KR960041173A - Irreversible HIV Protease Inhibitor with Anti-Aids (AIDS) Effect, Method of Preparation and Composition Comprising the Same - Google Patents
Irreversible HIV Protease Inhibitor with Anti-Aids (AIDS) Effect, Method of Preparation and Composition Comprising the Same Download PDFInfo
- Publication number
- KR960041173A KR960041173A KR1019950013367A KR19950013367A KR960041173A KR 960041173 A KR960041173 A KR 960041173A KR 1019950013367 A KR1019950013367 A KR 1019950013367A KR 19950013367 A KR19950013367 A KR 19950013367A KR 960041173 A KR960041173 A KR 960041173A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- formula
- phenyl
- amino
- valinyl
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/55—Protease inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D303/46—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by amide or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
Abstract
본 발명은 HIV 프로테아제의 억제제로서 유용한 신규 화합물 및 그의 제조방법 및 이를 포함하는 조성물에 관한 것으로서, 하기의 일반식(Ⅰ)의 시스-에폭사이드 구조를 갖는 화합물 및 그의 약학적으로 허용되는 염, 수화물 또는 용매화물은, HIV 프로테아제의 비가역적 억제제로서 억제 효과는 높은 반면 그 세포독성은 낮기 때문에, 에이즈 또는 HIV감염의 치료 또는 예방용 제제로서 유용하게 사용될 수 있다.The present invention relates to a novel compound useful as an inhibitor of HIV protease, a method for preparing the same, and a composition comprising the same, the compound having a cis-epoxide structure of the following general formula (I) and a pharmaceutically acceptable salt and hydrate thereof Alternatively, solvates can be usefully used as agents for the treatment or prevention of HIV or HIV infection because of their high inhibitory effect and low cytotoxicity as irreversible inhibitors of HIV proteases.
상기 식에서, R1, R2및 R3는 명세서중에서 정의한 바와 같다.In the above formula, R 1 , R 2 and R 3 are as defined in the specification.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.
Claims (6)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1019950013367A KR0161140B1 (en) | 1995-05-26 | 1995-05-26 | Irrevesible hiv protease inhibitors with anti-aids effect, process for the preparation thereof and compositions containing the same |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1019950013367A KR0161140B1 (en) | 1995-05-26 | 1995-05-26 | Irrevesible hiv protease inhibitors with anti-aids effect, process for the preparation thereof and compositions containing the same |
Publications (2)
Publication Number | Publication Date |
---|---|
KR960041173A true KR960041173A (en) | 1996-12-19 |
KR0161140B1 KR0161140B1 (en) | 1998-12-01 |
Family
ID=19415504
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019950013367A KR0161140B1 (en) | 1995-05-26 | 1995-05-26 | Irrevesible hiv protease inhibitors with anti-aids effect, process for the preparation thereof and compositions containing the same |
Country Status (1)
Country | Link |
---|---|
KR (1) | KR0161140B1 (en) |
-
1995
- 1995-05-26 KR KR1019950013367A patent/KR0161140B1/en not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
KR0161140B1 (en) | 1998-12-01 |
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A201 | Request for examination | ||
E902 | Notification of reason for refusal | ||
E701 | Decision to grant or registration of patent right | ||
GRNT | Written decision to grant | ||
FPAY | Annual fee payment |
Payment date: 20020729 Year of fee payment: 5 |
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LAPS | Lapse due to unpaid annual fee |