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公开(公告)号：JPH1053531A
公开(公告)日：1998-02-24
申请号：JP12050297
申请日：1997-05-12
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , SCHMIDT WOLFGANG DR , BARTNIK ECKART DR , HUELS CHRISTOPH DR , SEIFFGE DIRK DR
Abstract: PROBLEM TO BE SOLVED: To provide a method useful for treatment and prevention of diseases accompanying excess cell adhesion derived by selectin receptor by using a polymer of acryclic acid or methacrylic acid. SOLUTION: Polyacrylic acids and polymers of methacrylic acid or their salts, preferably polyacrylic acids having molecular weight of 900-63,000g/mol, are effective for treatment and prevention of diseases relating to selectin receptor-induced excess cell adhesion at tissues affected with a disease, particularly diseases of cardiac and vascular system or rheumatic diseases. This medicine is possible to administrate intravenously, orally or nonorally, or as pieces of transplantation and through rectum. The polyacrylic acids and polymethacrylic acids with high molecular weights are extremely strong and specific p-selectin antagonists.
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公开(公告)号：DE19700774A1
公开(公告)日：1998-07-16
申请号：DE19700774
申请日：1997-01-13
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR
Abstract: Analogues of formula (I) of the so-called sulfatides (3-O-sulphated galactosyl ceramides) are disclosed in which the natural ceramide is substituted by a simple dialkylated unit. This aglycone may be O-, S- or C-glycosidically linked. These analogues may also contain several sulphate or other acid groups instead of just one such group. Also disclosed is the preparation of these compounds and their use for producing medicaments and diagnostic agents. In the formula (I), R , R independently represent -(CH2)n-CH3; n is an integer from 10 to 30; R -R independently represent OH, OSO3H, OCH2COOH, CH(COOH)2, O(CH2)2CH(COOH)2 or non-toxic salts of the corresponding acids, provided that at least one radical R -R be other than OH, and the hydroxy groups can be provided with protective groups such as benzyl, benzylidene or isopropylidene; and S stands for O, S, (CH2)2O or CH2O.
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公开(公告)号：CZ294096A3
公开(公告)日：1997-04-16
申请号：CZ294096
申请日：1996-10-07
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , SCHOLKENS BERNWARD PROF DR , KLEMM PETER DR , HULS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07D295/20 , A61K31/215 , A61K31/33 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/08 , C07D207/16 , C07D211/34 , C07D211/62 , C07D405/00 , C07H15/203 , C07H15/207 , C07H17/00 , C07H19/04
Abstract: The invention relates to conjugates which consist of mono- or polycarboxylated piperidine or pyrrolidine derivatives and pyranoses, furanoses or polyalcohols linked via a chain or a cyclic system. The carboxyl groups of the piperidine derivatives can either be located directly on the ring or linked to the ring via a short chain. The invention additionally relates to the preparation of these compounds and to their use for the production of pharmaceuticals and diagnostics.
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公开(公告)号：DE19537334A1
公开(公告)日：1997-04-10
申请号：DE19537334
申请日：1995-10-09
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , SCHOELKENS BERNWARD PROF DR , KLEMM PETER DR , HUELS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07D295/20 , A61K31/215 , A61K31/33 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/08 , C07D207/16 , C07D211/34 , C07D211/62 , C07D405/00 , C07H15/203 , C07H15/207 , C07H17/00 , C07H19/04 , C07H15/26 , C07H1/00
Abstract: Piperidine and pyrrolidine derivs. of formula (I) are new. Z = pyranoside, pyranosyl residue bound via. the 6-position, alkyl pyranoside bound via the 6-position, furanoside, furanosyl residue bound via the 5-position, alkyl furanoside bound via the 5-position or a polyalcohol; A = O, CH2 or S; R ,R = H, (CH2)mX or CH2O(CH2)mX ; or R + R = 5- or 6-membered carbocycle or heterocycle with at least one substit. R ,R or R ; E = N, C or CH; R = (CH2)pCOOH, (COOH)2, (CH2)pCH(COOH)2, (CH2)p(COOH)2, (CH2)pC(CH2-C6H5)(COOH)2, CONHC(COOH)2 or a gp. of formula (a)-(d); m = 1-20; p = 0-10; q, r = 0-3;m = 1-3; provided that q + r + n = 4 or 5; R -R = H, OH, O(CH2)wX or CH2O(CH2)wX ; w = 1-19; Y ,Y = O, NH or S; and X -X = H, NH2, COOH, OH, CH2OH, CH2NH2, 1-20C alkyl or 6-10C aryl.
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公开(公告)号：DE4408248A1
公开(公告)日：1995-09-14
申请号：DE4408248
申请日：1994-03-11
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , BARTNIK ECKART DR , SEIFFGE DIRK DR
IPC: A61K31/785 , A61K31/70 , A61K31/7028 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P43/00 , C07H3/04 , C07H3/06 , C07H15/04 , C07H15/207 , C07H17/04 , C08G69/10 , C08G69/48 , C08G73/06 , C08G73/10 , G01N33/545
Abstract: Cpds. of formula (I) are new, with the exception of sialyl Lewis-X and -A, and derivs. of these which contain a N3, NH2 or OH substit. in place of a N-acetyl gp., or contain glycerin in place of fucose: R , R = H, CH2X or CH2O(CH2)mX ; or R +R = a six-membered substd. carbo- or hetero-cycle; R = O, S, H or CH2OX ; R , R = O- alpha -NANA (where NANA is N-acetylneuraminic acid), O- beta -NANA, OSO3H, or another monobasic acid; R = H, OH or 1-25C alkyl; or R +R = a six-membered substd. carbo- or heterocycle; Y = O- alpha -NANA, O- beta -NANA, OSO3H, or another monobasic acid; Z = a pyranose, a furanose or an open-chain polyalcohol; m, n, p, q = 1-20; X, X , X = H, NH2, COOH, OH, CH2OH, CH2NH, aryl, 1-25C alkyl or CH2O(CH2)qX; X = H, 1-25C alkyl or aryl; or X +X = O or S.
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Patent Agency Ranking
公开(公告)号：DE19648681A1
公开(公告)日：1998-05-28
申请号：DE19648681
申请日：1996-11-25
Applicant: HOECHST AG
Inventor： KRETZSCHMAR GERHARD DR , TOEPFER ALEXANDER DR
Abstract: The invention relates to benzoic acid derivatives, in which alpha -C-fucosides or alpha -C-mannosides and alkyl chains or rings, which have at least one acid function, are attached in positions 3 and 5 of the aromatic ring, via ether linkages and short spacer groups. The invention relates furthermore to a procedure for the production of these compounds and their application in the production of medicaments and diagnostic reagents.
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公开(公告)号：DE4430005A1
公开(公告)日：1996-02-29
申请号：DE4430005
申请日：1994-08-25
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , BARTNICK ECKART DR , SEIFFGE DIRK DR
Abstract: Malonic acid derivs. of formula (I) are new. R1-R3 = H, (CH2)mX or CH2O(CH2)mX1, or R1+R2 = 6-membered carbocycle or heterocycle substd. by at least one of R4, R5 and R6; A, B = O, S, NH, NHCO, OCNH, OCO, COO, NHCOO, OCONH, SCO, OCS, OCS2, S.CSO, NHCS2, SCS.NH or CH2; Z = pyranose, furanose, open-chained polyol, or -YX6; Y = O(CX2X3)n, (CX2X3)n, (CX2R7)n, (CR7R8)n, CH2(CX2X3)n, or a satd. or unsatd. 6-membered carbocycle or heterocycle with at least one substit. R9, or a combination of a ring and O(CX2X3)n, (CX2X3)n, (CX2R7)n or (CR7R8)n; R4-R6 = H, OH, (CH2)qX4, CH2O(CH2)qX5 or NH.COMe; R7-R9 = H, OH, (CH2)qX4 or CH2O(CH2)qX5; X, X1-X5 = H, NH2, COOH, OH, CH2OH, CH2NH2, 1-20C alkyl or 6-10C aryl; X6 = OH or -CR3(COOH)2; m, n, q = 1-20.
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公开(公告)号：DE19619238A1
公开(公告)日：1997-11-20
申请号：DE19619238
申请日：1996-05-13
Applicant: HOECHST AG
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公开(公告)号：DE19602355A1
公开(公告)日：1997-07-31
申请号：DE19602355
申请日：1996-01-24
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , BARTNIK ECKART DR , HUELS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07H15/04 , A61K31/70 , A61K31/7028 , A61K31/715 , A61K49/00 , A61P9/00 , A61P9/08 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/06 , A61P43/00 , C07C55/02 , C07C55/22 , C07C55/24 , C07C55/26 , C07C59/235 , C07C217/08 , C07C219/06 , C07C229/24 , C07H3/04 , C07H3/06 , C08B37/00 , C07H1/00
Abstract: Multiple fucosylated carboxylic acid derivatives of formula (I) and their salts are new. R , R = H, OH, COOH, NH2, NHAc, O(CH2)cX , (CH2)cX , CH2O(CH2)cX or Z; A, B, D, E, G = O, S, NH, NHC(O), C(O)NH, OC(O), NHC(O)O, OC(O)NH, NHC(O)NH, SC(O), C(S)O, OC(S)S, SC(S)O, NHC(S)S, SC(S)NH, CH2, OCH2, CH2O, CH2NH, or NHCH2; V , V = C or N, provided that R or R is absent if V or V = N; Q, Y = (CX , X )b, (CX , R )b, CR , R )b or CH2(CX , X )b; an optionally saturated 5 or 7 membered carbo- or hetero-cycle or a combination of these and (CX , X )b, (CX , R )b, (CR , R )b; R , R = H, OH, COOH, NH2, NHC(O)CH3, O(CH2)dX or CH2O(CH2)dX ; X -X = H, NH2, COOH, OH, CH2OH, CH2NH2, 1-20C alkyl or 6-10C aryl; K, L = HCGZ or CH2; R -R = H, OH or GZ; Z = pyranoside, C6 bonded pyranoside residue, C6 bonded alkylpyranoside, furanoside, C5 bonded alkylfuranoside, or a polyalcohol having one or more hydroxyl groups substituted by R or R bonded via G; a-d, l-n, p, q, t, v-y, = 0-20; and r, z = 0 or 1, provided that when r = 0, then q and t = 0 and R and R are absent.
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公开(公告)号：CZ9602940A3
公开(公告)日：1997-04-16
申请号：CZ294096
申请日：1996-10-07
Applicant: HOECHST AG
Inventor： TOEPFER ALEXANDER DR , KRETZSCHMAR GERHARD DR , SCHOLKENS BERNWARD PROF DR , KLEMM PETER DR , HULS CHRISTOPH DR , SEIFFGE DIRK DR
IPC: C07D295/20 , A61K31/215 , A61K31/33 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/08 , C07D207/16 , C07D211/34 , C07D211/62 , C07D405/00 , C07H15/203 , C07H15/207 , C07H17/00 , C07H19/04
CPC classification number: C07H15/207
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