| Patent Number |
Title Of Patent |
Date Issued |
| RE40525 |
Hepatitis C inhibitor tri-peptides |
September 30, 2008 |
| A racemate diastereoisomer and optical isomer of a compound of formula (I): ##STR00001## wherein B is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; |
| 7439258 |
Viral polymerase inhibitors |
October 21, 2008 |
| A compound of the formula I: ##STR00001## wherein: X is CH or N; Y is O or S; Z is OH, NH.sub.2, NMeR.sup.3, NHR.sup.3; OR.sup.3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substi |
| 7344723 |
Self-replicating RNA molecule from hepatitis C virus |
March 18, 2008 |
| A unique HCV RNA molecule is provided having an enhanced efficiency of establishing cell culture replication. Novel adaptive mutations have been identified within the HCV non-structural region that improves the efficiency of establishing persistently replicating HCV RNA in cell cultu |
| 7323567 |
RSV polymerase inhibitors |
January 29, 2008 |
| Compounds or enantiomers of formula (I) or a salt thereof: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein, are useful for the manufacture of a medicament for the treatment or prevention of respiratory syncytial virus infection in a mammal. |
| 7294457 |
Direct binding assay for identifying inhibitors of HCV polymerase |
November 13, 2007 |
| A method for identifying compounds binding to HCV polymerase comprising the steps of: contacting said HCV polymerase or an analog thereof with a probe formula I: ##STR00001## wherein A is O, S, N, NR.sup.1, or CR.sup.1, wherein R.sup.1 is defined herein; ----- represents either a si |
| 7276373 |
Surrogate cell-based system and method for assaying the activity of hepatitis C virus NS3 protea |
October 2, 2007 |
| The present invention concerns the development of a cell-based assay system having improved sensitivity to HCV NS3 protease activity when compared to known assays, which is useful for screening test compounds capable of modulating (particularly inhibiting) HCV NS3 protease activity. |
| 7273861 |
Non-nucleoside reverse transcriptase inhibitors |
September 25, 2007 |
| Compounds represented by formula 1: ##STR00001## wherein R.sup.1 is H, halogen, (C.sub.1-4)alkyl, O(C.sub.1-4)alkyl, and haloalkyl; R.sup.2 is H or methyl; R.sup.3 is H or (C.sub.1-4)alkyl; R.sup.4 is H or (C.sub.1-4)alkyl; R.sup.5 is (C.sub.1-4)alkyl, (C.sub.1-4)alkyl(C.sub.3-7)cyc |
| 7264811 |
Purified active HCV NS2/3 protease |
September 4, 2007 |
| A method for producing a refolded, inactive form of recombinantly produced NS2/3 protease which comprises the steps of: a) purifying the protease from inclusion bodies in the presence of a chaotropic agent; and b) refolding the purified protease by contacting it with a reducing agent |
| 7167801 |
Method of identifying potential inhibitors of human papillomavirus protein E2 using x-ray atomic |
January 23, 2007 |
| A crystallizable composition, comprising an human papillomavirus (HPV-11) E2 transactivation domain (TAD)-like polypeptide of SEQ ID NO. 2 complexed with an inhibitor L (sodium (2R,3R,4S,5R)-5-(3,4-dichlorophenyl)-5'-methyl-1',3'-dioxo-4-({[4-(1,2,3-- thiadiazol-4-yl)phenyl]amino}carb |
| 7157486 |
Viral polymerase inhibitors |
January 2, 2007 |
| An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: ##STR00001## wherein: A is O, S, NR.sup.1, or CR.sup.1, wherein R.sup.1 is defined herein; ----- represents either a single or a double bond; R.sup.2 is selected from: H, halogen, R.sup.21, |
| 7141574 |
Viral polymerase inhibitors |
November 28, 2006 |
| An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: ##STR00001## wherein: A is O, S, NR.sup.1, or CR.sup.1, wherein R.sup.1 is defined herein; - - - - - represents either a single or a double bond; R.sup.2 is selected from: H, halogen, R.sup.2 |
| 7119099 |
Inhibitors of papilloma virus |
October 10, 2006 |
| A compound of formula (I) or its enantiomers or diastereoisomers thereof: ##STR00001## wherein: A,; X, W, R.sup.1, Y; R.sup.3; and R.sup.4 are as defined herein.The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provi |
| 7119072 |
Macrocyclic peptides active against the hepatitis C virus |
October 10, 2006 |
| Compounds of formula I: ##STR00001## wherein R.sup.1 is hydroxy or NHSO.sub.2R.sup.1A wherein R.sup.1A is (C.sub.1-8)alkyl, (C.sub.3-7)cycloalkyl or {(C.sub.1-6)alkyl-(C.sub.3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O(C.sub.1-6) |
| 7105510 |
Non-nucleoside reverse transcriptase inhibitors |
September 12, 2006 |
| Compounds represented by formula I: ##STR00001## wherein R.sup.1 is H, halogen, (C.sub.1-4)alkyl, O(C.sub.1-4)alkyl, and haloalkyl; R.sup.2 is H or (C.sub.1-4)alkyl; R.sup.3 is H or (C.sub.1-4)alkyl; R.sup.4 is (C.sub.1-4)alkyl, (C.sub.1-4)alkyl(C.sub.3-7)cycloalkyl, or (C.sub.3-7)c |
| 6956117 |
Self-replicating RNA molecule from hepatitis C virus |
October 18, 2005 |
| A unique HCV RNA molecule is provided having an enhanced efficiency of establishing cell culture replication. Novel adaptive mutations have been identified within the HCV non-structural region that improves the efficiency of establishing persistently replicating HCV RNA in cell cultu |
| 6916622 |
Regions of papilloma virus E1 helicase involved in E1 oligomerization |
July 12, 2005 |
| There is provided an amino acid sequence comprised within the PV E1 protein region A delineated by amino acids 352 and 439, and any derivative variant or fragment thereof, necessary for the oligomerization of the E1 protein. This amino acid sequence is capable of self-association and of |
| 6852501 |
Methods for determining ATPase activity and uses thereof |
February 8, 2005 |
| The present invention uses the principle that phosphomolybdate binds to hydrophobic surfaces to isolate the phosphomolybdate complex from other phosphate-containing molecules and further uses the SPA concept to bring a radiolabeled phosphomolybdate complex in close contact with a scintil |
| 6825176 |
E2 displacement assay for identifying inhibitors of HPV |
November 30, 2004 |
| The present invention generally relates to an assay for identifying inhibitors of Human Papillomavirus (HPV), comprising: a) contacting a HPV E2 transactivation domain with a probe to form a E2:probe complex and measuring a signal from said probe to establish a base line level; b) |
| 6815159 |
Purified active HCV NS2/3 protease |
November 9, 2004 |
| A method for producing a refolded, inactive form of recombinantly produced NS2/3 protease which comprises the steps of: a) purifying the protease from inclusion bodies in the presence of a chaotropic agent; and b) refolding the purified protease by contacting it with a reducing agent and |
| 6811970 |
Assay for identifying inhibitors of HIV RT dimerization |
November 2, 2004 |
| A method for measuring heterodimerization of HIV RT, which comprises the steps of:a) providing a first solution comprising p66 subunit homodimers in the presence of a dissociation agent; b) contacting the first solution with p51 RT subunits and incubating in the presence of a reassociati |
| 6794404 |
Viral polymerase inhibitors |
September 21, 2004 |
| A compound of the formula I: ##STR1##wherein: X is CH or N; Y is O or S; Z is OH, NH.sub.2, NMeR.sup.3, NHR.sup.3 ; OR.sup.3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituent |
| 6767991 |
Hepatitis C inhibitor peptides |
July 27, 2004 |
| Disclosed herein are hepatitis C viral protease inhibitors of formula (I): ##STR1##wherein a is 0 or 1; b is 0 or 1; Y is H or C.sub.1-6 alkyl; B is H, an acyl derivative or a sulfonyl derivative; R.sub.6, when present, is C.sub.1-6 alkyl substituted with carboxyl; R.sub.5, when present |
| 6759409 |
Inhibitors of papilloma virus |
July 6, 2004 |
| A compound of formula (I) or its enantiomers or diastereoisomers thereof: ##STR1##wherein: A,; X, W, R.sup.1, Y; R.sup.3 ; and R.sup.4 are as defined herein.The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a met |
| 6716836 |
Non-nucleoside reverse transcriptase inhibitors |
April 6, 2004 |
| A compound of formula I: ##STR1##wherein A is a connecting chain of (C.sub.1-3) alkyl; B is O or S; R.sup.1 is H, (C.sub.1-6) alkyl, halo, CF.sub.3, or OR.sup.1a wherein R.sup.1a is H or (C.sub.1-6)alkyl; R.sup.2 is H or Me; R.sup.3 is H or Me; R.sup.4 is H, (C.sub.1-4) alkyl, (C. |
| 6673791 |
Non-nucleoside reverse transcriptase inhibitors |
January 6, 2004 |
| Compounds represented by formula I: ##STR1##wherein R.sup.2 is H, halogen, NHNH.sub.2, (C.sub.1-4)alkyl, O(C.sub.1-6)alkyl, and haloalkyl; R.sup.4 is H or Me; R.sup.5 is H or (C.sub.1-4)alkyl; R.sup.11 is (C.sub.1-4)alkyl, (C.sub.1-4)alkyl(C.sub.3-7)cycloalkyl, or (C.sub.3-7)cycloalk |
| 6608027 |
Macrocyclic peptides active against the hepatitis C virus |
August 19, 2003 |
| The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. ##STR1##wherein W, R.sup.21, R.sup.22, R.sup.3, R.sup.4, D and A are as defined herein, or a pharmaceutically acceptable salts or |
| 6596924 |
Graft animal model for high induction of papillomas, the propagation of papillomavirus and evalu |
July 22, 2003 |
| The present invention relates to a graft animal model for propagating papilloma virus and for evaluating and testing candidate therapeutic agents against papilloma virus. The animal model comprises, a recipient animal engrafted with injured skin graft infected with a host-specific pa |
| 6534523 |
Hepatitis C inhibitor tri-peptides |
March 18, 2003 |
| Racemates, diastereoisomers and optical isomers of a compound of formula (I): ##STR1##wherein B is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydroxy; |
| 6492181 |
Atpase assay |
December 10, 2002 |
| The present invention uses the principle that phosphomolybdate binds to hydrophobic surfaces to isolate the phosphomolybdate complex from other phosphate-containing molecules and further uses the SPA concept to bring a radiolabeled phosphomolybdate complex in close contact with a scintil |
| 6479508 |
Viral polymerase inhibitors |
November 12, 2002 |
| A compound of the formula I: ##STR1##wherein: X is CH or N; Y is O or S; Z is OH, NH.sub.2, NMeR.sup.3, NHR.sup.3 ; OR.sup.3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substitu |
| 6458959 |
Anti-herpesvirus compounds and methods for identifying, making and using same |
October 1, 2002 |
| This invention relates to methods for inhibiting herpes replication and for treating herpes infection in a mammal by inhibiting the herpes helicase-primase enzyme complex. This invention also relates to thiazolyphenyl derivatives that inhibit the herpes helicase-primase and to pharma |
| 6448281 |
Viral polymerase inhibitors |
September 10, 2002 |
| A compound of the formula I: ##STR1##wherein: X is CH or N; Y is O or S; Z is OH, NH.sub.2, NMeR.sup.3, NHR.sup.3 ; OR.sup.3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituent |
| 6420380 |
Hepatitis C inhibitor tri-peptides |
July 16, 2002 |
| Racemates, diastereoisomers and optical isomers of a compound of formula (I): ##STR1##wherein B is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydroxy; |
| 6420359 |
Non-nucleoside reverse transcriptase inhibitors |
July 16, 2002 |
| Provided are compounds of the general formula I: ##STR1##wherein R.sup.2 is selected from the group consisting of H, F, Cl, (C.sub.1-4) alkyl, (C.sub.3-4) cycloalkyl and CF.sub.3 ; R.sup.4 is H or Me; R.sup.5 is H, Me or Et, with the proviso that R.sup.4 and R.sup.5 are not both Me, |
| 6410531 |
Hepatitis C inhibitor tri-peptides |
June 25, 2002 |
| Racemates, diastereoisomers and optical isomers of a compound of formula (I): ##STR1##whereinB is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydroxy; hydr |
| 6329417 |
Hepatitis C inhibitor tri-pepitides |
December 11, 2001 |
| Racemates, diastereolsomers and optical isomers of a compound of formula (I): ##STR1##wherein B is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydroxy; hyd |
| 6329379 |
Hepatitis C inhibitor tri-peptides |
December 11, 2001 |
| Racemates, diastereoisomers and optical isomers of a compound of formula (I): ##STR1##whereinB is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydroxy; hydr |
| 6323202 |
HSV primase inhibitors |
November 27, 2001 |
| The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: ##STR1##whereinR.sub.1 is hydroxy or amino;R.sub.2 is hydrogen, halo, (C.sub.1-4)alkyl or (C.sub.1-4)alkoxy; R.sub.3 is hydrogen, halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, amino or azido; |
| 6323180 |
Hepatitis C inhibitor tri-peptides |
November 27, 2001 |
| A racemate, diastereoisomer and optical isomer of a compound of formula (I): ##STR1##wherein B is H, a C.sub.6 or C.sub.10 aryl, C.sub.7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C.sub.1-6 alkyl; C.sub.1-6 alkoxy; C.sub.1-6 alkanoyl; hydrox |
| 6313095 |
Antiherpes tetrapeptide derivatives having a substituted aspartic acid side chain |
November 6, 2001 |
| Disclosed herein are tetrapeptide derivatives of the formula X--NH--CHR.sup.1 --C(W.sup.1)--NR.sup.2 --CH[CH.sub.2 C(O)--Y]--C(W.sup.2)--NH--CH[CR.sup.3 (R.sup.4)--COOH]--C(W.sup.3)--NH--CHR.sup.5 --Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R. |
| 6306580 |
Preparation of human papillomavirus E1 having helicase activity and method therefor |
October 23, 2001 |
| The present invention relates to a method for isolating cloned papillomavirus E1 protein from a eukaryotic expression system having demonstrable and reproducible viral helicase activity and preparation containing essentially pure E1 protein. The invention further relates to the use o |
| 6268207 |
Enzymatic resolution of 1-amino-2-vinylcyclopropyl caboxylic acid methyl ester |
July 31, 2001 |
| An enantiomeric-resolving process for obtaining (1R,2S)-1-amino-2-vinylcyclopropyl carboxylic acid methyl ester by use of an esterase, and especially Alcalase.RTM., is disclosed. |
| 6242439 |
Azetidinone derivatives for the treatment of HCMV infections |
June 5, 2001 |
| A compound of formula I ##STR1##wherein R.sup.1 is hydrogen, methyl, ethyl, methoxy or methylthio; R.sup.2 and R.sup.3 each independently is hydrogen or lower alkyl; R.sup.4 is hydrogen, lower alkyl, methoxy, ethoxy or benzyloxy; R.sup.5 is lower alkyl, lower cycloalkyl, (CH.sub.2).s |
| 6239125 |
Azetidinone derivatives for the treatment of HCMV infections |
May 29, 2001 |
| A compound of formula 1: ##STR1##wherein Y is S or O;R.sub.1 is C.sub.1-6 alkyl; (C.sub.0-6 alkyl)aryl; (C.sub.0-6 alkyl)Het; orR.sub.1 is an amino acid analog or dipeptide analog of the formula: ##STR2##wherein R.sub.2 is H, C.sub.1-10 alkyl; or an amide or ester group;A is C.sub.6-10 aryl, |
| 6211170 |
Azetidinone derivatives for the treatment of HCMV infections |
April 3, 2001 |
| A compound of formula I: ##STR1##wherein R.sub.1 is hydrogen, methyl, ethyl, methoxy or methylthio; R.sub.2 and R.sub.3 each independently is hydrogen or C.sub.1-3 alkyl; R.sub.4 is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; R.sub.5 is lower alkyl, lower cycloalkyl, (CH.su |
| 6194143 |
Substrates for human cytomegalovirus protease |
February 27, 2001 |
| Human cytomegalovirus (HCMV) protease is a slow-processing enzyme in vitro. Disclosed herein are improved fluorogenic and radiometric peptide substrates for CMV protease. The improved substrates have a Tbg-Tbg-Asn(NMe.sub.2) sequence replacing the Val-Val-Asn sequence, corresponding |
| 6143715 |
Hepatitis C inhibitor peptide analogues |
November 7, 2000 |
| Compound of formula (I) active against the Hepatitis C virus: ##STR1## wherein B is an acyl derivative; a is 0 or 1; R.sub.6, when present, is carboxy(lower)alkyl; b is 0 or 1; R.sub.5, when present, is C.sub.1-6 alkyl, or carboxy (lower)alkyl; Y is H or C.sub.1-6 alkyl; R.sub.4 is |
| 5948935 |
Process and intermediates for (s)-.alpha.-amino-1-carboxycyclopentaneacetic acid |
September 7, 1999 |
| Disclosed herein is a process for preparing (S)-.alpha.-amino-1-carboxycyclopentaneacetic acid which is a useful intermediate for preparing peptidomimetic inhibitors of herpes viral ribonucleotide reductase. The process comprises the preparation of the key intermediate ##STR1## |
| 5925762 |
Practical synthesis of urea derivatives |
July 20, 1999 |
|
| 5846941 |
Isosteric antiherpes peptide derivatives II |
December 8, 1998 |
| Disclosed herein are peptidomimetic compounds of the formula A--B--D--CH.sub.2 CH{CH.sub.2 C(O)R.sup.1 }C(O)--NHCH{CR.sup.2 (R.sup.3)COOH}C(O)--E wherein A is a terminal group, for example an optionally substituted phenylalkanoyl, and B is a N-methyl amino acid residue; or A and B to |
