Nitrogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding (e.g., 2-amino Indoles, Etc.) Patents (Class 548/483)
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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: 20100167927Abstract: The invention relates to substituted amino-thiourea compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amino-thiourea compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds. The substituted amino-thiourea compounds are defined by the following formula (I): wherein A, B, R1, R2, R3, R4, R5.1, R5.2 and R6 are defined as in the description.Type: ApplicationFiled: May 13, 2008Publication date: July 1, 2010Applicant: BASF SEInventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Patent number: 7705023Abstract: There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: GrantFiled: June 17, 2005Date of Patent: April 27, 2010Assignee: Biolipox ABInventors: Kristofer Olofsson, Benjamin Pelcman, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Patent number: 7696231Abstract: 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.(I).Type: GrantFiled: October 24, 2002Date of Patent: April 13, 2010Assignee: Laboratoires Serono SAInventors: Agnes Bombrun, Patrick Gerber, Denis Church
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Patent number: 7691895Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.Type: GrantFiled: November 8, 2007Date of Patent: April 6, 2010Assignee: Ligand Pharmaceuticals, Inc.Inventors: Jyun-Hung Chen, E. Adam Kallel, Thomas Lau, Matthew H. McNeill, Todd A. Miller, Bao N. Nguyen, Richard J. Penulian, Dean P. Phillips, Daniel A. Ruppar, Lin Zhi, Jackline E. Dalgard
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Publication number: 20100063301Abstract: Disclosed herein are various methods for synthesizing compounds that modulate thrombopoietin activity. Also disclosed are intermediates useful for the preparation of these compounds.Type: ApplicationFiled: March 14, 2007Publication date: March 11, 2010Applicant: LIGAND PHARMACEUTICALS INCInventor: Dean Phillips
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Patent number: 7666897Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds has the structure of formula (IV) wherein: R1, R2, R3, R4, R5, R6, R7, R8, R5A, R6A, R7A, R8A, R22 and R23 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.Type: GrantFiled: September 5, 2008Date of Patent: February 23, 2010Assignee: SRI InternationalInventors: Ling Jong, Wan-Ru Chao
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Publication number: 20100041628Abstract: Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKK? and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKK?. In the formula, R1 represents a hydrogen atom, a lower alkyl group, an aryl group, a hydroxy group, or the like; R2 represents a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or the like; and m represents 0, 1, 2, or the like.Type: ApplicationFiled: January 15, 2008Publication date: February 18, 2010Inventors: Hiroshi Enomoto, Kenji Kawashima, Kazuhiro Kudou, Minoru Yamamoto, Masaaki Murai, Takaaki Inaba, Noriko Ishizaka
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Patent number: 7662824Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: March 16, 2006Date of Patent: February 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Kristi Leonard, Tianbao Lu, Robert W. Tuman, Dana L. Johnson, Anna C. Maroney, Jan L. Sechler, Richard W. Connors, Richard S. Alexander, Maxwell D. Cummings, Robert A. Galemmo, Thomas P. Markotan
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Publication number: 20100004295Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl or the like, R2 and R8 are each independently hydrogen or lower alkyl, X is optionally substituted lower alkylene or the like, Y is —OCONR7— or the like, R7 is hydrogen, lower alkyl or the like, Z is optionally substituted carbocyclyl or the like, W is optionally substituted alkylene or the like.Type: ApplicationFiled: August 28, 2007Publication date: January 7, 2010Inventor: Naoki Kouyama
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Patent number: 7642281Abstract: This invention provides a method of treating a subject suffering from a cognitive impairment or a cognitive disorder which comprises administering to the subject an amount of an indolone compound effective to treat the subject's cognitive impairment or disorder.Type: GrantFiled: December 8, 2006Date of Patent: January 5, 2010Assignee: Helicon Therapeutics, Inc.Inventor: Thomas P. Blackburn
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Patent number: 7612065Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: March 28, 2007Date of Patent: November 3, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Susanne Wilke, Francesco Salituro, Edmund Harrington, Jingrong Cao, Guy Bemis, Huai Gao
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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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Patent number: 7479357Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.Type: GrantFiled: September 13, 2002Date of Patent: January 20, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait, Anatoliy V. Vakulenko
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Patent number: 7465750Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 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. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.Type: GrantFiled: September 6, 2006Date of Patent: December 16, 2008Assignee: H. Lundbeck A/SInventors: Thomas P. Blackburn, Michael J. Konkel, Lakmal W. Boteju, Ian Jamie Talisman, John M. Wetzel, Mathivanan Packiarajan, Heidi Chen, Hermo Jimenez
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Publication number: 20080242655Abstract: The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: November 29, 2007Publication date: October 2, 2008Inventors: Simon Charles Goodacre, Karen Williams, Stephen Price, Hazel Joan Dyke, John Gary Montana, Mark S. Stanley, Liang Bao, Wendy Lee
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Patent number: 7429610Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (III) wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, R20, and R21 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.Type: GrantFiled: February 7, 2006Date of Patent: September 30, 2008Assignee: SRI InternationalInventors: Ling Jong, Wan-Ru Chao
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Publication number: 20080206180Abstract: A hair and/or scalp treatment composition comprising an amino-oxo-indole-ylidene compound of general formula (I): (I) formula should be here in which: R1, R2, R3 and R4 are each, independently, hydrogen or a monovalent organic group selected from alkyl, alkenyl, alkynyl, aryl, alkylenearyl, cycloalkyl, cycloalkenyl, and heterocyclyl.Type: ApplicationFiled: February 27, 2006Publication date: August 28, 2008Inventors: Ranjit Bhogal, Jasveen Chugh, Helen Meldrum
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Publication number: 20080188473Abstract: There is provided a compound of formula: (I) wherein X, R1, R2, R3, R4, R5, R6, R7 and R8 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: June 17, 2005Publication date: August 7, 2008Inventors: Kristofer Olofsson, Benjamin Pelcman, Wesley Schaal, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Patent number: 7405300Abstract: The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: GrantFiled: September 1, 2004Date of Patent: July 29, 2008Assignee: Aventis Pharmaveuticals Inc.Inventors: John Z. Jiang, Jack Roger Koehl, Shujaath Mehdi, Neil David Moorcroft, Kwon Yon Musick, Philip Marvin Weintraub, Paul Robert Eastwood
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Publication number: 20080146594Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.Type: ApplicationFiled: November 8, 2007Publication date: June 19, 2008Applicant: Ligand Pharmaceutical, Inc.Inventors: Jyun-Hung Chen, E. Adam Kallel, Thomas Lau, Matthew H. McNeill, Todd A. Miller, Bao N. Nguyen, Richard J. Penuliar, Dean P. Phillips, Daniel A. Ruppar, Lin Zhi, Jackline E. Dalgard
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Publication number: 20080119648Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Patent number: 7368605Abstract: Formula (I) compounds are described where the groups are as identified in the text, and their use as medicines, particularly as anti-diabetes, serum glucose-lowering and anti-obesity agents. They are useful for the prophylaxis and treatment of diabetes, particularly type 2 diabetes, and its complications, syndrome X, the various forms of insulin resistance, and hyperlipidaemias, as well as for the treatment of obesity.Type: GrantFiled: December 1, 2003Date of Patent: May 6, 2008Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Emanuela Tassoni, Maria Ornella Tinti, Pompeo Pessotto, Maurizio Botta, Pederico Corelli
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Patent number: 7342038Abstract: The present invention provides substituted 3,3-diphenyl indole compounds, as well as analogues thereof, which are specific potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.Type: GrantFiled: June 1, 2004Date of Patent: March 11, 2008Assignees: President and Fellow of Harvard College, Children's Medical Center Corporation, NuChem Pharmaceuticals Inc.Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Patent number: 7338966Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: June 9, 2005Date of Patent: March 4, 2008Assignee: SmithKline Beecham CorporationInventors: Karen Elizabeth Lackey, Edgar Raymond Wood, III
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Patent number: 7314887Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.Type: GrantFiled: October 21, 2005Date of Patent: January 1, 2008Assignee: Ligand Pharmaceuticals, Inc.Inventors: Jyun-Hung Chen, E. Adam Kallel, Thomas Lau, Matthew H. McNeill, Todd A. Miller, Bao N. Nguyen, Richard J. Penuliar, Dean P. Phillips, Daniel A. Ruppar, Lin Zhi, Jackline E. Dalgard
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Patent number: 7265130Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: December 30, 2003Date of Patent: September 4, 2007Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Patent number: 7241799Abstract: Cannabimimetic indole derivatives are presented which have preferentially high affinities for one of the cannabinoid CB1 or CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals.Type: GrantFiled: November 5, 2004Date of Patent: July 10, 2007Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Hongfeng Deng
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Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Patent number: 7166635Abstract: This invention is directed to indolone derivatives which are selective antagonists for 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. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.Type: GrantFiled: February 28, 2005Date of Patent: January 23, 2007Assignee: H. Lundbeck A/SInventors: Michael Konkel, John M. Wetzel, Jamie Talisman
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Patent number: 7153881Abstract: The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2)n, where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; R1 and R2 can be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereofType: GrantFiled: August 7, 2001Date of Patent: December 26, 2006Assignee: Acure Pharma ABInventors: Torbjörn Lundstedt, Anna Skottner, Arne Boman, Per Andersson, Victor Andrianov, Ivars Kalvins
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Patent number: 7141674Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: October 21, 2003Date of Patent: November 28, 2006Assignee: Johnson & Johnson Consumer Companies, Inc.Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 7112682Abstract: An improved process for the preparation of N-amino nitrogen heterocyclic compounds is disclosed and claimed. In an embodiment of this invention, a compound of the formula (VI) is prepared starting from the corresponding indole derivative by way of N-amination and subsequently forming an hydrazone by the reaction with a keto compound in a single step. Further reduction of the hydrazone and subsequent coupling with a pyridine compound affords the compound of formula VI or a suitable salt thereof.Type: GrantFiled: October 1, 2004Date of Patent: September 26, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Franz Weiberth, George Everett Lee, Reda G. Hanna, Juergen Mueller-Lehar, Silke Dubberke, Roland Utz
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Patent number: 7081470Abstract: This invention is directed to indolone derivatives which are antagonists for 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: GrantFiled: April 16, 2003Date of Patent: July 25, 2006Assignee: H. Lundbeck A/SInventors: Michael Konkel, John M. Werzel, Jamie Talisman
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Patent number: 7078427Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.Type: GrantFiled: February 3, 2004Date of Patent: July 18, 2006Assignee: SRI InternationalInventors: Ling Jong, Wan-Ru Chao
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Patent number: 7078429Abstract: Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.Type: GrantFiled: December 9, 2003Date of Patent: July 18, 2006Assignee: WyethInventor: Lee D. Jennings
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Patent number: 7071217Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio, Edgar Raymond Wood, III
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Patent number: 7030123Abstract: The invention provides a compound of Formula (I). Wherein R1, R2, R3, R10 and R11 have the meanings given in the description. Such compounds are predicted to cause the selective destruction of tumour vasculature. They may therefore be used to inhibit and/or reverse, and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis.Type: GrantFiled: May 25, 2001Date of Patent: April 18, 2006Assignee: AstraZeneca ABInventors: Jean-Claude Arnould, Thomas Geoffrey Bird, Francis Thomas Boyle, David Charles Blakey
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Patent number: 6969729Abstract: The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents.Type: GrantFiled: October 16, 2002Date of Patent: November 29, 2005Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Tino Dyhring Jørgensen, Philip K. Ahring, Palle Christophersen, Dorte Strøbaek, Lene Teuber, Søren Peter Olesen
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Patent number: 6958416Abstract: The invention relates to derivatives of valproyltaurinamide of formula (I) in which R1 and R2 are independently hydrogen, a C1-C6-alkyl group, an arylalkyl group or an aryl group. The derivatives are especially useful for the treatment of epilepsy, affective illness, cognitive disorders, neurodegenerative disease, neuropathic pain syndrome, migraine, stroke, brain ischemia, or head trauma injury.Type: GrantFiled: March 5, 2002Date of Patent: October 25, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Meir Bialer, Boris Yagen, Nina Isoherranen
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Patent number: 6900236Abstract: Novel cannabimimetic indole derivatives are presented which have preferential high affinities for one of the cannabinoid CB1 CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.Type: GrantFiled: October 18, 2000Date of Patent: May 31, 2005Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Hongfeng Deng
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Publication number: 20040242695Abstract: The invention relates to derivatives of valproyltaurinamide of formula (I) in which R1 and R2 are independently hydrogen, a C1-C6-alkyl group, an arylalkyl group or an aryl group. The derivatives are especially useful for the treatment of epilepsy, affective illness, cognitive disorders, neurodegenerative disease, neuropathic pain syndrome, migraine, stroke, brain ischemia, or head trauma injury.Type: ApplicationFiled: July 14, 2004Publication date: December 2, 2004Inventors: Meir Bialer, Boris Yagen, Nina Isoherranen
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Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors
Patent number: 6825352Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: August 30, 2002Date of Patent: November 30, 2004Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan -
Publication number: 20040220229Abstract: The invention provides compounds of formula (I) 1Type: ApplicationFiled: April 30, 2004Publication date: November 4, 2004Applicant: Pfizer IncInventors: Donald L. Bussolotti, Ronald B. Gammill
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Patent number: 6723848Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: in which X, R1, R2, R3, R4, R5 and n are as defined in claim 1, by reacting tetrahydrobenzo-fused heterocycles of formula II: in which X, R1, R2, R3, R4, R5, n and Ac are as defined in claim 1, with a catalytic amount of a noble metal catalyst in the presence of a hydrogen acceptor and then deacylating the acylated amino group by the addition of an amine.Type: GrantFiled: October 9, 2002Date of Patent: April 20, 2004Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030216356Abstract: The invention provides a compound of Formula (I) wherein: R1 and R2 are independently selected from hydrogen, halogen, —CN, a hydrocarbyl group or a group of Formula (II); wherein W is aryl or a heterocyclic group, R4 is independently select from hydrogen, halogen, —OH, amino, alkanoylamino, —OPO3H2, or a hydrocarbyl group, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified or two R4 groups together form an optionally substituted cyclic or heterocyclic group; X is selected from $M(y) S+—, +—O—+, —+S(O)+—, —+S(O2)+— and —+NH—; p is an integer from 0 to 4; and q is an integer from 1 to 4; R3 and R10 are independently selected from hydrogen, lower alkyl or a group of Formula (IV): wherein Y is selected from +NH+—, —$M(Y)O$M(Y)— or a bond; Z is selected from +NH+—, —+O&ngr;&mdashType: ApplicationFiled: November 13, 2002Publication date: November 20, 2003Inventors: Jean-Claude Arnould, Thomas Geoffrey Bird, Francis Thomas Boyle, David Charles Blakey
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Publication number: 20030195234Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhihit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: ApplicationFiled: February 27, 2003Publication date: October 16, 2003Inventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio
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Publication number: 20030153763Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: ApplicationFiled: December 17, 2002Publication date: August 14, 2003Inventors: N. Laxma Reddy, Michael Maillard, David Berlove, Sharad Magar, Graham J. Durant