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US4923863A Expired / Lapsed US ⏱️ 0.0 years remaining

Morpholine derivatives, pharmaceutical compositions and use

Assignee: Glaxo Group Ltd
•
Filing: 1989-06-06
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Granted: 1990-05-08
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Expires: 2009-06-06
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Abstract

Abstract Compounds are disclosed of formula (I): ##STR1## wherein R 1 and R 2 are the same or different and are C 1-6 alkyl or C 3-6 alkenyl; or --NR 1 R 2 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR 3 (where R 6 represents C 1-6 alkyl, OR 4 or --NHR 4 , and R 4 represents hydrogen, C 1-6 alkyl, aryl, ar(C 1-6 )alkyl) or ═NOR 5 (where R 5 represents C 1-6 alkyl); X represents a direct bond, --CH 2 -- or --CH 2 O--; Ar represents a substituted phenyl moiety; and physiologically acceptable salts thereof. The compounds are indicated as useful for the treatment of pain and cerebral ischaemia. Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.

Inventors

  • 👤 David I. C. Scopes
  • 👤 David E. Bays

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 04:49
CPC Classifications
C; C07; C07D; C07D265/00; C07D265/28; C07D265/30; A; A61; A61P; A61P25/00; A61P25/04; A61P9/00; A61P9/10

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 127 words
A compound of formula (I) ##STR9## wherein R 1 and R 2 are the same or different and are C 1-6 alkyl or C 3-6 alkenyl; or --NR 1 R 2 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR 3 (where R 6 represents C 1-6 alkyl, OR 4 or --NHR 4 , and R 4 represents hydrogen, C 1-6 alkyl, aryl, ar(C 1-6 )alkyl) or ═NOR 5 (where R 5 represents C 1-6 alkyl); X represents a direct bond, --CH 2 -- or --CH 2 O--; Ar represents a substituted phenyl moiety; and physiologically acceptable salts thereof.
Claim 2
Dependent Claim 127 words
A compound of formula (I) ##STR9## wherein R 1 and R 2 are the same or different and are C 1-6 alkyl or C 3-6 alkenyl; or --NR 1 R 2 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR 3 (where R 6 represents C 1-6 alkyl, OR 4 or --NHR 4 , and R 4 represents hydrogen, C 1-6 alkyl, aryl, ar(C 1-6 )alkyl) or ═NOR 5 (where R 5 represents C 1-6 alkyl); X represents a direct bond, --CH 2 -- or --CH 2 O--; Ar represents a substituted phenyl moiety; and physiologically acceptable salts thereof.
Claim 3
Dependent Claim 17 words
A compound according to claim 1 wherein --NR 1 R 2 represents a tetrahydropyridine or pyrrolidine ring.
Claim 4
Dependent Claim 15 words
A compound according to claim 2 wherein --NR 1 R 2 represents a pyrrolidine ring.
Claim 5
Dependent Claim 17 words
A compound according to claim 1 wherein X represents --CH 2 -- and Ar represents halosubstituted phenyl.
Claim 6
Dependent Claim 6 words
4-[(3,4-Dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)morpholine and its physiologically acceptable salts.
Claim 7
Dependent Claim 6 words
4-[(3,4-Dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)morpholine and its physiologically acceptable salts.
Claim 8
Dependent Claim 32 words
A pharmaceutical composition which comprises an effective amount of a compound of formula (I) as defined in claim 1 or a physiologically acceptable salt thereof together with a pharmaceutically acceptable carrier thereof.
Claim 9
Dependent Claim 35 words
A method of treating a human suffering from pain or cerebral ischaemia which comprises administering an effective amount of a compound of formula (I) as defined in claim 1 or a physiologically acceptable salt thereof.

References Cited (Backward Citations)

US2428239A Cited
US3586713A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1993-05-07 1993-11-06 1994-05-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1997-05-07 1997-11-06 1998-05-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2001-05-07 2001-11-06 2002-05-08 $7700.00 Window Closed / Lapsed

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