Patents Represented by Attorney, Agent or Law Firm Thomas E. Jackson
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Patent number: 5811402Abstract: This invention relates to a compound of the Formula IX--C(O)--Y--C(O)--NH--CH.sub.2 --G--Im I(wherein X, Y, G and Im have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.Type: GrantFiled: March 17, 1997Date of Patent: September 22, 1998Assignee: Eli Lilly and CompanyInventors: Valentine Joseph Klimkowski, Michael Robert Wiley
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Patent number: 5726159Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
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Patent number: 5710130Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 20, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5707966Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 13, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5705487Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5602101Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.Type: GrantFiled: October 5, 1994Date of Patent: February 11, 1997Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, James H. Wikel, Michael R. Wiley
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Patent number: 5599793Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: March 2, 1995Date of Patent: February 4, 1997Assignee: Eli Lilly and CompanyInventors: Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5578574Abstract: This invention relates to L-arginine aldehyde derivatives, having the formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: March 2, 1995Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: Robert T. Shuman, Robert B. Rothenberger, Kenneth D. Kurz, Daniel J. Sall, Gerald F. Smith, Michael R. Wiley
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Patent number: 5576333Abstract: The present invention concerns novel carboxamide derivatives of formula I, ##STR1## wherein R.sup.1, R.sup.2, J, m, and M have any of the values defined in the specification, which antagonize the pharmacological actions of one of the endogenous neuropeptide tachykinins at the neurokinin 2 (NK2) receptor, making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the novel carboxamide derivatives for use in such treatment, methods for their use, and processes and intermediates for the manufacture of the novel carboxamide derivatives.Type: GrantFiled: November 3, 1993Date of Patent: November 19, 1996Assignee: Zeneca LimitedInventor: Scott C. Miller
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Patent number: 5488037Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.Type: GrantFiled: March 4, 1994Date of Patent: January 30, 1996Assignee: Eli Lilly and CompanyInventors: Daniel J. Sall, Robert T. Shuman
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Patent number: 5484772Abstract: This invention relates to L-arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.Type: GrantFiled: October 5, 1994Date of Patent: January 16, 1996Assignee: Eli Lilly and CompanyInventors: Daniel J. Sall, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
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Patent number: 5441960Abstract: The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates ##STR2## useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones and methods for their use.Type: GrantFiled: April 8, 1993Date of Patent: August 15, 1995Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Philip D. Edwards, Andrew Shaw, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
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Patent number: 5439888Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 4, 1994Date of Patent: August 8, 1995Assignee: Eli Lilly and CompanyInventors: Robert T. Shuman, Gerald F. Smith
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Patent number: 5436229Abstract: This invention relates to bisulfite adducts of L-Arginine aldehyde derivatives, pharmaceutical formulations containing those adducts and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.Type: GrantFiled: March 4, 1994Date of Patent: July 25, 1995Assignee: Eli Lilly and CompanyInventors: Kenneth J. Ruterbories, Robert T. Shuman
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Patent number: 5410064Abstract: The invention concerns novel 1,3-dioxane alkenoic acid derivatives of the formula I ##STR1## wherein: n is the integer 1 or 2; Y is methyleneoxy, vinylene or ethylene;A.sup.1 is (1-6C)alkylene;R.sup.1 is a group of the formula R.sup.2.A.sup.2 -, in which:R.sup.2 is phenyl unsubstituted or bearing up to three substituents which are independently selected from (1-6C)alkyl, (1-6C)alkoxy, (2-6C)alkanoyl, (1-6C)alkylthio, (1-6C)alkylsulphonyl, halogeno, trifluoromethyl, nitro and cyano;A.sup.2 is a direct bond to R.sup.2 or a group of the formula --W--C(R.sup.4)(R.sup.5)-- wherein W is oxygen, methylene or a direct bond to R.sup.2, and R.sup.4 and R.sup.5 are independently (1-4C)alkyl;Q is a heterocyclyl group selected from thiazol-5-yl and imidazol-5-yl, the latter being unsubstituted or bearing a (1-12C)alkyl group at the 1-position of the imidazole ring; andR.sup.3 is hydroxy, a physiologically acceptable alcohol residue, or (1-4C)alkanesulphonamido;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 24, 1993Date of Patent: April 25, 1995Assignee: Imperial Chemical Industries plcInventors: Alan W. Faull, Keith Russell, William J. Watkins
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Patent number: 5352694Abstract: A physical form of (R)-3-methoxy-4-[1-methyl-5-(2-methyl-4,4,4-trifluorobutylcarbamoyl)indol -3-ylmethyl]-N-(2-methylphenylsulphonyl)benzamide substantially free of other physical forms, which form is crystalline and has an X-ray powder diffraction pattern with specific peaks at 2.theta.=14.0, 19.4, 22.0, 22.4 and 24.7.degree. , processes for preparing the form and pharmaceutical compositions containing it. The compound is a leukotriene antagonist useful in the treatment of diseases such as asthma.Type: GrantFiled: September 3, 1992Date of Patent: October 4, 1994Assignee: Imperial Chemical Industries PLCInventor: Murray W. Cuthbert
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Patent number: 5340819Abstract: Compounds of general formula I, ##STR1## and pharmaceutically acceptable salts thereof, in which R.sup.1 has any of the meanings given in the specification, pharmaceutical compositions comprising them and their use in the treatment of urinary incontinence.Type: GrantFiled: October 20, 1992Date of Patent: August 23, 1994Assignee: Imperial Chemical Industries plcInventors: Cyrus J. Ohnmacht, Robert J. Harris, Diane A. Trainor
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Patent number: 5338734Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: November 25, 1992Date of Patent: August 16, 1994Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5338727Abstract: There is provided a novel therapeutic agent for use in the prevention or treatment of adult respiratory distress syndrome and for use in the manufacture of a medicament for the prevention or treatment of adult respiratory distress syndrome, as well as a method of prevention or treatment of adult respiratory distress syndrome with the therapeutic agent and a method of treatment of cystic fibrosis with the therapeutic agent in combination with one or more other agents indicated for the treatment of adult respiratory distress syndrome.Type: GrantFiled: August 3, 1992Date of Patent: August 16, 1994Assignee: Imperial Chemical Industries PLCInventors: Mitchell Glass, Joseph C. Williams, Ross L. Stein
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Patent number: 5319097Abstract: The invention provides a pharmaceutical composition comprising a particular physical form of N-[4-[5-(cyclopentyloxy-carbonyl)amino-1-methylindol-3-yl-methyl]-3-methox ybenzoyl]-2-methylbenzenesulphonamide and polyvinylpyrrolidone. It also provides methods for preparing this physical form, and another physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyll-2-methylbenzenesulphonamide useful in the preparation of the first mentioned physical form. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example asthma.Type: GrantFiled: December 11, 1991Date of Patent: June 7, 1994Assignee: Imperial Chemical Industries PLCInventors: James J. Holohan, Ieuan J. Edwards