Arylalkane-sulfonamides having endothelin-antagonist activity

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

C514S255050, C514S256000, C514S272000, C514S273000, C544S123000, C544S296000, C544S319000

Reexamination Certificate

active

07091201

ABSTRACT:
The invention relates to novel aryl-alkane-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.

REFERENCES:
patent: 0 633 259 (1995-01-01), None
patent: 0 743 307 (1996-11-01), None
patent: 0 882 719 (1998-12-01), None
patent: 1 549 494 (1967-10-01), None
patent: WO 98/57938 (1998-12-01), None
Simone, Oncology: Introduction, Cecil Textbook of Medicine, 20thEdition, vol. 1, pp. 1004-1010, 1996.
Layzer, Degenerative Diseases o the Nervous System, Cecil Textbook of Medicine, 20thEdition, vol. 2, pp. 2050-2057; 1996.
Damasio, Alzheimer's Disease and related Dementias, Cecil Textbook of Medicine, 20thEdition, vol. 2, pp. 1992-1996, 1996.
Arai et al., “Cloning and expression of a cDNA encoding an endothelin receptor”. Nature. Dec. 20-27, 1990; 348(6303):730-732.
Breu et al., “In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors”. FEBS Lett. Nov. 15, 1993;334(2):210-214.
Brown et al., “Isomerizations Akin to the Dimroth Rearrangement .III The Conversion of Simple s-Triazolo[4,3-α]pyrimidines into Their[1,5-α]Isomers”. Aust. J. Chem. 1977, 30:2515-2525.
Brown et al., “Pyrimidne Reactions”. Aust. J. Chem. 1964, 17:794-802.
Crosby et al., “n-Butyl 5-Chloro-2-pyrimidoxyacetate-A Plant Growth Regulator Analog”. J. Org. Chem. 1960, 25:1916-1919.
Gohring et al., “Development of a process to prepare 2-cyanopyrimidine on commercial scale”. Chimia, 1996, 50:538-543.
Jacobsen et al., “Phenylation of pyrimidinones using diphenyliodonium salts”. J. Chem. Soc. Perkin Trans. 1999, 1:3265-3268.
Kempf et al., “Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol”. J Med Chem. Feb. 5, 1993;36(3):320-330.
Kohara et al., “Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres”. J Med Chem. Dec. 20, 1996;39(26):5228-5235.
Koppel et al., “Pyrimidines. X. (Antibiotics. II) Synthesis of Bacimethrin, 2-Methoxy Analog of Thiamine, and Related Alkoxypyrimidines”. J. Org. Chem. 1962, 27:3614-3617.
Maggiali et al. “Effetti Anti H1-Istaminici E Antimuscarinici Di Composti 2-E E-[Benzil-(2-Dimetilaminoetil)Amino]Pirimidinici”. II Farmaco 1988, 43:277-292 (in Italian with English Summary).
March, J. Advanced Organic Chemistry. 4thEd., 1994, p. 499.
McMillen et al., “Endothelins: polyfunctional cytokines”. J Am Coll Surg. May 1995;180(5):621-637.
Neidhart et al., “Discovery of RO 48-5695: A potent mixed endothelin receptor antagonist optimized from Bosentan. Bioorg”. Med. Chem. Lett. 1997, 7:2223-2228.
Neidhart et al., “The discovery of nonpeptide endothelin receptor antagonists. Progression towards Bosentan”. Chimia 1996, 50:519-524.
Nugent et al., “Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV”. J Med Chem. Sep. 24, 1998;41(20):3793-3803.
Ogawa et al., Molecular cloning of a non-isopeptide-selective human endothelin receptor. Biochem Biophys Res Commun. Jul. 15, 1991;178(1):248-255.
Ohlstein et al., Drug. Dev. Res. 1993, 29:108.
Rubanyi et al., “Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology”. Pharmacol Rev. Sep. 1994;46(3):325-415. Review.
Sakurai et al., “Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor”. Nature. Dec. 20-27, 1990;348(6303):732-735.
Sumner et al., Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction. Br J Pharmacol. Nov. 1992;107(3):858-860.
Ueda et al., “Nuleosides. XVII. Pyrimidinyl Amino Acids”. J. Med. Chem. 1963, 6:697-701.
Yamanaka et al., “Preparation of Novel β-Trifluoromethyl vinamidinium Salt and Its Synthetic Application to Trifluoromethylated Heterocycles”. Tetrahedron Lett. 1996, 37:1829-1832.
Yanagisawa et al., “A novel potent vasoconstrictor peptide produced by vascular endothelial cells”. Nature. Mar. 31, 1988;332(6163):411-415.
Zhong et al., “Active-Site-Directed Modification of Subtilisin”. J. Am. Chem. Soc. 1991, 113:2259-2263.

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

Arylalkane-sulfonamides having endothelin-antagonist activity does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Arylalkane-sulfonamides having endothelin-antagonist activity, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Arylalkane-sulfonamides having endothelin-antagonist activity will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3624702

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