Patent classifications
C07D211/10
CYCLIC PEPTIDE COMPOUND HAVING KRAS INHIBITORY ACTION
The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.
IDO inhibitors
- James Aaron Balog ,
- Emily Charlotte Cherney ,
- Weiwei Guo ,
- Audris Huang ,
- Jay A. Markwalder ,
- Steven P. Seitz ,
- Weifang Shan ,
- David K. Williams ,
- Natesan Murugesan ,
- Susheel Jethanand Nara ,
- Saumya Roy ,
- Soodamani Thangavel ,
- Ramesh Kumar Sistla ,
- Srinivas Cheruku ,
- Srinivasan Thangathirupathy ,
- Yadagiri Kanyaboina ,
- Nagalakshmi Pulicharla
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Production and use of zinc amides
Compounds, methods of making the compounds and methods of using the compounds are generally described herein. The compounds are generally of formula R.sup.1R.sup.2NZnY LiY, wherein R.sup.1 and R.sup.2 are independently selected from H, aryl, heteroaryl containing one or more heteroatoms, alkyl, alkenyl, alkynyl, and silicon derivatives thereof; and each Y is independently selected from F, Cl, Br, I, CN, SCN, NCO, HalO.sub.3, HalO.sub.4, NO.sub.3, BF.sub.4, PF.sub.6, H, an alcoholate of formula OR.sup.5, a carboxylate of formula R.sup.5CO.sub.2; a thiolate of formula SR.sup.5, R.sup.5P(O)O.sub.2, SCOR.sup.5, SCSR.sup.5, O.sub.nSR.sup.5 and NO.sub.n, wherein n=2 or 3; wherein R.sup.5 is selected from substituted or unsubstituted aryls or heteroaryls containing 3 to 24 carbon atoms and one or more heteroatoms selected from B, O, N, S, Se, P, linear, branched or cyclic, substituted or unsubstituted alkyls, alkenyls, alkynyls or H; and wherein Hal is a halogen selected from Cl, Br and I.
Production and use of zinc amides
Compounds, methods of making the compounds and methods of using the compounds are generally described herein. The compounds are generally of formula R.sup.1R.sup.2NZnY LiY, wherein R.sup.1 and R.sup.2 are independently selected from H, aryl, heteroaryl containing one or more heteroatoms, alkyl, alkenyl, alkynyl, and silicon derivatives thereof; and each Y is independently selected from F, Cl, Br, I, CN, SCN, NCO, HalO.sub.3, HalO.sub.4, NO.sub.3, BF.sub.4, PF.sub.6, H, an alcoholate of formula OR.sup.5, a carboxylate of formula R.sup.5CO.sub.2; a thiolate of formula SR.sup.5, R.sup.5P(O)O.sub.2, SCOR.sup.5, SCSR.sup.5, O.sub.nSR.sup.5 and NO.sub.n, wherein n=2 or 3; wherein R.sup.5 is selected from substituted or unsubstituted aryls or heteroaryls containing 3 to 24 carbon atoms and one or more heteroatoms selected from B, O, N, S, Se, P, linear, branched or cyclic, substituted or unsubstituted alkyls, alkenyls, alkynyls or H; and wherein Hal is a halogen selected from Cl, Br and I.
N-Acylethanolamine Hydrolyzing Acid Amidase (NAAA) Inhibitors And Their Use Thereof
A compound is represented as Formula I, a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Compounds of Formula I are inhibitors of N-acylethanolamine hydrolyzing acid amidase (NAAA). The present technology is directed to compounds, compositions, and methods to inhibit N-acylethanolamine hydrolyzing acid amidase and to treat N-acylethanolamine hydrolyzing acid amidase mediated conditions in a subject.
Solenopsin and derivatives, therapeutic compositions; and methods related thereto
This disclosure relates to solenopsin derivatives, pharmaceutical compositions, and therapeutic uses related thereto. In certain embodiments, the disclosure relates to compounds of the following formula: ##STR00001## or salts, esters or prodrugs thereof as described herein.
Solenopsin and derivatives, therapeutic compositions; and methods related thereto
This disclosure relates to solenopsin derivatives, pharmaceutical compositions, and therapeutic uses related thereto. In certain embodiments, the disclosure relates to compounds of the following formula: ##STR00001## or salts, esters or prodrugs thereof as described herein.
AMINO LIPID COMPOUND, PREPARATION METHOD THEREFOR, COMPOSITION THEREOF AND USE THEREOF
The present disclosure relates to an amino lipid compound, a preparation method therefor, a composition thereof and the use thereof. Specifically, the present disclosure relates to an amino lipid compound represented by formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof, and the use thereof in the formulation of a lipid nanoparticle for delivering an active ingredient. The present disclosure also relates to a composition containing the amino lipid compound, and in particular relates to a lipid nanoparticle and the use thereof.
##STR00001##
AMINO LIPID COMPOUND, PREPARATION METHOD THEREFOR, COMPOSITION THEREOF AND USE THEREOF
The present disclosure relates to an amino lipid compound, a preparation method therefor, a composition thereof and the use thereof. Specifically, the present disclosure relates to an amino lipid compound represented by formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof, and the use thereof in the formulation of a lipid nanoparticle for delivering an active ingredient. The present disclosure also relates to a composition containing the amino lipid compound, and in particular relates to a lipid nanoparticle and the use thereof.
##STR00001##
LIGHT-EMITTING RADICAL CATION PROBE IN SITU GENERATED BY ACID INDUCTION, AND PREPARATION THEREFOR AND APPLICATION THEREOF
The present invention belongs to a technical field of a medical material. Disclosed are a light-emitting radical cation probe generated in situ by acid induction, and preparation therefor and application thereof. The light-emitting radical cation probe is obtained by oxidation of a compound of formula I in an acidic condition, and has a structure of formula II. A preparation method for the light-emitting radical cation probe is further disclosed. The radical cation probe of the present invention is generated by an in situ reaction in an acidic environment without a seperation, has the advantages of emitting red to near-infrared light, high generation efficiency and good stability, and can be used in fluorescence imaging. The radical cation probe of the present invention can achieve in situ imaging in an acidic stomach environment and gastrointestinal imaging. The probe of the present invention is further used in preparing a probe for monitoring and measuring a food digestion process in a stomach or preparing a reagent for monitoring and measuring treatment of anti-gastric drug that neutralizes gastric acid.
##STR00001##