- NOVEL ISOINDOLINE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-α so as to effectively treat cancer and inflammatory diseases.
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Paragraph 0172-0174
(2020/01/22)
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- Nickel-Catalyzed Asymmetric Reductive Cross-Coupling between Heteroaryl Iodides and α-Chloronitriles
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A Ni-catalyzed asymmetric reductive cross-coupling of heteroaryl iodides and α-chloronitriles has been developed. This method furnishes enantioenriched α,α-disubstituted nitriles from simple organohalide building blocks. The reaction tolerates a variety of heterocyclic coupling partners, including pyridines, pyrimidines, quinolines, thiophenes, and piperidines. The reaction proceeds under mild conditions at room temperature and precludes the need to pregenerate organometallic nucleophiles.
- Kadunce, Nathaniel T.,Reisman, Sarah E.
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supporting information
p. 10480 - 10483
(2015/09/28)
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- ANTIVIRAL COMPOUNDS
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The present invention relates to a compound of formula: (I) or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing a viral infection such as HIV using the same.
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Paragraph 0189
(2013/03/26)
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- INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS
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The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved
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Page/Page column 130
(2011/10/03)
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- GSK-3BETA INHIBITOR
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For the purpose of providing a GSK-3β inhibitor containing a 2-aminopyridine compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (IA): wherein each symbol is as defined in the specification. or a salt thereof or a prodrug thereof.
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Page/Page column 25
(2011/04/13)
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- Base-catalyzed halogen dance reaction and oxidative coupling sequence as a convenient method for the preparation of dihalo-bisheteroarenes
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Figure presented A one-pot preparation of the 2,2′-dibromo-1, 1′-bisheteroarenes 3a-d from bromo-heteroarenes utilizing the sequence of the base-catalyzed halogen dance (BCHD) reaction and CuCl2-promoted oxidative coupling of the in situ formed α-lithio-β-halo-heteroarenes 2a-d provides a convenient access to precursors for the preparation of tricyclic heteroaromatic cores. The structures of 3a,b,d, 6, and 9 were confirmed by single-crystal X-ray analysis, and dibromides 3a and 3b were used for the preparation of dithieno-[2,3-b:3′,2′-d]-pyrrole 10a and its selenophene analogue 10b, respectively.
- Getmanenko, Yulia A.,Tongwa, Paul,Timofeeva, Tatiana V.,Marder, Seth R.
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supporting information; experimental part
p. 2136 - 2139
(2010/08/05)
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- Traceless solid-phase synthesis of mappicine ketone library via multiple chemoselective palladium-catalyzed reactions on benzenesulfonate linker
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We report here a solid-phase synthesis of a library of mappicine ketone, a leading antiviral compound with activity against herpes viruses and human cytomegalovirus. The synthesis is based on multiple chemoselective palladium-catalyzed reactions involving
- Tsukamoto, Hirokazu,Suzuki, Risako,Kondo, Yoshinori
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scheme or table
p. 2005 - 2010
(2009/04/10)
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- Modulation of the reactivity, stability and substrate- and enantioselectivity of an epoxidation catalyst by noncovalent dynamic attachment of a receptor functionality - Aspects on the mechanism of the Jacobsen-Katsuki epoxidation applied to a supramolecular system
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The synthesis of the components of the dynamic supramolecular hydrogen-bonded catalytic system 2 + 3 is described. The catalytic performance and substrate- and enantioselectivity of Mn(salen) catalyst 2 were investigated in the presence and absence of the Zn(porphyrin) receptor unit 3. The effects of pyridine and pyridine N-oxide donor ligands were also studied. Some aspects on the mechanism of the Jacobsen-Katsuki epoxidation, based on literature observations, are introduced as a means to analyse the behaviour of 2 and its modulation by the formation of macrocycle 1 with 3. A complete association model of the metal-free system 4 + 5 refutes the earlier assumption that macrocycle 1 is the predominant form of catalyst 2 under the standard epoxidation reaction conditions with 2 + 3. Evidence are provided that receptor-binding substrates and nonbinding substrates, respectively, are epoxidised by two different catalytic species, or two distinct distributions of species in competitive epoxidations using catalytic system 2 + 3. The two species are assigned to the endo and exo faces of the Mn(salen) catalyst in macrocycle 1, and to equivalently folded oligomeric structures with monomers 2 and 3 in adjacent positions. The Royal Society of Chemistry 2006.
- Jonsson, Stefan,Odille, Fabrice G. J.,Norrby, Per-Ola,Waernmark, Kenneth
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p. 1927 - 1948
(2008/02/03)
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- BACTERICIDE COMPOSITION AND METHOD OF CONTROLLING PLANT DISEASE
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It is to provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing as active ingredients (a) a benzoylpyridine derivative represented by the formula (I) or its salt: (wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2' is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2" is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2' and R2" may form a condensed ring containing an oxygen atom) and (b) at least one another fungicide.
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Page/Page column 12-13
(2008/06/13)
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- Discovery of trans-3,4′-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation
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A novel series of Akt/PKB inhibitors derived from a screening lead (1) has been prepared. The novel trans-3,4′-bispyridinylethylenes described herein are potent inhibitors of Akt/PKB with IC50 values in the low double-digit nanomolar range against Akt1. Compound 2q shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor to modest selectivity against closely related kinases in the AGC and CMGC families. The cellular activities including inhibition of cell growth and phosphorylation of downstream target GSK3 are also described. The X-ray structure of compound 2q complexed with PKA in the ATP binding site was determined.
- Li, Qun,Li, Tongmei,Zhu, Gui-Dong,Gong, Jianchun,Claibone, Akiyo,Dalton, Chris,Luo, Yan,Johnson, Eric F.,Shi, Yan,Liu, Xuesong,Klinghofer, Vered,Bauch, Joy L.,Marsh, Kennan C.,Bouska, Jennifer J.,Arries, Shannon,De Jong, Ron,Oltersdorf, Tilman,Stoll, Vincent S.,Jakob, Clarissa G.,Rosenberg, Saul H.,Giranda, Vincent L.
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p. 1679 - 1685
(2007/10/03)
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- 3-BENZOYL-2,4,5-SUBSTITUTED PYRIDINE DERIVATIVES OR SALTS THEREOF AND BACTERICIDES CONTAINING THE SAME
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To provide 3-benzoyl-2,4,5-substituted pyridine derivatives or their salts, fungicides containing them, and intermediates for producing them. By providing a group of compounds comprising specific 3-benzoyl-2,4,5-substituted pyridine derivatives or their s
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Page/Page column 6
(2010/02/13)
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- Heteroaryl fused azapolycyclic compounds
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The present invention provides a compound having the structure of formula I: wherein R1 is hydrogen, (C1-C6) alkyl, unconjugated (C3-C6) alkenyl, benzyl, YC(═O)(C1-C6) alkyl or —CH2CH2—O—(C1-C4) alkyl; X is CH2 or CH2CH2; Y is (C2-C6) alkylene; Z is (CH2)m, CF2, or C(═O), where m is 0, 1 or 2; R2 and R3 are selected independently from hydrogen, halogen, —(C1-C6) alkyl optionally substituted with from 1 to 7 halogen atoms, and —O(C1-C6) alkyl optionally substituted with from 1 to 7 halogen atoms, or R2 and R3 each together with the atom to which it is connected independently form C(═O), S→O, S(═O)2, or N→O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.
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- HETEROCYCLIC KINASE INHIBITORS
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Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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- A synthetic approach to 2,3,4-substituted pyridines useful as scaffolds for tripeptidomimetics
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The synthesis of 2,3,4-substituted pyridine derivatives useful as scaffolds in the development of peptidomimetics is described. The use of a variety of electrophiles in a halogen-dance reaction to produce 3-alkyl-2-fluoro-4-iodo- pyridine derivatives as 'functionalized scaffolds' and the possibility to differentiate between the reactivities of the two halogen handles have been explored. Coupling of amino acid derivatives in the 4-position of the pyridine was found to proceed efficiently by conversion of iodo-pyridine to a Grignard derivative, which was allowed to react with a protected amino aldehyde. Substitution of fluorine in the 2-position of the pyridine was found to be facile with alkoxide nucleophiles, whereas amines were much less reactive.
- Saitton, Stina,Kihlberg, Jan,Luthman, Kristina
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p. 6113 - 6120
(2007/10/03)
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- First Metalation of Aryl Iodides: Directed Ortho-Lithiation of Iodopyridines, Halogen-Dance, and Application to Synthesis
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Metalation of iodopyridines was succesfully achieved by LDA at low temperature.In many cases, lithiation is ortho directed by the iodo group which subsequently ortho-migrates very fast to give stabilized iodolithiopyridines.This procedure was applied to 2
- Rocca, P.,Cochennec, C.,Marsais, F.,Thomas-dit-Dumont, L.,Mallet, M.,et al.
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p. 7832 - 7838
(2007/10/02)
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