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Patent # Description
2019/0002464 IMIDAZO[4,5-B]PYRIDIN-2-YL AMIDES AS KV7 CHANNEL ACTIVATORS
Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related...
2019/0002463 ANTI-PARASITIC COMPOUNDS AND USES THEREOF
The present disclosure provides compounds of Formula (I'), Formula (II), and Formula (III). The compounds described herein may useful in treating and/or...
2019/0002462 NOVEL PYRROLO[3,2-c]PYRIDINE-6-AMINO DERIVATIVES
The present invention relates to novel pyrrolo[3,2-c]pyridine-6-amino derivatives that inhibit the spindle checkpoint function of Monospindle 1 (Mps1--also...
2019/0002461 NOVEL POLYMORPH OF RIOCIGUAT AND ITS PROCESS FOR THE PREPARATION
The present invention relates to novel polymorph of riociguat and process for preparing the polymorph. The present invention also relates to the improved...
2019/0002460 SMALL MOLECULE INHIBITORS OF EGFR AND PI3K
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a pyrido-pyrimidin-amine...
2019/0002459 HYDROXYPHENYL PHENANTHROLINES AS POLYMERIZABLE BLOCKERS OF HIGH ENERGY LIGHT
Described are high energy light blocking compounds and ophthalmic devices containing the compounds. In particular, described are hydroxyphenyl phenanthroline...
2019/0002458 NOVEL DIHYDROPYRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF...
A compound according to Formula Ia: ##STR00001## wherein L.sub.1, G, and R.sup.1 are as described herein. The present invention relates to novel compounds according...
2019/0002457 SIGMA-2 RECEPTOR LIGAND DRUG CONJUGATES AS ANTITUMOR COMPOUNDS, METHODS OF SYNTHESIS AND USES THEREOF
Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding...
2019/0002456 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...
2019/0002455 KINASE INHIBITORS AND METHODS FOR MAKING AND USING
Disclosed embodiments concern kinase inhibitors, such as interleukin receptor associated kinases (IRAK) inhibitors, and compositions comprising such...
2019/0002454 NRF2 Regulators
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
2019/0002453 INHIBITORS OF BETA-HYDROXYLASE FOR TREATMENT OF CANCER
The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel ...
2019/0002452 FXR RECEPTOR MODULATOR, PREPARATION METHOD THEREFOR, AND USES THEREOF
Provided is a modulator of FXR receptor and preparation and use thereof, which relates to the technical filed of medicinal chemistry. The embodiment provides a...
2019/0002451 METHOD FOR PRODUCING BENZOXAZOLE COMPOUND
A compound represented by the formula (1) ##STR00001## having controlling effects on harmful organisms can be produced by cyclizing a compound represented by the...
2019/0002450 COMPOSITIONS FOR BINDING SPHINGOSINE-1-PHOSPHATE RECEPTOR 1 (S1P1), IMAGING OF S1P1, AND METHODS OF USE THEREOF
Among the various aspects of the present disclosure is the provision of a compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1,...
2019/0002449 CRYSTALLIZATION PROCEDURE FOR OBTAINING CANAGLIFLOZIN HEMIHYDRATE CRYSTALS
The present invention relates to an improved crystallization procedure to obtain canagliflozin hemihydrate crystals having a narrow particle size distribution...
2019/0002448 SUBSTITUTED BENZOFURANYL AND BENZOXAZOLYL COMPOUNDS AND USES THEREOF
The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by...
2019/0002447 BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN...
The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred...
2019/0002446 AGONISTS OF EPHA AND THEIR USES
A method of treating cancer in a subject includes administering to the subject a therapeutically effective amount of a small molecule agonist of EphA2 receptor...
2019/0002445 PROCESS FOR PREPARING LIFITEGRAST AND INTERMEDIATES THEREOF
The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses...
2019/0002444 CRYSTALLINE FORMS OF VILAZODONE HYDROCHLORIDE AND VILAZODONE FREE BASE
The present application relates to crystalline and amorphous Vilazodone hydrochloride. The present application further relates to amorphous solid dispersions...
2019/0002443 SUBSTITUTED AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to substituted amide derivatives having dual pharmacological activity towards both the sigma (.sigma.) receptor, and the...
2019/0002442 RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AS WELL AS PREPARATION...
The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation...
2019/0002441 6-HYDROXY-4-OXO-1,4-DIHYDROPYRIMIDINE-5-CARBOXAMIDES AS APJ AGONISTS
The present invention provides compounds of Formula (I): ##STR00001## wherein all variables are as defined in the specification, and compositions comprising any...
2019/0002440 VORICONAZOLE INTERMEDIATE AND VORICONAZOLE SYNTHESIS METHOD
Provided is a synthesis method for a voriconazole intermediate condensate as shown in formula II or an acid addition salt thereof. As shown in reaction formula...
2019/0002439 HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
The present invention provides, in part, compounds of Formula I: ##STR00001## and pharmaceutically acceptable salts thereof; processes for the preparation of;...
2019/0002438 INDANE DERIVATIVES AND THE USE THEREOF AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the...
2019/0002437 THERAPEUTIC INHIBITORY COMPOUNDS
Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma...
2019/0002436 RESPIRATORY SYNCYTIAL VIRUS INHIBITORS
Compounds of Formula (I): (Formula I), wherein Z.sup.1 is NR.sup.1A, CHR.sup.1A, CR.sup.1BR.sup.1B; one of Z.sup.2 and Z.sup.3 is CH or CR.sup.1A', the other...
2019/0002435 PROCESS FOR PREPARING AN ANTI-CANCER AGENT, ...
The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)meth- yl)cyclopropanamine...
2019/0002434 CRYSTALS OF QUINAZOLINE DERIVATIVE AND PREPARATION METHOD THEREFOR
The invention relates to Crystal form I, Crystal form II and Crystal form III of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]- ...
2019/0002433 Quinazoline Derivatives as VEGF Inhibitors
The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R' represents halogeno or C.sub.1-3alkyl; X.sup.1...
2019/0002432 PYRAZOLE DERIVATIVES
Provided herein are compounds of the formula I: as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the...
2019/0002431 SOMATOSTATIN MODULATORS AND USES THEREOF
Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such...
2019/0002430 LIQUID-CRYSTALLINE MEDIUM AND LIQUID-CRYSTAL DISPLAY COMPRISING THE SAME
The invention relates to a liquid-crystalline medium, preferably having a nematic phase and dielectric anisotropy of 0.5 or more, which comprises one or more...
2019/0002429 Derivatives of Xanthone Compounds
The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.
2019/0002428 PROCESS FOR THE PRODUCTION OF ALPHA-TOCOTRIENOL AND DERIVATIVES
The invention discloses novel processes for production, enrichment and/or isolation of alpha-tocotrienol from source material comprising at least one...
2019/0002427 STEREOISOMER OF FLOCOUMAFEN, COMPOSITION AND RODENTICIDE BAIT COMPRISING SAME, AND METHOD FOR CONTROLLING...
Disclosed is a configurational stereoisomer, referred to as enantiomer E.sub.4, of flocoumafen, the enantiomer E.sub.4 having, as determined by the...
2019/0002426 Small Molecule Lipid II Inhibitors
Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and...
2019/0002425 C-Glucoside Derivative Containing Fused Phenyl Ring or Pharmaceutically Acceptable Salt Thereof, Process for...
The present disclosure relates to C-glycoside derivatives having a fused phenyl ring or pharmaceutical acceptable salts thereof, a method for preparing the...
2019/0002424 PREPARATION OF 3-HYDROXY-3,6-DIMETHYLHEXAHYDROBENZOFURAN-2-ONE AND DERIVATIVES THEREOF
The present invention relates to the synthesis of intermediate compounds which can be used in the synthesis of mint lactone and related compounds, including...
2019/0002423 HIGHLY PURIFID PHARMACEUTICAL GRADE TASIMELTEON
A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP...
2019/0002422 PROCESS FOR THE EPOXIDATION OF PROPENE TO PROPYLENE OXIDE
A continuous process for the preparation of propylene oxide, comprising providing a liquid feed stream comprising propene, hydrogen peroxide, methanol, water,...
2019/0002421 PROCESS AND NOVEL POLYMORPHIC FORM OF VORTIOXETINE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is...
2019/0002420 PROCESS AND INTERMEDIATES FOR PREPARATION OF THIAZINE DERIVATIVES
The present invention provides a process for preparation of the compound of formula (VI), wherein each symbol is as defined in the specification, without using...
2019/0002419 PROCESS FOR PREPARING 1,1,3-TRIOXO-1,2-BENZOTHIAZOLE-6-CARBOXAMIDE
A process for preparing, 1,1,3-Trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: reacting 2-chloro-sulfonyl-terephthalic acid dialkyl ester of...
2019/0002418 ADENYLYL CYCLASE INHIBITORS FOR CHRONIC PAIN AND OPIOID DEPENDENCE
This present application disclosed a series of selective adenylyl cyclase 1 (AC1) inhibitors as a pain therapeutic. Those compounds may provide an effective...
2019/0002417 MATERIALS FOR ELECTRONIC DEVICES
The present invention relates to compounds according to formula (I), which are suitable for use in electronic devices, preferably organic electroluminescent...
2019/0002416 CRYSTALLINE(2S,4R)-5-(5'-CHLORO-2'-FLUORO-[1,1'-BIPHENY]-4-YL)-2-(ETHOXYME- ...
In one aspect, the invention relates to a crystalline form of the structure: ##STR00001## or a pharmaceutically acceptable salt thereof, having neprilysin ...
2019/0002415 HYDROXYPHENYL NAPHTHOTRIAZOLES AS POLYMERIZABLE BLOCKERS OF HIGH ENERGY LIGHT
Described are high energy light blocking compounds and ophthalmic devices containing the compounds. In particular, described are hydroxyphenyl naphthotriazole...
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