Abstract:
PROBLEM TO BE SOLVED: To provide an improved HIV protease inhibitor that is very potent, that has reduced side-effects and that is effective against resistant strains of HIV.SOLUTION: This invention relates to: a compound of formula (I) as the HIV protease inhibitor; or a pharmaceutically acceptable salt form, stereoisomer, ester, salt of the ester, prodrug, salt of the prodrug, or combination thereof.
Abstract:
PROBLEM TO BE SOLVED: To provide an improved HIV protease inhibitor that is very potent, that has minimal side-effect and is effective against resistance strains of HIV.SOLUTION: A compound represented by formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof are disclosed. (in formula, A denotes an acetyl group substituted with a specified substituent, R, R, Rand Reach independently denotes alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycle, aryl, heteroaryl or the like and Rdenotes hydrogen and Rdenotes ORor Rdenotes hydrogen and Rdenotes OR, or Rand Rdenote -ORand Rdenotes hydrogen or a specifics substituent).
Abstract:
PROBLEM TO BE SOLVED: To provide prodrugs of HIV (human immune virus) protease inhibitors, pharmaceutical compositions including the prodrugs, and a method for inhibiting HIV protease activity and treating HIV infection using the same.SOLUTION: Compounds represented by formulae (I), (II), (III) are used. Here, Lis bond, -C(O)-, or -C(O)O-; Lis -(CRR)m; m is 1, 2, 3, 4, or 5; Rand Rare independently selected from a group comprising H, and C1 to 12 alkyl; Rand Rare H, C1 to 12 alkyl or arylalkyl; q is 1 or 2; t is 1 or 2; Ma and Mb are Mor M; Mis Na+ or others; Mis Ca2+ or others; and A represents a specific compound.
Abstract translation:要解决的问题:提供HIV(人免疫病毒)蛋白酶抑制剂的前药,包含前药的药物组合物,以及用于抑制HIV蛋白酶活性并用其治疗HIV感染的方法。 解决方案:使用由式(I),(II),(III)表示的化合物。 这里,L 1 SB>是键,-C(O) - 或-C(O)O-; L 2 SB>是 - (CR 1 SB> R 2 SB>)m; m为1,2,3,4或5; R 1 SB>和R 2 SB>独立地选自包括H和C 1-12烷基的基团; R 3 SB>和R 4 SB>是H,C1至12烷基或芳基烷基; q为1或2; t为1或2; Ma和Mb为M 1 SB>或M 2 SB>; M 1 SB>是Na +或其他; M 2 SB>是Ca2 +或其他; A表示特定的化合物。 版权所有(C)2013,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide compounds useful to treat hepatitis C (HCV) infections.SOLUTION: In the compounds, the uracil or thymine derivative are linked via a phenylene into either fused 2-ring cyclic system (R6) or alternatively via additional two-atom linker (L) to a 5-6 membered monocycle (R6). Application further discloses polymorphs and pseudopolymorphs of two specific compounds: N-(6(3-t-butyl-5-(2>4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)2-methoxy-phenyl)naphthalen-2-yl)methanesulfonamide and (E)-N-(4(3-t-butyl-5-(2,4-dioxo-3)4-dihydropyrimidin-1(2H)-yl)2-methoxy-styryl-phenyl)methanesulfonamide.
Abstract:
PROBLEM TO BE SOLVED: To provide anti-infective agents and the like, used either in combination with or in lieu of an interferon agent and/or ribavirin.SOLUTION: This invention relates to: (a) compounds and salts thereof that inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
Abstract:
A compound of the formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Abstract:
The instant invention provides compounds of formula (I) or a pharmaceutically acceptable salt, prodrug, or ester thereof, useful in the inhibition of neuraminidase enzymes from disease-causing microorganisms, especially influenza neuraminidase, pharmaceutical formulations containing same, processes and intermediates for preparing said compounds, as well as methods of using said compounds, including preventing and treating diseases caused by microorganisms having said neuraminidase enzyme.
Abstract:
Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
Abstract:
Enantiomerically enriched compounds having the absolute stereochemistry of the formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof, which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.
Abstract:
Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.