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1. 发明授权

US5484937A N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders 失效
标题翻译：用于治疗循环障碍的N-取代的N-（α-三唑基 - 甲苯酰基）吡咯化合物
公开(公告)号：US5484937A
公开(公告)日：1996-01-16
申请号：US117269
申请日：1993-09-07
申请人： Philippe R. Bovy , David B. Reitz , Robert E. Manning
发明人： Philippe R. Bovy , David B. Reitz , Robert E. Manning
IPC分类号： C07D521/00 , C07D403/10 , A61K31/41
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds 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.1 is selected from alkyl; and wherein R.sup.2 is selected from alkyl; and wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; 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：描述用于治疗循环系统疾病的一类N-取代的N-（α-三唑基甲苯磺酰基）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R1选自烷基; 并且其中R 2选自烷基; R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3，OH，其中R42和R43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 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。

2. 发明授权

US5175180A N-substituted N-(alpha-triazolyl-toluyl)pyrrole compounds and use for treatment of circulatory disorders 失效
标题翻译： N-取代的N-（ALPHA-TRIAZOLYL-TOLUYL）吡咯烷酮化合物和用于治疗循环障碍的用途
公开(公告)号：US5175180A
公开(公告)日：1992-12-29
申请号：US630714
申请日：1990-12-20
申请人： Philippe R. Bovy , David B. Reitz , Robert E. Manning
发明人： Philippe R. Bovy , David B. Reitz , Robert E. Manning
IPC分类号： C07D403/10 , C07D403/14
CPC分类号： C07D403/10 , C07D403/14
摘要： A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds 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.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; 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, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; 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：描述用于治疗循环系统疾病的一类N-取代的N-（α-三唑基甲苯磺酰基）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R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，正戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 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，丙硫基，丁硫基，和羟烷基; 其中R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3，OH，其中R42和R43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 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。

3. 发明授权

US6008368A Pharmaceutical compositions for treatment of circulatory disorders using N-substituted (.alpha.-imidazolyl-toluyl) pyrrole aniotensin II antagonists 失效
标题翻译：使用N-取代的（α-咪唑基 - 甲苯酰基）吡咯类抗生素II拮抗剂治疗循环障碍的药物组合物
公开(公告)号：US6008368A
公开(公告)日：1999-12-28
申请号：US976757
申请日：1997-11-24
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： C07D233/90 , C07D403/10 , A61K31/415 , A61K31/41 , C07D403/04 , C07D403/14
CPC分类号： C07D403/10
摘要： Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds 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.sup.3, R.sup.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 C02H and tetrazolyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compositions are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：描述了包含选自一类N-取代的（α-咪唑基 - 甲苯酰基）吡咯化合物的化合物的药物组合物用于治疗循环障碍。特别感兴趣的组合物包括下式的血管紧张素II拮抗剂化合物其中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。这些组合物特别可用于治疗或控制高血压和充血性心力衰竭。

4. 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。

5. 发明授权

US5187271A N-substituted (.alpha.-imidazolyl-toluyl) pyrrole compounds for treatment of circulatory disorders 失效
标题翻译： N-取代（（ALPHA）-IMIDAZOLYL-TOLUYL）用于治疗循环障碍的吡咯化合物
公开(公告)号：US5187271A
公开(公告)日：1993-02-16
申请号：US662584
申请日：1991-02-28
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： C07D403/10 , C07D403/14
CPC分类号： C07D403/10 , C07D403/14
摘要： A class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds 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 each of R.sup.0 and R.sup.1 is independently selected from hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl, cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl, alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy, alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl, alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; 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, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：描述用于治疗循环系统疾病的一类N-取代（α-咪唑基 - 甲苯酰基）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和R 1各自独立地选自氢，烷基，羟基烷基，甲酰基，卤素，卤代烷基，环烷基羰基，烷氧基，芳酰基，芳氧基，芳烷氧基，烷基羰基，烷氧基羰基，氰基，硝基，羧基，烷基羰基氧基，烷基羰基氧基烷基，烷氧基羰基烷基，芳烷氧基羰基烷基，烷基磺酰基，芳烷基磺酰基，芳基磺酰基; 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，丙硫基，丁硫基，和羟烷基; 其中R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，其中R 42和R 43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 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。

6. 发明授权

US5106834A Linear free-sulfhydryl-containing oligopeptide derivatives as antihypertensive agents 失效
标题翻译：含有线性游离巯基的寡肽衍生物作为抗高血压药
公开(公告)号：US5106834A
公开(公告)日：1992-04-21
申请号：US290667
申请日：1988-12-27
申请人： Philippe R. Bovy , Robert E. Manning , Joan M. O'Neal
发明人： Philippe R. Bovy , Robert E. Manning , Joan M. O'Neal
IPC分类号： A61K38/00 , C07K14/58
CPC分类号： C07K14/582 , A61K38/00
摘要： Synthesis and use of novel oligopeptides are described, many of which peptides contain one or several unnatural amino acids. These short linear peptide derivatives are characterized by the presence of a free sulfhydryl function. These compounds have a high affinity for the Atrial Natriuretic Peptide (ANP) receptor coupled to particulate guanylate cyclase. Such peptides are full agonists at the ANP receptor as demonstrated by the ability of the peptides to stimulate the production of cGMP and to relax smooth muscles in vitro. In accord with these observations, the compounds of the invention lower blood pressure in mammals. Preferred peptides are the following:Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; and Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH.sub.2.
摘要翻译：描述了新型寡肽的合成和应用，其中许多肽含有一个或多个非天然氨基酸。这些短的线性肽衍生物的特征在于存在游离的巯基官能团。这些化合物对与鸟苷酸环化酶颗粒偶联的心房利钠肽（ANP）受体具有高亲和力。这些肽是ANP受体的完全激动剂，如通过肽在体外刺激cGMP的产生和放松平滑肌的能力所证明的。根据这些观察结果，本发明化合物降低了哺乳动物的血压。优选的肽如下：Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; 和Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH 2。

7. 发明授权

US06451833B1 N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders 失效
标题翻译：用于治疗循环系统疾病的N-取代的（α-咪唑基 - 甲苯酰基）吡咯化合物
公开(公告)号：US06451833B1
公开(公告)日：2002-09-17
申请号：US09704389
申请日：2000-11-01
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： A61K314178
CPC分类号： C07D403/10 , C07D403/14
摘要： A class of N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein m is one; wherein each of R0 and R1 is independently selected from hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl, cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl, alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy, alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl, alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R5 and R8 must be selected from COOH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, wherein each of R42 and R43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：一类描述用于治疗循环系统疾病的N-取代（α-咪唑基 - 甲苯酰基）吡咯化合物。化合物特别有意义的是血管紧张素II拮抗剂，其中R 0和R 1各自独立地选自氢，烷基，羟基烷基，甲酰基，卤素，卤代烷基，环烷基羰基，烷氧基，芳酰基，芳氧基，芳烷氧基，烷基羰基，烷氧基羰基，氰基，硝基，羧基，烷基羰基氧基，烷基羰氧基烷基，烷氧基羰基烷基，芳烷氧基羰基烷基，烷基磺酰基，芳烷基磺酰基，芳基磺酰基; 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，丙硫基，丁硫基，和羟烷基; 其中R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，其中R 42和R 43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 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。

8. 发明申请

US20080261949A1 CYCLOHEXYL(ALKYL)PROPANOLAMINES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 有权
公开(公告)号：US20080261949A1
公开(公告)日：2008-10-23
申请号：US12144843
申请日：2008-06-24
申请人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
发明人： Philippe R. Bovy , Roberto Cecchi , Gilles Courtemanche , Tiziano Croci , Ambrogio Oliva , Nunzia Viviani
IPC分类号： A61K31/553 , C07C311/01 , A61K31/24 , A61K31/421 , C07D263/54 , C07D267/02
CPC分类号： C07C311/21 , C07C229/46 , C07C311/08 , C07C317/22 , C07C2601/14
摘要： The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

9. 发明授权

US5872122A Pyrimidinylamidino .beta.-amino acid derivatives useful as inhibitors of platelet aggregation 失效
标题翻译：可用作血小板聚集抑制剂的嘧啶基脒基β-氨基酸衍生物
公开(公告)号：US5872122A
公开(公告)日：1999-02-16
申请号：US951560
申请日：1997-10-16
申请人： Philippe R. Bovy , Henry E. Dayringer , Steven P. Adams
发明人： Philippe R. Bovy , Henry E. Dayringer , Steven P. Adams
IPC分类号： A61K38/00 , C07D239/30 , C07D401/12 , C07D405/12 , C07K5/02 , A61K31/505 , A61K38/06 , C07D239/26 , C07K5/08
CPC分类号： C07D401/12 , C07D239/30 , C07D405/12 , C07K5/021 , A61K38/00
摘要： This invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutical compositions of such compounds and a method of treatment to inhibit aggregation of platelets.
摘要翻译：本发明提供式IMA化合物或其药学上可接受的盐。本发明还提供了这种化合物的药物组合物和抑制血小板聚集的治疗方法。

10. 发明授权

US5104891A Cycloheptimidazolone compounds as angiotensin II antagonists for control of hypertension 失效
标题翻译：环丙沙星化合物作为血管紧张素II拮抗剂用于控制高血压
公开(公告)号：US5104891A
公开(公告)日：1992-04-14
申请号：US449700
申请日：1989-12-11
申请人： Philippe R. Bovy , Joan M. O'Neal , Timothy S. Chamberlain , Joe T. Collins
发明人： Philippe R. Bovy , Joan M. O'Neal , Timothy S. Chamberlain , Joe T. Collins
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/675 , A61P9/00 , A61P9/04 , A61P9/12 , A61P43/00 , C07D235/02 , C07D403/10 , C07F9/6558
CPC分类号： C07D235/02 , C07D403/10
摘要： A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.

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