- 2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy
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A transdermal SARM has a potential to have therapeutic benefit through anabolic activity in muscle while sparing undesired effects of benign prostate hyperplasia (BPH) and liver-mediated decrease in HDL-C. 2-Chloro-4-[(2-hydroxy-2-methyl-cyclopentyl)amino
- Saeed, Ashraf,Vaught, Grant M.,Gavardinas, Kostas,Matthews, Donald,Green, Jonathan E.,Losada, Pablo Garcia,Bullock, Heather A.,Calvert, Nathan A.,Patel, Nita J.,Sweetana, Stephanie A.,Krishnan, Venkatesh,Henck, Judith W.,Luz, John G.,Wang, Yong,Jadhav, Prabhakar
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p. 750 - 755
(2016/02/09)
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- SELECTIVE ANDROGEN RECEPTOR MODULATORS
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The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.
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Page/Page column 24-25
(2013/04/25)
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- Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators
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Herein we describe the discovery of ACP-105 (1), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone. Compound 1 was developed from a series of compounds found in a HTS screen using the receptor selection and amplification technology (R-SAT). In vivo, 1 improved anabolic parameters in a 2-week chronic study in castrated male rats. In addition to compound 1, a number of potent antiandrogens were discovered from the same series of compounds whereof one compound, 13, had antagonist activity at the AR T877A mutant involved in prostate cancer.
- Schlienger, Nathalie,Lund, Birgitte W.,Pawlas, Jan,Badalassi, Fabrizio,Bertozzi, Fabio,Lewinsky, Rasmus,Fejzic, Alma,Thygesen, Mikkel B.,Tabatabaei, Ali,Bradley, Stefania Risso,Gardell, Luis R.,Piu, Fabrice,Olsson, Roger
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supporting information; experimental part
p. 7186 - 7191
(2010/07/04)
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- CYCLIC AMINE COMPOUND
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A compound represented by the formula (I) or a salt thereof: (I) wherein the ring A represents a 5- to 8-membered ring which may have additional substituent besides R6, R7 and R8; R1 represents an electron-attracting group; R2, R3, R4 and R5 independently represent a hydrogen atom, a halogen atom, a group attached through a carbon atom, a group attached through a nitrogen atom, a group attached through an oxygen group, or a group attached through a sulfur atom; R6 represents a halogen atom, a group attached through a carbon atom, a group attached through a nitrogen atom, a group attached through an oxygen group, or a group attached through a sulfur atom, and R7 represents a cyano group, a nitro group, an acyl group which may have a substituent, a carboxyl group which may be esterified or amidated, or a hydrocarbon group which may have a substituent, or R6 and R7 together with a carbon atom to which they are attached may form a ring which may have a substituent; and R8 represents a hydrogen atom, a halogen atom, a group attached through a carbon atom, a group attached through an oxygen atom, or a group attached through a sulfur atom. The compound or salt has an excellent androgen receptor modulating effect, and is useful for the prevention/treatment of hypogonadism, partial androgen deficiency in aging male, decline in physical strength, cachexia, osteoporosis and the like.
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Page/Page column 87-88
(2010/11/25)
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- SUBSTITUTED N-ARYLPYRROLIDINES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS
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The present invention provides a compound of the formula: Formula I or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of Formula I.
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Page/Page column 45-46
(2010/11/25)
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- Aminophenyl derivatives as selective androgen receptor modulators
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Disclosed herein is a novel class of aminophenyl compounds having the structure: wherein R1 is cyano or nitro and ring A is a bi- or tricyclic bridged heterocycle and to their use as modulators of androgen receptor for the treatment or preventi
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Page/Page column 19
(2008/06/13)
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- CHEMICAL COMPOUNDS
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The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state
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