Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding Patents (Class 548/364.1)
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Patent number: 8642642Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.Type: GrantFiled: April 18, 2007Date of Patent: February 4, 2014Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KGInventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
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Publication number: 20140024680Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: ApplicationFiled: January 9, 2013Publication date: January 23, 2014Applicant: Bayer Intellectual Property GmbHInventor: Bayer Intellectual Property GmbH
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Publication number: 20140018544Abstract: The present invention provides NO-releasing NONOate(nitrogen bound)sulfonamide-linked-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, X, L, R2, R3, R4, and Z are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis or acne, using a compound of Formula (I).Type: ApplicationFiled: July 12, 2013Publication date: January 16, 2014Inventors: Eduardo J. Martinez, John J. Talley, Kevin D. Jerome, Terri L. Boehm
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Publication number: 20140011997Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: THERAVANCE, INC.Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
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Patent number: 8623902Abstract: Compounds of Formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: GrantFiled: June 9, 2009Date of Patent: January 7, 2014Assignee: Syngenta Crop Protection, LLCInventors: Daniel Stierli, Harald Walter, Sebastian Wendeborn, Antoine Daina
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Patent number: 8623860Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: December 14, 2012Date of Patent: January 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
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Publication number: 20130345419Abstract: Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 15, 2012Publication date: December 26, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Naoya Ono, Shoichi Kuroda, Yoshihisa Shirasaki, Tetsuo Takayama, Yoshinori Sekiguchi, Fumihito Ushiyama, Yusuke Oka
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Patent number: 8614243Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: GrantFiled: June 8, 2010Date of Patent: December 24, 2013Assignee: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Patent number: 8614206Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, 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: GrantFiled: September 26, 2012Date of Patent: December 24, 2013Assignee: F. Hoffmann-La Roche AGInventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
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Patent number: 8614242Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, 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: October 20, 2011Date of Patent: December 24, 2013Assignee: Bayer Intellectual Property GmbHInventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Publication number: 20130331328Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: GEORGETOWN UNIVERSITYInventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
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Patent number: 8598078Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: August 21, 2008Date of Patent: December 3, 2013Assignee: Syngenta Crop Protection, LLCInventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
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Patent number: 8592475Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: GrantFiled: October 14, 2009Date of Patent: November 26, 2013Assignee: GlaxoSmithKline LLCInventors: Meagan B. Rouse, Mark Andrew Seefeld
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Patent number: 8592471Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: GrantFiled: May 6, 2010Date of Patent: November 26, 2013Assignee: Gruenenthal GmbHInventors: 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
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Publication number: 20130310395Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 13, 2013Publication date: November 21, 2013Applicant: NOVARTIS AGInventors: Stephanie Kay DODD, Pascal FURET, Robert Martin GROTZFELD, Darryl Brynley JONES, Paul William MANLEY, Andreas MARZINZIK, Xavier Francois Andre PELLE, Bahaa SALEM, Joseph SCHOEPFER
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Patent number: 8586536Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: December 14, 2011Date of Patent: November 19, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
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Publication number: 20130303515Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.Type: ApplicationFiled: January 10, 2012Publication date: November 14, 2013Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédicte Pourbaix-L'ebraly
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Publication number: 20130296322Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: July 8, 2013Publication date: November 7, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Publication number: 20130289003Abstract: A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.Type: ApplicationFiled: October 25, 2011Publication date: October 31, 2013Inventors: Amjad Ali, Michael Man-Chu Lo, Robert K. Baker, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Edward Metzger, Lin Yan, Shrenik K. Shah, James Dellureficio, Jun Wang
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Patent number: 8569376Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.Type: GrantFiled: March 1, 2013Date of Patent: October 29, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Publication number: 20130274227Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
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Patent number: 8557858Abstract: A salt of (E)-N-{2-amino-phenyl)-3-{1-[4-(1-methyl-1 H-pyrazol-4-yl)-be?zenesulfonyl]-1 H-pyrrol-3-yl)-acrylamide selected from the group consisting of the hydrobromide, methansulfonate, hemi ethane-1,2-disulfonate, benzenesulfonate, toiuenesulfonate and 2-naphthalenesulfonate.Type: GrantFiled: March 11, 2009Date of Patent: October 15, 2013Assignee: 4SC AGInventors: Jürgen Volz, Martin Feth, Rolf-Peter Hummel, Matthias Müller, Thomas Maier, Bernd Müller
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Publication number: 20130237514Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.Type: ApplicationFiled: October 5, 2012Publication date: September 12, 2013Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
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Publication number: 20130231373Abstract: The present teachings relate to compounds of Formula (I): and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, R4, R5, ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula (I) and methods of use compounds of Formula (I) in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: August 27, 2010Publication date: September 5, 2013Applicant: Novartis AGInventors: Clinton Alan Brooks, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Gang Liu, Michael David Schultz
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Publication number: 20130231378Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: February 22, 2013Publication date: September 5, 2013Applicant: GlaxoSmithKline LLCInventors: Mark A. SEEFELD, Meagan B. Rouse, Dirk A. Heerding, Dennis S. Yamashita, Kenneth C. McMulty
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Patent number: 8524718Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: GrantFiled: September 6, 2012Date of Patent: September 3, 2013Assignee: Addex Pharma S.A.Inventors: Christelle Boléa, Sylvain Celanire
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Patent number: 8524750Abstract: A compound of Formula (I) wherein: either X is N and Y is CR5 or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and Me; R2 is selected from H, OH, OMe and Me; each R3 is independently selected from C1-3alkyl, F, Cl, Br, CF3 and NH2; R4 is selected from Me, CF3, NO2 and CHF2; R5 is selected from H, Me and CHF2; R6 is selected from H and Me; and p is 0-3, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.Type: GrantFiled: April 13, 2010Date of Patent: September 3, 2013Assignee: Glaxo Group LimitedInventors: Lluis Ballell Pages, Julia Castro Pichel, Raquel Fernandez Menendez, Esther Pilar Fernandez Velando, Silvia Gonzalez Del Valle, Maria Luisa Leon Diaz, Alfonso Mendoza Losana, Matthew James Wolfendale
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Publication number: 20130217727Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, 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: ApplicationFiled: October 20, 2011Publication date: August 22, 2013Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Patent number: 8513244Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: May 18, 2012Date of Patent: August 20, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Adam D. Hughes
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Patent number: 8492371Abstract: Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions are also disclosed.Type: GrantFiled: March 26, 2010Date of Patent: July 23, 2013Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Tongmei Li, Bo Liu, Sridhar Peddi, Xueqing Wang, Teodozyj Kolasa, Derek W. Nelson, Arturo Perez-Medrano
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Publication number: 20130184238Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: March 8, 2013Publication date: July 18, 2013Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130172312Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Inventors: Bernd NOSSE, Martin FLECK, Niklas HEINE, Gerald Juergen ROTH
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Publication number: 20130172316Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8470857Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: GrantFiled: August 14, 2009Date of Patent: June 25, 2013Assignee: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20130158004Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: ApplicationFiled: December 14, 2012Publication date: June 20, 2013Inventors: Martin FLECK, Bernd NOSSE, Niklas HEINE, Gerald Juergen ROTH
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Publication number: 20130158029Abstract: The invention refers to compounds of general formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: May 26, 2011Publication date: June 20, 2013Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia López, Antoni Torrens Jover, José Luis Diaz Fernández, Ana Maria Caamaño Moure
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Publication number: 20130150325Abstract: The present application relates to novel 3-(fluorovinyl)pyrazole derivatives, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: July 17, 2012Publication date: June 13, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael HÄRTER, Hartmut BECK, Karl-Heinz THIERAUCH, Peter ELLINGHAUS, Susanne GRESCHAT, Joachim SCHUHMACHER
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Patent number: 8461184Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: GrantFiled: July 27, 2010Date of Patent: June 11, 2013Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Bernard J. Vliet Van
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Publication number: 20130137687Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R7 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 20, 2012Publication date: May 30, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130131321Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
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Publication number: 20130123507Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.Type: ApplicationFiled: January 16, 2013Publication date: May 16, 2013Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO. LTD., JIANGSU HENGRUI MEDICINE CO. LTD.Inventors: JIANGSU HENGRUI MEDICINE CO. LTD., SHANGHAI HENGRUI PHARMACEUTICAL CO. LTD.
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Patent number: 8436034Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a? and I-A.a? in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: December 28, 2007Date of Patent: May 7, 2013Assignee: Abbott GmbH & Co. KGInventors: Andreas Kling, Wilfried Hornberger, Helmut Mack, Achim Moeller, Volker Nimmrich, Dietmar Seeman, Wilfried Lubisch
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Patent number: 8436001Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, 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: GrantFiled: April 6, 2011Date of Patent: May 7, 2013Assignee: F. Hoffmann-La Roche AGInventor: Xiaojing Wang
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Patent number: 8426471Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, and R4 are as defined herein.Type: GrantFiled: July 13, 2012Date of Patent: April 23, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Patent number: 8420690Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: GrantFiled: February 7, 2008Date of Patent: April 16, 2013Assignee: GlaxoSmithKline LLCInventors: Mark Andrew Seefeld, Meagan B. Rouse
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Patent number: 8415359Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: GrantFiled: August 5, 2011Date of Patent: April 9, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Publication number: 20130085132Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.Type: ApplicationFiled: August 30, 2012Publication date: April 4, 2013Applicant: JAPAN TOBACCO INC.Inventors: Tomoya MIURA, Yosuke OGOSHI, Kazuhito UEYAMA, Dai MOTODA, Toshihiko IWAYAMA, Koichi SUZAWA, Hironobu NAGAMORI, Hiroshi UENO, Akihiko TAKAHASHI, Kazuyuki SUGIMOTO
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Patent number: 8410158Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: GrantFiled: February 7, 2008Date of Patent: April 2, 2013Assignee: GlaxoSmithKline LLCInventors: Mark A. Seefeld, Meagan B. Rouse, Dirk A. Heerding
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Patent number: 8410159Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.Type: GrantFiled: July 29, 2011Date of Patent: April 2, 2013Assignee: Laboratories del Dr. Esteve, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Patent number: 8404679Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.Type: GrantFiled: April 23, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Andreas Koblet, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer