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Ataciguat HMR-1766

Hoechst Marion Roussel De Gmbh

5-Chloro-2-[[(5-chloro-2-thienyl)sulfonyl]amino]-N-[4-(4-morpholinylsulfonyl)phenyl]benzamide

C21H19Cl2N3O6S3

UNII-QP166M390Q;

576.49306 g/mol
A guanylate cyclase activator potentially for the treatment of aortic valve stenosis.

 

CAS No. 254877-67-3

  • Originator sanofi-aventis
  • Developer Mayo Clinic; National Center for Advancing Translational Sciences; Sanofi; sanofi-aventis
  • Class Anthranilic acids; Benzamides; Cardiovascular therapies; Chlorobenzenes; Morpholines; Small molecules; Sulfonamides; Thiophenes
  • Mechanism of Action Guanylate cyclase stimulants
  • 30 Jun 2015 Mayo Clinic plans a phase II trial for Aortic valve stenosis in USA (NCT02481258)
  • 29 Jan 2014 Phase-I clinical trials in Aortic valve stenosis in USA (PO)
  • 01 Jan 2010 Discontinued – Phase-II for Peripheral arterial occlusive disorders in Austria, Canada, France, Germany, Italy, Poland, Portugal, Russia, South Africa and USA (PO) prior to 2010

SYNTHESIS

str1

 

The Intermediates hown above is used in next step shown below

 

str1

 

 

Paper

Organic Letters (2013), 15(7), 1638-1641

http://pubs.acs.org/doi/abs/10.1021/ol400411v

http://pubs.acs.org/doi/suppl/10.1021/ol400411v/suppl_file/ol400411v_si_001.pdf

 

Abstract Image

The Ru(II)-catalyzed intermolecular o-C–H amidation of arenes in N-benzoylated sulfoximine with sulfonyl azides is demonstrated. The reaction proceeds with broad substrate scope and tolerates various functional groups. Base hydrolysis of the amidation product provides the anthranilic acid derivatives and methylphenyl sulfoximine (MPS) directing group. This method is successfully employed for the synthesis of HMR 1766.

 

PATENT

WO 2009043495

http://www.google.com/patents/WO2009043495A1?cl=en

 

Patent

http://www.google.com/patents/WO2008124505A2?cl=en

HMR-1766 (ataciguat sodium, see patent publication WO2000002851)

 

PATENT

http://www.google.com/patents/WO2000002851A1?cl=en

Patent Submitted Granted
TRA COMBINATION THERAPIES [US2007238674] 2007-10-11
sGC STIMULATORS OR sGC ACTIVATORS ALONE AND IN COMBINATION WITH PDE5 INHBITORS FOR THE TREATMENT OF CYSTIC FIBROSIS [US2013035340] 2011-02-03 2013-02-07
SOLUBLE GUANYLATE CYCLASE (SGC) MODULATORS FOR TREATMENT OF LIPID RELATED DISORDERS [US2013123354] 2013-01-08 2013-05-16
Novel combination [US2005059660] 2004-07-29 2005-03-17
SGC STIMULATORS OF SGC ACTIVATORS IN COMBINATION WITH PDE5 INHBITORS FOR THE TREATMENT OF ERECTILE DYSFUNCTION [US2014288079] 2014-03-18 2014-09-25
Patent Submitted Granted
novel use of activators and stimulators of soluble guanylate cyclase for the prevention or treatment of renal disorders [US2010016305] 2010-01-21
HETEROARYL-SUBSTITUTED PIPERIDINES [US8119663] 2009-12-10 2012-02-21
Use of soluble guanylate cyclase activators for the treatment of Raynaud’s Phenomenon [US2009215769] 2009-08-27
Use of Activators of Soluble Guanylate Cyclase for Promoting Wound Healing [US2009221573] 2009-09-03
Use of Suluble Guanylate Cyclase Acitvators for Treating Acute and Chronic Lung Diseases [US2009286781] 2009-11-19
Use of Activators of Soluble Guanylate Cyclase for Treating Reperfusion Damage [US2009298822] 2009-12-03
HETEROCYCLIC DERIVATIVE AND USE THEREOF [US2011028493] 2011-02-03
SUBSTITUTED PIPERIDINES [US8202862] 2010-12-02 2012-06-19
METHODS AND COMPOSITIONS FOR TREATING CARDIAC DYSFUNCTIONS [US2009022729] 2009-01-22
sGC STIMULATORS [US2014323448] 2014-04-29 2014-10-30

Ataciguat.png

 

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C1COCCN1S(=O)(=O)C2=CC=C(C=C2)NC(=O)C3=C(C=CC(=C3)Cl)NS(=O)(=O)C4=CC=C(S4)Cl


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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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