5-position Is Unsubstituted Or Alkyl Substituted Only Patents (Class 544/312)
  • Patent number: 9732044
    Abstract: The present invention relates generally to the field of pharmaceuticals and cosmetics. More specifically, the present invention pertains to certain N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of the following formula which are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in therapy, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin; seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. The present invention also relates to compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) an androgen receptor using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: August 15, 2017
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Publication number: 20150141428
    Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 21, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Publication number: 20150111892
    Abstract: The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.
    Type: Application
    Filed: May 27, 2013
    Publication date: April 23, 2015
    Inventors: Daniele Piomelli, Natalia Realini, Marco Mor, Chiara Pagliuca, Daniela Pizzirani, Rita Scarpelli, Tiziano Bandiera
  • Publication number: 20150105351
    Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Publication number: 20150073004
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Imre BATA, Veronika BARTONE BODOR, Attila VASAS, Peter BUZDER-LANTOS, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Zsuzsanna SZAMOSVOLGYI
  • Publication number: 20150051395
    Abstract: Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent ?4 integrin-inhibitory action.
    Type: Application
    Filed: April 24, 2013
    Publication date: February 19, 2015
    Applicant: AJINOMOTO CO., LTD.
    Inventors: Hirokazu Ueno, Takashi Yamamoto, Ryuta Takashita, Ryohei Yokoyama, Toshihiko Sugiura, Shunsuke Kageyama, Ayatoshi Ando, Hiroyuki Eda, Agung Eviryanti, Tomoko Miyazawa, Aya Kirihara, Itsuya Tanabe, Tarou Nakamura, Misato Noguchi, Manami Shuto, Masayuki Sugiki, Mizuki Dohi
  • Publication number: 20140378464
    Abstract: Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.
    Type: Application
    Filed: June 19, 2014
    Publication date: December 25, 2014
    Inventors: Johan Oslob, Robert Anderson, Danielle Aubele, Marc Evanchik, Jonathan Charles Fox, Brian Kane, Puping Lu, Robert McDowell, Hector Rodriguez, Yonghong Song, Arvinder Sran
  • Publication number: 20140378475
    Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: June 25, 2014
    Publication date: December 25, 2014
    Inventors: Douglas G. Batt, Myra Beaudoin Bertrand, George Delucca, Michael A. Galella, Soo Sung Ko, Charles M. Langevine, Qingjie Liu, Qing Shi, Anurag S. Srivastava, Joseph A. Tino, Scott Hunter Watterson
  • Publication number: 20140378491
    Abstract: The present invention provides novel cycloalkyl-substituted pyrimidine dione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.
    Type: Application
    Filed: June 19, 2014
    Publication date: December 25, 2014
    Inventors: Johan Oslob, Robert Anderson, Danielle Aubele, Marc Evanchik, Jonathan Charles Fox, Brian Kane, Robert McDowell, Hector Rodriguez, Yonghong Song, Arvinder Sran
  • Patent number: 8900638
    Abstract: The present invention provides a solid preparation containing compound (I) [compound (I) is as defined in the specification] or a salt thereof, and metformin hydrochloride, which is useful as a therapeutic drug for diabetes and the like, and superior in the preservation stability. A solid preparation having a first part and a second part: a first part: a part containing compound (I) or a salt thereof and substantially free of metformin hydrochloride a second part: a part containing metformin hydrochloride and substantially free of compound (I) and a salt thereof.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: December 2, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazumichi Yamamoto, Hiroyoshi Koyama
  • Patent number: 8883759
    Abstract: There is provided an agent for potentiating the effects of an anti-tumor agent. An anti-tumor effect potentiator containing, as an active ingredient, a uracil compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents a C1-5 alkylene group and one of methylene groups constituting the alkylene group is optionally substituted with an oxygen atom; R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a hydrogen atom or a halogen atom; and R3 represents a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl) C1-6 alkyl group, a halogeno-C1-6 alkyl group or a saturated heterocyclic group.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: November 11, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
  • Publication number: 20140294766
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 2, 2014
    Inventor: AbbVie Inc.
  • Publication number: 20140288065
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
  • Publication number: 20140288106
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: Sanofi
    Inventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
  • Publication number: 20140288049
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Patent number: 8841314
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: September 23, 2014
    Assignee: Pfizer Inc.
    Inventors: David Hepworth, Roger B. Ruggeri
  • Patent number: 8841313
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: September 23, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
  • Publication number: 20140275508
    Abstract: Artificial nucleosides including 2-methyl-nucleobase-substituted butane-1,3-diol nucleosides are disclosed. Four different stereoisomers of such nucleosides are possible. Oligonucleotides made up of the artificial nucleosides form homoduplexes of greater stability than DNA duplexes and have a reduced ability to hybridize to DNA or RNA.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Elitech Holding B.V.
    Inventors: Noah Scarr, Eugeny A. Lukhtanov
  • Patent number: 8835449
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: September 16, 2014
    Assignee: Pfizer Inc.
    Inventors: Edward L. Conn, David Hepworth, Roger B. Ruggeri
  • Patent number: 8822462
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: September 2, 2014
    Assignee: Emory University
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
  • Patent number: 8815883
    Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 26, 2014
    Assignee: The Trustees of Columbia Unviersity in the City of New York
    Inventors: Donald Landry, Shi-Xian Deng
  • Publication number: 20140235638
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 31, 2014
    Publication date: August 21, 2014
    Applicant: AbbVie Inc.
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20140234245
    Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
    Type: Application
    Filed: November 5, 2012
    Publication date: August 21, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Publication number: 20140235606
    Abstract: There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: AstraZeneca AB
    Inventors: Britt Anne Ingela Gullberg, Thomas Peter Larsson, Jeffrey Paul Stonehouse
  • Publication number: 20140228339
    Abstract: There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Application
    Filed: April 15, 2014
    Publication date: August 14, 2014
    Applicant: AstraZeneca AB
    Inventors: Stephen Connolly, Mark Richard Ebden, Iain Alastair Stewart Walters, Thomas Langer, Alan Robert Steven, Craig Robert Stewart, Paula Margaret Tomlin, Andrew John Williams
  • Patent number: 8778838
    Abstract: The present invention relates to aqueous concentrate formulations for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its anhydrate; N-(phosphonomethyl)glycine in the form of its free acid, in the form of the ammonium salt or a substituted ammonium salt or a mixture thereof; at least two different non-ionic surfactants with at least one of them comprising an ethylene oxide polymer moiety or an ethylene oxide/C3-C4-alkylene oxide block copolymer moiety, and water; wherein the pH-value of the formulation is below 6.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: July 15, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Sven Adam, Klaus Kolb, Juergen Jakob, Bernd Sievernich, Joerg Steuerwald, Steven Bowe, Joseph Zawierucha, Rex Liebl
  • Publication number: 20140135219
    Abstract: The present invention relates to the use of the ALS inhibitor herbicides for controlling unwanted vegetation in ALS inhibitor herbicide tolerant Brassica plants, more especially, the present invention relates to the use of ALS inhibitor herbicides for control of unwanted vegetation in Brassica growing areas which Brassica plants comprise non-transgenic mutations of their endogenous acetolactate synthase (ALS) genes I and III.
    Type: Application
    Filed: May 4, 2012
    Publication date: May 15, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ruediger Hain, MIchael Schindler, Katharina Wölfel, Ulrich Ebbinghaus-Kintscher, Arnd Voerste, Olga Malsam, Peter Lösel, Ulrich Görgens
  • Publication number: 20140128570
    Abstract: The present invention relates to ?-PNA monomers according to Formula I where substituent groups R1, R2, R3, R4, R5, R6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 8, 2014
    Inventors: Danith H. Ly, Srinivas Rapireddy, Bichismita Sahu
  • Patent number: 8685991
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: April 1, 2014
    Assignee: AbbVie Inc.
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20140066623
    Abstract: The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.
    Type: Application
    Filed: June 21, 2013
    Publication date: March 6, 2014
    Inventors: THOMAS A. STEITZ, PETER B. MOORE, JOYCE A. SUTCLIFFE, ADEGBOYEGA K. OYELERE, JOSEPH A. IPPOLITO
  • Patent number: 8653002
    Abstract: The present invention relates to aqueous suspension concentrate formulation for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its crystalline anhydrate; at least one non-ionic surfactant selected from polyoxyethylene-polyoxy-C3-C4-alkylene block copolymers; at least one anionic surfactant comprising at least one arylsulfonate group; and water; wherein the pH value of the formulation is in the range of 3 to 7.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: February 18, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Klaus Kolb, Bernd Sievernich, Heidi Emilia Saxell, Joerg Steuerwald, Steven Bowe, Rex Liebl, Terrance M. Cannan
  • Publication number: 20130324724
    Abstract: Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
    Type: Application
    Filed: May 31, 2013
    Publication date: December 5, 2013
    Inventors: Nhut Diep, Yuriy B. Kalyan
  • Publication number: 20130310379
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 21, 2011
    Publication date: November 21, 2013
    Applicant: CONSTELLATION PHARMACEUTICALS
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
  • Publication number: 20130296351
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: May 2, 2013
    Publication date: November 7, 2013
    Inventor: Pfizer Inc.
  • Publication number: 20130252986
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease and/or diabetic macular edema.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Patent number: 8530490
    Abstract: Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug. A uracil compound represented by the general formula (I) or a salt thereof: wherein n represents an integer of 1 to 3; X represents a bond, an oxygen atom, a sulfur atom, or the like; Y represents a linear or branched alkylene group having 1 to 8 carbon atoms, or the like; and Z represents —SO2NR1R2 or —NR3SO2—R4, wherein R1 and R2 each represent an alkyl group having 1 to 6 carbon atoms, an aralkyl group which is optionally substituted, or the like; R3 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R4 represents an aromatic hydrocarbon group, an unsaturated heterocyclic group, or the like.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: September 10, 2013
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
  • Publication number: 20130203991
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 8, 2013
    Applicant: ASTRAZENECA R&D ALDERLY PARK
    Inventor: AstraZeneca R&D Alderly Park
  • Publication number: 20130184299
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Application
    Filed: May 10, 2011
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
  • Publication number: 20130150390
    Abstract: A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.
    Type: Application
    Filed: December 12, 2012
    Publication date: June 13, 2013
    Inventors: Mie Kaino, Hiroyuki Meguro
  • Publication number: 20130150578
    Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 1, 2011
    Publication date: June 13, 2013
    Applicant: CADILA PHARMACEUTICALS LIMITED
    Inventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
  • Patent number: 8455639
    Abstract: The present invention is directed to a crystalline form of 2-[6-[3(R)-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]-benzonitrile, a process for the preparation of said crystalline form and the use thereof in the manufacture of a pharmaceutical composition.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: June 4, 2013
    Assignee: Sandoz AG
    Inventors: Johannes Ludescher, Josef Wieser, Gerhard Laus
  • Publication number: 20130123230
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 16, 2013
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Patent number: 8415351
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: April 9, 2013
    Assignee: Abbott Laboratories
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20130078256
    Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: November 20, 2012
    Publication date: March 28, 2013
    Applicant: Korea Research Institute of Chemical Technology
    Inventor: Korea Research Institute of Chemical Technology
  • Publication number: 20130059872
    Abstract: The present invention provides new amorphous forms of alogliptin benzoate, pharmaceutical compositions comprising same, methods for their preparation and use thereof in treating conditions mediated by DPP-IV, in particular, type 2 diabetes.
    Type: Application
    Filed: November 22, 2010
    Publication date: March 7, 2013
    Applicant: MAPI PHARMA LIMITED
    Inventors: Ehud Marom, Shai Rubnov
  • Publication number: 20130040926
    Abstract: There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Application
    Filed: July 11, 2012
    Publication date: February 14, 2013
    Inventors: Stephen CONNOLLY, Mark Richard EBDEN, Iain Alastair Stewart WALTERS, Thomas LANGER, Alan Robert STEVEN, Craig Robert STEWART, Paula Margaret TOMLIN, Andrew John WILLIAMS
  • Patent number: 8362026
    Abstract: The present invention relates to a crystalline form of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)-amino]sulfonyl]benzamide. The invention also relates to a process for the preparation of this crystalline form and to plant protection formulations which comprise this crystalline form of the phenyluracil.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: January 29, 2013
    Assignee: BASF SE
    Inventors: Thomas Schmidt, Joachim Gebhardt, Sandra Löhr, Michael Keil, Jan Hendrik Wevers, Peter Erk, Heidi Emilia Saxell, Gerhard Hamprecht, Werner Seitz, Guido Mayer, Bernd Wolf, Gerhard Cox, Alfred Michel, Cyrill Zagar, Robert Reinhard, Bernd Sievernich
  • Patent number: 8357695
    Abstract: The present invention relates to hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]-sulfonyl]benzamide. The invention also relates to a process for the preparation of these hydrates and to plant protection formulations which comprise hydrates of the phenyluracil I.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: January 22, 2013
    Assignee: BASF SE
    Inventors: Thomas Schmidt, Joachim Gebhardt, Sandra Löhr, Michael Keil, Jan Hendrik Wevers, Peter Erk, Heidi Emilia Saxell, Gerhard Hamprecht, Guido Mayer, Bernd Wolf, Gerhard Cox, Alfred Michel, Werner Seitz, Cyrill Zagar, Robert Reinhard, Bernd Sievernich
  • Publication number: 20130012490
    Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Patent number: 8324383
    Abstract: Methods of making polymorphs of the benzoate salt of 2-[[6-[(3r)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)-pyrimidinyl]methyl]-benzonitrile.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: December 4, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Mark Andres, Keith Lorimer