Pyrazolopyrimidine and pyrimidinyl bisphosphonic esters as anti-inflammatories
AssigneeThe Upjohn Company
InventorsRichard A. Nugent, Stephen T. Schlachter
Life of this patent
Estimating the term…
Abstract
Compounds useful in the treatment of inflammation structurally represented as ##STR1## wherein X is O or S and the R groups are as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents without inhibiting prostaglandin synthesis.
Claims9
A compound of Formula 1 or pharmaceutically acceptable salts thereof ##STR3## wherein each occurrence of R.sub.1 is the same or different and is selected from the group consisting of H, Na, K, C.sub.1 -C.sub.6 alkyl, CH.sub.2 -phenyl, phenyl (optionally substituted with 1 to 5 NO.sub.2, halo, or C.sub.1 -C.sub.4 alkyl), or both OR.sub.1 on the same P are taken together along with CH.sub.2 --CH.sub.2, CH.sub.2 --CH.sub.2 --CH.sub.2, or CH.sub.2 --C(CH.sub.3).sub.2 --CH.sub.2 to form a heterocyclic ring having one P, two O and two or three carbon atoms;
- R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, benzoyloxy, benzyloxy, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.3 -C.sub.7 cycloalkyl, phenyl (optionally substituted with 1 or 2 phenyls, or 1 to 5 halo, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio), 2-, 4- or 5-pyrimidyl (optionally substituted with 1 or 2 phenyls, or 1 to 3 halo, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, or C.sub.1 -C.sub.6 alkylthio), 2-, 3- or 4-pyridyl (optionally substituted with 1 or 2 phenyls, or 1 to 4 halo, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.10 alkyl, C.sub.3 - C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio), 1- or 2- naphthalenyl (optionally substituted with 1 or 2 phenyls, or 1 to 7 halo, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio);
- R.sub.3 is H, CN, CO.sub.2 R.sub.1, COR.sub.2, CON(R.sub.5).sub.2, halo, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.7 cycloalkyl, or phenyl;
- R.sub.5 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl;
- and
- R.sub.6 is H, halo, or C.sub.1 -C.sub.6 alkyl.
Dependencies are inferred from the claim text.