Chalcogen Attached Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 544/398)
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Patent number: 8969353
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: March 3, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Publication number: 20150011566
    Abstract: The present invention provides N-phenylpiperazine derivatives for use as multiple binders and/or antagonists of ?1A adrenoceptors, ?1D adrenoceptors and 5-HT1A serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions.
    Type: Application
    Filed: January 4, 2013
    Publication date: January 8, 2015
    Inventors: Claudia Lucia Martins Da Silva, Fernanda Chagas Da Silva, Luana Chaves Barberato, Luciana De Camargo Nascente, Jessica Barbosa Do Nascimento Viana, Renata Oliveira Silva, Laís Flávia Nunes Lemes, François German Noël, Luís Antônio Soares Romeiro
  • Patent number: 8927712
    Abstract: Process for the preparation of a mono-N-alkylpiperazine of the formula I in which R1 is C1- to C5-alkyl or 2-(2-hydroxyethoxy)ethyl, by reacting diethanolamine (DEOA) of the formula II with a primary amine of the formula H2N—R1 (III) in the presence of hydrogen and a catalyst molding, where the reaction is carried out in the liquid phase at an absolute pressure in the range from 150 to 250 bar and the amination is carried out by means of a catalyst molding, the precursor of which can be prepared according to a process in which (i) an oxidic material comprising copper oxide, aluminum oxide and lanthanum oxide is provided, (ii) pulverulent metallic copper and/or copper flakes and optionally graphite is added to the oxidic material, (iii) the mixture resulting from step ii is shaped to give a molding, where the oxidic material is obtainable by simultaneous or successive precipitation of the component copper oxide, of the component aluminum oxide and of the component lanthanum oxide and subsequent dry
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: January 6, 2015
    Assignee: BASF SE
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
  • Publication number: 20140357800
    Abstract: This invention relates to the treatment of carbon based fillers with amines, including piperazines and aziridines, to modify the surface of the filler.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 4, 2014
    Inventors: Mihael Wolfgang Backer, Thomas Chaussee, Olivier Debever, Francois De Buyl
  • Publication number: 20140352081
    Abstract: The present invention relates to a para-aminophenol compound of formula (I) the addition salts thereof with an acid and the solvates thereof, dye composition comprising the latter and a dyeing process.
    Type: Application
    Filed: September 13, 2012
    Publication date: December 4, 2014
    Applicant: L'OREAL
    Inventor: Aziz Fadli
  • Publication number: 20140343287
    Abstract: A process for the manufacture of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine and pharmaceutically acceptable salts is disclosed that involves reacting compounds of formula II, III, IV under Pd catalysis and in presence of phosphine ligands to give Compound I.
    Type: Application
    Filed: December 20, 2012
    Publication date: November 20, 2014
    Inventor: Kim Lasse Christensen
  • Publication number: 20140336337
    Abstract: This invention relates to the modification of polymeric materials containing reactive carbon-to-carbon unsaturation and to amines, including piperazines, which are used in such modification. A polymeric material containing carbon-to-carbon bonds can be modified by crosslinking or to make it susceptible to crosslinking.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 13, 2014
    Inventors: Michael Wolfgang Backer, Thomas Chaussee, Olivier Debever
  • Patent number: 8884015
    Abstract: Process for the preparation of a mono-N-alkylpiperazine of the formula I in which R1 is C1- to C5-alkyl or 2-(2-hydroxyethoxy)ethyl, by reacting diethanolamine (DEOA) of the formula II with a primary amine of the formula H2N—R1 (III) in the presence of hydrogen and a supported, metal-containing catalyst, where the catalytically active mass of the catalyst, prior to its reduction with hydrogen, comprises oxygen-containing compounds of aluminum, copper, nickel and cobalt and, in the range from 0.2 to 5.0% by weight, oxygen-containing compounds of tin, calculated as SnO, and the reaction is carried out in the liquid phase at an absolute pressure in the range from 95 to 145 bar.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: November 11, 2014
    Assignee: BASF SE
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
  • Patent number: 8829002
    Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: September 9, 2014
    Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
  • Patent number: 8809591
    Abstract: The present invention is directed to a process for the manufacture of 2,3,5-trimethyl-hydro-p-benzoquinone comprising the following steps: a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone; b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formal-dehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone; c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone; wherein the organic solvent in all steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, methyl tert.-amyl ether, methoxycyclopentane and any mixtures thereof. Preferably the organic solvent used in all steps a), b) and c) is the same.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: August 19, 2014
    Assignee: DSM IP Assets B.V.
    Inventors: Werner Bonrath, Thomas Netscher, Jan Schütz, Bettina Wüstenberg
  • Publication number: 20140121211
    Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogues, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 1, 2014
    Applicant: INDIAN INSTITUTE OF SCIENCE EDUCATION AND RESEARCH -PUNE
    Inventors: Harinath CHAKRAPANI, Satish Ramesh Malwal
  • Publication number: 20140107027
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Applicant: BHI LIMITED PARTNERSHIP
    Inventors: Xianqi Kong, David Migneault, Isabelle Valade, Xinfu Wu, Francine Gervais
  • Publication number: 20130324732
    Abstract: Process for the preparation of a mono-N-alkylpiperazine of the formula I in which R1 is C1- to C5-alkyl or 2-(2-hydroxyethoxy)ethyl, by reacting diethanolamine (DEOA) of the formula II with a primary amine of the formula H2N—R1 (III) in the presence of hydrogen and a supported, metal-containing catalyst, where the catalytically active mass of the catalyst, prior to its reduction with hydrogen, comprises oxygen-containing compounds of aluminum, copper, nickel and cobalt and, in the range from 0.2 to 5.0% by weight, oxygen-containing compounds of tin, calculated as SnO, and the reaction is carried out in the liquid phase at an absolute pressure in the range from 95 to 145 bar.
    Type: Application
    Filed: May 31, 2013
    Publication date: December 5, 2013
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
  • Publication number: 20130324731
    Abstract: Process for the preparation of a mono-N-alkylpiperazine of the formula I in which R1 is C1- to C5-alkyl or 2-(2-hydroxyethoxy)ethyl, by reacting diethanolamine (DEOA) of the formula II with a primary amine of the formula H2N—R1 (III) in the presence of hydrogen and a catalyst molding, where the reaction is carried out in the liquid phase at an absolute pressure in the range from 150 to 250 bar and the amination is carried out by means of a catalyst molding, the precursor of which can be prepared according to a process in which (i) an oxidic material comprising copper oxide, aluminum oxide and lanthanum oxide is provided, (ii) pulverulent metallic copper and/or copper flakes and optionally graphite is added to the oxidic material, (iii) the mixture resulting from step ii is shaped to give a molding, where the oxidic material is obtainable by simultaneous or successive precipitation of the component copper oxide, of the component aluminum oxide and of the component lanthanum oxide and subsequent dr
    Type: Application
    Filed: May 31, 2013
    Publication date: December 5, 2013
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
  • Patent number: 8569071
    Abstract: The present teachings provide methods for analyzing one or more amine-containing compounds in one or more samples using isobaric labels and parent-daughter ion transition monitoring (PDITM). In various embodiments, the methods comprise the steps of: (a) labeling one or more amine-containing compounds with different isobaric tags from a set of isobaric tags, each isobaric tag comprising a reporter ion portion; (b) combining at least a portion of each of the isobarically labeled amine-containing compounds to produce a combined sample; (c) subjecting at least a portion of the combined sample to PDITM; (d) measuring the ion signal of one or more of the transmitted reporter ions; and (e) determining the concentration of one or more of the isobarically labeled amine-containing compounds based at least on a comparison of the measured ion signal of the corresponding reporter ion to one or more measured ion signals of a standard compound.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: October 29, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subodh B. Nimkar, Subhasish Purkayastha, Darryl Pappin, Scott Daniels
  • Publication number: 20130267536
    Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.
    Type: Application
    Filed: December 13, 2011
    Publication date: October 10, 2013
    Applicant: ALLA CHEM, LLC
    Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
  • Publication number: 20130267707
    Abstract: The invention relates to derivatives of N,N?-substituted piperazines of the general formula (I): where R1 and R2 denote linear or branched (C1-C4)alkyl, linear or branched (C1-C4)alkoxy, CH3C(?O)O or halogen; n=1-5; m=0-3; Z denotes CH2, C?O or SO2; X denotes C(?NH)NH2, C(?NH)NHC(?NH)NH2 or CH2(CHR3)pCH2SO3H, where R3 denotes H, OH, CH3C(?O)O or HOSO2O and p=0-1; and G denotes low-molecular-weight organic or mineral acid, sodium, potassium or ammonium cations, or water. Said derivatives have antiaggregant, anticoagulant and vasodilatory properties. The invention further relates to a method for producing said derivatives by reacting N-substituted piperazines either with carboxamide amidating agents or salts thereof, or with haloalkyl sulfonic acids or salts thereof in organic solvents or in water in the presence of bases. The compounds may be used for the prophylaxis and treatment of disorders of the hemostatic system.
    Type: Application
    Filed: November 8, 2011
    Publication date: October 10, 2013
    Applicant: ZAKRYTOE AKTSIONERNOE OBSCHSHESTVO "VERTEX"
    Inventors: Olga Sergejevna Veselkina, Nikolay Borisovich Viktorov, Nikolay Nikolaevich Petrishchev, Yuliya Vyacheslavovna Poplavskaya
  • Publication number: 20130261039
    Abstract: A method of removing a residue from a surface, including applying to the surface a composition including (a) a quaternary ammonium hydroxide having a general formula (I): as defined herein, and (b) a dipolar aprotic solvent substantially free of water; and removing at least a substantial portion of the residue from the surface.
    Type: Application
    Filed: March 27, 2012
    Publication date: October 3, 2013
    Applicant: SACHEM, INC.
    Inventor: Charles B. Little
  • Patent number: 8546375
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: October 1, 2013
    Assignee: AstraZeneca AB
    Inventors: Susanne Doris Margit Bökman-Winiwarter, Marlene Fredenwall, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
  • Publication number: 20130225561
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 21, 2011
    Publication date: August 29, 2013
    Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
  • Publication number: 20130211080
    Abstract: The present invention is directed to a process for the manufacture of 2,3,5-trimethyl-hydro-p-benzoquinone comprising the following steps: a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone; b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formal-dehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone; c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone; wherein the organic solvent in all steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, tert.-amyl ether, methoxycyclopentane and any mixtures thereof. Preferably the organic solvent used in all steps a), b) and c) is the same.
    Type: Application
    Filed: August 25, 2011
    Publication date: August 15, 2013
    Applicant: DSM IP ASSETS B.V.
    Inventors: Werner Bonrath, Thomas Netscher, Jan Schütz, Bettina Wüstenberg
  • Publication number: 20130209483
    Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: August 15, 2013
    Applicant: SUTTER WEST BAY HOSPITALS
    Inventor: SUTTER WEST BAY HOSPITALS
  • Patent number: 8492163
    Abstract: This invention pertains to methods, mixtures, kits and compositions pertaining to analyte determination by mass spectrometry using labeling reagents that comprise a nucleophilic reactive group that reacts with a functional group of an analyte to produce a labeled analyte. The labeling reagents can be used as isobaric sets, mass differential labeling sets or in a combination of isobaric and mass differential labeling sets.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: July 23, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
  • Publication number: 20130123243
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Application
    Filed: October 18, 2012
    Publication date: May 16, 2013
    Inventor: Celtaxsys, Inc.
  • Patent number: 8436169
    Abstract: Process for preparing 1,4-bishydroxyethylpiperazine (BHEPIP) of the formula I wherein diethanolamine (DEOA) of the formula II is reacted in the liquid phase in a reactor at a temperature in the range from 130 to 300° C. in the presence of a copper-comprising, chromium-free heterogeneous catalyst.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: May 7, 2013
    Assignee: BASF SE
    Inventors: Christof Wilhelm Wigbers, Nina Challand, Johann-Peter Melder, Udo Rheude, Roman Dostalek
  • Patent number: 8420807
    Abstract: The invention relates to a method for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo [b,f]-1,4-thiazepine and pharmaceutically acceptable salts thereof comprising the reaction of 1-[2-(hydroxyethoxy)-ethyl]piperazine with dibenzo[b,f][1,4]thiazepin-11-ylamine.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: April 16, 2013
    Assignee: Fermion Oy
    Inventors: Arne Grumann, Dzintra Muceniece, Otto Soidinsalo
  • Publication number: 20120283266
    Abstract: The invention relates to a compound of Formula (I): (A?)x-(A)-(B)-(Z)-(L)-(D), wherein: (A) is heteroaryl or aryl; each (A?), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is chosen from —N(—R1)—R2, —O—R3, and —S—R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and
    Type: Application
    Filed: April 19, 2010
    Publication date: November 8, 2012
    Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
  • Publication number: 20120225890
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Application
    Filed: March 6, 2012
    Publication date: September 6, 2012
    Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, David Larsen, David L. Coffen, Charlotte Coffen
  • Patent number: 8158790
    Abstract: The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, —(CH2)a—X1—(CH2)b—(X1: the formula —NH—, —O— or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: April 17, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shojiro Miyazaki, Yuji Nakamura, Takahiro Nagayama, Taro Tokui, Yasuyuki Ogawa
  • Publication number: 20120053180
    Abstract: This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.
    Type: Application
    Filed: March 17, 2011
    Publication date: March 1, 2012
    Applicant: CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.
    Inventors: Sang Uk Kang, Min Jeong Kim, Byung Nam Kang, Wei Tan, Albert Charles Gyorkos, Suk Young Cho
  • Publication number: 20120040969
    Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
    Type: Application
    Filed: October 28, 2011
    Publication date: February 16, 2012
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
  • Patent number: 8106041
    Abstract: Medicament comprising, in a pharmaceutically acceptable vehicle, an anti-psychotic or an antidepressant (A), which, on its own, has an undesirable effect of a gain in body weight or sedation, and an antagonist and/or inverse agonist (B) of the histamine H3 receptor, the antagonist and/or inverse agonist of the histamine H3 receptor being present in a therapeutically effective amount for ensuring at least one of the following three effects: suppression or at least limitation of the undesirable effect of weight gain, suppression or limitation of the undesirable effect on alertness, epilepsy/convulsions, increase in the precognitive effect of the treatment. Use of such an antagonist or inverse agonist for the preparation of a medicament which is to ensure at least one of the said three effects in a patient treated by such an antipsychotic or antidepressant.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: January 31, 2012
    Assignee: Bioprojet
    Inventors: Jean-Charles Schwartz, Jeanne-Marie Lecomte
  • Publication number: 20120010189
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 12, 2012
    Applicant: AstraZeneca AB
    Inventors: Susanne Doris Margit Bökman-Winiwarter, Marlene FREDENWALL, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
  • Publication number: 20110306133
    Abstract: Disclosed are a culture medium, an additive, and a method for efficiently inducing the differentiation of mammalian somatic stem cells into cells having the characteristics of adipocytes under conditions of serum-free or low-serum culture medium. The culture medium for inducing the differentiation of mammalian somatic stem cells into adipocytes comprises a basal medium for culturing mammalian cells, an agent for inducing the differentiation of mammalian somatic stem cells into adipocytes, biotin, a ligand for endothelial cell differentiation gene (Edg) family receptors, vitamin C, and HEPES, which culture medium is serum-free or contains a low concentration of serum.
    Type: Application
    Filed: February 18, 2010
    Publication date: December 15, 2011
    Inventor: Yoshiyuki Hotta
  • Patent number: 8076328
    Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: December 13, 2011
    Assignee: Bayer CropScience AG
    Inventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
  • Publication number: 20110293703
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Application
    Filed: November 6, 2009
    Publication date: December 1, 2011
    Applicant: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Publication number: 20110288101
    Abstract: One aspect of the present invention relates to aqueous surgical compositions comprising a sigma-1 receptor agonist. Another aspect of the present invention relates to methods of irrigating ocular tissues during an ophthalmic surgical procedure such as cataract surgery. Such methods comprise bathing the ocular tissues with a composition comprising a sigma-1 receptor agonist.
    Type: Application
    Filed: May 20, 2011
    Publication date: November 24, 2011
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Lixin Wang, Marcia Danielle Ong, Chi-Chun Tsai, Michael Hartzer
  • Publication number: 20110281890
    Abstract: Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: July 25, 2011
    Publication date: November 17, 2011
    Inventor: Connie L. Sun
  • Publication number: 20110269775
    Abstract: Compounds of general formula (I) in which R1 and R0 have any of the meanings given in the specification have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: July 12, 2011
    Publication date: November 3, 2011
    Inventor: Connie L. Sun
  • Publication number: 20110212072
    Abstract: Described are a method and a composition for preventing and/or treating a disease related to mitochondrial dysfunction by inhibiting the fatty acid oxidation of one or more cells of an organism. Particularly, the fatty acid oxidation is inhibited by inhibiting the expression and/or activity of the enzyme Camitin-Palmitoyl-Transferase-1 (CPT-1) by means of an arylalkyl- or arlyoxyalkyl-substitued oxirane carboxylic acid or pharmaceutically acceptable salts and derivatives of the arylalkyl-substituted oxirane carboxylic acid.
    Type: Application
    Filed: April 19, 2011
    Publication date: September 1, 2011
    Applicant: MediGene AG
    Inventors: Thomas Henkel, Christoph Rehfuess
  • Publication number: 20110172239
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Application
    Filed: July 16, 2010
    Publication date: July 14, 2011
    Inventors: Alan D. SNOW, Beth NGUYEN, Gerardo CASTILLO, Virginia SANDERS, Thomas LAKE, Lesley LARSEN, Rex T. WEAVERS, Stephen LORIMER, David LARSEN, David L. COFFEN, Charlotte COFFEN
  • Patent number: 7968538
    Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: June 28, 2011
    Assignee: Galenea Corp.
    Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Silvia Noiman, Xiang Y. Yu, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
  • Patent number: 7964597
    Abstract: Disclosed are motilin agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: June 21, 2011
    Assignee: Glaxo Group Limited
    Inventors: Darren Jason Mitchell, Jonathan Thomas Seal, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
  • Publication number: 20110117125
    Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
    Type: Application
    Filed: December 31, 2008
    Publication date: May 19, 2011
    Applicants: TEKMIRA PHARMACEUTICALS CORPORATION, THE UNIVERSITY OF BRITISH COLUMBIA, ALNYLAM PHARMACEUTICALS
    Inventors: Michael J. Hope, Sean C. Semple, Jianxin Chen, Thomas D. Madden, Barbara Mui, Pieter R. Cullis, Marco A. Ciufolini, Kim F. Wong, Muthiah Manoharan, Rajeev G. Kallanthottathil
  • Patent number: 7932388
    Abstract: In some embodiments, this invention pertains to isotopically enriched N-substituted piperazines. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazines.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: April 26, 2011
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
  • Publication number: 20110070179
    Abstract: Compositions are disclosed comprising novel fluorinated cationic alcohols in a cosmetically acceptable vehicle. The fluorinated compounds alter a surface property of the hair to provide hair conditioning, for example. In embodiments, the compounds have improved water solubility and deposition properties.
    Type: Application
    Filed: September 16, 2010
    Publication date: March 24, 2011
    Applicant: Living Proof, Inc.
    Inventors: David T. Puerta, Lorna Nagamoottoo-Casse, Kevin T. Love
  • Publication number: 20110065622
    Abstract: Semiconductor processing compositions comprising amidoxime compounds having two or more amidoxime functional groups and their use in semiconductor processing to remove photoresist, polymeric materials, etching residues and copper oxides from semiconductor substrates, particularly substrates comprising copper, low-k dielectric material, titanium nitride, and/or titanium oxynitride.
    Type: Application
    Filed: September 13, 2010
    Publication date: March 17, 2011
    Inventors: Wai Mun Lee, Hua Cui, Mark A. Scialdone, Albert G. Anderson
  • Patent number: 7906341
    Abstract: This invention pertains to methods, mixtures, kits and compositions pertaining to analyte determination by mass spectrometry using labeling reagents that comprise a nucleophilic reactive group that reacts with a functional group of an analyte to produce a labeled analyte. The labeling reagents can be used as isobaric sets, mass differential labeling sets or in a combination of isobaric and mass differential labeling sets.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: March 15, 2011
    Assignee: DH Technologies Development Pte, Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
  • Publication number: 20110039819
    Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: April 9, 2009
    Publication date: February 17, 2011
    Inventors: Marion Hitchcock, Ingo Hartung