The Additional Hetero Ring Contains Nitrogen As The Only Ring Hetero Atom [e.g., N-(cyclopentylcarbonyl-l-histidyl)-pyrrolidine, Etc.] Patents (Class 548/314.7)
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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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Publication number: 20090181949Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R1-R4 have the meanings given in the specification.Type: ApplicationFiled: September 2, 2008Publication date: July 16, 2009Inventors: Cornelis G. KRUSE, Josephus H.M. LANGE, Arnoldus H.J. HERREMANS, Herman H. VAN STUIVENBERG
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Publication number: 20090171097Abstract: A synthesis method for pyrrole-imidazole polyamide is automated at a higher level and can produce a product with a high yield in a more stable manner. In a solid phase synthesis method, the automated synthesis of a polyimide can be promoted by using HCTU as a condensation-activator, the yield of a product can be increased by charging a monomer in a solid form, and a pyrrole-imidazole polyamide having any sequence can be synthesis by combining the synthesis method with a manual synthesis with an acid chloride.Type: ApplicationFiled: November 14, 2006Publication date: July 2, 2009Inventors: Hiroshi Sugiyama, Chikara Dohno, Noboru Fukuda
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Publication number: 20090156619Abstract: The present invention related to compounds of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Compounds of the present invention are useful for treating or preventing neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: October 26, 2006Publication date: June 18, 2009Inventors: Philip Jones, Jesus Maria Ontoria Ontoria
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Patent number: 7547694Abstract: The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: July 10, 2007Date of Patent: June 16, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Kirsten Arndt, Henri Doods, Gerhard Schaenzle
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Publication number: 20090149471Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: May 8, 2007Publication date: June 11, 2009Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Matthew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi k. Sawyer, Jan Antoinette C. Romero
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Publication number: 20090124559Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.Type: ApplicationFiled: December 15, 2006Publication date: May 14, 2009Applicant: Trustees of Tufts College Office of Technology and Industry CollaborationInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
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Publication number: 20090117074Abstract: The invention relates to compounds of formula (I) which are effective inhibitors of histone deacetylases.Type: ApplicationFiled: April 7, 2006Publication date: May 7, 2009Applicant: NYCOMED GmbHInventors: Thomas Maier, Thomas Bar, Thomas Beckers, Astrid Zimmermann, Frank Dullweber, Volker Gekeler
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Patent number: 7528156Abstract: The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: November 22, 2004Date of Patent: May 5, 2009Assignee: AstraZeneca ABInventors: Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
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Patent number: 7524867Abstract: The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB1 receptor modulators, in particular CB1 receptor antagonists or inverse agonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said imidazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art.Type: GrantFiled: May 27, 2005Date of Patent: April 28, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Josephus H. M Lange, Henderik C. Wals, Cornelis G. Kruse
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Publication number: 20090075975Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: November 24, 2008Publication date: March 19, 2009Inventors: Michael R. DeGraffenreid, JAY P. POWERS, Daqing Sun, Xuelei Yan
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Publication number: 20090069284Abstract: 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: October 21, 2008Publication date: March 12, 2009Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
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Patent number: 7501445Abstract: This invention relates to compounds of the following formula: in which R1, R2, A1, A2, X, Y, m, n, p, x and y are as defined herein, pharmaceutical compositions comprising the compounds and use of the compounds in treating enterovirus infection.Type: GrantFiled: October 30, 2006Date of Patent: March 10, 2009Assignee: National Health Research InstitutesInventors: Jyh-Haur Chern, Shin-Ru Shih, Chiung-Tong Chen, Chih-Shiang Chang, Chung-Chi Lee, Yen-Chun Lee, Chia-Liang Tai
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Publication number: 20090048225Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: ApplicationFiled: August 15, 2005Publication date: February 19, 2009Inventors: Don Richard Finley, Terry Patrick Finn, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Takako Takakuwa
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Publication number: 20090032106Abstract: There is provided novel n-type conjugated compounds based on 2-vinyl-4,5-dicyanoimidazole moieties conjugated via the vinyl group to an aromatic moiety. Also provided are thin films and photovoltaics comprising the novel compounds, as well as methods of synthesizing the compounds.Type: ApplicationFiled: July 31, 2007Publication date: February 5, 2009Inventors: Alan Sellinger, Richard Yee Cheong Shin, Thomas Kietzke, Zhikuan Chen, Sundarraj Sudhakar
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Patent number: 7482374Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: July 17, 2004Date of Patent: January 27, 2009Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Henry Anderson Kelly, Nigel Stephen Watson, Robert John Young
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Publication number: 20090005428Abstract: The present invention relates to novel compounds having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).Type: ApplicationFiled: December 21, 2006Publication date: January 1, 2009Inventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson, Maria Saxin
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Publication number: 20080311079Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: ApplicationFiled: April 10, 2008Publication date: December 18, 2008Applicant: Vertex Pharmaceuticals IncorporatedInventors: Robert B. Perni, John J. Court, Shawn D. Britt, Janos Pitlik, John H. van Drie
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Publication number: 20080306091Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tanglesType: ApplicationFiled: July 28, 2008Publication date: December 11, 2008Applicant: WyethInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Patent number: 7442713Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3, R4 and p are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.Type: GrantFiled: May 16, 2003Date of Patent: October 28, 2008Assignee: Merckle GmbHInventors: Stefan Laufer, Hans-Guenter Striegel, Wolfgang Albrecht, Karola Tollmann
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Publication number: 20080262045Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: ApplicationFiled: May 5, 2008Publication date: October 23, 2008Inventors: Anders Eriksson, Matti Lepisto, Michael Lundkvist, Magnus Munck Af Rosenschold, Pavol Zlatoidsky
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Patent number: 7425633Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, T, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting dipeptidyl peptidase IV or for treating Type II diabetes with such a compound.Type: GrantFiled: August 28, 2006Date of Patent: September 16, 2008Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Hsing-Pang Hsieh
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Patent number: 7417047Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: GrantFiled: June 29, 2006Date of Patent: August 26, 2008Assignee: WyethInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Publication number: 20080200511Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject).Type: ApplicationFiled: June 16, 2004Publication date: August 21, 2008Applicant: ASTON UNIVERSITYInventors: Martin Griffin, Ian George Coutts, Robert Edward Saint
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Patent number: 7407974Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: April 18, 2005Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
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Patent number: 7407972Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: December 20, 2004Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventor: Jeremy John Edmunds
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Patent number: 7402683Abstract: The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis in illnesses in people or animals, especially diseases of bacterial infection.Type: GrantFiled: April 14, 2003Date of Patent: July 22, 2008Assignee: Bayer HealthCare AGInventors: Nina Brunner, Christoph Freiberg, Thomas Lampe, Ben Newton, Michael Otteneder, Josef Pernerstorfer, Jens Pohlmann, Guido Schiffer, Mitsuyuki Shimada, Niels Svenstrup, Rainer Endermann, Peter Nell
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Patent number: 7399748Abstract: The present invention relates to an administration schedule comprising the intravenous administration of a ?-halogen-acryloyl distamycin derivative, or a pharmaceutically acceptable salt thereof. The above administration allows the treatment of a variety of tumors in mammals.Type: GrantFiled: September 21, 2001Date of Patent: July 15, 2008Assignee: Nerviano Medical Sciences S.r.l.Inventors: Camilla Fowst, Franzanne Vreeland, Maria Cristina Rosa Geroni
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Patent number: 7399868Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: GrantFiled: September 20, 2005Date of Patent: July 15, 2008Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
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Patent number: 7378433Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: December 13, 2006Date of Patent: May 27, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Patent number: 7368465Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: GrantFiled: March 13, 2002Date of Patent: May 6, 2008Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
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Patent number: 7361663Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: October 16, 2003Date of Patent: April 22, 2008Assignee: Aventis Pharmaceuticals Inc.Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
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Patent number: 7361654Abstract: The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Bristol-Myers Squibb Co.Inventors: James Sheppeck, T. G. Murali Dhar, Lidia Doweyko, John Gilmore, David Weinstein, Hai-Yun Xiao, Bingwei V. Yang, Arthur M. Doweyko
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Patent number: 7361678Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.Type: GrantFiled: March 5, 2003Date of Patent: April 22, 2008Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi S. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
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Patent number: 7354965Abstract: The present invention provides a novel azo compound, a curable composition comprising a colorant superior in the light-fastness and heat resistance of a dye, pattern-forming characteristics (developing characteristics) and liquid preserving characteristics, a color filter using the curable composition and a method of producing the color filter.Type: GrantFiled: September 16, 2004Date of Patent: April 8, 2008Assignee: FUJIFILM CorporationInventor: Katsumi Araki
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Patent number: 7335753Abstract: The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using such compounds as anti-infective, anti-proliferative agents, anti-inflammatory, and/or prokinetic agents.Type: GrantFiled: February 21, 2006Date of Patent: February 26, 2008Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Deping Wang, Joyce A. Sutcliffe, Adegboyega K. Oyelere, Timothy S. McConnell, Joseph A. Ippolito, John N. Abelson, Dane M. Springer, Joseph M. Salvino, Rongliang Lou, Joel A. Goldberg, Jay J. Farmer, Erin M. Duffy, Ashoke Bhattacharjee
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Publication number: 20080044379Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 8, 2007Publication date: February 21, 2008Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20070249593Abstract: 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: April 18, 2007Publication date: October 25, 2007Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Patent number: 7279471Abstract: The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: April 15, 2005Date of Patent: October 9, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Kirsten Arndt, Henri Doods, Gerhard Schaenzle
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Patent number: 7265135Abstract: The invention relates to novel 2-Oxy, 2-Amino, and 2-Thio-imidazole compounds of formula (I): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and methods of using them in the treatment of neurological disorders and other disorders and conditions mediated by the histamine H3 receptor.Type: GrantFiled: January 14, 2004Date of Patent: September 4, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael Bogenstaetter, Nicholas I. Carruthers, Jill A. Jablonowski, Timothy W. Lovenberg, Kiev S. Ly
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Patent number: 7244747Abstract: The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: November 30, 2004Date of Patent: July 17, 2007Assignee: UCB, S.A.Inventors: Benoit Kenda, Philippe Michel, Yannick Quesnel
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Patent number: 7232817Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 27, 2005Date of Patent: June 19, 2007Assignees: G.D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 7205323Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.Type: GrantFiled: October 12, 2005Date of Patent: April 17, 2007Assignee: Glenmark Pharmaceuticals S.A.Inventors: Abraham Thomas, Gopalan Balasubramanian, V. S. Prasada Rao Lingam, Daisy Manish Shah
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Patent number: 7186843Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.Type: GrantFiled: April 29, 2004Date of Patent: March 6, 2007Assignee: Daiichi Pharmaceutical Co. Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7138421Abstract: This invention relates to anti-androgenic N-[?-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.Type: GrantFiled: May 10, 2004Date of Patent: November 21, 2006Assignee: Schring AktiengesellschaftInventors: Arwed Cleve, Volker Schulze, Dieter Zopf, Jens Hoffmann, Andreas Reichel, Karsten Parczyk
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Patent number: 7132543Abstract: The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenylene derivative as at least one oxidation base, and to a process for dyeing keratin fibers and a multi-compartment kit using the claimed dye composition. Such a composition makes it possible to obtain a chromatic, powerful, unselective and fast coloration of keratin fibers.Type: GrantFiled: March 29, 2004Date of Patent: November 7, 2006Assignee: L'Oreal S.A.Inventors: Laure Ramos, Stéphane Sabelle
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Patent number: 7132414Abstract: The present invention relates to pharmaceutical compositions containing, as active ingredient, a compound of formula: in which R1 represents a radical —NHCOR4 or —N(R5)—Y—R6, Y is CO or SO2, R4 represents a radical -alk-SO2—R11, -alk-SO2—CH?CH—R11 or Het substituted with —SO2—R11 or a phenyl radical substituted with —SO2—R11 or -alk-SO2—R11, R5 represents a hydrogen atom or an alkyl radical, R6 represents a phenylalkyl, Het or Ar radical, to the novel derivatives of formula (I) and to their preparation, as well s to their use in treating various disorders of the nervous system.Type: GrantFiled: February 4, 2004Date of Patent: November 7, 2006Assignee: Aventis Pharma S.A.Inventors: Daniel Achard, Herve Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
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Patent number: 7132534Abstract: The invention relates to novel pyrrolidyl-substituted para-phenylenediamine derivatives, to dye compositions containing them and to the process for dyeing keratin fibers using these compositions. The present invention makes it possible in particular to obtain a chromatic, strong, relatively unselective and resistant coloration of keratin fibers.Type: GrantFiled: July 7, 2003Date of Patent: November 7, 2006Assignee: L'OrealInventors: Stéphane Sabelle, Laure Ramos, Madeleine LeDuc
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Patent number: 7129359Abstract: This invention relates to compounds of the following formula: in which R1, R2, A1, A2, X, Y, m, n, p, x and y are as defined herein, pharmaceutical compositions comprising the compounds and use of the compounds in treating enterovirus infection.Type: GrantFiled: November 19, 2003Date of Patent: October 31, 2006Assignee: National Health Research InstitutesInventors: Jyh-Haur Chern, Shin-Ru Shih, Chiung-Tong Chen, Chih-Shiang Chang, Chung-Chi Lee, Yen-Chun Lee, Chia-Liang Tai