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Patent # Description
2018/0194762 PYRAZOLO[3,4-b]PYRIDINE AND PYRROLO[2,3-b]PYRIDINE INHIBITORS OF BRUTON'S TYROSINE KINASE
Disclosed are pyrazolo[3,4-b]pyridine and pyrrolo[2,3-b]pyridine inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions...
2018/0194761 N2-PHENYL-PYRIDO[3,4- D]PYRIMIDINE-2, 8-DIAMINE DERIVATIVES AND THEIR USE AS MPS1 INHIBITORS
The present invention relates to compounds of formula I: ##STR00001## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are all as defined herein. The compounds of...
2018/0194760 HETEROBICYCLIC N-AMINOPHENYL-AMIDES AS INHIBITORS OF HISTONE DEACETYLASE
This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I) or any one of Compounds 100-175)...
2018/0194759 NOVEL FORMULATION OF MELOXICAM
The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam,...
2018/0194758 NOVEL PYRIMIDINES AS EGFR INHIBITORS AND METHODS OF TREATING DISORDERS
The application relates to a compound having Formula (I'): ##STR00001## which modulates the activity of EGFR, a pharmaceutical composition comprising the...
2018/0194757 NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula: ##STR00001## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the...
2018/0194756 NOVEL SOLUBLE GUANYLATE CYCLASE ACTIVATORS AND THEIR USE
The invention relates to activators of soluble guanylate cyclase and their use in pharmaceutical compositions, primarily topically administered ophthalmic...
2018/0194755 Tetrahydropyranyl Benzamide Derivatives
The present invention provides compounds of the Formula below ##STR00001## wherein R, R1-R3 are as described herein; methods of treating patients for diabetes...
2018/0194754 Polymorphs and Process for the Preparation of Quinazolinyl Derivatives
The present invention relates to Quinazolinyl derivatives polymorph, process and composition thereof. (I) ##STR00001##
2018/0194753 METHOD FOR PREPARING PYRAZOLECARBOXYLIC ACID DERIVATIVE, AND INTERMEDIATE THEREOF
Provided are a preparation method for synthesizing a pyrazolecarboxylic acid derivative of the following formula (I), which is suitable for industrial...
2018/0194752 NOVEL LEDIPASVIR CRYSTAL FORM AND PREPARATION METHOD THEREOF
The present invention relates to a novel Ledipasvir (LDV) crystal form and a preparation method thereof. Specifically, disclosed is an LDV solvate. The solvate...
2018/0194751 INDOLE DERIVATIVE, PREPARATION METHOD THEREOF, AND USE THEREOF IN PHARMACEUTICAL DRUG
An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a...
2018/0194750 NEW INDOLE COMPOUNDS HAVING ANTIPROTOZOAL ACTIVITY AND ITS USE AS WELL AS METHODS FOR PRODUCING THE SAME
In a first aspect, the present invention relates to new compounds as depicted in formula (I). In particular, compounds according to the present invention are...
2018/0194749 PLINABULIN COMPOSITIONS
Disclosed herein are plinabulin polymorphs, compositions, their use and preparation as therapeutic agents. In particular, some embodiments relate to plinabulin...
2018/0194748 SUBSTITUTED QUINAZOLINE COMPOUNDS AND METHODS OF USE THEREOF
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001## or a...
2018/0194747 Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation...
The present invention relates to compounds of general formula (I) ##STR00001## and the tautomers and the salts thereof, particularly the pharmaceutically...
2018/0194746 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...
2018/0194745 SUBSTITUTED OXOPYRIDINE DERIVATIVES
The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the...
2018/0194744 Third Generation Taxoids and Methods of Using Same
The invention includes taxoid compounds represented by the formula: ##STR00001## wherein: R.sup.1 represents a methyl group or a fluorine; R.sup.2 represents an...
2018/0194743 A process for the preparation of Mirabegron alpha-Form crystals
The present invention provides a process for the preparation of .alpha.-Form crystals of Mirabegron using a solvent selected from water.
2018/0194742 Antifungal Compounds
Compounds and compositions having antifungal activity, and methods of using the antifungal compounds and compositions, are described for use in treating fungal...
2018/0194741 NEW ANTI-MALARIAL AGENTS
The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the...
2018/0194740 DEOXYURIDINE TRIPHOSPHATASE INHIBITORS CONTAINING AMINO SULFONYL LINKAGE
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
2018/0194739 METHODS TO TREAT LYMPHOPLASMACYTIC LYMPHOMA
The present invention provides compounds of any one of Formulae (A), (I-11), (II), and (V) (e.g., compounds of Formula (A-1)-(A-18)), and methods for treating...
2018/0194738 PARG INHIBITORY COMPOUNDS
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R.sub.1a,...
2018/0194737 HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING
In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular...
2018/0194736 HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
2018/0194735 Sulfinylphenyl or Sulfonimidoylphenyl Benzazepines
This invention relates to novel sulfinylphenyl or sulfonimidoylphenyl benzazepine compounds of the formula ##STR00001## wherein X and R.sup.1 to R.sup.6 are as...
2018/0194734 A process for the preparation of Lorcaserin Hydrochloride
The present invention provides a process for the preparation of crystalline Lorcaserin hydrochloride hemihydrate of Formula (1a), which comprises, Formula (1a)...
2018/0194733 COMPOSITIONS AND METHODS OF TREATING RETINAL DISEASE
Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or...
2018/0194732 MULTI-API LOADING PRODRUGS
The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the...
2018/0194731 THERAPEUTIC COMPOUNDS
The invention provides compounds of formula (I): ##STR00001## wherein, A, C, D, X, and Y have any of the values defined in the specification, and salts thereof....
2018/0194730 4-[4-({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]CARBAMOYL}AMINO)-3-FLUOROPHENOX- Y]-N-METHYLPYRIDINE-2-CARBOXAMIDE...
The present invention relates to 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluoropheno- xy]-N-methylpyridine-2-carboxamide monohydrate, to...
2018/0194729 18F - TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) AND THEIR USE AS IMAGING AGENTS FOR...
The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various...
2018/0194728 METHOD FOR PREPARING PENTACHLOROPYRIDINE BY UTIILIZING DCTF RECTIFYING SHORT STEAMING RESIDUES
A method for preparing pentachloropyridine by utilizing DCTF rectifying short steaming residues, comprising the following steps: converting polymers in the...
2018/0194727 POLYMER ADDITIVE AND A METHOD FOR THE PRODUCTION THEREOF
The invention relates to a compound of formula (I), characterised by the characteristic signals in the X-ray diffraction powder pattern measured with Cu Kalpha...
2018/0194726 CRYSTALLINE COMPOUNDS
The present invention relates to crystalline forms of (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride and compositions comprising the same...
2018/0194725 PYRROLOMYCINS AND METHODS OF USING THE SAME
Provided herein are pyrrolomycin derivatives, which can be used to modulate Mcl-1, inhibit proliferation of bacteria and pathogens, as well as to treat...
2018/0194724 CYANOPYRROLIDINES AS DUB INHIBITORS FOR THE TREATMENT OF CANCER
The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention...
2018/0194723 PROCESS OF PURIFYING METHIONINE
The present invention provides a process for purifying methionine. A methionine product having a purity of up to 99% or higher is obtained by separating...
2018/0194722 INHIBITORS OF FATTY ACID AMIDE HYDROLASE (FAAH) ENZYME WITH IMPROVED ORAL BIOAVAILABILITY AND THEIR USE AS...
Described herein, inter alia, are compositions and methods useful for inhibiting fatty acid amide hydrolase.
2018/0194721 DIFLUOROALKYLCYCLOPROPYL AMINO ACIDS AND ESTERS, AND SYNTHESES THEREOF
The invention provides methods of synthesizing compounds in an asymmetric or enantioenriched fashion, wherein the compounds are useful intermediates in the...
2018/0194720 METHOD FOR PRODUCING ISOCYANATES
The invention relates to a method for producing isocyanates by reacting primary amines with phosgene in a stoichiometric excess in the gas phase, wherein the...
2018/0194719 CRYSTAL FORMS OF VERAPAMIL HYDROCHLORIDE
Novel crystal forms of (R)-(+)-verapamil hydrochloride are disclosed.
2018/0194718 NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula: ##STR00001## where R.sup.1-R.sup.5 and X are as defined in the specification, or a ...
2018/0194717 AMINO ACID DERIVATIVES AND ABSORBABLE POLYMERS THEREFROM
The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides,...
2018/0194716 THERAPEUTIC COMPOUNDS AND METHODS OF USE
The invention relates to protein biding interacting/binding compounds and methods of identifying and using them. The invention further relates to ...
2018/0194715 ANTICONVULSANT COMPOUNDS
The present application relates to compounds and methods for reducing the severity of convulsant activity or epileptic seizures, or for the treatment of...
2018/0194714 Lipids That Increase Insulin Sensitivity And Methods Of Using The Same
The invention provides, inter alia, fatty acyl hydroxy fatty acid (FAHFA; a novel class of estolide-related molecules) and diagnostic and treatment methods for...
2018/0194713 PROCESSES AND INTERMEDIATES FOR PREPARING alpha,omega-DICARBOXYLIC ACID-TERMINATED DIALKANE ETHERS
The present disclosure provides a process for the preparation of compounds of formula (III), ##STR00001## compounds of formula (V), ##STR00002## and...
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