CA2996685A1 - Peptidomimetic macrocycles and uses thereof - Google Patents

Peptidomimetic macrocycles and uses thereof Download PDF

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Publication number
CA2996685A1
CA2996685A1 CA2996685A CA2996685A CA2996685A1 CA 2996685 A1 CA2996685 A1 CA 2996685A1 CA 2996685 A CA2996685 A CA 2996685A CA 2996685 A CA2996685 A CA 2996685A CA 2996685 A1 CA2996685 A1 CA 2996685A1
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CA
Canada
Prior art keywords
independently
active agent
pharmaceutically active
peptidomimetic macrocycle
amino acid
Prior art date
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Pending
Application number
CA2996685A
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English (en)
French (fr)
Inventor
Manuel AIVADO
Vincent Guerlavais
Karen Olson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Rein Therapeutics Inc
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Aileron Therapeutics Inc
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Application filed by Aileron Therapeutics Inc filed Critical Aileron Therapeutics Inc
Publication of CA2996685A1 publication Critical patent/CA2996685A1/en
Pending legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/56Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/66Phosphorus compounds
    • A61K31/664Amides of phosphorus acids
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
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    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
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    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46Hydrolases (3)
    • A61K38/50Hydrolases (3) acting on carbon-nitrogen bonds, other than peptide bonds (3.5), e.g. asparaginase
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C12YENZYMES
    • C12Y305/00Hydrolases acting on carbon-nitrogen bonds, other than peptide bonds (3.5)
    • C12Y305/01Hydrolases acting on carbon-nitrogen bonds, other than peptide bonds (3.5) in linear amides (3.5.1)
    • C12Y305/01001Asparaginase (3.5.1.1)
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    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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    • G01N33/502Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
    • G01N33/5023Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects on expression patterns
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CA2996685A 2015-09-03 2016-09-02 Peptidomimetic macrocycles and uses thereof Pending CA2996685A1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201562214142P 2015-09-03 2015-09-03
US62/214,142 2015-09-03
US201662310254P 2016-03-18 2016-03-18
US62/310,254 2016-03-18
US201662344651P 2016-06-02 2016-06-02
US201662344791P 2016-06-02 2016-06-02
US62/344,651 2016-06-02
US62/344,791 2016-06-02
PCT/US2016/050194 WO2017040990A1 (en) 2015-09-03 2016-09-02 Peptidomimetic macrocycles and uses thereof

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Publication Number Publication Date
CA2996685A1 true CA2996685A1 (en) 2017-03-09

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CA2996685A Pending CA2996685A1 (en) 2015-09-03 2016-09-02 Peptidomimetic macrocycles and uses thereof

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US (2) US20170114098A1 (enExample)
EP (1) EP3344275B8 (enExample)
JP (1) JP6971970B2 (enExample)
KR (1) KR20180043835A (enExample)
CN (1) CN108348571B (enExample)
AU (1) AU2016315878A1 (enExample)
BR (1) BR112018003985A2 (enExample)
CA (1) CA2996685A1 (enExample)
IL (1) IL257706A (enExample)
MX (1) MX2018002723A (enExample)
WO (1) WO2017040990A1 (enExample)

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CA2939778C (en) 2007-01-31 2019-01-29 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
WO2008104000A2 (en) 2007-02-23 2008-08-28 Aileron Therapeutics, Inc. Triazole macrocycle systems
CA2682174C (en) 2007-03-28 2021-04-06 President And Fellows Of Harvard College Stitched polypeptides
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
WO2011038049A1 (en) 2009-09-22 2011-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
KR20130099938A (ko) 2010-08-13 2013-09-06 에일러론 테라퓨틱스 인코포레이티드 펩티도미메틱 거대고리
CN104039342A (zh) 2011-10-18 2014-09-10 爱勒让治疗公司 拟肽大环化合物
NZ627528A (en) 2012-02-15 2016-05-27 Aileron Therapeutics Inc Peptidomimetic macrocycles
SG11201503052RA (en) 2012-11-01 2015-05-28 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
MX2017003797A (es) 2014-09-24 2017-06-15 Aileron Therapeutics Inc Macrociclos peptidomimeticos y usos de los mismos.
MX389354B (es) 2014-09-24 2025-03-20 Aileron Therapeutics Inc Macrociclos peptidomimeticos y formulaciones de los mismos.
WO2016154058A1 (en) 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
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
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TW201818934A (zh) * 2016-10-17 2018-06-01 日商第一三共股份有限公司 Mdm2抑制劑與dna甲基轉移酶抑制劑之倂用治療法
JP2019537585A (ja) 2016-10-28 2019-12-26 アイカーン スクール オブ メディスン アット マウント シナイ Ezh2媒介性がんを治療するための組成物および方法
CA3045037A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
MX393780B (es) 2017-01-17 2025-03-24 Heparegenix Gmbh Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos
JP2020519595A (ja) * 2017-05-11 2020-07-02 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使用
WO2018223040A1 (en) * 2017-06-01 2018-12-06 Bristol-Myers Squibb Company Methods of treating a tumor using an anti-pd-1 antibody
WO2018218633A1 (en) * 2017-06-02 2018-12-06 Beijing Percans Oncology Co. Ltd. Combination therapies for treating cancers
US11472799B2 (en) 2018-03-06 2022-10-18 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (AKT) degradation / disruption compounds and methods of use
WO2019195959A1 (en) 2018-04-08 2019-10-17 Cothera Biosciences, Inc. Combination therapy for cancers with braf mutation
JP2021527666A (ja) 2018-06-21 2021-10-14 アイカーン スクール オブ メディスン アット マウント シナイ Wd40反復ドメインタンパク質5(wdr5)分解/破壊化合物および使用の方法
WO2020023502A1 (en) * 2018-07-23 2020-01-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
KR20210044251A (ko) 2018-08-13 2021-04-22 베이징 페르칸스 온콜로지 컴퍼니 리미티드 암 치료용 바이오마커
CN112218877B (zh) 2018-08-27 2025-07-25 瑞泽恩制药公司 拉曼光谱在下游纯化中的应用
WO2020112868A1 (en) * 2018-11-30 2020-06-04 Aileron Therapeutics, Inc. Combination therapy of peptidomimetic macrocycles
AR116904A1 (es) * 2018-12-11 2021-06-23 Kartos Therapeutics Inc Métodos y composiciones para el tratamiento de un trastorno oftálmico
CN109731104A (zh) * 2018-12-29 2019-05-10 苏州明基医院有限公司 一种多肽-稀土材料递送系统及制备方法和应用
CN114173878A (zh) * 2019-03-15 2022-03-11 艾瑞朗医疗公司 拟肽大环化合物及其用途
WO2020198734A1 (en) * 2019-03-28 2020-10-01 The Penn State Research Foundation Methods, compositions relating to treatment of cancer
CN114423463B (zh) 2019-05-06 2025-09-26 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
WO2021202961A1 (en) * 2020-04-02 2021-10-07 United States As Represented By Dept Of Veterans Affairs Methods of treating immunotherapy resistant metastatic melanoma
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
IL298592A (en) 2020-06-24 2023-01-01 Pmv Pharmaceuticals Inc Combination therapy for treatment of cancer
CN111825621A (zh) * 2020-07-22 2020-10-27 天津理工大学 一种奥拉帕尼与丙二酸的共晶及其制备方法
US11760747B2 (en) 2020-12-21 2023-09-19 Alkermes, Inc. Substituted piperidino compounds and related methods of treatment
CN115137731B (zh) * 2022-05-19 2023-11-21 上海交通大学医学院附属新华医院 Flt3抑制剂及其药学上可接受的盐在制备治疗皮肤t细胞淋巴瘤药物中的应用
WO2024083223A1 (zh) * 2022-10-21 2024-04-25 正大天晴药业集团股份有限公司 大环类化合物及其医药用途
GB202219576D0 (en) * 2022-12-22 2023-02-08 Univ Court Univ Of Glasgow Polypeptides
AU2024361979A1 (en) * 2023-10-20 2026-03-05 Alkermes, Inc. Compound for use in treating narcolepsy
WO2025096608A1 (en) * 2023-10-31 2025-05-08 The Board Of Trustees Of The Leland Stanford Junior University Egfr covalent inhibition with macrocycles

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US5364851A (en) 1991-06-14 1994-11-15 International Synthecon, Llc Conformationally restricted biologically active peptides, methods for their production and uses thereof
US5446128A (en) 1993-06-18 1995-08-29 The Board Of Trustees Of The University Of Illinois Alpha-helix mimetics and methods relating thereto
US5824483A (en) 1994-05-18 1998-10-20 Pence Inc. Conformationally-restricted combinatiorial library composition and method
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
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
CN1753912B (zh) 2002-12-23 2011-11-02 惠氏公司 抗pd-1抗体及其用途
WO2005118620A2 (en) 2004-05-27 2005-12-15 New York University Methods for preparing internally constraied peptides and peptidomimetics
ES2720160T3 (es) 2005-05-09 2019-07-18 Ono Pharmaceutical Co Anticuerpos monoclonales humanos contra muerte programada 1(PD-1) y métodos para tratar el cáncer usando anticuerpos dirigidos contra PD-1 solos o junto con otras sustancias inmunoterapéuticas
EA019344B1 (ru) 2005-07-01 2014-03-31 МЕДАРЕКС, Эл.Эл.Си. Человеческие моноклональные антитела против лиганда-1 запрограммированной гибели клеток (pd-l1) и их применения
US7932397B2 (en) 2006-11-22 2011-04-26 Massachusetts Institute Of Technology Olefin metathesis catalysts and related methods
CA2682174C (en) 2007-03-28 2021-04-06 President And Fellows Of Harvard College Stitched polypeptides
JP5191537B2 (ja) 2007-06-18 2013-05-08 エム・エス・ディー・オス・ベー・フェー ヒトのプログラムされたデスレセプターpd−1に対する抗体
CN103951541A (zh) 2008-01-25 2014-07-30 波士顿学院董事会 用于催化包括对映选择性烯烃复分解的复分解反应的方法
EP2328920A2 (en) 2008-08-25 2011-06-08 Amplimmune, Inc. Targeted costimulatory polypeptides and methods of use to treat cancer
JP2012509902A (ja) * 2008-11-24 2012-04-26 エルロン・セラピューティクス・インコーポレイテッド 改善された特性を有するペプチド模倣大環状分子
HUE065752T2 (hu) 2008-12-09 2024-06-28 Hoffmann La Roche Anti-PD-L1 antitestek és felhasználásuk T-sejt funkció elõsegítésére
EP2504028A4 (en) 2009-11-24 2014-04-09 Amplimmune Inc SIMULTANEOUS INHIBITION OF PD-L1 / PD-L2
WO2011097642A1 (en) 2010-02-08 2011-08-11 Trustees Of Boston College Efficient methods for z- or cis-selective cross-metathesis
KR20130099938A (ko) * 2010-08-13 2013-09-06 에일러론 테라퓨틱스 인코포레이티드 펩티도미메틱 거대고리
EA026924B1 (ru) 2011-08-01 2017-05-31 Дженентек, Инк. Способы лечения рака с использованием антагонистов, связывающихся с осью pd-1, и ингибиторов mek
NZ627528A (en) * 2012-02-15 2016-05-27 Aileron Therapeutics Inc Peptidomimetic macrocycles
EP2817023A4 (en) * 2012-02-22 2015-11-25 Univ New York REVERSIBLE NETWORKED SCREW-MOUNTED HYDROGEN BONDING SUPPLY MACROCYCLES
WO2015082384A1 (en) * 2013-12-05 2015-06-11 F. Hoffmann-La Roche Ag Novel combination treatment for acute myeloid leukemia (aml)
MX389354B (es) * 2014-09-24 2025-03-20 Aileron Therapeutics Inc Macrociclos peptidomimeticos y formulaciones de los mismos.
MX2017003797A (es) * 2014-09-24 2017-06-15 Aileron Therapeutics Inc Macrociclos peptidomimeticos y usos de los mismos.
WO2016154058A1 (en) * 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof

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