Xu A Lin

US Patent:

7273714, Sep 25, 2007

Filed:

Mar 9, 2006

Appl. No.:

11/373623

Inventors:

Ivan C. King - North Haven CT, US
Xu Lin - Branford CT, US

Assignee:

VION Pharmaceuticals, Inc. - New Haven CT

International Classification:

C12Q 1/48
G01N 33/53

US Classification:

435 15, 435 75

Abstract:

This invention provides a method to determine alkylguanyltransferase activity in a sample, comprising steps of placing the sample in an appropriate condition so that the AGT is functional; contacting the sample with an AGT Detector under conditions permitting the binding of AGT and AGTD to produce a signal; and measuring the signal, thereby determining the AGT activity in said sample. This invention provides different uses of this method.

US Patent:

7405317, Jul 29, 2008

Filed:

Sep 21, 2005

Appl. No.:

11/232252

Inventors:

Xu Lin - Branford CT, US
Ivan King - North Haven CT, US
Michael F. Belcourt - Wallingford CT, US
Terrence W. Doyle - Killingworth CT, US

Assignee:

Vion Pharmaceuticals Inc. - New Haven CT

International Classification:

C07F 9/22
C07C 313/04
C07C 313/06

US Classification:

558 61, 562 8, 558154, 558193, 558190

Abstract:

Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy.

US Patent:

8026395, Sep 27, 2011

Filed:

May 27, 2009

Appl. No.:

12/454997

Inventors:

Xu Lin - Branford CT, US
Ivan King - North Haven CT, US

Assignee:

Nanotherapeutics, Inc. - Alachua FL

International Classification:

C07C 303/00

US Classification:

564 81, 564 82

Abstract:

The present invention relates to simple, safe, high-yield methods of synthesizing VNP40101M, 1,2-bis(methylsulfonyl)-2-(2-chloroethyl)-2-(methylaminocarbonyl)hydrazine, an anti-neoplasia agent. One particularly preferred method uses methyl chloroformamide in a one-pot reaction at elevated temperatures to provide VNP40101M in high yield.

US Patent:

20020119955, Aug 29, 2002

Filed:

Oct 15, 2001

Appl. No.:

09/977659

Inventors:

Terrence Doyle - Killingworth CT, US
Srinivasa Karra - Hamden CT, US
Zujin Li - Orange CT, US
Xu Lin - Branford CT, US
John Mao - Guilford CT, US
Qi Qiao - Nutley NJ, US
Yang Xu - Cheshire CT, US

International Classification:

A61K031/675
C07F009/58

US Classification:

514/089000, 546/022000

Abstract:

The present invention relates to compounds according to the structure: Where R is H or CH; Ris phosphate which can be free acid or salt; Ris H, F, Cl, Br, I, OCH, OCF, CFor a C-Calkyl group; Ris H, F, Cl, Br, I, OCH, OCFor CF; and Rand Rare each independently H, F, Cl, Br, I, OCH, OCFor CF, with the proviso that when any two of R, R, Ror Rare other than H, the other two of R, R, Ror Rare H which may be used to treat neoplasia, including cancer.

US Patent:

20040254103, Dec 16, 2004

Filed:

Jun 13, 2003

Appl. No.:

10/461282

Inventors:

Xu Lin - Branford CT, US
Terrence Doyle - Killingworth CT, US
Ivan King - North Haven CT, US

International Classification:

A61K038/17
A61K038/10
A61K038/08
A61K038/06
A61K038/04
C07K014/47
C07K007/08
C07K007/06
C07C311/60

US Classification:

514/012000, 514/013000, 514/014000, 514/015000, 514/016000, 514/017000, 514/018000, 514/019000, 530/324000, 530/325000, 530/326000, 530/327000, 530/328000, 530/329000, 530/330000, 530/331000, 514/590000, 562/824000, 564/035000

Abstract:

The present invention relates to compounds according to the structure (I): Where R is —CHor —CHCHCl; R′ is C-Calkyl or —CHCHCl; Ror Ris OPOH, NO, OCO(Glu-OH), NHCO(Glu-OH), NHRand unassigned groups of R, R, R, Rand Rare, independently, H, F, Cl, Br, I, OH, OPOH, OCH, CF, OCF, NO, CN, SOCH, SOCF, COCH, COOCH, SCH, SF, NH, NHR, N(CH), OPOH, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R, R, R, Ror Rare other than H, the other two of unassigned groups of R, R, R, Ror Rare H. Ris H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

US Patent:

20050043244, Feb 24, 2005

Filed:

Sep 27, 2004

Appl. No.:

10/950890

Inventors:

Xu Lin - Branford CT, US
Terrence Doyle - Killingworth CT, US
Ivan King - North Haven CT, US

Assignee:

VION PHARMACEUTICALS, INC. - New Haven CT

International Classification:

A61K038/16
A61K038/10
A61K038/08
A61K038/06
A61K038/05
A61K038/04
A61K031/277
A61K031/175
A61K031/195

US Classification:

514012000, 514013000, 514014000, 514015000, 514016000, 514017000, 514018000, 514019000, 514114000, 514524000, 514562000, 514590000

Abstract:

The present invention relates to compounds according to the structure (I): Where R is —CHor —CHCHCl; R′ is C-Calkyl or —CHCHCl; Ror Ris OP0H, N0, OCO(Glu-OH), NHCO(Glu-OH), NHRand unassigned groups of R, R, R, Rand Rare, independently, H, F, Cl, Br, I, OH, OP0H, OCH, CF, OCF, NO, CN, SOCH, SOCF, COCH, COOCH, SCH, SFs, NH, NHR, N(CH), OPOH, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R, R, R, Ror Rare other than H, the other two of unassigned groups of R, R, R, Ror Rare H. Ris H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

US Patent:

20080076132, Mar 27, 2008

Filed:

Sep 18, 2007

Appl. No.:

11/856909

Inventors:

Ivan King - North Haven CT, US
Xu Lin - Branford CT, US

International Classification:

C12Q 1/68
C07D 473/30
G01N 33/53
C07D 473/34

US Classification:

435006000, 435007100, 435007710, 544276000, 544277000

Abstract:

This invention provides a method to determine alkylguanyltransferase activity in a sample, comprising steps of placing the sample in an appropriate condition so that the AGT is functional; contacting the sample with an AGT Detector under conditions permitting the binding of AGT and AGTD to produce a signal; and measuring the signal, thereby determining the AGT activity in said sample. This invention provides different uses of this method.

US Patent:

20090075945, Mar 19, 2009

Filed:

Apr 2, 2008

Appl. No.:

12/080357

Inventors:

Xu Lin - Branford CT, US
Ivan King - North Haven CT, US
Michael F. Belcourt - Wallingford CT, US
Terrence W. Doyle - Killingworth CT, US

Assignee:

Vion Pharmaceuticals, Inc. - New Haven CT

International Classification:

A61K 31/662
A61P 35/00

US Classification:

514117

Abstract:

Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Methods of treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy.where R is C-Calkyl or haloalkyl;R′ and R″ are each independently C-Calkyl; andRis C-Calkyl,or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.