Amino Nitrogen, Not Bonded Directly To Carbonyl, Containing Patents (Class 564/157)
  • Publication number: 20140038168
    Abstract: The present invention relates to a method of designing an inhibitor of the binding of HIV (human immunodeficiency virus) glycoprotein (gp)120 to a CD4-receptor or to the integrin alpha4 beta7 (a4b7). The inhibitor interacts with at least two amino acid residues comprised in six motifs within the 3-dimensional structure of gp120. Also provided are compounds, pharmaceutical compositions thereof and uses thereof in the development of an inhibitor of the binding of a HIV gp120 to a CD4-receptor or an integrin alpha4 beta7 (a4b7). The inhibitors are useful for the prevention or treatment of an HIV infection and/or diseases associated with an HIV infection.
    Type: Application
    Filed: October 27, 2011
    Publication date: February 6, 2014
    Applicant: KFLP BIOTECH, LLC
    Inventors: Andrey Vinnik, Peter Fedichev, Maxim Kholin, Christopher Molloy, Aron Katz
  • Publication number: 20140031370
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20140011857
    Abstract: The invention provides for novel compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.
    Type: Application
    Filed: September 12, 2011
    Publication date: January 9, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Robert A. Casero, Ian Bytheway, Patrick M. Woster
  • Patent number: 8624022
    Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: January 7, 2014
    Assignee: UCB Pharma, S.A.
    Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
  • Patent number: 8614238
    Abstract: The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W, AR1, n are as defined in claim 1.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: December 24, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Bradford S. Hamilton, Juergen Mack, Norbert Redemann, Corinna Schoelch
  • Publication number: 20130310577
    Abstract: Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with R4 being a branched C3-6 alkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10).
    Type: Application
    Filed: July 11, 2013
    Publication date: November 21, 2013
    Applicant: DSM IP ASSETS B.V.
    Inventors: Ben DE LANGE, Anna Maria Cornelia Francisca CASTELIJNS, Johannes Gerardus DE VRIES, Andreas Hendrikus Maria DE VRIES, Jeroen Antonius Franciscus BOOGERS
  • Publication number: 20130289112
    Abstract: Salts of kukoamine B, their preparation method and their pharmaceutical use in preparation of drugs for preventing and treating sepsis. Experiments indicate that salts of kukoamine B have a good effect on antagonizing the key factors inducing sepsis, and can be used in the preparation of drugs for preventing and treating sepsis. Under the current circumstances of the lack of effective measures for the treatment of sepsis in clinical practice, the medicinal formulations, which comprise the salts of kukoamine B, pharmaceutically acceptable carrier and/or diluent, provide a new approach for the prevention and treatment of sepsis.
    Type: Application
    Filed: March 21, 2011
    Publication date: October 31, 2013
    Applicant: TIANJIN CHASESUN PHARMACEUTICAL CO., LTD
    Inventors: Jiang Zheng, Xinchuan Zheng, Xin Liu, Hong Zhou, Ning Wang, Hongwei Cao, Yan Li, Yongling Lu, Kecen Zhao, Jingcheng Yang, Yang Yang, Yuanfeng Zhu, Guo Wei, Min Huang
  • Publication number: 20130281703
    Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.
    Type: Application
    Filed: March 13, 2013
    Publication date: October 24, 2013
    Inventors: Lin CHEN, Nimanthi JAYATHILAKA, Aidong HAN, Nicos A. PETASIS
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20130261132
    Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: October 3, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Per Vedso, Lars Kristian Albert BlÆher
  • Publication number: 20130253142
    Abstract: A novel separating agent for protein purification which not only can adsorb proteins in a sufficient amount for protein purification from a low concentration buffer but also can desorb the adsorbed protein easily just by altering the pH of the buffer and a simple and economical method for its production and a method for protein purification using it. One or two ligands selected from the group consisting of a ligand represented by the following formula (1): (wherein m is an integer of from 2 to 6) and a ligand represented by the following formula (2): (wherein each of R1 and R2 is independently a hydrogen atom or a C1-4 alkyl group, and n is an integer of from 1 to 6) are immobilized on a support via a urethane bond without intervention of a spacer arm.
    Type: Application
    Filed: May 17, 2013
    Publication date: September 26, 2013
    Applicant: TOSOH CORPORATION
    Inventors: Seiji MASUMOTO, Katsuo KOMIYA, Koji NAKAMURA
  • Publication number: 20130245084
    Abstract: Compounds of general formula (I) their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: LEO PHARMA A/S
    Inventor: Kristoffer Mansson
  • Publication number: 20130244262
    Abstract: The present invention provides a cardiomyocyte- and/or cardiac progenitor cell-proliferating agent comprising at least one compound selected from the group consisting of: a GSK3? inhibitor, ERK dephosphorylation inhibitor, Raf activator, CaMK2 inhibitor and p38 inhibitor; and a method for proliferating cardiomyocytes and/or cardiac progenitor cells using the agent.
    Type: Application
    Filed: November 17, 2011
    Publication date: September 19, 2013
    Applicant: KYOTO UNIVERSITY
    Inventors: Jun Yamashita, Hideki Uosaki
  • 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: 20130225841
    Abstract: A method for preparing Aliskiren and intermediate thereof, which comprises the following steps: reacting 4-bromo-1-methoxy-2-(3-methoxypropoxy)benzene with magnesium isopropyl chloride and n-BuLi to obtain the compound of formula XXII; reacting the product of methylsulfonylation of the compound of formula XIX with anhydrous LiBr to obtain the compound of formula XXI; obtaining the intermediate of Aliskiren shown as formula XV by reacting the compound of formula XXII with the compound of formula XXI in an ether as the solvent and in the presence of a catalyst containing iron; then reacting the compound of formula XV with the compound of formula VII to obtain the compound of formula XXIII, following removing R1 from the amino group and obtaining Aliskiren shown as formula I.
    Type: Application
    Filed: April 19, 2010
    Publication date: August 29, 2013
    Applicant: Zhejiang Tianyu Pharmaceutical Co., Ltd.
    Inventors: Yongjun Tu, Yi Zhang, Rongde Cheng, Lingchao Peng
  • 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: 20130190340
    Abstract: Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein.
    Type: Application
    Filed: June 30, 2011
    Publication date: July 25, 2013
    Applicant: Brandeis University
    Inventors: Lizbeth K. Hedstrom, Marcus Long, Deviprasad R. Gollapalli
  • Patent number: 8487132
    Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: July 16, 2013
    Assignees: Shandong Luye Pharmaceutical Co. Ltd.
    Inventor: Luping Zhang
  • Publication number: 20130172388
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher Education
    Inventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
  • Patent number: 8445538
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: May 21, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Xibin Liao, Roman Kats-Kagan, John E. Stelmach, Emma R. Parmee
  • Publication number: 20130102677
    Abstract: Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Forms A, B, and D, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed.
    Type: Application
    Filed: September 15, 2012
    Publication date: April 25, 2013
    Applicant: THE BROAD INSTITUTE, INC.
    Inventors: Edward Holson, Florence F. Wagner, G. Patrick Stahly
  • Publication number: 20130071899
    Abstract: A new route of synthesis of the compound Aliskiren of formula (I), used in the treatment of hypertension, is described.
    Type: Application
    Filed: June 3, 2011
    Publication date: March 21, 2013
    Applicant: Chemo Iberica, S.A.
    Inventors: Maurizio Taddei, Adele Russo, Elena Cini, Renata Riva, Marcello Rasparini, Luca Carcone, Luca Banfi, Romina Vitale, Stephen Roseblade, Antonio Carlo Zanotti-Gerosa
  • Publication number: 20130053412
    Abstract: The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W, AR1, n are as defined in claim 1.
    Type: Application
    Filed: October 15, 2010
    Publication date: February 28, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Bradford S. Hamilton, Juergen Mack, Norbert Redemann, Corinna Schoelch
  • Publication number: 20130035328
    Abstract: The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections.
    Type: Application
    Filed: July 19, 2012
    Publication date: February 7, 2013
    Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
  • Publication number: 20130030359
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
    Type: Application
    Filed: January 21, 2011
    Publication date: January 31, 2013
    Applicant: Ascendis Pharma A/S
    Inventors: Dirk Vetter, Harald Rau
  • Publication number: 20120329724
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.
    Type: Application
    Filed: September 7, 2012
    Publication date: December 27, 2012
    Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
  • Publication number: 20120321560
    Abstract: This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R1:-alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4, R3:—COOH, —OH, —SH, —NH2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R4: H, succinimidyl group, R2: —H,-alkyl. In II: R1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC?C(CN)2, —HC?CHNO2, -alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine.
    Type: Application
    Filed: April 17, 2010
    Publication date: December 20, 2012
    Inventors: Marquiza Sablón Carrazana, Chryslaine Rodriguez-Tanty, Alejandro Perera Pintado, Suchitil Rivera Marrero, Rafaela Perez Perera, Rosa Maria López Barroso, Anais Prats Capote, Hermán Vélez Castro, Carlos Serafin Pérez Martínez, Pedro Valdés Sosa
  • Publication number: 20120272462
    Abstract: The present invention relates to a compound of formula (I), where X, Y, T and Z are each as defined in claim 1, to its preparation and to its use.
    Type: Application
    Filed: January 17, 2012
    Publication date: November 1, 2012
    Applicant: DyStar Colours Deutschland GmbH
    Inventors: Roxana Barbieru, Carsten Harfmann, Werner Russ
  • Publication number: 20120272990
    Abstract: Dyes, compositions comprising dyes and methods for using the same are provided.
    Type: Application
    Filed: April 6, 2012
    Publication date: November 1, 2012
    Applicant: Living Proof, Inc.
    Inventors: Jana Lewis, Lorna Nagamoottoo-Casse, David Puerta
  • Publication number: 20120258960
    Abstract: The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.
    Type: Application
    Filed: August 26, 2010
    Publication date: October 11, 2012
    Applicant: IMTM GMBH
    Inventors: Siegfried Ansorge, Ute Bank, Karsten Nordhoff, Peter Roehnert, Sofia Stefin, Frank Striggow, Michael Taeger
  • Publication number: 20120238676
    Abstract: Oligomeric carbodiimides comprising at least one heterocyclic end group are used as stabilizers for polymers. The oligomeric carbodiimides may be compounds of the general formula (I), where A1, A2 are each independently, identically or differently, hydrocarbon groups having 2 to 20 carbon atoms, B1, B2 are each independently, identically or differently, heterocycles, C1-C30-alcohols, polyetherols, polyesterols, amines, polyether amines, polyester amines, thioalcohols, polyether thiols, polyester thiols, R1, R2 are each independently, identically or differently, n is an integer from 2 to 100, and wherein A1, A2, B1 and B2 may each be substituted at any desired position by C1-C20-alkyl, C2-C20-alkenyl, C2-C20-alkynyl, C1-C20-alkoxy, carbonyl oxygen (?O) or halogen, with the proviso that at least one B1 or B2 substituent is a heterocyclic end group. Processes for stabilizing polymers against hydrolysis using oligomeric carbodiimides are also disclosed.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 20, 2012
    Applicant: BASF SE
    Inventors: THEO SMIT, LAURENCE POTTIE, SIMONE SCHILLO, VOLKER FRENZ, ROELOF VAN DER MEER
  • Publication number: 20120238763
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: November 18, 2010
    Publication date: September 20, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki Murase, Toshihito Kumagai, Hisaya Wada, Hisahide Tanimoto, Koumei Ohta, Yoshihiro Kimura
  • Publication number: 20120225891
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: March 22, 2012
    Publication date: September 6, 2012
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20120220663
    Abstract: The present invention provides polymorphic forms of aliskiren hemifumarate, and processes for preparation thereof and for the preparation of the amorphous form of aliskiren hemifumarate. The present invention also provides pharmaceutical compositions comprising the aliskiren hemifumarate crystalline forms T1, T3 or T4, T5, T6, T7, T8 and at least one pharmaceutically acceptable excipient, and the use of these pharmaceutical compositions in the treatment of hypertension.
    Type: Application
    Filed: September 2, 2010
    Publication date: August 30, 2012
    Applicants: TEVA PHARMACEUTICALS USA, INC., TEVA PHARMACEUTICAL INDUSTRIES LTD.
    Inventors: Marina Etinger, Rinat Moshkovits Kaptsan, Ariel Mittelman
  • Publication number: 20120196916
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Application
    Filed: April 9, 2012
    Publication date: August 2, 2012
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Publication number: 20120196865
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Application
    Filed: July 19, 2010
    Publication date: August 2, 2012
    Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20120184520
    Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 19, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
  • Patent number: 8222456
    Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: July 17, 2012
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Dahui Liu, Gregory N. Tew, Michael L. Klein
  • Publication number: 20120178666
    Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 12, 2012
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
  • Publication number: 20120165555
    Abstract: The present invention provides a novel process for opening a lactone and/or a lactam ring. More particularly, the present invention provides a process that employs a novel catalyst in the opening of a lactone ring and/or a lactam ring. Additionally, the present invention also provides a novel deprotection process of any protecting group present in either the lactone ring-containing and/or lactam ring-containing compound and/or in the ring-opened product thereof.
    Type: Application
    Filed: August 11, 2010
    Publication date: June 28, 2012
    Inventors: Megan Alene Foley, Timothy F. Jamison, Oljan Repic
  • Publication number: 20120165276
    Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
    Type: Application
    Filed: May 6, 2008
    Publication date: June 28, 2012
    Applicant: Mpex Pharmaceuticals, Inc.
    Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
  • Patent number: 8207361
    Abstract: The present invention relates to solid crystalline Tigecycline, and crystalline forms thereof.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: June 26, 2012
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Evgeny Tsiperman, Sigalit Levi, Judith Aronhime, Tamas Koltai
  • Patent number: 8203005
    Abstract: The invention describes a novel technical process and novel intermediates useful for the manufacture of enantiomerically pure 8-aryloctanoic acids of the formula I which are pharmaceutically active compounds as rennin inhibitors.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: June 19, 2012
    Assignee: Carbo Design LLC
    Inventor: Milan Soukup
  • Patent number: 8198469
    Abstract: The present invention provides crystalline forms of Tigecycline, and methods of for preparation of crystalline forms and amorphous.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: June 12, 2012
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Evgeny Tsiperman, Sofia Gorohovsky-Rosenberg, Slavik Yurkovski, Sergei Fine, Tamás Koltai, Sigalit Levi, Leonid Metsger, Michal Rafilovich
  • Patent number: 8198470
    Abstract: The present invention provides processes for the preparation of crystalline forms of Tigecycline.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: June 12, 2012
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Sigalit Levi, Michal Rafilovich, Sofia Gorohovsky-Rosenberg, Slavik Yurkovski, Sergei Fine, Leonid Metsger, Evgeny Tsiperman
  • Publication number: 20120142668
    Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
    Type: Application
    Filed: August 11, 2010
    Publication date: June 7, 2012
    Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
  • Publication number: 20120142781
    Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
    Type: Application
    Filed: February 8, 2012
    Publication date: June 7, 2012
    Applicant: Magnesium Diagnostics Inc.
    Inventor: Ibert Clifton Wells
  • Publication number: 20120142646
    Abstract: The present invention provides compounds of formula (I) wherein k, Ar, R2, R3, R4, R5, R4?, R5?, R6, R7, A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 19, 2007
    Publication date: June 7, 2012
    Inventors: Lilian Alcaraz, Roger Victor Bonnert, Stephen Connolly, Anthony Ronald Cook, Adrian Fisher, Alexander Humphries, Piotr Raubo
  • Publication number: 20120135984
    Abstract: Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.
    Type: Application
    Filed: May 1, 2010
    Publication date: May 31, 2012
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty, Geoffrey Richard Heintzelman, Jeffrey D. Yingling, Casey Kopczynski
  • Patent number: 8178724
    Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: May 15, 2012
    Assignees: Shandong Luye Pharmaceutical Co., Ltd.
    Inventor: Luping Zhang