Spiro Ring System Patents (Class 514/409)
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Patent number: 11395815Abstract: The present invention relates to a compound for treating or preventing osteoarthritis. The compound relieves the joint pain, inhibits and attenuates the development of post-traumatic osteoarthritis in mouse model. The present invention also provides a pharmaceutical composition comprising the compound for treating or preventing osteoarthritis. The present invention further provides a method for treating or preventing osteoarthritis by administrating to the patient in need thereof with the pharmaceutical composition.Type: GrantFiled: March 24, 2020Date of Patent: July 26, 2022Assignees: ASCENTAGE PHARMA (SUZHOU) CO., LTD., ASCENTAGE PHARMA GROUP CORP LIMITEDInventors: Dajun Yang, Yifan Zhai, Douglas Dong Fang, Saijie Zhu
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Patent number: 11339181Abstract: The present invention relates to crystalline forms of the Janus kinase (JAK) inhibitor 3-((3S,4R)-3-methyl-6-(7H-pyrrolo [2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl)-3-oxopropanenitrile (Compound A), as well as, compositions thereof, methods of their preparation, methods of use thereof and methods of quantitation.Type: GrantFiled: December 20, 2017Date of Patent: May 24, 2022Assignee: Japan Tobacco Inc.Inventors: Yukihiro Kamiya, Noriaki Shimoyama, Ryuhei Okura, Satoru Noji
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Patent number: 10888548Abstract: Anti-Dandruff Agents A novel anti-dandruff composition comprising spirofuranone-lactam tetramic acid or derivatives thereof, and optionally at least one biologically derivable meroterpene. The spirofuranone-lactam tetramic acid is preferably a bio-active heterospirocyclic secondary metabolite of Aspergillus, such as pseurotin A. The biologically derivable meroterpene may be selected from fumagillin, fumagillin derivative, chlovalicin, or ovalicin. Use of said agents as anti-dandruff actives in anti-dandruff compositions, particularly shampoos and conditioners is also provided. The active is particularly effective against Malassezia yeasts and Malassezia furfur which may cause dandruff. A method of obtaining the anti-dandruff actives from culturing of Peyronellaea sp. strain RKDO347 is also described.Type: GrantFiled: June 8, 2016Date of Patent: January 12, 2021Assignee: Croda International PlcInventors: Russell Greig Kerr, David Patrick Overy, Fabrice Berrué
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Patent number: 10759751Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.Type: GrantFiled: March 7, 2019Date of Patent: September 1, 2020Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
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Patent number: 10716790Abstract: It is intended to provide a medicament and a method for treating cancer comprising a compound having MDM2 inhibiting activity and a compound having FLT3 inhibiting activity in combination. The present invention provides a medicament comprising (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a pharmaceutically acceptable salt thereof and N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea or a pharmaceutically acceptable salt thereof in combination, and a treatment method using these compounds or salts in combination.Type: GrantFiled: April 14, 2017Date of Patent: July 21, 2020Assignee: DAIICHI SANKYO COMPANY, LIMITEDInventor: Takahiko Seki
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Patent number: 10633347Abstract: Disclosed are a method for preparing an imidazole derivative and crystal form A and crystal form B thereof, and also disclosed is a method for preparing a compound of formula (I) and an intermediate thereof.Type: GrantFiled: January 8, 2019Date of Patent: April 28, 2020Assignee: SHANDONG DANHONG PHARMACEUTICAL CO., LTD.Inventors: Weihua Shi, Feng Xu, Zheng Wang, Weidong Li, Linghui Wu, Hongwei Li, Minggao Zeng, Kunmin Lai, Zhigan Jiang, Haiying He
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Patent number: 10369150Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.Type: GrantFiled: October 10, 2018Date of Patent: August 6, 2019Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as represented by the Department of Veterans AffairsInventors: Beibei Chen, Rama K. Mallampalli
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Patent number: 10323012Abstract: The present disclosure relates to miliusane and analogs thereof that are useful as anti-virals, such as anti-HIV and anti-influenza virus agents. The present disclosure provides methods for treating viral infections, such as AIDS, HIV, and influenza infections.Type: GrantFiled: November 3, 2017Date of Patent: June 18, 2019Assignee: Hong Kong Baptist UniversityInventor: Hongjie Zhang
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Patent number: 10227309Abstract: Disclosed are a method for preparing an imidazole derivative and crystal form A and crystal form B thereof, and also disclosed is a method for preparing a compound of formula (I) and an intermediate thereof.Type: GrantFiled: June 7, 2016Date of Patent: March 12, 2019Assignee: SHANDONG DANHONG PHARMACEUTICAL CO., LTD.Inventors: Weihua Shi, Feng Xu, Zheng Wang, Weidong Li, Linghui Wu, Hongwei Li, Minggao Zeng, Kunmin Lai, Zhigan Jiang, Haiying He
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Patent number: 9849127Abstract: The present invention relates to a pharmaceutical composition comprising a compound of formula (I) and methods of treating or preventing cell proliferation disorders comprising administering to a subject a therapeutically active amount or a preventive amount of such a compound.Type: GrantFiled: May 14, 2014Date of Patent: December 26, 2017Assignee: Medizinisch Hochschule HannoverInventors: Michael Heuser, Anuhar Chaturvedi, Matthias Preller
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Patent number: 9849109Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.Type: GrantFiled: February 23, 2015Date of Patent: December 26, 2017Assignee: AMIRA PHARMACEUTICALS, INC.Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
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Patent number: 9822071Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer miliusane lactam compounds. The present invention also includes its preparation and application method for treating cancer.Type: GrantFiled: June 1, 2017Date of Patent: November 21, 2017Assignee: Hong Kong Baptist UniversityInventor: Hongjie Zhang
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Patent number: 9695141Abstract: 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: GrantFiled: October 30, 2015Date of Patent: July 4, 2017Assignee: HONG KONG BAPTIST UNIVERSITYInventors: Hongjie Zhang, Yifu Guan
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Patent number: 9567299Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X, R1 to R7 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.Type: GrantFiled: October 22, 2014Date of Patent: February 14, 2017Assignee: JANSSEN SCIENCES IRELAND UCInventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Bernard Raboisson
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Patent number: 9480677Abstract: 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: October 9, 2014Date of Patent: November 1, 2016Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Alexandre Cadieux
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Patent number: 9428504Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.Type: GrantFiled: July 30, 2013Date of Patent: August 30, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Carl Thibeault, Charles G. Clark, Indawati DeLucca, Carol Hui Hu, Yoon Jeon, Patrick Y. S. Lam, Jennifer X. Qiao, Wu Yang, Yufeng Wang, Tammy C. Wang
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Patent number: 9320731Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.Type: GrantFiled: April 14, 2014Date of Patent: April 26, 2016Assignee: THERON PHARMACEUTICALS, INC.Inventors: Jürg R. Pfister, Gwenaella Rescourio, Meenakshi S. Venkatraman, Xiaoming Zhang
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Patent number: 9221836Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: GrantFiled: March 23, 2015Date of Patent: December 29, 2015Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takanobu Kuroita, Yasuhiro Imaeda, Kouichi Iwanaga, Naohiro Taya, Hidekazu Tokuhara
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Patent number: 9211333Abstract: 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: GrantFiled: March 15, 2013Date of Patent: December 15, 2015Assignee: HONG KONG BAPTIST UNIVERSITYInventor: Hongjie Zhang
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Patent number: 9120797Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.Type: GrantFiled: September 2, 2011Date of Patent: September 1, 2015Assignee: Gruenenthal GmbHInventors: Claudia Hinze, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
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Patent number: 9079913Abstract: 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: September 12, 2014Date of Patent: July 14, 2015Assignee: 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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Publication number: 20150126489Abstract: The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.Type: ApplicationFiled: May 8, 2013Publication date: May 7, 2015Applicant: ZAFGEN, INC.Inventors: Robert Zahler, James E. Vath
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Publication number: 20150118258Abstract: The present invention relates to fluorinated bridged spiro[2.4]heptane derivatives of formula (I), wherein n and R1 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: May 15, 2013Publication date: April 30, 2015Inventors: Olivier Corminboeuf, Davide Pozzi
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Publication number: 20150111939Abstract: A pharmaceutical dosage form for administration twice daily, once daily or less frequently, which contains 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.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Inventors: Nadja GRUENING, Marc SCHILLER, Ashish HEMANI, Chris KIRBY, Ingo FRIEDRICH
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Patent number: 9000189Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the compounds of the formula (I) and, secondly, at least one 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: November 22, 2007Date of Patent: April 7, 2015Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Rolf Pontzen, Christian Arnold, Ulrich Görgens, Olga Malsam, Udo Reckmann, Erich Sanwald, Stefan Lehr, Jan Dittgen, Dieter Feucht, Martin Hills, Christopher Rosinger
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Patent number: 9000025Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.Type: GrantFiled: August 19, 2011Date of Patent: April 7, 2015Assignee: Amira Pharmaceuticals, Inc.Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
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Patent number: 9000026Abstract: The invention relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumor disorders. The invention also relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selectively herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound.Type: GrantFiled: February 14, 2012Date of Patent: April 7, 2015Assignee: Bayer Intellectual Property GmbHInventors: Ningshu Liu, Kai Thede, Ursula Mönning, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Reiner Fischer
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Publication number: 20150094304Abstract: 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: December 11, 2014Publication date: April 2, 2015Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
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Patent number: 8993782Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the cis-alkoxyspirocyclic biphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention relates furthermore to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.Type: GrantFiled: November 22, 2007Date of Patent: March 31, 2015Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christian Arnold, Olga Malsam, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Martin Jeffrey Hills, Christopher Hugh Rosinger
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Publication number: 20150057326Abstract: A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.Type: ApplicationFiled: November 10, 2014Publication date: February 26, 2015Applicant: Trustees of Dartmouth CollegeInventor: Jimmy Wu
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Patent number: 8962672Abstract: 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 (29) listed in the disclosure.Type: GrantFiled: September 19, 2011Date of Patent: February 24, 2015Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Publication number: 20150031691Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.Type: ApplicationFiled: October 8, 2014Publication date: January 29, 2015Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
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Publication number: 20150025121Abstract: 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: October 9, 2014Publication date: January 22, 2015Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Alexandre Cadieux
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Publication number: 20150005260Abstract: The present invention relates to methods and kits for detecting diastolic dysfunction in subjects without clinical signs of heart failure.Type: ApplicationFiled: January 2, 2013Publication date: January 1, 2015Inventors: Faiez Zannad, Patrick Rossignol
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Publication number: 20150005358Abstract: The present invention relates to the control of fish parasites, especially Copepodae, by means of phenyl-substituted ketoenols.Type: ApplicationFiled: January 22, 2013Publication date: January 1, 2015Inventors: Jan Koesling, Reiner Fischer
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Patent number: 8921576Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.Type: GrantFiled: October 18, 2012Date of Patent: December 30, 2014Assignee: Kowa Company, Ltd.Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
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Patent number: 8912226Abstract: 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: GrantFiled: May 13, 2013Date of Patent: December 16, 2014Assignee: Gruenenthal GmbHInventors: Stefanie Frosch, Klaus Linz, Klaus Schiene
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Publication number: 20140357655Abstract: Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.Type: ApplicationFiled: January 15, 2013Publication date: December 4, 2014Inventors: Olaf Panknin, Stefan Bäurle, Sven Ring, Wolfgang Schwede, Wilhelm Bone, Katrin Nowak-Reppel, Eckhard Bender, Reinhard Nubbemeyer, Mark Jean Gnoth
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Patent number: 8901038Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.Type: GrantFiled: February 10, 2011Date of Patent: December 2, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Chieko Ueno, Arnd Voerste, Elmar Gatzweiler, Ines Heinemann, Ulrich Görgens
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Patent number: 8901117Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: GrantFiled: December 23, 2011Date of Patent: December 2, 2014Assignee: The Regents of The University of MichiganInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Publication number: 20140349987Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 3, 2012Publication date: November 27, 2014Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Publication number: 20140343077Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.Type: ApplicationFiled: August 22, 2012Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant
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Patent number: 8889703Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.Type: GrantFiled: February 23, 2011Date of Patent: November 18, 2014Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh Singh, Yajun Zheng
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Publication number: 20140336233Abstract: Compounds of the formulae (I) and (II) for controlling pathogens by foliar application.Type: ApplicationFiled: August 2, 2012Publication date: November 13, 2014Applicant: Bayer Intellectual Property GmbHInventors: Marie-Pascale Latorse, Marie-Claire Grosjean-Cournoyer
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Publication number: 20140336202Abstract: Methods of treating subjects with cancer and screening for MDM2 inhibitors that may be effective cancer therapeutics are provided herein. The cancers that may be treated using MDM2 inhibitors using the methods described herein include those that are or may become resistant to treatment with tyrosine kinase inhibitors. Methods of treating subjects with cancers that have, or develop in response to treatment with tyrosine kinase inhibitors, elevated levels of MDM2, Mcl-1 or PP5 or decreased levels of Huwe1 or CAS using MDM2 inhibitors are provided herein. The MDM2 inhibitors may be effective at treating these cancers alone or in combination with a tyrosine kinase inhibitor regardless of p53 status (mutant or wild-type) of the cancer.Type: ApplicationFiled: December 7, 2012Publication date: November 13, 2014Applicant: DUKE UNIVERSITYInventors: Sally Kornbluth, Manabu Kurokawa, Neil Spector, Mark Dewhirst
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Patent number: 8883840Abstract: 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: September 14, 2012Date of Patent: November 11, 2014Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Cadieux
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Publication number: 20140329865Abstract: The present invention relates to pesticidal mixtures comprising a component A and a component B, wherein component A is a compound of formula (I) wherein B1, B2, B3, X1, X2, X3, X4, Y1, Y2, Y3, R5, R7, and R8 are as defined in claim 1 and component B is an insecticide. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: ApplicationFiled: December 12, 2012Publication date: November 6, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Myriem El Qacemi, Jerome Yves Cassayre
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Patent number: 8877796Abstract: 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: July 17, 2013Date of Patent: November 4, 2014Assignee: 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: 8859466Abstract: The present invention relates to novel oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, B, D, Q1, Q2, and G have the meanings given above, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by addition of ammonium salts or phosphonium salts and, if appropriate, penetrants.Type: GrantFiled: July 22, 2008Date of Patent: October 14, 2014Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Gudrun Lange, Stefan Lehr, Christian Arnold, Dieter Feucht, Eva-Maria Franken, Martin Jeffrey Hills, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Jan Dittgen, Ulrich Görgens, Isolde Häuser-Hahn
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Patent number: 8859782Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.Type: GrantFiled: January 25, 2012Date of Patent: October 14, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Himmler