Properties and Exciting Facts About 3-Chloro-1,2-benzisoxazole

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PIPERAZINE AND PIPERIDINE DERIVATIVES AS ANTI-HIV-AGENTS

This invention relates to a compound of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, wherein R1 to R5are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation, compositions containing them and the uses of such derivatives. The compounds of the present invention inhibit the interaction of gp120 with CD4 and are 10 therefore of use in the treatment of HIV, a retroviral infection genetically related to HIV, or AIDS.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Photochemistry of matrix-isolated 3-chloro-1,2-benzisoxazole: Generation and characterization of 2-cyanophenoxyl radical and other reactive intermediates

Photochemistry of 3-chloro-1,2-benzisoxazole 1 in N2 and Ar matrices at 10 K leads to N-chloro-ketenimine 3 and 2-cyanophenyl-hypochlorite 4. The reaction kinetics and the observed photoisomerization of 3 to 4 indicate that ketenimine 3, possibly formed via an elusive vinylnitrene VN, is an intermediate in the formation of hypochlorite 4. A new pathway involving the formation of 2-cyanophenoxyl radical 5, which was captured only in Ar matrix, was also observed. Radical 5 is possibly formed via photodetachment of Cl atom from 1 (or VN) and might explain the formation of 3-chloro-6-oxocyclohexa-1,4-dienecarbonitrile 2 in N2 and Ar matrices. All the species were characterized by IR spectroscopy and theoretical calculations. The computed geometric and electronic structure of radical 5 is discussed. Overall, the results provided further insight into the mechanism of the photochemistry of 1,2-benzisoxazoles and allowed characterization of new interesting reactive intermediates.

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Method for treating allergies using substituted pyrazoles

A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Synthesis and Biological Evaluation of 1-(1,2-Benzisothiazol-3-yl)- and (1,2-Benzisoxazol-3-yl)piperazine Derivatives as Potential Antipsychotic Agents

Members of the series of title compounds were tested for potential antipsychotic activity in relevant receptor binding assays and behavioral screens.Structure-activity relationships within the series are discussed.Compound 24 (BMY 13859-1), a (1,2-benzisothiazol-3-yl)piperazine derivative, was selected for further study because of its potent and selective profile in primary CNS tests.It was active in the Sidman avoidance paradigm and blocked amphetamine-induced stereotyped behavior in dogs for up to 7 h.The compound’s lack of typical neuroleptic-like effects in therat catalepsy test and its failure to produce dopamine receptor supersensitivity following chronic administration indicate that it should not cause the movement disorders commonly associated with antipsychotic therapy.Although 24 has potent affinity for dopaminergic binding sites, its even greater affinity for serotonin receptors suggests that a serotonergic component may be relevant to its atypical profile.Compound 24 is currently undergoing clinical evaluation in schizophrenic patients.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY

The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R 1) n represents 0, 1, or 2 substituents, which can be the same or different, from the group C 1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono-or dialkyl (C 1-2)-amino, sulfonyl-(C 1-3)alkyl or-alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono-or dialkyl (C 1-2)-amino, X is O, S, NH or NCH 3, Y represents CH 2, or (CH 2) 2, (R 2) m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R 2) mis a methylene bridge or ethylene bridge, A is a group–CH 2–(CRH) p–wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2-or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono-or dialkyl (C 1-2)amino, sulfonyl-(C 1-3)alkyl or-alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono-or dialkyl (C 1-2)-amino.

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Benzisoxazole – Wikipedia,
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OXINDOLE SUBSTITUTED PIPERAZINE DERIVATIVES

The invention relates to compounds of the formula (I), wherein Ar, A, R, R1, R2, R3, R4 and R5 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of 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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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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3-O-HETEROARYL-INGENOL

The present invention relates to a compound according to formula (I) wherein R1 represents optionally substituted heteroaryl, and pharmaceutically acceptable salts, hydrates, solvates or pharmaceutically acceptable and physiologically cleavable esters thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. diseases associated with hyperplasia, neoplasia or dysplasia, with said compounds, to methods of treatment of cosmetic indications with said compounds, and to the use of said compounds in the manufacture of medicaments.

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Benzisoxazole – Wikipedia,
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Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase

This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.

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METHODS OF USING PIPERIDYL-BENZISOXAZOLE AND BENISOTHIAZOLE DERIVATIVES AS CHOLINESTERASE INHIBITORS

Disclosed herein are compounds of the formula wherein R1 R2, R7, R8, X, Y, M and L are defined as below The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer’s disease

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Reference£º
Benzisoxazole – Wikipedia,
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