Abstract: Disclosed are chiral hydrazine derivatives of the formula (Ia), (Ib), (Ic) and (Id) ##STR1## wherein: R.sup.1 and R.sup.2 are independently C.sub.1 -C.sub.10 alkyl;R.sup.3 is H or R.sup.4 wherein R.sup.4 is a hydroxy protecting group; andZ is H, --CHO, --C(O)OC(CH.sub.3).sub.3 or --C(O)OCH.sub.2 C.sub.6 H.sub.5.Also described is a process for preparing chiral hydrazines of the formula (Ia), (Ib), (Ic) and (Id).
Abstract: An immunosuppressive drug, an autoimmune disease treating drug, an immunosuppression enhancing drug and a cell adhesion inhibitor, each containing a thienotriazolodiazepine compound wherein the 2-position of its diazepine ring is alkylated as an active ingredient, an immunosuppression method, an autoimmune disease treating method, an immunosuppression enhancing method and a cell adhesion inhibiting method, each of which comprising administering the compound, and uses of the compound for the production of an immunosuppressive drug, an autoimmune disease treating drug, an immunosuppression enhancing drug and a cell adhesion inhibitor.
Abstract: The present invention is directed to a method for preventing or reducing ischemia following injury, such as reperfusion injury following ischemia, cellular damage associated with ischemic episodes, such as infarctions or traumatic injuries, and thus to prevent or reduce the consequent progressive necrosis of tissue associated with such ischemia. This effect is achieved by administering DHEA, DHEA derivatives or DHEA congeners to a patient as soon as possible after the injury. The present invention is further directed to methods for preventing or reducing bacterial translocation or adult respiratory distress syndrome in a patient. Similarly, bacterial translocation and adult respiratory distress syndrome are prevented or reduced by administering DHEA, DHEA derivatives or DHEA congeners to a patient.
Abstract: The present invention relates to sulfonated diphosphines of the formula (I) ##STR1## where M is hydrogen, ammonium, a monovalent metal or the equivalent of a polyvalent metal, a, b, c and d are each 0 or 1, with the proviso that a+b+c+d is an integer from 1 to 4, Ar is an m-(MSO.sub.3)--C.sub.6 H.sub.4 radical and M is as defined above, n is 0, 1 or 2, Ph is a phenyl radical, R.sup.1 and R.sup.2 are identical or different and are each an alkyl radical having from 1 to 10 carbon atoms or a cycloaliphatic radical having from 5 to 10 carbon atoms in the ring, and a process for their preparation.
Type:
Grant
Filed:
February 21, 1996
Date of Patent:
November 4, 1997
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Christoph Naumann, Ahmed Tafesh, Dieter Regnat, Hans-Jerg Kleiner
Abstract: The synthesis of paclitaxel obtained from the semi-synthesis of taxol using a protected baccatin III backbone which is esterified with a suitably protected side chain acid, thereby producing an intermediate which may be acylated and deprotected to produce paclitaxel.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
November 4, 1997
Assignees:
NaPro BioTherapeutics, Inc., Bryn Mawr College
Inventors:
Nicholas J. Sisti, Charles S. Swindell, Madhavi C. Chander
Abstract: Sulphonates are prepared by the neutralization of a sulphonic acid with a basic hydroxide or Oxide. The process requires the staged addition of sulphonic acid to a reaction mixture comprising basic hydroxide or oxide dispersed in water/diluent mixture; the reaction mixture is basic throughout the additions of acid and at least until the point of completion of the neutralization reaction. The basic hydroxide or oxide may also be added in stages. The sulphonate product has low viscosity, low haze and good stability and is essentially chloride free as halide promoters are not utilized in the manufacture of the product.
Type:
Grant
Filed:
April 6, 1995
Date of Patent:
November 4, 1997
Assignee:
Exxon Chemical Patents Inc.
Inventors:
Kenneth Alcock, Jeremy Roger Spencer, Christopher John Adams
Abstract: The present invention relates to novel substituted amino compounds of the formula I:R.sup.1 -(A).sub.a -(B).sub.b -(D).sub.c -(CH.sub.2).sub.m -N(R.sup.2)-(CH.sub.2).sub.n -R.sup.3as defined in the present application, and to a process for preparing such compounds. The invention also includes pharmaceutical compositions containing the present compounds, and the preparation of such compositions. The invention also relates to the use of the present compounds as inhibitors of blood-platelet aggregation, formation of metastases by carcinoma cells, and the binding of osteoclasts to bone surfaces, in the treatment of hosts in need thereof.
Type:
Grant
Filed:
July 18, 1995
Date of Patent:
October 28, 1997
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Gerhard Zoller, Bernd Jablonka, Melitta Just, Otmar Klingler, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig
Abstract: Aminomethanephosphonic acid and aminomethylphosphinic acids are interesting as biologically active compounds or as intermediates for the preparation of biologically active compounds. According to the invention, such compounds of the formula I ##STR1## in which R.sup.1 is OH, C.sub.1 -C.sub.4 -alkyl or phenyl, can be prepared in a technically simple manner by reacting compounds of the formula II ##STR2## in which R.sup.2 is H, C.sub.1 -C.sub.6 -alkyl, benzyl, phenyl, optionally substituted by C.sub.1 -C.sub.4 -alkyl, -alkoxy and/or halogen, and R.sup.1 is as defined above, with water, at 80.degree. to 300.degree. C.
Abstract: Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 14, 1997
Assignee:
Schering Aktiengesellschaft
Inventors:
Johannes Platzek, Ulrich Niedballa, Peter Mareski, Bernd Raduchel, Hanns-Joachim Weinmann, Andreas Muhler, Bernd Misselwitz
Abstract: The invention relates to a process for the production of diethylenetriaminepentacarboxylic acid tetraesters of general formula I ##STR1## in which R.sup.1 and Z have different meanings.
Type:
Grant
Filed:
April 18, 1996
Date of Patent:
October 14, 1997
Assignee:
Schering Aktiengesellschaft
Inventors:
Johannes Platzek, Ulrich Niedballa, Bernd Radeuchel
Abstract: The invention is a process for production of C.sub.3 to C.sub.6 aldehydes by hydroformylating a mixture containing: (a) C.sub.2 to C.sub.5 olefins and mixtures thereof, and (b) (i) C.sub.2 to C.sub.5 alkynes and mixtures thereof or (ii) C.sub.3 to C.sub.5 cumulated dienes and mixtures thereof or (iii) mixtures of (i) and (ii), with CO, H.sub.2 and a solution of a rhodium complex catalyst produced by complexing Rh and an organophosphorus compound at a concentration of Rh in solution from 1 to 1000 ppm by weight. Alternatively, the solution of rhodium complex catalyst can have a P/Rh atom ratio of at least 30. Alternatively, the solution of rhodium complex catalyst can have a P/Rh atom ratio greater than the value R.sub.L defined by the formula: ##EQU1## in which R.sub.B is the P/Rh ratio sufficient for a catalytically active Rh complex, pKa.sub.TPP is the pKa value for triphenylphosphine, pKa.sub.L is the pKa value for the triorganophosphorus compound, R is the gas constant, and .DELTA.S.sub.
Type:
Grant
Filed:
December 15, 1995
Date of Patent:
October 7, 1997
Assignee:
Exxon Research & Engineering Company
Inventors:
Gabor Kiss, Frank Hershkowitz, Harry W. Deckman, Michael Gerard Matturro, Istvan T. Horvath, Anthony M. Dean, Raymond A. Cook
Abstract: Integrated process for the production of ter-amyl alkyl ethers which comprises the feeding of a C.sub.5 hydrocarbon stream to an etherification reactor and the recycling of the remaining stream to the same reactor, after treatment in an isomerization section to convert linear pentenes into reactive isoamylenes. An absorption section on molecular sieves is inserted between the etherification reactor and the isomerization section to eliminate inert hydrocarbons, basically i-pentane and n-pentane.
Type:
Grant
Filed:
October 23, 1995
Date of Patent:
September 30, 1997
Assignees:
Enichem S.p.A., Snamprogetti S.p.A.
Inventors:
Roberto Trotta, Gianni Donati, Renato Paludetto, Paolo Chiudaroli
Abstract: A process for base hydrolysis of a fluorinated sulphonyl fluoride by treatment of the fluoride with at least one mole equivalent of water in a basic solvent for a sufficient time to obtain a salt of a corresponding fluorinated sulphonic acid with the basic solvent and separating the obtained salt from the solution, wherein the basic solvent is selected from the group of tertiary amines.
Abstract: N-arylaminoacrylic acid derivatives are obtained in good yields and in high purities when benzoylacetic acid derivatives are reacted with N-arylimino ethers. The products thus prepared are used, in particular, for the preparation of 4-quinolone-3-carboxylic acid derivatives, which have an outstanding bactericidal action.
Type:
Grant
Filed:
August 31, 1995
Date of Patent:
September 30, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Gunter Rauchschwalbe, Bernhard Beitzke, Wolfgang Eymann, Helmut Fiege
Abstract: A process for preparing alkoxylated alkyl glyceryl ether sulfonates which comprises reacting in the presence of water and the absence of ethanol a mixture of alkoxylated glycidyl ethers having as the major quantity of alkoxylated material ##STR1## with a salt of a sulfite bisulfite salt mixture at a temperature below about 110.degree. C. wherein R is an alkyl or alkenyl of 10 to 20 carbon atoms, inclusive, R' is hydrogen or methyl and n has an average value of 1 to 10 and obtaining a sulfonated alkoxylated product having as a major quantity of the alkoxylated material a salt ofR(OCH.sub.2 CHR.sup.1).sub.n OCH.sub.2 CHOHCH.sub.2 SO.sub.
Abstract: The present invention comprises a novel composition of matter having the general formula: ##STR1## wherein R.sub.1 is H or an alkoxide of from 5 to about 20 carbon atoms;x is an integer of from about 8 to 22 when R.sub.1 =H and from about 2 to 5 when R.sub.1 is an alkoxide;R.sub.2 is selected independently from H, (CH.sub.2 CH.sub.2 O).sub.m H, and (CH.sub.2 CH(CH.sub.3)O).sub.m H;R.sub.3 is selected independently from H, (CH.sub.2 CH.sub.2 O).sub.n H, and (CH.sub.2 CH(CH.sub.3)O).sub.n H;m and n are integers from 1 to 50; and y and z are integers from 2 to 10.
Type:
Grant
Filed:
July 12, 1996
Date of Patent:
September 30, 1997
Assignee:
Exxon Research & Engineering Company
Inventors:
Ramesh Varadaraj, Max Leo Robbins, Cornelius Hendrick Brons
Abstract: A method for preparing diphenol compounds, which method includes the steps of coupling a hydroxyphenyl carboxylic acid with a L-tyrosine ester in a water-miscible organic reaction solvent containing a carbodiimide capable of forming a water-soluble urea by-product, thereby forming a diphenol reaction product; and combining the reaction mixture with an amount of water effective to precipitate the diphenol as a water-immiscible organic phase, so that a water-immiscible organic phase is formed containing the diphenol reaction product. New diphenol monomers and polymers polymerized therefrom are also disclosed.
Type:
Grant
Filed:
March 29, 1996
Date of Patent:
September 23, 1997
Assignee:
Rutgers, The State University
Inventors:
Joachim B. Kohn, Stephen J. Brocchini, Arthur L. Schwartz
Abstract: Novel naphthyl-substituted .alpha.-amino acid derivatives, pharmaceutical compositions containing the same and a method of using the same, for the blockade of aspartate and glutamate receptors, are described. Novel intermediates of the napthyl-substituted .alpha.-amino acid derivatives are disclosed.
Type:
Grant
Filed:
September 15, 1995
Date of Patent:
September 16, 1997
Assignee:
Warner-Lambert Company
Inventors:
Christopher Franklin Bigge, James Jia-He Li
Abstract: Compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof inhibit matrix metalloproteinases and TNF.alpha. secretion and are useful in the treatment of inflammatory disease states. Also disclosed are matrix metalloproteinases and TNF.alpha. secretion inhibiting compositions and a method for inhibiting matrix metalloproteinases and TNF.alpha. secretion.
Type:
Grant
Filed:
November 14, 1995
Date of Patent:
September 9, 1997
Assignee:
Abbott Laboratories
Inventors:
Stephen W. Fesik, James B. Summers, Jr., Steven K. Davidsen, George S. Sheppard, Douglas H. Steinman, George M. Carrera, Jr., Alan Florjancic, James H. Holms