863204-64-2Relevant academic research and scientific papers
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators
Manfredi, Mark C.,Bi, Yingzhi,Nirschl, Alexandra A.,Sutton, James C.,Seethala, Ramakrishna,Golla, Rajasree,Beehler, Blake C.,Sleph, Paul G.,Grover, Gary J.,Ostrowski, Jacek,Hamann, Lawrence G.
, p. 4487 - 4490 (2007)
Replacement of the 3-oxo group of 2-chloro-4-[(7R,7aS)-7-hydroxy-1,3-dioxotetrahydro-1H-pyrrolo[1,2c]imidazol-2(3H)-yl]-3-methylbenzonitrile resulted in a sulfamide series of selective androgen receptor modulator (SARM) agonists.
Sulfonylpyrrolidine modulators of androgen receptor function and method
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Page/Page column 22, (2010/02/13)
Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1 is hydrogen (H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, arylalkyl or substituted arylalkyl, CO2R4a, CONR4aR4b, and CH2OR4a; R2 is hydrogen (H), OR3, SR3, halo, NHR3, NHCOR4c1, NHCO2R4c1, NHCONR4cR4d and NHSO2R4c; R3 in each functional group is hydrogen (H), alkyl or substituted alkyl, CHF2, CF3 and CON4e; R4, R4a, R4b, R4c, R4c1, R4d, R4e, R4f, R4g, or R4h in each functional group are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R5 and R5′ are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl, wherein at least one of R5 and R5′ is hydrogen, or R5 and R5′ taken together form a double bond with oxygen (O), sulfur (S), NR7 or CR7R7′; where R7 and R7′ are as defined herein; G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; and n is an integer of 1 or 2, m is an integer of 1 or 2, Z is oxygen (—O—) or NR4h, a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.
