C07D211/38

Benzimidazole Derivatives as Modulators of Retinoid-Related Orphan Receptor Gamma (RORy) and Pharmaceutical Uses Thereof

The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders.

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QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

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comprising treating a compound of Formula (I):

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with a transition metal catalyst and under alkylation conditions as valence and stability permit.

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

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comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

DOPAMINE D2 RECEPTOR LIGANDS

The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

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:

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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
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.

IMMUNOMODULATOR COMPOUNDS

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

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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.

SSAO INHIBITORS AND USE THEREOF
20210147360 · 2021-05-20 ·

The application relates to a compound of Formula (I′) or (I):

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or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.

HYDROFLUOROOLEFIN ETHERS, COMPOSITIONS, APPARATUSES AND METHODS FOR USING SAME
20210101858 · 2021-04-08 ·

A hydrofluoroolefin ether represented by the general Formula (I), compositions that include such compounds, and apparatuses and methods for use that include such compositions and compounds, wherein Formula (I) is represented by: R.sub.f—O—CH.sub.2CH═CHCH.sub.2—O—R.sub.f (I) wherein each Rf group is independently a linear, branched, and/or cyclic perfluoroalkyl group having 2 to 9 carbon atoms and optionally further including 1 to 3 nitrogen and/or oxygen catenary heteroatoms.


R.sub.f—O—CH.sub.2CH═CHCH.sub.2—O—R.sub.f   (I)