Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: The present invention provides cells which have a high ability to propagate influenza virus, are suitable for use in production of an influenza virus for preparing a vaccine, and are able to be cultured in vitro, and a method for producing an influenza virus using the cells. That is, the present invention provides cells for producing an influenza virus in which expression of one or more genes that encode proteins involved in an effect of suppressing influenza virus production in a cell is suppressed and the gene is at least one selected from the group including ACTG1 gene and the like, and a method for producing an influenza virus that includes infecting the cells for producing an influenza virus with an influenza virus and then culturing.

Abstract: Provided herein is a method of treating, preventing, or alleviating one or more symptoms of Chagas disease in a subject, comprising administering to the subject: (i) ascorbic acid, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof; (ii) a quinone compound, or a single enantiomer, a mixture of enantiomers, or a mixture of diastereomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof; and (iii) an antiparasitic agent.

Abstract: Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.

Abstract: Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.

Abstract: Provided herein are compounds that are broad-spectrum protein kinase binding agents, detectable tracers comprising such compounds, and method of use thereof for the detection of protein kinases.

Abstract: Compositions and methods for treating cardiovascular diseases and dyslipidemias are provided. The compositions can inhibit Wnt signaling and can reduce inflammation. The levels of cholesterol can be reduced when the compositions are administered to a subject, such as a human.

Abstract: This invention relates inter alia to novel imidazoquinoline derivatives and their use in therapy, particularly as vaccine adjuvants.

Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.

Abstract: The invention provides novel pyridylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory disease, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R1, R2, R3 and X are as defined in the specification.

Abstract: Disclosed herein, inter alia, are compositions and methods for modulating Ras and treating cancer.

Abstract: The present invention provides novel compounds of formula (Ia) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases, or cholestatic diseases.

Abstract: Disclosed herein are a compound of formula (I) and a preparation method and uses thereof. The compound shows a good inhibitory activity against ROCK, providing a new medicinal strategy to clinically treat the diseases associated with abnormal ROCK activity.

Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, and G, are defined herein.

Abstract: Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R1, R2 and R4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

Abstract: The present application relates to mass spectrometry methods for use in identifying proteins or other biomolecules which are bound irreversibly by test compounds.

Abstract: The present invention provides compounds of Formula (I): (Formula (I)), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are inhibitors to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ?v-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

Abstract: The present invention relates to methods for treating melanoma with apilimod and related compositions and methods.

Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R23, R24, L, A and B are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.

Abstract: The present disclosure relates to methods for preventing or treating a radiation-induced disease, disorder, or condition by administering apilimod to a subject in need thereof, and related compositions.

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: A diphenylaminopyrimidine and triazine compound of Formula I, or a pharmaceutically acceptable salt, stereoisomer, hydrate or solvate thereof is disclosed In formula I, A is C or N; X and Y are independently selected from hydrogen, halo, cyano, trifluoromethyl, alkoxy, alkyl, aryl, alkenyl, alkynyl and nitro; or X and Y, together with the atoms to which they are attached, form a phenyl or an heteroaromatic ring; R1 is R2 is CD3 or CD2CD3; R3 is R4 is hydrogen, methyl, trifluoromethyl, cyano or halo; R5 is hydrogen, alkyl, substituted and unsubstituted phenyl, allyl or propargyl; R6 and R7 are independently selected from hydrogen, alkyl, substituted and unsubstituted phenyl, allyl and propargyl; or R6 and R7, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heterocycloalkyl group. The compound has pharmacodynamic and pharmacokinetic properties and ALK kinase inhibitory activity.

Abstract: Disclosed is a compound for treating fibrosis-related diseases, and specifically disclosed are the compound represented by formula (I) and a pharmaceutically acceptable salt thereof.

Abstract: Provided herein is a method of preventing hair loss or promoting hair growth, the method including administering an effective amount of a PDE 3 inhibitor. More particularly, when the method of the present disclosure is used, an excellent hair loss prevention or hair growth promotion effect is obtained by inhibiting the activity of PDE 3.

Abstract: Subject-matter of the invention is a process for the preparation of key intermediates in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.

Abstract: The present invention provides pyrroles having hypolipidemic hypocholesteremic activities. The invention provides saroglitazar and its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof. The invention also provides a process for the preparation of saroglitazar. The invention further provides intermediates as well process for preparation thereof.

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

Abstract: The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula: where R1, R2, R2?, R3, R4, X1, X2, X3, X4, Q, and n are described herein.

Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

Abstract: The present invention relates to amide derivatives having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Abstract: To provide a compound highly active against pests, a pesticide using the compound, and a method for controlling pests by applying the compound. A phenoxyalkylbenzamide compound represented by the formula (I) or its salt; a pesticide containing it as an active ingredient, and a controlling method, which comprises applying an effective amount of the compound: wherein R1, Y and R3 are a hydrogen atom or the like, and Ar is as follows: wherein R4 and R7 are halogen or the like, R5 and R6 are a hydrogen atom or the like, m is from 0 to 5, and n is from 0 to 3.

Abstract: The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, R3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA2 enzyme.

Abstract: Provided herein are compositions and methods for the treatment of obesity and related disorders, including, but not limited to insulin resistance, diabetes, and hepatic steatosis. For example, in some embodiments, pharmaceutically acceptable compositions and methods are provided employing amlexanox, a derivative thereof, or a pharmaceutically acceptable salt thereof, alone or in combination with other agents and/or medical interventions, for the treatment, prevention, and management of such diseases and conditions.

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

Abstract: This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.

Abstract: The present invention relates to an improved process for the preparation of pyrroles derivatives having hypolipidemic and hypocholesteremic activities. In particular, the invention relates to an improved process for the preparation of 2-ethoxy-3-(4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)phenyl)propanoate and its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof. The invention also relates to an improved process for the preparation of mesylate compound (A1).

Abstract: Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and Francisella tularensis. The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics.

Abstract: The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, autoimmune, allergic, and degenerative disorders. In particular, the presently disclosed compounds are Syk inhibitors.

Abstract: The present invention concerns compounds of formula (I) or an N-oxide or salt thereof and their use for controlling parasites in and on warm-blooded animals or fish.

Abstract: The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (Pis) and/or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.

Abstract: Heteroaryldihydropyrimidine (HAP)-based fluorescent stains (compounds), as well as uses of such stains as diagnostic reagents, viral-tracking agents, and/or tools for drug discovery are described. The present invention relates to heteroaryldihydropyrimidine (HAP)-based fluorescent stains (compounds), as well as uses of such stains as diagnostic reagents, viral-tracking agents, and/or tools for drug discovery.

Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: The present invention provides a polysubstituted pyridine compound of Formula I, a preparation method, a use and a pharmaceutical composition thereof. The polysubstituted pyridine compound of Formula I according to the present invention has an excellent anti-tumor effect, can inhibit various cell kinases simultaneously, has significantly excellent pharmacokinetic characteristics, and is very suitable for oral and intravenous administration. The pharmaceutical composition according to the present invention can be useful for treating tumors and cancers.

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

Abstract: A compound represented by the general Formula (I), wherein hydrogen atoms shown as attached to pyrazole and benzimidazole rings are attached to one of nitrogen atoms of the pyrazole or benzimidazole ring, respectively; R1 represents —X-Q-P, wherein X is absent or represents —CH2—, —C(O)—, or —C(O)NH—(CH2)k—, wherein k is 0, 1 or 2; Q is selected from the group consisting of Q1, Q2, Q3, Q4 and Q5; P is absent or represents straight- or branched-chain C1-C3 alkyl, —(CH2)l—NR2R3, or —(CH2)m—C(O)—NR2R3, wherein l and m independently of each other represent 0, 1 or 2, with the proviso that when B in Q1 represents oxygen atom, then P is absent; and R2 and R3 independently represent C1 or C2 alkyl, or R2 and R3 together with nitrogen atom to which they are both attached form a 6-membered saturated heterocyclic ring, wherein one of carbon atoms can be replaced with oxygen, —NH— or —N(C1-C2)alkyl-; and acid addition salts thereof. The compound can be useful in the treatment of cancer diseases.

Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.

Abstract: Described herein are certain crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). Also described are methods of treating and/or preventing diseases using the crystalline forms or pharmaceutical compositions described herein.

Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2 R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

Abstract: The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.