中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

59 records (took 0.023 seconds)

    ANTAGONISTS OF VITRONECTIN RECEPTORS, PROCESS OF THEIR PREPARATION AND USE
    41.
    发明专利
    ANTAGONISTS OF VITRONECTIN RECEPTORS, PROCESS OF THEIR PREPARATION AND USE 未知

    公开(公告)号：CZ411297A3

    公开(公告)日：1998-07-15

    申请号：CZ411297

    申请日：1997-12-18

    Applicant: HOECHST AG ,  GENENTECH INC

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

    IPC: C07D295/18 ,  A61K31/33 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/536 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/66 ,  A61P9/00 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D235/30 ,  C07D239/84 ,  C07D243/06 ,  C07D243/24 ,  C07D253/06 ,  C07D253/08 ,  C07D263/52 ,  C07D265/12 ,  C07D265/18 ,  C07D267/08 ,  C07D277/60 ,  C07D279/00 ,  C07D471/04 ,  C07D521/00 ,  C07F9/6561

    Abstract: Amino substituted heterobicyclic and heteropolycyclic compounds of formula (I) and their salts are new: A = 5-10 membered mono- or polycyclic, aromatic or non-aromatic ring (optionally containing 1-4 N, O and/or S and optionally substituted by one or more of R -R ; B = direct bond; or alkyl, -CR =CR -, 5-10C aryl, 3-8C cycloalkyl, -C C-, -NR -, -NR -C(O)-, -NR -C(Q)-NR -, -O-C(O)-, -NR -S(O)n-, -Q- or -CR =CR - (all optionally mono- or disubstituted by alkyl), e.g. Me-Ph-Me or -Et-NR -C(O)-; Q = O or S; n = 1 or 2; 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-, -S(O)n, -S(O)n-NR , -NR -S(O)n, -CR =CR - or -C IDENTICAL C- (all optionally mono- or disubstituted by alkyl, -CR -CR - or 5-6C aryl); provided that D is not -CO-NR -, -C(O)-O-, -S(O)n or -S(O)n-NR if B is a direct bond; E = template of a fibrinogen receptor antagonist; G = -CR R -(CR R )p-(CH2)q-R ; R , R = H; 1-10C alkyl (optionally substituted by 1 or more F); 3-12C cycloalkyl; 3-12C 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 -aryl-R ; R N(R )R ; R R NR ; R N(R )CO(O)R ; R S(O)-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 one or more F); R = direct bond or alkyl; R = C(Q)R ; S(O)-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-; Y = NR or Q; p, q = 0 or 1; unless specified otherwise alky moieties have 1-8C, cycloalkyl moieties 3-14C and aryl moieties 5-14C; the compounds where E is a 6-membered aromatic ring (optionally containing 1-4 N atoms and/or 1-4 substituents) and the compound 4-methyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine are excluded.

    42.
    发明专利
    未知

    公开(公告)号：ID19245A

    公开(公告)日：1998-06-28

    申请号：ID973917

    申请日：1997-12-18

    Applicant: HOECHST AG ,  GENENTECH INC

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

    IPC: C07D295/18 ,  A61K31/33 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/536 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/66 ,  A61P9/00 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D235/30 ,  C07D239/84 ,  C07D243/06 ,  C07D243/24 ,  C07D253/06 ,  C07D253/08 ,  C07D263/52 ,  C07D265/12 ,  C07D265/18 ,  C07D267/08 ,  C07D277/60 ,  C07D279/00 ,  C07D471/04 ,  C07D521/00 ,  C07F9/6561 ,  A61K38/00 ,  A61K39/00 ,  A61K31/00 ,  C07D487/04 ,  C07D401/102 ,  C07D519/00 ,  C07K5/08

    Abstract: Amino substituted heterobicyclic and heteropolycyclic compounds of formula (I) and their salts are new: A = 5-10 membered mono- or polycyclic, aromatic or non-aromatic ring (optionally containing 1-4 N, O and/or S and optionally substituted by one or more of R -R ; B = direct bond; or alkyl, -CR =CR -, 5-10C aryl, 3-8C cycloalkyl, -C C-, -NR -, -NR -C(O)-, -NR -C(Q)-NR -, -O-C(O)-, -NR -S(O)n-, -Q- or -CR =CR - (all optionally mono- or disubstituted by alkyl), e.g. Me-Ph-Me or -Et-NR -C(O)-; Q = O or S; n = 1 or 2; 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-, -S(O)n, -S(O)n-NR , -NR -S(O)n, -CR =CR - or -C IDENTICAL C- (all optionally mono- or disubstituted by alkyl, -CR -CR - or 5-6C aryl); provided that D is not -CO-NR -, -C(O)-O-, -S(O)n or -S(O)n-NR if B is a direct bond; E = template of a fibrinogen receptor antagonist; G = -CR R -(CR R )p-(CH2)q-R ; R , R = H; 1-10C alkyl (optionally substituted by 1 or more F); 3-12C cycloalkyl; 3-12C 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 -aryl-R ; R N(R )R ; R R NR ; R N(R )CO(O)R ; R S(O)-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 one or more F); R = direct bond or alkyl; R = C(Q)R ; S(O)-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-; Y = NR or Q; p, q = 0 or 1; unless specified otherwise alky moieties have 1-8C, cycloalkyl moieties 3-14C and aryl moieties 5-14C; the compounds where E is a 6-membered aromatic ring (optionally containing 1-4 N atoms and/or 1-4 substituents) and the compound 4-methyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine are excluded.

    45.
    发明专利
    未知

    公开(公告)号：ID18919A

    公开(公告)日：1998-05-20

    申请号：ID973671

    申请日：1997-11-13

    Applicant: HOECHST AG

    Inventor： STILZ HANS ULRICH DR ,  WEHNER VOLKMAR DR ,  HULS CHRISTOPH DR ,  SEIFFGE DIRK DR

    IPC: A61K38/00 ,  A61K38/05 ,  C07D277/20 ,  A61K38/06 ,  A61K38/07 ,  A61P3/08 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P33/02 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D233/54 ,  C07D233/72 ,  C07D277/34 ,  C07K5/06 ,  C07K5/078 ,  C07K5/097 ,  C07K5/107 ,  C07K5/11 ,  C07K5/117 ,  A61K38/04 ,  A61K39/395

    Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer or mixture forms, or their salts as medicaments is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = direct bond, 3-12C cycloalkylene, (1-6C) alkylene-(3-12C) cycloalkylene, phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally mono- or disubstituted) etc.; B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenylene; D = CR2R3, NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het '-alkyl (where alkyl residues are optionally substituted by one or more F); R1 = SR21, SSR21, SOR22, SO2R22, S-OR21, SO-OR21, SO2-OR21, SCOR21, SCOOR22, SCSSR22, OCOR21, OCSR21, OCOOR22, OSO2R22, OSO-R22, OP(O)(OR21)2, P(O)(OR21)2, P(O)(R22)OR21, CN, halo etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl, alkenyl, alkynyl, alkenylcarbonyl, alkynylcarbonyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl or (3-8C) cycloalkylalkyl; R21 = H, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het'-alkyl (where alkyl residues are optionally substituted by one or more F); b, c, d, f = 0 or 1 provided not all are 0; e, g,h = 0-6; Ar = optionally substituted 6-14C aryl; Het' = optionally substituted heteroaryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.

    46.
    发明专利
    未知

    公开(公告)号：DE19647381A1

    公开(公告)日：1998-05-20

    申请号：DE19647381

    申请日：1996-11-15

    Applicant: HOECHST AG

    Inventor： STILZ HANS ULRICH DR ,  WEHNER VOLKMAR DR ,  HUELS CHRISTOPH DR ,  SEIFFGE DIRK DR

    IPC: C07D277/20 ,  A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61P3/08 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P33/02 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D233/54 ,  C07D233/72 ,  C07D277/34 ,  C07K5/06 ,  C07K5/078 ,  C07K5/097 ,  C07K5/107 ,  C07K5/11 ,  C07K5/117 ,  C07D521/00 ,  C07K5/00 ,  C07D233/02 ,  C07D263/02 ,  C07D277/02 ,  C07D207/08 ,  C07D403/02 ,  A61K38/04 ,  A61K31/395

    Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer or mixture forms, or their salts as medicaments is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = direct bond, 3-12C cycloalkylene, (1-6C) alkylene-(3-12C) cycloalkylene, phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally mono- or disubstituted) etc.; B = 1-6C alkylene (optionally substituted), 2-6C alkenylene, phenylene, phenylene-(1-3C) alkyl or (1-3C) alkylene-phenylene; D = CR2R3, NR3 or CH=CR3; E = tetrazolyl, SO3H etc.; R = H, alkyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het '-alkyl (where alkyl residues are optionally substituted by one or more F); R1 = SR21, SSR21, SOR22, SO2R22, S-OR21, SO-OR21, SO2-OR21, SCOR21, SCOOR22, SCSSR22, OCOR21, OCSR21, OCOOR22, OSO2R22, OSO-R22, OP(O)(OR21)2, P(O)(OR21)2, P(O)(R22)OR21, CN, halo etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl, alkenyl, alkynyl, alkenylcarbonyl, alkynylcarbonyl, pyridyl etc.; R13 = H, 1-6C alkyl, Ar, Ar-alkyl, 3-8C cycloalkyl or (3-8C) cycloalkylalkyl; R21 = H, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, Ar, Ar-alkyl, Het' or Het'-alkyl (where alkyl residues are optionally substituted by one or more F); b, c, d, f = 0 or 1 provided not all are 0; e, g,h = 0-6; Ar = optionally substituted 6-14C aryl; Het' = optionally substituted heteroaryl; unless specified otherwise alkyl moieties have 1-8C, alkenyl or alkynyl moieties 2-8C, cycloalkyl moieties 3-12C and bi- or tri-cycloalkyl moieties 6-12C.

    48.
    发明专利
    未知

    公开(公告)号：DE19629817A1

    公开(公告)日：1998-01-29

    申请号：DE19629817

    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 ,  A61K31/19 ,  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 ,  C07D471/04 ,  C07D401/14 ,  C07D247/02 ,  C07D227/00 ,  A61K31/33

    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.

Patent Agency Ranking