Abstract: The present invention provides a compound of the Formula (I): wherein X, R, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as defined herein, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention generally relates to compounds and methods for inhibiting the radical polymerization of unsaturated compounds, particularly vinyl monomers. More particularly, it relates to the use of stable hydroxyl amines to inhibit the polymerization of unsaturated compounds (e.g., vinyl monomers) wherein said stable hydroxylamine is soluble in organic solvents, particularly hydrocarbon solvents consisting of unsaturated and, therefore, polymerizable constituents.

Abstract: The invention provides compounds that inhibit ROCK activity. In certain embodiments the compounds of the invention enhance cognitive function. The invention is also directed to pharmaceutical compositions that comprise ROCK inhibitors and to methods enhance cognitive function and reducing and/or treat cognitive function decline.

Abstract: 2-Aminopyridine compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for modulating USP7, and for treating cancer and immune disorders such as inflammation mediated by USP7. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.

Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

Abstract: The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.

Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

Abstract: Methods for fluorinating organic compounds utilizing a novel organic reagent are described herein. The invention further discloses the utility of this reagent for incorporation of the 18 F isotope into hydroxyl group-containing organic molecules for PET imaging studies. Preparation of the reagents is described along with isolable intermediate structures from reaction of the reagent with a hydroxyl group-containing organic molecule.

Abstract: The present invention discloses a preparation method of 2,3-dimethyl phenyl-1-trityl-imidazole-4-ketone. In accordance with this method, imidazole-4-ethyl formate is used as a raw material; ethyl formate is used for amino protection, 1-trityl-1H-imidazole-4-formic acid is obtained after basic hydrolysis; 1-trityl-1H-imidazole-4-formic acid and N,O-dimethylhydroxylamine hydrochloride are subjected to condensation so as to obtain N-methoxyl-N-methyl-1-trityl-1H-imidazole-4-formamide; and N-methoxyl-N-methyl-1-trityl-1H-imidazole-4-formamide and a Grignard reagent prepared by the reaction of 2,3-dimethylbromobenzene with magnesium are subjected to a Grignard reaction, and then the target product 2,3-dimethyl phenyl-1-trityl-1H-imidazole-4-ketone is obtained. Compared with the reported preparation methods, the preparation method is more convenient to operate and is beneficial for industrial production.

Abstract: The present invention relates to quinazolinone and isoquinolinone derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.

Abstract: Disclosed are compounds of Formula I, or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R1, R2, R3, R4 and R5 are as described in this application, and methods of using said compounds in the treatment of cancer.

Abstract: The invention relates to novel oxazolidinone compound. More particularly, the invention relates to novel [(S)—N-[[3-[4-fluoro-3-morpholino phenyl]-2-oxooxazolidin-5-yl] methyl] acetamide] compound of Formula-I which was disclosed in Indian Patent Application No. 5063/CHE/2013 and corresponding PCT/IN2014/000018. The compound is a broad spectrum antimicrobial agent effective against Multi-Drug Resistant S. Maltophilia pathogen and a large number of gram positive and gram negative pathogens. The compound has shown excellent biological activities against S. Maltophilia which has developed resistance against a large number of antibiotics including some of the known and widely used oxazolidinone derivatives.

Abstract: The present invention provides new stable crystalline N-iodoamides -1-iodo-3,5,5-trimethylhydantoin (1-ITMH) and 3-iodo-4,4-dimethyl-2-oxazolidinone (IDMO). The present invention further provides a process for the preparation of organic iodides using N-iodoamides of this invention and recovery of the amide co-products from waste water.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.

Abstract: Compounds of general formula (I): wherein R1, R11, Y, R2, n and A are as defined herein are useful as inhibitors or metallo-?-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.

Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Abstract: The invention is directed to methods of inducing apoptosis, arresting cell cycle, or inhibiting cellular proliferation, or any combination thereof, in a tumor cell, by administration of an effective amount of an N-acyl homoserine lactone analog (AHL), optionally in conjunction with a tumor modulating agent such tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) to the patient. Novel bioactive analogs of an N-acyl homoserine lactone are also provided.

Abstract: Disclosed are a 3-furyl-2-cyano-2-acrylamide derivative with epidermal growth factor receptor (EGFR) inhibitory activity and pharmaceutical acceptable salt thereof, together with preparation method thereof, pharmaceutical composition comprising the compound, and application of the compound in treating senile dementia (AD). The new compound is shown as formula I, wherein R1 is selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl and C3-C6 cycloalkyl; R2 is selected from the group consisting of alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, aralkyl and heteroaralkyl; X is selected from the group consisting of CH2, NH, O and S; m and n are all integers greater than or equal to zero.

Abstract: We describe anhydride compounds suitable for physiologically labile modification of amine-containing molecules. The described anhydrides form reversible linkages having desirable kinetics for in vivo delivery of biologically active molecules. Also described are endosomolytic polymers formed by modification of membrane active polyamines with the described anhydrides.

Abstract: The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (VI), or a salt thereof and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (VI) and process for the preparation thereof.

Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.

Abstract: The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.

Abstract: The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.

Abstract: The invention relates to a process for preparing chloroacetaldehyde acetals of monohydric, dihydric or higher-functionality aliphatic alcohols, in which the chloroacetaldehyde acetal is obtained from an aqueous chloroacetaldehyde solution in the presence of the alcohol to be acetalized and an acid catalyst by azeotropic removal of water with the aid of a solvent, wherein the solvent is a halogenated solvent.

Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described; which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.

Abstract: Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof.

Abstract: Pyridazinone derivatives of the general formula (I) are described as herbicides. In this formula (I), Y, R1, R2 and R3 are each radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a substituted heterocycle.

Abstract: This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.

Abstract: Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert the resulting products to substantially a single salt form.

Abstract: The invention relates to substituted phenylalanine derivatives and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and/or severe perioperative blood loss.

Abstract: The instant invention provides photolysable compounds, and their use in reversible chemical induced dimerization and light-induced regulation of proteins.

Abstract: Provided herein are compositions and methods for reducing one or both of axonal degeneration and neuronal cell death associated with a disease or traumatic brain injury. An aminopropyl carbazole agent with potent neuroprotective properties is described. Specifically, (?)-(S)—N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine, is proposed as a new pharmacological agent for protecting patients against axonal degeneration and chronic consequences of TBI.

Abstract: Novel uncharged reactivators of human acetylcholinesterase, pharmaceutical compositions including the compounds, and their use for reactivating human acetylcholinesterase inhibited by at least one organophosphorus nerve agent.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

Abstract: A tetrazolinone compound represented by formula (1) wherein E represents the following group E16; Y represents —O—CH2—; Q represents the following group Q46; R8 represents a C1-C6 alkyl group; R3, R30 and R31 are the same or different and represent a hydrogen atom; A represents a C6-C16 aryl group optionally having one or more atoms or groups selected from Group P1; R5 represents a C1-C3 alkyl group; and X represents an oxygen atom or a sulfur atom, has excellent control activity against pests.

Abstract: In some embodiments, macromolecules and related methods are provided. In some embodiments, an iterative growth process may be used to form a macromolecule comprising one or more repeat units comprising a functionalizable pendant group, with precise control over mass, length, backbone sequence, pendant group sequence, and/or stereochemistry, amongst other features. Macromolecules (e.g., non-natural macromolecules) form from the iterative growth process, described herein, may be used for a wide variety of applications, including the delivery of active agents.

Abstract: The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

Abstract: The present invention relates to compounds of formula wherein R1/R2 are hydrogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl, OCH2-cycloalkyl or heterocycloalkyl which is optionally substituted by halogen, with the proviso that one of R1 and R2 is hydrogen, or R1 and R2 form together with the carbon atom to which they are attach a phenyl ring, which may be optionally substituted by lower alkyl; R3/R4 are hydrogen, halogen or cyano; with the proviso that one of R3 and R4 is hydrogen; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, h

Abstract: Present invention relates to crystalline form of suvorexant, amorphous form of suvorexant, amorphous solid dispersion of suvorexant, processes for their preparation and pharmaceutical dosage form thereof.

Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.

Abstract: Process for the preparation of a benzohetero[1,3]diazole compound disubstituted with heteroaryl groups which comprises reacting at least one benzohetero[1,3]diazole compound disubstituted with at least one heteroaryl compound. Said benzohetero[1,3]diazole compound disubstituted with heteroaryl groups can be advantageously used in the construction of luminescent solar concentrators (LSC). Furthermore, said benzohetero[1,3]diazole compound disubstituted with heteroaryl groups can be advantageously used in the construction of photovoltaic devices such as, for example, photovoltaic cells, photovoltaic modules, solar cells, solar modules, on both a rigid and flexible support. Said benzohetero[1,3]diazole compound disubstituted with heteroaryl groups can also be advantageously used as a precursor of monomeric units in the preparation of semiconductor polymers.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided. The compounds are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Pharmaceutical compositions comprised of one or more compounds of formula (I) are also provided.

Abstract: Compounds of the formula I or II: or pharmaceutically acceptable salts thereof, wherein R1 is a group of formula (a), (b), (c); (d) or (e): and m, n, X, Y, R1, R2, R3, R4, Rb and Rc are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

Abstract: Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.

Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.