On July 3, 2008, Adams, Ruth S.; Duffey, Matthew; Gould, Alexandra E.; Greenspan, Paul D.; Kulkarni, Bheemashankar A.; Vos, Tricia J. published a patent.Related Products of 887581-09-1 The title of the patent was Preparation of pyrazoline derivatives with Raf kinase inhibitory activity. And the patent contained the following:
The present invention provides certain pyrazoline compounds (shown as I; variables defined below; e.g. 2-[3-(pyridin-3-yl)-1-[[5-(pyridin-2-yl)-2-thienyl]carbonyl]-4,5-dihydro-1H-pyrazol-5-yl]phenol) useful as inhibitors of Raf kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of cancer. Semiquant. IC50 values for B-Raf kinase are reported for many examples of I. For I: R1 is a (un)substituted 5- or 6-membered N-containing heteroaryl ring, which ring optionally is fused to an aryl, heteroaryl, heterocyclyl, or cycloaliphatic ring, each of which is (un)substituted. R2 is a (un)substituted 5- or 6-membered aryl or heteroaryl ring, which ring optionally is fused to an aryl, heteroaryl, heterocyclyl, or cycloaliphatic ring, each of which is (un)substituted. R3 = H, fluoro, C1-4 aliphatic, and C1-4 fluoroaliph.; R4 is H, fluoro, or a C1-4 aliphatic or C1-4 fluoroaliph. (un)substituted, or R3 and R4, taken together with the C to which they are bound, form an (un)substituted 3- to 6-membered cycloaliphatic or 4- to 7-membered heterocyclic ring. L1 = -C(O)NRa(CRbRc)m-, -C(O)C(Rb):C(Rb)(CRbRc)m-, -C(O)(CRbRc)m-, and -SO2(CRbRc)m-, wherein the C(O) or SO2 functionality, resp., is bound to the N of the pyrazoline ring; Cy1 is a bivalent radical derived from a ring system = (un)substituted 5- or 6-membered aromatic rings having 0-4 ring N atoms and optionally 1-2 addnl. ring heteroatoms = O and S, which 5- or 6-membered aromatic ring optionally is fused to an aryl, heteroaryl, heterocyclyl, or cycloaliphatic ring, each of which is (un)substituted; et al. L2 is -(CRbRc)- or -(CRbRc)nX(CRbRc)n-; X = -O-, -C(O)-, -S-, -SO-, -SO2-, -NRa-, -C(Rf):C(Rf)-, -CC-, -NRaC(O)-, – C(O)NRa-, -SO2NRa, -NRaSO2-, and -NRaC(O)NRa-; Cy2 is a radical derived from a ring system = (un)substituted 5- or 6-membered aromatic rings having 0-4 ring N atoms and optionally 1-2 addnl. ring heteroatoms = O and S, which 5- or 6-membered aromatic ring optionally is fused to an aryl, heteroaryl, heterocyclyl, or cycloaliphatic ring, each of which is (un)substituted; et al; provided that R1 is not 6-bromo-1,2-dihydro-2-oxo-4-phenyl-3-quinolinyl; addnl. details are given in the claims. Although the methods of preparation are not claimed, preparations and/or characterization data for >400 examples of I are included. For example, 2-[3-(pyridin-3-yl)-1-[[5-(pyridin-2-yl)-2-thienyl]carbonyl]-4,5-dihydro-1H-pyrazol-5-yl]phenol was prepared in 3 steps (73, 94, and 72 % yields, resp.) starting from salicylaldehyde and 1-(pyridin-3-yl)ethanone and involving the following intermediates: (2E)-3-(2-hydroxyphenyl)-1-(pyridin-3-yl)prop-2-en-1-one and 2-[5-(pyridin-3-yl)-4,5-dihydro-1H-pyrazol-3-yl]phenol. The experimental process involved the reaction of (2-Bromo-5-methoxyphenyl)methanamine(cas: 887581-09-1).Related Products of 887581-09-1
The Article related to pyrazoline derivative preparation raf kinase inhibitor potential cancer drug, phenol pyrazolinyl preparation raf kinase inhibitor potential cancer drug, semicarbazone heterocyclic preparation raf kinase inhibitor potential cancer drug, alkylidenehydrazide heterocyclic preparation raf kinase inhibitor potential cancer drug and other aspects.Related Products of 887581-09-1
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Ether | (C2H5)2O – PubChem