C07D211/40

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
20210145771 · 2021-05-20 ·

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.

OXIME ETHER COMPOUNDS
20210147361 · 2021-05-20 ·

Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CH or N; Y is CH or N; R.sub.1 is —OH or —OP(O)(OH).sub.2; L.sub.1 is —CR.sub.3═N—O—CR.sub.aR.sub.a— or CR.sub.aR—O—N═CR.sub.3; L.sub.2 is a bond, —C(O)—, or S(O).sub.2—; and R.sub.2, R.sub.3, R.sub.a, m, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

##STR00001##

OXIME ETHER COMPOUNDS
20210147361 · 2021-05-20 ·

Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CH or N; Y is CH or N; R.sub.1 is —OH or —OP(O)(OH).sub.2; L.sub.1 is —CR.sub.3═N—O—CR.sub.aR.sub.a— or CR.sub.aR—O—N═CR.sub.3; L.sub.2 is a bond, —C(O)—, or S(O).sub.2—; and R.sub.2, R.sub.3, R.sub.a, m, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

##STR00001##

IMMUNOMODULATOR COMPOUNDS

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I):

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

IMMUNOMODULATOR COMPOUNDS

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I):

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

IMMUNOMODULATOR COMPOUNDS

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II):

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

IMMUNOMODULATOR COMPOUNDS

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II):

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Oxime ether compounds

Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CH or N; Y is CH or N; R.sub.1 is OH or OP(O)(OH).sub.2; L is CR.sub.3NOCR.sub.aR.sub.a or CR.sub.aRONCR.sub.3; L.sub.2 is a bond, C(O), or S(O).sub.2; and R.sub.2, R.sub.3, R.sub.a, m, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##

Oxime ether compounds

Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CH or N; Y is CH or N; R.sub.1 is OH or OP(O)(OH).sub.2; L is CR.sub.3NOCR.sub.aR.sub.a or CR.sub.aRONCR.sub.3; L.sub.2 is a bond, C(O), or S(O).sub.2; and R.sub.2, R.sub.3, R.sub.a, m, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##

Biaryl piperidine amide compounds and methods of use thereof

The present application is directed to biaryl piperidine amide compounds, or pharmaceutically acceptable salts, solvates, and prodrugs thereof, and methods of use thereof.