Spiro Ring System Patents (Class 514/409)
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Patent number: 8618156Abstract: Crystalline forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these crystalline modifications, the use of these modifications as well as a process for the enrichment of such crystalline modifications.Type: GrantFiled: July 6, 2012Date of Patent: December 31, 2013Assignee: Gruenenthal GmbHInventors: Michael Gruss, Stefan Kluge, Stefan Pruehs
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Patent number: 8614245Abstract: Crystalline forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these crystalline modifications, the use of these modifications as well as a process for the enrichment of such crystalline modifications.Type: GrantFiled: January 8, 2013Date of Patent: December 24, 2013Assignee: Gruenenthal GmbHInventors: Michael Gruss, Stefan Kluge, Stefan Pruehs
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Patent number: 8609712Abstract: Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.Type: GrantFiled: September 14, 2012Date of Patent: December 17, 2013Assignee: Wyeth LLCInventors: Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Anthony Francis Hadfield, Jean Louise Helom
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Publication number: 20130331369Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.Type: ApplicationFiled: August 8, 2013Publication date: December 12, 2013Applicant: Novartis AGInventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
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Publication number: 20130324581Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient, which is selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient, which is a propionic acid derivative selected from the group consisting of ibuprofen, naproxen, ketoprofen, flurbiprofen, fenoprofen, fenbufen, suprofen, pirprofen, indoprofen, tiaprofenic acid, oxaprozin, ibuproxam, flunoxaprofen, alminoprofen, naproxcinod, and the physiologically acceptable salts thereof.Type: ApplicationFiled: May 13, 2013Publication date: December 5, 2013Inventors: Stefanie FROSCH, Klaus LINZ, Klaus SCHIENE
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Publication number: 20130324580Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer agents based on miliusane compounds. The present invention also includes its preparation and application method for treating cancer.Type: ApplicationFiled: March 15, 2013Publication date: December 5, 2013Applicant: HONG KONG BAPTIST UNIVERSITYInventor: Hongjie ZHANG
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Publication number: 20130317076Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is a salicylic acid component selected from the group consisting of acetylsalicylic acid, salicylic acid, salicylamide, ethenzamide, salsalate, dipyrocetyl, benorilate, diflunisal, guacetisal, and the physiologically acceptable salts thereof.Type: ApplicationFiled: May 13, 2013Publication date: November 28, 2013Applicant: Gruenenthal GmbHInventor: Gruenenthal GmbH
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Publication number: 20130317075Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is a non-steroidal anti-rheumatic drug selected from the group consisting of indometacin, diclofenac, sulindac, tolmetin, zomepirac, aclofenac, bumadizone, etodolac, lonazolac, fentiazac, acemetacin, difenpiramide, oxametacin, proglumetacin, ketorolac, aceclofenac, bufexamac, mefenamic acid, tolfenamic acid, flufenamic acid, meclofenamic acid, and the physiologically acceptable salts thereof.Type: ApplicationFiled: May 13, 2013Publication date: November 28, 2013Applicant: Gruenenthal GmbHInventor: Gruenenthal GmbH
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Publication number: 20130317009Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is an anticonvulsant selected from the group consisting of retigabin, lamotrigine, lacosamide, levetiracetam, carbamazepine, sultiame, phenacemide, felbamate, topiramate, pheneturide, brivaracetam, selectracetam, zonisamide, stiripentol, beclamide, mexiletin, ralfinamide, methylphenobarbital, phenobarbital, primidone, barbexaclone, metharbital, ethotoin, phenyloin, amino(diphenylhydantoin) valeric acid, mephenyloin, fosphenyloin, paramethadione, trimethadione, ethadione, ethosuximide, phensuximide, mesuximide, clonazepam, lorazepam, diazepam, clobazam, oxcarbazepine, eslicarbazepine, rufinamide, valproic acid, valpromide, aminobutyric acid, progabide, tiagabine, and the physioloType: ApplicationFiled: May 13, 2013Publication date: November 28, 2013Applicant: Gruenenthal GmbHInventor: Gruenenthal GmbH
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Publication number: 20130310419Abstract: The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the ?7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system.Type: ApplicationFiled: January 31, 2012Publication date: November 21, 2013Applicant: LUPIN LIMITEDInventors: Neelima Sinha, Gourhari Jana, Navnath Popat Karche, Shridhar Keshav Adurkar, Girish Dhanraj Hatnapure, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130310385Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is an antidepressant.Type: ApplicationFiled: May 13, 2013Publication date: November 21, 2013Applicant: GRUENENTHAL GMBHInventors: Stefanie FROSCH, Klaus LINZ, Thomas CHRISTOPH
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Publication number: 20130310435Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient selected from paracetamol and propacetamol.Type: ApplicationFiled: May 13, 2013Publication date: November 21, 2013Applicant: Gruenenthal GmbHInventors: Stefanie FROSCH, Klaus LINZ, Klaus SCHIENE
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Publication number: 20130310434Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient selected from gabapentinoids and the physiologically acceptable salts thereof.Type: ApplicationFiled: May 13, 2013Publication date: November 21, 2013Applicant: Gruenenthal GmbHInventors: Stefanie FROSCH, Klaus LINZ, Thomas CHRISTOPH
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Publication number: 20130296395Abstract: The present invention relates to the use of tetramic acid derivatives of the formulae (I) or (II) for controlling animal pests after stem treatments (spraying on, painting on, injecting, applying), treatments of branches, stalks, shoots and twigs (painting on, spraying on, applying), influorescence treatments and bud treatments by injection.Type: ApplicationFiled: July 11, 2013Publication date: November 7, 2013Inventors: Reiner FISCHER, Heike HUNGENBERG, Wolfram ANDERSCH, Xavier Alain Marie VAN WAETERMEULEN
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Publication number: 20130296303Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: July 17, 2013Publication date: November 7, 2013Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
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Patent number: 8575208Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: GrantFiled: February 20, 2008Date of Patent: November 5, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Randy Scott Bethiel, Dylan Jacobs, Robert B. Perni, John Maxwell, Kevin Cottrell, Summer Halas
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Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Patent number: 8551982Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 13, 2012Date of Patent: October 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
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Publication number: 20130261163Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (23) listed in the disclosure.Type: ApplicationFiled: May 16, 2013Publication date: October 3, 2013Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Christoph Erdelen
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Publication number: 20130252962Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: March 6, 2013Publication date: September 26, 2013Inventors: Mikhail CHAFEEV, Sultan CHOWDHURY, Lauren FRASER, Jianmin FU, Jonathan LANGILLE, Shifeng LIU, Jianyu SUN, Shaoyi SUN, Serguei SVIRIDOV, Mark WOOD, Alla Yurevna ZENOVA, Qi JIA, Jean-Jacques Alexandre CADIEUX, Simon J. GAUTHIER, Amy Frances DOUGLAS, Tom HSIEH, Nagasree CHAKKA, Zoran CIKOJEVIC
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Patent number: 8541343Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: GrantFiled: November 29, 2010Date of Patent: September 24, 2013Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20130237532Abstract: The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient.Type: ApplicationFiled: April 9, 2013Publication date: September 12, 2013Applicant: LG Life Sciences Ltd.Inventors: Soon Ha KIM, Hyoung Jin KIM, Sun Young KOO, Chul Woong CHUNG, Sung Bae LEE, Heui Sul PARK, Seung Hyun YOON, Hyo Shin KWAK, Dong Ook SEO, Eok PARK
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Publication number: 20130231381Abstract: Crystalline forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these crystalline modifications, the use of these modifications as well as a process for the enrichment of such crystalline modifications.Type: ApplicationFiled: March 15, 2013Publication date: September 5, 2013Applicant: GRUENENTHAL GMBHInventors: Michael GRUSS, Stefan KLUGE, Sefan PRUEHS
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Patent number: 8518984Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: GrantFiled: November 12, 2010Date of Patent: August 27, 2013Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
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Patent number: 8518985Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.Type: GrantFiled: March 11, 2010Date of Patent: August 27, 2013Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Gorgens, Jan Dittgen, Dieter Feucht, Isolde Hauser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
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Patent number: 8512690Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: April 7, 2010Date of Patent: August 20, 2013Assignee: Novartis AGInventors: Trixi Brandl, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
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Publication number: 20130210884Abstract: The present invention relates to the discovery that mutations in SCN9A are causative of Congenital Indifference to Pain (CIP) in humans. The invention also relates to methods of using compounds small organic compounds to treat pain as well as to predict the effect of analgesic agents in patients, such as those possessing gain of function mutations.Type: ApplicationFiled: April 11, 2013Publication date: August 15, 2013Applicant: Xenon Pharmaceutical Inc.Inventors: Marcia MacDonald, Mark Samuels, Robin Sherrington, Yigal Paul Goldberg
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Patent number: 8507537Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: GrantFiled: October 13, 2007Date of Patent: August 13, 2013Assignee: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
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Publication number: 20130202701Abstract: The invention relates to a pharmaceutical dosage form comprising (1r,4r)-6?-Fluoro-(N-methyl- or N,N-dimethyl-)-4-phenyl-4?,9?-dihydro-3?H-spiro-[cyclohexane-1,1?-pyrano[3,4,b]-indol]-4-amine or a physiologically acceptable salt thereof, for use in the treatment of fibromyalgia or chronic fatigue syndrome.Type: ApplicationFiled: February 1, 2013Publication date: August 8, 2013Applicant: GRUENENTHAL GMBHInventor: GRUENENTHAL GMBH
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Publication number: 20130196973Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 13, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
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Publication number: 20130197050Abstract: The present invention provides novel lactams extracted from an alcohol extract of dehulled adlay seeds. The present invention also provides a process for the preparation of the lactams and a method for treating breast cancer in a subject, which method comprises administering to said subject an effective amount of the lactam and a pharmaceutically acceptable carrier or excipient.Type: ApplicationFiled: February 1, 2012Publication date: August 1, 2013Inventors: WENCHANG CHIANG, YUEH-HSIUNG KUO, YUN-LIAN LIN, CHENG-PEI CHUNG
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Patent number: 8497295Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: July 11, 2012Date of Patent: July 30, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Publication number: 20130190288Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130165424Abstract: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.Type: ApplicationFiled: March 9, 2012Publication date: June 27, 2013Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
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Publication number: 20130158046Abstract: Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: Mersana Therapeutics, IncInventors: Laura C. Akullian, Russell C. Petter, John J. Kane, Charles E. Hammond, Mao Yin, Aleksandr Yurkovetskiy, Cheri A. Stevenson
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Patent number: 8466188Abstract: This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.Type: GrantFiled: October 12, 2007Date of Patent: June 18, 2013Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Rajender Kamboj, Duanjie Hou, Shifeng Liu, Mehran Seid Bagherzadeh, Serguei Sviridov, Shaoyi Sun, Jianyu Sun, Nagasree Chakka, Tom Hsieh, Vandna Raina
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Publication number: 20130150420Abstract: Solid forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine hydrochloride, in particular crystalline forms and/or amorphous forms thereof, pharmaceutical compositions and medicaments containing these solid forms, the use of these solid forms, and a process for obtaining such solid forms.Type: ApplicationFiled: December 11, 2012Publication date: June 13, 2013Applicant: Gruenenthal GmbHInventor: Gruenenthal GmbH
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Publication number: 20130143942Abstract: The invention relates to a method of controlling aphids that are resistant to neonicotinoid insecticides, using the compound spirotetramat in free form or in agrochemically acceptable salt form as well as the use of compositions comprising said compound to control neonicontinoid resistant insects. In particular the methods relate to controlling neonicotinoid resistant insects in the Aphididae family, that are resistant to one or more neonicotinoid insecticides. Methods of the invention find particular use in controlling neonicotinoid resistant insects in crops of useful plants. Furthermore, the invention extends to methods of controlling plant viruses spread by neonicotinoid resistant insects.Type: ApplicationFiled: April 18, 2011Publication date: June 6, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventor: Russell Slater
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Publication number: 20130143941Abstract: This invention is directed to pharmaceutical compositions for topical administration to a mammal, wherein the pharmaceutical compositions comprise a spiro-oxindole compound, as an enantiomer, a racemate or a non-racemic mixture, or a pharmaceutically acceptable salt thereof. These pharmaceutical compositions are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions.Type: ApplicationFiled: February 25, 2011Publication date: June 6, 2013Inventors: Conrad Stewart Winters, Meidong Yang, Haigang Chen
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Publication number: 20130136719Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: May 25, 2012Publication date: May 30, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson
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Patent number: 8450358Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.Type: GrantFiled: June 28, 2010Date of Patent: May 28, 2013Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Cadieux
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Patent number: 8445527Abstract: The present invention provides a method of treating a HCV infection in a subject in need thereof by administering a compound of Formula I: or pharmaceutically acceptable salts thereof or stereoisomers thereof.Type: GrantFiled: May 22, 2012Date of Patent: May 21, 2013Assignee: Novartis AGInventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
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Publication number: 20130123324Abstract: Crystalline forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these crystalline modifications, the use of these modifications as well as a process for the enrichment of such crystalline modifications.Type: ApplicationFiled: January 8, 2013Publication date: May 16, 2013Applicant: Gruenenthal GmbHInventor: Gruenenthal GmbH
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Patent number: 8440710Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof. The are useful as HSL inhibitors and may, for example, be used in treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, and obesity.Type: GrantFiled: October 8, 2010Date of Patent: May 14, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Stephan Brugger, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Publication number: 20130116230Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: December 20, 2012Publication date: May 9, 2013Applicant: INCYTE CORPORATIONInventor: Incyte Corporation
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Publication number: 20130102604Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.Type: ApplicationFiled: December 10, 2012Publication date: April 25, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8420608Abstract: The novel active compound combinations comprising compounds of the formula (I) and spinetoram have very good insecticidal and/or acaricidal properties.Type: GrantFiled: November 13, 2009Date of Patent: April 16, 2013Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Wolfram Andersch, Heike Hungenberg
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Publication number: 20130072538Abstract: The present invention relates to the use of compounds of the formula (I) for controlling insects from the order beetles (Coleoptera), thrips (Tysanoptera), bugs (Hemiptera), flies (Diptera), leafhoppers (Auchenorrhyncha) and the families gall midges (Cecidomyiidae), leaf miners (Gracillariidae), tortrix moths (Tortricidae) and sawflies (Tenthredinidae) in which A, B, G, W, X, Y and Z have the abovementioned meanings.Type: ApplicationFiled: November 14, 2012Publication date: March 21, 2013Applicant: BAYER CROPSCIENCE AGInventor: BAYER CROPSCIENCE AG
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Publication number: 20130072537Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Cadieux
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Patent number: 8399453Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example. Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.Type: GrantFiled: July 19, 2011Date of Patent: March 19, 2013Assignee: Novartis AGInventors: Shi Hua Ang, Philipp Krastel, Seh Yong Leong, Liying Jocelyn Tan, Wei Lin Josephine Wong, Bryan K. S. Yeung, Bin Zou