Thiophenes useful for modulating the adenosine receptor

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

514258, 514267, 514291, 544250, 544278, 546 80, 546114, A61K 31505, A61K 3144, C07D49502, C07D49512

Patent

active

059394323

ABSTRACT:
The present invention relates to compounds of formulas (IA), (IB), and (IC): ##STR1## the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.

REFERENCES:
patent: 5585385 (1996-12-01), Natsugari et al.
Amoah-Apraku, B. et al., "Selective Potentiation by an A.sub.1 Adenosine Receptor Enhancer of the Negative Dromotropic Action of Adenosine in the Guinea Pig Heart," The Journal of Pharmacology and Experimental Therapeutics, vol. 266, No. 2, pp. 611-617 (1993).
Bhattacharya, Samita et al., "Effects of Long-Term Treatment with the Allosteric Enhancer, PD81,723, n Chinese Hamster Ovary Cells Expressing Recombinant Human A.sub.1 Adenosine Receptors," Molecular Pharmacology, vol. 50, pp. 104-111 (1996).
Bhattacharya, Samita et al., "The Allosteric Enhancer, PD 81,723, Stabilizes Human A.sub.1 Adenosine Receptor Coupling to G Proteins," Biochimica et Biophysica Acta, 1265: pp. 15-21, 1995.
Bruns, Robert et al., "Allosteric Enhancement of Adenosine A.sub.1 Receptor Binding and Function by 2-Amino-3-benzoylthiophenes," Molecular Pharmacology, vol. 38, No. 6, pp. 939-949 (1990).
Bruns, Robert et al., "Structure-Activity Relationships for Enhancement of Adenosine A.sub.1 Receptor Binding by 2-Amino-3benzoylthiophenes," Molecular Pharmacology, vol. 38, pp. 950-958 (1990).
Cao, X et al., "Adenosine A.sub.1 Receptor Enhancer, PD 81,723, and Cerebral Ischemia/Refperfusion Injusry in the Gerbil," General Pharmacology, vol. 26, No. 7, pp. 1545-1548 (1995).
Corral, Carlos et al., "Reacciones de Bischler y de Friedlander con 2-amino-3-aroil-tiofenos", Afinidad, Mar.-Apr. (1978).
Dennis, Don M. et al., "Modulation of Atrioventricular Nodal Function by Metabolic and Allosteric Regulators Endogenous Adenosine in Guinea Pig Heart," Circulation, vol. 94, No. 10, pp. 2551-2559 (1996). Journal Fur praktische Chemie, Band 317, Heft 5, pp. 705-711(1975).
Hromatka, O. et al., "Uber die Nitrierung von 7-Chlor-5-phenyl-1 pp. 709-714 (1973).
Janusz, Cynthia A. et al., "Functional activity of the adenosine binding enhancer, PD 81,723, in the in vitro hippocampal slice", Brain Research, vol. 567, pp. 181-187 (1991).
Kollias-Baker, C. et al., "Novel Approach for Enhancing Atrioventricular Nodal Conduction Delay Mediated by Endogenous Adenosine," Circulation Research, vol. 75, No. 6, pp. 972-980 (1994).
Kollias-Baker, C. et al., "Allosteric Enhancer PD 81,723 Acts by Novel Mechanism to Potentiate Cardiac Actions of Adenosine," Circulation Research, vol. 75, No. 6, 961-971 (1994).
Kollias-Baker, Cynthia, "The Allosteric Enhancer, PD 81,723, Potentiates the Cardiac Effects of Adenosine by Enhancing the Binding of Agonists to A.sub.1 Adenosine Receptors," A Dissertation presented to the Graduate School of the University of Florida (1994).
Leung, E. et al., "Enhancement of Adenosine A.sub.1 Receptor Functions by Benzoylthiophenes in Guinea Pig Tissues in Vitro," Archives of Pharmacology, vol. 352, No. 2, pp. 206-212, (1995).
Mizumura, Tsuneo et al., "PD 81,723, an Allosteric Enhancer of the A.sub.1 Adenosine Receptor, Lowers the Threshold for Ischemic Preconditioning in Dogs," Circulation Research, vol. 79, No. 3, pp. 415-423 (Sep. 1996).
Mudumbi, Ramagopal V. et al., "Cardia Functional Responses to Adensoine by PD 81, 723, an Allosteric Enhancer of the Adenosine A.sub.1 Receptor," American Journal of Physiology, vol. 264, pp. H1017-H1022, 1993.
Nakanishi, Michio et al., "Studies on Pcychotropic Drugs. 18..sup.1 Synthesis and Structure-Activity Relationships of Medicinal Chemistry, vol. 16, No. 3, pp. 214-219 (1973).
Robba, Max et al, "No. 144--Thienopyrimidines. IX--Etude de la Chimique de France, pp. 761-764 (1976).
Corral, Carlos et al., "Reacciones de Bischler y de Friedlander con 2-amino-3-aroil-tiofenos", Afinidad, Mar.-Apr. (1978).
CAS for Routh et al., Tachykinin Receptors In The Spinal Cord, Progress In Brain Research, vol. 104, pp. 93-108, 1995.
CAS for Chesselet et al., Ischemic Damage In The Striatum Of Adult Gerbils: Relative Sparing Of Somatostatinergic And Cholinergic Interneurons Contrasts With Loss Of Efferent Neurons, Experimental Neurology, vol. 110, No. 2, pp. 209-218, Nov. 1990.
CAS for Cragg et al., Tachykinin Antagonists In Carotid Body Responses To Hypoxia And Substance P In The Rat, Respiration Physiology, vol. 95, No. 3, pp. 295-310, Mar. 1994.
CAS for Benedek et al., Potentiation Of Thermoregulatory And Analgesic Effects Of Morphine By Calcium Antagonists, Pharmacological Research Communications, vol. 16, No. 10, pp. 1009-1018, Oct. 1984.
CAS for Ghio et al., Clinical Evaluation of Calcium-Antagonist Drugs, Journal Of Cardiovascular Pharmacology, vol. 20, pp. S71-S74, 1992.
CAS for Zhou et al., Effects Of Calcium Blockers On The Performance Of Left And Right Ventricles During Acute Hypoxia, Sheng Li Hseuh Pao, vol. 44, No. 3, pp. 237-243, Jun. 1992.
CAS for Ueno et al., Simultaneous Determination Of A New Dihydropyridine Calcium Blocker And Its Pyridine Metabolite In Dog Plasma By Column Switching High-Performance Liquid Chromatography With Electrochemical And Ultraviolet Detection, Analytical Scienc, 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

Thiophenes useful for modulating the adenosine receptor does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Thiophenes useful for modulating the adenosine receptor, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Thiophenes useful for modulating the adenosine receptor will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-315036

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