摘要:
This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of formula (I) wherein R 1 is hydrogen, and R 2 is cytosine or 5-fluorocytosine, and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents, particularly in combination therapy.
摘要:
The present invention relates to thiophene compounds having anticancer activity. In particular, compounds of formula (a) wherein G1, G2, G3, G4, G5, G6, G7, A1, A2, and X are as defined herein, are useful in the treatment of solid tumors in mammals.
摘要:
The present invention relates to heterocyclic Compounds having antiviral activity. In particular, Compounds of formula (I), wherein B, W, X, Y, Q, R1, R2, R3, R4 and n are as defined herein, are useful in the therapy and prophylaxis of viral infection in mammals.
摘要:
Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 and R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl, or halogen; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. For the treatment of pain and pharmaceutically acceptable compositions comprising those compounds. The compounds of this invention act as agonists at the opiate receptor.
摘要:
This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin having formula (I), their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.
摘要:
The present invention covers substituted purinyl compounds. In particular, the present invention concerns 6-substituted purinyl alkoxycarbonyl amino acids, more particularly arginine derivatives. The present invention further includes substituted purinyl compounds which stimulate the immune system and thereby help protect the body against pathogens and cancer.
摘要:
The present invention concerns the use and method of treatment of β-L-5-fluoro-2',3'-dideoxycytidine (β-L-5F-ddC), and pharmaceutically acceptable derivatives thereof, for use in the treatment of viral infections, specifically HIV and hepatitis B infections. The present invention also includes the use and method of treatment of β-D-5-fluoro-2',3'-dideoxycytidine (β-D-5F-ddC) for use in the treatment of hepatitis B infections.
摘要:
This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of formula (I) wherein R1 is hydrogen, and R2 is cytosine or 5-fluorocytosine, and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents, particularly in combination therapy.
wherein R₁ is hydrogen; R₂ is a purine or pyrimidine base or an analogue or derivative thereof; Z is S, S=O or SO₂; and pharmaceutically acceptable derivatives thereof. Also described are use of the compounds as antiviral agents, pharmaceutical formulations, and methods for the preparation of the compounds.
摘要翻译:公开了下式的化合物:其中R 1是氢; R 2是嘌呤或嘧啶碱或其类似物或衍生物; Z是S,S = O或SO 2; 及其药学可接受的衍生物。 还描述了这些化合物作为抗病毒剂,药物制剂和制备该化合物的方法的用途。