Therapeutic morpholino-substituted 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

C544S125000, C544S151000

Reexamination Certificate

active

07405211

ABSTRACT:
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders, neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer, and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

REFERENCES:
patent: WO 90/06921 (1990-06-01), None
patent: WO 91/19707 (1991-12-01), None
Sosnovskikh et al, Russian Chemical Bulletin, International Edition, vol. 50, No. 3, pp. 453-455, Mar. 2001.
Di Braccio et al., “1,2-fused pyrimidines VII. 3-(Dialkylamino)-1H-pyrimido[1,2-a]quinolin-1-ones and 2-(dialkylamino)-4H-pyrimido[2,1-a]isoquinolin-4-ones as antiplatelet compounds,”European Journal of Medicinal Chemistry(1995), vol. 30, No. 1, pp. 27-38.
Vlahos et al., “A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one(LY294002),”The Journal of Biological Chemistry(1994), vol. 269, No. 7, pp. 5241-5248.
Morris et al., “A novel synthesis of 2-aminochromones via phosgeniminium salts,”Journal of Organic Chemistry(1992), vol. 57, pp. 6502-6508.
Morris et al., “Synthesis and biological activity of a potent antiplatelet 7-aminofurochromone,”Bioorganic and Medicinal Chemistry Letters(1994), vol. 4, No. 21, pp. 2621-2626.
Morris et al., “Synthesis and biological evaluation of antiplatelet 2-aminochromones,”Journal of Medicinal Chemistry(1993), vol. 36, No. 14, pp. 2026-2032.
Benjamin et al., “2-Aminochromones block human platelet aggregation by inhibiting cyclic AMP-dependent phosphodiesterase leading to reduced platelet phospholipase C activity,”The Journal of Pharmacology and Experimental Therapeutics, vol. 265, No. 1, pp. 457-462.
Morris et al., “A cyclodehydration route to 2-aminochromones,”Synthetic Communications(1994), vol. 24, No. 6, pp. 849-858.
Cho et al., “Effects of inclusion complexation on the transepithelial transport of a lipophilic substance in vitro,”Pharmaceutical Research(1995), vol. 12, No. 4, pp. 560-564.
Supplementary European Search Report for EP 01 90 2568 dated Mar. 6, 2003.
Buchmann, Fred., J., et al., “Syntheses in the Quinoline Series. IV. 2, 4-Disubstituted Quinoline Derivatives,”Journal of the American Chemical Society, vol. 64, Jun. 1942, pp. 1357-1360, XP002231191.
Chiosis, Gabriela, et al., “LY294002-Geldanamycin Heterodimers as Selective Inhibitors of the P13K and P13K-Related Family,”Bioorganic&Medicinal Chemistry Letters, 2001, 11, pp. 909-913, XP002231192.
Database Crossfire Beilstein ′Online! Beilstein Institut zur Förderung der Chemischen Wissenchaften, Frankfurt am Main, DE; Database Accession No. BRN 1077329 XP002231193; Abstract, Ingalls, E.A.; Popp, F.D.,Journal of Heterocyclic Chemistry, vol. 4, 1967, pp. 523-526.
Sosnovskikh et al. “2-Polyfluoroalkylchromones 6. Synthesis of substituted 2-morpholino-2-trifluromethylchroman-4-ones,” Russian Chemical Bulletin (2001) 50(3):453-455.

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

Therapeutic morpholino-substituted 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 Therapeutic morpholino-substituted compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Therapeutic morpholino-substituted compounds will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2789731

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