CA2528375C - Macrocyclic antagonists of the motilin receptor - Google Patents
Macrocyclic antagonists of the motilin receptor Download PDFInfo
- Publication number
- CA2528375C CA2528375C CA2528375A CA2528375A CA2528375C CA 2528375 C CA2528375 C CA 2528375C CA 2528375 A CA2528375 A CA 2528375A CA 2528375 A CA2528375 A CA 2528375A CA 2528375 C CA2528375 C CA 2528375C
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- CA
- Canada
- Prior art keywords
- boc
- group
- hydrogen
- bts
- ddz
- 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
Classifications
-
- 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
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- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Zoology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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 |
---|---|
CA2528375A1 CA2528375A1 (en) | 2004-12-23 |
CA2528375C true CA2528375C (en) | 2013-11-19 |
Family
ID=33551871
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2528375A Expired - Fee Related CA2528375C (en) | 2003-06-18 | 2004-06-18 | Macrocyclic antagonists of the motilin receptor |
Country Status (9)
Families Citing this family (39)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
US8921521B2 (en) | 2003-06-18 | 2014-12-30 | Ocera Therapeutics, 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 |
USRE42013E1 (en) | 2003-06-18 | 2010-12-28 | 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 |
US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | 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 |
EP1633774B1 (en) * | 2003-06-18 | 2010-02-17 | Tranzyme Pharma Inc. | Macrocyclic antagonists of the motilin receptor |
SI1648922T1 (sl) * | 2003-07-31 | 2011-03-31 | Tranzyme Pharma Inc | Prostorsko opredeljene makrocikliäśne spojine uporabne za odkrivanje zdravil |
DE602004018782D1 (de) * | 2003-07-31 | 2009-02-12 | Tranzyme Pharma Inc | Räumlich definierte makrocyclen, die peptidbindungssurrogate enthalten |
JP5739766B2 (ja) * | 2004-06-18 | 2015-06-24 | 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 |
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 |
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 |
EP2054429B1 (en) * | 2006-09-11 | 2013-11-06 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders |
DK2118123T3 (en) | 2007-01-31 | 2016-01-25 | Dana Farber Cancer Inst Inc | Stabilized p53 peptides and uses thereof |
AU2015201862B2 (en) * | 2007-02-09 | 2016-10-13 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor modulators and methods of using the same |
EA200901077A1 (ru) * | 2007-02-09 | 2010-04-30 | Транзим Фарма, Инк. | Макроциклические модуляторы грелинового рецептора и их применение |
ES2610531T3 (es) | 2007-03-28 | 2017-04-28 | 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 |
EP2350031A2 (en) * | 2008-08-20 | 2011-08-03 | Ensemble Therapeutics Corporation | Macrocyclic compounds for inhibition of tumor necrosis factor alpha |
DK2462147T3 (en) * | 2009-08-05 | 2015-02-23 | Polyphor Ag | Conformationally limited fully synthetic macrocyclic compounds |
US20120270807A1 (en) * | 2009-10-23 | 2012-10-25 | Marsault Eric | Macrocyclic inhibitors of serine protease enzymes |
US20110105389A1 (en) | 2009-10-30 | 2011-05-05 | Hoveyda Hamid R | Macrocyclic Ghrelin Receptor Antagonists and Inverse Agonists and Methods of Using the Same |
ES2711526T3 (es) | 2010-08-13 | 2019-05-06 | Aileron Therapeutics Inc | Macrociclos peptidomiméticos |
RU2639523C2 (ru) | 2011-10-18 | 2017-12-21 | Эйлерон Терапьютикс, Инк. | Пептидомиметические макроциклы и их применение |
MX362492B (es) | 2012-02-15 | 2019-01-21 | Aileron Therapeutics Inc | Macrociclos peptidomiméticos. |
JP6450192B2 (ja) | 2012-02-15 | 2019-01-09 | エイルロン セラピューティクス,インコーポレイテッド | トリアゾール架橋した、およびチオエーテル架橋したペプチドミメティック大環状化合物 |
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US9119832B2 (en) | 2014-02-05 | 2015-09-01 | The Regents Of The University Of California | Methods of treating mild brain injury |
KR20170058424A (ko) | 2014-09-24 | 2017-05-26 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방 거대고리 및 이의 용도 |
EP3294318A4 (en) | 2015-03-20 | 2019-04-03 | Aileron Therapeutics, Inc. | PEPTIDOMIMETIC MACROCYCLES AND USES THEREOF |
DK3368544T3 (da) * | 2015-10-27 | 2020-08-24 | Hoffmann La Roche | Peptidmakrocykler mod Acinetobacter baumannii |
US20170121385A1 (en) | 2015-10-28 | 2017-05-04 | Oxeia Biopharmaceuticals, Inc. | Methods of treating neurodegenerative conditions |
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US11505573B2 (en) | 2018-03-28 | 2022-11-22 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
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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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- 2004-06-18 EP EP04737852A patent/EP1633774B1/en not_active Expired - Lifetime
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- 2004-06-18 US US10/872,142 patent/US7521420B2/en not_active Expired - Lifetime
- 2004-06-18 DK DK04737852.6T patent/DK1633774T3/da active
- 2004-06-18 WO PCT/CA2004/000913 patent/WO2004111077A1/en active Search and Examination
- 2004-06-18 DE DE602004025569T patent/DE602004025569D1/de not_active Expired - Lifetime
- 2004-06-18 ES ES04737852T patent/ES2338789T3/es not_active Expired - Lifetime
- 2004-06-18 JP JP2006515603A patent/JP4928261B2/ja not_active Expired - Fee Related
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- 2008-11-19 US US12/273,638 patent/US9181298B2/en active Active
- 2008-11-19 US US12/273,648 patent/US8129561B2/en not_active Expired - Fee Related
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Also Published As
Publication number | Publication date |
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JP4928261B2 (ja) | 2012-05-09 |
US20090137835A1 (en) | 2009-05-28 |
DK1633774T3 (da) | 2010-05-25 |
US20050054562A1 (en) | 2005-03-10 |
DE602004025569D1 (de) | 2010-04-01 |
US10040751B2 (en) | 2018-08-07 |
US20120226066A1 (en) | 2012-09-06 |
US20090240027A1 (en) | 2009-09-24 |
US20110245459A1 (en) | 2011-10-06 |
US20160221927A1 (en) | 2016-08-04 |
US8129561B2 (en) | 2012-03-06 |
ATE457995T1 (de) | 2010-03-15 |
US8497242B2 (en) | 2013-07-30 |
ES2338789T3 (es) | 2010-05-12 |
EP2210612A2 (en) | 2010-07-28 |
US20120226067A1 (en) | 2012-09-06 |
EP2210612A3 (en) | 2010-11-24 |
EP1633774A1 (en) | 2006-03-15 |
EP2210612B1 (en) | 2016-10-05 |
CA2528375A1 (en) | 2004-12-23 |
JP2007523853A (ja) | 2007-08-23 |
WO2004111077A1 (en) | 2004-12-23 |
US9181298B2 (en) | 2015-11-10 |
US7521420B2 (en) | 2009-04-21 |
EP1633774B1 (en) | 2010-02-17 |
US20120226072A1 (en) | 2012-09-06 |
US20120165566A1 (en) | 2012-06-28 |
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