Nitrigen Attached Directly To The Six-membered Hetero Ring Or To The Additional Hetero Ring By Nonionic Bonding Patents (Class 546/281.4)
  • Patent number: 10494760
    Abstract: Methods and formulations for controlling parasitic insect infestations, such as human lice infestations, on textiles. In one embodiment, a method includes applying an anti-parasitic formulation to a textile in need of treatment. In one embodiment, an anti-lice formulation includes an effective amount of at least one spinosyn, such as spinosad. In one embodiment, the anti-lice formulation is at least one of an aqueous suspension and an aqueous solution. The anti-lice formulation may also include one or more additional active ingredients and one or more carriers. The anti-lice formulation has parasiticidal activity when applied to a textile. For example, in one embodiment the anti-lice formulation is formulated to produce 100% adulticidal, nymphicidal, and ovicidal activity when applied to a textile in need of treatment.
    Type: Grant
    Filed: December 4, 2018
    Date of Patent: December 3, 2019
    Assignee: EctoGuard, LLC
    Inventors: Peter C. Canning, Joseph R. Winkle
  • Publication number: 20150126559
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 7, 2015
    Applicant: UNIVERSITA DEGLI STUDI DI FERRARA
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Publication number: 20150119397
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: January 8, 2015
    Publication date: April 30, 2015
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 8952151
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: February 10, 2015
    Assignee: Quanticel Pharmaceuticals, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150023889
    Abstract: Disclosed are compounds, compositions, and methods relating to fluoride aptamers, fluoride-responsive riboswitches, fluoride-regulated expression constructs, fluoride transporters, nucleic acids encoding fluoride transporters, expression constructs encoding fluoride transporters, and cells containing or including any combination of these.
    Type: Application
    Filed: September 17, 2012
    Publication date: January 22, 2015
    Inventors: Ronald Breaker, Jenny Baker, Narasimhan Sudarsan, Zasha Weinberg, Adam Roth, Tyler Ames, James Nelson
  • Publication number: 20150011551
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Applicant: Sanford- Burnham Medical Reseach Institute
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
  • Publication number: 20150005349
    Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I or II or a stereoisomer, tautomer, racemic, metabolite, pro- or pre-drug, salt, hydrate, or solvate thereof, wherein Ar, Cy, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
    Type: Application
    Filed: July 1, 2014
    Publication date: January 1, 2015
    Inventors: Robert Owen Messing, Michael A. Pleiss, Jon D. Levine
  • Patent number: 8853244
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: May 23, 2007
    Date of Patent: October 7, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
  • Publication number: 20140296254
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Publication number: 20140275132
    Abstract: The present invention relates to novel pyridine or pyrimidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with chemokine receptor modulation.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Veena Viswanath, Michael E. Garst, Haiqing Yuan, Xiaoxia Liu
  • Patent number: 8796314
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
  • Publication number: 20140213591
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 31, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 8772498
    Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 8, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Hans-Georg Lerchen, Peter Nell, Frank Süβmeier, Ursula Krenz
  • Patent number: 8697733
    Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: April 15, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Publication number: 20140065103
    Abstract: A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 14, 2013
    Publication date: March 6, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: VERTEX PHARMACEUTICALS INCORPORATED
  • Publication number: 20140057916
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • Publication number: 20140030223
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 30, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Martzman, Philip Anthony Morganelli, William J. Watkins, Hong Ye
  • Publication number: 20130338132
    Abstract: Compounds represented by the following formula (I), are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: June 14, 2012
    Publication date: December 19, 2013
    Applicant: Ajinomoto Co., Inc.
    Inventors: Takahiro Koshiba, Munetaka Tokumasu, Taisuke Ichimaru, Koji Ohsumi, Tadakiyo Nakagawa, Tatsuhiro Yamada, Kayo Matsumoto, Tamotsu Suzuki
  • Patent number: 8604212
    Abstract: Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. To provide a therapeutic or preventive agent for shock, comprising as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a cycloalkylcarbonyl group, an alkenylcarbonyl group, a thiophenecarbonyl group or a benzoyl group which may be substituted by a halogen atom; and Y is an alkylsulfonyl group.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: December 10, 2013
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Shuichi Yotsuya, Hiroshi Shikama
  • Publication number: 20130324501
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols according to formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: June 4, 2013
    Publication date: December 5, 2013
    Inventors: Elisabetta ARMANI, Carmelida Capaldi, Laura Carzaniga, Oriana Esposito
  • Publication number: 20130324557
    Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
    Type: Application
    Filed: November 4, 2011
    Publication date: December 5, 2013
    Applicant: SENOMYX, INC.
    Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung
  • Publication number: 20130315861
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 28, 2013
    Inventors: Eda Canales, Michael O'Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Philip Anthony Morganelli, William J. Watkins
  • Publication number: 20130267700
    Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: October 10, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜßMEIER, Ursula KRENZ
  • Patent number: 8518948
    Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: August 27, 2013
    Assignee: Ingenium Pharmaceuticals GmbH
    Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
  • Patent number: 8513462
    Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: August 20, 2013
    Assignee: Dow AgroSciences LLC
    Inventors: Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
  • Publication number: 20130190356
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genetech, Inc.
  • Patent number: 8492410
    Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Publication number: 20130123242
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 16, 2013
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
  • Patent number: 8420825
    Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: April 16, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Hans-Georg Lerchen, Peter Nell, Frank Süssmeier, Ursula Krenz
  • Publication number: 20130079348
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: March 2, 2011
    Publication date: March 28, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130035358
    Abstract: There is provided compounds of formula I, wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
    Type: Application
    Filed: March 14, 2011
    Publication date: February 7, 2013
    Inventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics, Robert Ronn, Christian Krog-Jensen
  • Patent number: 8367706
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: February 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Altman, Matthew Christopher, Jonathan B. Grimm, Andrew Haidle, Kaleen Konrad, Jongwon Lim, Rachel N. MacCoss, Michelle Machacek, Ekundayo Osimboni, Ryan D. Otte, Tony Siu, Kerrie Spencer, Brandon Taoka, Paul Tempest, Kevin Wilson, Hyun Chong Woo, Jonathan Young, Anna Zabierek
  • Publication number: 20120322801
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: March 4, 2011
    Publication date: December 20, 2012
    Applicant: Amakem NV
    Inventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • Publication number: 20120269864
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
  • Patent number: 8288589
    Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: October 16, 2012
    Assignee: Dow AgroSciences, LLC
    Inventors: Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
  • Patent number: 8288380
    Abstract: A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1—W2 represents CH—CH, or Y represents a single bond and W1—W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: October 16, 2012
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Publication number: 20120259123
    Abstract: The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, a medical composition containing the same, and a medical composition for the treatment or prophylaxis of respiratory diseases or glaucoma.
    Type: Application
    Filed: December 24, 2010
    Publication date: October 11, 2012
    Applicant: UBE INDUSTRIES, LTD.
    Inventors: Ryo Iwamura, Masayuki Tanaka, Tetsushi Katsube, Nobuhiko Shibakawa, Manabu Shigetomi, Eiji Okanari, Tomoko Kanda, Yasunori Tokunaga, Hiroshi Fujiwara
  • Publication number: 20120214799
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: April 9, 2012
    Publication date: August 23, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Guy Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
  • Publication number: 20120202808
    Abstract: A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1-W2 represents CH—CH, or represents a single bond and W1-W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.
    Type: Application
    Filed: April 17, 2012
    Publication date: August 9, 2012
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Publication number: 20120201749
    Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C?O or —C?O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR2, OR1, CN or CO2R; Z1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.
    Type: Application
    Filed: August 25, 2010
    Publication date: August 9, 2012
    Inventors: Melanie Jayne Crawshaw, Philip Spencer Fallon, Ashley Nicholas Jarvis, Jonathan Raymond Powell, Natalie Louise Winfield, David Selwood, Ian Charles Zachary, Haiyan Jia
  • Patent number: 8222634
    Abstract: The present invention relates to a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, driving voltage, and life time.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: July 17, 2012
    Assignee: LG Chem, Ltd.
    Inventors: Dong-Hoon Lee, Jae-Chol Lee, Jae-Soon Bae, Jun-Gi Jang, Kong-Kyeom Kim, Dae-Woong Lee
  • Patent number: 8198271
    Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyle
    Type: Grant
    Filed: May 25, 2009
    Date of Patent: June 12, 2012
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Publication number: 20120122862
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: January 30, 2012
    Publication date: May 17, 2012
    Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
  • Publication number: 20120114765
    Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
    Type: Application
    Filed: March 31, 2010
    Publication date: May 10, 2012
    Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
  • Publication number: 20120108636
    Abstract: The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 3, 2012
    Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
  • Publication number: 20120100990
    Abstract: The present invention relates to substituted 4-aminopicolinates as well as N-oxides and agriculturally acceptable salts thereof, and their use in controlling plant growth, particularly undesirable plant growth, in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredients and/or a safener.
    Type: Application
    Filed: June 21, 2010
    Publication date: April 26, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: William Guy Whittingham, Shuji Hachisu, Matthew Brian Hotson
  • Publication number: 20120059039
    Abstract: Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. To provide a therapeutic or preventive agent for shock, comprising as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a cycloalkylcarbonyl group, an alkenylcarbonyl group, a thiophenecarbonyl group or a benzoyl group which may be substituted by a halogen atom; and Y is an alkylsulfonyl group.
    Type: Application
    Filed: May 17, 2010
    Publication date: March 8, 2012
    Applicant: Ishihara Sangyo Kaisha Ltd
    Inventors: Shuichi Yotsuya, Hiroshi Shikama
  • Patent number: 8129532
    Abstract: Amino(oligo)thiophene dyes useful for studying the electrophysiology of organelles, cells, and tissues are described. Compared to previously known dyes, the amino(oligo)thiophene dyes exhibit improved (faster) response to membrane potential changes, as well as the ability to be excited by 1064 nanometer femtosecond pulses. Methods of preparing the amino( oligo )thiophene dyes are also described.
    Type: Grant
    Filed: July 30, 2008
    Date of Patent: March 6, 2012
    Assignee: The University of Connecticut
    Inventors: Leslie M. Loew, Ping Yan
  • Patent number: 8106073
    Abstract: The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: January 31, 2012
    Assignee: AstraZeneca AB
    Inventors: Simon David Guile, Toby Thompson