181269-87-4Relevant academic research and scientific papers
Synthesis of all isomers of pulcherrimine, a bitter principle in the sea urchin ovary
Sata, Noriko U,Kuwahara, Ryuji,Murata, Yuko
, p. 115 - 118 (2002)
All eight isomers of pulcherrimine, a bitter principle of the sea urchin (Hemicentrotus pulcherrimus) ovary have been synthesized, which led to revision of the absolute stereochemistry of pulcherrimine. The synthetic pulcherrimine and the 2S isomer were highly bitter at a concentration of 1.0 mM.
ARYL HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
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Paragraph 0248-249, (2021/04/17)
A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
Substituted piperidine amide derivative, preparation method thereof, and application of derivative to pharmacy
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, (2017/08/30)
The invention relates to a substituted piperidine amide derivative as shown in a general formula (I) or a stereisomer and pharmaceutically acceptable salt thereof, a preparation method of the derivative, medicinal combination as well as application of the derivative to the aspects of local anaesthesia or analgesia. The definition of each group of the general formula (I) is consistent with that of the description. (The general formula (I) is as shown in the description).
PDD AND BPD COMPOUNDS
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, (2016/12/26)
The invention relates to pyrridinobenzodiazepines (PDDs) comprising three fused 6-7- 6–membered rings and to benzopyrridodiazecines (BPDs) comprising three fused 6-8- 6–membered rings and, in particular, to PDD or BPD dimers linked together or PDD and BPD monomers linked to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, such as anti-proliferative agents. PDDs and BPDs may be represented by formula (I): and salts or solvates thereof, wherein R2, R4-R6 and R8 are independently selected substituent groups; and either: (i) R9 and R10 together form a double bond; (ii) R9 is H and R10 is OH; or (iii) R9 is H and R10 is ORA and RA is C1-6 alkyl; wherein each of m, n, u and w may be 0 or 1; where (a) the compound is a dimer with each monomer being the same or different and being of formula (I) where one of R1, R2, R3 and R7 of the first monomer and one of R'1, R'2, R3 and R'7 of the second monomer form together a bridge having the formula –X-L-X'- linking the monomers and m + n + u + w = 1; or (b) a dimer and one of R1, R2 and R3 of the first monomer and one of R'1, R'2 and R3 of the second monomer form together a bridge having the formula –X-L-X'- linking the monomers and m = n = u = w = o; or (c) one of R1, R2, R3 and R7 has the formula: –X- L-X'-D or -(CH2)f-O-R14 and m + n + u + w = o or 1; or (d) R7 has the formula: –X-L-X'- D or -(CH2)g-O -15 and m + n + u + w = 1; and X-L-X'- is a linker group and D has the formula (II) or (III):
HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE
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, (2013/08/15)
The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
The discovery of CCR3/H1 dual antagonists with reduced hERG risk
Barton, Patrick,Brough, Steven,Evans, Richard,Luckhurst, Christopher A.,Mochel, Tobias,Perry, Matthew W. D.,Rigby, Aaron,Sanganee, Hitesh,Sisson, Adam,Springthorpe, Brian,Bahl, Ash,Bowers, Keith,Riley, Robert J.
, p. 6688 - 6693,6 (2012/12/12)
A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to del
Orthoamides and iminium salts LXXVI [1]. A further contribution to the chemistry of trialkoxyacetonitriles
Kantlehner, Willi,Vettel, Markus,Eppinger, Bernhard
, p. 373 - 388 (2012/07/14)
An improved procedure for the preparation of trimethoxyacetonitrile (3a) starting from trichlo-roacetonitrile and sodium methanolate is described. Carbanions, obtained by the action of sodium hydride on nitriles, ethyl acetate and methylketones, react with trialkoxyacetonitriles 3 to give α-imino-orthocarboxylic acid trialkylesters 12, 14 and 20, which form an equilibrium with the tautomeric enamines 13, 15 and 21. The enamines 21 react with N,N-dimethylformamide dimethylacetal (24) to give amidines 25 which are cyclized to pyridinium salts 28 and 29 on treatment with benzyl bromide and acetyl chloride, respectively. The reaction of the enaminonitrile 13a with the orthoamide derivative of phenylpropiolic acid 30 affords the pyridine-2-orthocarboxylic acid trimethylester 31. The N,O-protected 4-hydroxy-piperidine 35 can be deprotonated by means of sec-butyl lithium. The carbanions thus formed are trapped with D2O, dimethyl sulfate, phenylisocyanate, CO2, and dimethyl carbonate delivering the piperidine derivatives 37-41. The heterocyclic orthoester 43 can be prepared analogously from 35 and 3a. The piperidine derivatives 44, 46 and 47 are prepared from the N,O-protected piperidines 39 and 41.
5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE ANTIBACTERIALS
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Page/Page column 58, (2008/12/05)
The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen
QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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Page/Page column 79-82, (2008/06/13)
The invention concerns quinazoline derivatives of the Formula (I), or pharmaceutically acceptable salts thereof: I wherein each of R1, R2, R3, R4 and m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.
NEW COMPOUNDS
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Page 46, (2010/02/06)
The present invention relates to new compounds of formula I, wherein P Q X1 X2 X3 X4 X5 R R1 R2 R3 R4R5 G M1 M2 M3 m and n are defined as in formula I, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
