- COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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The present invention provides a compound of formula (Ia) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, solid forms, combinations of pharmacologically active agents, pharmaceutical compositions and methods of using such compounds and solid forms thereof to treat or prevent parasitic diseases, for example malaria.
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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Paragraph 00906
(2020/06/19)
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- Vanadium-Catalyzed Oxidative Intramolecular Coupling of Tethered Phenols: Formation of Phenol-Dienone Products
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A mild and efficient method for the vanadium-catalyzed intramolecular coupling of tethered free phenols is described. The corresponding phenol-dienone products are prepared directly in good yields with low catalyst loadings. Electronically diverse tethered phenol precursors are well tolerated, and the catalytic method was effectively applied as the key step in syntheses of three natural products and a synthetically useful morphinan alkaloid precursor.
- Gilmartin, Philip H.,Kozlowski, Marisa C.
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p. 2914 - 2919
(2020/04/10)
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- A novel anti-Alzheimer agent inhibiting oligomerization and fibriliation of beta-amyloid protects neuronal cell from Aβ-induced cytotoxicity
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The present invention relates to development of a novel treatment agent for Alzheimerandprime;s disease, having ability of protecting neural cells and inhibiting fibrosis and oligomerization of beta-amyloid. A compound of the present invention is capable of, while maintaining therapeutic effects on Alzheimerandprime;s disease, recovering ability of directly inhibiting oligomerized and fibrous amyloid beta, which is inherent activities of existing curcumin, thereby being useful as a novel inhibitor.COPYRIGHT KIPO 2017
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- PHARMACEUTICAL COMPOUNDS
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This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.
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Page/Page column 91; 129
(2015/09/23)
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- Dicyanovinyl-substituted J147 analogue inhibits oligomerization and fibrillation of β-amyloid peptides and protects neuronal cells from β-amyloid-induced cytotoxicity
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A series of novel J147 derivatives were synthesized, and their inhibitory activities against β-amyloid (Aβ) aggregation and toxicity were evaluated by using the oligomer-specific antibody assay, the thioflavin-T fluorescence assay, and a cell viability assay in the transformed SH-SY5Y cell culture. Among the synthesized J147 derivatives, 3j with a 2,2-dicyanovinyl substituent showed the most potent inhibitory activity against Aβ42 oligomerization (IC50 = 17.3 μM) and Aβ42 fibrillization (IC50 = 10.5 μM), and disassembled the preformed Aβ42 fibrils with an EC50 of 10.2 μM. Finally, we confirmed that 3j is also effective at preventing neurotoxicity induced by Aβ42-oligomers as well as Aβ42-fibrils.
- Kim, Kyoungdo,Park, Kwang-Su,Kim, Mi Kyoung,Choo, Hyunah,Chong, Youhoon
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supporting information
p. 9564 - 9569
(2015/09/28)
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- A mild oxidation of deactivated naphthalenes and anthracenes to corresponding para-quinones by N-bromosuccinimide
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A new method to synthesize 1,4-naphthoquinone and 9,10-anthraquinone from naphthalene and anthracene functionalized with either -CHO or -COOH groups, using N-bromosuccinimide (NBS) in aqueous N,N-dimethylformamide at 75-80 °C, has been developed. Further, -CN and -CONH2 functionalized naphthalenes and anthracenes can also be transformed into respective para-quinones in a one pot reaction, after successive acid hydrolysis and subsequent reaction with NBS. We believe that the present finding may serve as a valuable alternative to the classical approaches for the synthesis of polycyclic quinones from polyaromatic carbaldehydes through Dakin oxidation followed by further oxidation of the resulting hydroquinone by heavy metal oxides.
- Natarajan, Palani,Vagicherla, Vinuta Devi,Vijayan, Muthana Thevar
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p. 3511 - 3515
(2014/06/10)
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- FSH RECEPTOR ANTAGONISTS
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The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders
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Page/Page column 64
(2013/04/10)
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- Analogues of orphan nuclear receptor small heterodimer partner ligand and apoptosis inducer (E)-4-[3-(1-adamantyl)-4-hydroxyphenyl]-3-chlorocinnamic acid. 2. Impact of 3-chloro group replacement on inhibition of proliferation and induction of apoptosis of
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The parent phenol of adapalene and its (E)-cinnamic acid analogue were found to induce cancer cell apoptosis but cause adverse systemic effects when administered to mice. In contrast, their respective 5-Cl- and 3-Cl-substituted analogues had their adverse
- Xia, Zebin,Correa, Ricardo G.,Das, Jayanta K.,Farhana, Lulu,Castro, David J.,Yu, Jinghua,Oshima, Robert G.,Fontana, Joseph A.,Reed, John C.,Dawson, Marcia I.
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experimental part
p. 233 - 249
(2012/03/10)
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- Synthesis and preliminary evaluation of curcumin analogues as cytotoxic agents
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A series of curcumin analogues with different substituents at the 4-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines. Several novel curcumin analogues, especially 32 and 34, exhibited selective and potent cytotoxic activity against human epidermoid carcinoma cell line A-431 and human glioblastoma cell line U-251, implying their specific potential in the chemoprevention and chemotherapy of skin cancer and glioma. The preliminary SAR information extracted from the results suggested that introduction of appropriate substituents to the 4′-positions could be a promising approach for the development of new cytotoxic curcumin analogues with special selectivity for A-431 and U-251 cell lines.
- Zhang, Qin,Zhong, Ying,Yan, Lin-Na,Sun, Xun,Gong, Tao,Zhang, Zhi-Rong
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p. 1010 - 1014
(2011/03/21)
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- (DIHYDRO) IMIDAZOISO (5, 1-A) QUINOLINES AS FSH RECEPTOR AGONISTS FOR THE TREATMENT OF FERTILITY DISORDERS
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The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula (1) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
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Page/Page column 30-31
(2010/12/26)
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- (DIHYDRO)IMIDAZOISO[5,1-A]QUINOLINES
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The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
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Page/Page column 11; 12
(2010/12/31)
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- Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IκB kinase-β (IKK-β)
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The identification and progression of a potent and selective series of isoquinoline inhibitors of IκB kinase-β (IKK-β) are described. Hit-generation chemistry based on IKK-β active-site knowledge yielded a weakly potent but tractable chemotype that was rapidly progressed into a series with robust enzyme and cellular activity and significant selectivity over IKK-α.
- Christopher, John A.,Bamborough, Paul,Alder, Catherine,Campbell, Amanda,Cutler, Geoffrey J.,Down, Kenneth,Hamadi, Ahmed M.,Jolly, Adrian M.,Kerns, Jeffrey K.,Lucas, Fiona S.,Mellor, Geoffrey W.,Miller, David D.,Morse, Mary A.,Pancholi, Kiritkant D.,Rumsey, William,Solanke, Yemisi E.,Williamson, Rick
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supporting information; experimental part
p. 3098 - 3102
(2010/03/03)
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- (DIHYDRO)PYRROLO[2,1-A]ISOQUINOLINES
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The invention relates to 5,6 - dihydropyrrolo [2,1-a] isoquinoline and pyrrolo[2,1-a] isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
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Page/Page column 100-101
(2009/10/09)
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- Halogen-lithium exchange between substituted dihalobenzenes and butyllithium: Application to the regioselective synthesis of functionalized bromobenzaldehydes
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Halogen-lithium interconversion reactions between unsymmetrically substituted mono- and bifunctional dihalobenzenes C6H 3XHal2 and C6H2XYHal2 (Hal=Br, I; X, Y=F, OR, CF3, CH(OMe)2) and butyllithium were investigated. The resultant organolithium intermediates were converted into the corresponding benzaldehydes in moderate to good yields. As a rule, bromine atoms in the position ortho to the functional group were replaced preferentially with lithium. Intramolecular competition experiments with bifunctional systems revealed that fluorine is capable of activating the neighboring bromine atom more strongly than methoxy and dimethoxymethyl groups. On the replacement of the non-activated bromine with iodine a complete reversal of this reactivity pattern can be accomplished due to the preferred iodine-lithium exchange.
- Da?browski, Marek,Kubicka, Joanna,Luliński, Sergiusz,Serwatowski, Janusz
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p. 6590 - 6595
(2007/10/03)
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- Indirect Electrooxidation of Alcohols by a Double Mediatory System with Two Redox Couples of +=O>/R2NO. and . or Br+>/Br- in an Organic-Aqueous Two-Phase Solution
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An indirect electrooxidation method for alcohol to aldehyde or ketone conversion has been developed.This method, applicable to chemoselective oxidation, employs two redox couples, consisting of 2,2,6,6-tetramethylpiperidine-1-oxyl derivatives 6 and active bromine species.The former is required for the chemical process and recycled, whereas the latter is to be involved in the electrochemical process.Three chemical events play an important role in this system: (1) the formation of . or Br+> from bromide ion by discharge on the anode in an aqueous solution, (2) the reaction of N-oxyl compounds 6 with active bromine species to generate N-oxoammonium ion 7, and (3) the oxidation of alcohols with 7 in an organic phase.Optimum conditions were established as follows: an aqueous 25percent NaBr solution buffered at pH 8.6 in a binary system, the use of 1-10 mol percent of 4-(benzoyloxy)piperidine derivatives 6, and adjustment of an electric current at 10-100 mA/cm2.The successful applications of the present method to the oxidation of a variety of primary and secondary alcohols including 1,n-diols, giving the corresponding carbonyl compounds, have delineated its synthetic utility.The chemoselective oxidation of a primary hydroxy group in the presence of secondary one has been achieved with a high selectivity by the present procedure.
- Inokuchi, Tsutomu,Matsumoto, Sigeaki,Torii, Sigeru
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p. 2416 - 2421
(2007/10/02)
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- Enantioselective total synthesis of medermycin (lactoquinomycin)
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Medermycin has been first synthesized from D-rhamnose derivatives and comfirmed to be identical with lactoquinomycin.
- Tatsuta, Kuniaki,Ozeki, Hidekazu,Yamaguchi, Mami,Tanaka, Masashi,Okui, Toshiharu
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p. 5495 - 5498
(2007/10/02)
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