- PARG INHIBITORY COMPOUNDS
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The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
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Paragraph 00186; 00187
(2016/07/05)
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- 2-(N-Methylanilino)-2-phenylsulfanylacetonitrile, A Reagent Tested for Electrophilic, Nucleophilic, and Radical Reactions
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2-(N-Methylanilino)-2-phenylsulfanylacetonitrile 1 has been readily prepared from 2-(N-methylanilino)acetonitrile and diphenyl disulfide.Alkylation of the anion of 1 with halogenoalkanes resulted in concurrent elimination of benzenethiol to give conjugated α-aminoalkenenitriles of 2E-configuration.Autoxidation of 1 in the presence of alkoxide ions afforded alkyl N-methyl-N-phenylcarbamates.Nucleophilic substitution of 1 with Grignard reagent or appropriate silyl compounds were promoted by CuI or Lewis acids to give varied α-amino nitriles.The 4-oxo-2-aminonitriles 9 obtained by condensation of 1 and titanium enolates can be considered as derivatives of 1,3-dicarbonyl compounds with the aldehyde group being activated to give an amino nitrile umpolung.When 1 was treated with tributylstannane, the corresponding amino nitrile α-radical was formed and the self-coupling product was isolated.
- Chen, Chih-Cheng,Chen, Same-Ting,Chuang, Tsung-Hsun,Fang, Jim-Min
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p. 2217 - 2222
(2007/10/02)
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- Reduction et photoreduction de derives de l'acide carbonique influence de l'hexamethylphosphorotriamide
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Photoreduction and reduction of carbonic acid derivatives in HMPT have been compared.The highest yield of alkane was obtained from N,N-dimethylthiocarbamates either by the photochemical method or by reduction with a dissolved metal.Competitive reactions have been characterized: - during the photoreduction not only the alkane but products of a photo-Fries rearrangement and products of a homolytic cleavage were detected; - basic reactions can compete with the reduction of carbonic acid derivatives by sodium in HMPT.
- Dembele, Albert,Deshayes, Henri,Pete, Jean-Pierre
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p. 671 - 680
(2007/10/02)
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- NOVEL SYNTHESES OF ARYLCARBAMIC ESTERS FROM CARBON DIOXIDE AND AROMATIC AMINE VIA A ZINC CARBAMATE.
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Arylcarbamic esters were synthesized directly from carbon dioxide and an aromatic amine via a zinc carbamate. The alkylation of the reaction mixture of carbon dioxide, an aromatic amine, and diethylzinc with dialkyl sulfate formed alkyl arylcarbamate in a high yield. Also, 2-hydroxycyclohexyl diphenylcarbamate was obtained selectively in a good yield by the reaction of carbon dioxide, epoxycyclohexane, and ethylzinc diphenylamide. Other arylcarbamates of 1,2-cyclohexanediol were obtained by the reactions of carbon dioxide, an aromatic amine, diethylzinc, and epoxycyclohexane.
- Yoshida,Ishii,Kawato,Yamashita,Yano,Inoue
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p. 2913 - 2916
(2007/10/02)
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- Process for the production of blocked compounds optionally containing free hydroxyl groups and their use for the production of polyurethanes
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The present invention relates to a process for the production of compounds containing reversibly blocked and, optionally, free alcoholic hydroxyl groups, characterized in that organic compounds containing at least one alcoholic hydroxyl group, but otherwise being inert under the reaction conditions are reacted at 0° to 140° C. with N,N'-disubstituted 5-acylimino-imidazolidine diones. The present invention also relates to the use of these compounds for the production of polyurethanes.
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- EFFECT OF STRUCTURAL FACTORS ON THE KINETICS OF THE REACTION OF ALKYL CHLOROFORMATES WITH ALIPHATIC-AROMATIC AMINES
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As a result of investigation of the effect of the structure of the reagents on the kinetics of acylation of aliphatic-aromatic amines by alkyl chloroformates it was shown that the reaction takes place by an addition-elimination mechanism without a controlling stage.The kinetic data obey the two-parameter Taft equation.
- Orlov, S. I.,Chimishkyan, A. L.,Lapin, A. S.,Grabarnik, M. S.
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p. 1905 - 1908
(2007/10/02)
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- The Partitioning of the Tetrahedral Intermediate from the Basic Methanolysis of Ethyl N-Aryl-N-methylcarbamates
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The ratio of amine to methyl carbamate from the title reaction provides information on the relative nucleofugalities of some amines and the ethoxide anion, which is consistent with previously postulated mechanism for basic amide methanolysis.
- Broxton, Trevor J.,Deady, Lesle W.,Lim, Richard H. K.
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p. 1993 - 1996
(2007/10/02)
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- Process for separating selenium, selenium compounds, sulfur and/or sulfur compounds from polyurethanes containing these elements and/or compounds
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A process for separating selenium, selenium compounds, sulfur and/or sulfur compounds from urethanes containing these elements and/or compounds by reacting said urethanes with an aqueous permanganate solution and then separating the resulting phase system.
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- HYDROGENATION OF N-ARYL CARBAMATES TO N-ALICYCLIC CARBAMATES.
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An economical, high-yield process is developed for the preparation of pure N-alicyclic carbamates by the rhodium-catalyzed hydrogenation of the corresponding N-aryl carbamates. The N-aryl carbamates are obtained by the simple reaction of low-cost aromatic
- Malz Jr.,Greenfield
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p. 358 - 362
(2007/10/06)
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