Heteroaryl, heterocyclic and aryl compounds which inhibit...

Details Heteroaryl, heterocyclic and aryl compounds which inhibit... Heteroaryl, heterocyclic and aryl compounds which inhibit...

2008-05-27

2008-05-27

Wilson, James O. (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C548S125000, C514S359000, C514S461000

Reexamination Certificate

active

07378529

ABSTRACT:
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

REFERENCES:
patent: 4018913 (1977-04-01), Okamoto et al.
patent: 4018915 (1977-04-01), Okamoto et al.
patent: 4036955 (1977-07-01), Okamoto et al.
patent: 4041156 (1977-08-01), Okamoto et al.
patent: 4046876 (1977-09-01), Okamoto et al.
patent: 4055636 (1977-10-01), Okamoto et al.
patent: 4055651 (1977-10-01), Okamoto et al.
patent: 4070457 (1978-01-01), Okamoto et al.
patent: 4073914 (1978-02-01), Kikumoto et al.
patent: 4085057 (1978-04-01), Masuda et al.
patent: 4096255 (1978-06-01), Kikumoto et al.
patent: 4104392 (1978-08-01), Okamoto et al.
patent: 4438122 (1984-03-01), Holmwood et al.
patent: 4505910 (1985-03-01), Bagli
patent: 4518600 (1985-05-01), Holmwood et al.
patent: 4544402 (1985-10-01), Schnurbusch et al.
patent: 4559345 (1985-12-01), Gomarasca et al.
patent: 4672065 (1987-06-01), Spatz
patent: 4908368 (1990-03-01), Murase et al.
patent: 4959364 (1990-09-01), Mueller et al.
patent: 4992439 (1991-02-01), Meanwell
patent: 5030644 (1991-07-01), Baldwin et al.
patent: 5120734 (1992-06-01), Klausener et al.
patent: 5238934 (1993-08-01), Knuppel et al.
patent: 5278184 (1994-01-01), Artico et al.
patent: 5510332 (1996-04-01), Kogan et al.
patent: 5580868 (1996-12-01), Lunkenheimer et al.
patent: 5770573 (1998-06-01), Arrhenius et al.
patent: 5814643 (1998-09-01), Duggan et al.
patent: 5861429 (1999-01-01), Sato et al.
patent: 5925644 (1999-07-01), Jakobi et al.
patent: 5942504 (1999-08-01), Grobelny
patent: 5955491 (1999-09-01), Sohda et al.
patent: 5962479 (1999-10-01), Chen
patent: 5972946 (1999-10-01), Murata et al.
patent: 6005117 (1999-12-01), Wehner et al.
patent: 2241149 (1997-07-01), None
patent: 2259224 (1998-01-01), None
patent: 19536891 (1997-04-01), None
patent: 2655636 (1997-06-01), None
patent: 19548709 (1997-07-01), None
patent: 19654483 (1998-01-01), None
patent: 19713000 (1998-10-01), None
patent: 116494 (1984-08-01), None
patent: 0 147 211 (1985-07-01), None
patent: 0 288 176 (1988-10-01), None
patent: 0330506 (1989-08-01), None
patent: 0330506 (1989-08-01), None
patent: 0 526 348 (1993-02-01), None
patent: 0 535 512 (1993-04-01), None
patent: 59212480 (1984-12-01), None
patent: WO 92/16549 (1992-10-01), None
patent: WO 93/12809 (1993-07-01), None
patent: WO 93/24154 (1993-12-01), None
patent: WO 96/01644 (1996-01-01), None
patent: WO 96/22966 (1996-08-01), None
patent: WO 96/32383 (1996-08-01), None
patent: WO 97/23451 (1997-07-01), None
patent: WO 98/00395 (1998-01-01), None
patent: WO 98/33783 (1998-08-01), None
patent: WO 98/53814 (1998-12-01), None
patent: WO 98/53817 (1998-12-01), None
patent: WO 99/06390 (1999-02-01), None
patent: WO 99/06391 (1999-02-01), None
patent: WO 99/06431 (1999-02-01), None
patent: WO 99/06432 (1999-02-01), None
patent: WO 99/06433 (1999-02-01), None
patent: WO 99/10312 (1999-03-01), None
patent: WO 99/37605 (1999-07-01), None
patent: WO 99/37618 (1999-07-01), None
patent: WO 99/52898 (1999-10-01), None
patent: WO 00/10313 (2000-02-01), None
Hladon, Buguslaw et al., In Vitro cytostatic activity of some amino acid 4-N-substituted cytosines,Arch. Immunol. Ther. Exp.(1992), 40(2), 145-50. (Abstract).
Hoffman, Seigfried; Schubert, Herman; Nitsche, Klaus, N-Pyrimidinylamino acids. III. N-(oxopyrimidinyl) derivatives of neutral amino acids,Z. Chem.(1972), 12(1) 21-2, Coden: Zeceal (Abstract).
Teranishi, Katsunori; Goto, Toshio, Synthesis and Chemiluminescense of Coelenterazine (Oplophorus Luciferin) analogs,Bull. Chem. Soc. Jpn.(1990), 63(11), 3132-40 , (Abstract).
Abraham, W.M., et al. “α4-Integrins Mediate Antigen -induced Late Bronchial Responses and Prolonged Airway Hyperresponsiveness in Sheep.”J. Clin. Invest.93: 776-787 (1994).
Bao, L., et al. “Correlation of VLA-4 integrin expression with metastatic potential in various human tumour cell lines.”Diff.52: 239-246 (1993).
Baron, J.L., et al. “Surface Expression of α4 Integrin by CD4 T Cells is Required for Their Entry into Brain Parenchyma.”J. Exp. Med.177: 57-68 (1993).
Baron, J.L., et al. et al. “The Pathogenesis of Adeoptive Murine Autonimmune Diabetes Requires an Interaction between α4-Integrins and Vascular Cell Adhesion Molecule-1.”J. Clin. Invest.93: 1700-1708 (1994).
Burkly, L.C., et al. “Protection Against Adoptive Transfer of Autoimmune Diabetes Mediated Through Very Late Antigent-4 Integrin.”Diabetes.43: 529-534 (1994).
Cybulsky, M.I., et al. “Endothelial Expression of a Mononuclear Leukocyte Adhesion Molecule During Atherogenesis.”Science.251: 788-791 (1991).
Elices, M.J., et al. “Expression and Functional Significance of Alternatively Spliced CS1 Fibronecting in Rheumatoid Arthritis Microvasculature.”J. Clin. Invest.93: 405-416 (1994).
Elices, M.J., et al. “VCAM-1 on Activated Endothelium Interacts with the leukocyte Integrin VLA-4 at a Site Distinct from the CLA-4/Fibronectin Binding Site.”Cell.60: 577-584 (1990).
Hamann, A., et al. “Role of α4-Integrins in Lymphocute Homing to Mucosal Tissues in Vivo.”J. Immunology.152: 3283-3292 (1994).
Hladon, B., et al. In Vitro cytostatic Activity of some amino acid 4-N-substituted cytosines.Arch. Immunol. Ther. Exp.40(2): 145-150 (1992). (Abstract).
Hoffman, S., et al. “N-Pyrimidinylamino acids. III. N-(oxopyrimidinyl) derivatives of neutral amino acids.”Z. Chem.12(1): 21-22 (1972), Coden: Zeceal (Abstract).
Kawaguchi, S., et al. “VLA-4 Molecules on Tumor Cells Initiate an Adhesive Interaction with VCAM-1 Molecules on Endothelial Cell Surface.”Japanese J. Cancer Res.83: 1304-1316 (1992).
Lauri, D., et al. “Decreased adhesion to endothelial cells and matrix proteins of H-2Kbgene transfected tumour cells.”British J. Cancer.68: 862-867 (1993).
Li, H., et al. “An Atherogenic Diet Rapidly Induces VCAM-1, a Cytokine-Regulatable Mononuclear Leeukocyte Adhesion Molecule, in Rabbit Aortic Endothelium.”Arterioscler. Thromb.13(2): 197-204 (1993).
Mulligan, M.S., et al. “Role of β1, β2 Integrins and ICAM-1 in Lung Injury after Deposition of IgG and gA Immune Complexes.”J. Immunol.150(6): 2407-2417 (1993).
Okarhara, H., et al. “Involvement of Very Late Activation Antigen 4 (VLA-4) and Vascular Cell Adhesion Molecule 1(VCAM-1) in Tumor Necrosis Factor α Enhancement of Experimental Metastasis.”Can. Res.54: 3233-3236 (1994).
Osborn, L. “Leukocyte Adhesion to Endothelium in Inflammation.”Cell.62: 3-6 (1990).
Paavonen, T., et al. “In Vivo Evidence of the Role of α4β1-VCAM-1 Interaction in Sarcoma, but not in Carcinoma Extravasation.”Int. J. Can.58: 298 (1994).
Paul, L.C.,et al. “Monoclonal Antibodies Against LFA-1 and VLA-4 Inhibit Graft Vasculitis in Rat Cardiac Allografts.”Transpl. Proceed.25(1): 813-814 (1993).
Postigo, A.A., et al. “Increased Binding of Synovial T Lumphocytes from Rheumatoid Arthritis to Endothelial-Leukocyte Adhesion Molecule-1 (ELAM-1) and Vascular Cell Adhesion Molecule-1 (VCAM-1).”J. Clin. Invest.89: 1445-1452 (1991).
Pretolani, M., et al. “Antibody to Very Late Activation Antigen 4 Prevents Antigen-induced Bronchial Hyperreactivity and Cellular Infiltration in the Guinea Pig Airways.”J. Exp. Med.180: 795-805 (1994).
Sasseville, V.G., et al. “Monocyte Adhesion to Endothelium in Simian Immunodeficiency Virus-Induced AIDS Encephalitis is Mediated by Vascular Cell Adhesion Molecule-1/α4β1Integrin Inter

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