AU2007219569B2 - Compounds analogous to growth hormone peptide secretagogues and preparations containing them - Google Patents
Compounds analogous to growth hormone peptide secretagogues and preparations containing themInfo
- Publication number
- AU2007219569B2 AU2007219569B2 AU2007219569A AU2007219569A AU2007219569B2 AU 2007219569 B2 AU2007219569 B2 AU 2007219569B2 AU 2007219569 A AU2007219569 A AU 2007219569A AU 2007219569 A AU2007219569 A AU 2007219569A AU 2007219569 B2 AU2007219569 B2 AU 2007219569B2
- Authority
- AU
- Australia
- Prior art keywords
- ghrelin
- ghs
- growth hormone
- receptor
- compounds
- 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.)
- Ceased
Links
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/60—Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Fodder In General (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CU20060050A CU23558A1 (es) | 2006-02-28 | 2006-02-28 | Compuestos análogos a los secretagogos peptidicos de la hormona de crecimiento |
| CU2006-0050 | 2006-02-28 | ||
| PCT/CU2007/000007 WO2007098716A1 (es) | 2006-02-28 | 2007-02-28 | Compuestos analogos a los secretagogos peptidicos de la hormona de crecimiento y preparaciones que los contienen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2007219569A1 AU2007219569A1 (en) | 2007-09-07 |
| AU2007219569B2 true AU2007219569B2 (en) | 2012-03-15 |
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Family Applications (1)
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|---|---|---|---|
| AU2007219569A Ceased AU2007219569B2 (en) | 2006-02-28 | 2007-02-28 | Compounds analogous to growth hormone peptide secretagogues and preparations containing them |
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| Country | Link |
|---|---|
| US (1) | US8367620B2 (enExample) |
| EP (1) | EP1997827B1 (enExample) |
| JP (1) | JP5183496B2 (enExample) |
| KR (1) | KR101409277B1 (enExample) |
| CN (1) | CN101432294B (enExample) |
| AR (1) | AR059646A1 (enExample) |
| AU (1) | AU2007219569B2 (enExample) |
| BR (1) | BRPI0708366A2 (enExample) |
| CA (1) | CA2637593C (enExample) |
| CL (2) | CL2007000528A1 (enExample) |
| CU (1) | CU23558A1 (enExample) |
| ES (1) | ES2441441T3 (enExample) |
| MX (1) | MX2008011142A (enExample) |
| MY (1) | MY184130A (enExample) |
| NO (1) | NO20084118L (enExample) |
| RU (1) | RU2416618C2 (enExample) |
| WO (1) | WO2007098716A1 (enExample) |
| ZA (1) | ZA200807162B (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2010052828A1 (ja) * | 2008-11-06 | 2010-05-14 | 国立大学法人名古屋大学 | 非虚血性心筋障害に対する医薬 |
| CU24473B1 (es) * | 2016-11-01 | 2020-02-04 | Centro De Ingenieria Genetica Y Biotecnologia Biocubafarma | Composición vacunal que comprende un péptido secretagogo de la hormona de crecimiento como adyuvante vacunal |
| RU2734835C1 (ru) * | 2020-02-11 | 2020-10-23 | Федеральное государственное бюджетное учреждение науки Лимнологический институт Сибирского отделение Российской академии наук (ЛИН СО РАН) | Способ повышения жизнестойкости эмбрионов рыб в аквакультуре |
Family Cites Families (92)
| 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 |
| ATE122357T1 (de) | 1988-01-28 | 1995-05-15 | Polygen Holding Corp | Polypeptide mit hormonwachstumsbefreiender wirkung. |
| 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 |
| JP2670680B2 (ja) | 1988-02-24 | 1997-10-29 | 株式会社ビーエムジー | 生理活性物質含有ポリ乳酸系微小球およびその製造法 |
| WO1992007578A1 (en) | 1990-10-25 | 1992-05-14 | Genentech, Inc. | 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 |
| WO1994011012A1 (en) | 1992-11-06 | 1994-05-26 | Merck & Co., Inc. | Substituted dipeptide analogs promote release of growth hormone |
| US5726319A (en) | 1992-11-06 | 1998-03-10 | Merck & Co., Inc. | Biphenyl 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 |
| NZ258412A (en) | 1992-12-11 | 1997-01-29 | Merck & Co Inc | Spiro-fused piperidine derivatives and pharmaceutical compositions |
| JPH09504525A (ja) | 1993-10-19 | 1997-05-06 | メルク エンド カンパニー インコーポレーテッド | ビスホスホン酸塩類と成長ホルモン分泌促進薬との併用剤 |
| 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 |
| KR960705808A (ko) | 1993-11-09 | 1996-11-08 | 조셉 에프. 디프리마 | 성장 호르몬의 방출을 촉진시키는 피페리딘, 피롤리딘 및 헥사하이드로-1H-아제핀(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 |
| EP0730578A4 (en) | 1993-11-24 | 1997-10-08 | Merck & Co Inc | COMPOUNDS CONTAINING INDOLYL GROUPS AND THE USE THEREOF TO PROMOTE THE RELEASE OF GROWTH HORMONES |
| US5721251A (en) | 1993-12-10 | 1998-02-24 | Merck & Co., Inc. | Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone |
| CA2179597A1 (en) | 1993-12-23 | 1995-06-29 | Nils Langeland Johansen | 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 |
| AU683121B2 (en) | 1993-12-23 | 1997-10-30 | Novo Nordisk A/S | Compounds with growth hormone releasing properties |
| 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 |
| CZ238197A3 (en) | 1995-01-27 | 1997-12-17 | Novo Nordisk As | Growth hormone formation stimulating compounds |
| WO1996024587A1 (en) | 1995-02-09 | 1996-08-15 | 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 |
| 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 |
| FI974368A0 (fi) | 1995-05-29 | 1997-11-28 | Pfizer | Kasvuhormonin vapautumista edistäviä dipeptidejä |
| IL122371A0 (en) | 1995-06-22 | 1998-06-15 | Novo Nordisk As | Compounds with growth hormone releasing properties |
| EP0761220A1 (en) | 1995-08-21 | 1997-03-12 | Eli Lilly And Company | 2-Acylaminopropanamides as growth hormone secretagogues |
| CA2203424A1 (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 |
| JPH11513989A (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薬の湿式造粒製剤 |
| EP0863900A1 (en) | 1995-10-27 | 1998-09-16 | Merck & Co., Inc. | Process for the preparation 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 |
| DE69633637T2 (de) | 1995-12-13 | 2006-03-09 | Merck & Co., Inc. | Wachstumshormonsekretionsförderer rezeptorfamilie |
| JP3798024B2 (ja) | 1995-12-13 | 2006-07-19 | 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物質レセプターアッセイ |
| 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 |
| AU715856B2 (en) | 1995-12-22 | 2000-02-10 | Novo Nordisk A/S | Compounds with growth hormone releasing properties |
| 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 |
| 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 |
| HUP9902668A3 (en) | 1996-04-24 | 2000-07-28 | Novo Nordisk As | Piperazine derivatives, pharmaceutical compositions containing them and their use |
| AU711884B2 (en) | 1996-05-07 | 1999-10-21 | Merck & Co., Inc. | Enhancement of sleep with a growth hormone secretagogue |
| AU2931997A (en) | 1996-05-07 | 1997-11-26 | Merck & Co., Inc. | Treatment of mood disorders 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 |
| CZ383298A3 (cs) | 1996-05-31 | 1999-07-14 | Novo Nordisk A/S | Cyklická (koherentní) léčba osteoporózy komponentou růstového hormonu a činidlem antiresopčně působícím na kost |
| 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 |
| 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 |
| WO1998051687A1 (en) | 1997-05-14 | 1998-11-19 | Fujisawa Pharmaceutical Co., Ltd. | Piperidino derivatives which promote growth hormone release |
| US5861149A (en) | 1997-06-04 | 1999-01-19 | Polyheal Ltd. | Methods for wound treatment |
| EP1005484A1 (en) | 1997-06-20 | 2000-06-07 | Novo Nordisk A/S | Compounds with growth hormone releasing properties |
| ATE356139T1 (de) | 1997-06-25 | 2007-03-15 | Pfizer | Dipeptidderivate zur förderung der sekretion von wachstumshormon |
| 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. |
| CN1213036C (zh) | 1997-08-22 | 2005-08-03 | 科研制药株式会社 | 新的酰胺类衍生物 |
| WO1999036431A1 (en) | 1998-01-16 | 1999-07-22 | 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 |
| 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. |
| 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 |
| KR20010052817A (ko) | 1998-06-16 | 2001-06-25 | 실버스타인 아써 에이. | 근골격 무름을 치료하기 위한 선택적인 에스트로겐 수용체조절제 및 성장 호르몬 분비촉진제의 치료적 혼합물 |
| AR018869A1 (es) | 1998-06-16 | 2001-12-12 | Pfizer Prod Inc | Composicion farmaceutica, su uso para la preparacion de medicamentos y estuche que la contiene |
| RU2298547C2 (ru) | 1998-06-30 | 2007-05-10 | Ново Нордиск А/С | Соединения и фармацевтическая композиция, обладающие свойствами высвобождения гормона роста, способ стимуляции выделения гормона роста из гипофиза млекопитающего |
| US6576656B1 (en) | 1998-08-20 | 2003-06-10 | Sumitomo Pharmaceuticals Co., Ltd. | Oxindole derivative |
| US6358951B1 (en) | 1998-08-21 | 2002-03-19 | Pfizer Inc. | Growth hormone secretagogues |
| EP1258250B1 (en) | 1999-12-28 | 2005-09-14 | Kaken Pharmaceutical Co., Ltd. | Nerve protective drugs |
| EP1353683A4 (en) | 2000-05-30 | 2004-05-12 | Merck & Co Inc | ANALOGS BY GHRELIN |
| EP1159964B1 (en) | 2000-05-31 | 2009-10-28 | Pfizer Products Inc. | Use of growth hormone secretagogues for stimulating gastrointestinal motility |
| CA2407659C (en) | 2000-06-13 | 2010-11-09 | Zentaris Ag | Growth hormone secretagogues |
| EP1297839A4 (en) | 2000-06-23 | 2005-12-07 | Kaken Pharma Co Ltd | PREVENTIVA OR THERAPEUTIC AGAINST HEART FAILURE |
| 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 |
| CU23043A1 (es) | 2001-12-20 | 2005-05-20 | Ct Ingenieria Genetica Biotech | Composicion farmaceutica que contiene factor de crecimiento epidrmico (egf) para la prevencion de la amputacion de pie diabetico. |
| US7476653B2 (en) | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
| WO2005039625A1 (en) | 2003-10-28 | 2005-05-06 | Rheoscience A/S | Growth hormone secretagogue receptor agonists |
| CA2544602A1 (en) | 2003-11-04 | 2005-05-26 | Elixir Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| WO2005048916A2 (en) | 2003-11-20 | 2005-06-02 | Biovitrum Ab | Tetrahydrospiro-beta-carboline-1,3 '-pyrrolidine derivatives and their use in ghsr-related disorders |
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Non-Patent Citations (2)
| Title |
|---|
| CORT JH et al: "Regional and systemic haemodynamic effects of some vasopressins", EUROP. J. CLIN. INVEST, vol. 5, 1975, pages 165-175 * |
| LAMMEK B et al: "Synthesis of three 1-9 NH2-terminallyextended arginine vasopressins with prolonged biological activities", EXPERENTIA, vol. 43, 1987, pages 1211-1212 * |
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0708366A2 (pt) | 2011-05-24 |
| CN101432294A (zh) | 2009-05-13 |
| US8367620B2 (en) | 2013-02-05 |
| JP5183496B2 (ja) | 2013-04-17 |
| ES2441441T3 (es) | 2014-02-04 |
| ZA200807162B (en) | 2009-06-24 |
| EP1997827A1 (en) | 2008-12-03 |
| WO2007098716A1 (es) | 2007-09-07 |
| US20100055118A1 (en) | 2010-03-04 |
| NO20084118L (no) | 2008-09-29 |
| JP2009528303A (ja) | 2009-08-06 |
| MX2008011142A (es) | 2008-09-08 |
| AU2007219569A1 (en) | 2007-09-07 |
| AR059646A1 (es) | 2008-04-16 |
| KR20080110763A (ko) | 2008-12-19 |
| CL2016001648A1 (es) | 2017-02-24 |
| RU2416618C2 (ru) | 2011-04-20 |
| CA2637593A1 (en) | 2007-09-07 |
| KR101409277B1 (ko) | 2014-06-24 |
| EP1997827B1 (en) | 2013-10-09 |
| RU2008138569A (ru) | 2010-04-10 |
| MY184130A (en) | 2021-03-19 |
| CA2637593C (en) | 2015-04-14 |
| CU23558A1 (es) | 2010-07-20 |
| CN101432294B (zh) | 2013-09-11 |
| CL2007000528A1 (es) | 2008-01-18 |
| WO2007098716A8 (es) | 2008-12-18 |
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