At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Publication number: 20120172364Abstract: Rate-controlled particles, comprising compounds of the formula as a solid dispersion.Type: ApplicationFiled: March 14, 2012Publication date: July 5, 2012Inventors: Thomas Hantke, Bettina Rehbock, Jörg Rosenberg, Jörg Breitenbach
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Publication number: 20120157484Abstract: Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:Type: ApplicationFiled: November 7, 2011Publication date: June 21, 2012Inventors: Arokiasamy DEVASAGAYARAJ, Haihong Jin, Qingyun Liu, Brett Marinelli, Lakshama Samala, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Wenxue Wu, Chengmin Zhang, Haiming Zhang
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Publication number: 20120157426Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: November 8, 2011Publication date: June 21, 2012Applicant: AVILA THERAPEUTICS, INC.Inventors: Kwangho Lee, Deqiang Niu, Matthew F. Baevsky
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Publication number: 20120149722Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: October 31, 2011Publication date: June 14, 2012Applicant: AVILA THERAPEUTICS, INC.Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Juswinder Singh
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Publication number: 20120142667Abstract: The invention relates to compounds of formula (I) wherein R1 to R5, X and X1 to X3 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: June 10, 2010Publication date: June 7, 2012Inventors: Nigel Ramsden, Jeremy Major, Adeline Morel, Mihiro Sunose, Nelly Piton
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Publication number: 20120142647Abstract: The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Inventors: Scott L. Dax, Richard Woodward, Sean Peng
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Patent number: 8188276Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: January 30, 2009Date of Patent: May 29, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G Payan, Susan Molineaux, Sasha J Holland, Jeffrey Wayne Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B Rossi
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Publication number: 20120129867Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: January 30, 2012Publication date: May 24, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Qing Xu, Mukund Mehrotra, Jack W. Rose, Wolin Huang, Chandrasekar Venkataramani, Anjali Pandey
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Patent number: 8178671Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: July 30, 2004Date of Patent: May 15, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
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Patent number: 8163745Abstract: This invention concerns 5-(hydroxymethylene and aminomethylene)pyrimidine derivatives having HIV (Human Immunodeficiency Virus) replication inhibiting properties, to the preparation thereof and to pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 30, 2007Date of Patent: April 24, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant, Benoit Antoine Schmitt
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Patent number: 8158641Abstract: The present invention relates to 2-arylamino-4-(aminoalkylene)aminopyrimidines inhibitors having the structure shown below: wherein R and R1 are as defined herein. The 2-arylamino-4 -(aminoalkylene)aminopyrimidines inhibit Protein Kinase C-alpha (PKC-?). The PKC-? inhibitors of the present invention are important for improving myocardial intracellular calcium cycling, resulting in improved myocardial contraction and relaxation performance and thereby slowing the progression of heart failure. The present invention further relates to compositions comprising said 2-arylamino-4 -(aminoalkylene)amino-pyrimidines and to methods for controlling, abating, or otherwise slowing the progression of heart failure.Type: GrantFiled: March 26, 2009Date of Patent: April 17, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Jane Far-Jine Djung, Adam Golebiowski, Jack A. Hunter, Gary P. Schrum
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Publication number: 20120088768Abstract: Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: ApplicationFiled: December 15, 2011Publication date: April 12, 2012Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Pingyu Ding, Sacha Holland, Dane Goff
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Publication number: 20120083006Abstract: The present invention relates to immobilization compounds (I), immobilization products and preparations thereof as well as methods and uses for the identification of kinase interacting compounds or for the purification or identification of kinase proteins.Type: ApplicationFiled: March 31, 2010Publication date: April 5, 2012Applicant: Cellzone AGInventors: Nigel Ramsden, Jeremy Major, John Harrison, Daniel Leggate, Paola Grandi
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Publication number: 20120076835Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 30, 2011Publication date: March 29, 2012Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts
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Publication number: 20120077832Abstract: The present invention provides a salt form, and compositions thereof, useful as an inhibitor of one or more protein kinases and which exhibits desirable characteristics for the same.Type: ApplicationFiled: August 8, 2011Publication date: March 29, 2012Applicant: AVILA THERAPEUTICS, INC.Inventors: Steven Richard Witowski, William Frederick Westlin, III, Richland Wayne Tester
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Publication number: 20120053179Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: ApplicationFiled: November 4, 2011Publication date: March 1, 2012Inventors: Dhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Chunguang Wang, Hans Pluempe, Achim Feurer, Samir Bennabi
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Publication number: 20120027733Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosed.Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Applicant: NEURALSTEM, INC.Inventors: Judith KELLEHER-ANDERSSON, Karl K. Johe
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Publication number: 20120022066Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: ApplicationFiled: July 20, 2011Publication date: January 26, 2012Applicant: Vestaron CorporationInventors: Robert M. Kennedy, Bruce A. Steinbaugh
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Patent number: 8101629Abstract: The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.Type: GrantFiled: July 28, 2010Date of Patent: January 24, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Paul Theodoor Agnes Stevens, Alex Herman Copmans, Jozef Peeters, Alfred Elisabeth Stappers, Roger Petrus Gerebern Vandecruys, Paul Stoffels
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Patent number: 8101627Abstract: The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.Type: GrantFiled: November 19, 2008Date of Patent: January 24, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Ankush Argade, Rajinder Singh, Hui Li
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Publication number: 20110319615Abstract: Pyrimidinyl aryl hydrazones are effective at controlling insects.Type: ApplicationFiled: September 8, 2011Publication date: December 29, 2011Applicant: DOW AGROSCIENCES LLCInventors: Katherine A. Guenthenspberger, Timothy C. Johnson, Noormohamed M. Niyaz, Ricky Hunter, Annette V. Brown, Tony K. Trullinger
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Publication number: 20110311593Abstract: The invention relates to N-hydroxylated amidines, guanidines and aminohydrazones for application on the skin. In particular, the invention relates to transdermal therapeutic systems containing N-hydroxylated amidines, guanidines and aminohydrazones as a prodrug, and to methods for producing and using such systems.Type: ApplicationFiled: February 5, 2010Publication date: December 22, 2011Inventors: Rudolf Matusch, Hans-Rainer Hoffmann, Bodo Asmussen, Andreas Koch
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Patent number: 8080551Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.Type: GrantFiled: June 26, 2006Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Publication number: 20110301141Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: June 1, 2011Publication date: December 8, 2011Applicant: Genentech, Inc.Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Janet Gunzner-Toste, Daniel Shore, Zachary Sweeney, Shumei Wang, Guiling Zhao
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Publication number: 20110294749Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: ApplicationFiled: June 28, 2011Publication date: December 1, 2011Applicant: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110294838Abstract: The invention relates to sulfoximine-substituted anilino-pyrimidine derivatives of formula (I). methods of production thereof, and use thereof as medication for the treatment of various diseases.Type: ApplicationFiled: October 9, 2009Publication date: December 1, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Lücking, Rolf Jautelat, Gerhard Siemeister, Julia Schulze, Philip Lienau
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Patent number: 8067422Abstract: The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans.Type: GrantFiled: March 4, 2008Date of Patent: November 29, 2011Assignee: Natco Pharma LimitedInventors: Amala Kishan Kompella, Bhujanga Rao Adibhatla Kali Satya, Sreenivas Rachakonda, Nannapaneni Venkaiah Chowdary
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Patent number: 8058434Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosed.Type: GrantFiled: November 4, 2010Date of Patent: November 15, 2011Assignee: Neuralstem, Inc.Inventors: Judith Kelleher-Andersson, Karl K. Johe
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Publication number: 20110275633Abstract: The present invention encompasses compounds of general formula (1) wherein R1-R3 and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 13, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Bodo Betzemeier, Heinz Stadtmueller
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Publication number: 20110275075Abstract: An in vitro method for screening candidate compounds for the preventive or curative treatment of alopecia is described. The method can include determining the capacity of a compound to modulate the expression or the activity of a SOX transcription factor. The use of modulators of the expression or the activity of the transcription factor for the treatment of alopecia is also described. Methods for the in vitro diagnosis or prognosis of the pathology are also described herein.Type: ApplicationFiled: September 21, 2009Publication date: November 10, 2011Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Sandrine Rethore
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Publication number: 20110275655Abstract: The present invention relates to the compound of formula (I): or a salt, preferably a pharmaceutically acceptable salt, thereof; is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases, as well of potential use in cancer therapy, specifically heme malignancies.Type: ApplicationFiled: January 11, 2010Publication date: November 10, 2011Applicant: GLAXO GROUP LIMITEDInventors: Francis Louis Atkinson, Vipulkumar Kantibhai Patel
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Publication number: 20110263625Abstract: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C3-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substitutType: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries, Frank Xavier Jozef Herwig Arts
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Patent number: 8044040Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: July 16, 2007Date of Patent: October 25, 2011Assignees: Bristol-Myers Squibb Company, Pharmacopeia, Inc.Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Publication number: 20110257154Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: June 29, 2011Publication date: October 20, 2011Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Patent number: 8039479Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: GrantFiled: November 20, 2007Date of Patent: October 18, 2011Assignee: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Bei Chen, Tetsuo Uno
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Publication number: 20110251222Abstract: The invention relates to sulphone-substituted anilinopyrimidine derivatives of the formula (I), to its preparation processes, and to its use as medicament for treating various diseases.Type: ApplicationFiled: October 8, 2009Publication date: October 13, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Lücking, Gerhard Siemeister, Philip Lienau, Rolf Jautelat, Julia Schulze
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Publication number: 20110251174Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 14, 2011Publication date: October 13, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl ZAHN, Guido BOEHMELT, Andreas MANTOULIDIS, Ulrich REISER, Matthias TREU, Ulrich GUERTLER, Andreas SCHOOP, Flavio SOLCA, Ulrike TONTSCH-GRUNT, Ralph BRUECKNER, Charlotte REITHER, Lars HERFURTH, Oliver KRAEMER, Heinz STADTMUELLER, Harald ENGELHARDT
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Publication number: 20110245156Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.Type: ApplicationFiled: December 9, 2009Publication date: October 6, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais M. Sielecki-Dzurdz
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Publication number: 20110245284Abstract: Alkoxy- and alkylthio-substituted anilinopyrimidines of the formula (I) in which R1 to R14 and E1, E2, E3, X and Y have the meanings given in the description, and agrochemically active salts thereof, their use, and methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seeds of plants, processes for preparing such compositions and treated seeds and also their use for controlling phytopathogenic hal inful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for the preparation of alkoxy- and alkylthio-substituted anilinopyrimidines of the formula (I).Type: ApplicationFiled: August 21, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Chirstoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano, Ulrich Heinemann
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Publication number: 20110245242Abstract: Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R10 and L1, L2, E1, E2, E3, Y and Z have the meanings given in the description, and agrochemically active salts thereof, their use and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing heterocyclically substituted anilinopyrimidinenes of the formula (I).Type: ApplicationFiled: August 21, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hille, Kerstin Ilgö, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Arnd Voerste, Peter Dahmen, Rurth Meissner, Christoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano
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Publication number: 20110245249Abstract: Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R12 and E1, E2, E3, L1, Y, Z and L2 have the meanings given in the description, and agrochemically active salts thereof, their use and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing heterocyclically substituted anilinopyrimidinenes of the formula (I).Type: ApplicationFiled: August 22, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Pierre Wasnaire, Jorg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Christoph Andreas Braun, Martin Kaussmann, Hiroyuki Hadano
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Patent number: 8030483Abstract: The present invention provides stereoisomers and stereoisomeric mixtures of 3-amino carbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.Type: GrantFiled: January 16, 2009Date of Patent: October 4, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Ankush Argade, Rajinder Singh, Hui Li
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Publication number: 20110237612Abstract: Thienylaminopyrimidines of the formula (I) in which to R1 to R10 and X1 and X2 have the meanings given in the description, and agrochemically active salts thereof, their use and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing thienylaminopyrimidines of the formula (I).Type: ApplicationFiled: August 22, 2009Publication date: September 29, 2011Applicant: BayerCropScience AGInventors: Jörg Nico Greul, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Carl Friedrich Nising, Pierre Wasnaire, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Christoph Andreas Braun, Martin Kaussmann, Hiroyuki Hadano
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Publication number: 20110230478Abstract: Use of 4-alkyl-substituted diaminopyrimidines of the formula (I) as fungicide in which R1 to R13 and X1 and X2 have the meanings given in the description, and agrochemically active salts thereof, and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing diaminopyrimidines of the formulae (Ia), (Ib) and (Ic).Type: ApplicationFiled: August 26, 2009Publication date: September 22, 2011Applicant: Bayer ScienceCrop AGInventors: Jörg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Urike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Christoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano, Marcel Calleja
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Publication number: 20110218338Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritus.Type: ApplicationFiled: April 11, 2011Publication date: September 8, 2011Inventors: Hui Cai, Frank Chavez, James P. Edwards, Anne E. Fitzgerald, Jing Liu, Neelakandha S. Mani, Danielle K. Neff, Michele C. Rizzolio, Brad M. Savall, Deborah M. Smith, Jennifer D. Venable, Jianmei Wei, Ronald L. Wolin
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Patent number: 8012959Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: GrantFiled: September 22, 2008Date of Patent: September 6, 2011Assignee: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masashiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110212077Abstract: The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: August 24, 2010Publication date: September 1, 2011Applicant: TargeGen, Inc.Inventors: Glenn Noronha, Chi Ching Mak, Jianguo Cao, Joel Renick, Andrew McPherson, Binqi Zeng, Ved P. Pathak, Daniel L. Lohse, John D. Hood, Richard M. Soll
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Patent number: 8008307Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: GrantFiled: August 6, 2007Date of Patent: August 30, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
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Patent number: 8003789Abstract: This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halType: GrantFiled: October 31, 2007Date of Patent: August 23, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 8003788Abstract: A method for preparing a compound of formula k or a salt or solvate thereof, wherein R1 is as defined herein, the method comprising treating a compound of formula j or a salt or solvate thereof, with ammonia, to form the compound of formula k.Type: GrantFiled: October 4, 2007Date of Patent: August 23, 2011Assignee: Roche Palo Alto LLCInventors: Charles Alois Dvorak, Keena Lynn Green, Gary R. Lee