- Copper-Catalyzed N1 Coupling of 3-Aminoindazoles and Related Aminoazoles with Aryl Bromides
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The N1-selective arylation of 3-aminoindazoles using copper catalysis is herein reported. The reaction uses readily accessible aryl bromides as coupling partners, including those from heterocycles, and allows easy access to a broad variety of substituted 3-aminoindazoles. The methodology was also examined on other aminoazoles of interest for the pharmaceutical industry.
- Cyr, Patrick,Joseph-Valcin, Eve-Marline,Boissarie, Patrick,Simoneau, Bruno,Marinier, Anne
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supporting information
(2021/12/02)
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- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
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Page/Page column 100
(2020/01/31)
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- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
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Page/Page column 174-175
(2020/07/31)
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- SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME
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ABSTRACT The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.
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Page/Page column 135; 136
(2016/09/15)
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- ANTI-INFECTIVE COMPOUNDS
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The present invention relates to small molecule compounds having the general formula (I): wherein A is a moiety selected from the group consisting of formulae (A) to (K) and their use in the treatment of bacterial infections, in particular Tuberculosis.
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Page/Page column 53
(2016/06/28)
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- Copper(I)/Copper(II)-Assisted Tandem Catalysis: The Case Study of Ullmann/Chan-Evans-Lam N1,N3-Diarylation of 3-Aminopyrazole
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Unprecedented CuI/CuII-assisted tandem catalysis allowing an Ullmann/Chan-Evans-Lam sequence was achieved. This three-component, one-pot reaction triggered by a change in the oxidation state of the metal leads to the selective N1,N3-diarylation of 3-aminopyrazole. This new method should be a valuable tool for small-molecule drug discovery that requires suitable regio- and/or chemoselective strategies for the N-arylation of nitrogen-containing heterocycles. Tandem power: The first assisted tandem copper-catalyzed process, triggered by a change in the oxidation state of the metal, is developed to allow a one-pot Ullman/Chan-Evans-Lam sequence leading to the selective N1,N3-diarylation of 3-aminopyrazole.
- Beyer, Astrid,Castanheiro, Thomas,Busca, Patricia,Prestat, Guillaume
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p. 2433 - 2436
(2015/08/24)
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- HETEROCYCLIC COMPOUNDS AND USE OF SAME
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Novel heterocyclic compounds are provided which display useful efficacy in the treatment of diseases caused by trypanosomatids. Particularly, the compounds of the invention are useful in the treatment of HAT and/or Chagas disease and/or Animal African trypanosomiasis (AAT).
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Paragraph 00225
(2016/01/08)
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- PYRAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF
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The present invention provides a pyrazole compound of the following general Formula [1b] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use wherein each symbol is the same as defined in the description
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Paragraph 0680; 0681; 0682
(2013/04/13)
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- Regiocontrolled synthesis of 3- and 5-aminopyrazoles, pyrazolo[3,4-d] pyrimidines, pyrazolo[3,4-b]pyridines and pyrazolo[3,4-b]quinolinones as MAPK inhibitors
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Microwave irradiation of a hydrazine and 3-methoxyacrylonitrile, ethoxymethylenemalononitrile or ethyl acetoacetate provides rapid access to 3- or 5-substituted pyrazoles in excellent yield and with total regiocontrol in a process that can be switched from one regioisomer to the other by choice of conditions. Subsequent reaction, either by microwave-assisted hydrolysis and cyclocondensation with formamide, Hantzsch-type three-component reaction with an aldehyde and ketone, or by cyclocondensation with 2-nitrobenzaldehyde, provides the pyrazolo[3,4-d]pyrimidine, pyrazolo[3,4-b]pyridine or pyrazolo[3,4-b] quinolin-4-one framework, respectively, of inhibitors of mitogen-activated protein kinases.
- Bagley, Mark C.,Baashen, Mohammed,Paddock, Victoria L.,Kipling, David,Davis, Terence
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p. 8429 - 8438
(2013/09/02)
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- Platinum complex and light-emitting device
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A platinum complex represented by the general formula (1) below, useful as a phosphorescence emission material, a tetradentate ligand useful for synthesizing the platinum complex, and a light-emitting device containing at least one of the platinum complex
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- Bicyclic heterocycles as cannabinoid receptor modulators
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds a
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Page/Page column 9
(2008/06/13)
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- PROCESS FOR MAKING PYRAZOLE COMPOUNDS
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This invention relates to a process for making pyrazole compoundsof formula I.
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- Long-acting fentanyl analogues: synthesis and pharmacology of N-(1-phenylpyrazolyl)-N-(1-phenylalkyl-4-piperidyl)propanamides.
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The synthesis of new fentanyl analogues in which the benzene ring of the propioanilido group has been replaced by phenylpyrazole is described. Antinociceptive activity was evaluated using the writhing and hot plate tests in mice. Two compounds, and, showe
- Jagerovic, Nadine,Cano, Carolina,Elguero, Jose,Goya, Pilar,Callado, Luis F,Meana, J Javier,Giron, Rocio,Abalo, Raquel,Ruiz, David,Goicoechea, Carlos,Martin, M A Isabel
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p. 817 - 827
(2007/10/03)
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- Substituted 1H-pyrazolo (1,5-a) pyrimidines and process for their preparation
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Compounds of general formula (I) STR1 wherein R1 is a 2-pyridyl, 3-pyridyl or 4-pyridyl group; (b) a phenyl ring, unsubstituted or substituted by one or two groups chosen from halogen, trihalo-C1 -C4 alkyl, C1 -
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- Aminopyrazoles. III. Novel "One-Flask" Preparation of 1-Phenylpyrazol-3-amine
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2-Chloroacrylonitrile (1a), 2,3-dichloropropanenitrile (1b), 2,3-dibromopropanenitrile (1c) or 3-chloroacrylonitrile (1d) react with phenylhydrazine (2) in the presence of potassium t-butoxide with the formation of 1-phenylpyrazol-3-amine (3) free of the 5-amino isomer.
- Ege, Guenter,Franz, Hermann
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p. 1265 - 1266
(2007/10/02)
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- Process for preparing 1-phenyl-3-aminopyrazoles
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1-PHENYL-3-AMINO-2-PYRAZOLINES ARE CATALYTICALLY OXIDIZED TO 1-PHENYL-3-AMINOPYRAZOLES, USING OXYGEN AND/OR AIR AS THE OXIDIZING AGENT AND IN THE PRESENCE OF COPPER SALTS, OPTIONALLY ASSOCIATED WITH METALLIC COPPER AND/OR AN AROMATIC, HETEROCYCLIC ORGANIC
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