C07D241/06

INHIBITORS FOR PROGRAMMED CELL NECROSIS AND PREPARATION METHOD THEREFOR AND USE THEREOF
20220213077 · 2022-07-07 ·

Provided in the present invention are inhibitors for programmed cell necrosis, a preparation method therefor and a use thereof. Specifically, provided in the present invention are a compound represented by formula I and a composition comprising same. The described compound may be used to prepare a pharmaceutical composition for the prevention and/or treatment of diseases involving cell death and/or inflammation.

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ANTIBODY AGAINST ADVANCED GLYCATION END PRODUCTS AND USE THEREOF

The present invention is directed to providing a monoclonal antibody having high selectivity and affinity for AGEs, particularly, AGEs derived from glyceraldehyde or AGEs derived from glycolaldehyde, and an analysis method utilizing the same. Another object of the present invention is to provide methods for diagnosing, treating and preventing a disease using the monoclonal antibody.

N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE

The invention relates to compounds of formula (I):

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or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.

N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE

The invention relates to compounds of formula (I):

##STR00001##

or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.

Methods for the synthesis of activated ethylfumarates and their use as intermediates

Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.

CONTRAST AGENTS FOR MAGNETIC RESONANCE IMAGING

The present invention provides contrast agents of the formula [N(A.sub.1,A.sub.2,A.sub.3) M](counter ion(s)) for use in a diagnostic method practiced on the human or animal body. It also refers to the contrast agents, as well as pharmaceutical compositions containing same. Further, it relates to a method of in vitro medical imaging, especially of diagnostic imaging, comprising administering said compound to a sample.

CONTRAST AGENTS FOR MAGNETIC RESONANCE IMAGING

The present invention provides contrast agents of the formula [N(A.sub.1,A.sub.2,A.sub.3) M](counter ion(s)) for use in a diagnostic method practiced on the human or animal body. It also refers to the contrast agents, as well as pharmaceutical compositions containing same. Further, it relates to a method of in vitro medical imaging, especially of diagnostic imaging, comprising administering said compound to a sample.

MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE

Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases such as chronic viral infection, chronic bacterial infections, cancer, sepsis or a neurological disorder.

##STR00001##

N-acyl amino acid compounds and methods of use

The invention relates to compounds of formula (I): ##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.

N-acyl amino acid compounds and methods of use

The invention relates to compounds of formula (I): ##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.