137641-62-4Relevant academic research and scientific papers
Substituted 5-oxo-pyrrolidine derivative, and preparation method and applications thereof
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Paragraph 0121-0123, (2019/01/21)
The invention belongs to the technical field of medicine, relates to a substituted 5-oxo-pyrrolidine derivative disclosed in generation formula I, and a preparation method and applications thereof, and more specifically relates to applications of the substituted 5-oxo-pyrrolidine derivative in preparation of anti-cerebral ischemia medicines as a nerve protective agent, and a pharmaceutical composition taking the substituted 5-oxo-pyrrolidine derivative and a pharmaceutically acceptable salt of the substituted 5-oxo-pyrrolidine derivative as active components. The pharmaceutical composition contains the substituted 5-oxo-pyrrolidine derivative and a pharmaceutical excipient and/or a diluent of the substituted 5-oxo-pyrrolidine derivative. In the general formula I, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Y, and n are defined in the patent specification and patent claims.
Transition-Metal-Free Amine Oxidation: A Chemoselective Strategy for the Late-Stage Formation of Lactams
Griffiths, Robert J.,Burley, Glenn A.,Talbot, Eric P. A.
supporting information, p. 870 - 873 (2017/02/26)
A metal-free strategy for the formation of lactams via selective oxidation of cyclic secondary and tertiary amines is described. Molecular iodine facilitates both chemoselective and regioselective oxidation of C-H bonds directly adjacent to a cyclic amine. The mild conditions, functional group tolerance, and substrate scope are demonstrated using a suite of diverse small molecule cyclic amines, including clinically approved drug scaffolds.
Pyroglutamic acid derivatives and related compounds which inhibit leukocyte adhesion mediated by VLA-4
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, (2008/06/13)
Disclosed are pyroglutamic acid derivatives and related compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflamma
STEROID SPARING AGENTS AND METHODS OF USING SAME
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Page/Page column 625, (2010/02/14)
This invention relates generally to the use of a steroid sparing agent for the preparation of a medicament for the treatment of inflammatory bowel diseases (IBD), asthma, multiple sclerosis (MS), rheumatoid arthritis (RA), graft versus host disease (GVHD), host versus graft disease, and various spondyloarthropathies, comprising administering a steroid sparing immunoglobulin or small molecule composition to a patient in need thereof. The invention also relates generally to combination therapies for the treatment of these conditions.
Pyroglutamic acid derivatives and related compounds which inhibit leukocyte adhesion mediated by VLA-4
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, (2008/06/13)
Disclosed are pyroglutamic acid derivatives and related compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflamma
Synthesis of 5S-(1-oxoalkyl and aryl)2-pyrrolidinone derivatives
Deskus, Jeffrey,Fan, Dongping,Smith, Michael B.
, p. 1649 - 1659 (2007/10/03)
N-Benzyl pyroglutamate esters react with aryllithium reagents and methyllithium to give moderate to good yields of 5-(I-oxoaryl) or 5-(I- oxoalkyl)-2-pyrrolidinone derivatives. The reaction proceeds without racemization, but is accompanied by formation of 5-(I-hydroxy- l-alkyl)-2- pyrrolidinone derivatives. This reaction gives very poor yields of ketone products with most other alkyl organolithium reagents such as n-butyllithium. Grignard reagents react to give primarily the alcohol.
A general N-alkylation procedure for ethyl pyroglutamate
Simandan, Tiberiu,Smith, Michael B.
, p. 1827 - 1838 (2007/10/03)
Despite several reported procedures for coupling alkyl halides and 5-oxoproline esters (pyroglutamate derivatives), no general method has been described. The reaction of pyrroglutamate with sodium hydride, in anhydrous THF in the presence of the halide, p
