Carbocyclic Ring Attached Indirectly To The Morpholine Ring By Nonionic Bonding Patents (Class 514/239.5)
  • Patent number: 8637058
    Abstract: Composition for controlling phytopathogens comprising compound of the formula: wherein: R1 represents H, or a CO—R? acyl group; R2, the same or different when n is equal to 2, is a halogen, optionally selected from fluorine, chlorine, bromine or iodine; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C1-C9 thioalkyl group; a C1-C9 halothioalkyl group; a C3-C9 cycloalkyl group; a C2-C10 carboalkoxyl group; a cyano group; a hydroxyl group; R? represents a hydrogen; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C2-C10 carboalkoxyl group; a phenyl group; n is a number ranging from 0 to 2; X represents an oxygen atom, a nitrogen or sulfur atom in combination with a fungicide; method for controlling phytopathogens with compound of formula (1) with or without another fungicide.
    Type: Grant
    Filed: November 18, 2002
    Date of Patent: January 28, 2014
    Assignee: Isagro S.p.A.
    Inventors: Lucio Filippini, Marilena Gusmeroli, Alexia Elmini, Carlo Garavaglia, Luigi Mirenna
  • Publication number: 20140024645
    Abstract: Phenoxy acetic acids and phenyl propionic acids and their use in treating type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, or obesity are provided herein. The present compounds are activators of PPAR? and may be useful for treating conditions mediated by the same.
    Type: Application
    Filed: September 3, 2013
    Publication date: January 23, 2014
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
  • Publication number: 20140024650
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
  • Publication number: 20140024532
    Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of formula I wherein R1 is difluoromethyl or trifluoromethyl and X is chloro, fluoro or bromo; and (B) at least one compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants, especially rust diseases on soybean plants.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 23, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
  • Publication number: 20140005196
    Abstract: This invention offers an effective method of inhibiting the expression of apolipoprotein E by mammalian cells. Apolipoprotein E is a protein that plays a significant role in the development of Alzheimer's Disease in humans. The method comprises administering an effective amount of a triarylmethyl amine compound having the general formula: wherein the R1 group may comprise acyclic amines and aliphatic amines. The R2 group may comprise one of three aryl varieties: aryl, substituted aryl, or heterocycle. Triarylamine compounds inhibit apolipoprotein E expression in mammalian cells. In one aspect of the invention the mammalian cells may be human cells, and more specifically may be human brain cells.
    Type: Application
    Filed: June 28, 2012
    Publication date: January 2, 2014
    Applicants: California State University Fullerton, California State University Fresno
    Inventors: Santanu Maitra, Nilay Patel
  • Patent number: 8609658
    Abstract: The invention provides well defined N,N-dialkylalkenyl ester compounds for treating glaucoma or ocular hypertension. The esters of the invention are particularly advantageous due to their stability in aqueous solutions.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: December 17, 2013
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, David W. Old
  • Publication number: 20130296271
    Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cell
    Type: Application
    Filed: December 27, 2011
    Publication date: November 7, 2013
    Applicant: SDS Biotech K.K.
    Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Tomoko Muraki, Ryutaro Katsuki
  • Publication number: 20130281292
    Abstract: The novel active compound combinations of a carboxamide of the general formula (I) (group 1) in which R, G, R1 and A have the meanings given in the description and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 24, 2013
    Inventors: Ulrike WACHENDORFF-NEUMANN, Peter DAHMEN, Ralf DUNKEL
  • Publication number: 20130281452
    Abstract: Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Inventors: Gregor BAHRENBERG, Sven KUEHNERT, Simon LUCAS, Wolfgang SCHROEDER
  • Patent number: 8551993
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: October 8, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
  • Publication number: 20130261122
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Applicant: N30 Pharmaceuticls, Inc.
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Publication number: 20130261120
    Abstract: The present invention relates to: *combinations of: component A: one or more omega-carboxyaryl-substituted diphenyl urea compounds of general formula (I), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (II), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; *use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and *a kit comprising such a combination.
    Type: Application
    Filed: September 29, 2011
    Publication date: October 3, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Florian Pühler, Marion Hitchcock
  • Patent number: 8546583
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a and (Rx)n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 30, 2007
    Date of Patent: October 1, 2013
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
  • Publication number: 20130244874
    Abstract: The present invention provides a composition comprising a) at least 1% by weight of copolymer synthesized from monomers M comprising i) at least one ethylenically unsaturated monomer M1 containing sulfonic acid groups, ii) at least one monomer M2 selected from C1-C4 alkyl (meth)acrylates, and iii) at least one monomer M3 selected from C6-C22 alkyl (meth)acrylates; b) at least 10% by weight of organic solvent; c) not more than 10% by weight of water; d) at least 1% by weight of water-insoluble pesticide; and e) at least 1% by weight of nonionic surfactant. Further provided is a process for preparing this composition by contacting the copolymer, the organic solvent, the water-insoluble pesticide, and the nonionic surfactant. The invention relates additionally to the agrochemical application of the composition.
    Type: Application
    Filed: November 23, 2011
    Publication date: September 19, 2013
    Applicant: BASF SE
    Inventors: Murat Mertoglu, Winfried Mayer, Cedric Dieleman
  • Publication number: 20130245019
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Application
    Filed: April 30, 2013
    Publication date: September 19, 2013
    Applicant: CONGENIA SRL
    Inventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Publication number: 20130231323
    Abstract: Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
    Type: Application
    Filed: September 6, 2011
    Publication date: September 5, 2013
    Applicant: DUKE UNIVERSITY
    Inventors: Pei Zhou, Eric J. Toone
  • Publication number: 20130225588
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 29, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130217692
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Application
    Filed: September 2, 2011
    Publication date: August 22, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Publication number: 20130217660
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 12, 2011
    Publication date: August 22, 2013
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Publication number: 20130203745
    Abstract: The present invention relates to bisaryl(thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl and —NH—CO-(1-4C)alkyl, or substituted with phenoxy, benzyl, benzyloxy, phenylethyl or morpholinyl, each optionally substituted with (1-4C)alkyl, and (8-10C)bicyclic group, bicyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms or oxo; A is selected from —CO—, —NH—, —O—, —S—, —SO— or —SO2—; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substit
    Type: Application
    Filed: July 8, 2011
    Publication date: August 8, 2013
    Applicant: AbbVie B.V.
    Inventors: Wouter I. Iwema Bakker, Raymond Bronger
  • Patent number: 8501763
    Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: August 6, 2013
    Assignee: The Scripps Research Institute
    Inventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
  • Publication number: 20130196984
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicants: Siena Biotech S.p.A., Hoffmann-La Roche Inc.
    Inventors: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
  • Publication number: 20130190288
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130190296
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: November 20, 2012
    Publication date: July 25, 2013
    Applicant: Dendreon Corporation
    Inventor: Dendreon Corporation
  • Publication number: 20130184238
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • 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
  • Publication number: 20130158035
    Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.
    Type: Application
    Filed: August 23, 2011
    Publication date: June 20, 2013
    Applicant: Brigham Young University
    Inventor: Marc Hansen
  • Publication number: 20130137690
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 28, 2013
    Publication date: May 30, 2013
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Matthew G. Stanton, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20130129839
    Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, N-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.
    Type: Application
    Filed: September 1, 2011
    Publication date: May 23, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Vann Gregory, Steven Gutteridge, Andrew Edmund Taggi, James Francis Bereznak
  • Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Patent number: 8435968
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: May 7, 2013
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Publication number: 20130102610
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.
    Type: Application
    Filed: December 7, 2012
    Publication date: April 25, 2013
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventor: High Point Pharmaceuticals, LLC
  • Patent number: 8404673
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: September 30, 2011
    Date of Patent: March 26, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20130071353
    Abstract: Inhibitors of retroviral propagation, methods of treatment and prevention of retroviral infections using the inhibitors, and pharmaceutical compositions including the inhibitors, are disclosed.
    Type: Application
    Filed: March 14, 2011
    Publication date: March 21, 2013
    Applicant: TRANA DISCOVERY, INC
    Inventors: Richard H. Guenther, Jerzy R. Szewczyk
  • Publication number: 20130052248
    Abstract: An item of clothing (10) for daily pharmacological treatment of a fungal infection, comprising: a textile material (20) to manage moisture when the item of clothing (10) is worn; microcapsules (30) grafted on the textile material (20); and antifungal agents encapsulated within the microcapsules (30) to pharmacologically treat the fungal infection when released from the microcapsules (30).
    Type: Application
    Filed: August 26, 2011
    Publication date: February 28, 2013
    Inventors: Marcus Chun Wah YUEN, Joanne Yiu Wan YIP, Kevin CHEUK, Chi Wai KAN, Shuk Yan CHENG
  • Publication number: 20130040954
    Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:
    Type: Application
    Filed: April 3, 2012
    Publication date: February 14, 2013
    Inventors: Rosemarie MANG, Werner HEILMAYER, Rudolf BADEGRUBER, Dirk B. STRICKMANN, Rodger NOVAK, Mathias FERENCIC, Atchyuta Rama Chandra Murty BULUSU
  • Publication number: 20130029992
    Abstract: The invention provides well defined N,N-dialkylalkenyl ester compounds for treating glaucoma or ocular hypertension. The esters of the invention are particularly advantageous due to their stability in aqueous solutions.
    Type: Application
    Filed: July 25, 2012
    Publication date: January 31, 2013
    Applicant: Allergan, Inc.
    Inventors: Robert M. Burk, David W. Old
  • Patent number: 8362016
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: January 29, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
  • Patent number: 8343972
    Abstract: The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: January 1, 2013
    Assignee: Nabriva Therapeutics AG
    Inventors: Rosemarie Mang, Heinz Berner
  • Patent number: 8338405
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: December 25, 2012
    Assignee: Dart Neuroscience LLC
    Inventors: Terence P. Keenan, Alan P. Kaplan
  • Publication number: 20120322761
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20120309763
    Abstract: A pharmaceutical composition intended to be applied to a perforated nail is described. In particular, a composition is descirbed that includes an antifungal agent that is in the form of an acid salt, advantageously a hydrochloride; and a solvent system; and advantageously a cationic or positively charged amphoteric surfactant. The described composition can have a viscosity of less than 500 cPs.
    Type: Application
    Filed: December 17, 2010
    Publication date: December 6, 2012
    Applicant: GALDERMA PHARMA S.A.
    Inventors: Claire Mallard, Nathalie Willcox
  • Publication number: 20120301552
    Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
    Type: Application
    Filed: December 23, 2011
    Publication date: November 29, 2012
    Applicant: JAPAN TOBACCO INC.
    Inventors: Yuko Shinagawa, Teruhiko Inoue, Toshihiro Kiguchi, Taku Ikenogami, Naoki Ogawa, Kenji Fukuda, Takashi Nakagawa, Masanori Shindo, Yuki Soejima
  • Publication number: 20120295910
    Abstract: The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: August 1, 2012
    Publication date: November 22, 2012
    Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
  • Publication number: 20120277193
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: September 20, 2010
    Publication date: November 1, 2012
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Frederick P. Roth, Murat Cokol, Hon Nian Chua
  • Publication number: 20120251492
    Abstract: Provided are a triterpene derivative represented by a general formula (I), a pharmaceutically acceptable salt thereof, and an agent for preventing or treating chronic hepatitis C comprising the triterpene derivative or the salt as an active ingredient: [in the formula (I), R1 represents a carboxyl group, a hydroxymethyl group, —CH2OSO3H, or and R2 represents —OR3 or —O— (CH2) m-OR4, where R3 represents a benzyl group which may be substituted with a hydroxymethyl group, a dimethylaminomethyl group, a phenylaminomethyl group, a morpholinomethyl group, a carboxyl group, or a formyl group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or a hydroxy C1-6 alkyl group, R4 represents a phenyl group which may be substituted with a carboxyl group, and m represents an integer of 1 to 3, with the proviso that a case where R1 is —CH2OH, and R3 is a C1-6 alkyl group, a C2-6 alkenyl group, or a benzyl group is excluded].
    Type: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Makoto Ishikawa, Shigeki Suzuki, Makoto Aoki, Nobuto Minowa, Kokichi Suzuki
  • Patent number: 8273740
    Abstract: The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.
    Type: Grant
    Filed: August 23, 2005
    Date of Patent: September 25, 2012
    Assignee: Actelion Pharmaceuticals, Ltd.
    Inventors: Heinz Fretz, Markus Gude, Kurt Hilpert, Julien Pothier, Markus Riederer, Matthias Steger
  • Publication number: 20120234721
    Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.
    Type: Application
    Filed: September 9, 2011
    Publication date: September 20, 2012
    Applicant: Neurotherapeutics Pharma, Inc.
    Inventors: Daryl W. HOCHMAN, John J. Partridge
  • Publication number: 20120232080
    Abstract: The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-? and should be useful for treating conditions mediated by the same.
    Type: Application
    Filed: May 8, 2012
    Publication date: September 13, 2012
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventor: Soren Ebdrup
  • Publication number: 20120225883
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 14, 2012
    Publication date: September 6, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang