FI68246C - Analogifoerfarande foer framstaellning av nya cyklopeptider - Google Patents
Analogifoerfarande foer framstaellning av nya cyklopeptider Download PDFInfo
- Publication number
- FI68246C FI68246C FI782907A FI782907A FI68246C FI 68246 C FI68246 C FI 68246C FI 782907 A FI782907 A FI 782907A FI 782907 A FI782907 A FI 782907A FI 68246 C FI68246 C FI 68246C
- Authority
- FI
- Finland
- Prior art keywords
- phe
- trp
- thr
- lys
- boc
- Prior art date
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
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- 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
-
- 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
-
- 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
- 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
-
- 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
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)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Endocrinology (AREA)
- Biochemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Claims (6)
1. Förfarande för framställning av terapeutiskt aktiva cyklo-peptider med formeln L r - phe - Phe - trp - Lys - Thr - Phe(W) - X - Y I 56 7 8 9 10 11 12 13 i vilken R betecknar Asn, Ala eller des-R, trp betecknar D-Trp eller L-Trp, som i bensenringen kan vara substituerade med halogenatomer 53 68246 eller nitrogrupper, W betecknar en vid L-fenylalaninrestens bensen-ring som substituent befintlig, eventuellt företrad hydroxylgrupp eller halogenatom, eller väte, X betecknar resten av en ω-amino-(C^-C7)-alkan(mono- eller di-)-karboxylsyra, eller är des-X, och Y betecknar resten av en ω-amino-(C^-C^)-alkan(mono- eller di-)-karboxyl-syra eller des-Y, samt av syraadditionssalter och kbmplex därav, kännetecknat därav, att a) skyddsgruppen(-grupperna) avspjälks frän en förening med farmein L R - Phe - Phe - trp - Lys (A) - Thr(B) - Phe (W) - X - Y -I II i vilken R, W, X, Y och trp betecknar detsanuna som ovan, A betecknar en ε-aminoskyddsgrupp eller väte och B betecknar hydroxylskydds-grupp eller väte, varvid endast en av symbolerna A och B kan beteck-na väte, eller b) en lineär peptid med formeln H - (II') - C III i vilken II' betecknar en den ovan definierade formeln II motsvaran-de rest, i vilken amidbindningen mellan tvä godtyckliga närliggande aminosyrarester i peptidringen är bruten, och C betecknar en fri hydroxylgrupp, en med en aktiveringsgrupp omvandlad hydroxylgrupp eller en hydrazinogrupp -NH-NI^/ cykliseras under samtidigt skydd av en lysinrestens ε-aminogrupp, och därefter avspjälks skyddsgrup-perna, och, om sä önskas, ur ett erhället syraadditionssalt frigörs den motsvarande basen och/eller en erhallen bas överförs i ett syraadditionssalt .
2. Förfarande enligt patentkravet 1, kännetecknat därav, att ett utgängsämne med formeln II, i vilken A betecknar en tert.-butoxikarbonylgrupp och B betecknar en tert.-but.ylgrupp, be-handlas med trifluorättiksyra.
3. Förfarande enligt patentkravet 1, kännetecknat därav, att man framställer en förening, i vilken resten av en ω-amino-(C^-C-,)-alkanmonokarboxylsyra motsvarar formeln - NH - (CH~) - CO - z n d vilken n betecknar ett heltal frän 2 tili 4.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| LU78191A LU78191A1 (de) | 1977-09-28 | 1977-09-28 | Verfahren zur herstellung von neuen cyclopeptiden |
| LU78191 | 1977-09-28 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| FI782907A FI782907A (fi) | 1979-03-29 |
| FI68246B FI68246B (fi) | 1985-04-30 |
| FI68246C true FI68246C (fi) | 1985-08-12 |
Family
ID=19728716
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI782907A FI68246C (fi) | 1977-09-28 | 1978-09-25 | Analogifoerfarande foer framstaellning av nya cyklopeptider |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US4238481A (sv) |
| EP (1) | EP0001295B1 (sv) |
| JP (1) | JPS5459293A (sv) |
| AT (1) | AT370090B (sv) |
| AU (1) | AU523050B2 (sv) |
| CA (1) | CA1111841A (sv) |
| DD (1) | DD140142A5 (sv) |
| DE (1) | DE2861672D1 (sv) |
| DK (1) | DK151034C (sv) |
| ES (1) | ES473677A1 (sv) |
| FI (1) | FI68246C (sv) |
| HU (1) | HU184612B (sv) |
| IE (1) | IE47380B1 (sv) |
| IL (1) | IL55643A (sv) |
| LU (1) | LU78191A1 (sv) |
| NO (1) | NO148957C (sv) |
| NZ (1) | NZ188517A (sv) |
| ZA (1) | ZA785488B (sv) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4328214A (en) * | 1979-07-04 | 1982-05-04 | Ciba-Geigy Corporation | Cyclopeptides and pharmaceutical preparations thereof and also processes for their manufacture |
| NZ195303A (en) * | 1979-10-31 | 1984-10-19 | Merck & Co Inc | Cyclic hexapeptide somatostatin analogues,and pharmaceutical compositions |
| US4369179A (en) * | 1979-12-14 | 1983-01-18 | Ciba-Geigy Corporation | Acylpeptides |
| EP0031303A3 (de) * | 1979-12-21 | 1981-11-04 | Ciba-Geigy Ag | Cyclooctapeptide und pharmazeutische Präparate davon, sowie Verfahren zur Herstellung derselben und ihre Anwendung |
| US4360516A (en) * | 1981-04-13 | 1982-11-23 | Merck & Co., Inc. | Modified D-retro cyclic hexapeptide somatostatin analogs |
| EP0083305B1 (de) * | 1981-12-24 | 1985-07-10 | Ciba-Geigy Ag | Cyclische Octapeptide und pharmazeutische Präparate davon, sowie Verfahren zur Herstellung derselben und ihre Anwendung |
| HUT42101A (en) * | 1985-01-07 | 1987-06-29 | Sandoz Ag | Process for preparing stomatostatine derivatives and pharmaceutical compositions containing such compounds |
| US4798821A (en) * | 1987-03-02 | 1989-01-17 | Merck & Co., Inc. | Antihypertensive therapy for diabetics |
| DE3822557C2 (de) * | 1987-07-10 | 1998-07-02 | Ciba Geigy Ag | Arzneimittel, enthaltend Somatostatine |
| CA2053250A1 (en) * | 1989-04-26 | 1990-10-27 | David H. Coy | Linear somatostatin analogs |
| US5633263A (en) * | 1989-04-26 | 1997-05-27 | The Administrators Of The Tulane Educational Fund | Linear somatostatin analogs |
| US5504069A (en) * | 1993-02-11 | 1996-04-02 | Biomeasure, Inc. | Inhibition of trauma-induced tumor growth |
| US5597894A (en) * | 1995-06-05 | 1997-01-28 | The Louisiana State University Medical Center Foundation | Multi-tyrosinated somatostatin analogs |
| EP0980253B1 (en) * | 1997-05-13 | 2004-03-31 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. | Somatostatin and somatostatin agonists for treating insulin insensitivity and syndrome x |
| WO1998051330A1 (en) * | 1997-05-13 | 1998-11-19 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A. (S.C.R.A.S.) | Method and compositions for treating hyperlipidemia and other conditions |
| WO1998051331A1 (en) * | 1997-05-13 | 1998-11-19 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A. (S.C.R.A.S.) | Somatostatin and somatostatin agonists for decreasing body weight |
| US6004928A (en) * | 1997-05-13 | 1999-12-21 | Biomeasure, Incorporated | Method of treating hyperlipidemia |
| US5968903A (en) * | 1998-05-07 | 1999-10-19 | Biomeasure, Incorporated | Inhibition of H. pylori proliferation |
| PT1401863E (pt) | 2001-06-08 | 2009-07-23 | Ipsen Pharma | Análogos quiméricos da somatostatina-dopamina |
| EP1511761B1 (en) * | 2003-04-07 | 2006-08-02 | Novetide Ltd. | Process for production of cyclic peptides |
| AU2004232314B2 (en) | 2003-04-22 | 2007-11-22 | Ipsen Pharma S.A.S. | Peptide vectors |
| CN102083451A (zh) | 2008-06-12 | 2011-06-01 | 赛恩泰新公司 | 癌症的抑制 |
| US20110171191A1 (en) | 2008-06-12 | 2011-07-14 | Syntaxin Limited | Suppression of neuroendocrine diseases |
| GB0820970D0 (en) | 2008-11-17 | 2008-12-24 | Syntaxin Ltd | Suppression of cancer |
| CA2822442C (en) | 2010-12-22 | 2021-03-16 | The Salk Institute For Biological Studies | Cyclic crf antagonist peptides |
| DK3007704T3 (da) | 2013-06-13 | 2021-03-29 | Antisense Therapeutics Ltd | Kombinationsterapi til akromegali |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4011182A (en) * | 1975-03-21 | 1977-03-08 | American Home Products Corporation | Cyclic undecapeptide analogs of somatostatin and intermediates |
| US4000259A (en) * | 1975-06-16 | 1976-12-28 | American Home Products Corporation | Cyclic dodecapeptide analogs of somatostatin and intermediates |
| NL7607987A (nl) * | 1975-08-08 | 1977-02-10 | Merck & Co Inc | Werkwijze voor het bereiden van peptiden. |
| US3988304A (en) * | 1975-08-25 | 1976-10-26 | American Home Products Corporation | Cyclic dodecapeptide derivatives of somatostatin and intermediates thereof |
| US4133805A (en) * | 1975-12-16 | 1979-01-09 | American Home Products Corporation | Cyclic undecapeptides related to somatostatin and intermediates therefor |
| US4054558A (en) * | 1976-05-24 | 1977-10-18 | American Home Products Corporation | Cyclic dodecapeptide and intermediates therefor |
| EP0000053B1 (en) * | 1977-06-08 | 1981-05-27 | Merck & Co. Inc. | Somatostatin analogs, process for their preparation and pharmaceutical compositions containing them |
| US4115554A (en) * | 1977-08-29 | 1978-09-19 | Merck & Co., Inc. | Somatostatin analogs |
-
1977
- 1977-09-28 LU LU78191A patent/LU78191A1/de unknown
-
1978
- 1978-09-15 US US05/942,565 patent/US4238481A/en not_active Expired - Lifetime
- 1978-09-25 FI FI782907A patent/FI68246C/fi not_active IP Right Cessation
- 1978-09-25 DD DD78208064A patent/DD140142A5/de unknown
- 1978-09-26 CA CA312,129A patent/CA1111841A/en not_active Expired
- 1978-09-26 ES ES473677A patent/ES473677A1/es not_active Expired
- 1978-09-26 DE DE7878100994T patent/DE2861672D1/de not_active Expired
- 1978-09-26 EP EP78100994A patent/EP0001295B1/de not_active Expired
- 1978-09-26 IL IL55643A patent/IL55643A/xx unknown
- 1978-09-27 IE IE1931/78A patent/IE47380B1/en unknown
- 1978-09-27 NZ NZ188517A patent/NZ188517A/xx unknown
- 1978-09-27 AU AU40229/78A patent/AU523050B2/en not_active Expired
- 1978-09-27 AT AT0698278A patent/AT370090B/de not_active IP Right Cessation
- 1978-09-27 ZA ZA00785488A patent/ZA785488B/xx unknown
- 1978-09-27 HU HU78CI1860A patent/HU184612B/hu unknown
- 1978-09-27 NO NO783268A patent/NO148957C/no unknown
- 1978-09-27 DK DK428478A patent/DK151034C/da not_active IP Right Cessation
- 1978-09-28 JP JP11983978A patent/JPS5459293A/ja active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| IE781931L (en) | 1979-03-28 |
| AU523050B2 (en) | 1982-07-08 |
| DE2861672D1 (en) | 1982-04-15 |
| EP0001295A2 (de) | 1979-04-04 |
| DK151034B (da) | 1987-10-12 |
| NO783268L (no) | 1979-03-29 |
| IL55643A (en) | 1981-12-31 |
| DK151034C (da) | 1988-02-22 |
| JPS5459293A (en) | 1979-05-12 |
| IL55643A0 (en) | 1978-12-17 |
| US4238481A (en) | 1980-12-09 |
| ES473677A1 (es) | 1980-05-16 |
| AU4022978A (en) | 1980-04-03 |
| NO148957B (no) | 1983-10-10 |
| DD140142A5 (de) | 1980-02-13 |
| FI782907A (fi) | 1979-03-29 |
| EP0001295A3 (en) | 1979-06-13 |
| NZ188517A (en) | 1981-04-24 |
| ATA698278A (de) | 1982-07-15 |
| AT370090B (de) | 1983-02-25 |
| HU184612B (en) | 1984-09-28 |
| DK428478A (da) | 1979-03-29 |
| CA1111841A (en) | 1981-11-03 |
| NO148957C (no) | 1984-01-18 |
| LU78191A1 (de) | 1979-05-25 |
| FI68246B (fi) | 1985-04-30 |
| IE47380B1 (en) | 1984-03-07 |
| EP0001295B1 (de) | 1982-03-17 |
| ZA785488B (en) | 1979-09-26 |
| JPS6218560B2 (sv) | 1987-04-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM | Patent lapsed |
Owner name: CIBA-GEIGY AG |