CA2286867A1 - Combinatorial libraries of peptidomimetic macrocycles and processes therefor - Google Patents

Combinatorial libraries of peptidomimetic macrocycles and processes therefor Download PDF

Info

Publication number
CA2286867A1
CA2286867A1 CA002286867A CA2286867A CA2286867A1 CA 2286867 A1 CA2286867 A1 CA 2286867A1 CA 002286867 A CA002286867 A CA 002286867A CA 2286867 A CA2286867 A CA 2286867A CA 2286867 A1 CA2286867 A1 CA 2286867A1
Authority
CA
Canada
Prior art keywords
group
hydrogen
formula
chloride
acid
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.)
Abandoned
Application number
CA002286867A
Other languages
English (en)
French (fr)
Inventor
David Mendel
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.)
Eli Lilly and Co
Original Assignee
Individual
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2286867A1 publication Critical patent/CA2286867A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures
    • C40B40/04—Libraries containing only organic compounds
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B50/00—Methods of creating libraries, e.g. combinatorial synthesis
    • C40B50/14—Solid phase synthesis, i.e. wherein one or more library building blocks are bound to a solid support during library creation; Particular methods of cleavage from the solid support
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/11—Compounds covalently bound to a solid support
CA002286867A 1997-04-11 1998-04-08 Combinatorial libraries of peptidomimetic macrocycles and processes therefor Abandoned CA2286867A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4353297P 1997-04-11 1997-04-11
US60/043,532 1997-04-11
PCT/US1998/007135 WO1998046631A1 (en) 1997-04-11 1998-04-08 Combinatorial libraries of peptidomimetic macrocycles and processes therefor

Publications (1)

Publication Number Publication Date
CA2286867A1 true CA2286867A1 (en) 1998-10-22

Family

ID=21927649

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002286867A Abandoned CA2286867A1 (en) 1997-04-11 1998-04-08 Combinatorial libraries of peptidomimetic macrocycles and processes therefor

Country Status (5)

Country Link
EP (1) EP1015479A4 (ja)
JP (1) JP2002506423A (ja)
AU (1) AU6895598A (ja)
CA (1) CA2286867A1 (ja)
WO (1) WO1998046631A1 (ja)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
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
CA2284459C (en) 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
WO2004111077A1 (en) 2003-06-18 2004-12-23 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor
DK1648922T3 (da) 2003-07-31 2011-03-14 Tranzyme Pharma Inc Rumligt definerede makrocykliske forbindelser, der er anvendelige til opdagelse af lægemidler
US7550431B2 (en) * 2003-07-31 2009-06-23 Tranzyme Pharma Inc. Spatially-defined macrocycles incorporating peptide bond surrogates
US8088733B2 (en) 2006-07-06 2012-01-03 Tranzyme Pharma Inc. Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders
US7981998B2 (en) 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US7960506B2 (en) * 2006-12-14 2011-06-14 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
PT2118123E (pt) 2007-01-31 2016-02-10 Harvard College Péptidos de p53 estabilizados e suas utilizações
CN109627287A (zh) 2007-02-23 2019-04-16 爱勒让治疗公司 三唑大环系统
WO2008121767A2 (en) 2007-03-28 2008-10-09 President And Fellows Of Harvard College Stitched polypeptides
EP2067787A1 (en) 2007-12-06 2009-06-10 Boehringer Ingelheim International GmbH Method for controlling insect populations
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
JP2013505300A (ja) 2009-09-22 2013-02-14 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
RU2582678C2 (ru) 2010-08-13 2016-04-27 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы
TWI643868B (zh) 2011-10-18 2018-12-11 艾利倫治療公司 擬肽巨環化合物
JP6450191B2 (ja) 2012-02-15 2019-01-09 エイルロン セラピューティクス，インコーポレイテッド ペプチドミメティック大環状化合物
EP2819688A4 (en) 2012-02-15 2015-10-28 Aileron Therapeutics Inc TRIAZOL AND THIOETHER-COUPLED PEPTIDOMIMETIC MACROCYCLES
WO2014071241A1 (en) 2012-11-01 2014-05-08 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
KR102570210B1 (ko) 2014-09-24 2023-08-23 에일러론 테라퓨틱스 인코포레이티드 펩티드모방 거대고리 및 이의 제제
KR20170058424A (ko) 2014-09-24 2017-05-26 에일러론 테라퓨틱스 인코포레이티드 펩티드모방 거대고리 및 이의 용도
JP2018516844A (ja) 2015-03-20 2018-06-28 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
WO2017004548A1 (en) 2015-07-01 2017-01-05 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5650489A (en) * 1990-07-02 1997-07-22 The Arizona Board Of Regents Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof
WO1994015958A2 (en) * 1993-01-08 1994-07-21 Tanabe Seiyaku Co., Ltd. Peptide inhibitors of cell adhesion
US7067326B2 (en) * 1994-01-13 2006-06-27 The Trustees Of Columbia University In The City Of New York Synthetic receptors, libraries and uses thereof
JPH10512570A (ja) * 1995-01-20 1998-12-02 モレキュメティックス リミテッド コンホメーション的に制限された逆ターンライブラリおよびそれらに関連する方法
WO1996040781A1 (en) * 1995-06-07 1996-12-19 Tanabe Seiyaku Co., Ltd. CYCLIC PEPTIDE INHIBITORS OF β1 AND β2 INTEGRIN-MEDIATED ADHESION

Also Published As

Publication number Publication date
JP2002506423A (ja) 2002-02-26
EP1015479A1 (en) 2000-07-05
WO1998046631A1 (en) 1998-10-22
AU6895598A (en) 1998-11-11
EP1015479A4 (en) 2002-07-24

Similar Documents

Publication Publication Date Title
CA2286867A1 (en) Combinatorial libraries of peptidomimetic macrocycles and processes therefor
Thompson et al. Synthesis and applications of small molecule libraries
EP0751765B1 (en) Sulfonamide derivatives and their use
JP3394777B2 (ja) 位相学的に分離された、コードされた固相ライブラリー
US5840485A (en) Topologically segregated, encoded solid phase libraries
US5549974A (en) Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof
US5846839A (en) Methods for hard-tagging an encoded synthetic library
US5646285A (en) Combinatorial non-peptide libraries
Früchtel et al. Organic chemistry on solid supports
US5541061A (en) Methods for screening factorial chemical libraries
AU729646B2 (en) A template for solution phase synthesis of combinatorial libraries
US5891737A (en) Combinatorial non-peptide libraries
WO1996000391A1 (en) Methods for the synthesis of diketopiperazines
Patek et al. Safety‐catch and multiply cleavable linkers in solid‐phase synthesis
Blondelle et al. Soluble combinatorial libraries of organic, peptidomimetic and peptide diversities
Beck-Sickinger et al. Combinatorial strategies in biology and chemistry
Wilson et al. Solid-supported syntheses of 3-thio-1, 2, 4-triazoles
CA2286862A1 (en) Combinatorial libraries of peptidomimetic aminothioether acids
Ni et al. [16] Encoded combinatorial chemistry: Binary coding using chemically robust secondary amine tags
Lebl et al. Construction and screening of libraries of peptide and non-peptide structures
WO1996040732A1 (en) Combinatorial non-peptide libraries
Han et al. Azatides as peptidomimetics: solution and liquid phase syntheses
Thompson III The solid-phase synthesis of prostaglandins
Ganesan Combinatorial synthetic design: The balance of novelty and familiarity
Krchňák et al. Combinatorial libraries of synthetic structures: Synthesis screening and structure determination

Legal Events

Date Code Title Description
FZDE Discontinued