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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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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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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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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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Cyclic amides (Tue, 13 Jun 2000)
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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Novel immunotherapeutic agents and their use in the reduction of cytokine levels (Fri, 21 Dec 2001)
Patent 334148 A phenyl compound has the formula (I) wherein X is -O- or -(CH2)n- and R1 is alkyl monocycloalkyl, polycycloalkyl or benzocyclic alkyl or X is -CH= and R1 is alkylidene, monocycloalkylidene or bicycloalkylidene; n is 0 to 3; R2 is hydrogen, nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl, alkylidenemethyl, alkoxy, or halo; R3 is (i) phenyl optionally at the 3, 4 or 5 position with 1 to 3 substituents selected independently from nitro, cyano, halo, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, optionally substituted carbamoyl, acetoxy, carboxy, hydroxy, optionally substituted amino, alkyl, cycloalkyl, alkoxy, cycloalkoxy, alkylidenemethyl, cycloalkylidenemethyl, phenyl, or methylenedioxy; (ii) optionally substituted pyridine, pyrrolidine, imidazole, naphthalene, or thiophene or (iii) optionally substituted cycloalkyl; each of R4 and R5 taken individually is hydrogen or R4 and R5 taken together are a carbon-carbon bond; Y is -COZ, -C(N, or alkyl; Z is -OH, -NR6R6, -R7, or ���OR7; R6 is hydrogen or alkyl; and R7 is alkyl or benzyl...
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Ring closure of N-phthaloylglutamines (Tue, 31 Oct 1995)
Cyclic imides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-(2,6-dioxo-3-piperidinyl)-4-azaisoindoline-1,3-dione.
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ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME (Thu, 09 May 2019)
Provided are 4′-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
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ISOINDOLE-IMIDE COMPOUNDS AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME (Thu, 08 Mar 2007)
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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SUBSTITUTED 2-(2,6-DIOXOPIPERIDIN-3-YL)-PHTHALIMIDES AND -1-OXOISOINDOLINES AND METHOD OF REDUCING TNF.ALPHA. LEVELS (Thu, 29 Jan 1998)
Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2.6- dioxopiperidin-3- yl)isoindolines reduce the levels of TNF-alpha in a mammal. A typical embodiments is 1- oxo-2-(2,6-dioxopiperidin-3-yl)-4.6.7-tetratfluoroisoindoline having the formula: (see above formula)
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N-methylaminomethyl isoindole compounds and compositions comprising and methods of using the same (Thu, 22 Dec 2011)
Patent 575689 Disclosed is a compound of formula (II) e.g. 3-(3,4-dichloro-phenyl)-1-[2-(2,6-dioxo-piperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl-methyl-1-methyl-ureay or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein: * denotes chiral center; X is CH2 or C=O; R is alkyl; alkoxy; amino; alkyl-amino; dialkylamino, for treating, managing or preventing a disease or disorder, wherein the disease or disorder is cancer, a disorder associated with angiogenesis, pain, macular degeneration or a related syndrome, a skin disease, a pulmonary disorder, an asbestos related disorder, a parasitic disease, an immunodeficiency disorder, a CNS disorder, CNS injury, atherosclerosis or a related disorder, dysfunctional sleep or a related disorder, hemoglobinopathy or a related disorder, or a TNF related disorder.
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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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Process for preparing thalidomide (Tue, 28 Jul 1998)
The specification provides for an improved process for preparing thalidomide. N-phthaloylglutamine or N-phthal-oylisoglutamine is cyclized with N,N'-carbonyldiimidazole with the improvement comprising heating the N-phthaloylglutamine or N-phthal-oylisoglutamine and N,N'-carbonyldiimidazole in refluxing anhydrous tetrahydrofuran. Step one of refluxing is performed in the presence of a base.
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5-substituted isoindoline compounds (Thu, 01 Dec 2016)
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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Substituted alkanohydroxamic acids and method of reducing TNFα levels (Tue, 10 Apr 2001)
Imido and amido substituted alkanohydroxamic acids reduce the levels of TNFα and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.
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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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Cyclic amides (Tue, 13 Mar 2001)
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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Imides as inhibitors of TNF alpha (Wed, 17 Nov 2004)
The present invention relates to compounds useful as inhibitors of TNF alpha and inhibitors of NFKB binding.
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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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