HRP970473B1 - 6-o-supstituirani ketolidi antibakterijskog djelovanja - Google Patents
6-o-supstituirani ketolidi antibakterijskog djelovanjaInfo
- Publication number
- HRP970473B1 HRP970473B1 HR970473A HRP970473A HRP970473B1 HR P970473 B1 HRP970473 B1 HR P970473B1 HR 970473 A HR970473 A HR 970473A HR P970473 A HRP970473 A HR P970473A HR P970473 B1 HRP970473 B1 HR P970473B1
- Authority
- HR
- Croatia
- Prior art keywords
- substituted
- alkyl
- aryl
- heteroaryl
- group
- Prior art date
Links
- 230000000844 anti-bacterial effect Effects 0.000 title 1
- 239000003835 ketolide antibiotic agent Substances 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 14
- 125000003118 aryl group Chemical group 0.000 abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000003107 substituted aryl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Saccharide Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Cephalosporin Compounds (AREA)
- Food Preservation Except Freezing, Refrigeration, And Drying (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Spoj formuleili njegova farmaceutski prihvatljivasol, naznačen time, daRc predstavlja vodik ili hidroksi zaštitnu skupinu; L predstavlja metilen ilikarbonil, uz uvjet da kada je L metilen, T je -O-,T je izabran iz skupine koja se sastoji od -O-, -NH- i -N(W-Rd)-, gdje je W odsutan ili izabran iz skupine koja se sastoji od -O-, -NH-CO-, -N=CH- i -NH-; te Rd je izabran iz skupine koju čine (1) vodik (2) C1-C6-alkil po izboru supstituiran s jednim ili više supstituenata izabranih iz skupine kojučine (a) aril, (b) supstituirani aril, (c) heteroaril, (d) supstituirani heteroaril, (e) hidroksi, (f) C1-C6-alkoksi, (g) NR7R8 gdje su R7 i R8 zasebno izabrani između vodika i C1-C6-alkil ili se R7 i R8 uzimaju zajedno s atomom dušika na kojeg su vezani dajući 3- do 7- člani prsten koji u slučaju kada je prsten 5- do 7- člani može po izboru sadržavati hetero funkciju izabranu iz skupine koju čine -O-, -NH-, -N(C1-C6-aIkil-)-, -N(aril)-, -N(aril- C1-C6-alkil)-, -N(supstituirani aril-C1-C6-alkil)-, -N(heteroaril), -N(heteroaril- C1-C6-alkil), -N-(supstituirani heteroaril- C1-C6-alki)l i -S- ili -S(O)n-gdje je n 1 ili 2, te (h) -CH2-M-R9gdje je M izabran iz skupine koju čine (i) -C(O)-NH-, (ii) -NH-C(O)-, (iii) -NH-, (iv)-N= (v)-N(CH3)-, (vi) -NH-C(O)-O-, (vii) -NH-C(O)-NH-, (viii) -O-C(O)-NH-, (ix) -O-C(O)-O-, (x)-O-, (xi)-S(O)n-gdje je n0, 1 ili 2, (xii)-C(O)-O-, (xiii) -O-C(O)-, te (xiv) -C(O)-, teR9 je izabran iz skupine koju čine (i) C1-C6-alkil, po izboru supstituiran sa supstituentom izabranim iz skupine koju čine (aa) aril, (bb) supstituirani aril, (cc) heteroaril, te (dd) supstituirani hetereoaril, (ii) aril (iii) supstituirani aril, (iv) heteroaril, (v) supstituirani heteroaril, te (vi) heterocikloalkil, (3) C3-C7-cikloalkil, (4) aril, (5) supstituirani aril, (6) heteroaril, te (7) supstituirani heteroaril, teR je izabran iz skupine koju čine (1) metil supstituiran udjelom izabranim iz skupine koju čine (a)-CN, (b)-F, (c) -CO2R16 gdje R16 je aril supstituiran C1-C3-alkil ili heteroaril supstituiran C1-C3alkil, (d) S(O)nR10 gdje R10 je C1-C3-alkil ili aril supstituirani C1-C3-alkil ili heteroaril supstituirani C1-C3-alkil i n = 0, 1 ili 2, (e) NHC(O)R10, (f) NHC(O)NRnR12 gdje su R11 i R12 svaki zasebno izabrani iz skupine koju čine vodik, C1-C3-alkil, C1-C3-alkil supstituiran s arilom, supstituirani aril, heteoaril ili supstituirani heteroaril, (g) aril, (h) suspstituirani aril, (i) heteroaril, te (j) supstituirani heteroaril, (2) C2-C10-alkil supstituiran s jednim ili više supstituenata izabranih iz skupine koju čine (a) halogen, (b) hidroksi, (c) C1-C3-alkoksi, (d) C1-C3-alkoksi-C1-C3-alkoksi, (e) okso, (f) -N3-, (g) -CHO, (h) -O-SO2-(supstituiran C1-C6-alkil), (i) -NRI3R14 gdje su R13 i R14 izabrani iz skupine koju čine (i) vodik, (ii) C1-C12-alkil, (iii) supstituirani C1-C12-alkil, (iv) C3-C12-alkenil, (v) supstituirani C3-C12-alkeni], (vi) C3-C12-alkinil, (vii) supstituirani C3-C12-alkinil, (viii) aril, (ix) C3-C8-cikloalkil, (x) supstituirani C3
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US70777696A | 1996-09-04 | 1996-09-04 | |
US08/888,350 US5866549A (en) | 1996-09-04 | 1997-07-03 | 6-O-substituted ketolides having antibacterial activity |
Publications (2)
Publication Number | Publication Date |
---|---|
HRP970473A2 HRP970473A2 (en) | 1998-08-31 |
HRP970473B1 true HRP970473B1 (hr) | 2007-02-28 |
Family
ID=27107953
Family Applications (5)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR970473A HRP970473B1 (hr) | 1996-09-04 | 1997-09-03 | 6-o-supstituirani ketolidi antibakterijskog djelovanja |
HRP20060277AA HRP20060277B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
HRP20060276AA HRP20060276B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
HRP20060278AA HRP20060278B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
HRP20060275AA HRP20060275B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
Family Applications After (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20060277AA HRP20060277B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
HRP20060276AA HRP20060276B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
HRP20060278AA HRP20060278B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
HRP20060275AA HRP20060275B1 (hr) | 1996-09-04 | 2006-08-11 | 6-0-supstituirani ketolidi antibakterijskog djelovanja |
Country Status (28)
Country | Link |
---|---|
US (4) | US6028181A (hr) |
EP (5) | EP1291352B1 (hr) |
JP (1) | JP4597274B2 (hr) |
KR (5) | KR20050044816A (hr) |
CN (4) | CN100460415C (hr) |
AT (5) | ATE296831T1 (hr) |
BG (1) | BG63547B1 (hr) |
BR (1) | BR9711661A (hr) |
CA (1) | CA2263972C (hr) |
CZ (1) | CZ300106B6 (hr) |
DE (5) | DE69733439T2 (hr) |
DK (5) | DK1291352T3 (hr) |
ES (5) | ES2242813T3 (hr) |
HK (1) | HK1021537A1 (hr) |
HR (5) | HRP970473B1 (hr) |
HU (1) | HU230166B1 (hr) |
ID (1) | ID19406A (hr) |
IL (1) | IL128681A0 (hr) |
NO (1) | NO314230B1 (hr) |
NZ (1) | NZ334274A (hr) |
PL (1) | PL188173B1 (hr) |
PT (5) | PT929563E (hr) |
RO (1) | RO121473B1 (hr) |
RU (1) | RU2192427C2 (hr) |
SI (1) | SI20023B (hr) |
SK (5) | SK285534B6 (hr) |
TR (1) | TR199901127T2 (hr) |
WO (1) | WO1998009978A1 (hr) |
Families Citing this family (85)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6495348B1 (en) | 1993-10-07 | 2002-12-17 | Regents Of The University Of Minnesota | Mitomycin biosynthetic gene cluster |
UA51730C2 (uk) * | 1996-09-04 | 2002-12-16 | Ебботт Лабораторіз | 6-o-заміщені кетоліди з антибактеріальною активністю, спосіб їх одержання (варіанти), фармацевтична композиція та спосіб регулювання бактеріальної інфекції у ссавців |
AP1060A (en) * | 1998-01-02 | 2002-04-23 | Pfizer Prod Inc | Novel erythromycin derivatives. |
ATE243219T1 (de) | 1998-04-24 | 2003-07-15 | Pfizer Prod Inc | 9a, 11b-dehydro derivative von 9-oxime-3-keto-6-0-methylerythromycin |
US6265202B1 (en) | 1998-06-26 | 2001-07-24 | Regents Of The University Of Minnesota | DNA encoding methymycin and pikromycin |
JP4573925B2 (ja) * | 1998-07-09 | 2010-11-04 | アベンティス・ファーマ・ソシエテ・アノニム | 新規のエリスロマイシン誘導体、その製造方法及びその薬剤としての使用 |
FR2792637B1 (fr) * | 1999-04-26 | 2001-06-01 | Hoechst Marion Roussel Inc | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
FR2780977B1 (fr) * | 1998-07-09 | 2000-09-01 | Hoechst Marion Roussel Inc | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
FR2785612A1 (fr) * | 1998-11-10 | 2000-05-12 | Hoechst Marion Roussel Inc | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
ID28286A (id) | 1998-11-03 | 2001-05-10 | Pfizer Prod Inc | Antibiotik-antibiotik makrolida baru |
JP2002539217A (ja) * | 1999-03-15 | 2002-11-19 | アボット・ラボラトリーズ | 抗菌活性を有する6−o−置換マクロライド |
US6514944B2 (en) | 1999-04-16 | 2003-02-04 | Kosan Biosciences, Inc. | Macrolide antiinfective agents |
US6451768B1 (en) | 1999-04-16 | 2002-09-17 | Kosan Biosciences, Inc. | Macrolide antiinfective agents |
US6939861B2 (en) | 1999-04-16 | 2005-09-06 | Kosan Biosciences, Inc. | Amido macrolides |
CN1241931C (zh) * | 1999-04-16 | 2006-02-15 | 高山生物科学股份有限公司 | 大环内酯抗感染药物 |
EP1181300B1 (en) * | 1999-06-07 | 2003-09-17 | Abbott Laboratories | 6-o-carbamate ketolide derivatives |
US6420535B1 (en) * | 1999-06-07 | 2002-07-16 | Abbott Laboratories | 6-O-carbamate ketolide derivatives |
US6437106B1 (en) * | 1999-06-24 | 2002-08-20 | Abbott Laboratories | Process for preparing 6-o-substituted erythromycin derivatives |
US6417366B2 (en) * | 1999-06-24 | 2002-07-09 | Abbott Laboratories | Preparation of quinoline-substituted carbonate and carbamate derivatives |
EP1101769A3 (en) | 1999-11-18 | 2001-10-24 | Pfizer Products Inc. | Nitrogen containing erythromycin derivatives |
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CA2451391A1 (en) * | 2001-07-03 | 2003-01-16 | Chiron Corporation | C12 modified erythromycin macrolides and ketolides having antibacterial activity |
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US6673774B2 (en) * | 2001-12-03 | 2004-01-06 | Enanta Pharmaceuticals, Inc. | 11-O-substituted macrolides and their descladinose derivatives |
BR0214748A (pt) | 2001-12-05 | 2004-11-23 | Ortho Mcneil Pharm Inc | Derivados 6-oacil-cetolidas de eritromicina, úteis como antibacterianos |
WO2003068790A2 (en) * | 2002-02-13 | 2003-08-21 | Abbott Laboratories | Macrolide antibacterial compounds |
US6831068B2 (en) * | 2002-02-13 | 2004-12-14 | Abbott Laboratories | Macrolide antibacterial compounds |
US20030162729A1 (en) * | 2002-02-13 | 2003-08-28 | Zhenkun Ma | Macrolides with activity against methicillin-resistant staphylococcus aureus |
IL163666A0 (en) | 2002-02-22 | 2005-12-18 | New River Pharmaceuticals Inc | Active agent delivery systems and methods for protecting and administering active agents |
US6995143B2 (en) | 2002-02-28 | 2006-02-07 | Basilea Pharmaceutica Ag | Macrolides with antibacterial activity |
US7910558B2 (en) * | 2002-05-13 | 2011-03-22 | Enanta Pharmaceuticals, Inc. | Bridged macrocyclic compounds and processes for the preparation thereof |
US6841664B2 (en) * | 2002-07-25 | 2005-01-11 | Enanra Pharmaceuticals, Inc. | 6,11-4-carbon bridged ketolides |
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WO2003102010A1 (en) * | 2002-05-31 | 2003-12-11 | Janssen Pharmaceutica N.V. | 3-descladinosyl-6-o-carbamoyl and 6-o-carbonoyl macrolide antibacterial agents |
JPWO2004078771A1 (ja) * | 2003-03-07 | 2006-06-08 | 大正製薬株式会社 | 2−フルオロ−6−o−置換ケトライド誘導体 |
ES2552682T3 (es) * | 2003-03-10 | 2015-12-01 | Merck Sharp & Dohme Corp. | Agentes antibacterianos novedosos |
CA2523541A1 (en) * | 2003-04-25 | 2004-11-11 | Chiron Corporation | Novel ketolide derivatives |
US6790835B1 (en) * | 2003-06-05 | 2004-09-14 | Enanta Pharmaceuticals, Inc. | Bicyclic macrolide derivatives |
US20040254126A1 (en) * | 2003-06-05 | 2004-12-16 | Yao-Ling Qiu | 11-12 Bicyclic erythromycin derivatives |
US20050101548A1 (en) * | 2003-09-12 | 2005-05-12 | Xiaodong Lin | Antimicrobial derivatives |
GB0327720D0 (en) * | 2003-11-28 | 2003-12-31 | Biotica Tech Ltd | Erythromycins and process for their preparation |
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WO2006024741A2 (fr) * | 2004-07-30 | 2006-03-09 | Palumed S.A. | Molecules hybrides qa ou q est une aminoquinoleine et a est un residu antibiotique, leur synthese et leurs utilisations en tant qu'agent antibacterien |
FR2874922A1 (fr) * | 2004-07-30 | 2006-03-10 | Palumed Sa | Molecules hybrides qa ou q est une aminoquinoleine et a est un residu antibiotique, leur synthese et leurs utilisations en tant qu'agent antibacterien |
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PL1836211T3 (pl) | 2004-12-21 | 2010-07-30 | Pfizer Prod Inc | Makrolidy |
US20060252710A1 (en) * | 2005-05-04 | 2006-11-09 | Guoqiang Wang | 6-11 Bridged oxime erythromycin derivatives |
US7384922B2 (en) * | 2005-05-04 | 2008-06-10 | Enanta Pharmaceuticals, Inc. | 6-11 bridged oxime erythromycin derivatives |
US7517859B2 (en) * | 2005-05-04 | 2009-04-14 | Enanta Pharmaceuticals, Inc. | Spirocyclic bicyclolides |
US8097708B2 (en) | 2006-02-07 | 2012-01-17 | Taisho Pharmaceutical Co., Ltd. | 10a-Azalide compound |
JP2010501541A (ja) | 2006-08-24 | 2010-01-21 | ウォックハート リサーチ センター | 抗菌活性を有する新規マクロライド及びケトライド |
US8293715B2 (en) | 2007-08-06 | 2012-10-23 | Taisho Pharmaceutical Co., Ltd. | 10a-Azalide compound crosslinked at 10a- and 12-positions |
WO2009039177A1 (en) * | 2007-09-17 | 2009-03-26 | Enanta Pharmaceuticals, Inc. | 6, 11-bicycloides: bridged biaryl macrolide derivatives |
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EP2214484A4 (en) * | 2007-10-25 | 2013-01-02 | Cempra Pharmaceuticals Inc | PROCESS FOR PREPARING ANTIBACTERIAL MAKROLIDE AGENTS |
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CA2793884C (en) | 2010-03-22 | 2019-09-10 | Cempra Pharmaceuticals, Inc. | Crystalline forms of a macrolide, and uses therefor |
DK2571506T3 (en) | 2010-05-20 | 2017-08-28 | Cempra Pharmaceuticals Inc | PROCEDURES FOR THE MANUFACTURE OF MACROLIDES AND KETOLIDES AND INTERMEDIATES |
US8796474B1 (en) | 2010-08-23 | 2014-08-05 | Rutgers, The State University Of New Jersey | Macrolide compounds and methods and intermediates useful for their preparation |
JP6042334B2 (ja) | 2010-09-10 | 2016-12-14 | 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 | 疾患治療のための水素結合形成フルオロケトライド |
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