- 6-MEMBERED HETEROARYLAMINOSULFONAMIDES FOR TREATING DISEASES AND CONDITIONS MEDIATED BY DEFICIENT CFTR ACTIVITY
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The invention relates to heteroaryl compounds, pharmaceutically acceptable salts thereof, and pharmaceutical preparations thereof. Also described herein are compositions and the use of such compounds in methods of treating diseases and conditions mediated by deficient CFTR activity, in particular cystic fibrosis.
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Page/Page column 79-80
(2021/05/21)
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- Discovery of 5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine as a WSB1 Degrader to Inhibit Cancer Cell Metastasis
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The gain of cell motility is an essential prerequisite for cancer metastasis. The ubiquitin ligase subunit WD repeat and SOCS box-containing 1 (WSB1) has been demonstrated to regulate hypoxia-driven tumor cell migration. However, there is still a lack of methods for discovering inhibitors targeting the WSB1 axis. Here, we employed phenotypic screening models and identified compound4that displayed migration inhibitory activity against WSB1-overexpressing cells. Further studies indicated that it may function as a WSB1 degrader, thus leading to the accumulation of the Rho guanosine diphosphate dissociation inhibitor 2 (RhoGDI2) protein, reversing the expression of downstream F-actin and formation of membrane ruffles, and disturbing the migration capacity of cancer cells. Moreover, compound4exhibited a promisingin vivoanticancer metastatic effects. Our findings show the discovery of a new WSB1 degrader, providing a unique solution for the treatment of cancer metastasis.
- Che, Jinxin,Jin, Zegao,Yan, Fangjie,You, Jieqiong,Xie, Jiangfeng,Chen, Binhui,Cheng, Gang,Zhu, Hong,He, Qiaojun,Hu, Yongzhou,Yang, Bo,Cao, Ji,Dong, Xiaowu
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p. 8621 - 8643
(2021/06/28)
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- HPK1 ANTAGONISTS AND USES THEREOF
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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.
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Paragraph 0862; 0863
(2021/03/19)
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- Directing Group Enables Electrochemical Selectively Meta-Bromination of Pyridines under Mild Conditions
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Without the use of catalysts and oxidants, a facile and sustainable electrochemical bromination protocol was developed. By introducing the directing groups, the regioselectivity of pyridine derivatives could be controlled at themeta-position utilizing the inexpensive and safe bromine salts at room temperature. A variety of brominated pyridine derivatives were obtained in 28-95% yields, and the reaction could be readily performed at a gram scale. By combining the installation and removing the directing group, the concept ofmeta-bromination of pyridines could be verified.
- Wu, Yanwei,Xu, Shanghui,Wang, Hong,Shao, Dongxu,Qi, Qiqi,Lu, Yi,Ma, Li,Zhou, Jianhua,Hu, Wei,Gao, Wei,Chen, Jianbin
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p. 16144 - 16150
(2021/07/19)
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- PYRIMIDINE TBK/IKKε INHIBITOR COMPOUNDS AND USES THEREOF
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The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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Paragraph 00187; 00224; 00225
(2019/05/10)
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- IAP inhibitor and its preparation and use (by machine translation)
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The invention of formula (I) compound and its pharmaceutically acceptable salt. Such compounds can be used for inhibiting IAP, thus can be used for the treatment of the IAP-mediated diseases, such as cancer, autoimmune diseases, and viral diseases. The invention also relates to pharmaceutical compositions of such compounds, the method of preparing such compounds and the compound or pharmaceutical composition in preparation for the treatment of cancer by the IAP-mediated, autoimmune diseases, and viral diseases in the application. (by machine translation)
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Paragraph 0101-0103
(2018/03/24)
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- FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF
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The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.
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Paragraph 0982
(2017/05/14)
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- FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF
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The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.
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Paragraph 0710
(2015/08/03)
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- Synthesis and solid-state fluorescence properties of pentacyclic 7-substituted-indeno[1′,2′:4,5]pyrido[2,1-a]isoindol-5-ones
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With the aim to design fluorescent solids, a series of indeno[1′,2′:4,5]pyrido[2,1-a]isoindol-5-ones with various substituents was prepared. In these π-extended pentacyclic derivatives, the presence of a methyl group in the 7-position was found to have a critical influence on the fluorescence properties in the solid state. Crystal packing of the non-substituted derivatives shows strong π-π interactions causing quenching of the fluorescence. In contrast, by introducing a methyl substituent in the 7-position we obtained compounds with fluorescence quantum yield up to 32% in the solid state.
- Chamas,Marchi,Presson,Aubert,Fort,Ceroni,Mamane
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p. 2715 - 2723
(2015/02/05)
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- TRISUBSTITUTED HETEROCYCLIC DERIVATIVES AS ROR GAMMA MODULATORS
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The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 71; 72
(2014/09/03)
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- Compounds and Their Use for Treatment of Amyloid Beta-Related Diseases
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The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of Aβ-related diseases.
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Page/Page column 15
(2012/05/21)
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- Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A2B adenosine receptor antagonists
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The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A2B adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat.
- Eastwood, Paul,Gonzalez, Jacob,Paredes, Sergio,Nueda, Arsenio,Domenech, Teresa,Alberti, Joan,Vidal, Bernat
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scheme or table
p. 1697 - 1700
(2010/08/06)
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- CONDENSED PYRIDINE DERIVATIVES USEFUL AS A28 ADENOSINE RECEPTOR ANTGONISTS
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The present invention relates to new antagonists of the A2B adenosine receptor represented by formula (I). Those compounds are useful for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor such as asthma, bronchoconstriction, allergic diseases, hypertension, atherosclerosis, reperfusion injury, myocardial ischemia, retinopathy, inflammation, gastrointestinal tract disorders, cell proliferation disorders, diabetes mellitus, and/or autoimmune diseases.
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Page/Page column 21
(2008/06/13)
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