Abstract: Novel chiral 1,4-diol cyclic sulfates and their use as precursors in the preparation of chiral phospholane ligands, and chiral complexes useful as catalysts for carrying out enantioselective reactions.
Abstract: Process of making the compounds having the formula ##STR1## wherein --OR.sup.1 comprises the C-13 side-chain of taxol and R.sup.3 comprises hydrogen.
Type:
Grant
Filed:
April 6, 1995
Date of Patent:
January 14, 1997
Assignee:
Abbott Laboratories
Inventors:
Geewananda P. Gunawardana, Larry L. Klein, James B. McAlpine
Abstract: A process for the production of 2-cyanoiminothiazolidine by reaction of 2-aminoethanethiol (cysteamine) with a dialkyl-N-cyanoimidocarbonate.
Abstract: A method of production of an ether compound from an acetal compound or a ketal compound which is excellent in conversion and selectivity and does not cause corrosion of apparatuses and a novel useful polyvinyl ether compound as lubricating oil for compression-type refrigerators, electric insulation oil and the like are disclosed. The method of production of the present invention comprises reaction of an acetal compound or a ketal compound with hydrogen in the presence of a solid catalyst having acidic property and hydrogenation ability to produce the corresponding ether compound. The polyvinyl ether compound of the present invention comprises the constituting unit expressed by the general formula: ##STR1## (characters in the general formula are the same as those described in the specification), contains none of unsaturated bond, acetal structure and aldehyde structure in the molecule and has weight average molecular weight in the range of 300 to 3000.
Abstract: Preparation of chlorophenylphosphanes of the formula(C.sub.6 H.sub.5).sub.n PCl.sub.3-nin which n is 1 or 2, triphenylphosphane (C.sub.6 H.sub.5).sub.3 P and phosphorus trichloride PCl.sub.3 are reacted at temperatures above 300.degree. C., for which liquid triphenylphosphane and gaseous phosphorus trichloride are introduced in a molar ratio of 1:(3 to 12) at the upper end of a vertically arranged, elongated and heated reaction zone. The reaction product discharged at the lower end of the reation zone is transferred to a residence zone charged with phosphorus pentachloride. Finally, the excess phosphorus trichloride is removed from the reaction product, via a subsequent fractionating zone, by heating the residence zone with the resultant formation of a PCl.sub.3 -depleted reaction product. The substances contained in the PCl.sub.3 -depleted reaction product are separated from one another by fractionated rectification under reduced pressure.
Abstract: Detergent compositions comprising a surfactant system that is either (1) a mixture nonionic and zwitterionic detergent surfactants; (2) a mixture of nonionic and amphoteric (non-zwitterionic) detergent surfactants; or (3) short chain nonionic detergent surfactant, the nonionic detergent surfactants preferably being short chain and/or having peaked distribution; optional hydrophobic cleaning solvent; and polycarboxylate, especially dicarboxylate, detergent builder provide superior cleaning of all of the soils commonly found in the bathroom. The compositions have a pH of from about 1 to about 5.5, preferably from about 2 to about 4 when the dicarboxylate builder is used. The compositions are in the form of aqueous liquids. Short chain peaked distribution nonionic detergent surfactants provide surprisingly superior sudsing characteristics.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 10, 1996
Inventors:
Ricky A.-M. Woo, Michel J. Carrie, William A. Cilley, Ronald A. Masters, Daniel W. Michael, Eddy Vos
Abstract: Dyestuffs of the formula ##STR1## in which D is the radical of an aromatic or heterocyclic diazo component andK is the radical of an aromatic or heterocyclic coupling component, or is the radical of an active methylene compound,are obtained in an ecologically advantageous manner by reacting an aromatic or heterocyclic diazo components of the formulaD--NH.sub.2and a coupling component of the formulaH--Kwith a nitrite, for example NaNO.sub.2, in the presence of CO.sub.2 at a pressure of 5-100 at. The process is suitable in particular for the preparation of concentrated dye-stuff solutions, because expensive operations, such as, for example, pressure permeation and reverse osmosis, can be omitted.
Type:
Grant
Filed:
September 14, 1995
Date of Patent:
November 26, 1996
Assignee:
Bayer Aktiengesellschaft
Inventors:
Roderich Raue, Alfred Brack, Karl-Heinrich Lange
Abstract: Salts of the formulaF.sub.n.A,wherein F is an anion of a metal-free anionic dye having m acid groupswherein m is 1 to 4, inclusive,A is a cation of an amine containing 1 to 6 sterically hindered amine groups, andn is 1 or 2,with the proviso that the salt contains 1 to n.times.m groups selected from ammonium and immonium groups, useful as pigments, particularly for the coloring of solvent-free and solvent-containing plastic materials, lacquers and printing inks.
Abstract: The present invention comprises novel preparations of polyoxypropylene/polyoxyethylene copolymers which retain the therapeutic activity of the commercial preparations, but substantially reduce the undesirable effects which are inherent in the prior art preparations. Because the preparations of polyoxypropylene/polyoxyethylene copolymers which comprise the present invention are a less polydisperse population of molecules than the prior art polyoxypropylene/polyoxyethylene copolymers, the biological activity of the copolymers is better defined and more predictable and the cardiotoxicity inherent in the native copolymers is substantially reduced.
Type:
Grant
Filed:
August 9, 1994
Date of Patent:
October 22, 1996
Assignee:
CytRx Corporation
Inventors:
R. Martin Emanuele, Mannarsamy Balasubramanian, Hameedsulthan S. Allaudeen
Abstract: This invention relates to novel chiral 1,4-diol cyclic sulfates and their use as precursors in the preparation of chiral phospholane ligands, and chiral complexes useful as catalysts for carrying out enantioselective reactions.
Abstract: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.
Abstract: There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O).sub.n --, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.
Abstract: Chiral 1,4-diol cyclic sulfates and their use as precursors in the preparation of chiral phospholane ligands, and chiral complexes useful as catalysts for carrying out enantioselective reactions.
Abstract: This invention provides 7-deoxy-.DELTA..sup.6,7 -taxol and 7-deoxy-.DELTA..sup.6,7 -taxol analogs of Formula I: ##STR1## The compounds of Formula I are useful for the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, gastric cancer, colon cancer, head and neck cancer, and leukemia.
Type:
Grant
Filed:
June 10, 1994
Date of Patent:
September 17, 1996
Assignee:
The Upjohn Company
Inventors:
Robert C. Kelly, Roy A. Johnson, Harvey I. Skulnick, Eldon G. Nidy
Abstract: The present invention is directed to the use of an inhibitor of NO activity, such as a nitric oxide scavenger or an NO synthase inhibitor, as an antitumor therapy to reduce tumor blood flow and oxygenation. The invention is also directed to administration of a nitric oxide scavenger or a nitric oxide synthase inhibitor to enhance the effectiveness of tumor therapy with hypoxic or acidic chemotherapeutic agents or hyperthermia. The invention is also directed to the administration of a nitric oxide synthase substrate to a subject previously administered a nitric oxide synthase inhibitor, in order to selectively inhibit tumor perfusion. In a specific example, administration of cell free hemoglobin, a nitric oxide scavenger, in conjunction with mitomycin C, a hypoxic cytotoxin, results in a significant delay in tumor growth of a human tumor xenograft in a mouse compared to mitomycin C alone.
Type:
Grant
Filed:
May 20, 1994
Date of Patent:
September 10, 1996
Assignees:
Duke University, Apex Bioscience, Inc., North Carolina State University
Inventors:
Mark W. Dewhirst, Robert E. Meyer, Joseph Bonaventura, Joseph DeAngelo
Abstract: This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Type:
Grant
Filed:
February 14, 1994
Date of Patent:
September 3, 1996
Assignee:
Eli Lilly and Company
Inventors:
Robert D. Dillard, J. Scott Sawyer, Michael J. Sofia
Abstract: The invention relates to benzopyran leukotriene B.sub.4 (LTB.sub.4) antagonists and pharmaceutical compositions containing the compounds. The compounds inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders.
Type:
Grant
Filed:
September 30, 1994
Date of Patent:
August 27, 1996
Assignee:
Pfizer Inc.
Inventors:
Kevin Koch, Lawrence S. Melvin, Jr., Lawrence A. Reiter, Sally G. Ruggeri
Abstract: Disperse dyes of formula ##STR1## wherein D is the radical of a diazo component of formula ##STR2## Z.sub.1 is a radical of formula ##STR3## Z.sub.2 is hydrogen or a radical of formula (4), X is hydrogen, halogen, CF.sub.3, R.sub.3, OR.sub.3, NH--CO--R.sub.7, NH--CO--OR.sub.8, NH--SO.sub.2 --R.sub.7 or ##STR4## wherein R.sub.3 is C.sub.1 -C.sub.6 alkyl; R.sub.4 and R.sub.5 are each independently of the other hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy-C.sub.2 -C.sub.4 alkyl; R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl or phenyl; and R.sub.8 is C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.4 alkoxy-C.sub.2 -C.sub.4 alkyl; A.sub.1 is hydrogen, halogen, SO.sub.2 R.sub.3, CF.sub.3, NO.sub.2 or CN; A.sub.2 is hydrogen, halogen or CN; A.sub.3 is hydrogen or halogen, with the proviso that at least one of the substituents X, A.sub.1, A.sub.2 and A.sub.3 may not be hydrogen, and A.sub.4 is hydrogen, halogen, nitro, R.sub.3, NHCOR.sub.3 or OR.sub.3.
Abstract: A process for reducing the molecular weight of polytetramethylene ether glycol without significant conversion of polytetramethylene ether glycol to tetrahydrofuran monomer is disclosed. The process involves a two-step procedure. The first step comprises reacting polytetramethylene ether glycol with a perfluoroalkyl carboxylic acid to form a perfluoroalkyl ester of polytetramethylene ether glycol. That ester is, in the second step, converted back to polytetramethylene ether glycol of reduced molecular weight by hydrolysis or alcoholysis.