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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

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：

5. 发明授权

US5149700A Substituted arylsulfonamides and benzamides 失效
标题翻译：取代的芳基磺酰胺和苯甲酰胺
公开(公告)号：US5149700A
公开(公告)日：1992-09-22
申请号：US785136
申请日：1991-10-30
申请人： John W. Ellingboe , Jehan F. Bagli , Michael W. Winkley
发明人： John W. Ellingboe , Jehan F. Bagli , Michael W. Winkley
IPC分类号： C07D209/40 , C07D213/74 , C07D213/76 , C07D215/38 , C07D235/14 , C07D235/30 , C07D239/42 , C07D239/48 , C07D239/84 , C07D487/04 , C07D521/00
CPC分类号： C07D213/74 , C07D209/40 , C07D213/76 , C07D215/38 , C07D231/12 , C07D233/56 , C07D235/14 , C07D235/30 , C07D239/42 , C07D239/48 , C07D239/84 , C07D249/08 , C07D487/04
摘要： This invention relates to substituted arylsulfonamides and benzamides possessing aniarrhythmic activity, to pharmaceutical compositions and to methods for production thereof.
摘要翻译：本发明涉及具有非心律失常活性的取代芳基磺酰胺和苯甲酰胺，药物组合物及其生产方法。

6. 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。

7. 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。

8. 发明授权

US4786638A 2,4-disubstituted-5-cyano-1,6-dihydro-6-oxo-1-pyrimidineacetic acid aldose reductase inhibitors 失效
标题翻译： 2,4-二取代-5-氰基-1,6-二氢-6-氧代-1-嘧啶乙酸醛糖还原酶抑制剂
公开(公告)号：US4786638A
公开(公告)日：1988-11-22
申请号：US61831
申请日：1987-06-12
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： C07D239/36 , C07D239/46 , C07D239/56 , C07D401/12 , A61K31/495 , A61K31/505 , C07D401/04 , C07D403/04
CPC分类号： C07D239/36 , C07D239/47 , C07D239/56 , C07D401/12
摘要： Disclosed herein are 2,4-disubstituted-5-cyano-1,6-dihydro-6-oxo-1-pyrimidineacetic acids and pharmaceutically acceptable salts thereof and methods of their preparation. The compounds are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
摘要翻译：本文公开了2,4-二取代-5-氰基-1,6-二氢-6-氧代-1-嘧啶乙酸及其药学上可接受的盐及其制备方法。该化合物是可用于治疗或预防糖尿病并发症的新型醛糖还原酶抑制剂。

9. 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。

10. 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.

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