(12) United States Patent (10) Patent No.: US 8,012,931 B2 Cujec Et Al
Total Page:16
File Type:pdf, Size:1020Kb
US008O12931B2 (12) United States Patent (10) Patent No.: US 8,012,931 B2 Cujec et al. (45) Date of Patent: Sep. 6, 2011 (54) MODIFIED FGF-21 POLYPEPTIDES AND 3. A g 3. colottis i etetal al. THEIR USES 4,670,417 A 6, 1987 Iwasaki et al. 4,671,958 A 6, 1987 Rodwell et al. (75) Inventors: Thomas P. Cujec, San Diego, CA (US); 4,680,338 A 7, 1987 Sundoro Roberto Mariani, San Diego, CA (US); 4,687,777 A 8/1987 Meguro et al. 4,689,406 A 8, 1987 Banks et al. isy's 4,699,784. A 10/1987 Shih et al. iego, CA (US); William reele, 4,738,921 A 4, 1988 Belagaje et al. West Hollywood, CA (US); Nick 4,755.465 A 7/1988 Gray et al. Knudsen, San Diego, CA (US); Lillian 26. A s 3. s 1 Ho, San Diego, CA (US), Jason 4,873,080 A 10/1989 Brickletray et al. al. Pinkstaff. Encinitas, CA (US), Vadim 4,873.255. A 10/1989 Yoshioka et al. Kraynov, San Diego, CA (US) 4,876, 197 A 10/1989 Burke et al 4,880,734 A 11/1989 Burke et al. (73) Assignee: Ambrx, Inc., La Jolla, CA (US) 4,897.405 A 1/1990 Alessi et al. 4.902,502 A 2f1990 Nitecki et al. (*)c Notice:- r Subject to any disclaimer, the term of this 4,929,5554,904,584 A 2,5/1990 1990 CreggShaw et al. patent is extended or adjusted under 35 5,002,953. A 3/1991 Hindley U.S.C. 154(b) by 0 days. 5,021,234 A 6, 1991 Ehrenfeld 5,061,717 A 10, 1991 Clarket al. (21) Appl. No.: 12/051,830 5,089,398 A 2/1992 Rosenberg et al. 5, 120,754 A 6/1992 Clark et al. 1-1. 5,122,614 A 6/1992 Zalipsky (22) Filed: Mar 19, 2008 5,132,317. A 7/1992 Cantello et al O O 5,162,601 A 1 1/1992 Slightom (65) Prior Publication Data 5,218,092 A 6/1993 Sasaki et al. 5,219,564 A 6/1993 Zalipsky et al. US 2008/O255045A1 Oct. 16, 2008 5,223,522 A 6/1993 Clark et al. 5,229,490 A 7, 1993 Tam Related U.S. Application Data (Continued) (60) Provisional application No. 60/921,297, filed on Mar. 30, 2007, provisional application No. 60/988,060, FOREIGN PATENT DOCUMENTS filed on Nov. 14, 2007. DE 3218121 A1 11F1983 (Continued) (51) Int. C. A6 IK38/8 (2006.01) OTHER PUBLICATIONS CI2P 2L/00 (2006.01) Abuchowski, A. et al. “Cancer therapy with chemically modified C07K I4/50 (2006.01) enzymes. I. Antitumor properties of polyethylene glycol CI2N 1/16 (2006.01) asparaginase conjugates. Cancer Biochem Biophys. Jun. CO7H 2 1/00 (2006.01) 1984;7(2): 175-86. Altschul, SF et al. “Gapped Blast and PSI-Blast: a (52) U.S. C. ... 514/9.1; 435/69.1:435/70.1; 435/255.2: new generation of protein database search programs. Nucleic Acids 530/350; 530/399; 536/23.1 Res. Sep. 1, 1997:25(17):3389-402. (58) Field of Classification Search ........................ None Altschul, SF et al. “Basic local alignment search tool.” J Mol Biol. See application file for complete search history. Oct. 5, 1990:215(3):403-10. Amann, E et al., “Vectors bearing a hybrid trp-lac promoter useful for References Cited regulated expression of cloned genes in Escherichia coli,” Gene. Nov. (56) 1983:25(2-3): 167-78. Anderson, JC et al., “Exploring the limits of codon and anticodon U.S. PATENT DOCUMENTS size.” Chem Biol. Feb. 2000:9(2):237-44. 2.968, 158 A 1/1961 Ruschig et al. Andresz, H et al. Abstract of "Chemische Synthese verzweigter 3,097,242 A 7, 1963 Hoehn et al. Polysaccharide, 5, Kopplung von Oligosacchariden und Amylose an 3,454,635 A 7, 1969 Weber et al. verschiedene Träger durch Hydrazonbindung.” Makromol. Chem. 3,501,495 A 3/1970 Beregi et al. 1978; 179:301 Abstract. 3,654,357 A 4, 1972 Bretschneider et al. Arnold, FH. "Protein engineering for unusual environments.” Curr 3,668,215 A 6/1972 Plumpe et al. Opin Biotechnol. Aug. 1993:4(4):450-5. 3,669,966 A 6, 1972 Ambrogi et al. AZOulay, M., et al. “Glutamine analogues as Potential Antimalarials.” 3,708.486 A 1/1973 Kutter et al. Eur, J. Med. Chem. (1991); 26(2):201-5. 3,773.919 A 11, 1973 Boswell et al. 4,287,200 A 9, 1981 Kawamatsu et al. (Continued) 4,289,872 A 9, 1981 Denkewalter et al. 4.412,989 A 11, 1983 Iwashita et al. Primary Examiner — Elly-Gerald Stoica 4.414,148 A 11, 1983 Jansen et al. 4.485,045 A 1 1/1984 Regen (74) Attorney, Agent, or Firm — John W. Wallen, III; Kristin 4,511,502 A 4, 1985 Builder et al. S. Eaton 4,511,503 A 4, 1985 Olson et al. 4,512.922 A 4, 1985 Jones et al. (57) ABSTRACT 4,544.545 A 10/1985 Ryan et al. 4,551,433 A 11, 1985 DeBoer Modified FGF-21 polypeptides and uses thereofare provided. 4,569,789 A 2f1986 Blattler et al. 4,572,912 A 2f1986 Yoshioka et al. 52 Claims, 40 Drawing Sheets US 8,012.931 B2 Page 2 U.S. PATENT DOCUMENTS RE37,343 E 8/2001 Tekamp-Olson 6,281.211 B1 8/2001 Cai et al. 2: A 168 t t 6,306,821 B1 10/2001 Mikos et al. 525s,185. A 1/1993 E. 6,312.923 B1 1 1/2001 Tekamp-Olson 52s698. A 1/1994 Nitecki 83.3 R 29: R el. 5,290,686 A 3/1994 Kendal et al. E. E. 2 S. 5,324,639 A 6/1994 Brierley et al. 6361969 B1 3/2002 Galeotti 5,324,844. A 6/1994 Zalipsky 6,368.825 B1 4/2002 Chao 5,382,657 A 1/1995 Karasiewicz et al. 6.420339 B1 7, 2002 Ge tal 5,446,090 A 8, 1995 Harris 4 W gg et al. 5,468.478 A 11/1995 Saifer et al. 6,423,685 B1 7/2002 Drummond et al. 5,473,034 A 12/1995 Yasui et al. 3.I - w R 29: St.oberts et etal. al. 5,476,653 A 12/1995 Pitt et al. 6,451,346 B1 9/2002 Shah et al. 3. A 3. ME l 6,451,561 B1 9/2002 Wells et al. 4. A 6 CE. ga's E: 1938: Billy et al. 5,559,213 A 9, 1996 Hakimi et al. 6521427 B1 2/2003 E. 5,571,709 A 11/1996 Devauchelle et al. 6.552167 B1 4/2003 Rose 5,580,723. A 12/1996 Wells et al. 6,586.207 B2 7/2003 Tirrelletal 5,583,023 A 12/1996 Cerutti et al. 6,602,498 B2 & 2003 Sh 5,602,034 A 2/1997 Tekamp-Olson 6,608.183 B1 8/2003 5,605,827 A 2f1997 Jackwood et al. 6610,281 B2 8, 2003 Harris 5,612.460 A 3/1997 Zalipsky 6,646,110 B2 1/2003 Nissen etal 5,629,203 A 5/1997 Shuster s’ s 2004 Itohet al. 5,629,384 A 5, 1997 Veronese et al. 858:- 4 R 3. Si.chultz et al. 5,643,575 A 7/1997 Martinez et al. 7,045,337 B2 * 5/2006 Schultz et al. ............. 435/252.3 5,650,234. A 7/1997 Dolence et al. 7,083,970 B2 8/2006 Schultz et al. 5,672,662 A 9/1997 Harris et al. 7,259,248 B2 8/2007 Itoh et al. 5,674,706 A 10/1997 Shuster 7.408,047 B1 * 8/2008 Thomason et al. .......... 536,231 RE35,749 E 3/1998 Rosenberg et al. 7,576, 190 B2 * 8/2009 Glaesner et al. 530,399 5,736,625. A 4, 1998 Callstrom et al. 7,582,607 B2 * 9/2009 Frye et al. ... 514/1.1 5,739,208 A 4, 1998 Harris 7,622.445 B2 * 1 1/2009 Frye et al. 514/1.1 5,747,646 A 5/1998 Hakimi et al. 7,655,627 B2 * 2/2010 Frye et al. ...................... 514/1.1 5,750,373 A 5, 1998 Garrard et al. 2001/0012628 A1 8/2001 Agarwal et al. 5,753,220 A 5/1998 Suzuki et al. 2001, 0021763 A1 9, 2001 Harris 3% A g R et al. 1 2001/0044526 A1 11/2001 Shen 5.766,885 A 6, 1998 AS a 2001/0056171 A1 12/2001 Kozlowski ww. Ting 2002/0002250 A1 1/2002 Bentley et al. 5,808.096 A 9, 1998 Zalipsky 2002, 0037949 A1 3, 2002 Harris et al. 5,824,778 A 10, 1998 Ishikawa et al. 2002/004.0076 A1 4/2002 Harris et al. 5,824,784. A 10/1998 Kinstler et al. 2002fOO42097 A1 4, 2002 Tirrell et al. 5,834,250 A 1 1/1998 Wells et al. 2002/0052009 A1 5/2002 Hornauer et al. 35 A EE Fami et al. 2002fOO52430 A1 5, 2002 Harris et al. 5. A 315 Enea 2002/0055169 A1 5/2002 Tekamp-Olson w I-1 2002/0072573 A1 6/2002 Bentley et al. s: A 1999 Sh 2002/0081660 A1 6/2002 Swartz et al. 5.861.379wwk A 1, 1999 Zh.i.get al.al 2002fO0869392002/0082345 A1Al 6,7, 2002 Kozlowski et al.