JP4541882B2 - Ｓｍａｃタンパク質のアポトーシスタンパク質阻害物質（ｉａｐ）との結合に対するペプチド阻害剤 - Google Patents
Ｓｍａｃタンパク質のアポトーシスタンパク質阻害物質（ｉａｐ）との結合に対するペプチド阻害剤 Download PDFInfo
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- JP4541882B2 JP4541882B2 JP2004518651A JP2004518651A JP4541882B2 JP 4541882 B2 JP4541882 B2 JP 4541882B2 JP 2004518651 A JP2004518651 A JP 2004518651A JP 2004518651 A JP2004518651 A JP 2004518651A JP 4541882 B2 JP4541882 B2 JP 4541882B2
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D401/02—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 containing two hetero rings
- C07D401/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/06—Tripeptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- 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
- C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- 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
- 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
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
-
- 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
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
- C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
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- Pharmacology & Pharmacy (AREA)
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- Engineering & Computer Science (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39315002P | 2002-07-02 | 2002-07-02 | |
| PCT/EP2003/007005 WO2004005248A1 (en) | 2002-07-02 | 2003-07-01 | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006501181A JP2006501181A (ja) | 2006-01-12 |
| JP2006501181A5 JP2006501181A5 (enExample) | 2006-08-31 |
| JP4541882B2 true JP4541882B2 (ja) | 2010-09-08 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| JP2004518651A Expired - Fee Related JP4541882B2 (ja) | 2002-07-02 | 2003-07-01 | Ｓｍａｃタンパク質のアポトーシスタンパク質阻害物質（ｉａｐ）との結合に対するペプチド阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20060128632A1 (enExample) |
| EP (1) | EP1519918A1 (enExample) |
| JP (1) | JP4541882B2 (enExample) |
| CN (1) | CN100384819C (enExample) |
| AU (1) | AU2003249920A1 (enExample) |
| BR (1) | BR0312408A (enExample) |
| CA (1) | CA2491041A1 (enExample) |
| WO (1) | WO2004005248A1 (enExample) |
Families Citing this family (78)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US7291615B2 (en) | 2003-05-01 | 2007-11-06 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
| CN1933847A (zh) * | 2004-01-16 | 2007-03-21 | 密歇根大学董事会 | Smac肽模拟物及其应用 |
| EP1713542A2 (en) * | 2004-02-05 | 2006-10-25 | Novartis AG | COMBINATION OF (a) A DNA TOPOISOMERASE INHIBITOR AND (b) AN IAP INHIBITOR |
| US7345081B2 (en) | 2004-03-23 | 2008-03-18 | Genentech, Inc. | Azabicyclo-octane inhibitors of IAP |
| PL2253614T3 (pl) * | 2004-04-07 | 2013-03-29 | Novartis Ag | Inhibitory IAP |
| KR100926203B1 (ko) | 2004-07-02 | 2009-11-09 | 제넨테크, 인크. | Ｉａｐ의 억제제 |
| JP5230865B2 (ja) | 2004-07-15 | 2013-07-10 | 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 | Ｉａｐ結合性化合物 |
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| EA012810B1 (ru) | 2005-02-25 | 2009-12-30 | Тетралоджик Фармасеутикалс | Димерные ингибиторы ингибиторов белков апоптоза (iap) |
| DE102005017116A1 (de) | 2005-04-13 | 2006-10-26 | Novartis Ag | Hemmstoffe für Inhibitoren von Apoptose Proteinen (IAP) |
| WO2006122408A1 (en) | 2005-05-18 | 2006-11-23 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| US8318717B2 (en) | 2005-05-25 | 2012-11-27 | 2Curex | Compounds modifying apoptosis |
| WO2006128455A2 (en) | 2005-05-25 | 2006-12-07 | 2Curex Aps | Compounds modifying apoptosis |
| US20100256046A1 (en) * | 2009-04-03 | 2010-10-07 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| AU2006308453B9 (en) | 2005-10-25 | 2011-12-01 | Pharmascience Inc. | IAP BIR domain binding compounds |
| WO2007106192A2 (en) * | 2005-12-19 | 2007-09-20 | Genentech, Inc. | Inhibitors of iap |
| US20090005411A1 (en) * | 2005-12-20 | 2009-01-01 | Novartic Ag | Combinations of Organic Compounds |
| US7622496B2 (en) * | 2005-12-23 | 2009-11-24 | Zealand Pharma A/S | Modified lysine-mimetic compounds |
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| US20100143499A1 (en) * | 2006-07-24 | 2010-06-10 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| WO2008014240A2 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| JP5452223B2 (ja) * | 2006-07-24 | 2014-03-26 | 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 | Ｉａｐ阻害剤 |
| MX2009000824A (es) | 2006-07-24 | 2009-02-04 | Tetralogic Pharmaceuticals Cor | Antagonistas dimericos de las proteinas inhibidoras de la apoptosis. |
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| US20100056495A1 (en) * | 2006-07-24 | 2010-03-04 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| PE20110217A1 (es) | 2006-08-02 | 2011-04-01 | 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 |
| AU2007307763A1 (en) | 2006-10-12 | 2008-04-17 | Novartis Ag | Pyrrolydine derivatives as IAP inhibitors |
| KR20090087094A (ko) | 2006-11-28 | 2009-08-14 | 노파르티스 아게 | Ｉａｐ 억제제 및 ｆｌｔ3 억제제의 조합물 |
| CN101605786A (zh) * | 2006-12-19 | 2009-12-16 | 健泰科生物技术公司 | 细胞凋亡抑制剂的咪唑并吡啶抑制剂 |
| ES2558856T3 (es) | 2006-12-21 | 2016-02-09 | Zealand Pharma A/S | Síntesis de compuestos de pirrolidina |
| CA2684169C (en) * | 2007-04-12 | 2012-06-19 | Joyant Pharmaceuticals, Inc. | Smac mimetic dimers and trimers useful as anti-cancer agents |
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| IL325835A (en) | 2016-12-23 | 2026-03-01 | Univ Yale | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
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| CN110944719A (zh) * | 2017-07-25 | 2020-03-31 | 合帕吉恩治疗公司 | 凋亡蛋白的二聚肽抑制剂 |
| WO2019021289A1 (en) | 2017-07-27 | 2019-01-31 | The National Institute for Biotechnology in the Negev Ltd. | SMAC / DIABLO INHIBITORS USEFUL IN THE TREATMENT OF CANCER |
| 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 |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
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| WO2021041348A1 (en) | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| AU2021342287A1 (en) | 2020-09-14 | 2023-04-13 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| PE20260006A1 (es) | 2023-01-26 | 2026-01-06 | Arvinas Operations Inc | Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos |
| WO2025256500A1 (zh) * | 2024-06-11 | 2025-12-18 | 温州玮祎康泽生物科技有限公司 | Xiap e3连接酶作为肿瘤治疗靶点及其靶向化合物的应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5801012A (en) * | 1996-09-17 | 1998-09-01 | Northwestern University | Methods and compositions for generating angiostatin |
| AU7473500A (en) * | 1999-09-01 | 2001-03-26 | University Of Pittsburgh | Identification of peptides that facilitate uptake and cytoplasmic and/or nucleartransport of proteins, dna and viruses |
| US6992063B2 (en) * | 2000-09-29 | 2006-01-31 | The Trustees Of Princeton University | Compositions and method for regulating apoptosis |
| WO2002030959A2 (en) * | 2000-10-13 | 2002-04-18 | Abbott Laboratories | Peptides derived from smac (diablo) and methods of use therefor |
| DE10105041A1 (de) * | 2001-02-05 | 2002-08-14 | Tell Pharm Ag Hergiswil | Tripeptide und Tripeptid-Derivate für die Behandlung neurodegenerativer Krankheiten |
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- 2003-07-01 CA CA002491041A patent/CA2491041A1/en not_active Abandoned
- 2003-07-01 AU AU2003249920A patent/AU2003249920A1/en not_active Abandoned
- 2003-07-01 WO PCT/EP2003/007005 patent/WO2004005248A1/en not_active Ceased
- 2003-07-01 BR BR0312408-8A patent/BR0312408A/pt not_active IP Right Cessation
- 2003-07-01 EP EP03762570A patent/EP1519918A1/en not_active Withdrawn
- 2003-07-01 US US10/519,042 patent/US20060128632A1/en not_active Abandoned
- 2003-07-01 CN CNB038156571A patent/CN100384819C/zh not_active Expired - Fee Related
- 2003-07-01 JP JP2004518651A patent/JP4541882B2/ja not_active Expired - Fee Related
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| CA2491041A1 (en) | 2004-01-15 |
| EP1519918A1 (en) | 2005-04-06 |
| JP2006501181A (ja) | 2006-01-12 |
| CN100384819C (zh) | 2008-04-30 |
| CN1665784A (zh) | 2005-09-07 |
| BR0312408A (pt) | 2005-04-19 |
| US20060128632A1 (en) | 2006-06-15 |
| AU2003249920A1 (en) | 2004-01-23 |
| WO2004005248A1 (en) | 2004-01-15 |
| US20060052311A1 (en) | 2006-03-09 |
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