Abstract: Provided herein are compounds, salts, solid forms, and pharmaceutical compositions that are related to EGFR inhibitors, such as N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-(2,2,2-trifluoroethyl)-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide, as well as methods of preparing the same. Also provided herein are methods of using the compounds, salts, solid forms, and pharmaceutical compositions for the treatment of diseases or disorders, such as cancer.

Abstract: Disclosed are a tartrate of 3-(5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl) pyrimidin-2-ylamino)-benzenesulfonamide and a polymorph thereof, which are inhibitors of protein kinases, in particular cyclin-dependent kinase 9 (CDK9), and can be used to treat proliferative disorders, such as cancer, and other diseases related to protein kinase/CDK activity.

Abstract: Compound that is an inhibitor of at least one of the A2A and A2B adenosine receptors, and compositions containing the compound and methods for synthesizing the compound, are described herein. The use of such compound and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.

Abstract: The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

Abstract: The present invention provides a new crystal form of a N-phenyl-2-aminopyrimidine compound, a crystal form of a pharmaceutically acceptable salt of said compound, and a preparation method for these crystal forms and use thereof. The present invention also relates to a pharmaceutical composition and a pharmaceutical preparation comprising the crystal form of said compound and the crystal form of the pharmaceutically acceptable salt of said compound, and use of these crystal forms, the pharmaceutical composition and the pharmaceutical preparation for treating diseases or conditions associated with the cell epidermal growth factor receptor (EGFR), for example, for treating or improving abnormal cell proliferative conditions, such as cancer.

Abstract: A type of deuterated 3-(4,5-substituted aminopyrimidine)phenyl derivatives and use thereof. The derivatives are compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds or salts thereof can be used for treatment or prevention of diseases or illnesses through certain mutant forms of epidermal growth factor receptors, inhibit the growth of various tumor cells effectively, and inhibit other proteases of EGFR and Her families, they can be used for preparing anti-tumor drugs.

Abstract: Disclosed are inhibitors of human galactokinase of formula (I) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I).

Abstract: Compound that is an inhibitor of at least one of the A2A and A2B adenosine receptors, and compositions containing the compound and methods for synthesizing the compound, are described herein. The use of such compound and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.

Abstract: The present disclosure relates to aniline pyrimidine derivatives or pharmaceutically acceptable salts thereof as EGFR inhibitors, specifically relates to compounds represented by formula (I) or pharmaceutically acceptable salts, pharmaceutical compositions, the method and uses thereof for treating EGFR mediated diseases.

Abstract: Object of the present invention is a process for the preparation of the pharmaceutical active ingredient Nilotinib free base or Nilotinib dihydrochloride dihydrate by means of an improved crystallization procedure.

Abstract: Methods and compounds are described for treating solid tumors, and in particular, malignant, neoplastic solid tumors such as glioblastoma and medulloblastoma, by inhibiting protein kinase MRK/ZAK activity. Also provided are pharmaceutical composition containing a MRK/ZAK inhibitor compound and a pharmaceutically acceptable carrier and a method of sensitizing tumor cells to radiation therapy comprising administering an effective amount of the MRK/ZAK inhibitor compound.

Abstract: The problem to be solved by the present invention is to provide a novel pharmaceutical composition for prevention and/or treatment of urinary incontinence, which differs from conventional drugs. The present invention provides a therapeutic agent for prevention and/or treatment of urinary incontinence having 1-[2-({[trans-3-fluoro-1-(3-fluoropyridin-2-yl)cyclobutyl]methyl}amino)pyrimidin-5-yl]-1H-pyrrole-3-carboxamide or a salt thereof, as an active ingredient.

Abstract: The invention provides gemcitabine derivatives shown in the following formula (I) and preparation methods thereof. The invention further relates to a pharmaceutical composition which comprising the said gemcitabine derivatives in an effective amount and a pharmaceutically acceptable excipient or additive. The invention further provides use of the said derivatives for preparing anti-tumor drugs. The compound designed by the invention is novel in structure and has a remarkable anti-tumor activity. According to the compound designed by the invention, the preparation starting materials have extensive sources and are easily obtained, the preparation method is simple and easy to operate, and the yield of the product is high, so that industrial production on a large scale is facilitated.

Abstract: The present invention relates to fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). R2 represents the group (a).

Abstract: The present invention relates to fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).

Abstract: Imidazolyl-pyrimidine and related compounds, as can utilize heme-iron coordination in the selective inhibition of neuronal nitric oxide synthase.

Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein.

Abstract: The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them.

Abstract: The present invention relates to methods and compositions for modulating levels of amyloid-? peptide (A?) exhibited by non-neuronal (i.e., peripheral) cells, fluids, or tissues. The invention also relates to modulation of A? levels via selective modulation (e.g., inhibition) of ?-secretase activity. The invention also relates to methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an A?-related disorder, by administering a compound that results in the modulation of ?-secretase in a non-neuronal tissue, either directly or indirectly to prevent, treat or ameliorate the symptoms of a brain A? disorder, such as Alzheimer's disease.

Abstract: Imidazolyl-pyrimidine and related compounds, as can utilize heme-iron coordination in the selective inhibition of neuronal nitric oxide synthase.

Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g.

Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.

Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I).

Abstract: The present invention relates a process for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the compound of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.

Abstract: The present invention is directed to benzoimidazol-2-yl pyrimidine derivatives useful as histamine H4 receptor modulators and processes for the preparation of such compounds.

Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.

Abstract: Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal tumors.

Abstract: Nilotinib salts and crystalline forms thereof have been prepared and characterized.

Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway.

Abstract: The present invention relates to compounds of formula (I): wherein R1 is NH2 or NHMe; R2 is halo; and one of R3 or R4 is hydrogen and the other is selected from —SO2NH2, —SO2NHMe or —SO2NMe2, —SO2NHEt, or —SO2NEt2; or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula (I) are inhibitors of protein kinases, especially cyclic dependent kinases (CDKs) such as CDK9. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which protein kinase/CDK activity is implicated.

Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

Abstract: Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritis.

Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.

Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R1, R4, X, G, n, p, W1, W2, W3, W4, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.

Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.

Abstract: Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.

Abstract: The present invention relates to a novel organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound according to the present invention has excellent luminous efficiency, power efficiency, and lifespan characteristic. Using the compounds of the present invention, it is possible to manufacture an OLED device with a long operating lifespan. In addition, the compounds can improve the power efficiency of the device to reduce overall power consumption.

Abstract: The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a novel organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound according to the present invention has high green luminous efficiency and superior material lifespan characteristics, compared with conventional phosphorescent host materials, and thus can provide an organic electroluminescent device which is excellent in operational lifespan, and induces increased power efficiency and improves power consumption.

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.

Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.