Four Or More Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/118)
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Publication number: 20090137581Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: March 24, 2008Publication date: May 28, 2009Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20090137549Abstract: The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation.Type: ApplicationFiled: November 8, 2007Publication date: May 28, 2009Inventors: Paul John Edward, Mark Stuart Chambers, Christel Jeanne Marie Menet, Stephen Robert Fletcher, Rebecca Elizabeth Jarvis, Herve Van De Poel, Alexander Sudau, Alastair Rae, Peter Stanley Thomas
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Publication number: 20090131624Abstract: Morpholino compounds are provided having the structure: where R1 is selected from the group consisting of lower alkyl, di(lower alkyl)amino, and phenyl; R2 is selected from the group consisting of lower alkyl, monocyclic arylmethyl, and monocyclic (aryloxy)methyl; R3 is selected from the group consisting of triarylmethyl and hydrogen; and Y is selected from the group consisting of: a protected or unprotected hydroxyl or amino group; a chlorophosphoramidate group; and a phosphorodiamidate linkage to the ring nitrogen of a further morpholino compound or a morpholino oligomer. Such compounds include doubly protected morpholino guanine (MoG) monomers. Also described is their use in synthesis of morpholino oligomers.Type: ApplicationFiled: November 14, 2008Publication date: May 21, 2009Applicant: AVI BIOPHARMA, INC.Inventors: MATTHEW DALE REEVES, DWIGHT D. WELLER
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Publication number: 20090131432Abstract: Compounds of formula (I) wherein R1 to R4 are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type I and type II diabetes mellitus, arthritis, obesity, allograft transplantation, or calcitonin-induced osteoporosis using these compounds.Type: ApplicationFiled: January 16, 2009Publication date: May 21, 2009Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Michael MARK, Roland MAIER, Ralf R. H. LOTZ
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Publication number: 20090124609Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 15, 2008Publication date: May 14, 2009Applicant: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20090124612Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: July 13, 2007Publication date: May 14, 2009Applicant: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20090118275Abstract: Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 23, 2008Publication date: May 7, 2009Applicants: Genentech, Inc., F. Hoffmann - La Roche AGInventors: Georgette M. Castanedo, Janet L. Gunzner, Kimberly Malesky, Simon Mathieu, Alan G. Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Sally Oxenford, Nan Chi Wan
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Publication number: 20090118263Abstract: An adenine compound represented by the formula (1): (1) [wherein A1 and A2 each independently represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1, L2, and L3 each independently represents alkylene or a single bond, provided that any methylene or methine group in L2 or L3 may be bonded to the nitrogen atom adjacent to L2 and L3 to form a 4- to 7-membered saturated nitrogenous heterocycle; L4 represents alkylene or a single bond; R1 represents (un)substituted alkyl, (un)substituted aryl, etc.; R2 represents hydrogen or (un)substituted alkyl; R3 represents (un)substituted alkyl, etc.; and X represents oxygen, etc.] or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.Type: ApplicationFiled: September 20, 2006Publication date: May 7, 2009Applicants: Dainippon Sumitomo Pharma Co., Ltd., ASTRAZENECA AKTIEBOLAGInventors: Kazuki Hashimoto, Tomoaki Nakamura, Kei Nakamura, Ayumu Kurimoto, Yoshiaki Isobe
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Patent number: 7521446Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: GrantFiled: April 26, 2006Date of Patent: April 21, 2009Assignee: Signal Pharmaceuticals, LLCInventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright
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Publication number: 20090098086Abstract: The invention relates to thienopyrimidine and pyrazolopyrimidine compounds of the Formulas (Ia) and (IIa), or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein compositions comprising the compounds, and methods for making and using the compounds.Type: ApplicationFiled: October 15, 2008Publication date: April 16, 2009Applicant: WyethInventors: Arie Zask, Joshua Aaron Kaplan, Jeroen Cunera Verheijen, Kevin J. Curran, David James Richard, Semiramis Ayral-Kaloustian
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Publication number: 20090088569Abstract: The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula wherein R1 to R4 and X are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, 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: ApplicationFiled: December 5, 2008Publication date: April 2, 2009Inventors: Matthias ECKHARDT, Frank HIMMELSBACH, Elke LANGKOPF, Norbert HAUEL, Mohammad TADAYYON, Leo THOMAS
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Publication number: 20090074717Abstract: Disclosed are compounds of Formula (I), pharmaceutically acceptable salts and solvates thereof, compositions thereof, and methods for their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: July 11, 2008Publication date: March 19, 2009Inventors: Martin Robert Leivers, Jesse Daniel Keicher, Franz Ulrich Schmitz, Roopa Rai, Ryan Lauchli, Sebastian Reinhard Johannes Liehr, Stephanie Anna Chan, Tony Loc Ton
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Publication number: 20090069289Abstract: 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: ApplicationFiled: August 22, 2008Publication date: March 12, 2009Applicant: PHARMACOPEIA, INC.Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Ansari Nasrin
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Patent number: 7501411Abstract: Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.Type: GrantFiled: May 30, 2007Date of Patent: March 10, 2009Assignee: Galapagos, NVInventors: Martin James Inglis Andrews, Paul Edwards, Mark Stuart Chambers, Wolfgang Schmidt, Juha Andrew Clase, Gregory Bar, Kim Louise Hirst, Angus MacLeod
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Patent number: 7495005Abstract: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted, and R2 to R4 are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type I and type II diabetes mellitus, arthritis, obesity, allograft transplantation and calcitonin-induced osteoporosis using these compounds.Type: GrantFiled: August 7, 2003Date of Patent: February 24, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz
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Patent number: 7494993Abstract: The present invention relates to novel amide derivatives of 7-amino-3-phenyl dihydropyrimido[4,5-d]pyrimidinones, to a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The present derivatives are new compounds of the general formula (I).Type: GrantFiled: August 30, 2005Date of Patent: February 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Richard Engh, Hubert Hertenberger, Konrad Honold, Birgit Masjost, Petra Rueger, Wolfgang Schaefer, Stefan Scheiblich, Manfred Schwaiger
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Publication number: 20090048442Abstract: Novel substituted pyrimido[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: ApplicationFiled: October 11, 2007Publication date: February 19, 2009Inventors: Jerry L. Adams, Jeffrey C. Boehm, John J. Taggart, Ralph F. Hall
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Publication number: 20090047249Abstract: The present application includes 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: June 26, 2008Publication date: February 19, 2009Inventors: Micheal Graupe, Randall L. Halcomb
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Publication number: 20090029973Abstract: The present invention relates to a compound represented by the formula: wherein W is C(R1) or N, each A is an optionally substituted aryl group or a heteroaryl group, X1 is —NR3—Y1—, —O—, —S—, —SO—, —SO2— or —CHR3— wherein R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 is optionally bonded to A to form an optionally substituted ring structure, R1 is a hydrogen atom or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom, R2 is a hydrogen atom or optionally substituted group bonded via a carbon atom or a sulfur atom, or R1 and R2, or R2 and R3 are optionally bonded to form an optionally substituted ring structure, or a salt thereof, and a tyrosine kinase inhibitor or an agent for the prophylaxis or treatment of cancer, which contains this compound or a prodrug thereof.Type: ApplicationFiled: July 14, 2008Publication date: January 29, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tomoyasu ISHIKAWA, Takahiko TANIGUCHI, Hiroshi BANNO, Masaki SETO
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Publication number: 20090029989Abstract: Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases.Type: ApplicationFiled: July 8, 2008Publication date: January 29, 2009Inventors: Jerry Leroy Adams, Jiri Kasparec, Domingos J. Silva, Catherine C. K. Yuan
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20090023723Abstract: The invention relates to purinone derivatives useful in treating disorders that are mediated by adenosine receptor function, including neurodegenerative diseases and inflammation.Type: ApplicationFiled: September 21, 2006Publication date: January 22, 2009Applicant: Pharmacopeia Drug Discovery, Inc.Inventors: Andrew G. Cole, Ian Henderson, Marc-Raleigh Brescia, Axel Metzger, Lan-Ying Qin, Gulzar Ahmed, Brian F. McGuinness, Yuefei Shao, Jingqi Duo
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Publication number: 20090023704Abstract: The present invention relates to novel xanthine compounds of the general formula (I) wherein R1, R2, R3 and R4 are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).Type: ApplicationFiled: April 17, 2008Publication date: January 22, 2009Applicant: ASTRAZENECA ABInventors: Leifeng Cheng, Sara Holmqvist, Florian Raubacher, Peter Schell
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Patent number: 7479558Abstract: The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.Type: GrantFiled: March 24, 2006Date of Patent: January 20, 2009Assignee: Glaxo Group LimitedInventors: James F. Callahan, Jeffrey C. Boehm, Zehong Wan, Hongxing Yan, Xichen Lin
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Publication number: 20090018331Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: ApplicationFiled: August 28, 2008Publication date: January 15, 2009Applicant: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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Patent number: 7476670Abstract: The invention relates to novel products of formula (I): in which: Y represents N, O, S, CHR3 or ?CR3 the dashed line representing a single or double bond, R and R1 represent in particular H, Hal, OH, alkyl, alkoxy, cyano, NO2, NR4R5, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, —S(O)n-NR4R5 with n representing 0 to 2, acyl, —NH—CO-alkyl or —NH—CO—NH-phenyl, R3 represents H, Hal, alkyl, cyano, NO2, NR4R5, trifluoromethyl or aryl, R2 represents R4, OR4, SR4 or NR4R5, R4 represents H, alkyl, cycloalkyl or aryl, either R4 and R5 are chosen from the values for R4, or R4 and R5 form, with N, a heterocyclic radical which may contain N, O and S, all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.Type: GrantFiled: February 17, 2004Date of Patent: January 13, 2009Assignee: Aventis Pharma S.A.Inventors: Florence Bordon-Pallier, Jean-Luc Haesslein
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Patent number: 7470697Abstract: The present invention provides compounds of the following formula and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: August 31, 2007Date of Patent: December 30, 2008Assignee: Adenosine Therapeutics, LLCInventors: Guoquan Wang, Robert D. Thompson
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Publication number: 20080319190Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: ApplicationFiled: August 15, 2008Publication date: December 25, 2008Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias GRAUERT, Matthias HOFFMANN, Martin STEEGMAIER, Flavio SOLCA, Jens QUANT
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Publication number: 20080318949Abstract: The invention discloses a series of pyrazolopyrimidinone derivatives, which have the following chemical structure, their preparation methods and use, It has been proved by pharmacological experiment that the said pyrazolopyrimidinone derivatives have high inhibitory activity against PDE5, and parts of them have a much stronger potency against PDE5 than against PDE6. Most of the compounds show low toxicity. The pyrazolopyrimidinone derivatives can be used in clinics for the palliative or curative treatment of symptoms or diseases relating to cardiovascular system, urinary system, especially for the palliative or curative treatment of erectile dysfunction.Type: ApplicationFiled: November 16, 2006Publication date: December 25, 2008Applicants: Topharman Shanghai Co., Ltd, Shanghai Institute of Materia MedicaInventors: Guanghui Tian, Shunan Lai, Zhen Wang, Yi Zhu, Xinjian Chen, Yurong Ji, Jinfeng Zhang, Weixi Jin, Heping Lv, Jinping Liu, Wei Wang, Ruyun Ji, Jingshan Shen
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Publication number: 20080300244Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 13, 2007Publication date: December 4, 2008Applicant: AstraZeneca ABInventors: Roger Victor BONNERT, Thomas McInally, Tobias Mochel, Stephen Thom
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Publication number: 20080293697Abstract: This invention relates to compounds of formula (I).Type: ApplicationFiled: March 30, 2005Publication date: November 27, 2008Inventors: Andrew Simon Bell, David Graham Brown, David Nathan Abraham Fox, Ian Roger Marsh, Andrew Ian Morrell, Dafydd Rhys Owen, Michael John Palmer, Carol Ann Winslow, Hwang Fun Lu, Thomas Edward Rogers
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Publication number: 20080293713Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, and R3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: ApplicationFiled: April 30, 2008Publication date: November 27, 2008Applicant: Abbott LaboratoriesInventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
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Patent number: 7452880Abstract: Compounds of the formula I: where A, B, X, Y, Z, k, R1, R2 and R3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a patient.Type: GrantFiled: February 25, 2005Date of Patent: November 18, 2008Inventors: Nidhi Arora, Roland Joseph Billedeau, Nolan James Dewdney, Tobias Gabriel, David Michael Goldstein, Teresa Alejandra Trejo-Martin
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Publication number: 20080280907Abstract: The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.Type: ApplicationFiled: January 4, 2006Publication date: November 13, 2008Applicant: Aaltana Pharma AGInventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Kulzer, Hermann Tenor, Hans-Peter Kley
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Publication number: 20080261973Abstract: The invention relates to sulphonamidoanilines of formula I, wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R1 represents NR4R5 or OR4, wherein R4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R5 represents hydrogen or unsubstituted or substituted alky, or R4 and R5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R2 is hydrogen, lower alkenyl or alkyl, R3 is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal bodyType: ApplicationFiled: December 20, 2006Publication date: October 23, 2008Applicant: Novartis AGInventors: Hans-Georg Capraro, Bernard Coupez, Pascal Furet, Paul W. Manley, Carole Pissot Soldermann
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Patent number: 7439240Abstract: The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.Type: GrantFiled: June 23, 2003Date of Patent: October 21, 2008Assignee: AstraZeneca ABInventors: Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
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Patent number: 7435731Abstract: Compounds of the formula Ia or Ib: wherein A, B, X, Y, Z, W, k, R1, R2, R3, R4 and R5 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a subject.Type: GrantFiled: February 25, 2005Date of Patent: October 14, 2008Assignee: Roche Palo Alto LLCInventors: Nidhi Arora, Roland Joseph Billedeau, Nolan James Dewdney, Tobias Gabriel, David Michael Goldstein, Counde O'Yang, Michael Soth
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Publication number: 20080249089Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs 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: ApplicationFiled: June 20, 2008Publication date: October 9, 2008Applicant: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R.H. Lotz, Mohammad Tadayyon
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Publication number: 20080242661Abstract: The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation.Type: ApplicationFiled: December 10, 2007Publication date: October 2, 2008Inventors: Graeme James Dykes, Stephen Robert Fletcher, Christel Jeanne Marie Menet, Nuria Merayo Merayo, Benoit Antoine Schmitt
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Publication number: 20080234262Abstract: The present invention relates to Pyrazolopyrimidine Analogs, methods of making Pyrazolopyrimidine Analogs, compositions comprising a Pyrazolopyrimidine Analog, and methods for treating mTOR-related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog. The invention also relates to treating PI3K-related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog.Type: ApplicationFiled: March 18, 2008Publication date: September 25, 2008Applicant: WyethInventors: Arie Zask, Pawel Wojciech Nowak, Jeroen Cunera Verheijen, Kevin J. Curran, Joshua Kaplan, David Malwitz, Matthew Gregory Bursavich, Derek Cecil Cole, Semiramis Ayral-Kaloustian, Ker Yu, David James Richard, Mark Lefever
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Patent number: 7425560Abstract: There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of the enzyme myeloperoxidase (MPO) is beneficial. Certain novel compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof are disclosed, together with processes for their preparation. The compounds of formulae (Ia) and (Ib) are MPO inhibitors and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders.Type: GrantFiled: April 15, 2003Date of Patent: September 16, 2008Assignee: AstraZeneca ABInventor: Anna-Karin Tidén
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Publication number: 20080221098Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.Type: ApplicationFiled: April 8, 2008Publication date: September 11, 2008Applicant: IRM LLCInventors: Taebo Sim, Hyun Soo Lee, Pingda Ren, Qiang Ding, Yi Liu, Bing Li, Lintong Li, Xia Wang, Tetsuo Uno, Guobao Zhang, Nathanael Schiander Gray, Shuli You
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Patent number: 7423038Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders than involve abnormal activation of the Abl, Bcr-abl, Bmx, c-RAF, CSK, Fes, FGFR3, Flt3, GSK3?, IR, JNK1? 1, JNK2? 2, Lck, MKK4, MKK6, p70S6K, PDGFR?, Rsk1, SAPK2?, SAPK2?, Syk and Trk? kinases.Type: GrantFiled: June 23, 2005Date of Patent: September 9, 2008Assignee: IRM LLC (a Delaware Limited Liability Corporation)Inventors: Pingda Ren, Xia Wang, Nathanael Schiander Gray, Yi Liu, Taebo Sim
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Publication number: 20080214541Abstract: The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage.Type: ApplicationFiled: September 20, 2007Publication date: September 4, 2008Applicants: IRM LLC, Scripps Research InstituteInventors: Xu Wu, Sheng Ding, Nathanael S. Gray
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Publication number: 20080200456Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: ApplicationFiled: December 14, 2007Publication date: August 21, 2008Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7414053Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: August 19, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Flavio Solca, Jens Juergen Quant
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Patent number: 7407955Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs 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: August 12, 2003Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
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Publication number: 20080177066Abstract: Disclosed are processes for preparing dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 4, 2005Publication date: July 24, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Guenter Linz, Gerd F. Kraemer, Ludwig Gutschera, Geert Asche
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Publication number: 20080146561Abstract: Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.Type: ApplicationFiled: August 1, 2007Publication date: June 19, 2008Inventors: Alex Muci, Jeffrey T. Finer, Pu-Ping Lu, Alan James Russell, Bradley P. Morgan, David J. Morgans
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Patent number: 7388002Abstract: Compounds represented by the formula: A is (CH2)nR2, —CH?CH2, CH2—CH?CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)CH2OH, CH2—CH(OH)CH3, CH2CH(OH)CH2OH, or CH(OH)CH(OH)CH3, R,R1 individually is H, NH2OH, Cl, Br, I, aryl, substituted aryl, heterocycle, NR3R4, OR3 or SR3, R2 is H, OH, F, N3, NH2, CO2H, SH, alkyl, substituted alkyl, S-alkyl, O-acyl, CONH2, or CONH-alkyl, n is 1-3, y is O, S or NH, W is O or S, Z, Z? individually is OR3, OR4, O(CH2)m—O—(CH2)xCH3, NH—CH(alkyl)CO2R3, alkyl, substituted alkyl, OCH2CH2S—C(O)CH3, OCH2CH2S—C(O)CH(CH3)2, OCH2CH2S—C(O)C(CH3)3, OCH2CH2—SC(O)aryl, OCH2CH2—S—S—OCH2CH2OH, OCH2OC(O)C(CH3)3, OCH2—O—C(O)OCH(CH3)2, or OCH2—O—C(O)CH(CH3)2 R3, R4 individually is H, alkyl, substituted alkyl, aryl, or substituted aryl; Both R3 and R4 can form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring; m is 1-3, x is 0-19; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.Type: GrantFiled: November 9, 2005Date of Patent: June 17, 2008Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan, Minwan Wu