- Synthesis of 5-chloro-7-azaindoles by Fischer reaction
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[Figure not available: see fulltext.] A simple and effective method on the basis of Fischer reaction in polyphosphoric acid is proposed for the synthesis of previously unknown heterocyclic structures that contain the 5-chloro-1H-pyrrolo[2,3-b]pyridine system. This method can be used for the synthesis of 3-substituted and 2,3-disubstituted 5-chloro-7-azaindoles with alkyl and aryl substituents.
- Alekseyev, Roman S.,Amirova, Sabina R.,Terenin, Vladimir I.
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p. 196 - 206
(2017/05/19)
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- HUMAN PLASMA KALLIKREIN INHIBITORS
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Disclosed are compounds of formula (I), as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
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Page/Page column 147
(2015/11/02)
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- CYANINE DYES AND THEIR CONJUGATES
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Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. The cyanine compounds of Formula (I), are presented: wherein Q is a portion of a polymethine bridge selected from the group consisting (Formula (X)). Also included are bioconjugates of the compounds of Formula (I), methods of labeling biomolecules with the compounds, and methods of imaging.
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Page/Page column 64-65
(2012/05/05)
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- Design and synthesis of a new class of membrane-permeable triazaborolopyridinium fluorescent probes
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A new class of fluorescent triazaborolopyridinium compounds was synthesized from hydrazones of 2-hydrazinylpyridine (HPY) and evaluated as potential dyes for live-cell imaging applications. The HPY dyes are small, their absorption/emission properties are
- Hapuarachchige, Sudath,Montano, Gilbert,Ramesh, Chinnasamy,Rodriguez, Delany,Henson, Lauren H.,Williams, Casey C.,Kadavakkollu, Samuel,Johnson, Dennis L.,Shuster, Charles B.,Arterburn, Jeffrey B.
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supporting information; experimental part
p. 6780 - 6790
(2011/06/22)
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- 4-(PYRIDIN-3-YL)-2-(PYRIDIN-2-YL)-1,2-DIHYDRO-3H-PYRAZOL-3-ONE DERIVATIVES AS SPECIFIC HIF-PROLYL-4-HYDROXYLASE INHIBITORS FOR TREATING CARDIOVASCULAR AND HAEMATOLOGICAL DISEASES
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The object of the invention is to provide new compounds which can be used for the treatment of diseases, in particular cardiovascular and haematological diseases. The present invention describes compounds which act as specific HIF-prolyl-4-hydroxylase inhibitors and which, because of this specific in vivo action mechanism, induce HIF target genes, such as erythropoietin, and the thus produced biological processes, such as erythropoiesis, after parenteral or oral administration. The present invention relates to compounds having the general formula (I), in which A stands for CH or N, R1 stands for a substituent selected from the group formed by (C1-C6)-alkyl, trifluoromethyl, halogen, cyano, nitro, hydroxy, (C1-C6)-alkoxy, amino, (C1-C6)-alkoxycarbonyl, hydroxycarbonyl and C(=O)-NH-R4; R2 stands for a substituent selected from the group formed by halogen, cyano, nitro, (C1-C6)-alkyl, trifluoromethyl, hydroxy, (C1-C6)-alkoxy, trifluoromethoxy, amino, hydroxycarbonyl and C(=O)-NH-R8; m equals 0, 1 or 2; n equals 0, 1, 2 or 3, it being possible for these meanings to be the same or different when R1 or R2 occurs multiple times; and R3 stands for hydrogen, (C1-C6)-alkyl or (C3-C7)-cycloalkyl. The invention also relates to the salts, solvates, and salt solvates of these compounds.
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Page/Page column 40
(2008/06/13)
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- Condensed pyrazole derivatives, process for producing the same and use thereof
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Novel pharmaceutical compositions for inhibiting Th2-selective immune response and pharmaceutical compositions for inhibiting cyclooxygenase comprising condensed pyrazole derivatives represented by the general formula (I): or salts thereof.
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- BICYCLIC TRIAZOLONE DERIVATIVES AND HERBICIDES CONTAINING THE SAME
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The present invention provides a bicyclic triazolone derivative represented by the formula:J-Ar [wherein, J is and Ar is ], which has excellent selective weeding activity and weed killer containing the said bicyclic triazolone derivative.
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- 2-(pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3 (2H)-One 1, 1-dioxides and compositions and method of use thereof
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2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
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- Substituted 2-acylpyridine-α-(N)-hetarlyhydrazones and medicaments containing the same
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Substituted 2-acylpyridine-α-(N)-hetarylhydrazones are described, which are suitable as active substances for the treatment of antimicrobial and in particular antimycobacterial diseases, as well as active substances for the treatment of malaria or malignant tumours. The compounds have a marked synergistic activity combined with inhibitors of folate synthase, dihydrofolic acid reductase, DNA-synthesis and RNA-synthesis.
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- Heterocyclic substituted-amino-pyrazolines
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This invention relates to novel 3-amino-1-heteroaryl-2-pyrazolines and their C4 and C5 analogs, useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.
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- 2-Pyridylhydrazides
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2-Pyridylhydrazides useful as antiinflammatory agents.
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