Aryl amide derivatives of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d] pyrimidine derivatives useful as ASK1 inhibitors, an evaluation of WO2012080735

Expert Opinion on Therapeutic Patents

Volumn 22, Issue 12, 2012, Pages 1479-1483

  Norman, Peter ^a  

^a NORMAN CONSULTING   (United Kingdom)

Author keywords

Apoptosis; ASK1; ASK1 inhibitor; Inflammation; Neuropathic pain; Osteoarthritis; Pain

Indexed keywords

4 (4 AMINOPIPERIDIN 1 YL) 7H PYRROLO[2,3 D]PYRIMIDINE DERIVATIVE; AMIDE; ANALGESIC AGENT; APOPTOSIS SIGNAL REGULATING KINASE 1; CELECOXIB; FREUND ADJUVANT; PREGABALIN; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ALLODYNIA; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CHEMICAL COMPOSITION; CONTROLLED STUDY; DRUG EFFICACY; DRUG SYNTHESIS; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; HYPERSENSITIVITY; IC 50; MOUSE; NONHUMAN;

AMIDES; ANALGESICS; ANIMALS; ANTI-INFLAMMATORY AGENTS; DRUG DESIGN; HUMANS; MAP KINASE KINASE KINASE 5; MOLECULAR STRUCTURE; NEURALGIA; OSTEOARTHRITIS; PATENTS AS TOPIC; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84869756296     PISSN: 13543776     EISSN: 17447674     Source Type: Journal    
DOI: 10.1517/13543776.2012.718760     Document Type: Article

References (25)

1. Ichijo H, Nishida E, Irie K, et al. Induction of apoptosis by ASK1, a mammalian MAPKKK that activates SAPK/JNK and p38 signaling pathways. Science 1997;275(5296):90-4
2. Matsukawa J, Matsuzawa A, Takeda K, Ichijo H. The ASK1-MAP kinase cascades in mammalian stress response. J Biochem 2004;136(3):261-5
3. Takeda K, Matsuzawa A, Nishitoh H, Ichijo H. Roles of MAPKKK ASK1 in stress-induced cell death. Cell Struct Funct 2003;28(1):23-9
4. Fujisawa T, Takeda K, Ichijo H. ASK family proteins in stress response and disease. Mol Biotechnol 2007;37(1):13-18
5. Kaji T, Yoshida S, Kawai K, et al. ASK3, a novel member of the apoptosis signal-regulating kinase family, is essential for stress-induced cell death in HeLa cells. Biochem Biophys Res Commun 2010;395(2):213-18
6. Takeda K, Shimozono R, Noguchi T, et al. Apoptosis signal-regulating kinase (ASK) 2 functions as a mitogen-activated protein kinase kinase kinase in a heteromeric complex with ASK1. J Biol Chem 2007;282(10):7522-31
7. Iriyama T, Takeda K, Nakamura H, et al. ASK1 and ASK2 differentially regulate the counteracting roles of apoptosis and inflammation in tumorigenesis. EMBO J 2009;28(7):843-53
8. Tobiume K, Matsuzawa A, Takahashi T, et al. ASK1 is required for sustained activations of JNK/p38 MAP kinases and apoptosis. EMBO Rep 2001;2(3):222-8
9. Volynets GP, Chekanov MO, Synyugin AR, et al. Identification of 3Hnaphtho[1,2,3-de]quinoline-2,7-diones as inhibitors of apoptosis signal-regulating kinase 1 (ASK1). J Med Chem 2011;54(8):2680-6
10. Volynets GP, Bdzhola VG, Kukharenko OP, Yarmoluk SM. Identification of ASK1 small-molecule inhibitors. Ukr Biochim J 2010;82(5):41-50
11. Wang BH, Xu GY, Ho PY, et al. Apoptosis signal-regulating kinase 1 inhibition attenuates cardiac myocyte hypertrophy and fibroblast collagen synthesis stimulated by angiotensin IIand TGFbeta: Therapeutic potential of ASK1 inhibitors in myocardial remodelling. Circulation 2011;124:A12344
12. Philpott KL, Brackenborough K, Skaper SD, et al. ASK1 kinase-dead knock-in mice and models of neurodegeneration. Alzheimer's & Dementia J Alzheimer's Association 2008;4(Suppl 4):T229-30
13. Takeda Pharmaceutical Co. Ltd. Fused Heterocyclic Compound. WO2008016131;2008
14. Takeda Pharmaceutical Co. Ltd. Apoptosis Signal-Regulating Kinase 1 Inhibitors. WO2009123986;2009
15. Takeda Pharmaceutical Co. Ltd. Apoptosis Signal-Regulating Kinase 1 Inhibitors. WO2010008843;2010
16. Takeda Pharmaceutical Co. Ltd. Pyrazolo [1, 5-A] Pyrimidine Derivatives As Apoptosis Signal-Regulating Kinase 1 Inhibitors. WO2011041293;2011
17. Takeda Pharmaceutical Co. Ltd. Apoptosis Signal-Regulating Kinase 1 Inhibitors. WO2011097079;2011
18. Gilead Sciences, Inc. Methods for identifying ask1 inhibitors useful for preventing and/or treating cardiovascular diseases. US20070276050;2007
19. Gilead Sciences, Inc. Apoptosis Signal-Regulating Kinase Inhibitors. WO2012003387;2012
20. Gilead Sciences, Inc. Apoptosis Signal-Regulating Kinase Inhibitors. WO2011008709;2011
21. Merck Serono SA. Triazolopyridine compounds and their use as ASK inhibitors. WO2009027283;2009
22. Convergence Pharmaceuticals, Ltd. ASK1 inhibiting pyrrolopyrimidine derivatives. WO2012080735;2012
23. Bamborough P, Drewry D, Harper G, et al. Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem 2008;51(24):7898-914
24. Convergence Pharmaceuticals the pipeline. Available from: Http://www. convergencepharma.com/index.asp? page-id=16
25. Brownlees J, Patel S, Hatcher J, et al. PT 148 Apoptosis Signal-Regulating Kinase (ASK1): A Novel Target For Inflammatory Pain 13th World Congress on Pain 2010 See. Available from: Http://iasp.omnibooksonline.com/ 2010.