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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/28276280/patent-disclosure-requirements-for-therapeutic-antibody-patents
#1
Carmela De Luca, Anastassia Trifonova
Therapeutic antibodies have grown to become an important product class within the biopharmaceutical market. A prerequisite to their commercialization is adequate patent protection. Disclosure requirements and the types of claims available in different jurisdictions can impact the scope of protection available for antibodies. Areas covered: A comparative review of statutory bases, patent office practices and selected decisions in Canada, the United States and the United Kingdom related to disclosure requirements is provided...
March 9, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28270021/tropomyosin-receptor-kinase-inhibitors-an-updated-patent-review-for-2010-2016-part-ii
#2
Justin J Bailey, Ralf Schirrmacher, Kristen Farrell, Vadim Bernard-Gauthier
TrkA/B/C receptor activation supports growth, survival, and differentiation of discrete neuronal populations during development, adult life, and ageing but also plays numerous roles in human disease onset and progression. Trk-specific inhibitors have therapeutic applications in cancer and pain and thus constitute a growing area of interest in oncology and neurology. There has been substantial growth in the number of structural classes of Trk inhibitors and the number of industrial entrants to the Trk inhibitor field over the past six years...
March 8, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28270010/tropomyosin-receptor-kinase-inhibitors-an-updated-patent-review-for-2010-2016-part-i
#3
Justin J Bailey, Ralf Schirrmacher, Kristen Farrell, Vadim Bernard-Gauthier
Tropomyosin receptor kinases (TrkA/B/C) play crucial roles in the development and maintenance of the nervous system, and aberrant expression of Trk has been implicated in neurological disorders as well as neural and non-neural neoplasms. Patent activity encompassing Trk inhibitors has grown substantially over the last 6 years, recognized by a rise in the number of pharmaceutical entrants to the field and the escalation of novel inhibitor chemotypes. Area covered: In Part I of this two part review, a biological and structural overview of Trk is provided in the context of Trk as a therapeutic target for cancer and pain, followed by the report of recent patent literature claiming small molecule inhibitors of Trk family kinases or which describe inhibitors developed for other kinase targets but include noteworthy Trk inhibition/application...
March 8, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28117607/leucine-rich-repeat-kinase-2-inhibitors-a-patent-review-2014-2016
#4
Paul Galatsis
Leucine-rich repeat kinase 2 (LRRK2) is a member of the Tyrosine Kinase-Like (TKL) branch of the kinome tree and is a multi-domain protein that includes GTPase and kinase activity. While genome-wide association studies (GWAS) has linked LRRK2 with Crohn's disease and leprosy, it has received the greatest attention due to it being implicated as one of the genetic loci associated with autosomal dominant inheritance in Parkinson's disease (PD). Areas covered: In this review, the small molecule patent literature from 2014-2016 with a focus on composition of matter and use patents was surveyed...
January 31, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28064544/recent-advances-of-pyrrolopyridines-derivatives-a-patent-and-literature-review
#5
Mohammed I El-Gamal, Hanan S Anbar
Several pyrrolopyridines or azaindoles have been reported in the literature as biologically-active molecules. Most of them are anticancer agents, and few possess other therapeutic effects. Areas covered: The most recent biologically-active pyrrolopyridine derivatives have been reviewed from the patents and research articles published from 2010 to the mid of 2016. Their structural and biological features have been explained. In general, the pyrrolopyridine scaffold mimics the purine ring of the ATP molecule...
January 27, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28121202/progress-of-middle-east-respiratory-syndrome-coronavirus-vaccines-a-patent-review
#6
Jiwon Choi, Mi-Gyeong Kim, Yu-Kyoung Oh, Young Bong Kim
Middle East respiratory syndrome coronavirus (MERS-CoV) has emerged as a new pathogen, causing severe complications and a high case fatality rate. No direct treatments are available as yet, highlighting the importance of prevention through suitable vaccination regimes. The viral spike (S) protein has been characterized as a key target antigen for vaccines. In particular, S protein domains have been utilized to produce high titers of neutralizing antibodies. Areas covered: Since the first report of MERS-CoV infection, a limited number of MERS-CoV-specific patents have been filed...
January 25, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28076686/small-molecule-hiv-1-entry-inhibitors-targeting-gp120-and-gp41-a-patent-review-2010-2015
#7
Wen Li, Lu Lu, Weihua Li, Shibo Jiang
It is essential to discover and develop small-molecule HIV-1 entry inhibitors with suitable pharmaceutical properties. Areas covered: We review the development of small-molecule HIV-1 entry inhibitors as evidenced in patents, patent applications, and related research articles published between 2010 and 2015. Expert opinion: HIV-1 Env gp120 and gp41 are important targets for development of HIV-1 entry inhibitors. The Phe43 pocket in gp120 and the highly conserved hydrophobic pocket on gp41 NHR-trimer are important targets for identification of HIV-1 attachment and fusion inhibitors, respectively...
January 19, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28067079/mglu5-negative-allosteric-modulators-a-patent-review-2013-2016
#8
Kyle A Emmitte
The pursuit of small molecule mGlu5 NAMs as treatments for a variety of psychiatric and neurodegenerative disorders has developed into a mature field. In addition to extensive preclinical studies, multiple compounds have advanced into clinical trials with the most advanced studies occurring in patients with FXS, PD-LID, and MDD. Areas covered: This review begins with an update of the clinical activity with mGlu5 NAMs, and then moves into a summary of patent applications filed since 2013. The summaries are organized into three separate sections: (1) inventions centered on improvements to existing clinical compounds; (2) new small molecules that maintain the prototypical disubstituted alkyne chemotype found in many mGlu5 NAM compounds; and (3) new small molecules that are not from a disubstituted alkyne chemotype...
January 19, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28074661/inosine-5-monophosphate-dehydrogenase-impdh-inhibitors-a-patent-and-scientific-literature-review-2002-2016
#9
Gregory D Cuny, Chalada Suebsuwong, Soumya S Ray
Inosine-5'-monophosphate dehydrogenase (IMPDH) is an enzyme involved in the de novo biosynthesis of guanine nucleotides. To date human IMPDH inhibitors have been approved for prevention of organ transplant rejection and as anti-viral agents. More recently, the use of IMPDH inhibitors for other indications including cancer and pathogenic microorganisms has been pursued. Areas covered: IMPDH inhibitors disclosed primarily in the patent and scientific literature from 2002 to the present are discussed. Several interesting chemotypes that have not been pursued by patent protection are also highlighted...
January 11, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28051882/are-sigma-modulators-an-effective-opportunity-for-cancer-treatment-a-patent-overview-1996-2016
#10
Simona Collina, Emanuele Bignardi, Marta Rui, Daniela Rossi, Raffaella Gaggeri, Alice Zamagni, Michela Cortesi, Anna Tesei
Although several molecular targets against cancer have been identified, there is a continuous need for new therapeutic strategies. Sigma Receptors (SRs) overexpression has been recently associated to different cancer conditions. Therefore, novel anticancer agents targeting SRs may increase the specificity of therapies, overcoming some of the common drawbacks of conventional chemotherapy. Areas covered: The present review focuses on patent documents disclosing SR modulators with possible application in cancer therapy and diagnosis...
January 4, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28033734/selective-histone-deacetylase-small-molecule-inhibitors-recent-progress-and-perspectives
#11
Hai-Tao Qin, Huan-Qiu Li, Feng Liu
Since the first pan-HDAC inhibitor SAHA was approved by U.S. FDA 10 years ago, HDACs including SIRT1-7 have received significant attention due to the fact that aberrant histone deacetylase activtiy has been implicated in a variety of human diseases, such as cancers, virus infection, and neurodegenerative diseases. During the past years, a considerable achievement of development of isoform- or class-selective HDAC inhibitors has been made, yielding many drug candidates for further clinical studies, which represents a state-of-the-art technology in the drug discovery arena...
December 29, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27998196/recent-trends-in-neuropathic-pain-patents
#12
Rodolfo do Couto Maia
Neuropathic pain (NP) is one of the most important health problems faced nowadays. NP is a chronic disease that cannot be treated like other pain conditions because it is developed from a nerve injury that evolves into a permanent dysfunction of the central and/or peripheral nervous system. Therefore, it involves the participation of several systems and should be viewed as a multi-factorial disease that needs a whole new pharmacological strategy in order to achieve the desired pain relief. Areas covered: The Espacenet site was used as the main source in order to perform the patent research for NP treatment...
December 28, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28024125/recent-progress-on-curcumin-based-therapeutics-a-patent-review-2012-2016-part-i-curcumin
#13
Rita Maria Concettaa Di Martino, Barbara Luppi, Alessandraa Bisi, Silviaa Gobbi, Angela Rampa, Angela Abruzzo, Federica Bellutia
curcumin is the main bioactive component contained in Curcuma Longa, largely employed in traditional medicine. Recently, beneficial properties, useful for prevention and treatment of several disorders, have been discovered for this compound. Peculiar structural feature is an α,β-unsaturated carbonyl system essential for establishing contacts with critical cysteine residues of several targets. This distinctive mechanism of action imparts to the molecule the ability to affect a large number of targets, accounting for its pleiotropic behaviour and definition of "privileged structure"...
December 26, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27977313/thioredoxin-reductase-inhibitors-a-patent-review
#14
Baoxin Zhang, Junmin Zhang, Shoujiao Peng, Ruijuan Liu, Xinming Li, Yanan Hou, Xiao Han, Jianguo Fang
Mammalian thioredoxin reductases (TrxRs) are selenocysteine-containing homodimeric flavin enzymes that catalyze the NADPH-dependent reduction of oxidized thioredoxins. Increasing evidence indicates that TrxRs are potential targets for anticancer drug development. This review summarizes patented inhibitors of mammalian TrxRs with an emphasis on those having potential applications in treatment of cancer. Areas covered: A background introduction of TrxR as well as the relevance of TrxR and cancer is provided in the first part of this review...
December 26, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28276283/novel-fused-pyrimidine-and-isoquinoline-derivatives-as-potent-hiv-1-nnrtis-a-patent-evaluation-of-wo2016105532a1-wo2016105534a1-and-wo2016105564a1
#15
Dongwei Kang, Zhipeng Huo, Gaochan Wu, Jiabao Xu, Peng Zhan, Xinyong Liu
In the three patent applications, the impact of changing the pyrimidine core of the rilpivirine (RPV) to a variety of alternative fused cores was explored, culminating in the identification of a series of conformationally restricted compounds with comparable potencies against WT and mutant HIV-1 strains with those of efavirenz (EFV) and RPV, and higher security in the Human Ether-a-go-go-Related Gene (hERG) assay. Areas covered: The present review provides a fused pyrimidine and isoquinoline derivatives as potent HIV-1 NNRTIs, and highlights the conformational restriction strategies in the development of NNRTIs...
April 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28266880/the-challenges-of-joint-performance-to-method-patents
#16
Feng-Chi Chen
Biotech patents are facing increasingly stern challenges. The patent statue holds that a multi-step method patent is not directly infringed unless all steps are carried out and attributed to a single entity. When separate steps are performed jointly by two or more parties, those parties are liable for divided infringement if there exists a direct infringement. Possibilities thus exist for unauthorized but non-infringing joint performance, i.e. enforcing a method patent will be difficult if joint performance stands as a valid defense against direct infringement...
April 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28048944/rho-kinase-inhibitors-a-patent-review-2014-2016
#17
Olivier Defert, Sandro Boland
The Rho-kinases (ROCK), ROCK1 and ROCK2, are potent, widespread biochemical modulators which have been extensively studied. Due to the involvement of ROCKs in multiple biological processes, ROCK inhibitors have pleiotropic actions and may be of relevance for a number of therapeutic applications. The drawback is however that their use might be limited by occurrence of side effects. Areas covered: Since the publication of the latest review in 2014, there have been significant advances in the field of ROCK inhibitors...
April 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27976971/thiadiazole-inhibitors-a-patent-review
#18
Kamal M Dawood, Thoraya A Farghaly
Four isomeric structures of thiadiazole motifs have outstanding pharmacological inhibitory applications are reported in this review. Thiadiazole nucleus is present in several biologically active natural products and commercial drugs. Most of thiadiazoles reported herein are emphasized to have broad spectrum of medicinal activities. Areas covered: This review represents the recent inhibitory activities of thiadiazole isomeric scaffolds and their broad-spectrum biological applications published as full texts during 2010-2016 as well as the patents published during 2005-2016...
April 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27976968/a-fgfr1-inhibitor-patent-review-progress-since-2010
#19
Tao Yu, Yanyan Yang, Yan Liu, Yinfeng Zhang, Hong Xu, Mengpeng Li, Murugavel Ponnusamy, Kun Wang, Jian-Xun Wang, Pei-Feng Li
FGFR1 is a well known molecular target for anticancer therapy. Many studies have proved that the regulation of FGFR1 activity is a promising therapeutic approach to treat a series of cancers. Therefore, the development of potent inhibitors has consequently become a key focus in the present drug discovery, and it is encouraging that several highly selective FGFR1 inhibitors have been identified from various sources in recent years. Areas covered: This article reviews patents and patent applications related to selective FGFR1 inhibitors published from 2010 to 2016...
April 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27967269/small-molecule-inhibitors-of-hepatitis-c-virus-hcv-non-structural-protein-5a-ns5a-a-patent-review-2010-2015
#20
Yan A Ivanenkov, Vladimir A Aladinskiy, Nikolay A Bushkov, Andrey A Ayginin, Alexander G Majouga, Alexandre V Ivachtchenko
Non-structural 5A (NS5A) protein has achieved a considerable attention as an attractive target for the treatment of hepatitis C (HCV). A number of novel NS5A inhibitors have been reported to date. Several drugs having favorable ADME properties and mild side effects were launched into the pharmaceutical market. For instance, daclatasvir was launched in 2014, elbasvir is currently undergoing registration, ledipasvir was launched in 2014 as a fixed-dose combination with sofosbuvir (NS5B inhibitor). Areas covered: Thomson integrity database and SciFinder database were used as a valuable source to collect the patents on small-molecule NS5A inhibitors...
April 2017: Expert Opinion on Therapeutic Patents
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