43rd week of 2017 patent applcation highlights part 25 |
Patent application number | Title | Published |
20170305870 | METHOD FOR PRODUCING 3-CHLORO-2-HYDROXYPROPYL (METH)ACRYLATE AND METHOD FOR PRODUCING GLYCIDYL (METH)ACRYLATE - To reduce formation of side products and to enhance a selectivity rate in a method for producing 3-chloro-2-hydroxypropyl (meth)acrylate and in a method for producing glycidyl (meth)acrylate. | 2017-10-26 |
20170305871 | LONG-CHAINED MONO AND DI-ESTERS OF 2,5-DI(HYDROXYMETHYL)TETRAHYDROFURAN, USE AND PRODUCTION THEREOF - The present invention relates to novel mono- and diesters of 2,5-di(hydroxymethyl)tetrahydrofuran, processes for their preparation by esterification in the presence of tertiary amines or in the presence of enzymatic esterification catalysts and the use of these mono- and diesters as interface-active compounds, rheology modifiers and emollients. The invention further relates to cosmetic and pharmaceutical compositions, and to detergents, cleaners and dishwashing compositions which comprise these mono- and diesters of 2,5-di(hydroxymethyl)-tetrahydrofuran. | 2017-10-26 |
20170305872 | IMPROVED 5-HYDROXYMETHYLFURFURAL PRODUCTION USING A MULTI-FLUORINATED ALCOHOL COMPOUND - The present invention relates to a process for producing a water cleavage product, a water cleavage product thus produced, a process for producing at least one water cleavage secondary product, a water cleavage secondary product thus produced and the use of a multi-fluorinated alcohol compound for the extraction of at least one water cleavage product from an aqueous phase. | 2017-10-26 |
20170305873 | FORMATION OF 2,5-FURAN DICARBOXYLIC ACID FROM ALDARIC ACIDS - The disclosure relates to a method for forming 2,5-furan dicarboxylic acid (FDCA) from aldaric acids. The aldaric acids are dehydrating and cyclizing via acid catalysis to form the FDCA product. Aldaric acids such as galactaric acid, gularic acid, mannaric acid, and glucaric acid can be used in the disclosed method, and the aldaric acids can be obtained from form renewable biomass sources which contain pectin, alginate, and/or other biomass carbohydrates. The FDCA can be used as a renewable feedstock for consumer product polymeric materials such as polyalkylene furoate polymers. | 2017-10-26 |
20170305874 | Diastereoselective Synthesis of (.+-.)-Epianastrephin, (.+-.)-Anastrephin and Analogs Thereof - A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R | 2017-10-26 |
20170305875 | 2-(ALKOXY OR ARYLOXY CARBONYL)-4-METHYL-6-(2,6,6-TRIMETHYLCYCLOHEX-1- ENYL)HEX-2-ENOIC ACID COMPOUNDS, ITS PREPARATION AND USE - Compounds of the formula 1 | 2017-10-26 |
20170305876 | 7,8-DIHYDOXYFLAVONE AND 7,8-SUBSTITUTED FLAVONE DERIVATIVES, COMPOSITIONS, AND METHODS RELATED THERETO - In certain embodiments, the disclosure relates to 7,8-dihydoxyflavone and 7,8-substituted flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diseases or conditions related to | 2017-10-26 |
20170305877 | Processes for the Preparation of Rotigotine and Intermediates Thereof - The present invention provides processes for the preparation of a compound of Formula 2 or a salt thereof, wherein R | 2017-10-26 |
20170305878 | sGC STIMULATORS - Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed. | 2017-10-26 |
20170305879 | PROCESS FOR THE PREPARATION OF 3-SUBSTITUTED (INDOL-1-YL)-ACETIC ACID ESTERS - The invention relates to an industrial scale process for the preparation of a compound of general formula (I): (Formula (I)) wherein R | 2017-10-26 |
20170305880 | SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): | 2017-10-26 |
20170305881 | NON-PLATINUM METAL COMPLEXES FOR EXCIMER BASED SINGLE DOPANT WHITE ORGANIC LIGHT EMITTING DIODES - Complexes and devices, such as organic light emitting devices and full color displays, including a compound of the formula wherein: M is Pd | 2017-10-26 |
20170305882 | BENZYL SUBSTITUTED INDAZOLES AS BUB1 KINASE INHIBITORS - Compounds of formula (I) and their use as pharmaceuticals. | 2017-10-26 |
20170305883 | Compositions and Methods for Inhibiting BMP - The present invention provides small molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions 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 and compositions 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. | 2017-10-26 |
20170305884 | PREPARATION METHOD FOR BEMACICLB - Disclosed are an intermediate of bemaciclib or abemaciclib and a preparation method therefor. The preparation method comprises condensation, amidine reaction, cyclization and other unit reactions. Serving the intermediate of bemaciclib as a raw material, bemaciclib is obtained through the guanidination reaction and the cyclization reaction. According to the preparation method, the raw material is easily available, the procedure is simple, and the preparation method is economical, environmentally friendly and suitable for industrial production. | 2017-10-26 |
20170305885 | THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE - Provided are compounds useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof a compound described herein. | 2017-10-26 |
20170305886 | PLANT GROWTH-PROMOTION AGENT AND METHOD FOR PROMOTING PLANT GROWTH - The present invention concerns: a plant growth-promoting agent comprising a compound represented by Formula (I) or a salt thereof: | 2017-10-26 |
20170305887 | ANTI-ENDOTHELIAL LIPASE COMPOUNDS AND METHODS OF USING THE SAME IN THE TREATMENT AND/OR PREVENTION OF CARDIOVASCULAR DISEASES - Endothelial Lipase (EL) inhibitors and methods of using such inhibitors for treating conditions implicating EL are provided herein. The present invention meets the needs in the field by providing small molecule inhibitors of EL function that can be used therapeutically to raise HDL cholesterol levels in blood, and can be used in the prevention and/or treatment of cholesterol and lipoprotein metabolism disorders, including, but not limited to, familial hypercholesterolemia, atherogenic dyslipidemia, atherosclerosis, and, more generally, cardiovascular disease (CVD). | 2017-10-26 |
20170305888 | 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 compositions. The pharmaceutical compositions are useful for reducing intraocular pressure in animals of the mammalian species. | 2017-10-26 |
20170305889 | METHODS OF TREATING CANCER - The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 2017-10-26 |
20170305890 | METHODS OF TREATING CANCER - The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 2017-10-26 |
20170305891 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN - The present invention provides for compounds of formula (I) | 2017-10-26 |
20170305892 | NOVEL AMINOPYRIDINE COMPOUNDS USEFUL AS INHIBITORS OF PROTEIN PRENYLATION - A compound for use in the treatment and/or prevention of diseases or disorders wherein an inhibition of protein prenylation is required, which is alternatively chosen among | 2017-10-26 |
20170305893 | HETEROCYCLIC COMPOUNDS AS DCTPP1 MODULATORS - The invention relates to compounds of formula I, or a pharmaceutically-acceptable salt thereof. The present invention also relates to pharmaceutical formulations comprising these compounds, and to their use as medicaments for the treatment of disorders where modulation of DCTPP (deoxycytidine triphosphate pyrophosphatase 1) activity exerts a therapeutic effect. | 2017-10-26 |
20170305894 | PPAR AGONISTS, COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Provided herein are compounds of Formula (I) and compositions useful in increasing PPARS activity. The compounds and compositions provided herein are useful for the treatment of PPARS related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases). | 2017-10-26 |
20170305895 | SUBSTITUTED AMINOTHIAZOLES FOR THE TREATMENT OF TUBERCULOSIS - Disclosed ore substituted aminothiazoles, which can be used for, among other things, the treatment of tuberculosis, pharmaceutical compositions containing the same, and methods of using the same. | 2017-10-26 |
20170305896 | PYRIMIDINONE COMPOUND - A pyrimidinone compound represented by formula (1): | 2017-10-26 |
20170305897 | BENZIMIDAZOLE-PROLINE DERIVATIVES - The present invention relates to compounds of the formula (II) | 2017-10-26 |
20170305898 | Composition and Method for Treating Metabolic Disorders - Bromocriptine citrate administered to a vertebrate, animal or human, can be used for any purpose including, e.g., the long-term modification and regulation of metabolic disorders, including prediabetes, obesity, insulin resistance, hyperinsulinemia, hyperglycemia and type 2 diabetes mellitus (T2DM) and/or, e.g., the treatment of other medical disorder(s) including immune or endocrine disorders or diseases. Bromocriptine citrate is administered over a limited or extended period at a time of day dependent on re-establishing the normal circadian rhythm of central dopaminergic activity of healthy members of a similar species and sex. Insulin resistance, hyperinsulinemia and hyperglycemia, T2DM, prediabetes, MS or all, can be controlled in humans on a long term basis by such treatment inasmuch as the daily administration of bromocriptine citrate resets neuronal activity timing in the neural centers of the brain to produce long term effects. | 2017-10-26 |
20170305899 | ANTIBIOTIC COMPOUNDS AND COMPOSITIONS, AND METHODS FOR IDENTIFICATION THEREOF - Disclosed herein are compounds and methods for inhibiting bacterial DNA repair enzymes, including AddAB and RecBCD helicase-nucleases. Pharmaceutical compositions and methods for treating a subject with an antibacterial agent are also disclosed herein. | 2017-10-26 |
20170305900 | HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF - Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. | 2017-10-26 |
20170305901 | THERAPEUTIC TARGETING OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 (IRAK4) IN CANCERS CHARACTERIZED BY REARRANGEMENTS IN THE MIXED LINEAGE LEUKEMIA GENE (MLL-r) - Disclosed are methods for treating cancers associated with rearrangements in the mixed lineage leukemia gene (MLL-r), including MLL-r leukemia. The methods typically include administering a therapeutic amount of one or more therapeutic agents that inhibit the biological activity of one or more members of the interleukin-1 signaling pathway such inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4). | 2017-10-26 |
20170305902 | TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE - The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 2017-10-26 |
20170305903 | DIAZEPINONE DERIVATIVES - The invention relates to compound of the formula I | 2017-10-26 |
20170305904 | COMPOUNDS FOR INHIBITING DRUG-RESISTANT STRAINS OF HIV-1 INTEGRASE - A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: | 2017-10-26 |
20170305905 | CRYSTALLINE FORM OF AN ANXIOLYTIC COMPOUND - The present invention provides a crystalline Form B of compound 1, and pharmaceutically compositions thereof. The present invention also provides methods of treating a disease (e.g., a disease of the central nervous system) using the pharmaceutical compositions. | 2017-10-26 |
20170305906 | Pro-Neurogenic Compounds - Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 2017-10-26 |
20170305907 | METHODS OF PRODUCING HETEROPOLYCYCLES VIA BIS-EPOXIDATION - A method of synthesizing a heteropolycycle, the method involving: reacting a bisepoxide with a first heteroatom nucleophile, to obtain a mixture comprising a diol compound; and further processing, to obtain the heteropolycycle with at least two heteroatoms within its polycyclic backbone, wherein each nitrogen within the polycyclic backbone of the heteropolycycle is introduced into the polycyclic backbone via an amine nucleophile. | 2017-10-26 |
20170305908 | SPIRO-INDOLINES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION (RSV) - Benzimidazoles of formula (I): wherein: one of X and Y is an N atom or a substituted C atom, and the other is CH; L is a single bond, C | 2017-10-26 |
20170305909 | CHEMICAL COMPOUNDS - The specification relates to compounds of Formula (I): | 2017-10-26 |
20170305910 | Substituted Xanthines and Methods of Use Thereof - Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5. | 2017-10-26 |
20170305911 | DEUTERATED QUINAZOLINONE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - Deuterated quinazolinone compounds and pharmaceutical compositions containing such compounds are provided. In particular, deuterated quinazolinone compounds of formula (I) are provided, as well as pharmaceutical compositions containing such compounds or crystal form, pharmaceutically acceptable salts, hydrates or solvates thereof. The deuterated quinazolinone compounds of formula (I) can be used for treating and/or preventing PI3K kinase-associated diseases, such as cancer, cell proliferative diseases and the like. | 2017-10-26 |
20170305912 | PROCESS FOR THE PREPARATION OF 3-PHENYL/HETEROARYL-6-PHENOXY-8-ALKYLAMINO-IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES - A process for the preparation of 3-phenyl/heteroaryl-6-phenoxy-8-alkylamino-imidazo[1,2-b]pyridazine derivatives and intermediates of this process. A crystalline form of N-cyclopropyl-4-{6-(2,3-difluor-4-methoxyphenoxy)-8-[(3,3,3-trifluorpropyl)amino]imidazo[1,2-b]pyridazin-3-yl}-2-methylbenzamide. The compounds are inhibitors of the Mps-1 kinase (Monopolar Spindle 1 kinase; also known as Tyrosine Threonine Kinase, TTK). | 2017-10-26 |
20170305913 | SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS - The present invention provides pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) and the compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. These pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGluRs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. | 2017-10-26 |
20170305914 | ACID ADDITION SALT OF IBRUTINIB - The present invention relates to acid addition salts of ibrutinib, a pharmaceutical composition comprising the same as well as a method of preparing the same. | 2017-10-26 |
20170305915 | INDAZOLE AND INDOLE DERIVATIVES AS INHIBITORS OF RETINOIC ACID RELATES ORPHAN RECEPTOR GAMMA (ROR GAMMA) FOR THE TREATMENT OF IMMUNE-RELATED DISEASES - The present invention provides compounds of formula (I), wherein A | 2017-10-26 |
20170305916 | METHYL DIAZEPANE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to methyl diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved. | 2017-10-26 |
20170305917 | COMPOUNDS - The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the characters are as defined in the description). The compounds of the general formula (I) are inhibitors of Factor XIa, so that they are useful in the prevention of and/or therapy for thromboembolic diseases. | 2017-10-26 |
20170305918 | DUAL-WARHEAD COVALENT INHIBITORS OF FGFR-4 - The disclosure includes compounds of Formula (I) | 2017-10-26 |
20170305919 | CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR - Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2017-10-26 |
20170305920 | 3-ACETYLENYL-PYRAZOLE-PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USES THEREOF - The present invention relates to the field of chemical and medicine, more particularly, 3-ethynylpyrazolopyrimidine derivatives and their preparation methods and uses. The invention provides a 3-ethynylpyrazolopyrimidine derivative, and the structure is shown in formula I. The present invention also provides preparation methods and use of 3-ethynylpyrazolopyrimidine derivatives, comprising the compounds and derivatives, and their pharmaceutical compositions for the use of the treatment and prevention of tumors. | 2017-10-26 |
20170305921 | FUSED TETRA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARP INHIBITORS - Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof. | 2017-10-26 |
20170305922 | CARM1 INHIBITORS AND USES THEREOF - Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein R1, R2a, R2b, R3 and Ring B are as defined herein, and Ring A is a group of Formula (A-i), (A-ii), or (A-iii): wherein R, R, R, R, and R are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described. | 2017-10-26 |
20170305923 | FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS - The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, X, Y, m, R1, R5, Ra and Rb are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject. | 2017-10-26 |
20170305924 | NARGENICIN COMPOUNDS AND USES THEREOF AS ANTIBACTERIAL AGENTS - The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by | 2017-10-26 |
20170305925 | PROCESS OF SYNTHESIZING 3-(4-METHYLPIPERAZINE-1-CARBONYL)-7-OXABICYCLO[2.2.1] HEPTANE-2-CARBOXYLIC ACID - The present invention provides a process for producing the compound having the structure: | 2017-10-26 |
20170305926 | MCL-1 INHIBITORS AND METHODS OF USE THEREOF - Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1 | 2017-10-26 |
20170305927 | ANTIBACTERIAL BASIC BIAROMATIC DERIVATIVES WITH AMINOALKOXY SUBSTITUTION - The invention relates to antibacterial compounds of formula I | 2017-10-26 |
20170305928 | NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - This invention relates to important intermediates in the preparation of a compound which is an inhibitor of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1). | 2017-10-26 |
20170305929 | QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - There are disclosed a series of quinuclidines having the Formula (I), which bind to the nicotinic α7 receptor and may be useful for the treatment of disorders of the central nervous system. | 2017-10-26 |
20170305930 | OPTICAL FILM - Provided is an optical film which has a maximum absorption at a wavelength in the range of 600 to 680 nm, has a high dichroic ratio, and is excellent in light resistance. The optical film includes: a polymer of a polymerizable liquid crystal compound; and a compound represented by the following general formula (1). | 2017-10-26 |
20170305931 | N-[2-(2-AMINO-6,6-DISUBSTITUTED-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZ- IN-8a(8H)-YL)-1,3-THIAZOL-4-YL] AMIDES - The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, | 2017-10-26 |
20170305932 | Fused Pentacyclic Imidazole Derivatives - A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof. | 2017-10-26 |
20170305933 | TYK2 INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders. | 2017-10-26 |
20170305934 | NAPHTHYRIDINE COMPOUNDS AS JAK KINASE INHIBITORS - The invention provides compounds of formula (I): | 2017-10-26 |
20170305935 | Novel 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative - There is provided a 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative which is useful in the treatment of respiratory syncytial virus (RSV) infection and for the prevention of disease associated with RSV infection. (Formula (1)). | 2017-10-26 |
20170305936 | SOLID STATE FORMS OF CRISABOROLE - Solid state forms of Crisaborole and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof are disclosed. | 2017-10-26 |
20170305937 | PROCESS FOR THE PREPARATION OF AMINOARYL- AND AMINOHETEROARYL BORONIC ACIDS AND ESTERS - The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters thereof of formula (I) in high yields | 2017-10-26 |
20170305938 | FLUORINE-CONTAINING ALKYLSILANE COMPOUND AND METHOD FOR PRODUCING THE SAME - A fluorine-containing alkylsilane compound represented by the general formula: | 2017-10-26 |
20170305939 | METHOD FOR THE DIRECT SYNTHESIS OF METHYL CHLOROSILANES IN FLUIDIZED-BED REACTORS - Methylchlorosilanes are synthesized by an at least two stage reaction in which contact composition from a first fluidized bed reactor is fed to a second fluidized bed reactor. | 2017-10-26 |
20170305940 | PROCESS FOR SILANE OLIGOMER COMPOSTITION PREPARATION AND USE THEREOF - Epoxy silane oligomers are prepared from a glycidoxypropyl alkoxysilane in the presence of an alcohol and an esterification and/or transesterification catalyst, and have improved storage stability. The oligomers are particularly useful as scrub-resistant additives for aqueous architectural coatings. | 2017-10-26 |
20170305941 | Silylated Pyrimidine Prodrugs And Methods Of Their Use - Silylated-pyrimidine prodrugs, compositions that include the silylated-pyrimidine prodrugs, methods for making the silylated-pyrimidine prodrugs and compositions, and methods for treating cancer using the silylated-pyrimidine prodrugs and compositions. | 2017-10-26 |
20170305942 | MIXED LIGAND GOLD(I) COMPLEXES AS ANTI-CANCER AGENTS - Gold(I) complex with mixed ligands as an anticancer agent. The gold(I) ion is coordinated to a dithiocarbamate ligand and a phosphorus-containing ligand (e.g. phosphines). Also described are a pharmaceutical composition incorporating the gold(I) complex, a methods of synthesizing the gold(I) complex, and a method for treating cancer. | 2017-10-26 |
20170305943 | COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS - Compounds and methods are provided for treating bacterial infections. | 2017-10-26 |
20170305944 | METHOD OF BIOTRANSFORMATION OF BENZOPYRONE COMPOUNDS INTO THE CORRESPONDING PHOSPHATE-CONJUGATED DERIVATIVES - The present invention is related to a biotransformation process, effected by means of an isolated polypeptide possessing benzopyrone phosphate synthetase activity, and also a microorganism comprising a nucleic acid sequence that encodes the polypeptide, for the preparation of phosphate-conjugated derivatives of benzopyrone compounds. The hydrophilic property of the benzopyrone compounds is enhanced after catalyzed by the benzopyrone phosphate synthetase of the present invention. | 2017-10-26 |
20170305945 | Phosphinyl Amidine Compounds, Metal Complexes, Catalyst Systems, and Their Use to Oligomerize or Polymerize Olefins | 2017-10-26 |
20170305946 | COMPOSITIONS AND METHODS COMPRISING RHENIUM FOR THE TREATMENT OF CANCERS - Compositions and methods comprising rhenium are provided. In some embodiments, the rhenium compounds comprise a bidentate ligand. In some embodiments, the rhenium compounds are used in method for treating cancer. | 2017-10-26 |
20170305947 | DEHYDROGENATION OF NEAT FORMIC ACID - A formic acid decomposition catalyst system includes organometallic complexes having formula 1: | 2017-10-26 |
20170305948 | NOVEL PRECATALYST SCAFFOLDS FOR CROSS-COUPLING REACTIONS, AND METHODS OF MAKING AND USING SAME - The present invention provides novel transition-metal precatalysts that are useful in preparing active coupling catalysts. In certain embodiments, the precatalysts of the invention are air-stable and moisture-stable. The present invention further provides methods of making and using the precatalysts of the invention. | 2017-10-26 |
20170305949 | A METHOD OF PURIFYING LIGNIN BY SUBJECTING A SLURRY COMPRISING LIGNIN TO AN ELECTRIC FIELD - The present invention relates to a process for purifying, such as salt/ion depletion, and/or ash reduction,and/or sulphur removal, and/or free sugar depletion,and/or VOC depletion or fractionating,preferably by using dewatering, of a slurry comprising a lignin or lignin derivative or a combination thereof. A lignin or lignin derivative obtainable from said process and uses thereof are also disclosed. | 2017-10-26 |
20170305950 | GLYCAN ANALYSIS AND PROFILING - The invention provides methods and tools, for example, glycan arrays, for the analysis of glycans and anti-glycan antibodies. Embodiments of the invention may be used to detect proteins, antibodies, diseases and/or pathogenic agents. In other embodiments, methods of the invention are used to develop or optimize arrays and antibodies. | 2017-10-26 |
20170305951 | HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTINS AND CXCR4 CHEMOKINE RECEPTORS - Compounds, compositions, and methods for treatment and/or prevention of cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow progenitor cells) into circulating blood and enhancing retention of the cells in the blood are disclosed. For example, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine receptors are described and pharmaceutical compositions comprising at least one of the same. | 2017-10-26 |
20170305952 | PHARMACEUTICAL COMPOSITION, METHODS FOR TREATING AND USES THEREOF - The invention relates to a pharmaceutical composition according to the claim | 2017-10-26 |
20170305953 | 14-MEMBERED KETOLIDES AND METHODS OF THEIR PREPARATION AND USE - Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macro-cyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided. | 2017-10-26 |
20170305954 | SYNTHESIS OF 2', 3'-DIDEOXYNUCLEOSIDES FOR AUTOMATED DNA SYNTHESIS AND PYROPHOSPHOROLYSIS ACTIVATED POLYMERIZATION - Methods for preparation of 2′,3′-dideoxynucleotides support structures, such as 2′,3′-dideoxyguanosine, 2′,3′-dideoxyadenosine, and 3′-deoxythymidine support structures are disclosed. Various methods of using such structures are also provided, such as their use for automated DNA synthesis and pyrophosphorolysis activated polymerization. | 2017-10-26 |
20170305955 | Reprogramming of Cellular Adhesion - Disclosed are membrane-anchored polynucleotides, and compositions comprising the membrane-anchored polynucleotides. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds and compositions in research and therapeutic applications. | 2017-10-26 |
20170305956 | Ligand-Modified Double-Stranded Nucleic Acids - The invention provides for double stranded nucleic acid molecules comprising a 5′ extension of the sense or antisense strand and further comprising a plurality of nucleotides that are conjugated to a ligand and methods of using the double-stranded nucleic acid molecules. Ligand-modified oligomers where the sense stands form a tetraloop provide new potent and stable RNA interference agents. These dsNA molecules are synthesized using a plurality of nucleotides that include ligand-modified monomers, nucleotide analog monomers, modified nucleotide monomers and the like, using standard nucleotide synthetic methods and systems. | 2017-10-26 |
20170305957 | CRYSTALLINE FORMS OF 5alpha-ANDROSTANE-3beta,5,6beta-TRIOL AND PREPARATION METHODS THEREFOR - The present invention relates to four crystalline forms (crystalline forms A, B, C and D) of 5α-androstane-3β,5,6β-triol (YC-6) and preparation methods therefor. The four crystalline forms have significant difference in their lattice parameters, 2θ values and intensity in X-ray power diffraction, and melting points, etc. The study on its polymorphism is very important for further studying its effect, bioavailability and stability. | 2017-10-26 |
20170305958 | CRYSTALLINE FORMS OF 5alpha-ANDROSTANE-3beta,5,6beta-TRIOL AND PREPARATION METHODS THEREFOR - The present invention relates to four crystalline forms (crystalline forms A, B, C and D) of 5α-androstane-3β,5,6β-triol (YC-6) and preparation methods therefor. The four crystalline forms have significant difference in their lattice parameters, 2θ values and intensity in X-ray power diffraction, and melting points, etc. The study on its polymorphism is very important for further studying its effect, bioavailability and stability. | 2017-10-26 |
20170305959 | ANTILEISHMANIAL COMPOSITIONS AND METHODS OF USE - In one aspect, the invention relates methods and compositions for treating parasitic diseases, for example, leishmaniasis. In a further aspect, the compounds of the methods and compositions are isolated from | 2017-10-26 |
20170305960 | NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF - Compounds are provided according to Formula (I): | 2017-10-26 |
20170305961 | Steroids as Agonists for FXR - The invention relates to compounds of formula (I): | 2017-10-26 |
20170305962 | C17-ARYL SUBSTITUTED BETULINIC ACID ANALOGS - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: | 2017-10-26 |
20170305963 | PEPTIDE FRAGMENT CONDENSATION AND CYCLISATION USING A SUBTILISIN VARIANT WITH IMPROVED SYNTHESIS OVER HYDROLYSIS RATIO - The invention relates to a method for enzymatically synthesizing an (oligo)peptide, comprising coupling (a) an (oligo)peptide C-terminal ester or thioester and (b) an (oligo)peptide nucleophile having an N-terminally unprotected amine, wherein the coupling is carried out in a fluid comprising water, and wherein the coupling is catalyzed by a subtilisin BPN′ variant or a homologue thereof, which comprises the following mutations compared to subtilisin BPN′ represented by SEQUENCE ID NO: 2 or a homologue sequence thereof: a deletion of the amino acids corresponding to positions 75-83; a mutation at the amino acid position corresponding to S221, the mutation being S221C or S221 selenocysteine; preferably a mutation at the amino acid position corresponding to P225 wherein the amino acid positions are defined according to the sequence of subtilisin BPN′ represented by SEQUENCE ID NO: 2. Further, the invention relates to an enzyme suitable for use as a catalyst in a method of the invention. | 2017-10-26 |
20170305964 | IMMUNOGLOBULIN AGGREGATE REMOVAL - For the removal of high molecular weight compounds from recombinantly produced polypeptides generally chromatographic methods are employed. It has been found that underivatized controlled pore glass (uCPG) selectively binds high molecular weight compounds present in a solution. The purified polypeptide can be recovered e.g. from the flow through of a chromatography column containing uCPG as chromatography material. It has been found that this effect is pronounced at a pH value of about 4 to 6 in buffered solutions. With approximately 100 m | 2017-10-26 |
20170305965 | Fab REGION-BINDING PEPTIDE - The objective of the present invention is to provide a Fab region-binding peptide which is excellent in a binding capability to a Fab region of IgG, an affinity separation matrix which has the peptide as a ligand, and a method for producing a Fab region-containing protein by using the affinity separation matrix. In addition, the objective of the present invention is to provide a DNA which encodes the peptide, a vector which contains the DNA, and a transformant which is transformed by the vector. The above-described problems can be solved by utilizing a Protein G variant having the mutation of an amino acid substitution at the specific position. | 2017-10-26 |
20170305966 | METHOD FOR PRODUCING A STABLE PRECIPITATE ENRICHED IN PHYCOBILIPROTEINS. - The invention relates to a novel method for producing a stable precipitate enriched in phycobiliproteins by means of salicylic acid precipitation. The invention also relates to the use of said precipitate enriched in phycobiliproteins for producing cosmetic or dermatological, and food or nutraceutical compositions. | 2017-10-26 |
20170305967 | METHODS FOR REDUCING CD36 EXPRESSION - The invention provides a method for treating one or more complications of diabetes in a mammal. The method comprises administering to a mammal in need thereof an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (p | 2017-10-26 |
20170305968 | PEPTIDES WHOSE UPTAKE IN CELLS IS CONTROLLABLE - Disclosed herein, in certain embodiments, is a selective transport molecule with increased in vivo circulation. In some embodiments, a selective transport molecule disclosed herein has the formula (A-X-B-C)-M, wherein C is a cargo moiety; A is a peptide with a sequence comprising 5 to 9 consecutive acidic amino acids, wherein the amino acids are selected from: aspartates and glutamates; B is a peptide with a sequence comprising 5 to 20 consecutive basic amino acids; X is a linker; and M is a macromolecular carrier. | 2017-10-26 |
20170305969 | B-Lamella Blocking Peptide Used for Preventing and/or Treating Alzheimer's Disease - Provided in the present invention are a β-sheet breaker peptide used for preventing and/or treating Alzheimer's disease, and the use thereof for preventing and/or treating Alzheimer's disease. The amino acid sequence of the β-sheet breaker peptide is His-Lys-Gln-Leu-Pro-Phe-Tyr-Glu-Glu-Asp (SEQ ID NO:1). The polypeptide can specially bind to a β-amyloid protein monomer (Aβ | 2017-10-26 |