Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.

Abstract: This invention relates to a process for the preparation of Form A of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide. Also disclosed herein is Form A of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide, or pharmaceutical compositions thereof, obtainable by the process described herein.

Abstract: The present invention relates to a novel cyclic compound represented by Formula 1, and an organic light emitting device comprising an organic material layer including the novel cyclic compound and having improved efficiency, low driving voltage, and enhanced lifetime characteristic:

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.

Abstract: The present invention includes novel bridged bicycloalkyl-substituted aminothiazole compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.

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: An apparatus includes a conduit with two process fluid inlets at one end of the conduit, one process fluid outlet at an opposing end, a heat exchange medium inlet, and a heat exchange medium outlet. One of the fluid inlets includes a tube extending into the conduit and a perforated node at the end of the tube, and the other of the fluid inlets is arranged up stream of the perforated node. The apparatus further includes hollow tubes positioned longitudinally within the conduit between the two process fluid inlets, the process fluid outlet, the heat exchange medium inlet and the heat exchange medium outlet. In addition, the apparatus includes a collection vessel positioned proximate the fluid outlet and fibers extending through each of the hollow tubes, wherein one end of the fibers is secured to the perforated node and the other end of the fibers extends into the collection vessel.

Abstract: The present invention relates to a new class of compounds of formula (I) having an antiviral effect and the uses thereof.

Abstract: The present invention relates to a new compound of formula I: or pharmaceutically acceptable salt, solvate or stereoisomer thereof, wherein: V1 is C or N, V2 is C(R2) or N, whereby if V1 is C then V2 is N, if V1 is C then V2 is C(R2), or if V1 is N then V2 is C(R2); each n, k is independently 0, 1; each R2, R11 is independently H, D, Hal, CN, NR?R?, C(O)NR?R?, C1-C6 alkoxy; R3 is H, D, hydroxy, C(O)C1-C6 alkyl, C(O)C2-C6 alkenyl, C(O)C2-C6 alkynyl, C1-C6 alkyl; R4 is H, Hal, CN, CONR?R?, hydroxy, C1-C6 alkyl, C1-C6 alkoxy; L is CH2, NH, O or chemical bond; R1 is selected from the group of the fragments, comprising: Fragment 1, Fragment 2, Fragment 3 each A1, A2, A3, A4 is independently CH, N, CHal; each A5, A6, A7, A8, A9 is independently C, CH or N; R5 is H, CN, Hal, CONR?R?, C1-C6 alkyl, non-substituted or substituted by one or more halogens; each R? and R? is independently selected from the group, comprising H, C1-C6 alkyl, C1-C6 cycloalkyl, aryl; R6 is selected from the group: [formula II] each R7, R8, R9

Abstract: Disclosed are piperidine-2,6-dione derivatives and treatment of Crohn's disease.

Abstract: A 1,2,4-triazine-3-amine derivative, a preparation therefor, and use thereof in medicine are provided. Specifically, a 1,2,4-triazine-3-amine derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and use thereof as a therapeutic agent, in particular as an A2a or A2b receptor antagonist, and use thereof in the preparation of a medicament for treating a condition or disorder that is ameliorated by means of inhibition of the A2a or A2b receptor are provided. Each substituent in general formula (I) is defined in the description.

Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

Abstract: The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing thereof, and a use thereof for inhibiting activity of mutant IDH2 and treating cancer.

Abstract: Presented herein are MCT4 inhibitors and uses thereof for treating cancer.

Abstract: This invention provides, among other things, compounds useful for treating diseases such as cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.

Abstract: An object of the present invention is to provide a methyllactam ring compound that has an SGLT1 inhibitory activity and is useful for a drug, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof. A compound of Formula [I]: or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.

Abstract: The invention relates, in certain aspects, to developable forms of certain compounds that are useful to treat and/or prevent EBV infection and related conditions in a subject. The invention further provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection and/or lytic EBV infection.

Abstract: Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical com-positions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.

Abstract: Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.

Abstract: Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.

Abstract: The present invention provides solid forms of SGLT2 inhibitors, to processes for their preparation and their use in the purification of SGLT2 inhibitors and also provided pharmaceutical compositions comprising them and their use in therapy.

Abstract: The present invention provides solid forms of SGLT2 inhibitors, to processes for their preparation and their use in the purification of SGLT2 inhibitors and also provided pharmaceutical compositions comprising them and their use in therapy.

Abstract: Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds of Formula I described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

Abstract: Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds have the following structure: in which Z is an oxadiazole. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2/Smad3 signaling pathway.

Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels.

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.

Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, • B is a saturated or partially unsaturated monocyclic or bicyclic, heterocyclic group optionally substituted by one or more R 10 groups; * X is selected from SO2, CO2, CO, CONR11 and (CR12 R13) p. Said compounds are capable of inhibiting PAICS and are useful in the treatment of proliferative disorders. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).

Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: •B is an aryl or heteroaryl group optionally substituted by one or more R10 groups; and *X is selected from 0, (CR11R12)p and (CR11R12)p CO. Said compounds are capable of inhibiting PAICS and are useful in the treatment of proliferative disorders. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).

Abstract: The invention relates to a compound wherein R1 is selected from —I, —Br, —Cl, —F, C1-C6-alkyl, —O(CH2)mCH3, —(CH2)mOCH3, C1-C6-haloalkyl, a cycloalkyl, a heterocycle, a aryl or heteroaryl, wherein R2 is selected from H, C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, —CH2—(C3-C6-cycloalkyl), or —(CH2)rOCH3, wherein R3 is —NH2, —NH—R4, —NHC(?O)—R4, —NHC(?O)NH—R4, —NHC(?S)—R4 or —NHC(?S)NH—R4, wherein R4 is selected from a cycloalkyl, a heterocycle, a aryl or a heteroaryl, or -L-R5, wherein L is selected from C1-C5-alkyl, a cycloalkyl, a heterocycle, a aryl, or a heteroaryl, and R5 is selected from —OH, —CH2OH, —NH2, —COOH, —CONH2, —CONH—R6 or carboxylic acid isosteres, wherein R6 is selected from C1-C4-alkyl, with n, m and r being 0, 1, 2, 3, 4 or 5 and their use.

Abstract: The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other -threonine kinase mediated diseases, having the Formula: (I) wherein A, L, R1, R2, R3, and n are described herein.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein R1, R2, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.

Abstract: The present invention relates to compounds of the formula I or II: (I) (II) processes for their preparation and their use as pharmaceutical agents or compositions in the treatment, of neurological disorders.

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.

Abstract: The present disclosure relates to novel crystalline forms of VX-787, processes for preparation thereof and use thereof. VX-787 is a viral-protein inhibitor drug. The present disclosure provides crystalline form CS1, crystalline form CS2, crystalline form CS3, and crystalline form CS4 of compound (I) hydrochloride. The present disclosure also provides crystalline form CS3 and crystalline form CS9 of compound (I).free form.

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

Abstract: This disclosure is directed to various compounds and methods of preparation of improved compounds that are capable of functioning as cannabinoid receptor 1 (CB1) antagonists with reduced central nervous system (CNS) side effects. The application is also directed to pharmaceutical compositions containing one or more of these compounds, which may also contain one or more additional therapeutic agents. It is also directed to methods of treatment of various conditions that may be responsive to antagonism of the CB1 receptors, including, but not limited to, metabolic syndromes (including liver disease, obesity, and diabetes).

Abstract: Provided is an amino pyrazolopyrimidine compound as represented by the following structural formula used as a neurotrophic factor tyrosine kinase receptor inhibitor. The compound can inhibit the activity of Trk kinase and can treat diseases mediated by a Trk tyrosine kinase receptor in mammals.

Abstract: The invention discloses a type of fused imidazole compound, preparation method and application thereof. The structure of the compound is shown in general formula I. The definition of each group therein is as described in the specification. These compounds are capable of selectively inhibiting indoleamine 2,3-dioxygenase (IDO). The compounds can act as an IDO inhibitor for treating and/or preventing a disease having a pathological feature with IDO-mediated tryptophan metabolic pathways, for example, cancer, eve disease, autoimmune disease, psychological disorder, depression symptom, anxiety disorder and other diseases.

Abstract: The present invention relates to a compound of the general formula (III) or a salt, solvate or prodrug thereof, as well as medical uses involving them, wherein A1, A2, A3, A4, A5, A6, Y, R2 and R7 are as defined herein, and methods for producing such compounds.

Abstract: The invention relates to novel bioactive polycyclic ether compounds comprising a spiro-linked five-membered cyclic imine. In particular, the invention relates to a compound designated portimine, its congeners and the use of these compounds in anticancer therapy. In a second aspect the invention provides a pharmaceutical preparation comprising as active ingredient a congener of the first aspect of the invention. Preferably, the pharmaceutical preparation is indicated for use in the treatment of subjects with neoplasia. More preferably, the pharmaceutical preparation is indicated for use in the treatment of subjects with lymphoid malignancies. Preferably, the lymphoid malignancies are selected from the group consisting of: chronic lymphocytic leukaemia (CLL) and pediatric acute lymphoblastic leukaemia (ALL).

Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: The present invention relates to a thienopyrimidine derivative and use thereof in medicine, and also to a pharmaceutical composition containing the compound. The compound or pharmaceutical composition is used for inhibiting acetyl-CoA carboxylase (ACC). The present invention also relates to a method of preparing such compound and pharmaceutical composition, as well as their use in the treatment or prevention of diseases regulated by acetyl-CoA carboxylase in mammals, especially in humans.

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: The present invention relates to 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.

Abstract: Synthetic methods for the preparation of ligands and metal-ligand complexes are disclosed.

Abstract: A method of making an organoaminosilane compound, comprising i) combining A) a compound comprising a primary or secondary amine, B) monosilane (SiH4), and C) a catalyst, where the catalyst comprises magnesium or boron, where A), B) and C) are combined under sufficient conditions to form the organoaminosilane compound and hydrogen. A method of making a silylamine, the method comprising: i) forming an organoaminosilane compound by i) combining A) a compound comprising a primary or secondary amine, B) monosilane (SiH4), and C) a catalyst, where the catalyst comprises magnesium or boron, and ii) combining ammonia and the organoaminosilane compound produced in i) under sufficient conditions to form a silylamine product and a byproduct, where the byproduct is a primary or secondary amine.

Abstract: New cationic lipids are provided that are useful for delivering macromolecules, such as nucleic acids, into eukaryotic cells. The lipids can be used alone, in combination with other lipids and/or in combination with other transfection enhancing reagents to prepare transfection complexes.

Abstract: The present disclosure provides a phosphorus-containing compound, which includes a structure represented by formula (I). Formula (I) is defined as in the specification. The present disclosure further provides a flame-retardant thermoset made by the phosphorus-containing compound including the structure represented by formula (I). The present disclosure also provides a manufacturing method for the phosphorus-containing compound.