专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

101. 发明授权

US4039668A Corticoid-containing inhalants 失效
标题翻译：含有CORTICOID的含量
公开(公告)号：US4039668A
公开(公告)日：1977-08-02
申请号：US714668
申请日：1976-08-16
申请人： Peter Fuchs , Erich Gerhards , Heinz Matthes , Hans Wendt , Rudolf Wiechert
发明人： Peter Fuchs , Erich Gerhards , Heinz Matthes , Hans Wendt , Rudolf Wiechert
IPC分类号： A61K9/00 , A61K31/57 , A61K31/58
CPC分类号： A61K9/0075 , A61K31/57 , A61K9/008
摘要： Inhalants comprising at least one corticoid of the general formula ##STR1## wherein --B--A-- is CH.sub.2 --CH.sub.2 --, CH=CH-- or CCl=CH--; X is a hydrogen atom, a fluorine atom, or methyl; Y is a hydrogen atom, a fluorine atom or a chlorine atom; Z is methylene, hydroxymethylene, fluoromethylene, a chloromethylene, or carbyl; R.sub.1 is a hydrogen atom or methyl and R.sub.2 is a hydrogen atom, or R.sub.1 and R.sub.2 collectivey are isopropylidenedioxy; and R.sub.3 is hydrocarbon of 1-12 carbon atoms, are useful for the treatment of allergic diseases of the respiratory tract.

102. 发明授权

US4036695A Process for the preparation of estrene-3,17-dione derivatives 失效
标题翻译：雌激素-3,17-二酮衍生物的制备方法
公开(公告)号：US4036695A
公开(公告)日：1977-07-19
申请号：US633415
申请日：1975-11-19
申请人： Karl Petzoldt , Rudolf Wiechert
发明人： Karl Petzoldt , Rudolf Wiechert
IPC分类号： C12P33/12 , C07J1/00 , C07J21/00 , C07J31/00 , C07J53/00 , C12R1/80 , C07B29/02
CPC分类号： C07J31/006 , C07J1/0059 , C07J21/006 , C07J53/008 , Y10S435/929 , Y10S435/933 , Y10S435/935
摘要： Estrene-3,17-diones of the formula ##STR1## wherein X is oxo, or ketalized oxo, preferably alkylenedioxy of 2-6 carbon atoms or o-phenylenedioxy;.DELTA. is a carbon atom linked to the adjacent carbon atoms by a double bond and two single bonds;R.sub.1 is methyl or ethyl, andR.sub.2 and R.sub.3 collectively are a carbon-to-carbon bond or methylene, useful as intermediates for the production of pharmacologically active steroids, are prepared by fermenting 18-ethyl-4-estrene-3,17-dione or 18-methyl-4-estrene-3,17-dione with a fungal culture of the genus Penicillium or Fusarium to produce the corresponding 15.alpha.-hydroxy-steroid;In either order, converting the hydroxy group of the thus-produced 15.alpha.-hydroxy steroid to a sulfonic acid ester thereof and ketalizing the 3-keto group thereof; andTreating the ketalized and esterified steroid with a base to form a .DELTA..sup.15 -compound or with dimethylsulfoxonium methylide to form a 15.beta.,16.beta.-methylene compound and, optionally, hydrolyzing the 3-ketal group.
摘要翻译：其中X是氧代或缩酮化的氧代，优选2-6个碳原子的亚烷基二氧基或邻苯二氧基的式（III）的雌二烯-3,17-二酮; DELTA是通过双重债券和两个单一债券连接到相邻碳粉的碳钢; R1是甲基或乙基，R2和R3统称为碳 - 碳键或亚甲基，可用作制备药理活性类固醇的中间体，是通过发酵18-乙基-4-雌酮-3,17-二酮或18-甲基-4-雌二烯-3,17-二酮与青霉属或镰刀菌属的真菌培养物反应以产生相应的15α-羟基类固醇; 无论如何，将THUS生产的15α-羟基甾体的羟基转化为硫酸酯，并将其3-酮醇酯组进行KETAL化; 并用碱处理酮化和纯化的甾体以形成DELTA 15化合物或用二甲基甲硅烷基甲酸酯形成15β，16β-乙烯基化合物，并且有选择地水解3-KETAL基团。

103. 发明授权

US4033995A D-homo steroids 失效
标题翻译： D-类固醇
公开(公告)号：US4033995A
公开(公告)日：1977-07-05
申请号：US609707
申请日：1975-09-02
申请人： Robert C. Nickolson , Ulrich Kerb , Rudolf Wiechert
发明人： Robert C. Nickolson , Ulrich Kerb , Rudolf Wiechert
IPC分类号： A61K31/185 , A61K31/21 , C07J63/00
CPC分类号： C07J63/008 , Y10S435/832 , Y10S435/911 , Y10S514/861 , Y10S514/863
摘要： D-Homo-21-carboxylic acids of the formula ##STR1## the represents a single bond or a double bond; X is a hydrogen atom, a fluorine atom, or methylene;Y is a hydrogen atom, a fluorine atom, or a chlorine atom;Z is methylene, carbonyl, .beta.-hydroxymethylene, a .beta.-alkanoyloxymethylene or when Y is a chlorine atom, also .beta.-fluoromethylene or .beta.-chloromethylene;R.sub.1 is a hydrogen atom or methyl; andR.sub.2 is a hydrogen atom, hydroxy or alkanoyloxy; and their physiologically acceptable salts with bases and the 21-esters thereof, possess topical anti-inflammatory activity.
摘要翻译：式“IMAGE”的D-homo-21-羧酸代表单键或双键; X是氢原子，氟原子或亚甲基; Y是氢原子，氟原子或氯原子; Z是亚甲基，羰基，β-羟基亚甲基，β-烷酰氧基亚甲基或当Y是氯原子时，也是β-氟亚甲基或β-氯亚甲基; R1是氢原子或甲基; R2为氢原子，羟基或烷酰氧基; 并且其与碱及其21-酯的生理上可接受的盐具有局部抗炎活性。

104. 发明授权

US4028400A D-homosteroids 失效
标题翻译： D-类固醇
公开(公告)号：US4028400A
公开(公告)日：1977-06-07
申请号：US507884
申请日：1974-09-20
申请人： Leo Alig , Andor Furst , Peter Keller , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人： Leo Alig , Andor Furst , Peter Keller , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
IPC分类号： C07J63/00
CPC分类号： C07J63/008
摘要： The present invention relates to steroids. More particularly, the invention is concerned with D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same.
摘要翻译：本发明涉及类固醇。更具体地，本发明涉及D-类固醇，其制备方法和含有它的药物制剂。

105. 发明授权

US4026922A D-Homo-pregnene steroids 失效
标题翻译： D-异孕烯类固醇
公开(公告)号：US4026922A
公开(公告)日：1977-05-31
申请号：US619065
申请日：1975-10-02
申请人： Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人： Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
IPC分类号： C07C69/013 , A61K31/12 , A61K31/215 , A61K31/22 , A61K35/56 , B01J23/00 , C07B61/00 , C07C45/00 , C07C49/587 , C07C67/00 , C07J63/00 , C07J71/00 , C12P33/02
CPC分类号： C07J71/001 , C07J63/00 , C07J63/008 , Y10S514/96
摘要： The present disclosure relates to novel D-homo-pregnene steroids useful as progestational agents.
摘要翻译：本公开内容涉及可用作促孕剂的新型D-同型孕激素类固醇。

106. 发明授权

US4024166A Process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones 失效
标题翻译：制备13 {62-烷基-4-锑烯-3,17-二酮的方法
公开(公告)号：US4024166A
公开(公告)日：1977-05-17
申请号：US621384
申请日：1975-10-10
申请人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
发明人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
IPC分类号： B01J23/00 , C07B61/00 , C07C317/14 , C07D317/26 , C07D317/72 , C07J1/00
CPC分类号： C07C317/00 , C07D317/26 , C07D317/72 , C07J1/0059
摘要： Novel process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones of the formula ##STR1## wherein R.sub.1 is methyl or ethyl, consists of REACTING A 7A.beta.-ALKYL,5,6,7,7A-TETRAHYDROINDANE-1,5-DIONE WITH FORMALDEHYDE AND AN ARYLSULFINIC ACID OR AN ADDUCT OF FORMALDEHYDE AND ARYLSULFINIC ACID TO PRODUCE A TETRAHYDROINDANE DERIVATIVE;Hydrogenating the tetrahydroindane derivative with hydrogen in the presence of a palladium-, platinum-, or rhodium-containing hydrogenation catalyst to produce a perhydroindane derivative;Condensing the perhydroindane derivative in the presence of a proton-accepting agent with a 7,7-alkylenedioxy-3-oxooctanoic acid ester;Treating the product obtained with a strong aqueous base and then heating the product in an inert solvent to produce a 4,5-secosteroid;Hydrogenating the 4,5-secosteroid in the presence of a palladium-, platinum-, rhodium-, or nickel-containing hydrogenation catalyst; andHydrolyzing and cyclizing the hydrogenated 4,5-secosteroid by treatment with a strong acid.
摘要翻译：用于制备式“IMAGE”的13β-烷基-4-单宁-3,17-二酮的新方法，其中R 1是甲基或乙基，由反应A7Aβ-烷基，5,6,7,7a- 四氢呋喃-1,5-二酮与甲醛和氨基磺酸或甲醛和芳香酸的添加以生产四氢衍生物衍生物; 在含有氢氧化钯，或含氢氧化铑的氢化催化剂存在下氢化四氢呋喃衍生物生成四氢呋喃衍生物; 在具有7,7-亚甲基氧化亚硝酸酯酸酯的接受原料的情况下，冷凝该衍生物衍生物; 处理用强碱性基质获得的产品，然后加入产品中的产品用于生产4,5代谢物; 在含有钯，铑，铑，或含镍的氢化催化剂存在下氢化4,5-二氧化硫; 并通过用强酸处理氢化和循环氢化的4,5代谢物。

107. 发明授权

US4012420A 9,10-Secoestrane derivatives and their production 失效
标题翻译： 9,10-Secoestrane衍生物及其生产
公开(公告)号：US4012420A
公开(公告)日：1977-03-15
申请号：US570072
申请日：1975-04-21
申请人： Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
发明人： Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
IPC分类号： C07C49/84 , C07C69/01 , C07C401/00 , C07D317/46 , C07D319/08
CPC分类号： C07D317/46 , C07C49/84 , C07C69/01
摘要： 9,10-Secoestranes, useful as intermediates in the total synthesis of steroids, of the formula ##STR1## WHEREIN N IS 1 OR 2, R.sub.1 is lower alkyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen, alkoxy or acyloxy, X is free or ketalized carbonyl or free, esterified or etherified hydroxymethylene, and Y is carbonyl or dialkoxymethylene are produced by condensing, in the presence of a basic catalyst, ##STR2## WHEREIN X, n, R.sub.1, R.sub.2, R.sub.3, R.sub.4 have the values given above, and Z is Cl, Br or I, to produce a 9,10-secoestrane of the above formula wherein Y is a free carbonyl group, which can then, if desired, be ketalized to a corresponding compound wherein Y is dialkoxymethylene or like ketal group.
摘要翻译： 9,10-Secoestranes，用作类固醇总合成中的中间体，式为“IMAGE”，其中N为1或2，R 1为低级烷基，R 2，R 3和R 4为氢，烷氧基或酰氧基，X为游离或缩酮化的羰基或游离的，酯化的或醚化的羟基亚甲基，Y是羰基或二烷氧基亚甲基，是在碱性催化剂存在下，通过在上述给定的值下，并且Z是Cl，Br或I，以产生上式的9,10-隔离子，其中Y是游离羰基，如果需要，其可以被缩醛化成相应的化合物，其中Y是二烷氧基亚甲基或类似的缩酮基。

108. 发明授权

US3965128A 6.beta.,7.beta.-Epoxy-1.alpha.,2.alpha.-methylen-D-homo-4-pregnen-3,20-di ones 失效
标题翻译： 6 {62,7 {62-环氧-1 {60,2 {60-亚甲基-D-同-4-孕烯-3,20-二酮
公开(公告)号：US3965128A
公开(公告)日：1976-06-22
申请号：US508492
申请日：1974-09-23
申请人： Andor Furst , Marcel Muller , Leo Alig , Peter Keller , Ulrich Kerb , Rudolf Wiechert
发明人： Andor Furst , Marcel Muller , Leo Alig , Peter Keller , Ulrich Kerb , Rudolf Wiechert
IPC分类号： C07D303/32 , C07J63/00 , C07D303/44
CPC分类号： C07J63/008
摘要： New 6.beta.,7.beta.-epoxy-17.alpha.-hydroxy or acyloxy-1.alpha.,2.alpha.-methylen-D-homo-4-pregnen-3,20-diones having surprising progestational activity are disclosed.
摘要翻译：公开了具有惊人刺激活性的新的6β，7β-环氧-17α-羟基或酰氧基-1α，2α-亚甲基-D-同-4-孕烯-3,20-二酮。

109. 发明授权

US5569652A Dihydrospirorenone as an antiandrogen 失效
标题翻译：二氢螺旋酮作为抗雄激素
公开(公告)号：US5569652A
公开(公告)日：1996-10-29
申请号：US162387
申请日：1993-12-07
申请人： Sybille Beier , Walter Elger , Yukishige Nishino , Rudolf Wiechert
发明人： Sybille Beier , Walter Elger , Yukishige Nishino , Rudolf Wiechert
IPC分类号： A61K31/565 , A61K31/585 , C07J1/00 , C07J21/00 , C07J53/00
CPC分类号： A61K31/585
摘要： Dihydrospirorenone, ##STR1## preferably together with an estrogen, can be used for the production of a pharmaceutical agent suitable for treatment of hormonal irregularities during premenopause (menstruation stabilization), for hormonal substitution therapy during menopause, for treatment of androgen-induced disorders and/or for contraception.
摘要翻译：二氢螺旋酮，（I）优选与雌激素一起可用于制备适于治疗绝经前（月经稳定）期间的激素不规则，用于更年期期间的激素替代疗法用于治疗雄激素诱导疾病和/或避孕。

110. 发明授权

US5145847A 14,17.alpha.-etheno- and -ethanoestratrienes, processes for the preparation of these compounds, as well as their use for the production of medicinal agents 失效
标题翻译： 14,17（ALPHA） - 乙酸和乙二胺，其制备这些化合物的方法，以及其用于生产药物的用途
公开(公告)号：US5145847A
公开(公告)日：1992-09-08
申请号：US558340
申请日：1990-07-27
申请人： Rolf Bohlmann , Hermann Kunzer , Rudolf Wiechert , David Henderson , Martin Schneider , Yukishige Nishino
发明人： Rolf Bohlmann , Hermann Kunzer , Rudolf Wiechert , David Henderson , Martin Schneider , Yukishige Nishino
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J53/00
CPC分类号： C07J53/002
摘要： Disclosed are novel 14,17.alpha.-etheno- and -ethanoestratrienes according to general Formula I ##STR1## wherein X is a --CH.sub.2 --CH.sub.2 or ##STR2## R.sup.1 is a hydrogen atom, a C.sub.1 - to C.sub.15 -acyl, benzoyl, C.sub.1 - to C.sub.15 -alkyl, C.sub.3 - to C.sub.9 -cycloalkyl or alkylcycloalkyl group, andR.sup.2 is the grouping ##STR3## wherein R.sup.3 and R.sup.4 independently of each other mean a hydrogen atom or a straight-chain or branched, optionally partially or completely fluorinated C.sub.1 -C.sub.8 -alkyl group,a process for their preparation, pharmaceutical preparations containing these compounds, as well as their use for the production of medicinal agents.The novel compounds exhibit strong antiestrogenic efficacy.
摘要翻译：公开了根据通式I（I）的新型14,17α-乙烯 - 和 - 乙二醇三亚甲基，其中X是-CH 2 -CH 2或者R 1是氢原子，C 1至C 15酰基，苯甲酰基，C 1至C 15 - 烷基，C 3至C 9 - 环烷基或烷基环烷基，并且R 2为分组，其中R 3和R 4彼此独立地表示氢原子或直链或支链，任选地部分或部分完全氟化的C 1 -C 8烷基，其制备方法，含有这些化合物的药物制剂，以及它们用于制备药剂的用途。新化合物表现出强的抗雌激素疗效。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式