Patents Examined by Cecilia M. Jaisle
  • Patent number: 8710057
    Abstract: The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: April 29, 2014
    Assignee: Tolero Pharmaceuticals, Inc.
    Inventors: David J. Bearss, Xiao-Hui Liu, Hariprasad Vankayalapati, Yong Xu
  • Patent number: 8710058
    Abstract: Compounds of the present invention concern 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The compound, 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile, has the following structural formula: The hydrochloride solvates and crystalline modifications thereof according to the invention are useful for treatment of physiological and/or pathophysiological conditions, such as cancer, that are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, especially Met-kinase. The present invention further relates to processes of manufacturing these crystalline modifications.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: April 29, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz Hermann Bokel, Frank Stieber, Cristina Donini
  • Patent number: 8703768
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • Patent number: 8697866
    Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: April 15, 2014
    Assignee: Xcovery Holding Company LLC
    Inventors: Congxin Liang, Zhigang Li
  • Patent number: 8680101
    Abstract: The invention relates to a pharmaceutical composition containing pimobendan as an active ingredient. The invention also relates to a crystalline form of pimobendan, as well as to a combination of said crystalline form with at least one other therapeutically active ingredient. Moreover, the invention relates to uses of said crystalline form, as well as to a pharmaceutical composition containing it. Finally, the invention relates to a process for preparing a crystalline form of pimobendan.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: March 25, 2014
    Assignee: Eurovet Animal Health B.V.
    Inventors: Marinus Maria Martinus Boeren, Rudolf Johannes Paridaans, Sanita Petkune, Viesturs Lusis, Dzintra Muceniece
  • Patent number: 8673917
    Abstract: The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes.
    Type: Grant
    Filed: September 2, 2009
    Date of Patent: March 18, 2014
    Assignee: Sanofi
    Inventors: Gerhard Zoller, Marc Dietrich Voss, Hans Matter, Andreas Herling
  • Patent number: 8673916
    Abstract: The present invention is directed to methods of treating disorders mediated by Histamine H3 receptors by administering novel pyridazinone derivatives. In particular, the pyridazinone compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: March 18, 2014
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
  • Patent number: 8669254
    Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 11, 2014
    Assignee: Hoffman-La Roche Inc.
    Inventors: Paul Hebeisen, Stephan Roever
  • Patent number: 8664222
    Abstract: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallization in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: March 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenter Linz, Peter Sieger, Matthias Grauert, Rolf Schmid
  • Patent number: 8653077
    Abstract: 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: Grant
    Filed: September 28, 2011
    Date of Patent: February 18, 2014
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Kennith O. Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 8653262
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Grant
    Filed: May 29, 2008
    Date of Patent: February 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Silke Hobbie
  • Patent number: 8653091
    Abstract: Fused heterocyclic compounds are provided according to formula 1a or 1b: where R1, R2, and R3 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: February 18, 2014
    Assignee: Evotec AG
    Inventors: Zhi-Liang Wei, John Kincaid, Michael G. Kelly, Donogh John Roger O'Mahony, Carl Kaub
  • Patent number: 8653076
    Abstract: The invention relates to novel inhibitors of kinases of the general formula (I): in which Q and R1 are defined in the claims, method for preparing such inhibitors, intermediates for preparing such inhibitors and uses of such inhibitors.
    Type: Grant
    Filed: June 20, 2007
    Date of Patent: February 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Olaf Prien, Knut Eis, Benjamin Bader, Judith Guenther, Arne Von Bonin
  • Patent number: 8648088
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3?, R4, and R4? are as defined herein or to a pharmaceutically acceptable 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).
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: February 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 8637511
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: January 28, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sham Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
  • Patent number: 8637518
    Abstract: Compounds of the formula (I), in which Y, R1, R2, R3 and R3? 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: Grant
    Filed: November 24, 2009
    Date of Patent: January 28, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Patent number: 8637513
    Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Patent number: 8633211
    Abstract: A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: January 21, 2014
    Assignee: Novartis AG
    Inventor: Roger John Taylor
  • Patent number: 8629155
    Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: January 14, 2014
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
  • Patent number: 8623862
    Abstract: The present invention relates to compounds corresponding to formula (I): X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: January 7, 2014
    Assignee: Sanofi
    Inventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon