Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/316)
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Publication number: 20100004444Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.Type: ApplicationFiled: September 10, 2009Publication date: January 7, 2010Applicant: AstraZeneca ABInventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
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Publication number: 20100003709Abstract: This invention relates to crystallised human neutrophil elastase and the use of its three-dimensional structure to design modulators for human neutrophil elastase.Type: ApplicationFiled: December 13, 2005Publication date: January 7, 2010Applicant: Bayer HealthCare AGInventors: Peter Reinemer, Heike Gielen-Haertwig, Ulrich Rosentreter, Volkhart Li, Axel Harrenga, Dietmar Schomburg, Karsten Niefind, Guido Hansen
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Patent number: 7642303Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.Type: GrantFiled: October 13, 2005Date of Patent: January 5, 2010Inventors: Thomas L. Shakely, James John Krutak
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Publication number: 20090325988Abstract: Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: ApplicationFiled: June 3, 2009Publication date: December 31, 2009Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Christian Harcken, Rajashekhar Betageri, Todd Bosanac, Michael Jason Burke, Soojin Kim, Daniel Kuzmich, Thomas Wai-Ho Lee, Zhibin Li, Pingrong Liu, John Lord, Hossein Razavi, Jonathan Timothy Reeves, Daivd Thomson
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Publication number: 20090318425Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: June 23, 2009Publication date: December 24, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Edcon Chang, Stephen L. Gwaltney, Angie Vassar
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Publication number: 20090318467Abstract: The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.Type: ApplicationFiled: June 15, 2009Publication date: December 24, 2009Inventors: Jean-Michel Adam, Johannes Aebi, Alferd Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Publication number: 20090306074Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiazolidinedione derivatives.Type: ApplicationFiled: April 11, 2007Publication date: December 10, 2009Inventors: Michael Gerard Darcy, Steven David Knight, Nicholas D. Adams, Stanley J. Schmidt
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Publication number: 20090306112Abstract: The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: December 10, 2009Applicant: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Publication number: 20090291971Abstract: The present invention relates to processes for the preparation of heteroaryl ethers. In some embodiments, the processes relate to cross coupling reactions between triazol-1-yloxy and triazol-1-yl heterocycles with aryl boronic acids. In a further aspect, this invention also relates to compounds that are useful for the treatment of oncological diseases or disorders, and for the treatment of inflammation.Type: ApplicationFiled: October 30, 2008Publication date: November 26, 2009Applicant: WyethInventors: Tarek Suhayl Mansour, Sumrit Wacharasindhu, Zhao-Kui Wan, Sujata Bardhan
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Publication number: 20090292121Abstract: A therapeutic drug for cancer containing a substance selected from the group consisting of a novel cyanopyridine derivative, a pharmaceutically acceptable salt, a hydrate, a water adduct and a solvate as an active ingredient can be provided.Type: ApplicationFiled: April 28, 2006Publication date: November 26, 2009Inventors: Masahiko Morioka, Hiroshi Ikegami, Makoto Sakiyama, Masayuki Hayashi, Shinsuke Ooike, Yasuhiro Fujino, Daisuke Abe, Hideo Tomozane
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Publication number: 20090275599Abstract: A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects.Type: ApplicationFiled: June 18, 2007Publication date: November 5, 2009Applicant: TORAY INDUSTRIES, INC.Inventors: Kenichi Hayashi, Mie Kaino, Hiroyuki Meguro
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Publication number: 20090264401Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: April 21, 2009Publication date: October 22, 2009Applicant: AstraZeneca ABInventors: Adrian Liam GILL, Andrew Leach, Martin Packer, James Stewart Scott, Pernilla Sorme, John Gibbin Swales, Paul Robert Owen Whittamore
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Publication number: 20090258853Abstract: This invention relates to compounds which are agonists of somatostatin and selective toward somatostatin receptor subtype SSTR2. The compounds are useful in the treatment and prevention of diabetes, and diabetes-related pathologies, including retinopathy, neuropathy and nephropathy. Many of the compounds are orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostatin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof.Type: ApplicationFiled: March 9, 2007Publication date: October 15, 2009Inventors: Brian Eastman, Craig W. Lindsley, Scott E. Wolkenberg, Zhijian Zhao
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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: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Publication number: 20090258854Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: ApplicationFiled: April 9, 2009Publication date: October 15, 2009Inventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearny, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillan, JR., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 7595326Abstract: A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 ?M.Type: GrantFiled: February 9, 2007Date of Patent: September 29, 2009Assignee: Champions Biotechnology, Inc.Inventors: Saeed R. Khan, Gurulinsappa Hallur, Manuel Hidalgo, Antonio Jimeno
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Publication number: 20090215803Abstract: A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.Type: ApplicationFiled: October 23, 2006Publication date: August 27, 2009Inventors: Kenneth D. Rice, Neel Kumar Anand, Arlyn Arcalas, Charles M. Blazey, Joerg Bussenius, Wai Ki Vickey Chan, Hongwang Du, Sergey Epshteyn, Mohamed Abdulkader Ibrahim, Patrick Kearney, Abigail R. Kennedy, Moon Hwan Kim, Jean-Claire Limun Manalo, Csaba J. Peto, Tsze H. Tsang, Amy Lew Tsuhako, Peiwen Zhou, Elena S. Koltun
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Publication number: 20090215730Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.Type: ApplicationFiled: May 5, 2006Publication date: August 27, 2009Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gomez
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Publication number: 20090216013Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: ApplicationFiled: August 8, 2008Publication date: August 27, 2009Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedso, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce-Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswara Santhosh
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Publication number: 20090209451Abstract: The present invention relates to heteroarylaminopyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.Type: ApplicationFiled: April 13, 2009Publication date: August 20, 2009Applicant: Bayer Pharmaceuticals CorporationInventors: Joachim Rudolph, Phillip Wickens, Chih-Yuan Chuang, Libing Chen, Steven Magnuson, Alan Olague, Ning Qi
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Publication number: 20090209564Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: March 19, 2007Publication date: August 20, 2009Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
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Patent number: 7566723Abstract: The invention relates to novel 1-Phenyl-3,4-dihydropyrimidin-2(1H)-one derivatives having the formula processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: August 28, 2003Date of Patent: July 28, 2009Assignee: Bayer Healthcare AGInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 7566724Abstract: The compounds of the disclosure, for example, the compound represented by the formula: has excellent therapeutic and prophylactic effects against inflammatory bowel disease. Further, they are excellent in absorption and in vivo stability when administered orally in comparison with conventional compounds. That is, the compounds can be administered orally, and can have excellent therapeutic or prophylactic effect sustained for a longer period of time.Type: GrantFiled: December 22, 2005Date of Patent: July 28, 2009Assignee: Toray Industries, Inc.Inventors: Noriyuki Hirano, Hideki Inoue, Takashi Nagahara, Tomofumi Ohyama, Mie Kaino, Kenichi Hayashi, Sunao Hara, Ryutaro Suzuki
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Publication number: 20090182144Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].Type: ApplicationFiled: February 6, 2007Publication date: July 16, 2009Applicant: Taisho Pharmaceutical Co., Ltd.Inventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
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Patent number: 7560464Abstract: The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.Type: GrantFiled: April 13, 2005Date of Patent: July 14, 2009Assignee: Icagen, Inc.Inventors: Xiaodong Wang, Kerry Leigh Spear, Alan Bradley Fulp, Darrick Seconi, Takeshi Suzuki, Takahiro Ishii, Ayako Moritomo
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Patent number: 7560467Abstract: The present invention relates to indazolo-tetrahydropyrimidine-carboxamide derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such indazolo-tetrahydropyrimidine-carboxamide derivatives are useful in the treatment of diseases associated with inappropriate ROCK-1 kinase.Type: GrantFiled: June 18, 2004Date of Patent: July 14, 2009Assignee: SmithKline Beecham CorporationInventors: David Harold Drewry, Brian Evans, Krista B. Goodman, Darren Victor Steven Green, David Kendall Jung, Dennis Lee, Robert A. Stavenger, Sjoerd Nocolaas Wadman
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Publication number: 20090170883Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.Type: ApplicationFiled: November 12, 2008Publication date: July 2, 2009Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
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Publication number: 20090124615Abstract: The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 29, 2007Publication date: May 14, 2009Inventors: Kevin Kuntz, Kyle Allen Emmitte, Tara Renae Rheault, Stephon Smith, Keith Hornberger, Hamilton Dickson, Mui Cheung
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Publication number: 20090118283Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: May 7, 2009Applicant: Devgen NVInventors: Olivier Raynald Defert, Gert De Wilde, Petra Blom, Dirk Casimir Maria Leysen, Thomas Brown, Nadzeya Kaval
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Publication number: 20090111791Abstract: Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.Type: ApplicationFiled: March 8, 2007Publication date: April 30, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephane De Lombaert, Anne Bettina Eldrup, Jennifer A. Kowalski, Ingo Andreas Mugge, Fariba Soleymanzadeh, Alan David Swinamer, Steven John Taylor
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Publication number: 20090105248Abstract: Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.Type: ApplicationFiled: December 18, 2008Publication date: April 23, 2009Inventors: Ginny D. Ho, Deen Tulshian, Shu-Wei Yang
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Publication number: 20090105279Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: April 23, 2009Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Publication number: 20090099218Abstract: This invention provides a series of BPU analogues; their synthesis and evaluated biological activity. BPU sulfur analogues were found to possess up to 20 fold increased potency, when compared to compound 1, in various cancerous cell lines.Type: ApplicationFiled: September 16, 2008Publication date: April 16, 2009Inventors: Saeed R. Khan, Gurulingappa Hallur, Manuel Hidalgo, Antonio Jimeno
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Publication number: 20090088422Abstract: The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 13, 2008Publication date: April 2, 2009Inventors: Akira Kubo, Ritsuo Imashiro, Hiroaki Sakurai, Hidetaka Miyoshi, Akihito Ogasawara, Hajime Hiramatsu, Tatsuo Nakajima, Tetsu Nakane
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Publication number: 20090062294Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 23, 2008Publication date: March 5, 2009Inventors: Richard Apodaca, J. Guy Breitenbucher, Natalie A. Hawryluk, William M. Jones, John M. Keith, Jeffrey E. Merit, Mark S. Tichenor, Amy K. Timmons
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Publication number: 20090054446Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: October 31, 2008Publication date: February 26, 2009Inventors: Dominik FEUERBACH, Konstanze Hurth, Timothy John Ritchie
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Publication number: 20090042896Abstract: The invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, R4, n, o, p, and q are as defined herein and to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: August 4, 2008Publication date: February 12, 2009Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
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Publication number: 20090042841Abstract: This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds and compositions in the treatment of lower urinary tract disorders, such as neuromuscular dysfunction of the lower urinary tract, and in the treatment of migraine and gastroesophagael reflux disease (GERD).Type: ApplicationFiled: August 4, 2008Publication date: February 12, 2009Applicant: Recordati Ireland LimitedInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani, Matteo Longhi
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Publication number: 20090036467Abstract: A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.Type: ApplicationFiled: August 1, 2008Publication date: February 5, 2009Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20090023763Abstract: New antagonists of the A2B adenosine receptor represented by formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of the A2B adenosine receptor.Type: ApplicationFiled: April 12, 2005Publication date: January 22, 2009Inventors: Bernat Vidal Juan, Paul Robert Eastwood, Jacob Gonzalez Rodriguez
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Publication number: 20090017003Abstract: The present invention relates to novel thiosulfonates derivatives. The present invention also provides methods for preventing, treating and/or reducing inflammation-associated diseases in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous or cutaneous systems as well as infective and tumoral diseases employing said compounds.Type: ApplicationFiled: March 1, 2007Publication date: January 15, 2009Applicant: SULFIDRIS S.R.L.Inventors: Piero Del Soldato, Giancarlo Santus, Anna Sparatore
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Patent number: 7473695Abstract: The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 maybe the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 20, 2004Date of Patent: January 6, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Kubo, Ritsuo Imashiro, Hiroaki Sakurai, Hidetaka Miyoshi, Akihito Ogasawara, Hajime Hiramatsu, Tatsuo Nakajima, Tetsu Nakane
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Publication number: 20080312262Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.Type: ApplicationFiled: August 21, 2008Publication date: December 18, 2008Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Jacques Froissant, Christian Hoornaert
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Publication number: 20080306098Abstract: A method for modulating at least one pharmacokinetic property of a protease inhibitor upon administration to a host is provided. One administers to the host an effective amount of a bifunctional compound of less than about 5000 daltons comprising the protease inhibitor or an active derivative thereof and a pharmacokinetic modulating moiety. The pharmacokinetic modulating moiety binds to at least one intracellular protein. The bifunctional compound has at least one modulated pharmacokinetic property upon administration to the host as compared to a free drug control that comprises the protease inhibitor.Type: ApplicationFiled: May 5, 2008Publication date: December 11, 2008Inventors: Mitchell W. Mutz, Jason E. Gestwicki
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Publication number: 20080300191Abstract: Disclosed are protease inhibitors for coronaviruses and SARS-CoV, or picornaviruses, and the use of these protease inhibitors for preventing, reducing, ameliorating and treating a disease or condition caused by coronaviruses and SARS-CoV, or picornaviruses.Type: ApplicationFiled: May 6, 2004Publication date: December 4, 2008Inventors: Sui Xiong Cai, William E. Kemnitzer, Hong Zhang, Han-Zhong Zhang
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Publication number: 20080300247Abstract: The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 29, 2007Publication date: December 4, 2008Inventors: Kevin Kuntz, Kyle Allen Emmitte, Tara Renae Rheault, Stephon Smith, Keith Hornberger, Hamilton Dickson, Mui Cheung
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Publication number: 20080275031Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: June 16, 2008Publication date: November 6, 2008Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Publication number: 20080269267Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof aType: ApplicationFiled: April 18, 2008Publication date: October 30, 2008Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman