1. A multilayer film comprising:
a first layer comprising at least about 40% of one or more modified polyamides, based on the weight of the first layer;
a second layer comprising at least about 40% of one or more unmodified polyamides, based on the weight of the second layer; and
a third layer comprising at least about 40% of one or more tie polymers selected from ethylenevinyl acetate copolymer, ethylene(meth)acrylic acid copolymer, ethyleneC1-C12 alkyl (meth)acrylate copolymer, and anhydride-modified polyolefin, based on the weight of the third layer; wherein
the second layer is directly adhered to the first and third layers.
2. The film of claim 1 wherein the first layer comprises at least about 40% of one or more modified amorphous polyamides, based on the weight of the first layer.
3. The film of claim 1 wherein the first layer comprises one or more modified amorphous polyamides in an amount sufficient to impart to the film an oxygen transmission rate of at most about 150 cubic centimeters (at standard temperature and pressure) per square meter per day per 1 atmosphere of oxygen pressure differential measured at 0% relative humidity and 23\xb0 C.
4. The film of claim 1 wherein the first layer comprises at least about 40% modified nylon-6,I6,T, based on the weight of the first layer.
5. The film of claim 1 wherein the first layer comprises at least about 40% of one or more modified amorphous polyamides, based on the weight of the first layer, wherein the one or more modified amorphous polyamides have at least about 40 mole % modified amino end groups relative to the total amount of free and modified amino end groups of the one or more modified amorphous polyamides.
6. The film of claim 1 wherein the first layer comprises at least about 40% of one or more modified amorphous polyamides, based on the weight of the first layer, wherein the one or more modified amorphous polyamides have a mole ratio of free amino end groups to free carboxyl end groups of less than about 50:100.
7. The film of claim 1 wherein the first layer comprises at least about 70% of one or more modified polyamides, based on the weight of the first layer.
8. The film of claim 1 wherein the first layer comprises at least about 70% of one or more modified amorphous polyamides, based on the weight of the first layer.
9. The film of claim 1 wherein the first layer comprises at least about 90% of one or more modified amorphous polyamides, based on the weight of the first layer.
10. The film of claim 1 wherein the second layer comprises at least about 70% of one or more unmodified polyamides, based on the weight of the second layer.
11. The film of claim 1 wherein the second layer comprises at least about 90% of one or more unmodified polyamides, based on the weight of the second layer.
12. The film of claim 1 wherein the one or more unmodified polyamides of the second layer are selected from one or more of nylon-6; nylon-6,6; nylon-6,12; nylon-12; and nylon-6,66.
13. The film of claim 1 wherein the third layer comprises at least about 70% of the one or more tie polymers, based on the weight of the third layer
14. The film of claim 1 wherein the one or more tie polymers of the third layer comprise anhydride-modified polymer.
15. The film of claim 1 wherein the one or more tie polymers of the third layer comprise anhydride-modified ethylenevinyl acetate copolymer.
16. The film of claim 1 wherein the wherein the one or more tie polymers of the third layer comprise anhydride-modified ethyleneC1-C12 alkyl (meth)acrylate copolymer.
17. The film of claim 1 wherein the one or more tie polymers of the third layer comprise ethylenevinyl acetate copolymer.
18. The film of claim 1 wherein the one or more tie polymers of the third layer comprise ethylene(meth)acrylic acid copolymer.
19. The film of claim 1 wherein the one or more tie polymers of the third layer comprise ethyleneC1-C12 alkyl (meth)acrylate copolymer.
20. The film of claim 1 wherein the one or more tie polymers of the third layer comprise ethylenevinyl acetate copolymer having a vinyl acetate content of at least about 25 weight %.
21. The film of claim 1 further comprising a fourth layer directly adhered to the third layer, the fourth layer comprising one or more polyolefins.
22. A package comprising the film of claim 1.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
What is claimed is
1. Phenylalanine derivatives of the following general formula (1) or pharmaceutically acceptable salts thereof:
109
wherein a represents one of the following general formulae (2), (2-1), (2-2), (2-3), (2-4) and (2-5):
110
wherein Arm represents a cyclic alkyl group or an aromatic ring containing 0, 1, 2, 3 or 4 hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen atoms,
R1 represents a hydrogen atom, an alkyl group which may have a substituent(s), 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 hydroxyalkyl group, a lower halogenoalkyl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, an alkenyl group which may have a substituent(s), a lower hydroxyalkenyl group, a lower halogenoalkenyl group, an alkynyl group which may have a substituent(s), an aryl group, a heteroaryl group, a lower alkyloxycarbonyl group, a substituted or unsubstituted carbamoyl group, a lower alkanoyl group, an aroyl group, a lower alkylsulfonyl group or a substituted or unsubstituted sulfamoyl group,
R2 to R6 and R10 to R33 may be the same or different from one another and each represents a hydrogen atom, an alkyl group which may have a substituent(s), 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 hydroxyalkyl group, a lower halogenoalkyl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, an alkenyl group which may have a substituent(s), a lower hydroxyalkenyl group, a lower halogenoalkenyl group, an alkynyl group which may have a substituent(s), an aryl group, a heteroaryl 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, a halogen atom, a hydroxyl group, 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 lower hydroxylalkoxyl group, a lower halogeno alkoxyl group, a lower halogenoalkylthio group, a cycloalkyloxy group which may contain a hetero atom(s) in the ring thereof, an aryloxy group, a heteroaryloxy group, a nitro group, a cyano group, a substituted or unsubstituted amino group, carboxyl group or a trialkylammonium group,
B represents a hydroxyl group, an alkoxyl group, a substituted lower alkoxyl group or a hydroxylamino group,
in cases where A represents the general formula (2), (2-1), (2-2), (2-3) or (2-4), C represents an aryl group, a heteroaryl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, 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), an alkyl group which may have a substituent(s), a lower hydroxyalkyl group, a lower halogenoalkyl group, an alkenyl group which may have a substituent(s), a lower hydroxyalkenyl group, a lower halogenoalkenyl group, an alkynyl group which may have a substituent(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 hydroxylalkoxyl group, a lower halogeno alkoxyl group, a substituted or unsubstituted amino group or a lower alkylthio group, or C also represents an organic group of the following general formula (3):
111
wherein D and D may be the same or different from one another and each represents a hydrogen atom, an alkyl group which may have a substituent(s), an alkenyl group which may have a substituent(s) or an alkynyl group which may have a substituent(s), and
D and D may be bonded together to form a ring which may contain one or two oxygen, nitrogen or sulfur atoms,
E represents an amino group or a lower alkylamino group which may have a substituent(s), including an amino group(s) having two substituents wherein the substituents are bonded together to form a ring,
in cases where A represents the general formula (2-5), C represents an organic group of the general formula (3), and
J and J may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkyloxy group, a nitro group, an amino group or a hydroxyl group.
2. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 1, wherein A represents the general formula (2) wherein Arm represents a cyclic alkyl group or an aromatic ring containing 0, 1, 2, 3 or 4 hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen atoms,
R1 represents a hydrogen atom, an alkyl group which may have a substituent(s), 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 hydroxyalkyl group, a lower halogenoalkyl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, an alkenyl group which may have a substituent(s), a lower hydroxyalkenyl group, a lower halogenoalkenyl group, an alkynyl group which may have a substituent(s), an aryl group, a heteroaryl group, a lower alkyloxycarbonyl group, a substituted or unsubstituted carbamoyl group, a lower alkanoyl group, an aroyl group, a lower alkylsulfonyl group or a substituted or unsubstituted sulfamoyl group,
R2, R3, R4, R5 and R6 may be the same or different from one another and each represents a hydrogen atom, an alkyl group which may have a substituent(s), 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 hydroxyalkyl group, a lower halogenoalkyl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, an alkenyl group which may have a substituent(s), a lower hydroxyalkenyl group, a lower halogenoalkenyl group, an alkynyl group which may have a substituent(s), an aryl group, a heteroaryl 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, a halogen atom, a hydroxyl group, 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 lower hydroxylalkoxyl group, a lower halogeno alkoxyl group, a lower halogenoalkylthio group, a cycloalkyloxy group which may contain a hetero atom(s) in the ring thereof, an aryloxy group, a heteroaryloxy group, a nitro group, a cyano group, a substituted or unsubstituted amino group, carboxyl group or a trialkylammonium group,
B represents a hydroxyl group, an alkoxyl group, a substituted lower alkoxyl group or a hydroxylamino group,
C represents an aryl group, a heteroaryl group, a cycloalkyl group which may contain a hetero atom(s) in the ring thereof, 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), an alkyl group which may have a substituent(s), a lower hydroxyalkyl group, a lower halogenoalkyl group, an alkenyl group which may have a substituent(s), a lower hydroxyalkenyl group, a lower halogenoalkenyl group, an alkynyl group which may have a substituent(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 hydroxylalkoxyl group, a lower halogeno alkoxyl group, a substituted or unsubstituted amino group or a lower alkylthio group, or C represents an organic group of the above general formula (3),
wherein D and D may be the same or different from one another and each represents a hydrogen atom, an alkyl group which may have a substituent(s), an alkenyl group which may have a substituent(s) or an alkynyl group which may have a substituent(s), and
D and D may be bonded together to form a ring which may contain one or two oxygen, nitrogen or sulfur atoms,
E represents an amino group or a lower alkylamino group which may have a substituent(s), including an amino group(s) having two substituents wherein the substituents are bonded together to form a ring, and
J and J may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkyloxy group, a nitro group, an amino group or a hydroxyl group.
3. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein, in the general formula (1), A represents the above general formula (2) wherein Arm is a benzene ring, R1 is a lower alkyl group, R2 is a lower alkyl group, a lower alkoxyl group or a hydrogen atom, R3, R4, R5 and R6 may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower halogenoalkyl group, a hydroxyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an amino group substituted with a lower alkyl group, an amino group substituted with a lower alkanoyl group, an amino group substituted with a lower alkyloxycarbonyl group, a lower alkylsulfonyl groups or a lower trialkylammonium group.
4. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein B represents a hydroxyl group or a lower alkoxyl group.
5. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein C represents the above general formula (3) or the following general formulae (3-1), (3-2), (3-3) or (3-4):
112
wherein R7 represents a halogen atom or methyl group, R8 represents a halogen atom, methyl group, trifluoromethyl group, methoxy group or a hydrogen atom, R9 represents a hydrogen atom, halogen atom, hydroxyl group, lower alkyl group, cycloalkyl group which may contain a hetero atom(s) in the ring thereof, lower alkoxyl group, lower alkylthio group, lower halogenoalkyl group, lower halogenoalkoxyl group, lower halogenoalkylthio group, nitro group, cyano group, amino group, amino group substituted with a lower alkyl group(s), lower trialkylammonium group, lower alkylsulfonylamino group or tetrazolyl group.
6. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein, in the general formula (1), A represents the above general formula (2) wherein Arm is a benzene ring, R1 is a lower alkyl group, R2 is a lower alkyl group, a lower alkoxyl group or a hydrogen atom, R3, R4, R5 and R6 may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower halogenoalkyl group, a hydroxyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an amino group substituted with a lower alkyl group, a lower alkylsulfonyl groups or a lower trialkylammonium group,
B represents a hydroxyl group or a lower alkoxyl group, and
C represents the above general formulae (3), (3-1), (3-2), (3-3) or (3-4).
7. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein, in the general formula (1), A represents the above general formula (2) wherein Arm is a benzene ring, R1 is a lower alkyl group, R2 is a lower alkyl group, R3, R4, R5 and R6 may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower halogenoalkyl group, a hydroxyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an amino group substituted with a lower alkyl group, a lower alkylsulfonyl groups or a lower trialkylammonium group,
B represents a hydroxyl group or a lower alkoxyl group,
C represents the above general formulae (3-1) or (3-2), and
J and J are a hydrogen atom.
8. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein, in the general formula (1), A represents the above general formula (2) wherein Arm is a benzene ring, R1 is a lower alkyl group, R2 is a lower alkoxyl group, R3, R4, R5 and R6 may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower halogenoalkyl group, a hydroxyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an amino group substituted with a lower alkyl group, a lower alkylsulfonyl groups or a lower trialkylammonium group,
B represents a hydroxyl group or a lower alkoxyl group,
C represents the above general formulae (3-1) or (3-2), and
J and J are a hydrogen atom.
9. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein, in the general formula (1), A represents the above general formula (2) wherein Arm is a benzene ring, R1 is a lower alkyl group, R2 is a hydrogen atom, R3, R4, R5 and R6 may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower halogenoalkyl group, a hydroxyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an amino group substituted with a lower alkyl group, a lower alkylsulfonyl groups or a lower trialkylammonium group,
B represents a hydroxyl group or a lower alkoxyl group,
C represents the above general formulae (3-1) or (3-2), and
J and J are a hydrogen atom.
10. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 2, wherein, in the general formula (1), A represents the above general formula (2) wherein Arm is a benzene ring, R1 is a methyl group or an ethyl group, R2 is a methoxy group, an ethoxy group, a propoxy group, a methyl group, an ethyl group, a propyl group or a butyl group, R3, R4, R5 and R6 may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower halogenoalkyl group, a hydroxyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an amino group substituted with a lower alkyl group, a lower alkylsulfonyl groups or a lower trialkylammonium group,
B represents a hydroxyl group,
C represents the above general formulae (3-1) or (3-2) wherein R7 represents a halogen atom or methyl group, R8 represents a halogen atom, R9 represents a hydrogen atom, halogen atom, hydroxyl group, lower alkyl group, lower alkoxyl group, lower alkylthio group, lower halogenoalkyl group, lower halogenoalkoxyl group, lower halogenoalkylthio group, nitro group, cyano group, amino group, lower alkylamino group, trialkylammonium group, methanesulfonyl amino group or tetrazolyl group, and
J and J are a hydrogen atom.
11. Phenylalanine derivatives of the following general formula (22) or pharmaceutically acceptable salts thereof:
113
wherein A represents one of the following general formulae (23-1), (23-2), (23-3) and (23-4):
114
wherein Arm represents a cyclic alkyl group or an aromatic ring containing 0, 1, 2, 3 or 4 hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen atoms,
the composite line of solid line and dotted line in the formula (23-4) represents a single bond or a double bond,
U, V and X represent C(O), S(O)2, C(-R38)(-R39), C(C(R38)(R39)), C(S), S(O), P(O)(OH) or P(H)(O),
W represents C(-R40) or a nitrogen atom,
R34 to R40 may be the same or different from one another and each represents 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 hydroxylalkoxyl group, a lower halogenoalkyl group, a lower halogeno alkoxyl 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, R38 and R39 may be bonded together to form a ring which may contain one or two oxygen, nitrogen or sulfur atoms,
B represents a hydroxyl group, a lower alkoxyl group, a substituted lower alkoxyl group or a hydroxylamino group,
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),
G and G may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkyloxy group or nitro group.
12. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 1, wherein, in the general formula (1), A represents the following general formula (2-6):
115
B represents a hydroxyl group or a lower alkoxyl group,
C represents the general formulae (3-1), (3-2) or (3-3):
116
R7 represents a halogen atom or a methyl group, R8 represents a halogen atom, R9 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxyl group, a lower alkylthio group, a lower halogenoalkyl group, a lower halogeno alkoxyl group, a lower halogenoalkylthio group, a nitro group, a cyano group, an amino group, a lower alkylamino group, a trialkylammonium group, a methansulfonylamino group or a tetrazolyl group, and
J and J represent a hydrogen atom.
13. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 1, wherein, in the general formula (1), A represents the following general formula (2-7):
117
B represents a hydroxyl group or a lower alkoxyl group,
C represents the general formulae (3-1), (3-2) or (3-3):
118
R7 represents a halogen atom or a methyl group, R8 represents a halogen atom, R9 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxyl group, a lower alkylthio group, a lower halogenoalkyl group, a lower halogeno alkoxyl group, a lower halogenoalkylthio group, a nitro group, a cyano group, an amino group, a lower alkylamino group, a trialkylammonium group, a methansulfonylamino group or a tetrazolyl group, and
J and J represent a hydrogen atom.
14. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 12, wherein, in the general formula (1), A represents the general formula (2-6), B represents a hydroxyl group or a lower alkoxyl group, C represents the above general formula (3-1) wherein R7 represents a chlorine atom, R8 represents a chlorine atom, R9 represents a hydrogen atom, and
J and J are a hydrogen atom.
15. The phenylalanine derivatives or pharmaceutically acceptable salts thereof according to claim 13, wherein, in the general formula (1), A represents the general formula (2-7), B represents a hydroxyl group or a lower alkoxyl group, C represents the general formula (3-1) wherein R7 represents a chlorine atom, R8 represents a chlorine atom, R9 represents a hydrogen atom, and
J and J are a hydrogen atom.
16. An 4 integrin antagonist containing a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.
17. An 4 integrin antagonist containing a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 11 as an active ingredient.
18. A therapeutic agent or preventive agent for inflammatory diseases in which 4 integrin-depending adhesion process participates in the pathology, which contains a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.
19. A therapeutic agent or preventive agent for inflammatory diseases in which 4 integrin-depending adhesion process participates in the pathology, which contains a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 11 as an active ingredient.
20. A pharmaceutical composition containing a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.
21. A pharmaceutical composition containing a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 11 as an active ingredient.
22. A therapeutic agent or preventive agent for rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjgren’s syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection, which contains a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.
23. A therapeutic agent or preventive agent for rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjgren’s syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection, which contains a phenylalanine derivative or a pharmaceutically acceptable salt thereof according to claim 11 as an active ingredient.