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    Peptide antagonists of bradykinin
    66.
    发明专利
    Peptide antagonists of bradykinin 未知

    公开(公告)号：CY2113B1

    公开(公告)日：2002-04-26

    申请号：CY9800030

    申请日：1998-09-29

    Applicant: HOECHST AG

    Inventor： BREIDOHL GERHARD DR ,  HENKE STEPHAN DR ,  KNOLLE JOCHEN DR ,  SCHOLKENS BERNWARD PROF DR ,  HOCK FRANZ DR

    IPC: A61K38/00 ,  A61K38/08 ,  A61K38/17 ,  A61P29/00 ,  A61P37/08 ,  C07K1/02 ,  C07K7/06 ,  C07K7/18 ,  A61K37/42

    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.

    69.
    发明专利
    未知

    公开(公告)号：BR9706387A

    公开(公告)日：2000-03-14

    申请号：BR9706387

    申请日：1997-12-17

    Applicant: HOECHST AG ,  GENENTECH INC

    Inventor： PEYMAN ANUSCHIRWAN DR ,  KNOLLE JOCHEN DR ,  WEHNER VOLKMAR DR ,  BREIPOHL GERHARD DR ,  GOURVEST JEAN-FRANCOIS DR ,  CARNIATO DENIS DR ,  GADEK THOMAS RICHARD DR

    IPC: C07D473/00 ,  A61K31/52 ,  A61P3/00 ,  A61P9/00 ,  A61P13/12 ,  A61P19/00 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D233/00 ,  C07D239/00 ,  C07D401/12 ,  C07D403/12 ,  C07D473/02 ,  C07D473/26 ,  C07D473/34 ,  C07D473/40

    Abstract: Purine derivatives of formula (I) and (Ia), and their salts, are new. One of R', R" = (CR1R2)nA-(CR1R2)m(CR1R3)i-(CR1R2)qR4 and the other = (CR1R2)rA'-(CR1R2)s(CR1R3)k-(CR1R2)tDE; X = H, NH2, OH, NHCOR6; A, A' = bond, CONR5, NR5CO, C(O), NR5, O, S, SO, SO2, Ar, 2-4C alkynylene, 2-4C alkenylene, or a 3-7 membered ring (optionally containing 1-2 Het and optionally substituted by =O, =S or R3); Ar = 5-14C arylene optionally with 1-5 C replaced by heteroatoms; R1, R2 = H, F, Cl, CN, nitro, 1-10C alkyl, 3-14C cycloalkyl, (3-12C cycloalkyl)(1-8C alkyl), 5-14C aryl, (5-14C aryl)(1-8C alkyl), R7-O-R6, R7-S(O)p-R6 or R7N-R6R61; R3 = H, F, Cl, CN, nitro, 1-14C alkyl, 3-14C cycloalkyl, (3-14C cycloalkyl)(1-8C alkyl), 5-14C aryl, (5-14C aryl)(1-8C alkyl), R7-O-R6, R7-S(O)p-R6, R7N-R6R61, R7OCOR6, R7COR6, R7COOR6, R7OCONR5R6, R7NR5S(O)pR6, R7NR5COOR6, R7NR5COR6, R7NR5CONR5R6, R7NR5S(O)pNR5R6, R7S(O)pR6, R7NS(O)pNR5R6, R7NR6COSR6, R7COR6 or R7CONR5R6, (where alkyl is optionally substituted, and alkyl (sic) and aryl are all optionally substituted, by one or more of F, Cl, Br, CN, NO2, R7NR5R6, R7NR6R61, R7COOR6, R7COR6, ; R7CONR5R6, R7S(O)pNR5R6, R6 or R7OR6); R4 = COR8, CSR8, S(O)pR8, POR8R81, a D- or L-aminoacid or a 4-8-membered saturated or unsaturated heterocycle containing 1-4 Het; R5 = H, 1-10C alkyl, 3-14C cycloalkyl, (3-14C cycloalkyl)-1-8C alkyl, 5-14C aryl or (5-14C aryl)-1-8C alkyl; R6, R61 = H, 1-8C alkyl, 3-14C cycloalkyl, 1-8C alkyl (substituted by 3-14C cycloalkyl or ArH) or ArH; or R6+R61 complete a ring system which may contain Het; R7 = a bond or 1-4C alkylene; R8, R81 = OH, 1-8C alkoxy, (5-14C aryl)(1-8C alkoxy), 5-14C aryloxy, (1-8C alkylcarbonyloxy)(1-4C alkoxy), (5-14C aryl)(1-8C alkyl)carbonyloxy(1-6C alkoxy), NR6R61, 1-8C dialkylaminocarbonylmethyloxy, (5-14C aryl)(1-8C dialkyl)aminocarbonylmethyloxy, 5-14C arylamino or an L or D amino acid; B = bond, O, S, NR5, NR5CO, CONR5, or a 3-7 membered ring (optionally containing 1-2 heteroatoms and optionally substituted by one or two =O, =S or R3); D = bond, NR6, CONR6, NR6CO, SO2NR6, NR6CONR6, NR6CSNR6, NR6S(O)uNR6, NR6COO, NR6N=CR6, NR6S(O)u, (5-14C aryl)CO, (5-14C aryl)S(O)u, N=CR6, CR6=N or CR6=N-NR6; E = H, NR6C(R6)=NR6, C(=NR6)NR6R61, NR6C(=NR6)NR6R61, or a 4-11 membered monocyclic or polycyclic aromatic or non-aromatic ring system (optionally containing 1-4 Het and optionally mono- to tri- substituted by R3, R5, =O, =S or C(=NR6)NR6R61); Het = N, O, S; n, m, s, t = 0-5; i, k = 0 or 1; p, q = 0-2; r = 0-6; u = 1 or 2.

    70.
    发明专利
    未知

    公开(公告)号：DK0672701T3

    公开(公告)日：2000-01-03

    申请号：DK95103319

    申请日：1995-03-08

    Applicant: HOECHST AG

    Inventor： UHLMANN EUGEN DR ,  KNOLLE JOCHEN DR ,  BREIPOHL GERHARD DR

    IPC: C07C231/02 ,  C07C233/36 ,  C07C233/47 ,  C07C237/12 ,  C07D239/46 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07K1/00 ,  C07K1/04 ,  C07K1/113 ,  C07K5/04 ,  C07K14/00 ,  C07K14/485 ,  C07K14/52 ,  C08G69/06 ,  C08G69/10

    Abstract: A process is claimed for preparing peptide nucleic acid (PNA) oligomers of formula (I). Ro=H, 1-18C alkanoyl, 2-19C alkoxycarbonyl, 3-8C cycloalkanoyl (sic), 7-15C aroyl, 3-13C heteroaroyl or a gp. which enhances the intracellular uptake of the oligomer or interacts with a target nucleic acid during hybridisation; A and Q=amino acid residues; k and m=0-20; B=a nucleotide base, opt. in prodrug form; Qo=OH, NH2 or NHR''; R''=1-18C alkyl, 2-18C aminoalkyl or 2-18C hydroxyalkyl; n=1-50. The process comprises: (a) opt. coupling amino acids (Q') to a support of formula L-(Polymer) by solid-phase synthesis to give (Q')m-L-(Polymer), where L=a linking gp. contg. Qo in latent form and Q'=Q with optional side-chain protection; (b) coupling a cpd. of formula (II) to L-(Polymer) or (Q')m-L-(Polymer), where PG=a base-labile protecting gp. and B'=a nucleotide base with a protected exocyclic amino gp.; (c) removing PG; (d) repeating steps (b) and (c) n-1 times; (e) opt. coupling amino acids (A') to the prod. by solid-phase synthesis, where A'=A with optional side-chain protection, and introducing Ro if Ro is other than H; and (f) cleaving the PNA oligomer from the prod. of formula (III) and simultaneously or subsequently deprotecting B', A' and Q'. Also claimed are cpds. (II) and a process for preparing them.

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