JP2010519318A5 - - Google Patents
Download PDFInfo
- 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 (enExample) | 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 (enExample) |
| EP (4) | EP2114428B1 (enExample) |
| JP (2) | JP4997293B2 (enExample) |
| CN (3) | CN109627287A (enExample) |
| AU (1) | AU2008218116B2 (enExample) |
| BR (1) | BRPI0807578A2 (enExample) |
| CA (1) | CA2678941C (enExample) |
| ES (3) | ES2398310T3 (enExample) |
| IL (2) | IL200532A (enExample) |
| WO (1) | WO2008104000A2 (enExample) |
Families Citing this family (75)
| 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 |
| EP1680443B9 (en) * | 2003-11-05 | 2014-09-03 | 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 |
| CA2686827C (en) * | 2006-12-14 | 2014-09-16 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| US7981998B2 (en) * | 2006-12-14 | 2011-07-19 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| US8889632B2 (en) | 2007-01-31 | 2014-11-18 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| CN109627287A (zh) | 2007-02-23 | 2019-04-16 | 爱勒让治疗公司 | 三唑大环系统 |
| EP2508531B1 (en) | 2007-03-28 | 2016-10-19 | President and Fellows of Harvard College | Stitched polypeptides |
| US10716828B2 (en) * | 2007-05-02 | 2020-07-21 | Dana-Farber Cancer Institute, Inc. | Methods of modulating cellular homeostatic pathways and cellular survival |
| WO2009110952A2 (en) * | 2007-12-31 | 2009-09-11 | New York University | Control of viral-host membrane fusion with hydrogen bond surrogate-based artificial helices |
| BRPI0907754A2 (pt) * | 2008-02-08 | 2015-07-21 | Aileron Therapeutics Inc | Macrociclos peptidomiméticos terapêuticos |
| 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 |
| WO2009149214A2 (en) * | 2008-06-03 | 2009-12-10 | Aileron Therapeutics, Inc. | Compositions and methods for enhancing cellular transport of biomolecules |
| EP2356139A4 (en) * | 2008-07-23 | 2013-01-09 | Harvard College | LIGURE COMBINED POLYPEPTIDES |
| US8586707B2 (en) | 2008-09-16 | 2013-11-19 | The Research Foundation Of State University Of New York | Stapled peptides and method of synthesis |
| CA2737918A1 (en) * | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| CN102203126A (zh) * | 2008-09-22 | 2011-09-28 | 爱勒让治疗公司 | 用于制备纯化的多肽组合物的方法 |
| CA2737916A1 (en) * | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| AU2009294869A1 (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 |
| US8524653B2 (en) * | 2008-09-22 | 2013-09-03 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| WO2010060112A1 (en) | 2008-11-24 | 2010-05-27 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles with improved properties |
| EP2376100B1 (en) | 2009-01-14 | 2017-10-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| ES2684169T3 (es) * | 2009-01-23 | 2018-10-01 | Pacific Scientific Energetic Materials Company | Preparación de un explosivo primario exento de plomo |
| AU2010217889B2 (en) * | 2009-02-27 | 2014-12-18 | Mimetogen Pharmaceuticals Inc. | Peptidomimetic cyclic compounds for treating retinitis pigmentosa |
| WO2011008260A2 (en) | 2009-07-13 | 2011-01-20 | President And Fellows Of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| CA2774973A1 (en) | 2009-09-22 | 2011-03-31 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| BR112012008831A2 (pt) * | 2009-10-14 | 2019-09-24 | Aileron Therapeutics Inc | macrociclos de peptideomiméticos aprimorados. |
| WO2011058188A1 (en) * | 2009-11-16 | 2011-05-19 | Centre National De La Recherche Scientifique - Cnrs - | Compounds and methods for purifying peptides produced by solid phase peptide synthesis |
| US9227995B2 (en) * | 2010-04-23 | 2016-01-05 | Øyvind Jacobsen | Peptides |
| SI2603600T1 (sl) | 2010-08-13 | 2019-04-30 | Aileron Therapeutics, Inc. | Peptidomimetični makrocikli |
| WO2012040459A2 (en) | 2010-09-22 | 2012-03-29 | 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 |
| US9029332B2 (en) | 2010-12-15 | 2015-05-12 | The Research Foundation For The 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 |
| WO2012174423A1 (en) | 2011-06-17 | 2012-12-20 | President And Fellows Of Harvard College | Stabilized polypeptides as regulators of rab gtpase function |
| TW201806968A (zh) | 2011-10-18 | 2018-03-01 | 艾利倫治療公司 | 擬肽巨環化合物 |
| US8987274B2 (en) | 2011-10-28 | 2015-03-24 | Merck Sharp & Dohme Corp | Macrocycles that increase p53 activity and the uses thereof |
| WO2013071039A1 (en) * | 2011-11-09 | 2013-05-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| EP2809660B1 (en) | 2012-02-02 | 2016-01-20 | Ensemble Therapeutics Corporation | Macrocyclic compounds for modulating il-17 |
| KR102112373B1 (ko) | 2012-02-15 | 2020-05-18 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방체 마크로사이클 |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| US9278984B2 (en) | 2012-08-08 | 2016-03-08 | Pacific Scientific Energetic Materials Company | Method for preparation of a lead-free primary explosive |
| CA3113959A1 (en) | 2012-09-26 | 2014-04-03 | President And Fellows Of Harvard College | Proline-locked stapled peptides and uses thereof |
| WO2014071241A1 (en) | 2012-11-01 | 2014-05-08 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
| WO2014100065A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| WO2014138429A2 (en) | 2013-03-06 | 2014-09-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and use thereof in regulating hif1alpha |
| EP3782638A1 (en) | 2013-03-13 | 2021-02-24 | President and Fellows of Harvard College | Stapled and stitched polypeptides and uses thereof |
| WO2014201370A1 (en) | 2013-06-14 | 2014-12-18 | President And Fellows Of Harvard College | Stabilized polypeptide insulin receptor modulators |
| WO2015038938A1 (en) | 2013-09-13 | 2015-03-19 | The California Institute For Biomedical Research | Modified therapeutic agents and compositions thereof |
| US9745342B2 (en) * | 2013-10-28 | 2017-08-29 | 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 |
| CN114805527A (zh) | 2014-05-21 | 2022-07-29 | 哈佛大学的校长及成员们 | Ras抑制肽和其用途 |
| HRP20241124T1 (hr) * | 2014-09-11 | 2024-11-22 | Seagen Inc. | Ciljana isporuka lijekovitih tvari koje sadrže tercijarni amin |
| BR112017005598A2 (pt) * | 2014-09-24 | 2017-12-12 | Aileron Therapeutics Inc | macrociclos peptidomiméticos e usos dos mesmos |
| JP2018503595A (ja) | 2014-09-24 | 2018-02-08 | 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およびその製剤 |
| WO2016154058A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| US10059741B2 (en) | 2015-07-01 | 2018-08-28 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US10023613B2 (en) | 2015-09-10 | 2018-07-17 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles as modulators of MCL-1 |
| US11229708B2 (en) | 2015-12-04 | 2022-01-25 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| 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 |
| US11198715B2 (en) | 2016-07-22 | 2021-12-14 | Massachusetts Institute Of Technology | Selective Bfl-1 peptides |
| CA3036768A1 (en) | 2016-09-30 | 2018-04-05 | Fujifilm Corporation | Cyclic peptide, affinity chromatography support, labeled antibody, antibody drug conjugate, and pharmaceutical preparation |
| MA50124A (fr) | 2017-09-08 | 2020-07-15 | Seattle Genetics Inc | Procédé de préparation de tubulysines et d'intermédiaires de celles-ci |
| CN120118207A (zh) | 2017-12-15 | 2025-06-10 | 丹娜-法伯癌症研究院有限公司 | 稳定肽-介导的靶向蛋白降解 |
| US11091522B2 (en) | 2018-07-23 | 2021-08-17 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| WO2020060975A1 (en) * | 2018-09-17 | 2020-03-26 | Massachusetts Institute Of Technology | Peptides selective for bcl-2 family proteins |
| EP4069726A4 (en) | 2019-12-04 | 2024-03-20 | The Scripps Research Institute | GLP2 RECEPTOR AGONISTS AND METHOD OF USE |
| AU2022289610A1 (en) | 2021-06-09 | 2024-01-25 | The Scripps Research Institute | Long-acting dual gip/glp-1 peptide conjugates and methods of use |
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 |
| AU3439589A (en) | 1988-03-24 | 1989-10-16 | Terrapin Diagnostics, 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 |
| WO1994025482A1 (en) | 1993-04-23 | 1994-11-10 | Evans Herbert J | 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 |
| DK0832096T3 (da) | 1995-05-04 | 2001-10-01 | Scripps Research Inst | Syntese af proteiner ved nativ kemisk ligering |
| 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 |
| AU6895598A (en) | 1997-04-11 | 1998-11-11 | Eli Lilly And Company | Combinatorial libraries of peptidomimetic macrocycles and processes therefor |
| US7064193B1 (en) | 1997-09-17 | 2006-06-20 | The Walter And Eliza Hall Institute Of Medical Research | Therapeutic molecules |
| US6326354B1 (en) | 1998-08-19 | 2001-12-04 | Washington University | Modulation of apoptosis with bid |
| CA2363077A1 (en) | 1999-03-01 | 2000-09-08 | Variagenics, Inc. | Methods for targeting rna molecules |
| HK1044954B (en) | 1999-03-29 | 2008-11-21 | 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 |
| US6703382B2 (en) | 2000-08-16 | 2004-03-09 | Georgetown University Medical Center | Small molecule inhibitors targeted at Bcl-2 |
| WO2002072597A2 (en) | 2001-03-09 | 2002-09-19 | University Of Louisville | Helicomimetics and stabilized lxxll peptidomimetics |
| US20040106548A1 (en) | 2001-09-07 | 2004-06-03 | Schmidt Michelle A | Conformationally constrained labeled peptides for imaging and therapy |
| WO2003057158A2 (en) | 2001-12-31 | 2003-07-17 | Dana-Farber Cancer Institute, Inc. | Method of treating apoptosis and compositions thereof |
| WO2003059933A2 (en) | 2002-01-03 | 2003-07-24 | 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 |
| US7375234B2 (en) | 2002-05-30 | 2008-05-20 | The Scripps Research Institute | Copper-catalysed ligation of azides and acetylenes |
| WO2004022766A1 (ja) | 2002-09-06 | 2004-03-18 | Kaneka Corporation | Ｌ−αーメチルシステイン誘導体の製造方法 |
| CA2496400A1 (en) | 2002-09-09 | 2004-03-18 | Dana-Farber Cancer Institute, Inc. | Bh3 peptides and method of use thereof |
| ATE452888T1 (de) * | 2002-11-07 | 2010-01-15 | Kosan Biosciences Inc | Trans-9,10-dehydroepothilon c und d, analoga davon und verfahren zu deren herstellung |
| 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 |
| WO2005032471A2 (en) * | 2003-10-03 | 2005-04-14 | Merck & Co., Inc. | Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease |
| US20070207947A1 (en) | 2003-10-16 | 2007-09-06 | Aplagen Gmbh | Stabilized Peptides |
| EP1680443B9 (en) | 2003-11-05 | 2014-09-03 | 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 |
| JP4762995B2 (ja) * | 2004-10-29 | 2011-08-31 | シェーリング コーポレイション | 抗ウイルス物質としての置換５−カルボキシアミドピラゾールおよび置換［１，２，４］トリアゾール |
| ES2428869T3 (es) | 2005-01-24 | 2013-11-12 | Pepscan Systems B.V. | Compuestos de unión, compuestos inmunógenos y peptidomiméticos |
| US20070020620A1 (en) * | 2005-07-14 | 2007-01-25 | Finn M G | Compositions and methods for coupling a plurality of compounds to a scaffold |
| WO2008033557A2 (en) * | 2006-09-15 | 2008-03-20 | Siemens Medical Solutions Usa, Inc. | 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 |
| CA2686827C (en) | 2006-12-14 | 2014-09-16 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| US7981998B2 (en) | 2006-12-14 | 2011-07-19 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| US8889632B2 (en) | 2007-01-31 | 2014-11-18 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| CN109627287A (zh) | 2007-02-23 | 2019-04-16 | 爱勒让治疗公司 | 三唑大环系统 |
| EP2508531B1 (en) | 2007-03-28 | 2016-10-19 | President and Fellows of Harvard College | Stitched polypeptides |
| US10716828B2 (en) | 2007-05-02 | 2020-07-21 | Dana-Farber Cancer Institute, Inc. | Methods of modulating cellular homeostatic pathways and cellular survival |
| WO2009110952A2 (en) | 2007-12-31 | 2009-09-11 | New York University | Control of viral-host membrane fusion with hydrogen bond surrogate-based artificial helices |
| EP3663318A1 (en) | 2008-01-07 | 2020-06-10 | Amgen Inc. | Method for making antibody fc-heterodimeric molecules using electrostatic steering effects |
| BRPI0907754A2 (pt) | 2008-02-08 | 2015-07-21 | Aileron Therapeutics Inc | Macrociclos peptidomiméticos terapêuticos |
| US20110144303A1 (en) | 2008-04-08 | 2011-06-16 | Aileron Therapeutics, Inc. | Biologically Active Peptidomimetic Macrocycles |
| US20090326192A1 (en) | 2008-04-08 | 2009-12-31 | Aileron Therapeutics, Inc. | Biologically active peptidomimetic macrocycles |
| WO2009149214A2 (en) | 2008-06-03 | 2009-12-10 | Aileron Therapeutics, Inc. | Compositions and methods for enhancing cellular transport of biomolecules |
| EP2356139A4 (en) | 2008-07-23 | 2013-01-09 | Harvard College | LIGURE COMBINED POLYPEPTIDES |
| US9399666B2 (en) | 2008-09-18 | 2016-07-26 | New York University | Inhibiting interaction between the HIF-1ALPHA and p300/CBP with hydrogen bond surrogate-based helices |
| AU2009294869A1 (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 |
| CA2737916A1 (en) | 2008-09-22 | 2010-03-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US8524653B2 (en) | 2008-09-22 | 2013-09-03 | 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 |
| CN102203126A (zh) | 2008-09-22 | 2011-09-28 | 爱勒让治疗公司 | 用于制备纯化的多肽组合物的方法 |
| WO2010060112A1 (en) | 2008-11-24 | 2010-05-27 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles with improved properties |
| EP2376100B1 (en) | 2009-01-14 | 2017-10-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| WO2011008260A2 (en) | 2009-07-13 | 2011-01-20 | President And Fellows Of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| CA2774973A1 (en) | 2009-09-22 | 2011-03-31 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| BR112012008831A2 (pt) | 2009-10-14 | 2019-09-24 | Aileron Therapeutics Inc | macrociclos de peptideomiméticos aprimorados. |
| SI2603600T1 (sl) | 2010-08-13 | 2019-04-30 | Aileron Therapeutics, Inc. | Peptidomimetični makrocikli |
| 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 |
| IN2014CN02398A (enExample) | 2011-08-31 | 2015-06-19 | Univ New York | |
| TW201806968A (zh) | 2011-10-18 | 2018-03-01 | 艾利倫治療公司 | 擬肽巨環化合物 |
| WO2013059530A2 (en) | 2011-10-18 | 2013-04-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| HK1205454A1 (en) * | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| KR102112373B1 (ko) | 2012-02-15 | 2020-05-18 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방체 마크로사이클 |
| WO2014071241A1 (en) | 2012-11-01 | 2014-05-08 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
| WO2014138429A2 (en) | 2013-03-06 | 2014-09-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and use thereof in regulating hif1alpha |
| US20170037086A1 (en) | 2014-04-09 | 2017-02-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles with pth activity |
| BR112017005598A2 (pt) | 2014-09-24 | 2017-12-12 | Aileron Therapeutics Inc | macrociclos peptidomiméticos e usos dos mesmos |
| JP2018503595A (ja) | 2014-09-24 | 2018-02-08 | 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およびその製剤 |
| WO2016154058A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| US10059741B2 (en) | 2015-07-01 | 2018-08-28 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US10464975B2 (en) | 2015-07-02 | 2019-11-05 | Dana-Farber Cancer Institute, Inc. | Stabilized anti-microbial peptides |
| US20170037105A1 (en) | 2015-08-03 | 2017-02-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| AU2016315878A1 (en) | 2015-09-03 | 2018-03-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| US10023613B2 (en) | 2015-09-10 | 2018-07-17 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles as modulators of MCL-1 |
| WO2017165299A2 (en) | 2016-03-21 | 2017-09-28 | Aileron Therapeutics, Inc. | Companion diagnostic tool for peptidomimetic macrocycles |
| 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 |
-
2008
- 2008-02-25 CN CN201811034176.3A patent/CN109627287A/zh active Pending
- 2008-02-25 EP EP08730678A patent/EP2114428B1/en not_active Not-in-force
- 2008-02-25 EP EP12174832.1A patent/EP2564862B1/en not_active Not-in-force
- 2008-02-25 EP EP12174833.9A patent/EP2564863B1/en not_active Not-in-force
- 2008-02-25 CN CN200880009510.8A patent/CN101663044B/zh not_active Expired - Fee Related
- 2008-02-25 ES ES08730678T patent/ES2398310T3/es active Active
- 2008-02-25 CA CA2678941A patent/CA2678941C/en not_active Expired - Fee Related
- 2008-02-25 AU AU2008218116A patent/AU2008218116B2/en not_active Ceased
- 2008-02-25 BR BRPI0807578-6A patent/BRPI0807578A2/pt not_active IP Right Cessation
- 2008-02-25 US US12/037,041 patent/US7981999B2/en not_active Expired - Fee Related
- 2008-02-25 WO PCT/US2008/054922 patent/WO2008104000A2/en not_active Ceased
- 2008-02-25 EP EP17187148.6A patent/EP3301108A1/en not_active Withdrawn
- 2008-02-25 ES ES12174833.9T patent/ES2648687T3/es active Active
- 2008-02-25 JP JP2009551061A patent/JP4997293B2/ja not_active Expired - Fee Related
- 2008-02-25 CN CN201410299323.5A patent/CN104086641A/zh not_active Withdrawn
- 2008-02-25 ES ES12174832.1T patent/ES2649941T3/es active Active
-
2009
- 2009-08-20 IL IL200532A patent/IL200532A/en active IP Right Grant
-
2011
- 2011-04-29 US US13/097,930 patent/US8637686B2/en not_active Expired - Fee Related
-
2012
- 2012-02-09 US US13/370,057 patent/US9023988B2/en not_active Expired - Fee Related
-
2014
- 2014-11-26 JP JP2014238716A patent/JP6046686B2/ja not_active Expired - Fee Related
-
2015
- 2015-04-02 US US14/677,679 patent/US9493509B2/en not_active Expired - Fee Related
- 2015-09-20 IL IL241729A patent/IL241729A/en active IP Right Grant
-
2016
- 2016-04-07 US US15/093,426 patent/US9957296B2/en not_active Expired - Fee Related
- 2016-04-08 US US15/093,869 patent/US10030049B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2015110654A5 (enExample) | ||
| JP2010513314A5 (enExample) | ||
| CA1234800A (en) | Processes for the preparation of new conjugates of vinblastine or of vinblastine derivatives and the products of such processes | |
| US7084244B2 (en) | Conformationally constrained backbone cyclized peptide analogs | |
| JP2014231516A5 (enExample) | ||
| JP2013505300A5 (enExample) | ||
| CN102203245A (zh) | 拟肽大环化合物 | |
| JP2006077017A (ja) | コンホメーション的に固定された主鎖環化ペプチド類似体 | |
| CN101663044A (zh) | 三唑大环系统 | |
| CN102197048A (zh) | 拟肽大环化合物 | |
| CN104961795A (zh) | 用于制备纯化的多肽组合物的方法 | |
| CA2089747A1 (en) | Cyclopeptides, a method of preparing them, and their use as drugs | |
| AU2009294874A1 (en) | Peptidomimetic macrocycles | |
| US20050267017A1 (en) | Conformationally constrained C-backbone cyclic peptides | |
| JPWO2012121057A1 (ja) | 新規な非ペプチド性架橋構造を含む架橋ペプチド、ならびに該架橋ペプチドの合成方法および該方法に用いる新規な有機化合物 | |
| JP2002536428A (ja) | タンパク質結合のための改良化化合物 | |
| Olsen et al. | Fukuyama–Mitsunobu alkylation in amine synthesis on solid phase revisited: N-alkylation with secondary alcohols and synthesis of curtatoxins | |
| JP2004309372A5 (enExample) | ||
| JP2013509396A5 (enExample) | ||
| ten Brink et al. | Ring-closing metathesis for the synthesis of side chain knotted pentapeptides inspired by vancomycin | |
| JP2002517461A (ja) | ブラジキニンアンタゴニスト | |
| WO2023102255A1 (en) | Peptide-encoded libraries of small molecules for de novo drug discovery | |
| JP2020529472A5 (enExample) | ||
| Baker et al. | Novel reagents and reactions for drug design | |
| US20210122781A1 (en) | Stapled peptides |