Search Results - "Weikert, Robert"

Unbound Brain Concentration Determines Receptor Occupancy: A Correlation of Drug Concentration and Brain Serotonin and Dopamine Reuptake Transporter Occupancy for Eighteen Compounds in Rats by Liu, Xingrong, Vilenski, Olga, Kwan, Joyce, Apparsundaram, Subbu, Weikert, Robert

“…It is a commonly accepted hypothesis that central nervous system (CNS) activity is determined by the unbound brain drug concentration. However, limited…”
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2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression by Carter, David S., Cai, Hai-Ying, Lee, Eun Kyung, Iyer, Pravin S., Lucas, Matthew C., Roetz, Ralf, Schoenfeld, Ryan C., Weikert, Robert J.

“…The discovery and optimization of a novel series of 2-substituted N-aryl piperazine based triple reuptake inhibitors is described. Recently a class of…”
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Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain by Lucas, Matthew C., Weikert, Robert J., Carter, David S., Cai, Hai-Ying, Greenhouse, Robert, Iyer, Pravin S., Lin, Clara J., Lee, Eun Kyung, Madera, Ann Marie, Moore, Amy, Ozboya, Kerem, Schoenfeld, Ryan C., Steiner, Sandra, Zhai, Yansheng, Lynch, Stephen M.

“…Two new series of monoamine triple reuptake inhibitors (TRIs) have been discovered through scaffold homologation of our recently reported series of…”
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Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors by BANNWART, Linda M, CARTER, David S, LYNCH, Stephen M, MADERA, Ann Marie, MOORE, Amy, OZBOYA, Kerem, RAPTOVA, Lubica, ROETZ, Ralf, SCHOENFELD, Ryan C, STEIN, Karin Ann, STEINER, Sandra, VILLA, Marzia, CAI, Hai-Ying, WEIKERT, Robert J, YANSHENG ZHAI, CHOY, Jason C, GREENHOUSE, Robert, JAIME-FIGUEROA, Saul, LYER, Pravin S, LIN, Clara J, EUN KYUNG LEE, LUCAS, Matthew C

“…A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro…”
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Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors by Lucas, Matthew C., Carter, David S., Cai, Hai-Ying, Lee, Eun Kyung, Schoenfeld, Ryan C., Steiner, Sandra, Villa, Marzia, Weikert, Robert J., Iyer, Pravin S.

“…A variety of novel aminoheterocycle scaffolds as selective monoamine reuptake inhibitors have been prepared and one of these scaffolds is achiral. The main…”
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Simultaneous Inhibition of Angiopoietin-2 and Vascular Endothelial Growth Factor-A with Faricimab in Diabetic Macular Edema: BOULEVARD Phase 2 Randomized Trial by Sahni, Jayashree, Patel, Sunil S, Dugel, Pravin U, Khanani, Arshad M, Jhaveri, Chirag D, Wykoff, Charles C, Hershberger, Vrinda S, Pauly-Evers, Meike, Sadikhov, Shamil, Szczesny, Piotr, Schwab, Dietmar, Nogoceke, Everson, Osborne, Aaron, Weikert, Robert, Fauser, Sascha

“…The phase 2 BOULEVARD trial compared safety and efficacy of faricimab, a novel bispecific antibody targeting angiopoietin-2 and vascular endothelial growth…”
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Safety and Efficacy of Different Doses and Regimens of Faricimab vs Ranibizumab in Neovascular Age-Related Macular Degeneration: The AVENUE Phase 2 Randomized Clinical Trial by Sahni, Jayashree, Dugel, Pravin U, Patel, Sunil S, Chittum, Mark E, Berger, Brian, Del Valle Rubido, Marta, Sadikhov, Shamil, Szczesny, Piotr, Schwab, Dietmar, Nogoceke, Everson, Weikert, Robert, Fauser, Sascha

“…Faricimab, the first bispecific antibody designed for intraocular use, simultaneously and independently binds and neutralizes angiopoietin 2 (Ang-2) and…”
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326-OR: Faricimab for Diabetic Macular Edema: A Novel Anti–Angiopoietin-2/Anti–Vascular Endothelial Growth Factor Bispecific Antibody in Clinical Trials by SHETH, VEERAL, SAHNI, JAYASHREE, STOILOV, IVAYLO, WILLIS, JEFFREY R., WEIKERT, ROBERT

“…In the United States, diabetic retinopathy (DR) and diabetic macular edema (DME) are a leading cause of blindness among working-age adults. The introduction of…”
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Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action by Han, Xingchun, Zhou, Chengang, Jiang, Min, Wang, Yongguang, Wang, Jianhua, Cheng, Zhanling, Wang, Min, Liu, Yongqiang, Liang, Chungen, Wang, Jianping, Wang, Zhanguo, Weikert, Robert, Lv, Wenzhe, Xie, Jianxun, Yu, Xin, Zhou, Xue, Luangsay, Souphalone, Shen, Hong C, Mayweg, Alexander V, Javanbakht, Hassan, Yang, Song

“…Chronic hepatitis B virus (HBV) infection is a serious public health burden, and current therapies cannot achieve satisfactory cure rate. There are high unmet…”
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Results and evaluation of a first‐in‐human study of RG7342, an mGlu5 positive allosteric modulator, utilizing Bayesian adaptive methods by Sturm, Stefan, Delporte, Marie‐Laure, Hadi, Salah, Schobel, Scott, Lindemann, Lothar, Weikert, Robert, Jaeschke, Georg, Derks, Michael, Palermo, Giuseppe

“…Aim The objectives of this first‐in‐human study were to evaluate the safety and tolerability, pharmacokinetics and pharmacodynamics, and maximum tolerated dose…”
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Synthesis of Mexiletine Stereoisomers and Related Compounds via SNAr Nucleophilic Substitution of a Cr(CO)3-Complexed Aromatic Fluoride by Loughhead, David G, Flippin, Lee A, Weikert, Robert J

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Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents by Connor, David T, Cetenko, Wiaczeslaw A, Mullican, Michael D, Sorenson, Roderick J, Unangst, Paul C, Weikert, Robert J, Adolphson, Richard L, Kennedy, John A, Thueson, David O

“…The synthesis and antiallergic activity of a series of novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles are described. A number of the…”
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Simultaneous Inhibition of Angiopoietin-2 and Vascular Endothelial Growth Factor-A with Faricimab in Diabetic Macular Edema by Sahni, Jayashree, Patel, Sunil S., Dugel, Pravin U., Khanani, Arshad M., Jhaveri, Chirag D., Wykoff, Charles C., Hershberger, Vrinda S., Pauly-Evers, Meike, Sadikhov, Shamil, Szczesny, Piotr, Schwab, Dietmar, Nogoceke, Everson, Osborne, Aaron, Weikert, Robert, Fauser, Sascha

“…The phase 2 BOULEVARD trial compared safety and efficacy of faricimab, a novel bispecific antibody targeting angiopoietin-2 and vascular endothelial growth…”
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Structure−Activity Relationships for Inhibition of Inosine Monophosphate Dehydrogenase by Nuclear Variants of Mycophenolic Acid by Nelson, Peter H, Carr, Stephen F, Devens, Bruce H, Eugui, Elsie M, Franco, Fidencio, Gonzalez, Carlos, Hawley, Ronald C, Loughhead, David G, Milan, David J, Papp, Eva, Patterson, John W, Rouhafza, Sussan, Sjogren, Eric B, Smith, David B, Stephenson, Rebecca A, Talamas, Francisco X, Waltos, Ann-Marie, Weikert, Robert J, Wu, John C

“…Structure−activity relationships in the region of the phthalide ring of the inosine monophosphate dehydrogenase inhibitor mycophenolic acid have been explored…”
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Asymmetric Synthesis and Stereochemical Assignment of RS-97613, a Potent Immunosuppressive and Antiinflammatory Agent by Smith, David B, Waltos, Ann Marie, Loughhead, David G, Weikert, Robert J, Morgans, David J, Rohloff, John C, Link, John O, Zhu, Rong-rong

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Novel indolecarboxamidotetrazoles as potential antiallergy agents by Unangst, Paul C, Connor, David T, Stabler, S. Russell, Weikert, Robert J, Carethers, Mary E, Kennedy, John A, Thueson, David O, Chestnut, James C, Adolphson, Richard L, Conroy, M. C

“…The synthesis and antiallergic potential of a series of novel indolecarboxamidotetrazoles are described. A number of compounds inhibit the release of histamine…”
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Synthesis of Mexiletine Stereoisomers and Related Compounds via S(N)Ar Nucleophilic Substitution of a Cr(CO)(3)-Complexed Aromatic Fluoride by Loughhead, David G., Flippin, Lee A., Weikert, Robert J.

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Synthesis and anthelmintic activity of 3'-benzoylurea derivatives of 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole by Weikert, Robert J, Bingham, Stanford, Emanuel, Mark A, Fraser-Smith, Elizabeth B, Loughhead, David G, Nelson, Peter H, Poulton, Anthony L

“…Reaction of 3-amino derivatives of the nematocides tetramisole and levamisole with variously substituted benzoylisocyanates gave a series of benzoylureas I…”
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Synthesis of Mexiletine Stereoisomers and Related Compounds via S N Ar Nucleophilic Substitution of a Cr(CO) 3 -Complexed Aromatic Fluoride by Loughhead, David G., Flippin, Lee A., Weikert, Robert J.

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The Florisil ® catalyzed [1,3]-sigmatropic shift of allyl phenyl ethers — An entryway into novel mycophenolic acid analogues by Talamás, Francisco X., Smith, David B., Cervantes, Alicia, Franco, Fidencio, Cutler, Serena T., Loughhead, David G., Morgans, David J., Weikert, Robert J.

“…Florisil ® was found to be effective in promoting the [1,3]-sigmatropic shift of mycophenolic acid related allyl phenyl ethers. Several novel mycophenolic acid…”
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