Bicyclo Ring Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.04)
Isoquinolines (including hydrogenated) (Class 514/253.05)
Quinolines (including hydrogenated) (Class 514/253.06)
  • 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
    Publication number: 20120283239
    Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 8, 2012
    Applicant: MSD OSS B.V.
    Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
  • BRADYKININ RECEPTOR AGONISTS AND USES THEREOF TO TREAT OCULAR HYPERTENSION AND GLAUCOMA
    Publication number: 20120283260
    Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.
    Type: Application
    Filed: July 24, 2012
    Publication date: November 8, 2012
    Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.
    Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
  • SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT
    Publication number: 20120277210
    Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
    Type: Application
    Filed: October 27, 2011
    Publication date: November 1, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Nathaniel Catron, David Lindley, Jonathan M. Miller, Eric A. Schmitt, Ping Tong
  • PHARMACEUTICAL COMPOSITION CONTAINING FUSED HETERO-RING DERIVATIVE
    Publication number: 20120277238
    Abstract: The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is —O—, etc., n is an integer of 0 to 6; X is —N(R7)— or —O—; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is —C(R8)? or —N?; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is ?O, ?S, etc.; B ring is a ring represented by the following formula: wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: July 29, 2010
    Publication date: November 1, 2012
    Applicant: Shionogi & Co., Ltd
    Inventors: Yuuki Tachibana, Masayoshi Miyagawa, Tsutomu Masuda, Tsuyoshi Hasegawa
  • Novel Azaheterocyclic Compounds
    Publication number: 20120277228
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: July 22, 2010
    Publication date: November 1, 2012
    Inventors: Amanda E. Sutton, Nadia Brugger, Thomas E. Richardson, Harold George Vandeveer, Bayard R. Huck, Ruoxi Lan, Justin Potnick
  • NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
    Publication number: 20120277247
    Abstract: A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
    Type: Application
    Filed: April 27, 2012
    Publication date: November 1, 2012
    Inventors: Christel Jeanne Marie Menet, Alastair James Hodges, Huw David Vater
  • Aminotriazolopyridines, compositions thereof, and methods of treatment therewith
    Patent number: 8299056
    Abstract: Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: October 30, 2012
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Sogole Bahmanyar, R.J. Bates, Kate Blease, Andrew Calabrese, Thomas Daniel, Mercedes Delgado, Jan Elsner, Paul Erdman, Bruce Fahr, Gregory Ferguson, Branden Lee, Lisa Nadolny, Garrick Packard, Patrick Papa, Veronique Plantevin-Krenitsky, Jennifer Riggs, Patricia Rohane, Sabita Sankar, John Sapienza, Yoshitaka Satoh, Victor Sloan, Randall Stevens, Lida Tehrani, Jayashree Tikhe, Eduardo Torres, Andrew Wallace, Brandon Wade Whitefield, Jingjing Zhao
  • BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS
    Publication number: 20120269766
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H? function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
    Type: Application
    Filed: October 12, 2010
    Publication date: October 25, 2012
    Applicant: Yale University
    Inventors: David Spiegel, Christopher Parker
  • TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS
    Publication number: 20120264747
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
    Type: Application
    Filed: June 21, 2012
    Publication date: October 18, 2012
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Wendy Liu
  • 2-HETEROARYL CARBOXAMIDES
    Publication number: 20120258964
    Abstract: The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Application
    Filed: March 6, 2012
    Publication date: October 11, 2012
    Applicant: Bayer Schering Pharma AG
    Inventors: Joachim Luithle, Frank-Gerhard Böss, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Franz-Josef Van Der Staay
  • Substituted N-(1H-Indazol-4-yl)Imidazo[1,2-a]Pyridine-3-Carboxamide Compounds as cFMS Inhibitors
    Publication number: 20120258952
    Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4 and R5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.
    Type: Application
    Filed: December 20, 2010
    Publication date: October 11, 2012
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Mark Laurence Boys, Michael F. Bradley, Robert Kirk DeLisle, D. David Hennings, April L. Kennedy, Fredrik P. Marmsater, Matthew David Medina, Mark C. Munson, Bryson Rast, James P. Rizzi, Martha E. Rodriguez, George T. Topalov, Qian Zhao
  • 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
  • HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES
    Publication number: 20120252799
    Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 4, 2012
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
  • NOVEL COMPOUNDS
    Publication number: 20120252805
    Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase II enzyme.
    Type: Application
    Filed: December 16, 2010
    Publication date: October 4, 2012
    Inventors: Deborah Chen, Kiew Ching Lee, Lamont Roscoe Terrel
  • PYRAZOLOPYRIDINE DERIVATIVES AS ANTICANCER AGENT
    Publication number: 20120245170
    Abstract: The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent.
    Type: Application
    Filed: October 13, 2010
    Publication date: September 27, 2012
    Applicant: Pierre Fabre Medicament
    Inventors: Karim Bedjeguelal, Rémi Rabot, El Bachir Kaloun, Patrice Mayer, Arnaud Marchand, Nicolas Rahier, Philippe Schambel, Hugues Bienayme
  • 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
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8273737
    Abstract: The present invention is directed to 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: Grant
    Filed: January 15, 2009
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang
  • TRIAZOLOPYRIDINE COMPOUNDS AND THEIR USE AS ASK INHIBITORS
    Publication number: 20120238565
    Abstract: The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation.
    Type: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Applicant: MERCK SERONO SA
    Inventors: DOMINIQUE SWINNEN, Catherine Jorand-Lebrun, Tania Grippi-Vallotton, Mathilde Muzerelle, Amanda Royle, Jacqueline Macritchie, Richard Hill, Jeffrey P. Shaw
  • PHARMACEUTICAL FORMULATIONS OF SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES WITH PROTEASE INHIBITORS
    Publication number: 20120238583
    Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
    Type: Application
    Filed: May 17, 2012
    Publication date: September 20, 2012
    Inventors: Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell, John F. Kadow, Zhiwei Yin, Qiufen May Xue, Alicia Regueiro-Ren, John D. Matiskella, Yasutsugu Ueda
  • Piperazinylpiperidine derivatives as chemokine receptor antagonists
    Patent number: 8268826
    Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: September 18, 2012
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Ganfeng Cao, Taisheng Huang, Lihua Chen, Ke Zhang, Anlai Wang, David Meloni, Rajan Anand, Joseph Glenn, Brian W. Metcalf
  • CYCLIC (AZA)INDOLIZINECARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
    Publication number: 20120232081
    Abstract: The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, wherein R, Ra, R10, R20, R30, R40, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 19, 2012
    Publication date: September 13, 2012
    Applicant: SANOFI
    Inventors: Henning STEINHAGEN, Bodo SCHEIPER, Hans MATTER, Gary MCCORT, Guillaume BEGIS, Pascale GOBERVILLE, Berangere THIERS
  • QUINOLIZIDINONE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20120232076
    Abstract: The present invention is directed to 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: November 15, 2010
    Publication date: September 13, 2012
    Inventors: Scott D. Kuduk, Ronald K. Chang
  • Imidazopyridines
    Patent number: 8263584
    Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: September 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Ruben Alvarez Sanchez, Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS
    Publication number: 20120225855
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
    Type: Application
    Filed: May 14, 2012
    Publication date: September 6, 2012
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Christopher Hurley, Jun Liang, Wendy Liu, Joseph P. Lyssikatos
  • 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
  • PYRIDINYLIMIDAZOLONE DERIVATIVES FOR THE INHIBITION OF PI3 KINASES
    Publication number: 20120220587
    Abstract: Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.
    Type: Application
    Filed: September 6, 2010
    Publication date: August 30, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Ulrich Emde, Hans Peter Buchstaller, Markus Klein, Christina Esdar, Joerg Bomke
  • APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
    Publication number: 20120214796
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 23, 2012
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Compositions, synthesis, and methods of using quinolinone based atypical antipsychotic agents
    Patent number: 8247420
    Abstract: The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: August 21, 2012
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu P. Mohapatra, Seema Rani Bhat
  • 3-CARBAMOYL-2-PYRIDONE DERIVATIVES
    Publication number: 20120208813
    Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
    Type: Application
    Filed: February 28, 2012
    Publication date: August 16, 2012
    Inventors: Natsuki ISHIZUKA, Takashi SASATANI, Yoshiharu HIRAMATSU, Masanao INAGAKI, Masahide ODAN, Hiroshi HASHIZUMI, Susumu MITSUMORI, Yasuhiko FUJII, Yoshikazu FUKUI, Hideaki WATANABE, Jun SATO
  • ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
    Publication number: 20120202784
    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: Application
    Filed: January 13, 2012
    Publication date: August 9, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, JR., Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Suganthini S. Nanthakumar, Jingrong Cao, Upul Keerthi Bandarage, Anne-Laure Grillot
  • NEW 5-ALKYNYL-PYRIDINES
    Publication number: 20120196872
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein R1, R2, R3, Ra, Rb, Rc, X, Y and Z are defined as mentioned hereinafter, the individual diastereomers, the individual enantiomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: June 2, 2010
    Publication date: August 2, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alexander Dreyer, Henri Doods, Kai Gerlach, Dirk Gottschling, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle
  • APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
    Publication number: 20120190688
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: March 26, 2012
    Publication date: July 26, 2012
    Inventors: Milan Bruncko, Hong Ding, George A. Doherly, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert A. Mantei, Todd M. Hansen
  • BCL-2/BCL-XL INHIBITORS AND THERAPEUTIC METHODS USING THE SAME
    Publication number: 20120189539
    Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.
    Type: Application
    Filed: January 24, 2012
    Publication date: July 26, 2012
    Applicant: THE REGENTS OF UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
  • 1,2,3-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THIER USE FOR THE TREATMENT OF PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
    Publication number: 20120184525
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: May 11, 2010
    Publication date: July 19, 2012
    Applicants: ADDEX PHARMA S.A., JANSSEN PHARMACEUTICALS, INC
    Inventors: Jose Maria Cid-Nunez, Daniel Oehlrich, Andres Avelino Trabanco-Suarez, Gary John Tresadern, Juan Antonio Vega Ramiro, Gregor James MacDonald
  • 1,6- AND 1,8-NAPHTHYRIDINES
    Publication number: 20120184562
    Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 19, 2012
    Inventor: Kin-Chun Luk
  • TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS
    Publication number: 20120184534
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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: Application
    Filed: December 1, 2011
    Publication date: July 19, 2012
    Inventors: Guy Brenchley, Dean Boyall, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
  • 7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
    Publication number: 20120184528
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: May 11, 2010
    Publication date: July 19, 2012
    Applicants: ADDEX PHARMA S.A., JANSSEN PHARMACEUTICALS, INC
    Inventors: Jose Maria Cic-Nunez, Ana Isabel De Lucas Olivares, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
  • PYRAZOLOPYRIDINE KINASE INHIBITORS
    Publication number: 20120184524
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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: Application
    Filed: December 1, 2011
    Publication date: July 19, 2012
    Inventors: Dean Boyall, Guy Brenchley, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
  • PHENYLACETAMIDES SUITABLE AS PROTEIN KINASE INHIBITORS
    Publication number: 20120184561
    Abstract: The invention relates to compounds of the formula I, wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof; as well as their use, methods of use for them and methods of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.
    Type: Application
    Filed: July 13, 2011
    Publication date: July 19, 2012
    Inventors: Guido BOLD, Pascal FURET, Vito GUAGNANO, Clive McCARTHY, Andrea VAUPEL
  • HETEROARYLS AND USES THEREOF
    Publication number: 20120178723
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 11, 2011
    Publication date: July 12, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • HETEROCYCLIC COMPOUNDS AS JAK RECEPTOR AND PROTEIN TYROSINE KINASE INHIBITORS
    Publication number: 20120178740
    Abstract: The invention relates to compounds of general formula (I) wherein A, R1, R2, R3, R4, R5, R9, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.
    Type: Application
    Filed: July 8, 2010
    Publication date: July 12, 2012
    Applicant: LEO PHARMA A/S
    Inventors: Simon Feldbæk Nielsen, Daniel Rodriguez Greve, Carsten Ryttersgaard, Gunnar Grue-Sørensen, Erik Rytter Ottosen, Tina Dahlerup Poulsen, Søren Christian Schou, Anthony Murray
  • Oxazolidinone antibiotics
    Patent number: 8217029
    Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.
    Type: Grant
    Filed: April 11, 2008
    Date of Patent: July 10, 2012
    Assignee: Actelion Pharmaceuticals Ltd
    Inventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
    Patent number: 8211894
    Abstract: The invention provides heteroarylene substituted 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, A, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: July 3, 2012
    Assignee: Theravance, Inc.
    Inventors: Daniel D. Long, Lan Jiang, Daisuke Roland Saito, Priscilla Van Dyke
  • SALTS AND CRYSTALLINE FORMS OF AN APOPTOSIS-INDUCING AGENT
    Publication number: 20120157470
    Abstract: Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
    Type: Application
    Filed: November 21, 2011
    Publication date: June 21, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Nathaniel Catron, Shuang Chen, Yuchuan Gong, Geoff G. Zhang
  • KINASE INHIBITORS
    Publication number: 20120149680
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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: Application
    Filed: October 18, 2011
    Publication date: June 14, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Michael Mortimore, Andrew Miller, Philip Collier, Stephen Young, Guy Brenchley, Chris Davis, Heather Twin, Chau Mak, Dean Boyall, Shazia Keily, Luca Settimo
  • ORGANIC COMPOUNDS
    Publication number: 20120142685
    Abstract: The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: April 4, 2008
    Publication date: June 7, 2012
    Inventors: Markus Rolf Dobler, Charles Francis Jewell, JR., Erik Meredith, Lauren G. Monovich, Sarah Siska, Anette Von Matt, Maurice Van Eis, Taeyoung Yoon, Christoph Gaul, Michael Paul Capparelli
  • TRAZODONE AND TRAZODONE HYDROCHLORIDE IN PURIFIED FORM
    Publication number: 20120142699
    Abstract: A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
    Type: Application
    Filed: February 10, 2012
    Publication date: June 7, 2012
    Applicant: AZIENDE CHIM. RIUN. ANG. FRANC. A.C.R.A.F. S.p.A.
    Inventors: Marcello MARCHETTI, Tommaso Iacoangeli, Giovanni Battista Ciottoli, Giuseppe Biondi
  • OXAZOLIDINONE-QUINOLONE HYBRID ANTIBIOTICS
    Publication number: 20120142635
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Application
    Filed: February 8, 2012
    Publication date: June 7, 2012
    Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
  • TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS
    Publication number: 20120136000
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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: Application
    Filed: January 27, 2010
    Publication date: May 31, 2012
    Inventors: Juan-Miguel Jimenez, John Studley, Ronald Knegtel, Luca Settimo, Damien Fraysse, Philip N. Collier, Guy Brenchley, Dean Boyall, Andrew Miller, Heather Twin, Stephen Young
  • Bicyclic Heteroaryl Compounds
    Publication number: 20120135986
    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: January 25, 2012
    Publication date: May 31, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antionette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer