- TRICYCLIC PYRIDONES AND PYRIMIDONES
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A compound of Formula (I) is provided: (I) where the variables are defined herein.
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Paragraph 0723; 0727-0729
(2021/06/26)
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- SPIRO-LACTAM COMPOUNDS AND METHODS OF TREATING VIRAL INFECTIONS USING THE SAME
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Disclosed are compounds, and pharmaceutically acceptable salts thereof, that can ameliorate or treat a viral infection in a subject in need thereof. The disclosure also includes conjugates of such compounds with a protease.
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Page/Page column 86
(2021/12/28)
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- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 51-52
(2018/03/01)
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- COMPOUNDS FOR THE INHIBITION OF CELLULAR PROLIFERATION
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Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.
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Page/Page column 113-114
(2012/02/01)
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- Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
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A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
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Page/Page column 30
(2010/11/24)
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- HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl
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Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.
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Page/Page column 82; 83
(2008/06/13)
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- ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
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The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, Rl and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
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Page/Page column 92
(2008/06/13)
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- The relationship between physicochemical properties, in vitro activity and pharmacokinetic profiles of analogues of diamine-containing efflux pump inhibitors
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Following the optimization of diamine-containing efflux pump inhibitors with respect to in vitro potentiation activity, in vivo stability and acute toxicity, we addressed the question of how to control the pharmacokinetic properties of the series. Upon in
- Watkins, William J.,Landaverry, Yakira,Leger, Roger,Litman, Renee,Renau, Thomas E.,Williams, Nicole,Yen, Rose,Zhang, Jason Z.,Chamberland, Suzanne,Madsen, Deidre,Griffith, David,Tembe, Vrushali,Huie, Keith,Dudley, Michael N.
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p. 4241 - 4244
(2007/10/03)
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- Chiral Synthesis and Enzymatic Resolution of (S)-(-)Piperazine-2-Carboxylic Acid Using Enzyme Alcalase
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Enantiomerically pure (S)-piperazine-2-carboxylic acid was synthesized by kinetic resolution of methyl-4-(tert-butyroxycarbonyl)-piperazine-2-carboxylate using a low cost enzyme alcalase.
- Wu, Guosheng,Zhao, Hua,Luo, Robert G.,Wei, Dean,Malhotra, Sanjay V.
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p. 343 - 345
(2007/10/03)
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- Design and synthesis of piperazine-based matrix metalloproteinase inhibitors
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A new generation of cyclic matrix metalloproteinase (MMP) inhibitors derived from dl-piperazinecarboxylic acid has been described. The design involves: incorporation of hydroxamic acid as the bidentate chelating agent for catalytic Zn2+, placement of a sulfonamide group at the 1N-position of the piperazine ring to fill the S1' pocket of the enzyme, and finally attachment of diverse functional groups at the 4N-position to optimize potency and peroral absorption. A unique combination of all three elements produced inhibitor 20 with high affinity for MMPs 1, 3, 9, and 13 (24, 18, 1.9, and 1.3 nM, respectively). X-ray crystallography data obtained for MMP-3 cocrystallized with 20 gave detailed information on key binding interactions defining an overall scaffold geometry for piperazine-based MMP inhibitors.
- Cheng, Menyan,De, Biswanath,Pikul, Stanislaw,Almstead, Neil G.,Natchus, Michael G.,Anastasio, Melanie V.,McPhail, Sara J.,Snider, Catherine E.,Taiwo, Yetunde O.,Chen, Longyin,Dunaway, C. Michelle,Gu, Fei,Dowty, Martin E.,Mieling, Glen E.,Janusz, Michael J.,Wang-Weigand, Sherry
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p. 369 - 380
(2007/10/03)
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- Amino acid derivatives
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Compounds of the formula STR1 wherein R1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulphonyl, arylsulphonyl, monoaralkylcarbamoyl, cinnamoyl or α-aralkoxycarbonylaminoalkanoyl and R2 is hydrogen or R1 and R2 together with the nitrogen atom to which they are attached represent a cyclic imide group of the formula STR2 in which P and Q together represent an aromatic system; R3 is alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkyl- sulphinylalkyl, carbamoylalkyl or alkoxycarbonylalkyl or, when n stands for zero, R3 can also represent alkylthioalkyl or, when n stands for 1, R3 can also represent alkylsulphonylalkyl; R4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; R5 is hydrogen and R6 is hydroxy or R5 and R6 together represent oxo; R7 and R8 together represent a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH2 -- group is replaced by --NH--, --N(alkoxycar- bonyl)--, --N(alkyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring; and R9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula STR3 in which R10 and R11 each represent alkyl; and their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
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