- PROCESSES FOR FLUORINATION
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The present technology relates to fluorination reactions. Specifically, processes useful for making the fungicide compound, DFT are disclosed. More broadly, also disclosed herein are processes useful for deoxyfluorination at the α-aromatic position of a given compound.
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Paragraph 0179; 0184-0187; 0205
(2021/04/10)
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- NEW ANTI-MALARIAL AGENTS
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The present invention is related to new derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to dihydroisoquinoline derivatives useful for the preparation of a pharmaceutical for
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Paragraph 0198-0199
(2021/10/15)
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- PROCESSES FOR FLUORINATION
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The present technology relates to fluorination reactions. Specifically, processes useful for making the fungicide compound, DFT are disclosed. More broadly, also disclosed herein are processes useful for deoxyfluorination at the α-aromatic position of a given compound.
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Paragraph 0188
(2020/03/05)
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- Deoxyfluorination of (Hetero)aryl Aldehydes Using Tetramethylammonium Fluoride and Perfluorobutanesulfonyl Fluoride or Trifluoromethanesulfonic Anhydride
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This Communication describes the conversion of (hetero)aryl aldehydes into the corresponding (hetero)aryl difluoromethyl products using anhydrous NMe4F in combination with perfluorobutanesulfonyl fluoride or trifluoromethanesulfonic anhydride.
- Ferguson, Devin M.,Melvin, Patrick R.,Sanford, Melanie S.
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p. 398 - 401
(2019/09/06)
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- Room Temperature Deoxyfluorination of Benzaldehydes and α-Ketoesters with Sulfuryl Fluoride and Tetramethylammonium Fluoride
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A method for the room temperature deoxyfluorination of benzaldehydes and α-ketoesters using sulfuryl fluoride and Me4NF is described. A large scope of aryl and heteroaryl substrates is demonstrated, and this method compares favorably to other common deoxyfluorination methods for many substrates.
- Melvin, Patrick R.,Ferguson, Devin M.,Schimler, Sydonie D.,Bland, Douglas C.,Sanford, Melanie S.
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supporting information
p. 1350 - 1353
(2019/03/08)
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- 3-OXO-6-HETEROARYL-2-PHENYL-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES
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The present invention covers 3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyridazine- 4-carboxamide compounds of general formula (I): in which R1, R2, R4, R5, R6, X, Y and Z are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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Page/Page column 63; 64
(2019/06/11)
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- 2-HETEROARYL-3-OXO-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES FOR THE TREATMENT OF CANCER
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The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I), in which X, R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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Page/Page column 82
(2018/09/08)
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- Manufacturing method of making heteroarylacetic compd. defluoromethyl
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PROBLEM TO BE SOLVED: To provide a method for easily producing a difluoromethyl heteroaryl compound with high yield at low cost. SOLUTION: In the method for producing the difluoro methyl heteroaryl compound, a halogenated heteroaryl compound and a α-silyldifluoro acetate ester compound are reacted with each other in the presence of a metal halogenated compound. COPYRIGHT: (C)2012,JPOandINPIT
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Paragraph 0082-0084
(2018/10/03)
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- HETEROARYL SYK INHIBITORS
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The invention relates to new substituted heteroarylsof formula (1) wherein A is selected from the group consisting of N and CH, D is selected from the group consisting of S and O, E is C, T is C, G is C, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R1, M and R3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
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Page/Page column 37
(2015/11/10)
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- NOVEL 4-AMINO-6-(PYRIDYL AND 2-SUBSTITUTEDPHENYL)-PICOLINATES AND 6-AMINO-2-(PYRIDYL AND 2-SUBSTITUTEDPHENYL)-PYRIMIDINE-4-CARBOXYLATES AND THEIR USE AS HERBICIDES
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4-amino-6-(pyridyl and 2-substitutedphenyl)-picolinic acids and their derivatives; 6-amino-2-(pyridyl and 2-substitutedphenyl)-pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
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Paragraph 0257; 0258
(2014/09/29)
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- SYNERGISTIC PESTICIDAL COMPOSITIONS
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Synergistic pesticidal compositions including a pesticide/herbicide mixture are provided.
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-
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- SUBSTITUTED QUINOLINES AND THEIR USE AS MEDICAMENTS
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The invention relates to new substituted quinolines of formula (1) wherein R1 is a linear or branched C1-6-alkyl, wherein R1 may optionally be substituted by R3 which is selected from the group consisting of a three-, four-, five-, six- or seven-membered cycloalkl; a five-, six- or seven-membered, saturated heterocycle comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; and a five- or six-membered heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; wherein R3 may optionally be substituted further substituted as defined in claim 1 and wherein R2 is selected from the group consisting of halogen, phenyl, a five- or six-membered monocyclic heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; a bicyclic, nine-, ten- or eleven-membered, either aromatic or non-aromatic, but not fully saturated heterocycle comprising one, two, three or four heteroatoms each independently selected from the group consisting of N, S and O; wherein R2 may optionally be further substituted as defined in claim 1, and their use in the preparation of medicaments for the treatment of disease such as asthma, COPD, allergic rhinitis, allergic dermatitis and rheumatoid arthritis.
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Page/Page column 61
(2013/03/26)
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- Substituted Quinolines and Their Use As Medicaments
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Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
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Paragraph 0203; 0204
(2013/03/26)
-
- Novel Imidazole Derivatives Useful for the Treatment of Arthritis
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The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.
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Page/Page column 11
(2012/12/13)
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- Copper-mediated difluoromethylation of (hetero)aryl iodides and β-styryl halides with tributyl(difluoromethyl)stannane
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Owing to their unique properties, molecules containing the difluoromethyl group (CF2H) are of great interest. Tributyl(difluoromethyl)stannane has now been used for the selective and efficient direct ipso difluoromethylation of aryl iodides, he
- Prakash, G. K. Surya,Ganesh, Somesh K.,Jones, John-Paul,Kulkarni, Aditya,Masood, Kamil,Swabeck, Joseph K.,Olah, George A.
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supporting information
p. 12090 - 12094
(2013/01/16)
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- Stable insecticide compositions and methods for producing same
-
Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound exhibiting increased stability, along with methods for preparing same, are disclosed.
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Page/Page column 11
(2010/07/08)
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- Stable insecticide compositions
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Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound and an organic acid or a salt thereof exhibit increased stability.
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Page/Page column 11
(2010/07/08)
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- ANTHELMINTIC AGENTS AND THEIR USE
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This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the co
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Page/Page column 40
(2010/12/31)
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- INCREASING PLANT VIGOR
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Compositions and processes for improving plant vigor are disclosed.
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Page/Page column 13
(2009/02/11)
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- AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF
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Compounds are provided according to formula (1 ) : where A, B, W, X', L, R1, R3, R4b, and m' are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
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Page/Page column 58
(2009/10/22)
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- Insecticidal N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines
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N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.
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Page/Page column 13-14
(2010/11/28)
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- PYRIDYLMETHYLSULFONE DERIVATIVE
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Disclosed is a novel compound having an effect of inhibiting the production/secretion of β-amyloid protein. A compound represented by the general formula (1) or a salt or a solvate of the compound or the salt; and a pharmaceutical agent comprising the compound, salt or solvate.
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Page/Page column 168-169
(2008/06/13)
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