Aventis Pharma Deutschland, Gmbh

Sanofi-A Ventis Deutschland Gmbh

Hoechst Marion Roussel Deutschland Gmbh

Holger Faasch

Udo Hedtmann

Erich F Paulus

Uwe Westenfelder

Andreas Gappisch

Hans-Hermann Lau

The invention relates to a crystal modification of the compound of the formula Iand 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.

Crystal form of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide

The invention relates to a crystal modification of the compound of the formula Iand the processes for the preparation of and use that crystal modifications. 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.

Crystal form on N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide

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.

Process for crystallizing N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide

The invention relates to a crystal modification of the compound of the formula I

Crystal form of N-(4-triflouromethylphenyl)-5-methylisoxazole-4-carboxamide

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.

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Hochheim, Germany

Holger Faasch