GB1447462A – Alpha-thiolincosaminides and the preparation thereof
– Google Patents
GB1447462A – Alpha-thiolincosaminides and the preparation thereof
– Google Patents
Alpha-thiolincosaminides and the preparation thereof
Info
Publication number
GB1447462A
GB1447462A
GB700174A
GB700174A
GB1447462A
GB 1447462 A
GB1447462 A
GB 1447462A
GB 700174 A
GB700174 A
GB 700174A
GB 700174 A
GB700174 A
GB 700174A
GB 1447462 A
GB1447462 A
GB 1447462A
Authority
GB
United Kingdom
Prior art keywords
hydrogen
alkyl
formula
carboxacyl
thiolincosaminides
Prior art date
1973-03-06
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
Application number
GB700174A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pharmacia and Upjohn Co
Original Assignee
Upjohn Co
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.)
1973-03-06
Filing date
1974-02-15
Publication date
1976-08-25
1974-02-15
Application filed by Upjohn Co
filed
Critical
Upjohn Co
1976-08-25
Publication of GB1447462A
publication
Critical
patent/GB1447462A/en
Status
Expired
legal-status
Critical
Current
Links
Espacenet
Global Dossier
Discuss
Classifications
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
C—CHEMISTRY; METALLURGY
C07—ORGANIC CHEMISTRY
C07D—HETEROCYCLIC COMPOUNDS
C07D327/00—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
C07D327/02—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
C07D327/04—Five-membered rings
C—CHEMISTRY; METALLURGY
C07—ORGANIC CHEMISTRY
C07D—HETEROCYCLIC COMPOUNDS
C07D327/00—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
C07D327/02—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
C07D327/06—Six-membered rings
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
Abstract
1447462 Thiolincosaminides UPJOHN CO 15 Feb 1974 [6 March 1973] 7001/74 Heading C2C Novel compounds (I) wherein either R 1 and R 2 are taken independently and R 1 is hydrogen and R 2 is AcNH- wherein Ac is carboxacyl or an acyl radical of the formula wherein Z is hydrogen, alkyl or a protective group removable by hydrogenolysis and R 5 is alkyl; or R 1 and R 2 are taken together and are a divalent group of the formula wherein Z and R 5 are as defined above; when R 1 and R 2 are taken together, R 3 is hydrogen, and when R 1 and R 2 are taken independantly, R 3 is a monovalent thio group in the 7(S)- position of the formula wherein A is hydrogen or hydroxyl, either B is hydrogen in which case n is zero or 1, or B is hydroxyalkyl in which case n is zero, X is oxygen or sulphur with the proviso that it is not sulphur if Ac is carboxacyl (and R 1 and R 2 are taken together), and D is an acyl radical derived from a hydrocarbon carboxylic acid; R 4 is alkyl and Y is hydrogen or carboxacyl, are made by reacting an alkyl N-acyl-6,7-aziridino- 6-deamino-7-deoxy-α-thiolincosaminide with a carboxylic acid and a cyclic sulphur compound of formula to give (I) where R 3 is said monovalent thio group; compounds (I) where R 1 and R 2 together signify said divalent group are made by acylating aziridino thiolincosaminides. The invention also comprises processes for converting the products (I) into lincomycin derivatives. Pharmaceutical preparations contain (I) where Y is H as active ingredient.
GB700174A
1973-03-06
1974-02-15
Alpha-thiolincosaminides and the preparation thereof
Expired
GB1447462A
(en)
Applications Claiming Priority (1)
Application Number
Priority Date
Filing Date
Title
US338459A
US3870699A
(en)
1973-03-06
1973-03-06
Lincomycin analogs
Publications (1)
Publication Number
Publication Date
GB1447462A
true
GB1447462A
(en)
1976-08-25
Family
ID=23324898
Family Applications (1)
Application Number
Title
Priority Date
Filing Date
GB700174A
Expired
GB1447462A
(en)
1973-03-06
1974-02-15
Alpha-thiolincosaminides and the preparation thereof
Country Status (15)
Country
Link
US
(2)
US3870699A
(en)
JP
(1)
JPS5857439B2
(en)
BE
(1)
BE811931A
(en)
CA
(1)
CA1020938A
(en)
CH
(1)
CH617440A5
(en)
CS
(1)
CS195677B2
(en)
FR
(1)
FR2220252B1
(en)
GB
(1)
GB1447462A
(en)
HU
(2)
HU170910B
(en)
NL
(1)
NL7402239A
(en)
PL
(4)
PL101373B1
(en)
SE
(2)
SE420098B
(en)
SU
(1)
SU944506A3
(en)
YU
(1)
YU36744B
(en)
ZA
(1)
ZA74935B
(en)
Families Citing this family (12)
* Cited by examiner, † Cited by third party
Publication number
Priority date
Publication date
Assignee
Title
JPH01280176A
(en)
*
1988-04-30
1989-11-10
Sekisui Plastics Co Ltd
Drilling of concrete structure
ES2243763T3
(en)
*
2001-08-28
2005-12-01
Pharmacia Corporation
CRYSTALINE CLINDAMYCIN FREE BASE.
MXPA05001689A
(en)
*
2002-08-15
2005-05-27
Vicuron Pharm Inc
Lincomycin derivatives possessing antibacterial activity.
US7199105B2
(en)
*
2002-08-15
2007-04-03
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
JP5064237B2
(en)
2005-12-09
2012-10-31
Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社
Lincomycin derivatives and antibacterial agents containing the same as active ingredients
TWI499414B
(en)
*
2006-09-29
2015-09-11
Lexicon Pharmaceuticals Inc
Inhibitors of sodium glucose co-transporter 2 and methods of their use
WO2008146919A1
(en)
2007-05-31
2008-12-04
Meiji Seika Kaisha, Ltd.
Lincosamide derivative, and antibacterial agent comprising the same as active ingredient
WO2008146917A1
(en)
*
2007-05-31
2008-12-04
Meiji Seika Kaisha, Ltd.
Lincomycin derivatives and antibacterial agents containing the same as the active ingredient
TWI472521B
(en)
*
2008-07-17
2015-02-11
Lexicon Pharmaceuticals Inc
Solid forms of (2s,3r,4r,5s,6r)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2h-pyran-3,4,5-triol and methods of their use
Family Cites Families (3)
* Cited by examiner, † Cited by third party
Publication number
Priority date
Publication date
Assignee
Title
US3271385A
(en)
*
1964-04-13
1966-09-06
Upjohn Co
Carbamoyl derivatives of lincomycin and processes for producing them
US3702322A
(en)
*
1970-04-06
1972-11-07
Upjohn Co
Derivatives of lincomycin and its analogs and process
US3689474A
(en)
*
1970-08-04
1972-09-05
Upjohn Co
7-mercapto-7-deoxylincomycins and process for preparing the same
1973
1973-03-06
US
US338459A
patent/US3870699A/en
not_active
Expired – Lifetime
1974
1974-02-07
CA
CA191,996A
patent/CA1020938A/en
not_active
Expired
1974-02-12
ZA
ZA740935A
patent/ZA74935B/en
unknown
1974-02-15
GB
GB700174A
patent/GB1447462A/en
not_active
Expired
1974-02-19
NL
NL7402239A
patent/NL7402239A/xx
not_active
Application Discontinuation
1974-03-01
JP
JP49023475A
patent/JPS5857439B2/en
not_active
Expired
1974-03-04
SE
SE7402842A
patent/SE420098B/en
unknown
1974-03-05
SU
SU742003195A
patent/SU944506A3/en
active
1974-03-05
YU
YU0582/74A
patent/YU36744B/en
unknown
1974-03-05
FR
FR7407423A
patent/FR2220252B1/fr
not_active
Expired
1974-03-05
HU
HU74UO00000100A
patent/HU170910B/en
unknown
1974-03-05
CS
CS741577A
patent/CS195677B2/en
unknown
1974-03-06
CH
CH316074A
patent/CH617440A5/de
not_active
IP Right Cessation
1974-03-06
BE
BE141690A
patent/BE811931A/en
not_active
IP Right Cessation
1974-03-06
PL
PL1974169322A
patent/PL101373B1/en
unknown
1974-03-06
PL
PL1974196623A
patent/PL102862B1/en
unknown
1974-03-06
PL
PL1974196625A
patent/PL102863B1/en
unknown
1974-03-06
PL
PL1974196622A
patent/PL102355B1/en
unknown
1974-03-09
HU
HUUO104A
patent/HU170525B/hu
unknown
1976
1976-10-08
US
US05/730,835
patent/USRE29558E/en
not_active
Expired – Lifetime
1977
1977-10-27
SE
SE7712151A
patent/SE435625B/en
unknown
Also Published As
Publication number
Publication date
JPS5857439B2
(en)
1983-12-20
CH617440A5
(en)
1980-05-30
PL102862B1
(en)
1979-04-30
AU6569774A
(en)
1975-08-21
SU944506A3
(en)
1982-07-15
PL102355B1
(en)
1979-03-31
BE811931A
(en)
1974-09-06
FR2220252A1
(en)
1974-10-04
HU170525B
(en)
1977-06-28
SE435625B
(en)
1984-10-08
FR2220252B1
(en)
1977-11-10
US3870699A
(en)
1975-03-11
PL101373B1
(en)
1978-12-30
NL7402239A
(en)
1974-09-10
PL102863B1
(en)
1979-04-30
JPS49134617A
(en)
1974-12-25
CS195677B2
(en)
1980-02-29
CA1020938A
(en)
1977-11-15
SE7712151L
(en)
1977-10-27
USRE29558E
(en)
1978-02-28
ZA74935B
(en)
1974-12-24
YU58274A
(en)
1982-02-25
YU36744B
(en)
1984-08-31
SE420098B
(en)
1981-09-14
HU170910B
(en)
1977-09-28
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Legal Events
Date
Code
Title
Description
1977-01-06
PS
Patent sealed [section 19, patents act 1949]
1986-10-08
PCNP
Patent ceased through non-payment of renewal fee
