- 3-AMINO-PYRIDINES AS GPBAR1 AGONISTS
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This invention relates to novel 3-aminopyridines of the formula wherein B1, B2 and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes
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Page/Page column 61
(2012/09/22)
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- 3-AMINO-PYRIDINES AS GPBAR1 AGONISTS
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This invention relates to novel 3-aminopyridines of the formula (I) wherein B1, B2 and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
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Page/Page column 128
(2012/09/21)
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- The first porous MOF with photoswitchable linker molecules
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We synthesized a porous twofold interpenetrated MOF [Zn2(NDC) 2(1)] (coined CAU-5) using 3-azo-phenyl-4,4′-bipyridine (1), 2,6-naphthalenedicarboxylic acid, and Zn(NO3)2· 6H2O. The azo-functionality protrudes into the pores, and can be switched, by irradiation with UV light (365 nm), from the thermodynamically stable trans-isomer to the cis-isomer. Back-switching was achieved thermally and with an irradiation wavelength of λmax = 440 nm.
- Modrow, Antje,Zargarani, Dordaneh,Herges, Rainer,Stock, Norbert
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supporting information; scheme or table
p. 4217 - 4222
(2011/06/18)
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- AZA-BETA-CARBOLINES AND METHODS OF USING SAME
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Provided are compounds having the general structure according to Formula (I): Further provided are pharmaceutical compositions comprising these compounds. The invention still further provides methods of treating alcoholism, methods of reducing alcohol intake, methods of treating anhedonia, and methods of treating anxiety using theses compounds or the compositions containing them.
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Page/Page column 24-25; sheet 16
(2009/12/24)
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- IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT' OF CANCER
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The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. wherein: R1 hydrogen, hydroxy, halo, methyl, C1-C2 alkoxy, amino, or rnethylamino; R2 is hydrogen, halo, or cyano; R3 is hydrogen or halo;, R4 is hydrogen, halo, or methyl; provided that at least two of R1, R2, R3, and R4 are hydrogen; R5 is hydrogen, halo, or methyl; or a pharmaceutically acceptable salt thereof.
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Page/Page column 8-9
(2008/12/06)
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- TRIAZOLYL AMINOPYRIMIDINE COMPOUNDS
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The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.
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Page/Page column 26
(2009/01/20)
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- Nonsteroidal glucocorticoid agonists: Tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (Transrepression/Transactivation) efficacy selectivity
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The synthesis and biological activity of tetrahydronaphthalene derivatives coupled to various heterocycles are described. These compounds are potent glucocorticoid receptor agonists with efficacy selectivity in an NFκB glucocorticoid receptor (GR) agonist assay (representing transrepression effects) over an MMTV GR agonist assay (representing transactivation effects). Quinolones, indoles, and C- and N-linked quinolines are some of the heterocycles that provide efficacy selectivity. For example, the isoquinoline 49D1E2 has NFκB agonism with pIC50 of 8.66 (89%) and reduced efficacy in MMTV agonism (6%), and the quinoline 55D1E1 has NFκB agonism with pIC 50 of 9.30 (101%) and reduced efficacy in MMTV agonism with pEC 50 of 8.02 (47%). A description of how a compound from each class is modeled in the active site of the receptor is given.
- Biggadike, Keith,Boudjelal, Mohamed,Clackers, Margaret,Coe, Diane M.,Demaine, Derek A.,Hardy, George W.,Humphreys, Davina,Inglis, Graham G. A.,Johnston, Michael J.,Jones, Haydn T.,House, David,Loiseau, Richard,Needham, Deborah,Skone, Philip A.,Uings, Iain,Veitch, Gemma,Weingarten, Gordon G.,McLay, Iain M.,Macdonald, Simon J. F.
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p. 6519 - 6534
(2008/09/17)
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- Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
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The invention relates to tetrahydronaphthyridine derivatives having formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said tetrahydronaphthyridine derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 57
(2008/06/13)
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- Synthesis of optically active ring-A substituted tryptophans as IDO inhibitors
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The first synthesis of optically active 7-methoxy-d-tryptophan as well as other ring-A substituted tryptophans is described.
- Li, Xiaoyan,Yin, Wenyuan,Sarma, P.V.V. Srirama,Zhou, Hao,Jun Ma,Cook, James M.
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p. 8569 - 8573
(2007/10/03)
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- Compounds and their use
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This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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- Synthesis of 3-Amino-4-phenylpyridines: a Novel Strategy for the Preparation of CD Ring Models of Streptonigrin
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An efficient synthesis of 3-amino-4-phenylpyridine derivatives is reported. 3-Pivaloylaminopyridines were lithiated by butyl-lithium before reaction with iodine as electrophile to afford 4-iodo-3-pivaloylaminopyridines.Cross-coupling of the latter with su
- Marsais, Francis,Rovera, Jean-Claude,Turck, Alain,Godard, Alain,Queguiner, Guy
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p. 2611 - 2612
(2007/10/02)
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- Metalation/SRN1 Coupling in Heterocyclic Synthesis. A Convenient Methodology for Ring Functionalization
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Lithiation, iodination, and fluorine substitution on 2-fluoropyridine gave 2-substituted 3-iodopyridines, which were further subjected to iodine SRN1 substitution by carbon, sulfur, and phosphorus nucleophiles.Iodine substitution by enolates on 2-amino-3-iodopyridines afforded ketones, which were further cyclized to various 1,2-disubstituted pyrrolopyridines. 2-Amino-3-iodo-, 3-amino-4-iodo, and 4-amino-3-iodopyridines were prepared by directed metalation of 2-, 3-, and 4-(pivaloylamino)pyridines.Substitution of iodine by enolates under SRN1 conditions and acidic cyclization led to various 2-substituted pyrrolo, --, and -pyridines in high yields.
- Estel, L.,Marsais, F.,Queguiner, G.
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p. 2740 - 2744
(2007/10/02)
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