ES2602789T3 - Productos intermedios conectores para la síntesis de moduladores macrocíclicos del receptor de la grelina - Google Patents

Productos intermedios conectores para la síntesis de moduladores macrocíclicos del receptor de la grelina Download PDF

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Publication number
ES2602789T3
ES2602789T3 ES12195556.1T ES12195556T ES2602789T3 ES 2602789 T3 ES2602789 T3 ES 2602789T3 ES 12195556 T ES12195556 T ES 12195556T ES 2602789 T3 ES2602789 T3 ES 2602789T3
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boc
bts
compound
nmeala
ghrelin
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Spanish (es)
Inventor
Hamid Hoveyda
Graeme Fraser
Sophie Beauchemin
Martin Brassard
David Drutz
Eric Marsault
Luc Quellet
Mark L Peterson
Zhigang Wang
Kamel Benkali
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Ocera Therapeutics Inc
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Ocera Therapeutics Inc
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ES12195556.1T 2007-02-09 2008-02-08 Productos intermedios conectores para la síntesis de moduladores macrocíclicos del receptor de la grelina Active ES2602789T3 (es)

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US (3) US9371297B2 (cg-RX-API-DMAC7.html)
EP (2) EP2644618B1 (cg-RX-API-DMAC7.html)
JP (2) JP2010518090A (cg-RX-API-DMAC7.html)
KR (1) KR20090107088A (cg-RX-API-DMAC7.html)
CN (1) CN101657436A (cg-RX-API-DMAC7.html)
AU (1) AU2008241532A1 (cg-RX-API-DMAC7.html)
BR (1) BRPI0807046A2 (cg-RX-API-DMAC7.html)
CA (1) CA2677399C (cg-RX-API-DMAC7.html)
EA (1) EA200901077A1 (cg-RX-API-DMAC7.html)
ES (2) ES2602789T3 (cg-RX-API-DMAC7.html)
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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
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
US20090198050A1 (en) * 2003-06-18 2009-08-06 Tranzyme Pharma Inc. Macrocyclic Modulators of the Ghrelin Receptor
US8921521B2 (en) 2003-06-18 2014-12-30 Ocera Therapeutics, Inc. Macrocyclic modulators of the Ghrelin receptor
CA2528375C (en) 2003-06-18 2013-11-19 Tranzyme Pharma, Inc. Macrocyclic antagonists of the motilin receptor
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
CA2677045C (en) 2007-01-31 2016-10-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
MX2009008561A (es) * 2007-02-13 2010-01-15 Helsinn Therapeutics Us Inc Metodo para tratar trastornos proliferativos celulares utilizando secretagogos.
CA2682174C (en) 2007-03-28 2021-04-06 President And Fellows Of Harvard College Stitched polypeptides
TWI429436B (zh) * 2007-04-10 2014-03-11 Helsinn Therapeutics Us Inc 使用生長激素促泌素治療或預防嘔吐之方法
US20080287371A1 (en) * 2007-05-17 2008-11-20 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor for modulation of the migrating motor complex
EP2259791A2 (en) * 2008-03-05 2010-12-15 Tel HaShomer Medical Research Infrastructure and Services Ltd. Glp-1 receptor agonists and related active pharmaceutical ingredients for treatment of cancer
WO2010102253A2 (en) * 2009-03-06 2010-09-10 Angstrom Pharmaceuticals, Inc. Compositions and methods for modulation of cell migration
HUE047515T2 (hu) * 2009-09-09 2020-04-28 Novaremed Ltd N-Szubsztituált benzolpropánamidok fájdalom és gyulladás kezelésében történõ alkalmazásra
BR112012007137A2 (pt) 2009-09-30 2015-09-15 Harvard College metodos para modulacao da autofagia por meio da modulacao de produtos genicos inibidores da autofagia
US20120270807A1 (en) * 2009-10-23 2012-10-25 Marsault Eric Macrocyclic inhibitors of serine protease enzymes
US20110105389A1 (en) 2009-10-30 2011-05-05 Hoveyda Hamid R Macrocyclic Ghrelin Receptor Antagonists and Inverse Agonists and Methods of Using the Same
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
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
US8835444B2 (en) 2010-02-02 2014-09-16 Novartis Ag Cyclohexyl amide derivatives as CRF receptor antagonists
CA2795698A1 (en) * 2010-03-05 2011-09-09 Angstrom Pharmaceuticals, Inc. Modulation of intracellular signaling
WO2011140176A1 (en) * 2010-05-04 2011-11-10 Glaxosmithkline Llc Methods for treating or preventing cardiovascular disorders and providing cardiovascular protection
CN103347517B (zh) 2010-08-11 2018-10-02 德雷克塞尔大学 治疗帕金森病中运动障碍的d3多巴胺受体激动剂
WO2012021875A1 (en) 2010-08-13 2012-02-16 Aileron Therapeutics, Inc. Peptidomimetic macrocycles with triazole linkers
AR086554A1 (es) 2011-05-27 2014-01-08 Novartis Ag Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina
CN108929375A (zh) 2011-10-18 2018-12-04 爱勒让治疗公司 拟肽大环化合物
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
CN112500466B (zh) 2012-02-15 2022-05-03 艾瑞朗医疗公司 拟肽大环化合物
CA2864120A1 (en) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
CA2867043A1 (en) 2012-05-03 2013-11-07 Novartis Ag L-malate salt of 2,7-diaza-spiro[4.5]dec-7-yle derivatives and crystalline forms thereof as ghrelin receptor agonists
CN104470524A (zh) * 2012-05-25 2015-03-25 拉夸里亚创药株式会社 用于治疗胃酸缺乏症的生长激素释放肽受体激动剂
CN104812384B (zh) 2012-11-01 2020-09-18 爱勒让治疗公司 二取代的氨基酸及其制备和使用方法
EP3197478A4 (en) 2014-09-24 2018-05-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
WO2016123233A1 (en) * 2015-01-28 2016-08-04 Aratana Therapeutics, Inc. Compositions and methods for chronic use of a weight-gaining compound
SG11201707750YA (en) 2015-03-20 2017-10-30 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
TW202045001A (zh) 2019-02-01 2020-12-16 美商富曼西公司 作為除草劑的經取代吡啶類及嘧啶類化合物
KR20210126022A (ko) * 2019-02-08 2021-10-19 스코프라 시앙스 쌍테 에 휴마이네스 에스.에.쎄. 뉴로텐시너직 작용제 및 통증을 치료 또는 예방하는 이의 사용 방법
CN109879935B (zh) * 2019-03-04 2020-11-20 南京工业大学 一种多肽的液相合成方法
WO2022006470A1 (en) 2020-07-01 2022-01-06 Vanderbilt University Methods of treatment for a kidney disease
CN113616654B (zh) * 2021-06-18 2022-08-12 广州市妇女儿童医疗中心 Gsk872在制备治疗肠道病毒71型感染导致的疾病的药物中的用途
CN115960080B (zh) * 2021-10-13 2024-03-15 南京知和医药科技有限公司 一种多环化合物及其作为胃饥饿素受体激动剂的用途

Family Cites Families (152)

* 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
DE2540552A1 (de) 1974-09-12 1976-03-25 American Cyanamid Co Cycloalkylderivate von 1-aryloxy-3- amino-2-propanolen
NZ188418A (en) 1977-10-03 1981-02-11 Mobil Oil Corp Lubricants containing oil and an oxazoline
JPS56142272A (en) 1980-04-09 1981-11-06 Teikoku Hormone Mfg Co Ltd Hydrazinopyridazine derivative
IL85472A (en) * 1987-03-09 1991-06-30 Procter & Gamble Pharmaceutical compositions for treating gastrointestinal disorders
ATE122357T1 (de) 1988-01-28 1995-05-15 Polygen Holding Corp Polypeptide mit hormonwachstumsbefreiender wirkung.
ATE113607T1 (de) 1988-01-28 1994-11-15 Polygen Holding Corp Polypeptidverbindungen mit wachstumshormonfreisetzender aktivität.
US5158978A (en) * 1990-02-05 1992-10-27 British Technology Group (U.S.A.) Thyroid hormone treatment of acute cardiovascular compromise
ATE133073T1 (de) 1990-10-25 1996-02-15 Genentech Inc Verwendung gegen reaktive sauerstoffverbindungen schützender wirkstoffe
US6294346B1 (en) * 1991-07-08 2001-09-25 Neurospheres Holdings, Ltd. Use of multipotent neural stem cells and their progeny for the screening of drugs and other biological agents
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
AU676525B2 (en) 1992-11-06 1997-03-13 Merck & Co., Inc. Substituted dipeptide analogs promote release of growth hormone
US5578593A (en) 1992-12-11 1996-11-26 Merck & Co., Inc. Spiro piperidines and homologs promote release of growth hormone
WO1994013696A1 (en) 1992-12-11 1994-06-23 Merck & Co., Inc. Spiro piperidines and homologs which promote release of growth hormone
BR9407869A (pt) 1993-10-19 1996-10-29 Merck & Co Inc Combinaçao composiçao farmacêutica e processo para o tratamento de osteoporose
CA2175218A1 (en) 1993-11-09 1995-05-18 Gregori J. Morriello 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
US5494919A (en) 1993-11-09 1996-02-27 Merck & Co., Inc. 2-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
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
CZ291382B6 (cs) 1993-12-23 2003-02-12 Novo Nordisk A/S Peptidické deriváty ovlivňující uvolňování růstového hormonu, farmaceutický přípravek je obsahující a jejich použití
PL181280B1 (pl) 1993-12-23 2001-07-31 Novo Nordisk As oraz zawierajaca je kompozycja farmaceutyczna PL PL PL PL PL PL PL PL
US5777112A (en) 1994-06-13 1998-07-07 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
AR003108A1 (es) 1995-01-27 1998-07-08 Novo Nordisk As Compuestos con propiedades de liberacion de la hormona del crecimiento, composicion farmaceutica que los contienen, el uso de los mismos para la preparación de un medicamento.
AU4534696A (en) 1995-02-09 1996-08-27 Novo Nordisk A/S Compounds with growth hormone releasing properties
AU4534596A (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
WO1996033189A1 (en) 1995-04-19 1996-10-24 Merck & Co., Inc. Process for the preparation of spiroindolines
WO1996035713A1 (en) 1995-05-08 1996-11-14 Pfizer, Inc. Dipeptides which promote release of growth hormone
EP0828754B1 (en) 1995-05-29 2005-02-02 Pfizer Inc. Dipeptides which promote release of growth hormone
CA2224434A1 (en) 1995-06-22 1997-01-09 Novo Nordisk A/S Compounds with growth hormone releasing properties
WO1997006803A1 (en) 1995-08-21 1997-02-27 Eli Lilly And Company 2-acylaminopropanamides as growth hormone secretagogues
WO1997007117A1 (en) 1995-08-21 1997-02-27 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
EA199800337A1 (ru) 1995-10-27 1998-10-29 Мерк Энд Ко., Инк. Способ получения гормона роста, усиливающего секрецию
US5767124A (en) 1995-10-27 1998-06-16 Merck & Co., Inc. Polymorphic forms of a growth hormone secretagogue
KR19990067097A (ko) 1995-10-27 1999-08-16 폴락 돈나 엘. 성장 호르몬 분비 촉진제의 제조 방법
AU7522896A (en) 1995-10-27 1997-05-15 Merck & Co., Inc. Wet granulation formulation of a growth hormone secretagogue
DE69636394T2 (de) 1995-12-13 2007-07-19 Merck & Co., Inc. Testverfahren für die sekretionsrezeptoren von wachstumshormonen
DE69633637T2 (de) 1995-12-13 2006-03-09 Merck & Co., Inc. Wachstumshormonsekretionsförderer rezeptorfamilie
WO1997022367A1 (en) 1995-12-20 1997-06-26 Merck & Co., Inc. Radiolabeled growth hormone secretagogue
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
EP0869974B1 (en) 1995-12-22 2009-03-04 Novo Nordisk A/S Compounds with growth hormone releasing properties
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
CA2252761A1 (en) 1996-04-24 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
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
AU2764797A (en) 1996-05-14 1997-12-05 Novo Nordisk A/S Somatostatin agonists and antagonists
US6071926A (en) 1996-05-22 2000-06-06 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
ATE304528T1 (de) 1996-07-22 2005-09-15 Novo Nordisk As Verbindungen mit wachstumshormon-freisetzenden eigenschaften
WO1998010653A1 (en) 1996-09-13 1998-03-19 Merck & Co., Inc. Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
AU4993497A (en) 1996-10-25 1998-05-22 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
GB2324726A (en) 1997-05-01 1998-11-04 Merck & Co Inc Combination Therapy for the Treatment of Osteoporosis
GB9709082D0 (en) * 1997-05-06 1997-06-25 Ciba Geigy Ag Organic compositions
WO1998051687A1 (en) 1997-05-14 1998-11-19 Fujisawa Pharmaceutical Co., Ltd. Piperidino derivatives which promote growth hormone release
AU7906998A (en) 1997-06-20 1999-01-04 Novo Nordisk A/S Compounds with growth hormone releasing properties
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)
AU7445498A (en) 1997-06-25 1999-01-04 Pfizer Inc. Dipeptide derivatives as growth hormone secretagogues
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.
ZA987385B (en) 1997-08-19 2000-04-18 Lilly Co Eli Growth hormone secretagogues.
CA2301566A1 (en) 1997-08-22 1999-03-04 Kaken Pharmaceutical Co., Ltd. N-acylated lipophilic amino acid derivatives
ATE377026T1 (de) 1997-09-08 2007-11-15 Metabolic Pharm Ltd Behandlung von fettleibigkeit
AU766305B2 (en) 1998-01-16 2003-10-16 Novo Nordisk A/S Compounds with growth hormone releasing properties
WO1999039730A1 (en) 1998-02-09 1999-08-12 Kaken Pharmaceutical Co., Ltd. Oral preparations containing peptides promoting the secretion of growth hormone
IL137353A0 (en) 1998-03-03 2001-07-24 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) carbamoyl)-2-(2-naphthyl)ethyl)amid
US6657063B1 (en) 1998-04-30 2003-12-02 Pfizer Inc. Combinations of β3 agonists and growth hormone secretagogues
SI1077941T1 (sl) 1998-05-11 2010-01-29 Novo Nordisk As Spojine, ki imajo lastnost sproščanja rastnega hormona
JP4574849B2 (ja) 1998-06-09 2010-11-04 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を調製するための方法
EA200001189A1 (ru) 1998-06-16 2001-06-25 Пфайзер Продактс Инк. Терапевтические комбинации (избирательных) модуляторов рецепторов эстрогенов (имрэ) и стимуляторов секреции гормона роста (ссгр) для лечения скелетно-мышечной слабости
AP9901582A0 (en) 1998-06-16 1999-06-30 Pfizer Prod Inc Combination therapy for musculoskeletal frailty.
US6919315B1 (en) 1998-06-30 2005-07-19 Novo Nordisk A/S Compounds with growth hormone releasing properties
PL199853B1 (pl) 1998-06-30 2008-11-28 Novo Nordisk As Związek o właściwościach uwalniania hormonu wzrostu, kompozycja zawierająca ten związek oraz jego zastosowanie do stymulowania uwalniania hormonu wzrostu
CA2340095A1 (en) 1998-08-10 2000-02-24 Merck & Co., Inc. Canine growth hormone secretagogue receptor
US6639076B1 (en) 1998-08-18 2003-10-28 Eli Lilly And Company Growth hormone secretagogues
CA2340701C (en) 1998-08-20 2009-05-26 Sumitomo Pharmaceuticals Co., Ltd. Oxindole derivatives as growth hormone releasers
US6358951B1 (en) 1998-08-21 2002-03-19 Pfizer Inc. Growth hormone secretagogues
JP2002542151A (ja) 1999-02-18 2002-12-10 科研製薬株式会社 成長ホルモン分泌促進物質としての新規なアミド誘導体
US6828331B1 (en) 1999-02-19 2004-12-07 Eli Lilly And Company Growth hormone secretagogues
US6353005B1 (en) 1999-03-02 2002-03-05 Sepracor, Inc. Method and compositions using (+) norcisapride in combination with proton pump inhibitors or H2 receptor antagonist
US6362202B1 (en) 1999-03-02 2002-03-26 Sepracor Inc. Methods and compositions using (−) norcisapride in combination with proton pump inhibitors or H2 receptor antagonists
US6194382B1 (en) * 1999-03-03 2001-02-27 Albert Einstein College Of Medicine Of Yeshiva University Method and composition for treating irritable bowel syndrome using low doses of opioid receptor antagonists
US6518292B1 (en) 1999-03-12 2003-02-11 Bristol-Myers Squibb Co. Heterocyclic aromatic compounds usefuls as growth hormone secretagogues
EP1190059A1 (en) 1999-06-30 2002-03-27 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
US20040092511A1 (en) 1999-12-10 2004-05-13 Billstein Stephan Anthony Pharmaceutical combinations and their use in treating gastrointestinal and abdominal viscera disorders
TWI263496B (en) 1999-12-10 2006-10-11 Novartis Ag Pharmaceutical combinations and their use in treating gastrointestinal disorders
CA2395996A1 (en) 1999-12-28 2001-07-05 Kaken Pharmaceutical Co., Ltd. Neuroprotective drug
EP1149583A3 (en) 2000-04-13 2001-11-14 Pfizer Products Inc. Combinations of corticotropin releasing factor antagonists and growth hormone secretagogues
DOP2001000154A (es) 2000-05-25 2002-05-15 Pfizer Prod Inc Combinación de secretagogos de hormona del crecimiento y antidepresivos
CA2411667A1 (en) 2000-05-30 2001-12-06 Merck & Co. Inc. Ghrelin analogs
ES2333097T3 (es) 2000-05-31 2010-02-17 Raqualia Pharma Inc Uso de secretagogos de la hormona de crecimiento para estimular la motilidad gastrointestinal.
PL216676B1 (pl) 2000-06-13 2014-05-30 Aeterna Zentaris Gmbh Związki pobudzające wydzielanie hormonu wzrostu, kompozycja farmaceutyczna zawierająca takie związki oraz ich zastosowanie
CA2413252A1 (en) 2000-06-23 2002-12-20 Takahiko Murata 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
KR20020010206A (ko) * 2000-07-27 2002-02-04 이시우 인터루킨 12와 보조활성인자 ｂ7.1 유전자를 함유하는ｄｎａ 벡터 및 이벡터가 도입된 항암 세포백신
WO2002064746A2 (en) 2001-02-14 2002-08-22 Uab Research Foundation Combined transductional and transcriptional targeting system for improved gene delivery
PT1379224E (pt) * 2001-03-29 2009-10-22 Synergy Pharmaceuticals Inc Agonistas do receptor da guanilato ciclase para o tratamento de inflamação de tecidos e carcinogénese
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
WO2003088914A2 (en) * 2002-04-18 2003-10-30 The University Of Iowa Research Foundation Methods of inhibiting and treating bacterial biofilms by metal chelators
JPWO2004014412A1 (ja) 2002-08-09 2005-12-02 科研製薬株式会社 心筋細胞保護剤
MY139563A (en) 2002-09-04 2009-10-30 Bristol Myers Squibb Co Heterocyclic aromatic compounds useful as growth hormone secretagogues
US7635709B2 (en) 2002-09-26 2009-12-22 The United States Of America As Represented By The Department Of Veterans Affairs Compositions and methods for bowel care in individuals with chronic intestinal pseudo-obstruction
WO2004084943A1 (en) 2003-03-19 2004-10-07 Beth Israel Deaconess Medical Center, Inc Use of antagonists of ghrelin or ghrelin receptor to treat intestinal inflammation
GB0307863D0 (en) 2003-04-04 2003-05-14 Merck Sharp & Dohme Therapeutic treatment
RS20050868A (sr) 2003-05-27 2007-08-03 Altana Pharma Ag., Farmaceutske kombinacije inhibotora protonske pumpe i jedinjenje koje modifikuje gastrointestinalni motilitet
GB0313772D0 (en) 2003-06-13 2003-07-23 Merck Sharp & Dohme Therapeutic treatment
CA2528375C (en) 2003-06-18 2013-11-19 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
US7491695B2 (en) 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
NL1024009C2 (nl) 2003-07-28 2005-02-07 Vmi Epe Holland Loopvlakapplicatieinrichting.
PL1648922T3 (pl) * 2003-07-31 2011-05-31 Tranzyme Pharma Inc Przestrzennie określone związki makrocykliczne użyteczne w dziedzinie odkrywania leków
EP1648923B1 (en) * 2003-07-31 2008-12-31 Tranzyme Pharma Inc. Spatially-defined macrocycles incorporating peptide bond surrogates
WO2005039625A1 (en) 2003-10-28 2005-05-06 Rheoscience A/S Growth hormone secretagogue receptor agonists
CN1901908A (zh) 2003-11-04 2007-01-24 伊利舍医药品公司 治疗性化合物及其用途
GB0329275D0 (en) 2003-12-18 2004-01-21 Merck Sharp & Dohme Therapeutic treatment
RS20050796A (sr) 2004-01-06 2007-08-03 Panacea Biotec Ltd., Farmaceutske smeše koje sadrže inhibitor protonske pumpe i prokinetičko sredstvo
TW200530181A (en) 2004-01-13 2005-09-16 Bristol Myers Squibb Co Heterocyclic compounds useful as growth hormone secretagogues
US20080171700A1 (en) 2004-04-07 2008-07-17 Gastrotech Pharma A/S Use Of Secretagogue For The Teatment Of Ghrelin Deficiency
WO2005097174A2 (en) 2004-04-07 2005-10-20 Gastrotech Pharma A/S Uses of a combination of ghrelin and somatotropin for the treatment of cachexia
US7034050B2 (en) 2004-04-28 2006-04-25 Romano Deghenghi Pseudopeptides growth hormone secretagogues
US20050277677A1 (en) 2004-06-10 2005-12-15 Heiman Mark L Method for treating emesis with ghrelin agonists
JP2008506651A (ja) 2004-07-14 2008-03-06 ノバルティス アクチエンゲゼルシャフト Ｄｐｐ−ｉｖ阻害剤と５−ｈｔ３および／または５−ｈｔ４受容体を調節する化合物の組合せ剤
JP2008508221A (ja) 2004-07-28 2008-03-21 グラクソ グループ リミテッド 消化器疾患の治療に有用なピペラジン誘導体
AU2005272598B2 (en) 2004-08-12 2011-11-17 Helsinn Therapeutics (U.S.), Inc. Method of stimulating the motility of the gastrointestinal system using growth hormone secretagogues
US20080261873A1 (en) 2004-08-18 2008-10-23 Elixir Pharmaceuticals, Inc. Growth-Hormone Secretagogues
US8143425B2 (en) 2004-10-12 2012-03-27 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
WO2006046977A1 (en) * 2004-10-26 2006-05-04 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and methods of using the same
WO2006045314A2 (en) 2004-10-27 2006-05-04 Gastrotech Pharma A/S Use of a growth hormone secretatogue for increasing or maintaining lean body mass and/or for treatment of chronic obstructive pulmonary disease
WO2006045319A2 (en) 2004-10-27 2006-05-04 Gastrotech Pharma A/S Uses of growth hormone secretagogues in the treatment of individuals suffering from renal and/or liver failure
DK1814590T4 (da) * 2004-11-01 2014-02-24 Amylin Pharmaceuticals Llc Behandling af obesitet og beslægtede sygdomme.
CU23529A1 (es) 2005-03-02 2010-06-17 Ct Ingenieria Genetica Biotech Combinación de egf/ghrp-6 para la neuroregeneración del sistema nervioso central posterior al dano autoinmune
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
EP1906951A4 (en) 2005-07-01 2009-05-27 Dynogen Pharmaceuticals Inc COMPOSITIONS AND METHODS FOR TREATING GASTROINTESTINAL HYPOMOTILITY AND RELEVANT DISEASES
SI1937262T1 (sl) 2005-09-29 2019-09-30 Ipsen Pharma Spojina za uporabo pri zdravljenju gastrointestinalne dismotilitete
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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CA2677399A1 (en) 2008-10-30
AU2008241532A1 (en) 2008-10-30
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US20080194672A1 (en) 2008-08-14
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