- FUSED BICYCLIC COMPOUNDS USEFUL AS UBIQUITIN-SPECIFIC PEPTIDASE 30 INHIBITORS
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The present disclosure relates to compounds of formula (Ι') and pharmaceutically acceptable salts thereof useful as inhibitors of Ubiquitin Specific Peptidase 30 (USP30), pharmaceutical compositions thereof, and methods of use thereof. Compounds as disclo
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Paragraph 0185
(2019/12/04)
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- IMIDAZOPYRIDINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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A series of imidazo[l,2-a]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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- Carbamoyl tetrahydropyridine derivatives
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Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1and R2are identical or different, and each represents a hydrogen atom, a C1-C5alkyl group, or the like; Y1-Y2represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6are identical or different, and each represents a hydrogen atom or an alkyl group; R7represents a hydrogen atom, a C1-C5alkyl group, or the like; and R8represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
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- CARBAMOYL TETRAHYDROPYRIDINE DERIVATIVES
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Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y
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- Synthesis of the sialidase inhibitor siastatin B.
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[structure] The resolved piperidinecarboxylate (R)-7 was converted to siastatin B (1) by an efficient and stereoselective sequence that includes a bromo-beta-lactonization and an N-acyliminium azidation. Two analogues (3 and 4) of siastatin were also prepared.
- Knapp,Zhao
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p. 4037 - 4040
(2007/10/03)
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