The Other Ring Nitrogen Has A Substituent Which Includes Chalcogen Single Bonded To Acyclic Carbon Patents (Class 544/394)
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Patent number: 10927084Abstract: 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: GrantFiled: January 18, 2018Date of Patent: February 23, 2021Assignee: TOSOH CORPORATIONInventors: Arimitsu Takemoto, Hiroshi Awano, Hisao Eguchi, Manabu Yanase
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Patent number: 8987441Abstract: 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: GrantFiled: September 21, 2011Date of Patent: March 24, 2015Assignee: Shionogi & Co., Ltd.Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
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Publication number: 20140329746Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Patent number: 8835419Abstract: 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: GrantFiled: November 30, 2012Date of Patent: September 16, 2014Assignee: 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
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Publication number: 20140235650Abstract: 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: ApplicationFiled: June 22, 2012Publication date: August 21, 2014Applicant: MetabolysInventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
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BIPHENYL DERIVATIVES, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND PREPARATION METHOD THEREOF
Publication number: 20140228568Abstract: 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: ApplicationFiled: February 8, 2013Publication date: August 14, 2014Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Hyunah CHOO, Young-Jae KIm, Jeeyeon KIM, Mi Young YEOM -
Patent number: 8778949Abstract: 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: GrantFiled: January 10, 2011Date of Patent: July 15, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Eric L. Stangeland, Lori Jean Patterson
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Patent number: 8778948Abstract: 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: GrantFiled: December 22, 2009Date of Patent: July 15, 2014Assignee: NHWA Pharma, CorporationInventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
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Patent number: 8765950Abstract: 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: GrantFiled: January 9, 2012Date of Patent: July 1, 2014Assignee: Purdue Research FoundationInventors: Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
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Publication number: 20140155409Abstract: 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: ApplicationFiled: June 22, 2012Publication date: June 5, 2014Applicant: MetabolysInventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
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Publication number: 20140086834Abstract: 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: ApplicationFiled: May 24, 2011Publication date: March 27, 2014Applicant: UNIVERSITA' DEGLI STUDI DI BARI ''ALDO MORO''Inventors: Marcello Leopoldo, Enza Lacivita, Nicola Colabufo, Paola De Giorgio, Francesco Berardi, Roberto Perrone
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Patent number: 8674089Abstract: 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: GrantFiled: June 28, 2010Date of Patent: March 18, 2014Assignee: DIC CorporationInventors: Kutzner Fabian, Gaudl Kai-uwe, Yoshinobu Sakurai, Tatsushi Okuda
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Publication number: 20140030189Abstract: 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: ApplicationFiled: June 12, 2013Publication date: January 30, 2014Inventors: Ajay Purohit, Thomas D. Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
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Publication number: 20130296455Abstract: 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: ApplicationFiled: December 27, 2011Publication date: November 7, 2013Applicant: ADEKA CORPORATIONInventors: Yosuke Maeda, Masaaki Shimizu, Koichi Shigeno
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Publication number: 20130172315Abstract: 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: ApplicationFiled: November 30, 2012Publication date: July 4, 2013Applicant: ChemoCentryx, Inc.Inventor: ChemoCentryx, Inc.
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Publication number: 20130064770Abstract: 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: ApplicationFiled: May 26, 2011Publication date: March 14, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Ian Martin Newington, Duncan George Wynn, Robert James Domett Nairne, Benedicte Guilbert, Subrata Mandal, Jinto Jose, Sunderaraman Varadarajan, Chitralekha Rangaswamy, Helen Betts, Rebecca Davis
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Patent number: 8252796Abstract: 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: GrantFiled: September 29, 2009Date of Patent: August 28, 2012Assignees: CSPC Zhonggi Pharmaceutical Technology (Shijiazhuang) Co. Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng
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Publication number: 20120190846Abstract: 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: ApplicationFiled: June 28, 2010Publication date: July 26, 2012Applicant: DIC CORPORATION.Inventors: Kutzner Fabian, Gaudl Kai-uwe, Yoshinobu Sakurai, Tatsushi Okuda
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Publication number: 20120107830Abstract: 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: ApplicationFiled: January 9, 2012Publication date: May 3, 2012Inventors: Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
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Patent number: 8153637Abstract: 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: GrantFiled: December 16, 2010Date of Patent: April 10, 2012Assignee: SanofiInventors: Marco Baroni, Olaf Ritzeler, Marco Zanchet
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Publication number: 20110318388Abstract: 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: ApplicationFiled: October 19, 2009Publication date: December 29, 2011Applicant: Akaal Pharma Pty LtdInventors: Gurmit S. Gill, Damian W. Grobelny
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Publication number: 20110294822Abstract: 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: ApplicationFiled: December 22, 2009Publication date: December 1, 2011Applicant: NHWA PHARMA. CORPORATIONInventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
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THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF
Publication number: 20110183996Abstract: 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: ApplicationFiled: September 29, 2009Publication date: July 28, 2011Applicant: Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng -
Patent number: 7985752Abstract: 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: GrantFiled: May 29, 2009Date of Patent: July 26, 2011Assignee: SK Holdings Co., Ltd.Inventors: Yonggil Kim, Nahmryune Cho, Yunhee Kim, Joon Heo, Seonmin Dong, Mi Kyung Ji, Man-Young Cha, Kiho Lee
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Publication number: 20110124657Abstract: 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: ApplicationFiled: July 30, 2009Publication date: May 26, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosalia Pascual-Ramon, H. Helmut Buschmann
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Publication number: 20100317854Abstract: 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: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20100286164Abstract: 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: ApplicationFiled: October 10, 2008Publication date: November 11, 2010Applicant: The Brigham and Women's Hospital, IncInventors: Corinne Elizabeth Augelli-Szafran, Michael S. Wolfe, Han-Xun Wei
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Patent number: 7829713Abstract: 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: GrantFiled: February 27, 2007Date of Patent: November 9, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Terrence P. Keenan, Alan P. Kaplan
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Publication number: 20100279997Abstract: 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: ApplicationFiled: October 28, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20100227855Abstract: 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: ApplicationFiled: March 16, 2010Publication date: September 9, 2010Applicant: ENDORECHERCHE, INC.Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, René Maltais
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Publication number: 20100221182Abstract: 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: ApplicationFiled: December 21, 2007Publication date: September 2, 2010Inventors: Ajay Purohit, Thomas D, Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
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Patent number: 7750012Abstract: 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: GrantFiled: August 3, 2006Date of Patent: July 6, 2010Assignee: deCODE genetics ehfInventors: Vincent Sandanayaka, Jasbir Singh, Li-Ming Zhou, Mark E. Gurney
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Publication number: 20100056545Abstract: 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: ApplicationFiled: April 23, 2009Publication date: March 4, 2010Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Kye Jung SHIN, Hyung Kook LEE, Eun Joo ROH, Dong Jin KIM, Kyung Il CHOI, Hyewhon RHIM, Hye Jin CHUNG, Seon Hee SEO
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Patent number: 7671055Abstract: 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: GrantFiled: October 20, 2005Date of Patent: March 2, 2010Assignee: FMC CorporationInventors: Edward J. Barron, Y. Larry Zhang, Frank J. Zawacki, John W. Lyga, George Theodoridis
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Patent number: 7642262Abstract: 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: GrantFiled: December 3, 2004Date of Patent: January 5, 2010Assignee: Asubio Pharma Co., Ltd.Inventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura
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Publication number: 20090253710Abstract: 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: ApplicationFiled: June 30, 2008Publication date: October 8, 2009Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic
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Publication number: 20090219526Abstract: 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: ApplicationFiled: December 29, 2008Publication date: September 3, 2009Inventors: Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
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Patent number: 7488731Abstract: 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: GrantFiled: July 24, 2007Date of Patent: February 10, 2009Assignee: 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
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Patent number: 7417043Abstract: 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: GrantFiled: December 21, 2004Date of Patent: August 26, 2008Assignee: NeuroSearch Sweden ABInventors: 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
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Patent number: 7390812Abstract: 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: GrantFiled: June 14, 2004Date of Patent: June 24, 2008Assignee: Gruenenthal GmbHInventors: Heinz Uragg, Corinne Maul, Helmut Buschmann, Bernd Sundermann, Hagen-Heinrich Hennies
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Patent number: 7256289Abstract: 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: GrantFiled: June 7, 2005Date of Patent: August 14, 2007Assignee: WyethInventors: Ivo Ladislav Jirkovsky, Joseph Zeldis, Gregg Brian Feigelson
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Patent number: 7241765Abstract: 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: GrantFiled: May 17, 2006Date of Patent: July 10, 2007Assignee: Neurogen CorporationInventors: 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
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Patent number: 7226925Abstract: 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: GrantFiled: June 18, 2003Date of Patent: June 5, 2007Assignee: Biovitrum ABInventors: Björn M. Nilsson, Erik Ringberg, Birger Sjöberg, Mattias Jönsson
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Patent number: 7186277Abstract: 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: GrantFiled: March 24, 2004Date of Patent: March 6, 2007Assignee: L'Oreal SAInventors: Alain Genet, Stéphane Sabelle
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Patent number: 7153858Abstract: 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: GrantFiled: January 30, 2004Date of Patent: December 26, 2006Assignee: 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
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Patent number: 7105521Abstract: 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: GrantFiled: June 30, 2003Date of Patent: September 12, 2006Assignee: Syn-Tech Chem & Pharm Co., Ltd.Inventor: Ing-Jun Chen
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Patent number: 7090703Abstract: 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: GrantFiled: March 24, 2004Date of Patent: August 15, 2006Assignee: L'OrealInventors: Stéphane Sabelle, Alain Genet, Madeleine Leduc
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Patent number: 7071197Abstract: 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: GrantFiled: June 16, 2003Date of Patent: July 4, 2006Assignee: Recordati S.A.Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 7067501Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.Type: GrantFiled: May 20, 2004Date of Patent: June 27, 2006Assignee: H. Lundbeck A/SInventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
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Patent number: 7019137Abstract: 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: GrantFiled: March 10, 2003Date of Patent: March 28, 2006Assignee: WyethInventors: Ivo Jirkovsky, Joseph Zeldis, Gregg Brian Feigelson