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(12) United States Patent (10) Patent No.: US 9,682,960 B2 Labrie Et Al

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(12) United States Patent (10) Patent No.: US 9,682,960 B2 Labrie Et Al USOO968296OB2 (12) United States Patent (10) Patent No.: US 9,682,960 B2 Labrie et al. (45) Date of Patent: Jun. 20, 2017 (54) NON-STEROIDAL ANTANDROGENS AND (56) References Cited SELECTIVE ANDROGEN RECEPTOR MODULATORS WITH APYRIDYL MOETY U.S. PATENT DOCUMENTS 3,742.951 7, 1973 Zaffaroni (71) Applicants: Fernand Labrie, Quebec (CA); 3,797.494 3, 1974 Zaffaroni Shankar Mohan Singh, Quebec (CA); 4,568,343 2, 1986 Leeper et al. Richard Labrecque, St-Nicolas (CA); 5,064,654 11, 1991 Berner et al. 5,071,644 12, 1991 Viegas et al. Liviu Constantin Ciobanu, Quebec 5,071,657 12, 1991 Oloff et al. (CA) 5,411,981 5, 1995 Gaillard-Kelly et al. 5,556,983 9, 1996 Claussner et al. (72) Inventors: Fernand Labrie, Quebec (CA); 5,750,553 5, 1998 Claussner et al. 6,071,957 6/2000 Miller et al. Shankar Mohan Singh, Quebec (CA); 7/2000 Claussner et al. Richard Labrecque, St-Nicolas (CA); 6,087,509 Liviu Constantin Ciobanu, Quebec (Continued) (CA) FOREIGN PATENT DOCUMENTS (73) Assignee: ENDORECHERCHE, INC. (CA) CA 2 677 295 9, 2008 CA 2 773 591 3, 2011 EP 0 002892 A1 7/1979 (*) Notice: Subject to any disclaimer, the term of this EP O 100 172 A1 2, 1984 patent is extended or adjusted under 35 EP O 279 982 A1 8, 1988 U.S.C. 154(b) by 0 days. EP O 494 819 A1 7, 1992 EP O 578516 A1 1, 1994 Appl. No.: 14/567,970 EP O 580 459 A1 1, 1994 (21) FR 2 671 348 A1 7, 1992 Filed: Dec. 11, 2014 FR 2 693 461 A1 1, 1994 (22) (Continued) (65) Prior Publication Data OTHER PUBLICATIONS US 2015/O175576 A1 Jun. 25, 2015 Silverman, R. “The Organic Chemistry of Drug Design and Drug Action.” 2004, NY Elsevier, pp. 20-32.* Related U.S. Application Data (Continued) (60) Provisional application No. 61/918,133, filed on Dec. Primary Examiner — Heidi Reese 19, 2013. (74) Attorney, Agent, or Firm — Ostrolenk Faber LLP (57) ABSTRACT (51) Int. C. CO7D 40/04 (2006.01) Compounds having the structure or their salts: CO7D 403/2 (2006.01) A6 IK 3/4439 (2006.01) R2 R W A6 IK3I/444 (2006.01) A 6LX 3L/24709 (2006.01) (CH)-4A A6 IK 3/4725 (2006.01) R3 N N-(CH)- A6 IK 3/496 (2006.01) A6 IK3I/506 (2006.01) X (- A 6LX 3/57 (2006.01) R4 Rs O R6 A6 IK 45/06 (2006.01) R. 24G. Gin G CO7D 40/12 (2006.01) cx"no 10-y-Rh CO7D 40/4 (2006.01) -Y-( G6 A6 IK 38/09 (2006.01) -J lsG -i. \Gs-G M A6 IK3I/58 (2006.01) (52) U.S. C. CPC .......... C07D 403/12 (2013.01); A61 K3I/444 are used to treat or reduce the likelihood of acquiring (2013.01); A61 K3I/4439 (2013.01); A61 K androgen-dependent diseases, such as prostate cancer, 31/4709 (2013.01); A61 K3I/4725 (2013.01); benign prostatic hyperplasia, polycystic ovarian syndrome, A6 IK3I/496 (2013.01); A61K 3 1/506 acne, hirsutism, seborrhea, androgenic alopecia, male bald (2013.01); A61 K3I/517 (2013.01); A61 K ness, muscle atrophy and weakness, sarcopenia, male 3 1/58 (2013.01); A61K 38/09 (2013.01); A61 K hypogonadism, erectile dysfunction, female sexual dysfunc 45/06 (2013.01); C07D 401/12 (2013.01); tion and osteoporosis. They can be formulated together with C07D 401/14 (2013.01) pharmaceutically acceptable diluent or carrier or otherwise (58) Field of Classification Search made into any pharmaceutical dosage form. Combinations None with other active pharmaceutical agents are also disclosed. See application file for complete search history. 24 Claims, 8 Drawing Sheets US 9,682,960 B2 Page 2 (56) References Cited Dominique Lesuisse, et al. “Discovery of the first Non-ATP Com petitive IGF-1R Kinase Inhibitors: Advantages incomparison With U.S. PATENT DOCUMENTS Competitive Inhibitors.” Bioorganic & Medicinal Chemistry Let ters, vol. 21, (2011), pp. 2224-2228. 6,242,611 B1 6/2001 Claussner et al. Ando, T., Yamawaki, J., Saito, Y. Takai, Y. Yamataka, H.:(1980). 7,001,911 B2 2/2006 Salvati et al. Neighboring group participation in Solvolysis. X. Dissection of 7,138.421 B2 11/2006 Cleve et al. Ar-5 and Ar-6 pathways in trifluoroacetolysis of 4-arylbutylo 7,141,578 B2 11/2006 Salvati et al. 7,268,232 B2 9/2007 Schlienger et al. methyl-2-naphthalenesulfonates. Bull. Chem. Soc. Jpn. 53(8): 7,271,188 B2 9, 2007 Tachibana et al. 234.8-2356. 7.427,682 B2 9, 2008 Lanter et al. Aucoin, M.W., Wassersug, R.J.; (2006). The sexuality and social 7,709,516 B2 * 5/2010 Labrie.................. CO7D 207/40 performance of androgen-deprived (castrated) men throughout his 514/389 tory: Implications for modern day cancer patients. Soc. Sci. Med., 7,759,366 B2 * 7/2010 Jaehne ................. CO7D 233/72 63: 3.162-3173. 514,341 Balog, A., Salvati, M.E., Shan, W., Mathur, A., Leith, L.W. Wei, 7,759.520 B2 7, 2010 Dalton et al. D.D., Attar, R.M., Geng, J., Rizzo, C.A., Wang, C., Krystek, S.R., 7,803,970 B2 9, 2010 Dalton et al. Tokarski, J.S., Hunt, J.T., Gottardis, M., Weinmann, R.; (2004). The 2004/O181064 A1 9, 2004 Sun et al. Synthesis and evaluation of 2.2.1-bicycloaZahydantoins as andro 2009,027.0361 A1 10/2009 Ito et al. gen receptor antagonists. Bioorg. Med, Chem. Lett., 14: 6107-6111. 2010/0331418 A1 12/2010 Koh et al. Bhasin, S., Pencina, M., Kaur Jasuja, G., Travison, T.G., Coviello, 2012,0004270 A1 1, 2012 Miller A., Orwoll, E. Wang, PY., Nielson, C. Wu, F., Tajar, A., Labrie, F. 2012,004 1046 A1 2/2012 Varchi et al. 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