ES2526902T3 - Procesos de producción de inhibidores de la girasa y topoisomerasa IV - Google Patents

Procesos de producción de inhibidores de la girasa y topoisomerasa IV Download PDF

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Publication number
ES2526902T3
ES2526902T3 ES12708416.8T ES12708416T ES2526902T3 ES 2526902 T3 ES2526902 T3 ES 2526902T3 ES 12708416 T ES12708416 T ES 12708416T ES 2526902 T3 ES2526902 T3 ES 2526902T3
Authority
ES
Spain
Prior art keywords
formula
gyrase
topoisomerase
inhibitors
production processes
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.)
Active
Application number
ES12708416.8T
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English (en)
Inventor
Dean Shannon
Tiansheng Wang
Simon Giroux
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
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Publication of ES2526902T3 publication Critical patent/ES2526902T3/es
Active legal-status Critical Current
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Classifications

    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

Un método para preparar un compuesto de fórmula (I)**Fórmula** o una sal farmacéuticamente aceptable de este, don de R es H o F; y cada uno de los componentes R3, R4 y R5 es independientemente un grupo hidroxilo protegido opcionalmente o un alquilo sustituido opcionalmente; que comprende proporcionar un compuesto fenilpirimidínico de fórmula (II)**Fórmula** donde R es H o F, y cada uno de los componentes R3, R4 y R5 es independientemente un grupo hidroxilo protegido opcionalmente o un alquilo sustituido opcionalmente; y hacer reaccionar el compuesto fenilpirimidínico de fórmula (II) con un derivado de urea de fórmula A o B:**Fórmula**

Description

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Claims (1)

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ES12708416.8T 2011-01-14 2012-01-13 Procesos de producción de inhibidores de la girasa y topoisomerasa IV Active ES2526902T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161432990P 2011-01-14 2011-01-14
US201161432990P 2011-01-14
PCT/US2012/021281 WO2012097274A1 (en) 2011-01-14 2012-01-13 Process of making gyrase and topoisomerase iv inhibitors

Publications (1)

Publication Number Publication Date
ES2526902T3 true ES2526902T3 (es) 2015-01-16

Family

ID=45815947

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12708416.8T Active ES2526902T3 (es) 2011-01-14 2012-01-13 Procesos de producción de inhibidores de la girasa y topoisomerasa IV

Country Status (19)

Country Link
US (2) US8471014B2 (es)
EP (1) EP2663556B1 (es)
JP (1) JP6006235B2 (es)
KR (1) KR101882172B1 (es)
CN (1) CN103384665B (es)
AR (1) AR084864A1 (es)
AU (1) AU2012205420B2 (es)
BR (1) BR112013017968B1 (es)
CA (1) CA2824519C (es)
ES (1) ES2526902T3 (es)
IL (1) IL227405B (es)
MX (1) MX355561B (es)
NZ (1) NZ612920A (es)
PT (1) PT2663556E (es)
RU (1) RU2619116C2 (es)
SG (1) SG191945A1 (es)
TW (1) TWI534143B (es)
WO (1) WO2012097274A1 (es)
ZA (1) ZA201305232B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012097273A1 (en) * 2011-01-14 2012-07-19 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
CN103384666A (zh) * 2011-01-14 2013-11-06 沃泰克斯药物股份有限公司 固体形式的促旋酶抑制剂（r）-1-乙基-3-[5-[2-（1-羟基-1-甲基-乙基）嘧啶-5-基]-7-（四氢呋喃-2-基）-1氢-苯并咪唑-2-基]脲
EP2663557B1 (en) * 2011-01-14 2015-05-27 Vertex Pharmaceuticals Incorporated Pyrimidine gyrase and topoisomerase iv inhibitors
MX355561B (es) 2011-01-14 2018-04-23 Spero Trinem Inc Proceso para hacer inhibidores de girasa y topoisomerasa iv.
EP2721026B1 (en) * 2011-06-20 2016-03-02 Vertex Pharmaceuticals Incorporated Phosphate esters of gyrase and topoisomerase inhibitors
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
CA2938459A1 (en) 2014-02-03 2015-08-06 Spero Gyrase, Inc. Antibacterial compounds

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DE2015676A1 (de) 1970-04-02 1971-10-21 Farbenfabriken Bayer Ag, 5090 Leverkusen Neue Imine der 2-Formyl-chinoxalindi-N-oxidcarbon-säure-(3) und deren Salze, Verfahren zu ihrer Herstellung und ihre Verwendung als antimikrobielle Mittel
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
CA2028530A1 (en) 1989-11-21 1991-05-22 Christian Hubschwerlen Substituted pyrimidobenzimidazole derivatives
DE19514313A1 (de) 1994-08-03 1996-02-08 Bayer Ag Benzoxazolyl- und Benzothiazolyloxazolidinone
HRP960159A2 (en) 1995-04-21 1997-08-31 Bayer Ag Benzocyclopentane oxazolidinones containing heteroatoms
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
TW538046B (en) 1998-01-08 2003-06-21 Hoechst Marion Roussel Inc Aromatic amides having antiobiotic activities and the preparation processes, intermediates and pharmaceutical composition thereof
AUPP873799A0 (en) 1999-02-17 1999-03-11 Fujisawa Pharmaceutical Co., Ltd. Pyridine compounds
GB9911594D0 (en) 1999-05-19 1999-07-21 Smithkline Beecham Plc Novel compounds
GB9912413D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
HUP0303494A3 (en) 2000-12-15 2009-08-28 Vertex Pharma Parmaceutical compositions containing bacterial gyrase inhibitors and uses thereof
EP1511482B1 (en) * 2002-06-13 2006-11-15 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
AR042956A1 (es) * 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
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
US8404852B2 (en) 2003-01-31 2013-03-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US8193352B2 (en) 2003-01-31 2012-06-05 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
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JP4528722B2 (ja) * 2003-03-07 2010-08-18 興和株式会社 ベンゾフラン誘導体
US8394803B2 (en) * 2005-11-07 2013-03-12 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
GB0612428D0 (en) 2006-06-22 2006-08-02 Prolysis Ltd Antibacterial agents
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EP2663557B1 (en) * 2011-01-14 2015-05-27 Vertex Pharmaceuticals Incorporated Pyrimidine gyrase and topoisomerase iv inhibitors
WO2012097273A1 (en) 2011-01-14 2012-07-19 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
MX355561B (es) 2011-01-14 2018-04-23 Spero Trinem Inc Proceso para hacer inhibidores de girasa y topoisomerasa iv.
CN103384666A (zh) * 2011-01-14 2013-11-06 沃泰克斯药物股份有限公司 固体形式的促旋酶抑制剂（r）-1-乙基-3-[5-[2-（1-羟基-1-甲基-乙基）嘧啶-5-基]-7-（四氢呋喃-2-基）-1氢-苯并咪唑-2-基]脲
EP2721026B1 (en) 2011-06-20 2016-03-02 Vertex Pharmaceuticals Incorporated Phosphate esters of gyrase and topoisomerase inhibitors
EP2828257B1 (en) 2012-03-22 2017-07-26 Biota Europe Ltd Antibacterial compounds
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

Also Published As

Publication number Publication date
JP6006235B2 (ja) 2016-10-12
WO2012097274A1 (en) 2012-07-19
MX2013008164A (es) 2013-08-27
TW201307332A (zh) 2013-02-16
US8912326B2 (en) 2014-12-16
KR20140037028A (ko) 2014-03-26
CN103384665B (zh) 2018-01-09
US8471014B2 (en) 2013-06-25
CA2824519A1 (en) 2012-07-19
US20120184742A1 (en) 2012-07-19
KR101882172B1 (ko) 2018-07-26
RU2619116C2 (ru) 2017-05-12
IL227405A0 (en) 2013-09-30
EP2663556A1 (en) 2013-11-20
TWI534143B (zh) 2016-05-21
CA2824519C (en) 2020-06-16
AU2012205420A1 (en) 2013-08-01
IL227405B (en) 2018-05-31
EP2663556B1 (en) 2014-10-15
BR112013017968A2 (pt) 2016-07-12
AR084864A1 (es) 2013-07-10
SG191945A1 (en) 2013-08-30
AU2012205420B2 (en) 2016-12-08
MX355561B (es) 2018-04-23
BR112013017968B1 (pt) 2021-03-16
CN103384665A (zh) 2013-11-06
NZ612920A (en) 2015-10-30
RU2013137751A (ru) 2015-02-20
US20130261305A1 (en) 2013-10-03
ZA201305232B (en) 2014-11-26
PT2663556E (pt) 2014-11-27
JP2014503558A (ja) 2014-02-13

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