CN102596922A - 有效的缀合物和亲水性连接体 - Google Patents
有效的缀合物和亲水性连接体 Download PDFInfo
- Publication number
- CN102596922A CN102596922A CN2009801623736A CN200980162373A CN102596922A CN 102596922 A CN102596922 A CN 102596922A CN 2009801623736 A CN2009801623736 A CN 2009801623736A CN 200980162373 A CN200980162373 A CN 200980162373A CN 102596922 A CN102596922 A CN 102596922A
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- Prior art keywords
- cell
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- antibody
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- binding agent
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Cell Biology (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2009/059620 WO2010126551A1 (en) | 2009-04-30 | 2009-10-06 | Potent conjugates and hydrophilic linkers |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102596922A true CN102596922A (zh) | 2012-07-18 |
Family
ID=46467238
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009801623736A Pending CN102596922A (zh) | 2009-10-06 | 2009-10-06 | 有效的缀合物和亲水性连接体 |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP2486023A4 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2013506709A (cg-RX-API-DMAC7.html) |
| KR (1) | KR20120080611A (cg-RX-API-DMAC7.html) |
| CN (1) | CN102596922A (cg-RX-API-DMAC7.html) |
| IL (1) | IL219020A0 (cg-RX-API-DMAC7.html) |
| IN (1) | IN2012DN02780A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2010126551A1 (cg-RX-API-DMAC7.html) |
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103044677A (zh) * | 2012-12-28 | 2013-04-17 | 上海景宇生物科技有限公司 | 一种异端基遥爪聚乙二醇及其制备方法 |
| CN103083652A (zh) * | 2013-02-06 | 2013-05-08 | 中国科学院过程工程研究所 | 一种以异型双功能试剂为连接桥的脑膜炎多糖结合疫苗及其制备方法 |
| CN103254311A (zh) * | 2013-05-09 | 2013-08-21 | 齐鲁制药有限公司 | 一种制备抗体-美登素类生物碱药物偶联物的方法 |
| CN103483357A (zh) * | 2013-10-12 | 2014-01-01 | 齐鲁制药有限公司 | 一种抗体-美登素偶联物的中间体新晶型及其制备方法 |
| CN105188763A (zh) * | 2013-03-13 | 2015-12-23 | 诺华股份有限公司 | 抗体药物缀合物和相应的抗体 |
| CN105435241A (zh) * | 2015-12-10 | 2016-03-30 | 浙江大学 | 一种iRGD-抗癌药物偶联物及其制备方法和应用 |
| CN105530942A (zh) * | 2013-08-26 | 2016-04-27 | 瑞泽恩制药公司 | 包含大环内酯类非对映异构体的药物组合物、其制备方法和治疗用途 |
| CN112543770A (zh) * | 2018-06-26 | 2021-03-23 | 伊缪诺金公司 | 靶向adam9的免疫缀合物及其使用方法 |
| CN113842468A (zh) * | 2014-09-02 | 2021-12-28 | 伊缪诺金公司 | 用于配制抗体药物缀合物组合物的方法 |
| CN114502201A (zh) * | 2019-08-28 | 2022-05-13 | 星药私人有限公司 | 靶向性树枝状体缀合物 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105175434A (zh) | 2009-02-05 | 2015-12-23 | 伊缪诺金公司 | 新型苯并二氮杂*衍生物 |
| EP3620467A1 (en) | 2010-03-12 | 2020-03-11 | Debiopharm International SA | Cd37-binding molecules and immunoconjugates thereof |
| CN103313990B (zh) * | 2010-11-17 | 2016-07-20 | 基因泰克公司 | 丙氨酰美登醇抗体偶联物 |
| WO2012086857A1 (ko) * | 2010-12-21 | 2012-06-28 | (주)파낙스이엠 | 광역학 진단 또는 치료를 위한 결합체 및 이의 제조방법 |
| DK2675480T3 (en) | 2011-02-15 | 2019-04-15 | Immunogen Inc | PROCEDURES FOR PREPARING CONJUGATES |
| MX2013011385A (es) * | 2011-04-01 | 2014-03-13 | Immunogen Inc | Moleculas de union a cd37 y sus inmunoconjugados. |
| MX2014006087A (es) * | 2011-11-21 | 2014-08-01 | Immunogen Inc | Metodo de tratamiento de tumores que son resistentes a terapias contra el receptor del factor de crecimiento epidermico (egfr) con agentes citotoxicos conjugados con anticuerpos dirigidos contra el receptor del factor de crecimiento epidermico. |
| WO2014089177A2 (en) | 2012-12-04 | 2014-06-12 | Massachusetts Institute Of Technology | Compounds, conjugates and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines |
| US9415118B2 (en) * | 2013-03-13 | 2016-08-16 | Novartis Ag | Antibody drug conjugates |
| MY183572A (en) | 2013-03-15 | 2021-02-26 | Regeneron Pharma | Biologically active molecules, conjugates thereof, and therapeutic uses |
| US10208125B2 (en) | 2013-07-15 | 2019-02-19 | University of Pittsburgh—of the Commonwealth System of Higher Education | Anti-mucin 1 binding agents and uses thereof |
| MX2016001541A (es) * | 2013-08-02 | 2016-08-18 | Sanofi Sa | Uso de anticuerpo inmunoconjugado anti-muc1 maitansinoide para el tratamiento de tumores solidos. |
| CA3187392A1 (en) | 2013-10-15 | 2015-04-23 | Seagen Inc. | Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics |
| AU2015210578B2 (en) * | 2014-01-29 | 2020-04-16 | Jiangsu Hengrui Medicine Co., Ltd. | Ligand-cytotoxic drug conjugate, preparation method therefor, and uses thereof |
| GB201402009D0 (en) | 2014-02-06 | 2014-03-26 | Oncomatryx Biopharma S L | Antibody-drug conjugates and immunotoxins |
| EP3125943A4 (en) * | 2014-04-04 | 2017-12-06 | Merck Sharp & Dohme Corp. | Phosphate based linkers for intracellular delivery of drug conjugates |
| US12174205B2 (en) | 2014-04-17 | 2024-12-24 | Northwestern University | Phosphatidylethanolamine-specific probes |
| US9982045B2 (en) * | 2014-08-12 | 2018-05-29 | Novartis Ag | Anti-CDH6 antibody drug conjugates |
| US10456479B2 (en) * | 2015-03-19 | 2019-10-29 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and ligand-drug conjugates thereof |
| MX386328B (es) | 2015-03-27 | 2025-03-18 | Regeneron Pharma | Derivados de maitansinoide, conjugados de los mismos, y metodos de uso. |
| BR112017026027A2 (pt) | 2015-06-08 | 2018-08-14 | Debiopharm Int Sa | combinações de imunoconjugado anti-cd37 e anticorpo anti-cd20 |
| AU2016297087B2 (en) | 2015-07-21 | 2021-02-18 | Immunogen, Inc | Methods of preparing cytotoxic benzodiazepine derivatives |
| MA42706A (fr) | 2015-08-28 | 2021-04-14 | Debiopharm Int Sa | Anticorps et dosages pour la détection de cd37 |
| CA3006000A1 (en) | 2015-12-04 | 2017-06-08 | Seattle Genetics, Inc. | Conjugates of quaternized tubulysin compounds |
| US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| MX390630B (es) | 2016-01-25 | 2025-03-21 | Regeneron Pharma | Derivados de maitansinoide, conjugados de los mismos y metodos de uso. |
| JP7073266B2 (ja) | 2016-03-25 | 2022-05-23 | シージェン インコーポレイテッド | Peg化薬物リンカー及びその中間体を調製するためのプロセス |
| US10918627B2 (en) | 2016-05-11 | 2021-02-16 | Massachusetts Institute Of Technology | Convergent and enantioselective total synthesis of Communesin analogs |
| GB201615725D0 (en) | 2016-09-15 | 2016-11-02 | Polytherics Ltd | Novel cytotoxic agents and conjugates thereof |
| US10772972B2 (en) * | 2016-09-23 | 2020-09-15 | Regeneron Pharmaceuticals, Inc. | Anti-STEAP2 antibody drug conjugates, and compositions and uses thereof |
| JP2020510608A (ja) | 2016-11-02 | 2020-04-09 | デビオファーム インターナショナル, エス. アー. | 抗cd37イムノコンジュゲート療法を改善するための方法 |
| EP3554544A4 (en) | 2016-12-16 | 2020-07-29 | Bluefin Biomedicine, Inc. | ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE |
| US11730822B2 (en) | 2017-03-24 | 2023-08-22 | Seagen Inc. | Process for the preparation of glucuronide drug-linkers and intermediates thereof |
| WO2018209239A1 (en) | 2017-05-11 | 2018-11-15 | Massachusetts Institute Of Technology | Potent agelastatin derivatives as modulators for cancer invasion and metastasis |
| US10646585B2 (en) | 2017-09-15 | 2020-05-12 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and ligand-drug conjugates thereof |
| US10640508B2 (en) | 2017-10-13 | 2020-05-05 | Massachusetts Institute Of Technology | Diazene directed modular synthesis of compounds with quaternary carbon centers |
| EP3703700A4 (en) * | 2017-11-01 | 2021-08-04 | Arrowhead Pharmaceuticals, Inc. | INTEGRIN LIGANDS AND USES OF THESE LATEST |
| JP2021525735A (ja) | 2018-05-30 | 2021-09-27 | デビオファーム インターナショナル, エス. アー. | 抗cd37免疫コンジュゲート投薬レジメン |
| US11535634B2 (en) | 2019-06-05 | 2022-12-27 | Massachusetts Institute Of Technology | Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof |
| US12030888B2 (en) | 2021-02-24 | 2024-07-09 | Massachusetts Institute Of Technology | Himastatin derivatives, and processes of preparation thereof, and uses thereof |
| IL307421A (en) | 2021-04-08 | 2023-12-01 | Arrowhead Pharmaceuticals Inc | Rnai agents for inhibiting expression of receptor for advanced glycation end-products, compositions thereof, and methods of use |
| CN119780422B (zh) * | 2024-11-19 | 2025-11-07 | 深圳市锦瑞生物科技股份有限公司 | 碱性磷酸酶抗体标记物及其制备方法、检测试剂和试剂盒 |
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Also Published As
| Publication number | Publication date |
|---|---|
| EP2486023A4 (en) | 2014-05-07 |
| IL219020A0 (en) | 2012-06-28 |
| WO2010126551A1 (en) | 2010-11-04 |
| IN2012DN02780A (cg-RX-API-DMAC7.html) | 2015-09-18 |
| KR20120080611A (ko) | 2012-07-17 |
| EP2486023A1 (en) | 2012-08-15 |
| JP2013506709A (ja) | 2013-02-28 |
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