ATE478685T1 - Prodrugs mit neuen biospaltbaren verbindern - Google Patents

Prodrugs mit neuen biospaltbaren verbindern

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Publication number
ATE478685T1
ATE478685T1 AT05781464T AT05781464T ATE478685T1 AT E478685 T1 ATE478685 T1 AT E478685T1 AT 05781464 T AT05781464 T AT 05781464T AT 05781464 T AT05781464 T AT 05781464T AT E478685 T1 ATE478685 T1 AT E478685T1
Authority
AT
Austria
Prior art keywords
prodrugs
compounds
biocleavable
new
formula
Prior art date
Application number
AT05781464T
Other languages
English (en)
Inventor
Apparao Nicholas Satyam
Original Assignee
Piramal Life Sciences Ltd
Satyam Apparao
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Piramal Life Sciences Ltd, Satyam Apparao filed Critical Piramal Life Sciences Ltd
Priority claimed from PCT/IB2005/052797 external-priority patent/WO2006027711A2/en
Application granted granted Critical
Publication of ATE478685T1 publication Critical patent/ATE478685T1/de

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/14—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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    • 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
    • A61K47/54—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 compound
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Families Citing this family (158)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6355666B1 (en) 2000-06-23 2002-03-12 Medinox, Inc. Protected forms of pharmacologically active agents and uses therefor
US7186855B2 (en) * 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
WO2002100347A2 (en) * 2001-06-11 2002-12-19 Xenoport, Inc. Prodrugs of gaba analogs, compositions and uses thereof
US7544681B2 (en) * 2001-09-27 2009-06-09 Ramot At Tel Aviv University Ltd. Conjugated psychotropic drugs and uses thereof
US20060281797A1 (en) * 2001-12-11 2006-12-14 University Of Virginia Patent Foundation Neurorestoration with R(+) Pramipexole
ES2351303T3 (es) * 2001-12-11 2011-02-02 University Of Virginia Patent Foundation Utilización de pramipexol para el tratamiento de la esclerosis lateral amiotrófica.
ES2449017T3 (es) * 2002-06-21 2014-03-17 The University Of Utah Research Foundation Compuestos reticulados, y métodos de preparación y uso de los mismos
US8288557B2 (en) 2004-07-23 2012-10-16 Endocyte, Inc. Bivalent linkers and conjugates thereof
JP5284779B2 (ja) * 2005-06-07 2013-09-11 ラモット・アット・テル・アビブ・ユニバーシテイ・リミテッド コンジュゲート化された向精神薬の新規な塩およびその調製方法
ES2334061T3 (es) * 2005-08-15 2010-03-04 University Of Virginia Patent Foundation Neurorrestauracion con pramipexol r(+).
WO2007028129A1 (en) * 2005-09-02 2007-03-08 Pfizer Inc. Hydroxy substituted 1h-imidazopyridines and methods
DE602006007177D1 (de) 2005-12-05 2009-07-16 Nitto Denko Corp Polyglutamat-aminosäure-konjugate und verfahren
US8518926B2 (en) * 2006-04-10 2013-08-27 Knopp Neurosciences, Inc. Compositions and methods of using (R)-pramipexole
PL2026803T3 (pl) 2006-05-16 2012-05-31 Knopp Neurosciences Inc Kompozycje R(+) i S(-) pramipeksolu i sposoby ich zastosowania
CN101511388B (zh) * 2006-07-17 2012-10-24 特拉维夫大学拉莫特有限公司 含有精神药物或gaba激动剂和有机酸的缀合物以及它们在治疗疼痛和其它cns疾病中的用途
CA2830727C (en) 2006-10-12 2016-11-29 Bhi Limited Partnership Methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid
US8524695B2 (en) * 2006-12-14 2013-09-03 Knopp Neurosciences, Inc. Modified release formulations of (6R)-4,5,6,7-tetrahydro-N6-propyl-2,6-benzothiazole-diamine and methods of using the same
WO2008079818A2 (en) * 2006-12-21 2008-07-03 Soluprin Pharmaceuticals, Inc. Intravenous administration of water soluble analgesic formulations
US20080181852A1 (en) * 2007-01-29 2008-07-31 Nitto Denko Corporation Multi-functional Drug Carriers
CN101678124A (zh) 2007-03-14 2010-03-24 恩多塞特公司 结合配体连接的微管溶素递药缀合物
EP2137171A4 (de) 2007-03-14 2010-05-19 Knopp Neurosciences Inc Synthese von chiralaufgereinigten substituierten benzothiazoldiaminen
CN101674852A (zh) * 2007-04-10 2010-03-17 日东电工株式会社 多功能聚谷氨酸盐药物载体
DK2155254T3 (da) * 2007-05-09 2013-03-04 Nitto Denko Corp Med platinlægemidler konjugerede polymere
EP2155255B1 (de) 2007-05-09 2013-08-14 Nitto Denko Corporation Zusammensetzungen, die eine hydrophobe Verbindung und ein Polyaminosäurekonjugat beinhalten
CN101707869A (zh) * 2007-05-09 2010-05-12 日东电工株式会社 具有多种药物的聚谷氨酸盐结合物和聚谷氨酸盐-氨基酸结合物
PT2164501E (pt) * 2007-05-31 2016-06-02 Paradigm Biopharmaceuticals Ltd Xilanos sulfatados para tratamento ou profilaxia de doenças respiratórias
CN101784565B (zh) 2007-06-25 2014-12-10 恩多塞特公司 含有亲水性间隔区接头的共轭物
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
EP2175878A4 (de) * 2007-07-11 2014-12-03 Belrose Pharma Inc Polymer-arzneiabgabesystem mit einem mehrfach substituierten aromatischen teil
CA2731801C (en) * 2007-07-23 2013-11-26 Kingsway Pharmaceuticals Inc. Therapeutic formulations for the treatment of cold and flu-like symptoms
WO2009101616A1 (en) 2008-02-11 2009-08-20 Ramot At Tel Aviv University Ltd. Novel conjugates for treating neurodegenerative diseases and disorders
CN104096236A (zh) * 2008-03-06 2014-10-15 日东电工株式会社 用于治疗癌症的聚合物紫杉醇结合物和方法
EP2285419A4 (de) 2008-05-20 2012-05-02 Neurogesx Inc Leberschützende mutuale paracetamol-prodrugs
US20110190356A1 (en) * 2008-08-19 2011-08-04 Knopp Neurosciences Inc. Compositions and Methods of Using (R)- Pramipexole
US20100068786A1 (en) * 2008-09-16 2010-03-18 Chmielewski Jean A Methods and compositions for reversing p-glycoprotein medicated drug resistance
EP2398761A4 (de) * 2009-02-18 2015-11-04 Bezwada Biomedical Llc Verzögerte freisetzung von stickoxid und wirkstoffen aus funktionalisierten makromeren und oligomeren
AR076540A1 (es) * 2009-05-01 2011-06-22 Eurand Inc Composiciones de comprimidos de desintegracion oral que comprenden combinaciones de analgesicos no- opioides y opioides, forma de dosificacion. metodo de preparacion. metodo para tratar dolor
CA2774239C (en) * 2009-09-18 2017-06-20 Georgetown University Treatment for oxidative stress and/or hypertension
US8815860B2 (en) * 2009-09-24 2014-08-26 Emory University Methods for preventing oxidative stress injury of a tissue by a Folate-TEMPOL conjugate
CA2782514A1 (en) * 2009-12-09 2011-06-16 Biolinerx Ltd. Methods of improving cognitive functions
EP2539857A4 (de) 2010-02-24 2013-07-24 Univ Ramot Kristalline formen des tri-mesylatsalzes von perphenazin-gaba und herstellungsverfahren dafür
EP2383255A1 (de) 2010-04-28 2011-11-02 Lacer, S.A. Neue Verbindungen, deren Synthese und Verwendung bei der Schmerzbehandlung
CA2800497C (en) * 2010-05-10 2019-03-12 The Regents Of The University Of California Methods for preparing ratiometric combinatorial nanoparticules
WO2011158259A1 (en) * 2010-06-18 2011-12-22 Matrix Laboratories Ltd Novel process for the preparation of (3s)-tetrahydrofuran-3-yl (is, 2r)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-(phosphonooxy) propylcarbamate and its pharmaceutically acceptable salts thereof
US9517257B2 (en) 2010-08-10 2016-12-13 Ecole Polytechnique Federale De Lausanne (Epfl) Erythrocyte-binding therapeutics
US9850296B2 (en) 2010-08-10 2017-12-26 Ecole Polytechnique Federale De Lausanne (Epfl) Erythrocyte-binding therapeutics
CA2807942C (en) 2010-08-10 2021-07-27 Ecole Polytechnique Federale De Lausanne Erythrocyte-binding therapeutics
US8916610B2 (en) 2010-09-22 2014-12-23 Ramot At Tel-Aviv University Ltd. Acid addition salt of a nortriptyline-GABA conjugate and a process of preparing same
CA2822447C (en) * 2010-12-23 2018-05-01 Alkermes Pharma Ireland Limited Multi-api loading prodrugs
WO2012112689A1 (en) * 2011-02-15 2012-08-23 The University Of North Carolina At Chapel Hill Nanoparticle, liposomes, polymers, agents and proteins modified with reversible linkers
MX2013011000A (es) 2011-03-24 2014-03-27 Opko Pharmaceuticals Llc Descubrimiento de biomarcador en fluido biologico complejo usando genotecas basadas en microesferao particula y kits de diagnostico y terapeuticos.
WO2012162175A1 (en) 2011-05-20 2012-11-29 Howard University Emetine derivatives, prodrugs containing same, and methods of treating conditions using same
WO2013010045A1 (en) 2011-07-12 2013-01-17 Biotime Inc. Novel methods and formulations for orthopedic cell therapy
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
ES2885523T3 (es) 2011-11-23 2021-12-14 Therapeuticsmd Inc Formulaciones y terapias de reposición hormonal de combinación naturales
US9512096B2 (en) 2011-12-22 2016-12-06 Knopp Biosciences, LLP Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds
WO2013126797A1 (en) 2012-02-24 2013-08-29 Purdue Research Foundation Cholecystokinin b receptor targeting for imaging and therapy
US8993614B2 (en) 2012-03-15 2015-03-31 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides
JP2015514718A (ja) 2012-04-03 2015-05-21 サンガート， インコーポレイテッド スクシンイミド活性化されたニトロキシル化合物およびタンパク質のニトロキシル化のためのその使用のための方法
AU2013256362A1 (en) * 2012-05-01 2014-11-13 Catabasis Pharmaceuticals, Inc. Fatty acid conjugates of statin and FXR agonists: compositions and methods of use
CN103450468B (zh) * 2012-05-30 2016-06-15 北京凯正生物工程发展有限责任公司 青蒿琥酯聚乙二醇化衍生物、其药物组合物及其用途
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
ES2822914T3 (es) 2012-08-21 2021-05-05 Janssen Pharmaceutica Nv Haptenos de aripiprazol y su uso en inmunoensayos
PT3663317T (pt) 2012-08-21 2023-01-23 Janssen Pharmaceutica Nv Anticorpos para haptenos de quetiapina e sua utilização
EP3556759B1 (de) 2012-08-21 2023-11-29 Janssen Pharmaceutica NV Haptene von paliperidon
WO2014031668A2 (en) 2012-08-21 2014-02-27 Ortho-Clinical Diagnostics, Inc Antibodies to quetiapine and use thereof
CN104755093B (zh) 2012-08-21 2018-11-16 詹森药业有限公司 奥氮平半抗原的抗体及其用途
CN104755928B (zh) 2012-08-21 2017-05-10 詹森药业有限公司 奥氮平的抗体及其用途
EP3492473B1 (de) * 2012-08-21 2025-07-30 Janssen Pharmaceutica NV Haptene von olanzapin
AU2013305965B2 (en) 2012-08-21 2017-08-24 Saladax Biomedical Inc. Antibodies to paliperidone and use thereof
CA2882489A1 (en) 2012-08-21 2014-02-27 Ortho-Clinical Diagnostics, Inc. Antibodies to paliperidone haptens and use thereof
TR201809424T4 (tr) 2012-08-21 2018-07-23 Janssen Pharmaceutica Nv Risperidon ve paliperidon haptenleri.
JP6374387B2 (ja) 2012-08-21 2018-08-15 ヤンセン ファーマシューティカ エヌ．ベー． リスペリドンハプテンへの抗体及びその使用
ES2978909T3 (es) 2012-08-21 2024-09-23 Janssen Pharmaceutica Nv Anticuerpos contra haptenos de aripiprazol y uso de los mismos
TR201816416T4 (tr) 2012-08-21 2018-11-21 Janssen Pharmaceutica Nv Risperidona yönelik antikorlar ve bunların kullanımı.
ES2762105T3 (es) 2012-08-21 2020-05-22 Janssen Pharmaceutica Nv Anticuerpos para aripiprazol y uso de los mismos
CA2882557C (en) 2012-08-21 2020-10-27 Ortho-Clinical Diagnostics, Inc. Haptens of quetiapine for use in immunoassays
WO2014047592A2 (en) * 2012-09-21 2014-03-27 Basil Rigas Compounds and compositions for use in the prevention and treatment of inflammation-related disorders, pain and fever, skin disorders, cancer and precancerous conditions thereof
AU2013331440A1 (en) 2012-10-16 2015-04-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
US9024069B2 (en) * 2012-11-09 2015-05-05 Ironwood Pharmaceuticals, Inc. NONOate derivatives and uses thereof
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
WO2014124208A1 (en) * 2013-02-07 2014-08-14 The Research Foundation Of The City University Of New York NSAIDs DERIVATIVES AND USES THEREOF
US9662313B2 (en) 2013-02-28 2017-05-30 Knopp Biosciences Llc Compositions and methods for treating amyotrophic lateral sclerosis in responders
CN103319388B (zh) * 2013-06-08 2014-11-05 西安交通大学 一种双功能聚乙二醇衍生物及其制备方法
HRP20251187T1 (hr) 2013-07-12 2025-11-21 Areteia Therapeutics, Inc. Liječenje povišenih razina eozinofila i/ili bazofila
US9468630B2 (en) 2013-07-12 2016-10-18 Knopp Biosciences Llc Compositions and methods for treating conditions related to increased eosinophils
US9763918B2 (en) 2013-08-13 2017-09-19 Knopp Biosciences Llc Compositions and methods for treating chronic urticaria
US9642840B2 (en) 2013-08-13 2017-05-09 Knopp Biosciences, Llc Compositions and methods for treating plasma cell disorders and B-cell prolymphocytic disorders
WO2015035258A1 (en) 2013-09-06 2015-03-12 The Rockefeller University Treatment and prevention of autism and autism spectrum disorders
ES2904276T3 (es) 2013-09-27 2022-04-04 Massachusetts Inst Technology Nanoestructuras de proteínas biológicamente activas sin vehículo
WO2015092819A2 (en) * 2013-12-21 2015-06-25 Nektar Therapeutics (India) Pvt. Ltd. Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5- amine
WO2015108835A1 (en) * 2014-01-14 2015-07-23 Sarmont Llc 3,3-disubstituted-1-hydroxytriaz-1-ene 2-oxides and wound-healing compositions using them
CA2946064C (en) * 2014-02-21 2023-09-26 Ecole Polytechnique Federale De Lausanne (Epfl) Glycotargeting therapeutics
US10946079B2 (en) 2014-02-21 2021-03-16 Ecole Polytechnique Federale De Lausanne Glycotargeting therapeutics
US10046056B2 (en) 2014-02-21 2018-08-14 École Polytechnique Fédérale De Lausanne (Epfl) Glycotargeting therapeutics
US10953101B2 (en) 2014-02-21 2021-03-23 École Polytechnique Fédérale De Lausanne (Epfl) Glycotargeting therapeutics
MX2016014281A (es) 2014-05-22 2017-02-22 Therapeuticsmd Inc Formulaciones y terapias de reemplazo de combinación de hormonas naturales.
WO2016057657A1 (en) * 2014-10-07 2016-04-14 The Research Foundation For The State University Of New York Functional segregated telodendrimers and nanocarriers and methods of making and using same
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
WO2017027843A1 (en) 2015-08-12 2017-02-16 Massachusetts Institute Of Technology Cell surface coupling of nanoparticles
AU2016370853A1 (en) 2015-12-17 2018-06-07 Saladax Biomedical Inc. Antibodies to quetiapine and use thereof
CN108431040B (zh) 2015-12-17 2022-07-26 詹森药业有限公司 利培酮的抗体及其用途
US10286077B2 (en) 2016-04-01 2019-05-14 Therapeuticsmd, Inc. Steroid hormone compositions in medium chain oils
AU2017239645A1 (en) 2016-04-01 2018-10-18 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
EP3468581A1 (de) 2016-06-13 2019-04-17 Torque Therapeutics, Inc. Verfahren und zusammensetzungen zur förderung der immunzellenfunktionen
US11103499B2 (en) 2016-08-26 2021-08-31 EXCIVA (UG) (haftungsbeschränkt) Compositions and methods thereof
KR20190074310A (ko) 2016-11-08 2019-06-27 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체
US11229657B2 (en) 2017-04-21 2022-01-25 Lunella Biotech, Inc. Targeting hypoxic cancer stem cells (CSCs) with doxycycline: implications for improving anti-angiogenic therapy
EP3612187B1 (de) 2017-04-21 2022-04-13 Lunella Biotech, Inc. Vitamin c und doxycyclin: eine synthetische letale kombinationstherapie zur eradikation von krebsstammzellen (cscs)
CA3063871A1 (en) 2017-05-18 2018-11-22 Regeneron Pharmaceuticals, Inc. Cyclodextrin protein drug conjugates
CA3063450A1 (en) 2017-05-19 2018-11-22 Lunella Biotech, Inc. Companion diagnostics for mitochondrial inhibitors
CU20190092A7 (es) 2017-05-19 2020-10-20 Lunella Biotech Inc Antimitoscinas: inhibidores específicos de la biogénesis mitocondrial para erradicar células madre cancerosas
US11253579B2 (en) 2017-06-16 2022-02-22 The University Of Chicago Compositions and methods for inducing immune tolerance
AU2018283383B2 (en) 2017-06-16 2023-03-16 The Regents Of The University Of California Conjugates of active pharmaceutical ingredients
MX2019014806A (es) 2017-06-26 2020-02-10 Lunella Biotech Inc Mitocetoscinas: agentes terapeuticos basados en mitocondrias que fijan como objetivo el metabolismo de cetonas en celulas cancerosas.
CN109207531B (zh) * 2017-07-03 2022-04-19 上海医药工业研究院 甲砜霉素与氟苯尼考关键中间体的生物制备方法
EP3678701A4 (de) 2017-09-05 2021-12-01 Torque Therapeutics, Inc. Therapeutische proteinzusammensetzungen und verfahren zur herstellung und verwendung davon
JP2020532565A (ja) 2017-09-05 2020-11-12 トルク セラピューティクス， インコーポレイテッド 可逆性リンカーおよびその使用
WO2019050850A1 (en) * 2017-09-05 2019-03-14 Primetime Life Sciences, Llc BIGUANIDINE DERIVATIVES OF THERAPEUTIC AGENTS, AND PREPARATION METHODS AND METHODS OF USING SAME
CA3076821A1 (en) 2017-09-28 2019-04-04 Asdera Llc Use of cyclodextrins in diseases and disorders involving phospholipid dysregulation
JP7426931B2 (ja) 2017-11-07 2024-02-02 レゲネロン ファーマシューティカルス，インコーポレーテッド 抗体薬物コンジュゲートのための親水性リンカー
BR112020013492A2 (pt) 2018-01-08 2020-12-08 Regeneron Pharmaceuticals, Inc. Esteroides e conjugados de anticorpo dos mesmos
WO2019213335A1 (en) * 2018-05-04 2019-11-07 Carnot2, Llc Orally bioavailable prodrugs of edaravone with altered pharmacokinetic properties and methods of use thereof
WO2019213333A1 (en) * 2018-05-04 2019-11-07 Carnot2, Llc Combination therapies with edaravone and prodrugs of edaravone that are orally bioavailable and have altered pharmacokinetic properties
AU2019265734B2 (en) 2018-05-09 2026-03-19 Anokion Sa Compositions and methods concerning immune tolerance
KR20210008008A (ko) 2018-05-09 2021-01-20 리제너론 파마슈티칼스 인코포레이티드 항-msr1 항체 및 이의 사용 방법
CN109459521B (zh) * 2018-12-25 2020-05-05 华东理工大学 一种四环素类抗生素痕量分析的固相萃取柱与应用
US20240108747A1 (en) 2019-03-21 2024-04-04 Lonza Sales Ag Extracellular vesicle conjugates and uses thereof
BR112021018694A2 (pt) 2019-03-21 2021-11-30 Codiak Biosciences Inc Vesículas extracelulares para distribuição de vacina
AU2020258483A1 (en) 2019-04-17 2021-11-11 Evox Therapeutics, Ltd. Compositions of exosomes and AAV
WO2020223530A1 (en) * 2019-04-30 2020-11-05 Cure Biopharma Inc. Gemcitabine prodrugs
WO2021003445A1 (en) 2019-07-03 2021-01-07 Codiak Biosciences, Inc. Extracellular vesicles targeting t cells and uses thereof
PE20221005A1 (es) * 2019-07-11 2022-06-15 Sun Pharma Advanced Res Co Ltd Derivados de la camptotecina
CA3147680A1 (en) 2019-08-14 2021-02-18 Dalia BURZYN Extracellular vesicle-aso constructs targeting stat6
EP4013872A1 (de) 2019-08-14 2022-06-22 Codiak BioSciences, Inc. Extrazelluläre vesikel mit auf kras abzielenden antisense-oligonukleotiden
CA3147369A1 (en) 2019-08-14 2021-02-18 Dalia BURZYN Extracellular vesicle-aso constructs targeting cebp/beta
WO2021030773A1 (en) 2019-08-14 2021-02-18 Codiak Biosciences, Inc. Extracellular vesicle-nlrp3 antagonist
US20220354963A1 (en) 2019-08-14 2022-11-10 Codiak Biosciences, Inc. Extracellular vesicle linked to molecules and uses thereof
CA3147366A1 (en) 2019-08-14 2021-02-18 Adam T. BOUTIN Extracellular vesicles with stat3-antisense oligonucleotides
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations
WO2021184021A1 (en) 2020-03-13 2021-09-16 Codiak Biosciences, Inc. Extracellular vesicle-aso constructs targeting pmp22
WO2022066883A1 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Extracellular vesicles comprising kras antigens and uses thereof
EP4216993A2 (de) 2020-09-23 2023-08-02 Codiak BioSciences, Inc. Verfahren zur herstellung von extrazellulären vesikeln
US20230364127A1 (en) 2020-10-06 2023-11-16 Codiak Biosciences, Inc. Extracellular vesicle-aso constructs targeting stat6
CN117377499A (zh) 2021-02-17 2024-01-09 隆萨销售股份有限公司 经由优化的接头和锚定部分与生物活性分子连接的细胞外囊泡
CN116999566A (zh) * 2021-12-24 2023-11-07 四川省医学科学院·四川省人民医院 纳米递送系统在制备抗结肠炎相关结直肠癌药物中的应用
CN116966187B (zh) * 2022-04-22 2025-11-21 深圳埃格林医药有限公司 地昔帕明前药的新用途
CN117731796B (zh) * 2023-12-14 2026-01-13 中国科学院基础医学与肿瘤研究所(筹) 一类白蛋白-紫杉醇孪药纳米粒的制备及应用
CN119375409B (zh) * 2024-12-30 2025-03-25 利安隆（天津）制药有限公司 一种替普瑞酮的检测方法

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2666787A (en) 1949-08-20 1954-01-19 Basf Ag Production of sulfonyl-isocyanates
ZA886812B (en) 1987-11-23 1989-07-26 Bristol Myers Co Anti-tumor prodrugs
IT1256450B (it) 1992-11-26 1995-12-05 Soldato Piero Del Esteri nitrici con attivita' farmacologica e procedimento per la loro preparazione
IT1276071B1 (it) 1995-10-31 1997-10-24 Nicox Ltd Compositi ad attivita' anti-infiammatoria
US7115661B1 (en) 1999-12-29 2006-10-03 Queen's University At Kingston Methods and compositions for mitigating pain
US6310052B1 (en) 1996-06-04 2001-10-30 Queen's University At Kingston Nitrate esters and their use for neurological conditions
US5807847A (en) * 1996-06-04 1998-09-15 Queen's University At Kingston Nitrate esters
IL120531A (en) * 1997-03-26 2006-12-31 Yissum Res Dev Co Nitric oxide donors and pharmaceutical compositions containing them
US5767134A (en) 1997-05-15 1998-06-16 Vion Pharmaceuticals, Inc. Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP
US6169078B1 (en) 1998-05-12 2001-01-02 University Of Florida Materials and methods for the intracellular delivery of substances
EP1085846A2 (de) 1998-06-08 2001-03-28 Advanced Medicine, Inc. Mehrfachbindende inhibitoren des microsomalen triglyceridtransferase-proteins
CA2319142A1 (en) 1998-06-08 1999-12-16 Advanced Medicine, Inc. Novel therapeutic agents for membrane transporters
IT1307928B1 (it) 1999-01-26 2001-11-29 Nicox Sa Metodo di sintesi di nitrossimetilfenil esteri di derivatidell'aspirina.
IT1311924B1 (it) 1999-04-13 2002-03-20 Nicox Sa Composti farmaceutici.
IL146047A0 (en) 1999-04-23 2002-07-25 Alza Corp Releasable linkage and compositions containing same
ITMI991517A1 (it) 1999-07-09 2001-01-09 Nicox Sa Procedimento per ottenere nitrossimetil fenil esterni di derivati dell'acido salicilico
IT1314184B1 (it) 1999-08-12 2002-12-06 Nicox Sa Composizioni farmaceutiche per la terapia di condizioni di stressossidativo
EP2269654A3 (de) 1999-08-24 2011-04-13 Cellgate Inc. Verbesserung des Verabreichung von Arzneimitteln durch und in epitheliale Gewebe rch Verwendung von Oligoarginin-Gruppen
IT1319202B1 (it) 2000-10-12 2003-09-26 Nicox Sa Farmaci per le malattie a base infiammatoria.
IT1319201B1 (it) 2000-10-12 2003-09-26 Nicox Sa Farmaci per il diabete.
ITMI20010985A1 (it) 2001-05-15 2002-11-15 Nicox Sa Farmaci per il morbo di alzheimer
ITMI20011307A1 (it) 2001-06-21 2002-12-21 Nicox Sa Farmaci per l'epilessia
ITMI20011308A1 (it) 2001-06-21 2002-12-21 Nicox Sa Farmaci per il dolore cronico
ITMI20011744A1 (it) 2001-08-09 2003-02-09 Nicox Sa Farmaci per le vasculopatie
AUPR879601A0 (en) 2001-11-09 2001-12-06 Biota Scientific Management Pty Ltd Novel chemical compounds and their use
WO2004039771A1 (en) 2001-11-15 2004-05-13 Department Of Science And Technology Diallyldisulphide compounds having antilipidemic and antioxidant activity
ITMI20020773A1 (it) 2002-04-11 2003-10-13 Nicox Sa Farmaci per il trattamento dell'artrite
ITMI20021391A1 (it) 2002-06-25 2003-12-29 Nicox Sa Nitroderivati di inibitori della cicloossigenasi-2
ITMI20021399A1 (it) 2002-06-25 2003-12-29 Nicox Sa Inibitori della cicloossigenasi 2
CA2491127A1 (en) 2002-07-03 2004-01-15 Nitromed, Inc. Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
JP4634144B2 (ja) 2002-08-01 2011-02-16 ニコックス エスエー ニトロソ化プロトンポンプ阻害剤、組成物および使用方法
EP2517730A3 (de) * 2003-01-27 2013-01-02 Endocyte, Inc. Vitaminrezeptorbindende Wirkstofffreisetzungskonjugate
US7166638B2 (en) 2003-05-27 2007-01-23 Nicox S.A. Statin derivatives
US7169805B2 (en) 2003-05-28 2007-01-30 Nicox S.A. Captopril derivatives
PL379197A1 (pl) 2003-06-19 2006-07-24 Nicox S.A. Nitroksylowe pochodne enalaprilu i pokrewne związki jako inhibitory ACE do leczenia chorób sercowo-naczyniowych
US20070037821A1 (en) 2003-09-26 2007-02-15 Nitromed, Inc. Nitrosated glutamic acid compounds, compositions and methods of use

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US20110269709A1 (en) 2011-11-03
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EP2266623A3 (de) 2011-10-12
US8349901B2 (en) 2013-01-08
US20060205674A2 (en) 2006-09-14
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EP2269657A3 (de) 2012-06-27
US8354455B2 (en) 2013-01-15
TW200616604A (en) 2006-06-01
US20110274695A1 (en) 2011-11-10
US20110269722A1 (en) 2011-11-03
US20060046967A1 (en) 2006-03-02
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