CN102958928B - 二聚体smac模拟物 - Google Patents
二聚体smac模拟物 Download PDFInfo
- Publication number
- CN102958928B CN102958928B CN201080058719.0A CN201080058719A CN102958928B CN 102958928 B CN102958928 B CN 102958928B CN 201080058719 A CN201080058719 A CN 201080058719A CN 102958928 B CN102958928 B CN 102958928B
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- Prior art keywords
- ring
- alkyl
- group
- optionally substituted
- independently
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- 0 C[C@@](CCCN1C(C(*)(*=C)N(*)C(*)=O)=O)C1I*IIIC(*CC1)N1C(C(*)(*)N(*)C(*)=O)=O Chemical compound C[C@@](CCCN1C(C(*)(*=C)N(*)C(*)=O)=O)C1I*IIIC(*CC1)N1C(C(*)(*)N(*)C(*)=O)=O 0.000 description 5
- PFFNMSUCZWZXEO-UHFFFAOYSA-N CC(C(CC(C1)C(CC(C2)C3)(CC2(C2)C(C)=O)CC32C(C)=O)C1C(C)=O)=O Chemical compound CC(C(CC(C1)C(CC(C2)C3)(CC2(C2)C(C)=O)CC32C(C)=O)C1C(C)=O)=O PFFNMSUCZWZXEO-UHFFFAOYSA-N 0.000 description 1
- WTCIGZIYYSQRIO-UHFFFAOYSA-N CC(CC(C1)(F)F)N1I Chemical compound CC(CC(C1)(F)F)N1I WTCIGZIYYSQRIO-UHFFFAOYSA-N 0.000 description 1
- ZXULNOJBFFRYHH-UHFFFAOYSA-N CC(CC(C1)=O)N1I Chemical compound CC(CC(C1)=O)N1I ZXULNOJBFFRYHH-UHFFFAOYSA-N 0.000 description 1
- DHZSARNCWFKZHX-UHFFFAOYSA-N CC(CC(C1)F)N1I Chemical compound CC(CC(C1)F)N1I DHZSARNCWFKZHX-UHFFFAOYSA-N 0.000 description 1
- IBWWRXNFLWYPEN-UHFFFAOYSA-N CC(CC1)N1I Chemical compound CC(CC1)N1I IBWWRXNFLWYPEN-UHFFFAOYSA-N 0.000 description 1
- WDUZQEMCZZTDEB-UHFFFAOYSA-N CC(CSC1)N1I Chemical compound CC(CSC1)N1I WDUZQEMCZZTDEB-UHFFFAOYSA-N 0.000 description 1
- OYPIPTHCYGVCOE-UHFFFAOYSA-N CC(Cc1ccccc1C1)N1I Chemical compound CC(Cc1ccccc1C1)N1I OYPIPTHCYGVCOE-UHFFFAOYSA-N 0.000 description 1
- UCGGIDNDFRKFKY-UHFFFAOYSA-N CCC(C(C(C1)OC)c2c1cccc2)NC Chemical compound CCC(C(C(C1)OC)c2c1cccc2)NC UCGGIDNDFRKFKY-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
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- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/191—Tumor necrosis factors [TNF], e.g. lymphotoxin [LT], i.e. TNF-beta
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D401/00—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D403/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
- C07K14/4747—Apoptosis related proteins
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- 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
- C07K5/06—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
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- 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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Epidemiology (AREA)
- Zoology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Toxicology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- AIDS & HIV (AREA)
- Emergency Medicine (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102958928A CN102958928A (zh) | 2013-03-06 |
| CN102958928B true CN102958928B (zh) | 2015-05-13 |
Family
ID=43992315
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080058719.0A Expired - Fee Related CN102958928B (zh) | 2009-10-28 | 2010-10-28 | 二聚体smac模拟物 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US8551955B2 (https=) |
| EP (2) | EP2784076A1 (https=) |
| JP (2) | JP5529282B2 (https=) |
| CN (1) | CN102958928B (https=) |
| CA (1) | CA2789879A1 (https=) |
| WO (1) | WO2011059763A2 (https=) |
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|---|---|---|---|---|
| WO2014025759A1 (en) * | 2012-08-09 | 2014-02-13 | Bristol-Myers Squibb Company | Iap antagonists |
| US9422332B2 (en) * | 2012-08-15 | 2016-08-23 | Hoffmann-La Roche Inc. | Azaheterocycles as BIR2 and/or BIR3 inhibitors |
| US9603889B2 (en) * | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| US9309248B2 (en) * | 2012-10-11 | 2016-04-12 | Hoffmann-La Roche Inc. | Azaindolines |
| JP6333267B2 (ja) * | 2012-10-11 | 2018-05-30 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | アザインドリン |
| AU2013357493A1 (en) * | 2012-12-11 | 2015-04-30 | F. Hoffmann-La Roche Ag | Dimeric compounds |
| 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 |
| EP3019517A1 (en) * | 2013-07-12 | 2016-05-18 | Bristol-Myers Squibb Company | Iap antagonists |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP3143026B1 (en) | 2014-05-13 | 2024-07-10 | Novartis AG | Compounds and compositions for inducing chondrogenesis |
| 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 |
| 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 |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| CA2988436A1 (en) * | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
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| 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 |
| MX2019007646A (es) | 2016-12-23 | 2019-09-06 | Arvinas Operations Inc | Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso. |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
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| KR20210006356A (ko) | 2018-04-04 | 2021-01-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
| 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 |
| AR117206A1 (es) * | 2018-11-30 | 2021-07-21 | Glaxosmithkline Ip Dev Ltd | Derivados de octahidropirrolo[2,1-b][1,3]tiazepin-7-carboxamido útiles en la terapia para el vih y para el tratamiento del cáncer |
| WO2020148447A1 (en) | 2019-01-17 | 2020-07-23 | Debiopharm International S.A. | Combination product for the treatment of cancer |
| CN113677399B (zh) * | 2019-04-05 | 2024-10-11 | 和博医药有限公司 | 凋亡蛋白抑制剂的二价拮抗剂 |
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| MX2022003628A (es) | 2019-09-25 | 2022-07-21 | Debiopharm Int Sa | Regímenes de dosificación para el tratamiento de pacientes con carcinoma de células escamosas avanzado localmente. |
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| EP4190452B1 (de) | 2021-12-01 | 2024-07-24 | Eppendorf SE | Abstandshalter zum halten von übereinandergestapelten pipettenspitzenträgern auf abstand voneinander |
| 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 |
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- 2010-10-28 EP EP14167843.3A patent/EP2784076A1/en not_active Withdrawn
- 2010-10-28 CN CN201080058719.0A patent/CN102958928B/zh not_active Expired - Fee Related
- 2010-10-28 US US12/914,840 patent/US8551955B2/en not_active Expired - Fee Related
- 2010-10-28 JP JP2012537075A patent/JP5529282B2/ja not_active Expired - Fee Related
- 2010-10-28 CA CA2789879A patent/CA2789879A1/en not_active Abandoned
- 2010-10-28 WO PCT/US2010/054546 patent/WO2011059763A2/en not_active Ceased
- 2010-10-28 EP EP10830467.6A patent/EP2493879B1/en not_active Not-in-force
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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
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| WO1994000486A1 (en) * | 1992-06-20 | 1994-01-06 | The Wellcome Foundation Limited | Neuropeptide y antagonists |
| WO2008128121A1 (en) * | 2007-04-12 | 2008-10-23 | Joyant Pharmaceuticals, Inc. | Smac mimetic dimers and trimers useful as anti-cancer agents |
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| US20130344026A1 (en) | 2013-12-26 |
| JP5529282B2 (ja) | 2014-06-25 |
| CA2789879A1 (en) | 2011-05-19 |
| JP2013509429A (ja) | 2013-03-14 |
| EP2493879A2 (en) | 2012-09-05 |
| CN102958928A (zh) | 2013-03-06 |
| WO2011059763A3 (en) | 2011-10-06 |
| JP2014167006A (ja) | 2014-09-11 |
| US20110195043A1 (en) | 2011-08-11 |
| EP2784076A1 (en) | 2014-10-01 |
| EP2493879B1 (en) | 2014-05-14 |
| US8551955B2 (en) | 2013-10-08 |
| WO2011059763A2 (en) | 2011-05-19 |
| EP2493879A4 (en) | 2013-04-03 |
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