- CYANOGUANIDINES AND THEIR USE AS ANTIVIRAL AGENTS
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This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (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.
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Page/Page column 98
(2014/01/17)
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- KINASE INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE
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Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use
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Page/Page column 12
(2009/03/07)
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- Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma
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The discovery of a pyrrolopyrimidine class of LIM-kinase 2 (LIMK2) inhibitors is reported. These LIMK2 inhibitors show good potency in enzymatic and cellular assays and good selectivity against ROCK. After topical dosing to the eye in a steroid induced mouse model of ocular hypertension, the compounds reduce intraocular pressure to baseline levels. The compounds also increase outflow facility in a pig eye perfusion assay. These results suggest LIMK2 may be an effective target for treating ocular hypertension and associated glaucoma.
- Harrison, Bryce A.,Whitlock, N. Andrew,Voronkov, Michael V.,Almstead, Zheng Y.,Gu, Kun-Jian,Mabon, Ross,Gardyan, Michael,Hamman, Brian D.,Allen, Jason,Gopinathan, Suma,McKnight, Beth,Crist, Mike,Zhang, Yulian,Liu, Ying,Courtney, Lawrence F.,Key, Billie,Zhou, Julia,Patel, Nita,Yates, Phil W.,Liu, Qingyun,Wilson, Alan G. E.,Kimball, S. David,Crosson, Craig E.,Rice, Dennis S.,Rawlins, David B.
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supporting information; experimental part
p. 6515 - 6518
(2010/03/31)
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- NOVEL COMPOUNDS
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There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
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Page/Page column 142
(2008/12/06)
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- 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 3 INHIBITORS FOR THE TREATMENT OF ANDROGEN DEPENDENT DISEASES
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In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of
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- 17 Beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
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In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of
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- 17-Beta hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
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There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17β-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.
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- Proteomimetic compounds and methods
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The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.
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- Piperazine derivative
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A piperazine compound represented by formula (1): wherein X is —CH2—, —C(O)— or —CH(CH3)—; R1is a hydrogen atom or alkyl group; and R2is a hydrogen atom, alkyl group, hydroxyalkyl group, arylalkyl group, heteroarylalkyl group, carboxyalkyl group, carboxamidoalkyl group, aminoalkyl group or guanidinoalkyl group; an acid-addition salt thereof, or a hydrate thereof. The compound has excellent inhibitory effects on both cell adhesion and cell infiltration and is useful for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.
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- Antiviral indoleoxoacetyl piperazine derivatives
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
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- CHIRAL LIGANDS CONTAINING HETEROATOMS. V ENANTIOSELECTIVE KETONE REDUCTION USING CHIRAL DIAMINES/METAL HYDRIDE SYSTEMS
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New chiral reducing agents prepared from zinc or magnesium dichloride, optically active diamines and diisobutylaluminium hydride, have been studied.These complexes were used in the reduction of a series of prochiral ketones and, compared with similar tin(
- Falorni, Massimo,Giacomelli, Giampaolo,Lardicci, Luciano
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p. 765 - 769
(2007/10/02)
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