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A novel glycerol derivative which is effective to reduce blood pressure has the formula: STR1 wherein R1 is an alkyl group having 10-22 carbon atoms, R2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (–(Q)l — is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R5, R6 and R7 is hydrogen, lower alkyl, aryl or aralkyl.

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Reference:
Thiazole | C3H4641NS – PubChem,
Thiazole | chemical compound | Britannica

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An efficient 1,5-cyclooctadiene-PdCl 2 /dicyclohexyl(2?,4?,6?-triisopropylbiphenyl-2-yl)phosphine (XPhos) catalytic system was developed for C-H allylation of polyfluoroarenes with allylic pivalates. The reactions showed excellent functional-group tolerance, good yields, and high regioselectivities. Mechanistic investigations supported a (pi-allyl)palladium complex pathway through a directed oxidative addition of the allylic pivalate to palladium, followed by sequential nucleophilic attack by the polyfluorobenzene and reductive elimination. In a gram-scale reaction, a palladium loading of 0.5 mol% was enough to afford the required product in good yield.

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Reference:
Thiazole | C3H4638NS – PubChem,
Thiazole | chemical compound | Britannica

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The anthraquinone moiety of dynemicin A was synthesized by Diels-Alder reaction between bromonaphthoquinone and a novel diene having the D ring and aromatization as key steps.

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Thiazole | C3H4634NS – PubChem,
Thiazole | chemical compound | Britannica

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The Pd-catalyzed cross-coupling of allylic carbonates and allylB(pin) is described. The regioselectivity of this reaction is sensitive to the bite angle of the ligand, with small-bite-angle ligands favoring the branched substitution product. This mode of regioselection is consistent with a reaction that operates by a 3,3? reductive elimination reaction. In the presence of appropriate chiral ligands, this reaction is rendered enantioselective and applies to both aromatic and aliphatic allylic carbonates.

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Reference:
Thiazole | C3H4631NS – PubChem,
Thiazole | chemical compound | Britannica

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Therapeutic preparations containing indazole derivatives

The invention concerns pharmaceutical compositions containing a 1,2-dihydro-3H-indazol-3-one derivative of the formula I STR1 wherein Ra is hydrogen, halogeno, nitro, hydroxy, (2-6C)alkanoyloxy, (1-6C)alkyl, (1-6C)alkoxy, fluoro-(1-4C)alkyl, (2-6C)alkanoyl, amino, (1-6C)alkylamino, di-[(1-4C)alkyl]amino, (2-6C)alkanoylamino or hydroxy-(1-6C)alkyl; Rb is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; and Y is a group of the formula –A1 –X–A2 –Q in which A1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene, or A1 is phenylene; X is oxy, thio, sulphinyl, sulphonyl, imino, (1-6C)alkylimino, (1-6C)alkanoylimino, iminocarbonyl or phenylene, or X is a direct link to A2 ; A2 is (1-6C)alkylene, (3-6C)alkenylene or (3-6C)alkynylene or A2 is cyclo(3-6C)alkylene or is a direct link to Q, or the group –A1 –X–A2 — is a direct link to Q; or Y is (2-10)alkyl, (3-10C)alkenyl or (3-6C)alkynyl; and Q is aryl or heteroaryl. The invention also provides novel 1,2-dihydro-3H-indazol-3-ones, processes for their production and the use of 1,2-dihydro-3H-indazol-3-ones for the manufacture of medicaments for the treatment of various allergic and inflammatory diseases.

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Reference:
Thiazole | C3H4632NS – PubChem,
Thiazole | chemical compound | Britannica

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This invention relates to piperazine derivatives of formula (I), wherein Y is bond or lower alkylene, R1 is aryl which may have substituent(s), R2 is aryl or indolyl, each of which may have substituent(s), R3 is hydrogen or lower alkyl, and R4 is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human beings or animals. 1

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Reference£º
Thiazole | C3H4629NS – PubChem,
Thiazole | chemical compound | Britannica

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Novel triazole compounds with a dioxane ring were synthesized. Condensation of the diol precursor 10 with various aromatic aldehydes 11 – 13 under acidic conditions afforded a series of dioxane-triazole compounds 14 – 16. The antifungal activities of the compounds 14 – 16 were evaluated in vivo in mice infection models against Candida and Aspergillus species. High activities were seen for the derivatives with one or two double bond(s) and an aromatic ring substituted with an electron-withdrawing group in the side chain. Among the derivatives, R-102557 (16R: Ar=4-(2,2,3,3- tetrafluoropropoxy)phenyl) showed excellent in vivo activities against Candida, Aspergillus and Cryptococcus species. It also showed high tolerance in a preliminary toxicity study in rats.

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Reference£º
Thiazole | C3H4635NS – PubChem,
Thiazole | chemical compound | Britannica

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3-Descladinosyl-6-O-carbamoyl and 6-O-carbonoyl macrolide antibacterial agents of the formula: 1wherein R1, W, R3, R4, R5, R6, X, X?, and Z are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

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Reference£º
Thiazole | C3H4644NS – PubChem,
Thiazole | chemical compound | Britannica

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The invention concerns a thiazole of the formula I, wherein Q? is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;, X is oxy, thio, sulphinyl, sulphonyl or imino;, Ar is phenylene which may optionally bear one or two substituents, or Ar is an optionally substituted 6-membered heterocyclene moiety contining up to three nitrogen atoms;, R? is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;, R? is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl or substituted (1-4C)alkyl or R? is optionally substituted benzoyl; and, Q? is optionally substituted thiazolyl;, or a pharmaceutically-acceptable salt thereof. The invention also concerns processes for the manufacture of a thiazole of the formula I and pharmaceutical compositions containing said thiazole.

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Thiazole | C3H4633NS – PubChem,
Thiazole | chemical compound | Britannica

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A series of 33 N-1 side chain-modified analogs of 1-[(2- hydroxyethoxy)methyl]-6-(phenylthio)thymine (1, HEPT) were synthesized and evaluated for their anti-HIV-1 activity. In particular, the influence of substitution of the terminal hydroxy group of the acyclic structure of HEPT and the structural rigidity of this side chain were investigated. Halo (7, 8), azido (9), and amino (10-15) derivatives were synthesized from HEPT via the p-tosylate derivative 6. Acylation of the primary amine 15 afforded the amido analogs 16-20. The diaryl derivatives 26-29 were prepared by reaction of HEPT, or of the 6-(2-pyridylthio) analog 23, with diaryl disulfides in the presence of tri-n-butylphosphine. Compounds 39-41, in which the N-1 side chain is rigidified by incorporation of an E-configured double bond, were obtained by palladium(0)-catalyzed coupling of several different 6- (arylthio)uracil derivatives (37, 38) with allyl acetates 33. Compounds 13, 40a,c,d,f, and 41, incorporating an aromatic ring at the end of the acyclic side chain, were found to be more potent than the known diphenyl-substituted HEPT analog BPT (2), two of them, 40c,d, being 10-fold more active.

A series of 33 N-1 side chain-modified analogs of 1-[(2- hydroxyethoxy)methyl]-6-(phenylthio)thymine (1, HEPT) were synthesized and evaluated for their anti-HIV-1 activity. In particular, the influence of substitution of the terminal hydroxy group of the acyclic structure of HEPT and the structural rigidity of this side chain were investigated. Halo (7, 8), azido (9), and amino (10-15) derivatives were synthesized from HEPT via the p-tosylate derivative 6. Acylation of the primary amine 15 afforded the amido analogs 16-20. The diaryl derivatives 26-29 were prepared by reaction of HEPT, or of the 6-(2-pyridylthio) analog 23, with diaryl disulfides in the presence of tri-n-butylphosphine. Compounds 39-41, in which the N-1 side chain is rigidified by incorporation of an E-configured double bond, were obtained by palladium(0)-catalyzed coupling of several different 6- (arylthio)uracil derivatives (37, 38) with allyl acetates 33. Compounds 13, 40a,c,d,f, and 41, incorporating an aromatic ring at the end of the acyclic side chain, were found to be more potent than the known diphenyl-substituted HEPT analog BPT (2), two of them, 40c,d, being 10-fold more active.

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Reference£º
Thiazole | C3H4639NS – PubChem,
Thiazole | chemical compound | Britannica