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1. 发明授权

US5104892A Substituted benzimidazole derivatives possessing Class III antiarrhythmic activity 失效
标题翻译：具有III类抗心律失常活性的取代的苯并咪唑衍生物
公开(公告)号：US5104892A
公开(公告)日：1992-04-14
申请号：US612727
申请日：1990-11-13
申请人： John A. Butera , Jehan F. Bagli , John W. Ellingboe
发明人： John A. Butera , Jehan F. Bagli , John W. Ellingboe
IPC分类号： C07D215/12 , C07D235/14 , C07D241/42 , C07D263/56 , C07D307/81
CPC分类号： C07D263/56 , C07D215/12 , C07D235/14 , C07D241/42 , C07D307/81
摘要： This invention relates to N-heteroalkyl-substituted 1-aryloxy-2-propanolamine and proplyamine derivatives possessing anti-arrhythmic activity, to pharmaceutical compositions and to method for production thereof.
摘要翻译：本发明涉及具有抗心律不齐活性的N-杂烷基取代的1-芳氧基-2-丙醇胺和具有抗心律不齐活性的丙胺衍生物，涉及药物组合物及其生产方法。

2. 发明授权

US5206252A Thiadiazolyl-amino derivatives of benzopyrans and indanes 失效
标题翻译：苯并吡喃和茚满的噻二唑基 - 氨基衍生物
公开(公告)号：US5206252A
公开(公告)日：1993-04-27
申请号：US880433
申请日：1992-05-08
申请人： John A. Butera , Jehan F. Bagli
发明人： John A. Butera , Jehan F. Bagli
IPC分类号： C07D285/10 , C07D417/12
CPC分类号： C07D285/10 , C07D417/12
摘要： The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.2-6 alkoxycarbonyl, nitro, cyano, halogeno, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.2-6 alkanoylamino, C.sub.2-6 perfluoroalkanoylamino, C.sub.1-12 mono- or di-alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-12 arylsulfonyl, carboxyl, C.sub.2-12 mono- or di-alkylcarbamoyl, or hydrogen; a and b together form an --O-- linkage or a direct bond; R.sub.3 and R.sub.4, independent from each other, are C.sub.1-6 alkyl when a and b form an --O-- linkage or, H or C.sub.1-6 alkyl when a and b form a direct bond; either R.sub.5 is hydrogen, hydroxyl, C.sub.2-6 alkanoyloxy, C.sub.7-12 aroyloxy, carbamoyloxy, formyloxy, C.sub.2-6 alkoxycarbonyloxy, mono or di C.sub.2-12 alkylcarbamoyloxy, and R.sub.6 is hydrogen, or R.sub.5 and R.sub.6 together are a bond; R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkanocarbonyl, or C.sub.16 alkanosulfonyl; X is selected from the following: --NR.sub.8 R.sub.9, wherein R.sub.8 and R.sub.9, independent from each other are hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkylcarbonyl, C.sub.7-12 arylalkyl, thienylmethyl, pyridinylmethyl, piperazinylmethyl, or pyrimidinylmethyl, or R.sub.8 and R.sub.9 taken together are polymethylene of 3-10 carbon atoms or R.sub.8 and R.sub.9 taken with the nitrogen atom to which they are attached complete a piperazine, morpholine, pyrroline, pyrrolidinone, imidazole, imidazolone, piperidine or piperidinone ring structure; or --OR.sub.10, wherein R.sub.10 is hydrogen, C.sub.1-6 alkyl or C.sub.2-6 alkylcarbonyl; and n is an integer from 0-2; or a pharmaceutically acceptable salt thereof, are useful antihypertensive, K channel activators.
摘要翻译：下式的化合物，其中R 1和R 2彼此独立地选自如下：C 1-6全氟烷氧基，C 1-6全氟烷基，C 1-6烷基，C 1-6烷氧基，羟基，C 2-6 烷氧基羰基，硝基，氰基，卤代C 1-6烷基磺酰氨基，C 1-6全氟烷基磺酰氨基，氨基，C 2-6烷酰基氨基，C 2-6全氟烷酰基氨基，C 1-12单烷基氨基或二烷基氨基，C 1-6烷基磺酰基，C 6-12芳基磺酰基，羧基，C 2-12单 - 或二 - 烷基氨基甲酰基或氢; a和b一起形成-O-键或直接键; 当a和b形成-O-键时，R 3和R 4彼此独立地为C 1-6烷基，当a和b形成直接键时，R 3和R 4为H或C 1-6烷基; R5是氢，羟基，C2-6烷酰氧基，C7-12芳酰氧基，氨基甲酰氧基，甲酰氧基，C2-6烷氧基羰基氧基，一或二C2-12烷基氨基甲酰氧基，R6是氢，或R5和R6一起是一个键; R7是氢，C1-6烷基，C1-6链烷羰基或C16链烷磺酰基; X选自如下：-NR 8 R 9，其中R 8和R 9彼此独立地是氢，C 1-6烷基，C 2-6烷基羰基，C 7-12芳烷基，噻吩基甲基，吡啶基甲基，哌嗪基甲基或嘧啶基甲基，或R 8和R 9 一起是3-10个碳原子的聚亚甲基或与其所连接的氮原子一起取代的R 8和R 9完全是哌嗪，吗啉，吡咯啉，吡咯烷酮，咪唑，咪唑啉酮，哌啶或哌啶酮环结构; 或-OR 10，其中R 10是氢，C 1-6烷基或C 2-6烷基羰基; n为0-2的整数; 或其药学上可接受的盐是有用的抗高血压K通道激活剂。

3. 发明授权

US5084463A N-quinolinyl alkyl-substituted 1-aryloxy-2-propanolamine and propylamine derivatives possessing class III antiarrhythmic activity 失效
标题翻译：具有Ⅲ类抗心律失常活性的N-喹啉基烷基取代的1-芳氧基-2-丙醇胺和丙胺衍生物
公开(公告)号：US5084463A
公开(公告)日：1992-01-28
申请号：US634678
申请日：1990-12-27
申请人： John A. Butera , Jehan F. Bagli
发明人： John A. Butera , Jehan F. Bagli
IPC分类号： C07D215/12 , C07D235/14 , C07D241/42 , C07D263/56 , C07D307/81
CPC分类号： C07D263/56 , C07D215/12 , C07D235/14 , C07D241/42 , C07D307/81
摘要： This invention relates to N-heteroalkyl-substituted 1-aryloxy-2-propanolamine and propylamine derivatives possessing anti-arrhythmic activity, to pharmaceutical compositions and to methods for production thereof.
摘要翻译：本发明涉及具有抗心律不齐活性的N-杂烷基取代的1-芳氧基-2-丙醇胺和丙胺衍生物，药物组合物及其生产方法。

4. 发明授权

US4994459A Aryloxypropane substituted piperazine derivatives with antiarrhythmic and antifibrillatory activity 失效
标题翻译：丙烯酰氧基丙烷取代的哌嗪衍生物具有抗心律失常和抗纤维化作用
公开(公告)号：US4994459A
公开(公告)日：1991-02-19
申请号：US449273
申请日：1989-12-11
申请人： John A. Butera , Jehan F. Bagli
发明人： John A. Butera , Jehan F. Bagli
IPC分类号： C07D213/74 , C07D239/42
CPC分类号： C07D239/42 , C07D213/74
摘要： This invention relates to certain substituted piperazines possessing anti-arrhythmic activity, to pharmaceutical compositions and to methods for production thereof.
摘要翻译：本发明涉及具有抗心律不齐活性的某些取代的哌嗪，药物组合物及其生产方法。

5. 发明授权

US5254689A Piperdinyl and piperazinyl derivatives 失效
标题翻译：哌嗪基和哌嗪衍生物
公开(公告)号：US5254689A
公开(公告)日：1993-10-19
申请号：US957568
申请日：1992-10-07
申请人： John A. Butera , Jehan F. Bagli , John W. Ellingboe
发明人： John A. Butera , Jehan F. Bagli , John W. Ellingboe
IPC分类号： C07D211/30 , C07D211/44 , C07D249/12 , C07D295/192 , C07D401/12 , C07D401/00 , C07D241/04 , C07D295/00 , C07D403/00
CPC分类号： C07D295/192 , C07D211/30 , C07D211/44 , C07D401/12
摘要： Compounds of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl;Y is ##STR2## --CH.sub.2 --, --O--, --S--, or --SO.sub.2 --; X is --CH.dbd. or --N.dbd.;R.sup.2 is hydrogen when n is 0, otherwise it is hydrogen or --OH;n is one of the integers 0, 1, 2, 3, 4, 5 or 6;A is ##STR3## where R.sup.3 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl; or ##STR4## where R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms; with the provisos that:a) X is --CH.dbd. when Y is ##STR5## --O-- or --S-- and when Y is ##STR6## and R.sup.2 is --OH; b) X is --N.dbd. when A is ##STR7## and c) A is ##STR8## when Y is --S-- or --SO.sub.2 -- and X is --CH.dbd., and their pharmaceutically acceptable salts are Class III antiarrhythmic agents.
摘要翻译：其中R 1是1至6个碳原子的烷基磺酰氨基，6至10个碳原子的芳基磺酰氨基，-NO 2，-CN，1-咪唑基或1,2,4-三唑-1-基的下式的化合物： Y是-CH 2 - ， - O - ， - S-或-SO 2 - ; X是-CH =或-N =; 当n为0时，R2为氢，否则为氢或-OH; n是整数0,1,2,3,4,5或6之一; A是其中R 3是具有1至6个碳原子的烷基磺酰氨基，6至10个碳原子的芳基亚磺酰氨基，-NO 2，-CN，1-咪唑基或1,2,4-三唑-1-基; 或其中R 4是氢或1至6个碳原子的烷基; 条件是：a）X是-CH =当Y是-O - 或-S-时，当Y是＆lt; IMAGE＆gt;且R 2是-OH时; b）X是-N =当A为时，c）当Y为-S-或-SO 2 - 且X为-CH =时，A为，其药学上可接受的盐为III类抗心律失常药。

6. 发明授权

US5202346A Piperidinyl and piperazinyl derivatives 失效
标题翻译：哌啶基和哌嗪衍生物
公开(公告)号：US5202346A
公开(公告)日：1993-04-13
申请号：US841922
申请日：1992-02-25
申请人： John A. Butera , Jehan F. Bagli , John W. Ellingboe
发明人： John A. Butera , Jehan F. Bagli , John W. Ellingboe
IPC分类号： C07D211/30 , C07D211/44 , C07D295/192 , C07D401/12
CPC分类号： C07D295/192 , C07D211/30 , C07D211/44 , C07D401/12
摘要： Compounds of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2,--CN, 1-imidazolyl or 1,2,4-triazol-1-yl;Y is ##STR2## --CH.sub.2 --, --O--, --S--, or --SO.sub.2 --; X is --CH.dbd. or --N.dbd.;R.sup.2 is hydrogen when n is 0, otherwise it is hydrogen or --OH;n is one of the integers 0, 1, 2, 3, 4, 5 or 6;A is ##STR3## where R.sup.3 is alkylsulfonamido of 1 to 6 carbons atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl; or ##STR4## where R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms; with the provisos that;a) X is --CH.dbd. when Y is ##STR5## --O-- or --S-- and when Y is ##STR6## and R.sup.2 is --OH; b) X is --N.dbd. when A is ##STR7## c) A is ##STR8## when Y is --S-- or --SO.sub.2 -- and X is --CH.dbd., and their pharmaceutically acceptable salts are Class III antiarrhythmic agents.
摘要翻译：其中R 1是1至6个碳原子的烷基磺酰氨基，6至10个碳原子的芳基磺酰氨基，-NO 2，-CN，1-咪唑基或1,2,4-三唑-1-基的下式的化合物： Y是-CH 2 - ， - O - ， - S-或-SO 2 - ; X是-CH =或-N =; 当n为0时，R2为氢，否则为氢或-OH; n是整数0,1,2,3,4,5或6之一; A是，其中R3是1至6个碳原子的烷基磺酰氨基，6至10个碳原子的芳基磺酰氨基，-NO 2，-CN，1-咪唑基或1,2,4-三唑-1-基; 或其中R 4是氢或1至6个碳原子的烷基; 但条件是： a）当Y是-O - 或-S-时，X是-CH =，并且当Y是＆lt; IMAGE＆gt;且R 2是-OH时; b）X为-N =当A为时，当Y为-S-或-SO 2 - 且X为-CH =时，A为，其药学上可接受的盐为III类抗心律失常药。

7. 发明授权

US4469694A 2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives 失效
标题翻译： 2-（1-哌嗪基）-2,4,6-环庚三烯-1-酮衍生物
公开(公告)号：US4469694A
公开(公告)日：1984-09-04
申请号：US124164
申请日：1980-02-25
申请人： Jehan F. Bagli , Tibor Bogri , Katherine Voith
发明人： Jehan F. Bagli , Tibor Bogri , Katherine Voith
IPC分类号： C07D209/16 , C07D209/48 , C07D233/54 , C07D233/76 , C07D241/04 , C07D263/14 , C07D295/116 , C07D295/13 , C07D295/15 , C07D295/185 , A61K31/495
CPC分类号： C07D209/48 , C07D209/16 , C07D233/64 , C07D233/76 , C07D241/04 , C07D263/14 , C07D295/116 , C07D295/13 , C07D295/15 , C07D295/185
摘要： 2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
摘要翻译：公开了2-（1-哌嗪基）-2,4,6-环庚三烯-1-酮衍生物，其治疗上可接受的酸加成盐，其制备方法，使用该衍生物的衍生物和药物组合物的方法。衍生物在哺乳动物中表现出多巴胺受体刺激活性，可用于治疗高催乳素血症，溢乳症，闭经，阳ence，帕金森综合征，糖尿病，肢端肥大症，高血压和其他中枢神经系统疾病。

8. 发明授权

US4183955A Troponyl-oxamic acid derivatives for treating allergic conditions 失效
标题翻译：用于治疗过敏症状的丙酰基 - 恶唑酸衍生物
公开(公告)号：US4183955A
公开(公告)日：1980-01-15
申请号：US938558
申请日：1978-08-31
申请人： Jehan F. Bagli , Tibor Bogri
发明人： Jehan F. Bagli , Tibor Bogri
IPC分类号： A61K31/16 , C07C102/00
CPC分类号： C07C243/00
摘要： Tropone derivatives characterized by having a derivative of oxamic acid at positions 2 and or 5 are disclosed. In addition, the tropone nucleus can be optionally further substituted. The foregoing compounds are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of said compounds are disclosed.
摘要翻译：公开了特征在于具有位置2和/或5上的恶唑酸的衍生物的皮质酮衍生物。此外，可以任选进一步取代环丙烯酮核。上述化合物可用于预防或治疗哺乳动物的过敏状况。公开了制备和使用所述化合物的方法。

9. 发明授权

US3987081A Alkyl derivatives of prostanoic acids and preparation thereof 失效
标题翻译：丙酸的烷基衍生物及其制备方法
公开(公告)号：US3987081A
公开(公告)日：1976-10-19
申请号：US567034
申请日：1975-04-10
申请人： Nedumparambil A. Abraham , Jehan F. Bagli , Tibor Bogri
发明人： Nedumparambil A. Abraham , Jehan F. Bagli , Tibor Bogri
IPC分类号： C07C405/00 , C07F9/40 , C07F9/54 , C07C177/00
CPC分类号： C07F9/5407 , C07C405/00 , C07F9/4006
摘要： 15- And/or 16-alkyl derivatives of 9,15-dioxygenated prost-13-enoic, prosta-4,13-dienoic and prosta-5,13-dienoic acid, lower alkyl esters thereof and homologs thereof, as well as a process for preparing these derivatives are disclosed. The compounds possess hypotensive, antihypertensive, bronchospasmolytic, gastric acid secretion inhibiting, abortifacient, estrus synchronizing and ovulation regulating properties. The compounds also inhibit the aggregation of platelets and promote the disaggregation of aggregated platelets. Methods for their use are also disclosed.

10. 发明授权

US5880122A 3-Carboxamide derivatives of 5H-pyrrolo�2,1-c!�1,4!-benzodiazepines 失效
标题翻译： 3,5-吡咯并[2,1-c] [1,4] - 苯并二氮杂卓的3-甲酰胺衍生物
公开(公告)号：US5880122A
公开(公告)日：1999-03-09
申请号：US955511
申请日：1997-10-22
申请人： Eugene J. Trybulski , Albert J. Molinari , Jehan F. Bagli , Mark A. Ashwell , Thomas J. Caggiano
发明人： Eugene J. Trybulski , Albert J. Molinari , Jehan F. Bagli , Mark A. Ashwell , Thomas J. Caggiano
IPC分类号： C07D487/04 , A61K31/55 , C07D487/12
CPC分类号： C07D487/04
摘要： This invention relates to tricyclic non-peptide vasopressin antagonists which are useful in treating conditions where decreased vasopressin levels are desired, such as in congestive heart failure, in disease conditions with excess renal water reabsorption and in conditions with increased vascular resistance and coronary vasoconstriction, the compounds having the general structure: ##STR1##
摘要翻译：本发明涉及三环非肽加压素拮抗剂，其可用于治疗需要血管升压素水平降低的病症，例如充血性心力衰竭，具有过量肾脏水吸收的疾病状况和血管阻力增加和冠状动脉血管收缩增加的病症。具有一般结构的化合物：

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