Abstract: An improved process for preparing a compound of Formula (I): ##STR1## comprising: (a) treating a compound of Formula (Ia): ##STR2## with an alcohol comprising a compound of Formula (Ib-A) and an acid comprising a compound of Formula (Ib-B): ##STR3## wherein R.sub.a is selected from the group consisting essentially of hydrogen; (C.sub.1 -C.sub.6) alkyl; phenyl and (C.sub.1 -C.sub.3) alkyl-phenyl wherein said phenyl groups are optionally substituted by one or two substituents selected from the group consisting essentially of --(C.sub.1 -C.sub.4) alkyl; --O(C.sub.1 -C.sub.
Abstract: Calcium, magnesium, lidocaine and benzathine salts of 2-oxindole-1-carboxamides are useful for the treatment of joint disease by intra-articular administration.
Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein the broken line in formula I indicates a single or double bond, and wherein R, R.sub.1, X.sub.1 and X.sub.2 are as defined herein. The invention further relates to pharmaceutical compositions containing the compounds of formula I, and to methods of inhibiting phosphodiesterase type IV or the production of tumor necrosis factor in a mammal by administering the compounds of formula I to said mammal.
Abstract: This invention relates to a method of treating cancer by administering a compound of the formula wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E.sup.1, E.sup.2, p, Het' and Het" are defined as indicated in the specification.
Type:
Grant
Filed:
May 27, 1997
Date of Patent:
September 7, 1999
Assignee:
Pfizer Inc
Inventors:
Joseph P. Lyssikatos, Robert A. Volkmann
Abstract: A process for preparing a compound of formula (I) or a phamaceutically-acceptable salt thereof, comprising: 1) reacting a compound. of formula (III), in which R is a straight or branched chain alkyl having from one to four carbon atoms, with an alkali metal hydroxide in an aqueous medium at a temperature of about 80.degree. to 120.degree. C. and time of about 20 to 100 hours to form a reaction product; 2) cyclizing the reaction product of step 1) with formic acid and formaldehyde to form a formiate compound; and 3) neutralizing the formiate compound of step 2) with an aqueous base.
Abstract: Pharmaceutically active benzimidazole derivatives are disclosed comprising compounds of the formula: ##STR1## particularly wherein X is nitrogen, R.sup.1 is phenyl or heteroaryl, and one of R.sup.2 or R.sup.3 is hydroxy.
Type:
Grant
Filed:
January 31, 1997
Date of Patent:
March 30, 1999
Assignee:
Pfizer Inc.
Inventors:
William S. Faraci, Anton F. J. Fliri, Brian T. O'Neill, Mark A. Sanner, Stevin H. Zorn
Abstract: A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 or the like. Representative compounds are (3S,4R,5S,6S)-5-?3,5-bis(trifluoromethyl)-benzyloxy!-N,N-dimethyl-6-diphen ylmethyl-1-azabicyclo?2.2.2!octan-3-carboxamide, and -3-carboxylic acid.
Abstract: A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.
Type:
Grant
Filed:
January 26, 1996
Date of Patent:
December 8, 1998
Assignee:
Pfizer Inc
Inventors:
W. Stephen Faraci, Arthur A. Nagel, Robin W. Spencer, Fredric J. Vinick
Abstract: A process for preparing the chiral (4S)-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone is disclosed wherein racemic 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone is asymmetrically reduced by contacting the racemic tetralone with an asymmetric reagent to produce a mixture of cis and trans alcohols, separating the cis from the trans alcohols, and oxidizing the (4S) enantiomer of the resulting cis and trans alcohols. Also disclosed are novel intermediates used in the synthesis of the above chiral tetralone.
Abstract: Hydroxyalkylidene phosphonates, which give excellent inhibition of the formation, deposition and adherence of scale-forming salts, especially calcium carbonate, in aqueous systems, are degraded by the oxidizing biocides bromine and chlorine used to control microbial growth in such aqueous systems. It has been found that organic sulfonamides provide excellent protection against such degradation when they are added to the aqueous system along with the hydroxyalkylidene phosphonate scale inhibitors.
Abstract: Polyether polyamino methylene phosphonates, which possess high calcium tolerance and have been found to give excellent inhibition of the formation, deposition and adherence of scale-forming salts, especially calcium carbonate, in aqueous systems involving severe conditions which include elevated pH, high dissolved solids content, and high saturation levels of calcium carbonate, are degraded by the oxidizing biocides bromine and chlorine used to control microbial growth in such aqueous systems. It has been found that organic sulfonamides provide excellent protection against such degradation when they are added to the aqueous system along with the polyether polyamino methylene phosphonate scale inhibitors.
Abstract: Polyether polyamino methylene phosphonate N-oxides possess high calcium tolerance and have been found to give excellent inhibition of the formation, deposition and adherence of scale-forming salts, especially calcium carbonate, under severe conditions which include elevated pH, high dissolved solids content, and high saturation levels of calcium carbonate.
Abstract: A new antibiotic cyclic lipopeptide having the formula ##STR1## wherein R is H SEQ ID NO:1 or OH SEQ ID NO:2 and a method of producing is described. The agent has very high activity against human pathogens and is of very low mammalian toxicity.
Type:
Grant
Filed:
December 19, 1990
Date of Patent:
April 26, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Robert E. Schwartz, David F. Sesin, Prakash S. Masurekar, Jerrold M. Liesch, Thomas C. Hallada, Otto D. Hensens
Abstract: Polyether polyamino methylene phosphonates, when added to various industrial water systems in concentrations between 0.1 mg/L and 50 mg/L, stabilize soluble zinc, manganese and iron ions and their reaction products, in desirable forms and reduced particle sizes. In particular, this stabilization can be achieved under severe conditions which include elevated pH, high dissolved solids content, and high saturation levels of calcium carbonate.
Type:
Grant
Filed:
July 1, 1992
Date of Patent:
November 16, 1993
Assignee:
Calgon Corporation
Inventors:
Jasbir S. Gill, Charles J. Schell, Nancy S. Sherwood
Abstract: N,N-bis(phosphonomethyl)-2-amino-1-propanol, derivatives and corresponding lower alkyl ethers and N-oxides thereof possess high calcium tolerance and have been found to give excellent inhibition of the formation, deposition and adherence of scale-forming salts, especially calcium carbonate, under severe conditions which include elevated pH, high dissolved solids content, and high saturation levels of calcium carbonate.
Type:
Grant
Filed:
March 30, 1992
Date of Patent:
November 9, 1993
Assignee:
Calgon Corporation
Inventors:
Shih-Ruey T. Chen, Gary F. Matz, Raymond J. Schaper
Abstract: An anionic/cationic polymer mixture comprising:(a) a polyanion selected from polyacrylic acid, polymethacrylic acid, and polymaleic anhydride, each optionally copolymerized with each other, or optionally copolymerized with acrylamide up to a molar unit ratio of 1:1, provided that the total polyanionic weight average molecular weight is from about 1 to 5 thousand, and(b) the polycation poly(dimethyldiallylammonium chloride) having a weight average molecular weight of from about 25 thousand to 1 million,wherein the weight ratio of polyanion (a) to polycation (b) is from 1:2 to 1:8, has been found to give excellent inhibition of the formation, deposition and adherence of various alkali metal and alkaline earth metal scales, e.g., sodium sulfate, sodium carbonate, and calcium carbonate scales in the stringent conditions which characterize black liquor heaters, evaporators, etc.
Abstract: A method for flow injection analysis of total inorganic phosphate contained in an aqueous system such a cooling tower or boiler is described which uses a reducing agent and preservative composition therefore as the carrier for the sample to be analyzed, thereby creating a facile process which permits conversion of the various polyphosphates to orthophosphate and development of the molybdenum blue complex color reaction at 60.degree.-95.degree. C. and under 2-10 psi. This method has less stringent pressure and temperature requirements than those employed heretofore, thus permitting the use of more reliable and economic devices for measuring total inorganic phosphate in the field.
Abstract: A method for flow injection analysis of total inorganic phosphate contained in an aqueous system such as a cooling tower or boiler is described which uses a reducing agent and preservative composition therefore as the carrier for the sample to be analyzed, thereby creating a facile process which permits conversion of the various polyphosphates to orthophosphate and development of the molybdenum blue complex color reaction at 60.degree.-95.degree. C. and under 2-10 psi. This method has less stringent pressure and temperature requirements than those employed heretofore, thus permitting the use of more reliable and economic devices for measuring total inorganic phosphate in the field.