Abstract: The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same and methods of using the same for treating viral infection or as an assay standard or reagent.
Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: ##STR1## or steroisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent, wherein:R.sup.1 is C.sub.1-3 alkyl substituted with 1-7 halogen;R.sup.2 is optionally substituted C.sub.1-5 alkyl, optionally substituted C.sub.2-5 alkenyl, or optionally substituted C.sub.2-5 alkynyl;R.sup.3, at each occurrence, is independently selected from C.sub.1-4 alkyl, OH, C.sub.1-4 alkoxy, F, Cl, Br, I, NR.sup.5 R.sup.5a, NO.sub.2, CN, C(O)R.sup.6, NHC(O)R.sup.7, and NHC(O)NR.sup.5 R.sup.5a ;R.sup.5 and R.sup.5a are independently selected from H and C.sub.1-3 alkyl;R.sup.6 is selected from H, OH, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and NR.sup.5 R.sup.5a ;R.sup.
Abstract: The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
October 2, 1998
Date of Patent:
May 2, 2000
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie, Jr.
Abstract: This invention relates to a method of prevention and/or treatment of thrombosis in a mammal without significantly altering bleeding time or coagulation. This invention further relates to methods of using selective inhibitors of the binding of vitronectin to the .alpha..sub.v .beta..sub.3 receptor, alone or in combination with other therapeutic agents, for the inhibition of thrombus formation and/or the treatment of thromboembolic disorders.
Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
Type:
Grant
Filed:
October 21, 1998
Date of Patent:
March 28, 2000
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
Abstract: This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.
Type:
Grant
Filed:
December 29, 1997
Date of Patent:
February 8, 2000
Assignee:
DuPont Pharmaceuticals Company
Inventors:
William Frank DeGrado, Shaker Ahmed Mousa, Michael Sworin, John Andrew Barrett, Scott David Edwards, Thomas David Harris, Milind Rajopadhye, Shuang Liu
Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
Type:
Grant
Filed:
June 18, 1998
Date of Patent:
December 7, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Robert A. Galemmo, Jr., Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
Abstract: The present invention describes indazoles of cyclic ureas of formula I: ##STR1## wherein X is a linker group and Y may be acyclic or cyclic, which are useful as inhibitors of HIV protease, and pharmaceutical compositions and diagnostic kits comprising the same.
Type:
Grant
Filed:
March 30, 1998
Date of Patent:
November 16, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
James D. Rodgers, Barry L. Johnson, Haisheng Wang
Abstract: A novel process for making compounds of Formula I, ##STR1## wherein X is a leaving group selected from the group Br, Cl, TsO, MsO, and TfO and R is a 1,2-diol, from a compound of Formula II: ##STR2## is described.
Abstract: A novel method of diagnosing or radioimaging breast tumors using .sup.99m Tc- or .sup.186/188 Re-tertiary-butyl isonitrile complex and a kit for diagnosing or radioimaging breast tumors containing tertiary-butyl isonitrile and a solubilization aid are presented.
Type:
Grant
Filed:
January 23, 1997
Date of Patent:
October 5, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Paul David Crane, David Charles Onthank, Milind Rajopadhye
Abstract: The present application describes m-amidino phenyl analogs of formula I: ##STR1## wherein D can be amidino and E can be phenyl, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
February 19, 1997
Date of Patent:
August 24, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Thomas Peter Maduskuie, Jr., Joseph Cacciola, John Matthew Fevig, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
Abstract: Processes for the preparation of R-.alpha.-propyl-piperonyl amine and its analogs, such compounds being useful intermediates in the preparation of elastase inhibitors, and intermediates useful for making R-.alpha.-propyl-piperonyl amine are described.
Type:
Grant
Filed:
March 21, 1997
Date of Patent:
August 3, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Hui-Yin Li, Luigi Anzalone, Robert Eugene Waltermire
Abstract: The present invention relates to compounds of formulae I and II: ##STR1## or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as inhibitors of HIV protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Type:
Grant
Filed:
November 7, 1997
Date of Patent:
August 3, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
James David Rodgers, Robert Frank Kaltenbach, III
Abstract: The present application describes N-(amidinophenyl)cyclourea analogs of formula I: ##STR1## which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
April 16, 1997
Date of Patent:
July 20, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Thomas Peter Maduskuie, Jr., Robert Anthony Galemmo, Jr., Celia Dominguez, Mimi Lifen Quan, Karen Anita Rossi, Petrus Fredericus Wilhelmus Stouten, Jung-Hui Sun, Brian Lloyd Wells
Abstract: The present invention describes novel radiopharmaceuticals of formula (I): ##STR1## wherein J, K, L, and M, are amino acids or derivatives thereof and R', R.sup.1, R.sup.2 and n are as defined herein, that are radiolabeled cyclic compounds containing chelators which act as antagonists of the platelet glycoprotein IIb/IIIa complex, methods of using the same as imaging agents for the diagnosis of arterial and venous thrombi, and novel reagents for the preparation of the same and kits comprising the reagents.
Abstract: A novel human corticotropin releasing hormone (CRH) receptor which is a splice variant of the human CRH.sub.2 receptor subfamily and is designated human CRHR2.gamma.. Fragments of CRHR2.gamma.. Nucleic acid molecules which encode CRHR2.gamma. and fragments, expression vectors comprising the nucleic acid molecules, and host cells containing the expression vectors. Antibodies and antibody fragments capable of binding the novel receptor. Nucleic acid molecules capable of hybridizing with the above nucleic acid molecules. Use of the novel receptor and receptor fragments, antibodies and antibody fragments in testing compounds for CRH antagonist activity and in treating diseases.
Type:
Grant
Filed:
May 21, 1997
Date of Patent:
March 30, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Brian Lee Largent, Ai-Ru Chen, Walter Alan Kostich, Karen Marie Sperle
Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
Type:
Grant
Filed:
August 18, 1997
Date of Patent:
March 23, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
Abstract: This invention relates to novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer, and to kits useful for their preparation. The radiopharmaceuticals of this invention are comprised of a transition metal radionuclide, a transition metal chelator, a biologically active group connected to said chelator, a first ancillary ligand, a second ancillary ligand capable of stabilizing the radiopharmaceutical, optionally having a linking group between said chelator and said biologically active group. Preferred radiopharmaceuticals of this invention have the formula:?(Q).sub.d' L.sub.n --C.sub.h' !.sub.x --M.sub.t (A.sub.L1).sub.y (A.sub.L2).sub.z,wherein the shown variables are as defined herein.
Abstract: This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.
Type:
Grant
Filed:
March 28, 1994
Date of Patent:
March 9, 1999
Assignee:
The Dupont Merck Pharmaceutical Company
Inventors:
William Frank DeGrado, Shaker Ahmed Mousa, Michael Sworin, John Andrew Barrett, Scott David Edwards, Thomas David Harris, Milind Rajopadhye, Shuang Liu
Abstract: The present invention relates to benzoxazinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
Type:
Grant
Filed:
October 1, 1997
Date of Patent:
February 23, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
David Donald Christ, Anthony Joseph Cocuzza, Soo Sung Ko, Jay Andrew Markwalder, Abdul Ezaz Mutlib, Rodney Lawrence Parsons, Jr., Mona Patel, Steven Paul Seitz