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Patent # Description
2017/0137443 BORON-BASED PRODRUG STRATEGY FOR INCREASED BIOAVAILABILITY AND LOWER-DOSAGE REQUIREMENTS FOR DRUG MOLECULES...
Boron-based prodrugs of phenol- or aromatic hydroxyl group-containing therapeutic molecules ("original drugs"), uses thereof, and methods of making the same,...
2017/0137442 MONONUCLEAR SALEN INDIUM CATALYSTS AND METHODS OF MANUFACTURE AND USE THEREOF
The present application provides salen indium catalysts of the following general structure wherein R is a coordinating alkoxide comprising at least one...
2017/0137441 Piperidine Derivatives And Compositions For the Inhibition Of Nicotinamide Phosphoribosyltransferase (NAMPT)
The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound...
2017/0137440 METHODS FOR THE ACYLATION OF MAYTANSINOL
Disclosed is a method of preparing an amino acid ester of maytansinol by reacting maytansinol with an N-carboxyanhydride of an amino acid (NCA) in the presence...
2017/0137439 sGC STIMULATORS
Compounds of Formulae I' and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds...
2017/0137438 METHODS FOR THE PREPARATION OF 1,3-BENZODIOXOLE HETEROCYCLIC COMPOUNDS
The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds and intermediates for the same. The compounds are...
2017/0137437 SYNTHESIS OF HALICHONDRIN ANALOGS AND USES THEREOF
The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting...
2017/0137436 Pyranodipyridine Compound
Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof: ##STR00001## ##STR00002## ##STR00003## ##STR00004## ##STR00005##
2017/0137435 2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES
The present invention relates to compounds of formula of formula I wherein X, L and R.sup.1 are as described herein, compositions containing compounds of...
2017/0137434 CRYSTALLINE FORMS OF 2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4,5-E]AZEPIN-4-Y- L)ACETAMIDE
The present disclosure relates to a crystalline form of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-y- l)acetamide, which is useful...
2017/0137433 CRYSTALLINE, ANHYDROUS FORMS OF OXYMORPHONE HYDROCHLORIDE
Crystalline, anhydrous hydrochloride salts of 4,5.alpha.-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one (oxymorphone) are disclosed and three polymorphic forms...
2017/0137432 SELECTIVE REDUCTION OF MORPHINAN ALKALOIDS
The present disclosure relates to selective reduction of morphinan alkaloids in a continuous flow system. In particular, the present disclosure relates to...
2017/0137431 MOLECULAR CONTAINERS AND METHODS OF MAKING AND USING SAME
Acyclic CB[n]-type compounds, methods of making such compounds, and uses of the compounds. For example, these compounds can be used as nanocontainers to...
2017/0137430 Nuclear Transport Modulators And Uses Thereof
The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by formula I: ...
2017/0137429 ANTI-INFLUENZA COMPOSITIONS AND METHODS
Disclosed are novel compounds comprising an imino-ribose derivative covalently linked to a carbocycle or heterocycle. Pharmaceutical compositions comprising...
2017/0137428 AZEPANYL-DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME WITH ANTIPARASITIC ACTIVITY
The present invention provides compounds of Formula (i). Furthermore, pharmaceutical compositions are provided comprising at least one compound of Formula (i),...
2017/0137427 IMIDAZO-PYRIDAZINE DERIVATIVES AS CASEIN KINASE 1 DELTA/EPSILON INHIBITORS
The invention provides compounds of Formula (I) and pharmaceutically-acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity...
2017/0137426 HETEROCYCLIC COMPOUNDS AS AXL INHIBITORS
Compounds of Formula I and their uses of effective AXL inhibitors and for the treatment of physical condition mediated by AXL. ##STR00001##
2017/0137425 TRICYCLIC COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
The disclosure provides compounds of formula I including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for...
2017/0137424 SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS
The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are...
2017/0137423 COMPOUNDS ACTING AT MULTIPLE PROSTAGLANDIN RECEPTORS GIVING A GENERAL ANTI-INFLAMMATORY RESPONSE
The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen...
2017/0137422 ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVIRUS INFECTION
Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are...
2017/0137421 QUINOLIZINONE DERIVATIVES AS PI3K INHIBITORS
Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R.sup.1-R.sup.4, and n...
2017/0137420 PYRIDINO[1,2-A]PYRIMIDONE ANALOGUE USED AS P13K INHIBITOR
Disclosed is a pyridino[1,2-a]pyrimidone analogue used as a PI3K inhibitor. The present invention particularly relates to a compound represented by formula (I)...
2017/0137419 DERIVATIVES OF 2H-PYRAZOLO[4,3-C]QUINOLIN-3(5H)-ONE AND USE THEREOF
The invention relates to compounds of formula (I) or the pharmaceutically acceptable solvates thereof, as well as to the use thereof as a drug. ##STR00001##
2017/0137418 SMALL MOLECULAR PROBES, PROCESSES AND USE THEREOF
The present disclosure relates to compounds which function as small molecule fluorescent probes which aid in recognition of specific sequences in DNA and...
2017/0137417 PHENYLPIPERIDINECARBOXAMIDE DERIVATIVES AS FUNGICIDES
Phenylpiperidinecarboxamide derivatives of the formula (I) ##STR00001## in which the symbols R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each as defined in the...
2017/0137416 6-AMINO-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL OR 3-AMINOCHROMAN-7-YL DERIVATIVES
The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and R.sup.1 are as described herein, compositions...
2017/0137415 SULFONAMIDE COMPOUNDS AS VOLTAGE GATED SODIUM CHANNEL MODULATORS
The present invention relates to the compound of Formula (I) wherein the substituents are as described herein, and their use in a medicine for the treatment of...
2017/0137414 COMPOUNDS AND THEIR METHODS OF USE
Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that...
2017/0137413 NOVEL HALOGEN-SUBSTITUTED COMPOUNDS
The invention relates inter alia to halogen-substituted compounds of the general formula (I) ##STR00001## in which the A.sub.1-A.sub.4, T, W, Q, R.sup.1 and...
2017/0137412 SUBSTITUTED PYRROLIDINES AS FACTOR XIA INHIBITORS FOR THE TREATMENT THROMBOEMBOLIC DISEASES
The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are...
2017/0137411 COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in...
2017/0137410 FUSED CYCLOALKYL-PYRIMIDINE COMPOUNDS AND USES THEREOF
Fused cycloalkyl-pyrimidine compounds that are kinase inhibitors, such as multi-kinase inhibitors, are provided. The compounds may be used in a method of...
2017/0137409 Amine Cationic Lipids and Uses Thereof
The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such...
2017/0137408 PROCESSES FOR THE PREPARATION OF PYRAZOLE DERIVATIVES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR
The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof,...
2017/0137407 HETEROCYCLIC COMPOUNDS AND USES THEREOF
Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods...
2017/0137406 ERK INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
2017/0137405 COMPOUNDS FOR THE TREATMENT OF HIV
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a...
2017/0137404 CRYSTALLINE FORM OF A SUBSTITUTED QUINOLINE COMPOUND AND PHARMACEUTICAL COMPOSITIONS THEREOF
The present invention relates to a crystalline form of N-(3-fluoro-4-((7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl)oxy)phenyl)-1,- ...
2017/0137403 REGIOSELECTIVE N-2 ARYLATION OF INDAZOLES
A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: ##STR00001## comprising a copper-catalyzed,...
2017/0137402 INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic...
2017/0137401 Chemokine CXCR4 and CCR5 Receptor Modulators and Uses Related Thereto
The disclosure relates to chemokine receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions...
2017/0137400 FLAVAGLINE DERIVATIVES
The invention relates to compounds of the following general formula (I) in the form of one of the enantiomers thereof or a mixture of the enantiomers thereof,...
2017/0137399 HIGH-PURITY MAGNESIUM LITHOSPERMATE B AND PREPARATION METHOD THEREFOR
The present invention relates to a method for preparing magnesium lithospermate B. The method is characterized in that: magnesium lithospermate B is extracted...
2017/0137398 OPSIN-BINDING LIGANDS, COMPOSITIONS AND METHODS OF USE
Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in...
2017/0137397 METHODS FOR PURIFYING 5-(HALOMETHYL)FURFURAL
The present disclosure provides methods for purifying a 5-(halomethyl)furfural composition, including 5-(chloromethyl)furfural, at operating conditions that...
2017/0137396 PROCESS FOR THE SELECTIVE OXIDATION OF 5-HYDROXYMETHYLFURFURAL
Process for the selective production of oxidized furan derivatives starting from 5-hydroxymethyl-2-furfural in the presence of a solvent, an oxidation agent, a...
2017/0137395 PROCESS FOR THE PRODUCTION OF FURAN AND ITS DERIVATIVES
The present invention provides a process for the production of furan, said process comprising the steps of: i) contacting furfural with a decarbonylation...
2017/0137394 ALKYLENE OXIDE SEPARATION SYSTEMS, METHODS, AND APPARATUSES
A propylene oxide separation system that comprises a distillation column, a decanter, and water wash system. The distillation column is configured to receive a...
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