Abstract: The present invention relates to an improved process for the preparation of [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid dihydrate, represented by the following structural formula (I).

Abstract: The present invention describes a novel process for preparing piperidine-4-carbothioamide hydrochloride.

Abstract: The invention relates to tetrahydroquinoline derivatives and their use in the treatment and/or the prevention of a disease wherein the Epac protein is involved, such as inflammation, cancer, vascular diseases, kidney diseases, cognitive disorders and cardiac diseases.

Abstract: The present invention pertains to a new compound E)-2-(5-((4-methoxy-2-(trifluoromethyl)quinolin-6-yl)methoxy)-2-((4-(trifluoromethyl) benzyl)oxy)-benzylidene) hexanoic acid (MTTB), and its derivatives. The compounds of the invention are useful as selective peroxisome proliferator-activated receptor gamma (PPAR?) antagonists and are indicated for the use in the treatment of immune related diseases such as systemic inflammation, sepsis and septic shock.

Abstract: Provided are heterocyclic compounds having a ROR?t inhibitory action represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity.

Abstract: Bifunctional compounds that increase uric acid excretion and reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders or uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are provided. Pharmaceutical compositions comprising the bifunctional compounds are also provided.

Abstract: The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt:

Abstract: The present invention provides novel functionalized mixtures 4- and 5-vinyl substituted regioisomers of 1,2,3-triazoles via 1,3-dipolar cycloaddition. Functionalized alkyne moieties with a terminal alcoholic functionality are reacted with functionalized organic moieties with a terminal leaving group and an azide to provide an alcoholic functionalized mixture of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties. The mixture may be converted to a wide variety of useful functionalized mixtures of 4- and 5-vinyl substituted regioisomers of 1,2,3-triazole moieties, which in turn can be converted to a wide variety of useful polymers The novel alcoholic functionalized mixtures of 4- and 5-substituted regioisomers can be separated by chromatography to provide the purified 4- and 5-alcoholic functionalized substituted 1,2,3-triazole moieties. The novel compounds of the invention can be employed in a wide variety of compositions (Formulae (I), (II)); wherein R1, R2, R3, and R4, are defined herein.

Abstract: The present invention relates to a process for the preparation of the ketone compounds (IA) and their use as intermediates for the preparation of triazole fungicides.

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

Abstract: Synthesizing bio-plasticizers with acidic ionic liquids as catalysts. The acidic ionic liquids are Bronsted acidic ionic liquids, which are composed of alkyl sulfone pyridinium and strong Bronsted acid. Epoxidized fatty acid alkyl esters could be obtained via epoxidation of fatty acid alkyl esters using the acidic ionic liquids as catalysts. The epoxidized fatty acid alkyl esters perform well as bio-plasticizers, which could be substituted for phthalate ester plasticizers. The acidic ionic liquids catalysts provide good catalytic performance, are easy to separate, reusable, and may reduce corrosion of pipelines.

Abstract: Psicose is converted into 5-hydroxymethylfurfural or an alkyl ether thereof in a process for the catalyzed conversion of psicose, including the steps of: a. forming a feed including psicose and water or at least one alkanol or a mixture thereof and b. converting the psicose in the feed at a temperature in the range of 50 to 300 degrees Celsius in the presence of a catalyst.

Abstract: The present disclosure provides methods to produce substituted furans (e.g., halomethylfurfural, hydroxymethylfurfural, and furfural), by acid-catalyzed conversion of biomass using a gaseous acid in a multiphase reactor, such as a fluidized bed reactor.

Abstract: Furfural is produced from biomass material containing pentosan, in high yields, in a production process comprising treating the biomass with a solution containing at least one ?-hydroxysulfonic acid thereby hydrolyzing the biomass to produce a product stream containing at least one C5-carbohydrate compound in monomeric and/or oligomeric form, and dehydrating the C5-carbohydrate compound in the presence of an acid, in a biphasic reaction medium comprising an aqueous phase and a water-immiscible organic phase, at a temperature in the range of from about 100° C. to about 250° C. to produce a dehydration product stream containing furfural. An aqueous stream is separated from the dehydration product that can be optionally recycled to the hydrolysis step.

Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.

Abstract: A method is described for making single isomers of synthetic beraprost diol, a key intermediate for making 314-d isomer of beraprost. The method requires fewer steps than the known methods for making these compounds and can be used to scale up the reaction more easily to produce commercial quantities.

Abstract: The present invention concerns compounds that selectively inhibit the activity of the Hedgehog (Hh) pathway, their preparation and uses thereof. The compounds of the present invention are useful in treating Hh-dependent tumors, such as medulloblastoma (MB).

Abstract: The present invention relates to a method for synthesizing cyclocarbonates by reacting an epoxy compound and carbon dioxide at atmospheric pressure and elevated temperature in the presence of a heterogeneous catalyst system comprising an alkali metal halide and silica as well as the use of said catalyst system for the synthesis of cyclocarbonates.

Abstract: The present invention relates to 3-[(benzo[d][1,3]dioxolan-4-yl)-oxy]-3-arylpropylamine compounds of formula I or pharmaceutically acceptable salts thereof and use thereof. The compound may be used to prepare an antidepressant agent.

Abstract: A compound represented by a formula [1D] as shown below (wherein R1A, R1B, R2A, R2B, R3A and R3B represent a hydrogen atom, an optionally substituted C1-6 alkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside.

Abstract: The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate are also disclosed.

Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate are also disclosed.

Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate are also disclosed.

Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

Abstract: The present invention provides novel GOAT inhibitors and their salts and pharmaceutical compositions thereof.

Abstract: A series of substituted 4,5,6,7-tetrahydrobenzimidazole derivatives, being potent modulators of human TNF? 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.

Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof a compound described herein.

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.

Abstract: Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.

Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.

Abstract: Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders or uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided.

Abstract: This invention relates to a compound, as defined in the specification and as represented by the compound of formula (I): useful in the treatment of mycoses, to compositions containing it and its use in therapy.

Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula (I), wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.

Abstract: Compounds of formula I are provided herein, as well as the use of these compounds for controlling invertebrate pests. Plant propagation material and agricultural and veterinary compositions including these compounds are also provided. Compounds for use as intermediate compounds in the preparation of the compounds of formula I are also described.

Abstract: The present invention provides a compound of formula 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: Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy-induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain).

Abstract: The present disclosure relates to crystalline form of (S)—N—((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, salts and hydrates thereof. This disclosure also relates to solid oral formulation of (S)—N—((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, pharmaceutically acceptable salts, solvates (including hydrates) thereof, as well as methods of treatment using the same.

Abstract: Provided herein are deuterated O-sulfated beta-lactam hydroxamic acids and deuterated N-sulfated beta-lactams, pharmaceutical compositions thereof and methods of treating infectious disease with deuterated compounds or pharmaceutical compositions thereof.

Abstract: The present application relates to a compound of formula (I) The present application also relates to synthesizing the compound of formula I and treating a patient with the compound of formula I having a neuropsychiatric illnesses such as a depressive disorder, schizophrenia; alcohol, nicotine, and morphine withdrawal induced depression and hyperalgesia; neuropathic pain caused by anticancerous drugs; diabetic neuropathic pain; obsessive compulsive disorder; alcohol withdrawal syndrome; static and dynamic allodynia in diabetic and cancer patients on anticancer therapy and chronic pain therapy.

Abstract: Disclosed are substituted aromatic N-heterocyclic compounds. The disclosed compounds typically exhibit kinase inhibition activity, for example, and inhibit Mnk1 kinase and/or Mnk2 kinase. The disclosed compounds may be used in pharmaceutical compositions and methods for treating diseases or disorders associated with Mnk1 kinase activity and/or Mnk2 kinase activity, such as cancers, diabetes, autism, and fragile X syndrome.

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: Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen, or substituted or unsubstituted alkyl, R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or the like, with the proviso that R1, R2 and R3 are not simultaneously hydrogen, X is a single bond, —S—, —O—, —NR5—, —C(?O)— or the like, R5 is hydrogen, or substituted or unsubstituted alkyl, Y is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl or the like.

Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5 and Ar are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: A process for making certain spiroheterocyclic pyrrolidine dione derivatives.

Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.

Abstract: Disclosed are nucleopeptide compounds that include a nucleobase, and an amino acid. Certain compounds further comprise a glycoside. The compounds may self-assemble to form supramolecular hydrogels. Also, the compounds may be used as a platform to examine specific biological functions (e.g., binding to DNA and RNA) of a dynamic supramolecular system that is able to interact with both proteins and nucleic acids. Other uses include: methods of growing cells and methods of delivering a substance to a cell.

Abstract: 6,8-Disubstituted-9-(heterocyclyl)purines for use in pharmaceutical and cosmetic compositions and applications are provided. These 6,8-disubstituted-9-(heterocyclyl)purines have a wide range of biological activities, including for example antioxidant, anti-inflammatory, anti-senescent, anti-aging, as well as well as other activities which are especially useful in pharmaceutical and cosmetic applications. Compositions may include additional excipients and auxiliary substances. Methods of treatment of animals, mammals, plants, cells, yeast, and cells in tissue culture are also disclosed.