-
公开(公告)号:NO831593A
公开(公告)日:1983-05-06
申请号:NO831593
申请日:1983-05-05
Applicant: HOECHST AG
Inventor: TEETZ VOLKER , GEIGER ROLF , URBACH HANSJOERG , BECKER REINHARD , SCHOELKENS BERWARD
IPC: C07C20060101 , C07C229/16 , C07C
-
公开(公告)号:NO823674L
公开(公告)日:1983-05-06
申请号:NO823674
申请日:1982-11-04
Applicant: HOECHST AG
Inventor: TEETZ VOLKER , GEIGER ROLF , URBACH HANSJOERG , BECKER REINHARD , SCHOELKENS BERNWARD
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 , C07D
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.
-
公开(公告)号:CA1341296C
公开(公告)日:2001-09-25
申请号:CA418453
申请日:1982-12-23
Applicant: HOECHST AG
Inventor: HENNING RAINER , URBACH HANSJORG , BECKER REINHARD , GAUL HOLGER , GEIGER ROLF , TEETZ VOLKER
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: Disclosed are cis, exo- and trans-compounds of the formula I (see formula I) in which n denotes 0, 1 or 2, R1 denotes hydrogen, (C1-C6)- alkyl which can optionally be substituted by amino, (C1-C4)- acyl- or bezoylamino, (C2-C6)-alkenyl, (C5-C9)-cycloalkyl, (C5-C9)-cycloalkenyl, (C5-C7)-cycloalkyl-(C1-C4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C1-C2)-alkyl, (C1-C2)-alkoxy or halogen, aryl-(C1-C4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R2 denotes hydrogen, (C1-C6)-alkyl, (C2-C6)alkenyl or aryl-(C1-C4)- alkyl Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C1-C6)-alkyl, (C2-C6)-alkenyl, (C5-C9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C1-C4)-alkyl, (C1-C4)-alkoxy, hydroxyl, halogen, nitro, amino, (C1-C4)- alkylamino, di-(C1-C4-alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process ofr the preparation thereof, agents containing them, their use as a medicine and intermediates for the prepara- tion thereof.
-
公开(公告)号:HRP940767A2
公开(公告)日:1997-02-28
申请号:HRP940767
申请日:1994-10-25
Applicant: HOECHST AG , RUHRCHEMIE AG
Inventor: WAGNER ADALBERT , ENGLERT HEINRICH , KLEEMANN HEINZ-WERNER , GERHARDS HERMAN , SCHOELKENS BERNWARD , BECKER REINHARD , LINZ WOLFGANG , CAILLE M JEAN-CLOUDE , VEVERT M JEAN-PAUL
IPC: A61K31/40 , A61K31/415 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/64 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D207/34 , C07D207/36 , C07D233/54 , C07D233/66 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/90 , C07D249/02 , C07D255/02 , C07D257/02 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D453/02 , C07D521/00
Abstract: Azole derivative of the general formula (I) in which A, L, O, R , X, Y, Z and q have the meanings given, a process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have, for example, the following meanings: R = (C2-C10)-alkyl Z = nitrogen X and Y = independently of one another CR L = -CH2- q = zero or 1 A = biphenyl radical which is substituted, for example, by R R = halogen or hydrogen R = SO2-NH-CO-OR and R = phenyl, are highly active antagonists of angiotensin II receptors.
-
公开(公告)号:BG60936B2
公开(公告)日:1996-06-28
申请号:BG9855194
申请日:1994-02-24
Applicant: HOECHST AG
Inventor: URBACH HANSJOERG , HENNING RAINER , TEETZ VOLKER , GEIGER ROLF , BECKER REINHARD , 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.
-
公开(公告)号:LT3373B
公开(公告)日:1995-08-25
申请号:LTIP716
申请日:1993-06-25
Applicant: HOECHST AG
Inventor: WAGNER ADALBERT , ENGLERT HEINRICH , KLEEMANN HEINZ-WERNER , GERHARDS HERMANN , SCHOELKENS BERNWARD , BECKER REINHARD , LINZ WOLFGANG
IPC: A61K20060101 , A61K31/40 , A61K31/425 , C07D20060101 , C07D207/30 , C07D257/04 , C09F20060101
Abstract: Azole derivatives, which have a general formula (I): where A, Z, O, R1, X, Y, Z and q have indicated meanings, their extraction method, pharmaceutical preparations and the use of these compounds, as medical substances. The azole derivatives, which have a formula (I), in which the symbols, for example, have these meanings:R - (C2-C10)-alkyl,Z - azote,X, Y - independently from one another, CR ,Z - -CH2-,q - 0 or 1,A - biphenyl residue, in which there is a substitute, for example, R ,R - halogen or hydrate,R - SO2-NH-CO-R andR - phenylare very effective antagonists of angiotensin-II-receptors.
-
公开(公告)号:NZ247059A
公开(公告)日:1995-03-28
申请号:NZ24705993
申请日:1993-03-04
Applicant: HOECHST AG
Inventor: HEITSCH HOLGER , HENNING RAINER , WAGNER ADALBERT , GERHARDS HERMANN , BECKER REINHARD , SCHOLKENS BERNWARD
IPC: A61K31/4164 , A61K31/64 , A61P9/10 , A61P9/12 , A61K31/415 , 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.
-
公开(公告)号:NO176763B
公开(公告)日:1995-02-13
申请号:NO880628
申请日:1988-02-12
Applicant: HOECHST AG
Inventor: URBACH HANSJORG , HENNING RAINER , SCHOLKENS BERNWARD , BECKER REINHARD
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.
-
公开(公告)号:AU653760B2
公开(公告)日:1994-10-13
申请号:AU9011091
申请日:1991-12-31
Applicant: HOECHST AG
Inventor: WAGNER ADALBERT , VEVERT JEAN-PAUL , CAILLE JEAN-CLAUDE , ENGLERT HEINRICH , KLEEMANN HEINZ-WERNER , GERHARDS HERMANN , SCHOLKENS BERNWARD , BECKER REINHARD , LINZ WOLFGANG
IPC: A61K31/40 , A61K31/415 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/64 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D207/34 , C07D207/36 , C07D233/54 , C07D233/66 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/90 , C07D249/02 , C07D255/02 , C07D257/02 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D453/02 , C07D521/00 , A61K31/41 , A61K31/495
Abstract: Azole derivative of the general formula (I) in which A, L, O, R , X, Y, Z and q have the meanings given, a process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have, for example, the following meanings: R = (C2-C10)-alkyl Z = nitrogen X and Y = independently of one another CR L = -CH2- q = zero or 1 A = biphenyl radical which is substituted, for example, by R R = halogen or hydrogen R = SO2-NH-CO-OR and R = phenyl, are highly active antagonists of angiotensin II receptors.
-
公开(公告)号:NO930817L
公开(公告)日:1993-09-08
申请号:NO930817
申请日:1993-03-05
Applicant: HOECHST AG
Inventor: HEITSCH HOLGER , HENNING RAINER , WAGNER ADALBERT , GERHARDS HERMANN , BECKER REINHARD , SCHOELKENS BERNWARD
IPC: A61K31/4164 , A61K31/64 , A61K31/415 , A61P9/10 , A61P9/12 , C07D233/84 , C07D233/86 , C07D233/90 , A61K31/45
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.
-
-
-
-
-
-
-
-
-