At Least Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/236)
  • Heterocyclic flaviviridae virus inhibitors
    Patent number: 8815858
    Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: August 26, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor
  • SUBSTITUTED IMIDAZOPYRIDAZINES
    Publication number: 20140228370
    Abstract: The present invention relates to substituted imidazopyridazine compounds of general formula (I): in which A, Q, R1, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 14, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Knut Eis, Florian Puehler, Ludwig Zorn, Arne Scholz, Philip Lienau, Mark Jean Gnoth, Ulf Bömer, Judith Günther
  • PYRIMIDINE PDE10 INHIBITORS
    Publication number: 20140228368
    Abstract: The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: August 20, 2012
    Publication date: August 14, 2014
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, Jeffrey Kern, Mark E. Layton, Izzat T. Raheem
  • WATER SOLUBLE SALTS OF ALDOSE REDUCTASE INHIBITORS FOR TREATMENT OF DIABETIC COMPLICATIONS
    Publication number: 20140228319
    Abstract: The present invention relates to pharmaceutically acceptable water soluble salts of aldose reductase inhibitors, 2-(8-oxo-7-((5-trifluromethyl)-1H-benzo[d]imidazol-2-yl)methyl)7,8-dihydropyrazin[2,3-d]pyridazin-5-yl)acetic acid and [4-oxo-(5-trifluoromethyl-benzothaiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid (also known as zopolrestat), pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to mammals these salt and compositions.
    Type: Application
    Filed: February 11, 2014
    Publication date: August 14, 2014
    Inventor: Banavara L. Mylari
  • PREPARATION AND METHODS OF USE FOR ORTHO-ARYL 5-MEMBERED HETEROARYL-CARBOXAMIDE CONTAINING MULTI-TARGETED KINASE INHIBITORS
    Publication number: 20140228367
    Abstract: The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.
    Type: Application
    Filed: February 5, 2014
    Publication date: August 14, 2014
    Inventor: Gary A. Flynn
  • Bicyclic Pyridazine Compounds as PIM Inhibitors
    Publication number: 20140221344
    Abstract: The invention relates to bicyclic compounds of formulas I and I?, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
    Type: Application
    Filed: April 19, 2012
    Publication date: August 7, 2014
    Inventors: Derin C. D'amico, Bradley J. Herberich, Claire L.M. Jackson, Liping H. Pettus, Andrew Tasker, Hui-Ling Wang, Bin Wu, Ryan Wurz
  • HETEROARYL SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
    Publication number: 20140221322
    Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
    Type: Application
    Filed: November 5, 2013
    Publication date: August 7, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
  • LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
    Publication number: 20140213538
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 31, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
  • Protein Kinase Inhibitors (Variants), Use Thereof in Treating Oncological Diseases and a Pharmaceutical Composition Based Thereon
    Publication number: 20140213592
    Abstract: The present invention relates to the treatment of oncological, chronic inflammatory and similar diseases with the aid of new families of chemical compounds having improved efficiency with regard to the inhibition of Abl kinase and mutant forms thereof, as well as other therapeutically significant kinases. It describes protein kinase inhibitors in the form of compounds of general formula (I) and compounds of general formula (II), or a tautomer, an individual isomer, a mixture of isomers, a pharmaceutically acceptable salt, a solvate or a hydrate thereof.
    Type: Application
    Filed: April 1, 2014
    Publication date: July 31, 2014
    Applicant: Obshchestvo s ogranichennoy otvetstvennostyou "Fusion Pharma"
    Inventors: Germes G. CHILOV, Ilya Y. TITOV
  • Myosin light chain kinase inhibitor compounds, compositions and related methods of use
    Patent number: 8791116
    Abstract: Pyridazinyl compounds, compositions and related methods of use.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: July 29, 2014
    Assignee: Northwestern University
    Inventors: Daniel Martin Watterson, Linda J. Van Eldik, Heather Behanna, Hantamalala Ralay Ranaivo
  • LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
    Publication number: 20140200215
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: March 12, 2013
    Publication date: July 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • SUBSTITUTED AMINOIMIDAZOPYRIDAZINES
    Publication number: 20140194430
    Abstract: The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 30, 2012
    Publication date: July 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Knut Eis, Florian Pühler, Ludwig Zorn, Arne Scholz, Philip Lienau, Mark Jean Gnoth, Ulf Bömer, Judith Günther, Jörg Fanghänel, Daniel Korr
  • Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof
    Patent number: 8772481
    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatments of protein kinase mediated diseases, including inflammation and related conditions.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: July 8, 2014
    Assignee: Amgen Inc.
    Inventors: Andrew Tasker, Liping H. Pettus, Ryan Wurz
  • Thiophene-carboxamides useful as inhibitors of protein kinases
    Patent number: 8759389
    Abstract: The present invention relates to compounds useful as inhibitors of PLK protein kinase of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: June 24, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Sharn Ramaya, Shazia Keily
  • SUBSTITUTED IMIDAZOPYRIDINES AND IMIDAZOPYRIDAZINES AND THE USE THEREOF
    Publication number: 20140171434
    Abstract: The present application relates to novel substituted imidazopyridines and imidazopyridazines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: May 2, 2012
    Publication date: June 19, 2014
    Applicants: BAYER PHARMA AKTIENGESSELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Volkhart Min-Jian Li
  • Chemical Compounds
    Publication number: 20140171435
    Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
    Type: Application
    Filed: December 12, 2013
    Publication date: June 19, 2014
    Applicant: Pfizer Limited
    Inventors: Kiyoyuki Omoto, Robert McKenzie Owen, David Cameron Pryde, Christine Ann Louise Watson, Mifune Takeuchi
  • BROMODOMAIN INHIBITORS
    Publication number: 20140162971
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 14, 2013
    Publication date: June 12, 2014
    Inventors: Le WANG, John K PRATT, Keith F. McDANIEL, Yujia DAI, Steven D FIDANZE, Lisa HASVOLD, John H. Holms, Warren M. KATI, Dachun LIU, Robert A Mantei, William J. McCLELLAN, George S. SHEPPARD, Carol K. Wada
  • DIBENZOOXEPIN DERIVATIVE
    Publication number: 20140163008
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 12, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • BICYCLIC INHIBITORS OF ALK
    Publication number: 20140155389
    Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
    Type: Application
    Filed: January 20, 2012
    Publication date: June 5, 2014
    Applicant: ABBVIE INC.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
  • Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
    Patent number: 8741897
    Abstract: Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Rajashekhar Betageri, Michel J. Emmanuel, Abdelhakim Hammach, Christian Hanke Justus Joachim Harcken, Thomas Martin Kirrane, Jr., Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, Usha R. Patel, John Robert Proudfoot, Hossein Razavi, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
  • PYRIDAZINONE DERIVATIVES
    Publication number: 20140142088
    Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the 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.
    Type: Application
    Filed: November 18, 2013
    Publication date: May 22, 2014
    Applicant: CEPHALON, INC.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Alison L. Zulli
  • Pyrimido-pyridazinone compounds and methods of use thereof
    Patent number: 8729079
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: May 20, 2014
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Inhibitors of PI3 kinase
    Patent number: 8729074
    Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: May 20, 2014
    Assignee: Amgen Inc.
    Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
  • TRIAZOLOPYRIDAZINE
    Publication number: 20140135336
    Abstract: Disclosed are compounds of general formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 15, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Dirk KESSLER, Ulrich REISER, Christian SMETHURST, Andreas STEFFEN
  • HETEROAROMATIC COMPOUNDS AS PI3 KINASE MODULATORS AND METHODS OF USE
    Publication number: 20140134133
    Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: November 10, 2013
    Publication date: May 15, 2014
    Applicants: Calitor Sciences, LLC
    Inventor: Ning Xi
  • Imidazo[1,2-b]pyridazine derivatives and their use as PDE10 inhibitors
    Patent number: 8716282
    Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: May 6, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Sergio-Alvar Alonso-de Diego, Kelly Ann Swinney, Carina Leys, Johan Erwin Edmond Weerts, Stijn Wuyts
  • PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME
    Publication number: 20140121205
    Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.
    Type: Application
    Filed: March 8, 2013
    Publication date: May 1, 2014
    Applicant: Usher III Initiative
    Inventors: Roland Werner Bürli, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
  • PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGENERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME
    Publication number: 20140121197
    Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.
    Type: Application
    Filed: March 8, 2013
    Publication date: May 1, 2014
    Inventors: Roland Werner BÜRLI, William Rameshchandra Krishna ESMIEU, Christopher James LOCK, Karine Fabienne MALAGU, Andrew Pate OWENS, William E. HARTE
  • Imidazo[1,2-B]pyridazine and pyrazolo[1 .5-A]pyrimidine derivatives and their use as protein kinase inhibitors
    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
  • IMIDAZOPYRIDAZINES AS AKT KINASE INHIBITORS
    Publication number: 20140113901
    Abstract: Imidazopyridazines of formula (I) a process for their production and the use thereof.
    Type: Application
    Filed: April 7, 2011
    Publication date: April 24, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Lars Bärfacker, William Sott, Andrea Hägebarth, Stuart Ince, Hartmut Rehwinkel, Oliver Politz, Roland Neuhaus, Hans Briem, Ulf Bömer
  • SUBSTITUTED IMIDAZOPYRIDINES AND THE USE THEREOF
    Publication number: 20140113900
    Abstract: The present application relates to novel substituted imidazopyridazines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: May 2, 2012
    Publication date: April 24, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexander Straub, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
  • NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20140100231
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 10, 2014
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
  • FUSED BICYCLIC IMIDAZOLES
    Publication number: 20140088110
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Swen HÖLDER, Armin ZÜLCH, Thomas BÄR, Thomas MAIER, Astrid ZIMMERMANN, Thomas BECKERS, Volker GEKELER, Hemant JOSHI, Yogesh MUNOT, Umesh BHISE, Sunil CHAVAN, Sachin SHIVATARE, Sarvesh PATEL, Vikas GORE
  • Compounds
    Patent number: 8674113
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
  • APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
    Publication number: 20140073640
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Application
    Filed: August 12, 2013
    Publication date: March 13, 2014
    Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
  • HETEROARYL SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
    Publication number: 20140066412
    Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
  • AURORA KINASE MODULATORS AND METHOD OF USE
    Publication number: 20140066430
    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: October 3, 2013
    Publication date: March 6, 2014
    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
  • Aminooxazole Inhibitors of Cyclin Dependent Kinases
    Publication number: 20140051694
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: NEOSOME LIFE SCIENCES, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Oxo-substituted imidazo[1,2B]pyridazines, their preparation and use as pharmaceuticals
    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
  • Protein Kinase Inhibitors
    Publication number: 20140031354
    Abstract: The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
    Type: Application
    Filed: July 30, 2012
    Publication date: January 30, 2014
    Applicant: Astar Biotech LLC
    Inventors: Chunrong YU, Haihong Huang, Dongfeng Zhang, Peng Li
  • Heterocycle phenyl amide T-type calcium channel antagonists
    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
  • 1-(Arylmethyl)quinazoline-2,4(1H,3H)-diones as PARP Inhibitors and the Use Thereof
    Publication number: 20140023642
    Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
    Type: Application
    Filed: March 31, 2012
    Publication date: January 23, 2014
    Applicant: Impact Therapeutics, Inc.
    Inventors: Sui Xiong Cai, Ye Edward Tian, Haijun Dong, Qingbing Xu, Lizhen Wu, Lijun Liu, Yangzhen Jiang, Qingli Bao, Guoxiang Wang, Feng Yin, Chengyun Gu, Xiuhua Hu, Xiaozhu Wang, Sishun Kang, Shengzhi Chen
  • Potassium channel modulators
    Patent number: 8629143
    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: Grant
    Filed: November 18, 2010
    Date of Patent: January 14, 2014
    Assignee: AbbVie Inc.
    Inventors: Brian S. Brown, Tongmei Li, Arturo Perez-Medrano, Sridhar Peddi
  • Polymorphic and hydrate forms, salts and process for preparing 6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline
    Patent number: 8629144
    Abstract: The invention relates to novel polymorphic and hydrate forms and salts of 6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline, to methods for their preparation, to pharmaceutical compositions comprising at least one of said polymorphic or hydrate forms or salts, and to the therapeutic and/or prophylactic use of such compositions. The invention also provides new manners for preparing said compound.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: January 14, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Carina Leys, Julius Walter Jozef Dickens, Sigrid Carl Maria Stokbroekx
  • TREATMENT OF PROLIFERATIVE DISORDERS WITH A CHEMILUMINESCENT AGENT
    Publication number: 20140010867
    Abstract: Methods employing chemiluminescent agents as therapeutically active agents in the treatment of proliferative disorders are disclosed. The chemiluminiscent agents are used in the disclosed method without a therapeutically effective amount of a photosensitizer. Novel chemiluminescent agents having the general formula: are also disclosed, wherein X, Y, Z, R3 and R5-R9 are as defined herein.
    Type: Application
    Filed: March 22, 2012
    Publication date: January 9, 2014
    Applicants: Ariel-University Research and Development Company Ltd., Semorex Technologies Ltd.
    Inventors: Bernard S. Green, Galia Luboshits, Michael A. Firer
  • NOVEL 6-TRIAZOLOPYRIDAZINE SULFANYL BENZOTHIAZOLE DERIVATIVES AS MET INHIBITORS
    Publication number: 20140005189
    Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.
    Type: Application
    Filed: August 27, 2013
    Publication date: January 2, 2014
    Applicant: SANOFI
    Inventors: Eva Albert, Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler
  • Pyridone and aza-pyridone compounds and methods of use
    Patent number: 8618107
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: December 31, 2013
    Assignees: Gilead Connecticut, Inc., Genentech, Inc.
    Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
  • COMPOSITIONS AND USES THEREOF TO AMELIORATE PAIN
    Publication number: 20130345424
    Abstract: Hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, compositions comprising hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, and methods for using them for the treatment of pain are described.
    Type: Application
    Filed: March 2, 2012
    Publication date: December 26, 2013
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Riyi Shi
  • RADIOLABELED PDE10A LIGANDS
    Publication number: 20130343992
    Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Application
    Filed: December 21, 2012
    Publication date: December 26, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • SUBSTITUTED IMIDAZOPYRIDAZINES
    Publication number: 20130338133
    Abstract: The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) in which R3, R5, and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: September 6, 2011
    Publication date: December 19, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Ulrich Klar, Marcus Koppitz, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Philip Lienau, Gerhard Siemeister, Antje Margret Wengner