ZA946920B - Improved prodrugs for enzyme mediated activation - Google Patents

Improved prodrugs for enzyme mediated activation

Info

Publication number
ZA946920B
ZA946920B ZA946920A ZA946920A ZA946920B ZA 946920 B ZA946920 B ZA 946920B ZA 946920 A ZA946920 A ZA 946920A ZA 946920 A ZA946920 A ZA 946920A ZA 946920 B ZA946920 B ZA 946920B
Authority
ZA
South Africa
Prior art keywords
mediated activation
enzyme mediated
improved prodrugs
prodrugs
improved
Prior art date
Application number
ZA946920A
Other languages
English (en)
Inventor
Klaus Bosslet
Joerg Czech
Dieter Hoffmann
Andra Vasella
Roland Hoos
Francois Tillequin
Jean-Claude Florent
Michel Azoulay
Claude Monneret
Jean-Claude Jacquesy
Jean-Pierre Gesson
Michel Koch
Original Assignee
Behringwerke Ag
Hoechst Sa Lab
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 Behringwerke Ag, Hoechst Sa Lab filed Critical Behringwerke Ag
Publication of ZA946920B publication Critical patent/ZA946920B/xx

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/549Sugars, nucleosides, nucleotides or nucleic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6891Pre-targeting systems involving an antibody for targeting specific cells
    • A61K47/6899Antibody-Directed Enzyme Prodrug Therapy [ADEPT]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
ZA946920A 1993-09-09 1994-09-08 Improved prodrugs for enzyme mediated activation ZA946920B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP93114475A EP0647450A1 (fr) 1993-09-09 1993-09-09 Prodrogues améliorées pour activation médiée par enzyme

Publications (1)

Publication Number Publication Date
ZA946920B true ZA946920B (en) 1995-04-12

Family

ID=8213248

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA946920A ZA946920B (en) 1993-09-09 1994-09-08 Improved prodrugs for enzyme mediated activation

Country Status (13)

Country Link
US (1) US5621002A (fr)
EP (2) EP0647450A1 (fr)
JP (1) JP3773120B2 (fr)
KR (1) KR100385830B1 (fr)
AT (1) ATE208213T1 (fr)
AU (1) AU678494B2 (fr)
CA (1) CA2131662C (fr)
DE (1) DE69428957T2 (fr)
DK (1) DK0642799T3 (fr)
ES (1) ES2167343T3 (fr)
NO (1) NO313126B1 (fr)
PT (1) PT642799E (fr)
ZA (1) ZA946920B (fr)

Families Citing this family (143)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5525606A (en) 1994-08-01 1996-06-11 The United States Of America As Represented By The Department Of Health And Human Services Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
DE19512484A1 (de) 1995-04-04 1996-10-17 Bayer Ag Kohlenhydratmodifizierte Cytostatika
ES2257756T3 (es) * 1996-03-12 2006-08-01 Sanofi-Aventis Deutschland Gmbh Nuevos profarmacos para la terapia de tumores y enfermedades inflamatorias.
ATE365562T1 (de) * 1996-05-03 2007-07-15 Immunomedics Inc Zielgerichtete kombinations-immuntherapie für krebs
DE19631288A1 (de) * 1996-08-02 1998-02-05 Hoechst Ag Neue Inhibitoren der ß-Glucuronidase
JP2001501601A (ja) * 1996-09-12 2001-02-06 メルク エンド カンパニー インコーポレーテッド 前立腺ガンの治療において有用な共役体
DE19720312A1 (de) * 1997-05-15 1998-11-19 Hoechst Ag Zubereitung mit erhöhter in vivo Verträglichkeit
US6127333A (en) * 1997-07-10 2000-10-03 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
US6391305B1 (en) 1997-09-10 2002-05-21 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
ZA9810974B (en) * 1997-12-02 1999-06-03 Merck & Co Inc Conjugates useful in the treatment of prostate cancer
US20040081659A1 (en) * 1997-12-02 2004-04-29 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
NZ504615A (en) * 1997-12-02 2003-05-30 Merck & Co Inc Conjugates useful in the treatment of prostate cancer
CA2319836C (fr) 1998-02-06 2010-11-23 De Montfort University Promedicaments actives par hydroxylation
GB2334256A (en) 1998-02-12 1999-08-18 Univ Montfort Hydroxylation activated prodrugs
AU2531599A (en) * 1998-02-12 1999-08-30 De Montfort University Hydroxylation activated drug release
US6043367A (en) * 1998-09-30 2000-03-28 Roffler; Steve Proactive antitumor compounds
US6174858B1 (en) 1998-11-17 2001-01-16 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
AU772153B2 (en) * 1999-02-12 2004-04-08 Molecular Insight Pharmaceuticals, Inc. Matrices for drug delivery and methods for making and using the same
FR2791679B1 (fr) * 1999-03-31 2003-04-11 Fabre Pierre Dermo Cosmetique Bioprecurseurs aptes a liberer un derive retinoique par mise a profit de l'activite enzymatique de la surface cutanee et compositions pharmaceutiques et/ou cosmetiques
US6703020B1 (en) * 1999-04-28 2004-03-09 Board Of Regents, The University Of Texas System Antibody conjugate methods for selectively inhibiting VEGF
DE19925810A1 (de) * 1999-06-07 2000-12-14 Paz Arzneimittelentwicklung Anwendung von Verapamil und Verapamilderivaten zur Herstellung von Arzneimitteln mit Glucuronidase hemmender Wirkung
US6734192B1 (en) 1999-08-23 2004-05-11 Mp-1 Inc. Treatment of viral infections
GB2355007A (en) * 1999-10-08 2001-04-11 Michael Francis Holick Tamoxifen analogue glycosides and use thereof
WO2002032400A1 (fr) * 2000-10-16 2002-04-25 Neopharm, Inc. Preparation liposomales a base de mitoxantrone
AU2003230750A1 (en) * 2002-03-29 2003-10-13 Threshold Pharmaceuticals, Inc. Compositions and methods for treating cancer
CA2490626A1 (fr) * 2002-06-20 2003-12-31 Nippon Suisan Kaisha, Ltd. Promedicament, utilisation de ce dernier en medecine et procede de production de ce promedicament
EP1537146B9 (fr) 2002-07-15 2011-07-06 Board Of Regents, The University Of Texas System Anticorps se fixant a des phospholipides anioniques et des aminophospholipides et leur utilisation dans le traitement d'infections virales
WO2004043396A2 (fr) * 2002-11-09 2004-05-27 Nobex Corporation Promedicaments contenant du carbamate modifie et methodes de synthese de ces derniers
CA2506080A1 (fr) 2002-11-14 2004-05-27 Syntarga B.V. Promedicaments concus en tant qu'espaceurs de liberation multiple a elimination automatique
DE10256982A1 (de) 2002-12-05 2004-06-24 Schering Ag Neue Effektor-Konjugate, Verfahren zu Ihrer Herstellung und Ihre Pharmazeutische Verwendung
EP1581218A1 (fr) * 2002-12-05 2005-10-05 Schering AG Analogues d'epothilone permettant l'administration specifique d'un site dans le traitement de maladies proliferatives
AU2005216251B2 (en) * 2004-02-23 2011-03-10 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
EA016186B1 (ru) * 2005-09-26 2012-03-30 Медарекс, Инк. Человеческие моноклональные антитела к cd70 и их применение
EP1881000A1 (fr) * 2006-07-17 2008-01-23 Institut National De La Sante Et De La Recherche Medicale (Inserm) Conjugés du 2-fluoro-2-deoxy-glucose en tant qu'agents antitumoraux
US8232254B2 (en) 2006-10-06 2012-07-31 Wisconsin Alumni Research Foundation Colchicine neoglycosides and methods for their synthesis and use
CA2672468A1 (fr) * 2006-12-14 2008-06-19 Medarex, Inc. Anticorps humains se liant a cd70 et utilisations de ceux-ci
WO2008153394A2 (fr) * 2007-06-14 2008-12-18 Academisch Medisch Centrum Nouveaux pro-médicaments anti-inflammatoires
FR2920877B1 (fr) * 2007-09-10 2010-01-22 Commissariat Energie Atomique Substrats fluorescents saccharidiques, leur procede de procede de preparation et leurs utisations.
NZ586053A (en) 2007-11-09 2012-09-28 Peregrine Pharmaceuticals Inc Anti-vegf antibody compositions and methods
CA2716390C (fr) 2008-02-25 2016-08-23 Eyegate Pharma S.A.S. Apport ameliore d'une substance therapeutique a des tissus oculaires par iontophorese
CA2793890C (fr) 2010-04-15 2017-08-15 Spirogen Developments Sarl Pyrrolobenzodiazepines et conjugues de celles-ci
FR2960153B1 (fr) 2010-05-20 2012-08-17 Centre Nat Rech Scient Nouveaux bras autoreactifs et prodrogues les comprenant
EP3812387A1 (fr) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology, Inc. Inhibiteurs de protéine kinase hétérocycliques
EP2750713B1 (fr) 2011-10-14 2015-09-16 Spirogen Sàrl Pyrrolobenzodiazépines et conjugués associés
CN104080811B (zh) 2011-11-04 2019-09-27 酵活有限公司 在Fc结构域中具有突变的稳定异源二聚的抗体设计
BR112014016870A2 (pt) 2012-01-09 2017-06-27 Huesken Dieter composições orgânicas para tratar doenças relacionadas com beta-catenina
WO2013177481A1 (fr) 2012-05-25 2013-11-28 Immunogen, Inc. Benzodiazépines et leurs conjugués
ES2680153T3 (es) 2012-10-12 2018-09-04 Adc Therapeutics Sa Conjugados de anticuerpos anti-PSMA-pirrolobenzodiazepinas
EP2906297B1 (fr) 2012-10-12 2017-12-06 ADC Therapeutics SA Conjugués anticorps - pyrrolobenzodiazépine
ES2703151T3 (es) 2012-10-12 2019-03-07 Adc Therapeutics Sa Conjugados de anticuerpos de pirrolobenzodiazepinas
EP2906253B9 (fr) 2012-10-12 2019-04-10 ADC Therapeutics SA Conjugués anticorps anti-psma - pyrrolobenzodiazépine
CN105102004B (zh) 2012-10-12 2019-01-25 Adc疗法责任有限公司 吡咯并苯并二氮杂卓-抗cd22抗体结合物
ME03486B (fr) 2012-10-12 2020-01-20 Medimmune Ltd Pyrrolobenzodiazépines et ses conjugués
PT2906296T (pt) 2012-10-12 2018-06-01 Medimmune Ltd Conjugados de pirrolobenzodiazepina-anticorpo
JP6243918B2 (ja) 2012-10-16 2017-12-06 トレロ ファーマシューティカルズ, インコーポレイテッド Pkm2調節因子およびそれらの使用方法
BR112015014669B1 (pt) 2012-12-21 2023-09-26 Medimmune Limited Compostos pirrolobenzodiazepinas, conjugados compreendendo os mesmos e uso destes para tratar uma doença proliferativa
CN105246894A (zh) 2012-12-21 2016-01-13 斯皮罗根有限公司 用于治疗增殖性和自身免疫疾病的非对称吡咯并苯并二氮杂卓二聚物
EP2958907B1 (fr) 2013-02-19 2018-02-28 Novartis AG Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des estrogènes
EP2968596B1 (fr) 2013-03-13 2019-03-06 Medimmune Limited Pyrrolobenzodiazépines et leurs conjugués
US20160031887A1 (en) 2013-03-13 2016-02-04 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
BR112015021965B1 (pt) 2013-03-13 2022-05-03 Medimmune Limited Conjugados e compostos de pirrolobenzodiazepinas, composição farmacêutica, uso dos mesmos para o tratamento de uma doença proliferativa e método de síntese dos ditos compostos
CA2905993C (fr) 2013-03-14 2022-12-06 Tolero Pharmaceuticals, Inc. Derives de 4-amino-pyrimidinyle-2-amino-phenyle substitues et compositions pharmaceutiques a base de ceux-ci en tant qu'inhibiteurs dejak2 et d'alk2
US9950078B2 (en) 2013-10-11 2018-04-24 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
EP3054983B1 (fr) 2013-10-11 2019-03-20 Medimmune Limited Conjugués anticorps-pyrrolobenzodiazépines
EP3054986B1 (fr) 2013-10-11 2019-03-20 Medimmune Limited Conjugués anticorps-pyrrolobenzodiazépine
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015092634A1 (fr) 2013-12-16 2015-06-25 Novartis Ag Composés et compositions de 1,2,3,4-tétrahydroisoquinoléine en tant qu'antagonistes et agents de dégradation sélectifs des récepteurs des œstrogènes
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
ES2699351T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de SHP2
CN105899493B (zh) 2014-01-17 2019-03-29 诺华股份有限公司 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物
EP3125943A4 (fr) 2014-04-04 2017-12-06 Merck Sharp & Dohme Corp. Lieurs à base de phosphates pour introduction intracellulaire de conjugués médicamenteux
GB201406767D0 (en) 2014-04-15 2014-05-28 Cancer Rec Tech Ltd Humanized anti-Tn-MUC1 antibodies anf their conjugates
EP3193940A1 (fr) 2014-09-10 2017-07-26 Medimmune Limited Pyrrolobenzodiazépines et leurs conjugués
GB201416112D0 (en) 2014-09-12 2014-10-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
BR112017011111A2 (pt) 2014-11-25 2017-12-26 Adc Therapeutics Sa conjugados de pirrolobenzodiazepina-anticorpo
PE20171307A1 (es) 2014-12-23 2017-09-05 Novartis Ag Compuestos de triazolopirimidina y usos de los mismos
US10189813B2 (en) 2015-03-25 2019-01-29 Novartis Ag Formylated N-heterocyclic derivatives as FGFR4 inhibitors
GB201506411D0 (en) 2015-04-15 2015-05-27 Bergenbio As Humanized anti-axl antibodies
GB201506402D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
GB201506389D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
JP6718889B2 (ja) 2015-06-19 2020-07-08 ノバルティス アーゲー Shp2の活性を阻害するための化合物および組成物
EP3310779B1 (fr) 2015-06-19 2019-05-08 Novartis AG Composés et compositions pour l'inhibition de l'activité de shp2
JP6878316B2 (ja) 2015-06-19 2021-05-26 ノバルティス アーゲー Shp2の活性を阻害するための化合物および組成物
WO2017062334A1 (fr) 2015-10-05 2017-04-13 Merck Sharp & Dohme Corp. Conjugués anticorps-peptides ayant une activité agoniste au niveau des récepteurs au glucagon et au peptide-1 similaire au glucagon
EP3359194A4 (fr) 2015-10-06 2019-04-24 Merck Sharp & Dohme Corp. Conjugué anticorps-médicament pour applications anti-inflammatoires
GB201601431D0 (en) 2016-01-26 2016-03-09 Medimmune Ltd Pyrrolobenzodiazepines
US10869929B2 (en) 2016-01-29 2020-12-22 Merck Sharp & Dohme Corp. Phosphonate linkers and their use to facilitate cellular retention of compounds
GB201602356D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201602359D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
WO2017149463A1 (fr) 2016-03-01 2017-09-08 Novartis Ag Composés indole cyano-substitués et leur utilisation en tant qu'inhibiteurs de lsd1
GB201607478D0 (en) 2016-04-29 2016-06-15 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
SI3452465T1 (sl) 2016-05-04 2021-04-30 Genoscience Pharma Substituirani derivati 2,4-diamino-kinolina za uporabo v zdravljenju proliferativnih bolezni
PL3468972T3 (pl) 2016-06-14 2020-11-16 Novartis Ag Związki i kompozycje do hamowania aktywności shp2
JP2019524872A (ja) 2016-06-20 2019-09-05 ノバルティス アーゲー 癌の治療に有用なイミダゾピリミジン化合物
JP2019522049A (ja) 2016-06-20 2019-08-08 ノバルティス アーゲー トリアゾロピリジン化合物及びその使用
EP3472168B1 (fr) 2016-06-20 2024-01-10 Novartis AG Formes cristallines d'un composé de triazolopyrimidine
WO2018005963A1 (fr) * 2016-07-01 2018-01-04 Zoneone Pharma, Inc. Synthèse de nouveaux pro-médicaments de méthylumbelliférone et leur inclusion dans des formules d'administration de médicaments à base de lipides.
GB201617466D0 (en) 2016-10-14 2016-11-30 Medimmune Ltd Pyrrolobenzodiazepine conjugates
GB201702031D0 (en) 2017-02-08 2017-03-22 Medlmmune Ltd Pyrrolobenzodiazepine-antibody conjugates
UA125198C2 (uk) 2017-02-08 2022-01-26 Ейдісі Терапьютікс Са Кон'югати піролобензодіазепін-антитіло
WO2018146506A1 (fr) * 2017-02-10 2018-08-16 Universitat Politècnica De València Dérivés thérapeutiques
ES2926144T3 (es) 2017-04-18 2022-10-24 Medimmune Ltd Conjugados de pirrolobenzodiazepina
JP7408396B2 (ja) 2017-04-20 2024-01-05 アーデーセー セラピューティクス ソシエテ アノニム 併用療法
WO2018229222A1 (fr) 2017-06-14 2018-12-20 Adc Therapeutics Sa Régimes posologiques pour l'administration d'un cam anti-cd19
UY37774A (es) 2017-06-19 2019-01-31 Novartis Ag Compuestos 5-cianoindol sustituidos y usos de los mismos
HRP20220311T1 (hr) 2017-08-18 2022-05-13 Medimmune Limited Konjugati pirolobenzodiazepina
TW201912639A (zh) 2017-09-11 2019-04-01 美商克魯松藥物公司 Shp2之八氫環戊烷并[c]吡咯別構抑制劑
CN108021787B (zh) * 2017-12-08 2021-10-15 华东理工大学 一种根据基元反应拓扑结构构建动态代谢网络的方法
GB201803342D0 (en) 2018-03-01 2018-04-18 Medimmune Ltd Methods
GB201806022D0 (en) 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
KR20240033296A (ko) 2018-07-25 2024-03-12 어드밴스드 엑셀러레이터 어플리케이션즈 안정한 농축 방사성 핵종 복합체 용액
WO2020021465A1 (fr) 2018-07-25 2020-01-30 Advanced Accelerator Applications (Italy) S.R.L. Procédé de traitement de tumeurs neuroendocrines
CN112512597A (zh) 2018-07-26 2021-03-16 大日本住友制药肿瘤公司 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂
US20200115389A1 (en) 2018-09-18 2020-04-16 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
WO2020068867A1 (fr) 2018-09-25 2020-04-02 Black Diamond Therapeutics, Inc. Dérivés de quinazoline utilisés en tant qu'inhibiteur de tyrosine kinase, compositions, leurs procédés de préparation et leur utilisation
JP2022502496A (ja) 2018-09-25 2022-01-11 ブラック ダイアモンド セラピューティクス,インコーポレイティド チロシンキナーゼ阻害剤組成物、作製方法、および使用方法
CN112867512A (zh) 2018-09-25 2021-05-28 意大利国际先进加速器应用有限公司 联合疗法
JP2022502385A (ja) 2018-09-29 2022-01-11 ノバルティス アーゲー Shp2の活性を阻害するための化合物の製造方法
KR20210146290A (ko) 2019-02-12 2021-12-03 스미토모 다이니폰 파마 온콜로지, 인크. 헤테로시클릭 단백질 키나제 억제제를 포함하는 제제
US11712433B2 (en) 2019-03-22 2023-08-01 Sumitomo Pharma Oncology, Inc. Compositions comprising PKM2 modulators and methods of treatment using the same
AU2020263959A1 (en) 2019-04-24 2021-11-25 Heidelberg Pharma Research Gmbh Amatoxin antibody-drug conjugates and uses thereof
GB201908128D0 (en) 2019-06-07 2019-07-24 Adc Therapeutics Sa Pyrrolobenzodiazepine-antibody conjugates
CN114302878A (zh) 2019-07-03 2022-04-08 大日本住友制药肿瘤公司 酪氨酸激酶非受体1(tnk1)抑制剂及其用途
BR112022002518A2 (pt) 2019-08-15 2022-07-19 Black Diamond Therapeutics Inc Compostos de alquinila quinazolina
WO2021195206A1 (fr) 2020-03-24 2021-09-30 Black Diamond Therapeutics, Inc. Formes polymorphes et utilisations associées
AR123185A1 (es) 2020-08-10 2022-11-09 Novartis Ag Compuestos y composiciones para inhibir ezh2
WO2022043256A1 (fr) 2020-08-23 2022-03-03 Cobiores Nv Combinaisons synergiques de médicaments anticancéreux liés à une fraction tétrapeptidique et d'agents immunothérapeutiques
WO2022043557A1 (fr) 2020-08-31 2022-03-03 Advanced Accelerator Applications International Sa Méthode de traitement de cancers exprimant le psma
EP4204020A1 (fr) 2020-08-31 2023-07-05 Advanced Accelerator Applications International S.A. Méthode de traitement de cancers exprimant le psma
WO2022043556A1 (fr) 2020-08-31 2022-03-03 Novartis Ag Composition pharmaceutique stable
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Alk﹘5抑制劑和彼之用途
JP2023554520A (ja) 2020-12-22 2023-12-27 コビオレス エヌヴイ テトラペプチド部分を含む化合物
AU2021409561A1 (en) 2020-12-22 2023-07-06 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
EP4277901A1 (fr) 2021-01-13 2023-11-22 Monte Rosa Therapeutics, Inc. Composés d'isoindolinone
WO2022170052A1 (fr) 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Dérivés de quinazoline, dérivés de pyridopyrimidine, dérivés de pyrimidopyrimidine et leurs utilisations
WO2022167664A1 (fr) 2021-02-07 2022-08-11 Cobiores Nv Composés comprenant une fraction tétrapeptidique
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
EP4323349A1 (fr) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Composés amide d'isoindolinone utilisés pour traiter des maladies associées à gspt1
EP4323350A1 (fr) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Composés d'iso-indolinone
TW202317589A (zh) 2021-07-14 2023-05-01 美商尼坎醫療公司 作為kras抑制劑的伸烷基衍生物
US20230303509A1 (en) 2022-03-28 2023-09-28 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
US20230355792A1 (en) 2022-04-07 2023-11-09 Heidelberg Pharma Research Gmbh Methods of improving the therapeutic index
WO2023240024A1 (fr) 2022-06-08 2023-12-14 Nikang Therapeutics, Inc. Dérivés de sulfamide utilisés en tant qu'inhibiteurs de kinase 2 dépendant de la cycline

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2212014A1 (de) * 1971-04-21 1972-10-26 Deutsche Akademie der Wissenschaf ten zu Berlin, χ 1199 Berlin Verfahren zur fermentativen Spaltung von Transportformen von Chemotherapeutika, insbesondere Cancerostatica
WO1981001145A1 (fr) * 1979-10-18 1981-04-30 Univ Illinois Medicaments "pro-drugs" pouvant etre actives par des enzymes hydrolytiques
NZ225599A (en) * 1987-08-04 1991-09-25 Bristol Myers Co Antibody-enzyme conjugates and combinations with prodrugs for the treatment of tumour cells
WO1990003188A1 (fr) * 1988-09-30 1990-04-05 Neorx Corporation Elements de liaison clivables pour la reduction de la retention d'immunoconjugues par des organes non cibles
DE4106389A1 (de) * 1991-02-28 1992-09-03 Behringwerke Ag Fusionsproteine zur prodrug-aktivierung, ihre herstellung und verwendung
DE4002888A1 (de) * 1990-02-01 1991-08-08 Behringwerke Ag Anthracyclin-glycosyl-prodrugs, verfahren zu ihrer herstellung und ihre verwendung in kombination mit funktionalisierten tumorspezifischen enzymkonjugaten
FR2676058B1 (fr) * 1991-04-30 1994-02-25 Hoechst Lab Prodrogues glycosylees, leur procede de preparation et leur utilisation dans le traitement des cancers.

Also Published As

Publication number Publication date
AU678494B2 (en) 1997-05-29
JP3773120B2 (ja) 2006-05-10
DE69428957D1 (de) 2001-12-13
CA2131662A1 (fr) 1995-03-10
AU7169994A (en) 1995-03-23
JPH07149667A (ja) 1995-06-13
DK0642799T3 (da) 2002-02-25
KR100385830B1 (ko) 2003-08-19
NO943319D0 (no) 1994-09-08
CA2131662C (fr) 2008-09-02
KR950007874A (ko) 1995-04-15
NO943319L (no) 1995-03-10
DE69428957T2 (de) 2002-06-06
US5621002A (en) 1997-04-15
EP0642799B1 (fr) 2001-11-07
ES2167343T3 (es) 2002-05-16
EP0647450A1 (fr) 1995-04-12
NO313126B1 (no) 2002-08-19
ATE208213T1 (de) 2001-11-15
PT642799E (pt) 2002-04-29
EP0642799A1 (fr) 1995-03-15

Similar Documents

Publication Publication Date Title
ZA946920B (en) Improved prodrugs for enzyme mediated activation
NZ330187A (en) Apparatus for forming a roof tile having a cleaving apparatus
AU2631988A (en) D-cycloserine and its prodrugs as cognitive enhancers
GB9514438D0 (en) Stabilisation process and an enzyme for use in such a process
EG19860A (en) Enzymatic resolution of endo - bicyclo (2,2,1) heptan -2-ol and derived pharmaceutical agents
AU6267694A (en) High active enzyme granulates
MY114140A (en) Novel enzymes and prodrugs for use in antibody-directed enzyme prodrug therapy.
AU6451494A (en) Peptidic phosphinyloxymethyl ketones as interleukin-1beta- converting enzyme inhibitors
AU693827B2 (en) Enzymatic hydrolysis method for the conversion of C-7 sugar to C-7 hydroxyl taxanes
AU1093795A (en) Dual-sided push-pull amplifier
AU2569097A (en) Process for the production of plants with enhanced growth characteristics
AU1097988A (en) Alkylmelatonins
IE812615L (en) Deesterifying enzyme
CA2179234A1 (fr) Adhesif a base d'urethane et de gamma-butyrolactone, reticulable par l'humidite
AUPM334794A0 (en) Enzyme based bioremediation
AU7879487A (en) Proteine protease inhibitors from streptomyces
AU1117988A (en) Cytochrome p-450 enzymes
AU1112695A (en) An enzymatic process for making morphine-6-glucuronide or substituted morphine-6-glucuronide
AU5855998A (en) Optical long-distance signal transmission with optical amplification
AU5253798A (en) Ubch7-like ubiquitin-conjugating enzyme
AU3099795A (en) Enzyme from microbial source: phthalyl amidase
AU7509996A (en) Waterstop with injection channel
EP0957083A3 (fr) Procédé de stablisation de cyanhydrines
AU571559B2 (en) Alpha-allenic-alpha amino acids
AU2024397A (en) An enzyme