KR101052433B1 - 자이라제 및/또는 토포이소머라제 ⅳ 억제제로서의 2-우레이도-6-헤테로아릴-3ｈ-벤조이미다졸-4-카복실산 유도체 및 이를 포함하는 세균 감염 치료용 약제학적 조성물 - Google Patents

자이라제 및/또는 토포이소머라제 ⅳ 억제제로서의 2-우레이도-6-헤테로아릴-3ｈ-벤조이미다졸-4-카복실산 유도체 및 이를 포함하는 세균 감염 치료용 약제학적 조성물 Download PDF

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KR101052433B1
KR101052433B1 KR1020047020292A KR20047020292A KR101052433B1 KR 101052433 B1 KR101052433 B1 KR 101052433B1 KR 1020047020292 A KR1020047020292 A KR 1020047020292A KR 20047020292 A KR20047020292 A KR 20047020292A KR 101052433 B1 KR101052433 B1 KR 101052433B1
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formula
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ring
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KR20050009748A (ko
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차립슨폴
데이닝어데이비드디
드럼죠셉
그릴롯안느-로르
랴오위성
올리버-샤퍼파트리시아
스타모스딘
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버텍스 파마슈티칼스 인코포레이티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/06—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Urology & Nephrology (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020047020292A 2002-06-13 2003-06-11 자이라제 및/또는 토포이소머라제 ⅳ 억제제로서의 2-우레이도-6-헤테로아릴-3ｈ-벤조이미다졸-4-카복실산 유도체 및 이를 포함하는 세균 감염 치료용 약제학적 조성물 Expired - Fee Related KR101052433B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US38866502P 2002-06-13 2002-06-13
US60/388,665 2002-06-13
US42907702P 2002-11-26 2002-11-26
US60/429,077 2002-11-26
PCT/US2003/018401 WO2003105846A1 (en) 2002-06-13 2003-06-11 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

Publications (2)

Publication Number Publication Date
KR20050009748A KR20050009748A (ko) 2005-01-25
KR101052433B1 true KR101052433B1 (ko) 2011-07-29

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KR1020047020292A Expired - Fee Related KR101052433B1 (ko) 2002-06-13 2003-06-11 자이라제 및/또는 토포이소머라제 ⅳ 억제제로서의 2-우레이도-6-헤테로아릴-3ｈ-벤조이미다졸-4-카복실산 유도체 및 이를 포함하는 세균 감염 치료용 약제학적 조성물

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US (2) US7727992B2 (https=)
EP (1) EP1511482B1 (https=)
JP (1) JP4489586B2 (https=)
KR (1) KR101052433B1 (https=)
CN (1) CN1674898A (https=)
AT (1) ATE345132T1 (https=)
AU (1) AU2003245442B2 (https=)
CA (1) CA2489128C (https=)
DE (1) DE60309701T2 (https=)
ES (1) ES2277088T3 (https=)
IL (1) IL165715A (https=)
MX (1) MXPA04012628A (https=)
NO (1) NO20050099L (https=)
PL (1) PL374191A1 (https=)
RU (1) RU2333208C2 (https=)
TW (1) TWI282335B (https=)
WO (1) WO2003105846A1 (https=)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100590859B1 (ko) * 1999-09-14 2006-06-19 삼성전자주식회사 교환기 시스템의 기능 시험방법
PL374191A1 (en) * 2002-06-13 2005-10-03 Vertex Pharmaceuticals Incorporated 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
US7618974B2 (en) 2003-01-31 2009-11-17 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AR042956A1 (es) * 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
US8404852B2 (en) 2003-01-31 2013-03-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7569591B2 (en) 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7582641B2 (en) 2003-01-31 2009-09-01 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US8193352B2 (en) 2003-01-31 2012-06-05 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US20060223849A1 (en) 2005-03-14 2006-10-05 Mjalli Adnan M Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors
JP2009514894A (ja) * 2005-11-07 2009-04-09 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 ジャイレース阻害剤としてのベンズイミダゾール誘導体
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200906412A (en) * 2007-06-12 2009-02-16 Astrazeneca Ab Piperidine compounds and uses thereof
SI2203439T1 (sl) 2007-09-14 2011-05-31 Ortho Mcneil Janssen Pharm 1',3'-disubstituirani 4-fenil-3,4,5,6-tetrahidro-2H-1'H-(1,4')bipiridinil-2'-oni
EP2229379A2 (en) * 2007-12-07 2010-09-22 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
EP2344470B1 (en) 2008-09-02 2013-11-06 Janssen Pharmaceuticals, Inc. 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
JP5690277B2 (ja) 2008-11-28 2015-03-25 ジャンセン ファーマシューティカルズ， インコーポレイテッド． 代謝型グルタミン酸受容体の調節因子としてのインドールおよびベンゾオキサジン誘導体
GB0821913D0 (en) 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
BRPI1010831A2 (pt) 2009-05-12 2016-04-05 Addex Pharmaceuticals Sa derivados de 1,2,4-triazolo[4,3-a]piridina e seu como moduladores alostéricos positivos de receptores de mglur2
CN102439008B (zh) 2009-05-12 2015-04-29 杨森制药有限公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其用于治疗或预防神经和精神病症的用途
RU2012146246A (ru) 2010-03-31 2014-05-10 Актелион Фармасьютиклз Лтд Антибактериальные производные изохинолин-3-илмочевины
WO2011151619A1 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile associated disease
ES2803556T3 (es) 2010-06-01 2021-01-27 Summit Oxford Ltd Compuestos para el tratamiento de enfermedades asociadas a clostridium difficile
WO2011151620A1 (en) 2010-06-01 2011-12-08 Summit Corporation 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
WO2011151618A2 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile-associated disease
US9271967B2 (en) 2010-11-08 2016-03-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
ES2536433T3 (es) 2010-11-08 2015-05-25 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
AU2011328203B2 (en) 2010-11-08 2015-03-19 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
US8476281B2 (en) 2011-01-14 2013-07-02 Vertex Pharmaceuticals Incorporated 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
KR101882172B1 (ko) 2011-01-14 2018-07-26 스페로 트리넴, 인코포레이티드 자이라제 및 토포이소머라제 ⅳ 억제제의 제조방법
BR112013017977A2 (pt) * 2011-01-14 2019-09-24 Vertex Pharma formas sólidas de inibidor de girase (r) 1-etil-3-[5-[2-{1-hidroxi-1-metil-etil}pirimidin-5-il]-7-(tetrai-drofuran-2-il)-1h-benzimidazol-2-il]ureia
RU2609259C2 (ru) 2011-01-14 2017-01-31 Сперо Тринем, Инк. Пиримидиновые ингибиторы гиразы и топоизомеразы iv
AR088729A1 (es) 2011-03-29 2014-07-02 Actelion Pharmaceuticals Ltd Derivados de 3-ureidoisoquinolin-8-ilo y una composicion farmaceutica
CN103702994B (zh) 2011-06-20 2016-03-23 沃泰克斯药物股份有限公司 旋转酶和拓扑异构酶抑制剂的磷酸酯
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
US9018216B2 (en) 2012-07-18 2015-04-28 Vertex Pharmaceuticals Incorporated Solid forms of (R)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1H-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof
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
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
MX386697B (es) 2014-01-21 2025-03-19 Janssen Pharmaceutica Nv Combinaciones que comprenden agonistas ortostericos o moduladores alostericos positivos del receptor glutamatergico metabotropico de subtipo 2 y su uso
ME03518B (me) 2014-01-21 2020-04-20 Janssen Pharmaceutica Nv Kombinacije koje obuhvataju pozitivne alosterične modulatore ili ortosterične agoniste metabotropnog glutamatergičnog receptora podtipa 2 i njihova primjena
US20170007615A1 (en) 2014-02-03 2017-01-12 Biota Europe Ltd Antibacterial Compounds
HK1232071A1 (zh) * 2014-02-12 2018-01-05 Albert Einstein College Of Medicine, Inc. 使用mtan抑制剂治疗h.pylori感染
WO2016127102A2 (en) 2015-02-06 2016-08-11 Ernesto Abel-Santos Inhibiting germination of clostridium perfringens spores to reduce necrotic enteritis
CA3057431A1 (en) 2017-03-24 2018-09-27 Taisho Pharmaceutical Co., Ltd. 2(1h)-quinolinone derivative
US20200345637A1 (en) * 2018-01-19 2020-11-05 Aiviva Biopharma, Inc. Suspension compositions of multi-target inhibitors
IL289453B2 (en) 2019-07-17 2026-03-01 Summit Oxford Ltd Process for preparing ridinilazole and its crystalline forms
WO2021126118A1 (en) * 2019-12-20 2021-06-24 Anadolu Üni̇versi̇tesi̇ Synthesis of 2-(substitutedphenyl)-5-(substitutedheteroaryl)- 1h-benzimidazole derivatives and investigation of their biological effects
GB202100471D0 (en) 2021-01-14 2021-03-03 Summit Oxford Ltd Preparation of antibacterial compounds
GB202100470D0 (en) 2021-01-14 2021-03-03 Summit Oxford Ltd Solid tablet dosage for of ridinilazole
WO2023039159A2 (en) 2021-09-09 2023-03-16 Abel Santos Ernesto Inhibitors of c. difficile spore germination
NL2033609B1 (en) * 2022-11-24 2024-05-30 Innes John Centre DNA Gyrase Inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0433648A1 (de) * 1989-11-21 1991-06-26 F. Hoffmann-La Roche Ag Substituierte Pyrimidobenzimidazolderivate

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8803429D0 (en) * 1988-02-15 1988-03-16 Fujisawa Pharmaceutical Co Imidazole compounds processes for preparation thereof & pharmaceutical composition comprising same
ATE188379T1 (de) * 1992-10-14 2000-01-15 Merck & Co Inc Fibrinogenrezeptor-antagonisten
US5527910A (en) * 1992-12-30 1996-06-18 Cheil Foods & Chemicals, Inc. Pyridone carboxylic acid compounds and their uses for treating infectious diseases caused by bacteria
DE4344074A1 (de) * 1993-12-23 1995-06-29 Hoechst Schering Agrevo Gmbh Bicyclische Heteroarylverbindungen, Verfahren zu deren Herstellung, diese enthaltende Mittel und deren Verwendung als Safener
DE19514313A1 (de) 1994-08-03 1996-02-08 Bayer Ag Benzoxazolyl- und Benzothiazolyloxazolidinone
US5643935A (en) * 1995-06-07 1997-07-01 The University Of North Carolina At Chapel Hill Method of combatting infectious diseases using dicationic bis-benzimidazoles
ES2124167B1 (es) * 1996-06-04 1999-09-16 Espanola Prod Quimicos Nuevos derivados del bencimidazol con actividad antihistaminica.
GB9911594D0 (en) 1999-05-19 1999-07-21 Smithkline Beecham Plc Novel compounds
DE60131015T2 (de) * 2000-12-15 2008-07-10 Vertex Pharmaceuticals Inc., Cambridge Bakterielle gyrase-hemmer und deren verwendung
PL374191A1 (en) * 2002-06-13 2005-10-03 Vertex Pharmaceuticals Incorporated 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
US7569591B2 (en) * 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7582641B2 (en) * 2003-01-31 2009-09-01 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7618974B2 (en) * 2003-01-31 2009-11-17 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AR042956A1 (es) * 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0433648A1 (de) * 1989-11-21 1991-06-26 F. Hoffmann-La Roche Ag Substituierte Pyrimidobenzimidazolderivate

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US20110104207A1 (en) 2011-05-05
AU2003245442B2 (en) 2009-02-05
WO2003105846A1 (en) 2003-12-24
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KR20050009748A (ko) 2005-01-25
CA2489128C (en) 2012-01-03
AU2003245442A1 (en) 2003-12-31
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ES2277088T3 (es) 2007-07-01
CN1674898A (zh) 2005-09-28
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IL165715A (en) 2009-12-24
NO20050099L (no) 2005-03-14
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US8426426B2 (en) 2013-04-23
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TW200404785A (en) 2004-04-01
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US7727992B2 (en) 2010-06-01
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