JP5529282B2 - 二量体Ｓｍａｃ模倣薬 - Google Patents
二量体Ｓｍａｃ模倣薬 Download PDFInfo
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- JP5529282B2 JP5529282B2 JP2012537075A JP2012537075A JP5529282B2 JP 5529282 B2 JP5529282 B2 JP 5529282B2 JP 2012537075 A JP2012537075 A JP 2012537075A JP 2012537075 A JP2012537075 A JP 2012537075A JP 5529282 B2 JP5529282 B2 JP 5529282B2
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- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Zoology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Toxicology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
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| US25578809P | 2009-10-28 | 2009-10-28 | |
| US61/255,788 | 2009-10-28 | ||
| PCT/US2010/054546 WO2011059763A2 (en) | 2009-10-28 | 2010-10-28 | Dimeric smac mimetics |
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| JP2014084316A Division JP2014167006A (ja) | 2009-10-28 | 2014-04-16 | 二量体Ｓｍａｃ模倣薬 |
Publications (3)
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| JP2013509429A JP2013509429A (ja) | 2013-03-14 |
| JP2013509429A5 JP2013509429A5 (enExample) | 2013-12-05 |
| JP5529282B2 true JP5529282B2 (ja) | 2014-06-25 |
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| JP2012537075A Expired - Fee Related JP5529282B2 (ja) | 2009-10-28 | 2010-10-28 | 二量体Ｓｍａｃ模倣薬 |
| JP2014084316A Pending JP2014167006A (ja) | 2009-10-28 | 2014-04-16 | 二量体Ｓｍａｃ模倣薬 |
Family Applications After (1)
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| JP2014084316A Pending JP2014167006A (ja) | 2009-10-28 | 2014-04-16 | 二量体Ｓｍａｃ模倣薬 |
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| EP (2) | EP2493879B1 (enExample) |
| JP (2) | JP5529282B2 (enExample) |
| CN (1) | CN102958928B (enExample) |
| CA (1) | CA2789879A1 (enExample) |
| WO (1) | WO2011059763A2 (enExample) |
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| EP2882740B1 (en) * | 2012-08-09 | 2017-03-01 | Bristol-Myers Squibb Company | Iap antagonists |
| EP2885275A1 (en) * | 2012-08-15 | 2015-06-24 | F. Hoffmann-La Roche AG | Azaheterocycles as bir2 and/or bir3 inhibitors |
| WO2014055461A1 (en) * | 2012-10-02 | 2014-04-10 | Bristol-Myers Squibb Company | Iap antagonists |
| WO2014056867A1 (en) * | 2012-10-11 | 2014-04-17 | F. Hoffmann-La Roche Ag | Azaindolines |
| MX2015004525A (es) * | 2012-10-11 | 2015-07-06 | Hoffmann La Roche | Azaindolinas. |
| EA201591024A1 (ru) * | 2012-12-11 | 2015-09-30 | Ф. Хоффманн-Ля Рош Аг | Димерные соединения |
| 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 |
| US9637518B2 (en) | 2013-07-12 | 2017-05-02 | Bristol-Myers Squibb Company | IAP antagonists |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| PE20161432A1 (es) | 2014-05-13 | 2017-01-08 | Novartis Ag | Compuestos y composiciones para inducir condrogenesis |
| 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 |
| CA2974367A1 (en) | 2015-01-20 | 2016-07-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of the androgen receptor |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| US20180147202A1 (en) | 2015-06-05 | 2018-05-31 | Arvinas, Inc. | TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE |
| BR112017028269A2 (pt) * | 2015-07-13 | 2018-09-04 | Arvinas Inc | composto, composição farmacêutica, uso de uma quantidade efetiva de um composto, estado ou condição de doença, e, método para identificar um composto. |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| EP3535265A4 (en) | 2016-11-01 | 2020-07-08 | Arvinas, Inc. | PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE |
| RS64976B1 (sr) | 2016-12-01 | 2024-01-31 | Arvinas Operations Inc | Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora |
| RU2019121527A (ru) | 2016-12-23 | 2021-01-15 | Эрвинэс Оперейшнс, Инк. | Химерные молекулы, нацеливающиеся на протеолиз egfr, и связанные с ними способы применения |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, 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 |
| JP7679173B2 (ja) | 2016-12-23 | 2025-05-19 | アルビナス・オペレーションズ・インコーポレイテッド | Ｒａｆ（急速進行性線維肉腫）ポリペプチドの標的分解のための化合物および方法 |
| 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 |
| CN117551089A (zh) | 2017-01-26 | 2024-02-13 | 阿尔维纳斯运营股份有限公司 | 雌激素受体蛋白水解调节剂及相关使用方法 |
| EP3686185B1 (en) | 2017-09-22 | 2023-12-13 | Seoul National University R & DB Foundation | Fluorene derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising same as effective ingredient for preventing or treating hcv-related disease |
| 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 |
| JP7720698B2 (ja) | 2018-04-04 | 2025-08-08 | アルビナス・オペレーションズ・インコーポレイテッド | タンパク質分解の調節因子および関連する使用方法 |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| CA3121140A1 (en) * | 2018-11-30 | 2020-06-04 | Glaxosmithkline Intellectual Property Development Limited | Compounds useful in hiv therapy |
| US20220096436A1 (en) | 2019-01-17 | 2022-03-31 | Debiopharm International S.A. | Combination product for the treatment of cancer |
| AU2020252216A1 (en) * | 2019-04-05 | 2021-11-04 | Hepagene Therapeutics (HK) Limited | Bivalent antagonists of inhibitors of apoptosis proteins |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 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 |
| KR20220054347A (ko) | 2019-08-26 | 2022-05-02 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 유도체로 유방암을 치료하는 방법 |
| CA3151770A1 (en) | 2019-09-25 | 2021-04-01 | Silvano BRIENZA | Dosing regimens for treatment of patients with locally advanced squamous cell carcinoma |
| US20230115837A1 (en) * | 2019-11-08 | 2023-04-13 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitor of apoptosis (iap) protein antagonists |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| JP2023541434A (ja) | 2020-09-14 | 2023-10-02 | アルビナス・オペレーションズ・インコーポレイテッド | エストロゲン受容体の標的化分解のための化合物の結晶性形態 |
| IL305835A (en) | 2021-03-15 | 2023-11-01 | Maze Therapeutics Inc | Glycogen synthase 1 (GYS1) inhibitors and methods of using them |
| EP4190452B1 (de) | 2021-12-01 | 2024-07-24 | Eppendorf SE | Abstandshalter zum halten von übereinandergestapelten pipettenspitzenträgern auf abstand voneinander |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| KR20250151412A (ko) | 2023-01-26 | 2025-10-21 | 아비나스 오퍼레이션스, 인코포레이티드 | 세레블론계 kras 분해 단백질 및 이와 관련된 용도 |
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| US5932566A (en) | 1994-06-16 | 1999-08-03 | Pfizer Inc. | Ansamycin derivatives as antioncogene and anticancer agents |
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| US6790785B1 (en) | 2000-09-15 | 2004-09-14 | The Board Of Trustees Of The University Of Illinois | Metal-assisted chemical etch porous silicon formation method |
| WO2003086470A2 (en) | 2002-04-17 | 2003-10-23 | Deutsches Krebsforschungszentrum | Smac-peptides as therapeutics against cancer and autoimmune diseases |
| US7138402B2 (en) | 2003-09-18 | 2006-11-21 | Conforma Therapeutics Corporation | Pyrrolopyrimidines and related analogs as HSP90-inhibitors |
| EP1723122B1 (en) * | 2004-03-01 | 2014-11-19 | Board of Regents, The University of Texas System | Dimeric small molecule potentiators of apoptosis |
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| PL1851200T3 (pl) * | 2005-02-25 | 2014-06-30 | Tetralogic Pharm Corp | Dimeryczne inhibitory IAP |
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| TWI543988B (zh) * | 2006-03-16 | 2016-08-01 | 科學製藥股份有限公司 | 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 |
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| 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 |
| US20110117081A1 (en) * | 2008-05-05 | 2011-05-19 | Aegera Therapeutics, Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
-
2010
- 2010-10-28 EP EP10830467.6A patent/EP2493879B1/en not_active Not-in-force
- 2010-10-28 US US12/914,840 patent/US8551955B2/en not_active Expired - Fee Related
- 2010-10-28 EP EP14167843.3A patent/EP2784076A1/en not_active Withdrawn
- 2010-10-28 WO PCT/US2010/054546 patent/WO2011059763A2/en not_active Ceased
- 2010-10-28 CA CA2789879A patent/CA2789879A1/en not_active Abandoned
- 2010-10-28 CN CN201080058719.0A patent/CN102958928B/zh not_active Expired - Fee Related
- 2010-10-28 JP JP2012537075A patent/JP5529282B2/ja not_active Expired - Fee Related
-
2013
- 2013-08-22 US US13/973,979 patent/US20130344026A1/en not_active Abandoned
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2014
- 2014-04-16 JP JP2014084316A patent/JP2014167006A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP2493879A4 (en) | 2013-04-03 |
| US20110195043A1 (en) | 2011-08-11 |
| JP2014167006A (ja) | 2014-09-11 |
| WO2011059763A3 (en) | 2011-10-06 |
| US20130344026A1 (en) | 2013-12-26 |
| CN102958928A (zh) | 2013-03-06 |
| CN102958928B (zh) | 2015-05-13 |
| WO2011059763A2 (en) | 2011-05-19 |
| EP2493879A2 (en) | 2012-09-05 |
| EP2493879B1 (en) | 2014-05-14 |
| US8551955B2 (en) | 2013-10-08 |
| CA2789879A1 (en) | 2011-05-19 |
| EP2784076A1 (en) | 2014-10-01 |
| JP2013509429A (ja) | 2013-03-14 |
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