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US 8,772,314 B2Granted
Glycine derivatives and medicinal compositions thereof
AssigneeChiesi Farmaceutici S.p.A.
InventorsGabriele Amari, Mauro Riccaboni, Marco Farina
Life of this patent
Estimating the term…
Abstract
Alkaloid aminoester derivatives according to formula (I) and (VI) act as muscarinic receptor antagonists.
Claims12
A compound of formula (I):
- wherein:
- R1 is —H, or linear or branched (C1-C10)alkyl, (C2-C6)alkenyl, aryl, (C3-C8)cycloalkyl, (C5-C10)heterocycloalkyl, aryl(C1-C6)alkyl, or heteroaryl, each of which may be optionally substituted by one or more substituents selected from the group consisting of a halogen atom, —OH, oxo (═O), —SH, —NO2, —N(R5)(R8), —CN, —CON(R5)2, —NHCO(R5), —COR5, —CO2R5, (C1-C10)alkylsulfanyl, (C1-C10)alkylsulfinyl, (C1-C10)alkylsulfonyl, (C1-C10)alkyl, (C1-C10)alkylcarboxyl, (C1-C10)alkoxy, aryl, aryloxy, and heteroaryl;
- G is —OC(O)—, —SO2—, or —C(O)—;
- R2 is —H or (C1-C10)alkyl or aryl(C1-C6)alkyl, each of which may be optionally substituted by one or more substituents selected from the group consisting of a halogen atom, —OH, oxo (═O), —SH, —NO2, —N(R5)2, —CN, —CON(R5)2, —NHCO(R5), —CO(R5), —CO2(R5), (C1-C10)alkylsulfanyl, (C1-C10)alkylsulfinyl, (C1-C10)alkylsulfonyl, (C1-C10)alkyl, (C1-C10)alkylcarboxyl, (C1-C10)alkoxy, aryl, aryloxy, and heteroaryl;
- R3 is —H or (C1-C10)alkyl, aryl, (C3-C8)cycloalkyl, heteroaryl, aryl(C1-C6)alkyl, or heteroaryl(C1-C6)alkyl, each of which may be optionally substituted by one or more substituents selected from the group consisting of a halogen atom, —OH, oxo (═O), —SH, —NO2, —N(R5)2, —CN, —CON(R5)2, —NHCO(R5), —CO(R5), —CO2(R5), (C1-C10)alkylsulfanyl, (C1-C10)alkylsulfinyl, (C1-C10)alkylsulfonyl, (C1-C10)alkyl, (C1-C10)alkylcarboxyl, (C1-C10)alkoxy, aryl, aryloxy, aryl(C1-C10)alkylenoxy, and heteroaryl;
- R6 is a group of formula (i):
- wherein
- A− is a physiologically acceptable anion;
- R4 is a group of formula (Y):
- —(CH2)p-P—(CH2)q-W (Y)
- wherein
- p is 0 or an integer from 1 to 4;
- q is 0 or an integer from 1 to 4;
- P is absent or is —O—, —S—, —SO—, —SO2—, —C(O)—, —N(R5)-, —CH═CH—, —N(R5)(SO2)—, —N(R5)(COO)—, —N(R5)(C(O))—, —S(O2)N(R5)-, —CO(O)N(R5)-, or —C(O)N(R5)-;
- W is —H, or linear or branched (C1-C10)alkyl, (C2-C6)alkenyl, aryl, (C3-C8)cycloalkyl, (C5-C10)heterocycloalkyl, aryl(C1-C6)alkyl, or heteroaryl, each of which may be optionally substituted by one or more substituents selected from the group consisting of a halogen atom, —OH, oxo (═O), —SH, —NO2, —N(R5)2, —CN, —CON(R5)2, —NH(COR5), —CO(R5), —CO2(R5), (C1-C10)alkylsulfanyl, (C1-C10)alkylsulfinyl, (C1-C10)alkylsulfonyl, (C1-C10)alkyl, (C1-C10)alkylcarboxyl, (C1-C10)alkoxy, aryl, aryloxy, and heteroaryl;
- R5 and R8 are each independently —H, or (C1-C10)alkyl, (C1-C10)alkoxy, (C2-C6)alkynyl, (C2-C6)alkenyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C10)alkyl, heteroaryl, (C1-C10)alkyl-heteroaryl, or aryl, each of which may be optionally substituted by one or more substituents selected from the group consisting of a halogen atom, —OH, oxo (═O), —SH, —NO2, —CN, —CONH2, (C1-C10)alkylsulfanyl, (C1-C10)alkylsulfinyl, (C1-C10)alkylsulfonyl, (C1-C10)alkyl, (C1-C10)alkylcarboxyl, (C1-C10)alkoxy, aryl, aryloxy, and heteroaryl;
- or a pharmaceutically acceptable salt thereof.
14 more elements
Dependencies are inferred from the claim text.