Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 546/216)
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Patent number: 9896416Abstract: There are described new 1-alkyl-1-methyl-4-[(2,2-diphenyl-2-propoxy)acetoxy]piperidinium halides and pharmaceutical compositions comprising a 1-alkyl-1-methyl-4-[(2,2-diphenyl-2-propoxy)acetoxy]piperidinium halide as an active ingredient. These products are non-selective muscarinic acetylcholine receptor antagonists acting in the periphery and not in the brain.Type: GrantFiled: July 30, 2013Date of Patent: February 20, 2018Assignee: Chase Parmaceuticals CorporationInventors: Kathleen E. Clarence-Smith, Thomas N. Chase
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Patent number: 9758539Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R1, R2 or R3 is —P(?O)(OH)2, and the other two of R1, R2 and R3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.Type: GrantFiled: May 18, 2016Date of Patent: September 12, 2017Assignee: Tolero Pharmaceuticals, Inc.Inventors: Adam Siddiqui-Jain, David J. Bearss
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Patent number: 9242959Abstract: The present invention concerns novel (aza)benzhydryl ether derivatives which exhibit H4-receptor binding activity. The present invention also concerns their process of preparation and their therapeutical uses.Type: GrantFiled: June 5, 2013Date of Patent: January 26, 2016Assignee: BIOPROJETInventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
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Patent number: 9035061Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.Type: GrantFiled: November 26, 2013Date of Patent: May 19, 2015Assignee: Theravance Biopharma R&D IP, LLCInventor: Pierre-Jean Colson
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Publication number: 20150126518Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.Type: ApplicationFiled: October 30, 2014Publication date: May 7, 2015Applicant: HANALL BIOPHARMA CO., LTD.Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
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Publication number: 20150112067Abstract: The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are CGRP receptor antagonists, useful for the treatment of migraine. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of Formulae B (after salt break) and C with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent.Type: ApplicationFiled: March 13, 2013Publication date: April 23, 2015Inventors: Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyushi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch, Teresa Andreani
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Patent number: 8975280Abstract: A compound of Formula I are provided: wherein R is: R1 is a substituted or unsubstituted alkyl group; W1-4 are independently selected from hydrogen, substituted or unsubstituted alkyl groups, substituted or unsubstituted haloalkyl groups, substituted or unsubstituted alkanoyl groups, substituted or unsubstituted aroyl groups, or substituted or unsubstituted haloalkanoyl groups; X1-5 are independently selected from H, NO2, N3, and NH2; Y is absent or is a substituted or unsubstituted C1-alkyl group, other than carbonyl; Z is selected from a bond or NH, provided that when Z is a bond, Y is absent, and provided that when Z is NH, Y is a substituted or unsubstituted C1-alkyl group, other than carbonyl. Also provided are D-arabinitol compounds, methods for preparing such compounds and compositions of such compounds, and methods of using such compounds.Type: GrantFiled: May 22, 2007Date of Patent: March 10, 2015Assignee: The Chancellor, Masters and Scholars of The University of OxfordInventors: Terry D. Butters, Raymond A. Dwek, George W. J. Fleet
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Patent number: 8969571Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: November 22, 2013Date of Patent: March 3, 2015Assignee: Theravance Respiratory Company, LLCInventors: Mathai Mammen, Adam Hughes, Yan Chen
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Publication number: 20150057443Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.Type: ApplicationFiled: August 21, 2014Publication date: February 26, 2015Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
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Patent number: 8940743Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: GrantFiled: October 24, 2006Date of Patent: January 27, 2015Assignee: Janssen Pharmaceutica NVInventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
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Publication number: 20150025110Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: October 9, 2014Publication date: January 22, 2015Inventors: Henrietta Dehmlow, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Hans Richter
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Publication number: 20140371269Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof, where the variables for R1, R2, and R3 are as described herein; methods of treating a condition such as hypertriglyceridemia; and processes for preparing the compounds.Type: ApplicationFiled: January 16, 2013Publication date: December 18, 2014Applicant: Eli Lilly and CompanyInventors: Maria Carmen Fernandez, Maria Rosario Gonzalez-Garcia, Bin Liu, Lance Allen Pfeifer
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Patent number: 8912219Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: GrantFiled: March 14, 2014Date of Patent: December 16, 2014Assignee: Genentech, Inc.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
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Publication number: 20140296343Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.Type: ApplicationFiled: March 31, 2014Publication date: October 2, 2014Inventors: Frank M. LONGO, Stephen M. MASSA, Sandeep GUPTA
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Publication number: 20140275032Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Genentech, Inc.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
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Patent number: 8791134Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention 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, ischemia/reperfusion injury and cancer.Type: GrantFiled: October 18, 2012Date of Patent: July 29, 2014Assignee: Cardioxyl Pharmaceuticals, Inc.Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
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Publication number: 20140163024Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 10, 2013Publication date: June 12, 2014Applicant: GENENTECH, INC.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
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Publication number: 20140086896Abstract: The present invention provides novel compositions as well as methods for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.Type: ApplicationFiled: November 19, 2013Publication date: March 27, 2014Applicant: AMICUS THERAPEUTICS, INC.Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
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Patent number: 8680281Abstract: This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3 ), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: GrantFiled: January 7, 2009Date of Patent: March 25, 2014Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbHInventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Robert D. Simpson
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Publication number: 20140038943Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 10, 2013Publication date: February 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
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Patent number: 8642583Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: GrantFiled: October 29, 2009Date of Patent: February 4, 2014Assignee: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi T. Tran, Victoria D. Wong
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Patent number: 8633322Abstract: The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: October 28, 2010Date of Patent: January 21, 2014Assignee: Janssen Pharmaceutica NVInventors: Michael H. Parker, Dennis J. Hlasta, Yifang Huang, Allen B. Reitz, Edward C. Lawson, Carsten Schubert, Eric Strobel, Brett A. Tounge, Kimberly White, Michael P. Winters, Shyamali Ghosh
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Publication number: 20140011796Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
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Patent number: 8624033Abstract: A process for the preparation of 14-O—[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl)acetyl]mutilins of formula feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O—[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.Type: GrantFiled: October 26, 2012Date of Patent: January 7, 2014Assignee: Nabriva Therapeutics AGInventors: Ingolf Macher, Andreas Berger, Martin Decristoforo
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Patent number: 8580405Abstract: The present invention provides a novel naphthothiophene compound having a high lowest excited triplet level (T1).Type: GrantFiled: April 11, 2011Date of Patent: November 12, 2013Assignee: Canon Kabushiki KaishaInventors: Naoki Yamada, Jun Kamatani, Akihito Saitoh
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Publication number: 20130296569Abstract: The invention relates to a process to prepare pharmacologically active phosphoric acid mono-(1-{4-[(S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2,6-difluoro phenyl}-4-methoxy methyl-piperidin-4-yl)ester.Type: ApplicationFiled: February 3, 2011Publication date: November 7, 2013Inventors: Vijaykumar Jagdishwar Patil, Rajkumar Vishwanath Hangarge, Burhanuddin Munshi Zaki Ahmed, Loganathan Velupillai, Bharat Kalidas Trivedi
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Publication number: 20130287727Abstract: The present specification discloses psyllid attractants, compositions comprising such attractants, lures, traps and other devices using such attractants, methods and uses to attract, capture and/or kill psyllids using such attractants, compositions and/or lures, traps and/or other devices, and methods and uses for monitoring a psyllid population using such attractants, compositions and/or lures, traps and/or other devices.Type: ApplicationFiled: April 25, 2013Publication date: October 31, 2013Applicant: INSCENT, INC.Inventors: Daniel F. Woods, Spiros Dimitratos
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Patent number: 8518934Abstract: The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: June 11, 2009Date of Patent: August 27, 2013Assignee: Shonogi & Co., Ltd.Inventor: Hidenori Mikamiyama
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Publication number: 20130203815Abstract: The present invention provides compounds represented by general formula (I): wherein, R1, R2, R3, L and T are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, and prodrugs thereof. The invention also relates to processes for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful in the treatment of a condition or disorder mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?) and interleukins such as IL-1, IL-6, and IL-8. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (I) or its pharmaceutical composition, to a mammal in need thereof.Type: ApplicationFiled: March 25, 2011Publication date: August 8, 2013Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Babasaheb Pandurang Bandgar, Jalindar Vasant Totre
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Publication number: 20130203734Abstract: Disclosed herein are methods of preventing or treating inflammatory diseases using sulfonamide analogs of 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I?), and the medical uses of the compounds, are described herein.Type: ApplicationFiled: June 8, 2011Publication date: August 8, 2013Inventors: David John Grainger, David John Fox
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Patent number: 8501778Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.Type: GrantFiled: June 20, 2008Date of Patent: August 6, 2013Assignees: NHWA Pharma. Corporation, Shanhai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
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Publication number: 20130190288Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130178612Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.Type: ApplicationFiled: September 22, 2011Publication date: July 11, 2013Applicant: CHIRALGEN, LTD.Inventors: Takeshi Wada, Mamoru Shimizu
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Patent number: 8450345Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.Type: GrantFiled: February 22, 2010Date of Patent: May 28, 2013Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics CorporationInventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
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Publication number: 20130109718Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: October 24, 2012Publication date: May 2, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8431563Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 23, 2011Date of Patent: April 30, 2013Assignee: Amgen Inc.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Publication number: 20130085127Abstract: A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.Type: ApplicationFiled: May 23, 2011Publication date: April 4, 2013Applicant: ASKA Pharmaceutical Co., LtdInventors: Makoto Okada, Koichi Hasumi, Takahiro Nishimoto, Miwa Yoshida, Kouki Ishitani, Tomoji Aotsuka, Hashime Kanazawa
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Publication number: 20130045951Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention 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, ischemia/reperfusion injury and cancer.Type: ApplicationFiled: October 18, 2012Publication date: February 21, 2013Applicant: CARDIOXYL PHARMACEUTICALS, INC.Inventor: CARDIOXYL PHARMACEUTICALS, INC.
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Patent number: 8362040Abstract: Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: GrantFiled: May 28, 2010Date of Patent: January 29, 2013Assignee: Novartis AGInventors: Richard Sedrani, Juergen Klaus Maibaum, Werner Breitenstein, Holger Sellner, Claus Ehrhardt, Nils Ostermann
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Patent number: 8334389Abstract: A process for the preparation of 14-O-[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl) acetyl]mutilins of formula (I) feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O-[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.Type: GrantFiled: October 3, 2007Date of Patent: December 18, 2012Assignee: Nabriva Therapeutics AGInventors: Ingolf Macher, Andreas Berger, Martin De Cristoforo
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Patent number: 8329911Abstract: The invention provides compounds of formula I: wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: November 12, 2009Date of Patent: December 11, 2012Assignee: Theravance, Inc.Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Eric L. Stangeland
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Patent number: 8324251Abstract: The present application describes modulators of MIP-1? or CCR-1 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, ring A, T, V, X, R1, R2 and R8, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: GrantFiled: October 3, 2007Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventor: Percy H. Carter
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Patent number: 8318737Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: GrantFiled: February 16, 2011Date of Patent: November 27, 2012Assignees: Canthera Therapeutics Inc., The General Hospital CorporationInventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova, Sam Lee
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Patent number: 8273895Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: GrantFiled: December 14, 2010Date of Patent: September 25, 2012Assignee: Opko Health, Inc.Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Patent number: 8263624Abstract: The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: GrantFiled: May 25, 2007Date of Patent: September 11, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Härter, Tobias Wunberg, Swen Allerheiligen, Marcus Bauser, Ulrich Rester, Stefan Heitmeier
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Publication number: 20120225854Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 23, 2011Publication date: September 6, 2012Applicant: AMGEN INC.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Publication number: 20120225890Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: March 6, 2012Publication date: September 6, 2012Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, David Larsen, David L. Coffen, Charlotte Coffen
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Dopamine transporter inhibitors for use in treatment of movement disorders and other CNS indications
Patent number: 8258305Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.Type: GrantFiled: February 21, 2006Date of Patent: September 4, 2012Assignee: Prexa Pharmaceuticals, Inc.Inventor: James R. Hauske -
Patent number: 8211916Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: January 22, 2008Date of Patent: July 3, 2012Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Publication number: 20120142659Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Applicant: ASTRAZENECA ABInventors: Jonas Bostrõm, Hans Emtenäs, Kenneth Granberg, Mickael Mogemark, Antonio Llinas