WO2008146919A1 - リンコサミド誘導体及びこれを有効成分とする抗菌剤 - Google Patents

リンコサミド誘導体及びこれを有効成分とする抗菌剤 Download PDF

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Publication number
WO2008146919A1
WO2008146919A1 PCT/JP2008/060045 JP2008060045W WO2008146919A1 WO 2008146919 A1 WO2008146919 A1 WO 2008146919A1 JP 2008060045 W JP2008060045 W JP 2008060045W WO 2008146919 A1 WO2008146919 A1 WO 2008146919A1
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WO
WIPO (PCT)
Prior art keywords
group
derivative
lincosamide
membered monocyclic
monocyclic heterocyclic
Prior art date
Application number
PCT/JP2008/060045
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English (en)
French (fr)
Inventor
Eijirou Umemura
Kou Kumura
Satomi Masaki
Kazutaka Ueda
Yoshinari Wakiyama
Yasuo Sato
Mikio Yamamoto
Keiichi Ajito
Takashi Watanabe
Chizuko Kaji
Original Assignee
Meiji Seika Kaisha, 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 Meiji Seika Kaisha, Ltd. filed Critical Meiji Seika Kaisha, Ltd.
Priority to US12/451,752 priority Critical patent/US7867980B2/en
Priority to JP2009516374A priority patent/JP5290166B2/ja
Priority to EP08777056A priority patent/EP2166015A4/en
Publication of WO2008146919A1 publication Critical patent/WO2008146919A1/ja

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/14—Acyclic radicals, not substituted by cyclic structures attached to a sulfur, selenium or tellurium atom of a saccharide radical
    • C07H15/16—Lincomycin; Derivatives thereof
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

　本発明によれば、式（Ｉ）［式中、Ａは、アリール基を表してＲ１は、５または６員の単環式の複素環基を表すかまたは、Ａは４～６員の単環式の複素環基を表して、Ｒ１はアリール基または、５または６員の単環式の複素環基を表し、Ｒ２は水素原子またはＣ１－６アルキル基を表し、Ｒ３はＣ１－６アルキル基またはＣ３－６シクロアルキル－Ｃ１－４アルキル基を表し、Ｒ４、Ｒ５、およびＲ６は水素原子を表し、Ｒ７はＣ１－６アルキル基を表し、ｍは１～３を表す］の化合物またはその薬理学的に許容されうる塩もしくは溶媒和物が提供される。この化合物は、耐性肺炎球菌に強い活性を有する新規リンコサミド誘導体である。またこの化合物は、抗菌剤として用いることができ、細菌性感染症の予防または治療に有用である。 　　【化１】
PCT/JP2008/060045 2007-05-31 2008-05-30 リンコサミド誘導体及びこれを有効成分とする抗菌剤 WO2008146919A1 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US12/451,752 US7867980B2 (en) 2007-05-31 2008-05-30 Lincosamide derivatives and antimicrobial agents comprising the same as active ingredient
JP2009516374A JP5290166B2 (ja) 2007-05-31 2008-05-30 リンコサミド誘導体及びこれを有効成分とする抗菌剤
EP08777056A EP2166015A4 (en) 2007-05-31 2008-05-30 LINCOSAMIDE DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING ACTIVE SUBSTANCE

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-146200 2007-05-31
JP2007146200 2007-05-31

Publications (1)

Publication Number Publication Date
WO2008146919A1 true WO2008146919A1 (ja) 2008-12-04

Family

ID=40075149

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/060045 WO2008146919A1 (ja) 2007-05-31 2008-05-30 リンコサミド誘導体及びこれを有効成分とする抗菌剤

Country Status (4)

Country Link
US (1) US7867980B2 (ja)
EP (1) EP2166015A4 (ja)
JP (1) JP5290166B2 (ja)
WO (1) WO2008146919A1 (ja)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2397283T3 (es) * 2006-07-25 2013-03-06 Cephalon, Inc. Derivados de piridizinona
CA2871766C (en) 2011-12-08 2020-06-16 The Board Of Regents Of The University Of Texas System Piperidine-based small molecule 5-hydroxytryptamine 2c receptor (5-ht2cr) allosteric modulators
CZ2017137A3 (cs) * 2017-03-10 2018-05-23 Mikrobiologický ústav AV ČR, v. v. i. Linkosamidy, jejich příprava a použití
WO2019032936A1 (en) * 2017-08-10 2019-02-14 President Adn Fellows Of Harvard College LINCONSAMIDE ANTIBIOTICS AND USES THEREOF
US11566039B2 (en) 2017-08-10 2023-01-31 President And Fellows Of Harvard College Lincosamide antibiotics and uses thereof
CN108226324B (zh) * 2017-12-14 2021-01-12 兆科（广州）眼科药物有限公司 一种盐酸克林霉素的杂质控制方法
CN108203404A (zh) * 2018-03-02 2018-06-26 上海博邦医药科技有限公司 (r)-3-苯基哌啶或/和(s)-3-苯基哌啶以及尼拉帕尼的手性中间体的合成方法
CN112110898B (zh) * 2020-09-25 2022-07-05 西南大学 辛弗林磺酰化衍生物及其中间体、制备方法和应用

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3418414A (en) 1966-08-31 1968-12-24 Upjohn Co Trimethylsilyl ethers of lincomycin and its compounds
US3544551A (en) 1968-04-30 1970-12-01 Upjohn Co 7-mercapto-7-deoxylincomycins and process for preparing the same
US3689474A (en) 1970-08-04 1972-09-05 Upjohn Co 7-mercapto-7-deoxylincomycins and process for preparing the same
DE2229950A1 (de) 1971-06-23 1972-12-28 The Upjohn Co., Kalamazoo, Mich. (V.St.A.) Verfahren zur Herstellung von Alkyl-7-deoxy-7RS tief n -alpha-thiolincosaminiden
US3767649A (en) 1971-11-15 1973-10-23 Upjohn Co Process for making derivatives of lincomycin and its analogs
US3870699A (en) 1973-03-06 1975-03-11 Upjohn Co Lincomycin analogs
US3915954A (en) 1971-11-15 1975-10-28 Upjohn Co Derivatives of lincomycin and its analogs and process
WO2005007665A2 (en) * 2003-06-17 2005-01-27 Vicuron Pharmaceuticals Inc. Lincomycin derivatives possessing antibacterial activity
WO2005012320A2 (en) 2003-06-17 2005-02-10 Vicuron Pharmaceuticals, Inc. Novel lincomycin derivatives possessing antimicrobial activity
JP2006504673A (ja) * 2002-08-15 2006-02-09 バイクロン ファーマシューティカルズ， インコーポレイテッド 抗菌活性を有するリンコマイシン誘導体
WO2006055070A2 (en) * 2004-11-17 2006-05-26 Vicuron Pharmaceuticals Inc. Novel lincomycin derivatives possessing antibacterial activity
JP2007146200A (ja) 2005-11-25 2007-06-14 Nisshin Steel Co Ltd アルミニウム材料に対するスポット溶接性に優れた溶融アルミニウムめっき鋼板
WO2007066805A1 (ja) * 2005-12-09 2007-06-14 Meiji Seika Kaisha, Ltd. リンコマイシン誘導体およびこれを有効成分とする抗菌剤

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7199105B2 (en) * 2002-08-15 2007-04-03 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity
US7256177B2 (en) * 2003-06-17 2007-08-14 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity
US7199106B2 (en) * 2003-06-17 2007-04-03 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antimicrobial activity

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3418414A (en) 1966-08-31 1968-12-24 Upjohn Co Trimethylsilyl ethers of lincomycin and its compounds
US3544551A (en) 1968-04-30 1970-12-01 Upjohn Co 7-mercapto-7-deoxylincomycins and process for preparing the same
US3689474A (en) 1970-08-04 1972-09-05 Upjohn Co 7-mercapto-7-deoxylincomycins and process for preparing the same
DE2229950A1 (de) 1971-06-23 1972-12-28 The Upjohn Co., Kalamazoo, Mich. (V.St.A.) Verfahren zur Herstellung von Alkyl-7-deoxy-7RS tief n -alpha-thiolincosaminiden
US3915954A (en) 1971-11-15 1975-10-28 Upjohn Co Derivatives of lincomycin and its analogs and process
US3767649A (en) 1971-11-15 1973-10-23 Upjohn Co Process for making derivatives of lincomycin and its analogs
US3870699A (en) 1973-03-06 1975-03-11 Upjohn Co Lincomycin analogs
JP2006504673A (ja) * 2002-08-15 2006-02-09 バイクロン ファーマシューティカルズ， インコーポレイテッド 抗菌活性を有するリンコマイシン誘導体
WO2005007665A2 (en) * 2003-06-17 2005-01-27 Vicuron Pharmaceuticals Inc. Lincomycin derivatives possessing antibacterial activity
WO2005012320A2 (en) 2003-06-17 2005-02-10 Vicuron Pharmaceuticals, Inc. Novel lincomycin derivatives possessing antimicrobial activity
WO2006055070A2 (en) * 2004-11-17 2006-05-26 Vicuron Pharmaceuticals Inc. Novel lincomycin derivatives possessing antibacterial activity
JP2007146200A (ja) 2005-11-25 2007-06-14 Nisshin Steel Co Ltd アルミニウム材料に対するスポット溶接性に優れた溶融アルミニウムめっき鋼板
WO2007066805A1 (ja) * 2005-12-09 2007-06-14 Meiji Seika Kaisha, Ltd. リンコマイシン誘導体およびこれを有効成分とする抗菌剤

Non-Patent Citations (14)

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Title
BIRKENMEYER R.D. ET AL.: "Synthesis and antimicrobial activity of clindamycin analogues: Pirlimycin, a potent antibacterial agent", J. MED. CHEM., vol. 27, no. 2, 1984, pages 216 - 223, XP002174848 *
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J. ANTIBIOTICS, vol. 49, 1996, pages 941
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See also references of EP2166015A4 *
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TETRAHEDRON LETT., vol. 35, 1994, pages 2053
TETRAHEDRON LETT., vol. 43, 2002, pages 3499

Also Published As

Publication number Publication date
US7867980B2 (en) 2011-01-11
JP5290166B2 (ja) 2013-09-18
EP2166015A1 (en) 2010-03-24
EP2166015A4 (en) 2012-09-05
US20100184746A1 (en) 2010-07-22
JPWO2008146919A1 (ja) 2010-08-19

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