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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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Zalicus Granted Composition-of-Matter Patent for Z944


Neurological disordersA class of its own

Z944 R1=F, R2=Cl

http://courses.washington.edu/phcol512/data/Tringham.pdf

disclaimer-The above link was available on the web freely, email  me immediately      amcrasto@gmail.com or call India +91  9323115463

Research Article

EPILEPSY

T-Type Calcium Channel Blockers That Attenuate Thalamic Burst Firing and Suppress Absence Seizures

  • Elizabeth Tringham, et AL

Sci Transl Med 15 February 2012 4:121ra19. DOI:10.1126/scitranslmed.3003120

…T-type calcium channel blockers, termed Z941 and Z944, were identified

http://stm.sciencemag.org/search?journal_search_keyword_go.y=8&submit=yes&fulltext=z944&andorexacttitleabs=and&andorexactfulltext=and&where=fulltext&journal_search_keyword_go.x=10&hopnum=1

Key Patent Provides Broad Coverage for Z944 through April 2029

CAMBRIDGE, Mass.Feb 20, 2013 – Zalicus Inc. , a biopharmaceutical company that discovers and develops novel treatments for patients suffering from pain, today announced that it has been granted a patent by the U.S. Patent and Trademark office (USPTO) covering its product candidate Z944. United States patent number 8,377,968 entitled “N-Piperidinyl Acetamide Derivatives as Calcium Channel Blockers” provides broad coverage for Z944 including compositions of matter and certain therapeutic methods of use through April 2029. Z944 is a novel, oral, T-type calcium channel blocker which has demonstrated efficacy in a number of preclinical inflammatory pain models and other disease models. Z944 completed Phase 1 single and multiple ascending dose clinical studies in late 2012 and the Company plans to continue further clinical development with Z944 during 2013.

“This key patent provides the foundation of a solid and enforceable intellectual property estate for Z944, with issued claims through April 2029,” commented Mark H.N. Corrigan, MD, President and CEO of Zalicus. “Based on our preclinical and early-stage clinical work, we are excited to further explore the potential of Z944 as a novel, oral, non-opioid pain treatment.”

Absence seizures — which are a common type of seizure in children with genetic generalized epilepsy — could now be treated by a potential new class of drugs with enhanced selectivity and efficacy over the drugs that are currently used in the clinic.

The molecular mechanisms underlying absence seizures are unclear; nevertheless, current literature indicates that the low-voltage-activated Cav3.1 and Cav3.2 T-type calcium channels have a crucial role. T-type calcium channels are also thought to be the site of action of the first-line drug ethosuximide; however, as it is nonspecific, ethosuximide causes side effects such as drowsiness, and not all patients respond to treatment. Therefore, the authors sought to identify a more specific and potent T-type calcium channel blocker.

A rational drug design approach produced two candidates — Z941 and Z944 — that had suitable properties for further development. They both had nanomolar affinities for Cav3.2 channels and significantly improved potencies compared to ethosuximide and valproate (another drug used for treating absence seizures). Importantly, Z944 has a higher affinity for the inactivated state of T-type channels (the state that is predominant during seizure activity) than for the closed state, and a higher affinity for neuronal T-type channels than for the cardiovascular-related channels.

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