Phenylacetic acid compound
AssigneeOno Pharmaceutical Co., Ltd.
InventorsAtsushi Naganawa, Toshihiko Nagase
Life of this patent
Estimating the term…
Abstract
A compound represented by formula (I), wherein R1 represents a hydrogen atom, etc., R2 and R3 each independently represents a hydrogen atom, optionally oxidized C1-4 alkyl group or optionally protected hydroxyl group, or R2 and R3 taken together represent optionally oxidized C2-5 alkylene group, R4 represents an optionally oxidized C1-6 alkyl group, etc., R5 represents an optionally oxidized C1-6 alkyl group, etc., R6 represents an optionally oxidized C1-6 alkyl group, etc., m represents 0 or an integer from 1 to 3, n represents 0 or an integer from 1 to 4, and i represents 0 or an integer from 1 to 7.
Claims9
A compound represented by formula (I-a),
- wherein
- R1 represents a hydrogen atom or C1-4 alkyl group,
- R4, R5 and R6 each independently represents a halogen atom, optionally oxidized C1-6 alkyl group, optionally protected hydroxyl group, trihalomethyl group, —SO2R7 group, —SOR7 group, or —SR7 group,
- R7 represents a C1-6 alkyl group or optionally substituted phenyl group,
- indicates that the bond is attached in front of the sheet,
- m represents 0 or an integer from 1 to 3,
- n represents 0 or an integer from 1 to 4, and
- i represents 0 or an integer from 1 to 7,
- with the proviso that when m is 2 or more, R4 may be the same or different, when n is 2 or more, R5 may be the same or different, and when i is 2 or more, R6 may be the same or different,
- or a salt thereof, an N-oxide thereof or a hydrate thereof, and
- with the further proviso that the compound represented by formula (I-a) is not 1-(3-((2,6-dimethyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)cyclopropanecarboxylic acid, a salt thereof, or an N-oxide thereof.
A compound selected from the group consisting of
- (1) 1-(3-((2-ethyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)cyclopropanecarboxylic acid,
- (2) 1-(3-((2-ethyl-6-methyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)cyclopropanecarboxylic acid,
- (3) (3-((2,6-dimethyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)acetic acid,
- (4) (3-((2-ethyl-6-methyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)acetic acid,
- (5) hydroxy(3-((2,6-dimethyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)acetic acid, and
- (6) 2-hydroxy-2-(3-((2,6-dimethyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)propionic acid,
- or a salt thereof, an N-oxide thereof or a hydrate thereof,
- or 1-(3-((2,6-dimethyl-4-(((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methoxy)benzoyl)amino)-4-(trifluoromethyl)phenyl)cyclopropanecarboxylic acid hydrate.
A method for treatment of a disease comprising administering an effective dose of a compound represented by formula (I-a)
- wherein
- R1 represents a hydrogen atom or C1-4 alkyl group,
- R4, R5 and R6 each independently represents a halogen atom, optionally oxidized C1-6 alkyl group, optionally protected hydroxyl group, trihalomethyl group, —SO2R7 group, —SOR7 group, or —SR7 group,
- R7 represents a C1-6 alkyl group or optionally substituted phenyl group,
- indicates that the bond is attached in front of the sheet,
- m represents 0 or an integer from 1 to 3,
- n represents 0 or an integer from 1 to 4, and
- i represents 0 or an integer from 1 to 7,
- with the proviso that when m is 2 or more, R4 may be the same or different, when n is 2 or more, R5 may be the same or different, and when i is 2 or more, R6 may be the same or different,
- or a salt thereof, an N-oxide thereof or a hydrate thereof,
- wherein the disease is an allergic disease, systemic mastocytosis, anaphylaxis shock, bronchoconstriction, urticaria, eczema, acne, allergic bronchial pulmonary aspergillosis, sinusitis, migraine, nasal polypus, anaphylactic vasculitis, eosinophilic syndrome, contact dermatitis, a disease generated secondarily as a result of behavior accompanied by itch, a chronic obstructive pulmonary disease, ischemic reperfusion injury, cerebrovascular accident, traumatic brain disorder, hepatopathy, graft rejection, chronic rheumatoid arthritis, pleurisy, osteoarthritis, Crohn's disease, ulcerative colitis, irritable bowel syndrome, interstitial cystitis, muscular dystrophy, polymyositis multiple sclerosis or a sleeping disorder.
Dependencies are inferred from the claim text.