Heterocyclic sulfonamide inhibitors of beta amyloid...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C548S313100

Reexamination Certificate

active

11035005

ABSTRACT:
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia:wherein, R1is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3is hydrogen, lower alkyl, or substituted lower alkyl; R4is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7or N; and R7is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

REFERENCES:
patent: 5593846 (1997-01-01), Schenk et al.
patent: 5703129 (1997-12-01), Felsenstein et al.
patent: 5741794 (1998-04-01), Bowles et al.
patent: 5852007 (1998-12-01), Chatterjee
patent: 6218418 (2001-04-01), Pevarello et al.
patent: 6248775 (2001-06-01), Vazquez et al.
patent: 6610734 (2003-08-01), Kreft et al.
patent: 6657070 (2003-12-01), Resnick
patent: 6878742 (2005-04-01), Kreft et al.
patent: 652009 (1995-05-01), None
patent: 1088821 (2001-04-01), None
patent: WO-9912910 (1999-03-01), None
patent: WO-98/22493 (1998-05-01), None
patent: WO-00/50391 (2000-08-01), None
patent: WO-01/23379 (2001-04-01), None
patent: WO-01/27091 (2001-04-01), None
patent: WO-01/27108 (2001-04-01), None
patent: WO-01/70677 (2001-09-01), None
patent: WO-01/94318 (2001-12-01), None
patent: WO-02/057252 (2002-07-01), None
patent: WO-03/050062 (2003-06-01), None
Augelli-Szafran et al., “β-amyloid as a target for Alzheimer's Disease therapy”,Annual Reports in Medicinal ChemistryCh. 3 1999 pp. 21-30.
Dodart et al., “The beta-amyloid precursor protein and its derivatives: from biology to learning and memory processes”,Rev. Neurosci. 2000 11(2-3):75-93.
Dovey et al., “Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain”,J. Neurochem. Jan. 2001 76(1):173-181.
Esler et al., “Transition-state analogue inhibitors of gamma-secretase bind directly to presenilin-1”,Nat. Cell Biol.Jul. 2000 2(7):428-434.
Ghosh et al., “Design of Potent Inhibitors for Human Brain Memapsin 2 (-Secretase)”,J. Am. Chem. Soc.Apr. 12, 2000 122(14):3522-3523.
Goate, “Monogenetic determinants of Alzheimer's disease: APP mutations”,Cell Mol. Life Sci. Sep. 1998 54(4):897-901.
Josien, “Recent advances in the development of gamma-secretase inhibitors”,Curr. Opin. Drug Disc. Dev.Jul. 2002 5(4):513-525.
Larner et al., “Review—Central and peripheral nervious systems—Alzheimer's disease: Towards therapeutic manipulation of the amyloid precursor protein and amyloid peptides”,Exp. Opin. Ther. Patents1997 7(10):1115-1127.
Li et al., “Photoactivated—secretase inhibitors directed to the active site covalently label presenilin 1”,NatureJun. 8, 2000 405(6787):689-694.
Li et al., “The amyloid precursor protein of Alzheimer disease in human brain and blood”,J. Leukocyte Biol. Oct. 1999 66(4):567-574.
Moore et al., “Inhibiton of β-amyloid formation as a therapeutic strategy”,Exp. Opin. Ther. Patents1999 9(2):135-146.
Naslund et al., “Correlation between elevated levels of amyloid beta-peptide in the brain and cognitive decline”,J. Am. Med. Assoc.Mar. 22-29, 2000 283(12):1571-1577.
Olson et al., “Chapter 4. Secretase inhibitors as therapeutics for Alzheimer's Disease”,Ann. Reprts in Med. Chem. 2000 35:31.
Rishton et al., “Fenchylamine sulfonamide inhibitors of amyloid beta peptide production by the gamma-secretase proteolytic pathway: potential small-molecule therapeutic agents for the treatment of Alzheimer's disease”,J. Med. Chem. Jun. 15, 2000 43(12):2297-2299.
Roggo, “Inhibition of BACE, a promising approach to Alzheimer's disease therapy”,Curr. Top. Med. Chem. Apr. 2002 2(4):359-370.
Sabbagh et al., “62 -amyloid and treatment opportunities for Alzheimer's Disease”,Alzheimer's Disease Review1997 3:1-19.
Sinha et al., “Purification and cloning of amyloid precursor protein beta-secretase from human brain”,NatureDec. 2, 1999 402(6761):537-540.
Small et al., “Alzheimer's disease and the amyloid beta protein: What is the role of amyloid?”,J. Neurochem. Aug. 1999 73(2):443-449.
Tung et al., “Design of substrate-based inhibitors of human beta-secretase”,J. Med. Chem. Jan. 17, 2002 45(2):259-262.
Varghese et al., “Alzheimer's disease: Recent advances on the amyloid hypothesis”,Ann. Reports Med. Chem. 1997 32:11-20.
Findeis et al., “Modified-peptide inhibitors of amyloid β-peptide polymerization”,Biochem. May 1999 38(21):6791-6800.
Lu et al., “Indium-mediated organometallic reactions in aqueous media. Stereoselectivity in the crotylation of sulfonimines bearing a proximal chelating group”,J. Org. Chem. May 18, 2001 66(10):3467-3473.
Saha et al., “Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization”,Bioorg. Med. Chem. Lett. Oct. 2, 2000 10(19):2175-2178.

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

Heterocyclic sulfonamide inhibitors of beta amyloid... does not yet have a rating. At this time, there are no reviews or comments for this patent.

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

Rate now

     

Profile ID: LFUS-PAI-O-3916225

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