Phosphorus Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/243)
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Patent number: 7615542Abstract: The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nuleocoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others.Type: GrantFiled: December 8, 2003Date of Patent: November 10, 2009Assignees: University of Georgia Research Foundation, Inc., Emory UNiversityInventors: Chung K. Chu, Raymond F. Schinazi
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Publication number: 20090270618Abstract: Cidofovir or foscarnet based compounds having an amino acid or dipeptide esters are provided as prodrugs.Type: ApplicationFiled: March 16, 2009Publication date: October 29, 2009Inventors: John Hilfinger, Charles E. McKenna, Boris A. Kashemirov, Chi Pham, Kanokkarn Saejueng, Larryn Peterson
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Publication number: 20090269759Abstract: Nucleotide analogs that can sustain the enzymatic synthesis of double-stranded nucleic acid from a nucleic template are described. The nucleotide analogs include: (i) a base selected from the group consisting of adenine, guanine, cytosine, thymine, uracil and their analogs; (ii) a label attached to the base or analog of the base via a cleavable linker; (iii) a deoxyribose; and (iv) one or more phosphate groups. The linker and/or the label inhibits template directed polymerase incorporation of a further nucleotide substrate onto an extended primer strand. In addition, cleavage of the linker leaves a residue attached to the base which is not present in the natural nucleotide and which does not inhibit extension of the primer strand. The nucleotide analogs can therefore be used as reversible terminators in sequencing by synthesis methods without blocking the 3? hydroxyl group. Methods of sequencing DNA using the substrates are also described.Type: ApplicationFiled: January 16, 2009Publication date: October 29, 2009Applicant: LIFE TECHNOLOGIESInventors: Steven M. Menchen, JR., Barnett Rosenblum, Paul Kenney, Shoeb I. Khan, Zhaochun Ma, Jer-Kang Chen, Joe Lam, Boli Huang
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Publication number: 20090264339Abstract: This invention relates to heterocyclic compounds of the formulas shown in the specification. It also relates to methods for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, and tissue injuries with one of the heterocyclic compounds.Type: ApplicationFiled: November 3, 2008Publication date: October 22, 2009Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Chi-Feng Yen, Cheng-Kung Hu, Chang-Pin Huang, Ying-Huey Huang, Gholam Hossein Hakimelahi, Chi-Hsin Richard King
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Patent number: 7605147Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative represented by the following formula (1): in which represents single bond or double bond, R1, R2, R3, R7 and R8 are defined herein, Y represents —O—, —S—, —CH(Z)-, ?C(Z)-, —N(Z)-, ?N—, or —SiH(Z)-, wherein Z represents hydrogen, hydroxy or halogen, or represents C1-C7-alkyl, C1-C5-alkoxy, allyl, hydroxy-C1-C7-alkyl, C1-C7-aminoalkyl or phenyl, Q represents a group having the following formula: wherein X1, and X2 independently of one another represent hydrogen, amino, hydroxy or halogen, or represent C1-C7-alkyl, C1-C5-alkoxy, allyl, hydroxy-C1-C7-alkyl, phenyl or phenoxy each of which is optionally substituted by nitro or C1-C5-alkoxy, or represent C6-C10-arylthio which is optionally substituted by nitro, amino, C1-C6-alkyl or C1-C4-alkoxy, or represent C6-C12-arylamino, C1-C7-alkylamino, di(C1-C7-alkyl)amino, C3-C6-cycloalkylamino or a structure of wherein n denotes an integer of 1 or 2 and Y1 represents O, CH2 or N—Type: GrantFiled: June 20, 2006Date of Patent: October 20, 2009Assignee: LG Life Sciences Ltd.Inventors: 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, Jong-Ryoo Choi, Jeong-Min Kim, Kee-Yoon Roh
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Publication number: 20090215726Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.Type: ApplicationFiled: March 30, 2006Publication date: August 27, 2009Inventors: Karl Y. Hosterler, James R. Beadle, Hyunah Choo
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Patent number: 7579332Abstract: The invention provides compounds with activity against infectious diseases. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication, of the virus. The compounds of the invention may be useful for treating human patients infected with a human retrovirus, such as human immunodeficiency virus (strains of HIV-l or HIV-2) or human T-cell leukemia virus (HTLV-1 or HTLV-II) which results in acquired immunodeficiency syndrome (AIDS) and/or related diseases.Type: GrantFiled: July 30, 2004Date of Patent: August 25, 2009Assignee: Gilead Sciences, Inc.Inventor: Steven H. Krawczyk
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Publication number: 20090203647Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: January 22, 2009Publication date: August 13, 2009Applicant: DOW AGROSCIENCES LLCInventors: Zoltan L. Benko, Timothy Boebel, Nneka T. Breaux, Kristy Bryan, George E. Davis, Jeffrey B. Epp, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, Bassam S. Nader, W. J. Owen, Mark A. Pobanz, James M. Ruiz, Frisby D. Smith, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, David H. Young
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Patent number: 7553826Abstract: Compounds of Formula I, their preparation and uses are described: wherein: M and V are cis to one another and MH is cytarabine; the 5? oxygen of said cytarabine is attached to the phosphorus; V is 4-pyridyl; and pharmaceutically acceptable prodrugs and salts thereof.Type: GrantFiled: October 18, 2006Date of Patent: June 30, 2009Assignee: Metabasis Therapeutics, Inc.Inventors: Serge Boyer, Mark D. Erion
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Publication number: 20090163712Abstract: Compounds of Formula (I): can be prepared by a multi-step process from compounds of Formula (II): wherein G is Cl, Br or I.Type: ApplicationFiled: December 17, 2008Publication date: June 25, 2009Applicants: Gilead Sciences, Inc., Korea Research Institute of Chemical TechnologyInventors: Hongyan Guo, Stacey Heumann, Ill Young Lee, Michael L. Mitchell, Steven Pfeiffer, Jong Chan Son
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Publication number: 20090156545Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are obtained by attaching the phosphonate nucleoside of interest to alkyloxyalkyl-phosphate or alkyl-phosphate in a phosphate-phosphono anhydride linkage to provide a modified nucleoside phosphonate drug.Type: ApplicationFiled: March 30, 2006Publication date: June 18, 2009Inventors: Karl Y. Hostetler, James R. Beadle, Jacqueline C. Ruiz
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Patent number: 7544672Abstract: Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.Type: GrantFiled: March 29, 2006Date of Patent: June 9, 2009Assignee: Conforma Therapeutics CorporationInventors: Srinivas Rao Kasibhatla, Marco Antonio Biamonte, Jiandong Shi, Marcus F. Boehm
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Publication number: 20090131372Abstract: The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, 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: June 24, 2008Publication date: May 21, 2009Inventors: James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Thorsten Kirschberg, Steven Krawczyk, Hyung-Jung Pyun, William J. Watkins
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Publication number: 20090105279Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: April 23, 2009Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Patent number: 7511051Abstract: Cidofovir-based compounds having an amino acid, dipeptide or tripeptide attached to a cidofovir or cyclic cidofovir framework. The compounds show enhanced oral bioavailability and increased binding to the PepT1 transporter. The present invention also provides compositions and methods for treating virus infections, and a method of preparing cidofovir.Type: GrantFiled: July 1, 2005Date of Patent: March 31, 2009Assignees: University of Southern California, TSRL, Inc.Inventors: Charles E. McKenna, Boris A. Kashemirov, Ulrika Tehler, John Hilfinger
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Publication number: 20080293648Abstract: This invention provides methods, novel formulations and kits to reduce the toxicity of anticancer drugs. Disclosed are therapeutics and treatment methods employing anticancer drags that exhibit a known toxicity, including, for example, adriamycin, campthothecin, and the like, chemically linked to a phosphonoformic acid partial ester resulting in a novel formulation that significantly decreases drug-related toxicity, enhances synergy with other chemotherapeutic drugs and provides increased efficacy against drug-resistant cancers.Type: ApplicationFiled: December 19, 2007Publication date: November 27, 2008Applicant: Saha Pharmaceuticals, Inc.Inventor: Jayanta Saha
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Publication number: 20080286230Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: ApplicationFiled: December 27, 2007Publication date: November 20, 2008Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
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Publication number: 20080255356Abstract: The present invention provides bipyrimidinyl diphosphine compounds of the formula wherein R is optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; R? and R? are independently optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; or an enantiomer thereof; or an enantiomeric mixture thereof. The compounds of the formula (I) are chiral atropisomeric bipyrimidinyl diphosphine compounds and, thus, may be employed as ligands to generate chiral transition metal catalysts which may be applied in a variety of asymmetric reactions, e.g., in palladium catalyzed asymmetric allylic substitution reactions. The compounds of the present invention are easily accessible in high enantiomeric purity according to the methods disclosed herein.Type: ApplicationFiled: June 5, 2008Publication date: October 16, 2008Inventors: Albert Sun-Chi Chan, Gang Chen, Rongwei Guo, Jing Wu
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Patent number: 7435739Abstract: The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.Type: GrantFiled: November 16, 2004Date of Patent: October 14, 2008Inventors: Jinshan Chen, Matthew A. Marx, Susan D. LaGreca, Matthew D. Wessel
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Publication number: 20080207554Abstract: This invention relates to the fields of organic chemistry, pharmaceutical chemistry, biochemistry, molecular biology and medicine. In particular it relates to compounds that activate RNaseL, and to the use of the compounds for treating and/or ameliorating a disease or a condition, such as a viral infection.Type: ApplicationFiled: January 30, 2008Publication date: August 28, 2008Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence M. Blatt, Harri Lonnberg
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Patent number: 7407965Abstract: The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, 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: August 5, 2008Assignee: Gilead Sciences, Inc.Inventors: James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Thorsten Kirschberg, Steven Krawczyk, Hyung-Jung Pyun, William J. Watkins
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Patent number: 7407946Abstract: Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a sulphur atom and optionally containing one or more nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: GrantFiled: December 22, 2003Date of Patent: August 5, 2008Assignee: AstraZeneca ABInventor: Andrew Austen Mortlock
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Publication number: 20080153783Abstract: Pyrimidine I and pyrimidinone II phosphonate compounds and methods for viral inhibition are disclosed. The compounds include at least one phosphonate group covalently attached at any site.Type: ApplicationFiled: November 1, 2005Publication date: June 26, 2008Applicant: GILEAD SCIENCES, INC.Inventors: Haolun Jin, Choung U. Kim
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Patent number: 7312329Abstract: An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to theType: GrantFiled: December 3, 2004Date of Patent: December 25, 2007Assignee: Glenmark Pharmaceuticals LimitedInventors: Narendra Joshi, Shekhar Bhaskar Bhirud, Batchu Chandrasekhar, K. Eswara Rao, Subhash Damle
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Patent number: 7259154Abstract: Compounds of the formula and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.Type: GrantFiled: December 23, 2003Date of Patent: August 21, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Joseph Cox, Tahir Nadeem Majid, Stephanie Daniele Deprets, Shelley Amendola, Iain McFarlane McLay, Christopher Edlin, David John Aldous, Brian Pedgrift, Frank Halley, Michael Edwards, Bernard Baudoin
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Publication number: 20070191606Abstract: The present invention provides novel 2,2-bis(4-hydroxyphenyl)-alkyl onium salts as illustrated by 2,2-bis(4-hydroxyphenyl)-tridecyl(1,2-dimethylimidazolium)bromide and a process for preparation thereof by hydroxyalkylating acetoacetate to the corresponding hyroxyalkylacetoacetate, dealkoxycarbonylating the hydroxyalkyl acetoacetate to ?-hydroxyalkan-2-one and contacting the ?-hydroxyalkan-2-one with phenol in the presence of an acidic catalyst to give 2,2-bis(4-hydroxyphenyl)alkanol, brominating the 2,2-bis(4-hydroxyphenyl)alkanol to 2,2-bis(4-hydroxyphenyl)alkyl bromide, quaternizing 1,2-dimethylimidazole with the 2,2-bis(4-hydroxyphenyl)alkyl bromide to 2,2-bis(4-hydroxyphenyl)alkyl(1,2-dimethylimidazolium)bromide. The products can be used as reactive modifiers for layered phyllosilicates that can be used in the preparation of polymer-nanocomposites, wherein the said polymers are prepared from 2,2-bis(4-hydroxyphenyl)propane as one of the reacting monomers.Type: ApplicationFiled: October 13, 2006Publication date: August 16, 2007Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Shroff Rama Mallikarjuna, Swaminathan Sivaram
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Patent number: 7205404Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I in their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.Type: GrantFiled: March 3, 2000Date of Patent: April 17, 2007Assignee: Metabasis Therapeutics, Inc.Inventors: Mark D. Erion, K. Raja Reddy, Serge H. Boyer
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Patent number: 7176310Abstract: This invention is directed to compound of the following formula (I): wherein R1, R2, R3 and R4 are as described herein. These compounds and pharmaceutical compositions containing the compounds are useful in treating inflammatory disorders in mammals.Type: GrantFiled: April 4, 2003Date of Patent: February 13, 2007Assignee: UCB SAInventors: Theodore A. Baughman, Jim P. Boyce, Ihab S. Darwish, J. Jeffry Howbert, Nathan C. Ihle, Randy W. Jackson, Scott C. Jeffrey, Dean Maeda, Kraig M. Yager
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Patent number: 7164014Abstract: The invention features linker molecules that have at one terminus a amino-protecting group and at the other terminus a phosphorous activating group, typically phosphoramidite. The linker molecules can be used, for example, to produce amino-modified linkers that space an oligonucleotide from a solid support. The invention also features an amino-protected nucleotide that includes an activated phosphorous group such as a phosphoramidite for the production of a 5? amino-modified oligonucleotide. The invention further provides a phthalimido-modified support that can be used to synthesize a polynucleotide that includes an amino group at the 3? terminus.Type: GrantFiled: September 27, 2002Date of Patent: January 16, 2007Assignee: Linden Technologies, Inc.Inventors: Tai-Nang Huang, Ming Shen
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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: 7144866Abstract: Provided is a compound represented by the general formula (I) or a salt thereof: wherein, —XY— represents —CH?CH— and the like, between R2 and the carbon atom at 5-position represents a single bond or a double bond, R1 represents a lower alkyl group, a formyl group, a carboxyl group, a lower alkoxycarbonyl group (wherein a lower alkyl moiety of said lower alkoxycarbonyl group may be substituted with a heterocyclic group) and the like, and R1a represents a hydrogen atom, provided when R1 represents a lower alkoxycarbonyl group and the like, R1a may further represents a lower alkoxycarbonyl group and the like, when between R2 and the carbon atom at 5-position is a single bond, R2 represents a hydroxyl group and the like, and when between R2 and the carbon atom at the 5-position is a double bound, R2 combines with the carbon atom at 5-position to form a hydroxime group (—C(?NOH)) and the like, and R3 represents a hydroxyl group or a tri(lower alkyl)silyloxy group.Type: GrantFiled: August 8, 2001Date of Patent: December 5, 2006Assignee: The Kitasato InstituteInventors: Satoshi Omura, Kenichiro Nagai, Toshiaki Sunazuka
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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: 7115592Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).Type: GrantFiled: June 16, 2004Date of Patent: October 3, 2006Assignees: Institute of Organic Chemistry, Biochemistry of the Academy of Sciences of the Czech RepublicInventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy, Dana Hockova
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Patent number: 7115738Abstract: Compounds are described and claimed comprising general formula: The compounds have substituents as described herein and are useful, e.g., for their ability to bind nucleic acids and thereby effect purifications, probing techniques and gene inhibition.Type: GrantFiled: March 13, 2001Date of Patent: October 3, 2006Assignee: Active MotifInventors: Vladimir Efimov, Joseph Fernandez, Dorothy Archdeacon, John Archdeacon, Oksana Chakhmakhcheva, Alla Buryakova, Mikhail Choob, Kyle Hondorp
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Patent number: 7098341Abstract: The present invention relates to a process for preparing haptens for immunoassay of phosphorothioate pesticides, which comprises the steps of reacting O-methyl(ethyl) dichlorothiophosphate with a phenolic compound to obtain O-methyl(ethyl) O-aryl chlorothiophosphate, and reacting the O-(methyl)ethyl O-aryl chlorothiophosphate thus obtained with aminocarboxylic acid to give desired haptens. In accordance with the present invention, haptens having a structure of O-methyl(ethyl) O-aryl N-(carboxyalkyl)phosphoramidothioate or O-methyl(ethyl) O-aryl N-alkyl-N-(carboxyalkyl)phosphoramidothioate can be simply prepared with a high yield by employing two-step processes in a cost-efficient manner.Type: GrantFiled: June 25, 2004Date of Patent: August 29, 2006Inventors: Yong-Tae Lee, Hye-Sung Lee, Yoo-Jung Kim
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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: 7060290Abstract: Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.Type: GrantFiled: February 16, 2000Date of Patent: June 13, 2006Assignee: Supergen, Inc.Inventors: Bruce H. Morimoto, Peter L. Barker
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Patent number: 7030230Abstract: A process of purifying phosphoramidite precursors useful in inter alia synthesis of oligonucleotides comprises dissolving a crude phosphoramidite in a polar phase, adding a basic compound to the polar phase, adding a portion of water to the polar phase, contacting the polar phase with a first apolar phase to extract impurity into the apolar phase, separating the first apolar phase from the polar phase, adding a second aliquot of water to the polar phase, and contacting the polar phase with a second apolar phase, whereby the phosphoramidite partitions into the second apolar phase.Type: GrantFiled: October 25, 2002Date of Patent: April 18, 2006Assignee: ISIS Pharmaceuticals, Inc.Inventors: Bruce Ross, Quanlai Song
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Patent number: 7030103Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: October 8, 2002Date of Patent: April 18, 2006Assignee: Methylgene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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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: 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: 6919322Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: March 7, 2001Date of Patent: July 19, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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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: 6908924Abstract: The present invention is directed to a compound, method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N4-acylcytosine-1,3-dioxolane and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.Type: GrantFiled: December 16, 2002Date of Patent: June 21, 2005Assignee: Pharmasset, Inc.Inventors: Kyoichi A. Watanabe, Junxing Shi, Michael J. Otto
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Patent number: 6878697Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC, RD, w, x, y, and z are as defined herein, and to their preparation and use.Type: GrantFiled: June 21, 2002Date of Patent: April 12, 2005Assignee: Ariad Pharmaceuticals, Inc.Inventors: Chester A. Metcalf, III, William C. Shakespeare, Tomi K. Sawyer, Yihan Wang, Regine Bohacek
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Patent number: 6872711Abstract: The present invention relates to novel ?-substituted-?-aminoethylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.Type: GrantFiled: October 22, 2001Date of Patent: March 29, 2005Assignee: Ilex Oncology Research S.A.Inventors: Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
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Patent number: 6858393Abstract: The invention relates to acyclic chain terminator nucleotide analogs. More particularly, the invention relates to phosphonomethoxyethyl nucleotide analogs and detectably labeled versions thereof, especially fluorescently labeled versions thereof. The invention further relates to the use of chain terminating phosphonomethoxyethyl nucleotide analogs in methods of synthesizing a polynucleotide, labeling a polynucleotide, determining polynucleotide sequence information, and kits therefor.Type: GrantFiled: March 13, 2002Date of Patent: February 22, 2005Assignee: Stratagene CaliforniaInventors: Jack Dewayne Anderson, Jeffrey Carl Braman
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Patent number: 6844437Abstract: The invention concerns a process for the manufacture of tert-butyl (E)-(6-[2-4-(4-flourophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl)-(4R,6S)-2,2-dimethyl[1,3]-dioxan-4-yl)acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.Type: GrantFiled: February 15, 2000Date of Patent: January 18, 2005Assignees: Astrazeneca AB, Shionogi & Co. Ltd.Inventors: Nigel P Taylor, Loius J Diorazio, Haruo Koike, Mikio Kabaki
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Publication number: 20040260091Abstract: The invention relates to a process for the manufacture of ligands capable of forming metal complexes and such complexes; novel ligands with new backbones, complexes thereof with transition metals, the use of complexes of said ligands with transition metals as catalysts, as well as novel intermediates for the manufacture of said ligands. The ligand complexes are useful in stereoselective synthesis, especially hydrogenation, of various organic molecules. Especially, the process according to the invention is directed to the synthesis of compounds of the formulae IA and IIA, wherein the substituents have the meanings given in the description, and to novel compounds of these formulae as ligands.Type: ApplicationFiled: March 31, 2004Publication date: December 23, 2004Inventor: Ulrich Berens
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Patent number: 6833364Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.Type: GrantFiled: March 26, 2001Date of Patent: December 21, 2004Assignee: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Elke Stahl, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky