Abstract: The present invention relates to a benzothiazole derivative of formula 1 or a pharmaceutically acceptable salt thereof and a process for preparation thereof. The present invention also relates to a pharmaceutical composition comprising the compounds and the use of the compounds in the preparation of an anti-tumor medicament.

Abstract: Disclosed herein are oxiran amines useful for the treatment of a variety of diseases. The oxiran amines are useful in the manufacture of pharmaceutical compositions. The pharmaceutical composition may be used for the treatment or prevention of a disease caused by a virus having a lipid membrane or the pharmaceutical composition may be used for diseases requiring cell proliferation or immune-regulation.

Abstract: Continuous flow systems and methods produce succinic anhydride by a double carbonylation of ethylene oxide with carbon monoxide and at least one catalyst. In some embodiments, the double carbonylation occurs using a single catalyst. In other embodiments, a first catalyst is used to promote the first carbonylation, and a second catalyst different from the first catalyst is used to promote the second carbonylation. The succinic anhydride is isolated from the product stream by crystallization and the catalyst is recycled to the reaction stream.

Abstract: Disclosed are antioxidative, natural compounds, their salts, chelates and cleavage derivatives that exhibit a superior combination of properties. The compounds can be used for a variety of purposes, including stabilizing foods, cosmetics, beverages and nutritional supplement. The compounds can be prepared by substantially cleaving a humic acid of formula I to provide at least one antioxidant compounds of formula II, formula III, formula IV, formula V, formula VI, salts, or chelates thereof.

Abstract: An anhydrous crystalline form of S-equol has been discovered. Form I, the anhydrous crystalline form of S-equol has been isolated and characterized for the first time. As compared to other forms of S-equol, such as the known hydrate or other solvate forms, the anhydrous crystalline form of S-equol has improved properties.

Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R5, R6, W, and A are defined herein.

Abstract: The instant invention describes tetrazole compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: The present invention is directed to 2-hydroxymethyl 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 pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract: The present invention provides a new group of protein kinase inhibitors, aminopyrimidine derivatives, and pharmaceutically acceptable salts thereof that are useful for treating cell proliferative disease and disorder such as cancer and immune disease. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefore. The invention also provides useful intermediates generated during the syntheses of the aminopyrimidine derivatives.

Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.

Abstract: The present invention relates to (E)-ethyl 2-(2-methyl-3-((2-(naphtho[2,1-b]furan-2-carbonyl)hydrazono)methyl)-1H-indol-1-yl)acetate as a novel tubulin polymerization inhibitor and a method for synthesizing the same. The compound of the present invention can inhibit mitosis and induce apoptosis and thus be used as an anticancer agent, by binding to tubulin to inhibit microtube polymerization. According to the synthesis method of the present invention, the reaction is simplified and the efficiency is 60%, or higher, leading to a very high yield, thereby providing an effective synthesis method.

Abstract: Acetone solvate crystals of trityl olmesartan medoxomil are provided.

Abstract: This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders.

Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.

Abstract: The invention relates to the tartrate salt of 5-chloro-thiophene-2-carboxylic acid [(S)-2-[methyl-3-(2-oxo-pyrrolidin-1-yl) -benzenesulfonylamino]-3-(4-methyl-piperazin-1-yl)-3-oxo-propyl]amide, to its crystalline form, to its preparation and to its therapeutic use.

Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.

Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

Abstract: This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand-[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

Abstract: The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.

Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:

Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds of Formula I are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders.

Abstract: The present invention is directed to arylpyrrolopyridine derivatives of formula (A) (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Lewy body dementia, Parkinson's disease cancer.

Abstract: In one aspect, the invention relates to 3-benzylquinazolin-4(3H)-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction 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.

Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

Abstract: A process for the production of a formulation of HIV attachment inhibitor piperazine tris salt prodrug compound involves dissolving the prodrug compound in a solvent to form a solution; adding a first quantity of a first anti-solvent to the solution; then dispersing a first quantity of HPMC in the solution; adding a second quantity of the first anti-solvent to the solution; dispersing a second quantity of HPMC in the solution; then adding a second anti-solvent to the solution so as to crystallize the compound with the HPMC and thereby form the formulation, wherein the second anti-solvent is a combination of acetone and isopropyl acetate (IPAC). The formulation is then washed, and dried.

Abstract: The present application provides a compound of formula (1) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative diseases.

Abstract: The present invention relates to a pyrazolo[1,5-a]pyrimidine derivative of general formula 1 and a pharmaceutically acceptable salt thereof. The present invention also relates to use of compounds of formula 1 in the preparation of an anti-tumor medicament.

Abstract: The present application relates to compounds being of Formula (I), (II), (III), (IV), (V), (VI), (IIIa), (IIIb), (IIIc), (IIId), (IIIe), (IIIf), and (IIIg). Compounds of Formula (I) have the structure: wherein Q, R1, R18, R19, M, A and Y are as defined herein. The compounds of the application can modulate the activity of histone demethylases (HDMEs), and can be useful for the prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, e.g., cancer.

Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.

Abstract: The present invention relates to a bisulfate of a Janus kinase (JAK) inhibitor and a preparation method therefor. More specifically, the present invention relates to a (3aR,5s,6aS)-N-(3-methoxyl-1,2,4-thiadiazole-5-group)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-group)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate shown in the formula (I), a preparation method therefor, and an application thereof. The bisulfate shown in the formula (I) can be well suitable as a Janus kinase (JAK) inhibitor in clinical work for treating rheumatism or rheumatoid arthritis.

Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.

Abstract: The fused heterocyclic compound represented by formula (1) has excellent effectiveness in pest control. In the formula (1), J represents formula J1, J2, J3, J4, J5 or J6; A1; A2; A3; A4; A5; B1; B2; B4; B5; and B6 each represent a nitrogen atom, etc.; B3 represents NR15, etc.; R1 represents a C1-C6 chain hydrocarbon group, etc., optionally substituted with one or more atoms or groups selected from group X; the pairs R2 and R3 and R5 and R6 are the same or different, and represent a C1-C6 chain hydrocarbon group, etc., optionally substituted with one or more atoms or groups selected from group X; R4 represents a C1-C6 chain hydrocarbon group, etc., optionally substituted with one or more atoms or groups selected from group W; and n represents 0, 1, or 2.

Abstract: Disclosed in the present invention is a method for preparing Ticagrelor (I), comprising the following steps: a cyclization reaction of 5-amino-1,4-di-substituted-1,2,3-triazole (II) and dialkyl carbonate (HI), to obtain 9-substituted-2,6-dihydroxy-8-azapurine (IV); chlorination of intermediate (IV), to obtain 9-substituted-2,6-dichloro-8-azapurine (V); an amination reaction of intermediate (V) and trans-(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine (VI) generates 9-substituted-6-amino-substituted-2-chloro-8-azapurine (VII); and a propanethiolation reaction of intermediate (VII) and propanethiol (VIII), to obtain Ticagrelor (I). The preparation method is simple in process, has a high chemical and chiral purity and provides a new preparation method for industrializing Ticagrelor.

Abstract: This disclosure relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities. A tricyclic heterocyclic compound represented by the formula (Ib), wherein the rings Ab and Bb, Xb, Yb, R1b, R2b, R3b, L1b, L2b, L3b and nb are as defined in the specification.

Abstract: The present invention provides a substituted pyridine compound of the formula I or an agriculturally suitable salt or N-oxide thereof, wherein the variables in the formula I are defined as in the description. Substituted pyridine compounds of formula I are useful as herbicides.

Abstract: A macrocyclic compound having the structure of Formula (A), wherein each of R1 and R2 is independently (i) a 5-6 membered monocyclic aromatic ring containing 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or (ii) an 8-10 membered bicyclic aromatic ring containing 0-6 heteroatoms independently selected from nitrogen, oxygen, or sulfur. Each R1 and R2 may independently be substituted by 0, 1, 2, 3, or 4 substituents. Z1 represents a covalent bond, an atom, or a functional group comprising a grouping of atoms, wherein the grouping of atoms includes at least one heteroatom selected from the group consisting of N, O, P, and S. Also, Z1 may represent (i) a 5-6 membered monocyclic aromatic ring containing 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or (ii) an 8-10 membered bicyclic aromatic ring containing 0-6 heteroatoms independently selected from nitrogen, oxygen, or sulfur.

Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Metal organic framework compositions can have a face centered cubic structure.

Abstract: Disclosed are hydrophobic inorganic particles obtained by surface-modifying inorganic particles with an organic compound, in which the organic compounds are one or more kinds selected from compounds included in Groups (i) to (v): (1) amine and carboxylic acid which are monobasic acid having 8 or more carbon atoms (in the case of carboxylic acid, carbons in the carboxyl group are excluded) and having a straight chain or a branched chain; (ii) amine and carboxylic acid which are dibasic acid having 6 or more carbon atoms (in the case of carboxylic acid, carbons in the carboxyl group are excluded) and having a straight chain or a branched chain; (iii) amine and carboxylic acid which are monobasic acid having a straight chain or a branched chain including a carbon-carbon double bond; (iv) amine and carboxylic acid which are monobasic acid or dibasic acid having an aromatic ring; and (v) alcohol or phenol compound having 6 or more carbon atoms.

Abstract: Special hydroxysilanes, which can be obtained by reacting ?-(3,4-epoxycyclohexyl)alkyltrialkoxysilanes with secondary amines, and adducts of the hydroxysilanes in the form of polymers containing silane groups. The hydroxysilanes can be produced having high purity in a simple process and are very stable in storage after production. The polymers containing silane groups that can be obtained by means of the hydroxysilanes have advantageous properties. The polymers enable moisture-curing compositions, which contain no isocyanate groups and which are suitable as elastic adhesives and sealants.

Abstract: A method for producing a cyclic aminoorganoxysilane compound is provided. The method comprises the step of conducting dehydrochlorination coupling of a chloroalkylalkoxysilane compound represented by the formula: wherein R1 is a straight or branched divalent C1-10 hydrocarbon group, R2 is hydrogen atom or an unsubstituted or substituted C1-10 monovalent hydrocarbon group, R3 and R4 are respectively a C1-10 monovalent hydrocarbon group, and n is 0, 1, or 2 and an aminoalcohol represented by the formula: wherein R5 is a straight or branched C2-10 divalent hydrocarbon group which may contain a heteroatom and R6 is hydrogen atom or a straight or branched C1-10 monovalent hydrocarbon group, and promoting intramolecular transesterification to thereby produce a cyclic aminoorganoxysilane compound represented by the formula: wherein R1 to R6 and n are as defined above.

Abstract: Dinitrosyl iron complexes are disclosed, which are represented by the following formula (I): [(R1R2N(CH2)nNR3(CH2)mNR4R5)Fe(NO)2]z??(I) wherein the definitions of R1, R2, R3, R4, R5, n, m and z are the same as those defined in the specification. In addition, the present invention further provides a use of the aforementioned dinitrosyl iron complexes, and a water splitting device using the same.

Abstract: The present invention relates to fractions of high purity lignin which are thermally stable, and to methods of producing said fractions from lignocellulosic material.

Abstract: A method of preparing a low-molecular lignin derivative comprises the step of: preparing lignin by hydrolyzing lignocellulosic biomass with an acid; preparing a first mixture by mixing 100 parts by weight of the lignin and 500 parts or more by weight of a phenolic compound; preparing a second mixture by mixing the first mixture with a solvent including the hydrophobic polar solvent; and recovering a low-molecular lignin derivative from the second mixture.

Abstract: The present invention relates to a novel method for synthesising, without a solvent, N-alkyl-glycosyl(di)amine derivatives represented by the following general formula (I): The invention also concerns the use of N-alkyl-glycosyl(di)amine derivatives represented by the general formula (I), and N-alkyl-glycosyl(di)ammonium quaternary salts represented by the general formula (II) and N-alkyl-glycamine derivatives represented by the general formula (III) obtained from N-alkyl-glycosyl(di)amine derivatives represented by the general formula (I), as antibacterial and/or antifungal agents against phytopathogens.