JP2000516592A - コンフォメーション的に固定された主鎖環化ソマトスタチン類似体 - Google Patents
コンフォメーション的に固定された主鎖環化ソマトスタチン類似体Info
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- JP2000516592A JP2000516592A JP10508666A JP50866698A JP2000516592A JP 2000516592 A JP2000516592 A JP 2000516592A JP 10508666 A JP10508666 A JP 10508666A JP 50866698 A JP50866698 A JP 50866698A JP 2000516592 A JP2000516592 A JP 2000516592A
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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
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
- C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
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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
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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
- A61P5/00—Drugs for disorders of the endocrine system
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
-
- 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
-
- 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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- G—PHYSICS
- G01—MEASURING; TESTING
- G01R—MEASURING ELECTRIC VARIABLES; MEASURING MAGNETIC VARIABLES
- G01R31/00—Arrangements for testing electric properties; Arrangements for locating electric faults; Arrangements for electrical testing characterised by what is being tested not provided for elsewhere
- G01R31/28—Testing of electronic circuits, e.g. by signal tracer
- G01R31/317—Testing of digital circuits
- G01R31/3181—Functional testing
- G01R31/3185—Reconfiguring for testing, e.g. LSSD, partitioning
- G01R31/318533—Reconfiguring for testing, e.g. LSSD, partitioning using scanning techniques, e.g. LSSD, Boundary Scan, JTAG
- G01R31/318541—Scan latches or cell details
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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
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- 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
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Endocrinology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- General Engineering & Computer Science (AREA)
- Physics & Mathematics (AREA)
- General Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. 一般式(I): [式中、a〜cはそれぞれが独立に1〜8の整数または0を表し;(AA)はアミノ酸 残基を表し、その際、各鎖中のアミノ酸残基は同じでも異なっていてもよく;Q はHまたはアシル基を表し;Eはヒドロキシル基、カルボキシル保護基またはア ミノ基を表し、また、末端カルボキシル基はCH2-OHに還元することができ;R1お よびR2はそれぞれ、特定の保護基と結合していてもよいアミノ酸側鎖を表し;そ して線は式:-(CH2)x-M-(CH2)y-の架橋基を表し;ここでMはアミド、チオエー テル、チオエステルおよびジスルフィドよりなる群から選ばれ;xおよびyはそ れぞれが独立に1〜10の整数を表す] を有する、主鎖環化ソマトスタチン類似体。 2. 一般式(Va): [式中、mおよびnは1〜5であり;Xはカルボキシ末端アミドまたはカルボキ シ末端アルコールを表し;R5は存在しないかまたはGly、(D)-もしくは(L)-Ala、P he、Nalおよびβ-Asp(Ind)であり;R6およびR11は独立にGly-または(D)-もしく は(L)-Pheであり;R7はPheまたはTyrであり;R10は存在しないかまたはGly、Abu 、ThrもしくはValであり;R12は存在しないかまたはVal、ThrもしくはNalであり ;Y2はアミド、チオエーテル、チ オエステルおよびジスルフィドよりなる群から選ばれる] を有する、請求項1に記載の主鎖環化ソマトスタチン類似体。 3. 一般式(Vb): [式中、mおよびnは1〜5であり;Xはカルボシキ末端アミドまたはカルボキ シ末端アルコールを表し;R6およびR11は独立にGlyまたは(D)-もしくは(L)-Phe であり;R7はPheまたはTyrであり;R10は存在しないかまたはGly、Abu、Thrも しくはValであり;Y2はアミド、チオエーテル、チオエステルおよびジスルフィ ドよりなる群から選ばれる] を有する、請求項2に記載の主鎖環化ソマトスタチン類似体。 4. 構造: シクロ[NPhe-Tyr-(D)Trp-Lys-Val-NPhe]-Thr-X (式中、Xはカルボキシ末端酸、カルボキシ末端アミド、カルボキシ末端エステ ルまたはカルボキシ末端アルコールを表す) を有する、請求項3に記載の主鎖環化ソマトスタチン類似体。 5. 構造: (式中、Xはカルボキシ末端酸、カルボキシ末端アミド、カルボキシ末端エステ ルまたはカルボキシ末端アルコールを表す) を有する、請求項4に記載の主鎖環化ソマトスタチン類似体。 6. 構造: シクロ[NPhe-Phe-(D)Trp-Lys-Thr-NPhe]-Val-X (式中、Xはカルボキシ末端酸、カルボキシ末端アミド、カルボキシ末端エステ ルまたはカルボキシ末端アルコールを表す) を有する、請求項3に記載の主鎖環化ソマトスタチン類似体。 7. 構造: (式中、Xはカルボキシ末端酸、カルボキシ末端アミド、カルボキシ末端エステ ルまたはカルボキシ末端アルコールを表す) を有する、請求項6に記載の主鎖環化ソマトスタチン類似体。 8. 一般式(XI): [式中、iおよびjは独立に1〜5であり;Xはカルボキシ末端アミドまたはカ ルボキシ末端アルコールを表し;R5は(D)Pheもしくは(L)Phe、AlaまたはLysであ り;R6は存在しないかまたはPheであり;R7はTyrまたはPheであり;R10は存在し ないかまたはThr、Val、SerまたはAbuであり;R11はPhe、GlyまたはAlaであり; R12はTrp、Thr、Val、2-Nalまたは(D)2-Nalであり;Y1はアミド、チオエーテル 、チオエステルおよびジスルフィドよりなる群から選ばれる] を有する、請求項1に記載の主鎖環化ソマトスタチン類似体。 9. 一般式(XII): [式中、iおよびjは独立に1〜5であり;Xはカルボキシ末端アミドまたはカ ルボキシ末端アルコールを表し;R5はPhe、(L)2-ナフチルアラニンもしくは(D)2 -ナフチルアラニンであり;R6はPhe、GlyまたはAlaであり;R7は(D)Phe、pCl(D) Phe、pNH2Pheまたは(D)Tyrであり;R10は(D)Thr、(D)Val、(D)Ala、(D)Leuまた は(D)Gluであり;R11はPhe、GlyまたはAlaであり;R12は存在しないかまたはThr もしくはValであり;Y1はアミド、チオエーテル、チオエステルおよびジスルフ ィドよりなる群から選ばれる] を有する、請求項1に記載の主鎖環化ソマトスタチン類似体。 10.一般式(XIII): [式中、iおよびjは独立に1〜5であり;Xはカルボキシ末端アミドまたはカ ルボキシ末端アルコールを表し;R5は存在しないかまたは(D)Pheもしくは2-Nal であり;R6はPhe、Gly、LysまたはAlaであり;R7は(D)Phe、pCl(D)Phe、pNH2Phe または(D)Tyrであり;R10は(D)Thr、(D)Val、(D)Ala、(D)Leuまたは(D)Gluであ り;R11はPhe、GlyまたはAlaであり;R12はThr、Val、Ala、β-Ala、(L)2-ナフ チルアラニンまたは(D)2-ナフチルアラニンであり;Y1はアミド、チオエーテル 、チオエステルおよびジスルフィ-ドよりなる群から選ばれる] を有する、請求項1に記載の主鎖環化ソマトスタチン類似体。 11.一般式(XIV): [式中、iおよびjは独立に1〜5であり;Xはカルボキシ末端アミドまたはカ ルボキシ末端アルコールを表し;R1はAlaまたば(D)2-ナフチルアラニンであり;R4 はLysまたはArgであり;R5は(L)Asnまたは(D)Asnであり;R7はPhe、Gly、Alaま たはLysであり;Y1はアミド、チオエーテル、チオエステルおよびジスルフィド よりなる群から選ばれる] を有する、請求項1に記載の主鎖環化ソマトスタチン類似体。 12.請求項1〜11のいずれか一項に記載のソマトスタチン類似体および製剤学的 に許容される担体または希釈剤を含んでなる医薬組成物。 13.前記ソマトスタチン類似体が、 シクロ[NPhe-Tyr-(D)Trp-Lys-Val-NPhe]-Thr-X (式中、Xはカルボキシ末端酸、カルボキシ末端アミド、カルボキシ末端エステ ルまたはカルボキシ末端アルコールを表す) である、請求項12に記載の医薬組成物。 14.単位剤形である請求項13に記載の医薬組成物。 15.前記ソマトスタチン類似体が、 シクロ[NPhe-Phe-(D)Trp-Lys-Thr-NPhe]-Val-X (式中、Xはカルボキシ末端酸、カルボキシ末端アミド、カルボキシ末端エステ ルまたはカルボキシ末端アルコールを表す) である請求項12に記載の医薬組成物。 16.単位剤形である請求項15に記載の医薬組成物。 17.内分泌障害、新生物または代謝異常を治療する方法であって、治療上有効な 量の請求項1〜11のいずれか一項に記載のソマトスタチン類似体を、治療を必要 とする個体に投与することを含んでなる前記方法。 18.内分泌障害、新生物または代謝異常を治療するための薬剤の製造における、 請求項1〜11のいずれか一項に記載のソマトスタチン類似体の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/690,090 | 1996-07-31 | ||
US08/690,090 US5770687A (en) | 1995-06-07 | 1996-07-31 | Comformationally constrained backbone cyclized somatostatin analogs |
PCT/IL1997/000261 WO1998004583A1 (en) | 1996-07-31 | 1997-07-30 | Conformationally constrained backbone cyclized somatostatin analogs |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2000516592A true JP2000516592A (ja) | 2000-12-12 |
JP2000516592A5 JP2000516592A5 (ja) | 2005-02-10 |
JP4018752B2 JP4018752B2 (ja) | 2007-12-05 |
Family
ID=24771043
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50866698A Expired - Fee Related JP4018752B2 (ja) | 1996-07-31 | 1997-07-30 | コンフォメーション的に固定された主鎖環化ソマトスタチン類似体 |
Country Status (13)
Country | Link |
---|---|
US (1) | US5770687A (ja) |
EP (1) | EP0920446B1 (ja) |
JP (1) | JP4018752B2 (ja) |
KR (1) | KR100477710B1 (ja) |
CN (1) | CN1124282C (ja) |
AT (1) | ATE363911T1 (ja) |
AU (1) | AU711100B2 (ja) |
BR (1) | BR9710636A (ja) |
CA (1) | CA2262778C (ja) |
DE (1) | DE69737787T2 (ja) |
IL (1) | IL128084A0 (ja) |
NZ (1) | NZ334046A (ja) |
WO (1) | WO1998004583A1 (ja) |
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WO2003028527A2 (en) | 2001-09-21 | 2003-04-10 | The Administrators Of The Tulane Educational Fund | Diagnostic or therapeutic somatostatin or bombesin analog conjugates and uses thereof |
NZ534719A (en) * | 2002-03-01 | 2008-02-29 | Univ Tulane | Conjugates of therapeutic or cytotoxic agents and biologically active peptides |
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IL150384A0 (en) * | 2002-06-24 | 2002-12-01 | Peptor Ltd | Radiolabelled somatostatin analogs backbone cyclized through metal complexation |
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WO2005018682A2 (en) * | 2003-08-20 | 2005-03-03 | The Regents Of The University Of California | Somatostatin analogs with inhibitory activity to growth hormone release |
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IL109943A (en) * | 1994-06-08 | 2006-08-01 | Develogen Israel Ltd | Conformationally constrained backbone cyclized peptide analogs |
-
1996
- 1996-07-31 US US08/690,090 patent/US5770687A/en not_active Expired - Lifetime
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1997
- 1997-07-30 AU AU36331/97A patent/AU711100B2/en not_active Ceased
- 1997-07-30 BR BR9710636-4A patent/BR9710636A/pt not_active Application Discontinuation
- 1997-07-30 IL IL12808497A patent/IL128084A0/xx unknown
- 1997-07-30 WO PCT/IL1997/000261 patent/WO1998004583A1/en active IP Right Grant
- 1997-07-30 CA CA002262778A patent/CA2262778C/en not_active Expired - Fee Related
- 1997-07-30 EP EP97932978A patent/EP0920446B1/en not_active Expired - Lifetime
- 1997-07-30 DE DE69737787T patent/DE69737787T2/de not_active Expired - Fee Related
- 1997-07-30 KR KR10-1999-7000727A patent/KR100477710B1/ko not_active IP Right Cessation
- 1997-07-30 JP JP50866698A patent/JP4018752B2/ja not_active Expired - Fee Related
- 1997-07-30 CN CN97198197A patent/CN1124282C/zh not_active Expired - Fee Related
- 1997-07-30 NZ NZ334046A patent/NZ334046A/en unknown
- 1997-07-30 AT AT97932978T patent/ATE363911T1/de not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
IL128084A0 (en) | 1999-11-30 |
NZ334046A (en) | 1999-10-28 |
DE69737787D1 (de) | 2007-07-19 |
DE69737787T2 (de) | 2008-03-06 |
AU3633197A (en) | 1998-02-20 |
EP0920446A4 (en) | 2004-06-02 |
AU711100B2 (en) | 1999-10-07 |
EP0920446B1 (en) | 2007-06-06 |
EP0920446A1 (en) | 1999-06-09 |
BR9710636A (pt) | 2000-01-11 |
CN1124282C (zh) | 2003-10-15 |
KR100477710B1 (ko) | 2005-03-18 |
CA2262778C (en) | 2006-10-10 |
JP4018752B2 (ja) | 2007-12-05 |
ATE363911T1 (de) | 2007-06-15 |
US5770687A (en) | 1998-06-23 |
KR20000029654A (ko) | 2000-05-25 |
CA2262778A1 (en) | 1998-02-05 |
WO1998004583A1 (en) | 1998-02-05 |
CN1231672A (zh) | 1999-10-13 |
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