KR970006312A - 개선된 내용성을 갖는 제약 활성의 β-아미노산 - Google Patents
개선된 내용성을 갖는 제약 활성의 β-아미노산 Download PDFInfo
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- KR970006312A KR970006312A KR1019960028961A KR19960028961A KR970006312A KR 970006312 A KR970006312 A KR 970006312A KR 1019960028961 A KR1019960028961 A KR 1019960028961A KR 19960028961 A KR19960028961 A KR 19960028961A KR 970006312 A KR970006312 A KR 970006312A
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- amino acid
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- cyclopentane
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
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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
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- 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
- A61P31/04—Antibacterial agents
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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
- A61P31/10—Antimycotics
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/46—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C229/48—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Communicable Diseases (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Medicinal Preparation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
본 발명은 α-아미노산 및 (또는) 그 유도체와 시클로펜탄-β-아미노산 및(또는) 그 유도체의 혼합물, 상기 α-아미노산과 시클로펜탄-β-아미노산의 디펩티드, 및 상기 혼합물과 디펩티드의 혼합물에 관한 것이다.
본 발명의 혼합물 및 디펩티드는 순수한 시클로펜탄-β-아미노산에 비해 온혈 동물 내에서 개선된 내용성을 갖고, 질병, 특히 진균중의 치료에 적합하다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
1종 이상의 α-아미노산 및(또는) 그의 유도체와, 1종 이상이 시클로펜탄-β -아미노산 및(또는) 그의 유도체로 이루어지는 혼합물.
제1항에 있어서, 하기 화학식(Ia)의 α-아미노산을 포함하는 것이 특징인 혼합물.
식 중, R3는 탄소 원자수 3 내지 8의 시클로알킬이거나, 또는 탄소 원자수 6 내지 10의 아릴 또는 수소이거나, 또는 탄소 원자수 8 이하이 직쇄 또는 분지쇄 알킬이고, 여기서, 알킬은 시아노, 메틸티오, 히드록실, 메르캅토, 구아니딜 또는 식 -NR7R8또는 R9-OC-기에 의해 치환될 수 있거나, 또는 히디록실, 할로겐, 니트로, 탄소 원자수 8 이하의 알콕시 또는 -NR7R8기에 의해 치환되는 탄소 원자수 3 내지 8의 시클로알킬 또는 탄소 원자수 6 내지 10의 아릴에 의해 치환될 수 있으며, (식 중, R7및 R8은 서로 독립적으로 수소, 탄소 원자수 8 이하의 직쇄 또는 분지쇄 알킬 또는 페닐이고, R9은 히드록실, 벤질옥시, 탄소 원자수 6 이하의 알콕시 또는 상술한 -NR7R8기임) 또는 R3및 R4가 함께 식 -(CH2)3-의 기를 형성하고, R5가 수소이며, X는 히드록실, 탄소 원자수 6 내지 10의 아릴옥시, 탄소 원자수 6 이하의 알콕시 또는 -NR7R8기(여기서, R7및 R8은 상기에서 정의한 바와 같음)이다.
제1항 또는 제2항에 있어서, 하기 화학식(Ib)이 시클로펜탄-β-아미노산을 포함하는 것이 특징인 혼합물.
식 중, R1및 R2는 수소이거나, 또는 R1및 R2가 함께 식 =CH2의 기를 형성하고, R6는 수소이거나 또는 탄소 원자수 8 이하의 직쇄 또는 분지쇄 알킬 또는 페닐이고, Y는 수소, 탄소 원자수 8 이하의 직쇄 또는 분지쇄 알킬 또는 아릴이다.
제1항에 있어서, 제2항에 따른 α-아미노산 및 제3항에 따른 시클로펜탄-β-아미노산으로 이루어지는 혼합물.
α-아미노산 또는 그 유도체와, 시클로펜탄-β-아미노산 또는 그 유도체로 이루어지는 디펩티드.
제5항에 있어서, 제2항에 따른 화학식(Ia) 중, X가 α-아미노산과 시클로펜탄-β-아미노산의 공유 결합의 부위를 나타내는 것인 화학식(Ia)의 α-아미노산을 포함하는 디펩티드.
제5항 또는 제6항에 있어서, 제3항에 따른 화학식(Ib) 중, Y가 α-아미노산과 시클로펜탄-β-아미노산의 공유 결합의 부위를 나타내는 것인 화학식(Ib)의 시클로펜탄-β-아미노산을 포함하는 디펩티드.
하기 화학식(Ⅱ)의 화합물을 먼저 용매 중에서 염기 존재하에 하기 화학식(Ⅲ)의 보호된 아미노산과 반응시켜 하기 화학식(Ⅳ)의 화합물로 전환시키고, 최종적으로 아미노 보호기(R10)을 제거시키고, 필요에 따라 입체이성질체를 분리시키고, 에스테르〔식(Ib)에서 R6가 H가 아님〕를 얻으려는 경우, 산을 상응하는 알코올과 통상의 방법으로 반응시키고, 필요에 따라 디펩티드를 그의 염으로 전환시키는 것이 특징인 제5항 내지 제7항 중 어느 한 항에 따른 디펩티드의 제조 방법.
〔식 중, R1, R2, R3및 R4는 상기에서 정의한 바와 같고, R10은 아미노 보호기이며, R11은 펩티드 화학에서 통상적인 활성화 보호기, 바람직하게는 히드록시숙신이미드 에스테르기이거나, 또는 R10및 R11가 함께를 형성한다〕
질병, 특히 진균증을 치료하기 위한, 제1항 내지 제4항 중 어느 한 항에 따른 혼합물 및(또는) 제5항 내지 제7항 중 어느 한 항에 따른 디펩티드.
질병, 특히 진균증을 치료하기 위한, 제1항 내지 제4항 중 어느 한 항에 따른 혼합물 및(또는) 제5항 내지 제7항 중 어느 한 항에 따른 디펩티드로 이루어지는 약제.
※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19526274.3 | 1995-07-19 | ||
DE19526274A DE19526274A1 (de) | 1995-07-19 | 1995-07-19 | Verbesserung der Verträglichkeit von pharmazeutisch wirksamen beta-Aminosäuren |
Publications (2)
Publication Number | Publication Date |
---|---|
KR970006312A true KR970006312A (ko) | 1997-02-19 |
KR100433968B1 KR100433968B1 (ko) | 2004-08-30 |
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Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019960028961A KR100433968B1 (ko) | 1995-07-19 | 1996-07-18 | 개선된내용성을갖는제약활성의β-아미노산 |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20010073441A (ko) * | 2000-01-14 | 2001-08-01 | 최인도 | 패류종묘 착상판의 제조방법 |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6191306B1 (en) * | 1999-08-03 | 2001-02-20 | Eastman Chemical Company | Process for the preparation of cyclopropylglycine |
US8394813B2 (en) | 2000-11-14 | 2013-03-12 | Shire Llc | Active agent delivery systems and methods for protecting and administering active agents |
US20060014697A1 (en) | 2001-08-22 | 2006-01-19 | Travis Mickle | Pharmaceutical compositions for prevention of overdose or abuse |
US7169752B2 (en) | 2003-09-30 | 2007-01-30 | New River Pharmaceuticals Inc. | Compounds and compositions for prevention of overdose of oxycodone |
US7659253B2 (en) * | 2002-02-22 | 2010-02-09 | Shire Llc | Abuse-resistant amphetamine prodrugs |
US7105486B2 (en) * | 2002-02-22 | 2006-09-12 | New River Pharmaceuticals Inc. | Abuse-resistant amphetamine compounds |
US7700561B2 (en) * | 2002-02-22 | 2010-04-20 | Shire Llc | Abuse-resistant amphetamine prodrugs |
PT1644019E (pt) * | 2003-05-29 | 2012-05-23 | Shire Llc | Compostos de anfetamina resistentes ao abuso |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8716278D0 (en) * | 1987-07-10 | 1987-08-19 | Fujisawa Pharmaceutical Co | Antimicrobial agent |
JPH02174753A (ja) * | 1988-08-25 | 1990-07-06 | Fujisawa Pharmaceut Co Ltd | シス―2―アミノシクロペンタンカルボン酸誘導体およびその製法ならびに抗菌剤 |
DE4302155A1 (de) * | 1993-01-27 | 1994-07-28 | Bayer Ag | Verwendung von Cyclopentan- und -penten-beta-Aminosäuren |
US5631291A (en) * | 1992-05-29 | 1997-05-20 | Bayer Aktiengesellschaft | Cyclopentane- and -pentene-β-amino acids |
AU673824B2 (en) * | 1992-05-29 | 1996-11-28 | Bayer Aktiengesellschaft | Cyclopentane- and -pentene-beta-amino acids |
GB9216441D0 (en) * | 1992-08-03 | 1992-09-16 | Ici Plc | Fungicidal process |
WO1995007022A1 (en) * | 1993-09-07 | 1995-03-16 | Zeneca Limited | Fungicides |
DE19548825C2 (de) * | 1995-12-27 | 1999-03-25 | Rolf Dr Hermann | Neue, substituierte Cyclopentylaminderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
DE19604225A1 (de) * | 1996-02-06 | 1997-08-07 | Bayer Ag | Stoffzusammensetzungen aus alpha-Aminosäuren und Cyclohexen-beta-aminosäuren |
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1995
- 1995-07-19 DE DE19526274A patent/DE19526274A1/de not_active Withdrawn
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1996
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- 1996-07-08 DK DK00110958T patent/DK1043332T3/da active
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- 1996-07-18 BR BR9603124A patent/BR9603124A/pt active Search and Examination
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20010073441A (ko) * | 2000-01-14 | 2001-08-01 | 최인도 | 패류종묘 착상판의 제조방법 |
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