Bicyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/349)
  • Patent number: 10047086
    Abstract: The present invention is directed to imidazo[1,5-a]pyridine and imidazo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: May 31, 2017
    Date of Patent: August 14, 2018
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Leah C. Konkol, Neil Lajkiewicz, Liang Lu, Meizhong Xu, Wenqing Yao, Zhiyong Yu, Colin Zhang, Chunhong He
  • Patent number: 9937172
    Abstract: A mixture of heteropolycycles has preferably two particular heteropolycycles and more preferably, no more than 10 wt. %, 5 wt. %, 2.5 wt. %, 1 wt. %, 0.5 wt. %, 0.1 wt. %, 0.01 wt. %, 0.001 wt. %, or no more than a detectable amount of one of the two.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: April 10, 2018
    Inventor: Derek Alton Lightner
  • Patent number: 9193726
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: November 17, 2014
    Date of Patent: November 24, 2015
    Assignee: Pfizer Inc.
    Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Michael Eric Green, Nandini Chaturbhai Patel, Cory Michael Stiff, Tuan Phong Tran, Gregory Wayne Kauffman, Antonia Friederike Stepan, Patrick Robert Verhoest
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150141411
    Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Frederik Jan Rita Rombouts, Andres Avelino Trabanco-Suarez, Henricus Jacobus Maria Gijsen, Gregor James Macdonald, Francois Paul Bischoff, Sergio-Alvar Alonso-de-Diego, Adriana Ingrid Velter, Yves Emiel Maria Van Roosbroeck
  • Patent number: 9018209
    Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: April 28, 2015
    Assignee: Yale University
    Inventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
  • Patent number: 9018211
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Yuping Zhu, Aurash Shahripour, Haifeng Tang, Lihu Yang, Shawn P. Walsh, Nardos H. Teumelsan
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150099732
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
    Type: Application
    Filed: March 7, 2013
    Publication date: April 9, 2015
    Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
  • Patent number: 8999975
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2 and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are inhibitors of Cathepsin C.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters, Doris Riether, Wolfgang Wienen
  • Patent number: 8999981
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: April 7, 2015
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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 metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Patent number: 8987441
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: March 24, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
  • Patent number: 8987249
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
  • Patent number: 8981092
    Abstract: Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: March 17, 2015
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Danilo Mirizzi, Giovanni Cervi, Matteo D'Anello, Gianluca Mariano Enrico Papeo, Ron Ferguson, Francesco Casuscelli
  • Publication number: 20150072959
    Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20150057264
    Abstract: Compounds of the formula I in which R1, X and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Applicant: Merck Patent GmbH
    Inventors: Dieter Dorsch, Hans-Peter Buchstaller, Gerard Moinet, Ansgar Wegener
  • Patent number: 8962580
    Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: February 24, 2015
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
  • Patent number: 8962627
    Abstract: The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: February 24, 2015
    Assignee: Prestwick Chemical, Inc.
    Inventors: Stephan Schann, Stanislas Mayer, Christophe Morice, Bruno Giethlen
  • Patent number: 8952004
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: February 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
  • Patent number: 8946223
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, R1a, R1b, R1c, R1d, n, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: February 3, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Janice Chin, Kenneth M. Gigstad, He Xu
  • Publication number: 20150031876
    Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
    Type: Application
    Filed: September 5, 2014
    Publication date: January 29, 2015
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
  • Publication number: 20150018345
    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep
    Type: Application
    Filed: February 20, 2013
    Publication date: January 15, 2015
    Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding
  • Publication number: 20150018334
    Abstract: The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the aryl pyrazoles of the present invention, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Asitha ABEYWARDANE, John BROADWATER, Steven Richard BRUNETTE, Thomas Martin KIRRANE, JR., Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Qiang ZHANG
  • Publication number: 20150011556
    Abstract: There are provided compounds of the formula wherein R1 and R2 are as described herein. The compounds are useful as anticancer agents.
    Type: Application
    Filed: September 22, 2014
    Publication date: January 8, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Johannes Hermann, Ann Catherine Petersen, Jutta Wanner, Lin Yi
  • Patent number: 8916564
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: December 23, 2014
    Assignee: Pfizer Inc.
    Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Michael Eric Green, Nandini Chaturbhai Patel, Cory Michael Stiff, Tuan Phong Tran, Gregory Wayne Kauffman, Antonia Friederike Stepan, Patrick Robert Verhoest
  • Patent number: 8906911
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 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: Grant
    Filed: March 29, 2013
    Date of Patent: December 9, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
  • Publication number: 20140356360
    Abstract: The present invention relates to piperazinyl derivatives of formula (I) and the use thereof as a drug, particularly for the treatment of cancer, the pharmaceutical compositions containing said derivatives, and the method for synthesising same.
    Type: Application
    Filed: December 28, 2012
    Publication date: December 4, 2014
    Inventor: Marc-Henry PITTY
  • Patent number: 8895739
    Abstract: Functionalized bis-peptides as well as other amide-containing compounds are obtained by acylation of hindered amines. The functionalized bis-peptides are useful as shape-programmable nanostructures that are immune to denaturation and that contain arrays of functional groups having designed catalytic, protein-binding and/or sensor capabilities.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: November 25, 2014
    Assignees: Temple University of the Commonwealth System of Higher Education, University of Pittsburgh of the Commonwealth System of Higher Education
    Inventors: Christian E. Schafmeister, Zachary Z. Brown
  • Patent number: 8895560
    Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: November 25, 2014
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
  • Publication number: 20140336189
    Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Sylvain COTE-DES-COMBES, Jacques FROISSANT, Jean-Francois GIBERT, Frank MARGUET, Christophe PACAUD, Frederic PUECH, Antoine RAVET
  • Patent number: 8877743
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: November 4, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Publication number: 20140315880
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
  • Publication number: 20140296214
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: October 2, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Publication number: 20140249146
    Abstract: The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco Casuscelli, Alessandra Badari, Sten Christian Orrenius, Claudia Piutti, Teresa Disingrini
  • Publication number: 20140249129
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: February 20, 2014
    Publication date: September 4, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Patent number: 8822449
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Grant
    Filed: August 25, 2009
    Date of Patent: September 2, 2014
    Assignee: Sanofi
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Publication number: 20140243347
    Abstract: The present invention relates to substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 28, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco Casuscelli, Elena Casale, Marisa Montemartini, Claudia Piutti
  • Patent number: 8815869
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: August 26, 2014
    Assignee: AbbVie Inc.
    Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
  • Patent number: 8809427
    Abstract: Provided is a phthalocyanine compound which is halogen-free and which has a green hue, excellent resistance to organic solvents and acids, and high chroma. Also provided are a metal-free phthalocyanine compound or a metal phthalocyanine compound represented by specified general formula (1-1) or (1-2) and having a N,N?-disubstituted imidazolone structure or piperazinedione structure introduced therein, and a coloring composition including the compound and a synthetic resin. The phthalocyanine compound of the present invention exhibits a clear green color and is halogen-free, and is thus useful as a clear green pigment for coloring materials such as a coating material, plastic, a printing ink, rubber, leather, textile printing, a color filter, a jet ink, a heat transfer ink, etc.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: August 19, 2014
    Assignee: DIC Corporation
    Inventors: Hitoshi Kondou, Yoshiyuki Sano, Yutaka Tachikawa
  • Patent number: 8802694
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: August 12, 2014
    Assignee: Targacept, Inc.
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
  • Publication number: 20140221357
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 7, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20140221311
    Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3?, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I).
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Genesis M. Bacani, Wendy Eccles, Anne E. Fitzgerald, Steven D. Goldberg, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Alice Lee-Dutra, Jing Liu, Kelly J. McClure, Steven P. Meduna, Daniel J. Pippel, Mark D. Rosen, Zachary S. Sales
  • Patent number: 8796454
    Abstract: Herein we describe compositions and methods for the synthesis of [2.2.2]-diazabicyclic structures comprising a domino reaction sequence involving aldol condensation, alkene isomerization, and intramolecular hetero-Diels-Alder cycloaddition. Excellent diastereofacial control during the cycloaddition is enforced with a removable chiral phenyl aminal diketopiperazine substituent. The reaction sequence rapidly generates molecular complexity and is competent with both enolizable and non-enolizable aldehyde substrates. This method provides an efficient route to [2.2.2]-diazabicyclic structures, common to bioactive prenylated indole alkaloids such as the brevianamides and stephacidins.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: August 5, 2014
    Assignee: College of William and Mary
    Inventor: Jonathan R. Scheerer
  • Patent number: 8796257
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: August 5, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Patent number: 8791117
    Abstract: Embodiments of this invention provide methods for therapeutic use of cyclic G-2-Allyl Proline to treat cognitive disorders as well as manufacture of medicaments including tablets, capsules, injectable solutions that are useful for treatment of such conditions.
    Type: Grant
    Filed: March 8, 2011
    Date of Patent: July 29, 2014
    Assignee: Neuren Pharmaceuticals Limited
    Inventors: Michael John Bickerdike, Jian Guan
  • Patent number: 8791119
    Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Sanofi
    Inventors: Sylvain Cote Des Combes, Jacques Froissant, Jean-Francois Gibert, Frank Marguet, Christophe Pacaud, Frédéric Puech, Antoine Ravet
  • Publication number: 20140206680
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.
    Type: Application
    Filed: June 20, 2012
    Publication date: July 24, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Mark E. Adams, Rongliang Chen, Mitsunori Kono, Betty Lam, Matthew Lardy, Srinivasa Reddy Natala, Steven James Wilkens, Zhe Nie