663955-59-7Relevant articles and documents
RET inhibitor, pharmaceutical composition comprising same and application of RET inhibitor and pharmaceutical composition in medicines
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, (2021/11/10)
The invention belongs to the field of medicines, and relates to an RET inhibitor, a pharmaceutical composition comprising the same and application of the RET inhibitor and the pharmaceutical composition in medicines. Specifically, the invention relates to
Photochemical Dual-Catalytic Synthesis of Alkynyl Sulfides
Santandrea, Jeffrey,Minozzi, Clémentine,Cruché, Corentin,Collins, Shawn K.
supporting information, p. 12255 - 12259 (2017/09/06)
A photochemical dual-catalytic cross-coupling to form alkynyl sulfides via C(sp)?S bond formation is described. The cross-coupling of thiols and bromoalkynes is promoted by a soluble organic carbazole-based photocatalyst using continuous flow techniques. Synthesis of alkynyl sulfides bearing a wide range of electronically and sterically diverse aromatic alkynes and thiols can be achieved in good to excellent yields (50–96 %). The simple continuous flow setup also allows for short reaction times (30 min) and high reproducibility on gram scale. In addition, we report the first application of photoredox/nickel dual catalysis towards macrocyclization, as well as the first example of the incorporation of an alkynyl sulfide functional group into a macrocyclic scaffold.
Design of α7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies
Ouach, Aziz,Pin, Frederic,Bertrand, Emilie,Vercouillie, Johnny,Gulhan, Zuhal,Mothes, Céline,Deloye, Jean-Bernard,Guilloteau, Denis,Suzenet, Franck,Chalon, Sylvie,Routier, Sylvain
, p. 153 - 164 (2015/11/18)
We report here the synthesis of a large library of 1,2,3-triazole derivatives which were in vitro tested as α7 nAchR ligands. The SAR study revealed that several crucial factors are involved in the affinity of these compounds for α7 nAchR such as a (R) quinuclidine configuration and a mono C-3 quinuclidine substitution. The triazole ring was substituted by a phenyl ring bearing small OMe/CH2F groups or fluorine atom and by several heterocycles such as thiophenes, furanes, benzothiophenes or benzofuranes. Among the 30 derivatives tested, the two derivatives 10 and 39 with Ki in the nanomolar range were identified (2.3 and 3 nM respectively). They exhibited a strict selectivity toward the α4β2 nicotinic receptor (up to 1 μM) but interacted with the 5HT3 receptors with Ki around 3 nM. Synthesis, SAR studies and a full description of the derivatives are reported.
1,4-DISUBSTITUTED 1,2,3-TRIAZOLES, METHODS FOR PREPARING SAME, AND DIAGNOSTIC AND THERAPEUTIC USES THEREOF
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Paragraph 0435; 0438, (2014/02/16)
A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; orX is a carbon atom and Y is a nitrogen atom;the Ar group is an aryl or heteroaryl group; andthe RN and RN′ groups, together with the carbon atoms
SUBSTITUTED QUINOLINES AND THEIR USE AS MEDICAMENTS
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Page/Page column 48, (2013/03/26)
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.
Substituted Quinolines and Their Use As Medicaments
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Paragraph 0113; 0114, (2013/03/26)
Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
Palladium-catalyzed coupling between aryl halides and trimethylsilylacetylene assisted by dimethylaminotrimethyltin
Cai, Liangzhen,Yang, Dujuan,Sun, Zhonghua,Tao, Xiaochun,Cai, Lisheng,Pike, Victor W.
, p. 1059 - 1062 (2012/01/04)
Palladium-catalyzed coupling between aryl halides, especially less reactive ones or N-heteroaryls, and trimethylsilylacetylene in the presence of dimethylaminotrimethyltin generated the coupled products in high yields. The reaction does not need CuI and base as auxiliary agents.
Synthesis of new 1-(2-, 3-, or 4-methanesulfonylphenyl)-2-[5-(N- hydroxypyridin-2(1H)-one)]acetylene regioisomers: A search for novel cyclooxygenase and lipoxygenase inhibitors
Chowdhury, Morshed A.,Chen, Hua,Abdellatif, Khaled R. A.,Dong, Ying,Petruk, Kenneth C.,Knaus, Edward E.
experimental part, p. 58 - 61 (2009/05/07)
A group of acetylene regioisomers were designed such that a cyclooxygenase-2 (COX-2) SO2Me pharmacophore was located at the ortho-, meta-, or para-position of the acetylene C-1 phenyl ring, and an iron-chelating 5-lipoxygenase (5-LOX) N-hydroxy
Synthesis and biological evaluation of 1-(benzenesulfonamido)-2-[5-(N-hydroxypyridin-2(1H)-one)]acetylene regioisomers: A novel class of 5-lipoxygenase inhibitors
Chowdhury, Morshed Alam,Chen, Hua,Abdellatif, Khaled R.A.,Dong, Ying,Petruk, Kenneth C.,Knaus, Edward E.
experimental part, p. 4195 - 4198 (2009/04/10)
A hitherto unknown class of linear acetylene regioisomers were designed such that a SO2NH2 group was located at the ortho-, meta-, or para-position of the acetylene C-1 phenyl ring, and a N-hydroxypyridin-2(1H)-one moiety was attached via its C-5 position to the C-2 position on an acetylene template (scaffold). All three regioisomers inhibited 5-lipoxygenase (5-LOX), where the relative potency order was 2-SO2NH2 (IC50 = 10 μM) >3-SO2NH2 (IC50 = 15 μM) >4-SO2NH2 (IC50 = 68 μM) relative to the reference drug nordihydroguaiaretic acid (NDGA; IC50 = 35 μM). The 2-SO2NH2 regioisomer (ED50 = 86.0 mg/kg po) exhibited excellent oral anti-inflammatory (AI) activity that was more potent than aspirin (ED50 = 128.9 mg/kg) and marginally less potent than ibuprofen (ED50 = 67.4 mg/kg). The N-hydroxypyridin-2(1H)one moiety provides a novel pharmacophore for the design of cyclic hydroxamic mimetics capable of chelating 5-LOX iron for exploitation in the design of 5-LOX inhibitory AI drugs.
3-‘4-HETEROCYCLYL -1,2,3,-TRIAZOL-1-YL!-N-ARYL-BENZAMIDES AS INHIBITORS OF THE CYTOKINES PRODUCTION FOR THE TREATMENT OF CHRONIC INFLAMMATORY DISEASES
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Page/Page column 76, (2008/06/13)
Disclosed compounds of formula (I), which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
