cas 288-14-2, Isoxazole | Articles data

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Pouchan et al.
p. 39,40,42,43
(1976)
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Development of safe and economical synthesis of isoxazole
Isoxazole is a five membered heterocyclic compound having various pharmacological actions. The new practical synthesis of isoxazole from the easily available malonadehyde tetraethyl acetal by avoiding the use of toxic reagent such as cadmium chloride under environment friendly conditions has been developed.
Nitlikar, Lakshmikant H.,Shinde, Devanand B.
p. 637 - 639
(2013/12/04)

Photocycloaddition of aromatic and aliphatic aldehydes to isoxazoles: Cycloaddition reactivity and stability studies
The first photocycloadditions of aromatic and aliphatic aldehydes to methylated isoxazoles are reported. The reactions lead solely to the exo-adducts with high regio- and diastereoselectivities. Ring methylation of the isoxazole substrates is crucial for high conversions and product stability. The 6-arylated bicyclic oxetanes 9a-9c were characterized by X-ray structure analyses and showed the highest thermal stabilities. All oxetanes formed from isoxazoles were highly acid-sensitive and also thermally unstable. Cleavage to the original substrates is dominant and the isoxazole derived oxetanes show type T photochromism.
Griesbeck, Axel G.,Franke, Marco,Neudoerfl, Joerg,Kotaka, Hidehiro
experimental part
p. 127 - 134
(2011/05/16)

Reactivity of neutral nitrogen donors in square-planar d8 metal complexes: The system chloro(2,2′:6′,2″-terpyridine)platinum(II) cation with five-membered N-donor heterocycles in methanol
The kinetics of the forward and reverse steps of the reaction [Pt(terpy)Cl]+ + nu ? [Pt(terpy)(nu)]2+ + Cl- (terpy = 2,2′:6′,2″-terpyridine, nu = one of a number of thiazoles, oxazole, isoxazole, imidazole, pyrazole and 3,5-dimethylpyrazole, covering a wide range of basicities) have been studied in methanol at 25 °C. Both forward and reverse reactions obey the usual two-term rate law observed in square-planar substitution. The second-order rate constants for the forward reactions, k2f, show a slight dependence upon the basicity of the entering nu, while the steric hindrance due to the presence of one methyl group in the α position to the nitrogen markedly decreases the reactivity. The second-order rate constants for the reverse reactions, k2r, are very sensitive to the nature of the leaving group and a plot of log k2r against the pKa of the conjugate acids of the unhindered five-membered N-donors is linear with a slope of -0.51. The results are compared with data from the literature regarding a series of pyridines reacting with the [Pt(terpy)Cl]+ cation under the same experimental conditions. Both in the forward and in the reverse reaction, the reactivity depends not only upon the ligand basicity but also upon the nature of the nucleophile in the order: (thiazoles, oxazole, isoxazole, imidazole, pyrazoles) > pyridines for the entry of N-donors and on the contrary for the displacement by Cl-. Steric retardation, due to the presence of a methyl group in the α position to the nitrogen, is remarkably lower for five-membered N-donors if compared to pyridines both in the forward and in the reverse reaction.
Pitteri, Bruno,Bortoluzzi, Marco
p. 2698 - 2704
(2008/10/09)

NOVEL FLORFENICOL-TYPE ANTIBIOTICS
The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals
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(2008/06/13)

Phosphate transport inhibitors
Disclosed are compounds which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1—W—X—Y—Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C1-C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function. The methods comprise the step of administering an effective amount of the one of the compounds described above.
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(2008/06/13)

Small-molecule inhibitors of interleukin-2
Compounds of formulae I and I′, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are antagonists of IL-2/IL-2R binding; and are useful for the treatment of interleukin-2 mediated diseases, such as autoimmune diseases (such as rheumatoid arthritis, multiple sclerosis, uveitis, and psoriasis), allograft rejection, and graft-versus-host disease.
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(2008/06/13)

Cocaine receptor binding ligands
The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.
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(2008/06/13)

Substituted N-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl) derivatives, their production and use as pharmaceutical agents
Substituted N-(1,4,5,6-tetrahydro-cyclopentapyrazol-3-yl) derivatives, their production, as well as intermediate products for their production, and the use as pharmaceutical agents for treating various diseases are described.
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(2008/06/13)

Heterocycle substituted purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: with Y, V, A, R1, R2, R3, R4, R7, and n1 defined herein.
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(2008/06/13)

Cocaine receptor binding ligands
The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.
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(2008/06/13)

Trisubstituted heterocyclic compounds and their use as fungicides
Compounds of general formula (I): in which:Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-Q1-T-Q2, -GZ and Y, such that the substituant -GZ is adjacent to both. the other substituants being as defined in the description,process for preparing these compounds,fungicidal compositions comprising these compounds,processes for treating plants by applying these compounds or compositions.
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(2008/06/13)

METHODS AND COMPOUNDS FOR INHIBITING MRP1
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(2008/06/13)

Benzamidine derivatives as factor XA inhibitors
Novel compounds of the formula I in which X, Y, R1, R2and R3are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
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(2008/06/13)

Cocaine receptor binding ligands
The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases or in determining the doses of therapeutic agents that occupy significant numbers of receptors.
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(2008/06/13)

Estrogen receptor modulators
Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
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(2008/06/13)

Substituted thiadiazolesulfonamides
Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1β participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).
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(2008/06/13)

Thienycyclohexanone derivatives as ligands of the GABAA α5 receptor subtype
A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.
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(2008/06/13)

Substituted thienobenzisoxazole derivatives for enhancing cognition
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: STR1 wherein A is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, arylC1-6 alkyl, aryl, S(O)p R1, OR1 or NR1 R12 ; B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR10 R11 ; R1 is hydrogen, optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl or C3-6 cycloalkenyl, optionally substituted aryl, arylC1-6 alkyl, arylC2-6 alkenyl or arylC2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring; R2 and R3 are hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl or CH2 (CO)m NR8 R9 ; R5 is NR6 R7, C1-6 alkyl or C1-6 alkoxy; R6 is independently as defined for R4 ; R7 is aryl optionally substituted by halogen, nitro or cyano; R8 is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, C2-6 alkenyl, C2-6 alkynyl; arylC1-6 alkyl, arylC2-6 alkenyl or arylC2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro or cyano; thiophene or pyridine; R9 is C1-6 alkyl; C2- alkenyl; C2-6 alkynyl; or phenyl optionally substituted by one, two or three substituents independently chosen from halogen, CF3, OCH3, nitro and cyano; R10 and R11 are individually hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C3-8 cycloalkyl or R10 and R11, together with the nitrogen atom to which they are attached, form a saturated 4 to 8 membered ring optionally containing an oxygen atom or a further nitrogen atom as a ring member, the further nitrogen atom being unsubstituted or substituted by C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl; R12 is hydrogen or C1-6 alkyl; m is zero or 1; p is zero, 1 or 2; q is 0, 1 or 2; and r is 0, 1 or 2; the preparation of these compounds, their use in enhancing cognition in disease states, particularly Alzheimer's disease, and methods of treatment using them.
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(2008/06/13)

Isoxazole compounds as cyclooxygenase inhibitors
A class of substituted isoxazolyl compounds is described for use in treating cyclooxygenase-2 related disorders. Compounds of particular interest are defined by Formula I STR1 wherein R1, R2, and R3, are described in the specification.
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(2008/06/13)

METHODS FOR CONTROLLING INVERTEBRATE PESTS USING COCAINE RECEPTOR BINDING LIGANDS
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(2008/06/13)

Combinatorial libraries of substrate-bound cyclic organic compounds
The invention relates to libraries of cyclic organic compounds and method of producing and assaying such libraries. According to the invention, each cyclic organic compound is constructed from a starting material in the form of a solid surface derivatized with a starting resin. Compounds are reacted with the resin to add or to form a cyclic group. The reactions are preferable carried out using a split resin procedure so that different compounds can be reacted with a plurality of subamounts so as to increase the size of the library. For example, compounds are reacted with a solid support bound starting resin to obtain a compound which includes an aldehyde functional group wherein the aldehyde compound or compounds reacted with it have substituents which are varied such that a mixture of products is obtained. The invention further relates to methods of producing combinatorial libraries of cyclic organic compounds from substrate bound compounds by cleaving the compounds from the support after synthesizing is completed and to assaying libraries of such compounds.
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(2008/06/13)

SUBSTITUTED 6- AND 7- AMINOTETRAHYDROISOQUINOLINECARBOXYLIC ACIDS
Compounds of the formula I STR1 are suitable for the preparation of pharmaceuticals for the prophylaxis and therapy of disorders involving increased activity of matrix-degrading metalloproteinases.
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(2008/06/13)

SUBSTITUTED ISOXAZOLES FOR THE TREATMENT OF INFLAMMATION
A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II wherein R1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof
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(2008/06/13)

Heteroaromatic compounds and crop protection agents containing them
Heteroaromatic compounds of the formulae IA and IB STR1 where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings: R1 alkyl, alkoxy, alkylamino R2 alkyl; A a direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereof B hydrogen, halogen, alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetaryl U CH2, CHCl, CHR2 or NOR2 ; X hydrogen, cyano, nitro, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof, amino which may bear one or two of the abovementioned groups; m 1 or 2, Y oxygen or sulfur; Z1 -Z2, Z3 -Z4, together with the carbon atom to which they are bonded, are the radical of a heteroaromatic, and fungicides containing these compounds.
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(2008/06/13)

3,5-disubstituted 2-isoxazolines and isoxazoles, agents containing them and their use
Novel 3,5-disubstituted 2-isoxazolines and isoxazoles and novel pharmaceuticals are described which are suitable, in particular, for the prophylaxis and/or treatment of pathological, neurodegenerative disorders in humans and animals. Processes for the preparation of these 3,5-disubstituted 2-isoxazolines and isoxazolines and isoxazoles are additionally indicated.
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(2008/06/13)

Substituted pyridine compounds having herbicidal activity
The present invention provides novel herbicidal pyridines characterized by having in the 3- or 5-position an aliphatic or aromatic 1-ketone.
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(2008/06/13)

4 Benzoyl isoxazole derivatives
4-Benzoyl isoxazole derivatives of the formula I: wherein:, R represents alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, optionally substituted cycloalkyl, -CO2R3,-COR5,cyano,nitro, -CONR31R4 or a halogen atom;, R1 represents :-, hydrogen , alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl or optionally substituted cycloalkyl, R2 represents :-, halogen, R5, -SR5, -SOR5, -SO2R5, -SO2NR31R4,-CO2R3, -COR5, -CONR31R4, -CSNR31R4, -OR5, a nitro group, a cyano group, a group -O(CH2)q-OR5 or alkyl substituted by OR5;, R3, R31 and R4, which may be the same or different, each represents:-, hydrogen, alkyl or haloalkyl;, R5 represents alkyl or haloalkyl;, n represents an integer from 1 to 5; and, q represents an integer from 1 to 3;, and agriculturally acceptable salts thereof and their use as herbicides is described.
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(2008/06/13)

Benzo-fused cyclic compounds
Herbicidal benzo-fused cyclic compounds of the formula STR1 wherein Q is STR2 Y is O or S, W is STR3 T is O, S, --NH-- or STR4 and R4 may represent, together with T, chlorine, Z is O or S, X is hydrogen or halogen, n is 0 or 1 and R is C3-6 cycloalkyl, an optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms, and salts thereof.
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(2008/06/13)

Herbicidal compounds
A compound of the formula in which, R1 represents an optionally substituted alkyl, alkenyl, alkynyl, aryl or aralkyl radical;, R2 represents a chlorine atom, a group of the formula, , O - or, a group of the formula O-R6 wherein R6 represents an optionally substituted heterocyclic ring of which at least the ring member bonded to the oxygen atom or one of the adjacent ring members is a hetero atom; and, one of R3 and R4 represents a hydrogen atom and the other represents an alkyl radical; The invention also provides processes for the preparation of compounds of formula I, herbicidal compositions containing them and their use as herbicides.
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(2008/06/13)

Antibacterial monic acid derivatives
A compound of the formula (I) STR1 wherein R is a group STR2 R1 is hydrogen, phenyl, C1-20 alkyl, C2-8 alkenyl or C2-8 alkynyl each of which may optionally be substituted; or C3-7 cycloalkyl, X is a divalent group --Y--C=C--, and Y is oxygen or sulphur, have antibacterial and/or antimycoplasmal activity.
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(2008/06/13)

Antiarthritic β-cycloalkyl-β-oxopropionitriles
Disclosed herein are novel β-cycloalkyl-β-oxopropionitriles which exhibit anti-inflammatory/antiarthritic activities.
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(2008/06/13)

Herbicidal thiophenesulfonamides
Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophenesulfonamide are useful as herbicides and plant growth regulants.
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(2008/06/13)

THE CHEMISTRY OF FULMINIC ACID REVISED
The availability of a new synthesis of fulminic acid by hydrolysis of trimethylsilanecarbonitrile oxide allowed a reinvestigation of the chemistry of the title compound.Thus, cycloadditions to olefinic and acetylenic dipolarophiles are improved with respect to previous results and the oligomerisation is proved to occur via the reactive species hydroxyiminoacetonitrile oxide 7 and hydroxyiminomethyl-hydroxyimino-acetonitrile oxide 8.The Z-configuration, found for the oxime groups in these intermediates, is maintained in their derivatives, under kinetic control.
Sarlo, Francesco De,Guarna, Antonio,Brandi, Alberto,Goti, Andrea
p. 5181 - 5186
(2007/10/02)

SIMPLE IN SITU PREPARATION OF FULMINIC ACID
Fulminic acid, generated in situ by hydrolysis of trimethylsilanecarbonitrile oxide, is employed in cycloaddition reactions.
Sarlo, Francesco De,Brandi, Alberto,Guarna, Antonio,Goti, Andrea,Corezzi, Silvia
p. 1815 - 1816
(2007/10/02)

Spiroketals useful as intermediates in the synthesis of milbemycin and avermectin macrolides
Milbemycin and avermectin macrolides are synthesized by the cyclized linking of separately synthesized northern and southern hemisphere intermediates. The northern hemisphere intermediate is a spiroketal alkenyl aldehyde, and the southern hemisphere intermediate is an aryl alkenyl phosphine oxide anion.
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(2008/06/13)

2-Cyanosteroids
The invention relates to novel 2-cyanosteroids of Formula I which are useful for the induction of menses and the termination of pregnancy.
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(2008/06/13)

Isoxazolylbenzamides as insecticides
The present invention is directed to isoxazolyl and benzisoxazolyl benzamide compounds useful as insecticides.
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(2008/06/13)

Process for the preparation of alkenoyl-substituted cyclohexenes
New heterocyclic derivatives containing nitrogen useful for perfumery and the flavour industry and use of same as perfuming and/or flavouring ingredients in the manufacture of perfumes and perfumed products and/or in the preparation of artificial flavours for foodstuffs, beverages, animal feeds, pharmaceutical preparations and tobacco products. Process for preparing the said heterocyclic derivatives which are equally useful as starting materials for preparing known fragrance compounds.
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(2008/06/13)

Process for the production of iron complexes of tetraazaannulenes
Process for the production of iron complexes of tetraazaannulenes starting from isoxazole, o-phenylene diamines and iron compounds. The process yields the iron complexes in good yields and a state of high catalytic activity for oxidation processes.
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(2008/06/13)

7-Oxa steroids
7-Oxa steroids which may be substituted in the 3-position with a hydroxy or oxo group or in the 2-position with a hydroxymethylene group or in the 2- and 3-positions with a substituent that forms a 5-membered heterocyclic ring, useful as antigonadotropic agents and a method of preparing these 7-oxa steroids from 3-hydroxy Δ5 -steroids including intermediates in this process.
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(2008/06/13)

Process for the preparation of damascenone derivatives
New alicyclic ketones useful for perfumery and flavor industry and process for preparing same. Use of said compounds as perfuming and/or flavoring, ingredients in the manufacture of perfumes and perfumed products and/or in the preparation of artificial flavors for foodstuffs, beverages, animal feeds, pharmaceutical preparations and tobacco products.
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(2008/06/13)