4056-78-4Relevant articles and documents
Polycyclic amide derivative as CDK9 inhibitor, and preparation method and application thereof
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Paragraph 0265-0269, (2021/07/24)
The invention belongs to the technical field of polycyclic amide derivatives, and particularly relates to a polycyclic amide derivative as a CDK9 inhibitor, and a preparation method and application thereof. The polycyclic amide derivative shows excellent CDK9 enzyme inhibitory activity, and can be used for preparing drugs for treating cancers, especially hematologic cancers including acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, follicular lymphoma and the like and solid tumors, such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia and follicular lymphoma, including breast cancer, prostate cancer, ovarian cancer, hepatocellular carcinoma, pancreatic cancer, kidney cancer, stomach cancer, colorectal cancer, lung cancer and the like.
SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Page/Page column 179, (2012/11/07)
Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
Liquid-phase catalytic oxidation of C6-C7 cycloolefins into carboxylic acids in a pseudohomogeneous system
Alimardanov, Kh. M.,Sadygov,Garibov,Abbasov,Abdullaeva, M. Ya.,Dzhafarova
experimental part, p. 236 - 242 (2011/06/09)
Liquid-phase oxidation of cyclohexene, methylcyclohexene isomers, and norbornene with a 30% solution of hydrogen peroxide in a pseudohomogeneous system involving highly dispersed compounds of Group-VIb and -VIIIb metals supported by nanosize carbon particles was studied.
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N -{2-[4-(2-methoxyphenyl)piperazin-1-yl] ethyl}- N -(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor
Al Hussainy, Rana,Verbeek, Joost,Van Der Born, Dion,Braker, Anton H.,Leysen, Josée E.,Knol, Remco J.,Booij, Jan,Herscheid
supporting information; experimental part, p. 3480 - 3491 (2011/07/07)
Here we describe the design, synthesis, and pharmacological profile of 5-HT1A receptor ligands related to 1 (WAY-100635). The cyclohexyl moiety in 1 and its O-desmethylated analogue 3 were replaced by the bridgehead iodinated bridge-fused rings: adamantyl, cubyl, bicyclo[2.2.2]octyl, or bicyclo[2.2.1]heptyl. All analogues displayed a (sub)nanomolar affinity for the 5-HT1A receptor in vitro. Compounds 6b and 7b appeared to be selective for this receptor over other relevant receptors and could easily be iodinated with radioactive iodine-123. In humane hepatocytes, [ 123I]6b showed a low propensity for amide hydrolysis and a stable carbon-iodine bond. The biodistribution of [123I]6b and [ 123I]7b in rats revealed that the carbon-iodine bond was also stable in vivo. Unfortunately, the brain uptake and the specificity for both radioligands were significantly lower than those of the parent molecule 1. In conclusion, the designed tracers are not suitable for SPECT imaging.
Catalytic oxidative cleavage of olefins by RuO4 organic solvent-free under ultrasonic irradiation
Rup, Sandrine,Sindt, Michèle,Oget, Nicolas
scheme or table, p. 3123 - 3126 (2010/08/07)
All the works reported about oxidative cleavage of olefins by the RuCl3/NaIO4 catalytic system have been performed in biphasic water/organic solvent(s). The first organic solvent-free oxidation of C{double bond, long}C double bond by 2% RuCl3/4.1 equiv NaIO4/H2O is described here using both the emulsifier Aliquat 336 and 20 kHz ultrasonic irradiation.
HETEROBICYCLIC METALLOPROTEASE INHIBITORS
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Page/Page column 167, (2008/06/13)
The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.
Ruthenium catalysed oxidation without CCl4 of oleic acid, other monoenic fatty acids and alkenes
Zimmermann, Fran?ois,Meux, Eric,Mieloszynski, Jean-Luc,Lecuire, Jean-Marie,Oget, Nicolas
, p. 3201 - 3203 (2007/10/03)
Ruthenium catalysed oxidation of alkenes and monoenic fatty acids is reported. The study of the influence of cosolvents (H2O/MeCN/X) shows that toxic CCl4 initially used in the Sharpless system (H 2O/MeCN/CCl4) can be avoided and demonstrates that the oxidative cleavage of CC bond could be accomplished in good yields with H 2O/MeCN/AcOEt solvent system in a ratio 3/2/2, respectively.
Synthesis of Bridgehead-Bridgehead Substituted Bicycloalkanes
Della, Ernest W.,Tsanaktsidis, John
, p. 1705 - 1718 (2007/10/02)
A convenient synthetic route to several bicycloalkanes bearing substitution at both bridgehead positions is described.The two-step procedure, which involves alkylation of the monoenolates of readily available cyclohexane diesters with 1,2-dihaloethane followed by a base-inducted cyclization of the derived haloethylated product, was successfully applied to the synthesis of dimethyl bicyclooctane-1,4-dicarboxylate, dimethyl bicycloheptane-1,4-dicarboxylate and dimethyl bicyclooctane-1,5-dicarboxylate.Additionally, it was found that the two latter diesters could be obtained in quite acceptable yields in a one-pot procedure through their corresponding cyclohexyl bisenolate precursors.
1,1-Alkanediol dicarboxylate linked antibacterial agents
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, (2008/06/13)
Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula STR1 where A is the residue of certain dicarboxyic acids, R3 is H or (C1 -C3), n is zero or 1 such that when n is zero R is P or B and R1 is the residue of certain esters, H or a salt thereof; and when n is 1, one of R and R1 is P and the other is B, and P is STR2 where R2 is H or certain acyl groups, and B is the residue of a beta-lactamase inhibiting carboxylic acid; a method for their use, pharmaceutical compositions thereof and intermediates useful in their production.