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1. 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。

2. 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。

3. 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。

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

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.

7. 发明授权

US06320054B1 Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US06320054B1
公开(公告)日：2001-11-20
申请号：US09526033
申请日：2000-03-15
申请人： Leo Alig , Albrecht Edenhofer , Kurt Hilpert , Thomas Weller
发明人： Leo Alig , Albrecht Edenhofer , Kurt Hilpert , Thomas Weller
IPC分类号： C07D27720
CPC分类号： C07D417/12 , A61K38/00 , C07D277/48 , C07D277/56 , C07K5/1024
摘要： Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.
摘要翻译：下式的化合物及其可药用的盐和酯，其中R1，R2和R3具有本文所述的含义，抑制粘合蛋白与不同类型细胞表面的结合，从而影响细胞和细胞基质互动这些化合物可以以药物制剂的形式用于控制或预防肿瘤，肿瘤转移，肿瘤生长，骨质疏松症，佩吉特氏病，糖尿病性视网膜病变，黄斑变性，血管干预后的再狭窄，牛皮癣，关节炎，纤维化，肾衰竭，以及由病毒，细菌或真菌引起的感染。

8. 发明授权

US06297266B1 Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US06297266B1
公开(公告)日：2001-10-02
申请号：US09420387
申请日：1999-10-19
申请人： Leo Alig , Kurt Hilpert , Thomas Weller
发明人： Leo Alig , Kurt Hilpert , Thomas Weller
IPC分类号： C07D27748
CPC分类号： C07D277/48
摘要： Compounds of formula (I) as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance described in the specification, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasizing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infections caused by viruses, bacteria or fungi.
摘要翻译：式（I）化合物及其药学上可接受的盐和酯，其中R1，R2和R3具有说明书中描述的含义，抑制粘附蛋白与不同类型细胞表面的结合，从而影响细胞和细胞 - 基质相互作用。它们可以以药物制剂的形式用于控制或预防肿瘤，肿瘤转移，肿瘤生长，骨质疏松症，佩吉特氏病，糖尿病性视网膜病变，黄斑变性，血管干预后的再狭窄，牛皮癣，关节炎，纤维化，肾衰竭以及作为病毒，细菌或真菌引起的感染。

9. 发明授权

US6001855A Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US6001855A
公开(公告)日：1999-12-14
申请号：US218200
申请日：1998-12-22
申请人： Leo Alig , Albrecht Edenhofer , Kurt Hilpert , Thomas Weller
发明人： Leo Alig , Albrecht Edenhofer , Kurt Hilpert , Thomas Weller
IPC分类号： C07D277/20 , A61K31/00 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P9/00 , A61P13/00 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P27/00 , A61P27/02 , A61P31/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D207/04 , C07D277/24 , C07D277/48 , C07D277/56 , C07D295/04 , C07D417/02 , C07D417/06
CPC分类号： C07D417/06 , C07D277/48 , C07D277/56
摘要： Compounds of formula I ##STR1## as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance given in claim 1, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasing, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, kidney failure as well as infections caused by viruses, bacteria or fungi.
摘要翻译：式I化合物及其药学上可用的盐和酯，其中R1，R2和R3具有权利要求1中给出的含义，抑制粘附蛋白与不同类型细胞表面的结合，从而影响细胞和细胞 - 矩阵相互作用它们可以以药物制剂的形式用于控制或预防肿瘤，肿瘤转移，骨质疏松症，佩吉特氏病，糖尿病性视网膜病变，黄斑变性，血管干预后的再狭窄，牛皮癣，关节炎，肾衰竭以及由病毒引起的感染，细菌或真菌。

10. 发明授权

US06344562B1 Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US06344562B1
公开(公告)日：2002-02-05
申请号：US09878704
申请日：2001-06-11
申请人： Leo Alig , Albrecht Edenhofer , Kurt Hilpert , Thomas Weller
发明人： Leo Alig , Albrecht Edenhofer , Kurt Hilpert , Thomas Weller
IPC分类号： C07D27720
CPC分类号： C07D417/12 , A61K38/00 , C07D277/48 , C07D277/56 , C07K5/1024
摘要： Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.
摘要翻译：下式的化合物及其可药用的盐和酯，其中R1，R2和R3具有本文所述的含义，抑制粘合蛋白与不同类型细胞表面的结合，从而影响细胞和细胞基质互动这些化合物可以以药物制剂的形式用于控制或预防肿瘤，肿瘤转移，肿瘤生长，骨质疏松症，佩吉特氏病，糖尿病性视网膜病变，黄斑变性，血管干预后的再狭窄，牛皮癣，关节炎，纤维化，肾衰竭，以及由病毒，细菌或真菌引起的感染。

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