PMID

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Article Title

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Antiinflammatory 2,6-di-tert-butyl-4-(2-arylethenyl)phenols.

Boehringer Ingelheim Pharmaceuticals

N-Arylsulfonyl-a-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.

Boehringer Ingelheim Pharmaceuticals

Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.

Boehringer Ingelheim Pharmaceuticals

Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).

Boehringer Ingelheim Pharmaceuticals

Discovery of 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide analogs as new RORC modulators.

Boehringer Ingelheim Pharmaceuticals

Selective CB2 receptor agonists. Part 1: the identification of novel ligands through computer-aided drug design (CADD) approaches.

Boehringer Ingelheim Pharmaceuticals

Selective CB2 receptor agonists. Part 3: the optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model.

Boehringer Ingelheim Pharmaceuticals

Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

Boehringer Ingelheim Pharmaceuticals

Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists.

Boehringer Ingelheim Pharmaceuticals

Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.

Boehringer Ingelheim Pharmaceuticals

Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects.

Boehringer Ingelheim Pharmaceuticals

Substituted phenyl as a steroid A-ring mimetic: providing agonist activity to a class of arylsulfonamide nonsteroidal glucocorticoid ligands.

Boehringer Ingelheim Pharmaceuticals

Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists.

Boehringer Ingelheim Pharmaceuticals

Discovery of potent, selective chymase inhibitors via fragment linking strategies.

Boehringer Ingelheim Pharmaceuticals

Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.

Boehringer Ingelheim Pharmaceuticals

Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.

Boehringer Ingelheim Pharmaceuticals

Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.

Boehringer Ingelheim Pharmaceuticals

Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.

Boehringer Ingelheim Pharmaceuticals

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.

Boehringer Ingelheim Pharmaceuticals

Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.

Boehringer Ingelheim Pharmaceuticals

The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.

Boehringer Ingelheim Pharmaceuticals

Pyrazinoindolone inhibitors of MAPKAP-K2.

Boehringer Ingelheim Pharmaceuticals

Identification of dissociated non-steroidal glucocorticoid receptor agonists.

Boehringer Ingelheim Pharmaceuticals

Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.

Boehringer Ingelheim Pharmaceuticals

Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.

Boehringer Ingelheim Pharmaceuticals

Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.

Boehringer Ingelheim Pharmaceuticals

Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.

Boehringer Ingelheim Pharmaceuticals

Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.

Boehringer Ingelheim Pharmaceuticals

Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.

Boehringer Ingelheim Pharmaceuticals

Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones.

Boehringer Ingelheim Pharmaceuticals

NMR line-broadening and transferred NOESY as a medicinal chemistry tool for studying inhibitors of the hepatitis C virus NS3 protease domain.

Boehringer Ingelheim Pharmaceuticals

Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.

Boehringer Ingelheim Pharmaceuticals

Indole RSK inhibitors. Part 1: discovery and initial SAR.

Boehringer Ingelheim Pharmaceuticals

Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13.

Boehringer Ingelheim Pharmaceuticals

Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.

Boehringer Ingelheim Pharmaceuticals

Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.

Boehringer Ingelheim Pharmaceuticals

Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.

Boehringer Ingelheim Pharmaceuticals

Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: optimization of drug-like properties and target independent parameters.

Boehringer Ingelheim Pharmaceuticals

1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability.

Boehringer Ingelheim Pharmaceuticals

Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain.

Boehringer Ingelheim Pharmaceuticals

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 2, optimization for blood pressure reduction in spontaneously hypertensive rats.

Boehringer Ingelheim Pharmaceuticals

SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability.

Boehringer Ingelheim Pharmaceuticals

Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method.

Boehringer Ingelheim Pharmaceuticals

Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.

Boehringer Ingelheim Pharmaceuticals

Optimization of piperidyl-ureas as inhibitors of soluble epoxide hydrolase.

Boehringer Ingelheim Pharmaceuticals

Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase.

Boehringer Ingelheim Pharmaceuticals

Structure-based optimization of arylamides as inhibitors of soluble epoxide hydrolase.

Boehringer Ingelheim Pharmaceuticals

Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.

Boehringer Ingelheim Pharmaceuticals

A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.

Boehringer Ingelheim Pharmaceuticals

5-Aminomethylbenzimidazoles as potent ITK antagonists.

Boehringer Ingelheim Pharmaceuticals

Morpholine containing CB2 selective agonists.

Boehringer Ingelheim Pharmaceuticals

Discovery and optimization of p38 inhibitors via computer-assisted drug design.

Boehringer Ingelheim Pharmaceuticals

New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.

Boehringer Ingelheim Pharmaceuticals

Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.

Boehringer Ingelheim Pharmaceuticals

Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors.

Boehringer Ingelheim Pharmaceuticals

Discovery of potent and selective PKC-theta inhibitors.

Boehringer Ingelheim Pharmaceuticals

Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.

Boehringer Ingelheim Pharmaceuticals

Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.

Boehringer Ingelheim Pharmaceuticals

A concise asymmetric route for the synthesis of a novel class of glucocorticoid mimetics containing a trifluoromethyl-substituted alcohol.

Boehringer Ingelheim Pharmaceuticals

Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.

Boehringer Ingelheim Pharmaceuticals

The kinetics of binding to p38MAP kinase by analogues of BIRB 796.

Boehringer Ingelheim Pharmaceuticals

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).

Boehringer Ingelheim Pharmaceuticals

Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors.

Boehringer Ingelheim Pharmaceuticals

Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.

Boehringer Ingelheim Pharmaceuticals

Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357.

Boehringer Ingelheim Pharmaceuticals

Phosphotyrosine-containing dipeptides as high-affinity ligands for the p56lck SH2 domain.

Boehringer Ingelheim Pharmaceuticals

Discovery and optimization of pyrazole amides as antagonists of CCR1.

Boehringer Ingelheim Pharmaceuticals

A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.

Boehringer Ingelheim Pharmaceuticals

Antiinflammatory 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones: novel inhibitors of COX-2.

Boehringer Ingelheim Pharmaceuticals

Identification of novel azaindazole CCR1 antagonist clinical candidates.

Boehringer Ingelheim Pharmaceuticals

Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as antagonists of the NMDA receptor-channel complex.

Boehringer Ingelheim Pharmaceuticals

Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity.

Boehringer Ingelheim Pharmaceuticals

Time-resolved ligand exchange reactions: kinetic models for competitive inhibitors with recombinant human renin.

Boehringer Ingelheim Pharmaceuticals

Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones.

Boehringer Ingelheim Pharmaceuticals

Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.

Boehringer Ingelheim Pharmaceuticals

Effect of structure on potency and selectivity in 2,6-disubstituted 4-(2-arylethenyl)phenol lipoxygenase inhibitors.

Boehringer Ingelheim Pharmaceuticals

Discovery and optimization of oxadiazole-based FLAP inhibitors.

Boehringer Ingelheim Pharmaceuticals

Inhibition of human leukocyte elastase by N-substituted peptides containing alpha,alpha-difluorostatone residues at P1.

Boehringer Ingelheim Pharmaceuticals

Cycloalkyl nitrile pyrazolo pyridones as Janus kinase inhibitors

Merck Sharp & Dohme

Phenyl-dihydropyridine derivatives as aldosterone synthase inhibitors

Hoffmann-La Roche

Phenyl-dihydropyridine derivatives as inhibitors of aldosterone synthase

Hoffmann-La Roche

Imidazo[2,1-b]thiazole derivatives, their preparation and use as medicaments

Laboratories Del Dr. Esteve

Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors

Beigene

Therapeutic agent for FGFR inhibitor-resistant cancer

Taiho Pharmaceutical

Factor XIa inhibitors

Merck Sharp & Dohme

Benzofurans substituted with secondary benzamide as HCV inhibitors

Bristol-Myers Squibb

MNK inhibitors and methods related thereto

Effector Therapeutics

Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-B] pyridine and pyrazolo [3, 4-B] pyridine derivatives as protein kinase inhibitors

Arrien Pharmaceuticals

Ethynyl derivatives

Hoffmann-La Roche

2-benzyl-benzimidazole complement factor B inhibitors and uses thereof

Novartis

Compounds and compositions for the inhibition of NAMPT

Forma Tm

Polyetherimide compositions and methods for the manufacture and use thereof

Sabic Global Technologies

Inhibitors of sodium glucose cotransporter 1

Lexicon Pharmaceuticals

Piperidine/piperazine derivatives

Janssen Pharmaceutica

Piperidinyl-indole derivatives complement factor B inhibitors and uses thereof

Novartis

Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies.

National Tsing Hua University

Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity.

Gilead Sciences

A new series of C3-aza carbocyclic influenza neuraminidase inhibitors: synthesis and inhibitory activity.

Gilead Sciences