The Additional Hetero Ring Is A 1,3-diazine Ring (including Hydrogenated) Patents (Class 514/263.21)
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Publication number: 20120003313Abstract: The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.Type: ApplicationFiled: September 12, 2011Publication date: January 5, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Anja KOHLRAUSCH, Patrick ROMER, Gerd SEIFFERT
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Publication number: 20110306622Abstract: This disclosure relates to methods of selecting a subset of subjects having a hematological disorder and treating the selected group with a PI3K-delta inhibitor. In particular, the methods disclose evaluating levels of characteristic chemokine biomarkers, such as CCL2, CCL3, CCL4, CCL5, CXCL13, CCL17, CCL22, or TNF-alpha to select subjects that would have a greater chance of benefiting from treatment with a PI3K-delta inhibitor. The PI3K-delta inhibitors disclosed in this application are a type of quinazolinone-purinyl family of compounds.Type: ApplicationFiled: June 10, 2011Publication date: December 15, 2011Applicant: Calitoga Pharmaceuticals, Inc.Inventors: Brian LANNUTTI, Langdon Miller, Heather Webb
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Publication number: 20110301182Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for improving glycemic control in type 2 diabetes patients with inadequate glycemic control despite metformin therapy.Type: ApplicationFiled: January 7, 2010Publication date: December 8, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Klaus Dugi
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Patent number: 8071609Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: August 11, 2006Date of Patent: December 6, 2011Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
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Publication number: 20110294803Abstract: Methods for treating CNS disorders such as schizophrenia, psychosis and cognitive disorders using specific inhibitors of phosphatidylinositol-3-kinase p110 delta (PIK3CD) expression and/or activity are described. Methods of determining risk of CNS disorders and methods of determining treatment response are also described. An integrative systems biology approach to identify a signaling mechanism and genetic network associated with schizophrenia and with schizophrenia-associated risk variation in ErbB4. A risk pathway associated with ErbB4 genetic variation involving increased expression of a PI3K-linked ErbB4 receptor CYT-1 and a specific PI3K enzyme, PIK3CD has been identified.Type: ApplicationFiled: December 4, 2009Publication date: December 1, 2011Inventors: Amanda J. Law, Daniel R. Weinberger
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Publication number: 20110275561Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients with insufficient glycemic control despite a therapy with an oral and/or a non-oral antidiabetic drug.Type: ApplicationFiled: October 15, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eva Ulrike Graefe-Mody, Thomas Klein, Michael Mark, Hans-Juergen Woerle
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Publication number: 20110263493Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.Type: ApplicationFiled: August 5, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
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Patent number: 8026244Abstract: There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.Type: GrantFiled: April 12, 2007Date of Patent: September 27, 2011Assignee: AstraZeneca ABInventors: Anna-Karin Tiden, Jenny Viklund
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Publication number: 20110230480Abstract: Compounds of the formula are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.Type: ApplicationFiled: May 27, 2011Publication date: September 22, 2011Inventors: 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: 20110206766Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and a partner drug, processes for the preparation thereof, and their use to treat certain diseases.Type: ApplicationFiled: April 2, 2009Publication date: August 25, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas Friedl, Michael Braun, Kenji Egusa, Hikaru Fujita, Megumi Maruyama, Takaaki Nishioka
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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: 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: 20110112069Abstract: The specification describes the use of selected purine derivatives for the treatment of hyperproliferative diseases.Type: ApplicationFiled: August 15, 2008Publication date: May 12, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Michael Mark, Mohammad Tadayyon, Leo Thomas
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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: 20110065731Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.Type: ApplicationFiled: November 15, 2010Publication date: March 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus DUGI, Frank HIMMELSBACH, Michael MARK
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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: 20110046165Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.Type: ApplicationFiled: January 5, 2009Publication date: February 24, 2011Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Katrina Chan, Christian Rommel, Liansheng Li
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Publication number: 20110044942Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.Type: ApplicationFiled: April 20, 2010Publication date: February 24, 2011Inventors: Kamal D. PURI, Jerry B. Evarts, Brian Lannutti, Neill A. Giese
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Patent number: 7879865Abstract: The present application is directed to a method of treating diseases of the central nervous system (CNS) comprising administering to a individual in need of treatment a therapeutically effective amount of an inhibitor of histone deacetylase. In particular embodiments, the CNS disease is a neurodegenerative disease. In further embodiments, the neurogenerative disease is an inherited neurodegenerative disease, such as those inherited neurodegenerative diseases which are polyglutamine expansion diseases. The individual can be a mammal such as a primate or human.Type: GrantFiled: November 18, 2005Date of Patent: February 1, 2011Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Victoria M. Richon, Paul A. Marks, Richard A. Rifkind
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Publication number: 20110021541Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: November 12, 2008Publication date: January 27, 2011Inventors: Stephen L. White, Fuqiang Ruan, Edward A. Kesicki, Eugene Thorsett, Francine Farouz
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Publication number: 20110014196Abstract: The invention relates to compounds comprising a plurality of enzyme substrates suitably linked and further carrying one or more cargo entities. In particular such compounds have the structure (substrate)n-linker-(cargo)m wherein “substrate” is a substrate specific for an enzyme-type protein; n is 2 or more; “linker” is a linking unit consisting of 1 to 300 atoms; “cargo” is a drug, a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, or a functional group which can be transformed into a drug or a detectable label; and m is 1 or more. The invention further relates to a corresponding molecular shuttles having the structure (fusion protein)n-linker-(cargo)m wherein “fusion protein” is a proteinaceous binding entity fused to an enzyme-type protein for which specific substrates exist. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.Type: ApplicationFiled: October 2, 2008Publication date: January 20, 2011Applicant: COVALYS BIOSCIENCES AGInventors: Andreas Brecht, Florent Beaufils
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Publication number: 20100324047Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: June 5, 2008Publication date: December 23, 2010Applicant: AMGEN INC.Inventors: Adrian L. Smith, Elizabeth M. Doherty, Qi Huang, Gang Liu
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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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Publication number: 20100286126Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: ApplicationFiled: April 19, 2007Publication date: November 11, 2010Applicant: NOVARTIS AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20100256167Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: March 25, 2010Publication date: October 7, 2010Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg
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Publication number: 20100256168Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: March 25, 2010Publication date: October 7, 2010Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg
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Publication number: 20100249155Abstract: The invention provides compounds, compositions and methods to treat certain inflammatory conditions and/or oncology by administering a compound that inhibits PI3K isoforms, particularly the delta isoform. It further provides specific stereoisomers of a compound useful for these methods. In particular, the compound is an optically active atropisomer of 2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one.Type: ApplicationFiled: March 24, 2010Publication date: September 30, 2010Inventors: Jerry B. Evarts, Roger G. Ulrich
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Publication number: 20100209506Abstract: The present invention relates to pharmaceutical compositions of linagliptin, pharmaceutical dosage forms, their preparation, their use and methods for treating metabolic disorders.Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Wolfram EISENREICH
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Publication number: 20100204172Abstract: Disclosed are compounds that are AGT inactivators that include a folate residue, e.g., a compound of formula (I), wherein X1, X2, R1, and R2 are as described herein. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells and inactivating AGT in a tumor cell. The methods comprise, inter alia, administering a compound or pharmaceutically acceptable salt of formula (I).Type: ApplicationFiled: March 12, 2008Publication date: August 12, 2010Applicants: Department of Health and Human Services, The Penn State Research FoundationInventors: Robert C. Moschel, Anthony E. Pegg, Sahar Javanmard, Natalia Loktionova, Gary Pauly
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Publication number: 20100202963Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient.Type: ApplicationFiled: November 13, 2009Publication date: August 12, 2010Inventors: W. Michael GALLATIN, Roger G. Ulrich, Neill A. Giese
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Patent number: 7772226Abstract: 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: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: 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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Publication number: 20100190784Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, wherein, R1a, R1b, R2a, R2b, U1, U2, X1, X2 and L are as defined herein.Type: ApplicationFiled: April 19, 2007Publication date: July 29, 2010Inventors: Robin Alec Fairhurst, Roger John Taylor
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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: 20100168139Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: October 7, 2009Publication date: July 1, 2010Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Publication number: 20100152211Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: October 7, 2009Publication date: June 17, 2010Inventors: Chanchal SADHU, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Patent number: 7732455Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provided. These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: December 14, 2007Date of Patent: June 8, 2010Assignee: PGx Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20100129311Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100029693Abstract: The present invention relates generally to phosphoinositide 3-kinases (PI3Ks), and more particularly to specific, selective, improved PI3K? inhibitors and methods of inhibiting undesirable levels of PI3K? activity using these PI3K? inhibitors to treat disorders mediated by PI3K?.Type: ApplicationFiled: August 10, 2009Publication date: February 4, 2010Inventors: Jason DOUANGPANYA, Joel S. Hayflick, Kamal D. Puri
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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: 20100004236Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: ApplicationFiled: February 26, 2009Publication date: January 7, 2010Inventors: Ashok Tehim, Allen T. Hopper, Ruiping Liu, Hans-Juregen Ernst Hess, Yajing Rong
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Publication number: 20090325967Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, formula (1), or stereoisomers or pharmaceutically acceptable salts thereof, wherein A, U1, U2, R1a, R1b, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: September 13, 2007Publication date: December 31, 2009Inventors: Robin Alec Fairhurst, Roger John Taylor
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Publication number: 20090325982Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: ApplicationFiled: September 4, 2009Publication date: December 31, 2009Inventors: Allen T. HOPPER, Ruiping LIU
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Patent number: 7618962Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: February 27, 2006Date of Patent: November 17, 2009Assignee: PGX Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7601723Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: February 27, 2006Date of Patent: October 13, 2009Assignee: PGx Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20090215798Abstract: The present invention relates to compounds and uses of compounds which interact with chitinase enzymes, in particular inhibition of those enzymes.Type: ApplicationFiled: June 21, 2006Publication date: August 27, 2009Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Danile Marinus Ferdinand Van Aalten, Ian Michael Eggleston
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Patent number: 7579348Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: February 27, 2006Date of Patent: August 25, 2009Assignee: PGxHealth, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20090181934Abstract: A composition comprising, separately or together: a component (A) that is an adenosine A2a receptor agonist as defined in the specification; and a component (B) that is one or more compounds selected from: (i) a corticosteroid, (ii) a beta-2 adrenoceptor agonist, (iii) an antimuscarinic agent, (iv) an A2B antagonist, (v) an antihistamine, (vi) a caspase inhibitor, (vii) an ENaC inhibitor, (viii) an LTB4 antagonist, (ix) an LTD4 antagonist, (x) a serine protease inhibitor, (xi) a PDE4 inhibitor and (xii) a dual-acting beta-2 adrenoceptor agonist/muscarinic antagonist, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.Type: ApplicationFiled: October 8, 2008Publication date: July 16, 2009Inventor: Robin Alec FAIRHURST