N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides as BACE1 inhibitors: a patent evaluation of WO2013041499 [0.03%]
作为BACE1抑制剂的N-(3-(2-氨基-6,6-二氟-4,4a,5,6,7,7a-六氢环戊并[e][1,3]恶嗪-4-基)苯基)胺类化合物:对WO2013041499专利申请的评估
Jean Dessolin
Jean Dessolin
A new series of oxazin amides have been synthesized from isoxazoles using a reaction to increase the heterocyclic ring size and were evaluated as BACE1 inhibitors. The innovative compounds were able to diminish amyloid-β peptide concentrat...
Alberto Leoni,Alessandra Locatelli,Rita Morigi et al.
Alberto Leoni et al.
Introduction: Thiazole is a well-known five-membered heterocyclic compound. Various methods have been worked out for its synthesis. In the last few decades, a lot of work has been done on thiazole ring in order to find ne...
Mineralocorticoid receptor modulators: a patent review (2007 - 2012) [0.03%]
盐皮质激素受体调节剂专利回顾(2007-2012)
Matthieu Collin,Frederic Niemann,Frédéric Jaisser
Matthieu Collin
Introduction: Considered for years as a 'renal hormone' leading to the control of renal excretion of minerals (explaining the term 'mineralocorticoid' used to describe this hormone), aldosterone is now recognized as a key...
Should ANVISA be permitted to reject pharmaceutical patent applications in Brazil? [0.03%]
巴西应允许国家卫生监督局拒绝药品专利申请吗?
Lisa L Mueller,Silvia Moreira Taketsuma Costa
Lisa L Mueller
Pharmaceutical manufacturers who seek new markets for expansion are particularly attracted to Brazil given its potential for growth and the expectation that it will be the fifth largest drug market by 2015. Given the significance of Brazil ...
Highly selective Janus kinase 3 inhibitors based on a pyrrolo[2,3-d]pyrimidine scaffold: evaluation of WO2013085802 [0.03%]
基于吡咯并[2,3-d]嘧啶的jak3高选择性抑制剂:评估wo2013085802
Peter Norman
Peter Norman
A series of pyrrolo[2,3-d]pyrimidine derivatives have previously been claimed as Janus kinase (JAK) 1 selective inhibitors. Introduction of a 4-aryl substituent onto this bicyclic scaffold modulates the JAK selectivity profile, thus providi...
Philip Webber
Philip Webber
For over 20 years, the US Patent & Trademark Office (USPTO) has been granting patents to DNA sequences. But on 13 June 2013, the US Supreme Court decided that genomic DNA sequences are unpatentable because they are products of nature. This ...
New developments around histamine H(3) receptor antagonists/inverse agonists: a patent review (2010 - present) [0.03%]
组胺H3受体拮抗剂/反向激动剂的新进展:2010至今专利回顾
Dorota Łażewska,Katarzyna Kieć-Kononowicz
Dorota Łażewska
Introduction: Histamine H3 receptor (H3R) is involved in the central and peripheral regulation of levels of histamine and other neurotransmitters (e.g., acetylcholine, noradrenaline, dopamine or serotonin). H3R antagonist...
Small molecule inhibitors of PIM1 kinase: July 2009 to February 2013 patent update [0.03%]
蛋白激酶PIM1的小分子抑制剂:2009年7月~2013年2月专利动态更新
Gubbi M Arunesh,Ekambaram Shanthi,Mudeenahally H Krishna et al.
Gubbi M Arunesh et al.
Introduction: The proviral insertion in murine (PIM) lymphoma proteins for which three isoforms, PIM1, PIM2 and PIM3 have been identified, belonging to the family of serine/threonine kinases has emerged recently as an imp...
Akul Y Mehta,Yingzi Jin,Umesh R Desai
Akul Y Mehta
Introduction: Thromboembolic incidences have increased nearly 33% in the past decade and directly affect nearly 0.5% of the population. Heparin, warfarin and current direct thrombin inhibitors (DTIs), the primary anticoag...
Somnath Halder,Sanjay Kumar,Rajiv Sharma
Somnath Halder
Introduction: Type 2 diabetes (T2D) is a complex metabolic disorder characterized by persistent hyperglycemia and a wide range of underlying metabolic defects. The prevalence and incidence of T2D are expected to dramatica...