ES2393498T3 - Moduladores macrocíclicos del receptor de ghrelina - Google Patents
Moduladores macrocíclicos del receptor de ghrelina Download PDFInfo
- Publication number
- ES2393498T3 ES2393498T3 ES05785185T ES05785185T ES2393498T3 ES 2393498 T3 ES2393498 T3 ES 2393498T3 ES 05785185 T ES05785185 T ES 05785185T ES 05785185 T ES05785185 T ES 05785185T ES 2393498 T3 ES2393498 T3 ES 2393498T3
- Authority
- ES
- Spain
- Prior art keywords
- boc
- modulator
- bts
- phe
- use according
- 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.)
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Classifications
-
- 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
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 |
US872142 | 2004-06-18 | ||
US62164204P | 2004-10-26 | 2004-10-26 | |
US621642P | 2004-10-26 | ||
US62200504P | 2004-10-27 | 2004-10-27 | |
US622005P | 2004-10-27 | ||
US64227105P | 2005-01-07 | 2005-01-07 | |
US642271P | 2005-01-07 | ||
US149731 | 2005-06-10 | ||
US11/149,731 US7476653B2 (en) | 2003-06-18 | 2005-06-10 | Macrocyclic modulators of the ghrelin receptor |
PCT/US2005/020857 WO2006009674A1 (en) | 2004-06-18 | 2005-06-13 | Macrocyclic modulators of the ghrelin receptor |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2393498T3 true ES2393498T3 (es) | 2012-12-21 |
Family
ID=35427667
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES05785185T Active ES2393498T3 (es) | 2004-06-18 | 2005-06-13 | Moduladores macrocíclicos del receptor de ghrelina |
Country Status (7)
Families Citing this family (59)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8921521B2 (en) | 2003-06-18 | 2014-12-30 | Ocera Therapeutics, Inc. | Macrocyclic modulators of the Ghrelin receptor |
US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
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 |
US7491695B2 (en) * | 2003-06-18 | 2009-02-17 | Tranzyme Pharma Inc. | Methods of using macrocyclic modulators of the ghrelin receptor |
SI1648922T1 (sl) * | 2003-07-31 | 2011-03-31 | Tranzyme Pharma Inc | Prostorsko opredeljene makrocikliäśne spojine uporabne za odkrivanje zdravil |
WO2005012332A1 (en) * | 2003-07-31 | 2005-02-10 | Tranzyme Pharma | 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 |
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 |
SI1937262T1 (sl) * | 2005-09-29 | 2019-09-30 | Ipsen Pharma | Spojina za uporabo pri zdravljenju gastrointestinalne dismotilitete |
CU23558A1 (es) | 2006-02-28 | 2010-07-20 | Ct Ingenieria Genetica Biotech | Compuestos análogos a los secretagogos peptidicos de la hormona de crecimiento |
US20100227806A1 (en) | 2006-03-10 | 2010-09-09 | Tulipano Giovanni | Use Of A Ghrelin Agonist To Improve 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 |
EP2054429B1 (en) | 2006-09-11 | 2013-11-06 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders |
CA2939778C (en) | 2007-01-31 | 2019-01-29 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 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 |
EP2142562B1 (en) | 2007-03-28 | 2013-07-03 | President and Fellows of Harvard College | Stitched polypeptides |
US20100216706A1 (en) * | 2007-05-15 | 2010-08-26 | Horvath Tamas L | Ghrelin Protects Substantia Nigra Dopamine Neurons |
CN101951937A (zh) * | 2007-12-21 | 2011-01-19 | 赫尔辛医疗股份公司 | 使用伊帕瑞林刺激胃肠系统动力的方法 |
US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
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 |
MX2012003912A (es) * | 2009-09-30 | 2012-08-17 | Tranzyme Pharma Inc | Sales, solvatos y composiciones farmaceuticas de los agonistas macrociclicos del receptor de ghrelina y metodos para su uso. |
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 |
US20120270807A1 (en) * | 2009-10-23 | 2012-10-25 | Marsault Eric | Macrocyclic inhibitors of serine protease enzymes |
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 |
AR080056A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de ciclohexil-amida como antagonistas de los receptores de crf |
CN102762572A (zh) | 2010-02-01 | 2012-10-31 | 诺瓦提斯公司 | 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物 |
WO2011095450A1 (en) | 2010-02-02 | 2011-08-11 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
WO2011146845A1 (en) * | 2010-05-21 | 2011-11-24 | Tranzyme Pharma, Inc. | Modified macrocyclic ghrelin receptor modulators and methods of using the same |
CA2805406A1 (en) * | 2010-06-16 | 2011-12-22 | 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 |
EP2603600B1 (en) | 2010-08-13 | 2018-11-21 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
EP2726467A4 (en) | 2011-07-01 | 2015-01-21 | Harvard College | MACROCYCLIC INHIBITORS OF INSULIN DEGRADATION ENZYME (IDE) AND USES THEREOF |
KR20140100937A (ko) | 2011-10-18 | 2014-08-18 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
CN102557989B (zh) * | 2011-12-19 | 2013-12-25 | 深圳翰宇药业股份有限公司 | 优利莫瑞林中间体以及优利莫瑞林制备方法 |
WO2013119800A1 (en) | 2012-02-07 | 2013-08-15 | Massachusetts Institute Of Technology | Use of antagonists of ghrelin or ghrelin receptor to prevent or treat stress-sensitive psychiatric illness |
WO2013123266A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
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 |
TWI667024B (zh) * | 2012-09-27 | 2019-08-01 | 美商雅瑞塔那醫療公司 | 使用食慾喪失控制化合物之組合物及方法 |
KR102499918B1 (ko) | 2012-10-24 | 2023-02-14 | 다이이찌 산쿄 가부시키가이샤 | 근위축성 측삭 경화증 치료제 |
US9604919B2 (en) | 2012-11-01 | 2017-03-28 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
US9724396B2 (en) | 2013-03-15 | 2017-08-08 | Massachusetts Institute Of Technology | Use of antagonists of growth hormone or growth hormone receptor to prevent or treat stress-sensitive psychiatric illness |
US9119832B2 (en) | 2014-02-05 | 2015-09-01 | The Regents Of The University Of California | Methods of treating mild brain injury |
CN103864588B (zh) * | 2014-03-25 | 2015-09-09 | 河北工业大学 | 一种2,3-二甲氧基苯甲醛的制备方法 |
BR112017005598A2 (pt) | 2014-09-24 | 2017-12-12 | Aileron Therapeutics Inc | macrociclos peptidomiméticos e usos dos mesmos |
US10092621B2 (en) | 2014-11-12 | 2018-10-09 | Lyric Pharmaceuticals Inc. | Treatment of enteral feeding intolerance |
PT3250203T (pt) | 2015-01-28 | 2021-11-30 | Elanco Animal Health Incorporated | Composição para utilização crónica como composto para ganho de peso |
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 |
EP3294318A4 (en) | 2015-03-20 | 2019-04-03 | Aileron Therapeutics, Inc. | PEPTIDOMIMETIC MACROCYCLES AND USES THEREOF |
WO2016172631A2 (en) | 2015-04-24 | 2016-10-27 | President And Fellows Of Harvard College | Substrate selective inhibitors of insulin-degrading enzyme (ide) and uses thereof |
RU2729609C2 (ru) | 2015-10-27 | 2020-08-11 | Ф. Хоффманн-Ля Рош Аг | Пептидные макроциклы против acinetobacter baumannii |
US20170121385A1 (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 |
CN107759660A (zh) * | 2017-12-05 | 2018-03-06 | 陕西慧康生物科技有限责任公司 | 一种三肽‑29的液‑固相合成方法 |
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-
2005
- 2005-06-10 US US11/149,731 patent/US7476653B2/en not_active Ceased
- 2005-06-13 CA CA2579726A patent/CA2579726C/en not_active Expired - Fee Related
- 2005-06-13 WO PCT/US2005/020857 patent/WO2006009674A1/en active Application Filing
- 2005-06-13 ES ES05785185T patent/ES2393498T3/es active Active
- 2005-06-13 EP EP11009050.3A patent/EP2457893B1/en active Active
- 2005-06-13 EP EP05785185A patent/EP1773869B9/en not_active Not-in-force
- 2005-06-13 EP EP11009051A patent/EP2457925A1/en not_active Withdrawn
- 2005-06-13 CN CN2005800280726A patent/CN101111512B/zh not_active Expired - Fee Related
- 2005-06-13 JP JP2007516620A patent/JP5363726B2/ja not_active Expired - Fee Related
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2009
- 2009-01-09 US US12/351,395 patent/US8334256B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
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CN101111512B (zh) | 2013-05-01 |
US20060025566A1 (en) | 2006-02-02 |
US20090221689A1 (en) | 2009-09-03 |
CA2579726A1 (en) | 2006-01-26 |
WO2006009674A8 (en) | 2009-11-26 |
EP1773869B9 (en) | 2013-01-23 |
EP2457893A1 (en) | 2012-05-30 |
EP1773869A1 (en) | 2007-04-18 |
EP1773869B1 (en) | 2012-08-22 |
CN101111512A (zh) | 2008-01-23 |
EP2457925A1 (en) | 2012-05-30 |
JP2008504238A (ja) | 2008-02-14 |
EP2457893B1 (en) | 2017-08-16 |
WO2006009674A1 (en) | 2006-01-26 |
CA2579726C (en) | 2015-01-13 |
US8334256B2 (en) | 2012-12-18 |
US7476653B2 (en) | 2009-01-13 |
JP5363726B2 (ja) | 2013-12-11 |
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