UY25805A1 - Azalidas de 13 miembros y su uso como agentes antibióticos. - Google Patents

Azalidas de 13 miembros y su uso como agentes antibióticos.

Info

Publication number
UY25805A1
UY25805A1 UY25805A UY25805A UY25805A1 UY 25805 A1 UY25805 A1 UY 25805A1 UY 25805 A UY25805 A UY 25805A UY 25805 A UY25805 A UY 25805A UY 25805 A1 UY25805 A1 UY 25805A1
Authority
UY
Uruguay
Prior art keywords
alkyl
pyrazolyl
methyl
compounds
alkynyl
Prior art date
Application number
UY25805A
Other languages
English (en)
Inventor
Ziegler Carl Bernard
Blize Alan Elwood
Dirlam John Philip
Bertinato Peter
Ragan Colman Brendan
Morton Barry James
Rafka Robert John
Original Assignee
Pfizer Prod Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22327457&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UY25805(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of UY25805A1 publication Critical patent/UY25805A1/es

Links

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
    • 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
    • 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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biotechnology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pyrane Compounds (AREA)

Abstract

La invención se refiere a azalidas de 13 miembros de fórmula (1), en la que: R1 es acetilo, 3-N,N-dimetilamino-2-propenoílo, 1-N-metil-5-pirazolilo, 3-pirazolilo, 1-metil-N-3-pirazolilo, 1-N-bencil-3-pirazolilo, 1-N-(3-hidroxibencil)-3-pirazolilo, 3-isoxazolilo; R2 es H o alquilo; R6 es H o metilo; cada R7 es independientemente H, alquilo, alquenilo, alquinilo, -C(O)alquilo, -C(O)alquenilo, -C(O)alquinilo, -C(O)N(H)alquilo, -SO2(O)alquilo o un grupo fosfato; R8 es H o metilo; R9 es según fig. 2 o 4''-oxocladinosilo; y R12 es alquilo, alquenilo, alquinilo, -CH2S(O)2alquilo, -CH2Oalquilo, -CH2Ndi-alquilo, -CH2(arilo) o -CH2(heteroarilo); y a sales farmacéuticamente aceptables de los mismos. Dichos compuestos son agentes antibacterianos que pueden usarse para tratar diversas infecciones bacterianas y protozoarias. La invención también se refiere a composiciones farmacéuticas que contienen a dichos compuestos, y a procedimientos de tratamiento de infecciones bacterianas y protozoarias mediante la administración de estos compuestos. La invención también se refiere a procedimientos de preparación de los compuestos de fórmula (1) y a intermedios útiles en dicha preparación.
UY25805A 1998-11-20 1999-11-17 Azalidas de 13 miembros y su uso como agentes antibióticos. UY25805A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10939998P 1998-11-20 1998-11-20

Publications (1)

Publication Number Publication Date
UY25805A1 true UY25805A1 (es) 2001-08-27

Family

ID=22327457

Family Applications (1)

Application Number Title Priority Date Filing Date
UY25805A UY25805A1 (es) 1998-11-20 1999-11-17 Azalidas de 13 miembros y su uso como agentes antibióticos.

Country Status (46)

Country Link
US (1) US6329345B1 (es)
EP (1) EP1131331B1 (es)
JP (1) JP3842973B2 (es)
KR (1) KR100477774B1 (es)
CN (2) CN101367853A (es)
AP (1) AP2001002142A0 (es)
AR (3) AR019496A1 (es)
AT (1) ATE260927T1 (es)
AU (1) AU766106B2 (es)
BG (1) BG65107B1 (es)
BR (2) BRPI9915480B8 (es)
CA (1) CA2351429C (es)
CO (1) CO5380019A1 (es)
CZ (1) CZ303099B6 (es)
DE (1) DE69915336T2 (es)
DK (1) DK1131331T3 (es)
DZ (1) DZ2944A1 (es)
EA (2) EA009729B1 (es)
EG (1) EG23823A (es)
ES (1) ES2216581T3 (es)
GT (1) GT199900198A (es)
HK (1) HK1041269A1 (es)
HR (1) HRP20010374B1 (es)
HU (1) HU229008B1 (es)
ID (1) ID28548A (es)
IL (3) IL142631A0 (es)
IS (1) IS2350B (es)
MA (1) MA26707A1 (es)
ME (1) ME00467B (es)
MY (1) MY122353A (es)
NO (3) NO319796B1 (es)
NZ (1) NZ511199A (es)
OA (1) OA11713A (es)
PA (1) PA8485601A1 (es)
PE (1) PE20001378A1 (es)
PL (1) PL198580B1 (es)
PT (1) PT1131331E (es)
RS (1) RS50302B (es)
SI (1) SI1131331T1 (es)
SK (1) SK284607B6 (es)
TN (1) TNSN99214A1 (es)
TW (2) TWI243824B (es)
UA (1) UA70972C2 (es)
UY (1) UY25805A1 (es)
WO (1) WO2000031097A1 (es)
ZA (1) ZA200104019B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HN1998000086A (es) 1997-06-11 1999-03-08 Pfizer Prod Inc Derivados de 9 - desofo - 9 aza - 9a - homoeritromicina a - c - 4 sustituidos.
AP9801420A0 (en) * 1998-01-02 1998-12-31 Pfizer Prod Inc Novel macrolides.
UA70972C2 (uk) * 1998-11-20 2004-11-15 Пфайзер Продактс Інк. 13-членні азаліди і їх застосування як антибіотиків
JP2003500414A (ja) * 1999-05-24 2003-01-07 ファイザー・プロダクツ・インク １３−メチルエリスロマイシン誘導体
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
AP2002002652A0 (en) * 2000-04-27 2002-12-31 Pfizer Prod Inc The use of azalide antibiotic composition for treating or preventing a bacterial or protozoal infection in mammals.
MXPA03009786A (es) * 2001-04-27 2004-01-29 Pfizer Prod Inc Procedimiento para preparar derivados de 9-desoxo-9a-aza-9a-homoeritromicina a 4"-sustituidos.
JP4311203B2 (ja) * 2001-08-08 2009-08-12 大正製薬株式会社 １１ａ−アザライド化合物及びその製造方法
US7601695B2 (en) * 2003-03-10 2009-10-13 Optimer Pharmaceuticals, Inc. Antibacterial agents
WO2004108744A2 (en) * 2003-05-19 2004-12-16 Prasad K Deshpande Azalides and azaketolides having antimicrobial activity
CA2546195A1 (en) * 2003-11-21 2005-06-02 Pfizer Products Inc. The use of anti biotics as vaccine adjuvants
EP1985620A4 (en) * 2006-02-07 2012-08-15 Taisho Pharmaceutical Co Ltd COMPOUND 10a-AZALIDE
US8293715B2 (en) 2007-08-06 2012-10-23 Taisho Pharmaceutical Co., Ltd. 10a-Azalide compound crosslinked at 10a- and 12-positions
US8299035B2 (en) 2008-05-15 2012-10-30 Taisho Pharmaceutucal Co., Ltd. 10a-azalide compound having 4-membered ring structure
WO2012038372A1 (en) * 2010-09-20 2012-03-29 Novartis Ag Novel process for the preparation of 9-deoxo-9a-aza- 9a-homoerythromycin a modified in the c-4'' of the cladinose ring by an epoxide group
CN102295672B (zh) * 2011-07-13 2014-06-04 武汉回盛生物科技有限公司 一种泰拉菌素的合成方法
WO2013013834A1 (en) 2011-07-27 2013-01-31 Farma Grs, D.O.O. New crystalline forms of tulathromycin
CN102786569B (zh) * 2012-09-07 2016-12-07 安徽中升药业有限公司 泰拉霉素中间体及其制备方法与泰拉霉素的制备方法
SI3027634T1 (sl) * 2013-07-31 2018-10-30 Farma Grs, D.O.O. Proces za pripravo tulatromicina
CN109748942A (zh) * 2014-05-16 2019-05-14 普莱柯生物工程股份有限公司 一种大环内酯类化合物
CN104725446B (zh) * 2015-03-26 2017-10-27 宁夏泰瑞制药股份有限公司 一种从泰拉霉素粗品中分离泰拉霉素a和泰拉霉素b的方法
EP3883647A1 (en) * 2018-11-19 2021-09-29 Zikani Therapeutics, Inc. C10-alkylene substituted 13-membered macrolides and uses thereof
US20220177508A1 (en) * 2018-11-19 2022-06-09 Zikani Therapeutics, Inc. C10-Cyclic Substituted 13-Membered Macrolides and Uses Thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
YU43116B (en) 1979-04-02 1989-04-30 Pliva Pharm & Chem Works Process for preparing 11-aza-4-o-cladinosyl-6-o-desosaminyl-15-ethyl-7,13,14-trihydroxy-3,5,7,9,12,14-hexamethyl-oxacyclopentadecane-2-one(11-aza-10-deox
SI8110592A8 (en) * 1981-03-06 1996-06-30 Pliva Pharm & Chem Works Process for preparing of n-methyl-11-aza-10-deoxo-10-dihydroerythromycine a and derivatives thereof
US4474768A (en) * 1982-07-19 1984-10-02 Pfizer Inc. N-Methyl 11-aza-10-deoxo-10-dihydro-erytromycin A, intermediates therefor
SI8611592A8 (en) * 1986-09-12 1995-04-30 Pliva Pharm & Chem Works Process for preparing complexes of N-methyl-11-aza-10-deoxo-10-dihydroeritromicine A and 11-aza-10-deoxo-10-dihydroeritromicine A with metals
US5106961A (en) 1987-05-26 1992-04-21 Eli Lilly And Company Erythromycin ring-contracted derivatives
SI9011409A (en) 1990-07-18 1995-10-31 Pliva Pharm & Chem Works O-methyl azitromycin derivates, methods and intermediates for their preparation and methods for preparation of pharmaceuticals products which comprise them
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
GB2327084A (en) * 1997-07-08 1999-01-13 Merck & Co Inc 9a-Aza-3-ketolide antibiotics
UA70972C2 (uk) * 1998-11-20 2004-11-15 Пфайзер Продактс Інк. 13-членні азаліди і їх застосування як антибіотиків

Also Published As

Publication number Publication date
IL189430A (en) 2010-05-31
IS2350B (is) 2008-04-15
HRP20010374B1 (en) 2006-09-30
BR9915480A (pt) 2001-07-31
NZ511199A (en) 2003-08-29
JP2002530422A (ja) 2002-09-17
HK1041269A1 (zh) 2002-07-05
HUP0104313A3 (en) 2003-12-29
US6329345B1 (en) 2001-12-11
NO20050893L (no) 2001-07-17
IS5918A (is) 2001-04-17
ZA200104019B (en) 2002-06-17
EP1131331B1 (en) 2004-03-03
EA009729B1 (ru) 2008-02-28
IL142631A0 (en) 2002-03-10
NO20050904L (no) 2001-07-17
PA8485601A1 (es) 2000-09-29
ME00467B (me) 2011-10-10
JP3842973B2 (ja) 2006-11-08
SI1131331T1 (en) 2004-08-31
BG65107B1 (bg) 2007-02-28
GT199900198A (es) 2001-05-11
CZ303099B6 (cs) 2012-04-04
OA11713A (en) 2005-01-25
WO2000031097A1 (en) 2000-06-02
NO330249B1 (no) 2011-03-14
AR019496A1 (es) 2002-02-20
NO319796B1 (no) 2005-09-19
SK6632001A3 (en) 2002-07-02
CN1326460A (zh) 2001-12-12
ATE260927T1 (de) 2004-03-15
HUP0104313A2 (hu) 2002-02-28
EA200400701A1 (ru) 2004-12-30
HRP20010374A2 (en) 2002-06-30
BG105600A (en) 2001-12-29
CA2351429C (en) 2005-07-12
IL189430A0 (en) 2008-06-05
TWI243824B (en) 2005-11-21
AR059524A2 (es) 2008-04-09
CZ20011754A3 (cs) 2002-03-13
EG23823A (en) 2007-09-19
NO329629B1 (no) 2010-11-22
PE20001378A1 (es) 2000-12-14
DE69915336D1 (de) 2004-04-08
DZ2944A1 (fr) 2004-03-15
PL198580B1 (pl) 2008-06-30
AU766106B2 (en) 2003-10-09
ES2216581T3 (es) 2004-10-16
NO20012464L (no) 2001-07-17
AU1068600A (en) 2000-06-13
KR20010086043A (ko) 2001-09-07
CN101367853A (zh) 2009-02-18
CA2351429A1 (en) 2000-06-02
MY122353A (en) 2006-04-29
DK1131331T3 (da) 2004-06-14
MA26707A1 (fr) 2004-12-20
TNSN99214A1 (fr) 2005-11-10
RS50302B (sr) 2009-09-08
AP2001002142A0 (en) 2001-05-09
IL142631A (en) 2010-05-31
TW200404077A (en) 2004-03-16
HU229008B1 (en) 2013-07-29
EA200100416A1 (ru) 2001-10-22
YU33401A (sh) 2004-05-12
EP1131331A1 (en) 2001-09-12
TWI243825B (en) 2005-11-21
DE69915336T2 (de) 2005-01-13
ID28548A (id) 2001-05-31
EA005156B1 (ru) 2004-12-30
BRPI9915480B1 (pt) 2015-12-29
PT1131331E (pt) 2004-06-30
NO20012464D0 (no) 2001-05-18
KR100477774B1 (ko) 2005-03-21
SK284607B6 (sk) 2005-07-01
AR059523A2 (es) 2008-04-09
BRPI9915480B8 (pt) 2022-05-10
UA70972C2 (uk) 2004-11-15
CO5380019A1 (es) 2004-03-31
PL347784A1 (en) 2002-04-22

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Legal Events

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Effective date: 20121227