PT74720B - Process for preparing modified d.retro cyclic hexapeptide somatostatin analogs - Google Patents

Process for preparing modified d.retro cyclic hexapeptide somatostatin analogs

Info

Publication number: PT74720B
Authority: PT; Portugal
Prior art keywords: loweralkyl; benzyl; loweralkoxy; substituent; halogen
Prior art date: 1981-04-13

Application number

PT74720A

Other languages

English (en)

Other versions

PT74720A (en

Inventor

Roger M Freidinger

Daniel F Veber

Original Assignee

Merck & 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.)

1981-04-13

Filing date

1982-04-07

Publication date

1985-01-08

1982-04-07 Application filed by Merck & Co Inc filed Critical Merck & Co Inc

1982-05-01 Publication of PT74720A publication Critical patent/PT74720A/pt

1985-01-08 Publication of PT74720B publication Critical patent/PT74720B/pt

Links

125000004122 cyclic group Chemical group 0.000 title 1
238000004519 manufacturing process Methods 0.000 title 1
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 1
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 6
229910052736 halogen Inorganic materials 0.000 abstract 4
150000002367 halogens Chemical class 0.000 abstract 4
-1 hydroxy, amino Chemical group 0.000 abstract 4
125000001424 substituent group Chemical group 0.000 abstract 4
125000000217 alkyl group Chemical group 0.000 abstract 3
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
229910052717 sulfur Inorganic materials 0.000 abstract 2
239000011593 sulfur Substances 0.000 abstract 2
125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
125000004432 carbon atom Chemical group C* 0.000 abstract 1
150000001875 compounds Chemical class 0.000 abstract 1
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
229910052739 hydrogen Inorganic materials 0.000 abstract 1
239000001257 hydrogen Substances 0.000 abstract 1
125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
125000001147 pentyl group Chemical group C(CCCC)* 0.000 abstract 1
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- 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
- 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)
Life Sciences & Earth Sciences (AREA)
Organic Chemistry (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Diabetes (AREA)
Veterinary Medicine (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Endocrinology (AREA)
Animal Behavior & Ethology (AREA)
Bioinformatics & Cheminformatics (AREA)
Public Health (AREA)
Engineering & Computer Science (AREA)
Genetics & Genomics (AREA)
Biochemistry (AREA)
Obesity (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Toxicology (AREA)
Zoology (AREA)
Gastroenterology & Hepatology (AREA)
Hematology (AREA)
Biophysics (AREA)
Emergency Medicine (AREA)
Molecular Biology (AREA)
Ophthalmology & Optometry (AREA)
Peptides Or Proteins (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Plural Heterocyclic Compounds (AREA)

PT74720A 1981-04-13 1982-04-07 Process for preparing modified d.retro cyclic hexapeptide somatostatin analogs PT74720B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US06/254,010 US4360516A (en)	1981-04-13	1981-04-13	Modified D-retro cyclic hexapeptide somatostatin analogs

Publications (2)

Publication Number	Publication Date
PT74720A PT74720A (en)	1982-05-01
PT74720B true PT74720B (en)	1985-01-08

Family

ID=22962578

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PT74720A PT74720B (en)	1981-04-13	1982-04-07	Process for preparing modified d.retro cyclic hexapeptide somatostatin analogs

Country Status (9)

Country	Link
US (1)	US4360516A (pt)
EP (1)	EP0063308B1 (pt)
JP (1)	JPS57179142A (pt)
AT (1)	ATE14439T1 (pt)
DE (1)	DE3264861D1 (pt)
DK (1)	DK159382A (pt)
ES (1)	ES511335A0 (pt)
GR (1)	GR75544B (pt)
PT (1)	PT74720B (pt)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4427661A (en) *	1982-07-30	1984-01-24	Merck & Co., Inc.	Fluorinated cyclic hexapeptide somatostatin analogs
CH655505B (pt) *	1982-08-24	1986-04-30
DE3303345A1 (de) *	1983-02-02	1984-08-02	Hoechst Ag, 6230 Frankfurt	Cyclische peptide mit somatostatin-wirkung
US4508711A (en) *	1983-04-18	1985-04-02	American Cyanamid Company	Cyclic pentapeptide displaying somatostatin antagonism and method of treatment of mammals therewith
US4522813A (en) *	1983-10-27	1985-06-11	Merck & Co., Inc.	Cyclic hexapeptide somatostatin analogs
US4612302A (en) *	1983-11-14	1986-09-16	Brigham And Women's Hospital	Clinical use of somatostatin analogues
US4612366A (en) *	1985-06-17	1986-09-16	Merck & Co., Inc.	Cyclic hexapeptide somatostatin analogs
AU1194092A (en) *	1991-02-06	1992-09-07	Georgetown University	Receptor blocking peptides of fibroblast growth factor receptor
ATE181240T1 (de) *	1991-02-08	1999-07-15	Biomeasure Inc	Verwendung von somatostatinanalogen zur behandlung von melanomen
US5811512A (en) *	1991-08-22	1998-09-22	The Trustees Of The University Of Pennsylvania	Non-peptide peptidomimetics and related cyclic hexapeptides
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
US5770687A (en) *	1995-06-07	1998-06-23	Peptor Limited	Comformationally constrained backbone cyclized somatostatin analogs
CA2290592A1 (en) *	1997-05-13	1998-11-19	Michael Anthony Cawthorne	Somatostatin and somatostatin agonists for decreasing body weight
EP0981364B1 (en) *	1997-05-13	2006-03-01	Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S.	Method and compositions for treating hyperlipidemia
US6004928A (en) *	1997-05-13	1999-12-21	Biomeasure, Incorporated	Method of treating hyperlipidemia
CA2289499C (en) *	1997-05-13	2010-02-23	Michael Anthony Cawthorne	Somatostatin and somatostatin agonists for treating insulin insensitivity and syndrome x
US5968903A (en) *	1998-05-07	1999-10-19	Biomeasure, Incorporated	Inhibition of H. pylori proliferation
NZ530007A (en)	2001-06-08	2006-02-24	Sod Conseils Rech Applic	Somatostatin-dopamine chimeric analogues that retain both somatostatin and dopamine activity in vivo and display enhanced biological activity
CA2523197C (en)	2003-04-22	2016-05-24	Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S.	Peptide vectors
WO2009150470A2 (en)	2008-06-12	2009-12-17	Syntaxin Limited	Suppression of cancers
EP2310028B1 (en)	2008-06-12	2016-11-16	Ipsen Bioinnovation Limited	Fusion proteins for use in the treatment of acromegaly
GB0820970D0 (en)	2008-11-17	2008-12-24	Syntaxin Ltd	Suppression of cancer
EP3007704B1 (en)	2013-06-13	2021-01-06	Antisense Therapeutics Ltd	Combination therapy for acromegaly

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CA1101843A (en) *	1976-08-02	1981-05-26	Daniel F. Veber	Cyclic hexapeptides useful for increasing feed efficiency
US4162248A (en) *	1976-10-14	1979-07-24	Merck & Co., Inc.	Somatostatin analogs
LU78191A1 (de) *	1977-09-28	1979-05-25	Ciba Geigy Ag	Verfahren zur herstellung von neuen cyclopeptiden
US4190648A (en) *	1979-03-13	1980-02-26	Merck & Co., Inc.	Peptides having somatostatin activity
US4235886A (en) *	1979-10-31	1980-11-25	Merck & Co., Inc.	Cyclic hexapeptide somatostatin analogs
NZ195303A (en) *	1979-10-31	1984-10-19	Merck & Co Inc	Cyclic hexapeptide somatostatin analogues,and pharmaceutical compositions

1981
- 1981-04-13 US US06/254,010 patent/US4360516A/en not_active Expired - Fee Related
1982
- 1982-04-06 EP EP82102924A patent/EP0063308B1/en not_active Expired
- 1982-04-06 AT AT82102924T patent/ATE14439T1/de not_active IP Right Cessation
- 1982-04-06 DE DE8282102924T patent/DE3264861D1/de not_active Expired
- 1982-04-07 DK DK159382A patent/DK159382A/da not_active Application Discontinuation
- 1982-04-07 GR GR67845A patent/GR75544B/el unknown
- 1982-04-07 PT PT74720A patent/PT74720B/pt unknown
- 1982-04-08 ES ES511335A patent/ES511335A0/es active Granted
- 1982-04-10 JP JP57059001A patent/JPS57179142A/ja active Granted

Also Published As

Publication number	Publication date
ES8304068A1 (es)	1983-02-16
DE3264861D1 (en)	1985-08-29
EP0063308A1 (en)	1982-10-27
JPS57179142A (en)	1982-11-04
PT74720A (en)	1982-05-01
DK159382A (da)	1982-10-14
US4360516A (en)	1982-11-23
GR75544B (pt)	1984-07-27
JPH0360839B2 (pt)	1991-09-17
ATE14439T1 (de)	1985-08-15
EP0063308B1 (en)	1985-07-24
ES511335A0 (es)	1983-02-16

Publication	Publication Date	Title
PT74720A (en)	1982-05-01	Process for preparing modified d-retro cyclic hexapeptide somatostatin analogs
RO92607A (ro)	1987-11-30	Procedeu pentru prepararea unor derivati de dihidropiridazinona
ES8206474A1 (es)	1982-08-16	Un procedimiento para la obtencion de un derivado acilado sustituido de acido octahidro-1h-indol-2-carboxilico
IL80216A0 (en)	1987-01-30	3-vinyl-and 3-ethinyl-beta-carboline derivatives,processes for the preparation thereof and pharmaceutical compositions containing the same
FI870090A0 (fi)	1987-01-12	Laongkedjade alkylresorcinolfosfiter.
CA1273641C (en)	1990-09-04	ALCENIC DERIVATIVES OF L-AMINOCARBOXYLIC ACIDS
DK165247C (da)	1993-04-26	2,3,4,5-substituerede 1,6-naphthyridinderivater, deres fremstilling samt anvendelse af disse til fremstilling af laegemidler til bekaempelse af cardiale, cerebrale og perifere karlidelser, myocardial iskaemi, cerebral infarkt, lungethrombose, stenoser, arterioscleroser og hjerte-kredsloebslidelser og laegemiddel indeholdende disse derivater
DE69106386D1 (en)	1995-02-09	Oxysulfonylcarbamate.
DK149270C (da)	1986-08-25	Analogifremgangsmaade til fremstilling af beta-carbolin-3-carboxylsyrederivater
KR860009011A (ko)	1986-12-19	치환된 이속사졸 유도체의 제조방법
GB2015521A (en)	1979-09-12	Pyrrolidin-2-one derivatives
KR830010101A (ko)	1983-12-26	티에닐과 벤조티에닐-t-부틸아미노페녹시프로파놀의 제조방법
KR840004105A (ko)	1984-10-06	N,n- 치환된 아졸 카복스 아미드 유도체의 제조방법
DK210387D0 (da)	1987-04-24	Heterocykliske forbindelser og fremgangsmaade til deres fremstilling samt farmaceutiske midler indeholdende disse
KR870006836A (ko)	1987-08-13	브라시노 라이드 유사체의 제조방법
KR870006045A (ko)	1987-07-08	8α-아실아미노에르고린의 제법 및 그 약학 조성물
ES8104218A1 (es)	1981-04-16	Un procedimiento para la preparacion de una sal de un acido alquilen-bis-ditiocarbamico
KR830007509A (ko)	1983-10-21	아미노산 유도체의 제조방법