The present invention relates to an oxa spiro derivative, a preparation method therefor, and applications thereof in medicines. Particularly, the present invention relates to an oxa spiro derivative represented by formula (I), a preparation method therefor, and a pharmaceutical composition comprising the derivative, applications thereof as an MOR receptor agonist, and applications in the preparation of drugs for treating and/or preventing pains and pains-related diseases. Substituent groups in the formula (I) are same as definitions in the specification. ##STR00001##

The present invention relates to an improved crystallization procedure to obtain canagliflozin hemihydrate crystals having a narrow particle size distribution by removing a small part of the crystalline suspension in the crystallization vessel from said vessel and subjecting said part to particle size reduction of the formed crystals followed by heating and reintroducting said part of the crystalline suspension again in the crystallization vessel which is kept within a specific temperature range.

The present invention relates to certain novel substituted thiophene compounds and the finding that they display useful efficacy in the inhibition of the p38 MAPK enzyme. This provides for use of the compounds in various treatment methodologies related to MAPK inhibition, including the treatment of inflammation.

The present invention relates to certain novel substituted thiophene compounds and the finding that they display useful efficacy in the inhibition of the p38 MAPK enzyme. This provides for use of the compounds in various treatment methodologies related to MAPK inhibition, including the treatment of inflammation.

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.

Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.

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).

A sulfoxide compound and method of producing benzothiophene derivatives using the same are provided. The sulfoxide compound is represented by formula (I), wherein R.sub.1 and R.sub.2 are individually and independently benzoyl group; alkyl, acyl or silyl group of C.sub.1-C.sub.6 straight chain or branched chain; or alkenyl group of C.sub.3-C.sub.6 straight chain or branched chain; and X is halogen atom. The sulfoxide compound reacts with alkynyl compound, and then the synthesis efficiency of benzothiophene derivatives can be effectively increased. ##STR00001##

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.