Additional Hetero Ring Other Than The Six-membered Hetero Rings Patents (Class 514/333)
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Publication number: 20140148471Abstract: The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Peter JESCHKE, Adeline KÖHLER, Joachim KLUTH, Friedrich August MÜHLTHAU, Yoshitaka SATO, Arnd VOERSTE, Eiichi SHIMOJO
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Publication number: 20140141975Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. Novel pyridine compounds for use in controlling pests are disclosed.Type: ApplicationFiled: November 1, 2013Publication date: May 22, 2014Applicant: Dow AgroSciences, LLCInventors: Noormohamed M. Niyaz, Francis E. Tisdell, Gerald B. Watson, James M. Renga, William C. Lo, Maurice C. H. Yap
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Publication number: 20140142097Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseasesType: ApplicationFiled: April 11, 2012Publication date: May 22, 2014Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
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Publication number: 20140142146Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: ApplicationFiled: November 21, 2013Publication date: May 22, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20140142081Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: ApplicationFiled: November 21, 2013Publication date: May 22, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
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Publication number: 20140142083Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: EPIZYME, INC.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy James Nelson Wigle, Masashi Seki
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Publication number: 20140134262Abstract: The present invention provides a compound of Formula I: for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride level; wherein R1, X1, R7, R5, C, L and p are defined herein. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride levels.Type: ApplicationFiled: July 6, 2012Publication date: May 15, 2014Inventors: Yoshie Arai, Margaret Elizabeth Brousseau, Jessie Gu, Tomoko Hayashi, Hironobu Mitani, Muneto Mogi, Kazuhiko Nonomura, Ken Yamada
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Publication number: 20140135322Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.Type: ApplicationFiled: July 13, 2012Publication date: May 15, 2014Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
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Publication number: 20140135331Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: May 16, 2013Publication date: May 15, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
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Patent number: 8716483Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 19, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alan B. Cooper, Yang Nan, Yongqi Deng, Gerald W. Shipps, Jr., Neng-Yang Shih, Hugh Y. Zhu, Jagdish A. Desai, James J-S Wang, Sunil Paliwal, Hon-Chung Tsui, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Ahmed Samatar
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Publication number: 20140121213Abstract: In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.Type: ApplicationFiled: July 3, 2012Publication date: May 1, 2014Inventors: Jeffrey Charles Boehm, Roderick S. Davis, Jeffrey Kerns, Guoliang Lin, Robert D. Murdoch, Hong NIE
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Patent number: 8710081Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: GrantFiled: July 16, 2013Date of Patent: April 29, 2014Assignee: Panmira Pharmaceuticals, LLCInventors: John H. Hutchinson, Petpiboon Peppi Prasit, Mark Moran, Jillian F. Evans, Jasmine Eleanor Zunic, Nicholas Simon Stock
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Publication number: 20140113907Abstract: The present invention provides a pyridylaminoacetic acid compound represented by the following formula (1): (wherein R1, R2, R3, Y and Z are as defined in the description and claims), or a pharmacologically acceptable salt thereof. Since the pyridylaminoacetic acid compound has EP2 agonistic action, it is useful as a therapeutic or prophylactic drug for respiratory diseases such as asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: December 16, 2013Publication date: April 24, 2014Applicant: UBE INDUSTRIES, LTD.Inventors: Ryo IWAMURA, Masayuki TANAKA, Tetsushi KATSUBE, Manabu SHIGETOMI, Eiji OKANARI, Yasunori TOKUNAGA, Hiroshi FUJIWARA
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Publication number: 20140113931Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: March 15, 2013Publication date: April 24, 2014Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Patent number: 8703760Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: December 17, 2010Date of Patent: April 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
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Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Publication number: 20140107132Abstract: The invention relates to certain compounds of Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: December 17, 2013Publication date: April 17, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Gary Bohnert, Nha Huu Vo, Qinglin Che, Zhiqiang Xia, Lijun Sun
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Patent number: 8697690Abstract: The present invention is directed to isoindolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: June 27, 2011Date of Patent: April 15, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Scott D. Kuduk, Youheng Shu, Zhi-Qiang Yang
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Patent number: 8697730Abstract: Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: GrantFiled: October 24, 2008Date of Patent: April 15, 2014Assignee: Panmira Pharmaceuticals, LLCInventors: Melissa Virginia Rewolinski, Kevin Murray Schaab, Christopher David King, Nicholas Simon Stock
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Patent number: 8697733Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: June 20, 2013Date of Patent: April 15, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20140100223Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:Type: ApplicationFiled: September 26, 2013Publication date: April 10, 2014Applicants: PRESIDENT & FELLOWS OF HARVARD COLLEGE, THE BROAD INSTITUTE, INC.Inventors: Mahmud Hussain, Daisuke Ito, Jason Law, Matthias Leiendecker, Ke Liu, Benito Munoz, Stuart Schreiber, Alykhan Shamji, Andrew Stern
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Publication number: 20140099333Abstract: The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 8, 2013Publication date: April 10, 2014Applicant: SANOFIInventors: Lothar SCHWINK, Martin BOSSART, Heiner GLOMBIK, Matthias GOSSEL, Dieter KADEREIT, Thomas KLABUNDE, Thomas MAIER, Siegfried STENGELIN
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Publication number: 20140100250Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.Type: ApplicationFiled: May 4, 2012Publication date: April 10, 2014Inventors: Michael D. Altman, Maria Emilia Di Francesco, Andrew M. Haidle, Ryan D. Otte, John Michael Ellis, Kaleen Konrad Childers, Alan B. Northrup, Liping Wang
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Patent number: 8691821Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: November 2, 2011Date of Patent: April 8, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
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Patent number: 8686004Abstract: The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds.Type: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Martin Füβlein, Peter Jeschke, Adeline Köhler, Joachim Kluth, Friedrich August Mühlthau, Yoshitaka Sato, Arnd Voerste, Eiichi Shimojo
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Patent number: 8686007Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 12, 2012Date of Patent: April 1, 2014Assignee: Cytokinetics, Inc.Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Patent number: 8685964Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: GrantFiled: October 12, 2010Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
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Patent number: 8685986Abstract: The present invention is to provide a medical composition for the treatment or prophylaxis of glaucoma which comprises a pyridylaminoacetic acid compound represented by the formula (1): wherein R1, R2, R3, Y, and Z are defined in the specification.Type: GrantFiled: March 30, 2010Date of Patent: April 1, 2014Assignee: Ube Industries, Ltd.Inventors: Masahiko Hagihara, Kenji Yoneda, Eiji Okanari, Manabu Shigetomi
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Publication number: 20140088071Abstract: Compounds of Formula (IA) and Formula (IB) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: November 2, 2011Publication date: March 27, 2014Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Takashi Nakai, Thomas Wai-Ho Lee, Charles Kim, Joel Moore, Nicholas Robert Perl, Jason Rohde
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Publication number: 20140088148Abstract: Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.Type: ApplicationFiled: April 4, 2012Publication date: March 27, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Sivanesan Dakshanamurthy, Milton L. Brown, Robert Clarke, Ayesha N. Shahjahan, Jaqueline Smith
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Patent number: 8680120Abstract: A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: GrantFiled: July 26, 2010Date of Patent: March 25, 2014Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Naohiro Kawamura, Tatsuhiro Kondo, Atsushi Kondo
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Tris-Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors
Publication number: 20140080866Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.Type: ApplicationFiled: November 26, 2013Publication date: March 20, 2014Applicant: University of Kentucky Research FoundationInventors: Peter Crooks, Linda DWOSKIN, Roger Papke, Guangrong ZHENG, Sangeetha SUMITHRAN -
Patent number: 8673941Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: GrantFiled: July 30, 2009Date of Patent: March 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
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Publication number: 20140073658Abstract: Disclosed herein are compounds, or pharmacologically acceptable salts thereof, having glucokinase activating activity.Type: ApplicationFiled: September 9, 2013Publication date: March 13, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Satoru Kaneko, Hiroyuki Tsuruoka, Masatoshi Honzumi, Manabu Abe, Taishi Yoshida
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Publication number: 20140073634Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 13, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
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Publication number: 20140068820Abstract: The present invention relates to novel pyrazole compounds of the formulae I and II, to their salts and their N-oxides which can be used for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The present invention also relates to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a pyrazole radical of the formulae A1, A2 or A3 # denotes the binding site to the remainder of formulae I or II; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and wherein R41, R42, R43, R51, R52, R53, R61, R62, R63, are as defined in claim 1.Type: ApplicationFiled: November 6, 2013Publication date: March 6, 2014Applicant: BASF SEInventors: Steffen GROSS, Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang von DEYN, Michael PUHL, Karsten KOERBER, Douglas D. ANSPAUGH, Deborah L. CULBERSTON, Hassan OLOUMI-SADEGHI
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Publication number: 20140057882Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.Type: ApplicationFiled: October 8, 2013Publication date: February 27, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta ARMANI, GABRIELE AMARI, LAURA CARZANIGA, CARMELIDA CAPALDI, ORIANA ESPOSITO, GINO VILLETTI, RENATO DE FANTI
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Publication number: 20140057920Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20140057916Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20140057926Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
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Patent number: 8658650Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.Type: GrantFiled: January 28, 2010Date of Patent: February 25, 2014Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
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Publication number: 20140051681Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: ApplicationFiled: May 3, 2013Publication date: February 20, 2014Inventors: David John AUGERI, Jeffrey Thomas BAGDANOFF, Simon David Peter BAUGH, Marianne CARLSEN, Kenneth Gordon CARSON, John Anthony GILLERAN, Wei HE, Tamas ORAVECZ, Konstantin SALOJIN, Leonard SUNG
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Publication number: 20140051575Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: March 30, 2012Publication date: February 20, 2014Inventors: Juergen Benting, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Daniela Portz, Anne-Sophie Rebstock, Ulrike Wachendorff-Neumann
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Patent number: 8653000Abstract: The present invention relates to imine compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.Type: GrantFiled: September 30, 2011Date of Patent: February 18, 2014Assignee: BASF SEInventors: Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertrud Bandur, Deborah L. Culbertson, Douglas D. Anspaugh, Franz Josef Braun
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Publication number: 20140045811Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 18, 2013Publication date: February 13, 2014Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
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Publication number: 20140045895Abstract: A pharmaceutical depot comprising (i) 5-fluoro-2-[[(1S)-1-(5-fluoro-2-pyridyl)ethyl]amino]-6-[(5-isopropoxy-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.Type: ApplicationFiled: September 12, 2013Publication date: February 13, 2014Applicant: ASTRAZENECA ABInventors: Armelle Marie-Laudine JANIN, Philip Alexander Macfaul, Rachel Marie Pugh, Emily Jane Roberts, Ian Alun Nash
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Publication number: 20140045778Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:Type: ApplicationFiled: January 3, 2013Publication date: February 13, 2014Applicants: THE KITASATO INSTITUTE, MEIJI SEIKA PHARMA CO., LTD.Inventors: MEIJI SEIKA PHARMA CO., LTD., THE KITASATO INSTITUTE
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Publication number: 20140045896Abstract: The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.Type: ApplicationFiled: May 2, 2012Publication date: February 13, 2014Applicant: XUANZHU PHARMA CO., LTD.Inventors: Hui Zhang, Mingwei Fan, Liang Sun
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Publication number: 20140045815Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: September 5, 2013Publication date: February 13, 2014Applicant: Samumed, LLCInventors: John Hood, Sunil Kumar KC
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Patent number: 8648201Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R7 and Y have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors and for the treatment of inflammatory diseases.Type: GrantFiled: June 17, 2010Date of Patent: February 11, 2014Assignee: MERCK PATENT GmbHInventors: Michel Calderini, Margarita Wucherer-Plietker, Ulrich Graedler, Christina Esdar