Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/351)
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Patent number: 7759367Abstract: The present invention relates to compositions comprising 1,2-dihydropiridin-2-one compounds and an immunoregulatory or anti-inflammatory agent. The compositions are useful for the prevention or the treatment of neurodegenerative diseases, for example demyelinating disorders.Type: GrantFiled: December 6, 2002Date of Patent: July 20, 2010Assignee: Eisai R&D Management Co., Ltd.Inventor: Terence Smith
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Publication number: 20100179197Abstract: Multi-substituted pyridyl sulfoximines are useful as insecticides.Type: ApplicationFiled: March 18, 2010Publication date: July 15, 2010Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers
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Publication number: 20100173951Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.Type: ApplicationFiled: June 4, 2008Publication date: July 8, 2010Inventors: Lawrence Wennogle, Peng Li, Jun Zhao
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Patent number: 7745426Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuro-protective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.Type: GrantFiled: August 12, 2004Date of Patent: June 29, 2010Assignees: D-Pharm Ltd., Advanced Neuroprotective Systems Ltd.Inventors: Svetlana Dolina, Vitaly Shteiman, Marina Vinnikova, Israel Shapiro
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Patent number: 7744911Abstract: A clear, water based, homogeneous insect repellent sunscreen composition, comprising an oil soluble hydrophobic sunscreen component, an amido insect repellent component, an alcohol component, and water.Type: GrantFiled: August 25, 2006Date of Patent: June 29, 2010Assignee: Avon Products, IncInventors: Andrew H. Pechko, Vincent T. Polywoda
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Publication number: 20100160390Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.Type: ApplicationFiled: March 2, 2010Publication date: June 24, 2010Applicant: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Publication number: 20100152252Abstract: The present invention relates to heterocyclyl-substituted-ethylamino-phenyl compounds of general formula (I), wherein K-L-M-N, Z and R1, R2, R3, R4 are as described in the claims methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: December 21, 2007Publication date: June 17, 2010Applicant: LABORATORIOS DEL DR. ESTEVE,S.A.Inventors: Mónica Garcia-López, Antonio Torrens-Jover, Luz Romero-Alonso, Helmut H. Buschmann
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Publication number: 20100152207Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: June 17, 2010Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
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Publication number: 20100137377Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: April 9, 2008Publication date: June 3, 2010Inventors: Anders Klarskov Petersen, Soren Ebdrup
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Patent number: 7728011Abstract: The present invention relates to novel skin-friendly dermally applicable liquid formulations comprising permethrin and agonists or antagonists of nicotinic acetylcholine receptors of insects for controlling parasitic insects on animals.Type: GrantFiled: October 9, 2003Date of Patent: June 1, 2010Assignee: Bayer Animal Health GmbHInventors: Kirkor Sirinyan, Hubert Dorn, Martin Gilges, Olaf Hansen
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Patent number: 7723364Abstract: Compound of general formula (I): Process for preparing this compound. Fungicidal composition comprising a compound of general formula (I). Method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: July 19, 2004Date of Patent: May 25, 2010Assignee: Bayer Cropscience SAInventors: Darren James Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier, Isabelle Christian
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Publication number: 20100113522Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: ApplicationFiled: October 13, 2009Publication date: May 6, 2010Applicant: Amgen Inc.Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
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Publication number: 20100111900Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: October 30, 2009Publication date: May 6, 2010Inventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
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Publication number: 20100081643Abstract: 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: September 21, 2009Publication date: April 1, 2010Inventors: BRETT C. BOOKSER, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
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Publication number: 20100075971Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: ApplicationFiled: December 1, 2009Publication date: March 25, 2010Inventors: Jacques DUMAS, Wendy Lee, Yuanwei Chen, Lila Adnane, William J. Scott, Sharad Verma, Jianqing Chen, Zhi Chen, Lin Yi
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Publication number: 20100076032Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: ApplicationFiled: November 11, 2009Publication date: March 25, 2010Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
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Patent number: 7674808Abstract: 4-pyridone (4-pyridinone) derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.Type: GrantFiled: May 29, 2007Date of Patent: March 9, 2010Assignee: Glaxo Group LimitedInventors: Jose Maria Bueno Calderon, Jesus Chicharro Gonzalo, Milagros Lorenzo Garcia, M Pilar Manzano Chinchon
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Patent number: 7674807Abstract: Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.Type: GrantFiled: March 1, 2005Date of Patent: March 9, 2010Assignee: Bayer CropScience AGInventors: Katsuaki Wada, Takuya Gombuchi, Yasushi Yoneta, Yuichi Otsu, Katsuhiko Shibuya, Norihiko Nakakura, Rüdiger Fischer, Tetsuya Murata, Eiichi Shimojo
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Publication number: 20100048643Abstract: Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.Type: ApplicationFiled: October 29, 2009Publication date: February 25, 2010Inventors: Gary M. Dull, Julio A. Munoz
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Publication number: 20100035879Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: May 29, 2009Publication date: February 11, 2010Inventors: Steven W. Elmore, Milan Bruncko, Cheol-Min Park
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Publication number: 20100028447Abstract: The present invention generally relates to pharmaceutical compositions for the intranasal, buccal, or sublingual administration of metanicotine analogs.Type: ApplicationFiled: January 22, 2008Publication date: February 4, 2010Applicant: TARGACEPT, INC.Inventors: Sharon Rae Letchworth, Merouane Bencherif, Gary Maurice Dull, David Moore, John W. James
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Patent number: 7655677Abstract: The present invention provides a composition for controlling a house insect pest, such as termites, ants or cockroaches, which comprises, as active ingredients, at least two compounds selected from the group consisting of (a) a certain pyridine compound, (b) a benzoylurea compound, (c) a pyrethroid compound and (d) a certain hydrazone compound; and a composition for controlling a house insect pest, which comprises, as an active ingredient, a certain hydrazone compound.Type: GrantFiled: April 18, 2008Date of Patent: February 2, 2010Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Masayuki Morita, Osamu Imai
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Publication number: 20100022601Abstract: The sulfoneamide compounds having the following Formula (1), which can be used as an effective component of a CaSR antagonizing agent useful for prophylaxis and/or treatment of bone disorders including osteoporosis and etc., are provided. The compounds have an excellent activity of promoting PTH secretion. In addition, the compounds are useful as an effective component of a medicament for the prophylaxis and/or treatment of bone disorders such as osteoporosis, bone fracture, hypoparathyroidism and the like.Type: ApplicationFiled: June 2, 2009Publication date: January 28, 2010Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Masami OGAWA, Kazuhiko KITAGAWA, Hiromitsu SHIRAHASHI, Satomi KURIBAYASHI
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Publication number: 20100016376Abstract: The present invention relates to a pyridone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.Type: ApplicationFiled: October 26, 2007Publication date: January 21, 2010Applicant: LG Life Sciences Ltd.Inventors: Hye Kyung Chang, Yeong Soo Oh, Yong Jin Jang, Sung Sub Kim, Kyeong Sik Min, Chul Woong Chung, Mi Jeong Park, Jung Gyu Park
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Publication number: 20090324569Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: December 31, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Patent number: 7629365Abstract: 3-Chloro-6-(hydroxymethyl)-2-methyl-5-[4-({4-[(trifluoromethyl)oxy]phenyl}oxy)phenyl]-4(1H)-pyridinone, having the following formula: is described along with its pharmaceutically acceptable salts, processes for its preparation, pharmaceutical formulations thereof and its uses in treatment of certain parasitic infections such as malaria.Type: GrantFiled: May 31, 2007Date of Patent: December 8, 2009Assignee: Glaxo Group LimitedInventors: Jose Maria Bueno Calderon, Jesus Chicharro Gonzalo, M Pilar Manzano Chinchon
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Publication number: 20090298890Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: July 5, 2007Publication date: December 3, 2009Applicant: BAYER CROPSCIENCE SAInventors: Pierre-Yves Coqueron, Marie-Claire Grosjean-Cournoyer, Philippe Desbordes, Pierre Genix, Benoit Hartmann, Amos Mattes, Klaus Kunz, Rudiger Fischer, Oliver Gaertzen, Oswald Ort, Darren Mansfield, Alain Villier
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Publication number: 20090275611Abstract: Compounds are provided which bind to and are agonist, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein R1, R2, R3, X and Ar have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: April 2, 2007Publication date: November 5, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
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Publication number: 20090264436Abstract: Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.Type: ApplicationFiled: April 17, 2009Publication date: October 22, 2009Inventors: Craig McKelvey, Sarah Geers, Justin Moser, Bhagwant Rege, Dina Zhang, Sutthilug Sotthivirat
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Publication number: 20090264477Abstract: Effective treatments of pain and/or inflammation are provided. Through the administration of an effective amount of at least one beta adrenergic agonist at or near a target site, one can reduce, prevent or treat pain and/or inflammation.Type: ApplicationFiled: April 15, 2009Publication date: October 22, 2009Applicant: Warsaw Orthopedic, Inc., An Indiana CorporationInventors: John Myers ZANELLA, Sara D. Waynick
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Publication number: 20090264476Abstract: Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabinoid inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.Type: ApplicationFiled: April 17, 2009Publication date: October 22, 2009Inventors: Craig McKelvey, Sarah Geers, Justin Moser, Bhagwant Rege, Dina Zhang, Sutthilug Sotthivirat
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Patent number: 7605164Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: February 14, 2006Date of Patent: October 20, 2009Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
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Publication number: 20090258884Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: ApplicationFiled: April 16, 2009Publication date: October 15, 2009Inventors: William K. Hagmann, Linus S. Lin, Shrenik K. Shah, Ravindra N. Guthikonda, Hongbo Qi, Linda L. Chang, Ping Liu, Helen M. Armstrong, James P. Jewell, Thomas J. Lanza, JR.
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Publication number: 20090253688Abstract: The present invention relates to semicarbazide derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: ApplicationFiled: February 14, 2005Publication date: October 8, 2009Applicant: Merck Patent GmbHInventors: Hans-Peter Buchstaller, Dirk Finsinger, Frank Stieber, Matthias Wiesner, Christiane Amendt, Christian Sirrenberg, Frank Zenke, Matthias Grell
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Patent number: 7585883Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.Type: GrantFiled: October 31, 2005Date of Patent: September 8, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Ankush Argade, David Carroll, Alexander B. Rossi
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Publication number: 20090221596Abstract: The invention relates to compounds of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and X are as defined in the description, to processes and intermediates for their preparation, and to their use for controlling pests.Type: ApplicationFiled: May 6, 2006Publication date: September 3, 2009Inventors: Iris Escher, Michael Müller, Peter Jeschke, Michael Beck, Oliver Gaertzen, Olga Malsam, Peter Lösel, Ulrich Ebbinghaus-Kintscher, Christian Arnold, Karl-Josef Haack
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Publication number: 20090221650Abstract: Methods for treating and/or preventing at least one symptom of a disorder associated with oxidative stress, carbonyl stress, or combinations thereof in a subject. In some embodiments, the methods include administering to the subject an effective amount of pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods for treating or preventing a nephropathy, acute renal injury, acute renal failure, or combinations thereof in a subject, and formulations adapted for intravenous administration comprising pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing.Type: ApplicationFiled: February 29, 2008Publication date: September 3, 2009Inventors: Billy G. Hudson, Paul Voziyan, Alp Ikizler
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Patent number: 7550490Abstract: The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis.Type: GrantFiled: July 11, 2007Date of Patent: June 23, 2009Assignee: Shenzhen Chipscreen Biosciences Ltd.Inventors: Xian-Ping Lu, Zhibin Li, Aihua Xie, Leming Shi, Boyu Li, Zhiqiang Ning, Song Shan, Tuo Deng, Weiming Hu
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Patent number: 7550488Abstract: The present invention discloses methods of application employing B5/B6 vitamins in molecular transport creams or gels to deliver B6 in a high dose to bring about therapeutic ways in human or mammal tissues to reverse a disease process or injury to bring about normal function of the affected tissues. Examples of disease changes to normal include, but are not limited to strokes, cellulitis, facial acne, precancerous lesions, nerve injury like paresthesia, periorbital hematoma, pentathol general anesthesia recovery, headaches, improved sight, hypothyroidism, dental pain, dental gingivitis, insect bites, delayed hypersensitivity states, phlebitis of veins and synergism of steroid activity.Type: GrantFiled: December 30, 2005Date of Patent: June 23, 2009Assignee: Dr. N's Health Care Products LLCInventor: Alfred A Nickel
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Publication number: 20090156639Abstract: The present invention relates to composition comprising at least one L-type calcium channel blocker, particularly the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, in combination with at least one cholinesterase inhibitor, particularly donepezil, and uses thereof in methods of treatment.Type: ApplicationFiled: February 20, 2009Publication date: June 18, 2009Inventors: Crista Trippodi-Murphy, Gregory M. Rose, Axel Unterbeck
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Publication number: 20090149496Abstract: The invention relates to the use of Kv1.5 inhibitors for the therapy or prophylaxis of respiratory disorders, sleep-related respiratory disorders, central and obstructive sleep apneas, upper airway resistance syndrome, Cheyne-Stokes respiration, snoring, disrupted central respiratory drive, sudden child death, postoperative hypoxia and apnea, muscle-related respiratory disorders, respiratory disorders after long-term ventilation, respiratory disorders during adaptation in high mountains, acute and chronic lung disorders with hypoxia and hypercapnia, neurodegenerative disorders, dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, cancer disorders, breast cancer, lung cancer, colon cancer and prostate cancer.Type: ApplicationFiled: October 16, 2008Publication date: June 11, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Joachim BRENDEL, Heinz GOEGELEIN, Klaus WIRTH, Walter KAMM
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Publication number: 20090137529Abstract: The compounds of the present invention are prodrugs of modulators of the Cannabinoid-1 (CB 1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB 1) receptor. In particular, compounds of the present invention are 5 prodrugs of antagonists or inverse agonists of the CB 1 receptor. The invention is concerned with the use of these compounds to be converted to compounds that modulate the Cannabinoid-1 (CB 1) receptor. As such, the compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-10 Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: May 11, 2007Publication date: May 28, 2009Inventors: William K. Hagmann, Milton L. Hammond
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Publication number: 20090131456Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: ApplicationFiled: January 26, 2009Publication date: May 21, 2009Inventors: Julian M.C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Publication number: 20090124664Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: ApplicationFiled: November 24, 2006Publication date: May 14, 2009Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
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Patent number: 7531535Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: December 13, 2007Date of Patent: May 12, 2009Assignee: Bristol-Meyers Squibb CompanyInventors: Donald J. P. Pinto, Jennifer X. Qiao
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Publication number: 20090118338Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
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Publication number: 20090105309Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: October 20, 2004Publication date: April 23, 2009Applicant: GLAXO GROUP LIMITEDInventors: Philip Charles Box, Diane Mary Coe, Heather Hobbs
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Patent number: RE40703Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: GrantFiled: October 3, 2006Date of Patent: April 28, 2009Assignee: Schering AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka