1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
  • Primary Amines And Derivatives Thereof As Modulators Of The 5-HT2A Serotonin Receptor Useful For The Treatment Of Disorders Related Thereto
    Publication number: 20120270861
    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: March 9, 2012
    Publication date: October 25, 2012
    Inventors: BRADLEY TEEGARDEN, DENNIS CHAPMAN, JUYI CHOI, KONRAD FEICHTINGER, SANGDON HAN, HONNAPPA JAYAKUMAR, THUY-AND TRAN, JINGDONG XU, NING ZOU
  • Diazole derivatives
    Patent number: 8293916
    Abstract: The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.
    Type: Grant
    Filed: November 5, 2009
    Date of Patent: October 23, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Paul Spurr, Eric Vieira
  • Antibacterial quinoline derivatives
    Patent number: 8293732
    Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: October 23, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jérôme Emile Georges Guillemont, Ismet Dorange, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
  • CSF-1R inhibitors, compositions, and methods of use
    Patent number: 8293769
    Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: October 23, 2012
    Assignee: Novartis AG
    Inventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
  • SUBSTITUTED DIHYDROPYRAZOLONES AND USE THEREOF AS HIF-PROLYL-4 -HYDROXYLASE INHIBITORS
    Publication number: 20120264704
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Application
    Filed: October 26, 2007
    Publication date: October 18, 2012
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
  • TYROSINE KINASE INHIBITORS
    Publication number: 20120264735
    Abstract: The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: December 14, 2010
    Publication date: October 18, 2012
    Inventors: Jonathan Young, Barbara Czako, Michael Altman, David Guerin, Michelle Martinez, Alexey Rivkin, Kevin Wilson, Kathryn Lipford, Catherine White, Laura Surdi, Stephanie Chichetti, Matthew H. Daniels, Sean P. Ahearn, Danielle Falcone, Ekundayo Osimboni
  • SUBSTITUTED AMINOQUINOXALINES AS TYROSINE THREONINE KINASE INHIBITORS
    Publication number: 20120263708
    Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: August 24, 2010
    Publication date: October 18, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
  • Aminobenzoquinazolinone M1 Receptor Positive Allosteric Modulators
    Publication number: 20120264761
    Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: December 13, 2010
    Publication date: October 18, 2012
    Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng DiMarco, Thomas J. Greshock
  • Melanocortin receptor agonists
    Patent number: 8288386
    Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: October 16, 2012
    Assignee: LG Life Sciences Ltd.
    Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
  • PYRIDOPYRAZINE DERIVATIVES AND THEIR USE
    Publication number: 20120259151
    Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
    Type: Application
    Filed: April 4, 2012
    Publication date: October 11, 2012
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Matthias GERLACH, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
  • VIRAL INHIBITORS
    Publication number: 20120258969
    Abstract: Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 11, 2012
    Inventors: Steven S. Bondy, David A. Oare, Gerhard Puerstinger
  • NOVEL ANTIPLATELET AGENT
    Publication number: 20120258951
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: December 17, 2010
    Publication date: October 11, 2012
    Applicant: Mitsubishi Tanage Pharma Corporation
    Inventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
  • Cyclic and acyclic hydrazine derivatives compositions including them and uses thereof
    Patent number: 8283351
    Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of the functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a cyclic or acyclic hydrazine derivative including those of formulas II or III: or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: October 9, 2012
    Assignee: Institute for OneWorld Health
    Inventors: Michael Geoffrey Neil Russell, Huw David Vater, Jacqueline Anne Macritchie, Kevin James Doyle, David Brown, Joanne Peach
  • QUINOLINE AMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20120252808
    Abstract: The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: December 13, 2010
    Publication date: October 4, 2012
    Inventors: Scott D. Kuduk, Kelly-Ann S. Schlegel, Zhi-Qiang Yang
  • Chemical Compounds 572
    Publication number: 20120252770
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: March 23, 2012
    Publication date: October 4, 2012
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES
    Publication number: 20120252817
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Application
    Filed: May 26, 2010
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Rene Marc Lemieux, Steven Richard Brunette, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Bryan McKibben, Craig Andrew Miller, Antonio J. M. Barbosa
  • Inhibitors of Janus kinases
    Patent number: 8278335
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, Andrew Haidle, Anna A. Zabierek, Kaleen M. Konrad, Michael D. Altman
  • Substituted 4-hydroxypyrimidine-5-carboxamides
    Patent number: 8278304
    Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh
  • Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
    Patent number: 8278316
    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 2, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Saleem Ahmad
  • OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20120245162
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein.
    Type: Application
    Filed: September 20, 2011
    Publication date: September 27, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Weimin LIU, Ho Yin LO, Pui Leng LOKE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
  • NOVEL (HETEROCYCLE/TETRAHYDROPYRIDINE)-(PIPERAZINYL)-1-ALCANONE AND (HETEROCYCLE/DIHYDROPYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE DERIVATIVES, AND USE THEREOF AS p75 INHIBITORS
    Publication number: 20120245150
    Abstract: The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: SANOFI
    Inventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
  • GPR119 AGONIST
    Publication number: 20120245344
    Abstract: A compound represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes: wherein each of R23, R24, and R25 is hydrogen, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylsulfonyl, or the like; each of Q0 and T0 is CH2 or the like, or Q0 and T0 are combined to form CH?CH or the like; A0 is (CH2)p, C(O), or a bond; B0 is a bond or the like; one of U0 and V0 is N, and the other is CR31 or the like; each of X0 and Y0 is CH2CH2 or the like; Z0 is C(O)OR32 or the like; and each of R21 and R22 is hydrogen, a halogen atom, hydroxyl, C1-8 alkyl, or the like.
    Type: Application
    Filed: August 30, 2010
    Publication date: September 27, 2012
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Tsuyoshi Endo, Hiroto Tanaka, Toshihiro Takahashi, Toshihiro Kunigami
  • NOVEL (HETEROCYCLE/CONDENSED PIPERIDINE)-(PIPERAZINYL)-1-ALKANONE OR (HETEROCYCLE/CONDENSED PYRROLIDINE)-(PIPERAZINYL)-1-ALKANONE DERIVATIVES AND USE THEREOF AS p75 INHIBITORS
    Publication number: 20120245149
    Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyI)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: SANOFI
    Inventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
  • PYRIDAZINE COMPOUNDS, COMPOSITIONS AND METHODS
    Publication number: 20120245125
    Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.
    Type: Application
    Filed: June 8, 2012
    Publication date: September 27, 2012
    Applicants: Northwestern University
    Inventors: D. Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki
  • (1, 1, 1,3,3,3 -HEXAFLUORO-2 HYDROXYPROPAN- 2 -YL) PHENYL DERIVATIVE, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF ATHEROSCLEROSIS
    Publication number: 20120238574
    Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.
    Type: Application
    Filed: October 26, 2010
    Publication date: September 20, 2012
    Applicant: N.V. ORGANON
    Inventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
  • New Compounds 806
    Publication number: 20120238579
    Abstract: The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.
    Type: Application
    Filed: March 23, 2012
    Publication date: September 20, 2012
    Inventors: Yevgeni Besidki, Inger Kers, Martin Nylôf, Lars Sandberg, Karin Skogholm
  • Pyridazinone derivatives as PARP inhibitors
    Patent number: 8268827
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: September 18, 2012
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA.
    Inventors: Danila Branca, Gabriella Dessole, Federica Ferrigno, Philip Jones, Olaf Kinzel, Samuele Lillini, Ester Muraglia, Giovanna Pescatore, Carsten Schultz-Fademrecht
  • Tri-cyclic pyrazolopyridine kinase inhibitors
    Patent number: 8268999
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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.
    Type: Grant
    Filed: August 24, 2011
    Date of Patent: September 18, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alex Aronov, Jon H. Come, Kevin Michael Cottrell, Arnaud Le Tiran, Valerie Marone, Gabriel Martinez Botella, David Messersmith, Emilie Porter Huck, Ronald Lee Grey, Jr.
  • 1,2-Disubstituted Heterocyclic Compounds
    Publication number: 20120232265
    Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: November 7, 2011
    Publication date: September 13, 2012
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • 3-AMINO-PYRIDINES AS GPBAR1 AGONISTS
    Publication number: 20120232051
    Abstract: This invention relates to novel 3-aminopyridines of the formula wherein B1, B2 and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: February 28, 2012
    Publication date: September 13, 2012
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Prabha Saba Karnachi, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
  • 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
    Publication number: 20120232071
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Glucokinase Activators
    Publication number: 20120225887
    Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: April 10, 2012
    Publication date: September 6, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
  • IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20120225885
    Abstract: The present invention relates to novel imidazole compounds, pharmaceutical compositions comprising the imidazole compounds and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 6, 2012
    Inventors: Ashwin U. Rao, Anandan Palani, Robert G. Aslanian
  • 8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE
    Publication number: 20120225876
    Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R1a and R1b may be the same or different and each independently represents a C1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X1 represents a hydroxyl group or an aminocarbonyl group; Z1 represents a single bond or the like; and R2 represents an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group or the like.
    Type: Application
    Filed: November 11, 2010
    Publication date: September 6, 2012
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Yoshihiro Horiuchi, Kiyoto Sawamura, Hiroaki Fujiwara
  • HETEROARYLAMINOQUINOLINES AS TGF-BETA RECEPTOR KINASE INHIBITORS
    Publication number: 20120225875
    Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: October 12, 2010
    Publication date: September 6, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Alfred Jonczyk, Christiane Amendt, Frank Zenke
  • COMPOUNDS FOR ALZHEIMER'S DISEASE
    Publication number: 20120225873
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: April 13, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS
    Publication number: 20120225886
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: August 24, 2010
    Publication date: September 6, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gregori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • ANDROGEN RECEPTOR MODULATING COMPOUNDS
    Publication number: 20120225867
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: October 27, 2010
    Publication date: September 6, 2012
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES
    Publication number: 20120225854
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: August 23, 2011
    Publication date: September 6, 2012
    Applicant: AMGEN INC.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • BICYCLIC TRIAZOLE AND PYRAZOLE LACTAMS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
    Publication number: 20120225844
    Abstract: In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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: December 16, 2011
    Publication date: September 6, 2012
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Carrie K. Jones, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Chrysa Malosh
  • Pyridazine compound and use thereof
    Patent number: 8258136
    Abstract: A pyridazine compound of the formula: has an excellent plant disease controlling effect.
    Type: Grant
    Filed: November 28, 2006
    Date of Patent: September 4, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Akio Manabe
  • Pyridazinone glucokinase activators
    Patent number: 8258134
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Grant
    Filed: March 9, 2009
    Date of Patent: September 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
  • Chemical compounds—643
    Patent number: 8258140
    Abstract: The invention concerns bicyclic compounds of Formula I wherein , R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: September 4, 2012
    Assignee: Astrazeneca AB
    Inventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
  • TRICYCLIC INHIBITORS OF KINASES
    Publication number: 20120220572
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 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: February 28, 2012
    Publication date: August 30, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
  • AZA-BICYCLOALKYL ETHERS AND THEIR USE AS ALPHA7-NACHR AGONISTS
    Publication number: 20120220599
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 2, 2012
    Publication date: August 30, 2012
    Inventors: Dominik FEUERBACH, Konstanze HURTH, Timothy John RITCHIE
  • OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20120220561
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: August 12, 2011
    Publication date: August 30, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
  • (3-FLUORO-2-HYDROXY)PROPYL-FUNCTIONALIZED ARYL DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR THE DIAGNOSIS OR TREATMENT OF NEURODEGENERATIVE BRAIN DISEASES
    Publication number: 20120214994
    Abstract: The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salt thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to ?-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 23, 2012
    Inventors: Dae-Yoon Chi, Byoung-Se Lee, Sirion Uthaiwan, So-Young Chu, Yu-Jin Bae, Chansoo Park, Dae-Hyuk Moon, Jin-Sook Ryu, Jae-Seung Kim, Seung-Jun Oh
  • 2-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses
    Publication number: 20120214815
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 23, 2012
    Applicant: UCB Pharma, S.A.
    Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
  • TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
    Publication number: 20120214789
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: May 2, 2012
    Publication date: August 23, 2012
    Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
  • CANNABINOID RECEPTOR MODULATORS
    Publication number: 20120214766
    Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.
    Type: Application
    Filed: August 27, 2010
    Publication date: August 23, 2012
    Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue