Substituted isoquinolines as ultra short acting neuromuscular blockers
AssigneesGlaxo Wellcome Inc., Cornell Research Foundation, Inc.
InventorsEric Cleveland Bigham, Grady Evan Boswell, John Joseph Savarese, Roy Archibald Swaringen, Jr., Sanjay Shashikant Patel, Eric Eugene Boros, Robert Anthony Mook, Jr., Vincente Samano
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Abstract
Ultrashort acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein: X is a halogen; h is from 1 to 2; Y is hydrogen or methoxy; Z1 and Z2 are methyl; W1 and W2 are carbon; and A is a pharmaceutically acceptable anion.
Claims7
A compound of Formula (I)
- wherein:
- X is halogen;
- h is from 1 to 2;
- Y is hydrogen or methoxy;
- Z1 and Z2 are methyl;
- W1 and W2 are carbon;
- and
- A is a pharmaceutically acceptable anion.
A compound of Formula (II)
- wherein:
- T is hydroxyl or halide;
- Y is hydrogen or methoxy;
- Z is methyl;
- W is carbon;
- X is halogen;
- n is 0 or 1;
- h is 1 or 2;
- and
- A is a pharmaceutically acceptable anion.
A process for the preparation of a compound of Formula (Ib)
- wherein
- h is 1;
- and
- X is halogen;
- Y is hydrogen or methoxy;
- Z1 and Z2 are methyl;
- W1 and W2 are carbon;
- and A is a pharmaceutically acceptable anion
- which comprises reacting a compound of Formula (Ia)
- wherein:
- h is 2;
- and
- X, Y, Z1, Z2, W1, W2, and A are as defined herein
- with a base in a polar aprotic solvent.
A process for the preparation of a compound of Formula (I)
- wherein:
- X is halogen;
- h is from 1 to 2;
- Y is hydrogen or methoxy;
- Z1 and Z2 are methyl;
- W1 and W2 are carbon;
- and
- A is a pharmaceutically acceptable anion
- comprising reacting a compound of Formula (II)
- wherein:
- T is hydrogen hydroxyl or halide;
- X is halogen;
- Y is hydrogen or methoxy;
- Z is methyl;
- W is carbon;
- n is 0 or 1;
- h is 1 or 2;
- and
- A is a pharmaceutically acceptable anion
- with a compound of Formula (III)
- wherein:
- Y is hydrogen or methoxy;
- Z is methyl;
- W is carbon;
- n is 0 or 1;and
- A is a pharmaceutically acceptable anion
- in an organic solvent.
Dependencies are inferred from the claim text.