Patent EP0335355A2 successfully refreshed from Google Patents.
EP0335355A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Bis-(hydroxymethyl) cyclobutyl purines and pyrimidines
Assignee: ER Squibb and Sons LLC
•
Filing: 1989-03-29
•
Granted: —
•
Expires: 2009-03-29
Abstract
Abstract Antiviral activity is exhibited by compounds having the formula and its pharmaceutically acceptable salts wherein R 1 is wherein R 2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; R 3 is fluoro, chloro, bromo, iodo, hydrogen, methyl, trifluoromethyl, ethyl, n-propyl, 2-fluoroethyl, 2-chloroethyl, or wherein R 4 is chloro, bromo, iodo, hydrogen methyl or trifluoromethyl; R s is alkyl; R 6 is hydrogen, alkyl, substituted alkyl, or aryl; and R 7 and R 8 are independently hydrogen,
Inventors
- 👤 William Allen Slusarchyk
- 👤 Robert Zahler
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-29 12:46
CPC Classifications
C; C07; C07D; C07D473/00; C07D473/02; C07D473/18; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/52; C07D239/54; A; A61; A61P; A61P31/00; A61P31/12; A61P31/20; A61P31/22; C07C; C07C35/00; C07C35/02; C07C35/04; C07D239/50; C07D239/545; C07D239/553; C07D487/00; C07D487/02; C07D487/04; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
74 words
A compound having the formula and its pharmaceutically acceptable salts wherein R 1 is wherein R 2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; R 3 is fluoro, chloro, bromo, iodo, hydrogen, methyl, trifluoromethyl, ethyl, n-propyl, 2-fluoroethyl, 2-chloroethyl, or wherein R 4 is chloro, bromo, iodo, hydrogen methyl or trifluoromethyl; Rs is alkyl; R 6 is hydrogen, alkyl, substituted alkyl, or aryl; and R 7 and R 8 are independently hydrogen,
Claim 2
Dependent Claim
74 words
A compound having the formula and its pharmaceutically acceptable salts wherein R 1 is wherein R 2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; R 3 is fluoro, chloro, bromo, iodo, hydrogen, methyl, trifluoromethyl, ethyl, n-propyl, 2-fluoroethyl, 2-chloroethyl, or wherein R 4 is chloro, bromo, iodo, hydrogen methyl or trifluoromethyl; Rs is alkyl; R 6 is hydrogen, alkyl, substituted alkyl, or aryl; and R 7 and R 8 are independently hydrogen,
Claim 3
Dependent Claim
10 words
A compound in accordance with claim 1 wherein R, is
Claim 4
Dependent Claim
17 words
A compound in accordance with claim 1 wherein R 7 and R 8 are independently hydrogen or
Claim 5
Dependent Claim
22 words
A compound in accordance with claim 1 wherein R 7 and R 8 are independently hydrogen or -P0 3 H 2 .
Claim 6
Dependent Claim
15 words
A compound in accordance with claim 1 wherein R 7 and R 8 are hydrogen.
Claim 7
Dependent Claim
11 words
A compound in accordance with claim 1 wherein R 1 is
Claim 8
Dependent Claim
9 words
A compound in accordance with claim 1, (1 α,2β,3α)-9-[2,3-bis(hydroxymethyl)cyclobutyl]-guanine.
Claim 9
Dependent Claim
9 words
A compound in accordance with claim 1, (1 α,2β,3β)-3-(6-amino-9H-purin-9-yl)-1,2-cyclobutanedimethanol.
Claim 10
Dependent Claim
9 words
A compound in accordance with claim 1, (1α,2β,3α)-1-[2,3-bis(hydroxymethyl)cyciobutyl]-5-methyl-2,4(1 H,3H)-pyrimidinedione.
Claim 11
Dependent Claim
9 words
A compound in accordance with claim 1, (1α,2β,3α)-4-amino-1-[2,3-bis(hydroxymethyl)cyctobutyl]-2-(1 H)-pyrimidinone.
Claim 12
Dependent Claim
9 words
A compound in accordance with claim 1, [1α(E),2β,3α]-1-[2,3-bis(hydroxymethyl)cyclobutyl]-5-(2-bromoethenyl)-2,4(1 H,3H)pyrimidinedione.
Claim 13
Dependent Claim
8 words
A compound in accordance with claim 1, (1α,2β,3α)-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-8-bromo-1,9,dihydro-6H-purin-6-one.
Claim 14
Dependent Claim
9 words
A compound in accordance with claim 1, (1α,2β,3α)-1-[2,3-bis(hydroxymethyl)cycfobutyl]-5-iodo-2,4-(1 H,3H)-pyrimidinedione.
Claim 15
Dependent Claim
8 words
A compound in accordance with claim 1, (1α,2β,3α)-5-amino-3-[2,3-bis(hydroxymethyl)cyclobutyl]-3,5-dihydro-7H-1,2,3-triazolo[4,5-d]-pyrimidin-7-one.
Claim 16
Dependent Claim
12 words
A compound of the formula wherein P is a hydroxy protecting group.
Claim 17
Dependent Claim
12 words
A compound of the formula wherein P is a hydroxy protecting group.
Claim 18
Dependent Claim
12 words
A compound of the formula wherein P is a hydroxy protecting group.
Claim 19
Dependent Claim
12 words
A compound of the formula wherein P is a hydroxy protecting group.
Claim 20
Dependent Claim
17 words
A compound of formula wherein X is a leaving group and P is a hydroxy protecting group.
Claim 21
Dependent Claim
17 words
A compound of formula wherein X is a leaving group and P is a hydroxy protecting group.
Claim 22
Dependent Claim
19 words
A compound in accordance with claim 17 wherein X is chloro, bromo, iodo, or an aryl or alkyl sulfonate.
Claim 23
Dependent Claim
122 words
A process for preparing compounds of the formula and its pharmaceutically acceptable salts wherein R 1 is wherein R 2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; R 3 is fluoro, chloro, bromo, iodo, hydrogen, methyl, trifluoromethyl, ethyl, n-propyl, 2-fluoroethyl, 2-chloroethyl, or wherein R 4 is chloro, bromo, iodo, hydrogen methyl or trifluoromethyl; Rs is alkyl; R 6 is hydrogen, alkyl, substituted alkyl, or aryl; and R 7 and R 8 are independently hydrogen, ; which comprises reacting a compound of the formula wherein P is a protecting group, X is a leaving group with a compound of the formula R 1 H which is optionally protected and removing the protecting groups to yield a compound of formula 1.
Claim 24
Dependent Claim
122 words
A process for preparing compounds of the formula and its pharmaceutically acceptable salts wherein R 1 is wherein R 2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; R 3 is fluoro, chloro, bromo, iodo, hydrogen, methyl, trifluoromethyl, ethyl, n-propyl, 2-fluoroethyl, 2-chloroethyl, or wherein R 4 is chloro, bromo, iodo, hydrogen methyl or trifluoromethyl; Rs is alkyl; R 6 is hydrogen, alkyl, substituted alkyl, or aryl; and R 7 and R 8 are independently hydrogen, ; which comprises reacting a compound of the formula wherein P is a protecting group, X is a leaving group with a compound of the formula R 1 H which is optionally protected and removing the protecting groups to yield a compound of formula 1.
Claim 25
Dependent Claim
25 words
A pharmaceutical composition comprising a pharmaceutically effective amount of a compound according to any of claims 1 to 14 or of their pharmaceutically acceptable salts.
Claim 26
Dependent Claim
25 words
An antiviral agent comprising a pharmaceutically effective amount of a compound according to any of claims 1 to 14 or of their pharmaceutically acceptable salts.
Claim 27
Dependent Claim
33 words
Use of a compound according to any of claims 1 to 14 or of their pharmaceutically acceptable salts for the preparation of pharmaceutical preparations for the treatment of viral infections in mammalian species.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.