The Five-membered Hetero Ring Consists Of One Nitrogen And Four Carbons Patents (Class 514/408)
  • Patent number: 7541045
    Abstract: A concentrated quaternary ammonium compound (QAC) solution comprising a QAC with a concentration from greater than about 10% by weight and at least one solubility enhancing agent, such as an alcohol, is disclosed. A diluted QAC solution is used to contact food products to prevent microbial growth on the food products from a broad spectrum of foodborne microbial contamination. A method of contacting the food products with the dilute QAC for an application time of at least 0.1 second is disclosed. The foods that can be treated by this method are meat and meat products, seafood, vegetables, fruit, dairy products, pet foods and snacks, and any other food that can be treated and still retain its appearance and texture. One of the treatment methods is spraying and misting the QAC solutions on the food products for an application time of at least 0.1 second to prevent broad spectrum foodborne microbial contamination.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: June 2, 2009
    Assignee: University of Arkansas
    Inventors: Cesar Compadre, Philip Breen, Hamid Salari, E. Kim Fifer, Danny L. Lattin, Michael Slavik, Yanbin Li, Timothy O'Brien, Amy L. Waldroup, Thomas F. Berg
  • Publication number: 20090118289
    Abstract: The present invention relates to compounds having the general formula (I) with the definitions of A, X, R1-R6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of ?-secretase activity.
    Type: Application
    Filed: October 21, 2005
    Publication date: May 7, 2009
    Applicant: CELLZOME AG
    Inventors: Francis Wilson, Alison Reid, Valerie Reader, Richard John Harrison, Mihiro Sunose, Remedios Hernandez-Perni, Jeremy Major, Cyrille Boussard, Kathryn Smelt, Jess Taylor, Adeline Leformal, Andrew Cansfield, Svenja Burckhardt
  • Publication number: 20090118316
    Abstract: The present invention relates to methods of stimulating osteoblast function with a PYK2 inhibitor in subjects with osteoporosis, bone fractures, non-unions, pseudoarthroses, periodontal disease or other disorders of bone metabolism. Optionally, the method further comprises administration of a second therapeutic bone agent. The present invention also relates to methods to identify a PYK2 inhibitor effective as a therapeutic bone agent comprising administering a test agent to an osteoblast-like cell and determining if osteoblast function is stimulated. Optionally, the identifying method further comprises contacting the test agent with PYK2 and determining if PYK2 activity is inhibited.
    Type: Application
    Filed: June 10, 2005
    Publication date: May 7, 2009
    Inventors: Lisa M. Olson, Thomas A. Brown, Leonard Buckbinder, Angel Guzman-Perez, John C. Kath, Hua Zhu Ke, Michael J. Luzzio
  • Publication number: 20090105125
    Abstract: The disclosure provides methods for treating fatty liver disease and associated conditions by inhibiting the synthesis of glucosphingolipids, as exemplified by the use of glucosylceramide synthase substrate analogs.
    Type: Application
    Filed: May 9, 2007
    Publication date: April 23, 2009
    Inventors: Hongmei Zhao, Nelson S. Yew, Seng H. Cheng, Canwen Jiang, Cynthia Marie Arbeeny
  • Patent number: 7521062
    Abstract: The present invention is directed to novel immune potentiators, novel vaccine adjuvants, novel compounds and pharmaceutical compositions, novel methods for treating viral infections, including HCV, by administering the compounds, and novel methods for modulating an immune response by administering the compounds.
    Type: Grant
    Filed: December 29, 2003
    Date of Patent: April 21, 2009
    Assignee: Novartis Vaccines & Diagnostics, Inc.
    Inventors: Paul A. Barsanti, Nathan Brammeier, Anthony Diebes, Liana Marie Lagniton, Simon Ng, Zhi-Jie Ni, Keith B. Pfister, Casey Philbin, Nicholas Valiante, Allan S. Wagman, Weibo Wang, Amy J. Weiner
  • Publication number: 20090087405
    Abstract: The invention relates to a method of treating immunologic diseases or pathological conditions involving an immunologic component using certain Lck inhibitors already known as kinase inhibitors for therapy in oncology, optionally in combination with one or more other drugs selected from NSAIDs, steroids, DMARDs, immunsuppressives, biologic response modifiers and antinfectives, pharmaceutical compositions comprising said Lck inhibitors together with said other drugs, and the use of the Lck inhibitors for the manufacture of a pharmaceutical composition for the treatment of immunologic diseases or pathological conditions involving an immunologic component.
    Type: Application
    Filed: December 12, 2008
    Publication date: April 2, 2009
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Gerald Juergen ROTH, Armin HECKEL, Rainer WALTER, Frank HILBERG, Rudolf HAUPTMANN, Martin Friedrich STEFANIC, Florian COLBATZKY, Steffen ERNST
  • Patent number: 7511070
    Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.
    Type: Grant
    Filed: November 9, 2005
    Date of Patent: March 31, 2009
    Assignee: Poniard Pharmaceuticals, Inc.
    Inventors: David J. Grainger, James C. Metcalfe, Sudhakar Kasina
  • Publication number: 20090076114
    Abstract: The present invention relates to cis-1,2-substituted stilbene derivatives, or their pharmaceutically acceptable salts, glucosides or solvates, a pharmaceutical composition comprising the compound, and use of said compound for preparation of a drug for treatment and/or prevention of diabetes or improvement of diabetic complications.
    Type: Application
    Filed: July 20, 2005
    Publication date: March 19, 2009
    Inventors: Zhiyun Kang, Zuze Wu, Zhuangrong Sun, Zhongxiong Tang
  • Publication number: 20090062366
    Abstract: [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).
    Type: Application
    Filed: May 18, 2006
    Publication date: March 5, 2009
    Applicant: ASTELLAS PHARAMA INC.
    Inventors: Shunichiro Hachiya, Makoto Oku, Hana Mukai, Takashi Shin, Keisuke Matsuura, Ryushi Seo, Takashi Kamikubo, Yoh Terada, Masanao Sanagi, Kousei Yoshihara, Taisuke Takahashi
  • Publication number: 20090062338
    Abstract: Pharmaceutical compositions are provided that are useful in treating cardiovascular disease. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of one or more genes related to the cardiovascular disease. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of cardiovascular disease. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl), and the cardiovascular disease is myocardial infarction.
    Type: Application
    Filed: February 2, 2006
    Publication date: March 5, 2009
    Inventors: Louis Habash, Clarence Jones
  • Patent number: 7498447
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: March 3, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20090054426
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Application
    Filed: August 21, 2008
    Publication date: February 26, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Publication number: 20090054420
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Application
    Filed: August 21, 2008
    Publication date: February 26, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
  • Patent number: 7495111
    Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.
    Type: Grant
    Filed: June 15, 2006
    Date of Patent: February 24, 2009
    Assignee: Wyeth
    Inventors: P. Sivaramakrishnan Ramamoorthy, Zhongqi Shen, Boyd L. Harrison
  • Patent number: 7495022
    Abstract: Disclosed are agents that inhibit histone deacetylase. More specifically, the present invention relates to novel hydroxamic acid derivatives or pharmaceutically acceptable salts thereof for anticancer agents or other therapeutic agents based on their histone deacetylase inhibitory activity.
    Type: Grant
    Filed: April 10, 2003
    Date of Patent: February 24, 2009
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Dae-Kee Kim, Ju Young Lee, Nam Kyu Lee, Jae-Sun Kim, Junwon Lee, Suk Ho Lee, Jin Young Choi, Je Ho Ryu, Nam Ho Kim, Guang-Jin Im, Tae Kon Kim, Jung-Woo Seo, Young-Jue Bang
  • Patent number: 7491831
    Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: February 17, 2009
    Assignee: Plexxikon, Inc.
    Inventors: Dean R. Artis, Prabha N. Ibrahim, Jack Lin, Chao Zhang
  • Publication number: 20090041869
    Abstract: The present invention discloses Resistance Management (RM) practices that are critical to safeguard Bacillus thuringiensis as a natural resource and sustain genetically modified corn expressing Bt toxins as a suitable method for ECB and WCRW management. A useful tool in developing RM strategies is to develop laboratory selected colonies that exhibit high levels of resistance to a particular toxin. The availability of selected strains allows determination of the genetic expression of resistance (i.e., dominant vs. recessive, autosomal vs. sex-linked) and whether or not the resistance mechanism is specific for a given toxin. In addition, the availability of resistant strains will allow estimation of the particular resistance allele frequency in the field, and provides a tool to identify the biochemical and physiological basis of resistance and a means to develop molecular probes to monitor the evolution of resistance in the field.
    Type: Application
    Filed: October 15, 2008
    Publication date: February 12, 2009
    Applicant: PIONEER HI-BRED INTERNATIONAL, INC.
    Inventor: DANIEL J. COSGROVE
  • Patent number: 7485662
    Abstract: An object of the present invention is to provide a therapeutic agent for diabetes mellitus or insulin resistance improving agent, or to provide foods and drinks, food and drink additives, and feeds or feed additives for treating diabetes mellitus or improving insulin diabetes. In order to achieve such an object, the present invention provides a therapeutic agent for diabetes mellitus and insulin resistance improving agent comprising hydroxyproline, a hydroxyproline derivative or a pharmaceutically acceptable salt thereof or foods and drinks, food and drink additives, feeds or feed additives for treatment of diabetes mellitus or improvement of insulin resistance comprising the same.
    Type: Grant
    Filed: March 19, 2004
    Date of Patent: February 3, 2009
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshikazu Kamiya, Akio Shirai, Miho Takada, Fumiko Ogino
  • Publication number: 20090029922
    Abstract: The invention relates to the use of a sphingosine-1-phosphate receptor agonist in the treatment of heart diseases.
    Type: Application
    Filed: October 2, 2008
    Publication date: January 29, 2009
    Inventors: Volker Brinkmann, Gilles Feutren, Robert Paul Hof
  • Publication number: 20090029962
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: July 21, 2008
    Publication date: January 29, 2009
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 7482364
    Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: January 27, 2009
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
  • Patent number: 7482475
    Abstract: Disclosed herein is a compound having a structure Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 9, 2007
    Date of Patent: January 27, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Robert M. Burk
  • Patent number: 7482472
    Abstract: The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production of these compounds, pharmaceutical compositions containing them, and methods of using them for the prevention and/or treatment of various diseases.
    Type: Grant
    Filed: March 12, 2007
    Date of Patent: January 27, 2009
    Assignee: Bayer Healthcare AG
    Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer
  • Publication number: 20090018116
    Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Application
    Filed: May 20, 2005
    Publication date: January 15, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Shujuan Jin, Ziping Liu, Claire Milburn, Miroslaw Tomaszewski, Christopher Walpole, Zhong-Yong Wei, Hua Yang
  • Patent number: 7476746
    Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: January 13, 2009
    Assignee: Plexxikon, Inc.
    Inventors: Dean R. Artis, Prabha N. Ibrahim, Jack Lin, Chao Zhang
  • Patent number: 7476747
    Abstract: A compound comprising or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: January 13, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20090012144
    Abstract: Novel optically active ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, and m are each as defined in the description, a plurality of the processes for preparing these substances and their use for controlling pests.
    Type: Application
    Filed: July 28, 2008
    Publication date: January 8, 2009
    Inventors: Andrew Plant, Thomas Geller, Bernd Gallenkamp, Rolf Grosser, Albrecht Marhold, Christoph Erdelen, Andreas Turberg, Olaf Hansen
  • Patent number: 7473779
    Abstract: Novel derivatives of amidines of formula wherein the substituents are defined as in the specification which are useful for inhibiting activity on NO-synthase enzymes producing nitrogen mono oxide and/or trapping the reactive oxygen species (ROS) making them useful for treating various diseases.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: January 6, 2009
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
  • Patent number: 7468383
    Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.
    Type: Grant
    Filed: February 9, 2006
    Date of Patent: December 23, 2008
    Assignee: Cephalon, Inc.
    Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassara, Germano D'Arasmo, Ernesto Menta, Ambrogio Oliva
  • Patent number: 7465811
    Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: December 16, 2008
    Assignee: Laboratoires Fournier S.A.
    Inventors: Luc Lebreton, Christine Dumas, Christine Massardier, Michel Bondoux
  • Patent number: 7456210
    Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the specification and to pharmaceutically acceptable salts thereof for the treatment of diseases, which are mediated by monoamine oxidase B inhibitors, for example Alzheimer's disease and senile dementia.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: November 25, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez-Sarmiento, Wolfgang Wostl, Rene Wyler
  • Publication number: 20080287506
    Abstract: Certain novel N,N-di(heteroarylalkyl)amine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein Ar Ar1, a, b, c, R, Rd, Re, Rf, Rg, Rh, R?, R3 and Rk are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Application
    Filed: October 27, 2005
    Publication date: November 20, 2008
    Applicant: Bayer CropScience AG
    Inventors: David M. Roush, John F. Chiarello, George Theodoridis, Hongyan Qi
  • Publication number: 20080286285
    Abstract: Compositions and methods included herein describe the treatment of atherosclerosis and other vascular diseases such as thrombosis, restenosis after angioplasty and/or stenting, and vein-graft disease after bypass surgery, by inhibition of the expression or biologic activity of the toll-like receptor 4 (TLR4) and/or myeloid differentiation factor 88 (MyD88). TLR4 cell signal transduction is at least partially responsible for the manifestation, continuation, and/or worsening of atherosclerosis and other forms of vascular disease. The present invention provides several means with which to inhibit this signal transduction pathway by affecting the biological activity of the TLR4 receptor and/or MyD88.
    Type: Application
    Filed: May 25, 2005
    Publication date: November 20, 2008
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Moshe Arditi, Tripathi Rajavashisth, Prediman K. Shah
  • Publication number: 20080275003
    Abstract: The present invention relates to bis-cationic compounds comprising quaternary ammonium groups and/or quaternary phosphonium groups. The invention also relates to the use of bis-cationic compounds as Phospholipase B inhibitors and the use of bis cationic compounds for the treatment or prevention of microbial infection.
    Type: Application
    Filed: November 12, 2004
    Publication date: November 6, 2008
    Applicant: THE UNIVERSITY OF SYDNEY
    Inventors: Alfred Werner Widmer, Katrina Anne Jolliffe, Lesley Catherine Wright, Tania Christine Sorrell
  • Publication number: 20080269283
    Abstract: Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:
    Type: Application
    Filed: June 27, 2008
    Publication date: October 30, 2008
    Inventors: Pingchen Fan, Hiroyuki Goto, Xiao He, Makoto Kukutani, Marc Labelle, Dustin L. McMinn, Jay P. Powers, Yosup Rew, Daqing Sun, Xuelei Yan
  • Publication number: 20080269189
    Abstract: Compounds, compositions, and methods of avoiding edema while treating or preventing PPAR?-mediated diseases, including cancer, using derivatives and prodrugs are provided.
    Type: Application
    Filed: March 21, 2006
    Publication date: October 30, 2008
    Inventors: Martin E. Sanders, David D. Karpf
  • Publication number: 20080261985
    Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Application
    Filed: November 16, 2007
    Publication date: October 23, 2008
    Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
  • Publication number: 20080255095
    Abstract: 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: Application
    Filed: June 18, 2007
    Publication date: October 16, 2008
    Applicant: BTG INTERNATIONAL LIMITED
    Inventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
  • Publication number: 20080234293
    Abstract: Cannabinoid derivatives according to formula (I) are disclosed wherein, X, Y, R1, R2, and W can have the definitions provided herein. Without limitation, use of such compounds, their salts or pro-drug, or compositions containing the compounds, salts, or pro-drug, to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.
    Type: Application
    Filed: March 3, 2008
    Publication date: September 25, 2008
    Inventors: Bob M. Moore, Himanshu Bhattacharjee, Charles R. Yates, Leslie Stuart
  • Publication number: 20080226753
    Abstract: The present invention discloses Resistance Management (RM) practices that are critical to safeguarding Bacillus thuringiensis as a natural resource and to sustaining genetically modified crops that express Bt toxins for managing ECB and WCRW. The methods involve blending seed transformed with a nucleic acid encoding a different pesticidal protein, where both proteins target the same pest, but use different modes of pesticidal action. The seed can be also treated with pesticidal agents.
    Type: Application
    Filed: March 29, 2005
    Publication date: September 18, 2008
    Applicant: PIONEER HI-BRED INTERNATIONAL, INC.
    Inventor: Daniel J. Cosgrove
  • Publication number: 20080227767
    Abstract: Methods and compositions which are useful in the treatment of amyloidosis. In particular, methods and compositions are provided for inhibiting, preventing and treating amyloid deposition, e.g., in pancreatic islets, wherein the amyloidotic deposits are islet amyloid polypeptide (IAPP)-associated amyloid deposition or deposits. The methods of the invention involve administering to a subject a therapeutic compound which inhibits IAPP-associated amyloid deposits. Accordingly, the compositions and methods of the invention are useful for inhibiting IAPP-associated amyloidosis in disorders in which such amyloid deposition occurs, such as diabetes.
    Type: Application
    Filed: May 22, 2008
    Publication date: September 18, 2008
    Applicant: Neurochem (International) Limited
    Inventors: Walter A. Szarek, Donald F. Weaver, Xianqi Kong, Ajay Gupta, David Migneault
  • Patent number: 7425569
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
    Type: Grant
    Filed: October 11, 2007
    Date of Patent: September 16, 2008
    Assignee: Pfizer Inc
    Inventors: Paul Anthony Bradley, Kevin Neil Dack, Patrick Stephen Johnson, Sarah Elizabeth Skerratt
  • Patent number: 7423170
    Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.
    Type: Grant
    Filed: January 23, 2006
    Date of Patent: September 9, 2008
    Assignee: Arizona Biomedical Research Commission
    Inventors: Seth D. Rose, Scott R. Lefler, Steven R. Ottersberg, Ann Y. Kim, Karl J. Okolotowicz, Rosemarie F. Hartman
  • Publication number: 20080194666
    Abstract: A method of treating an individual with a condition which condition is one wherein the individual with the condition benefits from the administration of GnRH and/or a GnRH analogue, the method comprising administering to the individual GnRH and/or a GnRH analogue and an inhibitor of prostaglandin synthesis and/or a prostaglandin receptor antagonist. The methods of the invention also include combating a sex-hormone dependent disease in an individual, and regulating fertility in an individual.
    Type: Application
    Filed: April 3, 2006
    Publication date: August 14, 2008
    Applicant: MEDICAL RESEARCH COUNCIL
    Inventors: Henry Nicolas Jabbour, Robert Peter Millar, Zvi Naor
  • Patent number: 7411091
    Abstract: This invention is related to compounds and use of N-Acyl-N?-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 group; R1 is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8 alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1-C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R4, R5 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is hydrogen or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, in
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: August 12, 2008
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Cibele Maria Sabido David, Laura Faravelli, Stefania Gagliardi, Elena Colombo, Patricia Salvati
  • Publication number: 20080188537
    Abstract: A benzamide derivative, especially amisulpride, is used to prevent or treat bipolar depression of a patient suffering from bipolar disorder I or bipolar disorder II.
    Type: Application
    Filed: January 11, 2008
    Publication date: August 7, 2008
    Inventor: Jean-Michel AZORIN
  • Publication number: 20080188456
    Abstract: A method for repelling arthropods involving treating an object or area with an arthropod repelling effective amount of at least one compound having the formula wherein X is O, S, NH, N-NH2, N-CH3 or CH2, R? is H or alkyl, R? is alkyl, n is 0, 1, 2, 3 or 4, and mixtures thereof, optionally including a carrier material or canier. The compound is preferably selected from homopiperazine, 1-methylhomopiperazine, 1-methylpyrrolidine, (R)-(?)-2-methylpiperazine, (S)-(+)-2-methylpiperazine, 2-methylpiperazine, 1-methylpiperazine, pyrrolidine, 1-methylpiperidine, piperidine, 1-ethylpiperazine, 1-methylimidazolidine, 1-methylthiomorpholine, 1,4-dimethylpiperazine, homopiperidine, imidazolidine, 4-methylpiperidine, thiomorpholine, 1-amino-4-methylpiperazine, 4-methylmorpholine, azocane, 2,6-dimethylpiperazine, 2,5-dimethylpiperazine, piperazine, 1-methlyhomopiperidine, or mixtures thereof.
    Type: Application
    Filed: December 10, 2007
    Publication date: August 7, 2008
    Inventors: Ulrich R. Bernier, Kenneth Posey, Daniel L. Kline, Donald Barnard, Kamal Chauhan
  • Patent number: 7407982
    Abstract: The present invention relates to novel covalent oligo and polyalkylene glycol conjugates with synthetic inhibitors of trypsin-type serine proteases, in particular inhibitors of the hemocoagulation protease thrombin, synthetic intermediates stages required in their production and their use for producing active ingredients for the treatment or prophylaxis of thrombotic complications.
    Type: Grant
    Filed: January 23, 2002
    Date of Patent: August 5, 2008
    Assignee: HaemoSys GmbH
    Inventors: Torsten Steinmetzer, Götz Nowak
  • Patent number: 7408071
    Abstract: There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5?, R6, R7, and p as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: August 5, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Shirong Zhu, John E. Macor, Shuhao Shi, Samuel Gerritz
  • Publication number: 20080176838
    Abstract: The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.
    Type: Application
    Filed: June 8, 2005
    Publication date: July 24, 2008
    Applicant: SANTHERA PHARMACEUTICALS (DEUTSCHLAND) AG
    Inventors: Paul John Edwards, Silvia Cerezo-Galvez, Achim Feurer, Oliver Hill, Meinolf Thiemann, Victor Giulio Matassa, Sonja Nordhoff, Meritxell Lopez-Canet