Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/68)
  • Patent number: 10881656
    Abstract: The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.
    Type: Grant
    Filed: February 14, 2017
    Date of Patent: January 5, 2021
    Assignee: THE GENERAL HOSPITAL CORPORATION
    Inventors: Othon Iliopoulos, Michael Albert Zimmer
  • Patent number: 10655091
    Abstract: This application relates to thiophene azo dyes for use as hueing agents, laundry care compositions comprising such thiophene azo dyes, processes for making such thiophene azo dyes, and laundry care compositions and methods of using the same. The thiophene azo dyes contain a formally charged moiety and are generally comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. These thiophene azo dyes are advantageous in providing a hueing effect, for example, a whitening effect to fabrics, while not building up over time and causing undesirable blue discoloration to the treated fabrics. The thiophene azo dyes are also generally stable to bleaching agents used in laundry care compositions.
    Type: Grant
    Filed: July 26, 2019
    Date of Patent: May 19, 2020
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Linn Mahaffey, Jr., Xiaoyong Michael Hong, Eduardo Torres, Dominick Joseph Valenti
  • Patent number: 10435651
    Abstract: This application relates to thiophene azo dyes for use as hueing agents, laundry care compositions comprising such thiophene azo dyes, processes for making such thiophene azo dyes, and laundry care compositions and methods of using the same. The thiophene azo dyes contain a formally charged moiety and are generally comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. These thiophene azo dyes are advantageous in providing a hueing effect, for example, a whitening effect to fabrics, while not building up over time and causing undesirable blue discoloration to the treated fabrics. The thiophene azo dyes are also generally stable to bleaching agents used in laundry care compositions.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: October 8, 2019
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Linn Mahaffey, Jr., Xiaoyong Michael Hong, Eduardo Torres, Dominick Joseph Valenti
  • Patent number: 9856439
    Abstract: This application relates to thiophene azo dyes for use as hueing agents, laundry care compositions comprising such thiophene azo dyes, processes for making such thiophene azo dyes, and laundry care compositions and methods of using the same. The thiophene azo dyes contain a formally charged moiety and are generally comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. These thiophene azo dyes are advantageous in providing a hueing effect, for example, a whitening effect to fabrics, while not building up over time and causing undesirable blue discoloration to the treated fabrics. The thiophene azo dyes are also generally stable to bleaching agents used in laundry care compositions.
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: January 2, 2018
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Linn Mahaffey, Jr., Xiaoyong Michael Hong, Eduardo Torres, Dominick Joseph Valenti
  • Patent number: 9487740
    Abstract: This application relates to thiophene azo dyes for use as hueing agents, laundry care compositions comprising such thiophene azo dyes, processes for making such thiophene azo dyes, and laundry care compositions and methods of using the same. The thiophene azo dyes contain a formally charged moiety and are generally comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. These thiophene azo dyes are advantageous in providing a hueing effect, for example, a whitening effect to fabrics, while not building up over time and causing undesirable blue discoloration to the treated fabrics. The thiophene azo dyes are also generally stable to bleaching agents used in laundry care compositions.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: November 8, 2016
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Robert Linn Mahaffey, Jr., Xiaoyong Michael Hong, Eduardo Torres, Dominick Joseph Valenti
  • Patent number: 9029411
    Abstract: This invention provides thiophene compounds of formula I: wherein R1, R2, R3, R4, n, p, and m 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 26, 2009
    Date of Patent: May 12, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christelle C. Renou, Tricia J. Vos, Matthew O. Duffey, Robert Downham
  • 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
  • Patent number: 9012493
    Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: April 21, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
  • Publication number: 20150031658
    Abstract: This invention relates generally to the discovery of a method of inhibiting, preventing or treating bacterial infections. The invention also relates to a method of inhibiting bacterial capsule biogenesis.
    Type: Application
    Filed: October 15, 2014
    Publication date: January 29, 2015
    Inventors: Patrick C. Seed, Carlos C. Goller, Apurba Dutta, Brooks Maki, Frank Schoenen, James Noah, Lucile White
  • Patent number: 8916183
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
  • Patent number: 8889732
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Patent number: 8835654
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 16, 2014
    Assignee: BHI Limited Partnership
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Patent number: 8766001
    Abstract: The present invention relates to the improvement in organic electroluminescent devices by using compounds of the formula (1), in particular as hole-injection or hole-transport materials in a hole-injection or hole-transport layer.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Merck Patent GmbH
    Inventors: Christof Pflumm, Arne Buesing, Amir Hossain Parham, Rocco Fortte, Holger Heil, Philipp Stoessel
  • Patent number: 8741946
    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 (e.g. hepatitis C infections), particularly drug resistant Flaviviridae virus infections.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: June 3, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: William J. Watkins, Eda Canales, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith
  • Publication number: 20140027747
    Abstract: The present invention relates to a compound, which is represented by one chemical formula among the chemical formulas (1) to (3), an organic electronic element comprising the compound, and an electronic device comprising the organic electronic element. The compound is characterized by comprising at least one phenyl group having at least one substitution with deuterium or tritium.
    Type: Application
    Filed: March 29, 2012
    Publication date: January 30, 2014
    Applicant: DUKSAN HIGH METAL CO., LTD.
    Inventors: Soungyun Mun, Bumsung Lee, Jungcheol Park, Kiwon Kim, Yongwook Park, Jeongkeun Park, Heesun Ji, Junghwan Park
  • Publication number: 20140018548
    Abstract: A chiral hydrogenated H8-BINOL bisphosphine compound is provided, with the structure shown as the following formula (I), wherein both R1 and R2 are halogen, H or C1-C10 aliphatic group; R3 is H or C1-C10 aliphatic group; R4 is halogen, amino, nitro, H, C1-C10 aliphatic group or C1-C10 aromatic group; and X is phenyl, substituted phenyl, cyclohexyl, substituted cyclohexyl, C6-C30 aromatic group, or C6-C30 heterocyclic aromatic group containing one or more heteroatoms selected from N, S, O. The present invention further provides a catalyst for an asymmetric catalytic hydrogenation reaction which contains the compound, wherein the catalyst can produce more than 90% of enantiomers and efficiency with the turnover number of greater than 100,000 in the asymmetric hydrogenation reaction of imines.
    Type: Application
    Filed: March 2, 2011
    Publication date: January 16, 2014
    Applicants: DALIAN HETEROGENEOUS CATALYST CO., LTD., YOUTH CHEMICAL CO., LTD., JIANGSU YANGNONG CHEMICAL CO., LTD.
    Inventor: Jin Li
  • Publication number: 20130324537
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: November 21, 2012
    Publication date: December 5, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Abbott GmbH & Co. KG, Abbott Laboratories, Andrea Hager-Wernet
  • Publication number: 20130299799
    Abstract: A photoelectric conversion device comprising an electrically conductive film, an organic photoelectric conversion film, and a transparent electrically conductive film, wherein the organic photoelectric conversion film contains a compound represented by the following formula (1) and an n-type organic semiconductor: wherein each of R1 and R2 independently represents a substituted aryl group, an unsubstituted aryl group, a substituted heteroaryl group or an unsubstituted heteroaryl group, each of R3 to R11 independently represents a hydrogen atom or a substituent provided that an acidic group is excluded, m represents 0 or 1, n represents an integer of 0 or more, R1 and R2, R3 and R4, R3 and R5, R5 and R6, R6 and R8, R7 and R8, R7 and R9, or R10 and R11 may be combined each other to form a ring, and when n is an integer of 2 or more, out of a plurality of R7's and R8's, a pair of R7's, a pair of R8's, or a pair of R7 and R8 may be combined each other to form a ring.
    Type: Application
    Filed: July 18, 2013
    Publication date: November 14, 2013
    Inventors: Katsuyuki YOFU, Kimiatsu NOMURA, Mitsumasa HAMANO, Tetsuro MITSUI
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Patent number: 8557808
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: October 15, 2013
    Assignees: North Carolina Central University, The University of North Carolina at Chapel Hill, Albert Einstein College of Medicine of Yeshiva University
    Inventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
  • Patent number: 8546444
    Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.
    Type: Grant
    Filed: May 28, 2012
    Date of Patent: October 1, 2013
    Assignee: Magnachem International Laboratories, Inc.
    Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
  • Patent number: 8525577
    Abstract: A photoelectric conversion device comprising an electrically conductive film, an organic photoelectric conversion film, and a transparent electrically conductive film, wherein the organic photoelectric conversion film contains a compound represented by the following formula (1) and an n-type organic semiconductor: wherein each of R1 and R2 independently represents a substituted aryl group, an unsubstituted aryl group, a substituted heteroaryl group or an unsubstituted heteroaryl group, each of R3 to R11 independently represents a hydrogen atom or a substituent provided that an acidic group is excluded, m represents 0 or 1, n represents an integer of 0 or more, R1 and R2, R3 and R4, R3 and R5, R5 and R6, R6 and R8, R7 and R8, R7 and R9, or R10 and R11 may be combined each other to form a ring, and when n is an integer of 2 or more, out of a plurality of R7's and R8's, a pair of R7's, a pair of R8's, or a pair of R7 and R8 may be combined each other to form a ring.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: September 3, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Katsuyuki Yofu, Kimiatsu Nomura, Mitsumasa Hamano, Tetsuro Mitsui
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20130217759
    Abstract: The invention provides sulphonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: October 12, 2011
    Publication date: August 22, 2013
    Applicant: Zafgen Inc.
    Inventors: Robert Zahler, Hazel Joan Dyke, Thomas David Pallin, Susan Mary Cramp
  • Publication number: 20130131340
    Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.
    Type: Application
    Filed: September 20, 2011
    Publication date: May 23, 2013
    Inventors: Barry Forman, Donna Yu
  • Patent number: 8420695
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: April 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
  • Patent number: 8410163
    Abstract: Substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carbonitriles and substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carboxamides and their salts are tubulin polymerization inhibitors, useful in the treatment of cancer.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: April 2, 2013
    Assignee: Telik, Inc.
    Inventors: Paul P. Beroza, Komath V. Damodaran, Stella Lui, Wenli Ma, Zhuo Wang, Hua Xu
  • Patent number: 8367846
    Abstract: The present invention provides a method of producing 2-alkyl-3-aminothiophene derivative represented by Formula (4), the method comprising oxidizing a compound represented by the following Formula (1) to produce a compound represented by the following Formula (3) and reducing the compound represented by the following Formula (3): wherein in Formula (1), Formula (3), and Formula (4), R represents an alkyl group, a cycloalkyl group, or a bicycloalkyl group; and X represents a hydroxyl group, a halogen atom acyloxy group, an alkylsulfonyl group, or an arylsulfonyl group.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: February 5, 2013
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yasuaki Fukazawa, Yoji Aoki, Haruko Mita, Hironori Komatsu
  • Publication number: 20120322797
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.
    Type: Application
    Filed: December 9, 2010
    Publication date: December 20, 2012
    Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITY, ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
  • Patent number: 8318796
    Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: November 27, 2012
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Patent number: 8314130
    Abstract: The invention relates to certain compounds including substituted pyridines, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: November 20, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Gary Bohnert, Nha Vo, Qinglin Che, Zhiqiang Xia, Lijun Sun
  • Patent number: 8309554
    Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: November 13, 2012
    Assignee: Threshold Pharmaceuticals
    Inventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
  • 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
  • Publication number: 20120225895
    Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.
    Type: Application
    Filed: November 9, 2010
    Publication date: September 6, 2012
    Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
  • Publication number: 20120202750
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Patent number: 8222430
    Abstract: The present invention provides a 1-heterodiene derivative represented by formula (2) or salt thereof: (in formula (2), W represents hydrogen atom or the like, A represents oxygen atom or the like, R1 represents an optionally substituted C1-6 alkyl group or the like, m represents an integer of 0 to 10, n represents an integer of 1 to 4, X1 represents oxygen atom or the like, p represents an integer of 0 to 5, R3 represents an optionally substituted C1-6 alkyl group or the like, r presents an integer of 0 to 5, the 1-heterodiene derivative exists in E-form, Z-form or a mixture thereof according to the carbon-carbon undefined double stereo bond in formula (2)).
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 17, 2012
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Koichi Kutose, Jyun Takahashi, Isami Hamamoto, Makio Yano, Jyunko Morohoshi, Jyun Kanazawa
  • Publication number: 20120164103
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: March 9, 2012
    Publication date: June 28, 2012
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
  • Patent number: 8197722
    Abstract: Compositions capable of simultaneous two-photon absorption and higher order absorptivities are provided. Compounds having a donor-pi-donor or acceptor-pi-acceptor structure are of particular interest, where the donor is an electron donating group, acceptor is an electron accepting group, and pi is a pi bridge linking the donor and/or acceptor groups. The pi bridge may additionally be substituted with electron donating or withdrawing groups to alter the absorptive wavelength of the structure. Also disclosed are methods of generating an excited state of such compounds through optical stimulation with light using simultaneous absorption of photons of energies individually insufficient to achieve an excited state of the compound, but capable of doing so upon simultaneous absorption of two or more such photons. Applications employing such methods are also provided, including controlled polymerization achieved through focusing of the light source(s) used.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: June 12, 2012
    Assignee: The California Institute of Technology
    Inventors: Seth Marder, Joseph Perry
  • Patent number: 8188145
    Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.
    Type: Grant
    Filed: April 18, 2005
    Date of Patent: May 29, 2012
    Assignee: Magnachem International Laboratories, Inc.
    Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
  • 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: 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: 20120108573
    Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula fare capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Inventors: Ursula SCHINDLER, Karl SCHÖNAFINGER, Hartmut STROBEL
  • Publication number: 20120101286
    Abstract: Substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carbonitriles and substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carboxamides and their salts are tubulin polymerization inhibitors, useful in the treatment of cancer.
    Type: Application
    Filed: February 9, 2010
    Publication date: April 26, 2012
    Applicant: TELIK INC.
    Inventors: Paul P. Beroza, Komath V. Damodaran, Stella Lui, Wenli Ma, Zhuo Wang, Hua Xu
  • Patent number: 8158675
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: April 17, 2012
    Assignee: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
  • Patent number: 8153823
    Abstract: Disclosed is a method for commercially producing 2-alkenyl-3-aminothiophene derivatives, which are useful as intermediates for agricultural chemicals, at low cost. Specifically disclosed is a method for introducing alkenyl groups into the 2-position of 3-aminothiophene derivatives by reacting 3-aminothiophene derivatives represented by the general formula (2) below or salts thereof with a ketone represented by the general formula (1) below without using a protecting group.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: April 10, 2012
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Takeshi Kakimoto, Toshio Kitashima
  • Publication number: 20120022116
    Abstract: Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject.
    Type: Application
    Filed: July 13, 2011
    Publication date: January 26, 2012
    Inventors: Huayun Deng, Ye Fang, Mingqian He, Haibei Hu, Weijun Niu, Haiyan Sun
  • Publication number: 20110251388
    Abstract: The present invention provides a 1-heterodiene derivative represented by formula (2) or salt thereof: (in formula (2), W represents hydrogen atom or the like, A represents oxygen atom or the like, R1 represents an optionally substituted C1-6 alkyl group or the like, m represents an integer of 0 to 10, n represents an integer of 1 to 4, X1 represents oxygen atom or the like, p represents an integer of 0 to 5, R3 represents an optionally substituted C1-6 alkyl group or the like, r presents an integer of 0 to 5, the 1-heterodiene derivative exists in E-form, Z-form or a mixture thereof according to the carbon-carbon undefined double stereo bond in formula (2)).
    Type: Application
    Filed: December 17, 2009
    Publication date: October 13, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Koichi Kutose, Jyun Takahashi, Isami Hamamoto, Makio Yano, Jyunko Morohoshi, Jyun Kanazawa
  • Publication number: 20110251206
    Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 13, 2011
    Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
  • Publication number: 20110190310
    Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: May 14, 2009
    Publication date: August 4, 2011
    Inventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
  • Publication number: 20110190480
    Abstract: The present invention relates to dyes of the general formula CAT+ Y? (I), where Y? is an anion selected from the group of the cyanoborates, fluoroalkylphosphates, fluoroalkylborates or imidates and CAT+ is a cation selected from the group of the azine, xanthene, polymethine, styryl, azo, tetrazolium, pyrylium, benzopyrylium, thiopyrylium, benzothiopyrylium, thiazine, oxazine, triarylmethane, diarylmethane, methine, acridine, quinoline, isoquinoline or quaternary azafluorenone dyes, for colouring plastics and plastic fibres, for the preparation of flexographic printing inks, as ball-point pen pastes, as stamp ink, for colouring leather and paper, for use in data acquisition systems, reprography, in ink microfilters, in photogalvanics, laser technology and the photo industry.
    Type: Application
    Filed: April 11, 2011
    Publication date: August 4, 2011
    Inventors: Nikolai (Mykola) IGNATYEV, Urs Welz-Biermann, Helge Willner, Maik Finze, Eduard Bernhardt, Andriy Kucheryna