Patent EP0508792A1 successfully refreshed from Google Patents.
EP0508792A1
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EP
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Anti-tumor and anti-psoriatic agents
Assignee: Merck Sharp & Dohme LLC
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Filing: 1992-04-09
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Granted: —
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Expires: 2012-04-09
Abstract
Abstract Compounds of formula: or pharmaceutically acceptable salts thereof wherein X, Y, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 , are as set forth herein are described. These compounds are useful as anti-tumor agents. These compounds are also useful as anti-psoriatic agents.
Inventors
- 👤 Stuart W. Mccombie
- 👤 Bandarpalle B. Shankar
- 👤 Michael P. Kirkup
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-29 18:19
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/22; A; A61; A61P; A61P17/00; A61P35/00; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/044
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
463 words
A compound of the formula or a pharmaceutically acceptable salt thereof, wherein X is O or S; Y is O, NH, (H,H), (H,OH) or S; with the proviso that when X is S, Y is not NH, (H,H) or (H,OH); R 1 , R 2 , R 3 and R 4 may be the same or different and each independently is H, C 1 -C 7 alkyl, C 1 -C 7 substituted alkyl, -CHO, CN, -CON(R 8 ,R 9 ), -COOR 7 , -CH=NOR 8 , -CH=NNHCONH 2 , F, Cl, Br, OH, N 3 , -OC 1 -C 7 alkyl, -OC 1 -C 7 substituted alkyl, -OCOR 9 , SH, S(C 1 -C 7 )alkyl, S(C 1 -C 7 )substituted alkyl, SCOR₁₀, S(O) n R₁₁, NH 2 , N(R₁₂,R₁₃), and N( acyl, R₁₄); R 1 , and R 2 taken together may be O, NOH, NOR 8 , =CH 2 or NNHCONH 2 ; R 3 , and R 4 taken together may be O, NOH, NOR 8 , =CH 2 or NNHCONH 2 ; R 1 and R 4 taken together may be a carbon-carbon bond with the proviso that R 2 and R 3 may be the same or different and each independently is selected from the group consisting of H, C 1 -C 7 alkyl, C 1 -C 7 substituted alkyl, -CHO, CN, -COOR 7 , -CON(R 8 , R 9 ), -CH=NOR₁₀, and -CHN=NNHCONH 2 ; R 5 and R 6 are independently H, C 1 -C 7 alkyl, C 1 -C 7 substituted alkyl, F, Cl, Br, OH, N 3 , - OC 1 -C 7 alkyl, - OC 1 -C 7 substituted alkyl, -OCOR₁₅, SH, S(C 1 -C 7 )alkyl, S(C 1 -C 7 ) substituted alkyl, SCOR₁₆, S(O) n R₁₇, NH 2 , N(R₁₈,R₁₉), and N (acyl, R₂₀); R 7 , R 8 , R 9 , R₁₀, R₁₁, R₁₂, R₁₃, R₁₄, R₁₅, R₁₆, R₁₇, R₁₈, R₁₉, and R₂₀ may be the same or different and each independently is H alkyl or substituted alkyl; and n is 1 or 2; with the proviso that R 1 and R 2 may not both be directly attached to the 10-position via a heteroatom and R 3 and R 4 may not both be directly attached to the 11-position via a heteroatom ; and with the still further proviso that the total number of carbon atoms for those R 1 , R 2 , R 3 , and R 4 which are C 1 -C 7 alkyl may not exceed 14; and with the still further proviso that when X and Y are both O, then R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 cannot all be H.
Claim 2
Dependent Claim
13 words
A compound according to claim 1, wherein X and Y are both O.
Claim 3
Dependent Claim
62 words
A compound according to claim 1, wherein one of R 1 , R 2 , R 3 or R 4 is selected from the group consisting of OH, N 3 , OC 1 -C 7 alkyl, OC 1 -C 7 substituted alkyl, OCOR 9 , SH, S(C 1 -C 7 )alkyl, S(O) n R₁₁, NH 2 , N(R₁₂,R₁₃), and N (acyl, R₁₄).
Claim 4
Dependent Claim
56 words
A compound according to claim 1, wherein R 1 is C 1 -C 3 alkyl substituted with OH, and R 2 is H; or wherein R 2 is C 1 -C 3 alkyl substituted with OH, and R 1 is H; and R 3 , R 4 , R 5 , and R 6 are H.
Claim 5
Dependent Claim
19 words
A compound according to claim 1, selected from the group consisting of and or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
12 words
The compound according to claim 1 or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
23 words
A pharmaceutical composition comprising a therapeutically effective amount of a compound as defined in claim 1 in combination with a pharmaceutically acceptable carrier.
Claim 8
Dependent Claim
30 words
A method for treating tumors in a mammal which comprises administering to a mammal in need of such treatment an anti-tumor effective amount of a compound according to claim 1.
Claim 9
Dependent Claim
30 words
A method for treating psoriasis in a mammal which comprises administering to a mammal in need of such treatment an anti-psoriatic effective amount of a compound according to claim 1.
Claim 10
Dependent Claim
29 words
A method for preparing a compound of formula I according to claim 1 which comprises carrying out the processes of Formula Schemes 2, 3, 4, 5, 6, or 7.
References Cited (Backward Citations)
EP0303697A1
Cited
EP0410389A1
Cited
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