A method of treating lower respiratory tract disease by administration of an anti-infective agent and topical administration of an anti-inflammatory agent is provided. A device and method of treating lower respiratory tract disease by small particle aerosol administration of corticosteroids or anti-inflammatory drugs are also described.

A method for treating infectious respiratory diseases

Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.

Androgen receptor modulator compounds and methods

A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT1- like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Imidazole, triazole and tetrazole derivatives

Trypanothione reductase (TryR) is a genetically validated drug target in the parasite Trypanosoma brucei, the causative agent of human African trypanosomiasis Here we report the discovery, synthesis, and development of a novel series of TryR inhibitors based on a 3,4-dihydroquinazoline scaffold In addition, a high resolution crystal structure of TryR, alone and in complex with substrates and inhibitors from this series, is presented This represents the first report of a high resolution complex between a noncovalent ligand and this enzyme Structural studies revealed that upon ligand binding the enzyme undergoes a conformational change to create a new subpocket which is occupied by an aryl group on the ligand Therefore, the inhibitor, in effect, creates its own small binding pocket within the otherwise large, solvent exposed active site The TryR–ligand structure was subsequently used to guide the synthesis of inhibitors, including analogues that challenged the induced subpocket This resulted in the d

http://www.drugdiscovery.dundee.ac.uk/sites/www.drugdiscovery.dundee.ac.uk/files/Dihydroquinazolines%20as%20a%20novel%20class%20of%20trypanosoma%20brucei%202011.pdf

Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein Crystallography

4-Amino-1-(b-D-ribofuranosyl)quinazolin-2-one (3) was prepared by a direct glycosylation of 4-aminoquinazolin-2-one (7) using the Vorbruggen’s silylation method and provided exclusively the b-anomer. This quinazoline nucleoside and its 2� ,3� -O-isopropylidene derivative (9) did not undergo the coupling reaction with dialkyl disulfides in the presence of tri-n-butylphosphine unless their 4-amino groups were protected by N,N-dimethylaminomethylidene. This approach provides a viable alternative synthetic route to 5� -alkylthio-5� -deoxy nucleosides.

/pdf/nucleosides-xi-synthesis-and-antiviral-evaluation-of-5-3of9bjj6mr.pdf

Nucleosides XI. Synthesis and antiviral evaluation of 5'-alkylthio-5'-deoxy quinazolinone nucleoside derivatives as S-adenosyl-L-homocysteine analogs.

Synthetic Studies on Quinazoline Derivatives. II. : The Reactions of 2-Trichloro-and 2-Trifluoroacetamidobenzophenones with Primary Amines

2(1H)-Quinazolinone derivatives are prepared by reacting an indole-2-isocyanate derivative with an oxidizing agent, or by reacting an indole-2-isocyanate derivative with ozone to yield an ozone adduct thereof and converting said adduct. The obtained quinazolinone derivatives are useful as anti-inflammatory agent, or as intermediates for preparing other medicines.

Production of quinazolinone compounds

Verfahren zur Herstellung von Benzodiazepinderivaten

3,4-Dihydro-2(1H)-quinazolinone derivatives of the formula, ##STR1## wherein R 1 and R 2 signify individually a hydrogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a trifluoromethyl group, a lower alkylthio group, a lower alkylsulfonyl group or a halogen atom; R 3 signifies a phenyl group, a halophenyl group, a lower alkylphenyl group, a lower alkoxyphenyl group, a trifluoromethylphenyl group, a lower cycloalkyl group, a lower cycloalkenyl group, a pyridyl group, a pyrrolyl group, a furyl group, a thienyl group or a naphthyl group; R 4 signifies a lower alkyl group, a lower alkenyl group, an aralkyl group, a lower cycloalkylalkyl group, a lower cycloalkyl group, a lower alkoxyalkyl group, a lower alkylthioalkyl group, a lower hydroxyalkyl group, a lower alkanoyloxyalkyl group, a phenyl group, a halophenyl group, a trifluoromethylphenyl group, a lower alkylphenyl group a lower alkoxyphenyl group, a pyridyl group or a group of the formula ##STR2## wherein n signifies an integer of 1 to 4; and R 5 and R 6 signify individually a lower alkyl group, provided that they may form together with the adjacent nitorgen atom an optionally substituted 5- or 6-membered heterocyclic ring, which may further contain a hetero atom); and R signifies a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkoxyalkyl group, a lower alkylthioalkyl group, an aralkyl group, a lower cycloalkylalkyl group, a lower trihalomethylalkyl group or a group of the formula ##STR3## (wherein n, R 5 and R 6 signify the same as defined above), which have excellent pharmacological properties such as central nervous system depressant, anti-inflammatory, analgestic and anti-microbial activities, can be produced by reducing a compound of the formula, ##STR4## wherein R, R 1 , R 2 , R 3 and R 4 have the same meanings as defined above; and X 1 , X 2 and X 3 signify individually a halogen atom, or by the substitution reaction of the ring nitrogen atom of a 1 or 3-unsubstituted 3,4-dihydro-2(1H)-quinazolinone derivative.

Quinazolinone derivatives and a process for production thereof

A compound of the formula:
 wherein Y is a free or esterified carboxyl group, or a group of the formula:
 (wherein R a and R b are each independently a hydrogen atom, a C 1 -C 4 alkyl group, a C 3 -C 7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C 1 -C 4 alkyl group, or, when taken together with the adjacent nitrogen atom, they represent a 5 to 7 membered saturated heterocyclic goup); R' is a C 1 -C 12 alkyl group, a C 2 -C 12 alkenyl group, a C 2 -C 12 alkynyl group, a C 3 -C 10 cycloalkyl group, a C 4 -C 10 cycloalkenyl group, a hydroxy C 1 -C 13 alkyl group, an C 1 -C 12 alkyl group substituted with a group of the formula:
 (wherein R c and R d are each independently a hydrogen atom, or a C,-C 4 alkyl group), a C 3 -C 10 heterocyclic group, a phenyl group optionally substituted with one to three substituents selected from the group consisting of halogen atom, hydroxyl group, C 1 -C 4 alkyl group, trifluoromethyl group, C 1 -C 4 alkoxy group, and group of the formula:
 (wherein R c and R d are as defined above) or a group of the formula:
 [wherein A is a C 1 -C 7 alkylene chain and B is a C 3 -C 10 cycloalkyl group, a C 4 -C 10 cycloalkenyl group, a C 1 -C 12 alkoxy group, a C 1 -C 12 alkylthio group, a C 3 -C 10 cycloalkoxy group, a C 4 -C 10 cycloalkenyloxy group, a C 3 -C 10 heterocyclic group, or a phenyl or phenoxy group optionally substituted with one to three substituents selected from the group consisting of halogen atom, hydroxy group, C 1 -C 4 alkyl group, group of the formula:
 (wherein R c and R d are as defined above), trifluoromethyl group, C 1 -C 4 alkylthio group and C,-C 4 alkoxy group]; n is 2, 3 or 4; R 2 and R 3 are hydrogen atoms or, when taken together, they mean a single linkage to form a trans double bond between the adjacent carbon atoms, and E is a cis or trans vinylene group; provided that when n is 3 and R' is a n-octyl group, a 2-octenyl group or a 2,5-octadienyl group, R 2 and R 3 are hydrogen atoms, and that when n is 2, E is a trans vinylene group or a non-toxic pharmaceutically acceptable salt thereof. Said compound have potent anti-leucotriene B 4 action, and are useful in the treatment of inflammation and allergy.

Michihiro Yamamoto

Papers

Synthetic Studies on Quinazoline Derivatives. II. : The Reactions of 2-Trichloro-and 2-Trifluoroacetamidobenzophenones with Primary Amines

Production of quinazolinone compounds

Verfahren zur Herstellung von Benzodiazepinderivaten

Quinazolinone derivatives and a process for production thereof

Unsaturated fatty acid derivatives and their production