Plural Ring Oxygens In The Hetero Ring Patents (Class 514/452)
  • 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
  • Patent number: 8557862
    Abstract: A synergistic antimicrobial composition having two components. The first component is glutaraldehyde. The second component is 2,6-dimethyl-1,3-dioxan-4-yl acetate.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: October 15, 2013
    Assignee: Dow Global Technologies LLC
    Inventor: Bei Yin
  • Publication number: 20130267538
    Abstract: The invention relates the method of treatment or amelioration of mitochondrial disorders such as Alzheimer's disease, Parkinson's disease, Friedreich's ataxia (FRDA), cerebellar ataxias, Leber's hereditary optic neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, stroke (MELAS), Myoclonic Epilepsy with Ragged Red Fibers (MERFF), amyotrophic lateral sclerosis (ALS), motor neuron diseases, Huntington's disease, macular degeneration, and epilepsy, with chroman derivatives of Formula I or Formula II as described herein.
    Type: Application
    Filed: April 24, 2013
    Publication date: October 10, 2013
    Inventors: Gail WALKINSHAW, Sekhar BODDUPALLI, Bing WANG, Guy M. MILLER
  • Publication number: 20130267561
    Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.
    Type: Application
    Filed: March 7, 2013
    Publication date: October 10, 2013
    Applicant: Evolva Sa
    Inventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama, Melya Hughes Crameri, Thierry Bonnaud, Joanne Kelleher, David Pearson
  • Patent number: 8551982
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Publication number: 20130253045
    Abstract: The present invention relates to prodrugs of compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.
    Type: Application
    Filed: March 6, 2013
    Publication date: September 26, 2013
    Applicant: Evolva Sa
    Inventors: Peteris Alberts, Alexandra Santana Sorensen
  • Publication number: 20130253044
    Abstract: Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.
    Type: Application
    Filed: March 5, 2013
    Publication date: September 26, 2013
    Inventors: James D. McChesney, Gilles Tapolsky, David E. Emerson, John Marshall, Tauseef Ahmed, Allen Cohn, Michael Kurman, Manuel Modiano
  • Publication number: 20130245053
    Abstract: The present disclosure relates to pesticidal compositions and to methods for controlling pests such as insects and other arthropods. More particularly, the disclosure relates to a pesticidal compositions containing mineral oil and one or more additional components which, when used in combination, act synergistically to control insect and pest populations.
    Type: Application
    Filed: May 8, 2013
    Publication date: September 19, 2013
    Inventor: Steven R. Sims
  • Patent number: 8536130
    Abstract: Use of 1-phenyl-3-dimethylaminopropane compounds for the production of medicaments for treating neuropathic pain, preferably polyneuropathic pain, also preferably diabetic neuropathic pain, more preferably diabetic peripheral neuropathic pain, and furthermore preferably for treating diabetic peripheral neuropathy.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: September 17, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Thomas Christoph, Elmar Friderichs, Babette-Yvonne Koegel, Murielle Meen
  • Patent number: 8536196
    Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.
    Type: Grant
    Filed: January 18, 2008
    Date of Patent: September 17, 2013
    Assignee: Evolva SA
    Inventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Prathama S. Mainkar, Melya Hughes Crameri, Thierry Bonnaud, Joanne Kelleher, David Pearson
  • Publication number: 20130236420
    Abstract: The invention relates to the use of a silibinin component for the production of a medicament that is adapted for parenteral administration for the treatment of viral hepatitis, preferably of hepatitis B or C, in particular for the reduction of the virus load. The medicament preferably contains no silidianin and/or no silichristin and/or no isosilibinin.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Applicant: MADAUS GmbH
    Inventors: LUCIO CLAUDIO ROVATI, MASSIMO MARIA D'AMATO, ULRICH MENGS, RALF-TORSTEN POHL, PETER FERENCI
  • Patent number: 8524766
    Abstract: The present invention relates to novel 1-(2,3-dihydro-1,4-benzodioxin-2-yl)-methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically as dopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: September 3, 2013
    Assignee: NSAB, Filial af Neurosearch Sweden AB, Sverige
    Inventors: Clas Sonesson, Peder Svensson, Jonas Karlsson
  • Publication number: 20130217760
    Abstract: Disclosed is a method for enhancing therapeutic effect of anticancer therapies for an animal, comprising administering one or more dibenzo-p-dioxin derivative in an effective amount to the animal in anticancer therapies. The method augments therapeutic effects of an anticancer therapies, with the suppression of side effects of the anticancer therapies.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 22, 2013
    Applicant: BOTAMEDI INC.
    Inventor: BOTAMEDI INC.
  • Publication number: 20130210905
    Abstract: The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.
    Type: Application
    Filed: December 17, 2012
    Publication date: August 15, 2013
    Applicant: The Gov. of the U.S.A as Represented by the Secretary of the Dept. of Health and Human Service
    Inventor: The Gov. of the U.S of America as Represented by the Secretary of the Dept. of Health and Human Services
  • Publication number: 20130209392
    Abstract: The present invention provides cyclic dimers of alpha acids and polymers derived therefrom. Also provided are processes for preparing and methods of using the cyclic dimers and the polymers derived from the cyclic dimers.
    Type: Application
    Filed: February 8, 2013
    Publication date: August 15, 2013
    Applicant: NOVUS INTERNATIONAL INC.
    Inventor: Novus International Inc.
  • Patent number: 8506997
    Abstract: The present invention refers to a new compound containing Silymarin with Carbopol for the treatment of Diabetes Mellitus. This compound morphologically and structurally regenerates the damage that occurs in the pancreatic tissue in Diabetes Mellitus, and regenerates the insulin-producing pancreatic cells (? cells). It therefore regulates the serum levels of this hormone. Furthermore, it restores and maintains the normal concentrations of the blood glucose.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: August 13, 2013
    Assignee: Universidad Autonoma Metropolitana
    Inventor: Claudia Angelica Soto Peredo
  • Publication number: 20130196976
    Abstract: Disclosed are a composition for reducing beta amyloid-induced neurotoxicity by inhibiting ?-secretase activity, comprising a dibenzofuran derivative, and a method for preparing the same. Further disclosed is that the combination of the dibenzofuran derivative with a ?-secretase inhibitor or an anti-inflammatory agent shows higher activity with respect to reducing beta amyloid-induced neurotoxicity.
    Type: Application
    Filed: March 12, 2013
    Publication date: August 1, 2013
    Applicant: PHLORONOL, INC.
    Inventor: PHLORONOL, INC.
  • Publication number: 20130196973
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Publication number: 20130197030
    Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.
    Type: Application
    Filed: March 8, 2013
    Publication date: August 1, 2013
    Applicant: Evolva Sa
    Inventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
  • Patent number: 8497298
    Abstract: The present invention is a method for the glucose related disorders and lipid related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) or formula (II) as herein defined. The present invention is further directed to methods of treatment comprising co-therapy with an anti-diabetic agent, and anti-lipid agent and/or an anti-obesity agent.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: July 30, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Virginia L. Smith-Swintosky, Allen B. Reitz
  • Patent number: 8492372
    Abstract: The present invention relates to novel 1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: July 23, 2013
    Assignee: Integrated Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Peder Svensson, Mikael Andersson
  • Publication number: 20130184222
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Patent number: 8486994
    Abstract: The present invention relates to prodrugs of compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.
    Type: Grant
    Filed: January 18, 2008
    Date of Patent: July 16, 2013
    Assignee: Evolva SA
    Inventors: Peteris Alberts, Alexandra Santana Sorensen
  • Publication number: 20130178516
    Abstract: The present invention relates to plant extracts, specifically, the extracts of Chinese medicine Chenopodium ambrosioides L. and the composition comprising thereof. The extracts of Chinese medicine Chenopodium ambrosioides L. are prepared by conventional methods for the extraction of volatile oil, and can be used to treat Helicobacter Pylori -induced diseases of digestive system, such as gastritis, gastric ulcer, etc., with easy availability of raw materials, simple preparations, prominent effects, and less side-effect.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 11, 2013
    Applicant: Tasly Pharmaceutical Group Co., Ltd.
    Inventors: Feng Wei, Zhengliang Ye, Jun Gao, Chongnian Luo, Dekun Li, Jianming Chen, Yonghong Zhu, Junfeng Xiong, Xiaoli Zheng, Guangming Zhang, Ying Zhao
  • Patent number: 8455497
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: June 4, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • Publication number: 20130102641
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Application
    Filed: December 13, 2012
    Publication date: April 25, 2013
    Applicant: XENOPORT, INC.
    Inventor: XENOPORT, INC.
  • Patent number: 8426459
    Abstract: The invention relates to a composition containing flavanolignans, e.g., isolated from Silybum marianum, and basic amino acids and, optionally, other auxiliary substances, in the form of mixture, and to the method of preparation of these compositions by mixing the components and their homogenization. The invention is applicable particularly in the pharmaceutical industry, cosmetics, food industry, breweries, distilleries, and in the industry of beverage production.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: April 23, 2013
    Assignee: Agra Group, A.S.
    Inventors: Milan Stuchlik, Jiri Kopenec
  • Publication number: 20130085176
    Abstract: The present invention is directed to a process for the preparation of sulfamide derivatives.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 4, 2013
    Applicant: JOHNSON & JOHNSON
    Inventor: JOHNSON & JOHNSON
  • Publication number: 20130085175
    Abstract: The present invention is directed to an improved process for the preparation of sulfamide derivatives.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 4, 2013
    Applicant: JOHNSON & JOHNSON
    Inventor: Johnson & Johnson
  • Publication number: 20130084330
    Abstract: Disclosed is a composition for treating arthritis containing a dibenzo-p-dioxin derivative as an active ingredient. This dibenzo-p-dioxin derivative is very effective in inhibiting NF-kB and AP-1 activity, alleviates the symptoms of degenerative arthritis and rheumatoid arthritis without irritating the skin or causing side effects, and can continue to exhibit improvement effects for a considerable period of time after discontinuation of treatment. Additionally, when the dibenzo-p-dioxin derivative is contained in liposomes, the composition of the invention exhibits much greater effects on treating arthritis by absorption through skin, and thus is useful for the treatment of degenerative arthritis and rheumatoid arthritis.
    Type: Application
    Filed: November 29, 2012
    Publication date: April 4, 2013
    Applicant: LIVECHEM, INC.
    Inventor: Livechem, Inc.
  • Patent number: 8409574
    Abstract: Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: April 2, 2013
    Inventors: James D. McChesney, Gilles Tapolsky, David E. Emerson, John Marshall, Tauseef Ahmed, Allen Cohn, Michael Kurman, Manuel Modiano
  • Publication number: 20130078272
    Abstract: Antifungal compounds, an antifungal compound extracted from Epicoccum purpurascens, also known as Epicoccum nigrum, methods of producing the antifungal compounds, isolates and compositions comprising the antifungal compounds, and methods of using the antifungal compounds.
    Type: Application
    Filed: December 9, 2010
    Publication date: March 28, 2013
    Applicant: Auckland UniServices Limited
    Inventor: Silas Granato Villas-Boas
  • Publication number: 20130079293
    Abstract: Isolated compounds from adelostemma gracillimum refined fractions and compositions containing the compounds are provided by the present invention. Adelostemma gracillimum refined fractions and the extraction process thereof are also provided by the present invention. The uses of the compounds and the adelostemma gracillimum refined fractions for inhibiting the activities of NMDA receptor or amyloid-beta peptide, for improving memory, and for treating neurodegenerative diseases, neuropathological conditions or epilepsy are further provided by the present invention.
    Type: Application
    Filed: March 18, 2011
    Publication date: March 28, 2013
    Applicant: BIOTECHNOLOGY RESEARCH CORPORATION LIMITED
    Inventors: Nancy Yuk-yu Ip, Fanny Chui-Fun Ip, Shengjun Guo
  • Publication number: 20130071328
    Abstract: This invention discloses a series of novel propynoic acid carbamoyl methyl-amides (PACMAs), methods for synthesizing the PACMAs and pharmaceutical compositions containing the PACMAs. These novel compounds and compositions show cytotoxicity in cancer cells and are useful as lead compounds for anti-cancer drugs or pharmaceutical agents. This invention also discloses treatment methods that uses the PACMAs and pharmaceutical compositions as well as methods for promoting the release and nuclear localization of the transcription factor Nrf2.
    Type: Application
    Filed: March 22, 2012
    Publication date: March 21, 2013
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Nouri NEAMATI, Nicos A. PETASIS, Roppei YAMADA
  • Publication number: 20130072520
    Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)— or ?N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(?O)—, —O—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nit
    Type: Application
    Filed: November 28, 2011
    Publication date: March 21, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: David BROWN, Ian COLLINS, Lloyd CZAPLEWSKI, David HAYDON
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Publication number: 20130053385
    Abstract: The use of a compound of formula I wherein the substituents are as defined in claim 1, or compositions containing them in controlling insects, acarines, nematodes or molluscs.
    Type: Application
    Filed: December 7, 2010
    Publication date: February 28, 2013
    Applicants: SYNGENTA LIMITED, SYNGENTA CROP PROTECTION LLC
    Inventors: Stephane Andre Marie Jeanmart, Russell Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Michel Muehlebach
  • Publication number: 20130053392
    Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
    Type: Application
    Filed: February 14, 2011
    Publication date: February 28, 2013
    Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
  • Patent number: 8377422
    Abstract: Compounds of formula (I) wherein R1-R5, n and m have the same meaning as given in the description, having cooling properties are disclosed. Furthermore a process of their production and consumer products comprising them are disclosed.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: February 19, 2013
    Assignee: Givaudan S.A.
    Inventors: Stefan Michael Furrer, Thomas Scott McCluskey
  • Publication number: 20130039854
    Abstract: A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: February 14, 2013
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Jean C. SHIH, Leland CHUNG, Haiyen E. ZHAU, Boyang Jason WU, Bogdan Z. OLENYUK
  • Patent number: 8367358
    Abstract: The present disclosure discloses a reagent for differentiating and counting leukocytes which includes: (1) cationic cyanine compounds selected from those having the following general formulae I and II; (2) cationic surfactants selected from those having the following general formulae III, IV and/or V; (3) at least one nonionic surfactant; and (4) optionally, at least one anionic compound selected from those having one or more carboxyl or sulphonyl groups; and optionally includes alcohol compounds. Also disclosed is a kit comprising the reagent for differentiating and counting leukocytes. Further disclosed is a method for differentiating and counting leukocytes using the reagent and kit. Use of the reagent, kit and method disclosed enables the identification of leukocytes in blood samples into five subtypes in a very short time, or at least achieves the differentiation and counting of four leukocyte groupings. Moreover, immature and abnormal cells can be identified.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: February 5, 2013
    Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.
    Inventors: Lei Ting, Xu Bing, Kuang Yuji, Zhang Baohua, Shao Jianhui
  • Publication number: 20130030008
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 1, 2012
    Publication date: January 31, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Publication number: 20130022668
    Abstract: The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
    Type: Application
    Filed: September 15, 2012
    Publication date: January 24, 2013
    Applicant: TAPESTRY PHARMACEUTICALS, INC.
    Inventors: James D. McChesney, Gilles TAPOLSKY, David L. EMERSON, John MARSHALL, Tauseef AHMED, Allen COHN, Michael KURMAN, Manuel MODIANO
  • Publication number: 20120321552
    Abstract: Screening and diagnostic reagents, kits and methods for primary and/or metastatic stomach or esophageal cancer are disclosed. Compositions for and methods of imaging and treating primary and/or metastatic stomach or esophageal cancer are disclosed. Vaccines compositions and methods of for treating and preventing primary and/or metastatic stomach or esophageal cancer are disclosed.
    Type: Application
    Filed: October 20, 2011
    Publication date: December 20, 2012
    Applicant: THOMAS JEFFERSON UNIVERSITY
    Inventors: Scott A. Waldman, Jason Park, Stephanie Schulz
  • Patent number: 8334109
    Abstract: A reagent for blood analysis includes: (1) a compound having the general formula I; and (2) at least one surfactant selected from cationic surfactants and nonionic surfactants. In another aspect a method for differentiating and counting blood cells is provided, the method includes the following steps: (a) mixing a blood sample with the reagent for blood analysis according to the present disclosure to form a cell suspension; (b) detecting scattered light signals and fluorescence signals of cells in the blood sample; and (c) differentiating and counting the cells in the blood sample based upon the scattered light signals and fluorescence signals. The reagent for blood analysis may be effective for identifying and counting erythroblasts and/or basophils in a blood sample to be detected, and meanwhile counting leukocytes therein.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: December 18, 2012
    Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.
    Inventors: Zhang Baohua, Xu Bing, Kuang Yuji, Lei Ting, Shao Jianhui, Bao Dequan
  • Publication number: 20120316066
    Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.
    Type: Application
    Filed: December 2, 2011
    Publication date: December 13, 2012
    Applicant: Intrexon Corporation
    Inventors: Robert Eugene HORMANN, Bing Li
  • Publication number: 20120316230
    Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.
    Type: Application
    Filed: February 15, 2012
    Publication date: December 13, 2012
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Publication number: 20120302523
    Abstract: A method of making an endoperoxide from a diene and oxygen in the presence of a photocatalyst having an excited state lifetime of at least 100 nanoseconds, the endoperoxide being represented by the formula: where R1 is an aryl substituted with at least one group selected from the group consisting of alkoxy, hydroxyl, halogen, carbamate, sulfonamide, silyloxy, amide, and combinations thereof or a substituted or unsubstituted heteroaryl, R2 is hydrogen, alkyl, alkynyl, or aryl, R3 is hydrogen, alkyl, alkynyl, or aryl, R4 is alkynyl or aryl, R5 is hydrogen or a substituent, R6 is hydrogen or a substituent, and A1, A2, and A3 are the same or different atoms and form a divalent group that combines with the two carbon atoms of the endoperoxide ring to form a saturated or unsaturated, substituted or unsubstituted ring system of a size of from five to six atoms.
    Type: Application
    Filed: May 27, 2011
    Publication date: November 29, 2012
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Tehshik P. Yoon, Jonathan D. Parrish, Michael A. Ischay
  • Patent number: 8318772
    Abstract: The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R1, R2 and n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: November 27, 2012
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Bohua Zhong, Youzhi Zhang, Yanping Zhang, Rui Xue, Xinhua He, Yunfeng Li, Hongxia Chen, Nan Zhao, Meiying Li
  • Publication number: 20120295874
    Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.
    Type: Application
    Filed: October 7, 2010
    Publication date: November 22, 2012
    Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATION
    Inventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold