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filingDate 2019-03-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2020-11-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-115015-A1
titleOfInvention DERIVATIVES OF AZAESPIRO PIPERAZINE
abstract The present provides, in part, compounds of formula (1), or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: X¹, X², R¹, R², m and n are as described herein; processes for the preparation of; intermediaries used in the preparation of; and compositions containing said compounds, N-oxides or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, for example, Alzheimer's disease, Parkinson's disease, schizophrenia (for example, their cognitive symptoms and negative), pain, addiction and a sleep disorder. Claim 1: A compound of formula (1), or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: X¹ and X² are each independently CH or nitrogen, as long as X¹ and X² are not both CH; R¹ is selected from the group consisting of halogen, cyano, hydroxy, -SF₅, nitro, -N (R⁶) (R⁷), C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ alkylthio, C₁₋ ₆ alkoxy, C₃₋₆ cycloalkyl, -O-heterocycloalkyl (4 to 6 members), C₆₋₁₀ aryl, heteroaryl (5 to 10 members) and heterocycloalkyl (4 to 8 members), wherein said C₁₋₆ alkyl, C₂₋ ₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ alkylthio, C₁₋₆ alkoxy, C₃₋₆ cycloalkyl, -O-heterocycloalkyl (4 to 6 members), C₆₋₁₀ aryl, heteroaryl (5 to 10 members), and heterocycloalkyl (4 to 8 members) are optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, cyano, hydroxy, -N (R⁶) (R⁷), C₁₋₆ alkyl, C₁₋₆ alkoxy, C₃₋₆ cycloalkyl, and heteroaryl (5 to 6 membered), wherein said C₁₋₆ alkyl, C₁₋₆ alkoxy, and heteroaryl (5 to 6 membered) are optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, cyano, hydroxy, C₁₋ ₆ alkyl and C₁₋₆ alkoxy; R² is selected from the group consisting of hydrogen, halogen, cyano, hydroxy, -SF₅, nitro, -N (R⁶) (R⁷), C₁₋₆ alkyl, and C₁₋₆ alkoxy, wherein said C₁₋₆ alkyl and C₁ ₋₆ alkoxy are optionally substituted with 1 to 3 halogens; R⁶ and R⁷ are each independently selected from hydrogen, C₁₋₆ alkyl, or C (O) -CH₃; m is 1 or 2; and n is 1 or 2.
priorityDate 2018-03-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 44.