C07D217/22

ARYL CYCLOPROPYL-AMINO-ISOQUINOLINYL AMIDE COMPOUNDS

Provided herein are arylcyclopropyl amino-isoquinoline amide compounds. In particular, the disclosure 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 disclosure are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, diseases characterized by abnormal growth, such as cancers, and inflammatory diseases. The disclosure further provides compositions containing isoquinoline amide compounds.

IRE1 small molecule inhibitors

Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

IRE1 small molecule inhibitors

Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

FUSED RING COMPOUND AND APPLICATION THEREOF

Disclosed is a fused ring compound and an application thereof. Disclosed is a fused ring compound represented by formula I, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, an isotope compound, a crystal form, a nitrogen oxide, a solvate, or a solvate of the pharmaceutically acceptable salt thereof. The fused ring compound of the present invention has high P2X4 antagonistic activity, excellent selectivity, low toxicity and excellent metabolic stability.

##STR00001##

1,3-SUBSTITUTED CYCLOBUTYL DERIVATIVES AND USES THEREOF
20220324811 · 2022-10-13 ·

Provided herein are compounds and pharmaceutical compositions useful for treating diseases or disorders mediated by the TRPV1 receptor. The present invention also provides methods for treating ocular diseases or disorders by administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I) or a pharmaceutical composition described herein.

##STR00001##

Sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I): ##STR00001##
wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the α-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Compounds for the treatment of acute and chronic kidney disease

The present disclosure is concerned with thioquinolinone compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Compounds for the treatment of acute and chronic kidney disease

The present disclosure is concerned with thioquinolinone compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

CHARGED ION CHANNEL BLOCKERS AND METHODS FOR USE
20230107360 · 2023-04-06 ·

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts 5 thereof:

##STR00001##

The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.