Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Theodore P. Broten"'
Autor:
Roger M. Freidinger, Jerry Di Salvo, RoseAnn P. Price, Randall C. Newton, Richard W. Ransom, Raymond S.L. Chang, Michael A. Patane, Theodore P. Broten, Robert M. DiPardo, Mark G. Bock
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1959-1962
We disclose a new compound class of potent and selective alpha-1A adrenergic receptor antagonists exemplified by the geminally, disubstituted cyclic imide 7. The optimization of lead compounds resulting in the cyclic imide motif is highlighted. The r
Autor:
Robert J. Bendesky, Wai C. Wong, Theodore P. Broten, Fengqi Zhang, Dake Tian, Carlos Forray, James Fang, Sriram Tyagarajan, Dhanapalan Nagarathnam, and Kamlesh P. Vyas, Shou Wu Miao, George Chiu, Mohammad R. Marzabadi, T. G. Murali Dhar, Charles Gluchowski, Kathryn Schneck, Paul J. Kling, Raymond S.L. Chang, Bharat Lagu, Jack Zhang, Wanying Sun, Stacey O'Malley, Tsing B. Chen, Richard W. Ransom, Terry W. Schorn, Charles M. Harrell, John M. Wetzel
Publikováno v:
Journal of Medicinal Chemistry. 42:4764-4777
Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype selectivity for the cloned human alpha(1a) receptor. Systematic modifications of 12 led to identification of highly potent and subtype-selective compounds such as (+
Autor:
Miao Shou Wu, Stacey O'Malley, Kamlesh P. Vyas, Paul J. Kling, Raymond S.L. Chang, Wanying Sun, Wai C. Wong, Richard W. Ransom, Kanyin Zhang, John M. Wetzel, Jian Peng, Charles Gluchowski, Theodore P. Broten, Dhanapalan Nagarathnam, Carlos Forray, Fengqi Zhang, Dake Tian, Bharat Lagu, Tsing B. Chen, Mohammad R. Marzabadi
Publikováno v:
Journal of Medicinal Chemistry. 42:4804-4813
We have previously disclosed dihydropyridines such as 1a,b as selective alpha(1a) antagonists as a potential treatment for benign prostatic hyperplasia (BPH). The propensity of dihydropyridines toward an oxidation led us to find suitable replacements
Autor:
Theodore P. Broten, Jill M. Erb, Mark G. Bock, Jennie B. Nerenberg, Raymond S.L. Chang, Jeffrey M. Bergman, Stacey O'Malley, Ann L. Scott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:291-294
The 4-oxospiro[benzopyran-2,4'-piperidine] ring system is contained within potent class III antiarrhythmic agents. We highlight how these agents can be chemically transformed into a new class of potent (1 nM) and selective (25-fold) alpha 1a-receptor
Autor:
Dhanapalan Nagarathnam, Terry W. Schorn, Wai C. Wong, John M. Wetzel, Carlos Forray, Raymond S.L. Chang, William E. Heydorn, George Chiu, Theodore P. Broten, C. Gluchowski, Xingfang Hong, T. A. Branchek, Shou Wu Miao, James Fang, Mohammad R. Marzabadi
Publikováno v:
Journal of Medicinal Chemistry. 41:5320-5333
We report the synthesis and evaluation of novel alpha1a adrenoceptor subtype-selective antagonists. Systematic modification of the lipophilic 4,4-diphenylpiperidinyl moiety of the dihydropyridine derivatives 1 and 2 provided several highly selective
Autor:
Theodore P. Broten, Wayne J. Thompson, Hee Yoon Lee, Ann L. Scott, Jill M. Erb, Joel R. Huff, Terry W. Schorn, Jennie B. Nerenberg, Raymond S.L. Chang, Tsing B. Chen, James P. Guare, Stacey O'Malley, Peter M. Munson, Jeffrey M. Bergman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2467-2472
Benign prostatic hyperplasia can be managed pharmacologically with alpha-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the alpha-1a receptor subtype may offer advantages in clinical applications with respect to hypotensiv
Autor:
Theodore P. Broten, William J. Greenlee, Robert A. Gabel, Nathan B. Mantlo, Peter K. S. Siegl, Debra Ondeyka, Salah D. Kivlighn, Raymond S.L. Chang, Gloria J. Zingaro, Raymond E. Gibson
Publikováno v:
European Journal of Pharmacology. 294:439-450
L-163,017 (6-[benzoylamino]-7-methyl-2-propyl-3-[(2′-(N-(3-methyl-1-butoxy)carbonylaminosulfonyl)[1,1′]-biphenyl-4-yl]-methyl]-3H-imidazo-[4,5-b] is a potent, orally active, nonpeptide angiotensin II receptor antagonist. Conscious rats and dogs w
Autor:
Robert A. Gabel, Theodore P. Broten, Gloria J. Zingaro, Linda W. Schaffer, Peter K. S. Siegl, Arthur A. Patchett, Terry W. Schorn, William J. Greenlee, Prasun K. Chakravarty, Elizabeth M. Naylor, Salah D. Kivlighn
Publikováno v:
American Journal of Hypertension. 8:58-66
MK-996, N-(4'-(5,7-dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridin-3-yl- methyl)1,1'-biphenyl-2-yl)-sulfonylbenzamide, is a potent, orally active, highly selective, nonpeptide angiotensin II (AII) receptor antagonist. MK-996 prevents the pressor response t
Publikováno v:
Expert Opinion on Investigational Drugs. 3:925-944
Nonpeptide angiotensin II (ANG II) receptor antagonists are a new class of inhibitors of the renin angiotensin system (RAS). Several ANG II receptor antagonists are currently in clinical development for the treatment of hypertension and heart failure
Autor:
Theodore P. Broten, Stacey O'Malley, Jeffrey M. Bergman, Jill M. Erb, Mark G. Bock, Jennie B. Nerenberg, Ann L. Scott, Raymond S.L. Chang
Publikováno v:
ChemInform. 30
The 4-oxospiro[benzopyran-2,4′-piperidine] ring system is contained within potent class III antiarrhythmic agents. We highlight how these agents can be chemically transformed into a new class of potent ( 25-fold) α 1a -receptor subtype adrenergic