AR024463A1 - SOMATOSTATINE AGONISTS - Google Patents
SOMATOSTATINE AGONISTSInfo
- Publication number
- AR024463A1 AR024463A1 ARP000103155A ARP000103155A AR024463A1 AR 024463 A1 AR024463 A1 AR 024463A1 AR P000103155 A ARP000103155 A AR P000103155A AR P000103155 A ARP000103155 A AR P000103155A AR 024463 A1 AR024463 A1 AR 024463A1
- Authority
- AR
- Argentina
- Prior art keywords
- trp
- cys
- group
- tyr
- alkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
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- 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
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P3/06—Antihyperlipidemics
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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- 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
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- 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
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
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- 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
- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing 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)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Oncology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Obesity (AREA)
- Virology (AREA)
- Gastroenterology & Hepatology (AREA)
- AIDS & HIV (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Neurology (AREA)
- Dermatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
Abstract
Se refiere a péptidos cíclicos de formula (1): X-A1-ciclo(D-Cys-A3-A4-Lys-A6-A7)-A8-Y o su sal farmacéuticamente aceptable, en donde: X es H, formula (2) oformula (3); A1 y A3 son cada uno independientemente el isomero D- o L- de un aminoácidoselecc ionado entre el grupo que consiste en Phe, Tyr, Tyr(I), Trp,3-Pal, 4-Pal, Cpa y NaI; A4 es L-Trp, D-Trp, L-beta-metil-Trp o D-beta-metil-Trp; A6 es -NH-(CHR1)n-CO-, donde n es 2, 3 o 4; A7 es L- o D-Cys; A8 es elisomero D o L de un aminoácidoselecci onado entre el grupo que consiste en Phe, Tyr, Tyr(I), Trp, NaI, Cpa, Val, Leu, IIe, Ser y Thr; Y es NR2R3 donde R2 y R3son cada uno independientemente H o alquilo C1-5; R1 se selecciona entre el grupo que consiste en H, alquilo C1-4 y-CH2-arilo; en donde dicho arilo es unaporcion optativamente sustituida seleccionada entre el grupo que consiste en fenilo, 1-naftilo y 2-naftilo, en donde dicha porcion optativamente sustituida esoptativamente sustituida con uno o más sustituyentescada uno selec cionado independientemente entre el grupo que consiste en alquiloC1-6, alquenilo C2-6,alquinilo C2-6, arilo, arilalquilo C1-6, alcoxi C1-6, -N(R4R5), -COOH, -CON(R4R5), halo, -OH, -CN, y -NO2; R4 y R5 cada uno es, independientementepara cadaaparicio n, H o alquilo C1-3; donde el Cys de A2 está unido al Cys de A7 por un enlace di-sulfuro formado de los grupos tiol de cada Cys; composicionesfarmacéuticas que comprenden dichos péptidos y el uso de las mismas como un agonista delos subtipos del rec eptor de somatostatina. Los péptidos de la presentese unen selectivamente al tipo 5 del receptor de los subtipos de somatostatina y producen un efecto agonista de los receptores de subtipo de somatostatina alas cuales se unenlos péptidos.Refers to cyclic peptides of formula (1): X-A1-cycle (D-Cys-A3-A4-Lys-A6-A7) -A8-Y or its pharmaceutically acceptable salt, wherein: X is H, formula ( 2) oformula (3); A1 and A3 are each independently the D- or L- isomer of an amino acid selected from the group consisting of Phe, Tyr, Tyr (I), Trp, 3-Pal, 4-Pal, Cpa and NaI; A4 is L-Trp, D-Trp, L-beta-methyl-Trp or D-beta-methyl-Trp; A6 is -NH- (CHR1) n-CO-, where n is 2, 3 or 4; A7 is L- or D-Cys; A8 is the D or L elisomer of an amino acid selected from the group consisting of Phe, Tyr, Tyr (I), Trp, NaI, Cpa, Val, Leu, IIe, Ser and Thr; Y is NR2R3 where R2 and R3 are each independently H or C1-5 alkyl; R1 is selected from the group consisting of H, C1-4 alkyl and -CH2-aryl; wherein said aryl is an optionally substituted portion selected from the group consisting of phenyl, 1-naphthyl and 2-naphthyl, wherein said optionally substituted portion is optionally substituted with one or more substituents each one independently selected from the group consisting of C1-alkyl. 6, C2-6 alkenyl, C2-6 alkynyl, aryl, C1-6 arylalkyl, C1-6 alkoxy, -N (R4R5), -COOH, -CON (R4R5), halo, -OH, -CN, and -NO2 ; R4 and R5 each is, independently for each space n, H or C1-3 alkyl; where the Cys of A2 is linked to the Cys of A7 by a di-sulfide bond formed from the thiol groups of each Cys; Pharmaceutical compositions comprising said peptides and their use as an agonist of the subtypes of the somatostatin receptor. The peptides of the present selectively bind to type 5 receptor somatostatin subtypes and produce an agonist effect of somatostatin subtype receptors to which peptides bind.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14102899P | 1999-06-25 | 1999-06-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR024463A1 true AR024463A1 (en) | 2002-10-02 |
Family
ID=22493842
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP000103155A AR024463A1 (en) | 1999-06-25 | 2000-06-23 | SOMATOSTATINE AGONISTS |
Country Status (14)
Country | Link |
---|---|
EP (1) | EP1189942A1 (en) |
JP (1) | JP4041311B2 (en) |
CN (1) | CN1367792A (en) |
AR (1) | AR024463A1 (en) |
AU (1) | AU770958B2 (en) |
BR (1) | BR0011919A (en) |
CA (1) | CA2377265A1 (en) |
CZ (1) | CZ20014534A3 (en) |
HU (1) | HUP0201696A3 (en) |
IL (1) | IL146941A0 (en) |
MX (1) | MXPA01013127A (en) |
PL (1) | PL352763A1 (en) |
RU (1) | RU2263677C2 (en) |
WO (1) | WO2001000676A1 (en) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1813625B1 (en) * | 2001-03-06 | 2009-04-29 | Il Consorzio Ferrara Richerche | Method of modulating the profileration of medullary thyroid carcinoma cells |
US7189856B2 (en) | 2001-12-28 | 2007-03-13 | Gideon Shapiro | Non-peptide somatostatin receptor ligands |
EP2527008A3 (en) * | 2007-04-30 | 2013-01-16 | Technion Research & Development Foundation Ltd. | Anticancerous polymeric agents |
US8470770B2 (en) | 2007-04-30 | 2013-06-25 | Technion Research & Development Foundation Ltd. | Antimicrobial agents |
EA021897B1 (en) * | 2009-11-23 | 2015-09-30 | Палатин Текнолоджиз, Инк. | Melanocortin-1 receptor-specific cyclic peptides |
WO2011151782A1 (en) | 2010-06-02 | 2011-12-08 | Preglem Sa | A role for somatostatin to modulate initiation of follicular growth in the human ovary |
US10039813B2 (en) | 2012-02-07 | 2018-08-07 | Massachusetts Institute Of Technology | Use of antagonists of ghrelin or ghrelin receptor to prevent or treat stress-sensitive psychiatric illness |
US9724396B2 (en) | 2013-03-15 | 2017-08-08 | Massachusetts Institute Of Technology | Use of antagonists of growth hormone or growth hormone receptor to prevent or treat stress-sensitive psychiatric illness |
WO2016138099A1 (en) | 2015-02-24 | 2016-09-01 | Massachusetts Institute Of Technology | Use of ghrelin or functional ghrelin receptor agonists to prevent and treat stress-sensitive psychiatric illness |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0083305B1 (en) * | 1981-12-24 | 1985-07-10 | Ciba-Geigy Ag | Cyclic octapeptides and pharmaceutical compositions thereof, and processes for their production and use |
HU207104B (en) * | 1991-01-25 | 1993-03-01 | Biosignal Kutato Fejlesztoe Kf | Process for producing new somatostatin analogs inhibiting tumour growth and pharmaceutical compositions comprising such compounds |
ATE284413T1 (en) * | 1993-08-09 | 2004-12-15 | Sod Conseils Rech Applic | THERAPEUTIC PEPTIDE DERIVATIVES |
RU2179172C2 (en) * | 1996-12-04 | 2002-02-10 | Сосьете Де Консей Де Решерш Э Д'Аппликасьон Сьентифик С.А. (С.К.Р.А.С.) | Somatostatin receptor antagonists |
ATE234113T1 (en) * | 1997-05-01 | 2003-03-15 | Cedars Sinai Medical Center | METHOD FOR TREATING HYPERPROLACTINEMIA AND PROLACTINOMAS |
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 |
PT980253E (en) * | 1997-05-13 | 2004-08-31 | Conseils De Rec Appl Scient S | SOMATOSTATIN AND SOMATOSTATIN AGONISTS TO TREAT INSULIN INSULIN AND X SYNDROME |
US7026289B2 (en) * | 1997-05-13 | 2006-04-11 | Societe De Conseils De Recherches Et D'applications Scientifiques, Sas | Method and compositions for treating hyperlipidemia and other conditions |
-
2000
- 2000-06-23 AR ARP000103155A patent/AR024463A1/en unknown
- 2000-06-23 CA CA002377265A patent/CA2377265A1/en not_active Abandoned
- 2000-06-23 EP EP00948520A patent/EP1189942A1/en not_active Ceased
- 2000-06-23 MX MXPA01013127A patent/MXPA01013127A/en unknown
- 2000-06-23 RU RU2002101732/04A patent/RU2263677C2/en not_active IP Right Cessation
- 2000-06-23 WO PCT/US2000/017401 patent/WO2001000676A1/en active IP Right Grant
- 2000-06-23 IL IL14694100A patent/IL146941A0/en unknown
- 2000-06-23 CZ CZ20014534A patent/CZ20014534A3/en unknown
- 2000-06-23 AU AU62000/00A patent/AU770958B2/en not_active Ceased
- 2000-06-23 PL PL00352763A patent/PL352763A1/en not_active Application Discontinuation
- 2000-06-23 CN CN00811189A patent/CN1367792A/en active Pending
- 2000-06-23 BR BR0011919-9A patent/BR0011919A/en not_active Application Discontinuation
- 2000-06-23 HU HU0201696A patent/HUP0201696A3/en unknown
- 2000-06-23 JP JP2001506685A patent/JP4041311B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
RU2263677C2 (en) | 2005-11-10 |
BR0011919A (en) | 2002-03-19 |
CN1367792A (en) | 2002-09-04 |
HUP0201696A3 (en) | 2002-10-28 |
WO2001000676A1 (en) | 2001-01-04 |
MXPA01013127A (en) | 2002-11-04 |
JP4041311B2 (en) | 2008-01-30 |
CA2377265A1 (en) | 2001-01-04 |
HUP0201696A2 (en) | 2002-09-28 |
IL146941A0 (en) | 2002-08-14 |
CZ20014534A3 (en) | 2002-06-12 |
EP1189942A1 (en) | 2002-03-27 |
AU770958B2 (en) | 2004-03-11 |
AU6200000A (en) | 2001-01-31 |
JP2003503369A (en) | 2003-01-28 |
PL352763A1 (en) | 2003-09-08 |
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