专利号:US-7879999-B2 优先权日:2003-12-17 标 题:Method for the synthesis of exocyclic derivatives of cycloalkyl-hydrazines and exocyclic derivatives of heterocycloalkyl-hydrazines 发明人:DELALU HENRI; COLAS-DURICHE CECILE; BERTHET JACQUES; LEURENT PHILIPPE 权利人:ISOCHEM SA; CENTRE NAT RECH SCIENT; UNIV CLAUDE BERNARD LYON 摘要:The invention relates to a method for the synthesis of exocyclic derivatives of cycloalkyl-hydrazines and exocyclic derivatives of heterocycloalkyl-hydrazines The invention is characterised in that the method comprises a step consisting in demixing a solution containing said synthesised derivative, by reacting a heterocyclic amine with monochloramine, in an organic phase and an aqueous phase with the addition of anhydrous sodium hydroxide. According to the invention, the starting amine which has not reacted is collected and reused directly without any additional treatment. The inventive method can also be used to obtain the corresponding exocyclic heterocycloalkyl-hydrazine or cycloalkyl-hydrazinederivative derivative at a low cost compared to that of other known methods.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-RE41998-E 优先权日:1990-02-26 标题 :Compositions and methods of treatment of sympathetically maintained pain 发明人:CAMPBELL JAMES N 权利人:ARCLON THERAPEUTICS INC 摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.
专利号:WO-2024134480-A1 优先权日:2022-12-21 标题:Heterocyclic acrylic acid derivatives as monomers for the synthesis of polymers for use in ion exchange articles 发明人:RASMUSSEN JERALD K; HOCHSTEIN REBECCA A; FISHMAN JOSHUA M; VOLOSHIN ALEXEI M; WATTS ANNABELLE; RICHARDSON KRISTOPHER E; BISHOP LOGAN D C; GRIESGRABER GEORGE W; WLASCHIN KATIE F; COLAK ATAN SEMRA; JULIK EMILY; VAIL ANDREW W 权利人:3M INNOVATIVE PROPERTIES COMPANY 摘要:The present invention relates to monomers of formula (I) having a nitrogen atom that can be protonated at relatively low pH values (e.g., less than pH 9.5 or less than pH 9), polymers containing monomeric units derived from these monomers, anion exchange separation articles having the polymers grafted to a porous substrate, and methods of using the anion separation articles to separate mixtures of materials with different ionic content are described. Advantageously, the anion exchange separation articles can be used to separate biomaterials that cannot be subjected to high pH conditions (e.g., greater than 9 or 9.5) and/or to high ionic strength conditions (e.g., greater than 0.5M or 1M).
专利号:US-7935704-B2 优先权日:2003-08-01 标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:PALLADINO MICHAEL A; LLOYD GEORGE KENNETH; HAYASHI YOSHIO; NICHOLSON BENJAMIN 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ″, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.
专利号:US-7956058-B2 优先权日:2002-08-02 标 题:Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:HAYASHI YOSHIO; PALLADINO JR MICHAEL A; GRODBERG JENNIFER 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ′, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.
[参考文献]: Henryk Foks, Et Al. Synthesis And Antibacterial Activity Of 1H-Pyrazolo[3,4-B]Pyrazine And -Pyridine Derivatives. Farmaco. 2005 Jun-Jul;60(6-7):513-7.
合成参考文献
摘要:Treacy, S. M.; Zhang, X.; Rovis, T., Science of Synthesis, (2021) , 644.