27258-32-8Relevant articles and documents
THIENO[3,2-B] PYRROLE[3,2-D]PYRIDAZINONE DERIVATIVES AND THEIR USE AS PKM2 DERIVATIVES FOR THE TREATMENT OF CANCER, OBESITY AND DIABETES RELATED DISORDERS
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Page/Page column 104, (2020/08/28)
Described herein are compounds that regulate pyruvate kinase activity, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I) wherein R2, L1-L2, U1-U7, m, ring A, and Q are as defined herein.
Pyrazolopyridine compound and use thereof
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Paragraph 0420; 0422; 0423, (2018/11/03)
The present invention relates to a pyrazolopyridine compound and use thereof, and further relates to a pharmaceutical composition comprising the pyrazolopyridine compound. The pyrazolopyridine compound or the pharmaceutical composition can be used as a so
Synthesis of trans-disubstituted pyrazolylcyclopropane building blocks
Nosik, Pavel S.,Ryabukhin, Sergey V.,Artamonov, Oleksiy S.,Grygorenko, Oleksandr O.
, p. 1629 - 1636 (2016/08/16)
Diastereoselective synthesis of trans-disubstituted pyrazolylcyclopropane building blocks (i.e. carboxylic acids and amines) is described starting from easily available pyrazolecarbaldehydes. The key step of the synthesis was Corey–Chaikowsky cyclopropanation of the corresponding α,β-unsaturated Weinreb amides. The title compounds were prepared in four or six steps and 32–60 and 17–40?% overall yields, respectively, on up to 50?g scale. The building blocks obtained are good starting points for the design of lead-like libraries; they themselves can be considered as isosteric analogs of CNS-active drug tranylcyclopropamine. Graphical abstract: [Figure not available: see fulltext.]
Method for the Production of N-Substituted (3-Dihalomethyl-1-Methyl-Pyrazole-4-yl) Carboxamides
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Page/Page column 16, (2010/07/10)
The present invention relates to a process for preparing N-substituted (3-dihalomethylpyrazol-4-yl)carboxamides of the formula (I) in which R1 is optionally substituted phenyl or C3-C7-cycloalkyl, R1a is hydrogen or fluorine, or R1a together with R1 is optionally substituted C3-C5-alkanediyl or C5-C7-cycloalkanediyl, R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C4-alkoxy-C1-C2-alkyl, X is F or Cl and n is 0, 1, 2 or 3; which comprises A) providing a compound of the formula (II) in which X is F or Cl, Y is Cl or Br and R2 has one of the meanings given above and B) reacting a compound of the formula (II) with carbon monoxide and a compound of the formula (III) in which R1, R1a and n have one of the meanings given above; in the presence of a palladium catalyst; to intermediates used for the preparation according to the process according to the invention, and also to processes for their preparation.
First copper-catalyzed intramolecular amidation in substituted 4-iodopyrazoles leading to the synthesis of pyrazolo [4,3-b] pyridin-5-onesn
Nag, Somnath,Nayak, Maloy,Batra, Sanjay
supporting information; body text, p. 2715 - 2723 (2010/01/15)
An unprecedented copper-catalyzed intramolecular amidation of substituted 4-iodopyrazoles generated either via Baylis-Hillman or Horner-Wadsworth-Emmons chemistry for the synthesis of pyrazolo[4,3-b]pyridine-5-ones is described. In addition, the effect of
4(SPIROPIPERIDINYL)METHYL SUBSTITUTED PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Page 39-40, (2010/02/07)
3-Substituted pyrrolidines having a spiropiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
4-[(4-(CARBOXYETHYL) PIPERIDINYL) METHYL] PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Page 31; 24, (2010/02/07)
3-Substituted pyrrolidines having a 4-carboxypiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.