- ATG7 INHIBITORS AND THE USES THEREOF
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Disclosed are chemical entities which are compounds of formula (I) : or a pharmaceutically acceptable salt thereof, wherein R1, R2, and Ra have the values described herein. Chemical entities according to the disclosure can be useful as inhibitors of ATG7. Further provided are pharmaceutical compositions comprising a chemical entity of the disclosure and methods of using the compositions in the treatment of cancer.
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Paragraph 00395
(2018/05/27)
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- FLUOROINDOLE DERIVATIVES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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The present invention relates to compound of formula (I), or stereoisomers and pharmaceutically acceptable salts as muscarinic M1 receptor positive allosteric modulators. This invention also relates to methods of making such compounds and pharmaceutical compositions comprising such compounds. The compounds of this invention are useful in the treatment of various disorders that are related to muscarinic M1 receptor.(Formula I) (I)
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Page/Page column 23
(2017/03/28)
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- PYRIMIDONE COMPOUNDS USED AS LP-PLA2 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, Rs
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Paragraph 0132; 0133
(2017/11/18)
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- ISOINDOLINONE AND PYRROLOPYRIDINONE DERIVATIVES AS AKT INHIBITORS
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The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the act
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Paragraph 0174
(2013/04/24)
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- COMPOUNDS
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Disclosed are compounds that inhibit Lp-PLA2 activity, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
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Page/Page column 37
(2012/06/30)
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- 13C NMR spectra of 4-hydroxymethylpyrazoles and their chemical behavior at heating
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It was established that in the13C NMR spectra of 4-hydroxymethylpyrazoles the carbon atom of hydroxymethyl group of 1,3,5-trimethyl-4-hydroxymethylpyrazole is deshielded by 6.28-6.78 ppm compared to 1-methyl-4-hydroxymethyl-, 1,3-dimethyl-4-hydroxymethyl-and 1,5-dimethyl-4-hydroxymethylpyrazoles. It is assumed that this difference is related to their dissimilar behavior at heating. Pleiades Publishing, Ltd., 2010.
- Baltayan,Rstakyan,Antanosyan,Tadevosyan,Attaryan,Asratyan
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experimental part
p. 1001 - 1003
(2011/01/05)
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- SYNTHESIS OF SUBSTITUTED-3-AMINOPYRAZOLES
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The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1'H-4,4'-bispyrazole.
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Page/Page column 30
(2009/01/24)
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- 7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors
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7-Aminopyrazolo[1,5-a]pyrimidine urea receptor tyrosine kinase inhibitors have been discovered. Investigation of structure-activity relationships of the pyrazolo[1,5-a]pyrimidine nucleus led to a series of 6-(4-N,N′-diphenyl) ureas that potently inhibited
- Frey, Robin R.,Curtin, Michael L.,Albert, Daniel H.,Glaser, Keith B.,Pease, Lori J.,Soni, Niru B.,Bouska, Jennifer J.,Reuter, David,Stewart, Kent D.,Marcotte, Patrick,Bukofzer, Gail,Li, Junling,Davidsen, Steven K.,Michaelides, Michael R.
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experimental part
p. 3777 - 3787
(2009/04/07)
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- Amino-Containing Compounds Which Inhibit Memapsin 2 Beta-Secretase Activity and Methods of Use Thereof
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The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.
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Page/Page column 20
(2008/12/05)
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- A2B ADENOSINE RECEPTOR ANTAGONISTS
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Disclosed are novel compounds that are A2B adenosine receptor antagonists having the following structure (I) wherein R1 and R2 are independently chosen from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl, and R4 is an optionally substituted heteroaryl moiety. The compounds of the invention are useful for treating various disease states, including asthma, chronic obstructive pulmonary disorder, pulmonary inflammation, emphysema, diabetic disorders, inflammatory gastrointestinal tract disorders, immunological/inflammatory disorders, cardiovascular diseases, neurological disorders, and diseases related to angiogenesis.
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Page/Page column 42
(2008/06/13)
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