Abstract: 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:
Grant
Filed:
September 1, 1995
Date of Patent:
March 10, 1998
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
Abstract: 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:
Grant
Filed:
September 1, 1995
Date of Patent:
January 20, 1998
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
Abstract: 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:
Grant
Filed:
September 1, 1995
Date of Patent:
January 13, 1998
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
Abstract: 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:
Grant
Filed:
September 1, 1995
Date of Patent:
January 6, 1998
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
Abstract: 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:
Grant
Filed:
October 5, 1994
Date of Patent:
February 11, 1997
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, James H. Wikel, Michael R. Wiley
Abstract: 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:
Grant
Filed:
March 2, 1995
Date of Patent:
February 4, 1997
Assignee:
Eli Lilly and Company
Inventors:
Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
Abstract: 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:
Grant
Filed:
March 2, 1995
Date of Patent:
November 26, 1996
Assignee:
Eli Lilly and Company
Inventors:
Robert T. Shuman, Robert B. Rothenberger, Kenneth D. Kurz, Daniel J. Sall, Gerald F. Smith, Michael R. Wiley
Abstract: 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.
Abstract: 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.
Abstract: 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:
Grant
Filed:
October 5, 1994
Date of Patent:
January 16, 1996
Assignee:
Eli Lilly and Company
Inventors:
Daniel J. Sall, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
Abstract: 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:
Grant
Filed:
April 8, 1993
Date of Patent:
August 15, 1995
Assignee:
Zeneca Limited
Inventors:
Peter R. Bernstein, Philip D. Edwards, Andrew Shaw, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
Abstract: 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:
Grant
Filed:
March 4, 1994
Date of Patent:
July 25, 1995
Assignee:
Eli Lilly and Company
Inventors:
Kenneth J. Ruterbories, Robert T. Shuman
Abstract: 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:
Grant
Filed:
March 24, 1993
Date of Patent:
April 25, 1995
Assignee:
Imperial Chemical Industries plc
Inventors:
Alan W. Faull, Keith Russell, William J. Watkins
Abstract: 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.
Abstract: 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:
Grant
Filed:
October 20, 1992
Date of Patent:
August 23, 1994
Assignee:
Imperial Chemical Industries plc
Inventors:
Cyrus J. Ohnmacht, Robert J. Harris, Diane A. Trainor
Abstract: 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:
Grant
Filed:
November 25, 1992
Date of Patent:
August 16, 1994
Assignee:
Zeneca Inc.
Inventors:
Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
Abstract: 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:
Grant
Filed:
August 3, 1992
Date of Patent:
August 16, 1994
Assignee:
Imperial Chemical Industries PLC
Inventors:
Mitchell Glass, Joseph C. Williams, Ross L. Stein
Abstract: 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.
Abstract: The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Ra, Rb, A, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
Type:
Grant
Filed:
April 2, 1993
Date of Patent:
March 15, 1994
Assignee:
Imperial Chemical Industries PLC
Inventors:
Arnold H. Ratcliffe, Robert J. Pearce, Keith H. Gibson, Robin Wood, Brian B. Masek