Kon Tatsuya (Ashiya JPX) Kato Shiro (Sakai JPX) Morie Toshiya (Matsubara JPX) Karasawa Tadahiko (Toyonaka JPX) Yoshida Naoyuki (Matsubara JPX)
출원인 / 주소
Dainippon Pharmaceutical Co., Ltd. (Osaka JPX 03)
인용정보
피인용 횟수 :
30인용 특허 :
2
초록▼
An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, [Figure] (1) wherein Y represents -NH-or -O-; R1 and R2 are identical or different and each represents a hydrogen atom, a lower
An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, [Figure] (1) wherein Y represents -NH-or -O-; R1 and R2 are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R1 and R2, taken together, form a lower alkylene group; R3 represents a hydrogen atom, a lower alkyl group, or a phenyl group; R4 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group; R5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group, a nitro group, an amino group or an acylamino group; m represents a number of 1, 2, 3 or 4; n represents a number of 1, 2 or 3; and p represents a number of 1, 2, 3 or 4. This compound is useful as a potent and selective antagonist of serotonin 3 (5-HT3) receptor.
대표청구항▼
An indazole-3-carboxylic acid compound represented by the following formula (I) or a physiologically acceptable acid addition salt or quaternary ammonium salt thereof. [Figure] (I) wherein Y represents -NH-or -O-; R1 and R2 are identical or different and each represents (1) hydrogen; (2) C1-C6 alkyl
An indazole-3-carboxylic acid compound represented by the following formula (I) or a physiologically acceptable acid addition salt or quaternary ammonium salt thereof. [Figure] (I) wherein Y represents -NH-or -O-; R1 and R2 are identical or different and each represents (1) hydrogen; (2) C1-C6 alkyl; (3) C1-C6 alkyl substituted by (a) C3-C8 cycloalkyl, (b) C5-C8 cyclo-alkenyl, (c) C1-C6 alkoxy, (d) hydroxy, (e) cyano, (f) oxo, (g) C2-C4 alkanoyloxy, (h) unsubstituted, mono- or di-substituted benzoyloxy wherein said substituent is halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano, nitro or carboxy, (i) amino, (j) mono- or di-C1-C4 alkylamino, (k) C2-C4 alkanoyl-amino, (1) unsubstituted, mono- or di-substituted benzoylamino wherein said substituent is halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, nitro, cyano or carboxy, (m) 5 to 8-membered heteroalicyclic or heteroaromatic having 1 to 2 hetero atoms selected from oxygen, nitrogen and suflur atoms, or (n) halogen; (4) C3-C8 cycloalkyl; (5) C2-C6 alkenyl; (6) C5-C8 cycloalkenyl; (7) C2-C6 alkynyl; (8) phenyl-C1-C6 alkyl in which the phenyl is unsubstituted or is substituted by (a) halogen, (b) C1-C6 alkyl, (c) tribluoromethyl, (d) hydroxy, (e) C1-C6 alkoxy, (f) amino, (g) mono- or di-C1-C6 alkylamino, (h) C2-C6 alkanoylamino, (i) unsubstituted, mono- or di-substituted benzoylamino wherein said substituent is halogen, C1-C4 alkyl, tribluoromethyl, hydroxy, C1-C4 alkoxy, amino, nitro, cyano or carboxy, (j) nitro, (k) cyano, (1) carboxy, or (m) C2-C4 alkoxycarbonyl; (9) C2-C6 akoxycarbonyl; (10) phenyl-C1-C6 alkyloxycarbonyl in which the phenyl is unsubstituted or is substituted by (a) halogen, (b) C1-C6 alkyl, (c) trifluoromethyl, (d) hydroxy, (e) C1-C6 alkoxy, (f) amino, (g) nitro, (h) cyano, or (i) carboxy; (11) C2-C6 alkanoyl; or (12) benzoyl which is unsubstituted or is substituted by (a) halogen, (b) C1-C6 alkyl, (c) trifluromethyl, (d) hydroxy, (e) C1-C6 alkoxy, (f) amino, (g) nitro, (h) cyano, or (i) carboxy; or R1 and R2, taken together, form C1-C6 alkylene; R3 represents hydrogen, C1-C6 alkyl, or phenyl; R4 represents (1) hydrogen; (2) C1-C6 alkyl; (3) C1-C6 alkyl substituted by (a) C3-C8 cycloalkyl, (b) C5-C8 cycloalkenyl, (c) C1-C6 alkoxy, (d) hydroxy, (e) cyano, (f) oxo, (g) C2-C4 alkanoyloxy, (h) unsubstituted, mono- or di-substituted benzoyloxy wherein said substituent is halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, nitro, cyano or carboxy, (i) amino, (j) mono- or di-C1-C4 alkylamino, (k) C2-C4 alkanoyl amino, (1) unsubstituted, mono- or di-substituted benzoylamino wherein said substituent is halogne, C1-C4 alkyl, tribluoromethyl, hydroxy, C1-C4 alkoxy, amino, nitro, cyano or carboxy, (m) 5 to 8 membered heteroalicyclic or heteroaromatic having 1 to 2 hetero atoms selected from oxygen, nitrogen and sulfur atoms, or (n) halogen; (4) C3-C8 cycloalkyl; (5) C2-C6 alkenyl; (6) C5-C8 cycloalkenyl; (7) C2-C6 alkynyl; (8) phenyl-C1-C6 alkyl in which the phenyl is unsubstituted or is substituted by (a) halogen, (b) C1-C6 alkyl, (c) tribluoromethyl, (d) hydroxy, (e) C1-C6 alkoxy, (f) amino, (g) mono- or di-C1-C6 alkylamino, (h) C2-C6 alkanoylamino, (i) unsubstituted, mono- or di-substituted benzoylamino wherein said substituent is halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, nitro, cyano or carb oxy, (j) nitro, (k) cyano, (l) carboxy or (m) C2-C4 alkoxycarbonyl; (9) C2-C6 alkoxycarbonyl; (10) phenyl-C1-C6 alkoxycarbonyl in which the phenyl is unsubstituted or is substituted by (a) halogen, (b) C1-C6 alkyl, (c) trifluoromethyl, (d) hydroxy, (e) C1-C6 alkoxy, (f) amino, (g) nitro, (h) cyano, or (i) carboxy; (11) C2-C6 alkanoyl; or (12) benzoyl which is unsubstituted or is mono- or di-substituted by (a) halogen, (b) C1-C6 alkyl, (c) trifluoromethyl, (d) hydroxy, (e) C1-C6 alkoxy, (f) amino, (g) nitro, (h) cyano, or (i) carboxy; R5 represetns hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxy trifluoromethyl, nitro, amino, C2-C6 alkanoylamino or benzoylamino; m represents 1 or 2; n represents 2 or 3; and p represents 1, 2 or 3.
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