10,10-dialkyl prostanoic acid derivatives as agents for...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S443000, C514S530000, C514S573000, C548S253000, C549S053000

Reexamination Certificate

active

06875787

ABSTRACT:
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;wherein the dashed line indicates the presence or absence of a bond, the hatched wedge indicates the α (down) configuration, and the solid triangle indicates the β (up) configuration;B is a single, double, or triple covalent bond;n is 0-6;X is CH2, S or O;Y is any pharmaceutically acceptable salt of CO2H, or CO2R, CONR2, NHCH2CH2OH, N(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, orR is H, C1-6alkyl or C2-6alkenyl;R2and R3are C1-6linear alkyl which may be the same or different, and may be bonded to each other such that they form a ring incorporating the carbon to which they are commonly attached;R4is hydrogen, R, C(═O)R, or any group that is easily removed under physiological conditions such that R4is effectively hydrogen;R5is hydrogen or R;R6isiv) hydrogen;v) a linear or branched hydrocarbon containing between 1 and 8 carbon atoms, which may contain one or more double or triple bonds, or oxygen or halogen derivatives of said hydrocarbon, wherein 1-3 carbon or hydrogen atoms may be substituted by O or a halogen; orvi) aryloxy, heteroaryloxy, C3-8cycloalkyloxy, C3-8cycloalkyl, C6-10aryl or C3-10heteroaryl, wherein one or more carbons is substituted with N, O, or S; and which may contain one or more substituents selected from the group consisting of halogen, trihalomethyl, cyano, nitro, amino, hydroxy, C6-10aryl, C3-10heteroaryl, aryloxy, heteroaryloxy, C1-6alkyl, OR, SR, and SO2R.Some of the compounds of the present invention and some of their methods of preparation are also novel an nonobvious.

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Bito, L.Z.,Prostaglandins old concepts and new perspectives, Arch Ophthalmol—vol. 105, Aug. 1987, pp. 1036-10-39.
Bito, L.Z.,Prostaglandins and related compounds as potential ocular therapeutic agents, Chpt. 18, Biological Protection with Prostaglandins, vol. 1, CRC Press, Inc., M.M. Cohen, Editor.
Bito, L.Z.,Prostaglandins, other eicosanoids, and their derivatives as potential antiglaucoma agents, Chap. 20, pp. 477-505, Glaucoma: Applied pharmacology in medical treatment , Grune & Stratton, Inc., S.Drance, et al., Editors.
Brooks, D.W., et al.,Asymmetric Microbial Reduction of prochiral 2,2-disubstituted cycloalkanediones, J. Org. Chem. 1987, 52, 3223-3232.
Nilsson, S., et al.PGF2,Increases uveoscieral outflow, Invest Ophthalmol Vis Sci 1987; 28(3 Suppl) :284.

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