Anti-cancer cyclopenta [ g ]quinazonline compounds

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

C544S249000

Reexamination Certificate

active

08063056

ABSTRACT:
Cyclopenta[g]quinazolines of the formula (I):—wherein:A is a group OR or NR0R1wherein R0and R1are each independently hydrogen C1-4alkyl, C3-4alkenyl, C3-4alkynyl, C2-4hydroxyalkyl, C2-4halogenoalkyl or C1-4cyanoalkyl, or R0and R1together with the intermediate N form a five- or six-membered heterocyclic ring;p is an integer in the range 1 to 4;R2is hydrogen, C1-4alkyl, C3-4alkenyl, C3-4alkynyl, C2-4hydroxyalkyl, C2-4halogenoalkyl or C1-4cyanoalkyl;Ar1is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4alkyl and C1-4alkoxy; andR3is a group of one of the following formulae:in-line-formulae description="In-line Formulae" end="lead"?-A1-Ar2-A2-Y1-A5-CON(R)CH(Y4)Y5-A8-X—Ar4in-line-formulae description="In-line Formulae" end="tail"?and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.

REFERENCES:
patent: 5747499 (1998-05-01), Bavetsias et al.
patent: 7297701 (2007-11-01), Bavetsias et al.
patent: 7528141 (2009-05-01), Bavetsias et al.
patent: 7705006 (2010-04-01), Bavetsias et al.
patent: WO 94/11354 (1994-05-01), None
patent: WO 94 11354 (1994-05-01), None
patent: WO 95 30673 (1995-11-01), None
patent: WO 00 50417 (2000-08-01), None
Bavetsias, V. et al; “Design and Synthesis of Cyclopenta'g!quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents”;Journal of Medicinal Chemistry, American Chemical Society, Wash., US, vol. 43, No. 10, 2000, pp. 1910-1926-26; XP002187697.
Melin, C. et al; “Novel cyclopenta'g!quinazoline dipeptide antifolates: Thymidylate synthase inhibitors with activity independent of the reduced folate carrier and folylpolyglutamate synthetase”,Chemistry and Biology of Peteridines and Folates; 1997, Proceedings of the Int'l Symposium on Pteridines and Folates, 11th, Berchtesgaden, Germany; Eds. Pfleiderer, Wolfgang; Rokos, Hartmut; Publ.: Blackwell Wissenschafts-VErlag; Jun. 15-20, 1997, pp. 139-144, XP009000407.
Bavetsias, V. , et al; “Synthetis and antitumour activity of cyclopenta'g!quinazoline-based antifolates, a novel class of thymidylate synthase (TS) inhibitors”;Chemistry and Biology of Pteridines and Folates 1997, Proceedings of the Int'l Symposium on Pteridines and Folates, 11th, Berchtesgaden, Germany, Eds.: Pfleiderer, Wolfgang; Rokos, Hartmut; Publ.: Blackwell Wissenschafts-Verlag, Jun. 15-20, 1997, pp. 205-208, XP009000408.
Roth, K.D., et al; “Nicholas Reactions of Amines”;Tetrahedron Letters(1993) vol. 34, No. 18, pp. 2919-2911.
Theti et al;Clinical Cancer Research, vol. 5, Nov. 1999 (Supplemental) at #566.
Jackman et al;Proceedings of the American Association for Cancer Research, 41, Mar. 2000 at #33.
Sausville, E.A., et al; “Contributions of Human Tumor Xenografts to Anticancer Drug Development”;Cancer Res.; vol. 66, No. 7; pp. 3351-3354 (2006).
Johnson, J., et al; “Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials”;British Journal of Cancer; vol. 84, No. 10; pp. 1424-1431 (2001).
Campbell, I.G., et al; “Folate-binding Protein Is a Marker for Ovarian Cancer”;Cancer Research; vol. 51; pp. 5329-5338 (1991).

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

Anti-cancer cyclopenta [ g ]quinazonline 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 Anti-cancer cyclopenta [ g ]quinazonline compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Anti-cancer cyclopenta [ g ]quinazonline compounds will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-4308109

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