107 articles for S Patel
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PMID
Data
Article Title
Organization
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
Genentech
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
Pfizer
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Wuxi Apptec
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.
Astex Pharmaceuticals
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
TBA
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Merck Research Laboratories
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Genentech
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Astex Pharmaceuticals
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Astex Pharmaceuticals
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.
Merck Research Laboratories
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Merck
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine (23).
Merck Research Laboratories
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.
Glaxosmithkline
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Glaxosmithkline
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Glaxosmithkline
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.
Glaxosmithkline
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring.
Pfizer
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
Johnson & Johnson Pharmaceutical Research & Development
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Glaxosmithkline
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Merck Sharp and Dohme Research Laboratories
2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.
Novartis Institute For Medical Sciences
Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-ß2-agonist for the treatment of chronic obstructive pulmonary disease.
Pfizer
Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
Chroma Therapeutics
Inhalation by design: dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD.
Pfizer
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
Chroma Therapeutics
Conformationally-restricted amino acid analogues bearing a distal sulfonic acid show selective inhibition of system x(c)(-) over the vesicular glutamate transporter.
The University of Montana
1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channel
TBA
C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
TBA
Potent, selective, water-soluble benzodiazepine-based CCKB receptor antagonists that contain lipophilic carboxylate surrogates
TBA
L-708,474: The C5-cyclohexyl analogue of L-365,260, a selective high affinity ligand for the CCKB/gastrin receptor
TBA
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Glaxosmithkline
Modulation of peripheral serotonin levels by novel tryptophan hydroxylase inhibitors for the potential treatment of functional gastrointestinal disorders.
Lexicon Pharmaceuticals
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.
Merck Research Laboratories
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.
The Institute of Cancer Research
Interleukin-1β converting enzyme (ICE): A comprehensive review on discovery and development of caspase-1 inhibitors.
L J University Ahmedabad
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
Astrazeneca Pharmaceuticals
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Merck Research Laboratories
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
Novartis Institutes For Biomedical Research
Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors.
Pharmaron Beijing
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
Merck Sharp and Dohme Research Laboratories
Discovery of boronic acid-based potent activators of tumor pyruvate kinase M2 and development of gastroretentive nanoformulation for oral dosing.
National Institute of Pharmaceutical Education and Research-Ahmedabad
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Merck
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
Janssen Research and Development
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.
Merck Sharp & Dohme Research Laboratories
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
Genentech
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Merck Sharp and Dohme Research Laboratories
3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
Merck Sharp & Dohme Research Laboratories
2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.
Merck Sharp & Dohme Research Laboratories
Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist.
Merck Sharp & Dohme Research Laboratories
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.
Merck Sharp and Dohme Research Laboratories
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
Merck Sharp and Dohme Research Laboratories
Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.
Merck Sharp & Dohme Research Laboratories
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.
Merck Sharp & Dohme Research Laboratories
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Merck Sharp and Dohme Research Laboratories
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
Merck Sharp and Dohme Research Laboratories
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
Merck Sharp and Dohme Research Laboratories
Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.
Neuroscience Research Centre
Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility.
Merck Research Laboratories
Fragment-based drug discovery applied to Hsp90. Discovery of two lead series with high ligand efficiency.
Astex Therapeutics
Tumor pyruvate kinase M2 modulators: a comprehensive account of activators and inhibitors as anticancer agents.
National Institute of Pharmaceutical Education and Research Ahmedabad
Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
Janssen Research and Development
Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.
Wuxi Apptec
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Genentech
Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane.
Merck Sharp and Dohme Research Laboratories
AROMATIC HETEROCYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR AND USES THEREOF
Innovstone Therapeutics
Small molecule inhibitors of GPCR GPR68 and related receptors for treating cancer, glioblastoma, and other indications
University of Maryland, Baltimore
6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives as PDE3A and PDE3B inhibitors for treating cancer
Bayer Aktiengesellschaft
Fused heterocyclic derivatives, their preparation methods thereof and medical uses thereof
Beijing Innocare Pharma Tech
Piperazinyl norbenzomorphan compounds and methods for using the same
University Of Texas
Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
Bristol-Myers Squibb
Sulfoximine substituted quinazolines for pharmaceutical compositions
Evotec Internatonal
Potent inhibitory effects of benzyl and p-xylidine-bis dithiocarbamate sodium salts on activities of mushroom tyrosinase.
University of Tehran
High-speed synthesis of potent C2-symmetric HIV-1 protease inhibitors by in-situ aminocarbonylations.
Uppsala University
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Smithkline Beecham Pharmaceuticals
G protein-coupled receptor kinase 2 inhibitors and methods for use of the same
University of Michigan
Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy.
University of Illinois
Discovery of a novel class of reversible non-peptide caspase inhibitors via a structure-based approach.
Burnham Institute