Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
1,4-diazine as one of the cyclos (Class 514/249)
  • Inhibition of Nonsense Mediated mRNA Decay by Drugs that Prevent Hypusination of Eukaryotic Initiation Factor 5A
    Publication number: 20140206637
    Abstract: Provided are methods for treating a NAD comprising administering to a patient suffering from a NAD an inhibitor of NMD and a nonsense suppressor, whereby degradation of NMD susceptible mRNA is decreased and translation termination at a misplaced nonsense codon is blocked.
    Type: Application
    Filed: June 13, 2012
    Publication date: July 24, 2014
    Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Tsafi Pe'ery, Michael B. Mathews, Mainul Hoque, Hartmut M. Hanauske-Abel
  • PHTHALAZINONES AND ISOQUINOLINONES AS ROCK INHIBITORS
    Publication number: 20140206686
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 24, 2014
    Inventors: Peter W. Glunz, Yan Zou, Mimi L. Quan
  • Imidazopyridine Compounds
    Publication number: 20140206662
    Abstract: A method of treating inflammation, an inflammatory disease, an immune or an autoimmune disorder comprising administering to a patient in need thereof compounds of formula (I): and their pharmaceutically acceptable salts and solvates, which are inhibitors of SSAO activity. The compounds inhibit SSAO activity.
    Type: Application
    Filed: March 13, 2014
    Publication date: July 24, 2014
    Applicant: PROXIMAGEN LTD.
    Inventors: Marianne Nilsson, Martin Haraldsson, Sofia Henriksson, Rikard Emond, Edward Savory, Iain Simpson
  • COMPOSITIONS AND METHODS FOR TREATING COLON CANCER
    Publication number: 20140206693
    Abstract: Certain embodiments are directed to methods of treating a pathophysiological state or symptoms thereof resulting from aldose reductase-mediated signaling in a cytotoxic pathway using an aldose reductase specific inhibitor.
    Type: Application
    Filed: January 27, 2014
    Publication date: July 24, 2014
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Satish K Srivastava, Kota V Ramana
  • Imidazopyridin-2-one derivatives
    Patent number: 8785438
    Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 22, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
  • LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
    Publication number: 20140200215
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: March 12, 2013
    Publication date: July 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS
    Publication number: 20140194408
    Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: March 13, 2014
    Publication date: July 10, 2014
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • SUBSTITUTED AMINOIMIDAZOPYRIDAZINES
    Publication number: 20140194430
    Abstract: The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 30, 2012
    Publication date: July 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Knut Eis, Florian Pühler, Ludwig Zorn, Arne Scholz, Philip Lienau, Mark Jean Gnoth, Ulf Bömer, Judith Günther, Jörg Fanghänel, Daniel Korr
  • Crystalline forms for 5-amino-2, 3-dihydrophthalazine-1, 4-dione sodium salt, pharmaceutical preparations containing the same and method for the production of said forms
    Patent number: 8772294
    Abstract: The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: July 8, 2014
    Assignee: MetrioPharm AG
    Inventors: Josef Breu, Wolfgang Brysch, Astrid Kaiser, Beate Ludescher, Gerrit Maass, Thomas Martin, Wolfgang Milius, Michael Niedermaier
  • Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof
    Patent number: 8772481
    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatments of protein kinase mediated diseases, including inflammation and related conditions.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: July 8, 2014
    Assignee: Amgen Inc.
    Inventors: Andrew Tasker, Liping H. Pettus, Ryan Wurz
  • Modulators of aldehyde dehydrogenase and methods of use thereof
    Patent number: 8772295
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: July 8, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Targeted Conjugates Encapsulated in Particles and Formulations Thereof
    Publication number: 20140187501
    Abstract: Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.
    Type: Application
    Filed: December 30, 2013
    Publication date: July 3, 2014
    Applicant: Blend Therapeutics, Inc.
    Inventors: Mark T. Bilodeau, Sudhakar Kadiyala, Rajesh Shinde, Brian White, Richard Wooster, Timothy Edward Barder
  • METHODS OF PREDICTING OUTCOMES OF CHEMOTHERAPY TREATMENTS AND ALTERNATIVE THERAPIES
    Publication number: 20140187537
    Abstract: This disclosure relates to diagnostic and therapeutic methods and systems related thereto. In certain embodiments, the disclosure contemplates methods of improving chemotherapy treatments by administering chemotherapy agents, analyzing CHFR gene expression, methylation, or both, and determining an appropriate therapeutic strategy. Analysis of data herein revealed that reduced CHFR expression levels was a predictor of improved overall survival of subject with non-small cell lung cancer.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 3, 2014
    Applicant: EMORY UNIVERSITY
    Inventor: Johann C. Brandes
  • 3-hydroxyisothiazole 1-oxide derivatives
    Patent number: 8765752
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 1, 2014
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventor: Munetaka Ohkouchi
  • IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
    Publication number: 20140179674
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Inventors: Brian E. Fink, Libing Chen, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Andrew James Nation, Yufen Zhao, Litai H. Zhang
  • PRESELECTION OF SUBJECTS FOR THERAPEUTIC TREATMENT BASED ON HYPOXIC STATUS
    Publication number: 20140178366
    Abstract: The present invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of hypoxia in cancerous cells in the subject. In one embodiment, the invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of lactate dehydrogenase (LDH) in a cell, e.g., a cancerous cell. The invention also provides methods for treating cancer in a subject by administering an effective amount of an agent to the subject, wherein the subject has been selected based on a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 26, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Ronald K. Blackman, Vojo Vukovic
  • DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS
    Publication number: 20140179697
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: December 23, 2013
    Publication date: June 26, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode Johnson, Emily M. Stocking, Devin M. Swanson
  • QUINOLONE COMPOUND
    Publication number: 20140179675
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Substituted bicyclic amines for the treatment of diabetes
    Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • SUBSTITUTED IMIDAZOPYRIDINES AND IMIDAZOPYRIDAZINES AND THE USE THEREOF
    Publication number: 20140171434
    Abstract: The present application relates to novel substituted imidazopyridines and imidazopyridazines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: May 2, 2012
    Publication date: June 19, 2014
    Applicants: BAYER PHARMA AKTIENGESSELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Volkhart Min-Jian Li
  • TRICYCLIC COMPOUNDS
    Publication number: 20140171417
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Mahbub AHMED, Alexander ASHALL-KELLY, Louisa GUERITZ, Jeffrey MCKENNA, Joseph MCKENNA, Simon MUTTON, Rakesh PARMAR, Jon SHEPHERD, Paul WRIGHT
  • ENHANCEMENT OF CELLULAR TRANSPLANTATION USING SMALL MOLECULE MODULATORS HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY
    Publication number: 20140171419
    Abstract: The present invention provides methods for enhancing cellular transplantation by exposing cells in vitro or ex vivo, or a recipient of cells, to a small molecule hepatocyte growth factor/scatter factor mimetic. Exemplary compounds are described.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 19, 2014
    Applicant: ANGION BIOMEDICA CORP
    Inventors: Lambertus J.W.M Oehlen, Itzhak D. Goldberg
  • DISUBSTITUTED OCTAHYDROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS
    Publication number: 20140171430
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 19, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
  • PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
    Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Chemical Compounds
    Publication number: 20140171435
    Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
    Type: Application
    Filed: December 12, 2013
    Publication date: June 19, 2014
    Applicant: Pfizer Limited
    Inventors: Kiyoyuki Omoto, Robert McKenzie Owen, David Cameron Pryde, Christine Ann Louise Watson, Mifune Takeuchi
  • Antiviral drugs for treatment of infection
    Patent number: 8754082
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: June 17, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
  • 8-fluorophthalazin-1(2H)-one compounds
    Patent number: 8754077
    Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: June 17, 2014
    Assignee: F. Hoffmann-La Roche AG
    Inventors: James J. Crawford, Daniel F. Ortwine, BinQing Wei, Wendy B. Young
  • USE IN BRAIN DEGENERATIVE DISEASES
    Publication number: 20140162964
    Abstract: Disclosed is a new use for sphingosine-1-phosphate (S1P) receptor agonists in the treatment of progressive dementia or brain degenerative diseases.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 12, 2014
    Applicant: NOVARTIS AG
    Inventors: Volker Brinkmann, Nicole Kaneider, Christian J. Wiedermann
  • HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
    Publication number: 20140163035
    Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: July 20, 2012
    Publication date: June 12, 2014
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm, Mark Murphy
  • INHIBITORS OF ANANDAMIDE TRANSPORT AND THEIR THERAPEUTIC USES
    Publication number: 20140163034
    Abstract: Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB1 cannabinoid receptor-mediated analgesia in a mouse model of inflammatory pain. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the modulation of anandamide transport would be of benefit.
    Type: Application
    Filed: November 25, 2013
    Publication date: June 12, 2014
    Applicants: IIT-Istituto Italiano di Tecnologia, The Regents of the University of California
    Inventors: Daniele Piomelli, Jin Fu, Giovanni Bottegoni, Andrea Cavalli, Tiziano Bandiera
  • DIBENZOOXEPIN DERIVATIVE
    Publication number: 20140163008
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 12, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • BROMODOMAIN INHIBITORS
    Publication number: 20140162971
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 14, 2013
    Publication date: June 12, 2014
    Inventors: Le WANG, John K PRATT, Keith F. McDANIEL, Yujia DAI, Steven D FIDANZE, Lisa HASVOLD, John H. Holms, Warren M. KATI, Dachun LIU, Robert A Mantei, William J. McCLELLAN, George S. SHEPPARD, Carol K. Wada
  • Combination of brimonidine and timolol for topical ophthalmic use
    Patent number: 8748425
    Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.
    Type: Grant
    Filed: August 1, 2013
    Date of Patent: June 10, 2014
    Assignee: Allergan Sales, LLC
    Inventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
  • PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS
    Publication number: 20140155404
    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: Application
    Filed: February 10, 2014
    Publication date: June 5, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Chu-Biao Xue, Genfeng Cao, Taisheng Huang, Lihua Chen, Ke Zhang, Anlai Wang, David J. Meloni, Rajan Anand, Joseph Glenn, Brian W. Metcalf
  • BICYCLIC INHIBITORS OF ALK
    Publication number: 20140155389
    Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
    Type: Application
    Filed: January 20, 2012
    Publication date: June 5, 2014
    Applicant: ABBVIE INC.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
  • Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
    Patent number: 8741897
    Abstract: Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Rajashekhar Betageri, Michel J. Emmanuel, Abdelhakim Hammach, Christian Hanke Justus Joachim Harcken, Thomas Martin Kirrane, Jr., Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, Usha R. Patel, John Robert Proudfoot, Hossein Razavi, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
  • Polycyclic heteroaryl substituted triazoles useful as Axl inhibitors
    Patent number: 8741898
    Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: June 3, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
  • MATRIX METALLOPROTEINASE INHIBITORS
    Publication number: 20140148459
    Abstract: This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, periodontitis, multiple sclerosis, gingivitis, gingivitis, atherosclerosis, dry eye, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and pounds.
    Type: Application
    Filed: September 26, 2011
    Publication date: May 29, 2014
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Manoj Kumar Khera, Ajay Soni, Jitendra Sattigeri, Viswajanani Sattigeri, Biswajit Das, Ian A. Cliffe, Pradip Kumar Bhatnagar, Abdul Rehman Abdul Rauf, Arpita Musib, Subham Saha, Neeraj Kumar Yadav, Sabir Ahammed, Ranadheer R. Reddy, Abhijit Ray, Punit Srivastava, Sunanda Ghosh Dastidar
  • NOVEL COMPOSITIONS AND METHODS OF PREVENTING OR AMELIORATING ABNORMAL THROMBUS FORMATION AND CARDIOVASCULAR DISEASE
    Publication number: 20140147448
    Abstract: The invention includes compositions and methods useful for treating preventing abnormal thrombus formation and subsequent cardiovascular disease in diabetic patients and patients with increased cardiovascular risk.
    Type: Application
    Filed: June 5, 2012
    Publication date: May 29, 2014
    Applicant: Yale University
    Inventors: John Hwa, WaiHo Tang
  • Crystalline (8,9)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1-1,2,4-triazol-5-yl)-8,9-dihydro-2-pyrido[4,3,2-de]phthalazin-3(7)-one tosylate salt
    Patent number: 8735392
    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: Grant
    Filed: October 20, 2011
    Date of Patent: May 27, 2014
    Assignee: BioMarin Pharmaceutical Inc.
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Shichun Peng
  • PYRIDAZINONE DERIVATIVES
    Publication number: 20140142088
    Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
    Type: Application
    Filed: November 18, 2013
    Publication date: May 22, 2014
    Applicant: CEPHALON, INC.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Alison L. Zulli
  • ANTIFUNGAL AGENTS AND USES THEREOF
    Publication number: 20140142107
    Abstract: Antimicrobial agents, compositions that include the agent(s) and use(s) thereof are provided. Also disclosed are screening assays for identifying antimicrobial agents.
    Type: Application
    Filed: September 4, 2013
    Publication date: May 22, 2014
    Applicant: University of Massachusetts
    Inventors: Paul Kaufman, Jessica Lopes Da Rosa-Spiegler, Reeta Prusty Rao, Ahmed Fazly
  • 1,4-disubstituted pyridazine analogs there of and methods for treating SMN-deficiency-related conditions
    Patent number: 8729263
    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: Grant
    Filed: August 7, 2013
    Date of Patent: May 20, 2014
    Assignee: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Natalie Dales, Aleem Fazal, Timothy Brian Hurley, John Kerrigan, Gary O'Brien, Lei Shu, Robert Sun, Moo Je Sung
  • Inhibitors of PI3 kinase
    Patent number: 8729074
    Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: May 20, 2014
    Assignee: Amgen Inc.
    Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
  • Pyrimido-pyridazinone compounds and methods of use thereof
    Patent number: 8729079
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: May 20, 2014
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8729078
    Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: May 20, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Joseph Billedeau, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens, Yimin Qian, Sung-Sau So, Kshitij C. Thakkar, Jutta Wanner, Omar Jose Morales
  • Methods and materials for assessing responsiveness to PARP inhibitors and platinating agents
    Patent number: 8729048
    Abstract: This document provides methods and materials involved in assessing responsiveness to PARP inhibitors and platinating agents. For example, methods and materials for using levels of non-homologous end-joining pathway members (e.g., artemis mRNA or polypeptide levels, Ku80 mRNA or polypeptide levels, or DNA-PKcs mRNA or polypeptide levels) to determine if cancer cells that are homologous recombination-deficient are likely to be susceptible or resistant to PARP inhibitors and platinating agents are provided.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: May 20, 2014
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Scott H. Kaufmann, Anand G. Patel
  • Alkylated piperazine compounds
    Patent number: 8729072
    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 immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: May 20, 2014
    Assignee: F. Hoffman-La Roche AG
    Inventors: James John Crawford, Wendy B. Young
  • NOVEL EZRIN INHIBITORS AND METHODS OF MAKING AND USING
    Publication number: 20140135325
    Abstract: The invention encompasses compound and pharmaceutical composition comprising the compound of the following Formula (I): or pharmaceutically acceptable salts or prodrugs thereof, that are useful for inhibiting ezrin protein in a cell or for inhibiting the growth of a cancer cell.
    Type: Application
    Filed: October 7, 2013
    Publication date: May 15, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton L. Brown, Mikell Paige, Jeffrey A. Torestsky, Aykut Uren, George Kosturko, Gullay Bulut
  • HETEROAROMATIC COMPOUNDS AS PI3 KINASE MODULATORS AND METHODS OF USE
    Publication number: 20140134133
    Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: November 10, 2013
    Publication date: May 15, 2014
    Applicants: Calitor Sciences, LLC
    Inventor: Ning Xi