Benzene Ring Bonded Directly To Urea Nitrogen Patents (Class 514/596)
  • Patent number: 10640494
    Abstract: A compound is represented as Formula I, a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof: Compounds of Formula I are inhibitors of N-acylethanolamine hydrolyzing acid amidase (NAAA).
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: May 5, 2020
    Assignee: NORTHEASTERN UNIVERSITY
    Inventors: Michael Malamas, Alexandros Makriyannis, Kumara Vadivel Subramanian, Kyle M. Whitten, Nikolai M. Zvonok, Jay Matthew West, Michael McCormack, Spiro Pavlopoulos
  • Patent number: 9827236
    Abstract: Methods for reducing the glycation of nutrient and endogenous proteins and methods for reducing the peroxidation of nutrient and endogenous lipids are provided herein. Several inhibitors and conditions of inhibiting glycation of nutrient and endogenous proteins and peroxidation of nutrient and endogenous lipids are also provided herein. Also provided are the methods for inhibiting and treating the conditions associated with the formation of glycated proteins, such as Alzheimer's disease, neuropathy, retinopathy and nephropathy and the methods for inhibiting and treating the conditions associated with the formation of peroxidized lipids, such as cancer and atherosclerosis.
    Type: Grant
    Filed: May 10, 2015
    Date of Patent: November 28, 2017
    Inventor: Mythri Ambatipudi
  • Patent number: 9181261
    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: Grant
    Filed: May 17, 2013
    Date of Patent: November 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Publication number: 20150148395
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Patent number: 9029322
    Abstract: The present invention relates to a method for identifying a drug candidate for enhancing expression of p21cip1/waf1 in a human patient suffering from a medical condition that can be treated by enhancing expression of p21C?1/waf1. The method includes (a) providing a cell line comprising a nucleic acid sequence that comprises a p21cip1/waf1 promoter operationally ligated to a reporter domain; (b) exposing the cell line to a compound; and (c) identifying a compound that induces expression of the reporter domain. The compound that induces expression of the reporter domain is a drug candidate for treating a medical condition that can be treated by enhancing expression of p21cip1/waf1.
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: May 12, 2015
    Assignee: Cornell University
    Inventors: Rajiv R. Ratan, Brett C. Langley, Brian S. Ko
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Publication number: 20150065575
    Abstract: Determinations of the level of expression of S100A8/A9 protein serve as a prognostic indicator of the therapeutic response to a given type of chemotherapy treatment and as a monitoring indicator of the effectiveness of an on-going chemotherapy treatment for the treatment of breast cancer in human patients. Kits can be used for performing these determinations.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 5, 2015
    Inventors: Joan Massague, Swarnali Acharyya
  • Publication number: 20150056213
    Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.
    Type: Application
    Filed: March 7, 2013
    Publication date: February 26, 2015
    Inventors: Eduardo M. Sotomayor, Joel Bergman, Alan Kozikowski, Karrune Veeraprasert Woan, Alejandro V. Villagra
  • Publication number: 20150045389
    Abstract: The present invention is a screening assay for identifying inhibitors of Pseudomonas aeruginosa CFTR Inhibitory Factor as well as compounds identified by the screening assay for use in compositions and methods for ameliorating or treating a respiratory disease such as cystic fibrosis or secondary infection thereof.
    Type: Application
    Filed: April 9, 2013
    Publication date: February 12, 2015
    Inventors: Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
  • Publication number: 20140329860
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.
    Type: Application
    Filed: March 24, 2014
    Publication date: November 6, 2014
    Applicant: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Publication number: 20140194433
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • Publication number: 20140162996
    Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.
    Type: Application
    Filed: July 29, 2013
    Publication date: June 12, 2014
    Applicant: CITY OF HOPE
    Inventors: Samuel RAHBAR, James L. FIGAROLA, Christopher LINCOLN, David HORNE, Rachael MOONEY, Monika POLEWSKI, George SOMLO, Lixin YANG
  • Publication number: 20140142136
    Abstract: The present invention relates to methods and compounds for regulating or enhancing erythropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.
    Type: Application
    Filed: November 19, 2013
    Publication date: May 22, 2014
    Inventors: Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Robert C. Stephenson
  • Patent number: 8686042
    Abstract: The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3?, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: April 1, 2014
    Assignee: Neuropharma, S.A.
    Inventors: Ana Martinez Gil, Miguel Medina Padilla, Mercedes Alonso Cascon, Ana Fuertes Huerta, Maria Luisa Navarro Rico, Maria Jose Perez Puerto, Ana Castro Morera, Ester Martin Aparicio
  • Publication number: 20140088156
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Application
    Filed: February 14, 2012
    Publication date: March 27, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Patent number: 8653304
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20140045944
    Abstract: A synergistic antimicrobial composition containing 3-iodo-2-propynyl-butylcarbamate and fluometuron.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: Dow Global Technologies LLC
    Inventors: Emerentiana Sianawati, Sangeeta Ganguly
  • Patent number: 8637554
    Abstract: The invention provides methods for enhancing iodine absorption in a thyroid in a subject and treating thyroid cancer by administering to the subject a composition which includes a multi-kinase inhibitor. Furthermore, the invention provides methods for improving a medical diagnostic procedure based on radioactive iodine in a subject by administering to the subject a composition comprising a multi-kinase inhibitor.
    Type: Grant
    Filed: May 7, 2009
    Date of Patent: January 28, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Marcia S. Brose
  • Publication number: 20130345164
    Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.
    Type: Application
    Filed: April 21, 2011
    Publication date: December 26, 2013
    Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY
    Inventors: Alexei Vazquez, Darren Carpizo, Arnold Levine
  • Patent number: 8592466
    Abstract: Treatment of humans suffering from conditions caused by higher-than-normal dopaminergic activity in basal ganglia includes administering the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: November 26, 2013
    Assignee: Neuropill, Inc.
    Inventor: Ahmed Elkashef
  • Patent number: 8592405
    Abstract: A synergistic antimicrobial composition containing 3-iodo-2-propynyl-butylcarbamate and fluometuron.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: November 26, 2013
    Assignee: Dow Global Technologies LLC
    Inventors: Emerentiana Sianawati, Sangeeta S. Ganguly
  • Publication number: 20130267550
    Abstract: Methods and compositions are provided for treatment of disorders associated with aberrant adrenal cortex cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC), Cushing's syndrome and/or pituitary ACTH excess (Cushing's Disease). Such methods involve administration of an effective amount N-(2,6-bis(1-methylethyl)phenyl)-N?-((1-(4-(dimethylamino)phenyl)cyclopentyl)-methyl)urea hydrochloride to the patient.
    Type: Application
    Filed: March 13, 2013
    Publication date: October 10, 2013
    Inventors: Gary Hammer, Tom Kerppola, Raili Kerppola
  • Publication number: 20130261178
    Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C3 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; Z is linear C2-3 alkylene; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10 aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or further substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3;
    Type: Application
    Filed: July 5, 2010
    Publication date: October 3, 2013
    Inventors: Shailesh Mistry, Etienne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Publication number: 20130225642
    Abstract: The present invention provides a prophylactic or therapeutic agent for amyotrophic lateral sclerosis, containing a 1,3-diphenylurea derivative or multikinase inhibitor.
    Type: Application
    Filed: September 2, 2011
    Publication date: August 29, 2013
    Applicant: KYOTO UNIVERSITY
    Inventor: Ayako Asai
  • Patent number: 8507560
    Abstract: The present invention relates to a method of treating a disorder associated with modulation of the FPRL-1 receptor which comprises administering a therapeutically effective amount of a pharmaceutical composition comprising a 3,4-dihydroisoquinolin-2(1H)-yl-3-phenylurea derivative.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: August 13, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Michael E. Garst, Veena Viswanath
  • Publication number: 20130178446
    Abstract: The present invention is directed to the topical application of the malonamide ACAT inhibitors described by Formula I. Other aspects of the invention are directed to topical formulations of these diamides, their use to treat sebaceous gland disorders and their use to alleviate oily skin.
    Type: Application
    Filed: March 4, 2013
    Publication date: July 11, 2013
    Applicant: Medicis Pharmaceutical Corporation
    Inventors: Catherine R. Kostlan, Raj Neil Raheja, Meera Tugnait, Kimberly Wade
  • Patent number: 8476208
    Abstract: Disclosed are a water-soluble metal-processing agent and a coolant both of which have excellent microbial deterioration resistance and are less likely to go rotten, a method for preparing the agent or the coolant, and a metal processing method. The water-soluble metal-processing agent or the coolant comprises an N,N,N?,N?-tetraalkyldiamine compound. The metal processing method is characterized by processing a metal of interest by using the water-soluble metal-processing agent or the coolant.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: July 2, 2013
    Assignee: Yushiro Chemical Industry Co., Ltd.
    Inventors: Toru Kadokawa, Akio Saito
  • Publication number: 20130158067
    Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, Rz, A, m, n, p, q, s, and positions a and b are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: December 17, 2012
    Publication date: June 20, 2013
    Applicant: ABBVIE INC.
    Inventor: AbbVie Inc.
  • Patent number: 8466200
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: February 7, 2012
    Date of Patent: June 18, 2013
    Assignee: Merck Patent GmbH
    Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
  • Publication number: 20130123300
    Abstract: A compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, is provided. Also, a composition containing a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents, is provided. Further, use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof for anti-apoptosis is provided, preventing or treating a disease or disorder associated with apoptosis; especially for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Application
    Filed: May 14, 2010
    Publication date: May 16, 2013
    Applicant: CHINESE PLA GENERAL HOSPITAL
    Inventors: Kunlun He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Bai
  • Publication number: 20130065963
    Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Application
    Filed: July 17, 2012
    Publication date: March 14, 2013
    Applicant: Georgetown University
    Inventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
  • Patent number: 8383652
    Abstract: Novel biaromatic compounds that modulate peroxisome proliferator-activator receptors, known as PPAR, having the formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively, in cosmetic compositions.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: February 26, 2013
    Assignee: Galderma Research & Development
    Inventors: Jean-Guy Boiteau, Laurence Clary, Laurent Chantalat, Michel Rivier
  • Publication number: 20120329799
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more carboxamide fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. Group (A): a group consisting of thifluzamide, oxadixyl, pencycuron, benalaxyl-M, fenhexamid, furametpyr, isopyrazam, isotianil, mepronil, tecloftalam, boscalid, fluopyram, fluopicolide, carpropamid, diclocymet, mandipropamid, dimethomorph, flumorph, penthiopyrad, and bixafen.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 27, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Publication number: 20120322765
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more inorganic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. group (A): a group consisting of fludioxonil, pencycuron, ametoctradin, chloroneb, chlorothalonil, oxine-copper, cyflufenamid, dichlofluanid, dicloran, diethofencarb, dinocap, dithianon, edifenphos, fenaminosulf, fentin, fluazinam, fluoroimide, flusulfamide, flutianil, fosetyl-Al, hydrargaphen, iprobenfos, metrafenon, milneb, penflufen, phosdiphen, phthalide, prothiocarb, pyrazophos, sedaxane, silthiofam, spiroxamine, tebufloquin, and tolyfluanid.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 20, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Publication number: 20120276121
    Abstract: The present invention relates to the use of inhibitors of scavenger receptor class proteins, in particular ScarB1 for the production of a medicament for treatment of and/or prophylaxis against infections, involving liver cells and/or hematopoietic cells, in particular malaria.
    Type: Application
    Filed: July 13, 2012
    Publication date: November 1, 2012
    Applicants: INSTITUTO DE MEDICINA MOLECULAR, FACULDADE DE MEDICINA DA UNIVERSIDADE DE LISBOA, CENIX BIOSCIENCE GMBH
    Inventors: MICHAEL HANNUS, CECILIE MARTIN, MARIA M. MOTA, MIGUEL PRUDENCIO, CHRISTINA DIAS RODRIGUES
  • Patent number: 8283378
    Abstract: Novel phenylurea compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: October 9, 2012
    Assignee: Galderma Research & Development
    Inventor: Thibaud Portal
  • Patent number: 8247454
    Abstract: A liquid antibacterial soap comprising trichlorocarbanilide, wherein the composition includes, 0.1-5 wt. % trichlorocarbanilide, 0-40 wt. % water, 0.1-40 wt. % of a surfactant or mixture of surfactants, 10-60 wt. % of lower glycols to render the composition visually clear and stable, and 0.1-10 wt. % of a mixture of additional adjuvant ingredients.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: August 21, 2012
    Assignee: The Dial Corporation
    Inventors: Timothy J. Taylor, Priscilla S. Fox
  • Patent number: 8247438
    Abstract: Treatment of schizophrenia or humans suffering from conditions associated with high dopamine levels in ventral striatum or caudate nucleus administers the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: August 21, 2012
    Assignee: Neuropill, Inc.
    Inventor: Ahmed Elkashef
  • Patent number: 8226963
    Abstract: The present invention provides lignin-pesticide complexes, methods for making lignin-pesticide complexes, and methods for treating or controlling insect infestations on animals by administering such complexes. Advantageously, the lignin-pesticide complexes of the present invention can be used in feed-through products to control insect infestation on livestock or pets. Various insects such as face flies, house flies, stable flies, and horn flies can be controlled and treated using the feed-through products of the present invention.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: July 24, 2012
    Assignee: Wellmark International
    Inventors: Kim W. Yang, Dennis Lee Murphy, Casey Shane White, Maria N. Parfenova, Joe Doyle McDaniel, Jinren Ko
  • Publication number: 20120172396
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Application
    Filed: February 7, 2012
    Publication date: July 5, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Denis CARNIATO, Christine CHARON, Johannes GLEITZ, Didier ROCHE, Bjoern HOCK
  • Publication number: 20120135974
    Abstract: A synergistic antimicrobial composition containing 3-iodo-2-propynyl-butylcarbamate and fluometuron.
    Type: Application
    Filed: July 28, 2010
    Publication date: May 31, 2012
    Inventors: Emerentiana Sianawati, Sangeeta S. Ganguly
  • Patent number: 8173841
    Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: May 8, 2012
    Assignee: Xention Limited
    Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
  • Publication number: 20120040986
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: August 11, 2011
    Publication date: February 16, 2012
    Inventors: Bernd RIEDL, Jacques DUMAS, Uday KHIRE, Timothy B. LOWINGER, William J. SCOTT, Roger A. SMITH, Jill E. WOOD, Mary-Katherine MONAHAN, Reina NATERO, Joel RENICK, Robert N. SIBLEY
  • Patent number: 8093266
    Abstract: Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.
    Type: Grant
    Filed: January 2, 2008
    Date of Patent: January 10, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Dahmann, Eugene Richard Hickey, Xiang Li, Wang Mao, Daniel R. Marshall, Tina M. Morwick, Robert Sibley, Roger John Snow, Ronald J. Sorcek, Frank Wu, Erick Richard Roush Young
  • Patent number: 8088826
    Abstract: This invention relates to tetrahydro-Naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tethrahydro—Naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
    Type: Grant
    Filed: April 15, 2008
    Date of Patent: January 3, 2012
    Assignee: Xention Limited
    Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
  • Patent number: 8076332
    Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.
    Type: Grant
    Filed: December 26, 2007
    Date of Patent: December 13, 2011
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Patent number: 8053449
    Abstract: Various methods of administering medication(s) that inhibit the nonenzymatic formation of glycation and dehydration condensation complexes known as advanced glycation end-products (AGEs) or modulate the advanced glycation end-product receptor (RAGE) are provided. Also, a medication releasing medical devices, wherein at least a portion of the medical device releasably includes at least one of these medication(s) are provided.
    Type: Grant
    Filed: October 2, 2006
    Date of Patent: November 8, 2011
    Assignee: Cell Viable Corporation
    Inventor: Jill D. Fabricant
  • Patent number: 8048896
    Abstract: Various methods of administering medication(s) that inhibit the nonenzymatic formation of glycation and dehydration condensation complexes known as advanced glycation end-products (AGEs) or modulate the advanced glycation end-product receptor (RAGE) are provided.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: November 1, 2011
    Assignee: Cell Viable Corporation
    Inventor: Jill D. Fabricant
  • Publication number: 20110262386
    Abstract: Disclosed herein, in certain embodiments, is a method for treating an MIF-mediated disorder. In some embodiments, the method comprises administering an active agent that inhibits (i) MIF binding to CXCR2 and CXCR4 and/or (ii) MIF-activation of CXCR2 and CXCR4; (iii) the ability of MIF to form a homomultimer; or a combination thereof.
    Type: Application
    Filed: March 20, 2009
    Publication date: October 27, 2011
    Applicant: CAROLUS THERPEUTICS, INC.
    Inventors: Jürgen Bernhagen, Joshua Robert Schultz, Benedikt Vollrath, Alma Zernecke, Christian Weber