Adenosyl Patents (Class 536/27.3)
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Patent number: 7528247Abstract: The present invention for the stereoselective preparation of 2-deoxy-?-D-adenine nucleosides wherein a blocked 2-deoxy-?-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.Type: GrantFiled: January 9, 2004Date of Patent: May 5, 2009Assignee: Genzyme CorporationInventors: William E. Bauta, Brian D. Burke, Brian E. Schulmeier, William R. Cantrell, Jr., Dennis P. Lovett, Jose Puente
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Publication number: 20090105468Abstract: Orthogonally protected 3?-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3?-amino group in the presence of the unprotected nucleoside base.Type: ApplicationFiled: December 22, 2008Publication date: April 23, 2009Inventors: Sergei M. Gryaznov, Krisztina Pongracz, Daria Zielinska
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Patent number: 7514417Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists having the structure of Formula I: which are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: May 19, 2006Date of Patent: April 7, 2009Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Rao Kalla, Thao Perry, Jeff Zablocki, Xiaofen Li
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Patent number: 7504497Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae III, IIIa, and IIIb, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae IIIa and IIIb, which are potent and have a good oral bioavailability.Type: GrantFiled: November 9, 2006Date of Patent: March 17, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: James G. Douglass, III, Paul S. Watson, Carl A. Samuelson, Christopher S. Crean
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Patent number: 7488720Abstract: Disclosed are novel compounds that are A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, diseases related to release of nonesterified fatty acids, and myocardial infarction.Type: GrantFiled: October 11, 2006Date of Patent: February 10, 2009Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Xiaofen Li, Jeff Zablocki
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Patent number: 7485717Abstract: Orthogonally protected 3?-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3?-amino group in the presence of the unprotected nucleoside base.Type: GrantFiled: June 30, 2005Date of Patent: February 3, 2009Assignee: Geron CorporationInventors: Sergei M. Gryaznov, Krisztina Pongracz, Daria Zielinska
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Patent number: 7465544Abstract: The present invention discloses compounds and methods used to specifically target substrates of methylation by S-adenosyl-L-methionine (SAM)-dependent methyltransferases. The substrates can be peptides, single stranded nucleic acids or double stranded nucleic acids, including RNA, DNA and PNA or phospholipids. The compounds disclosed are SAM analogs that are ligated to a methylation site by the methyltransferase. Also disclosed, are reacting groups that are ligatable to the cofactor analogs and can also be used as detectable labels. The reacting group can be used to cleave the substrate providing a methylation footprint. The invention can be used clinically to determine methylation state of a gene or gene promoter such as those involved in imprinting and transcription. In some preferred embodiments, the invention includes a kit, which can include one or more suitable SAM analogs and may include one or more detectable labels. In other preferred embodiments, the invention includes a pharmaceutical composition.Type: GrantFiled: January 11, 2006Date of Patent: December 16, 2008Assignee: Wisconsin Alumni Research FoundationInventors: Scott R. Rajski, Lindsay R. Comstock, Rachel L. Weller
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Publication number: 20080261821Abstract: The present invention provides novel mechanism-based crosslinkers useful in covalently linking a kinase and an interactor.Type: ApplicationFiled: July 21, 2005Publication date: October 23, 2008Applicant: THE REGENTS OF TE UNIVERSITY OF CALIFORNIAInventors: Dustin Maly, Kevan M. Shokat
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Patent number: 7300923Abstract: Disclosed are syntheses suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: August 29, 2005Date of Patent: November 27, 2007Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Michael Organ, Yaroslav Bilokin, Stanislas Mayer, Anthony Disanti, Scott Miller, Peter Kernast
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Patent number: 7297787Abstract: An improved process for preparing N6 -substituted aminopurine ribofuranose nucleosides. Compounds of this type are known to be usefull in the prepartation of compounds having activitity at adenosine receptors, e.g. Adenosine A1 receptor. The process comprises the step of reacting a 6-halopurine ribofuranose nucleoside with an amine in the presence of CaCO3 , wherein acid is added to the reaction mixture.Type: GrantFiled: March 19, 2002Date of Patent: November 20, 2007Assignee: Glaxo Group LimitedInventors: Malcolm Berry, John C. Roberts, Shiping Xie
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Patent number: 7294486Abstract: There is described a process for the synthesis of a fluoronucleoside compound, said process comprising mixing a substrate and an enzyme from Streptomyces cattelya as catalyst. The process may be used to produce an 18F labelled fluoronucleoside compound. There is also described an enzyme derived from Streptomyces cattelya which has the capacity to catalyse the synthesis of a fluoronucleoside compound.Type: GrantFiled: September 5, 2002Date of Patent: November 13, 2007Assignee: The University Court of the University of St. AndrewsInventors: David O'Hagan, Christoph Schaffrath
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Patent number: 7271157Abstract: Disclosed is a synthesis suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonist having the structure of Formula I: wherein R is optionally substituted phenyl, that are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: June 30, 2005Date of Patent: September 18, 2007Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Jeff Zablocki
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Patent number: 7265111Abstract: The present invention relates to compounds according to the general formula (I) wherein X is selected from the group consisting of wherein n and p are independently 0, 1, 2, or 3, provided that n+p is a least 1; and unsubstituted and at least monosubstituted C1-C10-alkylene-Y, C2-C10-alkylene-Y, C3-C10-cycloalkylene-Y and C3-C10-cycloalkenylene-Y; and R1, A, B, Q, T, Y, E and W have the meanings given in the description. These compounds are useful for the manufacture of a medicament for the treatment of insulin resistance, type 2 diabetes, metabolic syndrome, lipid disorders or cardiovasular disease or for providing an anti-lipolytic effect.Type: GrantFiled: June 27, 2003Date of Patent: September 4, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Antony Bigot, Siegfried Stengelin, Gerhard Jaehne, Andreas Herling, Guenter Mueller, Franz Jakob Hock, Michael R Myers
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Patent number: 7262176Abstract: Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.Type: GrantFiled: November 25, 2003Date of Patent: August 28, 2007Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Patent number: 7217815Abstract: Various 2?-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particularly useful as therapeutic agents, and especially as antiviral agents.Type: GrantFiled: October 23, 2002Date of Patent: May 15, 2007Assignee: Valeant Pharmaceuticals North AmericaInventors: Haoyun An, Yili Ding, Stephanie Z. Shaw, Zhi Hong
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Patent number: 7179896Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: July 15, 2005Date of Patent: February 20, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 7157440Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: May 27, 2004Date of Patent: January 2, 2007Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Patent number: 7148042Abstract: A glyoxal-guanosine-group compound is prepared either by reacting glyoxal-guanine with any one of ribose-1-phosphate and 2-deoxyribose-1-phosphate in the presence of purine nucleoside phosphorylase, or by reacting glyoxal-guanine with any one selected from the group consisting of uridine, 2?-deoxyuridine and thymidine, together with phosphate ion, in the presence of purine nucleoside phosphorylase and pyrimidine nucleoside phosphorylase. The glyoxal-guanosine-group compound is then decomposed by alkali, whereby a guanosine-group compound consisting of guanosine and 2?-deoxyguanosine is prepared.Type: GrantFiled: July 8, 2003Date of Patent: December 12, 2006Assignee: Yuki Gosei Kogyo Co., Ltd.Inventors: Yoichi Mikami, Seiichiro Matsumoto, Yoshinori Hayashi, Toyoki Sato
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Patent number: 7141396Abstract: A glyoxal-guanosine-group compound is prepared either by reacting glyoxal-guanine with any one of ribose-1-phosphate and 2-deoxyribose-1-phosphate in the presence of purine nucleoside phosphorylase, or by reacting glyoxal-guanine with any one selected from the group consisting of uridine, 2?-deoxyuridine and thymidine, together with phosphate ion, in the presence of purine nucleoside phosphorylase and pyrimidine nucleoside phosphorylase. The glyoxal-guanosine-group compound is then decomposed by alkali, whereby a guanosine-group compound consisting of guanosine and 2?-deoxyguanosine is prepared.Type: GrantFiled: July 8, 2003Date of Patent: November 28, 2006Assignee: Yuki Gosei Kogyo Co., Ltd.Inventors: Yoichi Mikami, Seiichiro Matsumoto, Yoshinori Hayashi, Toyoki Sato
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Patent number: 7141397Abstract: A glyoxal-guanosine-group compound is prepared either by reacting glyoxal-guanine with any one of ribose-1-phosphate and 2-deoxyribose-1-phosphate in the presence of purine nucleoside phosphorylase, or by reacting glyoxal-guanine with any one selected from the group consisting of uridine, 2?-deoxyuridine and thymidine, together with phosphate ion, in the presence of purine nucleoside phosphorylase and pyrimidine nucleoside phosphorylase. The glyoxal-guanosine-group compound is then decomposed by alkali, whereby a guanosine-group compound consisting of guanosine and 2?-deoxyguanosine is prepared.Type: GrantFiled: July 8, 2003Date of Patent: November 28, 2006Assignee: Yuki Gosei Kogyo Co., Ltd.Inventors: Yoichi Mikami, Seiichiro Matsumoto, Yoshinori Hayashi, Toyoki Sato
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Patent number: 7109180Abstract: 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heartType: GrantFiled: March 30, 2004Date of Patent: September 19, 2006Assignee: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
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Patent number: 7094769Abstract: The present invention relates to compounds of the formula: and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.Type: GrantFiled: October 1, 2003Date of Patent: August 22, 2006Assignee: Pfizer IncInventors: Simon J. Mantell, Peter T. Stephenson
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Patent number: 7084127Abstract: The present invention concerns novel C2,5?-disubstituted and N6?,C2,5?-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.Type: GrantFiled: March 3, 2002Date of Patent: August 1, 2006Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.Inventors: Erica Van Tilburg, Ad Ijzerman
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Patent number: 7022727Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.Type: GrantFiled: September 3, 2004Date of Patent: April 4, 2006Assignee: Pfizer IncInventors: Terence Vernon Silk, Julian Duncan Smith
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Patent number: 7005425Abstract: Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a beta blocker, calcium channel blocker, or a cardiac glycoside.Type: GrantFiled: April 18, 2003Date of Patent: February 28, 2006Assignee: CV Therapeutics, Inc.Inventors: Luiz Belardinelli, Arvinder Dhalla
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Patent number: 6969766Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: April 25, 2003Date of Patent: November 29, 2005Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 6946449Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: July 11, 2002Date of Patent: September 20, 2005Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Patent number: 6914138Abstract: Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the intermediate is a 5-position modified pyrimidine ring, and the amine contains a second hydrogen, it can do a second Michael reaction with the ene-one or the ene-imine in the pyrimidine ring. Appropriate modification of the amine reactant can yield products with various bioactivities. The nucleosides can be used therapeutically as anti-cancer, anti-bacterial or anti-viral drugs. The nucleosides can also be used for diagnostic applications, for example, by incorporating a radiolabel or fluorescent label into the molecule.Type: GrantFiled: August 9, 2002Date of Patent: July 5, 2005Assignee: Gilead Sciences, Inc.Inventors: Gary Kirschenheuter, Bruce Eaton
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Patent number: 6903079Abstract: The invention provides a novel class of substituted nucleoside derivatives having the formula: A-Z1-L-Z2-G wherein: A and G are connected via Z1 and Z2 respectively, to a linker, L; and A is: wherein: X1 and X2 are N; X3 is —N?CH; R1 and R2 are independently H, alkyl, NH2, OH, SH, Cl, NHR9, or N?NR9, where R9 is alkyl, aryl, or arylalkyl; R5 and R6 are independently alkyl, or R5 and R6 taken together form a —C(CH3)2— group; Z1 is —CH2O—, —CH2NR10—, —CH2NR10C(O)—, —CONR10—, —CO2—, —CH2NHCONH—, —CH2—, —CH2NHCSNH—, —CO—, —CH2CO2—, —NHCO2—, —S—, —SO2—, —CH2S—, or —SO—; Z2 is —NR10CO—, —C(O)NR10—, —NHCONH—, —OC(O)—, —C(O)O—, NHCS, —CSNH—, —NHCSNH—, —O—, —CO—, —OCO—, —OCONH—, —NH—, —CH2—, —CH—alkyl—, —NHCO2—, —S—, —SO2—, CS—, or —SO—; L is H, O, S, C1-15 alkylene chain optionally substituted in one or more positions, a 5, 6 or 7 membered carbocycle, piperidine, piperazine, pyrole, imidazole, benzimidazole, tetrazoles, indole, isoquinoline, quinoline, or pyrrolidine, any of the 5, 6 or 7 membered carbocyclType: GrantFiled: December 16, 2002Date of Patent: June 7, 2005Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Garry Southan, Andrew Salzman, Csaba Szabo, Siya Ram
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Patent number: 6884880Abstract: A process for substantially enhancing the regio and stereoselective synthesis of 9-?-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-?-D- or L-purine nucleoside analogs were obtained. This regio and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs and in particular 2?-deoxy, 3?-deoxy, 2?-deoxy-2?-?-fluoro and 2?,3?-dideoxy-2?-?-fluoro purine nucleoside analogs in high yield without virtually any formation of the 7-positional isomers. The compounds are drugs or intermediates to drugs.Type: GrantFiled: August 21, 2002Date of Patent: April 26, 2005Assignee: Ash Stevens, Inc.Inventors: Pranab K. Gupta, Stephen A. Munk
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Patent number: 6855818Abstract: 2-adenosine C-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.Type: GrantFiled: March 19, 2001Date of Patent: February 15, 2005Assignee: CV Theraeputics, Inc.Inventors: Jeff A. Zablocki, Venkata P. Palle, Elfatih O. Elzein
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Patent number: 6852746Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.Type: GrantFiled: December 3, 2002Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Terence Vernon Silk, Julian Duncan Smith
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Publication number: 20040229838Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: June 15, 2004Publication date: November 18, 2004Applicant: Pfizer IncInventors: Simon John Mantell, Sandra Marina Monaghan, Peter Thomas Stephenson
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Publication number: 20040198692Abstract: 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.Type: ApplicationFiled: March 30, 2004Publication date: October 7, 2004Applicant: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
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Publication number: 20040198693Abstract: A3 agonists, methods of using such A3 agonists and pharmaceutical compositions containing such A3 agonists. The A3 agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia.Type: ApplicationFiled: April 12, 2004Publication date: October 7, 2004Inventors: Michael P. DeNinno, Hiroko Masamune, Robert W. Scott
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Publication number: 20040192635Abstract: The invention relates to compositions comprising acyl derivatives of 2′-deoxyribonucleosides. The invention also relates to methods of treating or preventing radiation, mutagen and sunlight-induced cellular damage, methods for improving wound healing and tissue repair, and methods for ameliorating the effects of aging comprising administering the compositions of the present invention to an animal.Type: ApplicationFiled: April 15, 2004Publication date: September 30, 2004Applicant: Wellstat Therapeutics CorporationInventors: Reid W. Von Borstel, Michael K. Bamat
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Patent number: 6780429Abstract: The present invention provides a chain-shortened polynucleotide wherein the proportion of a 2′-5′ phosphodiester bond is up to 3% based on the whole phosphodiester bonds or a salt thereof and a pharmaceutical composition containing the same, and a method for producing the same.Type: GrantFiled: August 13, 2001Date of Patent: August 24, 2004Assignee: Nippon Shinyaku Co., Ltd.Inventors: Shinji Matsuyama, Kouichi Ishiyama, Junzo Seki, Tadaaki Ohgi
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Publication number: 20040162422Abstract: The present invention is concerned with pharmaceutical compositions containing certain adenosine derivatives having an acetylene group in the 4′ position, which are adenosine A1 agonists, and to their use in therapy.Type: ApplicationFiled: March 4, 2004Publication date: August 19, 2004Inventors: Adrian Hall, Karamjit Singh Jandu, Christopher James Lunniss, Maria Victoria Vinader, Robert Ian West
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Patent number: 6770634Abstract: 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.Type: GrantFiled: March 12, 2002Date of Patent: August 3, 2004Assignee: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
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Publication number: 20040132686Abstract: The present invention concerns novel C2,5′-disubstituted and N6′,C2,5′-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.Type: ApplicationFiled: March 4, 2004Publication date: July 8, 2004Inventors: Erica Van Tilburg, Ad Ijzerman
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Patent number: 6759395Abstract: The invention provides a novel soft gelatin capsule comprising a fill material consisting essentially of S-adenosylmethionine (SAMe) salt disposed within an enteric coated soft gelatin film.Type: GrantFiled: December 18, 2001Date of Patent: July 6, 2004Assignee: Orchid Chemicals & Pharmaceuticals, Ltd.Inventors: Canakapalli Bhaktavatsala Rao, Prasanta Kumar Chakrabarti, Hema Ravishankar
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Publication number: 20040127452Abstract: The present invention concerns novel C2,5′-disubstituted and N6,C2,5′-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.Type: ApplicationFiled: September 3, 2003Publication date: July 1, 2004Applicants: UNIVERSITEIT LEIDEN, CAN-FITE BIOPHARMA LTD.Inventors: Erica Van Tilburg, Ad Ijzerman
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Publication number: 20040127434Abstract: The present invention relates to compounds according to the general formula (I) 1Type: ApplicationFiled: June 27, 2003Publication date: July 1, 2004Inventors: Antony Bigot, Siegfried Stengelin, Gerhard Jaehne, Andreas Herling, Guenter Mueller, Franz Jakob Hock, Michael R. Myers
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Publication number: 20040121978Abstract: Disclosed are novel adenosine A3 receptor agonists, useful for treating various disease states, including neurological and cardiac ischemia, asthma, leukopenia and neutropenia, cancer and inflammation.Type: ApplicationFiled: September 8, 2003Publication date: June 24, 2004Inventor: Gloria Cristalli
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Patent number: 6753322Abstract: The present invention relates to compounds of the formula: and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.Type: GrantFiled: June 5, 2001Date of Patent: June 22, 2004Assignee: Pfizer IncInventors: Simon John Mantell, Peter Thomas Stephenson
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Publication number: 20040116374Abstract: Novel C2, 8-disubstituted adenosine derivatives disclosed herein have been found to be potent adenosine receptor agonists, in particular for the A2A receptor. The said compounds have biological activity against conditions such as hypertension, ischemic heart disease, ischemic brain disease, psychosis and wound healing. Further, the invention also discloses a process for the preparation of such compounds and pharmaceutical compositions comprising them.Type: ApplicationFiled: February 9, 2004Publication date: June 17, 2004Inventors: Erica Van Tilburg, Ad Ijzerman
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Publication number: 20040116376Abstract: Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.Type: ApplicationFiled: November 25, 2003Publication date: June 17, 2004Inventors: Elfatih Elzein, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Patent number: 6740644Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, —SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine A1 receptor.Type: GrantFiled: February 26, 2003Date of Patent: May 25, 2004Assignee: Smithkline Beecham CorporationInventors: Colin David Eldred, Andrew Michael Kenneth Pennell
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Publication number: 20040077584Abstract: The present invention relates to compounds of the formula: 1Type: ApplicationFiled: October 1, 2003Publication date: April 22, 2004Applicant: Pfizer IncInventors: Simon J. Mantell, Peter T. Stephenson
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Patent number: 6713623Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.Type: GrantFiled: November 13, 2001Date of Patent: March 30, 2004Assignee: Pharmasset, Ltd.Inventors: Krzysztof W. Pankiewicz, Krystyna Lesiak, Kyoichi A. Watanabe