56443-69-7Relevant academic research and scientific papers
Total synthesis of heliannuol B, an allelochemical from Helianthus annuus
Roy, Amalesh,Biswas, Bidyut,Sen, Prabir K.,Venkateswaran, Ramanathapuram V.
, p. 6933 - 6936 (2007)
A total synthesis of the allelochemical heliannuol B 1 is described employing ring closing metathesis to generate the central benzoxepane ring system.
Efficient and enantioselective total syntheses of heliannuols A and K
Kanematsu, Makoto,Soga, Kana,Manabe, Yuki,Morimoto, Sachie,Yoshida, Masahiro,Shishido, Kozo
experimental part, p. 4758 - 4766 (2011/07/31)
The second-generation enantioselective synthesis of heliannuol A and the first enantioselective total synthesis of heliannuol K (via two routes) have both been accomplished efficiently; (heliannuol A, nine steps and 25% yield; heliannuol K, seven steps an
(THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS
-
Page/Page column 23, (2011/04/14)
The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyloptionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms,amino, di(1-4C)alkylamino, -SO2-(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl, -NH-CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH3-O- and the linking group –Y-(CH2)n-X- wherein Y is attached to R1 and selected from a bond, -O-, -S-, -SO-, -SO2-, -CH2-O-, -CO-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, -C=C-and -C≡C-; n is an integer from 1 to 10; and X is attached to the phenylene / pyridyl group and selected from a bond, -O-, -S-, -SO-, -SO2 -, -NH, -CO-, -C=C-and -C≡C-; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH2)2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is is (3-6C)cycloalkylene-R5 or -CO-CH2-R5, wherein R5 is -OH, -PO3H2, -OPO3H2, -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO2-; or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
Pyrimidinones as Casein Kinase II (CK2) Modulators
-
Page/Page column 29, (2009/09/07)
A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE β2 ADRENERGIC RECEPTOR
-
Page/Page column 82, (2008/12/05)
The present invention provides a Compound of formula (I), wherein: R1 is a group selected from -CH2OH,-NH(CO)H; and R2 is a hydrogen atom; or R1 together with R2 form the group -NH-C(O)-CH=CH-, wherei
Studies towards the conception of new selective PPARβ/δ ligands
Ekambome Bassene, Carine,Suzenet, Franck,Hennuyer, Nathalie,Staels, Bart,Caignard, Daniel-Henri,Dacquet, Catherine,Renard, Pierre,Guillaumet, Gerald
, p. 4528 - 4532 (2007/10/03)
In order to define new PPARβ/δ ligands, SAR study on the selective PPARβ/δ activator L-165,041 led to the identification of one key functional group for selective PPARβ/δ activation. Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARβ/δ ligand GW501516, the conception of new ligands showing good affinity for PPARβ/δ is reported. Finally, synthesis and biological evaluation of pyridine analogues have shown the benefical effect of the pyridine ring on the PPARβ/δ subtype selectivity.
Selective bromination of acetophenone derivatives with bromine in methanol
Goswami, Jonalee,Goswami, Amrit
, p. 469 - 471 (2007/10/03)
Acetophenone derivatives are selectively brominated in the acetyl side-chain with bromine in methanol at 0-5° by manipulating the electron density in the aromatic ring in good yield.
4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists
-
, (2011/05/18)
PCT No. PCT/US96/20872 Sec. 371 Date Sep. 16, 1998 Sec. 102(e) Date Sep. 16, 1998 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97/23216 PCT Pub. Date Jul. 3, 1997Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
LOW MELTING NEMATIC DERIVATIVES OF PHENYL 3-METHYL-BENZOYLOXYBENZOATE.
Young,Green
, p. 7 - 9 (2007/10/13)
A series of forty-eight low melting nematogenic dialkyl derivatives of type R**3 equals CH//3 (R**1 and R**2 are n-alkyls) are presented, one of which melts to the nematic phase at 43 C. The compounds were prepared by a six-step procedure with an average yield per step of 90%.
