Francis G. Fang - Andover MA, US James E. Foy - Andover MA, US Lynn Hawkins - Concord MA, US Charles Lemelin - North Chelmsford MA, US Andre Lescarbeau - Sommerville MA, US Xiang Nu - Malden MA, US Kuo-Ming Wu - Acton MA, US
Assignee:
Eisai R & D Management Co., Ltd. - Tokyo
International Classification:
C07F 9/02
US Classification:
558166, 558172
Abstract:
The present invention provides methods for preparing TLR-4 receptor agonist E6020:and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
Reagents And Methods For The Beta-Keto Amide Synthesis Of A Synthetic Precursor To Immunological Adjuvant E6020
Bruce DeCosta - Salem NH, US Francis G. Fang - Andover MA, US James E. Foy - Andover MA, US Lynn Hawkins - Concord MA, US Charles Lemelin - North Chelmsford MA, US Xiang Niu - Malden MA, US Kuo-Ming Wu - Acton MA, US
Assignee:
Eisai R & D Management Co., Ltd.
International Classification:
C07F 9/02
US Classification:
558114, 558171
Abstract:
This invention relates to the synthesis for a precursor of E6020, compound 26, via a β-keto amide alcohol intermediate, compound 22. The synthesis reacts compound 22 with compound 25 and the resultant intermediate is oxidized to produce compound 26, the precursor to E6020. Compounds 22 and 25, and their crystalline forms, represent separate embodiments of the invention. The invention also relates to compounds of formulas (3) and (4) and processes for their preparation.
Reagents And Methods For The Beta-Keto Amide Synthesis Of A Synthetic Precursor To Immunological Adjuvant E6020
Bruce DeCosta - Salem NH, US Francis G. Fang - Andover MA, US James E. Foy - Andover MA, US Lynn Hawkins - Concord MA, US Charles Lemelin - North Chelmsford MA, US Xiang Niu - Watertown MA, US Kuo-Ming Wu - Acton MA, US
Assignee:
Eisai R&D Management Co., Ltd. - Tokyo
International Classification:
C07C 229/00
US Classification:
554109
Abstract:
This invention relates to the synthesis for a precursor of E6020, compound 26, via a β-keto amide alcohol intermediate, compound 22. The synthesis reacts compound 22 with compound 25 and the resultant intermediate is oxidized to produce compound 26, the precursor to E6020. Compounds 22 and 25, and their crystalline forms, represent separate embodiments of the invention. The invention also relates to compounds of formulas (3) and (4) and processes for their preparation.
Francis G. Fang - Andover MA, US James E. Foy - Andover MA, US Lynn Hawkins - Concord MA, US Charles Lemelin - North Chelmsford MA, US Andre Lescarbeau - Sommerville MA, US Xiang Niu - Malden MA, US Kuo-Ming Wu - Acton MA, US
Assignee:
Eisai R&D Management Co., Ltd.
International Classification:
C07F 9/02
US Classification:
558171, 558172
Abstract:
The present invention provides methods for preparing TLR-4 receptor agonist E6020:and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates useful for implementing the inventive methods.
Francis G. Fang - Andover MA, US James E. Foy - Andover MA, US Lynn Hawkins - Concord MA, US Charles Lemelin - North Chelmsford MA, US Andre Lescarbeau - Sommerville MA, US Xiang Niu - Malden MA, US Kuo-Ming Wu - Acton MA, US
Assignee:
Eisai R&D Management Co., Ltd.
International Classification:
C07C 229/00
US Classification:
554110, 554109
Abstract:
The present invention provides methods for preparing TLR-4 receptor agonist E6020:.
- Tokyo, JP James E. Foy - Andover MA, US Lynn Hawkins - Concord MA, US Charles Lemelin - North Chelmsford MA, US Andre LesCarbeau - Sommerville MA, US Xiang Niu - Malden MA, US Kuo-Ming Wu - Acton MA, US
Assignee:
Eisai R&D Management Co., Ltd. - Tokyo
International Classification:
C07D 263/14
US Classification:
548239
Abstract:
The present invention provides methods for preparing TLR-4 receptor agonist E6020:
Process For The Preparation Of Anti-Malarial Drugs
Cletus Onwuzurike Ugwuegbulam - Stevenage, GB James Edward Foy - Dresher PA
Assignee:
SmithKline Beecham p.l.c. - Brentford SmithKline Beecham Corporation - Philadelphia PA
International Classification:
C07D21516
US Classification:
546153, 514312
Abstract:
The invention relates to novel intermediates and processes for the preparation of quinoline compounds useful as anti-malarial drugs and novel intermediates useful in the process. A process for the preparation of a compound of formula (I) in which R is C alkyl; R and R are independently hydrogen, halogen, trifluoromethyl or C alkoxy; R is C alkyl; R is hydrogen or C alkyl; and R or amino which comprises reacting a compound of formula (II) in which R , R and R are as defined in formula (I) and X is a leading group with a compound of formula (III).
- Tokyo, JP James E. Foy - Andover MA, US Lynn Hawkins - Concord MA, US Charles Lemelin - North Chelmsford MA, US Andre LesCarbeau - Sommerville MA, US Xiang Niu - Malden MA, US Kuo-Ming Wu - Acton MA, US
Assignee:
Eisai R&D Management Co.. Ltd. - Tokyo
International Classification:
C07D 263/14
US Classification:
548239
Abstract:
The present invention provides methods for preparing TLR-4 receptor agonist E6020:and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
Isbn (Books And Publications)
Artistry of the Mentally Ill: A Contribution to the Psychology and Psychopathology of Configuration