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Tricyclic pyrazole derivatives, as cannabinoid receptor antagonists
专利权人:
NEUROSCIENZE PHARMANESS S.C. A R.L.
发明人:
LAZZARI, PAOLO,RUIU, STEFANIA,PINNA, GERARD AIME,MURINEDDU, GABRIELE
申请号:
ES05010832
公开号:
ES2378379T3
申请日:
2005.05.19
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A tricyclic pyrazole derivative of formula (I) that has an affinity for cannabinoidergic CB1 and / or CB2 receptors: ** Formula ** in which: - A is - (CH2) t-, in which t is equal to 1 , 2 or 3; - B is thiophene, optionally substituted with a number of substituents from 1 to 4, and said substituents are the same or different from each other, and are selected from the following: halogen, C1-C7 alkyl, or phenyl; - R is a group selected from the following: - linear or branched C1-C10 alkyl, in which the end of the main chain that is not attached to the nitrogen atom has a CH2-W termination, and W is a halogen, - aryl or arylalkyl, unsubstituted or having one to five substituents, the same or different from each other, selected from halogen or C1-C7 alkyl; - R 'is an amide substituent of the formula -C (O) -NH-T', and T 'is selected from: - C1-C8 alkyl; - C1-C7 haloalkyl; - aryl, arylalkyl or arylalkyl, optionally containing a heteroatom selected from S, N, or O, unsubstituted or optionally having one to four substituents, the same or different from each other, and said substituents are selected from halogen, C1- alkyl C7, C1-C7 haloalkyl, C1-C7 haloalkoxy, C1-C7 alkylthio, or C1-C7 alkoxy; - a C3-C15 cycloalkyl unsubstituted or substituted with one or more C1-C7 alkyl chains, and said chains are one to four for the C5-C15 cycloalkyl, and are one to three for the C4 cycloalkyl, and are one two for the C3 cycloalkyl, and said alkyl groups are the same or different from each other; - a group having the formula: in which R3 and R4, the same or different from each other, represent hydrogen or C1-C3 alkyl, with the proviso that R3 and R4 are not both hydrogen; - a group having the formula: in which R5 represents a C1-C3 alkyl and k is an integer between 1 and 3; or - an NR1R2 group, in which R1 and R2, the same or different, have the following meanings: - hydrogen; - C1-C7 alkyl; - aryl, arylalkyl or arylalkyl unsubstituted or optionally having in the aromatic rings one to f
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