53 results about "Benzoxepin" patented technology

The present invention is directed to crystal forms of the 5-HT2C agonist (S)-(8-(2,6-dichlorophenyl)-6-fluoro-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanamine hydrochloride, as well as compositions, processes of preparation, and uses thereof.

A transition metal-containing catalyzer is arranged on a particle filter installed in the exhaust gas line of an internal combustion engine and cannot be separated therefrom without being destroyed. To reduce emissions, at least one molecular sieve which retains polychlorinated dibenzodioxins and polychlorinated dibenzofurans is arranged between the transition metal-containing catalyzer and the exhaust gas outlet. Further, the input side of the molecular sieve and / or the output side of the catalyzer has an oxidation activity for hydrocarbons, polychlorinated dibenzodioxins and polychlorinated dibenzofurans upstream of the molecular sieve.

The present invention relates to a compound of the general formula (I) wherein Het is an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring having at least one nitrogen atom; R1 is hydrogen, hydroxy, C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl or C2-C4 alkynyl; R2 and R3 is each and independently selected from hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl, C2-C4 alkynyl, C1-C4 alkoxy, halogen and cyano, provided that R2 and R3 may not both be hydrogen; R4 is C1-C4 alkyl, C3-C4 cycloalkyl, C2-C4 alkenyl or C2-C4 alkynyl; Ar is an optionally substituted aromatic ring system selected from pyridinyl; 1-naphthyl; 5,6,7,8-tetrahydro-1-naphthyl; quinolinyl; 2,3-dihydro-1,4-benzodioxinyl; 1,3-benzodioxolyl; 5,6,7,8-tetrahydroquinolinyl; 5,6,7,8-tetrahydroisoquinolinyl; 5,6,7,8-tetrahydroquinazolin-4-yl; 1-benzo[b]thiophen-7-yl; 1-benzo[b]thiophen-4-yl; 1-benzo[b]thiophen-3-yl; isoquinolinyl; quinazolinyl; and indan-4-yl; or Ar is substituted phenyl; or an enantiomer thereof or any salt thereof; to a pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I and to new intermediates used in the preparation thereof.

The invention discloses a rhodamine-oxadiazole derivative and a preparation method and an application thereof. The specific preparation method comprises the following step: with N-aminoethylpiperazine, rhodamine B, DIPEA (Diisopropyl Ethyl Amine), 4-chloro-7-nitro-2, 1, 3-benzoxepin oxadiazole and K2CO3 with a mol ratio of (1-10): 1: (1-20): (1-1.5): 1 as reactants, preparing a product by a two-step-one-pot method, wherein the product can be used for H<+> ion colorimetry and used as a fluorescent probe. The structure designed and synthesized by the invention is short in synthesis route and mild in reaction conditions, an intermediate is unnecessary to be separated to obtain a target probe with a high yield, and no obvious FRET (fluorescence resonance energy transfer) exists between the oxadiazole and rhodamine fluorophores with matched spectrums in the structure, so that the H<+> can be detected through three channels, and the rhodamine-oxadiazole derivative has high selectivity, high sensitivity and large application potential.

Deuterium-labeled 4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidines substituted with pyrrolo[3,4-b]pyridin-5-one, furo[3,4-b]pyridin-5(7H)-one, or [1,2,4]triazolo[4,3-a]pyrimidin-3(2H)-one are positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

This invention relates to a highly reliable material for an organic electroluminescent element exhibiting high luminance, high luminous efficiency, little deterioration in emission, and suitability for use and storage at high temperatures and to an organic electroluminescent element using said material. The material is a diaminodibenzodioxin derivative represented by general formula (1)wherein Ar1, Ar2, Ar3, and Ar4 are substituted or unsubstituted aryl groups and Ar1, Ar2, and the nitrogen atom bonded thereto or Ar3, Ar4, and the nitrogen atom bonded thereto may form a nitrogen-containing heterocyclic ring; and this diaminodibenzodioxin derivative may be incorporated in the light-emitting layer, the hole-transporting layer, or the hole-injecting layer of an organic electroluminescent element.

This invention relates to a highly reliable material for an organic electroluminescent element exhibiting high luminance, high luminous efficiency, little deterioration in emission, and suitability for use and storage at high temperatures and to an organic electroluminescent element using said material. The material is a diaminodibenzodioxin derivative represented by general formula (1) wherein Ar1, Ar2, Ar3, and Ar4 are substituted or unsubstituted aryl groups and Ar1, Ar2, and the nitrogen atom bonded thereto or Ar3, Ar4, and the nitrogen atom bonded thereto may form a nitrogen-containing heterocyclic ring; and this diaminodibenzodioxin derivative may be incorporated in the light-emitting layer, the hole-transporting layer, or the hole-injecting layer of an organic electroluminescent element.

A transition metal-containing catalyzer is arranged on a particle filter installed in the exhaust gas line of an internal combustion engine and cannot be separated therefrom without being destroyed. To reduce emissions, at least one molecular sieve which retains polychlorinated dibenzodioxins and polychlorinated dibenzofurans is arranged between the transition metal-containing catalyzer and the exhaust gas outlet. Further, the input side of the molecular sieve and / or the output side of the catalyzer has an oxidation activity for hydrocarbons, polychlorinated dibenzodioxins and polychlorinated dibenzofurans upstream of the molecular sieve.

Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.

A compound of Formula (I) or a pharmaceutically acceptable salt thereof:wherein:R1 represents a group selected from:i) phenyl optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2;furanyl, thiophenyl, pyrrolyl, pyridyl, cyclohexyl or naphthyl, each of which is optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2; andiii) benzo[1,3]dioxo5-yl or 2,3-dihydrobenzo[1,4]dioxin-6-yl;R2 represents CF3, C1-4alkyl, or CHF2;when R1 represents optionally substituted furanyl, thiophenyl, pyrrolyl, pyridyl or naphthyl, R3 represents Et;when R1 represents optionally substituted cyclohexyl, R3 represents Et or Me;otherwise R3 represents Et, Me, Br or OMe,compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided, together with certain novel compounds.

Benzodioxino-naphtho[1,2-b]pyran compounds having particularly advantageous photochromic properties, such as, high sensitivity / coloration, two distinct absorption bands in the 430-500 nm range and 520-620 nm range of the visible spectrum may be generally described as a naphthopyran having a central nucleus of the formula: wherein F is a 1,4-benzodioxine ring with its 2,3 positions fused to the i, j, or k faces; and R1 and R2 are the atoms or groups providing photochromic properties to the naphthopyran.

The present invention relates to novel 1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Compounds of the general formula Iwhereineach of m and n is independently 0 or 1;R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—;R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3;X is a bond, —CH2—, or —NH—;A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; andR4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy;or pharmaceutically acceptable salts, hydrates or solvates thereof,have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.

A process for the stereoselective preparation of insecticide 6,7,8,9,10,10-hexahalo-1,5,5a,6,9,9a-hexahydro-6,9-methano-2,4,3-benzodioxathiepin-3-oxide of the general formula I:wherein X is a halogen such as fluorine, chlorine or bromine. The process comprises reacting 1,4,5,6,7,7-hexahalo-5-norbornene-2,3-dimethanol of the general formula IV:wherein X is as defined above, with a cyclic sulfite ring forming reagent optionally in an inert organic solvent at ambient to 139° C., wherein the reaction is carried out in the presence of a stereo isomer directing agent comprising an isomer of the compound of the formula I different from the desired isomer. The molar ratio of the stereoisomer directing agent to the dimethanol compound of the formula IV is at least 0.07.

The invention relates to a pharmaceutical composition of a polycyclic anaplastic lymphoma kinase inhibitor as well as a preparation method and application of the pharmaceutical composition. In particular to a pharmaceutical preparation of 5-chloro-N4-(2-(isopropyl sulfonyl) phenyl)-N2-(7-methyl-8-(piperidine-4-yl)-2, 3-dihydrobenzo [b] [1, 4] dioxin-5-yl) pyrimidine-2, 4-diamine, a method for preparing the pharmaceutical preparation and application of the pharmaceutical preparation.

The invention relates to a salt and a crystal form of a polycyclic anaplastic lymphoma kinase inhibitor, a preparation method of the salt and the crystal form, a pharmaceutical composition containing the salt and the crystal form, and application of the salt and the crystal form or the pharmaceutical composition. Specifically, the invention relates to a salt and a crystal form of a compound 5-chloro-N4-(2-(isopropyl sulfonyl) phenyl)-N2-(7-methyl-8-(piperidine-4-yl)-2, 3-dihydrobenzo [b] [1, 4] dioxin-5-yl) pyrimidine-2, 4-diamine used as an anaplastic lymphoma kinase inhibitor, a preparation method of the salt and the crystal form, a pharmaceutical composition containing the salt and the crystal form, and a preparation method of the pharmaceutical composition. The invention also discloses application of the salt and the crystal form or the pharmaceutical composition in drugs for preventing and / or treating anaplastic lymphoma kinase mediated cancers or non-cancerous related diseases.

A pharmaceutical composition of a polycyclic anaplastic lymphoma kinase inhibitor, a preparation method therefor, and use thereof. In particular, the present disclosure relates to a pharmaceutical preparation of 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(7-methyl-8-(piperidin-4-yl)-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)pyrimidine-2,4-diamine, a preparation method therefor, and use thereof.

The invention belongs to the technical field of medicinal chemistry. The invention discloses a novel protein kinase inhibitor, of which the structural formula is shown as a formula I, wherein, R1 represents hydroxyl, carboxyl, acylamino or hydrogen; R2 represents nitro, amino, acylamino, hydroxyl, sulfydryl, halogen or trifluoromethyl; R3 represents alkoxy or hydroxyl; ring A represents benzopyrone, 1H-benzo[d]imidazole, substituted hydroxyl 1H-benzo[d]imidazole, benzoxazole, 1H-pyrrolo[2, 3-b]pyridine, benzopyrrole, 2, 3-dihydrobenzo[b][1, 4]dioxin, or 1H-indazole; X represents an ester groupor an amide group; and ring B represents a benzene ring, a nitrogen-containing five-membered heterocyclic ring or a nitrogen-containing six-membered heterocyclic ring. According to the invention, a novel protein kinase inhibitor is obtained by utilizing a splicing principle, and an anti-tumor effect is achieved by inhibiting tumor cell proliferation and promoting tumor cell apoptosis.

Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy) piperidin-1-yl)-[1,2,4]triazolo[4,3-b]pyridazine of formula (Ib), which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

The present invention relates to a method for preparing an ethanol extract of Ecklonia cava, and a composition for preventing, alleviating or treating cognitive dysfunction, comprising same as an active ingredient. The ethanol extract of Ecklonia cava, of the present invention, contains phlorotannin oligomer, eckol, 7-phloroeckol, 6,6'-bieckol, 6,8'-bieckol, dibenzodioxin-fucodiphlorethol, diekcol, phlorofuroeckol A and 2,7''- phloroglucinol-6,6'-bieckol in ratios of 1-2 : 5-6 : 6.5-7.5 : 7-8 : 20-21 : 3-4 : 47-48 : 4.5-5.5 : 1.5-2.5, respectively, has excellent effects of improving behavioral function, improving antioxidant system, improving mitochondrial function, improving cholinergic system, alleviating toxicity caused by Aβ aggregation and Tau hyperphosphorylation, improving inflammation and inhibiting cell death, and thus can be effectively used as a pharmaceutical composition or health functional food composition for preventing, alleviating, or treating cognitive dysfunction.

The present invention relates to alpha2-adrenergic receptor subtype C (alpha-2C) antagonists, in particular 3-substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)azacycles of formula (I), for use in a method for the treatment and / or prevention of sleep-related breathing disorders, preferably obstructive and central sleep apnea and snoring.

The present invention relates to novel 1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a preparation method of 1-(5-methoxy-2, 3-dihydro-1, 4-benzodioxane-8-yl) ethanone. Comprising the following steps: cuprous cyanide and an initial raw material are added into N, N-dimethylformamide for nitrogen displacement, and the initial raw material is 5-bromo-8-methoxy-2, 3-dihydro-benzo [1, 4] dioxin or 5-chloro-8-methoxy-2, 3-dihydro-benzo [1, 4] dioxin; cooling after the reaction, adding ammonia water, extracting, combining organic phases, and purifying to obtain 5-cyano-8-methoxy-2, 3-dihydro-benzo [1, 4] dioxin; the preparation method comprises the following steps: reacting 5-cyano-8-methoxy-2, 3-dihydro-benzo [1, 4] dioxin with anhydrous tetrahydrofuran, dropwise adding a tetrahydrofuran solution of a methyl Grignard reagent, and reacting until no 5-cyano-8-methoxy-2, 3-dihydro-benzo [1, 4] dioxin exists; the method comprises the following steps of: extracting, concentrating and drying, and purifying to obtain the 1-(5-methoxy-2, 3-dihydro-1, 4-benzodioxane-8-yl) ethanone, namely the 1-(5-methoxy-2, 3-dihydro-1, 4-benzodioxane-8-yl) ethanone. The method has the advantages of easily available raw materials, stable process and simple operation. The method can be applied to isotope labeling synthesis of C13 and C14 compounds.

The invention relates to a crystal form of a polycyclic anaplastic lymphoma kinase inhibitor, a preparation method of the crystal form, a pharmaceutical composition containing the crystal form, and application of the crystal form or the pharmaceutical composition. Specifically, the invention relates to a crystal form of a compound 5-chloro-N4-(2-(isopropyl sulfonyl) phenyl)-N2-(7-methyl-8-(piperidine-4-yl)-2, 3-dihydrobenzo [b] [1, 4] dioxin-5-yl) pyrimidine-2, 4-diamine as shown in a formula (1) as an anaplastic lymphoma kinase inhibitor, a preparation method of the crystal form, a pharmaceutical composition containing the crystal form, and an application of the crystal form or the pharmaceutical composition in medicines for preventing and / or treating anaplastic lymphoma kinase mediated cancers or non-cancerous related diseases.

Deuterium-labeled 4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidines substituted with pyrrolo[3,4-b]pyridin-5-one, furo[3,4-b]pyridin-5(7H)-one, or [1,2,4]triazolo[4,3-a]pyrimidin-3(2H)-one are positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.