Ab Science

Centre National De La Recherche Scientifique

Institut Curie

Institut National De La Sante Et De La Recherche Medicale

Assistance Publique-hopitaux De Paris

Universite Paris Cité

Imagine Institut Des Maladies Genetiques Necker Enfants Malades

Alain Moussy

Jean-Pierre Kinet

Abdellah Benjahad

Camille Georges Wermuth

Willy Picoul

Didier Pez

Franck Sandrinelli

Jason Martin

Emmanuel Chevenier

Bruno Giethlen

Anne Lermet

Marco Ciufolini

David Grierson

Claire Schalon

Martine Croisy

Philippe Reginault

Marco A Ciufolini

Francois Bellamy

Olivier Hermine

François Bellamy

Jean Pierre Kinet

Patrice Dubreuil

Bruno Gielthen

Thiago Trovati Maciel

Slimane Allali

Colin Mansfield

Caroline Carvalho

David Piquemal

Rachel Rignault-bricard

Camille Wermuth

A 2-aminoarylthiazole derivative or a pharmaceutically acceptable salt or solvate thereof, in particular masitinib or a pharmaceutically acceptable salt or solvate thereof, for use in the treatment of sickle cell disease in a patient in need thereof. Also, a 2-aminoarylthiazole derivative or a pharmaceutically acceptable salt or solvate thereof, in particular masitinib or a pharmaceutically acceptable salt or solvate thereof, for use in the prevention and/or treatment of acute chest syndrome (ACS) in a sickle cell disease patient in need thereof.

Masitinib for the treatment of sickle cell disease

The present invention relates to compounds of general formula (I). wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.

Compounds with anti-tumoral activity

The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, autoimmune, allergic, hematological, inflammatory and degenerative disorders. In particular, the compounds of the invention are Syk inhibitors. The invention also relates to a process for manufacturing the compounds of the invention.

Oxazole derivatives that inhibit Syk

A method for treating patients afflicted with cancer, wherein the patients are treated with a compound including tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, in particular masitinib, optionally in combination with at least one antineoplastic agent. The tyrosine kinase inhibitor, mast cell inhibitor or c-Kit inhibitor, and the optional at least one antineoplastic agent, are administered in a dosage regimen that includes a therapeutically effective amount. Also described are methods for predicting therapeutic response to the treatment in a given patient and therefore identification of applicable patient subpopulations based upon these predictor factors; sometimes referred to as biomarkers. One method is based upon the clinical marker of pain intensity. Another method is based upon gene expression predictive biomarkers assessed via RNA expression in peripheral blood cell samples collected prior to treatment with the compound, which is also used for treating patients afflicted with pancreatic cancer.

Use of masitinib for treatment of cancer in patient subpopulations identified using predictor factors

Disclosed are compounds of formula I or pharmaceutically acceptable salts thereof: Wherein n, R, R, R, R, R, A, Q and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.

Benzimidazole derivatives as selective proteine kinase inhibitors

Disclosed is a method for treating patients afflicted with non-aggressive or moderately aggressive amyotrophic lateral sclerosis (ALS) whose rate of change of the revised Amyotrophic Lateral Sclerosis Functional Rating Scale (ALSFRS-R) prior to treatment initiation is &#x3c;1.1 points per month, the method including administering a tyrosine kinase inhibitor or mast cell inhibitor, in particular masitinib, or a pharmaceutically acceptable salt or solvate thereof, optionally in combination with at least one pharmaceutically active ingredient.

Use of masitinib for treatment of an amyotrophic lateral sclerosis patient subpopulation

The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, autoimmune, allergic, and degenerative disorders. In particular, the presently disclosed compounds are Syk inhibitors.

Diazaspiroalkaneone-substituted oxazole derivatives as spleen tyrosine kinase inhibitors

The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including the administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen.

Treatment of mastocytosis with masitinib

The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof: wherein R, R, R, A, Q, W and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.

Selective protein kinase inhibitors

The present invention relates to the treatment of severe persistent asthma, and in particular severe persistent corticosteroid-dependent or corticosteroid-resistant asthma, comprising administration a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof.

Treatment of severe persistant asthma with masitinib

Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.

2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors

The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors.

Thiazole and oxazole kinase inhibitors

The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.

Aminothiazole compounds as kinase inhibitors and methods of using the same

The present invention relates to a tyrosine kinase inhibitor or a mast cell inhibitor, and in particular masitinib or a pharmaceutically acceptable salt thereof, for the treatment of human multiple sclerosis.

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Paris, France

Alain Moussy