862129-81-5Relevant articles and documents
Synthesis of Functionalized [3], [4], [5] and [6]Dendralenes through Palladium-Catalyzed Cross-Couplings of Substituted Allenoates
Lippincott, Daniel J.,Linstadt, Roscoe T. H.,Maser, Michael R.,Lipshutz, Bruce H.
supporting information, p. 847 - 850 (2017/01/14)
A mild method for the synthesis of highly functionalized [3]–[6]dendralenes is reported, representing a general strategy to diversely substituted higher homologues of the dendralenes. The methodology utilizes allenoates bearing various substitution patter
Method for synthesizing 3, 6-dihydro-2H-pyrazine (thiazine) furan-4-boric acid ester
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Paragraph 0016, (2016/10/31)
The invention discloses a method for synthesizing 3, 6-dihydro-2H-pyrazine (thiazine) furan-4-boric acid ester. According to the method, tetrahydropyrazole (thiazine) furan-4-ketone serves as the raw material, generates hydrazone with p-toluenesulfonhydrazide, then reacts with NBS/organic alkali to generate alkenyl bromide and next forms Grignard reagent with magnesium metal, after the Grignard reagent is formed, boron reagent is added for a reaction, and the 3, 6-dihydro-2H-pyrazine (thiazine) furan-4-boric acid ester is obtained. By means of the method, ultralow temperature, column chromatography and palladium catalyzed coupling in a literature method are avoided, raw materials are easy to obtain, cost is low, conditions are mild, and the method has potential industrial application and amplification prospect.
BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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, (2015/06/25)
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
NOVEL AZABENZIMIDAZOLE HEXAHYDROFURO[E,2-B]FURAN DERIVATIVES
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, (2015/10/28)
Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be usef
PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
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Page/Page column 195, (2010/06/15)
Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety
Richardson, Timothy I.,Frank, Scott A.,Wang, Minmin,Clarke, Christian A.,Jones, Scott A.,Ying, Bai-Ping,Kohlman, Dan T.,Wallace, Owen B.,Shepherd, Timothy A.,Dally, Robert D.,Palkowitz, Alan D.,Geiser, Andrew G.,Bryant, Henry U.,Henck, Judith W.,Cohen, Ilene R.,Rudmann, Daniel G.,McCann, Denis J.,Coutant, David E.,Oldham, Samuel W.,Hummel, Conrad W.,Fong, Kin C.,Hinklin, Ronald,Lewis, George,Tian, Hongqi,Dodge, Jeffrey A.
, p. 3544 - 3549 (2008/02/07)
Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using serum estrogen levels as a biomarker for ovarian stimulation.
Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia
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Page/Page column 18, (2010/02/15)
The present invention relates to a method of treating schizophrenia which comprises administering a therapeutically effective amount of a compound of formula I wherein R1, R2, and R3 are as defined in the specification or to pharmaceutically active acid-addition salts thereof.
SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Page/Page column 14-15, (2008/06/13)
The present invention relates to a selective estrogen receptor modulator of formula I: or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.