| Patent Number |
Title Of Patent |
Date Issued |
| 6903224 |
Substituted 1,3-oxathiolanes |
June 7, 2005 |
| Substituted 1,3-oxathiolanes, such as cis- and trans-2-ethoxycarbonyl-5-hydroxy-1,3-oxathiolane and cis- and trans-2-ethoxycarbonyl-5-acetoxy-1,3-oxathiolane, are suitable as intermediates for the production of substituted 1,3-oxathiolanes nucleoside analogs having antiviral properti |
| 6784161 |
Method for the treatment or prevention of flavivirus infections using nucleoside analogues |
August 31, 2004 |
| The present invention relates to a method for the treatment or prevention of Flavivirus infections using nucleoside analogues in a host comprising administering a therapeutically effective amount of a compound having the formula I or a pharmaceutically acceptable salt thereof. |
| 6747036 |
Methods of treating leukemia |
June 8, 2004 |
| The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: ##STR1##wherein B is cytosine or 5-fluorocy |
| 6743910 |
Stereoselective synthesis of nucleoside analogues |
June 1, 2004 |
| The invention is a process for stereoselectively producing a dioxolane nucleoside analogue from an anomeric mixture of .beta. and .alpha. anomers represented by the following formula A or formula B: ##STR1##wherein R is selected from the group consisting of C.sub.1-6 alkyl and C.sub. |
| 6630488 |
Quinolizinones as integrin inhibitors |
October 7, 2003 |
| The present invention is directed towards novel compounds that are effective inhibitors of integrins, particularly .alpha..sub.IIb.beta..sub.3 or .alpha..sub.v integrins such as .alpha..sub.v.beta..sub.3 and .alpha..sub.v.beta..sub.5. One embodiment of the present invention comprises |
| 6630480 |
Methods of treating leukemia |
October 7, 2003 |
| The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: ##STR1## wherein B is cytosine or 5-fluo |
| 6605614 |
[1,8] naphthyridine derivatives having antiviral activity |
August 12, 2003 |
| The present invention is concerned with novel [1,8] naphthyridine derivatives useful for the inhibition of the hepatitis virus, more specifically the hepatitis C virus. |
| 6545001 |
Antiviral nucleoside analogues |
April 8, 2003 |
| The invention relates to cis-nucleosides of formula (I): ##STR1##and pharmaceutically acceptable salts thereof, wherein X, R.sub.3, R.sub.4 and are as defined herein. The nucleosides can be in racemic form or in the form of their (+) or (-) enantiomers. The compounds are useful for t |
| 6541625 |
Stereoselective synthesis of nucleoside analogues |
April 1, 2003 |
| The invention is a process for stereoselectively producing a dioxolane nucleoside analogue from an anomeric mixture of .beta. and .alpha. anomers represented by the following formula A or formula B: ##STR1##wherein R is selected from the group consisting of C.sub.1-6 alkyl and C.sub. |
| 6534520 |
Antiviral compounds |
March 18, 2003 |
| The present invention relates to heterocyclic Compounds having antiviral activity. In particular, Compounds of formula (I): ##STR1##wherein B, W, X, Y, Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n are as defined herein, are useful in the therapy and prophylaxis of viral infection in m |
| 6511983 |
Pharmaceutical combination of antiviral agents |
January 28, 2003 |
| In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of viral infections comprising a at least one antiviral active compound of formula (1): ##STR1##and at least one further therapeutic agent chosen from nucleoside analogues |
| 6444656 |
Antiviral phosphonate nucleotides |
September 3, 2002 |
| The present invention relates to a novel nucleotide analogue having the general formula (I) and pharmaceutically acceptable salts, esters, or salt of such esters: ##STR1##wherein n, X, Q U R1', R1, Z and R.sub.2 are defined here within. The compounds object of the present invention m |
| 6369066 |
Substituted 1,3-oxathiolanes with antiviral properties |
April 9, 2002 |
| This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): ##STR1##wherein;R.sub.1 is hydrogen, and R.sub.2 is cytosine or 5-fluorocytosine;and pharmaceutically acceptable salts and esters thereof.This invention also relates to pharmaceutical |
| 6358963 |
Antiviral nucleoside analogues |
March 19, 2002 |
| The current invention is down to (+) an (-) enantiomers, as well as racemic mixtures of nucleoside analogs, wherein the carbohydrate portion of the analog is a dioxolane moiety and the nucleobase moiety is N.sup.6 -carbocyclic-alkylamino-substituted-2-amino-purine moiety attached via its |
| 6350753 |
2-Substituted-4-substituted-1,3-dioxolanes and use thereof |
February 26, 2002 |
| Nucleoside analogues containing a 1,3-dioxolane structure are suitable antiviral agents, particulary for the treatment of the HIV infections in mammals, especially humans. Examples of the nucleoside analogues include:cis-2-acetoxymethyl-4-(thymin-1'-yl)-1,3,-dioxolane,cis-2-hydroxymethyl-4-( |
| 6340690 |
Antiviral methods using [1,8]naphthyridine derivatives |
January 22, 2002 |
| The present invention is concerned with novel [1,8] naphthyridine derivatives useful for the inhibition of the hepatitis virus, more specifically the hepatitis C virus. |
| 6287574 |
Proteinase K resistant surface protein of neisseria meningitidis |
September 11, 2001 |
| A highly conserved, immunologically accessible antigen at the surface of Neisseria meningitidis organisms. Immunotherapeutic, prophylactic and diagnostic compositions and methods useful in the treatment, prevention an diagnosis of Neisseria meningitidis diseases. A proteinase K resistant |
| 6274620 |
Thiophene integrin inhibitors |
August 14, 2001 |
| The present invention comprises compounds that are effective inhibitors of integrins, particularly .alpha.v.beta.3 and .alpha.v.beta.5 integrins. Particularly, the compounds are of formula I ##STR1##and pharmaceutically acceptable salts thereof wherein X,Y.sub.1 W, R1 to R5, A and B |
| 6255318 |
Antiviral compounds |
July 3, 2001 |
| The present invention relates to heterocyclic Compounds having antiviral activity. In particular, Compounds of formula (I): ##STR1##wherein B, W, X, Y, Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n are as defined herein, are useful in the therapy and prophylaxis of viral infection in m |
| 6228860 |
Substituted 1,3-oxathiolanes with antiviral properties |
May 8, 2001 |
| This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): ##STR1##wherein;R.sub.1 is hydrogen, and R.sub.2 is cytosine or 5-fluorocytosine, and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharm |
| 6180639 |
1,3-oxathiolane nucleoside analogues |
January 30, 2001 |
| (-)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one, its pharmaceutically acceptable derivatives, pharmaceutical formulation thereof, methods for its preparation and its uses as an antiviral agent are described. |
| 6175008 |
Processes for preparing substituted 1,3-oxathiolanes with antiviral properties |
January 16, 2001 |
| Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1##wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to inte |
| 6156737 |
Use of dideoxy nucleoside analogues in the treatment of viral infections |
December 5, 2000 |
| The present invention is directed to a method of treating hepatitis B viral infections in mammals comprising the administration of .beta.-L-5-fluoro-2',3'-dideoxycytidine and pharmaceutically acceptable derivatives thereof. |
| 6069250 |
Method and compositions for the synthesis of dioxolane nucleosides with .beta.-configuration |
May 30, 2000 |
| The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an |
| 6057314 |
Low molecular weight bicyclic thrombin inhibitors |
May 2, 2000 |
| This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin, their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as a |
| 6054474 |
Heterocyclic compounds for the treatment of pain and use thereof |
April 25, 2000 |
| Polycyclic alkaloids of formula (I), ##STR1## wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl opt |
| 6005107 |
Antiviral compounds |
December 21, 1999 |
| Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH.sub.2, CH-halogen, CH--N.sub.3, or C.dbd.CH.sub.2 ;Q and U are independently selected from: O, S, and CH(R.sub.a) wherein R.sub. |
| 5990104 |
Polycyclic alcaloid-derivatives as NMDA-receptor antagonists |
November 23, 1999 |
| Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substitut |
| 5980913 |
Peptides having immunomodulatory activity |
November 9, 1999 |
| The present invention relates to peptides having an immunomodulatory activity. The present invention is concerned with the tetrapeptide H-Lys-Asn-Pro-Tyr-OH (SEQ.ID NO:1) and analogues thereof as immunomodulators. The present invention also includes the use of such peptides as vaccin |
| 5955493 |
Thiamorphinans with neuroprotective activity |
September 21, 1999 |
| The present invention relates to morphinan derivatives that are neuroprotective against excitatory amino acid (EAA) cytotoxicity. In particular, morphinan derivatives of the invention act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor and are useful as pr |
| 5922867 |
Method and compositions for the synthesis of dioxolane nucleosides with .beta. configuration |
July 13, 1999 |
| The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an |
| 5763606 |
Stereoselective synthesis of nucleoside analogues using bicyclic intermediate |
June 9, 1998 |
| The present invention relates to a process for producing predominantly pure cis nucleoside analogues of formula (I), wherein X is S, or O; Y is S, CH.sub.2, O or CH(R); wherein R is azido or halogen; and R.sub.2 is a purine or pyrimidine base; via the coupling of a silylated purine or |
| 5756706 |
Processes for the diastereoselective synthesis of nucleoside analogues |
May 26, 1998 |
| The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity, and intermediates useful in those processes. |
| 5744596 |
Nucleoside analogues and synthetic intermediates |
April 28, 1998 |
| The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes. |
| 5736523 |
Antineoplastic heteronapthoquinones |
April 7, 1998 |
| This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals. |
| 5696254 |
Processes for the diastereoselective synthesis of nucleoside analogues |
December 9, 1997 |
| The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity, and intermediates useful in those processes. |
| 5693787 |
Intermediates in the synthesis of 1,3-oxathiolanyl cytosine nucleoside analogues |
December 2, 1997 |
| The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes. |
| 5688771 |
Lipophilic oligopeptides with immunomodulating activity |
November 18, 1997 |
| New, small and structurally simple immunomodulating oligopeptides are disclosed. The oligopeptides of this invention possess a long, lipophilic alkyl chain. These immunomodulating oligopeptides can be used in conjunction with anti-viral or anti-cancer agents in the treatment of human |
| 5684164 |
Processes for preparing substituted 1,3-oxathiolanes with antiviral properties |
November 4, 1997 |
| Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to |
| 5663320 |
Processes for the diastereoselective separation of nucleoside analogue synthetic intermediates |
September 2, 1997 |
| The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes. |
| 5618820 |
1,3-oxathiolane nucleoside analogues and methods for using same |
April 8, 1997 |
| The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives |
| 5606037 |
Processes antineoplastic heteronaphthoquinones |
February 25, 1997 |
| This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals. |
| 5593970 |
Heterocyclic anthracycline analogs |
January 14, 1997 |
| Novel pyrano heterocyclic anthracycline derivatives are described, which are useful in the treatment of cancer and tumors, such as breast cancer, leukemia, lung cancer, colon cancer, ovarian cancer, renal cancer, and melanoma. As well, these compounds may be used ex vivo for the treatmen |
| 5587480 |
Substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes with antiviral properties |
December 24, 1996 |
| This invention relates to novel substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes or pharmaceutically acceptable salts and esters thereof, of the formula: ##STR1## wherein X is S, S.dbd.O, or SO.sub.2 ;Y is O, S, S.dbd.O, or SO.sub.2 ;R.sub.1 is hydrogen, trisubstituted si |
| 5538975 |
1,3-oxathiolane nucleoside compounds and compositions |
July 23, 1996 |
| The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives |
| 5532246 |
Use of 1,3-oxathiolane nucleoside analogues in the treatment of hepatitis B |
July 2, 1996 |
| Use of a compound of formula (I) or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of hepatitis B is disclosed. ##STR1## |
| 5486520 |
1,3-oxathiolanes useful in the treatment of hepatitis |
January 23, 1996 |
| The present invention relates to the use of nucleoside analogues in the treatment of viral infections. More specifically it is concerned with the use of 1,3-oxathiolane nucleoside analogues in the treatment of hepatitis, in particular hepatitis B. |
| 5466806 |
Processes for preparing substituted 1,3-oxathiolanes with antiviral properties |
November 14, 1995 |
| Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to |
| 5466806 |
Processes for preparing substituted 1,3-oxathiolanes with antiviral properties |
November 14, 1995 |
| Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to |
| 5371185 |
1-amino thiorcyl benzimidazoyl-2-one compounds |
December 6, 1994 |
| This invention relates to 1-amino thioacylbenzimidazoyl-2-one derivatives having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined herein. These compounds are useful as thioacylating reagents. This invention also relates to a process for producing cyclic and |
