Patent classifications
C07D295/15
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##
CURCUSONE DITERPENOIDS AND USES THEREOF
The present disclosure provides the first asymmetric total synthesis and target identification of the curcusone natural products. The novel convergent synthesis is built upon a cheap and abundant chiral pool molecule (8) and features a thermal [3,3]-sigmatropic rearrangement and an FeCl3-promoted global hydrolysis/adol condensation cascade to rapidly construct the critical cycloheptadienone core. By performing chemoproteomics with the alkyne probe 37, we identified the previously “undruggable” oncogenic protein BRAT1 as a key cellular target of 1d. Furthermore, 1d inhibits BRAT1 in cancer cells, thereby reducing cancer cell migration, increasing susceptibility to DNA damage, and inducing chemosensitization to the approved drug etoposide. Compound 1d is the first known small-molecule inhibitor for BRAT1, a master regulator of the DDR and DNA repair. Composition matters and methods of uses are within the scope of this disclosure.
Process and intermediates for the preparation of benzo[b]thiophene compounds
A process for preparing compounds of formula (I), or a salt or solvate thereof, including Brexpiprazole, which process comprises cyclization of a compound of formula (II) or (III), or a salt or solvate thereof. The invention also refers to intermediates of said process. ##STR00001##
Process and intermediates for the preparation of benzo[b]thiophene compounds
A process for preparing compounds of formula (I), or a salt or solvate thereof, including Brexpiprazole, which process comprises cyclization of a compound of formula (II) or (III), or a salt or solvate thereof. The invention also refers to intermediates of said process. ##STR00001##
Lithium-ion battery and apparatus
The present application provides a lithium-ion battery and an apparatus, and the lithium-ion battery includes an electrode assembly and an electrolytic solution, the electrode assembly includes a positive electrode sheet, a negative electrode sheet and a separation film. A positive active material of the positive electrode sheet includes Li.sub.x1Co.sub.y1M.sub.1-yO.sub.2-z1Q.sub.z1, 0.5≤x1≤1.2, 0.8≤y1≤1.0, 0≤z1≤0.1, M is selected from one or more of Al, Ti, Zr, Y, and Mg, and Q is selected from one or more of F, Cl, and S. The electrolytic solution contains vinylene carbonate, fluoroethylene carbonate, 1,3-propane sultone, and an additive A. The additive A is a polynitrile six-membered nitrogen-heterocyclic compound with a relatively low oxidation potential. The lithium-ion battery has superb cycle performance and storage performance, especially under high-temperature and high-voltage conditions.
Lithium-ion battery and apparatus
The present application provides a lithium-ion battery and an apparatus, and the lithium-ion battery includes an electrode assembly and an electrolytic solution, the electrode assembly includes a positive electrode sheet, a negative electrode sheet and a separation film. A positive active material of the positive electrode sheet includes Li.sub.x1Co.sub.y1M.sub.1-yO.sub.2-z1Q.sub.z1, 0.5≤x1≤1.2, 0.8≤y1≤1.0, 0≤z1≤0.1, M is selected from one or more of Al, Ti, Zr, Y, and Mg, and Q is selected from one or more of F, Cl, and S. The electrolytic solution contains vinylene carbonate, fluoroethylene carbonate, 1,3-propane sultone, and an additive A. The additive A is a polynitrile six-membered nitrogen-heterocyclic compound with a relatively low oxidation potential. The lithium-ion battery has superb cycle performance and storage performance, especially under high-temperature and high-voltage conditions.
CRYSTALLINE FORMS OF ERAVACYCLINE
The invention relates to crystalline forms of the bis-HCl salt of a compound represented by Structural Formula 1, and pharmaceutical compositions comprising crystalline forms of the bis-HCL salt of a compound represented by Structural Formula 1 described herein. The crystalline forms of the bis-HCl salt of a compound of Structural Formula 1 and compositions comprising the crystalline forms of the compound of Structural Formula 1 provided herein, in particular, crystalline Form I, crystalline Form J, crystalline Form A, and crystalline Form B, or mixtures thereof, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders. Also described herein are methods for preparing the crystalline forms (e.g., Forms I, J, B and A) of the bis-HCl salt of a compound represented by Structural Formula 1.
CRYSTALLINE FORMS OF ERAVACYCLINE
The invention relates to crystalline forms of the bis-HCl salt of a compound represented by Structural Formula 1, and pharmaceutical compositions comprising crystalline forms of the bis-HCL salt of a compound represented by Structural Formula 1 described herein. The crystalline forms of the bis-HCl salt of a compound of Structural Formula 1 and compositions comprising the crystalline forms of the compound of Structural Formula 1 provided herein, in particular, crystalline Form I, crystalline Form J, crystalline Form A, and crystalline Form B, or mixtures thereof, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders. Also described herein are methods for preparing the crystalline forms (e.g., Forms I, J, B and A) of the bis-HCl salt of a compound represented by Structural Formula 1.
Modified conjugated diene-based polymer and method of preparing the same
The present invention relates to a modifier represented by Formula 1, a method of preparing the same, a modified conjugated diene-based polymer having a high modification ratio which includes a modifier-derived functional group, and a method of preparing the polymer.