公开(公告)号：US06362190B1

公开(公告)日：2002-03-26

申请号：US09853057

申请日：2001-05-10

申请人： Jules Shafer ,  Denise M. Visco

发明人： Jules Shafer ,  Denise M. Visco

IPC分类号： A61K31341

摘要： The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with an oral composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis and sarcoidosis.

公开(公告)号：US06232315B1

公开(公告)日：2001-05-15

申请号：US09407821

申请日：1999-09-28

申请人： Jules Shafer ,  Denise M. Visco

发明人： Jules Shafer ,  Denise M. Visco

IPC分类号： A61K31341

CPC分类号： A61K31/497 ,  A61K31/00 ,  A61K31/341 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K2300/00

摘要： The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof. The invention is also a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor and an NSAID, e.g., a COX-2 inhibitor. Such diseases include but are not limited to nephritis, systemic lupus, erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylene-carboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof and the COX-2 inhibitor is 3-phenyl-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明是治疗患者炎性疾病的方法，其包括用包含凝血酶抑制剂的组合物治疗患者。 这些疾病包括但不限于肾炎，系统性红斑狼疮，类风湿性关节炎，肾小球性肾炎和囊状病。 在一类方法中，凝血酶抑制剂选自3-（2-苯乙基氨基）-6-甲基-1-（2-氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基）-2-吡嗪酮，N ' - [[1-（氨基亚氨基甲基）-4-哌啶基]甲基] -N-（3,3-二苯基丙酰基）-L-脯氨酸酰胺和3-（2-苯乙基氨基）-6-甲基-1-（2- 氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基）-2-吡啶酮或其药学上可接受的盐。本发明还是一种治疗患者炎症性疾病的方法，其包括用包含凝血酶抑制剂和NSAID的组合物治疗患者 ，例如COX-2抑制剂。 这些疾病包括但不限于肾炎，系统性红斑狼疮，红斑狼疮，类风湿性关节炎，肾小球性肾炎和囊性疾病。 在一类方法中，凝血酶抑制剂选自3-（2-苯乙基氨基）-6-甲基-1-（2-氨基-6-甲基-5-亚甲基 - 甲酰胺基甲基吡啶基）-2-吡嗪酮 ，N' - [[1-（氨基亚氨基甲基）-4-哌啶基]甲基] -N-（3,3-二苯基丙酰基）-L-脯氨酰胺和3-（2-苯乙基氨基）-6-甲基-1-（ 2-氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基）-2-吡啶酮或其药学上可接受的盐，COX-2抑制剂是3-苯基-4-（4-（甲基磺酰基）苯基）-2-（5H） - 呋喃酮或其药学上可接受的盐。