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US 6,441,033 B1Granted
11β-fluoro 15β-hydroxy PGF2α analogs as FP receptor antagonists
AssigneeAlcon Manufacturing, Ltd.
InventorsNajam A. Sharif, Brenda W. Griffin
Life of this patent
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Abstract
Methods and compositions for the antagonism of FP receptor-mediated biological responses are disclosed.
Claims13
A method of inhibiting FP receptor-mediated response in a biological system where FP receptors are present, comprising introducing into the biological system a receptor antagonizing effective amount of a compound of formula I:
- wherein:
- R1=CO2R, CONR4R5, CH2OR6, or CH2NR7R8;
- where:
- R=H or cationic salt moiety, or CO2R=pharmaceutically acceptable ester moiety;
- R4, R5=same or different=H or alkyl;
- R6=H, acyl, or alkyl;
- R7, R8=same or different=H, acyl, or alkyl;
- with the proviso that if one of R7, R8=acyl, then the other=H or alkyl;
- n=0 or 2;
- R2, R3=same or different=H, alkyl, or acyl;
- =single or non-cumulated double bond, with the provisos that if a double bond is present between carbons 4 and 5, it is of the cis configuration;
- and that if a double bond is present between carbons 13 and 14, it is of the trans configuration;
- and
- X—Y=(CH2)pY1;
- where p=0-6;
- and
- wherein:
- W=CH2, O, S(O)q, NR10, CH2CH2, CH═CH, CH2O, CH2S(O)q, CH═N, or CH2NR9;
- where q=0-2, and R10=H, alkyl, or acyl;
- Z=H, alkyl, alkoxy, acyl, acyloxy, halo, trihalomethyl, amino, alkylamino, acylamino, or hydroxy;
- and
- =single or double bond.
19 more elements
A method of treating a mammal with an FP receptor related disorder selected from the group consisting of:
- ocular hyperemia, cystoid macular edema, iris hyperpigmentation, iris melanogenesis, acute and chronic inflammation, benign prostatic hypertrophy, uterine cramps, irritable bowel disease, cardiac arrythmias, epilepsy, excessive bone deposition, and premature labor, comprising administering to such mammal a therapeutically effective amount of a compound of formula I:.
- wherein:
- R1=CO2R, CONR4R5, CH2OR6, or CH2NR7R8;
- where:
- R=H or cationic salt moiety, or CO2R=pharmaceutically acceptable ester moiety;
- R4, R5=same or different=H or alkyl;
- R6=H, acyl, or alkyl;
- R7, R8=same or different=H, acyl, or alkyl;
- with the proviso that if one of R7, R8=acyl, then the other=H or alkyl;
- n=0 or 2;
- R2, R3=same or different=H, alkyl, or acyl;
- =single or non-cumulated double bond, with the provisos that if a double bond is present between carbons 4 and 5, it is of the cis configuration;
- and that if a double bond is present between carbons 13 and 14, it is of the trans configuration;
- X=(CH2)m or (CH2)mO, where m=1-6;
- and
- Y=phenyl, optionally substituted with alkyl, halo, trihalomethyl, alkoxy, acyl, acyloxy, amino, alkylamino, acylamino, or hydroxy;
- or
- X—Y=(CH2)pY1;
- where p=0-6;
- and
- wherein:
- W═CH2, O, S(O)q, NR10, CH2CH2, CH═CH, CH2O, CH2S(O)q, CH═N, or CH2NR9;
- where q=0-2, and R10=H, alkyl, or acyl;
- Z=H, alkyl, alkoxy, acyl, acyloxy, halo, trihalomethyl, amino, alkylamino, acylamino, or hydroxy;
- and
- =single or double bond.
23 more elements
Dependencies are inferred from the claim text.