Abstract: Cycloalkylamine derivatives may be used for preventing or treating diseases in humans, animals, and have demonstrated efficacy specifically in treating type 2 diabetes. In an embodiment, the cycloalkylamine derivatives can include a compound selected from the group consisting of cycloheptanamine salts, cyclohexanamine salts, cyclopentanamine salts 1-cycloheptyl-[4,4?-bipyridin]-1-ium, N1,N2-dicycloheptyloxalamide, 1-[3?,5?-bis(trifluoromethyl)phenyl]-3-cycloheptylurea, 1,1?-(4-methyl-1,3-phenylene)bis(3-cycloheptylurea), 1-(2?-aminopyrimidin-4?-yl)-3-cycloheptylurea, 4-amino-N-(cycloheptylcarbamoyl)benzenesulfonamide, 4-(3?-cycloheptylureido)-N-(5?-methylisoxazol-3?-yl)benzenesulfonamide, N-(cycloheptylcarbamoyl)-4-methylbenzenesulfonamide, 1-cycloheptylguanidine hydrochloride, (E)-amino[(amino(cycloheptylamino)methylene)amino]methaniminium chloride, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

Abstract: A 5-methoxyquinazoline derivative compound I, having a structure represented by formula I: A 5-methylquinazoline derivative compound II, having a structure represented by formula II A method for preparing crystals of a 5-methoxyquinazoline derivative compound I and a 5-methylquinazoline derivative compound I, includes: adding 0.8847 g of 5-methoxyisatin, 0.8256 g of 5-methylisatin, 2.6963 g of ammonium formate, and 100 mL of anhydrous methanol in a 250 mL round-bottomed flask; heating and stirring a resulting mixture for refluxing for 48 hrs, stopping reaction, and performing rotary filtration and obtaining a crude filter residue; and performing column chromatography on the crude filter residue using dichloromethane and anhydrous methanol at a volume ratio of 1:1, and respectively obtaining the crystal of 5-methoxyquinazoline derivative compound I and the crystal of 5-methylquinazoline derivative compound II.

Abstract: The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.

Abstract: The present embodiments are directed, in part, to 5-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, such as those of Formula I, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of delta opioid receptor, biased and/or unbiased, and/or methods for treating pain, migraines, headaches, depression, Parkinson's Disease, anxiety, and/or overactive bladder, and other disorders and conditions described herein or any combination thereof.

Abstract: The invention relates to pyrimidinone derivatives of the general Formula I, or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Abstract: The invention relates to carboxamide-pyrimidine derivatives of the general formula I, or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

Abstract: The present invention relates to the intravaginal use of sex steroid precursor (e.g. DHEA) for the reduction of the incidence or recurrence of breast cancer in postmenopausal women. The dosage of sex steroid precursor is limited to 25 mg per day or less. Further administration of selective estrogen receptor modulator is disclosed for the above-reduction.

Abstract: Provided is a compound of formula I or a pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, isotopic substituent, polymorph, prodrug, or metabolite thereof. Also provided is a method for preparing the compound of formula I. The compound of formula I has higher inhibitory activity against SHP2, and thus can be used to prevent or treat a disease related to SHP2.

Abstract: Provided herein are crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate. Pharmaceutical compositions comprising crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate are also disclosed.

Abstract: A pharmaceutical composition containing palbociclib tosylate and letrozole, in which palbociclib tosylate and letrozole are in one dosage unit, and the particles of the active ingredient palbociclib tosylate and letrozole are not separated from each other, and the production of the pharmaceutical preparation, the granule containing palbociclib tosylate and letrozole, the use of the pharmaceutical preparation and special blister packaging that facilitates the use of a specific dosage regimen.

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with an inhibitor of MAPK/ERK kinase-1 and -2 (MEK1 and MEK2; MAP2K1 and MAP2K2), such as trametinib.

Abstract: Provided herein are methods of treating, managing and/or preventing viral infections. A particular method comprises administering to a subject in need thereof an effective amount of an adaptor associated kinase 1 inhibitor of the formula wherein R1, R2 and R3 are defined herein.

Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

Abstract: Compounds and compositions are provided as inhibitors of the Wnt/?-catenin pathway for the treatment of diseases that implicate the same.

Abstract: Methods of treating glioblastoma are provided comprising: administering a therapeutically effective amount of azeliragon, or a pharmaceutically acceptable salt thereof, and co-administering an effective amount of radiation therapy (RT), to a patient who has been diagnosed with glioblastoma. In another aspect, methods are provided for treating grade I, grade II, and grade III gliomas, the method comprising administering a therapeutically effective amount of azeliragon, or a pharmaceutically acceptable salt thereof, and co-administering an effective amount of radiation therapy (RT), to a patient who has been diagnosed with glioma.

Abstract: Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.

Abstract: Disclosed are a diazaindole derivative as shown in formula I and the use thereof in the preparation of a drug for treating Chk1-related diseases.