WO2001025257A3 - Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery - Google Patents
Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery Download PDFInfo
- Publication number
- WO2001025257A3 WO2001025257A3 PCT/CA2000/001151 CA0001151W WO0125257A3 WO 2001025257 A3 WO2001025257 A3 WO 2001025257A3 CA 0001151 W CA0001151 W CA 0001151W WO 0125257 A3 WO0125257 A3 WO 0125257A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- bivalent radical
- libraries
- compounds useful
- drug discovery
- macrocyclic compounds
- Prior art date
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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)
- Anesthesiology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
Abstract
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE60032159T DE60032159T2 (en) | 1999-10-04 | 2000-10-04 | COMBINATIONAL PREPARATION OF LIBRARIES FROM MACROCYCLIC COMPOUNDS FOR THE DISCOVERY OF PHARMACEUTICAL ACTIVE SUBSTANCES |
DK00965687T DK1218403T3 (en) | 1999-10-04 | 2000-10-04 | Combination synthesis of libraries of macrocyclic compounds useful for drug discovery |
AU76361/00A AU7636100A (en) | 1999-10-04 | 2000-10-04 | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
JP2001528200A JP5005865B2 (en) | 1999-10-04 | 2000-10-04 | Combinatorial synthesis of macrocyclic compound libraries useful for drug discovery |
EP00965687A EP1218403B1 (en) | 1999-10-04 | 2000-10-04 | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CA2,284,459 | 1999-10-04 | ||
CA2284459A CA2284459C (en) | 1999-10-04 | 1999-10-04 | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2001025257A2 WO2001025257A2 (en) | 2001-04-12 |
WO2001025257A3 true WO2001025257A3 (en) | 2001-12-06 |
Family
ID=4164289
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/CA2000/001151 WO2001025257A2 (en) | 1999-10-04 | 2000-10-04 | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
Country Status (10)
Country | Link |
---|---|
US (5) | US7169899B1 (en) |
EP (1) | EP1218403B1 (en) |
JP (5) | JP5005865B2 (en) |
AT (1) | ATE346857T1 (en) |
AU (1) | AU7636100A (en) |
CA (1) | CA2284459C (en) |
DE (1) | DE60032159T2 (en) |
DK (1) | DK1218403T3 (en) |
ES (1) | ES2187393T1 (en) |
WO (1) | WO2001025257A2 (en) |
Families Citing this family (33)
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 |
US7566711B2 (en) * | 2001-10-12 | 2009-07-28 | 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 |
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 |
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 |
USRE42624E1 (en) | 2003-06-18 | 2011-08-16 | Tranzyme Pharma Inc. | Methods of using 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 |
US8921521B2 (en) * | 2003-06-18 | 2014-12-30 | Ocera Therapeutics, Inc. | 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 |
US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
DE602004025569D1 (en) * | 2003-06-18 | 2010-04-01 | Tranzyme Pharma Inc | MACROCYCLIC MOTILIN RECEPTOR ANTAGONISTS |
DE602004018782D1 (en) | 2003-07-31 | 2009-02-12 | Tranzyme Pharma Inc | SPATIALLY DEFINED MACROCYCLES CONTAINING PEPTIDE BONDING SURROGATES |
WO2005012331A1 (en) * | 2003-07-31 | 2005-02-10 | Tranzyme Pharma | Spatially-defined macrocyclic compounds useful for drug discovery |
JP5730835B2 (en) * | 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 | Use of macrocyclic modulators of ghrelin receptor |
AU2005277389A1 (en) | 2004-08-18 | 2006-03-02 | 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 |
JP5122446B2 (en) * | 2005-06-13 | 2013-01-16 | トランザイム・ファーマ,インコーポレイテッド | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of use thereof |
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 |
WO2008061192A2 (en) * | 2006-11-15 | 2008-05-22 | Dana-Farber Cancer Institute, Inc. | Stabilized maml peptides and uses thereof |
BRPI0807046A2 (en) | 2007-02-09 | 2015-05-26 | Tranzyme Pharma Inc | Compound, pharmaceutical composition, methods of treating a disorder, cardiovascular disease and a patient suffering from reduced or dysfunctional gastrointestinal motility and, kit. |
AU2010204648B2 (en) | 2009-01-14 | 2016-09-01 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
CA2774973A1 (en) | 2009-09-22 | 2011-03-31 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
JP2013509434A (en) | 2009-10-30 | 2013-03-14 | トランザイム・ファーマ,インコーポレイテッド | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of use thereof |
US10059741B2 (en) | 2015-07-01 | 2018-08-28 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
US10407442B2 (en) | 2015-09-24 | 2019-09-10 | Cyclenium Pharma Inc. | Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same |
EP3458630A4 (en) * | 2016-05-16 | 2020-01-08 | Cyclenium Pharma Inc. | Libraries of diverse macrocyclic compounds and methods of making and using the same |
CN107200699A (en) * | 2017-06-30 | 2017-09-26 | 重庆天原化工有限公司 | A kind of esterification process and its application |
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WO1992013878A2 (en) * | 1991-02-07 | 1992-08-20 | Board Of Trustees Of The University Of Illinois | Conformationally restricted mimetics of beta turns and beta bulges and peptides containing the same |
WO1996022304A1 (en) * | 1995-01-20 | 1996-07-25 | Molecumetics, Ltd. | Conformationally constrained reverse-turn library and methods relating thereto |
WO1998046631A1 (en) * | 1997-04-11 | 1998-10-22 | Eli Lilly And Company | Combinatorial libraries of peptidomimetic macrocycles and processes therefor |
WO1998054577A1 (en) * | 1997-05-28 | 1998-12-03 | Beth Israel Deaconess Medical Center, Inc. | Cyclic peptide libraries and methods of use thereof to identify binding motifs |
US5900427A (en) * | 1996-05-03 | 1999-05-04 | Wisconsin Alumni Research Foundation | N-heteroarenesulfonyl-protected amino acid reagents for peptide synthesis |
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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 |
US5635477A (en) | 1991-09-30 | 1997-06-03 | The Dupont Merck Pharmaceutical Company | Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA |
DE69319733T2 (en) | 1992-06-04 | 1999-01-14 | Merrell Dow Pharma | IN THE INFORMATION RESTRICTED PEPTIDE ANALOGS AS AN ACTIVE SUBSTANCE AGAINST PLATE AGGREGATION |
US6355613B1 (en) | 1996-07-31 | 2002-03-12 | Peptor Limited | Conformationally constrained backbone cyclized somatostatin analogs |
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 |
AU2003207940A1 (en) | 2002-01-03 | 2003-07-30 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Conformationally constrained c-backbone cyclic peptides |
TWI294882B (en) * | 2002-12-09 | 2008-03-21 | Hoffmann La Roche | Anhydrous crystalline azido cytosine hemisulfate derivative |
DE602004025569D1 (en) * | 2003-06-18 | 2010-04-01 | Tranzyme Pharma Inc | MACROCYCLIC MOTILIN RECEPTOR ANTAGONISTS |
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1999
- 1999-10-04 CA CA2284459A patent/CA2284459C/en not_active Expired - Lifetime
-
2000
- 2000-10-04 DK DK00965687T patent/DK1218403T3/en active
- 2000-10-04 WO PCT/CA2000/001151 patent/WO2001025257A2/en active IP Right Grant
- 2000-10-04 DE DE60032159T patent/DE60032159T2/en not_active Expired - Lifetime
- 2000-10-04 AT AT00965687T patent/ATE346857T1/en not_active IP Right Cessation
- 2000-10-04 JP JP2001528200A patent/JP5005865B2/en not_active Expired - Lifetime
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US8188216B2 (en) | 2012-05-29 |
DK1218403T3 (en) | 2007-04-10 |
EP1218403A2 (en) | 2002-07-03 |
JP2015057390A (en) | 2015-03-26 |
JP6407942B2 (en) | 2018-10-17 |
US20050049234A1 (en) | 2005-03-03 |
US20150315235A1 (en) | 2015-11-05 |
ATE346857T1 (en) | 2006-12-15 |
US20120046441A1 (en) | 2012-02-23 |
EP1218403B1 (en) | 2006-11-29 |
JP2012140400A (en) | 2012-07-26 |
WO2001025257A2 (en) | 2001-04-12 |
US9409945B2 (en) | 2016-08-09 |
JP2017075154A (en) | 2017-04-20 |
JP5755530B2 (en) | 2015-07-29 |
US20070117154A1 (en) | 2007-05-24 |
JP5005865B2 (en) | 2012-08-22 |
DE60032159D1 (en) | 2007-01-11 |
CA2284459A1 (en) | 2001-04-04 |
JP2012162528A (en) | 2012-08-30 |
CA2284459C (en) | 2012-12-11 |
DE60032159T2 (en) | 2007-10-25 |
AU7636100A (en) | 2001-05-10 |
ES2187393T1 (en) | 2003-06-16 |
JP6373699B2 (en) | 2018-08-15 |
US8008440B2 (en) | 2011-08-30 |
JP5680577B2 (en) | 2015-03-04 |
US9018419B2 (en) | 2015-04-28 |
JP2003511387A (en) | 2003-03-25 |
US7169899B1 (en) | 2007-01-30 |
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