CN103080122A - 大环内脂的结晶形式及其用途 - Google Patents

大环内脂的结晶形式及其用途 Download PDF

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Publication number
CN103080122A
CN103080122A CN2011800174629A CN201180017462A CN103080122A CN 103080122 A CN103080122 A CN 103080122A CN 2011800174629 A CN2011800174629 A CN 2011800174629A CN 201180017462 A CN201180017462 A CN 201180017462A CN 103080122 A CN103080122 A CN 103080122A
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cem
crystalline form
water
solution
powder diffraction
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CN2011800174629A
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Chinese (zh)
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D·E·佩雷拉
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Cempra Pharmaceuticals Inc
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Cempra Pharmaceuticals Inc
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Application filed by Cempra Pharmaceuticals Inc filed Critical Cempra Pharmaceuticals Inc
Priority to CN201810569806.0A priority Critical patent/CN108570083A/zh
Publication of CN103080122A publication Critical patent/CN103080122A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • 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
    • 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
    • A61K31/04—Nitro compounds
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN2011800174629A 2010-03-22 2011-03-22 大环内脂的结晶形式及其用途 Pending CN103080122A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201810569806.0A CN108570083A (zh) 2010-03-22 2011-03-22 大环内脂的结晶形式及其用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31606310P 2010-03-22 2010-03-22
US61/316,063 2010-03-22
PCT/US2011/029424 WO2011119604A1 (en) 2010-03-22 2011-03-22 Crystalline forms of a macrolide, and uses therefor

Related Child Applications (1)

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CN201810569806.0A Division CN108570083A (zh) 2010-03-22 2011-03-22 大环内脂的结晶形式及其用途

Publications (1)

Publication Number Publication Date
CN103080122A true CN103080122A (zh) 2013-05-01

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CN2011800174629A Pending CN103080122A (zh) 2010-03-22 2011-03-22 大环内脂的结晶形式及其用途
CN201810569806.0A Pending CN108570083A (zh) 2010-03-22 2011-03-22 大环内脂的结晶形式及其用途

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US (4) US8975386B2 (https=)
EP (2) EP3009442B1 (https=)
JP (4) JP5711352B2 (https=)
KR (2) KR102006200B1 (https=)
CN (2) CN103080122A (https=)
AU (2) AU2011232627B2 (https=)
BR (1) BR112012023950A2 (https=)
CA (1) CA2793884C (https=)
DK (1) DK2550286T3 (https=)
ES (1) ES2564097T3 (https=)
HR (1) HRP20160168T1 (https=)
IL (1) IL222018B (https=)
MX (1) MX361413B (https=)
MY (1) MY162411A (https=)
NZ (1) NZ602544A (https=)
PL (1) PL2550286T3 (https=)
RU (1) RU2650883C2 (https=)
SI (1) SI2550286T1 (https=)
WO (1) WO2011119604A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104151382A (zh) * 2014-08-08 2014-11-19 广东东阳光药业有限公司 一种固态大环内酯的新晶型
CN104311611A (zh) * 2014-08-13 2015-01-28 广东东阳光药业有限公司 一种制备固态大环内酯的方法

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EP1638549A4 (en) 2003-03-10 2011-06-15 Optimer Pharmaceuticals Inc NEW ANTIBACTERIAL AGENTS
EP2214484A4 (en) 2007-10-25 2013-01-02 Cempra Pharmaceuticals Inc PROCESS FOR PREPARING ANTIBACTERIAL MAKROLIDE AGENTS
JP5711135B2 (ja) 2008-10-24 2015-04-30 センプラ ファーマシューティカルズ，インコーポレイテッド 胃腸疾患を治療するための方法
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
ES2608285T3 (es) 2009-09-10 2017-04-07 Cempra Pharmaceuticals, Inc. Procedimientos para el tratamiento de paludismo, tuberculosis y enfermedades por MAC
MX361413B (es) * 2010-03-22 2018-12-05 Cempra Pharmaceuticals Inc Star Formas cristalinas de un macrólido y usos para las mismas.
CN102917708B (zh) 2010-05-20 2015-11-25 森普拉制药公司 制备大环内酯和酮内酯及其中间体的方法
EP2613630A4 (en) 2010-09-10 2014-01-15 Cempra Pharmaceuticals Inc HYDROGEN BOND FOR THE PREPARATION OF FLUOROCHETOLIDES FOR THE TREATMENT OF DISEASES
NZ700182A (en) 2012-03-27 2017-02-24 Cempra Pharmaceuticals Inc Parenteral formulations for administering macrolide antibiotics
AU2014239959A1 (en) 2013-03-14 2015-10-01 Cempra Pharmaceuticals, Inc. Methods for treating respiratory diseases and formulations therefor
CN105188712A (zh) 2013-03-15 2015-12-23 森普拉制药公司 用于制备大环内酯抗菌剂的收敛方法
JP6437523B2 (ja) 2013-04-04 2018-12-12 プレジデント アンド フェローズ オブ ハーバード カレッジ マクロライドならびにそれらの調製および使用の方法
SG11201700827RA (en) * 2014-08-05 2017-03-30 Cempra Pharmaceuticals Inc Powder oral suspension formulations of antibacterial agents
CN106998685A (zh) 2014-10-08 2017-08-01 哈佛大学的校长及成员们 14‑元酮内酯及其制备和使用方法
EP3273969A4 (en) 2015-03-25 2018-11-21 President and Fellows of Harvard College Macrolides with modified desosamine sugars and uses thereof
JP6112696B1 (ja) * 2015-10-05 2017-04-12 富山化学工業株式会社 ソリスロマイシンを含む錠剤
EP3190122A1 (en) * 2016-01-08 2017-07-12 LEK Pharmaceuticals d.d. A novel synthetic pathway towards solithromycin and purification thereof
WO2018045294A1 (en) * 2016-09-02 2018-03-08 Cempra Pharmaceuticals, Inc. Processes for preparing fluoroketolides
EP4069251A4 (en) * 2019-12-02 2023-12-06 Aliquantumrx, Inc. SALTS AND POLYMORPHS OF CETHROMYCIN FOR THE TREATMENT OF DISEASES

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104151382A (zh) * 2014-08-08 2014-11-19 广东东阳光药业有限公司 一种固态大环内酯的新晶型
CN104311611A (zh) * 2014-08-13 2015-01-28 广东东阳光药业有限公司 一种制备固态大环内酯的方法

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WO2011119604A1 (en) 2011-09-29
BR112012023950A2 (pt) 2016-07-05
AU2016203986A1 (en) 2016-06-30
US20160244472A1 (en) 2016-08-25
JP6121387B2 (ja) 2017-04-26
AU2011232627B2 (en) 2016-03-17
US20130252915A1 (en) 2013-09-26
MY162411A (en) 2017-06-15
KR20180101643A (ko) 2018-09-12
US20190040096A1 (en) 2019-02-07
MX2012010895A (es) 2013-02-15
KR20130056226A (ko) 2013-05-29
MX361413B (es) 2018-12-05
CA2793884C (en) 2019-09-10
ES2564097T3 (es) 2016-03-17
US20130018008A1 (en) 2013-01-17
HK1177937A1 (en) 2013-08-30
EP2550286A1 (en) 2013-01-30
RU2650883C2 (ru) 2018-04-18
HRP20160168T1 (hr) 2016-03-25
SI2550286T1 (sl) 2016-04-29
PL2550286T3 (pl) 2016-07-29
US8975386B2 (en) 2015-03-10
CN108570083A (zh) 2018-09-25
JP2020002168A (ja) 2020-01-09
AU2011232627A1 (en) 2012-10-18
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AU2016203986B2 (en) 2016-10-06
IL222018B (en) 2019-05-30
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EP2550286A4 (en) 2013-10-02
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JP2013522367A (ja) 2013-06-13
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