- In vitro and in vivo evaluation of fluorinated indanone derivatives as potential positron emission tomography agents for the imaging of monoamine oxidase B in the brain
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Monoamine oxidases (MAOs) play a key role in the metabolism of major monoamine neurotransmitters. In particular, the upregulation of MAO-B in Parkinson's disease, Alzheimer's disease and cancer augmented the development of selective MAO-B inhibitors for d
- Duki?-Stefanovi?, Sladjana,Hang Lai, Thu,Toussaint, Magali,Clau?, Oliver,Jevti?, Ivana I.,Penji?evi?, Jelena Z.,Andri?, Deana,Ludwig, Friedrich-Alexander,Gündel, Daniel,Deuther-Conrad, Winnie,Kosti?-Raja?i?, Sladjana V.,Brust, Peter,Teodoro, Rodrigo
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supporting information
(2021/07/21)
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- BICYCLIC COMPOUNDS
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Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
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Paragraph 00639
(2020/06/01)
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- MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).
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Page/Page column 39
(2018/03/25)
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- FLUOROINDOLE DERIVATIVES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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The present invention relates to compound of formula (I), or stereoisomers and pharmaceutically acceptable salts as muscarinic M1 receptor positive allosteric modulators. This invention also relates to methods of making such compounds and pharmaceutical compositions comprising such compounds. The compounds of this invention are useful in the treatment of various disorders that are related to muscarinic M1 receptor.(Formula I) (I)
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Page/Page column 23
(2017/03/28)
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- Synthesis, in Vitro Evaluation, and Radiolabeling of Fluorinated Puromycin Analogues: Potential Candidates for PET Imaging of Protein Synthesis
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There is currently no ideal radiotracer for imaging of protein synthesis rate (PSR) by positron emission tomography (PET). Existing fluorine-18-labeled amino acid-based radiotracers predominantly visualize amino acid transporter processes, and in many cases they are not incorporated into nascent proteins at all. Others are radiolabeled with the short-half-life positron emitter carbon-11, which is rather impractical for many PET centers. Based on the puromycin (6) structural manifold, a series of 10 novel derivatives of 6 was prepared via Williamson ether synthesis from a common intermediate. A bioluminescence assay was employed to study their inhibitory action on protein synthesis, which identified the fluoroethyl analogue 7b as a lead compound. The fluorine-18 analogue was prepared via nucleophilic substitution of the corresponding tosylate precursor in a modest radiochemical yield of 2 ± 0.6% with excellent radiochemical purity (>99%) and showed complete stability over 3 h at ambient temperature.
- Betts, Helen M.,Milicevic Sephton, Selena,Tong, Carmen,Awais, Ramla O.,Hill, Philip J.,Perkins, Alan C.,Aigbirhio, Franklin I.
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supporting information
p. 9422 - 9430
(2016/11/11)
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- LABELLED CHROMONE DERIVATIVES
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The present invention relates to compounds having selective binding for MAO-B as compared with MAO-A. The invention also provides radioactive versions of these compounds, and precursor compounds for the synthesis of these radioactive compounds. The radioa
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Page/Page column 12
(2016/07/05)
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- NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVES AND METHOD FOR PREPARING THE SAME
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The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).
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Paragraph 0471; 0472; 0473
(2014/09/16)
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- NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVE AND A PRODUCTION METHOD FOR SAME
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The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).
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Paragraph 0452; 0453; 0454
(2014/12/09)
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- PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as ALzheimer?s disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor
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Page/Page column 70
(2011/04/14)
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- Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: Advantages in comparison with competitive inhibitors
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A new series of IGF-1R inhibitors related to hydantoins were identified from a lead originating from HTS. Their noncompetitive property as well as their slow binding characteristics provided a series of compounds with unique selectivity and excellent cellular activities.
- Lesuisse, Dominique,Mauger, Jacques,Nemecek, Conception,Maignan, Sébastien,Boiziau, Janine,Harlow, Greg,Hittinger, Augustin,Ruf, Swen,Strobel, Hartmut,Nair, Anil,Ritter, Kurt,Malleron, Jean-Luc,Dagallier, Anne,El-Ahmad, Youssef,Guilloteau, Jean-Pierre,Guizani, Houlfa,Bouchard, Hervé,Venot, Corinne
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body text
p. 2224 - 2228
(2011/05/15)
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- N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
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A series of N1-heterocyclic pyrimidinediones were extensively evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Inhibitor 1 is active against NNRTI-resistant viruses including RT mutant K103N. The co-crystal structure of inhibit
- Mitchell, Michael L.,Son, Jong Chan,Lee, Ill Young,Lee, Chong-Kyo,Kim, Hae Soo,Guo, Hongyan,Wang, Jianhong,Hayes, Jaclyn,Wang, Michael,Paul, Amber,Lansdon, Eric B.,Chen, James M.,Eisenberg, Gene,Geleziunas, Romas,Xu, Lianhong,Kim, Choung U.
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scheme or table
p. 1585 - 1588
(2010/06/17)
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- Novel HIV reverse transcriptase inhibitors
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The invention is related to compounds of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
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Page/Page column 37-38
(2008/06/13)
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- COMBINATION OF CB2 MODULATORS AND PDE4 INHIBITORS FOR USE IN MEDICINE
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Combination of one or more CB2 modulators such as a compound of formula (I), (II) and (III); and one more PDE4 inhibitors are useful of treating conditions which are mediated by the activity of CB2 receptors or conditions which are mediated by PDE4, such
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Page/Page column 38; 110
(2010/02/13)
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- PYRIMIDINE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS
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The present invention relates to novel pyrimidine derivatives such as compounds of the formula (I) and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.
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Page/Page column 39
(2010/02/13)
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- PYRIDINE DERIVATIVES AS CB2 RECEPTOR MODULATORS
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The present invention relates to novel pyridine derivatives of formula (I) pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increas
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- Novel cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
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The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
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- PYRIMIDINE COMPOUNDS
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The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decreas
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- SUBSTITUTED PHENYL COMPOUNDS WITH A SUBSTITUENT HAVING A 1,3-BENZODIOXOLE RING
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This invention is directed to compounds of formula I STR1 wherein R 1 is CN, CH 2 CN, CH=CHCN, CHO, or CH=CHCO. sub. 2 H;R 2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio wherein each of the aryl and heteroaryl moieties is optionally substituted;R 3 is halogen;R 4 is optionally substituted aryl or optionally substituted heteroaryl;R. sup.5 is carboxy or an acid isostere; X is oxygen or sulphur; and n is zero or 1; or an N-oxide thereof, prodrug thereof solvate thereof, or pharmaceutically acceptable salt thereof, which compounds have endothelin antagonist activity. The invention is also directed to methods for preparing the compounds of formula I and their pharmaceutical use.
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- Substituted phenyl compounds with a substituent having a thienyl ring
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This invention is directed to compounds of formula I wherein R1 is CN, CH2CN, CH=CHCN, CHO, or CH=CHCO2H; R2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio wherein each of the aryl and heteroaryl moieties is optionally substituted; R3 is halogen; R4 is optionally substituted aryl or optionally substituted heteroaryl; R5 is carboxy or an acid isostere; X is oxygen or sulphur; and n is zero or 1; or an N-oxide thereof, prodrug thereof solvate thereof, or pharmaceutically acceptable salt thereof, which compounds have endothelin antagonist activity. The invention is also directed to methods for preparing the compounds of formula I and their pharmaceutical use.
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- Fluoropyridinylmethyl cyclopropanecarboxylate insecticides
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Insecticidal compounds of the formula STR1 formulations thereof, their use for control of foliar or soil-borne insects, their method of preparation and certain novel intermediates for their preparation are disclosed and exemplified.
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