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61. 发明授权

KR100618663B1 뉴클레오티드 동족체 조성물 有权
标题翻译：核苷类似物组合物
公开(公告)号：KR100618663B1
公开(公告)日：2006-09-08
申请号：KR1019997012410
申请日：1998-07-23
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 아리밀리머티엔. , 리토마스티.케이. , 마네즈로렌스브이. , 멍거존디.주니어 , 프리스베어니스트제이. , 슐체리사엠. , 켈리다프네이.
IPC分类号： C07F9/6561
CPC分类号： A61K31/675 , C07F9/65616
摘要： 본 발명은 아데포버 디피복실의 결정형 및 결정을 제조하는 방법에 관한 것이다. 본 발명의 조성물 및 방법은 결정형 아데포버 디피복실의 대규모 합성 또는 치료적 투약 형태로 배합에 적합한 특성을 갖는다. 본 발명의 조성물은 아데포버 디피복실의 무수 결정형을 함유한다.

62. 发明公开

KR1020060038451A (R)-9-[(2-포스포노메톡시)프로필]아데닌(ΡΜΡΑ)의 제조 방법 有权
标题翻译：用于制备PMPA和合成方法的中间体
公开(公告)号：KR1020060038451A
公开(公告)日：2006-05-03
申请号：KR1020067001297
申请日：1998-07-23
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 문거존디.주니어 , 로오로프존시. , 슐쯔리사엠.
IPC分类号： C07F9/6561 , C07D473/34 , C07F9/00
CPC分类号： C07F9/65616 , C07D473/34
摘要： The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p -toluenesulfonylmethoxy-phosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.
摘要翻译：本发明提供包含双（POC）PMPA和富马酸（1:1）的组合物。该组合物可用作制备抗病毒化合物的中间体，或可用于给患者施用抗病毒治疗或预防。当口服给药时，组合物特别有用。本发明还提供了在PMPA合成中制备PMPA和中间体的方法。实施方案包括在有机溶剂如DMF中的叔丁醇锂，9-（2-羟丙基）腺嘌呤和对甲苯磺酰基甲氧基膦酸二乙酯。与通过现有方法制备的二乙基PMPA相比，反应产生含有改进的副产物谱的二乙基PMPA制剂。

63. 发明公开

KR1020060038364A 뉴클레오티드 동족체의 제조에 사용되는 중간체의 제조방법 有权
标题翻译：制备核苷类似物的中间体的制备方法
公开(公告)号：KR1020060038364A
公开(公告)日：2006-05-03
申请号：KR1020057020625
申请日：1998-07-23
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 아리밀리머티엔. , 리토마스티.케이. , 마네즈로렌스브이. , 멍거존디.주니어 , 프리스베어니스트제이. , 슐체리사엠. , 켈리다프네이.
IPC分类号： C07F9/6561 , A61K31/675 , C07F9/00
CPC分类号： A61K31/675 , C07F9/65616
摘要： The invention provides crystalline forms of adefovir dipivoxil and methods to prepare the crystals. The compositions and methods of the present invention have desirable properties for large scale synthesis of crystalline adefovir dipivoxil or for its formulation into therapeutic dosages. Invention compositions include an anhydrous crystal form of adefovir dipivoxil.
摘要翻译：本发明提供结晶形式的阿德福韦酯和制备晶体的方法。本发明的组合物和方法具有用于大规模合成结晶阿德福韦酯或其制剂成治疗剂量的所需性质。本发明组合物包括无水晶形阿德福韦酯。

64. 发明公开

KR1020000052697A 혈관내피 성장인자 핵산 리간드 복합체 有权
标题翻译：血管内皮生长因子（VEGF）核酸配体复合物
公开(公告)号：KR1020000052697A
公开(公告)日：2000-08-25
申请号：KR1019997003488
申请日：1997-10-17
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 잔지크네보자 , 골드래리 , 슈미트폴지. , 바지스칸드라 , 윌리스미첼
IPC分类号： A61K38/00
CPC分类号： C12N15/115 , A61K9/0019 , A61K9/0048 , A61K9/127 , A61K38/00 , A61K47/544 , C07H21/00 , C07K14/52 , C12N15/88 , C12N2310/321 , C12N2310/322 , C12N2310/3515 , C12N2310/3521
摘要： PURPOSE: A high affinity 2' Fluoro (2'-F) pyrimidine RNA ligands to vascular endothelial growth factor (VEGF) is provided. CONSTITUTION: A method for preparing a complex is comprised of a VEGF Nucleic Acid Ligand and a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound by identifying a VEGF Nucleic Acid Ligand by SELEX methodology and associating the VEGF Nucleic Acid Ligand with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. A Lipid construct comprising a VEGF Nucleic Acid Ligand or Complex and methods for making the same is included.
摘要翻译：目的：提供高亲和力2'氟（2'-F）嘧啶RNA配体血管内皮生长因子（VEGF）。构成：通过SELEX方法鉴定VEGF核酸配体并将VEGF核酸配体与非 - 免疫原性，高分子量化合物或亲脂性化合物的VEGF核酸配体结合，免疫原性，高分子量化合物或亲脂性化合物。包括含有VEGF核酸配体或复合物的脂质构建体及其制备方法。

65. 发明公开

KR1020000029705A 뉴클레오타이드 동족체 有权
标题翻译：核素类似物
公开(公告)号：KR1020000029705A
公开(公告)日：2000-05-25
申请号：KR1019997000806
申请日：1997-07-25
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 아리밀리머티엔. , 컨디케네쓰씨. , 도오티죠셉피. , 킴종유 , 올리아이레자 , 스텔라발렌티노제이.
IPC分类号： C07F9/6561
CPC分类号： C07F9/65121 , C07F9/65616
摘要： PURPOSE: Nucleotide analogs are provided which are useful as intermediates for the preparation of antiviral compounds or oligonucleotides, or are useful for administration directly to patients for antiviral therapy or prophylaxis. CONSTITUTION: Novel compounds comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbonates having the structure -OC(R2)2OC(O)X(R)a, wherein R2 independently is H, C1-12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR3 in which R3 is C1-12 alkyl; X is N or O; R is independently H, C1-12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, -O-, -N=, -NR4, -N(R4)2-or OR3, R4 independently is -H or C1-8 alkyl, provided that at least one R is not H; and a is 1 or 2, with the proviso that when a is 2 and X is N, (a) two R groups can be taken together to form a carbo cycle or oxygen-containing heterocycle, or (b) one R additionally can be OR3.
摘要翻译：目的：提供可用作制备抗病毒化合物或寡核苷酸的中间体的核苷酸类似物，或可用于直接给予患者进行抗病毒治疗或预防。构成：新型化合物包含具有结构-OC（R 2）2 OC（O）X（R）a的碳酸酯和/或碳酸酯的抗病毒膦基甲氧基核苷酸类似物的酯，其中R2独立地为H，C1-12烷基，芳基，烯基，炔基，烷基芳基，炔基芳基，烷芳基，芳基炔基，芳基烯基或芳基烷基，其未被取代或被卤素，叠氮基，硝基或OR 3取代，其中R 3是C 1-12烷基; X为N或O; R是独立的H，C1-12烷基，芳基，烯基，炔基，烷基芳基，炔基芳基，烷芳基，芳基炔基，芳基烯基或芳基烷基，它们是未取代的或被卤素，叠氮基，硝基，-O - ， - N = ，-N（R 4）2 - 或OR 3，R 4独立地是-H或C 1-8烷基，条件是至少一个R不是H; 和a为1或2，条件是当a为2且X为N时，（a）两个R基团可以一起形成碳环或含氧杂环，或（b）一个R另外可以是 OR3。

66. 发明授权

KR102153996B1 인간 면역결핍 바이러스의 치료를 위한 치료 조성물 有权
公开(公告)号：KR102153996B1
公开(公告)日：2020-09-09
申请号：KR1020187015929
申请日：2016-11-08
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 홍,레이 , 콜맨,벤자민,미카 , 코지아라,조안나엠.
IPC分类号： A61K9/20 , A61K9/28 , A61K9/24 , A61K9/00 , A61K31/5365 , A61K31/513 , A61K31/553 , A61K31/675

67. 发明授权

KR102108864B1 부분입체 이성질성으로 순수한 포스포라미데이트 전구약물의 제조 방법 有权
公开(公告)号：KR102108864B1
公开(公告)日：2020-05-12
申请号：KR1020197018279
申请日：2011-07-19
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 초,에이솝 , 클라크,마이클,오‘닐한라한 , 월켄하우어,스코트,알란
IPC分类号： C07H19/02 , C07H19/10 , C07H19/20 , C07H1/00 , C07H1/06 , C07D309/10

69. 发明授权

KR102068856B1 항바이러스 치료를 위한 2'-치환된 카바-뉴클레오시드 유사체 有权
公开(公告)号：KR102068856B1
公开(公告)日：2020-01-21
申请号：KR1020147028523
申请日：2013-03-11
申请人： 길리애드 사이언시즈, 인코포레이티드
发明人： 클락마이클오닐핸러헌
IPC分类号： C07H19/23 , C07H19/12 , A61K31/706 , A61K45/06 , A61P31/16

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