- COMPOUNDS, COMPOSITIONS AND METHODS FOR HISTONE LYSINE DEMETHYLASE INHIBITION
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The present disclosure relates generally to compounds and pharmaceutical compositions for the selective inhibition of histone lysine demethylase5 (KDM5), particularly KDM5B, and methods of their use in treating conditions and diseases associated with KDM5 activity.
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Paragraph 0737; 0765
(2022/03/09)
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- Influences of Histidine-1 and Azaphenylalanine-4 on the Affinity, Anti-inflammatory, and Antiangiogenic Activities of Azapeptide Cluster of Differentiation 36 Receptor Modulators
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Azapeptide analogues of growth hormone releasing peptide-6 (GHRP-6) exhibit promising affinity, selectivity, and modulator activity on the cluster of differentiation 36 receptor (CD36). For example, [A1, azaF4]- and [azaY4
- Chignen Possi, Kelvine,Mulumba, Mukandila,Omri, Samy,Garcia-Ramos, Yesica,Tahiri, Houda,Chemtob, Sylvain,Ong, Huy,Lubell, William D.
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supporting information
p. 9263 - 9274
(2017/11/30)
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- GUANIDINOBENZOIC ACID COMPOUND
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[Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they
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Paragraph 0144
(2014/08/06)
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- CYCLOHEXYLPYRAZOLE-LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compound
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- Synthesis of novel structurally simplified estrogen analogues with electron-donating groups in ring A
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A library of 25 novel estrogen analogues were prepared in five to eight steps from mostly commercially available substituted anisoles via bromination, formylation, Corey-Fuchs reaction, elimination, and Sonogashira reaction. Georg Thieme Verlag Stuttgart.
- Tietze, Lutz F.,Vock, Carsten A.,Krimmelbein, Ilga K.,Nacke, Linda
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experimental part
p. 2040 - 2060
(2009/12/27)
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- INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11Beta-HSD type 1 activity. X-17377
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- INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: (I) having 11 -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11 -HSD type 1 activity.
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- PROPHYLACTIC/THERAPEUTIC AGENT FOR DIABETES
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The present invention relates to a 11β-hydroxysteroid dehydrogenase 1 inhibitor comprising a compound represented by the formula (1): wherein each symbol is as defined in the description, or a salt thereof, or a prodrug thereof. The 11β-hydroxysteroid dehydrogenase 1 inhibitor of the present invention has a superior activity, and is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, insulin resistance, obesity, abnormal lipid metabolism, hypertension and the like, and the like.
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Page/Page column 134-135
(2008/06/13)
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- CYCLOHEXYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: having 11β -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
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Page/Page column 28
(2008/06/13)
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- CYCLOHEXYLIMIDAZOLE LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: ( I ) having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds
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Page/Page column 38
(2008/06/13)
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- INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: ( I ) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11β-HSD type 1 activity.
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Page/Page column 38
(2008/06/13)
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- SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: ( I ) possessing 11β -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 β -HSD type 1 activity.
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Page/Page column 29
(2008/06/13)
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- PIERIDINYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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ABSTRACT The present invention discloses novel compounds of Formula I: ( I ) having 11-Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-Beta-HSD type 1 activity. X-17433 PCT -1-
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Page/Page column 42-43
(2008/06/13)
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- HYDROXY-BIPHENYL-CARBALDEHYDE OXIME DERIVATIVES AND THEIR USE AS ESTROGENIC AGENTS
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This invention provides estrogen receptor modulators having the structure formula (I): wherein R1 to R6 and R8 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
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- ERbeta ligands. Part 1: the discovery of ERbeta selective ligands which embrace the 4-hydroxy-biphenyl template.
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The synthesis and structure-activity relationships of a series of simple biphenyls is described. Optimization of the 4-hydroxy-biphenyl template led to compounds with ERbeta selectivity on the order of 20-70-fold.
- Edsall Jr., Richard J,Harris, Heather A,Manas, Eric S,Mewshaw, Richard E
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p. 3457 - 3474
(2007/10/03)
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- Ring-Substituted y1,2-Bis(4-hydroxyphenyl)ethylenediamine>dichloroplatinum(II) Complexes: Compounds with a Selective Effect on the Hormone-Dependent Mammary Carcinoma
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dichloroplatinum(II) complexes with one substituent in the 2-position (CH3, CF3, F, Br, I: meso- and dl-1-PtCl2, meso-(3-5)-PtCl2, meso-(7 and 8)-PtCl2) or two substituents in the 2,6-position (CH3, Cl: meso-2-PtCl2, meso- and dl-6-PtCl2) in both benzene rings were synthesized and tested for estrogenic and toxic activities.Two complexes (meso-6-PtCl2 and meso-7-PtCl2) possess both effects.In comparative tests on estrogen receptor positive and negative mammary tumors in cell culture (MCF 7, ER+ and MDA-MB 231, ER-) and in animals (MXT, ER+ and MXT, ER-, mouse), meso-6-PtCl2 shows a selective effect on the estrogen receptor positive mammary carcinoma.A further increase of efficacy was achieved with the water-soluble (sulfato)platinum(II) derivative (meso-6-PtSO4).On the DMBA-induced hormone dependent mammary carcinoma of the SD rat, meso-6-PtSO4 is significantly more active than its ligand (meso-6) and cisplatin.
- Karl, Johann,Gust, Ronald,Spruss, Thilo,Schneider, Martin R.,Schoenenberg, Helmut,et al.
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