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Substituted acylhydroxamic acids and method of reducing TNF alpha levels (Fri, 26 Sep 2003)
Patent 519638 A chirally pure (R) or chirally pure (S) or a mixture of (R) or (S) acylhydroxamic acid derivative or an addition salt thereof has the formula (I) wherein: the carbon atom designated * constitutes a center of chirality; R4 is hydrogen or- (C=O)-R12; R1 and R2 independently are alkyl, phenyl, benzyl, pyridyl methyl, pyridyl, imidazloyl, imidazolylmethyl, or CHR*(CH2)nNR*R0; R*and R0 independently are hydrogen, alkyl, phenyl, benzyl, pyridylmethyl, pyridyl, imidazloyl or imidazolylmethyl; n is 0 to 2; R5 is C=O, CH2, CH2-CO-, or SO2; R6 and R7 independently are nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl, alkoxy, cycloalkoxy, halo, bicycloalkyl, tricycloalkoxy, 1-indanyloxy, 2-indanyloxy, -cycloalkylidenemethyl, or alkylidenemethyl; R8, R9, R10 and R11 are independently (i) hydrogen, nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkylamino, dialkylamino, acylamino, alkyl, alkoxy halo, or (ii) one of R8, R9, R10 and R11 is acylamino, and the remaining of R8, R9, R10 and R11 are hydrogen, or (iii) hydrogen if R8 and R9 taken together are benzo, quinoline, quinoxaline, benzimidazole, benzodioxole, 2-hydroxybenzimidazole, methylenedioxy, dialkoxy or dialkyl, or (iv) hydrogen if R10 and R11 taken together are benzo, quinoline, quinoxaline, benzimidazole, benzodioxole, 2-hydroxybenzimidazole, methylenedioxy, dialkoxy, or dialkyl, or (v) hydrogen if R9 and R10 taken together are benzo...
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Pharmaceutically active isoindoline derivatives (Fri, 28 Nov 2003)
Patent 519459 Isoindolin-1-one and Isoindoline-1, 3-dione substituted in the 2-position with an alpha -(3, 4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF alpha and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4,5-diaminoisoindoline-1,3-dione.
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COMPOSITIONS AND METHODS FOR INDUCING CONFORMATIONAL CHANGES IN CEREBLON OTHER E3 UBIQUITIN LIGASES (Wed, 30 Dec 2015)
Provided herein are compositions, therapeutic methods, screening methods, computational methods and biomarkers based upon the elucidation of the interaction among cerebloR, its substrates and certain compounds or agents, including small molecules, peptides, and proteins.
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Isoindole-imide compounds, compositions, and uses thereof (Fri, 28 Oct 2005)
Patent 526893 Isoindole-imide compounds of formula (I) and pharmaceutical compositions comprising these compounds are disclosed. The described compounds are useful for modulating the production of TNF-alpha, IL-1beta, IL-10, or T-cells in a mammal. The compounds are also useful in the manufacture of a medicament for treating cancer, an inflammatory disorder, or heart disease.
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Diphenylethylene compounds and uses thereof (Fri, 29 Aug 2008)
Patent 542407 Disclosed is a diphenylethylene compound of formula (I) or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the substituents are described within the specification. Also disclosed is the use of the above compound for the preparation of a composition for inhibiting angiogenesis, for inhibiting or reducing tubulin polymerization or tubulin stability in a cell, for inhibiting PDE4 activity in a cell, for treating or ameliorating an inflammatory disorder, for inhibiting or ameliorating cancer and for treating or ameliorating a central nervous system disorder.
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PROCESS FOR THE PREPARATION OF THALIDOMIDE (Thu, 12 Jan 1995)
The present invention relates to compounds which are useful for reducing levels of TNF.alpha. in a mammal. Examples of compounds include those of formula: wherein, for example, R7 is a cyclic alkyl, a substituted phenyl, etc ...; n is 1 and R12 is an alkoxy, a disubstituted amino, etc ...; those of formula: wherein, for example, Z is or R4 NH- n is 1, 2 or 3; R1 is a divalent residue of 3,4-pyridine, pyrrolidine, etc ...; R2 is -CO- or -SO2-; R3 is a substituted phenyl, pyridyl, etc ...; and R4 is alanyl, argynyl, etc.
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ISOINDOLE-IMIDE COMPOUNDS, COMPOSITIONS, AND USES THEREOF (Thu, 01 Aug 2002)
The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potents inhibitors of the production of the TNF-.alpha. in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory, allergic; and autoimmune diseases.
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Isoindole-imide compounds and compositions comprising and methods of using the same (Thu, 20 Mar 2008)
This invention relates to isoindole-imide compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
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ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME (Wed, 09 Aug 2017)
Provided herein is a compound, which is or a pharmaceutically acceptable salt or stereoisomer thereof. Also provided is a compound or a pharmaceutical composition of the invention for use in a method for treating, managing or preventing various diseases and disorders as described herein.
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Pharmaceutically active isoindoline derivatives (Tue, 29 Sep 2015)
Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an α-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNFα and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4,5-diaminoisoindoline-1,3-dione.
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Pharmaceutically active isoindoline derivatives (Wed, 01 Dec 2010)
Cyclopropyl-N-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl] -3-oxoisoindoline-4-yl}-carboxamide, or an acid addition salt thereof, for use in treating cancer.
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Use of nitrogen substituted thalidomide analogs for the treatment of macular degenerator (Thu, 24 Jul 2003)
The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, nitrogen-substituted thalidomide analogs and di-substituted thalidomide analogs have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.
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Synthesis and anti-tumor activity of nitrogen substituted thalidomide analogs (Thu, 10 May 2007)
The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, nitrogen-substituted thalidomide analogs and di-substituted thalidomide analogs have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.
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Immunotherapeutic agents (Tue, 17 Jul 2001)
Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor α, nuclear factor κB, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovis replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
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Cyclic amides (Tue, 02 Mar 1999)
Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.
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IMMUNOTHERAPEUTIC AGENTS AND THEIR USE IN THE REDUCTION OF CYTOKINE LEVELS (Wed, 02 Jun 1999)
Cyano and carboxy derivatives of substituted styrenes of formula (I), in which Y is -COZ, -C$m(Z)N, or lower alkyl of 1 to 5 carbon atoms; Z is -OH, -NR?6¿R?6¿, -R?7¿, or -OR?7¿; X, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿, and R?7¿ have the values given in the description are inhibitors of tumor necrosis factor $g(a), nuclear factor $g(k)B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
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ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME (Wed, 09 Aug 2017)
Provided herein is a compound of formula (IV): or a pharmaceutically acceptable salt, solvate or stereoisomer thereof, wherein X, Y, R 11 , R 12 and R 13 are as defined herein. Also provided is a compound or a pharmaceutical composition of the invention for use in a method for treating, managing or preventing various diseases and disorders as described herein.
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5-substituted isoindoline compounds (Thu, 01 Jan 2015)
This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
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5-SUBSTITUTED QUINAZOLINONE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME (Thu, 28 Dec 2017)
Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed. embedded image
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Substituted phenethylsulfones and method of reducing TNF.alpha. levels (Tue, 01 Feb 2000)
Phenethylsulfones substituted in the position .alpha. to the phenyl group with a 1-oxoisoindoline or 1,3-dioxoisoindoline group reduce the levels of TNF.alpha. in a mammal. Typical embodiments are 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-aminoisoindoline- 1,3-dione and 2-[1-(3-cyclopentyloxy-4-methoxyphenyl)-2-methylsulfonylethyl]isoindoline- 1,3-dione.
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