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1. 发明申请

WO1996001841A1 CATIONIC LIPIDS FOR DELIVERY OF NUCLEIC ACIDS TO CELLS 审中-公开
标题翻译：用于向细胞递送核酸的阳离子脂肪
公开(公告)号：WO1996001841A1
公开(公告)日：1996-01-25
申请号：PCT/US1995008567
申请日：1995-07-07
申请人： GILEAD SCIENCES, INC. , GLAXO WELLCOME INC.
发明人： GILEAD SCIENCES, INC. , GLAXO WELLCOME INC. , DEPRINCE, Randolph, B. , FACCHINE, Kevin, L. , LEWIS, George, S. , LEWIS, Jason, G. , LIN, Kuei-Ying , MATTEUCCI, Mark, D. , MOOK, Robert, A., Jr. , WAGNER, Richard, W.
IPC分类号： C07K05/06
CPC分类号： C07K5/06095 , A61K9/1272 , A61K38/00 , C07C237/06 , C07C237/20 , C07C237/22 , C07C271/22 , C07C279/14 , C07C279/22 , C07C279/24 , C07J41/0055 , C07K5/06086 , C12N15/88
摘要： The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted arginine, lysine or ornithine residues, or derivatives thereof, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.
摘要翻译：本发明涉及其合成中的新的阳离子脂质和中间体，其可用于将核酸或肽转染到原核或真核细胞中。脂质包含与亲油部分连接的一个或两个取代的精氨酸，赖氨酸或鸟氨酸残基或其衍生物。当与聚阴离子例如核酸或肽混合时，脂质形成复合物。复合物允许聚阴离子有效转移到细胞中，通常对细胞没有显着的毒性。

2. 发明申请

WO1998004569A1 NUCLEOTIDE ANALOGS 审中-公开
标题翻译：核素类似物
公开(公告)号：WO1998004569A1
公开(公告)日：1998-02-05
申请号：PCT/US1997013244
申请日：1997-07-25
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , ARIMILLI, Murty, N. , CUNDY, Kenneth, C. , DOUGHERTY, Joseph, P. , KIM, Choung, U. , OLIYAI, Reza , STELLA, Valentino, J.
IPC分类号： C07F09/6561
CPC分类号： C07F9/65616 , C07F9/6512
摘要： Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure -OC(R )2OC(O)X(R)a, wherein R independently is H, C1-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR in which R is C1-C12 alkyl; X is N or O; R is independently H, C1-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, -O-, -N=, -NR -, -N(R )2- or OR , R independently is -H or C1-C8 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 carbocycle or oxygen-containing heterocycle, or (b) one R additionally can be OR . The compounds 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. Embodiments are particularly useful when administered orally.
摘要翻译：提供新的化合物，其包含抗病毒膦基甲氧基核苷酸类似物与具有结构-OC（R 2）2 OC（O）X（R）a的碳酸酯和/或氨基甲酸酯的酯，其中R 2独立地是H，C1- C 2 -C 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 -C 12烷基; X为N或O; R是独立的H，C 1 -C 12烷基，芳基，烯基，炔基，链烯基芳基，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，-O - ， - N = 4， - （R 4）2 - 或OR 3，R 4独立地是-H或C 1 -C 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OR <3>。该化合物可用作制备抗病毒化合物或寡核苷酸的中间体，或可用于直接给患者施用抗病毒治疗或预防。当口服给药时，实施方案特别有用。

3. 发明申请

WO1996001840A1 CATIONIC LIPIDS FOR DELIVERY OF NUCLEIC ACIDS TO CELLS 审中-公开
标题翻译：向细胞输送核酸的阳离子脂肪
公开(公告)号：WO1996001840A1
公开(公告)日：1996-01-25
申请号：PCT/US1995008555
申请日：1995-07-07
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , LIN, Kuei-Ying , LEWIS, Jason, G. , MATTEUCCI, Mark, D. , WAGNER, Richard, W.
IPC分类号： C07K05/06
CPC分类号： C07K5/06095 , A61K9/1272 , A61K38/00 , C07C237/06 , C07C237/20 , C07C237/22 , C07C271/22 , C07C279/14 , C07C279/22 , C07C279/24 , C07J41/0055 , C07K5/06086 , C12N15/88
摘要： The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two arginine, lysine or ornithine residues linked to a lipohilic moiety. The lipids form a composition when mixted with polyanions such as nucleic acids. The compositions permit efficient transfer of polyanions into cells without significant toxicity to the cells.
摘要翻译：本发明涉及其合成中的新的阳离子脂质和中间体，其可用于将核酸或肽转染到原核或真核细胞中。脂质包含一个或两个与亲水部分连接的精氨酸，赖氨酸或鸟氨酸残基。当与聚阴离子如核酸混合时，脂质形成组合物。组合物允许聚阴离子有效转移到细胞中，而对细胞没有显着的毒性。

4. 发明申请

WO1993012135A1 NUCLEASE STABLE AND BINDING COMPETENT OLIGOMERS AND METHODS FOR THEIR USE 审中-公开
标题翻译：核素稳定和结合的竞争性寡聚体及其使用方法
公开(公告)号：WO1993012135A1
公开(公告)日：1993-06-24
申请号：PCT/US1992010793
申请日：1992-12-11
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , SWAMINATHAN, Sundaramoorthi , JONES, Robert, J. , MATTEUCCI, Mark , MUNGER, John , PUDLO, Jeff
IPC分类号： C07H21/04
CPC分类号： C07H21/00 , C12Q1/6839
摘要： Oligomers are disclosed which have modified internucleotide linkages and can form triplex and duplex structures by binding to complementary nucleic acid sequences. The oligomers of the invention may be incorporated into pharmaceutically acceptable carriers and may be constructed to have any desired sequence. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.
摘要翻译：公开了寡核苷酸，其具有修饰的核苷酸间键，并且可以通过结合互补核酸序列形成三链体和双链体结构。本发明的寡聚体可以并入药学上可接受的载体中，并且可以构建成具有任何所需的序列。本发明的组合物可用作药剂以治疗各种疾病如病毒，并且可用于诊断目的以检测病毒或疾病状况。

5. 发明申请

WO1992014842A1 APTAMERS SPECIFIC FOR THROMBIN AND METHODS OF USE 审中-公开
标题翻译：适用于沙门氏菌的APTAMERS及其使用方法
公开(公告)号：WO1992014842A1
公开(公告)日：1992-09-03
申请号：PCT/US1992001367
申请日：1992-02-21
申请人： GILEAD SCIENCES, INC. , TOOLE, John, J. , GRIFFIN, Linda, C. , BOCK, Louis, C. , LATHAM, John, A. , KRAWCZYK, Steven
发明人： GILEAD SCIENCES, INC.
IPC分类号： C12Q01/68
CPC分类号： G01N33/86 , C12N15/111 , C12N15/115 , C12N2310/16 , C12N2310/315 , C12N2310/318 , C12N2310/33 , C12N2310/332 , C12N2310/335 , C12N2320/13 , G01N2333/974
摘要： Oligonucleotide sequences that mediate specific binding to thrombin and optionally contain modified bases, sugars, or sugar linkages are disclosed. Single-stranded DNA oligomers are obtained that bind thrombin and inhibit its function in vitro and in vivo. The thrombin binding oligomers are useful for therapeutic, diagnostic and manufacturing purposes. An improved method for identifying these oligomers is also described, involving complexation of the support-bound thrombin with a mixture of oligonucleotides containing random sequences under conditions wherein a complex is formed with the specifically binding sequences, but not with the other members of the oligonucleotide mixture. The thrombin-oligonucleotide complexes are then separated from both the support and the uncomplexed oligonucleotides and the complexed members of the oligonucleotide mixture are recovered from the separated complex and subsequently amplified using standard techniques.
摘要翻译：公开介导特异性结合凝血酶并任选地含有修饰的碱基，糖或糖键的寡核苷酸序列。获得结合凝血酶并在体外和体内抑制其功能的单链DNA寡聚体。凝血酶结合寡聚体可用于治疗，诊断和制造目的。还描述了用于鉴定这些寡聚体的改进方法，包括在其中使用特异性结合序列而不与寡核苷酸混合物的其它成员形成复合物的条件下使载体结合的凝血酶与含有随机序列的寡核苷酸的混合物络合。然后从载体和未复合的寡核苷酸中分离出凝血酶 - 寡核苷酸复合物，并从分离的复合物中回收寡核苷酸混合物的复合成员，随后使用标准技术扩增。

6. 发明申请

WO1992013869A1 METHYLENE PHOSPHONATE NUCLEOSIDE ANALOGS AND OLIGONUCLEOTIDE ANALOGS MADE THEREFROM 审中-公开
标题翻译：甲基磷酸核苷类似物和寡核苷酸类似物
公开(公告)号：WO1992013869A1
公开(公告)日：1992-08-20
申请号：PCT/US1992001020
申请日：1992-02-07
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , BUHR, Chris , MATTEUCCI, Mark , BISCHOFBERGER, Norbert, W. , FROEHLER, Brian
IPC分类号： C07H19/20
CPC分类号： C07H19/06 , C07H19/04 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： Oligonucleotide analogs and nucleoside analogs as well as methods for their synthesis are described. The nucleoside analogs are useful as antiviral agents and as agents to treat tumors or infectious agents. The oligonucleotides are useful in diagnostic and therapeutic applications.
摘要翻译：描述了寡核苷酸类似物和核苷类似物以及它们的合成方法。核苷类似物可用作抗病毒剂和用作治疗肿瘤或感染因子的药剂。寡核苷酸可用于诊断和治疗应用。

7. 发明申请

WO1998007685A1 PREPARATION OF CYCLOHEXENE CARBOXYLATE DERIVATIVES 审中-公开
标题翻译：环己基羧酸酯衍生物的制备
公开(公告)号：WO1998007685A1
公开(公告)日：1998-02-26
申请号：PCT/US1997014813
申请日：1997-08-22
申请人： GILEAD SCIENCES, INC. , KENT, Kenneth, M. , KIM, Choung, U. , MCGEE, Lawrence, R. , MUNGER, John, D. , PRISBE, Ernest, J. , POSTICH, Michael, J. , ROHLOFF, John, C. , ST. JOHN, Daphne, E. , WILLIAMS, Matthew, A. , ZHANG, Lijun
发明人： GILEAD SCIENCES, INC.
IPC分类号： C07C227/08
CPC分类号： C07D203/26 , C07C227/08 , C07C2601/16 , C07D303/40 , C07D317/46 , Y02P20/55
摘要： The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates such as those having formulas (I)-(IV), such as those having formulas (I)-(IV), useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
摘要翻译：本发明提供了新的合成方法和组合物。特别地，制备中间体的新方法如具有式（I） - （IV）的那些，例如具有式（I） - （IV）的那些，可用于神经氨酸酶抑制剂的合成和用作中间体的组合物本身有用的新方法提供神经氨酸酶抑制剂的合成。

8. 发明申请

WO1995007920A1 NUCLEOTIDE ANALOGS 审中-公开
标题翻译：核素类似物
公开(公告)号：WO1995007920A1
公开(公告)日：1995-03-23
申请号：PCT/US1994010539
申请日：1994-09-16
申请人： GILEAD SCIENCES, INC. , BISCHOFBERGER, Norbert, W. , JONES, Robert, J. , ARIMILLI, Murty, N. , LIN, Kuei-Ying , LOUIE, Michael, S. , MCGEE, Lawwrence, R. , PRISBE, Ernest, J. , LEE, William, A. , CUNDY, Kenneth, C.
发明人： GILEAD SCIENCES, INC.
IPC分类号： C07H19/10
CPC分类号： C07H19/20 , C07F9/6512 , C07F9/65616 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07F9/65785 , C07H11/00 , C07H19/10
摘要： Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolysed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for the synthesis and use are described.
摘要翻译：公开了以与磷酸酯核苷酸类似物的磷原子结合的氨基酸连接的氨基酸或酯连接基团的存在为特征的核苷酸类似物。类似物包含在体内水解产生相应的膦酸酯核苷酸类似物的磷酰胺化物或酯键。描述了合成和使用的方法和中间体。

9. 发明申请

WO1994004548A1 CHEMICALLY REVERSIBLE APTAMERS 审中-公开
标题翻译：化学可逆的APTAMERS
公开(公告)号：WO1994004548A1
公开(公告)日：1994-03-03
申请号：PCT/US1993007130
申请日：1993-07-29
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , BISCHOFBERGER, Norbert , FISHBACK, James, A.
IPC分类号： C07H21/00
CPC分类号： C07H19/10 , C07H19/20 , C07H21/00
摘要： New aptamers comprise at least one binding region capable of binding specifically to a target and at least one linking group wherein P(O)O or P(O)S is replaced by P(O)SR, wherein R is a substituted or unsubstituted C1-20 alkyl optionally containing an ether (-O-) linkage, aryl, alkenyl, cycloalkyl, cycloalkenyl, aryalkyl or (I) in which R1, R2, and R3 each is hydrogen or C1-9 alkyl, and Y is a bond, O, S or NH. The method for obtaining the aptamers includes a step of treating recovered aptamers with base to convert the hydrocarbyl thioate linkages to phosphodiester linkages thereby forming a dehydrocarbylated aptamer prior to amplification.
摘要翻译：新适体包含能够特异性结合靶和至少一个连接基团的至少一个结合区，其中P（O）O或P（O）S被P（O）SR替代，其中R是取代或未取代的C1 任选地含有醚（-O-）键，芳基，烯基，环烷基，环烯基，芳烷基或（Ⅰ）中的R 1，R 2和R 3各自为氢或C 1-8烷基，Y为键， O，S或NH。获得适体的方法包括用碱处理回收的适配子以将硫代酯键连接成磷酸二酯键，从而在扩增前形成脱氢化的适体。

10. 发明申请

WO1993007157A1 ANTIVIRAL ACYCLIC PHOSPHONOMETHOXYALKYL SUBSTITUTED, ALKENYL AND ALKYNYL PURINE AND PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：替代的ACYCLIC磷酸二羟基烷基取代的烷基和亚苄基嘌呤和吡嗪衍生物
公开(公告)号：WO1993007157A1
公开(公告)日：1993-04-15
申请号：PCT/US1992008686
申请日：1992-10-09
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , MARTIN, John, C. , BRONSON, Joanne, J. , YU, Kuo-Long
IPC分类号： C07F09/38
CPC分类号： C07F9/65616 , C07F9/6512
摘要： Disclosed are acyclic phosphonomethoxyalkyl substituted, alkenyl and alkynyl purine and pyrimidine derivatives and a pharmaceutical composition comprising said purine and pyrimidine derivatives. The compounds are useful in the treatment of viral infections, especially those caused by human immunodeficiency virus (HIV).
摘要翻译：公开了无环膦基甲氧基烷基取代的烯基和炔基嘌呤和嘧啶衍生物以及包含所述嘌呤和嘧啶衍生物的药物组合物。这些化合物可用于治疗病毒感染，特别是由人类免疫缺陷病毒（HIV）引起的病毒感染。

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