Three Or More Hetero Atoms In The Tetracyclo Ring System Patents (Class 514/287)
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Publication number: 20110071179Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: September 17, 2010Publication date: March 24, 2011Inventors: Alam Jahangir, Stephen M. Lynch, Michael Soth, Hanbiao Yang
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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: 20110046161Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: ApplicationFiled: April 16, 2009Publication date: February 24, 2011Inventors: Nigel J. Liverton, John A. McCauley, John W. Butcher, Kevin F. Gilbert, Charles J. McIntyre, Michael T. Rudd
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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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Publication number: 20110028450Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 27, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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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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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: 20100227851Abstract: Provided are novel use of an extract of Lycoris chejuensis or a compound isolated therefrom for inhibition of ?-amyloid production and/or prevention, improvement and/or treatment of a neurodegenerative disease, more specifically a ?-amyloid production inhibitor, and/or a composition for prevention or treatment of a neurodegenerative disease containing one or more kinds selected from the group consisting of an extract of Lycoris chejuensis, and/or dihydrolycoricidine, 2-methoxypancracine, lycoricidine, and/or lycoricidinol, as an active ingredient; a method for inhibiting ?-amyloid production, and/or preventing and/or treating a neurodegenerative disease using the same; and, a method for preparing the same.Type: ApplicationFiled: October 28, 2009Publication date: September 9, 2010Applicant: Korea Institute of Science and TechnologyInventors: Hyun-Ok Yang, Hak-Cheol Kwon, Jin-Soo Park, Sung-Kwon Chung, Myung-Soo Kim
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Publication number: 20100210658Abstract: 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 17, 2010Publication date: August 19, 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: 20100183550Abstract: Compounds of a certain formula I, 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: ApplicationFiled: March 30, 2010Publication date: July 22, 2010Inventors: Matthias VENNEMANN, Thomas Baer, Gudrun Groegor
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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: 20100113494Abstract: The present invention provides 13,13a-dihydroberberine derivatives or their physiologically acceptable salts represented by the following formula, pharmaceutical compositions comprising the same, and uses thereof. The 13,13a-dihydroberberine derivatives have an activity of promoting glucose absorption in muscle cells, and the whole animal tests show that the present compounds have effects on improving glucose-tolerance and insulin-resistance, facilitating weight loss, relieving fatty liver and the like. Thus, the present compounds can be used in treating diabetes mellitus, adiposity, fatty liver and complications thereof induced by insulin resistance.Type: ApplicationFiled: September 30, 2007Publication date: May 6, 2010Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Lihong Hu, Jia Li, Jingya Li, Hankun Zhang, Zhe Cheng, Jiming Ye, David E. James, Edward W. Kraegen
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Publication number: 20100099698Abstract: The present invention relates to a composition for improving skin conditions comprising matrine and oxymatrine as an active ingredient. Matrine and oxymatrine have lower cytotoxicity than retinol used as anti-wrinkle agents and exhibit the inhibition effect on collagenase activity and promotion effect on collagen biosynthesis at a molecular level, contributing to excellent efficacy in improvement of skin wrinkles. In addition, both matrine and oxymatrine exhibit the inhibition effect on melanin production by inhibiting intracellular tyrosinase activity, the improving effects of UV-induced skin damage and the skin growth promotion or hair loss prevention. Therefore, matrine and oxymatrine have the excellent improvement effects on skin conditions. Furthermore, matrine and oxymatrine have the excellent anti-obesity and anti-oxidation effects. The composition of this invention can be applied to cosmetic, pharmaceutical and food composition having no cytotoxicities and side effects.Type: ApplicationFiled: February 21, 2008Publication date: April 22, 2010Applicant: Biospectrum Inc.Inventors: Deok Hoon Park, Eun Sun Jung, Jong Sung Lee
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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: 20100069380Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: March 18, 2010Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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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: 20100041617Abstract: The invention provides compositions and methods for inhibiting cell motility, metastatic cancer and viral infections in a mammal that involve increasing the activity or expression of MxA.Type: ApplicationFiled: September 27, 2005Publication date: February 18, 2010Inventors: Jane Trepel, Alexandra Lin, Sunmin Lee, Chand Khanna, Min-Jung Lee, Eun J. Chung, Ruilli Huang, David G. Covell
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Patent number: 7652029Abstract: Compositions and uses associated with the MT477 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT477 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT477 family and pharmaceuticals that contain such chemicals.Type: GrantFiled: July 11, 2005Date of Patent: January 26, 2010Assignee: Medisyn Technologies, Inc.Inventors: Javier Llompart, Jorge Galvez, Kollol Pal
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Publication number: 20090312330Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., X is halogen atom, C1-C6haloalkyl, etc., Y is halogen atm, C1-C6alkyl, etc., R1 is C1-C12alkyl arbitrarily substituted with R16, C3-C12alkenyl, arbitrarily substituted with R16 is oxygen atom or sulfur atom, —N(R20)R19, etc., R2 is hydrogen atom, C1-C4alkoxy C1-C6alkyl, etc., R3 is C1-C6haloalkyl, etc., R16 is halogen atom, cyano, phenyl substituted with (Z)p1, D-1 to D-60, E-1 to E-49, etc., R19 is phenyl, phenyl substituted with (Z)p1, etc., R20 is hydrogen atom, C1-C6alkyl, etc., Z is halogen atom, nitro, C1-C4alkoxy, etc., D-1 to D-60 are 5- or 6-membered aromatic heterocyclic rings, E-1 to E-49 are 5- or 6-membered saturated heterocyclic rings, m is an integer of 0 to 5, n is an integer of 0 to 4, p1 is an integer of 1 to 5. The pesticide containing these compounds.Type: ApplicationFiled: July 27, 2009Publication date: December 17, 2009Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi Mita, Takamasa Kikuchi, Takashi Mizukoshi, Manabu Yaosaka, Mitsuaki Komoda
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Patent number: 7632844Abstract: The compounds of formula I in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as indicated in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: December 17, 2007Date of Patent: December 15, 2009Assignee: Nycomed GmbHInventors: Ulrich Kautz, Beate Schmidt
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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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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: 20090203646Abstract: The present invention concerns a method for reducing or preventing development of adhesions, fibrosis or scar tissue within serous body cavities by using sodium narcistatin.Type: ApplicationFiled: February 12, 2009Publication date: August 13, 2009Inventors: Cheri Lubahn, Dianne Lorton
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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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Patent number: 7541463Abstract: The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5-or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.Type: GrantFiled: October 31, 2005Date of Patent: June 2, 2009Assignees: East China University of Science and Technology, Shanghai Institute of Materia Medica, Chinese Academy of Science, Dalian University of TechnologyInventors: Xuhong Qian, Yonggang Li, Yufang Xu, Jian Ding, Liping Lin, Zehong Miao, Hong Zhu, Baoyuan Qu
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Patent number: 7541346Abstract: Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexylcarbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient route to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium pancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray crystallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.Type: GrantFiled: February 4, 2008Date of Patent: June 2, 2009Assignee: Arizona Board of Regents, a body corporate of the State of Arizona, Acting for and on Behalf of the Arizona State UniversityInventors: George R. Pettit, Noeleen Melody
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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
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Publication number: 20090093455Abstract: 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: October 3, 2008Publication date: April 9, 2009Inventors: Johnny Yasuo NAGASAWA, Fabrice PIERRE, Mustapha HADDACH, Michael SCHWAEBE, Levan DARJANIA, Jeffrey P. WHITTEN
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Patent number: 7501435Abstract: The instant invention provides for compounds which comprise substituted triazoloquinazolinones 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: April 24, 2007Date of Patent: March 10, 2009Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Edward J. Brnardic, Vadim Y. Dudkin, Mark E. Fraley, Shaei Y. Huang, Cheng Wang
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Publication number: 20090062324Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.Type: ApplicationFiled: August 19, 2008Publication date: March 5, 2009Applicant: H. Lundbeck A/SInventors: Morten Jorgensen, Benny Bang- Andersen, Ask Puschl, Niels Mork, Jennifer Larsen
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Patent number: 7485649Abstract: 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: January 5, 2006Date of Patent: February 3, 2009Assignee: Merck & Co., Inc.Inventors: Edward J. Brnardic, Mark E. Fraley, Robert M. Garbaccio
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Publication number: 20090030025Abstract: Optionally substituted chromenoisoquinolines and analogs and derivatives thereof are described herein. In addition, syntheses of these compounds are described herein. In addition, uses of these compounds as dopamine receptor binding compounds are described herein.Type: ApplicationFiled: August 20, 2008Publication date: January 29, 2009Applicant: PURDUE RESEARCH FOUNDATIONInventors: David Nichols, Val J. Watts
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Patent number: 7482360Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.Type: GrantFiled: September 21, 2006Date of Patent: January 27, 2009Assignee: Schering CorporationInventors: Duane A. Burnett, Wen-Lian Wu
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Publication number: 20090023767Abstract: 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: ApplicationFiled: December 29, 2006Publication date: January 22, 2009Inventors: Edward J. Brnardic, Mark E. Fraley
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Publication number: 20090012077Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.Type: ApplicationFiled: June 25, 2008Publication date: January 8, 2009Inventors: Alexander Graham Dossetter, Nicola Murdoch Heron
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Publication number: 20090005356Abstract: 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: ApplicationFiled: May 29, 2008Publication date: January 1, 2009Applicant: 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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Publication number: 20080300246Abstract: 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 diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK2? 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR?, PKA, PKB?, PKD2, Rsk1, SAPK2?, SAPK2?, SAPK3, SGK, Tie2 and TrkB kinases.Type: ApplicationFiled: August 9, 2006Publication date: December 4, 2008Applicant: IRM LLCInventors: Yongping Xie, Guobao Zhang, Xing Wang, Nathanael S. Gray, Yi Liu
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Publication number: 20080214594Abstract: 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: ApplicationFiled: January 5, 2006Publication date: September 4, 2008Inventors: Edward J. Brnardic, Mark E. Fraley, Robert M. Garbaccio
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Publication number: 20080182866Abstract: In accordance with the present invention, tetracyclic caboline derivatives that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, these compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.Type: ApplicationFiled: March 15, 2005Publication date: July 31, 2008Inventors: Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson
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Publication number: 20080139601Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferabType: ApplicationFiled: December 15, 2004Publication date: June 12, 2008Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelen, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera