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51. 发明授权

US08563776B2 L-Threonine derivatives of high therapeutic index 有权
公开(公告)号：US08563776B2
公开(公告)日：2013-10-22
申请号：US12556968
申请日：2009-09-10
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： C07C229/00
CPC分类号： A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要： The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

52. 发明授权

US08563717B2 Adenine derivatives 有权
标题翻译：腺嘌呤衍生物
公开(公告)号：US08563717B2
公开(公告)日：2013-10-22
申请号：US13058465
申请日：2009-08-07
申请人： Helene Bazin-Lee , Diane Mary Coe , Linos Lazarides , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
发明人： Helene Bazin-Lee , Diane Mary Coe , Linos Lazarides , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
IPC分类号： A61K31/522 , A61P29/02 , A61P37/08 , C07D473/16
CPC分类号： C07D473/16 , A61K31/522 , C07D473/18
摘要： The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH2)n— moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是C 1-6烷基氨基或C 1-6烷氧基; R2是具有以下结构的基团：n是具有1至6的整数; Het是含有一个氮原子的6元饱和杂环，其中Het与杂环的任何碳原子连接至 - （CH 2）n - 部分; R3是氢，C1-8烷基或C3-7环烷基C0-6烷基; 其盐是人类干扰素的诱导剂。诱导人类干扰素的化合物可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，治疗感染性疾病和癌症，并且也可用作疫苗佐剂。

53. 发明申请

US20130197220A1 Morpholino Nucleic Acid Derivatives 有权
标题翻译：吗啉代核酸衍生物
公开(公告)号：US20130197220A1
公开(公告)日：2013-08-01
申请号：US13876194
申请日：2011-09-29
申请人： Toshihiro Ueda
发明人： Toshihiro Ueda
IPC分类号： C07D473/18
CPC分类号： C07D473/18 , C07F9/65583 , C07F9/65616
摘要： The present invention provides a useful morpholino nucleic acid derivative for synthesizing a morpholino nucleic acid oligomer. The present invention provides a compound represented by the following general formula (1) or a salt thereof. Here, R1 represents hydrogen, trityl and so on. R2 represents an amide or an imine. R3 represents a hydroxy group which may be protected by trialkylsilyl and so on, or a group represented by the following general formula (5): (wherein X represents O or S, Y represents dialkylamino or alkoxy, and Z represents chlorine).
摘要翻译：本发明提供了用于合成吗啉代核酸低聚物的有用的吗啉代核酸衍生物。本发明提供由下述通式（1）表示的化合物或其盐。这里，R 1表示氢，三苯甲基等。 R2代表酰胺或亚胺。 R3表示可被三烷基甲硅烷基等保护的羟基或由以下通式（5）表示的基团：（其中X表示O或S，Y表示二烷基氨基或烷氧基，Z表示氯）。

54. 发明申请

US20130157973A1 PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING GASTROINTESTINAL INFECTIONS AND DISORDERS 审中-公开
标题翻译：药物组合物和治疗胃肠道感染和疾病的方法
公开(公告)号：US20130157973A1
公开(公告)日：2013-06-20
申请号：US13720968
申请日：2012-12-19
申请人： Gilead Sciences, Inc.
发明人： Uri Aryeh Lopatin , Daniel B. Tumas
IPC分类号： C07D475/06 , A61K31/522 , A61K45/06 , A61K31/7072 , A61K31/52 , C07D473/18
CPC分类号： C07D475/06 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/675 , A61K31/7068 , A61K31/7072 , A61K45/06 , C07D473/18 , Y02A50/409 , Y02A50/411 , Y02A50/423 , A61K2300/00
摘要： Methods of treating gastrointestinal disorders, in a patient in need thereof, including disorders of the liver and pancreas, using an amount of an orally dosed TLR-7 compound in an amount sufficient to increase IFN in the gastrointestinal area, including the liver, but not significantly increasing systemic IFN.
摘要翻译：在有需要的患者中治疗胃肠道疾病的方法，包括肝脏和胰腺的病症，使用一定量的经口给药的TLR-7化合物，其量足以增加包括肝脏在内的胃肠道区域中的IFN而不是显着增加全身性IFN。

55. 发明申请

US20130144058A1 PROCESS FOR THE SYNTHESIS OF CARBONUCLEOSIDE AND INTERMEDIATES FOR USE THEREIN 有权
标题翻译：合成碳水化合物及其使用的中间体的方法
公开(公告)号：US20130144058A1
公开(公告)日：2013-06-06
申请号：US13700259
申请日：2011-05-30
申请人： Dino Alberico , Joshua Clayton , Craig Dixon , Boris Gorin
发明人： Dino Alberico , Joshua Clayton , Craig Dixon , Boris Gorin
IPC分类号： C07D473/02 , C07H19/16 , C07D473/18 , A61K31/522
CPC分类号： C07H19/16 , C07D319/08 , C07D473/18 , C07D493/04 , Y02P20/55
摘要： Disclosed is a process for preparing a carbonucleoside of formula (1) and intermediates for use therein. The process involves the step of reacting a compound of formula (2) with a compound of formula (3) under Mitsunobu-type reaction conditions to obtain a compound of formula (4), wherein PG1, PG2, PG3 and PG4 are protecting groups. The compound of formula (4) is deprotected to form the compound of formula (1), as shown below.
摘要翻译：公开了制备式（1）的核苷和其中使用的中间体的方法。该方法包括在Mitsunobu型反应条件下使式（2）化合物与式（3）化合物反应的步骤，得到式（4）化合物，其中PG1，PG2，PG3和PG4是保护基。将式（4）的化合物脱保护以形成式（1）的化合物，如下所示。

56. 发明授权

US08324381B2 Preparation of ester of purine derivatives 有权
标题翻译：嘌呤衍生物的酯的制备
公开(公告)号：US08324381B2
公开(公告)日：2012-12-04
申请号：US11725681
申请日：2007-03-20
申请人： Dharmaraj Ramachandra Rao , Rajendra Narayanrao Kankan , Vidyadhar Purushottam Pande
发明人： Dharmaraj Ramachandra Rao , Rajendra Narayanrao Kankan , Vidyadhar Purushottam Pande
IPC分类号： C07D473/18
CPC分类号： C07D473/18
摘要： A process for the preparation of valganciclovir with triacetyl ganciclovir (V) as a starting material, comprising the following steps: selective hydrolysis, reacting with a coupling agent and CBZ valine and a solvent, followed by hydrolysis under basic conditions and hydrogenolysis in the presence of a catalyst.
摘要翻译：用三乙酰基更昔洛韦（V）作为起始原料制备缬更昔洛韦的方法，包括以下步骤：选择性水解，与偶联剂和CBZ缬氨酸和溶剂反应，然后在碱性条件下水解，并在催化剂

57. 发明申请

US20120289471A1 NOVEL COMPOUNDS WITH HIGH THERAPEUTIC INDEX 审中-公开
标题翻译：具有高效治疗指数的新型化合物
公开(公告)号：US20120289471A1
公开(公告)日：2012-11-15
申请号：US13449791
申请日：2012-04-18
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： C07K7/64 , A61K31/702 , A61K38/13 , C07D499/68 , A61K31/43 , C07H17/08 , A61K31/7048 , C07C229/36 , A61K31/223 , C07D207/16 , A61K31/401 , C07C69/612 , A61K31/24 , C07C69/757 , A61K31/215 , A61K31/616 , C07D491/16 , A61K31/436 , C07D495/04 , A61K31/4365 , C07J71/00 , A61K31/58 , A61P29/00 , A61P37/06 , C07H15/203
CPC分类号： A61K38/12 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616 , Y02A50/411
摘要： The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译：本发明涉及由与其上具有羟基，氨基，羧基或酰化衍生物的药物或药物结合的氨基酸组成的新型治疗化合物。这些高治疗指数衍生物与其制备的药物具有相同的效用，并且它们具有增强的药理学和药物性质。事实上，本发明的新型药物衍生物增强至少一种如本文所定义的治疗质量。本发明还涉及含有其的药物组合物。

58. 发明授权

US08232275B2 2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and -pyrimidines as antiviral agents 有权
标题翻译：作为抗病毒剂的2,2-双 - （羟甲基）环丙烯甲基 - 嘌呤和嘧啶
公开(公告)号：US08232275B2
公开(公告)日：2012-07-31
申请号：US13183722
申请日：2011-07-15
申请人： Jiri Zemlicka , Shaoman Zhou , John C. Drach
发明人： Jiri Zemlicka , Shaoman Zhou , John C. Drach
IPC分类号： C07D239/52 , A61K31/505
CPC分类号： C07D239/36 , C07D239/54 , C07D473/18 , C07D473/30 , C07D473/34 , C07D473/40
摘要： Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
摘要翻译：对病毒有活性的化合物具有下式：其中B是嘌呤或嘧啶杂环或碱基。在优选的实施方案中，嘌呤包括6-氨基嘌呤（腺嘌呤），6-羟基嘌呤（次黄嘌呤），2-氨基-6-羟基嘌呤（鸟嘌呤），2,6-二氨基嘌呤，2-氨基-6-叠氮基嘌呤，2 2-氨基-6-卤代嘌呤如2-氨基-6-氯嘌呤，2-氨基-6-氟嘌呤，2-氨基-6-烷氧基嘌呤如2-氨基-6-甲氧基嘌呤，2-氨基-6-环丙基氨基嘌呤 2-氨基-6-烷基氨基或2-氨基-6-二烷基氨基取代的嘌呤，2-氨基-6-硫嘌呤，2-氨基-6-烷硫基取代的嘌呤，3-脱氮嘌呤，7-脱氮嘌呤和8-氮杂嘌呤。嘧啶含有胞嘧啶，尿嘧啶和胸腺嘧啶，5-卤素取代的胞嘧啶和尿嘧啶，5-烷基取代的胞嘧啶和尿嘧啶，包括具有饱和或不饱和烷基的衍生物和6-氮杂嘧啶。

59. 发明申请

US20120135951A1 3'-AZIDO PURINE NUCLEOTIDE PRODRUGS FOR TREATMENT OF VIRAL INFECTIONS 有权
标题翻译：用于治疗病毒感染的3'-AZIDO PURINE NUCLEOTIDE PRODRUGS
公开(公告)号：US20120135951A1
公开(公告)日：2012-05-31
申请号：US13132920
申请日：2009-12-09
申请人： Raymond F. Schinazi, Ph.D. , John W. Mellors , Nicolas Paul Sluis-Cremer , Steven J. Coats, Ph.D. , Richard Anthony Whitaker , Brian David Herman , Jong Hyun Cho , Longhu Zhou , Hongwang Zhang
发明人： Raymond F. Schinazi, Ph.D. , John W. Mellors , Nicolas Paul Sluis-Cremer , Steven J. Coats, Ph.D. , Richard Anthony Whitaker , Brian David Herman , Jong Hyun Cho , Longhu Zhou , Hongwang Zhang
IPC分类号： A61K31/7076 , A61P31/18 , A61P31/20 , C07H19/207
CPC分类号： C07D473/34 , A61K31/437 , C07D473/16 , C07D473/18 , C07H19/173 , C07H19/20 , C07H19/207
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, and HBV, in human patients or other animal hosts. The compounds are 3′-azido-2′,3′-dideoxy purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 and HBV.
摘要翻译：本发明涉及在人类患者或其他动物宿主中用于治疗或预防病毒感染，特别是HIV和HBV的化合物，组合物和方法。化合物是3'-叠氮基-2'，3'-二脱氧嘌呤单磷酸酯及其药学上可接受的盐，前药和其它衍生物。特别地，这些化合物对HIV-1和HBV显示出有效的抗病毒活性。

60. 发明申请

US20110306610A1 9-SUBSTITUTED 8-OXOADENINE COMPOUND 有权
标题翻译： 9-取代的8-氧杂环丁烯化合物
公开(公告)号：US20110306610A1
公开(公告)日：2011-12-15
申请号：US13187260
申请日：2011-07-20
申请人： Ayumu KURIMOTO , Kazuki Hashimoto , Yoshiaki Isobe , Stephen Brough , Ian Millichip , Hiroki Wada , Roger Bonnert , Thomas Mcinally
发明人： Ayumu KURIMOTO , Kazuki Hashimoto , Yoshiaki Isobe , Stephen Brough , Ian Millichip , Hiroki Wada , Roger Bonnert , Thomas Mcinally
IPC分类号： A61K31/522 , C07D413/14 , A61P37/08 , A61P37/00 , A61P31/12 , A61P35/00 , C07D473/18 , A61K31/5377
CPC分类号： C07D473/18 , A61K31/522 , A61K31/5377
摘要： The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.
摘要翻译：本发明提供具有免疫调节活性的8-氧代腺嘌呤化合物，例如干扰素诱导活性，可用作抗病毒剂和抗变应性剂，其由下式（1）表示：[其中环A表示6-10元芳香族碳环等，R表示卤素原子，烷基等，n表示0-2的整数，Z1表示亚烷基，X2表示氧原子，硫原子，SO2，NR5，CO，CONR5，NR5CO 等等，Y1，Y2和Y3独立地表示单键或亚烷基，X1表示氧原子，硫原子，NR4（R4是氢原子或烷基）或单键，R2表示取代或未取代的烷基基团，R 1表示氢原子，羟基，烷氧基，烷氧基羰基或卤代烷基]或其药学上可接受的盐。

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