C07D209/46

Anti-fibrotic compounds

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

METHODS OF MANUFACTURING A BIFUNCTIONAL COMPOUND
20230069491 · 2023-03-02 ·

This disclosure pertains to the preparation of bifunctional compounds (e.g., Compound 1), intermediates in the preparation of such compounds, and preparation of such intermediates.

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Synthesis of N-vinyl compounds by reacting cylic NH-compounds with acetylene in presence of homogenous catalyst

A process can be used to produce N-vinyl compounds by homogeneous catalysis. In the process, acetylene is reacted with a cyclic compound having at least one nitrogen as a ring member, hearing a substitutable hydrogen residue (cyclic compound C), in a liquid phase in the presence of a ruthenium complex containing at least one phosphine as a ligand (RuCat).

SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.

USP30 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of USP30, and the treatment of USP30-mediated disorders.

Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof

The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof

The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

Halo-allylamine SSAO/VAP-1 inhibitor and use thereof
11649233 · 2023-05-16 · ·

The present invention belongs to the pharmaceutical technical field, and specifically relates to a haloallylamine compound represented by formula I, a pharmaceutically acceptable salt, an ester or a stereoisomer thereof, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, L.sub.1, C.sub.y1, R.sub.7 are defined as in the specification; the present invention also relates to pharmaceutical preparations and pharmaceutical compositions containing these compounds, and their use in preventing and/or treating the SSAO/VAP-1 protein-related or SSAO/VAP-1 protein-mediated disease. ##STR00001##

Halo-allylamine SSAO/VAP-1 inhibitor and use thereof
11649233 · 2023-05-16 · ·

The present invention belongs to the pharmaceutical technical field, and specifically relates to a haloallylamine compound represented by formula I, a pharmaceutically acceptable salt, an ester or a stereoisomer thereof, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, L.sub.1, C.sub.y1, R.sub.7 are defined as in the specification; the present invention also relates to pharmaceutical preparations and pharmaceutical compositions containing these compounds, and their use in preventing and/or treating the SSAO/VAP-1 protein-related or SSAO/VAP-1 protein-mediated disease. ##STR00001##

TARGETED NITROXIDE AGENTS

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.