ES2654623T3 - Inhibidores bivalentes de proteínas IAP y métodos terapéuticos que los usan - Google Patents

Inhibidores bivalentes de proteínas IAP y métodos terapéuticos que los usan Download PDF

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Publication number
ES2654623T3
ES2654623T3 ES13831176.6T ES13831176T ES2654623T3 ES 2654623 T3 ES2654623 T3 ES 2654623T3 ES 13831176 T ES13831176 T ES 13831176T ES 2654623 T3 ES2654623 T3 ES 2654623T3
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hours
protein
structures
formula
separation
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Spanish (es)
Inventor
Shaomeng Wang
Rong SHENG
Haiying Sun
Liu Liu
Jianfeng Lu
Donna Mceachern
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University of Michigan System
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University of Michigan System
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • AIDS & HIV (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
ES13831176.6T 2012-08-23 2013-08-16 Inhibidores bivalentes de proteínas IAP y métodos terapéuticos que los usan Active ES2654623T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261692429P 2012-08-23 2012-08-23
US201261692429P 2012-08-23
PCT/US2013/055384 WO2014031487A1 (en) 2012-08-23 2013-08-16 Bivalent inhibitors of iap proteins and therapeutic methods using the same

Publications (1)

Publication Number Publication Date
ES2654623T3 true ES2654623T3 (es) 2018-02-14

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ES13831176.6T Active ES2654623T3 (es) 2012-08-23 2013-08-16 Inhibidores bivalentes de proteínas IAP y métodos terapéuticos que los usan

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US (1) US8883771B2 (enExample)
EP (1) EP2888265B1 (enExample)
JP (1) JP6247298B2 (enExample)
KR (2) KR102237888B1 (enExample)
CN (3) CN109575049B (enExample)
AU (1) AU2013306087B2 (enExample)
CA (1) CA2882496C (enExample)
ES (1) ES2654623T3 (enExample)
HK (1) HK1211030A1 (enExample)
MX (1) MX366130B (enExample)
RU (1) RU2649975C2 (enExample)
WO (1) WO2014031487A1 (enExample)

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US10441654B2 (en) 2014-01-24 2019-10-15 Children's Hospital Of Eastern Ontario Research Institute Inc. SMC combination therapy for the treatment of cancer
JP2017511348A (ja) * 2014-04-16 2017-04-20 成都大学 Ｂｃｒ−Ａｂｌ二倍体の阻害剤、その調製方法及びその用途
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
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
CA3020792A1 (en) 2016-04-20 2017-10-26 Glaxosmithkline Intellectual Property Development Limited Conjugates comprising ripk2 inhibitors
WO2017194390A1 (en) * 2016-05-09 2017-11-16 F. Hoffmann-La Roche Ag Dimeric compounds
CN118436801A (zh) 2016-05-20 2024-08-06 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
GB201610147D0 (en) 2016-06-10 2016-07-27 Glaxosmithkline Ip Dev Ltd Novel compounds
GB2567126A (en) * 2017-06-23 2019-04-10 Femtogenix Ltd PBC compounds
CN107987083A (zh) * 2017-11-24 2018-05-04 江苏亚盛医药开发有限公司 用于治疗和/或预防与肝炎病毒相关的疾病或病症的双二氮杂双环化合物
JP7616987B2 (ja) 2018-07-13 2025-01-17 エフ． ホフマン－ラ ロシュ アーゲー Ｒｔｅｌ１発現の調節用のオリゴヌクレオチド
MX2020013730A (es) 2018-07-31 2021-05-27 Ascentage Pharma Suzhou Co Ltd Metodo para tratar el cancer mediante la combinacion de un inhibidor de iap y un modulador de una molecula de punto de control inmunitario.
CN112533898A (zh) 2018-07-31 2021-03-19 日商泛美克斯股份有限公司 杂环化合物
US20220016079A1 (en) 2018-11-26 2022-01-20 Debiopharm International S.A. Combination treatment of hiv infections
US10870663B2 (en) 2018-11-30 2020-12-22 Glaxosmithkline Intellectual Property Development Limited Compounds useful in HIV therapy
WO2021026349A1 (en) 2019-08-08 2021-02-11 Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center Combination therapy for treatment of cancer
WO2021058794A1 (en) 2019-09-25 2021-04-01 Debiopharm International S.A. Dosing regimens for treatment of patients with locally advanced squamous cell carcinoma
EP4061361A4 (en) * 2019-11-19 2023-11-29 Ascentage Pharma (Suzhou) Co., Ltd. TREATMENT METHODS WITH IAP INHIBITOR
US20230029259A1 (en) * 2019-12-02 2023-01-26 Ascentage Pharma (Suzhou) Co., Ltd. Combination of iap inhibitors and parp or mek inhibitors or other chemotherapeutic agents
TWI777321B (zh) 2019-12-04 2022-09-11 大陸商蘇州亞盛藥業有限公司 藥物組合及其用途
CN114828852A (zh) 2019-12-24 2022-07-29 豪夫迈·罗氏有限公司 用于治疗hbv的靶向hbv的抗病毒药剂和/或免疫调节剂的药物组合
CN114728006A (zh) * 2020-05-04 2022-07-08 苏州亚盛药业有限公司 治疗冠状病毒感染的方法
WO2022012671A1 (en) * 2020-07-16 2022-01-20 Ascentage Pharma (Suzhou) Co., Ltd. The crystalline forms or amorphous forms of bisdiazabicyclic compounds or salts thereof
CN116963732A (zh) * 2021-02-23 2023-10-27 苏州亚盛药业有限公司 药物组合物及其制备方法
WO2023011488A1 (zh) 2021-08-02 2023-02-09 苏州亚盛药业有限公司 一种药物组合及其用途
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same
CA3254393A1 (en) 2022-05-23 2023-11-30 Inhibrx Biosciences, Inc. DR5 AGONIST AND IAP ANTAGONIST POLYTHERAPY
US12508320B2 (en) 2023-06-29 2025-12-30 SeeCure Taiwan Co., Ltd. Drug conjugate, pharmaceutical composition and method of treating hepatitis
WO2025090605A1 (en) * 2023-10-24 2025-05-01 University Of Houston System Combination of iap inhibitors and cellular kinase inhibitors, such as ponatinib, for use in the treatment of cancer or pulmonary diseases, such as copd, cystic fibrosis, pulmonary fibrosis and covid-19
WO2025261398A1 (en) * 2024-06-19 2025-12-26 Ascentage Pharma (Suzhou) Co., Ltd. Methods for treating diseases caused by hiv infection
CN119100970B (zh) * 2024-08-30 2025-09-30 中国药科大学 基于热休克蛋白90的二价抑制剂及其制备方法和应用

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US20040072831A1 (en) * 2001-10-12 2004-04-15 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
AU2005218555B2 (en) 2004-03-01 2008-01-03 Board Of Regents, The University Of Texas System Dimeric small molecule potentiators of apoptosis
CN101128425B (zh) * 2005-02-25 2012-12-26 泰特拉洛吉克药业公司 Iap二聚体抑制剂
HRP20141253T1 (en) * 2006-05-05 2015-03-13 The Regents Of The Universitiy Of Michigan Intermediates for the preparation of bivalent smac mimetics
HRP20140885T1 (hr) * 2007-04-13 2014-11-21 The Regents Of The University Of Michigan Diazo bicikliäśki smac mimetici i njihove primjene
WO2011050068A2 (en) * 2009-10-23 2011-04-28 The Regents Of The University Of Michigan Bivalent diazo bicyclic smac mimetics and the uses thereof

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WO2014031487A1 (en) 2014-02-27
EP2888265A1 (en) 2015-07-01
US8883771B2 (en) 2014-11-11
AU2013306087B2 (en) 2017-08-10
KR102237888B1 (ko) 2021-04-07
JP6247298B2 (ja) 2017-12-13
KR102111704B1 (ko) 2020-05-15
EP2888265B1 (en) 2017-10-11
EP2888265A4 (en) 2016-01-27
AU2013306087A1 (en) 2015-03-12
HK1211030A1 (en) 2016-05-13
KR20200054334A (ko) 2020-05-19
CA2882496C (en) 2020-07-14
CN104718209A (zh) 2015-06-17
CN109485662B (zh) 2021-12-21
JP2015528447A (ja) 2015-09-28
WO2014031487A8 (en) 2014-05-30
MX2015002371A (es) 2015-10-05
US20140057924A1 (en) 2014-02-27
MX366130B (es) 2019-06-28
CN109485662A (zh) 2019-03-19
CA2882496A1 (en) 2014-02-27
CN109575049A (zh) 2019-04-05
RU2015107552A (ru) 2016-10-10
KR20150044937A (ko) 2015-04-27
RU2649975C2 (ru) 2018-04-06
CN109575049B (zh) 2021-07-30

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