The Additional Chalcogen Containing Hetero Ring Is Part Of A Polycyclo Ring System Patents (Class 514/263.24)
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Publication number: 20110118257Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: November 3, 2010Publication date: May 19, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
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Publication number: 20110118276Abstract: The present invention relates to adenosine A2B receptor antagonists and their use for the prevention and treatment of atherosclerosis by administering to a mammal, in need thereof, a therapeutically effective amount of an adenosine A2B receptor antagonist, or a pharmaceutically acceptable salt thereof, alone or in combination with other anti-atherosclerotic agents.Type: ApplicationFiled: July 15, 2009Publication date: May 19, 2011Inventor: Edward Leung
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Publication number: 20110104054Abstract: Hsp90 inhibitors having are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.Type: ApplicationFiled: November 4, 2010Publication date: May 5, 2011Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-bufi, Joungnam Kim, Steven M. Larson, Peter Smith-Jones
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Publication number: 20110105417Abstract: Conjugated compounds comprising a therapeutic or diagnostic agent linked to a substrate for a cell membrane transporter or receptor by lipophilic linker are provided.Type: ApplicationFiled: June 26, 2009Publication date: May 5, 2011Inventors: Ashim K. Mitra, Swapan Kumar Samanta
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Publication number: 20110086868Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: ApplicationFiled: December 16, 2010Publication date: April 14, 2011Applicant: NOVA Southeastern UniversityInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7915268Abstract: The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory diseases, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: March 29, 2011Assignee: Wyeth LLCInventors: Yingchun Lu, Celia Kingsbury, Adolph Bohnstedt, Michael Ohlmeyer, Vidyadhar Paradkar
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Publication number: 20110070192Abstract: Processes for the preparation of racemic and optically active nucleoside analogs of formula (A) are described. These compounds are useful as anti-infective agents, antisense therapeutic agents and hybridization assay probes.Type: ApplicationFiled: November 8, 2004Publication date: March 24, 2011Inventors: Bruno Tse, Borcherng Hong, Wei-Hung Chen, Yea-Fen Jiang, Shuo-Cang Zhang, Subramanian Marappan, Sepehr Sarshar
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Patent number: 7906518Abstract: The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2?,3?-methylidene acetal adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.Type: GrantFiled: June 26, 2007Date of Patent: March 15, 2011Assignee: CBT Development LimitedInventor: Edward D. Savory
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Patent number: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Publication number: 20110046166Abstract: Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.Type: ApplicationFiled: March 24, 2009Publication date: February 24, 2011Applicant: Office of Technology Transfer, NIHInventors: Kenneth A. Jacobson, Artem Melman
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Publication number: 20100249122Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.Type: ApplicationFiled: September 5, 2007Publication date: September 30, 2010Applicant: Emory UniversityInventor: Daniel Kalman
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Publication number: 20100210579Abstract: Disclosed are novel compounds a compound of Formula I that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.Type: ApplicationFiled: March 15, 2010Publication date: August 19, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Publication number: 20100183564Abstract: The present invention relates to compounds and compositions for expanding the number of CD34+ cells for transplantation. The invention further relates to a cell population comprising expanded hematopoietic stem cells (HSCs) and its use in autologous or allogeneic transplantation for the treatment of patients with inherited immunodeficient and autoimmune diseases and diverse hematopoietic disorders to reconstitute the hematopoietic cell lineages and immune system defense.Type: ApplicationFiled: October 29, 2009Publication date: July 22, 2010Applicant: IRM LLCInventors: Anthony E. Boitano, Michael Cooke, Shifeng Pan, Peter G. Schultz, John Tellew, Yongqin Wan, Xing Wang
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Publication number: 20100179128Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Patent number: 7754728Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: GrantFiled: September 26, 2003Date of Patent: July 13, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Publication number: 20100063071Abstract: Compositions and dosage forms including adenosine receptor antagonists such as 3-[4-(2,6-Dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-bicyclo[2.2.2]oct-1-yl]-propionic acid and methods of using the same are described herein.Type: ApplicationFiled: June 12, 2009Publication date: March 11, 2010Inventors: William F. Kiesman, Mary Fure, John Kuczek, Aaron Deykin, Barry Ticho, David Bird, Vince Covari
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Publication number: 20100035901Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: ApplicationFiled: November 5, 2007Publication date: February 11, 2010Inventors: David Festus Charles Moffat, Simon Christopher Hirst, Stuart Thomas Onions
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Patent number: 7645763Abstract: The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, the mixtures thereof, and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: February 22, 2005Date of Patent: January 12, 2010Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
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Publication number: 20090298808Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: January 6, 2009Publication date: December 3, 2009Inventors: Wenqing Yao, Chunhong He, Jingcong Zhuo
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Patent number: 7608601Abstract: The present invention relates to the use of nucleoside derivatives of formula I wherein B signifies a 9-purinyl residue B1 of formula or a 1-pyrimidyl residue B2 of formula wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof; for the treatment of diseases mediated by the Hepatitis C Virus (HCV), for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.Type: GrantFiled: July 15, 2004Date of Patent: October 27, 2009Assignee: Roche Palo Alto LLCInventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Patent number: 7601713Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.Type: GrantFiled: December 15, 2006Date of Patent: October 13, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
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Publication number: 20090253665Abstract: Pharmaceutical compositions comprising an aldosterone inhibitor and an adenosine A1 receptor antagonist (AA1RA) and methods of treating cardiovascular disease comprising identifying a patient in need of such treatment, and administering a pharmaceutical composition disclosed herein to said patient are disclosed.Type: ApplicationFiled: June 16, 2009Publication date: October 8, 2009Inventors: Lauren Otsuki, Kenneth Widder, Howard C. Dittrich
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Publication number: 20090233872Abstract: [Problems] To provide a neuronal cell death inhibitor and a therapeutic agent for a neurodegenerative disease, particularly Parkinson's disease. [Means for Solving Problems] It is known that DJ-1 protein is involved in Parkinson's disease and is capable of inhibiting neuronal cell death caused by oxidative stress. Based on this knowledge, screening is made for a low molecular weight molecule capable of binding to an active site of DJ-1 protein (i.e., a region around a cysteine residue at position-106) using an analysis softwear FastDock (Fujitsu Ltd.). When various tests are made using candidate low molecular weight compounds each having a binding energy of ?60 kcal/mol or lower, these compounds show a therapeutic effect on a neurodegenerative disease.Type: ApplicationFiled: November 17, 2006Publication date: September 17, 2009Applicant: National University Corporation Hokkaido UniversityInventor: Hiroyoshi Ariga
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Patent number: 7579354Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.Type: GrantFiled: July 10, 2006Date of Patent: August 25, 2009Inventors: William F. Kiesman, Carol L. Ensinger, Russell C. Petter, James E. Dowling, Gnanasambandam Kumaravel, He Xi Chang, Ko Chung Lin
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Publication number: 20090203689Abstract: Disclosed are novel compounds of Formula I useful for treating various disease states, in particular, insulin resistance, diabetes, dyslipidemia, coronary artery disease, and inflammation. The compounds of the present invention elevate cellular expression of the ABCA-1 gene as well as increasing the level of ABCA-1 protein, which may result in an increase in HDL levels in the plasma of a mammal, in particular humans.Type: ApplicationFiled: February 6, 2009Publication date: August 13, 2009Inventors: Arvinder Dhalla, Jeffrey Chisholm, Luiz Belardinelli
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Patent number: 7569574Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.Type: GrantFiled: August 4, 2003Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
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Publication number: 20090131370Abstract: Compounds of Formulae I-XVI, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of viral diseases including hepatitis C viral infection, cancer, diabetes, and other diseases are described: formula (I).Type: ApplicationFiled: July 29, 2005Publication date: May 21, 2009Applicant: METABASIS THERAPEUTICS , INC.Inventors: K. Raja Reddy, Mark D. Erion
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Patent number: 7494984Abstract: The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: August 29, 2006Date of Patent: February 24, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Roger Remillard, Serge Plamondon
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Publication number: 20080293747Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.Type: ApplicationFiled: November 9, 2006Publication date: November 27, 2008Inventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
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Publication number: 20080253965Abstract: Hsp90 inhibitors are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2. alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.Type: ApplicationFiled: February 1, 2006Publication date: October 16, 2008Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
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Publication number: 20080234297Abstract: The present invention relates to HSP90 inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2007Publication date: September 25, 2008Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
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Publication number: 20080221132Abstract: The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.Type: ApplicationFiled: September 10, 2007Publication date: September 11, 2008Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20080207649Abstract: The present invention relates to a method of treating various neurodegenerative disorders, in which a xanthine derivative represented by formula (I): or a pharmaceutically acceptable salt thereof, as an active ingredient, is administered.Type: ApplicationFiled: April 30, 2008Publication date: August 28, 2008Inventors: Junichi SHIMADA, Masako Kurokawa, Ken Ikeda, Fumio Suzuki, Yoshihisa Kuwana
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Patent number: 7358235Abstract: Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical compositions including analogs of nitrobenzylthioinosine.Type: GrantFiled: October 6, 2004Date of Patent: April 15, 2008Assignees: Gruenenthal GmbH, Leiden UniversityInventors: Claudia Puetz, Corinna Sundermann, Bernd Sundermann, Adriaan Pieter Ijzerman, Reynier Tromp, Jacobien Von Frijtag Drabbe Kuenzel
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Publication number: 20040266722Abstract: The present invention relates to the use of nucleoside derivatives of formula I 1Type: ApplicationFiled: July 15, 2004Publication date: December 30, 2004Inventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Publication number: 20040214789Abstract: The use of a compound of formula (Ia): 1Type: ApplicationFiled: December 8, 2003Publication date: October 28, 2004Inventors: Barry V.L. Potter, Andreas H. Guse, Georg W. Mayr, Katrin Schweitzer
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Publication number: 20040157793Abstract: The present invention relates to 3′ substituted-2′, 3′-didehydro-2′, 3′-dideoxy-&bgr;-L-nucleosides and their pharmaceutically acceptable salts and prodrugs thereof, for the treatment of infectious viral diseases, in general, particularly HBV and HIV viral infections and more particularly, HBV and HIV viral infections that are resistant to other antiviral drugs.Type: ApplicationFiled: November 12, 2003Publication date: August 12, 2004Inventors: Lieven J. Stuyver, Chung K. Chu
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Patent number: 6774130Abstract: Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S.Type: GrantFiled: April 9, 1999Date of Patent: August 10, 2004Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Stephen J. Klaus, Anil M. Kumar, Baoqing Gong
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Publication number: 20040116448Abstract: The invention relates to medicaments and compounds for the treatment of diseases caused by highly proliferating cells, such as tumor cells, especially blasts of children suffering from acute leukemia. The invention also relates to the preparation of the corresponding medicaments and compounds.Type: ApplicationFiled: January 29, 2004Publication date: June 17, 2004Inventors: Hans-Gunther Schmalz, Aram Prokop, Thomas P. Wieder, Peter T. Daniel
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Publication number: 20040102459Abstract: Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11, is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or proType: ApplicationFiled: November 13, 2003Publication date: May 27, 2004Inventors: Roger John Gillespie, Joanne Lerpiniere, Claire Elizabeth Dawson, Suneel Gaur, Robert Mark Pratt, Gemma Caroline Stratton, Scott Murray Weiss
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Publication number: 20040067966Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.Type: ApplicationFiled: August 21, 2003Publication date: April 8, 2004Applicant: Biogen, Inc.Inventors: William F. Kiesman, Carol L. Ensinger, Russell C. Petter, James E. Dowling, Gnanasambandam Kumaravel, He Xi Chang, Ko Chung Lin
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Publication number: 20040067967Abstract: The invention provides a pharmaceutical composition for treatment or prevention of urinary dysfunction in a mammal. The composition includes a pharmaceutically effective amount of one or more substances capable of enabling the bladder of the mammal to mimic conditions found in advanced pregnancy. Alternately, the pharmaceutical composition has a pharmaceutically effective amount of one or more substances adapted to regulate the expression of one or more ATPases that control the supply of ATP to P2X receptors in the bladder of the mammal. In one aspect, the pharmaceutical composition may downregulate expression of subtype receptors P2X1, P2X2, P2X3 and P2X5, possibly upregulating expression of subtype receptors P2X4 and P2X6.Type: ApplicationFiled: October 2, 2003Publication date: April 8, 2004Inventors: Julian Alexander Barden, Angus Gidley-Baird
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Publication number: 20030225038Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.Type: ApplicationFiled: June 12, 2003Publication date: December 4, 2003Applicant: Biogen, Inc.Inventors: Carol L. Ensinger, James E. Dowling, Russell C. Petter, Gnanasambandam Kumaravel
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Patent number: 6649600Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be usefull in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: wherein: R3 is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from: and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.Type: GrantFiled: November 13, 2000Date of Patent: November 18, 2003Assignee: Biogen, Inc.Inventors: William F. Kiesman, Carol L. Ensinger, Russell C. Petter, James E. Dowling, Gnanasambandam Kumaravel, He Xi Chang, Ko Chung Lin
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Publication number: 20030207841Abstract: A compound of the formula (1): 1Type: ApplicationFiled: May 5, 2003Publication date: November 6, 2003Applicant: SANKYO COMPANY LIMITEDInventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
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Publication number: 20030186978Abstract: The present invention relates to novel telomerase inhibitors possessing antitumor activity and to a process for preparing the same. Furthermore, these compounds enhance the efficacy of other chemotherapeutic agents, in the treatment of cancer.Type: ApplicationFiled: May 23, 2003Publication date: October 2, 2003Inventors: Alberto Bargiotti, Antonella Ermoli, Maria Menichincheri, Ermes Vanotti, Luisella Bonomini, Antonella Fretta
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Patent number: 6620796Abstract: The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.Type: GrantFiled: November 8, 2000Date of Patent: September 16, 2003Assignee: Micrologix Biotech Inc.Inventors: Wenqiang Zhou, Yi Jin, Arlene Roland, Radhakrishnan Iyer
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Publication number: 20030158214Abstract: The present invention relates to a therapeutic agent for neurodegenerative disorders, comprising a xanthine derivative represented by formula (I): 1Type: ApplicationFiled: March 3, 2000Publication date: August 21, 2003Inventors: JUNICHI SHIMADA, MASAKO KUROKAWA, KEN IKEDA, FUMIO SUZUKI, YOSHIHISA KUWANA
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Publication number: 20030069423Abstract: Novel processes for the preparation of adenosine compounds and intermediates thereto. The adenosine compounds prepared by the present processes may be useful as cardiovascular agents, more particularly as antihypertensive and anti-ischemic agents, as cardioprotective agents which ameliorate ischemic injury or myocardial infarct size consequent to myocardial ischemia, and as an antilipolytic agents which reduce plasma lipid levels, serum triglyceride levels, and plasma cholesterol levels. The present processes may offer improved yields, purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.Type: ApplicationFiled: May 10, 2002Publication date: April 10, 2003Inventors: Timothy A. Ayers, Geoffrey A. D'Netto, Gregory G. Kubiak, James J. Mencel, Michael K. O'Brien, Matthew R. Powers, John J. Shay, Adam W. Sledeski, David S. Teager, Benoit Vanasse