Patent classifications
C07D519/00
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.
NOVEL IMIDAZOPYRAZINE DERIVATIVES
Provided are novel imidazopyrazine derivatives having the general formula (I), wherein R.sup.1 to R.sup.11 are as described herein
##STR00001##
and pharmaceutically acceptable salts thereof.
Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases.
NOVEL IMIDAZOPYRAZINE DERIVATIVES
Provided are novel imidazopyrazine derivatives having the general formula (I), wherein R.sup.1 to R.sup.11 are as described herein
##STR00001##
and pharmaceutically acceptable salts thereof.
Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases.
NITROGEN-CONTAINING COMPOUND, ELECTRONIC COMPONENT AND ELECTRONIC DEVICE INCLUDING SAME
The present disclosure provides a nitrogen-containing compound, and an electronic component and an electronic device including the same, and belongs to the technical field of organic electroluminescence. The nitrogen-containing compound provided by the present disclosure has polycyclic conjugation properties, the compound has a core structure of fused indolocarbazole. The bond energy between the atoms is high, thus the compound has a good thermal stability, and facilitates solid state accumulation between the molecules. The electroluminescence device with the compound as a luminescent layer material has a long service life. According to the nitrogen-containing compound provided by the present disclosure with an indolocarbazole structure connecting with a nitrogen-containing group (triazine, pyridine and pyrimidine) and a benzoxazole or benzothiazole group respectively has a high dipole moment, thereby improving the polarity of the material. Using the nitrogen-containing compound of the present disclosure as the luminescent layer material of the organic electroluminescence device, the electron transport performance of the device can be improved, and the luminous efficiency and service life of the device can be improved.
NITROGEN-CONTAINING COMPOUND, ELECTRONIC COMPONENT AND ELECTRONIC DEVICE INCLUDING SAME
The present disclosure provides a nitrogen-containing compound, and an electronic component and an electronic device including the same, and belongs to the technical field of organic electroluminescence. The nitrogen-containing compound provided by the present disclosure has polycyclic conjugation properties, the compound has a core structure of fused indolocarbazole. The bond energy between the atoms is high, thus the compound has a good thermal stability, and facilitates solid state accumulation between the molecules. The electroluminescence device with the compound as a luminescent layer material has a long service life. According to the nitrogen-containing compound provided by the present disclosure with an indolocarbazole structure connecting with a nitrogen-containing group (triazine, pyridine and pyrimidine) and a benzoxazole or benzothiazole group respectively has a high dipole moment, thereby improving the polarity of the material. Using the nitrogen-containing compound of the present disclosure as the luminescent layer material of the organic electroluminescence device, the electron transport performance of the device can be improved, and the luminous efficiency and service life of the device can be improved.
HPK1 antagonists and uses thereof
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
HPK1 antagonists and uses thereof
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
METHODS AND COMPOSITIONS FOR MODULATING SPLICING
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
METHODS AND COMPOSITIONS FOR MODULATING SPLICING
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
KRas G12C inhibitors
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.