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1. 发明专利

JP2014159450A Nucleotide analogs 审中-公开
标题翻译：核素类似物
公开(公告)号：JP2014159450A
公开(公告)日：2014-09-04
申请号：JP2014083387
申请日：2014-04-15
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： ARIMILLI MURTY N , CUNDY KENNETH C , DOUGHERTY JOSEPH P , KIM CHOUNG U , OLIYAI REZA , STELLA VALENTINO J
IPC分类号： A61K31/663 , C07F9/6561 , A61K31/662 , A61K31/675 , A61P31/12 , A61P43/00 , C07F9/6512
CPC分类号： C07F9/65616 , C07F9/65121
摘要： PROBLEM TO BE SOLVED: To provide antiviral phosphonomethoxy nucleotide analogs and intermediates therefor useful for efficient oral delivery.SOLUTION: The phosphonomethoxy nucleotide analogs are represented by the specified formula (5) or the like.
摘要翻译：要解决的问题：提供用于有效口服递送的抗病毒膦酰基甲氧基核苷酸类似物及其中间体。解决方案：膦甲氧基核苷酸类似物由指定的式（5）等表示。

2. 发明专利

JP2009263389A Nucleotide analog compound 审中-公开
标题翻译：核苷类似物化合物
公开(公告)号：JP2009263389A
公开(公告)日：2009-11-12
申请号：JP2009157357
申请日：2009-07-01
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： ARIMILLI MURTY N , LEE THOMAS T K , MANES LAWRENCE V , MUNGER JOHN D JR , PRISBE ERNEST J , SCHULTZE LISA M , KELLY DAPHNE E
IPC分类号： C07F9/6561 , A61K31/662 , A61K31/675 , A61P31/12 , A61P31/14 , A61P31/18 , A61P31/20 , A61P31/22 , C07F9/6524
CPC分类号： A61K31/675 , C07F9/65616
摘要： PROBLEM TO BE SOLVED: To provide: compositions comprising adefovir dipivoxil (AD) of a new form having desirable properties for large scale synthesis or for formulation into therapeutic dosages; AD having good melting point, and/or flow or bulk density properties, which facilitate manufacturing and formulating compositions containing AD; a storage-stable form of AD; AD which can be readily filtered and easily dried; highly purified AD having at least about a 97% (w/w) purity and preferably at least about 98%; to eliminate or minimize by-products made during AD synthesis; and a method for purifying AD that avoids expensive and time-consuming column chromatography. SOLUTION: Crystalline adefovir dipivoxil is produced by crystallization of a crude product with di-n-butyl ether. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供：包含具有用于大规模合成或配制成治疗剂量的所需性质的新形式的阿德福韦酯（AD）的组合物; AD具有良好的熔点和/或流动或体积密度特性，其有利于制造和配制含有AD的组合物; AD的储存稳定形式; AD易于过滤并容易干燥; 具有至少约97％（w / w）纯度，优选至少约98％的高度纯化的AD; 消除或最小化AD合成过程中产生的副产物; 以及用于纯化AD的方法，其避免昂贵且耗时的柱色谱法。解决方案：结晶阿德福韦酯通过粗产物与二正丁基醚的结晶来制备。版权所有（C）2010，JPO＆INPIT

3. 发明专利

JP2005306879A Nucleotide analog compound 审中-公开
标题翻译：核苷类似物化合物
公开(公告)号：JP2005306879A
公开(公告)日：2005-11-04
申请号：JP2005145754
申请日：2005-05-18
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： ARIMILLI MURTY N , LEE THOMAS T K , MANES LAWRENCE V , MUNGER JOHN D JR , PRISBE ERNEST J , SCHULTZE LISA M , KELLY DAPHNE E
IPC分类号： A61K31/675 , A61P31/12 , A61P31/14 , A61P31/18 , A61P31/20 , A61P31/22 , C07F9/6524 , C07F9/6561
CPC分类号： A61K31/675 , C07F9/65616
摘要： PROBLEM TO BE SOLVED: To provide a composition containing 9-[2-[[bis[(pivaloyloxy)-methoxy]phosphinyl]methoxy]ethyl]adenine (adefovir dipivoxil; hereinafter referred to as AD) in a new form, having desirable properties for large-scale synthesis or for its formulation into therapeutic administration, to provide the AD having a good melting point, and/or a fluidity characteristic, or a bulk density characteristic for making it easy to produce the composition containing the AD and to formulate the composition, having a form fit to be stably stored, and capable of being rapidly filtered and easily dried, to provide the high-purity AD having a purity of at least about 97 (w/w)%, and preferably, having a purity of at least about 98 (w/w)%, and to provide a method for purifying the AD, capable of removing or minimizing a by-product produced during the synthesis of the AD, without using gas chromatography which is expensive and consumes time. SOLUTION: This crystalline AD has forms as follows: an anhydrous crystal form; a hydrate-type form; a methanol solvate-type form; a fumaric acid salt thereof; and a complex thereof. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：为了提供新形式的含有9- [2 - [[二[（新戊酰氧基） - 甲氧基]氧膦基]甲氧基]乙基]腺嘌呤（阿德福韦酯;以下称为AD）的组合物，具有用于大规模合成或其制剂治疗性施用的所需性质，以提供具有良好熔点，和/或流动性特征或体积密度特性的AD，以使得容易地制备含有AD和以配制具有适于稳定储存的形式并能够快速过滤并容易干燥的组合物，以提供纯度至少为约97（w / w）％的高纯度AD，优选具有纯度为至少约98（w / w）％，并且提供能够除去或最小化AD合成期间产生的副产物的AD的纯化方法，而不使用昂贵的并且消耗的气相色谱时间。解决方案：该结晶AD具有以下形式：无水晶形; 水合型形式; 甲醇溶剂合物型; 其富马酸盐; 及其复合物。版权所有（C）2006，JPO＆NCIPI

4. 发明专利

JP2011016847A Nucleotide analog 审中-公开
标题翻译：核素模拟
公开(公告)号：JP2011016847A
公开(公告)日：2011-01-27
申请号：JP2010233086
申请日：2010-10-15
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： ARIMILLI MURTY N , CUNDY KENNETH C , DOUGHERTY JOSEPH P , KIM CHOUNG U , OLIYAI REZA , STELLA VALENTINO J
IPC分类号： A61K31/663 , C07F9/6561 , A61K31/675 , A61P31/12 , A61P31/18 , C07F9/6512
CPC分类号： C07F9/65616 , C07F9/65121
摘要： PROBLEM TO BE SOLVED: To provide intermediates for phosphonomethoxy nucleotide analogs, particularly intermediates useful for efficient oral administration of these analogs.SOLUTION: Novel compounds comprising esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure of -OC(R)OC(O)X(R), wherein Rcomplies with a specific definition, 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.
摘要翻译：要解决的问题：提供膦甲氧基核苷酸类似物的中间体，特别是可用于有效口服这些类似物的中间体。解决方案：包含具有-OC（R）结构的具有碳酸酯和/或氨基甲酸酯的抗病毒膦基甲氧基核苷酸类似物的酯的新型化合物其中具有特定定义的R（O）X（R）可用作制备抗病毒化合物或寡核苷酸的中间体，或可用于直接给予患者进行抗病毒治疗或预防。

5. 发明专利

JP2006290898A Nucleotide analogs 审中-公开
标题翻译：核素类似物
公开(公告)号：JP2006290898A
公开(公告)日：2006-10-26
申请号：JP2006159159
申请日：2006-06-07
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： BISCHOFBERGER NORBERT W , JONES ROBERT J , ARIMILLI MURTY N , LIN KUEI-YING , LOUIE MICHAEL S , MCGEE LAWRENCE R , PRISBE ERNEST J , LEE WILLIAM A , CUNDY KENNETH C
IPC分类号： C07D239/47 , C07F9/547 , A61K31/66 , A61K31/662 , A61K31/664 , A61K31/665 , A61K31/67 , A61K31/685 , A61K31/70 , A61K38/00 , A61K49/00 , A61P27/02 , A61P31/12 , A61P33/02 , A61P35/00 , C07F9/553 , C07F9/58 , C07F9/6512 , C07F9/6518 , C07F9/653 , C07F9/6533 , C07F9/6539 , C07F9/6558 , C07F9/6561 , C07F9/6571 , C07F9/6574 , C07F9/6578 , C07F9/6584 , C07H11/04 , C07H19/10 , C07H19/20 , C07J9/00 , C07K2/00 , G01N33/53
CPC分类号： C07F9/65785 , C07F9/65121 , C07F9/65616 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/10 , C07H19/20
摘要： PROBLEM TO BE SOLVED: To provide a compound of formula I, wherein L 1 and L 2 are each independently an amino acid or polypeptide residue bound to the phosphorus atom of the compound through an amidate bond, or an oxyester, a thioester, a substituted or un-substituted amine, or OH, but one or both of L 1 and L 2 are amino acids or polypeptide residues; and a carboxyl group bound to amidate N with five or less atoms is esterified or amidated, and the stereoisomer or salt of the compound, to provide their production method, and to provide their uses. SOLUTION: The compound of formula I, and the stereoisomer or salt of the compound, their production methods, and their uses are provided. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：待解决的问题：为了提供式I化合物，其中L 1 和L 2 各自独立地是与磷原子结合的氨基酸或多肽残基化合物通过酰胺键，或氧酯，硫酯，取代或未取代的胺或OH，但L SP 1和/或SP 2中的一个或两个是氨基酸或多肽残基; 并且与五个或更少原子结合的酰胺化N的羧基被酯化或酰胺化，并且化合物的立体异构体或盐，以提供其制备方法并提供其用途。解决方案：提供了式I化合物，化合物的立体异构体或盐，其制备方法及其用途。版权所有（C）2007，JPO＆INPIT

6. 发明专利

JP2007297406A Nucleotide analog 审中-公开
标题翻译：核素模拟
公开(公告)号：JP2007297406A
公开(公告)日：2007-11-15
申请号：JP2007180398
申请日：2007-07-09
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： ARIMILLI MURTY N , CUNDY KENNETH C , DOUGHERTY JOSEPH P , KIM CHOUNG U , OLIYAI REZA , STELLA VALENTINO J
IPC分类号： A61K31/663 , C07F9/6561 , A61K31/675 , A61P31/12 , A61P31/14 , A61P31/18 , A61P43/00 , C07F9/6512
CPC分类号： C07F9/65616 , C07F9/65121
摘要： PROBLEM TO BE SOLVED: To provide an intermediate for a phosphonomethoxy nucleotide analogue, especially the intermediate suitable for the use in the efficient oral delivery of such the analogue. SOLUTION: The compound is a new compound containing an ester of an antiviral phosphonomethoxy nucleotide analogue with a carbonate and/or carbamate having a structure: -OC(R 2 ) 2 OC(O)X(R) a . The compound is useful as an intermediate for preparing an antiviral compound or an oligonucleotide, and also useful for direct administration to a patient for antiviral treatment or prevention. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供膦甲氧基核苷酸类似物的中间体，特别是适合用于有效口服递送这种类似物的中间体。解决方案：该化合物是含有具有以下结构的具有以下结构的碳酸酯和/或氨基甲酸酯的抗病毒膦基甲氧基核苷酸类似物的酯的新化合物：-OC（R 2 SP 2） SB> OC（O）X（R）一。该化合物可用作制备抗病毒化合物或寡核苷酸的中间体，并且也可用于直接施用于患者以进行抗病毒治疗或预防。版权所有（C）2008，JPO＆INPIT

7. 发明专利

JP2006306882A Nucleotide analog 审中-公开
标题翻译：核素模拟
公开(公告)号：JP2006306882A
公开(公告)日：2006-11-09
申请号：JP2006159160
申请日：2006-06-07
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： BISCHOFBERGER NORBERT W , JONES ROBERT J , ARIMILLI MURTY N , LIN KUEI-YING , LOUIE MICHAEL S , MCGEE LAWRENCE R , PRISBE ERNEST J , LEE WILLIAM A , CUNDY KENNETH C
IPC分类号： C07D239/47 , C07F9/6524 , A61K31/66 , A61K31/665 , A61K31/67 , A61K31/675 , A61K31/685 , A61K31/70 , A61K31/7076 , A61K38/00 , A61K49/00 , A61P27/02 , A61P31/12 , A61P31/18 , A61P31/22 , A61P33/02 , A61P35/00 , C07F9/547 , C07F9/553 , C07F9/58 , C07F9/6512 , C07F9/6518 , C07F9/653 , C07F9/6533 , C07F9/6539 , C07F9/6558 , C07F9/6561 , C07F9/6571 , C07F9/6574 , C07F9/6578 , C07F9/6584 , C07H11/04 , C07H19/10 , C07H19/16 , C07H19/20 , C07J9/00 , C07K2/00 , G01N33/53
CPC分类号： C07F9/65785 , C07F9/65121 , C07F9/65616 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/10 , C07H19/20
摘要： PROBLEM TO BE SOLVED: To provide a new nucleotide analog exhibiting an antitumor/antineoplastic activity, an antimicrobial activity of a wide spectrum and other desired activities. SOLUTION: The invention provides a compound of formula: B-Z-PO(-L 1 )-L 2 wherein -Z- is exemplified by -CH 2 -O-CH 2 -CH 2 -; B is exemplified by adenin-9-yl; and L 1 and L 2 are each exemplified by -NHCH(CH 3 )-CO(O)OCH 2 C 6 H 5 , and a stereoisomer and salt of the compound, a method for producing the compound, etc., and use of the compound, etc. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：待解决的问题：提供具有抗肿瘤/抗肿瘤活性的新型核苷酸类似物，具有广谱和其它所需活性的抗微生物活性。解决方案：本发明提供了一种下列化合物：BZ-PO（-L-SB> 1-SB）-L SB 2，其中-Z-的例子为-CH 2 -O-CH 2 -CH 2 - ; B是腺嘌呤-9-基; 和L 1 和L 2 各自以-NHCH（CH 3 SB 3）-CO（O）OCH 2 SB SB 化合物的立体异构体和盐，化合物的制备方法等，以及该化合物的用途等。版权所有（C）2007，JPO＆INPIT

8. 发明专利

JP2006182779A Nucleotide analog 审中-公开
标题翻译：核素模拟
公开(公告)号：JP2006182779A
公开(公告)日：2006-07-13
申请号：JP2005361122
申请日：2005-12-14
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： BISCHOFBERGER NORBERT W , JONES ROBERT J , ARIMILLI MURTY N , LIN KUEI-YING , LOUIE MICHAEL S , MCGEE LAWRENCE R , PRISBE ERNEST J , LEE WILLIAM A , CUNDY KENNETH C
IPC分类号： C07D239/47 , C07F9/6574 , A61K31/66 , A61K31/665 , A61K31/67 , A61K31/675 , A61K31/685 , A61K31/70 , A61K38/00 , A61K49/00 , A61P27/02 , A61P31/12 , A61P33/02 , A61P35/00 , C07F9/547 , C07F9/553 , C07F9/58 , C07F9/6512 , C07F9/6518 , C07F9/653 , C07F9/6533 , C07F9/6539 , C07F9/6558 , C07F9/6561 , C07F9/6571 , C07F9/6578 , C07F9/6584 , C07H11/04 , C07H19/10 , C07H19/20 , C07J9/00 , C07K2/00 , G01N33/53
CPC分类号： C07F9/65785 , C07F9/65121 , C07F9/65616 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/10 , C07H19/20
摘要： PROBLEM TO BE SOLVED: To provide a nucleotide analog compound having antiviral activity. SOLUTION: A compound represented by formula Ib, its stereoisomer and salt have antiviral activity (wherein, X 1 indicates O or S; # indicates a carbon having optical activity; B indicates a residue of a nucleic acid base; and L 1 indicates a group such as alkoxycarbonylmethoxy and acylmethoxy). COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供具有抗病毒活性的核苷酸类似物化合物。解决方案：由式Ib表示的化合物，其立体异构体和盐具有抗病毒活性（其中，X 1 表示O或S;＃表示具有光学活性的碳; B表示核酸碱基; L 1 表示烷氧基羰基甲氧基和酰基甲氧基等基团）。版权所有（C）2006，JPO＆NCIPI

9. 发明专利

JP2003342283A Nucleotide analogue compound 有权
标题翻译：核苷类似物化合物
公开(公告)号：JP2003342283A
公开(公告)日：2003-12-03
申请号：JP2003148228
申请日：2003-05-26
申请人： Gilead Sciences Inc , ギリアードサイエンシーズ, インコーポレイテッド
发明人： ARIMILLI MURTY N , LEE THOMAS T K , MANES LAWRENCE V , MUNGER JOHN D JR , PRISBE ERNEST J , SCHULTZE LISA M , KELLY DAPHNE E
IPC分类号： A61K31/675 , A61P31/12 , A61P31/14 , A61P31/18 , A61P31/20 , A61P31/22 , C07F9/6524 , C07F9/6561
CPC分类号： A61K31/675 , C07F9/65616
摘要： PROBLEM TO BE SOLVED: To obtain adefovir dipivoxil (AD) having a good melting point and/or flow characteristics or density characteristics for facilitating the production and formulation of a composition containing the AD, having a stable form for its storage, immediately filtrable and easily dried, having at least approximately 97% (wt/wt) purity, preferably at least approximately 98% purity, a composition containing a new form AD having a desirable properties for a large scale synthesis or the formulation for a therapeutic administration, and a method for purifying capable of removing or minimizing byproducts produced during the AD synthesis and not using a column chromatography which is expensive and time consuming. SOLUTION: The composition contains the crystalline adefovir dipivoxil. COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：为了获得具有良好熔点和/或流动特性或密度特性的阿德福韦酯（AD），用于促进含有AD的组合物的生产和配制，其具有稳定的储存形式，立即可过滤并易于干燥，具有至少约97％（wt / wt）纯度，优选至少约98％的纯度，包含具有用于大规模合成或用于治疗性给药的制剂的期望性质的新型AD的组合物，以及能够除去或最小化在AD合成期间产生的副产物并且不使用昂贵且耗时的柱色谱的纯化方法。
解决方案：组合物含有结晶阿德福韦酯。版权所有（C）2004，JPO

10. 发明申请

WO9904774A3 NUCLEOTIDE ANALOG COMPOSITIONS 审中-公开
标题翻译：核苷类似物组合物
公开(公告)号：WO9904774A3
公开(公告)日：1999-04-15
申请号：PCT/US9815304
申请日：1998-07-23
申请人： GILEAD SCIENCES INC , ARIMILLI MURTY N , LEE THOMAS T K , MANES LAWRENCE V , MUNGER JOHN D JR , PRISBE ERNEST J , SCHULTZE LISA M , KELLY DAPHNE E
发明人： ARIMILLI MURTY N , LEE THOMAS T K , MANES LAWRENCE V , MUNGER JOHN D JR , PRISBE ERNEST J , SCHULTZE LISA M , KELLY DAPHNE E
IPC分类号： A61K31/675 , A61P31/12 , A61P31/14 , A61P31/18 , A61P31/20 , A61P31/22 , C07F9/6524 , C07F9/6561
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：本发明提供了阿德福韦酯的结晶形式和制备晶体的方法。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配制成治疗剂量的理想特性。发明组合物包括阿德福韦酯的无水晶形。

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