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Patent 4025558
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Document Number
US Patent 4025558
Issued Date
May 24, 1977
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Abstract
This invention relates to novel benzospiran derivatives embraced by the formula ##STR1## wherein the sum of A and B is at least the integer 2; A is selected from the group consisting of --(CH.sub.2)--.sub.n wherein n is 1 through 5 and --(C.sub.n H.sub.2n -.sub.2 XY)-- wherein X is selected from the group consisting of hydroxy, acetoxy, amino and acetamido and Y is hydrogen, and X when taken together with Y is selected from the group consisting of =O and =CR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; B is absent or --(CH.sub.2)--.sub.n wherein n is 1 through 3; R.sup.1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R.sup.2 is selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, ##STR2## WHEREIN N IS 2 THROUGH 5 AND Ar is phenyl having zero through three substituents selected from the group consisting of lower alkyl of 1 through 3 carbon atoms, lower alkoxy of 1 through 3 carbon atoms, bromine, chlorine and fluorine; R.sup.1 and R.sup.2 taken together with --N< is a saturated heterocyclic amino radical selected from the group consisting of unsubstituted and substituted pyrrolidino, piperidino, and hexamethylenimino; Z is selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, lower alkoxy of 1 through 3 carbon atoms, nitro, amino, monoalkylamino of 1 through 3 carbon atoms, acylamido of 1 through 4 carbon atoms, bromine, chlorine and fluorine; and a pharmacologically acceptable acid addition salt thereof. It also relates to intermediates and processes for the preparation of the aforesaid novel compounds (1) and novel derivatives thereof. The administration to humans and animals of the novel compounds (1) depresses their central nervous systems and lowers their blood pressures.
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Organic compounds - US Patent 4025558 Drawing
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Number of Claims:
10
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Owner
The Upjohn Company (Kalamazoo, MI)
Published
May 24, 1977
Application Number
05/623,171
Filed
October 16, 1975
US Classification
564/345   540/543 546/15 549/333 549/342 549/347 552/1 560/126 560/250 560/255 560/28 560/45 560/59 562/459 564/342 564/344 568/306 568/309 568/314 568/327 568/428
Int'l Classification
C07C   49/755   (20060101)   C07C   49/697   (20060101)   C07C   49/747   (20060101)   C07C   49/675   (20060101)   C07C   49/00   (20060101)   C07C   49/683   (20060101)   C07C   59/54   (20060101)   C07C   57/50   (20060101)   C07C   57/00   (20060101)   C07C   59/00   (20060101)   C07C   205/45   (20060101)   C07C   205/00   (20060101)   C07D   319/08   (20060101)   C07D   317/00   (20060101)   C07D   319/00   (20060101)   C07C   59/86   (20060101)   C07D   317/22   (20060101)   C07D   295/135   (20060101)   C07D   295/096   (20060101)   C07D   295/00   (20060101)   C07D   295/033   (20060101)  
Examiner
Parent Case
This is a division of application Ser. No. 460,449, filed Apr. 12, 1974 and now U.S. Pat. No. 3,932,425.
USPTO Field of Search
260/57.5CA   260/57.5C   260/501.18   260/501.19  
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