Five-membered Nitrogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/253.09)
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Publication number: 20110263559Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Inventors: Xuqing ZHANG, Marta G. ABAD, Alan C. GIBBS, Gee-Hong KUO, Lawrence C. KUO, Fengbin SONG, Zhihua SUI
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Publication number: 20110263566Abstract: 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives, which are useful for PBK inhibitors, are provided.Type: ApplicationFiled: July 30, 2009Publication date: October 27, 2011Inventors: Yo Matsuo, Yingfu Li, Joel Walker, Feryan Ahmed, Ryuji Ohsawa, Shoji Hisada
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Patent number: 8044079Abstract: The invention relates to novel oxindole derivative of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: December 1, 2006Date of Patent: October 25, 2011Assignee: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Publication number: 20110257194Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substitutes A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.Type: ApplicationFiled: May 20, 2011Publication date: October 20, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Hérve Geneste, Andrea Hager-Wernet
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Patent number: 8039622Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: GrantFiled: November 10, 2009Date of Patent: October 18, 2011Assignee: LG Life Sciences Ltd.Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, Dong Sup Shim, Soo Yong Chung
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Publication number: 20110245269Abstract: The present invention provides compounds of the formula, wherein A, B, G, R2, R6, and X are defined herein, pharmaceutical compositions of the same, and methods for treating or inhibiting development of AGE- and/or ALE-associated complications in subjects in need thereof.Type: ApplicationFiled: December 9, 2010Publication date: October 6, 2011Applicant: NephroGenex, Inc.Inventors: Raja G. Khalifah, Roger E. Marti
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Publication number: 20110245232Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: March 25, 2011Publication date: October 6, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker, Jayne Froggett
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Publication number: 20110245247Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: March 28, 2011Publication date: October 6, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker
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Publication number: 20110245223Abstract: The present invention provides a compound represented by the following formula [1?] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11?HSD1 inhibitor, containing the compound or a salt thereof.Type: ApplicationFiled: December 1, 2010Publication date: October 6, 2011Applicant: Japan Tobacco Inc.Inventors: Hiroshi Yamamoto, Yasuhiro Ohe, Hiroyuki Goto, Kazuhito Harada, Shinji Yata, Takashi Ito, Jun Nishiu, Makoto Kakutani, Shunsuke Fujii, Kota Asahina
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Patent number: 8017616Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: GrantFiled: December 21, 2009Date of Patent: September 13, 2011Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Stuart B. Rosenblum, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Douglas W. Hobbs
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Publication number: 20110218175Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.Type: ApplicationFiled: February 23, 2011Publication date: September 8, 2011Inventors: Yat Sun Or, Guoqiang Wang, Xuri Gao
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Patent number: 8012969Abstract: The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography.Type: GrantFiled: January 11, 2006Date of Patent: September 6, 2011Assignee: GE Healthcare LimitedInventors: Christopher John Helal, Gunnar Antoni, Bengt Langstrom, Jia Zhi Sheng, Susan Beth Sobolov-Jaynes, Timothy James McCarthy
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Publication number: 20110212973Abstract: [Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that a piperazine-1-carboxylate compound, in which benzimidazol-2-ylcarbonyl, benzofuran-2-ylcarbonyl or the like binds to the 4-position of the piperazine, has an excellent FAAH inhibitory activity and further has an action to increase the effective bladder capacity, an action to ameliorate sleep disorders, an anti-diuretic action, and an analgesic activity on lower urinary tract pain including bladder pain and the like, thereby completed the present invention.Type: ApplicationFiled: November 5, 2009Publication date: September 1, 2011Inventors: Takahiro Ishii, Takashi Sugane, Ryosuke Munakata, Satoshi Aoki, Masahide Higaki, Akiyoshi Someya
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Publication number: 20110212962Abstract: There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.Type: ApplicationFiled: October 2, 2009Publication date: September 1, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20110207743Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.Type: ApplicationFiled: October 27, 2009Publication date: August 25, 2011Inventors: Jerry Leroy Adams, Thomas H Faitg, Neil W Johnson, Hong Lin
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Publication number: 20110207688Abstract: The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.Type: ApplicationFiled: February 20, 2010Publication date: August 25, 2011Inventors: James Patrick Dunn, Todd Richard Elworthy, Dimitrios Stefanidis, Zachary Kevin Sweeney
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Publication number: 20110207742Abstract: There is to provide is an agent for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion comprising an effective amount of 2-[4-[2-(benzimidazole-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-p yridyl]acetamide (hereinafter, referred to as compound 1), its pharmaceutically acceptable salt or a hydrate thereof and Pitavastatin, and a pharmaceutically acceptable carrier, wherein the agent is intended to be simultaneously administered, or separately administered with interval of time to a patient in need thereof There is also to provide a method for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion, comprising simultaneously administering, or separately administering with interval of time an effective amount of the compound 1, its pharmaceutically acceptable salt or a hydrate thereof and an effecType: ApplicationFiled: April 28, 2011Publication date: August 25, 2011Applicant: KOWA CO., LTD.Inventors: Hideyuki Kobayashi, Yasunobu Yoshinaka, Kimiyuki Shibuya
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Patent number: 7998963Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.Type: GrantFiled: February 12, 2009Date of Patent: August 16, 2011Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20110195072Abstract: The present invention provides a method of selecting subjects suffering or being predisposed to suffering from a proliferative disease in non-neuroendocrine tissues for treatment with a Ret inhibitor. The present invention also provides Ret inhibitors as medicaments for subjects suffering or being predisposed to suffering from a proliferative disease in non-neuroendocrine tissues.Type: ApplicationFiled: September 10, 2007Publication date: August 11, 2011Inventors: Anne Boulay, Madlaina Breuleux, Nancy Hynes, Heidi A. Lane
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Patent number: 7994202Abstract: A nitrogen-containing bicyclic heterocyclic compound represented by the following formula (1) is provided. When the compound or a salt thereof is administered to a human being or an animal, the compound has a strong antagonistic action against EP1 receptors, and is useful, for example, as an active ingredient of a medicine for the prevention and/or treatment of overactive bladder. The compound is also useful as an active ingredient of a medicine for the prevention and/or treatment of symptoms such as frequency urinary, urinary urgency, or urinary incontinence.Type: GrantFiled: July 14, 2009Date of Patent: August 9, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Masakazu Atobe, Kenji Naganuma, Akifumi Morimoto
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Publication number: 20110178061Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: ApplicationFiled: December 17, 2010Publication date: July 21, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Andreas P. Termin, Esther Ann Martinborough, Nicole Hilgraf, Charles J. Cohen, Corey Anderson
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Publication number: 20110172238Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: July 16, 2010Publication date: July 14, 2011Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, JR., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingcan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
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Publication number: 20110172244Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: February 20, 2009Publication date: July 14, 2011Applicant: IRM LLCInventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
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Publication number: 20110166139Abstract: The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.Type: ApplicationFiled: June 15, 2009Publication date: July 7, 2011Applicant: ASTRAZENECA ABInventors: Bernard Christophe Barlaam, Patrick Ple, Kevin Michael Foote, Clifford David Jones
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Publication number: 20110160196Abstract: The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: December 22, 2010Publication date: June 30, 2011Inventors: Zhaozhong J. Jia, Yonghong Song, Robert M. Scarborough, Carroll Scarborough, Anjali Pandey
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Publication number: 20110152260Abstract: The present invention relates to modulators of IRAK kinases of formula (I) and provides compositions comprising such modulators, as well as methods therewith for treating IRAK-mediated or IRAK-associated conditions or diseases.Type: ApplicationFiled: September 7, 2007Publication date: June 23, 2011Applicant: Biogen Idec Ma Inc.Inventors: Kevin Guckian, Charles Jewell, Patrick Conlon, Edward Yin Shiang Lin, Timothy Chan
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Patent number: 7964602Abstract: The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.Type: GrantFiled: December 1, 2006Date of Patent: June 21, 2011Assignee: Glaxo Group LimitedInventors: Gregor James MacDonald, Darren Jason Mitchell, Mervyn Thompson, Susan Marie Westaway
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Publication number: 20110144106Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1.Type: ApplicationFiled: December 3, 2010Publication date: June 16, 2011Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Hongying Yun
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Publication number: 20110136809Abstract: The present invention relates to compounds of formula (I), pharmaceutical compositions which contain them and methods for treating cancer using compounds of formula (I).Type: ApplicationFiled: November 8, 2010Publication date: June 9, 2011Applicant: Bayer Pharmaceuticals CorporationInventors: Wendy LEE, Gaetan LADOUCEUR, Jacques DUMAS, Roger SMITH, Shihong YING, Gan WANG, Zhi CHEN, Qingjie LIU, Holia Hatoum MOKDAD
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Patent number: 7956058Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1?, R1?, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.Type: GrantFiled: June 7, 2006Date of Patent: June 7, 2011Assignee: Nereus Pharmaceuticals, Inc.Inventors: Yoshio Hayashi, Michael A. Palladino, Jr., Jennifer Grodberg
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Patent number: 7951807Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substituents A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.Type: GrantFiled: July 13, 2005Date of Patent: May 31, 2011Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Herve Geneste
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Publication number: 20110124628Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 22, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
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Publication number: 20110124658Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.Type: ApplicationFiled: December 28, 2007Publication date: May 26, 2011Applicant: ABBOTT GMBH & CO. KGInventors: Astrid Netz, Thorsten Oost, Herve' Geneste, Wilfried Martin Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20110118236Abstract: An object of the present invention is to provide a novel AMPA receptor potentiator. A compound represented by the following formula (I) or a salt thereof: wherein in formula (I) R1 represents (1) a halogen atom, or (2) cyano group, or the like; Ra and Rb each independently represent a hydrogen atom or C1-4 alkyl; L represents a bond, or a spacer in which the number of atoms in the main chain is 1 to 8; Ring A represents (1) a non-aromatic carbon ring of 4-8 carbon atoms, or (2) a 4- to 8-membered non-aromatic heterocycle either of which is optionally substituted with 1 or more substituents selected from (a) halogen atoms, and (b) cyano group; and Ar represents a substituted phenyl group, or optionally substituted 5- or 6-membered aromatic heterocyclic group.Type: ApplicationFiled: March 25, 2009Publication date: May 19, 2011Inventors: Michiyo Mochizuki, Shotaro Miura
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Publication number: 20110118280Abstract: The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: January 24, 2011Publication date: May 19, 2011Applicant: SANOFI-AVENTISInventors: Marco BARONI, Letizia PULEO
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Publication number: 20110118246Abstract: The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: May 19, 2011Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 7943605Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.Type: GrantFiled: October 25, 2006Date of Patent: May 17, 2011Assignee: UCB Pharma S.A.Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
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Publication number: 20110105454Abstract: The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.Type: ApplicationFiled: December 23, 2008Publication date: May 5, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Braje, Astrid Netz, Thorsten Oost, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Patent number: 7935704Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1?, R1?, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.Type: GrantFiled: February 4, 2005Date of Patent: May 3, 2011Assignee: Nereus Pharmaceuticals, Inc.Inventors: Michael A. Palladino, George Kenneth Lloyd, Yoshio Hayashi, Benjamin Nicholson
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Publication number: 20110098236Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Publication number: 20110098237Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan, Sergi Gulnik, John W. Erickson
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Patent number: 7932250Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].Type: GrantFiled: July 1, 2005Date of Patent: April 26, 2011Assignee: Daiichi Sankyo Company, LimitedInventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Publication number: 20110092516Abstract: The present invention relates to novel 5-halogen-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: ApplicationFiled: December 5, 2008Publication date: April 21, 2011Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20110082129Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.Type: ApplicationFiled: June 25, 2009Publication date: April 7, 2011Inventors: Christopher Adams, Qi-Ying Hu, Leslie Wighton McQuire, Julien Papillon
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Patent number: 7919489Abstract: The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: August 20, 2007Date of Patent: April 5, 2011Assignee: Aicuris GmbH & Co. KGInventors: Holger Zimmermann, David Brueckner, Kerstin Henninger, Ulrich Rosentreter, Martin Hendrix, Joerg Keldenich, Dieter Lang, Martin Radtke, Daniela Paulsen, Armin Kern
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Publication number: 20110076230Abstract: The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted indole derivatives, compositions, and therapeutic uses and processes for making such compounds.Type: ApplicationFiled: May 28, 2009Publication date: March 31, 2011Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Scott Wolkenberg
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Publication number: 20110077241Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: ApplicationFiled: July 20, 2010Publication date: March 31, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste, Andrea Hager-Wernet
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Publication number: 20110077253Abstract: The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: ApplicationFiled: December 5, 2008Publication date: March 31, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Astrid Netz, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh