Chalcogen Attached Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 544/398)
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Publication number: 20150093365Abstract: 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: ApplicationFiled: March 14, 2013Publication date: April 2, 2015Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
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Patent number: 8969353Abstract: 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: GrantFiled: November 6, 2009Date of Patent: March 3, 2015Assignee: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
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Publication number: 20150011566Abstract: 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: ApplicationFiled: January 4, 2013Publication date: January 8, 2015Inventors: 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
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Patent number: 8927712Abstract: 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 dryType: GrantFiled: May 31, 2013Date of Patent: January 6, 2015Assignee: BASF SEInventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
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Publication number: 20140357800Abstract: This invention relates to the treatment of carbon based fillers with amines, including piperazines and aziridines, to modify the surface of the filler.Type: ApplicationFiled: December 7, 2012Publication date: December 4, 2014Inventors: Mihael Wolfgang Backer, Thomas Chaussee, Olivier Debever, Francois De Buyl
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Publication number: 20140352081Abstract: 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: ApplicationFiled: September 13, 2012Publication date: December 4, 2014Applicant: L'OREALInventor: Aziz Fadli
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Publication number: 20140343287Abstract: 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: ApplicationFiled: December 20, 2012Publication date: November 20, 2014Inventor: Kim Lasse Christensen
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Publication number: 20140336337Abstract: 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: ApplicationFiled: December 7, 2012Publication date: November 13, 2014Inventors: Michael Wolfgang Backer, Thomas Chaussee, Olivier Debever
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Patent number: 8884015Abstract: 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: GrantFiled: May 31, 2013Date of Patent: November 11, 2014Assignee: BASF SEInventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
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Patent number: 8829002Abstract: 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: GrantFiled: December 13, 2011Date of Patent: September 9, 2014Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Patent number: 8809591Abstract: 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: GrantFiled: August 25, 2011Date of Patent: August 19, 2014Assignee: DSM IP Assets B.V.Inventors: Werner Bonrath, Thomas Netscher, Jan Schütz, Bettina Wüstenberg
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Publication number: 20140121211Abstract: 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: ApplicationFiled: November 30, 2012Publication date: May 1, 2014Applicant: INDIAN INSTITUTE OF SCIENCE EDUCATION AND RESEARCH -PUNEInventors: Harinath CHAKRAPANI, Satish Ramesh Malwal
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Publication number: 20140107027Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Applicant: BHI LIMITED PARTNERSHIPInventors: Xianqi Kong, David Migneault, Isabelle Valade, Xinfu Wu, Francine Gervais
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Publication number: 20130324732Abstract: 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: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
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Publication number: 20130324731Abstract: 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 drType: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
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Patent number: 8569071Abstract: 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: GrantFiled: September 8, 2009Date of Patent: October 29, 2013Assignee: DH Technologies Development Pte. Ltd.Inventors: Subodh B. Nimkar, Subhasish Purkayastha, Darryl Pappin, Scott Daniels
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Publication number: 20130267536Abstract: 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: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: ALLA CHEM, LLCInventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Publication number: 20130267707Abstract: 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: ApplicationFiled: November 8, 2011Publication date: October 10, 2013Applicant: ZAKRYTOE AKTSIONERNOE OBSCHSHESTVO "VERTEX"Inventors: Olga Sergejevna Veselkina, Nikolay Borisovich Viktorov, Nikolay Nikolaevich Petrishchev, Yuliya Vyacheslavovna Poplavskaya
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Publication number: 20130261039Abstract: 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: ApplicationFiled: March 27, 2012Publication date: October 3, 2013Applicant: SACHEM, INC.Inventor: Charles B. Little
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Patent number: 8546375Abstract: 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: GrantFiled: July 5, 2011Date of Patent: October 1, 2013Assignee: AstraZeneca ABInventors: 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
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Publication number: 20130225561Abstract: 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: ApplicationFiled: October 21, 2011Publication date: August 29, 2013Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
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Publication number: 20130211080Abstract: 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: ApplicationFiled: August 25, 2011Publication date: August 15, 2013Applicant: DSM IP ASSETS B.V.Inventors: Werner Bonrath, Thomas Netscher, Jan Schütz, Bettina Wüstenberg
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Publication number: 20130209483Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.Type: ApplicationFiled: November 30, 2012Publication date: August 15, 2013Applicant: SUTTER WEST BAY HOSPITALSInventor: SUTTER WEST BAY HOSPITALS
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Patent number: 8492163Abstract: 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: GrantFiled: January 31, 2011Date of Patent: July 23, 2013Assignee: DH Technologies Development Pte. Ltd.Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
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Publication number: 20130123243Abstract: 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: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Inventor: Celtaxsys, Inc.
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Patent number: 8436169Abstract: 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: GrantFiled: October 28, 2011Date of Patent: May 7, 2013Assignee: BASF SEInventors: Christof Wilhelm Wigbers, Nina Challand, Johann-Peter Melder, Udo Rheude, Roman Dostalek
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Patent number: 8420807Abstract: 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: GrantFiled: January 30, 2009Date of Patent: April 16, 2013Assignee: Fermion OyInventors: Arne Grumann, Dzintra Muceniece, Otto Soidinsalo
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Publication number: 20120283266Abstract: 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, andType: ApplicationFiled: April 19, 2010Publication date: November 8, 2012Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
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Publication number: 20120225890Abstract: 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: ApplicationFiled: March 6, 2012Publication date: September 6, 2012Inventors: 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
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Patent number: 8158790Abstract: 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: GrantFiled: June 22, 2007Date of Patent: April 17, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Shojiro Miyazaki, Yuji Nakamura, Takahiro Nagayama, Taro Tokui, Yasuyuki Ogawa
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Publication number: 20120053180Abstract: 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: ApplicationFiled: March 17, 2011Publication date: March 1, 2012Applicant: 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
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Publication number: 20120040969Abstract: 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: ApplicationFiled: October 28, 2011Publication date: February 16, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: 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
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Patent number: 8106041Abstract: 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: GrantFiled: June 25, 2004Date of Patent: January 31, 2012Assignee: BioprojetInventors: Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Publication number: 20120010189Abstract: 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: ApplicationFiled: July 5, 2011Publication date: January 12, 2012Applicant: AstraZeneca ABInventors: 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
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Publication number: 20110306133Abstract: 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: ApplicationFiled: February 18, 2010Publication date: December 15, 2011Inventor: Yoshiyuki Hotta
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Patent number: 8076328Abstract: 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: GrantFiled: April 8, 2008Date of Patent: December 13, 2011Assignee: Bayer CropScience AGInventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Publication number: 20110293703Abstract: 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: ApplicationFiled: November 6, 2009Publication date: December 1, 2011Applicant: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
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Publication number: 20110288101Abstract: 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: ApplicationFiled: May 20, 2011Publication date: November 24, 2011Applicant: ALCON RESEARCH, LTD.Inventors: Lixin Wang, Marcia Danielle Ong, Chi-Chun Tsai, Michael Hartzer
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Publication number: 20110281890Abstract: 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: ApplicationFiled: July 25, 2011Publication date: November 17, 2011Inventor: Connie L. Sun
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Publication number: 20110269775Abstract: 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: ApplicationFiled: July 12, 2011Publication date: November 3, 2011Inventor: Connie L. Sun
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Publication number: 20110212072Abstract: 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: ApplicationFiled: April 19, 2011Publication date: September 1, 2011Applicant: MediGene AGInventors: Thomas Henkel, Christoph Rehfuess
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Publication number: 20110172239Abstract: 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: ApplicationFiled: July 16, 2010Publication date: July 14, 2011Inventors: 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
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Patent number: 7968538Abstract: 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: GrantFiled: January 25, 2006Date of Patent: June 28, 2011Assignee: 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
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Patent number: 7964597Abstract: Disclosed are motilin agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: GrantFiled: November 26, 2008Date of Patent: June 21, 2011Assignee: Glaxo Group LimitedInventors: Darren Jason Mitchell, Jonathan Thomas Seal, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
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Publication number: 20110117125Abstract: 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: ApplicationFiled: December 31, 2008Publication date: May 19, 2011Applicants: TEKMIRA PHARMACEUTICALS CORPORATION, THE UNIVERSITY OF BRITISH COLUMBIA, ALNYLAM PHARMACEUTICALSInventors: 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
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Patent number: 7932388Abstract: 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: GrantFiled: December 11, 2007Date of Patent: April 26, 2011Assignee: DH Technologies Development Pte. Ltd.Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
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Publication number: 20110070179Abstract: 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: ApplicationFiled: September 16, 2010Publication date: March 24, 2011Applicant: Living Proof, Inc.Inventors: David T. Puerta, Lorna Nagamoottoo-Casse, Kevin T. Love
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Publication number: 20110065622Abstract: 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: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Wai Mun Lee, Hua Cui, Mark A. Scialdone, Albert G. Anderson
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Patent number: 7906341Abstract: 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: GrantFiled: June 28, 2007Date of Patent: March 15, 2011Assignee: DH Technologies Development Pte, Ltd.Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
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Publication number: 20110039819Abstract: 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: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung