4,4-Difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or salt thereof
AssigneeAstellas Pharma Inc.
InventorsHiroyuki Koshio, Issei Tsukamoto, Akio Kakefuda, Seijiro Akamatsu, Chikashi Saitoh
Life of this patent
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Abstract
A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.
Claims28
1-12. (canceled)
A method of agonizing an arginine vasopressin V2 receptor, comprising contacting an arginine vasopressin V2 receptor with a pharmaceutical composition comprising a carrier and a 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound represented by a formula (I) or a pharmaceutically acceptable salt thereof
- wherein the symbols have the following meanings:
- R1:
- amino which may be substituted, —OH or —O-lower alkyl,
- R2:
- CF3 or halogen,
- R3:
- H or halogen,
- a, b:
- each represents single bond or double bond, wherein one is single bond and the other is double bond,
- —X—:
- (1) —CH═CH—, —CH═N—, —N═CH—, —N═N— or —S— when a is single bond and b is double bond,
- (2) —N— when a is double bond and b is single bond,
- Y:
- (1) CH or N when a is single bond and b is double bond,
- (2) S when a is double bond and b is single bond,
- -A-:
- —O—, —S—, —NH— or —N(lower alkyl), and
- B:
- lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl or aryl, each of which may be substituted.
A method of treating nocturia, comprising administering to a patient having nocturia a pharmaceutical composition comprising a carrier and a 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound represented by a formula (I) or a pharmaceutically acceptable salt thereof
- wherein the symbols have the following meanings:
- R1:
- amino which may be substituted, —OH or —O-lower alkyl,
- R2:
- CF3 or halogen,
- R3:
- H or halogen,
- a, b:
- each represents single bond or double bond, wherein one is single bond and the other is double bond,
- —X—:
- (1) —CH═CH—, —CH═N—, —N═CH—, —N═N— or —S— when a is single bond and b is double bond,
- (2) —N— when a is double bond and b is single bond,
- Y:
- (1) CH or N when a is single bond and b is double bond,
- (2) S when a is double bond and b is single bond,
- -A-:
- —O—, —S—, —NH— or —N(lower alkyl), and
- B:
- lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl or aryl, each of which may be substituted.
A method of treating central diabetes insipidus, comprising administering to a patient having central diabetes insipidus a pharmaceutical composition comprising a carrier and a 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound represented by a formula (I) or a pharmaceutically acceptable salt thereof
- wherein the symbols have the following meanings:
- R1:
- amino which may be substituted, —OH or —O-lower alkyl,
- R2:
- CF3 or halogen,
- R3:
- H or halogen,
- a, b:
- each represents single bond or double bond, wherein one is single bond and the other is double bond,
- —X—:
- (1) —CH═CH—, —CH═N—, —N═CH—, —N═N— or —S— when a is single bond and b is double bond,
- (2) —N— when a is double bond and b is single bond,
- Y:
- (1) CH or N when a is single bond and b is double bond,
- (2) S when a is double bond and b is single bond,
- -A-:
- —O—, —S—, —NH— or —N(lower alkyl), and
- B:
- lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl or aryl, each of which may be substituted.
Dependencies are inferred from the claim text.