At Least Three Ring Hetero Atoms In The Bicyclo Ring System (e.g., Furo- Imidazole, (1,2-a) Imidazole, Pyrazo (1,2-a) Imidazolidine, Etc.) Patents (Class 548/303.1)
  • Patent number: 10323030
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: June 18, 2019
    Assignee: Syngenta Participations AG
    Inventors: Ottmar Franz Hueter, Andrew Edmunds, Andre Jeanguenat, Pierre Joseph Marcel Jung, Anke Buchholz, Michel Muehlebach
  • Patent number: 9334285
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein Cy, R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: May 10, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jennifer Burke, Matthew A. Cerny, Derek Cogan, Kosea S. Frederick, John Lord, Daniel Richard Marshall, Bryan P. McKibben, Simon Suprenant, Maolin Yu, Yunlong Zhang, Lee Fader
  • Patent number: 9224959
    Abstract: A leaving substituent-containing compound including a partial structure represented by the following General Formula (I): where a pair of X1 and X2 or a pair of Y1 and Y2 each represent a hydrogen atom; the other pair each represent a group selected from the group consisting of a halogen atom and a substituted or unsubstituted acyloxy group having one or more carbon atoms; a pair of the acyloxy groups represented by the pair of X1 and X2 or the pair of Y1 and Y2 may be identical or different, or may be bonded together to form a ring; R1 to R4 each represent a hydrogen atom or a substituent; and Q1 and Q2 each represent a hydrogen atom, a halogen atom or a monovalent organic group, and may be bonded together to form a ring.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: December 29, 2015
    Assignee: Ricoh Company, Ltd.
    Inventors: Daisuke Goto, Satoshi Yamamoto, Toshiya Sagisaka, Takuji Kato, Takashi Okada, Masato Shinoda, Shinji Matsumoto, Masataka Mohri, Keiichiro Yutani
  • Patent number: 9029189
    Abstract: Bicyclic guanidine compounds are described. Metal bicyclic guanidinate and its use in vapor deposition processes to deposit a metal-containing thin film are also described. Methods of making alkaline earth metal N,N?dialkylacetamidinates or bicyclic guanidinates including dissolution of alkaline earth metal into liquid ammonia followed by addition of a solution of an amidine or guanidine ligand in the free base from are provided.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: May 12, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Roy Gerald Gordon, Leonard Neil Jacques Rodriguez
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Publication number: 20150005288
    Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: January 22, 2013
    Publication date: January 1, 2015
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbH
    Inventors: Frank Süssmeier, Mario Lobell, Sylvia Grünewald, Michael Härter, Bernd Buchmann, Joachim Telser, Hannah Jörissen, Melanie Heroult, Antje Kahnert, Klemens Lustig, Niels Lindner
  • Publication number: 20140371235
    Abstract: A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing
    Type: Application
    Filed: October 10, 2012
    Publication date: December 18, 2014
    Applicant: University of Pittsburgh - Of the Commonweath System of Higher Education
    Inventors: Zhou Wang, Joel Byron Nelson, Minh Mindy Bao Nguyen, John S. Lazo, Paul A. Johnston, Peter Wipf
  • Patent number: 8912341
    Abstract: Enantiomeric bicyclic lactone compounds as can be prepared via an N-heterocyclic carbene-catalyzed annulation reaction.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: December 16, 2014
    Assignee: Northwestern University
    Inventors: Karl A. Scheidt, Elizabeth O. McCusker
  • Publication number: 20140329858
    Abstract: The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 6, 2014
    Inventors: Mark Gary Bock, Dinesh Chikkanna, Marc Gerspacher, Vinayak Khairnar, Bharat Lagu, Chetan Pandit
  • Patent number: 8853212
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: October 7, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Patent number: 8815926
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: August 26, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Lv Liao, Robert Mah, Liang Mao, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Patent number: 8815918
    Abstract: There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.
    Type: Grant
    Filed: April 1, 2010
    Date of Patent: August 26, 2014
    Assignee: Centro Nacional de Investigaciones Oncologicas (CNIO)
    Inventors: Joaquin Pastor Fernández, Guido Kurz, Sonia Martinez Gonzalez
  • Publication number: 20140206886
    Abstract: Enantiomeric bicyclic lactone compounds as can be prepared via an N-heterocyclic carbene-catalyzed annulation reaction.
    Type: Application
    Filed: January 16, 2014
    Publication date: July 24, 2014
    Applicant: Northwestern University
    Inventors: Karl A. Scheidt, Elizabeth O. McCusker
  • Patent number: 8785639
    Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: July 22, 2014
    Assignee: AbbVie Inc.
    Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
  • Publication number: 20140194622
    Abstract: The present invention provides methods for the synthesis of polycyclic guanidine compounds. In certain embodiments, provided methods include the step of contacting a described reagent with a triamine compound to provide a polycyclic guanidine compound.
    Type: Application
    Filed: January 6, 2014
    Publication date: July 10, 2014
    Applicant: Novomer, Inc.
    Inventor: Alexei Gridnev
  • Patent number: 8759535
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: June 24, 2014
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • Patent number: 8710239
    Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: April 29, 2014
    Assignee: Bial—Portela & C.A., S.A.
    Inventors: Alexander Beliaev, David Alexander Learmonth
  • Patent number: 8703103
    Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: April 22, 2014
    Assignee: Air Products and Chemicals, Inc.
    Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
  • Publication number: 20140011798
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: January 24, 2013
    Publication date: January 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
  • Publication number: 20130331384
    Abstract: The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.
    Type: Application
    Filed: February 14, 2012
    Publication date: December 12, 2013
    Applicant: The Regents of the University of California
    Inventors: Richard L. Gallo, Teruaki Nakatsuji
  • Patent number: 8598217
    Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: December 3, 2013
    Assignees: Astex Therapeutics Ltd., Novartis AG
    Inventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
  • Publication number: 20130296355
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8575360
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: November 5, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rene Marc Lemieux, Steven Richard Brunette, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Bryan McKibben, Craig Andrew Miller, Antonio J. M. Barbosa
  • Patent number: 8552205
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Patent number: 8546147
    Abstract: The present invention relates to compound of formula I: and their use as chemiluminescent and/or bioluminescent reagents.
    Type: Grant
    Filed: July 12, 2010
    Date of Patent: October 1, 2013
    Assignee: Universita degli Studi di Siena
    Inventors: Germano Giuliani, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero
  • Patent number: 8524899
    Abstract: Methods and compositions are provided for forming complexes between dsDNA and novel oligomers comprising fused six-membered rings. By appropriate choice of target sequences and oligomers, complexes comprising oligomer-DNA are obtained with high association constants. The formation of complexes can be used for identification of specific dsDNA sequences, for inhibiting gene transcription, and as a therapeutic for inhibiting proliferation of undesired cells or modulation of expression of specific genes.
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: September 3, 2013
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Christoph A. Briehn, Dorte Renneberg, Philipp Weyermann, Raymond Doss, Michael Marques
  • Patent number: 8519150
    Abstract: Provided are a ?-electron conjugated polymer having a constitutional unit represented by general formula (2) that is suitable as an electrochromic material that changes from a desired colored state to a decolored state, a new compound that is a raw material of the polymer, and a method for producing the polymer: wherein each X independently represents one selected from the group consisting of an oxygen atom, a sulfur atom, —NH—, and —NR1— (wherein R1 is an optionally substituted alkyl group having 1 to 20 carbon atoms or an optionally substituted aryl group having 6 to 20 carbon atoms); each Y independently represents an oxygen atom or a sulfur atom; each Z independently represents one selected from the group consisting of a hydrogen atom and optionally substituted organic groups having 1 to 20 carbon atoms, and W is one selected from the group consisting of an ethynylene group, an optionally substituted ethenylene group, optionally substituted arylene groups, and optionally substituted divalent heteroaromati
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: August 27, 2013
    Assignee: Kuraray Co., Ltd.
    Inventors: Yoshirou Kondou, Kirihiro Nakano, Tomiaki Otake
  • Publication number: 20130210877
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 15, 2013
    Applicant: NEONC TECHNOLOGIES INC.
    Inventors: Thomas Chen, Daniel Levin, Satish Puppali
  • Publication number: 20130190290
    Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: January 23, 2013
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: BAYER INTELLECTUAL PROPERTY GmbH
  • Patent number: 8492542
    Abstract: The present invention is directed to a method producing bicyclic guanidine comprising heating a cyclic thiourea to a temperature ranging from ?140° C. in a substantially non-hydrocarbon solvent to form the bicyclic guanidine.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: July 23, 2013
    Assignee: PPG Industries Ohio, Inc.
    Inventors: Britt A. Minch, Charles R. Hickenboth, Richard F. Karabin, Steven R. Zawacky, Thomas R. Hockswender, Gregory J. McCollum
  • Patent number: 8481750
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: July 9, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jennifer A. Kowalski, Matt Aaron Tschantz
  • Patent number: 8450354
    Abstract: The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: May 28, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, Anitha Hari, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Mohan Rao, Raju Bore Gowda, Robert Carl Andrews, Rongyuan Xie, Soumya P. Sahoo, Tan Ren, William Kenneth Banner
  • Patent number: 8389554
    Abstract: Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: March 5, 2013
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Guenter Hoelzemann, Hartmut Greiner, Emilie Rossignol, Dominique Swinnen
  • Patent number: 8377945
    Abstract: This disclosure concerns compounds which are useful as inhibitors of spleen tyrosine kinase (Syk) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of Syk. This disclosure also relates to pharmaceutical compositions containing these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: February 19, 2013
    Assignee: Rigel Pharmaceuticals Inc.
    Inventors: Jing Zhang, Rajinder Singh, Dane Goff, Taisei Kinoshita
  • Publication number: 20120277240
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: February 17, 2011
    Publication date: November 1, 2012
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20120259112
    Abstract: The present invention provides methods for the synthesis of polycyclic guanidine compounds. In certain embodiments, provided methods include the step of contacting a described reagent with a triamine compound to provide a polycyclic guanidine compound.
    Type: Application
    Filed: December 17, 2010
    Publication date: October 11, 2012
    Applicant: Novomer, Inc.
    Inventor: Alexei Gridnev
  • Publication number: 20120202834
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: February 7, 2012
    Publication date: August 9, 2012
    Applicant: PFIZER INC.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8173811
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: May 8, 2012
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt
  • Publication number: 20120035351
    Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion.
    Type: Application
    Filed: January 28, 2011
    Publication date: February 9, 2012
    Applicant: AIR PRODUCTS AND CHEMICALS, INC.
    Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
  • Publication number: 20110224188
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Application
    Filed: November 20, 2008
    Publication date: September 15, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Antonio Jose del Moral Barbosa, Joerg Martin Benzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan Mckibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Publication number: 20110151615
    Abstract: Bicyclic guanidine compounds are described. Metal bicyclic guanidinate and its use in vapor deposition processes to deposit a metal-containing thin film are also described. Methods of making alkaline earth metal N,N?dialkylacetamidinates or bicyclic guanidinates including dissolution of alkaline earth metal into liquid ammonia followed by addition of a solution of an amidine or guanidine ligand in the free base from are provided.
    Type: Application
    Filed: February 20, 2009
    Publication date: June 23, 2011
    Applicant: President and Fellows of Harvard College
    Inventors: Roy G. Gordon, Leonard Neil Jacques Rodriguesz
  • Patent number: 7906649
    Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: March 15, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Ann E. Weber, Jason Cox
  • Patent number: 7906512
    Abstract: Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: March 15, 2011
    Assignee: Alcon, Inc.
    Inventors: Mark R. Hellberg, Steven T. Miller, Andrew Rusinko
  • Publication number: 20110009392
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: August 4, 2008
    Publication date: January 13, 2011
    Inventors: Zhaoning Zhu, William J. Greenlee, John P. Caldwell, Robert D. Mazzola, JR., Brian McKittrick, Chad E. Bennett, Xianhai Huang, Hubert B. Josien, Duane A. Burnett
  • Patent number: 7867629
    Abstract: A specific derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising the compound. An organic electroluminescence device comprising at least one of organic compound layers including a light emitting layer sandwiched between an anode and a cathode, wherein said at least one of the organic compound layers comprises the derivative of the heterocyclic compound having nitrogen atom as a sole component or as mixed component. The organic electroluminescence device achieves elevation of luminance and excellent efficiency of light emission, and also achieves long lifetime by an improvement of an electrode adhesion.
    Type: Grant
    Filed: September 26, 2003
    Date of Patent: January 11, 2011
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Hiroshi Yamamoto, Masahide Matsuura, Hidetsugu Ikeda, Mineyuki Kubota, Masahiro Kawamura
  • Publication number: 20100316649
    Abstract: This disclosure concerns compounds which are useful as inhibitors of spleen tyrosine kinase (Syk) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of Syk. This disclosure also relates to pharmaceutical compositions containing these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: June 14, 2010
    Publication date: December 16, 2010
    Inventors: Jing Zhang, Rajinder Singh, Dane Goff, Taisei Kinoshita
  • Patent number: 7803952
    Abstract: The present invention relates to a process for the manufacture of cyclic monocarboxylic esters (lactones) and related compounds by hydrogenation of cyclic dicarboxylic acid anhydrides in the presence of metal catalysts.
    Type: Grant
    Filed: April 7, 2006
    Date of Patent: September 28, 2010
    Assignee: DSM IP Assets B.V.
    Inventors: Werner Bonrath, Reinhard Karge, Felix Roessler
  • Patent number: 7781431
    Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: August 24, 2010
    Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
    Inventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
  • Publication number: 20100184794
    Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: October 17, 2007
    Publication date: July 22, 2010
    Inventors: Tsuneo Yasuma, Yasufumi Miyamoto
  • Patent number: 7750034
    Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 19, 2007
    Date of Patent: July 6, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber