19-12-2013 дата публикации
Номер: US20130336921A1
Автор:
Bell Noah,
Carreras Christopher,
Chang Han-Ting,
Charmot Dominique,
Chen Tao,
Jacobs Jeffrey W.,
Labonte Eric,
Leadbetter Michael R.,
Lewis Jason G.,
Navre Marc,
Reich Nicholas
Принадлежит:
ARDELYX, INC.
Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): 2. A compound of wherein Y is halogen.3. A compound of wherein Y is chloro.4. A compound of wherein Y is alkylamino.5. A compound of wherein Y is diethylamino.6. A compound of wherein Y is alkoxy.7. A compound of wherein Y is heterocyclyl.9. A compound of wherein Y is —O(cycloalkyl).10. A compound of wherein X is —ZR claim 1 , and wherein Z is aryl or heteroaryl and Ris a non-hydrogen substituent11. A compound of wherein Z is aryl.12. A compound of wherein Z is phenyl.14. A compound of wherein Z is heteroaryl.15. A compound of wherein Z is pyridinyl.17. A compound of wherein Ris:{'sub': 2', '0-2', '1-6', '6', '3, '(a) —CHS(O)(optionally substituted Calkyl)C(═O)NRR,'}{'sub': 2', '0-2', '1-6', '6', '3, '(b) —CHS(O)O(optionally substituted Calkyl)NRR,'}{'sub': 2', '0-2', '1-6', '4, '(c) —C(HS(O)(optionally substituted Calkyl)C(═O)OR,'}{'sub': 2', '0-2', '1-6', '4, '(d) —CHS(O)(optionally substituted Calkyl)OR,'}{'sub': 2', '2', '1-6', '5, '(e) —CHS(O)O(optionally substituted Calkyl)R,'}{'sub': 2', '0-2', '5, '(f) —CHS(O)R,'}{'sub': 2', '0-2', '6', '3, '(g) —CHS(O)NRR,'}{'sub': 2', '0-2', '2', '2', 'x', '4, '(h) —CHS(O)(CHCHO)R,'}{'sub': 2', '6', '2', '2', 'x', '4, '(i) —CHNR(CHCHO)R,'}{'sub': 6', '1-6', '6', '3, '(j) —C(═)NR(optionally substituted Calkyl)C(═O)NRR,'}{'sub': 6', '1-6', '6', '3, '(k) —C(═O)NR(optionally substituted Calkyl)NRR,'}{'sub': 6', '1-6', '4, '(l) —C(═O)NR(optionally substituted Calkyl)C(═O)OR,'}{'sub': 6', '1-6', '4, '(m) —C(═O)NR(optionally substituted Calkyl)OR,'}{'sub': 6', '1-6', '5, '(n) —C(═O)NR(optionally substituted Calkyl)R, or'}{'sub': 6', '2', '2', 'x', '4, '(o) —C(═O)NR(CHCHO)R;'}wherein{'sub': 3', '1-6, 'Ris hydrogen, hydroxyl, alkoxy, optionally substituted Calkyl, optionally substituted aryl, optionally substituted ...
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