Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Reexamination Certificate
2004-12-27
2010-06-01
Kumar, Shailendra (Department: 1621)
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
C544S238000, C544S336000, C544S356000, C544S358000, C514S242000, C514S252010, C514S252120, C514S252100, C514S272000, C514S336000
Reexamination Certificate
active
07728131
ABSTRACT:
The present invention is directed to an amide derivative having excellent BCR-ABL tyrosine kinase inhibitory activity, or a salt thereof.The present invention provides an amide derivative represented by the following general formula (1):[Chemical 23](wherein R1represents —CH2—R11, etc.; R2represents alkyl, halogen, haloalkyl, etc.; R3represents hydrogen, etc.; Het1 represents a group of the formula [6] as above, etc.; and Het2 represents pyrimidinyl, etc.), or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient.The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.
REFERENCES:
patent: 5521184 (1996-05-01), Zimmermann
patent: 7494997 (2009-02-01), Asaki et al.
patent: 2006/0014742 (2006-01-01), Asaki
patent: O 564 409 (1993-03-01), None
patent: WO 02/22597 (2002-03-01), None
patent: WO 2004/014903 (2004-02-01), None
S. Kimura, et. al., NS-187, a Potent and Selective Dual Bcr-Abl/Lyn Tyrosine Kinase Inhibitor, is a Novel Agent for Imatinib-Resistant Leukemia, Blood, vol. 16, No. 12, 3948-3954 (Dec. 1, 2005).
T. Asaki, et. al., Design and Synthesis of 3-substituted Benzamide Derivatives as Bcr-Abl Kinase Inhibitors, 16 Bioorganic & Medicinal Chemistry Letters 1421-1425 (2006).
R. Parise, et. al., Liquid Chromatographic— Mass Spectrometric Assay for Quantitation of Imatinib and its Main Metabolite (CGP 74588) in Plasma, 791 J. Chromatography B 39-44 (2003).
B. Druker, et. al., Activity of a Specific Inhibitor of the BCR-ABL Tyrosine Kinase in the Blast Crises of Chronic Myeloid Leukemia and Acute Lumphoblastic Leukemia with the Philadelphia Chromosome, N. Engl. J. Med., vol. 344, No. 14, 1038-1042 (Apr. 5, 2001).
M. Gorre, et. al., Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation and Amplification, Science, vol. 293 876-880 (Aug. 3, 2001).
MV Blagosklonny, STI-571 Must Select for Drug-Resistant Cells but ‘No Cell Breathes Fire Out of its Nostrils Like a Dragon’, 16 Leukemia 570-572 (2002).
A. Hochhaus, et. al., Moleculor and Chromosomal Mechanisms of Resistance to Imatinib (STI 1571) Therapy, 16 Leukemia 2190-2196 (2002).
W.K. Hofmann, et. al., Ph+Acute Lymphoblastic Leukemia Resistant to the Tyrosine Kinase Inhibitor STI 1571 has a Unique BCR-ABL Gene Mutation, Blood, vol. 99, No. 5 1860-1862 (Mar. 1, 2002).
M. Deininger, et. al., The Molecular Biology of Chronic Myleoid Leukemia, Blood, vol. 96, No. 10 3343-3356 (Nov. 15, 2000).
Asaki Tetsuo
Segawa Jun
Sugiyama Yukiteru
Kumar Shailendra
Nippon Shinyaku Co. Ltd.
Troutman Sanders LLP
LandOfFree
Amide derivative and medicine does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Amide derivative and medicine, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Amide derivative and medicine will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4200426