Benzodiazepine derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C07D24324, C07D41312, C07D40312, A61K 3155

Patent

active

055569692

ABSTRACT:
Compounds of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or specified optionally substituted alkyl, R.sup.2 is specified optionally substituted phenyl or pyridyl, x is 0, 1, 2 or 3, R.sup.3 is a specified alkyl, halo or amino and R.sup.4 is specified cycoalkyl or bicycloalkyl; and salts and prodrugs thereof, are useful as antagonists of cholecystokin and gastrin receptors.

REFERENCES:
patent: 4820834 (1989-04-01), Evans et al.
patent: 5010076 (1991-04-01), Waldeck et al.
patent: 5218114 (1993-06-01), Bock
patent: 5360802 (1994-11-01), Chambers
Koszykcki, Clin. Neuropharm. 15, Suppl 1, PtB p. 598 (1992).
V. Mutt, "Gastrointestinal Hormones," G. B. J. Green, Ed., Raven Press, NY, pp. 169-221 and G. Nission, ibid pp. 127-167.
Mutt and Jorpes, Biochem. J., 125, 678 (1981).
A. J. Stunkard and E. Stellar, Ed., "Eating and Its Disorders" Raven Press, New York, 1984, p. 67.
A. J. Prange, et al., "Peptides in the Central Nervous System", Ann Repts. Med. Chem. 17, 31, 33 (1982).
J. A. Williams, Biomed, Res. 3 107 (1982).
J. E. Morley, Life, Sci. 30, 479 (1982).
T. H. Moran, et al. "Two Brain cholecystokinin receptors: implications for behavoural actions", Brain Res., pp. 175-179 (1986).
P. L. Faris, et al, Science, 226, 1215 (1984).
M. F. O'Neill, et al., Brain Research, 534 287 (1990).
Rasmusson, et al., 1991, Eur. J. Pharmacol., 209, 135-138.
Woodruff, et al., 1991, Neuropeptides 19, 45-46.
Cervo, et al., 1988, Eur. J. Pharmacol., 158, 53-59.
Singh, et al., 1992, Br. J. Pharmacol., 105, 8-10.
K. Okyama, Hokkaido J. Med. Sci., 206-216 (1985).
Xue, et al., Peptides, 8, 1987, 769-772.
Almegand Eur. J. Pharmacol., 211 (2) 183-187 (1992).
A. Bill, et al., Acta Physiol. Scand., 138 479-485 (1990).
M. Bock, et al., J. Med. Chem., 32, 13-16 (1989).
Coppa, et al., Ann. Surg., 202-203 (1985).
"Chapter 4. Peptides in the Central Nervous System: Focus on Thyrotropin Releasing Hormone and Neurotensin", A. J. Prange, Jr. and C. B. Nemeroff, Annual Reports in Medicinal Chemistry, (1982), vol. 17, pp. 31, 33.
"Cholecystokinin: A Hormone and a Neurotransmitter", J. A. Williams, Biomedical Research (1982), vol. 3, pp. 107-121.
"Minireview--The Ascent of Cholecystokinin (CCK)--from Gut to Brain", J. E. Morley, Life Sciences, (1982), vol. 30, No. 6, pp. 479-493.
"Two brain cholecystokinin receptors: implications for behavioral actions", T. H. Moran, et al., Brain Research, (1986), vol. 362, pp. 175-179.
"Morphine Analgesia Potentiated but Tolerance Not Affected by Active Immunization Against Cholecystokinin", P. L. Faris, et al., Science, (Dec. 1984), vol. 226, pp. 1215-1217.
"Blockade of CCK-B receptors by L-365, 260 induces analgesia in the squirrel monkey", M. F. O'Neill, et al., Brain Research, (1990), vol. 534, pp. 287-290.
"Cholecystokinin (CCK) and schizophrenia: the selective CCKBETA antagonist LY262691 decreases midbrain dopamine unit activity", K. Rasmussen, et al., European Journal of Pharmacology, (1991), vol. 209, pp. 135-138.
"Functional Role of Brain CCK Receptors", G. N. Woodruff, et al., Neuropeptides, (1991), vol. 19, (Suppl.) pp. 45-46.
"8-Hydroxy-2-(di-n-propylamino)tetralin, a selective serotonin 1A receptor agonist, reduces the immobility of rats in the forced swimming test by acting on the nucleus raphe dorsalis", L. Cervo, et al., European Journal of Pharmacology, (1988), vol. 158, pp. 53-59.
"The antagonism of benzodiazepine withdrawal effects by the selective cholecystokininBeta receptor antagonist CI-988", L. Singh, et al., British Journal of Pharmacology, (1992), vol. 105, pp. 8-10.
"Effects of the Anti-Tumor Drugs and Gastrointestinal Hormones on the Growth of the Pancreatic Duct Cell Adenocarcinoma in the Homologous Transplanted Animal Models", K. Okyama, Hokkaido Journal of Medical Science, (1985), pp. 206-216.
"The Influence of Proglumide, a Putative CCK Antagonist, on Cerebral Ischemia in Gerbil", C. Xue, et al., Peptides, (1987), vol. 8, pp. 769-772.
"Cholecystokinin contracts isolated human and monkey iris sphincters; a study with CCK receptor antagonists", B. Almegard, et al., European Journal of Pharmacology, (1992), vol. 211, pp. 183-187.
"Chapter 7 Cholecystokinin: Isolation, Structure, and Functions", Vildor Mutt, Gastrointestinal Hormones, Raven Press, NY, 1980, pp. 169-221;"Chapter 6 Gastrin: Isolation, Characterization, and Functions", Goran Nisson, Gastrointestional Hormones, Raven Press, NY, 1980, pp. 127-167.
"Hormonal Polypeptides of the Upper Intestine", V. Mutt and E. Jorpes, Journal of Biochemistry, (1981), vol. 125, p. 678.
"Gut Hormone Hypothesis of Postprandial Satiety", G. P. Smith, edited by A. J. Stunkard and E. Stellar, Raven Press, NY (1984) pp. 67-75.
Regulatory Peptides, 35 (1991), pp. 1-10, by S. Kawa bata et al. "The Effect of cholecytstokinin receptor antagonists MK-329 and L-365, 260 . . . "
Am. Soc. Pharm. Ex. Ther., 46:943-948. 1994, by S. Patel et al. "Biological Properties of the Benzodiazepine Amidine Derivative L-740, 093 . . . ".
"Cholecystokinin causes contraction of the pupilary sphincter in monkeys but not in cats, rabbits, rats, and guinea-pigs: antagonism by lorglumide", A. Bill, et al., Acta Physiol. Scand., (1990), vol. 138, pp. 479-485.
"Benzodiazepine Gastrin and Brain Cholecystokinin Receptor Ligands: L-365, 260", M. G. Bock, et al., Journal of Medicinal Chemistry, (1989), vol. 32, pp. 13-16.
"Hepatic Resection for Metastatic Colon and Rectal Cancer--An Evaluation of Preoperative and Postoperative Factors", G. F. Coppa, et al., Annual Surgery, (Aug. 1985), vol. 202, pp. 203-208.
"L-365,260, a CCKBeta Antagonist, Blocks CCK-4-Panic in Panic Disorder", D. Koszycki, Clinical Neuropharmacology, (1992), vol. 15, Suppl. 1, Part B, 59B.
Kawabata, Regulatory Peptides 35, pp. 1-10 (1991).
Patel, Molecular Pharm 46, 943 (1994).

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

Benzodiazepine derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.

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

Rate now

     

Profile ID: LFUS-PAI-O-414085

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