Piperidinyl compounds as NK1 or NK2 antagonists

Details Piperidinyl compounds as NK1 or NK2 antagonists Piperidinyl compounds as NK1 or NK2 antagonists

1997-11-26

1999-12-07

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514252, 514318, 514319, 514327, 514331, 514291, 514297, 544336, 544405, 544408, 544409, 546 80, 546102, 546217, 546233, A61K 31445, C07D21152

Patent

active

059984449

ABSTRACT:
Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

REFERENCES:
patent: 3518274 (1970-06-01), Strycker
patent: 3862946 (1975-01-01), Havera
patent: 3906100 (1975-09-01), Havera
patent: 4782061 (1988-11-01), Kruse et al.
patent: 4920116 (1990-04-01), Morgan et al.
patent: 4962113 (1990-10-01), Tsushima et al.
patent: 5236921 (1993-08-01), Emonds-alt et al.
patent: 5434158 (1995-07-01), Shah
patent: 5521199 (1996-05-01), Jacobs et al.
patent: 5534525 (1996-07-01), Miller
patent: 5559131 (1996-09-01), Miller
patent: 5559132 (1996-09-01), Miller
patent: 5567700 (1996-10-01), Miller
patent: 5576333 (1996-11-01), Miller
patent: 5589489 (1996-12-01), Shenvi et al.
patent: 5602138 (1997-02-01), Miller
patent: 5635509 (1997-06-01), Jacobs et al.
patent: 5654299 (1997-08-01), Shenvi et al.
patent: 5677317 (1997-10-01), Miller
patent: 5705505 (1998-01-01), Shenvi et al.
patent: 5710169 (1998-01-01), Russell
patent: 5731309 (1998-03-01), Bernstein et al.
patent: 5739149 (1998-04-01), Jacobs et al.
A. Graham et al., "Isolation and Characterisation of the Human Lung NK-2 Receptor Gene Using Rapid Amplification of cDNA Ends", Biochemical and Biophysical Research Communications, (1991), vol. 177, No. 1, 8-16.
X. Emonds-Alt et al., "Pharmacological Profile and Chemical Synthesis of SR 48968, a Non-Peptide Antagonist of the Neurokinin A (NK2) Receptor", Biorganic & Medicinal Chemistry Letters, (1993), vol. 3, No. 5, 925-930.
D. Aharony et al., "Pharmacologic Characterization of the Novel Ligand [4,5-3H-LEU9]Neurokinin-A Binding to NK-2 Receptors on Hamster Urinary Bladder Membranes", Neuropeptides, (1992), 23, 121-130.
M. Needham et al., "LCR/MEL: A Versatile System for High-Level Expression of Heterologous Proteins in Erythroid Cells", Nucleic Acids Research, (1992), vol. 20, No. 5, 997-1003.
O. E. Fancher et al., "New Analgesic N-Substituted Carboxamides", Analgesic N-Substituted Carboxamides, (1964), 721-725.
A. Onistschenko et al., "Zur Regioselektivitat der nucleophilen Ringoffnung von aktivierten 2-Phenylaziridinen", Chem. Ber., 119, (1986), 2678-2680.
Maggi, C.A. et al., American Review of Respiratory Disease, (Aug. 1991), 144(2), pp. 363-367, abstract only.
K. Nagarajan et al., "Synthesis of trans-N-2-aryl(Heteryl)Ethenamidines", Proc. Indian Acad. Sci. (Chem. Sci.), (1992), vol. 104, No. 3, 383-397.
M. Ichinose et al., "Protection against bradykinin-induced bronchoconstriction in asthmatic patients by neurokinin receptor antagonist", The Lancet, (1992), vol. 340, 1248-1251.
B. G. Advani et al.; Tetrahedron Letters, No. 56, pp. 5825-5828 (1968).
Maggi et al. "Tachykinin receptors and tachykinin recptor antagonists" J. Auton. Pharm. v. 13, pp. 23-93, relevant pp. only, 1993.
Spatola et al. "Amide bond surrogates:pseudopeptides and macrocycles" Tetrahedron v. 44, pp. 821-833, 1988.

Affiliated with

Also associated with

Rating

Piperidinyl compounds as NK1 or NK2 antagonists does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Piperidinyl compounds as NK1 or NK2 antagonists, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Piperidinyl compounds as NK1 or NK2 antagonists will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-824315