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1. 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。

2. 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。

3. 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.

4. 发明授权

US4375470A 2(1-Piperazinyl)-cycloheptimidazole antihypertensive composition and methods 失效
标题翻译： 2（1-哌嗪基） - 环庚咪唑抗高血压组合物及方法
公开(公告)号：US4375470A
公开(公告)日：1983-03-01
申请号：US198024
申请日：1980-10-17
申请人： Jehan F. Bagli , Tibor Bogri
发明人： Jehan F. Bagli , Tibor Bogri
IPC分类号： C07D235/02 , C07D307/24 , A61K31/495 , C07D401/14 , C07D403/04
CPC分类号： C07D235/02 , C07D307/24
摘要： 2-(1-Piperazinyl)-cycloheptimidazole derivatives are disclosed. The foregoing compounds are useful antihypertensive agents.
摘要翻译：公开了2-（1-哌嗪基） - 环庚咪唑衍生物。上述化合物是有用的抗高血压药。

5. 发明授权

US4152456A Tropone derivatives 失效
标题翻译：铁磁粉衍生物
公开(公告)号：US4152456A
公开(公告)日：1979-05-01
申请号：US840465
申请日：1977-10-07
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 , C07C61/38
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.
摘要翻译：公开了由草酸或乙酸的氨基，硫代或氧代衍生物取代的酮基衍生物。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。公开了制备和使用化合物的方法。

6. 发明授权

US4048328A Alkyl derivatives of 4,5-dehydro PGF.sub.1 失效
标题翻译： 4,5-脱氢PGF的烷基衍生物（HD 1
公开(公告)号：US4048328A
公开(公告)日：1977-09-13
申请号：US696453
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 , C07C177/00
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 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。

7. 发明授权

US4007171A Intermediates for prostanoic acids 失效
标题翻译：前列腺酸中间体
公开(公告)号：US4007171A
公开(公告)日：1977-02-08
申请号：US567036
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 , C07C69/74
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.
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。该化合物具有低血压，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。

8. 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。

9. 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.

10. 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.

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