07th week of 2016 patent applcation highlights part 18 |
Patent application number | Title | Published |
20160046561 | SUBSTITUTED TETRACYCLINE COMPOUNDS - The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms. | 2016-02-18 |
20160046562 | Styrenated Phenol Compound and Method of Preparing the Same - Provided is a styrenated phenol compound represented by Formula 1 in which styrenated phenol and hydroxylamine bind to each other: | 2016-02-18 |
20160046563 | SYNTHETIC BUILDING BLOCKS FOR THE PRODUCTION OF MATERIALS FOR ORGANIC ELECTROLUMINESCENCE DEVICES - The present invention relates to compounds which are suitable as synthesis precursors for the production of electronically active materials for use in organic electroluminescence devices. | 2016-02-18 |
20160046564 | AMIDINE COMPOUND AND USE THEREOF - An amidine compound represented by formula (1) | 2016-02-18 |
20160046565 | XYLYLENE DICARBAMATE, METHOD FOR PRODUCING XYLYLENE DIISOCYANATE, XYLYLENE DIISOCYANATE, AND METHOD FOR RESERVING XYLYLENE DICARBAMATE - Xylylene dicarbamate contains impurities represented by formulas (1) to (4) below at a ratio of less than 100 ppm as a total amount thereof on a mass basis. | 2016-02-18 |
20160046566 | DIARYLIODONIUM SALT - Provided is a compound that allows easy introduction of a pentafluorosulfanylaryl group into a compound of interest. | 2016-02-18 |
20160046567 | PROCESS FOR TREATING BIOMASS TO PRODUCE MATERIALS USEFUL FOR BIOFUELS - Since biomass is always accompanied by caustic inorganic materials, we have found that the formation of the anion salt of α-hydroxysulfonic acid represent the largest “loss” of the α-hydroxysulfonic acid in the potential reversible acid pretreatment process. By titrating the α-hydroxysulfonic acid salt with strong mineral acid and then reverting the alfa-hydroxysulfonic acid as its primary components, the acid components can be recovered substantially quantitatively. | 2016-02-18 |
20160046568 | DICARBOXYLIC ACID COMPOUND - It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. Solution: A compound represented by a general formula (I) or a pharmacologically acceptable salt thereof. [In the formula, R | 2016-02-18 |
20160046569 | N-HYDROXYMETHANESULFONAMIDE NITROXYL DONORS - The disclosed subject matter provides N-hydroxymethanesulfonamide compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure. | 2016-02-18 |
20160046570 | N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES - The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. | 2016-02-18 |
20160046571 | METHOD FOR THE PREPARATION OF (3S,3S') 4,4'-DISULFANEDIYLBIS (3-AMINOBUTANE 1-SULFONIC ACID) - The present invention relates to a new method for the preparation of (3S,3S′) 4,4′-disulfanediylbis(3-aminobutane 1-sulfonic acid) in five steps from (S)-ethyl 2-(benzyloxycarbonylamino)-4-(neopentyloxysulfonyl)butanoate A. | 2016-02-18 |
20160046572 | Process for Preparing Sulfimines and Their in-situ Conversion into N-(1-Amino-Benzoyl)-Sulfimines - The present invention relates to a process for preparing a compound of the formulae (Ia) or (Ib), or a mixture thereof, | 2016-02-18 |
20160046573 | IDENTIFYING PATIENT RESPONSE TO S1P RECEPTOR MODULATOR ADMINISTRATION - The invention provides a method of assessing the appropriate therapeutic dose of 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid to administer to a patient in need thereof. It is determined whether a patient has a particular metabolizer genotype. If the patient does not have a particular genotype, 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof is administered at a standard dose. If the patient has the poor metaboliser genotype, either 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, is administered at a dose below that of the standard therapeutic dose; or is not dosed at all. | 2016-02-18 |
20160046574 | SEROTONIN RECEPTOR MODULATORS - Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. | 2016-02-18 |
20160046575 | Novel Forms of [R-(R*,R*)]-2-(4-Fluorophenyl)-Beta, Gamma-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-[(Phenylamino)carbonyl]-1H-P- yrrole-1-Heptanoic Acid Calcium Salt (2:1) - Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease. | 2016-02-18 |
20160046576 | NOVEL PYRROLE DERIVATIVES - There are provided inter alia compounds of formula (I) | 2016-02-18 |
20160046577 | N-Haloalkylindoline Intermediates, Their Process And Use In Preparation of Silodosin And its Derivatives - The present invention provides novel indoline compounds, derivatives of Formula 1 and salts thereof; which can be effectively used for the preparation of a1-adrenoceptor antagonists, Silodosin and its pharmaceutically acceptable salts. | 2016-02-18 |
20160046578 | INHIBITORS OF PRMT5 AND METHODS OF THEIR USE - In one aspect, the invention relates to PRMT5 inhibitors, including optionally substituted N-alkyl-9H-carbazole analogs, derivatives thereof, and related compounds; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation and benign hematologic diseases using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2016-02-18 |
20160046579 | THERAPEUTIC COMPOUNDS AND COMPOSITIONS - Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases. | 2016-02-18 |
20160046580 | METHODS OF PRODUCING SULFILIMINE COMPOUNDS - Methods of producing a sulfilimine compound, such as N-cyano-S-methyl-S-[1-(6-trifluoromethyl-3-pyridinyl)ethyl]sulfilimine or other substituted sulfilimine compound. The method includes combining a sulfide compound, cyanamide, a hypochlorite compound, and a base, and oxidizing the sulfide compound to form the sulfilimine compound. The sulfide compound may include a 2-trifluoromethyl-5-(1-substituted)alkyl-thiopyridine compound. The base may include sodium hydroxide. A buffer, such as a phosphate buffer, may, optionally, be used in the reaction. | 2016-02-18 |
20160046581 | Factor XIa Inhibitors - The present invention provides a compound of Formula (I) | 2016-02-18 |
20160046582 | CRYSTALS OF LAQUINIMOD SODIUM AND IMPROVED PROCESS FOR THE MANUFACTURE THEREOF - The subject invention provides a mixture of Crystalline Laquinimod sodium particles, wherein (i) ≧90% of the total amount by volume of the laquinimod sodium particles have a size of ≦40 μm or (ii) ≧50% of the total amount by volume of the laquinimod sodium particles have a size of ≦15 μm and wherein: a) the mixture has a bulk density of 0.2-0.4 g/mL; b) the mixture has a tapped density of 0.40-0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 20 ppm relative to the amount by weight of laquinimod sodium; d) an amount of MCQ in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of MCQCA in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; or f) an amount of MCQME in the mixture is no more than 0.12% relative to the amount of laquinimod sodium as measured by HPLC. The subject invention also provides a pharmaceutical composition comprising an amount of laquinimod and at least one of BH-3-HKAQ, MCQ, MCQCA, MCQME, NEA, and MCQEE. The subject invention also provides processes for preparing BH-3-HLAQ, MCQ, MCQCA, MCQEE, and compounds prepared by said processes. Further provided is a process for testing whether a sample of laquinimod contains an undesirable impurity. Further provided is a process for preparing a validated pharmaceutical composition comprising laquinimod, for preparing a pharmaceutical composition comprising laquinimod, or for distributing a validated batch of a pharmaceutical composition comprising laquinimod, for validating a batch of a pharmaceutical product containing laquinimod and a pharmaceutically acceptable carrier for distribution, and for preparing a packaged pharmaceutical composition comprising laquinimod, each comprising determining the amount of at least one of BH-3-HLAO, MCQ, MCQCA, MCQME2016-02-18 | |
20160046583 | ISOQUINOLINE DERIVATIVES - The present invention relates to the use of compounds of general formula | 2016-02-18 |
20160046584 | COMPOSITIONS AND METHODS OF USING THE COMPOSITIONS FOR PLAQUE SOFTENING - Disclosed herein is a compound for use in a composition applied to a blood vessel, wherein the compound softens and/or disrupts the crystalline matrix of calcified plaque. Methods of treatment comprising applying the disclosed composition are also disclosed. Plaque-softening compounds are also disclosed. | 2016-02-18 |
20160046585 | HALOGENOPYRAZOLES AS INHIBITORS OF THROMBIN - There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin. | 2016-02-18 |
20160046586 | SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS - In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2016-02-18 |
20160046587 | PREPARATION AND METHOD FOR USE IN THE TREATMENT OF RESPIRATORY DISEASES - The present disclosure relates to a novel active compound having the formula Ia: | 2016-02-18 |
20160046588 | METHOD FOR OBTAINING SOLUTIONS OF OTA IN A CONCENTRATED SULFURIC ACID MEDIUM; SAID SOLUTIONS; AND METHOD FOR PREPARING ONTA - A method for obtaining solutions that contain 1,2,4-triazole-5-one (OTA) in concentrated sulphuric acid, includes using 3-amino-1,2,4-triazole (ATA) as a precursor of OTA. There is also provided a method for preparing 3-nitro-1,2,4-triazole-5-one (4) (ONTA) from the solutions. | 2016-02-18 |
20160046589 | Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases - The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R | 2016-02-18 |
20160046590 | SONIC HEDGEHOG MODULATORS - Sonic Hedgehog modulators and methods of use thereof are provided for. | 2016-02-18 |
20160046591 | INHIBITION OF IL-2 PRODUCTION - An object is to find a substance which inhibits IL-2 production.
| 2016-02-18 |
20160046592 | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DIABETES - An object is to provide a novel compound which has a glycogen synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. Provided is a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: | 2016-02-18 |
20160046593 | Preparation of Ambrox from Labdanes of Dysoxylum hongkongense, and the Preparation of New Diterpenoids from Dysoxylum hongkongense - The present invention discloses eight new diterpenoids, i.e. Dysongensins A to H, extracted from the leaves and twigs of | 2016-02-18 |
20160046594 | Anticancer Miliusane Derivatives - The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer agents based on miliusane compounds. The present invention also includes its preparation and application method for treating cancer. | 2016-02-18 |
20160046595 | PHENYL C-GLUCOSIDE DERIVATIVE CONTAINING DEOXYGLUCOSE STRUCTURE, PREPARATION METHOD AND USE THEREOF - The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R | 2016-02-18 |
20160046596 | INHIBITORS OF THE KYNURENINE PATHWAY - The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase. | 2016-02-18 |
20160046597 | RORC2 INHIBITORS AND METHODS OF USE THEREOF - The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions. | 2016-02-18 |
20160046598 | Glutarimide Derivatives, Use Thereof, Pharmaceutical Composition Based Thereon and Methods for Producing Glutarimide Derivatives - The present invention relates to novel biologically active glutarimide derivatives of general formula I or pharmaceutically acceptable salts thereof, their use as an agent for the treatment of upper respiratory tract diseases, pharmaceutical compositions comprising the glutarimide derivatives of general formula I, methods for preparing the glutarimide derivatives of general formula I by heating a dicarboxylic acid monoamide of general formula II with a dehydrating agent. | 2016-02-18 |
20160046599 | SUBSTITUTED PIPERIDINE COMPOUNDS AND THEIR USE AS OREXIN RECEPTOR MODULATORS - The present invention is directed to compounds of Formula I: wherein X is CR | 2016-02-18 |
20160046600 | 1,2,5-SUBSTITUTED BENZIMIDAZOLES AS FLAP MODULATORS - The present invention relates to compounds of Formula (I), | 2016-02-18 |
20160046601 | HETEROCYCLIC COMPOUND AND USE THEREOF - Compounds represented by the formulas | 2016-02-18 |
20160046602 | INHIBITORS OF C-FMS KINASE - The invention is directed to compounds of Formula I: | 2016-02-18 |
20160046603 | Crystalline Forms of D-Glucitol, 1-Deoxy-1-(Methylamino)-, 1-(6-Amino-3,5-Difluoropyridine-2-Yl)-8-Chloro-6-Fluoro-1,4-Dihydro-7-(3-- Hydroxyazetidin-1-Yl)-4-Oxo-3-Quinolinecarboxylate - The present disclosure relates generally to crystalline forms of anhydrous D-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1- yl)-4-oxo-3-quinolinecarboyxlate, compositions comprising the same, and methods of making the same. Delafloxacin is an fluoroquinolone antibiotic with the chemical structure and the chemical name 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboyxlate. Studies have indicated the existence of three anhydrous polymorphs of delafloxacin, as well as a trihydrate and methanol and ethanol solvates. | 2016-02-18 |
20160046604 | HETEROARYL SUBSTITUTED INDAZOLES - Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 2016-02-18 |
20160046605 | PROTEIN KINASE C INHIBITORS AND METHODS OF THEIR USE - PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity. | 2016-02-18 |
20160046606 | CXCR4 Receptor Antagonists - The compounds of formula (I) are antagonists of the CXCR4 receptor | 2016-02-18 |
20160046607 | METHOD FOR PRODUCING SUBSTITUTED ANTHRANILIC ACID DERIVATIVES - The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) | 2016-02-18 |
20160046608 | C-Linked Heterocycloaklyl Substituted Pyrimidines and their uses - The present invention provides for pyrimidine compounds of Formula I-I and embodiments thereof | 2016-02-18 |
20160046609 | SYNTHESIS AND NOVEL SALT FORMS OF (R)-5-((E)-2-PYRROLIDIN-3YLVINYL)PYRIMIDINE - The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts. | 2016-02-18 |
20160046610 | 3-HETEROARYL SUBSTITUTED INDAZOLES - Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 2016-02-18 |
20160046611 | NOVEL CHROMONE ALKALOID DYSOLINE FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISORDERS - The present invention relates to novel chromone alkaloid of formula 1 isolated from the plant | 2016-02-18 |
20160046612 | Heterocyclic Derivative and Pharmaceutical Drug - The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: | 2016-02-18 |
20160046613 | 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 for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 2016-02-18 |
20160046614 | AUTOTAXIN INHIBITOR COMPOUNDS - Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity. | 2016-02-18 |
20160046615 | Novel Crystal Form of Dabrafenib Mesylate and Preparation Method Thereof - Disclosed are a novel crystal form of Dabrafenib mesylate and preparation method thereof. The novel crystal form of the present invention is more stable in water or an aqueous system, and has greater solubility and dissolution in water, thus having better stability and bioavailability compared with the existing crystal forms. | 2016-02-18 |
20160046616 | NRF2 SMALL MOLECULE INHIBITORS FOR CANCER THERAPY - Small molecule inhibitors of Nrf2 and methods of their use are provided for treating or preventing a disease, disorder or condition associated with an Nrf2-regulated pathway. The compound can be administered as a single agent or can be administered to enhance the efficacy of a chemotherapeutic drug and/or radiation therapy. | 2016-02-18 |
20160046617 | SODIUM CHANNEL MODULATORS FOR THE TREATMENT OF PAIN - Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I: | 2016-02-18 |
20160046618 | Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: | 2016-02-18 |
20160046619 | IMIDAZOLIDINONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Described are compounds of Formula I | 2016-02-18 |
20160046620 | METHODS OF CONTROLLING NEONICOTINOID RESISTANT PESTS - The invention relates to a method of controlling insects (in particular insects of the order Hemiptera, especially aphids and whitefly) that are resistant to neonicotinoid insecticides, to methods of controlling insects whereby undesired insects are affected but beneficial arthropods are not affected, using compounds of formula I (where A and R1 are as defined above) and, further, to novel compounds of formula I which are useful in the aforementioned methods and/or which possess enhanced insecticidal properties, and to compositions containing said compounds. | 2016-02-18 |
20160046621 | INDOLOACRIDINE-CONTAINING DERIVATIVE, PREPARATION PROCESS AND USE THEREOF, AND ORGANIC LUMINESCENT DEVICE - The disclosure provides an indoloacridine-containing derivative represented by formula (I), wherein A is a group represented by formula (II), and wherein X, Y, Z and W represent a carbon atom or a nitrogen atom, and at least one of W, X, Y and Z represent a nitrogen atom; R represents a phenyl group, a biphenylyl group, a naphthyl group or a phenanthryl group. The disclosure further provides a process for preparing the compound. The disclosure further provides an organic electroluminescent device comprising the compound. This compound can be used as a phosphorescence host material, a hole-injecting material or a hole-transporting material in an organic electroluminescent device. | 2016-02-18 |
20160046622 | IMIDAZO[4,5-C]PYRIDINE AND PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS SSAO INHIBITORS - The compounds of formula (I) are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumour growth. | 2016-02-18 |
20160046623 | SALT OF PYRAZOLOQUINOLINE DERIVATIVE, AND CRYSTAL THEREOF - The present invention provides a salt of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, malonic acid, maleic acid, tartaric acid, methanesulfonic acid, benzenesulfonic acid and toluenesulfonic acid; or a crystal thereof with a potential to be used as drug substance in pharmaceuticals. | 2016-02-18 |
20160046624 | PYRIDO[2,3-d]PYRIMIDINE-2,4(1H,3H)-DIONE DERIVATIVES - This invention relates to novel Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione derivatives of Formula (I): | 2016-02-18 |
20160046625 | BENZIMIDAZOLE AND AZABENZIMIDAZOLE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE - Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein. | 2016-02-18 |
20160046626 | BICYCLIC SULFONAMIDE COMPOUNDS AS SODIUM CHANNEL INHIBITORS - The present invention provides compounds of Formula I, | 2016-02-18 |
20160046627 | ITK and JAK Kinase Inhibitors - The present invention relates to compounds described by Formula I: | 2016-02-18 |
20160046628 | Pd-CATALYZED COUPLING OF PYRAZOLE AMIDES - A novel process for the preparation of imidazo[1,2-a]pyridine compounds of the formula | 2016-02-18 |
20160046629 | SYNTHESIS OF AUTOPHAGY INDUCING COMPOUND AND THE USES THEREOF - The present invention relates to a composition comprising compound of formula CB6 or CB8, | 2016-02-18 |
20160046630 | PERIPHERALLY RESTRICTED DIPHENYL PURINE DERIVATIVES - The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: | 2016-02-18 |
20160046631 | PURINE DERIVATIVES AS CB2 RECEPTOR AGONISTS - The invention relates to a compound of formula (I) | 2016-02-18 |
20160046632 | OCTAHYDROPYRROLOPYRROLES THEIR PREPARATION AND USE - The present invention provides compounds comprising variously substituted octahydropyrrolopyrroles, their synthesis, methods of making, methods of using, compositions and formulations thereof. | 2016-02-18 |
20160046633 | BMP INHIBITORS AND METHODS OF USE THEREOF - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia. | 2016-02-18 |
20160046634 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas. | 2016-02-18 |
20160046635 | NOVEL BREATHING CONTROL MODULATING COMPOUNDS, AND METHODS OF USING SAME - The present invention includes pyrimido[5,4-d]pyrimidines that are useful in the prevention and/or treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of preventing and/or treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of at least one compound of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of at least one compound of the invention. | 2016-02-18 |
20160046636 | TYPE II RAF KINASE INHIBITORS - The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions. | 2016-02-18 |
20160046637 | PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AS CB2 RECEPTOR AGONISTS - The invention relates to a compound of formula (I) | 2016-02-18 |
20160046638 | CERTAIN PROTEIN KINASE INHIBITORS - Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof. | 2016-02-18 |
20160046639 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS - The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R | 2016-02-18 |
20160046640 | SUBSTITUTED 7-AZABICYCLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS - The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphihalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyi, tlisazolyl, isoxazolvl, pyrazolyl, imidazothiazolyi, benzimidazolyl, or indazolyi; R | 2016-02-18 |
20160046641 | SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND PHARMACEUTICAL USE OF SAME AS HIV INTEGRASE INHIBITOR - [Problem] Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent. | 2016-02-18 |
20160046642 | Compounds for Treating Respiratory Syncytial Virus Infections - The present invention relates to compounds of formula (I) | 2016-02-18 |
20160046643 | HIGHLY EFFICIENT POLARIZING AGENTS FOR DYNAMIC NUCLEAR POLARIZATION - The invention relates to compounds of general formula (I) wherein X is C═O or SO | 2016-02-18 |
20160046644 | Method for Preparing a Pyripyropene Compound - The present invention relates to a method for preparing the pyripyropene compound of the formula (I) which method comprises the following steps: i) subjecting a pyripyropene compound of formula Pyripyropene A to an alkaline hydrolysis to yield a 1,7,11-trideacetylpyripyropene A, ii) reacting 1,7,11-trideacetylpyripyropene A obtained in step i) with cyclopropane carbonyl chloride to yield a raw product containing the pyripyropene compound of formula (I); iii) subjecting the raw product of step ii) to crystallization to yield a crystalline pyripyropene compound of formula (I) and a mother liquor; and iv) recycling the mother liquor or a pyripyropene compound containing fraction thereof to the alkaline hydrolysis of step i). | 2016-02-18 |
20160046645 | Production of Pyripyropenes from Dry Biomass - The invention pertains to processes to produce dry biomass of pyripyropene producer organisms, processes to obtain pyripyropenes from such dry biomass, as well as to processes to produce compounds of Formula III and/or Formula IV and/or Formula V from the pyripyropenes obtained from the dry biomass. The invention does further pertain to the dry biomass itself, as well as processes using said dry biomass to obtain pyripyropenes for the production of compounds of Formula III and/or Formula IV and/or Formula V, including processes using said dry biomass to obtain pyripyropenes or compounds of Formula III and/or Formula IV and/or Formula V in order to produce pest control compositions, in particular insecticides, comprising such compounds. | 2016-02-18 |
20160046646 | METHODS FOR PREPARING SGLT2 INHIBITORS - This invention relates to methods for preparing a sodium-glucose transporter 2 (SGLT2) inhibitor, a cocrytalline SGLT2 and (S)-5-oxopyrrolidine-2-carboxylic acid (L-PGA) complex, and intermediates useful in the preparation of the said SGLT2 inhibitor. | 2016-02-18 |
20160046647 | COMPOSITIONS COMPRISING THIENOPYRIMIDINE AND THIENOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine and thienopyridine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin). | 2016-02-18 |
20160046648 | 4-PHENYLPIPERIDINES, THEIR PREPARATION AND USE - The present invention provides a compound having the structure: (structurally represented) wherein R | 2016-02-18 |
20160046649 | N-ALKYL-2-PHENOXYETHANAMINES, THEIR PREPARATION AND USE - The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is alkyl; A is absent or present, and when present is —C(O)— or —C(O)NH—; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is —C(O)—, or a pharmaceutically acceptable salt thereof. | 2016-02-18 |
20160046650 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 2016-02-18 |
20160046651 | TREATMENT OF MALARIA USING INHIBITORS OF THE ISPD ENZYME IN THE NON-MEVALONATE PATHWAY - Compounds are disclosed that inhibit the methylerythritol cytidyltransferase (IspD) enzyme in the non-mevalonate pathway (MEP pathway), which is present in many organisms including the | 2016-02-18 |
20160046652 | Organoboron Compounds and Methods of Making Same - The invention provides organoboron precursors and facile photoirradiation and/or heating methods of making corresponding elimination products. Some elimination products are polycyclic aromatic molecules wherein a number of aromatic C—C moieties have been replaced by a B—N moiety to form azaborine compounds with interesting properties such as electronic, photophysical, luminescent, as well as chemical properties. Examples of polymer films that were doped with such compounds are shown wherein irradiated portions of the polymer film luminesce. The invention further provides methods of producing photoluminescence and electroluminescence, and uses of the compounds of the invention in luminescent probes, sensors, electroluminescent devices, hydrogen storage materials, optoelectronic materials, and bioactive molecules. | 2016-02-18 |
20160046653 | SILYLATION OF AROMATIC HETEROCYCLES BY EARTH ABUNDANT TRANSITION-METAL-FREE CATALYSTS - The present invention describes chemical systems and methods for silylating aromatic organic substrates, said system or method comprising or consisting essentially of a mixture of (a) at least one organosilane and (b) at least one strong base, the definition of strong base now also including hydroxide, especially KOH, said system being preferably, but not necessarily substantially free of a transition-metal compound, and said methods comprising contacting a quantity of the organic substrate with a mixture of (a) at least one organosilane and (b) at least one strong base, under conditions sufficient to silylate the aromatic substrate; wherein said system is substantially free of a transition-metal compound. | 2016-02-18 |
20160046654 | Prodrugs Of Bicyclic Substituted Pyrimidine Type PDE-5 Inhibitors - Provided are prodrugs of a bicyclic substituted pyrimidine type PDE-5 inhibitors, pharmaceutically acceptable salts or stereoisomers thereof. Also provided are methods for preparing these prodrug compounds, pharmaceutical preparations, and pharmaceutical compositions, as well as a use of these compounds, pharmaceutical preparations and pharmaceutical compositions in the manufacture of medicaments for treatment and/or prophylaxis of sexual dysfunction and lower urinary tract symptoms. | 2016-02-18 |
20160046655 | NOVEL PROCESS FOR PREPARING CEFTAROLINE FOSAMIL - The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process. | 2016-02-18 |
20160046656 | NOVEL PHYTOSPHINGOSINE-1-PHOSPHATE DERIVATIVE, PREPARATION METHOD THEREFOR, AND COMPOSITION FOR PREVENTING AND TREATING HAIR LOSS OR FOR GROWING HAIR COMPRISING SAME - The present invention provides: O-cyclic phytospingosine-1-phosphate (0-C-P1P), N-cyclic phytospingosine-1-phosphate (N-C-P1P), a pharmaceutically acceptable salt thereof, or a solvate thereof; a preparation method therefor; a cosmetic composition comprising the same for preventing hair loss or for growing hair; and a pharmaceutical composition for preventing and treating hair loss or for growing hair. | 2016-02-18 |
20160046657 | ORGANOPALLADIUM COMPOUNDS AS POLYMERIZATION CATALYSTS - A series of bicycloalkene-palladium compounds having utility as addition polymerization catalysts are disclosed. Also disclosed are the methods of making these compounds. | 2016-02-18 |
20160046658 | PROCESS FOR THE DIASTEREOSELECTIVE PREPARATION OF RUTHENIUM COMPLEXES - The present invention relates to a process for the preparation of a compound of formula (I), wherein X is —CH | 2016-02-18 |
20160046659 | DEVICE FOR PURIFYING NUCLEIC ACIDS - The invention relates to a device ( | 2016-02-18 |
20160046660 | CONVERGENT PROCESSES FOR PREPARING MACROLIDE ANTIBACTERIAL AGENTS - The invention described herein relates to processes for preparing ketolide antibacterial agents. In particular, the invention relates to intermediates and processes for preparing ketolides that include a 1,2,3-triazole substituted side chain. | 2016-02-18 |