JP2010510236A5 - - Google Patents
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- Publication number
- JP2010510236A5 JP2010510236A5 JP2009537371A JP2009537371A JP2010510236A5 JP 2010510236 A5 JP2010510236 A5 JP 2010510236A5 JP 2009537371 A JP2009537371 A JP 2009537371A JP 2009537371 A JP2009537371 A JP 2009537371A JP 2010510236 A5 JP2010510236 A5 JP 2010510236A5
- Authority
- JP
- Japan
- Prior art keywords
- polypeptide
- independently
- modified polypeptide
- formula
- 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.)
- Pending
Links
- 229920001184 polypeptide Polymers 0.000 claims description 97
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 97
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 97
- 150000001413 amino acids Chemical class 0.000 claims description 43
- 125000000217 alkyl group Chemical group 0.000 claims description 38
- 125000003342 alkenyl group Chemical group 0.000 claims description 25
- 229910052799 carbon Inorganic materials 0.000 claims description 25
- 125000000304 alkynyl group Chemical group 0.000 claims description 17
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 14
- 150000001875 compounds Chemical class 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 10
- 101100455978 Arabidopsis thaliana MAM1 gene Proteins 0.000 claims description 9
- 125000003275 alpha amino acid group Chemical group 0.000 claims description 6
- 125000005647 linker group Chemical group 0.000 claims description 6
- PFNFFQXMRSDOHW-UHFFFAOYSA-N spermine Chemical compound NCCCNCCCCNCCCN PFNFFQXMRSDOHW-UHFFFAOYSA-N 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 4
- 239000003054 catalyst Substances 0.000 claims description 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000001475 halogen functional group Chemical group 0.000 claims description 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 150000001720 carbohydrates Chemical class 0.000 claims description 3
- 229910052757 nitrogen Inorganic materials 0.000 claims description 3
- 238000006798 ring closing metathesis reaction Methods 0.000 claims description 3
- 229940063675 spermine Drugs 0.000 claims description 3
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical group C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 210000000170 cell membrane Anatomy 0.000 claims description 2
- 229920001577 copolymer Polymers 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 235000014655 lactic acid Nutrition 0.000 claims description 2
- 239000004310 lactic acid Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims description 2
- 230000008685 targeting Effects 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 238000002198 surface plasmon resonance spectroscopy Methods 0.000 claims 4
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 4
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical group N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 2
- 208000009052 Precursor T-Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 2
- 208000017414 Precursor T-cell acute lymphoblastic leukemia Diseases 0.000 description 2
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 description 2
- 239000003638 chemical reducing agent Substances 0.000 description 2
- 239000007800 oxidant agent Substances 0.000 description 2
- 101100398918 Arabidopsis thaliana IPMS2 gene Proteins 0.000 description 1
- 101000851434 Homo sapiens Tumor necrosis factor ligand superfamily member 13B Proteins 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical group [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 description 1
- 102100036922 Tumor necrosis factor ligand superfamily member 13B Human genes 0.000 description 1
- 229960002685 biotin Drugs 0.000 description 1
- 235000020958 biotin Nutrition 0.000 description 1
- 239000011616 biotin Substances 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000012285 osmium tetroxide Substances 0.000 description 1
- 229910000489 osmium tetroxide Inorganic materials 0.000 description 1
- 229910052707 ruthenium Inorganic materials 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85937906P | 2006-11-15 | 2006-11-15 | |
| PCT/US2007/084838 WO2008061192A2 (en) | 2006-11-15 | 2007-11-15 | Stabilized maml peptides and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014007579A Division JP2014114298A (ja) | 2006-11-15 | 2014-01-20 | 安定化させたｍａｍｌペプチドおよびその使用法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010510236A JP2010510236A (ja) | 2010-04-02 |
| JP2010510236A5 true JP2010510236A5 (enExample) | 2011-01-27 |
Family
ID=39402481
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009537371A Pending JP2010510236A (ja) | 2006-11-15 | 2007-11-15 | 安定化させたｍａｍｌペプチドおよびその使用法 |
| JP2014007579A Pending JP2014114298A (ja) | 2006-11-15 | 2014-01-20 | 安定化させたｍａｍｌペプチドおよびその使用法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014007579A Pending JP2014114298A (ja) | 2006-11-15 | 2014-01-20 | 安定化させたｍａｍｌペプチドおよびその使用法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9074009B2 (enExample) |
| EP (3) | EP2997973A1 (enExample) |
| JP (2) | JP2010510236A (enExample) |
| AU (1) | AU2007319193A1 (enExample) |
| CA (1) | CA2669696A1 (enExample) |
| WO (1) | WO2008061192A2 (enExample) |
Families Citing this family (42)
| 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 |
| EP2997973A1 (en) | 2006-11-15 | 2016-03-23 | Dana-Farber Cancer Institute, Inc. | Stabalized maml peptides and uses thereof |
| US7981998B2 (en) * | 2006-12-14 | 2011-07-19 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| BRPI0720306A2 (pt) * | 2006-12-14 | 2014-02-04 | Aileron Therapeutics Inc | Sistemas de macrociclização da bis-sufidrila |
| DK2118123T3 (en) * | 2007-01-31 | 2016-01-25 | Dana Farber Cancer Inst Inc | Stabilized p53 peptides and uses thereof |
| ES2649941T3 (es) | 2007-02-23 | 2018-01-16 | Aileron Therapeutics, Inc. | Aminoácidos sustituidos para preparar péptidos macrocíclicos unidos a triazol |
| US8592377B2 (en) | 2007-03-28 | 2013-11-26 | President And Fellows Of Harvard College | Stitched polypeptides |
| EP2356139A4 (en) * | 2008-07-23 | 2013-01-09 | Harvard College | LIGURE COMBINED POLYPEPTIDES |
| CN102197048A (zh) * | 2008-09-22 | 2011-09-21 | 爱勒让治疗公司 | 拟肽大环化合物 |
| CA2737922A1 (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 |
| BRPI0920899A2 (pt) * | 2008-11-24 | 2016-04-26 | Aileron Therapeutics Inc | macrociclos peptidomiméticos com propriedades melhoradas |
| US9175047B2 (en) | 2009-01-14 | 2015-11-03 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| AU2010273220B2 (en) | 2009-07-13 | 2015-10-15 | President And Fellows Of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| CN102712675A (zh) | 2009-09-22 | 2012-10-03 | 爱勒让治疗公司 | 拟肽大环化合物 |
| ES2711526T3 (es) | 2010-08-13 | 2019-05-06 | Aileron Therapeutics Inc | Macrociclos peptidomiméticos |
| WO2012040459A2 (en) * | 2010-09-22 | 2012-03-29 | President And Fellows Of Harvard College | Beta-catenin targeting peptides and uses thereof |
| US9487562B2 (en) | 2011-06-17 | 2016-11-08 | President And Fellows Of Harvard College | Stabilized polypeptides as regulators of RAB GTPase function |
| WO2012174409A1 (en) * | 2011-06-17 | 2012-12-20 | President And Fellows Of Harvard College | Stabilized variant maml peptides and uses thereof |
| TW201806968A (zh) | 2011-10-18 | 2018-03-01 | 艾利倫治療公司 | 擬肽巨環化合物 |
| EP2819688A4 (en) | 2012-02-15 | 2015-10-28 | Aileron Therapeutics Inc | TRIAZOL AND THIOETHER-COUPLED PEPTIDOMIMETIC MACROCYCLES |
| BR112014020103A2 (pt) | 2012-02-15 | 2018-10-09 | Aileron Therapeutics, Inc. | macrociclos peptidomiméticos |
| WO2013151665A2 (en) | 2012-04-02 | 2013-10-10 | modeRNA Therapeutics | Modified polynucleotides for the production of proteins associated with human disease |
| US9254311B2 (en) | 2012-04-02 | 2016-02-09 | Moderna Therapeutics, Inc. | Modified polynucleotides for the production of proteins |
| WO2014052647A2 (en) | 2012-09-26 | 2014-04-03 | President And Fellows Of Harvard College | Proline-locked stapled peptides and uses thereof |
| US20150225471A1 (en) | 2012-10-01 | 2015-08-13 | President And Fellows Of Harvard College | Stabilized polypeptide insulin receptor modulators |
| 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 |
| EP3391898A3 (en) * | 2013-03-13 | 2019-02-13 | President and Fellows of Harvard College | Stapled and stitched polypeptides and uses thereof |
| JP2016523241A (ja) | 2013-06-14 | 2016-08-08 | 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 | 安定化されたポリペプチドインスリン受容体調節剤 |
| ES2796857T3 (es) | 2014-04-17 | 2020-11-30 | Inst Nat Sante Rech Med | Polipéptidos y usos de los mismos para reducir la motilidad celular mediada por CD95 |
| CA2949535C (en) | 2014-05-21 | 2023-09-12 | President And Fellows Of Harvard College | Ras inhibitory peptides and uses thereof |
| AU2015320545C1 (en) | 2014-09-24 | 2020-05-14 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and formulations thereof |
| EP3197478A4 (en) | 2014-09-24 | 2018-05-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| WO2016154058A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| US11155577B2 (en) | 2015-06-22 | 2021-10-26 | University Of Utah Research Foundation | Thiol-ene based peptide stapling and uses thereof |
| US10059741B2 (en) | 2015-07-01 | 2018-08-28 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| WO2017044633A1 (en) | 2015-09-10 | 2017-03-16 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles as modulators of mcl-1 |
| US11034720B2 (en) | 2016-07-17 | 2021-06-15 | University Of Utah Research Foundation | Thiol-yne based peptide stapling and uses thereof |
| AU2018329956A1 (en) | 2017-09-07 | 2020-08-20 | Fog Pharmaceuticals, Inc. | Agents modulating beta-catenin functions and methods thereof |
| WO2019178313A1 (en) * | 2018-03-14 | 2019-09-19 | Dana-Farber Cancer Institute, Inc. | Stabilized peptides for biomarker detection |
| MX2021001943A (es) | 2018-08-20 | 2021-07-15 | Fog Pharmaceuticals Inc | Colecciones de péptidos, agentes peptídicos y métodos de uso de los mismos. |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0633933A1 (en) | 1992-03-23 | 1995-01-18 | Imperial Cancer Research Technology Limited | Leucine zippers |
| 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 |
| AU722985B2 (en) | 1996-07-12 | 2000-08-17 | Mcgill University | Compounds and methods for modulating cell adhesion |
| US20020168761A1 (en) * | 2000-01-24 | 2002-11-14 | Gour Barbara J. | Peptidomimetic modulators of cell adhesion |
| US5851775A (en) | 1997-03-20 | 1998-12-22 | Johns Hopkins University | β-catenin, Tcf-4, and APC interact to prevent cancer |
| FR2775187B1 (fr) * | 1998-02-25 | 2003-02-21 | Novartis Ag | Utilisation de l'epothilone b pour la fabrication d'une preparation pharmaceutique antiproliferative et d'une composition comprenant l'epothilone b comme agent antiproliferatif in vivo |
| US6277824B1 (en) * | 1998-07-10 | 2001-08-21 | Adherex Technologies | Compounds and methods for modulating adhesion molecule function |
| US7192713B1 (en) * | 1999-05-18 | 2007-03-20 | President And Fellows Of Harvard College | Stabilized compounds having secondary structure motifs |
| CA2284459C (en) * | 1999-10-04 | 2012-12-11 | Neokimia Inc. | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
| WO2003004645A1 (en) * | 2001-07-03 | 2003-01-16 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Diagnosis and treatment of cancer involving the notch pathway |
| ES2586387T3 (es) * | 2003-11-05 | 2016-10-14 | Dana-Farber Cancer Institute, Inc. | Péptidos alfa helicoidales adecuados para activar o inhibir la muerte celular |
| US7202332B2 (en) * | 2004-05-27 | 2007-04-10 | New York University | Methods for preparing internally constrained peptides and peptidomimetics |
| DE102004033312A1 (de) * | 2004-07-08 | 2006-01-26 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Kontinuierliches Metatheseverfahren mit Ruthenium-Katalysatoren |
| EP1765378B1 (en) | 2004-07-12 | 2014-04-16 | Medical Research Fund of Tel Aviv Sourasky Medical Center | Agent capable of downregulating an msf-a-dependent hif-1a and use thereof in cancer treatment |
| EP2997973A1 (en) | 2006-11-15 | 2016-03-23 | Dana-Farber Cancer Institute, Inc. | Stabalized maml peptides and uses thereof |
| US7981998B2 (en) | 2006-12-14 | 2011-07-19 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| BRPI0720306A2 (pt) | 2006-12-14 | 2014-02-04 | Aileron Therapeutics Inc | Sistemas de macrociclização da bis-sufidrila |
| ES2649941T3 (es) * | 2007-02-23 | 2018-01-16 | Aileron Therapeutics, Inc. | Aminoácidos sustituidos para preparar péptidos macrocíclicos unidos a triazol |
| US8592377B2 (en) | 2007-03-28 | 2013-11-26 | President And Fellows Of Harvard College | Stitched polypeptides |
| WO2009110952A2 (en) * | 2007-12-31 | 2009-09-11 | New York University | Control of viral-host membrane fusion with hydrogen bond surrogate-based artificial helices |
| DE112009000300T5 (de) | 2008-02-08 | 2011-01-20 | Aileron Therapeutics, Inc., Cambridge | Therapeutische Peptidomimetische Makrocyclen |
| EP2310407A4 (en) * | 2008-04-08 | 2011-09-14 | Aileron Therapeutics Inc | BIOLOGIC EFFECTIVE PEPTIDOMIMETIC MACROCYCLES |
| US20110144303A1 (en) * | 2008-04-08 | 2011-06-16 | Aileron Therapeutics, Inc. | Biologically Active Peptidomimetic Macrocycles |
| WO2010033879A2 (en) * | 2008-09-18 | 2010-03-25 | New York University | Inhibiting interaction between hif-1a and p300/cbp with hydrogen bond surrogate-based helices |
| KR101754799B1 (ko) * | 2010-03-26 | 2017-07-07 | 삼성전자주식회사 | 화소 회로, 이를 포함하는 디스플레이 장치 및 디스플레이 장치의 구동방법 |
-
2007
- 2007-11-15 EP EP15171539.8A patent/EP2997973A1/en not_active Withdrawn
- 2007-11-15 EP EP12158552A patent/EP2489360A1/en not_active Withdrawn
- 2007-11-15 CA CA002669696A patent/CA2669696A1/en not_active Abandoned
- 2007-11-15 EP EP07871487A patent/EP2091552A4/en not_active Ceased
- 2007-11-15 AU AU2007319193A patent/AU2007319193A1/en not_active Abandoned
- 2007-11-15 JP JP2009537371A patent/JP2010510236A/ja active Pending
- 2007-11-15 WO PCT/US2007/084838 patent/WO2008061192A2/en not_active Ceased
-
2009
- 2009-06-04 US US12/478,504 patent/US9074009B2/en not_active Expired - Fee Related
-
2014
- 2014-01-20 JP JP2014007579A patent/JP2014114298A/ja active Pending
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