The Additional Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/61)
  • Publication number: 20150045324
    Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Applicant: HANMI SCIENCE CO., LTD
    Inventors: Mi Young CHA, Seok Jong KANG, Mi Ra KIM, Ju Yeon LEE, Ji Young JEON, Myoung Gi JO, Eun Joo KWAK, Kwang Ok LEE, Tae Hee HA, Kwee Hyun SUH, Maeng Sup KIM
  • Publication number: 20150031689
    Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 29, 2015
    Inventors: Rangan Maitra, Alan Bradley Fulp, Yanan Zhang, Herbert H. Seltzman
  • Publication number: 20150031678
    Abstract: The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 29, 2015
    Applicant: LABORATORIES DEL DR. ESTEVE S.A.
    Inventors: José Luis Diaz Fernández, Ma Rosa Cuberes Altisent
  • Publication number: 20150018309
    Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: February 23, 2013
    Publication date: January 15, 2015
    Inventors: Craig W Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, James C. Tarr, James M. Salovich
  • Publication number: 20150011752
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Application
    Filed: September 4, 2014
    Publication date: January 8, 2015
    Inventors: Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
  • Patent number: 8906913
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: December 9, 2014
    Assignee: Panacea Biotec Limited
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Publication number: 20140330008
    Abstract: The present invention relates to a process for the preparation of 2-amino-pyrimidine-5-boronic acid of formula (I). or salts or esters thereof.
    Type: Application
    Filed: May 5, 2014
    Publication date: November 6, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Torsten Busch, Michael Nonnenmacher
  • Patent number: 8853199
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: October 7, 2014
    Assignees: Array Biopharma, Inc., Genentech, Inc.
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlachter, Anna L. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
  • Publication number: 20140288046
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 25, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • 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: 8815926
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: August 26, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Lv Liao, Robert Mah, Liang Mao, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20140228352
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Publication number: 20140221333
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: July 19, 2012
    Publication date: August 7, 2014
    Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
  • Publication number: 20140213549
    Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.
    Type: Application
    Filed: July 8, 2011
    Publication date: July 31, 2014
    Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
  • Publication number: 20140194414
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 10, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Publication number: 20140113882
    Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 24, 2014
    Applicants: Cancer Research Technology Limited, Cephalon, Inc.
    Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
  • Publication number: 20140005183
    Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Application
    Filed: June 27, 2013
    Publication date: January 2, 2014
    Inventors: Paul Galatsis, Matthew Merrill Hayward, Bethany Lyn Kormos, Travis T. Wager, Lei Zhang, Antonia Friederike Stepan, Jaclyn Louise Henderson, Ravi G. Kurumbail, Patrick Robert Verhoest
  • Publication number: 20140005143
    Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.
    Type: Application
    Filed: July 8, 2011
    Publication date: January 2, 2014
    Applicants: Daiichi Sankyo Company, Limited, Ube Industries, Ltd.
    Inventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
  • Publication number: 20130338153
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 19, 2013
    Applicant: AFRAXIS, INC.
    Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
  • Publication number: 20130331378
    Abstract: A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as a therapeutic agent for lower urinary tract symptoms (LUTS), particularly, overactive bladder syndrome (OABs), or a prophylactic agent therefor and furthermore, is also useful in the treatment, prevention, or suppression of various pathological conditions in which the EP1 receptor is involved, such as inflammatory disease, pain disease, osteoporosis, and cancer. [A is a benzene ring or the like, Y1 is C1-6 alkylene, R1 is —C(?O)—OZ1 or the like, Z1 is H or the like, R2 is a branched C3-6 alkyl group or the like, R3 is H or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like].
    Type: Application
    Filed: January 25, 2012
    Publication date: December 12, 2013
    Applicants: KISSEI PHARMACEUTICAL CO., LTD., KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Shigeki Seto, Kentaro Umei, Yosuke Nishigaya, Asao Tanioka, Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
  • Patent number: 8586576
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: November 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc Labroli, Kartik M. Keertikar
  • Patent number: 8580782
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or compositions.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: November 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc A. Labroli, Kartik M. Keertikar
  • Patent number: 8569504
    Abstract: For the prevention and/or treatment of chymase-mediated diseases such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like, a drug is provided having as an active ingredient a compound having extremely strong chymase inhibitory activity, high safety, and high metabolic stability. The compound represented by the formula (I): wherein all symbols have the same meanings as in the description, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a pharmaceutical ingredient having chymase inhibitory activity for preventing and/or treating of chymase-mediated disease, such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: October 29, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Jun Takeuchi, Takayuki Inukai, Masaru Sakai
  • Patent number: 8518945
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: August 27, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
  • Patent number: 8476278
    Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: July 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Panduranga Adulla P. Reddy, Tzu T. Wong, Lianyun Zhao, Shuyi Tang, Marc A. Labroli, Timothy J. Guzi, M. Arshad Siddiqui
  • Patent number: 8445675
    Abstract: Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabilizer, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: May 21, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Detlef Mohr, Claus Veit, Fridtjof Traulsen
  • Publication number: 20130116236
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: November 6, 2012
    Publication date: May 9, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8435980
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y 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: Grant
    Filed: July 15, 2010
    Date of Patent: May 7, 2013
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Jane Gong, Magdalena Przytulinska, Douglas Steinman, James Holms, Chunqiu Lai, Gui-Dong Zhu, Keith Woods
  • Publication number: 20130109653
    Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.
    Type: Application
    Filed: July 8, 2011
    Publication date: May 2, 2013
    Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
  • Publication number: 20130109670
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Application
    Filed: December 18, 2012
    Publication date: May 2, 2013
    Applicant: PFIZER INC.
    Inventor: PFIZER INC.
  • Publication number: 20130029969
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: February 16, 2011
    Publication date: January 31, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Misaki Homma, Toru Miyazaki, Yuya Oguro, Osamu Kurasawa
  • Publication number: 20120329780
    Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
    Type: Application
    Filed: April 23, 2012
    Publication date: December 27, 2012
    Applicant: Origenis GmbH
    Inventors: Michael Thormann, Andreas Treml, Michael Almstetter, Nadine Traube
  • Patent number: 8338590
    Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substitutes A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: December 25, 2012
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Hervé Geneste, Andrea Hager-Wernet, legal representative
  • Patent number: 8268994
    Abstract: The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: September 18, 2012
    Assignee: SGX Pharmaceuticals, Inc.
    Inventors: William D. Arnold, Pierre Bounaud, Chixu Chen, Brian Eastman, Andreas Gosberg, Stefan N. Gradl, Stephanie Hopkins, Zhe Li, Ian McDonald, Paul A. Sprengeler, Ruo W. Steensma, Mark E. Wilson
  • Patent number: 8258129
    Abstract: The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are as defined in the disclosure, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: September 4, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
  • Publication number: 20120220566
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
    Type: Application
    Filed: October 15, 2010
    Publication date: August 30, 2012
    Applicant: Rib-X Pharmaceuticals, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
  • Patent number: 8211892
    Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives of Formula (I): as disclosed herein, to their preparation and to their therapeutic application.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: July 3, 2012
    Assignee: Sanofi-Aventis
    Inventors: Alain Jean Braun, Olivier Crespin, Claudie Namane, Eric Nicolai, Francois Pacquet, Cecile Pascal, Christophe Philippo, Olivier Venier
  • Publication number: 20120165320
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
    Type: Application
    Filed: June 22, 2010
    Publication date: June 28, 2012
    Applicant: PANACEA BIOTEC LTD.
    Inventors: Rajseh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Publication number: 20120114739
    Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
    Type: Application
    Filed: April 8, 2010
    Publication date: May 10, 2012
    Inventors: Yongqi Deng, Binyuan Sun, Hongbo Zeng, Matthew Richards, Gerald W. Shipps, JR., Cliff C. Cheng, Yinyan Zhao, Andrew McRiner, Zhaoyang Meng, Yang Nan, Mehul F. Patel, Iwona E. Wrona, Panduranga Adulla Reddy, Brian M. Eklov, Shuyi Tang, Duan Liu, Amit K. Mandal, Lianyun Zhao, M. Asshad Siddiqui
  • Publication number: 20120077787
    Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.
    Type: Application
    Filed: December 6, 2011
    Publication date: March 29, 2012
    Applicant: NOVARTIS AG
    Inventors: Daniel Kaspar Baeschlin, Nils OSTERMANN, Francois GESSIER, Finton SIROCKIN, Kenji NAMOTO
  • Patent number: 8143247
    Abstract: Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
    Type: Grant
    Filed: May 7, 2009
    Date of Patent: March 27, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerd Munzert, Martin Steegmaier, Anke Baum
  • Patent number: 8138172
    Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: March 20, 2012
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.
    Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
  • Publication number: 20120065189
    Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.
    Type: Application
    Filed: May 27, 2010
    Publication date: March 15, 2012
    Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
  • Patent number: 8067409
    Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 29, 2011
    Assignee: Abbott Laboratories
    Inventors: Nwe Y. Ba-Maung, Randy L. Bell, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Robert D. Hubbard, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
  • Patent number: 8058270
    Abstract: Disclosed is the use of a compound of general Formula (1), optionally in form of its tautomers, racemates, enantiomers, diastereomers and the mixtures thereof and optionally in form of the pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, physiologically functional derivatives or prodrugs thereof, for the preparation of a pharmaceutical composition for the treatment of diseases characterized by abnormal cell proliferation in a human or non-human mammalian body by inhibition of polo like kinases as mitotic regulators.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: November 15, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerd Munzert, Martin Steegmaier
  • Publication number: 20110218189
    Abstract: The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKC? mediated disorders.
    Type: Application
    Filed: April 8, 2009
    Publication date: September 8, 2011
    Applicant: N.V. ORGANON
    Inventors: Andrew Laird Roughton, Koc-kan Ho, Michael Ohlmeyer, David Diller, Irina Neagu, Celia Kingsbury, Jui-Hsiang Chan, Johannes Petrus, Mmaria Lommerse, Neeltje Miranda Teerhuis, Jacobus Comelis Henricus Maria Wijkmans, Ralf Plate
  • Patent number: 8008298
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: August 30, 2011
    Assignee: Roche Palo Alto
    Inventors: Joe Timothy Bamberg, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Alam Jahangir, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, David Bernard Smith, Michael Soth, Hanbiao Yang
  • Publication number: 20110172217
    Abstract: The present invention provides compounds or a pharmaceutically acceptable salt thereof which inhibit the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and are therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused morpholine compound shown in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 2, 2009
    Publication date: July 14, 2011
    Applicant: Shionogi & Co., Ltd.
    Inventors: Masahiko Fujioka, Susumu Mitsumori, Akira Kugimiya, Daisuke Taniyama
  • Publication number: 20110159563
    Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 30, 2011
    Inventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, JR., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
  • Patent number: RE44205
    Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing comp
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil