- GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
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Page/Page column 76
(2014/10/15)
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- COMPOSITIONS AND METHODS FOR THE TREATMENT OF MALARIA
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The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.
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Page/Page column 73; 74
(2014/10/15)
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- NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS
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The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.
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Page/Page column 49-50
(2011/12/14)
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- THIAZOLE AND OXAZOLE KINASE INHIBITORS
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The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 141
(2009/07/17)
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- An efficient synthesis of cyanamide from amine promoted by a hypervalent iodine(III) reagent
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In a one-pot strategy we have achieved an efficient method for the synthesis of organic cyanamides starting from dithiocarbamic acid salts/amines. In this strategy the in situ generated alkyl or aryl isothiocyanates, obtained by the desulfurization of dithiocarbamic acid salts with diacetoxyiodobenzene (DIB) react with aqueous ammonia forming alkyl or aryl thiourea which on subsequent oxidative desulfurization with DIB led to the formation of corresponding cyanamide in good yields. Mild reaction conditions, shorter reaction time, an environmentally benign protocol, and easy isolation of the desired product make the present methodology a suitable alternative for the preparation of various organic cyanamides.
- Ghosh, Harisadhan,Yella, Ramesh,Ali, Abdur Rezzak,Sahoo, Santosh K.,Patel, Bhisma K.
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experimental part
p. 2407 - 2410
(2009/07/26)
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- SUBSTITUTED N-ALKYLPYRIMIDINONES
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This invention is directed generally to substituted pyrimidinone compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such substituted pyrimidinone include compounds generally corresponding in structure to the following formula (I): wherein R1, R2, R3, R4A, R4B, R4C, R4D and R4E are as defined in this specification. This invention also is directed to compositions of such substituted pyrimidinones (particularly pharmaceutical compositions), intermediates for the syntheses of such substituted pyrimidinones, methods for making such substituted pyrimidinones, and methods for treating (including preventing) conditions (typically pathological conditions) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
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Page/Page column 200-201
(2010/11/08)
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- THIAZOLE DERIVATIVES AND USE THEREOF
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The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
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Page/Page column 158
(2008/06/13)
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- CYSTEINE PROTEASE INHIBITORS
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A compound of the formula (II) wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(=O)2 ; where Ra is H, C1-C4 alkyl or CH3C(=O); R5 is independently selected from H or methyl; E is -C(=O)-, -S(=O)m-, -NR5S(=O)m-, -NR5C(=O)-, -OC(=O)-, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
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Page/Page column 96-97
(2010/02/12)
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- Hepatitis C inhibitor tri-peptides
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Disclosed herein are compounds of formula (1): wherein Ris hydroxy or NHSO2Rwherein Ris (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O-(C1-6)alkyl, amido, amino or phenyl, or Ris C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O-(C1-6) alkyl, amido, amino or phenyl; Ris (C4-6)cycloalkyl; Ris t-btuyl or (C5-6) cycloalkyl and Ris (C4-6)cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of HCV NS3 protease.
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- Hepatitis C inhibitor tri-peptides
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Disclosed herein are compounds of formula (1): wherein R1is hydroxy or NHSO2R1Awherein R1Ais (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O—(C1-6)alkyl, amido, amino or phenyl, or R1Ais C6or C10aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O—(C1-6) alkyl, amido, amino or phenyl; R2is (C4-6)cycloalkyl; R3is t-butyl or (C5-6) cycloalkyl and R4is (C4-6)cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of HCV NS3 protease.
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- A General Procedure for Synthesis of NG-Alkyl, and NG-Aryl-L-Arginines as Potential Nitric Oxide Synthase Inhibitors
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A general procedure for the synthesis of NG-alkyl, and NG-aryl-L-arginines with relatively high overall yield is reported. The key step involved the coupling of protected L-ornithine 4 with isothiourea 7 to give the fully protected NG-aryl-L-arginine derivative 8. Subsequent deprotection of 8 in acidic condition provided the final target compound 9 with an overall yield of more than 80%.
- Chen, Bor-Cherng,Shiu, Shi,Yang, Ding-Yah
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p. 549 - 553
(2007/10/03)
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- NG-Allyl- and NG-Cyclopropyl-L-arginine: Two Novel Inhibitors of Macrophage Nitric Oxide Synthase
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NG-Methyl-L-arginine has recently been shown to inactivate the inducible murine macrophage nitric oxide (.NO) synthase (Olken, N.M.; Rusche, K.M.; Richards, M.K.; Marletta, M.A.Biochem.Biophys.Res.Commun. 1991, 177, 828-833).NG-Allyl-L-arginine and NG-cyclopropyl-L-arginine were synthesized as potential mechanism-based enzyme inhibitors to exploit the chemistry presumed to occur at the active site.NG-Cyclopropyl-L-arginine was found to be a potent reversible inhibitor with a Ki = 7.7 μM.NG-Allyl-L-arginine was found to be both a potent reversible (Ki = 2.1 μM) and irreversible inhibitor of the enzyme.The irreversible inhibition demonstrated pseudo-first-order inactivation kinetics with kinact = 0.026 min-1 and Ki = 3.4 μM.Stereospecific protection of the inactivation was afforded by L-arginine, and saturability of the inactivation rate was observed.Our studies indicate that both reversible and irreversible inhibition of the inducible .NO synthase can be achieved with relatively simple modifications of the substrate L-arginine.
- Olken, Norman M.,Marletta, Michael A.
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p. 1137 - 1144
(2007/10/02)
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