198835-02-8Relevant articles and documents
Nitrogen-containing heterocyclic amino derivative, preparation method thereof and anti-HIV-1 medicine
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Paragraph 0457-0460; 0469-0471, (2021/08/21)
The invention provides a nitrogen-containing heterocyclic ring amino derivative, a preparation method thereof and an anti-HIV-1 medicine, and belongs to the technical field of medicine application. The nitrogen-containing heterocyclic ring amino derivative provided by the invention can interfere with the process of hydrolyzing Gap and Gap-Pol precursor polyprotein by HIV-1 protease, and has high HIV-1 protease inhibitory activity; meanwhile, the nitrogen-containing heterocyclic ring amino derivative provided by the invention has remarkable inhibitory activity on wild type anti-HIV-1 medicine strains and high anti-DRV-medicine strains, has low cytotoxicity, and has a good application prospect as an anti-AIDS medicine.
FXR RECEPTOR AGONIST
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Paragraph 0258; 0261-0262, (2020/06/02)
The present invention belongs to the technical field of pharmaceuticals, and particularly relates to a compound of formula (I), a pharmaceutically acceptable salt thereof, an ester thereof or a stereoisomer of the compound, the salt or the ester, wherein
Synthesis and biological evaluation of pyrimidine derivatives with diverse azabicyclic ether/amine as novel GPR119 agonist
Yang, Zunhua,Fang, Yuanying,Park, Haeil
, p. 2515 - 2519 (2017/05/10)
A class of novel pyrimidine derivatives bearing diverse conformationally restricted azabicyclic ether/amine were designed, synthesized and evaluated for their GPR119 agonist activities against type 2 diabetes. Most compounds exhibited superior hEC50
SUBSTITUTED 2-AZABICYCLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS
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Paragraph 0177; 0178, (2014/09/30)
The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
Synthesis of novel azanorbornylpurine derivatives
H?ebabecky, Hubert,Dejmek, Milan,Dra?ínsky, Martin,?ála, Michal,Leyssen, Pieter,Neyts, Johan,Kaniaková, Martina,Kr?ek, Jan,Nencka, Radim
, p. 1286 - 1298 (2012/02/15)
Azanorbornylpurine derivatives were prepared by Mitsunobu reaction of appropriate hydroxyazanorbornane derivative with 6-chloropurine or construction of purine base at azanorbornylamines. The prepared target compounds were evaluated for antiviral activity and effect on neuronal and muscle nicotinic acetylcholine receptors.
Improved synthesis of monoprotected 5- and 6-amino-2-azanorbornanes
Dacenko, Oleksandr P.,Manoylenko, Olga V.,Grygorenko, Oleksandr O.,Mykhailiuk, Pavel K.,Volochnyuk, Dmitriy M.,Shishkin, Oleg V.,Tolmachev, Andrey A.
, p. 981 - 992 (2011/04/25)
(Chemical Equation Presented) An improved synthesis of Boc-monoprotected 5- and 6-amino-2-azanorbornanes is reported. The synthetic scheme consists of five steps and allows multigram quantities of the title compounds to be obtained. The regio- and stereochemistries of the products are established by two-dimensional NMR experiments. Copyright Taylor & Francis Group, LLC.
Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes
Xia, Yan,Chackalamannil, Samuel,Greenlee, William J.,Jayne, Charles,Neustadt, Bernard,Stamford, Andrew,Vaccaro, Henry,Xu, Xiaoying,Baker, Hana,O'Neill, Kim,Woods, Morgan,Hawes, Brian,Kowalski, Tim
scheme or table, p. 3290 - 3296 (2011/06/24)
The lead optimization studies of a series of GPR119 agonists incorporating a nortropanol scaffold are described. Extensive structure-activity relationship (SAR) studies of the lead compound 20f led to the identification of compound 36j as a potent, single digit nanomolar GPR119 agonist with high agonist activity. Compound 36j was orally active in lowering blood glucose levels in a mouse oral glucose tolerance test and increased plasma insulin levels in a rat hyperglycemic model. It showed good to excellent pharmacokinetic properties in rats and monkeys and no untoward activities in counter-screen assays. Compound 36j demonstrated an attractive in vitro and in vivo profile for further development.
PIPERAZINO DERIVATIVES AS NEUROKININ ANTAGONISTS
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Page/Page column 38, (2010/11/08)
The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc', l and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
Heterocyclic compounds
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, (2008/06/13)
The present invention provides heterocyclic 2-aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic ptor.
