Compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C544S117000

Reexamination Certificate

active

07902189

ABSTRACT:
There is provided a compound of formula I:or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.

REFERENCES:
patent: 4560685 (1985-12-01), Roch et al.
patent: 5990117 (1999-11-01), Pamukcu et al.
patent: 6894005 (2005-05-01), Maetzke et al.
patent: 2003/0187026 (2003-10-01), Li et al.
patent: 2008/0194546 (2008-08-01), Hummersone et al.
patent: 45790 (1974-12-01), None
patent: 1252783 (1989-04-01), None
patent: 2242162 (1972-08-01), None
patent: 0185259 (1986-06-01), None
patent: 1277738 (2003-01-01), None
patent: 97/22596 (1997-06-01), None
patent: 97/30035 (1997-08-01), None
patent: 97/32856 (1997-09-01), None
patent: 98/13354 (1998-04-01), None
patent: 98/35985 (1998-08-01), None
patent: 99/02166 (1999-01-01), None
patent: 00/40529 (2000-07-01), None
patent: 00/41669 (2000-07-01), None
patent: 00/47212 (2000-08-01), None
patent: WO 01/17972 (2001-03-01), None
patent: 01/60814 (2001-08-01), None
patent: 01/32651 (2001-10-01), None
patent: 01/92224 (2001-12-01), None
patent: 02/04434 (2002-01-01), None
patent: 02/08213 (2002-01-01), None
patent: WO 2004/052890 (2004-06-01), None
patent: WO 2004/099159 (2004-11-01), None
patent: WO 2006/069805 (2006-07-01), None
patent: WO 2006/135993 (2006-12-01), None
patent: WO 2007/060404 (2007-05-01), None
Nishikawa et al, Chem. Pharm. Bull. 24(9), 2057-2077, (1976).
Malagu et al. “The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase” Bioorganic & Medicinal Chemistry Letters 19(20): 5950-5953 (2009).
Brunn et al. “Direct inhibition of the signaling functions of the mammalian target of rapamycin by the phosphoinositide 3-kinase inhibitors, wortmannin and LY294002” EMBO J, 15(19):5256-5267 (1996).
Chiu et al. “RAPT1, a Mammalian Homolog of Yeast Tor, Interacts with the FKBP12/ Rapamycin Complex” Proc Natl Acad Sci, 91(26):12574-12578 (1994).
Deutsch “In vitro and in vivo experiences with an antiaggregating agent SH-869 SU” International Congress Series (Platelets, Proc. Int. Symp. Blood Platelets, 1974) 357:319-323 (1975).
Lawrence et al. “Modulation of the protein kinase activity of mTOR” Curr Top Microbiol Immunol, 279:199-213 (2004).
Stocks et al. “Structure-driven HtL: Design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity” Bioorg. Med. Chem. Lett. 15(14):3459-3462 (2005).
Terada et al. “Rapamycin Selectively Inhibits Translation of mRNAs Encoding Elongation Factors and Ribosomal Proteins” Proc Natl Acad Sci, 91(24):11477-11481 (1994).
Abraham “Phosphoinositide 3-kinase related kinases” Current Opin. Immunol. 8:412-418 (1996).
Berge et al. “Pharmaceutical Salts” J. Pharm. Sci. 66(1):1-19 (1977).
Bernadi “PML inhibits HIF-1α translation and neoangiogenesis through repression of mTOR” Nature 442(17):779-785 (2006).
Bjornsti and Houghton “The TOR pathway: a target for cancer therapy” Nature Reviews Cancer 4:335-348 (2004).
Brown et al. “A mammalian protein targeted by G1-arresting rapamycin—receptor complex” Nature 369:756-758 (1994).
Burnett et al. “RAFT1 phosphorylation of the translational regulators p70 S6 kinase and 4E-BP1” Proc. Natl. Acad. Sci. 95:1432-1437 (1998).
Charier et al. “An efficient fluorescent probe for ratiometric pH measurements in aqueous solutions” Angew. Chem. Int. Ed. 43:4785-4788 (2004).
Choo and Blenis “TORgeting oncogene addiction for cancer therapy” Cancer Cell 9:77-79 (2006).
Cristofano and Pandolfi “The multiple roles of PTEN in tumor suppression” Cell 100:387-390 (2000).
Dahia “PTEN, a unique tumor suppressor gene” Endocrine-Related Cancer 7:115-129 (2000).
Easton and Houghton “Therapeutic potential of target of rapamycin inhibitors” Expert Opinion on Therapeutic Targets 8:551-564 (2004).
Edinger et al. “Differential effects of rapamycin on mammalian target of rapamycin signaling functions in mammalian cells” Cancer Research 63:8451-8460 (2003).
Eisen et al. “Everolimus for the prevention of allograft rejec on and vasculopathy in cardiac-transplant recipients” New England Journal of Medicine 349(91:847-858 (2003).
Eshleman et al. “Inhibition of the mammalian taret of rapamycin sensitizes U87 xenografts to fractionated radiation therapy” Cancer Research 62:7291-7297 (2002).
Gingras et al. “Regulation of 4E-BP1 phosphorylation: a novel two-step mechanism” Genes and Development 13:1422-1437 (1999).
Gingras et al. “Regulation of translation initiation by FRAP/mTOR” Genes and Development 15:807-826 (2001).
Griffin et al. “Selective benzopyranone and pyrimido[2,1-α]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: Synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro” Journal of Medicinal Chemistry 48(2):569-585 (2005).
Hay “The Akt-mTOR tango and its relevance to cancer” Cancer Cell 8:179-183 (2005).
Hayakawa et al. “Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110α inhibitors” Bioorganic and Medicinal Chemistry 14(20):6847-6858 (2006).
Huang and Houghton “Inhibitors of mammalian target of rapamycin as novel antitumor agents: From bench to clinic” Curr. Opin. in Invest. Drugs 3:295-304 (2002).
Huang and Houghton “Targeting mTOR signaling for cancer therapy” Curr. Opin. Pharmacol. 3:371-377 (2003).
Jagtap et al. “The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly (ADP-ribose) polymerase-1 (PARP-1)” Bioorg. Med. Chem. Lett. 14:81-85 (2004).
Jeffries et al. “Rapamycin suppresses 5′TOP mRNA translation through inhibition of p70s6k” EMBO J. 16(12):3693-3704 (1997).
Lellek et al. “Straightforward synthesis of axially chiral 1,4-naphthodiazepine derivatives” Synlett 11:1616-1618 (2000).
Morice et al. “A randomized comparison of a sirolimus-eluting stent with a standard stent for coronary revascularization” New England Journal of Medicine 346(23):1773-1780 (2002).
Neuhaus et al. “mTOR inhibitors: An overview” Liver Transplantation 7(6):473-484 (2001).
Nishikawa et al. “Structure-activity relationships of the diuretic activity of triaza- and tetraaza-naphthalene compounds” Chem. Pharm. Bull., 24(9):2057-2077 (1976)—Abstract.
Sabatini et al. “RAFT1: A mammalian protein that binds to FKBP12 in a rapamycin-dependent fashion and is homologous to yeast TORs” Cell 78:35-43 (1994).
Sabers et al. “Isolation of a protein target of the FKBP12-rapamycin complex in mammalian cells” J Biol. Chem. 270(2):815-822 (1995).
Samuels et al “High frequency of mutations of the PIK3CA gene in human cancers” Science 304:554 (2004).
Sarbassov et al. “Rictor, a novel binding partner of mTOR, defines a rapamycin-insensitive and raptor-independent pathway that regulates the cytoskeleton” Current Biology 14: 1296-1302 (2004).
Sawyers “Will mTOR inhibitors make it as cancer drugs?” Cancer Cell 4:343-348 (2003).
Schmelze and Hall “TOR, a central controller of cell growth” Cell 103:253-262 (2000).
Sehgal “Sirolimus: its discovery, biological properties, and mechanism of action” Transplantation Proceedings 35(Suppl 3A):7S-14S (2003).
Sugimoto et al. “An improved method for chlorination of nitrogen-containing p-deficient heteroaromatics using triphenylphosphine and trichloroisocyanuric acid” Heterocycles 65(1):18-85 (2005).
Tanaka et al. “Inhibitors of Acyl CoA:cholesterol O-a

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Compounds does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Compounds will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2652203

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.