Patent classifications
C07D233/61
SUBSTITUTED 3-AMINO-4-METHYLBENZENESULFONAMIDES AS SMALL MOLECULE INHIBITORS OF UBIQUITIN-SPECIFIC PROTEASE 28
The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof and pharmaceutical composition comprising the compound of formula (I). The present composition also relates to methods treating a disease or disorder associated with ubiquitin-specific protease 28 (USP28), methods of treating cancer, and methods of inhibiting USP28.
##STR00001##
NOVEL AMINO ACID DERIVATIVES
- Naoki OKADA ,
- Kyosuke UEDA ,
- Masatoshi TAKUWA ,
- Shunichi NAKANO ,
- Kotaro TOKUMOTO ,
- Tomoko ASHIZAWA ,
- Shuhei YAMAKOSHI ,
- Yutaka KOBAYASHI ,
- Katsuma MATSUI ,
- Ayumu MATSUDA ,
- Masatoshi MATSUMOTO ,
- Keiichi MASUYA ,
- Atsushi YOSHIZAWA ,
- Masahiko KINEBUCHI ,
- Takeru EHARA ,
- Masami YAMADA ,
- Kouki MORIMOTO ,
- Yoshihide MIZUKOSHI ,
- Haruaki KURASAKI ,
- Motoki MURAI ,
- Kentarou FUKUMOTO ,
- Douglas Robert CARY
A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve solubility of polypeptides comprising the derivative therein.
NOVEL AMINO ACID DERIVATIVES
- Naoki OKADA ,
- Kyosuke UEDA ,
- Masatoshi TAKUWA ,
- Shunichi NAKANO ,
- Kotaro TOKUMOTO ,
- Tomoko ASHIZAWA ,
- Shuhei YAMAKOSHI ,
- Yutaka KOBAYASHI ,
- Katsuma MATSUI ,
- Ayumu MATSUDA ,
- Masatoshi MATSUMOTO ,
- Keiichi MASUYA ,
- Atsushi YOSHIZAWA ,
- Masahiko KINEBUCHI ,
- Takeru EHARA ,
- Masami YAMADA ,
- Kouki MORIMOTO ,
- Yoshihide MIZUKOSHI ,
- Haruaki KURASAKI ,
- Motoki MURAI ,
- Kentarou FUKUMOTO ,
- Douglas Robert CARY
A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve solubility of polypeptides comprising the derivative therein.
Compound used as autophagy regulator, and preparation method therefor and uses thereof
It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators. ##STR00001##
a-CARBONYL ALKENYL ESTER PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.
LIPIDS FOR USE IN LIPID NANOPARTICLE FORMULATIONS
Compounds are provided having the following structure:
##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.3, L.sup.1, L.sup.2, G.sup.1, G.sup.2 and G.sup.3 are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.
Tead inhibitors and uses thereof
The present invention provides compounds, compositions thereof, and methods of using the same.
Compositions and methods for the treatment of oral infectious diseases
The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI and formula XII and, the methods for the treatment of oral infectious diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral infectious diseases.
Compositions and methods for the treatment of oral infectious diseases
The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI and formula XII and, the methods for the treatment of oral infectious diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral infectious diseases.
ISOTOPE-ENRICHED 3-AMINO-1-PROPANESULFONIC ACID DERIVATIVES AND USES THEREOF
There are provided isotope-enriched compounds of Formula (I) and pharmaceutically acceptable salts or esters thereof, as well as pharmaceutical compositions thereof and methods of use thereof for prevention and treatment of amyloid-β related diseases, such as Alzheimer's disease.
R.sup.1R.sup.2X—CR.sub.2—CH.sub.2—CH.sub.2—SO.sub.3H (I)