Phthalazines (including Hydrogenated) Patents (Class 544/237)
  • Patent number: 8129380
    Abstract: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl, which groups are optionally substituted; or RC and R1 together with the carbon and oxygen atoms to which they are attached form a spiro-C5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C5-7 aromatic ring.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: March 6, 2012
    Assignee: AstraZeneca AB
    Inventors: Keith Allan Menear, Muhammad Hashim Javaid, Sylvie Gomez, Marc Geoffrey Hummersone, Carlos Fenandez Lence, Niall Morrison Barr Martin, David Alan Rudge, Craig Anthony Roberts, Kevin Blades
  • Publication number: 20120053181
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: April 28, 2010
    Publication date: March 1, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Publication number: 20120046267
    Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
    Type: Application
    Filed: February 11, 2011
    Publication date: February 23, 2012
    Inventors: Keith R. Hornberger, Dan M. Berger, Xin Chen, Andrew P. Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Lifu Ma, Mark J. Mulvihill, Bijoy Panicker, Kam W. Siu, Arno G. Steinig, James G. Tarrant, Jing Wang, Qinghua Weng, Rajaram Sangem, Ramesh C. Gupta
  • Patent number: 8119635
    Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: February 21, 2012
    Assignee: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
  • Publication number: 20120040949
    Abstract: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Application
    Filed: August 11, 2011
    Publication date: February 16, 2012
    Inventors: Steven Joseph Berthel, Roland Joseph Billedeau, Christine E. Brotherton-Pleiss, Fariborz Firooznia, Stephen Deems Gabriel, Xiaochun Han, Ramona Hilgenkamp, Saul Jaime-Figueroa, Buelent Kocer, Francisco Javier Lopez-Tapia, Yan Lou, Lucja Orzechowski, Timothy D. Owens, Jenny Tan, Peter Michael Wovkulich
  • Publication number: 20120040983
    Abstract: 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 A4, L, R1, R2, R3, R5 and m are as 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, ankylosing spondylitis, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Application
    Filed: October 7, 2009
    Publication date: February 16, 2012
    Applicant: Amgen Inc.
    Inventors: Andrew Tasker, James R. Falsey, Robert M. Rzasa, Bradley J. Herberich, Dawei Zhang
  • Patent number: 8106047
    Abstract: 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: Grant
    Filed: January 4, 2006
    Date of Patent: January 31, 2012
    Assignee: NYCOMED GmbH
    Inventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Külzer, Hermann Tenor, Hans-Peter Kley
  • Patent number: 8101612
    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of p38 kinase mediated diseases and related inflammatory conditions. The compounds have a general Formula II wherein L1, L2, R1a, R1b, R1c, R2, R3, R3a, R4, R5 and p 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 kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Grant
    Filed: September 4, 2007
    Date of Patent: January 24, 2012
    Assignee: Amgen Inc.
    Inventors: Andrew Tasker, Dawei Zhang, Liping H. Pettus, Rob M. Rzasa, Kelvin K. C. Sham, Shimin Xu, Partha Chakrabarti
  • Publication number: 20120015950
    Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or o
    Type: Application
    Filed: November 13, 2009
    Publication date: January 19, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
  • Patent number: 8097627
    Abstract: The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: January 17, 2012
    Assignee: Bayer Pharma AG
    Inventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
  • Publication number: 20120004234
    Abstract: This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
    Type: Application
    Filed: February 4, 2010
    Publication date: January 5, 2012
    Applicant: Schering Corporation
    Inventors: Jason L. Davis, Michael John Mayer, Hubert B. Josien
  • Publication number: 20110312936
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
  • Publication number: 20110301347
    Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.
    Type: Application
    Filed: August 15, 2011
    Publication date: December 8, 2011
    Inventors: Markus BERGER, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schäcke
  • Publication number: 20110301162
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-6, L1, R1, R4-6 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinase proteins. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds and methods of treating disease states related to the activity of Aurora kinase.
    Type: Application
    Filed: August 4, 2009
    Publication date: December 8, 2011
    Applicant: AMGEN INC.
    Inventors: Holly L. Deak, Stephanie D. Geuns-Meyer, Jason Brooks Human, Matthew W. Martin, Isaac Marx
  • Patent number: 8063070
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: November 22, 2011
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Publication number: 20110275792
    Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.
    Type: Application
    Filed: July 15, 2011
    Publication date: November 10, 2011
    Inventor: Thomas Piccariello
  • Publication number: 20110275642
    Abstract: The invention is related to a method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals of the formula II wherein 5-nitro-2,3-dihydrophthalazine-1,4-dione is solved in water solution of MOH1 where M has the below mentioned meaning, with formation of solution of 5-nitro-2,3-dihydrophthalazine-1,4-dione alkali metal salt, which is catalytically transformed into 5-amino-2,3-dihydrophthalazine-1,4-dione salt at the temperature 40-900C by means of hydrogen under the pressure 1-4 MPa in at the presence of a transition metal catalyst (Pt, Pd) on activated carbon, and separation of crystalline 5-amino-2,3-dihydrophthalazine-1,4-dione salt is performed by water solution diluting with lower alcohol or cyclic lower ether with cooling to the temperature ?5° C. to ?15° C., providing that there is used 5-nitro-2,3-dihydrophthalazine-1,4-dione formed in the reaction of anhydride of 3-nitrophthalic acid with hydrazine hydrate in anhydrous acetic acid at the temperature 100-110° C.
    Type: Application
    Filed: January 15, 2010
    Publication date: November 10, 2011
    Applicant: Abidopharma PL SP. Z.O.O.
    Inventors: Admir Musaevich Abidov, Aleksei Silantievich Ishmuratov, Vitalij Vilkin, Irina Georgievna Danilova
  • Publication number: 20110269722
    Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.
    Type: Application
    Filed: December 23, 2010
    Publication date: November 3, 2011
    Inventor: Apparao Satyam
  • Publication number: 20110263530
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Application
    Filed: June 28, 2011
    Publication date: October 27, 2011
    Applicant: Amgen Inc.
    Inventors: Victor J. CEE, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
  • Patent number: 8044242
    Abstract: The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
    Type: Grant
    Filed: March 8, 2007
    Date of Patent: October 25, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alexandra A. Nirschl, Xiaojun Zhang
  • Patent number: 8044041
    Abstract: The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives of formula (III) that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: October 25, 2011
    Assignee: Forest Laboratories Holdings Limited
    Inventors: Gian-Luca Araldi, Matthew Ronsheim, Melanie Ronsheim
  • Publication number: 20110257187
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, Y, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Application
    Filed: April 14, 2011
    Publication date: October 20, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Alexander R. Shoemaker, Thomas D. Penning, Jianchun Gong
  • Publication number: 20110250145
    Abstract: Methods of imaging distribution of myeloperoxidase activity in a subject are disclosed. These methods include the use of bioluminescent substrates, including luminol and wavelength-shifted analogues of luminol. Bioluminescent myeloperoxidase substrates that emit light at longer wavelengths compared to luminol are shown to be useful for imaging myeloperoxidase activity in vivo. The disclosed methods can be used for imaging sites of inflammation and other pathological conditions associated with abnormal levels of MPO activity in vivo. Methods of synthesis of luminol analogues are also disclosed.
    Type: Application
    Filed: November 3, 2009
    Publication date: October 13, 2011
    Applicant: Washington University
    Inventors: Vijay Sharma, Seth Gammon, David Piwnica-Worms, Shimon Gross
  • Publication number: 20110237571
    Abstract: The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Application
    Filed: June 1, 2011
    Publication date: September 29, 2011
    Inventors: Gian-Luca Araldi, Matthew Ronsheim, Melanie Ronsheim
  • Publication number: 20110196153
    Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.
    Type: Application
    Filed: February 8, 2011
    Publication date: August 11, 2011
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Quan Jiang, Lei Lu
  • Publication number: 20110190304
    Abstract: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
    Type: Application
    Filed: October 22, 2009
    Publication date: August 4, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Jolie Anne Bastian, Philip Arthur Hipskind, Daniel Jon Sall, Takako Wilson (nee Takakuwa)
  • Publication number: 20110183985
    Abstract: The present invention provides fused aryl and heteroaryl derivatives of Formula I: wherein X, V, Y, U, W, Z, R1, R2, Cy, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: December 17, 2010
    Publication date: July 28, 2011
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Hui-Yin Li
  • Patent number: 7985762
    Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3—NS4A protease.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: July 26, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
  • Patent number: 7981891
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: July 19, 2011
    Assignee: Amgen Inc.
    Inventors: Holly Deak, Stephanie Geuns-Meyer, Brian L. Hodous, Zihao Hua, Mathew Martin, Hanh Nho Nguyen, Philip Olivieri, Kate Panter, Karina Romero, Laurie Schenkel, Ryan White
  • Patent number: 7981892
    Abstract: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: July 19, 2011
    Assignee: Eli Lilly and Company
    Inventors: Philip Arthur Hipskind, Takako Wilson (nee Takakuwa)
  • Patent number: 7981890
    Abstract: A compound of the formula (I): wherein RH represents one or more optional substituents on the fused cyclohexene ring; R1 is selected from H and halo; RN is selected from H and optionally substituted C1-10 alkyl; and RC1 and RC2 are independently selected from H, R, C(?O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: July 19, 2011
    Assignee: AstraZeneca AB
    Inventors: Muhammad Hashim Javaid, Keith Allan Menear, Niall Morrison Barr Martin
  • Patent number: 7981889
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: July 19, 2011
    Assignees: Kudos Pharmaceuticals Limited, Maybridge Limited
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • Patent number: 7977333
    Abstract: Substituted and pyridines and pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1 and R2 may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using these materials are also disclosed.
    Type: Grant
    Filed: November 24, 2003
    Date of Patent: July 12, 2011
    Assignee: Bayer Healthcare LLC
    Inventors: Jacques P. Dumas, Stephen J. Boyer, Julie A. Dixon, Teddy K. Joe, Harold C. E. Kluender, Wendy Lee, Dhanapalan Nagarathnam, Robert N. Sibley, Ning Su
  • Publication number: 20110165120
    Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.
    Type: Application
    Filed: February 28, 2011
    Publication date: July 7, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
  • Publication number: 20110160187
    Abstract: The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.
    Type: Application
    Filed: May 6, 2005
    Publication date: June 30, 2011
    Applicant: Neurogen Corporation
    Inventors: Taeyoung Yoon, Jun Yuan, Kyungae Lee, George D. Maynard, Nian Liu
  • Publication number: 20110130399
    Abstract: The invention relates to new phthalazine derivatives of formula I, and to processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment especially of a disease that responds to the inhibition of especially the vascular endothelial growth factor receptor kinase, preferably the treatment of a proliferative disease, or the treatment of inflammatory rheumatic or rheumatoid arthritis and/or pain; and the use of such a compound alone or in combination with one or more other pharmaceutically active compounds for the manufacture of a pharmaceutical preparation for the treatment of said diseases in an animal.
    Type: Application
    Filed: November 24, 2010
    Publication date: June 2, 2011
    Applicant: NOVARTIS AG
    Inventors: Guido BOLD, Paul William MANLEY
  • Publication number: 20110124642
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring Z1, R1, p, R3, and R4 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: November 18, 2010
    Publication date: May 26, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Brian S. Brown, Tongmei Li, Arturo Perez-Medrano, Sridhar Peddi
  • Publication number: 20110105329
    Abstract: Substituted quinolinones of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one compound of the formula I to act on plants, their seed and/or their habitat.
    Type: Application
    Filed: October 29, 2010
    Publication date: May 5, 2011
    Applicant: BASF SE
    Inventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree van der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska, Anja Simon, Richard Roger Evans
  • Publication number: 20110105509
    Abstract: Disclosed are compounds of Formula (I): which are useful as antagonists of the CRTH2 receptors. Pharmaceutical compositions containing compounds of Formula (I) and the use of compounds of Formula (I) to treat diseases or disorders that are responsive to inhibition of the binding of endogenous ligands to the CRTH2 receptor are also disclosed. Methods for preparing and using these compounds are further described.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 5, 2011
    Applicant: Wyeth, LLC
    Inventors: Neelu Kaila, Eddine Saiah, Bruce Christopher Follows, Adrian Huang, Kristin Marie Janz, Michael Dennis Lowe, Alessandro Fabio Moretto, Jennifer Romanic Thomason, Tarek Suhayl Mansour, Cara Margaret May Williams
  • Publication number: 20110098304
    Abstract: Componds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such componds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.
    Type: Application
    Filed: November 19, 2009
    Publication date: April 28, 2011
    Inventors: Bijoy Panicker, Dawoon Jung, Xiaokang Zhu, David E. Smith, Dong Sung Lim
  • Publication number: 20110098305
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: May 20, 2009
    Publication date: April 28, 2011
    Inventors: Jonathan Bayldon Baell, Guillaume Laurent Lessene, Brad Edmund Sleebs, Wayne Fairbrother, John Flygare, Michael F.T. Koehler
  • Patent number: 7915410
    Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: March 29, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, Yoon Jeon, John Lloyd, Heather Finlay
  • Publication number: 20110071141
    Abstract: Condensed-ring aryl compounds of formula (I) and use of the same as a agrochemical for controlling noxious organisms wherein (X)mQ, A, R1, (Y)n and the grouping —W1—W2—W3—W4— are as defined herein.
    Type: Application
    Filed: March 13, 2009
    Publication date: March 24, 2011
    Inventors: Tetsuya Murata, Yasushi Yoneta, Jun Mihara, Kei Domon, Mamoru Hatazawa, Koichi Araki, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Ulrich Görgens, Arnd Voerste, Angela Becker, Eva-Maria Franken, Klaus-Helmut Müller
  • Publication number: 20110065709
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D?, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
    Type: Application
    Filed: March 19, 2009
    Publication date: March 17, 2011
    Applicant: Amgen Inc.
    Inventors: Ryan White, Jason Human
  • Publication number: 20110065684
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, L1, L2, X, Y, Q and Z have defined meanings.
    Type: Application
    Filed: August 13, 2010
    Publication date: March 17, 2011
    Inventors: Laurence Anne Mevellec, Ludo E.J. Kennis, Josephus Carolus Mertens, Jacobus A.J. Van Dun, Maria V.F. Somers, Walter B.L. Wouters
  • Patent number: 7902194
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: March 8, 2011
    Assignee: Roche Palo Alto
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Patent number: 7902193
    Abstract: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C?O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(?O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: March 8, 2011
    Assignee: Maybridge Limited
    Inventors: Muhammad Hashim Javaid, Keith Allan Menear, Sylvie Gomez, Marc Geoffrey Hummersone, Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Xiao-Ling Fan Cockcroft, Frank Kerrigan
  • Publication number: 20110054171
    Abstract: Salts of optically active [4-(2-diphenylphosphanylnaphthalen-1-yl)phthalazin-1-yl]-(1-phenylethyl)amines represented by the formulas (1) to (4) with an optically active organic sulfonic acid, and a production method thereof.
    Type: Application
    Filed: January 14, 2009
    Publication date: March 3, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Erick M. Carreira, Shoji Fukuyo, Hiroshi Kadono, Kazuo Murakami
  • Publication number: 20110046143
    Abstract: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
    Type: Application
    Filed: April 1, 2009
    Publication date: February 24, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Philip Arthur Hipskind, Takako Wilson (nee Takakuwa)
  • Publication number: 20110034450
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: April 6, 2009
    Publication date: February 10, 2011
    Applicant: BAYER SCHERING PHARMA AKTIEGESELLSCHAFT
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li