KR890011902A - Dideoxydidehydrocarbocyclic nucleosides - Google Patents

Dideoxydidehydrocarbocyclic nucleosides Download PDF

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KR890011902A
KR890011902A KR1019890000551A KR890000551A KR890011902A KR 890011902 A KR890011902 A KR 890011902A KR 1019890000551 A KR1019890000551 A KR 1019890000551A KR 890000551 A KR890000551 A KR 890000551A KR 890011902 A KR890011902 A KR 890011902A
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South Korea
Prior art keywords
compound
pharmaceutically acceptable
purin
hydrogen
formula
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KR1019890000551A
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Korean (ko)
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KR0127137B1 (en
Inventor
빈스 로버트
후아 메이
레슬리 마이어스 피터
스토리 리차드
Original Assignee
추후보충
리전츠 오브 더 유니버시티 오브 미네소타
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Priority claimed from US07/146,252 external-priority patent/US4916224A/en
Priority claimed from GB888821011A external-priority patent/GB8821011D0/en
Priority claimed from US07/278,652 external-priority patent/US4931559A/en
Application filed by 추후보충, 리전츠 오브 더 유니버시티 오브 미네소타 filed Critical 추후보충
Publication of KR890011902A publication Critical patent/KR890011902A/en
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Publication of KR0127137B1 publication Critical patent/KR0127137B1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Abstract

내용 없음No content

Description

디데옥시디데히드로카르보시클릭 뉴클레오시드Dideoxydidehydrocarbocyclic nucleosides

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (18)

하기 일반식(Ⅰ)로 표시되는 화합물 및 그의 제약상 허용되는 유도체류.Compounds represented by the following general formula (I) and pharmaceutically acceptable derivatives thereof. 상기식중 X는 수소, NRR1, SR, OR 또는 할로겐이고, Z는 수소, OR2또는 NRR1기이고, R, R1및 R2는 서로 동일하거나 또는 상이한 것으로서, 수소, C1-4알킬 및 아릴기 중에서 선택된다.Wherein X is hydrogen, NRR 1 , SR, OR or halogen, Z is hydrogen, OR 2 or NRR 1 and R, R 1 and R 2 are the same as or different from each other, hydrogen, C 1-4 Alkyl and aryl groups. 제1항에 의한 일반식(Ⅰ)의 화합물 및 그의 제약상 허용되는 염류.A compound of formula (I) according to claim 1 and a pharmaceutically acceptable salt thereof. 제1항 또는 제2항에 있어서, 일반식(Ⅰ)의 화합물에서 Z가 H, OH 또는 NH2기인 화합물.The compound of claim 1 or 2, wherein Z in the compound of formula (I) is H, OH or NH 2 group. 제1항 내지 제3항중 어느 하나의 항에 있어서, Z가 NH2기인 화합물.The compound of any one of claims 1-3, wherein Z is an NH 2 group. 제1항 내지 제4항중 어느 하나의 항에 있어서, X가 수소, 클로로, NH2, SH 또는 OH기인 화합물.The compound of any one of claims 1-4 where X is a hydrogen, chloro, NH 2 , SH or OH group. 제1항 내지 제5항중 어느 하나의 항에 있어서, X가 OH기인 화합물.The compound according to any one of claims 1 to 5, wherein X is an OH group. 제1항 내지 제5항중 어느 하나의 항에 있어서, X가 H 또는 NH2기인 화합물.6. The compound of claim 1, wherein X is H or NH 2. 7 . (1α,4α)-4-(6-클로로-9H-푸린-9-일)-2-시클로펜테닐 카르비놀, (1α,4α)-4-(6-히드록시-9H-푸린-9-일)-2-시클로펜테닐 카르비놀, (1α,4α)-4-(6-아미노-9H-푸린-9-일)-2-시클로펜테닐 카르비놀, (1α,4α)-4-(6-메르캅토-9H-푸린-9-일)-2-시클로펜테닐 카르비놀, (1α,4α)-4-(2,6-디아미노-9H-푸린-9-일)-2-시클로펜테닐 카르비놀, (1α,4α)-4-(2-아미노-6-클로로-9H-푸린-9-일)-2-시클로펜테닐 카르비놀 및 (1α,4α)-4-(2-아미노-9H-푸린-9-일)-2-시클로펜테닐 카르비놀 중에서 선택되는 화합물.(1α, 4α) -4- (6-chloro-9H-purin-9-yl) -2-cyclopentenyl carbinol, (1α, 4α) -4- (6-hydroxy-9H-purin-9- Yl) -2-cyclopentenyl carbinol, (1α, 4α) -4- (6-amino-9H-purin-9-yl) -2-cyclopentenyl carbinol, (1α, 4α) -4- ( 6-mercapto-9H-purin-9-yl) -2-cyclopentenyl carbinol, (1α, 4α) -4- (2,6-diamino-9H-purin-9-yl) -2-cyclo Pentenyl carbinol, (1α, 4α) -4- (2-amino-6-chloro-9H-purin-9-yl) -2-cyclopentenyl carbinol and (1α, 4α) -4- (2- Amino-9H-purin-9-yl) -2-cyclopentenyl carbinol. (1α,4α)-4-(2-아미노-6-히드록시-9H-푸린-9-일)-2-시클로펜테닐 카르비놀.(1α, 4α) -4- (2-amino-6-hydroxy-9H-purin-9-yl) -2-cyclopentenyl carbinol. 제1항 내지 제9항중 어느 하나의 항에 있어서, 실질적으로 라세미 혼합물 형태의 화합물.10. A compound according to any one of the preceding claims in the form of a racemic mixture substantially. 제1항 내지 제9항중 어느 하나의 항에 있어서, 실질적으로 광학 이성질체로 되는 화합물.10. A compound according to any one of claims 1 to 9, which is substantially an optical isomer. 제1항 내지 제9항중 어느 하나의 항에 있어서, 실질적으로 D 이성질체로 되는 화합물.10. A compound according to any one of claims 1 to 9, consisting essentially of the D isomer. 유효한 치료제로서의 용도의 제1항 내지 제12항중 어느 하나의 항에 의한 일반식(Ⅰ)의 화합물 또는 그의 제약상 허용되는 유도체.A compound of formula (I) or a pharmaceutically acceptable derivative thereof according to any one of claims 1 to 12 for use as an effective therapeutic agent. 비루스 감염 치료용 의약품 제조 용도의 제1항 내지 제12항중 어느 하나의 항에 의한 일반식(Ⅰ)의 화합물 및 그의 제약상 허용되는 유도체.A compound of formula (I) according to any one of claims 1 to 12, and a pharmaceutically acceptable derivative thereof, for use in the manufacture of a medicament for the treatment of virus infection. 제1항 내지 제12항중 어느 하나의 항에 의한 일반식(Ⅰ)의 화합물 또는 그의 제약상 허용되는 유도체와 이를 위한 제약상 허용되는 담체로 되는 약제.A medicament comprising a compound of formula (I) according to any one of claims 1 to 12 or a pharmaceutically acceptable derivative thereof and a pharmaceutically acceptable carrier therefor. 제1항 내지 제12항중 어느 하나의 항에 의한 일반식(Ⅰ)의 화합물 또는 그의 제약상 허용되는 염과 이를 위한 제약상 허용되는 담체로 되는 약제.A medicament comprising a compound of formula (I) according to any one of claims 1 to 12 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor. 제15항에 있어서, 추가로 부가의 치료제로 되는 약제.The agent according to claim 15, which is further an additional therapeutic agent. 하기 일반식(Ⅱ)로 표시되는 화합물 및 그의 제약상 허용되는 유도체류.Compounds represented by the following general formula (II) and pharmaceutically acceptable derivatives thereof. 상기식중 X는 수소, HRR1, SR, OR, 할로겐 또는 그의 보호 형태이고, Y는 OH 또는 그의 보호 형태이고, Z는 수소, OR2, NRR1또는 그의 보호 형태이고, R, R1및 R2는 서로 동일하거나 또는 상이한 것으로서, 수소, C1-4알킬 및 아릴기 중에서 선택된다.Wherein X is hydrogen, HRR 1 , SR, OR, halogen or a protected form thereof, Y is OH or a protected form thereof, Z is hydrogen, OR 2 , NRR 1 or a protected form thereof, R, R 1 and R 2 is the same as or different from each other and is selected from hydrogen, C 1-4 alkyl and aryl groups. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019890000551A 1988-01-20 1989-01-19 Dideoxy dehydrocarbo cyclic nucleosides KR0127137B1 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US07/146,252 US4916224A (en) 1988-01-20 1988-01-20 Dideoxycarbocyclic nucleosides
GB888821011A GB8821011D0 (en) 1988-09-07 1988-09-07 Chemical compounds
US8821011.7 1988-12-05
US278,652 1988-12-05
US07/278,652 US4931559A (en) 1988-01-20 1988-12-05 Optically-active isomers of dideoxycarbocyclic nucleosides
US146,252 1988-12-05

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KR890011902A true KR890011902A (en) 1989-08-23
KR0127137B1 KR0127137B1 (en) 1997-12-29

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JP (1) JP2793825B2 (en)
KR (1) KR0127137B1 (en)
AT (1) AT397801B (en)
AU (2) AU626278B2 (en)
BE (1) BE1003815A4 (en)
CA (1) CA1339896C (en)
CH (1) CH679152A5 (en)
DE (1) DE3901502C2 (en)
DK (1) DK175131B1 (en)
ES (1) ES2010091A6 (en)
FI (1) FI93546C (en)
FR (1) FR2626002B1 (en)
GB (1) GB2217320B (en)
GR (1) GR890100033A (en)
HU (1) HU203755B (en)
IE (1) IE62275B1 (en)
IL (1) IL88999A (en)
IT (1) IT1229531B (en)
LU (1) LU87437A1 (en)
MY (1) MY103801A (en)
NL (1) NL8900122A (en)
NO (1) NO169123C (en)
NZ (1) NZ227663A (en)
OA (1) OA09031A (en)
PL (1) PL163814B1 (en)
PT (1) PT89482B (en)
RU (1) RU2114846C1 (en)
SE (1) SE505213C2 (en)
YU (1) YU47791B (en)

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US5631370A (en) 1988-01-20 1997-05-20 Regents Of The University Of Minnesota Optically-active isomers of dideoxycarbocyclic nucleosides
GB8815265D0 (en) * 1988-06-27 1988-08-03 Wellcome Found Therapeutic nucleosides
US4939252A (en) * 1989-04-20 1990-07-03 Hoffmann-La Roche Inc. Novel intermediates for the preparation of Carbovir
ATE183508T1 (en) * 1989-06-27 1999-09-15 Wellcome Found THERAPEUTIC NUCLEOSIDES
GB8916478D0 (en) * 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
GB8916479D0 (en) * 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
GB8916477D0 (en) * 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
GB8916480D0 (en) * 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
MY104575A (en) * 1989-12-22 1994-04-30 The Wellcome Foundation Ltd Therapeutic nucleosides.
US5126452A (en) * 1990-04-06 1992-06-30 Glaxo Inc. Synthesis of purine substituted cyclopentene derivatives
US5241069A (en) * 1990-04-06 1993-08-31 Glaxo Inc. Carbonate intermediates for the synthesis of purine substituted cyclopentene derivatives
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KR960705825A (en) * 1993-11-12 1996-11-08 게리 디. 스트리트 6-Oxo-nucleosides useful as immunosuppressants
GB9721780D0 (en) * 1997-10-14 1997-12-10 Glaxo Group Ltd Process for the synthesis of chloropurine intermediates
US6433170B1 (en) 1998-10-30 2002-08-13 Lonza Group Method for producing 4-[2',5'-diamino-6'-halopyrimidine-4'-yl)amino]- cyclopent-2-enylmethanols
PL198180B1 (en) * 1998-10-30 2008-06-30 Lonza Ag Method for producing 4-[(2',5'-diamino-6'-halopyrimidine-4'-yl)amino]-cyclopent-2-enylmethanols
TWI229674B (en) 1998-12-04 2005-03-21 Astra Pharma Prod Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses
GB9903091D0 (en) * 1999-02-12 1999-03-31 Glaxo Group Ltd Therapeutic nucleoside compound
AR039540A1 (en) 2002-05-13 2005-02-23 Tibotec Pharm Ltd MICROBICIDE COMPOUNDS WITH PIRIMIDINE OR TRIAZINE CONTENT
WO2020022486A1 (en) 2018-07-27 2020-01-30 富士フイルム株式会社 Cyclopentenyl purine derivative or salt thereof
JP2023519882A (en) 2020-03-27 2023-05-15 ソム、イノベーション、バイオテック、ソシエダッド、アノニマ Compounds useful for treating synucleinopathies

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MY104575A (en) * 1989-12-22 1994-04-30 The Wellcome Foundation Ltd Therapeutic nucleosides.

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GB8901187D0 (en) 1989-03-15
IL88999A0 (en) 1989-08-15
IT1229531B (en) 1991-09-04
CA1339896C (en) 1998-06-02
GR890100033A (en) 1994-03-31
FI890286A0 (en) 1989-01-19
OA09031A (en) 1991-03-31
BE1003815A4 (en) 1992-06-23
NO890253D0 (en) 1989-01-19
PT89482B (en) 1994-02-28
DK23489D0 (en) 1989-01-19
FI93546C (en) 1995-04-25
GB2217320A (en) 1989-10-25
YU12389A (en) 1991-10-31
PT89482A (en) 1989-10-04
PL163814B1 (en) 1994-05-31
PL277261A1 (en) 1989-09-18
LU87437A1 (en) 1989-08-30
JPH02196788A (en) 1990-08-03
IE890153L (en) 1989-07-20
GB2217320B (en) 1992-04-08
NO890253L (en) 1989-07-21
DK23489A (en) 1989-07-21
FI93546B (en) 1995-01-13
HU203755B (en) 1991-09-30
AU2867189A (en) 1989-07-20
RU2114846C1 (en) 1998-07-10
SE8900192L (en) 1989-07-21
DE3901502C2 (en) 2002-06-13
MY103801A (en) 1993-09-30
NL8900122A (en) 1989-08-16
CH679152A5 (en) 1991-12-31
SE8900192D0 (en) 1989-01-19
IE62275B1 (en) 1995-01-25
FR2626002B1 (en) 1994-01-28
AU637015B2 (en) 1993-05-13
AU626278B2 (en) 1992-07-30
ES2010091A6 (en) 1989-10-16
IL88999A (en) 1994-12-29
SE505213C2 (en) 1997-07-14
AU1018092A (en) 1992-03-12
NZ227663A (en) 1990-09-26
NO169123B (en) 1992-02-03
KR0127137B1 (en) 1997-12-29
HUT48887A (en) 1989-07-28
AT397801B (en) 1994-07-25
DK175131B1 (en) 2004-06-14
FR2626002A1 (en) 1989-07-21
IT8947546A0 (en) 1989-01-19
DE3901502A1 (en) 1989-07-27
ATA10689A (en) 1993-11-15
NO169123C (en) 1992-05-13
JP2793825B2 (en) 1998-09-03
FI890286A (en) 1989-07-21
YU47791B (en) 1996-01-09

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