117738-77-9Relevant articles and documents
NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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, (2013/03/26)
The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists
Yea, Christopher M.,Allan, Christine E.,Ashworth, Doreen M.,Barnett, James,Baxter, Andy J.,Broadbridge, Janice D.,Franklin, Richard J.,Hampton, Sally L.,Hudson, Peter,Horton, John A.,Jenkins, Paul D.,Penson, Andy M.,Pitt, Gary R. W.,Rivière, Pierre,Robson, Peter A.,Rooker, David P.,Semple, Graeme,Sheppard, Andy,Haigh, Robert M.,Roe, Michael B.
scheme or table, p. 8124 - 8134 (2009/11/30)
Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. The analogue of AVP, desmopressin, has proven an effective drug for diseases where a reduction of urine output is desired. However, its peptidic nature limits its bioavailability. We report herein the discovery of potent, nonpeptidic, benzylurea derived agonists of the vasopressin V2 receptor. We describe substitutions on the benzyl group to give improvements in potency and subsequent modifications to the urea end group to provide improvements in solubility and increased oral efficacy in a rat model of diuresis. The lead compound 20e (VA106483) is reported for the first time and has been selected for clinical development.
Piperazines as oxytocin agonists
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Page/Page column 9-10, (2010/02/11)
Disclosed are novel compounds according to general formula I, which have shown OT agonist activity.
Acyl sulfonamide anti-proliferatives: Benzene substituent structure-activity relationships for a novel class of antitumor agents
Lobb, Karen L.,Hipskind, Philip A.,Aikins, James A.,Alvarez, Enrique,Cheung, Yiu-Yin,Considine, Eileen L.,De Dios, Alfonso,Durst, Gregory L.,Ferritto, Rafael,Grossman, Cora Sue,Giera, Deborah D.,Hollister, Beth A.,Huang, Zhongping,Iversen, Philip W.,Law, Kevin L.,Li, Tiechao,Lin, Ho-Shen,Lopez, Beatriz,Lopez, Jose E.,Martin Cabrejas, Luisa M.,McCann, Denis J.,Molero, Victoriano,Reilly, John E.,Richett, Michael E.,Shih, Chuan,Teicher, Beverly,Wikel, James H.,White, Wesley T.,Mader, Mary M.
, p. 5367 - 5380 (2007/10/03)
Two closely related diaryl acylsulfonamides were recently reported as potent antitumor agents against a broad spectrum of human tumor xenografts (colon, lung, breast, ovary, and prostate) in nude mice. Especially intriguing was their activity against colorectal cancer xenografts. In this paper, rapid parallel synthesis along with traditional medicinal chemistry techniques were used to quickly delineate the structure-activity relationships of the substitution patterns in both phenyl rings of the acylsufonamide anti-proliferative scaffold. Although the molecular target of the compounds remains unclear, we determined that the vascular endothelial growth factor-dependent human umbilical vein endothelial cells assay in combination with a soft agar disk diffusion assay allowed for optimization of potency in the series. The pharmacokinetic properties and in vivo activity in an HCT116 xenograft model are reported for representative compounds.
benzamide derivatives as oxytocin agonists and vasopressin antagonists
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Page 24, (2010/02/08)
Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or Via receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.
Vasopressin agonist formulation and process
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Page/Page column 58, (2010/02/09)
This invention provides novel formulations for vasopressin agonist compounds, or a pharmaceutically acceptable salt thereof, having the general structure: and processes for making them, the formulations comprising from about 1% to about 20% of active ingredient, from about 1% to about 18% of a surfactant component, from about 50% to about 80% of a component of one or more polyethylene glycols, from about 1% to about 20% of a component of one or more sucrose fatty acid esters and/or polyvinylpyrrolidone and, optionally, one or more preservatives or antioxidants.
Tricyclic vasopressin agonists
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, (2008/06/13)
This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.
N-acylamino acid amide compounds and intermediates for preparation thereof
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, (2008/06/13)
The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.
AZOLE INHIBITORS OF CYTOKINE PRODUCTION
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, (2008/06/13)
Compounds having the formula are useful for treating diseases that are prevented by or ameliorated with Interleukin-2, Interleukin-4, or Interleukin-5 production inhibitors.
