Disclosed in the present invention are a compound represented by formula Ib or IIb, a cis or trans isomer, enantiomer, diastereomer, racemate, tautomer, solvate, hydrate, and pharmaceutically acceptable salt thereof, or a mixture thereof, a pharmaceutical composition containing the compound, and a use of the compound as a GPR40 agonist, wherein n, E, G1, L1, L2, R1, R2, R3, R4, R5, R5b, R6, R7, X5, X6, X7, Y, Y1, Z, Z1, and the possible isotopic substitution label of each element in the compound are as defined in the description.
Disclosed in the present invention are a compound represented by formula Ib or IIb, a cis or trans isomer, enantiomer, diastereomer, racemate, tautomer, solvate, hydrate, and pharmaceutically acceptable salt thereof, or a mixture thereof, a pharmaceutical composition containing the compound, and a use of the compound as a GPR40 agonist, wherein n, E, G1, L1, L2, R1, R2, R3, R4, R5, R5b, R6, R7, X5, X6, X7, Y, Y1, Z, Z1, and the possible isotopic substitution label of each element in the compound are as defined in the description.
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 317/54 - Radicals substituted by oxygen atoms
C07D 317/66 - Nitrogen atoms not forming part of a nitro radical
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
2.
BENZO OXYGEN-CONTAINING HETEROCYCLIC COMPOUND AND MEDICAL APPLICATION THEREOF
Disclosed in the present invention are a compound represented by formula Ib or IIb, a cis or trans isomer, enantiomer, diastereomer, racemate, tautomer, solvate, hydrate, and pharmaceutically acceptable salt thereof, or a mixture thereof, a pharmaceutical composition containing the compound, and a use of the compound as a GPR40 agonist, wherein n, E, G1, L1, L2, R1, R2, R3, R4, R5, R5b, R6, R7, X5, X6, X7, Y, Y1, Z, Z1, and the possible isotope substitution label of each element in the compound are as defined in the description.
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/00 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
C07D 407/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group
C07D 307/00 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
3.
BENZO OXYGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND MEDICAL APPLICATION THEREOF
Disclosed in the present invention are a compound represented by formula Ib or IIb, a cis or trans isomer, enantiomer, diastereomer, racemate, tautomer, solvate, hydrate, and pharmaceutically acceptable salt thereof, or a mixture thereof, a pharmaceutical composition containing the compound, and a use of the compound as a GPR40 agonist, wherein n, E, G1, L1, L2, R1, R2, R3, R4, R5, R5b, R6, R7, X5, X6, X7, Y, Y1, Z, Z1, and the possible isotope substitution label of each element in the compound are as defined in the description.
A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
C07D 307/00 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
C07D 405/00 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
C07D 407/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
4.
BENZO OXYGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND MEDICAL APPLICATIONS THEREOF
Disclosed in the present invention are a compound of formula Ia or IIa, a cis-trans isomer, enantiomer, diastereomer, racemate, tautomer, solvate, hydrate, or pharmaceutically acceptable salt thereof or a mixture of said substances, a pharmaceutical composition containing the compound, and a use of the compound as a GPR40 agonist, wherein n, E, E1, G1, L, R1, R2, R3, R4, R5, R5b, R6, R7, Ra, Rb, Rc, Rd, Re, Rf, Rg, Ri, Rj, X1, X2, X3, X4, Y, Y1, Z1, and possible isotope substitution markers for each element in the compound are as defined in the specification.
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
5.
CRYSTAL FORM OF POLYCYCLIC HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, APPLICATIONS THEREOF AND COMPOSITION THEREOF
Disclosed in the present invention are crystal forms of a polycyclic heterocyclic compound, preparation methods therefor, applications thereof and a composition thereof. The present invention provides polymorphic forms of a compound of Formula I. The crystal forms have high purity, good stability and good absorption, are crystalline powder in state and facilitate dispersion, composition, disposition and use of a medicine; the preparation methods for the crystal forms are simple, quick, mild in preparation conditions and stable in yield; the used solvents are environment-friendly and have extremely low toxicity; and the crystal forms of the compound are suitable for large-scale production.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
This patent discloses a group of HCV inhibiting chemical compounds, their stereoisomers, tautomers, isotope isomers, hydrates, esterified or amidated prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions and applications thereof, and the application of the mixture of one or more of these compositions in the preparation of HCV inhibitory drugs. The described compounds can effectively inhibit HCV NS5A, and can be used for preparing medicines for the prevention and treatment of HCV-NS5A infection.(see above formula)
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
7.
COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR INHIBITING HEPATITIS C VIRUS, AND USES THEREOF
Compounds and pharmaceutical compositions for inhibiting the hepatitis c virus (HCV), and uses thereof, are disclosed. The present invention provides compounds as represented by formula (Ia) or (Ib), stereoisomers thereof, tautomers thereof, esterified or amidated prodrugs thereof, and pharmaceutically acceptable salts thereof. The invention further provides for the use of a mixture of one or more of said compounds as represented by formula (Ia) or (Ib), stereoisomers thereof, tautomers thereof, esterified or amidated prodrugs thereof, and pharmaceutically acceptable salts thereof, in preparing a medicament for inhibiting HCV. Compounds of the present invention may effectively inhibit HCV NS5A, and can be used in preparing a medicament for preventing and/or treating the HCV (HCV NS5A) infectious virus. The invention therefore has excellent market potential.
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
Provided are compounds for inhibiting a hepatitis C virus (HCV), stereisomers, tautomers, isotope isomers, hydrates, esterified or amidated prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions thereof and uses thereof, as well as uses of mixtures formed by one or more of the components in the preparation of medicines for inhibiting the HCV. The compounds can effectively inhibit the hepatitis C virus NS5A, and can be used for preparing medicines for preventing and/or treating diseases of the hepatitis C virus (HCV-NS5A) infection.
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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
C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.
C07K 5/083 - Tripeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
10.
Polyheterocyclic compounds highly potent as HCV inhibitors
The present invention discloses the structure, preparation methods and uses of a series of novel polyheterocyclic based compounds (Ia-Ib and IIa-IIb) that are highly effective for inhibiting hepatitis C virus (HCV):
where the structural variables are defined herein. The present invention is also provides a method of treating HCV infection by the polyheterocyclic based HCV inhibitory compounds, compositions and therapeutic methods.
A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
11.
MACROCYCLIC HETEROCYCLIC COMPOUND FOR INHIBITING HEPATITIS C VIRUS AND PREPARATION AND USE THEREOF
Provided is a type of macrocyclic heterocyclic compound as represented by formula Ia and lb, and an intermediate, preparation method, and use thereof. The macrocyclic heterocyclic compound has an inhibition activity against the hepatitis C virus.
The present invention discloses novel polyheterocyclic based compounds having general formula Ia-Ib and IIa-IIb, and preparation methods and uses thereof. These compounds are highly effective for inhibition of hepatitis C virus (HCV). The present invention is also related to treatment of HCV infection by the polyheterocyclic based HCV inhibitory compounds and compositions thereof, and to therapeutic methods thereof.
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
The present invention discloses novel polyheterocyclic based compounds having general formula Ia-Ib and IIa-IIb, and preparation methods and uses thereof. These compounds are highly effective for inhibition of hepatitis C virus (HCV). The present invention is also related to treatment of HCV infection by the polyheterocyclic based HCV inhibitory compounds and compositions thereof, and to therapeutic methods thereof.
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
The present invention discloses the structure, preparation methods and uses of a series of novel polyheterocyclic based compounds (Ia-Ib and IIa-IIb) that are highly effective for inhibiting hepatitis C virus (HCV):
where the structural variables are defined herein. The present invention is also provides a method of treating HCV infection by the polyheterocyclic based HCV inhibitory compounds, compositions and therapeutic methods.
A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
patents
