The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/263.23)
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Publication number: 20080139566Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: ApplicationFiled: January 24, 2008Publication date: June 12, 2008Inventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Patent number: 7335654Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: GrantFiled: August 8, 2003Date of Patent: February 26, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Allen T. Hopper, Ruiping Liu
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Publication number: 20080019957Abstract: A method of treating skin changes and conditions in human skin including applying a topical preparation that includes an active agent including probucol, a derivative of probucol or a combination of probucol and a derivative of probucol.Type: ApplicationFiled: July 20, 2007Publication date: January 24, 2008Inventors: Birgit Neudecker, Falko Diedrich, Eberhard Wieland
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Publication number: 20080009508Abstract: The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives.Type: ApplicationFiled: July 9, 2007Publication date: January 10, 2008Inventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Ludek Frohlich, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Patent number: 7291623Abstract: A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 5, 2003Date of Patent: November 6, 2007Assignee: Alchemia LimitedInventors: Wim Meutermans, Karl Schafer, Michael L. West, Craig Muldoon, Fiona Foley, Natalie Bouloc, Gerald Tometzki
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Patent number: 7268141Abstract: A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:Type: GrantFiled: February 12, 2004Date of Patent: September 11, 2007Assignee: Schering CorporationInventors: Samuel Chackalamannil, Yuguang Wang, Craig Boyle, Andrew Stamford
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Publication number: 20070203159Abstract: The invention provides an antimycobacterial 6-aryl-9-(m- or p-substituted-benzyl) purine and purine analog compounds.Type: ApplicationFiled: February 28, 2006Publication date: August 30, 2007Applicant: Universitetet i OlsoInventors: Lise-Lotte Gundersen, Morten Braendvang
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Patent number: 7256196Abstract: The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 2,8,9-substituted purines and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.Type: GrantFiled: December 7, 2004Date of Patent: August 14, 2007Assignee: The Procter & Gamble CompanyInventors: Mark Sabat, Michael Philip Clark, Todd Andrew Brugel, Adam Golebiowski, John Charles Van Rens, Biswanath De
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Patent number: 7247639Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.Type: GrantFiled: June 4, 2004Date of Patent: July 24, 2007Assignee: Endacea, Inc.Inventors: Constance N. Wilson, John J. Partridge
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Patent number: 7217702Abstract: Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A blockers are useful for the treatment of Parkinsons disease and other diseases.Type: GrantFiled: April 4, 2005Date of Patent: May 15, 2007Assignee: Adenosine Therapeutics, LLCInventors: Anthony Beauglehole, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7202252Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: GrantFiled: February 17, 2004Date of Patent: April 10, 2007Assignee: Endacea, Inc.Inventors: Constance Neely Wilson, John J. Partridge
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Patent number: 7199127Abstract: Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R1 is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3? are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocarbonyl, whereas R3 and R3? do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.Type: GrantFiled: October 24, 2003Date of Patent: April 3, 2007Assignees: United States of America, Represented by the Secretary, Department of Health and Human Services, Ewha Womans UniversityInventors: Lak Shin Jeong, Kenneth A. Jacobson, Hyung Ryong Moon, Hea Ok Kim
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Patent number: 7189730Abstract: Disclosed are novel A2A adenosine receptor antagonists of the formula: wherein: R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is optionally substituted lower alkyl or optionally substituted cycloalkyl; R3 is hydrogen, halogen, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl; X is —O—, —S—, or —NH—; and Y is optionally substituted alkylene; and the pharmaceutically acceptable salts thereof; which are useful for treating various disease states, for example cardiovascular disorders, including tissue damage due to ischemia, CNS diseases, including Parkinson's disease, depression, and the like.Type: GrantFiled: December 18, 2002Date of Patent: March 13, 2007Assignee: CV Therapeutics, Inc.Inventor: Gloria Cristalli
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Patent number: 7148229Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: February 11, 2004Date of Patent: December 12, 2006Assignee: Hoffman-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
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Patent number: 7148226Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.Type: GrantFiled: November 19, 2003Date of Patent: December 12, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen Borchardt, Javier Gonzalez, Hui Li, Maria Angelica Linton, John Howard Tatlock
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Patent number: 7135475Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: June 12, 2003Date of Patent: November 14, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
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Patent number: 7129239Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. wherein A is an optionally substituted aryl or an optionally substituted heteroaryl; B is an optionally substituted aryl or an optionally substituted heteroaryl; R1 is hydrogen, (C1–C4)alkyl, halo-substituted (C1–C4)alkyl, or (C1–C4)alkoxy; and R4 is as described herein.Type: GrantFiled: October 20, 2003Date of Patent: October 31, 2006Assignee: Pfizer Inc.Inventor: David A. Griffith
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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: 7001910Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.Type: GrantFiled: November 15, 2000Date of Patent: February 21, 2006Assignee: Vita-Invest S.A.Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
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Patent number: 6969720Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: wherein: X=N; V=NH; O; S; or CH2; A=CH2; (CH2)2; (CH2)3; OCH2CH2; or CHCH3; and Y, R1, R2, R3, R4, and n1 are defined herein.Type: GrantFiled: September 11, 2001Date of Patent: November 29, 2005Assignee: AMR Technology, Inc.Inventor: Michael Peter Trova
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Patent number: 6936602Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.Type: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
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Adenine based inhibitors of adenylyl cyclase, pharmaceutical compositions, and method of use thereof
Patent number: 6887880Abstract: The present invention relates to derivatives and analogues of adenine of the formula: wherein L, A, Y and Z are those defined herein. Compounds of the present invention are useful in inhibiting adenylyl cyclase activity. The present invention also relates to a method of preventing and inhibiting a patient's fibroproliferative vasculopathy following vascular injury or a vascular surgical operation which includes administering to the patient, an effective amount of a compound according to the invention subsequent to a vascular injury, or subsequent to a vascular surgical operation, for one to two weeks after the injury or surgical operation, effective to treat or prevent a patient's fibroproliferative vasculopathy such as chronic allograft rejection or vascular restenosis following vascular trauma. The present invention also relates to a method for measuring the inhibition of adenylyl cyclase activity and a method for treating congestive heart failure.Type: GrantFiled: November 20, 2001Date of Patent: May 3, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: Daniel Levy, Charles Marlowe, Kim Kane-Maguire, Robert M. Scarborough -
Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
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Publication number: 20040265376Abstract: Disclosed are orally deliverable pharmaceutical compositions of 2′-deoxy-2′-(fluoromethylene)cytidine (“FMdC”) and methods for providing enhanced bioavailability of FMdC in vivo.Type: ApplicationFiled: April 19, 2004Publication date: December 30, 2004Inventor: Richard E. Jones
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Publication number: 20040254201Abstract: Disclosed are compounds of the formulaType: ApplicationFiled: July 9, 2004Publication date: December 16, 2004Inventors: Bernard Belleau, Pierette Belleau, Dilip M. Dixit, Nghe Nguyen-Ba
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Patent number: 6812232Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: wherein: V= NH; O; S; or CH2; R7 is a heterocycle selected from the group consisting of: thiophene; furan; pyrrole; thiazole; pyrazole; imidazole; isoxazole; isothiazole; and 1,3,4-thiadiazole; and Y, A, R1, R2, R3, R4, and n1 are defined herein.Type: GrantFiled: September 6, 2002Date of Patent: November 2, 2004Assignee: AMR Technology, Inc.Inventor: Michael Peter Trova
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Publication number: 20040198691Abstract: 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: ApplicationFiled: February 2, 2004Publication date: October 7, 2004Inventors: Gloria Cristalli, Venkata Palle, Jeff Zablocki
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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: 20040152708Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.Type: ApplicationFiled: November 7, 2003Publication date: August 5, 2004Inventors: Yong Li, Kurt Sundermann, Li Tang, David Myles
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Patent number: 6767906Abstract: This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R1 is &agr;) —S(═O)k—NR6R7, in which k is 1 or 2, wherein under the proviso that R6 and R7 cannot be simultaneously hydrogen &agr;1) R6, R7 can be identical or different from one another and represent an aliphatic, carbocyclic, heterocyclic, carbocyclic-aliphatic or heterocyclic-aliphatic radical; hydrogen or lower aliphatic acyl; or &agr;2) R6 and R7 together are an alkylene or alkenylene radical having from 3 up to and including 9 C atoms, in which 1-3 C atoms can be replaced by oxygen, sulfur or nitrogen, &bgr;) N-(aryl lower alkyl)carbamoyl, or &ggr;) a radical of the formula —NH—S(═O)i—R8, in which i is 1 or 2, R8 is an aliphatic, carbocyclic or heterocyclic radical; or &dgr;) a radical of the formula —NH—C(═O)—R9, and the other variable substituents are as defined herein.Type: GrantFiled: August 10, 2001Date of Patent: July 27, 2004Assignee: Novartis AGInventors: Patricia Imbach, Hans-Georg Capraro, Jürg Zimmermann, Giorgio Caravatti, Pascal Furet, Wolfgang Karl-Diether Brill
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Publication number: 20040110718Abstract: The present invention comprises novel and known purine and pyrimidine nucleoside derivatives which have been discovered to be active against hepatitis C virus (HCV). The use of these derivatives for the treatment of HCV infection is claimed as are the novel nucleoside derivatives disclosed herein.Type: ApplicationFiled: October 3, 2003Publication date: June 10, 2004Inventors: Rene Devos, Brian William Dymock, Christopher John Hobbs, Wen-Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Publication number: 20040106572Abstract: The present invention concerns the use of an active ingredient selected from the group consisting of agonists of the adenosine receptor system, for inhibiting viral replication in cells. In particular, the invention provides a composition and method for inhibiting viral replication in cells, the method comprising presenting to the cells an effective amount of the active ingredient. According to one embodiment, the adenosine agonist is an A3 receptor agonist (A3RAg). The invention is particularly useful, for although not limited to, inhibiting the replication of HIV virus in human cells.Type: ApplicationFiled: January 15, 2004Publication date: June 3, 2004Inventors: Pnina Fishman, Kamel Khalili
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Publication number: 20040097461Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: June 20, 2003Publication date: May 20, 2004Inventors: Jean-Pierre Sommadossi, Paulo LaColla
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Publication number: 20040097462Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: June 20, 2003Publication date: May 20, 2004Inventors: Jean-Pierre Sommadossi, Paulo LaColla
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Publication number: 20040087540Abstract: The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.Type: ApplicationFiled: April 28, 2003Publication date: May 6, 2004Applicant: Micrologix Biotech Inc.Inventors: Wenqiang Zhou, Yi Jin, Arlene Roland, Radhakrishnan Parameswaran Iyer
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Publication number: 20040072849Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): 1Type: ApplicationFiled: July 17, 2003Publication date: April 15, 2004Inventors: Stuart L. Schreiber, Scott M. Sternson, Jason C. Wong, Christina M. Grozinger, Stephen J. Haggarty, Kathryn M. Koeller
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Publication number: 20040067900Abstract: The invention encompasses nucleoside compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: July 22, 2003Publication date: April 8, 2004Inventors: Richard G. Wilde, Paul D. Kennedy, Neil G. Almstead, Ellen M. Welch, James J. Takasugi, Westley J. Friesen
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Publication number: 20040063659Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.Type: ApplicationFiled: September 18, 2003Publication date: April 1, 2004Applicant: Merrell Pharmaceuticals Inc.Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
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Publication number: 20040058893Abstract: In accordance with the present invention there is provided a nucleoside analogue of formula (I) or (Ia) which is useful as an antiviral agent.Type: ApplicationFiled: February 28, 2003Publication date: March 25, 2004Applicant: BioChem Pharma Inc.Inventor: Nghe Nguyen-Ba
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Publication number: 20040053921Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: October 24, 2002Publication date: March 18, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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Publication number: 20040043959Abstract: The present invention is directed to combination therapies for treating cell proliferative disorders associated with methylthioadenosine phosphorylase (MTAP) deficient cells in a mammal. The combination therapies selectively kill MTAP-deficient cells by administering an inhibitor of de novo inosinate synthesis and administering an anti-toxicity agent, wherein the inhibitors of de novo inosinate synthesis are inhibitors of glycinamide ribonucleotide formyltransferase (“GARFT”) and/or aminoinidazolecarboximide ribonucleotide formyltransferase (“AICARFT”), and the anti-toxicity agent is an MTAP substrate (e.g. methylthioadenosine or “MTA”), a precursor of MTA, an analog of an MTA precursor or a prodrug of an MTAP substrate.Type: ApplicationFiled: February 14, 2003Publication date: March 4, 2004Inventors: Laura A. Bloom, Theodore J. Boritzki, Richard Ogden, Donald Skalitzky, Pei-Pei Kung, Luke Zehnder, Leslie Kuhn, Jerry Jialun Meng
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Publication number: 20040002476Abstract: The invention is a compound, composition, use for and a method of treating Flaviviridae (Hepacivirus, Flavirius, Pestivirus) infections, including BVDV and HCV, or abnormal cellular proliferation, including malignant tumors, in a host including animals, and especially humans, using a &bgr;-D or &bgr;-L nucleoside of general formula (I)-(XX), or their pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: February 13, 2003Publication date: January 1, 2004Inventors: Lieven J. Stuyver, Junxing Shi, Kyoichi A. Watanabe
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Publication number: 20030236216Abstract: The present invention relates to the use of nucleoside derivatives of formula I 1Type: ApplicationFiled: June 11, 2002Publication date: December 25, 2003Inventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Publication number: 20030232830Abstract: &bgr;-lactamases are the most widespread resistance mechanism to &bgr;-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also &bgr;-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.Type: ApplicationFiled: February 19, 2003Publication date: December 18, 2003Inventors: Brian K. Shoichet, Rachel A. Powers
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Publication number: 20030225037Abstract: In accordance with the present invention there is provided a method for treating or preventing a Flaviviridea viral infection in a host comprising administering a therapeutically effective amount of at least one compound of formula (I) or (II) 1Type: ApplicationFiled: March 27, 2003Publication date: December 4, 2003Applicant: BioChem Pharma Inc.Inventor: Richard Storer
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Patent number: 6653312Abstract: Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.Type: GrantFiled: March 16, 2001Date of Patent: November 25, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
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Publication number: 20030199525Abstract: The present application is directed to pyrazolopyrimidine and furopyrimnidine analogs of the formula (I) 1Type: ApplicationFiled: March 21, 2002Publication date: October 23, 2003Inventors: Gavin C. Hirst, Lee D. Arnold, Andrew Burchat, Neil Wishart, Carol K. Wada, Michael R. Michaelides, Zhiqin Ji, Melanie Muckey
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Publication number: 20030191086Abstract: Various substituted nitrogen heterocyclic derivatives and their pharmaceutically acceptable salt derivatives are provided for use as medicaments, and particularly, as antimitotic, anti-viral, anti-cancer, anti-degenerative, immunosuppressive, and anti-microbial drugs or, vaccines. These heterocyclic derivatives can be used as an active agent in a pharmaceutical, as well as a diagnostic utility. To this end, several families of heterocyclic derivatives are provided including pyrrolopyrimidines, pyrazolopyrimidines, purines, and imidazopyridines. In particular, certain tri-substituted and tetra-substituted purines and pyrazolopyrimidines and their deaza analogues are provided for inhibiting cyclin-dependent kinase (“cdk”) proteins, viruses, and immunostimulation.Type: ApplicationFiled: February 5, 2003Publication date: October 9, 2003Applicant: USTAV EXPERIMENTALNI BOTANIKY AV CRInventors: Jan Hanus, Vladimir Krystof, Marian Hajduch, Jaroslav Vesely, Miroslav Strnad
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Publication number: 20030187000Abstract: A polymerase inhibitor has first moiety coupled to a second moiety via an optional linker in which the first moiety binds to an initiation nucleotide binding site of a polymerase and forms at least two hydrogen bonds with an RNA template strand that is associated with the polymerase, and in which the second moiety comprised a compound that binds to a site proximal to the nucleotide binding site of the polymerase and thereby increases the affinity of the polymerase inhibitor to the polymerase.Type: ApplicationFiled: December 27, 2002Publication date: October 2, 2003Inventors: Nanhua Yao, Haoyun An, Todd Appleby, Shahul Nilar, Yili Ding, Zhi Hong
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Publication number: 20030186924Abstract: A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula Ig 1Type: ApplicationFiled: November 16, 2001Publication date: October 2, 2003Applicant: MEDIVIR ABInventors: Xiao-Xiong Zhou, Nils Gunnar Johansson, Horst Wahling, Christian Sund, Hans Wallberg, Lourdes Salvador, Stefan Lindstrom, Christer Sahlberg