189333-49-1Relevant articles and documents
Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents
Lv, Kai,You, Xuefu,Wang, Bin,Wei, Zengquan,Chai, Yun,Wang, Bo,Wang, Apeng,Huang, Guocheng,Liu, Mingliang,Lu, Yu
, p. 636 - 641 (2017)
A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent in vitro activity (MIC 0.15 μM) against the drug susceptive Mycobacterium tuberculosis H37Rv strain and two clinically isolated multidrug-resistant strains. Compounds 11l and 11m display acceptable safety, greater aqueous solubility, and better pharmacokinetic profiles than PBTZ169, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.
3,9- DIAZASPIRO[5,5] UNDECANE COMPOUND AS FLT3 AND AXL INHIBITORS
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, (2021/08/05)
Disclosed in the present invention is a novel compound as FLT3 and AXL inhibitors. Sepcifically, disclosed are a compound represented by fomula (I) and a pharmacologically acceptable salt thereof.
Preparation method of 3-alkyl-3, 9-diazaspiro [5, 5] undecane
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, (2020/08/29)
The invention relates to a preparation method of 3-alkyl-3, 9-diazaspiro [5, 5] undecane. The preparation method comprises the following steps: a. reacting a compound I with cyanoacetate under the action of ammonia water and a catalyst to obtain a compoun
Polymorphism of novel spiroarylphosphine oxide
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, (2019/11/20)
The invention relates to a polymorphic substance of a compound (2-((5-chloro-2-((2-methoxyl-4-(9-methyl-3,9-diaza-sprio[5.5]hendecane-3-yl)phenyl)amino)pyrimidine-4-yl)amino)phenyl)dimethyl phosphineoxide (compound I). The invention further relates to a m
Preparation method, intermediate and crystal form of spironolamine arylphosphine oxide
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, (2017/08/30)
The invention discloses a preparation method and a crystal form of high-purity spironolamine arylphosphine oxide. The invention further discloses a method for preparing a compound shown as a formula (I) and an intermediate compound.
Spiro aryl phosphorus oxide or sulfide
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, (2016/10/08)
The invention discloses a spiro aryl phosphorus oxide or sulfide as ALK inhibitor, and in particular discloses a compound shown in a formula (I) as an ALK inhibitor or a pharmaceutically acceptable salt thereof.
CEPHEM COMPOUND HAVING CATECHOL GROUP
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, (2013/03/26)
A compound of the formula: wherein X is -N=, -CH=, or the like; W is -CH2- or the like; U is -S- or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3/su
COMPOUNDS AND METHODS FOR PREPARING DIAZASPIRO DERIVATIVES
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Page/Page column 16, (2009/09/05)
Compounds and methods are provided for the synthesis of diazaspiro derivatives of the Formula: wherein R is as described herein. Such compounds are useful, for example, as intermediates in the synthesis of biologically active compounds.
SUBSTITUTED AZASPIRO DERIVATIVES
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Page/Page column 28, (2008/12/08)
Substituted azaspiro derivatives of the Formula:are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
SPIROCYCLIC SULFONAMIDES AND RELATED COMPOUNDS
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, (2010/11/29)
Spirocyclic sulfonamides and related compounds of Formula 1 are provided : (Formula (I)): in which the variables are as described herein. Such compounds may be used to modulate bradykinin receptor activity in vivo or in vitro, and are particularly useful