ES476901A1 - Un procedimiento para la preparacion de nuevos derivados de somatostatina. - Google Patents
Un procedimiento para la preparacion de nuevos derivados de somatostatina.Info
- Publication number
- ES476901A1 ES476901A1 ES476901A ES476901A ES476901A1 ES 476901 A1 ES476901 A1 ES 476901A1 ES 476901 A ES476901 A ES 476901A ES 476901 A ES476901 A ES 476901A ES 476901 A1 ES476901 A1 ES 476901A1
- Authority
- ES
- Spain
- Prior art keywords
- hydrogen
- phe
- protecting group
- thr
- intermediates
- 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
Links
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical class C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000006239 protecting group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000004793 Polystyrene Substances 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 229920002223 polystyrene Polymers 0.000 abstract 1
- 239000011347 resin Substances 0.000 abstract 1
- 229920005989 resin Polymers 0.000 abstract 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 abstract 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
- 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
-
- 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
- Y10S930/28—Bound to a nonpeptide drug, nonpeptide label, nonpeptide carrier, or a nonpeptide resin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biophysics (AREA)
- Medicinal Chemistry (AREA)
- Zoology (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Endocrinology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
Abstract
Un procedimiento para la preparación de nuevos derivados de somatostatina de fórmula (II), R-D-Val-Gly-L-Cys(R1)-L-Lys(R2)-L-Asn-L-Phe-L-Phe-L-Trp(R5)-L-Lys(R2)-L-Thr(R3)-L-Phe-L-Thr(R3)-L-Phe-L-Thr(R3)-L-Ser(R4)-L-Cys(R1)-X, en la cual: R es un hidrógeno o un grupo de protección de ¿amino R1 es un hidrógeno o un grupo de protección de tio; R2 es hidrógeno o un grupo de protección de ¿amino; R3 y R4 son cada uno hidrógeno o un grupo de protección hidroxi; R5 es hidrógeno o formilo; y X es hidroxi o *** en donde la resina es poliestireno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US05/789,472 US4100117A (en) | 1977-04-21 | 1977-04-21 | Somatostatin analogs and intermediates thereto |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES476901A1 true ES476901A1 (es) | 1979-10-16 |
Family
ID=25147748
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES469005A Expired ES469005A1 (es) | 1977-04-21 | 1978-04-20 | Un procedimiento para la preparacion de nuevos derivados de somatostatina |
| ES476901A Expired ES476901A1 (es) | 1977-04-21 | 1979-01-16 | Un procedimiento para la preparacion de nuevos derivados de somatostatina. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES469005A Expired ES469005A1 (es) | 1977-04-21 | 1978-04-20 | Un procedimiento para la preparacion de nuevos derivados de somatostatina |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US4100117A (es) |
| JP (1) | JPS53132588A (es) |
| AR (1) | AR221699A1 (es) |
| AT (1) | AT361142B (es) |
| AU (1) | AU519275B2 (es) |
| BE (1) | BE866117A (es) |
| BG (1) | BG28703A3 (es) |
| CA (2) | CA1102315A (es) |
| CH (1) | CH634039A5 (es) |
| CS (1) | CS202096B2 (es) |
| DD (1) | DD135900A5 (es) |
| DE (1) | DE2816854A1 (es) |
| DK (1) | DK174278A (es) |
| ES (2) | ES469005A1 (es) |
| FI (1) | FI64576C (es) |
| FR (1) | FR2387941A1 (es) |
| GB (1) | GB1596328A (es) |
| GR (1) | GR68945B (es) |
| HU (1) | HU177435B (es) |
| IE (1) | IE46868B1 (es) |
| IL (1) | IL54533A (es) |
| IT (1) | IT1094462B (es) |
| NL (1) | NL7804218A (es) |
| NZ (1) | NZ187009A (es) |
| PL (2) | PL115827B1 (es) |
| PT (1) | PT67913B (es) |
| RO (2) | RO81079A (es) |
| SE (1) | SE7804397L (es) |
| SU (2) | SU730295A3 (es) |
| YU (1) | YU91578A (es) |
| ZA (1) | ZA782247B (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4202802A (en) * | 1978-10-02 | 1980-05-13 | Eli Lilly And Company | Peptides related to somatostatin |
| US4199501A (en) * | 1978-11-20 | 1980-04-22 | Eli Lilly And Company | Peptides related to somatostatin |
| US4199500A (en) * | 1978-11-20 | 1980-04-22 | Eli Lilly And Company | Peptides related to somatostatin |
| US4428942A (en) | 1982-05-17 | 1984-01-31 | The Salk Institute For Biological Studies | Analogs of somatostatin |
| GB8423431D0 (en) * | 1984-09-17 | 1984-10-24 | Sandoz Ltd | Organic compounds |
| SE8702550D0 (sv) * | 1987-06-18 | 1987-06-18 | Anders Grubb | Cysteinproteashemmare |
| NZ240214A (en) | 1990-10-16 | 1993-02-25 | Takeda Chemical Industries Ltd | Polymer compositions comprising a polylactic acid and a copolymer of glycolic acid and a hydroxycarboxylic acid; use as carrier for prolonged release pharmaceutical compositions of water soluble drugs |
| ATE161716T1 (de) | 1992-08-07 | 1998-01-15 | Takeda Chemical Industries Ltd | Herstellung von mikrokapseln, die wasserlösliche arzneimittel enthalten |
| ATE178789T1 (de) * | 1994-02-21 | 1999-04-15 | Takeda Chemical Industries Ltd | Polyester matrix für eine pharmazeutische zusammensetzung mit verzögerter freigabe |
| US6117455A (en) | 1994-09-30 | 2000-09-12 | Takeda Chemical Industries, Ltd. | Sustained-release microcapsule of amorphous water-soluble pharmaceutical active agent |
| CA2192782C (en) | 1995-12-15 | 2008-10-14 | Nobuyuki Takechi | Production of microspheres |
| CN1095681C (zh) * | 1996-06-20 | 2002-12-11 | 久光制药株式会社 | 一种用于离子电渗疗法的装置结构 |
| US6309633B1 (en) | 1999-06-19 | 2001-10-30 | Nobex Corporation | Amphiphilic drug-oligomer conjugates with hydroyzable lipophile components and methods for making and using the same |
| US7169889B1 (en) | 1999-06-19 | 2007-01-30 | Biocon Limited | Insulin prodrugs hydrolyzable in vivo to yield peglylated insulin |
| WO2002043709A1 (fr) | 2000-12-01 | 2002-06-06 | Takeda Chemical Industries, Ltd. | Procede de production d'une preparation contenant une substance bioactive |
| US6867183B2 (en) * | 2001-02-15 | 2005-03-15 | Nobex Corporation | Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith |
| US7060675B2 (en) * | 2001-02-15 | 2006-06-13 | Nobex Corporation | Methods of treating diabetes mellitus |
| US6835802B2 (en) * | 2001-06-04 | 2004-12-28 | Nobex Corporation | Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties |
| US6828297B2 (en) | 2001-06-04 | 2004-12-07 | Nobex Corporation | Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same |
| US6828305B2 (en) * | 2001-06-04 | 2004-12-07 | Nobex Corporation | Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same |
| US7713932B2 (en) * | 2001-06-04 | 2010-05-11 | Biocon Limited | Calcitonin drug-oligomer conjugates, and uses thereof |
| US6713452B2 (en) | 2001-06-04 | 2004-03-30 | Nobex Corporation | Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same |
| US6858580B2 (en) * | 2001-06-04 | 2005-02-22 | Nobex Corporation | Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same |
| US6913903B2 (en) * | 2001-09-07 | 2005-07-05 | Nobex Corporation | Methods of synthesizing insulin polypeptide-oligomer conjugates, and proinsulin polypeptide-oligomer conjugates and methods of synthesizing same |
| US7166571B2 (en) * | 2001-09-07 | 2007-01-23 | Biocon Limited | Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same |
| US7312192B2 (en) * | 2001-09-07 | 2007-12-25 | Biocon Limited | Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same |
| US7196059B2 (en) | 2001-09-07 | 2007-03-27 | Biocon Limited | Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith |
| WO2003105768A2 (en) * | 2002-06-13 | 2003-12-24 | Nobex Corporation | Methods of reducing hypoglycemic episodes in the treatment of diabetes mellitus |
| CN101027318B (zh) * | 2004-07-19 | 2016-05-25 | 比奥孔有限公司 | 胰岛素-低聚物共轭物，制剂及其用途 |
| US9241908B2 (en) | 2007-10-16 | 2016-01-26 | Biocon Limited | Orally administrable solid pharmaceutical composition and a process thereof |
| US20150157619A1 (en) | 2012-07-10 | 2015-06-11 | Takeda Pharmaceutical Company Limited | Pharmaceutical preparation for injection |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2608336A1 (de) * | 1975-03-11 | 1976-09-30 | Sandoz Ag | Neue organische verbindungen, ihre herstellung und verwendung |
| US4372884A (en) * | 1975-08-06 | 1983-02-08 | The Salk Institute For Biological Studies | Pharmaceutically active peptides |
-
1977
- 1977-04-21 US US05/789,472 patent/US4100117A/en not_active Expired - Lifetime
-
1978
- 1978-04-17 GB GB14916/78A patent/GB1596328A/en not_active Expired
- 1978-04-18 NZ NZ187009A patent/NZ187009A/xx unknown
- 1978-04-18 DE DE19782816854 patent/DE2816854A1/de not_active Withdrawn
- 1978-04-18 AR AR271820A patent/AR221699A1/es active
- 1978-04-18 IL IL54533A patent/IL54533A/xx unknown
- 1978-04-18 PT PT67913A patent/PT67913B/pt unknown
- 1978-04-18 YU YU00915/78A patent/YU91578A/xx unknown
- 1978-04-18 SE SE7804397A patent/SE7804397L/xx unknown
- 1978-04-18 RO RO78102194A patent/RO81079A/ro unknown
- 1978-04-18 JP JP4621378A patent/JPS53132588A/ja active Pending
- 1978-04-18 FI FI781184A patent/FI64576C/fi not_active IP Right Cessation
- 1978-04-18 RO RO7893835A patent/RO76054A/ro unknown
- 1978-04-19 AU AU35253/78A patent/AU519275B2/en not_active Expired
- 1978-04-19 BE BE1008847A patent/BE866117A/xx not_active IP Right Cessation
- 1978-04-19 IE IE765/78A patent/IE46868B1/en unknown
- 1978-04-19 ZA ZA00782247A patent/ZA782247B/xx unknown
- 1978-04-19 GR GR56030A patent/GR68945B/el unknown
- 1978-04-19 CA CA301,500A patent/CA1102315A/en not_active Expired
- 1978-04-19 FR FR7811580A patent/FR2387941A1/fr active Granted
- 1978-04-20 AT AT282878A patent/AT361142B/de not_active IP Right Cessation
- 1978-04-20 DK DK174278A patent/DK174278A/da active IP Right Grant
- 1978-04-20 NL NL7804218A patent/NL7804218A/xx not_active Application Discontinuation
- 1978-04-20 CH CH425778A patent/CH634039A5/de not_active IP Right Cessation
- 1978-04-20 IT IT22552/78A patent/IT1094462B/it active
- 1978-04-20 HU HU78EI790A patent/HU177435B/hu unknown
- 1978-04-20 ES ES469005A patent/ES469005A1/es not_active Expired
- 1978-04-20 SU SU782607708A patent/SU730295A3/ru active
- 1978-04-21 BG BG039503A patent/BG28703A3/xx unknown
- 1978-04-21 PL PL1978217479A patent/PL115827B1/pl unknown
- 1978-04-21 PL PL1978206280A patent/PL114533B1/pl unknown
- 1978-04-21 CS CS782580A patent/CS202096B2/cs unknown
- 1978-04-21 DD DD78204957A patent/DD135900A5/xx unknown
-
1979
- 1979-01-05 SU SU792705047A patent/SU904519A3/ru active
- 1979-01-16 ES ES476901A patent/ES476901A1/es not_active Expired
-
1980
- 1980-12-08 CA CA366,345A patent/CA1113928A/en not_active Expired
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD1A | Patent lapsed |
Effective date: 20001204 |