220844-82-6Relevant academic research and scientific papers
Guanidine compound for preventing and treating chronic pain medication (by machine translation)
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Paragraph 0257-0266, (2020/08/27)
The invention relates to a guanidine compound as shown in general formula (I) as a guanidine compound for preventing and treating chronic pain disease. A pharmaceutically acceptable salt thereof, a prodrug thereof, a solvate thereof, a deuterated substanc
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones
Higuchi, Robert I.,Arienti, Kristen L.,López, Francisco J.,Mani, Neelakhanda S.,Mais, Dale E.,Caferro, Thomas R.,Long, Yun Oliver,Jones, Todd K.,Edwards, James P.,Zhi, Lin,Schrader, William T.,Negro-Vilar, Andrés,Marschke, Keith B.
, p. 2486 - 2496 (2008/02/01)
Recent interest in orally available androgens has fueled the search for new androgens for use in hormone replacement therapy and as anabolic agents. In pursuit of this, we have discovered a series of novel androgen receptor modulators derived from 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. These compounds were synthesized and evaluated in competitive binding assays and an androgen receptor transcriptional activation assay. A number of compounds from the series demonstrated single-digit nanomolar agonist activity in vitro. In addition, lead compound (R)-16e was orally active in established rodent models that measure androgenic and anabolic properties of these agents. In this assay, (R)-16e demonstrated full efficacy in muscle and only partially stimulated the prostate at 100 mg/kg. These data suggest that these compounds may be utilized as selective androgen receptor modulators or SARMs. This series represents a novel class of compounds for use in androgen replacement therapy.
QUINAZOLINE DERIVATIVES FOR USE AGAINST CANCER
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Page/Page column 179, (2008/06/13)
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R1, q, R2, R3, R4, R5, Ring A, X1, R6, r and R7 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Page/Page column 49, (2008/06/13)
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Page/Page column 26, (2010/11/23)
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
Androgen receptor modulator compounds and methods
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, (2008/06/13)
Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
Heteroaromatic Analogues of the α2-Adrenoreceptor Partial Agonist Clonidine
Chapleo, Christopher B.,Butler, Richard C. M.,England, David C.,Myers, Peter L.,Roach, Alan G.,et al.
, p. 1627 - 1630 (2007/10/02)
A 1,4-dioxane analogue (1) of the α2-adrenoreceptor partial agonist clonidine (2) has previously been shown to possess an interesting but complex pharmacological profile.In this study, from a series of other heterocyclic analogues of clonidine,
