16432 results about "Pharmaceutical medicine" patented technology

Compounds shown as formula (I) or stereoisomers thereof, or pharmaceutically acceptable salts, solvates or prodrugs thereof, a pharmaceutical composition comprising same, and the use of same in the preparation of drugs for preventing and / or treating diseases or disorders related to RAS protein activity, such as cancer.

Compounds or their pharmaceutically acceptable salts can modulate the G12D 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 disclosed herein 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.

A fused ring compound, a pharmaceutical composition comprising same, and the use thereof. The compound has a structure as represented by formula (I), or is a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer or a mixture form thereof, a metabolite, a metabolic precursor, an isotope-substituted form, a pharmaceutically acceptable salt, a hydrate, a solvate, a polymorph or a co-crystal thereof. The compound can be used for treating one or more cancers caused by KRAS mutation.

Provided herein are compounds of Formula (IV-b), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein (e.g., a dysregulated KRas protein (e.g., a mutated or amplified KRas protein)). This disclosure also provides compositions containing the compounds as provided herein, or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

Disclosed in the present invention is a novel fused heterocyclic compound having CDK target inhibitory activity. Specifically disclosed are a compound having a structure as shown in formula (I) and serving as a CDK target inhibitor, or a pharmaceutically acceptable salt, solvate, hydrate, isotopic substituent or isomer thereof.

A fused ring compound, a pharmaceutical composition comprising same, and a use. The compound has a structure represented by formula (I) or a tautomer, mesomere, racemate, enantiomer, diastereomer or mixture thereof, metabolite, metabolic precursor, isotope substitution form, pharmaceutically acceptable salt, hydrate, solvate, polymorph or eutectic thereof. The compound can be used for treating a cancer caused by KRAS mutations, and said cancer is selected from one or more cancers caused by KRAS G12C, KRAS G12V, KRAS G12A and G12D mutations. In particular, the compound can serve as a G12D inhibitor and has relatively high inhibitory activity.

The compositions and methods provided herein include a pharmaceutical formulation for oral administration comprising a daily dose of a modified release formulation of minoxidil or a pharmaceutically acceptable salt thereof. Also provided herein are pharmaceutical formulations for oral administration comprising a daily dose of a modified release formulation of minoxidil or a pharmaceutically acceptable salt thereof and one or more additional active agents. Also provided herein are methods of treating hair loss by administering to a subject in need thereof a daily dose of a modified release formulation of minoxidil or a pharmaceutically acceptable salt thereof. Further provided herein is a kit including a slow modified release vehicle comprising oral minoxidil or a pharmaceutically acceptable salt thereof.

Provided herein are compounds having a Formula (I), or a pharmaceutically acceptable salt thereof. Also provided herein are methods of preparing the compounds and methods of using the compounds in inhibiting PI3K in a cell, and / or in treating various diseases such as cancer.

The invention belongs to the technical field of medicines, and relates to tetrahydropyridopyrimidine compounds as well as a preparation method and application thereof, in particular to tetrahydropyridopyrimidine compounds or pharmaceutically acceptable salts thereof as well as a preparation method and application thereof in preparation of antitumor drugs. The structure of the tetrahydropyridopyrimidine compound or the pharmaceutically acceptable salt thereof is as shown in a general formula (I), and R1-R4 are as shown in the specification and claims. The compound provided by the invention can be used for preparing a KRAS G12C inhibitor, is used for inhibiting G12C mutation of KRAS, has an obvious inhibiting effect on lung cancer, pancreatic cancer or colon cancer, and can be used for preparing antitumor drugs. # imgabs0 #

Disclosed herein are compounds having the Formula I: SHP-L-Hs (I) and pharmaceutically acceptable salts thereof, wherein SHP is a chemical entity that binds to SHP2 protein, L is a linker, and Hs is chemical entity that binds HSP90 protein. Pharmaceutical compositions comprising the disclosed compounds and their uses for treating diseases responsive to modulation of SHP2 protein are also provided.

Provided is a medicine for treating or preventing cancer that contains a first active ingredient and that is used in combination with a second active ingredient, wherein: the first active ingredient is a compound represented by formula (1), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof; and the second active ingredient is GDC-6036 or a pharmaceutically acceptable salt thereof.

The invention discloses a benzylamine formyl compound as well as a preparation method and application thereof. Specifically, the invention provides benzylamine formyl compounds as shown in a general formula I and pharmaceutically acceptable salts thereof, and the benzylamine formyl compounds and the pharmaceutically acceptable salts thereof have excellent inhibitory activity on SOS1 protein and can be used for treating cancers. # imgabs0 #

The present application relates to the technical field of medicines, and relates to a macrocyclic compound containing amide substitution, in particular to a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof in the treatment of disease.

Disclosed in the present invention is a phosphoinositide 3-kinase allosteric inhibitor for treating a disease related to PI3K regulation. Specifically, provided is a compound as represented by formula I or a pharmaceutically acceptable salt thereof. The phosphoinositide 3-kinase allosteric inhibitor of the present invention can effectively conduct allosteric targeted inhibition on a PI3Kα mutation, in particular, a PI3KαH1047R mutation, has relatively good selectivity, and is expected to treat and / or prevent related diseases or disorders.

The invention relates to the field of medicinal chemistry, in particular to quinoline compounds or pharmaceutically acceptable salts, isomers, solvates, compositions and medical application thereof. Pharmacological tests prove that the quinoline compound disclosed by the invention has a relatively good affinity effect on KRASG12D-cRaf. When the concentration is 10 M, the compound C1, the compound C3, the compound C4, the compound C6, the compound C11, the compound C12, the compound C13, the compound C16, the compound C22 and the compound C23 have a certain inhibition effect on KRASG12D-cRaf. Particularly, the compound C1 and the compound C12 both show a strong inhibition effect on KRASG12D-cRaf.

The invention provides a polypeptide or a derivative and a pharmaceutically acceptable salt thereof. The amino acid sequence of the polypeptide is as shown in SEQ ID NO: 1. The polypeptide or the derivative and the pharmaceutically acceptable salt thereof disclosed by the invention can be combined with GLP-1R and GCGR, and is used for effectively activating the GLP-1R and the GCGR. Therefore, the polypeptide or the derivative and the pharmaceutically acceptable salt thereof can be used for detecting GLP-1R and / or GCGR, and can also be used for treating or preventing GLP-1R and / or GCGR related diseases (such as metabolic disorder related diseases, such as obesity, diabetes, fatty liver diseases, non-alcoholic fatty liver diseases and the like).

The present invention relates to an oxo-tricyclic derivative and the pharmaceutical use thereof, in particular to a compound as shown in general formula (I), or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a cocrystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating diseases associated with WRN activity or expression level.

Provided herein is a Drug-Linker of Formula (I) or a pharmaceutically acceptable salt thereof, wherein D is a drug unit, K1 is selected from (i) a peptide unit, (ii) an oligosaccharide, and (iii) a polyether, and M1 is a group which can react with a ligand to form a connector unit. Such compounds can be useful as anti-cancer agents.

The invention relates to compounds of Formula I, II II-1, III, or III-1 and pharmaceutically acceptable salts thereof, and methods of making and using the same. The compounds of the invention are effective in inhibiting and / or degrading KRAS protein with a G12D mutation and are suitable for use in methods of treating cancers mediated, in whole or in part, by KRAS G12D mutation.

The invention provides a tetrahydropyridinopyrazole derivative and application thereof in medicine, and particularly relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or eutectic of the compound, and an intermediate and a preparation method of the tetrahydropyridinopyrazole derivative. The invention also relates to application in preparation of related medicines for treating diabetes mellitus. # imgabs0 #

Related to macrocyclic compounds and therapeutic uses thereof. Disclosed a compound of formula (I), or a pharmaceutically acceptable salt thereof, a solvate thereof or a solvate of the pharmaceutically acceptable salt, and their use for the preparation of a medicament of treatment of cancer. Provided herein are useful compounds for the inhibition of RAS mutant and the compound shows good inhibitory activity against RAS.

The invention relates to compounds of formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a prodrug thereof, a deuterated molecule thereof or a PROTAC molecule thereof that selectively inhibit the activity of K-Ras G12D protein, compositions comprising the same, the methods of using the same and related intermediates.

The present invention relates to a compound as shown in formula (A) having a pan-RAS inhibitory effect, or an isotopic derivative or stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound, and the use of the compound of formula (A) in the prevention and / or treatment of cancers, tumors, inflammatory diseases, autoimmune diseases or immune-mediated diseases.

A compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof wherein X-Y is -NHSO2- or -SO2NH-; R1 is H, CN or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, optionally substituted heteroaryl, SO2NR14R15, CONR10R11 and alkyl; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H or halo; and R10, R11, R12, R14, and R15 are H or alkyl; R13 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m is 0-3. The compounds of formula (I) modulate ERAP1 (endoplasmic reticulum aminopeptidase 1) and are for use in treating proliferative, immune or inflammatory disorders, particularly cancer or leukemia. The compounds of formula (I) stimulate a neo-antigen directed immune response in the subject. A method for producing an antigen-presenting cell which presents a neo-antigen using compounds of formula (I) is disclosed. An immunogenic composition comprising an antigen-presenting cell is also disclosed. Exemplified compounds include 4-cyclopropyl-3-(N-(2-(morpholin-3-yl)-5-(trifluoromethyl)phenyl)sulfamoyl)benzoic acid.

The invention provides a pharmaceutical composition for intranasal administration comprising a salt of sumatriptan or a physiologically acceptable solvate thereof, an alkyl glycoside or saccharide alkyl ester and optionally at least one pharmaceutically acceptable excipient, wherein the said composition provides Tmax value of less than 30 minutes upon said administration. Other aspects and embodiments are contemplated and described.The invention also provides a pharmaceutical composition for intranasal administration comprising a triptan, a pharmaceutically acceptable vehicle and a mucosal permeation enhancer, wherein upon said administration said composition provides a Tmax substantially equivalent to subcutaneous administration of said triptan. Other aspects and embodiments are contemplated and described.

The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic protein.

A spiro compound, and a preparation method therefor and a use thereof. Specifically, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite, or prodrug thereof, a pharmaceutical composition comprising the compound, a preparation method therefor, and a use thereof in preparation of a drug for preventing or treating KRAS-mediated related diseases.

A long-acting injection preparation and a preparation method therefor. The preparation contains an active compound such as the compound as shown in formula (I) or formula (II), or compound 6, or a stereoisomer, pharmaceutically acceptable salt or deuterated compound thereof, and at least one pharmaceutically acceptable carrier.

Disclosed in the present invention are a quinazoline compound, and a pharmaceutical composition thereof and the use thereof. Provided in the present invention is a compound as represented by formula I, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The compounds of the present invention have a good degradation effect on the KRAS protein with a G12D mutation, have a good inhibitory activity against the proliferation of tumor cells with a KRAS G12D mutation, and exhibit good pharmacokinetic properties.