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Piperidine derivatives as subtype selective N-methyl-D-aspartate antagonists

Described are piperidines of Formula I 1 and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson”s disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Novel Compounds as Autotaxin Inhibitors and Pharmaceutical Compositions Comprising the Same

The present invention refers to a top gun [su [su] party [tu [tu] it buys as well as methods for treating and preventing auto [thak [thak] providence activation or increasing the concentration by inhibiting compound or novel therapeutic compositions and auto [thak [thak] new compositions containing number are disclosed. [Thak [thak] new inhibitors of the present invention to novel compounds are auto number, production generated by gun [su [su] party [tu [tu] it buys, cardiovascular diseases, cancer, metabolic disorders, kidney disease, liver disease, inflammatory diseases, nervous system diseases, respiratory disorder, fibrous diseases, ocular disorders, biliary the body characteristic which will cry chronic itch or acute or chronic organ transplant rejection reaction form and other forms of useful for the treatment or prevention. (by machine translation)

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Benzoxazole – Wikipedia,
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Synthesis of some novel benzoxazolinonylcarboxamides as potential anti-inflammatory agents

The synthesis of new 2(3H )-benzoxazolinonylcarboxamides starting from 2-amino-4,6-dimethylpyridine and 2(3H )-benzoxazolone which were designed as anti-inflammatory agents is described. These derivatives were synthesised from 2(3H )-(benzoxazolinon-6-yl)carboxylic acids, which were obtained by Friedel-Crafts acylation of 2(3H )-benzoxazolone derivatives with oxalyl chloride and acetylchloride in the presence of the AlCl3-DMF complex. The constitution of the products was supported by elemental analysis IR and 1H NMR spectral data.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Extracurricular laboratory:new discovery of 2-Oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acid

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54903-16-1, Name is 2-Oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acid, belongs to benzoxazole compound, is a common compound. Recommanded Product: 2-Oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acidIn an article, once mentioned the new application about 54903-16-1.

SMYD INHIBITORS

The present invention relates to sulfonamide carboxamides and having formula I, a pharmaceutically acceptable salt and solvates and efficacy. The invention also relates, SMYD protein, e.g., of formula I for treating disorders SMYD2 SMYD3 or isolation of reaction to the use of compounds are disclosed. The compounds of the invention particularly useful for treating cancer: [Formula I] In the formula, A, Y, B, X, and Z defined as described herein. (by machine translation)

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Benzoxazole – Wikipedia,
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Properties and Exciting Facts About 2-Oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acid

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NEW BENZOYL UREA DERIVATIVES

The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C1-C4 alkyl or C1-C4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and-CH= and/or-CH2-groups an optionally substituted 4-7 membered homo-or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo-or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo-or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo-or thioxo-oxazolidine, or 3-oxo-l,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C1-C 4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxy or optionally esterized carboxyl group, W is oxygen atom, as well as C1-C4 alkylene, C2-C4 alkenylene, aminocarbonyl,-NH-,-N(alkyl)-,-CH2O-,-CH 2S-,-CH(OH)-,-OCH2-group, wherein the meaning of alkyl is a C1-C4 alkyl group-, when the dotted bonds ( — ) represent simple C-C bonds then U is hydroxy group or hydrogen atom or when W is C1-C4 alkylene or C2-C4 alkenylene group, then one of the dotted bonds ( — ) can represent a further double C-C bond and in this case U means an electron pair, which participate in the double bond and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. Furthermore objects of the present invention are the pharmaceutical compositions containing new benzoyl urea derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions.

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NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME

The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson”s disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.

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Benzoxazole – Wikipedia,
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With dopamine D3 receptor that regulate the activity of the compound and use thereof (by machine translation)

The invention relates to a dopamine D3 receptor that regulate the activity of the compound and its use. In particular, dopamine receptor D3R can be used as a post-traumatic stress disorder syndrome (PTSD) and the new target, used for the prevention, treatment or auxiliary for the treatment of trauma/PTSD and anti-PTSD drug screening. On the other hand, the invention also relates to a dopamine receptor D3R that regulate the activity of the compounds in the preparation of the prevention, treatment and/or auxiliary treating PTSD use in the medicament. (by machine translation)

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Benzoxazole – Wikipedia,
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COMPOUNDS FOR MODULATING S1P1 ACTIVITY AND METHODS OF USING THE SAME

The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of S1P1 receptor and methods of using the same.

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Benzoxazole – Wikipedia,
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PIPERAZINE DERIVATIVE

A compound which specifically binds to a receptor of NR1/ NR2B, and is used as a NR2B receptor antagonist is provided.It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist.A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is -N(R4)-C(=O)-C(=O)-, -N(R4)-(CR5R6)p-C(=O)-, -N(R4)-C(-O)-(CR7R8)q- or -C(=O)-N(R4)-(CR7R8)q-, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.A compound which specifically binds to a receptor of NR1/ NR2B, and is used as a NR2B receptor antagonist is provided. It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein R 1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is -N(R 4 )-C(=O)-C(=O)-, -N(R 4 )-(CR 5 R 6 ) p -C(=O)-, -N(R 4 )-C(-O)-(CR 7 R 8 ) q – or -C(=O)-N(R 4 )-(CR 7 R 8 ) q -, p and q are each independently an integer of 1 to 3, R 4 , R 5 , R 6 , R 7 and R 8 are each independently a hydrogen atom or lower alkyl, A 1 is benzoxazolinone or the like, and A 2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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THIADIAZOLE MODULATORS OF PKB

The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating disease mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem