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1. 发明授权

US06576780B1 Hydroxyamidino derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译：羟脒衍生物可用作一氧化氮合酶抑制剂
公开(公告)号：US06576780B1
公开(公告)日：2003-06-10
申请号：US09687353
申请日：2000-10-13
申请人： Rolando E. Gapud , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Barnett S. Pitzele , Suzanne S. Metz , R. Keith Webber , Foe S. Tjoeng , Robert E. Manning , Mihaly V. Toth
发明人： Rolando E. Gapud , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Barnett S. Pitzele , Suzanne S. Metz , R. Keith Webber , Foe S. Tjoeng , Robert E. Manning , Mihaly V. Toth
IPC分类号： C07F708
CPC分类号： C07D233/64 , C07C257/14 , C07C259/14 , C07C275/16 , C07C313/28 , C07C323/60 , C07C327/22 , C07C329/02 , C07C329/06 , C07C333/04 , C07C391/00 , C07D223/12 , C07D261/08 , C07F7/081
摘要： The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：本发明公开了可用作一氧化氮合酶抑制剂的羟基脒基衍生物。

2. 发明授权

US06207708B1 Hydroxyamidino derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译：羟脒衍生物可用作一氧化氮合酶抑制剂
公开(公告)号：US06207708B1
公开(公告)日：2001-03-27
申请号：US09038292
申请日：1998-03-11
申请人： Rolando E. Gapud , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Barnett S. Pitzele , Suzanne S. Metz , R. Keith Webber , Foe S. Tjoeng , Robert E. Manning , Mihaly V. Toth
发明人： Rolando E. Gapud , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Barnett S. Pitzele , Suzanne S. Metz , R. Keith Webber , Foe S. Tjoeng , Robert E. Manning , Mihaly V. Toth
IPC分类号： A61K3119
CPC分类号： C07D233/64 , C07C257/14 , C07C259/14 , C07C275/16 , C07C313/28 , C07C323/60 , C07C327/22 , C07C329/02 , C07C329/06 , C07C333/04 , C07C391/00 , C07D223/12 , C07D261/08 , C07F7/081
摘要： The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：本发明公开了可用作一氧化氮合酶抑制剂的羟基脒基衍生物。

4. 发明授权

US5945408A Hydroxyanidino derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译：羟基亚氨基衍生物可用作一氧化氮合酶抑制剂
公开(公告)号：US5945408A
公开(公告)日：1999-08-31
申请号：US689463
申请日：1996-08-08
申请人： R. Keith Webber , Foe S. Tjoeng , Robert E. Manning
发明人： R. Keith Webber , Foe S. Tjoeng , Robert E. Manning
IPC分类号： A61K31/00 , A61K31/155 , A61K31/195 , A61K31/197 , A61K31/22 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/42 , A61K31/535 , A61K31/5377 , A61K31/5395 , A61K31/55 , A61P9/00 , A61P25/04 , A61P29/00 , A61P37/00 , C07C257/14 , C07C259/14 , C07C271/22 , C07C275/16 , C07C313/28 , C07C313/34 , C07C323/60 , C07C327/22 , C07C329/02 , C07C329/06 , C07C333/04 , C07C391/00 , C07D223/12 , C07D233/56 , C07D233/76 , C07D261/08 , C07D273/02 , C07F7/08 , C07K5/068 , C07F7/10 , A01N55/00
CPC分类号： C07F7/0818 , C07C257/14 , C07C259/14 , C07C275/16 , C07C313/28 , C07C323/60 , C07C327/22 , C07C329/02 , C07C329/06 , C07C333/04 , C07C391/00 , C07D223/12 , C07D261/08
摘要： The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：本发明公开了可用作一氧化氮合酶抑制剂的羟基脒基衍生物。

5. 发明授权

US07132437B2 Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension 失效
标题翻译：用于治疗高血压的肾选择性联苯基烷基1H-取代-1,2,4-三唑血管紧张素II拮抗剂
公开(公告)号：US07132437B2
公开(公告)日：2006-11-07
申请号：US10852711
申请日：2004-05-24
申请人： David B. Reitz , Robert E. Manning
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D403/10 , H01M2/1055 , H04B1/3883 , H04B2001/3894
摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-[[4′-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl][1,1′-biphenyl]-2-yl]]carbonylhydrazide, (shown below) is an example:
摘要翻译：描述了肾选择性化合物，其在一个实施方案中是优先在肾中转化为能够阻断血管紧张素II（AII）受体的化合物的前药。这些前药是由两种组分形成的缀合物，即由AII拮抗剂化合物提供的第一组分和当两种组分在缀合物内化学连接时能够从第一组分切割的第二组分。两种组分通过在肾脏中有选择性地切割的键化学连接，例如通过酶。然后释放的AII拮抗剂化合物可用于阻断肾脏内的AII受体。特别感兴趣的结合物是联苯甲基1H-取代-1,2,4-三唑化合物的谷氨酰基衍生物，其中N-乙酰谷氨酸5 - [[4' - [（3,5-二丁基-1H-1,2,4-三唑） 4-三唑-1-基）甲基] [1,1'-联苯] -2-基]]羰酰肼，（如下所示）是一个实例：

6. 发明授权

US06630497B2 1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders 失效
标题翻译： 1-苯基咪唑-2-酮联苯甲基化合物，用于治疗循环系统疾病
公开(公告)号：US06630497B2
公开(公告)日：2003-10-07
申请号：US09825029
申请日：2001-04-03
申请人： David B. Reitz , Robert E. Manning
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A61K314178
CPC分类号： C07D403/10 , C07D233/70
摘要： A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein each of R1, R2 and R3 is independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrido, and with the further proviso that when each of R1 and R3 is hydrido, then R2 cannot be chloro; wherein R4 is hydrido; wherein R5 is alkyl; and wherein R6 is tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：描述了一类用于治疗循环障碍的1-苯基咪唑-2-酮联苯甲基化合物。 R 1，R 2和R 3各自独立地选自氢，烷基，烷氧基，氰基，卤素，羟基，羧基，烷氧基羰基，甲酰基和乙酰基。 ; 烷基羰基和卤代烷基羰基; 条件是R 1，R 2和R 3中的至少一个必须是除氢环以外的取代基，另外条件是当R 1和R 3各自为氢时那么R 2不能是氯; 其中R 4是氢的; 其中R 5是烷基; 并且其中R 6是四唑基; 或其立体异构体或其互变异构体或其药学上可接受的盐。这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

7. 发明授权

US06268392B1 Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors 失效
标题翻译：使用回肠胆汁酸转运抑制苯并噻二嗪和HMG Co-A还原酶抑制剂的联合治疗
公开(公告)号：US06268392B1
公开(公告)日：2001-07-31
申请号：US09037308
申请日：1998-03-09
申请人： Bradley T. Keller , Kevin C. Glenn , Robert E. Manning
发明人： Bradley T. Keller , Kevin C. Glenn , Robert E. Manning
IPC分类号： A61K3138
CPC分类号： C07D495/04 , A61K31/22 , A61K31/366 , A61K31/38 , A61K31/405 , A61K45/06 , C07D337/06 , C07D337/08 , C07D409/10 , C07D495/10 , C08G65/329 , A61K2300/00
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and EG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
摘要翻译：提供了新的苯并噻庚因，衍生物和类似物; 含有它们的药物组合物; 以及在医学中使用这些化合物和组合物的方法，特别是用于预防和治疗哺乳动物中高脂血症的疾病，例如与动脉粥样硬化或高胆固醇血症有关的那些。还提供了使用回肠胆汁酸转运抑制剂和EG Co-A还原酶抑制剂联合治疗高脂血症的组合物和方法。

8. 发明授权

US5736579A Substituted spiro compounds for the treatment of inflammation 失效
公开(公告)号：US5736579A
公开(公告)日：1998-04-07
申请号：US341734
申请日：1994-11-18
申请人： David B. Reitz , Robert E. Manning , Horng-Chi Huang , Jinglin Li
发明人： David B. Reitz , Robert E. Manning , Horng-Chi Huang , Jinglin Li
IPC分类号： C07C311/16 , C07C311/29 , C07C317/14 , C07C317/22 , C07C323/65 , C07D213/34 , C07D213/61 , C07D213/70 , C07D317/56 , A61K31/44 , A61K31/10 , A61K31/18
CPC分类号： C07D213/70 , C07C311/16 , C07C311/29 , C07C317/14 , C07C317/22 , C07C323/65 , C07D213/34 , C07D213/61 , C07D317/56 , C07C2102/50 , Y10S514/883 , Y10S514/886
摘要： A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.

9. 发明授权

US5504106A Phenyl amidine alkanoic acids and lactones useful as platelet aggregation inhibitors 失效
标题翻译：苯脒链烷酸和内酯可用作血小板聚集抑制剂
公开(公告)号：US5504106A
公开(公告)日：1996-04-02
申请号：US256707
申请日：1994-07-21
申请人： Norman A. Abood , Robert E. Manning , Masateru Miyano
发明人： Norman A. Abood , Robert E. Manning , Masateru Miyano
IPC分类号： C07C257/18 , C07D309/30 , C07D405/04 , A61K31/34
CPC分类号： C07D405/04 , C07C257/18 , C07D309/30
摘要： This invention relates to phenyl amidine alkanoic acids and lactones having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.
摘要翻译： PCT No.PCT / US93 / 05861 Sec。 371日期：1994年7月21日 102（e）日期1994年7月21日PCT提交1993年6月23日PCT公布。出版物WO94 / 0042400 日本1994年1月6日。本发明涉及具有下式的苯基脒链烷酸和内酯或其药学上可接受的盐，其可用于抑制血小板聚集。本发明还涉及这种苯基脒衍生物的药物组合物。

10. 发明授权

US5451597A Treatment of circulatory disorders using n-substituted (.alpha.-imidazolyl-toluyl) pyrrole angiotensin II antagonists 失效
标题翻译：使用N-取代的（α-咪唑基 - 甲苯酰基）吡咯血管紧张素II拮抗剂治疗循环障碍
公开(公告)号：US5451597A
公开(公告)日：1995-09-19
申请号：US66057
申请日：1993-05-27
申请人： Philippe R. Bovy , Joe T. Collins , Robert E. Manning
发明人： Philippe R. Bovy , Joe T. Collins , Robert E. Manning
IPC分类号： A61K31/4178 , C07D233/90 , C07D403/10 , C07D403/14 , A61K31/415 , A61K31/41 , C07D403/04
CPC分类号： C07D403/10 , A61K31/4178 , C07D403/14
摘要： A class of N-substituted (.alpha.-imidazolyltoluyl)pyrrole compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sub.3, R.sub.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.8 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl, methoxycarbonyl with the proviso that at least one of R.sup.5 and R.sup.8 is an acidic group selected from CO.sub.2 H and tetrazolyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：描述了一类用于治疗循环系统疾病的N-取代的（α-咪唑基甲苯磺酰基）吡咯化合物。特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R 0选自CH 2 OH，CO 2 H，CHO，CO 2 CH 3，CO 2 C 2 H 5，CH 2 OCH 3，CH 2 OCHOCH 3和CH 2 -CO 2 C 2 H 5; 其中R 1选自Cl，CF 3，CHO，正丁基，氰基，CO 2 CH 3和CO 2 CH 2 CH 3; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基，，丁硫基和羟烷基; 其中R3，R4，R6，R7，R9和R10各自为氢; 其中R 5和R 8各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基，甲氧基羰基，条件是R 5和R 8中的至少一个是选自CO 2 H和四唑基的酸性基团。或其互变异构体或其药学上可接受的盐。这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

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