Strategies for TGF-β modulation: a review of recent patents

Bibliography

• Sporn MB, Roberts AB. Autocrine growth factors and cancer. Nature 1985;313(6005):745-7
   PubMed Web of Science ®Google Scholar
• Akhurst RJ, Fee F, Balmain A. Localized production of TGF-beta mRNA in tumour promoter-stimulated mouse epidermis. Nature 1988;331(6154):363-5
   PubMed Web of Science ®Google Scholar
• Laping NJ, Huet S. TGF-beta receptor kinase inhibitors for the treatment of fibrosis. Proteins Cell Regul 2006;5:443-59
   Google Scholar
• Wolf G, Mueller E, Stahl RA, Ziyadeh FN. Angiotensin II-induced hypertrophy of cultured murine proximal tubular cells is mediated by endogenous TGF-beta. J Clin Invest 1993;92(3):1366-72
   PubMed Web of Science ®Google Scholar
• Juknevicius I, Segal Y, Kren S, Effect of aldosterone on renal TGF-beta. Am J Physiol Renal Physiol 2004;286(6):F1059-62
   Web of Science ®Google Scholar
• Gaedeke J, Neumayer H-H, Peters H. Pharmacological management of renal fibrotic disease. Expert Opin Pharmacother 2006;7(4):377-386
   Google Scholar
• Clinical Trials.gov. NCT000320970
   Google Scholar
• Clinical Trials.gov. NCT00381134, 2006; NCT00140985, 2005
   Google Scholar
• Yingling JM, Blanchard KL, Sawyer JS. Development of TGF-beta signaling inhibitors for cancer therapy. Nat Rev Drug Discov 2004;3(12):1011-21
   PubMed Web of Science ®Google Scholar
• Schlingensiepen R, Goldbrunner M, Szyrach MNI, Intracerebral and intrathecal infusion of the TGF-beta2-specific antisense phosphorothioate oligonucleotide AP 12009 in rabbits and primates: toxicology and safety. Oligonucleotides 2005;15(2):94-104
   PubMedGoogle Scholar
• Schlingensiepen K-H, Schlingensiepen R, Steinbrecher A, Targeted tumor therapy with the TGF-beta2 antisense compound AP 12009. Cytokine Growth Factor Rev 2006;17(1-2):129-39
   PubMed Web of Science ®Google Scholar
• Schlingensiepen K-H, Fischer-Blass B, Schmaus S, Ludwig S. Antisense therapeutics for tumor treatment: the TGF-beta2 inhibitor AP 12009 in clinical development against malignant tumors. Recent Results Cancer Res 2008;177 (Pancreatic Cancer):137-50
   PubMedGoogle Scholar
• Specht H. Clinical proof of concept for TGF-beta2 inhibitor AP 12009 in phase IIb. EMEA provides guidance on phase II design and approval requirements. Antisense Pharma press release 2008
   Google Scholar
• Cambridge Antibody Technology. Press release 2005
   Google Scholar
• Denton CP, Merkel PA, Furst DE, Recombinant human anti-transforming growth factor beta 1 antibody therapy in systemic sclerosis. A multicenter, randomized, placebo-controlled phase I/II trial of CAT-192. Arthritis Rheum 2007;56(1):323-33
   PubMedGoogle Scholar
• Clinical Trials.gov, NCT00464321, 2007; NCT00356460, 2006; NCT00125385, 2009
   Google Scholar
• Eli Lilly Company Research Pipeline April 15th 2009
   Google Scholar
• Kontani K, Kajino K, Huangi C-H, Spontaneous elicitation of potent antitumor immunity and eradication of established tumors by administration of DNA encoding soluble transforming growth factor-beta II receptor without active antigen-sensitization. Cancer Immunol Immunother 2006;55(5):579-87
   PubMed Web of Science ®Google Scholar
• Fujita T, Teramoto K, Ozaki Y, Inhibition of transforming growth factor-beta-mediated immunosuppression in tumor-draining lymph nodes augments antitumor responses by various immunologic cell types. Cancer Res 2009;69(12):5142-50
   PubMed Web of Science ®Google Scholar
• Ezquerro I-J, Lasarte J-J, Dotor J, A synthetic peptide from transforming growth factor betatype III receptor inhibits fribrogenesis in rats with carbin tetrachloride liver injury. Cytokine 2003;22(1-2):12-20
   PubMed Web of Science ®Google Scholar
• Hermida N, Lopez B, Gonzalez A, A synthetic peptide from transforming growth factor-beta1 type III receptor prevents myocardial fibrosis in spontaniously hypertensive rats. Cardiovascular Res 2009;81(3):601-9
   PubMed Web of Science ®Google Scholar
• Borras Cuesta F, Casares Agar N, Proyecto De Biomedicina Cima SL, Use of TGF-beta inhibitor peptides in the preparation of immune response modulating agent. WO2007048857; 2007
   Google Scholar
• Clinical Trials.gov. NCT00574613
   Google Scholar
• Huse M, Chen Y-G, Massague J, Kuriyan J. Crystal structure of the cytoplasmic domain of the type I TGF-beta receptor in complex with FKBP12. Cell, 1999;96(3):425-36
   PubMed Web of Science ®Google Scholar
• Sawyer JS, Anderson BD, Beight DW, Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of transforming growth factor-b type 1 receptor kinase domain. J Med Chem 2003;46(19):3953-6
   PubMed Web of Science ®Google Scholar
• Sawyer JS, Beight DW, Britt KS, Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-b type 1 receptor kinase domain. Bioorg Med Chem Lett 2004;14:3581-4
   PubMed Web of Science ®Google Scholar
• Gellibert F, Woolven J, Fouchet M-H, Identification of 1,5-naphtyridine derivatives as a novel series of potent and selective TGF-b type 1 receptor inhibitors. J Med Chem 2004;47(18):4494-506
   PubMed Web of Science ®Google Scholar
• Callahan JF, Burgess JL, Fornwald JA, Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). J Med Chem 2002;45(5):999-1001
   PubMed Web of Science ®Google Scholar
• Singh J, Chuaqui CE, Boriack-Sjodin A, Successful shape-based virtual screening: the discovery of a potent inhibitor of the type 1 TGF-beta receptor kinase (TGF-betaR1). Bioorg Med Chem Lett 2003;13(24):4355-9
   PubMed Web of Science ®Google Scholar
• Biogen Idec MA, Inc. Pyrimidinylpyrazoles as TGF-beta inhibitors. WO2006/026305; 2006
   Google Scholar
• Biogen Idec MA, Inc. Spiro compounds as antagonists of TGF-beta. WO2009/009059; 2009
   Google Scholar
• Eli Lilly and Company. Fused pyrazole derivatives as TGF-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms. WO2005/092894; 2005
   Google Scholar
• Eli Lilly and Company. TGF-beta inhibitors. WO2006/052568; 2006
   Google Scholar
• Eli Lilly and Company. A pyridin quinolin substituted pyrrolo [1,2-B] pyrazole monohydrate as TGF-beta inhibitor. WO2007/018818; 2007
   Google Scholar
• Pfizer Products, Inc. Therapeutic pyrazolyl thienopyridines. WO2008/047198; 2008
   Google Scholar
• In2gen Co., Ltd. 2-Pyridyl substituted imidazoles as ALK5 and/or Alk4 inhibitors. US2008319022; 2008
   Google Scholar
• In2gen Co., Ltd. 2-Pyridyl substituted imidazoles as ALK5 and/or Alk4 inhibitors. WO200530028; 2005
   Google Scholar
• Biogen Idec MA, Inc. Pyrimidinylimidazoles as TGF-beta inhibiors. WO2006/026306; 2006
   Google Scholar
• Biogen Idec MA, Inc. Transforming growth factor modulator. WO2007/076086; 2007
   Google Scholar
• Biogen Idec MA, Inc. Transforming growth factor modulator. WO2007/076127; 2007
   Google Scholar
• Taisho Pharmaceutical Co., Ltd. Thiazole derivative. US2007/01854428; 2007
   Google Scholar
• Merck Patent GMBH. Triazabenzo[E]azulene derivatives for the treatment of tumors. WO2008/052628; 2008
   Google Scholar
• Merck Patent GMBH. Triazolderivate. DE102005061840; 2005
   Google Scholar
• Biogen Idec MA, Inc. Imidazolone compounds and methods of making and using the same. WO2008094556; 2008
   Google Scholar
• Biogen Idec MA, Inc. Furanone compounds and methods of making and using the same. WO2008094574; 2008
   Google Scholar
• Biogen Idec MA, Inc. Substituted pyrazalones. WO2007059359; 2007
   Google Scholar
• Astrazeneca UK Limited. Pyridinyiloxy pyridines as ALK5 inhibitors. WO2009022171; 2009
   Google Scholar
• Astrazeneca AB. Chemical compounds-821. US2009/0048269; 2009
   Google Scholar
• Kirin Beer Kabushiki Kaisha. Compounds having TGF-beta inhibitory activity and pharmaceutical composition containing same. WO2005080377; 2005
   Google Scholar
• Merck Patent GMBH. 5-Cyano-thienopyridines for the treatment of tumors. WO2009049743; 2009
   Google Scholar
• Scios, Inc. Carboxamide inhibitors of TGF-beta. WO2006105222; 2006
   Google Scholar
• Scios, Inc. Quinazoline derivatives as medicaments. WO2005032481; 2005
   Google Scholar
• SK Chemicals Co Ltd. Korea Research Institite of Chemical Technology. Novel Benzopyran derivatives having inhibitory activities against liver fibrosis and cirrhosis and their pharmaceutical uses. WO2006/070984; 2006
   Google Scholar
• Schlingensiepen KH, Fischer-Blass B, Schmaus S, Ludwig S. Antisense therapeutics for tumor treatment: the TGF-beta2 inhibitor AP 12009 in clinical development against malignant tumors. Recent Results Cancer Res 2008;177:137-50
   PubMedGoogle Scholar
• Hau P, Jachmiczak P, Schlingensiepen R, Inhibition of TGF-beta2 with AP 12009 in recurrent malignant gliomas: from preclinical to phase I/II studies. Oligonucleotides 2007;17(2):201-12
   PubMed Web of Science ®Google Scholar
• Schlingensiepen KH, Schlingensiepen R, Steinbrecher A, Targeted tumour therapy with the TGF-beta2 antisense compound AP 12009. Cytokine Growth Factor Rev 2006;17(1-2):129-39
   PubMed Web of Science ®Google Scholar
• Schlingensiepen R, Goldbrunner M, Szyrach MN, Intracerebral and intrathecal infusion of the TGF-b2-specific antisense phospphorothioate oligonucleotide AP 12009 in rabbits and primates: toxycology and safety. Oligonucleotides 2005;15:94-104
   PubMed Web of Science ®Google Scholar
• Stauber AJ, Zimmermann JL, Berridge B. Pathobiology of a valvulopathy in fisher 344 rats given a transforming growth factor-betaR1 kinase inhibitor. Soc toxicol annual meeting 2006; abstract 290
   Google Scholar
• Calvo-Aller E, Baselga J, Glatt S, First human dose escalation study in patients with metastatic malignancies to determine safety and pharmacokinetics of LY2157299, a small molecule inhibitor of the transforming growth factor-beta receptor I kinase. ASCO Annual Meeting 2008
   Google Scholar