Patent US4532929A successfully refreshed from Google Patents.
EP0235752A2
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EP
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Piperidine derivative, pharmaceutical composition containing the same and use
Assignee: Eisai Co Ltd
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Filing: 1987-02-26
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Granted: —
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Expires: 2007-02-26
Abstract
Abstract A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: in which R 1 is a lower alkyl or a tolyl, R 2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R 3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is -CO-, -CH 2 - or -CHOH-, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, -CH 2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, 1 being 1 or 2, -A-B, A being -(CH 2 )n-, n being an integer of 1 to 5, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl. group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkene having a double bond formed between carbon atoms adjacent to each other by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof, k being an integer of 2 to 5, - (CH 2 )p-CO-, p being an integer of 1 to 4, B being cyano, - NR 4 R 5 , a heterocyclic ring or a condensed aromatic ring. A pharmaceutical composition containing said compounds as active ingredient, and the use of said compound in the preparation of a medicament for the treatment of arrhythmia are also disclosed.
Inventors
- 👤 Hitoshi Oinuma
- 👤 Motosuke Yamanaka
- 👤 Kazutoshi Miyake
- 👤 Tomonori Hoshiko
- 👤 Norio Minami
- 👤 Tadao Shoji
- 👤 Yoshiharu Daiku
- 👤 Kohei Sawada
- 👤 Kenichi Nomoto
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 16:53
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/18; C07D211/20; C07D211/22; C07D401/00; C07D401/02; C07D401/04; A; A61; A61P; A61P9/00; A61P9/06; C07D211/26; C07D211/28; C07D211/30; C07D211/32; C07D401/06; C07D401/14; C07D405/00; C07D405/02; C07D405/04; C07D409/00; C07D409/02; C07D409/04; C07D417/00; C07D417/02; C07D417/04; C07D471/00; C07D471/02; C07D471/04; C07D473/00; C07D473/02; C07D473/04; C07D473/06; C07D473/10
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
122 words
A process for preparing a piperidine derivative having the formula (I) shown below and a pharmacologically acceptable salt thereof in which Rl is a lower alkyl or a tolyl, R2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cylcoalkylalkyl, X is -CO-, g is an integer of 1 to 3, h is an integer of 1 to 3, and Y is hydrogen, which comprises hydrolyzing a compound of formula ( I ) in which Rl, R2, R3, X, g and h are as defined above and Y is -COR' where R' is lower alkyl or phenyl, and if necessary, converting the product to a pharmacologically acceptable salt.
Claim 2
Dependent Claim
122 words
A process for preparing a piperidine derivative having the formula (I) shown below and a pharmacologically acceptable salt thereof in which Rl is a lower alkyl or a tolyl, R2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cylcoalkylalkyl, X is -CO-, g is an integer of 1 to 3, h is an integer of 1 to 3, and Y is hydrogen, which comprises hydrolyzing a compound of formula ( I ) in which Rl, R2, R3, X, g and h are as defined above and Y is -COR' where R' is lower alkyl or phenyl, and if necessary, converting the product to a pharmacologically acceptable salt.
Claim 3
Dependent Claim
312 words
A process for preparing a piperidine derivative having the formula (I) and a pharmacologically acceptable salt thereof, in which Rl, R2, R3, X, g and h are as defined in claim 1 and Y is a lower alkyl, a lower alkenyl, cyano, -CH2COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, 1 being 1 or 2, -A-B, A being -(CH2)n-, n being an integer of 1 to 5, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkene having a double bond formed between carbon atoms adjacent to each other by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof, -(CH2)k-S-, k being an integer of 2 to 5, -(CH2)p-CO-, p being an integer of 1 to 4, B being cyano, -NR4R5, R4 and R5 each being hydrogen or a lower alkyl, R6 being hydrogen, a lower alkyl, a lower alkoxy, cyano, imidazolyl, hydroxyl or a halogen, R7 and R8 each being hydrogen, a halogen, a lower alkyl, a lower alkoxy or methanesulfonamido, R9, R10 and Rll each being hydrogen or a lower alkyl, which comprises reacting a compound of formula (I) in which Rl, R2, R3, X, g and h are as defined in claim 1, and Y is hydrogen with a compound of the formula wherein Z is a halogen atom, methanesulfoxyloxy or p-toluenesulfooxyloxy group and Y is as defined above except for hydrogen, and if necessary converting the product to a pharmacologically acceptable salt.
Claim 4
Dependent Claim
94 words
A process for preparing a compound having the formula (I), in which Rl, R2, R3, g,. h and X are as defined in claim 1 and Y is R6 being as defined in claim 2, or a pharmacologically acceptable salt thereof, which comprises reacting a compound of formula (I) in which Rl, R2, R3, g, h and X are as defined in claim 1 and Y is hydrogen, with a compound having the formula: in which R6 is as defined in claim 2 and if necessary converting the product to a pharmacologically acceptable salt.
Claim 5
Dependent Claim
80 words
A process for preparing a compound of formula (I) in which Rl, R2, R3, g and h are as defined in claim 1, X is -CHOH- and Y has any of the definitions given in claim 2, or a pharmacologically acceptable salt thereof, which comprises reducing a compound of formula (I), in which Rl, R2, R3, g, h and Y are as defined above and X is -CO- , and if necessary converting the product to a pharmacologically acceptable salt.
Claim 6
Dependent Claim
100 words
A process for preparing a compound of formula (I), in which Rl, R2, X, g and h are as defined in claim 1, Y has any of the definitions given in claim 2 except for hydrogen, and R3 is lower alkyl, or a pharmacologically acceptable salt thereof, which comprises reacting a compound of formula (I) in which Rl, R2, X, g, h and Y are as defined above and R3 is hydrogen with a compound of the formula wherein R' is lower alkyl and Hal is a halogen atom and if necessary converting the product to a pharmacologically acceptable salt.
Claim 7
Dependent Claim
83 words
A process for preparing a compound of formula (I) in which Rl, R2, R3, g and h are as defined in claim 1, X is -CH 2 - and Y has any of the definitions as in claim 2 or a pharmacologically acceptable salt thereof, which comprises reducing a compound of formula (I) in which Rl, R2, R3, g, h and Y are as defined above and X is -CO- or -CHOH-, and if necessary converting the product to a pharmacologically acceptable salt.
Claim 8
Dependent Claim
93 words
A process for preparing a compound of formula (I) in which Rl, R2, R3, X, g and h are as defined in claim 1 and Y is or or a pharmacologically acceptable salt thereof, which comprises subjecting a compound of formula (I) in which Rl, R2, R3, X, g and h are as defined in claim 1 and Y is hydrogen, to a Mannich reaction using respectively, and an appropriate amount of formaldehyde, R10 and Rll being as defined in claim 2, and if necessary converting the product to a pharmacologically acceptable salt.
Claim 9
Dependent Claim
99 words
A process for preparing a compound of formula (I) in which Rl, R2, X, g and h are as defined in claim 1, and R3 and Y are lower alkyl, lower alkenyl or cycloalkyl, or a pharmacologically acceptable salt thereof, which comprises reacting a compound of formula (I) in which Rl, R2, X , g and h are as defined above and R3 and Y are hydrogen, with a compound of formula in which R' is lower alkyl, lower alkenyl or cycloalkyl and Hal is a halogen atom and if necessary converting the product to a pharmacologically acceptable salt.
Claim 10
Dependent Claim
78 words
A process for preparing a compound of formula (I) in which Rl, R2, g and h are as defined in claim 1, X is -CHOH-, R3 is lower alkyl and Y is as defined in claim 2 or a pharmacologically acceptable.salt thereof, which comprises reducing a compound of formula (I) in which Rl, R2, R3, g, h and Y are as defined above and X is -CO-, and if necessary converting the product to a pharmacologically acceptable salt.
Claim 11
Dependent Claim
23 words
Use of the compounds produced in any of claims 1 to 9 in the preparation of a medicament for the treatment of arrhythmia.
References Cited (Backward Citations)
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