Awesome and Easy Science Experiments about 3-Chloro-1,2-benzisoxazole

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SUBSTITUTED 1-PIPERIDIN-4-YL-4-PYRROLIDIN-3-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS

This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions ; inflammation ; allergic disorders ; emesis ; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders ; vasospastic diseases ; fibrosing and collagen diseases ; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Simple exploration of Benzo[d]isoxazol-3-ol

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Inhibitors of Hepatitis C Virus

Macrocyclic peptides are disclosed having the general formula: wherein R3, R3?, R4, R6, R?, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extended knowledge of 1,2-Benzisoxazole-3-acetic Acid

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IMPROVED AND SIMPLIFIED PROCESS FOR THE PREPARATION OF 1,2-BENZISOXAZOLE-3-ACETIC ACID

A process for preparation of 1,2-benzisoxazole-3-acetic acid reacting 4-hydroxy coumarin and hydroxylamine in water according to the following scheme of reaction. Formula (I).

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

The important role of Benzo[d]isoxazol-3-amine

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Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines

We report herein the SAR studies of a series of indole- and indolizine-glyoxylamides that demonstrate substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types of various origins (e.g., breast, colon, uterine).

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Properties and Exciting Facts About 3-Methyl-1,2-benzisoxazol-6-ol

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Synthesis of 1,3-bis(heteroaryloxy)-2-hydroxypropanes as symmetrical analogs of DSCG using phase transfer catalyst and their pharmacological activities

1,3-Bis(coumarinoxy)-2-hydroxypropanes (I-III), 1,3-bis(benzisoxazoloxy)-2-hydroxypropanes (IV) and 1,3-bis(benzofuranoxy)-2-hydroxypropanes (V) have been synthesised by treating substituted hydroxycoumarins, benzisoxazoles and benzofurans respectively with epoxide in the presence of a phase transfer catalyst, and found to possess passive cutaneous anaphylaxis and antiallergic activities.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

More research is needed about Benzo[d]isoxazol-3-ol

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Discovery of isatin and 1H-indazol-3-ol derivatives as D-amino acid oxidase (DAAO) inhibitors

D-Amino acid oxidase (DAAO) is a potential target in the treatment of schizophrenia as its inhibition increases brain D-serine level and thus contributes to NMDA receptor activation. Inhibitors of DAAO were sought testing [6+5] type heterocycles and identified isatin derivatives as micromolar DAAO inhibitors. A pharmacophore and structure-activity relationship analysis of isatins and reported DAAO inhibitors led us to investigate 1H-indazol-3-ol derivatives and nanomolar inhibitors were identified. The series was further characterized by pKa and isothermal titration calorimetry measurements. Representative compounds exhibited beneficial properties in in vitro metabolic stability and PAMPA assays. 6-fluoro-1H-indazol-3-ol (37) significantly increased plasma D-serine level in an in vivo study on mice. These results show that the 1H-indazol-3-ol series represents a novel class of DAAO inhibitors with the potential to develop drug candidates.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Discovery of Benzo[d]isoxazol-3-ol

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Inhibitors of Hepatitis C Virus

Macrocyclic peptides are disclosed having the general formula: wherein R3, R3?, R4, R6, R?, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

A new application about 3,5-Dichlorobenzo[d]isoxazole

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QUINUCLIDINYLOXY-ISOXAZOLE COMPOUNDS AND THEIR THERAPEUTIC USES

Compounds of formula (I): STR1 wherein R 1 is hydrogen, halogen or alkyl; R 2 is hydrogen, alkyl, optionally substituted phenyl or a heterocycle; or R 1 and R 2 together form a group of formula–CR 4 =CR 5–CR 6 =CR 7–, where R. sup. 4, R 5, R 6 and R 7 are hydrogen, halogen, alkyl group, alkoxy, halomethyl, alkylamino, dialkylamino, hydroxy, nitro, aliphatic carboxylic acylamino or amino; and R 3 is piperidyl, substituted piperidyl or quinuclidinyl. The compounds are useful in the treatment and prophylaxis of cognitive disorders, notably senile dementia, including Alzheimer’s disease. Processes for preparing the compounds are also provided.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extended knowledge of Benzo[d]isoxazol-6-ol

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Chemistry is traditionally divided into organic and inorganic chemistry. Computed Properties of C7H5NO2, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 65685-55-4

Compositions for dental restoration

A combined chemical-light-polymerization type composition for dental restoration consists of a formulation A composed mainly of a. an ethylenically polymerizable unsaturated compound, b. a photopolymerization initiator and c. a reducing agent, and a formulation B composed mainly of d. a filler and e. an organic perioxide. The formulations A and B are separately packaged and designed to be mixed for use.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of 3-Chloro-1,2-benzisoxazole

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Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds

This application relates to compounds of the formula STR1 wherein R1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer’s disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics