Patent classifications
C07D207/20
A CONJUGATION LINKER CONTAINING 2,3-DIAMINOSUCCINYL GROUP
- Robert Yongxin Zhao ,
- Qingliang YANG ,
- Yuanyuan HUANG ,
- Linyao ZHAO ,
- Hangbo YE ,
- Xiaotao ZHUO ,
- Chengyu YANG ,
- Jun LEI ,
- Yifang XU ,
- Huihui GUO ,
- Wenjun LI ,
- Shun GAI ,
- Lu BAI ,
- Zhixiang GUO ,
- Junxiang JIA ,
- Jun ZHENG ,
- Xiaomai ZHOU ,
- Hongsheng XIE ,
- Qianqian TONG ,
- Mingjun CHAO ,
- Yanhong TONG ,
- Zhicang YE ,
- Chen LIN ,
- Yanlei YANG ,
- Binbin CHEN
The present invention relates to a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (a dual-linker) containing a 2,3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.
AZOLINE COMPOUNDS SUBSTITUTED BY A CARBOCYCLIC CONDENSED RING SYSTEM
Compounds of formula (I)
##STR00001##
as defined herein are provided. Uses of these compounds for controlling invertebrate pests, protecting plant propagation material and providing an agricultural and a veterinary composition including the compounds are also described. Compounds for use as intermediate compounds in the preparation of compounds I are also described.
AZOLINE COMPOUNDS SUBSTITUTED BY A CARBOCYCLIC CONDENSED RING SYSTEM
Compounds of formula (I)
##STR00001##
as defined herein are provided. Uses of these compounds for controlling invertebrate pests, protecting plant propagation material and providing an agricultural and a veterinary composition including the compounds are also described. Compounds for use as intermediate compounds in the preparation of compounds I are also described.
NOVEL SMALL MOLECULE SHC BLOCKERS USED FOR TREATING LIVER DISEASE AND METABOLIC DISEASE
The subject matter disclosed herein is directed to novel She inhibitors of Formula (II). These compounds are useful for treating impaired insulin sensitivity, glucose tolerance, obesity, diabetes, metabolic syndrome, NAFLD, NASH, PSC, PBC, or other metabolic syndrome component conditions.
##STR00001##
NOVEL SMALL MOLECULE SHC BLOCKERS USED FOR TREATING LIVER DISEASE AND METABOLIC DISEASE
The subject matter disclosed herein is directed to novel She inhibitors of Formula (II). These compounds are useful for treating impaired insulin sensitivity, glucose tolerance, obesity, diabetes, metabolic syndrome, NAFLD, NASH, PSC, PBC, or other metabolic syndrome component conditions.
##STR00001##
ARYL HETEROCYCLIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
##STR00001##
Acyclic carbene ligand for ruthenium complex formation, ruthenium complex catalyst, and use thereof
Provided are a novel acyclic carbene ligand for ruthenium complex formation; a ruthenium complex catalyst using the ligand; a method of using the complex as a catalyst in an ethylene-metathesis ethenolysis reaction; a method of preparing the ruthenium complex catalyst; and a method of preparing a linear alpha-olefin, the method including the step of reacting a linear or cyclic alkene compound in the presence of the ruthenium complex catalyst. The acyclic carbene ligand of the present invention and the ruthenium complex catalyst using the same have high selectivity and turnover number for terminal olefin formation in an ethylene-metathesis ethenolysis reaction, and thus linear α-olefins may be prepared with a high yield.
Acyclic carbene ligand for ruthenium complex formation, ruthenium complex catalyst, and use thereof
Provided are a novel acyclic carbene ligand for ruthenium complex formation; a ruthenium complex catalyst using the ligand; a method of using the complex as a catalyst in an ethylene-metathesis ethenolysis reaction; a method of preparing the ruthenium complex catalyst; and a method of preparing a linear alpha-olefin, the method including the step of reacting a linear or cyclic alkene compound in the presence of the ruthenium complex catalyst. The acyclic carbene ligand of the present invention and the ruthenium complex catalyst using the same have high selectivity and turnover number for terminal olefin formation in an ethylene-metathesis ethenolysis reaction, and thus linear α-olefins may be prepared with a high yield.
FUNCTIONALIZED 1,3-BENZENE DIOLS AND THEIR METHOD OF USE FOR THE TREATMENT OF RADIATION DERMATITIS AND OTHER SKIN DISORDERS
Methods, compounds and compositions for treating and preventing dermatological disorders and ocular irritancy are disclosed. The compounds and compositions comprise a functionalized 1,3-benzene diol, such as 5-(2-(1H-1,2,3-triazol-1-yl)ethyl)-2-((1R,6R)-3-methyl-6-(prop-1-en-2-yl)cyclohex-2-enyl)benzene-1,3-diol and ethyl 3-(3,5-dihydroxy-4-((1R,6R)-3-methyl-6-(prop-1-en-2-yl)cyclohex-2-enyl)benzyl)azetidine-1-carboxylate.
COMPOSITION FOR LITHOGRAPHY AND PATTERN FORMATION METHOD
An object of the present invention is to provide a composition for lithography capable of obtaining a film in contact with a resist layer or an underlayer film capable of forming a pattern excellent in exposure sensitivity the like. The object can be achieved by a composition for lithography containing a compound having at least one element selected from the group consisting of iodine, tellurium, and fluorine, or a resin having a constituent unit derived from the compound, wherein a total mass of the atoms in the compound is 15% by mass or more and 75% by mass or less.