KR101278732B1 - Ｉａｐ의 피롤리딘 억제제 - Google Patents

Ｉａｐ의 피롤리딘 억제제 Download PDF

Info

Publication number
KR101278732B1
KR101278732B1 KR1020077013861A KR20077013861A KR101278732B1 KR 101278732 B1 KR101278732 B1 KR 101278732B1 KR 1020077013861 A KR1020077013861 A KR 1020077013861A KR 20077013861 A KR20077013861 A KR 20077013861A KR 101278732 B1 KR101278732 B1 KR 101278732B1
Authority
KR
South Korea
Prior art keywords
mmol
alkyl
mixture
methyl
minutes
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.)
Expired - Lifetime
Application number
KR1020077013861A
Other languages
English (en)
Korean (ko)
Other versions
KR20070089174A (ko
Inventor
프레데릭 코헨
비키 시아오-웨이 쯔이
쿠옹 리
존 에이. 플리게어
Original Assignee
제넨테크, 인크.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36129810&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR101278732(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 제넨테크, 인크. filed Critical 제넨테크, 인크.
Publication of KR20070089174A publication Critical patent/KR20070089174A/ko
Application granted granted Critical
Publication of KR101278732B1 publication Critical patent/KR101278732B1/ko
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D417/14—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020077013861A 2004-12-20 2005-12-19 Ｉａｐ의 피롤리딘 억제제 Expired - Lifetime KR101278732B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US63820204P 2004-12-20 2004-12-20
US60/638,202 2004-12-20
PCT/US2005/046161 WO2006069063A1 (en) 2004-12-20 2005-12-19 Pyrrolidine inhibitors of iap

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020127028837A Division KR20120127754A (ko) 2004-12-20 2005-12-19 Ｉａｐ의 피롤리딘 억제제

Publications (2)

Publication Number Publication Date
KR20070089174A KR20070089174A (ko) 2007-08-30
KR101278732B1 true KR101278732B1 (ko) 2013-07-09

Family

ID=36129810

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020077013861A Expired - Lifetime KR101278732B1 (ko) 2004-12-20 2005-12-19 Ｉａｐ의 피롤리딘 억제제
KR1020127028837A Ceased KR20120127754A (ko) 2004-12-20 2005-12-19 Ｉａｐ의 피롤리딘 억제제

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020127028837A Ceased KR20120127754A (ko) 2004-12-20 2005-12-19 Ｉａｐ의 피롤리딘 억제제

Country Status (18)

Country Link
US (4) US20060167066A1 (https=)
EP (1) EP1836201B2 (https=)
JP (2) JP5007235B2 (https=)
KR (2) KR101278732B1 (https=)
CN (1) CN101146803A (https=)
AT (1) ATE477254T1 (https=)
AU (1) AU2005319305B2 (https=)
CA (1) CA2588921C (https=)
DE (1) DE602005022936D1 (https=)
DK (1) DK1836201T4 (https=)
EA (1) EA019420B1 (https=)
ES (1) ES2349110T5 (https=)
IL (1) IL183514A (https=)
MX (1) MX2007007195A (https=)
NO (1) NO339157B1 (https=)
NZ (1) NZ589670A (https=)
WO (1) WO2006069063A1 (https=)
ZA (1) ZA200704910B (https=)

Families Citing this family (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1401850A1 (en) 2001-06-20 2004-03-31 Nuevolution A/S Nucleoside derivatives for library preparation
EP1487978B1 (en) 2002-03-15 2008-11-19 Nuevolution A/S An improved method for synthesising templated molecules
WO2004013070A2 (en) 2002-08-01 2004-02-12 Nuevolution A/S Multi-step synthesis of templated molecules
PT2348125T (pt) 2002-10-30 2017-08-29 Nuevolution As Método para a síntese de um complexo bifuncional
AU2003291964A1 (en) 2002-12-19 2004-07-14 Nuevolution A/S Quasirandom structure and function guided synthesis methods
US20070026397A1 (en) 2003-02-21 2007-02-01 Nuevolution A/S Method for producing second-generation library
EP1670939B1 (en) 2003-09-18 2009-11-04 Nuevolution A/S A method for obtaining structural information concerning an encoded molecule and method for selecting compounds
RS52545B (sr) 2004-04-07 2013-04-30 Novartis Ag Inhibitori protein apoptoze (iap)
AU2005274937B2 (en) 2004-07-15 2011-08-18 Medivir Ab IAP binding compounds
MX2007007195A (es) 2004-12-20 2007-10-08 Genentech Inc Inhibidores de pirrolidina de iap.
ES2456671T3 (es) 2005-02-25 2014-04-23 Tetralogic Pharmaceuticals Corporation Inhibidores diméricos de IAP
US7772177B2 (en) 2005-05-18 2010-08-10 Aegera Therapeutics, Inc. BIR domain binding compounds
WO2007003961A2 (en) * 2005-06-30 2007-01-11 Prosidion Limited Gpcr agonists
US20100256046A1 (en) * 2009-04-03 2010-10-07 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
DE102005046907A1 (de) 2005-09-30 2007-04-12 Voith Patent Gmbh Verfahren und Vorrichtung zur Herstellung einer Tissuebahn
WO2007048224A1 (en) 2005-10-25 2007-05-03 Aegera Therapeutics Inc. Iap bir domain binding compounds
HUE056836T2 (hu) 2005-12-01 2022-03-28 Nuevolution As Enzimatikus kódolási eljárások nagy könyvtárak hatékony szintéziséhez
WO2007106192A2 (en) 2005-12-19 2007-09-20 Genentech, Inc. Inhibitors of 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
AU2007250443B2 (en) 2006-05-16 2013-06-13 Pharmascience Inc. IAP BIR domain binding compounds
CL2007002166A1 (es) 2006-07-24 2008-01-25 Tetralogic Pharm Corp Compuestos derivados de heterociclos de nitrogeno, antagonistas de los inhibidores de las proteinas de la apoptosis; sus composiciones farmaceuticas; y uso de dichos compuestos para el tratamiento del cancer.
KR20090041391A (ko) 2006-07-24 2009-04-28 테트랄로직 파마슈티칼스 이량체성 ｉａｐ 길항제
WO2008014229A2 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100056495A1 (en) * 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
WO2008014240A2 (en) * 2006-07-24 2008-01-31 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
US8044209B2 (en) 2006-10-12 2011-10-25 Novartis Ag Pyrrolydine derivatives as IAP inhibitors
US8063218B2 (en) * 2006-12-19 2011-11-22 Genentech, Inc. Imidazopyridine inhibitors of IAP
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
PE20130150A1 (es) * 2007-04-30 2013-02-27 Genentech Inc Inhibidores de las 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
JP5176452B2 (ja) * 2007-09-27 2013-04-03 住友化学株式会社 光学活性なテトラヒドロピラニルグリシン化合物の製造方法
ES2398791T3 (es) * 2008-01-11 2013-03-21 Genentech, Inc. Inhibidores de IAP
JP5581219B2 (ja) 2008-01-25 2014-08-27 ミレニアム ファーマシューティカルズ， インコーポレイテッド チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用
TW201011006A (en) * 2008-06-16 2010-03-16 Nuevolution As IAP binding compounds
CN102171209A (zh) 2008-08-02 2011-08-31 健泰科生物技术公司 Iap抑制剂
JP2012500272A (ja) * 2008-08-16 2012-01-05 ジェネンテック， インコーポレイテッド Ｉａｐのアザインドールインヒビター
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
WO2010090716A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
RU2404166C1 (ru) * 2009-04-14 2010-11-20 Учреждение Российской Академии Наук Институт Нефтехимии И Катализа Ран Способ получения 1-ацетилизохинолина
US8283372B2 (en) 2009-07-02 2012-10-09 Tetralogic Pharmaceuticals Corp. 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic
UY32826A (es) 2009-08-04 2011-02-28 Takeda Pharmaceutical Compuestos heterocíclicos
PE20121132A1 (es) 2009-08-12 2012-09-04 Novartis Ag Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis
WO2011035083A1 (en) 2009-09-18 2011-03-24 Novartis Ag Biomarkers for iap inhibitor compounds
EP2784076A1 (en) 2009-10-28 2014-10-01 Joyant Pharmaceuticals, Inc. Dimeric SMAC mimetics
KR20120118008A (ko) * 2009-12-18 2012-10-25 아이데닉스 파마슈티칼스, 인코포레이티드 5,5-융합 아릴렌 또는 헤테로아릴렌 간염 ｃ 바이러스 억제제
WO2011098904A1 (en) 2010-02-12 2011-08-18 Aegera Therapeutics, Inc. Iap bir domain binding compounds
WO2011127933A1 (en) 2010-04-16 2011-10-20 Nuevolution A/S Bi-functional complexes and methods for making and using such complexes
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012126881A1 (en) 2011-03-22 2012-09-27 Syngenta Participations Ag Insecticidal compounds
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
CN102757426A (zh) * 2011-04-28 2012-10-31 中国医学科学院医药生物技术研究所 一种苯并异恶唑基取代的噻唑类化合物、制备方法及用途
NO2755614T3 (https=) 2012-01-03 2018-03-31
CA2861066C (en) 2012-01-12 2024-01-02 Yale University Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase
US9353419B2 (en) 2012-05-04 2016-05-31 Novartis Ag Biomarkers for IAP inhibitor therapy
GB201218862D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
GB201218850D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218864D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
ES2828510T3 (es) * 2013-02-15 2021-05-26 Univ Nat Corp Tokyo Medical & Dental Agente terapéutico para tratar un cáncer en el que NRF2 está estabilizado
US9498532B2 (en) 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
NZ710929A (en) 2013-03-15 2018-02-23 Novartis Ag Antibody drug conjugates
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
ES2883289T3 (es) 2013-12-20 2021-12-07 Astex Therapeutics Ltd Compuestos heterocíclicos bicíclicos y sus usos en terapia
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2015187998A2 (en) 2014-06-04 2015-12-10 Sanford-Burnham Medical Research Institute Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy
US10786578B2 (en) 2014-08-05 2020-09-29 Novartis Ag CKIT antibody drug conjugates
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
KR20170040249A (ko) 2014-08-12 2017-04-12 노파르티스 아게 항-cdh6 항체 약물 접합체
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
EP3310813A1 (en) 2015-06-17 2018-04-25 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
TN2018000112A1 (en) 2015-10-29 2019-10-04 Novartis Ag Antibody conjugates comprising toll-like receptor agonist
IL290809B2 (en) 2016-11-01 2024-01-01 Arvinas Operations Inc Tau-protein targeting protacs and associated methods of use
KR102674902B1 (ko) 2016-12-01 2024-06-14 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
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
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
MX2019007646A (es) 2016-12-23 2019-09-06 Arvinas Operations Inc Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.
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
AU2018211975B2 (en) 2017-01-26 2022-05-26 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
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
EP3630162A1 (en) 2017-05-24 2020-04-08 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
BR112019024556A2 (pt) 2017-05-24 2020-06-23 Novartis Ag Proteínas enxertadas com citocina de anticorpo e métodos para uso no tratamento de câncer
AU2018308116A1 (en) * 2017-07-25 2020-02-13 Hepagene Therapeutics (HK) Limited Dimeric peptide inhibitors of apoptosis proteins
KR102707188B1 (ko) * 2017-11-13 2024-09-13 치아타이 티안큉 파마수티컬 그룹 주식회사 Iap 억제제로서 유용한 smac 모방물 및 그 용도
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
TWI812673B (zh) 2018-02-12 2023-08-21 美商富曼西公司 用於防治無脊椎害蟲之萘異噁唑啉化合物
KR20210006356A (ko) 2018-04-04 2021-01-18 아비나스 오퍼레이션스, 인코포레이티드 단백질분해 조절제 및 연관된 사용 방법
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
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
US20200038513A1 (en) 2018-07-26 2020-02-06 Arvinas Operations, Inc. Modulators of fak proteolysis and associated methods of use
EP3841100A1 (en) 2018-08-20 2021-06-30 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
KR102642203B1 (ko) 2018-09-07 2024-03-04 아비나스 오퍼레이션스, 인코포레이티드 급속 진행형 섬유육종 폴리펩티드의 표적화 분해를 위한 다중 고리 화합물 및 방법
EP3873532A1 (en) 2018-10-31 2021-09-08 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
JP7607564B2 (ja) 2018-12-21 2024-12-27 ノバルティス アーゲー Ｐｍｅｌ１７に対する抗体及びその結合体
EP3924055B1 (en) 2019-02-15 2024-04-03 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
WO2020179859A1 (ja) 2019-03-06 2020-09-10 第一三共株式会社 ピロロピラゾール誘導体
MX2021013729A (es) * 2019-05-10 2021-12-10 Chia Tai Tianqing Pharmaceutical Group Co Ltd Cristalina de imitador smac utilizado como inhibidor de iap y metodo de preparacion del mismo.
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
WO2021023698A1 (en) 2019-08-02 2021-02-11 Lanthiopep B.V Angiotensin type 2 (at2) receptor agonists for use in the treatment of cancer
IL320609A (en) 2019-08-26 2025-07-01 Arvinas Operations Inc Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents
MX2022007759A (es) 2019-12-20 2022-07-19 Novartis Ag Combinacion del anticuerpo anti tim-3 mbg453 y anticuerpo anti tgf-beta nis793, con o sin decitabina o el anticuerpo anti pd-1 spartalizumab, para el tratamiento de mielofibrosis y sindrome mielodisplasico.
CN113354530B (zh) * 2020-03-07 2025-11-18 东莞市东阳光动物保健药品有限公司 一种制备4-乙酰基-1-萘甲酸的方法
WO2021220178A1 (en) 2020-04-29 2021-11-04 Cominnex Zrt. Iap antagonists and their therapeutic applications
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
CA3185455A1 (en) 2020-06-11 2021-12-16 Novartis Ag Zbtb32 inhibitors and uses thereof
CN115916199A (zh) 2020-06-23 2023-04-04 诺华股份有限公司 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案
US20230271940A1 (en) 2020-08-03 2023-08-31 Novartis Ag Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
JP7834721B2 (ja) 2020-08-28 2026-03-24 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
AR123492A1 (es) 2020-09-14 2022-12-07 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógeno
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
CA3235132A1 (en) 2021-04-16 2022-10-20 Novartis Ag 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
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005097791A1 (en) 2004-04-07 2005-10-20 Novartis Ag Inhibitors of iap

Family Cites Families (57)

* 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
CA2012306A1 (en) 1989-03-28 1990-09-28 Werner Neidhart Amino acid derivatives
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
MD1367C2 (ro) 1992-11-13 2000-11-30 Idec Pharmaceuticals Corporation Metode de tratament al limfomului celulelor B, anticorpi anti-CD20, hibridom.
US5559209A (en) * 1993-02-18 1996-09-24 The General Hospital Corporation Regulator regions of G proteins
SK56798A3 (en) 1995-10-30 1998-12-02 Smithkline Beecham Corp Protease inhibitors, pharmaceutical composition containing them and their use
AU7127298A (en) 1997-04-14 1998-11-11 Emory University Serine protease inhibitors
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
EP1315811A2 (en) 2000-08-24 2003-06-04 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
AU2002253432B2 (en) 2001-04-05 2005-03-24 Torrent Pharmaceuticals Ltd. Heterocyclic compounds for aging-related and diabetic vascular complications
CA2449168A1 (en) 2001-05-31 2002-12-05 The Trustees Of Princeton University Iap binding peptides and assays for identifying compounds that bind iap
US20030157522A1 (en) * 2001-11-09 2003-08-21 Alain Boudreault 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)
ATE415413T1 (de) * 2002-07-15 2008-12-15 Univ Princeton Iap-bindende verbindungen
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
WO2005049853A2 (en) 2003-11-13 2005-06-02 Genentech, Inc. Compositions and methods for screening pro-apoptotic compounds
US7932382B2 (en) 2004-01-16 2011-04-26 The Regents Of The University Of Michigan Conformationally constrained Smac mimetics and the uses thereof
CA2553871A1 (en) 2004-01-16 2005-08-04 The Regents Of The University Of Michigan Smac peptidomimetics and the uses thereof
CN1926118A (zh) 2004-03-01 2007-03-07 德克萨斯大学董事会 二聚的小分子细胞凋亡增强剂
WO2005094818A1 (en) 2004-03-23 2005-10-13 Genentech, Inc. Azabicyclo-octane inhibitors of iap
BRPI0511350A (pt) 2004-07-02 2007-12-04 Genentech Inc composto, métodos de indução da apoptose em uma célula, de sensibilização de uma célula à um sinal apoptótico, de inibição da ligação de uma proteìna iap e de tratamento de uma doença e cáncer e usos de um composto
EP1773348A4 (en) 2004-07-12 2009-05-20 Idun Pharmaceuticals Inc TETRA PEPTIDE ANALOGS
AU2005274937B2 (en) 2004-07-15 2011-08-18 Medivir Ab IAP binding compounds
MX2007007195A (es) 2004-12-20 2007-10-08 Genentech Inc Inhibidores de pirrolidina de iap.
ES2456671T3 (es) 2005-02-25 2014-04-23 Tetralogic Pharmaceuticals Corporation Inhibidores diméricos de IAP
US7772177B2 (en) 2005-05-18 2010-08-10 Aegera Therapeutics, Inc. BIR domain binding compounds
WO2007048224A1 (en) 2005-10-25 2007-05-03 Aegera Therapeutics Inc. Iap bir domain binding compounds
WO2007106192A2 (en) 2005-12-19 2007-09-20 Genentech, Inc. Inhibitors of iap
US7205737B1 (en) 2006-01-04 2007-04-17 Robert Bosch Gmbh Systems and methods of monitoring a motor load
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
BRPI0708942A2 (pt) 2006-03-21 2011-06-14 Joyant Pharmaceuticals Inc composto promotor de apoptose, uso e mÉtodo de produÇço do mesmo e composiÇço farmacÊutica
CN101490100B (zh) 2006-04-07 2012-08-22 派奥特雷克株式会社 交联的硝基氧聚合物的制备方法
WO2008014238A2 (en) 2006-07-24 2008-01-31 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
US8329159B2 (en) 2006-08-11 2012-12-11 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8044209B2 (en) 2006-10-12 2011-10-25 Novartis Ag Pyrrolydine derivatives as IAP inhibitors
US8063218B2 (en) 2006-12-19 2011-11-22 Genentech, Inc. Imidazopyridine inhibitors of IAP
PE20130150A1 (es) 2007-04-30 2013-02-27 Genentech Inc Inhibidores de las iap
ES2398791T3 (es) 2008-01-11 2013-03-21 Genentech, Inc. Inhibidores de IAP
CN102171209A (zh) 2008-08-02 2011-08-31 健泰科生物技术公司 Iap抑制剂
JP2012500272A (ja) 2008-08-16 2012-01-05 ジェネンテック， インコーポレイテッド Ｉａｐのアザインドールインヒビター

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005097791A1 (en) 2004-04-07 2005-10-20 Novartis Ag Inhibitors of iap

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Journal of Organic Chemistry, 1999, Vol. 64, No. 14, 5329-5332. *
Tetrahedron, 2002, Vol. 58, No. 40, 8127-8143 *

Also Published As

Publication number Publication date
DK1836201T4 (da) 2013-11-11
CA2588921C (en) 2015-10-20
EP1836201B1 (en) 2010-08-11
JP5007235B2 (ja) 2012-08-22
EA019420B1 (ru) 2014-03-31
AU2005319305B2 (en) 2012-08-23
NO339157B1 (no) 2016-11-14
JP2012184230A (ja) 2012-09-27
EA200701467A1 (ru) 2007-12-28
WO2006069063A1 (en) 2006-06-29
KR20070089174A (ko) 2007-08-30
US9040706B2 (en) 2015-05-26
US20090318409A1 (en) 2009-12-24
KR20120127754A (ko) 2012-11-23
EP1836201A1 (en) 2007-09-26
AU2005319305A1 (en) 2006-06-29
IL183514A (en) 2015-11-30
CA2588921A1 (en) 2006-06-29
MX2007007195A (es) 2007-10-08
US20090176822A1 (en) 2009-07-09
ES2349110T3 (es) 2010-12-28
ZA200704910B (en) 2008-09-25
US20060167066A1 (en) 2006-07-27
DK1836201T3 (da) 2010-12-06
HK1109155A1 (en) 2008-05-30
NO20073783L (no) 2007-09-19
NZ589670A (en) 2013-01-25
CN101146803A (zh) 2008-03-19
IL183514A0 (en) 2007-09-20
JP2008524333A (ja) 2008-07-10
US20140080805A1 (en) 2014-03-20
EP1836201B2 (en) 2013-09-04
ATE477254T1 (de) 2010-08-15
ES2349110T5 (es) 2013-11-27
US8609845B2 (en) 2013-12-17
DE602005022936D1 (de) 2010-09-23

Similar Documents

Publication Publication Date Title
KR101278732B1 (ko) Ｉａｐ의 피롤리딘 억제제
RU2466131C2 (ru) Имидазопиридиновые ингибиторы iap
JP5368428B2 (ja) Ｉａｐのインヒビター
JP5155184B2 (ja) Ｉａｐのインヒビター
US20110218211A1 (en) Azaindole inhibitors of iap
KR20100110870A (ko) Ｉａｐ의 억제제
HK1109155B (en) Pyrrolidine inhibitors of iap

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20070619

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20101217

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20120904

Patent event code: PE09021S01D

A107 Divisional application of patent
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20121102

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20130325

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20130619

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20130619

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
FPAY Annual fee payment

Payment date: 20160330

Year of fee payment: 4

PR1001 Payment of annual fee

Payment date: 20160330

Start annual number: 4

End annual number: 4

FPAY Annual fee payment

Payment date: 20170330

Year of fee payment: 5

PR1001 Payment of annual fee

Payment date: 20170330

Start annual number: 5

End annual number: 5

FPAY Annual fee payment

Payment date: 20180329

Year of fee payment: 6

PR1001 Payment of annual fee

Payment date: 20180329

Start annual number: 6

End annual number: 6

FPAY Annual fee payment

Payment date: 20190327

Year of fee payment: 7

PR1001 Payment of annual fee

Payment date: 20190327

Start annual number: 7

End annual number: 7

PR1001 Payment of annual fee

Payment date: 20200324

Start annual number: 8

End annual number: 8

PR1001 Payment of annual fee

Payment date: 20210329

Start annual number: 9

End annual number: 9

PR1001 Payment of annual fee

Payment date: 20220325

Start annual number: 10

End annual number: 10

PR1001 Payment of annual fee

Payment date: 20230327

Start annual number: 11

End annual number: 11

PR1001 Payment of annual fee

Payment date: 20240527

Start annual number: 12

End annual number: 12