JP4928261B2 - モチリン受容体の大環状拮抗薬 - Google Patents
モチリン受容体の大環状拮抗薬 Download PDFInfo
- Publication number
- JP4928261B2 JP4928261B2 JP2006515603A JP2006515603A JP4928261B2 JP 4928261 B2 JP4928261 B2 JP 4928261B2 JP 2006515603 A JP2006515603 A JP 2006515603A JP 2006515603 A JP2006515603 A JP 2006515603A JP 4928261 B2 JP4928261 B2 JP 4928261B2
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- group
- alkyl
- heterocycle
- independently selected
- 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.)
- Expired - Fee Related
Links
- 0 C*CCOc1cc(OCCO)ccc1 Chemical compound C*CCOc1cc(OCCO)ccc1 0.000 description 3
- VVWRJUBEIPHGQF-MDZDMXLPSA-N CC(C)OC(/N=N/C(OC(C)C)=O)=O Chemical compound CC(C)OC(/N=N/C(OC(C)C)=O)=O VVWRJUBEIPHGQF-MDZDMXLPSA-N 0.000 description 1
- BWCIAGYOTGPTSI-UHFFFAOYSA-N CC(C)OC(N(C)[N+](C)(C(OC(C)C)=O)[O-])=O Chemical compound CC(C)OC(N(C)[N+](C)(C(OC(C)C)=O)[O-])=O BWCIAGYOTGPTSI-UHFFFAOYSA-N 0.000 description 1
- GDESWOTWNNGOMW-UHFFFAOYSA-N Oc1cc(OC(c2ccccc2)=O)ccc1 Chemical compound Oc1cc(OC(c2ccccc2)=O)ccc1 GDESWOTWNNGOMW-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/2214—Motilins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C41/00—Preparation of ethers; Preparation of compounds having groups, groups or groups
- C07C41/01—Preparation of ethers
- C07C41/18—Preparation of ethers by reactions not forming ether-oxygen bonds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
- C07C67/333—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
- C07C67/343—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- 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
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US47922303P | 2003-06-18 | 2003-06-18 | |
US60/479,223 | 2003-06-18 | ||
PCT/CA2004/000913 WO2004111077A1 (en) | 2003-06-18 | 2004-06-18 | Macrocyclic antagonists of the motilin receptor |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2007523853A JP2007523853A (ja) | 2007-08-23 |
JP4928261B2 true JP4928261B2 (ja) | 2012-05-09 |
Family
ID=33551871
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006515603A Expired - Fee Related JP4928261B2 (ja) | 2003-06-18 | 2004-06-18 | モチリン受容体の大環状拮抗薬 |
Country Status (9)
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2012006961A (ja) * | 2004-06-18 | 2012-01-12 | Tranzyme Pharma Inc | グレリン受容体の大環状モジュレーターの使用方法 |
Families Citing this family (38)
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CA2284459C (en) * | 1999-10-04 | 2012-12-11 | Neokimia Inc. | Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery |
US7476653B2 (en) | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
JP4928261B2 (ja) * | 2003-06-18 | 2012-05-09 | トランザイム・ファーマ・インコーポレイテッド | モチリン受容体の大環状拮抗薬 |
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 |
AU2004261329B2 (en) * | 2003-07-31 | 2011-10-27 | Ocera Therapeutics, Inc. | Spatially-defined macrocyclic compounds useful for drug discovery |
US7550431B2 (en) * | 2003-07-31 | 2009-06-23 | Tranzyme Pharma Inc. | Spatially-defined macrocycles incorporating peptide bond surrogates |
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 |
US20090275648A1 (en) * | 2005-06-13 | 2009-11-05 | Fraser Graeme L | 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 |
PT2118123E (pt) | 2007-01-31 | 2016-02-10 | Harvard College | Péptidos de p53 estabilizados e suas utilizações |
AU2015201862B2 (en) * | 2007-02-09 | 2016-10-13 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor modulators and methods of using the same |
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. |
ES2430067T3 (es) | 2007-03-28 | 2013-11-18 | President And Fellows Of Harvard College | Polipéptidos cosidos |
US20080287371A1 (en) * | 2007-05-17 | 2008-11-20 | Tranzyme Pharma Inc. | Macrocyclic antagonists of the motilin receptor for modulation of the migrating motor complex |
WO2010022249A2 (en) * | 2008-08-20 | 2010-02-25 | Ensemble Discovery Corporation | Macrocyclic compounds for inhibition of tumor necrosis factor alpha |
WO2011015241A1 (en) * | 2009-08-05 | 2011-02-10 | Polyphor Ag | Conformationally constrained, fully synthetic macrocyclic compounds |
EP2491004A4 (en) * | 2009-10-23 | 2013-07-03 | Tranzyme Pharma Inc | MACROCYCLIC INHIBITORS OF SERINE PROTEASE CYMS |
JP2013509434A (ja) | 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 | 大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法 |
KR20180058866A (ko) | 2010-08-13 | 2018-06-01 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
BR112014009418A2 (pt) | 2011-10-18 | 2017-04-18 | Aileron Therapeutics Inc | macrociclos peptidomiméticos |
US8927500B2 (en) | 2012-02-15 | 2015-01-06 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
US8987414B2 (en) | 2012-02-15 | 2015-03-24 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
JP6526563B2 (ja) | 2012-11-01 | 2019-06-05 | エイルロン セラピューティクス,インコーポレイテッド | 二置換アミノ酸ならびにその調製および使用の方法 |
US9119832B2 (en) | 2014-02-05 | 2015-09-01 | The Regents Of The University Of California | Methods of treating mild brain injury |
JP2017533889A (ja) | 2014-09-24 | 2017-11-16 | エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. | ペプチド模倣大環状分子およびその使用 |
CA2979847A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
PT3368544T (pt) | 2015-10-27 | 2020-08-20 | Hoffmann La Roche | Péptidos macrocíclicos contra acinetobacter baumannii |
WO2017075535A1 (en) | 2015-10-28 | 2017-05-04 | Oxeia Biopharmaceuticals, Inc. | Methods of treating neurodegenerative conditions |
EP3388444A1 (en) * | 2017-04-10 | 2018-10-17 | F. Hoffmann-La Roche AG | Anti-bacterial peptide macrocycles and use thereof |
US11505573B2 (en) | 2018-03-28 | 2022-11-22 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
US11819532B2 (en) | 2018-04-23 | 2023-11-21 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
CN108752214A (zh) * | 2018-07-09 | 2018-11-06 | 上海华堇生物技术有限责任公司 | 一种2-羟基-β-硝基苯乙烯的新制备方法 |
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WO2004111077A1 (en) | 2004-12-23 |
ES2338789T3 (es) | 2010-05-12 |
US8497242B2 (en) | 2013-07-30 |
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US7521420B2 (en) | 2009-04-21 |
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EP2210612A3 (en) | 2010-11-24 |
EP2210612B1 (en) | 2016-10-05 |
CA2528375C (en) | 2013-11-19 |
US20120226072A1 (en) | 2012-09-06 |
US20110245459A1 (en) | 2011-10-06 |
US20160221927A1 (en) | 2016-08-04 |
JP2007523853A (ja) | 2007-08-23 |
US20050054562A1 (en) | 2005-03-10 |
ATE457995T1 (de) | 2010-03-15 |
US20120165566A1 (en) | 2012-06-28 |
US20120226067A1 (en) | 2012-09-06 |
US10040751B2 (en) | 2018-08-07 |
EP1633774A1 (en) | 2006-03-15 |
EP1633774B1 (en) | 2010-02-17 |
EP2210612A2 (en) | 2010-07-28 |
US20120226066A1 (en) | 2012-09-06 |
DE602004025569D1 (de) | 2010-04-01 |
DK1633774T3 (da) | 2010-05-25 |
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