| US 7,507,824 B2 | ||
| Spiro(2H-1benzopyran-2,4′-piperidine) derivates as glycine transport inhibitors | ||
| Samuel George Gibson, Motherwell (United Kingdom); and David John Miller, Airdrie (United Kingdom) | ||
| Assigned to N.V. Organon, Oss (Netherlands) | ||
| Filed on Aug. 08, 2003, as Appl. No. 10/637,681. | ||
| Application 10/637681 is a division of application No. 10/130557, granted, now 6,645,973, previously published as PCT/EP00/11351, filed on Nov. 13, 2000. | ||
| Claims priority of application No. 99309137 (EP), filed on Nov. 17, 1999. | ||
| Prior Publication US 2004/0029904 A1, Feb. 12, 2004 | ||
| Int. Cl. C07D 471/10 (2006.01); A61K 31/438 (2006.01) | ||
| U.S. Cl. 546—15 [546/16; 546/18; 514/278] | 5 Claims |
1. A spiro[2H-1-benzopyran-2,4′-piperidine] derivative having formula I:
![]() wherein the dotted line represents an optional bond;
Y represents 1-2 substituents independently selected from hydrogen, halogen, (C1-6)alkyl optionally substituted with one or more halogens, (C1-6)alkyloxy optionally substituted with one or more halogens, (C2-6)alkenyloxy, (C2-6)alkynyloxy, pyridinylmethyloxy, SR3, NR3R4, OSO2R5, and NR3SO2R4; or 2 substituents Y may together form O—(CH2)n—O or O—(CF2)n—O, where n is 1 or 2;
X represents 1-3 substituents independently selected from hydrogen, halogen, hydroxy, (C1-4)alkyloxy, SR3, NR3SO2R4 and (C1-4)alkyl, optionally substituted with halogen;
R1 is hydrogen, (C1-4)alkyl or (C6-12)aryl;
R2, R3 and R4 are independently hydrogen or (C1-4) alkyl;
R5 is (C1-4)alkyl (optionally substituted with one or more halogens) or (C6-12)aryl (optionally substituted with (C1-4)alkyl); or a pharmaceutically acceptable salt thereof,
wherein at least one of Y represents 1 substituent selected from pyridinylmethyloxy; or at least 2 substituents Y together
form O—(CH2)n—O or O—(CF2)n—O, where n is 1 or 2.
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