Patent ID: 6559160
Filing Date: 2003-05-06
Classification: A61P,C07D

Abstract:
A composition comprising a pharmaceutically acceptable excipient and a compound having the formula: whereinthe subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, wherein each substituent of the substituted aryl or substituted heteroaryl is independently selected from the group consisting of halogen, â€”ORâ€², â€”OC(O)Râ€², â€”NRâ€²Râ€³, â€”SRâ€², â€”Râ€², â€”CN, â€”NO2, â€”CO2Râ€², â€”CONRâ€²Râ€³, â€”C(O)Râ€², â€”OC(O)NRâ€²Râ€³, â€”NRâ€³C(O)Râ€², â€”NRâ€³C(O)2Râ€², â€”NRâ€²â€”C(O)NRâ€³Râ€²â€³, â€”NHâ€”C(NH2)&boxH;NH, â€”NRâ€²C(NH2)&boxH;NH, â€”NHâ€”C(NH2)&boxH;NRâ€², â€”S(O)Râ€², â€”S(O)2Râ€², â€”S(O)2NRâ€²Râ€³, â€”N3, â€”CH(Ph)2, perfluoro(C1-C4)alkoxy, and perfluoro(C1-C4)alkyl, wherein Râ€², Râ€³and Râ€²â€³ are independently selected from hydrogen, (C1-C8)alkyl and heteroalkyl, unsubstituted aryl and heteroaryl, unsubstituted aryl-(C1-C4)alkyl, and unsubstituted aryloxy-(C1-C4)alkyl; and optionally further wherein two of the substituents on adjacent atoms of the aryl or heteroaryl ring may be replaced with a substituent of the formula â€”Tâ€”C(O)â€”(CH2)qâ€”Uâ€”, wherein T and U are independently â€”NHâ€”, â€”Oâ€”, â€”CH2â€”or a single bond, and q is an integer of from 0 to 2, or a substituent of the formula â€”Aâ€”(CH2)râ€”Bâ€”, wherein A and B are independently â€”CH2â€”, â€”Oâ€”, â€”NHâ€”, â€”Sâ€”, â€”S(O)â€”, â€”S(O)2â€”, â€”S(O)2Nâ€²â€”or a single bond, and r is an integer of from 1 to 3, and wherein one of the single bonds of the ring so formed may optionally be replaced with a double bond, or a substituent of the formula â€”(CH2)sâ€”Xâ€”(CH2)tâ€”, where s and t are independently integers of from 0 to 3, and X is â€”Oâ€”, â€”NRâ€²â€³â€”, â€”Sâ€”, â€”S(O)â€”, â€”S(O)2â€”, or â€”S(O)2NRâ€²â€³â€”and the substituent Râ€²â€³ in â€”NRâ€²â€³â€” and â€”S(O)2NRâ€²â€³â€” is selected from hydrogen or unsubstituted (C1-C6)alkyl; R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl; R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl; each R3 is independently a substituent selected from the group consisting of -halogen, ORb, â€”OC(O)Rb, â€”NRbRc, â€”SRb, â€”Rb, â€”CN, â€”NO2, â€”CO2Rb, â€”CONRbRc, â€”C(O)Rb, â€”OC(O)NRbRc, â€”NRcC(O)Rb, â€”NRcC(O)2Rb, , â€”NRbâ€”C(O)NRcRd, â€”NHâ€”C(NH2)&boxH;NH, â€”NRbC(NH2)&boxH;NH, â€”NHâ€”C(NH2)&boxH;NRb, â€”S(O)Rb, â€”S(O)2Rb, â€”S(O)2NRbRc, â€”N3, â€”CH(Ph)2, perfluoro(C1-C4)alkoxy, and perfluoro(C1-C4)alky, and where Rb, Rc and Rd are independently selected from hydrogen, (C1-C8)alkyl and heteroalkyl, unsubstituted aryl and heteroaryl, unsubstituted aryl-(C1-C4)alkyl, and unsubstituted aryloxy-(C1-C4)alkyl; Y is a member selected from the group consisting of substituted or unsubstituted (C2-C8)alkllene and substituted or unsubstituted (C2-C8)heteroalkylene; Z is â€”NR4R5, wherein R4 and R5 are independently selected from the group consisting of hydrogen and (C1-C8)alkyl and optionally taken together with the nitrogen atom to which each is attached to form one 5- , 6- or 7- membered ring; and, wherein each of said substituted alkyl, heteroalkyl, alkylene or heteroalkylene of Y, R1, R2 is independently substituted with one or members independently selected from the group consisting of â€”ORe,&boxH;O, &boxH;NRe, &boxH;Nâ€”ORe, â€”NReRf, â€”SRe, -halogen, â€”SiReRfRg, â€”OC(O)Re, â€”C(O)Re, â€”CO2Re, â€”CONReRf, â€”OC(O)NReRf, â€”NRfC(O)Rc, â€”NRcâ€”C(O)NRfRg, â€”NRfC(O)2Re, â€”NHâ€”C(NH2)&boxH;NH, â€”NReC(NH2)&boxH;NH, â€”NHâ€”C(NH2)&boxH;NRe, â€”S(O)Re, â€”S(O)2Rc, â€”S(O)2NRe, Rf, â€”CN and â€”NO2 in a number ranging from zero to (2mâ€²+1), wherein mâ€² is the total number of carbon atoms in said alkyl, heteroalkyl, alkylene or heteroalkylene of said substituted alkyl, heteroalkyl, alkylene or heteroalkylene of Y, R1, and R2; and Re, Rfand Rg each independently is hydrogen, unsubstituted (C1-C8)alkyl and heteroalkyl, unsubstituted aryl, aryl substituted with from 1 to 3 halogens, unsubstitated alkyl, alkoxy or thioalkoxy groups, or aryl-(C1-C4)alkyl groups; and optionally, when Re and Rf are attached to the same nitrogen atom, Re and Rf can be taken together with the nitrogen atom to form one 5-, 6- , or 7-membered ring.