C07D279/06

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.

PROCESS AND INTERMEDIATES FOR PREPARATION OF THIAZINE DERIVATIVES

The present invention provides a process for preparation of the compound of formula (VI), wherein each symbol is as defined in the specification, without using any intermediate compound showing mutagenicity. The process comprises salt formation of the intermediate compound of formula (I) with acid to enable optical resolution to isolate the intermediate compound of formula (II) in a stereo-selective manner.

##STR00001##

PROCESS AND INTERMEDIATES FOR PREPARATION OF THIAZINE DERIVATIVES

The present invention provides a process for preparation of the compound of formula (VI), wherein each symbol is as defined in the specification, without using any intermediate compound showing mutagenicity. The process comprises salt formation of the intermediate compound of formula (I) with acid to enable optical resolution to isolate the intermediate compound of formula (II) in a stereo-selective manner.

##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.

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.

SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS
20180265524 · 2018-09-20 ·

This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS
20180265524 · 2018-09-20 ·

This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides

The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) ##STR00001## in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, n have the meanings given in the descriptionto their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.

N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides

The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) ##STR00001## in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, n have the meanings given in the descriptionto their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.