309962-75-2Relevant academic research and scientific papers
QUINAZOLINE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
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, (2022/01/12)
Provided herein are novel compounds, for example, compounds having a Formula (I), Formula (II), or Formula (III), or a pharmaceutically acceptable salt thereof. Also provided herein are methods of preparing the compounds and methods of using the compounds, for example, in inhibiting KRAS G12D in a cancer cell, and/or in treating various cancer such as pancreatic cancer, colorectal cancer, lung cancer or endometrial cancer.
KRAS G12C INHIBITORS
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Paragraph 0435, (2020/07/25)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Second basic pKa: An overlooked parameter in predicting phospholipidosis-inducing potential of diamines
Sakai, Hiroki,Inoue, Hidekazu,Murata, Kenji,Toba, Tetsuya,Takemoto, Naohiro,Matsumoto, Takahiro,Kawabata, Takeo
, (2020/02/13)
In this paper, we present the phospholipidosis-inducing potential (PLIP) of forty fragment-sized diamines derived from N-benzyl-4-(methylamino)piperidine and discuss the relationship between their PLIP and the physicochemical properties. Our results demonstrate that the previously reported methods are not suitable for predicting the PLIP of fragment-sized diamines; the second basic pKa can distinguish PLIP-positive diamines from PLIP-negative diamines more accurately than ClogP or most basic pKa. To the best of our knowledge, this is the first report describing the relationship between PLIP and second basic pKa.
Substituted diazabicycloalkane derivatives
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Page/Page column 36, (2010/02/11)
Compounds of formula (I) [in-line-formulae]Z-Ar1—Ar2??(I) [/in-line-formulae] wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
Heterocyclic substituted aminoazacycles useful as central nervous system agents
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Page 51, (2010/02/07)
Heterocyclic substituted aminoazacyclic compounds of the formula (I):Z-R3, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
Diazabicyclic central nervous system active agents
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, (2008/06/13)
Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
