445468-63-3Relevant academic research and scientific papers
Intramolecular interactions in 2,6-pyridylacetylenes and their Co2(CO)4dppm complexes
Dana, Bogdan H,Robinson, Brian H,Simpson, Jim
, p. 251 - 269 (2002)
A series of 2,6-ethynylpyridyl compounds BrC5H3N(C2)R, C5H3N[(C2)R]2, C5H3N(C2SiMe3)(C2 R) R = H, Fc, {C5H3N-(C2SiMe 3)2} and {C5H3N[C2 C5H3N(C2SiMe3)]2} have been prepared in order to study through-space and through-bond interactions between the ethynyl arms. The structure of BrC5 H3N[FcC2Co2(CO)4dppm] shows that the C02-alkyne unit is preferentially distorted, rather than the ethynyl arms bent, in order to minimise steric interactions. Although, there is no evidence for through-bond or through-space electronic communication between the redox centres, intramolecular interactions force a η2(dppm)-η1(dppm) equilibrium upon the oxidised Co2(CO)4dppm unit, which is seen in the electrochemistry and OTTLE data.
1-CYANO-PYRROLIDINE DERIVATIVES AS DUB INHIBITORS
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Paragraph 0701-0702, (2020/11/30)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.
AgI-directed triple-stranded helicates with meta-ethynylpyridine ligands
Li, Qiaolian,Huang, Fu,Fan, Yaxun,Wang, Yilin,Li, Jianfeng,He, Yujian,Jiang, Hua
, p. 3235 - 3244 (2015/04/27)
A series of triple-stranded complexes, [1a3Ag]BF4, [1b3Ag]BF4, [2a3Ag2](BF4)2, [2b3Ag2](BF4)2, and [33Ag3/
AgI-directed triple-stranded helicates with meta-ethynylpyridine ligands
Li, Qiaolian,Huang, Fu,Fan, Yaxun,Wang, Yilin,Li, Jianfeng,He, Yujian,Jiang, Hua
, p. 3235 - 3244 (2014/07/22)
A series of triple-stranded complexes, [1a3Ag]BF4, [1b3Ag]BF4, [2a3Ag2](BF 4)2, [2b3Ag2](BF4) 2, and [33Ag3
Design of glycosyltransferase inhibitors: Pyridine as a pyrophosphate surrogate
Wang, Shuai,Cuesta-Seijo, Jose A.,Lafont, Dominique,Palcic, Monica M.,Vidal, Sebastien
supporting information, p. 15346 - 15357 (2013/11/06)
A series of ten glycosyltransferase inhibitors has been designed and synthesized by using pyridine as a pyrophosphate surrogate. The series was prepared by conjugation of carbohydrate, pyridine, and nucleoside building blocks by using a combination of gly
Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6- dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)
Watterson, Scott H.,Langevine, Charles M.,Van Kirk, Katy,Kempson, James,Guo, Junquing,Spergel, Steven H.,Das, Jagabandhu,Moquin, Robert V.,Dyckman, Alaric J.,Nirschl, David,Gregor, Kurt,Pattoli, Mark A.,Yang, Xiaoxia,McIntyre, Kim W.,Yang, Guchen,Galella, Michael A.,Booth-Lute, Hollie,Chen, Laishun,Yang, Zheng,Wang-Iverson, David,McKinnon, Murray,Dodd, John H.,Barrish, Joel C.,Burke, James R.,Pitts, William J.
scheme or table, p. 7006 - 7012 (2012/01/13)
The synthesis, structure-activity relationships (SAR), and biological results of pyridyl-substituted azaindole based tricyclic inhibitors of IKK2 are described. Compound 4m demonstrated potent in vitro potency, acceptable pharmacokinetic and physicochemical properties, and efficacy when dosed orally in a mouse model of inflammatory bowel disease.
PYRAZOLE[1,5a]PYRIDINE DERIVATIVES
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Page/Page column 56, (2010/07/09)
Pyrazolo[1,5-a]pyridine derivatives of formula I, wherein the meaning for R1, R2 and R3 is as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors.
Double elimination protocol for the synthesis of arylene ethynylenes containing heteroaromatic rings
Orita, Akihiro,Ye, Fangguo,Babu, Govindarajulu,Ikemoto, Tomohiro,Otera, Junzo
, p. 716 - 727 (2007/10/03)
The double elimination reaction of β-substituted sulfones offers a versatile strategy for synthesis of arylene ethynylene kits containing heteroaromatic rings. A sequence of aldol reaction between α-sulfonyl carbanion and aldehyde, trapping the resulting aldolate to give β-substituted sulfone, and double elimination of this intermediate can be integrated in one pot. This protocol allows thiophene, pyridine, and ferrocene units to be accommodated in phenylene ethynylene arrays.
Metal-assisted assembly of pyridine-containing arylene ethynylene strands to enantiopure double helicates
Orita, Akihiro,Nakano, Takehiro,An, De Lie,Tanikawa, Kazumi,Wakamatsu, Kan,Otera, Junzo
, p. 10389 - 10396 (2007/10/03)
Pyridine-containing arylene ethynylene strands were connected to the 2- and 2′-positions of (R)- and (S)-1,1′-binaphthyl templates. The arylene ethynylene moieties underwent intramolecular coordination with Ag(I) or Cu(I) ion to afford enantiopure double helicates. The double-helical structure was elucidated on the basis of circular dichroic (CD) spectra. The importance of intramolecular complexation of the double strands for the helicate formation was confirmed by comparison with a ligand bearing a single strand. Connection of the strands through an ether linkage enabled a sorting out of the Cotton effect induced by double-helical arylene ethynylene moieties. The CD exciton chirality method unambiguously proved that the termini of the strands approach each other upon complexation and that the sense of the induced helicity is the same as predicted by molecular modeling.
Double elimination protocol for access to pyridine-containing arylene-ethynylenes
Orita, Akihiro,Nakano, Takehiko,Yokoyama, Taisaku,Babu, Govindarajulu,Otera, Junzo
, p. 1298 - 1299 (2007/10/03)
The arylene-ethynylene arrays involving pyridine were constructed successfully by taking advantage of double elimination reaction of β-substituted sulfones (sulfoximines) which are easily accessible from arylmethyl sulfones (sulfoximines) and aromatic aldehydes. This protocol was utilized for synthesis of an enantiopure arylene-ethynylene framework bearing a binaphthyl stereogenic core.
