US2005096298A1PendingUtilityA1
Novel perines
Priority: Dec 17, 1999Filed: Nov 22, 2004Published: May 5, 2005
Est. expiryDec 17, 2019(expired)· nominal 20-yr term from priority
Inventors:Chester A. Metcalf, IiiManfred WeigeleTomi K. SawyerRegine BohacekWilliam C. ShakespeareRajeswari SundaramoorthiYihan WangDavid C. Dalgarno
C07D 471/04C07F 9/65583C07F 9/6561C07D 487/04C07F 9/405C07F 9/4012C07F 9/58C07F 9/65616A61K 47/54A61K 47/548
51
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Claims
Abstract
Novel purines and uses of these compounds for the treatment of bone related disorders and cancer is disclosed.
Claims
exact text as granted — not AI-modified1 - 195 . (canceled)
196 . A compound having formula (I) comprising:
wherein
R A is H or R F ;
R B is R F ;
R C is R F or -ZR E ,
R D is H, halogen, R F or -ZR E
each occurrence of Z is O, —S— or NR F ;
R E is H or R F , and
R C bears a substituent comprising a phosphorus-containing moiety of type (a) or type (b):
wherein a type (a) phosphorus-containing moiety has the structure —P(O)YR G YR H , in which:
each occurrence of R G and R H is independently H or R F , and
each occurrence of Y is independently a covalent bond, O, —S— or N(Rj) 2 , wherein Rj, for each occurrence, is independently H or R F ; and
wherein a type (b) phosphorus-containing moiety has one of the following structures:
wherein each occurrence of M is independently CV 2 , —NV—, or —S—, wherein each occurrence of V is independently hydrogen, OH, halogen, or aliphatic; each occurrence of x is independently an integer from 1-6; and each occurrence of R 1 is independently H or R F ; and,
each occurrence of R F is an aliphatic, heteroaliphatic, aryl or heteroaryl moiety;
wherein each aliphatic and heteroaliphatic moiety may be branched or unbranched, cyclic or acyclic and substituted or unsubstituted, and each aryl and heteroaryl moiety may be substituted or unsubstituted.
197 . The compound of claim 196 , wherein R C is R F or -ZR E and bears a phosphorus-containing moiety of type (b) in which each occurrence of x is independently 1 or 2.
198 . The compound of claim 197 wherein at least one occurrence of Y is O.
199 . The compound of claim 197 wherein at least one occurrence of Y is a covalent bond.
200 . The compound of claim 197 wherein each occurrence of Y is O.
201 . The compound of claim 196 , wherein R C is R F or -ZR E and bears a phosphorus-containing moiety of type (a) having the structure —P(O)YR G YR H , in which each occurrence of R G and R H is independently H or R F .
202 . The compound of claim 201 wherein at least one occurrence of Y is O.
203 . The compound of claim 201 wherein at least one occurrence of Y is a covalent bond.
204 . The compound of claim 201 wherein each occurrence of Y is O.
205 . The compound of claim 196 , wherein R D is hydrogen.
206 . The compound of claim 196 , wherein R C is -ZR E comprising an aliphatic, heteroaliphatic, aryl, or heteroarylgroup bearing a phosphorus-containing moiety of type (a).
207 . The compound of claim 201 , wherein R C is -ZR E comprising an aliphatic, heteroaliphatic, aryl, or heteroarylgroup bearing a phosphorus-containing moiety of type (b).
208 . The compound claim 196 containing an aliphatic, heteroaliphatic, aryl, or heteroaryl group substituted with 0-3 substituents selected from halogen, lower alkyl, lower alkenyl, aryl, heteroaryl, carbonyl, thiocarbonyl, ketone, aldehyde, amino, acylamino, amido, amidino, cyano, nitro, azido, sulfonyl, sulfoxido, sulfate, sulfonate, sulfamoyl, sulfonamido, phosphoryl, phosphorothioate, phosphorothicate, phosphonate, phosphinate, —(CH 2 ) p alkyl, —(CH 2 ) p alkenyl, —CH 2 ) p alkynyl, —CH 2 ) p aryl, —(CH 2 ) p aralkyl, —(CH 2 ) p OH, —CH 2 ) p O-lower alkyl, —(CH 2 ) p O-lower alkenyl, —O(CH 2 ) n R, —(CH 2 ) p SH, —(CH 2 ) p S-lower alkyl, —(CH 2 ) p S-lower alkenyl, —S(CH 2 ) n R, (CH 2 ) p N(R) 2 , —(CH 2 ) p NR-lower alkyl, —(CH 2 ) p NR-lower alkenyl, —NR(CH 2 ) n R, wherein each occurrence of R represents, independently H, or a substituted or unsubstituted aryl, heterocycle, heteroaryl, alkylaryl, alkenyl, or alkyl moiety, and wherein each occurrence of p independently represents an integer from 0-10.
209 . The compound of claim 196 , wherein R C is substituted with at least one phosphorus moiety selected from:
210 . The compound of claim 196 , wherein R B is an aryl, heteroaryl, alkylaryl, or alkylheteroaryl optionally substituted with one or more halogen groups.
211 . The compound of claim 196 , wherein R A is a substituted or unsubstituted, branched or unbranched, cyclic or acyclic aliphatic or heteroaliphatic moiety optionally substituted by one of more hydroxyl moieties.
212 . The compound of claim 211 containing an aliphatic R A comprising a methyl, isopropyl, cyclopentyl or cyclohexyl group.
213 . The compound of claim 196 , wherein R C is —R F , —OR F , —SR F or —NHR F .
214 . A pharmaceutical composition comprising the compound of any one of claims 196 - 213 and a pharmaceutically acceptable carrier or excipient.
215 . A method for treating osteoporosis or another bone-related disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of any one of claims 196 - 213 .
216 . A method for inhibiting the growth of tumor cells comprising contacting cells with a therapeutically effective amount of a compound of any one of claims 196 - 213 .Join the waitlist — get patent alerts
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