- HEPATITIS B VIRUS SURFACE ANTIGEN INHIBITOR
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10-oxo-6,1-dihydrobenzo[e]pyrido[1,2-c][1,3]oxazine-9-carboxylic acid derivatives of formula (I) as hepatitis B surface antigen inhibitors or pharmaceutically acceptable salts thereof, and uses of a compound of formula (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions thereof in preparation of medicaments for treatment of viral hepatitis B.
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Paragraph 0217; 0218
(2020/01/22)
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- Synthesis of 2,5-di(hydroxyalkyl)-1,3-thiazoles
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A general approach towards synthesis of 2(5)-hydroxyalkyl-substituted 1,3-thiazole derivatives has been proposed. The method includes lithiation of 1,3-thiazole ring followed by reacting the formed thiazole lithium derivatives with electrophiles.
- Sinenko,Slivchuk,Bal'On, Ya. G.,Brovarets
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p. 1855 - 1861
(2015/10/12)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 123
(2013/10/22)
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- Cu-catalyzed cross-dehydrogenative coupling reactions of (benzo)thiazoles with cyclic ethers
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Copper-catalyzed cross-dehydrogenative coupling (CDC) reactions of (benzo)thiazoles with cyclic ethers were developed under mild conditions. In particular, the formation of C-C bonds via the CDC reactions between non-benzo-fused azoles and ethers are reported for the first time. In addition, the acetals, known as the masked 2-thiazolecarboxaldehydes, could be successfully obtained by this CDC reaction. The preliminary mechanism and supportive DFT calculations are discussed as well.
- Xie, Zengyang,Cai, Yuping,Hu, Hongwen,Lin, Chen,Jiang, Juli,Chen, Zhaoxu,Wang, Leyong,Pan, Yi
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supporting information
p. 4600 - 4603
(2013/09/24)
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- SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
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This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
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Page/Page column 76
(2011/09/20)
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- Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor
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Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintainin
- Shen, Hong C.,Ding, Fa-Xiang,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Ren, Ning,Cai, Tian-Quan,Deng, Qiaolin,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
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p. 6303 - 6306
(2008/04/12)
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- NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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The present invention encompasses compounds of Formula (I); as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.
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Page/Page column 55-56
(2010/11/08)
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- CONDENSED HETEROCYCLIC COMPOUNDS AS CALCITONIN AGONISTS
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The present invention relates to novel fused heterocyclic ring system compounds and methods for their use in the treatment and prevention of diseases or conditions which are related to irregular calcification.
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Page/Page column 66
(2010/02/07)
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- Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
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Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
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- Novel NMDA Antagonists: Replacement of the Pyridinium Ring of 6,11-Ethanobenzoquinolizinium Cations with Heteroisoquinolinium Cations
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Replacement of the pyridinium ring of 6,11-ethanobenzoquinolizinium cations with thiazolium (4a and 4b) and N-methylimidazolium (4c and 4d) resulted in equipotent compounds in the TCP binding assay.The corresponding N-methyl-1,2,4-triazolium analogs were less potent in this assay.The thiazolium derivative 4b, with a Ki = 2.9 nM, is being evaluated as a possible neuroprotective N-methyl-D-aspartic acid (NMDA) anatgonist.
- Kumar, Virendra,Carbateas, Phil M.,Dority, John A.,Earley, William G.,Mallamo, John P.,et al.
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p. 1826 - 1830
(2007/10/02)
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