JP2015057390A5 - - Google Patents
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- Publication number
- 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 |
| US7576084B2 (en) | 2001-10-12 | 2009-08-18 | 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 |
| 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 |
| DK1633774T3 (da) | 2003-06-18 | 2010-05-25 | Tranzyme Pharma Inc | Makrocykliske motilinreceptorantagonister |
| 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 |
| US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, 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 |
| USRE42013E1 (en) | 2003-06-18 | 2010-12-28 | 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 |
| CA2533820C (en) * | 2003-07-31 | 2016-12-13 | Tranzyme Pharma | Spatially-defined macrocycles incorporating peptide bond surrogates |
| AU2004261329B2 (en) | 2003-07-31 | 2011-10-27 | 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 |
| WO2006023608A2 (en) | 2004-08-18 | 2006-03-02 | Elixir Pharmaceuticals, Inc. | Growth-hormone secretagogues |
| US20060116316A1 (en) * | 2004-10-14 | 2006-06-01 | Kinsella Todd M | 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 |
| CN101657436A (zh) | 2007-02-09 | 2010-02-24 | 特兰齐姆制药公司 | 大环生长素释放肽受体调节剂及其使用方法 |
| US9175047B2 (en) | 2009-01-14 | 2015-11-03 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| CN102712675A (zh) * | 2009-09-22 | 2012-10-03 | 爱勒让治疗公司 | 拟肽大环化合物 |
| 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 |
| CA2998885C (en) | 2015-09-24 | 2020-09-01 | Cyclenium Pharma Inc. | Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same |
| 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)
| 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 |
| WO1993024520A1 (en) | 1992-06-04 | 1993-12-09 | Merrell Dow Pharmaceuticals Inc. | Conformationally restrained peptide analogs as antiplatelet agents |
| 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 |
| WO1998046631A1 (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 |
| 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 |
| DK1633774T3 (da) * | 2003-06-18 | 2010-05-25 | Tranzyme Pharma Inc | Makrocykliske motilinreceptorantagonister |
-
1999
- 1999-10-04 CA CA2284459A patent/CA2284459C/en not_active Expired - Lifetime
-
2000
- 2000-10-04 EP EP00965687A patent/EP1218403B1/en not_active Expired - Lifetime
- 2000-10-04 US US09/679,331 patent/US7169899B1/en not_active Expired - Lifetime
- 2000-10-04 JP JP2001528200A patent/JP5005865B2/ja 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 AT AT00965687T patent/ATE346857T1/de not_active IP Right Cessation
- 2000-10-04 DK DK00965687T patent/DK1218403T3/da active
-
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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