Claims
- 1. A compound of the formula wherein:R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR9, where R9 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, aryl or heteroaryl and R10 and R11 are each independently hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, or aryl;R2 and R3 are each independently selected from the group consisting of hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R2 and R3 together form a cycloalkyl or a cycloaryl moiety; R5 is hydrogen, hydroxyl, oxo, or together with R6 and the carbons to which they are attached form a cyclic carbonate; R6 is hydrogen, hydroxyl, OR12 where R12 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, or together with R5 and the carbons to which they are attached form a cyclic carbonate; and R8 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl.
- 2. The compound as in claim 1 whereinR is hydroxyl or methoxy; R1 is hydrogen or hydroxyl; R2 and R3 are each independently C1-5 alkyl, phenyl, or benzyl; R5 is hydrogen, hydroxyl, or oxo; R6 is hydrogen, hydroxyl, or C1-5 alkoxy; and R8 is C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, alkylaryl, alkenylaryl, or alkynylaryl.
- 3. A compound according to claim 1, whereinR is hydroxyl or methoxy; R1 is hydrogen or hydroxyl; R2 is methyl; R3 is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, secbutyl or tertbutyl; R5 is hydrogen, hydroxyl, or oxo; R6 is hydrogen, hydroxyl, or methoxy; and R8 is methyl, ethyl, vinyl, propyl, isobutyl, pentyl, prop-2-enyl, propargyl, but-3-enyl, 2-azidoethyl, 2-fluoroethyl, 2-chloroethyl, cyclohexyl, phenyl, or benzyl.
- 4. A compound according to claim 2, whereinR is methoxy; R1 is hydroxyl; R2 is methyl; R3 is ethyl or isopropyl; R5 and R6 are each hydroxyl; and R8 is ethyl.
- 5. A method of treating a subject suffering from impaired GI motility comprising administering to a subject in need thereof a composition comprising a compound according to claim 1.
- 6. A method according to claim 5, wherein the subject is a human suffering from gastroparesis, gastroesophageal reflux disease, anorexia, gall bladder stasis, postoperative paralytic ileus, scleroderma, intestinal pseudoobstruction, gastritis, emesis, or chronic constipation (colortic inertia).
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a continuation of U.S. application Ser. No. 09/788,314, filed Feb. 15, 2001, now U.S. Pat. No. 6,562,795 B2; which claims the benefit of U.S. Provisional Application No. 60/183,338, filed Feb. 18, 2000; the disclosures of which are incorporated herein by reference.
STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT
This invention was made with Government support under SBIR Grant No. 1R43 DK57380-01, awarded by the National Institute of Diabetes, Digestive and Kidney Diseases. The Government has certain rights in this invention.
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Number |
Date |
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Number |
Date |
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Parent |
09/788314 |
Feb 2001 |
US |
Child |
10/409429 |
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US |