Patent classifications
A61P27/14
Substituted pyrazolo{4,3-D}pyrimidines as kinase inhibitors
The present invention relates to novel compounds of formula (I) ##STR00001##
that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
METHODS FOR TREATING RHINITIS AND CONJUNCTIVITIS
Apparatus, methods, and kits for treating symptoms associated with common ailments, such as headaches, rhinitis, asthma, epilepsy, nervous disorders and the like, are provided. The apparatus comprises dispensers for carbon dioxide other therapeutic gases. The methods comprise delivering small volumes of these gases to patients in a manner where the gas infuses into a body region in order to bathe the mucous membranes therein. It has been found that even very short exposure of patients to small volumes and high concentrations of such gases can provide significant relief from symptoms.
METHODS AND COMPOSITIONS INVOLVING RECOMBINANT HYPOALLERGENS
This disclosure describes recombinant hypoallergens and methods of treating allergy that involve administering a recombinant hypoallergen to a subject. Generally, the recombinant hypoallergen includes at least one amino acid modification compared to a corresponding wildtype allergen. As a result, the recombinant hypoallergen binds to IgE that specifically binds to the allergen, but induces release of histamine from basophils to a degree less than the wildtype allergen.
Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
Ocular therapy using glucocorticoid derivatives selectively penetrating posterior segment tissues
Ophthalmically therapeutic materials, such as liquid-containing compositions and polymeric drug delivery systems, include a therapeutic component that includes an Glucocorticoid Derivative which, upon delivery to the posterior segment of a mammalian eye, does not significantly diffuse to the anterior segment of said eye. Methods of making and using the present materials are also described.
Methods and compositions for daily ophthalmic administration of phentolamine to improve visual performance
The invention provides methods, compositions, and kits containing phentolamine for improving visual performance. In particular, the invention provides improvement in visual performance, such as improvement in visual acuity, by daily ophthalmic administration of a phentolamine solution to an eye of a patient at or near the bedtime of the patient for an extended duration while minimizing the occurrence of adverse side effects, such as eye redness during the patient's waking hours.
KINASE INHIBITORS
There are provided compounds of formula I,
##STR00001##
wherein T, A, Q, Z, G, R.sup.4, R.sup.5a, R.sup.5b and n have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Glutaminase inhibitors
The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine.
OPTIONALLY FUSED HETEROCYCLYL-SUBSTITUTED DERIVATIVES OF PYRIMIDINE USEFUL FOR THE TREATMENT OF INFLAMMATORY, METABOLIC, ONCOLOGIC AND AUTOIMMUNE DISEASES
Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
METHOD OF TREATMENT AND COMPOSITIONS COMPRISING A DUAL PI3K DELTA-GAMMA KINASE INHIBITOR AND A CORTICOSTEROID
This present disclosure relates to a method of treating autoimmune, respiratory and/or inflammatory diseases or conditions, e.g., asthma, COPD, rheumatoid arthritis and idiopathic Pulmonary Fibrosis (IPF). The method comprises administering a dual PI3K delta and gamma inhibitor and a corticosteroid. The present invention also relates to pharmaceutical compositions containing a dual PI3K delta and gamma inhibitor and a corticosteroid.