Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-06-17
2000-05-02
Stockton, Laura L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514373, 514523, 548210, 548211, 548229, 548230, 558426, A61K 3142, A61K 31425, C07D26322, C07D27506
Patent
active
060573503
ABSTRACT:
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
REFERENCES:
patent: 3193559 (1965-07-01), Regnier et al.
patent: 4593042 (1986-06-01), Liang
patent: 4661491 (1987-04-01), Regnier
patent: 4769371 (1988-09-01), Atwal
patent: 4847379 (1989-07-01), Atwal
patent: 4855301 (1989-08-01), Atwal et al.
patent: 5202330 (1993-04-01), Atwal et al.
patent: 5231179 (1993-07-01), Terashima et al.
patent: 5380737 (1995-01-01), Dunlap et al.
W. C. Wong et al., "Design and Synthesis of Dihydropyrimidines as Alpha 1a Adrenoceptor Selective Antagonists", Abstract No. MEDI 064, 215th ACS National Meeting, Dallas, TX (Mar. 29-Apr. 2, 1998).
B. Lagu et al., "Design, Synthesis and Evaluation of Dihydropyrimidinones as Alpha 1a Selective Antagonists", Abstract No, MEDI 065, 215th ACS National Meeting, Dallas, TX (Mar. 29-Apr. 2, 1998).
D. Nagarathnam et al., "Design, Synthesis and Evaluation of Dihydropyrimidinones as Alpha 1a Selective Antagonists: 6, Synthesis and Structure-Activity Relationship of SNAP 6553 and Analogs", Abstract No. MEDI 066, 215th ACS National Meeting, Dallas, TX (Mar.-Apr. 2, 1998).
M. R. Marzabadi et al, "Design, Synthesis and Evaluation of Dihydropyrimidinones and Dihydropyrimidines as Alpha 1a Selective Antagonists: Modification of the Diarylpiperidine Moiety", Abstract No. MEDI 067, 215th ACS National Meeting, Dallas, TX (Mar. 29-Apr. 2, 1998).
Derwent CPI Abstracts No. 90-041598, "Remedy for Dysuria", Abstract of JP01-319418, Nippon Chemifar (1990).
Derwent CPI Abstracts No. 87-027600, "New 1,3-oxazolidin-2-one derivatives", Abstract of JP61-286375, Nippon Chemifar (1987).
G. C. Rovnyak et al., "Dihydropyrimidine Calcium Channel Blockers. 4. Basic 3-Substitutued-4-aryl-1, 4-dihydropyrimidine-5-carboxylic Acid Esters. Potent Antihypertensive Agents", J. Med. Chem., 35(17), 3254-63 (1992).
K. S. Atwal et al., "Dihydropyrimidine Calcium Channel Blockers. 3. 3-Carbamoyl-4-aryl-1,2,3,4-tetrahydro-6-methyl-5-pyrimidinecarboxylic Acid Esters as Orally Effective Antihypertensive Agents", J. Med. Chem., 34(2), 806-11 (1991).
K. S. Atwal et al., "Dihydropyrimidine Calcium Channel Blockers. 2. 3-Substituted-4-aryl-1, 4-dihydro-6-methyl-5-pyrimidinecarboxylic Acid Esters as Potent Mimics of Dihydropyridines", J. Med. Chem., 33(9), 2629-35 (1990).
K. S. Atwal et al., "Substituted 1,4-Dihydropyrimidines. 3. Synthesis of Sellectively Functionalized 2-Hetero-1,4-dihydropyrimidines", J. Org. Chem., 54(25), 5898-907 (1989).
Bock Mark G.
Lagu Bharat
Nagarathnam Dhanapalan
Patane Michael A.
Wong Wai C.
Merck & Co. , Inc.
Stockton Laura L.
Synaptic Pharmaceutical Corp.
Walton Kenneth R.
Winokur Melvin
LandOfFree
Alpha 1a adrenergic receptor 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 Alpha 1a adrenergic receptor antagonists, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Alpha 1a adrenergic receptor antagonists will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1594204