52664-01-4Relevant articles and documents
CRYSTALLINE SUBSTITUTED CYCLOHEXYL PYRAZOLO[1,5-A]PYRIMIDINYL CARBOXAMIDE COMPOUND AND THERAPEUTIC USES THEREOF
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Paragraph 00233; 00236, (2019/07/14)
The invention provides crystalline 5,7-dimethyl-N-((1S*,4S)-4-(pentyloxy)cyclohexyl) pyrazolo[1,5-a]pyrimidine-3-carboxamide, compositions containing the crystalline compound, methods for making the crystalline compound, medical kits, and methods for usin
Design, Synthesis, and Evaluation of the Anticancer Properties of a Novel Series of α-(Benzoylamino)-β-substituted Acrylic Amide Derivatives of Pyrazolo[1,5-a]pyrimidine
Sasikumar,Mohanasrinivasan,Ajeesh Kumar,Krishnaswamy
, p. 214 - 225 (2018/01/26)
A novel series of α-(benzoylamino)-β-substituted acrylic amide derivatives of pyrazolo[1,5-a]pyrimidine has been synthesized using a convergent multistep synthesis. The synthesized compounds were characterized by 1H NMR, 13C NMR, ESI-MS, and IR analyses. Those new compounds were screened for their in vitro antiproliferative activity using an MTT assay analysis. Out of nine derivatives synthesized in the current study, compounds 13g, 13d, 13h, and 13i exhibited the greatest anticancer activities in HeLa and HepG2 cell lines. The in vitro anticancer activity of compound 13g against HeLa, HepG2, and MCF-7 cell lines is superior to the marketed drugs paclitaxel and SAHA.
Design, Synthesis, and Evaluation of the Anticancer Properties of a Novel Series of Imidazolone Fused Pyrazolo[1,5-a]pyrimidine Derivatives
Ajeesh Kumar,Bodke, Yadav D.,Gowda, Ashwath N.,Sambasivam, Ganesh,Bhat, Kishore G.
, p. 1904 - 1924 (2017/05/29)
A novel series of imidazolone fused pyrazolo[1,5-a]pyrimidine derivatives has been designed and synthesized using a convergent approach, and the structures of these compounds were confirmed by 1H NMR, 13C NMR, ESI-MS, and IR analyses. These new compounds were tested for their in vitro antiproliferative activity using an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Out of the 20 derivatives prepared in the current study, compounds 8h, 8n, and 8r exhibited good anticancer activities tested against HeLa cells and HepG2 cells. However, the in vitro anticancer activity of compound 8r against HeLa, HepG2, and MCF-7 cell lines is superior to the marketed drugs Paclitaxel and SAHA.
Design, synthesis, and evaluation of the anticancer properties of a novel series of carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5-a]pyrimidine derivatives
Ajeesh Kumar,Nair, Kanya B.,Bodke, Yadav D.,Sambasivam, Ganesh,Bhat, Kishore G.
, p. 2221 - 2234 (2016/11/17)
Abstract: A series of novel carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5-a]pyrimidine analog were designed and synthesized. The newly synthesized compounds were characterized by 1H NMR, 13C NMR, ESI–MS, and IR and were tested for their in vitro antiproliferative activity by MTT assay. Out of these twenty derivatives, five compounds showed good anticancer activity against HeLa cell line. These are superior with less than 10?μg/cm3 of IC50 when compared to the marketed anticancer drug paclitaxel with 30?μg/cm3 of IC50 against Hela cell line. Graphical abstract: [Figure not available: see fulltext.]
SUBSTITUTED PYRAZOLO(1,5-A)PYRIMIDINES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00219, (2016/06/01)
The invention provides substituted pyrazolo[l,5-a]pyrimidine and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[l,5-a]pyrimidine compounds described herein include 5,7- dimethyl-N-phenylpyrazolo[l,5-a]pyrimidine-3-carboxamide compounds and variants thereof.
SUBSTITUTED PYRAZOLOPYRIMIDINES AS GLUCOCEREBROSIDASE ACTIVATORS
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Page/Page column 17, (2012/06/30)
Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) in which variables R1-R7 and X are described in the application.
Discovery, structure - Activity relationship, and biological evaluation of noninhibitory small molecule chaperones of glucocerebrosidase
Patnaik, Samarjit,Zheng, Wei,Choi, Jae H.,Motabar, Omid,Southall, Noel,Westbroek, Wendy,Lea, Wendy A.,Velayati, Arash,Goldin, Ehud,Sidransky, Ellen,Leister, William,Marugan, Juan J.
experimental part, p. 5734 - 5748 (2012/08/07)
A major challenge in the field of Gaucher disease has been the development of new therapeutic strategies including molecular chaperones. All previously described chaperones of glucocerebrosidase are enzyme inhibitors, which complicates their clinical development because their chaperone activity must be balanced against the functional inhibition of the enzyme. Using a novel high throughput screening methodology, we identified a chemical series that does not inhibit the enzyme but can still facilitate its translocation to the lysosome as measured by immunostaining of glucocerebrosidase in patient fibroblasts. These compounds provide the basis for the development of a novel approach toward small molecule treatment for patients with Gaucher disease. This article not subject to U.S. Copyright. Published 2012 by the American Chemical Society.
PREPARATION AND CHARACTERIZATION OF PYRAZOLOPYRIMIDINES
Maquestiau, A.,Taghret, H.,Eynde, J.-J. vanden
, p. 131 - 136 (2007/10/02)
1-Phenyl-1,3-butadione readily reacts with 3(5)-amino-1H-pyrazoles to yield mixtures of pyrazolopyrimidines which are identified by 1H nmr.Selective preparation of 5-methyl-7-phenylpyrazolopyrimidines can be achieved when 3-amino-1-phenyl-2-
