Pyrazoles Patents (Class 514/406)
-
Patent number: 9156790Abstract: Compounds according to formula I: wherein Ar is a fused aryl group, R1 is selected from alkyl and aryl amides, CF3, and CH2OH, and R2 is selected from hydrogen, —C(?O)CH2NH2, and —C(?O)CH2CH2NH2 are described. The compounds are effective for inhibiting p21-activated kinases, and can be used for prevention and treatment of cancer.Type: GrantFiled: March 31, 2014Date of Patent: October 13, 2015Assignee: Ohio State Innovation FoundationInventors: Ching-Shih Chen, Matthew David Ringel, Motoyashi Saji, Yihui Ma
-
Patent number: 9145369Abstract: The present invention relates to a novel method for preparing 1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful precursor for the preparation of fungicides, by means of reductive dehalogenation, starting from N-alkyl-3-haloalkyl-5-halopyrazolecarbaldehyde.Type: GrantFiled: May 10, 2013Date of Patent: September 29, 2015Assignee: BAYER CROPSCIENCE AGInventors: Sergii Pazenok, Norbert Lui, Thomas Norbert Mueller
-
Patent number: 9126946Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.Type: GrantFiled: October 27, 2009Date of Patent: September 8, 2015Assignee: Arena Pharmaceuticals, Inc.Inventors: Marlon Carlos, Weitong Dong, Mark Macias, Suzanne Michiko Sato, Lee Alani Selvey
-
Patent number: 9079899Abstract: A method of treating infection by Staphylococcus in a subject by administering a pharmaceutical composition including a celecoxib derivative of formula I or a pharmaceutically acceptable salt thereof is described. The preparation of numerous celecoxib derivatives for testing as potential anti-staphylococcal agents is also described.Type: GrantFiled: October 31, 2011Date of Patent: July 14, 2015Assignee: THE OHIO STATE UNIVERSITYInventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, Samuel K. Kulp
-
Patent number: 9078874Abstract: Compounds having inverse agonist functional selectivity for GABAA receptors containing the ?5 subunit for use as a medicament in the treatment of cognitive impairments in subjects suffering from Down syndrome. The use of these compounds is disclosed. Pharmaceutical compositions for such treatment can comprise these compounds or suitable pharmaceutically acceptable salt thereof, a polyethoxylated castor oil and dimethyl sulfoxide (DMSO). Methods are disclosed for enhancing cognitive function, or treating or lessening the severity of cognitive impairments, in subjects suffering from Down syndrome by administering to a subject in need thereof a pharmaceutically effective amount of one or more of these compounds.Type: GrantFiled: August 24, 2010Date of Patent: July 14, 2015Assignee: Centre National De La Recherche Scientifique—CNRSInventors: Marie-Caude Potier, Robert Dodd, Benoît Delatour, Jérôme Braudeau, Yann Herault
-
Patent number: 9073930Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 12, 2013Date of Patent: July 7, 2015Assignee: Merck Sharp & DohmeInventors: Ann E. Weber, Tesfaye Biftu
-
Publication number: 20150148349Abstract: The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 27, 2013Publication date: May 28, 2015Applicant: NOVARTIS AGInventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
-
Publication number: 20150148343Abstract: The present invention relates to novel sirtuin-modulating compounds, corresponding pharmaceutical compositions comprising a sirtuin-modulating compound, alone and/or in combination with another therapeutic agent, and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.Type: ApplicationFiled: January 29, 2015Publication date: May 28, 2015Inventors: Robert B. PERNI, Christopher Oalmann, Chi B. Vu
-
Publication number: 20150141418Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: ApplicationFiled: January 26, 2015Publication date: May 21, 2015Applicant: PTC Therapeutics, Inc.Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
-
Publication number: 20150141247Abstract: The present invention relates to novel 1-methyl-3-dihalogenomehtyl-5-halogenopyrazole(thio)biphenyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: ApplicationFiled: May 6, 2013Publication date: May 21, 2015Inventors: Simon Maechling, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise
-
Publication number: 20150141455Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 27, 2013Publication date: May 21, 2015Applicant: NOVARTIS AGInventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
-
Publication number: 20150141477Abstract: The present invention relates to compounds of the formula (I), wherein the residues R1 to R5, V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 16, 2013Publication date: May 21, 2015Inventors: Marc Nazare, Detlef Kozian, Andreas Evers, Werngard Czechtizky
-
Patent number: 9034911Abstract: The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like.Type: GrantFiled: October 27, 2009Date of Patent: May 19, 2015Assignee: Arena Pharmaceuticals, Inc.Inventors: Lee Alani Selvey, Marlon Carlos, Paul Maffuid, Yun Shan, William L. Betts, III, Deam Windate Given, III, Ryan M. Hart, Zezhi Jesse Shao
-
Publication number: 20150133422Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.Type: ApplicationFiled: November 8, 2013Publication date: May 14, 2015Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
-
Publication number: 20150132385Abstract: The present invention relates to nanocrystalline solid dispersion compositions having discrete particles, wherein each discrete particle comprises crystals of at least one pharmaceutical active; veterinary active; nutraceutical active dispersed in the matrix of at least one crystallization inducer and/or coexisting with crystals of crystallization inducer, optionally along with pharmaceutically acceptable excipients. The present invention also encompasses a novel one-step process for generation of nanocrystalline solid dispersions. The present invention is particularly of use for improving the dissolution of pharmaceutical actives, veterinary actives; nutraceutical actives exhibiting dissolution-limited bioavailability. Dissolution enhancement is because of the decreased crystallite size of the pharmaceutical active.Type: ApplicationFiled: March 7, 2013Publication date: May 14, 2015Inventors: Arvind Kumar Bansal, Ajay Kumar Raju Dantuluri, Shete Ganesh Bhaskarao, Pawar Yogesh Bapurao
-
Publication number: 20150126477Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;Type: ApplicationFiled: February 24, 2012Publication date: May 7, 2015Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
-
Publication number: 20150126371Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.Type: ApplicationFiled: May 29, 2013Publication date: May 7, 2015Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
-
Publication number: 20150126573Abstract: The present invention relates to methods and compositions for the prevention or treatment of chronic obstructive pulmonary disease.Type: ApplicationFiled: May 7, 2013Publication date: May 7, 2015Inventors: Jorge Bernardo Boczkowski, Serge Adnot, Maylis Dagouassat, Jean-Marie Gagliolo
-
Publication number: 20150126363Abstract: The present invention provides a composition comprising a pesticide and a copolymer, which contains in polymerized form acrylic acid and/or methacrylic acid (monomer A); a mono C12-C22 alkyl terminated poly(C2-6 alkylene glycol)(meth)acrylate (monomer B); and a C1-C8 alkyl(meth)acrylate (monomer C). Further on, it provides a process for preparing said composition by contacting the pesticide and the copolymer; a method for controlling phytopathogenic fungi and/or unwanted plant growth and/or unwanted insect or mite infestation and/or for regulating the growth of plants, wherein said composition is caused to act on the respective pests, their habitat or the plants to be protected from the respective pest, to the soil and/or to unwanted plants and/or the crop plants and/or their habitat; and a plant propagation material comprising said composition.Type: ApplicationFiled: March 22, 2013Publication date: May 7, 2015Inventors: Murat Mertoglu, Ann-Kathrin Marguerre, Vandana Kurkal-Siebert, Son Nguyen-Kim
-
Patent number: 9024041Abstract: There is provided a compound of formula (I): wherein: J represents (A): or (B): compositions comprising same, processes for preparing said compounds and use thereof in treatment, particularly in the treatment of inflammatory disease, such as asthma, COPD and 15 rheumatoid arthritis.Type: GrantFiled: April 8, 2011Date of Patent: May 5, 2015Assignee: Respivert Ltd.Inventors: John King-Underwood, Peter John Murray, Jonathan Gareth Williams, Ildiko Buck, Stuart Thomas Onions
-
Patent number: 9023883Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.Type: GrantFiled: March 14, 2014Date of Patent: May 5, 2015Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
-
Patent number: 9023874Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: GrantFiled: November 11, 2010Date of Patent: May 5, 2015Assignee: Merial, Inc.Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
-
Patent number: 9023882Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.Type: GrantFiled: June 12, 2012Date of Patent: May 5, 2015Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
-
Publication number: 20150119375Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: ApplicationFiled: May 6, 2013Publication date: April 30, 2015Applicant: Bayer Cropscience AGInventors: Pierre-Yves Coqueron, Mazen Es-Sayed, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Stephane Brunet, Helene Lachaise, Jean-Pierre Vors
-
Publication number: 20150119438Abstract: The present invention provides 3-{1-[5-chloro-2-(2-ethylbutoxy)benzyl]-5-methyl-1H-pyrazol-3-yl}propanoicacid in crystalline form. The present invention further provides methods for treating disorders associated with DP1, FP, TP, EP1 and EP4 prostaglandin (PG) receptors.Type: ApplicationFiled: October 31, 2014Publication date: April 30, 2015Inventors: Ke Wu, Gyorgy F. Ambrus
-
Publication number: 20150119243Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: ApplicationFiled: May 6, 2013Publication date: April 30, 2015Applicant: Bayer Cropscience AGInventors: Simon Maechling, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise, Pierre Genix
-
Publication number: 20150119242Abstract: The present invention relates to novel pyrazole(thio)tetrahydronaphthyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: ApplicationFiled: May 6, 2013Publication date: April 30, 2015Applicant: Bayer Cropscience AGInventors: Simon Maechling, Mazen Es-Sayed, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise
-
Publication number: 20150119329Abstract: The present invention is directed to a composition for the treatment or prevention of cerebral malaria that comprises an angiotensin receptor type-2 agonist and an antimalaria drug. The present invention is further directed to methods for treating and preventing cerebral malaria that involve administering an angiotensin receptor type-2 agonist and/or an angiotensin receptor type-1 antagonist.Type: ApplicationFiled: April 16, 2013Publication date: April 30, 2015Applicant: NEW YORK UNIVERSITYInventors: Ana Maria Rodriguez Fernandez, Julio Gallego-Delgado
-
Publication number: 20150119241Abstract: The present invention relates to novel 1-methyl-3-dihalogenomethyl-5-halogenopyrazole(thio)indanyl carbox-amides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: ApplicationFiled: May 6, 2013Publication date: April 30, 2015Inventors: Pierre-Yves Coqueron, Simon Maechling, Mazen Es-Sayed, Pierre Wasnaire, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stéphane Brunet, Hélène Lachaise, Pierre Genix
-
Publication number: 20150119439Abstract: The invention provides saturated acyl guanidine compounds that inhibit F1F0-ATPase, and methods of using saturated acyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: June 7, 2013Publication date: April 30, 2015Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
-
Patent number: 9018241Abstract: Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.Type: GrantFiled: December 17, 2012Date of Patent: April 28, 2015Assignee: Janssen Pharmaceutica, NVInventors: John R. Carson, James J. McNally
-
Patent number: 9018233Abstract: The invention relates to diaminoaryl derivatives substituted by carbamate, salts thereof and a pesticidal composition containing the same, which exhibit superior pest control effects against various insect pests of insect species, in particular against moths such as the diamondback moth or Spodoptera litura.Type: GrantFiled: May 7, 2013Date of Patent: April 28, 2015Assignees: Kyung Nong Corporation, Korea Research Institute of Chemical TechnologyInventors: Sung Youn Chang, Jung Nyoung Heo, Hyuk Lee, Hwan Jung Lim, Bum Tae Kim, Joo Kyung Kim, Jong-Kwan Kim
-
Patent number: 9018132Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 18, 2014Date of Patent: April 28, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
-
Publication number: 20150111890Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: April 19, 2013Publication date: April 23, 2015Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
-
Patent number: 9012478Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: GrantFiled: July 3, 2013Date of Patent: April 21, 2015Assignee: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
-
Publication number: 20150105433Abstract: Provided herein are methods for preventing or treating a viral infection in a subject, wherein the viral infection is mediated by a virus comprising one or more viral RNA molecules translated by a ribosomal shunting mechanism or a non-IRES mediated mechanism. The methods comprise administering to a subject an agent that reduces ribosomal protein (Rps25) expression or function. Also provided are methods of inhibiting or promoting ribosomal shunting-mediated translation or non-IRES mediated translation. Also provided are methods of screening for an agent that inhibits or promotes ribosomal shunting-mediated translation or non-IRES mediated translation.Type: ApplicationFiled: April 25, 2013Publication date: April 16, 2015Inventor: Sunnie R. Thompson
-
Publication number: 20150105429Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicant: GENENTECH, INC.Inventors: Benjamin Fauber, Olivier Rene
-
Publication number: 20150105375Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
-
Publication number: 20150105430Abstract: A method treats or prevents neuropathic pain with a synergistically-enhanced analgesic effect at a dose at which a calcium channel ?2? ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent used in the method includes as effective ingredients a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel ?2? ligand.Type: ApplicationFiled: December 19, 2014Publication date: April 16, 2015Inventors: Naoki Izumimoto, Hidenori Mochizuki
-
Publication number: 20150105403Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: March 14, 2013Publication date: April 16, 2015Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
-
Patent number: 9006249Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: June 7, 2012Date of Patent: April 14, 2015Assignee: Novartis AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
-
Publication number: 20150099728Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
-
Publication number: 20150099779Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.Type: ApplicationFiled: April 30, 2013Publication date: April 9, 2015Inventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
-
Publication number: 20150099766Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Michael MAUE, Isabelle ADELT, Wolfgang GIENCKE, Markus HEIL, Peter JESCHKE, Bernd-Wieland KRÜGER, Friedrich August MÜHLTHAU, Alexander SUDAU, Klaus RAMING, Ulrich EBBINGHAUS-KINTSCHER, Martin ADAMCZEWSKI, Arnd VOERSTE, Ulrich GÖRGENS, Tobias KAPFERER, Mark Wilhelm DREWES, Angela BECKER, Eva-Maria FRANKEN
-
Patent number: 8999956Abstract: The present invention relates to fungicidal N-[(het)arylalkyl)]pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogs, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: GrantFiled: June 1, 2011Date of Patent: April 7, 2015Assignee: Bayer Intellectual Property GmbHInventors: Jurgen Benting, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Ruth Meissner, Ulrike Wachendorff-Neumann
-
Patent number: 8999968Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: GrantFiled: July 3, 2013Date of Patent: April 7, 2015Assignee: University Health NetworkInventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
-
Publication number: 20150094350Abstract: The present invention relates to novel 1-methyl-3-dihalogenomethyl-5-halogenopyrazole(thio)benzofuranyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: ApplicationFiled: May 6, 2013Publication date: April 2, 2015Inventors: Joerg Nico Greul, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise
-
Publication number: 20150093338Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: October 8, 2014Publication date: April 2, 2015Inventor: Michael Farber
-
Patent number: 8993612Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: GrantFiled: October 6, 2010Date of Patent: March 31, 2015Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V S Varanasi, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
-
Publication number: 20150087683Abstract: Invented is a method of treating steroid responsive dermatoses in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a compound selected from the group consisting of: N-{(1S)-2-Amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide or a pharmaceutically acceptable salt thereof, and the compound N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide or a pharmaceutically acceptable salt thereof, to such mammal.Type: ApplicationFiled: April 22, 2013Publication date: March 26, 2015Inventors: Pankaj Agarwal, Vinod Kumar, Qing Xie