CN102753558B - 硝基咪唑并噁嗪及其在抗结核治疗中的应用 - Google Patents

硝基咪唑并噁嗪及其在抗结核治疗中的应用 Download PDF

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Publication number
CN102753558B
CN102753558B CN201080041453.9A CN201080041453A CN102753558B CN 102753558 B CN102753558 B CN 102753558B CN 201080041453 A CN201080041453 A CN 201080041453A CN 102753558 B CN102753558 B CN 102753558B
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Prior art keywords
imidazo
nitro
oxazine
dihydro
trifluoromethoxy
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Expired - Fee Related
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CN201080041453.9A
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Chinese (zh)
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CN102753558A (zh
Inventor
威廉·亚历山大·丹尼
安德鲁·M·托姆普松
亚德里恩·布拉泽
马振坤
布赖恩·德斯蒙德·帕尔默
哈米什·斯科特·萨瑟兰
伊韦塔·克门托娃
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Global Alliance for TB Drug Development
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Global Alliance for TB Drug Development
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    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201080041453.9A 2009-07-31 2010-07-30 硝基咪唑并噁嗪及其在抗结核治疗中的应用 Expired - Fee Related CN102753558B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23039609P 2009-07-31 2009-07-31
US61/230,396 2009-07-31
PCT/US2010/043906 WO2011014774A1 (en) 2009-07-31 2010-07-30 Nitroimidazooxazines and their uses in anti-tubercular therapy

Publications (2)

Publication Number Publication Date
CN102753558A CN102753558A (zh) 2012-10-24
CN102753558B true CN102753558B (zh) 2014-10-15

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CN201080041453.9A Expired - Fee Related CN102753558B (zh) 2009-07-31 2010-07-30 硝基咪唑并噁嗪及其在抗结核治疗中的应用

Country Status (12)

Country Link
EP (1) EP2459571B1 (enExample)
JP (1) JP5781072B2 (enExample)
KR (1) KR101746482B1 (enExample)
CN (1) CN102753558B (enExample)
AU (1) AU2010278777B2 (enExample)
BR (1) BR112012002278A2 (enExample)
CA (1) CA2769359C (enExample)
ES (1) ES2536997T3 (enExample)
IN (1) IN2012DN01414A (enExample)
NZ (1) NZ598121A (enExample)
RU (1) RU2542988C2 (enExample)
WO (1) WO2011014774A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9051333B2 (en) 2011-04-15 2015-06-09 Otsuka Pharmaceutical Co., Ltd. 6,7-dihydroimidazo [2,1-b] [1,3]oxazine bactericides
CN104059082B (zh) * 2013-03-21 2016-08-03 苏州迈泰生物技术有限公司 硝基咪唑杂环类化合物及其在制备治疗结核病药物中的应用
KR101682356B1 (ko) 2014-11-04 2016-12-06 한국화학연구원 이미다조 옥사진 유도체, 이의 약학적으로 허용 가능한 염 또는 이의 광학이성질체 및 이를 유효성분으로 함유하는 약제학적 조성물
BR112017015744A2 (pt) 2015-01-29 2018-03-13 Medshine Discovery Inc composto apresentando uma estrutura de fórmula (i), um sal farmaceuticamente aceitável do mesmo ou um isômero ótico do mesmo, composição farmacêutica e uso do composto de fórmula (i) para o tratamento e prevenção de mycobacterium tuberculosis ou outras infecções microbianas
CN108047248A (zh) * 2018-02-12 2018-05-18 丹诺医药(苏州）有限公司 噁唑烷酮-硝基咪唑类偶联分子的应用
CN113527331B (zh) * 2020-04-17 2024-05-28 南京长澳医药科技有限公司 硝基咪唑类衍生物及其制备方法和用途
CN113355439A (zh) * 2021-06-07 2021-09-07 深圳市普瑞康生物技术有限公司 一种结核分枝杆菌潜伏感染及发病的新型组合检测方法
CN114469946B (zh) * 2022-02-24 2023-10-24 首都医科大学附属北京胸科医院 德拉马尼作为cxcl10抑制剂的用途

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997001562A1 (en) * 1995-06-26 1997-01-16 Pathogenesis Corporation Nitroimidazole antibacterial compounds and methods of use thereof
US6087358A (en) * 1995-06-26 2000-07-11 Pathogenesis Corporation Nitro-[2,1-b]imidazopyran compounds and antibacterial uses thereof
WO2006043121A1 (en) * 2004-10-20 2006-04-27 Ranbaxy Laboratories Limited Oxazolidinone derivatives as antimicrobials
CN1922154A (zh) * 2004-02-18 2007-02-28 大塚制药株式会社 生产4－硝基咪唑化合物的方法
WO2007075872A2 (en) * 2005-12-23 2007-07-05 Novartis Ag Nitroimidazole compounds
CN100497345C (zh) * 2003-10-31 2009-06-10 大塚制药株式会社 治疗结核病的2,3-二氢-6-硝基咪唑并[2,1-b]唑化合物
WO2009120789A1 (en) * 2008-03-26 2009-10-01 Global Alliance For Tb Drug Development Bicyclic nitroimidazoles covalently linked to substituted phenyl oxazolidinones

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Publication number Priority date Publication date Assignee Title
AU679626B2 (en) 1994-03-08 1997-07-03 Wyeth Thiazolidinedione derivatives as anti-hyperglycemic agents
TWI347946B (en) * 2002-10-11 2011-09-01 Otsuka Pharma Co Ltd 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound
ATE382609T1 (de) 2004-01-16 2008-01-15 Sumitomo Chemical Co Malononitrilverbindungen als pestizide
JP2009502922A (ja) * 2005-07-28 2009-01-29 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 カスパーゼ阻害剤プロドラッグ

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997001562A1 (en) * 1995-06-26 1997-01-16 Pathogenesis Corporation Nitroimidazole antibacterial compounds and methods of use thereof
US6087358A (en) * 1995-06-26 2000-07-11 Pathogenesis Corporation Nitro-[2,1-b]imidazopyran compounds and antibacterial uses thereof
CN100497345C (zh) * 2003-10-31 2009-06-10 大塚制药株式会社 治疗结核病的2,3-二氢-6-硝基咪唑并[2,1-b]唑化合物
CN1922154A (zh) * 2004-02-18 2007-02-28 大塚制药株式会社 生产4－硝基咪唑化合物的方法
WO2006043121A1 (en) * 2004-10-20 2006-04-27 Ranbaxy Laboratories Limited Oxazolidinone derivatives as antimicrobials
WO2007075872A2 (en) * 2005-12-23 2007-07-05 Novartis Ag Nitroimidazole compounds
WO2009120789A1 (en) * 2008-03-26 2009-10-01 Global Alliance For Tb Drug Development Bicyclic nitroimidazoles covalently linked to substituted phenyl oxazolidinones

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
《抗结核病药物的研究进展》;王超 等;《中国热带医学》;20080430;第8卷(第4期);673-675 *
Synthesis and Structure-activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains;Hamish S. Sutherland et al.;《J. Med. Chem.》;20091207;第53卷;855-866 *
Synthesis, Reduction Potentials, and Antitubercular Activity of Ring A/B Analogues of the Bioreductive Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824);Andrew M. Thompson et al.;《J. Med. Chem.》;20081217;第52卷;637－645 *

Also Published As

Publication number Publication date
ES2536997T3 (es) 2015-06-01
AU2010278777B2 (en) 2015-05-07
JP5781072B2 (ja) 2015-09-16
BR112012002278A2 (pt) 2020-09-15
WO2011014774A1 (en) 2011-02-03
KR101746482B1 (ko) 2017-06-27
RU2542988C2 (ru) 2015-02-27
EP2459571B1 (en) 2015-03-11
IN2012DN01414A (enExample) 2015-06-05
CA2769359C (en) 2017-03-07
EP2459571A1 (en) 2012-06-06
NZ598121A (en) 2013-04-26
CN102753558A (zh) 2012-10-24
CA2769359A1 (en) 2011-02-03
JP2013500996A (ja) 2013-01-10
RU2012107176A (ru) 2013-09-10
AU2010278777A1 (en) 2012-03-01
KR20120084713A (ko) 2012-07-30

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