-
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
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 , 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.
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32.
公开(公告)号:CZ9702344A3
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
CPC classification number: C07D233/52
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33.
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.
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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
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公开(公告)号:DE59713013D1
公开(公告)日:2009-08-13
申请号:DE59713013
申请日:1997-07-17
Applicant: GENENTECH INC , HOECHST AG
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 , C07D233/52 , 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 , C07D233/54 , 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.
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36.
公开(公告)号:MY132635A
公开(公告)日:2007-10-31
申请号:MYPI9703358
申请日:1997-07-23
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: C07D239/02 , A61K31/305 , A61K31/53 , A61P35/00
Abstract: THERE ARE DESCRIBED CYCLOALKYL DERIVATIVES OF THE FORMULA (I) IN WHICH R1, Y, A, B, D, E, F AND G HAVE THE MEANING INDICATED HEREIN, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS. THE COMPOUNDS ACCORDING TO THE INVENTION CAN BE USED AS VITRONECTIN RECEPTOR ANTAGONISTS AND AS INHIBITORS OF BONE RESORPTION.
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公开(公告)号:CZ292672B6
公开(公告)日:2003-11-12
申请号:CZ172997
申请日:1997-06-04
Applicant: HOECHST AG
Inventor: STILZ HANS ULRICH DR , BECK GERHARD DR , RADAU MANFRED DR
IPC: C07D233/78 , A61K31/415 , A61K31/416 , A61K31/4164 , A61K31/4166 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/14 , A61P35/00 , A61P35/04 , C07D233/72 , C07D233/74 , C07D233/76
Abstract: The present invention relates to a hydrogen maleate of 3-(2-(4-(4-(aminoiminomethyl)phenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl)acetylamino)-3-phenylpropionic acid ethyl ester of the general formula I, in which HB represents maleic acid, as well as physiologically acceptable salts thereof, processes of their preparation, their use in medicaments and pharmaceutical preparations in which these compounds are comprised.
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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
Inventor: STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , HULS 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
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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公开(公告)号:ES2190503T3
公开(公告)日:2003-08-01
申请号:ES97119638
申请日:1997-11-10
Applicant: HOECHST AG
Inventor: STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , KNOLLE JOCHEN DR , BARTNIK ECKART DR , HULS CHRISTOPH DR
IPC: C07D233/00 , A61K31/415 , A61K31/4166 , A61K31/4178 , A61K31/421 , A61K31/426 , A61K38/00 , A61K38/06 , A61K38/07 , A61K38/39 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P33/02 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D233/32 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/86 , C07D257/00 , C07D403/12 , C07D405/12 , C07K5/02 , C07K5/023 , C07K5/078 , C07K5/08 , C07K5/097 , C07K5/10 , C07K5/117 , C07K7/06 , C07K14/78
Abstract: Use of N-substituted pyrrolidone, imidazolidinone, oxazolidinone or thiazolidinone derivatives of formula (I), in all stereoisomer (or mixture) forms, or their salts 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, 3-7C cycloalkylene, (1-6C) alkylene-phenylene, or the divalent residue of a 5- or 6-membered ring containing 1 or 2 N (optionally substituted); 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, 3-8C cycloalkyl, Ar or Ar-alkyl ; R1 = X-NH-C(=NH)-(CH2)p or X1-NH-(CH2)p; p = 0-3; X = H, 1-6C alkyl, (1-6C) alkylcarbonyl, Ar-(1-6C) alkoxycarbonyl, CN, OH, etc.; X1 = X etc.; R2 = H, alkyl, Ar, Ar-alkyl or 3-8C cycloalkyl; R3 = H, alkyl, Ar, alkenyl, alkynyl, 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; 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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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
Inventor: STILZ HANS ULRICH DR , WEHNER VOLKMAR DR , HUELS 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
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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