DK1218403T3 - Kombinationssyntese af biblioteker af makrocykliske forbindelser, der er anvendelige til medikamentopdagelse - Google Patents

Kombinationssyntese af biblioteker af makrocykliske forbindelser, der er anvendelige til medikamentopdagelse

Info

Publication number
DK1218403T3
DK1218403T3 DK00965687T DK00965687T DK1218403T3 DK 1218403 T3 DK1218403 T3 DK 1218403T3 DK 00965687 T DK00965687 T DK 00965687T DK 00965687 T DK00965687 T DK 00965687T DK 1218403 T3 DK1218403 T3 DK 1218403T3
Authority
DK
Denmark
Prior art keywords
bivalent radical
libraries
compounds useful
drug discovery
macrocyclic compounds
Prior art date
Application number
DK00965687T
Other languages
Danish (da)
English (en)
Inventor
Pierre Deslongchamps
Yves Dory
Ruoxi Lan
Gilles Berthiaume
Luc Ouellet
Original Assignee
Tranzyme Pharma Inc
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 Tranzyme Pharma Inc filed Critical Tranzyme Pharma Inc
Application granted granted Critical
Publication of DK1218403T3 publication Critical patent/DK1218403T3/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C07K5/0817—Tripeptides with the first amino acid being basic the first amino acid being Arg
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0819—Tripeptides with the first amino acid being acidic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S930/00—Peptide or protein sequence
    • Y10S930/01—Peptide or protein sequence
    • Y10S930/27—Cyclic peptide or cyclic protein

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Analytical Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
DK00965687T 1999-10-04 2000-10-04 Kombinationssyntese af biblioteker af makrocykliske forbindelser, der er anvendelige til medikamentopdagelse DK1218403T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CA2284459A CA2284459C (en) 1999-10-04 1999-10-04 Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
PCT/CA2000/001151 WO2001025257A2 (en) 1999-10-04 2000-10-04 Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery

Publications (1)

Publication Number Publication Date
DK1218403T3 true DK1218403T3 (da) 2007-04-10

Family

ID=4164289

Family Applications (1)

Application Number Title Priority Date Filing Date
DK00965687T DK1218403T3 (da) 1999-10-04 2000-10-04 Kombinationssyntese af biblioteker af makrocykliske forbindelser, der er anvendelige til medikamentopdagelse

Country Status (10)

Country Link
US (5) US7169899B1 (US07794700-20100914-C00152.png)
EP (1) EP1218403B1 (US07794700-20100914-C00152.png)
JP (5) JP5005865B2 (US07794700-20100914-C00152.png)
AT (1) ATE346857T1 (US07794700-20100914-C00152.png)
AU (1) AU7636100A (US07794700-20100914-C00152.png)
CA (1) CA2284459C (US07794700-20100914-C00152.png)
DE (1) DE60032159T2 (US07794700-20100914-C00152.png)
DK (1) DK1218403T3 (US07794700-20100914-C00152.png)
ES (1) ES2187393T1 (US07794700-20100914-C00152.png)
WO (1) WO2001025257A2 (US07794700-20100914-C00152.png)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
US7662960B2 (en) * 2001-04-26 2010-02-16 Choongwae Pharma Corporation Beta-strand mimetics and method relating thereto
US7576084B2 (en) 2001-10-12 2009-08-18 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
US7671054B1 (en) 2001-10-12 2010-03-02 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
US7232822B2 (en) 2001-10-12 2007-06-19 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
US7566711B2 (en) * 2001-10-12 2009-07-28 Choongwae Pharma Corporation Reverse-turn mimetics and method relating thereto
AU2002346915A1 (en) * 2001-10-15 2003-04-28 Therascope Ag A method of forming a dynamic combinatorial library using a scaffold
US20030144260A1 (en) * 2002-01-03 2003-07-31 Yissum Research Development Company Of The Hebrew University Of Jerusalem Heterocyclic compounds, method of developing new drug leads and combinatorial libraries used in such method
US7476653B2 (en) 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
US8921521B2 (en) 2003-06-18 2014-12-30 Ocera Therapeutics, Inc. Macrocyclic modulators of the Ghrelin receptor
DK1633774T3 (da) 2003-06-18 2010-05-25 Tranzyme Pharma Inc Makrocykliske motilinreceptorantagonister
US7491695B2 (en) 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US20090198050A1 (en) * 2003-06-18 2009-08-06 Tranzyme Pharma Inc. Macrocyclic Modulators of the Ghrelin Receptor
USRE42013E1 (en) 2003-06-18 2010-12-28 Tranzyme Pharma Inc. Macrocyclic modulators of the ghrelin receptor
USRE42624E1 (en) 2003-06-18 2011-08-16 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US7550431B2 (en) 2003-07-31 2009-06-23 Tranzyme Pharma Inc. Spatially-defined macrocycles incorporating peptide bond surrogates
EP2316846B1 (en) 2003-07-31 2019-10-02 Ocera Therapeutics, Inc. Spatially-defined macrocyclic compounds useful for drug discovery
JP5730835B2 (ja) * 2004-06-18 2015-06-10 オセラ セラピューティクス， インコーポレイテッド グレリン受容体の大環状モジュレーターの使用方法
JP2008510706A (ja) 2004-08-18 2008-04-10 エリクシアー ファーマシューティカルズ， インコーポレイテッド 成長ホルモン分泌促進物質
EP1810028A2 (en) * 2004-10-14 2007-07-25 Rigel Pharmaceuticals, Inc. Heterocyclic inhibitors of ires-mediated translation and methods of use thereof
WO2006046977A1 (en) * 2004-10-26 2006-05-04 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and methods of using the same
CA2583345A1 (en) * 2005-06-13 2006-12-28 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same
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
EP2431380A3 (en) 2006-09-11 2013-07-03 Tranzyme Pharma, Inc. Macrocyclic antagonist of the motilin receptor for treatment of gastrointestinal dysmotility disorders
EP2997973A1 (en) * 2006-11-15 2016-03-23 Dana-Farber Cancer Institute, Inc. Stabalized maml peptides and uses thereof
EP2644618B1 (en) 2007-02-09 2016-08-17 Ocera Therapeutics, Inc. tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators
BRPI1006139A2 (pt) 2009-01-14 2017-05-30 Aileron Therapeutics Inc macrociclos peptidomiméticos
US20130072439A1 (en) * 2009-09-22 2013-03-21 Huw M. Nash Peptidomimetic macrocycles
CN102812037A (zh) 2009-10-30 2012-12-05 特兰齐姆制药公司 大环生长素释放肽受体拮抗剂和反向激动剂及其使用方法
WO2017004548A1 (en) 2015-07-01 2017-01-05 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2017049383A1 (en) 2015-09-24 2017-03-30 Cyclenium Pharma Inc. Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same
JP2019527672A (ja) * 2016-05-16 2019-10-03 サイクルニウム ファーマ インコーポレイテッド 多様な大環状化合物のライブラリならびにその製造方法および使用方法
CN107200699A (zh) * 2017-06-30 2017-09-26 重庆天原化工有限公司 一种酯化方法及其应用

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4252951A (en) * 1979-10-09 1981-02-24 Eli Lilly And Company Isolation of syn-7-(2-amino-4-thiazolyl)-(methoxyimino)acetamido-3-acetoxymethyl-3-cephem-4-carboxylic acid
CA2103577A1 (en) 1991-02-07 1992-08-08 Michael Kahn Conformationally restricted mimetics of beta turns and beta bulges and peptides containing the same
US5635477A (en) 1991-09-30 1997-06-03 The Dupont Merck Pharmaceutical Company Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA
ES2121088T3 (es) 1992-06-04 1998-11-16 Merrell Pharma Inc Analogos de peptidos limitados conformacionalmente como agentes antiplaquetarios.
WO1996022304A1 (en) * 1995-01-20 1996-07-25 Molecumetics, Ltd. Conformationally constrained reverse-turn library and methods relating thereto
US5900427A (en) * 1996-05-03 1999-05-04 Wisconsin Alumni Research Foundation N-heteroarenesulfonyl-protected amino acid reagents for peptide synthesis
US6355613B1 (en) * 1996-07-31 2002-03-12 Peptor Limited Conformationally constrained backbone cyclized somatostatin analogs
CA2286867A1 (en) * 1997-04-11 1998-10-22 Eli Lilly And Company Combinatorial libraries of peptidomimetic macrocycles and processes therefor
US20020068301A1 (en) * 1997-05-28 2002-06-06 Hung-Sen Lai Cyclic peptide libraries and methods of use thereof to identify binding motifs
AUPP254898A0 (en) * 1998-03-24 1998-04-23 University Of Queensland, The Peptide turn mimetics
US6235877B1 (en) 1999-08-04 2001-05-22 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Peptido-mimetic compounds containing RGD sequence useful as integrin inhibitors
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
US20030144260A1 (en) 2002-01-03 2003-07-31 Yissum Research Development Company Of The Hebrew University Of Jerusalem Heterocyclic compounds, method of developing new drug leads and combinatorial libraries used in such method
IL162604A0 (en) 2002-01-03 2005-11-20 Yissum Res Dev Co Conformationally constrained c-backbone cyclic peptides
TWI294882B (en) * 2002-12-09 2008-03-21 Hoffmann La Roche Anhydrous crystalline azido cytosine hemisulfate derivative
DK1633774T3 (da) * 2003-06-18 2010-05-25 Tranzyme Pharma Inc Makrocykliske motilinreceptorantagonister

Also Published As

Publication number Publication date
US20150315235A1 (en) 2015-11-05
EP1218403B1 (en) 2006-11-29
JP5680577B2 (ja) 2015-03-04
JP6373699B2 (ja) 2018-08-15
JP2012162528A (ja) 2012-08-30
WO2001025257A3 (en) 2001-12-06
JP2017075154A (ja) 2017-04-20
JP2015057390A (ja) 2015-03-26
US7169899B1 (en) 2007-01-30
JP2003511387A (ja) 2003-03-25
CA2284459A1 (en) 2001-04-04
US20120046441A1 (en) 2012-02-23
ATE346857T1 (de) 2006-12-15
DE60032159T2 (de) 2007-10-25
US8188216B2 (en) 2012-05-29
JP6407942B2 (ja) 2018-10-17
CA2284459C (en) 2012-12-11
JP5755530B2 (ja) 2015-07-29
US9018419B2 (en) 2015-04-28
US20050049234A1 (en) 2005-03-03
US9409945B2 (en) 2016-08-09
US8008440B2 (en) 2011-08-30
ES2187393T1 (es) 2003-06-16
US20070117154A1 (en) 2007-05-24
DE60032159D1 (de) 2007-01-11
AU7636100A (en) 2001-05-10
WO2001025257A2 (en) 2001-04-12
EP1218403A2 (en) 2002-07-03
JP5005865B2 (ja) 2012-08-22
JP2012140400A (ja) 2012-07-26

Similar Documents

Publication Publication Date Title
DK1218403T3 (da) Kombinationssyntese af biblioteker af makrocykliske forbindelser, der er anvendelige til medikamentopdagelse
NO20033579D0 (no) Fremgangsmåte for syntetisering av camptothecin relaterte forbindelser
NO20025186D0 (no) FremgangsmÕte for syntese av en ecteinascidinforbindelse
ATE307123T1 (de) Synthese von epothilonen, ihren zwischenprodukten und analogen verbindungen
UY26899A1 (es) Derivados de pirazol fusionados
EA200301289A1 (ru) Новые производные пиррола в качестве фармацевтических средств
EA200200940A1 (ru) Производные азетидина, способ их получения и содержащие их фармацевтические композиции
BR0213140A (pt) Fungicidas de pirazol-pirimidina
AR038818A1 (es) Compuesto de piperidina, uso del mismo para preparar un medicamento, composicion farmaceutica que lo comprende y procedimiento para su preparacion
DE60118754D1 (de) Bicyclische verbindungen als h3 rezeptor liganden
CN101351444B (zh) 具有组蛋白脱乙酰基酶抑制活性的吡咯衍生物
WO2002079753A3 (en) 2-aminobenzoxazole derivatives and combinatorial libraries thereof
DE60235365D1 (de) Verfahren zur herstellung von 7-amino-syn-3,5-dihydroxyheptansäurederivaten und zwischenverbindungen diesesverfahrens und deren herestellung
DE69802453D1 (de) Herstellung von bioaktiven Verbindungen durch Plasmasynthese
CY1106396T1 (el) Γραμμικες ή κυκλικες ουριες, μεθοδος παρασκευης αυτων και φαρμακευτικες συνθεσεις οι οποιες τις πepιεχουν
DK1569918T3 (da) Triazinforbindelser og anvendelse deraf til fremstilling af multidimensionale biblioteker for affinitetskromatografi
Hu et al. Solid-phase based synthesis of jasplakinolide analogs by intramolecular azide–alkyne cycloadditions
WO1999032447A3 (en) 2,4,6-trisubstituted pyridines with estrogenic activity and methods for the solid phase synthesis thereof
IL153682A0 (en) Variolin derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same
NO20032401L (no) Fremgangsmåte ved fremstilling av taksanderivater
ATE399778T1 (de) Glucopyranosid, verfahren zu deren isolierung, pharmazeutische zusammensetzung und verwendung davon
ATE360818T1 (de) Festphasensynthese von n,n-disubstituierten diazacycloalkylcarboxy-derivaten
HUP9900114A2 (hu) Szubsztituált N-metilén-tiokarbamid-származékok és ezeket tartalmazó kártevőírtó készítmények
DK1307436T3 (da) Fremgangsmåde til fremstilling af baccatin III-derivater
DK1250335T3 (da) Fremgangsmåde og mellemprodukter til fremstilling af imidazopyridiner