Pyrazolobenzamides and derivatives as factor Xa inhibitors

Details Pyrazolobenzamides and derivatives as factor Xa inhibitors Pyrazolobenzamides and derivatives as factor Xa inhibitors

2008-06-03

2008-06-03

Kifle, Bruck (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S119000

Reexamination Certificate

active

07381732

ABSTRACT:
The present application describes pyrazolobenzamides and derivatives thereof of Formula I:in-line-formulae description="In-line Formulae" end="lead"?P4-P-M-M4Iin-line-formulae description="In-line Formulae" end="tail"?or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

REFERENCES:
patent: 6413980 (2002-07-01), Fevig et al.
patent: 6492384 (2002-12-01), Mederski et al.
patent: 6506771 (2003-01-01), Pinto et al.
patent: 2002/0091116 (2002-07-01), Zhu
patent: 2003/0018023 (2003-01-01), Pinto et al.
patent: 2003/0191115 (2003-10-01), Pinto et al.
patent: 1078917 (2001-02-01), None
patent: 1 426 364 (2004-06-01), None
patent: 1 433 788 (2004-06-01), None
patent: WO99/64044 (1999-12-01), None
patent: WO 00/39131 (2000-07-01), None
patent: WO 01/19798 (2001-03-01), None
patent: WO 02/094197 (2002-11-01), None
patent: WO03/024222 (2003-03-01), None
patent: WO 03/026652 (2003-04-01), None
patent: WO 2004/056815 (2004-07-01), None
Tummino, P.J. et al., “The Human Immunodeficiency Virus Type 1 (HIV-1) Nucleocapsid Protein Zinc Ejection Activity of Disulfide Benzamides and Benzisothiazolones: Correlation with Anti-HIV and Virucidal Activities” Feb. 1997, Antimicrobial Agents and Chemotherapy, American Society for Microbiology, pp. 394-400.
Penglie, Zhang et al., “Design, Synthesis and SAR of Monobenzamidines and Aminoisoquinolines as Factor Xa Inhibitors”, Biorganic & Medicinal Chemistry Letters, vol. 12, 2002, pp. 1657-1661.
Akio, Kakefuda et al., “N-Nethylbenzanilide Derivatives as a Novel Class of Selective Vla Receptor Antagonists” Biorganic & Medicinal Chemistry Letters, vol. 12, 2002, pp. 229-232.
Collington, D.M et al., “Internuclear Cyclisation, Part XXV, Aromatisation of Some Spirocyclohexadiene Dimers” J.Chem. Soc, vol. 1968, pp. 1026-1028.
Vasileva et al., “Synthesis and biological activity of acyl derivatives of 4-aminoantipyrine”, Pharm. Chem. J. vol. 17, No. 9, 1983, pp. 633-635.
Wilputte-Steinert, L.P. et al., “Contribution a l'etude de l'action des bases sur les sels d'ammonium quaternaries”, Bull. Soc. Chim. Belges, vol. 78, 1969, pp. 77-88.
Hamuro et al., “Oligoanthranilamdes, Non-Peptide Subunits that Show Formation of Specific Secondary Structure”, J. Am. Chem. Soc., vol. 118, 1996, pp. 7529-7541.
Database Crossfire Beilstein, Database accession No. 3178824 (BRN) & Krasowitzkii; Kotschergina; DANKAS Dok1. Akad, Nauk SSSR; 86; 1952; pp. 1121-1123; Chem. Abstr. 1953, 12319 abstract.
Database Crossfire Beilstein; Database accession No. 8398405 (BRN) & Supuran, Claudiu; Manole, Gheorghe; Schiketanz, Ana; Gheorghiu, Mircea D.; Puscas, loan; RRCHAX Rev. Roum. Chim. 36; 1-3; 1991- 251-255 abstract.
Elodi, S. et al., “Optimization of Conditions for the Catalytic Effect of The Factor IXa—Factor VIII Complex: Probable role of the complex in the amplification of blood coagulation”, Thrombosis Research, vol. 15, pp. 617-629 (1979).

Affiliated with

Also associated with

Rating

Pyrazolobenzamides and derivatives as factor Xa inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Pyrazolobenzamides and derivatives as factor Xa inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyrazolobenzamides and derivatives as factor Xa inhibitors will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2799575