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81. 发明授权

US5093250A Process for producing optically active bicyclo[3.3.0]octanedione carboxylic acid esters 失效
标题翻译：生产光活性双酚（3.3.0）十八烷酸羧酸酯的方法
公开(公告)号：US5093250A
公开(公告)日：1992-03-03
申请号：US237113
申请日：1988-07-13
申请人： Karl Petzoldt , Werner Skuballa
发明人： Karl Petzoldt , Werner Skuballa
IPC分类号： C12P7/62 , C12P17/02 , C12P41/00
CPC分类号： C12P17/02 , C12P41/00 , C12P7/62
摘要： Claimed is a process for the production of optically active bicyclo[3.3.0]octanedione-carboxylic acid esters of Formula I ##STR1## wherein R.sub.1 and R.sub.2 jointly represent an oxygen atom, orR.sub.1 and R.sub.2 individually represent the residue OR.sub.4 where R.sub.4 means methyl- or ethyl-, andR.sub.3 is a straight or branched-chain alkyl group of 1-3 carbon atoms,comprising enantioselectively saponifying and decarboxylating with .alpha.-chymotrypsin an optically inactive, prochiral bicyclo[3.3.0]octanedionedicarboxylic acid diester of Formula II ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 have the meanings set forth above, and recovering a compound of Formula I.
摘要翻译： PCT No.PCT / DE87 / 00518 Sec。 371日期：1988年7月13日 102（e）日期1988年7月13日PCT提交1987年11月12日PCT公布。出版物WO88 / 03569 日期：1988年5月19日.Claimed是制备式I的光学活性双环[3.3.0]辛二酮 - 羧酸酯的方法，其中R1和R2共同代表氧原子，或R1和R2 独立地表示残基OR4，其中R 4表示甲基或乙基，R 3是1-3个碳原子的直链或支链烷基，其包括用α-胰凝乳蛋白酶对光选择性皂化和脱羧，其是光学无活性的前手性双环[3.3。 0]辛二酸二羧酸二酯其中R1，R2和R3具有上述含义，并回收式I化合物。

82. 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。

83. 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.

84. 发明授权

US4912251A Process for manufacturing symmetrical diesters of bicyclo[3.3.0]-octanedione dicarboxylic acid 失效
标题翻译：双环[3.3.0]辛二酮二羧酸的对称二酯的制备方法
公开(公告)号：US4912251A
公开(公告)日：1990-03-27
申请号：US328197
申请日：1989-03-17
申请人： Werner Skuballa
发明人： Werner Skuballa
IPC分类号： C07C67/343 , A61K31/215 , C07C49/707 , C07C49/753 , C07C69/716 , C07C69/757
CPC分类号： C07C67/343 , C07C2102/22
摘要： The invention concerns a process for manufacturing diesters of bicyclo[3.3.0]-octane dicarboxylic acid having general formula (I), where R.sub.1 is a straight-chain or branched-chain alkyl group with 1 to 10 C atoms. The process is charaterized by the fact that a 2-cyclopentenone derivative having general formula (III), where R.sub.2 is a hydrogen atom or a straight-chain or branched-chain alkyl group with 1 to 10 C atoms, which can be substituted, if necessary, by a phenyl group, is converted in the presence of a base with a diester of aceton dicarboxylic acid having formula (IV), where R.sub.1 has the meaning given above.
摘要翻译： PCT No.PCT / DE88 / 00414 Sec。 371日期：1989年3月17日 102（e）日期1989年3月17日PCT提交1988年7月1日PCT公布。公开号WO89 / 00555 日本1989年1月26日。本发明涉及一种制备具有通式（I）的双环[3.3.0] - 辛烷二羧酸二酯的方法，其中R 1为具有1至10个碳原子的直链或支链烷基 C原子。该方法的特征在于具有通式（III）的2-环戊烯酮衍生物，其中R 2是氢原子或具有1至10个C原子的直链或支链烷基，其可被取代，如果必需的苯基在碱的存在下用具有式（IV）的丙酮二羧酸的二酯转化，其中R 1具有上面给出的含义。

85. 发明授权

US4886788A Cyclodextrin clathrates of carbacyclin derivatives and their use as medicinal agents 失效
标题翻译：碳环糊精衍生物的环糊精包合物及其作为药物的用途
公开(公告)号：US4886788A
公开(公告)日：1989-12-12
申请号：US23506
申请日：1987-03-09
申请人： Werner Skuballa , Helmut Vorbrueggen , Helmut Dahl , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Werner Skuballa , Helmut Vorbrueggen , Helmut Dahl , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C59/46 , A61K31/557 , A61K47/48 , A61P7/02 , A61P9/12 , A61P11/08 , A61P43/00 , C07C51/00 , C07C51/347 , C07C59/125 , C07C59/62 , C07C67/00 , C07C69/732 , C07C405/00 , C07D521/00 , C08B37/00 , C08B37/16
CPC分类号： B82Y5/00 , A61K47/48969 , C07C405/0083 , C08B37/0015
摘要： Cyclodextrin clathrates of carbacyclin analogs of general Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkenyl of up to 10 carbon atoms,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 ##STR3## alkylene, or unsaturated alkylene each of which can optionally be substituted by fluorine atoms,m is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group, or --CR.sub.4 .dbd.CR.sub.5 -- group, wherein R.sub.4 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen, halogen, or an alkyl group of 1-5 carbon atoms,R.sub.2 is alkyl or alkenyl of up to 10 carbon atoms, cycloalkyl of 3-10 carbon atoms or an optionally substituted aryl group of 6-10 carbon atoms, or a heterocyclic group, andR.sub.3 is a free or functionally modified hydroxy group,n is 1, 2, 3, 4 or 5, andX is --CH.sub.2 -- or oxygenas valuable crystalline pharmaceuticals.
摘要翻译：通式Ⅰ的碳霉酸类似物的环糊精包合物其中R 1是氢，至多10个碳原子的烷基或链烯基，A是-CH 2 CH 2 - ，反式-CH = CH-或-C 3位C- 基团，W是游离或官能改性的羟基亚甲基基团或游离或官能改性的“IMAGE”，其中OH基团可以在α或β-位，D是亚烷基，或不饱和亚烷基，其各自可以任选被氟原子取代，m为1,2或3，E为直接键，-C 3位C基或-CR 4 = CR 5 - 基，其中R 4为氢或1-5碳烷基原子，R5为氢或1-5个碳原子的烷基，R5为氢，卤素或1-5个碳原子的烷基，R2为至多10个碳原子的烷基或烯基，环烷基为3 -10个碳原子或任选取代的6-10个碳原子的芳基或杂环基，R3是游离或官能改性的羟基，n是1,2,3,4或5，X是-CH 2 - 或氧作为有价值的结晶药物。

86. 发明授权

US4692464A Novel prostacyclin derivatives and a process for the preparation thereof 失效
公开(公告)号：US4692464A
公开(公告)日：1987-09-08
申请号：US352411
申请日：1982-02-26
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
IPC分类号： C07D309/12 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61P7/02 , A61P25/02 , A61P43/00 , C07C45/59 , C07C45/67 , C07C45/71 , C07C51/00 , C07C51/353 , C07C59/46 , C07C62/32 , C07C67/00 , C07C67/343 , C07C69/732 , C07C401/00 , C07C405/00 , C07D317/72 , C07D319/12 , C07C177/00
CPC分类号： C07D317/72 , A61K31/557 , C07C405/0083 , C07C45/59 , C07C45/673 , C07C45/71 , C07C62/32 , C07D319/12
摘要： Compounds 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;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--;W is hydroxymethylene, RO-methylene, CH.sub.3 or CH.sub.3, ##STR2## wherein OH or OR is in the .alpha.- or .beta.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;D and E together are a direct bond, orD is C.sub.1-10 alkylene, C.sub.1-10 alkenylene or C.sub.1-10 alkynylene or one of these groups substituted by fluorine, andE is oxygen, --C.tbd.C-- or a direct bond;R.sub.2 is (a) a C.sub.1-10 hydrocarbon aliphatic radical, (b) a C.sub.6-10 hydrocarbon aliphatic radical substituted by C.sub.6-10 aryl or by 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; (c) C.sub.4-10 cycloalkyl, (d) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (e) C.sub.6-10 aryl, (f) 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; andR.sub.3 is OH or OR; and, when R.sub.1 is hydrogen, the salts thereof with physiologically compatible bases, are effective as antihypertensive, bronchiodilators, thrombocyte aggregation inhibitors, inter alia.

87. 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。

88. 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。

89. 发明授权

US4364950A 5-Cyano-prostacyclin derivatives and use as medicines 失效
标题翻译： 5-Cyano-prostacyclin衍生物用作药物
公开(公告)号：US4364950A
公开(公告)日：1982-12-21
申请号：US317621
申请日：1981-11-02
申请人： Werner Skuballa , Helmut Vorbruggen , Bernd Raduchel , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Helmut Vorbruggen , Bernd Raduchel , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： A61K31/557 , A61P7/02 , A61P9/12 , A61P11/08 , A61P43/00 , C07D307/935 , C07D307/937 , C07F7/18 , C07F9/40
CPC分类号： C07D307/935 , C07D307/937 , C07F7/1856 , C07F9/4015
摘要： 5-cyano-prostacyclins of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ; R.sub.2 and R.sub.3 each independently is (a) H, (b) C.sub.1-10 -alkyl, (c) C.sub.1-10 -alkyl substituted by halo, C.sub.1-4 -alkoxy or phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted as defined below, (d) C.sub.4-10 -cycloalkyl, (e) C.sub.4-10 -cycloalkyl substituted by C.sub.1-4 -alkyl, (f) phenyl, 1-naphthyl or 2-naphthyl, (g) phenyl, 1-naphthyl or 2-naphthyl substituted by 1-3 halogen atoms, phenyl, 1-3 alkyl groups of 1-4 C atoms each, or a chloromethyl-, fluoromethyl-, trifluoromethyl-, carboxyl-, hydroxy- or alkoxy-group of 1-4 C atoms, or (h) an aromatic, 5- or 6-membered heterocyclic ring containing one hetero atom which is O, N or S, the remaining atoms being carbon; R.sub.3 also possibly being an acyl group of a C.sub.1-15 -hydrocarbon carboxylic or sulfonic acid;B is straight chain or branched alkylene of 2-10 C atoms;W is hydroxymethylene or ##STR2## wherein the OH group may be in the alpha or beta position, and is optionally modified by replacement of the H atom of the OH with an ether or acyl group which is conventional for such replacements in prostaglandins and which is readily cleavable at physiological pH's;R.sub.4 is hydroxy, optionally modified as described for W above;R.sub.5, R.sub.6, R.sub.7 and R.sub.8 each independently is hydrogen, alkyl of 1-5 C atoms or methoxy; andR.sub.9 is alkyl of 1-5 C atoms orfor compounds wherein R.sub.2 is H, the salts thereof with physiologically compatible bases have valuable pharmacalogical properties, e.g., hypertonic and bronchodilatory activities.
摘要翻译：其中R1是OR2或NHR3的式“IMAGE”的5-氰基 - 前列环素; R 2和R 3各自独立地为（a）H，（b）C 1-10 - 烷基，（c）被卤素，C 1-4 - 烷氧基或苯基，1-萘基或2-萘基取代的C 1-10 - 烷基，（d）C 4-10 - 环烷基，（e）被C 1-4 - 烷基取代的C 4-10 - 环烷基，（f）苯基，1-萘基或2-萘基，（g）苯基，萘基或被1-3个卤素原子取代的2-萘基，苯基，1-4个C原子的1-3个烷基，或1个氯甲基 - ，氟甲基 - ，三氟甲基 - ，羧基 - ，羟基或烷氧基 -4个C原子，或（h）含有一个杂原子的芳族的5或6元杂环，它是O，N或S，其余的原子是碳; R3也可能是C1-15-烃羧酸或磺酸的酰基; B是2-10个C原子的直链或支链亚烷基; W是羟基亚甲基或其中OH基团可以在α或β位置，并且任选地通过用在前列腺素中这种替代物常规的醚或酰基取代OH的H原子来任意修饰，并且其是在生理pH值下易于切割; R4是羟基，任选地按照上述W所述进行改性; R5，R6，R7和R8各自独立地为氢，1-5个C原子的烷基或甲氧基; 并且R 9为1-5个C原子的烷基，或对于其中R 2为H的化合物，其与生理上相容的碱的盐具有有价值的药理学性质，例如高渗和支气管扩张活性。

90. 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。

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