Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/322)
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Patent number: 8067603Abstract: The invention relates to a group of novel benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these imidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1): wherein the symbols have the meanings as given in the description.Type: GrantFiled: September 22, 2004Date of Patent: November 29, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Jacobus A. J. Den Hartog, Gustaaf J. M. Van Scharrenburg, Herman H. Van Stuivenberg, Tinka Tuinstra, Jan-Willem Terpstra
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Patent number: 8067613Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: GrantFiled: July 15, 2008Date of Patent: November 29, 2011Assignee: Abbott LaboratoriesInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D Penning, Gui-Dong Zhu
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Publication number: 20110288088Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: May 17, 2011Publication date: November 24, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.I.Inventors: Tiziano BANDIERA, Andrea LOMBARDI BORGIA, Sten Christian ORRENIUS, Ettore PERRONE, Italo BERIA, Daniele FANCELLI, Arturo GALVANI
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Patent number: 8063036Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 7, 2010Date of Patent: November 22, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20110281868Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman
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Publication number: 20110281843Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 15, 2009Publication date: November 17, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri
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Publication number: 20110281855Abstract: The present invention provides a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol. The present invention further provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol.Type: ApplicationFiled: April 21, 2011Publication date: November 17, 2011Applicant: GRUENENTHAL GMBHInventor: RAMESH SESHA
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Publication number: 20110281840Abstract: This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, R5, R6, R7, k, m, n, p, q, r and s are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity.Type: ApplicationFiled: January 22, 2010Publication date: November 17, 2011Inventors: Kazuo Ando, Yasuhiro Iwata
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Publication number: 20110275612Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.Type: ApplicationFiled: May 14, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
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Publication number: 20110275616Abstract: Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.Type: ApplicationFiled: July 18, 2011Publication date: November 10, 2011Applicant: AIKO BIOTECHNOLOGYInventors: Wolfgang Sadée, Edward Bilsky, Janet Yancey-Wrona
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Patent number: 8053431Abstract: The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: GrantFiled: November 1, 2006Date of Patent: November 8, 2011Assignee: High Point Pharmaceuticals, LLCInventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Publication number: 20110269742Abstract: Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.Type: ApplicationFiled: December 14, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Neil Moss, Christopher Ronald Sarko, Samantha Jayne Bamford, Pui Leng Loke, Spencer Charles R. Napier, Heather Tye, Mark Whittaker
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Publication number: 20110263648Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, A, B, W and n are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.Type: ApplicationFiled: October 21, 2009Publication date: October 27, 2011Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
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Publication number: 20110263588Abstract: The present invention relates to compounds that may be negative allosteric modulators of metabotropic receptors-subtype 5, and methods of making and using same.Type: ApplicationFiled: October 23, 2009Publication date: October 27, 2011Applicant: GLAXO GROUP LIMITEDInventors: Peter Bertinato, Merav Fichman, Shomir Ghosh, Jian Lin, Dalia Segal, Zhaoda Zhang
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Publication number: 20110263566Abstract: 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives, which are useful for PBK inhibitors, are provided.Type: ApplicationFiled: July 30, 2009Publication date: October 27, 2011Inventors: Yo Matsuo, Yingfu Li, Joel Walker, Feryan Ahmed, Ryuji Ohsawa, Shoji Hisada
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Publication number: 20110263559Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Inventors: Xuqing ZHANG, Marta G. ABAD, Alan C. GIBBS, Gee-Hong KUO, Lawrence C. KUO, Fengbin SONG, Zhihua SUI
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Publication number: 20110263560Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.Type: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Applicant: NOVARTIS AGInventors: Werner BREITENSTEIN, Takeru EHARA, Claus EHRHARDT, Philipp GROSCHE, Yuko HITOMI, Yuki IWAKI, Takanori KANAZAWA, Kazuhide KONISHI, Juergen Klaus MAIBAUM, Keiichi MASUYA, Atsuko Nihonyanagi, Nils OSTERMANN, Masaki SUZUKI, Atsushi TOYAO, Fumiaki YOKOKAWA
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Patent number: 8044213Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.Type: GrantFiled: December 10, 2009Date of Patent: October 25, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jianping Cai, Shaoqing Chen, Yi Chen, Xin-Jie Chu, Robert Alan Goodnow, Jr., Kang Le, Kin-Chun Luk, Steven Gregory Mischke, Peter Michael Wovkulich
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Publication number: 20110250268Abstract: The present invention is related to novel oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and one or more small carboxylic acid molecules as parietal cell activators in the gastric lumen. Unexpectedly, the compositions of the present invention are capable of enhancing the anti-acid activity of PPI in the stomach. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.Type: ApplicationFiled: April 19, 2011Publication date: October 13, 2011Inventors: Aleksey Kostadinov, David Ayelet, Sabina Glozman, Tal Atarot
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Publication number: 20110250172Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 8, 2011Publication date: October 13, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Yat Sun Or
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Publication number: 20110245231Abstract: The invention relates to novel drug substance for the treatment of alcohol dependence, pharmaceutical composition, medicament and method for treatment of dependence on using ethyl alcohol containing beverages.Type: ApplicationFiled: December 15, 2009Publication date: October 6, 2011Applicant: Alla Chem, LLCInventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
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Publication number: 20110237624Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Applicant: LABORATOIRE THERAMEXInventors: Benoit RONDOT, Jean LAFAY, Paule BONNET, Thierry CLERC, Igor DUC, Eric DURANTI, François PUCCIO, Jacqueline SHIELDS, Christian BLOT, Philippe MAILLOS
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Patent number: 8026233Abstract: Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders mediated by p38.Type: GrantFiled: March 27, 2007Date of Patent: September 27, 2011Assignee: Array BioPharma Inc.Inventors: Mark C. Munson, Kevin W. Hunt, Christopher T. Clark, Ganghyeok Kim, Laurence E. Burgess, James P. Rizzi
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Patent number: 8026257Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: GrantFiled: July 1, 2008Date of Patent: September 27, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Andrew P. Degnan, George O. Tora, Derek J. Denhart, Vivekananda M. Vrudhula, John E. Macor, Joanne J. Bronson
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Patent number: 8026256Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.Type: GrantFiled: October 26, 2005Date of Patent: September 27, 2011Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Erol K. Bayburt, John R. Koenig, Chih-Hung Lee
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Publication number: 20110230518Abstract: The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.Type: ApplicationFiled: December 15, 2009Publication date: September 22, 2011Applicant: MERCK SERONO S.A.Inventors: Mathilde Muzerelle, Anna Quattropani, Cyril Montagne, Jérôme Dorbais
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Patent number: 8022059Abstract: A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl; R4 is hydrogen, halogen or alkyl; R5 is hydrogen or alkyl; R6 and R7 are the same or different and each hydrogen or halogen, or a pharmaceutically acceptable salt thereof, which is useful as IKur blocker effective for preventing or treating cardiac arrhythmia such as atrial fibrillation.Type: GrantFiled: September 26, 2008Date of Patent: September 20, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Tetsuo Yamaguchi, Hiroyuki Kawanishi, Hideki Ushirogochi, Tatsuyuki Takahashi, Tohru Takebe
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Publication number: 20110224254Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20110224195Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: August 18, 2008Publication date: September 15, 2011Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
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Publication number: 20110224141Abstract: A method of treatment and/or prevention of cancer comprises administering agents which cause increased intracellular granularity in cancer cells, at least in an amount sufficient to inhibit proliferation of such cells and preferably in an amount sufficient to lead to cancer cell death. The method is particularly directed to refractory cancer, particularly hormone refractory prostate cancer. The agents identified cause increased intracellular granularity in the cancer cells, and also convert adherent cancer cells to non-adherent cancer cells, leading to cancer cell death. Using the present invention, cancer cells undergo increased intracellular granularity at relatively low agent concentrations, while also inhibiting cell proliferation. Increased concentrations lead to conversion of adherent cancer cells to non-adherent cancer cells, then to cell death.Type: ApplicationFiled: June 5, 2009Publication date: September 15, 2011Applicant: STC.UNMInventors: Todd A. Thompson, Debra Mackenzie, Tudor I. Oprea, Larry A. Sklar, Bruce S. Edwards, Mark Haynes
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Publication number: 20110224137Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).Type: ApplicationFiled: November 17, 2009Publication date: September 15, 2011Inventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Publication number: 20110224188Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: ApplicationFiled: November 20, 2008Publication date: September 15, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Antonio Jose del Moral Barbosa, Joerg Martin Benzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan Mckibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
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Publication number: 20110217383Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40 95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5 60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250 % by weight of a non-porous inert lubricant, 1 to 35 % by weight of a neutral cellulosic compound and 1 to 25 % by weight of an emulsifier, each calculated on dry weight of the polymer mixture.Type: ApplicationFiled: September 24, 2008Publication date: September 8, 2011Inventors: Hans Bär, Thomas Fürst, Gerhard Renner, Michael Gottschalk
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Patent number: 8012995Abstract: The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.Type: GrantFiled: September 28, 2000Date of Patent: September 6, 2011Assignee: Merck Serono SAInventors: Stephen Arkinstall, Serge Halazy, Dennis Church, Montserrat Camps, Thomas Rueckle, Jean Pierre Gotteland, Marco Biamonte
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Publication number: 20110212941Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: ApplicationFiled: November 3, 2009Publication date: September 1, 2011Inventors: Peter J. Manley, Kausik K. Nanda, B. Wesley Trotter
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Patent number: 8008326Abstract: The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.Type: GrantFiled: July 21, 2005Date of Patent: August 30, 2011Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Istvan Gyertyan, Jozsef Nagy, Sandor Kolok, Kornel Galgoczy, Katalin Saghy
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Patent number: 8008327Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: April 23, 2009Date of Patent: August 30, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Darren DiSalvo, Daniel Kuzmich, Can Mao, Hossein Razavi, Christopher Ronald Sarko, Alan David Swinamer, David Smith Thomson, Qiang Zhang
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Publication number: 20110207727Abstract: A series of novel thio-substituted anthra[1,2-d]imidazole-6,11-dione dervatives, and the preparation method and application of said derivatives, said application having a pharmaceutical composition containing said derivatives with therapeutically effective amount for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG
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Publication number: 20110207699Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 9, 2010Publication date: August 25, 2011Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd N. Soltwedel, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Clarence J. Maring, Michael D. Tufano, David A. Betebenner, Todd W. Rockway, Dachun Liu, John K. Pratt, Michael J. Lavin, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Publication number: 20110207777Abstract: Compounds of formula (I), salts and solvates are provided, Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: March 20, 2007Publication date: August 25, 2011Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Patent number: 8003669Abstract: The present invention has been made based on the finding that a compound acting on the ORL-1 receptor as an agonist acts as a non-photic entrainment factor, and advances the circadian rhythm phase, and provides a novel therapeutic agent for a sleep disorder such as circadian rhythm sleep disorder, more particularly, an agent for the prophylaxis and/or treatment of a sleep disorder, which contains an ORL-1 receptor agonist, and a novel compound useful as such agent for the prophylaxis and/or treatment.Type: GrantFiled: April 28, 2009Date of Patent: August 23, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Koji Teshima, Masanori Minoguchi
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Patent number: 8003668Abstract: The present invention comprises the use of amino-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes.Type: GrantFiled: September 14, 2007Date of Patent: August 23, 2011Assignee: Sanofi-AventisInventors: Elisabeth Defossa, Karl Schoenafinger, Gerhard Jaehne, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 8003806Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
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Publication number: 20110200586Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110201604Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
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Publication number: 20110201590Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: ApplicationFiled: August 25, 2009Publication date: August 18, 2011Applicant: SANOFI-AVENTISInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Publication number: 20110200587Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110195964Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: October 19, 2009Publication date: August 11, 2011Inventors: Qun Dang, De Michael Chung, Tony S. Gibson, Daniel K. Cashion, HongJian Jiang, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
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Patent number: 7994202Abstract: A nitrogen-containing bicyclic heterocyclic compound represented by the following formula (1) is provided. When the compound or a salt thereof is administered to a human being or an animal, the compound has a strong antagonistic action against EP1 receptors, and is useful, for example, as an active ingredient of a medicine for the prevention and/or treatment of overactive bladder. The compound is also useful as an active ingredient of a medicine for the prevention and/or treatment of symptoms such as frequency urinary, urinary urgency, or urinary incontinence.Type: GrantFiled: July 14, 2009Date of Patent: August 9, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Masakazu Atobe, Kenji Naganuma, Akifumi Morimoto
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Patent number: 7994197Abstract: Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (Cmax) and slightly delaying the peak such as to avoid activating the dopaminergic and adrenergic receptors, while achieving sufficient active binding to the serotonin receptors to provide relief from migraine symptoms within a timeframe that permits rapid resolution of migraine symptoms. Inhaler devices suitable for the methods are disclosed. Kits for practicing the methods of invention are disclosed.Type: GrantFiled: August 26, 2009Date of Patent: August 9, 2011Assignee: MAP Pharmaceuticals, Inc.Inventors: Robert O. Cook, Stephen B. Shrewsbury, Nabih N. Ramadan, Thomas A. Armer