Chalcogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 546/277.7)
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Publication number: 20120015966Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
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Publication number: 20110263565Abstract: The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: July 28, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Treu, Thomas Karner, Ulrich Reiser
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Publication number: 20110263614Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: March 14, 2011Publication date: October 27, 2011Inventors: Roger Bonnert, Rukhsana Mohammed, Mark Robert Dickinson
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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: 20110243844Abstract: Disclosed are mGluR4 positive allosteric modulator ligands of general formula (I) and radiolabeled derivates, their use as therapeutic agents for the treatment of central nervous system disorders modulated by mGluR4 and as ligands for the labeling and diagnostic imaging of mGluR4 in mammals.Type: ApplicationFiled: August 24, 2009Publication date: October 6, 2011Inventor: John A. McCauley
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Publication number: 20110230524Abstract: The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.Type: ApplicationFiled: November 27, 2009Publication date: September 22, 2011Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Pavel Mikhailovich Yamanushkin, Oleg Dmitrievich Mitkin, Vladimir Yurievich Vvedensky, Vadim Vasilievich Bichko
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Publication number: 20110224210Abstract: The invention relates to novel bis-amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.Type: ApplicationFiled: November 18, 2009Publication date: September 15, 2011Inventors: Hamed Aissaoui, Christoph Boss, Olivier Corminboeuf, Marie-Celine Frantz, Corinna Grisostomi
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Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
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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: 20110118241Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: ApplicationFiled: May 5, 2009Publication date: May 19, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110112067Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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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: 20110071195Abstract: The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.Type: ApplicationFiled: September 14, 2010Publication date: March 24, 2011Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajung Nan, Tao Pang, Lifang Yu, Mei Zhang
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Publication number: 20110034514Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: ApplicationFiled: October 18, 2010Publication date: February 10, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe
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Publication number: 20110009379Abstract: [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. [Means for Solution] The present inventors have extensively studied compounds having TRPA1 channel activation activity, and confirmed that an indolinone compound has a TRPA1 channel activation activity, and thus completed the present invention. The indolinone compound of the present invention has a TRPA1 channel activation activity and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder or the like.Type: ApplicationFiled: March 30, 2009Publication date: January 13, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hidetaka Kaku, Tomofumi Takuwa, Michihito Kageyama, Katsura Nozawa, Hitoshi Doihara
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Patent number: 7868008Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: February 15, 2006Date of Patent: January 11, 2011Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20110003810Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: March 29, 2010Publication date: January 6, 2011Applicant: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Wilfried Hornberger, Falko Ernst Wolter
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Publication number: 20100317663Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, Q, Z, r, and p are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with FAK overexpression, including proliferative diseases.Type: ApplicationFiled: February 19, 2009Publication date: December 16, 2010Inventors: Jerry Leroy Adams, Thomas H. Faitg, Neil W. Johnson, Xin Peng
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Publication number: 20100311715Abstract: This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.Type: ApplicationFiled: August 19, 2010Publication date: December 9, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, R. Scott Rowland, Dilrukshi Vitharana
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Publication number: 20100305100Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: July 1, 2010Publication date: December 2, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary Mitchell Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100305326Abstract: Disclosed herein are methods related to drug development. The methods typically include steps whereby two chemical fragments are identified as binding to a target protein and subsequently the two chemical fragments are joined to create a new chemical entity that binds to the target protein.Type: ApplicationFiled: June 2, 2010Publication date: December 2, 2010Applicant: Marquette UniversityInventor: Daniel S. Sem
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Publication number: 20100298343Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: ApplicationFiled: September 12, 2008Publication date: November 25, 2010Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda, Nicholas Simon Stock, Jeffrey Roger Roppe, Bowei Wang
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Patent number: 7834037Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: GrantFiled: October 27, 2007Date of Patent: November 16, 2010Assignee: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100273766Abstract: The invention relates to novel oxindole derivatives 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: ApplicationFiled: December 1, 2006Publication date: October 28, 2010Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Patent number: 7812036Abstract: The compounds of the subject invention have a structure according to formula I: wherein each of the substituents is given the definition as set forth in the specification and claims, or a salt or hydrate form thereof.Type: GrantFiled: April 21, 2005Date of Patent: October 12, 2010Assignee: N.V. OrganonInventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
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Patent number: 7795280Abstract: This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.Type: GrantFiled: November 3, 2003Date of Patent: September 14, 2010Assignee: N.V. OrganonInventors: Pedro Harold Han Hermkens, Herman Thijs Stock, Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse
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Publication number: 20100227863Abstract: The present application discloses substituted 3-(4-hydroxyphenyl)-indolin-2-one compounds (oxindole compounds) of the formula and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal, in particular in humans.Type: ApplicationFiled: April 28, 2008Publication date: September 9, 2010Applicant: TOPOTARGET A/SInventors: Mette Knak Christensen, Fredrik Bjoerkling
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Patent number: 7781591Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.Type: GrantFiled: June 13, 2007Date of Patent: August 24, 2010Assignee: Wyeth LLCInventors: Derek Cecil Cole, Diane Harris Boschelli, Yanong Daniel Wang, Magda Asselin, Diane Marie Joseph-McCarthy, Amarnauth Shastrie Prashad, Allan Wissner, Russell Dushin, Biqi Wu, Lawrence Nathan Tumey, Chuan S. Niu, Joan Chen
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Publication number: 20100179122Abstract: Compounds of Formula (I): are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Craig W. Lindsley, William H. Leister, Scott E. Wolkenberg
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Publication number: 20100168182Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly TrkA, TrkB, TrkC, PDGFR and c-kit.Type: ApplicationFiled: December 11, 2007Publication date: July 1, 2010Applicant: IRM LLCInventors: Yuan Mi, Pamela Albaugh, Yi Fan, Ha-Soon Choi, Zuosheng Liu, Shenlin Huang
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Publication number: 20100168101Abstract: The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.Type: ApplicationFiled: December 23, 2009Publication date: July 1, 2010Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Agnes BOMBRUN, Patrick Gerber, Dennis Church
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Publication number: 20100160318Abstract: 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.Type: ApplicationFiled: December 3, 2007Publication date: June 24, 2010Applicant: JIANGSU SIMCERE PHARMACEUTICAL R&D CO., LTD.Inventors: Feng Tang, Han Shen, Qiu Jin, Lei Ding, Jie Yang, Xiaojin Yin, Shiyue Lu
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Patent number: 7700641Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: GrantFiled: April 11, 2006Date of Patent: April 20, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Patent number: 7683067Abstract: Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.Type: GrantFiled: September 21, 2004Date of Patent: March 23, 2010Assignee: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg
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Publication number: 20100069384Abstract: The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V2 receptors of vasopressin (“V2 receptors”) and can therefore constitute active principles of pharmaceutical compositions.Type: ApplicationFiled: June 12, 2009Publication date: March 18, 2010Applicant: SANOFI-AVENTISInventors: Loic FOULON, Pierrick ROCHARD, Claudine SERRADEIL-LE GAL, Gerard VALETTE
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Patent number: 7678800Abstract: The present invention relates to 2-(1H-indolylsulfanyl)-aryl amine derivatives of the general formula I as the free base or salts thereof and their use for the treatment of affective disorders, pain, attention deficit hyperactivity disorder (ADHD) and stress urinary incontinence.Type: GrantFiled: July 13, 2005Date of Patent: March 16, 2010Assignee: H. Lundbeck A/SInventors: Jan Kehler, Friedrich Kroll, Karsten Juhl
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Publication number: 20100004179Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.Type: ApplicationFiled: June 29, 2009Publication date: January 7, 2010Inventors: Jeffrey A. Toretsky, Aykut Uren, Milton Lang Brown, Yali Kong
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Publication number: 20090318406Abstract: The present invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, A, B and Y are as defined in claim 1, medicinal products containing them and use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.Type: ApplicationFiled: August 24, 2007Publication date: December 24, 2009Applicant: ABBOTT GMBH & CO. KGInventors: Herve Geneste, Thorsten Oost, Astrid Netz, Charles W. Hutchins, Wolfgang Wernet, Wolfgang Lubisch, Liliane Unger, Wilfried Hornberger
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Publication number: 20090306144Abstract: New 3,3-disubstituted indol-2-one derivatives of the general formula (I) Compounds according to the invention are useful for the prophylaxis or treatment of the disorders of the central nervous system.Type: ApplicationFiled: July 28, 2009Publication date: December 10, 2009Inventors: Balazs VOLK, József Barkóczy, Gyula Simig, Tibor Mezei, Rita Kapillerné Dezsòfi, István Gacsályi, Katalin Pallagi, Gábor Gigler, György Lévay, Krisztina Móricz, Csilla Leveleki, Nóra Sziray, Gabor Szénási, András Egyed, Lászió Gábor Hársing
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Publication number: 20090298886Abstract: The present invention relates to 2-indolinone derivatives which are capable of inhibiting protein kinases and histone deacetylases. The compounds of this invention are therefore useful in treating diseases associated with abnormal protein kinase activities or abnormal histone deacetylase activities. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing these compounds are also disclosed.Type: ApplicationFiled: May 8, 2009Publication date: December 3, 2009Applicant: Chipscreen Biosciences, Ltd.Inventors: Xian-Ping LU, Zhi-Bin LI, Zhi-Qiang Ning
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Publication number: 20090291982Abstract: The present invention relates to a new compound of formula (I) 6-(5-cyano-2-hydroxy-1H-indol-3-yl)pyridine-3-carboxylic acid or a pharmaceutically acceptable salt thereof, in an essentially pure and isolated form, pharmaceutical formulations containing said compounds, to the use of said active compounds in therapy, and methods of prevention and/or treatment of conditions associated with glycogen synthase kinase-3 related disorders, comprising administering to a mammal, including human in need of such prevention and/or treatment, a therapeutically effective amount of said compound, as well as a process for preparing said compound.Type: ApplicationFiled: May 22, 2008Publication date: November 26, 2009Applicant: AstraZeneca ABInventors: Martina Claesson, Suzanne IVERSON HEMBERG, Fredrik Lake
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Patent number: 7560480Abstract: The present invention relates to alkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).Type: GrantFiled: March 10, 2005Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Gerald Juergen Roth, Joerg Kley, Stefan Hoerer, Ingo Uphues
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Publication number: 20090176840Abstract: This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 17, 2008Publication date: July 9, 2009Inventors: Michael Konkel, John M. Werzel, Jamie Talisman
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Publication number: 20090163518Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: March 4, 2009Publication date: June 25, 2009Inventors: Roger Bonnert, Rukhsana Rasul
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Publication number: 20090149460Abstract: The present invention provides new compounds of formula Ia and Ib: as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: ApplicationFiled: June 17, 2008Publication date: June 11, 2009Inventors: Stefan Berg, Sven Hellberg, Martin Nylof, Yafeng Xue
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Publication number: 20090069376Abstract: Substituted N—[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.Type: ApplicationFiled: April 17, 2006Publication date: March 12, 2009Inventors: Ping Liu, Carrie Jones, Thomas S. Reger
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Patent number: 7488743Abstract: The disclosure concerns indolin-2-one pyridine compounds of general formula (I): wherein R0, R1, R2, R3, R4, Z and B have the meanings given in the description, and pharmaceutically acceptable salts thereof; and also pharmaceutical compositions comprising, processes for making and methods of using said compounds.Type: GrantFiled: March 16, 2007Date of Patent: February 10, 2009Assignee: Sanofi-AventisInventors: Loïc Foulon, Claudine Serradeil-Le Gal, Gérard Valette
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Publication number: 20090018170Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: ApplicationFiled: October 27, 2007Publication date: January 15, 2009Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Nicholas Simon STOCK, Jeffrey Roger ROPPE
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Publication number: 20080275041Abstract: Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.Type: ApplicationFiled: September 21, 2004Publication date: November 6, 2008Applicant: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg