CA2579726C - Macrocyclic modulators of the ghrelin receptor - Google Patents

Macrocyclic modulators of the ghrelin receptor Download PDF

Info

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
Application number
CA2579726A
Other languages
English (en)
French (fr)
Other versions
CA2579726A1 (en
Inventor
Hamid Hoveyda
Mark Peterson
Graeme Fraser
Mahesh Ramaseshan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ocera Therapeutics Inc
Original Assignee
Ocera Therapeutics Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from US10/872,142 external-priority patent/US7521420B2/en
Application filed by Ocera Therapeutics Inc filed Critical Ocera Therapeutics Inc
Publication of CA2579726A1 publication Critical patent/CA2579726A1/en
Application granted granted Critical
Publication of CA2579726C publication Critical patent/CA2579726C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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
CA2579726A 2004-06-18 2005-06-13 Macrocyclic modulators of the ghrelin receptor Expired - Fee Related CA2579726C (en)

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)

Country Link
US (2) US7476653B2 (US20090221689A1-20090903-C00293.png)
EP (3) EP2457925A1 (US20090221689A1-20090903-C00293.png)
JP (1) JP5363726B2 (US20090221689A1-20090903-C00293.png)
CN (1) CN101111512B (US20090221689A1-20090903-C00293.png)
CA (1) CA2579726C (US20090221689A1-20090903-C00293.png)
ES (1) ES2393498T3 (US20090221689A1-20090903-C00293.png)
WO (1) WO2006009674A1 (US20090221689A1-20090903-C00293.png)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
DE602004018782D1 (de) * 2003-07-31 2009-02-12 Tranzyme Pharma Inc Räumlich definierte makrocyclen, die peptidbindungssurrogate enthalten
US7452862B2 (en) * 2003-07-31 2008-11-18 Tranzyme Pharma, Inc. Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists
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
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
PL1937262T3 (pl) 2005-09-29 2019-10-31 Ipsen Pharma Kompozycja do stosowania w leczeniu zaburzeń motoryki przewodu pokarmowego
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
CA2662897C (en) 2006-09-11 2017-11-07 Tranzyme Pharma, Inc. Macrocyclic antagonists 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
EP2644618B1 (en) * 2007-02-09 2016-08-17 Ocera Therapeutics, Inc. tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators
KR20160061439A (ko) 2007-03-28 2016-05-31 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
WO2008143835A1 (en) * 2007-05-15 2008-11-27 Yale University Ghrelin protects substantia nigra dopamine neurons
EP2234630A4 (en) * 2007-12-21 2012-08-08 Helsinn Therapeutics Us Inc METHOD OF STIMULATING THE MOTILITY OF THE GASTROINTESTINAL SYSTEM USING IPAMORELIN
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
KR20120081166A (ko) * 2009-09-30 2012-07-18 트랜자임 파르마 인크 매크로시클릭 그렐린 수용체 효능제의 염, 용매화물 및 약제학적 조성물 및 이를 사용하는 방법
EP2483406A2 (en) 2009-09-30 2012-08-08 President and Fellows of Harvard College Methods for modulation of autophagy through the modulation of autophagy-inhibiting gene products
EP2491020A4 (en) * 2009-10-23 2013-04-24 Tranzyme Pharma Inc METHODS OF USING MACROCYCLIC INHIBITORS OF SERINE PROTEASE ENZYMES
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
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー ＣＲＦ−１受容体アンタゴニストとしてのピラゾロ［５，１ｂ］オキサゾール誘導体
EP2531490B1 (en) 2010-02-02 2014-10-15 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
CN108570097A (zh) 2010-08-13 2018-09-25 爱勒让治疗公司 拟肽大环化合物
AU2012279202A1 (en) 2011-07-01 2014-02-20 President And Fellows Of Harvard College Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof
AU2012326026B2 (en) 2011-10-18 2017-04-13 Aileron Therapeutics, Inc. Peptidomimetic macrocyles
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
NZ627528A (en) 2012-02-15 2016-05-27 Aileron Therapeutics Inc Peptidomimetic macrocycles
US8987414B2 (en) 2012-02-15 2015-03-24 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
KR20220003640A (ko) * 2012-09-27 2022-01-10 아라타나 세라퓨틱스, 인크. 식욕부진을 조절 화합물 조성물 및 이의 이용 방법
KR20200108494A (ko) 2012-10-24 2020-09-18 다이이찌 산쿄 가부시키가이샤 근위축성 측삭 경화증 치료제
WO2014071241A1 (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
CA2961258A1 (en) 2014-09-24 2016-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
SG11201703884PA (en) 2014-11-12 2017-06-29 Lyric Pharmaceuticals Inc Treatment of enteral feeding intolerance
PL3250203T3 (pl) 2015-01-28 2022-04-25 Elanco Animal Health Incorporated Kompozycja do przewlekłego stosowania jako środek wspomagający przybieranie na wadze
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
JP2018516844A (ja) 2015-03-20 2018-06-28 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
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
CN108350028B (zh) 2015-10-27 2021-12-07 豪夫迈·罗氏有限公司 对抗鲍曼不动杆菌(Acinetobacter baumannii)的肽大环
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
US11674136B2 (en) 2018-02-09 2023-06-13 President And Fellows Of Harvard College DNA-templated macrocycle library
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

Family Cites Families (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3239345A (en) 1965-02-15 1966-03-08 Estrogenic compounds and animal growth promoters
US4411890A (en) 1981-04-14 1983-10-25 Beckman Instruments, Inc. Synthetic peptides having pituitary growth hormone releasing activity
US4036979A (en) 1974-01-25 1977-07-19 American Cyanamid Company Compositions containing 4,5,6,7-tetrahydrobenz[b]thien-4-yl-ureas or derivatives and methods of enhancing growth rate
NZ188418A (en) 1977-10-03 1981-02-11 Mobil Oil Corp Lubricants containing oil and an oxazoline
DE68919213T2 (de) 1988-01-28 1995-05-11 Polygen Holding Corp Polypeptidverbindungen mit wachstumshormonfreisetzender aktivität.
WO1989007110A1 (en) 1988-01-28 1989-08-10 Eastman Kodak Company Polypeptide compounds having growth hormone releasing activity
CA2092718C (en) 1990-10-25 2007-08-07 Grace H. W. Wong Use of protective agents against reactive oxygen species
US5663146A (en) 1991-08-22 1997-09-02 Administrators Of The Tulane Educational Fund Polypeptide analogues having growth hormone releasing activity
US5726319A (en) 1992-11-06 1998-03-10 Merck & Co., Inc. Biphenyl substituted dipeptide analogs promote release of growth hormone
JPH08503213A (ja) 1992-11-06 1996-04-09 メルク エンド カンパニー インコーポレーテッド 成長ホルモンの放出を促進する置換ジペプチド同族体
HUT72076A (en) 1992-12-11 1996-03-28 Merck & Co Inc Process for preparing spiro piperidines and homologs which promote release of growth hormone and pharmaceutical compositions containing them
US5536716A (en) 1992-12-11 1996-07-16 Merck & Co., Inc. Spiro piperidines and homologs which promote release of growth hormone
CZ109196A3 (en) 1993-10-19 1996-10-16 Merck & Co Inc Combination of active compounds and a pharmaceutical preparation for treating and preventing osteoporosis
US5494919A (en) 1993-11-09 1996-02-27 Merck & Co., Inc. 2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
CN1174504A (zh) 1993-11-09 1998-02-25 麦克公司 促进生长激素释放的哌啶、吡咯烷和六氢－1h－吖庚因
US5492916A (en) 1993-12-23 1996-02-20 Merck & Co., Inc. Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
JPH09505601A (ja) 1993-11-24 1997-06-03 メルク エンド カンパニー インコーポレーテッド インドリル基含有化合物類および成長ホルモン放出を促進するためのそれらの使用
US5721251A (en) 1993-12-10 1998-02-24 Merck & Co., Inc. Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
JP3181918B2 (ja) 1993-12-23 2001-07-03 ノボ ノルディスク アクティーゼルスカブ 成長ホルモン放出特性を持つ化合物
WO1995017422A1 (en) 1993-12-23 1995-06-29 Novo Nordisk A/S Compounds with growth hormone releasing properties
US5721250A (en) 1993-12-23 1998-02-24 Merck & Co. Inc. Di-and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
WO1995034311A1 (en) 1994-06-13 1995-12-21 Merck & Co., Inc. Piperazine compounds promote release of growth hormone
US5783582A (en) 1994-07-20 1998-07-21 Merck & Co., Inc. Piperidines and hexahydro-1H-azepines spiro substituted at the 4-position promote release of growth hormone
US5798337A (en) 1994-11-16 1998-08-25 Genentech, Inc. Low molecular weight peptidomimetic growth hormone secretagogues
AU4495996A (en) 1995-01-25 1996-08-14 Nippon Chemiphar Co. Ltd. Dihydrophenazine derivatives
WO1996022997A1 (en) 1995-01-27 1996-08-01 Novo Nordisk A/S Compounds with growth hormone releasing properties
WO1996024580A1 (en) 1995-02-09 1996-08-15 Novo Nordisk A/S Compounds with growth hormone releasing properties
AU4534696A (en) 1995-02-09 1996-08-27 Novo Nordisk A/S Compounds with growth hormone releasing properties
US5559128A (en) 1995-04-18 1996-09-24 Merck & Co., Inc. 3-substituted piperidines promote release of growth hormone
EP0823904A4 (en) 1995-04-19 1998-09-09 Merck & Co Inc METHOD FOR PRODUCING SPIROINDOLINES
WO1996038471A1 (en) 1995-05-29 1996-12-05 Pfizer Inc. Dipeptides which promote release of growth hormone
WO1996035713A1 (en) 1995-05-08 1996-11-14 Pfizer, Inc. Dipeptides which promote release of growth hormone
IL122371A0 (en) 1995-06-22 1998-06-15 Novo Nordisk As Compounds with growth hormone releasing properties
WO1997006803A1 (en) 1995-08-21 1997-02-27 Eli Lilly And Company 2-acylaminopropanamides as growth hormone secretagogues
EP0761219A1 (en) 1995-08-21 1997-03-12 Eli Lilly And Company 2-Acylaminopropanamines as growth hormone secretagogues
EP0766966A3 (en) 1995-09-08 2001-02-28 Eli Lilly And Company Method of treating insulin resistance
AU7169696A (en) 1995-09-26 1997-04-17 Merck & Co., Inc. 3-spirolactam, 3-spiroamino, 3-spirolactone and 3-spirobenzopyran piperidines and pyrrolidines promote release of growth hormone
CZ128298A3 (cs) 1995-10-27 1998-07-15 Merck And Co., Inc. Způsob výroby N-/1(R)-/(1,2-dihydro-1-methansulfonylspiro/3H-indol-3,4´-piperdin/-1´-yl)karbonyl/-2-(fenylmethyloxy)-ethyl/-2-amino-2-methylpropanamidu
WO1997015191A1 (en) 1995-10-27 1997-05-01 Merck & Co., Inc. Wet granulation formulation of a growth hormone secretagogue
US5767124A (en) 1995-10-27 1998-06-16 Merck & Co., Inc. Polymorphic forms of a growth hormone secretagogue
US5723616A (en) 1995-10-27 1998-03-03 Merck & Co., Inc. Process for the preparation of a growth hormone secretagogue
WO1997022004A1 (en) 1995-12-13 1997-06-19 Merck & Co., Inc. Assays for growth hormone secretagogue receptors
CA2240427C (en) 1995-12-13 2007-08-14 Merck & Co., Inc. Growth hormone secretagogue receptor family
IT1277113B1 (it) 1995-12-20 1997-11-04 Romano Deghenghi Composti oligopeptidici contenenti d-2-alchiltriptofano in grado di promuovere la liberazione dell'ormone della crescita
WO1997022367A1 (en) 1995-12-20 1997-06-26 Merck & Co., Inc. Radiolabeled growth hormone secretagogue
BR9612275A (pt) 1995-12-22 1999-07-13 Novo Nordisk As Composto composição farmacêutica processo para estimular a liberação do hormônio do crescimento pela pituitária e aumentar a taxa e a extensão do crescimento da produção do leite e lã ou para tratar doenças e uso de um composto
TW432073B (en) 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
WO1997034604A1 (en) 1996-03-21 1997-09-25 Merck & Co., Inc. 4-spiroindoline piperidines promote release of growth hormone
AU2722297A (en) 1996-04-03 1997-10-22 Merck & Co., Inc. Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
SE9601397D0 (sv) 1996-04-12 1996-04-12 Pharmacia Ab Use of growth hormone
WO1997040071A1 (en) 1996-04-19 1997-10-30 Novo Nordisk A/S Compounds with growth hormone releasing properties
US5919777A (en) 1996-04-24 1999-07-06 Novo Nordisk A/S Compounds with growth hormone releasing properties
PL329413A1 (en) 1996-04-24 1999-03-29 Novo Nordisk As Chemical compounds exhibiting properties capable to cause growth hormone release
WO1997041878A1 (en) 1996-05-07 1997-11-13 Merck & Co., Inc. Treatment of mood disorders with a growth hormone secretagogue
JP2000511885A (ja) 1996-05-07 2000-09-12 メルク エンド カンパニー インコーポレーテッド 成長ホルモン分泌促進薬による睡眠の強化
JP2001525793A (ja) 1996-05-14 2001-12-11 ノボ ノルディスク アクティーゼルスカブ ソマトスタチンの作動因子及び拮抗因子
US6071926A (en) 1996-05-22 2000-06-06 Arch Development Corporation Sleep quality improvement using a growth hormone secretagogue
KR20000016204A (ko) 1996-05-31 2000-03-25 한센 핀 베네드, 안네 제헤르 골다공증의 주기적(연계) 치료에 있어 성장호르몬 성분 및 뼈의항흡수 약물
JP4425992B2 (ja) 1996-07-22 2010-03-03 サファイア セラピューティクス，インコーポレイティド 成長ホルモン放出特性を有する化合物
AU4342097A (en) 1996-09-13 1998-04-02 Merck & Co., Inc. Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
WO1998018815A1 (en) 1996-10-25 1998-05-07 Merck & Co., Inc. Convergent process for the preparation of a growth hormone secretagogue
SE9703929D0 (sv) 1996-11-22 1997-10-28 Pharmacia & Upjohn Ab Therapeutical use and method
WO1998046569A1 (fr) 1997-04-11 1998-10-22 Sumitomo Pharmaceuticals Co., Ltd. Derives de benzene
WO1998051687A1 (en) 1997-05-14 1998-11-19 Fujisawa Pharmaceutical Co., Ltd. Piperidino derivatives which promote growth hormone release
EP1005484A1 (en) 1997-06-20 2000-06-07 Novo Nordisk A/S Compounds with growth hormone releasing properties
UA64751C2 (uk) 1997-06-25 2004-03-15 Пфайзер Продактс Інк. Спосіб лікування інсулінової толерантності речовинами, які посилюють секрецію гормону росту (варіанти) та фармацевтична композиція (варіанти)
UA53716C2 (uk) 1997-06-25 2003-02-17 Пфайзер Продактс Інк. Тартратна сіль заміщеного дипептиду, спосіб її одержання, проміжні сполуки та спосіб їх одержання, фармацевтична композиція (варіанти), спосіб підвищення рівнів ендогенного гормону росту та спосіб лікування або профілактики захворювань (варіанти)
ES2283055T3 (es) 1997-06-25 2007-10-16 Pfizer Inc. Derivados dipeptidos como secretagogos de la hormona de crecimiento.
ZA987383B (en) 1997-08-19 2000-02-17 Lilly Co Eli Treatment of congestive heart failure with growth hormone secretagogues.
US6864250B1 (en) 1997-08-22 2005-03-08 Kaken Pharmaceutical Co., Ltd. N-acylated lipophilic amino acid derivatives
EP1012189B1 (en) 1997-09-08 2007-10-31 Metabolic Pharmaceuticals Ltd. Treatment of obesity
JP4382279B2 (ja) 1998-01-16 2009-12-09 サファイア セラピューティクス，インコーポレイティド 成長ホルモン放出特性を有する化合物
WO1999039730A1 (fr) 1998-02-09 1999-08-12 Kaken Pharmaceutical Co., Ltd. Preparation a administration orale contenant des peptides favorisant la secretion d'hormone de croissance
DE69912930D1 (de) 1998-03-03 2003-12-24 Novo Nordisk As Neue salzformn von (2e)-5-amino-5-methylhex-2-enolsäure n-methyl-n-((1r)-1-(methylcarbamoyl)-2-phruylrthyl) carbamoyl)-2-(2-naphtyl)ethyl)amid
MA26618A1 (fr) * 1998-04-09 2004-12-20 Smithkline Beecham Corp Composes et compositions pharmaceutiques pour le traitement du paludisme
CA2329881C (en) 1998-05-11 2010-03-16 Novo Nordisk A/S Compounds with growth hormone releasing properties
EP1093463A1 (en) 1998-06-09 2001-04-25 Novo Nordisk A/S A method for preparing a compound with growth hormone releasing properties
PE20000646A1 (es) 1998-06-16 2000-08-05 Pfizer Prod Inc Terapia de combinacion para la fragilidad musculoesqueletica
ID26726A (id) 1998-06-16 2001-02-01 Pfizer Prod Inc Kombinasi terapeutik untuk kelemahan muskuloskeletal
CA2334315C (en) 1998-06-30 2011-07-26 Novo Nordisk A/S Compounds with growth hormone releasing properties
DE19831217A1 (de) * 1998-07-03 2000-01-05 Schering Ag Neue Porphyrinderivate, diese enthaltende pharmazeutische Mittel und ihre Verwendung in der photodynamischen Therapie und MRI-Diagnostik
US6645726B1 (en) 1998-08-10 2003-11-11 Merck & Co., Inc. Canine growth hormone secretagogue receptor
KR100680085B1 (ko) 1998-08-20 2007-02-28 다이닛본 스미토모 세이야꾸 가부시끼가이샤 성장호르몬 방출촉진제로서 옥신돌 유도체
US6358951B1 (en) 1998-08-21 2002-03-19 Pfizer Inc. Growth hormone secretagogues
CA2343214A1 (en) * 1998-09-03 2000-03-16 Chris Edward Williams Neuroprotection
JP2003503055A (ja) 1999-06-30 2003-01-28 ザイモジェネティクス，インコーポレイティド Ｓｇｉｐペプチド
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
AU2405401A (en) 1999-12-28 2001-07-09 Kaken Pharmaceutical Co., Ltd. Nerve protective drugs
AR030558A1 (es) * 2000-04-19 2003-08-27 Schering Corp COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,
CA2411667A1 (en) 2000-05-30 2001-12-06 Merck & Co. Inc. Ghrelin analogs
DE60140285D1 (de) * 2000-05-31 2009-12-10 Pfizer Prod Inc Verwendung von Wachstumshormonsekretagoga zur Förderung der Beweglichkeit des Verdauungstrakts
PT1524272E (pt) 2000-06-13 2007-07-25 Aeterna Zentaris Gmbh Secretagogos de hormona de crescimento
EP1297839A4 (en) 2000-06-23 2005-12-07 Kaken Pharma Co Ltd THERAPEUTIC AND PROPHYLACTIC AGENTS FOR CARDIAC INSUFFICIENCY
US6576686B1 (en) 2000-06-27 2003-06-10 Exxonmobil Chemical Patents Inc. Road marking compound comprising linear tetrablock copolymers
US6635784B2 (en) * 2000-09-29 2003-10-21 Eastman Chemical Company Process for the preparation of enantiomerically-enriched cyclopropylalanine derivates
AU2002250081A1 (en) 2001-02-14 2002-08-28 Uab Research Foundation Combined transductional and transcriptional targeting system for improved gene delivery
ITMI20011445A1 (it) 2001-07-06 2003-01-06 Europ Geie Analoghi della cortistantina capaci di legarsi selettivamente ai recettori dei secretagoghi dell'ormone della crescita
AU2003254902A1 (en) 2002-08-09 2004-02-25 Kaken Pharmaceutical Co., Ltd. Myocardial cell protecting agents
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
US7476653B2 (en) * 2003-06-18 2009-01-13 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
US7452862B2 (en) * 2003-07-31 2008-11-18 Tranzyme Pharma, Inc. Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists
DE602004018782D1 (de) 2003-07-31 2009-02-12 Tranzyme Pharma Inc Räumlich definierte makrocyclen, die peptidbindungssurrogate enthalten
EP2644618B1 (en) * 2007-02-09 2016-08-17 Ocera Therapeutics, Inc. tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators
KR20120081166A (ko) * 2009-09-30 2012-07-18 트랜자임 파르마 인크 매크로시클릭 그렐린 수용체 효능제의 염, 용매화물 및 약제학적 조성물 및 이를 사용하는 방법

Also Published As

Publication number Publication date
ES2393498T3 (es) 2012-12-21
EP2457893A1 (en) 2012-05-30
EP1773869B1 (en) 2012-08-22
CN101111512B (zh) 2013-05-01
EP2457893B1 (en) 2017-08-16
CA2579726A1 (en) 2006-01-26
US20090221689A1 (en) 2009-09-03
WO2006009674A1 (en) 2006-01-26
US7476653B2 (en) 2009-01-13
EP1773869A1 (en) 2007-04-18
US8334256B2 (en) 2012-12-18
JP2008504238A (ja) 2008-02-14
CN101111512A (zh) 2008-01-23
WO2006009674A8 (en) 2009-11-26
US20060025566A1 (en) 2006-02-02
EP2457925A1 (en) 2012-05-30
JP5363726B2 (ja) 2013-12-11
EP1773869B9 (en) 2013-01-23

Similar Documents

Publication Publication Date Title
CA2579726C (en) Macrocyclic modulators of the ghrelin receptor
US8349887B2 (en) Methods of treating cachexia with macrocyclic modulators of the ghrelin receptor
USRE42013E1 (en) Macrocyclic modulators of the ghrelin receptor
USRE42624E1 (en) Methods of using macrocyclic modulators of the ghrelin receptor
CA2677399C (en) Macrocyclic ghrelin receptor modulators and methods of using the same
US20090198050A1 (en) Macrocyclic Modulators of the Ghrelin Receptor
US20180110824A1 (en) Macrocyclic Modulators of the Ghrelin Receptor
US9493505B2 (en) Macrocyclic modulators of the ghrelin receptor
ES2646887T3 (es) Compuestos intermedios para moduladores macrocíclicos del receptor de ghrelina
JP5730835B2 (ja) 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) グレリン受容体の大環状モジュレーターの使用方法
AU2015201862B2 (en) Macrocyclic ghrelin receptor modulators and methods of using the same

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed

Effective date: 20220301

MKLA Lapsed

Effective date: 20200831