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IL-8 RECEPTOR ANTAGONISTS

Novel IL-8 receptor antagonists and methods of using them are provided.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Evaluation of Potent and Selective Small-Molecule Antagonists for the CXCR2 Chemokine Receptor

N,N?-Diarylureas were prepared, and the structure-activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active both in vitro against human neutrophils and in vivo in rabbit models of ear edema and neutropenia.

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Benzoxazole – Wikipedia,
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A new intramolecular migration of the imino group of O-arylketoximes to the aryl group under the Beckmann condition

ZrCl4-mediated decomposition of O-arylketoximes in benzene leads to regioselective intramolecular migration of the imino group from the oxygen to the ortho position of the aryl group via electron-deficient nitrogen intermediates.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Comparison of N,N?-diarylsquaramides and N,N?-diarylureas as antagonists of the CXCR2 chemokine receptor

N,N?-diarylsquaramides were prepared and evaluated as antagonists of CXCR2. The compounds were found to be potent and selective antagonists of CXCR2. Significant differences in SAR was observed relative to the previously described N,N?-diarylurea series. As was the case in the N,N?-diarylurea series, placing sulfonamide substituent adjacent to the acidic phenol significantly reduced the clearance in rat pharmacokinetic studies.

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Benzoxazole – Wikipedia,
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Diastereo- and enantioselective Pd(II)-catalyzed additions of 2-alkylazaarenes to N -boc imines and nitroalkenes

A chiral Pd(II)-bis(oxazoline) complex was found to be highly effective in promoting the first direct diastereo- and enantioselective addition of alkylazaarenes to N-Boc aldimines and nitroalkenes under mild conditions. Deprotection of Boc-protected products proceeded readily to provide amines in high yields.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Direct preparation of polyfunctional amino-substituted arylmagnesium reagents via an iodine-magnesium exchange reaction

The successive addition of PhMgCl and i-PrMgCl to functionalised iodoanilines allows their conversion to the corresponding amino-functionalised Grignard reagents, which react smoothly with a range of electrophiles in high yield.

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IL-8 RECEPTOR ANTAGONISTS

The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).

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Benzoxazole – Wikipedia,
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CONDENSED HETEROCYCLIC COMPOUND

A compound represented by the general formula (I) [R1 represents a C1-6 alkyl group, a halogen atom, or the like; A represents a phenylene group, or the like; X represents ?CH(R3)?, ?O?, ?NH?, or the like; Y represents ?O?, ?NH?, ?N?, or ?S?; . . . represents a single bond or double bond; n represents 1 to 3; R2 represents a C1-6 alkyl group, a C1-6 alkoxy group, or the like; and R3 represents hydrogen atom, a C1-6 alkyl group, or the like], or a salt thereof which has a blood LDL cholesterol-reducing action, and is useful as an active ingredient of medicaments.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Substituted hydroxy-anilino derivatives of cyclobutene-3,4-diones

The compound of the formula: STR1 wherein R1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, or polyfluoroalkyl; and one of R2, R3 and R4 is hydroxyl and the other two are, independently, H, CN, halogen, alkyl or hydroxyl; or a pharmaceutically acceptable salt thereof, is useful as a smooth muscle relaxant.

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Benzoxazole – Wikipedia,
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IL-8 RECEPTOR ANTAGONISTS

This invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease scates mediated by the chemokine, Interleukin-8 (IL-8). In particular, this invention relates to the novel compounds of Formula (Ia) and their use in treating chemokine mediated diseases wherein the chemokine binds to an IL-8 a or b receptor. Compounds of Formula (Ia) are represented by the structure: STR1 wherein interalia, X is oxygen or sulfur;

Rb is NR 6 R. sub.7, alkcyl, aryl, arylC 1-4 alkyl, aryl C 2-4 alkenyl, heteroaryl, heteroarylC 1-4 alkyl, heteroarylC 2-4 alkenyl, heterocyclic or heterocyclic C 1-4 alkyl, or a heterocyclic C 2-4 alkenyl moiety, camphor, all of which may be optionally substituted;< P>

R 1 is independently selected from hydrogen; halogen; nitro; cyano; C 1-10 alkyl; halosubstituted C 1-10 alkyl; C 2-10 alkoxy; halosubstituted C 1-10 alkoxy; azide; (CR. sub.8 R 8)q S(O) t R 4 ; hydroxy; hydroxy substituted C 1-4 alkyl; aryl; aryl C 1-4 alkyl; aryl C 2-10 alkenyl; aryloxy; aryl C 1-4 alkyloxy; heteroaryl; heteroarylalkyl; heteroaryl C 2-10 alkenyl; heteroaryl C 1-4 alkyloxy; heterocyclic; heterocyclic C 1-4 alkyl; heterocyclicC 1-4 alkyloxy; heterocyclic C 2-10 alkenyl; < P>

q is 0 or an integer having a value of 1 to 10; n is an integer having a value of 1 to 3;

m is an integer having a value of 1 to 3;

Y is hydrogen; halogen; nitro; cyano; halosubstituted C 1-10 alkyl; C 1-10 alkyl; C 2-10 alkenyl C. sub.1-10 alkoxy; halosubstituted C 1-10 alkoxy; azide; (CR 8 R. sub.8)qS(O) t R 4, (CR 8 R 8)qOR 4 ; hydorxy; hydroxy substituted C. sub.1-4 alkyl; aryl; aryl C 1-4 alkyl; aryloxy; arylC. sub.1-4 alkyloxy; aryl C 2-10 alkenyl; heteroaryl; heteroarylalkyl; heteroaryl C 1-4 alkyloxy; heteroaryl C 2-10 alkenyl; heterocyclic, heterocyclic C 1-4 alkyl; heterocyclicC 2-10 alkenyl;

or a pharmaceutically acceptable salt thereof.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem