Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.

Abstract: Provided are a crystalline form A of 2-[(2R)-2-methyl-2-pyrrolidyl]-1H-benzimidazole-7-carboxamide dihydrochloride and the preparation method and use thereof. The X-ray powder diffraction pattern of crystalline form A shows characteristic peaks at 2theta values of 8.3°±0.2°, 26.7°±0.2°, 16.1°±0.2°. Crystalline form A, compared with the existing crystalline forms, has a surprisingly excellent solubility, mechanical and storage stabilities and particle size distribution, is a more ideal crystalline fotbnn compared with the prior art forms, better satisfies medicinal requirements, and plays an important role in future optimization and development of the drug.

Abstract: Described herein are polymeric nanoparticles that include a therapeutic agent which is 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide (also known as AZD1152 hqpa) or a pharmaceutically acceptable salt thereof, and methods of making and using such therapeutic nanoparticles.

Abstract: The present invention relates to small molecule4-(piperazin-1-yl)quinazolin-2-amino compounds with formula (I) useful for inhibiting signalling by certain toll-like receptors (TLRs), especially TLR9. Toll-like receptors (TLRs) are members of the larger family of evolutionarily conserved pattern recognition receptors which are critical first line of defence for self-nonself discrimination by the host immune response. Aberrant TLR9 activation is implicated in autoreactive inflammation in different autoimmune diseases. The invention depicts compounds with formula (I), composition and methods can be used in a number of clinical applications, including as pharmaceutical agents and methods for treating conditions involving unwanted immune activity due to TLR9 activation.

Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, Cy and Y are defined herein, which are suitable for the treatment of diseases related to BTK, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.

Abstract: Disclosed are compounds of formula (I), pharmaceutical compositions comprising such compounds and methods/uses of using the same, for example, for treating a JAK-related disorder, such as cancer, cancer cachexia or an immune disorder: wherein R1 is methyl or ethyl; R2 is selected from methyl, ethyl, methoxy and ethoxy; R3 is selected from hydrogen, chlorine, fluorine, bromine and methyl; R4 is selected from methyl, ethyl and —CH2OCH3; R5 and R6 are each individually methyl or hydrogen; and R7 is selected from methyl, ethyl, —(CH2)2OH and —(CH2)2OCH3, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formulae I or Formula II: where R, L, X1, X2, X3, X4, X5, Y1, Y2, Y3, and Y4 are described herein.

Abstract: The present invention relates to a novel compound having a GPR119 agonistic activity, a method for preparing the same, and a pharmaceutical composition including the same as an effective component. The present invention has an effective hypoglycemic action and an effect on pancreatic beta cells, and also improves lipid metabolism which is a chronic cardiovascular risk factor, thereby having a treatment and/or prevention effect of a metabolic disease such as diabetes.

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 invention relates to fungicidal N-cycloalkyl-N-[(heterocyclylphenyl)methylene] carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides; particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract: The present invention relates to novel crystalline forms of compound (I), (3-Amino-oxetan-3-ylmethyl)-[2-(5,5-dioxo-5,6,7,9-tetrahydro-5lambda*6*-thia-8-aza-benzocyclohepten-8-yl)-6-methyl-quinazolin-4-yl]-amine and pharmaceutical compositions comprising the crystalline forms thereof disclosed herein, which may be used for the treatment or prophylaxis of a viral disease in a patient relating to respiratory syncytial virus (RSV) infection or a disease caused by RSV infection.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, B R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.

Abstract: Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyrldine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity.

Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: Provided herein is a compound, 1-(4-(3-amino-[1,2,3]triazolo[1,5-a]pyridin-4-yl)phenyl)-3-(3-chlorophenyl)urea, pharmaceutical compositions thereof, and crystal forms thereof. Also provided are particles (e.g., nanoparticles) comprising the compound, and pharmaceutical compositions thereof, that are mucus penetrating. Also provided herein are methods and kits for using the compound, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.

Abstract: The present invention relates to crystalline forms of a diazabicyclooctane derivative represented by Compound I, the process for producing the same and methods for using the same:

Abstract: The present invention provides a medicament useful for treatment and/or prevention of cancer, a vaccine adjuvant, and an inhibitor of immune checkpoint comprising a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein Bonds a-d, Ring A, R1, R1?, R2, R2?, R3-R8, and n are as defined in the present specification.

Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract: The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.

Abstract: A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.

Abstract: The present disclosure provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R7 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient. In another embodiment, these compounds are useful for treating respiratory dysfunction in patients by administering one or more of the compounds to a patient.

Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.

Abstract: The present invention provides a compound of Formula (I) including pharmaceutically acceptable salts thereof: and therapeutic uses of these compounds. The invention further provides pharmaceutical compositions comprising these compounds, compositions comprising these compounds with a therapeutic co-agent, and methods of using the compounds and compositions to treat viral infections.

Abstract: Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: A method for producing 1,4:3,6-dianhydrohexitols, including the steps of: a) supplying at least one hexitol, b) dehydrating the hexitol, and c) distillating the dehydration product produced in step b), wherein: the hexitol is supplied in the form of an aqueous solution in step a); and the distillation is carried out by means of a thin-film evaporator in step c).

Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.

Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.

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: A compound of formula Ia, Ib, Ic or Id: wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2 OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2 OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(?O)NH2, and —CH2 OH; R4b is either H or Me; R5 is either H or Me; m is 1 or 2; q is 0 or 1; R11a, R11b, R11c and R11d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH—C1-4 alkyl and cyano; R12a and R12b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2 OH; R12c and R12d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2 OH; R12e is H or Me; R13a and R13b are independently selected from H and Me; R14 is either H or Me; R16a

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The disclosure relates to compounds of formula (I) and pharmaceutically acceptable salts, and compositions thereof, wherein the substituents are as defined herein. Also provided are methods of making compounds of formula (I), and methods involving the compounds or compositions for treating disorders and diseases described herein.

Abstract: The invention provides heterobicyclic pyrimidinone compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary heterobicyclic pyrimidinone compounds described herein include 6-oxo-3,4-dihydro-2H,6H-pyrimido[2,1-b)][1,3]thiazine-7-carboxamide compounds.

Abstract: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is LY; each L is a direct bond, C1-C10 alkylene, C2-C10 alkenylene or C2-C10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R3 is independently H, C1-C10 alkyl, halogen, fluoro C1-C10 alkyl, O—C1-C10 alkyl, NH—C1-C10 alkyl, S—C1-C10 alkyl, O-fluoro C1-C10 alkyl, NH-acyl, NH—C(O)—NH—C1-C10 alkyl, C(O)—NH—C1-C10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110?, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.

Abstract: There are provided 5,6-dihydro-4H-dithieno[3,2-b:2?,3?-d]azepine derivatives (as defined in the disclosure) which are useful in the treatment of RSV infection and for the prevention of disease associated with RSV infection.

Abstract: The present invention is directed to crystalline vinorelbine monotartrate and its use for the prevention and treatment of cancer, particularly non-small cell lung cancer or breast cancer. The present invention also relates to a corresponding method for the manufacture of crystalline vinorelbine monotartrate.

Abstract: The present invention refers to a process for removing Cs, and optionally Rb, from aqueous fluids including body fluids by fluorine containing reagents, the synthesis of fluorine containing, water-insoluble salts of said Cs isotopes and their use as therapeutic agents.

Abstract: A method of separating a metal organic framework (MOF) from a solution and associated apparatus. The method comprises: providing a MOF containing solution; contacting the MOF containing solution with an acoustic reflector surface such that, any high frequency ultrasound applied within the MOF containing solution reflects off the acoustic reflector surface; and applying a high frequency ultrasound of at least 20 kHz to the MOF containing solution. The MOF material is substantially separated from solution as aggregated sediment that settles out of solution.

Abstract: The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.

Abstract: Provided are phosphonopyrazole-based phosphohistidine analogs that are useful as haptens for the preparation of immunogens, immunogens that include these haptens linked to carrier molecules, antibodies thereto and uses of these antibodies, haptens, immunogens and phosphohistidine analogs.

Abstract: A Formula of a phosphorous fire-retardant hardener having fire-retardant and heat-resistant properties as well as a low-dielectric constant. With a preparation of glass-fiber laminated board, the hardener meets UL-94V fire-retardant requirements and has a dielectric constant 5 of 4.0 (1 GHz).

Abstract: Provided are an organic metal complex, its preparation method and light-emitting element containing the complex. The organic metal complex is selected from compounds shown as general formula I and combinations thereof. The ligand containing pyridine unit is introduced into the cyclometalated iridium(III) organic metal complex, and the obtained iridium(III) heterocomplex has a luminous range from near-infrared light to blue light, so that the ppz-Ir structure, which is originally non-luminous, can emit light at room temperature with advantages of wide application scope of spectrum and low cost of massive production.

Abstract: An example of a fusing agent includes a metal bis(dithiolene) complex, a thiol surfactant, a polar aprotic solvent, and a balance of water. In an example of a method of making the fusing agent, the metal bis(dithiolene) complex is exposed to an aqueous solution including a reducing agent and a thiol surfactant to form a reduced metal bis(dithiolene) complex and to dissolve the reduced metal bis(dithiolene) complex in the aqueous solution. The aqueous solution is incorporated into a vehicle including a water soluble organic solvent and an additive selected from the group consisting of an emulsifier, a surface tension reduction agent, a wetting agent, a scale inhibitor, an anti-deceleration agent, a chelating agent, an antimicrobial agent, and a combination thereof. The fusing agent may be utilized in a three-dimensional printing method and/or incorporated into a three-dimensional printing system.

Abstract: The present invention provides a novel, simple and reliable method for the separation of carbohydrate tautomers. The method comprises steps of chromatographically separating a sample using a chromatographic device. The method can be used to separate mono- and disaccharides tautomeric species including arabinose, xylose, fructose, mannose, galactose, glucose, lactose, and maltose.

Abstract: The present invention discloses a method for preparing sucralose-6-acetate in a biphasic liquid-liquid system. The method comprises slowly dropwise adding an inert non-polar solvent containing a chlorinating agent to an N,N-dimethyl formamide (DMF) solution of sucrose-6-acetate; then reacting the biphasic liquid-liquid mixture at a certain temperature for 9-20 hours; cooling the system to room temperature after stopping heating, and settling the solution to form layers, an upper layer being an inert non-polar solvent layer, and a lower layer being a DMF solution layer containing the product; hydrolyzing, neutralizing, and filtering the lower layer to obtain a filtrate, and then concentrating the filtrate to obtain a concentrate; dissolving the concentrate in water, and obtaining the product by extraction using ethyl acetate and crystallization, the inert non-polar solvent being an alkane solvent containing 8-18 carbon atoms that is not mutually soluble with DMF.

Abstract: The invention relates to a compound of general formula (I), and to the use thereof in medicine, or for the production of a medicament for the treatment of different diseases, preferably a cancer such as melanoma, lung carcinoma or breast cancer. For this purpose, the invention also relates to a pharmaceutical composition comprising said compound. In addition, the invention relates to a method for producing the compound of general formula (I).

Abstract: A method for producing P1,P4-di(uridine 5?-)tetraphosphate (UP4U) that can avoid reduction of the synthetic efficiency without using UTP free is developed. A method for producing UP4U comprising reacting a phosphoric acid-activating compound represented by formula [II] or [III] with a phosphoric acid compound selected from the group consisting of UMP, UDP, UTP and a pyrophosphoric acid or a salt thereof (excluding UTP free) in water or a hydrophilic organic solvent, in the presence of a metal ion selected from the group consisting of an iron (II) ion, an iron (III) ion, a trivalent aluminum ion, a trivalent lanthanum ion, and a trivalent cerium ion. where, in the formula [II], R1 represents a uridyl group binding to the 5?-position, X represents a heterocyclic group, and n represents an integer of 1 or 2, where, in the formula [III], X represents a heterocyclic group selected from the group consisting of an imidazolyl group, a benzimidazolyl group, and a 1,2,4-triazolyl group.

Abstract: The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.