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1. 发明授权

US5763436A Guanidine derivatives 失效
公开(公告)号：US5763436A
公开(公告)日：1998-06-09
申请号：US715038
申请日：1996-09-17
申请人： Jean Ackermann , David Banner , Klaus Gubernator , Paul Hadvary , Kurt Hilpert , Klaus Muller , Ludvik Labler , Gerard Schmid , Thomas B. Tschopp , Hans Peter Wessel , Beat Wirz
发明人： Jean Ackermann , David Banner , Klaus Gubernator , Paul Hadvary , Kurt Hilpert , Klaus Muller , Ludvik Labler , Gerard Schmid , Thomas B. Tschopp , Hans Peter Wessel , Beat Wirz
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P7/02 , A61P35/00 , C07D20060101 , C07D211/20 , C07D211/22 , C07D211/26 , C07D211/60 , C07D265/30 , C07D265/32 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D267/10
CPC分类号： C07D265/30 , C07D211/22 , C07D211/26 , C07D211/60 , C07D265/32 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.

2. 发明授权

US07071212B2 N-(4-carbamimidoyl-phenyl)-glycine derivatives 失效
标题翻译： N-（4-甲脒基 - 苯基） - 甘氨酸衍生物
公开(公告)号：US07071212B2
公开(公告)日：2006-07-04
申请号：US10639030
申请日：2003-08-12
申请人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
发明人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
IPC分类号： A61K31/445 , C07D265/30
CPC分类号： C07D207/27 , C07C257/18 , C07C259/18 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/96 , C07D213/30 , C07D213/55 , C07D213/65 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D235/18 , C07D249/08 , C07D261/04 , C07D271/06 , C07D277/24 , C07D295/155 , C07D307/12 , C07D307/20 , C07D307/54 , C07D309/12 , C07D309/14 , C07D317/64 , C07D319/18 , C07D321/10 , C07D333/24 , C07D335/04 , C07D403/12
摘要： The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
摘要翻译：本发明涉及下式的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物：其中R 1，E，X 1至X 4 本说明书和权利要求书中所定义的，以及其水合物或溶剂合物及其生理上可用的盐。

3. 发明授权

US06683215B2 N-(4-carbamimidoyl-phenyl)-glycine derivatives 失效
标题翻译： N-（4-甲脒基 - 苯基） - 甘氨酸衍生物
公开(公告)号：US06683215B2
公开(公告)日：2004-01-27
申请号：US10264943
申请日：2002-10-04
申请人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
发明人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
IPC分类号： C07C25116
CPC分类号： C07D207/27 , C07C257/18 , C07C259/18 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/96 , C07D213/30 , C07D213/55 , C07D213/65 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D235/18 , C07D249/08 , C07D261/04 , C07D271/06 , C07D277/24 , C07D295/155 , C07D307/12 , C07D307/20 , C07D307/54 , C07D309/12 , C07D309/14 , C07D317/64 , C07D319/18 , C07D321/10 , C07D333/24 , C07D335/04 , C07D403/12
摘要： The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
摘要翻译：本发明涉及下式的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物：其中R 1，E，X 1至X 4和G 1和G 2是如在说明书和权利要求书中所定义的，以及其水合物或溶剂合物及其生理上可用的盐。

4. 发明授权

US06476264B2 N-(4-carbamimidoyl-phenyl)-glycine derivatives 失效
标题翻译： N-（4-甲脒基 - 苯基） - 甘氨酸衍生物
公开(公告)号：US06476264B2
公开(公告)日：2002-11-05
申请号：US09758977
申请日：2001-01-12
申请人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
发明人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
IPC分类号： C07C22934
CPC分类号： C07D207/27 , C07C257/18 , C07C259/18 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/96 , C07D213/30 , C07D213/55 , C07D213/65 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D235/18 , C07D249/08 , C07D261/04 , C07D271/06 , C07D277/24 , C07D295/155 , C07D307/12 , C07D307/20 , C07D307/54 , C07D309/12 , C07D309/14 , C07D317/64 , C07D319/18 , C07D321/10 , C07D333/24 , C07D335/04 , C07D403/12
摘要： The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
摘要翻译：本发明涉及下式的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物：其中R1，E，X1至X4和G1和G2如说明书和权利要求书中所定义，以及水合物或溶剂合物和其生理上可用的盐。

5. 发明授权

US06242644B1 N-(4-carbamimidoyl-phenyl)-glycine derivatives 失效
标题翻译： N-（4-甲脒基 - 苯基） - 甘氨酸衍生物
公开(公告)号：US06242644B1
公开(公告)日：2001-06-05
申请号：US09460901
申请日：1999-12-14
申请人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
发明人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
IPC分类号： C07C24318
CPC分类号： C07D207/27 , C07C257/18 , C07C259/18 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/96 , C07D213/30 , C07D213/55 , C07D213/65 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D235/18 , C07D249/08 , C07D261/04 , C07D271/06 , C07D277/24 , C07D295/155 , C07D307/12 , C07D307/20 , C07D307/54 , C07D309/12 , C07D309/14 , C07D317/64 , C07D319/18 , C07D321/10 , C07D333/24 , C07D335/04 , C07D403/12
摘要： The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
摘要翻译：本发明涉及下式的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物：其中R1，E，X1至X4和G1和G2如说明书和权利要求书中所定义，以及水合物或溶剂合物和其生理上可用的盐。

6. 发明授权

US06548694B2 N-(4-carbamimidoyl-phenyl)-glycine derivatives 失效
标题翻译： N-（4-甲脒基 - 苯基） - 甘氨酸衍生物
公开(公告)号：US06548694B2
公开(公告)日：2003-04-15
申请号：US09858535
申请日：2001-05-16
申请人： Leo Alig , Katrin Groebke Zbinden , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Hans Peter Wessel
发明人： Leo Alig , Katrin Groebke Zbinden , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Hans Peter Wessel
IPC分类号： C07C22900
CPC分类号： C07D317/36 , C07C257/18 , C07C259/18 , C07D307/20
摘要： N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: wherein X and R1 to R5 are as defined herein, and includes hydrates or solvates and/or physiologically acceptable salts thereof and/or physiologically acceptable esters thereof.
摘要翻译： N-（4-脒甲酰基 - 苯基） - 甘氨酸衍生物具有下式：其中X和R 1至R 5如本文所定义，并且包括水合物或溶剂化物和/或其生理学上可接受的盐和/或其生理上可接受的酯。

7. 发明授权

US5767268A Sulfuric acid esters of amino sugars 失效
标题翻译：氨基糖的硫酸酯
公开(公告)号：US5767268A
公开(公告)日：1998-06-16
申请号：US639985
申请日：1996-04-26
申请人： Alexander Chucholowski , Jurgen Fingerle , Niggi Iberg , Hans Peter Marki , Rita Muller , Michael Pech , Marianne Rouge , Gerard Schmid , Thomas Tschopp , Hans Peter Wessel
发明人： Alexander Chucholowski , Jurgen Fingerle , Niggi Iberg , Hans Peter Marki , Rita Muller , Michael Pech , Marianne Rouge , Gerard Schmid , Thomas Tschopp , Hans Peter Wessel
IPC分类号： C07H5/04 , A61K31/70 , A61K31/7008 , A61P9/10 , A61P43/00 , C07H5/06 , C07H11/00 , C07H13/08 , C07H13/10 , C07H15/18 , C07H15/00
CPC分类号： C07H13/08 , C07H13/10 , C07H15/18
摘要： Compounds of formulas ##STR1## wherein, B is lower alkylene or an optionally substituted aromatic ring system; G.sup.1, G.sup.2 and G.sup.3 each independently signify a residue of a glycopyranoside, a glycopyranose or a derivative thereof, with at least one hydroxy group of residue G.sup.1, G.sup.2 or G.sup.3 being esterified with sulfuric acid, and pharmaceutically usable salts thereof, are useful for the treatment of disorders which are characterized by excessive or destructive proliferation of smooth muscle cells.
摘要翻译：其中B为低级亚烷基或任选取代的芳族环系;其中B为低级亚烷基或任选取代的芳族环系; G1，G2和G3各自独立地表示具有至少一个残基G1，G2或G3的羟基被硫酸酯化的糖吡喃糖苷，糖吡喃糖或其衍生物的残基，及其药学上可用的盐可用于治疗以平滑肌细胞过度或破坏性增殖为特征的疾病。

8. 发明授权

US5830920A Sulfuric acid esters of sugar alcohols 失效
标题翻译：糖醇的硫酸酯
公开(公告)号：US5830920A
公开(公告)日：1998-11-03
申请号：US639986
申请日：1996-04-26
申请人： Alexander Chucholowski , Jurgen Fingerle , Niggi Iberg , Hans Peter Marki , Rita Muller , Michael Pech , Marianne Rouge , Gerard Schmid , Thomas Tschopp , Hans Peter Wessel
发明人： Alexander Chucholowski , Jurgen Fingerle , Niggi Iberg , Hans Peter Marki , Rita Muller , Michael Pech , Marianne Rouge , Gerard Schmid , Thomas Tschopp , Hans Peter Wessel
IPC分类号： C07D251/70 , A61K31/165 , A61K31/27 , A61K31/35 , A61K31/352 , A61K31/53 , A61K31/70 , A61K31/7028 , A61P7/02 , A61P9/10 , A61P31/12 , A61P43/00 , C07C305/06 , C07C305/10 , C07D311/22 , C07H15/18 , A61K31/045 , C07C205/00
CPC分类号： C07H15/18 , C07C305/06 , C07C305/10
摘要： Compounds of the formula ##STR1## wherein n.sup.1 -n.sup.9 are each independently 0 or 1; m.sup.1 -m.sup.9 are each independently 0 or 1, but with the proviso that at least one of m.sup.1, m.sup.2 and m.sup.3, at least one of m.sup.4, m.sup.5 and m.sup.6 and, when present, at least one of m.sup.7, m.sup.8 and m.sup.9 is 1; and wherein X.sup.1 -X.sup.18 each independently is --O--, --CONR.sup.1,--NR.sup.1 CO-- or --NR.sup.1 --; R.sup.1 is hydrogen or lower alkyl; W is a benzene or s-triazine; Y.sup.1 -Y.sup.9 each independently is an aromatic ring systems; A.sup.1 -A.sup.3 each independently is a residue of a sugar alcohol devoid of the 1-hydroxy group or a derivative thereof, a residue of a sugar acid devoid of the 1-carboxy group or a derivative thereof or tris-(hydroxymethyl)-methyl; D is the di-residue of a sugar alcohol devoid of 2 hydroxy groups or a derivative thereof or the di-residue of a sugar dicarboxylic acid devoid of 2 carboxy group or a derivative thereof; Q.sup.1 -Q.sup.3 and Z.sup.1 -Z3 each independently are the di-residue of a sugar alcohol devoid of 2 hydroxy groups or a derivative thereof or the di-residue of a sugar dicarboxylic acid devoid of 2 carboxy groups or a derivative thereof or didesoxyglycopyranoside or a derivative thereof, wherein at least one hydroxy group of residues A.sup.1 -A.sup.3, D, Q.sup.1 -Q.sup.3 and Z.sup.1 -Z.sup.3 is esterified with sulfuric acid, and pharmaceutically usable salts thereof are useful for the treatment of disorders which are characterized by excessive or destructive proliferation of smooth muscle cells.
摘要翻译：式Ia的化合物或其中n1-n9各自独立地为0或1; m1-m9各自独立地为0或1，但条件是m1，m2和m3中的至少一个，m4，m5和m6中的至少一个，并且当存在时，m7，m8和m9中的至少一个为1 ; 并且其中X1-X18各自独立地为-O - ， - CONR1，-NR1CO-或-NR1-; R1是氢或低级烷基; W是苯或s-三嗪; Y1-Y9各自独立为芳环体系; A1-A3各自独立地为不含1-羟基或其衍生物的糖醇的残基，不含1-羧基的糖酸或其衍生物的残基或三 - （羟甲基） - 甲基; D是不含2个羟基的糖醇或其衍生物或不含2个羧基的糖二羧酸的二残基或其衍生物的二残基; Q1-Q3和Z1-Z3各自独立地为不含2个羟基的糖醇或其衍生物或不含2个羧基的糖二羧酸的二残基或其衍生物或二脱氧吡喃葡萄糖苷或二其衍生物，其中残基A1-A3，D，Q1-Q3和Z1-Z3中的至少一个羟基用硫酸酯化，其药学上可用的盐可用于治疗以过度或破坏性增殖为特征的病症的平滑肌细胞。

9. 发明授权

US07189756B2 Pyrrolidine derivatives 失效
标题翻译：吡咯烷衍生物
公开(公告)号：US07189756B2
公开(公告)日：2007-03-13
申请号：US10881427
申请日：2004-06-30
申请人： Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
发明人： Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
IPC分类号： A61K31/40 , C07D207/04
CPC分类号： C07D401/12 , C07D207/36 , C07D207/48 , C07D403/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/582
摘要： The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
摘要翻译：本发明涉及可用作金属蛋白酶抑制剂的吡咯烷衍生物。锌蛋白酶，并且其有效治疗与血管收缩相关的疾病状态。

10. 发明授权

US06790860B2 Pyrrolidine derivatives 失效
标题翻译：吡咯烷衍生物
公开(公告)号：US06790860B2
公开(公告)日：2004-09-14
申请号：US10373622
申请日：2003-02-25
申请人： Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
发明人： Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
IPC分类号： C07D20704
CPC分类号： C07D401/12 , C07D207/36 , C07D207/48 , C07D403/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/582
摘要： The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
摘要翻译：本发明涉及可用作金属蛋白酶抑制剂的吡咯烷衍生物。锌蛋白酶，并且其有效治疗与血管收缩相关的疾病状态。

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