The present invention relates to compounds of formula I inhibiting P2X purinoceptor 3; particularly the invention relates to compounds that are amino quinazoline derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of many disorders associated with P2X.sub.3 receptors mechanisms, such as respiratory diseases including cough, asthma, idiopathic pulmonary fibrosis (IPF) and chronic obstructive pulmonary disease (COPD).

The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I) to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

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K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

Malonic ester derivatives of the formula (I) ##STR00001##
in which the symbols A.sup.1, A.sup.2, Y, R.sup.10, p, X, R.sup.2, G, Q, L.sup.2 and R.sup.1 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

The present invention relates to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine salts and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine salts; especially to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride as well as to the use of these salts for preventing or treating migraine or pulmonary hypertension.

The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.

Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions,that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

The invention relates to bicyclic heterocycle compounds of formula (I): ##STR00001##
or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP), such as those of formula (III), and composition thereof are described herein. Exemplary disorders include schizophrenia and cognitive deficit. ##STR00001##