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公开(公告)号：US10195145B2
公开(公告)日：2019-02-05
申请号：US15283179
申请日：2016-09-30
发明人： Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Violetta Akopian , Yasunobu Tanaka , Elena Feinstein , Sharon Avkin-Nahum , Hagar Kalinski , Igor Mett , Kenjiro Minomi , Wenbin Ying , Yun Liu
IPC分类号： C12N15/113 , A61K9/127 , C12N15/11 , A61K31/713 , C07H21/02
摘要： 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.
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公开(公告)号：US10093923B2
公开(公告)日：2018-10-09
申请号：US14924284
申请日：2015-10-27
发明人： Xiaomei Jin , Lei Yu , Hirokazu Takahashi , Yasunobu Tanaka , Yoshiro Niitsu , Elena Feinstein , Sharon Avkin-Nachum , Hagar Kalinski , Igor Mett , Shai Erlich , Elizabeth C Squiers , Ning Chen
IPC分类号： C07H21/04 , C12N15/113 , A61K31/713
摘要： 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.
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公开(公告)号：US20170081663A1
公开(公告)日：2017-03-23
申请号：US15284494
申请日：2016-10-03
发明人： Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Violetta Akopian , Yasunobu Tanaka , Elena Feinstein , Sharon Avkin-Nahum , Hagar Kalinski , Igor Mett , Kenjiro Minomi , Wenbin Ying , Yun Liu , Zheng Hou , John A. Gaudette , Priya Karmali , Sridhar C. Nagarajan
IPC分类号： C12N15/113 , A61K47/18 , A61K47/24 , A61K31/713
CPC分类号： C12N15/113 , A61K9/0048 , A61K9/127 , A61K9/1271 , A61K31/713 , A61K45/06 , A61K47/18 , A61K47/186 , A61K47/24 , C07H21/02 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2320/32
摘要： 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.
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公开(公告)号：US20160208255A1
公开(公告)日：2016-07-21
申请号：US14979568
申请日：2015-12-28
发明人： Yoshiro Niitsu , Kenjirou Minomi , Jens Harborth , Cima Cina , Kwok Yin Tsang , Wenbin Ying , Hirokazu Takahashi
IPC分类号： C12N15/113
CPC分类号： A61B5/0071 , A61K31/713 , A61K49/0021 , C07D311/30 , C07F9/6533 , C12N15/113 , C12N15/1135 , C12N15/1137 , C12N2310/14 , C12N2310/322 , C12N2310/344 , C12N2310/3515 , C12N2310/531 , C12N2320/30 , C12N2320/32 , C12N2320/35 , C12N2320/53 , C12Q1/02 , G01N33/582 , H05K999/99 , C12N2310/3533 , C12N2310/3531 , C12N2310/321 , C12N2310/3521
摘要： This invention provides compounds, compositions and methods for modulating the expression of human p21 using RNA interference. The RNA interference molecules can be used in methods for preventing or treating diseases such as malignant tumor. A nucleic acid molecule can have a) a polynucleotide sense strand and a polynucleotide antisense strand; b) each strand of the molecule being from 15 to 30 nucleotides in length; c) a contiguous region of from 15 to 30 nucleotides of the antisense strand being complementary to a sequence of an mRNA encoding p21; and d) at least a portion of the sense strand can be complementary to at least a portion of the antisense strand, and the molecule has a duplex region of from 15 to 30 nucleotides in length.
摘要翻译： 本发明提供了使用RNA干扰来调节人p21的表达的化合物，组合物和方法。 RNA干扰分子可用于预防或治疗恶性肿瘤等疾病的方法。 核酸分子可具有a）多核苷酸有义链和多核苷酸反义链; b）分子的每条链长度为15至30个核苷酸; c）反义链的15至30个核苷酸的连续区域与编码p21的mRNA的序列互补; 和d）所述有义链的至少一部分可以与所述反义链的至少一部分互补，并且所述分子具有长度为15至30个核苷酸的双链体区。
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5.发明申请METHODS AND COMPOSITIONS FOR TREATING MALIGNANT TUMORS ASSOCIATED WITH KRAS MUTATION 有权用于治疗与KRAS突变相关的恶性肿瘤的方法和组合物公开(公告)号：US20160186183A1
公开(公告)日：2016-06-30
申请号：US14979573
申请日：2015-12-28
发明人： Yoshiro Niitsu , Kenjirou Minomi , Hiroki Nishita , Yusuke Nakashima , Miyono Miyazaki , Keiko Kajiwara , Jihua Liu , Li Wang , Jens Harborth , Bharat Majeti , Roger Adami , Wenbin Ying
IPC分类号： C12N15/113
CPC分类号： C07F9/6533 , A61K31/713 , C12N15/113 , C12N15/1135 , C12N15/1137 , C12N2310/14 , C12N2310/322 , C12N2310/344 , C12N2310/3515 , C12N2310/531 , C12N2320/30 , C12N2320/32 , C12N2320/35 , C12N2320/53 , C12Q1/02 , G01N33/582 , H05K999/99 , C12N2310/3533 , C12N2310/3531 , C12N2310/321 , C12N2310/3521
摘要： This invention provides methods and compositions for preventing, treating or ameliorating one or more symptoms of a malignant tumor associated with KRAS mutation in a mammal in need thereof, by identifying a tumor cell in the mammal, the tumor cell comprising at least one of: (i) a mutation of the KRAS gene, and (ii) an aberrant expression level of KRAS protein; and administering to the mammal a therapeutically effective amount of a composition comprising one or more RNAi molecules that are active in reducing expression of GST-π.
摘要翻译： 本发明提供了通过鉴定哺乳动物的肿瘤细胞来预防，治疗或改善与有需要的哺乳动物有关的KRAS突变相关的恶性肿瘤的一种或多种症状的方法和组合物，所述肿瘤细胞包含以下至少一种：（ i）KRAS基因的突变，和（ii）KRAS蛋白的异常表达水平; 以及向哺乳动物施用治疗有效量的包含一种或多种在降低GST-和pgr表达中有活性的RNAi分子的组合物。
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公开(公告)号：US20130267581A1
公开(公告)日：2013-10-10
申请号：US13921049
申请日：2013-06-18
发明人： Yoshiro Niitsu
IPC分类号： A61K47/10 , C12N15/113
CPC分类号： A61K47/10 , A61K9/1272 , A61K31/07 , A61K31/7105 , A61K45/06 , A61K47/551 , A61K47/6911 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2320/32 , A61K2300/00
摘要： Disclosed is a substance delivery carrier for an extracellular-matrix-producing cell in the bone marrow, which comprises a retinoid. Also disclosed in an agent for treating myelofibrosis by utilizing a substance capable of regulating the activity or proliferation of an extracellular-matrix-producing cell in the bone marrow.
摘要翻译： 公开了骨髓中细胞外基质产生细胞的物质递送载体，其包含类视色素。 还通过利用能够调节骨髓中细胞外基质产生细胞的活性或增殖的物质来治疗骨髓纤维化的药剂中也公开。
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公开(公告)号：US20190275158A1
公开(公告)日：2019-09-12
申请号：US16345205
申请日：2017-11-01
IPC分类号： A61K47/54 , A61K31/7105 , A61K45/06 , A61P17/00 , A61K47/34 , A61K47/10 , A61K47/20 , A61K47/24 , A61K47/22 , A61K47/18 , A61K9/127
摘要： The present invention relates to: a carrier for delivering a retinoid-containing substance used by extracellular-matrix-producing cells in the skin; a skin fibrosis treatment agent using said carrier; a preparation kit for said treatment agent; a production method for said carrier; and a production method for said treatment agent.
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公开(公告)号：US20180208547A1
公开(公告)日：2018-07-26
申请号：US15919098
申请日：2018-03-12
发明人： Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Zheng Hou , John A. Gaudette , Violetta Akopian , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Priya Karmali , Sridhar C. Nagarajan
IPC分类号： C07C237/08 , C12N15/113 , C07C333/04 , C07C323/60 , A61K47/18 , A61K47/54 , A61K9/127 , A61K9/10 , A61K9/00 , A61K31/713
CPC分类号： C07C237/08 , A61K9/0019 , A61K9/10 , A61K9/1271 , A61K31/713 , A61K47/186 , A61K47/543 , C07C323/60 , C07C333/04 , C12N15/113
摘要： Here described is a method of delivery of a drug to a stellate cell using a composition comprising a compound of formula I: wherein R1 and R2 are independently selected from C10 to C18 alkyl, C12 to C18 alkenyl, and oleoyl; R3 and R4 are independently selected from C1 to C6 alkyl and C2 to C6 alkanol; X is selected from —CH2—, —S—, and —O—, or X is absent; Y is selected from —(CH2)n, —S(CH2)n—, —O(CH2)n—, -thiophene-, -SO2(CH2)n—, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Z− is a counterion.
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公开(公告)号：US09976142B2
公开(公告)日：2018-05-22
申请号：US15301258
申请日：2015-04-01
IPC分类号： A61K38/00 , C12N15/113 , A61K9/127 , A61K31/713 , A61K38/17 , A61K47/64 , C12N15/11
CPC分类号： C12N15/113 , A61K9/1271 , A61K31/713 , A61K38/00 , A61K38/1703 , A61K47/64 , C12N15/111 , C12N2310/14 , C12N2320/32
摘要： Provided are: a targeting molecule targeting a target cell which is selected from the group consisting of a stellate cell, a myofibroblast, a cancer-associated fibroblast, a tumor cell and a cell expressing STRA6, said targeting molecule being selected from the group consisting of (1) a peptide containing an amino acid sequence in the cell-binding region of RBP, (2) a variant peptide of the aforesaid peptide (1), said variant peptide having a comparable targetability to peptide (1), and (3) a peptide mimetic having a comparable targetability to peptide (1) or peptide (2); a targeting agent, a carrier, a complex and a medicinal composition each comprising the targeting molecule; a method for treating, examining, diagnosing or monitoring a disease related to the aforesaid target cell; a method for labeling, detecting or imaging the target cell, etc.
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公开(公告)号：US09963424B2
公开(公告)日：2018-05-08
申请号：US15005569
申请日：2016-01-25
发明人： Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Zheng Hou , John A. Gaudette , Violetta Akopian , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Priya Karmali , Sridhar C. Nagarajan
IPC分类号： A61K9/10 , A61K31/713 , C07C237/08 , A61K9/00 , A61K9/127 , A61K47/18 , C12N15/113 , C07C323/60 , C07C333/04 , A61K47/54
CPC分类号： C07C237/08 , A61K9/0019 , A61K9/10 , A61K9/1271 , A61K31/713 , A61K47/186 , A61K47/543 , C07C323/60 , C07C333/04 , C12N15/113
摘要： Here described are compounds of formula I: wherein R1 and R2 are independently selected from C10 to C18 alkyl, C12 to C18 alkenyl, and oleoyl; R3 and R4 are independently selected from C1 to C6 alkyl and C2 to C6 alkanol; X is selected from —CH2—, —S—, and —O—, or X is absent; Y is selected from —(CH2)n, —S(CH2)n—, —O(CH2)n—, -thiophene-, —SO2(CH2)n—, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Z− is 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.
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