Chalcogen Or Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/380)
  • Publication number: 20130041000
    Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.
    Type: Application
    Filed: August 14, 2012
    Publication date: February 14, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takashi YAMAMOTO, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
  • Publication number: 20130039856
    Abstract: The present invention concerns medicaments for slowing ageing. The medicaments can include an inhibitor of microbial folate biosynthesis as well as agents capable of reducing folate uptake by an animal. Examples of such medicaments include inhibitors that reduce the activity of an enzyme in the folate biosynthesis pathway, such as sulfonamides including sulfamethoxazole. The invention also concerns a food supplement, additive, functional food, or nutraceutial comprising the inhibitor or agent or composition as discussed above, as well as methods for screening for an agent for use as a medicament for slowing ageing comprising determining whether a test agent inhibits microbial folate biosynthesis, or whether the test agent reduces folate uptake by a non-human animal.
    Type: Application
    Filed: February 25, 2011
    Publication date: February 14, 2013
    Applicant: University of Durham
    Inventor: David Weinkove
  • Patent number: 8372874
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: February 12, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Monika Ermann
  • Publication number: 20130030022
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • Patent number: 8362039
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: January 29, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Markus Ostermeier, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
  • Publication number: 20130022660
    Abstract: The present invention relates to the treatment and prevention of vasospasm. The present invention provides a system for treating a cerebral vasospasm in a human utilizing a pharmaceutical composition and administrating a therapeutically effective amount of the pharmaceutical composition to a predetermined location in close proximity to a cerebral artery within a subarachnoid space wherein the pharmaceutical composition produces a localized pharmacologic effect thereby treating the cerebral vasospasm.
    Type: Application
    Filed: July 22, 2012
    Publication date: January 24, 2013
    Applicant: EDGE THERAPEUTICS, INC.
    Inventors: R. Loch Macdonald, Brian A. Leuthner
  • Publication number: 20130012552
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more azole fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.
    Type: Application
    Filed: March 2, 2011
    Publication date: January 10, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Patent number: 8349871
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: January 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
  • Publication number: 20130005783
    Abstract: Substances and methods of use of substances capable of inhibiting serine-palmitoyltransferase (SPT) and/or capable of competing with L-alanine and glycine, including in the reaction catalysed by SPT, including L-serine and D-serine and other compounds, to suppress cytotoxic sphingolipid metabolites, in particular deoxy-sphingolipids. The substances and methods can be used to prevent and treat disease caused by or associated with elevated levels of deoxy-sphingolipids, namely, diabetes (type 1 and type 2 diabetes), particularly diabetic neuropathy, neurodegenerative diseases such as hereditary and sensory neuropathy type I (HSAN1), amyotrophic lateral sclerosis (ALS), Alzheimer disease, other neurological disorders (e.g. depressive disorders, schizophrenia), medication-induced neuriopathies (e.g. induced by treatment with cytostatics like paclitaxel, cis-platin compounds etc.) and other metabolic disorders such as glycogen storage disease type 1a and asthma.
    Type: Application
    Filed: August 24, 2012
    Publication date: January 3, 2013
    Inventor: Thorsten Hornemann
  • Publication number: 20120322800
    Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).
    Type: Application
    Filed: October 14, 2010
    Publication date: December 20, 2012
    Inventor: Julian Blagg
  • Publication number: 20120322770
    Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.
    Type: Application
    Filed: August 21, 2012
    Publication date: December 20, 2012
    Inventor: Robert P. RICCIARDI
  • Publication number: 20120315303
    Abstract: Methods and intravascular treatment devices for treating atherosclerosis are provided.
    Type: Application
    Filed: May 4, 2012
    Publication date: December 13, 2012
    Applicant: Medtronic Vascular, Inc.
    Inventors: AYALA HEZI-YAMIT, SUSAN EDWARDS, CAROL SULLIVAN, OLUWASHOLA SHAKIRAT SULAIMON, LORI GARCIA, STEFAN TUNEV
  • Publication number: 20120309724
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20120289522
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: October 1, 2010
    Publication date: November 15, 2012
    Inventors: Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
  • Patent number: 8309535
    Abstract: The invention describes methods and compositions for alleviating recurrent medical afflictions for which anxiety may cause or exacerbate the affliction. A subject suffering from the affliction is treated with a combination of a pharmaceutical that enhances learning, and a second pharmaceutical recognized to be useful for treatment of the affliction. Representative afflictions include insomnia, erectile dysfunction, female sexual dysfunction, neuropathic pain, attention deficit disorder, and depression.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: November 13, 2012
    Inventors: Jason P. McDevitt, Michael Davis
  • Patent number: 8299048
    Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: October 30, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • Patent number: 8299103
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: October 30, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether
  • Publication number: 20120269767
    Abstract: The present specification discloses beta-amino alcohols and methods of treating a neurodegenerative disease using such compounds.
    Type: Application
    Filed: April 30, 2012
    Publication date: October 25, 2012
    Applicant: BIOCOPEA LIMITED
    Inventors: Robin Mark Bannister, Michael Harvey Lyne
  • Patent number: 8288426
    Abstract: A composition comprising fenamidone (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 16, 2012
    Assignee: Bayer CropScience AG
    Inventors: Heike Hungenberg, Wolfgang Thielert, Koen Van Den Eynde
  • Patent number: 8288403
    Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: October 16, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
  • Patent number: 8273780
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: September 25, 2012
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
  • Publication number: 20120225909
    Abstract: [Objective] To provide a drug that selectively stimulates the ?3-adrenergic receptors, particularly a drug capable of preferentially stimulating the ?3-adrenergic receptors over the ?1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.
    Type: Application
    Filed: September 30, 2010
    Publication date: September 6, 2012
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Yasuhiro Wada, Akifumi Morimoto
  • Publication number: 20120225880
    Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.
    Type: Application
    Filed: March 1, 2012
    Publication date: September 6, 2012
    Applicant: National Health Research Institutes
    Inventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
  • Publication number: 20120225916
    Abstract: The invention describes methods and compositions for alleviating medical afflictions for which anxiety may cause or exacerbate the affliction. A subject suffering from the affliction is treated with a combination of a pharmaceutical compound that enhances learning, and a second pharmaceutical recognized to be useful for treatment of the affliction, wherein D-cycloserine is the pharmaceutical compound that enhances learning. Representative afflictions include pain, mood disorders, anxiety disorders including performance anxiety, insomnia, female sexual dysfunction, chronic fatigue, autism spectrum disorders, fibromyalgia, and attention deficit-hyperactivity disorder.
    Type: Application
    Filed: May 11, 2012
    Publication date: September 6, 2012
    Inventors: Jason P. McDevitt, Michael Davis
  • Publication number: 20120213807
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20120213806
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Publication number: 20120208795
    Abstract: The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamopituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.
    Type: Application
    Filed: January 13, 2012
    Publication date: August 16, 2012
    Applicant: Board of Supervisors of Louisiana State University & Agricultural & Mechanical College
    Inventor: Nicholas E. Goeders
  • Publication number: 20120202750
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Publication number: 20120202862
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: April 18, 2012
    Publication date: August 9, 2012
    Applicant: NOVARTIS AG
    Inventors: Yuki IWAKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI
  • Patent number: 8236334
    Abstract: Disclosed is a method for protecting a tree from insects by injecting the tree with a fungicide and/or an antibiotic, and applying a composition to the surface of the tree, said composition comprising water, an insect repellent, an antihistamine, and an insect poison.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: August 7, 2012
    Inventor: James S. Bass
  • Patent number: 8236822
    Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: August 7, 2012
    Assignee: Abbott Laboratories
    Inventors: Xueqing Wang, Michael J. Dart, Bo Liu
  • Publication number: 20120196839
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: August 3, 2010
    Publication date: August 2, 2012
    Applicant: AMIRA PHARMACEUTICALS INC.
    Inventors: John Howard Hutchinson, Thomas J. Seiders, Bowei Wang
  • Patent number: 8216971
    Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: July 10, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Koen van Den Eynde, Wolfgang Thielert, Heike Hungenberg
  • Patent number: 8217066
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: July 10, 2012
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Thomas Jon Seiders, Lucy Zhao, Jeannie M. Arruda, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
  • Publication number: 20120172396
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Application
    Filed: February 7, 2012
    Publication date: July 5, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Denis CARNIATO, Christine CHARON, Johannes GLEITZ, Didier ROCHE, Bjoern HOCK
  • Publication number: 20120172337
    Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.
    Type: Application
    Filed: March 8, 2012
    Publication date: July 5, 2012
    Applicant: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Patent number: 8211926
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: July 3, 2012
    Assignee: Cara Therapeutics, Inc.
    Inventor: Robert Zhiyong Luo
  • Publication number: 20120165339
    Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.
    Type: Application
    Filed: December 20, 2011
    Publication date: June 28, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
  • Publication number: 20120148509
    Abstract: Disclosed are a composition for alleviating ultraviolet irradiation-induced damage, which is stable and safe and can be used on a daily basis, and a pharmaceutical composition, an external skin preparation, a food composition and a medicine for cataract, each comprising aforesaid composition for alleviating ultraviolet irradiation-induced damage. Specifically disclosed is a composition for alleviating ultraviolet irradiation-induced damage which contains one or more kinds of compounds selected from the group consisting of methionine, D-serine and derivatives and/or salts of the same. The aforesaid composition may be an external preparation for the skin, an anti-wrinkle agent, a sunscreen agent, a medicinal composition for treating and/or preventing skin diseases, a food composition or a pharmaceutical product for cataract.
    Type: Application
    Filed: September 14, 2010
    Publication date: June 14, 2012
    Inventors: Yutaka Ashida, Yosuke Tojo, Chieko Mizumoto, Masashi Mita
  • Publication number: 20120149706
    Abstract: 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: Application
    Filed: February 21, 2012
    Publication date: June 14, 2012
    Inventors: Jacques DUMAS, Uday KHIRE, Timothy B. Lowinger, Holger PAULSEN, Bernd RIEDL, Willian J. SCOTT, Roger A. SMITH, Jill WOOD, Holia HATOUM-MOKDAD, Wendy LEE, Aniko REDMAN, Jeffrey JOHNSON, Robert SIBLEY
  • Publication number: 20120142677
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: December 15, 2009
    Publication date: June 7, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
  • Publication number: 20120129800
    Abstract: The present invention concerns an agent for prevention and treatment of pityriasis. The agent according to the present invention comprises at least one transaminase inhibitor effectively inhibiting the transamination process which is of pathogenetic relevance for the disease, prevents a recurrence of the disease and which protects the human skin flora. Upon release into the environment, no resistances are induced in other fungi.
    Type: Application
    Filed: January 14, 2010
    Publication date: May 24, 2012
    Applicant: Justus-Liebig-Universitat Giessen
    Inventor: Peter Mayser
  • Patent number: 8183265
    Abstract: The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: November 22, 2007
    Date of Patent: May 22, 2012
    Assignee: Merck Patent GmbH
    Inventors: Didier Roche, Denis Carniato, Liliane Doare, Christine Charon, Caroline Leriche
  • Publication number: 20120122780
    Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 17, 2012
    Applicant: Ardea Biosciences Inc.
    Inventors: Martha De La Rosa, Jean-Luc Girardet
  • Patent number: 8178568
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: May 15, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John Regan, Doris Riether
  • Publication number: 20120115841
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Application
    Filed: May 17, 2010
    Publication date: May 10, 2012
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20120115868
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Application
    Filed: November 2, 2011
    Publication date: May 10, 2012
    Inventors: Stephen Deems Gabriel, Andrew Thomas
  • Patent number: 8173652
    Abstract: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: May 8, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Maria-Clemencia Hernandez, Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20120100989
    Abstract: The invention relates to 3-aryl-4-(2-thienylmethylene)isoxazol-5(4H)-ones, to agrochemically active salts thereof, to their use and to methods and compositions for controlling phytopathogenic harmful fungi and insects in and/or on plants or in and/or on seed of plants, to processes for preparing such compositions and to treated seed, and to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in animal health, in the protection of materials and in the domestic and hygiene field. The present invention further relates to a process for preparing isoxazolone derivatives.
    Type: Application
    Filed: June 22, 2011
    Publication date: April 26, 2012
    Applicant: Bayer CropScience AG
    Inventors: Werner HALLENBACH, Oliver Guth, Thomas Seitz, Heinz-Juergen Wroblowsky, Philippe Desbordes, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Peter Lösel, Olga Malsam, Rachel Rama, Hiroyuki Hadano
  • Publication number: 20120095012
    Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
    Type: Application
    Filed: December 30, 2009
    Publication date: April 19, 2012
    Applicant: Elara Pharmaceuticals GmbH
    Inventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen