CA2286867A1 - Echantillotheques combinatoires de macrocycles peptidomimetiques et procedes correspondants - Google Patents

Echantillotheques combinatoires de macrocycles peptidomimetiques et procedes correspondants Download PDF

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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)
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/fr
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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Structural Engineering (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

La présente invention concerne une échantillothèque diversifiée de composés macrocycliques peptidomimétiques, les procédés de préparation correspondants et un dispositif permettant de constituer une source facilement accessible de chacun des différents membres de l'échantillothèque. Ce dispositif convient à des nécessaires de dosage et comme élément remplaçable dans des machines à doser automatisées.
CA002286867A 1997-04-11 1998-04-08 Echantillotheques combinatoires de macrocycles peptidomimetiques et procedes correspondants Abandoned CA2286867A1 (fr)

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 (fr) 1997-04-11 1998-04-08 Echantillotheques combinatoires de macrocycles peptidomimetiques et procedes correspondants

Publications (1)

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

Family

ID=21927649

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002286867A Abandoned CA2286867A1 (fr) 1997-04-11 1998-04-08 Echantillotheques combinatoires de macrocycles peptidomimetiques et procedes correspondants

Country Status (5)

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

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 (fr) * 1999-10-04 2012-12-11 Neokimia Inc. Synthese combinatoire de bibliotheques de composes macrocycliques utiles pour la decouverte de medicaments
CA2528375C (fr) 2003-06-18 2013-11-19 Tranzyme Pharma, Inc. Antagonistes macrocycliques du recepteur de motiline
DE602004030344D1 (de) * 2003-07-31 2011-01-13 Tranzyme Pharma Inc Räumlich definierte makrocyclische verbindungen, die sich für die entdeckung von arzneimittel eignen
WO2005012332A1 (fr) * 2003-07-31 2005-02-10 Tranzyme Pharma Composes macrocycliques definis spatialement incorporant des substituts de liaison peptidique
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
BRPI0720306A2 (pt) 2006-12-14 2014-02-04 Aileron Therapeutics Inc Sistemas de macrociclização da bis-sufidrila
US7981998B2 (en) 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
PL2118123T3 (pl) 2007-01-31 2016-06-30 Dana Farber Cancer Inst Inc Stabilizowane peptydy p53 i ich zastosowania
CA2678941C (fr) 2007-02-23 2018-11-27 Aileron Therapeutics, Inc. Systemes macrocycliques de triazole
JP5631201B2 (ja) 2007-03-28 2014-11-26 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 ステッチングされたポリペプチド
EP2067787A1 (fr) 2007-12-06 2009-06-10 Boehringer Ingelheim International GmbH Procédé pour le contrôle de populations d'insectes
AU2010204648B2 (en) 2009-01-14 2016-09-01 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
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
KR102104762B1 (ko) 2010-08-13 2020-04-24 에일러론 테라퓨틱스 인코포레이티드 펩티도미메틱 거대고리
EP2768518A4 (fr) 2011-10-18 2015-05-27 Aileron Therapeutics Inc Macrocycles peptidomimétiques
CA2864120A1 (fr) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Macrocycles peptidomimetiques reticules par triazole et par thioether
RU2642299C2 (ru) 2012-02-15 2018-01-24 Эйлерон Терапьютикс, Инк. P53 пептидомиметические макроциклы
BR112015009470A2 (pt) 2012-11-01 2019-12-17 Aileron Therapeutics Inc aminoácidos dissubstituídos e seus métodos de preparação e uso
EP3197478A4 (fr) 2014-09-24 2018-05-30 Aileron Therapeutics, Inc. Macrocycles peptidomimétiques et leurs utilisations
CN107106642B (zh) 2014-09-24 2021-02-26 艾瑞朗医疗公司 拟肽大环化合物及其制剂
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
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
EP3347372A4 (fr) 2015-09-10 2019-09-04 Aileron Therapeutics, Inc. Macrocycles peptidomimétiques en tant que modulateurs de 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
JPH08505628A (ja) * 1993-01-08 1996-06-18 田辺製薬株式会社 ペプチド型細胞接着阻害薬
WO1995019567A1 (fr) * 1994-01-13 1995-07-20 The Trustees Of Columbia University In The City Of New York Recepteurs de synthese, leurs bibliotheques et leurs utilisations
WO1996022304A1 (fr) * 1995-01-20 1996-07-25 Molecumetics, Ltd. Bibliotheque de substances mimetiques de retournement astreintes a une conformation et procedes associes
WO1996040781A1 (fr) * 1995-06-07 1996-12-19 Tanabe Seiyaku Co., Ltd. INHIBITEURS PEPTIDIQUES CYCLIQUES D'ADHERENCE CELLULAIRE INDUITE PAR INTEGRINE β1 ET β¿2?

Also Published As

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

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Legal Events

Date Code Title Description
FZDE Discontinued