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11. 发明授权

US4469695A 2-(4-Hydroxyalkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives 失效
标题翻译： 2-（4-羟基烷基-1-哌嗪基）-2,4,6-环庚三烯-1-酮衍生物
公开(公告)号：US4469695A
公开(公告)日：1984-09-04
申请号：US124165
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： C07D209/14 , A61K31/34 , A61K31/343 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/495 , A61P25/00 , A61P25/02 , A61P43/00 , C07D209/16 , C07D209/46 , C07D209/48 , C07D233/54 , C07D233/64 , C07D233/76 , C07D241/04 , C07D263/14 , C07D295/116 , C07D295/13 , C07D295/15 , C07D295/185 , C07D307/93
CPC分类号： C07D209/48 , C07D209/16 , C07D233/64 , C07D233/76 , C07D263/14 , C07D295/116 , C07D295/13 , C07D295/15 , C07D295/185
摘要： 2-(4-Hydroxyalkyl-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-（4-羟基烷基-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。

12. 发明授权

US4161608A 11 Hydroxy methyl 11-deoxyprostaglandin E.sub.1 失效
公开(公告)号：US4161608A
公开(公告)日：1979-07-17
申请号：US872972
申请日：1978-01-27
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 , C07D307/935 , C07D309/12 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12
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.dbd.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.dbd.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-deoxy-prostaglandin derivatives of formula ##STR3## in which (a), (c) and p, are as defined herein, (b) is trans CH.dbd.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.

13. 发明授权

US4089898A 11-Deoxyprostaglandin derivatives 失效
公开(公告)号：US4089898A
公开(公告)日：1978-05-16
申请号：US741077
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 , C07C177/00
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 Witting 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.dbd.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.dbd.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.dbd.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.

14. 发明授权

US4070482A Prostaglandin antagonists 失效
标题翻译：前列腺素拮抗剂
公开(公告)号：US4070482A
公开(公告)日：1978-01-24
申请号：US735929
申请日：1976-10-27
申请人： Wilbur Lippmann , Jehan F. Bagli
发明人： Wilbur Lippmann , Jehan F. Bagli
IPC分类号： A61K31/21 , B01J23/00 , C07B61/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07C405/00 , Y02P20/55 , Y10S514/815 , Y10S514/913 , Y10S514/916 , Y10S514/926 , Y10S514/927
摘要： 2-(1-Hydroxy-2-octynyl)- and 2-(3-hydroxy-1-octynyl)-5-oxocyclopentaneheptanoic acids, their salts and their corresponding lower alkyl esters are disclosed. The compounds inhibit the actions of prostaglandins. Methods for their preparation and use are given.
摘要翻译：公开了2-（1-羟基-2-辛炔基） - 和2-（3-羟基-1-辛炔基）-5-氧代环戊烷庚酸及其盐及其相应的低级烷基酯。这些化合物抑制前列腺素的作用。给出了其制备和使用方法。

15. 发明授权

US4057556A Troponyl-oxamic acid derivatives 失效
标题翻译：丙酰基 - 恶唑酸衍生物
公开(公告)号：US4057556A
公开(公告)日：1977-11-08
申请号：US697296
申请日：1976-06-17
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：公开了特征在于在位置2和/或5具有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。

16. 发明授权

US4054741A Derivatives of prostanoic acid 失效
标题翻译：前列腺酸的衍生物
公开(公告)号：US4054741A
公开(公告)日：1977-10-18
申请号：US697901
申请日：1976-06-21
申请人： Jehan F. Bagli , Tibor Bogri
发明人： Jehan F. Bagli , Tibor Bogri
IPC分类号： C07C57/52 , C07C59/42 , C07C405/00 , C07D317/72 , C07C177/00
CPC分类号： C07D317/72 , C07C405/00 , C07C57/52 , C07C59/42
摘要： Process for preparing prostanoic acid derivatives, in particular derivatives of 9,15-dioxygenated prostanoic acid and prost-13-enoic acid, related additionally unsaturated derivatives, homologs thereof and intermediates therefor, in which a lower alkyl ester of 2-(.omega.-carboxy-Y)cyclopent-2-en-1-one in which Y is CH.sub.2 --(a)--(CH.sub.2).sub.m wherein (a) is CH.sub.2 CH.sub.2, CH.dbd.CH or C.tbd.C and m is an integer from 2 - 4 is treated with nitromethane to yield 2-(.omega.-carboxy-Y)-3-nitromethyl-cyclopentan-1-one and the latter compound or its corresponding 1-hydroxy analog are converted to the corresponding aldehyde, 2-(.omega.-carboxy-Y)cyclopentan-1-on-3-al or 1-hydroxy-2-(.omega.-carboxy-Y)cyclopentan-3-al, respectively. Treatment of the aldehyde with the ylid prepared from the appropriate Wittig reagent, preferably a dimethyl 2-oxoalkylphosphonate of the formula (AlkO).sub.2 P(O)CH.sub.2 CO(CH.sub.2).sub.n CH.sub.3 in which n is an integer of from 1-6 and Alk is an alkyl containing from 1 - 3 carbon atoms yields the corresponding derivatives of 2-(.omega.-carboxy-Y)-3-(3-oxoalk-1-enyl)cyclopentan-1-one or -1-o1 in which the oxygen functions may be selectively protected and transformed by conventional means, and in which the unsaturated bonds may be reduced to a single bond. The prostanoic acid derivatives possess prostaglandin like biological activities. Methods for their use are also disclosed.
摘要翻译：制备前列腺酸衍生物，特别是9,15-双加氧的前列腺酸和前列腺-13-烯酸的衍生物的方法，其它不饱和衍生物，其同系物及其中间体，其中2-（ω-羧基 -Y）环戊-2-烯-1-酮，其中Y是CH 2 - （a） - （CH 2）m，其中（a）是CH 2 CH 2，CH = CH或C 3 D C，m是2-4的整数用硝基甲烷处理，得到2-（ω-羧基-Y）-3-硝基甲基 - 环戊烷-1-酮，将后一种化合物或其相应的1-羟基类似物转化为相应的醛，2-（ω-羧基-Y ）环戊烷-1-对 - 3-或1-羟基-2-（ω-羧基-Y）环戊烷-3-基。用合适的Wittig试剂，优选式（AlkO）2P（O）CH 2 CO（CH 2）n CH 3的二甲基-2-氧代烷基膦酸酯制备的内酰胺处理醛，其中n为1-6的整数，Alk为含有1-3个碳原子的烷基产生相应的2-（ω-羧基-Y）-3-（3-氧代链烯-1-基）环戊烷-1-酮或-1-o1的衍生物，其中氧官能团可以通过常规方法选择性地保护和转化，并且其中不饱和键可以还原成单键。前列腺酸衍生物具有前列腺素样生物活性。还公开了它们的使用方法。

17. 发明授权

US4004027A Prostaglandin antagonists 失效
标题翻译：前列腺素拮抗剂
公开(公告)号：US4004027A
公开(公告)日：1977-01-18
申请号：US545664
申请日：1975-01-28
申请人： Wilbur Lippmann , Jehan F. Bagli
发明人： Wilbur Lippmann , Jehan F. Bagli
IPC分类号： A61K31/21 , B01J23/00 , C07B61/00 , C07C67/00 , C07C401/00 , C07C405/00 , A61K31/215 , A61K31/19
CPC分类号： C07C405/00 , Y02P20/55 , Y10S514/815 , Y10S514/913 , Y10S514/916 , Y10S514/926 , Y10S514/927
摘要： 2-(1-Hydroxy-2-octynyl)- and 2-(3-hydroxy-1-octynyl)-5-oxocyclopentaneheptanoic acids, their salts and their corresponding lower alkyl esters are disclosed. The compounds inhibit the actions of prostaglandins. Methods for their preparation and use are given.
摘要翻译：公开了2-（1-羟基-2-辛炔基） - 和2-（3-羟基-1-辛炔基）-5-氧代环戊烷庚酸及其盐及其相应的低级烷基酯。这些化合物抑制前列腺素的作用。给出了其制备和使用方法。

18. 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。

19. 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。

20. 发明授权

US4906753A Preparation of 2,6-disubstituted-5-cyano-4-pyrimidinyloxyacetic acid aldose reductase inhibitors 失效
标题翻译： 2,6-二取代-5-氰基-4-嘧啶氧基乙酸醛糖还原酶抑制剂的制备
公开(公告)号：US4906753A
公开(公告)日：1990-03-06
申请号：US221586
申请日：1988-07-20
申请人： Jehan F. Bagli , John W. Ellingboe , Thomas R. Alessi
发明人： Jehan F. Bagli , John W. Ellingboe , Thomas R. Alessi
IPC分类号： C07D239/56
CPC分类号： C07D239/56
摘要： Disclosed herein are 2,6-disubstituted-5-cyano-4-pyrimidinyloxyacetic acids and pharmaceutically acceptable salts thereof and methods of their preparation. The compounds are new aldose reductase inhibitors useful for the treatment of prevention of diabetic complications.
摘要翻译：本文公开了2,6-二取代-5-氰基-4-嘧啶氧基乙酸及其药学上可接受的盐及其制备方法。该化合物是用于治疗预防糖尿病并发症的新的醛糖还原酶抑制剂。

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