171 results about "Ditazole" patented technology

For the purpose of providing a GSK-3β inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (I):wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

PCT No. PCT / US96 / 11613 Sec. 371 Date Sep. 14, 1998 Sec. 102(e) Date Sep. 14, 1998 PCT Filed Jul. 12, 1996 PCT Pub. No. WO97 / 03945 PCT Pub. Date Feb. 6, 1997Compounds of formula (I) wherein: R1 is -(CR4R5)nC(O)O(CR4R5)mR6, -(CR4R5)nC(O)NR4(CR4R5)mR6, (CR4R5)nO(CR4R5)mR6, or -(CR4R5)rR6: W is alkynyl or 2 carbon atoms; R3 is H or R7; Z is C(O)R13, (CH2)0-1C(O)OR13, (CH2)0-1C(O)NR10R13, (CH2)0-1C(R8R8)OR8, -NHC(O)R7, (CH2)0-1NR10R13, NH[C(O)C(O)OR8], CH2NH[C(O)CNR10R13], CH2S(O)qR7, CH[S(O)qR7]2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R7 is -(CR4R5)qR11 or C1-6 alkyl wherein the R11 or C1-6 alkyl group is unsubstituted or substituted one or more times by methyl or ethyl unsubstituted or substituted by 1-3 fluorines, -NR8R10, -CO2R8, -O(CH2qR8, -NR8C(O)R8 or R12; or the pharmaceutically acceptable salts thereof.

This invention provides substituted Phenyl-(2-[1,3,4]thiadiazol-2-yl-phenyl)-amine and (2-[1,3,4]Oxadiazol-2-yl-phenyl)phenyl-amine compounds which act as inhibitors of MAPK / ERK Kinase (“MEK”) enzymes and pharmaceutical compositions and methods for their use in immunomodulation and in the treatment and alleviation of inflammation, and proliferative diseases such as cancer and restenosis.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

The present invention relates to 1,2,4-oxadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and / or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

The present invention relates to 1,3,4-oxadiazole and thiadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and / or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

The invention relates to a process for preparing a salt of an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, b) i) the product thus obtained is hydrogenated, ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand and iii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.

Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C1-C4 alkyl, or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; and Q is H, C1-6alkyl, phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents, and G is defined herein. Also disclosed are method of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. There compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory disease.

Organometallic compounds and organic electroluminescence devices employing the same are provided. The organic compound has a chemical structure as represented below:wherein, A1 is diisopropyl carbodiimide ligand, 5-(2-pyridyl)-1,2,4-triazole ligand, acetylacetone with phenyl group ligand, 2-phenyl-1,3,4-oxadiazole ligand, or derivatives thereof. The organometallic compound of the disclosure can be applied in an organic electroluminescent device for enhancing the electroluminescent efficiency thereof.

The invention discloses a rhodamine derivative and a preparation method and application thereof. The rhodamine derivative is prepared by reacting rhodamine hydrazide and 4-chloro-7-nitro-2,1,3-benzoxaoxadiazole in the presence of an acid binding agent. The Cu<2+> and Fe<3+> can be respectively detected at high selectivity and high sensitivity. The designed and synthesized structure is short in synthetic route and mild in reaction conditions, the obtained derivative can be used for an aqueous phase system, and the ultraviolet-visible absorption spectrum and fluorescence spectrum are insensitive to the acid-base property of the system.

The invention relates to a compound containing 1,3-benzodiazole connected in series with gem-difluoromethylene groups and a synthesis method thereof. The structural formula of this type of compound is: where R is: -COOEt-Ph, -COOCH3-Ph, -NO2-Ph, Ph, -OCH3-Ph, -CH3-Ph, -CH3-Ph, -NO2-Ph, Pyridine, (Z)-CH=CHCOOEt, (E)-CH=CHCOOEt or (E)-CH=CHPh; X is: O, S or NCH2CH2CH2CH3. The compounds containing 1,3-benzodiazoles in tandem with gem-difluoromethylene groups of the present invention exhibit unique properties in novel liquid crystal materials, so efficient synthesis of such compounds becomes very meaningful. The synthesis method has the characteristics of simple operation, short steps and convenient post-processing.

The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.

The invention belongs to the technical field of medicines, relates to compounds having antitumor activity and having specific chemical structures, and particularly relates to pyrimidine type antitumorcompounds having a 1,3,4-oxadiazole structure and a preparation method and application thereof. The general structure formula of the pyrimidine type antitumor compounds is shown as follows in the description. The novel compounds greatly improve antitumor effects, and have more excellent anti-proliferation capability for human lung cancer A549 cells when compared with pyrimidine acylhydrazine compounds. Synthetic steps are simplified in a synthesis process, thus making future industrial production possible.

A method of detecting creatinine in body fluids using an indicator which produces a fluorescent response when oxidized in the presence of a copperII / creatinine complex. A preferred indicator is 4-(1-methylhydrazino)-7-nitro benzooxadiazole (MNBDH).

The present invention relates to 3,3'-azobis[1,2,4-oxadiazole-5-one-3-yl]-1,2,5-oxadiazole and energetic ion salts thereof, and belongs to the field of synthesis. 4-[5-amino-1,2,4-oxadiazole-3-yl-]-3-amino-1,2,5-oxadiazole is coupled by an aqueous solution of potassium permanganate to obtain 3,3'-azobis[5-amino-1,2,4-oxadiazole-3-yl-]-1,2,5-oxadiazole (compound 2), the compound 2 undergoes an oxidation reaction by a mixed solution of acetic anhydride and 100 wt% nitric acid (with a mass ratio of 2:1) to obtain 3,3'-azobis[1,2,4-oxadiazole-5-one-3-yl-]-1,2,5-oxadiazole, and the 3,3'-azobis[1,2,4-oxadiazole-5-one-3-yl-]-1,2,5-oxadiazole and an alkaline compound undergo a neutralization reaction to obtain the corresponding energetic ion salts. The above synthesis method has the advantages ofsafe and reasonable process, short reaction time, high yield, low production cost and basically no three wastes.

A pharmaceutical composition which comprises N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide with mannitol and / or 5 microcrystalline cellulose is described.

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.

For the purpose of providing a GSK-3β inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (I):wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

The present invention relates to the use of a compound of formula (I):or a pharmaceutically acceptable solvate or salt thereof in the preparation of a medicinal product for the prevention and / or the treatment of a disease in which the GLP-1 receptor participates or mediates, such as eating disorders or diseases, for example, obesity, anorexia, lipid dysfunction, diabetes, hyperinsulinism and cardiovascular diseases or metabolic syndrome.