Polycyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/244)
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Publication number: 20110130364Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.Type: ApplicationFiled: November 22, 2010Publication date: June 2, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Atsuro NAKAZATO, Taketoshi Okubo, Dai Nozawa, Mikako Yamaguchi, Tomoko Tamita, Ludo E.J. Kennis, Marcel F.L. De Bruyn, Jean-Pierre A.M. Bongartz, Frans M.A. Van Den Keybus, Yves E.M. Van Roosbroeck, Marcel G.M. Luyckx, Robert J.M. Hendrickx
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Publication number: 20110112292Abstract: Crystalline Form C of tenofovir disoproxil, salts thereof and a process for its preparation. The process involves adding a solution comprising tenofovir disoproxil and an organic solvent to salt-saturated water, whereby the crystalline Form C of tenofovir disoproxil precipitates. The crystalline Form C of tenofovir disoproxil may be converted to a salt thereof. There is also provided a process for purifying a crude product comprising tenofovir monoisoproxil and tenofovir disoproxil.Type: ApplicationFiled: July 30, 2008Publication date: May 12, 2011Applicant: CIPLA LIMITEDInventors: Manjinder Singh Phull, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
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Publication number: 20110105434Abstract: Anti-herpetic material such as 2-amino purine derivatives to prevent or treat autoimmune disease or a disease originating from an abnormal functioning of the sympathetic chain in a human subject. The disease is often of a tissue or organ associated with decreased blood flow to the tissue or organ (correlated with hypertonicity of the vessels feeding the tissue or organ). The treatment reduces inflammation, scarring, destruction, and pain in the tissue or organ affected and returns the tissue or organ to nearly normal functioning, while showing none of the side effects of previous treatments. Prolonged use of the anti-herpetic compounds reduces prodrome, vesicle formation and viral shedding. The anti-herpetic compounds may be administered alone or in combination with a compound that reduces the rate of renal excretion of the anti-herpetic compound. The anti-herpetic compounds are particularly useful when administered at a level equivalent in activity to 250 mg/kg famciclovir per day.Type: ApplicationFiled: November 20, 2008Publication date: May 5, 2011Inventor: Ray W. Exley
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Patent number: 7935817Abstract: Provided are a cocrystal of Adefovir dipivoxil and nicotinamide as well as a cocrystal of Adefovir dipivoxil and salicylamide cocrystal and processes for the preparation thereof.Type: GrantFiled: March 31, 2008Date of Patent: May 3, 2011Assignee: Apotex Pharmachem Inc.Inventors: Peter Garth Blazecka, Daqing Che, Cameron L. McPhail, Allan W. Rey
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Patent number: 7932259Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.Type: GrantFiled: April 21, 2008Date of Patent: April 26, 2011Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Dai Nozawa, Mikako Yamaguchi, Tomoko Tamita, Ludo E. J. Kennis, Marcel F. L. De Bruyn, Jean-Pierre A. M. Bongartz, Frans M. A. Van Den Keybus, Yves E. M. Van Roosbroeck, Marcel G. M. Luyckx, Robert J. M. Hendrickx
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Publication number: 20110071115Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: MUSTAPHA HADDACH, DAVID M. RYCKMAN, NICHOLAS RAFFAELE
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Publication number: 20110065671Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Joel M. Harris, Santhosh Francis, Bernard R. Neustadt, Craig D. Boyle, Hong Liu, Jinsong Hao, Andrew Starnford, Samuel Chackalamannil, William J. Greenlee
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Publication number: 20110059921Abstract: The invention relates to (among other things) oligomer-nitrogenous base conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over unconjugated nitrogenous base compounds.Type: ApplicationFiled: March 27, 2009Publication date: March 10, 2011Applicant: Ektar TherapeuticsInventor: Jennifer Riggs-Sauthier
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Patent number: 7871991Abstract: 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: GrantFiled: July 26, 2005Date of Patent: January 18, 2011Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
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Publication number: 20110009366Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.Type: ApplicationFiled: April 23, 2010Publication date: January 13, 2011Applicant: AVEXA LIMITEDInventors: Eric Dale Jones, Jonathan Alan Victor Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Vandegraff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherinie Macfarlane
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Publication number: 20110009368Abstract: The Present Invention Provides Tenofovir Disoproxil Succinate, Tenofovir Disoproxil L-Tartrate, Tenofovir Disoproxil oxalate, Tenofovir disoproxil saccharate, Tenofovir disoproxil citrate, Tenofovir disoproxil salicylate and various solid forms thereof, methods for the preparation thereof and their use in pharmaceutical applications, in particular in anti-HIV medicaments. The forms of Tenofovir disoproxil can be used in combination with other anti-HIV medicaments such as Efavirenz and Emtricitabine.Type: ApplicationFiled: December 11, 2008Publication date: January 13, 2011Applicant: ULTIMORPHIX TECHNOLOGIES B.V.Inventor: Evanthia Dova
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Publication number: 20100298256Abstract: Lipid-modified phosphodiester nucleoside prodrugs are described herein. The prodrugs can be used to treat viral infections and cancer.Type: ApplicationFiled: December 23, 2008Publication date: November 25, 2010Inventors: Steven Dong, Mel C. Schroeder
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Publication number: 20100292470Abstract: Adefovir Dipivoxil monohydrate crystalline is disclosed.Type: ApplicationFiled: July 31, 2008Publication date: November 18, 2010Applicant: NITEC PHARMA AGInventor: Stefania GALIMI
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Patent number: 7820631Abstract: A nucleoside analogue compound is provided which has a six-membered aromatic ring system, the aromatic ring system being substituted in the para position with an unbranched unsubstituted alkyl or alkoxy moiety, wherein the alkyl or alkoxy moiety, in total, has from 3 to 8 carbon atoms. This compound shows anti-vira1 activity, for example with respect to varicella zoster virus and can thus be used in therapeutic methods for the prophylaxis and treatment of viral infections such as varicella zoster virus.Type: GrantFiled: April 12, 2001Date of Patent: October 26, 2010Assignees: Rega Foundation, University College Cardiff Consultants LimitedInventors: Christopher McGuigan, Jan Balzarini
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Publication number: 20100261677Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: September 4, 2008Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20100261231Abstract: Novel cap analogs which are easily synthesized, resulting in high levels of capping efficiency and transcription and improved translation efficiencies are provided. Such caps are methylated at the N7 position of one or both guanosines of the dinucleotide cap as well as at the 3? position on the ribose ring. Substituent groups on the ribose ring also result in the cap being incorporated in the forward orientation. Also provided are methods useful for preparing capped analogs and using mRNA species containing such analogs are also contemplated herein, as well as kits containing the novel cap analogs.Type: ApplicationFiled: July 10, 2007Publication date: October 14, 2010Applicant: LIFE TECHNOLOGIES CORPORATION, a Delaware CorporationInventors: Anilkumar R. Kore, Shanmugasundaram Muthian
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Publication number: 20100249067Abstract: The invention relates to compounds of Formula (I), a polymorph, an enantiomer, a stereoisomer, a solvate, an N-oxide derivative, or a pharmaceutically acceptable salt thereof: Formula (I), which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.Type: ApplicationFiled: January 30, 2008Publication date: September 30, 2010Applicant: Biogen Idec MA Inc.Inventors: Srinivas Rao Kasibhatla, Kevin Hong, Lin Zhang, Marcus F. Boehm, Junhua Fan, Jean-Yves LeBrazidec
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Publication number: 20100249068Abstract: Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Guangyi Wang
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Publication number: 20100240613Abstract: The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.Type: ApplicationFiled: November 25, 2009Publication date: September 23, 2010Applicant: Japan Tobacco Inc.Inventors: Hisashi Kawasaki, Hiroyuki Abe, Kazuhide Hayakawa, Tetsuya Iida, Shinichi Kikuchi, Takayuki Yamaguchi, Toyomichi Nanayama, Hironori Kurachi, Masahiro Tamaru, Yoshikazu Hori, Mitsuru Takahashi, Takayuki Yoshida, Toshiyuki Sakai
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Publication number: 20100210598Abstract: Provided herein are small molecule conjugates that are agonists or antagonists of one or more toll-like receptors.Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Applicant: Regents of the University of California, San DiegoInventors: Dennis A. Carson, Howard B. Cottam, Tomoko Hayashi, Michael Chan
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Publication number: 20100204182Abstract: The present invention provides ectonucleotidase inhibitors represented by the following formula, including ecto-nucleotide triphosphate diphosphohydrolase (NTPDase) inhibitors and ecto-5?-nucleotidase (ecto-5?-NT) inhibitors, namely nucleotide mimetics as selective NTPDase or ecto-5?-NT inhibitors. It also provides methods for preparations of said compounds. Furthermore provided are pharmaceutical and diagnostic compositions comprising said compounds, and the use of said compounds in a medicament for treating diseases associated with ectonucleotidase activity and/or P1 or P2 receptors.Type: ApplicationFiled: May 24, 2007Publication date: August 12, 2010Applicant: RHEINISCHE FRIEDRICH-WILHELMS-UNIVERSITAT BONNInventors: Christa E. Müller, Andreas Brunschweiger, Jamshed Iqbal
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Publication number: 20100173870Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: ApplicationFiled: February 5, 2010Publication date: July 8, 2010Inventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Publication number: 20100168063Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.Type: ApplicationFiled: December 21, 2007Publication date: July 1, 2010Applicant: Avexa LimitedInventors: Eric Dale Jones, Jonathan Alan Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Vandegraff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherine MacFarlane
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Patent number: 7737127Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.Type: GrantFiled: March 26, 2007Date of Patent: June 15, 2010Assignee: University of Virginia Patent FoundationInventors: Joel M. Linden, Jayson M. Rieger, Timothy L. Macdonald, Gail W. Sullivan, Lauren Jean Murphree, Robert Alan Figler
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Patent number: 7737273Abstract: The present invention provides a novel process for the preparation of acyclic phosphonate nucleotide analogs using novel intermediates. Thus, for example, (R)-9-(2-phosphonomethoxypropyl)adenine is reacted with dimethylformamide dimethylacetal to give N4-dimethylaminomethyledino-9-(2-phosphonomethoxy ethyl) adenine, which is then reacted with chloromethyl-2-propyl carbonate in presence of triethylamine to give (R)-N4-Dimethylaminomethyledino-9-(2-phosphono methoxypropyl) adenine disoproxil, followed by deprotection with acetic acid to get tenofovir disoproxil. Tenofovir disoproxil is then treated with fumaric acid to give tenofovir disoproxil fumarate.Type: GrantFiled: July 26, 2005Date of Patent: June 15, 2010Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
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Patent number: 7723319Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.Type: GrantFiled: September 9, 2009Date of Patent: May 25, 2010Assignee: 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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Patent number: 7718658Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 31, 2005Date of Patent: May 18, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
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Publication number: 20100099869Abstract: This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.Type: ApplicationFiled: November 8, 2007Publication date: April 22, 2010Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE-CNRS, UNIVERSITE DE LA MEDITERRANEE, K.U. LEUVEN RESEARCH & DEVELOPMENTInventors: Bruno Canard, Karine Alvarez, Karine Barral, Jean-Louis Romette, Johan Neyts, Jan Balzarini
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Publication number: 20100093667Abstract: The invention is related to salts of anti-viral compounds, compositions containing such salts, and therapeutic methods that include the administration of such salts, as well as to processes and intermediates useful for preparing such salts.Type: ApplicationFiled: July 7, 2009Publication date: April 15, 2010Applicant: Gilead Sciences, Inc.Inventors: Benjamin R. Graetz, Richard Polniaszek
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Patent number: 7662960Abstract: Conformationally constrained compounds of structure: which mimic the secondary structure of ?-strand regions of biologically active peptides and proteins are disclosed. Such ?-strand mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents that inhibit protease, kinase and the like. Libraries containing the ?-strand mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members.Type: GrantFiled: May 30, 2003Date of Patent: February 16, 2010Assignee: Choongwae Pharma CorporationInventors: Michael Kahn, Masakatsu Eguchi, Sung Hwan Moon, Jae Uk Chung
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Publication number: 20090298794Abstract: The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof:Type: ApplicationFiled: May 28, 2009Publication date: December 3, 2009Inventors: William N. Washburn, Saleem Ahmad, Pratik Devasthale, Jeffrey A. Robl, Animesh Goswami, Zhiwei Guo, Ramesh N. Patel
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Patent number: 7625910Abstract: The present invention relates to a novel co-crystal of 2-{ethyl[3-({4-[(5-{2-[(3-fluorophenyl)amino]-2-oxoethyl}-1H-pyrazol-3-yl)amino]quinazolin-7-yl}oxy)propyl]amino}ethyl dihydrogen phosphate (AZD1152) which is an aurora kinase inhibitor that is useful in the treatment of hyperproliferative diseases such as cancer.Type: GrantFiled: May 15, 2007Date of Patent: December 1, 2009Assignee: AstraZeneca ABInventors: George Joseph Sependa, Richard Storey
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Patent number: 7625881Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structure and their use in treating mammals for various disease states.Type: GrantFiled: June 14, 2006Date of Patent: December 1, 2009Assignee: Gilead Palo Alto, Inc.Inventors: Rao Kalla, Dmitry Koltun, Jeff Zablocki, Elfatih Elzein
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Publication number: 20090286981Abstract: The present invention relates to novel Tenofovir disoproxil hemifumarate salt, which is prepared by dealkylation of Phosphonate esters by using mineral acids followed by esterification and crystallization to give crystalline Tenofovir disoproxil. The Tenofovir disoproxil is further converted to fumarate salts with improved yield.Type: ApplicationFiled: January 12, 2009Publication date: November 19, 2009Inventors: Uma Maheswer Rao Vasireddy, Siva Rama Prasad Vellanki, Raja Babu Balusu, Naga Durga Rao Bandi, Pavan Kumar Jujjavarapu, Sambasiva Rao Ginjupalli, Rama Krishna Pilli
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Publication number: 20090275535Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, 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 1, 2008Publication date: November 5, 2009Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang
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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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Patent number: 7608603Abstract: Compounds of formula Ia, Ib, Ic, Id, Ie, If, Ig or Ih: wherein X and Y are nitrogen or one of X and Y is nitrogen and the other is CRg, and W, D, E, R4, R5, R6 and Rg are as defined herein. Also disclosed are methods of making the subject compounds and methods of using the compounds in the treatment of p38 MAP kinase-mediated diseases.Type: GrantFiled: August 23, 2006Date of Patent: October 27, 2009Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Tobias Gabriel, Kristen Lynn McCaleb
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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: 20090258840Abstract: A compound of formula (1), and/or its salts, tautomers or solvates is used to treat hematological malignancies. In an embodiment, an organic acid salt of compound 1 is provided for general use in treatment of neoplasms, and in a further embodiment the salt is stabilized with carbohydrate.Type: ApplicationFiled: May 16, 2007Publication date: October 15, 2009Applicant: Gilead Sciences, Inc.Inventors: Lee S. Chong, William S. Lee, Adrian S. Ray, Hans Reiser, Daniel B. Tumas, William J. Watkins
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Publication number: 20090246818Abstract: The invention concerns stable nicotinamide adenine dinucleotide (NAD/NADH) and nicotinamide adenine dinucleotide phosphate (NADP/NADPH) derivatives, enzyme complexes of these derivatives and their use in biochemical detection methods and reagent matrices.Type: ApplicationFiled: May 26, 2009Publication date: October 1, 2009Inventors: Dieter Heindl, Joachim Hoenes, Carina Horn, Piet Herdewijn
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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: 20090202484Abstract: The present application provides for a compound of Formula (I) or (II): or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.Type: ApplicationFiled: July 6, 2007Publication date: August 13, 2009Applicant: Gilead Sciences, Inc.Inventors: Lee S. Chong, Manoj C. Desai, Brian Gallagher, Michael Graupe, Randall L. Halcomb, Hong Yang, Jennifer R. Zhang
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Patent number: 7566721Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.Type: GrantFiled: August 3, 2006Date of Patent: July 28, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Qun-Sheng Ji, Mark Joseph Mulvihill, Arno G. Steinig, Qinghua Weng
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Patent number: 7566781Abstract: The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.Type: GrantFiled: May 9, 2005Date of Patent: July 28, 2009Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Shunji Sakuraba, Minoru Moriya, Hidekazu Takahashi, Hiroyuki Kishino, Makoto Jitsuoka, Minoru Kameda, Akio Kanatani
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Publication number: 20090187019Abstract: The present invention relates to a new process for preparing diisopropyl {[1-(hydroxymethyl)-cyclopropyl]oxy}methylphosphonate (2), which is a key intermediate for synthesizing an antiviral (particularly, against hepatitis B virus) nucleoside analogue. The present invention also relates to new intermediates, and a process for preparing the antiviral nucleoside analogue from the compound (2) prepared according to the present invention.Type: ApplicationFiled: June 27, 2005Publication date: July 23, 2009Applicant: LG LIFE SCIENCE LTD.Inventors: Suk-Kyoon Yoon, Kun-Hye Nam, Sang-Who Lee, Won-Kyo Joung, Sang-Chul Choi, Ki-Kon Lee
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Patent number: 7563781Abstract: The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.Type: GrantFiled: January 11, 2006Date of Patent: July 21, 2009Assignee: Janssen Pharmaceutica NVInventors: Donald W. Ludovici, Richard W. Connors, Steven J. Coats, Li Liu, Bart L. De Corte, Dana L. Johnson, Mark J. Schulz
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Patent number: 7553825Abstract: Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ?O, —O(RX), ?S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX) (RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups; R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or R3d; R3a is —H, —F, —Cl, —Br, —I, —CF3, —CN, N3, —NO2, or —OR4; R3b is ?O, —O(R4), ?S, —N(R4), —N(O)(R4), —N(OR4), —N(O)(OR4), or —N(N(R4) (R4)); R3c is —R4, —N(R4)(R4), —SR4, —S(O)R4, —S(O)2R4, —S(O)(OR4), —S(O)2(OR4), —OC(R3b)R4, —OC(R3b)OR4, —OC(R3b)(N(R4)(R4)), —SC(R3b)R4, —SC(R3b)OR4, SC(R3b)Type: GrantFiled: December 29, 2004Date of Patent: June 30, 2009Assignee: Gilead Sciences, Inc.Inventors: Xiaoqin Cheng, Gary P. Cook, Manoj C. Desai, Edward Doerffler, Gong-Xin He, Choung U. Kim, William A. Lee, John C. Rohloff, Jianying Wang, Zheng-Yu Yang
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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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Publication number: 20090156558Abstract: The invention is related to phosphorus substituted antimetabolites, 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 2, 2008Publication date: June 18, 2009Inventors: Maria Fardis, Thorsten Kirschberg, William J. Watkins