Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/447)
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Patent number: 7709523Abstract: ?-Aminoamide derivatives useful as antimigraine agents, particularly for the treatment of head pain conditions such as migraine, cluster headache or other severe headache, are disclosed. The antimigraine agents of the invention are able to reduce or even stop the pain deriving from such conditions without, virtually, any side effects.Type: GrantFiled: November 18, 2003Date of Patent: May 4, 2010Assignee: Newron Pharmaceuticals SpAInventors: Patricia Salvati, Marcello Calabresi, Luciano Dho, Orietta Veneroni, Piero Melloni
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Publication number: 20100093775Abstract: 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: ApplicationFiled: July 24, 2009Publication date: April 15, 2010Applicant: VIROCHEM PHARMA INC.Inventors: Real DENIS, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constatin G. Yannopoulos, Laval Chan Chun Kong
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Patent number: 7696225Abstract: Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.Type: GrantFiled: October 26, 2004Date of Patent: April 13, 2010Assignee: OSI Pharmaceuticals, Inc.Inventors: Jason Bloxham, Andrew Phillip Crew, Ayako Honda, An-Hu Li, Bijoy Panicker, Graham Michael Wynne, Lawrence Tardibono, Jr.
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Patent number: 7696244Abstract: The invention provides compositions, including pharmaceutical preparations, which comprise one or more substituted thiophene, benzofuran, pyrimidinetrione, dihydropyridine, tetrahydrocarbazol or anthraquinone compounds. The invention also features methods of use of such compositions in increasing activity of mutant-cystic fibrosis transmembrane conductance regulator protein in a cell, e.g. by increasing ion transport in a mutant-CFTR.Type: GrantFiled: May 14, 2004Date of Patent: April 13, 2010Assignee: The Regents of the University of CaliforniaInventors: Alan Verkman, Luis J. V. Galietta, R. Kiplin Guy
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Publication number: 20100087515Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O)—, —S(?P)2-, —C(?O)O—, —C(?O)NR3-, —C(?S)—NR3, —C(?NH)—NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.Type: ApplicationFiled: October 29, 2007Publication date: April 8, 2010Applicant: Chroma Terapeutics LtdInventors: David Festus Charles Moffat, Stephen John Davies, Michael Hugh Charlton, Simon Christopher Hirst, Stuart Thomas Onions, Jonathan Gareth Williams
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Publication number: 20100069473Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- whereinType: ApplicationFiled: October 29, 2007Publication date: March 18, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Festus Charles Moffat, Stephen John Davies, Michael Hugh Charlton, Simon Christopher Hirst, Stuart Thomas Onions, Jonathon Gareth Williams
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Publication number: 20100063088Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20100063065Abstract: The invention discloses compounds of formula (I); wherein: R is a carboxylic acid or a derivative thereof; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, halo or trihalomethyl; R2 is aryl, heteroaryl, arylalkyl or heteroarylalkyl; R3 is H or F; and L is a linking group comprising a chain of from 2 to 8 atoms linking R and the carbonyl group (A); and pharmaceutically acceptable derivatives thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype ? (PPAR?). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.Type: ApplicationFiled: September 28, 2006Publication date: March 11, 2010Applicant: Inpharmatica LimitedInventors: Andrew Ayscough, David Rodyney Owen, Paul Meo, David James Pearson, Yvonne Walker, Richard Justin Boyce, Fabio Zuccotto
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Publication number: 20100041657Abstract: The present invention relates to compounds of formula I, in which at least one of R5, R6 and R7 is SR12, S(O)R12 or S(O)2R12 group where R12 is a C1-6haloalkyl group, that act, as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.Type: ApplicationFiled: May 11, 2006Publication date: February 18, 2010Applicant: NOVO NORDICK A/SInventors: Preben Houlberg Olesen, Holger Claus Hansen, Lise Brown Christiansen, Flemming Elmelund Nielsen, Anders Klarskov Petersen
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Publication number: 20100029753Abstract: Provided are compounds that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of CCR9 receptor activity.Type: ApplicationFiled: July 30, 2008Publication date: February 4, 2010Inventors: Eric C. Anderson, Ronald J. Biediger, Jie Chen, Brian Dupre, Pedro Lory, Robert V. Market, Keith A. Monk, Michael M. Savage, Reginald Tennyson, Brandon M. Young
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Publication number: 20100029754Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 7, 2009Publication date: February 4, 2010Applicant: ASTRAZENECA ABInventors: Alan Wellington Faull, Craig Johnstone, Andrew David Morley, Jeffrey Philip Poyser
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Publication number: 20100022525Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: October 4, 2007Publication date: January 28, 2010Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Patent number: 7652064Abstract: The present invention relates to AMPA receptor potentiators of Formula I: formulations comprising them, methods for their use, and intermediates useful for their preparation.Type: GrantFiled: June 6, 2006Date of Patent: January 26, 2010Assignee: Eli Lilly and CompanyInventor: Esteban Dominguez-Manzanares
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Publication number: 20090318462Abstract: 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: ApplicationFiled: August 18, 2009Publication date: December 24, 2009Applicant: The Penn State Research FoundationInventors: David A. Antonetti, Jeffrey M. Sundstrom, Charles D. Smith
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Publication number: 20090312706Abstract: Described herein are transdermal delivery devices composed of at least one resealable injection port and at least one local anesthetic reservoir. The device effectively delivers anesthetic to the skin of the subject prior to puncturing the skin by syringes, needle sticks, or other instruments intended to be inserted into the skin. In addition, this device can be used to deliver various therapeutic agents for either locally or systemically.Type: ApplicationFiled: April 16, 2009Publication date: December 17, 2009Inventors: Totada Shantha, Jessica Shantha, Erica Shantha, Lauren Shantha
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Publication number: 20090306003Abstract: An improved pesticide delivery system is disclosed. The system is based on a microblend comprising (a) an amphophilic compound containing at least one hydrophilic group and at least one hydrophobic group and (b) a second compound. Compositions based on the microblend and methods of using the compositions to control pests are also disclosed.Type: ApplicationFiled: January 10, 2007Publication date: December 10, 2009Applicant: Innovation Technologies, LLCInventors: Alexander V. Kabanov, Tatiana K. Bronitch, Michael Karas, Bruce L. Frank
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Patent number: 7625914Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: GrantFiled: December 20, 2005Date of Patent: December 1, 2009Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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Publication number: 20090292010Abstract: The present invention provides compositions comprising sucralose and 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one or salts, solvates, and/or esters thereof and methods of making the compositions by spray drying. The present invention also provides ingestible compositions comprising compositions of the present invention and methods of making such foods. The present invention also includes a process of preparing 2-amino-thiophene derivatives, which are key intermediates for preparing 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one.Type: ApplicationFiled: February 6, 2009Publication date: November 26, 2009Inventors: Rhondi Shigemura, Carolyn Podgurski, Boriruck Kitisin, Maria Suparno, Jennifer Ward, Thitiwan Lebien, Kevin Wirtz, James Robert Zeller
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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: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090214631Abstract: A process for the preparation of strontium ranelate or a hydrate thereof is provided comprising (a) reacting a tetraester compound of Formula II: wherein R, R1, R2, and R3 are independently a linear or branched C1-C6 alkyl group or a substituted or unsubstituted C3-C12 cyclic group, in the presence of a lithium base and in a solvent with an inorganic acid salt of strontium.Type: ApplicationFiled: August 18, 2006Publication date: August 27, 2009Inventors: Bobba Venkata Siva Kumar, Kosampally Srinivas, Sanjay Anantha Kale, Nitin Sharad Chandra Pradhan
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Publication number: 20090215829Abstract: The invention relates to thiophene carboxamides of formula (I), wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 4, 2009Publication date: August 27, 2009Inventors: Andrew David Morley, Jeffrey Philip POYSER
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Patent number: 7576117Abstract: A medicine containing, as an active ingredient, a cyclic amine derivative represented by the following formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1 to C6 alkyl addition salt thereof. The medicine has an action for treating or preventing diseases in which CCR3 participates, such as asthma and allergic rhinitis.Type: GrantFiled: August 4, 2000Date of Patent: August 18, 2009Assignee: Teijin LimitedInventors: Tatsuki Shiota, Masaki Sudoh, Tomonori Yokoyama, Yumiko Muroga, Takashi Kamimura, Akinobu Nakanishi
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Patent number: 7572826Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: January 13, 2004Date of Patent: August 11, 2009Assignee: AstraZeneca ABInventors: Alan Wellington Faull, Craig Johnstone, Andrew David Morley, Jeffrey Philip Poyser
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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: 20090181962Abstract: The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2, and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 3, 2007Publication date: July 16, 2009Inventors: Andrew Baxter, Stephen Brough, Alan Faull, Craig Johnstone, Thomas Mcinally
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Publication number: 20090170891Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 6, 2007Publication date: July 2, 2009Inventors: Steven L. Colletti, James R. Tata, Weichun Chen, Richard T. Beresis, Fa-Xiang Ding, Darby Rye Schmidt, Hong Shen, Subharekha Raghavan
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Patent number: 7553868Abstract: The invention relates to thiophene carboxamides of formula (I) wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: January 13, 2004Date of Patent: June 30, 2009Assignee: AstraZeneca ABInventors: Andrew David Morley, Jeffrey Philip Poyser
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Patent number: 7544710Abstract: The present invention relates to the use of the distrontium salt of 2-[N,N-di(carboxymethyl)amino]-3-cyano-4-carboxymethyl-thiophene-5-carboxylic acid in obtaining medicaments intended for the treatment of gastro-duodenal pain.Type: GrantFiled: November 4, 2003Date of Patent: June 9, 2009Assignee: Les Laboratoires ServierInventor: Yannis Tsouderos
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Patent number: 7541379Abstract: The present invention relates to di(amido-substituted)-heteroarene compounds and their use as osteoblastogenesis agents. The invention provides a method for inducing osteogenesis in a precursor cell capable of undergoing osteogenesis.Type: GrantFiled: October 10, 2006Date of Patent: June 2, 2009Assignee: The University of Hong KongInventors: Chi Ming Che, Annie Wai-Chee Kung
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Publication number: 20090137659Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 15, 2008Publication date: May 28, 2009Applicant: CALCIMEDICA, INC.Inventors: Gonul VELICELEBI, Kenneth A. STAUDERMAN, David P.M. PLEYNET, Song CHENG, Jeffrey P. WHITTEN
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Publication number: 20090093669Abstract: A method and apparatus for administering drugs through a dermal or mucosal layer such that the treatment device may be applied to the mammal for the transdermal or transmucosal administration of various drugs, pharmaceuticals, salts and prodrugs thereof is taught herein. The magnetic device has at least one magnet to provide an effective magnetic sphere of influence of the magnetic field at the desired site of action. The tissue-permeable drug formulation is positioned on the site of action and the magnetic device is positioned adjacent to tissue-permeable drug formulation wherein the magnetic sphere of influence of the magnetic field moves the drug through the dermal or mucosal layer by interaction with the magnetic moment (induced or permanent) of the drug sufficient to increase the movement of the drug beyond the movement caused by diffusion alone.Type: ApplicationFiled: October 3, 2008Publication date: April 9, 2009Inventors: WILLIAM A. FARONE, W. BRADLEY WORTHINGTON
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Publication number: 20090054396Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: ApplicationFiled: September 8, 2008Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Mei Su, Dingwei Yu, Stephanie Springer
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Publication number: 20090041747Abstract: The invention relates to novel compounds with formula (I) and their use in stabilization of Factor VIIa or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.Type: ApplicationFiled: February 24, 2006Publication date: February 12, 2009Applicant: NOVO NORDISK HEALTH CARE AGInventors: Anders Klarskov Petersen, Andrew Neil Bowler
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Publication number: 20080312314Abstract: Alpha crystalline form of strontium ranelate of formula (I): characterised by its powder X-ray diffraction diagram and by a water content of from 22 to 24%. Medicinal products containing the same which are useful in the treatment of osteoporosis and arthrosis.Type: ApplicationFiled: August 12, 2008Publication date: December 18, 2008Applicant: LES LABORATOIRES SERVIERInventors: Stephane Horvath, Isabelle Demuynck, Gerard Damien
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Publication number: 20080299080Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: November 15, 2007Publication date: December 4, 2008Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson, Constantin G. Yannopoulos, Guy Falardeau, Louis Vaillancourt, Real Denis
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Publication number: 20080300281Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: July 28, 2008Publication date: December 4, 2008Inventors: Jacques Dumas, Uday Khire, Timothy B. Lowinger, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, Holia Hatoum-Mokdad, Jeffrey Johnson, Aniko Redman, Robert Sibley
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Publication number: 20080261952Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
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Publication number: 20080255095Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.Type: ApplicationFiled: June 18, 2007Publication date: October 16, 2008Applicant: BTG INTERNATIONAL LIMITEDInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
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Publication number: 20080241243Abstract: The invention relates to a drug delivery device for providing local analgesia, local anesthesia or nerve blockade at a site in a human or animal in need thereof, the device comprising a fibrillar collagen matrix; and at least one drug substance selected from the group consisting of amino amide anesthetics, amino ester anesthetics and mixtures thereof, the at least one drug substance being substantially homogeneously dispersed in the collagen matrix, and the at least one drug substance being present in an amount sufficient to provide a duration of local analgesia, local anesthesia or nerve blockade which lasts for at least about one day after administration.Type: ApplicationFiled: March 28, 2007Publication date: October 2, 2008Inventors: Michael Myers, Philip Wallace Reginald
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Publication number: 20080241245Abstract: The invention relates to a drug delivery device for providing local analgesia, local anesthesia or nerve blockade at a site in a human or animal in need thereof, the device comprising a fibrillar collagen matrix; and at least one drug substance selected from the group consisting of amino amide anesthetics, amino ester anesthetics and mixtures thereof, the at least one drug substance being substantially homogeneously dispersed in the collagen matrix, and the at least one drug substance being present in an amount sufficient to provide a duration of local analgesia, local anesthesia or nerve blockade which lasts for at least about one day after administration.Type: ApplicationFiled: March 28, 2008Publication date: October 2, 2008Inventors: Michael Myers, Philip Wallace Reginald
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Patent number: 7423061Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: GrantFiled: August 12, 2004Date of Patent: September 9, 2008Assignee: AstraZeneca ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Stephanie Springer, Mei Su, Dingwei Yu
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Patent number: 7417057Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, —, where R,R,R 6, R 7, R8, R I1, R R 13, R 14, and X are described.Type: GrantFiled: April 28, 2003Date of Patent: August 26, 2008Assignee: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Publication number: 20080200468Abstract: Therapeutically active heteroaryl carboxylic acid derivatives of Formula (I) wherein R1, R2, W, X, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.Type: ApplicationFiled: February 14, 2006Publication date: August 21, 2008Inventors: Juliet Kay Simpson, Ivan Leo Pinto
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Publication number: 20080193464Abstract: The present invention discloses the identification of a human autism susceptibility gene, which can be used for the diagnosis, prevention and treatment of autism and related disorders, as well as for the screening of therapeutically active drugs. The invention more specifically discloses that the PRKCB1 gene of chromosome 16 and certain alleles thereof are related to susceptibility to autism and represent novel targets for therapeutic intervention. The present invention relates to particular mutations in the PRKCB1 gene and expression products, as well as to diagnostic tools and kits based on these mutations.Type: ApplicationFiled: June 30, 2005Publication date: August 14, 2008Inventors: Anne Philippi, Francis Rousseau, Peter Brooks, Jorg Hager
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Patent number: 7402608Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.Type: GrantFiled: December 9, 2003Date of Patent: July 22, 2008Assignee: ViroChem Pharma Inc.Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Oswy Z. Pereira, Carl Poisson, Melanie Proulx, Thumkunta Jagadeeswar Reddy, Zhang Ming-Qiang
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Patent number: 7393868Abstract: The present invention relates to AMPA receptor potentiators of Formula I: formulations comprising them, methods for their use, and intermediates useful for their preparation.Type: GrantFiled: June 5, 2006Date of Patent: July 1, 2008Assignee: Eli Lilly and CompanyInventors: Ana Maria Castano Mansanet, Frederic Laurent Cordier, Esteban Dominguez-Manzanares, Jian Eric Hong, William Joseph Hornback, Delu Jiang
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Patent number: 7388012Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.Type: GrantFiled: September 15, 2005Date of Patent: June 17, 2008Assignee: OSI Pharmaceuticals, Inc.Inventors: Andrew Crew, An-Hu Li, Hanqing Dong, Tao Zhang
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Publication number: 20080125432Abstract: The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula I, II, III or IV, stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.Type: ApplicationFiled: December 1, 2005Publication date: May 29, 2008Applicant: Devgen NVInventors: Petra Blom, Jan Octaaf De Kerpel, Eric Pierre Paul Rene Fourmaintraux, Titus Jan Kaletta, Dirk Leysen
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal