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公开(公告)号:CZ89288A3
公开(公告)日:1994-12-15
申请号:CS89288
申请日:1988-02-12
Applicant: HOECHST AG
Inventor: URBACH HANSJORG DR , HENNING RAINER DR , SCHOLKENS BERNWARD DR , BECKER REINHARD DR
IPC: C07D223/32 , A61K31/395 , A61K31/445 , A61K31/55 , A61K38/00 , A61P9/00 , A61P9/12 , A61P27/02 , A61P27/06 , A61P43/00 , C07D225/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07K5/02 , C07K5/06
Abstract: Cyclopenta-azocine and -azepine derivs. of formula (I) and their salts are new. In (I) m = 1 or 2; n = 0-2; R1 and R2 = H; 1-6C alkyl (opt. substd. once by OH, SH, 1-2C alkoxy, 1-2C alkylthio, COOH, 1-2C alkoxycarbonyl, 3-indolyl, imidazolyl, CONH2, amino or guanidino); 2-6C alkenyl; 3-9C cycloalkyl or cycloalkenyl; 3-7C cycloalkyl (1-4C) alkyl; 6-12C aryl (opt. partially hydrogenated) or 6-12C aryl (1-4C) alkyl (opt. OH substd. in aryl); R3 and R4 = H, 1-6C alkyl, 2-6C alkenyl or 6-12C aryl (1-4C) alkyl, opt. substd. in aryl by one MeO or NO2; Y = H or OH; Z = H; or Y and Z are together oxo; X = 1-6C alkyl (opt. substd. by NH2, acylamino, 1-6C alkylamino and/or di(1-4C)alkylamino); 2-6C alkenyl; 5-9C cycloalkyl, 1-R1-piperidin-4-yl, 6-12C aryl (opt. substd. by 1-3 of 1-4C alkyl or alkoxy, OH, halo, NO2, NH2 (itself opt. substd. by 1 or 2 1-4C alkyl) and/or methylenedioxy) or 3-indolyl; any free OH, SH, COOH, amino or guanidino can be protected conventionally.
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公开(公告)号:DE3885914D1
公开(公告)日:1994-01-13
申请号:DE3885914
申请日:1988-02-11
Applicant: HOECHST AG
Inventor: URBACH HANSJOERG DR , HENNING RAINER DR , SCHOELKENS BERNWARD DR , BECKER REINHARD DR
IPC: C07D223/32 , A61K31/395 , A61K31/445 , A61K31/55 , A61K38/00 , A61P9/00 , A61P9/12 , A61P27/02 , A61P27/06 , A61P43/00 , C07D225/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07K5/02 , C07K5/06 , A61K37/02
Abstract: Cyclopenta-azocine and -azepine derivs. of formula (I) and their salts are new. In (I) m = 1 or 2; n = 0-2; R1 and R2 = H; 1-6C alkyl (opt. substd. once by OH, SH, 1-2C alkoxy, 1-2C alkylthio, COOH, 1-2C alkoxycarbonyl, 3-indolyl, imidazolyl, CONH2, amino or guanidino); 2-6C alkenyl; 3-9C cycloalkyl or cycloalkenyl; 3-7C cycloalkyl (1-4C) alkyl; 6-12C aryl (opt. partially hydrogenated) or 6-12C aryl (1-4C) alkyl (opt. OH substd. in aryl); R3 and R4 = H, 1-6C alkyl, 2-6C alkenyl or 6-12C aryl (1-4C) alkyl, opt. substd. in aryl by one MeO or NO2; Y = H or OH; Z = H; or Y and Z are together oxo; X = 1-6C alkyl (opt. substd. by NH2, acylamino, 1-6C alkylamino and/or di(1-4C)alkylamino); 2-6C alkenyl; 5-9C cycloalkyl, 1-R1-piperidin-4-yl, 6-12C aryl (opt. substd. by 1-3 of 1-4C alkyl or alkoxy, OH, halo, NO2, NH2 (itself opt. substd. by 1 or 2 1-4C alkyl) and/or methylenedioxy) or 3-indolyl; any free OH, SH, COOH, amino or guanidino can be protected conventionally.
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公开(公告)号:CZ381192A3
公开(公告)日:1993-12-15
申请号:CS381192
申请日:1992-12-21
Applicant: HOECHST AG
Inventor: HEITSCH HOLGER DR , HENNING RAINER DR , WAGNER ADALBERT DR , GERHARDS HERMANN DR , BECKER REINHARD DR , SCHOLKENS BERNWARD PROF DR
IPC: A61K31/415 , A61K31/4164 , A61K31/64 , A61P9/10 , A61P9/12 , C07D233/84 , C07D233/86 , C07D233/90
Abstract: Compounds of the formula (I) in which R is, for example, ethyl, R is, for example, methyl, n is, for example, zero, R is, for example, COOH and R is, for example, SO2NHCONHCH3 are highly active antagonists of angiotensin II receptors.
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公开(公告)号:AT97913T
公开(公告)日:1993-12-15
申请号:AT88101975
申请日:1988-02-11
Applicant: HOECHST AG
Inventor: URBACH HANSJOERG DR , HENNING RAINER DR , SCHOELKENS BERNWARD DR , BECKER REINHARD DR
IPC: C07D223/32 , A61K31/395 , A61K31/445 , A61K31/55 , A61K38/00 , A61P9/00 , A61P9/12 , A61P27/02 , A61P27/06 , A61P43/00 , C07D225/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07K5/02 , C07K5/06 , A61K37/02
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公开(公告)号:CZ9104162A3
公开(公告)日:1993-09-15
申请号:CS416291
申请日:1991-12-30
Applicant: HOECHST AG
Inventor: TEETZ VOLKER DR , GEIGER ROLF PROF DR , URBACH HANSJORG DR , BECKER REINHARD DR , SCHOLKENS BERNWARD DR
IPC: C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC classification number: C07K5/0222 , A61K38/00 , C07D209/52
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公开(公告)号:DE3280196D1
公开(公告)日:1990-07-26
申请号:DE3280196
申请日:1982-11-02
Applicant: HOECHST AG
Inventor: TEETZ VOLKER DR , GEIGER ROLF PROF DR , URBACH HANSJOERG DR , BECKER REINHARD DR , SCHOELKENS BERNWARD DR
IPC: C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/28 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
Abstract: Compounds of the formula I (I) in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring alpha -aminoacid, which may be protected, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
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公开(公告)号:HK74989A
公开(公告)日:1989-09-22
申请号:HK74989
申请日:1989-09-14
Applicant: HOECHST AG
Inventor: URBACH HANSJOERG DR , HENNING RAINER DR , TEETZ VOLKER DR , GEIGER ROLF PROF DR , BECKER REINHARD DR , GAUL HOLGER
IPC: A61K38/55 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P7/10 , A61P9/08 , A61P9/12 , C07D209/02 , C07D209/08 , C07D209/32 , C07D209/34 , C07D209/42 , C07D209/52 , C07D215/22 , C07D215/227 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06
Abstract: 1. Claims for the Contracting states ; BE, CH, DE, FR, GB, IT, Li, Lu, NL, SE A compound of the formula I see diagramm : EP0084164,P21,F7 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts. 1. Claims for the Contracting state : Austria A process for the preparation of the compounds of the formula I see diagramm : EP0084164,P24,F4 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts, which a) comprises reacting a compound of the formula II see diagramm : EP0084164,P24,F6 wherein R1 , R2 , X, Y and Z have the meanings as in formula I, with a compound of the formula III see diagramm : EP0084164,P25,F1 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2 and W denotes a radical which can be cleaved off by hydrogenolysis or by acid, and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or b) for the preparation of compounds of the formula I, in which Y and Z together denote oxygen, comprises b1 ) reacting a compound of the formula IV see diagramm : EP0084164,P25,F3 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n and R1 have the meanings as in formula I and W has the meaning as in formula III, with a compound of the formula V, R2 O2 C-CH = CH-CO-X wherein R2 and X have the meanings as in formula I, and subsequently splitting off the radical W and, if appropriate, also the radical R2 to form the free carboxyl groups, or, b2 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the general formula VI, wherein R2 has the meaning as in formula I, and with a compound of the general formula VII OHC-CO2 R2 X-CO-CH3 wherein X has the meaning as in formula I, subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl group, or c) for the preparation of compounds of the formula I, in which Y and Z each denote hydrogen, comprises c1 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the formula VIII see diagramm : EP0084164,P25,F2 wherein R2 and X have the meanings as in formula I, reducing the Schiff's bases obtained and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or c2 ) catalytically reducing a compound of the formula I in which Y and Z together denote oxygen, with hydrogen, or d) for the preparation of compounds of the formula I, in which Y denotes hydroxyl and Z denotes hydrogen, comprises reducing a compound of the formula I, in which Y and Z together denote oxygen, catalytically with hydrogen or with a reducing agent, such as sodium borohydride, and, if appropriate, converting the compounds obtained according to (a)-(d) into their physiologically acceptable salts.
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公开(公告)号:HK74889A
公开(公告)日:1989-09-22
申请号:HK74889
申请日:1989-09-14
Applicant: HOECHST AG
Inventor: TEETZ VOLKER DR , GEIGER ROLF PROF DR , URBACH HANSJOERG DR , BECKER REINHARD DR , SCHOELKENS BERNWARD DR
IPC: C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/28 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06 , C07C101/28 , C07C101/34
Abstract: Compounds of the formula I (I) in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring alpha -aminoacid, which may be protected, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
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公开(公告)号:DE3801587A1
公开(公告)日:1989-08-03
申请号:DE3801587
申请日:1988-01-21
Applicant: HOECHST AG
Inventor: RUEGER WOLFGANG DR , URBACH HANSJOERG DR , BECKER REINHARD DR , HOCK FRANZ DR
Abstract: The invention relates to amino acid esters of the formula (I) in which n=1 or 2, R, R1, R2 and R3 denote hydrogen or a defined radical, R4 together with R5 and the atoms carrying them form a heterocyclic ring system, processes for their preparation, agents containing them and their use.
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公开(公告)号:AT39931T
公开(公告)日:1989-01-15
申请号:AT84100130
申请日:1984-01-09
Applicant: HOECHST AG
Inventor: HENNING RAINER DR , URBACH HANSJOERG DR , TEETZ VOLKER DR , BECKER REINHARD DR
IPC: A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D209/96 , C07D317/28 , C07D317/30 , C07D317/32 , C07D317/72 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/078 , C07K14/81 , A61K37/02
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