Abstract: The present invention relates to human interleukin-3 (hIL-3) variant or mutant proteins (muteins) fused with other colony stimulating factors (CSF), cytokines, lymphokines, interleukins, hematopoietic growth factors or IL-3 variants.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 8, 2000
Assignee:
G. D. Searle & Company
Inventors:
S. Christopher Bauer, Mark Allen Abrams, Sarah Ruth Braford-Goldberg, Maire Helen Caparon, Alan M. Easton, Barbara Kure Klein, John P. McKearn, Peter O. Olins, Kumnan Paik, John W. Thomas
Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
Type:
Grant
Filed:
July 2, 1998
Date of Patent:
November 30, 1999
Assignee:
G.D. Searle and Company
Inventors:
Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
Abstract: Described herein is a retroviral protease inhibiting compound of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof.
Type:
Grant
Filed:
January 2, 1998
Date of Patent:
October 19, 1999
Assignee:
G. D. Searle & Company
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan R. Nagarajan, David L. Brown, Joseph J. McDonald
Abstract: DNAs which encode human LTC.sub.4 synthase and expression vectors comprising such DNAs are provided. DNAs encoding human LTC.sub.4 synthase may be used in assay methods of the invention for detecting LTC.sub.4 synthase inhibitors. Nucleic acid probes capable of identifying cDNAs and/or genomic DNAs encoding LTC4 synthase, as well as LTC.sub.4 antisense oligonucleotides and analogs which may be administered to viable cells to inhibit production of LTC.sub.4 synthase are also provided.
Type:
Grant
Filed:
June 3, 1994
Date of Patent:
September 14, 1999
Assignee:
G. D. Searle & Company
Inventors:
David Paul Creely, Scott David Hauser, Dean James Welsch, Gwen Grabowski Krivi
Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.
Abstract: The invention is a process for producing N-substituted glucamines, a process for oxidizing an N-substituted glucamine with an oxidizing microbe or extract thereof, and a process for oxidizing an N-substituted glucamine with an oxidizing microbe or extract thereof and reducing the oxidized N-substituted glucamine to an N-substituted-1-deoxynojirimycin. In addition, a one pot process for producing N-substituted-1-deoxynojirimycin from D-glucose is disclosed.
Type:
Grant
Filed:
December 27, 1996
Date of Patent:
June 29, 1999
Assignee:
G.D. Searle & Company
Inventors:
Roy Walter Grabner, Bryan Hayden Landis, Ping Tu Wang, Michael Lee Prunier, Mike G. Scaros
Abstract: There is disclosed a novel process for preparing products of the reaction of elemental phosphorus and elemental sulfur under reaction conditions wherein the phosphorus and sulfur are combined in a pre-mix at temperatures below the reaction temperature. The pre-mix may contain a diluent which is preferably the product of the reaction. Phosphorus pentasulfide can be prepared by heating the pre-mix to reaction temperatures wherein lower exotherm temperatures and reduced vibration are observed. Organophosphorus and thionated products can be prepared by the reaction of elemental sulfur and elemental phosphorus together with an organic compound wherein the ratio of phosphorus and sulfur generally corresponding to P.sub.2 S.sub.5. The process obviates the need for separately preparing phosphorus pentasulfide to prepare thiohated and organophosphorus compounds.
Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising a therapeutically-effective amount of the compounds or salts in combination with a pharmaceutically-acceptable carrier and methods for treating 5-lipoxygenase mediated conditions, inflammation-associated disorders and allergies.
Type:
Grant
Filed:
October 25, 1994
Date of Patent:
June 3, 1997
Assignee:
G. D. Searle & Company
Inventors:
Ish K. Khanna, Michael A. Stealey, Richard M. Weier
Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
Type:
Grant
Filed:
March 14, 1995
Date of Patent:
February 18, 1997
Assignee:
G. D. Searle & Company
Inventors:
Nizal S. Chandrakumar, Richard A. Mueller
Abstract: A composition is described for use in memory and learning enhancement or for treatment of a cognitive disorder or a psychotic disorder. This composition contains the compound D-cycloserine and D-alanine and provides reduced adverse side effects typically associated with chronic D-cycloserine use.
Abstract: A class of 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest, hypoglycemia or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein Y.sub.m is --CH.sub.2 -- or --CH.sub.2 --CH.sub.
Abstract: Compounds characterized generally as pyridinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a pyridinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
Abstract: Described is a new class of polypeptide cell modulators characterized by being composed of two covalently linked cell modulators in a linear polypeptide sequence. Such dual function polypeptides have new and particularly useful activities when the component polypeptide cell modulators are interferons, lymphokines or cytotoxins which act through different and specific cell receptors to initiate complementary biological activities.
Type:
Grant
Filed:
December 2, 1985
Date of Patent:
June 19, 1990
Assignee:
G. D. Searle and Company
Inventors:
Leslie D. Bell, Keith G. McCullagh, Alan G. Porter
Abstract: Compounds of formula I ##STR1## are described which are useful to inhibit the formation of serum cholesterol by virtue of their ability to inhibit .beta.-hydroxy-.beta.-methylglutaryl-CoA(HMG CoA), the rate-controlling substance in the synthesis of serum cholesterol.
Type:
Grant
Filed:
December 21, 1988
Date of Patent:
January 23, 1990
Assignee:
G. D. Searle & Company
Inventors:
John S. Baran, Thomas J. Lindberg, Harman S. Lowrie
Abstract: The present disclosure relates to an external analgesic solid stick composition for the topical administration of active analgesic agents. The compositions are dimensionally stable solid compositions comprising an external analgesic agent incorporated into a non-reactive hydrophobic wax matrix.
Abstract: The invention relates to compounds of the formula: ##STR1## which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies and inflammatory conditions.
Type:
Grant
Filed:
June 14, 1988
Date of Patent:
December 19, 1989
Assignee:
G. D. Searle and Company
Inventors:
Masateru Miyano, Robert L. Shone, Daniel D. Sohn
Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
Type:
Grant
Filed:
January 20, 1988
Date of Patent:
November 14, 1989
Assignee:
G. D. Searle and Company
Inventors:
Donald W. Hansen, Jr., Barnett S. Pitzele, Michael Clare, Robert W. Hamilton