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US 7,605,165 B2Granted
Phenylalanine derivatives
AssigneeAjinomoto Co., Inc.
InventorsKazuyuki Sagi, Hiroyuki Izawa, Akira Chiba, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuji Tanaka, Miho Ono, Masahiro Murata
Life of this patent
Estimating the term…
Abstract
The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning α4 integrin.
Claims24
A phenylalanine compound of the following formula (1) or a pharmaceutically acceptable salt thereof:
- wherein A is a group represented by formula (3-3′):
- or (3-4):
- wherein Arm represents a benzene ring
- R1, R2, R3, and R4 may be the same or different from one another and each represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a substituted lower alkyl group, a lower alkenyl group, a substituted lower alkenyl group, a lower alkynyl group, a substituted lower alkynyl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, an aryl group, a heteroaryl group, a lower alkyl group substituted with a cycloalkyl group(s) which may contain a hetero atom(s) in the ring thereof, a lower alkyl group substituted with an aryl group(s), a lower alkyl group substituted with a heteroaryl group(s), a lower alkoxyl group, a lower alkylthio group, a lower alkoxyl group and lower alkylthio group substituted with a cycloalkyl group(s) which may contain a hetero atom(s) in the ring thereof, a lower alkoxyl group and lower alkylthio group substituted with an aryl group(s), a lower alkoxyl group and lower alkylthio group substituted with a heteroaryl group(s), a cycloalkyloxy group which may contain a hetero atom(s) in the ring thereof, an aryloxy group, a heteroaryloxy group, a lower hydroxyalkyl group, a lower hydroxyalkenyl group, a lower hydroxyalkoxyl group, a lower halogenoalkyl group, a lower halogenoalkoxyl group, a lower halogenoalkylthio group, a lower halogenoalkenyl group, nitro group, cyano group, a substituted or unsubstituted amino group, carboxyl group, a lower alkyloxycarbonyl group, a substituted or unsubstituted carbamoyl group, a lower alkanoyl group, an aroyl group, a lower alkylsulfonyl group, a substituted or unsubstituted sulfamoyl group or an ammonium group,
- B represents an organic group represented by the following formula (B-1) or (B-2), a substituted or unsubstituted amino group (except for a hydroxylamino group) or a substituted or unsubstituted mercapto group,
- wherein Y represents a substituted or unsubstituted divalent lower hydrocarbon group, E represents a substituted or unsubstituted acyloxy group, a substituted or unsubstituted lower alkoxycarbonyloxy group, a substituted or unsubstituted amino group, carboxyl group, a substituted or unsubstituted lower alkoxycarbonyl group, a halogen atom, an aryl group, a heteroaryl group, a substituted or unsubstituted alkoxyl group or a substituted or unsubstituted carbamoyl group, Rb1 represents a hydrogen atom or a lower alkyl group, and Y and E may be bonded together to form a ring,
- C represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkyl group substituted with a cycloalkyl group(s) which may contain a hetero atom(s) in the ring thereof, a lower alkyl group substituted with an aryl group(s) or a lower alkyl group substituted with a heteroaryl group(s),
- D represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, an aryl group, a heteroaryl group, a lower alkyl group substituted with a cycloalkyl group(s) which may contain a hetero atom(s) in the ring thereof a lower alkyl group substituted with an aryl group(s), a lower alkyl group substituted with a heteroaryl group(s), a lower alkoxyl group, a lower alkoxyl group substituted with a cycloalkyl group(s) which may contain a hetero atom(s) in the ring thereof, a lower alkoxyl group substituted with an aryl group(s), a lower alkoxyl group substituted with a heteroaryl group(s), a cycloalkyloxy group which may contain a hetero atom(s) in the ring thereof, an aryloxy group, a heteroaryloxy group, a lower hydroxyalkyl group, a lower hydroxyalkenyl group, a lower hydroxyalkoxyl group, a lower halogenoalkyl group, a lower halogenoalkoxyl group, a lower halogenoalkenyl group, nitro group, cyano group, a substituted or unsubstituted amino group, carboxyl group, a lower alkyloxycarbonyl group, a substituted or unsubstituted carbamoyl group, a lower alkanoyl group, an aroyl group, a lower alkylthio group, a lower alkylsulfonyl group or a substituted or unsubstituted sulfamoyl group,
- C and D may be bonded together to form a ring which may contain one or two oxygen, nitrogen or sulfur atoms,
- T represents an interatomic bond, C(=O), C(=S), S(=O), S(=O)2,N(H)-C(=O), or N(H)-C(=S),
- J and J′ may be the same or different from each other and each represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkyloxy group or a nitro group.
8 more elements
Dependencies are inferred from the claim text.