Claims
- 1. A product prepared by the treatment of a compound of the formula ##STR26## and its steroisomers, enantiomers, diasteroisomers and racemic mixtures with an amine of the formula H.sub.2 N-Z; where:
- R.sub.1 is hydrogen, an amino or alkylamino optionally substituted with a protecting group halo or haloalkyl;
- R.sub.2 is hydrogen, halo, sulfamyl, mono- and di-alkylsulfamyl or haloalkyl;
- R' and R" are hydrogen or alkyl; and
- Z is: ##STR27## and its racemic mixtures and stereospecific isomers.
- 2. A product according to claim 1 of the formula ##STR28##
- 3. A product according to claim 2 which further includes removal of the protecting group on R.sub.1 to form an amino or alkylamino.
- 4. A product according to claim 3 where R.sub.2 is chloro, R.sub.1 is amino and R' and R" are hydrogen.
- 5. A product according to claim 2 where R.sub.2 is chloro and R.sub.1, R' and R" are hydrogen.
- 6. A compound of the formula: ##STR29## where: R is NH-Z;
- R.sub.1 is hydrogen, an amino or alkylamino optionally substituted with a protecting group, halo or haloalkyl;
- R.sub.2 is hydrogen, halo, sulfamyl, mono- and di-alkylsulfamyl optionally substituted with a protecting group or haloalkyl;
- R' and R" are hydrogen or alkyl;
- vicinal R' and/or R" groups may form a C.dbd.C double bond; and
- Z is ##STR30## and its stereoisomers, enantiomers, diastereoisomers and racemic mixtures; or pharmaceutically acceptable salts thereof.
- 7. A compound according to claim 6 where: ##STR31## Z is
- 8. A compound according to claim 7 which is 10-[N-(1-azabicyclo[2.2.2.]-octan-3-yl)carboxamido-8-chloro-cis-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocine.
- 9. A compound according to claim 7 which is 10-[N-(1-azabicyclo[2.2.2.]-octan-3(S)-yl)carboxamido]-8-chloro-2(S),6(R)-methano-2H-3,4,5,6-tetrahydro-1-benzoxocine.
- 10. A compound according to claim 7 which is 10-[N-(1-azabicyclo[2.2.2.]-octan-3(S)-yl)carboxamido]-8-chloro-2(R),6(S)-methano-2H-3,4,5,6-tetrahydro-1-benzoxocine.
- 11. A method for the treatment of gastric disorders in humans and mammals suffering from such disorders comprising administering thereto an effective amount of a compound of claim 6.
- 12. A method for the treatment of emesis in humans and mammals in need of such treatment comprising administering thereto an effective amount of a compound of claim 6.
- 13. A pharmaceutical composition for the treatment of gastric disorders and/or emesis in humans and mammals wherein the active ingredient is an effective amount of a compound of claim 6 in admixture with a pharmaceutical carrier.
- 14. A method for the treatment of gastric disorders in humans and mammals suffering from such disorders comprising administering thereto an effective amount of a compound of claim 7.
- 15. A method for the treatment of emesis in humans and mammals in need of such treatment comprising administering thereto an effective amount of a compound of claim 7.
- 16. A pharmaceutical composition for the treatment of gastric disorders and/or emesis in humans and mammals wherein the active ingredient is an effective amount of a compound of claim 7 in admixture with a pharmaceutical carrier.
Parent Case Info
This application is a continuation-in-part of application Ser. No. 07/620,241, now abandoned, which was filed Nov. 29, 1990, which is a continuation-in-part of application Ser. No. PCT/US89/01739 having an International Filing Date of Apr. 25, 1989, which designates the United States and which now has entered the U.S. National stage as application Ser. No. 07/582,890, now abandoned, which we filed Oct. 1, 1990, which, in turn, is a continuation-in-part of application Ser. No. 07/186,824, filed Apr. 27, 1988, which issued Sep. 5, 1989, as U.S. Pat. No. 4,863,921.
US Referenced Citations (8)
Continuation in Parts (3)
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Number |
Date |
Country |
Parent |
620241 |
Nov 1990 |
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Parent |
582890 |
Oct 1990 |
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Parent |
186824 |
Apr 1988 |
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