Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.

Abstract: Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.

Abstract: The present disclosure provides a new process for preparing PI3K inhibitor buparsilib. The whole reaction route of the present invention is simple and easy to control for the industrial production.

Abstract: This invention relates to compounds of general formula (I) in which R1, R2, R3, R4, L, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.

Abstract: Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof.

Abstract: The compound N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-5-ethyl-1 -(pyrimidin-5-yl)-1H-pyrazole-4-carboxamide and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, is an inhibitor of RON and can be employed, for the treatment of cancer.

Abstract: The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.

Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.

Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.

Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.

Abstract: 6-Alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer.

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 ROR?. Also provided are pharmaceutical compositions 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: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.

Abstract: This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.

Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract: Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.

Abstract: The present invention provides compounds of Formula III and Formula VI, and processes for their preparation. The present invention further provides use of the compounds of Formula III and Formula VI for the preparation of tofacitinib or isomers or a mixture of isomers or salts thereof.

Abstract: An improved process for the preparation of a key intermediate for the synthesis of the active ingredient Omarigliptin is provided. The key intermediate is a compound having the following formula (I) wherein R1 is propargyl or allyl group and P is an amine protecting group. The compound of formula (I) is prepared by converting a compound of formula (IV) by an amination reaction to a compound of formula (III), which is then protected to provide a compound of formula (II), which is then alkylated to provide the compound of formula (I).

Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.

Abstract: A compound, having the following formula: or resonance form thereof, or salt thereof, or salt of resonance form thereof is provided, wherein R1-R4 and n are defined herein. Compositions and methods including the compound are also provided.

Abstract: Disclosed are a gonadotropin releasing hormone receptor antagonist and a pharmaceutical composition including the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.

Abstract: The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.

Abstract: The present invention relates to a chiral oxamide of formula (I) useful as an intermediate in the preparation of dorzolamide, and to the preparation thereof. The invention also relates to the preparation of dorzolamide, to the hydrochloride salt thereof, and to the active ingredient contained in a drug useful in the treatment of glaucoma, by means of the intermediate of formula (I).

Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.

Abstract: A dual H1/5-HT2A receptor antagonist of the formula: its uses, and methods for its preparation are described.

Abstract: Compounds of Formulae I? and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.

Abstract: The present invention relates to crystalline polymorphs of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), methods of use, and processes of preparing thereof.

Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.

Abstract: Gold(III) complexes with mixed ligands as anticancer agents. The gold(III) cations are coordinated to bidentate ligands having diamino functional groups: a diaminocyclohexane ligand and a 1,3-propylenediamine ligand. The diaminocyclohexane ligand can exist in both cis- and trans-configurations, resulting in isomeric gold(III) complexes. Also described are pharmaceutical compositions incorporating the gold(III) complexes, methods of synthesis, methods of treating cancer and methods of inhibiting cancer cell proliferation and inducing cancer cell apoptosis.

Abstract: The problem addressed by the present invention is to provide; solid solution pigment nanoparticles having a homogeneous solid solution ratio; a method for producing solid solution pigment nanoparticles having a homogeneous solid solution ratio in each primary particle; and a method for controlling the solid solution ratio of solid solution pigment nanoparticles. The solid solution pigment nanoparticles are prepared by precipitating at least two types of pigment by mixing a pigment precipitation solvent and; at least one type of pigment solution wherein at least two types of pigment are dissolved in a solvent: or at least two types of pigment solution wherein at least one type of pigment is dissolved in a solvent.

Abstract: A process for preparing amino acid-modified siloxanes that can be carried out under mild conditions is provided as well as organically modified silicones for care formulations for skin, hair and textiles that are toxicologically unobjectionable.

Abstract: The present invention provides thiophosphates and thiophosphate derivatives useful as antiwear additive components, lubricant additive compositions and lubricant compositions each comprising such compounds, and methods for making and using the same. In one aspect, the invention relates to a compound of formula (I): or a tribologically acceptable salt thereof.

Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process.

Abstract: Platinum(II) complexes having thione-based heterocyclic ligands as anticancer agents. The central platinum atom is coordinated by four of the ligands, each having a five-, six- or seven-membered heterocyclic ring with two nitrogen atoms at positions 1 and 3 of the ring and a thiocarbonyl group at position 2. Pharmaceutical compositions incorporated the platinum(II) complexes, methods of synthesizing the complexes and methods of treating cancers with the complexes or pharmaceutical compositions thereof are also described.

Abstract: A method for preparing isofagomine, its derivatives, intermediates and salts thereof using novel processes to make isofagomine from D-(?)-arabinose and L-(?)-xylose.

Abstract: Method for selective 2-sulfation of glycosides.

Abstract: The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula wherein B, R1, and R2 are as described herein, R3 is —OCH2(OCH2)n—O-L1-[D1], in which L1 is an ethylene group, wherein hydrogen atoms besides a hydrogen atom bonded to the ?-position relative to [D1] are optionally substituted by a straight chain or branched alkyl group, n is a positive integer, and [D1] is an electron-withdrawing group.

Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.

Abstract: Provided are compounds of Formula I, as well as pharmaceutical compositions containing compounds of Formula I and methods for treating Orthomyxoviridae virus infections by administering these compounds. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.

Abstract: A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures.

Abstract: The current invention reports a method for the purification of a not-glycosylated, heterologous polypeptide, which has been recombinantly produced in a prokaryotic cell, wherein the method comprises three chromatography steps of which the first chromatography step selected from i) hydrophobic charge induction chromatography, or ii) hydrophobic interaction chromatography, or iii) affinity chromatography, or iv) ion exchange chromatography, the second chromatography step is selected from i) anion exchange chromatography, or ii) cation exchange chromatography, or iii) hydroxylapatite chromatography, or iv) hydrophobic interaction chromatography, and the a third chromatography step is selected from i) hydrophobic charge induction chromatography, or ii) anion exchange chromatography, or iii) cation exchange chromatography, or iv) hydrophobic interaction chromatography, whereby the first chromatography step is an affinity chromatography in case of polypeptides capable of interacting with metal ligands, the second c

Abstract: The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an ?-oxoacyl aminocaprolactam derivative that is represented by formula (I) (in the formula, X is —O— or —N(R1)— and R1 represents an alkoxycarbonyl group having 1-10 carbon atoms); and a bone resorption inhibitor containing the ?-oxoacyl aminocaprolactam derivative.

Abstract: The disclosure includes novel processes for producing Sovaprevir comprising adding compound E to F-1 to provide Sovaprevir. The disclosure further includes intermediates useful for producing Sovaprevir. The disclosure also include a novel crystalline form of Sovaprevir, Form F, and a method for preparing spray-dried amorphous Sovaprevir from crystalline Form F.

Abstract: Novel compounds, particularly derivatives of boroarginine, boroornithine and borolysine that selectively modulate, regulate, and/or inhibit enteropeptidase. Compositions, particularly pharmaceutical compositions, as well as methods to treat excess weight, obesity and diseases associated with an abnormal fat metabolism.

Abstract: Disclosed is an evaluation peptide for evaluating the efficiency of a pretreatment in the quantification of a protein using a mass spectrometer, having high reliability and high general versatility. Also disclosed is an artificial standard protein comprising the evaluation peptide. Further disclosed is a method for quantifying a protein utilizing the artificial standard protein. Specifically disclosed is a method for selecting a peptide which consists of an amino acid sequence not agreeing with that in a naturally occurring protein and a variant thereof and capable of being detected by mass spectrometry and which has an amino acid that can be recognized by a protein-digesting enzyme, and using the peptide as an evaluation peptide for use in the quantification of a protein by a mass spectrometer.

Abstract: The present invention relates to pharmaceutically and/or diagnostically active compounds, in particular peptide analogs (peptidomimetics), which can be reversibly controlled between an active and an inactive state by irradiation with light of different wavelengths. The present invention further relates to an intermediate compound usable in the manufacture of such pharmaceutically and/or diagnostically active compounds, as well as a manufacturing method thereof.

Abstract: The invention relates to a novel class of self-assembling peptides, compositions thereof, methods for the preparation thereof and methods of use thereof. The invention also encompasses methods for tissue regeneration, increasing the production of extracellular matrix proteins, and methods of treatment comprising administering self-assembling peptides.

Abstract: A fusion protein for use as an immunogen enhancer for enhancing antigen-specific T cell responses is disclosed. The fusion protein comprises: (a) an antigen-presenting cell (APC)-binding domain or a CD91 receptor-binding domain; (b) a protein transduction domain; and (c) an antigen of a pathogen, wherein the APC-binding domain or the CD91 receptor-binding domain is located at the N-terminus of the fusion protein, and the antigen of the pathogen is located at the C-terminus of the protein transduction domain. The protein transduction domain is selected from the group consisting of: (i) a fusion polypeptide, comprising a T cell sensitizing signal-transducing peptide, a linker, and a translocation peptide; (ii) a T cell-sensitizing signal-transducing peptide; and (iii) a translocation peptide of 34-112 amino acid residues in length.