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    Novel cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists
    4.
    发明专利
    Novel cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists 未知

    公开(公告)号：AU726376B2

    公开(公告)日：2000-11-02

    申请号：AU2941897

    申请日：1997-07-22

    Applicant: HOECHST AG ,  GENENTECH INC

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

    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

    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.

    NOVEL CYCLOALKYL DERIVATIVES AS INHIBITORS OF BONE RESORPTION AND VITRONECTIN RECEPTOR ANTAGONISTS
    5.
    发明专利
    NOVEL CYCLOALKYL DERIVATIVES AS INHIBITORS OF BONE RESORPTION AND VITRONECTIN RECEPTOR ANTAGONISTS 未知

    公开(公告)号：HK1006779A1

    公开(公告)日：1999-03-19

    申请号：HK98105626

    申请日：1998-06-18

    Applicant: HOECHST AG ,  GENENTECH INC

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

    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 ,  A61K ,  C07C ,  C07D

    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.

    2,5-DIOXO-IMIDAZOLIDINES AND MEDICAMENTS
    6.
    发明专利
    2,5-DIOXO-IMIDAZOLIDINES AND MEDICAMENTS 未知

    公开(公告)号：NZ329177A

    公开(公告)日：1998-11-25

    申请号：NZ32917797

    申请日：1997-11-13

    Applicant: HOECHST AG

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

    IPC: A61K31/415 ,  A61K31/4166 ,  A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  C07D233/76 ,  A61P3/08 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P19/02 ,  A61P29/00 ,  A61P33/02 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D233/54 ,  C07D233/72 ,  C07K5/02 ,  C07K5/023 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K5/117

    Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer or mixture forms, or their salts is for inhibiting the adhesion and/or migration of leukocytes or inhibiting VLA-4 receptors is new. W = R1-A-CR13 or R1A-CH=C; Y = CO, CS or CH2; Z = O, S or CH2 etc.; A = 1-6C alkylene, 3-12C cycloalkylene, (1-6C), phenylene-(1-6C)alkyl, 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-phenyl; 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); R1 = H, 1-10C alkyl (optionally fluorinated), cycloalkyl, cycloalkylalkyl, O or S 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-alkyl or 3-8C cycloalkyl; b, c, d, f = 0 or 1, but not all 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.

    INHIBITORS OF LEUCOCITA-ADHESION AND WLA-4-ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    7.
    发明专利
    INHIBITORS OF LEUCOCITA-ADHESION AND WLA-4-ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：HU9702036A2

    公开(公告)日：1998-07-28

    申请号：HU9702036

    申请日：1997-11-14

    Applicant: HOECHST AG

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

    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 ,  C07K5/08

    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.

    8.
    发明专利
    未知

    公开(公告)号：TR199701645A2

    公开(公告)日：1998-07-21

    申请号：TR9701645

    申请日：1997-12-18

    Applicant: HOECHST AG ,  GENENTECH INC

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

    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 ,  C07D ,  A61K

    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.

    NOVEL HETEROCYCLIC COMPOUNDS, METHOD OF OBTAINING THEM, THEIR APPLICATION AS MEDICINES AND PHARMACEUTIC AGENT
    10.
    发明专利
    NOVEL HETEROCYCLIC COMPOUNDS, METHOD OF OBTAINING THEM, THEIR APPLICATION AS MEDICINES AND PHARMACEUTIC AGENT 未知

    公开(公告)号：PL323968A1

    公开(公告)日：1998-06-22

    申请号：PL32396897

    申请日：1997-12-20

    Applicant: HOECHST AG ,  GENENTECH INC

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

    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 ,  C07D ,  A61K

    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.

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