KR100700475B1 - 마크롤라이드 - Google Patents

마크롤라이드 Download PDF

Info

Publication number
KR100700475B1
KR100700475B1 KR1020017016822A KR20017016822A KR100700475B1 KR 100700475 B1 KR100700475 B1 KR 100700475B1 KR 1020017016822 A KR1020017016822 A KR 1020017016822A KR 20017016822 A KR20017016822 A KR 20017016822A KR 100700475 B1 KR100700475 B1 KR 100700475B1
Authority
KR
South Korea
Prior art keywords
azithromycin
compound
monohydrate form
formula
organic solvent
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
KR1020017016822A
Other languages
English (en)
Korean (ko)
Other versions
KR20020016862A (ko
Inventor
빅토르 센텔라스
라파엘 가르시아
마르타 포치
요세 디아고
요하네스 루데셔
이마쿨라다 보쉬
Original Assignee
바이오케미 에스.에이.
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
Priority claimed from GBGB9915216.7A external-priority patent/GB9915216D0/en
Priority claimed from GBGB9915218.3A external-priority patent/GB9915218D0/en
Priority claimed from GBGB9930059.2A external-priority patent/GB9930059D0/en
Application filed by 바이오케미 에스.에이. filed Critical 바이오케미 에스.에이.
Publication of KR20020016862A publication Critical patent/KR20020016862A/ko
Application granted granted Critical
Publication of KR100700475B1 publication Critical patent/KR100700475B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • 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
    • 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
    • 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
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
KR1020017016822A 1999-06-29 2000-06-27 마크롤라이드 Expired - Fee Related KR100700475B1 (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB9915218.3 1999-06-29
GBGB9915216.7A GB9915216D0 (en) 1999-06-29 1999-06-29 Organic compounds
GBGB9915218.3A GB9915218D0 (en) 1999-06-29 1999-06-29 Organic compounds
GB9915216.7 1999-06-29
GBGB9930059.2A GB9930059D0 (en) 1999-12-20 1999-12-20 Organic compounds
GB9930059.2 1999-12-20

Publications (2)

Publication Number Publication Date
KR20020016862A KR20020016862A (ko) 2002-03-06
KR100700475B1 true KR100700475B1 (ko) 2007-03-28

Family

ID=27269768

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020017016822A Expired - Fee Related KR100700475B1 (ko) 1999-06-29 2000-06-27 마크롤라이드

Country Status (10)

Country Link
US (1) US6703372B1 (enExample)
EP (2) EP1712556B1 (enExample)
JP (2) JP4703924B2 (enExample)
KR (1) KR100700475B1 (enExample)
AT (2) ATE469910T1 (enExample)
AU (1) AU5820400A (enExample)
DE (3) DE60044515D1 (enExample)
ES (2) ES2346782T3 (enExample)
HR (1) HRP20010956B1 (enExample)
WO (1) WO2001000640A1 (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20020231A2 (en) * 2002-03-18 2003-12-31 Pliva D D ISOSTRUCTURAL PSEUDOPOLYMORPHS OF 9-DEOXO-9a-AZA-9a-METHYL-9a-HOMOERYTHROMYCIN A
US6245903B1 (en) 1998-08-21 2001-06-12 Apotex, Inc. Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof
ES2260047T3 (es) 2000-07-25 2006-11-01 Laboratorio Silanes, S.A. De C.V. Proceso de etapa unica para la preparacion de 7,16-deoxi-2-aza-10-o-cladinosil-12-o-desosaminil-4,5-dihidroxi-6-etil-3,5,9,11,13,15-hexametilbiciclo(11.2.1)hexadeca-1(2)-en-ona y obtencion de una forma nueva de 9-deoxo-9a-metil-9a-homoeritromicina a.
ES2172417B1 (es) * 2000-07-31 2003-09-16 Sint Quimica Sa Nueva forma mejorada de azitromicina monohidrato de menor higroscopicidad, procedimiento de preparacion y composiciones farmaceuticas que la comprenden.
HU229488B1 (hu) 2000-11-27 2014-01-28 Sandoz Ag Eljárás makrolid hidrátok elõállítására
HRP20010301A2 (en) * 2001-04-27 2001-12-31 Pliva D D New therapeutic indication for azithromycin in the treatment of non-infective inflammatory diseases
US6861413B2 (en) 2001-05-22 2005-03-01 Pfizer Inc. Stable non-dihydrate azithromycin oral suspensions
EP1652851A1 (en) * 2001-05-22 2006-05-03 Pfizer Products Inc. New crystal form of Azithromycin
DE60209704T2 (de) 2001-05-22 2006-11-16 Pfizer Products Inc., Groton Neue kristallforme von azithromycin
NZ532063A (en) * 2001-12-21 2006-03-31 Pfizer Prod Inc Methods for wet granulating azithromycin
WO2003072589A1 (fr) * 2002-02-26 2003-09-04 Meiji Seika Kaisha, Ltd. Nouveau compose azalide cyclique a 15 chainons, nouveau derive diazalide cyclique a 16 chainons et procede de production de ceux-ci
CN1276919C (zh) * 2002-04-03 2006-09-27 韩美药品株式会社 阿奇霉素的制备方法及其中使用的结晶9－脱氧－9a－氮杂－9a－同型红霉素A水合物
ITMI20021209A1 (it) * 2002-06-04 2003-12-04 Chemi Spa Processo di preparazione di azitromicina ad elevata purezza
GB0214277D0 (en) * 2002-06-20 2002-07-31 Biochemie Gmbh Organic compounds
US6855813B2 (en) 2002-07-19 2005-02-15 Alembic Limited Process for the preparation of azithromycin monohydrate
HRP20020614A2 (en) 2002-07-22 2004-06-30 PLIVA-ISTRAŽIVAČKI INSTITUT d.o.o. Rhombic pseudopolymorph of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin a
GB0224197D0 (en) * 2002-10-17 2002-11-27 Biochemie Gmbh Organic compounds
US20050013835A1 (en) * 2003-07-15 2005-01-20 Pfizer Inc. Stable non-dihydrate azithromycin oral suspensions
EP1648473B1 (en) * 2003-07-24 2009-01-28 PLIVA HRVATSKA d.o.o. Single dose fast dissolving azithromycin
US20060189800A1 (en) * 2003-07-24 2006-08-24 Mitsuru Ohkubo Indolopyrrolocabazole derivative and antitumor agent
US7384921B2 (en) * 2004-02-20 2008-06-10 Enanta Pharmaceuticals, Inc. Polymorphic forms of 6-11 bicyclic ketolide derivatives
US7468428B2 (en) * 2004-03-17 2008-12-23 App Pharmaceuticals, Llc Lyophilized azithromycin formulation
US20060116336A1 (en) * 2004-03-17 2006-06-01 American Pharmaceutical Partners, Inc. Lyophilized azithromycin formulation
US7683162B2 (en) 2004-08-30 2010-03-23 Taro Pharmaceutical Industries Limited Process of preparing a crystalline azithromycin monohydrate
JP2008520686A (ja) * 2004-11-17 2008-06-19 スミスクライン・ビーチャム・コーポレイション 新規な抗菌化合物の使用
CN101177441B (zh) * 2007-12-05 2012-05-23 浙江耐司康药业有限公司 一种稳定的阿奇霉素一水合物结晶的制备方法
CN101445532B (zh) * 2008-12-30 2011-09-21 广东东阳光药业有限公司 阿奇霉素一水合物结晶的制备方法
CN102413826A (zh) 2009-03-13 2012-04-11 达·沃尔泰拉公司 用于消除革兰氏阴性菌的组合物和方法
CN102417531B (zh) * 2011-12-20 2014-06-11 浙江国邦药业有限公司 一种阿奇霉素一水合物的制备方法
CN105030704B (zh) * 2015-06-29 2018-09-07 石药集团欧意药业有限公司 阿奇霉素片剂及其制备方法
CN110684056B (zh) * 2018-07-05 2021-07-13 青岛农业大学 一种阿奇霉素中间体的化学合成方法
CN114516895A (zh) * 2020-11-19 2022-05-20 江苏威奇达药业有限公司 一种阿奇霉素胺结晶方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0984020A2 (en) * 1998-08-21 2000-03-08 Apotex Inc. Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof.

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA835204B (en) * 1982-07-19 1985-02-27 Pfizer N-methyl 11-aza-10-deoxo-10-dihydroerythromycin a,intermediates therefor and processes for their preparation
MX12213A (es) * 1987-07-09 1993-05-01 Pfizer Metodo de preparacion de dihidrato de azitromicina cristalino
ES2122905B1 (es) * 1996-07-11 1999-11-16 Astur Pharma Sa Sintesis de 11,12-hidrogenoortoborato de 9-desoxo-9a-aza-11,12-desoxi-9a-metil-9a-homoeritromicina a. un procedimiento para la preparacion de 9-desoxo-9a-aza-9a-metil-9a-homoeritromicina a dihidrato (azitromicina dihidrato).
GB9705323D0 (en) * 1997-03-14 1997-04-30 Biochemie Sa Organic compounds
EP0994889B1 (en) * 1997-07-08 2004-06-16 Biochemie S.A. Erythromycin a oxime solvates
PT102130A (pt) * 1998-03-13 1999-09-30 Hovione Sociedade Quimica S A Processo de preparacao de dihidrato de azitromicina
GB9824580D0 (en) * 1998-11-10 1999-01-06 Biochemie Sa Organic compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0984020A2 (en) * 1998-08-21 2000-03-08 Apotex Inc. Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof.

Also Published As

Publication number Publication date
US6703372B1 (en) 2004-03-09
WO2001000640A1 (en) 2001-01-04
ES2346782T3 (es) 2010-10-20
DE60029589D1 (de) 2006-09-07
EP1189915B1 (en) 2006-07-26
ATE334136T1 (de) 2006-08-15
HRP20010956B1 (hr) 2010-09-30
JP2003503417A (ja) 2003-01-28
EP1712556B1 (en) 2010-06-02
AU5820400A (en) 2001-01-31
DE20023815U1 (de) 2006-06-08
ES2267549T3 (es) 2007-03-16
DE60044515D1 (de) 2010-07-15
JP4703924B2 (ja) 2011-06-15
KR20020016862A (ko) 2002-03-06
EP1712556A1 (en) 2006-10-18
EP1189915A1 (en) 2002-03-27
ATE469910T1 (de) 2010-06-15
JP2011126894A (ja) 2011-06-30
HRP20010956A2 (en) 2003-08-31
DE60029589T2 (de) 2007-07-19

Similar Documents

Publication Publication Date Title
US6703372B1 (en) Macrolides
EP3027634B1 (en) Process for preparation of tulathromycin
EP1077986B1 (en) Improvements in macrolide production
KR900001166B1 (ko) 마크로라이드 유도체의 제조방법
EP1246831B1 (en) Preparation method of azithromycin dihydrate
CA2261732C (en) Preparation of crystal form ii of clarithromycin
HUP0300418A2 (hu) Eljárás klaritromicin (II) típusú kristálymódosulatainak az előállítására
HU230717B1 (hu) Eljárás a 4"-es helyzetben szubsztituált 9-dezoxo-9a-aza-9a-homoeritromicin-A-származékok előállítására
HRP20030430A2 (en) Macrolide solvates
JP2005529082A5 (enExample)
IE74885B1 (en) Pharmaceutical compounds
CA2376748C (en) Diphosphate salt of a 4''-substituted-9-deoxo-9a-aza-9a-homoerythromycin derivative and its pharmaceutical composition
KR20010080748A (ko) 클라리트로마이신 제조에 있어서 매크로리드 중간체
NZ502829A (en) Process of preparing organic azides characterised by the addition of an epoxy derivative of a carbohydrate providing for a safe pH to produce said azides
CA2322424A1 (en) 5-imino-13-deoxy anthracycline derivatives, their uses, and processes for preparing them
EP0548834B1 (en) Stable hexahydrate of etoposide 4'-phosphate disodium salt
US20050159371A1 (en) Process for producing erythromycin a derivative
GB2411399A (en) Purification of N4-acylcytidine derviatives via their alkali metal or alkaline earth metal salts
HK1118294A (en) Diphosphate salt of a 4"-substituted-9-deoxo-9a-aza-9a-homoerythromycin derivative and its pharmaceutical composition

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

FPAY Annual fee payment

Payment date: 20130221

Year of fee payment: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

FPAY Annual fee payment

Payment date: 20140221

Year of fee payment: 8

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 8

FPAY Annual fee payment

Payment date: 20150226

Year of fee payment: 9

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 9

LAPS Lapse due to unpaid annual fee
PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20160322

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

P22-X000 Classification modified

St.27 status event code: A-4-4-P10-P22-nap-X000

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20160322