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    2.
    发明专利
    未知

    公开(公告)号：PT796855E

    公开(公告)日：2002-07-31

    申请号：PT97103712

    申请日：1997-03-06

    Applicant: HOECHST AG ,  GENENTECH INC

    Inventor： GOURVEST JEAN-FRANCOIS ,  WEHNER VOLKMAR ,  JOCHEN KNOLLE ,  HANS ULRICH STILZ ,  DENIS CARNIATO ,  TOM GADEK ,  ROBERT MCDOWELL

    IPC: C07D233/24 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/435 ,  A61K31/505 ,  A61P3/08 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D233/76 ,  C07D233/96 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/04

    Abstract: 5-Membered azacyclic derivatives (I) and their salts are new. W = C(R )-D-B-A-R (a), C=C(R )-D-B-A-R (b) or a group of formula (c) or (d); the ring of formula (e) is saturated or partly or fully unsaturated, and optionally contains 1 or 2 N, O and/or S atoms and is optionally mono-, di- or trisubstituted by R or mono- or disubstituted by =Q; Y = CQ or CH2; Z = N(R ), Q or CH2; A = bond, 1-8C alkanediyl, CR =NNR , NR CQNR , QCQ'NR , NR S(O)nNR , OS(O)nNR , S(O)nNR , 3-12 cycloalkanediyl, C IDENTICAL C, NR CO, CONR , NR CO-5-14C arylene, O, S(O)n, 5-14C arylene, CO, CO-5-14C arylene, NR , NR SO2, OCO, COO, N=CR CR =N, CR =CR or S(O)n-5-14C arylene (all optionally substituted by NR and/or by 1 or 2 1-8C alkanediyl); Q, Q' = O or S; B = bond, 1-8C alkanediyl, 5-10C arylene, 3-8C cycloalkanediyl, C IDENTICAL C, NR , CO, CONR , NR CO, NR -CQ-NR , OCO, COO, SO, SO2, SONR , SO2NR , NR SO, NR SO2, Q or CR =CR (all optionally mono- or disubstitute d by 1-6C alkanediyl) or a divalent residue of a 5-6 membered saturated or unsaturated ring containing 1 or 2 N atoms (optionally mono- or disubstituted substituted by 1-6C alkyl or =Q); D, F = bond, 1-8C alkanediyl, 5-10C arylene, Q, NR , CONR , NR CO, NR CQNR , OCO, COO, CQ, SO, SO2, SO2NR , NR SO, NR SO2, CR =CR , C IDENTICAL C, CR =NNR , N=CR , CR =N or CHOH (all optionally mono- or disubstituted by 1-8C alkanediyl, CR =CR or 5-6C arylene); E = bond, 1-6C alkanediyl, 2-6C alkenediyl, 2-6C alkynediyl, phenylene, phenylene-1-3C alkanediyl or 1-3C alkanediyl-phenylene; G = CR R R )p(CH2)qR ; L = C(R ) or N; R = H, 1-8C alkyl (optionally substituted by 3-12C cycloalkyl or 5-14C aryl), 1-8C alkylcarbonyl, 3-12C cycloalkyl-carbonyl, (3-12C cycloalkyl- or 5-14C aryl-substituted) 1-6C alkylcarbonyl, 5-14C aryl-carbonyl, 3-12C cycloalkyl or 5-14C aryl (where all alkyl are optionally substituted by 1 or more F); R = NR CR ), C(=NR )NR R , NR C(=NR )NR R , or a 4-14 membered mono- or polycyclic optionally aromatic ring (optionally containing 1-4 N, O and/or S and optionally substituted by R -R ); R , R = H. 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkyl, 5-14C aryl, 5-14C aryl-1-8C alkyl, NH2; NR OR , R OR , R COOR , R -5-14C aryl-R , R N(R )2, R -NR -(1-8C hydroxyalkyl), R CON(R )2, R NR COR , R COR8, C(=NR )N(R )2; NR C(=NR )N(R )2 or (1-18C alkyl)-COO-1-6C alkoxycarbonyl; R -R = H, F, OH, 1-8C alkyl, 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkyl, R QR , R OCOR , R COOR , R -5-14C aryl-R , R N(R )R , R N(R )2, R OCONR R , R N(R )S(O)nR , R NR COQR , R NR COR , R N(R )CON(R )R , R N(R )S(O)nNR R , R S(O)nR , R NR COSR , R COR , R CONR R or R S(O)nNR R ; R = H, 1-8C alkyl (optionally substituted by 3-12C cycloalkyl or 5-14C aryl), 3-12C cycloalkyl or 5-14C aryl (where all alkyl are optionally substituted by 1 or more F); R = bond or 1-8C alkanediyl; R = CQR , S(O)nR , P(O)nR or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S atoms; R = OH, 1-8C alkoxy, 5-14C aryl-1-8C alkoxy, 5-14C aryloxy, 1-8C alkylcarbonyloxy-1-4C alkoxy, 5-14C aryl-1-8C alkylcarbonyloxy-1-4C alkoxy, NH2, mono- or di-1-8C alkylamino, 5-14C aryl-1-8C alkylamino, 1-8C dialkylaminocarbonylmethoxy, 5-14C aryl-1-8C dialkylaminocarbonylmethoxy, 5-14C arylamino or a D- or L-amino acid; R -R = H, 1-10C alkyl (optionally substituted by one or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkyl, 5-14C aryl, 5-14C aryl-1-8C alkyl, NH2, R OR , R COOR , R N(R )2, R -5-14C aryl-R ; R -NR (1-8C hydroxyalkyl), R CON(R )R , R N(R )COR , R COR , NR C(=NR )-NR R , C(=NR )NR R or Q; or 2 of R -R which are adjacent form -OCH2O-, -OCH2CH2O- or -OC(CH3)2O-; R = H, 1-10C alkyl optionally substituted by 1 or more F, 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkyl, 5-14C aryl, 5-14C aryl-1-8C alkyl, 2-20C alkenyl or 2-10C alkynyl; m = 1-6; n = 1 or 2; p, q = 0 or 1; with provisos.

    Peptide as bradykinin-antagonistes
    8.
    发明专利
    Peptide as bradykinin-antagonistes 未知

    公开(公告)号：LV10290B

    公开(公告)日：1995-08-20

    申请号：LV920699

    申请日：1992-12-23

    Applicant: HOECHST AG

    Inventor： GERHARD BREIPOHL ,  STEPHAN HENKE ,  JOCHEN KNOLLE ,  BERNWARD SCHILKENS ,  FRANZ HOCK

    IPC: A61K38/00 ,  A61K38/08 ,  A61K38/17 ,  A61P29/00 ,  A61P37/08 ,  C07K1/02 ,  C07K7/06 ,  C07K7/18

    Abstract: Peptides of the formula I A-B-C-E-F-K-(D)-Tic-G-M-F'-I (I> in which A is hydrogen, alkyl, alkanoyl, alkoxycarbonyl, alkylsulphonyl, cycloalkyl, aryl, arylsulphonyl, heteroaryl or an amino acid, each of which can optionally be substituted, B is a basic amino acid, C is a di- or tripeptide, E is the residue of an aliphatic or alicyclic-aliphatic amino acid, F is, independently of one another, an amino acid which is optionally substituted in the side chain or is a direct bond, G is an amino acid, F' is defined as F, can be -NH-(CH2)2-8 or a direct bond, I is -OH, -NH2 or -NHC2H5, and K is a radical -NH-(CH2)1-4-CO-, or is a direct bond, have a bradykinin-antagonistic action. Their therapeutic uses comprise all pathological states which are mediated, induced or assisted by bradykinin and bradykinin-related peptides. The peptides of the formula I are prepared by known methods of peptide synthesis.

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