Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Publication number: 20140303158
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 9, 2014
    Publication date: October 9, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Patent number: 8853125
    Abstract: The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, etc.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: October 7, 2014
    Assignee: BASF SE
    Inventors: Steffen Groβ, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Prashant Deshmukh, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Faraneh Oloumi
  • Patent number: 8853156
    Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
  • Publication number: 20140296231
    Abstract: The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I): in which A, R1, R3 and n 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 5, 2012
    Publication date: October 2, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Knut EIS, Florian PÜHLER, Ludwig ZORN, Arne SCHOLZ, Philip LIENAU, Mark Jean GNOTH, Ulf BÖMER, Judith GÜNTHER, Marion HITCHCOCK
  • Publication number: 20140296220
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein B, R1, R2, R4, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Application
    Filed: June 18, 2014
    Publication date: October 2, 2014
    Inventors: Gui-Dong Zhu, Jane Gong, Andrew S. Judd, Virajkumar B. Ghandi, Alexander R. Shoemaker, Thomas D. Penning, Michael R. Michaelides, Chunqiu Lai, Keith W. Woods
  • Publication number: 20140296243
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 2, 2014
    Applicant: CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, Jean-Christophe Harmange, Alexandre Cote, Alexander M. Taylor
  • Patent number: 8846676
    Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: September 30, 2014
    Assignee: Sanofi
    Inventors: Antonio Almario Garcia, Mathieu Barrague, Philippe Burnier, Cecile Enguehard-Gueiffier, Zhongli Gao, Pascal George, Alain Gueiffier, Adrien Tak Li, Frederic Peuch, Roy Vaz, Qiuxia Zhao
  • Publication number: 20140288082
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
  • Publication number: 20140288052
    Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 25, 2014
    Inventors: Charles A. Blum, Jeremy S. Disch, Stephanie K. Springer
  • Publication number: 20140288069
    Abstract: The present invention relates to amino imidazopyridazine 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 10 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 14, 2012
    Publication date: September 25, 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
  • Publication number: 20140288017
    Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 8841297
    Abstract: This invention provides the compound 5,8-Dimethyl-2-[2-(1-methyl-4-phenyl-1H-imidazol-2-yl)-ethyl]-[1,2,4]thazolo[1,5-a]pyrazine and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: September 23, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohammed M. Farah
  • Publication number: 20140275069
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: February 25, 2014
    Publication date: September 18, 2014
    Inventors: Katja JANTOS, Michael OCHSE, Hervé GENESTE, Jayne FROGGETT, Clarissa JAKOB, Karla DRESCHER, Jürgen DINGES
  • Publication number: 20140283218
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.
    Type: Application
    Filed: June 27, 2012
    Publication date: September 18, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Roger Graham Hall, Andrew Edmunds, Andre Jeanguenat, Thomas Pitterna, Sebastian Rendler
  • Publication number: 20140275070
    Abstract: The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin).
    Type: Application
    Filed: March 10, 2014
    Publication date: September 18, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li
  • Publication number: 20140274933
    Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: FLATLEY DISCOVERY LAB
    Inventor: Bridget M. Cole
  • Patent number: 8835432
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: September 16, 2014
    Assignee: Amgen Inc.
    Inventors: Minna Bui, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Brian Lucas
  • Publication number: 20140255386
    Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
    Type: Application
    Filed: July 24, 2012
    Publication date: September 11, 2014
    Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTE
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Publication number: 20140256733
    Abstract: Provided herein are imidazopyridine compounds having an inhibitory effect on mixed lineage kinases (MLKs), methods of their synthesis, and methods of their therapeutic. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and pharmaceutical compositions.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Applicant: Califia Bio, Inc.
    Inventors: VAL S. GOODFELLOW, THONG X. NGUYEN, SATHEESH B. RAVULA, HARRIS A. GELBARD
  • Publication number: 20140256705
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Y have any of the values defined 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 11, 2014
    Publication date: September 11, 2014
    Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George S. Sheppard, Carol K. Wada, Kevin R. Woller
  • Publication number: 20140256717
    Abstract: There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: September 11, 2014
    Applicant: Centro Nacional de Investigaciones Oncológicas (CNIO)
    Inventors: Joaquín Pastor Fernández, Rosa Maria Álvarez Escobar, Rosario Concepción Riesco Fagundo, Ana Belén García García, Antonio Rodríguez Hergueta, Jose Ignacio Martin Hernando, Carmen Blanco Aparicio, David Álvaro Cebrián Muñoz
  • Publication number: 20140249150
    Abstract: The invention described herein features methods, compositions, and kits that utilize activators of pyruvate kinase M2 (PKM2) for the treatment or amelioration of disorders related to PKM2 function and characterized by abnormally low levels of serine.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 4, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventor: Charles Kung
  • Publication number: 20140249151
    Abstract: [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11?-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11?-HSD1.
    Type: Application
    Filed: October 17, 2012
    Publication date: September 4, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shimpei Kawakami, Minoru Sakurai, Noriyuki Kawano, Takayuki Suzuki, Nobuyuki Shiraishi, Wataru Hamaguchi, Ryuichi Sekioka, Hiroyuki Moritomo, Ayako Motitomo
  • Publication number: 20140249147
    Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided, are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 4, 2014
    Applicant: GlaxoSmithKline, LLC
    Inventors: Charles A. Blum, Stephanie K. Springer, Chi B. Vu
  • Patent number: 8822468
    Abstract: The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification, the application of a compound of formula (I) in a process for the treatment of the human or animal body, in particular with regard to C-Met tyrosine kinase mediated disease; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner; processes for the preparation of a compound of formula (I).
    Type: Grant
    Filed: March 2, 2009
    Date of Patent: September 2, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Clive McCarthy, Joseph Schoepfer, Carsten Spanka, Melanie Stang, Frederic Stauffer
  • Patent number: 8822689
    Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.
    Type: Grant
    Filed: September 19, 2012
    Date of Patent: September 2, 2014
    Assignees: Merial Limited, Aventis Agriculture
    Inventors: Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Robert Toms Jacobs
  • Publication number: 20140243339
    Abstract: This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating cancer, by combining VEGF(R) inhibitors and inhibitors of HGF/SF:c-Met.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Amgen Inc.
    Inventors: Teresa L. Burgess, Angela Coxon, Isabelle Dussault, Paula Kaplan-Lefko, Anthony J. Polverino, Darrin Beaupre
  • Publication number: 20140243336
    Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
  • Publication number: 20140243308
    Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: Incyte Corporation
    Inventors: Wenqing Yao, Colin Zhang, Meizhong Xu, Jincong Zhuo, Chunhong He
  • 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
  • Publication number: 20140235622
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Application
    Filed: January 28, 2014
    Publication date: August 21, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
  • Publication number: 20140235630
    Abstract: The present invention relates to pharmaceutical compositions that contain PI3K inhibitors (e.g., PBKa-specific inhibitors) and PARP inhibitors. The invention also provides methods for the treatment of proliferative diseases such as cancer (e.g., breast cancer) by administering the composition(s) to a subject.
    Type: Application
    Filed: September 28, 2012
    Publication date: August 21, 2014
    Inventors: Gerburg Wulf, Lewis C. Cantley
  • Patent number: 8809360
    Abstract: The present invention relates to use of a pyridine compound of the following formula [I]: wherein R is a substituted pyridyl group having the following formula: R0 is a C1-6 alkoxy-C1-6 alkyl group, R1 and R2 are the same or different and a C1-6 alkoxy group, X is a group of the formula: ?N— or a group of the formula: Ring A is a saturated or unsaturated 10-membered nitrogen-containing hetero-bicyclic group optionally having a substituent(s), the dotted line means the presence or absence of a double bond, or a pharmaceutically acceptable salt thereof for the preparation of a medicament for treatment of skin lesion.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: August 19, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Tamotsu Takagi, Atsuko Naotsuka
  • Publication number: 20140228369
    Abstract: Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 14, 2014
    Applicant: BioMarin Pharmaceutical Inc.
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Shichun Peng
  • 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
  • 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
  • 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
  • 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
  • Publication number: 20140221315
    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: Application
    Filed: April 3, 2014
    Publication date: August 7, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • 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
  • Publication number: 20140221319
    Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.
    Type: Application
    Filed: April 13, 2012
    Publication date: August 7, 2014
    Applicants: Mayo Foundation for Medical Education and Research, President and Fellows of Harvard College
    Inventors: David A. Sinclair, Nathan L. Price, Eduardo N. Chini, Jon C. Clardy, Shugeng Cao
  • Publication number: 20140221338
    Abstract: The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: August 6, 2012
    Publication date: August 7, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing
  • Publication number: 20140221345
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 7, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20140221365
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: GENENTECH, INC.
    Inventors: James John Crawford, Wendy B. Young
  • 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
  • Publication number: 20140213570
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: April 1, 2014
    Publication date: July 31, 2014
    Applicant: NOVARTIS AG
    Inventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
  • Publication number: 20140212509
    Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.
    Type: Application
    Filed: May 24, 2013
    Publication date: July 31, 2014
    Applicant: ABBVIE INC.
    Inventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
  • 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
  • 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