- Continuous synthesis method for substituted benzoic acid organic matter
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The invention provides a continuous synthesis method for a substituted benzoic acid organic matter. The continuous synthesis method comprises the following steps: in the presence of a catalyst and anorganic solvent, continuously putting an organic matter of a formula (I) shown in the specification, and oxygen into a continuous reaction device, carrying out a continuous oxidation reaction so as toobtain the substituted benzoic acid organic matter, and continuously discharging the substituted benzoic acid organic matter, wherein the substituted benzoic acid organic matter is of a structure ofa formula (II) shown in the specification. Oxygen is a green reagent and is cheap and easy to obtain, a great amount of wastes are not generated after reactions are completed, and the system is easy to treat. Due to continuous reaction operation, the risk that the solvent has flash evaporation explosion because of high-concentration oxygen in in-batch reactions can be reduced. Under same oxidationconditions, due to a continuous preparation process, escape of oxygen can be reduced, the utilization rate of oxygen can be greatly increased, operation can be also simplified, the security of reactions can be improved, and the yield of the substituted benzoic acid organic matter can be increased.
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Paragraph 0067-0069; 0138
(2019/10/01)
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- HISTONE DEACETYLASE INHIBITORS
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The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
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Page/Page column 13; 14
(2012/05/04)
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- HISTONE DEACETYLASE INHIBITORS
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The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
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Page/Page column 38
(2011/04/13)
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- 4- (4- (IMIDAZOL-4-YL) PYRIMIDIN-2-YLAMINO) BENZAMIDES AS CDK INHIBITORS
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Compounds of the formula: (I): wherein variable groups are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
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Page/Page column 80
(2008/06/13)
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- INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
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The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras
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- Method of treating cancer
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The present invention relates to methods of treating cancer using a combination of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase. The invention also relates to methods of preparing such compositions.
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- Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents
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A series of novel diaryl ether lactams have been identified as very potent dual inhibitors of protein farnesyltransferase (FTase) and protein geranylgeranyltransferase I (GGTase-I), enzymes involved in the prenylation of Ras. The structure of the complex formed between one of these compounds and FTase has been determined by X-ray crystallography. These compounds are the first reported to inhibit the prenylation of the important oncogene Ki-Ras4B in vivo. Unfortunately, doses sufficient to achieve this endpoint were rapidly lethal.
- DeSolms, S. Jane,Ciccarone, Terrence M.,MacTough, Suzanne C.,Shaw, Anthony W.,Buser, Carolyn A.,Ellis-Hutchings, Michelle,Fernandes, Christine,Hamilton, Kelly A.,Huber, Hans E.,Kohl, Nancy E.,Lobell, Robert B.,Robinson, Ronald G.,Tsou, Nancy N.,Walsh, Eileen S.,Graham, Samuel L.,Beese, Lorena S.,Taylor, Jeffrey S.
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p. 2973 - 2984
(2007/10/03)
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to compounds which inhibit a prenyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting a prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to compounds which inhibit prenyl-protein transferase and particularly, the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this in
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- Diaryl ether inhibitors of farnesyl-protein transferase
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Imidazolemethyl diaryl ethers are potent inhibitors of farnesyl-protein transferase. The SNAr displacement reaction used to prepare these diaryl ethers was amenable to rapid parallel synthesis of FPTase inhibitors. The use of a broad range of c
- MacTough, Suzanne C.,Desolms, S. Jane,Shaw, Anthony W.,Abrams, Marc T.,Ciccarone, Terrence M.,Davide, Joseph P.,Hamilton, Kelly A.,Hutchinson, John H.,Koblan, Kenneth S.,Kohl, Nancy E.,Lobell, Robert B.,Robinson, Ronald G.,Graham, Samuel L.
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p. 1257 - 1260
(2007/10/03)
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- 4-benzoyl isoxazoles and their use as herbicides
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The invention relates to 4-benzoylisoxazoles having the formula: STR1 wherein: R is hydrogen or --CO2 R5 ; R1 is alkyl, cyclopropyl or 1-methylcyclopropyl; R2 is chlorine, bromine, optionally substituted alkyl,
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- Processes for preparing ortho-substituted benzoic acids
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A novel process for the synthesis of ortho-substituted benzoic acid by lithiating an unprotected benzoic acid and a number of novel orth-substituted benzoic acids are described.
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