Patent classifications
C07D513/22
SYNTHESIS OF AMANIN AND ITS DERIVATIVES
The present invention relates to the chemical synthesis of amanin and its derivatives. The present invention also relates to intermediate products of the amanin synthesis.
Macrocyclic compounds as TRK kinases inhibitors
Provided are certain TRK inhibitors, pharmaceutical compositions thereof, and methods of use thereof.
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.
CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE
- Robert Yongxin Zhao ,
- Yuanyuan Huang ,
- Qingliang Yang ,
- Shun Gai ,
- Hangbo Ye ,
- Linyao Zhao ,
- Chengyu Yang ,
- Yifang Xu ,
- Huihui Guo ,
- Minjun CHAO ,
- Qianqian Tong ,
- Wenjun Li ,
- Xiang CAI ,
- Xiaomai Zhou ,
- Hongsheng Xie ,
- Junxiang Jia ,
- Haifeng ZHU ,
- Zhixiang GUO ,
- Shuihong GAO ,
- Chunyan WANG ,
- Chen Lin ,
- Yanlei YANG ,
- Zhicang YE ,
- Jie PENG ,
- Jun XU ,
- Xiaotao Zuo ,
- Qingyu SU
A conjugation of a cytotoxic drug to a cell-binding molecule with a bis-linker (dual-linker) as shown in Formula (I). Bis-linkage methods of making a conjugate of a cytotoxic drug/molecule to a cell-binding agent in a specific manner are also described, as well as application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.
##STR00001##
wherein “” is an optional bond; X, Y, Z.sub.1, and Z.sub.2 are a functional group; m.sub.1 and n are a integer; L.sub.1 and L.sub.2 are a linker.
CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE
- Robert Yongxin Zhao ,
- Yuanyuan Huang ,
- Qingliang Yang ,
- Shun Gai ,
- Hangbo Ye ,
- Linyao Zhao ,
- Chengyu Yang ,
- Yifang Xu ,
- Huihui Guo ,
- Minjun CHAO ,
- Qianqian Tong ,
- Wenjun Li ,
- Xiang CAI ,
- Xiaomai Zhou ,
- Hongsheng Xie ,
- Junxiang Jia ,
- Haifeng ZHU ,
- Zhixiang GUO ,
- Shuihong GAO ,
- Chunyan WANG ,
- Chen Lin ,
- Yanlei YANG ,
- Zhicang YE ,
- Jie PENG ,
- Jun XU ,
- Xiaotao Zuo ,
- Qingyu SU
A conjugation of a cytotoxic drug to a cell-binding molecule with a bis-linker (dual-linker) as shown in Formula (I). Bis-linkage methods of making a conjugate of a cytotoxic drug/molecule to a cell-binding agent in a specific manner are also described, as well as application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.
##STR00001##
wherein “” is an optional bond; X, Y, Z.sub.1, and Z.sub.2 are a functional group; m.sub.1 and n are a integer; L.sub.1 and L.sub.2 are a linker.
TERNARY PHOTOACTIVE LAYER COMPOSITION AND ORGANIC SOLAR CELL COMPRISING SAME
The present disclosure relates to a ternary photoactive layer composition and an organic solar cell including the same. According to the present disclosure, excessive crystal growth and aggregation can be prevented during large-area coating of a photoactive layer, uniform morphology can be achieved without significant phase separation, an organic solar cell with superior photovoltaic cell characteristics can be realized, and superior performance may be maintained even after long-term exposure to heat by preventing the morphological change of the photoactive layer.
TERNARY PHOTOACTIVE LAYER COMPOSITION AND ORGANIC SOLAR CELL COMPRISING SAME
The present disclosure relates to a ternary photoactive layer composition and an organic solar cell including the same. According to the present disclosure, excessive crystal growth and aggregation can be prevented during large-area coating of a photoactive layer, uniform morphology can be achieved without significant phase separation, an organic solar cell with superior photovoltaic cell characteristics can be realized, and superior performance may be maintained even after long-term exposure to heat by preventing the morphological change of the photoactive layer.
COMPOUNDS, CONJUGATES, AND COMPOSITIONS OF EPIPOLYTHIODIKETOPIPERAZINES AND POLYTHIODIKETOPIPERAZINES AND USES THEREOF
The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
Ras inhibitors
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
Heteroaromatic macrocyclic ether chemotherapeutic agents
Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of Formula (I): ##STR00001##
pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The disclosure further relates to methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof.