40843-55-8Relevant academic research and scientific papers
Method for selectively preparing hydroquinone monoether compound or quinol compound (by machine translation)
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Paragraph 0034-0039; 0050-0052; 0089-0090, (2020/12/30)
The method comprises the following steps: taking an organic boric acid compound and a p-benzoquinone compound as a reaction raw material, under the action of a copper catalyst, selectively reacting to obtain a hydroquinone monoether compound or a quinol compound. Compared with the prior art, the method disclosed by the invention adopts a one-pot reaction, can selectively obtain two products through solvent control, is suitable for preparing various types of hydroquinone monoether compounds and quinol compounds, and has wide applicability. The substrate functional group is high in tolerance and wide in substrate range. The raw material and the catalyst are cheap and easily available, the reaction conditions are mild, the reaction solvent is green and environment-friendly, the post-treatment is simple, and the yield and purity of the product are high. The preparation method is convenient. The method is rapid and efficient, and has a good application prospect in drug molecule synthesis. (by machine translation)
Amino propylene glycol derivatives, its preparation method and its pharmaceutical composition and use thereof
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, (2018/11/22)
The invention discloses a class of amino propanediol derivatives, a preparation method, drug compositions and uses thereof, and particularly relates to a class of new immunoloregulation agents represented by a general formula (I), a preparation method, drug compositions containing the immunoloregulation agents, and especially uses of the immunoloregulation agents as immunoloregulation drugs. The compound with characteristics of excellent treatment effect and low toxicity can be used in the fields of immunologic derangement and immunosuppression, and can further be used for treatment of hypoimmunity, organ transplant rejection and autoimmune diseases. The formula I is defined in the instruction.
BIARYL SUBSTITUTED NITROGEN CONTAINING HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION
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Page/Page column 10, (2008/06/13)
The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and pr
BIARYL SUBSTITUTED HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION
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Page/Page column 24; 42, (2008/06/13)
The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is
5-Aryl thiazolidine-2,4-diones as selective PPARγ agonists
Koyama, Hiroo,Boueres, Julia K.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,Miller, Daniel J.,Tolman, Richard L.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 1801 - 1804 (2007/10/03)
A series of 5-aryl thiazolidine-2,4-diones containing 4-phenoxyphenyl side chains was designed, synthesized, and evaluated for PPAR agonist activities. One such compound 28 exhibited comparable levels of glucose correction to rosiglitazone in the db/db mouse type 2 diabetes animal model.
5-Aryl thiazolidine-2,4-diones: Discovery of PPAR dual α/γ agonists as antidiabetic agents
Desai, Ranjit C.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 2795 - 2798 (2007/10/03)
A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARα/γ agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.
Structure-activity relationship studies on 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A4 (LTA4) hydrolase
Penning, Thomas D.,Chandrakumar, Nizal S.,Chen, Barbara B.,Chen, Helen Y.,Desai, Bipin N.,Djuric, Stevan W.,Docter, Stephen H.,Gasiecki, Alan F.,Haack, Richard A.,Miyashiro, Julie M.,Russell, Mark A.,Yu, Stella S.,Corley, David G.,Durley, Richard C.,Kilpatrick, Brian F.,Parnas, Barry L.,Askonas, Leslie J.,Gierse, James K.,Harding, Elizabeth I.,Highkin, Maureen K.,Kachur, James F.,Kim, Suzanne H.,Krivi, Gwen G.,Villani-Price, Doreen,Pyla, E. Yvonne,Smith, Walter G.,Ghoreishi-Haack, Nayereh S.
, p. 721 - 735 (2007/10/03)
Leukotriene B4 (LTB4) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA4 hydrolase is the rate-limiting step for LTB4 production, this enzyme represents an attractive pharmacological target for the suppression of LTB4 production. From an in- house screening program, SC-22716 (1, 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA4 hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA4 hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.
4-Phenoxy-phenoxy-alkane-carboxylic acid derivatives and process for their manufacture
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, (2008/06/13)
Novel 4-phenoxy-phenoxy-alkane-carboxylic acid derivatives of the formula I STR1 in which R1 stands for hydrogen, methylthio, cyclopentyl, cyclohexyl, phenyl, methylcyclohexyl, ethylcyclohexyl, or R1 and R3 together stand for a --CH=CH--CH=CH-- bridge or--unless at least one of the substituents R2 to R8 stands for hydrogen, or if R9 stands for a radical having at least 2 carbon atoms--for chlorine, R2 and R3, independent of one another, each stands for hydrogen, chlorine or alkyl of 1 to 4 carbon atoms, R4 stands for hydrogen, chlorine, alkyl of 1 to 4 carbon atoms, cyclopentyl, cyclohexyl, methylcyclohexyl or R3 and R4 together stand for a --CH=CH--CH=CH-- bridge, R5, R6 and R7, independent of one another, each stands for hydrogen or alkyl of 1 to 4 carbon atoms, R8 stands for hydrogen, alkyl of 1 to 4 carbon atoms or allyl, R9 stands for alkyl of 1 to 10 carbon atoms or phenyl and X stands for hydrogen, the cation of a physiologically acceptable inorganic or organic base of a hydrocarbon radical of 1 to 10 carbon atoms, having a strong action on the lipide and cholesterine metabolism and a process for their manufacture.
4-Phenoxy-phenoxy-alkane-carboxylic acid derivatives and process for their manufacture
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, (2008/06/13)
Novel 4-phenoxy-phenoxy-alkane-carboxylic acid derivatives of the formula I STR1 in which R1 stands for hydrogen, methylthio, cyclopentyl, cyclohexyl, phenyl, methylcyclohexyl, ethylcyclohexyl, or R1 and R3 together stand for a --CH=CH--CH=CH-- bridge or--unless at least one of the substituents R2 to R8 stands for hydrogen, or if R9 stands for a radical having at least 2 carbon atoms--for chlorine, R2 and R3, independent of one another, each stands for hydrogen, chlorine or alkyl of 1 to 4 carbon atoms, R4 stands for hydrogen, chlorine, alkyl of 1 to 4 carbon atoms, cyclopentyl, cyclohexyl, methylcyclohexyl or R3 and R4 together stand for a --CH=CH--CH=CH-- bridge, R5, R6 and R7, independent of one another, each stands for hydrogen or alkyl of 1 to 4 carbon atoms, R8 stands for hydrogen, alkyl of 1 to 4 carbon atoms or allyl, R9 stands for alkyl of 1 to 10 carbon atoms or phenyl and X stands for hydrogen, the cation of a physiologically acceptable inorganic or organic base of a hydrocarbon radical of 1 to 10 carbon atoms, having a strong action on the lipide and cholesterine metabolism and a process for their manufacture.
