The Cyano Is Bonded Directly To A Benzene Ring Patents (Class 514/522)
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Publication number: 20130324602Abstract: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.Type: ApplicationFiled: April 23, 2013Publication date: December 5, 2013Inventors: James T. DALTON, Duane D. MILLER
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Publication number: 20130296422Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(?O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.Type: ApplicationFiled: November 1, 2011Publication date: November 7, 2013Applicant: ARIGEN PHARMACEUTICALS, INC.Inventors: Hiroyuki Saimoto, Kiyoshi Kita, Yoshisada Yabu, Masaichi Yamamoto
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Publication number: 20130281444Abstract: The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II: and the synthesis and the application thereof.Type: ApplicationFiled: August 9, 2012Publication date: October 24, 2013Inventors: Deh-Ming CHANG, Hsu-Shan HUNAG, Chia-Chung LEE, Chun-Liang CHEN
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Patent number: 8563606Abstract: The present invention relates to solid forms of (S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.Type: GrantFiled: June 5, 2011Date of Patent: October 22, 2013Assignee: GTx, Inc.Inventors: James T. Dalton, David A. Dickason, Seoung-Soo Hong, Thomas G. Bird, Tai Ahn
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Patent number: 8557282Abstract: The present invention relates to an extended release composition comprising as active compound Venlafaxine Hydrochloride, in which Venlafaxine Hydrochloride is coated on a non pareil inert core, which coated core is then coated with polymeric layer which enables the controlled release of the Venlafaxine Hydrochloride.Type: GrantFiled: November 21, 2011Date of Patent: October 15, 2013Assignee: Lycored Bio Ltd.Inventor: Yoram Sela
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Patent number: 8546448Abstract: A process for forming a solid electrolytic capacitor and an electrolytic capacitor formed by the process. The process includes: providing an anode wherein the anode comprises a porous body and an anode wire extending from the porous body; applying a thin polymer layer onto the dielectric, and forming a dielectric on the porous body to form an anodized anode; applying a first slurry to the anodized anode to form a blocking layer wherein the first slurry comprises a first conducting polymer with an median particle size of at least 0.05 ?m forming a layer of crosslinker on the blocking layer; and applying a layer of a second conducting polymer on the layer of crosslinker.Type: GrantFiled: September 15, 2011Date of Patent: October 1, 2013Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. von Borstel, Ramchandran Arudchandran, Rita O'Neil
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Publication number: 20130244962Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.Type: ApplicationFiled: April 11, 2013Publication date: September 19, 2013Applicant: Merck Frosst Canada Ltd.Inventors: Elise ISABEL, Christopher MELLON, Christian BEAULIEU
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Publication number: 20130231362Abstract: The present invention is directed to methods of treating or preventing the development of obesity by administering compounds that stabilize mast cells. In addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing obesity.Type: ApplicationFiled: April 15, 2013Publication date: September 5, 2013Applicant: The Brigham and Women's Hospital, IncInventor: Guo-Ping Shi
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Publication number: 20130225610Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Inventor: Marc Hansen
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Publication number: 20130225621Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: August 29, 2013Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.Inventors: James Turkson, Patrick Gunning
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Publication number: 20130190396Abstract: Therapeutic ureido-sulfonamide compositions having compounds with the formula R-Q-Ar—SO2NH2 are disclosed, which compounds selectively inhibit CAIX and CAXII, and which are effective to inhibit hypoxic tumor growth, suppress metastases, and impair and deplete cancer stem cells in mammals.Type: ApplicationFiled: January 9, 2013Publication date: July 25, 2013Applicant: METASIGNAL THERAPEUTICS INC.Inventor: METASIGNAL THERAPEUTICS INC.
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Publication number: 20130184343Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: March 4, 2013Publication date: July 18, 2013Applicants: Syngenta Crop Protection LLC, Syngenta Participations AGInventor: Syngenta Participations AG
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Patent number: 8486381Abstract: The present invention relates to methods for treating intestinal fluid balance disorders and modulating intestinal fluid secretion and absorption using calcimimetics and calcilytics.Type: GrantFiled: August 28, 2006Date of Patent: July 16, 2013Assignee: Amgen Inc.Inventors: John Peter Geibel, Steven Charles Hebert, David Martin, Deborah A. Russell
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Publication number: 20130172335Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130158112Abstract: A pharmaceutical composition for inhibiting amyloid beta peptide in a subject includes a compound having the formula (I): where M is selected from a substituted or unsubstituted alkyl, halo, alkoxy, aryl, cyclic, or heterocyclic group; p is an integer from 0-3; X1 is a 3-9 atoms in length linker connecting A and B; B is selected from a substituted or unsubstituted aryl, alkoxy or amine group; and a pharmaceutically acceptable salt thereof; and a pharmaceutical carrier.Type: ApplicationFiled: June 20, 2012Publication date: June 20, 2013Inventors: Jonathan D. Smith, Enakshi Chakrabarti, Subrata Ghosh, Marti Sayre, Gregory Tochtrop
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Publication number: 20130150381Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of dis orders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: June 13, 2013Applicant: ARDEA BIOSCIENCE, INC.Inventors: Samedy Ouk, Jean-Michel Vernier, Esmir Gunic
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Patent number: 8445534Abstract: This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, pro-drug, polymorph, crystal, or any combination thereof.Type: GrantFiled: December 7, 2009Date of Patent: May 21, 2013Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
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Publication number: 20130122085Abstract: This invention provides a pharmaceutical composition comprising Compound I-V, including inter alia solid dosage forms of powder-filled capsule formulations, liquid-filled softgel capsules (softgels), tablets, and sustained release dosage forms, and uses thereof in treating a variety of diseases or conditions in a subject, for example, treating a muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.Type: ApplicationFiled: November 1, 2012Publication date: May 16, 2013Applicant: GTx, Inc.Inventor: GTx, Inc.
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Publication number: 20130116227Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.Type: ApplicationFiled: July 12, 2011Publication date: May 9, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
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Publication number: 20130109701Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. 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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Patent number: 8426465Abstract: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.Type: GrantFiled: November 22, 2011Date of Patent: April 23, 2013Assignee: University of Tennesse Research FoundationInventors: James T. Dalton, Duane D. Miller
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Publication number: 20130079372Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.Type: ApplicationFiled: November 26, 2012Publication date: March 28, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
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Publication number: 20130035348Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: April 6, 2011Publication date: February 7, 2013Applicant: BRIGHAM YOUNG UNIVERSITYInventor: Marc Hansen
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Publication number: 20130035387Abstract: This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.Type: ApplicationFiled: September 26, 2012Publication date: February 7, 2013Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventor: UNIVERSITY OF TENNESSEE RESEARCH FOU
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Patent number: 8362074Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: October 31, 2007Date of Patent: January 29, 2013Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Publication number: 20120309812Abstract: The present invention relates to certain bisamide derivatives of formula (I), to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests compounds.Type: ApplicationFiled: February 1, 2011Publication date: December 6, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Renold
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Publication number: 20120295907Abstract: The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.Type: ApplicationFiled: April 14, 2010Publication date: November 22, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Maienfisch, Christopher Richard Ayles Godfrey, Pierre Joseph Marcel Jung, Ottmar Franz Hueter, Peter Renold
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Patent number: 8314146Abstract: The present invention relates to novel thioamide derivatives of formula (I) and formula (Ia): wherein, R3, R4, R5, R6, R7, P, Q, T, V, W, X, Y, Z, a, m and n are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.Type: GrantFiled: April 13, 2011Date of Patent: November 20, 2012Assignee: Merial LimitedInventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Philip Reid Timmons
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Patent number: 8314137Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.Type: GrantFiled: July 22, 2009Date of Patent: November 20, 2012Assignee: Trustess of Dartmouth CollegeInventors: Tadashi Honda, Emilie David, Dale Mierke
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Patent number: 8309603Abstract: This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.Type: GrantFiled: March 23, 2010Date of Patent: November 13, 2012Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Jeff Kearbey
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Publication number: 20120283215Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.Type: ApplicationFiled: September 14, 2010Publication date: November 8, 2012Applicants: The Regents of the University of California, a California Corporation, University of Texas at El Paso, Health and Human ServicesInventors: Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Tonos de Leon, Heather Balsiger, Robert Fletterick
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Publication number: 20120264823Abstract: The invention relates to compounds of Formula (I): (A?)x-(A)-(B)—(Z)-(L)-C(?O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A?), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.Type: ApplicationFiled: April 19, 2010Publication date: October 18, 2012Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
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Publication number: 20120238533Abstract: The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.Type: ApplicationFiled: September 3, 2010Publication date: September 20, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Arwed Cleve, Ulrich Lücking, Stefan Bäurle, Martin Fritsch, Jens Schröder, Bernd-Wolfgang Igl
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Publication number: 20120232138Abstract: Novel amidoacetonitrile compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for controlling endoparasites on warm-blooded animals.Type: ApplicationFiled: November 22, 2010Publication date: September 13, 2012Applicant: Novartis AGInventors: Thomas Goebel, Noëlle Gauvry, Heinz Sager
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20120201803Abstract: A process for forming a solid electrolytic capacitor and an electrolytic capacitor formed by the process. The process includes: providing an anode wherein the anode comprises a porous body and an anode wire extending from the porous body; applying a thin polymer layer onto the dielectric, and forming a dielectric on the porous body to form an anodized anode; applying a first slurry to the anodized anode to form a blocking layer wherein the first slurry comprises a first conducting polymer with an median particle size of at least 0.05 ?m forming a layer of crosslinker on the blocking layer; and applying a layer of a second conducting polymer on the layer of crosslinker.Type: ApplicationFiled: September 15, 2011Publication date: August 9, 2012Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, James Dennen O'Neil, Reid W. von Borstel, Ramchandran Arudchandran
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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Publication number: 20120142771Abstract: The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.Type: ApplicationFiled: February 7, 2012Publication date: June 7, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Seiji IWAMA, Tomoyuki Tanaka, Nana Yajima
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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: 20120135975Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: May 14, 2007Publication date: May 31, 2012Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, William K. Hagmann, Jeffrey J. Hale, Irene E. Whitney
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Publication number: 20120136052Abstract: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.Type: ApplicationFiled: November 22, 2011Publication date: May 31, 2012Inventors: James T. DALTON, Duane D. Miller
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Publication number: 20120122968Abstract: There is provided a method for promoting dynamin ring formation and/or maintenance of dynamin rings in a cell, comprising treating the cell with an effective amount of a dynamin ring stabilizer, or a prodrug or pharmaceutically acceptable salt of the dynamin ring stabilizer. The maintenance or accumulation of dynamin ring formation has particular application in the prophylaxis or treatment of a kidney disease or condition characterized by proteinuria. A dynamin ring stabilizer can be any agent that interacts with dynamin to promote dynamin ring assembly and/or inhibit dynamin ring disassembly. There are also provided methods for prophylaxis or treatment of podocyte dysfunction and/or maintaining or inducing actin cytoskeleton formation in a cell utilizing dynamin ring stabilizers, and for screening a test agent for use as a dynamin ring stabilizer.Type: ApplicationFiled: May 21, 2010Publication date: May 17, 2012Applicants: THE GENERAL HOSPITAL CORPORATION, CHILDREN'S MEDICAL RESEARCH INSTITUTEInventors: Phillip J. Robinson, Sanja Sever
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Publication number: 20120121693Abstract: The present invention provides methods of treating baldness in a subject and generating new hair follicles, comprising epidermal disruption and administration of a compound that promotes a differentiation of an uncommitted epidermal cell into a hair follicle cell. The present invention also provides methods for hair removal and inducing hair pigmentation.Type: ApplicationFiled: December 15, 2011Publication date: May 17, 2012Inventors: George COTSARELIS, Mayumi Ito
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Publication number: 20120122975Abstract: The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.Type: ApplicationFiled: April 14, 2010Publication date: May 17, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Maienfisch
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Publication number: 20120094977Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: May 25, 2011Publication date: April 19, 2012Applicant: Dendreon CorporationInventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
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Patent number: 8148561Abstract: A storage-stable, smooth-feeling, non-comedogenic fatty acid ester mixture of 2-ethylhexanol and fatty acids comprising 2-ethylhexyl fatty acid esters, wherein the aggregate amount of C12 and C14 2-ethylhexyl fatty acid esters is 85% or more of the mixture, based on the total weight of all fatty acid esters in the mixture, which mixtures are useful in or as an oil component of a cosmetic or pharmaceutical preparation.Type: GrantFiled: September 6, 2006Date of Patent: April 3, 2012Assignee: Cognis IP Management GmbHInventors: Achim Ansmann, Rolf Kawa, Lars Zander
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Publication number: 20120058974Abstract: The present invention relates to an agrochemical composition comprising pesticide and UV absorber. The invention furthermore relates to UV-absorbers and to the use thereof in agrochemical compositions. It moreover relates to a method of controlling phytopathogenic fungi and/or undesirable plant growth and/or undesirable insect or mite infestation and/or of regulating plant growth.Type: ApplicationFiled: March 10, 2010Publication date: March 8, 2012Applicant: BASF SEInventors: Andrea Misske, Christian Bittner, Michael Ishaque, Markus Hoffmann, Richard Riggs, Ruediger Sens, Andre Kabat, Sylke Haremza, Douglas D. Anspaugh, David M. Terry
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Publication number: 20120041046Abstract: The present invention concerns compounds of general Formula (I): method of preparation and uses thereof.Type: ApplicationFiled: April 12, 2010Publication date: February 16, 2012Applicant: CNR - CONSIGLIO NAZIONALE DELLE RICERCHEInventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
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Publication number: 20120035139Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.Type: ApplicationFiled: April 16, 2010Publication date: February 9, 2012Inventors: Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
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Patent number: RE44339Abstract: Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy, X is (CH2)n—R, where n is 0 or 1 and R is a group with non-bonding electrons, with the provisos that: (a) when Y and Z are H, X is not F, OH, MeO or NO2 in the 4-position and is not OH in the 2 or 6-position (b) when Y or Z is H then X, Y and Z are such that (i) the groups in the 3- and 4-positions are not both OMe, (ii) the groups in the 4- and 5-positions are not both OMe, (iii) the groups in 3- and 5-positions are not OMe if the group in the 4-position is OH, and (iv) the groups in the 3- and 5-positions are not OH if the group in the 4-position is methyl.Type: GrantFiled: August 31, 2011Date of Patent: July 2, 2013Assignee: Givaudan S.A.Inventors: Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack, Lori W. Tigani