31.
    发明专利
    未知

    公开(公告)号:ID18903A

    公开(公告)日:1998-05-20

    申请号:ID973672

    申请日:1997-11-13

    Applicant: HOECHST AG

    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.

    IMINO DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF

    公开(公告)号:CZ234497A3

    公开(公告)日:1998-03-18

    申请号:CZ234497

    申请日:1997-07-22

    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

    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

    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

    35.
    发明专利
    未知

    公开(公告)号:DE59713013D1

    公开(公告)日:2009-08-13

    申请号:DE59713013

    申请日:1997-07-17

    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.

    38.
    发明专利
    未知

    公开(公告)号:ES2191803T3

    公开(公告)日:2003-09-16

    申请号:ES97119636

    申请日:1997-11-10

    Applicant: HOECHST AG

    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.

    Heterocycles as inhibitors of leukocyte adhesion and as antagonists of VLA-4

    公开(公告)号:SI0842945T1

    公开(公告)日:2003-06-30

    申请号:SI9730499

    申请日:1997-11-10

    Applicant: HOECHST AG

    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.

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