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1. 发明授权

US06303792B1 Process for crystallizing N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide 有权
标题翻译：结晶N-（4-三氟甲基苯基）-5-甲基异恶唑-4-甲酰胺的方法
公开(公告)号：US06303792B1
公开(公告)日：2001-10-16
申请号：US09510157
申请日：2000-02-22
申请人： Hans-Hermann Lau , Udo Hedtmann , Holger Faasch , Andreas Gappisch
发明人： Hans-Hermann Lau , Udo Hedtmann , Holger Faasch , Andreas Gappisch
IPC分类号： C07D26114
CPC分类号： C07D261/18
摘要： The invention relates to a process for obtaining N-(4-trifluoromethylphenyl)-5-methyl-isoxazole-4-carboxamide in crystalline form, which is essentially free of byproducts. For this purpose, N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide is transferred into an organic solvent or into mixtures of organic solvents and water, the amount of byproduct in the solution is determined by quantitative analysis and an equimolar amount of a base is added. N-(4-Trifluoromethylphenyl)-5-methyl-isoxazole-4-carboxamide is isolated from the resulting solution by crystallization.
摘要翻译：本发明涉及一种获得结晶形式的N-（4-三氟甲基苯基）-5-甲基 - 异恶唑-4-甲酰胺的方法，其基本上不含副产物。为此，将N-（4-三氟甲基苯基）-5-甲基异恶唑-4-甲酰胺转移到有机溶剂或有机溶剂和水的混合物中，通过定量分析和等摩尔量确定溶液中副产物的量的基地被添加。通过结晶从所得溶液中分离出N-（4-三氟甲基苯基）-5-甲基 - 异恶唑-4-甲酰胺。

2. 发明授权

US06900334B2 Crystal form on N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide 有权
标题翻译： N-（4-三氟甲基苯基）-5-甲基异恶唑-4-甲酰胺的晶体形式
公开(公告)号：US06900334B2
公开(公告)日：2005-05-31
申请号：US10302872
申请日：2002-11-25
申请人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
发明人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
IPC分类号： A61K31/42 , A61P1/00 , A61P3/08 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P25/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/08 , B01D9/02 , C07D261/18
CPC分类号： C07D261/18
摘要： The invention relates to a crystal modification of the compound of the formula I and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.
摘要翻译：本发明涉及式I化合物的晶体改性及其制备和使用方法1。本发明用于治疗急性免疫性发作，例如败血症，过敏，移植物抗宿主和宿主对移植物反应，自身免疫性疾病，特别是类风湿性关节炎，系统性红斑狼疮，多发性硬化，牛皮癣，特应性皮炎，哮喘，荨麻疹，鼻炎，葡萄膜炎，II型糖尿病，肝纤维化，囊性纤维化，结肠炎，癌症，如肺癌，白血病，卵巢癌，肉瘤，卡波西肉瘤，脑膜瘤，肠癌，淋巴癌，脑肿瘤，乳腺癌，胰腺癌，前列腺癌或皮肤癌。

3. 发明授权

US06221891B1 Crystal form of N-(4-triflouromethylphenyl)-5-methylisoxazole-4-carboxamide 有权
标题翻译：晶型N-（4-三氟甲基苯基）-5-甲基异恶唑-4-甲酰胺
公开(公告)号：US06221891B1
公开(公告)日：2001-04-24
申请号：US09428499
申请日：1999-10-28
申请人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
发明人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
IPC分类号： A61K3142
CPC分类号： C07D261/18
摘要： The invention relates to a crystal modification of the compound of the formula I and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.
摘要翻译：本发明涉及式I化合物的晶体改性以及制备和使用晶体修饰的方法1.本发明用于治疗急性免疫性发作，例如败血症，过敏反应，移植物抗宿主和宿主自身免疫性疾病，特别是类风湿性关节炎，系统性红斑狼疮，多发性硬化，牛皮癣，特应性皮炎，哮喘，荨麻疹，鼻炎，葡萄膜炎，II型糖尿病，肝纤维化，囊性纤维化，结肠炎，癌症等作为肺癌，白血病，卵巢癌，肉瘤，卡波西氏肉瘤，脑膜瘤，肠癌，淋巴癌，脑肿瘤，乳腺癌，胰腺癌，前列腺癌或皮肤癌。

4. 发明授权

US6060494A Crystal form of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide 有权
公开(公告)号：US6060494A
公开(公告)日：2000-05-09
申请号：US129783
申请日：1998-08-06
申请人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
发明人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
IPC分类号： A61K31/42 , A61P1/00 , A61P3/08 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P25/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/08 , B01D9/02 , C07D261/18 , C07D261/08
CPC分类号： C07D261/18
摘要： The invention relates to a crystal modification of the compound of the formula I ##STR1## and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.

5. 发明授权

US06995272B2 Crystal form of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide 有权
标题翻译：晶型N-（4-三氟甲基苯基）-5-甲基异恶唑-4-甲酰胺
公开(公告)号：US06995272B2
公开(公告)日：2006-02-07
申请号：US10830307
申请日：2004-04-23
申请人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
发明人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
IPC分类号： C07D261/18
CPC分类号： C07D261/18
摘要： The invention relates to a crystal modification of the compound of the formula I and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.
摘要翻译：本发明涉及式I化合物的晶体改性：化学式id =“CHEM-US-00001”num =“000

6. 发明授权

US06552202B2 Crystal form of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide 有权
标题翻译：晶型N-（4-三氟甲基苯基）-5-甲基异恶唑-4-甲酰胺
公开(公告)号：US06552202B2
公开(公告)日：2003-04-22
申请号：US09764258
申请日：2001-01-19
申请人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
发明人： Holger Faasch , Udo Hedtmann , Uwe Westenfelder , Erich Paulus
IPC分类号： C07D26118
CPC分类号： C07D261/18
摘要： The invention relates to a crystal modification of the compound of the formula I and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type 11 diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.
摘要翻译：本发明涉及式I化合物的晶体改性以及制备和使用晶体修饰的方法1.本发明用于治疗急性免疫性发作，例如败血症，过敏反应，移植物抗宿主和宿主 - 反接种反应，自身免疫性疾病，特别是类风湿性关节炎，系统性红斑狼疮，多发性硬化，牛皮癣，特应性皮炎，哮喘，荨麻疹，鼻炎，葡萄膜炎，11型糖尿病，肝纤维化，囊性纤维化，结肠炎，癌症等作为肺癌，白血病，卵巢癌，肉瘤，卡波西氏肉瘤，脑膜瘤，肠癌，淋巴癌，脑肿瘤，乳腺癌，胰腺癌，前列腺癌或皮肤癌。

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