- Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment
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A series of octahydropyrrolo[3,4-c]pyrroles were synthesized and evaluated by orexin 1 and 2 receptor (OX1 & 2R) antagonists assays. Compound 14l with potent OXR antagonist activity and suitable pharmacokinetic behavior was chosen to be investigated in an EEG study, which demonstrated effects of sleep promotion comparable to Suvorexant. Furthermore, the di-fluro substituted analogs exhibited reduced hERG inhibition while maintaining moderate potency.
- Wu, Songliang,Sun, Yu,Hu, Yi,Zhang, Hongmei,Hou, Lijuan,Liu, Xing,Li, Yufeng,He, Haiying,Luo, Zhi,Chen, Yuan,Wang, Yuhe,Shi, Weihua,Shen, Liang,Cao, Changqing,Liang, Wei,Xu, Qing,Lv, Qiang,Lan, Jiong,Li, Jian,Chen, Shuhui
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supporting information
p. 1458 - 1462
(2017/03/08)
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- AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
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The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Paragraph 0485-0486
(2014/08/19)
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- AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
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The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter-and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Paragraph 00313
(2013/06/05)
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- LACTAM ACETAMIDES AS CALCIUM CHANNEL BLOCKERS
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The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
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Page/Page column 19
(2011/10/10)
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- FURO[3,2-D]PYRIMIDINE DERIVATIVES
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Furo[3,2-d]pyrimidine derivatives of formula I, wherein the meanings for the various substituents are as defined in the description. These compounds are useful as H4 receptor antagonists.
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Page/Page column 56
(2009/06/27)
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- 2 -AMINO-PYRIMIDINE DERIVATIVES AS HISTAMINE H4 ANTAGONISTS
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2-Aminopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 55-56
(2009/07/03)
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- QUINOLONECARBOXYLIC ACID COMPOUNDS, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
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This invention discloses novel quinolonecarboxylic acid derivatives, pharmaceutically acceptable salts or hydrates thereof, and their preparation methods and medical uses. The compounds in this invention show potent antibacterial activity against broad-sp
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Page/Page column 10
(2010/11/26)
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- Bicyclic amine derivatives
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A compound represented by formula (I) or a salt thereof: STR1 wherein X1 and X2 each represent a halogen atom; R1 represents a hydrogen atom or a substituent; R2 represents a substituted or unsubstituted bicyclic heterocyclic substituent of the following formula; STR2 wherein R3, R4, Y, Z, m, n, p, q and r are as defined herein; A represents a nitrogen atom or a substituted carbon atom; and R represents a hydrogen atom or a substituent. The compound exhibits potent antimicrobial activity and also high safety due to reduced lipophilicity.
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