Inhibitors of α4β1 mediated cell adhesion
AssigneesPharmacia & Upjohn Company, Tanabe Seiyaku Co., Ltd.
InventorsJames Blinn, Robert Chrusciel, Jed Fisher, Steven Tanis, Edward Thomas, Thomas Lobl, Bradley Teegarden
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Abstract
The present invention relates to compound of formula (I), that are potent inhibitors of α4β1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing α4β1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.
Claims9
A compound of the formula:
- wherein
- R1 is hydrogen or C1-3 alkyl;
- R2 is hydrogen or C1-6 alkyl;
- in addition, R1 and R2 may be attached to the same carbon atom and may form a carbocyclic ring of 5-8 atoms together with the carbon atom to which they are attached or be attached to the same atom and form a ring of 5-8 atoms of the formula:
- together with the carbon atom to which they are attached;
- R3 and Y represent
- a) R3 is C7-17 arylalkyl, (C1-6 alkyl)-OH, (C1-6 alkyl)-CO2—R11, (C1-6 alkyl)-CN, adamantyl, phenyl, or one of the following:
- and Y is —C(═O)—, or
- b) R3 is C1-6 alkyl, C7-17 arylalkyl, (C1-6 alkyl)-OH, (C1-6 alkyl)-CO2—R11, (C1-6 alkyl)-CN, adamantyl, phenyl, or one of the following:
- and Y is —C(═O)—, —SO2—, or —C(═O)N(R10)—;
- R4 is —OH, NH21 NHOH, or is of the formula
- R5 is a formula of the following:
- wherein R7 is hydrogen or Cl;
- R6 is N or CH;
- R8 is —NH—Y1—, or —CONH—;
- R10 is C1-6 alkyl, or (C1-6 alkyl)-OH, or hydrogen;
- R11 is hydrogen or CH3;
- W is (C1-6 alkyl);
- X is S;
- Y1 is —CO—, —C(═O)O—, —SO2—, or —C(═O)N(R10)—;
- Z is O, CH2, or N—R11;
- l is 1 or 2;
- m is 2;
- n is 0;
- o is 0 or 1;
- p is 0;
- and
- q is 0 or 1.
Dependencies are inferred from the claim text.