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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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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 LIFE SCIENCES LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 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, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, 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 Open superstar 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 30 PLUS year tenure till date June 2021, Around 35 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, 90 Lakh plus views on dozen plus blogs, 233 countries, 7 continents, 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 33 lakh plus views on New Drug Approvals Blog in 233 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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Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ


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(-)-32 as an off-white solid.
Analytical data
LCMS 418 [M+H]+1
H NMR (400 MHz, DMSO-d6) δ 8.23 (s, 1H), 6.88 (d, J = 8.0 Hz, 1H), 6.68 (s, 1H), 6.61 (dd,J = 11.2, 2.0 Hz, 1H), 6.49-6.38 (m, 2H), 6.33 (s, 1H), 5.61 (m, 1H), 4.88 (s, 2H), 4.20(t, J = 4.3 Hz, 2H), 3.35-3.18 (m, 6H).
Optical rotation [α]D20 -38.5° (c = 0.107, DMSO)

 

 

PAPER

Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ

Medivation, Inc., 525 Market Street, 36th Floor, San Francisco, California 94105, United States
Integral BioSciences, Pvt. Ltd., C-64, Hosiery Complex Phase II Extension, Noida, Uttar Pradesh 201306, India
§ Curadev, Pvt. Ltd., B-87, Sector 83, Noida, Uttar Pradesh 201305, India
Fundación Ciencia y Vida, Avenida Zañartu 1482, Ñuñoa, Santiago 7780272, Chile
Departamento de Ciencias Biológicas, Facultad de Ciencias Biológicas, Universidad Andrés Bello, Santiago 8370146, Chile
ACS Med. Chem. Lett., Article ASAP
DOI: 10.1021/acsmedchemlett.6b00356

Image result for Medivation, Inc

Son Pham

Son Pham

Associate Director, Medicinal Chemistry at Medivation

Roopa Rai

Roopa Rai

Sr. Director, Medicinal Chemistry at Medivation

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Brahmam Pujala

Brahmam Pujala

Senior Research Scientist at Integral Biosciences

Ashu Gupta

Ashu Gupta

Research Scientist at Integral Biosciences

rambabu guguloth

Rambabu guguloth

Abstract

Abstract Image

The aberrant activation of B-cells has been implicated in several types of cancers and hematological disorders. BTK and PI3Kδ are kinases responsible for B-cell signal transduction, and inhibitors of these enzymes have demonstrated clinical benefit in certain types of lymphoma. Simultaneous inhibition of these pathways could result in more robust responses or overcome resistance as observed in single agent use. We report a series of novel compounds that have low nanomolar potency against both BTK and PI3Kδ as well as acceptable PK properties that could be useful in the development of treatments against B-cell related diseases.

Image result for Curadev

Monali Banerjee

Director, R&D

Ms. Banerjee has more than 10 years of research experience, during which she has held positions of increasing responsibility. Her past organizations include TCG Lifesciences (Chembiotek) and Sphaera Pharma. Ms. Banerjee is a versatile scientist with a deep understanding of the fundamental issues that underlie various aspects of drug discovery. At Curadev, she has been responsible for target selection, patent analysis, pharmacophore design, assay development, ADME/PK and in vivo and in vitro pharmacology. Ms. Banerjee holds a Masters in Biochemistry and a Bachelors in Chemistry both from Kolkata University.

Nidhi Adlaka & Neha Munjal are developing a bioprocess for butanediol. Over the next few decades, chemical routes of manufacture will gradually be replaced by more environment friendly biological methods.Nidhi Adlaka & Neha Munjal are developing a bioprocess for butanediol. Over the next few decades, chemical routes of manufacture will gradually be replaced by more environment friendly biological methods.

Image result for Arjun Surya CURADEV

Dr. Arjun Surya, CSO, Curadev enthralling participants with anecdotes of his entrepreneurial jrney in drugdiscovery

Manish Tandon

Manish Tandon

Co-founder Curadev Pharma Pvt Ltd

//////////////B-cell BCR BTK inhibitor p110δ PI3K pyrazolopyrimidineNovel Dual Inhibitors, BTK , PI3Kδ, Medivation, Integral BioSciences,  Curadev, Fundación Ciencia y Vida, Departamento de Ciencias Biológicas,

Nc1ccc2CC(Cc2c1)n6nc(c3cc(F)c4OCCNc4c3)c5c(N)ncnc56

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

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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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