公开(公告)号：US20130281470A1

公开(公告)日：2013-10-24

申请号：US13921233

申请日：2013-06-19

申请人： Richard Anthony Vere Hodge ,  Raymond Schinazi

发明人： Richard Anthony Vere Hodge ,  Raymond Schinazi

IPC分类号： A61K31/522

CPC分类号： A61K31/522 ,  A61K31/661

摘要： A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.

摘要翻译： 一种治疗方法：i）哺乳动物，包括人类中的HIV-1感染; 或ii）哺乳动物，包括人类中的HBV感染; 该方法包括向需要这种治疗的人施用有效量的式（A）化合物的三磷酸的（R） - 对映异构体或其药学上可接受的盐; 和用于该方法的化合物。

公开(公告)号：US06949521B2

公开(公告)日：2005-09-27

申请号：US09849870

申请日：2001-05-04

申请人： Chung K. Chu ,  Lakshmi P. Kotra ,  Konstantine Manouilov ,  Jinfa Du ,  Raymond Schinazi

发明人： Chung K. Chu ,  Lakshmi P. Kotra ,  Konstantine Manouilov ,  Jinfa Du ,  Raymond Schinazi

IPC分类号： C07D499/21 ,  A61K31/00 ,  A61K31/505 ,  A61K31/52 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7076 ,  A61K47/48 ,  A61P43/00 ,  C07D239/46 ,  C07D473/16 ,  C07D473/34 ,  C07D501/14 ,  C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/167 ,  C07H19/173 ,  C07H19/19 ,  C07H19/20 ,  A01N43/04

CPC分类号： A61K31/7076 ,  A61K47/52 ,  C07H19/04 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

摘要： Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

摘要翻译： 提供药物前药组合物，其包含能够在体内转化为药物的药物的叠氮衍生物。 具有胺，酮和羟基取代基的药物的叠氮衍生物在体内转化为相应的药物，增加药物的半衰期。 此外叠氮化物前药通常比相应的药物更好地穿透血脑屏障。 特别有用的是虫草素，2'-F-ara-ddI，AraA，阿昔洛韦，喷昔洛韦和相关药物的叠氮衍生物。 有用的叠氮化物前药是治疗脂环族胺，酮和羟基取代的化合物的叠氮化物衍生物，包括芳烷基，杂环芳烷基和环状脂族化合物，其中胺或氧部分在环上，或胺或氧部分在其上 脂肪族侧链，以及治疗性嘌呤和嘧啶，核苷类似物和磷酸化核苷类似物。

公开(公告)号：US20050209196A1

公开(公告)日：2005-09-22

申请号：US10530088

申请日：2003-12-08

申请人： Chung Chu ,  Raymond Schinazi

发明人： Chung Chu ,  Raymond Schinazi

IPC分类号： A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/65 ,  A61K31/675 ,  A61K31/70 ,  A61K45/06

CPC分类号： A61K45/06 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/65 ,  A61K31/675 ,  A61K31/70 ,  A61K2300/00

摘要： The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nucleoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others. These agents are generally selected from the group consisting of 3TC (Lamivudine), AZT (Zidovudine), (−)-FTC, ddI (Didanosine), ddC (zalcitabine), abacavir (ABC), tenofovir (PMPA), D-D4FC (Reverset), D4T (Stavudine), Racivir, L-D4FC, NVP (Nevirapine), DLV (Delavirdine), EFV (Efavirenz), SQVM (Saquinavir mesylate), RTV (Ritonavir), IDV (Indinavir), SQV (Saquinavir), NFV (Nelfinavir), APV (Amprenavir), LPV (Lopinavir), fuseon and mixtures thereof. The TK dependent agents, such as AZT and D4T, may be used in combination with one of the dioloxane thymine compounds according to the present invention, but the use of such agents may be less preferred. In preferred compositions according to the present invention, R1 is preferably H or a C2-C18 acyl group or a monophosphate group. Pharmaceutical compositions and methods of reducing the likelihood that a patient at risk for contract an HIV infection will contract the infection are other aspects of the present invention.

公开(公告)号：US20050004148A1

公开(公告)日：2005-01-06

申请号：US10700276

申请日：2003-11-03

申请人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

发明人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

IPC分类号： A61K31/505 ,  A61K20060101 ,  A61K31/00 ,  A61K31/39 ,  A61K31/513 ,  A61K31/695 ,  A61K31/7064 ,  A61K31/7068 ,  A61P31/12 ,  A61P31/18 ,  C07D20060101 ,  C07D239/02 ,  C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07D451/00 ,  C07F7/18 ,  C07H19/06 ,  C07H19/10 ,  C12P19/38 ,  C12P41/00 ,  C07

CPC分类号： C07D405/04 ,  C07D327/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10

摘要： A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

摘要翻译： 公开了用于治疗人体中HIV和HBV感染的方法和组合物，其包括给予有效量的2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷，其药学上可接受的衍生物 ，包括在药学上可接受的载体中的5'或N 4烷基化或酰化衍生物或其药学上可接受的盐。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。