1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
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Publication number: 20130012503Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 20, 2012Publication date: January 10, 2013Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
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Publication number: 20130012382Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents are as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
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Publication number: 20130005965Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: July 2, 2012Publication date: January 3, 2013Applicants: BRISTOL-MYERS SQUIBB COMPANY, ALBANY MOLECULAR RESEARCH, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Publication number: 20130005705Abstract: The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: June 27, 2012Publication date: January 3, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
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Publication number: 20130005695Abstract: The invention provides compounds of formula (I) wherein R4 is a group of formula (II) or (IIIa) or (IIIb) and R1, R2, R3, R5, a, b and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparationType: ApplicationFiled: May 15, 2012Publication date: January 3, 2013Applicant: AstraZeneca ABInventors: Rhonan Ford, Andrew Mather, Antonio Mete
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Patent number: 8344010Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: GrantFiled: December 23, 2009Date of Patent: January 1, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: V. S. Prasadarao Lingam, Abraham Thomas, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20120328661Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: October 20, 2010Publication date: December 27, 2012Applicant: ALLERGAN, INC.Inventors: Todd M. Heidelbaugh, John R. Cappiello, Phong X. Nguyen, Dario G. Gomez
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Publication number: 20120329802Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 20, 2012Publication date: December 27, 2012Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger
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Publication number: 20120329743Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: June 14, 2012Publication date: December 27, 2012Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
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Patent number: 8338607Abstract: Agents for pest control comprising cyclic amine compounds represented by the formula (1) or salts thereof or N-oxides thereof as an active ingredient, wherein Cy1 represents an unsubstituted or substituted 5-membered heterocycle or unsubstituted or substituted group represented by the formula (a) below, wherein Y1 and Y2 each independently represents nitrogen or carbon and symbol * represents the bonding positions.Type: GrantFiled: October 6, 2006Date of Patent: December 25, 2012Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Masahiro Kawaguchi, Daisuke Hanai, Takao Iwasa
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Publication number: 20120322784Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: December 16, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
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Publication number: 20120322785Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.Type: ApplicationFiled: December 14, 2011Publication date: December 20, 2012Applicant: Genentech, Inc.Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
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Publication number: 20120322795Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 14, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Zhidong CHEN, Stephane DE LOMBAERT, Michel Jose EMMANUEL, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Hidenori TAKAHASHI
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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Publication number: 20120316176Abstract: The present invention relates to derivatives of 7,8-dihydro-1H-imidazo[2,1-b]purin-4(5H)-one, compositions thereof and methods of use thereof for treating or preventing pain or an inflammatory disease.Type: ApplicationFiled: December 16, 2010Publication date: December 13, 2012Inventors: Deen Tulshian, Michael F. Czarniecki, Julius Matasi, Stephanie N. Brumfield
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Patent number: 8329725Abstract: The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: May 22, 2009Date of Patent: December 11, 2012Assignee: SanofiInventors: Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Ulrike Wendler, Maike Glien, Hans Matter, Eugen Falk
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Patent number: 8329692Abstract: Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: July 4, 2008Date of Patent: December 11, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20120309964Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.Type: ApplicationFiled: February 24, 2011Publication date: December 6, 2012Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
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Publication number: 20120309752Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, Y1, Y2, Y3, G, J, X1 and X2 are as defined in the disclosure.Type: ApplicationFiled: January 7, 2011Publication date: December 6, 2012Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Andris Juris Liepa, Robert James Pasteris, Thomas Martin Stevenson
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Patent number: 8324234Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein, R1, R3, R4, and R6 are each independently C1-3 alkyl; and R2 and R5 are each independently a hydrogen atom or C1-3 alkyl.Type: GrantFiled: February 6, 2009Date of Patent: December 4, 2012Assignee: Shiseido Company Ltd.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
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Patent number: 8324186Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: April 15, 2010Date of Patent: December 4, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Heather Rae Hufnagel, Zhihua Sui
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Patent number: 8324199Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: March 12, 2009Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Zilun Hu, Mimi L. Quan
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Publication number: 20120302576Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Publication number: 20120295913Abstract: In one aspect, the invention relates to bicyclic pyrazole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: December 7, 2011Publication date: November 22, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Carrie K. Jones, Shaun R. Stauffer, José Manuel Bartolome-Nebreda, Gregor James McDonald, Susana Conde-Ceide, Han Min Tong
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Publication number: 20120295896Abstract: The present invention relates to compounds of formula (I) and (IA): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: September 20, 2011Publication date: November 22, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, Jonathon Alan DINES, John D. HUBER, Weimin W. LIU, Pui Leng LOKE, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20120295902Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: December 17, 2010Publication date: November 22, 2012Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Patent number: 8314087Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: February 15, 2008Date of Patent: November 20, 2012Assignee: Amgen Inc.Inventors: Brian K. Albrecht, Steven Bellon, Shon Booker, Alan C. Cheng, Derin D'Amico, Noel D'Angelo, Jean-Christophe Harmange, Tae-Seong Kim, Longbin Liu, Mark H. Norman, Aaron C. Siegmund, Markian Stec, Ning Xi, Kevin Yang
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Patent number: 8314103Abstract: The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1? (HIF-1?) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1? pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-?.Type: GrantFiled: August 6, 2008Date of Patent: November 20, 2012Assignee: Piramal Enterprises LimitedInventors: Sanjay Kumar, Kalpana Sanjay Joshi, Vijaykumar Deore, Mandar Ramesh Bhonde, Nilambari Nilkanth Yewalkar, Amol Arun Padgaonkar, Asha Adrian Kulkarni-Almeida, Maggie Joyce Rathos, Sapna Parikh, Nilesh Madhukar Dagia
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Publication number: 20120289493Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: May 8, 2012Publication date: November 15, 2012Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20120289505Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: December 30, 2010Publication date: November 15, 2012Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Publication number: 20120289507Abstract: The present invention relates generally to novel compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders. The present invention includes novel compounds, novel compositions, methods of their use and methods of their manufacture, where such compounds are generally pharmacologically useful as agents in therapies whose mechanism of action involve methods of inhibiting tumorigenesis, tumor growth and tumor survival using agents that inhibit the Hedgehog and Smo signaling pathway.Type: ApplicationFiled: July 20, 2012Publication date: November 15, 2012Applicant: NOVARTIS AGInventors: Feng HE, Stefan PEUKERT, Karen MILLER-MOSLIN, Naeem YUSUFF, Zhuoliang CHEN, Bharat LAGU
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Publication number: 20120289700Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).Type: ApplicationFiled: December 17, 2010Publication date: November 15, 2012Inventors: Isami Hamamoto, Keiji Koizumi, Makio Yano, Masahiro Kawaguchi, Hazumi Nomura, Tetsuya Haruyama
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Publication number: 20120283264Abstract: 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: ApplicationFiled: November 2, 2011Publication date: November 8, 2012Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
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Patent number: 8304414Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: April 25, 2008Date of Patent: November 6, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Françoise Pierard
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Patent number: 8304434Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: GrantFiled: September 30, 2008Date of Patent: November 6, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengcheng Patrick Shao, Sriram Tyagarajan, Feng Ye
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Publication number: 20120277243Abstract: The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3?, R4, and R4? are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: ApplicationFiled: April 24, 2012Publication date: November 1, 2012Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20120277242Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: ApplicationFiled: June 11, 2012Publication date: November 1, 2012Applicant: ARRAY BIOPHARMA, INC.Inventors: Thomas Daniel AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Jay Bradford FELL, John P. FISCHER, Indrani W. GUNAWARDANA, Ronald Jay HINKLIN, Ajay SINGH, Timothy M. TURNER, Eli M. WALLACE
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Publication number: 20120277206Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: May 11, 2012Publication date: November 1, 2012Applicant: Andrea Boesciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Publication number: 20120277213Abstract: The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.Type: ApplicationFiled: April 23, 2012Publication date: November 1, 2012Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20120277205Abstract: The present invention relates to compounds corresponding to formula (I): in which: A represents a divalent aromatic radical; X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R3 represents a hydroxyl or a group —NR7R8; R4 represents a hydrogen atom, a halogen atom, a cyano, a phenyl, a group Alk, a group OAlk or a group —NR9R10; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: ApplicationFiled: September 13, 2011Publication date: November 1, 2012Applicant: SANOFIInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
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Publication number: 20120277430Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Takahiko TANIGUCHI, Jun Kunitomo
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Publication number: 20120277204Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Takahiko TANIGUCHI, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
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Publication number: 20120277431Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Takahiko Taniguchi, Jun Kunitomo
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Patent number: 8299076Abstract: Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: May 17, 2006Date of Patent: October 30, 2012Assignees: Array Biopharma Inc., Astrazeneca ABInventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, Jim Blake, Richard Anthony Storey, Rebecca Jane Booth, John David Pittam, John Leonard, Mark Richard Fielding
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Patent number: 8298994Abstract: The invention relates to 1-(3-diazinyl)pyrazol-4-ylacetic acid derivatives of the general formula (I) and salts thereof in which Het, R1, R2, R3, R4, R5, R6 and n are as defined in the specification. The compounds (I) and their salts are suitable as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants, and can be prepared by processes as described in the specification.Type: GrantFiled: June 17, 2009Date of Patent: October 30, 2012Assignee: Bayer Cropscience AGInventors: Harald Jakobi, Arianna Martelletti, Joerg Tiebes, Jan Dittgen, Dieter Feucht, Isolde Haeuser-Hahn, Heinz Kehne, Christopher Hugh Rosinger
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Patent number: 8299055Abstract: The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKK? inhibiting activity and the like and is useful for the prevention and/or treatment of IKK?-associated diseases or symptoms and the like.Type: GrantFiled: October 1, 2009Date of Patent: October 30, 2012Assignee: Asahi Kasei Pharma CorporationInventors: Shunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
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Publication number: 20120270856Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: ApplicationFiled: July 2, 2012Publication date: October 25, 2012Inventors: Tomoharu IINO, Akio OHNO, Norikazu OTAKE, Takuya SUGA, Masanori ASAI
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Publication number: 20120270871Abstract: Pyrrolopyridinylpyrimidin-2-ylamine derivatives of the formula (I), in which R1-R6 and R1 have the meanings indicated in claim 1, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: October 12, 2010Publication date: October 25, 2012Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Margarita Wucherer-Plietker, Christina Esdar, Brian Hodous