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Ortho Effects in Shiff Bases of Diaminodicyanoethane

In the electron impact mass spectra of azomethines derived from various substituted aromatic aldehydes and diaminodicyanoethene the superposition of two ortho effects concurring with the azomethine group is apparent: one involving the amino group of the diaminodicyanoethene part accounts for the cyclization to + ions and the other involving ortho substituents of the benzylidene part which can interact with the azomethine moiety is responsible for specific fragment ions, suppressing the typical fragmentations of azomethines.The ortho effect was studied for the o-nitro derivative by labelling experiments, analysis of metastable transitions and collisional activation comparing model ions, demonstrating that the specific +. and +. ions are the result of cyclization processes.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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MUSCARINIC AGONISTS

Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Compounds and uses thereof for decreasing activity of hormone-sensitive lipase

Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Benzo[d]isoxazol-3-ol DAAO inhibitors

Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer”s disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein

  • Z1 is N or CR3;
  • Z2 is N or CR4;
  • Z3is O or S;
  • A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof;
  • R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2;
  • R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl;
  • at least one of R1, R2, R3 and R4 is other than hydrogen; and
  • at least one of Z1 and Z2 is other than N.

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    Reference£º
    Benzisoxazole – Wikipedia,
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METHOD FOR THE PREPARATION OF FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

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Benzisoxazole – Wikipedia,
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1,2-BENZISOXAZOL-3(2H)-ONE.

A new condensing agent, N,N prime -carbonyldi left bracket 1,2-benzisoxazol-3(2H)-one right bracket (6), was readily prepared by the reaction of 1,2-benzisoxazol-3-ol and trichloromethyl chloroformate in toluene. The condensing agent 6 was shown to be very useful for the preparation of amides, esters, and dipeptides under mild conditions. A successful polyamide synthesis by one-pot polycondensation of isophthalic acid with diamines using 6 is also described.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Preparation of heterocyclic pharmaceutical compositions as muscarinic agonists.

Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Muscarinic agonists

Compounds are provided which are useful in the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4 or both m1 and m4, receptor activity has a beneficial effect. Also a use is provided of the compounds in the manufacture of pharmaceutical compositions for treating such diseases and conditions.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Hepatitis C virus inhibitors

Macrocyclic peptides are disclosed having the general formula: wherein R?, R3, R3?, R4, R6, 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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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Chromatography-free, Mitsunobu-triggered heterocyclizations of salicylhydroxamic acids to 3-hydroxybenzisoxazoles

The Mitsunobu reaction has become one of the most powerful tools to alkylate acidic pronucleophiles. A significant caveat of Mitsunobu chemistry, however, is that the reaction mixture is often plagued with purification problems owing to the phosphine oxide and hydrazine dicarboxylate by-products. In addition to the development of more readily separable Mitsunobu reagents, the product’s physicochemical properties may be exploited to facilitate purification. In this regard, we present a swift and efficient preparation of 3-hydroxybenzisoxazoles by the Mitsunobu-triggered heterocyclizations of salicylhydroxamic acids, which can be isolated by an acid?base work-up. As expected, a range of functional groups was compatible with the chemistry.

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