Abstract:
Compounds having formula (I), wherein W and W are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted naphthyl; R anb R are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R is selected from thienyl, furyl, phenyl, naphthyl, benzo[b]thienyl, alkyl, hydroxyl, and hydrogen; Y an alkylene of one to six carbon atoms; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) -OR , (c) -NR R , (d) -NR SO2R (e) -NH-Tetrazolyl, and (f) glycinyl; inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.
Abstract translation:具有式(I)的化合物,其中W 1和W 2独立地选自任选取代的喹啉基,任选取代的苯并噻唑基,任选取代的苯并恶唑基,任选取代的苯并咪唑基,任选取代的喹喔啉基,任选取代的萘基; R 1和R 2独立地选自氢,烷基,卤代烷基,烷氧基,卤素; R 3选自噻吩基,呋喃基,苯基,萘基,苯并[b]噻吩基,烷基,羟基和氢; Y为1至6个碳原子的亚烷基; 并且M选自(a)药学上可接受的代谢可裂解基团,(b)-OR 4,(c)-NR 5 R 6,(d)-NR 4 SO 2 R 7 e)-NH-四唑基,和(f)甘氨酰; 抑制白细胞三烯生物合成,可用于治疗过敏性和炎性疾病状态。 还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。
Abstract:
A prefilled, two-constituent system is provided with first and second containers or barrels. The first barrel includes a first chamber having a dispensing end or delivery end. The delivery end defines a dispensing passage or delivery passage communicating through the delivery end to accommodate the dispensing of fluid from the first chamber. A movable seal or reciprocable stopper is slidably disposed in the first chamber, and a first constituent is provided in the first chamber between the delivery end and the stopper. A second container or barrel is sized to be disposed in the first barrel and has a discharge end defining a discharge passage communicating through the discharge end to accommodate the discharge of fluid from the second barrel. A plunger is slidably disposed within the second barrel. A liquid second constituent is provided in the second barrel between the discharge end and the plunger. The first barrel stopper and the second barrel discharge end are engageable directly or indirectly to cooperatively define a coupling accommodating the flow of the liquid second constituent from the second barrel into the first chamber of the first barrel as the second barrel moves outwardly relative to the first chamber.
Abstract:
The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or Raman spectroscopy when directly attached to the support.
Abstract:
Antimicrobial compounds having formula (II), (III), (IV), (IV-A) or (V) as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compunds.
Abstract:
Provided are automated methods for distinguishing and differentiating cells in a whole blood sample. In one of the methods, a whole blood sample is provided. One or more tests to be performed on the whole blood sample is selected. The tests to be performed on the whole blood sample are correlated. A volume of the whole blood sample is aspirated into an automated instrument system which automatically performs conventional hematology analysis and fluorescent cytometry analysis on the whole blood sample. A first aliquot of the whole blood sample is dispensed into at least one sample receiving vessel. The first aliquot of the whole blood sample is mixed with a fluorescent reagent. The first aliquot of the whole blood sample mixed with fluorescent reagent is diluted and transported through a flow transducer system. The flow transducer system detects multi-angle light scatter and fluorescence from the first aliquot of the whole blood sample mixed with fluorescent reagent and counts and differentiates platelets or platelet clumps or both in the sample. Detecting and differentiation data for the one or more tests performed on the whole blood sample are stored. Results of the one or more tests performed on the whole blood sample are reported in a quantitative manner if so requested. The instrument system automatically performs all method steps without physically separating cells from the whole blood sample or an aliquot of the sample and results of a conventional hematology analysis may be utilized in at least reporting of results of the fluorescent cytometry testing.
Abstract:
Antimicrobial compounds having formula (I) wherein R and R are independently selected from the group consisting of hydrogen and C1-to-C4 alkanoyl; R and R are selected from the group consisting of (a) R is hydrogen and R is hydroxy, (b) R is hydroxy and R is hydrogen, (c) R and R taken together are =0; or selected from the group consisting of hydrogen and hydroxy; and R and R are independently selected from the group consisting of hydrogen, bromine and chlorine, with the proviso that at least one of R and R must be bromine. Also disclosed are pharmaceutical compositions comprising such compounds, methods of treating bacterial infection by the administration thereof and a process for preparing said compounds.
Abstract:
Novel macrocyclic 13-membered ring-contracted compounds derived from erythromycins A and B having formula (I) and pharmaceutically acceptable salts thereof, wherein R, R , R , R and X are specifically defined, having use in treating gastrointestinal disorders associated with hypermotilinemia, pharmaceutical compositions thereof, a method of treating gastrointestinal disorders associated with hypermotilinemia with said pharmaceutical compositions, and processes for the preparation thereof.
Abstract:
Antimicrobial compounds having formula (II), (III), (IV), (V), (VI), (VII), (VIII) and (IX) as well as the pharmaceutically acceptable salts, esters and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
Abstract:
A method is provided for preparing decapeptide and undecapeptide derivatives of LHRH by solution phase peptide chemistry as well as intermediate peptides useful in the same method.
Abstract:
A process of protecting a 1,2- or 1,3-aminoalcohol for reductive amination coupling is provided. The alcohol is protected with trimethylsilyl chloride. Trimethylsilyl protected norepinephrine derivatives useful in the preparation of arbutamine are also provided.