热塑性聚酯制成的泡沫体具有高均匀性，低开孔系数和在剪切应力下断裂时的高伸长率，聚酯泡沫含有至少一种热塑性弹性体如热塑性共聚酯弹性体，其量例如为0.5〜基于泡沫体重量的15重量％。泡沫体可以通过以与含有四羧酸和热塑性共聚酯弹性体的二酐的预混物的形式的混合物的混合物中发泡具有低特性粘度的起始聚酯来获得。

9. 发明申请

US20080132477A1 Macrocyclic Compounds Useful as Bace Inhibitors 审中-公开
标题翻译：用作Bace抑制剂的大环化合物
公开(公告)号：US20080132477A1
公开(公告)日：2008-06-05
申请号：US11794413
申请日：2006-01-13
申请人： Claudia Betschart , Andreas Lerchner , Rainer Machauer , Heinrich Rueger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
发明人： Claudia Betschart , Andreas Lerchner , Rainer Machauer , Heinrich Rueger , Marina Tintelnot-Blomley , Siem Jacob Veenstra
IPC分类号： A61K31/395 , C07D487/02
CPC分类号： C07D273/00 , C07D245/04 , C07D273/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/08
摘要： The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及式（I）的新型大环化合物，其中所有变量如说明书中所定义，大环中包括的环原子数为14,15,16或17，游离碱形式或以酸加成盐形式，其制备，用作药物和包含它们的药物。

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