Patent classifications
C07C237/04
Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
N-(3-(2-(4-CHLOROPHENOXY)ACETAMIDO)BICYCLO[1.1.1] PENTAN-1-YL)-2-CYCLOBUTANE-1- CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ATF4 INHIBITORS FOR TREATING CANCER AND OTHER DISEASES
The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula I:
##STR00001##
wherein X, a, b, C, D, L.sup.2, L.sup.3, Y.sup.1, Y.sup.2, R.sup.2, R.sup.4, R.sup.5, R.sup.6, z.sup.2, z.sup.4, z.sup.5, and z.sup.6 are as defined herein, and salts thereof.
The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
N-(3-(2-(4-CHLOROPHENOXY)ACETAMIDO)BICYCLO[1.1.1] PENTAN-1-YL)-2-CYCLOBUTANE-1- CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ATF4 INHIBITORS FOR TREATING CANCER AND OTHER DISEASES
The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula I:
##STR00001##
wherein X, a, b, C, D, L.sup.2, L.sup.3, Y.sup.1, Y.sup.2, R.sup.2, R.sup.4, R.sup.5, R.sup.6, z.sup.2, z.sup.4, z.sup.5, and z.sup.6 are as defined herein, and salts thereof.
The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Radiopaque monomers, polymers, microspheres, and methods related thereto
Radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of using the radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of manufacturing radiopaque monomers, polymers, and microspheres are disclosed herein.
QUATERNARY AMMONIUM SALT COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
A compound is shown in formula I and can be in the form of a pharmaceutically acceptable salt, or a stereoisomer, or a solvate, or a prodrug, or a metabolite. The compound takes effect rapidly and has a long-time local anesthetic effect following a single dose, with the sensory nerve blocking time being greater than the motor nerve blocking time, has both a long-acting local anesthetic effect and a selective local anesthetic effect, significantly reduces side effects of the compositions QX314 and QX314 and a quaternary ammonium salt compound with surfactant structural characteristics, and is safer. The compound of formula I of the present invention and a pharmaceutically acceptable salt thereof can be used for preparing drugs that have a long-time local anesthetic effect and a selective local anesthetic effect.
QUATERNARY AMMONIUM SALT COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
A compound is shown in formula I and can be in the form of a pharmaceutically acceptable salt, or a stereoisomer, or a solvate, or a prodrug, or a metabolite. The compound takes effect rapidly and has a long-time local anesthetic effect following a single dose, with the sensory nerve blocking time being greater than the motor nerve blocking time, has both a long-acting local anesthetic effect and a selective local anesthetic effect, significantly reduces side effects of the compositions QX314 and QX314 and a quaternary ammonium salt compound with surfactant structural characteristics, and is safer. The compound of formula I of the present invention and a pharmaceutically acceptable salt thereof can be used for preparing drugs that have a long-time local anesthetic effect and a selective local anesthetic effect.
Charged ion channel blockers and methods for use
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001##
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
Charged ion channel blockers and methods for use
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001##
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
AMINOMETHYL-FUNCTIONALIZED DENATONIUM DERIVATIVES, THEIR PREPARATION AND USE
The present invention is directed to compounds of the general formula (I) and salts thereof
##STR00001##
wherein X.sup. is halide, pseudohalide, sulphate, benzoate, acetate, trifluoroacetate, hydroxide, saccharinate or capsaicinate; R.sup.10 is hydrogen or C1-C10-alkyl; and R.sup.1-R.sup.9 independently are hydrogen, halogen, C1-C5-alkyl, C1-C4-alkoxy, C1-C20-alkoxycarbonyl. The invention is furthermore directed to a method for the preparation of these compounds. The compounds can be used as bitter substances in medicine, pharmaceutics and/or diagnostics. They can furthermore be used for the coupling to proteins and peptides by means of forming a peptide bond between the amino-group of the compounds of the present invention and a carboxyl-group of the protein or peptide.