Cyano Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/344)
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Publication number: 20100297046Abstract: The invention relates to compounds and methods for inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin, by way of fructosamine-3-kinase inhibition, thereby treating or prevention various diseases, disorders or conditions. Additionally, the invention relates to treatment of various diseases, disorders or conditions associated with or mediated by oxidative stress since 3DG induces ROS and AGEs, which are associated with the inflammatory response caused by oxidative stress.Type: ApplicationFiled: March 30, 2007Publication date: November 25, 2010Applicant: DYNAMIS THERAPEUTICS, INC.Inventors: Michael Schwartz, Francis Kappler, Bangying Su
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Patent number: 7816389Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: GrantFiled: January 11, 2007Date of Patent: October 19, 2010Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
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Patent number: 7816353Abstract: Compounds of formula III: wherein R5a, R3, X, Y, Q, R1a and R1b are as defined in the specification, pharmaceutically acceptable salts thereof, and methods of use thereof.Type: GrantFiled: October 22, 2004Date of Patent: October 19, 2010Assignee: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu
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Publication number: 20100261763Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alky groups, and optionally having hydroxyl and/or alkoxyl groups substituents.Type: ApplicationFiled: June 14, 2010Publication date: October 14, 2010Inventors: Helen E. BLACKWELL, Matthew D. BOWMAN, Jennifer C. O'NEILL, Joseph R. STRINGER
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Publication number: 20100256149Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 14, 2010Publication date: October 7, 2010Applicant: MERCK SERONO S.A.Inventors: Andreas Goutopoulos, Benny C. Askew, JR., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu
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Publication number: 20100247636Abstract: The present invention provides a composition comprising nilvadipine, or a salt, derivative, prodrug, or polymorph thereof, useful in the treatment and prevention of hypertension or related cardiovascular disorders. In one embodiment, the composition comprises nanoparticulate particles comprising nilvadipine, or a salt, derivative, prodrug, or polymorph thereof, and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. In another embodiment, the composition comprises a modified release composition that, upon administration to a patient, delivers nilvadipine, or a salt, derivative, prodrug, or polymorph thereof, in a bimodal, multimodal or continuous manner. The invention also relates to dosage forms containing such compositions, and to methods for the treatment and prevention of hypertension or related cardiovascular disorders.Type: ApplicationFiled: June 30, 2006Publication date: September 30, 2010Applicant: Elan Corporation, plcInventors: John G. Devane, Paul Stark, Niall M.M. Fanning, Gurvinder Singh Rekhi, Scott A. Jenkins, Gary Liversidge
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Patent number: 7786148Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and a compound capable of inhibiting the transport of electrons of the respiratory chain in phytopathogenic fungal organisms (b) in a (a)/(b) weight ratio of from 0.01 to 20. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the phytopathogenic fungi of crops by using this composition.Type: GrantFiled: February 10, 2005Date of Patent: August 31, 2010Assignee: Bayer Cropscience S.A.Inventors: Jean-Marie Gouot, Marie-Claire Grosjean-Cournoyer
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Patent number: 7786172Abstract: A method of treatment comprises administering 4-hydroxy tamoxifen percutaneously to a patient having mastalgia. The 4-hydroxy tamoxifen may be formulated in a hydroalcoholic gel or an alcoholic solution.Type: GrantFiled: December 15, 2003Date of Patent: August 31, 2010Assignee: Laboratories Besins InternationalInventors: Bruno de Lignières, Gabrielle Elisabeth Brink de Lignières, legal representative
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Patent number: 7781436Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: GrantFiled: July 25, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7776892Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I)(a) and a compound capable of inhibiting the spores germination or mycelium growth by acting on different metabolic routes (b) in a (a)/(b) weight ratio of from 0.01 to 20. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the phytopathogenic fungi of crops by using this composition.Type: GrantFiled: February 10, 2005Date of Patent: August 17, 2010Assignee: Bayer Cropscience S.A.Inventors: Marie-Claire Grosjean-Cournoyer, Jean-Marie Gouot
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Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20100197739Abstract: The present invention is directed to an insecticidal water based suspension concentrate formulation comprising a water-soluble insecticide selected from the group consisting of N-cyanomethyl-4-(trifluoromethyl)nicotinamide and (EZ)-1-(6-chloro-3-pyridylmethyl)-N-nitroimidazolidin-2-ylidineamine and at least one water-soluble salt selected from the group consisting of magnesium sulfate (hydrated and anhydrous forms) and sodium sulfate, wherein the water-soluble insecticide is present in an insecticidally effective amount and methods of use.Type: ApplicationFiled: October 16, 2007Publication date: August 5, 2010Applicant: FMC CORPORATIONInventors: Robin W. Dexter, Hong Liu
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Pharmaceutical compositions for reducing amyloid deposition, amyloid neurotoxicity, and microgliosis
Publication number: 20100183711Abstract: The present invention provides methods for reducing A? deposition, A? neurotoxicity and microgliosis in an animal or human afflicted with a cerebral amyloidogenic disease, such as Alzheimer's disease (AD), by administering therapeutically effective amounts of the (R)-enantiomer of the dihydropyridine compound nilvadipine, also known as (?)-nilvadipine, to the animal or human. Further provided are methods for reducing the risk of A? deposition, A? neurotoxicity and microgliosis in animals or humans suffering from traumatic brain injury by administering (?)-nilvadipine after the traumatic brain injury and continuing treatment for a prescribed period of time thereafter.Type: ApplicationFiled: February 1, 2010Publication date: July 22, 2010Inventors: Michael J. Mullan, Daniel Paris, Robert A. Ivey, III -
Publication number: 20100173886Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.Type: ApplicationFiled: May 22, 2008Publication date: July 8, 2010Inventors: Jason Bloxham, Stuart Edward Bradley, Tom Banksia Dupree, Peter Timothy Fry, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John Stewart
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Publication number: 20100166655Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: ApplicationFiled: March 15, 2007Publication date: July 1, 2010Applicants: JANSSEN PHARMACEUTICA N.V., ADDEX PHARMACEUTICALS S.A.Inventors: Hassan Julien Imogai, Vincent Mutel, Jose Maria Cid-Nunez, Jose Ignacio Andres-Gil, Andres Avelino Trabanco-Suarez, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Gregor James MaCdonald, Shirley Elizabeth Pullan, Robert Johannes Lutjens, Guillaume Albert Jacques Duvey, Vanthea Nhem, Terry Palrick Finn, Gagik Melikyan
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Publication number: 20100152207Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: June 17, 2010Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
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Patent number: 7737164Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alky groups, and optionally having hydroxyl and/or alkoxyl groups substituents.Type: GrantFiled: May 16, 2007Date of Patent: June 15, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Helen E. Blackwell, Matthew D. Bowman, Jennifer C. O'Neill, Joseph R. Stringer
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Patent number: 7723364Abstract: Compound of general formula (I): Process for preparing this compound. Fungicidal composition comprising a compound of general formula (I). Method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: July 19, 2004Date of Patent: May 25, 2010Assignee: Bayer Cropscience SAInventors: Darren James Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier, Isabelle Christian
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Patent number: 7700632Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.Type: GrantFiled: January 8, 2008Date of Patent: April 20, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Chang An Chu, Paul Gillespie, Jefferson Wright Tilley
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Patent number: 7691854Abstract: The invention relates to novel dihydropyridine derivatives, of Formula (I) processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: August 18, 2003Date of Patent: April 6, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 7629365Abstract: 3-Chloro-6-(hydroxymethyl)-2-methyl-5-[4-({4-[(trifluoromethyl)oxy]phenyl}oxy)phenyl]-4(1H)-pyridinone, having the following formula: is described along with its pharmaceutically acceptable salts, processes for its preparation, pharmaceutical formulations thereof and its uses in treatment of certain parasitic infections such as malaria.Type: GrantFiled: May 31, 2007Date of Patent: December 8, 2009Assignee: Glaxo Group LimitedInventors: Jose Maria Bueno Calderon, Jesus Chicharro Gonzalo, M Pilar Manzano Chinchon
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Publication number: 20090298872Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorder associated with the activation of steroid hormone nuclear receptors.Type: ApplicationFiled: December 13, 2005Publication date: December 3, 2009Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, John Wityak
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Patent number: 7625949Abstract: The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein.Type: GrantFiled: April 22, 2005Date of Patent: December 1, 2009Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Donald Roy Hirschfeld, Tania Silva, Zachary Kevin Sweeney, Harit Vora
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Publication number: 20090270423Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.Type: ApplicationFiled: March 27, 2009Publication date: October 29, 2009Inventors: Helen E. Blackwell, Matthew D. Bowman, Joseph R. Stringer
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Publication number: 20090156646Abstract: The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula: or a salt thereof, a prodrug thereof, and a pharmaceutical agent containing the same; wherein Ring A represents a 5- to 8-membered homocyclic or heterocyclic group optionally having a substituent other than formula —X-R1 wherein X represents a bond or a spacer, and R1 represents optionally substituted amino or an optionally substituted nitrogen-containing heterocyclic group; Ring B represents an optionally substituted benzene ring; R2 represents an optionally substituted homocyclic or heterocyclic group; and R3 and R4 independently represent a hydrogen atom, cyano, acyl or an optionally substituted hydrocarbon group.Type: ApplicationFiled: August 10, 2006Publication date: June 18, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Satoshi Sasaki, Atsuo Baba
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Publication number: 20090118338Abstract: 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: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
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Publication number: 20090092667Abstract: The present invention provides methods for reducing A? deposition, A? neurotoxicity and microgliosis in an animal or human afflicted with a cerebral amyloidogenic disease, such as Alzheimer's disease (AD), by administering therapeutically effective amounts of the (R)-enantiomer of the dihydropyridine compound nilvadipine, also known as (?)-nilvadipine, to the animal or human. Further provided are methods for reducing the risk of A? deposition, A? neurotoxicity and microgliosis in animals or humans suffering from traumatic brain injury by administering (?)-nilvadipine after the traumatic brain injury and continuing treatment for a prescribed period of time thereafter.Type: ApplicationFiled: October 3, 2008Publication date: April 9, 2009Applicant: ROSKAMP RESEARCH LLCInventors: Michael J. MULLAN, Daniel PARIS, Robert A. IVEY, III
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Patent number: 7507769Abstract: The present invention provides methods for treating and preventing benign breast disease by administering 4-hydroxy tamoxifen to a patient. When percutaneously administered to a patient's breasts, 4-hydroxy tamoxifen concentrates locally, and exerts an anti-estrogenic effect. In patients with benign breast disease, this effect induces disease regression. In patients at risk for developing breast cancer, the anti-estrogenic effect prevents formation of benign breast conditions that can lead to cancer.Type: GrantFiled: March 22, 2004Date of Patent: March 24, 2009Assignee: Laboratoires Besins InternationalInventor: Elisabeth Le Nestour
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Patent number: 7504421Abstract: The invention relates to compounds of general formula (I), a method for the production thereof and the use thereof as pharmacologically effective substances for a broad medical indication spectrum. Furthermore, selective adenosine receptor ligands, preferably selective adenosine A1-, adenosine A2a- and/or adenosine A2b-receptor ligands are provided for the prophylaxis and/or the treatment of diseases, especially cardiovascular diseases, diseases of the urogenital region, diseases of the respiratory tract, inflammatory and neuroinflammatory diseases, diabetes, especially pancreatic diabetes, neurodegenerative diseases, pain states, cancer as well as liver fibrosis and liver cirrhosis.Type: GrantFiled: February 21, 2006Date of Patent: March 17, 2009Inventors: Ulrich Rosentreter, Rolf Henning, Marcus Bauser, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Klaus Dembowsky, Olga Salcher-Schraufstatter, Johannes-Peter Stasch, Thomas Krahn, Elisabeth Perzborn
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Patent number: 7485653Abstract: The present invention provides certain substituted 1,4-dihydropyridine compounds, including pure enantiomeric forms and pharmaceutical formulations thereof. These compounds provide for elevation of ?-MyHC protein levels and ?-MyHC mRNA levels, and most frequently these same compounds provide simultaneous lowering of ?-MyHC protein levels and ?-MyHC mRNA levels. Thus, these compounds may be used alone or in conjunction with other drugs to treat heart failure.Type: GrantFiled: November 3, 2004Date of Patent: February 3, 2009Assignee: Gilead Sciences, Inc.Inventors: Kathy Schreiber, Larry Melvin
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Publication number: 20090012061Abstract: The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: ApplicationFiled: September 9, 2005Publication date: January 8, 2009Inventors: Timothy A. Blizzard, Carolyn A. Buser-Doepner, Douglas E. Frantz, Kelly Hamilton, Myle Hoang, Ling Lee, Christopher R. Moyes, Jerry A. Murry, Arash Soheili
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Publication number: 20080293687Abstract: The invention concerns benzamide compounds of Formula (I), wherein R1a, R1b, R1c, R2, R3, R4, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).Type: ApplicationFiled: August 31, 2005Publication date: November 27, 2008Inventors: Keith Hopkinson Gibson, Elaine Sophie Elizabeth Stokes, Michael James Waring, David Michael Andrews, Zbigniew Stanley Matusiak, Mark Andrew Graham
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Patent number: 7446117Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.Type: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
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Patent number: 7435743Abstract: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 30, 2005Date of Patent: October 14, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshiro, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuiyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Publication number: 20080249133Abstract: The present invention relates to the use of substituted 2-thio-3,5-dicyano-4-phenyl-6-amino-pyridines of the formula (I) for production of a medicament for the prophylaxis and/or treatment of nausea and vomiting.Type: ApplicationFiled: June 23, 2005Publication date: October 9, 2008Applicant: Bayer Healthcare AGInventors: Thomas Krahn, Wolfgang Thielemann, Ulrich Rosentreter, Nicole Diedrichs, Thomas Kramer
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Patent number: 7414055Abstract: The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 20, 2004Date of Patent: August 19, 2008Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Craig W. Lindsley, Zhicai Wu, Zhijian Zhao, John C. Hartnett
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Patent number: 7410986Abstract: 4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy, amino, carboxy, etc.; R6 is hydrogen, carbamoyl, cyano, carboxy, C1-6 alkoxycarbonyl, etc. and R7 is amino or C1-6 alkanoylamino. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and the like.Type: GrantFiled: November 19, 2001Date of Patent: August 12, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Sachiko Sasaki, Takashi Yoshino, Yuka Ikegami, Tsutomu Masuda, Mitsuyuki Shimada, Takuya Shintani, Makoto Shimazaki, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Masaomi Umeda, Hiroshi Komura, Nagahiro Yoshida
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Publication number: 20080176833Abstract: This invention provides novel dihydropyridine derivatives of the formula I having protein tyrosine kinase inhibitory activity, to process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions.Type: ApplicationFiled: December 13, 2007Publication date: July 24, 2008Inventors: Marc Adler, Stefan Baeurle, Judi Bryant, Ming Chen, Yuo-Ling Chou, Paul Hrvatin, Seock-Kyu Khim, Monica Kochanny, Wheeseong Lee, Michael Mamounas, Janet Meurer Ogden, Gary Bruce Phillips, Victor Selchau, Christopher West, Bin Ye, Shendong Yuan, Martin Krueger
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Publication number: 20080132545Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: July 31, 2007Publication date: June 5, 2008Inventors: Pu-Ping Lu, Xiangping Qian, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans
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Publication number: 20080119488Abstract: Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: July 24, 2005Publication date: May 22, 2008Applicant: EXELIXIS, INC.Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Haixia Wang, Yinong Xie, Lynne Canne Bannen, Diva Sze-Ming Chan, Ping Huang, Vasu Jammalamadaka, Richard G. Khoury, Morrison B. Mac, Jason Jevious Parks, Yong Wang, Wei Xu
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Patent number: 7320993Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Publication number: 20070287738Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.Type: ApplicationFiled: June 13, 2007Publication date: December 13, 2007Inventors: Derek Cecil Cole, Magda Asselin, Diane Harris Boschelli, Allan Wissner, Yanong Daniel Wang, Amarnauth Shastrie Prashad, Russell Dushin
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Patent number: 7276528Abstract: There are provided novel compounds of formula (I) wherein A, R1, R3, R4, R5, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory diseases, pain and CNS diseases.Type: GrantFiled: May 25, 2006Date of Patent: October 2, 2007Assignee: AstraZeneca ABInventors: Stephen Connolly, Glen Ernst
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Patent number: 7262209Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: October 2, 2002Date of Patent: August 28, 2007Assignee: Novartis Animal Health US, Inc.Inventors: Thomas Goebel, Pierre Ducray
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Publication number: 20070155799Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.Type: ApplicationFiled: December 18, 2006Publication date: July 5, 2007Inventors: Tomasz W. Glinka, Dale Edward Shuster, Chander Shekher Celly, Robert D. Simmons, Jason Zhang
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Patent number: 7148243Abstract: Compounds of the formula I: wherein Rx is cyano or bromo; R1 is halo; R2 is C114 C3 alkyl, and pharmaceutically acceptable salts and prodrugs thereof have activity as antiretrovirals.Type: GrantFiled: September 12, 2002Date of Patent: December 12, 2006Assignee: Medivir ABInventors: Christer Sahlberg, Rolf Noreen, Marita Hogberg, Per Engelhardt
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Patent number: 7135487Abstract: The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: May 29, 2003Date of Patent: November 14, 2006Assignee: Eli Lilly and CompanyInventors: Macklin B Arnold, Stephen R Baker, Thomas J Bleisch, Buddy E Cantrell, Ana M Escribano, Ken Matsumoto, Tracey E McKennon, Paul L Ornstein, Richard L Simon, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M Zimmerman
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Patent number: 7135486Abstract: This application relates to compounds of formula (I), wherein R1, R2, R3, and R4 are defined as recited in the claims, or a tautomer, salt, hydrate, or alkoxide thereof. A process for preparing such materials, pharmaceutical compositions containing them, and methods of treating a cardiovascular disorder by administering them to a patient are also disclosed and claimed.Type: GrantFiled: September 19, 2000Date of Patent: November 14, 2006Assignee: Bayer AktiengeselischaftInventors: Ulrich Rosentreter, Rolf Henning, Marcus Bauser, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Klaus Dembowsky, Olga Salcher-Schraufstätter, Johannes-Peter Stasch, Thomas Krahn, Elisabeth Perzborn
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Patent number: 7129255Abstract: This application relates to compounds of the formula wherein the groups R1–R6 are as defined in the specification and claims, and to a pharmaceutical composition containing the same, and to a method of using the same in treatment of cardiovascular disorders.Type: GrantFiled: March 25, 2002Date of Patent: October 31, 2006Assignee: Bayer AktiengesellschaftInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch, Mitsuyuki Shimada
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Patent number: 7125880Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: May 30, 2000Date of Patent: October 24, 2006Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen