JP5005865B2 - 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 - Google Patents
創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 Download PDFInfo
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- JP5005865B2 JP5005865B2 JP2001528200A JP2001528200A JP5005865B2 JP 5005865 B2 JP5005865 B2 JP 5005865B2 JP 2001528200 A JP2001528200 A JP 2001528200A JP 2001528200 A JP2001528200 A JP 2001528200A JP 5005865 B2 JP5005865 B2 JP 5005865B2
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- 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
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- Proteomics, Peptides & Aminoacids (AREA)
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Applications Claiming Priority (3)
| 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 |
| CA2,284,459 | 1999-10-04 | ||
| PCT/CA2000/001151 WO2001025257A2 (en) | 1999-10-04 | 2000-10-04 | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011179715A Division JP5755530B2 (ja) | 1999-10-04 | 2011-08-19 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2012049644A Division JP5680577B2 (ja) | 1999-10-04 | 2012-03-06 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
Publications (2)
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| JP2003511387A JP2003511387A (ja) | 2003-03-25 |
| JP5005865B2 true JP5005865B2 (ja) | 2012-08-22 |
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| JP2001528200A Expired - Lifetime JP5005865B2 (ja) | 1999-10-04 | 2000-10-04 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2011179715A Expired - Lifetime JP5755530B2 (ja) | 1999-10-04 | 2011-08-19 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2012049644A Expired - Fee Related JP5680577B2 (ja) | 1999-10-04 | 2012-03-06 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2014192560A Expired - Lifetime JP6373699B2 (ja) | 1999-10-04 | 2014-09-22 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2016220491A Expired - Lifetime JP6407942B2 (ja) | 1999-10-04 | 2016-11-11 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
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| JP2011179715A Expired - Lifetime JP5755530B2 (ja) | 1999-10-04 | 2011-08-19 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2012049644A Expired - Fee Related JP5680577B2 (ja) | 1999-10-04 | 2012-03-06 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2014192560A Expired - Lifetime JP6373699B2 (ja) | 1999-10-04 | 2014-09-22 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| JP2016220491A Expired - Lifetime JP6407942B2 (ja) | 1999-10-04 | 2016-11-11 | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
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| 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) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015057390A (ja) * | 1999-10-04 | 2015-03-26 | オセラ・セラピューティクス・インコーポレイテッドOcera Therapeutics, Inc. | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
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| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO1998046631A1 (en) * | 1997-04-11 | 1998-10-22 | Eli Lilly And Company | Combinatorial libraries of peptidomimetic macrocycles and processes therefor |
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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 |
| 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 |
| 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 |
-
1999
- 1999-10-04 CA CA2284459A patent/CA2284459C/en not_active Expired - Lifetime
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2000
- 2000-10-04 AU AU76361/00A patent/AU7636100A/en not_active Abandoned
- 2000-10-04 JP JP2001528200A patent/JP5005865B2/ja not_active Expired - Lifetime
- 2000-10-04 US US09/679,331 patent/US7169899B1/en not_active Expired - Lifetime
- 2000-10-04 EP EP00965687A patent/EP1218403B1/en not_active Expired - Lifetime
- 2000-10-04 WO PCT/CA2000/001151 patent/WO2001025257A2/en not_active Ceased
- 2000-10-04 ES ES00965687T patent/ES2187393T1/es active Pending
- 2000-10-04 DE DE60032159T patent/DE60032159T2/de not_active Expired - Lifetime
- 2000-10-04 DK DK00965687T patent/DK1218403T3/da active
- 2000-10-04 AT AT00965687T patent/ATE346857T1/de not_active IP Right Cessation
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2004
- 2004-10-07 US US10/961,856 patent/US8188216B2/en not_active Expired - Fee Related
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2006
- 2006-12-22 US US11/615,332 patent/US8008440B2/en not_active Expired - Fee Related
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2011
- 2011-08-19 JP JP2011179715A patent/JP5755530B2/ja not_active Expired - Lifetime
- 2011-08-26 US US13/218,784 patent/US9018419B2/en not_active Expired - Fee Related
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2012
- 2012-03-06 JP JP2012049644A patent/JP5680577B2/ja not_active Expired - Fee Related
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2014
- 2014-09-22 JP JP2014192560A patent/JP6373699B2/ja not_active Expired - Lifetime
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2015
- 2015-04-27 US US14/696,742 patent/US9409945B2/en not_active Expired - Fee Related
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2016
- 2016-11-11 JP JP2016220491A patent/JP6407942B2/ja not_active Expired - Lifetime
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998046631A1 (en) * | 1997-04-11 | 1998-10-22 | Eli Lilly And Company | Combinatorial libraries of peptidomimetic macrocycles and processes therefor |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015057390A (ja) * | 1999-10-04 | 2015-03-26 | オセラ・セラピューティクス・インコーポレイテッドOcera Therapeutics, Inc. | 創薬に有用な大環状化合物ライブラリーのコンビナトリアル合成 |
| US9409945B2 (en) | 1999-10-04 | 2016-08-09 | Ocera Therapeutics, Inc. | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
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| DK1218403T3 (da) | 2007-04-10 |
| US8008440B2 (en) | 2011-08-30 |
| US8188216B2 (en) | 2012-05-29 |
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| US9409945B2 (en) | 2016-08-09 |
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| DE60032159T2 (de) | 2007-10-25 |
| US20050049234A1 (en) | 2005-03-03 |
| ES2187393T1 (es) | 2003-06-16 |
| ATE346857T1 (de) | 2006-12-15 |
| US20150315235A1 (en) | 2015-11-05 |
| JP5680577B2 (ja) | 2015-03-04 |
| 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 |
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