Patent classifications
A61P1/06
Solid forms of an sGC stimulator
The present disclosure relates to crystalline solid forms of a stimulator of soluble guanylate cyclase (sGC), Compound I: ##STR00001##
Also provided herein are methods for the preparation of these solid forms. The invention also relates to pharmaceutical formulations and dosage forms comprising these solid forms and their uses thereof, alone or in combination with one or more additional agents, for treating and/or preventing various diseases or disorders; these diseases or disorders are ones that may benefit from sGC stimulation or from an increase in the concentration of nitric oxide (NO) and/or cyclic guanosine monophosphate (cGMP).
Conotoxin polypeptide κ-CPTx-bt105, and method for preparation thereof and application thereof
Disclosed are a conotoxin polypeptide -CPTx-bt105, a method for preparation thereof, and an application thereof. The conotoxin polypeptide of the present invention consists of 16 amino acids, has a molecular weight of 1626.62 daltons, and has the full sequence GICCVDDTCTTHSGCL (SEQ. ID NO. 1).
PRODRUGS OF PYRIDONE AMIDES USEFUL AS MODULATORS OF SODIUM CHANNELS
The invention relates to prodrug compounds of formula I:
##STR00001##
wherein R.sup.2, R.sup.3, R.sup.5, R.sup.7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.
SOLID DISPERSION OF RIFAXIMIN
A solid dispersion of rifaximin comprising rifaximin and pharmaceutically acceptable carrier. A pharmaceutical composition comprising the solid dispersion of rifaximin.
METHODS FOR THE TREATMENT OF DISEASES AMELIORATED BY PDE4 INHIBITION USING DOSAGE TITRATION OF APREMILAST
Methods of treating, managing or preventing diseases ameliorated by inhibiting PDE4 such as psoriasis, ankylosing spondylitis, Behcet's disease, rheumatoid arthritis, atopic dermatitis, Crohn's disease, and ulcerative colitis are disclosed. Specific methods encompass the administration of apremilast in specific dosage titration schedule, alone or in combination with a second active agent.
Engineered botulinum neurotoxin
Disclosed herein are botulinum neurotoxin (BoNT) polypeptides with a modified receptor binding domain of Clostridial botulinum serotype B (B-H.sub.c), comprising one or more substitution mutations corresponding to substitution mutations in serotype B, strain 1, V1118M; Y1183M; E1191M; E1191I; E1191Q; E1191T; S1199Y; S1199F; S1199L; S1201V; or combinations thereof. Specific combination mutations include E1191M and S1199L, E1191M and S1199Y, E1191M and S1199F, E1191Q and S1199L, E1191Q and S1199Y, or E1191Q and S1199F. Other substitution mutations are also disclosed. Isolated modified receptor binding domains, chimeric molecules, pharmaceutical compositions, and methods of using the same are also disclosed.
SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) AND USES THEREOF
Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
Compositions for use in improving stool consistency or frequency in infants or young children
The present invention relates to a nutritional composition comprising at least one fucosylated oligosaccharide for use in preventing and/or treating constipation and/or in improving stool consistency/frequency in an infant or a young child.
Pyridopyrimidines derivatives compounds
The present invention describes new pyridopyrimidine derivatives compounds with structure represented by General Formula (I): ##STR00001##
or pharmaceutically acceptable salts thereof, or their mixtures (in any ratio), a pharmaceutical composition containing them, a method for using the new pyridopyrimidine derivatives compounds as inhibitor of the cyclic nucleotide synthesis or as inhibitor of the cAMP and cGMP synthesis, and their uses in the prophylactic and/or curative treatment of diarrhea, colitis and irritable bowel syndrome.
METHODS FOR THE MANUFACTURE OF PROTEOLYTICALLY PROCESSED POLYPEPTIDES
A proteolytically active polypeptide comprising an acid sequence having at least 50% sequence identity with the sequence of SEQ ID NO: 1 with the proviso that the polypeptide does not comprise the amino acid sequence of SEQ ID NO: 1. A nucleic acid encoding the polypeptide. An antibody specifically binding to tile polypeptide. A method for the manufacture of a proteolytically processed polypeptide comprising contacting a first polypeptide having at least 50% sequence identity to SEQ ID NO: 1 with a second polypeptide that is susceptible to proteolysis by said first polypeptide.