The Other Ring Nitrogen Has A Substituent Which Includes Chalcogen Single Bonded To Acyclic Carbon Patents (Class 544/394)
  • Patent number: 10927084
    Abstract: To provide a friction-reducing agent containing no sulfur nor phosphorus and being excellent in friction-reducing properties, and a lubricating oil composition using it. An alkanolamine represented by the following formula is used as a friction-reducing agent: wherein A1 and A2 are each independently a hydroxy group or a hydrogen atom, provided that A1 and A2 are not hydrogen atoms at the same time, R1 is a hydrocarbon group having at most 30 carbon atoms, R2 to R6 are each independently a hydrogen atom or a hydrocarbon group having at most 30 carbon atoms, and m and n are each independently an integer of from 0 to 10.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: February 23, 2021
    Assignee: TOSOH CORPORATION
    Inventors: Arimitsu Takemoto, Hiroshi Awano, Hisao Eguchi, Manabu Yanase
  • Patent number: 8987441
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: March 24, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
  • Publication number: 20140329746
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Patent number: 8835419
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 16, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. MacMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20140235650
    Abstract: The invention relates to a compound of formula (I), where R1, R2, R7, m, n, and L1 are as defined in claim 1, and to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.
    Type: Application
    Filed: June 22, 2012
    Publication date: August 21, 2014
    Applicant: Metabolys
    Inventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
  • Publication number: 20140228568
    Abstract: Provided are biphenyl derivatives exhibiting activity towards central nervous system diseases by acting on the 5-HT7 receptor, pharmaceutically acceptable salts thereof, a method for preparing the compounds and pharmaceutical compositions including the compounds as an active ingredient.
    Type: Application
    Filed: February 8, 2013
    Publication date: August 14, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyunah CHOO, Young-Jae KIm, Jeeyeon KIM, Mi Young YEOM
  • Patent number: 8778948
    Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: July 15, 2014
    Assignee: NHWA Pharma, Corporation
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
  • Patent number: 8778949
    Abstract: The invention relates to compounds of formula I: where a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: July 15, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Lori Jean Patterson
  • Patent number: 8765950
    Abstract: The present disclosure provides isotopically substituted compounds of the formula (II): wherein T, U, V, W, X, Y, Z, R0, R3, R4, R5 and R6 are as defined in the detailed description. The method for detection and quantification using the same is also disclosed.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: July 1, 2014
    Assignee: Purdue Research Foundation
    Inventors: Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
  • Publication number: 20140155409
    Abstract: The invention relates to a compound of formula (I), where R1, R2, R3, m, n, and L1 are as defined in claim 1, to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.
    Type: Application
    Filed: June 22, 2012
    Publication date: June 5, 2014
    Applicant: Metabolys
    Inventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
  • Publication number: 20140086834
    Abstract: The invention relates to a new class of compounds able to inhibit with high affinity and selectivity the 5-HT7 receptor. The invention also relates to the utilization of such compounds as medicaments useful in the treatment and prevention of 5-HT7 receptor relating disorders of the central nervous system. The invention also relates to the isotopically labeled compounds for use in vivo diagnosis or imaging of a 5-HT7 condition.
    Type: Application
    Filed: May 24, 2011
    Publication date: March 27, 2014
    Applicant: UNIVERSITA' DEGLI STUDI DI BARI ''ALDO MORO''
    Inventors: Marcello Leopoldo, Enza Lacivita, Nicola Colabufo, Paola De Giorgio, Francesco Berardi, Roberto Perrone
  • Patent number: 8674089
    Abstract: The present invention provides a Michael addition reaction product between a specified compound having a group which functions as a Michael donor and a monomer or polymer having a group which functions as a Michael acceptor, a photoinitiator containing the Michael addition reaction product, and an active energy ray-curable composition containing the photoinitiator. The compound having a group functioning as a Michael donor used in the present invention is a phenyl ketone derivative and is characterized by having an amino group or a mercapto group as the group functioning as a Michael donor.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: March 18, 2014
    Assignee: DIC Corporation
    Inventors: Kutzner Fabian, Gaudl Kai-uwe, Yoshinobu Sakurai, Tatsushi Okuda
  • Publication number: 20140030189
    Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
    Type: Application
    Filed: June 12, 2013
    Publication date: January 30, 2014
    Inventors: Ajay Purohit, Thomas D. Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
  • Publication number: 20130296455
    Abstract: Disclosed are a dye that is excellent in solubility and heat-resistance, and a novel compound that is suitable for the dye, and specifically provides a yellow dye having a maximum absorption wavelength in the region of 420 to 470 nm. Also disclosed are a colored (alkali-developable) photosensitive composition and an optical filter using the dye, and specifically provides a color filter that does not decrease luminance and thus is preferable for an image display device such as a liquid crystal display panel. Specifically, disclosed are a novel compound represented by the following general formula (1), a dye using the compound, and a colored (alkali-developable) photosensitive composition and a color filter. The content of the above-mentioned general formula (1) is as described in the description.
    Type: Application
    Filed: December 27, 2011
    Publication date: November 7, 2013
    Applicant: ADEKA CORPORATION
    Inventors: Yosuke Maeda, Masaaki Shimizu, Koichi Shigeno
  • Publication number: 20130172315
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: July 4, 2013
    Applicant: ChemoCentryx, Inc.
    Inventor: ChemoCentryx, Inc.
  • Publication number: 20130064770
    Abstract: The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.
    Type: Application
    Filed: May 26, 2011
    Publication date: March 14, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Ian Martin Newington, Duncan George Wynn, Robert James Domett Nairne, Benedicte Guilbert, Subrata Mandal, Jinto Jose, Sunderaraman Varadarajan, Chitralekha Rangaswamy, Helen Betts, Rebecca Davis
  • Patent number: 8252796
    Abstract: The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: August 28, 2012
    Assignees: CSPC Zhonggi Pharmaceutical Technology (Shijiazhuang) Co. Ltd., Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng
  • Publication number: 20120190846
    Abstract: The present invention provides a Michael addition reaction product between a specified compound having a group which functions as a Michael donor and a monomer or polymer having a group which functions as a Michael acceptor, a photoinitiator containing the Michael addition reaction product, and an active energy ray-curable composition containing the photoinitiator. The compound having a group functioning as a Michael donor used in the present invention is a phenyl ketone derivative and is characterized by having an amino group or a mercapto group as the group functioning as a Michael donor.
    Type: Application
    Filed: June 28, 2010
    Publication date: July 26, 2012
    Applicant: DIC CORPORATION.
    Inventors: Kutzner Fabian, Gaudl Kai-uwe, Yoshinobu Sakurai, Tatsushi Okuda
  • Publication number: 20120107830
    Abstract: The present disclosure provides isotopically substituted compounds of the formula (II): wherein T, U, V, W, X, Y, Z, R0, R3, R4, R5 and R6 are as defined in the detailed description. The method for detection and quantification using the same is also disclosed.
    Type: Application
    Filed: January 9, 2012
    Publication date: May 3, 2012
    Inventors: Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
  • Patent number: 8153637
    Abstract: The present invention relates to phenyl-alkyl piperazines of formula (I): in which A, R1, R2 and R3 are as defined herein, having TNF-modulating activity. The invention also relates to the preparation thereof, pharmaceutical compositions thereof, and to the therapeutic use thereof.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: April 10, 2012
    Assignee: Sanofi
    Inventors: Marco Baroni, Olaf Ritzeler, Marco Zanchet
  • Publication number: 20110318388
    Abstract: The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.
    Type: Application
    Filed: October 19, 2009
    Publication date: December 29, 2011
    Applicant: Akaal Pharma Pty Ltd
    Inventors: Gurmit S. Gill, Damian W. Grobelny
  • Publication number: 20110294822
    Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.
    Type: Application
    Filed: December 22, 2009
    Publication date: December 1, 2011
    Applicant: NHWA PHARMA. CORPORATION
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
  • Publication number: 20110183996
    Abstract: The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art.
    Type: Application
    Filed: September 29, 2009
    Publication date: July 28, 2011
    Applicant: Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng
  • Patent number: 7985752
    Abstract: The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: July 26, 2011
    Assignee: SK Holdings Co., Ltd.
    Inventors: Yonggil Kim, Nahmryune Cho, Yunhee Kim, Joon Heo, Seonmin Dong, Mi Kyung Ji, Man-Young Cha, Kiho Lee
  • Publication number: 20110124657
    Abstract: The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor; to a method for identifying them as 5-HT7 ligands, especially as agonists, by using a pharmacophore and a descriptor's profile filter; to pharmaceutical compositions comprising them; and to their use in therapy, in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.
    Type: Application
    Filed: July 30, 2009
    Publication date: May 26, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Rosalia Pascual-Ramon, H. Helmut Buschmann
  • Publication number: 20100317854
    Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
    Type: Application
    Filed: August 23, 2010
    Publication date: December 16, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
  • Publication number: 20100286164
    Abstract: Aspects of the invention relate to substituted aryl propylamino-oxy-analogs and uses thereof. Aspects of the invention relate to compositions that are inhibitors of ?-secretase and uses thereof for treating subjects having, or at risk of developing, Alzheimer's disease.
    Type: Application
    Filed: October 10, 2008
    Publication date: November 11, 2010
    Applicant: The Brigham and Women's Hospital, Inc
    Inventors: Corinne Elizabeth Augelli-Szafran, Michael S. Wolfe, Han-Xun Wei
  • Patent number: 7829713
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: November 9, 2010
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Terrence P. Keenan, Alan P. Kaplan
  • Publication number: 20100279997
    Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
    Type: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20100227855
    Abstract: Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.
    Type: Application
    Filed: March 16, 2010
    Publication date: September 9, 2010
    Applicant: ENDORECHERCHE, INC.
    Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, René Maltais
  • Publication number: 20100221182
    Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
    Type: Application
    Filed: December 21, 2007
    Publication date: September 2, 2010
    Inventors: Ajay Purohit, Thomas D, Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
  • Patent number: 7750012
    Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: July 6, 2010
    Assignee: deCODE genetics ehf
    Inventors: Vincent Sandanayaka, Jasbir Singh, Li-Ming Zhou, Mark E. Gurney
  • Publication number: 20100056545
    Abstract: Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. wherein, X, R1, and R3 are as defined herein.
    Type: Application
    Filed: April 23, 2009
    Publication date: March 4, 2010
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Kye Jung SHIN, Hyung Kook LEE, Eun Joo ROH, Dong Jin KIM, Kyung Il CHOI, Hyewhon RHIM, Hye Jin CHUNG, Seon Hee SEO
  • Patent number: 7671055
    Abstract: Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: March 2, 2010
    Assignee: FMC Corporation
    Inventors: Edward J. Barron, Y. Larry Zhang, Frank J. Zawacki, John W. Lyga, George Theodoridis
  • Patent number: 7642262
    Abstract: A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: January 5, 2010
    Assignee: Asubio Pharma Co., Ltd.
    Inventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura
  • Publication number: 20090253710
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3?R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
    Type: Application
    Filed: June 30, 2008
    Publication date: October 8, 2009
    Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic
  • Publication number: 20090219526
    Abstract: The present disclosure provides isotopically substituted compounds of the formula (I): wherein T, U, V, W, X, Y, Z, R0, R3, R4, R5 and R6 are as defined in the detailed description. The method for detection and quantification using the same is also disclosed.
    Type: Application
    Filed: December 29, 2008
    Publication date: September 3, 2009
    Inventors: Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
  • Patent number: 7488731
    Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: February 10, 2009
    Assignee: Epix Delaware, Inc.
    Inventors: Dale S. Dhanoa, Dongli Chen, Oren Becker, Silvia Noiman, Srinivasa R. Cheruku, Yael Marantz, Anurag Sharadendu, Sharon Shacham, Alexander Heifetz, Pradyumna Mohanty, Boaz Inbal, Merav Fichman, Raphael Nudelman, Shay Bar-Haim
  • Patent number: 7417043
    Abstract: A 3-substituted 4-(phenyl-N-alkyl)-piperazine compound of the following formula: wherein R1 is selected from the group consisting of OSO2CF3, OSO2CH3, SO2R3, COCF3, COCH3 and COCH2CH3, wherein R3 is as defined hereafter; R2 is selected from the group consisting of C1-C4 alkyls, allyl, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl and 4,4,4-trifluorobutyl; R3 is selected from the group consisting of C1-C3 alkyls, CF3, and N(CH3)2; with the proviso that when R1 is SO2R3 and R3 is a C1-C3 alkyl, then R2 is not CH2CH2OCH3; or a pharmaceutically acceptable salt thereof are provided. Also, pharmaceutical compositions comprising the above compound and methods wherein the above compound is used for the treatment of various disorders are provided.
    Type: Grant
    Filed: December 21, 2004
    Date of Patent: August 26, 2008
    Assignee: NeuroSearch Sweden AB
    Inventors: Clas Sonesson, Ingela Marianne Svan, legal representative, Anders Kristoffer Lilja, legal representative, Liselott Lilja Rönnqvist, legal representative, Jenny Maria Carlberg, legal representative, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
  • Patent number: 7390812
    Abstract: N,N?-disubstituted piperazine compounds, processes for the production thereof, and pharmaceutical preparations containing these compounds. The use of N,N?-disubstituted piperazine compounds for the production of pharmaceutical preparations and in related methods of treatment.
    Type: Grant
    Filed: June 14, 2004
    Date of Patent: June 24, 2008
    Assignee: Gruenenthal GmbH
    Inventors: Heinz Uragg, Corinne Maul, Helmut Buschmann, Bernd Sundermann, Hagen-Heinrich Hennies
  • Patent number: 7256289
    Abstract: A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders. The intermediate compounds of Formula II and IV as set forth herein are also included.
    Type: Grant
    Filed: June 7, 2005
    Date of Patent: August 14, 2007
    Assignee: Wyeth
    Inventors: Ivo Ladislav Jirkovsky, Joseph Zeldis, Gregg Brian Feigelson
  • Patent number: 7241765
    Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: July 10, 2007
    Assignee: Neurogen Corporation
    Inventors: Alan J. Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Rajagopal Bakthavatchalam, Yiping Shen, Cheryl K. Steenstra, Helen Yin, Robert W. DeSimone, Xiao-shu He
  • Patent number: 7226925
    Abstract: The invention relates to compounds of the general Formula (I): The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of Formula (I).
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: June 5, 2007
    Assignee: Biovitrum AB
    Inventors: Björn M. Nilsson, Erik Ringberg, Birger Sjöberg, Mattias Jönsson
  • Patent number: 7186277
    Abstract: In one embodiment, the disclosure relates to a composition for dyeing keratin fibres, for example, human keratin fibres such as the hair, comprising at least one para-phenylenediamine derivative substituted with a diazacyclohexane or diazacycloheptane ring, the nitrogen in position 4 of which is a quaternary ammonium. The present disclosure may make it possible, for example, to obtain at least one of chromatic, strong, relatively unselective, fast coloration of keratin fibres.
    Type: Grant
    Filed: March 24, 2004
    Date of Patent: March 6, 2007
    Assignee: L'Oreal SA
    Inventors: Alain Genet, Stéphane Sabelle
  • Patent number: 7153858
    Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
    Type: Grant
    Filed: January 30, 2004
    Date of Patent: December 26, 2006
    Assignee: Epix Delaware, Inc.
    Inventors: Dale S. Dhanoa, Dongli Chen, Oren Becker, Silvia Noiman, Srinivasa Rao Cheruku, Yael Marantz, Anurag Sharadendu, Sharon Shachem, Alexander Heifetz, Pradyumna Mohanty, Boaz Inbal, Merav Fichman, Raphael Nudelman, Shay Bar-Haim
  • Patent number: 7105521
    Abstract: The present invention provides isoeugenol derivative compounds having the moiety and having ?2-adrenergic/5-HT2A antagonist, 5-HT re-uptake inhibition, and anti-oxidant activities.
    Type: Grant
    Filed: June 30, 2003
    Date of Patent: September 12, 2006
    Assignee: Syn-Tech Chem & Pharm Co., Ltd.
    Inventor: Ing-Jun Chen
  • Patent number: 7090703
    Abstract: The disclosure relates to novel para-phenylenediamine derivatives containing a cyclic diaza group, substituted with a cationic radical, as well as to the dye compositions comprising them, and to the method of dyeing keratin fibers using these compositions. The present invention may make it possible to obtain a chromatic, strong, relatively unselective and fast coloration on keratin fibers.
    Type: Grant
    Filed: March 24, 2004
    Date of Patent: August 15, 2006
    Assignee: L'Oreal
    Inventors: Stéphane Sabelle, Alain Genet, Madeleine Leduc
  • Patent number: 7071197
    Abstract: N,N-Disubstituted diazocycloalkanes of the formula I (R1=halogen, R2=(C3–C8)-cycloalkyl, R3=(C1–C4)-alkoxy or (C1–C4)-haloalkoxy group, m is 1 or 2 and n is 1 or 2, have affinity for serotonergic receptors. These compounds and their enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor.
    Type: Grant
    Filed: June 16, 2003
    Date of Patent: July 4, 2006
    Assignee: Recordati S.A.
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
  • Patent number: 7067501
    Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: June 27, 2006
    Assignee: H. Lundbeck A/S
    Inventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
  • Patent number: 7019137
    Abstract: A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.
    Type: Grant
    Filed: March 10, 2003
    Date of Patent: March 28, 2006
    Assignee: Wyeth
    Inventors: Ivo Jirkovsky, Joseph Zeldis, Gregg Brian Feigelson