40741-46-6Relevant academic research and scientific papers
Process for Preparation of Sulfonyl Carbamate Bile Acid Derivatives
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Paragraph 0266-0268, (2018/10/30)
The present invention relates to processes for preparing compounds of Formula (I) and compounds of Formula (II): or a pharmaceutically acceptable salt or solvate thereof. These compounds and pharmaceutical compositions are useful as FXR or TGRS modulators. Specifically, the present invention relates to bile acid derivatives and methods for their preparation and use. The present invention relates to a process for the preparation of the compounds of Formula (III), Formula (IV), Formula (V), and Formula (VI), The present invention also relates to a process for the preparation of compounds (VII), (VIII) and (IX),
MTH1 INHIBITORS FOR TREATMENT OF CANCER
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Page/Page column 124, (2015/12/30)
A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.
SUBSTITUTED INDOLE MCL-1 INHIBITORS
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Paragraph 00478, (2015/12/08)
The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
MTH1 INHIBITORS FOR TREATMENT OF INFLAMMATORY AND AUTOIMMUNE CONDITIONS
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Page/Page column 302; 303, (2016/04/04)
A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.
Discovery of novel HCV inhibitors: Synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B
Zhang, Xiaoyan,Zhang, Nanjing,Chen, Guangming,Turpoff, Anthony,Ren, Hongyu,Takasugi, James,Morrill, Christie,Zhu, Jin,Li, Chunshi,Lennox, William,Paget, Steven,Liu, Yalei,Almstead, Neil,George Njoroge,Gu, Zhengxian,Komatsu, Takashi,Clausen, Valerie,Espiritu, Christine,Graci, Jason,Colacino, Joseph,Lahser, Fred,Risher, Nicole,Weetall, Marla,Nomeir, Amin,Karp, Gary M.
, p. 3947 - 3953 (2013/07/27)
A novel series of 6-(indol-2-yl)pyridine-3-sulfonamides was prepared and evaluated for their ability to inhibit HCV RNA replication in the HCV replicon cell culture assay. Preliminary optimization of this series furnished compounds with low nanomolar potency against the HCV genotype 1b replicon. Among these, compound 8c has identified as a potent HCV replicon inhibitor (EC50 = 4 nM) with a selectivity index with respect to cellular GAPDH of more than 2500. Further, compound 8c had a good pharmacokinetic profile in rats with an IV half-life of 6 h and oral bioavailability (F) of 62%. Selection of HCV replicon resistance identified an amino acid substitution in HCV NS4B that confers resistance to these compounds. These compounds hold promise as a new chemotype with anti-HCV activity mediated through an underexploited viral target.
Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: Structure-based drug design, synthesis, and biological evaluation
Vernier, William,Chong, Wesley,Rewolinski, David,Greasley, Samantha,Pauly, Thomas,Shaw, Morena,Dinh, Dac,Ferre, Rose Ann,Nukui, Seiji,Ornelas, Martha,Reyner, Eric
scheme or table, p. 3307 - 3319 (2010/07/10)
A novel series of potent thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV was discovered using structure-based drug design. Synthesis, structure-activity relationship, and optimization of physicochemical properties are described. Low nanomolar potency was achieved, and selected compounds with improved thermodynamic solubility showed promising in vitro inhibition of carbonic anhydrase activity in rabbit iris ciliary body homogenate.
HETEROCYCLYL PYRIDYL SULFONAMIDE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS
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Page/Page column 15-16, (2008/12/05)
Objects of the present invention are the compounds of formula I, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as wel
ARYL PYRIDYL SULFONAMIDE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS
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Page/Page column 16, (2009/01/20)
Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
METHODS OF USING PI3K AND MEK MODULATORS
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Page/Page column 253, (2008/06/13)
The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
METHODS OF TREATING BY INHIBITING WITH QUINAXOLINE INHIBITORS OF PI3K-ALPHA
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Page/Page column 376, (2008/12/08)
The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
