未登录Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists
Yang, Lihu; Butora, Gabor; Jiao, Richard X.; Pasternak, Alex; Zhou, Changyou; Parsons, William H.; Mills, Sander G.; Vicario, Pasquale P.; Ayala, Julia M.; Cascieri, Margaret A.; MacCoss, Malcolm .png)
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收藏Expression and characterization of the chemokine receptor CCR2B from rhesus monkeyJin, H; Vicario, PP; Zweerink, H; Goyal, S; Hanlon, WA; Dorn, CP; Mills, SG; DeMartino, JA; Cascieri, MA; Struthers, M 分享 收藏 CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activityLynch, CL; Hale, JJ; Budhu, RJ; Gentry, AL; Finke, PE; Caldwell, CG; Mills, SG; MacCoss, M; Shen, DM; Chapman, KT; Malkowitz, L; Springer, MS; Gould, SL; DeMartino, JA; Siciliano, SJ; Cascieri, MA; Carella, A; Carver, G; Karen, H; Schleif, WA; Danzeisen, R; Hazuda, D; Kessler, J; Lineberger, J; Miller, M; Emini, E 分享 收藏 TRYPTOPHAN-DERIVED NK1 ANTAGONISTS - CONFORMATIONALLY CONSTRAINED HETEROCYCLIC BIOISOSTERES OF THE ESTER LINKAGELEWIS, RT; MACLEOD, AM; MERCHANT, KJ; KELLEHER, F; SANDERSON, I; HERBERT, RH; CASCIERI, MA; SADOWSKI, S; BALL, RG; HOOGSTEEN, K 分享 收藏 IDENTIFICATION OF A SERIES OF 3-(BENZYLOXY)-1-AZABICYCLO[2.2.2]OCTANE HUMAN NK1 ANTAGONISTSSWAIN, CJ; SEWARD, EM; CASCIERI, MA; FONG, TM; HERBERT, R; MACINTYRE, DE; MERCHANT, KJ; OWEN, SN; OWENS, AP; SABIN, V; TEALL, M; VANNIEL, MB; WILLIAMS, BJ; SADOWSKI, S; STRADER, C; BALL, RG; BAKER, R 分享 收藏 SYNTHESIS AND BIOLOGICAL EVALUATION OF NK1 ANTAGONISTS DERIVED FROM L-TRYPTOPHANMACLEOD, AM; CASCIERI, MA; MERCHANT, KJ; SADOWSKI, S; HARDWICKE, S; LEWIS, RT; MACINTYRE, DE; METZGER, JM; FONG, TM; SHEPHEARD, S; TATTERSALL, FD; HARGREAVES, R; BAKER, R 分享 收藏 An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administrationHarrison, T; Owens, AP; Williams, BJ; Swain, CJ; Williams, A; Carlson, EJ; Rycroft, W; Tattersall, FD; Cascieri, MA; Chicchi, GG; Sadowski, S; Rupniak, NMJ; Hargreaves, RJ 分享 收藏 The CXCR4 agonist ligand stromal derived factor-1 maintains high affinity for receptors in both Gαi-coupled and uncoupled statesDi Salvo, J; Koch, GE; Johnson, KE; Blake, AD; Daugherty, BL; DeMartino, JA; Sirotina-Meisher, A; Liu, Y; Springer, MS; Cascieri, MA; Sullivan, KA 分享 收藏 L-750355, a human β3-adrenoceptor agonist;: in vitro pharmacology and profile of activity in vivo in the rhesus monkeyForrest, MJ; Hom, G; Bach, T; Candelore, MR; Cascieri, MA; Strader, C; Tota, L; Fisher, MH; Szumiloski, J; Ok, HO; Weber, AE; Wyvratt, M; Vicario, P; Marko, O; Deng, LP; Cioffe, C; Hegarty-Friscino, B; MacIntyre, E 分享 收藏 分享 收藏 Discovery of a potent, orally bioavailable β3 adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamideMathvink, RJ; Tolman, JS; Chitty, D; Candelore, MR; Cascieri, MA; Colwell, LF; Deng, LP; Feeney, WP; Forrest, MJ; Hom, GJ; MacIntyre, DE; Miller, RR; Stearns, RA; Tota, L; Wyvratt, MJ; Fisher, MH; Weber, AE 分享 收藏 Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugsHale, JJ; Mills, SG; MacCoss, M; Dorn, CP; Finke, PE; Budhu, RJ; Reamer, RA; Huskey, SEW; Luffer-Atlas, D; Dean, BJ; McGowan, EM; Feeney, WP; Chiu, SHL; Cascieri, MA; Chicchi, GG; Kurtz, MM; Sadowski, S; Ber, E; Tattersall, FD; Rupniak, NMJ; Williams, AR; Rycroft, W; Hargreaves, R; Metzger, JM; MacIntyre, DE 分享 收藏 4,4-disubstituted piperidine high-affinity NK1 antagonists:: Structure-activity relationships and in vivo activityStevenson, GI; Huscroft, I; MacLeod, AM; Swain, CJ; Cascieri, MA; Chicchi, GG; Graham, MI; Harrison, T; Kelleher, FJ; Kurtz, M; Ladduwahetty, T; Merchant, KJ; Metzger, JM; MacIntyre, DE; Sadowski, S; Sohal, B; Owens, AP 分享 收藏 Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonistHale, JJ; Mills, SG; MacCoss, M; Finke, PE; Cascieri, MA; Sadowski, S; Ber, E; Chicchi, GG; Kurtz, M; Metzger, J; Eiermann, G; Tsou, NN; Tattersall, FD; Rupniak, NMJ; Williams, AR; Rycroft, W; Hargreaves, R; MacIntyre, DE 分享 收藏 A selective human β3 adrenergic receptor agonist increases metabolic rate in rhesus monkeysFisher, MH; Amend, AM; Bach, TJ; Barker, JM; Brady, EJ; Candelore, MR; Carroll, D; Cascieri, MA; Chiu, SHL; Deng, LP; Forrest, MJ; Hegarty-Friscino, B; Guan, XM; Hom, GJ; Hutchins, JE; Kelly, LJ; Mathvink, RJ; Metzger, JM; Miller, RR; Ok, HO; Parmee, ER; Saperstein, R; Strader, CD; Stearns, RA; Thompson, GM; Tota, L; Vicario, PP; Weber, AE; Woods, JW; Wyvratt, MJ; Zafian, PT; MacIntyre, DE 分享 收藏 Desensitization of β3-adrenergic receptor-stimulated adenylyl cyclase activity and lipolysis in ratsVicario, PP; Candelore, MR; Schaeffer, MT; Kelly, L; Thompson, GM; Brady, EJ; Saperstein, R; MacIntyre, DE; Tota, LM; Cascieri, MA 分享 收藏 Molecular cloning and characterization of a new receptor for galaninHoward, AD; Tan, C; Shiao, LL; Palyha, OC; McKee, KK; Weinberg, DH; Feighner, SD; Cascieri, MA; Smith, RG; VanDerPloeg, LHT; Sullivan, KA 分享 收藏 In vitro and in vivo predictors of the anti-emetic activity of tachykinin NK1 receptor antagonistsRupniak, NMJ; Tattersall, FD; Williams, AR; Rycroft, W; Carlson, EJ; Cascieri, MA; Sadowski, S; Ber, E; Hale, JJ; Mills, SG; MacCoss, M; Seward, E; Huscroft, I; Owen, S; Swain, CJ; Hill, RG; Hargreaves, RJ 分享 收藏 分享 收藏 L-733,060, a novel tachykinin NK1 receptor antagonist; Effects in [Ca2+](i) mobilisation, cardiovascular and dural extravasation assaysSeabrook, GR; Shepheard, SL; Williamson, DJ; Tyrer, P; Rigby, M; Cascieri, MA; Harrison, T; Hargreaves, RJ; Hill, RG 分享 收藏 
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