ES2187393T1 - Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos. - Google Patents

Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos.

Info

Publication number
ES2187393T1
ES2187393T1 ES00965687T ES00965687T ES2187393T1 ES 2187393 T1 ES2187393 T1 ES 2187393T1 ES 00965687 T ES00965687 T ES 00965687T ES 00965687 T ES00965687 T ES 00965687T ES 2187393 T1 ES2187393 T1 ES 2187393T1
Authority
ES
Spain
Prior art keywords
useful
bivalent radical
macrociclic
pharmacos
discovery
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
Application number
ES00965687T
Other languages
English (en)
Spanish (es)
Inventor
Pierre Deslongchamps
Yves Dory
Gilles Berthiaume
Luc Ouellet
Ruoxi Lan
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.)
Neokimia Inc
Original Assignee
Neokimia 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 Neokimia Inc filed Critical Neokimia Inc
Publication of ES2187393T1 publication Critical patent/ES2187393T1/es
Pending legal-status Critical Current

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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Analytical Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Anesthesiology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
ES00965687T 1999-10-04 2000-10-04 Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos. Pending ES2187393T1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ES2187393T1 true ES2187393T1 (es) 2003-06-16

Family

ID=4164289

Family Applications (1)

Application Number Title Priority Date Filing Date
ES00965687T Pending ES2187393T1 (es) 1999-10-04 2000-10-04 Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos.

Country Status (10)

Country Link
US (5) US7169899B1 (enExample)
EP (1) EP1218403B1 (enExample)
JP (5) JP5005865B2 (enExample)
AT (1) ATE346857T1 (enExample)
AU (1) AU7636100A (enExample)
CA (1) CA2284459C (enExample)
DE (1) DE60032159T2 (enExample)
DK (1) DK1218403T3 (enExample)
ES (1) ES2187393T1 (enExample)
WO (1) WO2001025257A2 (enExample)

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
US7671054B1 (en) 2001-10-12 2010-03-02 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
US7576084B2 (en) 2001-10-12 2009-08-18 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
WO2003034071A2 (en) * 2001-10-15 2003-04-24 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
US20090198050A1 (en) * 2003-06-18 2009-08-06 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
US7491695B2 (en) 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using 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
DE602004025569D1 (de) 2003-06-18 2010-04-01 Tranzyme Pharma Inc Makrozyklische motilin rezeptorantagonisten
US7476653B2 (en) 2003-06-18 2009-01-13 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
WO2005012332A1 (en) * 2003-07-31 2005-02-10 Tranzyme Pharma Spatially-defined macrocycles incorporating peptide bond surrogates
PL1648922T3 (pl) 2003-07-31 2011-05-31 Tranzyme Pharma Inc Przestrzennie określone związki makrocykliczne użyteczne w dziedzinie odkrywania leków
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
EP2389941A1 (en) 2004-08-18 2011-11-30 Elixir Pharmaceuticals, Inc. Growth-hormone secretagogues
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
CA2662897C (en) 2006-09-11 2017-11-07 Tranzyme Pharma, Inc. Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders
EP2091552A4 (en) * 2006-11-15 2010-01-06 Dana Farber Cancer Inst Inc STABILIZED MAML-PEPTIDES AND ITS USES
BRPI0807046A2 (pt) 2007-02-09 2015-05-26 Tranzyme Pharma Inc Composto, composição farmacêutica, métodos de tratar um distúrbio, uma doença cardiovascular e um paciente que sofre de motilidade gastrointestinal reduzida ou disfuncional e, kit.
EP2376100B1 (en) 2009-01-14 2017-10-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2011038049A1 (en) * 2009-09-22 2011-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US20110105389A1 (en) 2009-10-30 2011-05-05 Hoveyda Hamid R Macrocyclic Ghrelin Receptor Antagonists and Inverse Agonists and Methods of Using the Same
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP6783311B2 (ja) 2015-09-24 2020-11-11 サイクレニウム ファーマ インコーポレーテッド ヘテロアリール含有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
CA3024071C (en) * 2016-05-16 2023-02-21 Cyclenium Pharma Inc. Libraries of diverse macrocyclic compounds and methods of making and using the same
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
JPH06505486A (ja) 1991-02-07 1994-06-23 モレキュメティクス，リミティド βターンおよびβバルジのコンフォメーション的に制限された模倣物およびそれらを含有するペプチド
US5635477A (en) 1991-09-30 1997-06-03 The Dupont Merck Pharmaceutical Company Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA
JP3398747B2 (ja) 1992-06-04 2003-04-21 メレルダウファーマスーティカルズ インコーポレイテッド 抗血小板剤としての立体配位が制限されたペプチド類似体
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
AU6895598A (en) * 1997-04-11 1998-11-11 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
IL162604A0 (en) 2002-01-03 2005-11-20 Yissum Res Dev Co Conformationally constrained c-backbone cyclic peptides
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
TWI294882B (en) * 2002-12-09 2008-03-21 Hoffmann La Roche Anhydrous crystalline azido cytosine hemisulfate derivative
DE602004025569D1 (de) * 2003-06-18 2010-04-01 Tranzyme Pharma Inc Makrozyklische motilin rezeptorantagonisten

Also Published As

Publication number Publication date
DK1218403T3 (da) 2007-04-10
US8008440B2 (en) 2011-08-30
US8188216B2 (en) 2012-05-29
AU7636100A (en) 2001-05-10
US9409945B2 (en) 2016-08-09
JP6373699B2 (ja) 2018-08-15
DE60032159T2 (de) 2007-10-25
US20050049234A1 (en) 2005-03-03
ATE346857T1 (de) 2006-12-15
US20150315235A1 (en) 2015-11-05
JP5680577B2 (ja) 2015-03-04
JP5005865B2 (ja) 2012-08-22
DE60032159D1 (de) 2007-01-11
CA2284459C (en) 2012-12-11
US20120046441A1 (en) 2012-02-23
US7169899B1 (en) 2007-01-30
JP2015057390A (ja) 2015-03-26
EP1218403B1 (en) 2006-11-29
US20070117154A1 (en) 2007-05-24
EP1218403A2 (en) 2002-07-03
JP2012162528A (ja) 2012-08-30
WO2001025257A2 (en) 2001-04-12
US9018419B2 (en) 2015-04-28
JP6407942B2 (ja) 2018-10-17
WO2001025257A3 (en) 2001-12-06
CA2284459A1 (en) 2001-04-04
JP2017075154A (ja) 2017-04-20
JP2003511387A (ja) 2003-03-25
JP2012140400A (ja) 2012-07-26
JP5755530B2 (ja) 2015-07-29

Similar Documents

Publication Publication Date Title
ES2187393T1 (es) Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos.
ATE307123T1 (de) Synthese von epothilonen, ihren zwischenprodukten und analogen verbindungen
BG103250A (bg) Модифицирани аминокиселини и лекарствени средства, които съдържат тези съединения
CY1105087T1 (el) Νεες αντιβακτηριακες ουσιες
DE3752345D1 (de) Elektrolumineszente Verbindungen und Zwischenprodukte zur Herstellung
AU2001261319A1 (en) Combinatorial synthesis of material chips
DK1506203T3 (da) Syntese af epothiloner, mellemprodukter deraf, analoger deraf og anvendelser deraf
NO20025186D0 (no) FremgangsmÕte for syntese av en ecteinascidinforbindelse
NO20033579D0 (no) Fremgangsmåte for syntetisering av camptothecin relaterte forbindelser
EA200400893A1 (ru) N-арил-2-оксазолидинон-5-карбоксамиды, их производные и их применение в качестве антибактериальных средств
NO20004090D0 (no) Kjemiske forbindelser
PT1206484E (pt) Compostos e composicoes antipicornavirais, suas utilizacoes farmaceuticas e materiais para a sua sintese
ATE323076T1 (de) Bicyclische verbindungen als h3 rezeptor liganden
FI962371A0 (fi) Menetelmä kombinatoristen yhdistekirjastojen valmistamiseksi
Cheguillaume et al. Submonomer solution synthesis of hydrazinoazapeptoids, a new class of pseudopeptides
DE69802453D1 (de) Herstellung von bioaktiven Verbindungen durch Plasmasynthese
HUP0201475A2 (hu) Heteroarilamidin-, metilamidin- és guanidinszármazékok, előállításuk és alkalmazásuk, valamint e vegyületeket tartalmazó gyógyászati készítmények
DE69937045D1 (de) Cyclische amidderivate
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
WO2003022844A3 (en) Synthesis of epothilones intermediates thereto and analogues thereof
EA200100213A1 (ru) Способ синтеза производных (1h)-бензо[c]хинолизин-3-онов
CY1106396T1 (el) Γραμμικες ή κυκλικες ουριες, μεθοδος παρασκευης αυτων και φαρμακευτικες συνθεσεις οι οποιες τις πepιεχουν
Hu et al. Solid-phase based synthesis of jasplakinolide analogs by intramolecular azide–alkyne cycloadditions
Lai et al. Ring size effect in the PKC inhibitory activities of perhydroazepine analogs of balanol