193537-11-0Relevant articles and documents
SALT TYPE AND CRYSTAL TYPE OF 4H-PYRAZOLO [1, 5-ALPHA] BENZIMIDAZOLE COMPOUND AND PREPARATION METHOD AND INTERMEDIATE THEREOF
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Paragraph 0149; 0150; 0151, (2018/10/04)
Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo[1, 5-alpha]benzimidazole compound and the preparation method and intermediate thereof.
ACYL SULFONAMIDE NAV1.7 INHIBITORS
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Page/Page column 60, (2018/05/24)
The present disclosure relates to compounds of formula I which inhibit NaV1.7, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions. (I)
ANALOGUES OF 4H-PYRAZOLO[1,5-a] BENZIMIDAZOLE COMPOUND AS PARP INHIBITORS
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Paragraph 0660, (2017/02/28)
Disclosed is a series of analogues of 4H-pyrazolo[1,5-α]benzimidazole compound as PARP inhibitors. In particular, disclosed in the invention is a compound as shown by formula (I) or a pharmaceutically acceptable salt thereof as a PARP inhibitor.
TRIAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
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Page/Page column 314, (2015/03/28)
Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.
PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS
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Page/Page column 82, (2015/10/05)
The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile
Kazmierski, Wieslaw M.,Anderson, Don L.,Aquino, Christopher,Chauder, Brian A.,Duan, Maosheng,Ferris, Robert,Kenakin, Terrence,Koble, Cecilia S.,Lang, Dan G.,Mcintyre, Maggie S,Peckham, Jennifer,Watson, Christian,Wheelan, Pat,Spaltenstein, Andrew,Wire, Mary B.,Svolto, Angilique,Youngman, Michael
supporting information; experimental part, p. 3756 - 3767 (2011/07/30)
We recently described (J. Med. Chem. 2008, 51, 6538-6546) a novel class of CCR5 antagonists with strong anti-HIV potency. Herein, we detail SAR converting leads 1 and 2 to druglike molecules. The pivotal structural motif enabling this transition was the secondary sulfonamide substituent. Further finetuning of the substituent pattern in the sulfonamide paved the way to enhancing potency and bioavailability and minimizing hERG inhibition, resulting in discovery of clinical compound 122 (GSK163929).
A new synthesis of spiropyrrolidine-tetralones via an unexpected formal ring-contraction of 4-disubstituted piperidine to 3-disubstituted pyrrolidine
Bandarage, Upul K.,Davies, Robert J.
scheme or table, p. 6415 - 6417 (2011/01/03)
We have developed an efficient synthesis of novel racemic spiropyrrolidine-tetralones via an unexpected ring-contraction reaction of a 4-disubstituted piperidine to 3-disubstituted pyrrolidine. We suggest that intramolecular quaternization of the piperidi
CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
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Page/Page column 68-69, (2010/12/29)
This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist
He, Shuwen,Ye, Zhixiong,Dobbelaar, Peter H.,Sebhat, Iyassu K.,Guo, Liangqin,Liu, Jian,Jian, Tianying,Lai, Yingjie,Franklin, Christopher L.,Bakshi, Raman K.,Dellureficio, James P.,Hong, Qingmei,Tsou, Nancy N.,Ball, Richard G.,Cashen, Doreen E.,Martin, William J.,Weinberg, David H.,MacNeil, Tanya,Tang, Rui,Tamvakopoulos, Constantin,Peng, Qianping,Miller, Randy R.,Stearns, Ralph A.,Chen, Howard Y.,Chen, Airu S.,Strack, Alison M.,Fong, Tung M.,MacIntyre, D. Euan,Wyvratt Jr., Matthew J.,Nargund, Ravi P.
scheme or table, p. 2106 - 2110 (2010/08/19)
We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1
Kazmierski, Wieslaw M.,Aquino, Christopher,Chauder, Brian A.,Deanda, Felix,Ferris, Robert,Jones-Hertzog, Deborah K.,Kenakin, Terrence,Koble, Cecilia S.,Watson, Christian,Wheelan, Pat,Yang, Hanbiao,Youngman, Michael
experimental part, p. 6538 - 6546 (2009/11/30)
We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the 125I-[MIP-1β] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4-disubstitited piperidine class H, both potent CCR5 ligands (pIC50 = 8.30 and 9.00, respectively) and HIV-1 inhibitors (pIC50 = 7.80 and 7.84, respectively, in Ba-L-HOS assay). In addition, 64 and 68 were bioavailable in rodents, establishing them as lead molecules for further optimization toward CCR5 clinical candidates.
