PT1778718E - Inibidores de iap - Google Patents

Inibidores de iap Download PDF

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Publication number
PT1778718E
PT1778718E PT57683047T PT05768304T PT1778718E PT 1778718 E PT1778718 E PT 1778718E PT 57683047 T PT57683047 T PT 57683047T PT 05768304 T PT05768304 T PT 05768304T PT 1778718 E PT1778718 E PT 1778718E
Authority
PT
Portugal
Prior art keywords
alkyl
amino
aryl
mmol
cycloalkyl
Prior art date
Application number
PT57683047T
Other languages
English (en)
Portuguese (pt)
Inventor
Frederick Cohen
Kurt Deshayes
Wayne J Fairbrother
Bainian Feng
John Flygare
Lewis J Gazzard
Vickie Hsiao-Wei Tsui
Original Assignee
Genentech Inc
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 Genentech Inc filed Critical Genentech Inc
Publication of PT1778718E publication Critical patent/PT1778718E/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/177—Receptors; Cell surface antigens; Cell surface determinants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N5/00—Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
    • C12N5/06—Animal cells or tissues; Human cells or tissues
    • C12N5/0602—Vertebrate cells
    • C12N5/0693—Tumour cells; Cancer cells

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Wood Science & Technology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Steroid Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PT57683047T 2004-07-02 2005-07-05 Inibidores de iap PT1778718E (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US58550104P 2004-07-02 2004-07-02

Publications (1)

Publication Number Publication Date
PT1778718E true PT1778718E (pt) 2014-12-03

Family

ID=35311854

Family Applications (1)

Application Number Title Priority Date Filing Date
PT57683047T PT1778718E (pt) 2004-07-02 2005-07-05 Inibidores de iap

Country Status (21)

Country Link
US (4) US7244851B2 (enExample)
EP (1) EP1778718B1 (enExample)
JP (3) JP4850175B2 (enExample)
KR (2) KR100984459B1 (enExample)
CN (1) CN101035802A (enExample)
AU (2) AU2005270104A1 (enExample)
BR (1) BRPI0511350A (enExample)
CA (1) CA2570321C (enExample)
DK (1) DK1778718T3 (enExample)
ES (1) ES2524449T3 (enExample)
IL (1) IL179854A (enExample)
MX (1) MXPA06014969A (enExample)
NO (1) NO341816B1 (enExample)
NZ (1) NZ588799A (enExample)
PL (1) PL1778718T3 (enExample)
PT (1) PT1778718E (enExample)
RS (1) RS53734B1 (enExample)
RU (1) RU2401840C2 (enExample)
SI (1) SI1778718T1 (enExample)
WO (1) WO2006014361A1 (enExample)
ZA (1) ZA200700032B (enExample)

Families Citing this family (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7646707B2 (en) * 2003-12-23 2010-01-12 At&T Intellectual Property I, L.P. Method and system for automatically renaming logical circuit identifiers for rerouted logical circuits in a data network
EP1715882A4 (en) * 2004-01-16 2009-04-08 Univ Michigan SMAC-PEPTIDOMIMETIKA AND ITS USES
BRPI0506883A (pt) * 2004-01-16 2007-05-29 Univ Michigan miméticos de smac conformacionalmente comprimidos e seus usos
DK2253614T3 (da) 2004-04-07 2013-01-07 Novartis Ag IAP-inhibitorer
KR100984459B1 (ko) 2004-07-02 2010-09-29 제넨테크, 인크. Ｉａｐ의 억제제
WO2006010118A2 (en) * 2004-07-09 2006-01-26 The Regents Of The University Of Michigan Conformationally constrained smac mimetics and the uses thereof
CA2573644A1 (en) * 2004-07-12 2006-02-16 Idun Pharmaceuticals, Inc. Tetrapeptide analogs
ES2475207T3 (es) 2004-07-15 2014-07-10 Tetralogic Pharmaceuticals Corporation Compuestos de unión a IAP
DK1836201T4 (da) 2004-12-20 2013-11-11 Genentech Inc Pyrrolidininhibitorer af IAP.
MX2007010371A (es) 2005-02-25 2008-01-11 Tetralogic Pharmaceuticals Inhibidores dimericos iap.
JP4954983B2 (ja) 2005-05-18 2012-06-20 ファーマサイエンス・インコーポレイテッド Ｂｉｒドメイン結合化合物
CA2617642A1 (en) * 2005-08-09 2007-02-22 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
US20100256046A1 (en) * 2009-04-03 2010-10-07 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
WO2007048224A1 (en) * 2005-10-25 2007-05-03 Aegera Therapeutics Inc. Iap bir domain binding compounds
CN101374829A (zh) * 2005-12-19 2009-02-25 健泰科生物技术公司 Iap的抑制剂
TWI504597B (zh) * 2006-03-16 2015-10-21 Pharmascience Inc 結合於細胞凋亡抑制蛋白（ｉａｐ）之桿狀病毒ｉａｐ重複序列（ｂｉｒ）區域之化合物
CN101535300B (zh) 2006-05-16 2014-05-28 埃格拉医疗公司 Iap bir域结合化合物
WO2008014240A2 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100143499A1 (en) * 2006-07-24 2010-06-10 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
JP5452223B2 (ja) 2006-07-24 2014-03-26 テトラロジック ファーマシューティカルズ コーポレーション Ｉａｐ阻害剤
US20100056495A1 (en) * 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
WO2008014229A2 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
MX2009000824A (es) * 2006-07-24 2009-02-04 Tetralogic Pharmaceuticals Cor Antagonistas dimericos de las proteinas inhibidoras de la apoptosis.
PE20110220A1 (es) 2006-08-02 2011-04-11 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS
MX2009002019A (es) * 2006-08-24 2009-03-09 Novartis Ag Derivados de 2-(pirazin-2-il)-tiazol y 2-(1h-pirazol-3-il)-tiazol asi como compuestos relacionados como inhibidores de la estearoil-coa-desaturasa (scd) para el tratamiento de trastornos metabolicos, cardiovasculares, y otros.
CA2662574A1 (en) * 2006-09-22 2008-03-27 Novartis Ag Heterocyclic organic compounds
WO2008045905A1 (en) * 2006-10-12 2008-04-17 Novartis Ag Pyrrolydine derivatives as iap inhibitors
NZ577150A (en) * 2006-12-19 2012-04-27 Genentech Inc Imidazopyridine inhibitors of iap
WO2008074835A1 (en) * 2006-12-20 2008-06-26 Novartis Ag 2-substituted 5-membered heterocycles as scd inhibitors
JP5454943B2 (ja) * 2007-04-12 2014-03-26 ジョイアント ファーマスーティカルズ、インク． 抗癌剤として有用なｓｍａｃ模倣二量体及び三量体
WO2008134679A1 (en) * 2007-04-30 2008-11-06 Genentech, Inc. Inhibitors of iap
JP2010528587A (ja) * 2007-05-07 2010-08-26 テトラロジック ファーマシューティカルズ コーポレーション アポトーシス阻害タンパク質のアンタゴニストに対する感受性のバイオマーカーとしてＴＮＦα遺伝子の発現を用いる方法
US20100203012A1 (en) * 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
AU2009203971A1 (en) * 2008-01-11 2009-07-16 Genentech, Inc. Inhibitors of IAP
WO2009136290A1 (en) * 2008-05-05 2009-11-12 Aegera Therapeutics, Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
AU2009261919A1 (en) * 2008-06-27 2009-12-30 Pharmascience Inc. Bridged secondary amines and use thereof as IAP BIR domain binding compounds
JP2011529962A (ja) * 2008-08-02 2011-12-15 ジェネンテック， インコーポレイテッド Ｉａｐのインヒビター
US20110218211A1 (en) * 2008-08-16 2011-09-08 Genentech, Inc. Azaindole inhibitors of iap
WO2010033531A1 (en) 2008-09-17 2010-03-25 Tetralogic Pharmaceuticals Corp. Iap inhibitors
FR2939073B1 (fr) 2008-12-03 2010-12-31 Sidel Participations Formage des recipients avec contre-pression localisee
US20100317593A1 (en) * 2009-06-12 2010-12-16 Astrazeneca Ab 2,3-dihydro-1h-indene compounds
US8283372B2 (en) 2009-07-02 2012-10-09 Tetralogic Pharmaceuticals Corp. 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic
EP2478358A1 (en) 2009-09-18 2012-07-25 Novartis AG Biomarkers for iap inhibitor compounds
US8551955B2 (en) 2009-10-28 2013-10-08 Joyant Pharmaceuticals, Inc. Dimeric Smac mimetics
CN102050867A (zh) * 2009-11-10 2011-05-11 上海艾力斯医药科技有限公司 四肽类似物、制备方法及其应用
US9284350B2 (en) * 2010-02-12 2016-03-15 Pharmascience Inc. IAP BIR domain binding compounds
EP2558458B1 (de) 2010-04-16 2017-09-06 Bayer Intellectual Property GmbH Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
WO2013043591A1 (en) * 2011-09-21 2013-03-28 Albert Einstein College Of Medicine Of Yeshiva University Combination therapy for cancer
US20140243276A1 (en) 2011-09-30 2014-08-28 Tetralogic Pharmaceuticals Corporation Smac mimetic (birinapant) for use in the treatment of proliferative diseases (cancer)
NO2755614T3 (enExample) 2012-01-03 2018-03-31
US9353419B2 (en) 2012-05-04 2016-05-31 Novartis Ag Biomarkers for IAP inhibitor therapy
US9546174B2 (en) 2012-11-30 2017-01-17 Sanford-Burnham Medical Research Institute Inhibitor of apoptosis protein (IAP) antagonists
US9498532B2 (en) 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
ES2701051T3 (es) 2013-03-15 2019-02-20 Novartis Ag Conjugados de anticuerpo-fármaco
KR20160030099A (ko) 2013-06-25 2016-03-16 더 월터 앤드 엘리자 홀 인스티튜트 오브 메디컬 리서치 세포내 감염의 치료 방법
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
BR122022015241B1 (pt) 2013-12-20 2023-09-26 Astex Therapeutics Limited Compostos heterocíclicos bicíclicos intermediários para a preparação de um composto de fórmula (i)
WO2015109391A1 (en) 2014-01-24 2015-07-30 Children's Hospital Of Eastern Ontario Research Institute Inc. Smc combination therapy for the treatment of cancer
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2015168835A1 (en) * 2014-05-05 2015-11-12 Empire Technology Development Llc Composite task processor
JP6768522B2 (ja) 2014-06-04 2020-10-14 サンフォード−バーンハム メディカル リサーチ インスティテュート Ｈｉｖ治療におけるアポトーシスタンパク質阻害剤（ｉａｐ）のアンタゴニストの使用
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
MA40513A (fr) 2014-08-12 2017-06-21 Novartis Ag Conjugués médicament-anticorps anti-cdh6
GB201414730D0 (en) * 2014-08-19 2014-10-01 Tpp Global Dev Ltd Pharmaceutical compound
WO2016079527A1 (en) 2014-11-19 2016-05-26 Tetralogic Birinapant Uk Ltd Combination therapy
WO2016097773A1 (en) 2014-12-19 2016-06-23 Children's Cancer Institute Therapeutic iap antagonists for treating proliferative disorders
JP6817962B2 (ja) 2015-01-20 2021-01-20 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． ターゲティングされたアンドロゲン受容体分解のための化合物および方法
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
US20190194315A1 (en) 2015-06-17 2019-06-27 Novartis Ag Antibody drug conjugates
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3368092B9 (en) 2015-10-29 2020-07-29 Novartis AG Antibody conjugates comprising toll-like receptor agonist
PL3472149T3 (pl) 2016-06-21 2024-02-12 Orion Ophthalmology LLC Heterocykliczne pochodne prolinamidu
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
BR112019011200B1 (pt) 2016-12-01 2021-12-28 Arvinas Operations, Inc Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
JP2020505327A (ja) 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． Ｅｇｆｒタンパク質分解標的化キメラ分子およびその関連する使用方法
KR20250117470A (ko) 2016-12-23 2025-08-04 아비나스 오퍼레이션스, 인코포레이티드 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
BR112019015312A2 (pt) 2017-01-26 2020-03-10 Arvinas Operations, Inc. Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados
JOP20190187A1 (ar) 2017-02-03 2019-08-01 Novartis Ag مترافقات عقار جسم مضاد لـ ccr7
WO2018163051A1 (en) 2017-03-06 2018-09-13 Novartis Ag Methods of treatment of cancer with reduced ubb expression
WO2018185618A1 (en) 2017-04-03 2018-10-11 Novartis Ag Anti-cdh6 antibody drug conjugates and anti-gitr antibody combinations and methods of treatment
AR111651A1 (es) 2017-04-28 2019-08-07 Novartis Ag Conjugados de anticuerpos que comprenden agonistas del receptor de tipo toll y terapias de combinación
MY206158A (en) 2017-05-24 2024-12-02 Novartis Ag Antibody-cytokine engrafted proteins and methods of use in the treatment of cancer
WO2018215938A1 (en) 2017-05-24 2018-11-29 Novartis Ag Antibody-cytokine engrafted proteins and methods of use
WO2018215937A1 (en) 2017-05-24 2018-11-29 Novartis Ag Interleukin-7 antibody cytokine engrafted proteins and methods of use in the treatment of cancer
BR112020009369A2 (pt) 2017-11-13 2020-10-13 Chia Tai Tianqing Pharmaceutical Group Co., Ltd miméticos de smac usados como inibidores de iap e seus usos
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
JP7161849B2 (ja) * 2018-01-24 2022-10-27 株式会社クラレ 第一級アミンの製造方法
CN111655713B (zh) * 2018-02-09 2023-06-27 广东东阳光药业有限公司 Iap抑制剂及其在药物中的应用
WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
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
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
WO2020023851A1 (en) 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
JP7297053B2 (ja) 2018-08-20 2023-06-23 アルビナス・オペレーションズ・インコーポレイテッド 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解
IL281188B2 (en) 2018-09-07 2025-08-01 Arvinas Operations Inc Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
US20230053449A1 (en) 2018-10-31 2023-02-23 Novartis Ag Dc-sign antibody drug conjugates
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
KR20210107731A (ko) 2018-12-21 2021-09-01 노파르티스 아게 Pmel17에 대한 항체 및 이의 접합체
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
EP3936126A4 (en) * 2019-03-07 2022-12-21 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. COMBINATION OF IAP INHIBITOR AND IMMUNOCHECK POINT INHIBITOR
KR20220006611A (ko) * 2019-05-10 2022-01-17 치아타이 티안큉 파마수티컬 그룹 주식회사 Iap 억제제로서의 smac 모방물의 결정 및 그 제조방법
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
EP4007592A1 (en) 2019-08-02 2022-06-08 LanthioPep B.V. Angiotensin type 2 (at2) receptor agonists for use in the treatment of cancer
KR20220054347A (ko) 2019-08-26 2022-05-02 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 유도체로 유방암을 치료하는 방법
BR112022011902A2 (pt) 2019-12-20 2022-09-06 Novartis Ag Terapias de combinação
WO2021148396A1 (en) 2020-01-20 2021-07-29 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
CN111205232B (zh) * 2020-02-26 2022-07-01 浙江天宇药业股份有限公司 一种替格瑞洛中间体的合成方法
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
JP2023529211A (ja) 2020-06-11 2023-07-07 ノバルティス アーゲー Ｚｂｔｂ３２阻害剤及びその使用
KR20230027056A (ko) 2020-06-23 2023-02-27 노파르티스 아게 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법
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
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
WO2022056368A1 (en) 2020-09-14 2022-03-17 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
BR112023021475A2 (pt) 2021-04-16 2023-12-19 Novartis Ag Conjugados anticorpo-fármaco e métodos para produzir os mesmos
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación
WO2023214325A1 (en) 2022-05-05 2023-11-09 Novartis Ag Pyrazolopyrimidine derivatives and uses thereof as tet2 inhibitors
AU2023314354A1 (en) 2022-07-26 2024-11-21 Novartis Ag Crystalline forms of an akr1c3 dependent kars inhibitor
WO2024054591A1 (en) 2022-09-07 2024-03-14 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
US12448399B2 (en) 2023-01-26 2025-10-21 Arvinas Operations, Inc. Cereblon-based KRAS degrading PROTACs and uses related thereto

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE430062B (sv) * 1977-03-04 1983-10-17 Pharmacia Fine Chemicals Ab Kopplings- eller tioleringsreagens
DE2714880A1 (de) 1977-04-02 1978-10-26 Hoechst Ag Cephemderivate und verfahren zu ihrer herstellung
FR2575753B1 (fr) 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA1292840C (en) * 1985-09-26 1991-12-03 David Harry Hawke Sequencing of peptides
US4935494A (en) * 1988-11-15 1990-06-19 City Of Hope C-terminal peptide and protein sequencing
DK167813B1 (da) 1989-12-07 1993-12-20 Carlbiotech Ltd As Pentapeptidderivat, farmaceutisk acceptable salte heraf, fremgangsmaade til fremstilling deraf og farmaceutisk praeparat indeholdende et saadant derivat
WO1992001938A1 (en) 1990-07-20 1992-02-06 City Of Hope Derivatization of c-terminal proline
DK0752248T3 (da) 1992-11-13 2000-11-13 Idec Pharma Corp Terapeutisk anvendelse af kimæriske og radioaktivt mærkede antistoffer mod humant B-lymfocytbegrænset differentieringsantig
US5559209A (en) 1993-02-18 1996-09-24 The General Hospital Corporation Regulator regions of G proteins
TWI243828B (en) * 1998-03-19 2005-11-21 Vertex Pharma Inhibitors of caspases
US6335155B1 (en) 1998-06-26 2002-01-01 Sunesis Pharmaceuticals, Inc. Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
US6472172B1 (en) 1998-07-31 2002-10-29 Schering Aktiengesellschaft DNA encoding a novel human inhibitor-of-apoptosis protein
CA2355215A1 (en) 1998-12-28 2000-07-06 Jim Wells Identifying small organic molecule ligands for binding
US6608026B1 (en) 2000-08-23 2003-08-19 Board Of Regents, The University Of Texas System Apoptotic compounds
WO2002016418A2 (en) 2000-08-24 2002-02-28 Thomas Jefferson University An iap binding peptide or polypeptide and methods of using the same
WO2004007529A2 (en) 2002-07-15 2004-01-22 The Trustees Of Princeton University Iap binding compounds
AU2001293189A1 (en) 2000-09-29 2002-04-08 Trustees Of Princeton University Compositions and methods for regulating apoptosis
US6992063B2 (en) 2000-09-29 2006-01-31 The Trustees Of Princeton University Compositions and method for regulating apoptosis
WO2002030959A2 (en) 2000-10-13 2002-04-18 Abbott Laboratories Peptides derived from smac (diablo) and methods of use therefor
AU2002253908A1 (en) 2001-02-08 2003-02-17 Thomas Jefferson University A conserved xiap-interaction motif in caspase-9 and smac/diablo for mediating apoptosis
JP2004531731A (ja) 2001-05-31 2004-10-14 ザ トラスティーズ オブ プリンストン ユニバーシテイ Ｉａｐ結合ペプチドおよびｉａｐに結合する化合物を同定するアッセイ
WO2003040172A2 (en) 2001-11-09 2003-05-15 Aegera Therapeutics, Inc. Methods and reagents for peptide-bir interaction screens
EP1495124A2 (en) 2002-04-17 2005-01-12 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Smac-peptides as therapeutics against cancer and autoimmune diseases
WO2004005248A1 (en) 2002-07-02 2004-01-15 Novartis Ag Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
WO2004017991A1 (en) 2002-08-13 2004-03-04 Cell Center Cologne Gmbh Use of iap for the diagnosis and of iap-inhibitors for the treatment of hodgkin’s lymphomas
JP4315249B2 (ja) 2003-02-07 2009-08-19 ジェネンテック・インコーポレーテッド アポトーシス亢進のための組成物と方法
US20040171554A1 (en) * 2003-02-07 2004-09-02 Genentech, Inc. Compositions and methods for enhancing apoptosis
IL156263A0 (en) 2003-06-02 2004-01-04 Hadasit Med Res Service Livin-derived peptides, compositions and uses thereof
CA2543897A1 (en) 2003-11-13 2005-06-02 Genentech, Inc. Compositions and methods for screening pro-apoptotic compounds
DK2253614T3 (da) 2004-04-07 2013-01-07 Novartis Ag IAP-inhibitorer
KR100984459B1 (ko) * 2004-07-02 2010-09-29 제넨테크, 인크. Ｉａｐ의 억제제
ES2475207T3 (es) 2004-07-15 2014-07-10 Tetralogic Pharmaceuticals Corporation Compuestos de unión a IAP

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