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1. 发明授权

US4870104A 11-haloprostane derivatives, processes for their preparation and their use as medicinal agents 失效
标题翻译： 11-卤代前驱烷衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4870104A
公开(公告)日：1989-09-26
申请号：US929310
申请日：1986-11-12
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Claus-Steffen Sturzebecher , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Claus-Steffen Sturzebecher , Walter Elger
IPC分类号： C07D317/16 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D263/00 , C07D263/14 , C07D271/00 , C07D271/06 , C07D317/20 , C07D319/12 , C07D321/00 , C07D493/00 , C07D493/08
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0041 , C07D317/20
摘要： 11-Haloprostane derivatives of general formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis-CH.dbd.CH-group,B is a --CH.sub.2 --CH.sub.2 -- or trans-CH.dbd.CH-- or a --C.tbd.C-group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C-bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.
摘要翻译：其中X是F，Cl或Br，R1是残基CH 2 OH或者其中R 2表示氢原子，烷基，环烷基，芳基，苯甲酰基或杂环残基 A是-CH 2 -CH 2 - 或顺式-CH = CH-基，B是-CH 2 -CH 2 - 或反式-CH = CH-或-C 3 C C基，W是亚乙二氧基亚甲基或羟基亚甲基基团，D和E一起表示直接键合，或D表示C1-10亚烷基，E表示氧或硫原子，直接键，-C3OND C键或-CR6 = CR7-基，R6 R7表示氢原子，氯原子或烷基，R4表示羟基，R5表示氢原子，烷基，环烷基，芳基或杂环基，其盐与生理上相容的碱，工艺用于其制备，并且其用作抑制胃酸分泌的试剂。

2. 发明授权

US4284646A Prostanoic acid derivatives and their preparation 失效
标题翻译：前列腺酸衍生物及其制备
公开(公告)号：US4284646A
公开(公告)日：1981-08-18
申请号：US69193
申请日：1979-08-24
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
IPC分类号： A61K31/27 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/275 , A61P43/00 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/535 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0041 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07F9/5352
摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is an acid, ester, amide or hydroxyalkylene group; R.sub.2 and R.sub.3 are H or alkyl; R.sub.4 and R.sub.5 are both CH.sub.3 or one is Cl and the other is CH.sub.3 ; A is CH.sub.2 CH.sub.2 or --CH.dbd.CH; B is CH.sub.2 CH.sub.2, trans-CH.dbd.CH, --C.tbd.C--or ##STR2## W is free or functionally modified hydroxyalkylene or carbonyl; Z is free or functionally modified hydroxymethylene or carbonyl; X Y is either ##STR3## or, when Z is free or functionally modified hydroxymethylene, ##STR4## or, when Z is free or functionally modified carbonyl, --CH.dbd.CH--, R.sub.12 being H, CH.sub.3, CN or free or functionally modified hydroxy; and physiologically acceptable salts thereof when R.sub.1 is an acid group, possess pharmacological activity, including abortion triggering activity.
摘要翻译：其中R1是酸，酯，酰胺或羟基亚烷基的式IMA曲前酯衍生物; R2和R3是H或烷基; R4和R5都是CH3，一个是Cl，另一个是CH3; A是CH 2 CH 2或-CH = CH; B是CH 2 CH 2，反式-CH = CH，-C 3BOND C - 或W是游离或官能改性的羟基亚烷基或羰基; Z是游离的或官能改性的羟基亚甲基或羰基; 或者当Z是游离或官能改性的羟基亚甲基时，或者当Z是游离或官能改性羰基时，-CH = CH-，R 12是H，CH 3，CN或游离或官能改性的羟基 ; 当R1为酸基时，其生理上可接受的盐具有药理活性，包括流产触发活性。

3. 发明授权

US4983629A 11-haloprostane derivatives, processes for their preparation and their use as medicinal agents 失效
标题翻译： 11-卤代前驱烷衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4983629A
公开(公告)日：1991-01-08
申请号：US369168
申请日：1989-06-21
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Claus-Steffen Sturzebecher , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Claus-Steffen Sturzebecher , Walter Elger
IPC分类号： C07C405/00 , C07D317/20
CPC分类号： C07D317/20 , C07C405/00 , C07C405/0016 , C07C405/0041
摘要： 11-Haloprostane derivatives of general Formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--group,B is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH-- or a --C.tbd.C--group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C--bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.
摘要翻译：其中X是F，Cl或Br，R1是残基CH 2 OH或者其中R 2表示氢原子，烷基，环烷基，芳基，苯甲酰基或杂环残基 A是-CH 2 -CH 2 - 或顺式-CH = CH-基，B是-CH 2 -CH 2 - 或反式-CH = CH-或-C 3 C C基，W是亚乙二氧基亚甲基或羟基亚甲基基团，D和E一起表示直接键合，或D表示C1-10亚烷基，E表示氧或硫原子，直接键，-C3OND C键或-CR6 = CR7-基，R6 R7表示氢原子，氯原子或烷基，R4表示羟基，R5表示氢原子，烷基，环烷基，芳基或杂环基，其盐与生理上相容的碱，工艺用于其制备，并且其用作抑制胃酸分泌的试剂。

4. 发明授权

US4489092A Prostanoic acid derivatives and their preparation 失效
标题翻译：前列腺酸衍生物及其制备
公开(公告)号：US4489092A
公开(公告)日：1984-12-18
申请号：US413940
申请日：1982-09-01
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
IPC分类号： A61K31/27 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/275 , A61P43/00 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/535 , C07C177/00 , A61K31/557
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0041 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07F9/5352
摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is an acid, ester, amide or hydroxyalkylene group; R.sub.2 and R.sub.3 are H or alkyl; R.sub.4 and R.sub.5 are both CH.sub.3 or one is Cl and the other is CH.sub.3 ; A is CH.sub.2 CH.sub.2 or --CH.dbd.CH; B is CH.sub.2 CH.sub.2, trans-CH.dbd.CH, --C.tbd.C-- or ##STR2## W is free or functionally modified hydroxyalkylene or carbonyl; Z is free or functionally modified hydroxymethylene or carbonyl; X Y is either ##STR3## or, when Z is free or functionally modified hydroxymethylene, ##STR4## or, when Z is free or functionally modified carbonyl, --CH.dbd.CH--, R.sub.12 being H, CH.sub.3, CH or free or functionally modified hydroxy; and physiologically acceptable salts thereof when R.sub.1 is an acid group, possess pharmacological activity, including abortion triggering activity.
摘要翻译：其中R1是酸，酯，酰胺或羟基亚烷基的式IMA曲前酯衍生物; R2和R3是H或烷基; R4和R5都是CH3，一个是Cl，另一个是CH3; A是CH 2 CH 2或-CH = CH; B是CH 2 CH 2，反式-CH = CH，-C 3 D或W是游离或官能改性的羟基亚烷基或羰基; Z是游离的或官能改性的羟基亚甲基或羰基; 或者当Z是游离的或官能改性的羟基亚甲基时，或者当Z是游离的或官能改性的羰基时，-CH = CH-，R 12是H，CH 3，CH或游离或官能改性的羟基 ; 当R1为酸基时，其生理上可接受的盐具有药理活性，包括流产触发活性。

5. 发明授权

US4359467A Prostanoic acid derivatives and their preparation 失效
标题翻译：前列腺酸衍生物及其制备
公开(公告)号：US4359467A
公开(公告)日：1982-11-16
申请号：US256369
申请日：1981-04-22
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
IPC分类号： A61K31/27 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/275 , A61P43/00 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/535 , C07C177/00 , A61K31/557
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0041 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07F9/5352
摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is an acid, ester, amide or hydroxyalkylene group; R.sub.2 and R.sub.3 are H or alkyl; R.sub.4 and R.sub.5 are both CH.sub.3 or one is Cl and the other is CH.sub.3 ; A is CH.sub.2 CH.sub.2 or --CH.dbd.CH; B is CH.sub.2 CH.sub.2, trans- ##STR2## W is free or functionally modified hydroxyalkylene or carbonyl; Z is free or functionally modified hydroxymethylene or carbonyl; X Y is either ##STR3## or, when Z is free or functionally modified hydroxymethylene, ##STR4## or, when Z is free or functionally modified carbonyl, --CH.dbd.CH--, R.sub.12 being H, CH.sub.3, CN or free or functionally modified hydroxy; and physiologically acceptable salts thereof when R.sub.1 is an acid group, possess pharmacological activity, including abortion triggering activity.
摘要翻译：其中R1是酸，酯，酰胺或羟基亚烷基的式IMA曲前酯衍生物; R2和R3是H或烷基; R4和R5都是CH3，一个是Cl，另一个是CH3; A是CH 2 CH 2或-CH = CH; B是CH 2 CH 2，反式 - W是游离的或官能改性的羟基亚烷基或羰基; Z是游离的或官能改性的羟基亚甲基或羰基; 或者当Z是游离或官能改性的羟基亚甲基时，或者当Z是游离或官能改性羰基时，-CH = CH-，R 12是H，CH 3，CN或游离或官能改性的羟基 ; 当R1为酸基时，其生理上可接受的盐具有药理活性，包括流产触发活性。

6. 发明授权

US4191694A Prostaglandin-I.sub.2 derivatives 失效
标题翻译：前列腺素I2衍生物
公开(公告)号：US4191694A
公开(公告)日：1980-03-04
申请号：US928126
申请日：1978-07-26
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Bernd Muller , Gerda Mannesmann , Olaf Loge , Ekkehardt Schillinger , Jorge Casals-Stenzel
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Bernd Muller , Gerda Mannesmann , Olaf Loge , Ekkehardt Schillinger , Jorge Casals-Stenzel
IPC分类号： A61K31/557 , A61K31/34 , A61K31/343 , A61K31/5575 , A61P7/02 , A61P7/10 , A61P9/06 , A61P9/12 , A61P43/00 , C07C405/00 , C07D307/935 , C07D307/937 , C07D307/93
CPC分类号： C07D307/937 , C07C405/00 , Y10S514/821 , Y10S514/822 , Y10S514/869
摘要： Prostane derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ;R.sub.2 is hydrogen, C.sub.1-10 alkyl, C.sub.4-10 cycloalkyl, C.sub.6-10 aryl, or a 5 or 6 membered heterocyclic ring having 1-3 hetero atoms selected from O, N and S;R.sub.3 is the residue of a hydrocarbon carboxylic or sulfonic acid of 1-15 carbon atoms;W is (a) an OH-substituted methylene group, (b) a ##STR2## wherein the OH-groups in (a) or (b) can be in the .alpha.- or .beta.-position, or (c) such a group wherein the H atom of the OH group is replaced by the residue of a hydrocarbon carboxylic or sulfonic acid of 1-15 carbon atoms or by a conventional etherifying OH-blocking group;R.sub.4 is OH or hydroxy whose H atom is replaced as defined for W; andR.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 each independently is hydrogen or alkyl of 1-5 carbon atoms; or R.sub.9 and R.sub.10 together represent a direct bond; and, when R.sub.11 is alkyl, R.sub.10 can also be chlorine;and, for a derivative wherein R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases,have improved prostaglandin activity.
摘要翻译：其中R1为OR2或NHR3的式（Ⅰ）所示的前驱体衍生物; R2是氢，C1-10烷基，C4-10环烷基，C6-10芳基或具有1-3个选自O，N和S的杂原子的5或6元杂环; R3是1-15个碳原子的烃羧酸或磺酸的残基; W是（a）OH-取代的亚甲基，（b）其中（a）或（b）中的OH基可以是α或β-位，或（c）这样的基团其中OH基团的H原子被1-15个碳原子的烃羧酸或磺酸的残基或通过常规的醚化OH-封闭基团取代; R4是OH或羟基，其H原子被替换为W定义; R 5，R 6，R 7，R 8，R 9，R 10和R 11各自独立地为氢或1-5个碳原子的烷基; 或R 9和R 10一起代表直接键; 当R 11为烷基时，R 10也可为氯; 并且对于其中R 2是氢的衍生物，其与生理上相容的碱的盐具有改善的前列腺素活性。

7. 发明授权

US4789685A 9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents 失效
标题翻译： 9-氟前列腺素衍生物，其制备和用作药物
公开(公告)号：US4789685A
公开(公告)日：1988-12-06
申请号：US4733
申请日：1987-01-20
申请人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
发明人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0041
摘要： 9-fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, the physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.
摘要翻译：其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基的式I的α-氟仿烷基衍生物。或R1是残基，其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-，B是-CH2-CH2-，反式-CH = CH-或-C3BOND C，W是游离的或官能改性的羟基亚甲基，其中OH基可以是α或β位，D和E共同是直接键，或D是1-10的直链或支链亚烷基或亚链烯基可以任选被氟原子取代的碳原子，E是氧或硫，直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或烷基 R4是游离的或官能改性的羟基，R5是氢，任意取代的脂族基团，例如烷基或卤代取代的烷基，环烷基，任选被取代的芳基或杂环基，当R2是H时，生理上相容的盐具有有价值的药理学性质，例如作为骨质疏松症或流产者。

8. 发明授权

US4560786A .DELTA..sup.8,9 -Prostaglandin derivatives, their preparation and use as medicinal agents 失效
标题翻译： DELTA 8,9-前列腺素衍生物，其制备和用作药物
公开(公告)号：US4560786A
公开(公告)日：1985-12-24
申请号：US391734
申请日：1982-06-24
申请人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
发明人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
IPC分类号： A61K31/045 , A61K31/557 , A61K31/5575 , A61P25/04 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0041
摘要： .DELTA..sup.8,9 -Prostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 ; A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH;B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--W is a free or functionally modified hydroxymethylene group or free or functionally modified ##STR4## wherein the OH--group can be in the .alpha.-- or .beta.-- position; D and E jointly are a direct bond orD is straight chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen, sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine or alkyl;R.sub.4 is free or functionally modified hydroxy andR.sub.5 is an optionally substituted aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group, and when R.sub.2 is hydrogen, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g. luteolytic and abortifacient activities.
摘要翻译： DELTA 8,9-式I的前驱体衍生物其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基; 或R 1为，其中R 3为酸残基或R 2; A是-CH 2 -CH 2 - 或顺式-CH = CH; B是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3BOND C-W是游离或官能改性的羟基亚甲基或游离或官能改性的“IMAGE”，其中OH-基团可以是α或β - 位置 D和E共同是直接键合，或D是可以任选被氟原子取代的1-10个碳原子的直链或支链亚烷基或亚烯基，并且E是氧，硫，直接键，-C 3 D或 -CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自为氢，氯或烷基; R4是游离的或官能改性的羟基，R 5是任选取代的脂族基，环烷基，任选取代的芳基或杂环基，当R 2是氢时，其与碱的生理上相容的盐具有有价值的药理学性质。 luteolytic和流产活动。

9. 发明授权

US4454339A 9-Fluoroprostaglandin derivatives, and use as medicinal agents 失效
标题翻译： 9-氟前列腺素衍生物，用作药物
公开(公告)号：US4454339A
公开(公告)日：1984-06-12
申请号：US395448
申请日：1982-07-06
申请人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
发明人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0041
摘要： 9-Fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.-position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.
摘要翻译：其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基的式I的1-氟代衍生物（Ⅰ）或R1是残基，其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-，B是-CH2-CH2-，反式-CH = CH-或-C3BOND C，W是游离的或官能改性的羟基亚甲基，其中OH基可以是α-或β-位，D和E共同是直接键，或D是1-10的直链或支链亚烷基或亚烯基可以任选被氟原子取代的碳原子，E是氧或硫，直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或烷基 R4是游离的或官能改性的羟基，R5是氢，任意取代的脂族基团，例如烷基或卤代取代的烷基，环烷基，任选取代的芳基或杂环基，当R 2是H时，其生理上相容的盐具有碱性，具有有价值的药理学性质，例如作为纤溶素或流产。

10. 发明授权

US4217360A Novel 1,3-benzodioxaneprostanoic acid derivatives and process for the preparation thereof 失效
标题翻译：新型1,3-苯并二恶烷庚酸衍生物及其制备方法
公开(公告)号：US4217360A
公开(公告)日：1980-08-12
申请号：US2268
申请日：1979-01-10
申请人： Helmut Vorbrueggen , Norbert Schwarz , Olaf Loge , Walter Elger
发明人： Helmut Vorbrueggen , Norbert Schwarz , Olaf Loge , Walter Elger
IPC分类号： C07C37/62 , C07C37/66 , C07D319/08 , C07F9/655
CPC分类号： C07D319/08 , C07C37/62 , C07C37/66 , C07F9/65522
摘要： 1,3-Benzodioxaneprostanoic acid compound of the formula ##STR1## wherein R.sub.1 is hydroxy, alkoxy of 1-10 carbon atoms, methylsulfamido, substituted or unsubstituted aryloxy, or O--CH.sub.2 --U--V wherein U is a direct bond, carbonyl, or carbonyloxy, and V is phenyl or phenyl substituted, e.g. by one or more of phenyl, phenoxy, alkoxy of 1-2 carbon atoms, and halogen; A is --CH.sub.2 --CH.sub.2 -- or trans --CH.dbd.CH--; B is --CH.sub.2 --CH.sub.2 -- or cis- or trans--CH.dbd.CH--; Z is hydroxymethylene or carbonyl; X Y, if Z is hydroxymethylene, is ##STR2## or, if Z is carbonyl, is ##STR3## or --CH.dbd.CH--; R.sub.2 is hydrogen or alkyl of 1-5 carbon atoms; R.sub.3 and R.sub.4 each are H, F, Cl, Br, I or CF.sub.3, CH.sub.3 or alkoxy of 1-2 carbon atoms or R.sub.3 and R.sub.4 in 6-,7-position is methylendioxy; and if R.sub.1 is hydroxy, salts thereof with pharmaceutically acceptable bases, are agents for inducing menstruation, interrupting pregnancy, inducing labor and synchronizing the sexual cycle in female mammals.
摘要翻译：其中R1是羟基，1-10个碳原子的烷氧基，甲基亚磺酰氨基，取代或未取代的芳氧基或O-CH2-UV，其中U是直接键，羰基或羰基氧基的1,3-苯并二恶烷庚酸化合物，和V是苯基或苯基取代的，例如苯基，苯氧基，1-2个碳原子的烷氧基和一个或多个卤素; A是-CH 2 -CH 2 - 或反-CH = CH-; B是-CH 2 -CH 2 - 或顺式 - 或反式-CH = CH-; Z是羟基亚甲基或羰基; 如果Z是羟基亚甲基，X Y是或者如果Z是羰基，则是Y或CH = CH-; R2是氢或1-5个碳原子的烷基; R3和R4各自为H，F，Cl，Br，I或CF3，CH3或1-2个碳原子的烷氧基或6-7位的R3和R4是甲氧基; 并且如果R 1是羟基，则其盐与药学上可接受的碱，是诱导雌性哺乳动物诱发月经，中断怀孕，诱导劳动和同步性循环的药剂。

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