Two Of The Ring Nitrogens Are Bonded Directly To Each Other Patents (Class 546/119)
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Publication number: 20130165478Abstract: The present invention relates to novel pyrazolopyridinone derivatives according to formula (I) and a process of manufacturing thereof. These pyrazolopyridinone derivatives can be used as LPA receptor antagonists for the treatment of various herein disclosed diseases.Type: ApplicationFiled: August 5, 2011Publication date: June 27, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Kai Schiemann, Wolfgang Staehle, Dirk Wienke
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Publication number: 20130165439Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R5 are defined as in claim 1, which are suitable for treating diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: February 25, 2013Publication date: June 27, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Darryl MCCONNELL, Lars van der VEEN, Tobias WUNBERG
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Publication number: 20130156756Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.Type: ApplicationFiled: June 14, 2011Publication date: June 20, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Marcus Koppitz, Detlef Stöckigt, Olaf Prien
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Publication number: 20130150361Abstract: Compounds of formula (I): wherein R2, W, A, Y, and R1 are as defined in the specification, and pharmaceutically acceptable salts thereof, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130150343Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8461176Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives substantially enriched in an enantiomer of formula (I): and compounds of formula (IH) wherein R3, R4, R5, R6, R7, R13a, R13b, R14a, R14b, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.Type: GrantFiled: November 13, 2009Date of Patent: June 11, 2013Assignee: Merial LimitedInventors: Mark David Soll, Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Douglas Edward Wilkinson, Robert Toms Jacobs, Brent Christopher Beck
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Patent number: 8461180Abstract: Compounds of formula (I): wherein c, X, Y, R2, R4 and R5 are defined herein, are useful as inhibitors of HIV replication.Type: GrantFiled: November 13, 2008Date of Patent: June 11, 2013Assignee: Gilead Sciences, Inc.Inventors: Youla S. Tsantrizos, Murray D. Bailey, Punit-Kumar Bhardwaj, Christian Brochu, Paul J. Edwards, Lee Fader, Araz Jakalian, Stephen Kawai, Mathieu Parisien, Marc-Andre Poupart, Bruno Simoneau
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Publication number: 20130143914Abstract: Compounds of formula (I) are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory wherein R1 is a radical of formula (IA) or (IB) or (IC): 10 Y is -0- or —S(0)p- wherein p is 0, 1 or 2; A is an optionally substituted cycloalkylene radical having 5, 6 or 7 ring atoms fused to a phenyl ring; and R2, R3b and R4b are as defined in the claims.Type: ApplicationFiled: June 9, 2011Publication date: June 6, 2013Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Chi-Kit Woo, Monique Bodil Van Niel
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Publication number: 20130143863Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: ApplicationFiled: November 29, 2012Publication date: June 6, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130143915Abstract: The present invention relates to compounds of Formula (I), wherein R1 to R6 have the meaning as cited in the description and the claims. Said compounds are useful as TYK2 inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immuno logically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as their use as medicaments.Type: ApplicationFiled: June 28, 2011Publication date: June 6, 2013Applicant: CELLZOME LIMITEDInventors: Katie Ellard, Nigel Ramsden
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Publication number: 20130143900Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 26, 2012Publication date: June 6, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GMBH
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Patent number: 8455486Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: September 22, 2009Date of Patent: June 4, 2013Assignee: Genkyotex SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Patent number: 8455485Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: September 22, 2009Date of Patent: June 4, 2013Assignee: Genkyotex SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Patent number: 8450343Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).Type: GrantFiled: December 4, 2008Date of Patent: May 28, 2013Inventors: Xianhai Huang, Anandan Palani, Jun Qin, Robert G. Aslanian, Zhaoning Zhu, William Greenlee, Hubert Josien, Wei Zhou, Xiaohong Zhu, Chad E. Bennett, Dmitri Pissarnitski, Mihirbaran Mandal, Pawan Dhondi, Troy McCracken, Thomas Bara, Zhiqiang Zhao, Duane Burnett, John Clader
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Patent number: 8450340Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: GrantFiled: December 15, 2010Date of Patent: May 28, 2013Assignee: Samumed, LLCInventors: John Hood, Sunil Kumar K C, David Mark Wallace
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Patent number: 8450490Abstract: This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.Type: GrantFiled: September 14, 2012Date of Patent: May 28, 2013Assignee: Gilead Sciences, Inc.Inventors: William R. Baker, Shaopei Cai, Joshua Aaron Kaplan, Musong Kim, Gary Phillips, Lafe J. Purvis, II, Marcin Stasiak, Kirk L. Stevens, Josh Van Veldhuizen
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Patent number: 8445681Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: July 29, 2011Date of Patent: May 21, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Sharn Ramaya, Shazia Keily, Jingrong Cao
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Publication number: 20130123271Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder.Type: ApplicationFiled: June 22, 2011Publication date: May 16, 2013Applicant: FOVEA PHARMACEUTICALSInventors: David Middlemiss, Caroline Leriche
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Publication number: 20130121994Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of proliferative diseases, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: November 26, 2010Publication date: May 16, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Tobias Marquardt, Christof Wegscheid-Gerlach, Gerhard Siemeister, Stefan Prechtl, Antje Margret Wengner, Ulf Bömer
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Publication number: 20130123256Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: GENKYOTEX SAInventor: Genkyotex Sa
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Publication number: 20130116430Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: ApplicationFiled: December 28, 2012Publication date: May 9, 2013Applicant: FUJIFILM CORPORATIONInventors: Hideyasu FUJIWARA, Kimihiko SATO, Shinsuke MIZUMOTO, Yuichiro SATO, Hideki KURIHARA, Yohei KUBO, Hiyoku NAKATA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Shinji HAGIWARA, Mari YAMAMOTO
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Patent number: 8435987Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: August 3, 2011Date of Patent: May 7, 2013Assignee: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
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Patent number: 8431596Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.Type: GrantFiled: October 10, 2008Date of Patent: April 30, 2013Assignee: Cancer Research Technology LimitedInventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Wynne
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Publication number: 20130102587Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.Type: ApplicationFiled: March 14, 2011Publication date: April 25, 2013Applicant: PROXIMAGEN LIMITEDInventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
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Publication number: 20130102629Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 25, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130096110Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: February 11, 2011Publication date: April 18, 2013Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
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Patent number: 8420812Abstract: A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.Type: GrantFiled: December 23, 2009Date of Patent: April 16, 2013Assignee: SanofiInventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Jorge Alonso, Matthias Urmann, Nis Halland
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Patent number: 8420666Abstract: The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors.Type: GrantFiled: March 14, 2008Date of Patent: April 16, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Sonali Rudra, Nidhi Gupta, Lalit Kumar Baregama, Ritu Agarwal, Vinayak Vasantrao Khairnar, Mandadapu Raghu Ramaiah, Venkata P. Palle, Sarala Balachandran, Atul Kondaskar, Manohar Salla, Abhijit Ray, Sunanda G. Dastidar, Lalitha Vijaykrishnan
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Publication number: 20130085156Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 27, 2012Publication date: April 4, 2013Applicant: MSD K.K.Inventor: MSD K.K.
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Publication number: 20130085144Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.Type: ApplicationFiled: November 27, 2012Publication date: April 4, 2013Applicant: PIERRE FABRE MEDICAMENTInventor: PIERRE FABRE MEDICAMENT
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Patent number: 8410133Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds, the methods of using the aforementioned compounds, and compounds in the treatment of various diseases, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: June 2, 2010Date of Patent: April 2, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Philip Collier, Jeremy Green, Gregory Henkel, Michael Liu, Timothy Neuberger
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Publication number: 20130072495Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.Type: ApplicationFiled: May 16, 2011Publication date: March 21, 2013Inventors: An-Hu Li, Mark J. Mulvihill, Arno G. Steinig
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Publication number: 20130065895Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: August 13, 2012Publication date: March 14, 2013Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
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Patent number: 8394823Abstract: Disclosed are triazolopyridine compounds of the following Formula (I); or stereoisomers or salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof.Type: GrantFiled: April 10, 2009Date of Patent: March 12, 2013Assignee: Bristol-Myers Squibb CompanyInventor: Chongqing Sun
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Patent number: 8394795Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: February 27, 2009Date of Patent: March 12, 2013Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: Kateri A. Ahrendt, Alexandre J. Buckmelter, Jason De Meese, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, Paul Lunghofer, David Moreno, Brad Newhouse, Li Ren, Jeongbeob Seo, Hongqi Tian, Steven Mark Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
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Patent number: 8394843Abstract: Compounds are provided which have the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture which contain such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to activate glucokinase.Type: GrantFiled: July 18, 2011Date of Patent: March 12, 2013Assignee: Takeda California, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Robert J. Skene, Mingnam Tang, Sheldon X. Cao, David J. Hossfield, Jeffrey A. Stafford
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Publication number: 20130059835Abstract: The present invention provides heterocyclylamine derivatives of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: August 31, 2012Publication date: March 7, 2013Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, Wenqing Yao, Andrew P. Combs, Eddy W. Yue, Song Mei, Wenyu Zhu, Joseph Glenn, Thomas P. Maduskuie, JR., Richard B. Sparks, Brent Douty
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Patent number: 8389518Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: March 20, 2008Date of Patent: March 5, 2013Assignee: Genkyotex SAInventors: Patrick Page, Mike Orchard, Laetitia Fioraso-Cartier, Bianca Mottironi
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Publication number: 20130053375Abstract: Disclosed are quinoline compounds having the formula: wherein R1, R2 and A are as defined herein, and methods of making and using the same.Type: ApplicationFiled: May 6, 2011Publication date: February 28, 2013Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam Kenneth Charnley, Michael P. DeMartino, Xiaoyang Dong, Patrick Eidam, Pamela A. Haile, Philip Anthony Harris, Ami Lakdawala Shah, Bryan W. King, Robert W. Marquis, JR., John F. Mehlmann, Joseph J. Romano, Clark A. Sehon
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Patent number: 8383631Abstract: Provided are a novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one compound, a pharmaceutically acceptable salt compound thereof, a method for preparing the compound, and an anticancer pharmaceutical composition including the compound as an effective ingredient.Type: GrantFiled: September 16, 2010Date of Patent: February 26, 2013Assignee: Korea Institute of Science and TechnologyInventors: Ghilsoo Nam, Ae Nim Pae, Kyung Il Choi, Hyunah Choo, Vani Nelamane Devegowda, Seon Hee Seo
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Publication number: 20130039906Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
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Publication number: 20130039870Abstract: Cosmetic or dermatological preparations having an effective content of one or more thiazoles of the general formulaType: ApplicationFiled: February 21, 2011Publication date: February 14, 2013Applicant: Beiersdorf AGInventors: Ludger Kolbe, Cathrin Scherner
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Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
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Publication number: 20130035327Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 8, 2012Publication date: February 7, 2013Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20130035324Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 17, 2010Publication date: February 7, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Patent number: 8367829Abstract: This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.Type: GrantFiled: May 9, 2011Date of Patent: February 5, 2013Assignee: Gilead Sciences, Inc.Inventors: William R. Baker, Shaopei Cai, Joshua Aaron Kaplan, Musong Kim, Gary Phillips, Lafe J. Purvis, II, Marcin Stasiak, Kirk L. Stevens, Josh Van Veldhuizen
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Patent number: 8367830Abstract: The present invention relates to immobilization compounds of formula (I), immobilization products and preparations thereof as well as methods and uses for the identification of phosphatidylinositol kinase interacting compounds or for the purification or identification of phosphatidylinositol kinase proteins.Type: GrantFiled: May 14, 2010Date of Patent: February 5, 2013Assignee: Cellzome AGInventors: Kathryn Bell, Nigel Ramsden, Giovanna Bergamini Moore, Gitte Neubauer
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Publication number: 20130029995Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
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Publication number: 20130023532Abstract: Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R1, R1A, and R2 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: March 26, 2011Publication date: January 24, 2013Inventors: Linda N. Casillas, Subhas J. Chakravorty, Adam Kenneth Charnley, Pamela A. Haile, Terry Vincent Hughes, Jae U. Jeong, Jianxing Kang, Ami Lakdawala Shah, Lara Kathryn Leister, Robert W. Marquis, JR., Nathan Andrew Miller, Daniel J. Price, Clark A. Sehon, Gren Z. Wang, Daohua Zhang, Patrick Eidam