Abstract: A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3.
Abstract: Nucleic acid sequences, particularly DNA sequences, coding for all or a portion of human mevalonate kinase, expression vectors containing the DNA sequences, host cells containing the expression vectors, and methods for detecting the DNA sequences or the corresponding RNA sequences. The invention also concerns polypeptide molecules comprising all or a portion of human mevalonate kinase.
Type:
Grant
Filed:
February 6, 1990
Date of Patent:
September 20, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Richard D. Tanaka, Beverly S. Ricci, Stephen T. Mosley
Abstract: Nucleic acid sequences, particularly DNA sequences, coding for all or part of a trkC protein, expression vectors containing the DNA sequences, host cells containing the expression vectors, and methods utilizing these materials. The invention also concerns polypeptide molecules comprising all or part of a trkC protein and methods for producing these polypeptide molecules.
Abstract: Nucleic acid sequences, particularly DNA sequences, coding for all or part of a vav mouse proto-oncogene protein or for a modified vav mouse proto-oncogene protein, expression vectors containing the DNA sequences, host cells containing the expression vectors, and methods utilizing these materials. The invention also concerns polypeptide molecules comprising all or part of a vav mouse proto-oncogene protein or a modified vav mouse proto-oncogene protein, and methods for producing these polypeptide molecules.
Abstract: A method is provided for preparing 7-oxabicycloheptyl substituted heterocyclic aide prostaglandin analogs which are thromboxane A.sub.2 (TXA.sub.2) receptor antagonists or combined thromboxane A.sub.2 receptor antagonists/thromboxane synthetase inhibitors useful, for example, in the treatment of thrombotic and/or vasospastic disease, wherein a vinyl bromide of the formula, for example, ##STR1## wherein m, n, R.sup.1 and R.sup.2 are as defined herein is treated with a cyclizing agent to forth the corresponding oxazole.
Abstract: Cyclobutane intermediates wherein the absolute stereochemistry is (1S,2R) of the formula ##STR1## are disclosed. These intermediates are useful in the preparation of compounds having anti-viral activity.
Abstract: Microorganisms or reductases derived therefrom reduce a diketo ester ##STR1## to form the associated 3-hydroxy, 5-hydroxy, or 3,5-dihydroxy esters.
Type:
Grant
Filed:
May 15, 1992
Date of Patent:
June 28, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Ramesh N. Patel, Clyde G. McNamee, Amit Banerjee, Laszlo J. Szarka
Abstract: 10'-Desmethoxystreptonigrin, obtainable by cultivation of a strain of Streptomyces albus, A.T.C.C. No. 55161, and salts, esters and amides thereof. The novel compounds have antitumor and antibiotic activity.
Type:
Grant
Filed:
July 30, 1992
Date of Patent:
June 14, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Edward Meyers, Terrence W. Doyle, Veeraswamy Manne, Wen-Chih Liu
Abstract: Antibacterial activity has been found in compounds of the formula.Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: A is a bond or alkylene;Q completes a 5- or 6-membered saturated or unsaturated (including aromatic) heterocyclic ring having one or two, heteroatoms in the ring selected from nitrogen, ##STR2## sulfur or oxygen; X is attached to an available carbon atom in the heterocyclic ring and is hydrogen or oxo;Y is attached to an available carbon atom in the heterocyclic ring and is hydrogen, amino, hydroxyl, halogen, carboxamide, nitrile, or carboxyl, except that Y is not carboxyl when the bicyclic ring completed by Q is 2-quinolyl, 3-quinolyl, or quinoxalyl;and the remaining symbols are as defined in the specification.
Abstract: A method is provided for protecting against and/or treating ulcerative gastrointestinal conditions, including anti-inflammatory drug-induced gastrointestinal ulcers, using a thromboxane A.sub.2 receptor antagonist. In addition, a combination is provided which includes a thromboxane A.sub.2 receptor antagonist and an anti-inflammatory agent which combination may be used to treat inflammatory conditions, such as arthritis, while inhibiting formation of and/or treating gastrointestinal ulcers.
Type:
Grant
Filed:
December 23, 1992
Date of Patent:
May 17, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Bernard Rubin, Martin L. Ogletree, Eugene H. O'Keefe, A. K. Gunnar Aberg
Abstract: Novel compounds are disclosed having the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.
Abstract: The ostomy bag includes a multi-stage filter system that provides contamination protection for a deodorizing filter in the system. The multi-stage filter system also includes a gas transmissible protection filter that is impassible to semi-liquid waste material. The protection filter is located in the ostomy bag to precede the deodorizing filter such that gaseous waste must pass through the protection filter before it passes through the deodorizing filter. In one embodiment of the invention wherein the ostomy bag has a single chamber, the protection filter is a two layer structure with different pore counts that overlay the deodorizing filter. In another embodiment of the invention wherein the ostomy bag has dual chambers, the protection filter, without overlaying the deodorizing filter, is disposed across the flow path of gaseous waste to the deodorizing filter such that any gaseous waste that reaches the deodorizing filter must flow through the protection filter.
Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.
Abstract: A coupling for joining a pad or dressing to an ostomy bag including a first member 10 of closed loop form for defining a stoma aperture therein, the first member having a formation which defines two opposed walls, 11, 12, and a second member 20 of closed loop form also defining a stoma aperture. The second member has a projection or wall 21 dimensioned and positioned to fit between and resiliently bear against at least one of the walls when the members are connected in such a way as to make sealing engagement with at least the said one wall. The first member is of channel formation seen in cross section and has an upstanding tapering rib 24 extending from the base of the channel and between its walls. The second member has a tapering groove, of substantially complementary shape to the rib, in that surface of the rib projection or wall 21 which faces towards the first member in the mutually coupled condition of the first and second members.
Abstract: A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3 XII.
Abstract: A method is provided for preventing or reducing the risk of hypertension in normotensive patients having insulin resistance by administering a cholesterol lowering drug, such as pravastatin, alone or in combination with an ACE inhibitor, especially one containing a mercapto moiety, such as captopril or zofenopril.
Type:
Grant
Filed:
June 1, 1992
Date of Patent:
March 29, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Werner Tschollar, Cary S. Yonce, James L. Bergey, James C. Kawano
Abstract: A novel antibiotic substance, Scopularin, is prepared by cultivation of a strain of the microorganism, Scopulariopsis, A.T.C.C. No. 20,914. This compound and its alcohol derivative have also been found to have cytochrome P450 inhibition activity.
Type:
Grant
Filed:
January 31, 1989
Date of Patent:
March 15, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Donald R. Kirsch, Joseph O'Sullivan, Douglas W. Phillipson
Abstract: Imidazoles of the formula ##STR1## are prepared by treating a ketone ##STR2## with a nitrogenic acid, nitrite or nitrate in the presence of an acid to form a hydroxynitrile ##STR3## which is treated with R.sup.2 --CHO and an ammonium to form an N-hydroxyimidazole ##STR4## which is reduced in the presence of a buffer. In these compounds, R.sup.1 is hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, or --(CH.sub.2).sub.m Z(CH.sub.2).sub.n R.sup.3, each of which is optionally substituted with F or --CO.sub.2 R.sup.1 ; or aryl or aralkyl, each of which is optionally substituted with 1 or 2 groups selected from halogen, lower alkoxy, lower alkyl, or nitro;R.sup.3 is hydrogen, alkyl, cycloalkyl, lower alkenyl, or lower alkynyl;and the remaining symbols are as defined in the specification.
Abstract: 7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula ##STR1## wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or ##STR2## wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is ##STR3## then Y cannot be O, and when Z is --CH.dbd.CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO.sub.2 H, CO.sub.2 lower alkyl, CH.sub.2 OH, CO.sub.2 alkali metal, CONHSOR.sup.3, CONHR.sup.3a or --CH.sub.2 -5-tetrazolyl, X is O, S or NH; and where R.sup.1, R.sup.2, R.sup.3 and R.sup.3a are as defined herein.
Type:
Grant
Filed:
September 19, 1990
Date of Patent:
March 1, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Raj N. Misra, Philip M. Sher, Philip D. Stein, Steven E. Hall, David Floyd, Joel C. Barrish