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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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- 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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- 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
- 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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- C—CHEMISTRY; METALLURGY
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- 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
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- 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
- C07D403/14—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
-
- 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
-
- 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)
- 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)
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 (enExample) |
| EP (2) | EP2784076A1 (enExample) |
| JP (2) | JP5529282B2 (enExample) |
| CN (1) | CN102958928B (enExample) |
| CA (1) | CA2789879A1 (enExample) |
| WO (1) | WO2011059763A2 (enExample) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9453048B2 (en) * | 2012-08-09 | 2016-09-27 | Bristol-Myers Squibb Company | IAP antagonists |
| CA2878106A1 (en) * | 2012-08-15 | 2014-02-20 | 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 |
| US9340573B2 (en) * | 2012-10-11 | 2016-05-17 | Hoffmann-La Roche Inc. | Azaindolines |
| MX2015004525A (es) * | 2012-10-11 | 2015-07-06 | Hoffmann La Roche | Azaindolinas. |
| PE20151083A1 (es) * | 2012-12-11 | 2015-08-06 | Hoffmann La Roche | Compuestos dimericos |
| 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 |
| CA2947031C (en) | 2014-05-13 | 2023-01-24 | 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 |
| KR102564925B1 (ko) | 2015-01-20 | 2023-08-07 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | 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 |
| CA3042260C (en) | 2016-11-01 | 2023-10-03 | Arvinas, Inc. | Tau-protein targeting protacs and associated methods of use |
| RS64976B1 (sr) | 2016-12-01 | 2024-01-31 | Arvinas Operations Inc | Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora |
| CN110741004B (zh) | 2016-12-23 | 2023-10-17 | 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 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| JP2020505327A (ja) | 2016-12-23 | 2020-02-20 | 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. | Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法 |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| 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 |
| AU2018211975B2 (en) | 2017-01-26 | 2022-05-26 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| 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 |
| 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 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| EP3886987B1 (en) * | 2018-11-30 | 2023-11-15 | 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 |
| JP7455141B2 (ja) * | 2019-04-05 | 2024-03-25 | へパジーン セラピューティクス (エイチケイ) リミテッド | アポトーシスタンパク質の阻害剤の二価拮抗薬 |
| 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 |
| CN114667147B (zh) | 2019-08-26 | 2024-09-06 | 阿尔维纳斯运营股份有限公司 | 用四氢萘衍生物作为雌激素受体降解剂的治疗乳腺癌的方法 |
| CN114727984A (zh) | 2019-09-25 | 2022-07-08 | 德彪药业国际股份公司 | 治疗患有局部晚期鳞状细胞癌的患者的给药方案 |
| WO2021092500A1 (en) * | 2019-11-08 | 2021-05-14 | 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 |
| CR20230162A (es) | 2020-09-14 | 2023-06-02 | Arvinas Operations Inc | Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógenos |
| 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 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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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| 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 |
| EP1495124A2 (en) | 2002-04-17 | 2005-01-12 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Smac-peptides as therapeutics against cancer and autoimmune diseases |
| US7138401B2 (en) | 2003-09-18 | 2006-11-21 | Conforma Therapeutics Corporation | 2-aminopurine analogs having HSP90-inhibiting activity |
| 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 |
| JP5122275B2 (ja) | 2004-03-23 | 2013-01-16 | ジェネンテック, インコーポレイテッド | Iapのアザビシクロ−オクタンインヒビター |
| ME02125B (me) | 2004-04-07 | 2013-04-30 | Novartis Ag | Inhibitori protein apoptoze (iap) |
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| ES2475207T3 (es) | 2004-07-15 | 2014-07-10 | Tetralogic Pharmaceuticals Corporation | Compuestos de unión a IAP |
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| EA012810B1 (ru) * | 2005-02-25 | 2009-12-30 | Тетралоджик Фармасеутикалс | Димерные ингибиторы ингибиторов белков апоптоза (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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- 2010-10-28 EP EP14167843.3A patent/EP2784076A1/en not_active Withdrawn
- 2010-10-28 US US12/914,840 patent/US8551955B2/en not_active Expired - Fee Related
- 2010-10-28 WO PCT/US2010/054546 patent/WO2011059763A2/en not_active Ceased
- 2010-10-28 JP JP2012537075A patent/JP5529282B2/ja not_active Expired - Fee Related
- 2010-10-28 EP EP10830467.6A patent/EP2493879B1/en not_active Not-in-force
- 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
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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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| US8551955B2 (en) | 2013-10-08 |
| EP2493879A4 (en) | 2013-04-03 |
| WO2011059763A2 (en) | 2011-05-19 |
| CA2789879A1 (en) | 2011-05-19 |
| EP2493879B1 (en) | 2014-05-14 |
| JP2014167006A (ja) | 2014-09-11 |
| US20130344026A1 (en) | 2013-12-26 |
| EP2784076A1 (en) | 2014-10-01 |
| EP2493879A2 (en) | 2012-09-05 |
| JP5529282B2 (ja) | 2014-06-25 |
| JP2013509429A (ja) | 2013-03-14 |
| CN102958928A (zh) | 2013-03-06 |
| US20110195043A1 (en) | 2011-08-11 |
| WO2011059763A3 (en) | 2011-10-06 |
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