1016228-01-5Relevant academic research and scientific papers
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype
Temple, Kayla J.,Engers, Julie L.,Long, Madeline F.,Watson, Katherine J.,Chang, Sichen,Luscombe, Vincent B.,Jenkins, Matthew T.,Rodriguez, Alice L.,Niswender, Colleen M.,Bridges, Thomas M.,Conn, P. Jeffrey,Engers, Darren W.,Lindsley, Craig W.
, (2019/12/09)
This Letter details our efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, we investigated a plethora of core replacements. This exercise identified a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide core that provided improved M4 PAM activity and CNS penetration.
BACE1 INHIBITORS
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Page/Page column 65, (2016/06/01)
The present invention provides a compound of formula (I), having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention ar
C2-CARBOCYCLIC IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 57, (2016/01/29)
In its many embodiments, the present invention provides certain C2-carbocyclic iminothiazine dioxide compounds, including compounds Formula (I); or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, n, ring C, RC and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
5-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO-AND DIOXIDES AS BACE INHIBITORS,COMPOSITIONS,AND THEIR USE
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Page/Page column 120, (2012/11/06)
The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said ster
NOVEL 5,7-DISUBSTITUTED [1, 3] THIAZOLO [4, 5] PYRIMIDIN-2 (3H)-AMINE DEIRVATIVES AND THEIR USE IN THERAPY
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Page/Page column 32; 33, (2008/06/13)
There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX?3#191CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
NOVEL 5, 7-DISUBSTITUTED [1, 3 ] THIAZOLO [4, 5-D] PYRIMIDIN-2 (3H)-ONE DEREVATIVES AND THEIR USE IN THERAPY
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Page/Page column 39; 40, (2008/06/13)
There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3#191CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
