Patent classifications
A61K31/606
Metal-olsalazine coordination polymers for medical applications
Olsalazine (H.sub.4olz), a prodrug of the anti-inflammatory 5-aminosalicylic acid, is used as a ligand to synthesize a suite of M(H.sub.2olz) and M.sub.2(olz) materials, where M is a dication (e.g. Mg, Ca, Sr, Fe, Co, Ni, Cu, Zn). A family of metal olsalazine coordination polymers, coordination solids, and metal organic frameworks are described, which include 1-, 2-, and 3-dimensional structures. The materials resist degradation at acidic pH and release olsalazine preferentially at neutral pH. The mesoporous M.sub.2(olz) frameworks exhibit high surface areas with hexagonal pore apertures that are approximately 27 Å in diameter and contain coordinatively unsaturated metal sites. Biologically active molecules containing a Lewis-basic functional group can be grafted directly to the open metal sites of the frameworks. Dissolution of the frameworks under physiological conditions releases olsalazine (H.sub.4olz) and the grafted molecules so that multiple therapeutic components can be delivered together at different rates.
CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES FOR TREATING INFLAMMATORY BOWEL DISEASE
The present disclosure relates to methods for treating inflammatory bowel disease, with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof, that inhibit dipeptidyl peptidase 1 (DPP1) activity. In one embodiment, the compound of Formula (I) is (2S)—N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide.
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CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES FOR TREATING INFLAMMATORY BOWEL DISEASE
The present disclosure relates to methods for treating inflammatory bowel disease, with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof, that inhibit dipeptidyl peptidase 1 (DPP1) activity. In one embodiment, the compound of Formula (I) is (2S)—N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide.
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CONTROLLED RELEASE DOSAGE FORMS OF 5-AMINOSALICYLIC ACID AND PROCESS THEREOF
Accordingly, the invention provides controlled release minitablets of 5-ASA with high drug load and less net weight for easier administration. In another aspect of the present invention, the process of preparation of 5-ASA or its prodrugs/derivatives as coated minitablets, wherein the minitablets are prepared by wet granulation of 5-Aminosalicylic acid or its prodrugs/derivatives and at least one pharmaceutical retarding agent either at intra granular or extragranular stage and at least one pharmaceutical excipient or carrier of other categories for tableting. Then, the granules are size controlled through milling with size in the range of 100 microns to 700 microns. Further the granules are compressed using single tip or multi-tip punch and die to get the required size and shape and used as minitablets in sachets for administering with water/soft foods or encapsulated in capsules for whole administration.
CONTROLLED RELEASE DOSAGE FORMS OF 5-AMINOSALICYLIC ACID AND PROCESS THEREOF
Accordingly, the invention provides controlled release minitablets of 5-ASA with high drug load and less net weight for easier administration. In another aspect of the present invention, the process of preparation of 5-ASA or its prodrugs/derivatives as coated minitablets, wherein the minitablets are prepared by wet granulation of 5-Aminosalicylic acid or its prodrugs/derivatives and at least one pharmaceutical retarding agent either at intra granular or extragranular stage and at least one pharmaceutical excipient or carrier of other categories for tableting. Then, the granules are size controlled through milling with size in the range of 100 microns to 700 microns. Further the granules are compressed using single tip or multi-tip punch and die to get the required size and shape and used as minitablets in sachets for administering with water/soft foods or encapsulated in capsules for whole administration.
ACC INHIBITORS FOR USE IN TREATING MYCOBACTERIAL DISEASES
Compounds which are suitable for treating mycobacterial diseases and pharmaceutical compositions containing such compounds are provided. Also encompassed are such compounds for use in medicine. The disclosure further relates to a kit of parts comprising a pharmaceutical composition containing such compounds and at least one additional pharmaceutically active compound.
ACC INHIBITORS FOR USE IN TREATING MYCOBACTERIAL DISEASES
Compounds which are suitable for treating mycobacterial diseases and pharmaceutical compositions containing such compounds are provided. Also encompassed are such compounds for use in medicine. The disclosure further relates to a kit of parts comprising a pharmaceutical composition containing such compounds and at least one additional pharmaceutically active compound.
TOPICAL COMPOSITIONS AND METHODS FOR TREATING PAIN
Disclosed are compositions and methods for the treatment of pain and/or inflammation. In certain embodiments, the disclosed compositions and methods have anti-inflammatory activity. In some embodiments, the disclosed compositions and methods have analgesic activity. The present disclosure provides that two non-steroidal anti-inflammatory agents, as for example, 2-(4-isobutylphenyl)propanoic acid (ibuprofen), acetylsalicylic acid (aspirin), a muscle relaxant, and cannabidiol (CBD) can be used in combination in a topical formulation as an effective analgesic and/or anti-inflammatory agent.
TOPICAL COMPOSITIONS AND METHODS FOR TREATING PAIN
Disclosed are compositions and methods for the treatment of pain and/or inflammation. In certain embodiments, the disclosed compositions and methods have anti-inflammatory activity. In some embodiments, the disclosed compositions and methods have analgesic activity. The present disclosure provides that two non-steroidal anti-inflammatory agents, as for example, 2-(4-isobutylphenyl)propanoic acid (ibuprofen), acetylsalicylic acid (aspirin), a muscle relaxant, and cannabidiol (CBD) can be used in combination in a topical formulation as an effective analgesic and/or anti-inflammatory agent.
USE OF INHIBITORS OF BRUTONS TYROSINE KINASE (BTK)
Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.