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1. 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.

2. 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。

3. 发明授权

US4219479A 5-Cyano-prostacyclin derivatives 失效
标题翻译： 5-氰基前列环素衍生物
公开(公告)号：US4219479A
公开(公告)日：1980-08-26
申请号：US963240
申请日：1978-11-24
申请人： Helmut Vorbruggen , Werner Skuballa , Bernd Raduchel , Wolfgang Losert , Olaf Loge , Bernd Muller , Gerda Mannesmann
发明人： Helmut Vorbruggen , Werner Skuballa , Bernd Raduchel , Wolfgang Losert , Olaf Loge , Bernd Muller , Gerda Mannesmann
IPC分类号： A61K31/557 , A61K31/34 , A61K31/343 , A61K31/5575 , A61P1/04 , A61P7/02 , A61P9/12 , A61P11/00 , C07C405/00 , C07D307/935 , C07D307/937 , A61K31/335 , C07D307/93
CPC分类号： C07D307/937
摘要： Stabilized prostacyclins having a wide range of pharmacological activity and long duration of such activity, have the formula ##STR1## wherein R.sub.1 is (a) OR.sub.3, wherein R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl or a heterocyclic residue; or (b) NHR.sub.4 wherein R.sub.4 is an acid residue;B is straight-chain or branched alkylene of 2-10 carbon atoms;A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, trans--CH.dbd.CH-- or --C.tbd.C--,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 and E together are a direct bond; orD is straight-chain or branched alkylene of 1-5 carbon atoms; andE is oxygen or sulfur or a direct bond,R.sub.2 is alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group; andR.sub.5 is free or functionally modified hydroxy; and when R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases.
摘要翻译：具有广泛的药理活性和长时间的这种活性的稳定的前列环素具有下式（IMAGE），其中R1是（a）OR3，其中R3是氢，烷基，环烷基，芳基或杂环残基; 或（b）NHR 4，其中R 4是酸残基; B是2-10个碳原子的直链或支链亚烷基; A是-CH 2 -CH 2 - ，顺式-CH = CH-，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，其中OH-基团可以是在alpha或beta位置; D和E一起是直接的债券; 或D是1-5个碳原子的直链或支链亚烷基; 并且E是氧或硫或直接键，R 2是烷基，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; 并且当R3是氢时，其盐与生理上相容的碱基。

4. 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。

5. 发明授权

US4423067A Carbacyclins, their preparation and use 失效
标题翻译：卡巴菌素，其制备和用途
公开(公告)号：US4423067A
公开(公告)日：1983-12-27
申请号：US333099
申请日：1981-12-21
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： C07C69/708 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/23 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P11/08 , C07C51/00 , C07C51/367 , C07C59/125 , C07C67/00 , C07C231/00 , C07C231/02 , C07C235/06 , C07C235/88 , C07C301/00 , C07C303/40 , C07C311/51 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40 , C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D309/12 , C07F9/4015 , Y10S514/927
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, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;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## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.2 is hydrogen, the physiologically compatible salts thereof with bases, have valuable pharmacological properties.
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，杂环残基或NHR 3，其中R 3是酸残基或氢; X是氧; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; 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1-10个碳原子的直链或支链，饱和或不饱和的脂族基团，其可任选被氟原子取代，1,2-亚甲基，1,1-三亚甲基; E是-C 3 C或-CR 6 = CR 7 - ，其中R 6和R 7是氢或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是游离的或官能改性的羟基，当R2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。

6. 发明授权

US4708963A Novel carbacyclins, their preparation and use 失效
标题翻译：新型碳霉素，其制备和用途
公开(公告)号：US4708963A
公开(公告)日：1987-11-24
申请号：US738545
申请日：1985-05-28
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： C07C69/708 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/23 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P11/08 , C07C51/00 , C07C51/367 , C07C59/125 , C07C67/00 , C07C231/00 , C07C231/02 , C07C235/06 , C07C235/88 , C07C301/00 , C07C303/40 , C07C311/51 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40 , C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D309/12 , C07F9/4015 , Y10S514/927
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, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;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## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CH.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.2 is hydrogen, the physiologically compatible salts thereof with bases, have valuable pharmacological properties.
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，杂环残基或NHR 3，其中R 3是酸残基或氢; X是氧; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; 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1-10个碳原子的直链或支链，饱和或不饱和的脂族基团，其可任选被氟原子取代，1,2-亚甲基，1,1-三亚甲基; E是-C 3 C或-CR 6 = CH 7 - ，其中R 6和R 7是氢或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是游离的或官能改性的羟基，当R2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。

7. 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。

8. 发明授权

US4154953A Crystalline prostanoic acid esters 失效
标题翻译：结晶前列腺酸酯
公开(公告)号：US4154953A
公开(公告)日：1979-05-15
申请号：US826908
申请日：1977-08-19
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Prostanoic acid esters of the formulaPG-- CH.sub.2 -- X-- Ywherein PG is the prostanoyloxy radical of a prostaglandin, X is a carbon-carbon single bond, carbonyl or carbonyloxy, and Y is substituted phenyl are easily crystallized compounds at least as active as the unesterified prostanoic acid and useful for the purification of the parent prostaglandin are prepared by reacting, in the presence of an agent which splits off hydrogen halide, the unesterified prostaglandin with a halide of the formula Hal--CH.sub.2 --X--Y, wherein Hal is a halogen atom and X and Y have the values given above.
摘要翻译：式PG-CH2-X-Y的前列腺酸，其中PG是前列腺素的前烷氧基自由基，X是碳 - 碳单键，羰基或羰氧基，Y是取代的苯基，容易结晶化合物至少与通过使未分解的前列腺素与式Hal-CH2-XY的卤化物反应，其中Hal是卤素，其中Hal是卤素原子，X和Y具有上面给出的值。

9. 发明授权

US3962218A Novel prostanoic acid derivatives and processes for the preparation thereof 失效
标题翻译：新型乳酸衍生物及其制备方法
公开(公告)号：US3962218A
公开(公告)日：1976-06-08
申请号：US472738
申请日：1974-05-23
申请人： Bernd Raduchel , Werner Skuballa , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
发明人： Bernd Raduchel , Werner Skuballa , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
IPC分类号： C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D317/30 , C07D317/54 , C07D319/06 , C07C177/00 , C07D317/12 , C07D317/50 , C07D319/04
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07D317/30 , C07D317/54 , C07D319/06
摘要： Prostaglandins of the formula ##SPC1##Wherein R.sub.1 is HOCH.sub.2, --COOH, a salt thereof or an ester thereof; R.sub.2 is OH; and R.sub.3 is H or R.sub.2 and R.sub.3 collectively are = O. A is --CH.sub. 2 --CH.sub.2 -- or --(trans)--CH=CH--, B is --CH.sub. 2 CH.sub.2 --or --(cis)--CH=CH-- and R.sub.4 --O--O--R.sub.5 is a ketal group, are superior in physiological activity to the corresponding 15-.alpha.-hydroxy-prostaglandins.

10. 发明授权

US3984454A Crystalline prostanoic acid esters 失效
标题翻译：结晶前列腺酸酯
公开(公告)号：US3984454A
公开(公告)日：1976-10-05
申请号：US466173
申请日：1974-05-02
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
IPC分类号： A61K31/557 , A61K31/5575 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Prostanoic acid esters of the formulaPG -- CH.sub.2 -- X -- Ywherein PG is the prostanoyloxy radical of a prostaglandin, X is a carbon-carbon single bond, carbonyl or carbonyloxy, and Y is substituted phenyl are easily crystallized compounds at least as active as the unesterified prostanoic acid and useful for the purification of the parent prostaglandin are prepared by reacting, in the presence of an agent which splits off hydrogen halide, the unesterified prostaglandin with a halide of the formula Hal--CH.sub.2 --X--Y, wherein Hal is a halogen atom and X and Y have the values given above.
摘要翻译：式PG-CH2-X-Y的前列腺酸酯，其中PG是前列腺素的前烷氧基自由基，X是碳 - 碳单键，羰基或羰基氧基，Y是取代的苯基，其容易结晶化合物至少与通过使未分解的前列腺素与式Hal-CH2-XY的卤化物反应，其中Hal是卤素，其中Hal是卤素原子，X和Y具有上面给出的值。

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