- Design and synthesis of multipotent 3-aminomethylindoles and 7-azaindoles with enhanced protein phosphatase 2A-activating profile and neuroprotection
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We report the synthesis and pharmacological evaluation of new 3-aminomethylindoles derivatives with neuroprotective properties designed to present multi-target activity centered on reducing the neuronal Ca2+ overload and preventing phosphatase
- Lajarín-Cuesta, Rocío,Arribas, Raquel L.,Nanclares, Carmen,García-Frutos, Eva M.,Gandía, Luis,de los Ríos, Cristóbal
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- AZAINDOLE CARBOXAMIDE COMPOUNDS FOR THE TREATMENT OF MYCOBACTERIAL INFECTIONS
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Provided herein are compounds of Formula (I) and Formula (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.
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Page/Page column 246
(2021/04/02)
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- Preparation method 5- hydroxyl -7- azaindole (by machine translation)
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The invention discloses 5 -hydroxy- 7 7-azaindole preparation method, which takes 5 - X - 2 -nitropyridine as a raw material to react with benzyl alcohol sodium or sodium alkyl sodium alkoxide to generate 5 - R - 2 -nitropyridine, which is benzyl, methyl or ethyl X after being closed by a Grignard reagent ring after cyclization is carried, out, and ;R is high, yield. (by machine translation)
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- 5-methoxy-7-azaindole synthesis method
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The invention relates to a 5-methoxy-7-azaindole synthesis method, and provides a 5-methoxy-7-azaindole synthesis method, which comprises: a) preparing a compound 2 by using a compound 1 as a raw material; and b) preparing 5-methoxy-7-azaindole from the compound 2. Compared with the method in the prior art, the synthesis method of the present invention greatly shortens the synthesis route, effectively avoids the by-products in the prior art, and has increased total yield.
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- PROCESS FOR THE PREPARATION OF VENETOCLAX
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The present disclosure provides novel synthetic process for the preparation of venetoclax. The disclosed processes involve the use of novel intermediates. Processes for the preparation of these intermediates are also disclosed as well as methods for the preparation of particularly useful salts thereof.
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Page/Page column 31;32
(2018/03/06)
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- FAAH INHIBITORS
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The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the com
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Page/Page column 175-177
(2012/07/13)
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- AZAINDOLE GLUCOKINASE ACTIVATORS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
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Page/Page column 20
(2011/06/26)
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- COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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Page/Page column 37
(2008/12/06)
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- PYRROLO [2,3-B] PYRIDINES AS KINASE MODULATORS
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Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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Page/Page column 64-65
(2008/12/07)
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- JNK inhibitors
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The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neu
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Page/Page column 52
(2010/11/25)
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- Inhibitors of c-Jun N-terminal kinases for the treatment of neurodegenerative disorders relating to apoptosis and/or inflammation
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The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neu
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Page/Page column 51
(2010/11/26)
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- PYRROLO[2,3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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Page/Page column 122
(2010/11/25)
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- Synthesis of 7-azaserotonin: Its photophysical properties associated with excited state proton transfer reaction
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We report the synthesis of 3-(2-aminoethyl)-5-ol-1H-pyrrolo[2,3-b]pyridine (7-azaserotonin), which may potentially serve as an agonist or antagonist of serotonin receptors. In alcohols, the solvent (e.g., ethanol) catalyzed proton-transfer reaction takes place for 7-azaserotonin in the excited state, resulting in dual emission. Conversely, excited-state deprotonation takes place in neutral aqueous solution. The unique excitation behavior makes 7-azaserotonin versatile as a potential bioprobe. Copyright
- Wu, Pei-Wen,Hsieh, Wan-Ting,Cheng, Yi-Ming,Wei, Ching-Yen,Chou, Pi-Tai
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p. 14426 - 14427
(2008/01/27)
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- PPAR ACTIVE COMPOUNDS
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Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
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Page 158-159
(2008/06/13)
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- Preparation of 4-azaindole and 7-azaindole dimers with a bisalkoxyalkyl spacer in order to preferentially target melatonin MT1 receptors over melatonin MT2 receptors
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Several 4-azaindole and 7-azaindole dimer analogues of melatonin with a bisalkoxyalkyl spacer between the position 5 of each heterocycle were synthetized. Our aim was to investigate the influence of the spacers length on the selectivity of such compounds
- Larraya, Carlos,Guillard, Jerome,Renard, Pierre,Audinot, Valerie,Boutin, Jean A.,Delagrange, Philippe,Bennejean, Caroline,Viaud-Massuard, Marie-Claude
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p. 515 - 526
(2007/10/03)
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- Polycyclic azaindole compounds
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The invention relates to compounds of formula (I): wherein: G1represents an alkylene chain as defined in the description, A represents R2and R3represent hydrogen, alkyl, alkoxy or hydroxy or together form oxo, R4and R5represent hydrogen or together form aryl, R1is as defined in the description. and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.
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- Synthesis of new melatoninergic ligands including azaindole moiety
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A novel series of melatonin analogues, based on the azaindole nucleus is described. These compounds are prepared in several steps directly from the commercial available 7-azaindole or from substituted amino-, iodo- or/and nitropyridines using a catalysed palladium reaction or vicarious nucleophilic substitution of hydrogen (VNS) in order to elaborate the 6-, 5- and 4- azaindole derivatives respectively.
- Mazéas, Daniel,Guillaumet, Gérald,Viaud, Marie-Claude
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p. 1065 - 1080
(2007/10/03)
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