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    92.
    发明专利
    未知

    公开(公告)号：AT182602T

    公开(公告)日：1999-08-15

    申请号：AT95103319

    申请日：1995-03-08

    Applicant: HOECHST AG

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

    95.
    发明专利
    未知

    公开(公告)号：ID19253A

    公开(公告)日：1998-06-28

    申请号：ID973918

    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: A61K31/155 ,  A61K31/16 ,  A61K31/18 ,  A61K31/33 ,  A61K31/395 ,  A61K31/415 ,  A61K31/4184 ,  C07D239/00 ,  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 ,  C07K5/08 ,  A61K38/00 ,  A61K39/00 ,  A61K31/00 ,  C07D401/02 ,  C07D519/00

    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.

    IMINO DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF
    98.
    发明专利
    IMINO DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF 未知

    公开(公告)号：CZ234497A3

    公开(公告)日：1998-03-18

    申请号：CZ234497

    申请日：1997-07-22

    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

    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.

    New pyrrolidone, imidazolone, furanone or thiophenone derivatives
    99.
    发明专利
    New pyrrolidone, imidazolone, furanone or thiophenone derivatives 未知

    公开(公告)号：DE19626701A1

    公开(公告)日：1998-01-08

    申请号：DE19626701

    申请日：1996-07-03

    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: C07D233/76 ,  C07D233/96 ,  C07D403/12 ,  C07D471/10 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/47 ,  A61K31/505 ,  C07K5/06

    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?=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?=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?=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 (CR 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 (=NR ), 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 o

    100.
    发明专利
    未知

    公开(公告)号：ES2099102T3

    公开(公告)日：1997-05-16

    申请号：ES91106663

    申请日：1991-04-25

    Applicant: HOECHST AG

    Inventor： BREIPOHL 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

    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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