HRP920491B1 - O-methyl derivatives of azithromycin a, process and intermediates for their preparation, and process of preparation and use thereof in the preparation of pharmaceuticals - Google Patents

O-methyl derivatives of azithromycin a, process and intermediates for their preparation, and process of preparation and use thereof in the preparation of pharmaceuticals

Info

Publication number: HRP920491B1
Authority: HR; Croatia
Prior art keywords: preparation; azithromycin; pharmaceuticals; intermediates; methyl derivatives
Prior art date: 1990-07-18

Application number

HRP-1409/90A

Other languages

English (en)

Inventor

Slobodan Dokic

Original Assignee

Slobodan Dokic

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.)

1990-07-18

Filing date

1992-09-25

Publication date

1998-10-31

1992-09-25 Application filed by Slobodan Dokic filed Critical Slobodan Dokic

1992-09-25 Priority to HRP-1409/90A priority Critical patent/HRP920491B1/xx

1994-08-31 Publication of HRP920491A2 publication Critical patent/HRP920491A2/hr

1998-10-31 Publication of HRP920491B1 publication Critical patent/HRP920491B1/xx

Links

229960004099 azithromycin Drugs 0.000 title abstract 2
238000000034 method Methods 0.000 title 2
239000003814 drug Substances 0.000 title 1
239000000543 intermediate Substances 0.000 title 1
MQTOSJVFKKJCRP-BICOPXKESA-N azithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 MQTOSJVFKKJCRP-BICOPXKESA-N 0.000 abstract 1
150000003839 salts Chemical class 0.000 abstract 1

Classifications

- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Engineering & Computer Science (AREA)
Biochemistry (AREA)
Molecular Biology (AREA)
Genetics & Genomics (AREA)
Biotechnology (AREA)
Chemical Kinetics & Catalysis (AREA)
Animal Behavior & Ethology (AREA)
Oncology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Communicable Diseases (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Saccharide Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

HRP-1409/90A 1990-07-18 1992-09-25 O-methyl derivatives of azithromycin a, process and intermediates for their preparation, and process of preparation and use thereof in the preparation of pharmaceuticals HRP920491B1 (en)

Priority Applications (1)

Application Number	Priority Date	Filing Date	Title
HRP-1409/90A HRP920491B1 (en)	1990-07-18	1992-09-25	O-methyl derivatives of azithromycin a, process and intermediates for their preparation, and process of preparation and use thereof in the preparation of pharmaceuticals

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
YU140990		1990-07-18
HRP-1409/90A HRP920491B1 (en)	1990-07-18	1992-09-25	O-methyl derivatives of azithromycin a, process and intermediates for their preparation, and process of preparation and use thereof in the preparation of pharmaceuticals

Publications (2)

Publication Number	Publication Date
HRP920491A2 HRP920491A2 (en)	1994-08-31
HRP920491B1 true HRP920491B1 (en)	1998-10-31

Family

ID=25554060

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
HRP-1409/90A HRP920491B1 (en)	1990-07-18	1992-09-25	O-methyl derivatives of azithromycin a, process and intermediates for their preparation, and process of preparation and use thereof in the preparation of pharmaceuticals

Country Status (20)

Country	Link
US (1)	US5250518A (cs)
EP (1)	EP0467331B1 (cs)
JP (1)	JP2657132B2 (cs)
CN (1)	CN1029738C (cs)
AT (1)	ATE129715T1 (cs)
BG (1)	BG60593B1 (cs)
CA (1)	CA2046956C (cs)
CZ (1)	CZ280640B6 (cs)
DE (1)	DE69114198T2 (cs)
DK (1)	DK0467331T3 (cs)
ES (1)	ES2081397T3 (cs)
GR (1)	GR3018330T3 (cs)
HR (1)	HRP920491B1 (cs)
HU (4)	HU221803B1 (cs)
PL (1)	PL166379B1 (cs)
RO (1)	RO109338B1 (cs)
RU (1)	RU2045533C1 (cs)
SI (1)	SI9011409A (cs)
SK (1)	SK279075B6 (cs)
UA (1)	UA27105A1 (cs)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
HRP930014A2 (en) *	1993-01-08	1994-08-31	Pliva Pharm & Chem Works	9-deoxo-9a-aza-11-deoxy-9a-homoeritromycin a 9a, 11-cyclic carbamates
HRP931480B1 (en) *	1993-12-08	1997-08-31	Sour Pliva	9a-N-(N'-CARBAMONYL) and 9a-N-(N'-THIOCARBAMONYL) DERIVATES OF 9-DEOXO-9a-HOMOERYTHROMYCIN A
US5605889A (en) *	1994-04-29	1997-02-25	Pfizer Inc.	Method of administering azithromycin
SI1036083T1 (en) *	1997-10-16	2004-10-31	Pliva-Istra�iva�ki institut d.o.o.	Novel 9a-azalides
US6861411B1 (en)	1997-12-02	2005-03-01	Pfizer, Inc.	Method of treating eye infections with azithromycin
RU2122549C1 (ru) *	1997-12-29	1998-11-27	Закрытое акционерное общество "Фосфосорб"	Способ хроматографического выделения и очистки белков, пептидов и их комплексов
HRP970714B1 (en) *	1997-12-31	2003-08-31	Pliva Pharm & Chem Works	Beta,beta-disubstituted derivatives of 9-deoxo-9a-n-ethenyl-9a-aza-9a-homoerythromycin a
TW546302B (en)	1998-05-08	2003-08-11	Biochemie Sa	Improvements in macrolide production
UA70972C2 (uk)	1998-11-20	2004-11-15	Пфайзер Продактс Інк.	13-членні азаліди і їх застосування як антибіотиків
HRP980646B1 (en) *	1998-12-30	2008-02-29	GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o.	Novel oleandomycin derivatives
US7056893B2 (en)	1999-03-31	2006-06-06	Insite Vision, Inc.	Topical treatment for prevention of ocular infections
US6239113B1 (en)	1999-03-31	2001-05-29	Insite Vision, Incorporated	Topical treatment or prevention of ocular infections
HRP990116B1 (en) *	1999-04-20	2007-10-31	GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o.	NOVEL 8a AND 9a- 15-MEMBERED LACTAMES
US6465437B1 (en) *	1999-06-30	2002-10-15	Pfizer Inc.	Diphosphate salt of a 4″-substituted-9-deoxo-9A-AZA-9A- homoerythromycin derivative and its pharmaceutical composition
KR100336447B1 (ko) *	1999-11-24	2002-05-15	민경윤	클라리스로마이신의 개선된 제조방법
US6787342B2 (en) *	2000-02-16	2004-09-07	Merial Limited	Paste formulations
ATE297941T1 (de) *	2000-03-15	2005-07-15	Hanmi Pharm Ind Co Ltd	Verfahren zur herstellung von einer kristallinen form ii von clarythromycin
WO2002015842A2 (en)	2000-08-23	2002-02-28	Wockhardt Limited	Process for preparation of anhydrous azithromycin
RU2202619C2 (ru) *	2001-01-09	2003-04-20	Научно-исследовательский институт химии Нижегородского государственного университета им. Н.И. Лобачевского	Способ определения общей токсичности твердой, жидкой и газообразной сред
HRP20010301A2 (en) *	2001-04-27	2001-12-31	Pliva D D	New therapeutic indication for azithromycin in the treatment of non-infective inflammatory diseases
WO2003070173A2 (en)	2002-02-15	2003-08-28	Sympore Gmbh	Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
AU2003219770B2 (en)	2002-02-15	2008-10-09	Merckle Gmbh	Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
AU2003211113B2 (en)	2002-02-15	2007-08-09	Merckle Gmbh	Antibiotic conjugates
ITMI20022292A1 (it) *	2002-10-29	2004-04-30	Zambon Spa	9a-azalidi ad attivita' antiinfiammatoria.
AU2003264910A1 (en) *	2003-05-30	2005-01-21	Pliva - Istrazivacki Institut D.O.O.	Process for selective alkylation of macrolide and azalide derivatives
US7435805B2 (en) *	2003-05-30	2008-10-14	Glaxpsmithkline Istrazivacki	O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
WO2005021567A1 (en) *	2003-09-02	2005-03-10	Pliva - Istrazivacki Institut D.O.O.	O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
US7468428B2 (en)	2004-03-17	2008-12-23	App Pharmaceuticals, Llc	Lyophilized azithromycin formulation
PT1851236E (pt) *	2005-01-13	2010-10-25	Glaxosmithkline Zagreb	Macrólidos com actividade anti-inflamatória
US8362086B2 (en)	2005-08-19	2013-01-29	Merial Limited	Long acting injectable formulations
TW201038277A (en) *	2009-01-30	2010-11-01	Glaxosmithkline Zagreb	Anti-inflammatory macrolide
EP2384332A1 (en)	2009-01-30	2011-11-09	Glaxo Group Limited	9-deoxo- 9a-methyl- 9a- aza- 9a-h0m0erythr0mycin a derivatives for the treatment of neutrophil dominated inflammatory diseases
CN101830949B (zh) *	2009-03-13	2012-05-23	上海医药工业研究院	一种阿奇霉素衍生物、其中间体及其制备方法和应用
WO2011131749A1 (en)	2010-04-23	2011-10-27	Glaxo Group Limited	New 14 and 15 membered macrolides for the treatment of neutrophil dominated inflammatory diseases
CN102952166A (zh) *	2011-08-28	2013-03-06	山东方明药业集团股份有限公司	聚合物支载硼氢阴离子还原剂合成阿奇霉素中间体的方法
EP2831083A4 (en) *	2012-03-27	2016-03-09	Michael W Burnet	INFLAMMATORY MAKROLIDE
GB201608236D0 (en)	2016-05-11	2016-06-22	Fidelta D O O	Seco macrolide compounds
CN111148750A (zh) *	2017-04-20	2020-05-12	来兴泰德基金会	作为抗癌剂的包含鏻离子的阿奇霉素衍生物
JP2020517748A (ja) *	2017-04-20	2020-06-18	ライジングタイドファウンデーション	抗がん剤としてホスホニウムイオンを含むアジスロマイシン誘導体
US11197872B2 (en)	2017-04-21	2021-12-14	Lunella Biotech, Inc.	Vitamin C and doxycycline: a synthetic lethal combination therapy for eradicating cancer stem cells (CSCs)
CA3060509A1 (en)	2017-04-21	2018-10-25	Federica Sotgia	Targeting hypoxic cancer stem cells (cscs) with doxycycline: implications for improving anti-angiogenic therapy
KR20200010343A (ko)	2017-05-19	2020-01-30	루넬라 바이오테크 인코포레이티드	안티미토신: 암 줄기 세포를 근절하기 위한 미토콘드리아 생물발생의 표적화 억제제
US12006553B2 (en)	2017-05-19	2024-06-11	Lunella Biotech, Inc.	Companion diagnostics for mitochondrial inhibitors
RU2020102908A (ru)	2017-06-26	2021-07-27	Лунелла Байотек, Инк.	Митокетосцины: митохондриальная терапия, нацеленная на кетоновый метаболизм в раковых клетках

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4474768A (en) *	1982-07-19	1984-10-02	Pfizer Inc.	N-Methyl 11-aza-10-deoxo-10-dihydro-erytromycin A, intermediates therefor
JPS61103890A (ja) *	1984-10-26	1986-05-22	Taisho Pharmaceut Co Ltd	６−０−メチルエリスロマイシンａ誘導体
EP0184921A3 (en) *	1984-12-08	1986-10-29	Beecham Group Plc	Erythromycin derivatives
JPS63107994A (ja) *	1986-05-02	1988-05-12	Taisho Pharmaceut Co Ltd	エリスロマイシン誘導体
WO1989002271A1 (en) *	1987-09-10	1989-03-23	Pfizer	Azithromycin and derivatives as antiprotozoal agents

1990
- 1990-07-18 SI SI9011409A patent/SI9011409A/sl not_active IP Right Cessation
1991
- 1991-07-06 SK SK2195-91A patent/SK279075B6/sk unknown
- 1991-07-12 CA CA002046956A patent/CA2046956C/en not_active Expired - Fee Related
- 1991-07-16 CZ CS912195A patent/CZ280640B6/cs not_active IP Right Cessation
- 1991-07-16 RO RO148016A patent/RO109338B1/ro unknown
- 1991-07-17 BG BG94837A patent/BG60593B1/bg unknown
- 1991-07-17 DE DE69114198T patent/DE69114198T2/de not_active Expired - Fee Related
- 1991-07-17 DK DK91111948.5T patent/DK0467331T3/da active
- 1991-07-17 AT AT91111948T patent/ATE129715T1/de not_active IP Right Cessation
- 1991-07-17 ES ES91111948T patent/ES2081397T3/es not_active Expired - Lifetime
- 1991-07-17 EP EP91111948A patent/EP0467331B1/en not_active Expired - Lifetime
- 1991-07-17 RU SU915001127A patent/RU2045533C1/ru not_active IP Right Cessation
- 1991-07-17 UA UA5001127A patent/UA27105A1/uk unknown
- 1991-07-18 HU HU9802439A patent/HU221803B1/hu not_active IP Right Cessation
- 1991-07-18 HU HU9202619A patent/HU215158B/hu unknown
- 1991-07-18 CN CN91104907A patent/CN1029738C/zh not_active Expired - Fee Related
- 1991-07-18 JP JP3178514A patent/JP2657132B2/ja not_active Expired - Fee Related
- 1991-07-18 US US07/731,781 patent/US5250518A/en not_active Expired - Lifetime
- 1991-07-18 HU HU912408A patent/HUT59935A/hu unknown
- 1991-07-18 PL PL91291130A patent/PL166379B1/pl not_active IP Right Cessation
1992
- 1992-09-25 HR HRP-1409/90A patent/HRP920491B1/xx not_active IP Right Cessation
1995
- 1995-07-03 HU HU95P/P00748P patent/HU211659A9/hu unknown
- 1995-12-07 GR GR950403439T patent/GR3018330T3/el unknown

Also Published As

Publication number	Publication date
HU9202619D0 (en)	1992-12-28
CN1059728A (zh)	1992-03-25
CN1029738C (zh)	1995-09-13
HU221803B1 (hu)	2003-01-28
DE69114198T2 (de)	1996-06-27
PL166379B1 (en)	1995-05-31
CA2046956A1 (en)	1992-01-19
JP2657132B2 (ja)	1997-09-24
GR3018330T3 (en)	1996-03-31
JPH05132497A (ja)	1993-05-28
EP0467331A1 (en)	1992-01-22
CZ280640B6 (cs)	1996-03-13
SI9011409A (en)	1995-10-31
BG94837A (bg)	1993-12-24
HU211659A9 (en)	1995-12-28
HU215158B (hu)	1998-12-28
BG60593B1 (bg)	1995-09-29
PL291130A1 (en)	1992-11-16
HUT62307A (en)	1993-04-28
ES2081397T3 (es)	1996-03-01
CS219591A3 (en)	1992-03-18
HU9802439D0 (en)	1998-12-28
UA27105A1 (uk)	2000-02-28
US5250518A (en)	1993-10-05
RU2045533C1 (ru)	1995-10-10
DK0467331T3 (da)	1996-02-05
CA2046956C (en)	1999-01-05
SK279075B6 (sk)	1998-06-03
HU912408D0 (en)	1991-12-30
RO109338B1 (ro)	1995-01-30
HUT59935A (en)	1992-07-28
ATE129715T1 (de)	1995-11-15
DE69114198D1 (de)	1995-12-07
HRP920491A2 (en)	1994-08-31
EP0467331B1 (en)	1995-11-02

Legal Events

Date	Code	Title	Description
1994-08-31	A1OB	Publication of a patent application
1994-10-06	AIPI	Request for the grant of a patent on the basis of a substantive examination of a patent application
1998-10-31	B1PR	Patent granted
2007-01-15	PNAN	Change of the applicant name, address/residence	Owner name: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.,
2007-01-15	PPPP	Transfer of rights	Owner name: PLIVA-ISTRAZIVACKI INSTITUT D.O.O., HR
2007-07-13	ODRP	Renewal fee for the maintenance of a patent	Payment date: 20070713 Year of fee payment: 18
2009-01-19	PBON	Lapse due to non-payment of renewal fee	Effective date: 20080719

Publication	Publication Date	Title
HRP920491B1 (en)	1998-10-31	O-methyl derivatives of azithromycin a, process and intermediates for their preparation, and process of preparation and use thereof in the preparation of pharmaceuticals
IL89831A (en)	1992-12-01	Process for preparing derivatives of baccatine iii and of 10-deacetyl baccatine iii
DK0553202T3 (da)	1995-07-03	Fremgangsmåde til fremstilling af imidazo(4,5-c)quinolin-4-aminer
DE3270317D1 (en)	1986-05-07	Derivatives of amino acids and their therapeutic use
CA2146852A1 (en)	1994-04-28	New substituted pyrazole derivatives, processes for their preparation and their use as herbicides
FI111263B (fi)	2003-06-30	Uudet erytromysiinijohdannaiset, menetelmä niiden valmistamiseksi ja niiden käyttö lääkkeinä sekä menetelmässä käytettävät välituoteamiinit
NO890567D0 (no)	1989-02-09	Anthracyklin-derivater.
DK0722319T3 (da)	2003-04-14	Anthracyclinonderivater samt deres anvendelse ved amyloidose
CA2148595A1 (en)	1994-05-11	Molecule labelling using 2-hydrazinopyridine derivatives
ES2145772T3 (es)	2000-07-16	Uso de un complejo de ibuprofeno-beta-ciclodextrina para administracion oral.
MY132057A (en)	2007-09-28	Quinoxalinones, a process for their preparation and their use
ATE63921T1 (de)	1991-06-15	6-amino-anthracycline, verfahren zu ihrer herstellung und ihre verwendung.
DE69025505D1 (de)	1996-04-04	Tylosin-Derivate
TW350840B (en)	1999-01-21	N-acylpiperazine derivative, antibacterial drug and anti-ulcer drug
FI913699A0 (fi)	1991-08-02	Menetelmä farmaseuttisesti käyttökelpoisten 4'-epi-4'-aminoantrasykliinien valmistamiseksi sekä menetelmässä käytettävät välituotteet
CZ281393B6 (cs)	1996-09-11	Způsob výroby 6-(substituovaných amino)-propionyl derivátů forskolinu
EP0068033A4 (en)	1983-07-04	N-(4-phenyl-2-thiazolyl)carbamate derivatives, process for their preparation, and medicinal composition containing same.
PT86702A (pt)	1988-03-01	Process for preparing substituted methanesulphonamidophenethylamines
DK0424248T3 (da)	1996-03-04	20,21-dinoreburnamein med substitution i 15-stillingen, fremgangsmåde til deres fremstilling samt mellemprodukter til brug derved, deres anvendelse som lægemidler og præparater med indhold deraf
MY115291A (en)	2003-05-31	New substituted pyrazole derivatives, processes for their preparation nad their use as herbicides
HUT50127A (en)	1989-12-28	Process for producing compounds of antiarrythmic activity and pharmaceutical compositions containing
PT84061A (en)	1987-02-01	Process for the preparation of monosulfactams
SE8305231D0 (sv)	1983-09-28	Aminoglycoside derivatives, processes for their production and their use
HUT57718A (en)	1991-12-30	Process for producing thiourea derivative
MX9802933A (es)	1998-11-29	Derivados novedosos de amina de 2", 3"-didesoxiglicosidos de epipodofilotoxina, metodo de preparacion de los mismos y uso de los mismos con un farmaco y para tratamientos anticancer.