Patent classifications
C07D211/42
SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF
- Jean-Christophe Andrez ,
- Paul Robert Bichler ,
- Chien-An CHEN ,
- Sultan Chowdhury ,
- Shannon Marie Decker ,
- Christoph Martin Dehnhardt ,
- Thilo Focken ,
- Michael Edward Grimwood ,
- Ivan William HEMEON ,
- Qi Jia ,
- Jun LI ,
- Zhiguo Liu ,
- Daniel F. ORTWINE ,
- Brian Salvatore Safina ,
- Daniel SUTHERLIN ,
- Tao SHENG ,
- Shaoyi Sun ,
- Andrew D. WHITE ,
- Michael Scott Wilson ,
- Alla Yurevna Zenova ,
- Jiuxiang Zhu
The invention provides compounds having the general formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.A, R.sup.AA, subscript n, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Cyclohexene compounds and use thereof
A cyclohexene compound and use thereof, which relates to the technical field of pharmaceutical chemistry is provided. The cyclohexene compound is the cyclohexene compound having a structural formula I or a pharmaceutically acceptable salt, an ester group prodrug or a stereoisomer thereof. It is verified by activity assay for influenza NA that the cyclohexene compound has a great inhibiting activity against both wild-typed and drug-resistant influenza viruses, and the inhibiting activity IC.sub.50 of some compounds against wild-typed and drug-resistant influenza viruses is lower than 5 nM, showing significant inhibiting effect on influenza viruses. This shows that the cyclohexene compound or a pharmaceutically acceptable salt or a stereoisomer thereof has superior application prospect on preparing anti-influenza drugs, thereby providing a new drug choice for treating influenza clinically.
Cyclohexene compounds and use thereof
A cyclohexene compound and use thereof, which relates to the technical field of pharmaceutical chemistry is provided. The cyclohexene compound is the cyclohexene compound having a structural formula I or a pharmaceutically acceptable salt, an ester group prodrug or a stereoisomer thereof. It is verified by activity assay for influenza NA that the cyclohexene compound has a great inhibiting activity against both wild-typed and drug-resistant influenza viruses, and the inhibiting activity IC.sub.50 of some compounds against wild-typed and drug-resistant influenza viruses is lower than 5 nM, showing significant inhibiting effect on influenza viruses. This shows that the cyclohexene compound or a pharmaceutically acceptable salt or a stereoisomer thereof has superior application prospect on preparing anti-influenza drugs, thereby providing a new drug choice for treating influenza clinically.
COMPOUND OR SALT THEREOF AND LIPID PARTICLES
An object of the present invention is to provide a compound or a salt thereof constituting lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids, and to provide lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids. According to an aspect of the present invention, a compound represented by Formula (1) or a salt thereof is provided.
##STR00001##
In the formula, X represents NR.sup.1 or O, R represents a hydrogen atom, a hydrocarbon group, or the like, R.sup.2 and R.sup.3 each independently represent a hydrogen atom, a hydrocarbon group, or the like, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, and R.sup.12 each independently represent a hydrogen atom or an alkyl group, groups in any one or more pairs among R.sup.4 and R.sup.5, R.sup.10 and R.sup.5, R.sup.5 and R.sup.12, R.sup.4 and R.sup.6, R.sup.5 and R.sup.6, R.sup.6 and R.sup.7, R.sup.6 and R.sup.10, R.sup.12 and R.sup.7, and R.sup.7 and R.sup.8 may be linked to each other to form a 4- to 7-membered ring which may contain an O atom, a, b, c, and d are each independently represent an integer of 0 to 3, a+b is equal to or greater than 1, and c+d is equal to or greater than 1.
FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS
Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I).
##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.
METHODS OF REDUCING INFLAMMATION OF THE DIGESTIVE SYSTEM WITH INHIBITORS OF HIF-2- ALPHA
The present disclosure provides methods of reducing inflammation of the digestive system in a subject in need thereof, including subjects suffering from inflammatory bowel disease. Compositions for use in these methods are also provided.
Substituted oxazoles for the treatment of cancer
There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders. ##STR00001##
Substituted oxazoles for the treatment of cancer
There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders. ##STR00001##