WO2006009674A1 - Macrocyclic modulators of the ghrelin receptor - Google Patents
Macrocyclic modulators of the ghrelin receptor Download PDFInfo
- Publication number
- WO2006009674A1 WO2006009674A1 PCT/US2005/020857 US2005020857W WO2006009674A1 WO 2006009674 A1 WO2006009674 A1 WO 2006009674A1 US 2005020857 W US2005020857 W US 2005020857W WO 2006009674 A1 WO2006009674 A1 WO 2006009674A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- substituted
- ring
- alkyl
- hydrogen
- optionally
- Prior art date
Links
- 0 CC(C1*)=C(*)C(*)*C1I Chemical compound CC(C1*)=C(*)C(*)*C1I 0.000 description 13
- WEHMXWJFCCNXHJ-UHFFFAOYSA-N C=C=Cc1ccccc1 Chemical compound C=C=Cc1ccccc1 WEHMXWJFCCNXHJ-UHFFFAOYSA-N 0.000 description 1
- VXGRMCZTYDXKQW-YFKPBYRVSA-N CCC[C@@H](C(OC)=O)N Chemical compound CCC[C@@H](C(OC)=O)N VXGRMCZTYDXKQW-YFKPBYRVSA-N 0.000 description 1
- PONXAJCQJXECCB-UFKXBGGNSA-N C[C@H](C(N[C@H](Cc(cc1)ccc1F)C(NCCCc(ccc(Cl)c1)c1OCCN[C@H]1C2CC2)=O)=O)N(C)C1=O Chemical compound C[C@H](C(N[C@H](Cc(cc1)ccc1F)C(NCCCc(ccc(Cl)c1)c1OCCN[C@H]1C2CC2)=O)=O)N(C)C1=O PONXAJCQJXECCB-UFKXBGGNSA-N 0.000 description 1
- VLHQXRIIQSTJCQ-ZCFIWIBFSA-N C[C@H](C(O)=O)N(C)C(OC(C)(C)C)=O Chemical compound C[C@H](C(O)=O)N(C)C(OC(C)(C)C)=O VLHQXRIIQSTJCQ-ZCFIWIBFSA-N 0.000 description 1
- FPRSPUHXEPWUBZ-OAHLLOKOSA-N N[C@H](Cc1ccccc1)C(OCc1ccccc1)=O Chemical compound N[C@H](Cc1ccccc1)C(OCc1ccccc1)=O FPRSPUHXEPWUBZ-OAHLLOKOSA-N 0.000 description 1
- YZIXMEXARCDRCW-UHFFFAOYSA-N OCCCc1ccccc1C=O Chemical compound OCCCc1ccccc1C=O YZIXMEXARCDRCW-UHFFFAOYSA-N 0.000 description 1
- VCSQSPVHFDOWER-UHFFFAOYSA-N OCCCc1ccccc1CO Chemical compound OCCCc1ccccc1CO VCSQSPVHFDOWER-UHFFFAOYSA-N 0.000 description 1
- ADLOWZRDUHSVRU-UHFFFAOYSA-N OCCc1ccccc1Br Chemical compound OCCc1ccccc1Br ADLOWZRDUHSVRU-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- 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
- 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
- C07D498/08—Bridged 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
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Nutrition Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CA2579726A CA2579726C (en) | 2004-06-18 | 2005-06-13 | Macrocyclic modulators of the ghrelin receptor |
JP2007516620A JP5363726B2 (ja) | 2004-06-18 | 2005-06-13 | グレリン受容体の大環状モジュレーターの使用方法 |
CN2005800280726A CN101111512B (zh) | 2004-06-18 | 2005-06-13 | 生长素释放肽受体的大环调节剂 |
ES05785185T ES2393498T3 (es) | 2004-06-18 | 2005-06-13 | Moduladores macrocíclicos del receptor de ghrelina |
EP05785185A EP1773869B9 (en) | 2004-06-18 | 2005-06-13 | Macrocyclic modulators of the ghrelin receptor |
Applications Claiming Priority (11)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10/872,142 US7521420B2 (en) | 2003-06-18 | 2004-06-18 | Macrocyclic antagonists of the motilin receptor |
US10/872,142 | 2004-06-18 | ||
US62164204P | 2004-10-26 | 2004-10-26 | |
US60/621,642 | 2004-10-26 | ||
US62200504P | 2004-10-27 | 2004-10-27 | |
US60/622,055 | 2004-10-27 | ||
US60/622,005 | 2004-10-27 | ||
US64227105P | 2005-01-07 | 2005-01-07 | |
US60/642,271 | 2005-01-07 | ||
US11/149,731 US7476653B2 (en) | 2003-06-18 | 2005-06-10 | Macrocyclic modulators of the ghrelin receptor |
US11/149,731 | 2005-06-10 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2006009674A1 true WO2006009674A1 (en) | 2006-01-26 |
WO2006009674A8 WO2006009674A8 (en) | 2009-11-26 |
Family
ID=35427667
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US2005/020857 WO2006009674A1 (en) | 2004-06-18 | 2005-06-13 | Macrocyclic modulators of the ghrelin receptor |
Country Status (7)
Cited By (25)
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WO2006137974A2 (en) * | 2005-06-13 | 2006-12-28 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
WO2008033328A2 (en) | 2006-09-11 | 2008-03-20 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders |
WO2008130464A1 (en) * | 2007-02-09 | 2008-10-30 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor modulators and methods of using the same |
WO2010084050A2 (en) | 2009-01-13 | 2010-07-29 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
WO2011053821A1 (en) | 2009-10-30 | 2011-05-05 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
WO2011092293A2 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
WO2011092290A1 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists |
WO2011095450A1 (en) | 2010-02-02 | 2011-08-11 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
US20110237785A1 (en) * | 2003-07-31 | 2011-09-29 | Marsault Eric | Spatially-defined macrocyclic compounds useful for drug discovery |
EP2491004A2 (en) * | 2009-10-23 | 2012-08-29 | Tranzyme Pharma, Inc. | Macrocyclic inhibitors of serine protease enzymes |
JP2013040206A (ja) * | 2007-12-21 | 2013-02-28 | Helsinn Therapeutics (Us) Inc | 消化器系の運動をイパモレリンを用いて刺激する方法 |
US8921521B2 (en) | 2003-06-18 | 2014-12-30 | Ocera Therapeutics, Inc. | Macrocyclic modulators of the Ghrelin receptor |
US9096684B2 (en) | 2011-10-18 | 2015-08-04 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
US9845287B2 (en) | 2012-11-01 | 2017-12-19 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
US9957299B2 (en) | 2010-08-13 | 2018-05-01 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
US10030047B2 (en) | 2015-10-27 | 2018-07-24 | Hoffmann-La Roche Inc. | Peptide macrocycles against acinetobacter baumannii |
US10092621B2 (en) | 2014-11-12 | 2018-10-09 | Lyric Pharmaceuticals Inc. | Treatment of enteral feeding intolerance |
US10213477B2 (en) | 2012-02-15 | 2019-02-26 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
US10227380B2 (en) | 2012-02-15 | 2019-03-12 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
US10253067B2 (en) | 2015-03-20 | 2019-04-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
US10301351B2 (en) | 2007-03-28 | 2019-05-28 | President And Fellows Of Harvard College | Stitched polypeptides |
US10471120B2 (en) | 2014-09-24 | 2019-11-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
US11066443B2 (en) | 2017-04-10 | 2021-07-20 | Hoffmann-La Roche Inc. | 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 |
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7491695B2 (en) * | 2003-06-18 | 2009-02-17 | Tranzyme Pharma Inc. | Methods of using macrocyclic modulators of the ghrelin receptor |
US20090198050A1 (en) * | 2003-06-18 | 2009-08-06 | Tranzyme Pharma Inc. | Macrocyclic Modulators of the Ghrelin Receptor |
WO2004111077A1 (en) | 2003-06-18 | 2004-12-23 | Tranzyme Pharma Inc. | Macrocyclic antagonists of the motilin receptor |
US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
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 |
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 |
US20090275648A1 (en) * | 2005-06-13 | 2009-11-05 | Fraser Graeme L | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
CN101287464A (zh) * | 2005-09-29 | 2008-10-15 | 科学研究和应用咨询股份公司 | 用于刺激胃肠运动性的组合物和方法 |
CU23558A1 (es) | 2006-02-28 | 2010-07-20 | Ct Ingenieria Genetica Biotech | Compuestos análogos a los secretagogos peptidicos de la hormona de crecimiento |
EP2012809B1 (en) * | 2006-03-10 | 2013-05-22 | Ipsen Pharma | Use of a ghrelin agonist to improve the catabolic effects of glucocorticoid treatment |
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 |
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US20100216706A1 (en) * | 2007-05-15 | 2010-08-26 | Horvath Tamas L | Ghrelin Protects Substantia Nigra Dopamine Neurons |
US9724381B2 (en) | 2009-05-12 | 2017-08-08 | The Administrators Of The Tulane Educational Fund | Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof |
BR112012007183A2 (pt) * | 2009-09-30 | 2017-06-20 | Tranzyme Pharma Inc | solvato de um sal de um composto macrocíclico, forma polimórfica, processos para preparar a forma polimórfica e uma composição farmacêutica, composição farmacêutica, sal de um composto macrocíclico, e, métodos para estimular motilidade gastrintestinal, para tratar um distúrbio gastrintestinal e para tratar um indivíduo, e, kit |
CN102869775A (zh) | 2009-09-30 | 2013-01-09 | 哈佛大学校长及研究员协会 | 通过调节自噬抑制基因产物调节自噬的方法 |
WO2011146845A1 (en) * | 2010-05-21 | 2011-11-24 | Tranzyme Pharma, Inc. | Modified macrocyclic ghrelin receptor modulators and methods of using the same |
AU2011268256B8 (en) | 2010-06-16 | 2016-12-22 | Mcgill University | Growth hormone secretatogue receptor antagonists and uses thereof |
WO2012016186A1 (en) * | 2010-07-29 | 2012-02-02 | President And Fellows Of Harvard College | Macrocyclic kinase inhibitors and uses thereof |
AU2012279202A1 (en) | 2011-07-01 | 2014-02-20 | President And Fellows Of Harvard College | Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof |
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US10039813B2 (en) | 2012-02-07 | 2018-08-07 | Massachusetts Institute Of Technology | Use of antagonists of ghrelin or ghrelin receptor to prevent or treat stress-sensitive psychiatric illness |
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US10317418B2 (en) | 2015-02-24 | 2019-06-11 | Massachusetts Institute Of Technology | Use of ghrelin or functional ghrelin receptor agonists to prevent and treat stress-sensitive psychiatric illness |
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Also Published As
Publication number | Publication date |
---|---|
WO2006009674A8 (en) | 2009-11-26 |
EP2457893A1 (en) | 2012-05-30 |
US7476653B2 (en) | 2009-01-13 |
EP2457893B1 (en) | 2017-08-16 |
CN101111512A (zh) | 2008-01-23 |
US20090221689A1 (en) | 2009-09-03 |
US8334256B2 (en) | 2012-12-18 |
EP1773869B9 (en) | 2013-01-23 |
US20060025566A1 (en) | 2006-02-02 |
CA2579726A1 (en) | 2006-01-26 |
CA2579726C (en) | 2015-01-13 |
JP2008504238A (ja) | 2008-02-14 |
EP2457925A1 (en) | 2012-05-30 |
CN101111512B (zh) | 2013-05-01 |
EP1773869A1 (en) | 2007-04-18 |
ES2393498T3 (es) | 2012-12-21 |
JP5363726B2 (ja) | 2013-12-11 |
EP1773869B1 (en) | 2012-08-22 |
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