US20100120855A1 - Macrocylic inhibitors of hepatitis c virus - Google Patents

Macrocylic inhibitors of hepatitis c virus Download PDF

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Publication number
US20100120855A1
US20100120855A1 US11/995,941 US99594106A US2010120855A1 US 20100120855 A1 US20100120855 A1 US 20100120855A1 US 99594106 A US99594106 A US 99594106A US 2010120855 A1 US2010120855 A1 US 2010120855A1
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US
United States
Prior art keywords
formula
alkyl
compounds
compound
het
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
US11/995,941
Other languages
English (en)
Inventor
Kenneth Alan Simmen
Herman Augustinus
Pierre Jean-Maria Bernard Raboisson
Abdellah Tahri
Karl Magnus Nilsson
Bengt Bertil Samuelsson
Åsa Annica Kristina Rosenquist
Dmitry Antonov
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen R&D Ireland ULC
Medivir AB
Original Assignee
Tibotec Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37028035&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=US20100120855(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Tibotec Pharmaceuticals Ltd filed Critical Tibotec Pharmaceuticals Ltd
Publication of US20100120855A1 publication Critical patent/US20100120855A1/en
Priority to US13/109,395 priority Critical patent/US8754105B2/en
Assigned to MEDIVIR AB reassignment MEDIVIR AB ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: ANTONOV, DMITRY, NILSSON, KARL MAGNUS, ROSENQUIST, ASA ANNICA KRISTINA, SAMUELSSON, BENGT BERTIL
Assigned to TIBOTEC BVBA reassignment TIBOTEC BVBA ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: DE KOCK, HERMAN AUGUSTINUS, RABOISSON, PIERRE JEAN-MARIE BERNARD, SIMMEN, KENNETH ALAN, TAHRI, ABDELLAH
Assigned to TIBOTEC PHARMACEUTICALS LTD. reassignment TIBOTEC PHARMACEUTICALS LTD. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: TIBOTEC BVBA
Assigned to JANSSEN R&D IRELAND reassignment JANSSEN R&D IRELAND CHANGE OF NAME (SEE DOCUMENT FOR DETAILS). Assignors: TIBOTEC PHARMACEUTICALS
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
US11/995,941 2005-07-29 2006-07-28 Macrocylic inhibitors of hepatitis c virus Abandoned US20100120855A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US13/109,395 US8754105B2 (en) 2005-07-29 2011-05-17 Macrocyclic inhibitors of hepatitis C virus

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP05107068 2005-07-29
EP05107068.8 2005-07-29
EP05107414.4 2005-08-11
EP05107414 2005-08-11
PCT/EP2006/064814 WO2007014920A1 (en) 2005-07-29 2006-07-28 Macrocyclic inhibitors of hepatitis c virus

Publications (1)

Publication Number Publication Date
US20100120855A1 true US20100120855A1 (en) 2010-05-13

Family

ID=37028035

Family Applications (2)

Application Number Title Priority Date Filing Date
US11/995,941 Abandoned US20100120855A1 (en) 2005-07-29 2006-07-28 Macrocylic inhibitors of hepatitis c virus
US13/109,395 Expired - Fee Related US8754105B2 (en) 2005-07-29 2011-05-17 Macrocyclic inhibitors of hepatitis C virus

Family Applications After (1)

Application Number Title Priority Date Filing Date
US13/109,395 Expired - Fee Related US8754105B2 (en) 2005-07-29 2011-05-17 Macrocyclic inhibitors of hepatitis C virus

Country Status (12)

Country Link
US (2) US20100120855A1 (ja)
EP (1) EP1912996B1 (ja)
JP (1) JP5426164B2 (ja)
CN (1) CN101273042B (ja)
AR (1) AR055105A1 (ja)
BR (1) BRPI0614621A2 (ja)
DK (1) DK1912996T3 (ja)
ES (1) ES2389964T3 (ja)
MY (1) MY144895A (ja)
RU (1) RU2441870C2 (ja)
TW (1) TWI383980B (ja)
WO (1) WO2007014920A1 (ja)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8349869B2 (en) 2005-07-29 2013-01-08 Tibotec Pharmaceuticals Ltd. Macrocylic inhibitors of hepatitis C virus
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
US8841275B2 (en) 2010-11-30 2014-09-23 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections

Families Citing this family (59)

* Cited by examiner, † Cited by third party
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MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
AR048401A1 (es) 2004-01-30 2006-04-26 Medivir Ab Inhibidores de la serina-proteasa ns3 del vhc
MX2008001402A (es) * 2005-07-29 2008-04-04 Tibotec Pharm Ltd Inhibidores macrociclicos del virus de la hepatitis c.
TW200745061A (en) * 2005-07-29 2007-12-16 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis C virus
PE20070210A1 (es) * 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
TWI375670B (en) * 2005-07-29 2012-11-01 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis c virus
PE20070343A1 (es) * 2005-07-29 2007-05-12 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
ATE496042T1 (de) * 2005-07-29 2011-02-15 Tibotec Pharm Ltd Makrocyclische inhibitoren des hepatitis-c-virus
US7741281B2 (en) 2005-11-03 2010-06-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2008008776A2 (en) 2006-07-11 2008-01-17 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2008019289A2 (en) 2006-08-04 2008-02-14 Enanta Pharmaceuticals, Inc. Tetrazolyl macrocyclic hepatitis c serine protease inhibitors
US8343477B2 (en) 2006-11-01 2013-01-01 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7763584B2 (en) 2006-11-16 2010-07-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8003604B2 (en) 2006-11-16 2011-08-23 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7888464B2 (en) 2006-11-16 2011-02-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
US8383583B2 (en) 2007-10-26 2013-02-26 Enanta Pharmaceuticals, Inc. Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors
US8426360B2 (en) * 2007-11-13 2013-04-23 Enanta Pharmaceuticals, Inc. Carbocyclic oxime hepatitis C virus serine protease inhibitors
WO2009064955A1 (en) 2007-11-14 2009-05-22 Enanta Pharmaceuticals, Inc. Macrocyclic tetrazolyl hepatitis c serine protease inhibitors
WO2009070692A1 (en) 2007-11-29 2009-06-04 Enanta Pharmaceuticals, Inc. C5-substituted, proline-derived, macrocyclic hepatitis c serine protease inhibitors
WO2009079353A1 (en) 2007-12-14 2009-06-25 Enanta Pharmaceuticals, Inc. Triazole-containing macrocyclic hcv serine protease inhibitors
US8283309B2 (en) 2007-12-20 2012-10-09 Enanta Pharmaceuticals, Inc. Bridged carbocyclic oxime hepatitis C virus serine protease inhibitors
US8202996B2 (en) 2007-12-21 2012-06-19 Bristol-Myers Squibb Company Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide
CN102015652A (zh) 2008-03-20 2011-04-13 益安药业 作为丙型肝炎病毒抑制剂的氟化大环化合物
US8163921B2 (en) 2008-04-16 2012-04-24 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
JP5529120B2 (ja) 2008-05-29 2014-06-25 ブリストル−マイヤーズ スクイブ カンパニー C型肝炎ウイルス阻害剤
US7964560B2 (en) 2008-05-29 2011-06-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
US8207341B2 (en) 2008-09-04 2012-06-26 Bristol-Myers Squibb Company Process or synthesizing substituted isoquinolines
US8563505B2 (en) 2008-09-29 2013-10-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8044087B2 (en) 2008-09-29 2011-10-25 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8283310B2 (en) 2008-12-15 2012-10-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
JP5793084B2 (ja) 2008-12-23 2015-10-14 ギリアド ファーマセット エルエルシー プリンヌクレオシドの合成
CA2748057C (en) 2008-12-23 2018-07-03 Pharmasset, Inc. Nucleoside phosphoramidates
BRPI0922508A8 (pt) 2008-12-23 2016-01-19 Pharmasset Inc Análogos de nucleosídeo
CN104856991A (zh) 2009-02-27 2015-08-26 西佳技术公司 用于治疗和预防登革热病毒感染的噻吩并吡啶衍生物
US8377962B2 (en) 2009-04-08 2013-02-19 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI598358B (zh) 2009-05-20 2017-09-11 基利法瑪席特有限責任公司 核苷磷醯胺
AR077712A1 (es) 2009-08-05 2011-09-14 Idenix Pharmaceuticals Inc Inhibidores de serina proteasa macrociclica
PE20130198A1 (es) * 2010-03-10 2013-03-24 Abbvie Bahamas Ltd Composiciones solidas
JP5872539B2 (ja) 2010-03-31 2016-03-01 ギリアド ファーマセット エルエルシー プリンヌクレオシドホスホルアミダート
CN102858790A (zh) 2010-03-31 2013-01-02 吉利德制药有限责任公司 核苷氨基磷酸酯
US8759527B2 (en) 2010-08-25 2014-06-24 Bayer Cropscience Ag Heteroarylpiperidine and -piperazine derivatives as fungicides
WO2012109398A1 (en) 2011-02-10 2012-08-16 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating hcv infections
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8691757B2 (en) 2011-06-15 2014-04-08 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2012171332A1 (zh) 2011-06-16 2012-12-20 爱博新药研发(上海)有限公司 抑制丙型肝炎病毒的大环状杂环化合物及其制备和应用
SG10201602044WA (en) 2011-09-16 2016-04-28 Gilead Pharmassett Llc Methods For Treating HCV
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
MX360452B (es) 2012-10-19 2018-11-01 Bristol Myers Squibb Co Inhibidores del virus de la hepatitis c.
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US9598433B2 (en) 2012-11-02 2017-03-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014071007A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2014070974A1 (en) 2012-11-05 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
CA2852867C (en) 2013-01-31 2016-12-06 Gilead Pharmasset Llc Combination formulation of two antiviral compounds
WO2014137869A1 (en) 2013-03-07 2014-09-12 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
MX2016002185A (es) 2013-08-27 2016-06-06 Gilead Pharmasset Llc Formulacion combinada de dos compuestos antivirales.

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5484801A (en) * 1994-01-28 1996-01-16 Abbott Laboratories Pharmaceutical composition for inhibiting HIV protease
US5807876A (en) * 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US5948436A (en) * 1993-09-13 1999-09-07 Abbott Laboratories Pharmaceutical composition
US6037157A (en) * 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US6054472A (en) * 1996-04-23 2000-04-25 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
US6498178B2 (en) * 1999-03-19 2002-12-24 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US20050143316A1 (en) * 2003-11-20 2005-06-30 Yong Tu Hepatitis C virus inhibitors
US7671032B2 (en) * 2004-01-30 2010-03-02 Medivir Ab HCV NS-3 serine protease inhibitors

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US5559158A (en) 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
CN1116288C (zh) 1996-04-23 2003-07-30 沃泰克斯药物股份有限公司 用作肌苷-5'-一磷酸脱氢酶抑制剂的脲衍生物
JP4080541B2 (ja) 1996-10-18 2008-04-23 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
DE69816280T2 (de) 1997-03-14 2004-05-27 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren des impdh-enzyms
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US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
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UA74546C2 (en) * 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
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Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5948436A (en) * 1993-09-13 1999-09-07 Abbott Laboratories Pharmaceutical composition
US5484801A (en) * 1994-01-28 1996-01-16 Abbott Laboratories Pharmaceutical composition for inhibiting HIV protease
US6037157A (en) * 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US5807876A (en) * 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US6054472A (en) * 1996-04-23 2000-04-25 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
US6344465B1 (en) * 1996-04-23 2002-02-05 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
US6498178B2 (en) * 1999-03-19 2002-12-24 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US20050143316A1 (en) * 2003-11-20 2005-06-30 Yong Tu Hepatitis C virus inhibitors
US7671032B2 (en) * 2004-01-30 2010-03-02 Medivir Ab HCV NS-3 serine protease inhibitors

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8349869B2 (en) 2005-07-29 2013-01-08 Tibotec Pharmaceuticals Ltd. Macrocylic inhibitors of hepatitis C virus
US8741926B2 (en) 2005-07-29 2014-06-03 Janssen R&D Ireland Macrocyclic inhibitors of hepatitis C virus
US8754106B2 (en) 2005-07-29 2014-06-17 Janssen R&D Ireland Macrocyclic inhibitors of hepatitis C virus
US9040562B2 (en) 2005-07-29 2015-05-26 Janssen R&D Ireland Macrocyclic inhibitors of hepatitis C virus
US9353103B2 (en) 2005-07-29 2016-05-31 Janssen Sciences Ireland Uc Macrocyclic inhibitors of hepatitis C virus
US9623022B2 (en) 2005-07-29 2017-04-18 Janssen Sciences Ireland Uc Macrocyclic inhibitors of hepatitis C virus
US9856265B2 (en) 2005-07-29 2018-01-02 Janssen Sciences Ireland Uc Macrocyclic inhibitors of hepatitis C virus
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
US8841275B2 (en) 2010-11-30 2014-09-23 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections
US9394331B2 (en) 2010-11-30 2016-07-19 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections

Also Published As

Publication number Publication date
EP1912996A1 (en) 2008-04-23
US8754105B2 (en) 2014-06-17
AR055105A1 (es) 2007-08-08
DK1912996T3 (da) 2012-09-17
TW200800945A (en) 2008-01-01
RU2008107738A (ru) 2009-09-10
CN101273042A (zh) 2008-09-24
MY144895A (en) 2011-11-30
JP2009502883A (ja) 2009-01-29
ES2389964T3 (es) 2012-11-05
US20110237621A1 (en) 2011-09-29
CN101273042B (zh) 2013-11-06
TWI383980B (zh) 2013-02-01
JP5426164B2 (ja) 2014-02-26
BRPI0614621A2 (pt) 2011-04-12
EP1912996B1 (en) 2012-06-20
RU2441870C2 (ru) 2012-02-10
WO2007014920A1 (en) 2007-02-08

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Legal Events

Date Code Title Description
STCB Information on status: application discontinuation

Free format text: ABANDONED -- FAILURE TO RESPOND TO AN OFFICE ACTION

AS Assignment

Owner name: JANSSEN R&D IRELAND, IRELAND

Free format text: CHANGE OF NAME;ASSIGNOR:TIBOTEC PHARMACEUTICALS;REEL/FRAME:032092/0094

Effective date: 20120106

Owner name: TIBOTEC BVBA, BELGIUM

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:SIMMEN, KENNETH ALAN;DE KOCK, HERMAN AUGUSTINUS;RABOISSON, PIERRE JEAN-MARIE BERNARD;AND OTHERS;REEL/FRAME:032091/0483

Effective date: 20060904

Owner name: TIBOTEC PHARMACEUTICALS LTD., IRELAND

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNOR:TIBOTEC BVBA;REEL/FRAME:032091/0917

Effective date: 20080110

Owner name: MEDIVIR AB, SWEDEN

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:NILSSON, KARL MAGNUS;SAMUELSSON, BENGT BERTIL;ROSENQUIST, ASA ANNICA KRISTINA;AND OTHERS;REEL/FRAME:032091/0098

Effective date: 20060904