The Record: File 452 (cont'd)
Ric,
Thanks for the info from Prous Science Drug Data Report.
You indicated in your notes that this file has patent information. Is there more than I received before? If so, please pass it along.
Thanks,
Sharon
I can see by printing out the complete record that there is plenty of patent information. The record even has information on the patent family. These patent references will be good for follow up for Sharon.
I shall also send the pharmacology section. The "Action" portions also contain the chemical structure images.
Review the Action and Patent portions of the record and then go to the next page.
ACTION: Antiangiogenic agent that acts by inhibiting vascular
endothelial growth factor (VEGF) receptor tyrosine kinase (IC50 =
0.1-0.26 mcM). In vivo, compound was shown to inhibit tumor growth in
nude mice bearing s.c.-implanted human epidermoid carcinoma A-431 tumors
(T/C x 100 = 21, 16 and 9 at 25, 50 and 100 mg/kg/day p.o., respectively).
Within this series of phthalazine derivatives, the following are also
specifically claimed:271218, 271220, 271221, 271222, 271223, 271224,
271225, 271226, 271228, 271230, 271231, 271233, 271234, 271235, 271236,
271237, 271238, 271241, 271243. (Drug Data Report, Vol. 21, No. 2, p.
175, 1999)
ACTION: Orally active antineoplastic agent with inhibitory
activity against vascular endothelial growth factor (VEGF) receptor
tyrosine kinase (IC50 = 0.1-0.26 mcM) and high selectivity over kinases
from other receptor families including epidermal growth factor (EGF),
fibroblast growth factor (FGF-1, FGF-2), Tek, c-Src, v-Abl and protein
kinase C (PKC). In the submicromolar range, compound also inhibited KDR
and platelet-derived growth factor (PDGF) receptor autophosphorylation,
the proliferation of human umbilical vein endothelial cells (HUVEC) and
the sprouting of rat aortic pieces cultured in a fibrin gel. Compound did
not have any cytotoxic or antiproliferative activity against cells not
expressing VEGF receptors. At doses of 12.5-50 mg/kg/day p.o., it
dose-dependently inhibited VEGF- and PDGF- induced angiogenesis in an in
vivo mouse growth factor implant model and inhibited tumor growth in nude
mice bearing s.c.-implanted human epidermoid carcinoma A-431 tumors or
VEGF-dependent human ovarian carcinoma SKOV3. Preliminary data from a
phase I clinical study in advanced cancer patients demonstrated that
compound is well tolerated, is rapidly absorbed with a tmax of 1.1- 2.0 h,
has a terminal half-life of 4.5 h and is not associated with accumulation
following once-daily dosing. (Drug Data Report, Vol. 21, No. 2, p. 175,
1999 Drug Data Report, Vol. 22, No. 2, p. 188, 2000)
Previously Published in: Drug Data Report, Vol. 21, No. 2, p. 175, 1999
Drug Data Report, Vol. 22, No. 2, p. 188, 2000
Drugs of the Future, Vol. 27, No. 1, p. 43, 2002
Patents:
PHTHALAZINES WITH ANGIOGENESIS INHIBITING ACTIVITY
AUTHOR(s): Traxler, P., Frei, J., Wood, J., Bold, G., Altmann, K.-H.,
Mett, H., Stover, D.R.
APPLICANT(s): Novartis
FAMILY: 0970070 [EP 0970070] European Patent Office, January
12, 2000
5-01508800 [JP 501508800]Japan, July 3, 2001
[US 2002091261]United States of America, July
11, 2002
[US 2003191129]United States of America,
October 9, 2003
6,258,812 [US 6258812] United States of America, July
10, 2001
6,514,974 [US 6514974] United States of America,
February 4, 2003
6,710,047 [US 6710047] United States of America, March
23, 2004
WO98-035958[WO 9835958] W.I.P.O., August 20, 1998
PRIORITY: 315 [CH 97315] Switzerland, February 13, 1997
PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES
AUTHOR(s): Manley, P.W., Frei, J., Bold, G., Heng, R., Wood, J.M.,
Dawson King, J., Wietfeld, B.
APPLICANT(s): Novartis
FAMILY: 1165085 [EP 1165085] European Patent Office, January
2, 2002
[US 2003013718]United States of America,
January 16, 2003
[US 2004142934]United States of America, July
22, 2004
[US 2005176711]United States of America, August
11, 2005
[US 2006217388]United States of America,
September 28, 2006
6,686,347 [US 6686347] United States of America,
February 3, 2004
6,911,440 [US 6911440] United States of America, June
28, 2005
WO00-059509[WO 0059509] W.I.P.O., October 12, 2000
PRIORITY: 603 [CH 99603] Switzerland, March 30, 1999
9916064 [GB 9916064] Great Britain, July 8, 1999
METHOD FOR TREATING OCULAR NEOVASCULAR DISEASES
AUTHOR(s): Wood, J.M., Brazzell, R.K., Campochiaro, P.A., Kane, F.E.
APPLICANT(s): Novartis
FAMILY: 5-02522475 [JP 502522475]Japan, July 23, 2002
WO00-009098[WO 0009098] W.I.P.O., February 24, 2000
PRIORITY: 2-133,855 [US 133855] United States of America, August
13, 1998
IMPROVED TREATMENT OF NEOVASCULARIZATION
AUTHOR(s): Brazzell, R.K.
APPLICANT(s): Novartis
FAMILY: 1570859 [EP 1570859] European Patent Office, September
7, 2005
WO01-074389[WO 0174389] W.I.P.O., October 11, 2001
PRIORITY: 2-191,807 [US 191807] United States of America, March
24, 2000
USE OF 4-PYRIDYLMETHYLPHTHALAZINES FOR CANCER TREATMENT
AUTHOR(s): Dugan, M.H., Wood, J.M.
APPLICANT(s): Novartis
FAMILY: 1712234 [EP 1712234] European Patent Office, October
18, 2006
WO03-022282[WO 0322282] W.I.P.O., March 20, 2003
PRIORITY: 2-318,694 [US 318694] United States of America,
September 12, 2001
2-331,025 [US 331025] United States of America,
September 12, 2001
2-322,044 [US 322044] United States of America,
September 14, 2001
2-388,163 [US 388163] United States of America, June
12, 2002
USE OF C-KIT INHIBITORS FOR THE TREATMENT OF MYELOMA
AUTHOR(s): Anderson, K.C.
APPLICANT(s): Dana-Farber Cancer Institute, Novartis
FAMILY: WO03-028711[WO 0328711] W.I.P.O., April 10, 2003
PRIORITY: 2-325,491 [US 325491] United States of America,
September 27, 2001
COMBINATIONS COMPRISING A SELECTIVE CYCLOOXYGENASE-2 INHIBITOR
AUTHOR(s): Wood, A.W., Lassota, P., Chen, Y.-N.P.
APPLICANT(s): Novartis
FAMILY: WO03-035047[WO 0335047] W.I.P.O., May 1, 2003
PRIORITY: 2-344,734 [US 344734] United States of America,
October 25, 2001
2-344,735 [US 344735] United States of America,
October 25, 2001
2-336,033 [US 336033] United States of America,
November 15, 2001
USE OF 4-PYRIDYLMETHYL-PHTHALAZINE DERIVATIVES FOR THE MANUFACTURE OF
A
MEDICAMENT FOR THE TREATMENT OF MYELODYSPLASTIC SYNDROMES
AUTHOR(s): Dugan, M.H., List, A.
APPLICANT(s): Novartis, University of Arizona
FAMILY: 5-06502195 [JP 506502195]Japan, January 19, 2006
WO04-028542[WO 0428542] W.I.P.O., April 8, 2004
PRIORITY: 2-413,176 [US 413176] United States of America,
September 24, 2002
TREATMENT OF AMM
AUTHOR(s): Giles, F.
APPLICANT(s): Novartis
FAMILY: 5-06503874 [JP 506503874]Japan, February 2, 2006
WO04-033042[WO 0433042] W.I.P.O., April 22, 2004
PRIORITY: 2-417,622 [US 417622] United States of America, October
10, 2002
TREATMENT OF VON HIPPEL LINDAU DISEASE
AUTHOR(s): Kaelin, W.
APPLICANT(s): Dana-Farber Cancer Institute
FAMILY: 1581228 [EP 1581228] European Patent Office, October
5, 2005
5-06512360 [JP 506512360]Japan, April 13, 2006
[US 2006252763]United States of America,
November 9, 2006
WO04-056367[WO 0456367] W.I.P.O., July 8, 2004
PRIORITY: 2-435,049 [US 435049] United States of America,
December 20, 2002
2-538,990 [US 538990] United States of America, June
21, 2006
INHIBITORS OF THE MUTANT FORM OF KIT
AUTHOR(s): Fabbro, D., Buchdunger, E.
APPLICANT(s): Novartis
FAMILY: 1686997 [EP 1686997] European Patent Office, August 9,
2006
WO05-049032[WO 0549032] W.I.P.O., June 2, 2005
PRIORITY: 2-520,714 [US 520714] United States of America,
November 18, 2003
COMPOSITIONS AND USE FOR TYROSINE KINASE INHIBITORS TO TREAT PATHOGENIC
INFECTION
AUTHOR(s): Bornmann, W.G., Kalman, D., Sherman, M.A., Reeves, P.M.,
Swimm, A.I.
APPLICANT(s): Emory University
FAMILY: 1725295 [EP 1725295] European Patent Office, November
29, 2006
WO05-072826[WO 0572826] W.I.P.O., August 11, 2005
PRIORITY: 2-537,960 [US 537960] United States of America, January
21, 2004
2-553,681 [US 553681] United States of America, March
16, 2004
2-614,203 [US 614203] United States of America,
September 29, 2004
COMBINATIONS OF A VEGF RECEPTOR INHIBITOR WITH OTHER THERAPEUTIC AGENTS
AUTHOR(s): Manley, P.W., Bold, G., Wood, J.M., Kinder, F.R., Lane, H.,
Latour, E.J., Brueggen, J.B., Huang, J.M.-J.
APPLICANT(s): Novartis
FAMILY: 1667721 [EP 1667721] European Patent Office, June 14,
2006
WO05-027973[WO 0527973] W.I.P.O., March 31, 2005
PRIORITY: 2-505,255 [US 505255] United States of America,
September 23, 2003
COMBINATION OF A VEGF RECEPTOR INHIBITOR WITH A CHEMOTHERAPEUTIC AGENT
AUTHOR(s): Manley, P.W., Bold, G., Wood, J.M., Kinder, F.R. Jr., Lane,
H., Latour, E.J., Brueggen, J.B., Huang, J.M.-J.
APPLICANT(s): Novartis
FAMILY: 1682181 [EP 1682181] European Patent Office, July 26,
2006
WO05-027972[WO 0527972] W.I.P.O., March 31, 2005
PRIORITY: 2-505,250 [US 505250] United States of America,
September 23, 2003
PHARMACEUTICAL COMBINATION COMPRISING A CDK INHIBITOR AND A VEGF
RECEPTOR
INHIBITOR
AUTHOR(s): Siemeister, G.
APPLICANT(s): Schering AG
FAMILY: 1568368 [EP 1568368] European Patent Office, August 31,
2005
PRIORITY: 0490071 [EP 0490071] European Patent Office, February
26, 2004
COMBINATION OF ONCOLYTIC VIRUSES WITH ANGIOGENESIS INHIBITORS
AUTHOR(s): Iggo, R., McLaughlin, F., Fuerer, C., Homicsko, K.G.,
Lukashev, A.N.
APPLICANT(s): BTG
FAMILY: WO06-075165[WO 0675165] W.I.P.O., July 20, 2006
PRIORITY: 05658 [GB 05658] Great Britain, January 13, 2005
05659 [GB 05659] Great Britain, January 13, 2005
COMBINATION COMPRISING AN AGENT DECREASING VEGF ACTIVITY AND AN AGENT
DECREASING EGF ACTIVITY
AUTHOR(s): Traxler, P., Bold, G., Wood, J.M., Brandt, R.
APPLICANT(s): Novartis
FAMILY: 2427184 [CA 2427184] Canada, May 30, 2002
1339458 [EP 1339458] European Patent Office, September
3, 2003
5-04513964 [JP 504513964]Japan, May 13, 2004
[US 2004034026]United States of America,
February 19, 2004
[US 2006270665]United States of America,
November 30, 2006
WO02-041882[WO 0241882] W.I.P.O., May 30, 2002
PRIORITY: 0028467 [GB 0028467] Great Britain, November 22, 2000
0121813 [GB 0121813] Great Britain, September 10, 2001
USE OF VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR INHIBITORS FOR THE
TREATMENT OF GASTROINTESTINAL, GENITOURINARY, LYMPHOID AND PULMONARY
CANCERS
AUTHOR(s): Lebwohl, D., Berg, W., Kay, A.
APPLICANT(s): Novartis
FAMILY: WO06-113172[WO 06113172] W.I.P.O., October 26, 2006
PRIORITY: 2-670,870 [US 670870] United States of America, April
13, 2005
2-680,396 [US 680396] United States of America, May 12,
2005
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