AU2005270104A1 - Inhibitors of IAP - Google Patents

Inhibitors of IAP Download PDF

Info

Publication number
AU2005270104A1
AU2005270104A1 AU2005270104A AU2005270104A AU2005270104A1 AU 2005270104 A1 AU2005270104 A1 AU 2005270104A1 AU 2005270104 A AU2005270104 A AU 2005270104A AU 2005270104 A AU2005270104 A AU 2005270104A AU 2005270104 A1 AU2005270104 A1 AU 2005270104A1
Authority
AU
Australia
Prior art keywords
alkyl
amino
aryl
compound
cycloalkyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
AU2005270104A
Other languages
English (en)
Inventor
Frederick Cohen
Kurt Deshayes
Wayne J. Fairbrother
Bainian Feng
John Flygare
Lewis J. Gazzard
Vickie Hsiao-Wei Tsui
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
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 AU2005270104A1 publication Critical patent/AU2005270104A1/en
Priority to AU2009243421A priority Critical patent/AU2009243421B2/en
Abandoned legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/177Receptors; Cell surface antigens; Cell surface determinants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N5/00Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
    • C12N5/06Animal cells or tissues; Human cells or tissues
    • C12N5/0602Vertebrate cells
    • C12N5/0693Tumour cells; Cancer cells

Landscapes

  • 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)
  • Wood Science & Technology (AREA)
  • Biotechnology (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)
AU2005270104A 2004-07-02 2005-07-05 Inhibitors of IAP Abandoned AU2005270104A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2009243421A AU2009243421B2 (en) 2004-07-02 2009-11-30 Inhibitors of IAP

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58550104P 2004-07-02 2004-07-02
US60/585,501 2004-07-02

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2009243421A Division AU2009243421B2 (en) 2004-07-02 2009-11-30 Inhibitors of IAP

Publications (1)

Publication Number Publication Date
AU2005270104A1 true AU2005270104A1 (en) 2006-02-09

Family

ID=35311854

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2005270104A Abandoned AU2005270104A1 (en) 2004-07-02 2005-07-05 Inhibitors of IAP
AU2009243421A Expired AU2009243421B2 (en) 2004-07-02 2009-11-30 Inhibitors of IAP

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2009243421A Expired AU2009243421B2 (en) 2004-07-02 2009-11-30 Inhibitors of 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
CN1933847A (zh) * 2004-01-16 2007-03-21 密歇根大学董事会 Smac肽模拟物及其应用
CA2553874A1 (en) * 2004-01-16 2005-08-04 The Regents Of The University Of Michigan Conformationally constrained smac mimetics and the uses thereof
ES2394441T3 (es) 2004-04-07 2013-01-31 Novartis Ag Inhibidores de IAP
DK1778718T3 (da) * 2004-07-02 2014-11-10 Genentech Inc Iap-inhibitorer
US7674787B2 (en) * 2004-07-09 2010-03-09 The Regents Of The University Of Michigan Conformationally constrained Smac mimetics and the uses thereof
EP2457895A1 (en) * 2004-07-12 2012-05-30 Idun Pharmaceuticals, Inc. Tetrapeptide analogs
JP5230865B2 (ja) 2004-07-15 2013-07-10 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結合性化合物
ES2349110T5 (es) 2004-12-20 2013-11-27 Genentech, Inc. Inhibidores de IAP derivados de pirrolidina
CN103083644B (zh) 2005-02-25 2014-05-28 泰特拉洛吉克药业公司 Iap二聚体抑制剂
EP1883627B1 (en) 2005-05-18 2018-04-18 Pharmascience Inc. Bir domain binding compounds
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
CA2564872C (en) * 2005-10-25 2010-12-21 Aegera Therapeutics Inc. Iap bir domain binding compounds
RU2451025C2 (ru) * 2005-12-19 2012-05-20 Дженентек, Инк. Ингибиторы iap
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
SG171682A1 (en) * 2006-05-16 2011-06-29 Aegera Therapeutics Inc Iap bir domain binding compounds
WO2008014238A2 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
WO2008014240A2 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100144650A1 (en) * 2006-07-24 2010-06-10 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
EP2049563B1 (en) 2006-07-24 2014-03-12 Tetralogic Pharmaceuticals Corporation Dimeric iap antagonists
AR064235A1 (es) * 2006-07-24 2009-03-25 Tetralogic Pharmaceuticals Cor Dipeptidos antagonistas de iap, una composicion farmaceutica que los comprende y el uso de los mismos para el tratamiento del cancer
US20100056495A1 (en) * 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
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
JP2010501567A (ja) * 2006-08-24 2010-01-21 ノバルティス アクチエンゲゼルシャフト 代謝系、心血管系および他の障害の処置のためのステアロイル−CoA不飽和化酵素(SCD)阻害剤としての2−(ピラジン−2−イル)−チアゾールおよび2−(1H−ピラゾール−3−イル)チアゾール誘導体ならびに関連化合物
JP5351025B2 (ja) * 2006-09-22 2013-11-27 ノバルティス アーゲー ヘテロ環式有機化合物
JP5190062B2 (ja) * 2006-10-12 2013-04-24 ノバルティス アーゲー Iap阻害剤としてのピロリジン誘導体
US8063218B2 (en) * 2006-12-19 2011-11-22 Genentech, Inc. Imidazopyridine inhibitors of IAP
KR20090091337A (ko) * 2006-12-20 2009-08-27 노파르티스 아게 Scd 억제제로서의 2-치환 5-원 헤테로사이클
CA2684169C (en) * 2007-04-12 2012-06-19 Joyant Pharmaceuticals, Inc. Smac mimetic dimers and trimers useful as anti-cancer agents
AU2008245447C1 (en) * 2007-04-30 2014-11-20 Genentech, Inc. Inhibitors of IAP
WO2008137930A1 (en) * 2007-05-07 2008-11-13 Tetralogic Pharmaceuticals Corp. TNFα GENE EXPRESSION AS A BIOMARKER OF SENSITIVITY TO ANTAGONISTS OF INHIBITOR OF APOPTOSIS PROTEINS
US20100203012A1 (en) * 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
CN101970457A (zh) * 2008-01-11 2011-02-09 健泰科生物技术公司 Iap抑制剂
US20110117081A1 (en) * 2008-05-05 2011-05-19 Aegera Therapeutics, Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
US20110171171A1 (en) * 2008-06-27 2011-07-14 Aegera Therapeutics, Inc. Bridged secondary amines and use thereof as iap bir domain binding compounds
EP2318395A4 (en) * 2008-08-02 2011-10-26 Genentech Inc IPA INHIBITORS
EP2318401A4 (en) * 2008-08-16 2013-10-30 Genentech Inc AZAINDOLI INHIBITORS OF IPA
US8399683B2 (en) 2008-09-17 2013-03-19 Tetralogic Pharmaceuticals 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
WO2011035083A1 (en) 2009-09-18 2011-03-24 Novartis Ag Biomarkers for iap inhibitor compounds
WO2011059763A2 (en) 2009-10-28 2011-05-19 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
EP3263583A1 (en) 2010-02-12 2018-01-03 Pharmascience Inc. Iap bir domain binding compounds
AU2011240070A1 (en) 2010-04-16 2012-11-08 Bayer Intellectual Property Gmbh Heterocyclic compounds as pest control agents
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
KR20150011822A (ko) 2012-05-04 2015-02-02 노파르티스 아게 Iap 억제제 요법을 위한 바이오마커
CA2896577C (en) 2012-11-30 2024-01-23 Sanford-Burnham Medical Research Institute Inhibitor of apoptosis protein (iap) antagonists
US9498532B2 (en) 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
KR20150131173A (ko) 2013-03-15 2015-11-24 노파르티스 아게 항체 약물 접합체
SG11201509525XA (en) 2013-06-25 2016-01-28 Inst Medical W & E Hall Method of treating intracellular infection
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
AU2014369446C1 (en) * 2013-12-20 2020-03-12 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
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
US10300074B2 (en) 2014-06-04 2019-05-28 Sanford Burnham Prebys Medical Discovery Institute Use of inhibitor of apoptosis protein (IAP) antagonists in HIV therapy
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
US9982045B2 (en) 2014-08-12 2018-05-29 Novartis Ag Anti-CDH6 antibody drug conjugates
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
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
KR102564925B1 (ko) 2015-01-20 2023-08-07 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
WO2016203432A1 (en) 2015-06-17 2016-12-22 Novartis Ag Antibody drug conjugates
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
MA44334A (fr) 2015-10-29 2018-09-05 Novartis Ag Conjugués d'anticorps comprenant un agoniste du récepteur de type toll
WO2017222914A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Carbocyclic prolinamide derivatives
EP3472149B1 (en) 2016-06-21 2023-08-30 Orion Ophthalmology LLC Heterocyclic prolinamide derivatives
EP3535265A4 (en) 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE
PL3689868T3 (pl) 2016-12-01 2024-03-11 Arvinas Operations, Inc. Pochodne tetrahydronaftalenu i tetrahydroizochinoliny jako degradery receptorów estrogenowych
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
CN110753693A (zh) 2016-12-23 2020-02-04 阿尔维纳斯运营股份有限公司 Egfr蛋白水解靶向嵌合分子和相关使用方法
CN117510491A (zh) 2016-12-23 2024-02-06 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
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
IL300417A (en) 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzothiophene compounds, preparations containing them and their use in therapy
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
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
CN111107868A (zh) 2017-05-24 2020-05-05 诺华股份有限公司 抗体细胞因子移植蛋白及使用方法
PE20251254A1 (es) 2017-05-24 2025-05-06 Novartis Ag Proteinas de anticuerpo injertadas con citocina y metodos de uso en el tratamiento del cancer
KR102707188B1 (ko) 2017-11-13 2024-09-13 치아타이 티안큉 파마수티컬 그룹 주식회사 Iap 억제제로서 유용한 smac 모방물 및 그 용도
WO2019099926A1 (en) 2017-11-17 2019-05-23 Arvinas, 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
MX2020010420A (es) 2018-04-04 2020-12-11 Arvinas Operations Inc Moduladores de la proteólisis y métodos asociados de uso.
DK3820573T3 (da) 2018-07-10 2023-10-23 Novartis Ag 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidin-2,6-dion-derivativer og anvendelse deraf ved behandling af ikaros family zinc finger 2 (ikzf2)-afhængige sygdomme
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
WO2020023851A1 (en) 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
CA3109981A1 (en) 2018-09-07 2020-03-12 Arvinas Operations, Inc. Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
WO2020089811A1 (en) 2018-10-31 2020-05-07 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
PE20211296A1 (es) 2018-12-21 2021-07-20 Novartis Ag Anticuerpos anti-pmel17 y conjugados de los mismos
AU2020222345B2 (en) 2019-02-15 2022-11-17 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
US12479817B2 (en) 2019-02-15 2025-11-25 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
WO2020177765A1 (zh) * 2019-03-07 2020-09-10 正大天晴药业集团股份有限公司 Iap抑制剂与免疫检查点抑制剂的组合
DK3967702T3 (da) * 2019-05-10 2024-04-15 Chia Tai Tianqing Pharmaceutical Group Co Ltd Krystallisering af smac-mimic anvendt som iap-inhibitor og fremgangsmåde til fremstilling deraf
CN119954801A (zh) 2019-07-17 2025-05-09 阿尔维纳斯运营股份有限公司 Tau蛋白靶向化合物及相关使用方法
CN114514032A (zh) 2019-08-02 2022-05-17 兰提欧派普有限公司 用于治疗癌症的血管紧张素2型(at2)受体激动剂
MX2022002415A (es) 2019-08-26 2022-03-22 Arvinas Operations Inc Metodos de tratamiento del cancer de mama con derivados de tetrahidronaftaleno como degradadores del receptor de estrogenos.
JP2023506958A (ja) 2019-12-20 2023-02-20 ノバルティス アーゲー 骨髄線維症および骨髄異形成症候群を処置するための、デシタビンまたは抗pd-1抗体スパルタリズマブを伴うかまたは伴わない抗tim-3抗体mbg453および抗tgf-ベータ抗体nis793の組合せ
JP2023510426A (ja) 2020-01-20 2023-03-13 アストラゼネカ・アクチエボラーグ 癌を治療するための上皮細胞増殖因子受容体チロシンキナーゼ阻害剤
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
AU2021288224A1 (en) 2020-06-11 2023-01-05 Novartis Ag ZBTB32 inhibitors and uses thereof
WO2021260528A1 (en) 2020-06-23 2021-12-30 Novartis Ag Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
WO2022029573A1 (en) 2020-08-03 2022-02-10 Novartis Ag Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
JP2023539663A (ja) 2020-08-28 2023-09-15 アルビナス・オペレーションズ・インコーポレイテッド 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法
BR112023004656A2 (pt) 2020-09-14 2023-05-09 Arvinas Operations Inc Formas cristalinas e amorfas de um composto para a degradação direcionada do receptor de estrogênio
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
US20240252668A1 (en) 2021-04-16 2024-08-01 Anne-Sophie BLUEMMEL Antibody drug conjugates and methods for making thereof
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
CN119301125A (zh) 2022-07-26 2025-01-10 诺华股份有限公司 Akr1c3依赖性kars抑制剂的晶型
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
DE3685626T2 (de) * 1985-09-26 1993-01-28 Beckmann Research Inst Of The Sequenzierung von peptiden.
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
PT752248E (pt) 1992-11-13 2001-01-31 Idec Pharma Corp Aplicacao terapeutica de anticorpos quimericos e marcados radioactivamente contra antigenios de diferenciacao restrita de linfocitos b humanos para o tratamento do linfoma de celulas b
US5559209A (en) 1993-02-18 1996-09-24 The General Hospital Corporation Regulator regions of G proteins
ID27002A (id) * 1998-03-19 2001-02-22 Vertex Pharma Penghambat-penghambat kaspase
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
JP2002533726A (ja) 1998-12-28 2002-10-08 サネシス ファーマシューティカルス インコーポレイテッド 結合のための小有機分子リガンドの同定
US6608026B1 (en) 2000-08-23 2003-08-19 Board Of Regents, The University Of Texas System Apoptotic compounds
AU2001286730A1 (en) 2000-08-24 2002-03-04 Thomas Jefferson University An iap binding peptide or polypeptide and methods of using the same
US6992063B2 (en) 2000-09-29 2006-01-31 The Trustees Of Princeton University Compositions and method for regulating apoptosis
AU2001293189A1 (en) 2000-09-29 2002-04-08 Trustees Of Princeton University Compositions and methods for regulating apoptosis
WO2002030959A2 (en) 2000-10-13 2002-04-18 Abbott Laboratories Peptides derived from smac (diablo) and methods of use therefor
WO2003010184A2 (en) 2001-02-08 2003-02-06 Thomas Jefferson University A conserved xiap-interaction motif in caspase-9 and smac/diablo for mediating apoptosis
MXPA03010762A (es) 2001-05-31 2005-03-07 Univ Princeton Peptidos enlazantes de iap y ensayos para identificar los compuestos que enlazan el iap.
WO2003040172A2 (en) 2001-11-09 2003-05-15 Aegera Therapeutics, Inc. Methods and reagents for peptide-bir interaction screens
WO2003086470A2 (en) 2002-04-17 2003-10-23 Deutsches Krebsforschungszentrum Smac-peptides as therapeutics against cancer and autoimmune diseases
CN100384819C (zh) 2002-07-02 2008-04-30 诺瓦提斯公司 与细胞凋亡蛋白抑制剂结合的smac蛋白的肽抑制剂
EP1578777B1 (en) 2002-07-15 2008-11-26 The Trustees of Princeton University Iap binding compounds
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
US20040171554A1 (en) * 2003-02-07 2004-09-02 Genentech, Inc. Compositions and methods for enhancing apoptosis
DE60322120D1 (de) 2003-02-07 2008-08-21 Genentech Inc Zusammensetzungen und verfahren für verstärkte apoptose
IL156263A0 (en) 2003-06-02 2004-01-04 Hadasit Med Res Service Livin-derived peptides, compositions and uses thereof
WO2005049853A2 (en) 2003-11-13 2005-06-02 Genentech, Inc. Compositions and methods for screening pro-apoptotic compounds
ES2394441T3 (es) 2004-04-07 2013-01-31 Novartis Ag Inhibidores de IAP
DK1778718T3 (da) * 2004-07-02 2014-11-10 Genentech Inc Iap-inhibitorer
JP5230865B2 (ja) 2004-07-15 2013-07-10 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結合性化合物

Also Published As

Publication number Publication date
PT1778718E (pt) 2014-12-03
CA2570321A1 (en) 2006-02-09
RU2007104028A (ru) 2008-08-10
AU2009243421B2 (en) 2011-07-14
KR100984459B1 (ko) 2010-09-29
RU2401840C2 (ru) 2010-10-20
EP1778718B1 (en) 2014-10-08
US20120202750A1 (en) 2012-08-09
ES2524449T3 (es) 2014-12-09
KR100926203B1 (ko) 2009-11-09
PL1778718T3 (pl) 2015-03-31
US8110568B2 (en) 2012-02-07
NO20070606L (no) 2007-03-30
IL179854A (en) 2014-04-30
WO2006014361A1 (en) 2006-02-09
JP4850175B2 (ja) 2012-01-11
US8980837B2 (en) 2015-03-17
US20100256115A1 (en) 2010-10-07
CN101035802A (zh) 2007-09-12
NO341816B1 (no) 2018-01-29
ZA200700032B (en) 2008-05-28
KR20090089481A (ko) 2009-08-21
RS53734B1 (sr) 2015-06-30
NZ588799A (en) 2012-06-29
IL179854A0 (en) 2007-05-15
MXPA06014969A (es) 2007-02-08
BRPI0511350A (pt) 2007-12-04
EP1778718A1 (en) 2007-05-02
US20060014700A1 (en) 2006-01-19
US7244851B2 (en) 2007-07-17
SI1778718T1 (sl) 2015-01-30
AU2009243421A1 (en) 2009-12-17
JP2011251990A (ja) 2011-12-15
KR20070035060A (ko) 2007-03-29
JP2008505904A (ja) 2008-02-28
JP2014058522A (ja) 2014-04-03
CA2570321C (en) 2013-10-08
US20070299052A1 (en) 2007-12-27
JP5558428B2 (ja) 2014-07-23
DK1778718T3 (da) 2014-11-10

Similar Documents

Publication Publication Date Title
AU2009243421B2 (en) Inhibitors of IAP
US8907092B2 (en) Inhibitors of IAP
AU2005319305B2 (en) Pyrrolidine inhibitors of IAP
AU2006340014B2 (en) Inhibitors of IAP
AU2007337104A1 (en) Imidazopyridine inhibitors of IAP
US20110046066A1 (en) Inhibitors of iap
AU2011236020B2 (en) Inhibitors of IAP
AU2012244138A1 (en) Inhibitors of IAP

Legal Events

Date Code Title Description
MK5 Application lapsed section 142(2)(e) - patent request and compl. specification not accepted