7519-36-0Relevant articles and documents
MACROCYCLIC FUSED PYRRAZOLES AS MCL-1 INHIBITORS
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Paragraph 0881, (2020/08/13)
Provided are compounds represented by Formula IA: (IA), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R 1a, R 1b, L 1, L 2, L 3, X, A, B and C are as defined as set forth
MACROCYCLIC INDOLES AS MCL-1 INHIBITORS
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Paragraph 1284-1285, (2020/06/10)
Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R1a, R1b, R1h, L1, L2, L3, ?, ?, ? are as defined as set forth in the specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.
BENZOTRIAZOLE-DERIVED AND UNSATURATED AMIDE COMPOUND USED AS TGF- R1 INHIBITOR
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Paragraph 0145; 0146, (2019/04/29)
A benzotriazole-derived α and β-unsaturated amide compound used as TGF-βR1 inhibitor or a pharmaceutically acceptable salt thereof, the structure of the compound being as shown in formula (I).
Focal adhesion kinase inhibitor and use
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Paragraph 0372; 0378; 0379, (2019/01/08)
The invention belongs to the field of medicines, relates to a focal adhesion kinase inhibitor and use, in particular relates to a novel focal adhesion kinase inhibitor compound, or stereoisomers, geometric isomers, tautomers, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, further relates to the use of the compound and pharmaceutical compositions as medicines, in particular the use of the compound and pharmaceutical compositions in manufacture of medicines for treatment or prevention of cancer, pulmonary hypertension, and pathological angiogenesis-related diseases.
Prolinimines: N-Amino- l -Pro-methyl Ester (Hydrazine) Schiff Bases from a Fish Gastrointestinal Tract-Derived Fungus, Trichoderma sp. CMB-F563
Mohamed, Osama G.,Khalil, Zeinab G.,Capon, Robert J.
supporting information, p. 377 - 380 (2018/01/27)
A rice cultivation of a fish gastrointestinal tract-derived fungus, Trichoderma sp. CMB-F563, yielded natural products incorporating a rare hydrazine moiety, embedded within a Schiff base. Structures inclusive of absolute configurations were assigned to prolinimines A-D (1-4) on the basis of detailed spectroscopic and C3 Marfey's analysis, as well as biosynthetic considerations, biomimetic total synthesis, and chemical transformations. Of note, monomeric 1 proved to be acid labile and, during isolation, underwent quantitative transformation to dimeric 3 and trimeric 4. Prolinimines are only the second reported natural products incorporating an N-amino-Pro residue, the first to include l-Pro, the first to occur as Schiff bases, and the first to be isolated from a microorganism.
FACTOR IXA INHIBITORS
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Page/Page column 78-79, (2014/08/19)
The present invention provides a compound of Formula (I) (structurally represented) wherein R1 is H or C1-6 alkyl, R2 is H or C1-6 alkyl or CH20H, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or-CH20H, and when R2, R3, and R4 are H, then R1 is C 1-6 alkyl; A is 1 ) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and 0, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with -CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or 0, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
N-nitrosation of secondary amines using p-TSA-NaNO2 as a novel nitrosating agent under mild conditions
Borikar, Sanjay P.,Paul, Vincent
experimental part, p. 654 - 660 (2011/02/27)
A combination of p-toluenesulfonic acid (p-TSA) and sodium nitrite was used as a novel effective nitrosating agent for the N-nitrosation of secondary amines to their corresponding nitroso derivatives under mild and heterogeneous conditions in moderate to excellent yields.
A divergent strategy to the withasomnines
Foster, Robert S.,Huang, Jianhui,Vivat, Jerome F.,Browne, Duncan L.,Harrity, Joseph P. A.
experimental part, p. 4052 - 4056 (2009/12/06)
A concise synthesis of three members of the withasomnine family of natural products is reported. The synthesis features a regioselective sydnone-alkynylboronate cycloaddition followed by Suzuki cross coupling and silyl group removal, and marks the first d
Stabilisation of peptide foldamers in an aqueous medium by incorporation of azapeptide building blocks
Hetenyi, Anasztazia,Toth, Gabor K.,Somlai, Csaba,Vass, Elemer,Martinek, Tamas A.,Fueloep, Ferenc
experimental part, p. 10736 - 10741 (2010/04/30)
Stable foldamers in water: Helical peptidic foldamers including H12 and H10/12 helices were constructed and stabilised in water. The foldamers' extra rigidity stems from the strong hydrogen bonding network of the azapeptide groups (see graphic).
Efficient procedure for chemoselective N-nitrosation of secondary amines with trichloromelamine-NaNO2
Bamoniri,Zolfigol,Mirjalili,Fallah
, p. 1393 - 1396 (2008/03/27)
A combination of trichloromelamine and sodium nitrite in the presence of wet silica gel was used as an effective nitrosating agent for the transformation of secondary amines into the corresponding N-nitroso derivatives under mild and heterogeneous conditions in good to excellent yields.