JP5539898B2 - 抗菌活性縮合チアゾール - Google Patents

抗菌活性縮合チアゾール Download PDF

Info

Publication number
JP5539898B2
JP5539898B2 JP2010537517A JP2010537517A JP5539898B2 JP 5539898 B2 JP5539898 B2 JP 5539898B2 JP 2010537517 A JP2010537517 A JP 2010537517A JP 2010537517 A JP2010537517 A JP 2010537517A JP 5539898 B2 JP5539898 B2 JP 5539898B2
Authority
JP
Japan
Prior art keywords
ethyl
thiazol
mmol
urea
benzo
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.)
Expired - Fee Related
Application number
JP2010537517A
Other languages
English (en)
Japanese (ja)
Other versions
JP2011506417A (ja
JP2011506417A5 (https=
Inventor
ハイドン，デヴィッド，ジョン
ツザプルウスキ，ロイド，ジョージ
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.)
Biota Europe Ltd
Original Assignee
Biota Europe 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
Application filed by Biota Europe Ltd filed Critical Biota Europe Ltd
Publication of JP2011506417A publication Critical patent/JP2011506417A/ja
Publication of JP2011506417A5 publication Critical patent/JP2011506417A5/ja
Application granted granted Critical
Publication of JP5539898B2 publication Critical patent/JP5539898B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
JP2010537517A 2007-12-13 2008-12-12 抗菌活性縮合チアゾール Expired - Fee Related JP5539898B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0724342.1 2007-12-13
GBGB0724342.1A GB0724342D0 (en) 2007-12-13 2007-12-13 Anitbacterial compositions
PCT/GB2008/004114 WO2009074812A1 (en) 2007-12-13 2008-12-12 Antibacterial condensed thiazoles

Publications (3)

Publication Number Publication Date
JP2011506417A JP2011506417A (ja) 2011-03-03
JP2011506417A5 JP2011506417A5 (https=) 2012-02-16
JP5539898B2 true JP5539898B2 (ja) 2014-07-02

Family

ID=39048076

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2010537517A Expired - Fee Related JP5539898B2 (ja) 2007-12-13 2008-12-12 抗菌活性縮合チアゾール

Country Status (14)

Country Link
US (1) US8299065B2 (https=)
EP (1) EP2231653B1 (https=)
JP (1) JP5539898B2 (https=)
KR (1) KR20100105847A (https=)
CN (1) CN102015700B (https=)
AU (1) AU2008334427B2 (https=)
BR (1) BRPI0820656A2 (https=)
CA (1) CA2709021A1 (https=)
EA (1) EA018104B1 (https=)
ES (1) ES2416059T3 (https=)
GB (1) GB0724342D0 (https=)
MX (1) MX2010006428A (https=)
NZ (1) NZ586508A (https=)
WO (1) WO2009074812A1 (https=)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009254928A1 (en) * 2008-06-04 2009-12-10 Astrazeneca Ab Thiazolo [5, 4-B] pyridine and oxazolo [5, 4-B] pyridine derivatives as antibacterial agents
EP2321309A1 (en) * 2008-06-25 2011-05-18 Ranbaxy Laboratories Limited Benzothiazoles and aza-analogues thereof use as antibacterial agents
US9216979B2 (en) 2009-10-16 2015-12-22 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
KR101972992B1 (ko) * 2009-10-16 2019-04-29 멜린타 서브시디어리 코프. 항미생물성 화합물 및 이의 제조 방법 및 사용 방법
WO2011047320A2 (en) 2009-10-16 2011-04-21 Rib-X Pharmaceuticals, Inc. Antimicrobial compounds and methods of making and using the same
RU2012146246A (ru) * 2010-03-31 2014-05-10 Актелион Фармасьютиклз Лтд Антибактериальные производные изохинолин-3-илмочевины
EP2576570A1 (en) 2010-05-26 2013-04-10 Boehringer Ingelheim International GmbH 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
EP2625178A4 (en) * 2010-10-08 2014-04-30 Biota Europe Ltd BACTERIA TOPOISOMERASE II FOR INHIBITING 2-ETHYL CARBAMOYLAMINE-1,3-BENZOTHIAZOL-5-YLENE
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
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
KR101882172B1 (ko) 2011-01-14 2018-07-26 스페로 트리넴, 인코포레이티드 자이라제 및 토포이소머라제 ⅳ 억제제의 제조방법
RU2609259C2 (ru) 2011-01-14 2017-01-31 Сперо Тринем, Инк. Пиримидиновые ингибиторы гиразы и топоизомеразы iv
EP2691399B1 (en) * 2011-03-28 2016-07-13 F.Hoffmann-La Roche Ag Thiazolopyrimidine compounds
AR088729A1 (es) 2011-03-29 2014-07-02 Actelion Pharmaceuticals Ltd Derivados de 3-ureidoisoquinolin-8-ilo y una composicion farmaceutica
KR20140065378A (ko) 2011-04-15 2014-05-29 멜린타 테라퓨틱스, 인크. 항미생물 화합물 및 그의 제조 방법과 사용 방법
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
US9822108B2 (en) 2012-01-13 2017-11-21 Rutgers, The State University Of New Jersey Antimicrobial agents
US9475783B2 (en) 2012-03-21 2016-10-25 Rutgers, The State University Of New Jersey Antimicrobial agents
WO2013138860A1 (en) 2012-03-22 2013-09-26 Biota Europe Limited Antibacterial compounds
SG11201408419QA (en) * 2012-07-10 2015-01-29 Bayer Pharma AG Method for preparing substituted triazolopyridines
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
BR112014030284B1 (pt) 2012-07-18 2021-11-30 Sunshine Lake Pharma Co., Ltd Composto, composição farmacêutica, e, uso de um composto ou de uma composição farmacêutica
WO2014096300A2 (en) 2012-12-21 2014-06-26 Janssen R&D Ireland Antibacterial compounds
KR20160070066A (ko) 2013-09-09 2016-06-17 멜린타 테라퓨틱스, 인크. 항균 화합물, 및 이의 제조 방법 및 이용 방법
EP3038623A4 (en) 2013-09-09 2017-04-19 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
US9458150B2 (en) 2013-11-08 2016-10-04 Rutgers, The State University Of New Jersey Antimicrobial agents
US20170007615A1 (en) 2014-02-03 2017-01-12 Biota Europe Ltd Antibacterial Compounds
CN105367547B (zh) * 2014-08-19 2019-04-23 北京桦冠生物技术有限公司 一种噁唑啉酮抗生素的新合成工艺
AR102215A1 (es) * 2014-10-10 2017-02-15 Glaxosmithkline Ip Dev Ltd Compuesto de pirazol-4-carboxamida, composición farmacéutica que lo comprende y su uso para la fabricación de un medicamento
CA2979342A1 (en) 2015-03-11 2016-09-15 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
WO2017147316A1 (en) 2016-02-25 2017-08-31 Taxis Pharmaceuticals, Inc. Synthetic processes and intermediates
CN109069492B (zh) 2016-04-08 2021-12-10 快尔生物技术公司 环稠和的噻唑啉2-吡啶酮、其制备方法及其在治疗和/或预防结核中的用途
WO2017193016A1 (en) 2016-05-06 2017-11-09 Melinta Therapeutics, Inc. Antimicrobials and methods of making and using same
CA3057431A1 (en) 2017-03-24 2018-09-27 Taisho Pharmaceutical Co., Ltd. 2(1h)-quinolinone derivative
US10774093B2 (en) 2017-03-30 2020-09-15 Taxis Pharmaceuticals, Inc. Synthetic processes and synthetic intermediates
CN107325093B (zh) * 2017-07-09 2020-06-05 西南科技大学 具抗菌活性的硫脲类化合物合成及应用
BR112020017159A2 (pt) 2018-02-23 2020-12-22 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Inibidores de glutaminil ciclases bacterianas para uso no tratamento de doenças periodontais e relacionadas
MX2022002877A (es) 2019-09-13 2022-08-08 Nimbus Saturn Inc Antagonistas de cinasa progenitora hematopoyetica 1 (hpk1) y sus usos.
EP4291235A4 (en) 2021-02-12 2025-01-08 Nimbus Saturn, Inc. HPK1 ANTAGONISTS AND USES THEREOF
US11926625B2 (en) 2021-03-05 2024-03-12 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
WO2025202955A1 (en) 2024-03-28 2025-10-02 Pi Industries Ltd. Fused bicyclic compounds and their use as pest control agents

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH505543A (de) * 1968-11-01 1971-04-15 Ciba Geigy Ag Schädlingsbekämpfungsmittel
US4028374A (en) 1975-11-03 1977-06-07 Morton-Norwich Products, Inc. Antibacterial thiocyanatobenzothiazoles
JPS57149280A (en) * 1981-03-10 1982-09-14 Kyowa Hakko Kogyo Co Ltd Amino acid derivative and its preparation
KR20020084116A (ko) 2000-02-07 2002-11-04 애보트 게엠베하 운트 콤파니 카게 2-벤조티아졸릴 우레아 유도체 및 이의 단백질 키나제억제제로서의 용도
AU2001281817B2 (en) 2000-06-21 2005-11-24 F. Hoffmann-La Roche Ag Benzothiazole derivatives
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
AR042956A1 (es) 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
EP1680431A1 (en) 2003-10-17 2006-07-19 Rigel Pharmaceuticals, Inc. Benzothiazole and thiazole'5,5-b!pyridine compositions and their use as ubiquitin ligase inhibitors
US8470829B2 (en) * 2004-09-09 2013-06-25 Chugai Seiyaku Kabushiki Kaisha Imidazolidine derivative and use thereof
GB0612428D0 (en) 2006-06-22 2006-08-02 Prolysis Ltd Antibacterial agents

Also Published As

Publication number Publication date
WO2009074812A1 (en) 2009-06-18
GB0724342D0 (en) 2008-01-30
ES2416059T3 (es) 2013-07-30
CN102015700B (zh) 2014-12-03
NZ586508A (en) 2012-05-25
EP2231653A1 (en) 2010-09-29
MX2010006428A (es) 2010-09-30
JP2011506417A (ja) 2011-03-03
EP2231653B1 (en) 2013-04-03
CA2709021A1 (en) 2009-06-18
EA018104B1 (ru) 2013-05-30
CN102015700A (zh) 2011-04-13
AU2008334427A1 (en) 2009-06-18
BRPI0820656A2 (pt) 2015-06-16
US8299065B2 (en) 2012-10-30
US20100305067A1 (en) 2010-12-02
AU2008334427B2 (en) 2014-06-19
EA201000993A1 (ru) 2011-02-28
KR20100105847A (ko) 2010-09-30

Similar Documents

Publication Publication Date Title
JP5539898B2 (ja) 抗菌活性縮合チアゾール
KR101443795B1 (ko) 항균성 조성물
AU2007330600B2 (en) Antibacterial polycyclic urea compounds
AU2008334425A1 (en) Antibacterial compositions
US8481544B2 (en) Antibacterial compositions
AU2012200669B2 (en) Antibacterial compositions

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20111212

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20111212

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20111222

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130903

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131203

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140422

R150 Certificate of patent or registration of utility model

Ref document number: 5539898

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140501

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees