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 invention relates to processes for the conversion of nitrites to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.
Type:
Grant
Filed:
October 5, 1998
Date of Patent:
October 5, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Philip Ma, Pasquale N. Confalone, Hui-Yin Li
Abstract: The invention relates to a method of treating alcoholism and alcohol dependence in a mammal comprising administering to the mammal a therapeutically effective amount of a synergistic combination of: (i) at least one opioid antagonist, and (ii) at least one selective serotonin reuptake inhibitor. The invention also relates to compositions and kits containing the same.
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: This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents.
Type:
Grant
Filed:
November 19, 1996
Date of Patent:
August 3, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Douglas Guy Batt, Donald Joseph Phillip Pinto, Michael James Orwat, Joseph James Petraitis, William John Pitts
Abstract: The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
Type:
Grant
Filed:
April 11, 1997
Date of Patent:
August 3, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Michael Ernest Pierce, Anusuya Choudhury, Rodney Lawrence Parsons, Jr., Lilian Alicia Radesca
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 invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
Type:
Grant
Filed:
April 6, 1998
Date of Patent:
July 20, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Michael E. Pierce, Cheng Y. Chen, Anusuya Choudhury, Lilian A. Radesca, Lushi Tan, Dalian Zhao
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: Method for making 4-arylamino-1-alkyl-?1,2,3!triazolo?4,5-c!pyridines by base-promoted isomerization of 7-alkylamino-3-aryl-?1,2,3!triazolo?4,5-b!pyridines.
Type:
Grant
Filed:
March 19, 1998
Date of Patent:
June 15, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Jiacheng Zhou, Lynette M. Oh, Rajagopal Bakthavatchalam
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 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: 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: The present invention provides a process for the preparation of compounds of formula (V) below, and analogs thereof, which are useful as intermediates for the synthesis of HIV protease inhibitors, including cyclic ureas.
Abstract: This invention relates to novel substituted caprolactams, including 4-azacaprolactams, and derivatives thereof which inhibit HIV protease and are useful for treatment of HIV disease. Also included in this invention are pharmaceutical compositions containing such caprolactams, and to methods of using such caprolactams for the treatment of HIV disease.
Type:
Grant
Filed:
May 23, 1997
Date of Patent:
March 2, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Carl Nicholas Hodge, Christina Howard Fernandez, Prabhakar Kondaji Jadhav, Patrick Yuk-Sun Lam
Abstract: This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.
Type:
Grant
Filed:
December 31, 1996
Date of Patent:
March 2, 1999
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Prabhakar Kondaji Jadhav, George Clautice Emmett, Michael Ernest Pierce
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