Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2001-07-27
2003-04-08
Kifle, Bruck (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S211070, C514S212040, C514S212060, C514S212070, C514S212080, C540S488000, C540S521000, C540S522000, C540S523000, C540S524000, C540S527000
Reexamination Certificate
active
06544978
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease.
REFERENCES
The following publications, patents and patent applications are cited in this application as superscript numbers:
1
Glenner, et al.,
Biochem. Biophys. Res. Commun
., 120:885-890 (1984)
2
U.S. Pat. No. 4,666,829.
3
Selkoe,
Neuron
, 6:487-498 (1991)
4
Goate, et al.,
Nature
, 349:704-706 (1990)
5
Chartier Harlan, et al.,
Nature
, 353:844-846 (1989)
6
Murrell, et al.,
Science
, 254:97-99 (1991)
7
Mullan, et al.,
Nature Genet
., 1:345-347 (1992)
8
Schenk, et al., International Patent Application Publication No. WO 94/10569
, “Methods and Compositions for the Detection of Soluble
&bgr;-
Amyloid Peptide
”, published May 11, 1994
9
Selkoe, Scientific American, “
Amyloid Protein and Alzheimer's Disease
”, pp. 2-8, November, 1991
10
Tetrahedron Letters
, 34(48), 7685 (1993)
11
Losse, et al., Tetrahedron, 27:1423-1434 (1971)
12
Citron, et al., Nature, 360:672-674 (1992)
13
Hansen, et al., J. Immun. Meth., 119:203-210 (1989)
14
U.S. Pat. No. 3,598,859
15
Ogliaruso and Wolfe,
Synthesis of Lactones and Lactams
, Patai, et al. Editor, J. Wiley & Sons, New York, N.Y., USA, pp. 1085 et seq. (1993).
16
Ugi, et al.,
Tetrahedron
, 52(35):11657-11664 (1996)
17
Blade-Font,
Tetrahedron Lett
., 21:2443 (1980).
18
Freidinger, et al.,
J. Org. Chem
., 47:104-109 (1982)
19
Semple, et al.,
J. Med. Chem
., 39:45314536 (1996).
20
Holladay, et al.,
J. Org. Chem
., 56:3900-3905 (1991).
21
Donaruma, et al.,
Organic Reactions
, 11:1-156 (1960)
22
Wolff,
Organic Reactions
, 3:307-336 (1946)
23
Krow, et al.,
J. Org. Chem
., 61:5574-5580 (1996)
24
Tetrahedron
, 35:2433 (1979)
25
Gracias, et al.,
J. Am. Chem. Soc
., 117:8047-8048 (1995)
26
Milligan, et al.,
J. Am. Chem. Soc
., 117:10449-10459 (1995)
27
Miller, et al.,
J. Am. Chem. Soc
., 118:9606-9614 (1996)
28
March,
Advanced Organic Chemistry, Reaction Mechanisms and Structure
, 2nd Edition, McGraw-Hill Book Company, New York, N.Y., USA (1977)
29
Colombo, et al.,
Tetrahedron Lett
., 35(23):4031-4034 (1994)
30
Rogriguez, et al.,
Tetrahedron
, 52:7727-7736 (1996)
31
Parsons, et al.,
Biochem. Biophys. Res. Comm
., 117:108-113 (1983)
32
Watthey, et al.,
J. Med. Chem
., 28:1511-1516 (1985)
33
Armstrong, et al.,
Tetrahedron Lett
., 35:3239 (1994)
34
King, et al.,
J. Org. Chem
., 58:3384 (1993).
35
Hu, et al.,
Tetrahedron Lett
., 36(21):3659-3662 (1995).
36
Wada, et al.,
Bull. Chem. Soc. Japan
, 46:2833-2835 (1973)
37
Gaetzi,
Chem. Abs
., 66:28690m
38
Wheeler, et al.,
Organic Syntheses
, Coll. Vol. VI, p. 840
39
J. Med. Chem
., 28(12) 1886 (1985)
40
Brenner, et al., U.S. Pat. No. 2,938,029
41
Evans, et al.,
J. Am. Chem. Soc
., 112:4011-4030 (1990)
42
Micouin, et al.,
Tetrahedron
, 52:7719-7726 (1996)
43
Butcher, et al.,
Tetrahedron Lett
., 37(37):6685-6688 (1996)
44
M. L. Reupple, et al.,
J. Am. Chem. Soc
., 93:7021 et seq. (1971)
45
P. A. S. Smith,
Organic Reactions
, 3:337-449 (1946)
46
K. Orito, et al.,
Tetrahedron
, 36:1017-1021 (1980)
47
Krimm,
Chem. Ber
., 91:1057 (1958)
48
Suda, et al.,
J. Chem. Soc. Chem Comm
., 949-950, (1994)
49
Barton, et al.,
J. Chem. Soc
., 1764-1767 (1975)
50
Kitagawa, et al.,
J. Am. Chem. Soc
., 117:5169-5178 (1975)
51
Akhatar, et al.,
J. Org. Chem
., 55:5222-5225 (1990)
52
Nedenskov, et al.,
Acta Chem. Scand
., 12:1405-1410 (1958)
53
Sakakida, et al.,
Bull. Chem. Soc. Japan
, 44:478-480 (1971)
54
Hoffman, et al.,
Tet. Lett
., 30:42074210 (1989)
55
Vedejs, et al.,
Tet. Lett
., 33:3261-3
264
(1992)
56
van der Steen, et al.,
Tetrahedron
, 47, 7503-7524 (1991)
57
Hart, et al.,
Chem Rev
., 89:1447-1465 (1989)
58
Lowe, et al.,
Bioorg. Med. Chem. Lett
., 4:2877-2882 (1994)
59
McKennis, Jr., et al.,
J. Org. Chem
., 28:383-387 (1963)
60
Shirota, et al.,
J. Med. Chem
., 20:1623-1627 (1977)
61
Overberger, et al.,
J. Am. Chem. Soc
., 85:3431 (1963)
62
Herschmann,
Helv. Chim. Acta
, 32:2537 (1949)
63
Overberger, et al.,
Macromolecules
, 1:1 (1968)
64
Busacca, et al.,
Tet. Lett
., 33:165-168 (1992)
65
Croisier, et al., U.S. Pat. No. 4,080,449
66
J. A. Robl, et al.,
Tetrahedron Lett
., 36(10):1593-1596 (1995)
67
Flynn, et al.,
J. Med. Chem
., 36:2420-2423 (1993)
68
Orito, et al.,
Tetrahedron
, 36:1017-1021 (1980)
69
Kawase, et al.,
J. Org. Chem
., 54:3394-3403 (1989)
70
Lowe, et al.,
J. Med. Chem
., 37:3789-3811 (1994)
71
Robl, et al.,
Bioorg. Med. Chem. Lett
., 4:1789-1794 (1994)
72
Skiles, et al.,
Bioorg. Med. Chem. Lett
., 3:773-778 (1993)
73
Grunewald, et al.,
J. Med. Chem
., 39(18):3539 (1996)
74
Thomas, et al.,
J. Chem. Soc
., Perkin II, 747 (1986)
75
Warshawsky, et al.,
Bioorg. Med. Chem. Lett
., 6:957-962 (1996)
76
Ben-Ishai, et al.,
Tetrahedron
, 43:439450 (1987)
77
van Niel et al.,
Bioorg. Med. Chem. Lett
., 5:1421-1426 (1995)
78
Kawase, et al.,
J. Org. Chem
., 54:3394-3403 (1989)
79
Edwards, et al.,
Can. J. Chem
., 49:1648-1658 (1971)
80
Milligan, et al.,
J. Am. Chem. Soc
., 117:10449-10459 (1995)
81
Curran et al.,
Tet. Lett
., 36:191-194 (1995)
82
Slusarchyk, et al.,
Bioorg. Med. Chem. Lett
., 5:753-758 (1995)
83
Wyvratt, et al., Eur. Pat. Appl. 61187 (1982)
84
Cornille, et al.,
J. Am. Chem. Soc
., 117:909-917 (1995)
85
Kolc,
Coll. Czech. Chem. Comm
., 34:630 (1969)
86
Dickerman, et al.,
J. Org. Chem
., 14:530 (1949)
87
Dickerman, et al.,
J. Org. Chem
., 20:206 (1955)
88
Dickerman, et al.,
J. Org. Chem
., 19:1855 (1954)
89
Hoffman, et al.,
J. Org. Chem
., 27:3565 (1962)
90
Wasserman, et al.,
J. Am. Chem. Soc
., 103:461-2 (1981)
91
Crombie, et al.,
Tetrahedron Lett
., 27(42):5151-5154 (1986)
92
Yokoo, et al.,
Bull, Chem. Soc. Jap
., 29:631 (1956)
93
Burkholder, et al.,
Biog. Med. Chem. Lett
., 2:231 (1993)
94
Karanewsky, U.S. Pat. No. 4,460,579
95
Kametani, et al.,
Heterocycles
, 2:831-840 (1978)
96
Yanganasawa, et al.,
J. Med. Chem
., 30:1984-1991 (1987)
97
J. Das et al.,
Biorg. Med. Chem. Lett
., 4:2193-2198 (1994)
All of the above publications, patents and patent applications are herein incorporated by reference in their entirety to the same extent as if each individual publication, patent or patent application was specifically and individually indicated to be incorporated by reference in its entirety.
State of the Art
Alzheimer's Disease (AD) is a degenerative brain disorder characterized clinically by progressive loss of memory, cognition, reasoning, judgment and emotional stability that gradually leads to profound mental deterioration and ultimately death. AD is a very common cause of progressive mental failure (dementia) in aged humans and is believed to represent the fourth most common medical cause of death in the United States. AD has been observed in races and ethnic groups worldwide and presents a major present and future public health problem. The disease is currently estimated to affect about two to three million individuals in the United States alone. AD is at Resent incurable. No treatment that effectively prevents AD or reverses its symptoms and course is currently known.
The brains of individuals with AD exhibit characteristic lesions termed senile (or amyloid) plaques, amyloid angiopathy (amyloid deposits in blood vessels) and neurofibrillary tangles. Large numbers of these lesions, particularly amyloid plaques and neurofibrillary tangles, are generally found in several areas of the human brain important for memory and cognitive function in patients with AD. Smaller numbers of these lesions in a more restrictive anatomical distribution are also found in the brains of most aged humans who do not have clinical AD. Amyloid plaques and amyloid angiopathy also characterize the brains of individuals with Trisomy 21 (Down's Syndrome) and Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch Type HCHWA-D). At present, a definitive diagnosis of AD usually requires serving the aforementioned lesions in the brain tissue of patients
Audia James A.
Britton Thomas C.
Cwi Cynthia L.
Dressman Bruce A.
Droste James J.
Athena Neurosciences, Inc.
Burns Doane , Swecker, Mathis LLP
Kifle Bruck
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