Additional Hetero Ring Patents (Class 514/444)
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Patent number: 7763612Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.Type: GrantFiled: January 3, 2007Date of Patent: July 27, 2010Assignee: Algebra, Inc.Inventors: Philip F. Morgan, James L. Kelley
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Patent number: 7754755Abstract: The present invention provides inhibitors of 15-LO according to Formula I, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.Type: GrantFiled: September 21, 2005Date of Patent: July 13, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, John E. Macor, Zhengxiang Gu, Leena Fadnis
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Publication number: 20100172974Abstract: Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques are disclosed.Type: ApplicationFiled: March 12, 2010Publication date: July 8, 2010Inventors: Benjamin Oshlack, Mark Chasin, Hua-Pin Huang
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Publication number: 20100168183Abstract: The present invention provides a substituted cyclic compound of the following general formula I or II: its preparation process and its use as a glucagon-like peptide-1 receptor regulator for preventing or treating metabolic disorders including, but not limited to, diabetes, insulin resistance and obesity, etc.Type: ApplicationFiled: June 21, 2006Publication date: July 1, 2010Applicant: Shanghai Institute of Materia Medica, Chinese Academy of ScienceInventors: Mingwei Wang, Na Li, Xin Xie, Qing Liu, Caihong Zhou, Fajun Nan
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Publication number: 20100143296Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100144852Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula (I) wherein A is an oxygen atom or group —N(R12)—; (i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group —R5, —Z—Y—R5—Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group —R5, —Z—Y—R5, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—CO—R5, or —Z—CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom toType: ApplicationFiled: August 8, 2006Publication date: June 10, 2010Applicant: ARGENTA DISCOVERY LIMITEDInventors: Harry Finch, Nicholas Charles Ray, Richard James Bull, Monique Bodil van Niel, Andrew Stephen Robert Jennings
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Publication number: 20100137417Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: ApplicationFiled: February 9, 2006Publication date: June 3, 2010Inventors: Mark Donald Chappell, Scott Eugene Conner, Allie Edward Tripp, Guoxin Zhu
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Publication number: 20100137402Abstract: The subject of the present invention is compounds corresponding to formula (I): Wherein X, R1, R2, R3 and R4 are as described herein. The invention also relates to a method for the preparation and application of said compounds as cannabinoid CB1 receptor antagonists.Type: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Applicant: SANOFI-AVENTISInventors: Jean-Philippe DUCOUX, Francis BARTH, Murielle RINALDI-CARMONA, Christian CONGY
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Publication number: 20100137347Abstract: Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.Type: ApplicationFiled: January 21, 2008Publication date: June 3, 2010Applicant: ALLERGAN, INC.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Patent number: 7723378Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds particularly as immunosuppressant agents.Type: GrantFiled: March 20, 2006Date of Patent: May 25, 2010Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Jörg Velker, Thomas Weller
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Publication number: 20100113423Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: October 19, 2009Publication date: May 6, 2010Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Publication number: 20100113477Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: October 20, 2009Publication date: May 6, 2010Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20100099752Abstract: The present invention relates to pharmaceutical compositions containing bicyclic type compounds and to methods of using same, for example, in the treatment or prevention of anxiety, mania, depression, disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse, Parkinson's Disease, psychosis, migraine and/or cerebral ischaemia.Type: ApplicationFiled: June 17, 2009Publication date: April 22, 2010Applicant: SmithKline Beecham plc.Inventors: Wai Ngor Chan, John Morris Evans, Geoffrey Stemp, Neil Upton, Robert Nicholas Willette
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Patent number: 7700643Abstract: The invention relates to novel polymerisable thieno[3,2-b]thiophenes, to their use as semiconductors or charge transport materials, in optical, electro-optical or electronic devices like for example liquid, crystal displays, optical films, organic field effect transistors (FET or OFET) for thin film transistor liquid crystal displays and integrated circuit devices such as RFID tags, electroluminescent devices in flat panel displays, and in photovoltaic and sensor devices, and to field effect transistors, light emitting devices or ID tags comprising the novel compounds.Type: GrantFiled: May 13, 2005Date of Patent: April 20, 2010Assignee: Merck Patent GmbHInventors: Martin Heeney, Weimin Zhang, Iain McCulloch
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Patent number: 7687491Abstract: A compound having immunosuppressive activity with low toxicity or a pharmacological salt thereof.Type: GrantFiled: October 19, 2007Date of Patent: March 30, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Takahide Nishi, Tsuyoshi Nakamura, Yukiko Sekiguchi, Yumiko Mizuno, Takaichi Shimozato, Futoshi Nara
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Publication number: 20100076066Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: ApplicationFiled: March 14, 2008Publication date: March 25, 2010Inventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller
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Patent number: 7678790Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 23, 2005Date of Patent: March 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
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Patent number: 7674815Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: January 29, 2007Date of Patent: March 9, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Christoph Faeh, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Philippe Pflieger
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Patent number: 7671083Abstract: This invention provides phenylene-thiophene compounds that exhibit useful electronic properties such as high mobility and high on/off ratio. The invention also provides electronic devices incorporating these compounds. These devices include field effect transistors (FETs), thin film transistors (TFTs), display devices, light-emitting diodes, photovoltaic cells, photo-detectors, and memory cells. Further, the invention also describes a method for manufacturing these field effect transistors. The invention describes an electronic device comprising one or more compounds represented by Formula: (I) where R is selected from substituents comprising 1-20 carbon atoms, wherein the substituents are selected from substituted or unsubstituted alkyl groups, substituted or unsubstituted alkenyl groups, and substituted or unsubstituted alkynyl groups; n is an integer selected from 2 through 6; and m and m? are integers selected independently from 1 through 3.Type: GrantFiled: August 23, 2005Date of Patent: March 2, 2010Assignee: E.I. du Pont de Nemours and CompanyInventor: Marc B. Goldfinger
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Patent number: 7666863Abstract: The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.Type: GrantFiled: May 24, 2007Date of Patent: February 23, 2010Assignees: ViroPharma Incorporated, WYETHInventors: Ashis K. Saha, Christopher J Burns, Alfred M. Del Vecchio, Thomas R. Bailey, Jason A. Reinhardt, Bheemashankar A. Kulkarni, Thomas H. Faitg, Hao Feng, Susan R. Rippin, Charles W. Blackledge, David J. Rys, Thomas A. Lessen, John Swestock, Yijun Deng, Theodore J. Nitz
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Publication number: 20100041730Abstract: This invention relates to novel macromolecular compositions having oxidation inhibition characteristics that are exhibited when added to organic material normally susceptible to oxidative degradation in the presence of air or oxygen, such a petroleum products, synthetic polymers, and elastomeric substances.Type: ApplicationFiled: October 17, 2007Publication date: February 18, 2010Inventors: Mahmood Sabahi, Vincent J. Gatto, Hassan Y. Elnagar
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Publication number: 20100035948Abstract: The present invention provides a compound of formula I and a compound of formula II, methods of use and formulations thereof.Type: ApplicationFiled: October 8, 2007Publication date: February 11, 2010Inventors: Naresh Kumar, George Iskander
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Publication number: 20100029752Abstract: A pharmaceutical composition containing a pharmaceutical diluent and a compound of formula II: wherein: R8?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —C(O)R4, where R4 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or —OH, —OR7 or —NR7, where R7 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R9=—OR5, —NR5, —NH—NH—R5 where R5 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl, optionally containing halogen atoms; R10?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or —CH2C(O)R6, where R6 is OR7 and NR7, where R7?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl and can optionally contain halogen atoms. Also included in the invention are methods of using the pharmaceutical compositions and the chemical compounds used in the compositions.Type: ApplicationFiled: July 26, 2006Publication date: February 4, 2010Inventors: Francis P. Kuhajda, Craig A. Townsend, Susan M. Medghalchi, Jill M. McFadden
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Patent number: 7645777Abstract: A switching device is discloses that exhibits two stable resistance values to a voltage applied between electrodes. The switching device comprises thin films of a first electrode layer, an organic bistable material layer and a second electrode layer sequentially formed on a substrate, and the organic bistable material is a specified quinone compound.Type: GrantFiled: November 20, 2006Date of Patent: January 12, 2010Assignee: Fuji Electric Holdings Co., Ltd.Inventors: Nobuyuki Sekine, Haruo Kawakami, Hisato Kato, Keisuke Yamashiro, Kyoko Kato, Masami Kuroda
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Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
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Patent number: 7642276Abstract: Compounds of formula (I): wherein A is a 5-membered heteroaryl ring are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38, such as rheumatoid arthritis.Type: GrantFiled: July 30, 2003Date of Patent: January 5, 2010Assignee: SmithKline Beecham CorporationInventors: Richard Martyn Angell, Ian Robert Baldwin, Paul Bamborough, Nigel Marc Deboeck, Timothy Longstaff, Stephen Swanson
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Publication number: 20090318543Abstract: Taxanes having an ethyl ester or cyclopropyl ester substituent at C(10), a keto substituent at C(9), a hydroxy substituent at C(7), a thienyl substituent at C(3?) and a cyclobutyloxycarbamate or cyclopentyloxycarbamate substituent at C(3?), pharmaceutical compositions comprising such taxanes, methods of treatment and administration, and methods of preparation of medicaments comprising the taxanes.Type: ApplicationFiled: March 24, 2009Publication date: December 24, 2009Applicant: FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION, INC.Inventors: Phong Vu, Robert A. Holton
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Publication number: 20090281171Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J, B, Y, G and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 6, 2009Publication date: November 12, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Publication number: 20090281145Abstract: The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.Type: ApplicationFiled: May 7, 2009Publication date: November 12, 2009Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
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Publication number: 20090274655Abstract: Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.Type: ApplicationFiled: November 15, 2007Publication date: November 5, 2009Inventors: Richard Martin Grimes, Charles David Hartley, Jacqueline Elizabeth Mordaunt, Pritom Shah, Martin John Slater, Gemma Victoria White
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Patent number: 7592337Abstract: Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.Type: GrantFiled: March 7, 2003Date of Patent: September 22, 2009Assignee: Merck & Co., Inc.Inventors: Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, Dehua Huang, Steve F. Poon, Thomas S. Reger, Jeffrey R. Roppe, Nicholas D. Smith
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Patent number: 7592467Abstract: The present invention relates to novel inhibitors of prolyl endopeptidase of formula (1) wherein I, A, X, Y and Z are specified in the description. The compounds are useful for the treatment of diseases such as mild cognitive impairment (MCI), Alzheimer's disease, Down Syndrome, Parkinson disease and Chorea Huntington.Type: GrantFiled: April 7, 2006Date of Patent: September 22, 2009Assignee: Probiodrug AGInventors: Andre Johannes Niestroj, Ulrich Heiser, Hans-Ulrich Demuth, Susanne Aust
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Patent number: 7589120Abstract: The invention relates to compounds of formula (I): Wherein X, R1, R2, R3 and R4 are as described herein. The invention also relates to a method for preparing the aforementioned compounds and to their therapeutic application.Type: GrantFiled: July 10, 2007Date of Patent: September 15, 2009Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Jean-Philippe Ducoux, Murielle Rinaldi-Carmona
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Patent number: 7589111Abstract: A taxane having a cyclopentyl ester substituent at C10, a keto substituent at C9, a hydroxy substituent at C2, a 2-thienyl substituent at C3? and an isopropoxycarbamate substituent at C3?.Type: GrantFiled: February 14, 2005Date of Patent: September 15, 2009Assignee: Florida State University Research Foundation, Inc.Inventors: Robert A. Holton, Phong Vu
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Patent number: 7585865Abstract: Methods of treating or preventing a disease or disorder in a subject are provided by the present invention which include administering a composition including a therapeutically effective amount of a protein kinase C (PKC) zeta inhibitor. A disease or disorder treated or prevented by administration of a PKC zeta inhibitor is characterized by abnormal vascular permeability. Diseases or disorders treated or prevented by administration of a composition including a therapeutically effective amount of a PKC zeta inhibitor include cancer, an ischemic condition and microvascular complications of a systemic or local condition in the subject, such as diabetes and/or diabetic macular edema. Additionally, methods of inhibiting PKC zeta are provided which include incubating PKC zeta in vivo, in vitro and/or in silico with a PKC zeta inhibitor.Type: GrantFiled: July 23, 2007Date of Patent: September 8, 2009Assignee: The Penn State Research FoundationInventors: David A. Antonetti, Jeffrey M. Sundstrom, Charles D. Smith
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Publication number: 20090221488Abstract: Disclosed inter alia is the use of certain chromenone derivatives, which are modulators of a mitotic kinesin such as KSP, in the treatment of cellular proliferative diseases. The chromenones derivatives are administered with another chemotherapeutic agent selected from neutropenia treatment agents, alkylating agents, antimetabolites, platinating agents, topoisomerase inhibitors, tubulin agents and signalling inhibitors (e.g., kinase inhibitors). Pharmaceutical compositions comprising one or both types of active agents are also disclosed.Type: ApplicationFiled: December 7, 2006Publication date: September 3, 2009Inventors: Kenneth W. Wood, Lisa Belmont
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Publication number: 20090221643Abstract: Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl and thienyl optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, cyano, C(O)C1-4alkyl, NHSO2C1-4alkyl, NMeSO2C1-4alkyl, NHCOC1-4alkyl, NMeCOC1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl and CO2C1-4alkyl, or two Y groups together form a cyclic group —O(CH2)O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.Type: ApplicationFiled: February 6, 2007Publication date: September 3, 2009Inventors: Kevin Michael Thewlis, Simon Edward Ward
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Patent number: 7579340Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.Type: GrantFiled: August 22, 2007Date of Patent: August 25, 2009Assignee: Pfizer IncInventors: Ronald Biediger, Jie Chen, Daxin Gao, Robert Market, Chengde Wu
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Patent number: 7569600Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: GrantFiled: May 15, 2006Date of Patent: August 4, 2009Assignee: ViroChem Pharma Inc.Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
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Publication number: 20090192179Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: February 26, 2009Publication date: July 30, 2009Inventors: Bing Wang, Jian Chen
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Publication number: 20090182033Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; formula (I) wherein R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group -R5 or a group, -Z-Y—R5, or a group -Z-NR9R10, or a group -Z-N(R9)C(O)R11; and R3 is a lone pair, or C1-C6-alkyl; R4 is selected from one of the groups of formula (a), (b), (c) or (d); formulae (a), (b), (c), (d), Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R5 is an C1-C6-alkyl, aryl, arylalkyl; aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R6 is C1-C6-alkyl or a hydrogen atom; R7a and R7b area C1-C6-alkyl group or halogen; n and m are independently 0, 1, 2 or 3; R8a and R8b are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl and hydrogen; R8c is —OH, C1-C6-alkyl, hydroxy-C1-C6-alkyl, or a hydrogen atom; R8d is C1-C6Type: ApplicationFiled: December 14, 2006Publication date: July 16, 2009Applicant: ARGENTA DISCOVERY LTD.Inventors: Harry Finch, Nicholas Charles Ray, Monique Bodil Van Niel, Phillip Smith
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Patent number: 7524863Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: June 21, 2006Date of Patent: April 28, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
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Patent number: 7524869Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: October 1, 2003Date of Patent: April 28, 2009Assignee: Florida State University Research Foundation, Inc.Inventor: Robert A. Holton
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Publication number: 20090105286Abstract: The invention relates to drugs and the use thereof, wherein said drugs contain compounds selected from a group comprising general formulas (1), (2), (3) and (4) and/or enantiomers, diastereomers or the pharmaceutically acceptable salts thereof. Said drugs are used for treating autoimmune and tumoral diseases and/or for immunosuppresion.Type: ApplicationFiled: November 18, 2005Publication date: April 23, 2009Applicant: Rheinische Friedrich-Wilhelms UniversitatInventors: Michael Famulok, Waldemar Kolanus, Markus Hafner, Imke Grune, Barbara Tappertzhofen, Mirko Theis
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Patent number: 7521473Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.Type: GrantFiled: February 23, 2005Date of Patent: April 21, 2009Assignee: WyethInventors: Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Bruce C. Follows, Steven J. Kirincich, Michael J. Smith, Jun-Jun Wu, Kenneth W. Foreman, David V. Erbe, Yan-Ling Zhang, Weixin Xu, Steve Y. Tam
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Publication number: 20090093521Abstract: Synthesis of 2,5-bis-diamine-[1,4]benzoquinonic derivatives having the general formula (I), products and intermediates of said synthesis; the synthesis involves the use of p-benzoquinones having the general formula (IX) and diamines having the general formula (XI).Type: ApplicationFiled: June 13, 2005Publication date: April 9, 2009Inventors: Maria Laura Bolognesi, Rita Banzi, Anna Minarini, Carlo Melchiorre
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Patent number: 7507761Abstract: The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof.Type: GrantFiled: January 21, 2005Date of Patent: March 24, 2009Assignees: Universite de Liege, Universite Libre de BruxellesInventors: Sophie Sebille, Bernard Pirotte, Stéphane Boverie, Pascal De Tullio, Philippe Lebrun, Marie-Hélène Antoine
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Patent number: 7507754Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: August 14, 2007Date of Patent: March 24, 2009Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Publication number: 20090076012Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2.Type: ApplicationFiled: December 28, 2007Publication date: March 19, 2009Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20090069382Abstract: There is provided a compound of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: ApplicationFiled: April 12, 2006Publication date: March 12, 2009Inventors: Mathias Alterman, Anders Hallberg, Murugaiah Andappan Murugaiah Subbaiah