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Patent # Description
US-9,458,152 Bicyclic sulfonamide compounds as sodium channel inhibitors
The present invention provides compounds of Formula I, ##STR00001## and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium...
US-9,458,151 Isothiazole derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof
PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically...
US-9,458,150 Antimicrobial agents
The invention provides compounds of formula (I): ##STR00001## wherein R.sup.1-R.sup.3, n, and W have any of the values defined in the specification, and salts...
US-9,458,149 Crystal form of dabrafenib and preparation method and use thereof
The invention relates to Crystal Form VII of dabrafenib and preparation method thereof, wherein Crystal Form VII has the advantage of being more stable at room...
US-9,458,148 Crystalline form of masitinib
Provided is a polymorphic form of Masitinib mesylate, processes for its preparation, compositions comprising it and their medical use.
US-9,458,147 Sulfonamide compounds and uses as TNAP inhibitors
Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the...
US-9,458,146 Crystalline sodium salt of an HIV integrase inhibitor
A crystalline sodium salt of a compound of formula I (INN: Raltegravir) ##STR00001## or a hydrate/solvate thereof is disclosed as well as a process for...
US-9,458,145 Benzimidazole derivatives as bromodomain inhibitors
This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing...
US-9,458,144 Monomer, polymer, resist composition, and patterning process
A monomer (1) is prepared by reacting a compound (9) with a base or metal to form a metal enolate reagent, and reacting the metal enolate reagent with an...
US-9,458,143 Triazabutadienes as additives in adhesive systems
Triazabutadiene molecules that provide adhesive functionality, e.g., triazabutadiene molecules as underwater adhesives or water-reactive adhesives. The...
US-9,458,142 Substituted quinones or analogues as colouring agents
The invention relates to protein-adhesive dyes, to the preparation thereof and to preparations comprising same, and to a method for coloring keratin-containing...
US-9,458,141 Low molecular weight thyroid stimulating hormone receptor (TSHR) agonists
Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating...
US-9,458,140 Furanone compounds as kinase inhibitors
The present disclosure provides novel furanone compounds, or pharmaceutically acceptable salts, solvates or prodrugs thereof, as Raf kinase, especially BRAF...
US-9,458,139 Compounds and uses thereof for the modulation of hemoglobin
Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods...
US-9,458,138 Pyrrole compounds as granzyme B inhibitors
Pyrrole compounds as Granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Method for treating cutaneous...
US-9,458,137 Substituted indol-5-ol derivatives and their therapeutical applications
The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the...
US-9,458,136 Crystalline forms and processes for the preparation of cannabinoid receptor modulators
The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclop- ropa[a]pentalene-4-carboxylic...
US-9,458,135 Dihydroquinoline-2-one derivatives
The invention provides novel compounds having the general formula (I) ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7,...
US-9,458,134 Heterocycles as modulators of kinase activity
The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as...
US-9,458,133 Isoquinolines as potassium ion channel inhibitors
A compound of formula (I) (I) wherein A, R1, R1a, R3 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in...
US-9,458,132 Therapeutic compounds and compositions and their use as PKM2 modulators
Compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the...
US-9,458,131 Compounds and compositions used to epigenetically transform cells and methods related thereto
This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods...
US-9,458,130 Compositions and methods for treating schizophrenia
The disclosure provides a novel polymorph of Compound (I): ##STR00001## 2-((1-(2-(4-Fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-o- ne...
US-9,458,129 Histone demethylase inhibitors
Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising...
US-9,458,128 Catechol O-methyltransferase activity inhibiting compounds
Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods...
US-9,458,127 Bis-acylated hydroxylamine derivatives
The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of...
US-9,458,126 Monomer for binding nano-metal, conductive polymer composite and method of preparing the conductive polymer...
Disclosed herein is a monomer for binding nano-metal, which is useful for the preparation of a conductor having increased conductivity with ensuring flexibility...
US-9,458,125 Octahydro binaphthyl-based chiral compound-containing liquid-crystal composition and optical element
A liquid-crystal composition is composed of at least one chiral compound represented by general formula (K1) or (K2) and at least one achiral liquid-crystal...
US-9,458,124 Substituted pyran derivatives
Certain 3,6-disubstituted and 2,4,5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3,6 and 2,4,5...
US-9,458,123 Methods, pharmaceutical compositions, therapeutic systems, and compounds for treating B cell malignancies
This invention relates to a method of treating B cell malignancies, which involves administering to a subject a compound having a structure of formula (I) to...
US-9,458,122 Process for purifying crude furan 2,5-dicarboxylic acid using hydrogenation
A process to produce a dry purified furan-2,5-dicarboxylic acid (FDCA) is described. After oxidation of 5-(hydroxymethyl)furfural (5-HMF), a crude FDCA stream...
US-9,458,121 Epoxidation methods
A method for the epoxidation of alkylenes is provided. The method makes use of an epoxidation catalyst comprising a support, silver, manganese and greater than...
US-9,458,120 Phenoxypropanol derivative and pharmaceutical composition including the same
The present invention relates to a novel phenoxypropanol derivative, represented by the structure of Chemical Formula I, and a racemate thereof, a...
US-9,458,119 Process for production of DFMB derivatives
A process for the production of a compound of formula (III) which comprises a step of reacting a compound of formula (I) with an excess amount of a compound of...
US-9,458,118 Sodium channel modulators for the treatment of pain and diabetes
Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I or compounds of Formula I': ##STR00001## In...
US-9,458,117 Process for producing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid and complexes thereof
A process for producing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) including salts and hydrates thereof of general formula (I) from the...
US-9,458,116 Benzoguanamine compound having aminomethyl group, or salt thereof, and method for manufacturing the same
A benzoguanamine compound having an amino methyl group is represented by the following Formula (1), or a salt thereof: ##STR00001## wherein R represents a...
US-9,458,115 Synthesis of substituted pyrazines
A method for synthesizing a pyrazine-containing material according to one embodiment includes contacting an iminodiacetonitrile derivative with a base and a...
US-9,458,114 Quinazolines as potassium ion channel inhibitors
A compound of formula I ##STR00001## wherein A, X, Y, Z, R.sub.1 and R.sub.24 are described herein. The compounds are useful as inhibitors of potassium...
US-9,458,113 Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
Substituted dihydropyrimidinones of formula 1 ##STR00001## which are neutrophil elastase inhibitors and useful as medicaments for the treatment of, inter...
US-9,458,112 Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1
The present invention relates to compounds of formula I: ##STR00001## in which Y, Y.sub.1, Y.sub.4, Y.sub.5, Y.sub.6, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are...
US-9,458,111 Process for the synthesis of substituted urea compounds
A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof: ##STR00001## the process...
US-9,458,110 Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables...
US-9,458,109 Substituted berbines and processes for their synthesis
The present invention provides processes for the synthesis of substituted berbine compounds. Also provided are intermediates used in the synthesis of...
US-9,458,108 Heteroaryl compounds useful as inhibitors of E1 activating enzymes
This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the...
US-9,458,107 Process for the preparation of 4-{4-[({[4 ...
The present invention relates to a process for preparing 4-(4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluo- ...
US-9,458,106 Phenyl-pyridine/pyrazine amides for the treatment of cancer
The invention provides novel compounds having the general formula: ##STR00001## wherein R.sup.1, R.sup.2, A and W are as described herein, compositions...
US-9,458,105 Inhibitors of Bruton's tyrosine kinase
This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds...
US-9,458,104 Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan...
The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy...
US-9,458,103 Compositions and methods for inhibition of cathepsins
This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin,...
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