EP0000053A1 - Analogues de la somatostatine, procédé pour leur préparation et des compositions pharmaceutiques les contenant - Google Patents

Analogues de la somatostatine, procédé pour leur préparation et des compositions pharmaceutiques les contenant Download PDF

Info

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
Application number
EP78100095A
Other languages
German (de)
English (en)
Other versions
EP0000053B1 (fr
Inventor
Daniel Frank Veber
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0000053A1 publication Critical patent/EP0000053A1/fr
Application granted granted Critical
Publication of EP0000053B1 publication Critical patent/EP0000053B1/fr
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/655Somatostatins
    • C07K14/6555Somatostatins at least 1 amino acid in D-form
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL 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
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S930/00Peptide or protein sequence
    • Y10S930/01Peptide or protein sequence
    • Y10S930/16Somatostatin; 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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
EP78100095A 1977-06-08 1978-06-06 Analogues de la somatostatine, procédé pour leur préparation et des compositions pharmaceutiques les contenant Expired EP0000053B1 (fr)

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 (fr) 1978-12-20
EP0000053B1 EP0000053B1 (fr) 1981-05-27

Family

ID=25189555

Family Applications (1)

Application Number Title Priority Date Filing Date
EP78100095A Expired EP0000053B1 (fr) 1977-06-08 1978-06-06 Analogues de la somatostatine, procédé pour leur préparation et des compositions pharmaceutiques les contenant

Country Status (7)

Country Link
US (1) US4146612A (fr)
EP (1) EP0000053B1 (fr)
JP (1) JPS543085A (fr)
DE (1) DE2860734D1 (fr)
DK (1) DK252778A (fr)
IE (1) IE47421B1 (fr)
IT (1) IT1105131B (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0017746A1 (fr) * 1979-03-13 1980-10-29 Merck & Co. Inc. Peptides à activité analogue à la somatostatine, compositions les contenant et procédé pour la fabrication des peptides
EP0031303A2 (fr) * 1979-12-21 1981-07-01 Ciba-Geigy Ag Cyclooctapeptides et leurs préparations pharmaceutiques, procédé pour leur préparation et leur application
EP0408371A1 (fr) * 1989-07-14 1991-01-16 Smithkline Beecham Corporation Peptides de hemoregulation
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)

* Cited by examiner, † Cited by third party
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
CA2045495A1 (fr) * 1989-11-08 1991-05-09 Masutaka Ohsaki Peptides et procedes de production de peptides cycliques
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
WO1996014810A2 (fr) 1994-11-03 1996-05-23 The Saunders Group, Inc. Dispositif de traction transportable
US5597894A (en) * 1995-06-05 1997-01-28 The Louisiana State University Medical Center Foundation Multi-tyrosinated somatostatin analogs
WO1998051330A1 (fr) * 1997-05-13 1998-11-19 Societe De Conseils De Recherches Et D'applications Scientifiques S.A. (S.C.R.A.S.) Procede et compositions pour traiter l'hyperlipidemie et d'autres etats pathologiques
ATE245998T1 (de) * 1997-05-13 2003-08-15 Sod Conseils Rech Applic Somatostatin agoniste zur reduzierung von körpergewicht
US6004928A (en) * 1997-05-13 1999-12-21 Biomeasure, Incorporated Method of treating hyperlipidemia
DE69822810T2 (de) * 1997-05-13 2005-02-03 Société de Conseils de Recherches et d'Applications Scientifiques S.A.S. Somatostatin und somatostatin agoniste zur behandlung der insulinsunempfindlichkeit und syndrome x
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
ATE424414T1 (de) 2001-06-08 2009-03-15 Sod Conseils Rech Applic Chimere somatostatin-dopamin-analoga
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
CN102112145B (zh) 2008-06-12 2014-07-30 辛它可辛有限公司 神经内分泌病的抑制
EP2310029B1 (fr) 2008-06-12 2019-04-03 Ipsen Bioinnovation Limited Protéines de fusion pour leur utilisation dans le traitement du cancer
GB0820970D0 (en) 2008-11-17 2008-12-24 Syntaxin Ltd Suppression of cancer

Citations (2)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0017746A1 (fr) * 1979-03-13 1980-10-29 Merck & Co. Inc. Peptides à activité analogue à la somatostatine, compositions les contenant et procédé pour la fabrication des peptides
EP0031303A2 (fr) * 1979-12-21 1981-07-01 Ciba-Geigy Ag Cyclooctapeptides et leurs préparations pharmaceutiques, procédé pour leur préparation et leur application
EP0031303A3 (fr) * 1979-12-21 1981-11-04 Ciba-Geigy Ag Cyclooctapeptides et leurs préparations pharmaceutiques, procédé pour leur préparation et leur application
EP0408371A1 (fr) * 1989-07-14 1991-01-16 Smithkline Beecham Corporation Peptides de hemoregulation
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
IT7849736A0 (it) 1978-06-06
DE2860734D1 (en) 1981-09-03
US4146612A (en) 1979-03-27
IE781151L (en) 1978-12-08
EP0000053B1 (fr) 1981-05-27
IT1105131B (it) 1985-10-28
DK252778A (da) 1978-12-09
IE47421B1 (en) 1984-03-07
JPS543085A (en) 1979-01-11

Similar Documents

Publication Publication Date Title
EP0000053B1 (fr) Analogues de la somatostatine, procédé pour leur préparation et des compositions pharmaceutiques les contenant
US4191754A (en) Bicyclic somatostatin analogs
US4310518A (en) Cyclic hexapeptide somatostatin analogs
EP0017746B1 (fr) Peptides à activité analogue à la somatostatine, compositions les contenant et procédé pour la fabrication des peptides
Cai et al. Synthesis and biological activity of highly potent octapeptide analogs of somatostatin.
US4235886A (en) Cyclic hexapeptide somatostatin analogs
EP0143307B1 (fr) Hexapeptides cycliques analogues au somatostatin, procédé de leur préparation et compositions pharmaceutiques les contenant
US4087390A (en) Somatostatin analogs and intermediates thereto
EP0063308B1 (fr) D-rétro hexapeptides cycliques modifiés, analogues de somatostatine, leur procédé de préparation et compositions thérapeutiques les contenant
US4238481A (en) Novel cyclopeptides
KR850000415B1 (ko) 아실펩타이드의 제조방법
US4486415A (en) Cyclic hexapeptide somatostatin analogs
US4162248A (en) Somatostatin analogs
EP0206118B1 (fr) Analogues des hexapeptides cycliques de somatostatine, leur procédé de préparation et compositions pharmaceutiques les contenant
EP0000919B1 (fr) Analogues de somatostatine, leur procédé de préparation et leur utilisation comme produits pharmaceutiques.
US4703034A (en) Novel cyclic tetrapeptide
EP0190946A2 (fr) Antagonistes LHRH d'hexapeptide cyclique
EP0002264B1 (fr) Analogues de la somatostatine, leur procédé de préparation et leur composition pharmaceutique
EP0029310B1 (fr) Hexapeptides cycliques analogues à la somatostatine, procédé pour leur préparation et compositions pharmaceutiques les contenant
EP0002262B1 (fr) Analogues de la somatostatine et leur procédé de préparation
EP0113029B1 (fr) Hexapeptides dicycliques, leur procédé de préparation et leurs compositions pharmaceutiques
EP0104348A2 (fr) Héxapeptides cycliques fluorés analogues de somatostatine, leur procédé de préparation, les intermédiaires servant à leur préparation et les compositions pharmaceutiques les contenant
US4159263A (en) (D-Ala5)-somatostatin and analogues thereof
IE46462B1 (en) Somatostatin peptide analogues
JPS636560B2 (fr)

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

AK Designated contracting states

Kind code of ref document: A1

Designated state(s): BE CH DE FR GB LU NL SE

17P Request for examination filed
GRAA (expected) grant

Free format text: ORIGINAL CODE: 0009210

AK Designated contracting states

Kind code of ref document: B1

Designated state(s): BE CH DE FR GB LU NL SE

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: LU

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 19810630

REF Corresponds to:

Ref document number: 2860734

Country of ref document: DE

Date of ref document: 19810903

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: FR

Payment date: 19820322

Year of fee payment: 5

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: BE

Payment date: 19820331

Year of fee payment: 5

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: LU

Payment date: 19820525

Year of fee payment: 5

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: SE

Payment date: 19820630

Year of fee payment: 5

Ref country code: NL

Payment date: 19820630

Year of fee payment: 5

Ref country code: DE

Payment date: 19820630

Year of fee payment: 5

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: CH

Payment date: 19830301

Year of fee payment: 6

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: BE

Effective date: 19830606

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: SE

Effective date: 19830607

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: NL

Effective date: 19840101

GBPC Gb: european patent ceased through non-payment of renewal fee
NLV4 Nl: lapsed or anulled due to non-payment of the annual fee
PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: FR

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 19840229

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: DE

Effective date: 19840301

REG Reference to a national code

Ref country code: FR

Ref legal event code: ST

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: CH

Effective date: 19840630

REG Reference to a national code

Ref country code: CH

Ref legal event code: PL

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: GB

Effective date: 19881117

EUG Se: european patent has lapsed

Ref document number: 78100095.5

Effective date: 19850610

PLBE No opposition filed within time limit

Free format text: ORIGINAL CODE: 0009261

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: NO OPPOSITION FILED WITHIN TIME LIMIT