EA200200769A1 - Ингибиторы гиразы и их применение - Google Patents

Ингибиторы гиразы и их применение

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Publication number
EA200200769A1
EA200200769A1 EA200200769A EA200200769A EA200200769A1 EA 200200769 A1 EA200200769 A1 EA 200200769A1 EA 200200769 A EA200200769 A EA 200200769A EA 200200769 A EA200200769 A EA 200200769A EA 200200769 A1 EA200200769 A1 EA 200200769A1
Authority
EA
Eurasian Patent Office
Prior art keywords
giraz
inhibitors
oxazole
pyrazole
thiazole
Prior art date
Application number
EA200200769A
Other languages
English (en)
Other versions
EA005680B1 (ru
Inventor
Пол Чарифсон
Дин Стамос
Майкл Бадиа
Анн-Лор Грийо
Стивен Ронкин
Мартэн Трюдо
Original Assignee
Вертекс Фармасьютикалз Инкорпорейтед
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 Вертекс Фармасьютикалз Инкорпорейтед filed Critical Вертекс Фармасьютикалз Инкорпорейтед
Publication of EA200200769A1 publication Critical patent/EA200200769A1/ru
Publication of EA005680B1 publication Critical patent/EA005680B1/ru

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    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/427—Thiazoles 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • 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
    • 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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I)в которых кольцо А означает тиазол, оксазол, имидазол или пиразол, а заместители являются такими, как определено в описании, и к его фармацевтически приемлемым солям. Соединение ингибирует активность бактериальной гиразы и поэтому используется для лечения бактериальных инфекционных заболеваний млекопитающих.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200200769A 2000-01-18 2001-01-16 Ингибиторы гиразы и их применение для лечения бактериальной инфекции EA005680B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17667100P 2000-01-18 2000-01-18
US25433100P 2000-12-08 2000-12-08
PCT/US2001/001374 WO2001052845A1 (en) 2000-01-18 2001-01-16 Gyrase inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
EA200200769A1 true EA200200769A1 (ru) 2002-12-26
EA005680B1 EA005680B1 (ru) 2005-04-28

Family

ID=26872470

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200200769A EA005680B1 (ru) 2000-01-18 2001-01-16 Ингибиторы гиразы и их применение для лечения бактериальной инфекции

Country Status (23)

Country Link
US (2) US6608087B1 (ru)
EP (1) EP1251848B1 (ru)
JP (1) JP2003520233A (ru)
CN (1) CN1230166C (ru)
AR (1) AR027518A1 (ru)
AT (1) ATE269701T1 (ru)
AU (1) AU782883B2 (ru)
BR (1) BR0107713A (ru)
CA (1) CA2397686A1 (ru)
CO (1) CO5261612A1 (ru)
DE (1) DE60103974T2 (ru)
DK (1) DK1251848T3 (ru)
EA (1) EA005680B1 (ru)
ES (1) ES2222336T3 (ru)
HK (1) HK1053984B (ru)
MX (1) MXPA02007134A (ru)
MY (1) MY133572A (ru)
NZ (1) NZ520628A (ru)
PT (1) PT1251848E (ru)
SI (1) SI1251848T1 (ru)
TR (1) TR200401735T4 (ru)
TW (1) TWI287449B (ru)
WO (1) WO2001052845A1 (ru)

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WO2002088101A2 (en) * 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
DE60211348T2 (de) * 2001-08-13 2007-02-08 Janssen Pharmaceutica N.V. 2,4,5-trisubstituted thiazolyl derivative und deren antiinflammatorische wirkung
US6984652B2 (en) * 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
TW200526626A (en) 2003-09-13 2005-08-16 Astrazeneca Ab Chemical compounds
FR2865733B1 (fr) * 2004-02-04 2007-10-12 Merck Sante Sas Derives de thiazolylimidazole, leurs procedes de preparation, les compositions pharmaceutiques qui les contiennent et leurs applications en medecine
US20080234132A1 (en) * 2004-11-19 2008-09-25 Laurence Coquin Microcin B17 Analogs And Methods For Their Preparation And Use
NZ561613A (en) 2005-02-18 2010-12-24 Astrazeneca Ab Antibacterial piperidine derivatives
EP2028936A4 (en) * 2006-02-13 2014-02-26 Univ Boston COMPOSITIONS AND METHODS FOR POTENTIATING ANTIBIOTICS AND DISCOVERING DRUGS
JP5269779B2 (ja) 2006-06-21 2013-08-21 クック・バイオテック・インコーポレーテッド 胃腸瘻の治療に有用な瘻グラフト及び関連する方法とシステム
WO2008019292A2 (en) * 2006-08-04 2008-02-14 Trustees Of Boston University Compositions and methods for potentiating antibiotic activity
TW200906412A (en) * 2007-06-12 2009-02-16 Astrazeneca Ab Piperidine compounds and uses thereof
EP2217588A4 (en) * 2007-11-02 2013-12-04 Methylgene Inc INHIBITORS OF HISTONE DEACETYLASE
EP2250160B1 (en) 2008-01-25 2015-11-11 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
JP5384611B2 (ja) * 2008-03-21 2014-01-08 ノバルティス アーゲー 新規ヘテロ環式化合物およびそれらの使用
US8865732B2 (en) * 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
CN102089303A (zh) * 2008-07-17 2011-06-08 旭化成制药株式会社 含氮杂环化合物
PE20110843A1 (es) * 2008-09-22 2011-12-08 Cayman Chem Co Derivados de 5-(1h-imidazol-5-il)-2-fenilpirimidina, como inhibidores de prostaglandina d sintasa hematopoyetica
US8071605B2 (en) 2008-12-12 2011-12-06 Astrazeneca Ab Piperidine compounds for use in the treatment of bacterial infections
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AR077971A1 (es) 2009-08-26 2011-10-05 Astrazeneca Ab Derivados heterociclicos de urea y metodos de uso de los mismos
JP2013514287A (ja) * 2009-12-17 2013-04-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング スフィンゴシンキナーゼの阻害薬
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MA34797B1 (fr) 2010-08-11 2014-01-02 Millennium Pharm Inc Hétéroaryles et leurs utilisations
EP2603216A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
EP2627181A4 (en) 2010-10-13 2014-03-19 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
CN102911173A (zh) * 2012-11-08 2013-02-06 苏州施亚生物科技有限公司 5,6,7,8-四氢-2H-吡啶并[4,3-c]哒嗪-3-酮的合成方法
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
BR112016018048A2 (pt) 2014-02-03 2017-08-08 Spero Gyrase Inc Método para o tratamento ou prevenção de uma infecção bacteriana, uso de um inibidor de topoisomerase tipo ii bacteriana em combinação com uma polimixina ou derivado de polimixina no tratamento ou prevenção de uma infecção bacteriana, uso de um inibidor de topoisomerase tipo ii bacteriana em combinação com uma polimixina ou derivado de polimixina na preparação de um medicamento para o tratamento ou prevenção de uma infecção bacteriana, método para melhorar a atividade antibacteriana de um inibidor de topoisomerase tipo ii bacteriana, método para melhorar a eficácia bactericida de um inibidor de topoisomerase tipo ii bacteriana, composição, agente antibacteriano, processo, e, composto
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
EP3604281A4 (en) 2017-03-24 2020-08-19 Taisho Pharmaceutical Co., Ltd. 2 (1H) -CHINOLINONE DERIVATIVE
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WO2022129327A1 (en) 2020-12-17 2022-06-23 Univerza V Ljubljani New n-phenylpyrrolamide inhibitors of dna gyrase and topoisomerase iv with antibacterial activity

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Also Published As

Publication number Publication date
DK1251848T3 (da) 2004-10-18
US6608087B1 (en) 2003-08-19
ATE269701T1 (de) 2004-07-15
HK1053984A1 (en) 2003-11-14
AU782883B2 (en) 2005-09-08
CN1400898A (zh) 2003-03-05
AR027518A1 (es) 2003-04-02
ES2222336T3 (es) 2005-02-01
EA005680B1 (ru) 2005-04-28
PT1251848E (pt) 2004-10-29
SI1251848T1 (en) 2004-12-31
MY133572A (en) 2007-11-30
EP1251848A1 (en) 2002-10-30
TWI287449B (en) 2007-10-01
CA2397686A1 (en) 2001-07-26
US6930116B2 (en) 2005-08-16
US20040024030A1 (en) 2004-02-05
EP1251848B1 (en) 2004-06-23
BR0107713A (pt) 2002-11-19
AU3094001A (en) 2001-07-31
JP2003520233A (ja) 2003-07-02
DE60103974T2 (de) 2005-06-30
CO5261612A1 (es) 2003-03-31
WO2001052845A1 (en) 2001-07-26
HK1053984B (zh) 2006-07-28
CN1230166C (zh) 2005-12-07
NZ520628A (en) 2004-05-28
TR200401735T4 (tr) 2004-08-23
DE60103974D1 (de) 2004-07-29
MXPA02007134A (es) 2003-03-27

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU