Nitto-Denko Corporation

Yasunobu Tanaka

Yoshiro Niitsu

Joseph E Payne

Mohammad Ahmadian

Richard P Witte

Victor Knopov

Violetta Akopian

Loren A Perelman

John Gaudette

Zheng Hou

Elena Feinstein

Igor Mett

Hagar Kalinski

Lei Yu

Priya Prakash Karmali

Kenjiro Minomi

Sridhar C Nagarajan

Wenbin Ying

Sharon Avkin-Nahum

Yun Liu

Sharon Avkin-Nachum

Hirokazu Takahashi

Shai Erlich

Elizabeth C Squiers

Ning Chen

Xiaomei Jin

Sang Van

John A Gaudette

C Nagarajan Sridhar

Priya Karmali

Gang Zhao

Shouping Ji

Rishu Takimoto

Keiko Kajiwara

Miyono Miyazaki

Sharon Avkin-nachum

Kiminori Nakamura

Yun Lui

Here described is a composition comprising a compound of formula I: wherein Rand Ris independently selected from a group consisting of Cto Calkyl, Cto Calkenyl, and oleoyl group; Rand Rare independently selected from a group consisting of Cto Calkyl, and Cto Calkanol; X is selected from a group consisting of &#x2014;CH&#x2014;, &#x2014;S&#x2014;, and &#x2014;O&#x2014; or absent; Y is selected from &#x2014;(CH), &#x2014;S(CH), &#x2014;O(CH)&#x2014;, thiophene, &#x2014;SO(CH)&#x2014;, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Zis a counterion.

Cationic lipids for therapeutic agent delivery formulations

Here described are compounds consisting of the structure(targeting molecule)-linker-(targeting molecule),wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

Compounds for targeting drug delivery and enhancing siRNA activity

Here described is a method of delivery of a drug to a stellate cell using a composition comprising a compound of formula I: wherein Rand Rare independently selected from Cto Calkyl, Cto Calkenyl, and oleoyl; Rand Rare independently selected from Cto Calkyl and Cto Calkanol; X is selected from &#x2014;CH&#x2014;, &#x2014;S&#x2014;, and &#x2014;O&#x2014;, or X is absent; Y is selected from &#x2014;(CH), &#x2014;S(CH)&#x2014;, &#x2014;O(CH)&#x2014;, -thiophene-, &#x2014;SO(CH)&#x2014;, and ester; n&#x2550;1-4; a&#x2550;1-4; b&#x2550;1-4; c&#x2550;1-4; and Zis a counterion.

What is described is a method for treating a fibrotic disease by administering a pharmaceutical composition comprising a drug carrier, which comprises a lipid and a retinoid, and a double-stranded nucleic acid molecule, which comprises an antisense sequence to mRNA encoding human hsp47.

Method for treating fibrosis using siRNA and a retinoid-lipid drug carrier

What is described is a pharmaceutical composition for treating a fibrotic disease comprising a drug carrier, which comprises a lipid and a retinoid, and a double-stranded nucleic acid molecule, which comprises an antisense sequence to mRNA encoding human hsp47.

Retinoid-lipid drug carrier

Here described are compounds consisting of the structure

Provided herein are compositions, methods and kits for modulating expression of target genes, particularly heat shock protein 47 (hsp47). The compositions, methods and kits may include nucleic acid molecules (for example, short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA) or short hairpin RNA (shRNA)) that modulate a gene encoding hsp47, for example, the gene encoding human hsp47. The composition and methods disclosed herein may also be used in treating conditions and disorders associated with hsp47 such as liver fibrosis, pulmonary fibrosis, peritoneal fibrosis and kidney fibrosis.

Modulation of HSP47 expression

Here described are compounds of formula I: wherein Rand Rare independently selected from Cto Calkyl, Cto Calkenyl, and oleoyl; Rand Rare independently selected from Cto Calkyl and Cto Calkanol; X is selected from &#x2014;CH&#x2014;, &#x2014;S&#x2014;, and &#x2014;O&#x2014;, or X is absent; Y is selected from &#x2014;(CH), &#x2014;S(CH)&#x2014;, &#x2014;O(CH)&#x2014;, -thiophene-, &#x2014;SO(CH)&#x2014;, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Zis a counterion. Also described herein are compositions and pharmaceutical formulations including compounds of formula I which are useful for the delivery of therapeutic agents, and methods of using these compositions and formulations.

Here described are compounds of formula I: wherein Rand Ris independently selected from a group consisting of Cto Calkyl, Cto Calkenyl, and oleyl group; wherein Rand Rare independently selected from a group consisting of Cto Calkyl, and Cto Calkanol; wherein X is selected from a group consisting of &#x2014;CH&#x2014;, &#x2014;S&#x2014;, and &#x2014;O&#x2014; or absent; wherein Y is selected from &#x2014;(CH), &#x2014;S(CH), &#x2014;O(CH)&#x2014;, thiophene, &#x2014;SO(CH)&#x2014;, and ester, wherein n=1-4; wherein a=1-4; wherein b=1-4; wherein c=1-4; and wherein Z is a counterion; as well as compositions and pharmaceutical formulations including compounds of formula I which are useful for the delivery of therapeutic agents; and methods of using these compositions and formulations.

What is described are pharmaceutical compositions comprising a double-stranded nucleic acid molecule comprising a sense strand and an antisense strand wherein the sense and antisense strands are selected from the oligonucleotides described as SERPINH1_2 (SEQ ID NOS: 60 and 127), SERPINH1_45a (SEQ ID NOS: 98 and 165), and SERPINH1_51 (SEQ ID NOS: 101 and 168), and drug carrier comprising a mixture of a retinoid and a lipid vesicle, and methods of using these pharmaceutical compositions to treat a disease associated with hsp47 expression, including fibrosis.

Retinoid-liposomes for treating fibrosis

Growing community of inventors

Osaka, Japan

Yasunobu Tanaka