Patent classifications
C07D403/12
Amide compounds as kinase inhibitors, compositions and methods of treatment
The present disclosure relates to certain amides and heterocyclic compounds and uses of these amides and heterocyclic compounds to inhibit Rho-associated protein kinases and treat diseases including autoimmune disorders, graft versus host disease (GVHD), inflammation, cardiovascular disorders, central nervous system disorders, and neoplastic disorders.
INDOLINONE COMPOUNDS FOR USE AS MAP4K1 INHIBITORS
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring C, X.sup.1, X.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, m and n are as defined herein, which are useful as MAP4K1 inhibitors, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by MAP4K1.
##STR00001##
INDOLINONE COMPOUNDS FOR USE AS MAP4K1 INHIBITORS
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring C, X.sup.1, X.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, m and n are as defined herein, which are useful as MAP4K1 inhibitors, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by MAP4K1.
##STR00001##
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.
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 SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
##STR00001##
NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
##STR00001##
Biaryl inhibitors of Bruton's tyrosine kinase
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
Biaryl inhibitors of Bruton's tyrosine kinase
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
Substituted pyrazole-pyrimidines, variants thereof, and uses therefore
Disclosed herein are substituted pyrazole-pyrimidine compounds of Formula I and variants thereof for the treatment, for example, of diseases associated with P2X purinergic receptors: ##STR00001##
In one embodiment, the P2X3 and/or P2X2/3 antagonists disclosed herein are potentially useful, for example, for the treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.