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US 6,441,035 B2Granted
Heteroatom-interrupted analogs of 15-hydroxyeicosatetraenoic acid and methods of use
AssigneeAlcon Universal Ltd.
InventorsRaymond E. Conrow, Peter G. Klimko
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Abstract
Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.
Claims15
A composition for the treatment of dry eye and other disorders requiring the wetting of the eye comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of one or more compounds of the following formula I:
- wherein:
- R1 is CO2R, wherein R is H or CO2R forms an ophthalmically acceptable salt or an ophthalmically acceptable ester;
- K is C3-C6 alkyl, alkenyl, alkynyl or alkenyl group;
- A and X are the same or different and are a direct bond, CH2, NR7, O or S, with the proviso that at least one of A and X is NR7;
- B is H, or BB together comprises a double bonded O, S or NR8, with the proviso that BB comprises a double bonded O, S, or NR8 when A and X are the same or different and are NR7, O or S;
- wherein:
- NR7 and NR8 are the same or different and comprise a functionally modified amino group;
- p is 0 or 1;
- D—E and G—H are the same or different and are CH═CH or C≡C;
- and
- Y is
8 more elements
A method for the treatment of dry eye and other disorders requiring the wetting of the eye which comprises administering to a mammal a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of
- one or more compounds of the following formula I:
- wherein:
- R1 is CO2R, CONR2R3, CH2OR4, CH2NR5R6, CH2N3, CH2-Hal, CH2NO2, CH2SR20, COSR21 or 2,3,4,5-tetrazol-1-yl, wherein:
- R is H or CO2R forms a pharmaceutically acceptable salt or a pharmaceutically acceptable ester;
- NR2R3 and NR5R6 are the same or different and comprise a free or functionally modified amino group;
- OR4 comprises a free or functionally modified hydroxy group;
- Hal is F, Cl, Br or I;
- SR20 comprises a free or functionally modified thiol group;
- R21 is H, or COSR21 forms a pharmaceutically acceptable salt or a pharmaceutically acceptable thioester;
- K is C2-C8 alkyl, alkenyl, or alkynyl or a C3-C8 alkenyl group;
- A and X are the same or different and are a direct bond, CH2, NR7, O or S, with the proviso that at least one of A and X is NR7;
- B is H, or BB together comprises a double bonded O, S or NR8, with the proviso that BB comprises a double bonded O, S or NR8 when A and X are the same or different and are NR7 O or S;
- wherein:
- NR7 and NR8 are the same or different and comprise a functionally modified amino group;
- p is 0 or 1;
- D—E and G—H are the same or different and are CH2CH2, CH═CH or C≡C;
- and
- Y is C(O) or Y is
- wherein R9O constitutes a free or functionally modified hydroxy group.
16 more elements
A compound of formula I:
- wherein:
- R1 is CO2R, wherein R is H or CO2R forms an ophthalmically acceptable salt or an ophthalmically acceptable ester;
- K is C3-C6 alkyl, alkenyl, alkynyl or alkenyl group;
- A and X are the same or different and are a direct bond, CH2, NR7, O or S, with the proviso that at least one of A and X is NR7;
- B is H, or BB together comprises a double bonded O, S or NR8, with the proviso that BB comprises a double bonded O, S, or NR8 when A and X are the same or different and are NR7, O or S;
- wherein:
- NR7 and NR8 are the same or different and comprise a functionally modified amino group;
- p is 0 or 1;
- D—E and G—H are the same or different and are CH═CH or C≡C;
- and
- Y is
8 more elements
Dependencies are inferred from the claim text.