Nitrogen Attached Directly Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/159)
  • Patent number: 10766900
    Abstract: The present disclosure provides a Baricitinib intermediate, a method for preparing the Baricitinib intermediate, and a method for preparing Baricitinib or a pharmaceutically acceptable salt thereof using the Baricitinib intermediate. The method for preparing the Baricitinib intermediate involves the use of a divalent palladium catalyst or a nickel catalyst and provides the Baricitinib intermediate in high yield.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: September 8, 2020
    Assignee: FORMOSA LABORATORIES, INC.
    Inventor: Hsiang-Yun Lai
  • Patent number: 10611864
    Abstract: The present invention relates to a compound according to Formula (I) wherein R1 is a hydrocarbyl group selected from the group consisting of alkyl, alkenyl, aryl, aralkyl, and alkylaryl groups, and one or more combinations thereof; wherein R2 is a hydrogen atom, an aryl group or an alkyl group; and wherein R3, R4, R5 and R6, are the same or different and are each independently a hydrogen atom, a halogen atom, a cyano group, an amino group, a hydrocarbyl group selected from the group consisting of alkyl, alkenyl, aryl, aralkyl, and alkylaryl groups or an alkoxy group, and one or more combinations thereof as internal electron donor and to a process for the synthesis of a compound according to Formula (I), wherein R1 is a hydrocarbyl group selected from the group consisting of alkyl, alkenyl, aryl, aralkyl, alkoxycarbonyl and alkylaryl groups, and one or more combinations thereof; wherein R2 is a hydrogen atom or an alkyl group; wherein R3, R4, R5 and R6, are the same or different and are each independently sele
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: April 7, 2020
    Assignee: SABIC GLOBAL TECHNOLOGIES B.V.
    Inventors: Martin Alexander Zuideveld, Jaiprakash Brijlal Sainani, Osamah Al-Humaidan, Sudhakar R. Padmanabhan, Prashant Sukumar Shinge, Sharankumar G. Shetty, Abbas-Alli Ghudubhai Shaikh
  • Patent number: 10442822
    Abstract: An organosilicon compound represented by general formula (1). The present invention is able to provide an organosilicon compound which has excellent adhesion during processing and high bonding strength, while exhibiting antirust corrosion resistance at high levels, and which is useful as a metal surface treatment agent. (In the formula, R represents a hydrolyzable group; R? represents an alkyl group; A represents an alkylene group; R1 and R2, R2 and R3, or R3 and R4 among the R1, R2, R3 and R4 moieties may combine together to form an aliphatic or aromatic ring skeleton, and in cases where a ring skeleton is not formed, each one of the R1, R2, R3 and R4 moieties independently represents a hydrogen atom or an alkyl group; and m represents a number of 1-3.
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: October 15, 2019
    Assignee: SHIN-ETSU CHEMICAL CO., LTD.
    Inventor: Munenao Hirokami
  • Patent number: 9512062
    Abstract: A novel process is described which allows N-isopropyl(meth)acrylamide to be obtained in high purity and yield in a simple manner, by reacting methacrylic anhydride with isopropylamine, optionally in a solvent.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: December 6, 2016
    Assignee: EVONIK ROEHM GmbH
    Inventors: Joachim Knebel, Wilhelm Karnbrock, Volker Kerscher
  • Patent number: 9034922
    Abstract: A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH2)mR1; wherein m represents an integer of any one of 0 to 4; and R1 is any one of —NR5COR2, —NR5SO2R2, and —NR3R4; wherein R2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R3 and R4 represent a C1 to C6 alkyl group or the like; and R5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 19, 2015
    Assignees: THE UNIVERSITY OF TOKYO, KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Koji Eto, Ryoko Ohnishi, Hiromitsu Nakauchi, Takahiko Murata
  • Publication number: 20150080350
    Abstract: The present invention provides bumetanide, analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, analogs and methods for their use. These analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma. Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 19, 2015
    Inventors: John J. PARTRIDGE, Daryl W. HOCHMAN
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8895551
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: November 25, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20140315898
    Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
    Type: Application
    Filed: December 12, 2012
    Publication date: October 23, 2014
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
  • Publication number: 20140243334
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20140194416
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20140187614
    Abstract: The present invention provides new amino lipids and a convenient method for synthesising these compounds. These (cationic) amino lipids have good properties as transfection agents. The method is an economic versatile two step synthesis allowing the preparation of various amino lipids thus leading to the assembly of a combinatorial library of transfection agents. Moreover, the present invention provides lipid particles (liposomes) containing said amino lipids and their use for delivering bioactive agents into cells. The invention encompasses also the use of lipid particles containing the cationic amino lipids as medicament.
    Type: Application
    Filed: May 15, 2012
    Publication date: July 3, 2014
    Applicant: INCELLA GMBH
    Inventors: Gary Davidson, Pavel Levkin, Linxian Li, Yi Su, David Zahner
  • Publication number: 20140163017
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. 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: June 19, 2013
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Patent number: 8735424
    Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: May 27, 2014
    Assignee: Novartis AG
    Inventors: Matthew Burger, Mika Lindvall
  • Publication number: 20140113898
    Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
    Type: Application
    Filed: November 4, 2011
    Publication date: April 24, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
  • Publication number: 20140107335
    Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang
  • Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20140094445
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. 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: August 15, 2012
    Publication date: April 3, 2014
    Applicant: University of Utah Research Foundation
    Inventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140081017
    Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Publication number: 20140066446
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: August 30, 2013
    Publication date: March 6, 2014
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Patent number: 8623859
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: January 7, 2014
    Assignee: Evotec AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xiaolu Wang
  • Publication number: 20130317001
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC.
    Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
  • Publication number: 20130310384
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2011
    Publication date: November 21, 2013
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, Hanxun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe
  • Publication number: 20130310559
    Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.
    Type: Application
    Filed: February 6, 2013
    Publication date: November 21, 2013
    Applicant: SIGNUM BIOSCIENCES, INC.
    Inventors: Jeffry B. Stock, Maxwell Stock, Keshava Rapole, Seung-Yub Lee, Michael Voronkov, Eduardo Perez, Joel Gordon, Shuyi Chen, Jinglong Chen
  • Publication number: 20130281452
    Abstract: Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Inventors: Gregor BAHRENBERG, Sven KUEHNERT, Simon LUCAS, Wolfgang SCHROEDER
  • Publication number: 20130245018
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).
    Type: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Applicant: PIMCO 2664 LIMITED
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Publication number: 20130237702
    Abstract: A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.
    Type: Application
    Filed: August 31, 2012
    Publication date: September 12, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masayuki SUGIKI, Toru OKAMATSU, Tetsuo YANO, Shinya TANIGUCHI
  • Publication number: 20130177900
    Abstract: A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH2)mR1; wherein m represents an integer of any one of 0 to 4; and R1 is any one of —NR5COR2, —NR5SO2R2, and —NR3R4; wherein R2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R3 and R4 represent a C1 to C6 alkyl group or the like; and R5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.
    Type: Application
    Filed: September 16, 2011
    Publication date: July 11, 2013
    Applicants: KAKEN PHARMACEUTICAL CO., LTD., THE UNIVERSITY OF TOKYO
    Inventors: Koji Eto, Ryoko Ohnishi, Hiromitsu Nakauchi, Takahiko Murata
  • Publication number: 20130157851
    Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.
    Type: Application
    Filed: August 18, 2011
    Publication date: June 20, 2013
    Applicant: ISAGRO S.P.A.
    Inventors: Marilena Gusmeroli, Lucio Filippini, Franco Pellacini, Paolo Bravini, Alexia Elmini, Matteo Santino Vazzola, Christian Badaracco
  • Publication number: 20130096105
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: November 30, 2012
    Publication date: April 18, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Publication number: 20130065889
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: October 26, 2012
    Publication date: March 14, 2013
    Applicant: AXIKIN PHARMACEUTICALS, INC.
    Inventor: Axikin Pharmaceuticals, Inc.
  • Publication number: 20130065861
    Abstract: The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.
    Type: Application
    Filed: March 23, 2011
    Publication date: March 14, 2013
    Inventors: Tom Yao-Hsiang Wu, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan
  • Publication number: 20130029991
    Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: August 1, 2012
    Publication date: January 31, 2013
    Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
  • Publication number: 20120316173
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: January 11, 2011
    Publication date: December 13, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra Bartolozzi, Angela Berry, Doris Riether, Monika Ermann, James Edward Jenkins, Innocent Mushi
  • Publication number: 20120269724
    Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.
    Type: Application
    Filed: December 13, 2011
    Publication date: October 25, 2012
    Applicant: President and Fellows of Harvard College
    Inventors: Ashfaq Mahmood, Alun G. Jones, Naengnoi Limpa-Amara, Yijie Peng, Zeynep Akgun
  • Publication number: 20120271049
    Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.
    Type: Application
    Filed: June 28, 2012
    Publication date: October 25, 2012
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Norbert Götz, Michael Keil, Robert Reinhard, Ingo Sagasser, Werner Seitz
  • Publication number: 20120245137
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity, are disclosed. Specifically, a series of compounds containing aryl sulphone derivatives, as exemplified by Formula (I).
    Type: Application
    Filed: September 17, 2010
    Publication date: September 27, 2012
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan A. Pajouhesh, Robert Galemmo, JR., Richard Holland, Yuanxi Zhou, Yongbao Zhu, Eric Simonson, Navjot Chahal, Mike Grimwood
  • Publication number: 20120234721
    Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.
    Type: Application
    Filed: September 9, 2011
    Publication date: September 20, 2012
    Applicant: Neurotherapeutics Pharma, Inc.
    Inventors: Daryl W. HOCHMAN, John J. Partridge
  • Publication number: 20120214769
    Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: April 8, 2011
    Publication date: August 23, 2012
    Applicant: METABASIS THERAPEUTICS, INC.
    Inventors: Jorge E. Gomez-Galeno, K. Raja Reddy, Paul D. van Poelje, Robert Huerta Lemus, Thanh Huu Nguyen, Matthew P. Grote, Qun Dang, Scott J. Hecker, Venkat Reddy Mali, Mingwei Chen, Zhili Sun, Serge Henri Boyer, Haiqing Li, William Craigo
  • Publication number: 20120196849
    Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.
    Type: Application
    Filed: April 10, 2012
    Publication date: August 2, 2012
    Applicant: IRM LLC
    Inventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
  • Patent number: 8202999
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 6, 2006
    Date of Patent: June 19, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Patent number: 8193184
    Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.
    Type: Grant
    Filed: April 20, 2008
    Date of Patent: June 5, 2012
    Assignee: Unimed Pharma, SPOL, S.R.O.
    Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
  • Patent number: 8163735
    Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: April 24, 2012
    Assignee: Virobay, Inc.
    Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
  • Publication number: 20120088746
    Abstract: Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Application
    Filed: May 10, 2007
    Publication date: April 12, 2012
    Applicants: PFIZER INC., RENOVIS, INC.
    Inventors: Yuji Shishido, Kazunari Nakao, Satoshi Nagayama, Hirotaka Tanaka, Matthew Alexander James Duncton, Matthew Cox, John Kincaid, Kiran Sahasrabudhe, Maria de Los Angeles Estiarte-Martinez
  • Patent number: 8148422
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally
  • Publication number: 20120077976
    Abstract: Camphor-derived compounds are disclosed, which are represented as the following formula (I): wherein R1, R2, R3, and R4 each are defined as described in the specification. In addition, a method for manufacturing the camphor-derived compounds and application thereof are disclosed.
    Type: Application
    Filed: January 19, 2011
    Publication date: March 29, 2012
    Inventors: Biing-Jiun UANG, Bo-Yao Yang
  • Publication number: 20120022069
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: April 2, 2010
    Publication date: January 26, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20120015942
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: July 18, 2011
    Publication date: January 19, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20120004225
    Abstract: The present invention provides bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
    Type: Application
    Filed: January 22, 2010
    Publication date: January 5, 2012
    Applicant: NeuroTherapeutics Pharma, Inc.
    Inventors: Stephen Wanaski, John J. Partridge, Stephen D. Collins
  • Patent number: 8080541
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard