Patents Represented by Attorney John H. C. Blasdale
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Patent number: 5705611Abstract: Nucleic acids encoding the .beta.-chain of the human granulocyte-macrophage colony stimulating factor (GM-CSF) receptor, as well as the .beta.-chain itself, are provided. The .beta.-chain may be expressed with the .alpha.-chain in cellular hosts to form compositions useful in screening agonists and antagonists of human GM-CSF.Type: GrantFiled: January 7, 1993Date of Patent: January 6, 1998Assignee: Schering CorporationInventors: Kazuhiro Hayashida, Toshio Kitamura, Atsushi Miyajima
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Patent number: 5660711Abstract: A process is described for preparing 3-exomethylene cephalosporanic acid derivatives for use in the synthesis of cephalosporin antibiotics such as ceftibuten. The process comprises electrochemical reduction of a compound of the formula (IV) ##STR1## wherein: R.sup.3 is CH.sub.3 C(O)--; ##STR2## is an optional sulfoxide group; n is 2 or 3; R.sup.1 is H and R is H or NHR.sup.2, where R.sup.2 is H or a protecting group selected from C.sub.6 H.sub.5 CH.sub.2 OC(O)--, C.sub.6 H.sub.5 C(O)-- or C.sub.1 -C.sub.6 alkoxy-C(O)--; or wherein R and R.sup.1 together with the carbon atom to which they are attached comprise --C(O)--, and produces the desired 3-exomethylene compounds with low levels of the corresponding 3-methyl tautomers.Type: GrantFiled: December 8, 1995Date of Patent: August 26, 1997Assignee: Schering CorporationInventors: Derek Walker, Junning Lee, Charles R. Martin, Haiyan Zhang, Loris Sogli, Ermanno Bernasconi, Vinod Parakkal Menon
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Patent number: 5616777Abstract: 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).Type: GrantFiled: April 19, 1995Date of Patent: April 1, 1997Assignee: Schering CorporationInventors: David R. Andrews, Anantha Sudhakar
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Patent number: 5578616Abstract: The invention provides novel phenyl-alkyl-imidazoles of the formula ##STR1## wherein A, R.sup.1, R.sup.2, m and n are as defined in the specification, and the group --(CH.sub.2)n--A--R.sup.1 is at the 3- or 4-position, together with their pharmaceutically acceptable salts. These phenyl-alkyl-imidazoles and salts have valuable pharmacological properties, especially CNS activities and activity against inflammatory disease.Type: GrantFiled: June 6, 1995Date of Patent: November 26, 1996Assignee: Schering CorporationInventors: Robert G. Aslanian, Michael J. Green, Neng-Yang Shih
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Patent number: 5571910Abstract: A process is described for preparing 3-exomethylene cephalosporanic acid derivatives for use in the synthesis of cephalosporin antibiotics such as ceftibuten. The process comprises electrochemical reduction of a compound of the formula (IV) ##STR1## wherein: R.sup.3 is CH.sub.3 C(O)--; ##STR2## is an optional sulfoxide group; n is 2 or 3; R.sup.1 is H and R is H or NHR.sup.2, where R.sup.2 is H or a protecting group selected from C.sub.6 H.sub.5 CH.sub.2 OC(O)--, C.sub.6 H.sub.5 C(O)-- or C.sub.1 -C.sub.6 alkoxy--C(O)--; or wherein R and R.sup.1 together with the carbon atom to which they are attached comprise --C(O)--, and produces the desired 3-exomethylene compounds with low levels of the corresponding 3-methyl tautomers.Type: GrantFiled: May 26, 1995Date of Patent: November 5, 1996Assignee: Schering CorporationInventors: Derek Walker, Junning Lee, Charles R. Martin, Haiyan Zhang, Loris Sogli, Ermanno Bernasconi
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Patent number: 5561227Abstract: This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an azetidinone represented by the formula I ##STR1## from a carboxylic acid R.sup.2 --D--CH.sub.2 COOH, an aldehyde R.sup.1 --A--CHO and an amine RNH.sub.2, by the steps of: (a) converting a carboxylic acid to the corresponding acid chloride; (b) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a); (c) enolizing the product of step (b) and condensing with an imine; and (d) cyclizing the product of step (c). Steps (c) and (d) of this process are as shown in the following reaction scheme.Type: GrantFiled: June 23, 1994Date of Patent: October 1, 1996Assignee: Schering CorporationInventors: Tiruvettipuram K. Thiruvengadam, Chou-Hong Tann, Timothy L. McAllister
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Patent number: 5530125Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.Type: GrantFiled: August 19, 1994Date of Patent: June 25, 1996Assignee: Schering CorportionInventors: Joel G. Berger, Wei K. Chang, Joseph A. Kozlowski, Guowei Zhou
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Patent number: 5439916Abstract: 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: GrantFiled: August 31, 1990Date of Patent: August 8, 1995Assignee: Schering CorporationInventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Edmund J. Sybertz
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Patent number: 5241065Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.Type: GrantFiled: February 25, 1992Date of Patent: August 31, 1993Assignee: Schering CorporationInventors: Joel G. Berger, Wei K. Chang, Joseph A. Kozlowski, Guowei Zhou
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Patent number: 5126352Abstract: 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: GrantFiled: August 31, 1990Date of Patent: June 30, 1992Assignee: Schering CorporationInventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
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Patent number: 5116840Abstract: 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: GrantFiled: August 31, 1990Date of Patent: May 26, 1992Assignee: Schering CorporationInventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
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Patent number: 4948738Abstract: Monoclonal antibodies to .gamma.-interferon and hybridomas producing such antibodies are disclosed. The antibodies are preferably of the immunoglobulin subclass IgG.sub.1, .kappa., and do not bind to interferon-.alpha..sub.2.Type: GrantFiled: July 14, 1989Date of Patent: August 14, 1990Assignee: Laboratoires UNICETInventors: Jacques Banchereau, Odile Djossou, John Wijdenes, Helene Cabrillat, Catherine Favre