Process for the preparation of optically-active carbazole derivatives, new R- and S-carbazole derivatives and pharmaceutical compositions containing these compounds
Patent 5071868 Issued on December 10, 1991. Estimated Expiration Date: 
January 28, 2011. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
January 28, 2011. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent ReferencesCarbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions Use of D,L-and D-carazolol as anti-glaucoma agent Patent #: 4760085 InventorAssigneeApplicationNo. 631641 filed on 01/28/1991US Classes:514/411, Tricyclo ring system having the five-membered hetero ring as one of the cyclos514/302, Ring oxygen in the bicyclo ring system514/339, Ring nitrogen in the polycyclo ring system514/913, Glaucoma514/929, VASODILATOR546/115, Ring oxygen in the bicyclo ring system546/116, Acyclic chalcogen bonded directly to ring carbon of the bicyclo ring system546/276.7, Polycyclo ring system having the five-membered hetero ring as one of the cyclos548/444Chalcogen or nitrogen attached indirectly to the tricyclo ring system by acyclic nonionic bondingExaminersPrimary: Raymond, Richard L.Assistant: O'Sullivan, P. Attorney, Agent or FirmForeign Patent References
International ClassesA61K 031/40C07D 209/82 C07D 401/12 C07D 491/056 Foreign Application Priority Data1983-05-26 DEAbstractA process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbozole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.Field of SearchChalcogen or nitrogen attached indirectly to the tricyclo ring system by acyclic nonionic bondingRing oxygen in the bicyclo ring system Acyclic chalcogen bonded directly to ring carbon of the bicyclo ring system Ring oxygen in the bicyclo ring system Ring nitrogen in the polycyclo ring system Tricyclo ring system having the five-membered hetero ring as one of the cyclos VASODILATOR Glaucoma |
| ||||||||||||||
