CN101679218B - 晶体米诺环素碱及其制备方法 - Google Patents

晶体米诺环素碱及其制备方法 Download PDF

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Publication number
CN101679218B
CN101679218B CN2008800059328A CN200880005932A CN101679218B CN 101679218 B CN101679218 B CN 101679218B CN 2008800059328 A CN2008800059328 A CN 2008800059328A CN 200880005932 A CN200880005932 A CN 200880005932A CN 101679218 B CN101679218 B CN 101679218B
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China
Prior art keywords
minocycline base
crystalline
minocycline
organic solvent
base form
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Expired - Fee Related
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CN2008800059328A
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English (en)
Chinese (zh)
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CN101679218A (zh
Inventor
Z·门德斯
J·R·安图内斯
S·马托
W·赫吉
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Hovione Scientia Ltd
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Hovione Inter AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • 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
    • A61K31/65—Tetracyclines
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN2008800059328A 2007-02-23 2008-02-22 晶体米诺环素碱及其制备方法 Expired - Fee Related CN101679218B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PT103661 2007-02-23
PT103661A PT103661B (pt) 2007-02-23 2007-02-23 Processo de preparação de minociclina base cristalina
PCT/GB2008/000625 WO2008102161A2 (en) 2007-02-23 2008-02-22 Crystalline minocycline base and processes for its preparation

Publications (2)

Publication Number Publication Date
CN101679218A CN101679218A (zh) 2010-03-24
CN101679218B true CN101679218B (zh) 2013-10-30

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CN2008800059328A Expired - Fee Related CN101679218B (zh) 2007-02-23 2008-02-22 晶体米诺环素碱及其制备方法

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US (2) US8258327B2 (enExample)
EP (1) EP2125705B1 (enExample)
JP (4) JP2010519247A (enExample)
KR (1) KR101391132B1 (enExample)
CN (1) CN101679218B (enExample)
AU (1) AU2008217619B2 (enExample)
BR (2) BRPI0807319B1 (enExample)
CA (2) CA2722496C (enExample)
DK (1) DK2125705T3 (enExample)
ES (1) ES2610434T3 (enExample)
HU (1) HUE033030T2 (enExample)
IL (1) IL200544A0 (enExample)
MX (2) MX2009008980A (enExample)
NO (1) NO20092960L (enExample)
NZ (1) NZ579626A (enExample)
PL (1) PL2125705T3 (enExample)
PT (1) PT103661B (enExample)
RU (2) RU2485095C2 (enExample)
WO (1) WO2008102161A2 (enExample)
ZA (1) ZA200906517B (enExample)

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US9265725B2 (en) 2002-10-25 2016-02-23 Foamix Pharmaceuticals Ltd. Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof
US10117812B2 (en) 2002-10-25 2018-11-06 Foamix Pharmaceuticals Ltd. Foamable composition combining a polar solvent and a hydrophobic carrier
US20080138296A1 (en) 2002-10-25 2008-06-12 Foamix Ltd. Foam prepared from nanoemulsions and uses
US7704518B2 (en) 2003-08-04 2010-04-27 Foamix, Ltd. Foamable vehicle and pharmaceutical compositions thereof
US9668972B2 (en) 2002-10-25 2017-06-06 Foamix Pharmaceuticals Ltd. Nonsteroidal immunomodulating kit and composition and uses thereof
US20080242642A1 (en) 2007-04-02 2008-10-02 Medicis Pharmaceutical Corporation Minocycline oral dosage forms for the treatment of acne
US8722650B1 (en) 2005-06-24 2014-05-13 Medicis Pharmaceutical Corporation Extended-release minocycline dosage forms
US20080260655A1 (en) 2006-11-14 2008-10-23 Dov Tamarkin Substantially non-aqueous foamable petrolatum based pharmaceutical and cosmetic compositions and their uses
PT103661B (pt) 2007-02-23 2010-09-07 Hovione Farmaciencia S A Processo de preparação de minociclina base cristalina
US8636982B2 (en) 2007-08-07 2014-01-28 Foamix Ltd. Wax foamable vehicle and pharmaceutical compositions thereof
WO2009069006A2 (en) 2007-11-30 2009-06-04 Foamix Ltd. Foam containing benzoyl peroxide
WO2009090495A2 (en) 2007-12-07 2009-07-23 Foamix Ltd. Oil and liquid silicone foamable carriers and formulations
WO2010017310A1 (en) 2008-08-06 2010-02-11 Medicis Pharmaceutical Corporation Method for the treatment of acne and certain dosage forms thereof
PT104350A (pt) * 2009-01-23 2010-07-23 Hovione Farmaci Ncia S A Processo de isolamento de tigeciclina
WO2010125470A2 (en) 2009-04-28 2010-11-04 Foamix Ltd. Foamable vehicle and pharmaceutical compositions comprising aprotic polar solvents and uses thereof
PT104644B (pt) 2009-06-26 2012-11-06 Hovione Farmaciencia S A Formulação tópica contendo uma tetraciclina e método de tratamento de infecções cutâneas usando a mesma
WO2011013008A2 (en) 2009-07-29 2011-02-03 Foamix Ltd. Non surface active agent non polymeric agent hydro-alcoholic foamable compositions, breakable foams and their uses
CA2769625C (en) 2009-07-29 2017-04-11 Foamix Ltd. Non surfactant hydro-alcoholic foamable compositions, breakable foams and their uses
US8945516B2 (en) 2009-10-02 2015-02-03 Foamix Pharmaceuticals Ltd. Surfactant-free water-free foamable compositions, breakable foams and gels and their uses
US9849142B2 (en) 2009-10-02 2017-12-26 Foamix Pharmaceuticals Ltd. Methods for accelerated return of skin integrity and for the treatment of impetigo
US9561241B1 (en) 2011-06-28 2017-02-07 Medicis Pharmaceutical Corporation Gastroretentive dosage forms for minocycline
PT106063B (pt) * 2011-12-19 2017-05-30 Inst Superior Tecnico Minociclina cristalina termorresistente produzida por recristalização com dióxido de carbono
CN104151186B (zh) * 2014-08-11 2016-06-15 重庆福安药业(集团)股份有限公司 替加环素杂质的立体选择性制备方法
PT108223B (pt) * 2015-02-13 2018-05-08 Hovione Farm S A Novas formas polimórficas de minociclina base e processos para a sua preparação
CA2980527A1 (en) 2015-03-23 2016-09-29 BioPharmX, Inc. Pharmaceutical tetracycline composition for dermatological use
WO2017097891A1 (en) * 2015-12-10 2017-06-15 Sandoz Ag Crystalline eravacycline
MX377365B (es) 2016-09-08 2025-03-10 Journey Medical Corp Composiciones y métodos para tratar rosácea y acné.
WO2021191273A1 (en) 2020-03-24 2021-09-30 Hovione Scientia Limited Compositions for use in treating meibomian gland dysfunction
WO2022043457A1 (en) 2020-08-27 2022-03-03 Hovione Scientia Limited Methods and compositions for treating rosacea
CN117105812B (zh) * 2023-08-16 2025-09-26 常州市第四制药厂有限公司 一种米诺环素无菌软膏剂及制备方法

Citations (2)

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US3526629A (en) * 1968-04-02 1970-09-01 American Cyanamid Co Beta-hydroxyethylpiperazinocarboxymethyl - 7 - dimethylamino - 6 - deoxy-6-demethyltetracycline
US3901942A (en) * 1972-09-18 1975-08-26 Farmaceutici Italia Tetracycline derivatives substituted in the 7 position and process for preparing the same

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US299111A (en) * 1884-05-27 Process of and apparatus
US3148212A (en) 1961-12-22 1964-09-08 American Cyanamid Co Reductive alkylation process
USRE26253E (en) * 1963-05-17 1967-08-15 And z-alkylamino-g-deoxytetracycline
JPS5245716B1 (enExample) * 1970-07-10 1977-11-17
CN85101404A (zh) * 1985-05-16 1987-01-17 帝人株式会社 头孢菌素衍生物的生产过程
JPH0737433B2 (ja) 1987-06-11 1995-04-26 協和醗酵工業株式会社 ７−アミノ−６−デメチル−６−デオキシテトラサイクリンの製造法
US5202449A (en) * 1987-07-28 1993-04-13 Nippon Kayaku Kabushiki Kaisha Process for purifying 7-dimethylamino-6-demethyl-6-deoxytetracycline
US4918208A (en) * 1987-07-28 1990-04-17 Nippon Kayaku Kabushiki Kaisha Process for producing 7-dimethylamino-6-demethyl-6-deoxytetracycline
JPH04235188A (ja) * 1990-06-19 1992-08-24 Takeda Chem Ind Ltd ペネム化合物の結晶、その製造方法および抗菌剤
US5262173A (en) * 1992-03-02 1993-11-16 American Cyanamid Company Pulsatile once-a-day delivery systems for minocycline
DE4235133A1 (de) * 1992-10-19 1994-04-21 Bayer Ag Kristallines (R)-(-)-2-Cycloheptyl-N-methylsulfonyl-[4-(2-chinolinyl-methoxy)-phenyl]-acetamid
JP3623531B2 (ja) * 1993-06-07 2005-02-23 ビーエーエスエフ アクチェンゲゼルシャフト 結晶質ｌ−アスコルビン酸−２−燐酸エステルマグネシウム塩の製造法
EA000474B1 (ru) * 1995-07-17 1999-08-26 Варнер-Ламберт Компани Кристаллическая кислая кальциевая соль [r-(r*, r*)]-2-(4-фторфенил)-бета, дельта-дигидрокси-5-(1-метилэтил)-3-фенил-4-[(фениламино)карбонил]-1н-пиррол-1-гептановой кислоты (аторвастатин)
BR9813728A (pt) 1997-12-22 2000-10-10 Schering Corp Composição de dispersão molecular com elevada biodisponibilidade
IE991013A1 (en) * 1998-12-01 2000-07-12 Atropos Ltd A Device
CL2004001884A1 (es) * 2003-08-04 2005-06-03 Pfizer Prod Inc Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros.
AR057649A1 (es) * 2005-05-27 2007-12-12 Wyeth Corp Formas solidas cristalinas de tigeciclina y metodos para preparar las mismas
EP1910273A2 (en) * 2005-07-21 2008-04-16 Paratek Pharmaceuticals, Inc. 10-substituted tetracyclines and methods of use thereof
PT103661B (pt) 2007-02-23 2010-09-07 Hovione Farmaciencia S A Processo de preparação de minociclina base cristalina

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3526629A (en) * 1968-04-02 1970-09-01 American Cyanamid Co Beta-hydroxyethylpiperazinocarboxymethyl - 7 - dimethylamino - 6 - deoxy-6-demethyltetracycline
US3901942A (en) * 1972-09-18 1975-08-26 Farmaceutici Italia Tetracycline derivatives substituted in the 7 position and process for preparing the same

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ROBERT F. R. CHURCH et al..Synthesis of 7-Dimethylamino-6-demethyl-6- deoxytetracycline (Minocycline) via 9-Nitro-6-demethyl-6- deoxytetracycline.《J. Org. Chem.》.1971,第36卷(第5期),723-725. *

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BR122021000846B1 (pt) 2021-08-10
JP2017039742A (ja) 2017-02-23
AU2008217619B2 (en) 2013-01-10
US9416097B2 (en) 2016-08-16
DK2125705T3 (en) 2017-01-16
PL2125705T3 (pl) 2017-02-28
NO20092960L (no) 2009-11-20
BRPI0807319A2 (pt) 2017-05-02
MX340539B (es) 2016-07-13
HUE033030T2 (hu) 2017-11-28
PT103661A (pt) 2008-08-25
RU2009135403A (ru) 2011-03-27
JP2014169319A (ja) 2014-09-18
AU2008217619A1 (en) 2008-08-28
BRPI0807319B1 (pt) 2021-08-10
CA2722496C (en) 2014-06-10
ZA200906517B (en) 2010-09-29
IL200544A0 (en) 2010-05-17
WO2008102161A9 (en) 2008-11-13
KR20100014520A (ko) 2010-02-10
JP2019142882A (ja) 2019-08-29
JP2010519247A (ja) 2010-06-03
CA2722496A1 (en) 2008-08-28
ES2610434T3 (es) 2017-04-27
US20130030195A1 (en) 2013-01-31
WO2008102161A3 (en) 2009-01-08
CN101679218A (zh) 2010-03-24
PT103661B (pt) 2010-09-07
KR101391132B1 (ko) 2014-05-02
CA2835788A1 (en) 2008-08-28
WO2008102161A2 (en) 2008-08-28
EP2125705A2 (en) 2009-12-02
RU2485095C2 (ru) 2013-06-20
MX2009008980A (es) 2009-11-11
US20100286417A1 (en) 2010-11-11
US8258327B2 (en) 2012-09-04
RU2013112021A (ru) 2014-09-27
NZ579626A (en) 2011-12-22
CA2835788C (en) 2018-03-27
RU2577331C2 (ru) 2016-03-20
EP2125705B1 (en) 2016-10-12

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SE01 Entry into force of request for substantive examination
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Owner name: HOVIONE SCIENTIA LTD.

Free format text: FORMER OWNER: HOVIONE INT LTD.

Effective date: 20150908

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Granted publication date: 20131030

CF01 Termination of patent right due to non-payment of annual fee