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News Article | May 29, 2017
Site: www.prnewswire.com

NEW YORK, May 29, 2017 /PRNewswire/ -- This report analyzes the worldwide markets for Contract Research Outsourcing in US$ Million by the following Service Segments: Drug Discovery, Preclinical Research, and Clinical Research. The report provides separate comprehensive analytics for the US, Canada, Japan, Europe, Asia-Pacific, and Rest of World. Annual estimates and forecasts are provided for the period 2015 through 2022. Also, a six-year historic analysis is provided for these markets. Read the full report: http://www.reportlinker.com/p04910444/Global-Contract-Research-Outsourcing-Services.html Market data and analytics are derived from primary and secondary research. Company profiles are primarily based on public domain information including company URLs. The report profiles 115 companies including many key and niche players such as - Albany Molecular Research, Inc. - Charles River Laboratories International, Inc. - Chiltern International Ltd. - ICON plc Read the full report: http://www.reportlinker.com/p04910444/Global-Contract-Research-Outsourcing-Services.html I. INTRODUCTION, METHODOLOGY & PRODUCT DEFINITIONS Study Reliability and Reporting Limitations Disclaimers Data Interpretation & Reporting Level Quantitative Techniques & Analytics Product Definitions and Scope of Study II. EXECUTIVE SUMMARY 1. INDUSTRY OVERVIEW Outsourcing of R&D Projects to Propel CROs Services Market Growth Drivers in a Nutshell Evolving Macro Trends Driving CRO Demand CROs to Significantly Drive Outsourcing Penetration Focus on Efficient, Quality Services to Drive Specialty CROs Market Rise in Investments to Boost Growth Key Therapeutic Areas of Clinical Trial Research Table 1: Global Clinical Trial Services Market by Therapeutic Area: 2016 (includes corresponding Graph/Chart) Primary Factors Influencing CRO Market Pharma and Biotech Companies to Increase Dependence on CROs Outlook Notable Regional Developments Future Model of CRO 2. COMPETITIVE SCENARIO CRO - A Highly Fragmented Market Table 2: Leading Players in the Global Contract Research Outsourcing Market (2016E): Percentage Breakdown of Revenues by Player (includes corresponding Graph/Chart) Table 3: Percentage Breakup of Life Sciences Revenues (2016) of Major Players by Service Type- Preclinical, Phase I, Phase IIA, Phase IIB, Phase III, Phase IV/ Post-Approval, Central Lab and Others Large CROs Seek the Inorganic Growth Route Global CRO Marketspace - A Review of the M&A Activity in the Recent Years Select M&A Activity in the Global CRO Market Noteworthy Contracts of Major CROs CROs Adept with New Technologies to See More Business in Future Streamlining Development of Novel Trial Designs CROs with End-to End Capabilities in Demand Key Opportunities for CROs Technological Superiority - A Definite Advantage Strategies and Tactical Programs for CROs Survival Strategies in Mature CRO Markets Exit from the Industry Expand Scale Capture Niche Segments Strategies to Tap Opportunities in Growing Markets Mobilize Funds Expand Other Services Upgrade Technological and Knowledge Base Form Sub-Contracts or Regional Alliances 3. GROWTH DRIVERS, MARKET TRENDS & ISSUES Increased Spend on R&D Outsourcing Table 4: Global Pharmaceutical R&D Spending (US$ Billion) for the Years 2010 through 2017 (includes corresponding Graph/Chart) Table 5: Percentage Breakdown of Total Number of Compounds in Pipeline by Phase for Pre-Clinical, Phase I, Phase II and Phase III: 2016E (includes corresponding Graph/Chart) Enhancing Site Selection and Patient Enrollment CROs Enter into Alliances to Improve Efficiencies Adoption of Digital Technologies Gains Pace Rising Late-Stage Services Demand and Budget Restraints Drive Market Growth Toxicology Services Gain Notable Attention Pharma Companies Enter into Licensing Agreements with Biotech Companies for New Drug Discovery - A Mutually Beneficial Strategy Pharmaceutical & Biopharmaceutical Trends to Support CRO Penetration Table 6: Global Biopharma % R&D Outsourcing (2014-2020) (includes corresponding Graph/Chart) Table 7: New FDA Drug Approvals (2010-2016): Breakdown of Number of Approvals by Type for New Molecular Entity (NME) and Biologic License Application (BLA) Approvals (includes corresponding Graph/Chart) Focus on Regulatory Oversight and Enhanced Transparency Bodes Well for CROs eClinical Solutions Gain Traction Other Noteworthy Market Trends CROs Monetize Data Service Differentiation - A Sustaining Strategy CROs Tie Up with Diagnostic Companies for Patients Research Networks Move to Cloud Application of Mobile Devices to Collect Real Time Data Gains Ground CROs Provide Exclusive Offers to Lure Big Pharma Challenges Faced by Contract Research Organizations On-shore versus Offshore CRO Business Cutthroat Competition among CROs Management of Clinical Investigation Cost Containment Safety Concerns on Clinical Trials Pipeline Blocks Surging Global Population Offers Increased Growth Opportunities Table 8: Top 25 Countries Worldwide in Terms of Population: 2015 & 2016 (In Million) (includes corresponding Graph/Chart) Aging Population Boosts Opportunities for CRO Table 9: Global Population Statistics for the 65+ Age Group (2015) (includes corresponding Graph/Chart) Table 10: Comparison of Aging Population by Country (1980, 2015 & 2050): Percentage Share of Population Aged Above-65 Years of the Overall Population for Select Countries (includes corresponding Graph/Chart) Increasing Healthcare Expenditure to Spur Demand for Generics Table 11: Healthcare Spending as a Percentage of GDP by Region (2016E) (includes corresponding Graph/Chart) 4. CONTRACT RESEARCH OUTSOURCING - AN INSIGHT Concept Contract Research Organizations (CRO) Contract Research Outsourcing Major CRO Services Ancillary CRO Services Advantages from CRO Drug Discovery Pre-Clinical Studies Clinical Research - Factors Encouraging CRO Services at Various Phases Phase I Phase II Phase III Phase IV 5. RECENT INDUSTRY ACTIVITY WuXi AppTec Takes Over HD Biosciences Laboratory Corporation of America Holdings to Acquire Pharmaceutical Product Development PRA Health Sciences and Takeda Pharmaceutical Inks New Partnership AMRI Enters into Alliance with Bruker Daltonics and HighRes Biosolutions Pharmaceutical Product Development Establishes Rare Disease and Pediatric Center of Excellence Pharmaceutical Product Development to Start Clinical Research Unit in Las Vegas Bracket Acquires CLINapps PAREXEL International to Acquire ExecuPharm Cinven to Takeover BioClinica ICON to Takeover Clinical Research Management Pharmaceutical Product Development Acquires Evidera Velocity Fund Partners Acquires Indipharm Bioclinica Snaps Up Compass Research Charles River Laboratories International Takes Over Agilux Laboratories Charles River Laboratories International Snaps Up Blue Stream Laboratories Charles River Laboratories International Acquires WIL Research Pharmaron Announces the Acquisition of Quotient Bioresearch Amulet Capital Partners Acquires SynteractHCR Holdings IMS Health Merges with Quintiles Almac Clinical Technologies Enters into Partnership with inVentiv Health CSSi LifeSciences Unveils Fully Integrated Medical Device CRO Lovelace Biomedical Commences Operations as Preclinical CRO PAREXEL International Inks Services Agreement with Pfizer BioDuro Commences Operations as a Contract Research and Manufacturing Firm Charles River Laboratories International Forms Partnership with BioMotiv Laboratory Corporation of America Acquires Covance Charles River Laboratories International Snaps Up Oncotest Chiltern Acquires Theorem Clinical Research Charles River Laboratories International Takes Over Celsis International Albany Molecular Research Unveils Integrated Drug Discovery Center 6. FOCUS ON SELECT GLOBAL PLAYERS Albany Molecular Research, Inc. (USA) Charles River Laboratories International, Inc. (USA) Chiltern International Ltd. (UK) ICON plc (Ireland) INC Research, LLC (USA) InVentiv Health, Inc. (USA) Jubilant Biosys Ltd. (India) Laboratory Corporation of America® Holdings (USA) PAREXEL International Corp. (USA) Pharmaceutical Product Development, LLC. (USA) Pharmaron (China) PRA Health Sciences, Inc. (USA) Quintiles IMS Holdings, Inc. (USA) Ricerca Biosciences LLC (USA) Sygnature Discovery Limited (UK) SynteractHCR (USA) WuXi AppTec (China) 7. GLOBAL MARKET PERSPECTIVE Table 12: World Recent Past, Current & Future Analysis for Contract Research Outsourcing by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 13: World Historic Review for Contract Research Outsourcing by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 14: World 14-Year Perspective for Contract Research Outsourcing by Geographic Region - Percentage Breakdown of Revenues for US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) Table 15: World Recent Past, Current & Future Analysis for Contract Research Outsourcing for Drug Discovery by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 16: World Historic Review for Contract Research Outsourcing for Drug Discovery by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 17: World 14-Year Perspective for Contract Research Outsourcing for Drug Discovery by Geographic Region - Percentage Breakdown of Revenues for US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) Table 18: World Recent Past, Current & Future Analysis for Contract Research Outsourcing for Preclinical Research by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 19: World Historic Review for Contract Research Outsourcing for Preclinical Research by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 20: World 14-Year Perspective for Contract Research Outsourcing for Preclinical Research by Geographic Region - Percentage Breakdown of Revenues for US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) Table 21: World Recent Past, Current & Future Analysis for Contract Research Outsourcing for Clinical Research by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 22: World Historic Review for Contract Research Outsourcing for Clinical Research by Geographic Region - US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 23: World 14-Year Perspective for Contract Research Outsourcing for Clinical Research by Geographic Region - Percentage Breakdown of Revenues for US, Canada, Japan, Europe, Asia-Pacific (excluding Japan) and Rest of World Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) III. MARKET 1. THE UNITED STATES A.Market Analysis Outlook Drug Developers Rely on CROs to Improve Trial Efficiency and Cost Savings Trial Services Witness Higher Demand Strong Demand for Data Management Services Focus on Innovation and Productivity CROs Focus on Adaptive Clinical Trials Risk-based Monitoring Catches Pace Strategic Corporate Developments Key Players B.Market Analytics Table 24: US Recent Past, Current & Future Analysis for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 25: US Historic Review for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 26: US 14-Year Perspective for Contract Research Outsourcing by Service Type - Percentage Breakdown of Revenues for Drug Discovery, Preclinical Research and Clinical Research Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) 2. CANADA Market Analysis Table 27: Canadian Recent Past, Current & Future Analysis for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 28: Canadian Historic Review for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 29: Canadian 14-Year Perspective for Contract Research Outsourcing by Service Type - Percentage Breakdown of Revenues for Drug Discovery, Preclinical Research and Clinical Research Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) 3. JAPAN A.Market Analysis Strategic Corporate Development B.Market Analytics Table 30: Japanese Recent Past, Current & Future Analysis for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 31: Japanese Historic Review for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 32: Japanese 14-Year Perspective for Contract Research Outsourcing by Service Type - Percentage Breakdown of Revenues for Drug Discovery, Preclinical Research and Clinical Research Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) 4. EUROPE A.Market Analysis Outlook Providers Expand Services in Downstream Drug Development Strategic corporate developments Key Players B.Market Analytics Table 33: European Recent Past, Current & Future Analysis for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 34: European Historic Review for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 35: European 14-Year Perspective for Contract Research Outsourcing by Service Type - Percentage Breakdown of Revenues for Drug Discovery, Preclinical Research and Clinical Research Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) 5. ASIA-PACIFIC A.Market Analysis Outlook Asia-Pacific to Push up Volume Share in CRO Market R&D Outsourcing in Life Sciences on Rise Focus on Select Regional Markets China Market with Strong Growth Potential India Australia Popular Destination for Early Phase Clinical Trials Cost Savings through Tax Incentives Supportive Regulatory Framework Government Focus on Reducing Cost and Time Superior Clinical Trial Quality Strategic Corporate Development Key Players B.Market Analytics Table 36: Asia-Pacific Recent Past, Current & Future Analysis for Contract Research Outsourcing by Geographic Region - China, India and Rest of Asia-Pacific Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 37: Asia-Pacific Historic Review for Contract Research Outsourcing by Geographic Region - China, India and Rest of Asia-Pacific Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 38: Asia-Pacific 14-Year Perspective for Contract Research Outsourcing by Geographic Region - Percentage Breakdown of Revenues for China, India and Rest of Asia-Pacific Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) Table 39: Asia-Pacific Recent Past, Current & Future Analysis for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 40: Asia-Pacific Historic Review for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 41: Asia-Pacific 14-Year Perspective for Contract Research Outsourcing by Service Type - Percentage Breakdown of Revenues for Drug Discovery, Preclinical Research and Clinical Research Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) 6. REST OF WORLD A.Market Analysis Outlook Providers with Specialized Research Techniques to Boost Latin American CRO Market B.Market Analytics Table 42: Rest of World Recent Past, Current & Future Analysis for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2015 through 2022 (includes corresponding Graph/Chart) Table 43: Rest of World Historic Review for Contract Research Outsourcing by Service Type - Drug Discovery, Preclinical Research and Clinical Research Markets Independently Analyzed with Annual Revenue Figures in US$ Million for Years 2009 through 2014 (includes corresponding Graph/Chart) Table 44: Rest of World 14-Year Perspective for Contract Research Outsourcing by Service Type - Percentage Breakdown of Revenues for Drug Discovery, Preclinical Research and Clinical Research Markets for Years 2009, 2017 & 2022 (includes corresponding Graph/Chart) IV. COMPETITIVE LANDSCAPE Total Companies Profiled: 115 (including Divisions/Subsidiaries - 120) The United States (47) Canada (5) Japan (1) Europe (27) - France (2) - Germany (6) - The United Kingdom (3) - Spain (1) - Rest of Europe (15) Asia-Pacific (Excluding Japan) (35) Latin America (4) Read the full report: http://www.reportlinker.com/p04910444/Global-Contract-Research-Outsourcing-Services.html About Reportlinker ReportLinker is an award-winning market research solution. Reportlinker finds and organizes the latest industry data so you get all the market research you need - instantly, in one place. http://www.reportlinker.com __________________________ Contact Clare: clare@reportlinker.com US: (339)-368-6001 Intl: +1 339-368-6001 To view the original version on PR Newswire, visit:http://www.prnewswire.com/news-releases/global-contract-research-outsourcing---services-300465052.html


Li X.,Anacor Pharmaceuticals Inc. | Zhang S.,Anacor Pharmaceuticals Inc. | Zhang Y.-K.,Anacor Pharmaceuticals Inc. | Liu Y.,Anacor Pharmaceuticals Inc. | And 20 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

We have synthesized and evaluated a new series of acyclic P4-benzoxaborole-based HCV NS3 protease inhibitors. Structure-activity relationships were investigated, leading to the identification of compounds 5g and 17 with low nanomolar potency in the enzymatic and cell-based replicon assay. The linker-truncated compound 5j was found to exhibit improved absorption and oral bioavailability in rats, suggesting that further reduction of molecular weight and polar surface area could result in improved drug-like properties of this novel series. © 2011 Elsevier Ltd. All rights reserved.


Li X.,Anacor Pharmaceuticals Inc. | Zhang Y.-K.,Anacor Pharmaceuticals Inc. | Liu Y.,Anacor Pharmaceuticals Inc. | Ding C.Z.,Anacor Pharmaceuticals Inc. | And 29 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

We have designed and synthesized a novel series of α-amino cyclic boronates and incorporated them successfully in several acyclic templates at the P1 position. These compounds are inhibitors of the HCV NS3 serine protease, and structural studies show that they inhibit the NS3 protease by trapping the Ser-139 hydroxyl group in the active site. Synthetic methodologies and SARs of this series of compounds are described. © 2010 Elsevier Ltd.


Zhang Y.-K.,Anacor Pharmaceuticals Inc. | Plattner J.J.,Anacor Pharmaceuticals Inc. | Easom E.E.,Anacor Pharmaceuticals Inc. | Zhou Y.,Anacor Pharmaceuticals Inc. | And 10 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

A novel series of isoxazoline benzoxaborole small molecules was designed and synthesized for a structure-activity relationship (SAR) investigation to assess the ectoparasiticide activity against ticks and fleas. The study identified an orally bioavailable molecule, (S)-3,3-dimethyl-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)benzo[c][1,2]oxaborol-1(3H)-ol (38, AN8030), which was long lasting in dogs (t1/2 = 22 days). Compound 38 demonstrated 97.6% therapeutic effectiveness within 24 h of treatment, with residual efficacy of 95.3% against American dog ticks (Dermacentor variabilis) on day 30% and 100% against cat fleas (Ctenocephalides felis) on day 32 after a single oral dose at 50 mg/kg in dogs. © 2015 Elsevier Ltd. All rights reserved.


Li X.,Anacor Pharmaceuticals Inc. | Zhang Y.-K.,Anacor Pharmaceuticals Inc. | Liu Y.,Anacor Pharmaceuticals Inc. | Ding C.Z.,Anacor Pharmaceuticals Inc. | And 27 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

A novel series of P2-P4 macrocyclic HCV NS3/4A protease inhibitors with α-amino cyclic boronates as warheads at the P1 site was designed and synthesized. When compared to their linear analogs, these macrocyclic inhibitors exhibited a remarkable improvement in cell-based replicon activities, with compounds 9a and 9e reaching sub-micromolar potency in replicon assay. The SAR around α-amino cyclic boronates clearly established the influence of ring size, chirality and of the substitution pattern. Furthermore, X-ray structure of the co-crystal of inhibitor 9a and NS3 protease revealed that Ser-139 in the enzyme active site traps boron in the warhead region of 9a, thus establishing its mode of action. © 2010 Elsevier Ltd. All rights reserved.


Li X.,Anacor Pharmaceuticals Inc. | Zhang Y.-K.,Anacor Pharmaceuticals Inc. | Liu Y.,Anacor Pharmaceuticals Inc. | Zhang S.,Anacor Pharmaceuticals Inc. | And 19 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

HCV NS3/4A serine protease is essential for the replication of the HCV virus and has been a clinically validated target. A series of HCV NS3/4A protease inhibitors containing a novel acylsulfamoyl benzoxaborole moiety at the P1′ region was synthesized and evaluated. The resulting P1-P3 and P2-P4 macrocyclic inhibitors exhibited sub-nanomolar potency in the enzymatic assay and low nanomolar activity in the cell-based replicon assay. The in vivo PK evaluations of selected compounds are also described. © 2010 Elsevier Ltd. All rights reserved.


Ding C.Z.,Anacor Pharmaceuticals Inc. | Zhang Y.-K.,Anacor Pharmaceuticals Inc. | Li X.,Anacor Pharmaceuticals Inc. | Liu Y.,Anacor Pharmaceuticals Inc. | And 17 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

We disclose here a series of P4-benzoxaborole-substituted macrocyclic HCV protease inhibitors. These inhibitors are potent against HCV NS3 protease, their anti-HCV replicon potencies are largely impacted by substitutions on benzoxaborole ring system and P2 groups. P2 2-thiazole-isoquinoline provides best replicon potency. The in vitro SAR studies and in vivo PK evaluations of selected compounds are described herein. © 2010 Elsevier Ltd. All rights reserved.


PubMed | HIGH-TECH, Eli Lilly and Company, Anacor Pharmaceuticals Inc. and BioDuro LLC
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2015

A novel series of isoxazoline benzoxaborole small molecules was designed and synthesized for a structure-activity relationship (SAR) investigation to assess the ectoparasiticide activity against ticks and fleas. The study identified an orally bioavailable molecule, (S)-3,3-dimethyl-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)benzo[c][1,2]oxaborol-1(3H)-ol (38, AN8030), which was long lasting in dogs (t1/2=22 days). Compound 38 demonstrated 97.6% therapeutic effectiveness within 24 h of treatment, with residual efficacy of 95.3% against American dog ticks (Dermacentor variabilis) on day 30% and 100% against cat fleas (Ctenocephalides felis) on day 32 after a single oral dose at 50 mg/kg in dogs.

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