Abstract: The present invention is related to processes for preparing a composition comprising an enantiomeric excess of a substituted pyrrolo[2,3-d]pyrimidine utilizing chiral acids.

Abstract: The present disclosure is directed to polymorph Form 1 of 1H-pyrazole-1-propanenitrile, ?-(cyclopentyl-2,2,3,3,4,4,5,5-d8)-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (?R)-, phosphate (1:1) (deuruxolitinib phosphate). Also disclosed are methods of treatment using polymorph Form 1 of deuruxolitinib phosphate and methods of making polymorph Form 1 of deuruxolitinib phosphate.

Abstract: The present disclosure provides crystalline forms of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl)azetidin-3-yl)acetonitrile, pharmaceutical compositions comprising the crystalline forms, methods of using the crystalline forms, and processes for making the crystalline forms.

Abstract: This disclosure relates to JAK1 pathway inhibitors and the use thereof in treating gastrointestinal diseases or disorders such as ulcerative colitis.

Abstract: Disclosed is a method of treating in a subject hair loss disorders that are beneficially treated by administering a JAK1 and/or JAK2 inhibitor. The method comprises administering to the subject an amount in the range of about 4 mg to about 50 mg of Compound (I): or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising Compound (I) and the use of such compositions in the described methods.

Abstract: There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.

Abstract: Pyrrolo[2,3-d]pyrimidine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[2,3-d]pyrimidine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: The present application provides deazaguaine compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.

Abstract: Disclosed is a JAK1 and/or JAK2 inhibitor of the following structural formula: or a pharmaceutically acceptable salt thereof. This invention also provides pharmaceutical compositions comprising a compound of Formula (I), optionally including additional therapeutic agents, and use in methods of treatment for hair loss disorders.

Abstract: The present invention provides a novel compound inhibiting EGFR or a salt of the compound. According to one embodiment of the present invention, provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

Abstract: The present invention relates to methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.

Abstract: Described herein are Janus kinase (JAK) inhibitors of the Formula (I?): and methods of utilizing JAK inhibitors of the Formula (I?) in the treatment of diseases, disorders, or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract: The present invention provides: industrially desirable and novel optically-active cyclopentenone derivatives; and a novel industrial manufacturing method. The novel optically-active cyclopentenone derivatives and method for manufacturing the same are, respectively: an intermediate for industrially desirable and novel prostaglandin derivatives and the like; and a method for manufacturing the same. It is expected that the present invention will be commercialized and industrialized.

Abstract: Provided herein are methods of treating focal segmental glomerulosclerosis, said methods include administering to a subject in need thereof a therapeutically effective amount of a CCR2 antagonist. In some embodiments, the CCR2 antagonist is used in monotherapy. In some embodiments, the CCR2 antagonist is used in combination therapy. In some embodiments, the additional therapeutic agent is a RAAS blocker and/or an endothelin receptor inhibitor. The CCR2 antagonist may have the structure of formula (I).

Abstract: The present invention relates to a compound represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, and the compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions: wherein: R1 is pyrazolyl, isooxazolyl, isothiazolyl, phenyl, or benzothiazolyl, wherein the pyrazolyl, isoxazolyl, isothiazolyl, phenyl, or benzothiazolyl is optionally substituted with one Ra substituent; R2 is H, halogen, CN, or C1-5 alkyl; and Ra is C1-5 alkyl, C1-5 haloalkyl, C1-5 hydroxyalkyl, C3-6 cycloalkyl, tetrahydropyranyl, piperidinyl, or morpholino.

Abstract: Disclosed herein are methods for treating an individual having a Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) infection. The method may comprise administering a JAK inhibitor, for example ruxolitinib (JAKAFI®), to an individual in need thereof, such individual generally being an individual having, or suspecting of having, SARS-CoV-2 infection. The individual in need thereof may be an individual having, or suspected of having or at risk for developing SARS-CoV-2 infection-related cytokine storm. The individual in need thereof may further be an individual having, or suspected of having SARS-CoV-2 infection-related pneumonia.

Abstract: Disclosed are cyclic-di-nucleotide cGAMP analogs, methods of synthesizing the compounds, pharmaceutical compositions comprising the compounds thereof, and use of compounds and compositions in medical therapy.

Abstract: The present invention provides methods of treatment for hematological malignancies involving synergistic combination of a JAK2 inhibitor and a glucocorticoid or a JAK2 inhibitor, thalidomide or thalidomide derivative, and a glucocorticoid. The compositions and methods provide an unexpected efficacy in the treatment for hematological disorders. The hematological disorders treated by the current invention include multiple myeloma, and may also include hematological disorders that are refractory to prior cancer treatments, or a relapsed hematologic disorder.

Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

Abstract: The present invention relates to a novel pyrrolo-pyrimidine derivative compound, a preparation method therefor, and a pharmaceutical composition comprising the same compound as an effective ingredient for preventing or treating a protein kinase-related disease. The compound represented by Chemical Formula 1 according to the present invention, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an effective ingredient has outstanding inhibitory activity against LRRK2 kinase and against phosphorylation in the NIH-3T3 cell line, which is an LRRK2-expressing cell line, and NCC01 and 448T cell lines, which are both derived from patients with brain tumors. Verified to have inhibitory activity against various protein kinases in addition to LRRK2, the compound can find effective applications in the treatment or prevention of protein kinase-related diseases.

Abstract: The present disclosure relates to crystalline forms of Baricitinib and processes for preparation thereof. The present disclosure also relates to pharmaceutical composition containing these crystalline forms and use of these crystalline forms for preparing JAK inhibitor drugs and preparing drugs treating rheumatoid arthritis. The crystalline forms of the present disclosure have one or more improved properties compared with crystalline forms of the prior art and have significant values for future drug optimization and development.

Abstract: Provided are a novel pyrimidine compound that inhibits HER2 activity and exhibits brain penetration properties, or a salt thereof, and a pharmaceutical composition comprising the same. A compound represented by the following formula (I), or a salt thereof: wherein R1 represents a C1-C4 alkyl group optionally having a C1-C4 alkoxy group as a substituent, or a C3-C4 cycloalkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group optionally having 1 to 5 C1-C4 alkoxy groups or fluorine atoms each as a substituent(s), or a C1-C6 alkoxy group; R3 represents a hydrogen atom, or a C1-C4 alkyl group optionally having 1 to 5 fluorine atoms as a substituent(s); R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 represents a phenyl group optionally having 1 to 3 substituents selected from fluorine atoms and chlorine atoms.

Abstract: Disclosed herein are methods of preventing and/or treating lung injury and/or lung inflammation in a subject comprising administering to the subject a therapeutically effective dose of a PERK pathway inhibitor. Pharmaceutical compositions for the prevention and/or treatment of lung injury and/or lung inflammation comprising PERK pathway inhibitors are also provided. Also disclosed are uses of a PERK inhibitor in the manufacture of a medicament for the prevention and/or treatment of a lung injury and/or inflammation.

Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

Abstract: There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.

Abstract: An advantageous isolated morphic form of trilaciclib which is 2?-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7?,8?-dihydro-6?H-spiro[cyclohexane-1,9?-pyrazino[1?,2?:1,5]pyrrolo[2,3-d]pyrimidin]-6?-one, for example in the form of a di-hydrochloride salt or a dihydrochloride, dihydrate.

Abstract: The present invention provides methods for treating pruritus in a subject in need thereof comprising administering a therapeutically effective amount of a JAK inhibitor. Also provided are methods of intranasal administration of JAK inhibitors for use in treating pruritus.

Abstract: The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.

Abstract: Disclosed are 9-deazaaadenine derivatives of the general formula (I) and pharmaceutically acceptable salts thereof, wherein A is OH or NH2, and B is H or NH2. Methods for treating and/or suppressing a Zika virus infection with the compounds disclosed are also provided. Pharmaceutical compositions comprising the disclosed compounds are also provided. Such pharmaceutical compositions may optionally contain one or more additional active agents.

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

Abstract: A class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.

Abstract: This invention relates generally to the use of 5?-methylthioadenosine phosphorylase (MTAP) inhibitors for the treatment of lung diseases associated with inflammation, such as cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). Small molecule inhibitors of MTAP can sustain accumulation of endogenous MTA to therapeutically beneficial levels resulting in decreased inflammation in CF and COPD.

Abstract: This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.

Abstract: The present invention relates to an intravenous infusion dosage form of pemetrexed or its pharmaceutically acceptable salt, having long term stability.

Abstract: Disclosed are an intermediate of a pyrrolo six-membered heteroaromatic ring derivative as a JAK inhibitor and a preparation method therefor, and a method for preparing a pyrrolo six-membered heteroaromatic ring derivative using the intermediate. The method improves the reaction yield, is simple and easy to operate and control, and is conducive to expanded industrial production.

Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.

Abstract: The present invention relates to a compound according to formula I wherein R1 is alkyl; n is 1 or 2; R2 is selected from the group consisting of hydrogen, cyano, —SO2Ra, —SO2NRbRc, —C(O)Rb, phenyl and 5- and 6-membered heteroaryl or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to pharmaceutical compositions comprising said compounds, and to methods of treating proliferative or inflammatory skin disorders with said compounds.

Abstract: The present invention provides compounds which are of the formula (I) and (II) wherein X is selected from the group consisting of (III) and (IV); R is selected from the group consisting of (V) and (VI); Q is selected from the group consisting of (VII) and (VIII); and (IX) R2 is selected from the group consisting of (X) and (XI); or a pharmaceutically acceptable salt thereof, methods for treating obesity, type II diabetes, and compositions.

Abstract: The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

Abstract: Provided are compounds of the formula and pharmaceutically acceptable salts and composition thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g. HDAC2).

Abstract: The present invention relates to a pharmaceutical composition with enhanced stability, containing pemetrexed or a salt thereof, and a preparation method therefor. The present invention provides an injection preparation in liquid form containing pemetrexed, capable of ensuring sufficient stability during circulation and storage by selection of an optimum material and setting of an optimum concentration range in order to secure the stability of pemetrexed. The present invention can provide a pemetrexed preparation which is readily commercially prepared, can prevent microbial contamination occurring during lyophilization or reconstitution, and has enhanced convenience of administration and stability.

Abstract: A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided: Formula I, wherein, R is one selected from the group consisting of H and CH3; n is an integer ranging from 1 to 4; X is one selected from the group consisting of —CH2—, O, S, —NH—, —NHCHO—, —NHCOCH3—, and —NHCOCF3—; and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2?-fluoro-1,4-phenyl, and (c) 2,5-thienyl. Methods of treating a patient having cancer, targeting mitochondrial metabolism, and targeting SHMT2 and MTHFD2 using the compounds of this invention are disclosed.

Abstract: Disclosed are methods for the treatment of various solid tumors in patients in need of such treatment. The methods comprise administering to such a patient an NEDD8-activating enzyme (NAE) inhibitor such as ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]-pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) or a pharmaceutically acceptable salt in combination with one or more chemotherapeutic agents. Also disclosed are medicaments for use in the treatment of various solid tumors.

Abstract: Provided herein are methods of treating focal segmental glomerulosclerosis, said methods include administering to a subject in need thereof a therapeutically effective amount of a CCR2 antagonist. In some embodiments, the CCR2 antagonist is used in monotherapy. In some embodiments, the CCR2 antagonist is used in combination therapy. In some embodiments, the additional therapeutic agent is a RAAS blocker and/or an endothelin receptor inhibitor. The CCR2 antagonist may have the structure of formula (I).

Abstract: A method of determining the susceptibility of a cancer in a subject to treatment with an antimetabolite includes obtaining a sample of cancer cells from the subject, measuring the level of UDG expression in the cancer cells, and comparing the measured levels of UDG expression in the cancer cells to a control level.

Abstract: Provided herein are compounds useful for improving mRNA splicing in a cell. Exemplary compounds provided herein are useful for improving mRNA splicing in genes comprising at least one exon ending in the nucleotide sequence CAA. Methods for preparing the compounds and methods of treating diseases of the central nervous system are also provided.

Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.

Abstract: The present invention relates to compounds of formula I, wherein R1 is phenyl, lower alkyl, C3-6-cycloalkyl, —CH2—C3-6-cycloalkyl, or bridged C3-5-cycloalkyl, optionally substituted by one, two or three substituents, selected from halogen, lower alkyl or lower alkyl substituted by halogen; R2 is hydrogen, halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R3 is a five membered heteroaryl group, selected from wherein R6 is hydrogen or lower alkyl; R7 is halogen or lower alkyl; R8 is hydrogen or lower alkyl; R9 is hydrogen or lower alkyl; R4 is lower alkyl or lower alkyl substituted by hydroxy; R5/R5? is independently from each other hydrogen or lower alkyl; -( )n- is —CH2— or —CH2CH2— for n being 1 or 2; X is CH or N; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof.

Abstract: Provided herein are methods for treating, delaying progression of, or reducing the severity of amyotrophic lateral sclerosis (ALS) in a subject through administration of therapeutically effective amounts of agents (e.g., JAK kinase inhibitors (e.g., tofacitinib)) capable of interfering with central nervous system related natural killer cell (NK) levels and function.