- Novel imidazole compounds as a new series of potent, orally active inhibitors of 5-lipoxygenase
-
Replacement of the dihydroquinolinone pharmacophore of Zeneca's ZD2138 by ionizable imidazolylphenyl moiety has lead to the discovery of a novel series of potent and orally active 5-lipoxygenase (5-LO) inhibitors. The synthesis and structure-activity relationship (SAR) of this series of compounds are described herein.
- Mano, Takashi,Stevens, Rodney W.,Ando, Kazuo,Nakao, Kazunari,Okumura, Yoshiyuki,Sakakibara, Minoru,Okumura, Takako,Tamura, Tetsuya,Miyamoto, Kimitaka
-
p. 3879 - 3887
(2007/10/03)
-
- NOVEL SULFONYL DERIVATIVES
-
Sulfonyl derivatives represented by the following general formula (I): Q1-Q2-T1-Q3-SO2-QA and drugs containing the same (wherein Q1 is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q2 is a single band, oxygen, sulfur, C1-C6 alkylene or the like; QA is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T1 is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.
- -
-
-
- BENZAMIDINE DERIVATIVES
-
Benzamidine derivatives of the following formulae or analogs thereof, i. e., pharmaceutically acceptable salts thereof, are provided. These compounds or salts thereof have a blood-coagulation inhibiting effect based on an excellent effect of inhibiting the action of activated blood coagulation factor X, and they are useful as anticoagulants.
- -
-
-