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1. 发明授权

US4328221A Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof 失效
标题翻译：取代的类固醇 - 螺恶唑烷酮衍生物及其制备方法
公开(公告)号：US4328221A
公开(公告)日：1982-05-04
申请号：US220139
申请日：1980-12-24
申请人： Katalin Szilagyi nee Farago , Sandor Solyom , Lajos Toldy , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Katalin Szilagyi nee Farago , Sandor Solyom , Lajos Toldy , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： A61K31/58 , A61P7/10 , A61P9/12 , C07J43/00
CPC分类号： C07J43/006
摘要： Compounds of the formula (I) having aldosterone-antagonizing activity are disclosed ##STR1## wherein R.sub.3 and R.sub.4 are each C.sub.1 to C.sub.3 alkyl; andZ is one of the following groups ##STR2## wherein R.sub.1 is hydrogen or methyl;R.sub.6 is hydrogen, C.sub.1 to C.sub.3 alkylthio or C.sub.2 to C.sub.4 acylthio; andX is oxo, hydroximino, C.sub.1 to C.sub.3 alkoxyimino, carboxy-alkoxyimino wherein the alkoxy has 2 to 4 carbon atoms or a salt-converted carboxy-alkoxy-imino wherein the alkoxy has 2 to 4 carbon atoms.
摘要翻译：公开了具有醛固酮拮抗活性的式（I）化合物，其中R 3和R 4各自为C 1至C 3烷基; （a）其中R1是氢或甲基;（e）其中R1是氢或甲基;和（c） R6是氢，C1-C3烷硫基或C2-C4酰硫基; 并且X是氧代，肟基，C 1至C 3烷氧基亚氨基，其中烷氧基具有2至4个碳原子的羧基 - 烷氧基亚氨基或其中烷氧基具有2至4个碳原子的盐转化的羧基 - 烷氧基亚氨基。

2. 发明授权

US4218446A Substituted steroid-spiro-oxazolidinone derivatives and a process for the preparation thereof 失效
标题翻译：取代的类固醇 - 螺恶唑烷酮衍生物及其制备方法
公开(公告)号：US4218446A
公开(公告)日：1980-08-19
申请号：US25080
申请日：1979-03-29
申请人： Sandor Solyom , Lajos Toldy , Katalin Szilagyi nee Farago , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Sandor Solyom , Lajos Toldy , Katalin Szilagyi nee Farago , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： C07J31/00 , A61K31/58 , A61P5/38 , C07J43/00
CPC分类号： C07J43/006 , Y10S514/869
摘要： Diuretic pharmaceutically active steroid-spiro-oxazolidinone compounds of the formula (I), ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is C.sub.1-4 alkyl,R.sup.3 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl,Z.sup.1 and Z.sup.2 each are hydrogen or together form a second valence bond, or Z.sup.1 is hydrogen and Z.sup.2 is R.sup.4 --S--,Z.sup.3 and Z.sup.4 each are hydrogen or together form a second valence bond, or Z.sup.3 is hydrogen and Z.sup.4 is R.sup.4 --S--, with at least one of the pairs Z.sup.1 -Z.sup.2 and Z.sup.3 -Z.sup.4 representing hydrogen and an R.sup.4 --S-- group, andR.sup.4 is hydrogen or alkyl, alkenyl, aralkyl or acyl with up to 7 carbon atoms, provided that when Z.sup.1 and Z.sup.2 together form a valence bond, or Z.sup.1 represents a hydrogen atom and Z.sup.2 and R.sup.4 --S-- group then R.sup.1 is methyl.
摘要翻译：式（I）的利尿药物活性类固醇 - 螺恶唑烷酮化合物，其中R 1是氢或甲基，R 2是C 1-4烷基，R 3是氢，C 1-4烷基或C 2-4链烯基， Z1和Z2各自为氢或一起形成第二价键，或Z1为氢，Z2为R4-S-，Z3和Z4各自为氢或一起形成第二价键，或Z3为氢，Z4为R4-S - ，其中至少一对Z1-Z2和Z3-Z4代表氢和R4-S-基团，R4是氢或具有至多7个碳原子的烷基，烯基，芳烷基或酰基，条件是当Z1和 Z2一起形成价键，或Z1表示氢原子，Z2和R4-S-基团，则R1为甲基。

3. 发明授权

US4342754A Steroid-spiro-oxathiazolidine derivatives and a process for the preparation thereof 失效
标题翻译：类固醇 - 螺 - 恶噻唑烷衍生物及其制备方法
公开(公告)号：US4342754A
公开(公告)日：1982-08-03
申请号：US242711
申请日：1981-03-11
申请人： Sandor Solyom , Katalin Szilagyi nee Farago , Lajos Toldi , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Sandor Solyom , Katalin Szilagyi nee Farago , Lajos Toldi , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： A61K31/58 , A61P7/10 , C07J41/00 , C07J43/00
CPC分类号： C07J41/0088 , C07J43/006 , Y10S514/869
摘要： New steroid-spiro-oxathiazolidine derivatives pharmaceutical compositions containing the same, and to a process for the preparation thereof are disclosed.The new compounds have antimineral corticoide effects and have the following formula (I), ##STR1## wherein R.sub.1 is a C.sub.1-3 alkyl or a C.sub.2-4 alkenyl group, andZ is a group of the formulae (II) to (VI), ##STR2## wherein R.sub.2 is methyl or ethyl,R.sub.3 is hydrogen or methylR.sub.4 is hydrogen, a C.sub.1-3 alkyl group, a di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl group, a C.sub.2-4 alkylcarbonyl group, a C.sub.2-4 alkoxycarbonyl group or a C.sub.3-6 carboxyalkylcarbonyl group, andthe dotted lines may represent additional valence bonds, with the proviso that if Z is a group of the formula (VI), a double bond exists between the carbon atoms in positions 4 and 5 or 5 and 6, andif R.sub.4 is a di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl group or a C.sub.3-6 carboxyalkylcarbonyl group, the compounds may also be formed as their salts.
摘要翻译：公开了新的类固醇 - 螺 - 恶唑烷衍生物药物组合物及其制备方法。新化合物具有抗皮质素的作用，具有下式（I），其中R 1为C 1-3烷基或C 2-4链烯基，Z为式（II）〜（VI），其中R2是甲基或乙基，R3是氢或甲基R4是氢，（VI）其中R2是甲基或乙基， C 1-3烷基，二（C 1-4烷基） - 氨基-C 1-4烷基，C 2-4烷基羰基，C 2-4烷氧基羰基或C 3-6羧基烷基羰基，虚线可以代表额外的价键，条件是如果Z是式（VI）的基团，则在4位和5位或5位和6位之间的碳原子之间存在双键，如果R4是二 - （C1- 4烷基） - 氨基-C 1-4烷基或C 3-6羧基烷基羰基，化合物也可以形成为其盐。

4. 发明授权

US4180505A Novel steroidspirooxazolidines and process for their preparation 失效
标题翻译：新型甾体螺恶唑烷及其制备方法
公开(公告)号：US4180505A
公开(公告)日：1979-12-25
申请号：US886349
申请日：1978-03-14
申请人： Sandor S. L. Toldy , Katalin Szilagyi nee Farago , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Sandor S. L. Toldy , Katalin Szilagyi nee Farago , Inge Schafer , Eleonora Szondy , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： A61K9/62 , A61K31/58 , A61K31/585 , A61P5/38 , A61P7/10 , C07J21/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J53/00
CPC分类号： C07J43/006 , C07J21/00 , C07J41/0088 , C07J51/00 , C07J53/004
摘要： The invention relates to novel spirooxazolidines represented by the formula I ##STR1## wherein R.sub.1 is alkyl having from 1 to 4 carbon atoms;R.sub.2 is hydrogen, alkyl having from 1 to 4 carbon atoms, alkenyl having from 1 to 4 carbon atoms, or dialkylphosphinoxymethyl having in the alkyl moiety from 1 to 3 carbon atoms each;Z is one of the groups represented by the formulae III to XIV as subsequently defined therein.
摘要翻译：本发明涉及由式I（I）表示的新型螺恶唑烷，其中R 1为具有1至4个碳原子的烷基; R2是氢，具有1至4个碳原子的烷基，具有1至4个碳原子的烯基，或每个具有1至3个碳原子的烷基部分的二烷基膦氧基甲基; Z是其后定义的由式III至XIV表示的基团之一。

5. 发明授权

US4028348A 6-Amino-5.beta.,19-cycloandrostane derivatives 失效
标题翻译： 6-氨基-5 {62,19-环戊二烯衍生物
公开(公告)号：US4028348A
公开(公告)日：1977-06-07
申请号：US658863
申请日：1976-02-17
申请人： Pal Bite , Imre Moravcsik , Inge Schafer , Gyula Horvath , Zsuzsanna Mehesfalvi nee Vajna , Janos Borvendeg , Ilona Hermann nee Szente
发明人： Pal Bite , Imre Moravcsik , Inge Schafer , Gyula Horvath , Zsuzsanna Mehesfalvi nee Vajna , Janos Borvendeg , Ilona Hermann nee Szente
IPC分类号： C07J53/00 , C07J41/00 , C07J43/00
CPC分类号： C07J53/00
摘要： Novel 6-amino-5.alpha.,19-cycloandrostane derivatives of formula I and their pharmaceutically acceptable addition salts ##STR1## wherein X denotes any of the groups of the formula =CH(OR), =CO or =C=N-OR.sub.1,Y denotes any of the groups of the formula =CO, =CH(OR.sub.1), =C=N-OR.sub.1, =C(OR.sub.1)-C.tbd.CH or ##STR2## wherein R denotes a hydrogen atom, a C.sub.1-4 alkyl group or a C.sub.2-5 acyl group, andR.sub.1 denotes a hydrogen atom, a straight-chained or branched C.sub.1-5 alkyl group, a straight-chained or branched C.sub.1-5 hydroxyalkyl group, a C.sub.3-8 cycloalkyl group, an allyl group, or a benzyl group, andR.sub.3 has the same meaning as R.sub.2 but if R.sub.2 is a sec. or tert. alkyl group or an alicyclic group, then R.sub.3 can only be a hydrogen atom; and if R.sub.2 is a benzyl group then R.sub.3 can only be a hydrogen atom or a primary alkyl group, furtherR.sub.2 and R.sub.3 may denote together with the adjcacent nitrogen atom a piperidine, a morpholine, or an N-methylpiperazine group. These compounds have exhibited an aldosterone-antagonistic effect on rats.
摘要翻译：式I的新型6-氨基-5α，19-环戊二烯衍生物及其药学上可接受的加成盐（I）其中X表示式= CH（OR），= CO或= C = N -OR1，Y表示式= CO，= CH（OR1），= C = N-OR1，= C（OR1）-C3ONDCH或者其中R表示氢原子，C1 -4-烷基或C 2-5酰基，R 1表示氢原子，直链或支链C 1-5烷基，直链或支链C 1-5羟基烷基，C 3-8环烷基，烯丙基或苄基，R3与R2具有相同的含义，但如果R2为秒。或叔。烷基或脂环基，那么R 3只能是氢原子; 并且如果R 2是苄基，那么R 3只能是氢原子或伯烷基，R 2和R 3可以与相邻的氮原子一起表示哌啶，吗啉或N-甲基哌嗪基。这些化合物对大鼠表现出醛固酮拮抗作用。

6. 发明授权

US4806685A 1,1,2-triphenylpropane and -propene derivatives 失效
标题翻译： 1,1,2-三苯基丙烷和 - 丙烯衍生物
公开(公告)号：US4806685A
公开(公告)日：1989-02-21
申请号：US825777
申请日：1986-01-31
申请人： Gizella Abraham , Tibor Horvath , Lajos Toldy , Janos Borvendeg , Endre Csanyi , Eva Kiss , Ilona S. nee Hermann , Kalman Tory
发明人： Gizella Abraham , Tibor Horvath , Lajos Toldy , Janos Borvendeg , Endre Csanyi , Eva Kiss , Ilona S. nee Hermann , Kalman Tory
IPC分类号： C07C43/225 , C07C43/313 , C07D295/092 , C07D303/22 , C07D303/26 , C07C93/06
CPC分类号： C07D295/088 , C07C247/00 , C07C43/225 , C07C43/313 , C07D303/22 , C07D303/26
摘要： A novel 1,1,2-triphenylpropene derivative, namely: ##STR1## acts on the endocrine system of rats. It exerts oestrogenic or antioestrogenic effects of varying strength in rats, and furthermore inhibits the growth of the mammary tumor induced by 7,12-dimethyl-benz(a)anthracene in rats.
摘要翻译：一种新的1,1,2-三苯基丙烯衍生物，即：作用于大鼠的内分泌系统。它在大鼠中发挥不同强度的雌激素或抗雌激素作用，进而抑制7,12-二甲基 - 苯并（a）蒽在大鼠中诱导的乳腺肿瘤的生长。

7. 发明授权

US4310549A Treatment of hypertension with 1-tert.-butylamino-3-(2,5-dichlorophenoxy)-2-propanol 失效
标题翻译：用1-叔丁基氨基-3-（2,5-二氯苯氧基）-2-丙醇治疗高血压
公开(公告)号：US4310549A
公开(公告)日：1982-01-12
申请号：US72295
申请日：1979-09-04
申请人： Andor Hajos , Marton Fekete , Marianna Kurti , Tibor Lang , Lajos Toldy , Janos Borvendeg , Laszlo Nagy , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Andor Hajos , Marton Fekete , Marianna Kurti , Tibor Lang , Lajos Toldy , Janos Borvendeg , Laszlo Nagy , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： C07C217/34 , A61K31/055 , A61K31/13 , A61K31/135 , C07C20060101 , C07C57/00 , C07C67/00 , C07C213/00
CPC分类号： C07D303/24
摘要： 1-tert.-butylamino-3-(2,5-dichlorophenoxy)-2-propanol and its pharmaceutically acceptable acid addition salts possess hypotensive and bradycardizing effects. Thus they can be applied in human therapy for the treatment of hypertension and simultaneously also of tachycardia.
摘要翻译： 1-叔丁基氨基-3-（2,5-二氯苯氧基）-2-丙醇及其药学上可接受的酸加成盐具有降血压和减速作用。因此，它们可以应用于人类治疗用于治疗高血压，同时也可用于心动过速。

8. 发明授权

US4579954A Cimetidine monohydrate 失效
标题翻译：西咪替丁一水合物
公开(公告)号：US4579954A
公开(公告)日：1986-04-01
申请号：US604385
申请日：1984-04-27
申请人： Kalman Harsanyi , Gyorgy Domany , Oszkar Fuchs , Lajos Toldy , Gyorgy Fekete , Endre Kasztreiner , Bela Hegedus , Ferenc Morasz , Andras Rado , Tibor Lang , Arpad Lazar , Eva Csongor , Tibor Balogh , Janos Borvendeg , Jozsef Reiter , Tibor Somogyi , Margit Bidlo nee Igloy
发明人： Kalman Harsanyi , Gyorgy Domany , Oszkar Fuchs , Lajos Toldy , Gyorgy Fekete , Endre Kasztreiner , Bela Hegedus , Ferenc Morasz , Andras Rado , Tibor Lang , Arpad Lazar , Eva Csongor , Tibor Balogh , Janos Borvendeg , Jozsef Reiter , Tibor Somogyi , Margit Bidlo nee Igloy
IPC分类号： A61K31/415 , A61P1/04 , C07D233/54 , C07D233/64
CPC分类号： C07D233/64
摘要： The invention relates to the new monohydrate of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine (cimetidine), a histamine-H.sub.2 receptor antagonist which is called N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine H (cimetidine H) as well as to a process for the preparation of same, which comprises pouring a hot, homogeneous aqueous solution of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine, optionally containing also methylamine, onto ice and separating the N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine monohydrate.
摘要翻译：本发明涉及N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N' - 氰基胍（西咪替丁），组胺-H 2受体称为N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N'-氰基胍脒H（西咪替丁H）的方法以及其包括将热的均匀的N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N“ - 氰基胍的水溶液，任选地含有并将甲胺加到冰上并分离N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N'-氰基胍一水合物。

9. 发明授权

US4539199A Sustained release pharmaceutical compositions 失效
标题翻译：持续释放药物组合物
公开(公告)号：US4539199A
公开(公告)日：1985-09-03
申请号：US384084
申请日：1982-06-01
申请人： Erno Orban , Janos Borvendeg , Laszlo Nagy , Marta Sotinee Tolvay , Erzsebet Bander
发明人： Erno Orban , Janos Borvendeg , Laszlo Nagy , Marta Sotinee Tolvay , Erzsebet Bander
IPC分类号： A61K47/48 , A01N25/12 , A61K31/78
CPC分类号： A61K47/48176
摘要： Pharmaceutical compositions for sustained release of pharmaceutical compounds comprising a reaction product of a water soluble salt of a pharmaceutically active compound containing a primary, secondary or tertiary amino group, and an alkali or ammonium salt of a synthetic copolymer containing an acid group, and selected from the group consisting of methacrylic acid/methacrylic acid methyl ester, methacrylic acid/acrylic acid methyl ester and methacrylic acid/acrylic acid methyl ester/methacrylic acid methyl ester copolymers and a pharmaceutically acceptable excipient. The water soluble salt of a pharmaceutically active compound containing a primary, secondary or tertiary amino group is reacted in aqueous medium with an alkali or ammonium salt of a copolymer selected from the group consisting of the above mentioned copolymers, and the resulting product is converted into a pharmaceutical composition.
摘要翻译：用于持续释放药物组合物的药物组合物，其包含含有伯，仲或叔氨基的药物活性化合物的水溶性盐与含有酸基的合成共聚物的碱金属盐或铵盐的反应产物，并且选自由甲基丙烯酸/甲基丙烯酸甲酯，甲基丙烯酸/丙烯酸甲酯和甲基丙烯酸/丙烯酸甲酯/甲基丙烯酸甲酯共聚物和药学上可接受的赋形剂组成的组。含有伯，仲或叔氨基的药物活性化合物的水溶性盐在水性介质中与选自上述共聚物的共聚物的碱金属盐或铵盐反应，将所得产物转化为药物组合物。

10. 发明授权

US4418205A 16-Amino-18,19,20-trinor-prostaglandin derivatives, and acid addition salts 失效
标题翻译： 16-氨基-18,19,20-三肽前列腺素衍生物和酸加成盐
公开(公告)号：US4418205A
公开(公告)日：1983-11-29
申请号：US329039
申请日：1981-12-09
申请人： Eva Toth-Sarudy , Gabor Ambrus , Gyorgy Cseh , Janos Borvendeg , Imre Moravcsik , Gabriella Mezei
发明人： Eva Toth-Sarudy , Gabor Ambrus , Gyorgy Cseh , Janos Borvendeg , Imre Moravcsik , Gabriella Mezei
IPC分类号： A61K31/557 , A61K31/5575 , A61P15/00 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0041 , Y02P20/55
摘要： The invention relates to new 16-amino-18,19,20-trinor-prostaglandin derivatives of general formula I, having at C-17 a substituted or unsubstituted phenyl group, wherein C-15 and C-16 may have either S or R configuration, Y stands for a hydrogen atom or a lower alkyl group, W stands for a hydrogen atom, halogen atom, hydroxy group, lower alkyl or alkoxy group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrobenzyloxycarbonyl protective group of a 9.alpha.,11.alpha.,15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-17-phenyl-5-cis,13-trans-18,19,20-trinor-prostadienoic acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration, W is as defined above, and Y stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where W is as defined above and Y stands for a lower alkyl group, solely the p-nitrobenzyloxycarbonyl group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt.The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied in cattle raising for estrus and birth synchronization, furthermore in the veterinary praxis for the treatment of sterility, chronic endometritis and pyometry.
摘要翻译：本发明涉及具有C-17取代或未取代的苯基的通式I的新的16-氨基-18,19,20-三核 - 前列腺素衍生物，其中C-15和C-16可具有S或R 构型中，Y表示氢原子或低级烷基，W表示氢原子，卤素原子，羟基，低级烷基或烷氧基，以及它们的酸加成盐。这些化合物可以通过除去9α，11α，15-三羟基-16-对硝基苄氧羰基酰胺基-17-苯基-5-顺式，13-trn-18的酯基和对硝基苄氧羰基保护基来制备，其中C-15和C-16可以具有S或R构型，W如上所定义，Y代表低级烷基 - 在任选的序列中，具有通式XII-的19,20-三过 - 前列腺素酸衍生物 - 在通式I的那些化合物中的限制，其中W如上所定义，Y代表低级烷基，仅除去对硝基苄氧基羰基，所得到的通式I的产物任选地用有机或无机酸变成盐。本发明的新型前列腺素衍生物具有有价值的治疗特性，可用于发情期和出生同步的养牛，此外还适用于无菌治疗，慢性子宫内膜炎和高血压的兽医学应用。

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