Four Or More Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/118)
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Publication number: 20110207716Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: December 21, 2010Publication date: August 25, 2011Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20110190269Abstract: The invention relates to compounds of formula wherein R1, R1?, R2, R3, n, A, and hetaryl are defined herein or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: January 24, 2011Publication date: August 4, 2011Inventors: Karlheinz Baumann, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Publication number: 20110178067Abstract: 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: ApplicationFiled: January 9, 2011Publication date: July 21, 2011Inventors: 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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Publication number: 20110172228Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.Type: ApplicationFiled: July 8, 2009Publication date: July 14, 2011Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Michael Martin, Christian Rommel
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Publication number: 20110172216Abstract: Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I 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: January 29, 2009Publication date: July 14, 2011Applicants: Genentech, Inc., F. Hoffmann-La Roche AGInventors: Jennafer Dotson, Tim Heffron, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
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Patent number: 7968536Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: June 28, 2011Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Patent number: 7968544Abstract: 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: GrantFiled: June 26, 2008Date of Patent: June 28, 2011Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Randall L. Halcomb
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Publication number: 20110152242Abstract: A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH2; when n is two or three, V is CH2, O or NR5; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R1 groups; and R7 and R8 are independently hydrogen, hydroxy, halogen or C1-4alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, atType: ApplicationFiled: March 21, 2006Publication date: June 23, 2011Inventors: Tracy Bayliss, Rebecca Elizabeth Brown, Gregory John Hollingworth, Brian A. Jones, Christopher Richard Moyes, Lauren Rogers
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Publication number: 20110152257Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: ApplicationFiled: December 10, 2010Publication date: June 23, 2011Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindermann, Heinz Stadler, Eric Vieira
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Publication number: 20110144083Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs 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: February 23, 2011Publication date: June 16, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R. H. LOTZ
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Patent number: 7960397Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts of the following general formula are provided wherein R6 and R9 are as defined in the specification. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for application to mammalian cells, and especially human skin cells, in order to improve the cosmetic appearance of the mammalian cells, especially human skin.Type: GrantFiled: December 28, 2007Date of Patent: June 14, 2011Assignee: Institute of Experimental Botany, Academy of Sciences of the Czech RepublicInventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Publication number: 20110135668Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-1R), and/or insulin receptor (InsR) or a combination thereof.Type: ApplicationFiled: April 3, 2009Publication date: June 9, 2011Applicants: Novartis AGInventors: Bei Chen, Tao Jiang, Thomas H. Marsilje, Pierre-Yves Michellys, Truc Ngoc Nguyen, Pei Wei, Baogen Wu, Zhaobo Gao, Yonghui Ge, Chen Huang, Yuncheng Li
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Publication number: 20110135600Abstract: Compounds of the formula (I), in which X1, X2, X3, X4, X5, R1, R2, R3, R3?, R4, R6 and R7 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 16, 2009Publication date: June 9, 2011Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20110130395Abstract: 2-Morpholin-4-yl-9H-purine and 5-Morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, especially those substituted by 6-heteroaryl, are unexpected PI3 kinase isoform selective inhibitors with good drug properties and are useful in treating disorders related to abnormal PI3K activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.Type: ApplicationFiled: July 7, 2009Publication date: June 2, 2011Inventors: Congxin Liang, Zhigang Li
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Publication number: 20110130397Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: June 2, 2011Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Patent number: 7951803Abstract: Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.Type: GrantFiled: March 9, 2007Date of Patent: May 31, 2011Assignee: Pharmacopeia, LLCInventors: Andrew G. Cole, Marc-Raleigh Brescia, Joan J. Zhang, Zahid Hussain, David J. Diller, Axel Metzger, Gulzar Ahmed, Ian Henderson
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Publication number: 20110124641Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.Type: ApplicationFiled: March 16, 2009Publication date: May 26, 2011Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
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Patent number: 7947676Abstract: The invention concerns compounds of the formula (I) wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.Type: GrantFiled: December 12, 2005Date of Patent: May 24, 2011Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Publication number: 20110118221Abstract: The present invention relates to novel 1,4-diarylpyrimido[4,5-d]pyridazine-2,5-dione derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: April 24, 2009Publication date: May 19, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
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Publication number: 20110118238Abstract: This invention relates to chemical compounds of the formula (I), or a pharmaceutically acceptable salt thereof, which possess inhibitory activity against the spindle checkpoint kinase: Tyrosine Threonine Kinase (TTK)/monopolar spindle 1 (Mps1) and are accordingly useful for their anti-cancer effect in a warm-blooded animal such as man. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of a medicament for the treatment of conditions mediated by TTK/Mps1, for use either alone or in combination with other anti-pro liferative agents.Type: ApplicationFiled: August 20, 2008Publication date: May 19, 2011Applicant: ASTRAZENECA ABInventors: David Michael Andrews, Clifford David Jones, Iain Simpson, Richard Andrew Ward
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Publication number: 20110105499Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, B, R1, R2, R3, R4, R5 and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: March 19, 2009Publication date: May 5, 2011Applicant: Amgen Inc.Inventor: Andrew Tasker
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Publication number: 20110105500Abstract: The present invention relates to purine compounds of formula (I) that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumours and cancers as well as other disorders or conditions related to or associated with PI3K and/or mTOR kinases.Type: ApplicationFiled: June 25, 2009Publication date: May 5, 2011Applicant: S*BIO Pte Ltd.Inventors: Harish Kumar Mysore Nagaraj, Meredith Williams, Chang Kai Soh
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Publication number: 20110105498Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: April 24, 2008Publication date: May 5, 2011Applicant: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
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Publication number: 20110098294Abstract: The present invention provides a new patentable class of purine analog compounds, as well as compositions and methods of using them, for example, to prevent or treat various diseases and disorders in human and non-human animals.Type: ApplicationFiled: April 23, 2007Publication date: April 28, 2011Inventors: Dennis A. Carson, Howard B. Cottam, Guangyi Jin, Christina C.N. Wu, Kenji Takabayashi, Suzanne Grimshaw
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Publication number: 20110098295Abstract: A method of treating an undesirable AC8-related condition in a mammal is provided comprising the step of inhibiting AC8 in the mammalType: ApplicationFiled: October 22, 2010Publication date: April 28, 2011Inventor: Min Zhuo
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Publication number: 20110098248Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: October 15, 2010Publication date: April 28, 2011Applicant: Gilead Sciences, Inc.Inventors: Randall L. Halcomb, Paul A. Roethle
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Publication number: 20110092498Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 25, 2009Publication date: April 21, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Publication number: 20110092491Abstract: 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 cSRC, Lck, FGFR3, Flt3, TrkB, Bmx, and/or PFGFR? kinase activity.Type: ApplicationFiled: December 22, 2010Publication date: April 21, 2011Applicant: NOVARTIS AGInventors: Dai CHENG, Qiang DING, Dong HAN, Nathanael S. GRAY, Guobao ZHANG
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Publication number: 20110086841Abstract: The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.Type: ApplicationFiled: November 10, 2010Publication date: April 14, 2011Applicant: Genentech, Inc.Inventors: Zhonghua Pei, Joseph P. Lyssikatos, Kevin Hon Luen Lau, Wendy Lee, Kirk D. Robarge
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Publication number: 20110086840Abstract: The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.Type: ApplicationFiled: November 10, 2010Publication date: April 14, 2011Applicant: Genentech, Inc.Inventors: Zhonghua Pei, Joseph P. Lyssikatos, Wendy Lee, Kirk D. Robarge
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Publication number: 20110082139Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines 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, 2010Publication date: April 7, 2011Inventors: Guoquan WANG, Robert D. Thompson, Jayson M. Rieger
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Publication number: 20110082137Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V—W?*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.Type: ApplicationFiled: March 30, 2010Publication date: April 7, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Cornelia DORNER-CIOSSEK, Christian EICKMEIER, Dennis FIEGEN, Thomas FOX, Klaus FUCHS, Niklas HEINE, Holger ROSENBROCK, Gerhard SCHAENZLE
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Publication number: 20110054168Abstract: A method for preparing compound (4): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, thiomorpholine, etc., and R4 is C1-3 alkyl group, or a pharmaceutically acceptable salt, which is useful as a medicament, which comprises step (a) for preparing compound (2): wherein m, n, R1, R2 and R3 are the same as defined above, or its salt which comprises subjecting compound (1): wherein k is an integer of 1 or 2, R is hydrogen atom, halogen atom, etc., or a salt thereof to debenzylation reaction, and then step (b) for preparing compound (4) or a pharmaceutically acceptable salt which comprises reacting compound (2) or its salt prepared in the above step (a) or salt thereof and compound (3): wherein R4 is C1-3 alkyl group, in the presence of a boron-containing reducing agent.Type: ApplicationFiled: January 16, 2009Publication date: March 3, 2011Inventors: Ayumu Kurimoto, Wataru Katoda, Kazuki Hashimoto, Kazuhiko Takashi
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Publication number: 20110053915Abstract: The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins.Type: ApplicationFiled: December 12, 2008Publication date: March 3, 2011Applicant: ALLA CHEM, LLCInventors: Andrey Alexandrovich Ivaschenko, Yan Vadimovich Lavrovsky, Sergey Viktorovich Malyarchuk, Ilya Matusovich Okun, Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Alexander Viktorovich Khvat, Alexander Vasilievich Ivaschenko
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Publication number: 20110053907Abstract: Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110? isoform of PI3K.Type: ApplicationFiled: March 26, 2009Publication date: March 3, 2011Applicant: Auckland UniServices LimitedInventors: Gordon William Rewcastle, Peter Robin Shepherd, Glaire Chaussade, William Alexander Denny, Swarnalatha Akuratiya Gamage
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Publication number: 20110046369Abstract: A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.Type: ApplicationFiled: January 16, 2009Publication date: February 24, 2011Applicants: DAINIPPON SUMITOMO PHARMA CO., LTD., ASTRAZENECA AKTIEBOLAGInventors: Kazuki Hashimoto, Wataru Katoda, Kazuhiko Takahashi, Ayumu Kurimoto
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Publication number: 20110044943Abstract: 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: February 24, 2011Inventors: 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: 20110046131Abstract: A chemical genus of purines, which are useful as PKC? inhibitors, is disclosed.Type: ApplicationFiled: October 19, 2007Publication date: February 24, 2011Inventors: Irina Neagu, Andrew Laird Roughton, Koc-Kan Ho, David Diller, Jui-Hsiang Chan, Michael Ohlmeyer, Celia Kingsbury, Johannes Petrus Maria Lommerse, Neeltje Miranda, Jacobus Cornelis Henricus Maria Wijkmans
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Publication number: 20110034452Abstract: The invention relates to novel compounds of formula I where X, A?, Q1, Q2 Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: SANOFI-AVENTISInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
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Publication number: 20110034451Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: sanofi-aventisInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN, Bodo SCHEIPER
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Patent number: 7884109Abstract: The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 11, 2007Date of Patent: February 8, 2011Assignee: Wyeth LLCInventors: Michael J. Ohlmeyer, Adolph C. Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Gabriel Quintero, Ming You, Haengsoon Park, Yingchun Lu
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Patent number: 7884100Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in 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: June 12, 2007Date of Patent: February 8, 2011Assignee: PGxHealth, LLCInventors: Guoquan Wang, Robert D. Thompson, Jayson M. Rieger
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Publication number: 20110028715Abstract: A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straightened or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 14, 2010Publication date: February 3, 2011Applicants: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca AktiebolagInventors: Yoshiaki ISOBE, Tomoaki NAKAMURA
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Patent number: 7875608Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in 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: December 17, 2008Date of Patent: January 25, 2011Inventors: Robert D. Thompson, Guoquan Wang, Anthony Beauglehole, Frank Schmidtmann
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Publication number: 20110015193Abstract: The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterised by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X independently of each other being selected from C2-C6-alky1 or Ci-C6-alkoxy, where C2-C6-alkyl and C1-C6-alkoxy are at least dihalogenated up to perhalogenated. preferably with 2 to 6 halogen substituents, and the halogen atoms being selected from the group of fluoro, chloro and bromo, preferably fluoro; R2 being phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C1-C6-alkyI, C1-C6-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl. C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl.Type: ApplicationFiled: November 27, 2008Publication date: January 20, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian Eickmeier, Cornelia Dorner-Ciossek, Dennis Fiegen, Thomas Fox, Klaus Fuchs, Riccardo Giovannini, Niklas Heine, Martin Hendrix, Holger Rosenbrock, Gerhard Schaenzle
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Publication number: 20110015190Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).Type: ApplicationFiled: December 4, 2008Publication date: January 20, 2011Inventors: Xianhai Huang, Anandan Palani, Jun Qin, Robert Aslanian, Zhaoning Zhu, William Greenlee, Hubert Josien, Wei Zhou, Xiaohong Zhou, Chad E. Bennett, Dmitri Pissarnitski, Mihirbaran Mandal, Pawan Dhondi, Troy McCracken, Thomas Bara, Zhiqiang Zhao, Duane Burnett, John Clader
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Publication number: 20110009403Abstract: The present invention relates to purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with mTOR kinases.Type: ApplicationFiled: October 3, 2008Publication date: January 13, 2011Applicant: S*BIO Pte Ltd.Inventors: Harish Kumar Mysore Nagaraj, DiZhong Chen, Anders Poulsen, Meredith Williams
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Publication number: 20110009405Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.Type: ApplicationFiled: July 6, 2010Publication date: January 13, 2011Applicant: Pathway Therapeutics LimitedInventors: Gordon William Rewcastle, Kit Yee Tsang, Swarnalatha Akuratiya Gamage, Anna Claire Giddens
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Publication number: 20100324040Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: May 2, 2008Publication date: December 23, 2010Applicant: ASTRAZENECA ABInventors: Audrey Davies, Stephanos Ioannidis, Michelle Lamb, Mei Su, Tao Wang, Hai-Jun Zhang
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Patent number: 7851468Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).Type: GrantFiled: May 14, 2007Date of Patent: December 14, 2010Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner