Claims
- 1. A method of facilitating the placement of diagnostic and therapeutic instrumentation into the proximal small intestine of a human or other mammal comprising administering to such human or mammal a compound of the formula: ##STR7## or a pharmaceutically acceptable salt thereof, wherein the dotted line is an optional second C8--to--C9 bond;
- (i) one of R.sup.1 and R.sup.11 is hydrogen and the other is methyl, or (ii) R.sup.11 is methyl and R.sup.1 is hydroxy or, taken together with R.sup.5 and the carbons to which they are attached, forms a cyclic carbonate;
- R.sup.2 and R.sup.3 are independently selected from the group consisting of:
- hydrogen,
- loweralkyl,
- halo-substituted loweralkyl,
- cyano-substituted loweralkyl,
- hydroxy-substituted loweralkyl,
- amino-substituted loweralkyl,
- loweralkenyl,
- loweralkynyl,
- lower cycloalkyl,
- lower cycloalkylmethyl, and
- benzyl;
- or, taken together, R.sup.2 and R.sup.3 are --(CH.sub.2)n-- where n is two to six, so as to form, with the nitrogen to which they are attached, a 3- to 7-membered heterocycle;
- R.sup.4 is absent or is selected from the group consisting of:
- loweralkyl,
- loweralkenyl,
- loweralkynyl, and
- benzyl,
- and, when present, is accompanied by a pharmaceutically acceptable counterion so as to form a quaternary ammonium salt;
- R.sup.5 is selected from the group consisting of hydroxy and --OR.sup.9, wherein R.sup.9 is selected from the group consisting of:
- lower alkyl,
- loweralkanoyl, and
- --S(O).sub.2 CH.sub.3 ; or, taken together with R.sup.1 and the carbons to which they are attached, forms a cyclic carbonate;
- R.sup.6 is selected from the group consisting of hydrogen and loweralkyl; and
- R.sup.7 is selected from the group consisting of hydrogen and methyl; in an amount effective for enhancing gastrointestinal motility.
- 2. The method according to claim 1, wherein R.sup.1 in the compound is hydrogen.
- 3. The method according to claim 1, wherein at least one of R.sup.2 and R.sup.3 in the compound is selected from the group consisting of (i) hydrogen and (ii) loweralkyl other than methyl.
- 4. The method according to claim 2 wherein R.sup.4 in the compound is absent.
- 5. The method according to claim 2 wherein R.sup.5 in the compound is hydroxy.
- 6. The method according to claim 2 wherein R.sup.6 in the compound is hydrogen.
- 7. The method according to claim 2 wherein R.sup.7 in the compound is methyl.
- 8. The method according to claim 2 wherein R.sup.5 in the compound is hydroxy, R.sup.6 is hydrogen, and R.sup.7 is methyl.
- 9. The method according to claim 1, wherein the compound is selected from the group consisting of:
- 8,9-anhydro-4"-deoxyerythromycin B-6,9-hemiketal;
- 8,9-anhydro-4"-deoxy-3'-N-desmethylerythromycin A-6,9-hemiketal;
- 8,9-anhydro-4"-deoxy-3'-N-desmethyl-3'-N-ethylerythromycin A-6,9-hemiketal;
- 8,9-anhydro-4"-deoxy-3'-N-desmethylerythromycin B-6,9-hemiketal;
- 8,9-anhydro-4"-deoxy-3'-N-desmethyl-3'-N-ethylerythromycin B-6,9-hemiketal;
- 9-deoxo-4",6-dideoxy-8-epi-6,9 epoxyerythromycin A;
- 9-deoxo-4",6-dideoxy-6,9 epoxyerythromycin A;
- 9-deoxo-3'-N-desmethyl-4",6-dideoxy-8-epi-6,9-epoxyerythromycin A;
- 9-deoxo-3'-N-desmethyl-4",6-dideoxy-6,9-epoxyerythromycin A;
- 9-deoxo-3'-N-desmethyl-4",6-dideoxy-6,9-epoxy-3'-N-ethylerythromycin A; and
- 9-deoxo-4",6-dideoxy-8-epi-6,9-epoxyerythromycin B.
Parent Case Info
This application is a divisional of U.S. Ser. No. 08/284,730, filed Aug. 2, 1994, now U.S. Pat. No. 5,578,579, which is a continuation of U.S. Ser. No. 07/944,150, filed on Sep. 11, 1992, now abandoned, which is a continuation-in-part of U.S. Ser. No. 07/823,490, filed Jan. 21, 1992, now abandoned.
US Referenced Citations (6)
Foreign Referenced Citations (3)
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213 617 |
Mar 1987 |
EPX |
215 355 |
Mar 1987 |
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349 100 |
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Non-Patent Literature Citations (1)
Entry |
Sunazuka, et al., Chem. Pharm. Bulletin, 37(10): 2701-2709 (1989). |
Divisions (1)
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Date |
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284730 |
Aug 1994 |
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Continuations (1)
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944150 |
Sep 1992 |
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Continuation in Parts (1)
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823490 |
Jan 1992 |
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