Category: 99822-23-8

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Discovery and lead optimisation of a potent, selective and orally bioavailable RARbeta agonist for the potential treatment of nerve injury

Oxadiazole replacement of an amide linkage in an RARalpha agonist template 1, followed by lead optimisation, has produced a highly potent and selective RARbeta agonist 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (10) with good oral bioavailability in the rat and dog. This molecule increases neurite outgrowth in vitro and induces sensory axon regrowth in vivo in a rodent model of avulsion and crush injury, and thus has the potential for the treatment of nerve injury.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Chemistry, like all the natural sciences, category: Benzisoxazole, begins with the direct observation of nature¡ª in this case, of matter. In a Article£¬Which mentioned a new discovery about 99822-23-8.

A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists

Moderately potent, selective S1P1 receptor agonists identified from high-throughput screening have been adapted into lipophilic tails for a class of orally bioavailable amino acid-based S1P1 agonists represented by 7. Many of the new compounds are potent S1P1 agonists that select against the S1P2, S1P3, and S1P4 (although not S1P5) receptor subtypes. Analogues 18 and 24 are highly orally bioavailable and possess excellent pharmacokinetic profiles in the rat, dog, and rhesus monkey.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Related Products of 99822-23-8, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 99822-23-8, Name is 5-Fluorobenzo[d]isoxazol-3(2H)-one, molecular formula is C7H4FNO2, introducing its new discovery.

One Base for Two Shots: Metal-Free Substituent-Controlled Synthesis of Two Kinds of Oxadiazine Derivatives from Alkynylbenziodoxolones and Amidoximes

Different 1,2-migrations and cyclizations of a variety of alkynylbenziodoxolones (EBXs) and amidoximes under one-base conditions are described. This process provides an efficient protocol for the divergent synthesis of two oxadiazine derivatives via switchable selectivity of EBXs controlled by simply varying the substituents of the amidoximes, which feature transition metal-free conditions, simple execution, and high chemoselectivity.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Reference of 99822-23-8, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 99822-23-8, 5-Fluorobenzo[d]isoxazol-3(2H)-one, introducing its new discovery.

NOVEL HETEROCYCLIC METHYLENE PIPERIDINE DERIVATIVES AND THEIR USE

The present invention is directed to compounds of formula (I) compositions comprising them and their use.

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

Electric Literature of 99822-23-8, Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 99822-23-8, Name is 5-Fluorobenzo[d]isoxazol-3(2H)-one. In a document type is Article,introducing its new discovery.

One Base for Two Shots: Metal-Free Substituent-Controlled Synthesis of Two Kinds of Oxadiazine Derivatives from Alkynylbenziodoxolones and Amidoximes

Different 1,2-migrations and cyclizations of a variety of alkynylbenziodoxolones (EBXs) and amidoximes under one-base conditions are described. This process provides an efficient protocol for the divergent synthesis of two oxadiazine derivatives via switchable selectivity of EBXs controlled by simply varying the substituents of the amidoximes, which feature transition metal-free conditions, simple execution, and high chemoselectivity.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Recommanded Product: 99822-23-8, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 99822-23-8, Name is 5-Fluorobenzo[d]isoxazol-3(2H)-one, molecular formula is C7H4FNO2

A novel bifunctional chelating agent based on bis(hydroxamamide) for 99mTc labeling of polypeptides

This paper describes the synthesis and biological evaluation of a novel bifunctional chelating agent (BCA) based on bis(hydroxamamide) for 99mTc labeling of polypeptides. We successfully designed and synthesized C3(BHam)2¡¤COOH as a new BCA. C 3(BHam)2¡¤COOH formed a stable 99mTc complex and enabled us to prepare 99mTc-labeled polypeptides by using a 2,3,5,6-tetrafluorophenol (TFP) active ester of C3(BHam) 2¡¤COOH. 99mTc-C3(BHam) 2¡¤HSA prepared with C3(BHam)2¡¤TFP was stable in both murine plasma and an excess of l-cysteine without any dissociation of 99mTc from polypeptides. Furthermore, the blood clearance of 99mTc-C3(BHam)2¡¤HSA in mice was similar to that of 125I-HSA, suggesting that C 3(BHam)2¡¤COOH retained stable binding between 99mTc and the polypeptides in vivo. When 99mTc-C 3(BHam)2¡¤NGA was injected into mice, the radioactivity showed high hepatic uptake early on and a rapid clearance from the liver, indicating that C3(BHam)2¡¤COOH did not affect the pharmacokinetics of polypeptides in vivo and gave radiometabolites, which displayed a rapid elimination from the liver. Such characteristics would render C3(BHam)2¡¤COOH attractive as a new BCA for 99mTc labeling of polypeptides. Copyright

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

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 99822-23-8, Name is 5-Fluorobenzo[d]isoxazol-3(2H)-one,introducing its new discovery., Application In Synthesis of 5-Fluorobenzo[d]isoxazol-3(2H)-one

A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists

Moderately potent, selective S1P1 receptor agonists identified from high-throughput screening have been adapted into lipophilic tails for a class of orally bioavailable amino acid-based S1P1 agonists represented by 7. Many of the new compounds are potent S1P1 agonists that select against the S1P2, S1P3, and S1P4 (although not S1P5) receptor subtypes. Analogues 18 and 24 are highly orally bioavailable and possess excellent pharmacokinetic profiles in the rat, dog, and rhesus monkey.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Computed Properties of C7H4FNO2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 99822-23-8, Name is 5-Fluorobenzo[d]isoxazol-3(2H)-one, molecular formula is C7H4FNO2

SUBSTITUTED 3-ARYL-5-ARYL-[1,2,4]-OXADIAZOLES AND ANALOGS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF

The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Related Products of 99822-23-8, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 99822-23-8, Name is 5-Fluorobenzo[d]isoxazol-3(2H)-one, molecular formula is C7H4FNO2. In a Patent£¬once mentioned of 99822-23-8

BICYCLOHETEROARYL-HETEROARYL-BENZOIC ACID COMPOUNDS AS RETINOIC ACID RECEPTOR BETA (RARbeta) AGONISTS

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as “BHBA compounds”), which, inter alia, are (selective) retinoic acid receptor beta (RARbeta) (e.g., RARbeta2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARbeta (e.g., RARbeta2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RARbeta (e.g., RARbeta2), that are ameliorated by the activation of RARbeta (e.g., RARbeta2), etc., including, e.g., neurological injuries such as spinal cord injuries.

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

Electric Literature of 99822-23-8, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 99822-23-8, 5-Fluorobenzo[d]isoxazol-3(2H)-one, introducing its new discovery.

CRYSTALLINE FORMS OF 4-(5-(4,7-DIMETHYLBENZOFURAN-2-YL)-1,2,4-OXADIAZOL-3-YL)BENZOIC ACID AND PROCESSES FOR THEIR PREPARATION

The present invention pertains generally to the field of therapeutic compounds, and more specifically to crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (referred to herein as “BHBA-001”), which, inter alia, is a (selective) retinoic acid receptor beta (RARbeta) (e.g., RARbeta2) agonist. The present invention also pertains to pharmaceutical compositions comprising such crystalline forms, and the use of such crystalline forms and compositions, both in vitro and in vivo, to (selectively) activate RARbeta (e.g., RARbeta2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RARbeta (e.g., RARbeta2), that are ameliorated by the activation of RARbeta (e.g., RARbeta2), etc., including, e.g., neurological injuries such as spinal cord injuries.

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