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GDC-0919; NLG-919; RG-6078

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MF C18H22N2O
MW: 282.17321

GDC-0919; NLG-919; RG-6078, GDC0919; GDC-0919; GDC 0919; NLG919; NLG 919; NLG-919; RG6078; RG-6078; RG 6078.

 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol
CAS No.1402836-58-1

GDC-0919, also known as NLG919 and RG6078, is an orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, NLG919 targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the essential amino acid tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, this agent increases tryptophan levels, restores the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, T-lymphocytes, and causes a reduction in tumor-associated regulatory T-cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells

  • Originator Lankenau Institute for Medical Research
  • Developer Genentech; NewLink Genetics Corporation
  • Class Antineoplastics; Small molecules
  • Mechanism of Action Immunomodulators; Indoleamine-pyrrole 2,3-dioxygenase inhibitors

Phase I Solid tumours

Patent ID Date Patent Title
US2015210769 2015-07-30 ANTIBODY MOLECULES TO PD-1 AND USES THEREOF
US2014066625 2014-03-06 Fused Imidazole Derivatives Useful as IDO Inhibitors
  • 27 Sep 2015 Pharmacokinetics results from a phase-I clinical trial in Solid tumours presented at the European Cancer Congress 2015 (ECC-2015)
  • 27 Sep 2015 Positive efficacy and safety results from a phase-I clinical trial in Solid tumours presented at the European Cancer Congress 2015 (ECC-2015)
  • 31 Jul 2015 Phase-I clinical trials in Solid tumours (Combination therapy, Late-stage disease, Second-line therapy or greater) in USA (PO) (NCT02471846)

PATENT

http://www.google.com/patents/WO2012142237A1?cl=en

str1

PATENT

US-20160002249-A1 / 2016-01-07

Fused Imidazole Derivatives Useful as IDO Inhibitors

1304Image loading...1-cyclohexyl-2-(5H-imidazo[5,1- a]isoindol-5-yl)ethanol79 1H NMR (a mixture of diastereomers) 1.10-1.37 (m, 6H), 1.66-1.80 (m, 5H), 2.05 (m, 2H), 2.15 (m, 1H), 3.72 (m, 1H), 5.36 and 5.46 (two m, 1H), 7.16 (s, 1H), 7.25 (m, 1H), 7.34 (m, 1H), 7.43 (d, 1H, J = 7.6 Hz), 7.54 (d, 1H, J = 7.6 Hz), 7.80 (s, 1H)

WO2011056652A1 * Oct 27, 2010 May 12, 2011 Newlink Genetics Imidazole derivatives as ido inhibitors
WO2012142237A1 * Apr 12, 2012 Oct 18, 2012 Newlink Geneticks Corporation Fused imidazole derivatives useful as ido inhibitors
WO2014159248A1 Mar 10, 2014 Oct 2, 2014 Newlink Genetics Corporation Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization
US8722720 Oct 27, 2010 May 13, 2014 Newlink Genetics Corporation Imidazole derivatives as IDO inhibitors
US9260434 Oct 14, 2013 Feb 16, 2016 Newlink Genetics Corporation Fused imidazole derivatives useful as IDO inhibitors
US20140066625 * Oct 14, 2013 Mar 6, 2014 Newlink Genetics Corporation Fused Imidazole Derivatives Useful as IDO Inhibitors
US20160002249 * Jul 8, 2015 Jan 7, 2016 Newlink Genetics Corporation Fused Imidazole Derivatives Useful as IDO Inhibitors

REFERENCES

Nature Reviews Drug Discovery14,373(2015)doi:10.1038/nrd4658

http://www.ncbi.nlm.nih.gov/pubmed/21517759

http://www.roche.com/irp150128-annex.pdf

/////CRD1152, CRD 1152, CRD-1152, Curadev,  Research Collaboration, Licensing Agreement, Develop,  Cancer Immunotherapeutic, IDO1 and TDO inhibitors

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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 29 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 29 year tenure till date Aug 2016, Around 30 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 25 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 13 lakh plus views on New Drug Approvals Blog in 212 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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