TW202346277A - Ikaros鋅指家族降解劑及其用途 - Google Patents
Ikaros鋅指家族降解劑及其用途 Download PDFInfo
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- TW202346277A TW202346277A TW112109625A TW112109625A TW202346277A TW 202346277 A TW202346277 A TW 202346277A TW 112109625 A TW112109625 A TW 112109625A TW 112109625 A TW112109625 A TW 112109625A TW 202346277 A TW202346277 A TW 202346277A
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- compound
- alkyl
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- aryl
- heterocyclyl
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| Publication number | Priority date | Publication date | Assignee | Title |
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Family Cites Families (369)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4965288A (en) | 1988-02-25 | 1990-10-23 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5182297A (en) | 1988-02-25 | 1993-01-26 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5021456A (en) | 1988-02-25 | 1991-06-04 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US4943593A (en) | 1988-02-25 | 1990-07-24 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5059714A (en) | 1988-02-25 | 1991-10-22 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5252608A (en) | 1988-02-25 | 1993-10-12 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5120764A (en) | 1988-11-01 | 1992-06-09 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US4997854A (en) | 1989-08-25 | 1991-03-05 | Trustees Of Boston University | Anti-fibrotic agents and methods for inhibiting the activity of lysyl oxidase in-situ using adjacently positioned diamine analogue substrates |
| US20030125519A1 (en) | 1990-08-27 | 2003-07-03 | Peter Besmer | Ligand for the c-kit receptor and methods of use thereof |
| US6319494B1 (en) | 1990-12-14 | 2001-11-20 | Cell Genesys, Inc. | Chimeric chains for receptor-associated signal transduction pathways |
| DE4205148A1 (de) | 1991-05-25 | 1993-01-21 | Boehringer Mannheim Gmbh | Monoklonale antikoerper gegen c-kit |
| IL104570A0 (en) | 1992-03-18 | 1993-05-13 | Yeda Res & Dev | Chimeric genes and cells transformed therewith |
| US5874540A (en) | 1994-10-05 | 1999-02-23 | Immunomedics, Inc. | CDR-grafted type III anti-CEA humanized mouse monoclonal antibodies |
| WO1997027873A1 (en) | 1996-01-30 | 1997-08-07 | Brigham & Women's Hospital, Inc. | Antibodies for modulating cd47-mediated neutrophil transmigration |
| CA2226962A1 (en) | 1998-02-16 | 1999-08-16 | Marie Sarfati | Use of binding agents to cd47 and its ligands in the treatment or the prophylaxis of various inflammatory, autoimmune and allergic diseases and in the treatment of graft rejection |
| WO2001040307A1 (de) | 1999-11-30 | 2001-06-07 | Eberhard-Karls-Universität Tübingen Universitätsklinikum | Antikörper gegen signal-regulator-proteine |
| WO2002092784A2 (en) | 2001-05-15 | 2002-11-21 | Emory University | POLYNUCLEOTIDES AND POLYPEPTIDES RELATING TO THE MODULATION OF SIRP α-CD47 |
| FR2828206B1 (fr) | 2001-08-03 | 2004-09-24 | Centre Nat Rech Scient | Utilisation d'inhibiteurs des lysyl oxydases pour la culture cellulaire et le genie tissulaire |
| US8877901B2 (en) | 2002-12-13 | 2014-11-04 | Immunomedics, Inc. | Camptothecin-binding moiety conjugates |
| US8435529B2 (en) | 2002-06-14 | 2013-05-07 | Immunomedics, Inc. | Combining radioimmunotherapy and antibody-drug conjugates for improved cancer therapy |
| CA2478047C (en) | 2002-03-01 | 2014-01-21 | Immunomedics, Inc. | Rs7 antibodies |
| ATE508747T1 (de) | 2003-03-10 | 2011-05-15 | Eisai R&D Man Co Ltd | C-kit kinase-hemmer |
| EP1663204B1 (en) | 2003-08-29 | 2014-05-07 | Exelixis, Inc. | C-kit modulators and methods of use |
| US7803553B2 (en) | 2003-09-04 | 2010-09-28 | Riken | Methods of use of antibodies which recognize a protease cleavage site of an LAP fragment of TGF-β |
| CA2545166A1 (en) | 2003-11-11 | 2005-05-19 | Chugai Seiyaku Kabushiki Kaisha | Humanized anti-cd47 antibody |
| US8435539B2 (en) | 2004-02-13 | 2013-05-07 | Immunomedics, Inc. | Delivery system for cytotoxic drugs by bispecific antibody pretargeting |
| WO2005113556A1 (en) | 2004-05-13 | 2005-12-01 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| ATE417065T1 (de) | 2004-05-19 | 2008-12-15 | Medigene Ltd | Hochaffiner ny-eso-t-zellen-rezeptor |
| JP2008503473A (ja) | 2004-06-17 | 2008-02-07 | プレキシコン,インコーポレーテッド | C−kit活性を調節する化合物 |
| WO2006031221A1 (en) | 2004-09-13 | 2006-03-23 | Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Compositions comprising t cell receptors and methods of use thereof |
| US7442716B2 (en) | 2004-12-17 | 2008-10-28 | Merck Frosst Canada Ltd. | 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors |
| JP5086809B2 (ja) | 2004-12-17 | 2012-11-28 | メルク カナダ インコーポレイテッド | mPGES−1阻害剤としての2−(フェニルまたはヘテロ環式)−1H−フェナントロ[9,10−d]イミダゾール |
| ES2665422T3 (es) | 2005-03-03 | 2018-04-25 | Immunomedics Inc. | Anticuerpos L243 humanizados |
| US9707302B2 (en) | 2013-07-23 | 2017-07-18 | Immunomedics, Inc. | Combining anti-HLA-DR or anti-Trop-2 antibodies with microtubule inhibitors, PARP inhibitors, bruton kinase inhibitors or phosphoinositide 3-kinase inhibitors significantly improves therapeutic outcome in cancer |
| US20090142345A1 (en) | 2005-03-15 | 2009-06-04 | Takeda Pharmaceutical Company Limited | Prophylactic/therapeutic agent for cancer |
| US20130039861A1 (en) | 2005-04-06 | 2013-02-14 | Immunomedics, Inc. | Dye Conjugated Peptides for Fluorescent Imaging |
| EP1888529A2 (en) | 2005-05-18 | 2008-02-20 | Wyeth | 3-cyanoquinoline inhibitors of tpl2 kinase and methods of making and using the same |
| MX2007014258A (es) | 2005-05-18 | 2008-01-22 | Wyeth Corp | Inhibidores de 4,6-diamino-[1,7]naftiridin-3-carbonitrilo de la tpl2 cinasa y metodos de fabricacion y uso de los mismos. |
| TW201402124A (zh) | 2005-08-19 | 2014-01-16 | Array Biopharma Inc | 作為類鐸受體(toll-like receptor)調節劑之8-經取代苯并氮雜呯 |
| TWI382019B (zh) | 2005-08-19 | 2013-01-11 | Array Biopharma Inc | 作為類鐸受體(toll-like receptor)調節劑之胺基二氮雜呯 |
| JP5276846B2 (ja) | 2005-09-13 | 2013-08-28 | 国立大学法人三重大学 | T細胞レセプターをコードする核酸が挿入されてなるベクター及び該レセプターを発現する細胞 |
| KR100788161B1 (ko) | 2006-01-06 | 2007-12-21 | (주)아모레퍼시픽 | 벤즈이미다졸 아민 유도체 또는 아미노퀴놀린 유도체를 함유하는 피부 미백용 조성물 |
| TW200740776A (en) | 2006-02-06 | 2007-11-01 | Osi Pharm Inc | N-phenylbenzotriazolyl c-kit inhibitors |
| US7420040B2 (en) | 2006-02-24 | 2008-09-02 | Arius Research Inc. | Cytotoxicity mediation of cells evidencing surface expression of TROP-2 |
| TWI395754B (zh) | 2006-04-24 | 2013-05-11 | Amgen Inc | 人類化之c-kit抗體 |
| US20090192158A1 (en) | 2006-05-02 | 2009-07-30 | Stacia Kargman | Methods for Treating or Preventing Neoplasias |
| JP2009537145A (ja) | 2006-05-15 | 2009-10-29 | バイラル ロジック システムズ テクノロジー コーポレーション | 免疫学的疾患および障害を治療するためのcd47と関連した組成物および方法 |
| NZ594457A (en) | 2006-05-22 | 2013-06-28 | Univ California | Compositions and methods for the delivery of oxygen |
| ITMI20061053A1 (it) | 2006-05-30 | 2007-11-30 | Manuli Rubber Ind Spa | Raccordo per tubi flessibili per applicazioni oleodinamiche,industriali e aria condizionata,avente caratteristiche di tenuta migliorate. |
| WO2008005877A2 (en) | 2006-06-30 | 2008-01-10 | Board Of Regents, The University Of Texas System | Inhibitors of c-kit and uses thereof |
| US8877780B2 (en) | 2006-08-30 | 2014-11-04 | Celgene Corporation | 5-substituted isoindoline compounds |
| DE102006058450A1 (de) | 2006-12-12 | 2008-06-19 | Eberhard-Karls-Universität Tübingen | Zubereitungen zur Hemmung der Prostaglandin E2 Synthese |
| CA2691444C (en) | 2007-06-29 | 2016-06-14 | Gilead Sciences, Inc. | Purine derivatives and their use as modulators of toll-like receptor 7 |
| ES2700141T3 (es) | 2007-08-02 | 2019-02-14 | Gilead Biologics Inc | Anticuerpos inhibidores LOXL2 y usos de los mismos |
| EP2573112A1 (en) | 2007-10-11 | 2013-03-27 | The Hospital For Sick Children | Modulation of sirpa - cd47 interaction for increasing human hematopoietic stem cell engraftment and compounds therefor |
| TW200930369A (en) | 2007-11-15 | 2009-07-16 | Astrazeneca Ab | Bis-(sulfonylamino) derivatives in therapy |
| TW200930368A (en) | 2007-11-15 | 2009-07-16 | Astrazeneca Ab | Bis-(sulfonylamino) derivatives in therapy |
| US20090163586A1 (en) | 2007-12-20 | 2009-06-25 | Astrazeneca Ab | Bis-(Sulfonylamino) Derivatives in Therapy 205 |
| WO2009103778A1 (en) | 2008-02-19 | 2009-08-27 | Novasaid Ab | Compounds and methods |
| WO2009117987A2 (de) | 2008-03-26 | 2009-10-01 | Universität Tübingen | Verwendung von boswelliasäuren und synthetischen boswelliasäurederivaten zur hemmung der mikrosomalen prostaglandin e2 synthase und des cathepsin g |
| WO2009130242A1 (en) | 2008-04-23 | 2009-10-29 | Novasaid Ab | Low molecular weight derivatives and use thereof in treatment of prostaglandin e synthase related diseases |
| EP2119705A1 (en) | 2008-05-14 | 2009-11-18 | AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A. | 3-Aminocarbozole compound, pharmaceutical composition containing it and preparation method therefor |
| DE102008027331A1 (de) | 2008-06-07 | 2009-12-10 | Friedrich-Alexander-Universität Erlangen-Nürnberg | Verwendung von Indol-3-carbonsäureestern zur Hemmung der mikrosomalen Prostaglandin E2 Synthase |
| DE102008015432A1 (de) | 2008-06-12 | 2009-12-17 | Eberhard-Karls-Universität Tübingen | Verwendung von Pirinixinsäure-Derivaten zur Hemmung der Prostaglandin E2 Synthese |
| WO2010014913A1 (en) | 2008-08-01 | 2010-02-04 | Ventirx Pharmaceuticals, Inc. | Toll-like receptor agonist formulations and their use |
| US8652843B2 (en) | 2008-08-12 | 2014-02-18 | Oncomed Pharmaceuticals, Inc. | DDR1-binding agents and methods of use thereof |
| UY32138A (es) | 2008-09-25 | 2010-04-30 | Boehringer Ingelheim Int | Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables |
| US8450321B2 (en) | 2008-12-08 | 2013-05-28 | Gilead Connecticut, Inc. | 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor |
| RS53347B (sr) | 2008-12-09 | 2014-10-31 | Gilead Sciences, Inc. | Modulatori toll-sličnih receptora |
| WO2010070047A1 (en) | 2008-12-19 | 2010-06-24 | Novartis Ag | Soluble polypeptides for use in treating autoimmune and inflammatory disorders |
| WO2010083253A2 (en) | 2009-01-14 | 2010-07-22 | Viral Logic Systems Technology Corp. | Cd47 related compositions and methods for treating immunological diseases and disorders |
| ES3000111T3 (en) | 2009-02-13 | 2025-02-27 | Immunomedics Inc | Intermediates for preparing conjugates with an intracellularly-cleavable linkage |
| UY32470A (es) | 2009-03-05 | 2010-10-29 | Boehringer Ingelheim Int | Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones |
| WO2010106431A2 (en) | 2009-03-20 | 2010-09-23 | Ludwig Institute For Cancer Research Ltd | High affinity t-cell receptor-like ny-eso-1 peptide antibodies, methods, and uses thereof |
| TWI598347B (zh) | 2009-07-13 | 2017-09-11 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| CN105669553A (zh) | 2009-08-18 | 2016-06-15 | 文蒂雷克斯药品公司 | 作为toll样受体调节剂的取代的苯并氮杂* |
| RU2016108987A (ru) | 2009-08-18 | 2018-11-26 | Вентиркс Фармасьютикалз, Инк. | Замещенные бензоазепины в качестве модуляторов toll-подобного рецептора |
| WO2011023812A1 (en) | 2009-08-27 | 2011-03-03 | Novasaid Ab | Microsomal prostaglandin e synthase-1 (mpges1) inhibitors |
| JP5694345B2 (ja) | 2009-10-22 | 2015-04-01 | ギリアード サイエンシーズ, インコーポレイテッド | Toll様受容体の調節因子 |
| WO2011048004A1 (en) | 2009-10-23 | 2011-04-28 | Boehringer Ingelheim International Gmbh | Inhibitors of the microsomal prostaglandin e2 synthase-1 |
| CN102869682B (zh) | 2009-11-18 | 2016-10-19 | 曼康公司 | 单克隆抗体及其诊断用途 |
| ES2978177T3 (es) | 2009-12-02 | 2024-09-06 | Immunomedics Inc | Combinación de radio inmunoterapia y conjugados anticuerpo-fármaco para mejorar la terapia contra el cáncer |
| BR112012017164A2 (pt) | 2009-12-22 | 2019-09-24 | Novartis Ag | proteína de fusão de região constante de anticorpo-cd47 tetravalente |
| BR112012019693A2 (pt) | 2010-02-04 | 2017-06-20 | Gilead Biologics Inc | anticorpos que se ligam à lisil oxidase-like 2 (loxl2) e métodos de uso para eles. |
| PT2569013T (pt) | 2010-05-14 | 2017-02-08 | Univ Leland Stanford Junior | Anticorpos monoclonais humanizados e quiméricos para cd47 |
| US9089520B2 (en) | 2010-05-21 | 2015-07-28 | Baylor College Of Medicine | Methods for inducing selective apoptosis |
| US8586604B2 (en) | 2010-08-20 | 2013-11-19 | Boehringer Ingelheim International Gmbh | Inhibitors of the microsomal prostaglandin E2 synthase-1 |
| US8759537B2 (en) | 2010-08-20 | 2014-06-24 | Boehringer Ingelheim International Gmbh | 3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents |
| EP2608809B1 (en) | 2010-08-27 | 2019-05-22 | Gilead Biologics, Inc. | Antibodies to matrix metalloproteinase 9 |
| CN103237549A (zh) | 2010-10-01 | 2013-08-07 | 帆德制药股份有限公司 | 过敏性疾病的治疗方法 |
| EP3195868A3 (en) | 2010-10-01 | 2017-08-02 | VentiRx Pharmaceuticals, Inc. | Therapeutic use of a tlr agonist and combination therapy |
| WO2012054825A1 (en) | 2010-10-22 | 2012-04-26 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Anti-mage-a3 t cell receptors and related materials and methods of use |
| PH12013501201A1 (en) | 2010-12-09 | 2013-07-29 | Univ Pennsylvania | Use of chimeric antigen receptor-modified t cells to treat cancer |
| UY33779A (es) | 2010-12-10 | 2012-07-31 | Boehringer Ingelheim Int | ?2-(fenilamino)-1H-bencimidazol-5-carboxamidas novedosas? |
| US8466186B2 (en) | 2010-12-10 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Compounds |
| WO2012082647A2 (en) | 2010-12-13 | 2012-06-21 | The Regents Of The University Of California | PYRAZOLE INHIBITORS OF COX-2 AND sEH |
| AR084174A1 (es) | 2010-12-21 | 2013-04-24 | Lilly Co Eli | Compuestos de imidazol-2-benzamida utiles para el tratamiento de osteoartritis y una composicion farmaceutica |
| EP3208263A1 (en) | 2011-01-12 | 2017-08-23 | VentiRx Pharmaceuticals, Inc. | Substituted benzoazepines as toll-like receptor modulators |
| DK2663555T3 (en) | 2011-01-12 | 2017-03-27 | Ventirx Pharmaceuticals Inc | SUBSTITUTED BENZOAZEPINS AS MODULATORS OF TOLL-LIKE RECEPTORS |
| WO2012110860A1 (en) | 2011-02-17 | 2012-08-23 | Glenmark Pharmaceuticals S.A. | TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS |
| PT3590928T (pt) | 2011-04-08 | 2021-08-19 | Janssen Sciences Ireland Unlimited Co | Derivados de pirimidina para o tratamento de infeções virais |
| AR086044A1 (es) | 2011-05-12 | 2013-11-13 | Imclone Llc | Anticuerpos que se unen especificamente a un dominio extracelular de c-kit y usos de los mismos |
| AU2012258220B2 (en) | 2011-05-18 | 2017-01-19 | Janssen Sciences Ireland Uc | Quinazoline derivatives for the treatment of viral infections and further diseases |
| AR086254A1 (es) | 2011-05-26 | 2013-11-27 | Lilly Co Eli | Derivados de imidazol utiles para el tratamiento de artritis |
| WO2012170250A1 (en) | 2011-06-07 | 2012-12-13 | Radiation Control Technologies, Inc. | Morpholino oligonucleotides capable of inhibiting cd47-mediated cellular damage and uses thereof |
| PH12014500326B1 (en) | 2011-08-18 | 2018-01-10 | Nippon Shinyaku Co Ltd | Heterocyclic derivative and pharmaceutical drug |
| US9550835B2 (en) | 2011-08-23 | 2017-01-24 | Chugai Seiyaku Kabushiki Kaisha | Anti-DDR1 antibody having anti-tumor activity |
| GB201115529D0 (en) | 2011-09-08 | 2011-10-26 | Imp Innovations Ltd | Antibodies, uses and methods |
| AU2012309830B2 (en) | 2011-09-15 | 2017-03-30 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | T cell receptors recognizing HLA-A1- or HLA-Cw7-restricted mage |
| WO2013041865A1 (en) | 2011-09-22 | 2013-03-28 | Immunocore Limited | T cell receptors |
| HK1201065A1 (en) | 2011-10-04 | 2015-08-21 | Gilead Calistoga Llc | Novel quinoxaline inhibitors of pi3k |
| WO2013056352A1 (en) | 2011-10-19 | 2013-04-25 | University Health Network | Antibodies and antibody fragments targeting sirp-alpha and their use in treating hematologic cancers |
| TWI495644B (zh) | 2011-11-11 | 2015-08-11 | Rinat Neuroscience Corp | 營養層細胞表面抗原(Trop-2)之專一性抗體類及彼等之用途 |
| WO2013072825A1 (en) | 2011-11-16 | 2013-05-23 | Glenmark Pharmaceuticals S.A. | Phtalazinone derivatives as mpegs -1 inhibitors |
| US9427464B2 (en) | 2011-11-22 | 2016-08-30 | Chiome Bioscience Inc. | Anti-human TROP-2 antibody having an antitumor activity in vivo |
| BR112014015197A8 (pt) | 2011-12-21 | 2017-06-13 | Novira Therapeutics Inc | agentes antivirais de hepatite b |
| ES2816647T3 (es) | 2012-01-17 | 2021-04-05 | Univ Leland Stanford Junior | Reactivos SIRP-alfa de alta afinidad |
| UY34573A (es) | 2012-01-27 | 2013-06-28 | Gilead Sciences Inc | Inhibidor de la quinasa que regula la señal de la apoptosis |
| WO2013116562A1 (en) | 2012-02-03 | 2013-08-08 | Gilead Calistoga Llc | Compositions and methods of treating a disease with (s)-4 amino-6-((1-(5-chloro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile |
| KR102100388B1 (ko) | 2012-02-06 | 2020-04-13 | 인히브릭스, 인크. | Cd47 항체 및 그 사용 방법 |
| SG11201404743TA (en) | 2012-02-08 | 2014-09-26 | Janssen R & D Ireland | Piperidino-pyrimidine derivatives for the treatment of viral infections |
| AR089939A1 (es) | 2012-02-09 | 2014-10-01 | Glenmark Pharmaceuticals Sa | COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1 |
| US9518112B2 (en) | 2012-03-08 | 2016-12-13 | Ludwig Institute For Cancer Research Ltd | TGF-β1 specific antibodies and methods and uses thereof |
| WO2013153535A1 (en) | 2012-04-13 | 2013-10-17 | Glenmark Pharmaceuticals S.A. | TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS |
| TWI568722B (zh) | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲mPGES-1抑制劑之三唑酮化合物 |
| MX369417B (es) | 2012-08-10 | 2019-11-07 | Janssen Sciences Ireland Uc | Derivados de alquilpirimidina para el tratamiento de infecciones víricas y otras enfermedades. |
| US9682143B2 (en) | 2012-08-14 | 2017-06-20 | Ibc Pharmaceuticals, Inc. | Combination therapy for inducing immune response to disease |
| EP2892534B8 (en) | 2012-09-06 | 2021-09-15 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2014047624A1 (en) | 2012-09-24 | 2014-03-27 | Gilead Sciences, Inc. | Anti-ddr1 antibodies |
| DK2906563T3 (en) | 2012-10-10 | 2018-06-06 | Janssen Sciences Ireland Uc | PYRROLO [3,2-D] PYRIMIDINE DERIVATIVES FOR TREATING VIRUS INFECTIONS AND OTHER DISEASES |
| US20150297573A1 (en) | 2012-10-24 | 2015-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | TPL2 KINASE INHIBITORS FOR PREVENTING OR TREATING DIABETES AND FOR PROMOTING Beta-CELL SURVIVAL |
| EA035431B1 (ru) | 2012-11-16 | 2020-06-15 | Янссен Сайенсиз Айрлэнд Юси | Гетероциклические замещенные производные 2-амино-хиназолина в качестве модуляторов tlr7 и/или tlr8 для лечения вирусных инфекций |
| DK3725807T3 (da) | 2012-12-03 | 2026-01-12 | Novimmune Sa | Anti-cd47 antistoffer og fremgangsmåder til anvendelse deraf |
| BR112015013431A2 (pt) | 2012-12-12 | 2017-11-14 | Vasculox Inc | anticorpos monoclonais ou respectivos fragmentos ligantes de antígenos, composição farmacêutica, e usos de anticorpo monoclonal ou respectivo fragmento ligante de antígenos |
| US10744129B2 (en) | 2012-12-13 | 2020-08-18 | Immunomedics, Inc. | Therapy of small-cell lung cancer (SCLC) with a topoisomerase-I inhibiting antibody-drug conjugate (ADC) targeting Trop-2 |
| US9492566B2 (en) | 2012-12-13 | 2016-11-15 | Immunomedics, Inc. | Antibody-drug conjugates and uses thereof |
| US10413539B2 (en) | 2012-12-13 | 2019-09-17 | Immunomedics, Inc. | Therapy for metastatic urothelial cancer with the antibody-drug conjugate, sacituzumab govitecan (IMMU-132) |
| AU2013364068B2 (en) | 2012-12-21 | 2016-10-20 | Gilead Calistoga Llc | Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors |
| MX365640B (es) | 2012-12-21 | 2019-06-10 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasas y sus indicaciones. |
| JP6207100B2 (ja) | 2012-12-21 | 2017-10-04 | ギリアード カリストガ エルエルシー | イソキノリノンまたはキナゾリノンホスファチジルイノシトール3−キナーゼ阻害剤 |
| ES2886531T3 (es) | 2013-01-07 | 2021-12-20 | Omniox Inc | Formas poliméricas de proteínas H-NOX |
| CA2899679C (en) | 2013-01-29 | 2023-03-21 | Max-Delbruck-Centrum Fur Molekulare Medizin (Mdc) Berlin-Buch | High avidity antigen recognizing constructs |
| SG11201506639XA (en) | 2013-02-21 | 2015-09-29 | Janssen Sciences Ireland Uc | 2-aminopyrimidine derivatives for the treatment of viral infections |
| US8993771B2 (en) | 2013-03-12 | 2015-03-31 | Novira Therapeutics, Inc. | Hepatitis B antiviral agents |
| WO2014163684A1 (en) | 2013-04-03 | 2014-10-09 | Ibc Pharmaceuticals, Inc. | Combination therapy for inducing immune response to disease |
| WO2014167444A1 (en) | 2013-04-08 | 2014-10-16 | Glenmark Pharmaceuticals S.A. | SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS |
| PL3008053T3 (pl) | 2013-06-14 | 2018-08-31 | Gilead Calistoga Llc | Inhibitory 3-kinazy fosfatydyloinozytolu |
| GB201313377D0 (en) | 2013-07-26 | 2013-09-11 | Adaptimmune Ltd | T cell receptors |
| ES2860952T3 (es) | 2013-08-01 | 2021-10-05 | Univ Catholique Louvain | Proteína anti-garp y usos de la misma |
| WO2015059618A1 (en) | 2013-10-22 | 2015-04-30 | Glenmark Pharmaceuticals S.A. | SUBSTITUTED PYRIMIDINE COMPOUNDS AS mPGES-1 INHIBITORS |
| US9290505B2 (en) | 2013-12-23 | 2016-03-22 | Gilead Sciences, Inc. | Substituted imidazo[1,2-a]pyrazines as Syk inhibitors |
| AU2014371934B2 (en) | 2013-12-25 | 2020-01-23 | Daiichi Sankyo Company, Limited | Anti-TROP2 antibody-drug conjugate |
| US9771369B2 (en) | 2014-03-04 | 2017-09-26 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN106456749B (zh) | 2014-03-11 | 2021-03-30 | 小利兰·斯坦福大学托管委员会 | 抗SIRPα抗体和双特异性巨噬细胞增强型抗体 |
| DK3129023T3 (da) | 2014-03-27 | 2021-05-25 | Eicosis Llc | Potente opløselige epoxidhydrolase-inhibitorer |
| US10611837B2 (en) | 2014-04-10 | 2020-04-07 | Seattle Children's Hospital | Transgene genetic tags and methods of use |
| US10081629B2 (en) | 2014-04-14 | 2018-09-25 | Jiangsu Hengrui Medicine Co., Ltd. | Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof |
| WO2016023040A1 (en) | 2014-08-08 | 2016-02-11 | Alexo Therapeutics International | Sirp-alpha variant constructs and uses thereof |
| WO2016022971A1 (en) | 2014-08-08 | 2016-02-11 | The Board Of Trustees Of The Leland Stanford Junior University | Sirp alpha-antibody fusion proteins |
| PL3180363T3 (pl) | 2014-08-15 | 2020-02-28 | Merck Patent Gmbh | Białka fuzyjne immunoglobulin sirp-alfa |
| TWI751102B (zh) | 2014-08-28 | 2022-01-01 | 美商奇諾治療有限公司 | 對cd19具專一性之抗體及嵌合抗原受體 |
| JO3474B1 (ar) | 2014-08-29 | 2020-07-05 | Amgen Inc | مشتقات تيتراهيدرونافثالين التي تثبط بروتين mcl-1 |
| CA2961950A1 (en) | 2014-09-28 | 2016-03-31 | The Regents Of The University Of California | Modulation of stimulatory and non-stimulatory myeloid cells |
| GB201417803D0 (en) | 2014-10-08 | 2014-11-19 | Adaptimmune Ltd | T cell receptors |
| JO3581B1 (ar) | 2014-10-29 | 2020-07-05 | Lilly Co Eli | مركبات ميثيل-بيبيريدين جديدة مفيدة لتثبيط إنزيم سينثاز -1 بروستاجلاندين e2 ميكروسومي |
| TW201627299A (zh) | 2014-10-29 | 2016-08-01 | 美國禮來大藥廠 | 用於抑制微粒體前列腺素e合成酶1之新穎羧酸化合物 |
| EP3221358B1 (en) | 2014-11-18 | 2021-07-21 | Janssen Pharmaceutica, N.V. | Cd47 antibodies, methods, and uses |
| EP3227340B1 (en) | 2014-12-04 | 2020-06-17 | Mediterranea Theranostic S.R.L. | Humanized anti-trop-2 monoclonal antibodies and uses thereof |
| CN107206088A (zh) | 2014-12-05 | 2017-09-26 | 豪夫迈·罗氏有限公司 | 使用pd‑1轴拮抗剂和hpk1拮抗剂用于治疗癌症的方法和组合物 |
| EP3234144B1 (en) | 2014-12-15 | 2020-08-26 | Bellicum Pharmaceuticals, Inc. | Methods for controlled elimination of therapeutic cells |
| MX391051B (es) | 2014-12-30 | 2025-03-21 | Celgene Corp | Anticuerpos anti-cd47 y usos de los mismos. |
| WO2016115345A1 (en) | 2015-01-14 | 2016-07-21 | The Brigham And Women's Hospital, | Treatment of cancer with anti-lap monoclonal antibodies |
| KR102625835B1 (ko) | 2015-03-04 | 2024-01-17 | 주식회사유한양행 | Cd47에 결합하는 항체 치료제 |
| CA2978171A1 (en) | 2015-03-10 | 2016-09-15 | J.H. Frederik Falkenburg | T-cell receptors directed against the preferentially expressed antigen of melanoma and uses thereof |
| CA2979974A1 (en) | 2015-03-17 | 2016-09-22 | Omniox, Inc. | Modulation of tumor immunity by protein-mediated o2 delivery |
| US10358472B2 (en) | 2015-05-06 | 2019-07-23 | The Board Of Trustees Of The Leland Stanford Junior University | High affinity CD47 analogs |
| CN106188275A (zh) | 2015-05-06 | 2016-12-07 | 广州市香雪制药股份有限公司 | 识别ny-eso-1抗原短肽的t细胞受体 |
| SG11201708804WA (en) | 2015-05-07 | 2017-11-29 | Agenus Inc | Anti-ox40 antibodies and methods of use thereof |
| TW201702272A (zh) | 2015-05-22 | 2017-01-16 | 美國紀念斯隆 凱特琳癌症中心 | Prame肽專一性類t細胞受體抗體 |
| SG11201708303XA (en) * | 2015-05-22 | 2017-11-29 | Biotheryx Inc | Compounds targeting proteins, compositions, methods, and uses thereof |
| CN104804093A (zh) | 2015-05-27 | 2015-07-29 | 江苏春申堂药业有限公司 | 一种针对cd47的单域抗体 |
| WO2016196388A1 (en) | 2015-05-29 | 2016-12-08 | Juno Therapeutics, Inc. | Composition and methods for regulating inhibitory interactions in genetically engineered cells |
| WO2016205042A1 (en) | 2015-06-16 | 2016-12-22 | The Board Of Trustees Of The Leland Stanford Junior University | SIRPα AGONIST ANTIBODY |
| HK1248255A1 (zh) | 2015-06-24 | 2018-10-12 | 优瑞科生物技术公司 | 靶向ny-eso-1肽/mhc复合物的构建体及其用途 |
| MA42456B1 (fr) | 2015-06-25 | 2021-06-30 | Univ Health Network | Inhibiteurs de hpk1 et leurs procédés d'utilisation |
| US10195175B2 (en) | 2015-06-25 | 2019-02-05 | Immunomedics, Inc. | Synergistic effect of anti-Trop-2 antibody-drug conjugate in combination therapy for triple-negative breast cancer when used with microtubule inhibitors or PARP inhibitors |
| CN116059395A (zh) | 2015-06-29 | 2023-05-05 | 第一三共株式会社 | 用于选择性制造抗体-药物缀合物的方法 |
| AU2016304794B2 (en) | 2015-08-07 | 2021-07-15 | ALX Oncology Inc. | Constructs having a SIRP-alpha domain or variant thereof |
| US20190119350A1 (en) | 2015-09-09 | 2019-04-25 | Immune Design Corp. | Ny-eso-1 specific tcrs and methods of use thereof |
| AU2016323985B2 (en) | 2015-09-17 | 2022-12-15 | Novartis Ag | CAR T cell therapies with enhanced efficacy |
| RU2748401C2 (ru) | 2015-09-18 | 2021-05-25 | Арч Онколоджи, Инк. | Терапевтические антитела к CD47 |
| WO2017053423A1 (en) | 2015-09-21 | 2017-03-30 | Erasmus University Medical Center | Anti-cd47 antibodies and methods of use |
| WO2017076308A1 (zh) | 2015-11-04 | 2017-05-11 | 广州市香雪制药股份有限公司 | 识别ny-eso-1抗原短肽的tcr |
| MA43389A (fr) | 2015-12-02 | 2021-05-12 | Agenus Inc | Anticorps anti-ox40 et leurs procédés d'utilisation |
| WO2017096276A1 (en) | 2015-12-02 | 2017-06-08 | Agenus Inc. | Anti-gitr antibodies and methods of use thereof |
| CN108883173B (zh) | 2015-12-02 | 2022-09-06 | 阿吉纳斯公司 | 抗体和其使用方法 |
| EP3383431A4 (en) | 2015-12-02 | 2019-08-28 | Agenus Inc. | ANTI-GITR ANTIBODIES AND METHOD OF USE THEREOF |
| AU2016364891A1 (en) | 2015-12-03 | 2018-06-07 | Agenus Inc. | Anti-OX40 antibodies and methods of use thereof |
| GB201522592D0 (en) | 2015-12-22 | 2016-02-03 | Immunocore Ltd | T cell receptors |
| PT3402820T (pt) | 2016-01-11 | 2020-08-20 | Forty Seven Inc | Anticorpos monoclonais anti-cd47 quiméricos, de ratinho ou humanizados |
| CN108601841A (zh) | 2016-02-10 | 2018-09-28 | 免疫医疗公司 | Abcg2抑制剂与sacituzumab govitecan(immu-132)的组合克服表达trop-2的癌中对sn-38的抗性 |
| US11306107B2 (en) | 2016-02-25 | 2022-04-19 | Amgen Inc. | Compounds that inhibit MCL-1 protein |
| WO2017160861A1 (en) | 2016-03-15 | 2017-09-21 | The Regents Of The University Of California | Inhibitors for soluble epoxide hydrolase (seh) and fatty acid amide hydrolase (faah) |
| CN107286077B (zh) | 2016-04-01 | 2021-04-02 | 合肥中科普瑞昇生物医药科技有限公司 | 一种选择性的c-kit激酶抑制剂 |
| KR20190059874A (ko) | 2016-04-08 | 2019-05-31 | 어댑티뮨 리미티드 | T 세포 수용체 |
| DK3440106T3 (da) | 2016-04-08 | 2021-10-04 | Adaptimmune Ltd | T-cellereceptorer |
| SMT202200306T1 (it) | 2016-04-08 | 2022-09-14 | Immunocore Ltd | Recettori di cellule t |
| BR112018070637A2 (pt) | 2016-04-08 | 2019-02-05 | Adaptimmune Ltd | receptores de células t |
| BR112018070823A2 (pt) | 2016-04-14 | 2019-02-05 | Ose Immunotherapeutics | anticorpo sirpa anti-humano ou fragmento de ligação a antígeno do mesmo ou mimético de anticorpo de ligação a antígeno, composição farmacêutica, produto de combinação, molécula de ácido nucleico isolada, vetor, célula hospedeira isolada, polipeptídeo, métodos para fabricar um anticorpo, in vitro ou ex vivo para determinar células positivas para sirpa, de diagnóstico e para prever a resposta de um sujeito, e, uso de um anticorpo anti-sirpa ou um fragmento de ligação a antígeno do mesmo ou um mimético de ligação a anticorpo e in vitro ou ex vivo de pelo menos um anticorpo sirpa anti-humano ou fragmento de ligação a antígeno do mesmo ou mimético de anticorpo de ligação a antígeno. |
| CA3021898A1 (en) | 2016-04-26 | 2017-11-02 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Anti-kk-lc-1 t cell receptors |
| EP3454900A4 (en) | 2016-05-09 | 2020-01-29 | Celgene Corporation | CD47 ANTIBODIES AND METHODS OF USE |
| EP3243522A1 (en) | 2016-05-10 | 2017-11-15 | Université Pierre et Marie Curie (Paris 6) | Agonist agents of cd47 inducing programmed cell death and their use in the treatments of diseases associated with defects in programmed cell death |
| MX388576B (es) | 2016-06-07 | 2025-03-20 | Jacobio Pharmaceuticals Co Ltd | Derivados heterociclicos novedosos utiles como inhibidores de shp2. |
| CN106084052B (zh) | 2016-06-17 | 2019-12-27 | 长春金赛药业股份有限公司 | 抗cd47单克隆抗体及其应用 |
| CA3029457A1 (en) | 2016-06-30 | 2018-01-04 | Gilead Sciences, Inc. | 4,6-diaminoquinazolines as cot modulators and methods of use thereof |
| CN109862910A (zh) | 2016-08-03 | 2019-06-07 | 小利兰·斯坦福大学托管委员会 | 破坏巨噬细胞上的Fc受体接合增强抗SIRPα抗体疗法的功效 |
| CN106297966A (zh) | 2016-08-22 | 2017-01-04 | 广东纳路纳米科技有限公司 | 一种金属纳米线‑抗氧化材料复合的透明导电膜及其制备 |
| CN115819417A (zh) | 2016-09-09 | 2023-03-21 | 因赛特公司 | 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途 |
| US20180072741A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyrimidine compounds and uses thereof |
| WO2018049214A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
| US10280164B2 (en) | 2016-09-09 | 2019-05-07 | Incyte Corporation | Pyrazolopyridone compounds and uses thereof |
| JOP20190009A1 (ar) | 2016-09-21 | 2019-01-27 | Alx Oncology Inc | أجسام مضادة ضد بروتين ألفا منظم للإشارات وطرق استخدامها |
| AU2017332960B2 (en) | 2016-10-20 | 2019-09-12 | I-Mab Biopharma Us Limited | Novel CD47 monoclonal antibodies and uses thereof |
| EP3529276A4 (en) | 2016-10-21 | 2020-06-17 | Arch Oncology, Inc. | CD47 THERAPEUTIC ANTIBODIES |
| US11352425B2 (en) | 2016-11-08 | 2022-06-07 | Absos, Llc | Anti-CD47 antibodies |
| MA46770A (fr) | 2016-11-09 | 2019-09-18 | Agenus Inc | Anticorps anti-ox40, anticorps anti-gitr, et leurs procédés d'utilisation |
| WO2018098280A1 (en) | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use |
| WO2018097951A1 (en) | 2016-11-22 | 2018-05-31 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Anti-mage-a3/a6 antibodies |
| CN108779179B (zh) | 2016-11-28 | 2022-02-08 | 江苏恒瑞医药股份有限公司 | Cd47抗体、其抗原结合片段及其医药用途 |
| WO2018102366A1 (en) | 2016-11-30 | 2018-06-07 | Ariad Pharmaceuticals, Inc. | Anilinopyrimidines as haematopoietic progenitor kinase 1 (hpk1) inhibitors |
| BR112019011200B1 (pt) | 2016-12-01 | 2021-12-28 | Arvinas Operations, Inc | Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio |
| AU2017371070B2 (en) | 2016-12-09 | 2025-01-02 | Alector Llc | Anti-SIRP-alpha antibodies and methods of use thereof |
| EA201991197A1 (ru) | 2016-12-15 | 2020-01-13 | Ариад Фармасьютикалз, Инк. | БЕНЗИМИДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ c-Kit |
| CN117050032A (zh) | 2016-12-15 | 2023-11-14 | 阿瑞雅德制药公司 | 作为c-kit抑制剂的氨基噻唑化合物 |
| KR20250117470A (ko) | 2016-12-23 | 2025-08-04 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법 |
| BR112019013908A2 (pt) | 2017-01-06 | 2020-02-04 | Scholar Rock, Inc. | inibidores de tgfss1 isoforma-específicos, contexto-permissivos, e seus usos |
| JP2020503883A (ja) | 2017-01-13 | 2020-02-06 | アジェナス インコーポレイテッド | Ny−eso−1に結合するt細胞受容体およびその使用方法 |
| BR112019015312A2 (pt) | 2017-01-26 | 2020-03-10 | Arvinas Operations, Inc. | Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados |
| WO2018137705A1 (en) | 2017-01-26 | 2018-08-02 | Zai Lab (Shanghai) Co., Ltd. | Cd47 antigen binding unit and uses thereof |
| IL312367A (en) | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Cereblon ligands and bifunctional compounds comprising the same |
| CN110402248B (zh) | 2017-03-15 | 2023-01-06 | 豪夫迈·罗氏有限公司 | 作为hpk1抑制剂的氮杂吲哚类 |
| JP7037577B2 (ja) | 2017-03-15 | 2022-03-16 | フレッド ハッチンソン キャンサー リサーチ センター | 高親和性mage-a1特異的tcr及びその使用 |
| DE102017106305A1 (de) | 2017-03-23 | 2018-09-27 | Immatics Biotechnologies Gmbh | Neue T-Zellrezeptoren und deren Verwendung in Immuntherapien gegen prame-positive Krebsarten |
| EA202190196A1 (ru) | 2017-03-23 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| EP3600283A4 (en) | 2017-03-27 | 2020-12-16 | Immunomedics, Inc. | TREATMENT OF TROP-2 EXPRESSIVE TRIPLE NEGATIVE BREAST CANCER WITH SACITUZUMAB GOVITECAN AND A RAD51 INHIBITOR |
| EP3601259B1 (en) | 2017-03-30 | 2022-02-23 | F. Hoffmann-La Roche AG | Isoquinolines as inhibitors of hpk1 |
| AU2018244935A1 (en) | 2017-03-30 | 2019-08-15 | F. Hoffmann-La Roche Ag | Naphthyridines as inhibitors of HPK1 |
| JP6453507B2 (ja) | 2017-03-30 | 2019-01-16 | アムジエン・インコーポレーテツド | Mcl−1タンパク質を阻害する化合物 |
| KR102702926B1 (ko) | 2017-04-13 | 2024-09-06 | 사이로파 비.브이. | 항-sirp 알파 항체 |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| CN118271443A (zh) | 2017-05-16 | 2024-07-02 | 拜奥迪斯私人有限公司 | 抗SIRPα抗体 |
| WO2018217227A1 (en) | 2017-05-24 | 2018-11-29 | Immunomedics, Inc. | Novel anti-pd-1 checkpoint inhibitor antibodies that block binding of pd-l1 to pd-1 |
| CN108976278B (zh) | 2017-06-05 | 2021-04-06 | 海创药业股份有限公司 | 一种嵌合分子及其制备和应用 |
| WO2018225732A1 (ja) | 2017-06-05 | 2018-12-13 | 国立大学法人三重大学 | Mage-a4由来ペプチドを認識する抗原結合性タンパク質 |
| WO2018226542A1 (en) | 2017-06-09 | 2018-12-13 | Arvinas, Inc. | Modulators of proteolysis and associated methods of use |
| GB201709866D0 (en) | 2017-06-20 | 2017-08-02 | Immunocore Ltd | T cell receptors |
| CN109096395B (zh) | 2017-06-20 | 2022-06-24 | 华兰生物工程股份有限公司 | 阻断型cd47纳米抗体及其用途 |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| BR112020001653A2 (pt) | 2017-07-26 | 2020-07-21 | Forty Seven, Inc. | anticorpos anti-sirp-alfa e métodos relacionados |
| JP7262440B2 (ja) | 2017-08-02 | 2023-04-21 | フェインズ セラピューティクス,インコーポレーテッド | 抗cd47抗体及びその使用 |
| WO2019032624A1 (en) | 2017-08-08 | 2019-02-14 | Pionyr Immunotherapeutics, Inc. | COMPOSITIONS AND METHODS FOR DEACTIVATING TREM1-EXPRESSING MESHLOID CELLS |
| CN107446050A (zh) | 2017-08-11 | 2017-12-08 | 百奥泰生物科技(广州)有限公司 | Trop2阳性疾病治疗的化合物及方法 |
| CN111212852A (zh) | 2017-08-18 | 2020-05-29 | 超人肆有限公司 | 结合剂 |
| TWI793151B (zh) | 2017-08-23 | 2023-02-21 | 瑞士商諾華公司 | 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途 |
| CN109422811A (zh) | 2017-08-29 | 2019-03-05 | 信达生物制药(苏州)有限公司 | 抗cd47抗体及其用途 |
| CN108503708B (zh) | 2017-09-01 | 2021-07-30 | 北京智仁美博生物科技有限公司 | 抗人cd47抗体及其用途 |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| CN109422726B (zh) | 2017-09-04 | 2022-10-28 | 华东理工大学 | CD47/SIRPα的阻断剂及其应用 |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| US20200239530A1 (en) | 2017-09-27 | 2020-07-30 | Vividion Therapeutics, Inc. | Compounds and methods of modulating protein degradation |
| WO2019079701A1 (en) | 2017-10-20 | 2019-04-25 | Dana-Farber Cancer Institute, Inc. | HETEROBIFUNCTIONAL COMPOUNDS HAVING IMPROVED SPECIFICITY FOR BRD4 BROMODOMAINE |
| WO2019084030A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE |
| WO2019084026A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE |
| WO2019084538A1 (en) | 2017-10-27 | 2019-05-02 | Board Of Regents, The University Of Texas System | TUMOR SPECIFIC ANTIBODIES, T CELL RECEPTORS AND METHODS OF IDENTIFICATION THEREOF |
| AU2018358004A1 (en) | 2017-11-01 | 2020-05-28 | Hummingbird Bioscience Pte. Ltd. | CD47 antigen-binding molecules |
| EP3710443A1 (en) | 2017-11-17 | 2020-09-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| WO2019103203A1 (ko) | 2017-11-24 | 2019-05-31 | 주식회사 젬백스앤카엘 | 신규 펩티드 및 이를 포함한 조성물 |
| SG11202004864TA (en) | 2017-12-01 | 2020-06-29 | Seattle Genetics Inc | Cd47 antibodies and uses thereof for treating cancer |
| WO2019113123A1 (en) | 2017-12-04 | 2019-06-13 | Precithera, Inc. | TGF-ß RECEPTOR FUSION PROTEINS AND OTHER TGF-ß ANTAGONISTS FOR REDUCING TGF-ß SIGNALING |
| CN109879957B (zh) | 2017-12-06 | 2022-03-18 | 香雪生命科学技术(广东)有限公司 | 针对prame的高亲和力t细胞受体 |
| EP3720881A1 (en) | 2017-12-08 | 2020-10-14 | Elstar Therapeutics, Inc. | Multispecific molecules and uses thereof |
| AU2018383709B2 (en) | 2017-12-12 | 2025-09-11 | Pionyr Immunotherapeutics, Inc. | Anti-TREM2 antibodies and related methods |
| CA3087841A1 (en) | 2018-01-12 | 2019-07-18 | Aurigene Discovery Technologies Limited | 1,2,4-oxadiazole compounds as inhibitors of cd47 signalling pathways |
| CA3089512A1 (en) | 2018-01-24 | 2019-08-01 | Nanjing Legend Biotech Co., Ltd. | Anti-cd47 antibodies that do not cause significant red blood cell agglutination |
| GB201802201D0 (en) | 2018-02-09 | 2018-03-28 | Ultrahuman Five Ltd | Binding agents |
| CR20200347A (es) | 2018-02-13 | 2020-09-23 | Gilead Sciences Inc | Inhibidores pd-1/pd-l1 |
| CN110144009B (zh) | 2018-02-14 | 2020-01-21 | 上海洛启生物医药技术有限公司 | Cd47单域抗体及其用途 |
| TWI822726B (zh) | 2018-02-26 | 2023-11-21 | 德商梅迪基因免疫治療公司 | Nyeso t細胞受體 |
| WO2019173692A2 (en) | 2018-03-09 | 2019-09-12 | Agenus Inc. | Anti-cd73 antibodies and methods of use thereof |
| JP2021517130A (ja) | 2018-03-13 | 2021-07-15 | オーセ イミュノセラピューティクスOse Immunotherapeutics | 抗ヒトSIRPav1抗体の使用および抗v1抗体を製造する方法 |
| WO2019179366A1 (en) | 2018-03-20 | 2019-09-26 | Wuxi Biologics (Shanghai) Co. Ltd. | Novel anti-cd47 antibodies |
| PE20201265A1 (es) | 2018-03-21 | 2020-11-19 | Alx Oncology Inc | Anticuerpos contra proteina alfa reguladora de senal y metodos de uso |
| EP3773576A4 (en) * | 2018-03-26 | 2021-12-29 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| GB201804860D0 (en) | 2018-03-27 | 2018-05-09 | Ultrahuman Two Ltd | CD47 Binding agents |
| CN110305212A (zh) | 2018-03-27 | 2019-10-08 | 信达生物制药(苏州)有限公司 | 抗cd47抗体及其用途 |
| IL302595A (en) | 2018-04-13 | 2023-07-01 | Arvinas Operations Inc | Servalon ligands and bifunctional compounds containing them |
| CN110386984B (zh) | 2018-04-17 | 2022-04-22 | 杭州尚健生物技术有限公司 | 结合cd47蛋白的融合蛋白及其应用 |
| WO2019204683A1 (en) | 2018-04-19 | 2019-10-24 | Board Of Regents, The University Of Texas System | T cell receptors with mage-b2 specificity and uses thereof |
| CN110577597B (zh) | 2018-06-11 | 2021-10-22 | 康诺亚生物医药科技(成都)有限公司 | 一种阻断CD47和SIRPα相互作用的抗体 |
| CA3101338A1 (en) | 2018-06-13 | 2019-12-19 | Biotheryx, Inc. | Aminoamide compounds |
| US11634490B2 (en) | 2018-06-15 | 2023-04-25 | Accurus Biosciences, Inc. | Blocking antibodies against CD47 and methods of use thereof |
| AU2019294835B2 (en) | 2018-06-29 | 2025-04-17 | Dana-Farber Cancer Institute, Inc. | Ligands to cereblon (CRBN) |
| JP2021529219A (ja) | 2018-07-05 | 2021-10-28 | トリカン・バイオテクノロジー・カンパニー・リミテッドTrican Biotechnology Co., Ltd | ヒト抗cd47抗体およびその使用 |
| EP3821005A4 (en) | 2018-07-09 | 2022-10-26 | Genequantum Healthcare (Suzhou) Co., Ltd. | AGAINST TROPHOBLAST ANTIGEN 2 (TROP2) SPECIFIC ANTIBODIES |
| BR122022012697B1 (pt) * | 2018-07-10 | 2023-04-04 | Novartis Ag | Usos de derivados de 3-(5-hidróxi-1-oxoisoindolin-2-il)piperidina-2,6- diona, e kit |
| SG11202012338QA (en) | 2018-07-10 | 2021-01-28 | Univ Kobe Nat Univ Corp | ANTI-SIRPa ANTIBODY |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| SG11202012425QA (en) | 2018-07-13 | 2021-01-28 | Gilead Sciences Inc | Pd-1/pd-l1 inhibitors |
| WO2020019135A1 (zh) | 2018-07-23 | 2020-01-30 | 中国科学院微生物研究所 | 一种抗cd47抗体及其应用 |
| WO2020036977A1 (en) | 2018-08-13 | 2020-02-20 | Arch Oncology, Inc. | Therapeutic cd47 antibodies |
| EP3845561A4 (en) | 2018-08-31 | 2022-07-06 | Nanjing Sanhome Pharmaceutical Co., Ltd. | ANTI-CD47 ANTIBODIES AND ITS USE |
| CA3111381A1 (en) | 2018-09-05 | 2020-04-30 | The Regents Of The University Of California | Composition of ny-eso-1-specific t cell receptors restricted on multiple major histocompatibility complex molecules |
| CN110950949B (zh) | 2018-09-26 | 2022-04-05 | 香雪生命科学技术(广东)有限公司 | 一种识别ssx2抗原的t细胞受体 |
| BR112021005585A2 (pt) | 2018-09-27 | 2021-06-29 | Celgene Corporation | proteínas de ligação a sirpa e métodos de uso das mesmas |
| KR102716514B1 (ko) | 2018-10-10 | 2024-10-15 | 주식회사 노벨티노빌리티 | 신규 항-c-KIT 항체 |
| WO2020086647A1 (en) | 2018-10-23 | 2020-04-30 | Regeneron Pharmaceuticals, Inc. | Ny-eso-1 t cell receptors and methods of use thereof |
| US11203591B2 (en) | 2018-10-31 | 2021-12-21 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| WO2020092528A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
| CN113260384A (zh) | 2018-11-05 | 2021-08-13 | 西纳福克斯股份有限公司 | 用于靶向表达trop-2的肿瘤的抗体缀合物 |
| AU2019391016B2 (en) | 2018-12-03 | 2025-05-29 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of helios and methods of use |
| KR20210106437A (ko) | 2018-12-20 | 2021-08-30 | 노파르티스 아게 | 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 및 약학적 조합물 |
| US20220040324A1 (en) | 2018-12-21 | 2022-02-10 | Daiichi Sankyo Company, Limited | Combination of antibody-drug conjugate and kinase inhibitor |
| WO2020138489A1 (ja) | 2018-12-27 | 2020-07-02 | 塩野義製薬株式会社 | 新規抗ccr8抗体 |
| CA3123519A1 (en) | 2019-02-15 | 2020-08-20 | Novartis Ag | Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| CN113490528B (zh) | 2019-02-15 | 2024-12-03 | 诺华股份有限公司 | 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途 |
| JP2022533260A (ja) | 2019-05-24 | 2022-07-21 | バイオセリックス, インコーポレイテッド | タンパク質を標的とする化合物及びその医薬組成物並びにそれらの治療的応用 |
| IL288485B2 (en) | 2019-05-29 | 2026-04-01 | Daiichi Sankyo Co Ltd | Anti-TROP2 antibody conjugates - a drug for use in cancer treatment |
| KR102913106B1 (ko) | 2019-05-31 | 2026-01-19 | 셀진 코포레이션 | 치환된 1-옥소-이소인돌린-5-카르복스아미드 화합물, 그의 조성물 및 그를 사용한 치료 방법 |
| WO2020249063A1 (en) | 2019-06-13 | 2020-12-17 | Bio-Thera Solutions, Ltd. | Methods for the treatment of trop2 positive diseases |
| WO2020257648A1 (en) | 2019-06-20 | 2020-12-24 | Fred Hutchinson Cancer Research Center | Microlumenal targeting of cancer cells |
| WO2020263830A1 (en) | 2019-06-25 | 2020-12-30 | Gilead Sciences, Inc. | Flt3l-fc fusion proteins and methods of use |
| US20210093730A1 (en) | 2019-10-01 | 2021-04-01 | Immunomedics, Inc. | Biomarkers for antibody-drug conjugate monotherapy or combination therapy |
| KR20220092920A (ko) | 2019-10-30 | 2022-07-04 | 다나-파버 캔서 인스티튜트 인크. | 헬리오스의 소분자 분해제 및 사용 방법 |
| JP7629459B2 (ja) | 2019-11-19 | 2025-02-13 | ブリストル-マイヤーズ スクイブ カンパニー | Heliosタンパク質の阻害剤として有用な化合物 |
| IL294032A (en) | 2019-12-24 | 2022-08-01 | Carna Biosciences Inc | Compounds that regulate diacylglycerol kinase |
| KR20220124228A (ko) | 2020-01-20 | 2022-09-13 | 강푸 바이오파마슈티칼즈 리미티드 | 이소인돌린 유도체, 및 이의 제약 조성물 및 용도 |
| TWI890283B (zh) | 2020-02-14 | 2025-07-11 | 美商基利科學股份有限公司 | 結合ccr8之抗體及融合蛋白及其用途 |
| TW202140441A (zh) | 2020-03-23 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 經取代之側氧基異吲哚啉化合物 |
| CN111534585A (zh) | 2020-03-23 | 2020-08-14 | 至本医疗科技(上海)有限公司 | 一种非小细胞肺癌(nsclc)患者免疫疗法预后的方法 |
| US20230167081A1 (en) | 2020-04-30 | 2023-06-01 | President And Fellows Of Harvard College | 5-amino-2-piperidinon-3-yl-1-oxoisoindoline derivatives for degradation of ikzf2 degraders |
| CA3172589A1 (en) | 2020-05-21 | 2021-11-25 | Dana-Farber Cancer Institute, Inc. | Piperidine-2,6-diones as small molecule degraders of helios and methods of use |
| KR20230027056A (ko) | 2020-06-23 | 2023-02-27 | 노파르티스 아게 | 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 |
| TW202216771A (zh) | 2020-06-26 | 2022-05-01 | 德商拜耳廠股份有限公司 | 用於治療應用之ccr8抗體 |
| JP7819176B2 (ja) | 2020-08-03 | 2026-02-24 | ノバルティス アーゲー | ヘテロアリール置換3-(1-オキソイソインドリン-2-イル)ピペリジン-2,6-ジオン誘導体及びその使用 |
| US20240294489A1 (en) | 2020-08-03 | 2024-09-05 | Captor Therapeutics S.A. | Low molecular weight protein degraders and their applications |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| CN113271428A (zh) | 2020-09-30 | 2021-08-17 | 常熟九城智能科技有限公司 | 一种视频会议用户鉴权方法、装置及系统 |
| IL301690A (en) | 2020-10-16 | 2023-05-01 | Dana Farber Cancer Inst Inc | Piperidinyl small molecule degraders of helios and methods of use |
| CN112321715B (zh) | 2020-11-03 | 2022-05-10 | 博奥信生物技术(南京)有限公司 | 抗trop2纳米抗体及其制备方法和应用 |
| WO2022099117A1 (en) * | 2020-11-06 | 2022-05-12 | Prelude Therapeutics Incorporated | Brm targeting compounds and associated methods of use |
| WO2022159644A1 (en) * | 2021-01-23 | 2022-07-28 | Newave Pharmaceutical Inc. | Spirocyclic mdm2 modulator and uses thereof |
| WO2022187423A1 (en) | 2021-03-03 | 2022-09-09 | The Regents Of The University Of Michigan | Cereblon ligands |
| EP4320112B1 (en) | 2021-04-06 | 2025-05-14 | Bristol-Myers Squibb Company | Pyridinyl substituted oxoisoindoline compounds |
| WO2022219412A1 (en) | 2021-04-14 | 2022-10-20 | Monte Rosa Therapeutics Ag | Isoindolinone amide compounds useful to treat diseases associated with gspt1 |
| EP4323350A1 (en) | 2021-04-14 | 2024-02-21 | Monte Rosa Therapeutics AG | Isoindolinone compounds |
| JP2024517772A (ja) | 2021-04-29 | 2024-04-23 | ネオモルフ インコーポレイテッド | 置換された2-(2,6-ジオキソピペリジン-3-イル)-5-(1-ピペリジン-4-イル)イソインドリン-1,3-ジオン誘導体及びその使用 |
| WO2022232391A1 (en) | 2021-04-29 | 2022-11-03 | Dana-Farber Cancer Institute, Inc. | Phthalimido cereblon complex binders and transcription factor degraders and methods of use |
| CN117377675A (zh) | 2021-06-01 | 2024-01-09 | 正大天晴药业集团股份有限公司 | 含有并环或螺环的布鲁顿酪氨酸激酶降解剂 |
| WO2022254362A1 (en) | 2021-06-03 | 2022-12-08 | Novartis Ag | 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof |
| CA3221549A1 (en) | 2021-06-08 | 2022-12-15 | Liqiang Fu | Isoindolinone compounds, and uses thereof |
| CN115504963A (zh) | 2021-06-22 | 2022-12-23 | 苏州开拓药业股份有限公司 | 一种c-Myc蛋白降解剂 |
| CA3226162A1 (en) | 2021-07-09 | 2023-01-12 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| EP4367114A1 (en) | 2021-07-09 | 2024-05-15 | Plexium, Inc. | Cycloalkyl compounds and pharmaceutical compositions that modulate ikzf2 |
| US20250100996A1 (en) | 2021-07-09 | 2025-03-27 | Plexium, Inc. | Heterocycloalkyl and heteroaryl compounds and pharmaceutical compositions that modulate ikzf2 |
| CN117396208A (zh) | 2021-07-16 | 2024-01-12 | 达纳-法伯癌症研究所公司 | 细胞周期蛋白依赖性激酶4/6(cdk4/6)和ikzf2(helios)的小分子降解剂及其使用方法 |
| US20240409528A1 (en) | 2021-10-01 | 2024-12-12 | Dana-Farber Cancer Institute, Inc. | Binders of cereblon and methods of use thereof |
| WO2023116835A1 (zh) | 2021-12-24 | 2023-06-29 | 苏州开拓药业股份有限公司 | 一种具有酰亚胺骨架的多蛋白降解剂 |
| WO2023178181A1 (en) * | 2022-03-17 | 2023-09-21 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| CN114835680A (zh) | 2022-04-29 | 2022-08-02 | 成都分迪药业有限公司 | 卤素取代异吲哚啉化合物及其应用 |
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