Three Or More Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 546/64)
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Patent number: 8293762Abstract: Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions including them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.Type: GrantFiled: February 18, 2008Date of Patent: October 23, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Ermes Vanotti, Maria Menichincheri, Alessandra Scolaro
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Publication number: 20120095006Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.Type: ApplicationFiled: December 16, 2011Publication date: April 19, 2012Inventors: Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
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Patent number: 8158647Abstract: Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.Type: GrantFiled: May 29, 2008Date of Patent: April 17, 2012Assignee: SGX Pharmaceuticals, Inc.Inventors: Jeffrey M. Blaney, Andreas Gosberg, Stefan N. Gradl, Gavin Hirst, Stephanie A. Hopkins, Paul A. Sprengeler, Ruo W. Steensma, Johnny Uy
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Patent number: 8148392Abstract: 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula (I) and methods of using same in the treatment of cancer, in particular, solid cancers and leukemia are provided. Pharmaceutical compositions comprising the compounds are also provided.Type: GrantFiled: May 25, 2006Date of Patent: April 3, 2012Assignee: Lorus Therapeutics Inc.Inventors: Mario Huesca, Aiping H. Young, Yoon Lee, Aye Aye Khine, Jim A. Wright, Lisa Lock, Raed Al-Qawasmeh
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Publication number: 20120074389Abstract: Disclosed are a metal complex compound represented by the following Chemical Formula 1 or 3, and an organic light emitting diode device including the same. In Chemical Formulae 1 and 3, M1, M2, R1 to R14, y1 and y2 are as defined in the detailed description.Type: ApplicationFiled: July 12, 2011Publication date: March 29, 2012Applicant: Samsung Mobile Display Co., Ltd.Inventors: Yuji HAMADA, Kwan-Hee LEE
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Publication number: 20120058940Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: March 8, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG
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Publication number: 20120025697Abstract: A substance that facilitates hole injection and has high triplet excitation energy is provided. A light-emitting element having high emission efficiency is provided. A light-emitting element driven with a low voltage is provided. Or a light-emitting element having a long lifetime is provided. Provided is a light-emitting element including a triazolo[4,3-f]phenanthridine derivative or a triazolo[3,4-a]isoquinoline derivative. Provided is a triazolo[4,3-f]phenanthridine and triazolo[3,4-a]isoquinoline derivatives, which are novel and can be used for the light-emitting element.Type: ApplicationFiled: July 29, 2011Publication date: February 2, 2012Inventors: Hiroshi KADOMA, Yuko KAWATA, Nobuharu OHSAWA, Satoshi SEO
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Patent number: 8093390Abstract: Fused [1,2]imidazo[4,5-c] ring compounds, e.g., fused [1,2]imidazo[4,5-c]quinolines and [1,2]imidazo[4,5-c]naphthyridines, with a substituent, e.g., a substituted alkoxy substituent, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: February 10, 2006Date of Patent: January 10, 2012Assignee: 3M Innovative Properties CompanyInventors: Michael J. Rice, Bryon A. Merrill, Philip D. Heppner
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Patent number: 8088788Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: March 14, 2007Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Scott E. Langer, Philip D. Heppner
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Patent number: 8034938Abstract: Substituted fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—R1)— group in the fused ring at the 1-position of the imidazo ring, wherein R1 includes a functional group, for example, an amide, sulfonamide, urea, carbamate, ester, ketone, ether, a thio analog of the forgoing, sulfone, oxime, or hydroxylamine, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: December 29, 2005Date of Patent: October 11, 2011Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Tushar A. Kshirsagar, Sarah J. Slania, Michael E. Danielson
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Publication number: 20110245272Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: September 23, 2010Publication date: October 6, 2011Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20110218184Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: March 9, 2011Publication date: September 8, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Johnny Yasuo NAGASAWA, Fabrice Pierre, Mustapha Haddach, Michael Schwaebe, Levan Darjania, Jeffrey P. Whitten
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Patent number: 7994187Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-6alkyl, polyhaloC1-6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimidType: GrantFiled: April 3, 2007Date of Patent: August 9, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Bart Rudolf Romanie Kesteleyn, Wim Bert Griet Schepens
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Patent number: 7989089Abstract: The invention provides organic compounds of the general structure (1) that are photoluminescent and electroluminescent, emitting intense blue light. The invention further provides methods of synthesizing such compounds, methods of producing photoluminescence and electroluminescence, methods of applying the compounds in thin films, and uses of the compounds of the invention in luminescent probes, electroluminescent displays and as pH probes and metal ion detectors.Type: GrantFiled: April 16, 2004Date of Patent: August 2, 2011Assignee: LG Display Co., Ltd.Inventors: Suning Wang, Ruiyao Wang
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Publication number: 20110136800Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: November 5, 2010Publication date: June 9, 2011Inventors: Matthias Eckhardt, Stefan Peters, Herbert Nar, Frank Himmelsbach, Linghang Zhuang
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Publication number: 20110112299Abstract: Provided are a tetracyclic compound represented by the formula (I): [in the formula (I), the formula (A) represents a benzene ring or the like, X represents CH or a nitrogen atom, Q represents —O— or the like, R1, R2, and R3 may be the same or different and each represent a hydrogen atom or the like, l, m, and n each represent an integer from one to the maximum substitutable number of substituents, and R4 and R5 may be the same or different and each represent a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: July 3, 2009Publication date: May 12, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junichiro Yamamoto, Kiyotoshi Mori, Tomohiro Era, Yoshisuke Nakasato, Kenji Uchida
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110104109Abstract: The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Frank Bennett, Qingbei Zeng, Srikanth Venkatraman, Mousumi Sannigrahi, Kevin X. Chen, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20110077404Abstract: The invention relates to a novel process for the preparation of pharmacologically interesting indolopyridine derivatives containing tetracyclic tetrahydro-?-carboline-hydantoines linked to a basic side chain and the corresponding salts, which can be used as Eg5 inhibitor, with very high overall chemical yield and enantiomeric purity.Type: ApplicationFiled: March 5, 2009Publication date: March 31, 2011Applicant: 4SC AGInventors: Bernd Muller, Helmut Schlemper
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Patent number: 7914908Abstract: Azatriphenylene derivatives and their use in the electron-transporting layer of an electroluminescent device that comprises an anode, a spaced-apart cathode, and at least one electron-transporting layer disposed between the spaced-apart anode and cathode. Such EL devices provide lower drive voltage, improved power efficiency, and longer operational lifetime.Type: GrantFiled: November 2, 2007Date of Patent: March 29, 2011Assignee: Global OLED Technology LLCInventors: Shiying Zheng, Liang-Sheng Liao
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Patent number: 7910087Abstract: Novel luciferins, methods of making luciferins, and uses of the same are disclosed.Type: GrantFiled: February 29, 2008Date of Patent: March 22, 2011Assignee: University of MassachusettsInventor: Stephen C. Miller
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Publication number: 20110027226Abstract: Compounds of a certain formula I, in which R1, R2, R3 and R4 have the meanings indicated in the description, are effective Eg5-inhibiting compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: August 22, 2007Publication date: February 3, 2011Applicant: 4SC AGInventors: Matthias Vennemann, Juergen Braugner, Petra Gimmnich, Thomas Baer
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Patent number: 7875624Abstract: Methods of using compounds having Structure I or the salts or tautomers of the compounds in the treatment of disorders relating to cell adhesion and metastatic processes are presented herein.Type: GrantFiled: February 18, 2005Date of Patent: January 25, 2011Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Carla Heise, Sang H. Lee
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Publication number: 20110003843Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen orType: ApplicationFiled: February 19, 2008Publication date: January 6, 2011Inventors: Fabrice Lejeune, Jamal Tazi, David Grierson, Christian Rivalle, Florence Mahuteau-Betzer
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Publication number: 20110003738Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: January 6, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG
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Patent number: 7834180Abstract: Compounds having formula 1: are produced by contacting a compound having formula (6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base, wherein V, A, Z, L, L1, W, X, B?, R and n are as defined herein.Type: GrantFiled: November 19, 2008Date of Patent: November 16, 2010Assignee: Cylene Pharmaceuticals, Inc.Inventors: Peter C. Chua, Johnny Y. Nagasawa, Michael Schwaebe, Fabrice Pierre
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Patent number: 7816524Abstract: Compounds having formula 1 are produced by contacting a compound having formula(6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base, wherein V, A, Z, L, L1,W, X, B?, R and N are as defined herein.Type: GrantFiled: August 4, 2006Date of Patent: October 19, 2010Assignee: Cylene Pharmaceuticals, Inc.Inventors: Peter C. Chua, Johnny Y. Nagasawa, Michael Schwaebe, Fabrice Pierre
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Publication number: 20100255005Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: May 28, 2008Publication date: October 7, 2010Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
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Publication number: 20100239526Abstract: The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark Ashwell, Chris Brassard, Audra Dalton, Anton Filikov, Jason Hill, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Jianqiang Wang, Neil Westlund
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Publication number: 20100204239Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.Type: ApplicationFiled: February 2, 2010Publication date: August 12, 2010Inventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
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Patent number: 7763634Abstract: The instant invention provides for tetracyclic compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: GrantFiled: June 5, 2007Date of Patent: July 27, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Jonathan R. Young, Andrew Haidle, Paul Tempest, Michelle Machacek
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Publication number: 20100168417Abstract: 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula I that are capable of intracellular chelation of transition metals and of exerting antiproliferative effects in cancer cells, that are cytostatic and/or cytotoxic, are provided. Compounds of Formula I can also induce apoptosis in cancer cells and are thus capable of exerting a cytotoxic effect on cancer cells. The compounds of Formula I are also capable of selectively inhibiting the proliferation of one or more of prostate cancer cells, colon cancer cells, non-small lung cancer cells and leukemia cells. The compounds of Formula I are also capable of increasing the expression of the zinc-regulated tumour suppressor, KLF4 and thus are useful in inhibiting the proliferation of cancer cells in which KLF4 functions as a tumour-suppressor, including, but not limited to, bladder cancer, cancers of the gastrointestinal tract and various leukemias.Type: ApplicationFiled: May 25, 2006Publication date: July 1, 2010Inventors: Mario Huesca, Aiping H. Young, Yoon Lee, Aye Aye Khine, Jim A. Wright, Lisa Lock, Raed Al-Qawasmeh
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Patent number: 7718665Abstract: Compounds of the formula (1) in which R1, R2, R3, R4 and X have the meanings indicated in the description, are novel effective compounds with Eg5 inhibitory, anti-proliferative and/or apoptosis inducing activity.Type: GrantFiled: August 17, 2005Date of Patent: May 18, 2010Assignee: 4SC AGInventors: Matthias Vennemann, Thomas Baer, Gudrun Groegor, Jürgen Braunger, Petra Gimmnich, Thomas Maier, Heike Rothfels
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Publication number: 20100113415Abstract: The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.Type: ApplicationFiled: May 28, 2009Publication date: May 6, 2010Inventors: Hemaka A. Rajapakse, Keith P. Moore, Philippe G. Nantermet, John M. Sanders, Sophie Parmentier-Batteur, Robert J. Mark
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Publication number: 20100098634Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.Type: ApplicationFiled: July 24, 2009Publication date: April 22, 2010Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
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Patent number: 7696239Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.Type: GrantFiled: January 3, 2008Date of Patent: April 13, 2010Assignee: Janssen Pharmaceutica NVInventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
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Publication number: 20100069360Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1, R2, R3, R7 and X are as defined in the specification.Type: ApplicationFiled: August 28, 2007Publication date: March 18, 2010Inventors: Laszlo Revesz, Achim Schlapbach, Rudolf Walchli
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Publication number: 20100056556Abstract: Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions comprising them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.Type: ApplicationFiled: February 18, 2008Publication date: March 4, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Ermes Vanotti, Maria Menichincheri, Alessandro Scolaro
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Publication number: 20090306071Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 5, 2007Publication date: December 10, 2009Inventors: Jonathan R. Young, Andrew Haidle, Paul Tempest, Michelle Machacek
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Patent number: 7615638Abstract: In one embodiment of the present invention, a synthesis of grossularine-1 and N,N-didesmethylgrossularine-1 2 and analogs thereof based on a novel oxidative dimerization-electrocyclization sequence of 2-amino-4-(3-indolyl)imidazoles derived from oxotryptamine 3 is described.Type: GrantFiled: April 30, 2007Date of Patent: November 10, 2009Assignee: City of HopeInventors: David A. Horne, Richard Jove, Sangkil Nam, Kenichi Yakushijin, Fumiko Y. Yakushijin
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Publication number: 20090246169Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: February 21, 2007Publication date: October 1, 2009Inventors: Matthias Vennemann, Thomas Bar, Jürgen Braunger, Astrid Zimmermann, Volker Gekeler
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Publication number: 20090233902Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: February 21, 2007Publication date: September 17, 2009Inventors: Matthias Vennemann, Thomas Bãr, Jürgen Braunger, Astrid Zimmermann, Volker Gekeler
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Publication number: 20090221551Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: March 14, 2007Publication date: September 3, 2009Inventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Philip D. Heppner
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Publication number: 20090215766Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: ApplicationFiled: August 6, 2008Publication date: August 27, 2009Inventors: James D. Rodgers, Darius J. Robinson, Argyrios G. Arvanitis, Thomas P. Maduskuie, JR., Stacey Shepard, Louis Storace, Haisheng Wang, Maria Rafalski, Ravi Kumar Jalluri, Andrew P. Combs, Matthew L. Crawley
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Publication number: 20090209571Abstract: The invention encompasses novel compounds of Formula or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.Type: ApplicationFiled: May 15, 2007Publication date: August 20, 2009Inventors: Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Andre Giroux, Evelyn Martins, Pierre Hamel
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Publication number: 20090182001Abstract: The instant invention provides for compounds which comprise fused imidazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: July 18, 2006Publication date: July 16, 2009Inventors: Mark E. Fraley, Justin T. Steen
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Publication number: 20090170855Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-C6alkyl, polyhaloC1-C6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pType: ApplicationFiled: April 3, 2007Publication date: July 2, 2009Inventors: Bart Rudolf Romanie Kesteleyn, Wim Bert Griet Schepens
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Patent number: 7550477Abstract: The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: December 29, 2006Date of Patent: June 23, 2009Assignee: Merck & Co., Inc.Inventors: Edward J. Brnardic, Mark E. Fraley
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Publication number: 20090115316Abstract: Azatriphenylene derivatives and their use in the electron-transporting layer of an electroluminescent device that comprises an anode, a spaced-apart cathode, and at least one electron-transporting layer disposed between the spaced-apart anode and cathode. Such EL devices provide lower drive voltage, improved power efficiency, and longer operational lifetime.Type: ApplicationFiled: November 2, 2007Publication date: May 7, 2009Inventors: Shiying Zheng, Liang-Sheng Liao
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Publication number: 20090098218Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.Type: ApplicationFiled: July 16, 2008Publication date: April 16, 2009Inventors: Achim Schlapbach, Laszlo Revesz, Guido Koch