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152 results about "Ditazole" patented technology

Ditazole is a non-steroidal anti-inflammatory agent with analgesic and antipyretic activity similar to phenylbutazone. It is also a platelet aggregation inhibitor which is marketed in Spain and Portugal under the trade name Ageroplas.

Therapeutic agent

Agent for the depletion of an unwanted protein population from the plasma of a subject, which agent comprises a plurality of ligands covalently co-linked so as to form a complex with a plurality of the proteins in the presence thereof, wherein at least two of the ligands are the same or different and are capable of being bound by ligand binding sites present on the proteins, wherein the agent is a non-proteinaceous agent other than a D-proline of the formulawhereinR isthe groupR1 is hydrogen or halogen;X is —(CH2)n—; —CH(R2)(CH2)n—; —CH2O(CH2)n—; —CH2NH—; benzyl, —C(R2)═CH—; —CH2CH(OH)—; or thiazol-2,5-diyl;Y is —S—S—; —(CH2)n—; —O—; —NH—; —N(R2)—; —CH═CH—; —NHC(O)NH—;—N(R2)C(O)N(R2)—; —N[CH2C6H3(OCH3)2]—; —N(CH2C6H5)—; —N(CH2C6H5)C(O)N(CH2C6H5)—; —N(alkoxyalkyl)-; N(cycloalkyl-methyl)-; 2,6-pyridyl; 2,5-furanyl; 2,5-thienyl; 1,2-cyclohexyl; 1,3-cyclohexyl; 1,4-cyclohexyl; 1,2-naphthyl; 1,4-naphthyl; 1,5-naphthyl; 1,6-naphthyl; biphenylen; or 1,2-phenylen, 1,3-phenylen and 1,4-phenylen, wherein the phenylen groups are optionally substituted by 1-4 substituents, selected from halogen, lower alkyl, lower alkoxy, hydroxy, carboxy, —COO-lower alkyl, nitrilo, 5-tetrazol, (2-carboxylic acid pyrrolidin-1-yl)-2-oxo-ethoxy, N-hydroxycarbamimidoyl, 5-oxo[1,2,4]oxadiazolyl, 2-oxo-[1,2,3,5]oxathiadiazolyl, 5-thioxo[1,2,4]oxadiazolyl and 5-tert-butylsulfanyl-[1,2,4]oxadiazolyl;X′ is —(CH2)n—; —(CH2)nCH(R2)—; —(CH2)nOCH2—; —NHCH2—; benzyl, —CH═C(R2)—; —CH(OH)CH2; or thiazol-2,5-diyl;R2 is lower alkyl, lower alkoxy or benzyl andn is 0-3,or a pharmaceutically acceptable salt or mono- or diester thereof.
Owner:PENTRAXIN THERAPEUTICS LTD

Combinations comprising methotrexate and dhodh inhibitors

The present invention provides a combination which comprises (a) methotrexate and (b) a non-hepatotoxic DHODH inhibitor of formula (I): wherein: R1 is selected from the group consisting of hydrogen atoms, halogen atoms, C1-4 alkyl, C3-4 cycloalkyl, —CF3 and —OCF3, R2 is selected from the group consisting of hydrogen atoms, halogen atoms and C1-4 alkyl groups, R3 is selected from the group consisting of —COOR5, —CONHR5, tetrazolyl, —SO2NHR5 and —CONHSO2R5 groups, wherein R5 is selected from the group consisting of a hydrogen atom and linear or branched C1-4 alkyl groups, R4 is selected from the group consisting of a hydrogen atom and a C1-4 alkyl group, R9 is selected from the group consisting of a hydrogen atom and a phenyl group, G1 represents a group selected from N and CR6 wherein R6 is selected from the group consisting of hydrogen atoms, halogen atoms, C1-4 alkyl, C3-4 cycloalkyl, C1-4 alkoxy, —CF3, —OCF3, monocyclic N-containing C5-7 heteroaryl, monocyclic N— containing C3-7 heterocyclyl groups and C6-10 aryl groups which C6-10 aryl groups are optionally substituted with one or more substituents selected from halogen atoms and C1-4 alkyl groups, G1 represents a group selected from N and CR6 wherein R6 is selected from the group consisting of hydrogen atoms, halogen atoms, C1-4 alkyl, C3-4 cycloalkyl, C1-4 alkoxy, —CF3, —OCF3, mono-cyclic N-containing C5-7 heteroaryl, monocyclic N— containing C3-7 heterocyclyl groups and C6-10 aryl groups which C6-10 aryl groups are optionally substituted with one or more substituents selected from halogen atoms and C1-4 alkyl groups, G2 represents a group selected from: a hydrogen atom, a hydroxy group, a halogen atom, a C3-4 cycloalkyl group, a C1-4 alkoxy group and —NRaRb, wherein Ra represents a C1-4 alkyl group and Rb is selected from a group consisting of C1-4 alkyl group and C1-4alkoxy-C1-4 alkyl group, or Ra and Rb together with the nitrogen atom to which they are attached form a saturated 6 to 8 membered heterocyclic ring optionally containing one oxygen atom as an additional heteroatom, a monocyclic or bicyclic 5 to 10 membered heteroaromatic ring containing one or more nitrogen atoms which is optionally substituted by one or more substituents selected from halogen atoms, C1-4 alkyl, C1-4 alkoxy, C3-4 cycloalkyl, C3-4 cycloalkoxy, —CF3, —OCF3, and —CONR7R8, wherein R7 and R8 are independently selected from hydrogen atom, linear or branched C1-4 alkyl groups, C3-7 cycloalkyl groups, or R7 and R8 together with the nitrogen atom to which they are attached form a group of formula wherein n is an integer from 0 to 3, and a phenyl group which is optionally substituted by one or more substituents selected from halogen atoms, C1-4 alkyl, hydroxyl, C1-4 alkoxy, C3-4 cycloalkyl, C3-4 cycloalkoxy, cyano, —CF3, —OCF3, —CONR7R8, oxadiazolyl, triazolyl, pyrazolyl and imidazolyl groups, which oxadiazolyl, triazolyl, pyrazolyl and imidazolyl groups are optionally substituted by C1-4 alkyl or C3-7 cycloalkyl groups and wherein R7 and R8 are independently selected from hydrogen atom, linear or branched C1-4 alkyl groups, C3-7 cycloalkyl groups, or R7 and R8 together with the nitrogen atom to which they are attached form a group of formula wherein n is an integer from 0 to 3 or, when G′ represents CR6, G2 together with R6 forms a non-aromatic C5-10 carbocyclic group or a C6-10 aryl group, and the pharmaceutically acceptable salts and N-oxides thereof.
Owner:ALMIRALL

Indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one derivatives

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formulawhereinAr is a 6-membered heteroaryl group, containing one or two N-atoms, which are the groups, pyridinyl, pyrimidinyl, pyridazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms, selected from N, S or O, which groups are imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl;R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl;R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o—O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o—S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o—S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3;R3 is halogen or lower alkyl;X is CH or N;X1 is CH or N;n is 1 or 2;is 0, 1, 2 or 3;m is 0, 1 or 2;and the dotted line indicates a bond may or may not be present; or,a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and / or optical isomer and / or stereoisomer thereofThe compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.
Owner:F HOFFMANN LA ROCHE & CO AG

Tegafur derivative containing 1,3,4-thiadiazole heterocyclic ring and amide group

The invention provides a tegafur derivative containing a 1,3,4-thiadiazole heterocyclic ring and an amide group. The structural formula of the tegafur derivative is as shown in the specification. A preparation method of the tegafur derivative comprises the steps of (1) dissolving a 3-(methoxycarbonylmethyl)tegafur in methanol, dropwise adding a sodium hydroxide solution, extracting by using ethyl acetate and distilled water and separating out an organic layer and a water layer, next, extracting by using ethyl acetate and blending the organic layers, and adding anhydrous sodium sulfate to obtain 1-(tetrahydro-2-furyl)-3-carbethoxy-5-fluoro-2,4-pyrimidinedione; (2) blending 1-(tetrahydro-2-furyl)-3-carbethoxy-5-fluoro-2,4-pyrimidinedione with dioxane, then adding sulfoxide chloride to obtain a 1-(tetrahydro-2-furyl)-3-chloracetyl-5-fluoro-2,4-pyrimidinedione solution, and then adding dioxane, evenly mixing and then sealing for later use; (3) taking 2-amino-5-p-nitrophenyl-1,3,4-thiadiazole, dioxane and triethylamine, and dropwise adding the 1-(tetrahydro-2-furyl)-3-chloracetyl-5-fluoro-2,4-pyrimidinedione solution obtained in the step (2) to obtain a pure product 1-(tetrahydro-2-furyl)-3-acetamido-[5-p-nitrophenyl-(1,3,4-thiadiazole-2-yl)]-5-fluoro-2,4-pyrimidinedione. The tegafur derivative has anti-tumor effect and no obvious toxicity, and is used for clinically treating malignant tumors.
Owner:INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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