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51

Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity

Robert L. Hudkins, Lisa D. Aimone, Thomas R. Bailey, Robert J. Bendesky, Reddeppa reddy Dandu, Derek Dunn, John A. Gruner, Kurt A. Josef, Yin-Guo Lin, Jacquelyn Lyons, Val R. Marcy, Joanne R. Mathiase

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 361 KB

english, 2011

52

Amine-constrained pyridazinone histamine H3 receptor antagonists

Babu G. Sundar, Thomas Bailey, Edward Bacon, Lisa Aimone, Zeqi Huang, Jacquelyn Lyons, Rita Raddatz, Robert Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 911 KB

english, 2011

53

Synthesis and structure–activity relationships of 4,5-fused pyridazinones as histamine H3 receptor antagonists

Ming Tao, Rita Raddatz, Lisa D. Aimone, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 854 KB

english, 2011

54

Synthesis and evaluation of pyridazinone–phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity

Reddeppa reddy Dandu, John A. Gruner, Joanne R. Mathiasen, Lisa D. Aimone, Greg Hostetler, Caitlyn Benfield, Robert J. Bendesky, Val R. Marcy, Rita Raddatz, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 322 KB

english, 2011

55

Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists

Nadine C. Becknell, Jacquelyn A. Lyons, Lisa D. Aimone, John A. Gruner, Joanne R. Mathiasen, Rita Raddatz, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 993 KB

english, 2011

56

4,5-Dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists

Robert L. Hudkins, Lisa D. Aimone, Reddeppa reddy Dandu, Derek Dunn, John A. Gruner, Zeqi Huang, Kurt A. Josef, Jacquelyn A. Lyons, Joanne R. Mathiasen, Ming Tao, Allison L. Zulli, Rita Raddatz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 699 KB

english, 2012

57

Synthesis and evaluation of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues as histamine-3 receptor antagonists

Nadine C. Becknell, Reddeppa Reddy Dandu, Jacquelyn A. Lyons, Lisa D. Aimone, Rita Raddatz, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.12 MB

english, 2012

58

Synthesis and structure–activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H3 receptor inverse agonists

Ming Tao, Lisa D. Aimone, John A. Gruner, Joanne R. Mathiasen, Zeqi Huang, Jacquelyn Lyons, Rita Raddatz, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 358 KB

english, 2012

59

4-Phenoxypiperidine pyridazin-3-one histamine H3 receptor inverse agonists demonstrating potent and robust wake promoting activity

Robert L. Hudkins, Allison L. Zulli, Reddeppa reddy Dandu, Ming Tao, Kurt A. Josef, Lisa D. Aimone, R. Curtis Haltiwanger, Zeqi Huang, Jacquelyn A. Lyons, Joanne R. Mathiasen, Rita Raddatz, John A. Gr

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 408 KB

english, 2012

60

Synthesis and evaluation of a new series of 1′-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4′-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists

Reddeppa Reddy Dandu, Jacquelyn A. Lyons, Rita Raddatz, Zeqi Huang, Lisa D. Aimone, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 367 KB

english, 2012

61

Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists

Allison L. Zulli, Lisa D. Aimone, Joanne R. Mathiasen, John A. Gruner, Rita Raddatz, Edward R. Bacon, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 686 KB

english, 2012

62

Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists

Kurt A. Josef, Lisa D. Aimone, Jacquelyn Lyons, Rita Raddatz, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 384 KB

english, 2012

63

The involvement of the μ-opioid receptor in gastrointestinal pathophysiology: Therapeutic opportunities for antagonism at this receptor

Diane L. DeHaven-Hudkins, Robert N. DeHaven, Patrick J. Little, Lee M. Techner

Journal:

Pharmacology & Therapeutics

Year:

2008

Language:

english

File:

PDF, 429 KB

english, 2008

64

Optimization of 5-Pyridazin-3-one Phenoxypropylamines as Potent, Selective Histamine H3 Receptor Antagonists with Potent Cognition Enhancing Activity

Tao, Ming, Aimone, Lisa D., Huang, Zeqi, Mathiasen, Joanne, Raddatz, Rita, Lyons, Jacquelyn, Hudkins, Robert L.

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 422 KB

english, 2012

65

Caramiphen, iodocaramiphen and nitrocaramiphen are potent, competitive, muscarinic M1 receptor-selective agents

Robert L. Hudkins, James F. Stubbins, Diane L. DeHaven-Hudkins

Journal:

European Journal of Pharmacology

Year:

1993

Language:

english

File:

PDF, 332 KB

english, 1993

66

RLH-033, a novel, potent and selective ligand for the σ1 recognition site

Robert L. Hudkins, Richard B. Mailman, Diane L. DeHaven-Hudkins

Journal:

European Journal of Pharmacology

Year:

1994

Language:

english

File:

PDF, 177 KB

english, 1994

67

Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists

Nadine C. Becknell, Jacquelyn A. Lyons, Lisa D. Aimone, Zeqi Huang, John A. Gruner, Rita Raddatz, Robert L. Hudkins

Journal:

Bioorganic & Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 1.08 MB

english, 2012

68

Antipruritic and antihyperalgesic actions of loperamide and analogs

Diane L DeHaven-Hudkins, Alan Cowan, Luz Cortes Burgos, Jeffrey D Daubert, Joel A Cassel, Robert N DeHaven, George B Kehner, Virendra Kumar

Journal:

Year:

2002

Language:

english

File:

PDF, 127 KB

english, 2002

69

Effect of kappa opioid agonists on visceral nociception induced by uterine cervical distension in rats

Andreas Sandner-Kiesling, Hui-Lin Pan, Shao-Rui Chen, Robert L James, Diane L DeHaven-Hudkins, David M Dewan, James C Eisenach

Journal:

Year:

2002

Language:

english

File:

PDF, 193 KB

english, 2002

70

Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery

Ghose, Arup K., Herbertz, Torsten, Hudkins, Robert L., Dorsey, Bruce D., Mallamo, John P.

Journal:

ACS Chemical Neuroscience

Year:

2012

Language:

english

File:

PDF, 3.74 MB

english, 2012

71

Synthesis and Biological Profile of the pan-Vascular Endothelial Growth Factor Receptor/Tyrosine Kinase with Immunoglobulin and Epidermal Growth Factor-Like Homology Domains 2 (VEGF-R/TIE-2) Inhibitor 11-(2-Methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4 H -indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): A Novel Oncology Therapeutic Agent

Hudkins, Robert L., Becknell, Nadine C., Zulli, Allison L., Underiner, Ted L., Angeles, Thelma S., Aimone, Lisa D., Albom, Mark S., Chang, Hong, Miknyoczki, Sheila J., Hunter, Kathryn, Jones-Bolin, Su

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 1.90 MB

english, 2012

72

Discovery and Characterization of 6-{4-[3-( R )-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2 H -pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H 3 Receptor Inverse Agonist

Hudkins, Robert L., Raddatz, Rita, Tao, Ming, Mathiasen, Joanne R., Aimone, Lisa D., Becknell, Nadine C., Prouty, Catherine P., Knutsen, Lars J. S., Yazdanian, Mehran, Moachon, Gilbert, Ator, Mark A.,

Journal:

Journal of Medicinal Chemistry

Year:

2011

Language:

english

File:

PDF, 1007 KB

english, 2011

73

A Facile and Efficient Synthesis of 3-Amino-5-bromopyridine Derivatives Using Microwave Irradiation

reddy Dandu, Reddeppa, C. Rose, Adam, L. Hudkins, Robert

Journal:

Year:

2011

Language:

english

File:

PDF, 636 KB

english, 2011

74

Binding of dexetimide and levetimide to [3H](+)pentazocine- and [3H]1,3-Dl(2-tolyl)guanidine-defined σ recognition sites

Diane L. DeHaven-Hudkins, Robert L. Hudkins

Journal:

Year:

1991

Language:

english

File:

PDF, 300 KB

english, 1991

75

Anticonvulsant activity of caramiphen analogs

Diane L. Dehaven-Hudkins, J.Tim Allen, Robert L. Hudkins, James F. Stubbins, Frank C. Tortella

Journal:

Year:

1995

Language:

english

File:

PDF, 435 KB

english, 1995

76

Development and Scale-Up of an Optimized Route to the Pyridazin-3-one Histamine H3 Receptor Antagonist CEP-32215

Wang, Yi, Przyuski, Katrin, Roemmele, Renee C., Hudkins, Robert L., Bakale, Roger P.

Journal:

Organic Process Research & Development

Year:

2013

Language:

english

File:

PDF, 379 KB

english, 2013

77

Novel (4-Phenylpiperidinyl)- and (4-Phenylpiperazinyl)alkyl-Spaced Esters of 1-Phenylcyclopentanecarboxylic Acids as Potent .sigma.-Selective Compounds

Hudkins, Robert L., Mailman, Richard B., DeHaven-Hudkins, Diane L.

Journal:

Journal of Medicinal Chemistry

Year:

1994

Language:

english

File:

PDF, 1011 KB

english, 1994

78

Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity

Hudkins, Robert L., Josef, Kurt A., Becknell, Nadine C., Aimone, Lisa D., Lyons, Jacquelyn A., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 582 KB

english, 2014

79

Synthesis Of 2-Aryl- and 2-Vinyl-1H-indoles via Palladium-Catalyzed Cross-Coupling of Aryl and Vinyl Halides with 1-Carboxy-2-(tributylstannyl)indole

Hudkins, Robert L., Diebold, James L., Marsh, Frank D.

Journal:

Journal of Organic Chemistry

Year:

1995

Language:

english

File:

PDF, 371 KB

english, 1995

80

Fused Pyrrolo[2,3- c ]carbazol-6-ones: Novel Immunostimulants That Enhance Human Interferon-γ Activity

Hudkins, Robert L., Diebold, James L., Angeles, Thelma S., Knight, Ernest

Journal:

Journal of Medicinal Chemistry

Year:

1997

Language:

english

File:

PDF, 167 KB

english, 1997

81

Synthesis, Modeling, and In Vitro Activity of (3‘ S )- e pi -K-252a Analogues. Elucidating the Stereochemical Requirements of the 3‘-Sugar Alcohol on trkA Tyrosine Kinase Activity

Gingrich, Diane E., Yang, Shi X., Gessner, George W., Angeles, Thelma S., Hudkins, Robert L.

Journal:

Journal of Medicinal Chemistry

Year:

2005

Language:

english

File:

PDF, 416 KB

english, 2005

82

Mixed-Lineage Kinase 1 and Mixed-Lineage Kinase 3 Subtype-Selective Dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: Optimization, Mixed-Lineage Kinase 1 Crystallography, and Oral in Vivo Activity in 1-Methyl-4-phenyltetrahydropyridine Models

Hudkins, Robert L., Diebold, James L., Tao, Ming, Josef, Kurt A., Park, Chung Ho, Angeles, Thelma S., Aimone, Lisa D., Husten, Jean, Ator, Mark A., Meyer, Sheryl L., Holskin, Beverly P., Durkin, John

Journal:

Journal of Medicinal Chemistry

Year:

2008

Language:

english

File:

PDF, 751 KB

english, 2008

83

[Annual Reports in Medicinal Chemistry] Annual Reports in Medicinal Chemistry Volume 42 Volume 42 || Chapter 4 Recent Advances in Drug Discovery of Histamine H3 Antagonists

Hudkins, Robert L.

Year:

2007

Language:

english

File:

PDF, 159 KB

english, 2007

84

Correction to Synthesis and Biological Profile of the pan-Vascular Endothelial Growth Factor Receptor/Tyrosine Kinase with Immunoglobulin and Epidermal Growth Factor-Like Homology Domains 2 (VEGF-R/TIE-2) Inhibitor 11-(2-Methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4 H -indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): A Novel Oncology Therapeutic Agent

Hudkins, Robert L., Becknell, Nadine C., Zulli, Allison L., Underiner, Ted L., Angeles, Thelma S., Aimone, Lisa D., Albom, Mark S., Chang, Hong, Miknyoczki, Sheila J., Hunter, Kathryn, Jones-Bolin, Su

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 118 KB

english, 2012

85

Synthesis of 1H-Indolyl-2-benzimidazoles and 1H-Indolyl-2-benzothiazoles

L. Hudkins, Robert

Journal:

Year:

1995

Language:

english

File:

PDF, 146 KB

english, 1995

86

Serum amyloid A and inflammation in diabetic kidney disease and podocytes

Anderberg, Robert J, Meek, Rick L, Hudkins, Kelly L, Cooney, Sheryl K, Alpers, Charles E, Leboeuf, Renee C, Tuttle, Katherine R

Journal:

Laboratory Investigation

Year:

2015

Language:

english

File:

PDF, 3.81 MB

english, 2015

87

3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity

Hudkins, Robert L., Becknell, Nadine C., Lyons, Jacquelyn A., Aimone, Lisa D., Olsen, Mark, Haltiwanger, R. Curtis, Mathiasen, Joanne R., Raddatz, Rita, Gruner, John A.

Journal:

European Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 639 KB

english, 2015

88

Histamine H3 Antagonists for Treatment of Cognitive Deficits in CNS Diseases

Raddatz, Rita, Tao, Ming, Hudkins, Robert

Journal:

Current Topics in Medicinal Chemistry

Year:

2010

Language:

english

File:

PDF, 399 KB

english, 2010

89

Serum amyloid A and inflammation in diabetic kidney disease and podocytes

Anderberg, Robert J, Meek, Rick L, Hudkins, Kelly L, Cooney, Sheryl K, Alpers, Charles E, Leboeuf, Renee C, Tuttle, Katherine R

Journal:

Laboratory Investigation

Year:

2015

Language:

english

File:

PDF, 44 KB

english, 2015

90

3-(1′-Cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist

Hudkins, Robert L., Gruner, John A., Raddatz, Rita, Mathiasen, Joanne R., Aimone, Lisa D., Marino, Michael J., Bacon, Edward R., Williams, Michael, Ator, Mark A.

Journal:

Neuropharmacology

Year:

2015

Language:

english

File:

PDF, 787 KB

english, 2015

91

Overview: Recent Advances in the Medicinal Chemistry of Cannabinoids

Hudkins, Robert L, D'Ambra, Thomas E

Journal:

Expert Opinion on Therapeutic Patents

Year:

1993

Language:

english

File:

PDF, 1.04 MB

english, 1993

92

Editorial [Hot topic: Current Approaches for the Treatment of Cognitive Deficits in CNS Disease (Guest Editor: Robert L. Hudkins)]

Hudkins, Robert

Journal:

Current Topics in Medicinal Chemistry

Year:

2010

Language:

english

File:

PDF, 32 KB

english, 2010

93

Recent Advances in Targeting the Fatty Acid Biosynthetic Pathway using Fatty Acid Synthase Inhibitors

Angeles, Thelma S., Hudkins, Robert L.

Journal:

Expert Opinion on Drug Discovery

Year:

2016

Language:

english

File:

PDF, 948 KB

english, 2016

94

TEMPO (Technically Extended Multiparameter Optimization): An Advanced Robust Scoring Scheme To Calculate Central Nervous System (CNS) Druggability And Monitor Lead Optimization

Ghose, Arup K., Ott, Gregory R., Hudkins, Robert L

Journal:

ACS Chemical Neuroscience

Year:

2016

Language:

english

File:

PDF, 891 KB

english, 2016

95

Targeting the JNK Pathway for Therapeutic Benefit in CNS Disease

Bozyczko-Coyne, Donna, Saporito, Michael, Hudkins, Robert

Journal:

Current Drug Targets - CNS & Neurological Disorders

Year:

2002

Language:

english

File:

PDF, 189 KB

english, 2002

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