Abstract: Compounds of the formula I in which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in Claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

Abstract: The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.

Abstract: This application relates to various crystalline forms of 4-(2-((1R,2R)-2-hydroxycyclohexylamino)benzothiazol-6-yloxy)-N-methylpicolinamide hydrochloride salts as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including glioblastoma multiforme, breast cancer, pancreatic cancer and other solid tumors.

Abstract: Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which q, R11, R12, R13 and R14 are as defined in the specification, for use in therapy.

Abstract: The present disclosure provides a novel crystalline form of Lemborexant and processes for preparation thereof. Pharmaceutical composition containing Lemborexant, and use of Lemborexant for preparing orexin receptor antagonist drug, and use of Lemborexant for preparing drugs treating insomnia and irregular sleep-wake rhythm disorder are also provided. The crystalline form of the present disclosure have one or more improved properties compared with crystalline forms of prior arts, and has significant values for future drug optimization and development.

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

Abstract: A novel heterocyclic compound inhibiting a cyclin-dependent kinase (CDK) and a pharmaceutical composition containing the compound as an effective ingredient are disclosed. The heterocyclic compound according to the present invention or pharmaceutically acceptable salt thereof can be effectively used in treating or preventing cancers, degenerative brain diseases, etc.

Abstract: Described herein is the MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate, including crystalline forms and pharmaceutically acceptable salts and solvates thereof.

Abstract: The present invention discloses a compound represented by the following Formula (I) and a pharmaceutically acceptable salt thereof. The compound improves the THR? selectivity while maintaining good THR? agonistic activity, thereby improving properties of the finished drug.

Abstract: The present invention discloses an organic compound and an organic electroluminescence device using the organic compound as an emitting host material, an electron transfer material or a hole blocking material in the light emitting layer of the organic electroluminescence device. The organic compound may be for increasing a half-life or current efficiency of the organic electroluminescence device, and may be for lowering a driving voltage or power consumption of the organic electroluminescence device. The same definition as described in the present invention.

Abstract: It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.

Abstract: The present application refers to photo-switchable chemical inducers of dimerization for control of protein interactions in cells by light. A compound, a test system, methods and uses are disclosed how the invention can be applied in the investigation of intracellular protein interactions. The system is composed of a compound of the general formula (I) as the photo-caged dimerizer, with the ability to covalently bind to HaloTag and a high affinity binding to eDHFR, respectively. The system can be activated and deactivated selectively on illumination with light under different irradiation conditions.

Abstract: The invention provide novel pyrimidine derivatives and analogs having inhibitory activities towards certain tyrosine kinases, e.g., Bruton's tyrosine kinase (Btk) and/or Focal adhesion kinase (FAK), extracellular signal-regulated kinase (ERK), pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by such by tyrosine kinases, e.g., cancers, tumors, fibrosis, inflammatory diseases, autoimmune diseases, diabetes, or immunologically mediated diseases.

Abstract: Provided is a heterocyclic compound of Formula 1: and an organic light emitting device comprising the same.

Abstract: Provided is a hetero-cyclic compound of Chemical Formula 1: and an organic light emitting device comprising the same.

Abstract: Described herein is dioxolane-containing compound of formula (I) wherein (i) Rf1 and Rf2 are independently linear or branched perfluoroalkyi groups having with 1-8 carbon atoms and optionally comprise at least one catenated heteroatom, or (ii) Rf1 and Rf2 are bonded together to form a ring structure having 4-6 carbon atoms and optionally comprise one or more catenated heteroatoms; Rf2 is a linear or branched perfluoroalkyi groups having with 1-3 carbon atoms; and R4 and R5 are independently selected from H, F, Cl, a linear or branched alkyl group having 1-3 carbon atoms, optionally wherein the alkyl group comprises at least one of: fluorine, chlorine, a hydroxyl group, or a catenated heteroatom; for use in cleaning compositions, as an electrolyte solvent, as a heat transfer fluid, or a vapor phase soldering fluid.

Abstract: The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.

Abstract: The invention relates to succinimide compounds of formula I wherein the variables have the meanings as defined in the specification, to compositions comprising them, to active compound combinations comprising them, and to their use for protecting growing plants and animals from attack or infestation by invertebrate pests, furthermore, to seed comprising such compounds.

Abstract: Disclosed is a compound as shown in formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, and the present invention relates to the use of same in the preparation of a drug for treating FXR-related diseases.

Abstract: The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the compounds and methods of treatment.

Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as pesticides, especially as fungicides.

Abstract: Disclosed herein are methods and compositions comprising compounds capable of activating and increasing protein SUMOylation. Disclosed herein are methods and compositions comprising compounds capable of showing neuroprotective and cytoprotective effects when administered to injured cells. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, chronic traumatic encepholopathy, traumatic brain injury, or stroke.

Abstract: Disclosed herein are methods and compositions comprising compounds capable of activating and increasing protein SUMOylation. Disclosed herein are methods and compositions comprising compounds capable of showing neuroprotective and cytoprotective effects when administered to injured cells. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, chronic traumatic encepholopathy, traumatic brain injury, or stroke.

Abstract: Histone deacetylase (“HDAC”)-selective inhibitors covalently bonded to a linker covalently bonded to an E3 ubiquitin ligase ligand, and salts thereof; pharmaceutical compositions containing them; methods of using the composition to inhibit neoplastic cell growth in mammals, including humans.

Abstract: Disclosed are a compound as a selective JAK inhibitor, and an isomer, a solvate or a pharmaceutically acceptable salt thereof, wherein: the definitions of (A), R, R1 and n are described in detail in the specification. In addition, also disclosed are a medicament including the compound and salts thereof as an active ingredient, and the use thereof in the preparation of a medicament for treating JAK-related target diseases, such as immune system diseases, rheumatoid arthritis and tumors.

Abstract: The present invention relates to meta substituted phenylpyrazolo- and phenylpyrrolo-pyridazine derivatives having dual pharmacological activity towards both the ?2? subunit, in particular the ?2?-1 subunit, of the voltage-gated calcium channel and the NET 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: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The present disclosure relates to novel pyridine-containing macrocyclic compounds and libraries thereof that are useful as research tools for drug discovery efforts. This disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.

Abstract: The present disclosure relates to Ribociclib solid state forms, Ribociclib salts including Ribociclib succinate and solid state forms thereof, as well as processes for preparation thereof and pharmaceutical compositions thereof.

Abstract: Salts of cytisine have been prepared and incorporated in stable pharmaceutical compositions, including compositions comprising lactose. The salts are prepared by adding acid stock solutions to solutions of cytisine with heating, followed by cooling to ambient temperature. The salts and compositions are indicated in the treatment of nicotine addiction.

Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.

Abstract: The present invention relates to 2-phenyl-2H-pyrazolo[3,4-d]pyridazine derivatives having pharmacological activity towards the ?2? subunit, in particular the ?2?-1 subunit, of the voltage-gated calcium channel, in particular having dual pharmacological activity towards both the ?2? subunit, in particular the ?2?-1 subunit, of the voltage-gated calcium channel and the ?-opioid receptor. The present invention also relates 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: The present invention relates to an efficient and industrially advantageous process for preparing temozolomide and the carbamoyl-AICA intermediate through the use of N-methyl carbamoylimidazole in a good overall yield and high purity.

Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.

Abstract: The present invention relates to orexin receptor antagonists, pharmaceutical compositions comprising the antagonists, methods of making the antagonists, their use for the modulation of the orexin receptor, and to use of the antagonists as medicaments, in particular for treating diseases, disorders, or conditions mediated by orexin receptor activity. More specifically, there is provided a compound of Formula (I) including salts thereof, polymorphs, and isomers thereof (including optical, geometric and tautomeric isomers) as defined herein and isotopically-labelled compounds of Formula (I).

Abstract: A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target.

Abstract: The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to compounds of formula I a process for their manufacture, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels. R1, R2, R3, R4 and R5 have meanings given in the description.

Abstract: In certain embodiments compounds (e.g., triazolopyrimidine(s) and/or triazolopyridine(s)) are provided that are effective to lower p-tau and/or to prevent or reduce elevation of p-tau, particularly in response to stress (e.g., elevated cortisol levels). The 5 compounds are useful in the treatment or prophylaxis of pathologies characterized by abnormal amyloid plaque and or tangle formation and/or deposition.

Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.

Abstract: The present disclosure provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R7 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient. In another embodiment, these compounds are useful for treating respiratory dysfunction in patients by administering one or more of the compounds to a patient.

Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.

Abstract: The present invention relates to an improved process for the preparation of Pirlindole enantiomers, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is related to a novel pyrimidine derivative compound or a pharmaceutically acceptable salt thereof, a process for preparing the same, and a pharmaceutical composition using the same.

Abstract: Discussed is an organic compound of Formula 1 and an organic light emitting diode and an OLED device including the organic compound. In the organic compound, Ar1 is a heteroaryl group comprising a nitrogen atom, and Ar2 is a C6 to C30 aryl group, and R is a C1 to C10 alkyl group. The organic compound may be included in an emitting material layer of the organic light emitting diode as a host such that an emitting efficiency and a lifespan of the organic light emitting diode and the OLED device are improved.

Abstract: Provided is a pharmaceutical preparation that is suitable for more effectively exhibiting the efficacy of a glutamic acid derivative, which is a GGT-recognizable prodrug, by producing a composition including a glutamic acid derivative capable of rapidly releasing a physiologically active substance by being recognized by GGT, or a pharmacologically acceptable salt thereof; and a block copolymer in which a polyethylene glycol segment is linked to a polyamino acid segment with a hydrophobic group. Particularly, the composition based on a glutamic acid derivative that uses an antitumor compound as a physiologically active substance is capable of effectively accumulating the glutamic acid derivative at a tumor affected area, exhibits a superior effect against tumors, and is capable of suppressing the release of a physiologically active substance in bone marrow tissue where the expression ratio of GGT is low.

Abstract: The invention relates to new compounds of formula (I) wherein X represents a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine, which are useful for the preparation of 4,4?dihalodiphenylsulfones of formula (III) wherein X is as defined above.

Abstract: A compound of Formula I wherein X1 and X2 are independently CRX or N, and at least one of X1 or X2 is CRX; Y is selected from the group consisting of O, S, Se, NR?, BR?, CR?R?, and SiR?R?; R?, and R? are each independently selected from the group consisting of alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, and combinations thereof; R is selected from the group consisting of deuterium, halogen, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carboxylic acid, ether, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, and combinations thereof; RA, and RC each independently represent mono to the maximum allowable substitution, or no substitution; and each RX, RA, and RC is independently a hydrogen or a substituent selected from the group consisting of deuterium, halogen, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, alkoxy, aryloxy, amino, si

Abstract: Thienopyridinone compounds of Formula (I) and pharmaceutically acceptable salts thereof are described. In these compounds, one of X1; X2, and X3 is S and the other two are each independently CR, wherein R and all other variables are as defined herein. The compounds are shown to inhibit HPK1 kinase activity and to have in vivo antitumor activity. The compounds can be effectively combined with pharmaceutically acceptable carriers and also with other immunomodulatory approaches, such as checkpoint inhibition or inhibitors of tryptophan oxidation. Formula (I).