300 results about "Isoindoline" patented technology

The present invention is directed to the use of immunomodulatory compounds, particularly members of the class of compounds known as IMiDs™, and more specifically the compounds 4-(Amino)-2-(2,6-dioxo(3-piperidyl))-isoindoline-1,3-dione and 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2,6-dione, to induce the expression of fetal hemoglobin genes, genes essential for erythropoiesis, and genes encoding alpha hemoglobin stabilizing protein, within a population of CD34+ cells. These compounds are used to treat hemoglobinopathies such as sickle cell anemia or β-thalassemia, or anemias caused by disease, surgery, accident, or the introduction or ingestion of toxins, poisons or drugs.

Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and / or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4.

Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines reduce the levels of TNFα in a mammal. Typical embodiments are 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafuoroisoindoline and 1,3-dioxo-2-(2,6-dioxo-3 -methylpiperidin-3-yl)-4-aminoisoindoline.

Methods of treating cutaneous lupus in a human are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, 4-(amino)-2-(2,6-dioxo(3-piperidyl))-isoindoline-1,3-dione (ACTIMID™), 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (REVLIMID®), or cyclopropyl 2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindolin-4-yl}carboxamide, alone or alternatively, in combination with a second active agent.

This invention relates to N-methylaminomethyl-isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Methods of treating, preventing and / or managing a myeloproliferative disease are disclosed. Specific methods encompass the administration of 4-(amino)-2-(2,6-dioxo(3-piperidyl))-isoindoline-1,3-dione, or a pharmaceutically acceptable salt, solvate or stereoisomer thereof, in combination with a second active agent. Particular second active agents are is prednisone, JAK1 inhibitor, JAK2 inhibitor, FLT3 inhibitor, BCL2 inhibitor, and HDAC inhibitor.

The present application describes 2-(2′,6′-dioxo-3′-deutero-piperidin-3′-yl)isoindoles, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

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.

Substituted 2-(2,6-dioxopiperidin-3-yl) phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl) isoindolines reduce the levels of TNFα in a mammal. Typical embodiments are 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroisoindoline and 1,3-dioxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4-aminoisoindoline.

This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.

Novel isoindoline compounds are disclosed. Methods of treating, preventing and / or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.

Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.

The invention relates to a method for production of an aqueous dispersion of polymer-encapsulated pigments, characterised in that (a) an aqueous pigment dispersion, containing at least one organic pigment (P), selected from the group of azo, isoindolinone, isoindoline, anthanthrone, thioindigo, thiazinindigo, triarylcarbonium, quinophthalone, anthraquinone, dioxazine, phthalocyanine, quinacridone, quinacridonquinone, indanthrone, perylene, perinone, pyranthrone, diketopyrrolopyrrole, isoviolanthrone and azomethine pigments, at least one detergent (T), and water is prepared, (b) a monomer miniemulsion, stabilised by a hydrophobic organic compound with a water solubility at 20 DEG C of at most 5x10<-5> g / l, is prepared from a polymerisable monomer (M) and at least one detergent (T) in water, (c) a monomer pigment emulsion is prepared, whereby the aqueous dispersion from (a) and the monomer miniemulsion from (b) are mixed and homogenised and (d) the pigment-containing monomer from (c) is polymerised in the presence of a polymerisation initiator and / or by heat, whereupon an encapsulation of the pigment with the polymer thus formed occurs.

Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines are disclosed. The compounds are useful, for example, in reducing the levels of TNFα in a mammal.

Solid forms comprising (+)-2-[l-(3-Ethoxy-4-methoxyphenyl)-2- methylsulfonylethyl]-4-acetylaminoisoindoline-l,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and / or preventing disorders ameliorated by the reduction of levels of TNF-alpha or the inhibition of PDE4.

The invention discloses an application of a rhodamine B based fluorescence sensor which can specifically detect tin ions. According to the application, benzyl 3-(3', 6'-bis(diethyl amino)-3-oxo-spiro [isoindoline-1, 9'-xanthene]-2-yl) ethyl propionate is taken as a substrate, different heavy metal ions such as MgCl2*6H2O, SnCl2*H2O, CrCl3*6H2O, AgNO3, CaCl2, NaCl, PbCl2, KCl, MnCl2*4H2O, ZnCl2, CuCl2*2H2O, LiCl*H2O, Ba(NO3)2, HgCl2, CoCl2, FeCl2*4H2O, FeCl3*6H2O, CdCl2*2.5H2O, AlCl3 and the like are added, and fluorescent response is found only when SnCl2*H2O is added, so that the fluorescence sensor which can specifically detect tin ions is developed. The sensor has the advantages of high specificity and sensitivity and the like and has important application potentials in the aspects of disease diagnosis and health evaluation.

Compounds having the general formula II, III, or IVwherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and hetercocyclic group; wherein X′ is halogen, or C1-C4 haloalyl; wherein the Rx is a C1-C5 straight chain or branched chain alkyl or a C1-C4 straight chain or branched chain haloalkyl.

The invention discloses a fluorescence sensor for rhodamine B as well as preparation and a detection application thereof to Fe<3+>. The rhodamine B is used as a raw material to synthesize (2-(2-(((1H-pyrrol-2-yl)methyl)amino)ethyl)-3',6'-bis(dithylamino)spiro(isoindoline-1,9'-xanthen)-3-one). The structure is used as a substrate and a solution is prepared by the substrate; different metal ions are added into the solution; after ultraviolet visible light and fluorescence tests are carried out, ultraviolet and fluorescence absorption values are obviously changed after FeCl3*6H2O is added; in a certain range, the ultraviolet and fluorescence absorption values and the concentration of the Fe<3+> are in a linear relation so as to invent the fluorescence sensor for specially detecting the Fe<3+> based on the rhodamine B. The sensor has great application potential in medical and environmental sciences.

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.

The invention discloses a Cr<3+> sensor based on rhodamine B as well as a preparation and application of the Cr<3+> sensor. The intensity change of a characteristic peak of a rhodamine probe in a water phase is determined by adopting an ultraviolet-visible spectrophotometer and a fluorospectro photometer, so as to determine the presence of Cr<3+>. A target product 2,2'-sulfo-bi(N-(2-(3',6'-bi(lignocaine)-3-oxospiro[isoindoline-1,9'-xanthene]-2-yl)ethyl) acetamide) is synthesized by the rhodamine B as a precursor. The invention provides application of the target product in Cr<3+> detection; and the target product has a good detection effect on Cr<3+>. Compared with the prior art, the Cr<3+> sensor is easily available in raw materials, and simple in synthesis step, and has great application prospect in detection of the Cr<3+>; post-treatment is also convenient; and large-scale production is relatively easy to achieve.

The invention discloses a rhodamine B-based fluorescent sensor, preparation and application thereof. 2-(2-aminoethyl)-3',6'-bis(diethyl-amino)spiro[isoindoline-1,9'-xanthen]-3-one(A) and 4-(1,4,7,10-tetraoxa-13-azacycl-opentadecan-13-yl)-4-oxobutanoicacid(B) are taken as precursors to synthesize a fluorescent sensor (C). After addition of different heavy metal ions like NaCl, LiCl.H2O, KCl, NiCl, CuCl, AgNO3, SnCl2.2H2O, Ba(NO3)2, MnCl2.4H2O, ZnCl12, MgCl2.6H2O, CaCl2, CdCl2.2.5H2O, CuCl2.2H2O, FeCl2.4H2O, PbCl2, CoCl2.6H2O, HgCl2, Pd(C2H3O2)2, RhCl3.H2O, IrCl3, AlCl3, FeCl3.6H2O, and CrCl3.6H2O, analysis by ultraviolet-visible spectrum and spectrofluorimetry finds that the sensor only responses to iron ions, so that the fluorescent sensor can be used for specially detecting iron ions. The sensor has advantages of high sensitivity, simple operation and good specificity, and has important potential significance in disease diagnosis.

The invention relates to a synthesis method for 5-aminolevulinic acid hydrochloride. The synthesis method comprises the steps as follows: taking 1,3-dichloroacetone as a starting material, carrying out Gabriel reaction on the 1,3-dichloroacetone and phthalimide potassium in a water phase or an organic phase to obtain a high-purity intermediate (I), 2-(3-chloro-2-oxopropyl)isoindoline-1,3-diketone; reacting the intermediate (I) with malonic acid isopropyl ester or malonic acid diethyl ester in alkali condition to prepare an intermediate (II), 2-(3-(2,2-dimethyl-4,6-dioxo-1,3-dioxane-5-yl)-2-oxopropyl)isoindoline-1,3-diketone or an intermediate (III), 2-(3-(1,3-dioxoisobenzazole-2-yl)-2-oxopropyl)malonic acid diethyl ester; and hydrolyzing, decarboxylating and post-processing to obtain the high-purity 5-aminolevulinic acid hydrochloride.

Substituted 2-(2,6-dioxopiperidin-3-yl)-phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines reduce the levels of TNFα in a mammal. A typical embodiment is 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroisoindoline.

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.

This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.

The invention relates to a method for preparing 3-imino isoindoline ketone compounds and particularly discloses a method for preparing the 3-imino isoindoline ketone compounds through the activation method of palladium catalysis of the C-H bond, wherein the 3-imino isoindoline ketone compounds are as shown in the formula I (refer to the Specification). The method comprises the following steps: under the existence of an inert solvent, under the catalysis of a palladium catalyst, and under the action of an oxidizing agent, the compounds II (N-alkoxy amide compounds) and the compounds III (isonitrile compounds) react to obtain the compounds I, wherein the structures of the compounds I, compounds II and compounds III are as shown in the Specification. The method is high in efficiency, excellent in selectivity, economical, environment friendly, fewer in steps, simple and convenient to operate, wide in application range of substrates, and excellent in atom economy. The invention further provides a method for further conversion of the compounds I.

There is provided a pharmaceutical composition comprising (1) (R)-5,6-dimethoxy-2-[2,2,4,6,7-pentamethyl-3-(4-methylphenyl)-2,3-dihydro-1-benzofuran-5-yl]isoindoline, (2) a lipophilic component, and (3) a surfactant, which can stably and sufficiently provide improvement in the absorbability of the drug without being affected by the amount and quality of a meal.