CA2579726C - Macrocyclic modulators of the ghrelin receptor - Google Patents

Macrocyclic modulators of the ghrelin receptor Download PDF

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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
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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
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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
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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

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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
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-C00195.png)
EP (3) EP1773869B9 (US20090221689A1-20090903-C00195.png)
JP (1) JP5363726B2 (US20090221689A1-20090903-C00195.png)
CN (1) CN101111512B (US20090221689A1-20090903-C00195.png)
CA (1) CA2579726C (US20090221689A1-20090903-C00195.png)
ES (1) ES2393498T3 (US20090221689A1-20090903-C00195.png)
WO (1) WO2006009674A1 (US20090221689A1-20090903-C00195.png)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090198050A1 (en) * 2003-06-18 2009-08-06 Tranzyme Pharma Inc. Macrocyclic Modulators of the Ghrelin Receptor
ATE457995T1 (de) * 2003-06-18 2010-03-15 Tranzyme Pharma Inc Makrozyklische motilin rezeptorantagonisten
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
US8921521B2 (en) 2003-06-18 2014-12-30 Ocera Therapeutics, Inc. Macrocyclic modulators of the Ghrelin receptor
CA2533820C (en) * 2003-07-31 2016-12-13 Tranzyme Pharma Spatially-defined macrocycles incorporating peptide bond surrogates
EP2319859B1 (en) * 2003-07-31 2013-03-27 Tranzyme Pharma Inc. Spatially-defined macrocyclic compounds useful for drug discovery
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
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
US20090275648A1 (en) * 2005-06-13 2009-11-05 Fraser Graeme L Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same
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
ES2740108T3 (es) 2005-09-29 2020-02-05 Ipsen Pharma Composición para uso en el tratamiento de dismotilidad gastrointestinal
CU23558A1 (es) 2006-02-28 2010-07-20 Ct Ingenieria Genetica Biotech Compuestos análogos a los secretagogos peptidicos de la hormona de crecimiento
WO2007106385A2 (en) * 2006-03-10 2007-09-20 Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. 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
EP2431380A3 (en) 2006-09-11 2013-07-03 Tranzyme Pharma, Inc. Macrocyclic antagonist 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
US8592377B2 (en) 2007-03-28 2013-11-26 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
AU2008341160A1 (en) * 2007-12-21 2009-07-02 Helsinn Therapeutics (U.S.), 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
IN2012DN03297A (US20090221689A1-20090903-C00195.png) * 2009-09-30 2015-10-23 Tranzyme Pharma Inc
BR112012007160A2 (pt) 2009-09-30 2018-03-13 Harvard College metodos para modulacao da autofagia por meio da modulacao d eprodutos genicos inibidores da autofagia
WO2011050276A1 (en) * 2009-10-23 2011-04-28 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
US20120295942A1 (en) 2010-02-01 2012-11-22 Nicholas James Devereux Pyrazolo[5,1b]oxazole Derivatives as CRF-1 Receptor Antagonists
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
CN102753527B (zh) 2010-02-02 2014-12-24 诺华股份有限公司 用作crf受体拮抗剂的环己基酰胺衍生物
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
SI2603600T1 (sl) 2010-08-13 2019-04-30 Aileron Therapeutics, Inc. Peptidomimetični makrocikli
US9243038B2 (en) 2011-07-01 2016-01-26 President And Fellows Of Harvard College Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof
BR112014009418A2 (pt) 2011-10-18 2017-04-18 Aileron Therapeutics Inc macrociclos peptidomiméticos
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
CA2862038C (en) 2012-02-15 2021-05-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US8987414B2 (en) 2012-02-15 2015-03-24 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
TW202106298A (zh) 2012-09-27 2021-02-16 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
JP6262661B2 (ja) 2012-10-24 2018-01-17 第一三共株式会社 筋萎縮性側索硬化症治療剤
KR20150082307A (ko) 2012-11-01 2015-07-15 에일러론 테라퓨틱스 인코포레이티드 이치환 아미노산 및 이의 제조 및 사용 방법
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
CN106999541A (zh) 2014-09-24 2017-08-01 艾瑞朗医疗公司 拟肽大环化合物及其用途
MX2017006205A (es) 2014-11-12 2017-11-17 Lyric Pharmaceuticals Inc Tratamiento de la intoleracia a la alimentacion enteral.
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
SG11201707750YA (en) 2015-03-20 2017-10-30 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
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
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
WO2019168654A2 (en) 2018-02-09 2019-09-06 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
AU637316B2 (en) 1988-01-28 1993-05-27 Eastman Kodak Company Polypeptide compounds having growth hormone releasing activity
JPH03502326A (ja) 1988-01-28 1991-05-30 ポリゲン　ホールディング　コーポレイション 成長ホルモン放出活性を有するポリペプチド化合物類
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
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
US5726319A (en) 1992-11-06 1998-03-10 Merck & Co., Inc. Biphenyl substituted dipeptide analogs promote release of growth hormone
RU2168512C2 (ru) 1992-12-11 2001-06-10 Мерк Энд Ко., Инк. Спиропиперидины, способы их получения (варианты)
US5578593A (en) 1992-12-11 1996-11-26 Merck & Co., Inc. Spiro piperidines and homologs promote release of growth hormone
KR960705575A (ko) 1993-10-19 1996-11-08 도나 엘. 폴락 비스포스포네이트와 성장 호르몬 분비촉진제와의 배합물(Combination of bishosphonates and growth hormone secretagogues)
CA2175218A1 (en) 1993-11-09 1995-05-18 Gregori J. Morriello Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
US5494919A (en) 1993-11-09 1996-02-27 Merck & Co., Inc. 2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
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
CA2176140A1 (en) 1993-11-24 1995-06-01 Meng Hsin Chen Indolyl group containing compounds and the use thereof to promote the release of growth hormone(s)
US5721251A (en) 1993-12-10 1998-02-24 Merck & Co., Inc. Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
PL181286B1 (pl) 1993-12-23 2001-07-31 Novo Nordisk As Zwiazki o wlasciwosciach uwalniania hormonu wzrostu i zawierajace je kompozycje farmaceutyczne PL PL PL PL PL PL PL PL
HU224345B1 (hu) 1993-12-23 2005-08-29 Novo Nordisk A/S. Növekedési hormont felszabadító tulajdonságú peptidek, ezeket hatóanyagként tartalmazó gyógyszerkészítmények és alkalmazásuk
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
US5777112A (en) 1994-06-13 1998-07-07 Merck & Co., Inc Piperazine compounds promote release of growth hormone
WO1996002530A1 (en) 1994-07-20 1996-02-01 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
WO1996022996A1 (fr) 1995-01-25 1996-08-01 Nippon Chemiphar Co., Ltd. Derives de dihydrophenazine
HUP9702388A3 (en) 1995-01-27 1999-01-28 Novo Nordisk As Compounds with growth hormone releasing properties and pharmaceuticals contg. them
AU4534596A (en) 1995-02-09 1996-08-27 Novo Nordisk A/S Compounds with growth hormone releasing properties
WO1996024587A1 (en) 1995-02-09 1996-08-15 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
WO1996035713A1 (en) 1995-05-08 1996-11-14 Pfizer, Inc. Dipeptides which promote release of growth hormone
ATE288444T1 (de) 1995-05-29 2005-02-15 Pfizer Dipeptide, die die ausschüttung von wachstumshormonen stimulieren
HUP9802821A3 (en) 1995-06-22 2000-03-28 Novo Nordisk As Compounds with growth hormone releasing properties
AU6772996A (en) 1995-08-21 1997-03-12 Eli Lilly And Company 2-acylaminopropanamides as growth hormone secretagogues
AU6724496A (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
WO1997011697A1 (en) 1995-09-26 1997-04-03 Merck & Co., Inc. 3-spirolactam, 3-spiroamino, 3-spirolactone and 3-spirobenzopyran piperidines and pyrrolidines promote release of growth hormone
JPH11513984A (ja) 1995-10-27 1999-11-30 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剤の製造方法
US5767124A (en) 1995-10-27 1998-06-16 Merck & Co., Inc. Polymorphic forms of a growth hormone secretagogue
EA199800337A1 (ru) 1995-10-27 1998-10-29 Мерк Энд Ко., Инк. Способ получения гормона роста, усиливающего секрецию
CA2234817A1 (en) 1995-10-27 1997-05-01 Mandana Asgharnejad Wet granulation formulation of a growth hormone secretagogue
CA2240186A1 (en) 1995-12-13 1997-06-19 Merck & Co., Inc. Assays for growth hormone secretagogue receptors
WO1997021730A1 (en) 1995-12-13 1997-06-19 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
ES2323159T3 (es) 1995-12-22 2009-07-07 Novo Nordisk A/S Compuestos con propiedades de liberacion de la hormona del crecimiento.
TW432073B (en) 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
AU2334097A (en) 1996-03-21 1997-10-10 Merck & Co., Inc. 4-spiroindoline piperidines promote release of growth hormone
WO1997036873A1 (en) 1996-04-03 1997-10-09 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
AU2382097A (en) 1996-04-19 1997-11-12 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
CZ291982B6 (cs) 1996-04-24 2003-06-18 Novo Nordisk A/S Diamidový derivát uvolňující růstový hormon, jeho použití, farmaceutické prostředky ho obsahující a způsob stimulace uvolňování růstového hormonu
AU2931997A (en) 1996-05-07 1997-11-26 Merck & Co., Inc. Treatment of mood disorders with a growth hormone secretagogue
CA2253390A1 (en) 1996-05-07 1997-11-13 Merck & Co., Inc. Enhancement of sleep with a growth hormone secretagogue
WO1997043278A1 (en) 1996-05-14 1997-11-20 Novo Nordisk A/S Somatostatin agonists and antagonists
WO1997044042A1 (en) 1996-05-22 1997-11-27 Arch Development Corporation Sleep quality improvement using a growth hormone secretagogue
JP2000512274A (ja) 1996-05-31 2000-09-19 ノボ ノルディスク アクティ―ゼルスカブ 骨粗しょう症の周期的（整合性）治療における成長ホルモン成分及び骨抗吸収剤
EP0923539B1 (en) 1996-07-22 2002-06-05 Novo Nordisk A/S Compounds with growth hormone releasing properties
WO1998010653A1 (en) 1996-09-13 1998-03-19 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
AU6747498A (en) 1997-04-11 1998-11-11 Sumitomo Pharmaceuticals Company, Limited Benzene derivatives
JP2000514838A (ja) 1997-05-14 2000-11-07 藤沢薬品工業株式会社 成長ホルモンの放出を促進するピペリジノ誘導体
EP1005484A1 (en) 1997-06-20 2000-06-07 Novo Nordisk A/S Compounds with growth hormone releasing properties
JP3514774B2 (ja) 1997-06-25 2004-03-31 ファイザー・インク 成長ホルモン分泌促進薬としてのジペプチド誘導体
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)
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)
ZA987383B (en) 1997-08-19 2000-02-17 Lilly Co Eli Treatment of congestive heart failure with growth hormone secretagogues.
WO1999009991A1 (en) 1997-08-22 1999-03-04 Kaken Pharmaceutical Co., Ltd. Novel amide derivatives
CA2303395C (en) 1997-09-08 2008-12-02 Metabolic Pharmaceuticals Ltd Treatment of obesity
EP1047709B1 (en) 1998-01-16 2004-11-03 Novo Nordisk A/S Compounds with growth hormone releasing properties
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
ZA991572B (en) 1998-03-03 1999-09-03 Novo Nordisk As New salt forms of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoy L)-2-(2-naphthyl)ethyl)amide.
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
WO1999064456A1 (en) 1998-06-09 1999-12-16 Novo Nordisk A/S A method for preparing a compound with growth hormone releasing properties
ZA993975B (en) * 1998-06-16 2000-12-15 Pfizer Prod Inc Combination therapy for musculoskeletal frailty.
HUP0102395A2 (hu) 1998-06-16 2001-11-28 Pfizer Products Inc. Izom- és csontrendszeri gyengeség kezelésére alkalmas szelektív ösztrogén receptor modulátorok és növekedési hormon szekretagógok (GHS) kombinációját tartalmazó gyógyszerkészítmények
BRPI9911756B1 (pt) 1998-06-30 2016-06-14 Helsinn Healthcare Sa composto, uso do mesmo, e composição farmaceutica
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
WO2000009538A2 (en) 1998-08-10 2000-02-24 Merck & Co., Inc. Canine growth hormone secretagogue receptor
DE69923692T2 (de) 1998-08-20 2006-03-23 Sumitomo Pharmaceuticals Co., Ltd. Wachstumshormon-freisetzende oxindolderivate
US6358951B1 (en) 1998-08-21 2002-03-19 Pfizer Inc. Growth hormone secretagogues
CN1261158C (zh) * 1998-09-03 2006-06-28 诺兰兹公司 生长激素在制备用于诱导神经保护作用的药剂中的应用
AU5911000A (en) 1999-06-30 2001-01-31 Zymogenetics Inc. Sgip peptides
CA2284459C (en) 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
US6849597B2 (en) 1999-12-28 2005-02-01 Kaken Pharmaceutical Co., Ltd. Neuroprotective drug
CN1432022A (zh) * 2000-04-19 2003-07-23 先灵公司 含有烷基和芳基丙氨酸p2部分的丙型肝炎病毒的大环ns3－丝氨酸蛋白酶抑制剂
JP2004514651A (ja) 2000-05-30 2004-05-20 メルク　エンド　カムパニー　インコーポレーテッド グレリン類似体
ATE446758T1 (de) * 2000-05-31 2009-11-15 Pfizer Prod Inc Verwendung von wachstumshormonsekretagoga zur förderung der beweglichkeit des verdauungstrakts
ES2250416T3 (es) 2000-06-13 2006-04-16 Zentaris Gmbh Estimulante de secreciohn de hormona de crecimiento.
AU2001274601A1 (en) 2000-06-23 2002-01-02 Kaken Pharmaceutical Co., Ltd. Preventives or remedies for heart failure
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
WO2002064746A2 (en) 2001-02-14 2002-08-22 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
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
ATE457995T1 (de) * 2003-06-18 2010-03-15 Tranzyme Pharma Inc Makrozyklische motilin rezeptorantagonisten
US7491695B2 (en) 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
CA2533820C (en) 2003-07-31 2016-12-13 Tranzyme Pharma Spatially-defined macrocycles incorporating peptide bond surrogates
EP2319859B1 (en) 2003-07-31 2013-03-27 Tranzyme Pharma Inc. Spatially-defined macrocyclic compounds useful for drug discovery
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
IN2012DN03297A (US20090221689A1-20090903-C00195.png) 2009-09-30 2015-10-23 Tranzyme Pharma Inc

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