Patent ID: 6346526
Filing Date: 2002-02-12
Classification: A61P,C07D

Abstract:
A compound represented by formula I: including pharmaceutically acceptable salts thereof, wherein:R1 represents H or methyl; CO2M represents a carboxylic acid, or a carboxylate anion, provided that when CO2M represents a carboxylate anion it is balanced by Q; X represents CH2 or C&boxH;O; P represents hydrogen, hydroxyl, or F; each R independently represents Rb, â€ƒâ€”Het(Rb)3, C2-6 alkenyl, or a group Lâ€”Qâ€”Rq with the proviso that only one R group of the type Lâ€”Qâ€”Rq can be present; L is C1-4 straight or branched alkylene, uninterrupted, or interrupted by 1-2 of O, S, NRa, C(O), CO2 and C(O)NRa; Q represents: Y- is a charge balancing group; n is a value from 1 to 2, selected to maintain overeall charge neutrality; Ra is H or C1-6 alkyl; Rq is C1-6 alkyl, straight or branched uninterrupted, or interrupted by 1-2 of O, S, NRa, C(O), C(O)O, C(O)NRa, â€”CH&boxH;CH, â€”Het(Rb)3â€”, â€”C(O)Het(Rb)3â€”, â€”C(O)NRaHet(Rb)3â€”, said Rq being unsubstituted or substituted with 1-3 Rc groups; Het is a heteroaryl group; each Rb is independently selected from H, halo, ORa, OC(O)Ra, C(O)Ra, CN, C(O)NRaRd, NO2, NRaRd, SO2NRaRd and C1-4 alkyl unsubstituted or substituted with 1-3 groups selected from Re; each Rc is independently selected from halo, ORf, OC(O)Rf, SRf, S(O)Rf, SO2Rf, CN, C(O)Rf, CO2Rf, NRfRg, N+RaRfRgZâˆ’, C(O)NRaRf, â€”Het(Rb)3, C(&boxH;N+RaRf)RaZâˆ’, C(&boxH;N+RaRf)NRaRfZâˆ’, NRaC(&boxH;N+RaRf)RaZâˆ’, NRaC(&boxH;N+RaRf)NRaRfZâˆ’, heteroarylium(Rb)3Zâˆ’, SO2NRaRf, OC(O)NRaRf, NRaC(O)Rf, NRaC(O)NRaRf, and â€ƒor in the alternative, when 2 or more Rc groups are present, 2 Rc groups may be taken together with any intervening atoms to form a 3-6 membered carbocyclic ring, optionally interrupted with 1-3 of O, S, NRg, and C(O), said ring being unsubstituted or substituted with 1-3 Re groups; Rd is H or C1-4 alkyl, Re is selected from halo, ORa, NRaRd and CONRaRd; Rf is H; C1-6 straight or branched chain alkyl, unsubstituted or substituted with 1-3 Re groups; â€”Het(Rb)3; C3-6 cycloalkyl, unsubstituted or substituted with 1-3 Re groups, and Rg is H, C1-6 alkyl, unsubstituted or substituted with 1-3 Re groups; C3-6 cycloalkyl, unsubstituted or substituted with 1-3 Re groups; C(&boxH;N+RaRf)RaZâˆ’ or C(&boxH;N+RaRf)NRaRfZâˆ’; and Zâˆ’ is a charge balancing group Yâˆ’.