Plural Piperidine Rings Patents (Class 546/186)
  • Patent number: 9975864
    Abstract: The present disclosure provides crystalline piperidine sulfamoyl intermediates of formula 8 and 9. The present disclosure also relates to an improved process for the preparation of cobicistat using compounds of formulae 8 and 9.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: May 22, 2018
    Assignee: Mylan Laboratories Limited
    Inventors: Lakshmana Rao Vadali, Rameshbabu Konda, Ramesh Dandala
  • Patent number: 9409863
    Abstract: The present application relates to a process for preparing chloroamines which can be used as precursors for syntheses of fine chemicals and active ingredients from pharmaceuticals and/or agriculture, by reaction of secondary amines of the formula (II) with chlorine gas in the presence of an aqueous alkali metal or alkaline earth metal oxide base.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: August 9, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: Mark James Ford
  • Patent number: 8987303
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: March 24, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20140336285
    Abstract: The present invention relates to demulsifying and dehydrating formulations of heavy crude oil based block copolymers amine bifunctionalized with low polydispersities. These formulations can contain solvents whose boiling point is in the range from 35 to 200° C.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Gabriel Cendejas Santana, Eugenio Alejandro Flores Oropeza, Laura Veronica Castro Sotelo, Aristeo Estrada Buendia, Marcelo Lozada y Cassou, Flavio Salvador Vazquez Moreno
  • Publication number: 20140309114
    Abstract: Amine salts of certain herbicides that in free acid form include at least one carboxylic acid moiety are described. Herbicide salts comprising the cation of various imidazole, piperazine, piperidine, and morpholine compounds are provided. The herbicide amine salts described are suitable for formulation into herbicidal application mixtures and/or stable concentration compositions that exhibit acceptable volatility characteristics upon application.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventors: Junhua Zhang, Daniel R. Wright, William Abraham
  • Patent number: 8791136
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: July 29, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20140199601
    Abstract: The present invention aims to provide an additive for a non-aqueous electrolyte solution with excellent storage stability capable of forming a stable SEI on the surface of an electrode to improve cell performance such as a cycle performance, a discharge/charge capacity, and internal resistance, when the additive is used for electrical storage devices such as non-aqueous electrolyte solution secondary cells and electric double layer capacitors. The present invention also aims to provide a non-aqueous electrolyte solution containing the additive for a non-aqueous electrolyte solution and to provide an electrical storage device using the non-aqueous electrolyte solution.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 17, 2014
    Applicant: SUMITOMO SEIKA CHEMICALS CO., LTD.
    Inventors: Tomohiro Onozuka, Shohei Fujimoto, Koji Fujita
  • Publication number: 20140057877
    Abstract: This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan.
    Type: Application
    Filed: October 18, 2011
    Publication date: February 27, 2014
    Inventors: Michael A. Murphy, Mitchell R. Malachowski
  • Patent number: 8629163
    Abstract: Provided are tetrakis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: January 14, 2014
    Assignee: University of Kentucky Research Foundation
    Inventors: Peter A. Crooks, Linda P. Dwoskin, Zhenfa Zhang, Marharyta Pivavarchyk
  • Patent number: 8592588
    Abstract: A process is provided for the preparation of camptothecin derivatives, such as irinotecan, in a one-pot operation.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: November 26, 2013
    Assignee: Chatham Biotec, Limited
    Inventor: Ragina Naidu
  • Patent number: 8524665
    Abstract: In general, the present invention provides methods for treating disorders associated with the amygdala. The methods of treatment are based on the administration of a therapeutically effective amount of secretin to an individual suffering from a disorder associated with the amygdala, e.g., bipolar disorder or a substance use disorder.
    Type: Grant
    Filed: May 13, 2004
    Date of Patent: September 3, 2013
    Assignee: The McLean Hospital Corporation
    Inventors: Deborah A. Yurgelun-Todd, Perry F. Renshaw
  • Publication number: 20130126429
    Abstract: Methods for making sulfide scavenging compositions are provided. The compositions are secondary amine-formaldehyde adduct (SAFA) scavengers comprising less than about 40 wt % N-methyl secondary amines therein. The methods include reacting secondary amines with formaldehyde. Methods for removing sulfides from fluid streams are also provided. The methods include adding secondary amine-formaldehyde adduct (SAFA) scavengers to fluid streams. SAFA scavengers comprising less than about 40 wt % N-methyl secondary amines of the total weight of SAFA scavengers are also disclosed.
    Type: Application
    Filed: November 23, 2011
    Publication date: May 23, 2013
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: Ping Lue, Gregory Kaplan
  • Patent number: 8435978
    Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: May 7, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
  • Publication number: 20130053484
    Abstract: An intermediate of the formula (I) wherein the radicals R1 are independently of one another methyl, ethyl or n-propyl, is suitable for preparing a compound of the formula (A) wherein X is a group of the formula (A-I) or (A-II), Y is C11-C17alkyl, and Z is a direct bond, —(CH2)8— or —CH2—S—CH2—. The compounds of the formula (A) are useful for stabilizing an organic material against thermal, oxidative or light induced degradation.
    Type: Application
    Filed: March 2, 2011
    Publication date: February 28, 2013
    Applicant: BASF SE
    Inventors: Hans-Rudolf Meier, Kai-Uwe Schoning, Shrirang Bhikaji Hindalekar
  • Patent number: 8383660
    Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: February 26, 2013
    Assignee: Pfizer Inc.
    Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
  • Publication number: 20130043137
    Abstract: Provided is a copper plating technique that enables the filling of high aspect-ratio via-holes and through-holes in semiconductor substrates such as silicon substrates, organic material substrates or ceramic substrates. The disclosed technique involves a tertiary amine compound, which is obtained by reacting a heterocyclic compound with the epoxy group of a glycidyl ether group of a compound that has three or more glycidyl ether groups, and a quaternary amine compound thereof, as well as a copper plating additive, a copper plating bath, and a copper plating method employing the compounds.
    Type: Application
    Filed: April 30, 2010
    Publication date: February 21, 2013
    Applicant: JCU CORPORATION
    Inventors: Hiroki Yasuda, Ryoichi Kimizuka, Tatsuji Takasu, Takuro Sato, Hiroshi Ishizuka, Yasuhiro Ogo, Yuto Oyama, Yu Tonooka, Mikiko Kosaka, Aya Shimomura, Yumiko Shimizu
  • Patent number: 8377964
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
  • Patent number: 8362164
    Abstract: The embodiments of the invention relate to a multifunctional lithiated amine-containing compound comprising at least two molecules of lithiated amine in a molecule of the compound. In one embodiment, the compound has a formula where x is an integer of 1 or more, Q is (a) an element selected from the group consisting of O, S, N, P and Si or (b) an alkylene group having from 1 to 20 methylene groups, and R1 and R2 are the same or different and are selected from the group consisting of alkyls, cycloalkyls and aralkyls containing from 1 to 20 carbon atoms. In another embodiment, the compound comprises cyclic lithio amines and has a formula: where x is 1 or more, R3, R4 and R5 are the same or different and represent alkylene groups containing from 3 to 20 carbon atoms.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: January 29, 2013
    Assignee: Bridgestone Corporation
    Inventor: Yan Yan-Yong
  • Patent number: 8349923
    Abstract: The present invention relates to a novel method of flame retarding a polymeric substrate by adding a small but efficient amount of a synergistic mixture of at least one sterically hindered N-alkoxyamine (NOR), at least a metal salt of hypophosphorous (phosphinic) acid and at least one organo-halogen flame retardant. A further aspect of the invention is the flame retardant composition itself and together with a polymer. The present invention also relates to polymeric articles (e.g. moldings, films, fibers, etc.) that are stabilized against light, heat and oxygen and made flame retardant by incorporation of at least one sterically hindered N-alkoxy amine, at least a metal salt of hypophosphorous acid (phosphinic acid) and at least one organo-halogen flame retardant.
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: January 8, 2013
    Assignee: BASF SE
    Inventor: Michael Roth
  • Patent number: 8324248
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar1, Ar2, R1, R2, R3, R4, R5, R6, m, n, o, p, s, t, and u are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: December 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: 8304431
    Abstract: The present invention relates to the use of compounds and compositions of compounds having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for the treatment of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability-hypersensitivity-hyperaesthesia-dissociative phenomena-etc). The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: November 6, 2012
    Assignee: PharmaNeuroBoost N.V.
    Inventor: Erik Buntinx
  • Patent number: 8217170
    Abstract: The instant invention discloses a process for the preparation of compounds of the formula (I), wherein the general symbols are as defined in claim 1, which process comprises reacting a sterically hindered amine of the formula (II), wherein the general symbols are as defined in claim 1, with a compound of the formula (III) wherein the general symbols are as defined in claim 1, in the presence of a catalyst. The compounds of the formula (I) are useful as stabilizers for protecting organic materials, in particular synthetic polymers, reprographic materials or coating materials against oxidative, thermal or light-induced degradation.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: July 10, 2012
    Assignee: BASF SE
    Inventor: Massimiliano Sala
  • Patent number: 8158827
    Abstract: Disclosed are cationic lipid compounds and compositions of lipid aggregates for delivery of macromolecules and other compounds into cells. The compounds can be used alone or in combination with other compounds to prepare liposomes and other lipid aggregates suitable for transfection or delivery of compounds to target cells, either in vitro or in vivo. The compounds are preferably polycationic and preferably form highly stable complexes with various anionic macromolecules, particularly polyanions such as nucleic acids. These compounds have the property, when dispersed in water, of forming lipid aggregates which associate strongly, via their cationic portion, with polyanions. Also disclosed are intermediates for preparing the compound and compositions of the invention and methods of using the compounds to introduce other compounds into cells.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: April 17, 2012
    Assignee: Life Technologies Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Publication number: 20120029021
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Application
    Filed: January 17, 2011
    Publication date: February 2, 2012
    Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITY
    Inventors: Yong Ba, Errol V. Mathias
  • Publication number: 20110295000
    Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
    Type: Application
    Filed: August 8, 2011
    Publication date: December 1, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Guenther HUCHLER, Werner RALL, Uwe REIS
  • Publication number: 20110288251
    Abstract: The invention relates to novel O-dialkylamino-isoureas and polymerizable compositions comprising these O-dialkylamino-isoureas of compounds of the general formula (I). The invention further relates to the use of O-dialkylamino-isoureas as polymerization initiators, especially to prepare coatings or for controlled degradation of polyolefins.
    Type: Application
    Filed: December 28, 2009
    Publication date: November 24, 2011
    Applicant: BASF SE
    Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Antoine Carroy, Marc Faller
  • Patent number: 8049042
    Abstract: To provide a resist polymer comprising, as a structural unit, an acid-decomposable unit having a structure represented by formula (1) or (2) which exhibits a small line edge roughness and produces little defects in DUV excimer laser lithography or the like.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: November 1, 2011
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Hikaru Momose, Atsushi Ootake, Tadashi Nakamura, Akifumi Ueda
  • Patent number: 8013162
    Abstract: Sterically hindered hydroxy substituted alkoxyamine stabilizer compounds are made water compatible via certain backbones with affinity towards water. The sterically hindered amines are for example of formulae (5)-(7) These compounds are particularly effective in stabilizing aqueous polymer systems against the deleterious effects of oxidative, thermal and actinic radiation. The compounds are effective for example in stabilizing water borne coatings, aqueous inks, aqueous ink jet media and photocured aqueous systems.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: September 6, 2011
    Assignee: Ciba Corporation
    Inventors: Mervin G. Wood, Robert Detlefsen, James Galbo, Wanda Martin, Paul Kondracki, Michael P. DiFazio, Joseph E. Babiarz
  • Publication number: 20110144067
    Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 16, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Patent number: 7951821
    Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.
    Type: Grant
    Filed: March 1, 2007
    Date of Patent: May 31, 2011
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Benoit Marabout, Pierre Roger, Mireille Sevrin
  • Patent number: 7915293
    Abstract: This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical compositions comprising the compounds described in the invention for the treatment of conditions that require inhibition of ubiquitin ligases. Furthermore, the invention provides for methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound according to the invention.
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: March 29, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Usha V. Ramesh, Gary Charles Look, Rajinder Singh, Sarkiz D. Issakani
  • Patent number: 7902181
    Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: March 8, 2011
    Assignee: AstraZeneca AB
    Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
  • Patent number: 7858795
    Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 areas defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: December 28, 2010
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Trevor Mischki, Viengkham Malathong
  • Patent number: 7858789
    Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: December 28, 2010
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Christophe Thurieau, Jérôme Gonzalez, Christophe Moinet
  • Patent number: 7834182
    Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia, repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's diseas
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: November 16, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani
  • Patent number: 7816532
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: October 19, 2010
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
  • Publication number: 20100256114
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: June 17, 2010
    Publication date: October 7, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
  • Publication number: 20100249386
    Abstract: The present invention relates to the field of organic chemistry and in particular to organic free radicals used as polarizing agents in the technique of Dynamic Nuclear Polarization (DNP), which involves transferring the polarization of electron spins to the nuclei of a compound whose Nuclear Magnetic Resonance (NMR) is being observed. It concerns dinitroxide-type biradical polarizing agents characterized by a rigid linkage between the nitroxide units that enables optimal orientation and distance to be maintained between the aminoxyl groups of said nitroxide units. This particular structure enables, at low temperatures and high fields, optimal transfer of polarization and optimal enhancement of NMR/MAS signals of the polarized nuclei of the compound studied.
    Type: Application
    Filed: May 29, 2009
    Publication date: September 30, 2010
    Applicants: UNIVERSITE DE PROVENCE, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Olivier OUARI, Hakim KAROUI, Francois Le MOIGNE, Paul TORDO, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
  • Patent number: 7790897
    Abstract: The invention describes novel compound of the formula I, wherein the general symbols are as defined in claim 1, as stabilizers for protecting organic materials, in particular synthetic polymers, against oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: September 7, 2010
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Hans-Rudolf Meier, Gerrit Knobloch
  • Publication number: 20100197693
    Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: January 14, 2010
    Publication date: August 5, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
  • Patent number: 7759363
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: July 20, 2010
    Assignee: Theravance, Inc.
    Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
  • Publication number: 20100105686
    Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: October 27, 2007
    Publication date: April 29, 2010
    Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
  • Publication number: 20090326176
    Abstract: The embodiments of the invention relate to a multifunctional lithiated amine-containing compound comprising at least two molecules of lithiated amine in a molecule of the compound. In one embodiment, the compound has a formula where x is an integer of 1 or more, Q is (a) an element selected from the group consisting of O, S, N, P and Si or (b) an alkylene group having from 1 to 20 methylene groups, and R1 and R2 are the same or different and are selected from the group consisting of alkyls, cycloalkyls and aralkyls containing from 1 to 20 carbon atoms. In another embodiment, the compound comprises cyclic lithio amines and has a formula: where x is 1 or more, R3, R4 and R5 are the same or different and represent alkylene groups containing from 3 to 20 carbon atoms.
    Type: Application
    Filed: December 29, 2008
    Publication date: December 31, 2009
    Inventor: Yuan-Yong Yan
  • Publication number: 20090302842
    Abstract: The present invention provides methods for performing dynamic nuclear polarization using biradicals with a structure of formula (I) as described herein. In general, the methods involve (a) providing a frozen sample in a magnetic field, wherein the frozen sample includes a biradical of formula (I) and an analyte with at least one spin half nucleus; (b) polarizing the at least one spin half nucleus of the analyte by irradiating the frozen sample with radiation having a frequency that excites electron spin transitions in the biradical; (c) optionally melting the sample to produce a molten sample; and (d) detecting nuclear spin transitions in the at least one spin half nucleus of the analyte in the frozen or molten sample. The present invention also provides biradicals with a structure of formula (I) with the proviso that Q1 and Q2 are different when X1 and X2 are —O—. The present invention also provides methods for making biradicals with a structure of formula (IA) as described herein.
    Type: Application
    Filed: May 10, 2007
    Publication date: December 10, 2009
    Applicant: Massachusetts Institute of Tecnology
    Inventors: Robert G. Griffin, Kan-Nian Hu, Timothy M. Swager, Changsik Song, Eric Dane
  • Publication number: 20090275556
    Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.
    Type: Application
    Filed: August 27, 2008
    Publication date: November 5, 2009
    Inventors: Mingshi Dai, Bing Guan, Roert A. Bennett, Douglas F. Burdi, Shomir Ghosh, Gang Li, Charles Minor, Tracy J. Jenkins
  • Patent number: 7601872
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: October 13, 2009
    Assignee: Life Technologies Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Publication number: 20090202725
    Abstract: Sterically hindered hydroxy substituted alkoxyamine stabilizer compounds are made water compatible via certain backbones with affinity towards water. The sterically hindered amines are for example of formulae (5)-(7) These compounds are particularly effective in stabilizing aqueous polymer systems against the deleterious effects of oxidative, thermal and actinic radiation. The compounds are effective for example in stabilizing water borne coatings, aqueous inks, aqueous ink jet media and photocured aqueous systems.
    Type: Application
    Filed: April 9, 2009
    Publication date: August 13, 2009
    Inventors: Mervin G. Wood, Robert Detlefsen, James Galbo, Wanda Martin, Paul Kondracki, Michael P. DiFazio, Joseph E. Babiarz
  • Patent number: 7572918
    Abstract: Processes and intermediates for preparing substituted 4-amino-1-(pyridylmethyl)-piperidine and related compounds in high yield and high purity are described. The substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds prepared by the described processes are useful as muscarinic receptor antagonists.
    Type: Grant
    Filed: October 27, 2005
    Date of Patent: August 11, 2009
    Assignee: Theravance, Inc.
    Inventors: Matthew J Peterson, Junning Lee, Richard J Lee, Weijiang Zhang
  • Patent number: 7569586
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4,R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: August 4, 2009
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, Yu-Hua Ji
  • Patent number: 7547693
    Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypersomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder, and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's dis
    Type: Grant
    Filed: September 21, 2004
    Date of Patent: June 16, 2009
    Assignee: Banyu Pharmaceutical Co. Ltd.
    Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani