209858-74-2Relevant articles and documents
Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3 H-1,2,4-triazol-3-one, by Fragment-Based Drug Design
Sabat, Mark,Dougan, Douglas R.,Knight, Beverly,Lawson, J. David,Scorah, Nicholas,Smith, Christopher R.,Taylor, Ewan R.,Vu, Phong,Wyrick, Corey,Wang, Haixia,Balakrishna, Deepika,Hixon, Mark,Madakamutil, Loui,McConn, Donavon
supporting information, p. 12893 - 12902 (2021/09/13)
This publication details the successful use of FBDD (fragment-based drug discovery) principles in the invention of a novel covalent Bruton's tyrosine kinase inhibitor, which ultimately became the Takeda Pharmaceuticals clinical candidate TAK-020. Describe
PYRIDINYL AND FUSED PYRIDINYL TRIAZOLONE DERIVATIVES
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Paragraph 0469-0470, (2014/09/29)
Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.
SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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, (2011/02/24)
Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
N-(phenylsulfonyl)picolinamide derivatives, process for producing the same, and herbicide
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, (2008/06/13)
A herbicide containing as the active ingredient an N-(henylsulfonyl)picolinamide derivative represented by general formula (I) wherein X reprcsents a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, a C1-4 haloalkoxy, a (C1-4 alkoxy)carbonyl, a [di(C1-4 alkyl)amino]sulfonyl, an [N—(C1-4 alkyl)-N—(C1-4 alkoxy)amino]sulfonyl, a (C1-4 alkylamino)sulfonyl, a C1-4 alkylthio, a C1-4 alkylsulfinyl, a C1-4 alkylsulfonyl, or nitro; n is an integer of 0 to 5; Y represets a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, C1-4 haloalkoxy, a C1-4 alkylthio, a C1-4 haloalkylthio, amino, a C1-4 alkylamino, a di(C1-4 alkyl)amino, a (C1-4 alkoxy) C1-4 alkyl, a (C1-4 alkylthio) C1-4 alkyl, or nitro; and m is an integer of 0 to 4. This active ingredient is synthesized by condensing a substituted picolinic acid with a substituted benzenesulfonamide under dehydration, or by reacting the phenyl ester of a substituted picolinic acid with a substituted benzenesulfonamide in the presence of a basic compound.
6-(Nonsubstituted or substituted) phenoxy picolinic acids, process of preparing the same, and agricultural/horticultural germicides containing the same
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, (2008/06/13)
An agricultural or horticultural fungicide containing 6-(unsubstituted or substituted) phenoxy picolinic acid represented by the general formula (I), as an effective ingredient. wherein R is a halogen atom, a C1to C4alkyl group, a C1to C4haloalkyl group, a C1to C4alkoxy group, a C1to C4haloalkoxy group, a C1to C4alkylthio group, a C1to C4alkylamino group, a di(C1to C4alkyl)amino group or a C7to C8aralkyl(C1to C4alkyl)amino group; n2is an integer of 0 to 3; Y is a C1to C4alkyl group, a C1to C4haloalkyl group, a C1to C4alkoxy group, a C1to C4haloalkoxy group, a C1to C4alkylthio group, a C1to C4haloalkylthio group or a halogen atom; and m is an integer of 0 to 5, and when m and n2are not less than 2, Rs and Ys may be the same or different, respectively. The compound is useful as an effective ingredient of agricultural or horticultural fungicides.
6-phenoxy picolinic acid alkylidene hydrazide derivative, process for producing the same and herbicide using the same
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, (2008/06/13)
PCT No. PCT/JP98/02842 Sec. 371 Date Feb. 23, 2000 Sec. 102(e) Date Feb. 23, 2000 PCT Filed Jun. 25, 1998 PCT Pub. No. WO99/00370 PCT Pub. Date Jan. 7, 1999A 6-phenoxy picolinic acid alkylidene hydrazide derivative, a process for producing the derivative and a herbicide containing the derivative as an effective ingredient. Such a compound is a novel compound and is useful as an effective ingredient of herbicides.
Herbicidal picolinamide derivatives
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, (2008/06/13)
Herbicidal picolinamide derivatives are provided having the formula I STR1 which Z represents an oxygen or sulphur atom, R1 and R2 each independently represents a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, alkaryl, hydroxy, alkoxy, alkenyloxy, alkynyloxy, alkylcarbonyl, amino, mono- or di-alkylamino, alkoxycarbonylamino, arylamino, arylalkylamino or dialkylcarbamoyl group, or together represent an alkylene chain which is optionally interrupted by an oxygen or sulphur atom or by a group --NR-- in which R represents a hydrogen atom or an alkyl group, R3 independently represents a halogen atom or an alkyl or haloalkyl group, R4, R5 and R6 each independently represents a hydrogen or halogen atom, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, alkaryl, alkoxy, amino, mono- or di-alkylamino, alkoxycarbonylamino, arylamino, dialkylcarbamoyl, acyl or acylamido group or a cyano group, with the proviso that R5 and R6 do not represent an acyl, acylamido or cyano group, and n represents 0, 1, 2 or 3.