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Pasquale N Confalone, 79303 Centennial Cir, Wilmington, DE 19807

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303 Centennial Cir, Wilmington, DE 19807    302-6612073   

303 Centennial Cir APT Q, Wilmington, DE 19807   

722 Hertford Rd, Wilmington, DE 19803    302-4272843   

Greenville, DE   

West Caldwell, NJ   

Brentwood, TN   

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Us Patents

Efficient Method For The Conversion Of Nitriles To Amidines

US Patent:
6399784, Jun 4, 2002
Filed:
Jan 10, 2001
Appl. No.:
09/757459
Inventors:
Philip Ma - Chadds Ford PA
Pasquale N. Confalone - Wilmington DE
Hui-Yin Li - Newark DE
Assignee:
Bristol-Myers Squibb Pharma Company - Princeton NJ
International Classification:
C07D26102
US Classification:
548240, 548247, 548131, 558375, 564163, 564244, 564246
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.

Synthesis Of 1,3,5-Trisubstituted Pyrazoles

US Patent:
6465656, Oct 15, 2002
Filed:
Dec 3, 2001
Appl. No.:
10/005938
Inventors:
Jiacheng Zhou - Hockessin DE
Lynette May Oh - West Chester PA
Pasquale N. Confalone - Greenville DE
Hui-Yin Li - Hockessin DE
Philip Ma - West Chester PA
Assignee:
Bristol-Myers Squibb Pharma Company - Princeton NJ
International Classification:
C07D26120
US Classification:
548241, 5413697
Abstract:
A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.

Efficient Ligand-Mediated Ullmann Coupling Of Anilines And Azoles

US Patent:
6541639, Apr 1, 2003
Filed:
Jul 25, 2001
Appl. No.:
09/912950
Inventors:
Jiacheng Zhou - Hockessin DE
Pasquale N. Confalone - Greenville DE
Hui-Yin Li - Hockessin DE
Philip Ma - West Chester PA
Lynette M. Oh - West Chester PA
Lucius T. Rossano - Landenberg PA
Charles G. Clark - Cherry Hill NJ
Chris Teleha - Bear DE
Assignee:
Bristol-Myers Squibb Pharma Company - Princeton NJ
International Classification:
C07D21102
US Classification:
546249, 546250, 5462741, 548255, 5482658, 5483435, 548563
Abstract:
The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.

Process For The Preparation Of Macrocyclic Metalloprotease Inhibitors

US Patent:
6562963, May 13, 2003
Filed:
Jul 31, 2001
Appl. No.:
09/919564
Inventors:
Roberta L. Dorow - Portage MI, 49024
Silvio Campagna - New Castle DE, 19720
Pasquale N. Confalone - Greenville DE, 19807
Fuqiang Jin - Wilmington DE, 19810
Zhe Wang - Hockessin DE, 19707
International Classification:
C07C23101
US Classification:
540456, 544168, 560169, 560172, 564135, 564136, 564139, 564143, 564153, 564158, 564159, 564205, 564207, 564208
Abstract:
The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R is selected from the group consisting of: C alkyl substituted with 0-5 R , â(CH ) âC cycloalkyl substituted with 0-5 R , and â(CH ) -aryl substituted with 0-5 R. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

Efficient Method For The Conversion Of Nitriles To Amidines

US Patent:
6610858, Aug 26, 2003
Filed:
Apr 25, 2002
Appl. No.:
10/132233
Inventors:
Philip Ma - West Chester PA
Pasquale N. Confalone - Wilmington DE
Hui-Yin Li - Hockessin DE
Assignee:
Bristol-Myers Squibb Pharma Company - Princeton NJ
International Classification:
C07D26102
US Classification:
548240, 548247
Abstract:
The present invention relates to processes for the conversion of nitriles 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.

Asymmetric Synthesis Of Amino-Pyrrolidinones

US Patent:
6770763, Aug 3, 2004
Filed:
Mar 14, 2003
Appl. No.:
10/389528
Inventors:
Nicholas A. Magnus - Indianapolis IN
Pasquale N. Confalone - Greenville DE
Scott A. Savage - Yardley PA
Matthew Yates - Lafayette IN
Robert E. Waltermir - Hillsborough NJ
David J. Meloni - Bear DE
Silvio Campagna - Candia NH
Assignee:
Bristol-Myers Squibb Company - Princeton NJ
International Classification:
C07D20704
US Classification:
548550, 548551, 502333, 5462484
Abstract:
A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described. These compounds are useful as intermediates for MMP and TACE inhibitors.

Synthesis Of 4,5-Dihydro-Pyrazolo [3,4-C] Pyrid-2-Ones

US Patent:
6919451, Jul 19, 2005
Filed:
Dec 3, 2002
Appl. No.:
10/308741
Inventors:
Jiacheng Zhou - Hackessin DE, US
Lynette M. Oh - West Chester PA, US
Philip Ma - West Chester PA, US
Hui-Yin Li - Hockessin DE, US
Pasquale Confalone - Greenville DE, US
Assignee:
Bristol-Myers Squibb Company - Princeton NJ
International Classification:
C07D471/04
US Classification:
544127, 544333, 544405, 546119, 546120
Abstract:
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.

Method For The Synthesis Of 2′,3′-Dideoxy-2′,3′-Didehydronucleosides

US Patent:
6927291, Aug 9, 2005
Filed:
Mar 1, 2002
Appl. No.:
10/087112
Inventors:
Fuqiang Jin - Wilmington DE, US
Pasquale N. Confalone - Greenville DE, US
Assignee:
Pharmasset, Ltd. - Tucker GA
International Classification:
C07D405/04
US Classification:
544317
Abstract:
An efficient synthetic route to antiviral 2′,3′-dideoxy-2′,3′-didehydro-nucleosides, such as 2′,3′-dideoxy and 2′- or 3′-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of β-D and β-L-2′,3′-dideoxy-2′,3′-didehydro-nucleosides is described that includes: activating a compound of structure (1) wherein B is a pyrimidine or purine base and Y is O, S or CHwith an acyl halide of the formula X—C(═O)R, X—C(═O)C(R)OC(═O)Ror X—C(═O)OR(wherein X is a halogen, and each Ris independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2′,3′-dideoxy-2′,3′-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2′-acyl-3′-halonucleoside, the 3′-acyl-2′-halonucleoside, or a mixture thereof.

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