DE69929993T4 - Nicht-endogene, konstitutiv aktivierte, menschliche, an ein g-protein gekoppelte rezeptoren - Google Patents
Nicht-endogene, konstitutiv aktivierte, menschliche, an ein g-protein gekoppelte rezeptoren Download PDFInfo
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- DE69929993T4 DE69929993T4 DE69929993T DE69929993T DE69929993T4 DE 69929993 T4 DE69929993 T4 DE 69929993T4 DE 69929993 T DE69929993 T DE 69929993T DE 69929993 T DE69929993 T DE 69929993T DE 69929993 T4 DE69929993 T4 DE 69929993T4
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- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US170496 | 1998-10-13 | ||
| US09/170,496 US6555339B1 (en) | 1997-04-14 | 1998-10-13 | Non-endogenous, constitutively activated human protein-coupled receptors |
| PCT/US1999/023938 WO2000022129A1 (en) | 1998-10-13 | 1999-10-12 | Non-endogenous, constitutively activated human g protein-coupled receptors |
Publications (2)
| Publication Number | Publication Date |
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| DE69929993T2 DE69929993T2 (de) | 2006-10-26 |
| DE69929993T4 true DE69929993T4 (de) | 2008-08-28 |
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| DE1121431T Pending DE1121431T1 (de) | 1998-10-13 | 1999-10-12 | Nicht-endogene, konstitutiv aktivierte, menschliche, an ein g-protein gekoppelte rezeptoren |
| DE69929993A Expired - Lifetime DE69929993D1 (de) | 1998-10-13 | 1999-10-12 | Nicht-endogene, konstitutiv aktivierte, menschliche, an ein g-protein gekoppelte rezeptoren |
| DE69929993T Expired - Lifetime DE69929993T4 (de) | 1998-10-13 | 1999-10-12 | Nicht-endogene, konstitutiv aktivierte, menschliche, an ein g-protein gekoppelte rezeptoren |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
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| DE1121431T Pending DE1121431T1 (de) | 1998-10-13 | 1999-10-12 | Nicht-endogene, konstitutiv aktivierte, menschliche, an ein g-protein gekoppelte rezeptoren |
| DE69929993A Expired - Lifetime DE69929993D1 (de) | 1998-10-13 | 1999-10-12 | Nicht-endogene, konstitutiv aktivierte, menschliche, an ein g-protein gekoppelte rezeptoren |
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Families Citing this family (172)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7888466B2 (en) | 1996-01-11 | 2011-02-15 | Human Genome Sciences, Inc. | Human G-protein chemokine receptor HSATU68 |
| US6555339B1 (en) * | 1997-04-14 | 2003-04-29 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human protein-coupled receptors |
| USRE42190E1 (en) | 1998-11-20 | 2011-03-01 | Arena Pharmaceuticals, Inc. | Method of identifying a compound for inhibiting or stimulating human G protein-coupled receptors |
| US20030017528A1 (en) | 1998-11-20 | 2003-01-23 | Ruoping Chen | Human orphan G protein-coupled receptors |
| ES2308759T3 (es) * | 1998-11-20 | 2008-12-01 | Arena Pharmaceuticals, Inc. | Receptores acoplados a proteina g humanos huerfanos. |
| US7816492B2 (en) * | 1998-11-20 | 2010-10-19 | Arena Pharmaceuticals, Inc. | Human G protein-coupled receptors |
| GB9903767D0 (en) * | 1999-02-18 | 1999-04-14 | Univ Glasgow | Receptor assay |
| EP1235931A2 (en) * | 1999-07-30 | 2002-09-04 | Millennium Pharmaceuticals, Inc. | Compositions, kits, and methods for prognostication, diagnosis, prevention, and treatment of bone-related disorders and other disorders |
| JP4768946B2 (ja) * | 1999-11-17 | 2011-09-07 | アリーナ ファーマシューティカルズ, インコーポレイテッド | ヒトgタンパク質共役型受容体の内因性および非内因性型 |
| JP2003518628A (ja) * | 1999-12-10 | 2003-06-10 | アストラゼネカ アクチボラグ | 化合物 |
| EP1265922A2 (en) * | 1999-12-17 | 2002-12-18 | AstraZeneca AB | Agonists and antagonists of the receptor gpr19 and their use in appetite control |
| GB0003902D0 (en) * | 2000-02-18 | 2000-04-05 | Glaxo Group Ltd | Assay |
| US20030113810A1 (en) * | 2000-02-18 | 2003-06-19 | Alan Wise | Novel assay |
| GB0003898D0 (en) * | 2000-02-18 | 2000-04-05 | Glaxo Group Ltd | Assay |
| WO2001064872A2 (en) * | 2000-02-29 | 2001-09-07 | Millennium Pharmaceuticals, Inc. | Gene 2465: methods and compositions for the diagnosis and treatment of cardiovascular, hepatic and bone disease |
| US6436703B1 (en) * | 2000-03-31 | 2002-08-20 | Hyseq, Inc. | Nucleic acids and polypeptides |
| MXPA02010241A (es) * | 2000-04-26 | 2004-09-06 | Aventis Pharma Gmbh | Receptor edg8, su preparacion y uso. |
| EP1149907A1 (en) * | 2000-04-26 | 2001-10-31 | Aventis Pharma Deutschland GmbH | EDG8 receptor, its preparation and use |
| JP2003531637A (ja) * | 2000-05-03 | 2003-10-28 | アストラゼネカ アクチボラグ | 方 法 |
| AU2001274522A1 (en) * | 2000-06-15 | 2001-12-24 | Takeda Chemical Industries Ltd. | Novel g protein-coupled receptor protein and dna thereof |
| AU2001268471A1 (en) * | 2000-06-16 | 2002-01-02 | Incyte Genomics, Inc. | G-protein coupled receptors |
| CA2413195C (en) | 2000-06-21 | 2012-01-17 | Takeda Chemical Industries, Ltd. | Ligand to gpr8 and dna thereof |
| WO2002002767A1 (fr) * | 2000-07-04 | 2002-01-10 | Takeda Chemical Industries, Ltd. | Proteine de recepteur couple a la proteine g et adn correspondant |
| EP1364017A2 (en) * | 2000-08-18 | 2003-11-26 | Novartis AG | Inflammation related g-protein coupled receptor |
| WO2002018590A2 (en) * | 2000-08-30 | 2002-03-07 | John Hopkins University School Of Medicine | Identification of activated receptors and ion channels |
| AU2000276780A1 (en) * | 2000-10-02 | 2001-04-23 | Biofocus Discovery Limited | Cellular receptor mutations predicted by multiple-sequence-allignment |
| EP1344823A4 (en) * | 2000-11-30 | 2005-03-16 | Takeda Chemical Industries Ltd | NEW G-PROTEIN-COUPLED RECEPTOR PROTEINS AND THEIR DNAS |
| US7241579B2 (en) | 2000-12-22 | 2007-07-10 | Smithkline Beecham Corporation | Method of screening for GPR40 ligands |
| GB0031527D0 (en) * | 2000-12-22 | 2001-02-07 | Smithkline Beecham Plc | New use |
| CA2439383A1 (en) * | 2001-02-26 | 2002-09-06 | Arena Pharmaceuticals, Inc. | Endogenous and non-endogenous versions of human g protein-coupled receptors |
| US6809104B2 (en) | 2001-05-04 | 2004-10-26 | Tularik Inc. | Fused heterocyclic compounds |
| US6919176B2 (en) * | 2001-05-07 | 2005-07-19 | Amgen Inc. | Polypeptides and nucleic acids associated with cancer |
| ATE371863T1 (de) * | 2001-05-15 | 2007-09-15 | Takeda Pharmaceutical | Screening-verfahren |
| US20020177190A1 (en) * | 2001-05-24 | 2002-11-28 | Yanbin Liang | Recombinant simian GPR3 receptor |
| EP1404708A4 (en) * | 2001-06-05 | 2005-01-19 | Arena Pharm Inc | NON-ENDED, CONSTITUTIVELY ACTIVATED VERSIONS OF THE G-PROTEIN-COUPLED RECEPTOR GCR1 FROM PLANTS |
| JP2003018992A (ja) * | 2001-06-28 | 2003-01-21 | Inst Of Physical & Chemical Res | Pael受容体、Pael受容体発現細胞および動物、ならびにパーキンソン病治療薬のスクリーニング法 |
| WO2003006504A2 (en) * | 2001-07-13 | 2003-01-23 | Akzo Nobel N.V. | Allelic variants of gpr50 |
| US20030109044A1 (en) * | 2001-10-16 | 2003-06-12 | Millennium Pharmaceuticals, Inc. | Methods of using 279, a human G protein-coupled protein receptor |
| EP1450666A4 (en) * | 2001-11-05 | 2008-11-12 | Millennium Pharm Inc | METHOD AND COMPOSITIONS FOR TREATING HEART CIRCULAR ILLNESSES USING 139,258,1261,1486,2398,2414,7660,8587,10183,10550,12680,17921,32248,60489 OR 93804 |
| US6902902B2 (en) | 2001-11-27 | 2005-06-07 | Arena Pharmaceuticals, Inc. | Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders |
| DK1463759T3 (da) | 2002-01-07 | 2013-08-12 | Euroscreen Sa | Ligand for den G-proteinkoblede receptor GPR43 og anvendelser deraf |
| EP1336655A1 (en) * | 2002-01-12 | 2003-08-20 | Aventis Pharma Deutschland GmbH | Method of identifying protein CAMS (constitutively active mutants) |
| US20030175889A1 (en) * | 2002-01-23 | 2003-09-18 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated versions of human G protein coupled receptor: FSHR |
| WO2003066077A2 (en) * | 2002-02-06 | 2003-08-14 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with neuromedin u1 receptor (nmu1) |
| EP1479768B1 (en) | 2002-02-14 | 2010-04-28 | Takeda Pharmaceutical Company Limited | Novel screening method |
| AU2003218234A1 (en) * | 2002-03-15 | 2003-09-29 | Arena Pharmaceuticals, Inc. | Methods of expressing non-endogenous g protein coupled receptors in cells |
| AU2003241037A1 (en) * | 2002-06-08 | 2003-12-22 | Astrazeneca Ab | Methods for the detection of polymorphisms in human gpr50 |
| CA2494607A1 (en) * | 2002-08-01 | 2004-02-12 | Arena Pharmaceuticals, Inc. | Human g protein-coupled receptor and modulators thereof for the treatment of ischemic heart disease and congestive heart failure |
| WO2004015427A2 (en) * | 2002-08-06 | 2004-02-19 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g-protein coupled receptor 19 (gpr19) |
| AU2003251471A1 (en) * | 2002-08-06 | 2004-02-25 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with human cxc chemokine receptor 5(cxcr5) |
| JPWO2004017994A1 (ja) * | 2002-08-22 | 2005-12-08 | 協和醗酵工業株式会社 | 喘息の予防および/または治療剤 |
| AU2003276106A1 (en) * | 2002-10-24 | 2004-05-13 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with human g-protein coupled receptor 12 (gpr12) |
| US7056685B1 (en) * | 2002-11-05 | 2006-06-06 | Amgen Inc. | Receptor ligands and methods of modulating receptors |
| EP1562943A1 (en) | 2002-11-06 | 2005-08-17 | Amgen Inc. | Fused heterocyclic compounds |
| US7960369B2 (en) | 2002-11-08 | 2011-06-14 | Takeda Pharmaceutical Company Limited | Receptor function regulator |
| US7189524B1 (en) | 2002-11-25 | 2007-03-13 | Amgen, Inc. | Receptor ligands and methods of modulating receptors |
| AU2003297644A1 (en) * | 2002-12-04 | 2004-06-23 | Synaptic Pharmaceutical Corporation | Uses of the snorf55 receptor |
| US20040157253A1 (en) * | 2003-02-07 | 2004-08-12 | Millennium Pharmaceuticals, Inc. | Methods and compositions for use of inflammatory proteins in the diagnosis and treatment of metabolic disorders |
| EP1603585A2 (en) * | 2003-03-14 | 2005-12-14 | Bristol-Myers Squibb Company | Polynucleotide encoding a novel human g-protein coupled receptor variant of hm74, hgprbmy74 |
| WO2004083394A2 (en) * | 2003-03-18 | 2004-09-30 | Arena Pharmaceuticals Inc. | Human g protein-coupled receptors and modulators thereof for the treatment of inflammatory disorders |
| JPWO2004093912A1 (ja) * | 2003-04-23 | 2006-07-13 | 協和醗酵工業株式会社 | 好中球性炎症疾患の予防および/または治療剤 |
| US20080009551A1 (en) * | 2003-04-30 | 2008-01-10 | Arena Pharmaceuticals, Inc. | Methods and Compositions for Identifying Modulators of G Protein-Coupled Receptors |
| CA2525286C (en) * | 2003-05-20 | 2012-09-11 | The University Court Of The University Of Glasgow | Materials and methods relating to g-protein coupled receptor oligomers |
| ATE405827T1 (de) * | 2003-09-11 | 2008-09-15 | Takeda Pharmaceutical | Screening-verfahren |
| US20070276024A1 (en) * | 2003-10-09 | 2007-11-29 | Inverseon , Inc. | Methods for Treating Diseases and Conditions with Inverse Agonists and for Screening for Agents Acting as Inverse Agonists |
| EP1684764A2 (en) * | 2003-10-09 | 2006-08-02 | Inverseon, Inc. | Methods for treating diseases and conditions with inverse agonists and for screening for agents acting as inverse agonists |
| WO2005040829A2 (en) * | 2003-10-21 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 17 (gpr17) |
| WO2005040211A2 (en) * | 2003-10-23 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 1 (gpr1) |
| WO2005040828A2 (en) * | 2003-10-24 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 49 (gpr49) |
| WO2005040825A2 (en) * | 2003-10-24 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 20 (gpr20) |
| BR122018071808B8 (pt) | 2003-11-06 | 2020-06-30 | Seattle Genetics Inc | conjugado |
| WO2005074980A1 (en) * | 2004-01-29 | 2005-08-18 | Cellzome Ag | Treatment of neurodegenerative diseases by the use of gpr49 |
| CA2556757C (en) | 2004-02-20 | 2011-05-03 | Aventis Pharmaceuticals Inc. | Oxydecahydronaphthalene modulators of hm74 |
| WO2005101005A1 (en) * | 2004-04-15 | 2005-10-27 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g-protein coupled receptor 32 (gpr32) |
| ATE486962T1 (de) * | 2004-04-27 | 2010-11-15 | Takeda Pharmaceutical | Neuer ligand eines g-protein-konjugierten rezeptorproteins und verwendung davon |
| BRPI0510883B8 (pt) | 2004-06-01 | 2021-05-25 | Genentech Inc | composto conjugado de droga e anticorpo, composição farmacêutica, método de fabricação de composto conjugado de droga e anticorpo e usos de uma formulação, de um conjugado de droga e anticorpo e um agente quimioterapêutico e de uma combinação |
| US20100111856A1 (en) | 2004-09-23 | 2010-05-06 | Herman Gill | Zirconium-radiolabeled, cysteine engineered antibody conjugates |
| CN101065151B (zh) | 2004-09-23 | 2014-12-10 | 健泰科生物技术公司 | 半胱氨酸改造的抗体和偶联物 |
| US7528175B2 (en) * | 2004-10-08 | 2009-05-05 | Inverseon, Inc. | Method of treating airway diseases with beta-adrenergic inverse agonists |
| GB0508988D0 (en) | 2005-05-03 | 2005-06-08 | Novartis Ag | Organic compounds |
| US8429755B2 (en) | 2005-05-26 | 2013-04-23 | Sandisk Technologies Inc. | System and method for receiving digital content |
| US8673848B2 (en) | 2012-01-27 | 2014-03-18 | Novartis Ag | Synthetic apelin mimetics for the treatment of heart failure |
| JP2009511063A (ja) * | 2005-10-14 | 2009-03-19 | アリーナ ファーマシューティカルズ, インコーポレイテッド | Gpr22およびそれに関連する方法 |
| US7998685B2 (en) * | 2005-11-10 | 2011-08-16 | Arena Pharmaceuticals, Inc. | Methods of identifying candidate compounds of the human G protein-coupled receptor, GPR50, as modulators of body mass or adiposity |
| HRP20120336T1 (hr) | 2007-03-22 | 2012-05-31 | Heptares Therapeutics Limited | Receptori vezani na mutacije g-proteina i metode njihovog odabira |
| GB0724051D0 (en) | 2007-12-08 | 2008-01-16 | Medical Res Council | Mutant proteins and methods for producing them |
| GB0724860D0 (en) | 2007-12-20 | 2008-01-30 | Heptares Therapeutics Ltd | Screening |
| GB0802474D0 (en) | 2008-02-11 | 2008-03-19 | Heptares Therapeutics Ltd | Mutant proteins and methods for selecting them |
| EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
| WO2010091692A2 (en) * | 2009-04-30 | 2010-08-19 | H. Lundbeck A/S | Constitutively active mutants and uses thereof |
| GB0910725D0 (en) | 2009-06-22 | 2009-08-05 | Heptares Therapeutics Ltd | Mutant proteins and methods for producing them |
| US8470980B2 (en) | 2009-09-09 | 2013-06-25 | Centrose, Llc | Extracellular targeted drug conjugates |
| BR112012026213B1 (pt) | 2010-04-15 | 2021-12-28 | Medimmune Limited | Compostos de pirrolobenzodiazepinas, conjugado das mesmas, composição farmacêutica compreendendo o conjugado e uso do mesmo para o tratamento de uma doença proliferativa |
| WO2011156328A1 (en) | 2010-06-08 | 2011-12-15 | Genentech, Inc. | Cysteine engineered antibodies and conjugates |
| JP5804341B2 (ja) * | 2010-08-06 | 2015-11-04 | 国立大学法人山口大学 | エストロゲン関連疾患の判定方法 |
| CN103313990B (zh) | 2010-11-17 | 2016-07-20 | 基因泰克公司 | 丙氨酰美登醇抗体偶联物 |
| US8679767B2 (en) | 2011-05-12 | 2014-03-25 | Genentech, Inc. | Multiple reaction monitoring LC-MS/MS method to detect therapeutic antibodies in animal samples using framework signature peptides |
| SG11201401406YA (en) | 2011-10-14 | 2014-05-29 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| WO2013130093A1 (en) | 2012-03-02 | 2013-09-06 | Genentech, Inc. | Biomarkers for treatment with anti-tubulin chemotherapeutic compounds |
| PT2906298T (pt) | 2012-10-12 | 2018-12-28 | Medimmune Ltd | Conjugados de pirrolobenzodiazepina-anticorpos |
| US10695433B2 (en) | 2012-10-12 | 2020-06-30 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
| WO2014057074A1 (en) | 2012-10-12 | 2014-04-17 | Spirogen Sàrl | Pyrrolobenzodiazepines and conjugates thereof |
| EP2906250B1 (en) | 2012-10-12 | 2018-05-30 | ADC Therapeutics SA | Pyrrolobenzodiazepine-anti-psma antibody conjugates |
| SI2906253T1 (sl) | 2012-10-12 | 2018-11-30 | Adc Therapeutics Sa | Konjugati pirolobenzodiazepin-protitelo proti PSMA |
| SMT201800346T1 (it) | 2012-10-12 | 2018-09-13 | Medimmune Ltd | Coniugati pirrolobenzodiazepina-anticorpo |
| WO2014057122A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sàrl | Pyrrolobenzodiazepine-anti-cd22 antibody conjugates |
| US8921307B2 (en) | 2012-11-20 | 2014-12-30 | Novartis Ag | Synthetic linear apelin mimetics for the treatment of heart failure |
| UY35144A (es) | 2012-11-20 | 2014-06-30 | Novartis Ag | Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca |
| CN110627797A (zh) | 2012-12-21 | 2019-12-31 | 麦迪穆有限责任公司 | 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 |
| JP6307519B2 (ja) | 2012-12-21 | 2018-04-04 | メドイミューン・リミテッドMedImmune Limited | ピロロベンゾジアゼピンおよびその結合体 |
| EP2968596B1 (en) | 2013-03-13 | 2019-03-06 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
| AU2014230735B2 (en) | 2013-03-13 | 2018-03-15 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
| JP6340019B2 (ja) | 2013-03-13 | 2018-06-06 | メドイミューン・リミテッドMedImmune Limited | ピロロベンゾジアゼピン及びそのコンジュゲート |
| BR112016001376A2 (pt) | 2013-07-25 | 2017-10-24 | Novartis Ag | bioconjugados de polipeptídeos de apelin sintéticos |
| BR112016001542A2 (pt) | 2013-07-25 | 2017-08-29 | Novartis Ag | Polipeptídios cíclicos para o tratamento de insuficiência cardíaca |
| US10442836B2 (en) | 2013-08-12 | 2019-10-15 | Genentech, Inc. | 1-(chloromethyl)-2,3-dihydro-1H-benzo[E]indole dimer antibody-drug conjugate compounds, and methods of use and treatment |
| US10010624B2 (en) | 2013-10-11 | 2018-07-03 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
| GB201317982D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| EP3054985B1 (en) | 2013-10-11 | 2018-12-26 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
| WO2015052535A1 (en) | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| RU2689388C1 (ru) | 2013-12-16 | 2019-05-28 | Дженентек, Инк. | Пептидомиметические соединения и их конъюгаты антител с лекарственными средствами |
| EA201691023A1 (ru) | 2013-12-16 | 2016-10-31 | Дженентек, Инк. | Пептидомиметические соединения и их конъюгаты антитела с лекарственным средством |
| JP6980384B2 (ja) | 2013-12-16 | 2021-12-15 | ジェネンテック, インコーポレイテッド | 1−(クロロメチル)−2,3−ジヒドロ−1h−ベンゾ[e]インドール二量体抗体−薬物コンジュゲート化合物、並びに使用及び処置の方法 |
| CA2945706C (en) | 2014-04-25 | 2023-10-24 | Libramen Naturals Inc. | G-protein coupled receptor 22 transformed cell lines and uses therefor |
| US10188746B2 (en) | 2014-09-10 | 2019-01-29 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
| GB201416112D0 (en) | 2014-09-12 | 2014-10-29 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
| MX2017003123A (es) | 2014-09-12 | 2017-05-12 | Genentech Inc | Anticuerpos y conjugados modificados geneticamente con cisteina. |
| JP6622293B2 (ja) | 2014-09-12 | 2019-12-18 | ジェネンテック, インコーポレイテッド | アントラサイクリンジスルフィド中間体、抗体−薬物複合体、及び方法 |
| AU2015317653A1 (en) | 2014-09-17 | 2017-04-06 | Genentech, Inc. | Pyrrolobenzodiazepines and antibody disulfide conjugates thereof |
| US10780096B2 (en) | 2014-11-25 | 2020-09-22 | Adc Therapeutics Sa | Pyrrolobenzodiazepine-antibody conjugates |
| JP6752204B2 (ja) | 2014-12-03 | 2020-09-09 | ジェネンテック, インコーポレイテッド | 四級アミン化合物及びその抗体−薬物コンジュゲート |
| GB201506402D0 (en) | 2015-04-15 | 2015-05-27 | Berkel Patricius H C Van And Howard Philip W | Site-specific antibody-drug conjugates |
| GB201506411D0 (en) | 2015-04-15 | 2015-05-27 | Bergenbio As | Humanized anti-axl antibodies |
| MA43345A (fr) | 2015-10-02 | 2018-08-08 | Hoffmann La Roche | Conjugués anticorps-médicaments de pyrrolobenzodiazépine et méthodes d'utilisation |
| MA43354A (fr) | 2015-10-16 | 2018-08-22 | Genentech Inc | Conjugués médicamenteux à pont disulfure encombré |
| MA45326A (fr) | 2015-10-20 | 2018-08-29 | Genentech Inc | Conjugués calichéamicine-anticorps-médicament et procédés d'utilisation |
| GB201601431D0 (en) | 2016-01-26 | 2016-03-09 | Medimmune Ltd | Pyrrolobenzodiazepines |
| GB201602356D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
| GB201602359D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
| EP3416640A1 (en) | 2016-02-16 | 2018-12-26 | Deutsches Krebsforschungszentrum Stiftung des Öffentlichen Rechts | Modulators of tumor immune resistance for the treatment of cancer |
| EP3416641A1 (en) | 2016-02-16 | 2018-12-26 | Deutsches Krebsforschungszentrum Stiftung des Öffentlichen Rechts | Modulators of ccr9 for treating tumor resistance to immune responses |
| US20170315132A1 (en) | 2016-03-25 | 2017-11-02 | Genentech, Inc. | Multiplexed total antibody and antibody-conjugated drug quantification assay |
| GB201607478D0 (en) | 2016-04-29 | 2016-06-15 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
| ES2858151T3 (es) | 2016-05-20 | 2021-09-29 | Hoffmann La Roche | Conjugados de PROTAC-anticuerpo y procedimientos de uso |
| US20170370906A1 (en) | 2016-05-27 | 2017-12-28 | Genentech, Inc. | Bioanalytical analysis of site-specific antibody drug conjugates |
| EP3464280B1 (en) | 2016-06-06 | 2021-10-06 | F. Hoffmann-La Roche AG | Silvestrol antibody-drug conjugates and methods of use |
| WO2018031662A1 (en) | 2016-08-11 | 2018-02-15 | Genentech, Inc. | Pyrrolobenzodiazepine prodrugs and antibody conjugates thereof |
| CN110139674B (zh) | 2016-10-05 | 2023-05-16 | 豪夫迈·罗氏有限公司 | 制备抗体药物缀合物的方法 |
| GB201617466D0 (en) | 2016-10-14 | 2016-11-30 | Medimmune Ltd | Pyrrolobenzodiazepine conjugates |
| ES2871001T3 (es) | 2017-02-08 | 2021-10-28 | Adc Therapeutics Sa | Conjugados de pirrolobenzodiazepinas y anticuerpos |
| GB201702031D0 (en) | 2017-02-08 | 2017-03-22 | Medlmmune Ltd | Pyrrolobenzodiazepine-antibody conjugates |
| WO2018192944A1 (en) | 2017-04-18 | 2018-10-25 | Medimmune Limited | Pyrrolobenzodiazepine conjugates |
| CA3057748A1 (en) | 2017-04-20 | 2018-10-25 | Adc Therapeutics Sa | Combination therapy with an anti-axl antibody-drug conjugate |
| ES2988683T3 (es) | 2017-06-14 | 2024-11-21 | Adc Therapeutics Sa | Pautas posológicas para la administración de un CAF anti-CD19 |
| SG11202000358YA (en) | 2017-08-18 | 2020-02-27 | Medimmune Ltd | Pyrrolobenzodiazepine conjugates |
| KR20220156974A (ko) | 2017-09-20 | 2022-11-28 | 주식회사 피에이치파마 | 타일란스타틴 유사체 |
| 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 |
| CN119752801A (zh) * | 2018-08-01 | 2025-04-04 | 南克维斯特公司 | 用于免疫疗法的基因修饰的包含归巢受体或细胞因子和嵌合抗原受体的四顺反子系统 |
| GB201814281D0 (en) | 2018-09-03 | 2018-10-17 | Femtogenix Ltd | Cytotoxic agents |
| EP3870235A1 (en) | 2018-10-24 | 2021-09-01 | F. Hoffmann-La Roche AG | Conjugated chemical inducers of degradation and methods of use |
| EP3894427A1 (en) | 2018-12-10 | 2021-10-20 | Genentech, Inc. | Photocrosslinking peptides for site specific conjugation to fc-containing proteins |
| GB201901197D0 (en) | 2019-01-29 | 2019-03-20 | Femtogenix Ltd | G-A Crosslinking cytotoxic agents |
| MX2021010477A (es) | 2019-03-15 | 2021-10-01 | Medimmune Ltd | Dimeros de azetidobenzodiazepina y conjugados que los comprenden para uso en el tratamiento de cancer. |
| US11230699B2 (en) | 2020-01-28 | 2022-01-25 | Immunitybio, Inc. | Chimeric antigen receptor-modified NK-92 cells targeting EGFR super-family receptors |
| GB2597532A (en) | 2020-07-28 | 2022-02-02 | Femtogenix Ltd | Cytotoxic compounds |
| WO2022078524A2 (en) | 2021-11-03 | 2022-04-21 | Hangzhou Dac Biotech Co., Ltd. | Specific conjugation of an antibody |
| CN114848822A (zh) * | 2022-06-01 | 2022-08-05 | 合肥工业大学 | Gpr31抑制剂在制备预防和治疗血管钙化药物中的应用 |
| WO2024044659A1 (en) * | 2022-08-24 | 2024-02-29 | Tectonic Therapeutic, Inc. | Constitutively active g protein-coupled receptor compositions and methods of use thereof |
| EP4637833A2 (en) | 2022-12-23 | 2025-10-29 | Genentech, Inc. | Cereblon degrader conjugates, and uses thereof |
| WO2024220546A2 (en) | 2023-04-17 | 2024-10-24 | Peak Bio, Inc. | Antibodies and antibody-drug conjugates and methods of use and synthetic processes and intermediates |
| WO2025207642A1 (en) * | 2024-03-25 | 2025-10-02 | Seattle Children's Hospital D/B/A Seattle Children's Research Institute | Cxcr3 isoforms to improve recombinant receptor trafficking |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU7492291A (en) | 1990-02-26 | 1991-09-18 | Board Of Trustees Of The Leland Stanford Junior University | Identification and expression of insect steroid receptor dna sequences |
| DE69232876D1 (de) | 1991-10-01 | 2003-01-30 | Us Gov Health & Human Serv | Ein verfahren zur identifikation von liganden und ligandantagonisten |
| AU685054C (en) * | 1992-05-14 | 2003-02-27 | Baylor College Of Medicine | Mutated steroid hormone receptors, methods for their use and molecular switch for gene therapy |
| AU677968B2 (en) | 1992-09-25 | 1997-05-15 | H. Lundbeck A/S | DNA encoding human alpha 1 adrenergic receptors and uses thereof |
| EP0612845A3 (en) | 1993-02-26 | 1994-09-21 | American Cyanamid Co | Purified opioid receptor. |
| AU1173995A (en) | 1993-11-10 | 1995-05-29 | Arch Development Corporation | Ubiquitous nuclear receptor: compositions and methods |
| EP0743520A3 (en) * | 1993-12-30 | 1999-11-10 | The Salk Institute For Biological Studies | Novel uses for GAL4-receptor constructs |
| US5573944A (en) | 1994-07-22 | 1996-11-12 | President And Fellows Of Harvard College | Yeast cell expressing heterologous receptor kinase |
| US6114139A (en) | 1994-08-11 | 2000-09-05 | Takeda Chemical Industries, Ltd. | G-protein coupled receptor protein and a DNA encoding the receptor |
| CA2135253A1 (en) | 1994-11-07 | 1996-05-08 | Michael Dennis | Compound screening based on a window of chemical-messenger-independent activity |
| WO1996039442A1 (en) * | 1995-06-06 | 1996-12-12 | Human Genome Sciences, Inc. | G-protein receptor htnad29 |
| WO1997011159A1 (en) | 1995-09-20 | 1997-03-27 | Molecular Geriatrics Corporation | Yeast receptor and g-protein fusion protein |
| FR2742033B1 (fr) * | 1995-12-08 | 1998-01-16 | Achart Jacques | Appareil pour l'ouverture de coquillages de mollusques bivalves |
| US5750353A (en) | 1995-12-11 | 1998-05-12 | New England Medical Center Hospitals, Inc. | Assay for non-peptide agonists to peptide hormone receptors |
| EP0869975B1 (en) | 1995-12-11 | 2007-08-15 | New England Medical Center Hospitals, Inc. | Assay for and uses of peptide hormone receptor ligands |
| US5932779A (en) * | 1996-06-10 | 1999-08-03 | Millennium Pharmaceuticals, Inc. | Screening methods for compounds useful in the regulation of body weight |
| AU3648297A (en) | 1996-07-02 | 1998-01-21 | President And Fellows Of Harvard College | Receptor tyrosine phosphatase, and uses related thereto |
| WO1998013513A2 (en) * | 1996-09-24 | 1998-04-02 | Cadus Pharmaceutical Corporation | Methods and compositions for identifying receptor effectors |
| EP0960125A4 (en) | 1996-12-27 | 2002-09-25 | Merck & Co Inc | GALANIN RECEPTOR GalR2 AND NUCLEOTIDES ENCODING SAME |
| US6403305B1 (en) | 1997-02-06 | 2002-06-11 | Cornell Research Foundation, Inc. | Methods of identifying peptide agonists or negative antagonists of a G protein coupled receptor |
| WO1998038217A1 (en) | 1997-02-27 | 1998-09-03 | Milt Teitler | Constitutively activated serotonin receptors |
| US6555339B1 (en) * | 1997-04-14 | 2003-04-29 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human protein-coupled receptors |
| AU743259B2 (en) | 1997-04-14 | 2002-01-24 | Arena Pharmaceuticals, Inc. | A method of identifying modulators of cell surface membrane receptors useful in the treatment of disease |
| US5891720A (en) | 1997-04-17 | 1999-04-06 | Millennium Pharmaceuticals, Inc. | Isolated DNA encoding a novel human G-protein coupled receptor |
| EP0878542A3 (en) | 1997-04-22 | 2000-04-19 | Smithkline Beecham Corporation | cDNA clone HMTMF81 that encodes a novel human 7-transmembrane receptor |
| JP2002508660A (ja) | 1997-06-12 | 2002-03-19 | スミスクライン ビーチャム コーポレーション | Hm74a受容体 |
| US5955308A (en) | 1997-06-18 | 1999-09-21 | Smithkline Beecham Corporation | cDNA clone HEAOD54 that encodes a human 7-transmembrane receptor |
| US6222029B1 (en) | 1997-08-01 | 2001-04-24 | Genset | 5′ ESTs for secreted proteins expressed in brain |
| WO1999024569A1 (fr) | 1997-11-11 | 1999-05-20 | Ono Pharmaceutical Co., Ltd. | Recepteur d'acide lysophosphatidique humain et utilisation dudit recepteur |
| SE9704836D0 (sv) | 1997-12-22 | 1997-12-22 | Astra Pharma Inc | Novel receptor |
| DE69941330D1 (de) | 1998-03-26 | 2009-10-08 | Univ R | Neue g-protein-gekoppelte rezeptoren aus säugetieren mit extrazellulären leucin-reicher region |
| US6107324A (en) | 1998-04-14 | 2000-08-22 | Arena Pharmaceuticals Inc. | 5-HT2A receptor inverse agonists |
| AU751080B2 (en) * | 1998-07-31 | 2002-08-08 | Arena Pharmaceuticals, Inc. | Endogenous constitutively activated G protein-coupled orphan receptors |
| US6777204B1 (en) | 1998-09-03 | 2004-08-17 | Asahi Kasei Kabushiki Kaisha | Receptor protein and method for diagnosing inflammatory diseases by using the same |
| NZ510712A (en) | 1998-10-13 | 2004-11-26 | Arena Pharm Inc | Non-endogenous, constitutively activated human G protein-coupled receptors |
| US20030229216A1 (en) * | 1998-10-13 | 2003-12-11 | Ruoping Chen | Constitutively activated human G protein coupled receptors |
| CN1341123A (zh) | 1999-02-19 | 2002-03-20 | 武田药品工业株式会社 | 新型g蛋白偶联型受体蛋白及其dna |
| AU764310B2 (en) | 1999-07-15 | 2003-08-14 | Solvay Pharmaceuticals B.V. | Human G-protein coupled receptor |
| WO2001007606A1 (en) | 1999-07-27 | 2001-02-01 | Smithkline Beecham Plc | Axor21, a g-protein coupled receptor |
| CA2381979A1 (en) | 1999-08-17 | 2001-02-22 | Klaus Ducker | Pgpcr-3 polypeptides and dna sequences thereof |
| WO2001014577A1 (en) | 1999-08-24 | 2001-03-01 | Smithkline Beecham Corporation | Molecular cloning of a galanin like 7tm receptor (axor40) |
| WO2001016159A1 (en) | 1999-08-27 | 2001-03-08 | Smithkline Beecham Corporation | Gpcr, theant |
| GB9923889D0 (en) | 1999-10-08 | 1999-12-08 | Pfizer Ltd | Novel polypeptide |
| GB9924951D0 (en) | 1999-10-21 | 1999-12-22 | Pfizer Ltd | Novel polypeptide |
| CA2386509A1 (en) | 1999-10-27 | 2001-05-03 | Pharmacia & Upjohn Company | G protein-coupled receptors expressed in human brain |
| AU782959B2 (en) | 1999-11-17 | 2005-09-15 | Arena Pharmaceuticals, Inc. | Endogenous and non-endogenous versions of human G protein-coupled receptors |
-
1998
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- 1999-10-12 WO PCT/US1999/023938 patent/WO2000022129A1/en not_active Ceased
-
2001
- 2001-03-12 IL IL141965A patent/IL141965A/en not_active IP Right Cessation
-
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- 2002-09-20 US US10/251,385 patent/US7410777B2/en not_active Expired - Fee Related
-
2004
- 2004-07-08 AU AU2004203102A patent/AU2004203102B2/en not_active Ceased
-
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- 2008-01-16 AU AU2008200231A patent/AU2008200231A1/en not_active Abandoned
-
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- 2011-02-07 AU AU2011200511A patent/AU2011200511A1/en not_active Abandoned
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