JP2015057390A5 - - Google Patents
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- JP2015057390A5 JP2015057390A5 JP2014192560A JP2014192560A JP2015057390A5 JP 2015057390 A5 JP2015057390 A5 JP 2015057390A5 JP 2014192560 A JP2014192560 A JP 2014192560A JP 2014192560 A JP2014192560 A JP 2014192560A JP 2015057390 A5 JP2015057390 A5 JP 2015057390A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- formula
- monovalent
- same meaning
- moiety
- 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.)
- Granted
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- 238000010647 peptide synthesis reaction Methods 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- -1 macrocycle compound Chemical class 0.000 claims 3
- 150000002678 macrocyclic compounds Chemical class 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 claims 1
- PMMYEEVYMWASQN-DMTCNVIQSA-N Hydroxyproline Chemical compound O[C@H]1CN[C@H](C(O)=O)C1 PMMYEEVYMWASQN-DMTCNVIQSA-N 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- PMMYEEVYMWASQN-UHFFFAOYSA-N dl-hydroxyproline Natural products OC1C[NH2+]C(C([O-])=O)C1 PMMYEEVYMWASQN-UHFFFAOYSA-N 0.000 claims 1
- 229960002591 hydroxyproline Drugs 0.000 claims 1
- FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 claims 1
- 0 *C(C(*)=O)N(*(*)CI*)S(*)(=O)=O Chemical compound *C(C(*)=O)N(*(*)CI*)S(*)(=O)=O 0.000 description 2
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 |
| CA2,284,459 | 1999-10-04 |
Related Parent Applications (1)
| 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016220491A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015057390A JP2015057390A (ja) | 2015-03-26 |
| JP2015057390A5 true JP2015057390A5 (https=) | 2018-06-14 |
| JP6373699B2 JP6373699B2 (ja) | 2018-08-15 |
Family
ID=4164289
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (10)
| Country | Link |
|---|---|
| US (5) | US7169899B1 (https=) |
| EP (1) | EP1218403B1 (https=) |
| JP (5) | JP5005865B2 (https=) |
| AT (1) | ATE346857T1 (https=) |
| AU (1) | AU7636100A (https=) |
| CA (1) | CA2284459C (https=) |
| DE (1) | DE60032159T2 (https=) |
| DK (1) | DK1218403T3 (https=) |
| ES (1) | ES2187393T1 (https=) |
| WO (1) | WO2001025257A2 (https=) |
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 |
| 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 |
| 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 |
| WO2003033437A2 (en) * | 2001-10-15 | 2003-04-24 | Therascope Ag | A method of forming neuraminidase inhibitors by dynamic combinatorial chemistry and compounds obtained |
| 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 |
| US7491695B2 (en) * | 2003-06-18 | 2009-02-17 | Tranzyme Pharma Inc. | Methods of using macrocyclic modulators of the ghrelin receptor |
| US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
| US7521420B2 (en) | 2003-06-18 | 2009-04-21 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor |
| US8921521B2 (en) | 2003-06-18 | 2014-12-30 | Ocera Therapeutics, Inc. | Macrocyclic modulators of the Ghrelin receptor |
| USRE42013E1 (en) | 2003-06-18 | 2010-12-28 | Tranzyme Pharma Inc. | Macrocyclic modulators of the ghrelin receptor |
| US20090198050A1 (en) * | 2003-06-18 | 2009-08-06 | 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 |
| ATE490264T1 (de) | 2003-07-31 | 2010-12-15 | Tranzyme Pharma Inc | Räumlich definierte makrocyclische verbindungen, die sich für die entdeckung von arzneimittel eignen |
| US7550431B2 (en) * | 2003-07-31 | 2009-06-23 | Tranzyme Pharma Inc. | Spatially-defined macrocycles incorporating peptide bond surrogates |
| 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 |
| WO2006023608A2 (en) | 2004-08-18 | 2006-03-02 | Elixir Pharmaceuticals, Inc. | Growth-hormone secretagogues |
| WO2006052391A2 (en) * | 2004-10-14 | 2006-05-18 | 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 |
| EP1891090A2 (en) * | 2005-06-13 | 2008-02-27 | 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 |
| EP2054429B1 (en) | 2006-09-11 | 2013-11-06 | Tranzyme Pharma, Inc. | Macrocyclic antagonists 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 |
| KR20090107088A (ko) | 2007-02-09 | 2009-10-12 | 트랜자임 파르마 인크 | 거대고리 그렐린 수용체 조절제 및 이의 사용 방법 |
| WO2010083347A2 (en) | 2009-01-14 | 2010-07-22 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| US20130072439A1 (en) * | 2009-09-22 | 2013-03-21 | Huw M. Nash | Peptidomimetic macrocycles |
| EP2493910A1 (en) | 2009-10-30 | 2012-09-05 | Tranzyme Pharma, Inc. | 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 |
| WO2017197488A1 (en) * | 2016-05-16 | 2017-11-23 | 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)
| 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 |
| 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 |
| US5635477A (en) | 1991-09-30 | 1997-06-03 | The Dupont Merck Pharmaceutical Company | Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA |
| DE69319733T2 (de) | 1992-06-04 | 1999-01-14 | Merrell Dow Pharmaceuticals Inc., Cincinnati, Ohio | In der konformation beschränkte peptid analoge als wirkstoff gegen plättchenaggregation |
| JPH10512570A (ja) | 1995-01-20 | 1998-12-02 | モレキュメティックス リミテッド | コンホメーション的に制限された逆ターンライブラリおよびそれらに関連する方法 |
| 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 |
| JP2002506423A (ja) * | 1997-04-11 | 2002-02-26 | イーライ・リリー・アンド・カンパニー | ペプチド模倣型大員環のコンビナトリアルライブラリーとそのための方法 |
| 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 |
| EP1468013A4 (en) | 2002-01-03 | 2005-03-16 | Yissum Res Dev Co | CYCLIC PEPTIDES WITH CARBON SKELETON HAVING RESTRICTED CONFORMATION |
| 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 |
| US7521420B2 (en) * | 2003-06-18 | 2009-04-21 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor |
-
1999
- 1999-10-04 CA CA2284459A patent/CA2284459C/en not_active Expired - Lifetime
-
2000
- 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 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 AU AU76361/00A patent/AU7636100A/en not_active Abandoned
- 2000-10-04 EP EP00965687A patent/EP1218403B1/en 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
-
2004
- 2004-10-07 US US10/961,856 patent/US8188216B2/en not_active Expired - Fee Related
-
2006
- 2006-12-22 US US11/615,332 patent/US8008440B2/en not_active Expired - Fee Related
-
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
-
2012
- 2012-03-06 JP JP2012049644A patent/JP5680577B2/ja not_active Expired - Fee Related
-
2014
- 2014-09-22 JP JP2014192560A patent/JP6373699B2/ja not_active Expired - Lifetime
-
2015
- 2015-04-27 US US14/696,742 patent/US9409945B2/en not_active Expired - Fee Related
-
2016
- 2016-11-11 JP JP2016220491A patent/JP6407942B2/ja not_active Expired - Lifetime
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