16205-46-2Relevant articles and documents
Discovery of potent colony-stimulating factor 1 receptor inhibitors by replacement of hinge-binder moieties
Lee, Jung Wuk,Park, Jiwon,Kim, Jina,Kim, Jihyung,Choi, Changyu,Min, Kyung Hoon
, (2021/03/14)
Tumor-associated macrophages (TAMs) are predominantly associated with tumor growth. Colony-stimulating factor 1 receptor (CSF1R) acts as a key regulator of TAM survival and differentiation and is a molecular target for cancer therapies. Herein, novel CSF1
Azacycle diketone compound and preparation method thereof (by machine translation)
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Paragraph 0550-0553; 0556-0557, (2020/09/12)
The invention provides a azacyclodiketone compound which is characterized by being a compound represented by the following structure. The compound has inhibitory activity on cap-dependent endonuclease. (by machine translation)
2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof
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Paragraph 0197; 0742; 0745-0746, (2020/03/03)
The invention relates to 2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof. Specifically, the invention discloses the compounds represented by a formula (I) shown in the specification, enantiomers, diastereomers, racemates or a mixture of the compounds, or a pharmaceutically acceptable salt, hydrate and solvate of the compounds, a preparation method of the above materials, and applications of the above materials in preparation of an ASK1 small molecule inhibitor, or medicines for preventing and/or treating diseases related to ASK1, especially liver diseases, lung diseases, cardiovascular diseases, kidney diseases and metabolic diseases.
Synthesis of pyrazol [1,5-alpha] pyridine-3-carboxylic acid derivatives
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Paragraph 0064; 0082; 0083; 0084, (2019/02/04)
The invention relates to synthesis of pyrazol [1,5-alpha] pyridine-3-carboxylic acid derivatives, and belongs to the field of organic synthesis. Trimethylsulfonyl chloride is used as a raw material toreact with tert-butoxycarbonyl hydroxylamine to obtain a compound 3; then the compound 3 reacts with trifluoroacetic acid to obtain a mixed solution of a compound 4; the mixed solution directly reacts with pyrazine to obtain a compound 6 without carrying out separation, washing and drying; an ethyl propiolate reaction is continuously performed; a water phase obtained after the reaction is extracted by ethyl acetate; an organic extract obtained after extraction is dried by anhydrous MgSO4 and evaporated; remaining residues are subjected to recrystallization (ethyl acetate, methylbenzene or petroleum ether), separation, washing and drying to obtain a compound 8; the compound 8 further reacts with NaOH to obtain a compound 9. In the route, the second step and the third step are continuouslycarried out, so that not only is the risk of the process reduced, but also yield is over 70%. No matter whether the raw material is of a symmetrical structure, the target product can be accurately obtained. The synthesis is suitable for industrial production.
Development of Structurally Diverse N-Heterocyclic Carbene Ligands via Palladium-Copper-Catalyzed Decarboxylative Arylation of Pyrazolo[1,5-a]pyridine-3-carboxylic Acid
Alam, Khyarul,Kim, Seong Min,Kim, Do Joong,Park, Jin Kyoon
supporting information, p. 2661 - 2670 (2016/08/31)
A series of fused non-classical normal N-heterocyclic carbenes, Pyrpy-NHC precursors derived from pyrazolo[1,5-a]pyridines, has been prepared using palladium-copper-catalyzed decarboxylative arylation of pyrazolo[1,5-a]pyridine-3-carboxylic acid. Air-stable palladium and rhodium complexes of these ligands have been synthesized via mild transmetallation of Ag-Pyrpy-NHC. The structural properties of Rh(Pyrpy-NHC)(COD)Cl complexes were determined via X-ray analysis. The measurement of the CO stretching frequencies of dicarbonyl Rh-Pyrpy-NHC complexes revealed that the electron donating strength of Pyrpy-NHC could be tuned by varying the substituents of the aryl group. A catalytic study of the Pd-Pyrpy-NHC complexes revealed promising activity in the Suzuki–Miyaura reaction under ambient atmospheric conditions. (Figure presented.).
PYRAZOLE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 99, (2011/09/19)
New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
PYRAZOLE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS
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Page/Page column 89, (2010/04/27)
The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10- alkenyl, C2-C10-alkynyl, etc.; n is 0 to 4; or two radicals Rpx bound to the same ring- member may form an oxo substituent, or two radicals Rpx bound to adjacent ring- members may form a 3- to 7-membered fused cyclic radical; B is N or CR4, wherein R4 is H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkyl, etc.; X2 is O2a, NR2bR2c or S(O)mR2d, wherein m is 0, 1 or 2; R2a is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R1 is H, CN, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, etc.; R2, R3 and R5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material comprising at least one compound of formulae I or II, to a method for treating or protecting an animal from infestation or infection by parasites, to novel pyrazole compounds of formulae I or Il and agricultural composition containing those compounds.
Azaindole Derivatives with High Affinity for the Dopamine D4 Receptor: Synthesis, Ligand Binding Studies and Comparison of Molecular Electrostatic Potential Maps
Loeber, Stefan,Huebner, Harald,Gmeiner, Peter
, p. 97 - 102 (2007/10/03)
Piperazinylmethyl substituted pyrazolopyridines and related heterocycles were synthesized and found to recognize selectivity the dopamine D4 receptor. For the most potent derivative 10d a Ki value of 2.0 nM was observed. SAR studies including the comparison of molecular isopotential surfaces were performed.
Pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives and their pharmaceutical use
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, (2008/06/13)
Described herein are pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives represented by the following formula (I): STR1 wherein R 1 and R 2 individually mean a hydrogen atom or a lower alkyl group, R 3 denotes an azabicyclo group containing a tertiary nitrogen atom, and Y stands for --O-- or --NH--, or salts thereof. Their preparation process and serotonin receptor antagonists containing them as active ingredients are also described.
1,3-Dipolar Addition of Pyridine N-Imine to Acetylenes and the Use of C-13 NMR in Several Structural Assignments
Anderson, Paul L.,Hasak, James P,Kahle, Alicia D.,Paolella, Nicholas A.,Shapiro, Michael J.
, p. 1149 - 1152 (2007/10/02)
Addition of pyridine-N-imine to a variety of acetylenic mono- (Scheme I) and di- (Scheme II) carboxylic ester dipolarophiles was carried out.Several of the 3-azapyrrocoline esters obtained were further converted into acids, amides and hydrazides as shown in Schemes I and II.
