JP2010519318A5 - - Google Patents
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- Publication number
- JP2010519318A5 JP2010519318A5 JP2009551061A JP2009551061A JP2010519318A5 JP 2010519318 A5 JP2010519318 A5 JP 2010519318A5 JP 2009551061 A JP2009551061 A JP 2009551061A JP 2009551061 A JP2009551061 A JP 2009551061A JP 2010519318 A5 JP2010519318 A5 JP 2010519318A5
- Authority
- JP
- Japan
- Prior art keywords
- macrocycle
- peptidomimetic macrocycle
- peptidomimetic
- methyl
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000002678 macrocyclic compounds Chemical class 0.000 claims 52
- 239000000816 peptidomimetic Substances 0.000 claims 49
- 238000000034 method Methods 0.000 claims 37
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 239000003153 chemical reaction reagent Substances 0.000 claims 14
- 125000005647 linker group Chemical group 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 9
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 9
- 150000001413 amino acids Chemical class 0.000 claims 8
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 238000005710 macrocyclization reaction Methods 0.000 claims 8
- 108090000765 processed proteins & peptides Proteins 0.000 claims 8
- 229920001184 polypeptide Polymers 0.000 claims 7
- 239000002243 precursor Substances 0.000 claims 7
- 102000004196 processed proteins & peptides Human genes 0.000 claims 7
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 5
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 150000001345 alkine derivatives Chemical class 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims 3
- -1 macrocycle compound Chemical class 0.000 claims 3
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000004474 heteroalkylene group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 2
- 229920002521 macromolecule Polymers 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 238000010189 synthetic method Methods 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- JMHBRCHHTBVRNO-SSDOTTSWSA-N (2r)-2-amino-2-methylhex-5-ynoic acid Chemical compound OC(=O)[C@@](N)(C)CCC#C JMHBRCHHTBVRNO-SSDOTTSWSA-N 0.000 claims 1
- FSBNDYYRTZBHAN-ZCFIWIBFSA-N (2r)-2-amino-2-methylpent-4-ynoic acid Chemical compound OC(=O)[C@@](N)(C)CC#C FSBNDYYRTZBHAN-ZCFIWIBFSA-N 0.000 claims 1
- DGYHPLMPMRKMPD-SCSAIBSYSA-N (2r)-2-azaniumylpent-4-ynoate Chemical compound OC(=O)[C@H](N)CC#C DGYHPLMPMRKMPD-SCSAIBSYSA-N 0.000 claims 1
- JMHBRCHHTBVRNO-ZETCQYMHSA-N (2s)-2-amino-2-methylhex-5-ynoic acid Chemical compound OC(=O)[C@](N)(C)CCC#C JMHBRCHHTBVRNO-ZETCQYMHSA-N 0.000 claims 1
- WTFKXZRWELKUFM-VIFPVBQESA-N (2s)-2-amino-2-methyloct-7-ynoic acid Chemical compound OC(=O)[C@](N)(C)CCCCC#C WTFKXZRWELKUFM-VIFPVBQESA-N 0.000 claims 1
- FSBNDYYRTZBHAN-LURJTMIESA-N (2s)-2-amino-2-methylpent-4-ynoic acid Chemical compound OC(=O)[C@](N)(C)CC#C FSBNDYYRTZBHAN-LURJTMIESA-N 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- DGYHPLMPMRKMPD-UHFFFAOYSA-N L-propargyl glycine Natural products OC(=O)C(N)CC#C DGYHPLMPMRKMPD-UHFFFAOYSA-N 0.000 claims 1
- DGYHPLMPMRKMPD-BYPYZUCNSA-N L-propargylglycine Chemical group OC(=O)[C@@H](N)CC#C DGYHPLMPMRKMPD-BYPYZUCNSA-N 0.000 claims 1
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims 1
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 1
- HUZCMINOFBKDBN-NQPNHJOESA-N [(5r)-1,5-diamino-5-carboxyhexyl]-diazonioazanide Chemical compound OC(=O)[C@@](N)(C)CCCC(N)N=[N+]=[N-] HUZCMINOFBKDBN-NQPNHJOESA-N 0.000 claims 1
- QFLNJOIJUNDRFH-CNZKWPKMSA-N [(5r)-1,5-diamino-5-carboxypentyl]-diazonioazanide Chemical compound [N-]=[N+]=NC(N)CCC[C@@H](N)C(O)=O QFLNJOIJUNDRFH-CNZKWPKMSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000003125 aqueous solvent Substances 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 230000004071 biological effect Effects 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229960003104 ornithine Drugs 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 230000017854 proteolysis Effects 0.000 claims 1
- 239000003586 protic polar solvent Substances 0.000 claims 1
- 229910052707 ruthenium Inorganic materials 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
- 0 CC(*)=CCN=NN Chemical compound CC(*)=CCN=NN 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90307307P | 2007-02-23 | 2007-02-23 | |
| US60/903,073 | 2007-02-23 | ||
| PCT/US2008/054922 WO2008104000A2 (en) | 2007-02-23 | 2008-02-25 | Triazole macrocycle systems |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012063887A Division JP5657594B6 (ja) | 2007-02-23 | 2012-03-21 | トリアゾール大環状系 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010519318A JP2010519318A (ja) | 2010-06-03 |
| JP2010519318A5 true JP2010519318A5 (OSRAM) | 2011-04-14 |
| JP4997293B2 JP4997293B2 (ja) | 2012-08-08 |
Family
ID=39710801
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009551061A Expired - Fee Related JP4997293B2 (ja) | 2007-02-23 | 2008-02-25 | トリアゾール大環状系 |
| JP2014238716A Expired - Fee Related JP6046686B2 (ja) | 2007-02-23 | 2014-11-26 | トリアゾール大環状系 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014238716A Expired - Fee Related JP6046686B2 (ja) | 2007-02-23 | 2014-11-26 | トリアゾール大環状系 |
Country Status (10)
| Country | Link |
|---|---|
| US (6) | US7981999B2 (OSRAM) |
| EP (4) | EP3301108A1 (OSRAM) |
| JP (2) | JP4997293B2 (OSRAM) |
| CN (3) | CN109627287A (OSRAM) |
| AU (1) | AU2008218116B2 (OSRAM) |
| BR (1) | BRPI0807578A2 (OSRAM) |
| CA (1) | CA2678941C (OSRAM) |
| ES (3) | ES2398310T3 (OSRAM) |
| IL (2) | IL200532A (OSRAM) |
| WO (1) | WO2008104000A2 (OSRAM) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7192713B1 (en) | 1999-05-18 | 2007-03-20 | President And Fellows Of Harvard College | Stabilized compounds having secondary structure motifs |
| WO2005044839A2 (en) | 2003-11-05 | 2005-05-19 | Dana-Farber Cancer Institute, Inc. | Stabilized alpha helical peptides and uses thereof |
| WO2005118620A2 (en) * | 2004-05-27 | 2005-12-15 | New York University | Methods for preparing internally constraied peptides and peptidomimetics |
| JP2010510236A (ja) | 2006-11-15 | 2010-04-02 | ダナ−ファーバー キャンサー インスティテュート インク． | 安定化させたｍａｍｌペプチドおよびその使用法 |
| US7981998B2 (en) * | 2006-12-14 | 2011-07-19 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| WO2008076904A1 (en) | 2006-12-14 | 2008-06-26 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| CA2677045C (en) | 2007-01-31 | 2016-10-18 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| US7981999B2 (en) | 2007-02-23 | 2011-07-19 | Aileron Therapeutics, Inc. | Triazole macrocycle systems |
| KR101623985B1 (ko) * | 2007-03-28 | 2016-05-25 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 스티칭된 폴리펩티드 |
| EP2152294B1 (en) * | 2007-05-02 | 2017-07-26 | Dana-Farber Cancer Institute, Inc. | A bad bh3 domain peptide for use in treating or delaying the onset of diabetes. |
| JP5653219B2 (ja) * | 2007-12-31 | 2015-01-14 | ニューヨーク ユニバーシティ | 水素結合サロゲートをベースとする人工ヘリックスによるウイルス宿主膜融合の制御 |
| CN101980718A (zh) * | 2008-02-08 | 2011-02-23 | 爱勒让治疗公司 | 治疗性的拟肽大环化合物 |
| AU2014201269B2 (en) * | 2008-02-08 | 2016-09-15 | Aileron Therapeutics, Inc. | Therapeutic peptidomimetic macrocycles |
| US20090326192A1 (en) * | 2008-04-08 | 2009-12-31 | Aileron Therapeutics, Inc. | Biologically active peptidomimetic macrocycles |
| US20110144303A1 (en) * | 2008-04-08 | 2011-06-16 | Aileron Therapeutics, Inc. | Biologically Active Peptidomimetic Macrocycles |
| EP2285970A4 (en) * | 2008-06-03 | 2011-10-12 | Aileron Therapeutics Inc | COMPOSITIONS AND METHODS FOR REINFORCING THE CELL TRANSPORT OF BIOMOLECULES |
| WO2010011313A2 (en) | 2008-07-23 | 2010-01-28 | President And Fellows Of Harvard College | Ligation of stapled polypeptides |
| WO2010033617A2 (en) * | 2008-09-16 | 2010-03-25 | The Research Foundation Of State University Of New York | Stapled peptides and method of synthesis |
| CA2737922A1 (en) * | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| CN102884074A (zh) * | 2008-09-22 | 2013-01-16 | 爱勒让治疗公司 | 拟肽大环化合物 |
| WO2010034026A1 (en) * | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| JP2012503024A (ja) * | 2008-09-22 | 2012-02-02 | エルロン・セラピューティクス・インコーポレイテッド | ペプチド模倣大環状分子 |
| CA2737918A1 (en) * | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| AU2009294875C1 (en) | 2008-09-22 | 2015-05-14 | Aileron Therapeutics, Inc. | Methods for preparing purified polypeptide compositions |
| BRPI0920899A2 (pt) | 2008-11-24 | 2016-04-26 | Aileron Therapeutics Inc | macrociclos peptidomiméticos com propriedades melhoradas |
| JP2012515172A (ja) | 2009-01-14 | 2012-07-05 | エルロン・セラピューティクス・インコーポレイテッド | ペプチド模倣大環状分子 |
| BRPI1007320B1 (pt) * | 2009-01-23 | 2020-01-21 | Pacific Scient Energetic Materials Co | método para preparar um composto adequado para uso como explosivo primário |
| WO2010099436A1 (en) * | 2009-02-27 | 2010-09-02 | Mimetogen Pharmaceuticals, Inc. | Methods of treating retinitis pigmentosa |
| CA2768299C (en) | 2009-07-13 | 2018-03-20 | President And Fellows Of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| AU2010298338A1 (en) | 2009-09-22 | 2012-04-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US20110223149A1 (en) * | 2009-10-14 | 2011-09-15 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| CN102666565B (zh) * | 2009-11-16 | 2016-01-20 | 国家科学研究中心 | 用于纯化由固相肽合成法制备的肽的化合物和方法 |
| US9227995B2 (en) * | 2010-04-23 | 2016-01-05 | Øyvind Jacobsen | Peptides |
| KR102104762B1 (ko) | 2010-08-13 | 2020-04-24 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| US8957026B2 (en) | 2010-09-22 | 2015-02-17 | President And Fellows Of Harvard College | Beta-catenin targeting peptides and uses thereof |
| WO2012051405A1 (en) | 2010-10-13 | 2012-04-19 | Bristol-Myers Squibb Company | Methods for preparing macrocycles and macrocycle stabilized peptides |
| FR2967072B1 (fr) | 2010-11-05 | 2013-03-29 | Univ Dundee | Procede pour ameliorer la production de virus et semences vaccinales influenza |
| EP2637680B1 (en) | 2010-11-12 | 2017-03-01 | Dana-Farber Cancer Institute, Inc. | Cancer therapies |
| EP2651964B1 (en) | 2010-12-15 | 2018-02-28 | The Research Foundation of State University of New York | Cross-linked peptides and proteins, methods of making same, and uses thereof |
| WO2012173846A2 (en) * | 2011-06-06 | 2012-12-20 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US9487562B2 (en) | 2011-06-17 | 2016-11-08 | President And Fellows Of Harvard College | Stabilized polypeptides as regulators of RAB GTPase function |
| CN108929375A (zh) | 2011-10-18 | 2018-12-04 | 爱勒让治疗公司 | 拟肽大环化合物 |
| EP2771008A4 (en) | 2011-10-28 | 2015-04-08 | Merck Sharp & Dohme | MACROCYCLES FOR INCREASING P53 ACTIVITY AND USES THEREOF |
| WO2013071039A1 (en) * | 2011-11-09 | 2013-05-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| US9284283B2 (en) | 2012-02-02 | 2016-03-15 | Ensemble Therapeutics Corporation | Macrocyclic compounds for modulating IL-17 |
| EP2819688A4 (en) * | 2012-02-15 | 2015-10-28 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES CROSS-LINKED WITH TRIAZOLE AND THIOETHER |
| KR102112373B1 (ko) | 2012-02-15 | 2020-05-18 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방체 마크로사이클 |
| US9278984B2 (en) | 2012-08-08 | 2016-03-08 | Pacific Scientific Energetic Materials Company | Method for preparation of a lead-free primary explosive |
| PT2920197T (pt) | 2012-09-26 | 2021-06-11 | Harvard College | Péptidos agrafados com bloqueio de prolina e suas utilizações |
| KR20150082307A (ko) | 2012-11-01 | 2015-07-15 | 에일러론 테라퓨틱스 인코포레이티드 | 이치환 아미노산 및 이의 제조 및 사용 방법 |
| TW201429969A (zh) | 2012-12-20 | 2014-08-01 | Merck Sharp & Dohme | 作爲ｈｄｍ２抑制劑之經取代咪唑吡啶 |
| WO2014138429A2 (en) | 2013-03-06 | 2014-09-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and use thereof in regulating hif1alpha |
| US10081654B2 (en) | 2013-03-13 | 2018-09-25 | President And Fellows Of Harvard College | Stapled and stitched polypeptides and uses thereof |
| US10227390B2 (en) | 2013-06-14 | 2019-03-12 | President And Fellows Of Harvard College | Stabilized polypeptide insulin receptor modulators |
| JP6822839B2 (ja) | 2013-09-13 | 2021-01-27 | ザ・スクリップス・リサーチ・インスティテュート | 修飾された治療剤、及びその組成物 |
| EP3062810A4 (en) * | 2013-10-28 | 2017-05-03 | Naurex Inc. | Nmda receptor modulators and prodrugs, salts, and uses thereof |
| US10039809B2 (en) | 2013-12-18 | 2018-08-07 | The California Institute For Biomedical Research | Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof |
| JP6759109B2 (ja) | 2014-05-21 | 2020-09-23 | プレジデント アンド フェローズ オブ ハーバード カレッジ | Ｒａｓ抑制性ペプチドおよびその使用 |
| KR20230172035A (ko) * | 2014-09-11 | 2023-12-21 | 씨젠 인크. | 삼차 아민-함유 약물 물질의 표적화된 전달 |
| CN106999541A (zh) * | 2014-09-24 | 2017-08-01 | 艾瑞朗医疗公司 | 拟肽大环化合物及其用途 |
| SG10201902598VA (en) | 2014-09-24 | 2019-04-29 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and formulations thereof |
| MX2017011834A (es) | 2015-03-20 | 2018-04-11 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y usos de los mismos. |
| WO2017004548A1 (en) | 2015-07-01 | 2017-01-05 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| JP2018528217A (ja) | 2015-09-10 | 2018-09-27 | エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | Ｍｃｌ−１のモジュレーターとしてのペプチド模倣大環状分子 |
| ES2919323T3 (es) | 2015-12-04 | 2022-07-26 | Seagen Inc | Conjugados de compuestos de tubulisina cuaternizados |
| US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| US20170360881A1 (en) * | 2016-06-17 | 2017-12-21 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| WO2018017922A2 (en) | 2016-07-22 | 2018-01-25 | Massachusetts Institute Of Technology | Selective bfl-1 peptides |
| SG11201902818PA (en) * | 2016-09-30 | 2019-05-30 | Fujifilm Corp | Cyclic peptide, affinity chromatography support, labeled antibody, antibody drug conjugate, and pharmaceutical preparation |
| CA3073766A1 (en) | 2017-09-08 | 2019-03-14 | Seattle Genetics, Inc. | Process for the preparation of tubulysins and intermediates thereof |
| WO2019118893A1 (en) | 2017-12-15 | 2019-06-20 | Dana-Farber Cancer Institute, Inc. | Stabilized peptide-mediated targeted protein degradation |
| WO2020023502A1 (en) | 2018-07-23 | 2020-01-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| US11286299B2 (en) * | 2018-09-17 | 2022-03-29 | Massachusetts Institute Of Technology | Peptides selective for Bcl-2 family proteins |
| KR20240032010A (ko) | 2021-06-09 | 2024-03-08 | 더 스크립스 리서치 인스티튜트 | 장기 지속형 이중 gip/glp-1 펩타이드 접합체 및 사용 방법 |
Family Cites Families (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4000259A (en) * | 1975-06-16 | 1976-12-28 | American Home Products Corporation | Cyclic dodecapeptide analogs of somatostatin and intermediates |
| US4438270A (en) | 1977-07-11 | 1984-03-20 | Merrell Toraude Et Compagnie | α-Halomethyl derivatives of α-amino acids |
| US4191754A (en) * | 1979-02-28 | 1980-03-04 | Merck & Co., Inc. | Bicyclic somatostatin analogs |
| WO1989009233A1 (en) | 1988-03-24 | 1989-10-05 | Terrapin Technologies, Inc. | Molecular sticks for controlling protein conformation |
| US5650133A (en) * | 1990-01-19 | 1997-07-22 | Nycomed Salutar | Macrocyclic polyaza dichelates linked through ring nitrogens via an amide or ester functionality |
| CA2047042A1 (en) | 1990-07-19 | 1992-01-20 | John Hannah | Cyclic hiv principal neutralizing determinant peptides |
| US5364851A (en) * | 1991-06-14 | 1994-11-15 | International Synthecon, Llc | Conformationally restricted biologically active peptides, methods for their production and uses thereof |
| GB9114949D0 (en) | 1991-07-11 | 1991-08-28 | Smithkline Beecham Plc | Novel compounds |
| US5411860A (en) * | 1992-04-07 | 1995-05-02 | The Johns Hopkins University | Amplification of human MDM2 gene in human tumors |
| AU6770794A (en) | 1993-04-23 | 1994-11-21 | Herbert J. Evans | Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site |
| US5446128A (en) * | 1993-06-18 | 1995-08-29 | The Board Of Trustees Of The University Of Illinois | Alpha-helix mimetics and methods relating thereto |
| US5622852A (en) * | 1994-10-31 | 1997-04-22 | Washington University | Bcl-x/Bcl-2 associated cell death regulator |
| US6287787B1 (en) * | 1993-11-24 | 2001-09-11 | Torrey Pines Institute For Molecular Studies | Dimeric oligopeptide mixture sets |
| US5824483A (en) * | 1994-05-18 | 1998-10-20 | Pence Inc. | Conformationally-restricted combinatiorial library composition and method |
| US5770377A (en) * | 1994-07-20 | 1998-06-23 | University Of Dundee | Interruption of binding of MDM2 and P53 protein and therapeutic application thereof |
| US6169073B1 (en) * | 1995-02-16 | 2001-01-02 | Bayer Corporation | Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function |
| US5675001A (en) * | 1995-03-14 | 1997-10-07 | Hoffman/Barrett, L.L.C. | Heteroatom-functionalized porphyrazines and multimetallic complexes and polymers derived therefrom |
| MX9708500A (es) | 1995-05-04 | 1998-02-28 | Scripps Research Inst | Sintesis de proteinas mediante ligacion quimica nativa. |
| US5811515A (en) * | 1995-06-12 | 1998-09-22 | California Institute Of Technology | Synthesis of conformationally restricted amino acids, peptides, and peptidomimetics by catalytic ring closing metathesis |
| US5840833A (en) * | 1995-10-27 | 1998-11-24 | Molecumetics, Ltd | Alpha-helix mimetics and methods relating thereto |
| US5849954A (en) * | 1996-01-18 | 1998-12-15 | Research Corporation Technologies, Inc. | Method of peptide synthesis |
| US5849691A (en) | 1996-02-20 | 1998-12-15 | The United States Of America As Represented By The Department Of Health And Human Services | Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II |
| US5817752A (en) * | 1996-06-06 | 1998-10-06 | La Jolla Pharmaceutical Company | Cyclic polypeptides comprising a thioether linkage and methods for their preparation |
| US5663316A (en) * | 1996-06-18 | 1997-09-02 | Clontech Laboratories, Inc. | BBC6 gene for regulation of cell death |
| US7083983B2 (en) | 1996-07-05 | 2006-08-01 | Cancer Research Campaign Technology Limited | Inhibitors of the interaction between P53 and MDM2 |
| US5955593A (en) * | 1996-09-09 | 1999-09-21 | Washington University | BH3 interacting domain death agonist |
| US5965703A (en) * | 1996-09-20 | 1999-10-12 | Idun Pharmaceuticals | Human bad polypeptides, encoding nucleic acids and methods of use |
| US5856445A (en) * | 1996-10-18 | 1999-01-05 | Washington University | Serine substituted mutants of BCL-XL /BCL-2 associated cell death regulator |
| US6271198B1 (en) * | 1996-11-06 | 2001-08-07 | Genentech, Inc. | Constrained helical peptides and methods of making same |
| CA2286867A1 (en) | 1997-04-11 | 1998-10-22 | Eli Lilly And Company | Combinatorial libraries of peptidomimetic macrocycles and processes therefor |
| JP2001524301A (ja) * | 1997-09-17 | 2001-12-04 | ザ・ワルター・アンド・エリザ・ホール・インスティテュート・オヴ・メディカル・リサーチ | 新規治療用分子 |
| US6326354B1 (en) * | 1998-08-19 | 2001-12-04 | Washington University | Modulation of apoptosis with bid |
| WO2000052210A2 (en) | 1999-03-01 | 2000-09-08 | Variagenics, Inc. | Methods for targeting rna molecules |
| CA2368431C (en) * | 1999-03-29 | 2006-01-24 | The Procter & Gamble Company | Melanocortin receptor ligands |
| US6713280B1 (en) * | 1999-04-07 | 2004-03-30 | Thomas Jefferson University | Enhancement of peptide cellular uptake |
| US7192713B1 (en) | 1999-05-18 | 2007-03-20 | President And Fellows Of Harvard College | Stabilized compounds having secondary structure motifs |
| DE10009341A1 (de) * | 2000-02-22 | 2001-09-06 | Florian Kern | Verfahren zur antigen-spezifischen Stimulation von T-Lymphozyten |
| AU2001284942A1 (en) * | 2000-08-16 | 2002-02-25 | Georgetown University Medical Center | Small molecule inhibitors targeted at bcl-2 |
| US20050054770A1 (en) | 2001-03-09 | 2005-03-10 | Spatola Arno F. | Helicomimetics and stabilized lxxll peptidomimetics |
| US20040106548A1 (en) * | 2001-09-07 | 2004-06-03 | Schmidt Michelle A | Conformationally constrained labeled peptides for imaging and therapy |
| CA2471719A1 (en) * | 2001-12-31 | 2003-07-17 | Dana-Farber Cancer Institute, Inc. | Method of treating apoptosis and compositions thereof |
| AU2003207940A1 (en) | 2002-01-03 | 2003-07-30 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Conformationally constrained c-backbone cyclic peptides |
| WO2003070892A2 (en) | 2002-02-15 | 2003-08-28 | The Regents Of The University Of Michigan | Inhibitors of rgs proteins |
| US20030166138A1 (en) * | 2002-02-21 | 2003-09-04 | Todd Kinsella | Cyclic peptides and analogs useful to treat allergies |
| DK2226316T3 (en) * | 2002-05-30 | 2016-04-11 | Scripps Research Inst | Copper catalyzed ligation of azides and acetylenes |
| US20060051846A1 (en) | 2002-09-06 | 2006-03-09 | Kaneka Corporation | Process for producing l-alpha-methylcysteine derivative |
| WO2004022580A2 (en) * | 2002-09-09 | 2004-03-18 | Dana-Farber Cancer Institute, Inc. | Bh3 peptides and method of use thereof |
| KR100996996B1 (ko) * | 2002-11-07 | 2010-11-25 | 코산 바이오사이언시즈, 인코포레이티드 | 트랜스-9,10-디히드로에포틸론 ｃ 및 ｄ, 그것의 유사체 및 그것의 제조 방법 |
| WO2004058804A1 (en) | 2002-12-24 | 2004-07-15 | Walter And Eliza Hall Institute Of Medical Research | Peptides and therapeutic uses thereof |
| EP1452868A2 (en) | 2003-02-27 | 2004-09-01 | Pepscan Systems B.V. | Method for selecting a candidate drug compound |
| AU2003902743A0 (en) * | 2003-06-02 | 2003-06-19 | Promics Pty Limited | Process for the preparation of cyclic peptides |
| WO2005007675A2 (en) * | 2003-07-09 | 2005-01-27 | The Scripps Research Institute | TRIAZOLE ϵ-AMINO ACIDS |
| GB0317815D0 (en) | 2003-07-30 | 2003-09-03 | Amersham Health As | Imaging agents |
| DE602004014170D1 (de) * | 2003-10-03 | 2008-07-10 | Merck & Co Inc | Benzylether- und benzylamino-beta-sekretase-hemmer zur behandlung von alzheimer-krankheit |
| JP2007537989A (ja) | 2003-10-16 | 2007-12-27 | アプラーゲン ゲゼルシャフト ミット ベシュレンクテル ハフツング | 安定化ペプチド |
| WO2005044839A2 (en) * | 2003-11-05 | 2005-05-19 | Dana-Farber Cancer Institute, Inc. | Stabilized alpha helical peptides and uses thereof |
| US8193310B2 (en) | 2004-03-19 | 2012-06-05 | The University Of Queensland | Alpha helical mimics, their uses and methods for their production |
| WO2005118620A2 (en) | 2004-05-27 | 2005-12-15 | New York University | Methods for preparing internally constraied peptides and peptidomimetics |
| CN100335467C (zh) | 2004-06-04 | 2007-09-05 | 中国科学院上海有机化学研究所 | 一锅法区域选择性合成5－碘代－1，4－二取代－1，2，3－三氮唑化合物 |
| EP1602663A1 (en) * | 2004-06-04 | 2005-12-07 | Chiralix B.V. | Triazole-linked glycoamino acids and glycopeptides |
| DE602005014804D1 (de) * | 2004-10-29 | 2009-07-16 | Schering Corp | Substituierte 5-carboxyamidpyrazoles und ä1,2,4ütriazole als viruzide |
| EP1844337B1 (en) | 2005-01-24 | 2013-07-03 | Pepscan Systems B.V. | Binding compounds, immunogenic compounds and peptidomimetics |
| US20070020620A1 (en) * | 2005-07-14 | 2007-01-25 | Finn M G | Compositions and methods for coupling a plurality of compounds to a scaffold |
| US20080213175A1 (en) * | 2006-09-15 | 2008-09-04 | Kolb Hartmuth C | Click chemistry-derived cyclic peptidomimetics as integrin markers |
| JP2010510236A (ja) | 2006-11-15 | 2010-04-02 | ダナ−ファーバー キャンサー インスティテュート インク． | 安定化させたｍａｍｌペプチドおよびその使用法 |
| WO2008076904A1 (en) | 2006-12-14 | 2008-06-26 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| US7981998B2 (en) * | 2006-12-14 | 2011-07-19 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| CA2677045C (en) | 2007-01-31 | 2016-10-18 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| US7981999B2 (en) | 2007-02-23 | 2011-07-19 | Aileron Therapeutics, Inc. | Triazole macrocycle systems |
| KR101623985B1 (ko) | 2007-03-28 | 2016-05-25 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 스티칭된 폴리펩티드 |
| EP2152294B1 (en) | 2007-05-02 | 2017-07-26 | Dana-Farber Cancer Institute, Inc. | A bad bh3 domain peptide for use in treating or delaying the onset of diabetes. |
| JP5653219B2 (ja) | 2007-12-31 | 2015-01-14 | ニューヨーク ユニバーシティ | 水素結合サロゲートをベースとする人工ヘリックスによるウイルス宿主膜融合の制御 |
| ES2563027T3 (es) | 2008-01-07 | 2016-03-10 | Amgen Inc. | Método para fabricación de moléculas heterodímeras Fc de anticuerpos utilizando efectos de conducción electrostática |
| CN101980718A (zh) * | 2008-02-08 | 2011-02-23 | 爱勒让治疗公司 | 治疗性的拟肽大环化合物 |
| US20090326192A1 (en) * | 2008-04-08 | 2009-12-31 | Aileron Therapeutics, Inc. | Biologically active peptidomimetic macrocycles |
| US20110144303A1 (en) | 2008-04-08 | 2011-06-16 | Aileron Therapeutics, Inc. | Biologically Active Peptidomimetic Macrocycles |
| EP2285970A4 (en) | 2008-06-03 | 2011-10-12 | Aileron Therapeutics Inc | COMPOSITIONS AND METHODS FOR REINFORCING THE CELL TRANSPORT OF BIOMOLECULES |
| WO2010011313A2 (en) | 2008-07-23 | 2010-01-28 | President And Fellows Of Harvard College | Ligation of stapled polypeptides |
| CN102216322A (zh) | 2008-09-18 | 2011-10-12 | 纽约大学 | 用基于氢键替代的螺旋抑制HIF-1α和p300/CBP之间的相互作用 |
| CN102884074A (zh) | 2008-09-22 | 2013-01-16 | 爱勒让治疗公司 | 拟肽大环化合物 |
| AU2009294875C1 (en) * | 2008-09-22 | 2015-05-14 | Aileron Therapeutics, Inc. | Methods for preparing purified polypeptide compositions |
| WO2010034026A1 (en) | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| JP2012503024A (ja) | 2008-09-22 | 2012-02-02 | エルロン・セラピューティクス・インコーポレイテッド | ペプチド模倣大環状分子 |
| CA2737922A1 (en) * | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| CA2737918A1 (en) | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| BRPI0920899A2 (pt) * | 2008-11-24 | 2016-04-26 | Aileron Therapeutics Inc | macrociclos peptidomiméticos com propriedades melhoradas |
| JP2012515172A (ja) | 2009-01-14 | 2012-07-05 | エルロン・セラピューティクス・インコーポレイテッド | ペプチド模倣大環状分子 |
| CA2768299C (en) | 2009-07-13 | 2018-03-20 | President And Fellows Of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| AU2010298338A1 (en) | 2009-09-22 | 2012-04-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US20110223149A1 (en) | 2009-10-14 | 2011-09-15 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| KR102104762B1 (ko) | 2010-08-13 | 2020-04-24 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| ES2586411T3 (es) | 2011-03-04 | 2016-10-14 | New York University | Macrociclos sustitutos de enlace de hidrógeno como moduladores de Ras |
| WO2012173846A2 (en) | 2011-06-06 | 2012-12-20 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| WO2013033645A1 (en) | 2011-08-31 | 2013-03-07 | New York University | Thioether-,ether-, and alkylamine-linked hydrogen bond surrogate pertidomimentics |
| CN108929375A (zh) | 2011-10-18 | 2018-12-04 | 爱勒让治疗公司 | 拟肽大环化合物 |
| WO2013059530A2 (en) | 2011-10-18 | 2013-04-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| EP2819688A4 (en) | 2012-02-15 | 2015-10-28 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES CROSS-LINKED WITH TRIAZOLE AND THIOETHER |
| KR102112373B1 (ko) | 2012-02-15 | 2020-05-18 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방체 마크로사이클 |
| KR20150082307A (ko) | 2012-11-01 | 2015-07-15 | 에일러론 테라퓨틱스 인코포레이티드 | 이치환 아미노산 및 이의 제조 및 사용 방법 |
| WO2014138429A2 (en) | 2013-03-06 | 2014-09-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and use thereof in regulating hif1alpha |
| WO2015157508A1 (en) | 2014-04-09 | 2015-10-15 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles with pth activity |
| CN106999541A (zh) | 2014-09-24 | 2017-08-01 | 艾瑞朗医疗公司 | 拟肽大环化合物及其用途 |
| SG10201902598VA (en) | 2014-09-24 | 2019-04-29 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and formulations thereof |
| MX2017011834A (es) | 2015-03-20 | 2018-04-11 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y usos de los mismos. |
| WO2017004548A1 (en) | 2015-07-01 | 2017-01-05 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| AU2016287754B2 (en) | 2015-07-02 | 2021-02-25 | Dana-Farber Cancer Institute, Inc. | Stabilized anti-microbial peptides |
| US20170037105A1 (en) | 2015-08-03 | 2017-02-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US20170114098A1 (en) | 2015-09-03 | 2017-04-27 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| JP2018528217A (ja) | 2015-09-10 | 2018-09-27 | エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | Ｍｃｌ−１のモジュレーターとしてのペプチド模倣大環状分子 |
| JP2019520304A (ja) | 2016-03-21 | 2019-07-18 | エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | ペプチド模倣大環状分子に関するコンパニオン診断ツール |
| WO2017205786A1 (en) | 2016-05-27 | 2017-11-30 | Aileron Therapeutics, Inc. | Cell permeable peptidomimetic macrocycles |
| US20170360881A1 (en) | 2016-06-17 | 2017-12-21 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
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