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1. 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.

2. 发明授权

US4870104A 11-haloprostane derivatives, processes for their preparation and their use as medicinal agents 失效
标题翻译： 11-卤代前驱烷衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4870104A
公开(公告)日：1989-09-26
申请号：US929310
申请日：1986-11-12
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Claus-Steffen Sturzebecher , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Claus-Steffen Sturzebecher , Walter Elger
IPC分类号： C07D317/16 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D263/00 , C07D263/14 , C07D271/00 , C07D271/06 , C07D317/20 , C07D319/12 , C07D321/00 , C07D493/00 , C07D493/08
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0041 , C07D317/20
摘要： 11-Haloprostane derivatives of general formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis-CH.dbd.CH-group,B is a --CH.sub.2 --CH.sub.2 -- or trans-CH.dbd.CH-- or a --C.tbd.C-group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C-bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.
摘要翻译：其中X是F，Cl或Br，R1是残基CH 2 OH或者其中R 2表示氢原子，烷基，环烷基，芳基，苯甲酰基或杂环残基 A是-CH 2 -CH 2 - 或顺式-CH = CH-基，B是-CH 2 -CH 2 - 或反式-CH = CH-或-C 3 C C基，W是亚乙二氧基亚甲基或羟基亚甲基基团，D和E一起表示直接键合，或D表示C1-10亚烷基，E表示氧或硫原子，直接键，-C3OND C键或-CR6 = CR7-基，R6 R7表示氢原子，氯原子或烷基，R4表示羟基，R5表示氢原子，烷基，环烷基，芳基或杂环基，其盐与生理上相容的碱，工艺用于其制备，并且其用作抑制胃酸分泌的试剂。

3. 发明授权

US4835175A Indole derivatives pharmaceutical preparations based thereon, and .beta.-receptor stimulation therewith 失效
标题翻译：基于此的吲哚衍生物药物制剂和其中的β-受体刺激
公开(公告)号：US4835175A
公开(公告)日：1989-05-30
申请号：US917445
申请日：1986-10-10
申请人： Josef Heindl , Olaf Loge
发明人： Josef Heindl , Olaf Loge
IPC分类号： A61K31/403 , A61K31/404 , A61K31/405 , A61P25/02 , A61P25/04 , A61P29/00 , A61P37/08 , C07C205/37 , C07D209/08 , C07D209/42 , C07D413/14
CPC分类号： C07C255/00 , C07C205/37 , C07D209/08 , C07D209/42
摘要： Indole derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1-6 carbon atoms, or benzylR.sub.2 is hydrogen, alkyl of up to 4 carbon atoms, free or esterified hydroxyalkyl of up to 4 carbon atoms, or free, amidated or esterified carboxy or carboxyalkyl,R.sub.3 is hydrogen or alkyl containing 1-6 carbon atoms,R.sub.4 is hydrogen or alkyl containing 1-6 carbon atoms andR.sub.5 is hydrogen, or alkyl, alkenyl, or cycloalkyl, all of which per se contain up to 6 carbon atoms, and all of which are optionally substituted by a free or esterified carboxy group or by an optionally substituted phenyl group; or a polymethylene group of up to 8 carbon atoms linking the first indole residue to a second indole residue of Formula Ia ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined above,and the physiologically acceptable salts thereof with acids and, optionally, their alkali metal and alkaline earth metal salts,possess valuable pharmacological properties, such as stimulating .beta.-receptors and prevention of premature labor, are described.
摘要翻译：式I的吲哚衍生物其中R 1是氢，1-6个碳原子的烷基或苄基R 2是氢，至多4个碳原子的烷基，最多4个碳原子的游离或酯化的羟烷基，或游离的，酰胺化的或酯化的羧基或羧基烷基，R3是氢或含有1-6个碳原子的烷基，R4是氢或含1-6个碳原子的烷基，R5是氢或烷基，烯基或环烷基，其本身都是含有多达6个碳原子，并且所有这些都任选被游离或酯化的羧基或任选取代的苯基取代; 或至多8个碳原子的多亚甲基，其连接第一吲哚残基与式Ia的第二吲哚残基（Ia），其中R 1，R 2，R 3和R 4如上所定义，其生理上可接受的盐与描述了酸和任选的其碱金属和碱土金属盐，具有有价值的药理学性质，例如刺激β-受体和预防早产。

4. 发明授权

US4789685A 9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents 失效
标题翻译： 9-氟前列腺素衍生物，其制备和用作药物
公开(公告)号：US4789685A
公开(公告)日：1988-12-06
申请号：US4733
申请日：1987-01-20
申请人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
发明人： Werner Skuballa , Bernd Raduechel , Norbert Schwarz , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Michael-Harold Town
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0041
摘要： 9-fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and 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,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, the physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.
摘要翻译：其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基的式I的α-氟仿烷基衍生物。或R1是残基，其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-，B是-CH2-CH2-，反式-CH = CH-或-C3BOND C，W是游离的或官能改性的羟基亚甲基，其中OH基可以是α或β位，D和E共同是直接键，或D是1-10的直链或支链亚烷基或亚链烯基可以任选被氟原子取代的碳原子，E是氧或硫，直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或烷基 R4是游离的或官能改性的羟基，R5是氢，任意取代的脂族基团，例如烷基或卤代取代的烷基，环烷基，任选被取代的芳基或杂环基，当R2是H时，生理上相容的盐具有有价值的药理学性质，例如作为骨质疏松症或流产者。

5. 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。

6. 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。

7. 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。

8. 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.

9. 发明授权

US06225347B1 9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译： 9-卤素 - （Z） - 前列腺素衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US06225347B1
公开(公告)日：2001-05-01
申请号：US08313667
申请日：1994-09-27
申请人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C40500
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0025
摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or a —CR6═CR7 group, and R6 and R7 are different and mean a hydrogen atom, a chlorine atom or a C1-C4 alkyl group, R4 resents a free or functionally modified hydroxy group, R5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group, and if R2 means a hydrogen atom, its salts with physiologically compatible bases or its cyclodextrin chlathrates, process for their production and their pharmaceutical use.
摘要翻译：本发明涉及式Iin的9-卤素 - （Z）前列腺衍生物，其中Z代表基团.Hal表示α或β位上的氯或氟原子，R 1表示R 2表示氢原子，烷基，环烷基，芳基或杂环基或R 1表示基团，其中R 3表示酸基或基团R 2且A表示-CH 2 -CH 2 - ，反式-CH = CH或-C = C基团，W表示游离或功能修饰基团， OH基可以是α或β位，D和E一起代表直接键或D表示具有1-10个C原子的直链亚烷基，具有2-10个C原子的支链亚烷基或环状亚烷基具有3-10个C原子的基团，其任选地可以被氟原子取代，E表示氧或硫原子，直接键合，C = C键或-CR 6 = CR 7基团，并且R 6和R 7不同，一个氢原子，一个氯原子或一个C 1 -C 4烷基，R 4是一个游离的或官能改性的羟基，R 5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基，如果R 2表示氢原子，则其与生理上相容的碱或其环糊精的盐 chlathrates，生产过程及其药物用途。

10. 发明授权

US5891910A 9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译： 9-卤素 - （Z）前列腺素衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US5891910A
公开(公告)日：1999-04-06
申请号：US467888
申请日：1995-06-06
申请人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C405/00 , A61K31/557
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0025
摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I ##STR1## in which ##STR2## Z represents the radicals Hal represents a chlorine or fluorine atom,R.sub.1 represents ##STR3## A represents a --CH.sub.2 --CH.sub.2 --, a trans--CH=CH or --C.ident.C, W represents a free or a functionally modified ##STR4## group, D and E together represent a direct bond orD represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, andE represents an oxygen or sulfur atom, a direct bond, a C.ident.C bond or a --CR.sub.6 =CR.sub.7 group, and R.sub.6 and R.sub.7 are different and mean a hydrogen atom, a chlorine atom or a C.sub.1 -C.sub.4 alkyl group,R.sub.4 represents a free or functionally modified hydroxy,R.sub.5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group.
摘要翻译：本发明涉及式I的9-卤代 - （Z）前列腺衍生物，其中，Z表示基团，Hal表示氯或氟原子，R1表示A表示 -CH 2 -CH 2 - ，反式-CH = CH或-C = C，W表示游离或官能改性的基团，D和E一起表示直接键或D表示直链亚烷基，其中1 -10个C原子，具有2-10个碳原子的支链亚烷基或具有3-10个C原子的环状亚烷基，其任选可以被氟原子取代，E表示氧或硫原子，直接键，C = C键或-CR6 = CR7基，R6和R7不同，表示氢原子，氯原子或C1-C4烷基，R4表示游离或官能改性的羟基，R5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基。

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