专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5336764A 2'-fluorofuranosyl derivatives and novel method of preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides 失效
标题翻译： 2'-氟代呋喃糖苷衍生物和制备2'-氟嘧啶和2'-氟嘌呤核苷的新方法
公开(公告)号：US5336764A
公开(公告)日：1994-08-09
申请号：US968567
申请日：1992-10-29
申请人： Victor E. Marquez , John S. Driscoll , Ronald J. Wysocki, Jr. , Maqbool A. Siddiqui
发明人： Victor E. Marquez , John S. Driscoll , Ronald J. Wysocki, Jr. , Maqbool A. Siddiqui
IPC分类号： C07H1/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/18 , C07H13/08 , C07H15/04 , C07H15/203 , C07H19/06 , C07H19/10 , C07H19/16 , C07H23/00 , C07G3/00
CPC分类号： C07H23/00 , C07H19/10 , C07H19/16
摘要： A compound has the formula ##STR1## wherein R is selected from the group consisting of (C.sub.7 -C.sub.20)aroyl, (C.sub.6 -C.sub.20)aryl, aralkyl and alkylaryl, and (C.sub.1 -C.sub.10)alkyl-di(C.sub.6 -C.sub.20)aryl Si, R' is selected from the group consisting of (C.sub.1 -C.sub.10)alkyl, (C.sub.7 -C.sub.20)aroyl and (C.sub.2 -C.sub.12)acyl, all of which may be further substituted with O, S, N or alkyl, and R'" is selected from the group consisting of halogen, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)acyloxy, O-methane-sulfonyl and O-p-toluenesulfonyl. A composition of matter comprises 0.001 to 99.999 wt % of the above compound.
摘要翻译：化合物具有下式（IMAGE），其中R选自（C 7 -C 20）芳酰基，（C 6 -C 20）芳基，芳烷基和烷芳基，和（C 1 -C 10）烷基 - 二（C 6 -C 20）芳基 Si，R'选自（C 1 -C 10）烷基，（C 7 -C 20）芳酰基和（C 2 -C 12）酰基，所有这些可以进一步被O，S，N或烷基取代，R “选自卤素，（C 1 -C 10）烷氧基，（C 1 -C 10）酰氧基，O-甲磺酰基和对甲苯磺酰基。物质组合物含有0.001〜99.999重量％的上述化合物。

2. 发明授权

US5817799A 2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides 失效
标题翻译： 2'-氟呋喃糖苷衍生物及其制备方法2'-氟嘧啶核苷和2'-氟嘌呤核苷
公开(公告)号：US5817799A
公开(公告)日：1998-10-06
申请号：US556713
申请日：1990-07-23
申请人： Victor E. Marquez , John S. Driscoll , Ronald J. Wysocki, Jr. , Magbool A. Siddiqui
发明人： Victor E. Marquez , John S. Driscoll , Ronald J. Wysocki, Jr. , Magbool A. Siddiqui
IPC分类号： C07H1/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/18 , C07H13/08 , C07H15/04 , C07H15/203 , C07H19/06 , C07H19/10 , C07H19/16 , C07H23/00
CPC分类号： C07H23/00 , C07H19/10 , C07H19/16
摘要： A method of preparing a 2'-fluoro compound of the formula ##STR1## where B is selected from the group consisting of purines and pyrimidines, both of which may be substituted, comprises reacting a compound of the formula II(a) or II(b) ##STR2## where R and R' are as defined in the specification with an acid halide under conditions effective to obtain a halide of the formula ##STR3## where X is a halogen. A silane of the formula B-Si (R").sub.3 where R" is as defined in the specification, is added to this product (III) under conditions effective to obtain a compound of the formula (IV) ##STR4## The compound of formula (IV) is reacted with a reagent selected from the group consisting of ammonia, BCl.sub.3 and ((C.sub.1 -C.sub.10)alkyl).sub.4 NF, under conditions effective to obtain the compound of formula (I). The compounds of formula (I) resulting from these methods exhibit anti-HIV activities and are useful for therapy against the HIV virus.
摘要翻译：制备式（I）的2'-氟化合物的方法，其中B选自嘌呤和嘧啶，它们都可以被取代，包括使式II（a）的化合物与式（IIa）（IIb）其中R和R'如本说明书中所定义，与有效得到式（III）的卤化物的条件下的酰卤相同，其中X 是卤素。在有效获得式（IV）化合物的条件下，将式B-Si（R“）3的硅烷（其中R”如说明书中所定义）加入到该产物（III）中 IV）在有效获得式（I）化合物的条件下，使式（IV）化合物与选自氨，BCl 3和（（C 1 -C 10）烷基）4 NF的试剂反应。由这些方法得到的式（I）化合物表现出抗HIV活性，可用于治疗HIV病毒。

3. 发明授权

US4275057A Seven-membered ring compounds as inhibitors of cytidine deaminase 失效
标题翻译：七元环化合物作为胞苷脱氨酶的抑制剂
公开(公告)号：US4275057A
公开(公告)日：1981-06-23
申请号：US115900
申请日：1980-01-28
申请人： Victor E. Marquez , Paul S. Liu , John S. Driscoll
发明人： Victor E. Marquez , Paul S. Liu , John S. Driscoll
IPC分类号： C12N9/99 , C07D243/04 , C07D491/10 , C07D491/113 , C07D495/10 , C07H1/00 , C07H19/04 , C07H19/052 , A61K31/70 , C07H17/02
CPC分类号： C07D491/10 , C07D243/04 , C07D495/10 , C07H19/04 , C07H19/052
摘要： Seven-membered heterocyclic nucleosides used to inhibit the deamination enzyme responsible for the inactivation of arabinosylcytosine (ara--C). Preferred nucleosides containing a seven-member aglycone are as follows: ##STR1## Preferred aglycones are as follows: ##STR2## Active components utilized against pyrimidine deaminases from mammalian tissues (mouse kidney and human liver) showed optimum advantage when compared with tetrahydrouridine (THU).
摘要翻译：用于抑制负责灭活阿拉伯糖基胞嘧啶（ara-C）的脱氨酶的七元杂环核苷。含有七元糖苷配基的优选核苷如下：R = H，苯甲酰基，对 - 硝基苯甲酰基X = H，OR A = R，单 - ，二 - 和三 - 磷酸酯（PO3E2，P2O6E3，P3O9E4）E = H，Na优选的糖苷配基如下：图像1a：X = OCH 2 CH 2 O 1b：X = SCH 2 CH 2 S 1c：X = O 1d：X = H，OH 1e：X = 2H用于来自哺乳动物组织的嘧啶脱氨酶的活性成分小鼠肾和人肝）与四氢尿苷（THU）相比显示出最佳的优势。

4. 发明授权

US4975434A Antiviral and anticancer cyclopentenyl cytosine 失效
标题翻译：抗病毒和抗癌环戊烯胞嘧啶
公开(公告)号：US4975434A
公开(公告)日：1990-12-04
申请号：US307115
申请日：1989-01-31
申请人： Victor E. Marquez , John S. Driscoll , Mu-Ill Lim , Christopher K. Tseng , Alberto Haces , Robert I. Glazer
发明人： Victor E. Marquez , John S. Driscoll , Mu-Ill Lim , Christopher K. Tseng , Alberto Haces , Robert I. Glazer
IPC分类号： C07D239/46 , C07D239/54 , C07D239/56 , C07D317/44 , C07D405/04 , C07D471/04
CPC分类号： C07D239/47 , C07D239/54 , C07D239/56 , C07D317/44 , C07D405/04 , C07D471/04
摘要： Cyclopentenyl pyrimidine compounds have potent anti-viral, anti-tumor and differentiating activity. Of these compounds, cyclopentenyl cytosine has proved to be particularly effective in a variety of tumors, as well as having good antiviral activity and potent differentiating properties.
摘要翻译：环戊烯基嘧啶化合物具有有效的抗病毒，抗肿瘤和分化活性。在这些化合物中，已经证明环戊烯基胞嘧啶在多种肿瘤中特别有效，并且具有良好的抗病毒活性和有效的分化特性。

5. 发明授权

US5565437A 2',3'-dideoxy-2'-fluoro-purine nucleosides and methods for using same 失效
标题翻译： 2'，3'-二脱氧-2'-氟 - 嘌呤核苷及其使用方法
公开(公告)号：US5565437A
公开(公告)日：1996-10-15
申请号：US62520
申请日：1992-11-10
申请人： Victor E. Marquez , John S. Driscoll , Christopher K-H. Tseng , James A. Kelley , David G. Johns , Hiroaki Mitsuya
发明人： Victor E. Marquez , John S. Driscoll , Christopher K-H. Tseng , James A. Kelley , David G. Johns , Hiroaki Mitsuya
IPC分类号： A61K31/70 , C07H19/16
CPC分类号： C07H19/16 , Y10S514/885
摘要： Methods of treating a human infected with human immunodeficiency virus (HIV), such as a human with AIDS, with the purina nucleotides 2',3'-dideoxy-2'-beta-fluoroadenosine (FddA) and 2',3'-dideoxy-2'-beta-fluoroinosine (FddI) are disclosed. These nucleotides are stable in an acid environment and thus can be used for oral administration. Methods of inhibiting human immunodeficiency virus replication in a human T cell using these purina nucleotides are also disclosed.
摘要翻译：用艾滋病人用人类免疫缺陷病毒（HIV）感染的人与嘌呤核苷酸2'，3'-二脱氧-2'-β-氟腺苷（FddA）和2'，3'-双脱氧 -2'-β-氟肌苷（FddI）。这些核苷酸在酸性环境中是稳定的，因此可用于口服给药。还公开了使用这些嘌呤核苷酸在人T细胞中抑制人免疫缺陷病毒复制的方法。

6. 发明授权

US4788181A 5-substituted-2',3'-dideoxycytidine compounds with anti-HTLV-III activity 失效
标题翻译：具有抗HTLV-III活性的5-取代-2'，3'-双脱氧胞苷化合物
公开(公告)号：US4788181A
公开(公告)日：1988-11-29
申请号：US913575
申请日：1986-09-29
申请人： John S. Driscoll , Victor E. Marquez , Chong-Ho Kim , James A. Kelley
发明人： John S. Driscoll , Victor E. Marquez , Chong-Ho Kim , James A. Kelley
IPC分类号： C07D405/04 , A61K31/70 , C07H19/06 , C07H19/10
CPC分类号： C07D405/04
摘要： 5-substituted 2',3'-dideoxycytidine compounds and their monophosphates are disclosed which have been found to have potent activity against retroviruses. The 5-fluoro-and 5-aza-substituted 2',3'-dideoycytidine compounds have been found to be effective against HTLV-III/LAV virus.
摘要翻译：公开了已经发现其具有对逆转录病毒的有效活性的5-取代的2'，3'-双脱氧胞苷化合物及其单磷酸酯。已经发现5-氟代和5-氮杂取代的2'，3'-二脱氧胞苷化合物对HTLV-III / LAV病毒有效。

7. 发明授权

US5495010A Acid stable purine dideoxynucleosides 失效
标题翻译：酸稳定嘌呤双脱氧核苷
公开(公告)号：US5495010A
公开(公告)日：1996-02-27
申请号：US762082
申请日：1991-09-19
申请人： Victor E. Marquez , John S. Driscoll , Christopher K-H. Tseng , James A. Kelley , David G. Johns , Hiroaki Mitsuya
发明人： Victor E. Marquez , John S. Driscoll , Christopher K-H. Tseng , James A. Kelley , David G. Johns , Hiroaki Mitsuya
IPC分类号： A61K31/70 , C07H19/16
CPC分类号： C07H19/16 , Y10S514/885
摘要： Purine nucleosides active against human immunodeficiency virus which are substituted at the 2'-position by a strong electronegative group such as fluorine are stable in an acid environment and thus can be used for oral administration.
摘要翻译：通过强电负性基团如氟取代在2位上的针对人类免疫缺陷病毒的嘌呤核苷在酸性环境中是稳定的，因此可以用于口服给药。

8. 发明授权

US4968690A 3-deazaneplanocin, intermediates for it, and antiviral composition and method of treatment using it 失效
标题翻译： 3-deazaneplanocin，它的中间体，以及抗病毒组合物和使用它的治疗方法
公开(公告)号：US4968690A
公开(公告)日：1990-11-06
申请号：US299021
申请日：1989-01-19
申请人： Victor E. Marquez , John S. Driscoll , Mu-Ill Lim , Christopher K. Tseng , Alberto Haces , Robert I. Glazer
发明人： Victor E. Marquez , John S. Driscoll , Mu-Ill Lim , Christopher K. Tseng , Alberto Haces , Robert I. Glazer
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The new compound 3-deazaneplanocin A has been discovered to have potent anti-viral, anti-tumor activity and differentiating activity. A simple method for preparing 3-deazaneplanocin A has been developed involving nucleophilic substitution, which method can also be used to prepare a great variety of carbocyclic nucleosides.
摘要翻译：已经发现新的化合物3-脱氮普萘醌A具有有效的抗病毒，抗肿瘤活性和分化活性。已经开发了一种用于制备3-脱氮蛇嘌呤A的简单方法，其涉及亲核取代，该方法也可用于制备各种各样的碳环核苷。

9. 发明授权

US4105774A Hydantoin compounds and methods of use thereof 失效
标题翻译：乙内酰脲化合物及其使用方法
公开(公告)号：US4105774A
公开(公告)日：1978-08-08
申请号：US599602
申请日：1975-07-28
申请人： John S. Driscoll , Victor E. Marquez , Geoffrey Peng
发明人： John S. Driscoll , Victor E. Marquez , Geoffrey Peng
IPC分类号： A61K31/415 , A61K31/4166 , A61P35/00 , C07D233/72 , C07D233/74 , C07D233/76 , C07D233/78 , C07D235/02 , C07D233/20
CPC分类号： C07D235/02 , C07D233/72 , C07D233/74
摘要： Hydantoin derivatives of varying lipophilic character were prepared as nigen mustard carriers for CNS anti-tumor evaluation in transplanted mouse tumor test systems. Activity was studied in the murine ependymoblastoma brain tumor system. Multiple cures were observed for three of the four analogs examined. The compounds were also active in the intraperitoneal leukemia L1210 and P388 systems as well as in B16 melanoma and Lewis lung carcinoma.
摘要翻译：制备不同亲油性特征的乙内酰脲衍生物作为氮芥载体用于移植小鼠肿瘤试验系统中的CNS抗肿瘤评价。在小鼠室管瘤母细胞瘤脑肿瘤系统中研究了活性。观察到四种类似物中的三种检测到多种固化。该化合物在腹膜内白血病L1210和P388系统以及B16黑素瘤和Lewis肺癌中也是活跃的。

10. 发明授权

US5498719A Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors 失效
标题翻译：导致氟化逆转录酶抑制剂制备的关键中间体的非对映选择性过程
公开(公告)号：US5498719A
公开(公告)日：1996-03-12
申请号：US189095
申请日：1994-01-31
申请人： Victor E. Marquez , John S. Driscoll , Magbool A. Siddiqui
发明人： Victor E. Marquez , John S. Driscoll , Magbool A. Siddiqui
IPC分类号： C07D317/26 , C07D317/30 , C07D413/06
CPC分类号： C07D413/06 , C07D317/26 , C07D317/30
摘要： The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-.alpha.-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.
摘要翻译：本发明提供了一种关键前体的新型合成途径，即用于制备FddA的（S，S）-α-氟-2,2-二甲基-1,3-二氧戊环-4-丙酸酯 FddC。即时非对映选择性方法利用含有手性助剂的新型中间体。手性助剂可以是任何手性辅助部分，例如含有取代的恶唑烷酮基团的助剂。包含手性助剂的中间体在氟化糖的合成中首次使用氟化方法进行氟化，得到氟化中间体，其在除去手性基团后提供所需的关键中间体。总之，在本发明的方法中，通过手性烯醇化物与亲电氟化剂的反应将氟非对映选择性引入中间体，并且氟化的中间体衍生自甘露醇。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式