6854-07-5Relevant articles and documents
METHODS OF TREATING AGITATION
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Page/Page column 34, (2019/06/23)
The present disclosure relates generally to the treatment of agitation associated with neurodegenerative disorders.
Dipyridodiazepinone derivatives; synthesis and anti HIV-1 activity
Khunnawutmanotham, Nisachon,Chimnoi, Nitirat,Techasakul, Supanna,Thitithanyanont, Arunee,Saparpakorn, Patchreenart,Hannongbua, Supa,Choowongkomon, Kiattawee,Pungpo, Pornpan
supporting information; experimental part, (2010/04/22)
Ten dipyridodiazepinone derivatives were synthesized and evaluated for their anti HIV-1 reverse transcriptase activity against wildtype and mutant type enzymes, K103N and Y181C. Two of them were found to be promising inhibitors for HIV-1 RT.
AZAINDOLES AS INHIBITORS OF SOLUBLE ADENYLATE CYCLASE
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Page/Page column 68-69, (2009/04/25)
The present invention relates to azaindoles of general Formula (I), a method for the production thereof, and to the us e thereof for the production of pharmaceutical compositions.
Synthesis and biological evaluation of 2,4,6-functionalized derivatives of pyrido[2,3-d]pyrimidines as cytotoxic agents and apoptosis inducers
Sanmartin, Carmen,Dominguez, Maria Victoria,Cordeu, Lucia,Cubedo, Elena,Garcia-Foncillas, Jesus,Font, Maria,Palop, Juan Antonio
, p. 28 - 41 (2008/09/21)
In the search for new derivatives with anticancer activity that are able to induce a selective proapoptotic mechanism in cancer cells, we have designed, synthesized, and evaluated a series of new 2-(alkylsulfanyl)-N-alkylpyrido[2,3- d]pyrimidine-4-amine derivatives as cytotoxic and apoptosis inducers. The potential antitumor activity of the compounds was evaluated in vitro by examining their cytotoxic effects against human breast, colon, and bladder cancer-cell lines. The IC50 values of the compounds that showed cytotoxic activity were calculated. The cytotoxic compounds were then tested for their ability to induce caspase-3 activation and nuclear-chromatin degradation. Some compounds, such as 6c, 6d, 6e, 6j, 6o, and 6p, show significant in-vitro cytotoxicity in at least two of the three tested cell lines, induced apoptosis, and also produced a rapid dose-dependent increase in the caspase-3 level in some of the cell lines tested. In order to test the selectivity of the compounds, two non-tumoral human cell lines were used. Several compounds of the did not show cytotoxicity in these cell lines.
NOVEL ANXIOLYTIC COMPOUNDS
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Page/Page column 42, (2008/12/05)
The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.
MEDIATORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED THERETO
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Page/Page column 124, (2008/06/13)
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
Inhibitors of protein tyrosine phosphatase 1B
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Page/Page column 9; 25, (2008/06/13)
Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
Transformations of ortho-methoxyaryl(hetaryl)carboxamides into quinazolin-4-one and pyrido[2,3-d]pyrimidin-4-one derivatives
Ryabova,Makarov,Alekseeva,Shashhov,Chernyshev,Granik
, p. 1907 - 1914 (2007/10/03)
ortho-Chloroaryl(hetaryl)carboxamides containing one or two nitro groups at positions 3 and/or 5 of the ring undergo condensation accompanied by the pyrimidine ring closure on refluxing in an excess of sodium methoxide to form bicyclic products, viz., qui
CONFORMATIONALLY RESTRICTED AROMATIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD
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Page 222, (2010/02/06)
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure (I) or (IA) or (IB) including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0,1 or 2; R is H, alkyl, aryl or halogen; A is (1) a bond; (2) -O-; or (3) (i); B is: (ii) or (iii) or (iv) or (v) (wherein (a = 2, 3 or 4)) or (vi) or (vii) or (viii); and wherein L, L, R, R, R, R, R, R, R, R, R, X, (ix), (x) and (xi) are as defined herein.
Hepatitis C viral IRES inhibition by phenazine and phenazine-like molecules
Wang, Wuyi,Preville, Patrice,Morin, Nicolas,Mounir, Samir,Cai, Weizhong,Siddiqui, M. Arshad
, p. 1151 - 1154 (2007/10/03)
An in vitro assay based on the expression of Fluci reporter gene under the translational control of HCV IRES was used to evaluate and screen compound libraries. A structure-activity relationship study on a phenazine hit was conducted. Our data suggest that an intact phenazine or phenazine-like core with two distal polar substitutions is crucial for potency. (C) 2000 Elsevier Science Ltd. All rights reserved.
