Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
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Publication number: 20100249195Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: March 29, 2010Publication date: September 30, 2010Applicant: Synta Pharmaceuticals CorpInventors: Jun Jiang, Zhi-Qiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
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Publication number: 20100247468Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: ApplicationFiled: September 21, 2009Publication date: September 30, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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Publication number: 20100240677Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: ApplicationFiled: January 26, 2010Publication date: September 23, 2010Applicant: AVENTIS PHARMA LIMITEDInventors: Garry FENTON, Tahir Nadeem MAJID, Malcolm Norman PALFREYMAN
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Publication number: 20100240652Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.Type: ApplicationFiled: January 15, 2007Publication date: September 23, 2010Inventors: Karl Richard Gibson, Melanie Susanne Glossop
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Publication number: 20100239632Abstract: Effective treatments of pain and/or inflammation are provided. Through the administration of a biodegradable drug depot film, patch, strip or sponge being implantable at or near a cardiac tissue or within a nasal or sinus cavity, one can reduce, prevent or treat pain and/or inflammation.Type: ApplicationFiled: March 23, 2009Publication date: September 23, 2010Applicant: Warsaw Orthopedic, Inc.Inventor: Andrew J. Lowenthal WALSH
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Publication number: 20100240711Abstract: A preparation which can improve solubility of a NPYY5 receptor antagonist in water, even when the NPYY5 receptor antagonist is contained in the preparation at a high content is provided. A solid preparation containing a NPYY5 receptor antagonist, an amorphous stabilizer, and optionally an amorphousization inducing agent. Particularly, when the amorphous stabilizer is hydroxypropylmethylcellulose phthalate and/or hydroxypropylmethylcellulose acetate succinate, and the amorphousization inducing agent is urea and/or saccharine sodium at an addition amount of less than 8% by weight, dissolution out property of a water-hardly soluble NPYY5 receptor antagonist could be improved.Type: ApplicationFiled: September 18, 2008Publication date: September 23, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Masatoshi Takada, Yuki Murakami, Shunji Ichio, Minako Fujii, Asako Takakura, Takeshi Funaki
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Publication number: 20100234373Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: Amgen Inc.Inventors: Erin F. Dimauro, Jean E. Bemis, Stuart C. Chaffee, Ning Chen, Essa Hu, Roxanne Kunz, Matthew W. Martin, David C. McGowan, Shannon Rumfelt
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Publication number: 20100233185Abstract: Provided are methods, test devices, and diagnostic kits for predicting, assessing, and diagnosing the risk of a disease using salivary analysis. The methods comprise providing a whole (unfractionated) saliva sample from a subject; contacting an aliquot of the saliva with two or more lectins under conditions that allow the two or more lectins to bind to a lectin-binding component of the saliva; detecting the amount of bound lectin; and comparing the amount of bound lectin to the amount known to bind a saliva sample from a control patient, to predict the risk of a disease in the subject. Also provided are methods for reducing the risk of a disease and a method for assessing the risk of the disease at a defined level.Type: ApplicationFiled: May 24, 2010Publication date: September 16, 2010Inventors: Patricia Denny, Paul C. Denny, Mahvash Navazesh
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Publication number: 20100234432Abstract: The present application relates to novel substituted 6-phenylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, in particular dyslipidaemias, arteriosclerosis and heart failure.Type: ApplicationFiled: August 26, 2008Publication date: September 16, 2010Applicant: BAYER ANIMAL HEALTH GMBHInventors: Lars Baerfacker, Barbara Albrecht-Kuepper, Peter Kolkhof, Yolanda Cancho Grande, Adam Nitsche, Heinrich Meier, Carsten Schmeck, Jens Schamberger, Klemens Lustig
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Publication number: 20100234379Abstract: The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor. Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury.Type: ApplicationFiled: July 28, 2006Publication date: September 16, 2010Inventors: Ben A. Bahr, Alexandros Makriyannis, David A. Karanian
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Publication number: 20100234358Abstract: The present invention relates to the treatment of an individual diagnosed with nystagmus comprising administering to the individual an effective amount of a 1-aminoalkylcyclohexane derivative, for example neramexane or a pharmaceutically acceptable salt thereof, such as neramexane mesylate.Type: ApplicationFiled: June 6, 2008Publication date: September 16, 2010Applicant: MERZ PHARMA GMBH & CO. KGAAInventors: Angelika Hanschmann, Michael Althaus, Albrecht Stoffler
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Patent number: 7795315Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.Type: GrantFiled: January 23, 2009Date of Patent: September 14, 2010Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Yun He, Jason Christopher Wong
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Publication number: 20100226993Abstract: A composition for regenerative treatment of cartilage disease, which comprises a PDE4 inhibitor as an active ingredient, specifically a composition comprising a PDE4 inhibitor and a biocompatible and biodegradable polymer is provided, which composition, when formulated into a form suited to administer locally to affected cartilage region, such as microsphere preparation, can provide a pharmaceutical composition showing an excellent effect in regenerative treatment of cartilage.Type: ApplicationFiled: May 18, 2010Publication date: September 9, 2010Inventors: Masaharu TAKIGAWA, Naoki Sakurai, Toshiki Takagi, Noriyuki Yanaka, Yuji Horikiri, Takashi Tamura
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Publication number: 20100227888Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 19, 2010Publication date: September 9, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
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Publication number: 20100222217Abstract: N-[2-(Haloalkoxy)phenyl]heteroarylcarboxamides of the formula I, where n=0 or 1, Hal=halogen, X=C2-C4-haloalkyl, Het=a pyrazole, thiazole or pyridine radical (a), (b) or (c), where R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, R3=C1-C4-alkyl or C1-C4-haloalkyl and R5=halogen, C1-C4-alkyl or C1-C4-haloalkyl; except for N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-1,3-dimethylpyrazol-4-yl-carboxamide, N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-trifluoromethyl-1-methylpyrazol-4-yl-carboxamide and N-[2-(2,2,2-trifluorethoxy)phenyl]-3-trifluormethyl-1-methylpyrazol-4-yl-carboxamide. A fungicidal composition comprising at least one compound I, the use of the compounds I for preparing a composition suitable for controlling harmful fungi, a method for controlling harmful fungi using the compounds I and also seed comprising at least one compound I.Type: ApplicationFiled: August 2, 2006Publication date: September 2, 2010Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann
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Patent number: 7786167Abstract: The present invention provides compositions and methods for administering florfenicol to mammals. The compositions contain a prodrug of florfenicol in a pharmaceutically acceptable carrier. In one embodiment the prodrug is an esterized form of florfenicol. Examples of suitable prodrugs include one or a combination of one or a combination of the following: florfenicol acetate, florfenicol propionate, florfenicol butyrate, florfenicol pentanoate, florfenicol hexanoate, florfenicol heptanoate, florfenicol octanoate, florfenicol nanoate, florfenicol decanoate, florfenicol undecanoate, florfenicol dodecanoate, and florfenicol phthalate. In another embodiment the prodrug is converted into the florfenicol in vivo by the action of one or more endogenous esterases. The invention also provides new compounds, pharmaceutical compositions containing the compounds, and methods for their administration.Type: GrantFiled: October 10, 2007Date of Patent: August 31, 2010Assignee: IDEXX Laboratories, Inc.Inventors: Yerramilli V. S. N. Murthy, Robert H. Suva
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Patent number: 7786097Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: GrantFiled: July 21, 2009Date of Patent: August 31, 2010Assignee: Pfizer Inc.Inventors: Hengmiao (Henry) Cheng, Rajesh Devraj, Gary A Decresenzo, Xiao Hu, Kevin D. Jerome, Mark Obukowicz, Lisa Olson, Paul V. Rucker, Ronald Keith Webber
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Patent number: 7786147Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.Type: GrantFiled: March 9, 2005Date of Patent: August 31, 2010Assignees: Medical College of Georgia Research Institute., University of Georgia Research Foundation, Inc.Inventors: Jerry J. Buccafusco, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
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Publication number: 20100216778Abstract: Since a ROCK inhibitor exerts a potent analgesic effect by a single dose after the onset of a cartilage-related disease such as osteoarthritis, and can regenerate or suppress destruction of cartilage tissue and alleviate pain associated with cartilage diseases by multiple doses, administration of an therapeutically effective amount of the ROCK inhibitor to a patient with cartilage-related disease such as osteoarthritis or rheumatoid arthritis can treat the patient with cartilage-related disease and the ROCK inhibitor is thus useful.Type: ApplicationFiled: March 1, 2010Publication date: August 26, 2010Applicant: Astellas Pharma Inc.Inventor: Nobuaki TAKESHITA
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Patent number: 7781461Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: September 14, 2006Date of Patent: August 24, 2010Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Publication number: 20100210692Abstract: Methods of treatment using SIR1 modulators and compositions containing SIRT1 modulators are described. Combinations of a SIRT1 modulator and a second agent, and uses of such combinations, are also described.Type: ApplicationFiled: March 28, 2008Publication date: August 19, 2010Inventors: Stephen R. Farmer, Hong Wang, Li Qiang
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Publication number: 20100210638Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: April 28, 2010Publication date: August 19, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20100210693Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: May 3, 2010Publication date: August 19, 2010Inventors: Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
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Patent number: 7776893Abstract: The invention relates to the use of certain known PIDE4 inhibitors for the treatment of diabetes mellitus and accompanying disorders thereof.Type: GrantFiled: September 2, 2004Date of Patent: August 17, 2010Assignee: NYCOMED GmbHInventor: Hans-Peter Kley
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Publication number: 20100203051Abstract: Disclosed are methods and agents for detecting the presence or diagnosing the risk of ankylosing spondylitis (AS) in mammals. These methods are based on the detection of polymorphisms within any one or more of the ARTS-1 gene, the IL-23R gene, the TNFR1 gene locus, the TRADD gene locus and the chromosome loci 2P15 and 21Q22. The present invention also features methods for the treatment or prevention of AS based on the diagnosis.Type: ApplicationFiled: May 29, 2008Publication date: August 12, 2010Applicant: THE UNIVERSITY OF QUEENSLANDInventor: Matthew Arthur Brown
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Publication number: 20100190788Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: July 29, 2010Inventors: Olivier Defert, Philippe Van Rompaey, Petra Blom, Dirk Leysen, Gert De Wilde, Thomas Brown
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Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20100183606Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Inventors: ROBERT M BORZILLERI, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Patent number: 7754739Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: May 9, 2008Date of Patent: July 13, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
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Publication number: 20100168136Abstract: A compound having activity to inhibit production and/or secretion of ?-amyloid protein, and is useful for prevention and/or treatment of various diseases associated with abnormal production and/or secretion of ?-amyloid protein, the compound represented by the general formula (I): [wherein, R1 represents a C1-C6 alkyl group which may have 1 to 6 halogen atoms as substituent groups, a C2-C6 alkenyl group which may have 1 to 6 halogen atoms as substituent groups, or a C3-C7 cycloalkyl group which may have 1 to 6 halogen atoms as substituent groups; R2 represents a 6-membered nitrogen-containing monocyclic aromatic heterocyclic group having 1 to 3 substituent groups, or a 9- or 10-membered nitrogen-containing bicyclic heterocyclic group having 1 to 4 substituent groups; Z1, Z2 and Z3 each independently represent a hydrogen atom, a halogen atom or a cyano group; and n represents 0, 1 or 2], salts thereof, or solvates thereof.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hitoshi Iimori, Hideki Kubota, Satoru Miyauchi, Kayoko Motoki
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Publication number: 20100168102Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: July 1, 2010Applicant: Devgen NVInventors: Olivier Raynald Defert, Gert De Wilde, Petra Blom, Dirk Casimir Maria Leysen, Thomas Brown, Nadzeya Kaval
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Publication number: 20100168089Abstract: An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne.Type: ApplicationFiled: December 17, 2009Publication date: July 1, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: JÉRÔME AUBERT, ISABELLE CARLAVAN, JOHANNES VOEGEL
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Publication number: 20100160391Abstract: The present invention provides conjugates comprising a substituted aminopyridine covalently attached to an organic molecule via an amide bond. Such conjugates find utility as substrates for amide hydrolases, where the substituted aminopyridine acts as a fluorescent reporter of amide hydrolase activity. As a result, the conjugates described herein can advantageously be used in assays to detect amide hydrolase activity based upon measuring the fluorescence of a substituted aminopyridine that is released after amide hydrolysis. The conjugates of the present invention are also particularly useful in screening assays, which enable the identification of inhibitory molecules for amide hydrolases and other enzymes. The identified amide hydrolase inhibitors can be used in the treatment of a variety of diseases and disorders associated with aberrant amide hydrolase activity.Type: ApplicationFiled: July 9, 2007Publication date: June 24, 2010Inventors: Bruce D. Hammock, Huazhang Huang, Kosuke Nishi
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Publication number: 20100158993Abstract: Topical alcoholic gel compositions are disclosed that are useful for delivering therapeutic levels of an NSAID to target in and below the skin. The compositions comprise a topically active drug, an alcoholic solvent, a polymeric thickener, and optionally a keratolytic agent. In one embodiment, excellent viscosity for dermal application is attained without the need of a step for neutralizing the pH of the composition. Alcoholic and alcohol-free topical compositions comprising an NSAID prodrug are also disclosed. The compositions are particularly useful for the treatment of pseudofolliculitis barbae.Type: ApplicationFiled: December 21, 2009Publication date: June 24, 2010Applicant: ISW Group, Inc.Inventors: Monique Spann-Wade, Anthony Ward
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Publication number: 20100152253Abstract: The present invention relates to non-steroidal mimetics of brassinosteroids. More specifically, it relates to non-steroidal monocyclic compounds, capable of rescuing the brassinosteroid receptor null mutation bri1-116. Preferably, said compounds are low molecular weight, monocyclic halogenated compound.Type: ApplicationFiled: October 9, 2007Publication date: June 17, 2010Applicants: VIB VZW, Universiteit GentInventors: Dominique Audenaert, Tom Beeckman, Bert De Rybel, Jenny Russinova, Dirk G. Inze
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Publication number: 20100150868Abstract: A method of individually optimizing a treatment for an inflammation associated disease is provided. The method comprising contacting each of identical white blood cell samples of a subject in need thereof with a different pharmaceutical agent of a plurality of pharmaceutical agents for the inflammation associated disease, so as to allow elicitation of an anti-inflammatory activity in the white blood cell samples; assaying the anti-inflammatory activity in the white blood cell samples; and identifying a pharmaceutical agent of the plurality of pharmaceutical agents eliciting a strongest anti-inflammatory activity, the pharmaceutical agent being the individually optimized treatment for the inflammation associated disease, wherein when the inflammation associated disease is multiple sclerosis the white blood cell samples are inflamed white blood cell samples. Methods of treating an inflammation associated disease are also described.Type: ApplicationFiled: March 21, 2006Publication date: June 17, 2010Applicant: Tel HaShomer Medical Research Infrastructure and Services Ltd.Inventors: Anat Achiron, Michael Gurevich
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Publication number: 20100144799Abstract: The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesizing such enantiomers by means of a styrene oxide based synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits.Type: ApplicationFiled: February 16, 2010Publication date: June 10, 2010Applicant: FERMENTA BIOTECH (UK) LIMITEDInventors: Anupama Datla, Pramod Abaji Walavalker, Ashok Konda, Sreenath Babunath Trivikram
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Publication number: 20100144718Abstract: The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 17, 2009Publication date: June 10, 2010Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
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Publication number: 20100143347Abstract: The present invention concerns protection of an organ or tissue following an ischemic episode In particular aspects, the invention concerns organ preservation for transplantation, angina pectoris, kidney reperfusion injury, and so forth In specific embodiments, the organ is subjected to an inhibitor of an NCCa-ATP channel that is regulated by SUR1 Exemplary inhibitors include sulfonylurea compounds, such as glibenclamide, for exampleType: ApplicationFiled: January 11, 2008Publication date: June 10, 2010Inventor: J. Marc Simard
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Publication number: 20100144741Abstract: The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: November 22, 2007Publication date: June 10, 2010Inventors: Mathias Frederiksen, Rainer Martin Luond, Clive McCarthy, Henrik Moebitz, Jean-Michel Rondeau, Bernard Lucien Roy, Heinrich Rueeger
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Publication number: 20100137376Abstract: Disclosed is a plant disease control agent containing an amide compound represented by formula (1) below which has an excellent plant disease controlling effect as an active ingredient. (In the formula, X1, X2, Z1 and E1 are as defined in the description.Type: ApplicationFiled: July 11, 2008Publication date: June 3, 2010Inventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
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Patent number: 7727996Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: September 28, 2006Date of Patent: June 1, 2010Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Publication number: 20100130522Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.Type: ApplicationFiled: October 1, 2009Publication date: May 27, 2010Applicant: Synta Pharmaceuticals Corp.Inventors: JUN JIANG, Junyi Zhang, Shoujun Chen, Lijun Sun
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Publication number: 20100130503Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R2?, L, Het, p and p? are as defined herein, compositions containing them, and their use as medicinal products.Type: ApplicationFiled: November 24, 2009Publication date: May 27, 2010Applicant: SANOFI-AVENTISInventors: Fabienne THOMPSON, Patrick MAILLIET, Jean-Marie RUXER, Helene GOULAOUIC, François VALLEE, Herve MINOUX, Fabienne PILORGE, Luc BERTIN, Stephane HOURCADE, Maria MENDEZ-PEREZ, Peter HAMLEY
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Patent number: 7723364Abstract: Compound of general formula (I): Process for preparing this compound. Fungicidal composition comprising a compound of general formula (I). Method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: July 19, 2004Date of Patent: May 25, 2010Assignee: Bayer Cropscience SAInventors: Darren James Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier, Isabelle Christian
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Publication number: 20100120780Abstract: Provided are methods and compositions for the treatment of a sexual dysfunction such as premature ejaculation. In certain embodiments, a NMDA antagonist (e.g., dextromethorphan) is administered to a subject in combination with tramadol or a tramadol derivative to treat premature ejaculation. In certain embodiments, a capsaicinoid (e.g., capsaicin) and/or a phosphodiesterase type V inhibitor (e.g., sildenafil citrate) are further administered to the subject. Pharmaceutical preparations such as tablets and capsules are provided.Type: ApplicationFiled: April 18, 2008Publication date: May 13, 2010Inventor: Chandra Ulagaraj Singh
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Publication number: 20100113429Abstract: The invention relates to inhibitors of FtsZ polymerization and uses thereof.Type: ApplicationFiled: December 31, 2009Publication date: May 6, 2010Inventors: E. Lucile White, Robert C. Reynolds, William J. Suling
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Publication number: 20100112048Abstract: The present invention relates to a synergistic combination for preventing the onset and/or progression of dementia or Alzheimer's disease in individuals at increased risk thereof for example because of family history, genetic factors, and/or environmental factors. This combination comprises synergistically effective amounts of vitamin C, vitamin E, DHA and at least one NSAID such as ibuprofen.Type: ApplicationFiled: July 19, 2006Publication date: May 6, 2010Inventor: Majid Fotuhi
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Patent number: 7704995Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.Type: GrantFiled: May 2, 2003Date of Patent: April 27, 2010Assignee: Exelixis, Inc.Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
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Publication number: 20100099689Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: ApplicationFiled: September 18, 2009Publication date: April 22, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence CLARY, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel