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EP0050460A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Tridecyloxy- or tetradecyloxy-propane derivatives, and their use

Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1981-10-12
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Granted: —
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Expires: 2001-10-12
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Abstract

Abstract Tridecyloxy- or tetradecyloxy-propane derivatives of the formula: wherein R 1 is tridecyl or tetradecyl, R 2 is hydrogen or -OCH 3 , and R 3 , R 4 and R 5 independently represent hydrogen or C 1-3 alkyl, or represents cyclic ammonio, and their salts, have inhibitory activity to multiplication of tumor cells and antimicrobial activity.

Inventors

  • 👤 Motoo Hozumi
  • 👤 Susumu Tsushima
  • 👤 Yoshio Yoshioka

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-09 18:52
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/06; C07F9/08; C07F9/09; C07F9/10; A; A01; A01N; A01N57/00; A01N57/10; A01N57/12; A01N57/16; A61; A61P; A61P35/00; C07C; C07C43/00; C07C43/02; C07C43/03; C07C43/04; C07C43/13; C07F9/091; C07F9/547; C07F9/553; C07F9/576; C07F9/58

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 66 words
A pharmaceutical composition which comprises, as an active ingredient, an effective amount of a compound of the formula: wherein R 1 is tridecyl or tetradecyl, R 2 is hydrogen or -OCH 3 , and R 3 , R 4 and R 5 independently represent hydrogen or C 1-3 alkyl, or represents cyclic ammonio, or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable carrier.
Claim 2
Dependent Claim 66 words
A pharmaceutical composition which comprises, as an active ingredient, an effective amount of a compound of the formula: wherein R 1 is tridecyl or tetradecyl, R 2 is hydrogen or -OCH 3 , and R 3 , R 4 and R 5 independently represent hydrogen or C 1-3 alkyl, or represents cyclic ammonio, or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable carrier.
Claim 3
Dependent Claim 60 words
A compound of the formula: wherein R 1 is tridecyl or tetradecyl, R 2 is hydrogen or -OCH 3 , and R 3 , R 4 and R independently represent hydrogen or C 1-3 alkyl, or represents cyclic ammonio, provided that when R 1 is tetradecyl and R 2 is hydrogen, represents cyclic ammonio, or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim 60 words
A compound of the formula: wherein R 1 is tridecyl or tetradecyl, R 2 is hydrogen or -OCH 3 , and R 3 , R 4 and R independently represent hydrogen or C 1-3 alkyl, or represents cyclic ammonio, provided that when R 1 is tetradecyl and R 2 is hydrogen, represents cyclic ammonio, or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim 11 words
A compound according to Claim 2, wherein R 1 is tridecyl.
Claim 6
Dependent Claim 18 words
A compound according to Claim 2, wherein R 1 is tetradecyl and R 2 is -OCH 3 .
Claim 7
Dependent Claim 10 words
A compound according to Claim 2, wherein represents cyclic ammonio.
Claim 8
Dependent Claim 14 words
A compound according to Claim 5, wherein cyclic ammonio is pyridinio, oxazolio or thiazolio.
Claim 9
Dependent Claim 11 words
The compound according to Claim 2, which is (3-tetradecyloxy-2-methoxy)propyl 2-trimethylammonioethyl phosphate.
Claim 10
Dependent Claim 11 words
The compound according to Claim 2, which is (3-tridecyloxy-2-methoxy)propyl 2-trimethylammonioethyl phosphate.
Claim 11
Dependent Claim 11 words
The compound according to Claim 2, which is (3-tetradecyloxy-2-methoxy)propyl 2-pyridinioethyl phosphate.
Claim 12
Dependent Claim 11 words
The compound according to Claim 2, which is (3-tridecyloxy-2-methoxy)propyl 2-pyridinioethyl phosphate.
Claim 13
Dependent Claim 29 words
A composition as claimed in Claim 1 or a compound as claimed in any one of claims 2 to 10 for use in therapeutical treatment of a warm-blooded animal.
Claim 14
Dependent Claim 185 words
A process for producing a compound or its pharmaceutically acceptable salt as claimed in Claim 2 to 10, which comprises a) reacting a compound of the formula: wherein R 1 and R 2 are as defined in Claim 2 and Y is halogen, with a compound of the formula: wherein all the symbols are as defined in Claim 2 or represents cyclic amine which corresponds to cyclic ammonio as defined in Claim 2, or b) reacting a compound of the formula: wherein R 1 and R 2 are as defined in Claim 2, with a compound of the formula: wherein X is halogen, one of R 6 and R 7 corresponds to R 3 as defined in Claim 2 and another of R 6 and R 7 is a protective group for amino, or hydrolyzing the resulting compound, and then subjecting the hydrolyzed compound to a reaction for removal of the protective group to provide a compound as claimed in Claim 2 wherein R 4 and R 5 are hydrogen, and c) if desired, converting the thus obtained compound into a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim 22 words
A compound as defined in Claim 1, or a pharmaceutically acceptable salt thereof, for use in therapeutical treatment of a warm-blooded animal.

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