EP0000053A1 - Somatostatin-ähnliche Verbindungen, Verfahren zu ihrer Herstellung und pharmazeutische Zusammensetzungen, die sie enthalten - Google Patents
Somatostatin-ähnliche Verbindungen, Verfahren zu ihrer Herstellung und pharmazeutische Zusammensetzungen, die sie enthalten Download PDFInfo
- Publication number
- EP0000053A1 EP0000053A1 EP78100095A EP78100095A EP0000053A1 EP 0000053 A1 EP0000053 A1 EP 0000053A1 EP 78100095 A EP78100095 A EP 78100095A EP 78100095 A EP78100095 A EP 78100095A EP 0000053 A1 EP0000053 A1 EP 0000053A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- phe
- tyr
- thr
- peptide
- resin
- 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.)
- Granted
Links
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- 229910000041 hydrogen chloride Inorganic materials 0.000 description 1
- 239000000413 hydrolysate Substances 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 229940049920 malate Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 150000004702 methyl esters Chemical class 0.000 description 1
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 229920001184 polypeptide Polymers 0.000 description 1
- 229920003053 polystyrene-divinylbenzene Polymers 0.000 description 1
- 239000004304 potassium nitrite Substances 0.000 description 1
- 235000010289 potassium nitrite Nutrition 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000000376 reactant Substances 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000006894 reductive elimination reaction Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000010288 sodium nitrite Nutrition 0.000 description 1
- 238000003746 solid phase reaction Methods 0.000 description 1
- 239000008223 sterile water Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000000057 synthetic resin Substances 0.000 description 1
- IOGXOCVLYRDXLW-UHFFFAOYSA-N tert-butyl nitrite Chemical compound CC(C)(C)ON=O IOGXOCVLYRDXLW-UHFFFAOYSA-N 0.000 description 1
- HPGGPRDJHPYFRM-UHFFFAOYSA-J tin(iv) chloride Chemical compound Cl[Sn](Cl)(Cl)Cl HPGGPRDJHPYFRM-UHFFFAOYSA-J 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Classifications
-
- 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
- C07K14/655—Somatostatins
- C07K14/6555—Somatostatins at least 1 amino acid in D-form
-
- 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
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S930/00—Peptide or protein sequence
- Y10S930/01—Peptide or protein sequence
- Y10S930/16—Somatostatin; related peptides
Definitions
- This invention is concerned with novel somatostatin analogs having a more specific biological activity and duration of activity than naturally occurring somatostatin and which are easier to prepare because of the smaller ring size and having the structural formula: wherein
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Endocrinology (AREA)
- Toxicology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Obesity (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80467877A | 1977-06-08 | 1977-06-08 | |
| US804678 | 1977-06-08 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EP0000053A1 true EP0000053A1 (de) | 1978-12-20 |
| EP0000053B1 EP0000053B1 (de) | 1981-05-27 |
Family
ID=25189555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP78100095A Expired EP0000053B1 (de) | 1977-06-08 | 1978-06-06 | Somatostatin-ähnliche Verbindungen, Verfahren zu ihrer Herstellung und pharmazeutische Zusammensetzungen, die sie enthalten |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US4146612A (de) |
| EP (1) | EP0000053B1 (de) |
| JP (1) | JPS543085A (de) |
| DE (1) | DE2860734D1 (de) |
| DK (1) | DK252778A (de) |
| IE (1) | IE47421B1 (de) |
| IT (1) | IT1105131B (de) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0017746A1 (de) * | 1979-03-13 | 1980-10-29 | Merck & Co. Inc. | Peptide mit Somatostatin-Wirkung, sie enthaltende Zusammensetzungen und Verfahren zur Herstellung der Peptide |
| EP0031303A2 (de) * | 1979-12-21 | 1981-07-01 | Ciba-Geigy Ag | Cyclooctapeptide und pharmazeutische Präparate davon, sowie Verfahren zur Herstellung derselben und ihre Anwendung |
| EP0408371A1 (de) * | 1989-07-14 | 1991-01-16 | Smithkline Beecham Corporation | Hämoregulierende Peptide |
| US5700905A (en) * | 1992-09-01 | 1997-12-23 | The Trustees Of The University Of Pennsylvania | Synthetic somatostatin mimics |
| US5965694A (en) * | 1992-09-01 | 1999-10-12 | The Trustees Of The University Of Pennsylvania | Somatostatin mimics and synthetic methods therefor |
| US6001960A (en) * | 1992-09-01 | 1999-12-14 | The Trustees Of The University Of Pennsylvania | Synthetic somatostatin mimics |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LU78191A1 (de) * | 1977-09-28 | 1979-05-25 | Ciba Geigy Ag | Verfahren zur herstellung von neuen cyclopeptiden |
| NZ195303A (en) * | 1979-10-31 | 1984-10-19 | Merck & Co Inc | Cyclic hexapeptide somatostatin analogues,and pharmaceutical compositions |
| US4508711A (en) * | 1983-04-18 | 1985-04-02 | American Cyanamid Company | Cyclic pentapeptide displaying somatostatin antagonism and method of treatment of mammals therewith |
| DE3845000C2 (de) * | 1987-07-10 | 1998-11-19 | Novartis Ag | Anwendung von Octreotid zur Behandlung von Brustkrebs |
| KR920701248A (ko) * | 1989-11-08 | 1992-08-11 | 고지마 아끼로 | 펩티드, 및 환상 펩티드의 제조 방법 |
| US5504069A (en) * | 1993-02-11 | 1996-04-02 | Biomeasure, Inc. | Inhibition of trauma-induced tumor growth |
| DE4342907A1 (de) * | 1993-12-16 | 1995-06-22 | Bayer Ag | Neue cyclische Depsipeptide mit 18 Ringatomen und ihre Verwendung zur Bekämpfung von Endoparasiten |
| AU4405696A (en) * | 1994-11-03 | 1996-06-06 | Saunders Group Inc., The | Portable traction device |
| US5597894A (en) * | 1995-06-05 | 1997-01-28 | The Louisiana State University Medical Center Foundation | Multi-tyrosinated somatostatin analogs |
| US6004928A (en) * | 1997-05-13 | 1999-12-21 | Biomeasure, Incorporated | Method of treating hyperlipidemia |
| PT980253E (pt) * | 1997-05-13 | 2004-08-31 | Conseils De Rec Appl Scient S | Somatostatina e agonistas de somatostatina para tratar a insensibilidade a insulina e a sindrome x |
| ATE245998T1 (de) * | 1997-05-13 | 2003-08-15 | Sod Conseils Rech Applic | Somatostatin agoniste zur reduzierung von körpergewicht |
| EP0981364B1 (de) * | 1997-05-13 | 2006-03-01 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. | Methoden und zusammensetzungen zur behandlung der hyperlipidämie |
| US5968903A (en) * | 1998-05-07 | 1999-10-19 | Biomeasure, Incorporated | Inhibition of H. pylori proliferation |
| US6171273B1 (en) | 1999-08-06 | 2001-01-09 | The Saunders Group, Inc. | Self-seating occiput wedge system for applying a therapeutic traction force |
| ES2325880T3 (es) | 2001-06-08 | 2009-09-23 | Ipsen Pharma | Analogos quimericos de somatostatina-dopamina. |
| US7189214B1 (en) * | 2002-01-22 | 2007-03-13 | The Saunders Group, Inc. | Multi-axis cervical and lumbar traction table |
| US20040145462A1 (en) * | 2003-01-29 | 2004-07-29 | Honda Giken Kogyo Kabushiki Kaisha | Variable electronic display apparatus for a vehicle, and method of using same |
| US8709998B2 (en) | 2003-04-22 | 2014-04-29 | Ipsen Pharma S.A.S. | Peptide vectors |
| KR101642363B1 (ko) | 2008-06-12 | 2016-07-25 | 입센 바이오이노베이션 리미티드 | 신경내분비계 질환의 억제 |
| CN102083451A (zh) | 2008-06-12 | 2011-06-01 | 赛恩泰新公司 | 癌症的抑制 |
| GB0820970D0 (en) | 2008-11-17 | 2008-12-24 | Syntaxin Ltd | Suppression of cancer |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2460469A1 (de) * | 1974-12-20 | 1976-07-01 | Hoechst Ag | Neue peptide mit biologischer wirkung und verfahren zu ihrer herstellung |
| FR2336943A1 (fr) * | 1976-01-02 | 1977-07-29 | Ayerst Mckenna & Harrison | Derives de la somatostatine et leur preparation |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US781610A (en) * | 1904-01-11 | 1905-01-31 | Winfield S Livengood | Wagon-brake. |
| US3904594A (en) * | 1973-07-02 | 1975-09-09 | Salk Inst For Biological Studi | Somatostatin and acylated des-(ala' 1', gly' 2') derivatives thereof |
| US3882098A (en) * | 1974-01-03 | 1975-05-06 | American Home Prod | Synthesis of des-Ala{hu 1{b , Gly{hu 2{b , Asn{hu 5{b -SRIF and intermediates |
| US3933784A (en) * | 1975-01-27 | 1976-01-20 | American Home Products Corporation | Des-(ser13)-srif and intermediates |
| US4011182A (en) * | 1975-03-21 | 1977-03-08 | American Home Products Corporation | Cyclic undecapeptide analogs of somatostatin and intermediates |
-
1978
- 1978-06-06 IE IE1151/78A patent/IE47421B1/en unknown
- 1978-06-06 DE DE7878100095T patent/DE2860734D1/de not_active Expired
- 1978-06-06 IT IT49736/78A patent/IT1105131B/it active
- 1978-06-06 EP EP78100095A patent/EP0000053B1/de not_active Expired
- 1978-06-07 DK DK252778A patent/DK252778A/da unknown
- 1978-06-07 JP JP6872378A patent/JPS543085A/ja active Pending
- 1978-06-29 US US05/920,529 patent/US4146612A/en not_active Expired - Lifetime
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2460469A1 (de) * | 1974-12-20 | 1976-07-01 | Hoechst Ag | Neue peptide mit biologischer wirkung und verfahren zu ihrer herstellung |
| FR2336943A1 (fr) * | 1976-01-02 | 1977-07-29 | Ayerst Mckenna & Harrison | Derives de la somatostatine et leur preparation |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0017746A1 (de) * | 1979-03-13 | 1980-10-29 | Merck & Co. Inc. | Peptide mit Somatostatin-Wirkung, sie enthaltende Zusammensetzungen und Verfahren zur Herstellung der Peptide |
| EP0031303A2 (de) * | 1979-12-21 | 1981-07-01 | Ciba-Geigy Ag | Cyclooctapeptide und pharmazeutische Präparate davon, sowie Verfahren zur Herstellung derselben und ihre Anwendung |
| EP0031303A3 (de) * | 1979-12-21 | 1981-11-04 | Ciba-Geigy Ag | Cyclooctapeptide und pharmazeutische Präparate davon, sowie Verfahren zur Herstellung derselben und ihre Anwendung |
| EP0408371A1 (de) * | 1989-07-14 | 1991-01-16 | Smithkline Beecham Corporation | Hämoregulierende Peptide |
| US5700905A (en) * | 1992-09-01 | 1997-12-23 | The Trustees Of The University Of Pennsylvania | Synthetic somatostatin mimics |
| US5965694A (en) * | 1992-09-01 | 1999-10-12 | The Trustees Of The University Of Pennsylvania | Somatostatin mimics and synthetic methods therefor |
| US6001960A (en) * | 1992-09-01 | 1999-12-14 | The Trustees Of The University Of Pennsylvania | Synthetic somatostatin mimics |
Also Published As
| Publication number | Publication date |
|---|---|
| US4146612A (en) | 1979-03-27 |
| DK252778A (da) | 1978-12-09 |
| IE47421B1 (en) | 1984-03-07 |
| IT7849736A0 (it) | 1978-06-06 |
| JPS543085A (en) | 1979-01-11 |
| EP0000053B1 (de) | 1981-05-27 |
| IT1105131B (it) | 1985-10-28 |
| IE781151L (en) | 1978-12-08 |
| DE2860734D1 (en) | 1981-09-03 |
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