CA2579726C - Macrocyclic modulators of the ghrelin receptor - Google Patents
Macrocyclic modulators of the ghrelin receptor Download PDFInfo
- Publication number
- CA2579726C CA2579726C CA2579726A CA2579726A CA2579726C CA 2579726 C CA2579726 C CA 2579726C CA 2579726 A CA2579726 A CA 2579726A CA 2579726 A CA2579726 A CA 2579726A CA 2579726 C CA2579726 C CA 2579726C
- Authority
- CA
- Canada
- Prior art keywords
- boc
- modulator
- none
- bts
- phe
- 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
- 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 |
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 | |
US60/622,005 | 2004-10-27 | ||
US64227105P | 2005-01-07 | 2005-01-07 | |
US60/642,271 | 2005-01-07 | ||
US11/149,731 | 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 (2)
Publication Number | Publication Date |
---|---|
CA2579726A1 CA2579726A1 (en) | 2006-01-26 |
CA2579726C true CA2579726C (en) | 2015-01-13 |
Family
ID=35427667
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2579726A Expired - Fee Related CA2579726C (en) | 2004-06-18 | 2005-06-13 | Macrocyclic modulators of the ghrelin receptor |
Country Status (7)
Families Citing this family (59)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | 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 |
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 |
WO2005012332A1 (en) * | 2003-07-31 | 2005-02-10 | Tranzyme Pharma | Spatially-defined macrocycles incorporating peptide bond surrogates |
DK1648922T3 (da) * | 2003-07-31 | 2011-03-14 | Tranzyme Pharma Inc | Rumligt definerede makrocykliske forbindelser, der er anvendelige til opdagelse af lægemidler |
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 |
JP5122446B2 (ja) * | 2005-06-13 | 2013-01-16 | 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 |
US20090275648A1 (en) * | 2005-06-13 | 2009-11-05 | Fraser Graeme L | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
RU2566708C2 (ru) * | 2005-09-29 | 2015-10-27 | Ипсен Фарма С.А.С. | Композиции и способы стимуляции двигательной функции желудочно-кишечного тракта |
CU23558A1 (es) | 2006-02-28 | 2010-07-20 | Ct Ingenieria Genetica Biotech | Compuestos análogos a los secretagogos peptidicos de la hormona de crecimiento |
ES2424970T3 (es) | 2006-03-10 | 2013-10-10 | Ipsen Pharma | Uso de un agonista de la grelina para mejorar los efectos catabólicos del tratamiento con glucocorticoides |
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 |
CN101528765B (zh) | 2006-09-11 | 2015-04-22 | 欧塞拉治疗有限公司 | 用于治疗胃肠动力障碍病症的促胃动素受体的大环拮抗剂 |
CA2677045C (en) | 2007-01-31 | 2016-10-18 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
CA2677399C (en) | 2007-02-09 | 2016-09-13 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor modulators and methods of using the same |
KR101623985B1 (ko) | 2007-03-28 | 2016-05-25 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 스티칭된 폴리펩티드 |
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 |
JP2013506687A (ja) | 2009-09-30 | 2013-02-28 | プレジデント アンド フェロウズ オブ ハーバード カレッジ | オートファジー促進遺伝子産物の変調によりオートファジーを変調する方法 |
CA2775925A1 (en) * | 2009-09-30 | 2011-04-07 | Tranzyme Pharma, Inc. | Salts, solvates and pharmaceutical compositions of macrocyclic ghrelin receptor agonists and methods of using the same |
WO2011050270A2 (en) * | 2009-10-23 | 2011-04-28 | Tranzyme Pharma, Inc. | Macrocyclic inhibitors of serine protease enzymes |
CA2778990A1 (en) | 2009-10-30 | 2011-05-05 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
EP2531510B1 (en) | 2010-02-01 | 2014-07-23 | Novartis AG | Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists |
WO2011092293A2 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
ES2527849T3 (es) | 2010-02-02 | 2015-01-30 | Novartis Ag | Derivados de ciclohexilamida como antagonistas del receptor de CRF |
WO2011146845A1 (en) * | 2010-05-21 | 2011-11-24 | Tranzyme Pharma, Inc. | Modified macrocyclic ghrelin receptor modulators and methods of using the same |
US9315546B2 (en) | 2010-06-16 | 2016-04-19 | The Administrators Of The Tulane Educational Fund | Growth hormone secretatogue receptor antagonists and uses thereof |
US8975232B2 (en) | 2010-07-29 | 2015-03-10 | President And Fellows Of Harvard College | Macrocyclic kinase inhibitors and uses thereof |
CA2807685C (en) | 2010-08-13 | 2020-10-06 | Aileron Therapeutics, Inc. | P53 derived peptidomimetic macrocycle |
CN105873910A (zh) | 2011-07-01 | 2016-08-17 | 哈佛大学的校长及成员们 | 大环胰岛素降解酶(ide)抑制剂及其用途 |
JP6342808B2 (ja) | 2011-10-18 | 2018-06-13 | エイルロン セラピューティクス,インコーポレイテッド | ペプチドミメティック大環状化合物 |
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 |
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 |
AU2013221433B2 (en) | 2012-02-15 | 2018-01-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
CN107216380A (zh) | 2012-02-15 | 2017-09-29 | 爱勒让治疗公司 | 拟肽大环化合物 |
RU2648958C2 (ru) | 2012-09-27 | 2018-03-28 | Аратана Терапьютикс, Инк. | Композиции и способы применения соединения для борьбы с отсутствием аппетита |
CN110354265A (zh) | 2012-10-24 | 2019-10-22 | 第一三共株式会社 | 用于肌萎缩性侧索硬化的治疗剂 |
CA2887285A1 (en) | 2012-11-01 | 2014-05-08 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
WO2014144231A1 (en) | 2013-03-15 | 2014-09-18 | 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 |
CN112245565A (zh) | 2014-09-24 | 2021-01-22 | 艾瑞朗医疗公司 | 拟肽大环化合物及其用途 |
KR20170085539A (ko) | 2014-11-12 | 2017-07-24 | 리릭 파마슈티컬스 인크. | 경장 섭식 불내성의 치료 |
RU2680410C1 (ru) | 2015-01-28 | 2019-02-21 | Аратана Терапьютикс, Инк. | Композиции и способы длительного применения соединения для прироста массы тела |
WO2016138099A1 (en) | 2015-02-24 | 2016-09-01 | Massachusetts Institute Of Technology | Use of ghrelin or functional ghrelin receptor agonists to prevent and treat stress-sensitive psychiatric illness |
MX2017011834A (es) | 2015-03-20 | 2018-04-11 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y usos de los mismos. |
US11040976B2 (en) | 2015-04-24 | 2021-06-22 | President And Fellows Of Harvard College | Substrate selective inhibitors of insulin-degrading enzyme (IDE) and uses thereof |
KR20180063138A (ko) | 2015-10-27 | 2018-06-11 | 에프. 호프만-라 로슈 아게 | 아시네토박터 바우만니이에 대항하는 펩티드 거대고리 |
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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 ES ES05785185T patent/ES2393498T3/es active Active
- 2005-06-13 EP EP05785185A patent/EP1773869B9/en not_active Not-in-force
- 2005-06-13 WO PCT/US2005/020857 patent/WO2006009674A1/en active Application Filing
- 2005-06-13 CN CN2005800280726A patent/CN101111512B/zh not_active Expired - Fee Related
- 2005-06-13 EP EP11009051A patent/EP2457925A1/en not_active Withdrawn
- 2005-06-13 CA CA2579726A patent/CA2579726C/en not_active Expired - Fee Related
- 2005-06-13 EP EP11009050.3A patent/EP2457893B1/en active Active
- 2005-06-13 JP JP2007516620A patent/JP5363726B2/ja not_active Expired - Fee Related
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2009
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Also Published As
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US20060025566A1 (en) | 2006-02-02 |
EP2457925A1 (en) | 2012-05-30 |
WO2006009674A1 (en) | 2006-01-26 |
JP2008504238A (ja) | 2008-02-14 |
CA2579726A1 (en) | 2006-01-26 |
WO2006009674A8 (en) | 2009-11-26 |
US20090221689A1 (en) | 2009-09-03 |
US8334256B2 (en) | 2012-12-18 |
CN101111512A (zh) | 2008-01-23 |
EP1773869B9 (en) | 2013-01-23 |
EP2457893A1 (en) | 2012-05-30 |
US7476653B2 (en) | 2009-01-13 |
ES2393498T3 (es) | 2012-12-21 |
EP2457893B1 (en) | 2017-08-16 |
JP5363726B2 (ja) | 2013-12-11 |
CN101111512B (zh) | 2013-05-01 |
EP1773869A1 (en) | 2007-04-18 |
EP1773869B1 (en) | 2012-08-22 |
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