Importance

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Abstract

Benzodiazepine derivatives of formula (Ie) wherein one R¹ and R² is a benzodiazepinyl-containing group of formula (II) in which R⁸ is H or halo; the other of R¹ and R² is a group Z selected from H, C₃-C₆ cycloalkyl, halo, —NHR⁹, benzyl, phenyl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, wherein phenyl, heterocyclyl and heteroaryl are unsubstituted or substituted by one or two substituents selected from 4- to 10-membered heterocyclyl which is unsubstituted or substituted by OR, and from C₁-C₆ alkyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₃-C₆ cycloalkyl, halo, —OR, —(CH₂)_mOR, —NR₂, —(CH₂)_mNR₂, —NHR″, —SO_mNR₂, —SO_mR, —SR, nitro, —CO₂R, —CN, —CONR₂, —NHCOR, —CH₂NR¹⁰R¹¹ and —NR¹⁰R¹¹, in which each R is independently H or C₁-C₆ alkyl, R″ is C₃-C₆ cycloalkyl and m is 1 or 2; R⁹ is selected from phenyl and 4- to 10-membered heteroaryl wherein phenyl and heteroaryl are unsubstituted or substituted by halo; R¹⁰ and R¹¹ are each independently H or C₁-C₆ alkyl; or R¹⁰ and R¹¹ form, together with the N atom to which they are attached, either (a) a morpholine ring which is optionally bridged by a —CH₂— group linking two ring carbon atoms that are positioned para to each other, or (b) a spiro group of the following formula (b): and ring A is a ring of one of the following structural formulae (I-1), (I-2) and (I-3): and ring A is a ring of one of the following structural formulae (I-1), (I-2) and (I-3): in which Y is selected from O, S, SO₂ and NR, wherein R is as defined above, and each of R² to R⁷ is independently H, C₁-C₆ alkyl, C₁-C₆ hydroxyalkyl, C₃-C₆ cycloalkyl, halo, —OR, —CH₂OR, —NR₂, —CH₂NR¹²R¹³, —NRCOOR, —CH₂OR, —SO_mNR₂, —SO_mR, —CH₂SO_mR, nitro, —CO₂R, —CN, —CONR₂ or —NHCOR, in which R and m are as defined above and R¹² and R¹³ are each independently H, C₁-C₆ alkyl, benzyl, 4- to 10-membered heterocyclyl or R² and R¹³ form, together with the N atom to which they are attached, a 4- to 10-membered heteroaryl which is unsubstituted or a 4- to 10-membered heterocyclyl which is unsubstituted or substituted with C₁-C₆ alkyl or halo, or any two of R² to R⁷ that bond to the same carbon atom form a spiro ring selected from a C₃-C₆ cycloalkyl spiro ring and a spiro oxetane ring of the following structure: (Formula A) and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

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First Claim