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1. 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。

2. 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.

3. 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。

4. 发明授权

US4446147A Azaprostacyclins, their preparation and pharmaceutical use 失效
标题翻译：阿沙普罗环素，其制备和药物用途
公开(公告)号：US4446147A
公开(公告)日：1984-05-01
申请号：US350674
申请日：1982-02-22
申请人： Norbert Schwarz , Werner Skuballa , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Norbert Schwarz , Werner Skuballa , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： A61K31/40 , A61K31/403 , A61K31/557 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/08 , C07C57/03 , C07C57/13 , C07C57/26 , C07C57/52 , C07C405/00 , C07D209/52 , C07D307/935 , C07F9/40
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0041 , C07C57/03 , C07C57/13 , C07C57/26 , C07C57/52 , C07D209/52 , C07F9/4015 , C07F9/4018
摘要： Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group.
摘要翻译：式I的阿沙普罗环素其中R 1是氢，烷基，环烷基，芳基，杂环残基或任选在苯环上被溴，苯基，烷氧基或二烷氧基取代的苯甲酰甲基残基，W是游离或官能改性的羰基或其中R8是氢或1-5个碳原子的烷基，R9是氢或易裂解的醚或酰基残基，其中OR9-基团可以是α-或β-位， R2是游离的或官能改性的羟基。

5. 发明授权

US4567195A Azaprostacyclins, their preparation and pharmaceutical use 失效
标题翻译：阿沙普罗环素，其制备和药物用途
公开(公告)号：US4567195A
公开(公告)日：1986-01-28
申请号：US591719
申请日：1984-03-21
申请人： Norbert Schwarz , Werner Skuballa , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Norbert Schwarz , Werner Skuballa , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： A61K31/40 , A61K31/403 , A61K31/557 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/08 , C07C57/03 , C07C57/13 , C07C57/26 , C07C57/52 , C07C405/00 , C07D209/52 , C07D307/935 , C07F9/40
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0041 , C07C57/03 , C07C57/13 , C07C57/26 , C07C57/52 , C07D209/52 , C07F9/4015 , C07F9/4018
摘要： Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl of 1-5 carbon atoms, or fluorine,D is alkylene of 1-2 carbon atoms which can be substituted by alkyl groups of 1-5 carbon atoms,R.sub.5 is hydrogen or alkyl of 1-2 carbon atoms or, when D is alkylene of 1 or 2 carbon atoms, R.sub.5, together with R.sub.6, represents a bond,R.sub.6 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms, whereinR.sub.6 (R.sub.7) is halogen when R.sub.7 (R.sub.6), respectively, is alkyl of 1-2 carbon atoms orR.sub.5 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms whenD and R.sub.6 together form a carbocyclic ring closed via (CH.sub.2).sub.1-3 with D as --CH
摘要翻译：式I的阿沙普罗环素其中R 1是氢，烷基，环烷基，芳基，杂环残基或任选在苯环上被溴，苯基，烷氧基或二烷氧基取代的苯甲酰甲基残基，W是游离或官能改性的羰基或其中R8是氢或1-5个碳原子的烷基，R9是氢或易裂解的醚或酰基残基，其中OR9-基团可以是α-或β-位， R2是游离的或官能改性的羟基，R 3和R 4各自独立地是氢，1-5个碳原子的烷基或氟，D是可以被1-5个碳原子的烷基取代的1-2个碳原子的亚烷基原子，R5是氢或1-2个碳原子的烷基，或当D是1或2个碳原子的亚烷基时，R5与R6一起代表键，R6和R7各自独立地是氢或1-2碳的烷基原子，其中当R 7（R 6）分别为1-2个碳原子的烷基或R 5和R 7 eac时，R 6（R 7）为卤素 h独立地为氢或1-2个碳原子的烷基，当D和R6一起形成通过（CH 2）1-3封闭的碳环，其中D为-CH 3且R 6为-CH 2 - ，当R 1为氢时，其与碱的生理上相容的盐具有有价值的药理学性质，例如降血压和支气管扩张活性。

6. 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。

7. 发明授权

US4444788A 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：US4444788A
公开(公告)日：1984-04-24
申请号：US387140
申请日：1982-06-10
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 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0041
摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.- or .beta.-position,R.sub.1 is OR.sub.2, or NHR.sub.3 wherein R.sub.3 is H or the acyl group ofa C.sub.1-15 hydrocarbon carboxylic or sulfonic acid;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--, ##STR2## wherein the OH-group in each case can be in the .alpha.- or .beta.-position, and can be etherified or esterified by tetrahydropyranyl, tetrahydrofuranyl, .alpha.-ethoxyethyl, trimethylsilyl dimethyl, tert-butylsilyl, tribenzylsilyl, acetyl, propionyl, butyryl or benzoyl;D 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 pharmacological properties.
摘要翻译：其中9-氯原子可以是α-或β-位，R1是OR2或NHR3，其中R3是H或C1-15烃羧酸或磺酸的酰基; A是-CH 2 -CH 2 - 或顺式-CH = CH-，B是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C，，其中每种情况下的OH-基团可以是四氢呋喃基，α-乙氧基乙基，三甲基甲硅烷基二甲基，叔丁基甲硅烷基，三苄基甲硅烷基，乙酰基，丙酰基，丁酰基或苯甲酰基可以醚化或酯化。 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R 4是羟基或羟基醚化或酯化如上述W所定义; R5是C1-10烃脂族基团; C1-10烃基，被芳基取代的脂族基团，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。

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

US5013758A Novel carbacyclins, processes for their preparation and their use as medicinal agents 失效
标题翻译：新型碳霉素，其制备方法及其用作药物
公开(公告)号：US5013758A
公开(公告)日：1991-05-07
申请号：US434561
申请日：1989-11-13
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Claus-Steffen Stuerzebecher , Martin Haberey , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Claus-Steffen Stuerzebecher , Martin Haberey , Ekkehard Schillinger , Michael H. Town
IPC分类号： A61K31/557 , A61P9/12 , C07C51/00 , C07C51/367 , C07C59/125 , C07C67/00 , C07C405/00 , C07D309/12
CPC分类号： C07C405/0083 , C07D309/12
摘要： (5E)-13,14,18,18,19,19-hexadehydro-3-oxa-6a-carbaprostaglandin I.sub.2 derivatives of Formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 are hydrogen or alkyl of 1-5 carbon atoms, andR.sub.5 is an alkyl group of 1-5 carbon atoms, as well as the physiologically compatible salts thereof;have pharmacologically valuable activity.
摘要翻译：（I）的（5E）-13,14,18,18,19,19-六氢-3-氧杂-10-碳前列腺素I 2衍生物其中R 1，R 2，R 3，R 4为氢或烷基， -5个碳原子，R5是1-5个碳原子的烷基，以及其生理上相容的盐; 具有药理学有价值的活动。

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