Abstract: Disclosed herein are novel compounds of formula II ##STR1## and pharmaceutically acceptable salts thereof, wherein: Q represents H, halo or --OSO.sub.2 R" wherein R" is CH.sub.3, CF.sub.3, phenyl or tolyl;R.sup.3a represents H, alkyl, allyl, cyclopropylmethyl or COOR.sup.14 wherein R.sup.14 is alkyl, aryl, aralkyl or haloalkyl;R.sup.4 represents H, halo, alkyl, haloalkyl or alkoxy;R.sup.5a represents --OR.sup.10, --N(R.sup.9).sub.2, --O--C(R.sup.7).sub.2 .multidot.OCOR.sup.13, or alkoxy; wherein each R.sup.9 independently represents H, alkyl, alkoxy, alkoxyalkyl, aralkyl or aryl;R.sup.10 represents H, --COR.sup.9 or --CON(R.sup.9).sub.2 ; andR.sup.13 represents alkyl, aralkyl or aryl,with the proviso that R.sup.3a can not be hydrogen or alkyl when Q is hydrogen, R.sup.4 is hydrogen, and R.sup.5a is hydroxy.Compounds of formula II are useful intermediates for producing compounds having valuable pharmaceutical properties in treating psychosis, depression, pain and hypertension.
Type:
Grant
Filed:
February 21, 1991
Date of Patent:
September 21, 1993
Assignee:
Schering Corporation
Inventors:
Joel G. Berger, Wei K. Chang, Marjorie Peters
Abstract: Compounds of the formula ##STR1## wherein R.sub.9, J, K, Z and Het are as set forth herein as described. The compounds of formula I are useful as agents in the treatment of fungal infections.
Type:
Grant
Filed:
August 20, 1991
Date of Patent:
August 17, 1993
Assignee:
Schering Corporation
Inventors:
Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
Abstract: Certain aryl substituted naphthalene, benzoxepine, benzazepine and henzocycloheptene derivatives are disclosed. The compounds are useful in treating hyperproliferative skin disease, allergic reactions and inflammation.
Type:
Grant
Filed:
October 15, 1991
Date of Patent:
July 6, 1993
Assignee:
Schering Corporation
Inventors:
Neng-Yang Shih, Pietro Mangiaracina, Michael J. Green, Ashit K. Ganguly
Abstract: Novel 2,2-disubstituted glycerol-like compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor ("PAF"). Also disclosed are methods of synthesizing and using the compounds of the invention as well as pharmaceutical compositions thereof. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification.
Type:
Grant
Filed:
September 6, 1991
Date of Patent:
February 9, 1993
Assignee:
Schering Corporation
Inventors:
Daniel Solomon, James J. Kaminski, Steven K. White, Laura S. Lehman de Gaeta, Ashit K. Ganguly
Abstract: An antibiotic complex is produced by the microorganism, Actinomadura brunnea NRRL 15216, ATCC 39216. A novel antibiotic 7-chloro-8-methoxy-2'-N-methyltetracycline, isolated from the antibiotic complex, is active against gram-positive and gram-negative aerobes.
Abstract: Heterobicyclic and heterocyclic intermediate compounds and their use in treating inflammation, hyperproliferative skin conditions such as psoriasis and allergy are disclosed.
Type:
Grant
Filed:
December 10, 1990
Date of Patent:
January 26, 1993
Assignee:
Schering Corporation
Inventors:
Pauline C. Ting, Margaret H. Sherlock, Wing C. Tom, James J. Kaminski
Abstract: A method and composition for reducing and/or controlling elevated intraocular pressure, especially the elevated intraocular pressure associated with glaucoma, are disclosed in which an angiotensin II antagonist is administered to the eye.
Abstract: The present invention relates to a process for preparing bicyclic compounds and intermediates thereof. The compounds are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents.
Type:
Grant
Filed:
October 8, 1991
Date of Patent:
January 19, 1993
Assignee:
Schering Corporation
Inventors:
Dinesh Gala, Martin Steinman, Ashit Ganguly
Abstract: A method of treating leukocyte dysfunction in a mammal, preferably a human, wherein said dysfunction is associated with pyhsical trauma, is disclosed. Preferably the method is used wherein the dysfunction is associated with thermal injury. The method comprises administering to the mammal an effective amount of GM-CSF to potentiate the function of the dysfunctional leukocytes.The use of GM-CSF for the manufacture of a medicament for use in treating a patient having such leukocyte dysfunction and a pharmaceutical composition comprising GM-CSF for use in such treating are also disclosed.
Abstract: Methods of constructing and using gene expression systems to indicate the pertubation of fungal cell envelopes are provided. The recombinant genes produce indicator cleavage enzymes such as .beta.-galactosidase when galactose is able to enter the cell, despite the presence of glucose, through discontinuous cell envelopes. The indicator cleavage enzymes such as .beta.-galactosidase cleaves a colorimetric indicator placed in the media to produce an easily detected measurement of altered cell envelope permeability.
Type:
Grant
Filed:
March 16, 1988
Date of Patent:
December 1, 1992
Assignee:
Schering Corporation
Inventors:
Michael J. Ryan, Jason A. Lotvin, Elizabeth B. Smith, Karen J. Shaw
Abstract: A method for dehalogenating a compound of the generalized structure ##STR1## is disclosed where: R.sub.1, R.sub.2 and R.sub.3 independently are hydrogen or methyl or R.sub.1 and R.sub.3 taken together represent methylene, with the proviso that R.sub.1, R.sub.2 and R.sub.3 are not all methyl;X is a halogen;m is zero, 1 or 2; andY is a pharmaceutically acceptable acid.The method comprises contacting compound I with a catalytic hydrogenolysis system to replace the halogen with a hydrogen. A particularly preferred hydrogenolysis system comprises Pd/C and ammonium formate.
Abstract: The present invention relates to a monoclonal antibody-and to the hybridoma that produces it-specific for a surface antigen of activated B cells and T cells transformed by the virus HTLV-I. The hybridoma has been deposited with the European Collection of Annimal Cell Cultures (ECACC) under the number 88062301.
Abstract: Heterocyclic N-oxide derivatives of substituted benzo[5,6]cycloheptapyridines, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.
Type:
Grant
Filed:
December 10, 1990
Date of Patent:
September 29, 1992
Assignee:
Schering Corporation
Inventors:
John J. Piwinski, Michael J. Green, Jesse Wong
Abstract: A method of extracting granulocyte/macrophage colony stimulating factor (GM-CSF) from GM-SCF-expressing bacterial cells comprising treating a suspension of GM-CSF-containing bacterial cells with an acid and an enhancing agent, or with an acid that is itself an enhancing agent, removing substantially all of the suspension liquid from the cells, preparing a second suspension of the acidified cells, neutralizing said second suspension, and separating the GM-CSF-containing liquid from the suspended cells.
Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treatment allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
Type:
Grant
Filed:
August 31, 1990
Date of Patent:
June 30, 1992
Assignee:
Schering Corporation
Inventors:
Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
Abstract: Expression systems which utilize bacteriophage T7 RNA mutant polymerases and promoter regions are provided by this invention. These systems are utilized to produce large quantities of useful polypeptides and proteins.
Type:
Grant
Filed:
October 19, 1989
Date of Patent:
June 16, 1992
Assignee:
Schering Corporation
Inventors:
Richard L. Reim, Satwant K. Narula, Michael J. Ryan, Paul J. Leibowitz
Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
Type:
Grant
Filed:
August 31, 1990
Date of Patent:
May 26, 1992
Assignee:
Schering Corporation
Inventors:
Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
Abstract: A fast dissolving buccal tablet for administering a medicament includes the active ingredient, a lubricant and a water soluble sugar, such as sorbitol, combined such that the buccal tablet dissolves in about one minute.
Abstract: This invention provides a crystalline form of recombinant human granulocyte-macrophage colony-stimulating factor (r-h-GM-CSF) and methods for making such crystals.
Type:
Grant
Filed:
June 6, 1989
Date of Patent:
April 28, 1992
Assignee:
Schering Corporation
Inventors:
Paul Reichert, Gerald S. Hammond, Hung V. Le, Tattanahalli L. Nagabhushan, Paul P. Trotta
Abstract: Compounds having an optionally-substituted purine derivative portion and a carbobicyclic or heterobicyclic portion, which compounds are useful as phosphodiesterase inhibitors, are disclosed. Also disclosed are intermediates, methods for making the inhibitors, pharmaceutical compositions and methods for treating hypertension using the compounds.