Patent classifications
A61P13/10
ANTI-PACAP ANTIBODIES AND USES THEREOF
The present invention is directed to antibodies and antigen binding fragments thereof having binding specificity for PACAP. The antibodies and antigen binding fragments thereof comprise the sequences of the V.sub.H, V.sub.L, and CDR polypeptides described herein, and the polynucleotides encoding them. Antibodies and antigen binding fragments described herein bind to and/or compete for binding to the same linear or conformational epitope(s) on human PACAP as an anti-PACAP antibody. The invention contemplates conjugates of anti-PACAP antibodies and binding fragments thereof conjugated to one or more functional or detectable moieties. Methods of making said anti-PACAP antibodies and antigen binding fragments thereof are also contemplated. Other embodiments of the invention contemplate using anti-PACAP antibodies, and binding fragments thereof, for the diagnosis, assessment, and treatment of diseases and disorders associated with PACAP and conditions where antagonism of PACAP-related activities, such as vasodilation, photophobia, mast cell degranulation, and/or neuronal activation, would be therapeutically beneficial.
PROCESSES FOR PREPARING TRIAZOLE GLYCOLATE OXIDASE INHIBITORS
The present disclosure provides processes for preparing 1,2,3-tri-azole-4-carboxylic acid related compounds of formulae (I) and (II) via a Suzuki coupling reaction. The Suzuki coupling reaction is achieved by coupling a compound of formula (IV), a boron-containing derivative of 1,2,3-triazole-4-carb oxylate, with a cycloalkyl phenyl halide or sulfonate of formula (V).
##STR00001##
TREATMENT OF HYPERINFLAMMATORY SYNDROME
Described is an antagonist of a mammalian P2X7R for use in the treatment of a hyperinflammatory syndrome in a mammalian patient, by primary lymph node targeted administration of the said P2X7R antagonist in the said patient to a concentration in the said targeted lymph nodes that is above the maximal tolerable plasma level of the said antagonist in the said mammal.
TREATMENT OF HYPERINFLAMMATORY SYNDROME
Described is an antagonist of a mammalian P2X7R for use in the treatment of a hyperinflammatory syndrome in a mammalian patient, by primary lymph node targeted administration of the said P2X7R antagonist in the said patient to a concentration in the said targeted lymph nodes that is above the maximal tolerable plasma level of the said antagonist in the said mammal.
SYNTHESIS OF NOVEL EP4 ANTAGONIST AND USE IN CANCER AND INFLAMMATION
The present disclosure provides a novel compound effective in antagonizing EP4, which is a compound represented by Formula I, or a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug of the compound represented by Formula I:
##STR00001## wherein: R.sup.1 is selected from —CH.sub.3, —CHF.sub.2, and —CF.sub.3; R.sup.2 is selected from C.sub.2-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl, C.sub.2-C.sub.6 halogen-substituted alkyl, C.sub.3-C.sub.6 halogen-substituted cycloalkyl; R.sup.3 is selected from hydrogen, halogen, C.sub.1-C.sub.2 alkyl, C.sub.1-C.sub.2 fluorine- or chlorine-substituted alkyl; R.sup.4 is selected from hydrogen, halogen, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, C.sub.1-C.sub.6 halogen-substituted alkyl, C.sub.1-C.sub.6 halogen-substituted alkoxyl.
Injectable botulinum toxin formulations
This invention provides novel injectable compositions comprising botulinum toxin that may be administered to a subject for various therapeutic, aesthetic and/or cosmetic purposes. The injectable compositions contemplated by the invention exhibit one or more advantages over conventional botulinum toxin formulations, including reduced antigenicity, a reduced tendency to undergo unwanted localized diffusion following injection, increased duration of clinical efficacy or enhanced potency relative, faster onset of clinical efficacy, and/or improved stability.
Tumor necrosis factor-like ligand 1A specific antibodies and compositions and uses thereof
The present invention provides antibodies, or antigen-binding fragment thereof, which specifically bind to tumor necrosis factor (TNF)-like ligand 1A(TL1A) The invention further provides a method of obtaining such antibodies and nucleic acids encoding the same. The invention further relates to compositions and therapeutic methods for use of these antibodies for the treatment and/or prevention of TL1A mediated diseases, disorders or conditions.
Dihydronaphthalene derivative
A compound represented by general formula (I) wherein all the symbols are as defined in the specification has a selective S1P5 receptor agonist activity due to having a linker from a phenyl group to a cyclic substituent in a dihydronaphthalene skeleton; i.e., due to having a short linker of one atom or less as L in general formula (I), and can therefore serve as an agent for treating S1P5-mediated disease, e. g., neurodegenerative disease such as schizophrenia. ##STR00001##
Crystalline form of a 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compound
The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.