The Ring Nitrogen Is Bonded Directly To Nonshared Ring Carbons Of The Five-membered Hetero Ring (e.g., Isoindole, Etc.) Patents (Class 514/416)
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Patent number: 7776906Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.Type: GrantFiled: June 3, 2004Date of Patent: August 17, 2010Assignee: Bayer CropScience AGInventors: Wilhelm Brandes, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Krüger
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Publication number: 20100197725Abstract: The present invention relates to derivatives of 1-oxo-isoindoline-4-carboxamides and of 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides, to the preparation thereof and to the therapeutic use thereof.Type: ApplicationFiled: January 26, 2010Publication date: August 5, 2010Applicant: SANOFI-AVENTISInventors: Bernard BAUDOIN, Michel EVERS, Arielle GENEVOIS-BORELLA, Andreas KARLSSON, Jean-Luc MALLERON, Magali MATHIEU
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Patent number: 7759387Abstract: This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.Type: GrantFiled: September 30, 2004Date of Patent: July 20, 2010Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Ashok Kumar Gangopadhyay, Vadlamudi V. S. V. Rao, Ravindra Dattatraya Gupte, Gopal Vishnu Gole, Asha Kulkarni-Almeida, Sridevi Krishnan, Radha Bhaskar Panicker, Eleanor Pinto De Souza
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Patent number: 7759386Abstract: This invention relates to novel pharmaceutical carrier or excipient systems and oral pharmaceutical compositions comprising 1-[4-(2-Azepan-1yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol or 2-(4-Hydroxy-phenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)benzyl]-1H-indol-5-ol, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 20, 2007Date of Patent: July 20, 2010Assignee: Wyeth LLCInventors: Eric Joel Benjamin, Wendy Ann Dulin, Jiwaji Gulabrao Suryawanshi
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Publication number: 20100179145Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygType: ApplicationFiled: October 12, 2007Publication date: July 15, 2010Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Patent number: 7754725Abstract: Compounds having the formula (I): and in particular, those of subgenus VIIa are disclosed as inhibits or modulators of the activity of the heat shock protein Hsp90. As such they are useful for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma.Type: GrantFiled: March 1, 2007Date of Patent: July 13, 2010Assignee: Astex Therapeutics Ltd.Inventors: Gianni Chessari, Maria Grazia Carr, Miles Stuart Congreve, Robert Downham, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
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Publication number: 20100173960Abstract: The invention relates generally to novel compositions and methods comprising one or more cyclohexanehexol and one or more NSAID. The compositions and methods provide beneficial effects in the treatment and prevention of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, in particular neurodegenerative diseases.Type: ApplicationFiled: September 20, 2007Publication date: July 8, 2010Inventors: Antonio Cruz, Carl Damiani
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Patent number: 7745478Abstract: Process for the preparation of stable nitroxide radicals (I) starting from N-benzylphthalimide in three steps. In the first step, the N-benzylphthalimide is transformed into N-benzyl-1,1,3,3-tetralkylisoindoline by treatment with a Grignard reagent prepared in methyl-tert-butyl ether. In the second step, the N-benzyl-1,1,3,3-tetraalkylisoindoline is transformed into 1,1,3,3-tetra-alkylisoindoline by hydrogenolysis. In the third step, the 1,1,3,3-tetra-alkyl-isoindoline is transformed into the nitroxide radical by oxidation with hydrogen peroxide in the presence of a catalyst selected from acids and salts of polymolybdic or polytungstic acids.Type: GrantFiled: August 25, 2005Date of Patent: June 29, 2010Assignee: Polimeri Europa S.p.A.Inventors: Maria Caldararo, Riccardo Po, Marco Ricci
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Publication number: 20100152184Abstract: The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C?O, (C?O)O, (C?O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C?O or (C?O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims.Type: ApplicationFiled: October 12, 2007Publication date: June 17, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Miles Stuart Congreve, Lynsey Helen Fazal, Martyn Frederickson, Christopher William Murray, Michael Alistair O'Brien, Andrew James Woodhead, John Francis Lyons, Neil Thomas Thompson
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Publication number: 20100144825Abstract: The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.Type: ApplicationFiled: June 20, 2008Publication date: June 10, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Fiaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao, Linghang Zhuang
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Patent number: 7732479Abstract: Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided.Type: GrantFiled: August 18, 2005Date of Patent: June 8, 2010Assignee: Tel Aviv University Future Technology Development L.P.Inventors: Ehud Gazit, Tomer Cohen
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Publication number: 20100129363Abstract: Methods of treating, preventing and/or managing hematological cancers are disclosed. Specific methods encompass the administration of a PDE4 inhibitor alone or in combination with a second active agent. The invention further relates to methods of treating leukemias and lymphomas which comprise the administration of a PDE4 inhibitor. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: November 18, 2009Publication date: May 27, 2010Inventors: Jerome B. Zeldis, Peter H. Schafer
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Publication number: 20100112048Abstract: The present invention relates to a synergistic combination for preventing the onset and/or progression of dementia or Alzheimer's disease in individuals at increased risk thereof for example because of family history, genetic factors, and/or environmental factors. This combination comprises synergistically effective amounts of vitamin C, vitamin E, DHA and at least one NSAID such as ibuprofen.Type: ApplicationFiled: July 19, 2006Publication date: May 6, 2010Inventor: Majid Fotuhi
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Patent number: 7705023Abstract: There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: GrantFiled: June 17, 2005Date of Patent: April 27, 2010Assignee: Biolipox ABInventors: Kristofer Olofsson, Benjamin Pelcman, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Publication number: 20100092469Abstract: The present invention is directed to a combination of therapeutic compounds and treatment methods and kits using the combination. In particular, one of the combination affects the NCca-ATP channel of neural tissue, including neurons, glia and blood vessels within the nervous system. Exemplary SUR1 and/or TRPM4 antagonists that inhibit the NCca-ATP channel may be employed in the combination. The combination therapy also employs one or more of a non-selective cation channel blocker and/or an antagonist of VEFG, NOS, MMP, or thrombin. Exemplary indications for the combination therapy includes the prevention, diminution, and/or treatment of injured or diseased neural tissue, including astrocytes, neurons and capillary endothelial cells, that is due to ischemia, tissue trauma, brain swelling and increased tissue pressure, or other forms of brain or spinal cord disease or injury, for example.Type: ApplicationFiled: February 8, 2008Publication date: April 15, 2010Inventors: J. Marc Simard, Vladimir Gerzanich
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Publication number: 20100092474Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygType: ApplicationFiled: October 12, 2007Publication date: April 15, 2010Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Publication number: 20100076051Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: November 25, 2009Publication date: March 25, 2010Applicant: ABBOTT LABORATORIESInventors: Michael L. Curtin, Steven K. Davidsen, Robin R. Frey, Howard R. Heyman, James H. Holms, Michael Michaelides, Douglas H. Steinman
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Patent number: 7683088Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: January 16, 2007Date of Patent: March 23, 2010Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong-Heon Kim, De-Yi Yang, Razia Rizvi
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Patent number: 7683068Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: June 23, 2006Date of Patent: March 23, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
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Patent number: 7678825Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an ?-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF? and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)2-methylsulfonylethyl]4,5-diaminoisoindoline-1,3-dione.Type: GrantFiled: May 12, 2008Date of Patent: March 16, 2010Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller
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Patent number: 7674802Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: GrantFiled: August 3, 2006Date of Patent: March 9, 2010Assignee: deCODE genetics, ehfInventors: Vincent Sandanayaka, Jasbir Singh, Lei Zhao, Mark E. Gurney
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Patent number: 7674817Abstract: The antimicrobial acid-catalyzed coating composition of the invention is an acid-catalyzed coating composition formulated with at least one antimicrobial agent to provide antimicrobial activity to the coating composition and an article coated therewith.Type: GrantFiled: May 12, 2005Date of Patent: March 9, 2010Assignee: Akzo Nobel Coatings International B.V.Inventor: James H. Bray, III
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Publication number: 20100056489Abstract: A method for treating a patient suffering from neuropathic pain, comprising administering to a patient in need of such treatment an effective amount of an agonist drug capable of binding to the neuronal nicotinic receptor (NNR) but which does not readily cross the blood-brain barrier.Type: ApplicationFiled: September 25, 2009Publication date: March 4, 2010Inventors: LYNNE E. RUETER, Kathy L. Kohlhaas
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Patent number: 7666899Abstract: The present invention provides pharmaceutical compositions for the prevention or treatment of lipid metabolism disorders. The pharmaceutical compositions comprising, as an active ingredient, (2S)-2-benzl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic aid (generic name: mitiglinide) or a pharmaceutically acceptable salt thereof, or a hydrate thereof exert remarkable lipid metabolism improving effect, and are useful for, for example, hyperlipidemia such as hypertriglyceridemia of diabetic patients or the like.Type: GrantFiled: April 27, 2005Date of Patent: February 23, 2010Assignee: Kissei Pharmaceutical, Co. Ltd.Inventors: Juichi Fukuyama, Masayuki Yamada
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Publication number: 20100040628Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.Type: ApplicationFiled: August 11, 2009Publication date: February 18, 2010Applicant: OsteoGeneX, IncInventors: Debra Ellies, William Rosenberg
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Patent number: 7662824Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: March 16, 2006Date of Patent: February 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Kristi Leonard, Tianbao Lu, Robert W. Tuman, Dana L. Johnson, Anna C. Maroney, Jan L. Sechler, Richard W. Connors, Richard S. Alexander, Maxwell D. Cummings, Robert A. Galemmo, Thomas P. Markotan
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Patent number: 7662821Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.Type: GrantFiled: October 12, 2004Date of Patent: February 16, 2010Assignee: Bayer Schering Pharma AGInventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
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Patent number: 7662849Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: June 4, 2004Date of Patent: February 16, 2010Assignee: ViroBay, Inc.Inventors: John W. Patterson, Soon H. Woo
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Patent number: 7662847Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.Type: GrantFiled: May 9, 2005Date of Patent: February 16, 2010Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller
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Publication number: 20100022514Abstract: The invention relates to the use of compounds in the treatment of deacetylase-associated diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.Type: ApplicationFiled: December 17, 2007Publication date: January 28, 2010Inventors: Young Shin Cho, Lei Jiang, Michael Shultz
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Publication number: 20090318465Abstract: The present invention relates to a method for identifying compounds that act as insulin-sensitizers. The method can include screening of test compounds in two assays of insulin sensitivity. This method can identify lead compounds for the treatment of disorders caused by insulin resistance to glucose uptake. This invention also includes methods for treating insulin resistance and related disorders.Type: ApplicationFiled: September 20, 2007Publication date: December 24, 2009Inventors: Rosalind Adaikalasamy Marita, Somesh Sharma, Jessy Anthony, Kelkar Aditya, Sujit Kaur Bhumra, Aditee Ghate, Kumar Venkata Subrahman Nemmani, Nabajyoti Deka, Ashok Kumar Gangopadhyay
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Publication number: 20090312323Abstract: Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: ApplicationFiled: March 16, 2007Publication date: December 17, 2009Applicants: The Government of the United States of America, as represented by the Secretary, Department of HHS, Albany Molecular Research, Inc., Science Applications International CorporationInventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Publication number: 20090298818Abstract: The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (VI): or a salt, solvate, tautomer or N-oxide thereof; wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n, R1, R2a, R3, R4a, R8 and R10 are as defined in the claims. The invention also provides the use of a compound of the formula (VI) for the manufacture of a medicament for the prophylaxis or treatment of a fungal, protozoal, viral or parasitic disease state or condition (other than a disease state or condition due to Plasmodium falciparum) or for use in the prophylaxis or treatment of Ewing's sarcoma, atherosclerosis or lupus erythematosus.Type: ApplicationFiled: October 12, 2007Publication date: December 3, 2009Inventors: John Francis Lyons, Neil Thomas Thompson
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Publication number: 20090291983Abstract: Compounds of formula I wherein R1, R2, R3, R4, R5 and R6 are as described in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: July 12, 2007Publication date: November 26, 2009Applicant: AstraZeneca ABInventors: Yevgeni Besidski, Ylva Gravenfors, Inger Kers, Karin Skogholm, Mats Svensson
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Publication number: 20090286775Abstract: New bicyclic derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.Type: ApplicationFiled: June 28, 2006Publication date: November 19, 2009Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
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Patent number: 7615563Abstract: 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: GrantFiled: February 17, 2005Date of Patent: November 10, 2009Inventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Zimmerman
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Publication number: 20090275630Abstract: Composition containing, in a physiologically acceptable medium, at least one imidopercarboxylic acid compound and at least one N-acylated amino acid ester of formula (A) as described herein.Type: ApplicationFiled: March 20, 2009Publication date: November 5, 2009Applicant: L'OREALInventors: Roxane Provost, Geoffroy Remaut, Cecile Kermorvan, Celine Moussay
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Patent number: 7612065Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: March 28, 2007Date of Patent: November 3, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Susanne Wilke, Francesco Salituro, Edmund Harrington, Jingrong Cao, Guy Bemis, Huai Gao
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Patent number: 7601729Abstract: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH?CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1? each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl;Type: GrantFiled: September 10, 2004Date of Patent: October 13, 2009Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Publication number: 20090239926Abstract: Methods of treating, managing or preventing psoriasis or psoriatic arthritis are disclosed. Specific methods encompass the administration of cyclopropyl-N-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindoline-4-yl}carboxamide, alone or in combination with a second active agent. Pharmaceutical compositions and single unit dosage forms are also disclosed.Type: ApplicationFiled: March 24, 2009Publication date: September 24, 2009Inventors: Peter H. Schafer, George W. Muller, Patricia E.W. Rohane
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Publication number: 20090238870Abstract: Dividable galenical form for the modified release of active ingredient, wherein the non-subdivided galenical form and a portion of said form obtained by subdivision have identical dissolution profiles. Medicaments.Type: ApplicationFiled: August 22, 2008Publication date: September 24, 2009Applicant: LES LABORATOIRES SERVIERInventors: Gilles Fonknechten, Patrick Genty, Jean-Manuel Pean, Patrick Wuthrich
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Patent number: 7589117Abstract: The present invention relates to the novel isoindolone derivatives of the formula I in which R1 to R6 have the meanings stated in the claims. The inventive compounds are suitable as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.Type: GrantFiled: March 1, 2006Date of Patent: September 15, 2009Assignee: sanofi-aventis Deutschland GmbHInventors: Heinz-Werner Kleemann, Armin Hofmeister, Jean-Christophe Carry, Baptiste Ronan, Serge Mignani, Antony Bigot
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Publication number: 20090221575Abstract: The present invention is related to sulfonamide derivatives of Formula (Ia) where the groups are as defined in the description, and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: ApplicationFiled: October 24, 2006Publication date: September 3, 2009Applicant: Laboratoires Serono SAInventors: Patrick Gerber, Dominique Swinnen, Agnes Bombrun
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Patent number: 7582670Abstract: The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of anti-inflammatory cytokines. The method typically comprises administration of one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA. Preferably the pharmaceutical composition comprises one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, an anti-inflammatory agent, and a pharmaceutically acceptable carrier.Type: GrantFiled: April 13, 2005Date of Patent: September 1, 2009Assignee: Natrogen Therapeutics, Inc.Inventors: Longgui Wang, Xiao Mei Liu, Lian Mo, Simon K. Mencher, James P. McCarron, Jr.
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Publication number: 20090215742Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as HSP-90 inhibitors.Type: ApplicationFiled: April 21, 2006Publication date: August 27, 2009Inventors: Lee Andrew Funk, Mary Catherine Johnson, Pei-Pei Kung, Zhongxiang Zhou
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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: 20090215772Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbylamino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.Type: ApplicationFiled: April 13, 2006Publication date: August 27, 2009Applicant: Astex Therapeutics LimitedInventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead, Robert Downham, Theresa Rachel Phillips
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Publication number: 20090209532Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.Type: ApplicationFiled: July 17, 2006Publication date: August 20, 2009Inventors: Marko Ahlmark, Reijo Backstrom, Anne Luiro, Jarmo Pystynen, Eija Tiainen
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Publication number: 20090203665Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: April 13, 2009Publication date: August 13, 2009Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Publication number: 20090203761Abstract: The present invention relates to processes for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetylguanidine derivatives of the formula I via 3-hydroxy-2,3-dihydro-1H-isoindol-1-one derivatives or 3-(2-carbamoylphenyl)-acrylic ester derivatives as intermediates, to a process for optical resolution, and to intermediates of the process according to the invention.Type: ApplicationFiled: April 2, 2009Publication date: August 13, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Gerrit SCHUBERT, Joerg RIEKE-ZAPP, Johannes KEIL, Heinz-Werner KLEEMANN, Reda HANNA, Bao-Guo HUANG, Xiao-Dong WU, Yves GOURAUD