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1. 发明授权

US4532236A Certain prostacyclins and their blood-pressure-lowering and thrombocyte-aggregation-inhibiting compositions and methods 失效
公开(公告)号：US4532236A
公开(公告)日：1985-07-30
申请号：US531898
申请日：1983-07-27
申请人： Robert Nickolson , Helmut Vorbrueggen , Jorge Casals-Stenzel , Martin Haberey
发明人： Robert Nickolson , Helmut Vorbrueggen , Jorge Casals-Stenzel , Martin Haberey
IPC分类号： A61K31/34 , A61K31/557 , A61P43/00 , C07C51/09 , C07C51/38 , C07C55/32 , C07C57/52 , C07C69/533 , C07C69/593 , C07C69/65 , C07C405/00 , C07D307/935 , C07D307/937 , C07D407/00 , C07D407/12 , C07F7/18 , C07F9/40
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0033 , C07C51/09 , C07C51/38 , C07C55/32 , C07C57/52 , C07D307/937 , C07D407/12 , C07F7/1856 , C07F9/4015
摘要： Prostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 wherein R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms substituted, if desired, by halogen, aryl, C.sub.1 -C.sub.4 -alkoxy, or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue; or is the residue NHR.sub.4 wherein R.sub.4 means hydrogen, an alkanoyl residue, or an alkanesulfonyl residue of respectively 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--group,W is a ##STR2## wherein the OH-group can be respectively esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, C.sub.1 -C.sub.4 -alkoxyalkyl, or tri(C.sub.1 -C.sub.4 -alkyl)-silyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,D and E jointly mean a direct bond orD is a straight-chain or branched alkylene group of 1-5 carbon atoms,E is an oxygen atom or a direct bond,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms, a straight-chain or branched-chain alkenyl group of 2-6 carbon atoms which can be substituted by phenyl, halogen, or C.sub.1 -C.sub.4 -alkyl and, if D and E jointly represent a direct bond, is an alkynyl residue of 2-6 carbon atoms optionally substituted in the 1-position by halogen or C.sub.1 -C.sub.4 -alkyl,R.sub.5 is a hydroxy group which can be esterified with an alkanoic acid residue of 1-4 carbon atoms or which can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, alkoxyalkyl, or trialkylsilyl residue and, if R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases, and a process for the preparation thereof.The compounds exhibit blood-pressure-lowering and thrombocyte-aggregation-inhibiting activity.

2. 发明授权

US4721729A Novel carbacyclins, process for the preparation thereof, and their use as medicinal agents 失效
标题翻译：新型碳环霉素，其制备方法及其作为药剂的用途
公开(公告)号：US4721729A
公开(公告)日：1988-01-26
申请号：US702092
申请日：1985-02-08
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Robert Nickolson , Martin Haberey , Olaf Loge , Claus-Steffen Stuerzebecher
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Robert Nickolson , Martin Haberey , Olaf Loge , Claus-Steffen Stuerzebecher
IPC分类号： C07C43/14 , A61K31/557 , A61P43/00 , C07C27/00 , C07C35/31 , C07C35/52 , C07C41/00 , C07C45/00 , C07C49/24 , C07C49/255 , C07C49/76 , C07C67/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0083 , Y10S514/829
摘要： Carbacyclins of Formula I ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl, aralkyl, or heterocyclic group,Y is a keto group or a hydroxymethylene group,X is a --CH.sub.2 -- group or an oxygen atom,A is a --CH.sub.2 --CH.sub.2 --, a trans--CH.dbd.CH-- or a --C.tbd.C-- group,W is a hydroxymethylene group or a ##STR2## D is the group ##STR3## a straight-chain or branched, saturated alkylene group or unsaturated alkylene group of up to 5 carbon atoms which can optionally be substituted by 1-2 fluorine atoms,n is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.4 is hydrogen or an alkyl group and R.sub.5 is hydrogen, halogen or an alkyl group,R.sub.2 is an alkyl, cycloalkyl, aryl, or heterocyclic group, andR.sub.3 is a hydroxy group,are valuable, e.g., as cytoprotective agents.
摘要翻译：式I的卡巴菌素其中R 1是烷基，环烷基，芳基，芳烷基或杂环基，Y是酮基或羟亚甲基，X是-CH 2 - 基或氧原子，A是 -CH 2 -CH 2 - ，反式-CH = CH-或-C 3 C C基团，W是羟基亚甲基基团，或者D是基团，即直链或支链饱和亚烷基或至多5个碳原子的不饱和亚烷基，其可任选被1-2个氟原子取代，n为1,2或3，E为直接键，-C 3位C基团或-CR 4 = CR 5 - 基团，其中R 4是氢或烷基，R 5是氢，卤素或烷基，R 2是烷基，环烷基，芳基或杂环基，并且R 3是羟基，是有价值的，例如作为细胞保护剂。

3. 发明授权

US5190973A 20-alkyl-7-oxoprostacyclin derivatives useful as pharmaceuticals 失效
标题翻译：可用作药物的20-烷基-7-氧代前列环素衍生物
公开(公告)号：US5190973A
公开(公告)日：1993-03-02
申请号：US599916
申请日：1990-10-19
申请人： Robert Nickolson , Helmut Vorbrueggen , Claus S. Stuerzebecher , Martin Haberey
发明人： Robert Nickolson , Helmut Vorbrueggen , Claus S. Stuerzebecher , Martin Haberey
IPC分类号： C07C405/00 , C07D307/935 , C07D307/937
CPC分类号： C07D307/935 , C07C405/00 , C07D307/937
摘要： The invention concerns 20-alkyl-7-oxoprostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 where R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl or a heterocyclic residue, or the residue NHR.sub.4 where R.sub.4 means hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,n is 1 or 2,A is a CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--group,W is a ##STR2## or a ##STR3## wherein the OH-group can respectively be esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or etherified with a tetrahydropyranol, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms,R.sub.5 is a hydroxy group which can be esterified with an alkanoic acid residue of 1-4 carbon atoms or etherified with a tetrahydropyranyl, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue,R.sub.6 and R.sub.7 are hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms, or R.sub.6 and R.sub.7 jointly represent a trimethylene group,R.sub.8 and R.sub.9 jointly represent a linkage or hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms,and, if R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases; their production; and their use as medicinal agents.
摘要翻译：本发明涉及通式I（I）的20-烷基-7-氧代前列环素衍生物，其中R 1是残基OR 3，其中R 3表示氢或1-10个碳原子的任选被卤素，苯基，C 1 -C 4 - 烷氧基或C 1 -C 4 - 二烷基氨基; 环烷基，芳基或杂环残基，或残基NHR4，其中R4表示氢或分别为1-10个碳原子的烷酰基或烷磺酰基，n为1或2，A为CH2-CH2-，顺式-CH = CH- 或反式-CH = CH-基团，W为“IMAGE”或“IMAGE”，其中OH基团可分别用1-4个碳原子的苯甲酰基或链烷酸残基酯化，或用四氢吡喃醇醚化，四氢呋喃基，烷氧基烷基或三烷基甲硅烷基残基，其中游离或酯化的OH基可以是α或β-位，R2是1-6个碳原子的直链或支链烷基，R5是羟基，可以用1-4个碳原子的链烷酸残基酯化，或与四氢吡喃基，四氢呋喃基，烷氧基烷基或三烷基甲硅烷基残基醚化，R6和R7是氢或1-4个碳原子的直链或支链烷基，或R6和R7共同表示三亚甲基，R8和R9共同表示键或氢或1-4个碳原子的直链或支链烷基，如果R 3是氢，则其与生理上相容的碱的盐; 他们的生产; 并将其用作药剂。

4. 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。

5. 发明授权

US4029692A Steroid carboxylic acids and derivatives 失效
标题翻译：类固醇羧酸及其衍生物
公开(公告)号：US4029692A
公开(公告)日：1977-06-14
申请号：US671381
申请日：1976-03-29
申请人： Leo Alig , Robert Nickolson , Rudolf Wiechert , Andor Furst , Klaus Kieslich , Marcel Muller , Ulrich Kerb
发明人： Leo Alig , Robert Nickolson , Rudolf Wiechert , Andor Furst , Klaus Kieslich , Marcel Muller , Ulrich Kerb
IPC分类号： A61K31/185 , A61K31/19 , A61K31/21 , A61K31/215 , A61K31/22 , A61K31/56 , A61P5/38 , A61P29/00 , C07J63/00 , C12P33/02 , C07C69/74 , C07C61/36 , C07C69/16 , C07C69/28
CPC分类号： C07J63/008 , C07J63/00 , Y10S514/87 , Y10S514/93
摘要： The present disclosure relates to steroid carboxylic acids and derivatives thereof. More particularly, the disclosure is concerned with D-homosteroid carboxylic acids and their derivatives, a process for the preparation thereof and pharmaceutical compositions containing same. The instant compounds are active endocrinal agents, especially as antiinflammatory agents.
摘要翻译：本公开涉及类固醇羧酸及其衍生物。更具体地，本公开涉及D-类固醇类羧酸及其衍生物，其制备方法和含有它们的药物组合物。本发明化合物是活性内分泌剂，特别是作为抗炎剂。

6. 发明授权

US4348327A Process for the preparation of 17.alpha.-hydroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids 失效
标题翻译：制备17α-羟基和17aα-羟基-D-高聚羧酸的方法
公开(公告)号：US4348327A
公开(公告)日：1982-09-07
申请号：US276563
申请日：1981-06-23
申请人： Robert Nickolson , Ulrich Kerb , Rudolf Wiechert , Leo Alig , Andor Furst , Marcel Muller
发明人： Robert Nickolson , Ulrich Kerb , Rudolf Wiechert , Leo Alig , Andor Furst , Marcel Muller
IPC分类号： C07J3/00 , C07J41/00 , C07J63/00 , C07J9/00
CPC分类号： C07J63/008 , C07J3/005 , C07J41/0066 , C07J41/0094
摘要： 17.alpha.-hyroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids of the formula ##STR1## wherein n is 1 or 2,A is ##STR2## and R.sub.1 is H or CH.sub.3are prepared by hydrating the corresponding 17-nitriles with a mixture of a lower carboxylic acid and its anhydride in the presence of perchloric acid. The resultant 17.beta.-N-acylcarboxamide is then treated with an alkali metal hydroxide in a polyhydric alcohol at an elevated temperature. The product acids are intermediates, e.g., for the production of steroids having antiinflammatory activity.
摘要翻译：其中n为1或2的17α-羟基 - 和17α-羟基-D-高聚羧酸，其中n为1或2，A为H，并且R 1为H或CH 3是通过用相应的17-腈水解在高氯酸存在下，低级羧酸及其酸酐的混合物。然后在升高的温度下，用多元醇中的碱金属氢氧化物处理所得的17β-酰基羧酰胺。产物酸是中间体，例如用于生产具有抗炎活性的类固醇。

7. 发明授权

US4089852A Process for the preparation of 21-hydroxy-16-pregnen-20-one derivatives 失效
标题翻译：制备21-羟基-16-孕烯-20-酮衍生物的方法
公开(公告)号：US4089852A
公开(公告)日：1978-05-16
申请号：US682967
申请日：1976-05-04
申请人： Robert Nickolson
发明人： Robert Nickolson
IPC分类号： C07J1/00 , C07J13/00 , C07J17/00
CPC分类号： C07J13/005 , C07J1/0033 , C07J17/00
摘要： .DELTA..sup.16 -21-HYDROXY-20-KETO STEROIDS OF THE PREGNANE SERIES HAVING AN OTHERWISE UNSUBSTITUTED D-ring and a 13-methyl or -ethyl group, and 21-ethers and -esters thereof, are produced by reaction of a corresponding D-ring saturated 17-keto steroid with a lithium compound of the formula ##STR1## thereby converting the 17-keto group to a 17.beta.-hydroxy-20.alpha.-enol ether in which the 17.alpha.-side chain has the formula ##STR2## wherein R.sub.3 and R.sub.4 have the values given above, and, in any desired sequence, splitting off R.sub.3 and/or R.sub.4 enol ether by hydrolysis; eliminating 17.beta.-hydroxy group, preferably after acylation, with formation of a .DELTA..sup.16 -double bond; and, if desired, splitting off any blocking group.
摘要翻译：具有其他不分离的D-环和13-甲基或乙基的PREGNANE系列的DELTA 16-21-羟基-20-酮酸类固醇及其21-醚和 - 酯通过相应的D- 环状饱和的17-酮类固醇与式“IMAGE”的锂化合物反应，从而将17-酮基转化为17β-羟基-20α-烯醇醚，其中17α-侧链具有式，其中 R3和R4具有上述给出的值，并且以任何所需的顺序通过水解分离R3和/或R4烯醇醚; 消除17个β-羟基，优选在酰化后，形成DELTA16-双键; 并且如果需要，分解任何封闭基团。

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