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Benzisothiazole and benzisoxazole piperazine derivatives

Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is benzisothiazol-3-yl or benzisoxazol-3-yl and the other is alkylene attached to heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione and spirocyclopentylthiazolidinedione or butyrophenone-like groups. The compounds have psychotropic properties and 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspior[4.5]decane-7,9-dione is a typical embodiment having selective antipsychotic activity.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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TRICYLIC DELTA 3-PIPERIDINES AS PHARMACEUTICALS

The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C 1-6alkanediyl; n is 1 or 2; X is–O–,–S–,–S(=O)–or–S(=O) 2–; each R 1is independently hydrogen, halogen, C 1-6alkyl, nitro, hydroxy or C 1-4alkyloxy; D is an indole, a benzisoxazole, a benzisothiazole, a 2H-benzopyranone, a phenoxyphenyl, a benzamide, a benzophenone or a benzopyrimidinone having central alpha 2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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1,2-benzoisoxazole derivative or its salt and brain-protecting agent comprising the same

This invention relates to a 1,2-benzoisoxazole derivative represented by the following general formula (I) or its salt: STR1

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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,
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Iridium(I)-Catalyzed alpha-C(sp3)-H Alkylation of Saturated Azacycles

Saturated azacycles are commonly encountered in bioactive compounds and approved therapeutic agents. The development of methods for functionalization of the alpha-methylene C-H bonds of these highly privileged building blocks is of great importance, especially in drug discovery. While much effort has been dedicated toward this goal by using a directed C-H activation approach, the development of directing groups that are both general as well as practical remains a significant challenge. Herein, the design and development of novel amidoxime directing groups is described for Ir(I)-catalyzed alpha-C(sp3)-H alkylation of saturated azacycles using readily available olefins as coupling partners. This protocol extends the scope of saturated azacycles to piperidines, azepane, and tetrahydroisoquinoline that are incompatible with our previously reported directing group. A variety of olefin coupling partners, including previously unreactive disubstituted terminal olefins and internal olefins, are compatible with this transformation. The selectivity for a branched alpha-C(sp3)-alkylation product is also observed for the first time when acrylate is used as the reaction partner. The development of practical, one-step installation and removal protocols further adds to the utility of amidoxime directing groups.

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PROLINE DERIVATIVES AND USE THEREOF AS DRUGS

The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products.The present inventors have found that derivatives having a substituent introduced into the gamma-position of proline represented by the formula (I)wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

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Benzisoxazole – Wikipedia,
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N-coating heterocyclic compounds

A compound of the formula (I): wherein A is a hydrogen atom, an optionally substituted, unsaturated, N-containing heterocyclic group or a group of the formula (a): wherein R is an optionally substituted aryl group or an optionally substituted heterocyclic group; M is ?(CH2)n-, ?(CH2)n-O?(CH2)m-or ?(CH2)n-NH?(CH2)m-, wherein n and m are independently 0, 1 or 2; Q is an optionally substituted cycloalkylene group, an optionally substituted arylene group or an optionally substituted divalent heterocyclic group; and the moiety of the formula (b): is an optionally substituted, unsaturated, mono-, di-, tri- or tetra-cyclic, N-containing heterocyclic group which may contain additional hetero atom(s) selected from the group consisting of nitrogen, oxygen and sulfur atoms as the ring member(s), its prodrug or a pharmaceutically acceptable salt thereof.

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PYRIDYLOXYMETHYL AND BENZISOXAZOLE AZABICYCLIC DERIVATIVES

An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound according to formula (I) a pharmaceutical composition comprising same, and a method of treating one or more CNS or other disorders, including concurrent treatment of disorders such as chizophrenia and depression. Or the (R) or (S) enantiomer thereof, or the cis or trans isomer thereof, or a pharmaceutically acceptable salt, solvate or prodrug thereof, or of any of the foregoing, wherein m is 0 or 1, Z is wherein R7 is hydrogen or (C1-C3)alkoxy; R8 is hydrogen, hydroxy, or (C1-C3)alkoxy; and R9 is (C1-C3)alkoxy; X is oxygen or NR, wherein R is hydrogen or (C1-C6)alkyl; Y is methylene, wherein n is 0, 1 or 2; or oxygen, nitrogen or sulfur, wherein n is 2, 3 or 4; R1 and R2 are each independently hydrogen, halogen, or a (C1-C6) alkyl, (C1-C6)alkoxy or a (C1-C6) alkoxy(C1-C6)alkyl group, any one of which groups may be unsbustituted or substituted with one or more halogens.

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Synthesis of an Optically Active Octahydro-2H-pyrido<1,2-a>pyrazine Based CNS Agent

A synthesis of an optically active octahydro-2H-pyrido<1,2-a>pyrazine is presented.The key sequence involved the equilibration of an optically active cis-aldehyde to give the thermodynamic transaldehyde that was trapped by nitromethane anion.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics