Abstract: Described herein are compounds, including pharmaceutically acceptable salts thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat, prevent or diagnose blood-based diseases, disorders or conditions.

Abstract: The present invention relates to a maleate salt of a compound represented by formula I, a method for preparing the salt, a pharmaceutical composition containing the salt, and the use of the salt. The present invention also relates to crystalline forms C, D and E of the maleate salt of the compound represented by formula I, methods for preparing the crystalline forms, crystalline compositions and pharmaceutical compositions containing the crystalline forms, and uses thereof.

Abstract: Described herein are compounds, such as compounds of Formula (I) and pharmaceutically acceptable salts thereof, that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions, e.g.

Abstract: Disclosed are an EGFR inhibitor free base or acid salt polycrystalline form, a preparation method therefor, and an application thereof. The present invention specifically relates to an N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide free base or acid salt polycrystalline form, a preparation method therefor, and an application of the polycrystalline form in preparing a drug for treating an EGFR mutant activity-mediated disease. The present invention is used for inhibiting the activity of an L858R EGFR mutant, a T790M EGFR mutant and an exon 19 deletion activating mutant etc., may be widely applied in preventing and treating cancer, especially non-small cell lung cancer and other related diseases, and is expected to develop into a new generation of EGFR inhibitors.

Abstract: The invention provides a compound having a GLUT9 inhibitory activity. The compound is of Formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: A hair growth formulation includes minoxidil and foeniculum vulgare, atriplex nummularia extract, or a combination of foeniculum vulgare and atriplex nummularia extract. A method for increasing hair growth includes applying a hair growth formulation to a subject.

Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

Abstract: The present invention provides methods of treating MS using pyrimidine and pyridine compounds which are inhibitors of Bruton's tyrosine kinase (BTK).

Abstract: Described herein are methods and pharmaceutical formulations for treating ocular conditions.

Abstract: The pyrimidine derivatives as anti-diabetic agents are chloropyrimidinyl derivatives having the general formula of compound 81, wherein R1 is —N(CH3)CH2CH2OH (compound 81c) or —N(H)CH2CH2OH (compound 81f) or the general formula of compound 82, wherein R2 is —N(CH3)CH2CH2OH (compound 82c) or —N(CH2CH2)2O (compound 82d), as follows: The derivatives may be used for treating diabetes in humans or animals and have demonstrated efficacy, specifically in treating type 2 diabetes. Two methods of synthesizing the pyrimidine derivatives are described herein. The method using microwaves (Method B) is a green method that can provide high yields in a short time and with high purity. The compounds act as GLP-1 receptor agonists and are more potent than conventional drugs. As such, the compounds may be used in lower doses, and, hence, have fewer side effects.

Abstract: The present invention falls within the field of medical technology, and in particular relates to the use of a compound as shown in formula (I). In particular, the present invention relates to the use of the compound as shown in formula (I) in the preparation of a pharmaceutical composition for preventing and/or treating a nerve injury, or relieving a nerve injury-associated symptom, and further relates to the use thereof in the preparation of a healthcare product for protecting an injured nerve and/or improving motor function. After a nerve injury has occurred, the compound can reduce the production of pro-inflammatory cytokine, decrease the level of apoptosis, promote the survival of neuron, inhibit the formation of glial scar, and has a significant effect in promoting the recovery of motor function.

Abstract: The present disclosure provides the use of Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10 in methods and compositions for the treatment of neurological disorders and stress-induced conditions. Methods of increasing the levels of 5Thr3a on neuronal cells is also provided by contacting the neuronal cells with Akr1b8, an agonist of Akr1b8, Akr1B10, or an agonist of Akr1B10.

Abstract: A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.

Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.

Abstract: A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, 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: The present disclosure relates to methods of retarding hair loss or facilitating hair growth and/or regrowth. More specifically, the present disclosure relates to methods of using the disclosed compositions to increase the rate of terminal hair growth and/or regrowth in a mammal.

Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

Abstract: Described herein are methods and compositions for the treatment of ocular conditions and for the improvement of vision parameters using pharmaceutically acceptable ophthalmic pilocarpine formulations. A nonlimiting example of an ocular condition that may be treated with the methods and compositions disclosed herein is presbyopia.

Abstract: Disclosed herein are compounds, of the class of amine-bearing heterocycles, which act as positive allosteric modulators and silent allosteric modulators of the mu opioid receptor. These compounds are useful for the treatment of pain, drug addiction, and other CNS derived maladies that are controlled directly or indirectly by activation of the mu opioid receptor. Methods for making and using the allosteric modulators disclosed herein are also provided.

Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.

Abstract: The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, pharmaceutical compositions containing the same, processes for preparing the same, and methods of medical treatment using the same.

Abstract: The present invention is directed to novel protein kinase inhibitors comprising the chemical compound N-(2-chloro-6-methylphenyl)-2-[[2-methyl-6-(3-hydroxypyrrolidin-1-yl)pyrimidin-4-yl]amino]thiazole-5-carboxamide, its pharmaceutically acceptable salts, enantiomers, and enantiomeric mixtures, and methods of use to treat protein kinase-mediated diseases or conditions.

Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Abstract: Disclosed herein are combination therapies for the treatment of heart failure using a cardiac myosin activator, such as omecamtiv mecarbil, and a sinus node If current inhibitor, such as ivabradine. Also disclosed herein are compositions comprising a cardiac myosin activator and a sinus node If current inhibitor.

Abstract: The present invention provides a compound of Formula II, and salts thereof, and a pharmaceutical composition comprising a compound of Formula II: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, and wherein R3 is hydrogen, an alkyl group having from one to ten carbon atoms, or a halogen. Preferably the compound of Formula II includes wherein R3 is a halogen, and most preferably wherein the halogen is chlorine. Methods of treating a patient with cancer with these compounds are also provided.

Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.

Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.

Abstract: Indazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease states associated with glutamate dysfunction.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

Abstract: The present invention relates to a novel pyrimidine-4-carboxylic acid derivative having an anticancer activity, and the compound thereof is useful as a drug for treating and preventing tumor diseases, wherein the compound is represented by the Formula 1: or a pharmaceutically acceptable salt thereof, wherein: Q is a C6-C15 aryl group; or a C4-C13 heteroaryl group, wherein the heteroaryl contains 1, 2 or 3 heteroatoms substituted with 1-3 heteroatom(s) selected from the group consisting of nitrogen, oxygen or sulfur; R is a halogen; a C1-C10 haloalkyl substituted with 1-13 halogen atom(s); a C1-C10 alkoxy; a 5- or 6-membered heterocycloalkyl or (CH2)r-R1 wherein the heterocycloalkyl contains 1-2 heteroatom(s) selected from the group consisting of nitrogen and oxygen; R1 is a hydrogen; a C1-C10 alkoxy; amino; mono(C1-C10 alkyl)amino; di(C1-C10 alkyl)amino; or —NHC(O)-phenyl; n is 1, 2, 3, 4, 5, or 6; and r is 0, 1, 2, 3, 4, 5, or 6; and m is 0, 1, 2 or 3.

Abstract: The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.

Abstract: This disclosure provides solid forms of 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide, and methods of manufacturing and using these forms.

Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I) or any one of Compounds 100-175) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.

Abstract: The current disclosure relates to methods for treating pancreatic cancer or chronic pancreatitis in a subject comprising administering an antagonist of a dopamine receptor to the subject wherein the dopamine receptor is, in some specific cases dopamine receptor D2 (DRD2). The antagonist in some specific cases is an RNAi construct, an antibody, or a small molecule and in more specific cases pimozide or L-741,626. The disclosure also relates to diagnostic methods comprising the detection of the expression of DRD2 in pancreatic tissue and kits for doing the same.

Abstract: The present invention relates to novel polymorph of riociguat and process for preparing the polymorph. The present invention also relates to the improved process for the preparation of riociguat.

Abstract: An oral disintegrating tablet which contains rosuvastatin or a salt thereof and is stable to light is provided. An oral disintegrating tablet stable to light, temperature and humidity can be provided by preparing a multi-layered tablet containing rosuvastatin or a pharmaceutically acceptable salt thereof as an active ingredient, a light stabilizer, and an inorganic salt or a basic oxide.

Abstract: Amine substituted pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.

Abstract: A method to prepare a catheter locking formulation, comprising in a first step, dissolving trimethoprim in propylene glycol at a temperature greater than room temperature, and in a final step, adding absolute ethanol at about room temperature to a solution of trimethoprim, propylene glycol, EDTA Calcium Disodium Hydrate, phosphate buffered saline, and glycerin.

Abstract: Solid forms of Compound I (and its S-enantiomer, Compound II), active on protein kinases, were prepared and characterized: Also provided are methods of using the solid forms.

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts 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: The present invention relates to novel pyrazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for controlling harmful microorganisms in crop protection and in the protection of materials. Further, the present invention also relates to certain intermediates useful for producing said novel pyrazole derivatives.

Abstract: The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, pharmaceutical compositions containing the same, processes for preparing the same, and methods of medical treatment using the same.

Abstract: The present invention provides methods for treating and/or preventing mucositis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.

Abstract: Derivatives of licofelone for the treatment of chronic inflammatory diseases and epithelial cancers associated with chronic inflammation are disclosed. The agents target mPGES-1 and 5-LOX.

Abstract: Described herein are compounds, such as compounds of Formula (I) and pharmaceutically acceptable salts thereof, that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions, e.g.

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1-R6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. 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 TAF1-mediated disorders.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: A pesticidal composition comprises a compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R4, R5, R6, R7, Z, Q, and Y are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests, or to an area to control pests.