Muthusamy Te Jayaraman

US Patent:

8158601, Apr 17, 2012

Filed:

Jun 10, 2010

Appl. No.:

12/813448

Inventors:

Jianxin Chen - Cambridge MA, US
Steven Ansell - Cambridge MA, US
Akin Akinc - Cambridge MA, US
Joseph Robert Dorkin - Cambridge MA, US
Xiaojun Qin - Cambridge MA, US
William Cantley - Cambridge MA, US
Muthiah Manoharan - Cambridge MA, US
Jayaprakash K. Narayanannair - Cambridge MA, US
Muthusamy Jayaraman - Cambridge MA, US

Assignee:

Alnylam Pharmaceuticals, Inc. - Cambridge MA

International Classification:

A61K 31/70
A61K 47/00
C07C 229/00

US Classification:

514 44, 554103, 514785

Abstract:

The invention features a cationic lipid of formula I,Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.

US Patent:

8507455, Aug 13, 2013

Filed:

Dec 4, 2008

Appl. No.:

12/328537

Inventors:

Muthiah Manoharan - Weston MA, US
Muthusamy Jayaraman - Sharon MA, US
Jayaprakash K. Narayanannair - Wakefield MA, US

Assignee:

Alnylam Pharmaceuticals, Inc. - Cambridge MA

International Classification:

C12N 15/11
A61K 48/00
C07H 21/02
C07H 21/04

US Classification:

514 44A, 536 245

Abstract:

The present invention provides iRNA agent including at least one monomer having the structure shown in formula (I′).

US Patent:

8575123, Nov 5, 2013

Filed:

Apr 10, 2009

Appl. No.:

12/936961

Inventors:

Muthiah Manoharan - Cambridge MA, US
David Butler - Cambridge MA, US
Muthusamy Jayaraman - Cambridge MA, US

Assignee:

Tekmira Pharmaceuticals Corporation - Burnaby, BC

International Classification:

A61K 48/00
C12N 15/11
C12N 15/00
A01N 63/00
A01N 65/00

US Classification:

514 44R, 424 931, 4353201

Abstract:

The invention relates to compositions and methods for site-specific delivery of nucleic acids by combining them with targeting ligands and endosomolytic components.

US Patent:

8642076, Feb 4, 2014

Filed:

Aug 16, 2011

Appl. No.:

13/211094

Inventors:

Muthiah Manoharan - Cambridge MA, US
Akin Akinc - Cambridge MA, US
Muthusamy Jayaraman - Cambridge MA, US
Martin Maier - Cambridge MA, US

Assignee:

Tekmira Pharmaceuticals Corporation - Burnaby, British Columbia

International Classification:

A61K 9/48

US Classification:

424451

Abstract:

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.

US Patent:

20090247608, Oct 1, 2009

Filed:

Dec 4, 2008

Appl. No.:

12/328669

Inventors:

Muthiah Manoharan - Weston MA, US
Muthusamy Jayaraman - Sharon MA, US

Assignee:

ALNYLAM PHARMACEUTICALS, INC. - Cambridge MA

International Classification:

A61K 31/713
C07K 14/00
A61K 47/42
A61K 31/7088
C07K 7/04
C07K 5/04
A61K 47/12

US Classification:

514 44 A, 530324, 514773, 514 44 R, 530330, 530326, 530325, 530327, 530328, 514784

Abstract:

The present invention provides targeting lipids of structurewhere Lis a lipid, lipophile, alkyl, alkenyl or alkynyl, Lis a ligand or —CHCH(OCHCH)O(CH)CH-ligand, p is 1-1000, and q is 1-20. In addition, the invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo.

US Patent:

20110311582, Dec 22, 2011

Filed:

Nov 10, 2009

Appl. No.:

13/128283

Inventors:

Muthiah Manoharan - Cambridge MA, US
Muthusamy Jayaraman - Cambridge MA, US
laxman Eltepu - Cambridge MA, US
Steven Ansell - Cambridge MA, US
Jianxin Chen - Cambridge MA, US

International Classification:

A61K 39/12
C07D 203/08
A61K 47/44
A61K 31/7088
A61K 31/7105
A61K 31/713
C12N 5/071
C12N 15/85
A61K 39/00
A61K 39/02
A61P 37/04
A61P 31/12
A61P 31/04
A61P 33/00
A61P 35/00
C07C 229/30

US Classification:

4242041, 554103, 548968, 514785, 514 44 R, 4242781, 514 44 A, 435375, 435455, 4241841, 4242771, 4242341, 4242651

Abstract:

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention formula (I) provides lipids having the following structure XXXIII wherein: Rand Rare each independently for each occurrence optionally substituted C-Calkyl, optionally substituted C-Calkenyl, optionally substituted C-Calkynyl, optionally substituted C-Cacyl, or -linker-ligand; Ris H, optionally substituted C-Calkyl, optionally substituted C-Calkenyl, optionally substituted C-Calkynyl, alky lhetro cycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).

US Patent:

20110311583, Dec 22, 2011

Filed:

Nov 10, 2009

Appl. No.:

13/128287

Inventors:

Muthiah Manoharan - Cambridge MA, US
Muthusamy Jayaraman - Cambridge MA, US
David Butler - Medford MA, US
Jayaprakash K. Narayanannair - Cambridge MA, US
Martin Maier - Cambridge MA, US
Laxman Eltepu - carlsbad CA, US

Assignee:

ALNYLAM PHARMACEUTICALS, INC. - Cambridge MA

International Classification:

A61K 39/12
A61K 47/08
C07J 41/00
A61K 47/28
C07C 211/22
A61K 47/16
C07C 211/21
C07D 211/72
A61K 47/22
C07C 251/78
C07C 279/12
C07C 271/12
A61K 48/00
A61K 31/713
C12N 5/00
A61K 39/39
A61K 39/00
A61K 39/02
A61P 37/04
A61P 31/12
A61P 31/04
A61P 33/00
C07C 49/203

US Classification:

4242041, 568417, 514772, 552544, 514788, 564509, 546244, 564147, 564240, 560157, 514785, 514 44 R, 514 44 A, 435375, 4242831, 4241841, 4242771, 4242341, 4242651

Abstract:

(A1) Translate this text The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ?-aminoalkyls, ?-(substituted)aminoalkyls, ?-phosphoalkyls, ?-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(0)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ?-aminoalkyl, ?-(substituted)aminoalky, ?-phosphoalkyl or ?-thiophosphoalkyl.

US Patent:

20120027796, Feb 2, 2012

Filed:

Nov 10, 2009

Appl. No.:

13/128253

Inventors:

Muthiah Manoharan - Cambridge MA, US
David Butler - Medford MA, US
Jayaprakash K. Narayanannair - Cambridge MA, US
Muthusamy Jayaraman - Cambridge MA, US

Assignee:

ALNYLAM PHARMACEUTICALS, INC. - Cambridge MA

International Classification:

A61K 39/12
C07D 317/44
C07D 317/46
C07D 493/04
C07D 317/70
C07D 491/113
C07D 317/28
C07D 317/72
C07F 9/655
A61K 47/44
A61K 31/7088
A61K 31/713
C12N 5/071
A61K 39/39
A61K 39/00
A61K 39/02
A61P 37/04
A61P 31/04
A61P 31/12
A61P 33/00
A61P 35/00
C07D 491/056

US Classification:

4242041, 548453, 546115, 549439, 549440, 549435, 549433, 540593, 546 19, 549451, 549341, 540543, 548409, 548952, 549220, 514785, 514 44 R, 4242781, 514 44 A, 435375, 4241841, 4242771, 4242341, 4242651, 514788

Abstract:

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).