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US 7,351,725 B2Granted
N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as Edg receptor agonists
AssigneeMerck & Co., Inc.
InventorsGeorge A. Doherty, Zhen Li, Jeffrey J. Hale, Sander G. Mills
Life of this patent
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Abstract
The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
Claims10
A compound of Formula I
- or a pharmaceutically acceptable salt or hydrate thereof, wherein:
- Ar is phenyl;
- A is —CO2H;
- n is 2, 3 or 4;
- each R1 and R2 is independently selected from the group consisting of:
- hydrogen, halo, hydroxy, —CO2H, C1-6alkyl and phenyl, said C1-6alkyl and phenyl optionally substituted with 1-3 halo groups;
- R3 is selected from the group consisting of:
- hydrogen and C1-4alkyl, optionally substituted with 1-3 hydroxy or halo groups;
- each R4 is independently selected from the group consisting of:
- hydroxy, halo, —CO2H, C1-4alkyl, —S(O)kC1-3alkyl, wherein k is 0, 1 or 2, C1-3alkoxy, C3-6 cycloalkoxy, aryl and aralkoxy, the alkyl portions of said C1-4alkyl, —S(O)kC1-3alkyl, C1-3alkoxy and C3-6 cycloalkoxy optionally substituted with 1-3 halo groups;
- C is HET, wherein HET is thienyl;
- B is selected from the group consisting of:
- C1-6alkyl, C1-5alkoxy, —(C═O)—C1-5alkyl, —(C═O)—O—C1-4alkyl, —(C═O)—N(R6)(R7)—C1-4alkyl,
- phenyl and HET;
- and
- R6 and R7 are independently selected from the group consisting of:
- hydrogen, C1-9alkyl and —(CH2)p-phenyl, wherein p is 1 to 5 and phenyl is optionally substituted with 1-3 substituents independently selected from the group consisting of:
- C1-3alkyl and C1-3alkoxy, each optionally substituted with 1-3 halo groups.
15 more elements
A compound of Formula II
- or a pharmaceutically acceptable salt or hydrate thereof, wherein
- the group —B—C is attached to the phenyl ring at the 3- or 4-position;
- n is 2, 3 or 4;
- each R1 and R2 is independently selected from the group consisting of:
- hydrogen, —CO2H, hydroxy, halo, C1-3alkyl and phenyl, said C1-3alkyl and phenyl optionally substituted with 1-3 halo group;
- A is —CO2H;
- R3 is hydrogen or methyl;
- each R4 is independently selected from the group consisting of:
- halo, hydroxy, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, phenyl, benzyloxy and cyclopropyloxy;
- and
- B—C is
8 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt of any of the foregoing compounds.
Dependencies are inferred from the claim text.