会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明申请
    • 1-ARYLHETEROARYLALKYL SUBSTITUTED-1H-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS
    • 用于治疗循环障碍的1-ARYLHETEROARYLALKYL取代的1 H-1,2,4-三唑类化合物
    • WO1992018092A2
    • 1992-10-29
    • PCT/US1992002801
    • 1992-04-10
    • G.D. SEARLE & CO.REITZ, David, B.
    • G.D. SEARLE & CO.
    • A61K0
    • C07D231/12C07D233/56C07D249/08C07D401/06C07D401/10C07D401/14
    • A class of 1-arylheteroarylalkyl substituted-1H-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula (I) wherein A is selected from (1, 2, 3, 4, 5 and 6), wherein m is one; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, 2-ethylbutyl, 1,1-difluorobutyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, ethylbutyl, n-pentyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, phenyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and buthylthio; wherein R5 is an acidic group selected from CO¿2?H and tetrazole radicals; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
    • 5. 发明申请
    • N-SUBSTITUTED N-('alpha'-TRIAZOLYL-TOLUYL)PYRROLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS
    • N-取代的N-(α-三唑基 - 叔丁基)吡咯烷化合物,用于治疗循环障碍
    • WO1992011255A1
    • 1992-07-09
    • PCT/US1991008726
    • 1991-11-26
    • G.D. SEARLE & CO.BOVY, Philippe, R.REITZ, David, B.MANNING, Robert, E.
    • G.D. SEARLE & CO.
    • C07D403/14
    • C07D403/10C07D403/14
    • A class of N-substituted N-(α-triazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein m is one; wherein R1 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 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 R?3, R4, R5, R6, R7, R8, R9 and R10¿ is independently selected from hybrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R?5 and R8¿ must be selected from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, a), b) and c) wherein each of R?42 and R43¿ 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.
    • 7. 发明申请
    • N-SUBSTITUTED-1,2,4-TRIAZOLONE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS
    • 用于治疗心血管疾病的N-取代的1,2,4-三唑酮化合物
    • WO1991018888A1
    • 1991-12-12
    • PCT/US1991003449
    • 1991-05-23
    • G.D. SEARLE & CO.MANNING, Robert, E.REITZ, David, B.HUANG, Horng-Chih
    • G.D. SEARLE & CO.
    • C07D249/12
    • C07D403/10C07D249/12
    • A class of N-substituted-1,2,4-triazolone compounds is described for use in treatment of cardiovascular disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein R is selected from 2-oxo-2-(tricyclo[3.3.1.1. ]dec-2-yl)ethyl, 3-phenylpropyl, 2-oxo-2-phenylethyl, 2-hyroxy-2-phenylethyl, 1,1-dimethylethyloxycarbonylmethyl, hexyl, ethoxycarbonylmethyl, carboxymethyl, 1-naphthalenylmethyl, 2-cyclohexylethyl, pentyl, ethoxycarbonylmethoxyethyl substituted with phenyl, carboxymethoxyethyl substituted with phenyl, 3,5,5-trimethylhexyl, (2-phenylmethoxy)-1-(phenylmethyl)-E-ethenyl, 1-benzoyl-2-phenylethyl, 1-oxobutyl, 2-(2,5-dimethyoxyphenyl)-2-oxoethyl, 2-phenyl-2-(phenylmethoxyethyl, 2-(2,5-dimethioxy-phenyl)-2-hydroxyethyl, 2-naphthalenylmethyl, methoxycarbonyl-butyl, ethoxycarbonylethyl substituted with benzoyl, 1-benzyoyl-1-methylethyl, 1-pentanoic acid, cyclopropylmethyl, 3-phenyl-2E-propenyl and 3-acetonitrile; wherein R is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neopentyl, 1-cyanobutyl, propylthio and butylthio; wherein each of R through R is hydrido with the proviso that at least one of R and R must be selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (a), (b) and (c), wherein each of R and R is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
    • 描述了一类用于治疗心血管疾病的N-取代的1,2,4-三唑酮化合物。 特别感兴趣的化合物是式(I)的血管紧张素II拮抗剂,其中R 1选自2-氧代-2-(三环[3.3.1.1.33.2]癸-2-基)乙基,3-苯基丙基 ,2-氧代-2-苯基乙基,2-羟基-2-苯基乙基,1,1-二甲基乙氧基羰基甲基,己基,乙氧基羰基甲基,羧甲基,1-萘基甲基,2-环己基乙基,戊基,被苯基取代的乙氧基羰基甲氧基乙基,被苯基取代的羧基甲氧基乙基, ,5,5-三甲基己基,(2-苯基甲氧基)-1-(苯基甲基)-E-乙烯基,1-苯甲酰基-2-苯基乙基,1-氧代丁基,2-(2,5-二甲氧基苯基)-2-氧代乙基,2 - 苯基-2-(苯基甲氧基乙基,2-(2,5-二甲氧基 - 苯基)-2-羟乙基,2-萘基甲基,甲氧基羰基 - 丁基,苯甲酰基取代的乙氧基羰基乙基,1-苯甲酰基-1-甲基乙基,1-戊酸, 环丙基甲基,3-苯基-2-丙烯基和3-乙腈;其中R 2选自乙基,正丙基,异丙基,正丁基,仲丁基,异丁基,4-甲基丁基,叔丁基, 戊基,新戊基,1-氰基 乙硫基,丁硫基; 其中R 3至R 11各自为氢,条件是R 5和R 9中的至少一个必须选自COOH,SH,PO 3 H 2,SO 3 H,CONHNH 2,CONHNHSO 2 CF 3,OH,( a),(b)和(c),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。 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
    • 1H-SUBSTITUTED-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS
    • 1H-取代的1,2,4-三唑化合物用于治疗心血管疾病
    • WO1991017148A1
    • 1991-11-14
    • PCT/US1991002926
    • 1991-05-06
    • G.D. SEARLE & CO.REITZ, David, B.
    • G.D. SEARLE & CO.
    • C07D249/08
    • C07D249/08C07D231/12C07D233/56C07D249/10C07D403/10
    • A class of 1H-substituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders, especially cardiovascular disorders. Compounds of interest are angiotensin II antagonists of formula (II), wherein R1 is selected from hydroxy, formyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, n-hexyl, n-heptyl, n-octyl, n-nonyl, carboxyethyl, phenyl, benzyl, phenethyl, cyclopentyl, cyclohexyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, adamantyl, adamantylmethyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, dimethoxymethyl, diethoxymethyl, 1,1-dimethoxypropyl, 1,1-dimethoxybutyl, 1,1-dimethoxypentyl, hydroxypropyl, halo, monofluoromethyl, difluoromethyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, pentafluoroethyl, heptafluoropropyl, phenylacetyl, phenyldifluoroethyl, aminomethyl, aminoethyl, aminopropyl, acetylaminomethyl, t-butoxycarbonylaminoethyl, glutamic acid methyl ester and glutamic acid ethyl ester; wherein R2 is selected from carboxyethyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl and neopentyl; wherein each of R3 through R11 is hydrido with the proviso that at least one of R?5 and R9¿ must be selected from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (III), (IV) and (V), wherein each of R?40 and R41¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.