- Selective Functionalization of Aminoheterocycles by a Pyrylium Salt
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The functionalization of aminoheterocycles by using a pyrylium tetrafluoroborate reagent (Pyry-BF4) is presented. This reagent efficiently condenses with a great variety of heterocyclic amines and primes the C?N bond for nucleophilic aromatic substitution. More than 60 examples for the formation of C?O, C?N, C?S, or C?SO2R bonds are disclosed herein. In contrast to C?N activation through diazotization and polyalkylation, this method is characterized by its mild conditions and impressive functional-group tolerance. In addition to small-molecule derivatization, Pyry-BF4 allows the introduction of functional groups in a late-stage fashion to furnish highly functionalized structures.
- Moser, Daniel,Duan, Yaya,Wang, Feng,Ma, Yuanhong,O'Neill, Matthew J.,Cornella, Josep
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supporting information
p. 11035 - 11039
(2018/07/31)
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- SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Paragraph 0833; 0834
(2017/04/04)
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- QUINOLINES AND RELATED ANALOGS AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Paragraph 0369; 0370
(2016/08/17)
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- 5-SUBSTITUTED INDAZOLE-3-CARBOXAMIDES AND PREPARATION AND USE THEREOF
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Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, fibrotic disorders, cartilage (chondral) defects, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, and neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
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Paragraph 1279; 1281; 1282; 1290
(2015/11/09)
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- NOVEL AMINOMETHYL-PHENOL DERIVATIVES AS ANTIMALARIAL AGENTS
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The invention relates to novel aminomethyl-phenol derivatives of formula I wherein R1 to R4, X, A and B are as defined for formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention
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Page/Page column 68-69
(2014/05/24)
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- SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Provided herein are novel substituted bicyclic aza-heterocycle sirtuin- modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.
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Page/Page column 205
(2013/05/09)
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- 8-SUBSTITUTED QUINOLINES AND RELATED ANALOGS AS SIRTUIN MODULATORS
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Provided herein are 8-substituted quinolines and related analogues as sirtuin-modulating compounds of Structural Formula (I) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 137
(2010/09/18)
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- 2-AMINOQUINAZOLINE DERIVATIVES
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2-Aminoquinazoline derivatives represented by the general formula (I) or pharmacologically acceptable salts thereof: (I) wherein R1 and R2 are each independently hydrogen, substituted or unsubstituted lower alkyl, or the like; X is a bond or CR7aR7b (wherein R7a and R7b are each independently hydrogen or the like); when X is a bond, R3 is substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group, while when X is CR7aR7b, R3 is substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, or the like; R4 is hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or the like; and R5 is hydrogen, substituted or unsubstituted aryl, or the like.
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Page/Page column 102
(2008/06/13)
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