Patent classifications
C07D498/04
COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE
- Nadiya Sydorenko ,
- Rauful Alam ,
- Suresh Babu ,
- Anuradha Bhattacharyya ,
- Guangming Chen ,
- Matteo Chierchia ,
- Gary Mitchell Karp ,
- Tom Tuan Luong ,
- Anthony R. Mazzotti ,
- Young-Choon Moon ,
- Nicholas Walter Mszar ,
- Jana Narasimhan ,
- Jigar S. Patel ,
- Hongyu Ren ,
- Gang Wang ,
- Matthew G. Woll ,
- Nanjing Zhang ,
- Xiaoyan Zhang
The present description relates to compounds of Formula (I), forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
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Fused Azole Heterocycles as AHR Antagonists
The present disclosure relates to thiazolo-pyridine, oxazolo-pyridine, pyrrolo-pyridine, pyrrolo-pyrazine and pyrrolo-pyrimidine compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling.
Fused Azole Heterocycles as AHR Antagonists
The present disclosure relates to thiazolo-pyridine, oxazolo-pyridine, pyrrolo-pyridine, pyrrolo-pyrazine and pyrrolo-pyrimidine compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling.
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.
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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.
GEM-DISUBSTITUTED HETEROCYCLIC COMPOUNDS AND THEIR USE AS IDH INHIBITORS
The present invention relates to certain gem-disubstituted heterocyclic compounds, which modulate the activity of Isocitrate Dehydrogenase (IDH). The compounds of this invention are therefore useful in treating diseases caused by mutated IDH1 and/or mutated IDH2 enzyme and/or IDH1 wild type (wt) enzyme. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
GEM-DISUBSTITUTED HETEROCYCLIC COMPOUNDS AND THEIR USE AS IDH INHIBITORS
The present invention relates to certain gem-disubstituted heterocyclic compounds, which modulate the activity of Isocitrate Dehydrogenase (IDH). The compounds of this invention are therefore useful in treating diseases caused by mutated IDH1 and/or mutated IDH2 enzyme and/or IDH1 wild type (wt) enzyme. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
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COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
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GPR52 MODULATOR COMPOUNDS
The disclosures herein relate to novel compounds of Formula (1): (1) and salts thereof, wherein R.sup.1, Q, X, Y and Z are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.
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