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(12) United States Patent (10) Patent No.: US 9,303,024 B2 Walensky Et Al USOO93O3024B2 (12) United States Patent (10) Patent No.: US 9,303,024 B2 Walensky et al. (45) Date of Patent: Apr. 5, 2016 (54) PYRAZOL-3-ONES THAT ACTIVATE (56) References Cited PRO-APOPTOTC BAX U.S. PATENT DOCUMENTS (71) Applicant: Dana Farber Cancer Institute, Inc., 7, 160,870 B2 1/2007 Duffy et al. Boston, MA (US) 2009 OO12148 A1 1/2009 Maxfield et al. 2009,0163545 A1 6, 2009 Goldfarb 2011/0003851 A1 1/2011 Zhi et al. (72) Inventors: Loren D. Walensky, Newton, MA (US); Evripidis Gavathiotis, New York, NY FOREIGN PATENT DOCUMENTS (US) AR O49472 A1 8, 2006 CN 101343268 A 1, 2009 (73) Assignee: Dana-Farber Cancer Institute, Inc., CN 1017666O2 A T 2010 Boston, MA (US) DE 3728278 A1 6, 1988 s EP 2305250 A1 4/2011 WO O1-74769 A1 10, 2001 *) Notice: Subject to any disclaimer, the term of this WO 03-011855 A1 2, 2003 y WO WO2004O14902 A2 2, 2004 patent is extended or adjusted under 35 WO 2005-077939 A1 8, 2005 U.S.C. 154(b) by 0 days. WO WO2005077345 A1 8/2005 WO WO2005077368 A2 8, 2005 WO WO2007053.847 A2 5/2007 (21) Appl. No.: 14/350,847 WO 2009-071701 A1 6, 2009 WO WO2O11029046 A1 9, 2009 WO WO2O09130242 A1 10/2009 (22) PCT Filed: Oct. 11, 2012 WO WO2O10,042225 A2 4, 2010 OTHER PUBLICATIONS (86). PCT No.: PCT/US2012/059799 Chemical Abstracts Registry No. 7104-71-4, indexed in the Registry S371 (c)(1), file on STN CAS Online Nov. 16, 1984.* (2) Date: Apr. 10, 2014 Chemical Abstracts Registry No. 314292-25-6, indexed in the Reg istry file on STN CAS Online Jan. 17, 2001.* Chemical Abstracts Registry No. 314293-69-1, indexed in the Reg (87) PCT Pub. No.: WO2013/055949 istry file on STN CAS Online Jan. 17, 2001.* Chemical Abstracts Registry No. 314293-18-0, indexed in the Reg PCT Pub. Date: Apr. 18, 2013 istry file on STN CAS Online Jan. 17, 2001.* Gavathiotis et al., “Direct and selective small-molecule activation of O O proapoptotic BAX”. Nature Chemical Biology, 8(7):639-645 (May (65) Prior Publication Data 2012). Ren et al., “BID, BIM, and PUMA are Essential for Activation of the US 2014/O357687 A1 Dec. 4, 2014 BAX- and BAK-Dependent Cell Death Program'. Science, 330(6009): 1390-1393 (Dec. 2010). EP Patent Office, Partial Supplementary European Search Report, for Related U.S. Application Data EP Application No. 1284O7319-1453.2766355 PCT/ US2012059799, dated Jan. 18, 2015. (60) Provisional application No. 61/546,022, filed on Oct. International Search Report for PCT/US2012/059799 mailed Mar. 11, 2011. 13, 2013, 4 pages. Adam, et al., Synthesis and studies of Th(IV) and Ce(Ill) complexes with some azopyrazolone compounds, Delta Journal of Science, (51) Int. Cl. 11(3): 1089-103 (1987). CO7D 403/04 (2006.01) Amir, et al., Synthesis and antimicrobial activity of pyrazolinones CO7D 403/4 (2006.01) and pyrazoles having benzothiazole moiety, Med Chem Res, CO7D 417/04 (2006.01) 21:1261-1270 (2012). CO7D 417/4 (2006.01) Atta, Aly H., Reactions of 1-(2-benzothiazolyl)-4- A6 IK3I/4I55 2OO 6. O1 (dicyanomethylene)-3-methyl-2-pyrazolin-5-one towards amines, A6 IK3I/478 3:08: Heterocyclic Communications, 5(3):243-247 (1999). A6 IK3I/427 (2006.01) (Continued) gll, 17, 3.08: Primary Examiner — Laura L. Stockton (52) U.S. Cl (74) Attorney, Agent, or Firm — Fish & Richardson P.C. CPC .......... C07D 417/04 (2013.01); A61K 31/4155 (57) ABSTRACT (2013.01); A61K 31/4178 (2013.01); A61 K This application features pyrazol-3-one compounds that acti 31/427 (2013.01); A61 K3I/497 (2013.01); vate pro-apoptotic BAX. Also featured are methods of using C07D 403/04 (2013.01); C07D 403/14 Such compounds, e.g., for the treatment or prevention of (2013.01); C07D 413/04 (2013.01); C07D diseases, disorders, and conditions associated with deregu 417/14 (2013.01) lated apoptosis of cells (e.g., insufficient apoptosis of dis (58) Field of Classification Search eased or damaged cells or essentially the absence of apoptosis USPC 548/190, 312.4 of diseased or damaged cells). See application file for complete search history. 21 Claims, 65 Drawing Sheets US 9,303,024 B2 Page 2 (56) References Cited Mahesh, et al., Separation of some closely related 1-(2- benzothiazolyl)-3-methyl-4-arylhydrazono-pyrazoline-5-One OTHER PUBLICATIONS derivatives by thin layer chromatography, Fresenius' Zeitschrift fuer Baell, et al., New Substructure Filters for Removal of Pan Assay Analytische Chemie, 309(5):404 (1981). Interference Compounds (PAINS) from Screening Libraries and for Mamedov, et al., Reactions of Isomeric Arylchloropyruvates and Their Exclusion in Bioassays, J MedChem, 53(7): 2719-2740 (2010). Glycidates with Hydrazines, Russian Journal of Organic Chemistry, Bondock, et al., Ecofriendly solvent-free synthesis of thiazolylpyrazole derivatives, Monatshefte fuer Chemie 41(5):694-702 (2005). 139(11): 1329-1335 (2008). Naylor, et al., Identification of a chemical probe for NAACP by virtual Efros, et al., Benzothiazole derivatives. Preparation of screening, Nature Chemical Biology 5(4):220-226 (2009). I-benzothiazolyl-3-methyl-5(4H)-pyrazolone. Zhurnal Obshchei Parija, et al., Preparation of azamerocyanines and evaluation of the Khimi, 21:2046-50 (1951). effect of introduction of nitrogen atom in the chromophoric chain, El-Haty, A Co-Ordination and stability study. On some heterocyclic Journal of the Indian Chemical Society, 47(12): 1129-34 (1970). azopyrazolin-5-ones with Y(III), La(III), Ce(III) and UO, "ions, Jour Patel, et al., Synthesis and biological evaluation of some new nal of the Electrochemical Society of India, 40(3): 113-18 (1991). pyrazolones and imidazolinones, Oriental Journal of Chemistry Emandi, et al., 1-(2-Benzothiazolyl)-3-methyl-5-pyrazolone-based 19(2):435-440 (2003), Abstract Only). dyes, Revistade Chimie (Bucharest, Romania) 45(3): 179-82 (1994) Rosenbaum et al., Chemical screen to reducesterol accumulation in with English Abstract. Niemann–Pick Caisease cells identifies novel lysosomal acid lipase Erickson-Miller et al., Preclinical Activity of Eltromboapag (SB inhibitors, Biochimica et Biophysica Acta, Molecular and Cell Biol 4971 I5), an Oral, Nonpeptide Thrombopoietin Receptor Agonist, ogy of Lipids, 1791 (12), 1155-1165 (2009). Stem Cells, 27:424-430 (2009). Rout, M.K., Influence of structural changes on absorption. Ibrahim, et al., Synthesis of pyrazoles and fused pyrazoles. Novel Merocyanine dyes and aza-analogues of merocyanines, unsymmetri synthesis of pyrano 2,3-cpyrazole, thieno 2,3-cpyrazole and cal cyanines, and p-dialkylamino Styryl dives, Jour. & Proc. Inst. pyrazolo 3,4-bpyridine derivatives, Journal of the Indian Chemical Chem. (India), 35(3): 117-130 (1963). Society, 74(3):206-208 (1997). Chemical Structure Search Report by Science IP, dated Oct. 9, 2012 Kalluraya, et al., Synthesis of some triheterocyclic thiazole deriva (49 pages). tives of biological interest, Indian Journal of Heterocyclic Chemistry, 8(3):241-242 (1999). * cited by examiner U.S. Patent Apr. 5, 2016 Sheet 1 of 65 US 9,303,024 B2 Canonical BH3 Binding Site U.S. Patent Apr. 5, 2016 Sheet 2 of 65 US 9,303,024 B2 (S Hydrophobic O Hydrophilic Positive Charge & Negative Charge U.S. Patent Sheet 3 of 65 US 9,303,024 B2 21Y 2-42 O I I-O - Z| t ) LO S21 XY2 4. O U.S. Patent Apr. 5, 2016 Sheet 4 of 65 US 9,303,024 B2 OS O ‘ºaaOO.,08'Hoov/ICTH S Z] |- U.S. Patent Apr. 5, 2016 Sheet 6 of 65 US 9,303,024 B2 ‘TÁTOZeTUIT=TV7 U.S. Patent Apr. 5, 2016 US 9,303,024 B2 Z| U.S. Patent US 9,303,024 B2 OQ U.S. Patent US 9,303,024 B2 nHssºs'eseqs,6TU U.S. Patent Apr. 5, 2016 Sheet 11 of 65 US 9,303,024 B2 CN 4. Z -(2 - 1. 4 T 21 CN 24 A dnoI5)ozei?GI - ) t OOeuenTOLOp??uueleDV7–d 9Z//JejSUeII,OZTCI O- (y) | S z=(Y ls U.S. Patent Apr. 5, 2016 Sheet 12 of 65 US 9,303,024 B2 750,000 in Silico Small Molecules Glide/SPVS Docking 20,000 Top in Silico Hits Glide/XPVS Docking 1,000 Top in Silico Hits Interaction Analysis and Molecular Property-based Selection 100 Hits Tested Experimentally FIG 3A U.S. Patent Apr. 5, 2016 Sheet 13 of 65 US 9,303,024 B2 U.S. Patent Apr. 5, 2016 Sheet 14 of 65 US 9,303,024 B2 EC50 FITC-BIMSAHB, BAX WT: 283 nM; 95% CI: 225-355 200 C ?h 5 18O c ge s 160 3 140 N 120 C ? 100 10-9 10-8 10-7 10-6 10-5 Protein), M FG. 4A IC50 AC-BIMSAHB, BAX WT: 314 nM; 95% CI: 270-366 1 O O 8 O 6 O 4 O 2 O 1 O 9 10-8 10-7 10-6 10-5 Compound), M FIG. 4B U.S. Patent Apr. 5, 2016 Sheet 15 of 65 US 9,303,024 B2 SNNSNSNS NSN SYYYYYYYYYYYYYY. YYYYYYYYYYY. 6|& (%)XYSO) pun09 SHVSWIGOL U.S. Patent Apr. 5, 2016 Sheet 16 of 65 US 9,303,024 B2 IC50 BAM7, BAX: 3.31 uM; 95% CI: 2.66-4.12 BAM7(resynthesis), BAX: 4.41 uM; 95% CI: 3.60-5.55 BAM8 BAM9 BAM10 BAM11 BAM7(resynthesis) 2 100 5 O - 80 n & 3X 60 225 40 an 9 2 2O O 10-7 10-6 10-5 10-4 Compound), M FIG. 4D 1 O irSN' S FIG. 4E U.S. Patent Apr.
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