Plural Hetero Atoms In The Hetero Ring Patents (Class 514/439)
-
Patent number: 9044439Abstract: Compositions containing low doses of lipoic acid-based active agents and methods for using the same are provided. In particular, compositions containing low dose lipoic acid, lipoic acid derivatives, and lipoic acid seleno-derivatives and are provided to prevent and/or treat ocular diseases.Type: GrantFiled: November 7, 2008Date of Patent: June 2, 2015Assignee: Encore Health, LLCInventors: William Garner, Margaret Garner
-
Patent number: 8916183Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: GrantFiled: January 22, 2013Date of Patent: December 23, 2014Assignee: Dow AgroSciences, LLC.Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
-
Patent number: 8901176Abstract: New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.Type: GrantFiled: August 24, 2012Date of Patent: December 2, 2014Assignee: Newron Pharmaceuticals, S.P.A.Inventors: Ruggero Fariello, Carlo Cattaneo, Patricia Salvati, Luca Benatti
-
Patent number: 8883180Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: GrantFiled: August 29, 2013Date of Patent: November 11, 2014Assignee: Bayer Intellectual Property GmbHInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
-
Patent number: 8859612Abstract: The invention relates to the use of the compound hesperidin or of one of its derivatives for the manufacture of a composition designed to stimulate bone formation and/or inhibit bone resorption in man or animals.Type: GrantFiled: June 27, 2003Date of Patent: October 14, 2014Assignee: Institut National de la Recherche Agronomique (INRA)Inventors: Marie-Noëlle Horcajada, Véronique Coxam, Christine Morand, Marie-Jeanne Davicco
-
Patent number: 8828908Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: May 27, 2008Date of Patent: September 9, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
-
Publication number: 20140100242Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: September 17, 2013Publication date: April 10, 2014Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Bonnie Bassler, Lee Swem
-
Patent number: 8673963Abstract: The present invention is directed to provide an efficient production method which is capable of not only obtaining a cyclic sulfonic acid ester (sultone) at low cost and in high yield, but also the sulfonic acid ester (sultone) stably even in a commercial scale. The present invention relates to a method for producing hydroxysultone comprising a first step where a diol having a specified structure and a thionyl halide are reacted to obtain a cyclic sulfite having a specified structure, and a second step where the cyclic sulfite is reacted with water or/and alcohol; a method for producing an unsaturated sultone having a specified structure comprising a third step where a hydroxylsultone having a specified structure is reacted with an acid halide or an acid anhydride to obtain an intermediate, subsequently the intermediate is treated with a base; as well as a cyclic sulfite having a specified structure.Type: GrantFiled: August 3, 2010Date of Patent: March 18, 2014Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Ayako Kuramoto, Kuniaki Okamoto, Tsutomu Watahiki, Motoshige Sumino
-
Patent number: 8592466Abstract: Treatment of humans suffering from conditions caused by higher-than-normal dopaminergic activity in basal ganglia includes administering the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.Type: GrantFiled: July 18, 2012Date of Patent: November 26, 2013Assignee: Neuropill, Inc.Inventor: Ahmed Elkashef
-
Patent number: 8568756Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: GrantFiled: June 2, 2009Date of Patent: October 29, 2013Assignee: The Trustees of Princeton UniversityInventors: Bonnie Bassler, Lee Swem
-
Patent number: 8541466Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.Type: GrantFiled: August 4, 2009Date of Patent: September 24, 2013Assignee: Duke UniversityInventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
-
Patent number: 8450336Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.Type: GrantFiled: December 14, 2007Date of Patent: May 28, 2013Assignee: NPS Pharmaceuticals, IncInventors: Guy Higgins, Abdelmalik Slassi, Methvin Isaac
-
Patent number: 8410162Abstract: Compounds, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.Type: GrantFiled: June 15, 2010Date of Patent: April 2, 2013Assignee: Encore Health LLCInventors: William Garner, Margaret Garner, George Minno, David Gooden
-
Publication number: 20130078233Abstract: Compounds having one or more phenol moieties, derivatives thereof, compositions containing same and uses thereof for the treatment of amyloid-associated diseases are provided.Type: ApplicationFiled: November 27, 2012Publication date: March 28, 2013Applicant: Tel Aviv University Future Technology Development L.P.Inventor: Tel Aviv University Future Technology Development
-
Patent number: 8372880Abstract: Compounds having one or more phenol moieties, derivatives thereof, compositions containing same and uses thereof for the treatment of amyloid-associated diseases are provided.Type: GrantFiled: March 23, 2006Date of Patent: February 12, 2013Assignee: Tel Aviv University Future Technology Development L.P.Inventors: Ehud Gazit, Yair Porat
-
Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
-
Patent number: 8318785Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.Type: GrantFiled: July 17, 2006Date of Patent: November 27, 2012Assignee: Orion CorporationInventors: Marko Ahlmark, Reijo Bäckström, Anne Luiro, Jarmo Pystynen, Eija Tiainen
-
Patent number: 8282952Abstract: The invention relates to insect attractants containing compounds with pentagonal heterocyclic structures that are effective in attracting fruitflies.Type: GrantFiled: March 11, 2008Date of Patent: October 9, 2012Assignee: Activetrad (Proprietary) LimitedInventor: Christoffel J. Smit
-
Patent number: 8268862Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: January 24, 2011Date of Patent: September 18, 2012Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
-
Patent number: 8263640Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.Type: GrantFiled: June 1, 2010Date of Patent: September 11, 2012Assignee: NUtech VenturesInventors: Concetta Dirusso, Paul Black
-
Patent number: 8247438Abstract: Treatment of schizophrenia or humans suffering from conditions associated with high dopamine levels in ventral striatum or caudate nucleus administers the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.Type: GrantFiled: June 10, 2008Date of Patent: August 21, 2012Assignee: Neuropill, Inc.Inventor: Ahmed Elkashef
-
Patent number: 8183281Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.Type: GrantFiled: June 4, 2008Date of Patent: May 22, 2012Assignee: Novartis AGInventors: Neil John Press, Simon James Watson
-
Patent number: 8168212Abstract: Cosmetic compositions comprising non-natural, non-proteogenic amino acids and methods of using such compositions to impart antiaging benefits to the skin are disclosed. The non-natural, non-proteogenic amino acids are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging, and in particular, are enhancers of LOXL-1.Type: GrantFiled: November 14, 2008Date of Patent: May 1, 2012Assignee: Avon Products, IncInventors: Dmitri S. Ptchelintsev, Laurence Dryer, Xiaochun Luo
-
Patent number: 8143215Abstract: Compositions for enhancing satiety and weight loss in an individual, assays for assessing a tastant for enhancing satiety and weight loss, and methods of using the composition to suppress appetite and enhance weight loss are provided.Type: GrantFiled: January 16, 2009Date of Patent: March 27, 2012Inventor: Alan R. Hirsch
-
Patent number: 8119686Abstract: A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula: wherein R1a, R1b, R1c and R1d each represents a hydrogen atom, a halogen atom, an alkyl group which may have a substituent, or an alkoxy group which may have a substituent, and R2a and R2b each represents a hydrogen atom, or an alkyl group which may have a substituent (e.g.Type: GrantFiled: November 21, 2007Date of Patent: February 21, 2012Assignee: Hykes Laboratories LLCInventors: Shinji Yokoyama, Hashime Kanazawa, Tomoji Aotsuka
-
Patent number: 8030346Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: GrantFiled: April 29, 2008Date of Patent: October 4, 2011Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Roland Burli, Michael J. Frohn, Randall W. Hungate, Susana C. Neira, Anthony B. Reed
-
Patent number: 7973037Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: April 8, 2008Date of Patent: July 5, 2011Assignees: Axys Pharmaceuticals, Inc., Merck Canada Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
-
Patent number: 7968572Abstract: It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.Type: GrantFiled: October 2, 2006Date of Patent: June 28, 2011Assignee: Ono Pharmaceuticals Co., Ltd.Inventors: Hisao Nakai, Shingo Yamamoto, Shingo Nakatani, Tomomi Hirosaki
-
Publication number: 20110123586Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: June 2, 2009Publication date: May 26, 2011Inventors: Bonnie Bassler, Lee Swem
-
Patent number: 7928137Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.Type: GrantFiled: March 2, 2007Date of Patent: April 19, 2011Assignee: Tularik LimitedInventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
-
Publication number: 20110071125Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 9, 2008Publication date: March 24, 2011Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader
-
Patent number: 7893086Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: June 20, 2008Date of Patent: February 22, 2011Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
-
Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
-
Publication number: 20100317725Abstract: Compounds, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.Type: ApplicationFiled: June 15, 2010Publication date: December 16, 2010Applicant: Encore Health LLCInventors: William Garner, Margaret Garner, George Minno, Gooden David
-
Patent number: 7803796Abstract: Provided is a homopiperazine compound for inhibiting ribosomal frameshifting by binding to an RNA pseudoknot structure of SARS coronavirus. Particularly, the present invention provides a pharmaceutical composition for inhibiting synthesis of protein induced by ?1 frameshifting by binding to an RNA pseudoknot structure specifically existing in SARS coronavirus. The composition includes a therapeutically effective amount of homopiperazine compound of following chemical formula 1 or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier or excipient.Type: GrantFiled: December 20, 2007Date of Patent: September 28, 2010Assignee: Sungkyunkwan University Foundation For Corporate CollaborationInventors: Hyun-Ju Park, So-Jung Park, Yang-Gyun Kim
-
Publication number: 20100210683Abstract: There is provided a compound having an excellent controlling effect on arthropod pests represented by the formula (I-1): wherein Z represents an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; G represents a -A1-R1 group, etc.; X0 represents a -A2-R4 group, etc.; X represents a -A2-R4 group, etc.; X0 represents a -A3-R6 group, etc.; or X and X0 are optionally taken together to form a -A2-T0-A3- group; M1 represents a —R8 group, etc.; A1, A2 and A3 independently represent an oxygen atom, etc.; R1 and R8 independently represents an optionally substituted C1-C20 chain hydrocarbon group, etc.; R4 and R6 independently represent an optionally substituted C1-C6 chain hydrocarbon group, etc.; and T0 represents an optionally substituted C2-C6 alkanediyl group.Type: ApplicationFiled: July 25, 2008Publication date: August 19, 2010Applicant: SUMITOMO CHEMICAL COMPANY LIMITEDInventors: Hideo Kamiyama, Shigeyuki Itoh
-
Publication number: 20100160411Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, p, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: ApplicationFiled: October 24, 2007Publication date: June 24, 2010Applicant: WyethInventors: Gary Paul Stack, Ivana Bianchi, Stefania Vallese, Giovanna Luoni
-
Publication number: 20100029745Abstract: The present invention relates to compounds derived from substituted 3-phenyl-1-(thien-2-yl)propan-1-ones, pharmaceutical compositions comprising them as well as their therapeutic applications, notably in the field of human and animal health.Type: ApplicationFiled: December 28, 2007Publication date: February 4, 2010Inventor: Jean-Francois Delhomel
-
Publication number: 20090291102Abstract: There are provided various compounds and compositions comprising polyunsaturated fatty acid monoglycerides and derivatives thereof. These compounds and compositions can be useful as cancer chemopreventive agents. They can also be useful for enhancing solubility of various active agents and enhancing their bioavailability.Type: ApplicationFiled: August 5, 2009Publication date: November 26, 2009Inventor: Samuel FORTIN
-
Publication number: 20090192212Abstract: Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract.Type: ApplicationFiled: February 23, 2009Publication date: July 30, 2009Applicant: Encore Health, LLCInventors: William Garner, Margaret Garner, Ronald D. Blum
-
Publication number: 20090176805Abstract: The present application discloses derivatives of ethylene methanedisulfonate as cancer chemotherapeutic agents and methods of synthesizing such derivatives. The derivatives include modifications of ethylene methanedisulfonate by replacing one or both of the chemically most reactive hydrogens of the cyclic sulfonate ester structure. The derivatives of ethylene methanedisulfonate are more active than the parent ester (i.e., ethylene methanedisulfonate) as anticancer agents against a variety of cancers.Type: ApplicationFiled: November 26, 2008Publication date: July 9, 2009Inventors: Marshall W. Cronyn, Gail Marie Cronyn, Lori Ruth Cronyn
-
Publication number: 20090048315Abstract: A composition having sustained pain-relieving properties such that the composition may be administered to a subject to alleviate chronic pain. The composition includes an effective amount of at least one glutaminase inhibitor. A method for alleviating chronic pain in a subject for an extended period of time is also disclosed, in which the compound is administered to a subject suffering from chronic pain at a site of inflammation such that the administration of the compound results in a reduction in at least one of thermal and mechanical pain responses at the site of inflammation for a period of at least two days without any resulting acute pain behavior. The composition may further include an effective amount of at least one compound having analgesic effects such that the composition also alleviates acute pain.Type: ApplicationFiled: May 9, 2006Publication date: February 19, 2009Inventor: Kenneth E. Miller
-
Patent number: 7435834Abstract: The present invention relates to compounds of 2-thia-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-?(TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: April 9, 2003Date of Patent: October 14, 2008Assignee: GlaxoSmithKline Istrazivacki Center Zagreb D.O.O.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic, Ivana Ozimec
-
Patent number: 7417156Abstract: In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities.Type: GrantFiled: September 26, 2003Date of Patent: August 26, 2008Assignee: Johns Hopkins UniversityInventors: Gary H. Posner, Theresa A. Shapiro, Surojit Sur, Tanzina Labonte, Kristina Borstnik, Ik-Hyeon Paik, Andrew J. McRiner
-
Patent number: 7407987Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.Type: GrantFiled: November 30, 2006Date of Patent: August 5, 2008Assignee: Duke UniversityInventors: Mitchell Anthony deLong, John McMillan McIver, Robert Scott Youngquist
-
Patent number: 7388029Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.Type: GrantFiled: May 26, 2005Date of Patent: June 17, 2008Assignee: Duke UniversityInventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
-
Patent number: 7335673Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient.Type: GrantFiled: August 10, 2001Date of Patent: February 26, 2008Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Yoichiro Hoshina, Satoru Ikegami, Akihiko Okuyama, Tatsuhiro Harada, Atsushi Matsuo
-
Patent number: 7288246Abstract: A composition having sustained pain-relieving properties such that the composition may be administered to a subject to alleviate chronic pain. The composition includes an effective amount of at least one glutaminase inhibitor. A method for alleviating chronic pain in a subject for an extended period of time is also disclosed, in which the compound is administered to a subject suffering from chronic pain at a site of inflammation such that the administration of the compound results in a reduction in at least one of thermal and mechanical pain responses at the site of inflammation for a period of at least two days without any resulting acute pain behavior. The composition may further include an effective amount of at least one compound having analgesic effects such that the composition also alleviates acute pain.Type: GrantFiled: September 13, 2002Date of Patent: October 30, 2007Assignee: The Board of Regents of the University of OklahomaInventor: Kenneth E. Miller
-
Patent number: 7262309Abstract: The present invention relates to benzonaphthoazulene derivatives of tiophene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumor necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: October 12, 2004Date of Patent: August 28, 2007Assignee: GlaxoSmith Kline Istrazivocki Centar Zagreb, D.O.O.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic, Ivana Ozimec, Rudolf Trojko
-
Patent number: RE40558Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: October 20, 2005Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko