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1. 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。

2. 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。

3. 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。

4. 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。

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

US4284642A 1,3-Diaryl-2-imino-imidazolidines and compositions thereof 失效
标题翻译： 1,3-二芳基-2-亚氨基咪唑啉及其组合物
公开(公告)号：US4284642A
公开(公告)日：1981-08-18
申请号：US30149
申请日：1979-04-16
申请人： Lajos Toldy , Zoltan Zubovics , Mariann Kurti , Inge Schafer
发明人： Lajos Toldy , Zoltan Zubovics , Mariann Kurti , Inge Schafer
IPC分类号： A61K31/415 , A61K31/505 , A61P7/10 , A61P29/00 , C07D233/46 , C07D233/48 , C07D233/52 , C07D233/88 , C07D239/10 , C07D239/14 , C07D239/18 , C07D247/02
CPC分类号： C07D239/18 , C07D233/46 , C07D233/48 , C07D233/52 , C07D233/88 , C07D239/14 , C07D247/02 , Y10S514/869
摘要： The invention relates to new compounds of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.5 each represent a phenyl group, optionally substituted,R.sup.2 stands for hydrogen, formyl group, carboxy group, lower alkoxycarbonyl group, hydroxy-(lower)-alkoxycarbonyl group, or a lower alkyl group, optionally substituted,R.sup.3 and R.sup.4 each represent hydrogen atom or a lower alkyl group, with the proviso that when R.sup.1 and R.sup.5 each represent a phenyl group, R.sup.2 and R.sup.3 may not stand for hydrogen.These compounds possess valuable biological properties, and can be applied primarily as antiphlogistic or diuretic agents.
摘要翻译：本发明涉及通式（I）的新化合物，其中R 1和R 5各自表示苯基，任选被取代，R 2代表氢，甲酰基，羧基，低级烷氧基羰基，羟基 - （低级） - 烷氧基羰基或任选取代的低级烷基，R 3和R 4各自表示氢原子或低级烷基，条件是当R 1和R 5各自表示苯基时，R 2和R 3可以不表示氢。这些化合物具有宝贵的生物学特性，可以主要用作消炎或利尿剂。

7. 发明授权

US4369325A 1,3-Diaryl-2-imino-imidazolidines and compounds 失效
标题翻译： 1,3-二芳基-2-亚氨基 - 咪唑烷和化合物
公开(公告)号：US4369325A
公开(公告)日：1983-01-18
申请号：US292002
申请日：1981-08-11
申请人： Lajos Toldy , Zoltan Zubovics , Mariann Kurti , Inge Schafer
发明人： Lajos Toldy , Zoltan Zubovics , Mariann Kurti , Inge Schafer
IPC分类号： A61K31/415 , A61K31/505 , A61P7/10 , A61P29/00 , C07D233/46 , C07D233/48 , C07D233/52 , C07D233/88 , C07D239/10 , C07D239/14 , C07D239/18 , C07D247/02 , C07D233/44
CPC分类号： C07D239/18 , C07D233/46 , C07D233/48 , C07D233/52 , C07D233/88 , C07D239/14 , C07D247/02 , Y10S514/869
摘要： A compound of the general formula (I), ##STR1## is described wherein R.sup.1 and R.sup.5 each represent a phenyl group optionally substituted with 1 to 3 lower alkoxy, halo, lower alkyl, monohalo-(lower)-alkyl, dihalo-(lower)-alkyl and/or trihalo-(lower)-alkyl groups, R.sup.2 stands for hydrogen or a lower alkyl group optionally substituted with a hydroxy group or 1 to 3 halogen atoms, R.sup.3 and R.sup.4 each represent a hydrogen atom or a lower alkyl group, and R.sup.6 stands for a carbamoyl, thiocarbamoyl or amidino group having optionally one or two lower alkyl and/or lower alkoxycarbonyl substitutes, or a group of the general formula R.sup.7 -CO-wherein R.sup.7 stands for a lower analkoxy group, an aryloxy group, or an aralkoxy group, and n is equal to 0, provided that when R.sup.1 and R.sup.5 each represent a phenyl group, R.sup.2 and R.sup.3 may not stand for hydrogen or a pharmaceutically acceptable acid addition salt, a pure isomer or an isomeric mixture thereof. The compounds posses antiphlogistic and diuretic activity.
摘要翻译：描述了通式（I），化合物（I）的化合物，其中R 1和R 5各自表示任选被1至3个低级烷氧基，卤素，低级烷基，单卤代（低级）烷基，二卤代 - （低级） - 烷基和/或三卤代（低级） - 烷基，R2代表任选被羟基或1-3个卤素原子取代的氢或低级烷基，R3和R4各自表示氢原子或低级烷基，R6表示具有任选一个或两个低级烷基和/或低级烷氧基羰基取代基的氨基甲酰基，硫代氨基甲酰基或脒基，或通式为R7-CO-的基团，其中R7表示较低的苯氧基，芳氧基或芳烷氧基，n等于0，条件是当R 1和R 5各自表示苯基时，R 2和R 3可以不代表氢或药学上可接受的酸加成盐，纯异构体或其异构体混合物。这些化合物具有消炎和利尿活性。

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