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21. 发明授权

US4923874A Use of 8-azapurin-6-one derivatives for control of hypertension 失效
标题翻译：使用8-氮杂青霉素-6-酮衍生物来控制高血压
公开(公告)号：US4923874A
公开(公告)日：1990-05-08
申请号：US222680
申请日：1988-07-21
申请人： Ellen G. McMahon , Robert E. Manning
发明人： Ellen G. McMahon , Robert E. Manning
IPC分类号： A61K31/505 , A61K31/52
CPC分类号： A61K31/505 , A61K31/52
摘要： A class of 8-azapurin-6-one derivatives is described for use in control of hypertension. A compound of particular interest is 8-aza-2-(2-n-propoxyphenyl)purin-6-one.
摘要翻译：描述了一类用于控制高血压的8-氮杂青霉素-6-酮衍生物。特别令人感兴趣的化合物是8-氮杂-2-（2-正丙氧基苯基）嘌呤-6-酮。

22. 发明授权

US4054665A 2-Amino-5-(trifluoromethylphenylalkyl)-1,3,4 thiadiazoles used in the treatment of insomnia and anxiety 失效
标题翻译：用于治疗失眠和焦虑的2-氨基-5-（三氟甲基苯基烷基）-1,3,4噻二唑
公开(公告)号：US4054665A
公开(公告)日：1977-10-18
申请号：US665776
申请日：1976-03-10
申请人： Marcel K. Eberle , Robert E. Manning
发明人： Marcel K. Eberle , Robert E. Manning
IPC分类号： C07D285/12 , C07D285/135 , A61K31/425
CPC分类号： C07D285/135 , Y10S514/923
摘要： 2-amino-5-(substituted or unsubstituted phenylalkyl)-1,3,4-thiadiazoles, e.g., 2-amino-5-(3-trifluoromethylbenzyl)-1,3,4-thiadiazole, prepared, e.g., by ring closure, of corresponding 1-(substituted or unsubstituted phenylalkanoyl)-thiosemicarbazide in a strong acid medium. The compounds are useful as minor tranquilizers and sleep inducers.
摘要翻译： 2-氨基-5-（取代或未取代的苯基烷基）-1,3,4-噻二唑，例如2-氨基-5-（3-三氟甲基苄基）-1,3,4-噻二唑，例如通过闭环，在强酸介质中相应的1-（取代或未取代的苯基烷酰基） - 硫代氨基脲。这些化合物可用作微量镇静剂和睡眠诱导剂。

23. 发明授权

US3974283A N-substituted-4-T-butyl-1-pyridinethiocarboxamides and their use for treatment of inflammation or pain 失效
标题翻译： N-取代-4-叔丁基-1-吡啶乙酰胺及其用于治疗炎症或疼痛的用途
公开(公告)号：US3974283A
公开(公告)日：1976-08-10
申请号：US588249
申请日：1975-06-19
申请人： Robert E. Manning
发明人： Robert E. Manning
IPC分类号： C07D211/70 , A01N9/22 , C07D213/83
CPC分类号： C07D211/70
摘要： N-substituted-4-t-butyl-1-pyridinethiocarboxamides, e.g. N-methyl-4-t-1,2,3,6-tetrahydro-1-pyridinethiocarboxamides, are prepared by treating 4-t-butyl-1,2,3,6-tetrahydropyridine with a substituted isothiocyanate and are useful as anti-inflammatory and non-narcotic analgesic agents.
摘要翻译： N-取代-4-叔丁基-1-吡啶乙酰胺，例如 N-甲基-4-叔-1,2,3,6-四氢-1-吡啶乙酰胺通过用取代的异硫氰酸酯处理4-叔丁基-1,2,3,6-四氢吡啶并用作抗炎性和非麻醉止痛剂。

24. 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。

25. 发明授权

US5643906A Method of using N-arylheteroarylalkyl imidazol-2-one compounds for treatment of a glaucoma disorder 失效
标题翻译：使用N-芳基杂芳基烷基咪唑-2-酮化合物治疗青光眼病症的方法
公开(公告)号：US5643906A
公开(公告)日：1997-07-01
申请号：US86959
申请日：1993-07-01
申请人： David B. Reitz , Robert E. Manning
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A61K31/4439 , C07D401/06 , C07D401/10 , C07D401/14 , A61K31/535 , A61K31/445 , A61K31/505 , A61K31/411
CPC分类号： C07D401/06 , A61K31/4439 , C07D401/10 , C07D401/14
摘要： A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of a glaucoma disorder. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein R.sup.1 is selected from hydrido and alkyl; wherein each of R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrido, alkyl, alkoxy, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; wherein R.sup.5 is hydrido; wherein R.sup.6 is alkyl; wherein R.sup.7 is an acidic group selected from COOH and ##STR3## or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗青光眼病症的N-芳基杂芳基烷基咪唑-2-酮化合物。特别感兴趣的化合物是下式的血管紧张素II拮抗剂：其中A选自水合和烷基;其中A选自氢化和烷基; 其中R2，R3和R4各自独立地选自氢，烷基，烷氧基，卤素，羟基，羧基，烷氧基羰基，甲酰基和乙酰基; 其中R5是氢的; 其中R6是烷基; 其中R7是选自COOH和/或其立体异构体或互变异构体或其药学上可接受的盐的酸性基团。

26. 发明授权

US5612355A Phenyl amidine lactones useful as platelet aggregation inhibitors 失效
标题翻译：可用作血小板聚集抑制剂的苯基脒内酯
公开(公告)号：US5612355A
公开(公告)日：1997-03-18
申请号：US451815
申请日：1995-05-26
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 , C07D405/06 , A61K31/44
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：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。

27. 发明授权

US5451592A Method of using N-arylheteroarylalkyl 1-heteroaryl-imidazol-2-one compounds for treatment of a glaucoma disorder 失效
标题翻译：使用N-芳基杂芳基烷基1-杂芳基 - 咪唑-2-酮化合物治疗青光眼病症的方法
公开(公告)号：US5451592A
公开(公告)日：1995-09-19
申请号：US960603
申请日：1992-10-13
申请人： David B. Reitz , Robert E. Manning
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A61K31/4439 , C07D401/06 , C07D401/10 , C07D401/14 , A61K31/44
CPC分类号： C07D401/06 , A61K31/4439 , C07D401/10 , C07D401/14
摘要： A class of N-arylheteroarylalkyl 1-heteroaryl-imidazol-2-one compounds is described for use in treatment of glaucoma disorder. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein R.sup.1 is selected from hydrido and alkyl; wherein each of R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrido, alkyl, alkoxy, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; wherein R.sup.5 is hydrido; wherein R.sup.6 is alkyl; wherein R.sup.7 is an acidic group selected from COOH and ##STR3## or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗青光眼病症的N-芳基杂芳基烷基-1-杂芳基 - 咪唑-2-酮化合物。特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中A选自下列化合物：其中R 1选自氢和烷基; 其中R2，R3和R4各自独立地选自氢，烷基，烷氧基，卤素，羟基，羧基，烷氧基羰基，甲酰基和乙酰基; 其中R5是氢的; 其中R6是烷基; 其中R7是选自COOH和/或其立体异构体或互变异构体或其药学上可接受的盐的酸性基团。

28. 发明授权

US5416084A Benzo-fused thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的苯并稠合的硫代吗啉基封端的烷基氨基乙炔基丙氨酸氨基二醇化合物
公开(公告)号：US5416084A
公开(公告)日：1995-05-16
申请号：US198412
申请日：1994-02-22
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： C07D295/12 , A61K31/395 , A61K31/425 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D265/06 , C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13 , C07D498/08 , C07D279/16
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as benzo-fused thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused thiomorpholinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.ident.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常以苯并稠合的硫代吗啉基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物表征的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是式IO 2的化合物; 其中X选自氧原子和亚甲基; 其中B是苯并稠合的硫代吗啉基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自 - （CH 2）q -C = C-V，其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

29. 发明授权

US5409945A Benzyo-fused thiazolidinyl terminated alkylamino ethylnyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：苯偶姻稠合噻唑烷基封端的烷基氨基乙基丙氨酸二氨基二醇化合物治疗高血压
公开(公告)号：US5409945A
公开(公告)日：1995-04-25
申请号：US198425
申请日：1994-02-22
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： C07D295/12 , A61K31/395 , A61K31/425 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D265/06 , C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13 , C07D498/08 , C07D277/62 , C07D277/64
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as benzo-fused thiazolidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused thiazolidinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常被称为苯并稠合噻唑烷基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是式I的化合物（I）其中A选自CO和SO 2; 其中X选自氧原子和亚甲基; 其中B是苯并稠合噻唑烷基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自 - （CH 2）q -C 3 CON C-V，其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

30. 发明授权

US5409924A Benzo-fused oxazobicyclo terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的苯并稠合的恶唑二环端基烷基氨基乙炔基丙氨酸氨基二醇化合物
公开(公告)号：US5409924A
公开(公告)日：1995-04-25
申请号：US198419
申请日：1994-02-22
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： C07D295/12 , A61K31/395 , A61K31/425 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D265/06 , C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13 , C07D498/08 , C07D265/34
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as benzo-fused oxazobicyclo-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused oxazobicyclo group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常被称为苯并稠合的恶唑二环端基的烷基氨基乙炔基丙氨酸氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是式I的化合物（I）其中A选自CO和SO 2; 其中X选自氧原子和亚甲基; 其中B是苯并稠合的恶唑二环基团; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

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