Abstract: A substituted amino heterocyclic carboxamide compound as represent by formula (?), or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvent compound, a crystal form, a stereoisomer or an isotopic variant of the compound, and a pharmaceutical composition thereof, and the use thereof as an FLT3/AXL kinase inhibitor for treating acute myelocytic leukemia.
Abstract: The present disclosure provides a substituted pyrazolo[1,5-a]pyridine compound, a composition including the same, and a use thereof. The substituted pyrazolo[1,5-a]pyridine compounds is a compound represented by formula (I) or the tautomers, stereoisomers, prodrugs, crystal forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compound of the present disclosure and composition thereof are useful for treating RET kinase-mediated diseases or conditions and have more excellent pharmacokinetic properties.
Abstract: Provided are a substituted benzimidazole compound, and a composition comprising same and use thereof. The substituted benzimidazole compound is a compound represented by formula (I), or a pharmaceutically acceptable salt, prodrug, hydrate or solvate compound, polymorph, stereoisomer, or isotopic variation thereof. The compound can be used for treating and/or preventing related diseases caused by MEK, such as hyperproliferative diseases, pancreatitis, kidney diseases, blastocyte implantation, and diseases related to vasculogenesis or angiogenesis.
Abstract: The present invention provides a diarylpyrazole compound, a composition comprising same, and a use thereof. The diarylpyrazole compound refers to the compound represented by a formula (I) or a tautomer, a stereoisomer, a prodrug, a crystalline form, a pharmaceutically acceptable salt thereof, a hydrate, or a solvent compound. The compound and the composition of the present invention can be used for treating BRAF kinase mutant proliferative diseases and have better pharmacokinetic properties.
Abstract: Provided are a compound as represented by formula (D) and a preparation method therefor, where X2 is a halogen, Pg is selected from H and an amino protecting group, such as Cbz, Boc, Fmoc, Alloc, Teoc, methoxycarbonyl or ethoxycarbonyl. Also provided are a synthesized intermediate compound of the formula (D) compound and a preparation method for the intermediate compound.
Abstract: Provided is an alkynyl(hetero)aromatic compound having an inhibitory effect to protein tyrosine kinase, a pharmaceutical composition comprising same, preparation and usage thereof. Specifically, disclosed is an alkynyl(hetero)aromatic compound as shown in formula (I), wherein rings A, R1, R2, R3, R4, R5, L, and B are defined in the description, a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form, a prodrug or an isotopic variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases, such as anti-tumor.
Abstract: The present invention provides substituted pyrazole compounds, compositions containing same, and use thereof. The substituted pyrazole compounds comprise a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystalline form, pharmaceutically acceptable salt, hydrate, or solvate thereof. The compound represented by formula (I) can serve as a tissue selective androgen receptor modulator (SARM), particularly serving as a drug for treating prostate cancer and other AR-dependent conditions and diseases in which AR antagonism is desired.
Abstract: Provided are a crystal form of a free base or a pharmaceutically acceptable salt of (R)-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-fluoropyrrolidin-1-yl)-5-(pyrazin-2-yl)nicotinamide (compound A), a preparation method therefor, and use of the compound in preparation of drugs for treating diseases mediated by Bcr-Abl kinase and mutants thereof, such as chronic granulocytic leukemia. Also provided are a method for preparing compound A, and a preparation containing compound A.
Abstract: Disclosed are alkynyl (hetero) aromatic ring compounds that inhibit protein tyrosine kinases, pharmaceutical compositions comprising same, preparations therefor and uses thereof. Specifically, disclosed are an alkynyl (hetero) aromatic ring compound represented by formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form, a prodrug or an isotope variant thereof. The disclosed compounds may be used in the treatment and/or prevention of diseases associated with protein tyrosine kinase, such as in preventing tumors.
Abstract: An N-benzenesulfonylbenzamide compound represented by the formula (I), or a crystal form, a prodrug, pharmaceutically acceptable salts, a stereoisomer, a solvate or a hydrate thereof, a pharmaceutical composition containing same, and a use thereof as a Bcl-2 protein inhibitor for preparing a medicament for treatment of leukemia or a cancer.
Abstract: The present invention relates to a crystalline form of a free base of a compound of formula (A) (compound A) or a pharmaceutically acceptable salt thereof, a preparation method therefor, and use of the compound in the preparation of a medicament for treating and/or preventing diseases mediated by ALK kinase and mutants thereof, such as cell proliferative diseases, inflammation, infections, immunological diseases, organ transplantation, viral diseases, cardiovascular diseases or metabolic diseases.
Abstract: A substituted amino heterocyclic carboxamide compound as represent by formula (?), or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvent compound, a crystal form, a stereoisomer or an isotopic variant of the compound, and a pharmaceutical composition thereof, and the use thereof as an FLT3/AXL kinase inhibitor for treating acute myelocytic leukemia.
Abstract: An antiviral nucleoside reverse transcriptase inhibitor compound as shown in formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form or an isotopic derivative of the compound. A preparation method therefor, a pharmaceutical composition thereof, and a use thereof in the preparation of a drug for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV).
Abstract: A macrocycle represented by formula (I) and a pharmaceutical composition comprising the macrocycle, or a crystalline form, pharmaceutically acceptable salt, hydrate or solvent compound, stereoisomer, prodrug, or isotopic variant of the macrocycle. The macrocycle and the composition thereof inhibit a protein kinase.
Abstract: Provided in the present invention are a substituted aromatic fused ring derivative, a composition comprising the compound, and the use thereof. The substituted aromatic fused ring derivative is a compound as shown as formula (I) or a tautomer, stereoisomer, prodrug, crystal form, pharmaceutically acceptable salt, hydrate or solvate thereof. The compound and the composition of the present invention can be used to treat various protein tyrosine kinase-mediated diseases or conditions.
Type:
Application
Filed:
March 18, 2022
Publication date:
December 1, 2022
Applicant:
Shenzhen TargetRx, Inc.
Inventors:
Yihan Wang, Qingfeng Xing, Yixin Ai, Huanyin Li
Abstract: A substituted amino heterocyclic carboxamide compound as represent by formula (?), or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvent compound, a crystal form, a stereoisomer or an isotopic variant of the compound, and a pharmaceutical composition thereof, and the use thereof as an FLT3/AXL kinase inhibitor for treating acute myelocytic leukemia.
Abstract: The present invention relates to a pharmaceutical composition of a substituted pyridazinone compound and use thereof. The substituted pyridazinone compound is a compound as represented by formula (I), or a pharmaceutically acceptable salt, a prodrug, a hydrate or solvent compound, a crystalline form, and a stereoisomer or isotopic variant thereof. The compound is a THR-beta agonist which can be used for treating and/or preventing diseases regulated by thyroid hormone analogues.
Abstract: Provided in the present invention are a substituted pyrrolotriazine compound, a pharmaceutical composition thereof and a use thereof, the pyrrolotriazine compound being a compound represented by formula (I), or a pharmaceutically acceptable salt, prodrug, hydrate or solvent compound, crystalline form, stereoisomer or isotope variant thereof. The compound and composition of the present invention may be used in the treatment of conditions associated with KIT and/or PDGFR?.
Abstract: Provided are pharmaceutical compositions comprising substituted pyrazolo[1,5-a]pyrimidine compounds and the use thereof. The compositions may comprise the substituted pyrazolo[1,5-a]pyrimidine compound or a pharmaceutically acceptable salt, prodrug, hydrate or solvate, polymorph, stereoisomer or isotopic variant thereof, and can be used for treating diseases treatable with Trk kinase inhibitors.
Abstract: An antiviral nucleoside reverse transcriptase inhibitor compound as shown in formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form or an isotopic derivative of the compound. A preparation method therefor, a pharmaceutical composition thereof, and a use thereof in the preparation of a drug for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV).