14714-18-2Relevant academic research and scientific papers
SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Paragraph 0327; 0328, (2017/04/04)
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.
Development of an alternate synthesis for a key JAK2 inhibitor intermediate via sequential c-h bond functionalization
Campbell, Alison N.,Cole, Kevin P.,Martinelli, Joseph R.,May, Scott A.,Mitchell, David,Pollock, Patrick M.,Sullivan, Kevin A.
supporting information, p. 273 - 281 (2013/04/10)
The development of an alternative synthetic route to a functionalized imidazopyridazine which strategically streamlines the synthesis and avoids a number of problematic reagents is described. Key to the success of this alternative route is the use of two
SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Page/Page column 96, (2013/05/09)
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.
HETEROARYLS AND THEIR USE AS PI3K INHIBITORS
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Page/Page column 324-325, (2010/08/18)
This invention provides compounds of formula (IA) or (IB): wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
IMIDAZOPYRIDAZINES FOR USE AS PROTEIN KINASE INHIBITORS
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Page/Page column 111, (2009/06/27)
There is provided compounds of formula (I): wherein Z, M, R1, X, R3, R4 and R5 have meanings given in the description, an pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protei kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, an particularly in the treatment of cancer.
Condensed pyridazine derivatives, their production and use
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, (2008/06/13)
A condensed pyridazine derivative which is useful as a pharmaceutical composition for preventing or treating allergic skin diseases such as contact dermatitis, pruritus, dried dermatitis, acute urticaria and prurigo.
NASAL DROPS CONTAINING FUSED PYRIDAZINE DERIVATIVES
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, (2008/06/13)
A nose drop containing the compound (I) represented by the formula wherein Ar1 and Ar2 are each an aromatic group, Ar1 and Ar2 optionally form a condensed cyclic group together with the adjacent carbon atom, ring B is a nitrogen-containing heterocycle, X and Y are each a bond, an oxygen atom or S(O)p (p is 0 to 2), NR4 (R4 is H or a lower alkyl group) or a divalent linear lower hydrocarbon group optionally having substituents and containing 1 to 3 heteroatoms, A is N or CR7 (R7 is H, a halogen atom, a hydrocarbon group, an acyl group or a hydroxy group optionally having substituents), R1, R2 and R3 are each H, a halogen atom, a hydrocarbon group, an acyl group or a hydroxy group optionally having substituents, and R8 is H, a hydroxy group optionally substituted by a lower alkyl group or a carboxyl group, provided that the nitrogen-containing heterocycle represented by ring B is not a heterocycle represented by the formula wherein n is 0 - 1, or a salt thereof or a prodrug thereof, exhibits a superior prophylactic or therapeutic effect on allergic rhinitis and the like.
Condensed pyridazine derivatives, their production and use
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, (2008/06/13)
The present invention provides a compound represented by the formula: wherein Ar1 and Ar2 are independently an aromatic group which may be substituted, and Ar1 and Ar2 may form a condensed cyclic group with an adjacent carbon atom; ring B is a nitrogen-containing heterocycle which may be substituted; X and Y are the same or different and are independently a bond, an oxygen atom, S(O)p (p is an integer of 0 ot 2), NR4 wherein R4 is a hydrogen atom or a lower alkyl group, or a bivalent linear lower hydrocarbon group which may contain 1 to 3 hetero atoms and the bivalent linear lower hydrocarbon group may be substituted; A is a nitrogen atom or CR7 wherein R7 is a hydrogen atom, a halogen atom, a hydrocarbon which may be substituted, an acyl group or a hydroxy group which may be substituted; R1, R2 and R3 are the same or different and are independently a hydrogen atom, a halogen atom, a hydrocarbon group which may be substituted, an acyl group or a hydroxy group which may be substituted; R8 is a hydrogen atom, a hydroxy group which may be substituted by a lower alkyl or a carboxyl group, or a salt thereof, which exhibits excellent anti-histaminic or eosinophil chemotaxis-inhibiting activities and is useful in treatment or prevention of asthma, allergic conjunctivitis, allergic rhinitis, chronic urticaria or atopic dermatitis.
Research on heterocyclic compounds. XXX. Synthesis and pharmacological activity of 2-methylimidazo[1,2-b]pyridazine-3-carboxylic acids
Abignente,Arena,Luraschi,Saturnino,Rossi,Berrino,Cenicola
, p. 931 - 944 (2007/10/02)
A group of ethyl 2-methylimidazo[1,2-b]pyridazine-3-carboxylates were prepared by reaction in anhydrous ethanol of some substituted 3-aminopyridazines with ethyl 2-chloroacetoacetate. The corresponding carboxylic acids were obtained via alkaline or acid hydrolysis and then tested both in vivo to evaluate their antiinflammatory, analgesic and ulcerogenic actions and in vitro for their ability to inhibit the prostaglandin biosynthesis. The pharmacological results are discussed in terms of both structure-activity relationships and mechanism of action.
