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公开(公告)号:US5395843A
公开(公告)日:1995-03-07
申请号:US56241
申请日:1993-04-30
IPC分类号: C07D295/12 , A61K31/44 , A61K31/4412 , A61K31/4427 , A61K31/445 , A61K31/451 , A61P9/06 , A61P9/12 , A61P25/02 , A61P25/04 , A61P29/00 , C07D211/40 , C07D211/76 , C07D211/86 , C07D295/125 , C07D295/13 , C07D295/135 , C07D401/06 , C07D401/08 , C07D401/10
CPC分类号: C07D295/135 , C07D211/76 , C07D211/86 , C07D295/125
摘要: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## wherein A, R, R.sub.1, R.sub.2 and Y are as defined in the specification.
摘要翻译: 选自下式的化合物的所有可能的外消旋,对映异构体和非对映异构体形式的化合物其中E和G一起形成选自以下的基团:
IMAGE>其中A,R,R1,R2和Y如说明书中所定义。 -
公开(公告)号:US5356907A
公开(公告)日:1994-10-18
申请号:US955049
申请日:1992-10-01
IPC分类号: C07D295/12 , A61K31/44 , A61K31/4412 , A61K31/4427 , A61K31/445 , A61K31/451 , A61P9/06 , A61P9/12 , A61P25/02 , A61P25/04 , A61P29/00 , C07D211/40 , C07D211/76 , C07D211/86 , C07D295/125 , C07D295/13 , C07D295/135 , C07D401/06 , C07D401/08 , C07D401/10 , C07D409/04
CPC分类号: C07D295/135 , C07D211/76 , C07D211/86 , C07D295/125
摘要: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## wherein, A is a cycloalkyl of 3-6 carbon optionally substituted, R, R.sub.1, R.sub.2 and Y are defined in the specification.
摘要翻译: 选自下列化合物的化合物的化合物的化合物的所有可能的外消旋,对映体和非对映异构体形式的化合物,其中E和G一起形成选自以下的基团:
其中,A是任选取代的3-6个碳的环烷基,R 1,R 2,R 2和Y在本说明书中定义。 -
公开(公告)号:US5348971A
公开(公告)日:1994-09-20
申请号:US105329
申请日:1993-08-09
IPC分类号: C07D295/135 , C07D307/52 , A61K31/40 , C07D295/073
CPC分类号: C07D295/135 , C07D307/52 , C07C2102/08
摘要: Novel indanes in all possible stereoisomer forms of the formula ##STR1## wherein the substrates are as defined in the application and their non-toxic, pharmaceutically acceptable acid addition salts and their hydrates are disclosed as having central analgesic properties as well as antiarrhythmic and diuretic activities.
摘要翻译: 式中所有可能的立体异构体形式的新型茚满酮其中底物如本申请中所定义,并且它们的无毒,药学上可接受的酸加成盐及其水合物被公开为具有中枢镇痛特性以及抗心律不齐和利尿 活动
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公开(公告)号:US5559130A
公开(公告)日:1996-09-24
申请号:US346017
申请日:1994-11-29
IPC分类号: C07D295/12 , A61K31/44 , A61K31/4412 , A61K31/4427 , A61K31/445 , A61K31/451 , A61P9/06 , A61P9/12 , A61P25/02 , A61P25/04 , A61P29/00 , C07D211/40 , C07D211/76 , C07D211/86 , C07D295/125 , C07D295/13 , C07D295/135 , C07D401/06 , C07D401/08 , C07D401/10
CPC分类号: C07D295/135 , C07D211/76 , C07D211/86 , C07D295/125
摘要: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## or, if appropriate, its tautomer ##STR4## and ##STR5## or E is --COOR.sub.3 and G is ##STR6## wherein A, Y, R, Ra, R.sub.1 and R.sub.2 are as defined in the specification.
摘要翻译: 选自下列化合物的化合物的化合物:其中E和G一起形成选自以下的基团:由下列组成的组合:a)IMAGE或 如果合适,其互变异构体
和 或E是-COOR3,G是 ,其中A,Y,R,Ra,R1和R2如说明书中所定义。 -
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公开(公告)号:US06271395B1
公开(公告)日:2001-08-07
申请号:US08356912
申请日:1994-12-15
IPC分类号: C07D20948
CPC分类号: C07D295/135 , C07D311/96
摘要: A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula wherein the substituents are defined as in the application having a strong affinity for optical receptors, central analgesic, diuretic, anti-arrythmic, hypotensive and cerebral anti-ischemic activity.
摘要翻译: 在取代基中的选自对映体和非对映异构体形式及其混合物的化合物的定义如在对光学受体,中枢镇痛药,利尿剂,抗心律失常药,降血压药和脑抗缺血活性具有强亲合力的应用中 。
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公开(公告)号:US5141962A
公开(公告)日:1992-08-25
申请号:US516045
申请日:1990-04-27
IPC分类号: A61K31/135 , A61P25/30 , C07C213/00 , C07C215/52 , C07C217/60
CPC分类号: C07C217/60 , C07C215/52
摘要: A compound selected from the group consisting of N-pentyl-N-phenethyl-3-hydroxyphenethylamine of the formula ##STR1## and its non-toxic, pharmaceutically acceptable acid addition salts having a remarkably dissociated antagonist affinity for kappa opiate receptor.
摘要翻译: 选自由式I的N-戊基-N-苯乙基-3-羟基苯乙胺和其无毒的药学上可接受的酸加成盐的化合物,其对κ阿片受体具有显着解离的拮抗剂亲和力。
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公开(公告)号:US5130329A
公开(公告)日:1992-07-14
申请号:US591283
申请日:1990-10-01
IPC分类号: A61K31/165 , A61K31/33 , A61K31/38 , A61K31/381 , A61K31/40 , A61P7/10 , A61P9/06 , A61P9/12 , A61P25/04 , A61P25/28 , C07C67/00 , C07C209/00 , C07C209/16 , C07C209/60 , C07C211/42 , C07C215/44 , C07C215/70 , C07C217/74 , C07C233/79 , C07C235/14 , C07C271/52 , C07D295/12 , C07D295/135 , C07D333/54 , C07D333/60 , C07D521/00
CPC分类号: C07D295/135 , C07D333/60
摘要: Novel all possible enantiomeric and diastereoisomeric forms of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --No.sub.2, --NH.sub.2 and mono and dialkylamino of 1 to 5 alkyl carbon atoms, A and B have the trans configuration, one of A and B being ##STR2## R.sub.2 is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n2, n.sub.2 being an integer from 0 to 5 or branched alkylene of 2 to 8 carbon atoms or --CH.sub.2 --O--, Y is selected from the group consisting of phenyl, naphthyl, indenyl, heteromonocycle of 5 to 6 ring atoms and heterobicycle, all optionally having at least one substituent and the other of A and B is ##STR3## R.sub.4 and R.sub.5 individually being selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen to which they are attached form a 5 to 6 ring heterocycle optionally containing a heteroatom selected from the group consisting of --O--, --S-- and --NH-- and their non-toxic, pharmaceutically acceptable acid addition salts having central analgesic properties and a strong affinity for opiate receptors.
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公开(公告)号:US4988727A
公开(公告)日:1991-01-29
申请号:US409048
申请日:1989-09-19
申请人: Francois Clemence , Michel Fortin
发明人: Francois Clemence , Michel Fortin
IPC分类号: C07D295/135 , C07D295/155 , C07D333/24 , C07D333/54
CPC分类号: C07D295/135 , C07D295/155 , C07D333/24 , C07D333/54
摘要: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.2 monoalkylamino and dialkylamino of 1 to 4 alkyl carbon atoms and phenyl optionally substituted with at least one member of the group consisting of halogen and alkyl and alkoxy of 1 to 4 carbon atoms, R.sub.3 and R.sub.4 are individually hydrogen or alkyl or 1 to 5 carbon atoms or taken together with the nitrogen form a heterocyclic of 5 to 6 ring members and optionally containing --O--, --S-- or nitrogen in the ring and their non-toxic, pharmaceutically acceptable acid addition salts having central analgesic and antiarythmic activity among other activities.
摘要翻译: 选自下列化合物的化合物:其中X选自氢,卤素和1至5个碳原子的烷基和烷氧基,R 1和R 2的所有对映异构体和非对映异构体形式。 分别选自氢和1至5个碳原子的烷基,A和B之一为“IMAGE”,另一个为R 1为氢或1至5个碳原子的烷基,Z为 - ( CH 2)2至8个碳原子的正或支链亚烷基,n为0至5的整数,Y选自萘基,茚基,异双环烯烃和含有5至6个环成员的杂单环,全部任选被 由1至5个碳原子的烷基和烷氧基,卤素,-OH,-CF 3,-NO 2,-NH 2单烷基氨基和1至4个烷基碳原子的二烷基氨基组成的组中的至少一个和任选被至少一个成员取代的苯基 由卤素和烷基组成的组中 具有1至4个碳原子的烷氧基,R 3和R 4独立地为氢或烷基或1至5个碳原子,或与氮一起形成5至6个环成员的杂环,并任选地含有-O - , - S-或 环中的氮和它们的无毒的药学上可接受的酸加成盐,具有其他活性的中枢镇痛和抗血液活性。
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公开(公告)号:US6004979A
公开(公告)日:1999-12-21
申请号:US71586
申请日:1998-05-01
IPC分类号: A61K31/47 , C07D215/06 , C07D215/12 , C07D215/22 , C07D215/233 , C07D215/36 , C07D215/44 , C07D237/28 , C07D239/74 , C07D401/10
CPC分类号: C07D215/233 , C07D215/06 , C07D215/12 , C07D215/36 , C07D215/44 , C07D237/28 , C07D239/74 , C07D401/10
摘要: Compounds of the formula ##STR1## in all possible racemic, enantiomeric and diastereoisomeric forms and their non-toxic, pharmaceutically acceptable salts with acids and bases having antagonistic properties for angiotensin II receptors and a process and novel intermediates for their properties.
摘要翻译: 具有所有可能的外消旋,对映异构体和非对映异构体形式的式的化合物及其与具有拮抗血管紧张素II受体的酸和碱的无毒的药学上可接受的盐,以及它们的性质的方法和新的中间体。
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公开(公告)号:US4927832A
公开(公告)日:1990-05-22
申请号:US214673
申请日:1988-07-01
申请人: Francois Clemence , Daniel Frechet , Michel Fortin
发明人: Francois Clemence , Daniel Frechet , Michel Fortin
IPC分类号: A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/55 , A61P7/10 , A61P9/00 , A61P9/06 , A61P9/12 , A61P25/04 , C07D221/04 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号: C07D221/04
摘要: Novel enantiomeric and diasteroisomeric forms of tetrahydropyridines of the formula ##STR1## wherein n.sub.1 is 0 or 2, A is selected from the group consisting of --(CH.sub.2).sub.n2 -- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms and n.sub.2 is 0 to 5, Z is selected from the group consisting of phenyl, naphthyl, indenyl, heteromonocycle of 5 to 6 ring members and heterobicycle, each optionally substituted with at least one substituent and their non-toxic, pharmaceutically acceptable acid addition salts and quaternary ammonium salts having central analgesic properties as well as diuretic, anti-arrhythmic, anti-cerebral-ischemia and hypotensive properties.
摘要翻译: 新颖的对映异构体和非对映异构形式的式(I)其中n1为0或2,A选自 - (CH2)n2-和被具有总共2至8个碳原子的烷基取代的亚烷基, n2为0至5,Z选自苯基,萘基,茚基,5至6个环成员的异单环和杂双环,各自任选被至少一个取代基取代,其无毒的药学上可接受的酸加成盐和 具有中枢镇痛作用以及利尿,抗心律失常,抗脑缺血和降血压性质的季铵盐。
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