Oligomer-bis-chromonyl compound conjugates
View Patent ↗The invention provides oligomer-bis-chromonyl compound conjugates. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
1. A compound according to the following formula:
wherein:
R 1 is hydrogen, hydroxy, halo, lower alkyl, or lower alkoxy;
R 2 is hydrogen, hydroxy, halo, lower alkyl, or lower alkoxy;
R 3 is hydrogen, hydroxy, halo, lower alkyl, or lower alkoxy;
R 4 is hydrogen, hydroxy, halo, lower alkyl, or lower alkoxy;
R 5 is hydrogen, hydroxy, halo, lower alkyl, or lower alkoxy;
R 6 is hydrogen, hydroxy, halo, lower alkyl, or lower alkoxy;
L is
—CH 2 —CH═CH—CH 2 —, —CH 2 —CH(OH)—CH 2 —, —CH 2 —CH(OH)—CH 2 —O—CH 2 —CH(OH)—CH 2 —, —CH 2 —O—CH 2 —, —CH 2 —CH 2 —CH(CH 3 )—CH 2 —CH 2 —, —CH 2 —C(O)—CH 2 —, or —CH 2 —CH 2 —O—CH 2 —CH 2 —;
(a) is zero or one, wherein when (a) is zero, —X 1 -POLY 1 is —COOH;
(b) is one;
X 1 , when present, is —C(O)O—, —OC(O)—, —NH—C(O)O—, —OC(O)—NH—, or a carbonyl;
X 2 is —C(O)O—, —OC(O)—, —NH—C(O)O—, —OC(O)—NH—, or a carbonyl;
POLY 1 is a poly(ethylene oxide) oligomer having a number of repeating monomers in the range of from 1 to 30; and
POLY 2 is a poly(ethylene oxide) oligomer having a number of repeating monomers in the range of from 1 to 30.
2. The compound of claim 1 , wherein L is —CH 2 —CH(OH)—CH 2 —.
3. The compound of claim 1 , having the formula:
wherein (n) is an integer from 2 to 30.
4. The compound of claim 1 , wherein each poly(ethylene oxide) oligomer has a number of repeating monomers in the range of from 1 to 10.
5. The compound of claim 1 , wherein each poly(ethylene oxide) includes an alkoxy or hydroxy end-capping moiety.
6. A composition comprising: (i) a compound of claim 1 ; and (ii) a pharmaceutically acceptable excipient.
7. A composition of matter comprising a compound of claim 1 present in a dosage form.
8. A method of treating asthma, allergic rhinitis, allergic conjunctivitis, mastocytosis, dermatographic urticaria, or ulcerative colitis comprising administering to a subject a compound of claim 1 .