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Patent # Description
2018/0230127 Bicyclic-Fused Heteroaryl Or Aryl Compounds
Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor...
2018/0230126 NICOTINE SALTS, CO-CRYSTALS, AND SALT CO-CRYSTAL COMPLEXES
The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular,...
2018/0230125 MICROBIOCIDAL HETEROBICYCLIC DERIVATIVES
Compounds of the formula (I), wherein A, Y--X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.b, R.sub.c, R.sub.d, R.sub.5, R.sub.6, R.sub.7, R.sub.a, m and n are...
2018/0230124 PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the...
2018/0230123 BENZOTHIOPHENE ESTROGEN RECEPTOR MODULATORS
This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to...
2018/0230122 PRODUCTION METHOD FOR HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE, PRODUCTION INTERMEDIATE THEREOF, AND CRYSTAL
Compounds of formula (VI), which are useful as therapeutic drugs for diabetes, may be produced by reacting a compound of formula (II) with an acid halogenating...
2018/0230121 METHOD FOR PREPARATION OF THIOPHENE-2-CARBONYL CHLORIDES WITH OXALYL CHLORIDE
The invention discloses a method for the preparation of thiophene-2-carbonyl chlorides starting from thiophenes with oxalyl chloride at elevated temperature...
2018/0230120 CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS
The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as...
2018/0230119 USE OF 3-DEOXYANTHOCYANIDINS FOR TREATING OCCULAR DISEASES
Disclosed is a method for the treatment, prevention and/or stabilisation of ARMD, Stargardt disease, pigmentary retinopathy and/or diabetic retinopathy,...
2018/0230118 PREPARATION OF FURAN FATTY ACIDS FROM 5-(CHLOROMETHYL)FURFURAL
The present invention provides methods of making furfural fatty acids from (chloromethyl)furfural. The present invention also provides furfural fatty acids and...
2018/0230117 PART-STREAM DISTILLATION
A continuous process for preparing propylene oxide proceeds by (a) reacting propene with hydrogen peroxide in a reaction apparatus in the presence acetonitrile...
2018/0230116 PROCESS FOR THE PREPARATION OF VORTIOXETINE AND SALTS THEREOF
The present invention provides an improved process for preparation of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine; commonly known as vortioxetine...
2018/0230115 cGAS ANTAGONIST COMPOUNDS
Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the...
2018/0230114 1,3,4-OXADIAZOLE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICALCOMPOSITION...
The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) in-hibitory activity, stereoisomers thereof or pharmaceutically...
2018/0230113 1,3,4-OXADIAZOLE SULFAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL...
The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable...
2018/0230112 STEREOSPECIFIC PROCESS FOR 3-HETEROCYCLYLCYCLOALIPHATIC-1,2-DIOLS
A process for the stereoselective synthesis of chiral 3-heterocyclyl-1,2-dihydroxy cyclohexanes is disclosed. The process involves reacting a tricyclic...
2018/0230111 SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF
The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the...
2018/0230110 Isoxazole Carboxamides as Irreversible SMYD Inhibitors
The present disclosure provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein...
2018/0230109 TRIAZOLE COMPOUNDS AS T-TYPE CALCIUM CHANNEL BLOCKERS
The invention relates to compounds of formula (I) ##STR00001## wherein X, Y, R.sup.1, R.sup.2, (R.sup.4).sub.n, and (R.sup.5).sub.m are as defined in the...
2018/0230108 HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting...
2018/0230107 FORMATION OF N-PROTECTED 3,6-BIS-(4-AMINOBUTYL)-2,5-DIKETOPIPERAZINE THROUGH A CYCLIC ALPHA-N-PROTECTED AMINO...
A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic .alpha.-N protected active...
2018/0230106 REVERSIBLY PROTECTED TRIAZABUTADIENES AND TRIAZABUTADIENE-DERIVED FLUOROPHORES
Triazabutadiene molecules for use in applications. e.g., those involving fluorogenic molecules, e.g., triazabutadiene molecules configured to generate a...
2018/0230105 THERAPEUTIC COMPOUNDS
The invention provides compounds of formula Ia', Ib', Ic', and Id': ##STR00001## and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6,...
2018/0230104 A NOVEL PROCESS FOR PREPARING CRYSTALLINE METHYL ...
The present invention relates to a process for preparing crystalline methyl N-[2-[[[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl]phenyl]-N-me- thoxycarbamate...
2018/0230103 METHOD FOR PREPARATION OF 1-METHYL-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-5-OL
The invention discloses a method for the preparation of 1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-ol with high selectivity with respect to the content of the...
2018/0230102 CARBOXY SUBSTITUTED (HETERO) AROMATIC RING DERIVATIVES AND PREPARATION METHOD AND USES THEREOF
Carboxy-substituted (hetero)aryl derivatives, pharmaceutical compositions comprising these compounds, and methods of preparing such compounds and compositions...
2018/0230101 PROCESS FOR THE PREPARATION OF 5-AMINO-QUINOLIN-2(1H)-ONES AND THEIR TAUTOMER FORMS 5-AMINO-QUINOLIN-2-OLS
The present invention relates to a novel process for the preparation of 5-Amino-quinolin-2(1H)-ones and its tautomer's 5-amino-quinolin-2-ols. The present...
2018/0230100 Processes for Preparing Quinoline Derivatives
A process for preparing a compound of Formula I is disclosed, comprising the steps: ##STR00001## wherein: R.sup.1 is halo; R.sup.2 is halo; R.sup.3 is ...
2018/0230099 PROCESS FOR PREPARING CARBAZOLES
A process for preparing one or more carbazoles comprising (a) contacting one or more compounds represented by formula (1) below with diboron reagents in the...
2018/0230098 COMPOUNDS USEFUL AS CCR9 MODULATORS
The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them....
2018/0230097 PROCESS FOR PREPARATION OF APREMILAST AND NOVEL POLYMORPHS THEREOF
The present invention provides an improved process for preparation of an intermediate of apremilast. The present invention also provides an improved process...
2018/0230096 APOPTOSIS RELATED PROTEIN IN THE TGF-BETA SIGNALING PATHWAY (ARTS) MIMETIC COMPOUNDS, COMPOSITIONS, METHODS AND...
Provided are ARTS mimetic compounds that act as novel antagonists for XIAP and Bcl-2. Further, the novel ARTS mimetic compounds of the presently claimed...
2018/0230095 METHOD FOR PRODUCING PYRROLE DERIVATIVE, AND INTERMEDIATE THEREOF
The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity,...
2018/0230094 STABILIZER COMPOUND, LIQUID CRYSTAL COMPOSITION, AND DISPLAY ELEMENT
The present invention provides a compound represented by General Formula (I). The compound according to the present invention prevents the liquid crystal...
2018/0230092 NOVEL ANTIVIRAL AGENTS AGAINST HBV INFECTION
The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly...
2018/0230091 COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS
Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.
2018/0230090 SULFAMATE DERIVATIVE COMPOUNDS, PROCESSES FOR PREPARING THEM AND THEIR USES
The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a sulfamate derivative compound and/or...
2018/0230089 Amino Acid Derivatives and Their Uses
Provided are compounds described by the Formula I: ##STR00001## wherein: R.sub.1 is a linear or branched, saturated or unsaturated aliphatic group having from...
2018/0230088 IMAGING AGENTS
Provided herein is technology relating to imaging agents and particularly, but not exclusively, to methods of manufacturing fluorine-18-labeled...
2018/0230087 OLIGO-BENZAMIDE COMPOUNDS AND THEIR USE
The present invention includes bis- and tris-benzamide compounds that block AR signaling and have anticancer activity. Uses for these compounds, and...
2018/0230086 SELECTED AMIDE OF Y-HYDROXYBUTYRIC ACID AND USES THEREOF IN THE TREATMENT OF ALCOHOL MISUSE
The present invention relates to a selected amide of .gamma.-hydroxybutyric acid, a process of manufacture and uses thereof. The invention also includes a...
2018/0230085 1,4-DISUBSTITUTED IMIDAZOLE DERIVATIVE
The present invention provides a 1,4-disubstituted imidazole derivative of formula (1') wherein ring Q.sup.1 is optionally-substituted C.sub.6-10 aryl group,...
2018/0230084 Benzo Annulenes as Antiviral Agents
The present disclosure is concerned with benzo annulene compounds that are capable of inhibiting a viral infection and methods of treating viral infections...
2018/0230083 METHODS OF MANUFACTURING BENZOQUINOLINE COMPOUNDS
The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates...
2018/0230082 Crystalline Forms of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride
A hitherto unknown crystalline form of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the...
2018/0230081 PROCESS FOR PREPARING ISOPHORONE AMINO ALCOHOL (IPAA)
The present invention relates to an improved process for preparing 3-(aminomethyl)-3,5,5-trimethylcyclohexanol, called isophorone amino alcohol (IPAA)...
2018/0230080 ADENYLYL CYCLASE INHIBITORS FOR NEUROPATHIC AND INFLAMMATORY PAIN
The invention generally relates to adenylyl cyclase inhibitor compounds and methods for treating neuropathic or inflammatory pain by using those compounds.
2018/0230079 THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds having the general formula I: ##STR00001## and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n,...
2018/0230078 METHOD FOR PRODUCING HIGH-PURITY TEREPHTHALIC ACID
A method for producing high-purity terephthalic acid, comprising following steps (a) to (c): the step (a); obtaining crude terephthalic acid crystal by...
2018/0230077 METHOD AND APPARATUS FOR PRODUCING ACETIC ACID
A process for stably and safely producing acetic acid without increasing an internal pressure of a distillation column is provided. The process comprises (1) a...
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