BR112013017968A2 - processo para fazer inibidores de girase e de topoisomerase - Google Patents

processo para fazer inibidores de girase e de topoisomerase

Info

Publication number
BR112013017968A2
BR112013017968A2 BR112013017968A BR112013017968A BR112013017968A2 BR 112013017968 A2 BR112013017968 A2 BR 112013017968A2 BR 112013017968 A BR112013017968 A BR 112013017968A BR 112013017968 A BR112013017968 A BR 112013017968A BR 112013017968 A2 BR112013017968 A2 BR 112013017968A2
Authority
BR
Brazil
Prior art keywords
gyrase
compounds
making
topoisomerase inhibitors
formula
Prior art date
Application number
BR112013017968A
Other languages
English (en)
Other versions
BR112013017968B1 (pt
Inventor
Dean Shannon
Simon Giroux
Tiansheng Wang
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Publication of BR112013017968A2 publication Critical patent/BR112013017968A2/pt
Publication of BR112013017968B1 publication Critical patent/BR112013017968B1/pt

Links

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

processo para fazer inibidores de girase e de topoisomerase a presente aplicação refere-se aos compostos, intermediários e métodos para a preparação de compostos de fórmula (i) ou um dos sais farmaceuticamente aceitáveis dos mesmos, em que r é h ou f, e cada um de r3, r4 e r5 são como definidos na presente invenção. os compostos de fórmula (i) e composições farmacêuticas que compreendem os referidos compostos e sais inibem a girase bacteriana e/ou topo iv e são úteis no tratamento de infecções bacterianas.
BR112013017968-6A 2011-01-14 2012-01-13 processo para fazer inibidores de girase e de topoisomerase e compostos intermediários BR112013017968B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161432990P 2011-01-14 2011-01-14
US61/432,990 2011-01-14
PCT/US2012/021281 WO2012097274A1 (en) 2011-01-14 2012-01-13 Process of making gyrase and topoisomerase iv inhibitors

Publications (2)

Publication Number Publication Date
BR112013017968A2 true BR112013017968A2 (pt) 2016-07-12
BR112013017968B1 BR112013017968B1 (pt) 2021-03-16

Family

ID=45815947

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013017968-6A BR112013017968B1 (pt) 2011-01-14 2012-01-13 processo para fazer inibidores de girase e de topoisomerase e compostos intermediários

Country Status (19)

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

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8481551B2 (en) * 2011-01-14 2013-07-09 Vertex Pharmaceuticals Incorporated Gyrase and topoisomerase IV inhibitors
AU2012205416B2 (en) * 2011-01-14 2017-02-02 Spero Therapeutics, Inc. 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
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
PT2663556E (pt) 2011-01-14 2014-11-27 Vertex Pharma Processo de fabrico de inibidores de girase e topoisomerase iv
JP5977344B2 (ja) * 2011-06-20 2016-08-24 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ジャイレースおよびトポイソメラーゼ阻害剤のリン酸エステル
AR093226A1 (es) * 2012-07-18 2015-05-27 Vertex Pharma Formas solidas de dihidrogeno fosfato de (r)-2-(5-(2-(3-etilureido)-6-fluoro-7-(tetrahidrofuran-2-il)-1h-benzo[d]imidazol-5-il)pirimidin-2-il)propan-2-ilo y sus sales
US9572809B2 (en) 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases
SG11201606332PA (en) 2014-02-03 2016-09-29 Spero Gyrase Inc Antibacterial combinations comprising polymyxin

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE375983T1 (de) * 2000-12-15 2007-11-15 Vertex Pharma Bakterielle gyrase-hemmer und deren verwendung
ES2277088T3 (es) * 2002-06-13 2007-07-01 Vertex Pharmaceuticals Incorporated Derivados del acido 2-ureido-6-heteroaril-3h-benzoimidazol-4-carboxilico y compuestos relacionados como inhibidores de girasa y/o topoisomerasa iv para el tratamiento de infecciones bacterianas.
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
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
US7569591B2 (en) 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
MXPA05009500A (es) * 2003-03-07 2005-10-18 Kowa Co Derivado de benzofurano.
EP1948635A1 (en) * 2005-11-07 2008-07-30 Vertex Pharmaceuticals Incorporated Benzimidazole derivatives as gyrase inhibitors
US8481544B2 (en) 2006-06-22 2013-07-09 Biota Europe Limited Antibacterial compositions
GB0724349D0 (en) 2007-12-13 2008-01-30 Prolysis Ltd Antibacterial agents
GB0612428D0 (en) 2006-06-22 2006-08-02 Prolysis Ltd Antibacterial agents
NZ578159A (en) 2006-12-04 2012-01-12 Astrazeneca Ab Antibacterial polycyclic urea compounds
GB0724342D0 (en) 2007-12-13 2008-01-30 Prolysis Ltd Anitbacterial compositions
US20110166088A1 (en) 2008-06-25 2011-07-07 Ranbaxy Laboratories Limited Benzothiazoles and aza-analogues thereof use as antibacterial agents
US9481675B2 (en) 2009-09-11 2016-11-01 Merck Sharp & Dohme Corp. Gyrase inhibitors
CA2777741A1 (en) 2009-10-16 2011-04-21 Rib-X Pharmaceuticals, Inc. Antimicrobial compounds and methods of making and using the same
JP5864589B2 (ja) 2010-10-08 2016-02-17 ビオタ ヨーロッパ リミテッドＢｉｏｔａ Ｅｕｒｏｐｅ Ｌｔｄ 細菌トポイソメラーゼｉｉ阻害性２−エチルカルバモイルアミノ−１，３−ベンゾチアゾール−５−イル類
AU2012205416B2 (en) * 2011-01-14 2017-02-02 Spero Therapeutics, Inc. 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
US8481551B2 (en) 2011-01-14 2013-07-09 Vertex Pharmaceuticals Incorporated 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
PT2663556E (pt) 2011-01-14 2014-11-27 Vertex Pharma Processo de fabrico de inibidores de girase e topoisomerase iv
JP5977344B2 (ja) 2011-06-20 2016-08-24 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ジャイレースおよびトポイソメラーゼ阻害剤のリン酸エステル
JP2015514063A (ja) 2012-03-22 2015-05-18 ビオタ ヨーロッパ リミテッドＢｉｏｔａ Ｅｕｒｏｐｅ Ｌｔｄ 抗菌化合物
US9572809B2 (en) * 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases
AR093226A1 (es) * 2012-07-18 2015-05-27 Vertex Pharma Formas solidas de dihidrogeno fosfato de (r)-2-(5-(2-(3-etilureido)-6-fluoro-7-(tetrahidrofuran-2-il)-1h-benzo[d]imidazol-5-il)pirimidin-2-il)propan-2-ilo y sus sales

Also Published As

Publication number Publication date
WO2012097274A1 (en) 2012-07-19
EP2663556B1 (en) 2014-10-15
US20120184742A1 (en) 2012-07-19
KR101882172B1 (ko) 2018-07-26
US20130261305A1 (en) 2013-10-03
KR20140037028A (ko) 2014-03-26
IL227405B (en) 2018-05-31
AR084864A1 (es) 2013-07-10
SG191945A1 (en) 2013-08-30
JP2014503558A (ja) 2014-02-13
MX355561B (es) 2018-04-23
AU2012205420B2 (en) 2016-12-08
CA2824519A1 (en) 2012-07-19
EP2663556A1 (en) 2013-11-20
PT2663556E (pt) 2014-11-27
JP6006235B2 (ja) 2016-10-12
ZA201305232B (en) 2014-11-26
CA2824519C (en) 2020-06-16
RU2619116C2 (ru) 2017-05-12
NZ612920A (en) 2015-10-30
AU2012205420A1 (en) 2013-08-01
MX2013008164A (es) 2013-08-27
IL227405A0 (en) 2013-09-30
TWI534143B (zh) 2016-05-21
BR112013017968B1 (pt) 2021-03-16
CN103384665A (zh) 2013-11-06
CN103384665B (zh) 2018-01-09
US8912326B2 (en) 2014-12-16
RU2013137751A (ru) 2015-02-20
ES2526902T3 (es) 2015-01-16
US8471014B2 (en) 2013-06-25
TW201307332A (zh) 2013-02-16

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Legal Events

Date Code Title Description
B25G Requested change of headquarter approved

Owner name: VERTEX PHARMACEUTICALS INCORPORATED (US)

B25A Requested transfer of rights approved

Owner name: SPERO TRINEM, INC. (US)

B25B Requested transfer of rights rejected

Owner name: SPERO TRINEM, INC. (US)

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B25A Requested transfer of rights approved

Owner name: SPERO THERAPEUTICS INC. (US)

B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 13/01/2012, OBSERVADAS AS CONDICOES LEGAIS.