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1. 发明授权

US4497830A Carbacyclins, their preparation and pharmacological use 失效
标题翻译：卡巴菌素，其制备和药理学用途
公开(公告)号：US4497830A
公开(公告)日：1985-02-05
申请号：US381609
申请日：1982-05-24
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Gerda Mannesmann , Bob Nieuweboer
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Gerda Mannesmann , Bob Nieuweboer
IPC分类号： A61K31/557 , A61P43/00 , C07C29/147 , C07C33/05 , C07C33/12 , C07C41/26 , C07C43/178 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40
CPC分类号： C07D317/72 , C07C33/12 , C07C405/0083 , C07C43/178 , C07D309/12 , C07F9/4015
摘要： Compounds of Formula I ##STR1## wherein X is oxygen or CH.sub.2 ;A is CH.sub.2 --CH.sub.2, trans-CH.dbd.CH or C.tbd.C;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## and the OH groups may be in the .alpha.- or the .beta.-position; D is straight chain or branched, saturated or unsaturated hydrocarbon aliphatic of from 1 to 10 carbon atoms, which may be substituted by fluorine;E is C.tbd.C or CR.sub.3 .dbd.CR.sub.4, R.sub.3 and R.sub.4 being different and being hydrogen or alkyl of 1 to 5 carbon atoms;R.sub.1 is free or functionally modified hydroxy; andR.sub.2 is alkyl, cycloalkyl, optionally substituted aryl or heterocyclic,have valuable pharmacological properties, e.g., hypotensive and bronchodilatory characteristics. They can furthermore be used for prophylaxis and therapy of coronary infarct and as a treatment for stroke. They are produced by means of reduction of the corresponding 1-carbonic acid derivatives.
摘要翻译：式I的化合物其中X是氧或CH 2; A是CH 2 -CH 2，反式-CH = CH或C 3 C; W是游离或官能改性的羟基亚甲基或游离或功能修饰的“IMAGE”，OH基可以是α或β位; D是可以被氟取代的具有1至10个碳原子的直链或支链，饱和或不饱和的烃脂族; E为C 3或C 3或CR 3 = CR 4，R 3和R 4不同，为氢或1至5个碳原子的烷基; R1是游离或官能改性的羟基; 和R2是烷基，环烷基，任选取代的芳基或杂环，具有有价值的药理学性质，例如降血压和支气管扩张特征。它们还可用于冠状动脉梗塞的预防和治疗以及中风治疗。它们是通过还原相应的1-碳酸衍生物生产的。

2. 发明授权

US4378370A Certain 5-cyano-16-fluoro-prostacyclins and their use as pharmaceuticals 失效
标题翻译：某些5-氰基-16-氟前列环素及其作为药物的用途
公开(公告)号：US4378370A
公开(公告)日：1983-03-29
申请号：US309967
申请日：1981-10-06
申请人： Helmut Vorbrueggen , Bernd Raduechel , Werner Skuballa , Gerda Mannesmann , Jorge Casals-Stenzel , Ekkehard Schillinger
发明人： Helmut Vorbrueggen , Bernd Raduechel , Werner Skuballa , Gerda Mannesmann , Jorge Casals-Stenzel , Ekkehard Schillinger
IPC分类号： C07D307/935 , A61K31/34 , A61K31/557 , A61P43/00 , C07D307/93 , C07D307/937 , C07F7/18
CPC分类号： C07D307/937 , C07F7/1856 , Y10S514/826
摘要： Prostacyclin derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.3 wherein R.sub.3 is hydrogen or alkyl of 1-10 carbon atoms, or R.sub.1 is NHR.sub.4 wherein R.sub.4 is alkanoyl or alkanesulfonyl,B is alkylene of 1-5 carbon atoms,A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--,W is hydroxymethylene or ##STR2## wherein the OH-group is optionally substituted by alkanoyl of 1-4 carbon atoms and the free or substituted OH-group can be in the .alpha.- or .beta.- position,R.sub.2 is alkyl of 1-6 carbon atoms optionally substituted by phenyl, or R.sub.2 is phenyl,R.sub.5 is hydroxy optionally substituted by alkanoyl of 1-4 carbon atoms,R.sub.6 is hydrogen, fluorine, or alkyl of 1-4 carbon atomsor when R.sub.3 is hydrogen, a salt thereof with a physiologically compatible base,have pharmacological activity e.g., blood pressure-lowering and bronchodilatory effects.
摘要翻译： PCT No.PCT / DE81 / 00031 Sec。 371日期1981年10月6日 102（e）日期1981年10月6日PCT提交1981年2月5日PCT公布。出版物WO81 / 02296 日本1981年8月20日。其中R 1为OR 3的式（I）其中R 3为氢或1-10个碳原子的烷基，或R 1为NHR 4，其中R 4为烷酰基或链烷磺酰基，B为1- 5个碳原子，A是-CH 2 -CH 2 - ，顺式-CH = CH-或反式-CH = CH-，W是羟基亚甲基或其中OH基任选被1-4个碳原子的烷酰基取代并且游离或取代的OH基团可以在α或β位，R 2是任选被苯基取代的1-6个碳原子的烷基，或者R 2是苯基，R 5是任选被1-4碳的烷酰基取代的羟基原子，R6是氢，氟或1-4个碳原子的烷基，或当R3是氢时，其与生理上相容的碱的盐具有药理活性，例如降血压和支气管扩张作用。

3. 发明授权

US4954524A Carbacylcins, their preparation and use as medicinal agents 失效
标题翻译：肉桂胆碱，其制备和用作药剂
公开(公告)号：US4954524A
公开(公告)日：1990-09-04
申请号：US333812
申请日：1989-04-06
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Gerda Mannesmann , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Gerda Mannesmann , Ekkehard Schillinger , Michael H. Town
IPC分类号： A61K31/16 , A61K31/19 , A61K31/535 , A61K31/5375 , A61P7/02 , A61P9/12 , A61P11/08 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/10 , C07C231/12 , C07C233/21 , C07C235/06 , C07C235/08 , C07C235/14 , C07C235/16 , C07C235/30 , C07C405/00 , C07D295/18 , C07H13/04
CPC分类号： C07H13/04 , C07C405/0083
摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen or OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2,n is 2, 3, 4, or 5,X is hydrogen or fluorine,A 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 a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position, D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms, a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms, all of which can optionally be substituted by fluorine atoms,m is 1, 2, or 3,E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are different from each other and are hydrogen or alkyl or 1-5 carbon atoms, or are hydrogen or halogen,R.sub.4 is an aliphatic group, cycloalkyl, or optionally substituted aryl, or a heterocyclic group; andR.sub.5 is a free or functionally modified hydroxy group; andwhen R.sub.1 is OH, the salts thereof with physiologically compatible bases, have valuable pharmacological properties.

4. 发明授权

US5157042A 3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents 失效
标题翻译： 3-OXA-5-FLOORO-CARBACYCLINS，其制备和用作药物代理
公开(公告)号：US5157042A
公开(公告)日：1992-10-20
申请号：US713002
申请日：1991-06-10
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Gerda Mannesmann , Michael H. Town
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Gerda Mannesmann , Michael H. Town
IPC分类号： C07C69/708 , A61K31/225 , A61K31/35 , A61K31/351 , A61K31/557 , A61P7/02 , A61P9/12 , A61P11/08 , C07C51/00 , C07C51/367 , C07C59/125 , C07C59/62 , C07C67/00 , C07C67/31 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/06 , C07C235/08 , C07C235/88 , C07C405/00 , C07D309/12 , C07D317/72
CPC分类号： C07D317/72 , C07C405/0083
摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2 ;A 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 a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms; or a branched, saturated or straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms; all of which are substituted by fluorine atoms;n is 1, 2, or 3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.7 is hydrogen, halogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group; andR.sub.5 is a free or functionally modified hydroxy group; andwhen R.sub.1 is OH, the salts thereof with physiologically compatible bases,are valuable pharmacological agents.
摘要翻译：式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，烷基，环烷基，芳基，杂芳基或杂环残基; 或R1是NHR3，其中R3是酸残基（酰基）或R2; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位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基可以是α-或β-位; D是1-10个碳原子的直链饱和脂族基团; 或2-10个碳原子的支链，饱和或直链或支链的不饱和脂族基团; 所有这些都被氟原子取代; n为1,2或3; E是直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6是氢或1-5个碳原子的烷基，R 7是氢，卤素或1-5个碳原子的烷基; R4是脂族基团，环烷基，任选取代的芳基或杂环基; R5是游离或官能改性的羟基; 当R1是OH时，其与生理上相容的碱的盐是有价值的药剂。

5. 发明授权

US4618626A Novel carbacyclin esters, process for the preparation thereof, and their use as medicinal agents 失效
标题翻译：新型卡巴环素酯，其制备方法及其作为药剂的用途
公开(公告)号：US4618626A
公开(公告)日：1986-10-21
申请号：US777535
申请日：1985-09-16
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Gerda Mannesmann , Bob Nieuweboer , Michael-Harold Town
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Gerda Mannesmann , Bob Nieuweboer , Michael-Harold Town
IPC分类号： C07C69/708 , A61K31/557 , A61P1/04 , A61P9/08 , A61P9/12 , A61P11/08 , C07C67/10 , C07C69/732 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0083
摘要： Carbacyclin esters of Formula I ##STR1## wherein R.sub.1 is an unsubstituted or substituted aromatic residue,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 is an alkyl or cycloalkyl group, or an optionally substituted aryl group, or a heterocyclic group,X is an oxygen atom or the group --CH.sub.2 --,A is a --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--group,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position D is the group ##STR3## a straight-chain saturated alkylene group of 1-5 carbon atoms, a branched, saturated or a straight-chain or branched, unsaturated alkylene group of 2-5 carbon atoms, which groups can optionally be substituted by fluorine atoms,E is a direct bond, a --C.tbd.C--group, or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.2 and R.sub.5 mean a hydrogen atom or an alkyl group of 1-5 carbon atoms;are useful as blood-pressure-lowering agents, inter alia.
摘要翻译：式I的卡巴环素酯其中R 1是未取代或取代的芳族残基，R 2是游离或官能改性的羟基，R 3是烷基或环烷基，或任选取代的芳基或杂环基，X是氧原子或基团-CH 2 - ，A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3 C C基，W是游离或官能改性的羟基亚甲基，功能修饰的“IMAGE”，其中OH基可以在α或β位D是基团，即1-5个碳原子的直链饱和亚烷基，支链，饱和或直链或2-5个碳原子的支链不饱和亚烷基，该基团可任选被氟原子取代，E是直接键，-C 3 C C基或-CR 4 = CR 5 - 基，其中R 2和R 5表示氢原子或1-5个碳原子的烷基; 作为降血压剂特别有用。

6. 发明授权

US4552875A Novel carbacyclinamides, their preparation and use as medicinal agents 失效
标题翻译：新型卡巴胆碱，其制备和用作药物
公开(公告)号：US4552875A
公开(公告)日：1985-11-12
申请号：US510125
申请日：1983-07-01
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Gerda Mannesmann , Bob Nieuweboer , Michael H. Town
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Gerda Mannesmann , Bob Nieuweboer , Michael H. Town
IPC分类号： A61K31/16 , A61K31/19 , A61K31/535 , A61K31/5375 , A61P7/02 , A61P9/12 , A61P11/08 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/10 , C07C231/12 , C07C233/21 , C07C235/06 , C07C235/08 , C07C235/14 , C07C235/16 , C07C235/30 , C07C405/00 , C07D295/18 , C07H13/04 , C07C177/00 , A61K31/557
CPC分类号： C07H13/04 , C07C405/0083
摘要： Carbacyclinamides of Formula I ##STR1## wherein R.sub.1 is NHR.sub.4, wherein R.sub.4 is H, --(CH.sub.2).sub.n --R.sub.8 or straight-chained or branched aliphatic groups of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 each are straight-chained or branched, lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.4 and R.sub.5 together with the adjoining N-atom form a 5- or 6-membered heterocycle which can optionally contain additional hetero atoms and can be substituted; or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 is an aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, and R.sub.5 is straight-chained or branched aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms;n is 1-4;R.sub.8 is --CONH.sub.2 or --N(C.sub.1 -C.sub.4 -alkyl).sub.2 ;R.sub.2 is a free or functionally modified hydroxy group;R.sub.3 is aliphatic, cycloalkyl, optionally substituted aryl, or a heterocyclic group;X is oxygen or --CH.sub.2 --;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --CH.tbd.--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR3## a straight-chain, saturated aliphatic group of 1-5 carbon atoms, or a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-5 carbon atoms, all of which groups can optionally be substituted by fluorine atoms;m is 1-3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --wherein R.sub.6 and R.sub.7 are each a hydrogen atom or an alkyl group of 1-5 carbon atomshave valuable pharmacological properties.
摘要翻译：式I的卡拉菌素酰胺其中R 1是NHR 4，其中R 4是H， - （CH 2）n -R 8或1-10个碳原子的直链或支链脂族基团，3-10个碳原子的环烷基，芳基或2-8个碳原子的低级单 - 或多羟基烷基，或R1是NR4R5，其中R4和R5各自是2-8个碳原子的直链或支链，低级，单 - 或多羟基烷基，或R4和R5连同邻接的N-原子形成5-或6-元杂环，其可以任选地含有另外的杂原子并且可以被取代; 或R1是NR4R5，其中R4是1-10个碳原子的脂族基团，3-10个碳原子的环烷基，R5是1-10个碳原子的直链或支链脂族基团，3-10个碳原子的环烷基，芳基或更低级的2-8个碳原子的单或多羟基烷基; n为1-4; R8是-CONH2或-N（C1-C4-烷基）2; R2是游离或官能改性的羟基; R3是脂族，环烷基，任选取代的芳基或杂环基; X是氧或-CH 2 - ; A是-CH 2 -CH 2 - ，反式-CH = CH-或-CH 3 OCH 3 - 。 W是游离的或官能改性的羟基亚甲基或游离或功能改性的“IMAGE”，其中OH-基团可以是α-或β-位; D是1-5个碳原子的直链饱和脂族基团，或2-5个碳原子的支链，饱和或直链或支链不饱和脂肪族基团，所有这些基团可任选地为被氟原子取代; m为1-3; E是直接键，-C 3 D或-CR 6 = CR 7 - 其中R 6和R 7各自为氢原子或1-5个碳原子的烷基具有有价值的药理学性质。

7. 发明授权

US4315013A Certain pyrrole analogs of prostacyclin derivatives 失效
标题翻译：某些前列环素衍生物的吡咯类似物
公开(公告)号：US4315013A
公开(公告)日：1982-02-09
申请号：US122794
申请日：1980-02-19
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
IPC分类号： A61K31/40 , A61K31/403 , A61K31/557 , A61K31/5585 , A61P7/02 , A61P9/12 , A61P11/08 , A61P43/00 , C07C405/00 , C07D209/52 , A61K31/435 , C07D401/12 , C07D405/12
CPC分类号： C07D209/52 , C07C405/00 , C07C405/0041
摘要： Prostane derivatives of the formula ##STR1## wherein R.sub.1 is (a) hydrogen, (b) C.sub.1-10 alkyl, (c) C.sub.1-10 alkyl substituted by halogen; C.sub.1-4 alkoxy; C.sub.6-10 aryl; C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; di-C.sub.1-4 -alkylamino; or tri-C.sub.1-4 alkylammonium; (d) C.sub.4-10 cycloalkyl, (e) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (f) C.sub.6-10 aryl, (g) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S;W is hydroxymethylene or RO-methylene; or ##STR2## wherein OH or OR is in the .alpha.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently hydrogen or alkyl of 1-5 carbon atoms,R.sub.2 is OH or OR, R being as defined above,or, when R.sub.1 is H, a physiologically compatible salt thereof with a base.
摘要翻译：其中R 1为（a）氢，（b）C 1-10烷基，（c）被卤素取代的C 1-10烷基; C 1-4烷氧基; C6-10芳基; 被1-3个卤素原子取代的C 6-10芳基，苯基，1-3个C 1-4烷基或氯甲基，氟甲基，三氟甲基，羧基，羟基或C 1-4烷氧基; 二-C 1-4 - 烷基氨基; 或三-C 1-4烷基铵; （d）C 4-10环烷基，（e）被C 1-4烷基取代的C 4-10环烷基，（f）C 6-10芳基，（g）被1-3个卤素原子取代的C 6-10芳基，苯基， -3 C 1-4烷基或氯甲基，氟甲基，三氟甲基，羧基，羟基或C 1-4烷氧基，或（h）5或6个环原子的芳族杂环，其中一个为O，N或S; W是羟基亚甲基或RO-亚甲基; 或其中OH或OR位于α位且R是体内可水解和生理上可接受的醚或酰基，其是常规用于改变前列腺素中的OH基团; R 3，R 4，R 5和R 6各自独立地是氢或1-5个碳原子的烷基，R 2是OH或OR，R如上定义，或者当R 1是H时，其与碱的生理上相容的盐。

8. 发明授权

US5079259A Pharmaceutically active 9-chloroprostaglandins 失效
标题翻译：药物活性9氯罗丹明
公开(公告)号：US5079259A
公开(公告)日：1992-01-07
申请号：US96232
申请日：1987-09-08
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00
CPC分类号： C07C405/00 , C07C405/0041
摘要： A 9-chloroprostane of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha. or .beta.-position and R.sub.1, R.sub.4, R.sub.5, A, B, W, D and E are as described hereinafter which are useful as medical agents.

9. 发明授权

US4827017A Novel carbacyclins, processes for their production and their use as medicinal agents 失效
标题翻译：新型碳霉素，其生产工艺及其作为药剂的使用
公开(公告)号：US4827017A
公开(公告)日：1989-05-02
申请号：US21102
申请日：1987-03-03
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Ekkehard Schillinger , Claus-Steffen Stuerzebecher
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Ekkehard Schillinger , Claus-Steffen Stuerzebecher
IPC分类号： C07D309/12 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/12 , A61P11/08 , A61P43/00 , C07C45/00 , C07C49/835 , C07C51/00 , C07C65/19 , C07C67/00 , C07C69/76 , C07C69/773 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0083
摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2 wherein R.sub.2 is hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.6 -C.sub.10 -aryl, ##STR2## or a heterocyclic residue, or R.sub.1 is R.sub.3 wherein R.sub.3 is C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.6 -C.sub.10 -aryl, C.sub.7 -C.sub.14 -aralkyl or a heterocyclic residue,A 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 a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position, D is ##STR4## a straight-chain, saturated alkylene group of 1-10 carbon atoms, or a branched, saturated or a straight-chain or branched, unsaturated alkylene group of 2-10 carbon atoms, each of which can optionally by substituted by fluorine atoms,n is the number 1, 2 or 3,E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and one is hydrogen and the other alkyl of 1-5 carbon atoms, or one is hydrogen and the other is halogen, orE can also be --CH.sub.2 CH.sub.2 -- when R.sub.1 is R.sub.3,R.sub.4 is C.sub.1-10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, optionally substituted C.sub.6 -C.sub.10 -aryl or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy group and, when R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases;are useful as medicinal agents.
摘要翻译：式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，C 6 -C 10 - 芳基，或者杂环残基，或者R 1是R 3 其中R 3是C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，C 6 -C 10 - 芳基，C 7 -C 14 - 芳烷基或杂环残基，A是-CH 2 -CH 2 - ，反式-CH = CH-或-C - ，W是游离或官能改性的羟基亚甲基或游离的或功能上被修饰的“IMAGE”，其中OH基可以是α或β-位，D是直链，饱和的亚烷基 1-10个碳原子，或2-10个碳原子的支链，饱和或直链或支链不饱和的亚烷基，其各自可任选被氟原子取代，n为数1,2或3， E是-C 3位C或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，一个是氢，1-5个碳原子的另一个烷基，或一个是氢，另一个是卤素，或者也可以是当R 1为R 3，R 4为C 1-10时为-CH 2 CH 2 - 烷基，C 3 -C 10 - 环烷基，任选取代的C 6 -C 10 - 芳基或杂环基，R 5是游离或官能改性的羟基，并且当R 2是氢时，其与生理上相容的碱的盐; 作为药剂有用。

10. 发明授权

US5204371A Pharmaceutically active 9-chloroprostaglandins 失效
标题翻译：药用活性9-氯前列腺素
公开(公告)号：US5204371A
公开(公告)日：1993-04-20
申请号：US792574
申请日：1991-11-15
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
IPC分类号： C07C405/00
CPC分类号： C07C405/0041 , C07C405/00
摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.-or .beta.-position,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 --CH.tbd.C--, W is hydroxymethylene orD and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacologoical properties.
摘要翻译：其中9-氯原子可以是α-或β-位的式为“IMAGE”的化合物，A为-CH 2 -CH 2 - 或顺式-CH = CH-，B为-CH 2 -CH 2， - ， CH = CH-或-CH 3 B - ，W是羟基亚甲基或D和E一起代表直接键，或D是1-10个碳原子的直链或支链亚烷基，任选被氟取代，E是氧或硫或直接键，并且R4是如上定义的羟基或羟基醚化或酯化; R5是C1-10烃脂族基团; 被芳基取代的C1-10烃脂族基，对上述R2定义的取代芳基或卤素; 或环烷基，取代的环烷基，芳基，取代的芳基或芳族杂环，全部如上述R2所定义; 或其生理上可接受的盐，当R1为OH时，具有有价值的药理学性质。

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