- SPIROCYCLE COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Provided herein are compounds and compositions useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
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Paragraph 00216
(2019/03/17)
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- Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists
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A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives was synthesized, and their structure-activity relationships were examined in order to identify potent and selective arginine vasopressin V2 receptor agonists. Attempts to substitute other chemical groups in place of the 2-pyridilmethyl moiety of 1a led to the discovery that potent V2 binding affinity could be obtained with a wide range of functional groups. This structural tolerance allowed for the manipulation of other attributes, such as selectivity against V1a receptor affinity or avoidance of the undesirable inhibition of cytochrome P450 (CYP), without losing potent affinity for the V2 receptor. Some representative compounds obtained in this study were also found to decrease urine volume in awake rats.
- Tsukamoto, Issei,Koshio, Hiroyuki,Kuramochi, Takahiro,Saitoh, Chikashi,Yanai-Inamura, Hiroko,Kitada-Nozawa, Chika,Yamamoto, Eisaku,Yatsu, Takeyuki,Shimada, Yoshiaki,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
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experimental part
p. 3130 - 3141
(2009/09/30)
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- 1,2,3-TRIAZOLOAZINES ET AUTRES HETEROCYCLES AZOTES DERIVES D'AZINE-CARBOXALDEHYDES
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α-(N)-azine-carboxaldehydes are convenient precursors of 1,2,3-triazoloazines.Through oxidative cyclisation of the corresponding hydrazones we have prepared the new 1,2,3-triazolopyridazine and 1,2,3-triazolopyrazine.Unlike the other azaindolizines these compounds are degraded by electrophiles. attempts to prepare imidazopyrimidine or derivatives have been carried out either from 4-aminomethylpyrimidine or from ethyl 2-(4-pyrimidinyl)propionate.
- Maury, Georges,Meziane, Driss,Srairi, Driss,Paugan, Jean-Paul,Paugam, Renee
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p. 153 - 162
(2007/10/02)
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