| US 7,462,629 B2 | ||
| Immunosuppressant compounds and compositions | ||
| Shifeng Pan, San Diego, Calif. (US); Nathanael S. Gray, San Diego, Calif. (US); Yuan Mi, San Diego, Calif. (US); Yi Fan, San Diego, Calif. (US); and Wenqi Gao, San Diego, Calif. (US) | ||
| Assigned to IRM LLC, Hamilton (Bermuda) | ||
| Filed on May 19, 2004, as Appl. No. 10/849,450. | ||
| Claims priority of provisional application 60/471931, filed on May 19, 2003. | ||
| Prior Publication US 2005/0009786 A1, Jan. 13, 2005 | ||
| Int. Cl. A61K 31/4725 (2006.01); A61K 31/4035 (2006.01); A61K 31/397 (2006.01); C07D 217/12 (2006.01); C07D 209/44 (2006.01); C07D 205/12 (2006.01) | ||
| U.S. Cl. 514—307 [514/210.01; 514/307; 514/443; 546/139; 548/452; 548/950] | 11 Claims |
1. A compound of Formula I:
![]() in which:
n is 1, 2 or 3;
A is chosen from —X1C(O)OR6, —X1OP(O)(OR6)2, —X1P(O)(OR6)2, —X1S(O)2OR6, —X1P(O)(R6)OR6 and 1H-tetrazol-5-yl; wherein X1 is chosen from a bond and C1-3alkylene; and each R6 is independently chosen from hydrogen and C1-6alkyl;
X is a bond or is chosen from C1-4alkyelene, —X1OX2—, —X1NR7X2—, —X1C(O)NR7X2—, —X1NR7C(O)X2—, —X1S(O)X2—, —X1S(O)2X2—, —X1SX2— and C2-9heteroarylene; wherein X1 and X2 are independently chosen from a bond and C1-3alkylene; R7 is chosen from hydrogen and C1-6alkyl; and any heteroarylene of X is optionally substituted by a member of the group chosen from halo and C1-6alkyl;
Y is C6-10aryl, wherein any aryl of Y can be optionally substituted with 1 to 3 radicals chosen from halo, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkoxy, halo-substituted C1-6alkyl and halo-substituted C1-6alkoxy;
R1 is chosen from C6-10aryl and C2-9heteroaryl; wherein any aryl or heteroaryl of R1 is substituted by a radical chosen from C6-10arylC0-4alkyl, C2-9heteroarylC0-4alkyl, C3-8cycloalkylC0-4alkyl, or C3-8heterocycloalkylC0-4alkyl; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl group of R1 can be optionally substituted by one to five radicals chosen from halo, C1-6alkyl, C1-6alkoxy, halo-substituted-C1-6alkyl and halo-substituted-C1-6alkoxy; and any alkyl group of R1 can optionally have a methylene replaced by an atom or group chosen from —S—, —S(O)—, —S(O)2—, —NR7— and —O—; wherein R7 is chosen from hydrogen or C1-6alkyl;
R2, R3, R4 and R5 are independently chosen from hydrogen, C1-6alkyl, halo, hydroxy, C1-6alkoxy, halo-substituted C1-6alkyl and halo-substituted C1-6alkoxy; and the pharmaceutically acceptable salts, hydrates, solvates, isomers and prodrugs thereof.
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