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( 12 ) United States Patent US010266485B2 (12 ) United States Patent (10 ) Patent No. : US 10 , 266 , 485 B2 Benenato ( 45 ) Date of Patent: * Apr. 23, 2019 ( 54 ) COMPOUNDS AND COMPOSITIONS FOR ( 2013. 01 ) ; C07C 227/ 16 (2013 . 01 ) ; C07C INTRACELLULAR DELIVERY OF 227/ 18 ( 2013 .01 ) ; C07C 229 / 16 (2013 . 01 ) ; THERAPEUTIC AGENTS C07C 233 / 36 ( 2013 .01 ) ; C07C 235 / 10 (2013 .01 ) ; C07C 255 /24 ( 2013 . 01 ) ; C07C (71 ) Applicant: Moderna TX , Inc ., Cambridge , MA 271/ 20 ( 2013 . 01 ) ; C07C 275 / 14 ( 2013 . 01 ) ; (US ) C07C 279 /12 ( 2013 .01 ) ; C07C 279 / 24 ( 2013 . 01 ) ; C07C 279 /28 ( 2013 .01 ) ; C07C ( 72 ) Inventor: Kerry E . Benenato , Sudbury , MA (US ) 279 / 32 ( 2013 . 01 ) ; C07C 311 / 05 ( 2013 . 01 ) ; C07C 335 / 08 (2013 . 01 ) ; C070 207 / 27 (73 ) Assignee : ModernaTX , Inc. , Cambridge, MA ( 2013 .01 ) ; CO7D 233 / 72 ( 2013 . 01 ) ; C07D (US ) 249 /04 (2013 .01 ) ; C07D 263 / 20 ( 2013 .01 ) ; C07D 265 / 33 ( 2013 .01 ) ; C07D 271 / 06 ( * ) Notice : Subject to any disclaimer, the term of this ( 2013 .01 ) ; C07D 271/ 10 (2013 .01 ) ; C07D patent is extended or adjusted under 35 277 / 38 ( 2013 . 01 ) ; C07F 9 / 091 ( 2013 .01 ) ; U . S . C . 154 ( b ) by 0 days . CO7K 14 /505 ( 2013. 01 ) ; A61K 9 /1271 This patent is subject to a terminal dis (2013 .01 ) ; A61K 48 / 00 ( 2013 .01 ) ; C07C claimer . 2601/ 02 (2017 .05 ) ; C07C 2601 / 04 ( 2017 . 05 ) ; C07C 2601/ 14 ( 2017 .05 ) ; C07C 2601 / 18 (21 ) Appl . No. : 16 / 005 , 286 (2017 . 05 ) (58 ) Field of Classification Search (22 ) Filed : Jun . 11 , 2018 CPC .. A61K 39 /00 ; A61K 51 /08 ; CO7K 14 /81 ; C07H 21 /00 (65 ) Prior Publication Data USPC .. .. 424 / 9 . 1 ; 435 /91 . 1 , 91. 31 , 458 ; 514 /44 ; US 2018 / 0273467 A1 Sep . 27, 2018 536 /23 . 1 , 24 . 5 See application file for complete search history . Related U . S . Application Data (63 ) Continuation of application No. 15 /846 , 084, filed on ( 56 ) References Cited Dec . 18 , 2017 , which is a continuation of application U . S . PATENT DOCUMENTS (Continued ) 3 , 872 , 171 A 3 / 1975 Cronin et al. (51 ) Int . Ci. 4 , 957 , 735 A 9 / 1990 Huang A6IK 48 /00 ( 2006 .01 ) (Continued ) A61K 9 / 127 ( 2006 . 01 ) C07C 229 / 12 ( 2006 . 01 ) FOREIGN PATENT DOCUMENTS C07C 271/ 20 ( 2006 .01 ) C07C 279 / 12 ( 2006 .01 ) AU 652831 B2 9 / 1994 C07C 279 / 28 ( 2006 .01 ) CN 102068701 A 5 / 2011 C07C 279 /32 ( 2006 .01 ) (Continued ) C07D 233 / 72 ( 2006 .01 ) C07D 249 /04 ( 2006 .01 ) OTHER PUBLICATIONS CO7D 263/ 20 ( 2006 .01 ) CO7D 265 /33 ( 2006 .01 ) U . S . Appl. No . 15 / 846 ,084 . * C07D 271 /06 ( 2006 . 01 ) (Continued ) C07D 271 / 10 ( 2006 .01 ) CO7D 207/ 27 ( 2006 .01 ) Primary Examiner — Jane J Zara C07D 277 / 38 ( 2006 .01 ) (74 ) Attorney, Agent, or Firm — Cooley LLP ; Heidi A . C07C 275 / 14 ( 2006 . 01 ) Erlacher ; Christine C . Pemberton C07C 279 /24 ( 2006 . 01 ) CO7C 311/ 05 ( 2006 .01 ) C07C 229 / 16 (2006 .01 ) (57 ) ABSTRACT (Continued ) The disclosure features novel lipids and compositions (52 ) U .S . CI. involving the same. Nanoparticle compositions include a CPC .. .. .. C07C 229 / 12 ( 2013 .01 ) ; A61K 9 / 0019 novel lipid as well as additional lipids such as phospholipids , ( 2013 .01 ) ; A61K 9 / 0043 ( 2013 . 01 ) ; A6IK structural lipids, and PEG lipids . Nanoparticle compositions 9 / 0073 (2013 . 01 ) ; A61K 9 / 127 ( 2013 .01 ) ; further including therapeutic and / or prophylactics such as A61K 9 / 1272 ( 2013 . 01 ) ; A61K 9 / 1617 RNA are useful in the delivery of therapeutic and / or pro ( 2013 .01 ) ; A61K 9 / 1641 ( 2013 .01 ) ; A61K phylactics to mammalian cells or organs to , for example , 9 /5123 ( 2013 .01 ) ; A61K 9 /5146 ( 2013 .01 ) ; regulate polypeptide, protein , or gene expression . A61K 31 / 7105 ( 2013 .01 ) ; A61K 38 / 1725 ( 2013 .01 ) ; A61K 38 / 1816 ( 2013 . 01 ) ; A61K 47 /543 ( 2017 . 08 ) ; A61K 47 /6911 ( 2017 .08 ) ; 27 Claims, 11 Drawing Sheets A61K 48 / 005 ( 2013 . 01 ) ; A61K 48 /0033 Specification includes a Sequence Listing . US 10 ,266 ,485 B2 Page 2 Related U . S . Application Data 8 ,663 , 599 B1 3 /2014 Sung et al. 8 ,663 , 700 B2 3 / 2014 Troiano et al. No . 15 /476 ,253 , which is a continuation of applica 8 ,668 , 926 B1 3 / 2014 Mousa et al. tion No. PCT /US2016 /052352 , filed on Sep . 16 , 8 ,685 , 368 B2 4 /2014 Reineke 8 ,691 , 750 B2 4 / 2014 Constein et al . 2016 , now Pat . No. 9 , 868 ,691 . 8 ,697 ,098 B2 4 / 2014 Perumal et al. 8 , 703 , 204 B2 4 / 2014 Bloom et al . (60 ) Provisional application No. 62/ 393 ,940 , filed on Sep . 8 ,709 ,483 B2 4 / 2014 Farokhzad et al. 13 , 2016 , provisional application No. 62 /382 ,740 , 8 ,715 ,736 B2 5 /2014 Sachdeva et al. filed on Sep . 1 , 2016 , provisional application No . 8 ,715 , 741 B2 5 / 2014 Maitra et al . 62 /333 ,557 , filed on May 9 , 2016 , provisional 8 ,728 ,527 B2 5 / 2014 Singh application No. 62 / 266 , 460 , filed on Dec . 11 , 2015 , 8 , 734 ,832 B2 5 / 2014 O 'Hagan et al. 8 , 734 , 846 B2 5 / 2014 Ali et al. provisional application No . 62 / 253, 433 , filed on Nov. 8 ,734 ,853 B2 5 / 2014 Sood et al . 10 , 2015 , provisional application No. 62 /252 ,316 , 8 ,802 ,644 B2 8 / 2014 Chen et al . filed on Nov. 6 , 2015 , provisional application No . 9 ,006 , 487 B2 4 / 2015 Anderson et al . 62/ 220 , 091, filed on Sep . 17 , 2015, provisional 9 ,029 , 590 B2 5 / 2015 Colletti et al . 9 ,394 , 234 B2 7 /2016 Chen et al . application No. 62 / 220 ,085 , filed on Sep . 17 , 2015 . 9 , 867 ,888 B2 1 / 2018 Benenato 9 , 868 ,691 B2 * 1 / 2018 Benenato . A61K 9 /5123 (51 ) Int . Ci. 9 , 868, 692 B2 1 / 2018 Benenato C07C 335 /08 ( 2006 . 01 ) 9 , 868 ,693 B2 1 / 2018 Benenato C07C 233 /36 ( 2006 .01 ) 2003 / 0073619 Al 4 / 2003 Mahato et al . 2003/ 0092653 A1 5 / 2003 Kisich et al. C07C 235 / 10 ( 2006 .01 ) 2004 / 0142474 A1 7 / 2004 Mahato et al . C07C 255 / 24 ( 2006 .01 ) 2006 /0008910 Al 1 /2006 Maclachlan et al. CO7F 9 /09 ( 2006 .01 ) 2006 / 0083780 A1 4 / 2006 Heyes et al . A61K 9 / 16 ( 2006 .01 ) 2006 / 0172003 Al 8 / 2006 Meers et al. A61K 38 / 18 ( 2006 .01 ) 2006 /0204566 Al 9 / 2006 Smyth - Templeton et al . 2007 / 0252295 Al 11/ 2007 Panzner et al. CO7K 14 / 505 ( 2006 . 01 ) 2009 /0042825 Al 2 / 2009 Matar et al . A61K 9 /00 ( 2006 . 01 ) 2009 /0042829 A1 2 / 2009 Matar et al. A61K 47 / 54 ( 2017 . 01 ) 2011 / 0009641 Al 1 / 2011 Anderson et al . A61K 47 /69 (2017 .01 ) 2011 / 0200582 Al 8 /2011 Baryza et al. C07C 227 / 16 ( 2006 .01 ) 2011 /0244026 Al 10 / 2011 Guild et al. 2012 /0136073 A1 5 / 2012 Yang et al . A61K 9 / 51 ( 2006 .01 ) 2012 / 0177724 A1 7 / 2012 Irvine et al. A61K 31/ 7105 ( 2006 . 01) 2012 /0178702 A1 7 /2012 Huang A61K 38 / 17 ( 2006 .01 ) 2012 / 0295832 A1 11/ 2012 Constien et al . C07C 227 / 18 ( 2006 .01 ) 2013 / 0017223 Al 1 / 2013 Hope et al . 2013 / 0064894 Al 3 / 2013 Martin et al . 2013 /0065942 A1 3 /2013 Matar et al . (56 ) References Cited 2013 / 0090372 Al 4 / 2013 Budzik et al . 2013 /0108685 A1 5 /2013 Kuboyama et al. U . S . PATENT DOCUMENTS 2013 / 0115273 Al 5 /2013 Yang et al. 2013 /0115274 A1 5 / 2013 Knopov et al . 5 , 807 , 861 A 9 / 1998 Klein et al . 2013 /0116307 A1 5 /2013 Heyes et al. 6 ,303 , 378 B1 10 / 2001 Bridenbaugh et al . 2013 /0122104 A1 5 / 2013 Yaworski et al. 6 , 395 , 253 B2 5 / 2002 Levy et al . 2013 / 0123338 Al 5 / 2013 Heyes et al . 6 ,652 , 886 B2 11 / 2003 Ahn et al . 2013 / 0129785 Al 5 /2013 Manoharan et al . 6 ,696 ,038 B1 2 / 2004 Mahato et al. 2013 / 0130348 A1 5 / 2013 Gu et al. 7 , 268 , 120 B1 9 / 2007 Horton et al . 2013 / 0142868 A1 6 / 2013 Hoekman et al . 7 , 371 , 404 B2 5 / 2008 Panzner et al. 2013 /0142876 Al 6 / 2013 Howard et al. 7 , 943 , 168 B2 5 / 2011 Schlesinger et al . 2013 /0150625 A1 6 /2013 Budzik et al . 8 , 058 , 069 B2 11/ 2011 Yaworski et al . 2013 / 0156845 Al 6 / 2013 Manoharan et al. 8 , 158 ,601 B2 4 / 2012 Chen et al. 2013 /0156849 Al 6 / 2013 de Fougerolles et al . 8 ,420 , 123 B2 4 / 2013 Troiano et al. 2013 / 0164400 A1 6 / 2013 Knopov et al . 8 ,440 ,614 B2 5 / 2013 Castor 2013 / 0171241 A1 7 / 2013 Geall 8 ,449 , 916 B1 5 / 2013 Bellaire et al . 2013 /0172406 A1 7 / 2013 Zale et al . 8 ,450 , 298 B2 5 / 2013 Mahon et al. 2013 /0178541 A1 7 / 2013 Stanton et al . 8 , 460 ,696 B2 6 / 2013 Slobodkin et al. 2013 /0183244 Al 7 / 2013 Hanes et al . 8 , 460 , 709 B2 6 / 2013 Ausborn et al. 2013 /0183355 A1 7 / 2013 Jain et al . 8 , 563 , 041 B2 10 / 2013 Grayson et al . 2013 / 0183372 Al 7 / 2013 Schutt et al. 8 , 568, 784 B2 10 / 2013 Lillard et al. 2013 / 0183373 Al 7 / 2013 Schutt et al. 8 ,569 , 256 B2 10 /2013 Heyes et al. 2013 /0183375 A1 7 / 2013 Schutt et al . 8 , 580 , 297 B2 11/ 2013 Essler et al . 8 ,603 , 499 B2 12 / 2013 Zale et al. 2013 /0189351 A1 7 / 2013 Geall 8 ,603 , 500 B2 12 / 2013 Zale et al.
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