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21. 发明授权

US4333937A 2-(Piperazinyl)-4-pyrimioinamines 失效
标题翻译： 2-（哌嗪基）-4-嘧啶胺
公开(公告)号：US4333937A
公开(公告)日：1982-06-08
申请号：US141548
申请日：1980-04-18
申请人： Sumanas Rakhit , Jehan F. Bagli
发明人： Sumanas Rakhit , Jehan F. Bagli
IPC分类号： C07D239/00 , A61K45/06 , C07D235/00 , C07D239/48 , C07D239/95 , C07D263/00 , C07D277/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D498/00 , C07D498/04 , A61K31/505
CPC分类号： C07D239/48 , A61K45/06 , C07D239/95
摘要： Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of optionally substituted 2-cycloheptimidazolyl, 1,4,5,6,7,8-hexahydrocycloheptimidazol-2-yl, 2-benzoxazolyl, benzthiazol-2-yl, 1H-2-benzimidazolyl and 1-oxo-2,4,6-cycloheptarien-2-yl. The derivatives are useful for treating hypertension in a mammal.
摘要翻译：本文公开了2-（1-哌嗪基）-4-嘧啶胺衍生物，其酸加成盐，其制备方法，使用衍生物的衍生物和药物组合物的方法。通过在哌嗪基的4位具有新的取代基，最容易区分衍生物，该取代基选自任选取代的2-环庚基咪唑基，1,4,5,6,7,8-六氢环庚基咪唑-2-基，2-苯并恶唑基，苯并噻唑-2-基，1H-2-苯并咪唑基和1-氧代-2,4,6-环庚三烯-2-基。该衍生物可用于治疗哺乳动物的高血压。

22. 发明授权

US4152457A Tropone derivatives 失效
公开(公告)号：US4152457A
公开(公告)日：1979-05-01
申请号：US840938
申请日：1977-10-11
申请人： Jehan F. Bagli , Tibor Bogri
发明人： Jehan F. Bagli , Tibor Bogri
IPC分类号： A61K31/215 , A61K31/265 , C07C55/06 , C07C69/74 , C07C317/00 , C07C317/08 , C07C317/14 , C07C327/22 , C07C147/04 , C07C147/14
CPC分类号： C07C323/22 , C07C317/00 , C07C327/00 , C07C2101/18
摘要： Tropone derivatives substituted with an amino-, thio- or oxy-derivative of oxalic acid or acetic acid 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 the compounds are disclosed.

23. 发明授权

US4130649A Cyclohepta [B]pyridine-2-carboxylic acid derivatives 失效
标题翻译：环庚烯{8 B {9吡啶-2-羧酸衍生物
公开(公告)号：US4130649A
公开(公告)日：1978-12-19
申请号：US789397
申请日：1977-04-21
申请人： Jehan F. Bagli , Tibor Bogri
发明人： Jehan F. Bagli , Tibor Bogri
IPC分类号： C07D221/04 , C07D491/04 , A61K31/455
CPC分类号： C07D221/04 , C07D491/04
摘要： Cyclohepta[b]pyridine-2-carboxylic acid derivatives characterized by having a 4,7-dihydro-4,7-dioxo-1H-cyclohepta-[b]pyridine nucleus substituted at position 2 with a carboxylic acid or carboxylic acid ester are disclosed. In addition, the nucleus can be optionally further substituted at positions 1, 5,6 and 8. The foregoing compounds are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of the compounds are disclosed.
摘要翻译：公开了具有在2位被羧酸或羧酸酯取代的4,7-二氢-4,7-二氧代-1H-环庚氨基 - [b]吡啶核的环庚基[b]吡啶-2-羧酸衍生物。此外，核可任选地在1,5,6和8位进一步被取代。前述化合物可用于预防或治疗哺乳动物的过敏状况。公开了制备和使用化合物的方法。

24. 发明授权

US4125625A Troponyl-oxamic acid derivatives 失效
标题翻译：丙酰基 - 恶唑酸衍生物
公开(公告)号：US4125625A
公开(公告)日：1978-11-14
申请号：US801488
申请日：1977-05-31
申请人： Jehan F. Bagli , Tibor Bogri
发明人： Jehan F. Bagli , Tibor Bogri
IPC分类号： A61K31/16 , A61K31/12 , A61K31/135 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/225 , A61K31/325 , A61P37/08 , C07C62/38 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/00 , C07C233/32 , C07C233/56 , C07C241/00 , C07C243/28 , C07C311/49 , C07C313/00 , C07C323/62 , C07C103/42
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。

25. 发明授权

US4092427A Method of inducing abortion using alkyl derivatives of prostanoic acids 失效
标题翻译：使用前列腺酸的烷基衍生物诱导流产的方法
公开(公告)号：US4092427A
公开(公告)日：1978-05-30
申请号：US696245
申请日：1976-06-15
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 , A61K31/19 , A61K31/215
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, anti-hypertensive, 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.
摘要翻译： 9,15-双加氧前列腺-13-烯酸，前列腺-4,13-二烯酸和前列腺-5,13-二烯酸的15-和/或16-烷基衍生物，其低级烷基酯及其同系物，以及公开了制备这些衍生物的方法。该化合物具有降血压，抗高血压，支气管痉挛，胃酸分泌抑制，流产，发情同步和排卵调节特性。该化合物还抑制血小板的聚集并促进聚集的血小板的解聚。还公开了它们的使用方法。

26. 发明授权

US4048329A Alkyl derivatives of 4,5-dehydro PGE.sub.1 失效
标题翻译： 4,5-脱氢PGE的烷基衍生物{HD 1
公开(公告)号：US4048329A
公开(公告)日：1977-09-13
申请号：US696328
申请日：1976-06-15
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 , A61K31/19 , A61K31/215
CPC分类号： C07F9/4006 , C07C405/00 , C07F9/5407
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 possses 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.
摘要翻译： 9,15-双加氧前列腺-13-烯酸，前列腺-4,13-二烯酸和前列腺-5,13-二烯酸的15-和/或16-烷基衍生物，其低级烷基酯及其同系物，以及公开了制备这些衍生物的方法。化合物降血压，抗高血压，支气管痉挛，胃酸分泌抑制，流产，发情同步和排卵调节性质。该化合物还抑制血小板的聚集并促进聚集的血小板的解聚。还公开了它们的使用方法。

27. 发明授权

US4036856A Cyclopentanone derivatives 失效
公开(公告)号：US4036856A
公开(公告)日：1977-07-19
申请号：US741096
申请日：1976-11-11
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 , C07D307/88
CPC分类号： C07C405/00
摘要： A process for preparing 11-deoxyprostaglandin E.sub.1, E.sub.2 and E.sub.3 and analogs thereof is realized by treating an appropriate di(lower)alkyl 3-(optionally substituted)-2-formylcyclopropane-1,1-dicarboxylate with an ylid prepared from a Wittig reagent of formula (AlkO).sub.2 POCH.sub.2 CO-(c)-CH.sub.3 in which Alk is an alkyl containing one to three carbon atoms and (c) is either (CH.sub.2).sub.q wherein q is an integer from 1 to 6 or cis CH.sub.2 CH=CH(CH.sub.2).sub.r wherein r is an integer from 0 to 3 to obtain the corresponding compound of formula: ##STR1## in which R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl, R.sup.4 is lower alkyl and (c) is as defined herein. The latter compound is reduced with an alkali metal borohydride to yield the corresponding alcohol derivative. Condensation of this alcohol derivative or preferably its corresponding tetrahydropyran-2-yl ether derivative with a triester of formula CH(COOR.sup.6).sub.2 --(a)-(CH.sub.2)pCOOR in which R and R.sup.6 are lower alkyl, (a) is CH.sub.2 CH.sub.2, cis CH=CH or C.tbd.C and p is an integer from 2 to 4, gives the corresponding cyclopentanonetriester of formula ##STR2## in which (a), (c), p, R, R.sup.4 and R.sup.6 are as defined herein, R.sup.5 is hydrogen or tetrahydropyran-2-yl, respectively, and R.sup.7 is hydrogen or lower alkyl; the lactonized form of the cyclopentanonetriester being obtained from said alcohol derivative in which R.sup.2 is CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl. In the instance when R.sup.5 is tetrahydropyran-2-yl the cyclopentanonetriester is treated with an acid to give the corresponding compound in which R.sup.5 is hydrogen. The instant compound is then treated with a base under aqueous conditions, followed by optional esterification and acylation to give the desired 11-deoxyprostaglandin derivatives of formula ##STR3## in which (a), (c) and p, are as defined herein, (b) is trans CH=CH, R is hydrogen or lower alkyl, R.sup.1 is hydrogen or lower alkanoyl and R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is hydrogen or lower alkanoyl. The derivatives possess prostaglandin-like biological activity and methods for their use are given.

28. 发明授权

US4006136A Prostaglandin intermediates 失效
公开(公告)号：US4006136A
公开(公告)日：1977-02-01
申请号：US489856
申请日：1974-07-19
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： C07C45/67 , C07C49/20 , C07C49/203 , C07C405/00 , C07C69/74
CPC分类号： C07C405/00 , C07C45/673 , C07C49/20 , C07C49/203
摘要： A process for preparing 11-deoxyprostaglandin E.sub.1, E.sub.2 and E.sub.3 and analogs thereof is realized by treating an appropriate di(lower)alkyl 3-(optionally substituted)-2-formylcyclopropane-1,1-dicarboxylate with an ylid prepared from a Wittig reagent of formula (AlkO).sub.2 PCCH.sub.2 CO-(c)-CH.sub.3 in which Alk is an alkyl containing one to three carbon atoms and (c) is either (CH.sub.2).sub.q wherein q is an integer from 1 to 6 or cis CH.sub.2 CH=CH(CH.sub.2).sub.r wherein r is an integer from 0 to 3 to obtain the corresponding compound of formula: ##STR1## in which R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl, R.sup.4 is lower alkyl and (c) is as defined herein. The latter compound is reduced with an alkali metal borehydride to yield the corresponding alcohol derivative. Condensation of this alcohol derivative or preferably its corresponding tetrahydropyran-2-yl ether derivative with a triester of formula CH(COOR.sup.6).sub.2 -(a)-(CH.sub.2)pCOOR in which R and R.sup.6 are lower alkyl, (a) is CH.sub.2 CH.sub.2, cis CH=CH or CaC and p is an integer from 2 to 4, gives the corresponding cyclopentanonetriester of formula ##STR2## in which (a), (c), p, R, R.sup.4 and R.sup.6 are as defined herein, R.sup.5 is hydrogen or tetrahydropyran-2-yl, respectively, and R.sup.7 is hydrogen or lower alkyl; the lactonized form of the cyclopentanone-triester being obtained from said alcohol derivative in which R.sup.2 is CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl. In the instance when R.sup.5 is tetrahydropyran-2-yl the cyclopentanonetriester is treated with an acid to give the corresponding compound in which R.sup.5 is hydrogen. The instant compound is then treated with a base under aqueous conditions, followed by optional esterification and acylation to give the desired 11-deoxy-prostaglandin derivatives of the formula ##STR3## in which (a), (c) and p, are as defined herein, (b) is trans CH=CH, R is hydrogen or lower alkyl, R.sup.1 is hydrogen or lower alkanoyl and R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is hydrogen or lower alkanoyl. The derivatives possess prostaglandin-like biological activity and methods for their use are given.

29. 发明授权

US06511974B1 Tricyclic vasopressin agonists 失效
标题翻译：三环加压素激动剂
公开(公告)号：US06511974B1
公开(公告)日：2003-01-28
申请号：US09122020
申请日：1998-07-24
申请人： John P. Dusza , Peter S. Chan , Jay D. Albright , Jehan F. Bagli , Amedeo A. Failli , Mark A. Ashwell , Albert J. Molinari , Thomas J. Caggiano , Eugene J. Trybulski
发明人： John P. Dusza , Peter S. Chan , Jay D. Albright , Jehan F. Bagli , Amedeo A. Failli , Mark A. Ashwell , Albert J. Molinari , Thomas J. Caggiano , Eugene J. Trybulski
IPC分类号： A61K3155
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D487/04
摘要： This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.
摘要翻译：本发明涉及选自通式（I）的化合物或其药学上可接受的盐，酯或前体药物形式的新化合物：其中D，E和G是N或CH，其用作加压素激动剂并且可用于治疗疾病如尿崩症，夜间遗尿，夜尿症，尿失禁，出血和凝血障碍，以及不能暂时延迟排尿及其药物组合物和方法。

30. 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。

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