- Cobalt-Catalyzed Hydroalkynylation of Vinylaziridines
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Transition metal-catalyzed hydroalkynylation reactions are efficient transformations allowing the straightforward formation of functionalized alkynes. Therein, we disclose the cobalt-catalyzed hydroalkynylation of vinylaziridines giving rise to both linea
- Biletskyi, Bohdan,Kong, Lingyu,Tenaglia, Alphonse,Clavier, Hervé
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p. 2578 - 2585
(2021/03/18)
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- ARYLPYRAZOLES AND ARYLISOXAZOLES AND THEIR USE AS PKD MODULATORS
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The present invention provides novel organic compounds of formula (I) or (Ia): which may be inhibitors of a selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example PKD-1/2/3, inhibitors of histone deacetylase (HDA
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- SUBSTITUTED PHENYLETHYNYL GOLD-NITROGENATED HETEROCYCLIC CARBENE COMPLEX
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The present invention is directed to a substituted phenylethynylgold-nitrogen-containing heterocyclic carbene complex represented by the formula (1) or (2): wherein L represents a nitrogen-containing heterocyclic carbene ligand, and X represents an alkyl
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- NOVEL COMPOUNDS
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Compounds of the formula (I) are disclosed which are large conductance calcium activated potassium channel openers (BK channels openers) and are useful in the treatment of urinary tract disorders: (I), or a pharmaceutically acceptable salt thereof.
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- BENZO [b][1,4] DIOXEPINE DERIVATIVES
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This invention relates to compounds of the formula (I), wherein B, X, Y, Z, R1 and R2 are as defined in the description, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by ACCβ inhibitors.
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Page/Page column 28
(2010/02/11)
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- Benzodioxepine derivatives
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This invention relates to compounds of the formula wherein B, X, Y, Z, R1 and R2 are as defined in the description, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by ACCβ inhibitors.
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Page/Page column 8; 13
(2010/02/11)
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- DICARBA-closo-DODECABORANE DERIVATIVES
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A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I): wherein R1 represents a dicarba-closo-dodecaboran-yl which may be substituted with a lower alkyl group,
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- Dicarba-closo-dodecaboranes as a pharmacophore. Retinoidal antagonists and potential agonists
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Synthesis and biological evaluation of the first dicarba-closo- dodecaborane (carborane) derivatives of retinoids are described. Their retinoidal activity were examined in terms of the differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells. High retinoidal activity (agonist or antagonist for retinoic acid receptor (RAR)) requires a carboxylic acid moiety and an appropriate hydrophobic group located at a suitable position on the molecule. The 4-carboranyl-substituted compounds (7, 11) showed antagonistic activity but no agonistic activity even in the presence of the potent synergist HX630. On the other hand, the 3-carboranyl- substituted compounds (8, 12) showed potential agonistic activity, but no antagonistic activity. The results indicates that carboranes are applicable as the hydrophobic moiety of biologically active molecules.
- Iijima, Toru,Endo, Yasuyuki,Tsuji, Motonori,Kawachi, Emiko,Kagechika, Hiroyuki,Shudo, Koichi
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p. 398 - 404
(2007/10/03)
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- Novel dienes and dienophiles, VI: On the chemical behavior of Z-ethynyl-1,3-butadiene
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The behavior of 2-ethynyl-1,3-butadiene (1) as the diene component in Diels-Alder additions has been studied using a selection of representative double and triple bond dienophiles. The latter include maleic anhydride (5a), diethyl fumarate (6), benzoquinone (7), methyl acrylate (11), juglone (20), 1-methylcyclopropene (23), dimethyl acetylenedicarboxylate (26), propiolic aldehyde (32), 4-phenyl-1,2,4-triazolin-3,5-dione (35) and diethyl azodicarboxylate (37). [2 + 4] Cycloadducts were formed in all cases in varying yields. The addition is accompanied by thermal dimerization of 1 which leads to 1,4-diethynyl-4-vinyl-1-cyclohexene (43) and 1,6-diethynyl-1,5-cyclooctadiene (39). The mechanism of this dimerization is discussed. In a competition experiment towards maleic anhydride (5a), diene 1 was shown to be ca. five times less reactive than isoprene. VCH Verlagsgesellschaft mbH, 1996.
- Hopf, Henning,Jaeger, Helge,Ernst, Ludger
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p. 815 - 824
(2007/10/03)
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