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    PEPTIDE, PROCESS OF ITS PREPARATION, ITS USE FOR PREPARING A MEDICAMENT AND PHARMACEUTICAL PREPARATION IN WHICH SAID PEPTIDE IS COMPRISED
    11.
    发明专利
    PEPTIDE, PROCESS OF ITS PREPARATION, ITS USE FOR PREPARING A MEDICAMENT AND PHARMACEUTICAL PREPARATION IN WHICH SAID PEPTIDE IS COMPRISED 未知

    公开(公告)号：CZ285698B6

    公开(公告)日：1999-10-13

    申请号：CZ57293

    申请日：1993-04-02

    Applicant: HOECHST AG

    Inventor： BREIPOHL GERHARD DR ,  HENKE STEPHAN DR ,  KNOLLE JOCHEN DR ,  SCHOLKENS BERNWARD PROF DR ,  ALPERMANN HANS-GEORG DR ,  GERHARDS HERMANN DR ,  WIRTH KLAUS DR

    IPC: A61K38/00 ,  A61K38/04 ,  A61K38/08 ,  A61P43/00 ,  C07K7/06 ,  C07K7/18

    Abstract: Peptides of the formula I Z - P - A - B - C - E - F - K - (D)Q - G- M- F' - I (I), in which Z is optionally substituted (cyclo)alk(ano)yl(sulphonyl), (C1-C8)-alkoxycarbonyl, (hetero)ar(o)yl(sulphonyl), carbamoyl, P is a direct linkage or a radical II -NR -(U)-CO- (II> in which R is H, methyl or a urethane protective group, U is (cyclo)(aryl)alkylidene, (hetero)arylidene or (CHR )n, R is hydrogen, (cyclo)alkyl, (hetero)aryl, or in which R and R form, together with the atoms carrying them, a ring system; A is defined as P; B is a basic amino acid in the L or D configuration, C is a compound of the formula IIIa or IIIb G'-G'-Gly (IIIa> G'-NH-(CH2)p-CO (IIIb> in which p is 2 to 8 and G' are, independently of one another, a radical of the formula IV -NR -CHR -CO- (IV> in which R and R form, together with the atoms carrying them, a heterocyclic ring system; E is the residue of a neutral, acid or basic, aliphatic or alicyclic-aliphatic amino acid; F are, independently of one another, the radical of a neutral, acid or basic, aliphatic or aromatic amino acid, or a direct linkage; (D)Q is D-Tic, D-Phe, D-Dic, D-Thi or D-Nal, or a radical of the formula (V) in which X is O, S or a direct linkage, and R is H, (cyclo)alkyl or aryl(alkyl), G is defined as G' above or is a direct linkage; F' is defined as F, is a radical -NH-(CH2)q- with q = 2 to 8 or, if G is not a direct linkage, can be a direct linkage, and I is -OH, -NH2 or NHC2H5; K is the radical -NH-(CH2)x-CO- with x = 1-4 or is a direct linkage, and M is defined as F and their physiologically tolerated salts are described. They have excellent bradykinin-antagonistic action. They are obtained by reacting a fragment with a C-terminal free carboxyl group or its activated derivative with an appropriate fragment with an N-terminal free amino group, or by assembling the peptide stepwise, eliminating one or more protective groups temporarily introduced where appropriate to protect other functionalities in the compound obtained in this way, and converting the compounds of the formula I obtained in this way where appropriate into their physiologically tolerated salt.

    ANTAGONISTS OF VITRONECTIN RECEPTORS, PROCESS OF THEIR PREPARATION AND USE
    13.
    发明专利
    ANTAGONISTS OF VITRONECTIN RECEPTORS, PROCESS OF THEIR PREPARATION AND USE 未知

    公开(公告)号：CZ411397A3

    公开(公告)日：1998-07-15

    申请号：CZ411397

    申请日：1997-12-18

    Applicant: HOECHST AG ,  GENENTECH INC

    Inventor： WEHNER VOLKMAR DR ,  STILZ HANS ULRICH DR ,  PEYMAN ANUSCHIRWAN DR ,  KNOLLE JOCHEN DR ,  RUXER JEAN-MARIE DR ,  CARNIATO DENIS DR ,  LEFRANCOIS JEAN-MICHEL ,  GADEK THOMAS RICHARD DR ,  MCDOWELL ROBERT DR

    IPC: C07D239/00 ,  A61K31/155 ,  A61K31/16 ,  A61K31/18 ,  A61K31/33 ,  A61K31/395 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/472 ,  A61K31/55 ,  A61K38/04 ,  A61P9/00 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C279/20 ,  C07C279/24 ,  C07C311/64 ,  C07C313/30 ,  C07C327/00 ,  C07D217/24 ,  C07D233/04 ,  C07D235/16 ,  C07D243/06 ,  C07D253/06 ,  C07D253/08 ,  C07D263/52 ,  C07D267/08 ,  C07D277/60 ,  C07D471/02 ,  C07D471/04 ,  C07D487/04 ,  C07K5/04

    Abstract: Guanidine and cycloguanidine derivatives of formula A-B-D-E-F-G (I) and their salts are new. A = R R N-C(=NR )NR Z- or a group of formula (a) or (b); Z = C(Q) or S(O)n; Q = O or S; n = 1 or 2; R = 5-10 membered mono- or polycyclic, aromatic or non-aromatic ring (optionally containing 1-4 N, O and/or S and optionally substituted by 1 or more of R -R ); B = direct bond; or alkyl, -CR =CR -, 5-10C aryl, 3-8C cycloalkyl or -C IDENTICAL C- (all optionally mono- or disubstituted by 1-8C alkyl), e.g. Me-Ph-Me or Et-CH=CH-; D, F = direct bond or alkyl, 5-10C aryl, -Q-; -NR -, -CO-NR -, -NR -CO-, -NR -C(Q)-NR -, -O-C(O)-,-C(O)-O-, -C(Q)-, -S(O)n, -S(O)n-NR , -NR -S(O)n, -CR =CR -, -C IDENTICAL C-, -NR -N=CR -, -N=CR -, -R C=N- or -CH(OH)- (all optionally mono- or disubstituted by alkyl, -CR -CR - or 5-6C aryl), e.g. Me-Ph-CH=CH- or Et-O-, and D is optionally linked to B via one of these substituents; E = template of a fibrinogen receptor antagonist; G = -CR R -(CR R )p-(CH2)p-R ; R , R = H; 1-10C alkyl (optionally substituted by 1 or more F); cycloalkyl; cycloalkyl-alkyl; aryl; aryl-alkyl; R OC(O)R ; R R NC(O)R ; or R C(O)R ; R -R = H; F; OH; alkyl; cycloalkyl; cycloalkyl-alkyl; R QR ; R CO2R ; R OC(O)R ; R -5-14C aryl-R ; R N(R )R ; R R NR ; R N(R )CO(O)R ; R S(O)n-N(R )R ; R QC(O)N(R )R ; R C(O)N(R )R ; R N(R )C(O)N(R )R ; R N(R )S(O)N(R )R ; R S(O)nR ; R C(O)R ; R N(R )C(O)R ; or R N(R )S(O)nR ; R = H; Alk; cycloalkyl; cycloalkyl-Alk; aryl; or aryl-Alk; Alk = alkyl (optionally substituted by 1 or more F); R = direct bond or alkyl; R = C(Q)R ; S(O)n-NR ; P(O)nR ; or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S, e.g. tetrazolyl, imidazolyl, pyrazolyl, oxazolyl or thiadiazolyl; R = OH; alkoxy; aryl-alkoxy; aryloxy; alkylcarbonyloxy-(1-4C) alkoxy; aryl-alkylcarbonyloxy-(1-6C) alkoxy; NH2; NH(alkyl); N(alkyl)2; aryl-alkylamino; dialkylaminocarbonylmethoxy; aryl- dialkylaminocarbonylmethoxy; arylamino; or a L- or D-aminoacid; R -R = H; 1-10C alkyl (optionally substituted by one or more F); 3-12C cycloalkyl; 3-12C cycloalkyl-alkyl; aryl; aryl-alkyl; NH2; R ONR ; R OR ; R OC(O)R ; R R NR ; R -aryl-R ; HO-alkyl-N(R )R ; R N(R )C(O)R ; R C(O)N(R )R ; R C(O)R ; R R N-C(=NR )-NR ; R R N-C(=NR ); or Q; or two adjacent R R substituents form -O-(CH2)n-O- or -OC(CH3)2O-; p, q = 0 or 1; alkyl moieties have 1-8C, cycloalkyl moieties 3-14C and aryl moieties 5-14C unless specified otherwise; compounds where E is a 6-membered aromatic ring (optionally containing 1-4 N and/or 1-4 substituents ) and the compound 4-methyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine are excluded.

    New pyrrolidone, imidazolone, furanone or thiophenone derivatives
    16.
    发明专利
    New pyrrolidone, imidazolone, furanone or thiophenone derivatives 未知

    公开(公告)号：DE19635522A1

    公开(公告)日：1998-03-05

    申请号：DE19635522

    申请日：1996-09-02

    Applicant: HOECHST AG

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

    IPC: C07D233/66 ,  C07D233/96 ,  C07D277/32 ,  C07D403/12 ,  C07D471/10 ,  A61K31/41 ,  A61K31/415 ,  A61K31/42 ,  A61K31/44 ,  A61K31/505 ,  C07D207/34 ,  C07D263/34 ,  C07D413/12 ,  C07D417/12

    Abstract: 5-Membered azacyclic derivatives (I) and their salts are new. W = C(R16)-D-B-A-R1 (a), C=C(R16)-D-B-A-R1 (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 R16 or mono- or disubstituted by =Q; Y = CQ or CH2; Z = N(R0), Q or CH2; A = bond, 1-8C alkanediyl, CR2=NNR2, NR2CQNR2, QCQ'NR2, NR2S(O)nNR2, OS(O)nNR2, S(O)nNR2, 3-12 cycloalkanediyl, C triple bond C, NR2CO, CONR2, NR2CO-5-14C arylene, O, S(O)n, 5-14C arylene, CO, CO-5-14C arylene, NR2, NR2SO2, OCO, COO, N=CR2 CR2=N, CR2=CR3 or S(O)n-5-14C arylene (all optionally substituted by NR2 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 triple bond C, NR2, CO, CONR2, NR2CO, NR2-CQ-NR2, OCO, COO, SO, SO2, SONR2, SO2NR2, NR2SO, NR2SO2, Q or CR2=CR3 (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, NR2, CONR2, NR2CO, NR2CQNR2, OCO, COO, CQ, SO, SO2, SO2NR2, NR2SO, NR2SO2, CR2=CR3, C triple bond C, CR2=NNR2, N=CR2, CR2=N or CHOH (all optionally mono- or disubstituted by 1-8C alkanediyl, CR2=CR3 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 = CR4R5(CR6R7)p(CH2)qR10; L = C(R16) or N; R0 = 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); R1 = NR2CR2(=NR2), C(=NR2)NR2R3, NR2C(=NR2)NR2R3, or a 4-14 membered mono- or polycyclic optionally aromatic ring (optionally containing 1-4 N, O and/or S and optionally substituted by R12-R15); R2, R3 = 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; NR9OR8, R9OR8, R9COOR8, R9-5-14C aryl-R8, R9N(R8)2, R9-NR8-(1-8C hydroxyalkyl), R9CON(R8)2, R9NR8COR8, R9COR8, C(=NR8)N(R8)2; NR8C(=NR8)N(R8)2 or (1-18C alkyl)-COO-1-6C alkoxycarbonyl; R4-R7 = H, F, OH, 1-8C alkyl, 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkyl, R9QR8, R9OCOR8, R9COOR8, R9-5-14C aryl-R8, R9N(R2)R8, R9N(R8)2, R9OCONR8R2, R9N(R2)S(O)nR8, R9NR2COQR8, R9NR2COR8, R9N(R2)CON(R2)R8, R9N(R2)S(O)nNR2R8, R9S(O)nR8, R9NR2COSR8, R9COR8, R9CONR2R8 or R9S(O)nNR2R8; R8 = 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); R9 = bond or 1-8C alkanediyl; R10 = CQR11, S(O)nR11, P(O)nR11 or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S atoms; R11 = 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; R12-R15 = 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, R9OR8, R9COOR8, R9N(R8)2, R9-5-14C aryl-R8; R9-NR2 (1-8C hydroxyalkyl), R9CON(R2)R8, R9N(R2)COR8, R9COR8, NR2C(=NR3)-NR2R3, C(=NR2)NR2R3 or Q; or 2 of R12-R15 which are adjacent form -OCH2O-, -OCH2CH2O- or -OC(CH3)2O-; R16 = 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

    18.
    发明专利
    未知

    公开(公告)号：ID17828A

    公开(公告)日：1998-01-29

    申请号：ID972574

    申请日：1997-07-24

    Applicant: HOECHST AG ,  GENENTECH INC

    Inventor： WEHNER VOLKMAR DR ,  KNOLLE JOCHEN DR ,  STILZ HANS ULRICH DR ,  GOURVEST JEAN-FRANCOIS DR ,  CARNIATO DENIS DR ,  GADEK THOMAS RICHARD DR ,  MCDOWELL ROBERT DR ,  PITTI ROBERT MAURICE ,  BODARY SARAH CATHERINE DR

    IPC: C07C229/04 ,  A61K31/19 ,  A61K31/197 ,  A61K31/415 ,  A61K31/445 ,  A61P3/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P19/08 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C251/02 ,  C07D211/18 ,  C07D233/52 ,  C07D233/54 ,  C07D233/66 ,  C07D257/04 ,  C07D ,  A61K

    Abstract: Aromatic compounds of formula R1YABDEF'CR R R )p(CH2)q-R (I) and their salts are new. A = bond, Z, 1-8C alkanediyl, NR C(Q)NR , NR C(Q)Q, NR S(O)nNR , NR S(O)nO, NR -S(O)n, 3-12C cycloalkanediyl, C IDENTICAL C, NR C(O), C(O)NR , 5-14C arylene-C(O)NR , O, S(O)n, 5-14C arylene, CO, 5-14C arylene-CO, NR , SO2NR , CO2, CR =CR or 5-14C arylene-S(O)n (all optionally mono- or disubstituted by 1-8C alkanediyl, i.e. e.g. 1-8C alkanediyl-CONR -1-8C alkanediyl, 1-8C alkanediyl-CONR or CONR -1-8C alkanediyl); Z = NR -N=CR , N=CR or CR =N; Q = O or S; B = direct bond, 1-8C alkanediyl, CR =CR or C IDENTICAL C (all optionally mono- or disubstituted by 1-8C alkanediyl) or a divalent residue of a 5- or 6-membered saturated or unsaturated ring containing 1 or 2 N atoms (optionally mono- or disubstituted by 1-6C alkyl or Q); D, F' = bond, 1-8C alkanediyl, or Z, Q, NR , CONR , NR CO, NR C(Q)NR , OC(O), C(O)O, CQ, S(O), S(O)2, S(O)2NR , NR S(O), NR S(O)2, CR =CR , C IDENTICAL C or CH(OH) (all optionally mono- or disubstituted by 1-8C alkanediyl); E = 6-membered aromatic group optionally containing 1-4 N atoms (optionally mono- to tetra-substituted by R , R , F, Cl, Br, I, NO2 and OH); Y = bond or NR ; R = NR CR ), C(=NR )NR R , NR C(=NR )NR R , or a 4-10 membered monocyclic or polycyclic aromatic or non-aromatic ring optionally containing 1-4 N, O and/or S atoms (optionally substituted by 1 or more R -R ); R , R = H, 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-(1-8C)alkanediyl, 5-14C aryl, 5-14C aryl-(1-8C)alkanediyl, NH2, R NR OR , R OR , R COOR , R -5-14C arylene-R , R N(R )2, R NR 1-8C alkanediyl-OH, R CON(R )2, R NR C(O)R , R C(O)R , C(=NR )N(R )2 or (1-18C)alkylcarbonyloxy(1-6)alkanediyloxycarbonyl; R -R = H, F, OH, 1-8C alkyl, 3-12C cycloalkyl, 3-12C-cycloalkyl(1-8C)alkanediyl, R QR , R OCOR , R COOR , R -5-14C arylene-R , etc.; R = H, 1-8C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 1-8C-alkanediyl-3-12C cycloalkyl, 5-14C aryl or 1-8C alkanediyl-5-14C aryl; R = direct bond or 1-8C alkanediyl; R = C(Q)R , S(O)nR , P(O)(R )n or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S atoms; R = OH, 1-8C alkoxy, 1-8C alkanediyl-5-14C-aryl, 5-14C aryloxy, 1-4C alkanediyloxycarbonyl1-8C alkylcarbonyloxy, 5-14C aryl-1-8C alkanediylcarbonyloxy-1-6C alkanediyloxy, NH2, NH(1-8C alkyl), N(1-8C alkyl)2, 5-14C aryl-1-8C alkanediylamino, 1-8C dialkylaminocarbonylmethyleneoxy, 5-14C aryl-1-8C dialkylaminocarbonylmethyleneoxy, 5-14C arylamino or the residue of a L- or D-amino acid; R -R = H, 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, etc.; n = 1 or 2; p, q = 0 or 1; provided that at least 1 of A, D and F' = Z.

    19.
    发明专利
    未知

    公开(公告)号：DE19629816A1

    公开(公告)日：1998-01-29

    申请号：DE19629816

    申请日：1996-07-24

    Applicant: HOECHST AG

    Inventor： WEHNER VOLKMAR DR ,  KNOLLE JOCHEN DR ,  STILZ HANS ULRICH DR ,  GOURVEST JEAN-FRANCOIS DR ,  CARNIATO DENIS DR ,  GADEK THOMAS RICHARD DR ,  MAC DOWELL ROBERT DR ,  PITTI ROBERT MAURICE ,  BODARY SARAH CATHERINE DR

    IPC: C07C229/04 ,  A61K31/155 ,  A61K31/197 ,  A61K31/27 ,  A61K31/415 ,  A61K31/445 ,  A61K31/505 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C251/02 ,  C07C279/20 ,  C07C333/00 ,  C07D233/48 ,  C07D233/54 ,  C07D239/16 ,  C07D239/72 ,  C07D239/84 ,  C07C279/22 ,  C07C277/08 ,  C07B41/08 ,  C07B47/00 ,  A61K31/325 ,  C07B51/00 ,  C07D401/12 ,  C07D227/00 ,  C07D247/02 ,  C07D471/04 ,  A61K31/33

    Abstract: Substituted cycloalkanes of formula R YABDEF'C(R )(R )(CH2)qR (I) and their salts are new. A = bond, 1-8C alkanediyl, NR C(Q)NR , NR C(Q)Q, NR S(O)nNR , NR S(O)nO, NR S(O)n, 3-12C cycloalkanediyl, C IDENTICAL C, NR CO, CONR , 5-14C arylene-CONR , O, S(O)n, 5-14C arylene, CO, 5-14C arylene-CO, NR , SO2NR , CO2, CR =CR or 5-14C arylene-S(O)n (all optionally mono- or disubstituted by 1-8C alkanediyl (sic), e.g. -1-8C alkanediyl-CONR -1-8C alkanediyl, 1-8C alkanediyl-CONR or CONR -1-8C alkanediyl); Q = O or S; B = bond, 1-10C alkanediyl, CR =CR or C IDENTICAL C (all optionally mono- or disubstituted by 1-8C alkanediyl); D, F' = bond, 1-8C alkanediyl, or Q, NR , CONR , NR CO, NR C(Q)NR , OCO, COO, CQ, S(O)n, S(O)2NR , NR S(O)n, CR =CR , C IDENTICAL C or CH(OH) (all optionally mono- or disubstituted by 1-8C alkanediyl); E = 6-membered aromatic group optionally containing 1-4 N atoms and optionally mono- to tetra-substituted by R , R , F, Cl, Br, I, NO2 and OH; Y = bond or NR ; R = NR C(=NR )R , C(=NR )NR R , NR C(=NR )NR R or a 4-10 membered monocyclic or polycyclic aromatic or non-aromatic ring optionally containing 1-4 N, O and/or S atoms and optionally substituted by 1 or more R , R , R and R ; R , R = H, 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl, 5-14C aryl-1-8C alkanediyl, NH2, R N(R )OR , R OR , R COOR , R -5-14C arylene-R , R NR R , R NR -1-8C hydroxyalkyl, R CONR R , R NR C(O)R , R COR , C(=NR )NR R or 1-18C alkylcarbonyloxy-1-6C alkanediyloxycarbonyl; R = R QR , R OCOR , R COOR , R -5-14C arylene-R , R NR R , R NR R , R OCONR R , R NR S(O)nR , R NR COQR , R NR C(O)R , R N(R )C(O)N(R )R , R N(R )S(O)nN(R )R , R S(O)nR , R C(O)R , R CONR R , R S(O)nNR R , Cy or 1-8C alkyl substituted by Cy; Cy = monocyclic or polycyclic, saturated or mono- or poly-unsaturated 10-18C cycloalkyl optionally substituted by 1 or more Z'; Z' = 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl, 5-14C aryl-1-8C alkanediyl, 1-8C alkoxy, 5-14C aryl-1-8C alkanediyloxy, 5-14C aryloxy, 1-8C alkylcarbonyloxy-1-4C alkanediyloxy, NH2, NH(1-8C alkyl), N(1-8C alkyl)2, 5-14C aryl-1-8C alkanediylamino, 5-14C arylamino, =Q, NO2, OH, F, Cl, Br or I; R = H, F, 1-8C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl or 5-14C aryl-1-8C alkanediyl; R = Cy or 1-8C alkyl substituted by Cy; R = bond or 1-8C alkanediyl; R = H, 1-8C alkyl (optionally substituted by 1 or more F, or one 3-12C cycloalkyl or 5-14C aryl), 3-12C cycloalkyl or 5-14C aryl; R = C(Q)R , S(O)nR , P(O)(R )n or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S atoms; R = OH, 1-8C alkoxy(optionally substituted by 5-14C-aryl), 5-14C aryloxy, 1-8C alkylcarbonyloxy-1-4C alkanediyloxy, 5-14C aryl-1-8C alkanediylcarbonyloxy-1-6C alkanediyloxy, NH2, mono- or di- 1-8C alkylamino, 5-14C aryl-1-8C alkanediylamino, 1-8C dialkylaminocarbonylmethyleneoxy, 5-14C aryl-1-8C dialkylaminocarbonylmethyleneoxy, 5-14C arylamino or the residue of a L- or D-amino acid; R -R = H, 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl, 5-14C aryl-1-8C alkanediyl, NH2, R N(R )OR , R OR , R COOR , R NR R , R NR -1-8C hydroxyalkyl, R CONR R , R COR , NR C(=NR )NR R , C(=NR )NR R , R -5-14C arylene-R , R NR COR or Q; n = 1 or 2; q = 0 or 1.

    Peptide antagonists of bradykinin
    20.
    发明专利
    Peptide antagonists of bradykinin 未知

    公开(公告)号：GR3023172T3

    公开(公告)日：1997-07-30

    申请号：GR970400829

    申请日：1997-04-18

    Applicant: HOECHST AG

    Inventor： BREIPOHL GERHARD DR ,  HENKE STEPHAN DR ,  KNOLLE JOCHEN DR ,  SCHOELKENS BERNWARD PROF DR ,  HOCK FRANZ DR

    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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