138007-25-7Relevant articles and documents
MULTIFUNCTIONAL RADICAL QUENCHERS
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, (2014/05/07)
The invention provides a compound of formula (I): [insert formula (I)] wherein X, Y, and R1-R4 have any of the values defined in the specification, and salts thereof, as well as compositions comprising the compounds or salts. The compounds are useful for treating diseases associated with impaired mitochondrial function in an animal.
Synthesis of 1-benzothiepine and 1-benzazepine derivatives as orally active CCR5 antagonists
Aramaki, Yoshio,Seto, Masaki,Okawa, Tomohiro,Oda, Tsuneo,Kanzaki, Naoyuki,Shiraishi, Mitsuru
, p. 254 - 258 (2007/10/03)
Quaternary ammonium benzocycloheptene compound 1 has previously been reported as a clinical candidate for an injectable CCR5 antagonist. In order to develop an orally active CCR5 antagonist, derivatives of tertiary amine benzocycloheptene 2, the chemical precursor to 1, were investigated. The benzocycloheptene ring was converted to benzothiepine and benzazepine rings and it was found that these changes could enhance the potency of tertiary amine derivatives. In particular, the 1-benzothiepine-1,1-dioxide 11b and the N-methyl-1-benzazepine 18 showed increased activity and good preliminary pharmacokinetic properties. The synthesis of 1-benzothiepine and 1-benzazepine derivatives and their activity are described.