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1. 发明授权

US4031236A Novel thiophene derivatives and their preparation 失效
标题翻译：新型噻吩衍生物及其制备方法
公开(公告)号：US4031236A
公开(公告)日：1977-06-21
申请号：US579258
申请日：1975-05-20
申请人： Hanns Ahrens , Helmut Biere , Clemens Rufer , Ralph Schmiechen , Eberhard Schroeder , Olaf Loge , Wolfgang Losert , Ekkehard Schillinger
发明人： Hanns Ahrens , Helmut Biere , Clemens Rufer , Ralph Schmiechen , Eberhard Schroeder , Olaf Loge , Wolfgang Losert , Ekkehard Schillinger
IPC分类号： C07D333/34 , C07D409/12 , A61K31/41 , A61K31/38 , C07D257/04 , C07D333/24
CPC分类号： C07D333/34
摘要： Thiophene derivatives of the formula ##STR1## IN WHICH R.sub.x is --S--CHR.sub.5 --CONHOH or --S--CHR.sub.5 -5-tetrazolyl in which R.sub.5 is H or alkyl of 1-6 carbon atoms and R.sub.y is 0-2 of alkyl or alkoxy of 1-6 carbon atoms or halogen, and their pharmacologically acceptable salts with bases, possess antilipolytic activity.
摘要翻译：其中R x为-S-CHR 5 -CONHOH或-S-CHR 5 -5-四唑基的噻吩衍生物，其中R 5为H或1-6个碳原子的烷基，R y为烷基或烷氧基的0-2 1-6个碳原子或卤素，及其与碱的药理学上可接受的盐具有抗水解活性。

2. 发明授权

US4021450A Thiophene derivatives and their preparation 失效
标题翻译：噻吩衍生物及其制备方法
公开(公告)号：US4021450A
公开(公告)日：1977-05-03
申请号：US579196
申请日：1975-05-20
申请人： Hanns Ahrens , Helmut Biere , Clemens Rufer , Ralph Schmiechen , Eberhard Schroeder , Olaf Loge , Wolfgang Losert , Ekkehard Schillinger
发明人： Hanns Ahrens , Helmut Biere , Clemens Rufer , Ralph Schmiechen , Eberhard Schroeder , Olaf Loge , Wolfgang Losert , Ekkehard Schillinger
IPC分类号： C07D333/34 , C07D333/24
CPC分类号： C07D333/34
摘要： Thiophene derivatives of the formula ##STR1## WHEREIN R.sub.x is --S-CHR.sub.5 -COOH or -S-CH.sub.2 -CH.sub.2 -OH, R.sub.y is 1-2 of halogen alkoxy of 1-6 carbon atoms, aralkyl of 7-10 carbon atoms, phenyl, halophenyl or alkylcarbonyl of 1-6 carbon atoms in the alkyl group, and R.sub.5 is a hydrogen atom, when R.sub.y is a halogen atom, when R.sub.5 is alkyl, their enantiomers, and their pharmacologically acceptable salts thereof with bases, possess antilipolytic activity.
摘要翻译：式中的噻吩衍生物，其中Rx是-S-CHR5-COOH或-S-CH2-CH2-OH，R10是1-6个碳原子的卤代烷氧基的1-2，7-10个碳原子的芳烷基，苯基，卤代苯基或烷基中1-6个碳原子的烷基羰基，当R 5为卤素原子时，R 5为氢原子，当R 5为烷基时，其对映异构体及其与碱的药理学上可接受的盐具有抗水解活性。

3. 发明授权

US4058619A Thiophene derivatives having antilipolytic activity 失效
标题翻译：具有抗水解活性的噻吩衍生物
公开(公告)号：US4058619A
公开(公告)日：1977-11-15
申请号：US723309
申请日：1976-09-14
申请人： Hanns Ahrens , Helmut Biere , Clemens Rufer , Ralph Schmiechen , Eberhard Schroeder , Olaf Loge , Wolfgang Losert , Ekkehard Schillinger
发明人： Hanns Ahrens , Helmut Biere , Clemens Rufer , Ralph Schmiechen , Eberhard Schroeder , Olaf Loge , Wolfgang Losert , Ekkehard Schillinger
IPC分类号： C07D333/34 , A61K31/38
CPC分类号： C07D333/34
摘要： Thiophene derivatives of the formula ##STR1## WHEREIN R.sub.x is --S-CHR.sub.5 -COOH or --S-CH.sub.2 -CH.sub.2 -OH, R.sub.y is 1-2 of halogen alkoxy of 1-6 carbon atoms, aralkyl of 7-10 carbon atoms, phenyl, halophenyl or alkylcarbonyl of 1-6 carbon atoms in the alkyl group, and R.sub.5 is a hydrogen atom, when R.sub.y is a halogen atom, when R.sub.5 is alkyl, their enantiomers, and their pharmacologically acceptable salts thereof with bases, possess antilipolytic activity.
摘要翻译：式中的噻吩衍生物，其中Rx是-S-CHR5-COOH或-S-CH2-CH2-OH，R10是1-6个碳原子的卤代烷氧基的1-2，7-10个碳原子的芳烷基，苯基，卤代苯基或烷基中1-6个碳原子的烷基羰基，当R 5为卤素原子时，R 5为氢原子，当R 5为烷基时，其对映异构体及其与碱的药理学上可接受的盐具有抗水解活性。

4. 发明授权

US3960949A 1,2-Biguanides 失效
标题翻译： 1,2双胍
公开(公告)号：US3960949A
公开(公告)日：1976-06-01
申请号：US486758
申请日：1974-07-09
申请人： Hanns Ahrens , Clemens Rufer , Helmut Biere , Eberhard Schroder , Wolfgang Losert , Olaf Loge , Ekkehard Schillinger
发明人： Hanns Ahrens , Clemens Rufer , Helmut Biere , Eberhard Schroder , Wolfgang Losert , Olaf Loge , Ekkehard Schillinger
IPC分类号： C07C279/26 , C07C129/16
CPC分类号： C07C279/26
摘要： 1,2-Substituted biguanides of the formula ##EQU1## wherein R.sub.1 is saturated or unsaturated, straight-chain or branched hydrocarbon of 1-12 carbon atoms which is unsubstituted or substituted by one or more fluorine atoms; a cycloalkyl group of 3-6 carbon atoms; or an aryl or aralkyl group of the formula ##SPC1##With n being the integer 0, 1 or 2 and X being hydrogen or halogen; and R'.sub.1 is a hydrogen atom or a saturated or unsaturated, straight-chain or branched hydrocarbon group of 1-12 carbon atoms; or R.sub.1 and R'.sub.1 collectively with the nitrogen atom to which they are attached are a heterocyclic ring containing one or more hetero atoms; and R.sub.2 is saturated or unsaturated, straight-chain or branched hydrocarbon of 1-12 carbon atoms which is unsubstituted or substituted by one or more fluorine atoms; or cycloalkyl of 3-6 carbon atoms, alkoxyalkyl containing a total of 2-12 carbon atoms, or alkoxy of 1-6 atoms; mixtures thereof, and pharmaceutically acceptable acid addition salts thereof, are useful in the treatment of diabetes mellitus.
摘要翻译： 1,2-取代的式R'1 | R1-NC-NH-C-NH2的平行二亚胺平行平行NNH | R2其中R1是1-12个碳原子的饱和或不饱和的直链或支链烃，未取代或未取代的被一个或多个氟原子取代; 3-6个碳原子的环烷基; 或下式的芳基或芳烷基：其中N为整数0,1或2且X为氢或卤素; 并且R'1是1-12个碳原子的氢原子或饱和或不饱和的直链或支链烃基; 或者R1和R'1与它们所连接的氮原子一起是含有一个或多个杂原子的杂环; R2是未被取代或被一个或多个氟原子取代的1-12个碳原子的饱和或不饱和的直链或支链烃基; 或3-6个碳原子的环烷基，总共2-12个碳原子的烷氧基烷基或1-6个原子的烷氧基; 其混合物及其药学上可接受的酸加成盐可用于治疗糖尿病。

5. 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.

6. 发明授权

US4235930A Novel acetylenic prostaglandins and processes for the preparation thereof 失效
标题翻译：新型炔类前列腺素及其制备方法
公开(公告)号：US4235930A
公开(公告)日：1980-11-25
申请号：US920523
申请日：1978-06-29
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
IPC分类号： A61K31/18 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/435 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/20 , C07D307/935 , C07D309/12 , C07D333/32 , C07F9/40 , C07C177/00 , A61K31/557
CPC分类号： C07D307/935 , C07C405/00 , C07F9/4015 , Y02P20/55
摘要： Prostane derivatives of the formula ##STR1## wherein R.sub.1 is the residue OR.sub.2 and R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or is NHR.sub.3 wherein R.sub.3 is an acyl group derived from a hydrocarbon carboxylic or sulfonic acid of up to 15 carbon atoms;A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--Z is carbonyl or ##STR2## wherein the OR.sub.4 group can be in the .alpha.- or .beta.-position and R.sub.4 is H or a hydroxy-protective groupX Y is ##STR3## wherein R.sub.4 is as defined above, --CH.sub.2 -- CH.sub.2 -- or --CH.sub.2 --CH-- wherein R.sub.5 is alkyl or 1-5 carbon atoms, if Z is R.sub.5 carbonyl or ##STR4## X Y represents --CH.dbd.CH-- if Z is carbonyl: R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 each independently is hydrogen or an alkyl group of 1-5 carbon atoms; andR.sub.11 is alkyl of 1-5 carbon atoms;and if R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases are prostaglandins having prolonged duration of activity and increased selectivity of effectiveness.
摘要翻译：其中R1是残基OR2，R2是氢，烷基，环烷基，芳基或杂环残基的式或者是NHR 3，其中R 3是衍生自至多15个碳原子的烃羧酸或磺酸的酰基; A是-CH 2 -CH 2 - 或顺式-CH = CH-Z是羰基或者其中OR 4基团可以是α或β-位，R 4是H或羟基保护基团XY是其中R 4如上定义，-CH 2 -CH 2 - 或-CH 2 -CH-，其中R 5是烷基或1-5个碳原子，如果Z是R 5羰基或如果Z是羰基，则X代表-CH = CH- R6，R7，R8，R9和R10各自独立地为氢或1-5个碳原子的烷基; R11为1-5个碳原子的烷基; 并且如果R 2是氢，则其与生理上相容的碱的盐是具有延长的活性持续时间和增加的有效性选择性的前列腺素。

7. 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。

8. 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。

9. 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。

10. 发明授权

US4631276A Prostaglandins and prostacyclins, process for their preparation and their use as medicaments 失效
标题翻译：前列腺素和前列腺素，其制备过程及其用作药物
公开(公告)号：US4631276A
公开(公告)日：1986-12-23
申请号：US627572
申请日：1984-07-03
申请人： Helmut Vorbruggen , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
发明人： Helmut Vorbruggen , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
IPC分类号： C07C405/00 , C07D263/14 , C07D277/10 , C07D417/12 , C07F7/18 , C07D233/14 , A61K31/42
CPC分类号： C07D417/12 , C07C405/0041 , C07D263/14 , C07D277/10 , C07F7/1856
摘要： Compounds of Formula I ##STR1## wherein R.sub.1 is a prostaglandin or prostacyclin residue;Y is oxygen, sulfur, imino, or N-(C.sub.1 -C.sub.4 -alkyl) imino;Q is (CR.sub.6 R.sub.7).sub.p wherein p is an integer of 0 to 3;R.sub.2 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; C.sub.1 -C.sub.4 -alkoxycarbonyl; benzyloxycarbonyl; cyano; or di-C.sub.1 -C.sub.4 -alkylamino-carbonyl;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each independently is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; or aryl; andR.sub.3 and R.sub.4 together form a trimethylene, tetramethylene, or 1,3-butadienylene group when R.sub.2 and R.sub.5 together represent a direct bond;have valuable pharmacological properties, e.g., as blood-pressure-lowering or abortive agents.
摘要翻译：式I的化合物其中R 1是前列腺素或前列环素残基; Y是氧，硫，亚氨基或N-（C 1 -C 4 - 烷基）亚氨基; Q是（CR 6 R 7）p，其中p是0至3的整数; R2是氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; C 1 -C 4烷氧基羰基; 苄氧羰基氰基; 或二-C 1 -C 4烷基氨基 - 羰基; R3，R4，R5，R6和R7各自独立地为氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; 或芳基; 当R 2和R 5一起代表直接键时，R 3和R 4一起形成三亚甲基，四亚甲基或1,3-丁二烯基; 具有有价值的药理学性质，例如作为降血压药或降血糖药。

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