- Access and modulation of substituted 1-methyl-1,6-dihydropyrazolo[3,4-c]pyrazoles
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Despite the pharmacological potential of the pyrazolo[3,4-c]pyrazoles, only a few methods of preparation and direct functionalization of this moiety have been described. We report herein a convenient design of new pyrazolo[3,4-c]pyrazoles with a high therapeutic impact. The effective chosen strategy consists of hydrazine condensations and C-N Ullmann-type cross-coupling reactions with microwave activation. Moreover, chemoselective bromination of the newly formed bipyrazoles followed by Suzuki-Miyaura cross-coupling reactions allowed the synthesis of a variety of modulated heterobicycles.
- Ostache, Nicu-Cosmin,Hiebel, Marie-Aude,F?naru, Adriana-Lumini?a,Allouchi, Hassan,Guillaumet, Gérald,Suzenet, Franck
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- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to macrocyclic α-keto amide derivatives and their use as therapeutic agents.
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Paragraph 0573-0575
(2018/09/25)
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- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 0506; 0936
(2018/04/17)
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- Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate
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Computational modeling was used to direct the synthesis of analogs of previously reported phosphodiesterase 2A (PDE2A) inhibitor 1 with an imidazotriazine core to yield compounds of significantly enhanced potency. The analog PF-05180999 (30) was subsequen
- Helal, Christopher J.,Arnold, Eric,Boyden, Tracey,Chang, Cheng,Chappie, Thomas A.,Fisher, Ethan,Hajos, Mihaly,Harms, John F.,Hoffman, William E.,Humphrey, John M.,Pandit, Jayvardhan,Kang, Zhijun,Kleiman, Robin J.,Kormos, Bethany L.,Lee, Che-Wah,Lu, Jiemin,Maklad, Noha,McDowell, Laura,McGinnis, Dina,O'Connor, Rebecca E.,O'Donnell, Christopher J.,Ogden, Adam,Piotrowski, Mary,Schmidt, Christopher J.,Seymour, Patricia A.,Ueno, Hirokazu,Vansell, Nichole,Verhoest, Patrick R.,Yang, Edward X.
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p. 1001 - 1018
(2018/02/17)
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- PYRANOPYRIDONE INHIBITORS OF TANKYRASE
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There are provided compounds of the formula or a pharmaceutically acceptable salt thereof wherein X, M, Y, R1 and R2 are as defined herein. The compounds have activity as anticancer agents.
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Page/Page column 49
(2014/01/09)
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- Imidazo[5,1-f][1,2,4]Triazines for the Treatment of Neurological Disorders
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The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.
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Page/Page column 23
(2012/09/05)
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- Pyrazoles
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful
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Page/Page column 10
(2010/11/24)
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