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 (159)

* 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
ATE540678T1 (de) * 2001-06-11 2012-01-15 Xenoport Inc Prodrugs aus gaba-analoga, zusammensetzungen und ihre verwendungen
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7186855B2 (en) 2001-06-11 2007-03-06 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
ES2432527T3 (es) * 2001-12-11 2013-12-04 University Of Virginia Patent Foundation Uso de pramipexol para tratar la esclerosis lateral amiotrófica
AU2003299509A1 (en) * 2002-06-21 2004-05-13 University Of Utah Research Foundation Crosslinked compounds and methods of making and using thereof
JP5149620B2 (ja) * 2004-07-23 2013-02-20 エンドサイト，インコーポレイテッド ２価リンカーおよびその結合体
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
WO2007022182A1 (en) * 2005-08-15 2007-02-22 University Of Virginia Patent Foundation Neurorestoration with r(+) pramipexole
CA2620933A1 (en) * 2005-09-02 2007-03-08 Pfizer Inc. Hydroxy substituted 1h-imidazopyridines and methods
ATE465205T1 (de) * 2005-12-05 2010-05-15 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
ES2379117T3 (es) 2006-05-16 2012-04-20 Knopp Neurosciences, Inc. Composiciones de R(+) y S(-) pramipexol y métodos de utilización de las mismas
EP2051735B1 (de) * 2006-07-17 2012-08-29 Ramot, at Tel Aviv University Ltd. Konjugate mit einem psychotropische heilmittel oder einem gaba agonist und eine organische säure und ihre behandlung von schmerzen und andere erkrankungen des zns
PT2089417E (pt) * 2006-10-12 2015-04-14 Bhi Ltd Partnership Métodos, compostos, composições e veículos para administrar o ácido 3-amino-1-propanossulfónico
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
CN104127878A (zh) 2007-03-14 2014-11-05 恩多塞特公司 结合配体连接的微管溶素递药缀合物
CA2681110A1 (en) 2007-03-14 2008-09-18 Knopp Neurosciences, Inc. Synthesis of chirally purified substituted benzothiazole diamines
JP2010526159A (ja) * 2007-04-10 2010-07-29 日東電工株式会社 多機能性ポリグルタミン酸塩薬物担体
CN101730549B (zh) * 2007-05-09 2015-12-09 日东电工株式会社 与铂类药物结合的聚合物
PT2155255E (pt) 2007-05-09 2013-10-15 Nitto Denko Corp Composições que incluem um composto hidrofóbico e um conjugado de poliaminoácido
US20080279778A1 (en) * 2007-05-09 2008-11-13 Nitto Denko Corporation Polyglutamate conjugates and polyglutamate-amino acid conjugates having a plurality of drugs
AU2008255565B2 (en) * 2007-05-31 2013-10-24 Paradigm Biopharmaceuticals Ltd Sulphated xylans for treatment or prophylaxis of respiratory diseases
BRPI0812970A2 (pt) 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
TW200922624A (en) * 2007-07-11 2009-06-01 Enzon Pharmaceuticals Inc Polymeric drug delivery system containing a multi-substituted aromatic moiety
US20100288665A1 (en) * 2007-07-23 2010-11-18 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
WO2009111271A1 (en) * 2008-03-06 2009-09-11 Nitto Denko Corporation Polymer paclitaxel conjugates and methods for treating cancer
KR101717145B1 (ko) 2008-05-20 2017-03-16 노이로제스엑스, 인코포레이티드 간보호제 아세트아미노펜 공통 프로드러그
KR20110071064A (ko) * 2008-08-19 2011-06-28 크놉 뉴로사이언시스 인코포레이티드 (ｒ)-프라미펙솔을 사용하는 조성물 및 방법
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
JP5845172B2 (ja) * 2009-05-01 2016-01-20 アデア ファーマスーティカルズ，インコーポレイテッド 高および低用量薬物の組み合わせを含む口腔内崩壊錠組成物
EP2477977B1 (de) * 2009-09-18 2017-08-23 Georgetown University Behandlung von oxidativem stress und/oder bluthochdruck
WO2011037913A2 (en) * 2009-09-24 2011-03-31 Emory University Methods for preventing oxidative stress injury of a tissue by a folate-tempol conjugate
WO2011070579A1 (en) * 2009-12-09 2011-06-16 Biolinerx Ltd. Methods of improving cognitive functions
US8377929B2 (en) 2010-02-24 2013-02-19 Ramot At Tel-Aviv University Ltd. Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same
EP2383255A1 (de) 2010-04-28 2011-11-02 Lacer, S.A. Neue Verbindungen, deren Synthese und Verwendung bei der Schmerzbehandlung
RU2012151134A (ru) * 2010-05-10 2014-06-20 Дзе Реджентс Оф Дзе Юниверсити Оф Калифорния Логометрическая комбинаторная доставка лекарственных средств
US20130211108A1 (en) * 2010-06-18 2013-08-15 Mylan 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
US9850296B2 (en) 2010-08-10 2017-12-26 Ecole Polytechnique Federale De Lausanne (Epfl) Erythrocyte-binding therapeutics
WO2012021512A2 (en) 2010-08-10 2012-02-16 Ecole Polytechnique Federale De Lausanne Erythrocyte-binding therapeutics
US9517257B2 (en) 2010-08-10 2016-12-13 Ecole Polytechnique Federale De Lausanne (Epfl) Erythrocyte-binding therapeutics
WO2012038963A1 (en) 2010-09-22 2012-03-29 Ramot At Tel-Aviv University Ltd. An acid addition salt of a nortriptyline-gaba conjugate and a process of preparing same
JP6013364B2 (ja) * 2010-12-23 2016-10-25 アルカーメス ファーマ アイルランド リミテッド マルチプルａｐｉローディングプロドラッグ
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
AU2012230880B2 (en) 2011-03-24 2017-04-13 Opko Pharmaceuticals, Llc Biomarker discovery in complex biological fluid using bead or particle based libraries and diagnostic kits and therapeutics
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
BR112014012444B1 (pt) 2011-11-23 2021-12-14 Therapeuticsmd, Inc Composição farmacêutica compreendendo estradiol solubilizado, progesterona e um agente de solubilização, bem como usos desta para tratar um sintoma relacionado à menopausa em uma mulher
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
WO2013096816A1 (en) 2011-12-22 2013-06-27 Biogen Idec Ma Inc. Improved synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds
US10080805B2 (en) 2012-02-24 2018-09-25 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
CN104411807B (zh) 2012-04-03 2018-10-02 桑加特公司 琥珀酰亚胺活化型硝酰化合物及其用于蛋白质硝酰化的使用方法
BR112014027204A2 (pt) 2012-05-01 2017-06-27 Catabasis Pharmaceuticals Inc conjugados d ácido graxo de estatina e agonistas fxr; composições e método de usos
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
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
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
US9494608B2 (en) 2012-08-21 2016-11-15 Janssen Pharmaceutica Nv Antibodies to olanzapine and use thereof
ES2904838T3 (es) 2012-08-21 2022-04-06 Janssen Pharmaceutica Nv Haptenos de risperidona y paliperidona
ES2788716T3 (es) 2012-08-21 2020-10-22 Janssen Pharmaceutica Nv Anticuerpos para haptenos de quetiapina y uso de los mismos
ES2652641T3 (es) 2012-08-21 2018-02-05 Janssen Pharmaceutica Nv Haptenos de aripiprazol y su uso en inmunoensayos
CA2882562C (en) 2012-08-21 2019-08-27 Eric Hryhorenko Antibodies to aripiprazole and use thereof
JP2015529199A (ja) 2012-08-21 2015-10-05 オルソ−クリニカル ダイアグノスティクス，インコーポレイティド パリペリドンハプテンに対する抗体及びその使用
CN104736565B (zh) 2012-08-21 2019-03-12 詹森药业有限公司 利培酮半抗原的抗体及其用途
EP3462173B1 (de) 2012-08-21 2021-03-31 Janssen Pharmaceutica NV Antikörper gegen risperidon und verwendung davon
ES2978909T3 (es) 2012-08-21 2024-09-23 Janssen Pharmaceutica Nv Anticuerpos contra haptenos de aripiprazol y uso de los mismos
ES2654413T3 (es) 2012-08-21 2018-02-13 Janssen Pharmaceutica, N.V. Anticuerpos a quetiapina y uso de los mismos
AU2013305930B2 (en) 2012-08-21 2017-08-24 Saladax Biomedical Inc. Haptens of paliperidone
TR201816378T4 (tr) * 2012-08-21 2018-11-21 Janssen Pharmaceutica Nv Olanzapin haptenleri.
CA2882490A1 (en) 2012-08-21 2014-02-27 Ortho-Clinical Diagnostics, Inc. Antibodies to paliperidone and use thereof
JP6389177B2 (ja) 2012-08-21 2018-09-12 ヤンセン ファーマシューティカ エヌ．ベー． オランザピンハプテンに対する抗体及びその使用
ES2822907T3 (es) 2012-08-21 2021-05-05 Janssen Pharmaceutica Nv Haptenos de quetiapina para su uso en inmunoensayos
CA2885740A1 (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
EP2908818A4 (de) 2012-10-16 2016-07-13 Endocyte Inc Wirkstofffreisetzungskonjugate mit unnatürlichen aminosäuren und verfahren zur verwendung
US9024069B2 (en) * 2012-11-09 2015-05-05 Ironwood Pharmaceuticals, Inc. NONOate derivatives and uses thereof
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US10471072B2 (en) 2012-12-21 2019-11-12 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
US10537581B2 (en) 2012-12-21 2020-01-21 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
US10023555B2 (en) * 2013-02-07 2018-07-17 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
EP3838271B1 (de) 2013-07-12 2025-09-03 Areteia Therapeutics, Inc. Behandlung eines erhöhten spiegels von eosinophilen und/oder basophilen
US9468630B2 (en) 2013-07-12 2016-10-18 Knopp Biosciences Llc Compositions and methods for treating conditions related to increased eosinophils
ES2813674T3 (es) 2013-08-13 2021-03-24 Knopp Biosciences Llc Composiciones y métodos para el tratamiento de trastornos de células plasmáticas y trastornos prolinfocíticos de células b
CA2921381A1 (en) 2013-08-13 2015-02-19 Knopp Biosciences Llc Compositions and methods for treating chronic urticaria
US11103473B2 (en) 2013-09-06 2021-08-31 Asdera Llc Treatment and prevention of autism and autism spectrum disorders
EP3049114B1 (de) 2013-09-27 2021-11-10 Massachusetts Institute of Technology Trägerfreie biologisch aktive proteinnanostrukturen
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
US10953101B2 (en) 2014-02-21 2021-03-23 École Polytechnique Fédérale De Lausanne (Epfl) Glycotargeting therapeutics
US10946079B2 (en) 2014-02-21 2021-03-16 Ecole Polytechnique Federale De Lausanne Glycotargeting therapeutics
KR102717969B1 (ko) 2014-02-21 2024-10-15 에꼴 뽈리떼끄닉 뻬데랄 드 로잔느 (으뻬에프엘) 글리코타겟팅 치료제
US10046056B2 (en) 2014-02-21 2018-08-14 École Polytechnique Fédérale De Lausanne (Epfl) Glycotargeting therapeutics
RU2016143081A (ru) 2014-05-22 2018-06-26 Терапьютиксмд, Инк. Натуральные комбинированные гормонозаместительные составы и терапии
EP3204048A4 (de) * 2014-10-07 2018-06-27 The Research Foundation for the State University of New York Funktionelle getrennte telodendrimere und nanoträger sowie verfahren zur herstellung und verwendung davon
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
CN108990413A (zh) 2015-08-12 2018-12-11 麻省理工学院 纳米颗粒的细胞表面偶联
EP3390455A1 (de) 2015-12-17 2018-10-24 Janssen Pharmaceutica NV Antikörper gegen quetiapin und verwendung davon
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
US9931349B2 (en) 2016-04-01 2018-04-03 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
JP7185530B2 (ja) 2016-06-13 2022-12-07 トルク セラピューティクス， インコーポレイテッド 免疫細胞機能を促進するための方法および組成物
US11103499B2 (en) 2016-08-26 2021-08-31 EXCIVA (UG) (haftungsbeschränkt) Compositions and methods thereof
KR20250114431A (ko) 2016-11-08 2025-07-29 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체
US11197872B2 (en) 2017-04-21 2021-12-14 Lunella Biotech, Inc. Vitamin C and doxycycline: a synthetic lethal combination therapy for eradicating cancer stem cells (CSCs)
CA3060509A1 (en) 2017-04-21 2018-10-25 Federica Sotgia Targeting hypoxic cancer stem cells (cscs) with doxycycline: implications for improving anti-angiogenic therapy
KR20250008984A (ko) 2017-05-18 2025-01-16 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
KR20200010343A (ko) 2017-05-19 2020-01-30 루넬라 바이오테크 인코포레이티드 안티미토신: 암 줄기 세포를 근절하기 위한 미토콘드리아 생물발생의 표적화 억제제
US12006553B2 (en) 2017-05-19 2024-06-11 Lunella Biotech, Inc. Companion diagnostics for mitochondrial inhibitors
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
RU2020102908A (ru) 2017-06-26 2021-07-27 Лунелла Байотек, Инк. Митокетосцины: митохондриальная терапия, нацеленная на кетоновый метаболизм в раковых клетках
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
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
KR20210031848A (ko) 2017-09-05 2021-03-23 토크 테라퓨틱스, 인코포레이티드 가역적 링커 및 이의 용도
JP7285828B2 (ja) 2017-09-05 2023-06-02 トルク セラピューティクス， インコーポレイテッド 治療用タンパク質組成物ならびにその作製および使用方法
CA3076821A1 (en) 2017-09-28 2019-04-04 Asdera Llc Use of cyclodextrins in diseases and disorders involving phospholipid dysregulation
MX2020004691A (es) 2017-11-07 2020-08-20 Regeneron Pharma Enlazadores hidrofilicos para conjugados anticuerpo-farmaco.
CN112004557B (zh) 2018-01-08 2024-07-30 里珍纳龙药品有限公司 类固醇类化合物及其抗体偶联物
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
WO2019213335A1 (en) * 2018-05-04 2019-11-07 Carnot2, Llc Orally bioavailable prodrugs of edaravone with altered pharmacokinetic properties and methods of use thereof
EA202092723A1 (ru) 2018-05-09 2021-04-09 Зе Юниверсити Оф Чикаго Композиции и способы, касающиеся иммунной толерантности
CN112533951A (zh) 2018-05-09 2021-03-19 里珍纳龙药品有限公司 抗msr1抗体及其使用方法
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
CN114080232A (zh) 2019-03-21 2022-02-22 科迪亚克生物科学公司 用于疫苗递送的细胞外囊泡
KR20210141554A (ko) 2019-03-21 2021-11-23 코디악 바이오사이언시즈, 인크. 세포외 소포 접합체 및 이의 용도
BR112021020668A2 (pt) 2019-04-17 2022-01-11 Codiak Biosciences Inc Composições de exossomos e aav
WO2020223530A1 (en) * 2019-04-30 2020-11-05 Cure Biopharma Inc. Gemcitabine prodrugs
US20220251200A1 (en) 2019-07-03 2022-08-11 Codiak Biosciences, Inc. Extracellular vesicles targeting t cells and uses thereof
MX2022000474A (es) * 2019-07-11 2022-03-11 Sun Pharma Advanced Res Co Ltd Derivados de camptotecina con un resto disulfuro y un resto piperazina.
EP4013876A1 (de) 2019-08-14 2022-06-22 Codiak BioSciences, Inc. Extrazelluläre vesikel mit nlrp3-antagonist
KR20220070433A (ko) 2019-08-14 2022-05-31 코디악 바이오사이언시즈, 인크. Stat6을 표적으로 하는 세포외 소포-aso 작제물
CA3145924A1 (en) 2019-08-14 2021-02-18 Yi Zhang Extracellular vesicle linked to molecules and uses thereof
AU2020330133A1 (en) 2019-08-14 2022-03-17 Lonza Sales Ag Extracellular vesicle-ASO constructs targeting CEBP/beta
CA3147366A1 (en) 2019-08-14 2021-02-18 Adam T. BOUTIN Extracellular vesicles with stat3-antisense oligonucleotides
CA3147701A1 (en) 2019-08-14 2021-02-18 Codiak Biosciences, Inc. Extracellular vesicles with antisense oligonucleotides targeting kras
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
WO2022066898A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Methods of producing extracellular vesicles
WO2022076596A1 (en) 2020-10-06 2022-04-14 Codiak Biosciences, Inc. Extracellular vesicle-aso constructs targeting stat6
JP2024506711A (ja) 2021-02-17 2024-02-14 ロンザ セールス アーゲー 最適化リンカー及びアンカー部分を介して生物学的に活性な分子に連結した細胞外ベシクル
CN114344474B (zh) * 2021-12-24 2023-07-04 四川省医学科学院·四川省人民医院 用于炎症相关肿瘤的纳米递送系统及其应用
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
WO2025259830A1 (en) * 2024-06-12 2025-12-18 Board Of Regents Of The University Of Nebraska Copolymeric compositions and methods of use thereof
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
US5807847A (en) 1996-06-04 1998-09-15 Queen's University At Kingston Nitrate esters
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
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
CA2319142A1 (en) 1998-06-08 1999-12-16 Advanced Medicine, Inc. Novel therapeutic agents for membrane transporters
WO1999063929A2 (en) * 1998-06-08 1999-12-16 Advanced Medicine, Inc. Multibinding inhibitors of microsomal triglyceride transferase protein
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.
CA2368793A1 (en) 1999-04-23 2000-11-02 Alza Corporation 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
CA2381425A1 (en) 1999-08-24 2001-03-01 Cellgate, Inc. Enhancing drug delivery across and into epithelial tissues using oligo arginine moieties
IT1319201B1 (it) 2000-10-12 2003-09-26 Nicox Sa Farmaci per il diabete.
IT1319202B1 (it) 2000-10-12 2003-09-26 Nicox Sa Farmaci per le malattie a base infiammatoria.
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
AU2003247161A1 (en) 2001-11-15 2004-05-25 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
ITMI20021399A1 (it) 2002-06-25 2003-12-29 Nicox Sa Inibitori della cicloossigenasi 2
ITMI20021391A1 (it) 2002-06-25 2003-12-29 Nicox Sa Nitroderivati di inibitori della cicloossigenasi-2
CA2491127A1 (en) 2002-07-03 2004-01-15 Nitromed, Inc. Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
WO2004012659A2 (en) 2002-08-01 2004-02-12 Nitromed, Inc. Nitrosated proton pump inhibitors, compositions and methods of use
DK1592457T3 (da) * 2003-01-27 2012-10-22 Endocyte Inc Folat-vinblastin-konjugat som lægemiddel
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
ATE424199T1 (de) 2003-06-19 2009-03-15 Nicox Sa Enalapril-nitroxy-derivate und verwandte verbindungen als ace-hemmer zur behandlung von kardiovaskulären erkrankungen
EP1673384A4 (de) 2003-09-26 2007-02-07 Nitromed Inc Nitrosierte glutaminsäureverbindungen, zusammensetzungen und anwendungsverfahren

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US8349901B2 (en) 2013-01-08
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US8357723B2 (en) 2013-01-22
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