公开(公告)号：EP4410301A1

公开(公告)日：2024-08-07

申请号：EP21958636.9

申请日：2021-09-28

Applicant: Peking University Shenzhen Graduate School

Inventor： QUAN, Junmin ,  YANG, Zhen ,  LIU, Siyu ,  ZHANG, Qingzhou ,  HU, Minqiang ,  LI, Fengxia ,  FU, Jiamiao ,  ZHU, Zhendong ,  LI, Qinkai

IPC: A61K38/13 ,  A61K47/54 ,  A61P3/10 ,  A61P9/10 ,  A61P35/00

CPC classification number: A61P3/10 ,  A61K47/54 ,  A61K38/13 ,  A61P9/10 ,  A61P35/00

Abstract: The present invention belongs to the technical field of biomedicine, and specifically relates to an extracellular cyclophilin inhibitor and the use thereof, wherein the structural general formula of the extracellular cyclophilin inhibitor of the present invention is as shown in formula (I). According to the present invention, a group capable of reacting with sulfhydryl of cysteine at a specific site on blood albumin is extracted by means of a side chain of a new cyclosporin derivative, and a drug conjugate is rapidly formed after same enters the body, which can effectively restrict the drug to the extracellular area and form targeted inhibition of extracellular cyclophilin, thereby achieving the aim of treating diseases associated therewith.

公开(公告)号：EP4404976A1

公开(公告)日：2024-07-31

申请号：EP22872347.4

申请日：2022-09-22

Applicant: Nutaria Ltd.

Inventor： PORAT, Omer

IPC: A61K47/69

CPC classification number: A61K9/127 ,  A61K47/6911 ,  A61K47/54 ,  A61K45/06 ,  A61K31/522 ,  A61K31/12 ,  A61K9/5107

公开(公告)号：EP4370161A1

公开(公告)日：2024-05-22

申请号：EP22748031.6

申请日：2022-07-11

Applicant: Fondazione Istituto Italiano di Tecnologia ,  The Board of Trustees of the Leland Stanford Junior University ,  Irccs "ospedale Policlinico San Martino"

Inventor： PRIMAVERA, Rosita ,  DECUZZI, Paolo ,  THAKOR, Avnesh S. ,  DE PASCALE, Angelo

IPC: A61K47/69 ,  A61K47/54 ,  A61K47/62 ,  A61K38/28 ,  A61K9/14 ,  A61P3/10

CPC classification number: A61K38/28 ,  A61K47/6927 ,  A61K47/62 ,  A61K47/54 ,  A61P3/10 ,  A61K9/5031 ,  A61K9/0021

公开(公告)号：EP4353268A1

公开(公告)日：2024-04-17

申请号：EP22820607.4

申请日：2022-06-10

Applicant: Nibec Co., Ltd. ,  Seoul National University R&DB Foundation

Inventor： PARK, Yoon Jeong ,  CHUNG, Chong-Pyoung ,  LEE, Jue-Yeon

IPC: A61K48/00 ,  A61K47/64 ,  A61K47/54 ,  A61K47/69 ,  A61K31/7088 ,  A61K31/713 ,  A61P35/00 ,  A61P29/00 ,  A61K9/51

CPC classification number: A61P29/00 ,  A61K47/64 ,  A61K9/51 ,  A61K47/54 ,  A61K48/00 ,  A61K31/713 ,  A61K47/69 ,  A61P35/00 ,  A61K31/7088

Abstract: The present invention relates to a carrier for delivering oligonucleotides into cells for therapeutic use. To inhibit a target protein or promote expression of a target protein in a cell, a peptide-lipid conjugate is prepared, and a nanoparticle consisting of a peptide-lipid conjugate comprising oligonucleotides and a pharmaceutical composition comprising same are provided. It was confirmed that, by using the nanoparticle consisting of a peptide-lipid conjugate according to the present invention, oligonucleotides were effectively delivered into cells. In addition, by confirming that expression of a cancer-causing protein is reduced by the oligonucleotides and an anticancer effect is exhibited in an animal model in which cancer occurs, the nanoparticle consisting of a peptide-lipid conjugate was found to be effective in the delivery of oligonucleotides.

公开(公告)号：EP2640700B1

公开(公告)日：2018-10-31

申请号：EP11793580.9

申请日：2011-11-15

Applicant: Life Technologies Corporation

Inventor： YANG, Zhiwei ,  ANGRISH, Parul ,  DE MOLLERAT DU JEU, Xavier ,  WIEDERHOLT, Kristin ,  WU, Tao

IPC: C07D211/58 ,  A61K48/00 ,  C07C229/16 ,  C07C229/24 ,  C07C229/26 ,  C07C237/06 ,  C07D211/28

CPC classification number: A61K47/54 ,  A61K47/543 ,  A61K48/0008 ,  C07C227/06 ,  C07C229/08 ,  C07D211/28 ,  C07D211/58 ,  C12N15/1137 ,  C12N15/88 ,  C12N2310/11 ,  C12N2310/141 ,  C07C229/26

Abstract: There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.

公开(公告)号：EP2751120B1

公开(公告)日：2018-08-22

申请号：EP12781045.5

申请日：2012-09-20

Applicant: MedImmune Limited

Inventor： HOWARD, Philip Wilson

IPC: C07D519/00

CPC classification number: C07D487/04 ,  A61K47/54 ,  A61K47/55 ,  A61K47/60 ,  C07D519/00 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06156 ,  C07K5/06165

Abstract: A compound with the formula I wherein: R2 is of formula II where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl, as well as drug-linkers and drug-conjugates made from this compound.

公开(公告)号：EP3143032B1

公开(公告)日：2018-08-01

申请号：EP15722218.3

申请日：2015-05-13

Applicant: Institut Gustave Roussy

Inventor： PACI, Angelo ,  MARTENS, Thierry ,  RIVARD, Michaël ,  DESMAËLE, Didier ,  SKARBEK, Charles ,  COUVREUR, Patrick

IPC: C07F9/6584 ,  A61K9/14 ,  B82Y5/00 ,  A61P35/00 ,  A61K31/675 ,  A61K47/54

CPC classification number: A61K31/664 ,  A61K31/185 ,  A61K47/54 ,  C07F9/65846

Abstract: The present invention relates to novel derivatives of oxazaphosphorines, pharmaceutical compositions and therapeutic uses thereof, in particular for treating or preventing cancer.

公开(公告)号：EP2306986B1

公开(公告)日：2018-03-21

申请号：EP09771199.8

申请日：2009-06-26

Applicant: Prolynx LLC

Inventor： SANTI, Daniel, V. ,  ASHLEY, Gary ,  HEARN, Brian

IPC: A61K47/60 ,  A61K47/54 ,  A61K47/65

CPC classification number: A61K47/60 ,  A61K47/54 ,  C08G65/329 ,  C08G65/33317 ,  C08G65/33396 ,  C08L2203/02

Abstract: The present invention provides methods and compositions that permit controlled and prolonged drug release in vivo. The compounds are either prodrugs with tunable rates of release, or conjugates of the drug with macromolecules which exhibit tunable controlled rates of release.

公开(公告)号：EP3151817A4

公开(公告)日：2018-01-17

申请号：EP15803408

申请日：2015-06-05

Applicant: THE SCRIPPS RES INSTITUTE

Inventor： DONG JIAJIA ,  SHARPLESS K BARRY ,  KELLY JEFFERY W ,  BARANCZAK ALEKSANDRA ,  CHEN WENTAO

IPC: A61K31/10 ,  A61K31/16

CPC classification number: A61K47/48023 ,  A61K31/05 ,  A61K31/136 ,  A61K31/14 ,  A61K31/197 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4168 ,  A61K31/4245 ,  A61K31/4353 ,  A61K31/439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/485 ,  A61K31/505 ,  A61K31/515 ,  A61K31/53 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/65 ,  A61K31/655 ,  A61K31/70 ,  A61K31/7048 ,  A61K38/31 ,  A61K47/54 ,  A61K51/0497 ,  C07C305/26 ,  C07C2601/14 ,  C07C2603/18 ,  C07D277/82 ,  C07D295/088 ,  C07D295/185 ,  C07D295/26 ,  C07K1/02 ,  C07K1/1136 ,  C07K2/00

Abstract: This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

公开(公告)号：EP2287305B2

公开(公告)日：2017-11-29

申请号：EP10008929.1

申请日：2003-02-20

Applicant: Sirna Therapeutics, Inc.

Inventor： Mcswiggen, James ,  Beigelman, Leonid ,  Chowrira, Bharat ,  Pavco, Pamela ,  Fosnaugh, Kathy ,  Jamison, Sharon ,  Usman, Nassim ,  Thompson, James

IPC: C12N15/113 ,  A61K31/713

CPC classification number: C12N15/8218 ,  A61K38/00 ,  A61K47/54 ,  C07H21/02 ,  C12N15/111 ,  C12N15/1131 ,  C12N15/1138 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/315 ,  C12N2310/317 ,  C12N2310/318 ,  C12N2310/321 ,  C12N2310/322 ,  C12N2310/332 ,  C12N2310/344 ,  C12N2310/346 ,  C12N2310/53 ,  C12N2320/51 ,  C12N2330/30 ,  Y02A50/393 ,  C12N2310/3521

Abstract: The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.