Zobrazeno 1 - 10
of 92
pro vyhledávání: '"Raymond S.L. Chang"'
Autor:
Jacquelynn J. Cook, Rodney A. Bednar, Thomayant Prueksaritanont, Yvonne M. Leonard, Michael R. Wood, Qin Mei, Richard W. Ransom, Ronald K. Chang, Emily D. Adarayn, Robert M. DiPardo, Jian Yu, Audrey A. Wallace, Wei Lemaire, Scott D. Kuduk, Kathy L. Murphy, G. R. Sitko, Scott D. Mosser, Christina N. Di Marco, Mark G. Bock, Frank C. Clayton, Bang-Lin Wan, Kathy M. Schirripa, Marie A. Holahan, Roger M. Freidinger, Dennis L. Bohn, Douglas J. Pettibone, Raymond S.L. Chang, Cuyue Tang, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:716-720
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating α-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and
Autor:
Rachel K. Conley, J.K. Webb, Mark G. Bock, Alan Wheeldon, Robert M. DiPardo, Douglas J. Pettibone, Susan Boyce, Raymond S.L. Chang, Tsing-Bau Chen, Carl F. Homnick
Publikováno v:
European Journal of Pharmacology. 527:44-51
This study used behavioural and in vivo electrophysiological paradigms to examine the effects of systemic and spinal administration of a bradykinin B1 receptor antagonist, compound X, on acute nociceptive responses in the rat. In behavioural experime
Autor:
Punam Sandhu, Stacey O'Malley, Michael R. Wood, Tsing-Bau Chen, June J. Kim, Douglas J. Pettibone, Joseph J. Lynch, Wei Han, Gary L. Stump, Roger M. Freidinger, Tanya MacNeil, Bruce D. Dorsey, Richard W. Ransom, E V Lis, Raymond S.L. Chang, Charles M. Harrell, Peter J. Bondiskey, Robert M. DiPardo, Joan D. Ellis, Carl F. Homnick, Kathy L. Murphy, Mark G. Bock, Scott D. Kuduk, Patricia Miller
Publikováno v:
Journal of Medicinal Chemistry. 46:1803-1806
Antagonism of the bradykinin B(1) receptor was demonstrated to be a potential treatment for chronic pain and inflammation. Novel benzodiazepines were designed that display subnanomolar affinity for the bradykinin B(1) receptor (K(i) = 0.59 nM) and hi
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:
Mark G. Bock, Charles Gluchowski, Sriram Tyagarajan, Quanrong Shen, Tsing-Bau Chen, Mohammad R. Marzabadi, Carlos Forray, Dhanapalan Nagarathnam, Wai C. Wong, Stacey O'Malley, Barbara Francis, Dhar T G Murali, Douglas J. Pettibone, Jerry DiSalvo, Roger M. Freidinger, Miao Shou Wu, Raymond S.L. Chang, Bharat Lagu
Publikováno v:
European Journal of Pharmacology. 409:301-312
L-771,688 (SNAP 6383, methyl(4S)-4-(3, 4-difluorophenyl)-6-[(methyloxy)methyl]-2-oxo-3-[(?3-[4-(2-pyridin yl)-1-piperidinyl]propyl?amino)carbonyl]-1,2,3, 4-tetrahydro-5-pyrimidine carboxylate) had high affinity (Ki less than or = 1 nM) for [3H]prazos
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