HUP0401535A2 - Szomatosztatin antagonisták és alkalmazásuk - Google Patents

Szomatosztatin antagonisták és alkalmazásuk

Info

Publication number
HUP0401535A2
HUP0401535A2 HU0401535A HUP0401535A HUP0401535A2 HU P0401535 A2 HUP0401535 A2 HU P0401535A2 HU 0401535 A HU0401535 A HU 0401535A HU P0401535 A HUP0401535 A HU P0401535A HU P0401535 A2 HUP0401535 A2 HU P0401535A2
Authority
HU
Hungary
Prior art keywords
optionally substituted
alkyl
amino acid
aromatic
bzl
Prior art date
Application number
HU0401535A
Other languages
English (en)
Inventor
David H. Coy
William A. Murphy
Walajapet G. Rajeswaran
Original Assignee
The Administrators Of The Tulane Educational Fund
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 The Administrators Of The Tulane Educational Fund filed Critical The Administrators Of The Tulane Educational Fund
Publication of HUP0401535A2 publication Critical patent/HUP0401535A2/hu
Publication of HUP0401535A3 publication Critical patent/HUP0401535A3/hu

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/31—Somatostatins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic 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
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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

Abstract

A találmány az (I) általános képletű szomatosztatin antagonistákrairányul, melyben A1 jelentése szabadon megválaszthatóan szubsztituáltaromás a-aminosav; A2 jelentése szabadon megválaszthatóanszubsztituált aromás a-aminosav; A3 jelentése Dab, Dap, Lys vagy Orn;A4 jelentése b-hidroxivalin, Ser, Hser, vagy Thr; A5 jelentéseszabadon megválaszthatóan szubsztituált D- vagy L-aromás a-aminosav;és Y1 jelentése OH, NH2 vagy NHR1, ahol Rl jelentése (C1-6)alkil; ahola szóban forgó szabadon megválasztható aromás a-aminosavak mindegyikeszabadon megválasztott egy vagy több szubsztituenssel helyettesíthető,amelyeket egymástól függetlenül a következők közül választanak ki:halogén, NO2, OH, CN, (C1-6)alkil, (C2-6)alkenil, (C2-6)alkinil, (C1-6)alkoxi, Bzl, O-Bzl, és NR9R10, ahol R9 és Rl0 jelentése egymástólfüggetlenül H, O, vagy (C1-6)alkil; és ahol mindegyik amid peptidkötésamin nitrogén és az (I) általános képletű vegyületben A1aminocsoportja szabadon megválaszthatóan metilcsoporttalszubsztituálható, feltéve, hogy legalább egy a szóban forgómetilcsoport szerepel; vagy ezek gyógyszerészetileg elfogadható sói. Ó
HU0401535A 2001-03-08 2002-03-05 Somatostatin antagonists and their use HUP0401535A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27430801P 2001-03-08 2001-03-08
PCT/US2002/006676 WO2002072602A2 (en) 2001-03-08 2002-03-05 Somatostatin antagonists

Publications (2)

Publication Number Publication Date
HUP0401535A2 true HUP0401535A2 (hu) 2004-12-28
HUP0401535A3 HUP0401535A3 (en) 2009-07-28

Family

ID=23047655

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0401535A HUP0401535A3 (en) 2001-03-08 2002-03-05 Somatostatin antagonists and their use

Country Status (16)

Country Link
US (3) US7378488B2 (hu)
EP (1) EP1372688B1 (hu)
JP (3) JP4204322B2 (hu)
AR (1) AR035942A1 (hu)
AT (1) ATE394114T1 (hu)
AU (1) AU2002258465B2 (hu)
CA (1) CA2439498A1 (hu)
CZ (1) CZ299362B6 (hu)
DE (1) DE60226419D1 (hu)
DK (1) DK1372688T3 (hu)
ES (1) ES2306766T3 (hu)
HU (1) HUP0401535A3 (hu)
NO (1) NO20033911L (hu)
PL (1) PL362838A1 (hu)
RU (2) RU2263678C2 (hu)
WO (1) WO2002072602A2 (hu)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL366327A1 (en) * 2000-10-20 2005-01-24 The Administrators Of The Tulane Educational Fund Urotensin-ii agonists and antagonists
CZ299362B6 (cs) 2001-03-08 2008-07-02 The Administrators Of The Tulane Educational Fund Antagonisté somatostatinu
AU2002256105B2 (en) * 2001-04-09 2006-04-06 The Administrators Of The Tulane Educational Fund Somatostatin agonists
EP1522311A1 (fr) * 2003-10-10 2005-04-13 Institut National De La Sante Et De La Recherche Medicale (Inserm) Utilisation de la somatostine ou d'un de ses analogues pour préparer un médicament destiné à réguler la réserve folliculaire ovarienne chez la femme non ménopausée
US8017575B2 (en) * 2004-12-15 2011-09-13 Wilfred Wayne Lautt Treatment of insulin resistance by modulating somatostatin using somatostatin receptor antagonists
US8691761B2 (en) * 2006-10-16 2014-04-08 Jean E. F. Rivier Somatostatin receptor 2 antagonists
ES2526292T3 (es) 2006-10-16 2015-01-09 The Salk Institute For Biological Studies Antagonistas de la somatostatina selectivos para receptor (SSTR2)
EP2168983A1 (fr) * 2008-09-30 2010-03-31 Ipsen Pharma Nouveaux composés octapeptidiques et leur utilisation thérapeutique
SG10201400650QA (en) * 2008-10-29 2014-05-29 Kaneka Corp Method For Producing L-Amino Acid
EP2399931A1 (fr) * 2010-06-22 2011-12-28 Ipsen Pharma S.A.S. Nouveaux composés octapeptidiques et leur utilisation thérapeutique
EP3414259A4 (en) * 2016-02-09 2019-10-16 CDRD Ventures Inc. SOMATOSTATIN RECEPTOR ANTAGONIST COMPOUNDS AND METHOD FOR USE THEREOF
WO2021111503A1 (ja) * 2019-12-02 2021-06-10 花王株式会社 光吸収層及びその製造方法、分散液、光電変換素子、並びに太陽電池

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE43335T1 (de) * 1980-02-14 1989-06-15 Sandoz Ag Peptide die einen (1s,2r,3r)- oder (1r,2s,3s)-1nitrilo-1-carbonyl-3-methyl-2-oxyheptan oder hept-5-en-rest enthalten brauchbar in totaler synsthese von cyclosporinen, und verfahren zu ihrer herstellung.
JPS63146850A (ja) 1986-11-12 1988-06-18 メルク　エンド　カムパニー　インコーポレーテツド フエニルアラニル−ヒスチジン代用成分を有するレニン阻害剤
EP0278158A3 (en) 1986-11-12 1990-05-23 Merck & Co. Inc. Renin inhibitors containing phenylalanyl-histidine replacements
EP0273696A2 (en) 1987-01-02 1988-07-06 Merck & Co. Inc. Renin inhibitors containing histidine replacements
CH679045A5 (hu) 1987-06-29 1991-12-13 Sandoz Ag
JPS6426599U (hu) 1987-08-10 1989-02-15
ES2108684T3 (es) 1988-02-10 1998-01-01 Tap Pharmaceuticals Inc Analogo de la hormona de liberacion de la hormona luteinizante (lhrh).
CA2046594A1 (en) * 1989-12-08 1991-06-09 David H. Coy Octapeptide analogs of somatostatin having threonine at the sixth position
US7223833B1 (en) * 1991-05-24 2007-05-29 Isis Pharmaceuticals, Inc. Peptide nucleic acid conjugates
JPH06509075A (ja) 1991-07-01 1994-10-13 ユニヴァーシティ　テクノロジーズ　インターナショナル　インコーポレイテッド ＧｎＲＨ及び他の生物学的に活性なリガンドの非感度低下性類縁体
JP3480848B2 (ja) * 1992-06-19 2003-12-22 タカラバイオ株式会社 環状ペプチドの合成方法
US5569741A (en) * 1992-07-27 1996-10-29 Biomeasure, Inc. Cyclic octapeptide neuromedin B receptor antagonists
RO117259B1 (ro) * 1993-08-09 2001-12-28 Biomeasure Inc. Derivaţi peptidici, terapeutici
GB9402767D0 (en) 1994-02-14 1994-04-06 Sandoz Ltd Improvements in or relating to organic compounds
US5696230A (en) * 1994-08-31 1997-12-09 The Board Of Regents Of The University Of Nebraska High-affinity response-selective C-terminal analogs of C5a anaphylatoxin
US5750499A (en) * 1995-10-18 1998-05-12 The Salk Institute For Biological Studies Receptor-selective somatostatin analogs
US5846934A (en) * 1996-02-20 1998-12-08 American Cyanamid Company Pure somatostatin antagonist and methods of use thereof
US6355613B1 (en) * 1996-07-31 2002-03-12 Peptor Limited Conformationally constrained backbone cyclized somatostatin analogs
WO1998008528A1 (en) 1996-08-30 1998-03-05 Biomeasure Incorporated Method of inhibiting fibrosis with a somatostatin agonist
AU4133997A (en) * 1996-09-12 1998-04-02 Yarom Cohen Pharmaceutical composition for the treatment of syndrome x of reaven
JP4124820B2 (ja) 1996-12-04 2008-07-23 ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス ソマトスタチン類似体
US6887470B1 (en) * 1999-09-10 2005-05-03 Conjuchem, Inc. Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
ATE430162T1 (de) * 2001-03-06 2009-05-15 Il Consorzio Ferrara Richerche Verfahren zur modulation der proliferation von schilddrüsenkrebszellen
CZ299362B6 (cs) 2001-03-08 2008-07-02 The Administrators Of The Tulane Educational Fund Antagonisté somatostatinu
AU2002256105B2 (en) 2001-04-09 2006-04-06 The Administrators Of The Tulane Educational Fund Somatostatin agonists

Also Published As

Publication number Publication date
US20080020970A1 (en) 2008-01-24
ATE394114T1 (de) 2008-05-15
HUP0401535A3 (en) 2009-07-28
AU2002258465B2 (en) 2006-01-19
NO20033911D0 (no) 2003-09-04
RU2328504C2 (ru) 2008-07-10
RU2005117614A (ru) 2006-11-20
CA2439498A1 (en) 2002-09-19
EP1372688A4 (en) 2006-06-14
US7408024B2 (en) 2008-08-05
JP4204322B2 (ja) 2009-01-07
DK1372688T3 (da) 2008-08-25
WO2002072602A2 (en) 2002-09-19
DE60226419D1 (de) 2008-06-19
JP2008255120A (ja) 2008-10-23
EP1372688A2 (en) 2004-01-02
NO20033911L (no) 2003-10-29
CZ20032281A3 (cs) 2004-01-14
RU2263678C2 (ru) 2005-11-10
EP1372688B1 (en) 2008-05-07
US7378488B2 (en) 2008-05-27
AR035942A1 (es) 2004-07-28
CZ299362B6 (cs) 2008-07-02
JP2006342171A (ja) 2006-12-21
JP2004532824A (ja) 2004-10-28
PL362838A1 (en) 2004-11-02
US20040181032A1 (en) 2004-09-16
ES2306766T3 (es) 2008-11-16
WO2002072602A3 (en) 2003-03-20
RU2003129807A (ru) 2005-03-20
US20080171853A1 (en) 2008-07-17

Similar Documents

Publication Publication Date Title
HUP0303727A2 (hu) Szomatosztatin agonisták és ezek alkalmazása
HUP0401535A2 (hu) Szomatosztatin antagonisták és alkalmazásuk
EE04911B1 (et) Ühend ja farmatseutiline kompositsioon proteaasi inhibiitoritena, nende kasutamine ning meetod selle ühendi valmistamiseks
ZA967379B (en) Meta-guanidine, urea, thiourea or azacyclic amino benzoic acid compounds and derivatives thereof.
TR200200252T2 (tr) Şimerik polipeptidler, bunların üretimi için yöntem ve kullanımı
DE3784799D1 (de) Malonsaeurederivate und ihre synthesemethoden.
NO20052307L (no) Blandinger og fremgangsmater for a modifisere toksiske effekter av proteinlignende forbindelser.
BG104740A (en) Meta-azacyclic amino benzoic acid compounds and derivatives thereof being integrin antagonists
DE60235396D1 (de) 3-amido-1,2-benzisoxazolderivate, herstellungsverfahren und deren verwendung
GEP20074123B (en) Amino acids with affinity for the alpha−2−delta−protein
MA29416B1 (fr) Inhibiteurs d'age
ECSP11010962A (es) Nevos compuestos heterocíclicos nitrogenados, su preparación y su utilización como medicamentos antibacterianos
BR0317487A (pt) O r-isÈmero de compostos de aminoácido beta como derivados de antagonistas de receptores de integrina
HUP0201083A2 (hu) Új atorvastatinsók és az azokat tartalmazó gyógyszerkészítmények
HUP9800970A2 (hu) Eljárás neurogén és nem neurogén gyulladásgátló, valamint fájdalomcsillapító hatású heptapeptid szomatosztatinszármazékokat és peptidomimetikumokat tartalmazó gyógyászati készítmények előállítására
MX9702275A (es) Compuestos polipectidicos que contienen d-2 alquiltriptofano capaces de promover la liberacion de hormona del crecimiento.
TW200633955A (en) Manufacture process of organic compounds
TW200635880A (en) Manufacture process of organic compounds
DK1180094T3 (da) Kondenserede polycykliske aminosyrer som farmaceutiske midler
RU2006106721A (ru) Получение пептидов соматостатина
GEP20074100B (en) Novel amino acid derivatives, method for production thereof and pharmaceutical compositions comprising the same
EA200300900A1 (ru) Замещенные амины (варианты), способ их получения и их применение в качестве ингибиторов транспорта глицина (варианты), композиция (варианты), промежуточный иодид и способ его получения, способ лечения пациента (варианты)
PL1716147T3 (pl) Pochodne diazaspiropiperydyny jako inhibitory transportera 1 glicyny i transportera 2 glicyny
TW200509941A (en) Pharmaceutical solution composition
AU2003245979A1 (en) Amides of cyclic amino acids used as pde 4 inhibitors

Legal Events

Date Code Title Description
FA9A Lapse of provisional patent protection due to relinquishment or protection considered relinquished