Patents Assigned to Biochem Pharma
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Patent number: 6156737Abstract: 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.Type: GrantFiled: April 12, 1995Date of Patent: December 5, 2000Assignee: BioChem Pharma Inc.Inventors: Tarek Mansour, Allan H.L. Tse
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Patent number: 6127540Abstract: 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.a is hydrogen, OH, halogen, N.sub.3, NH.sub.2, SH, carboxyl, C.sub.1-6 alkyl or R.sub.a is CH.sub.2 (R.sub.b) wherein R.sub.b is hydrogen, OH, SH, NH.sub.2, C.sub.1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond;Z is selected from: O, a C.sub.1-6 alkoxy, a C.sub.1-6 thioalkyl, a C.sub.1-6 aminoalkyl, (CH.sub.2).sub.m wherein m is 0 or an integer, and N(R.sub.c).sub.2 wherein both R.sub.c are independently hydrogen or a C.sub.1-6 alkyl; andR2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.Type: GrantFiled: October 4, 1999Date of Patent: October 3, 2000Assignee: BioChem Pharma, Inc.Inventors: Nghe Nguyen-Ba, Miguel Quimpere, Laval Chan Chun Kong, William L. Brown, Gervais Dionne
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Patent number: 6110923Abstract: The present invention covers a method of treatment of cancer, in particular, colon carcinoma, comprising the step of administering the compound N2-(6-dimethylamino purin-9-yl)-7-pentyloxycarbonyl-L-arginine in combination with 5-fluorouracil. The present invention also covers pharmaceutical composition containing these two compounds for the treatment of cancer.Type: GrantFiled: June 7, 1995Date of Patent: August 29, 2000Assignee: Biochem Pharma Inc.Inventor: Guy Ely
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Patent number: 6069250Abstract: 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 intermediate of formula (II) below a temperature of about -10.degree. C. ##STR1## wherein R.sub.1 and L are as defined herein.Type: GrantFiled: February 17, 1999Date of Patent: May 30, 2000Assignee: Biochem Pharma Inc.Inventors: Tarek Mansour, Alex Cimpoia, Krzysztof Bednarski
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Patent number: 6057314Abstract: 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 agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.Type: GrantFiled: June 23, 1997Date of Patent: May 2, 2000Assignee: Biochem Pharma Inc.Inventors: John Dimaio, M. Arshad Siddiqui, John W. Gillard, Yves St-Denis, Micheline Tarazi, Patrice Preville, Sophie Levesque, Benoit Bachand, Annette Marian Doherty, Jeremy John Edmunds
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Patent number: 6054474Abstract: 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 optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6 or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X is O, S, SO, SO.sub.2, N--R.sub.5, or C--(R.sub.5).sub.2, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH.sub.2 then R1 is not CH.sub.3, R.sub.2 and R.sub.3 are not both H, R.sub.4 is not OH, m is not 3 and n is not 0.Type: GrantFiled: March 25, 1998Date of Patent: April 25, 2000Assignee: Biochem Pharma, Inc.Inventors: John Dimaio, Dilip M. Dixit
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Patent number: 6005107Abstract: 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.a is hydrogen, OH, halogen, N.sub.3, NH.sub.2, SH, carboxyl, C.sub.1-6 alkyl or R.sub.a is CH.sub.2 (R.sub.b) wherein R.sub.b is hydrogen, OH, SH, NH.sub.2, C.sub.1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond;Z is selected from: O, a C.sub.1-6 alkoxy, a C.sub.1-6 thioalkyl, a C.sub.1-6 aminoalkyl, (CH.sub.2).sub.m wherein m is 0 or an integer, and N(R.sub.c).sub.2 wherein both R.sub.c are independently hydrogen or a C.sub.1-6 alkyl; andR2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.Type: GrantFiled: June 4, 1997Date of Patent: December 21, 1999Assignee: BioChem Pharma, Inc.Inventors: Nghe Nguyen-Ba, Miguel Quimpere, Laval Chan Chun Kong, William L. Brown, Gervais Dionne
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Patent number: 5994361Abstract: The present invention comprises a compound of formula I: ##STR1## R.sub.1 of Formula I is substituted amino represented by formula NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1-4 alkyl, and unsubstituted amino with the proviso that R.sup.5 and R.sup.6 are not both hydrogen, and further that R.sup.5 and R.sup.6 are not both amino. R.sub.2 and R.sub.3 of Formula I are independently selected from the group consisting of hydrogen; C.sub.1-4 alkyl; amino; substituted or unsubstituted thiol; and halogen. Moreover, R.sub.4 of Formula I is represented by the formula R.sup.12 -X.sup.12 wherein R.sup.12 is a saturated or unsaturated linear hydrocarbon chain of 5-20 carbons optionally containing one or more interruptions within the chain by a heteroatom, and optionally substituted with one or more .dbd.O, or .dbd.S. Finally, X.sup.12 is selected from the group consisting of hydroxy, an aminoalkyl group, and a known amino acid bound by its .alpha.Type: GrantFiled: June 7, 1995Date of Patent: November 30, 1999Assignee: Biochem PharmaInventors: Christopher Penney, Boulos Zacharie, Lyne Gagnon, Giorgio Attardo, Timothy P. Connolly, Yves St-Denis, Salam Kadhim
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Patent number: 5990104Abstract: 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 substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.Type: GrantFiled: March 25, 1998Date of Patent: November 23, 1999Assignee: Biochem Pharma, Inc.Inventors: John Dimaio, Dilip M. Dixit
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Patent number: 5980913Abstract: 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 vaccine adjuvant.Type: GrantFiled: June 19, 1997Date of Patent: November 9, 1999Assignee: Biochem Pharma, Inc.Inventor: Christopher L. Penney
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Patent number: 5955493Abstract: 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 protective agents against peripheral and central nervous system NMDA-receptor mediated toxicity and convulsions.Type: GrantFiled: April 30, 1998Date of Patent: September 21, 1999Assignee: Biochem Pharma, Inc.Inventor: Simon Lemaire
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Patent number: 5955610Abstract: 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.a is hydrogen, OH, halogen, N.sub.3, NH.sub.2, SH, carboxyl, C.sub.1-6 alkyl or R.sub.a is CH.sub.2 (R.sub.b) wherein R.sub.b is hydrogen, OH, SH, NH.sub.2, C.sub.1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond;Z is selected from: O, a C.sub.1-6 alkoxy, a C.sub.1-6 thioalkyl, a C.sub.1-6 aminoalkyl, (CH.sub.2).sub.m wherein m is 0 or an integer, and N(R.sub.c).sub.2 wherein both R.sub.c are independently hydrogen or a C.sub.1-6 alkyl; andR2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.Type: GrantFiled: June 4, 1997Date of Patent: September 21, 1999Assignee: Biochem Pharma, Inc.Inventors: Nghe Nguyen-Ba, Miguel Quimpere, Laval Chan Chun Kong, William L. Brown, Gervais Dionne
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Patent number: 5922867Abstract: 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 intermediate of formula (II) below a temperature of about -10.degree. C. ##STR1## wherein R.sub.1 and L are defined herein.Type: GrantFiled: June 26, 1997Date of Patent: July 13, 1999Assignee: Biochem Pharma Inc.Inventors: Tarek Mansour, Alex Cimpoia, Krzysztof Bednarski
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Patent number: 5763606Abstract: 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 pyrimidine base in the presence of an appropriate Lewis acid with a bicyclic intermediate of formula (III) wherein Z is S or O; followed by conversion of the resulting intermediate of formula (II) to an alkyl ester and reduction to yield a compound of formula (I).Type: GrantFiled: February 2, 1995Date of Patent: June 9, 1998Assignee: BioChem Pharma, Inc.Inventors: Tarek S. Mansour, Colleen A. Evans, Haolun Jin, M. Arshad Siddiqui, Allan H. L. Tse
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Patent number: 5756706Abstract: 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.Type: GrantFiled: May 13, 1994Date of Patent: May 26, 1998Assignee: BioChem Pharma Inc.Inventors: Tarek Mansour, Allan H. L. Tse
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Patent number: 5744596Abstract: 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.Type: GrantFiled: June 5, 1995Date of Patent: April 28, 1998Assignee: Biochem Pharma Inc.Inventors: Tarek Mansour, Allan H. L. Tse
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Patent number: 5736523Abstract: 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.Type: GrantFiled: March 10, 1995Date of Patent: April 7, 1998Assignee: Biochem Pharma Inc.Inventors: Giorgio Attardo, Tibor Breining, Marc Courchesne, Serge Lamothe, Jean-Fran.cedilla.ois Lavallee, Dieu Nguyen, Rabindra Rej, Yves St-Denis, Wuyi Wang, Yao-Chang Xu, France Barbeau, Elaine Lebeau, Jean Louis Kraus
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Patent number: 5696254Abstract: 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.Type: GrantFiled: June 13, 1994Date of Patent: December 9, 1997Assignee: BioChem Pharma Inc.Inventors: Tarek Mansour, Haolun Jin, Allan H. L. Tse, M. Arshad Siddiqui
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Patent number: 5693787Abstract: 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.Type: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: BioChem Pharma Inc.Inventors: Tarek Mansour, Haolun Jin, Allan H. L. Tse, M. Arshad Siddiqui
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Patent number: 5688771Abstract: 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 and animal diseases. Processes for the syntheses of immunomodulating chemicals are also disclosed.Type: GrantFiled: October 3, 1994Date of Patent: November 18, 1997Assignee: BioChem Pharma Inc.Inventors: Christopher Penney, Boulos Zacharie