99780-98-0Relevant academic research and scientific papers
An Efficient Two-Step Preparation of α-, β-, γ- or δ-Amino Acids from 2-Pyrazinones, 2-Hydroxypyrimidines or 2-Pyridones Respectively
Zacharie, Boulos,Abbott, Shaun D.,Baigent, Christopher B.,Doyle, Christopher,Yalagala, Ravi Shekar
, p. 6486 - 6493 (2018/11/23)
A practical and efficient two-step procedure is reported for the preparation of a variety of α-, β-, γ- and δ-amino acids from 2-pyridone, 2-pyrazinone or 2-hydroxypyrimidine and derivatives. The procedure is amenable to scale-up and in most cases no chromatographic purification of the product is required. This approach is useful, especially in the synthesis of amino acids or deuterated amino acids that are not obtained by other methods.
ACC INHIBITORS AND USES THEREOF
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Paragraph 0410, (2017/05/17)
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
Substituted Pyrrololactams via Ring Expansion of Spiro-2H-pyrroles from Intermolecular Alkyne-Isocyanide Click Reactions
George, Jimil,Kim, Hun Young,Oh, Kyungsoo
supporting information, p. 628 - 631 (2017/02/10)
The facile synthesis of 6- to 8-membered pyrrololactams has been developed using a ring expansion of spiro-2H-pyrroles, the products of intermolecular alkyne-isocyanide click reactions. The key to successful ring expansion of spiro-2H-pyrroles to pyrrololactams is the enforced orbital overlap between the internal alkene and the amide carbonyl group through the conformationally locked bicyclic structures. The newly disclosed α-isocyano lactams, substrates for click reactions, should find their utility in the synthesis of pharmaceutically important heterocyclic compounds.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
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Paragraph 0789, (2013/03/26)
The present invention provides a novel compound having a superior activity as an ERR-alpha modulator and useful as an agent for the prophylaxis or treatment of ERR-alpha associated diseases. The present invention relates to a compound represented by the formula (1) wherein each symbol is as defined in the specification, or a salt thereof
Pyrrolopyrazine Kinase Inhibitors
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, (2011/10/10)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
ANTIVIRAL COMPOUNDS
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Page/Page column 504, (2010/12/17)
The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Synthesis and evaluation of anti-apoptotic activity of L-carnitine cyclic analogues and amino acid derivatives
Fringuelli, Renata,Utrilla Navarro, M. Pilar,Milanese, Lara,Bruscoli, Stefano,Schiaffella, Fausto,Riccardi, Carlo,De Simone, Claudio
, p. 271 - 277 (2007/10/03)
Two series of derivatives were synthesised. In one series (R)-4-hydroxy-2-pyrrolidinone was used as a mimic of cyclic L-carnitine analogue and in the second series 3-amino-2-piperidinone was used as a cyclic ornithine analogue. N-Benzyloxycarbonyl derivatives of some amino acids were also prepared. The newly synthesised compounds were tested for their ability to inhibit Fas-activated apoptosis of human Jurkatt T-cell line. The results confirm the previously described anti-apoptotic activity of carnitine and indicate new carnitine and amino acid analogues (1, 3, 6, 7, 20) that inhibit Fas-induced apoptosis.
4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE - 3 - CARBOXYLIC ACID AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES
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Page 163, (2008/06/13)
Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.
Inhibitors of peptide binding to MHC class II proteins
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, (2008/06/13)
The invention concerns pharmacologically useful peptide derivatives of the formula (I): P-AA1-AA2-AA3-AA4-AA5-AA6-AA7-AA8-Q, and pharmaceutically acceptable salts thereof, wherein either AA3 together with AA4, or AA4 together with AA5, or AA6 together with AA7 form a group of formula (II): in which Ra is selected from hydrogen and (1-4C)alkyl, and the remainder of AA1, AA2, AA3, AA4, AA5, AA6, AA7, and AA8 are L-amino acid residues; P is a hydrophobic residue; and Q is OH, NH2 or NRcRd. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds, and pharmaceutical compositions containing them, in treating MHC class II dependent T-cell mediated autoimmllne or inflammatory diseases, such as rheumatoid arthritis.
Conformationally Restricted Inhibitors of Angiotensin Converting Enzyme: Synthesis and Computations
Thorsett, Eugene D.,Harris, Elbert E.,Aster, Susan D.,Peterson, Elwood R.,Snyder, James P.,et al.
, p. 251 - 260 (2007/10/02)
A series of inhibitors of angiotensin converting enzyme (ACE, dipeptidyl carboxypeptidase, EC 3.4.15.1) is described which addresses certain conformational aspects of the enzyme-inhibitor interaction.In this study the alanylproline portion of the potent A
