Related to macrocyclic compounds and therapeutic uses thereof. Discloses 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.
C07D 487/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains three hetero rings
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
A61K 31/504 - PyridazinesHydrogenated pyridazines forming part of bridged ring systems
The present application relates to the field of pharmaceutical chemistry. Specifically, the present application relates to a triaromatic ring derivative, specifically a salt of (6-((5-(3-(4-(trifluoromethyl)phenyl)-1,2,4-oxadiazole-5-yl)pyrazine-2-yl)oxy)-1-methyl-1H-indol-2-yl)(4-(4-(2,2,2-trifluoroethoxy)benzyl)piperazin-1-yl)methanone, a crystal form thereof, a pharmaceutical composition thereof, a preparation method therefor, and a use thereof. The salt and the crystal form thereof provided in the present application have good stability, high solubility, high bioavailability, good efficacy, good tablet dissolution, good tablet compressibility, good fluidity, good crystal morphology, good crystal particle size distribution, can be stably stored, and have a simple and reliable preparation method and great development value.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
The present invention relates to a novel boron containing compounds and a pharmaceutical acceptable salt thereof, and their use for the preparation of a medicament of treatment of cancer. The compounds in the present disclosure have specifically ability to kill ERa positive cancer cells and show dramatically therapeutical potential.
Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist (S)-4-(1-(2-(4-fluorobenzyl)-4, 7-dihydro-5H-thieno [2,3-c]pyran-3-carboxamido) ethyl) benzoic acid, a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine
Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist ( S)-4-(1-(2-( 4-fluorobenzyl)-4, 7-dihydro-SH-thieno [2,3-c ] pyran-3- carboxamido) ethyl) benzoicacid,a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine.
Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist (S)-4-(1-(2-(4-fluorobenzyl) )-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxamido)ethyl)benzoic acid, a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine.
Disclosed by the present invention are a thienocyclic compound represented by formula (I), a pharmaceutically acceptable salt or a hydrate thereof, a composition containing the thienocyclic compound, and a preparation method therefor. Further disclosed by the present invention is an application of the thienocyclic compound as a prostaglandin EP4 receptor antagonist that is used for preventing and treating prostaglandin PGE2-mediated diseases, comprising malignant tumors, autoimmune diseases, inflammation, pain and osteoarthritis
Disclosed by the present invention are a thienocyclic compound represented by formula (I), a pharmaceutically acceptable salt or a hydrate thereof, a composition containing the thienocyclic compound, and a preparation method therefor. Further disclosed by the present invention is an application of the thienocyclic compound as a prostaglandin EP4 receptor antagonist that is used for preventing and treating prostaglandin PGE2-mediated diseases, comprising malignant tumors, autoimmune diseases, inflammation, pain and osteoarthritis
C07D 333/78 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
C07D 333/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Provided is a combination of an EP4 receptor antagonist and a PD-1 inhibitor for treating cancer. Specifically, provided is a product combination comprising: (i) a first pharmaceutical composition comprising (a) a first active ingredient, where the first active ingredient comprises an EP4 receptor antagonist and a pharmaceutically acceptable carrier; and (ii) a second pharmaceutical composition comprising (b) a second active ingredient, where the second active ingredient comprises a PD-1 inhibitor and a pharmaceutically acceptable carrier. The first pharmaceutical composition and the second pharmaceutical composition are different pharmaceutical compositions or the same pharmaceutical composition. The product combination of the present invention can synergistically treat malignant tumors.
C07D 333/78 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
C07D 333/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Disclosed are a class of triaromatic compounds targeting a bifunctional phosphorylation site of STAT3, such as compounds represented by formulas (I) to (V), or pharmaceutically acceptable salts, hydrates, solvates, metabolites or prodrugs thereof. Further proposed are pharmaceutical compositions comprising the compounds represented by formulas (I) to (V). Further proposed are applications of the triaromatic compounds in the preparation of drugs for preventing and/or treating diseases caused or regulated by activation of the bifunctional phosphorylation site of STAT3.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
10.
CLASS OF TRIAROMATIC COMPOUNDS TARGETING BIFUNCTIONAL PHOSPHORYLATION SITE OF STAT3 AND APPLICATIONS THEREOF
Disclosed are a class of triaromatic compounds targeting a bifunctional phosphorylation site of STAT3, such as compounds represented by formulas (I) to (V), or pharmaceutically acceptable salts, hydrates, solvates, metabolites or prodrugs thereof. Further proposed are pharmaceutical compositions comprising the compounds represented by formulas (I) to (V). Further proposed are applications of the triaromatic compounds in the preparation of drugs for preventing and/or treating diseases caused or regulated by activation of the bifunctional phosphorylation site of STAT3.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
patents
