PMID

Data

Article Title

Organization

Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].

Roche Palo Alto

Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.

Roche Palo Alto

Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism.

Roche Palo Alto

Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.

Roche Palo Alto

Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.

Roche Palo Alto

Discovery of a novel series of 4-quinolone JNK inhibitors.

Roche Palo Alto

2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression.

Roche Palo Alto

Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.

Roche Palo Alto

Discovery of potent and bioavailable GSK-3beta inhibitors.

Roche Palo Alto

Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.

Roche Palo Alto

Design and synthesis of novel CCR3 antagonists.

Roche Palo Alto

3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.

Roche Palo Alto

Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors

Roche Palo Alto

Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.

Roche Palo Alto

Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain.

Roche Palo Alto

X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.

Roche Palo Alto

Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.

Roche Palo Alto

Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.

Roche Palo Alto

Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.

Roche Palo Alto

Spiropiperidine CCR5 antagonists.

Roche Palo Alto

Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.

Roche Palo Alto

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: synthesis and optimization studies of benzothiazine-substituted tetramic acids.

Roche Palo Alto

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 4: structure-based design, synthesis, and biological evaluation of benzo[d]isothiazole-1,1-dioxides.

Roche Palo Alto

Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.

Roche Palo Alto

Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.

Roche Palo Alto

Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist.

Roche Palo Alto

Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.

Roche Palo Alto

Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Roche Palo Alto

Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase.

Roche Palo Alto

Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist.

Roche Palo Alto

Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.

Roche Palo Alto

Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.

Roche Palo Alto

Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents.

Roche Palo Alto

Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors.

Roche Palo Alto

Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.

Roche Palo Alto

Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.

Roche Palo Alto

Cyclic amide bioisosterism: strategic application to the design and synthesis of HCV NS5B polymerase inhibitors.

Roche Palo Alto

Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.

Roche Palo Alto

Bifunctional compounds and use for reducing uric acid levels

Acquist

Heteroaromatic compounds and their use as dopamine D1 ligands

Pfizer

Cytotoxic and potent CYP1 inhibitors from the marine algae Cymopolia barbata.

University of The West Indies

Beta adrenergic receptor binding in membrane preparations from mammalian brain.

TBA

Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.

Istituto Di Biostrutture E Bioimmagini-Cnr