A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.

Thrombin receptor antagonists

Compositions and methods comprising proteinase activated receptor antagonists are provided. More particularly, the present invention relates to the use of proteins, peptides and molecules that bind to proteinase activated receptor 2, and inhibit the processes associated with the activation of that receptor. More specifically, the present invention provides novel compositions and methods for the treatment of disorders and diseases such as those associated with abnormal cellular proliferation, angiogenesis, inflammation and cancer.

Compositions and methods comprising proteinase activated receptor antagonists

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK

This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crys-talline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer, hyperprolif-erative diseases and inflammatory conditions. The invention also concerns methods of making the compunds and compositions described herein.

Derivatives of n-(arylamino) sulfonamides including polymorphs as inhibitors of mek as well as compositions, methods of use and methods for preparing the same

Polymorphism and solvatomorphism 2007

A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. 3, and is represented by the formula for Compound 2: Chemical formula should be inserted here as it appears on the abstract in paper form. and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.

Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist

Process for the production of a crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist

PROBLEM TO BE SOLVED: To provide a crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist. SOLUTION: A compound 2 which is the crystalline polymorph of the bisulfate salt can be obtained from a thrombin receptor antagonist compound 1 according to a process represented by formula (A). The compound 2 has higher stability than that of the compound 1. The compound can be used as a pharmaceutical composition for treating thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, myocardial infarction, glomerulonephropathy, thrombotic stroke, thromboembolic cerebral stroke, peripheral vascular disease, inflammatory lesion, cerebral ischemia or cancer. COPYRIGHT: (C)2010,JPO&INPIT

Crystalline polymorph of bisulfate salt of thrombin receptor antagonist

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Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist

Process for the production of a crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist

Crystalline polymorph of bisulfate salt of thrombin receptor antagonist