Nonshared Hetero Atoms In At Least Two Rings Of The Polycyclo Ring System Patents (Class 514/81)
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Publication number: 20080139509Abstract: Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexylcarbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient route to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium pancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray crystallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.Type: ApplicationFiled: February 4, 2008Publication date: June 12, 2008Inventors: George R. Pettit, Noeleen Melody
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Publication number: 20080113929Abstract: Compositions and methods are provided for enhancing delivery of therapeutic agents. More specifically, compositions and methods are provided for improving antigen delivery to antigen-presenting cells. Conjugates between abasic oligonucleotides and antigen are provided, along with methods for their use in vaccination and in the treatment of cancer, infection, and allergy and asthma. Also provided are conjugates between abasic oligonucleotides and various immunostimulatory nucleic acids, including CpG oligonucleotides, as well as methods of use thereof. Also provided are conjugates between abasic oligonucleotides and various other agonists and antagonists of immunostimulation, as well as methods of use thereof.Type: ApplicationFiled: June 8, 2005Publication date: May 15, 2008Applicant: Coley Pharmaceutical GmbHInventors: Grayson B. Lipford, Alexandra Forsbach, Eugen Uhlmann, Hermann Wagner
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Patent number: 7368437Abstract: Methods and compounds for inhibiting the enzymes adenosine monophosphate deaminase or adenoside deaminase are provided. Such methods and compounds are useful in agriculture, horticulture and/or pharmacology as, for example, active compounds for crop protection or pharmaceuticals for humans or animals.Type: GrantFiled: March 16, 2000Date of Patent: May 6, 2008Assignee: Bayer CropScience AGInventors: Guido Bojack, Stephen Lindell, Christopher Rosinger, Philip Dudfield, Christopher G. Earnshaw
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Patent number: 7358250Abstract: Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of the substituents are provided herein.Type: GrantFiled: June 29, 2005Date of Patent: April 15, 2008Assignee: Amgen Inc.Inventors: Christopher N. Farthing, Paul Faulder, Alexander D. Frenkel, Martin J. Harrison, Xianyun Jiao, Frank Kayser, David J. Kopecky, Jinqian Liu, Sarah E. Lively, Rajiv Sharma, Stephen J. Shuttleworth
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Publication number: 20080076740Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 27, 2006Publication date: March 27, 2008Inventors: Zhenhong R. Cai, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Samuel E. Metobo, Michael R. Mish, Richard M. Pastor
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Patent number: 7323449Abstract: The present invention provides thionucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such thionucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the thionucleoside compounds of the present invention.Type: GrantFiled: July 18, 2003Date of Patent: January 29, 2008Assignees: Merck & Co., Inc., Isis Pharmaceuticals, Inc.Inventors: David B. Olsen, Balkrishen Bhat, Phillip Dan Cook
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Publication number: 20070299054Abstract: The present invention relates to an improved oral pharmaceutical composition containing at least one poorly water soluble active agent, the active agent containing at least one of an endothelin conversion enzyme (ECE) inhibitor and a neutral endopeptidase (NEP) inhibitor in an amount greater than 10% w/w of the composition, and an alkali system comprising a mixture of at least two alkaline compounds in a ratio of from 1:20 to 20:1. The present invention also relates to an improved oral pharmaceutical composition containing, SLV-306 or at least one pharmaceutically acceptable salt, ester, hydrate, solvate, isomer or derivative thereof, as an active agent, and an alkali system in an amount greater than 10% w/w of the composition comprising a mixture of at least two alkaline compounds and optionally at least one pharmaceutically acceptable excipient. The present invention further relates to a process for preparation of such improved compositions and methods for treatment using such compositions.Type: ApplicationFiled: June 21, 2007Publication date: December 27, 2007Inventors: Rajesh Jain, Kour C. Jindal, Amarjit Singh, Munish Talwar, Henricus R.M. Gorissen
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Patent number: 7312204Abstract: The present invention relates to insecticidal mixtures of chloronicotinyl insecticides of the formula (I) in which R1 represents C1-C5-alkyl, R2 represents hydrogen or C1-C5-alkyl or R1 and R2 together represent —CH2—CH2—; —CH2—CH2—CH2— or X represents an NH group, NCH3 group or represents sulphur, Y represents nitrogen or a CH group and Z represents cyano or nitro, with one or more of the synergists mentioned in the description.Type: GrantFiled: June 28, 2002Date of Patent: December 25, 2007Assignee: Bayer AktiengesellschaftInventors: Christoph Erdelen, Wolfgang Krämer, Kai-Uwe Brüggen
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Patent number: 7300924Abstract: The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: April 26, 2004Date of Patent: November 27, 2007Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Aesop Cho, William J. Watkins
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Patent number: 7285543Abstract: Novel purine compounds of Formula 1, pharmaceutically acceptable prodrugs and salts thereof, and their use as fructose 1,6-bisphosphatase inhibitors.Type: GrantFiled: April 7, 2005Date of Patent: October 23, 2007Assignee: Metabasis Therapeutics, Inc.Inventors: Qun Dang, Mark D. Erion, M. Rami Reddy, Edward D. Robinson, Srinivas Rao Kasibhatla, K. Raja Reddy
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Publication number: 20070197478Abstract: The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.Type: ApplicationFiled: February 16, 2007Publication date: August 23, 2007Inventors: Peter Jones, David Pryde, Thien Duc Tran
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Publication number: 20070191313Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.Type: ApplicationFiled: February 15, 2007Publication date: August 16, 2007Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
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Patent number: 7253154Abstract: The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which may have a substituent or the like; R2 is halogen, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur, in which R11 is hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CR12 or nitrogen, in which R12 has the same meaning as R3 above, and a xanthine oxidase inhibitor containing the compound as an active ingredient.Type: GrantFiled: November 14, 2002Date of Patent: August 7, 2007Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shinichi Yoshida, Atsushi Tendo, Kunio Kobayashi, Nobutaka Mochiduki, Tomio Yamakawa, Yoriko Shinohara
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Patent number: 7238679Abstract: Compounds of the following formula are disclosed: wherein RB is a substituted or unsubstituted aryl or heteroaryl moiety; at least one of RU and RL is a phosphorus-containing moiety, J, and the other of RU and RL is independently chosen from H; halogen; —CN; —NO2; -J; —SO2R; —SO2NRR?; or —ZRJ, wherein each occurrence of Z is independently —O—, —S— or —NR— and each occurrence of RJ is independently —R, —COR, —COOR or —CONRR?.Type: GrantFiled: December 23, 2003Date of Patent: July 3, 2007Assignee: Ariad Pharmaceuticals, Inc.Inventors: Terence P. Keenan, William C. Shakespeare
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Patent number: 7235538Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3, R6, R7, R9, and R10 are defined herein. The present invention also relates to pharmaceutical compositions comprising the compounds of formula I and the use of the compounds for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type-2 diabetes and obesity.Type: GrantFiled: July 17, 2003Date of Patent: June 26, 2007Assignee: Novo Nordisk A/SInventors: Anders Bendtz Kanstrup, Lise Brown Christiansen, Jane Marie Lundbeck, Christian K. Sams, Marit Kristiansen
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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: 7214668Abstract: Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine; V is selected from a group consisting of phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3-thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6; R6 is selected from the group consisting of C1-C3 alkyl, and CF3; and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 12, 2003Date of Patent: May 8, 2007Assignee: Metabasis Therapeutics, Inc.Inventors: K. Raja Reddy, Mark D. Erion, Michael C. Matelich, Joseph J. Kopcho
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Patent number: 7183268Abstract: Compounds which are active against viruses have the following Formulas: wherein B is 2-aminopurine-9-yl, which may be unsubstituted or substituted in the 6 position with NHR1, OR2, or SR3; R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, and C4-18 cycloalkyl, any of which may be optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl; R2 is selected from the group consisting of C2-18 alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl, and aryl; and R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl.Type: GrantFiled: September 15, 2004Date of Patent: February 27, 2007Assignees: Wayne State University, The Regents of the University of MichiganInventors: Jiri Zemlicka, John C. Drach, Xinchao Chen
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Patent number: 7157448Abstract: The present invention relates to a nucleoside phosphonate derivative represented by formula (1): pharmaceutically acceptable salts, and stereoisomers. This nucleoside phosphonate derivative is useful as an antiviral agent, particularly, against hepatitis B virus. Also disclosed are processes for the preparation of the nucleoside phosphonate derivative. Also disclosed are methods treating hepatitis B by administering a nucleoside phosphonate derivative of formula (1).Type: GrantFiled: January 18, 2002Date of Patent: January 2, 2007Assignee: LG Life Sciences Ltd.Inventors: Jong-Ryoo Choi, Jeong-Min Kim, Kee-Yoon Roh, Dong-Gyu Cho, Jae-Hong Lim, Jae-Taeg Hwang, Woo-Young Cho, Hyun-Sook Jang, Chang-Ho Lee, Tae-Saeng Choi, Chung-Mi Kim, Yong-Zu Kim, Tae-Kyun Kim, Seung-Joo Cho, Gyoung-Won Kim
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Patent number: 7151100Abstract: The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.Type: GrantFiled: August 9, 2000Date of Patent: December 19, 2006Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Lorenzo M. Leoni, Howard B. Cottam
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Patent number: 7148210Abstract: The invention provides a drug combination for the treatment of diseases associated with bone metastasis. The combination provides adenosine or a derivative thereof, a bisphosphonate, and a targeting agent(s) to decrease the signs or symptoms associated with such diseases.Type: GrantFiled: October 15, 2003Date of Patent: December 12, 2006Assignee: Trustees of Dartmouth CollegeInventor: Edward H. Abraham
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Patent number: 7129261Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.Type: GrantFiled: May 31, 2002Date of Patent: October 31, 2006Assignee: Medarex, Inc.Inventors: Howard P. Ng, Danny P.C. McGee, Oliver L. Saunders, Valeri Martichonok, Guoxian Wu, Zhihong Li, Geoffrey T. Yarranton
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Patent number: 7129227Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpesviruses, is disclosed. The method comprises administering to a subject in need of such treatment an infection-combating amount of a phospholipid or phospholipid derivative.Type: GrantFiled: October 4, 1999Date of Patent: October 31, 2006Assignees: Wake Forest University, University of North Carolina at Chapel HillInventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
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Patent number: 7115590Abstract: The present invention relates to phosphoramidate, and phosphate esters of (1R,cis)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1nethanol, processes for their preparation, and their use in treating viral infections.Type: GrantFiled: February 10, 2000Date of Patent: October 3, 2006Assignee: University College Cardiff Consultants LimitedInventors: Susan Mary Daluge, Christopher McGuigan
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Patent number: 7115589Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use. In these compounds, RB is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety which comprises one or more phosphorus-containing moieties.Type: GrantFiled: December 18, 2000Date of Patent: October 3, 2006Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Manfred Weigele, Tomi K. Sawyer, Regine Bohacek, William C. Shakespeare, Rajeswari Sundaramoorthi, Yihan Wang, David C. Dalgarno, Chester A. Metcalf, III
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Patent number: 7109165Abstract: This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids and antisense nucleic acid molecules.Type: GrantFiled: May 17, 2002Date of Patent: September 19, 2006Assignee: Sirna Therapeutics, Inc.Inventors: Jasenka Matulic-Adamic, Leonid Beigelman
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Patent number: 7098196Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.Type: GrantFiled: October 13, 2000Date of Patent: August 29, 2006Assignee: Johns Hopkins University School of MedicineInventors: Philip A. Beachy, James K. Chen, Anssi J. Taipale
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Patent number: 7098216Abstract: The invention provides derivatives of thiazolo[4,5-d1]pyrimidine and their use as inhibitors of proinflammatory cytokines.Type: GrantFiled: September 28, 2004Date of Patent: August 29, 2006Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Howard B. Cottam, Lynn Deng
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Patent number: 7087589Abstract: The present invention provides novel nucleoside and nucleotide derivatives that are useful agonists or antagonists of P1 or P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl group. The adenine or uracil is bonded to the constrained cycloakyl group. The compounds of the present invention are useful in the treatment or prevention of various diseases including airway diseases (through A2B, A3, P2Y2 receptors), cancer (through A3, P2 receptors), cardiac arrhythmias (through A1 receptors), cardiac ischemia (through A1, A3 receptors), epilepsy (through A1, P2X receptors), and Huntington's Disease (through A2A receptors).Type: GrantFiled: January 12, 2001Date of Patent: August 8, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Victor E. Marquez
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Patent number: 7071176Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.Type: GrantFiled: December 1, 2003Date of Patent: July 4, 2006Assignee: Parker Hughes InstituteInventors: Faith M. Uckun, Rakesh Vig
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Patent number: 7053070Abstract: Disclosed are compounds of the formula wherein R2, R5, R6, R7, and R8 are as defined herein. These compounds and their pharmaceutical compositions are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cdks and growth factor-mediated kinases.Type: GrantFiled: January 23, 2001Date of Patent: May 30, 2006Assignee: Warner-Lambert CompanyInventors: Richard John Booth, Ellen Myra Dobrusin, Vara Prasad Venkata Nagendra Josyula, Dennis Joseph Mc Namara, Peter Laurence Toogood
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Patent number: 7045525Abstract: A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.Type: GrantFiled: April 23, 1996Date of Patent: May 16, 2006Assignee: Novartis AGInventors: Richard Anthony Vere Hodge, Raymond F Schinazi
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Patent number: 7041666Abstract: Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, —C(?CH2)CH3, —C?C—CH3, —CH?C(CH3)2, or —CH?CH—CH3; R2 is —W—X, —NR19(CH2)m—W—X, and —NR19CH(CH3)—W—X, or R2 is alkyl, alkenyl and —NR18R19, each optionally substituted —W—X; R3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R18 is a bond, —CH(OH)—, —CH(CH3)—, —C(CH3)n—, —(CH2)n—or —O(CH2)n—; W is aryl or heteroaryl, each optionally substituted; X is H, NH2, or substituted amino, or X is —R18—Y-Z; and n, R19, Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.Type: GrantFiled: November 26, 2002Date of Patent: May 9, 2006Assignee: Schering CorporationInventors: Julius J. Matasi, John P. Caldwell, Deen Tulshian, Lisa S. Silverman, Bernard R. Neustadt
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Patent number: 7022686Abstract: Compounds of Formula I and II are disclosed as antagonists of subtype A1 adenosine receptors. These compounds are useful for treatment of various diseases and disorders, including systemic hypertension, renal failure, diabetes, asthma, an edematous condition, congestive heart failure, and renal dysfunction.Type: GrantFiled: May 27, 2003Date of Patent: April 4, 2006Assignee: Biogen Idec Inc.Inventors: Ko-Chung Lin, Chi Vu
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Patent number: 7018989Abstract: Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1 is O, NR3, S, CR3R4, CR3W1 or CW1W2, X2 and X6 are a bond or X6 is CH2 and X2 is O, NR3, S, CR3R4, CR3W1 or CW1W2, R3 and R4 are H, alkyl or phenyl, groups, W1 and W2 are heteroatoms, X3 is alkylene, X4 is oxygen or CH2, X5 is a bond or CH2, Z is O, NR5, S, alkyl or phenyl, R5 is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR6, S, CR6R7, CR6W3 or CW3W4, R6 and R7 are H, alkyl or phenyl, and W3 and W4 are hetero atoms, T1 and T2 are H or CH2R8, R8 is H, OH or F, or T1 and T2 together are —CH?CH— or —C(R9)(R10)C(R11)(R12)—, R9 is H, halogeno, CN, NH2, CO-alkyl, or alkyl, R10, R11, and R12 are H, N3, halogen, CN, NH2, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV. Particularly preferred are thymine and adenine derivatives of amino acid phenoxyphosphoroamidates.Type: GrantFiled: August 12, 2002Date of Patent: March 28, 2006Assignee: University College Cardiff Consultants, LTDInventors: Christopher McGuigan, Jan Balzarini
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Patent number: 6969707Abstract: This invention provides a novel class of substituted macrocyclic metallic complexes. The complexes are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described.Type: GrantFiled: July 29, 2002Date of Patent: November 29, 2005Assignee: Trustees of Princeton UniversityInventors: John T. Groves, Suzanne M. Moeller
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Patent number: 6967193Abstract: Novel purine compounds of the Formula 1, pharmacuetically acceptable prodrugs and salts thereof, and their use as fructose 1,6-bisphosphatase inhibitorsType: GrantFiled: July 7, 2003Date of Patent: November 22, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Qun Dang, Mark D. Erion, M. Rami Reddy, Edward D. Robinson, Srinivas Rao Kasibhatla, K. Raja Reddy
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Patent number: 6960572Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC, RD, RE, p, q and X are as defined herein, and to their preparation and use.Type: GrantFiled: June 21, 2002Date of Patent: November 1, 2005Assignee: Ariad Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III, Yihan Wang, Regine Bohacek
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Patent number: 6946450Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.Type: GrantFiled: May 13, 2003Date of Patent: September 20, 2005Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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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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Patent number: 6930101Abstract: The invention provides derivatives of thiazolo[4,5-dl]pyrimidine and their use as inhibitors of proinflammatory cytokines.Type: GrantFiled: May 17, 1999Date of Patent: August 16, 2005Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Howard B. Cottam, Lynn Deng
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Patent number: 6914052Abstract: The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity toward the host cells. In particular, the compounds according to the present invention show potent inhibition of the replication of the human immunodeficiency virus (HIV), while remaining substantially inert toward host cell DNA. Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of retroviruses, particularly HIV. The compounds of the invention comprise a (2,3?-dideoxy-?-ribofuranosyl) ring coupled to a heterocyclic nucleobase that lacks an “O2 carbonyl”, that enables them to selectively react with and inhibit viral reverse transcriptase, while remaining substantially unreactive toward human DNA polymerases.Type: GrantFiled: March 13, 2002Date of Patent: July 5, 2005Assignee: The Trustees of Boston CollegeInventors: Larry W. McLaughlin, Andrew W. Fraley, DongLi Chen, Tao Lan
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Patent number: 6900315Abstract: The present invention relates to novel compounds, compositions and methods for inhibiting the growth, elaboration and/or replication of HIV in human patients and to the prevention and treatment of human acquired immunodeficiency syndrome (AIDS) and other diseases caused by retroviral infection. More particularly, in preferred aspects, the present invention provides a method for the use of novel prodrug forms of 9-(2,3-Dideoxy-?-D-glycero-pent-2-enofuranosyl) guanine (d4G) for the prevention and treatment of both wild type and drug-resistant Human Immunodeficiency Virus (HIV), the causative pathogen of AIDS. Compounds according to the present invention are based upon the chemical formula: where X is OCH3, N3, NHCH3, N(CH3)2 or an aminocyclopropyl group; R1 is H or a C1 to C20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; and R2 is H or a C1 to C20 acyl or alkyl group.Type: GrantFiled: February 5, 2002Date of Patent: May 31, 2005Assignees: Yale University, University of Georgia Research Foundation, Inc.Inventors: Karen S. Anderson, Adrian Staffin Ray, Chung K. Chu, Yang Zhenjun
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Patent number: 6897201Abstract: The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a nucleoside 5?-pyrophosphate pyranoside or analogue, which is defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as found in glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with another therapeutic agent or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure. The present invention also provides a novel composition comprising a nucleoside 5?-pyrophosphate pyranoside or analogues.Type: GrantFiled: February 27, 2002Date of Patent: May 24, 2005Assignee: Inspire Pharmaceuticals, Inc.Inventors: Jose L. Boyer, Benjamin R. Yerxa, Robert Plourde, Jr., Edward G. Brown
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Patent number: 6841559Abstract: Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.Type: GrantFiled: November 20, 2000Date of Patent: January 11, 2005Assignee: Washington University of St. LouisInventors: Frederic Almqvist, Hans Emtenas, Scott J. Hultgren, Jerome S. Pinkner
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Publication number: 20040242532Abstract: A method and pharmaceutical composition for inhibiting infections of pathogenic microorganisms by inhibiting the production of ADP-glucose, particularly by inhibiting the activity of ADP-glucose pyrophosphorylase or glycogen synthase.Type: ApplicationFiled: June 14, 2004Publication date: December 2, 2004Inventor: Christopher Meyer
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Publication number: 20040242465Abstract: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.Type: ApplicationFiled: June 29, 2004Publication date: December 2, 2004Inventors: Norbert W. Bischofberger, Robert J. Jones, Murty N. Arimilli, Kuei-Ying Lin, Michael S. Louie, Lawrence R. McGee, Ernest J. Prisbe, William A. Lee, Kenneth C. Cundy
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Patent number: 6825180Abstract: Novel pyridopyrimidine-based compounds are found to be useful for the treatment or prevention of symptoms or manifestations associated with diseases or disorders affected by cytokine intracellular signaling.Type: GrantFiled: May 18, 2001Date of Patent: November 30, 2004Assignee: Cell Therapeutics, Inc.Inventors: Marc J. McKennon, J. Peter Klein, Michael Coon
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Publication number: 20040229839Abstract: Provided are compounds represented by: 1Type: ApplicationFiled: May 14, 2004Publication date: November 18, 2004Applicant: BIOCRYST PHARMACEUTICALS, INC.Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan
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Patent number: RE39264Abstract: The invention relates to pharmaceutical compositions for topical administration comprising a topically acceptable antiviral substance and an antiinflammatory glucocorticoid in a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the prophylactic and curative treatment of herpesvirus infections in mammals including man. The invention also relates to the use of a combination of a topically acceptable antiviral substance and an antiinflammatory glucocorticoid for the manufacture of a medicament for said prophylactic and curative treatment.Type: GrantFiled: February 2, 1996Date of Patent: September 5, 2006Assignee: Medivir ABInventors: Johan Harmenberg, Ann Harriet Margareta Kristofferson