WO2005012320A3 - Novel lincomycin derivatives possessing antimicrobial activity - Google Patents

Novel lincomycin derivatives possessing antimicrobial activity Download PDF

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Publication number
WO2005012320A3
WO2005012320A3 PCT/US2004/019689 US2004019689W WO2005012320A3 WO 2005012320 A3 WO2005012320 A3 WO 2005012320A3 US 2004019689 W US2004019689 W US 2004019689W WO 2005012320 A3 WO2005012320 A3 WO 2005012320A3
Authority
WO
WIPO (PCT)
Prior art keywords
lincomycin derivatives
antimicrobial activity
derivatives possessing
novel
possessing antimicrobial
Prior art date
Application number
PCT/US2004/019689
Other languages
French (fr)
Other versions
WO2005012320A2 (en
Inventor
Jason G Lewis
Sampath K Anandan
Hardwin O'dowd
Mikhail F Gordeev
Original Assignee
Vicuron Pharm Inc
Jason G Lewis
Sampath K Anandan
Hardwin O'dowd
Mikhail F Gordeev
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 US10/642,807 external-priority patent/US7164011B2/en
Priority claimed from US10/777,455 external-priority patent/US7199105B2/en
Priority to BRPI0411534-1A priority Critical patent/BRPI0411534A/en
Priority to CA002528592A priority patent/CA2528592A1/en
Priority to CN2004800203015A priority patent/CN1823083B/en
Priority to YUP-2005/0931A priority patent/RS20050931A/en
Priority to MXPA05013915A priority patent/MXPA05013915A/en
Priority to AU2004261550A priority patent/AU2004261550A1/en
Application filed by Vicuron Pharm Inc, Jason G Lewis, Sampath K Anandan, Hardwin O'dowd, Mikhail F Gordeev filed Critical Vicuron Pharm Inc
Priority to EP04776816A priority patent/EP1644393A2/en
Priority to EA200501830A priority patent/EA200501830A1/en
Priority to JP2006517464A priority patent/JP2007516172A/en
Publication of WO2005012320A2 publication Critical patent/WO2005012320A2/en
Publication of WO2005012320A3 publication Critical patent/WO2005012320A3/en
Priority to IL172183A priority patent/IL172183A0/en
Priority to IS8147A priority patent/IS8147A/en
Priority to NO20055893A priority patent/NO20055893L/en
Priority to TNP2005000322A priority patent/TNSN05322A1/en
Priority to HK06110528.4A priority patent/HK1090061A1/en

Links

Classifications

    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/14—Acyclic radicals, not substituted by cyclic structures attached to a sulfur, selenium or tellurium atom of a saccharide radical
    • C07H15/16—Lincomycin; Derivatives thereof

Abstract

Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. The compounds of the subject invention may exhibit potent activities against bacteria, including gram positive organisms, and may be useful antimicrobial agents. Methods of synthesis and of use the compounds are also disclosed.
PCT/US2004/019689 2003-06-17 2004-06-17 Novel lincomycin derivatives possessing antimicrobial activity WO2005012320A2 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
EA200501830A EA200501830A1 (en) 2003-06-17 2004-06-17 NEW LINCOMYCIN DERIVATIVES WITH ANTIMICROBIAL ACTIVITY
JP2006517464A JP2007516172A (en) 2003-06-17 2004-06-17 Novel lincomycin derivatives with antibacterial activity
CA002528592A CA2528592A1 (en) 2003-06-17 2004-06-17 Novel lincomycin derivatives possessing antimicrobial activity
CN2004800203015A CN1823083B (en) 2003-06-17 2004-06-17 Lincomycin derivatives possessing antibacterial activity
YUP-2005/0931A RS20050931A (en) 2003-06-17 2004-06-17 Novel lincomycin derivatives possessing antimicro bial activity
MXPA05013915A MXPA05013915A (en) 2003-06-17 2004-06-17 Novel lincomycin derivatives possessing antimicrobial activity.
AU2004261550A AU2004261550A1 (en) 2003-06-17 2004-06-17 Novel lincomycin derivatives possessing antimicrobial activity
BRPI0411534-1A BRPI0411534A (en) 2003-06-17 2004-06-17 lincomycin derivatives with antimicrobial activity
EP04776816A EP1644393A2 (en) 2003-06-17 2004-06-17 Novel lincomycin derivatives possessing antimicrobial activity
IS8147A IS8147A (en) 2003-06-17 2005-11-24 New lincomycin derivatives possessing antimicrobial activity
IL172183A IL172183A0 (en) 2003-06-17 2005-11-24 Novel lincomycin derivatives possessing antimicrobial activity
NO20055893A NO20055893L (en) 2003-06-17 2005-12-12 New linkomycin derivatives with antimicrobial activity
TNP2005000322A TNSN05322A1 (en) 2003-06-17 2005-12-16 NEW LINCOMYCIN DERIVATIVES WITH ANTIMICROBIAL ACTIVITY
HK06110528.4A HK1090061A1 (en) 2003-06-17 2006-09-21 Novel lincomycin derivatives possessing antimicrobial activity

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US47929603P 2003-06-17 2003-06-17
US47950203P 2003-06-17 2003-06-17
US60/479,502 2003-06-17
US60/479,296 2003-06-17
US10/642,807 2003-08-15
US10/642,807 US7164011B2 (en) 2002-08-15 2003-08-15 Lincomycin derivatives possessing antibacterial activity
US10/777,455 US7199105B2 (en) 2002-08-15 2004-02-11 Lincomycin derivatives possessing antibacterial activity
US10/777,455 2004-02-11

Publications (2)

Publication Number Publication Date
WO2005012320A2 WO2005012320A2 (en) 2005-02-10
WO2005012320A3 true WO2005012320A3 (en) 2005-10-20

Family

ID=40203032

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/019689 WO2005012320A2 (en) 2003-06-17 2004-06-17 Novel lincomycin derivatives possessing antimicrobial activity

Country Status (17)

Country Link
EP (1) EP1644393A2 (en)
JP (1) JP2007516172A (en)
KR (1) KR20060091050A (en)
AU (1) AU2004261550A1 (en)
BR (1) BRPI0411534A (en)
CA (1) CA2528592A1 (en)
EC (1) ECSP056233A (en)
GE (1) GEP20084437B (en)
HK (1) HK1090061A1 (en)
IL (1) IL172183A0 (en)
IS (1) IS8147A (en)
MA (1) MA27860A1 (en)
MX (1) MXPA05013915A (en)
NO (1) NO20055893L (en)
OA (1) OA13179A (en)
RS (1) RS20050931A (en)
WO (1) WO2005012320A2 (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1315859C (en) 2002-08-15 2007-05-16 维库罗恩医药品公司 Lincomycin derivatives possessing antibacterial activity
US7199105B2 (en) 2002-08-15 2007-04-03 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity
WO2005007665A2 (en) * 2003-06-17 2005-01-27 Vicuron Pharmaceuticals Inc. Lincomycin derivatives possessing antibacterial activity
US7199106B2 (en) 2003-06-17 2007-04-03 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antimicrobial activity
US7256177B2 (en) 2003-06-17 2007-08-14 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity
US7361743B2 (en) * 2004-02-11 2008-04-22 Pfizer Inc Lincomycin derivatives possessing antibacterial activity
AU2006285043A1 (en) * 2005-08-31 2007-03-08 Wyeth 9-aminocarbonylsubstituted derivatives of glycylcyclines
WO2007066805A1 (en) 2005-12-09 2007-06-14 Meiji Seika Kaisha, Ltd. Lincomycin derivative and antibacterial agent containing the same as active ingredient
EP2151447A4 (en) 2007-05-31 2012-09-05 Meiji Seika Kaisha Lincomycin derivatives and antibacterial agents containing the same as the active ingredient
WO2008146919A1 (en) 2007-05-31 2008-12-04 Meiji Seika Kaisha, Ltd. Lincosamide derivative, and antibacterial agent comprising the same as active ingredient
US20130267699A1 (en) 2011-06-24 2013-10-10 California Institute Of Technology Quaternary heteroatom containing compounds
US8822679B2 (en) * 2011-06-24 2014-09-02 California Institute Of Technology Quaternary heteroatom containing compounds
US10421696B2 (en) 2014-12-18 2019-09-24 California Institute Of Technology Enantioselective synthesis of α-quaternary mannich adducts by palladium-catalyzed allylic alkylation
CA2981041C (en) 2015-03-27 2023-09-05 California Institute Of Technology Asymmetric catalytic decarboxylative alkyl alkylation using low catalyst concentrations and a robust precatalyst
WO2017156239A1 (en) 2016-03-11 2017-09-14 California Institute Of Technology Compositions and methods for acylating lactams
EP3480190B1 (en) 2017-11-01 2023-01-04 California Institute of Technology Methods for enantioselective allylic alkylation of esters, lactones, and lactams with unactivated allylic alcohols
EP3699173A1 (en) 2018-10-18 2020-08-26 California Institute of Technology Gem-disubstituted pyrrolidines, piperazines, and diazepanes, and compositions and methods of making the same
CN110357839A (en) * 2019-08-29 2019-10-22 重庆经致制药技术开发有限公司 The preparation method of Bu Waxitan chiral intermediate

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3268556A (en) * 1964-04-13 1966-08-23 Upjohn Co Novel lincomycin derivatives
US3282917A (en) * 1964-08-17 1966-11-01 Upjohn Co Methyl n-(1-alkyl-4-alkoxy-prolyl)-alpha-thiolincosaminide compounds and process therefor
US3361739A (en) * 1964-07-01 1968-01-02 Upjohn Co Lincomycin derivatives and processes for preparing the same
US3364197A (en) * 1964-04-13 1968-01-16 Upjohn Co 2-hydroxyethyl 6, 8-dideoxy-6-(4-substituted-1-2-pyrrolidinecarboxamido)-7-o-methyl-1-thio-d-erythro-alpha-d-galacto-octopyranosides and process for producing them
US3496163A (en) * 1965-02-08 1970-02-17 Upjohn Co 7-halo-7-deoxylincomycins and process for preparing the same
US3539689A (en) * 1965-02-08 1970-11-10 Upjohn Co 7-halo-lincomycin composition and process of treatment
US3549615A (en) * 1968-10-17 1970-12-22 Upjohn Co Lincomycin derivatives and process for producing the same
US3555007A (en) * 1968-07-22 1971-01-12 Upjohn Co 7-deoxy-7-halo lincomycin d derivatives
GB1298295A (en) * 1970-04-20 1972-11-29 Upjohn Co Improvements in or relating to antibiotic derivatives and the preparation thereof
GB1347598A (en) * 1971-06-23 1974-02-27 Upjohn Co Lincomycin derivatives and the manufacture thereof
US3849396A (en) * 1973-01-08 1974-11-19 Upjohn Co Lincomycin and clindamycin 1-o-ethers
US4278789A (en) * 1979-11-23 1981-07-14 The Upjohn Company Lincomycin compounds
WO2004016632A2 (en) * 2002-08-15 2004-02-26 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3923602A (en) * 1973-10-25 1975-12-02 Upjohn Co Composition of matter and process
JPS5641239A (en) * 1979-09-13 1981-04-17 Hitachi Cable Ltd Flame-retardant composition
BRPI0411537A (en) * 2003-06-17 2006-08-01 Vicuron Pharm Inc lincomycin derivatives that have antibacterial activity

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3364197A (en) * 1964-04-13 1968-01-16 Upjohn Co 2-hydroxyethyl 6, 8-dideoxy-6-(4-substituted-1-2-pyrrolidinecarboxamido)-7-o-methyl-1-thio-d-erythro-alpha-d-galacto-octopyranosides and process for producing them
US3268556A (en) * 1964-04-13 1966-08-23 Upjohn Co Novel lincomycin derivatives
US3361739A (en) * 1964-07-01 1968-01-02 Upjohn Co Lincomycin derivatives and processes for preparing the same
US3282917A (en) * 1964-08-17 1966-11-01 Upjohn Co Methyl n-(1-alkyl-4-alkoxy-prolyl)-alpha-thiolincosaminide compounds and process therefor
US3496163A (en) * 1965-02-08 1970-02-17 Upjohn Co 7-halo-7-deoxylincomycins and process for preparing the same
US3539689A (en) * 1965-02-08 1970-11-10 Upjohn Co 7-halo-lincomycin composition and process of treatment
US3555007A (en) * 1968-07-22 1971-01-12 Upjohn Co 7-deoxy-7-halo lincomycin d derivatives
US3549615A (en) * 1968-10-17 1970-12-22 Upjohn Co Lincomycin derivatives and process for producing the same
GB1298295A (en) * 1970-04-20 1972-11-29 Upjohn Co Improvements in or relating to antibiotic derivatives and the preparation thereof
GB1347598A (en) * 1971-06-23 1974-02-27 Upjohn Co Lincomycin derivatives and the manufacture thereof
US3849396A (en) * 1973-01-08 1974-11-19 Upjohn Co Lincomycin and clindamycin 1-o-ethers
US4278789A (en) * 1979-11-23 1981-07-14 The Upjohn Company Lincomycin compounds
WO2004016632A2 (en) * 2002-08-15 2004-02-26 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BANNISTER B ET AL: "THE S-ALKYLATION OF SULPHIDES BY AN ACTIVATED CARBOHYDRATE EPIMINE UNDER ACIDIC CATALYSIS: THE FORMATION OF ALPHA-ACETAMIDO-SULPHIDES. PART 5. THE INTRODUCTION OF FUNCTIONALITY INTO THE SULPHIDE SUBSTITUENT", JOURNAL OF CHEMICAL RESEARCH. SYNOPSES, LONDON, GB, no. 4, 1989, pages 90 - 91, XP009044906, ISSN: 0308-2342 *
BANNISTER B: "THE S-ALKYLATION OF SULPHIDES BY AN ACTIVATED CARBOHYDRATE EPIMINE UNDER ACIDIC CATALYSIS: THE FORMATION OF ALPHA-ACETAMIDO-SULPHIDES. PART 4. REACTIONS WITH DITHIOACETALS AND MONOTHIOACETALS", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 1, CHEMICAL SOCIETY. LETCHWORTH, GB, no. 2, 1980, pages 540 - 552, XP009047301, ISSN: 0300-922X *
BIRKENMEYER R D ET AL: "Synthesis and antimicrobial activity of clindamycin analogues: pirlimycin, a potent antibacterial agent", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 27, no. 2, 1984, pages 216 - 223, XP002174848, ISSN: 0022-2623 *

Also Published As

Publication number Publication date
RS20050931A (en) 2008-04-04
OA13179A (en) 2006-12-13
IL172183A0 (en) 2011-08-01
WO2005012320A2 (en) 2005-02-10
NO20055893L (en) 2006-03-14
AU2004261550A1 (en) 2005-02-10
ECSP056233A (en) 2006-04-19
GEP20084437B (en) 2008-07-25
MA27860A1 (en) 2006-04-03
HK1090061A1 (en) 2006-12-15
BRPI0411534A (en) 2006-08-22
JP2007516172A (en) 2007-06-21
EP1644393A2 (en) 2006-04-12
IS8147A (en) 2005-11-24
CA2528592A1 (en) 2005-02-10
MXPA05013915A (en) 2006-07-03
KR20060091050A (en) 2006-08-17

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