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CSIR, INDIA-WO PATENT–synthesis of amprenavir and saquinavir

New Drug Approvals



A process for synthesis of syn azido epoxide and its use as intermediate in the synthesis of amprenavir and saquinavir
Published as ———WO-2013105118
Council of Scientific & Industrial Research


Gadakh, Sunita, Khanderao; Rekula, Reddy, Santhosh; Sudalai, Arumugam
Publication date 18-JUL-2013

HIV protease inhibitor

Disclosed herein is a novel route of synthesis of syn azide epoxide of formu 5, which is used as a common intermdeiate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt- catalyzed hydrolyti kinetic resolution of racemic anti-(2SR, 3SR) – 3 -azido – 4 -phenyl – 1, 2- epoxybutane (azido-epoxide

IN2012DE82 10-JAN-2012 [priority]

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Genentech announced positive results from the Phase 3 CLL11 study, Leukemia Trial

New Drug Approvals


Obinutuzumab (GA101)


Genentech announced positive results from the Phase 3 CLL11 study. At a pre-planned interim analysis, an independent data monitoring committee determined that the study met its primary endpoint showing that GA101 plus chlorambucil helped people live significantly longer without their disease worsening (progression-free survival; PFS) compared to Rituxan (rituximab) plus chlorambucil.

The CLL11 study is being conducted in cooperation with the German CLL Study Group (GCLLSG). These final data were reached well ahead of the target completion date in 2014 as a result of the magnitude of difference seen between the two study arms.


Afutuzumab is a monoclonal antibody being developed by Hoffmann-La Roche Inc. for the treatment of lymphoma.[1] It acts as an immunomodulator.[2][3] It was renamed obinutuzumab in 2009.[4]

Class/mechanism: Glyco-engineered anti-CD20 IgG1 type II monoclonal antibody. Engineered with a modified elbow hinge residue (valine instead…

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Alkermes unveils three new drug candidates

New Drug Approvals

Alkermes has unveiled three new drug candidates, including: a monomethyl fumarate (MMF) prodrug programme for the treatment of multiple sclerosis; ALKS 7106 for the treatment of pain; and RDB 1419, a cancer immunotherapy candidate based on interleukin-2 (IL-2) and its receptors, Alkermes’ first proprietary biologic.

According to Alkermes, these drug candidates demonstrate the company’s focus on unmet medical needs in specific patient populations and show the productivity of its expanded R&D capabilities.

read all at





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Natural Remedies for Ulcerative Colitis

New Drug Approvals


Written by Michael Sapko for

There are a number of medical treatments available to manage ulcerative colitis. Modern therapy is targeted at preventing flares and inducing remission (at least temporarily). These medications, however, have serious side effects, especially when taken for long periods. Corticosteroids, for example, can cause a number of cosmetic, psychological, and hormonal problems. Many patients simply cannot tolerate these medications. Children have particular problems with standard medications. When compliance with prescribed medicines is poor, treatment failure is common.1,2 Thus, many patients turn to natural remedies for their ulcerative colitis..

Some herbal or organic remedies may help promote gut health and prolong the time between remissions (flares).

  • Dietary modification includes elimination of food allergens and optimizing living conditions. A relatively high proportion of Europeans (either primary or of European descent) have an allergy to gluten, a substance found…

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Mavoglurant (AFQ-056) is an experimental drug candidate for the treatment of fragile X syndrome

New Drug Approvals



Mavoglurant (AFQ-056) is an experimental drug candidate for the treatment of fragile X syndrome.[1] It exerts its effect as an antagonist of the metabotropic glutamate receptor 5 (mGLU5).[2]

Mavoglurant is under development by Novartis and is currently in Phase II and Phase III clinical trials.[1][3] If successful, it would be the first drug to treat the underlying disorder instead of the symptoms of fragile X syndrome.[4]


  1. P. Cole (2012). “Mavoglurant”. Drugs of the Future37 (1): 7–12. doi:10.1358/dof.2012.37.1.1772147. 
  2. Levenga, J; Hayashi, S; De Vrij, FM; Koekkoek, SK; Van Der Linde, HC; Nieuwenhuizen, I; Song, C; Buijsen, RA et al. (2011). “AFQ056, a new mGluR5 antagonist for treatment of fragile X syndrome”. Neurobiology of disease42 (3): 311–7. doi:10.1016/j.nbd.2011.01.022. PMID 21316452. 
  3.  Jacquemont…

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