- Design, Conformation, and Crystallography of 2-Naphthyl Phenyl Ethers as Potent Anti-HIV Agents
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Catechol diethers that incorporate a 7-cyano-2-naphthyl substituent are reported as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Many of the compounds have 1-10 nM potencies toward wild-type HIV-1. An interesting conformational effect allows two unique conformers for the naphthyl group in complexes with HIV-RT. X-ray crystal structures for 4a and 4f illustrate the alternatives.
- Lee, Won-Gil,Chan, Albert H.,Spasov, Krasimir A.,Anderson, Karen S.,Jorgensen, William L.
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p. 1156 - 1160
(2016/12/16)
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- Benzo-hexatomic ring derivative used as DPP-4 inhibitor and application of benzo-hexatomic ring derivative
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The invention relates to a benzo-hexatomic ring derivative used as a DPP-4 inhibitor and application of the benzo-hexatomic ring derivative, in particular to compounds shown as in formula I, medicine compositions with the compounds shown as in the formula I and application of the compounds in preparing medicines for treating diseases related to DPP-4 or inhibiting the DPP-4.
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Paragraph 0251; 0252; 0253; 0254
(2016/10/09)
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- Dicationic DNA-targeted antiprotozoal agents: Naphthalene replacement of benzimidazole
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A series of naphthalene analogues of highly active benzimidazole diamidines were synthesized using sequential Stille and Suzuki coupling reactions for preparation of the bis-nitrile intermediates. All of the diamidines showed strong DNA affinities as judged by high ΔTm values with poly(dA-dT). The dicationic compounds were quite active in vitro versus Trypanosoma brucei rhodesiense (T. b. r.) exhibiting IC50 values ranging from 4 to 98 nM. These compounds were also active versus Plasmodium falciparum (P. f.) giving IC50 values ranging from 4 to 33 nM. Two of the compounds showed good activity in vivo in the STIB900 model for acute African trypanosomiasis; one gave 3/4 cures and the other gave 4/4 cures on ip dosage of 20 mg/kg for 4 days. The amidoxime prodrugs of the naphthalene analogues were essentially ineffective.
- Chackal-Catoen, Sarah,Miao, Yi,Wilson, W. David,Wenzler, Tanja,Brun, Reto,Boykin, David W.
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p. 7434 - 7445
(2007/10/03)
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- Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring
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A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine
- Ueno, Hiroshi,Yokota, Katsuyuki,Hoshi, Jun-Ichi,Yasue, Katsutaka,Hayashi, Mikio,Hase, Yasunori,Uchida, Itsuo,Aisaka, Kazuo,Katoh, Susumu,Cho, Hidetsura
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p. 3586 - 3604
(2007/10/03)
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- Pharmaceutical compounds
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This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.
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- Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors
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A series of benzoxazinone derivatives was designed and synthesized as factor Xa inhibitors. We demonstrated that the naphthyl moiety in the aniline-based compounds 1 and 2 can be replaced with benzene-fused heterobicycles and biaryls to give factor Xa inh
- Huang, Wenrong,Zhang, Penglie,Zuckett, Jingmei F.,Wang, Lingyan,Woolfrey, John,Song, Yonghong,Jia, Zhaozhong J.,Clizbe, Lane A.,Su, Ting,Tran, Katherine,Huang, Brian,Wong, Paul,Sinha, Uma,Park, Gary,Reed, Andrea,Malinowski, John,Hollenbach, Stanley J.,Scarborough, Robert M.,Zhu, Bing-Yan
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p. 561 - 566
(2007/10/03)
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- Azabicyclic compounds for the treatment of disease
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The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1-2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1-2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which α7 is known to be involved.
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- Amidine compounds
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A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
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- Urokinase inhibitors
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Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
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- Ukokinase inhibitors
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Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
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- A Short Synthesis of the Factor-Xa Inhibitor DX-9065a Using Palladium-Catalyzed Key Steps1
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We describe a new, efficient synthesis of DX-9065a (4), a potent inhibitor of the blood coagulation enzyme factor Xa (fXa) which has previously been prepared in more than 20 steps. We saved approximately 10 steps starting with a Pd-catalyzed cyanation of
- Kehr, Christiane,Neidlein, Richard,Engh, Richard A.,Brandstetter, Hans,Kucznierz, Ralf,Leinert, Herbert,Marzenell, Klaus,Strein, Klaus,Von Der Saal, Wolfgang
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p. 892 - 896
(2007/10/03)
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- Photoexcited proton transfer from enhanced photoacids
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Naphthols with electron-withdrawing groups such as cyano or methanesulfonyl at C-5 and C-8 exhibit greatly enhanced photoacidity. This increase in photoacidity enables the substituted naphthols to undergo excited-state proton transfer (ESPT) in alcohols and Me2SO in the absence of water. In aqueous tetrahydrofuran solution, efficient proton transfer to water occurs at much lower water concentrations than with the parent naphthol, and the kinetics of proton transfer indicate that a smaller water cluster is involved.
- Tolbert, Laren M.,Haubrich, Jeanne E.
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p. 10593 - 10600
(2007/10/02)
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- SYNTHESIS OF 6,7-SUBSTITUTED 2-NAPHTHOLS
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6,7-Substituted 2-naphthols were obtained with 52-70percent yields by the condensation of the benzoate or acetate of α,α,α',α'-tetrabromo-3,4-xylenol with various dienophiles, followed by hydrolysis of the obtained esters.
- Kopranenkov, V. N.,Makarova, E. A.,Luk'yanets, E. A.
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p. 303 - 306
(2007/10/02)
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