WO2002060879A3 - Bacterial gyrase inhibitors and uses thereof - Google Patents

Bacterial gyrase inhibitors and uses thereof Download PDF

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Publication number
WO2002060879A3
WO2002060879A3 PCT/US2001/048855 US0148855W WO02060879A3 WO 2002060879 A3 WO2002060879 A3 WO 2002060879A3 US 0148855 W US0148855 W US 0148855W WO 02060879 A3 WO02060879 A3 WO 02060879A3
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WO
WIPO (PCT)
Prior art keywords
relates
bacterial
present
gyrase inhibitors
bacterial gyrase
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.)
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PCT/US2001/048855
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French (fr)
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WO2002060879A2 (en
Inventor
Anne-Laure Grillot
Paul Charifson
Dean Stamos
Yusheng Liao
Michael Badia
Martin Trudeau
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Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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Publication date
Priority to BR0116216-0A priority Critical patent/BR0116216A/en
Priority to JP2002561029A priority patent/JP4516272B2/en
Priority to DK01994269T priority patent/DK1341769T3/en
Priority to APAP/P/2003/002824A priority patent/AP2003002824A0/en
Priority to HU0303494A priority patent/HUP0303494A3/en
Priority to KR1020037007970A priority patent/KR100944645B1/en
Priority to HK04104843.7A priority patent/HK1061851B/en
Priority to CA002433197A priority patent/CA2433197C/en
Priority to DE60131015T priority patent/DE60131015T2/en
Priority to EP01994269A priority patent/EP1341769B1/en
Priority to NZ526241A priority patent/NZ526241A/en
Priority to SI200130794T priority patent/SI1341769T1/en
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Priority to IL15603101A priority patent/IL156031A0/en
Priority to MXPA03005298A priority patent/MXPA03005298A/en
Publication of WO2002060879A2 publication Critical patent/WO2002060879A2/en
Publication of WO2002060879A3 publication Critical patent/WO2002060879A3/en
Priority to IL156031A priority patent/IL156031A/en
Priority to NO20032668A priority patent/NO327312B1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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Abstract

The present invention relates to compounds of the formula (I): or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
PCT/US2001/048855 2000-12-15 2001-12-12 Bacterial gyrase inhibitors and uses thereof Ceased WO2002060879A2 (en)

Priority Applications (16)

Application Number Priority Date Filing Date Title
NZ526241A NZ526241A (en) 2000-12-15 2001-12-12 Gyrase inhibitors and uses thereof
DK01994269T DK1341769T3 (en) 2000-12-15 2001-12-12 Bacterial gyrase inhibitors and applications thereof
APAP/P/2003/002824A AP2003002824A0 (en) 2000-12-15 2001-12-12 Gyrase inhibitors and uses thereof
HU0303494A HUP0303494A3 (en) 2000-12-15 2001-12-12 Parmaceutical compositions containing bacterial gyrase inhibitors and uses thereof
KR1020037007970A KR100944645B1 (en) 2000-12-15 2001-12-12 Zirase Inhibitors and Pharmaceutical Compositions Comprising the Same
HK04104843.7A HK1061851B (en) 2000-12-15 2001-12-12 Gyrase inhibitors and uses thereof
CA002433197A CA2433197C (en) 2000-12-15 2001-12-12 Gyrase inhibitors and uses thereof
DE60131015T DE60131015T2 (en) 2000-12-15 2001-12-12 Bacterial gyrase inhibitors and their use
EP01994269A EP1341769B1 (en) 2000-12-15 2001-12-12 Bacterial gyrase inhibitors and uses thereof
BR0116216-0A BR0116216A (en) 2000-12-15 2001-12-12 Gyrase inhibitors and their uses
JP2002561029A JP4516272B2 (en) 2000-12-15 2001-12-12 Bacterial gyrase inhibitors and uses thereof
SI200130794T SI1341769T1 (en) 2000-12-15 2001-12-12 Bacterial gyrase inhibitors and uses thereof
IL15603101A IL156031A0 (en) 2000-12-15 2001-12-12 Fused heterocyclic derivatives and pharmaceutical compositions containing the same
MXPA03005298A MXPA03005298A (en) 2000-12-15 2001-12-12 Gyrase inhibitors and uses thereof.
IL156031A IL156031A (en) 2000-12-15 2003-05-21 Fused imidazole and oxazole derivatives and pharmaceutical compositions containing the same as anti-bacterial agents
NO20032668A NO327312B1 (en) 2000-12-15 2003-06-12 Gyrase Inhibitors and Uses thereof

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US25609400P 2000-12-15 2000-12-15
US60/256,094 2000-12-15
US27529201P 2001-03-13 2001-03-13
US60/275,292 2001-03-13

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WO2002060879A3 true WO2002060879A3 (en) 2003-03-27

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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US9096590B2 (en) 2010-05-24 2015-08-04 Intellikine Llc Substituted benzoxazoles as PI3 kinase inhibitors
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
US9988373B2 (en) 2013-12-26 2018-06-05 Shionogi & Co., Ltd. Nitrogen-containing six-membered cyclic derivatives and pharmaceutical composition comprising the same

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04012628A (en) * 2002-06-13 2005-03-23 Patricia Olivershaffer 2-ureido-6-heteroaryl-3h-benzoimidazole-4-carboxylic acid derivatives and related compounds as gyrase and/or topoisomerase iv inhibitors for the treatment of bacterial infections.
AU2003266668A1 (en) * 2002-09-30 2004-04-23 Banyu Pharmaceutical Co., Ltd. 2-aminobenzimidazole derivative
US7582641B2 (en) * 2003-01-31 2009-09-01 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US8404852B2 (en) 2003-01-31 2013-03-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AR042956A1 (en) * 2003-01-31 2005-07-13 Vertex Pharma GIRASA INHIBITORS AND USES OF THE SAME
US7569591B2 (en) * 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US8193352B2 (en) * 2003-01-31 2012-06-05 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7618974B2 (en) * 2003-01-31 2009-11-17 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
FR2852957B1 (en) * 2003-03-31 2005-06-10 Sod Conseils Rech Applic NOVEL IMIDAZO-PYRIDINE DERIVATIVES AND THEIR USE AS A MEDICINAL PRODUCT
US6984652B2 (en) * 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
US20060029948A1 (en) * 2003-09-19 2006-02-09 Gary Lim Sealing cover and dye compatibility selection
US7417726B2 (en) * 2003-09-19 2008-08-26 Applied Biosystems Inc. Normalization of data using controls
US20060024690A1 (en) * 2003-09-19 2006-02-02 Kao H P Normalization of data using controls
US20050221357A1 (en) * 2003-09-19 2005-10-06 Mark Shannon Normalization of gene expression data
US20050255485A1 (en) * 2004-05-14 2005-11-17 Livak Kenneth J Detection of gene duplications
WO2005121132A1 (en) * 2004-06-11 2005-12-22 Shionogi & Co., Ltd. Fused heterocyclic compound having anti-hcv effect
MX2007004179A (en) 2004-10-07 2007-06-07 Warner Lambert Co Triazolopyridine derivatives as antibacterial agents.
WO2007037782A2 (en) * 2005-02-08 2007-04-05 The University Of North Carolina At Chapel Hill Method for treating prostate conditions
TW200804345A (en) * 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
US8394803B2 (en) 2005-11-07 2013-03-12 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
CA2642264A1 (en) * 2006-02-13 2007-08-30 Trustees Of Boston University Reca inhibitors with antibiotic activity, compositions and methods of use
PE20070978A1 (en) * 2006-02-14 2007-11-15 Novartis Ag HETEROCICLIC COMPOUNDS AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASES (PI3Ks)
US8481544B2 (en) 2006-06-22 2013-07-09 Biota Europe Limited Antibacterial compositions
AU2012200669B2 (en) * 2006-06-22 2012-11-01 Biota Europe Ltd Antibacterial compositions
GB0612428D0 (en) * 2006-06-22 2006-08-02 Prolysis Ltd Antibacterial agents
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008019292A2 (en) * 2006-08-04 2008-02-14 Trustees Of Boston University Compositions and methods for potentiating antibiotic activity
WO2008068470A1 (en) * 2006-12-04 2008-06-12 Astrazeneca Ab Antibacterial polycyclic urea compounds
WO2009001915A1 (en) * 2007-06-28 2008-12-31 Takeda Pharmaceutical Company Limited Substituted imidazole compound and use thereof
WO2009027732A1 (en) * 2007-08-24 2009-03-05 Astrazeneca Ab 5-6-bicyclic heteroaromatic compounds with antibacterial activity
AU2008335409A1 (en) * 2007-12-07 2009-06-18 Vertex Pharmaceuticals Incorporated Solid forms of 1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1H-benzo[d] imidazol-2-yl)urea
GB0724342D0 (en) 2007-12-13 2008-01-30 Prolysis Ltd Anitbacterial compositions
BRPI0913300A2 (en) * 2008-06-04 2018-05-22 Astrazeneca Ab compound, process for preparation and use thereof, method of treating bacterial infection in an animal, and pharmaceutical composition.
MX2010013310A (en) 2008-06-04 2011-03-01 Astrazeneca Ab Heterocyclic urea derivatives for the treatment of bacterial infections.
US20090325902A1 (en) * 2008-06-04 2009-12-31 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
GB0821913D0 (en) 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
TW201026695A (en) 2008-12-12 2010-07-16 Astrazeneca Ab Piperidine compounds and uses thereof-596
TW201026694A (en) 2008-12-12 2010-07-16 Astrazeneca Ab Compound 468
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NZ597140A (en) 2009-06-05 2014-01-31 Cephalon Inc Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
UY32856A (en) 2009-08-26 2011-03-31 Astrazeneca Ab UREA HETEROCYCLIC DERIVATIVES AND METHODS OF USE OF THE SAME
WO2011032050A2 (en) * 2009-09-11 2011-03-17 Trius Therapeutics, Inc. Gyrase inhibitors
EP2552893B1 (en) 2010-03-31 2014-10-29 Actelion Pharmaceuticals Ltd. Antibacterial isoquinolin-3-ylurea derivatives
WO2011151619A1 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile associated disease
WO2011151620A1 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile associated disease
WO2011151618A2 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile-associated disease
HRP20160397T1 (en) 2010-06-01 2016-08-12 Summit Therapeutics Plc Compounds for the treatment of clostridium difficile associated disease
WO2011151617A1 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile associated disease
US9181234B2 (en) 2010-10-08 2015-11-10 Biota Europe Ltd. Antibacterial compounds
PT2663556E (en) 2011-01-14 2014-11-27 Vertex Pharma Process of making gyrase and topoisomerase iv inhibitors
RU2625305C2 (en) * 2011-01-14 2017-07-13 Сперо Тринем, Инк. Solid forms of gyrase inhibitor (r)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl) pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1h-benzimidazol-2-yl] urea
JP6085829B2 (en) 2011-01-14 2017-03-01 スペロ トリネム， インコーポレイテッド Pyrimidine gyrase and topoisomerase IV inhibitors
EP2663558A1 (en) * 2011-01-14 2013-11-20 Vertex Pharmaceuticals Incorporated Solid forms of gyrase inhibitor (r)-1-ethyl-3-[5-[2-{1-hydroxy-1-methyl-ethyl}pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urea
AR088729A1 (en) 2011-03-29 2014-07-02 Actelion Pharmaceuticals Ltd DERIVATIVES OF 3-UREIDOISOQUINOLIN-8-ILO AND A PHARMACEUTICAL COMPOSITION
WO2012177707A1 (en) 2011-06-20 2012-12-27 Vertex Pharmaceuticals Incorporated Phosphate esters of gyrase and topoisomerase inhibitors
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KR101546743B1 (en) 2012-01-16 2015-08-24 한국과학기술원 Indole derivatives, Abl kinase inhibiting composition and pharmaceutical compositions for prevention and treatment of abnormal cell growth diseases comprising the same
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WO2014014845A1 (en) 2012-07-18 2014-01-23 Vertex Pharmaceuticals Incorporated Combination therapy comprising|1 -ethyl-3-[5-[2-{1 -hydroxy-1 -methyl-ethyl}pyrimidin-5-yl]-7-(tetra hydrofuran-2-|yl}-1 h-benzimidazol-2-yl]urea and derivatives thereof to treat mycobacterium|diseases
US9079935B2 (en) 2012-08-13 2015-07-14 The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Reducing risk of contracting Clostridium-difficile associated disease
EP2890691B1 (en) 2012-08-31 2018-04-25 Principia Biopharma Inc. Benzimidazole derivatives as itk inhibitors
EP3102203A2 (en) 2014-02-03 2016-12-14 Spero Gyrase, Inc. Antibacterial combinations comprising polymyxin
CN104876878B (en) * 2014-02-27 2018-04-27 中国科学院广州生物医药与健康研究院 - 2 alkyl substituted urea benzimidazoles compound of 5- aryl phenols and its application
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US12258342B2 (en) 2018-09-03 2025-03-25 Univerza V Ljubljani Class of DNA gyrase and/or topoisomerase IV inhibitors with activity against gram-positive and gram-negative bacteria
MX2022000598A (en) 2019-07-17 2022-03-04 Summit Oxford Ltd PREPARATION OF ANTIBACTERIAL COMPOUNDS.
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EP4263503A1 (en) 2020-12-17 2023-10-25 Univerza V Ljubljani New n-phenylpyrrolamide inhibitors of dna gyrase and topoisomerase iv with antibacterial activity
GB202100471D0 (en) 2021-01-14 2021-03-03 Summit Oxford Ltd Preparation of antibacterial compounds
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US12220421B2 (en) 2021-09-09 2025-02-11 The Boards Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Inhibitors of C. difficile spore germination
WO2024249488A2 (en) * 2023-05-30 2024-12-05 Beth Israel Deaconess Medical Center, Inc. Inhibitors of dyrk1a

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4174400A (en) * 1978-09-13 1979-11-13 Merck & Co., Inc. Anthelmintic benzimidazoles
US4512998A (en) * 1980-10-20 1985-04-23 Schering Corporation Anthelmintic benzimidazole carbamates
US5529998A (en) * 1994-08-03 1996-06-25 Bayer Aktiengesellschaft Benzoxazolyl- and benzothiazolyloxazolidinones
EP0738726A1 (en) * 1995-04-21 1996-10-23 Bayer Ag Heterobenzocyclopentane oxazolidinones having antibacterial activity
WO1999035155A1 (en) * 1998-01-08 1999-07-15 Hoechst Marion Roussel Novel aromatic amides, preparation method and application as medicines
WO2000049015A1 (en) * 1999-02-17 2000-08-24 Fujisawa Pharmaceutical Co., Ltd. Pyridine compounds and their pharmaceutical use
EP1055668A1 (en) * 1999-05-28 2000-11-29 Pfizer Inc. New 4-arylpiperidine derivatives for the treatment of pruritus
WO2000071522A1 (en) * 1999-05-19 2000-11-30 Smithkline Beecham Plc Benzimidazole derivatives and their use as methionyl t-rna synthetase inhibitors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4338315A (en) * 1979-11-14 1982-07-06 Eli Lilly And Company Antiviral method employing thiazinyl benzimidazole derivatives
US4401817A (en) * 1981-04-20 1983-08-30 Eli Lilly And Company Carbonyl-substituted 1-sulfonylbenzimidazoles
GB8803429D0 (en) * 1988-02-15 1988-03-16 Fujisawa Pharmaceutical Co Imidazole compounds processes for preparation thereof & pharmaceutical composition comprising same
FR2643903A1 (en) * 1989-03-03 1990-09-07 Union Pharma Scient Appl NOVEL BENZIMIDAZOLE DERIVATIVES, PROCESSES FOR PREPARING SAME, SYNTHESIS INTERMEDIATES, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, IN PARTICULAR FOR THE TREATMENT OF CARDIOVASCULAR DISEASES, AND DUODENIAL ULCERS
US5296486A (en) * 1991-09-24 1994-03-22 Boehringer Ingelheim Pharmaceuticals, Inc. Leukotriene biosynthesis inhibitors
DE4317657C1 (en) * 1993-05-27 1994-07-14 Voith Gmbh J M Coating device for coating running webs
EP0759774B1 (en) 1993-09-22 2002-06-12 XOMA Technology Ltd. Method of treating gram-negative bacterial infection by administration of bactericidal/permeability-increasing (bpi) protein product and antibiotic
WO1995019180A1 (en) 1994-01-14 1995-07-20 Xoma Corporation Anti-gram-positive bacterial methods and materials

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4174400A (en) * 1978-09-13 1979-11-13 Merck & Co., Inc. Anthelmintic benzimidazoles
US4512998A (en) * 1980-10-20 1985-04-23 Schering Corporation Anthelmintic benzimidazole carbamates
US5529998A (en) * 1994-08-03 1996-06-25 Bayer Aktiengesellschaft Benzoxazolyl- and benzothiazolyloxazolidinones
EP0738726A1 (en) * 1995-04-21 1996-10-23 Bayer Ag Heterobenzocyclopentane oxazolidinones having antibacterial activity
WO1999035155A1 (en) * 1998-01-08 1999-07-15 Hoechst Marion Roussel Novel aromatic amides, preparation method and application as medicines
WO2000049015A1 (en) * 1999-02-17 2000-08-24 Fujisawa Pharmaceutical Co., Ltd. Pyridine compounds and their pharmaceutical use
WO2000071522A1 (en) * 1999-05-19 2000-11-30 Smithkline Beecham Plc Benzimidazole derivatives and their use as methionyl t-rna synthetase inhibitors
EP1055668A1 (en) * 1999-05-28 2000-11-29 Pfizer Inc. New 4-arylpiperidine derivatives for the treatment of pruritus

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
KUS, CANAN ET AL: "Synthesis and antimicrobial activities of 5-fluoro-1,2,6- trisubstituted benzimidazole carboxamide and acetamide derivatives", ARCHIV DER PHARMAZIE (WEINHEIM, GERMANY) (2001), 334(11), 361-365, XP001113052 *
M.H. BEERS AND R. BERKOW: "The Merck Manual of Diagnosis and Therapy - Seventeenth Edition", 1999, MERCK RESEARCH LABORATORIES, WHITEHOUSE STATION, N.J., XP002216324 *
NICOLAUS B J R: "Symbiotic Approach to Drug Design", DECISION MAKING IN DRUG RESEARCH, XX, XX, 1983, pages 173 - 186, XP002197412 *
SINGH, SUDHIR K. ET AL: "Antiparasitic agents. Part 13. Synthesis of 4-aryl-2-substituted aminothiazoles as potential anthelmintics", INDIAN J. CHEM., SECT. B (1989), 28B(9), 786-9, XP001031866 *

Cited By (6)

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US9085560B2 (en) 2009-08-17 2015-07-21 Intellikine, Inc. Heterocyclic compounds and uses thereof
US9096590B2 (en) 2010-05-24 2015-08-04 Intellikine Llc Substituted benzoxazoles as PI3 kinase inhibitors
US9359352B2 (en) 2010-05-24 2016-06-07 Intellikine Llc Substituted benzimidazoles as PI3 kinase inhibitors
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
US9988373B2 (en) 2013-12-26 2018-06-05 Shionogi & Co., Ltd. Nitrogen-containing six-membered cyclic derivatives and pharmaceutical composition comprising the same

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HK1061851A1 (en) 2004-10-08
AU2006201397A1 (en) 2006-04-27
DE60131015D1 (en) 2007-11-29
JP2009102449A (en) 2009-05-14
EP1341769A2 (en) 2003-09-10
USRE40245E1 (en) 2008-04-15
IL156031A (en) 2011-11-30
US7414046B2 (en) 2008-08-19
CO7250441A2 (en) 2015-04-30
CY1107854T1 (en) 2013-06-19
EP1557410A3 (en) 2006-04-26
CN1266138C (en) 2006-07-26
SI1341769T1 (en) 2008-02-29
HUP0303494A3 (en) 2009-08-28
JP5196660B2 (en) 2013-05-15
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KR20030061855A (en) 2003-07-22
NO20032668D0 (en) 2003-06-12
NZ526241A (en) 2007-01-26
US20040043989A1 (en) 2004-03-04
PT1341769E (en) 2007-12-31
MXPA03005298A (en) 2003-10-06
DK1341769T3 (en) 2008-01-28
CA2433197C (en) 2009-11-24
PL362691A1 (en) 2004-11-02
BR0116216A (en) 2004-08-17
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US20030119868A1 (en) 2003-06-26
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US6632809B2 (en) 2003-10-14
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