Patent ID: 6750241
Filing Date: 2004-06-15
Classification: A61P,C07C,C07D,C07F

Abstract:
A compound of formula II:L-X-Lâ€ƒâ€ƒII or a pharmaceutically acceptable salt thereof; wherein:one L is a moiety of formula XXVIII: whereineach Rbk is independently selected from the group consisting of hydrogen, ailcyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, acylamino, acyloxy, alkoxy, substituted alkoxy, amino, substituted amino; aminoacyl, aminoacyloxy, aryl, carboxyl, carboxyalkyl, cyano, cycloalkyl, substituted cycloalkyl, halogen, heteroaryl, heterocyclic, hydroxy, oxyacylamino, nitro, thioalkoxy, substituted thioalkoxy, â€”SOâ€”Rbkâ€² and â€”SO2â€”Rhkâ€², where Rbâ€² is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, aryl, heteroaryl or heterocyclic; Rbl is aryl or heteroaryl, wherein the aryl or heteroaryl group is substituted with a covalent bond linking the moiety to the linker or with â€”(CH2)uâ€”Zâ€², where Zâ€² is a covalent bond linking the moiety to the linker and u is an integer from 1 to 3; m is an integer from 1 to 3; and the other L is a selected from the group consisting of: (a) a moiety of formula XXVIII; (b) a moiety of formula XXVI: whereinRhi is a covalent bond linking the moiety to the linker; (c) a moiety of formula VI: whereineach Rj is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl and a covalent bond linking the moiety to the linker; Rk is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, hydroxy, halogen and â€”CHO; each Q2 is independently NHjâ€², O and S, where Rjâ€² is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl or acyl; provided one and only one of Rj comprises a covalent bond linking the moiety to the linker; (d) a moiety of formula XXVII: whereineach Rbj is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyi, substituted alkenyl, alkynyl, substituted alkynyl, acyl and a covalent bond linking the moiety to the linker; Q11 is NRbjâ€², O, S or ailcylene, where RbJâ€² is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl or acyl; provided one and only one of Rbj, comprises a covalent bond linking the moiety to the linker; (e) a moiety of formula XVI: whereineach Raj is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, acylamino, acyloxy, alkoxy, substituted alkoxy, amino, substituted amino, aminoacyl, aminoacyloxy, aryl, carboxyl, carboxyalkyl, cyano, cycloalkyl, substituted cycloalkyl, halogen, heteroaryl, heterocyclic, hydroxy, oxyacylamino, nitro, thioalkoxy and substituted thioatkoxy; Ral is aryl or heteroaryl; each Rak is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloallcyl, substituted cycloalkyl, aryl, heteroaryl, heterocyclic, and a covalent bond linking the moiety to the linker; Q8 is NRalâ€², O, Sor alkylene, where Ralâ€² is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl or acyl; in is an integer from 1 to 3; provided one and only one of Rak comprises a covalent bond linking the moiety to the linker; (f) a moiety of formula XIX: whereinRas is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl and a covalent bond linking the moiety to the linker; Rat is selected from the group consisting of 4-phosphonomethyiphenyl, 4-phosphonodifluoromethyiphenyl, 3-carboxy-4-carboxymethoxyphenyl and 3,4-dihydroxyphenyl; Rau is aryl or heteroaryl, wherein the aryl or heteroaryl group is substituted with a covalent bond linking the moiety to the linker or with â€”OZâ€², where Zâ€² is a covalent bond linking the moiety to the linker; Rav is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl and alkaryl; provided one and only one of Ras and Rau comprises a covalent bond linking the moiety to the linker; (g) a moiety of formula VIII: whereineach Ro is independently selected from the group consisting of hydrogen, alkyl, substituted alkcyl, alkenyl, substituted alkenyl, alkynyl, substituted alkcynyl, alcyl, acylamino, acyloxy, alkoxy, substituted alkoxy, amino, substituted amino, aminoacyl, aminoacyloxy, aryl, carboxyl, carboxyalkyl, cyano, cycloalkyl, substituted cycloalkyl, halogen, heteroaryl, heterocyclic, hydroxy, oxyacylamino, nitro, thioalkoxy and substituted thioalkoxy; Rp is aryl or heteroaryl, wherein the aryl or heteroaryl group is substituted with a covalent bond linking the moiety to the linker or with â€”OZâ€² where Zâ€² is a covalent bond linking the moiety to the linker; Z is 2H or O; m is an integer from 1 to 3; (h) a moiety of formula X: whereineach Rt is independently selected from the group consisting of hydrogen, alkcyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, acylaniino, acyloxy, alkoxy, substituted alkoxy, amino, substituted amino, aminoacyl, aminoacyloxy, aryl, carboxyl, carboxyalkyl, cyano, cycloalkyl, substituted cycloalkyl, halogen, heteroaryl, heterocyclic, hydroxy, oxyacylamino, nitro, thioalkoxy and substituted thioalkoxy; each Ru is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, acylamino, acyloxy, alkoxy, substituted alkoxy, amino, substituted amino, aminoacyl, aminoacyloxy, aryl, carboxyl, carboxyalkyl, cyano, cycloalkcyl, substituted cycloalkyl, halogen, heteroaryl, heterocyclic, hydroxy, oxyacylaniino, nitro, thioalkoxy, substituted thioalkoxy and a covalent bond linking the moiety to the linker; Q5 is NRtâ€², O, S or alkylene, where Rtâ€² is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl or acyl; each m is independently an integer from 1 to 3; provided one and only one of Ru comprises a covalent bond linking the moiety to the linker; (i) a moiety of formula XX: whereineach Raw is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, acylamino, acyloxy, alkoxy, substituted alkoxy, amino, substituted amino, aminoacyl, aminoacyloxy, aryl, carboxyl, carboxyalkyl, cyano, cycloalicyl, substituted cycloalkyl, halogen, heteroaryl, heterocyclic, hydroxy, oxyacylamino, nitro, thioalkoxy and substituted thioallcoxy; each Rax is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, acylamino, acyloxy, alkoxy, substituted alkoxy, amino, substituted amino, aminoaeyl, aminoacyloxy, aryl, carboxyl, carboxyalkyl, cyano, cycloalkyl, substituted cycloallcyl, halogen, heteroaryl, heterocyclic, hydroxy, oxyacylamino, nitro, thioalkoxy, substituted thioalkoxy, a covalent bond linking the moiety to the linker and â€”OZâ€², where Zâ€² is a covalent bond linking the moiety to the linker; each m is independently an integer from 1 to 3; provided one and only one of Rax comprises a covalent bond linking the moiety to the linker; and (j) a moiety of formula XXIX: whereinRbn is selected from the group consisting of alkoxy, substituted alkoxy, hydroxy and â€”QZâ€², where Zâ€² is a covalent bond linking the moiety to the linker; Rbo is aryl or heteroaryl; Rbp is acyl, alkoxycarbonyl and a covalent bond linking the moiety to the linker; provided one and only one of Rbn and Rbp comprises a covalent bond linking the moiety to the linker; and X is a linker independently selected from a group of the formula: â€”Xaâ€”Zâ€”(Yaâ€”Z)mâ€²â€”Ybâ€”Zâ€”Xaâ€”whereinmâ€² is an integer of from 0 to 20; Xa at each separate occurrence is selected from the group consisting of â€”Oâ€”, â€”Sâ€”, â€”NRâ€”, â€”C(O)â€”, â€”C(O)Oâ€”, â€”C(O)NRâ€”, â€”C(S)â€”, â€”C(S)Oâ€”, â€”C(S)NRâ€”or a covalent bond; Z is at each separate occurrence is selected from the group consisting of alkylene, substituted alkylene, cycloalkylene, substituted cycloalkylene, alkenylene, substituted alkenylene, alkynylene, substituted alkynylene, cycloalkenylene, substituted cycloalkenylene, arylene, heteroarylene, heterocyclene, or a covalent bond; Ya and Yb at each separate occurrence are selected from the group consisting of: â€”C(O)NRâ€²â€”, â€”NRâ€²C(O)â€”, â€”NRâ€²C(O)NRâ€²â€”, â€”C(=NRâ€²)â€”NRâ€²â€”, â€”NRâ€²â€”C(=NRâ€²)â€”, â€”NRâ€²â€”C(O)â€”Oâ€”, â€”N=C(R)â€”NRâ€²â€”, â€”P(O)(ORâ€²)â€”Oâ€”, â€”S(O)nâ€”CRâ€²Râ€³â€”, â€”S(O)nâ€”NRâ€²â€”, â€”Sâ€”Sâ€” and a covalent bond; where n is 0, 1 or 2; and R, Râ€² and Râ€³ at each separate occurrence are selected from the group consisting of hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, alkenyl, substituted alkenyl, cycloalkenyl, substituted cycloalkyl, alkynyl, substituted alkynyl, aryl, heteroaryl and heterocyclic.