Chalcogens Bonded Directly To At Least Two Ring Carbons Of The Six-membered Hetero Ring Patents (Class 514/348)
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Publication number: 20130267564Abstract: A benzyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; A is a oxygen atom and the like, and m is an integer of 0-5, or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.Type: ApplicationFiled: December 22, 2011Publication date: October 10, 2013Applicant: NIHON NOHYAKU CO., LTD.Inventors: Ryota Kasahara, Hiroto Harayama, Eikou Satoh, Motofumi Nakano, Kosuke Fukatsu, Kayo Inukai
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Publication number: 20130252986Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease and/or diabetic macular edema.Type: ApplicationFiled: December 5, 2011Publication date: September 26, 2013Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
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Publication number: 20130237515Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.Type: ApplicationFiled: February 28, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
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Patent number: 8524747Abstract: The object of the present invention is to provide a pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B. The pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B contains DTCM glutarimide of the Formula (I) as an effective ingredient, thereby being able to inhibit nitric oxide (NO) production and prostaglandin production.Type: GrantFiled: June 25, 2009Date of Patent: September 3, 2013Assignee: Keio UniversityInventors: Kazuo Umezawa, Yuichi Ishikawa, Shigeru Nishiyama, Miyuki Tachibana, Ayumi Kaneda
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Publication number: 20130203822Abstract: Compound of Formula (I): wherein R1, R2 and R3, which are identical or different, are hydrogen atom or C1-4 alkyl, and R4 is a saturated C6-9 linear, branched or cyclic hydrocarbon radical or a radical of Formula (II) wherein X is S or O, Y is a hydrogen atom or up to 2 halogen atoms, Z is a single bond or a divalent radical being O, S, —CR2—, in which R is hydrogen or C1-4 alkyl, or other divalent radical with 2-10 carbon atoms and, optionally, O and/or S atoms linked in the form of a chain, wherein—if the radicals contain 2 or more O and/or S atoms—the latter are separated from one another by at least 2 carbon atoms, and it also being possible for 2 adjacent carbon atoms to be linked together by a double bond, and the free valencies of the carbon atoms being saturated by a hydrogen atom and/or C1-4 alkyl groups, Ar is an aromatic ring system which has up to two rings and which may be substituted by up to three radicals from the group of fluorine, chlorine, bromine, methoxy, C1-4 alkyl, trifluoromethyl and tType: ApplicationFiled: June 22, 2011Publication date: August 8, 2013Inventors: Alessandro Quattrone, Viktoryia Sidarovich, Valentina Adami
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Publication number: 20130195827Abstract: This invention concerns Reward Deficiency Syndrome (RDS) and obesity, and the role of catecholaminergic pathways in aberrant substance-seeking behavior, in particular cravings for carbohydrates. Also described are new nutrigenomic formulas having unique combinations of ingredients having a generalized anti-craving effect are, which can inhibit carbohydrate bingeing, inducing significant healthy fat loss and relapse prevention, as well genetic testing for certain polymorphisms correlated with RDS behaviors.Type: ApplicationFiled: September 27, 2012Publication date: August 1, 2013Inventors: Kenneth Blum, B. William Downs, Roger L. Waite, William J. Heaney
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Publication number: 20130197038Abstract: The invention is directed to a method of inducing angiogenesis at a site in an individual in need thereof comprising administering locally to the site an effective amount of one or more agents that induce hypoxia induced factor 1? (HIF-1?). In another aspect, the invention is directed to a method of inducing angiogenesis at a site in an individual in need thereof comprising administering locally to the site an effective amount of one or more agents that induce hypoxia induced factor 1? (HIF-1?) and one or more lysophospholipids. In addition, the invention is directed to methods of generating prevascularized tissue, methods of generating a vascular network in a device and compositions thereof.Type: ApplicationFiled: January 16, 2013Publication date: August 1, 2013Applicants: Massachusetts Institute of Technology, National University of SingaporeInventors: National University of Singapore, Massachusetts Institute of Technology
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Publication number: 20130190365Abstract: A therapeutically effective amount of deferiprone or deferasirox or physiologically acceptable salts thereof for the prevention, stabilization, treatment, or reversal of iron-induced FRDA disease in patients resulting from mitochondrial iron-induced damage to preferentially reduce the iron stores in the mitochondria. Also for the treatment of other conditions affecting the brain where a key element in the generation of the resultant pathology is the intracellular mishandling of iron.Type: ApplicationFiled: January 31, 2013Publication date: July 25, 2013Inventors: Arnold Munnich, Michael Spino, Ioav Cabantchik
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Publication number: 20130158010Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: ApplicationFiled: February 19, 2013Publication date: June 20, 2013Applicant: Aerpio Therapeutics Inc.Inventors: Robert Shalwitz, Joseph H. Gardner
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Publication number: 20130157851Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.Type: ApplicationFiled: August 18, 2011Publication date: June 20, 2013Applicant: ISAGRO S.P.A.Inventors: Marilena Gusmeroli, Lucio Filippini, Franco Pellacini, Paolo Bravini, Alexia Elmini, Matteo Santino Vazzola, Christian Badaracco
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Publication number: 20130137635Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.Type: ApplicationFiled: February 9, 2011Publication date: May 30, 2013Applicant: LEXICON PHARMACEUTICALS, INC.Inventor: Arthur Thomas Sands
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Publication number: 20130123304Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: ApplicationFiled: January 7, 2013Publication date: May 16, 2013Applicant: University of Tennessee Research FoundationInventor: University of Tennessee Research Foundation
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Publication number: 20130109708Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 4, 2011Publication date: May 2, 2013Applicant: Pfizer LimitedInventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
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Publication number: 20130084346Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: April 4, 2013Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
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Publication number: 20130023569Abstract: There is provided use of orally available or topically applied deferiprone for prevention of iron-induced eye damage. The use may be for preparation of a medicament or in a method of preventing iron-induced eye damage to an eye of a subject at risk for iron-induced eye damage, the method comprising administering a prophylactically effective amount of deferiprone to the subject. There is also provided the use of deferiprone for treatment of iron-related eye disorders. The use may be for preparation of a medicament or in a method of treatment of damage to an eye of a having eye damage associated with iron, the method comprising topically administering a therapeutically effective amount of deferiprone to the subject.Type: ApplicationFiled: November 12, 2009Publication date: January 24, 2013Applicants: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, APOTEX TECHNOLOGIES INC.Inventors: Michael Spino, Joshua Lawrence Dunaief
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Publication number: 20130012549Abstract: The present invention provides uses of a salt adduct comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, for the preparation of a medicament for the treatment, alleviation of symptoms of, relieving, improving and preventing a cognitive disease, disorder or condition in a subject. Additionally, the invention provides use of said salt adducts for the preparation of medicaments for the improvement of cognitive functions in a healthy subject.Type: ApplicationFiled: July 3, 2012Publication date: January 10, 2013Applicant: Alcobra Ltd.Inventors: Rina Yamin, Dalia Megiddo, Yaron Ilan
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Patent number: 8349876Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: October 14, 2009Date of Patent: January 8, 2013Assignee: The University of Tennesee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20130005744Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: January 3, 2013Inventors: Scott Wolkenberg, James C. Barrow, Scott T. Harrison, B. Wesley Trotter, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao
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Publication number: 20120328679Abstract: Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or bioavailability in a use environment.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Inventors: William J. Curatolo, Scott M. Herbig, James A. S. Nightingale
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Patent number: 8334263Abstract: Compositions of flupirtine for management of neuropathic or inflammatory pain optionally including one or more other analgesics including opiates, NSAIDS and other active agents in immediate and controlled release forms. Methods and systems for administration of these compositions.Type: GrantFiled: December 16, 2004Date of Patent: December 18, 2012Inventors: Raymond Nadeson, Adam Paul Tucker, Colin Goodchild
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Publication number: 20120316200Abstract: The present invention is directed to novel phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be useful in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.Type: ApplicationFiled: April 7, 2011Publication date: December 13, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Linus S. Lin, Richard Soll, Jingchao Dong, Hao Wu, Takao Suzuki, Bin Hu, Dejun Liu, Jinglai Hao, Ming Xu
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Patent number: 8318945Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.Type: GrantFiled: August 15, 2011Date of Patent: November 27, 2012Assignee: The Regents of the University of CaliforniaInventors: David T. Puerta, Seth M. Cohen, Jana A. Lewis
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Publication number: 20120294826Abstract: The present invention provides, inter alia, methods for ameliorating an adverse effect in a patient caused by an acute transfusion into the patient of a composition containing aged red blood cells using an iron chelator. Apparatuses and kits for ameliorating such adverse effects are also provided.Type: ApplicationFiled: December 1, 2011Publication date: November 22, 2012Inventors: Steven L. Spitalnik, Eldad A. Hod, Gary M. Brittenham
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Publication number: 20120276152Abstract: Methods and systems for treating an infarct by delivery of zinc chelator to modulate tissue.Type: ApplicationFiled: February 6, 2012Publication date: November 1, 2012Inventors: Syed Hossainy, John Stankus, Mikael Trollsas, Dariush Davalian
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Publication number: 20120270882Abstract: Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Frederich's Ataxia.Type: ApplicationFiled: July 5, 2010Publication date: October 25, 2012Applicant: APOTEX TECHNOLOGIES INC.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yangqing Zhao, Tao Xin, Birenkumar Shah, Blaise N'zemba, Jolanta Maria Wodzinska, Maryna Premyslova
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Publication number: 20120264790Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 1, 2012Publication date: October 18, 2012Applicant: SANOFIInventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
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Publication number: 20120258170Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.Type: ApplicationFiled: March 19, 2012Publication date: October 11, 2012Applicant: Nutracryst Therapeutics Private LimitedInventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
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Patent number: 8273773Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: July 22, 2009Date of Patent: September 25, 2012Assignee: Roche Palo Alto LLCInventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 8268821Abstract: The present invention relates generally to the field of pain management, and in particular, the management of neuropathic or inflammatory pain including a neuropathic or inflammatory component of nociceptive pain. More particularly, the present invention provides methods and compositions which treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic or inflammatory pain. The present invention further contemplates combination therapy involved in the treatment of pain in association with the treatment of a particular disease condition or pathology. The present invention further also provides sustained and slow release formulations, tamper-proof deliver systems and stents, catheters and other mechanical devices coated with formulations which permit sustained or slow release of active ingredients involved in pain management.Type: GrantFiled: December 1, 2010Date of Patent: September 18, 2012Assignee: Relevare Aust. Pty LtdInventors: Raymond Nadeson, Adam Paul Tucker, Colin Goodchild
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Publication number: 20120232098Abstract: The invention provides methods for treatment of acute coronary syndrome and prediction of adverse cardiac events on the basis of elevations of catalytic iron in biological fluid of a human subject. An embodiment of the invention provides a method for early detection of acute coronary syndrome (ACS) in a human subject at the time of presentation of the chest pain. The method includes analyzing a test sample of the biological fluid for amount of catalytic iron and detecting acute coronary syndrome in the human subject.Type: ApplicationFiled: May 21, 2012Publication date: September 13, 2012Inventors: Mohan Rajapurkar, Suhas Lele, Sudhir Shah
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Publication number: 20120225891Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: March 22, 2012Publication date: September 6, 2012Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Publication number: 20120225093Abstract: The present invention relates to compositions and methods of treating, inhibiting, or controlling HIV infection.Type: ApplicationFiled: October 11, 2011Publication date: September 6, 2012Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Michael B. Mathews, Hartmut M. Hanauske-Abel, Tsafi Pe'ery, Mainul Hoque, Paul Palumbo, Deepti Saxena, Darlene D'Alliessi-Gandolfi, Myung-Hee Park
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Publication number: 20120225890Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: March 6, 2012Publication date: September 6, 2012Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, David Larsen, David L. Coffen, Charlotte Coffen
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Publication number: 20120202781Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: ApplicationFiled: April 8, 2010Publication date: August 9, 2012Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
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Publication number: 20120196901Abstract: The present invention is directed to tertiary amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 22, 2010Publication date: August 2, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
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Publication number: 20120196900Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: ApplicationFiled: April 16, 2012Publication date: August 2, 2012Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20120196918Abstract: Pancreatic islet dysfunction, in both type 1 and type 2 diabetes results, in part, from cytokine-mediated inflammation leading to iNOS generation and the death of pancreatic islets. The production of pro-inflammatory cytokines involved in the generation of iNOS is facilitated by the availability of the hypusine-containing translational factor eIF5A, necessary for the maturation of antigen-presenting cells. Treatment with agents capable of interfering with the mRNA translating iNOS or with agents that can interfere with the hypusination of eIF5A, prevents the death of islets, lowers blood glucose levels, avoids insulin resistance, and generally avoids the inflammatory response in islets associated with type 1 and type 2 diabetes.Type: ApplicationFiled: April 8, 2010Publication date: August 2, 2012Inventors: Raghavendra G. Mirmira, Bernhard Maier
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Publication number: 20120190684Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: ApplicationFiled: July 22, 2011Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Publication number: 20120177634Abstract: This disclosure concerns novel demethylpenclomedine analogs. Also disclosed are pharmaceutical compositions and methods for using such compositions to treat hyperproliferative disorders.Type: ApplicationFiled: February 22, 2012Publication date: July 12, 2012Inventor: Lee Roy Morgan
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Patent number: 8202892Abstract: Cosmetic composition comprising at least one compound from advanced glycation end products (‘AGEs’) and/or precursors thereof as an agent for skin treatment, especially for protection and/or care of the skin. The present invention further provides a cosmetic composition comprising at least one compound from the group of the AGEs and/or precursors thereof, wherein the AGEs are prepared by reacting sugars with the amino acids lysine and/or arginine.Type: GrantFiled: January 7, 2010Date of Patent: June 19, 2012Assignee: Henkel AG & Co. KGaAInventors: Ursula Huchel, Christian Kropf, Thomas Welss, Melanie Giesen, Andreas Bock
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Publication number: 20120136002Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: May 18, 2010Publication date: May 31, 2012Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Publication number: 20120135002Abstract: The present invention relates to a pharmaceutical composition comprising: a) at least one iron uptake inhibitor, and b) at least one vitamin D and/or at least one analog thereof and/or at least one vitamin D receptor modulator, and optionally a pharmaceutically acceptable carrier.Type: ApplicationFiled: July 16, 2009Publication date: May 31, 2012Inventors: Ivan Cruz Moura, Olivier Hermine, Celine Callens, Severine Coulon
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Patent number: 8183266Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.Type: GrantFiled: June 4, 2008Date of Patent: May 22, 2012Assignee: Intra-Cellular Therapies, Inc.Inventors: Lawrence P. Wennogle, Peng Li, Jun Zhao
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Patent number: 8163781Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R5, A, B, Q, W, and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: August 13, 2009Date of Patent: April 24, 2012Assignee: Hoffman-La Roche Inc.Inventors: Jean-Baptiste Blanc, Li Chen, Fariborz Firooznia, Paul Gillespie, Robert Alan Goodnow, Jr., Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
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Publication number: 20120095058Abstract: The present invention discloses compounds and pharmaceutical compositions which are highly effective at inhibiting the accumulation of spliced and unspliced viral transcripts and their utilization for viral protein synthesis at cellular ribosomes, and at inhibiting the formation of the hypusine residue in cellular eIF-5A precursor proteins, the cellular cofactors that render spliced and unspliced viral transcripts translatable at the ribosomes of infectled cells. The invention further relates to methods of using such compounds and pharmaceutical compositions therefrom for inhibiting or preventing viral protein synthesis. Such inhibition cause a dose-dependent release from the virally induced arrest of the otherwise genetically preprogrammed apoptosis of virally infected cells, and in consequence, triggers their apoptotic ablation and the eradication of the chronic infection-mediating provirus integrated into their genome.Type: ApplicationFiled: December 1, 2004Publication date: April 19, 2012Inventors: H., M. Hanauske-Abel, Paul Palumbo, B., M. Cracchiolo, Myung-Hee Park, Edith Wolff, Axel-Rainer Hanauske, Michael B. Mathews, Deepti Saxena, Mainul Hoque
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Publication number: 20120095061Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.Type: ApplicationFiled: September 26, 2011Publication date: April 19, 2012Applicant: APOTEX TECHNOLOGIES INC.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng WANG, Yanqing Zhao
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Publication number: 20120093917Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical inhibitors of DNA repair proteins (Metnase) and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols.Type: ApplicationFiled: March 31, 2010Publication date: April 19, 2012Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray
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Patent number: 8158654Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: May 19, 2009Date of Patent: April 17, 2012Assignee: The University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20120077852Abstract: The application of hydroxypyridonone in effective amounts as external agent for patients suffering from skin micro-circulatory disorders (SMD) provides for a significant amelioration of subject conditions. Accordingly, the new use of hydroxypyridonones as external anti-inflammatory agent thereby combined with the depletion of hemosiderin residues offers a suitable treatment to SMD sufferers.Type: ApplicationFiled: December 1, 2011Publication date: March 29, 2012Inventor: Ghisalberti CARLO
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Patent number: 8138166Abstract: The present invention discloses a method to induce fatty liver in an animal. The steps of the method comprise: feeding an animal with a high calorie diet, and injecting a mitochondrial inhibitor into the animal to inhibit the mitochondrial activity of the animal, then resulting in fat accumulation and inflammation in the liver of the animal.Type: GrantFiled: July 8, 2010Date of Patent: March 20, 2012Assignee: Taipei Medical UniversityInventors: Rong-Hong Hsieh, Sheng-Mei Lin