KR950704482A - 치료용 항-hiv 올리고누클레오티드 및 이것을 함유하는 약제학적 제형(therapeutic anti-hiv oligonucleotide and pharmaceutical) - Google Patents
치료용 항-hiv 올리고누클레오티드 및 이것을 함유하는 약제학적 제형(therapeutic anti-hiv oligonucleotide and pharmaceutical)Info
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- KR950704482A KR950704482A KR1019950701317A KR19950701317A KR950704482A KR 950704482 A KR950704482 A KR 950704482A KR 1019950701317 A KR1019950701317 A KR 1019950701317A KR 19950701317 A KR19950701317 A KR 19950701317A KR 950704482 A KR950704482 A KR 950704482A
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- 108091034117 Oligonucleotide Proteins 0.000 title claims abstract 52
- 230000001225 therapeutic effect Effects 0.000 title claims abstract 10
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 title abstract 3
- 230000036436 anti-hiv Effects 0.000 title 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 241000713772 Human immunodeficiency virus 1 Species 0.000 claims abstract description 13
- 239000002773 nucleotide Substances 0.000 claims abstract 24
- 125000003729 nucleotide group Chemical group 0.000 claims abstract 23
- 238000009472 formulation Methods 0.000 claims abstract 8
- 239000000203 mixture Substances 0.000 claims abstract 8
- 238000000034 method Methods 0.000 claims abstract 5
- 230000035755 proliferation Effects 0.000 claims abstract 3
- 241000124008 Mammalia Species 0.000 claims abstract 2
- 101710163270 Nuclease Proteins 0.000 claims abstract 2
- 230000029087 digestion Effects 0.000 claims abstract 2
- 150000004713 phosphodiesters Chemical class 0.000 claims abstract 2
- 108020004999 messenger RNA Proteins 0.000 claims 4
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 3
- 230000001566 pro-viral effect Effects 0.000 claims 2
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
- 239000000074 antisense oligonucleotide Substances 0.000 claims 1
- 238000012230 antisense oligonucleotides Methods 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000000692 anti-sense effect Effects 0.000 description 1
- 238000004581 coalescence Methods 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 125000005642 phosphothioate group Chemical group 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
- C12N15/1131—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against viruses
- C12N15/1132—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against viruses against retroviridae, e.g. HIV
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
- A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
- A61K31/7125—Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
-
- 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
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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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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/31—Chemical structure of the backbone
- C12N2310/315—Phosphorothioates
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Abstract
본 발명에서는 HIV-1게놈의 보존된
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 HIV-1 게놈의 표적화된개시 영역 및 그것에 대한 본 발명의 안티센스 포스포티오에이트 누클레오티드의 상보성을 도시한 개략도,
제2도는 표적화된개시 영역 및 본 발명의 25합체를 도시하는 개략도,
제3도는 표적화된개시 영역 및 미츠쿠라등의 28합체를 도시한 개략도.
Claims (24)
- 최소한 하나의 비-포스포디에스테르 누클레오티드간 결합에 의해 결합된 약 25 내지 30누클레오티드를 가지며, 이 결합으로 인해 누클레아제 소화에 대해 올리고 누클레오티드가 내성을 갖게 되는, HIV-1 게놈의 보존된영역의 최소한의 누클레오티드 324 내지 348에 혼성화하는 누클레오티드 서열을 갖고 있는 올리고누클레오티드.
- 제1항에 있어서, 리소한 하나의 비-포스포디에스테르 누클레오티드간 결합이 포스포로티오에이트 결합인 것을 특징으로 하는 올리고누클레오티드.
- 제2항에 있어서, 올리고누클레오티드가 25개의 누클레오티드를 가지는 것을 특징으로 하는 올리고누클레오티드.
- 제3항에 있어서, 서열 목록에서 SEQ ID NO : 1로서 표시된 누클레오티드를 가지는 올리고누클레오티드.
- 제2항에 있어서, 올리고누클레오티드가 26개의 누클레오티드를 가지는 것을 특징으로 하는 올리고누클레오티드.
- 제5항에 있어서, 서열 목록에서 SEQ ID NO : 2로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 제5항에 있어서, 서열 목록에서 SEQ ID NO : 3으로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 제2항에 있어서, 올리고누클레오티드가 27개의 누클레오티드들 가지는 것을 특징으로 하는 올리고누클레오티드.
- 제8항에 있어서, 서열 목록에서 SEQ ID NO : 4로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 제2항에 있어서, 올리고누클레오티드가 28개의 누클레오티드를 가지는 것을 특징으로 하는 을리고누클레오티드.
- 제10항에 있어서, 서열 목록에서 SEQ ID NO : 5로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 제10항에 있어서, 서열 목록에서 SEQ ID NO : 6로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 제2항에 있어서, 올리고누클레오티드가 29개의 누클레오티드를 가지는 것을 특징으로 하는 올리고누클레오티드.
- 제13항에 있어서, 서열 목록에서 SEQ ID NO : 7로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 제2항에 있어서, 올리고누클레오티드가 30개의 누클레오티드를 가지는 것을 특징으로 하는 올리고누클레오티드.
- 제15항에 있어서, 서열 목록에서 SEQ ID NO : 8로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 제15항에 있어서, 서열 목록에서 SEQ ID NO : 9로서 표시된 누클레오티드 서열을 가지는 올리고누클레오티드.
- 생리적으로 허용되는 담체중에 제1항의 올리고누클레오티드를 포함하는 치료용 제형.
- 생리적으로 허용되는 담체중에 제4항의 올리고누클레오티드클 포함하는 치료용 제형.
- 제1항의 올리고누클레오티드인 제1의 올리고누클레오티드와 제2의 항-HIV-1 안티센스 올리고누클레오티드를 포함하는 치료용 제형.
- (a)생리적으로 허용되는 담체중에 제1항의 올리고누클레오티드를 포함하는 치료용 제형을 제공하는 단계 ; 그리고 (b)HIV-1 감염된 세포를, 감염된 세포에서 어떠한 HIV-1 프로바이러스 DNA 또는 mRNA의영역에 올리고누클레오티드가 결합되는 것을 가능하게 하기에 충분한 양의 치료용 제형으로 처리하는 단계로 이루어지며, 그로써, 올리고누클레오티드가 HIV-1 DNA또는 mRNA에 결합하여 HIV-1의 증식이 억제되는 것을 특징으로 하는, HIV-1 증식의 억제 방법.
- 제21항에 있어서, 상기 제공 단계가 최소한 하나의 포스포로티오에이트 결합에 의해 결합된 25개의 누클레오티드를 갖는 올리고누클레오티드를 제공하는 것을 포함하며, 올리고누클레오티드의 서열은 서열 목록에서 SEQ ID NO : 1로서 표시되는 것을 특징으로 하는 방법.
- (a)생리적으로 허용되는 담체중에 제1항의 올리고누클레오티드틀 포함하는 치료용 제형을 제공하는 단계 ; 그리고 (b)HIV-1 감염된 세포를, 감염된 세포에서 어떠한 HIV-1 프로바이러스 DNA 또는 mRNA의영역에 올리고누클레오티드가 결합하는 것을 가능하게 하기에 충분한 양의 치료용 제형으로 처리하는 단계로 이루어지며, 그로써, 올리고누클레오티드가 HIV-1 DNA 또는 mRNA에 결합하여 포유류에서 HIV-1 DNA의 발현 및 복제가 억제되는 것을 특징으로 하는, 포유류에서 HIV-1 감염을 치료하는 방법.
- 제23항에 있어서, 상기 제공 단계가 최소한 하나의 포스포로티오에이트 결합에 의해 결합된 25개의 누클레오티드를 갖는 올리고누클레오티드를 제공하는 것을 포함하며, 올리고누클레오티드의 서열은 서열 목록에서 SEQ ID NO : 1로서 표시되는 것을 특징으로 하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US95813592A | 1992-10-05 | 1992-10-05 | |
US958135 | 1992-10-05 | ||
PCT/US1993/009392 WO1994008004A1 (en) | 1992-10-05 | 1993-10-04 | Therapeutic anti-hiv oligonucleotide and pharmaceutical |
Publications (1)
Publication Number | Publication Date |
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KR950704482A true KR950704482A (ko) | 1995-11-20 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019950701317A Withdrawn KR950704482A (ko) | 1992-10-05 | 1993-10-04 | 치료용 항-hiv 올리고누클레오티드 및 이것을 함유하는 약제학적 제형(therapeutic anti-hiv oligonucleotide and pharmaceutical) |
Country Status (19)
Country | Link |
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US (1) | US5684147A (ko) |
EP (1) | EP0664833B1 (ko) |
JP (1) | JPH08504570A (ko) |
KR (1) | KR950704482A (ko) |
AT (1) | ATE146819T1 (ko) |
AU (1) | AU678415B2 (ko) |
BR (1) | BR9307191A (ko) |
CA (1) | CA2146364A1 (ko) |
CZ (1) | CZ85495A3 (ko) |
DE (1) | DE69306969T2 (ko) |
DK (1) | DK0664833T3 (ko) |
ES (1) | ES2096343T3 (ko) |
FI (1) | FI951600L (ko) |
GR (1) | GR3022315T3 (ko) |
HU (1) | HUT72400A (ko) |
NO (1) | NO951307L (ko) |
NZ (1) | NZ257434A (ko) |
PL (1) | PL308261A1 (ko) |
WO (1) | WO1994008004A1 (ko) |
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WO1989008146A1 (en) * | 1988-02-26 | 1989-09-08 | Worcester Foundation For Experimental Biology | Inhibition of htlv-iii by exogenous oligonucleotides |
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1993
- 1993-10-04 WO PCT/US1993/009392 patent/WO1994008004A1/en not_active Application Discontinuation
- 1993-10-04 JP JP6509354A patent/JPH08504570A/ja active Pending
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- 1993-10-04 HU HU9500995A patent/HUT72400A/hu unknown
- 1993-10-04 AT AT93924289T patent/ATE146819T1/de not_active IP Right Cessation
- 1993-10-04 CZ CZ95854A patent/CZ85495A3/cs unknown
- 1993-10-04 EP EP93924289A patent/EP0664833B1/en not_active Expired - Lifetime
- 1993-10-04 PL PL93308261A patent/PL308261A1/xx unknown
- 1993-10-04 KR KR1019950701317A patent/KR950704482A/ko not_active Withdrawn
- 1993-10-04 ES ES93924289T patent/ES2096343T3/es not_active Expired - Lifetime
- 1993-10-04 DE DE69306969T patent/DE69306969T2/de not_active Expired - Fee Related
- 1993-10-04 DK DK93924289.7T patent/DK0664833T3/da active
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- 1993-10-04 CA CA002146364A patent/CA2146364A1/en not_active Abandoned
- 1993-10-04 BR BR9307191A patent/BR9307191A/pt not_active Application Discontinuation
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1994
- 1994-10-07 US US08/319,823 patent/US5684147A/en not_active Expired - Lifetime
-
1995
- 1995-04-04 FI FI951600A patent/FI951600L/fi not_active Application Discontinuation
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1997
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CA2146364A1 (en) | 1994-04-14 |
HUT72400A (en) | 1996-04-29 |
WO1994008004A1 (en) | 1994-04-14 |
AU5402894A (en) | 1994-04-26 |
ES2096343T3 (es) | 1997-03-01 |
EP0664833B1 (en) | 1996-12-27 |
EP0664833A1 (en) | 1995-08-02 |
DK0664833T3 (da) | 1997-04-14 |
BR9307191A (pt) | 1999-03-30 |
ATE146819T1 (de) | 1997-01-15 |
NO951307L (no) | 1995-06-01 |
DE69306969D1 (de) | 1997-02-06 |
HU9500995D0 (en) | 1995-06-28 |
FI951600L (fi) | 1995-05-10 |
CZ85495A3 (en) | 1996-03-13 |
US5684147A (en) | 1997-11-04 |
AU678415B2 (en) | 1997-05-29 |
JPH08504570A (ja) | 1996-05-21 |
DE69306969T2 (de) | 1997-05-07 |
GR3022315T3 (en) | 1997-04-30 |
NZ257434A (en) | 1997-01-29 |
FI951600A0 (fi) | 1995-04-04 |
PL308261A1 (en) | 1995-07-24 |
NO951307D0 (no) | 1995-04-04 |
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