1,2-diamino-4,5-dimethoxycyclohexyl amide analgesic compounds
First Claim
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1. A compound having structural Formula I ##STR10## wherein the methoxy groups attached to the cyclohexane moiety are cis to one another and the two nitrogen atoms attached to the cyclohexane moiety are trans to one another;
- X is a direct bond, or is --O-- or --S--;
R1 and R2, together with the nitrogen atom to which they are attached form a pyrrolidinyl ringA is selected from ##STR11## phenyl;
phenyl substituted with from one to four halogen atoms;
phenyl substituted with one or two alkyl groups of from one to four carbon atoms;
phenyl substituted with one or two alkoxy groups of from one to four carbon atoms;
orphenyl substituted with one or two alkyl groups of from one to four carbon atoms and one or two halogen atoms;
ora pharmaceutically acceptable acid addition salt thereof.
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Abstract
Certain 1,2-diamino-4,5-dimethoxycyclohexane amide derivatives have analgesic activity, and bind selectively to the kappa opioid receptor site. Pharmaceutical compositions containing these compounds, and a method of alleviating pain in mammals are also disclosed.
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Citations
16 Claims
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1. A compound having structural Formula I ##STR10## wherein the methoxy groups attached to the cyclohexane moiety are cis to one another and the two nitrogen atoms attached to the cyclohexane moiety are trans to one another;
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X is a direct bond, or is --O-- or --S--; R1 and R2, together with the nitrogen atom to which they are attached form a pyrrolidinyl ring A is selected from ##STR11## phenyl;
phenyl substituted with from one to four halogen atoms;phenyl substituted with one or two alkyl groups of from one to four carbon atoms; phenyl substituted with one or two alkoxy groups of from one to four carbon atoms;
orphenyl substituted with one or two alkyl groups of from one to four carbon atoms and one or two halogen atoms;
ora pharmaceutically acceptable acid addition salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
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Specification
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Current AssigneeWarner-Lambert Company (Pfizer Inc.)
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Original AssigneeWarner-Lambert Company (Pfizer Inc.)
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InventorsHorwell, David C., Johnson, Stephen J.
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Primary Examiner(s)Brust, Joseph Paul
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Application NumberUS07/161,563Time in Patent Office537 DaysField of Search548/525, 548/528, 548/578, 514/422, 514/429US Class Current514/422CPC Class CodesC07D 295/135 with the ring nitrogen atom...C07D 307/79 with only hydrogen atoms, h...C07D 333/54 with only hydrogen atoms, h...
