- 1-(5-(2-CYANOPYRIDIN-4-YL)OXAZOLE-2-CARBONYL)-4-METHYLHEXAHYDROPYRROLO[3,4-B]PYRROLE-5(1H)-CARBONITRILE AS A USP30 INHIBITOR FOR THE TREATMENT OF MITOCHONDRIAL DYSFUNCTION, CANCER AND FIBROSIS
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The present invention relates to hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carbonitriles with activity as inhibitors of the deubiquitylating enzyme USP30, having utility in a variety of therapeutic areas, including conditions involving mitochondrial dysfunctio
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Page/Page column 41; 44
(2021/12/31)
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- Preparation of 2,7-diazabicyclo[3.3.0]octanes
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2,7-Diazabicyclo[3.3.0]octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula STR1 in which R1, R3, R4, R5, R7 and R8 may be identical or different and in each case denote H, C1 -C5 -alkyl (optionally substituted by halogen, hydroxyl or C1 -C3 -alkoxy), C1 -C3 -alkoxycarbonyl or C6 -C12 -aryl, R4 additionally denotes halogen, R2 and R6 may be identical or different, denote H, C1 -C6 -alkyl, benzyl, C6 -C12 -aryl, C1 -C3 -alkanoyl, benzoyl or C1 -C5 -alkoxycarbonyl, or R2 and R3 together denote a bridge of the structure (CH2)n, n=2-4, CH2 --CHOH--CH2, CH2 --S--CH2 or C(CH3)2 --S--CH2, excluding 2,7-diazabicyclo[3.3.0]octane. Also their preparation by the reaction STR2 Intermediates II are also new.
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