The Experts below are selected from a list of 321 Experts worldwide ranked by ideXlab platform
Roberto Perrone - One of the best experts on this subject based on the ideXlab platform.
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5 ht7 receptor modulators a medicinal chemistry survey of recent Patent Literature 2004 2009
Expert Opinion on Therapeutic Patents, 2010Co-Authors: Marcello Leopoldo, Enza Lacivita, Francesco Berardi, Roberto PerroneAbstract:Importance of the field: The 5-HT7 receptors are discretely localized within the CNS (thalamus, hypothalamus, limbic and cortical regions). The 5-HT7 receptors are also present in smooth muscle cells from blood vessels and have been reported in gastrointestinal tract as well as in rat lumbar dorsal root and sympathetic ganglia. The 5-HT7 receptors have been implicated in depression, disorders related to circadian rhythms, pain and migraine. Thus, there is a great interest in developing potent and selective 5-HT7 receptor modulators.Areas covered in this review: This review article highlights the research advances published in the Patent Literature between January 2004 and December 2009, giving emphasis to the medicinal chemist's standpoint.What the reader will gain: Readers will rapidly gain an overview of the various 5-HT7 receptor modulators reported in the Patent Literature in the past 6 years. Furthermore, the readers will learn which structure type can interact with 5-HT7 receptor and also the differ...
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5-HT7 receptor modulators: a medicinal chemistry survey of recent Patent Literature (2004 – 2009)
Expert Opinion on Therapeutic Patents, 2010Co-Authors: Marcello Leopoldo, Enza Lacivita, Francesco Berardi, Roberto PerroneAbstract:Importance of the field: The 5-HT7 receptors are discretely localized within the CNS (thalamus, hypothalamus, limbic and cortical regions). The 5-HT7 receptors are also present in smooth muscle cells from blood vessels and have been reported in gastrointestinal tract as well as in rat lumbar dorsal root and sympathetic ganglia. The 5-HT7 receptors have been implicated in depression, disorders related to circadian rhythms, pain and migraine. Thus, there is a great interest in developing potent and selective 5-HT7 receptor modulators.Areas covered in this review: This review article highlights the research advances published in the Patent Literature between January 2004 and December 2009, giving emphasis to the medicinal chemist's standpoint.What the reader will gain: Readers will rapidly gain an overview of the various 5-HT7 receptor modulators reported in the Patent Literature in the past 6 years. Furthermore, the readers will learn which structure type can interact with 5-HT7 receptor and also the differ...
David L Hughes - One of the best experts on this subject based on the ideXlab platform.
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Review of the Patent Literature: Synthesis and Final Forms of Antiviral Drugs Tecovirimat and Baloxavir Marboxil
Organic Process Research & Development, 2019Co-Authors: David L HughesAbstract:This article reviews synthetic routes and final polymorphic forms of two recently approved antiviral drugs, TPOXX (tecovirimat) for the treatment of smallpox and Xofluza (baloxavir marboxil), a treatment for influenza. The Patent Literature was the source of information for synthetic routes and final forms.
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biocatalysis in drug development highlights of the recent Patent Literature
Organic Process Research & Development, 2018Co-Authors: David L HughesAbstract:The recent Patent Literature on biocatalysis is reviewed, with a focus on significant advances in enzymatic catalysis involving ketoreductases, transaminases, hydroxylases, sulfur oxidation, and nitrilase resolutions and a progress report on the emerging area of imine reductases highlighting collaborations between academia and pharmaceutical companies.
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Biocatalysis in Drug Development—Highlights of the Recent Patent Literature
Organic Process Research & Development, 2018Co-Authors: David L HughesAbstract:The recent Patent Literature on biocatalysis is reviewed, with a focus on significant advances in enzymatic catalysis involving ketoreductases, transaminases, hydroxylases, sulfur oxidation, and nitrilase resolutions and a progress report on the emerging area of imine reductases highlighting collaborations between academia and pharmaceutical companies.
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asymmetric organocatalysis in drug development highlights of recent Patent Literature
Organic Process Research & Development, 2018Co-Authors: David L HughesAbstract:Enantioselective organocatalytic reactions published in the recent Patent Literature are highlighted in this review and include inter- and intramolecular phase-transfer conjugate additions catalyzed by quaternized cinchona alkaloids, a Diels–Alder reaction catalyzed by oxazaborolidine complexes, asymmetric Betti reactions, the Lonza synthesis of l-carnitine, and several Corey–Bakshi–Shibata reductions.
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Asymmetric Organocatalysis in Drug Development—Highlights of Recent Patent Literature
Organic Process Research & Development, 2018Co-Authors: David L HughesAbstract:Enantioselective organocatalytic reactions published in the recent Patent Literature are highlighted in this review and include inter- and intramolecular phase-transfer conjugate additions catalyzed by quaternized cinchona alkaloids, a Diels–Alder reaction catalyzed by oxazaborolidine complexes, asymmetric Betti reactions, the Lonza synthesis of l-carnitine, and several Corey–Bakshi–Shibata reductions.
Marcello Leopoldo - One of the best experts on this subject based on the ideXlab platform.
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5 ht7 receptor modulators a medicinal chemistry survey of recent Patent Literature 2004 2009
Expert Opinion on Therapeutic Patents, 2010Co-Authors: Marcello Leopoldo, Enza Lacivita, Francesco Berardi, Roberto PerroneAbstract:Importance of the field: The 5-HT7 receptors are discretely localized within the CNS (thalamus, hypothalamus, limbic and cortical regions). The 5-HT7 receptors are also present in smooth muscle cells from blood vessels and have been reported in gastrointestinal tract as well as in rat lumbar dorsal root and sympathetic ganglia. The 5-HT7 receptors have been implicated in depression, disorders related to circadian rhythms, pain and migraine. Thus, there is a great interest in developing potent and selective 5-HT7 receptor modulators.Areas covered in this review: This review article highlights the research advances published in the Patent Literature between January 2004 and December 2009, giving emphasis to the medicinal chemist's standpoint.What the reader will gain: Readers will rapidly gain an overview of the various 5-HT7 receptor modulators reported in the Patent Literature in the past 6 years. Furthermore, the readers will learn which structure type can interact with 5-HT7 receptor and also the differ...
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5-HT7 receptor modulators: a medicinal chemistry survey of recent Patent Literature (2004 – 2009)
Expert Opinion on Therapeutic Patents, 2010Co-Authors: Marcello Leopoldo, Enza Lacivita, Francesco Berardi, Roberto PerroneAbstract:Importance of the field: The 5-HT7 receptors are discretely localized within the CNS (thalamus, hypothalamus, limbic and cortical regions). The 5-HT7 receptors are also present in smooth muscle cells from blood vessels and have been reported in gastrointestinal tract as well as in rat lumbar dorsal root and sympathetic ganglia. The 5-HT7 receptors have been implicated in depression, disorders related to circadian rhythms, pain and migraine. Thus, there is a great interest in developing potent and selective 5-HT7 receptor modulators.Areas covered in this review: This review article highlights the research advances published in the Patent Literature between January 2004 and December 2009, giving emphasis to the medicinal chemist's standpoint.What the reader will gain: Readers will rapidly gain an overview of the various 5-HT7 receptor modulators reported in the Patent Literature in the past 6 years. Furthermore, the readers will learn which structure type can interact with 5-HT7 receptor and also the differ...
Yingzi Xu - One of the best experts on this subject based on the ideXlab platform.
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small molecule bace1 inhibitors a Patent Literature review 2006 2011
Expert Opinion on Therapeutic Patents, 2012Co-Authors: Gary Probst, Yingzi XuAbstract:Introduction: Alzheimer's disease is a devastating neurodegenerative disorder for which no disease-modifying therapy exists. The amyloid hypothesis, which implicates Aβ as the toxin initiating a biological cascade leading to neurodegeneration, is the most prominent theory concerning the underlying cause of the disease. BACE1 is one of two aspartyl proteinases that generate Aβ, thus inhibition of BACE1 has the potential to ameliorate the progression of Alzheimer's disease by abating the production of Aβ.Areas covered: This review chronicles small-molecule BACE1 inhibitors as described in the Patent Literature between 2006 and 2011 and their potential use as disease-modifying treatments for Alzheimer's disease. Over the past half a dozen years, numerous BACE1 inhibitors have been published in the Patent applications, but often these contain a paltry amount of pertinent biological data (e.g. potency, selectivity, and efficacy). Fortunately, numerous relevant publications containing important data have appear...
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Small-molecule BACE1 inhibitors: a Patent Literature review (2006 – 2011)
Expert Opinion on Therapeutic Patents, 2012Co-Authors: Gary D. Probst, Yingzi XuAbstract:Introduction: Alzheimer's disease is a devastating neurodegenerative disorder for which no disease-modifying therapy exists. The amyloid hypothesis, which implicates Aβ as the toxin initiating a biological cascade leading to neurodegeneration, is the most prominent theory concerning the underlying cause of the disease. BACE1 is one of two aspartyl proteinases that generate Aβ, thus inhibition of BACE1 has the potential to ameliorate the progression of Alzheimer's disease by abating the production of Aβ.Areas covered: This review chronicles small-molecule BACE1 inhibitors as described in the Patent Literature between 2006 and 2011 and their potential use as disease-modifying treatments for Alzheimer's disease. Over the past half a dozen years, numerous BACE1 inhibitors have been published in the Patent applications, but often these contain a paltry amount of pertinent biological data (e.g. potency, selectivity, and efficacy). Fortunately, numerous relevant publications containing important data have appear...
Sushruta Koppula - One of the best experts on this subject based on the ideXlab platform.
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novel small molecule inhibitors of programmed cell death pd 1 and its ligand pd l1 in cancer immunotherapy a review update of Patent Literature
Recent Patents on Anti-cancer Drug Discovery, 2019Co-Authors: Spandana Rajendra Kopalli, Taebong Kang, Sushruta KoppulaAbstract:BACKGROUND: In the last few decades, cancer immunotherapy has been extensively researched, and novel checkpoint signaling mechanisms involving Programmed Death (PD)-1 and PDLigand 1 (PD-L1) receptors have been targeted. The PD-1/PD-L1 binding and interaction play a critical role in the development of malignancies. OBJECTIVE: The present review focuses on recent Patents on the pharmacological and biological cancerregulating properties of PD-1/PD-L1 inhibitors involved in immunotherapeutic cancer drug development. METHODS: Thorough Patent Literature search published during the last seven years, including the World Intellectual Property Organization (WIPO®), United States Patent Trademark Office (USPTO®), Espacenet®, and Google Patents, to identify PD-1/PD-L1-targeting small molecule immunomodulators. RESULTS: Several small molecule PD-1/PD-L1 inhibitors were Patented for regulation of tumor progression by academic and industry-associated investigators. Most of the claimed Patents have been validated and confined to in vitro and in vivo mouse models limiting their entry into clinical settings. Majority of the Patents are claimed by the researchers at Aurigene Ltd. (India) on novel peptidomimetic compounds. It is worth to be noted that macrocyclic compounds such as the peptides QP20, HD20, WQ20, SQ20, and CQ-22 from Bristol-Myers Squibb (BMS) Company, biaryl, and heterocyclic derivatives including 1,3-dihydroxy-phenyl compounds were efficient in regulating the PD-1/PD-L1 protein-protein binding and interaction compared to those of the approved monoclonal antibodies. CONCLUSION: PD-1/PD-L1 inhibitors show significant anti-cancer responses as stand-alone agents and in combination with other cancer therapies. More efficient experimental studies and clinical trials are necessary to evaluate the host-tumor cells' interactions. Understanding the cancer microenvironment, and identifying specific biomarkers and X-ray crystalline structures of PD-1/PD-L1 complexes, including molecular and genomic signature studies are essential to determine the feasibility of PD-1/PD-L1 inhibitors for development into drug-like cancer immunotherapeutics.