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    PHARMACEUTICAL COMPOSITION FOR TREATING HYPERTENSION
    1.
    发明专利
    PHARMACEUTICAL COMPOSITION FOR TREATING HYPERTENSION 失效

    公开(公告)号：JPH10182456A

    公开(公告)日：1998-07-07

    申请号：JP31385097

    申请日：1997-11-14

    Applicant: HOECHST AG

    Inventor： BECKER REINHARD ,  HENNING RAINER ,  RUEGER WOLFGANG ,  TEETZ VOLKER ,  URBACH HANSJOERG

    IPC: A61K31/40 ,  A61K31/401 ,  A61K31/435 ,  A61K31/44 ,  A61K38/05 ,  A61K38/55 ,  A61K45/06 ,  A61P3/00 ,  A61P3/14 ,  A61P9/12 ,  A61P43/00

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject composition capable of enhancing effects of either one of an angiotensin converting enzyme inhibitor and a calcium antagonist with each other and administration of the both is reduced without manifesting adverse effects, by making the composition include both the substances. SOLUTION: This pharmaceutical composition comprises (A) an angiotensin converting enzyme inhibitor or its physiologically permissible salt, ramipril 2-[N-(1,S-ethoxycarbonyl-3-phenylpropyl-S-alanyl]-(1S,3S,5S)-2- azabicyclo-[3.3.0]octane-3-carbonic acid} represented formula I and (B) a calcium antagonist or its physiologically permissible salt felodipine [4-(2,3- dichlorophenyl)-2,6-dimethyl-3-methoxycarbonyl-5-ethoxycarbonyl-1,4- dihydropyridine] represented by formula II at a ratio of e.g. 1-5 pts.wt. ingredient A to 15-1 pts.wt. ingredient B.

    6.
    发明专利
    未知

    公开(公告)号：DK170444B1

    公开(公告)日：1995-09-04

    申请号：DK576782

    申请日：1982-12-28

    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.

    8.
    发明专利
    未知

    公开(公告)号：NO176763C

    公开(公告)日：1995-05-24

    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.

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