UY33794A - Inhibidores diméricos de las iap - Google Patents

Inhibidores diméricos de las iap

Info

Publication number
UY33794A
UY33794A UY0001033794A UY33794A UY33794A UY 33794 A UY33794 A UY 33794A UY 0001033794 A UY0001033794 A UY 0001033794A UY 33794 A UY33794 A UY 33794A UY 33794 A UY33794 A UY 33794A
Authority
UY
Uruguay
Prior art keywords
iap
dimeric
dimeric inhibitors
formula
inhibitors
Prior art date
Application number
UY0001033794A
Other languages
English (en)
Inventor
Christopher Sean Straub
Chen Zhuoliang
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of UY33794A publication Critical patent/UY33794A/es

Links

Classifications

    • 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
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • 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
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

El presente invento proporciona compuestos de la fórmula M- L- M' (donde M y M' son cada uno, de manera independiente, una fracción monomérica de la fórmula (I) y L es un enlazador). Se ha encontrado que los compuestos diméricos son efectivos para promover la apoptosis en células que se estén dividiendo rápidamente.
UY0001033794A 2010-12-13 2011-12-09 Inhibidores diméricos de las iap UY33794A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US42242210P 2010-12-13 2010-12-13

Publications (1)

Publication Number Publication Date
UY33794A true UY33794A (es) 2012-07-31

Family

ID=45349201

Family Applications (1)

Application Number Title Priority Date Filing Date
UY0001033794A UY33794A (es) 2010-12-13 2011-12-09 Inhibidores diméricos de las iap

Country Status (8)

Country Link
US (1) US8993523B2 (es)
EP (1) EP2651919A1 (es)
JP (1) JP2013545781A (es)
CN (1) CN103347874B (es)
AR (1) AR084251A1 (es)
TW (1) TW201307318A (es)
UY (1) UY33794A (es)
WO (1) WO2012080271A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
ES2883289T3 (es) 2013-12-20 2021-12-07 Astex Therapeutics Ltd Compuestos heterocíclicos bicíclicos y sus usos en terapia
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
CN109705191B (zh) * 2017-10-25 2022-04-29 广东东阳光药业有限公司 Iap抑制剂及其在药物中的应用
CN108610333B (zh) * 2018-06-08 2020-04-03 绍兴文理学院 诱导MDM2自我降解E3泛素连接酶二聚体酰胺类小分子PROTACs
WO2020027225A1 (ja) 2018-07-31 2020-02-06 ファイメクス株式会社 複素環化合物
JP2024539137A (ja) 2021-10-22 2024-10-28 ユニバーシティー オブ ヒューストン システム 上皮組織の慢性炎症性傷害、化生、異形成、および癌を処置するための方法および組成物
CN114163438A (zh) * 2021-12-13 2022-03-11 无锡捷化医药科技有限公司 一种2-甲基-3-羰基吡唑并[4,3-c]吡啶-7-羧酸盐酸盐的制备方法

Family Cites Families (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US5281620A (en) 1986-12-23 1994-01-25 Cancer Research Campaign Technology Limited Compounds having antitumor and antibacterial properties
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
ATE415413T1 (de) 2002-07-15 2008-12-15 Univ Princeton Iap-bindende verbindungen
US7229617B2 (en) 2002-11-27 2007-06-12 Irm Llc Methods and compositions for inducing apoptosis in cancer cells
KR20060126548A (ko) 2004-02-05 2006-12-07 노파르티스 아게 (a) DNA 토포이소머라제 억제제 및 (b) IAP 억제제조합물
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
AU2005274937B2 (en) 2004-07-15 2011-08-18 Medivir Ab IAP binding compounds
ES2456671T3 (es) 2005-02-25 2014-04-23 Tetralogic Pharmaceuticals Corporation Inhibidores diméricos de IAP
US20110183358A1 (en) 2005-03-17 2011-07-28 The Burnham Institute Methods and compositions for derepression of iap-inhibited caspase
US7772177B2 (en) 2005-05-18 2010-08-10 Aegera Therapeutics, Inc. BIR domain binding compounds
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2007021825A2 (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
US20070203749A1 (en) 2005-08-09 2007-08-30 Sri Chunduru Business methods for compounds for treatment of proliferative disorders
WO2007048224A1 (en) 2005-10-25 2007-05-03 Aegera Therapeutics Inc. Iap bir domain binding compounds
WO2007075525A2 (en) 2005-12-20 2007-07-05 Novartis Ag Combination of an iap-inhibitor and a taxane7
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
US8202902B2 (en) 2006-05-05 2012-06-19 The Regents Of The University Of Michigan Bivalent SMAC mimetics and the uses thereof
AU2007250443B2 (en) 2006-05-16 2013-06-13 Pharmascience Inc. IAP BIR domain binding compounds
WO2008014238A2 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
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
WO2008014240A2 (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
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
KR20090082221A (ko) 2006-10-19 2009-07-29 노파르티스 아게 유기 화합물
CN101541325A (zh) 2006-11-28 2009-09-23 诺瓦提斯公司 Iap抑制剂用于治疗急性髓性白血病的用途
WO2008066854A2 (en) 2006-11-28 2008-06-05 Novartis Ag Methods and compositions for inducing apoptosis in cancer cells
WO2008109057A1 (en) 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
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
WO2008144925A1 (en) 2007-05-30 2008-12-04 Aegera Therapeutics Inc. Iap bir domain binding compounds
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers
ES2398791T3 (es) 2008-01-11 2013-03-21 Genentech, Inc. Inhibidores de IAP
EP2242362A4 (en) 2008-01-24 2012-04-11 Tetralogic Pharm Corp IAP INHIBITORS
WO2009136290A1 (en) 2008-05-05 2009-11-12 Aegera Therapeutics, Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
WO2009155709A1 (en) * 2008-06-27 2009-12-30 Aegera Therapeutics Inc. Bridged secondary amines and use thereof as iap bir domain binding compounds
CN102171209A (zh) 2008-08-02 2011-08-31 健泰科生物技术公司 Iap抑制剂
WO2010015090A1 (en) 2008-08-07 2010-02-11 Aegera Therapeutics Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
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
AU2009293403A1 (en) 2008-09-17 2010-03-25 Tetralogic Pharmaceuticals Corp. IAP inhibitors
US20110177060A1 (en) 2008-09-19 2011-07-21 Aegera Therapeutics, Inc. Iap bir domain binding compounds
EP2350641B1 (en) 2008-09-22 2014-09-24 Amgen Inc. A combination of a tnf alpha inhibitor, an iap inhibitor and a trail receptor agonist for use in treating cancer
US8415486B2 (en) 2009-05-28 2013-04-09 Tetralogic Pharmaceuticals Corp. IAP inhibitors
CA2763614A1 (en) 2009-05-28 2010-12-02 Tetralogic Pharmaceuticals Corp. Iap inhibitors
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
UY32826A (es) 2009-08-04 2011-02-28 Takeda Pharmaceutical Compuestos heterocíclicos
ES2643233T3 (es) 2009-10-23 2017-11-21 The Regents Of The University Of Michigan Miméticos de SMAC bicíclicos diazo bivalentes y los usos de los mismos
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
WO2011068926A1 (en) 2009-12-04 2011-06-09 Tetralogic Pharmaceuticals Corp. Iap inhibitors
KR101230851B1 (ko) 2010-01-19 2013-02-07 한미사이언스 주식회사 세포사멸 유도 활성을 갖는 이미다조피라진온 유도체
WO2011098904A1 (en) 2010-02-12 2011-08-18 Aegera Therapeutics, Inc. Iap bir domain binding compounds
UY33236A (es) * 2010-02-25 2011-09-30 Novartis Ag Inhibidores dimericos de las iap
US20130266590A1 (en) 2010-12-13 2013-10-10 Novartis Ag Dimeric iap inhibitors

Also Published As

Publication number Publication date
US20130309247A1 (en) 2013-11-21
CN103347874A (zh) 2013-10-09
CN103347874B (zh) 2014-10-29
JP2013545781A (ja) 2013-12-26
EP2651919A1 (en) 2013-10-23
TW201307318A (zh) 2013-02-16
AR084251A1 (es) 2013-05-02
US8993523B2 (en) 2015-03-31
WO2012080271A1 (en) 2012-06-21

Similar Documents

Publication Publication Date Title
UY33794A (es) Inhibidores diméricos de las iap
UY33236A (es) Inhibidores dimericos de las iap
CO6670585A2 (es) Promotores de apotosis n-acilsufonamidas
ECSP13013074A (es) Nuevos derivados de piridina
CR20140166A (es) Compuestos de (hetero)arilciclopropilamina como inhibidores de lsd1
CO7240375A2 (es) Compuestos tricíclicos sustituidos como inhibidores del fgfr
GT201400147A (es) Pirimidinas y triazinas fusionadas sustituidas y su uso
CR20150250A (es) Nuevos derivados de piridina
CO6491116A2 (es) Derivados de 5-fluoropirimidinona
CR20140464A (es) Compuestos de heterociclilo
ECSP11011411A (es) Derivados de prolina como inhibidores de catepsina
ECSP12012174A (es) Derivados de n-(imidazopirimidin-7-il)-heteroarilamida y su uso como inhibidores de pde10a
MX2019010602A (es) Inhibidores de cdk.
UA108101C2 (xx) Похідні n3-заміщених n1-сульфоніл-5-фторпіримідинонів
CU20140025A7 (es) Pirimidinas anilladas sustituidas
UY34333A (es) ?métodos y composiciones para el control de malezas, y métodos para reducir la expresión de enzima dhps?
CR20150204A (es) Nuevos derivados de piridina
CR20150277A (es) Piridina-2-amidas utiles como agonistas cb2
DOP2011000382A (es) Sulfonamidas heterociclicas, usos y composiciones farmaceuticas de las mismas
DOP2014000036A (es) Compuestos de piridazinona y su uso como inhibidores daao
CR20150447A (es) Nuevos derivados de pirazol
CO6741154A2 (es) Compuestos de triazolopiridina
CL2012000508A1 (es) Composicion para la aplicacion en cultivos agricolas al aire libre o invernaderos que comprende zeolita, y aditivos; uso de la composicion para aumentar el rendimiento de los cultivos agricolas.
CR20150210A (es) Nuevos derivados de pirazina como agonistas receptores de cb2
CR20140217A (es) Compuestos de 1,2,5-oxadiazol sustituido y su uso como herbicidas ii

Legal Events

Date Code Title Description
109 Application deemed to be withdrawn

Effective date: 20200217

109 Application deemed to be withdrawn

Effective date: 20210618