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61. 发明授权

US4017545A Process for the preparation of bicycloalkane derivatives 失效
标题翻译：双链烷烃衍生物的制备方法
公开(公告)号：US4017545A
公开(公告)日：1977-04-12
申请号：US481241
申请日：1974-06-20
申请人： Gerhard Sauer , Hans Peter Lorenz , Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Rudolf Wiechert
发明人： Gerhard Sauer , Hans Peter Lorenz , Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Rudolf Wiechert
IPC分类号： C07C69/013 , C07B31/00 , C07B53/00 , C07C45/00 , C07C45/61 , C07C49/385 , C07C49/587 , C07C49/653 , C07C67/00 , C07C69/02 , C07C69/716 , C07C69/738 , C07C313/00 , C07C315/04 , C07C317/00 , C07C317/04 , C07C317/24 , C07D261/08 , C07D317/26 , C07D317/30 , C07D317/46 , C23C14/06 , C07C49/76
CPC分类号： C07D317/30 , C07C317/00
摘要： Bicycloalkanes useful as intermediates in the total synthesis of steroids of the formula ##STR1## WHEREIN N IS THE INTEGER 1 OR 2; R.sub.1 is lower-alkyl; X is free or ketalized carbonyl or free, esterified or etherified hydroxymethylene; and Y is --SO.sub.2 --R.sub.2 or --C(Z)(R.sub.3)--R.sub.4 wherein R.sub.2 is alkyl, aryl or aralkyl R.sub.3 is H or lower-alkyl, R.sub.4 is alkoxycarbonyl or acyl and Z is lower-alkoxycarbonyl, lower acyl, lower alkylsulfinyl or lower-alkylsulfonyl, are produced by the steps of hydrogenating a compound of the formula ##STR2## AND CONDENSING THE THUS-PRODUCED RING SATURATED COMPOUND WITH A SALT OF THE FORMULA C(Z)(R.sub.3)R.sub.4 .sup.-Me.sup.+ wherein n, X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Z have the values given above.
摘要翻译：双环烷烃可用作中间体，用于全合成类固醇，其结构式为“IMAGE”，其中N为整数1或2; R1是低级烷基; X是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; 并且Y是-SO 2 -R 2或-C（Z）（R 3）-R 4，其中R 2是烷基，芳基或芳烷基R 3是H或低级烷基，R 4是烷氧基羰基或酰基，Z是低级烷氧基羰基，低级酰基，低级烷基亚磺酰基或低级烷基磺酰基的方法是通过以下步骤制备的：将下式化合物氢化，并且将式（I）化合物与式（C）的（R 3）R 4 - >其中n，X，R1，R2，R3，R4和Z具有上面给出的值。

62. 发明授权

US3960842A Process for the preparation of 17.beta.-oxalyl steroids 失效
标题翻译：制备17种{62-草酰类固醇的方法
公开(公告)号：US3960842A
公开(公告)日：1976-06-01
申请号：US487987
申请日：1974-07-12
申请人： Gregor Haffer , Ulrich Eder , Henry Laurent , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
发明人： Gregor Haffer , Ulrich Eder , Henry Laurent , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
IPC分类号： C07J51/00 , C07J7/00 , C07J21/00 , C07J41/00
CPC分类号： C07J41/0094 , C07J21/006 , C07J7/0095
摘要： 20-Cyano-17.alpha.-H steroids having as the 17-position substituent the group ##EQU1## wherein R is H, alkyl of 1-8 carbon atoms or benzyl, having a 13-methyl or 13-ethyl group and which are unsubstituted or substituted with an .alpha.-methyl group in the 16-position are converted to the corresponding 20-keto steroids by reaction in an aprotic solvent with a deprotonating agent containing an alkali metal, an alkaline earth metal, copper(I) or thallium(I), and optionally additionally with a copper(I) salt or a thallium(I) salt or a silver(I) salt, and thereafter conducting an oxidative splitting reaction with oxygen. The thus-produced 17.beta.-oxalyl steroids possess pharmacological activity, e.g., anti-inflammatory activity, or are useful as intermediates for the production of pharmacologically active steroids.
摘要翻译：具有作为17位取代基的20-Cyano-17α-H类固醇，COOR | CHCN |其中R是H，1-8个碳原子的烷基或具有13-甲基或13-乙基的苄基，通过在非质子传递溶剂中与含有碱金属，碱土金属，铜（I）或铊的脱质子化剂反应将未取代或被16位上的α-甲基取代的α-甲基转化为相应的20-酮类固醇 I）和任选地另外加入铜（I）盐或铊（I）盐或银（I）盐，然后与氧进行氧化分解反应。由此产生的17β-草酰甾族类固醇具有药理学活性，例如抗炎活性，或可用作制备药理活性类固醇的中间体。

63. 发明授权

US3956347A Novel pregnanoic acid derivatives 失效
标题翻译：新型孕酸衍生物
公开(公告)号：US3956347A
公开(公告)日：1976-05-11
申请号：US460905
申请日：1974-04-15
申请人： Henry Laurent , Rudolf Wiechert , Klaus Mengel , Hans Wendt
发明人： Henry Laurent , Rudolf Wiechert , Klaus Mengel , Hans Wendt
IPC分类号： C07J7/00 , A61K31/57 , A61K31/67 , A61P29/00 , C07C20060101 , C07J1/00 , C07J3/00 , C07J5/00
摘要： Steroids of the formula ##SPC1##Wherein X is a hydrogen atom, a halogen atom or methyl; Y is a hydrogen atom or a halogen atom; Z is carbonyl, .beta.-acyloxymethylene or, when Y is a hydrogen atom, also methylene; R.sub.1 is a hydrogen atom or methyl; R.sub.2 is a hydrogen atom, an alkali metal atom or optionally substituted hydrocarbon; and --A--B-- is --CH=CH--, --CCl=CH-- or when at least one of X, Y and R.sub.1 is other than a hydrogen atom, --CH.sub.2 --CH.sub.2 --, which can be produced by oxidizing a corresponding 20-hydroxy steroid or a corresponding 21-aldehyde, possess topical anti-inflammatory activity.
摘要翻译：式WHEREIN X的类固醇是氢原子，卤素原子或甲基; Y是氢原子或卤素原子; Z是羰基，β-酰氧基亚甲基，或当Y是氢原子时也是亚甲基; R1是氢原子或甲基; R2是氢原子，碱金属原子或任选取代的烃; 并且-AB-是-CH = CH-，-CCl = CH-，或者当X，Y和R 1中的至少一个不是氢原子时，-CH 2 -CH 2 - 可以通过氧化相应的20- 羟基类固醇或相应的21-醛具有局部抗炎活性。

64. 再颁专利

USRE28690E 17.alpha.-Ethinyl-18-methyl-19-nortestosterone esters 失效
标题翻译： 17 {60-乙炔基-18-甲基-19-去甲睾酮酯
公开(公告)号：USRE28690E
公开(公告)日：1976-01-20
申请号：US490022
申请日：1974-07-19
申请人： Hans-Gunter Lehmann , Heinz Gibian , Rudolf Wiechert , Friedmund Neumann
发明人： Hans-Gunter Lehmann , Heinz Gibian , Rudolf Wiechert , Friedmund Neumann
IPC分类号： A61K31/569 , C07J1/00 , C07J75/00
CPC分类号： A61K31/569 , C07J1/00 , C07J75/00
摘要： A therapeutic compound for inhibiting ovulation comprising a 17-ester of 17.alpha.-ethinyl-18-methyl-19-nortestosterone wherein the said 17-ester group is formed from an aliphatic carboxylic acid having from six to 11 carbon atoms in the ester residue..Iaddend.

65. 发明授权

US4956482A Process for the preparation of pregnane derivatives 失效
标题翻译：孕烷衍生物的制备方法
公开(公告)号：US4956482A
公开(公告)日：1990-09-11
申请号：US325585
申请日：1989-03-20
申请人： Helmut Hofmeister , Klaus Annen , Henry Laurent , Rudolf Wiechert
发明人： Helmut Hofmeister , Klaus Annen , Henry Laurent , Rudolf Wiechert
IPC分类号： B01J23/50 , C07B61/00 , C07J1/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J41/00 , C07J63/00 , C07J75/00
CPC分类号： C07J5/0053 , C07J1/0011 , C07J1/0033 , C07J41/0038 , C07J63/008 , C07J7/0085
摘要： Known pregnane derivatives are prepared by esterification of know androstane derivatives to give new esters of Formula III ##STR1## wherein in each case symbolizes a single bond or a double bond,n is 1 or 2,R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen or formyl, andR.sub.3 is chlorine, hydroxy or an alkanoyloxy group of up to 6 carbon atoms,and reaction of the latter with Ag(I) and formic acid.

66. 发明授权

US4777165A 6.alpha., 16.beta.-dimethyl corticoids and their anti-inflammatory use 失效
标题翻译： 6α，16β-二甲基皮质激素及其抗炎用途
公开(公告)号：US4777165A
公开(公告)日：1988-10-11
申请号：US64029
申请日：1987-06-17
申请人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert , Michael Topert
发明人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert , Michael Topert
IPC分类号： A61K31/57 , A61K31/575 , A61P5/38 , C07J5/00 , C07J7/00 , C07J9/00 , C07J31/00 , C07J71/00 , A61K31/56 , C07J1/00
CPC分类号： C07J7/0055 , C07J31/006 , C07J5/0076 , C07J71/0015 , C07J9/00
摘要： 6.alpha.,16.beta.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond .sub.-------- is a single bond or a double bond, andX is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,Z is a hydrogen atom or, jointly with X, is a carbon-carbon bond,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom or a methyl group,are pharmacologically active compounds.
摘要翻译： 6α，16β-二甲基皮质类固醇通式Ⅰ（Ⅰ）其中键----是单键或双键，X是氢原子，氟原子，氯原子或溴原子，Z为氢原子，或与X一起为碳 - 碳键，R1为2-8个碳原子的甲酰基，烷酰基或烷氧基烷基，或苯甲酰基，Y为氢原子或甲基是药理活性化合物。

67. 发明授权

US4578475A Novel D-homosteroids 失效
标题翻译：新型D-类固醇激素
公开(公告)号：US4578475A
公开(公告)日：1986-03-25
申请号：US573983
申请日：1984-01-26
申请人： Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人： Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
IPC分类号： A61K31/15 , A61K31/275 , C07J63/00 , C07J71/00 , C07D211/70 , C07D307/94
CPC分类号： C07J71/001 , C07J63/008 , C07J71/0047 , C07J71/0063
摘要： The novel D-homosteroids of the formula ##STR1## wherein R.sup.1 represents a --CN, .dbd.NOH or .dbd.CH--NHOH group; R.sup.2 represents oxo or, where R.sup.1 represents a --CN group, R.sup.2 represents oxo or a --OAc group; or R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 of the steroid skeleton represents a [2,3-d]-fused isoxazole ring, a [3,2-c]-fused pyrazole ring, a [3,2-c]-fused N-acylated pyrazole ring or a [2,3-c]-fused furazan ring; Ac represents an acyl group; R.sup.3 and R.sup.4 represent methyl and R.sup.5 and R.sup.6 together represent an additional bond between carbon atoms 5 and 6 of the steroid skeleton; or R.sup.4 and R.sup.5 together represent --O--, R.sup.3 represents hydrogen or methyl, and R.sup.6 represents hydrogen; R.sup.7 represents hydrogen, lower-alkyl or ethynyl; R.sup.8 represents hydroxy or acyloxy; or R.sup.7 and R.sup.8 together represent a spiroether group of the formula ##STR2## or a spirolactone group of the formula ##STR3## the dotted 16,17-bond is an optional additional carbon-carbon bond; and the dotted 2,3-bond is an additional carbon-carbon bond when R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 form the isoxazole or pyrazole ring or when R.sup.2 represents a --OAc group,inhibit the synthesis of progesterone in organisms and can be used for fertility control. The novel D-homosteroids can be manufactured by molecular modifications of other D-homosteroids.
摘要翻译：式中，R1表示-CN，= NOH或= CH-NHOH基团的新型D-类固醇类化合物。 R 2表示氧代，或其中R 1表示-CN基，R 2表示氧代或-OCc基; 或R 1和R 2与类固醇骨架的碳原子2和3一起代表[2,3-d] - 稠合的异恶唑环，[3,2-c] - 引入的吡唑环，[3,2-c] - 引入的N-酰化吡唑环或[2,3-c] - 呋喃环; Ac表示酰基; R3和R4表示甲基，R5和R6一起代表类固醇骨架的碳原子5和6之间的附加键; 或R 4和R 5一起表示-O-，R 3表示氢或甲基，R 6表示氢; R7表示氢，低级烷基或乙炔基; R8表示羟基或酰氧基; 或者R 7和R 8一起表示式Ia的螺醚基或式Ia的螺内酯基团，点缀的16,17-键是任选的另外的碳 - 碳键; 当R 1和R 2与碳原子2和3一起形成异恶唑或吡唑环时，或当R 2表示-OAc基团时，虚线的2,3-键是另外的碳 - 碳键，抑制生物体中孕酮的合成，用于生育控制。新型D-类固醇可以通过其他D-类固醇激素的分子修饰来制造。

68. 发明授权

US4542024A 15,16 -Methylene-17.alpha.-pregna-4,6-diene-21-carboxylic acid salts, pharmaceutical preparations containing them and a process for their production 失效
标题翻译： 15,16-亚甲基-17α-核糖-4,6-二烯-21-羧酸盐，含有它们的药物制剂及其生产方法
公开(公告)号：US4542024A
公开(公告)日：1985-09-17
申请号：US630552
申请日：1984-07-13
申请人： Klaus Nickisch , Dieter Bittler , Henry Laurent , Rudolf Wiechert , Wolfgang Losert
发明人： Klaus Nickisch , Dieter Bittler , Henry Laurent , Rudolf Wiechert , Wolfgang Losert
IPC分类号： A61K31/585 , A61P5/38 , C07J53/00 , C07J9/00 , A61K31/56
CPC分类号： C07J53/008
摘要： New 15,16-methylene-17.alpha.-pregna-4,6-diene-21-carboxylic acid salts of formula I ##STR1## wherein R.sup.1 and R.sup.2 each alone is hydrogen or together they form an additional CC bond or a methylene group,M is an alkali metal,and the methylene group in the 15,16 position is in the .alpha. or .beta. position, in addition to having a strong antialdosterone effect, have reduced antiandrogenic and progestogenic side effects.
摘要翻译：式I的新的15,16-亚甲基-17α-脯氨酸-4,6-二烯-21-羧酸盐其中R 1和R 2各自独立地为氢或一起形成额外的CC键或亚甲基，M是碱金属，除了具有强的抗醛固酮作用之外，15,16位中的亚甲基位于α或β位，具有降低的抗雄激素和孕激素副作用。

69. 发明授权

US4472310A 5.beta.-Hydroxy-.DELTA..sup.6 -steroids and process for the preparation thereof 失效
标题翻译： 5β-羟基-DTATA 6-类固醇及其制备方法
公开(公告)号：US4472310A
公开(公告)日：1984-09-18
申请号：US359713
申请日：1982-03-11
申请人： Dieter Bittler , Henry Laurent , Klaus Nickisch , Robert Nickolson , Rudolf Wiechert
发明人： Dieter Bittler , Henry Laurent , Klaus Nickisch , Robert Nickolson , Rudolf Wiechert
IPC分类号： C07J1/00 , C07J21/00 , C07J53/00 , C07J71/00
CPC分类号： C07J21/003 , C07J1/0025 , C07J53/008 , C07J71/001
摘要： The disclosure concerns 5.beta.-hydroxy-.DELTA..sup.6 -steroids of the general formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower alkyl, or the tetrahydropyranyl residue andR.sup.2, R.sup.3 individually are respectively hydrogen or jointly are methylene andX stands for oxygen, the groupings ##STR2## (wherein R.sup.4 means hydrogen or acyl) and ##STR3## (wherein R.sup.5 means hydrogen or lower alkyl) and a process for the preparation thereof by reacting corresponding 7.alpha.-chloro-5.beta.,6.beta.-epoxy steroids in an inert solvent with metallic zinc in a lower aliphatic carboxylic acid or dilute mineral acid at temperatures of between room temperature and 100.degree. C., preferably at 40.degree.-70.degree. C.The compounds producible by this method are intermediates for the preparation of 3-keto-.DELTA..sup.4 -6.beta.,7.beta.-methylene steroids constituting pharmacologically valuable compounds, for example aldosterone antagonists.
摘要翻译： PCT No.PCT / DE81 / 00111 Sec。 371日期1982年3月11日 102（e）1982年3月11日PCT PCT。公开号WO82 / 00294 日本1982年2月4日。该公开内容涉及通式为“IMAGE”的5ββ-羟基-DTATA-类固醇，其中R 1为氢，酰基，低级烷基或四氢吡喃基，R2，R3分别为氢或共同（其中R 4表示氢或酰基）和（其中R 5表示氢或低级烷基）及其制备方法，通过使相应的7α- 氯代-5β，6β-环氧类固醇在惰性溶剂中与金属锌在低级脂族羧酸或稀无机酸中在室温至100℃之间，优选40℃-70℃的温度下进行。化合物通过该方法可生产的是制备构成药理学上有价值的化合物的3-酮-TATA4-6β，7β-亚甲基甾族化合物的中间体，例如醛固酮拮抗剂。

70. 发明授权

US4464365A 11.beta.-Chloro-.DELTA..sup.15 -steroids, a process for their preparation and pharmaceutical preparations containing them 失效
标题翻译： 11β-氯-LTATA 15-类固醇，其制备方法和含有它们的药物制剂
公开(公告)号：US4464365A
公开(公告)日：1984-08-07
申请号：US485800
申请日：1983-04-18
申请人： Helmut Hofmeister , Karl Petzoldt , Klaus Annen , Henry Laurent , Rudolf Wiechert , Yukeshige Nishino
发明人： Helmut Hofmeister , Karl Petzoldt , Klaus Annen , Henry Laurent , Rudolf Wiechert , Yukeshige Nishino
IPC分类号： A61K31/565 , C07J1/00 , C07J21/00 , C12P33/12 , A61K31/56
CPC分类号： C07J1/0081 , C07J1/0059 , C07J1/0096 , C07J21/006 , C12P33/12
摘要： 11.beta.-Chloro-.DELTA..sup.15 -steroids of Formula I ##STR1## wherein R.sup.1 is hydrogen or acyl andR.sup.2 is ethynyl, chloroethynyl, or propynyl have strong progestational activity.
摘要翻译：其中R 1是氢或酰基，R 2是乙炔基，氯乙炔基或丙炔基具有很强的促进活性。

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