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Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.

Novartis Institutes of Biomedical Research (Nibr)
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.

Novartis Institutes For Biomedical Research
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Ka inhibitor with high PI3K isoform selectivity and potent cellular activity.

Novartis Institutes For Biomedical Research
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Novartis Institutes For Biomedical Research
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.

Novartis Institutes For Biomedical Research
Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.

Novartis Institutes For Biomedical Research
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Novartis Institutes For Biomedical Research
The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.

Novartis Institutes For Biomedical Research
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.

Novartis Institute For Biomedical Research
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.

Novartis Pharma
4-Amidinoindan-1-one 2'-amidinohydrazone: a new potent and selective inhibitor of S-Adenosylmethionine decarboxylase.

Ciba-Geigy
2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.

Novartis Pharmaceuticals
New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.

Novartis Institutes For Biomedical Research
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Novartis Institute For Biomedical Research
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.

Novartis Institute of Biomedical Research
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Novartis Institutes For Biomedical Research
Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.

Novartis Institutes For Biomedical Research
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Novartis Institutes For Biomedical Research
Discovery of a new class of catalytic topoisomerase II inhibitors targeting the ATP-binding site by structure based design. Part I.

Novartis Institutes For Biomedical Research
Valsartan, a potent, orally active angiotensin II antagonist developed from the structurally new amino acid series

TBA
Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4.

Novartis Pharma
In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase.

Novartis Institutes for BioMedical Research
Entry into a new class of protein kinase inhibitors by pseudo ring design.

Novartis Institutes For Biomedical Research
Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.

Novartis Institutes for Biomedical Research
A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.

Novartis Institutes For Biomedical Research
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.

Novartis Institutes For Biomedical Research
Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.

Novartis Institutes For Biomedical Research
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.

Novartis Pharma
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.

Novartis Institutes For Biomedical Research
Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne.

Novartis Pharma
Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1.

Novartis Pharmaceuticals
Structure-based design of potent linear peptide inhibitors of the YAP-TEAD protein-protein interaction derived from the YAP omega-loop sequence.

Novartis Institutes For Biomedical Research
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.

Novartis Institutes For Biomedical Research
Mapping the X(+1) binding site of the Grb2-SH2 domain with alpha,alpha-disubstituted cyclic alpha-amino acids.

Novartis Pharma
Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2.

Novartis Pharmaceuticals
Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic.

Novartis Pharma
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.

Novartis
Highly potent inhibitors of the Grb2-SH2 domain.

Novartis Pharma
Structure-based design of peptidomimetic ligands of the Grb2-SH2 domain.

Novartis Pharma
Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.

Novartis Pharma
Potent antagonists of the SH2 domain of Grb2: optimization of the X+1 position of 3-amino-Z-Tyr(PO3H2)-X+1-Asn-NH2.

Novartis Pharma
Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain.

Novartis Pharma
4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase.

Ciba Pharmaceuticals
Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.

Ciba-Geigy
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Novartis Institutes For Biomedical Research
S-adenosylmethionine decarboxylase inhibitors: new aryl and heteroaryl analogues of methylglyoxal bis(guanylhydrazone).

Ciba-Geigy
Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.

Ciba-Geigy
Structure-based optimisation of 2-aminobenzylstatine derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome.

Novartis Pharma
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.

Novartis Institutes For Biomedical Research
2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.

Novartis Institutes For Biomedical Research
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.

Novartis Institutes For Biomedical Research
Nonpeptidic angiotensin II antagonists: synthesis and in vitro activity of a series of novel naphthalene and tetrahydronaphthalene derivatives.

Ciba-Geigy
SUBSTITUTED PYRAZINE-2-CARBOXAMIDES AS HPK1 INHIBITORS FOR THE TREATMENT OF CANCER

Astrazeneca
Process route of compound of formula (IV), crystal form and preparation method therefor

Shandong Danhong Pharmaceutical Co.
Oxy-cyanoquinolinone PDE9 inhibitors

Merck, Sharp & Dohme
Compounds and uses thereof

Kala Pharmaceuticals
Heterocyclic ring and carbocyclic derivative

Shionogi
Benzimidazole tetrahydrofuran derivatives

Merck Sharp & Dohme
Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity.

Jamia Hamdard University
Facile dimethyl amino group triggered cyclic sulfonamides synthesis and evaluation as alkaline phosphatase inhibitors.

University of Karachi
Bicyclic sulfonamide compounds as sodium channel inhibitors

Amgen
TRPA1 antagonists

Abbvie
Biochemical and structural analysis of inhibitors targeting the ADC-7 cephalosporinase of Acinetobacter baumannii.

Grand Valley State University
Amino-pyridine-containing spleen tyrosine kinase (SYK) inhibitors

Merck Sharp & Dohme
A facile one-pot synthesis of 2-arylamino-5-aryloxylalkyl-1,3,4-oxadiazoles and their urease inhibition studies.

Mirpur University of Science and Technology (Must)
Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof

Acetylon Pharmaceuticals
Fluorescence Linked Enzyme Chemoproteomic Strategy for Discovery of a Potent and Selective DAPK1 and ZIPK Inhibitor.

Duke University Medical Center
Substituted imidazopyr- and imidazotri-azines

Osi Pharmaceuticals
Identification and characterization of new inhibitors of fungal homoserine kinase.

Mcmaster University
Muscarinic cholinergic binding in rat brain.

TBA
Characterization of high affinity [3H]pirenzepine and (-)-[3H] quinuclidinyl benzilate binding to muscarinic cholinergic receptors in rabbit peripheral lung.

University of Arizona
Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.

University of Pittsburgh
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.

Glaxo Group Research
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.

Johns Hopkins University