In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia
Barrow, JC, Nantermet, PG, Selnick, HG, Glass, KL, Rittle, KE, Gilbert, KF, Steele, TG, Homnick, CF, Freidinger, RM, Ransom, RW, Kling, P, Reiss, D, Broten, TP, Schorn, TW, Chang, RSL, O'Malley, SS, Olah, TV, Ellis, JD, Barrish, A, Kassahun, K, Leppert, P, Nagarathnam, D, Forray, C
Published in Journal of medicinal chemistry (13.07.2000)
Published in Journal of medicinal chemistry (13.07.2000)
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Design and synthesis of novel alpha(1a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones
Nagarathnam, D, Miao, SW, Lagu, B, Chiu, G, Fang, J, Dhar, TGM, Zhang, J, Tyagarajan, S, Marzabadi, MR, Zhang, FQ, Wong, WC, Sun, WY, Tian, D, Wetzel, JM, Forray, C, Chang, RSL, Broten, TP, Ransom, RW, Schorn, TW, Chen, TB, O'Malley, S, Kling, P, Schneck, K, Bendesky, R, Harrell, CM, Vyas, KP, Gluchowski, C
Published in Journal of medicinal chemistry (18.11.1999)
Published in Journal of medicinal chemistry (18.11.1999)
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Design and synthesis of novel alpha(1a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety
Dhar, TGM, Nagarathnam, D, Marzabadi, MR, Lagu, B, Wong, WC, Chiu, G, Tyagarajan, S, Miao, SW, Zhang, FQ, Sun, WY, Tian, D, Shen, QR, Zhang, J, Wetzel, JM, Forray, C, Chang, RSL, Broten, TP, Schorn, TW, Chen, TB, O'Malley, S, Ransom, R, Schneck, K, Bendesky, R, Harrell, CM, Vyas, KP, Zhang, KY, Gilbert, J, Pettibone, DJ, Patane, MA, Bock, MG, Freidinger, RM, Gluchowski, C
Published in Journal of medicinal chemistry (18.11.1999)
Published in Journal of medicinal chemistry (18.11.1999)
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Design and synthesis of novel alpha(1a) adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia
Nagarathnam, D, Wetzel, JM, Miao, SW, Marzabadi, MR, Chiu, G, Wong, WC, Hong, XF, Fang, J, Forray, C, Branchek, TA, Heydorn, WE, Chang, RSL, Broten, T, Schorn, TW, Gluchowski, C
Published in Journal of medicinal chemistry (17.12.1998)
Published in Journal of medicinal chemistry (17.12.1998)
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Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists
Mantlo, Nathan B, Chakravarty, Prasun K, Ondeyka, Debra L, Siegl, Peter K. S, Chang, Raymond S, Lotti, Victor J, Faust, Kristie A, Schorn, Terry W, Chen, Tsing Bau
Published in Journal of medicinal chemistry (01.09.1991)
Published in Journal of medicinal chemistry (01.09.1991)
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De novo design of a novel oxazolidinone analogue as a potent and selective alpha(1A) adrenergic receptor antagonist with high oral bioavailability
Lagu, B, Tian, D, Jeon, Y, Li, C, Wetzel, JM, Nagarathnam, D, Shen, QR, Forray, C, Chang, RSL, Broten, TP, Ransom, RW, Chan, TB, O'Malley, SS, Schorn, TW, Rodrigues, AD, Kassahun, K, Pettibone, DJ, Freidinger, R, Gluchowski, C
Published in Journal of medicinal chemistry (27.07.2000)
Published in Journal of medicinal chemistry (27.07.2000)
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A HIGHLY POTENT, ORALLY-ACTIVE IMIDAZO[4,5-B]PYRIDINE BIPHENYLACYLSULFONAMIDE (MK-996-L-159,282) - A NEW ANGIOTENSIN-II RECEPTOR ANTAGONIST
CHAKRAVARTY, PK, NAYLOR, EM, CHEN, A, CHANG, RSL, CHEN, TB, FAUST, KA, LOTTI, VJ, KIVLIGHN, SD, GABLE, RA, ZINGARO, GJ, SCHORN, TW, SCHAFFER, LW, BROTEN, TP, SIEGL, PKS, PATCHETT, AA, GREENLEE, WJ
Published in Journal of medicinal chemistry (25.11.1994)
Published in Journal of medicinal chemistry (25.11.1994)
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Discovery of L-162,313: a nonpeptide that mimics the biological actions of angiotensin II
Kivlighn, S D, Huckle, W R, Zingaro, G J, Rivero, R A, Lotti, V J, Chang, R S, Schorn, T W, Kevin, N, Johnson, Jr, R G, Greenlee, W J
Published in The American journal of physiology (01.03.1995)
Published in The American journal of physiology (01.03.1995)
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TRIAZOLINONE BIPHENYLSULFONAMIDE DERIVATIVES AS ORALLY-ACTIVE ANGIOTENSIN-II ANTAGONISTS WITH POTENT AT(1) RECEPTOR AFFINITY AND ENHANCED AT(2) AFFINITY
ASHTON, WT, CHANG, LL, FLANAGAN, KL, HUTCHINS, SM, NAYLOR, EM, CHAKRAVARTY, PK, PATCHETT, AA, GREENLEE, WJ, CHEN, TB, FAUST, KA, CHANG, RSL, LOTTI, VJ, ZINGARO, GJ, SCHORN, TW, SIEGL, PKS, KIVLIGHN, SD
Published in Journal of medicinal chemistry (19.08.1994)
Published in Journal of medicinal chemistry (19.08.1994)
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Angiotensin II receptor subtypes in renal cortex of rats and rhesus monkeys
Gibson, R E, Thorpe, H H, Cartwright, M E, Frank, J D, Schorn, T W, Bunting, P B, Siegl, P K
Published in American journal of physiology. Renal physiology (01.09.1991)
Published in American journal of physiology. Renal physiology (01.09.1991)
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Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles
Ashton, Wallace T, Cantone, Christine L, Chang, Linda L, Hutchins, Steven M, Strelitz, Robert A, MacCoss, Malcolm, Chang, Raymond S. L, Lotti, Victor J, Faust, Kristie A
Published in Journal of medicinal chemistry (05.03.1993)
Published in Journal of medicinal chemistry (05.03.1993)
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Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists
Nerenberg, J B, Erb, J M, Thompson, W J, Lee, H Y, Guare, J P, Munson, P M, Bergman, J M, Huff, J R, Broten, T P, Chang, R S, Chen, T B, O'Malley, S, Schorn, T W, Scott, A L
Published in Bioorganic & medicinal chemistry letters (22.09.1998)
Published in Bioorganic & medicinal chemistry letters (22.09.1998)
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Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analog inhibitors containing a novel analog of statine
Boger, Joshua, Payne, Linda S, Perlow, Debra S, Lohr, Nancy S, Poe, Martin, Blaine, Edward H, Ulm, Edgar H, Schorn, Terry W, LaMont, Bruce I
Published in Journal of medicinal chemistry (01.12.1985)
Published in Journal of medicinal chemistry (01.12.1985)
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Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors
De Laszlo, S. E, Bush, B. L, Doyle, J. J, Greenlee, W. J, Hangauer, D. G, Halgren, T. A, Lynch, R. J, Schorn, T. W, Siegl, P. K. S
Published in Journal of medicinal chemistry (01.03.1992)
Published in Journal of medicinal chemistry (01.03.1992)
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In vivo pharmacology of a novel AT selective angiotensin II receptor antagonist, MK-996
KIVLIGHN, S, ZINGARO, G, GABEL, R, BROTEN, T, SCHORN, T, SCHAFFER, L, NAYLOR, E, CHAKRAVARTY, P, PATCHETT, A, GREENLEE, W
Published in American journal of hypertension (01.01.1995)
Published in American journal of hypertension (01.01.1995)
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Novel renin inhibitors containing the amino acid statine
Boger, J, Lohr, N S, Ulm, E H, Poe, M, Blaine, E H, Fanelli, G M, Lin, T Y, Payne, L S, Schorn, T W, LaMont, B I, Vassil, T C, Stabilito, I I, Veber, D F, Rich, D H, Bopari, A S
Published in Nature (London) (05.05.1983)
Published in Nature (London) (05.05.1983)
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Highly potent, orally active diester macrocyclic human renin inhibitors
Weber, Ann E, Steiner, Mark G, Krieter, Philip A, Colletti, Adria E, Tata, James R, Halgren, Thomas A, Ball, Richard G, Doyle, John J, Schorn, Terry W
Published in Journal of medicinal chemistry (01.10.1992)
Published in Journal of medicinal chemistry (01.10.1992)
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Quinazolinone Biphenyl Acylsulfonamides: A potent new class of angiotensin-II receptor antagonists
Chakravarty, Prasun K., Strelitz, Robert A., Chen, Tsing-Bau, Chang, Raymond S.L., Lotti, Victor J., Zingaro, Gloria J., Schorn, Terry W., Kivlighn, Salah D., Siegel, Peter K.S., Patchett, Arthur A., Greenlee, William J.
Published in Bioorganic & medicinal chemistry letters (06.01.1994)
Published in Bioorganic & medicinal chemistry letters (06.01.1994)
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Renin inhibitors containing C-termini derived from mercaptoheterocycles
Ashton, Wallace T, Cantone, Christine L, Meurer, Laura C, Tolman, Richard L, Greenlee, William J, Patchett, Arthur A, Lynch, Robert J, Schorn, Terry W, Strouse, John F, Siegl, Peter K. S
Published in Journal of medicinal chemistry (01.05.1992)
Published in Journal of medicinal chemistry (01.05.1992)
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