摘要:
Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3Kδ.
摘要:
Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要:
A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straightened or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof. The compound and salt are useful as a medicine.
摘要:
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
摘要:
Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.
摘要:
A substance for enhancing an aortic smooth muscle relaxation is provided. The substance is one selected from the group consisting of a compound of formula (I), a pharmaceutical acceptable therefrom and a solvate therefrom, wherein either of R1 and R2 is one of a hydrogen and a nitro group.
摘要:
The present invention relates to a method for producing a nucleoside derivative represented by formula (2), comprising the step of reducing a nucleoside of formula (1) in the presence of a noble metal catalyst comprising a carrier and a noble metal supported thereby, selected from the group consisting of (A) a homogeneously supported catalyst where the specific surface area of the noble metal is 95.0 m2/g or more and the particle size of the noble metal is 4.3 nm or less, and (B) a surface-loaded catalyst where the specific surface area of the noble metal is 56.0 m2/g or more and the particle size of the noble metal is 8.0 nm or less, wherein R1 is hydrogen or a protective group, R2 is NH2 or OH, R3 is an acyl group, and X is a chlorine or bromine atom. According to the present invention, the yield can be made equal even when the amount of catalyst is smaller than that used for the conventional products.
摘要:
The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
摘要:
The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
摘要:
Nonpolar thymidine analogs are provided comprising a dihalogenated or trihalogenated base of the structure: where R1 is a sugar moiety; R2 is H or CH3; an imaging moiety or a cytotoxic moiety and X1 and X2 are independently selected from I, Cl, Br, and F, with the proviso that not more than one F will be present at these positions.
摘要翻译:提供非极性胸苷类似物,其包含以下结构的二卤代或三卤代碱:其中R 1是糖部分; R 2是H或CH 3 N; 成像部分或细胞毒素部分,X 1和X 2独立地选自I,Cl,Br和F,条件是不超过一个F将 在这些位置出席。