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 Title: |
US5922697:
Compounds, compositions and methods for inhibiting the binding of proteins containing an SH2 domain to cognate phosphorylated proteins
[ Derwent Title ]
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| Country: |
US United States of America
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| Inventor: |
Lunney, Elizabeth A.; Ann Arbor, MI
Para, Kimberly S.; Ann Arbor, MI
Plummer, Mark S.; Dexter, MI
Prasad, Josyula V. N. V.; Ann Arbor, MI
Saltiel, Alan R.; Ann Arbor, MI
Sawyer, Tomi; Ann Arbor, MI
Shahripour, Aurash; Ann Arbor, MI
Singh, Juswinder; Malden, MA
Stankovic, Charles J.; Saline, MI
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| Assignee: |
Warner-Lambert Company, Morris Plains, NJ
other patents from WARNER-LAMBERT COMPANY (618615) (approx. 2,588)
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| Published / Filed: |
1999-07-13
/ 1998-03-31
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| Application Number: |
US1998000051038
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| IPC Code: |
Advanced:
A61K 31/66;
C07F 9/38;
C07F 9/40;
Core:
C07F 9/00;
more...
IPC-7:
A61K 31/66;
C07F 9/38;
C07F 9/40;
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| U.S. Class: |
Current:
514/119;
558/190;
562/015;
Original:
514/119;
568/190;
562/015;
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| Field of Search: |
558/190
562/015
514/119
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| Priority Number: |
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| Abstract: |
The present invention provides compounds that inhibit the binding of proteins containing an SH2 domain to cognate phosphorylated proteins. The invention also provides pharmaceutical compositions containing the compounds and methods of inhibiting the binding of proteins containing an SH2 domain to cognate phosphorylated proteins.
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| Attorney, Agent or Firm: |
Crissey, Todd M. ;
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| Primary / Asst. Examiners: |
Ramsuer, Robert W.;
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| INPADOC Legal Status: |
None
Family Legal Status Report
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| Parent Case: |
This application is a 371 of PCT/US96/15998, filed Oct. 2, 1996.
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| Designated Country: |
AL AM AZ BB BG BR BY CA CN CZ EE EP GE HU IL IS JP KE KG KR KZ LK LR LS LT LV MD MG MK MN MW MX NO NZ PL PT RO RU SD
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| Family: |
Show 4 known family members
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First Claim:
Show all 17 claims |
We claim:
1. A compound of the formula [Figure] wherein U and W are --C--; [Figure] x is [Figure] R11 is hydrogen, alkyl, --OH, substituted alkyl, or --NH2 ; R12 is hydrogen or alkyl;
- R13 is --(CH2)n CO2 H, alkyl, --(CH2)n --aryl, --(CH2)n -cycloalkyl, hydrogen, substituted cycloalkyl--(CH2)n --, substituted aryl--(CH2)n --, or substituted alkyl;
- R14 is independently --OPO3 Rc Rd, --CF2 PO3 Rc Rd, --CH2 PO3 Rc Rd, or --PO3 Rc Rd ;
- R15 and R16 are independently hydrogen, alkyl, halogen, --OR, --NRR', --COCF3, --(CH2)n CH2 OH, --(CH2)n CO2 H, --(CH2)n NRR', --(CH2)n CHO, or --Q--CH2- (CH2)n --NRR';
- R18 is --(CH2)n CO2 R, hydrogen, alkyl, --(CH2)n CONRR', substituted alkyl, or --(CH2)n -substituted aryl;
- R19 is hydrogen, RCONR'--, RR'NCONR"--, RSO2 NR'--, RR'NSO2 NR"--, or ROCONR'--;
- R20 is hydrogen, alkyl, cycloalkyl--(CH2)n --, substituted alkyl, aryl--(CH2)n --, --(CH2)n --CO2 H, substituted cycloalkyl--(CH2)n --, or substituted aryl--(CH2)n --;
- Ra is hydrogen, halogen, or alkyl;
- Rb is hydrogen, alkyl, --OR, --O(CH2)n -aryl, --NRR', --O(CH2)n -substituted alkyl, --SR, --O(CH2)n -substituted aryl, or --O(CH2)n -cycloalkyl;
- Rc and Rd are independently --R, --CH2 CH2 Z, --CH2 CHZ2, or --CH2 CZ3,
- Q is --O--, --NH--, --S--, --CH2 O--, --CH2 NH--, or --CH2 S--;
- Z is --Cl, --Br, or --F;
- R, R', and R" are independently hydrogen, alkyl, cycloalkyl--(CH2)n --, aryl--(CH2)n --, --CH2 --(CH2)n --CO2 H, substituted cycloalkyl--(CH2)n --, substituted alkyl, or substituted aryl--(CH2)n --; and
- each n is independently 0 to 5 , or the pharmaceutically acceptable salts thereof.
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| Background / Summary: |
Show background / summary
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| Drawing Descriptions: |
Show drawing descriptions
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| Description: |
Show description
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| PCT Number: |
PCT/US96/15998
WO9712903
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| PCT Pub./Filed Dates: |
1997-04-10 / 1996-10-02
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| § 371 / 102(e) Dates: |
1998-03-31 / 1998-03-31
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| Forward References: |
Show 1 U.S. patent(s) that reference this one
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| Foreign References: |
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| Other Abstract Info: |
DERABS C1997-235567
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| Other References: |
Songyang, Z., et al, "SH2 Domains Recognize Specific Phosphopeptide Sequences" Cell, Mar. 12, 1993, vol. 72:767-778.
Bilder, G.E., et al., "PDGF-Receptor Protein Tyrosine Kinase Activity (R-PTKA) in Carotoid Artery in Enhanced by Injury and Inhibited In Vivo by Tyrphostin RG 13291" Supplement to Circulation, Abstracts from the 65th Scientific Sessions, New Orleans, LA on Nov. 16-19, 1992, vol. 86, No. 4, Oct. 1992, Abstract 0675.
Bilder, G.E., et al, "Tyrosine Kinase Inhibitor (TKI), RG13291 Prevents Association of β-PDGF Receptor (β-PDGF-R) with P13Kinase in Vascular Smooth Muscle Cells (VSCM)" Supplement to Circulation, Abstracts form the 65th Scientific Sessions, New Orleans, LA, on Nov. 16-19, 1992, vol. 86, No. 4, Oct. 1992, Abstract 1160.
Graber, M., et al., "The Protein Tyrosine Kinase Inhibitor Herbimycin A, but not Genistein, Specifically Inhibits Signal Transduction by the T-cell Antigen Receptor" International Immunology, Jun. 1992, vol. 4, No. 11, 1201-1210.
(10 pages)
[ISI abstract]
Cohen, D.I. et al., "Participation of Tyrosine Phosphorylation in the Cytopathic Effect of Human Immunodeficiency Virus-1" Science, Apr. 1992, vol. 256:542-545.
(4 pages)
Cited by 4 patents
[ISI abstract]
Beaulieu, A.D., et al., "Nuclear Signaling in Human Neutrophils" J of Bio Chem, Jan. 5, 1992, vol. 267, No. 1: 426-432.
(7 pages)
Cited by 2 patents
[ISI abstract]
Eiseman, E. & Bolen, J.B., "Engagement of the High-affinity IgE Receptor Activates scr Protein-related Tyrosine Kinases" Letters to Nature, Jan. 2, 1992, vol. 355:78-80.
(3 pages)
Cited by 17 patents
[ISI abstract]
Margolis, B., "Proteins with SH2 Domains: Transducers in the Tyrosine Kinase Signaling Pathway" Cell Growth & Differention, Jan. 1992, vol. 3:73-80.
(8 pages)
Cited by 6 patents
[ISI abstract]
Glenney, J.R., Jr., "Tyrosine-phoshorylated Proteins: Mediators of Signal transduction from the Tyrosine Kinases" 1992, Biochimica et Biophysica Acta, 1134:113-127.
(15 pages)
[ISI abstract]
Paolini, R., et al., "Phosphorylation and Dephosphorylation of the High-affinity Receptor for Immunoglobulin E Immediately after Receptor Engagement and Disengagement" Oct. 31, 1991, Nature, vol. 353:855-858.
(4 pages)
Cited by 3 patents
[ISI abstract]
McColl, S.R., et al., "Involvement of Tyrosine Kinases in the Activation of Human Peripheral Blood Neutrophils by Granulocyte-Macrophage Colony-Stimulating Factor" Oct. 1, 1991, Blood, vol. 78, No. 7:1842-1852.
(11 pages)
[ISI abstract]
Dvir, A., et al., "The Inhibition of EGF-dependent Proliferation of Keratinocytes by Tryphostin Tyrosine Kinase Blockers" May 1991, J of Cell Biology, vol. 113, No. 4:857-865.
(9 pages)
Cited by 18 patents
[ISI abstract]
Cooke, M.P., et al., "Regulation of T Cell Receptor Signaling by a src Family Protien-Tyrosine Kinase (p59fyn)" Apr. 19, 1991, Cell, vol. 65, 281-291.
(11 pages)
Cited by 13 patents
[ISI abstract]
Bilder, G.E., et al. "Tyrphostins Inhibits PDGF-induced DNA Synthesis and Associated Early Events in Smooth Muscle Cells" 1991, Am J Physiol, 260:C721-C730.
(10 pages)
Cited by 32 patents
[ISI abstract]
June, C.H., et al., "Inhibition of Tyrosine Phosphorylation Prevents T-cell Receptor -mediated Signal Transduction" Oct. 1990, Proc Natl Acad Sci USA, vol. 87:7722-7726.
(5 pages)
Cited by 16 patents
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