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(12) United States Patent (10) Patent No.: US 9,315,447 B2 Gjorstrup Et Al

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(12) United States Patent (10) Patent No.: US 9,315,447 B2 Gjorstrup Et Al USOO9315447B2 (12) United States Patent (10) Patent No.: US 9,315,447 B2 Gjorstrup et al. (45) Date of Patent: *Apr. 19, 2016 (54) COMPOSITIONS AND METHODS FOR THE (52) U.S. Cl. TREATMENT OF INFLAMMATION CPC ............. C07C 69/732 (2013.01); C07C 69/734 (2013.01) (71) Applicant: A.T. Resolve Sarl, St-Legier (CH) (58) Field of Classification Search (72) Inventors: Per Gjorstrup, Cambridge, MA (US); CPC ............................ C07C 69/732; C07C 69/734 C. Eric SchwartZ, Wakefield, MA (US USPC ............................................................ 514f63 . Lric SchwartZ, eleld, (US) See application file for complete search history. (73) Assignee: A.T. RESOLVE SARL, Lausanne (CH) (56) References Cited (*) Notice: Subject to any disclaimer, the term of this U.S. PATENT DOCUMENTS patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. 4,172,896 A 10/1979 Uno et al. 4,346,227 A 8, 1982 Terahara et al. This patent is Subject to a terminal dis- 4,444,784. A 4, 1984 Hoffman et al. claimer. 4,681,893 A 7, 1987 Roth 5,354,772 A 10, 1994 Kathawala (21) Appl. No.: 14/207,342 (Continued) (22) Filed: Mar 12, 2014 FOREIGN PATENT DOCUMENTS (65) Prior Publication Data WO 2006,105.058 A2 10, 2006 WO 2009/038671 3, 2009 US 2014/0275,247 A1 Sep. 18, 2014 (Continued) Related U.S. Application Data OTHER PUBLICATIONS (63) Continuation of application No. 13/264,155, filed as & 8 s application No. PCT/US2010/030812 on Apr. 13, Becker et al., “Hydrolyse von Carbonsaurederivaten . Organikum, 2010, now Pat No. 8673,881. pp. 414-415 (1990) (No translation available). (Continued) (60) Provisional application No. 61/174,806, filed on May on1, 2009 they isional applicauonapplication No.No 61/168,739,, /39, filedIlle Primary Examiner — Deborah D Carr (74) Attorney, Agent, or Firm — Kilpatrick Townsend & (51) Int. Cl. Stockton LLP AOIN 55/00 (2006.01) A6 IK3I/695 (2006.01) (57) ABSTRACT CO7D 303/2 (2006.01) The invention relates to novel resolvin compounds and phar C07C 59/00 (2006.01) maceutical preparations thereof. The invention further relates C07F 7/02 (2006.01) to methods of treatment using the novel resolvin compounds C07F II/00 (2006.01) of the invention. C07C 69/732 (2006.01) C07C 69/734 (2006.01) 16 Claims, 7 Drawing Sheets A -- 1001 -- 102 E windwavywww.www.wrwrrrmamer-rrm-www. 2 4. 1 . US 9,315,447 B2 Page 2 (56) References Cited Iigo et al., “Inhibitory effects of docosahexaenoic acid on colon carninoma 26 metastasis to the lung.” Br: J. Cancer, (1997), U.S. PATENT DOCUMENTS 75(5):650-655. Simopoulous et al., “Workshop on the Essentiality of and Recom 5,358,970 A 10, 1994 Ruffet al. mended Dietary Intakes for Omega-6 and Omega-3 Fatty Acids.” 5,427,798 A 6/1995 Ludwig et al. 5,541,231 A 7, 1996 Ruffet al. (1999), J. Am. Coll. Nutr., 18(5):487-489. 5,731,000 A 3, 1998 Ruffet al. International Search Reportdated Jun. 29, 2010 in related PCT Appli 5,763,493 A 6, 1998 Ruffet al. cation No. PCT/US2010/030813. 6,110,973 A 8/2000 Young European Search report dated Jul. 26, 2012 in related European RE37,314 E 8, 2001 Hirai et al. Patent Application No. 10764985.7. 6,583,124 B2 6/2003 Asgharian Mexican Office Action dated Sep. 14, 2012 in related Mexican Patent 2005, 0004074 A1 1/2005 Lyons et al. 2005/OO31697 A1 2/2005 Vehige et al. Application No. MX/a/2011/010827 (with English Translation). 2005/0059744 A1 3/2005 Donello et al. New Zealand Examination Report dated Aug. 29, 2012 in related 2005, 0080056 A1 4, 2005 Horn New Zealand Application No. 596228. 2005/0228042 A1 10, 2005 Friswad et al. U.S. Office Action dated May 22, 2013 in parent U.S. Appl. No. 2005/0228047 A1* 10, 2005 Petasis .......................... 514,560 13/264,155, 5 pages. 2009,0294347 A1 12, 2009 Wochele et al. European Examination Report dated Nov. 13, 2013 in related Euro pean Patent Application No. 10764985.7. 5 pages. FOREIGN PATENT DOCUMENTS Russian Office Action dated Mar. 5, 2014 in related Russian Patent Application No. 2011 146005, 11 pages (with English Translation). WO 2009/051670 A2 4/2009 Mexican Office Action dated Apr. 24, 2014 in related Mexican Patent WO 2010/0395.61 4/2010 Application No. MX/a/2011/010827. 5 pages (with English Transla OTHER PUBLICATIONS tion). Chilean Office Action dated May 5, 2014 in related Chilean Patent Billman et al., “Prevention of Sudden Cardiac Death by Dietary Pure Application No. 2548-2011, 9 pages (with English Translation). w-3 Polyunsaturated Fatty Acids in Dogs.” Circulation, (1999), Japanese Office Action dated May 20, 2014 in related Japanese Patent 99:2452-2457. Application No. 2012-506110, 11 pages (with English Translation). Henkel-Hanke et al., “Artificial oxygen carriers: a current review.” AANA.J. (2007), 75(3):205-211. * cited by examiner U.S. Patent Apr. 19, 2016 Sheet 1 of 7 US 9,315,447 B2 p~~~~~••••••••••••••••••••••••-----------------------••••••••••~~~~~~~~--~~~~~~~~~~~~~~~.~~~~~~~); | w s w s wa (utifu) toeueolic (fruijfti) togeyua303 i s o 's es se ***;" tliffju) togesteguio U.S. Patent Apr. 19, 2016 Sheet 2 of 7 US 9,315,447 B2 smas . ac www. s: x \ {i : SN. Y. wi. S.x2 is: it c > . six is: C-3s. 2 is iii &f 88. s: sa c s $3. s U.S. Patent Apr. 19, 2016 Sheet 3 of 7 US 9,315,447 B2 s 3. s S. S. S &s 3s & 8 Ys s^ rw --wa U.S. Patent Apr. 19, 2016 Sheet 5 of 7 US 9,315.447 B2 Figure 5 U.S. Patent Apr. 19, 2016 Sheet 6 of 7 US 9,315,447 B2 Figure 6 U.S. Patent Apr. 19, 2016 Sheet 7 Of 7 US 9,315,447 B2 S. Figure 7 N: - - SS 3. s: 3. US 9,315,447 B2 1. 2 COMPOSITIONS AND METHODS FOR THE SUMMARY OF INVENTION TREATMENT OF INFLAMMATION The present invention provides a compound of formula I, RELATED APPLICATIONS (I) This application claims the benefit of priority to U.S. Pro visional Patent Application No. 61/168,739, filed Apr. 13, 2009, and U.S. Provisional Patent Application No. 61/174, 10 806, filed May 1, 2009, which applications are hereby incor porated by reference in their entirety. and pharmaceutically acceptable salts thereof, wherein: the stereochemistry of the carbon qq to carbon rr double BACKGROUND 15 bond is cis or trans; the stereochemistry of the carbon ss' to carbon tt'double bond is cis or trans; Supplementation of dietary omega-3 polyunsaturated fatty Re and Rfare independently selected from hydrogen, alkyl, acids (“c)-3 PUFAs) such as eicosapentaenoic acid, a com alkenyl, alkynyl, aryl, heteroaryl, acyl (e.g., alkoxyacyl, ponent of fish oils, may have beneficial effects in diseases aminoacyl), aminocarbonyl, alkoxycarbonyl, or silyl; E is a branched alkoxy Such as isopropoxy, isobutoxy, sec Such as arteriosclerosis, arthritis, asthma and cancer, which butoxy, tert-butoxy, 3-methylbutoxy, 2,2-dimethylpro may be mediated by antithrombotic, immunoregulatory and poxy, or 1.1.2-trimethylpropoxy. anti-inflammatory responses De Caterina, R. S. Endres, S. Rh and Ri are independently selected from hydrogen, alkyl, D. Kristensen, and E. B. Schmidt, editors. (1993). n-3 Fatty alkenyl, alkynyl, perfluoroalkyl, aryl or heteroaryl; 25 Rs is selected from i-iv as follows: i) CHCH(R)CH, where Acids and Vascular Disease. Springer-Verlag, London; R is hydrogen, alkyl, alkenyl, alkynyl, perfluoroalkyl, Lands, W. E. M., editor. (1987). Proceedings of the AOCS aryl, heteroaryl, fluoro, hydroxyl or alkoxy; ii) CHC Short Course on Polyunsaturated Fatty Acids and (RR)CH, where RandR, are each independently alkyl, Eicosanoids. American Oil Chemists’ Society, Champaign, alkenyl, alkynyl, perfluoroalkyl, aryl, or fluoro, or R and 30 R, are connected together to form a carbocyclic or hetero Ill.: Iigo, M. et al. (1997) Br. J. Cancer 75:650. The potential cyclic ring; iii) CHOCH, CHC(O)CH, or CHCH; or of (D-3 PUFAs for preventative actions in cardiovascular dis iv) Rs is a carbocyclic, heterocyclic, aryl or heteroaryl ring: eases was recently supported by the finding that major dietary and Rs and R are independently selected from hydrogen, alkyl, c)-3 PUFAs, such as eicosapentaenoic acid (C20:5 co-3; EPA) alkenyl, alkynyl, perfluoroalkyl, alkoxy, aryl or heteroaryl, and docosahexaenoic acid (C22:6 co-3; DHA), have a dra 35 or Rs and R are connected together to form a carbocyclic matic effect on ischemia-induced ventricular fibrillation or heterocyclic ring. Billman, G. E. et al. (1999) Circulation. 99:2452. Emer In certain embodiments, a compound of formula I is rep gence of Such possible preventative and/or therapeutic resented by formula II, actions of c)-3 PUFA supplementation in infant nutrition, 40 (II) cardiovascular diseases, and mental health has led to a call for ORf recommended dietary intakes by an international workshop Simopoulous, A. P. et al. (1999).J. Am. Coll. Nutr. 18:487. The Gruppo Italiano per lo Studio della Sopravvivense nell 45 Infarto Miocardio (GISSI) Prevenzione trial evaluated the effects of c)-3 PUFA supplementation with 11,300 patients and pharmaceutically acceptable salts thereof, wherein: surviving myocardial infarction taking ~1 g of c)-3 PUFA the stereochemistry of the carbon qq to carbon rr double daily (n=2,836) along with recommended preventive treat 50 bond is cis or trans; ments including aspirin, and reported a significant benefit the stereochemistry of the carbon ss' to carbon tt'double bond is cis or trans; with a decrease in cardiovascular death Marchioloi, R.
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