Category: 877151-43-4

On May 1, 2014, Papeo, Gianluca Mariano Enrico; Krasavin, Mikhail Yurievitch; Orsini, Paolo; Scolaro, Alessandra published a patent.Recommanded Product: 877151-43-4 The title of the patent was Preparation of carboxamido-isoindolinone derivatives as selective PARP-1 inhibitors. And the patent contained the following:

Provided are substituted 4-carboxamido-isoindolinone derivatives of formula I which selectively inhibit the activity of poly (ADP-ribose) polymerase (PARP-1) useful in the treatment of cancer, cardiovascular disease, central nervous system injury, and inflammation. I [wherein R is H or fluorine, when (a) n is 0 and m is 0, 1, 2, or 3 then R1 is 3- to 6-membered cycloalkyl or 4- to 6-membered heterocyclyl; and R2 is 3-, 5-, or 6-membered cycloalkyl, 4- to 6-membered heterocyclyl, or (hetero)aryl; (b) n is 1 and m is 0 then R1 is 3- to 6-membered cycloalkyl or aryl each which is optionally substituted; and R2 is null, 3- to 6-membered cycloalkyl, 4- to 6-membered heterocyclyl, (hetero)aryl, each which is optionally substituted; (c) n is 2 or 3 and m is 0 then R1 is 3- to 6-membered cycloalkyl, 4-to 6-membered heterocyclyl, or (hetero)aryl, each which is optionally substituted; and R2 is null, 3- to 6-membered cycloalkyl, 4- to 6-membered heterocyclyl, (hetero)aryl, each which is optionally substituted; (d) n and m are each independently 1, 2, or 3; R1 and R2 are independently 3- to 6-membered cycloalkyl, 4- to 6-membered heterocyclyl, or (hetero)aryl] or pharmaceutically acceptable salts thereof are claimed and exemplified. II was prepared in a multistep procedure (preparation given). I were assayed for antitumor activity in Capan-1 BRCA-2 mutated mouse model from which it was determined III exhibited tumor growth inhibition of 54% with no evidence of toxicity. The present invention also provides processes for preparing I and pharmaceutical compositions comprising I. The experimental process involved the reaction of Methyl 2-cyano-4-fluoro-6-methylbenzoate(cas: 877151-43-4).Recommanded Product: 877151-43-4

The Article related to carboxamidoisoindolinone derivative preparation parp inhibitor cancer inflammation cardiovascular disease, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 877151-43-4

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On February 23, 2006, Clayton, Joshua; Ma, Fupeng; Van Wagenen, Bradford; Ukkiramapandian, Radhakrishnan; Egle, Ian; Empfield, James; Isaac, Methvin; Slassi, Abdelmalik; Steelman, Gary; Urbanek, Rebecca; Walsh, Sally published a patent.COA of Formula: C10H8FNO2 The title of the patent was Preparation of isoindolones as metabotropic glutamate receptor potentiators. And the patent contained the following:

The title compounds I [R1 = (un)substituted 3-7 membered ring that may contain one or more heteroatoms selected from N, O and S; R2, R3 = H, alkyl, aryl, etc.; R4, R6 = H, OH, halo, etc.; R5 = H, halo, NO2, etc.; R7 = H, halo, NO2, etc.; R8, R9 = H, halo, NO2, etc.; or, where n is greater than 1, two or more R8 and/or R9 on adjacent carbons may be absent to form an alkenyl or alkynyl moiety], useful as metabotropic glutamate receptor modulators, particularly in neurol. and psychiatric disorders, were prepared E.g., a multi-step synthesis of II, was given. Generally, compounds I were active in assays described (e.g., mGluR2 assay) at concentrations (or with EC50 values) less than 10 μM. The pharmaceutical composition comprising the compound I is disclosed. The experimental process involved the reaction of Methyl 2-cyano-4-fluoro-6-methylbenzoate(cas: 877151-43-4).COA of Formula: C10H8FNO2

The Article related to isoindolone preparation metabotropic glutamate receptor potentiator mglur2, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C10H8FNO2

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On January 20, 2011, Papeo, Gianluca Mariano Enrico; Anatolievna Busel, Alina; Khvat, Alexander; Krasavin, Mikhail Yurievitch; Forte, Barbara; Zuccotto, Fabio published a patent.Quality Control of Methyl 2-cyano-4-fluoro-6-methylbenzoate The title of the patent was Preparation of 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamides as PARP inhibitors. And the patent contained the following:

The title compounds I [R = alkyl, alkenyl, alkynyl (each group substituted with one or more substituents selected from either NR3R4, Oalkyl, CO2alkyl and CONRaRb; wherein Ra, Rb = alkenyl, alkynyl, etc.; or NRaRb = (un)substituted heterocyclyl); R1 = H, halo, CN, NO2, etc.; R3, R4 = H, alkenyl, alkynyl, etc.; or NR3R4 = (un)substituted heterocyclyl] which selectively inhibit the activity of poly(ADP-ribose) polymerase PARP-1 with respect to poly(ADP-ribose) polymerase PARP-2, and therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation, were prepared and claimed. Thus, reacting 3-oxo-2-(piperidin-4-yl)-2,3-dihydro-1H-isoindole-4-carboxylic acid amide with 4,4-difluorocyclohexanone afforded the amide II. Exemplified compounds I were tested for their activity as PARP inhibitors (data given). The present invention also provides methods for preparing compounds I, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds The experimental process involved the reaction of Methyl 2-cyano-4-fluoro-6-methylbenzoate(cas: 877151-43-4).Quality Control of Methyl 2-cyano-4-fluoro-6-methylbenzoate

The Article related to oxoisoindolecarboxamide preparation parp inhibitor combination chemotherapy antitumor cardiovascular, central nervous system injury treatmentoxoisoindolecarboxamide preparation parp inhibitor, antiinflammatory isoindolecarboxamide oxo preparation parp inhibitor and other aspects.Quality Control of Methyl 2-cyano-4-fluoro-6-methylbenzoate

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts