Patent classifications
A61P11/06
SYNTHESIS OF HETEROCYCLIC COMPOUNDS
Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I):
##STR00001##
or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P.sup.1 and P.sup.2 are as defined in this disclosure.
SUBSTITUTED IMIDAZO[1, 2-A]PYRIDIN-2-YLAMINE COMPOUNDS, AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
Provided herein are substituted imidazo[1,2-a]pyridin-2-ylamine compounds, for example, of formula (A), and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a Janus kinase-mediated disease.
##STR00001##
COMPOSITION FOR PREVENTION OR TREATMENT OF BRONCHIAL ASTHMA COMPRISING PKR INHIBITOR AS ACTIVE INGREDIENT
The present invention relates to a composition for prevention or treatment of bronchial asthma comprising a PKR inhibitor as an active ingredient. The PKR inhibitor and derivatives thereof according to the present invention can be used as a pharmaceutical for prevention, amelioration or treatment of bronchial asthma and as a supplementary health food because the PKR inhibitor and derivatives thereof reduce the total counts of inflammatory cells, eosinophils, neutrophils and lymphocytes in bronchoalveolar lavage fluid of neutrophilic severe asthma-induced mice, reduce airway inflammation and airway hyper-responsiveness, and reduce inflammatory mediators.
CONTROLLED RELEASE PREPARATIONS
Controlled release preparations and soft capsules are provided. Also provided are emulsions and suspensions, including compositions and methods of manufacturing controlled release soft capsules, where the fill contains a suspension and/or an emulsion.
POLYMERIC DRUG CONJUGATES WITH TETHER GROUPS FOR CONTROLLED DRUG DELIVERY
Described herein is a cyclodextrin containing polymer conjugate.
SULPHATED HYALURONIC ACIDS AS REGULATOR AGENTS OF THE CYTOKINE ACTIVITY
The object of the present invention relates to the new and surprising use of sulfated hyaluronic acid (HAS) as regulator agent of the cytokine activity (pro- and antiinflammatory) and consequently the use of HAS for the preparation of a new medicine for the prevention and treatment of pathologies associated with the activation and/or deficiency of cytokines of a pro- and antiinflammatory nature. The Applicant has in fact discovered its exclusive capacity in modulating the activity of these particular proteins, it has studied the action mechanism and demonstrated the substantial difference between the different sulfated types known in the state of the art, but above all it has demonstrated an unexpectedly high activity of HAS vs different types and strains of Herpes virus, HIV, Cytomegalovirus and the virus of vesicular stomatitis.
COMBINATIONS OF A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2 ADRENORECEPTOR AGONIST
Combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, and methods of using them are provided.
ENZYMES AND METHODS FOR PRODUCING OMEGA-3 FATTY ACIDS
The present invention relates to methods of synthesizing long-chain polyunsaturated fatty acids, especially eicosapentaenoic acid, docosapentaenoic acid and docosahexaenoic acid, in recombinant cells such as yeast or plant cells. Also provided are recombinant cells or plants which produce long-chain polyunsaturated fatty acids. Furthermore, the present invention relates to a group of new enzymes which possess desaturase or elongase activity that can be used in methods of synthesizing long-chain polyunsaturated fatty acids. In particular, the present invention provides ω3 destaurases, Δ5 elongases and Δ6 desaturases with novel activities. Also provided are methods and DNA constructs for transiently and/or stably transforming cells, particularly plant cells, with multiple genes.
TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS
Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is (LQ).sub.mY; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.
##STR00001##
Novel formulation of metaxalone
The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments.