Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
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Patent number: 8138192Abstract: Methods of treating or preventing a vertigo, nausea, or vomiting condition comprising injecting a subject with a pharmaceutically acceptable formulation consisting essentially of an effective amount of meclizine or a pharmaceutically acceptable salt thereof, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 are disclosed. An injectable pharmaceutical formulation for treating or preventing a vertigo, nausea, or vomiting condition consisting essentially of an effective amount of meclizine, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 is also disclosed.Type: GrantFiled: October 31, 2007Date of Patent: March 20, 2012Assignee: Genebiology, Inc.Inventors: Walker Anderson Long, Edwin Curran Murphy, III
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Publication number: 20120046302Abstract: The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists.Type: ApplicationFiled: February 11, 2011Publication date: February 23, 2012Inventors: Kelly Papadakis, Nika Adham, Gary Samoriski
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Publication number: 20120040969Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: ApplicationFiled: October 28, 2011Publication date: February 16, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
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Publication number: 20120035188Abstract: Liquid formulations of lactic acid addition salts of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine are provided.Type: ApplicationFiled: April 16, 2010Publication date: February 9, 2012Applicant: H. LUNDBECK A/SInventors: Svend Treppendahl, Heidi Lopez De Diego
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Publication number: 20120028991Abstract: The present invention relates to pharmaceutical compositions containing dopamine receptor ligands and selective serotonin reuptake inhibitors and to methods of treating disorders such as schizophrenia, major depressive disorder and bipolar depression using combinations of dopamine receptor ligands and selective serotonin reuptake inhibitors. The present invention also relates to methods of treating depression using dopamine receptor ligands.Type: ApplicationFiled: October 10, 2011Publication date: February 2, 2012Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Gary Samoriski, Nika Adham
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Publication number: 20120022070Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.Type: ApplicationFiled: October 6, 2009Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
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Publication number: 20120015957Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: January 19, 2012Inventors: Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Victoria D. Wong
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Publication number: 20120004207Abstract: Compound corresponding to the general formula (I): in which A=N or CR2; R2?H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3?CHR4CONHR5; R4?H or C1-6-alkyl; R5?H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate. Therapeutic uses thereof.Type: ApplicationFiled: September 9, 2011Publication date: January 5, 2012Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Philippe Burnier, Christian Hoornaert, Jean Jeunesse, Frederic Puech
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Publication number: 20110312931Abstract: The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.Type: ApplicationFiled: June 2, 2011Publication date: December 22, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Christopher L. CIOFFI, Mark A. WOLF, Peter R. GUZZO, Shuang LIU, Kashinath SADALAPURE, Visweswaran PARTHASARATHY, Jun-Ho MAENG
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Publication number: 20110306614Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Patent number: 8076326Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein X is a bond or a group N—R4; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen, C1-C3 alkyl, fluorine, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, or C3-C4 cycloalkyl-CH2—; R5 is hydrogen, fluorine, chlorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R6 is hydrogen, fluorine or chlorine; and n is 1 or 2.Type: GrantFiled: April 30, 2010Date of Patent: December 13, 2011Assignees: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
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Patent number: 8076342Abstract: 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine hydrogen malonate salt and pharmaceutical comprising and uses of the same, including for the treatment of schizophrenia and other psychotic disorders are described.Type: GrantFiled: November 4, 2010Date of Patent: December 13, 2011Inventors: Heidi Lopez de Diego, Ole Nielsen, Lone Munch Ringgard, Henrik Svane, Allan Carsten Dahl, Mark Howells, Benny Bang-Andersen, Lars Ole Lyngso
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Publication number: 20110294775Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.Type: ApplicationFiled: August 12, 2008Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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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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Publication number: 20110281850Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: July 7, 2011Publication date: November 17, 2011Applicant: MANNKIND CORPORATIONInventors: Gary A. Flynn, Sandra Aeyoung Lee, Mary Faris, David William Brandt, Subrata Chakravarty
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Publication number: 20110269747Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: ApplicationFiled: July 13, 2011Publication date: November 3, 2011Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Publication number: 20110262566Abstract: Provided is a therapeutic agent for lower urinary tract symptom consisting of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof or a combination of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof and a compound selected from the group consisting of ?1-adrenergic receptor blockers, 5-? reductase inhibitors, antiandrogen drugs, ?3-adrenergic receptor agonists, phosphodiesterase V inhibitors, plant preparations, amino acid preparations, herbal medicines and the like. Also provided is a method of using in combination the above-described therapeutic agent and a surgical treatment such as bladder distention or surgery.Type: ApplicationFiled: November 2, 2009Publication date: October 27, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Natsuko Goto, Setsuko Yamamoto
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Publication number: 20110256129Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: April 25, 2011Publication date: October 20, 2011Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander Shoemaker, Michael Mitten
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Patent number: 8034818Abstract: Therapeutic uses of a compound corresponding to the general formula (I): in which A=N or CR2; R2=H, F, OH, CN, CF3, C1-6-alkyl, C1-6-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR2; B=covalent bond or C1-8-alkylene; R1=optionally substituted heteroaryl; R3=CHR4CONHR5; R4=H or C1-6-alkyl; R5=H, C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-C6-alkylene; in the form of a base, an acid-addition salt, a hydrate or a solvate.Type: GrantFiled: February 2, 2007Date of Patent: October 11, 2011Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Philippe Burnier, Christian Hoornaert, Jean Jeunesse, Frederic Puech
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Publication number: 20110245270Abstract: Use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases. For example, a method of treating pulmonary inflammation of an inflammatory disease selected from the group of asthma, interstitial pulmonary fibrosis (IPF), sarcoidosis, hypersensitivity pneumonitis (HP), and bronchiolitis obliterans with organizing pneumonitis (BOOP) in an animal in need thereof having said inflammation, including administering orally or by inhalation to said animal a nicotinic receptor agonist.Type: ApplicationFiled: June 15, 2011Publication date: October 6, 2011Applicant: UNIVERSITE LAVALInventors: Yvon CORMIER, Evelyne Israel-Assayag, Marie-Renée Blanchet
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Patent number: 8030489Abstract: Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.Type: GrantFiled: March 25, 2008Date of Patent: October 4, 2011Assignee: Astellas Pharma Inc.Inventors: Tatsuya Zenkoh, Eisuke Nozawa, Keisuke Matsuura, Ryushi Seo
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Publication number: 20110230446Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: May 25, 2011Publication date: September 22, 2011Applicants: Axys Pharmaceuticals, Inc., Merck Canada Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Chirstophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
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Patent number: 8022074Abstract: The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof; at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one ? receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.Type: GrantFiled: October 25, 2010Date of Patent: September 20, 2011Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Publication number: 20110218200Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.Type: ApplicationFiled: August 28, 2009Publication date: September 8, 2011Inventors: Christopher J. Barden, Michael D. Carter, Mark A. Reed, Donald F. Weaver, Arun Yadav, Shengguo Sun
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Publication number: 20110218207Abstract: Provided herein are isotopically enriched arylsulfonamides, for example, of Formula I, that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: March 1, 2011Publication date: September 8, 2011Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter
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Patent number: 8012982Abstract: The present invention is directed to compounds of formula (I): where X, Y, R1, R2 and R3 are defined therein, which can act as modulators of viral replication and/or virus production, especially of the hepatitis C virus (HCV).Type: GrantFiled: September 29, 2005Date of Patent: September 6, 2011Assignee: Istituto di Ricerche Biologia Molecolare P. Angeletti SpAInventors: Immacolata Conte, Caterina Ercolani, Claudio Giuliano, Giovanni Migliaccio, Gessica Filocamo, legal representative, Veronica Suriano, legal representative, Ian Stansfield
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Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
Publication number: 20110207739Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG -
Publication number: 20110207744Abstract: The invention relates to methods of treating cognitive dysfunction and improving cognitive functioning comprising the administration of trans-4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine or a pharmaceutically acceptable salt thereof to a patient in need thereof. Moreover the invention relates to an improved binder in a composition comprising 4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine.Type: ApplicationFiled: May 5, 2011Publication date: August 25, 2011Applicant: H. Lundbeck A/SInventors: Christina Kurre Olsen, Rene Holm, Christine Kau, Birgitte Willumsen, Klaus Peter Hertel, Lone Bruun, Karina Krojer Soby
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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: 20110178100Abstract: It is directed to provide a novel apoptosis inhibitor. Specifically directed is an apoptosis inhibitor containing a biphenylcarboxamide compound represented by the following formula (1) as an active ingredient, wherein R1 represents a hydrogen atom or a lower alkoxy group; R2 represents a hydrogen atom or a lower alkanoyl group; and n represents a number of 2 to 5.Type: ApplicationFiled: March 22, 2011Publication date: July 21, 2011Applicant: NIHON UNIVERSITYInventors: Kumiko Ishige, Yoshihisa Ito, Mioko Hirabayashi
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Publication number: 20110172246Abstract: 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: ApplicationFiled: January 10, 2011Publication date: July 14, 2011Inventors: Eric L. Stangeland, Lori Jean Patterson
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Publication number: 20110172174Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: October 31, 2007Publication date: July 14, 2011Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
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Patent number: 7973039Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: December 19, 2005Date of Patent: July 5, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110160200Abstract: The invention relates to methods of treating, preventing or delaying the onset or development of pulmonary hypertension using hydroxyl donors or pharmaceutically acceptable salts thereof. The invention further relates to methods of reducing mean pulmonary arterial pressure using hydroxyl donors or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: November 22, 2010Publication date: June 30, 2011Applicant: CARDIOXYL PHARMACEUTICALS, INC.Inventors: Reza Mazhari, Vincent J. Kalish
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Publication number: 20110160223Abstract: Provided are pharmaceutical compositions and methods of treatment or prophylaxis of certain neuropsychiatric conditions, in particular mood disorders. The compounds are of the general Formula I-V as described herein.Type: ApplicationFiled: November 2, 2010Publication date: June 30, 2011Inventors: Raymond J. Dingledine, Stephen F. Traynelis
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Patent number: 7968538Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.Type: GrantFiled: January 25, 2006Date of Patent: June 28, 2011Assignee: Galenea Corp.Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Silvia Noiman, Xiang Y. Yu, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20110145970Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Publication number: 20110152272Abstract: The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of urinary incontinence, preferably mixed incontinence or stress urinary incontinence. The invention also relates to the use of antagonists of 5-HT2C receptors for the treatment of urine retention. The present invention also relates to a method of treatment of incontinence, to assays to screen for compounds useful in the treatment of incontinence, and to methods of preparing compositions for the treatment of urinary incontinence.Type: ApplicationFiled: November 5, 2010Publication date: June 23, 2011Inventors: Gordon McMurray, Wesley Dennis Miner
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Publication number: 20110152245Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Katrin Groebke Zbinden, Roger Norcross, Philippe Pflieger
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Patent number: 7964605Abstract: The present invention relates to a novel piperazine derivative or pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition for treating central nervous system diseases comprising an effective amount of the piperazine compound and a method of treating central nervous system (CNS) disorder such as psychosis in a mammal.Type: GrantFiled: May 29, 2008Date of Patent: June 21, 2011Assignee: SK Holdings Co., Ltd.Inventors: Yonggil Kim, Kiho Lee, Nahmryune Cho, Jin Uk Yoo, Joon Heo, Choonho Ryu, Seonmin Dong, Man-Young Cha, Jong Gil Choi, Yunhee Kim, Mi Kyung Ji
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Publication number: 20110144125Abstract: The disclosure describes an animal model for simulating cardiac arrhythmia. Methods of discovering new anti-arrhythmia drugs using the model are described. Novel anti-arrhythmia agents are provided, as are pharmaceutical compositions made from the agents. Methods of inhibiting spontaneous mechanical activity in myocardially-derived biological systems, and methods of treating and preventing cardiac arrhythmia based on novel anti-arrhythmia agents are described. Kits for performing the above methods are also described.Type: ApplicationFiled: August 14, 2009Publication date: June 16, 2011Applicant: THE UAB RESEARCH FOUNDATIONInventor: Paul Wolkowicz
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Publication number: 20110144120Abstract: 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: ApplicationFiled: December 16, 2010Publication date: June 16, 2011Applicant: SANOFI-AVENTISInventors: Marco BARONI, Olaf RITZELER, Marco ZANCHET
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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: 20110118264Abstract: 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 mammalType: ApplicationFiled: January 28, 2011Publication date: May 19, 2011Inventors: Yonggil Kim, Nahmryune Cho, Yunhee Kim, Joon Heo, Seonmin Dong, Mi Kyung Ji, Man-Young Cha, Kiho Lee
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Publication number: 20110117214Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 15, 2010Publication date: May 19, 2011Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Ronald C. Newbold, Chengzhi Zhang
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Publication number: 20110112073Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Applicant: DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
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Publication number: 20110098282Abstract: Novel compounds of which the following is exemplary:Type: ApplicationFiled: August 12, 2008Publication date: April 28, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20110086863Abstract: The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I? and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine and chlorine.Type: ApplicationFiled: August 5, 2010Publication date: April 14, 2011Applicants: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Wilfried Martin Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Wolfgang Wernet, Matthias Mayrer, Ana Jongen-Relo, Anton Bespalov, Min Zhang
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Publication number: 20110077247Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Applicant: DAC S.r.I.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa