The Additional Hetero Ring Is Five-membered Consisting Of Carbon And Plural Nitrogens As The Only Ring Members Patents (Class 514/266.23)
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Publication number: 20110160232Abstract: Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.Type: ApplicationFiled: October 6, 2008Publication date: June 30, 2011Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson
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Publication number: 20110136766Abstract: Disclosed herein are Aurora kinase Inhibitors represented by Structural Formula (I): Values for the variables in Structural Formula (I) are defined herein.Type: ApplicationFiled: March 4, 2009Publication date: June 9, 2011Inventors: Linghang Zhuang, David A. Claremon, Suresh B. Singh, Lingling Shen, Yajun Zheng, John David Lawson
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Publication number: 20110129463Abstract: Provided are quinazolin-4(3A)-one derivatives, which are inhibitors of the ubiquitin ligase activity of a human polypeptide, particularly to POSH inhibitors, and to compositions and methods for the treatment RING E3 ubiquitin ligase related diseases.Type: ApplicationFiled: November 26, 2010Publication date: June 2, 2011Applicant: Proteologics, Ltd.Inventors: Omri EREZ, Philippe NAKACHE
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Publication number: 20110118258Abstract: Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.Type: ApplicationFiled: May 15, 2008Publication date: May 19, 2011Inventors: Stephen Martin Courtney, Mark Whittaker, Owen Clifford Mather, Christopher John Yarnold, Oliver Robin Barker, Christian Aldo Georges Napoleon Montalbetti, Thomas Hesterkamp, Mihaly Daniel Gardiner
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Publication number: 20110118289Abstract: The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from —CH group or a nitrogen atom (—N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R1 is independently selected from hydrogen (—H), C1-C4 alkyl, hydroxymethyl (—CH2OH), aminomethyl (—CH2NH2), alkylaminomethyl [CH2NH(R2)], or di-alkylaminomethyl [CH2N(R2)2], trifluoromethyl (—CF3).Type: ApplicationFiled: June 20, 2008Publication date: May 19, 2011Applicant: ROTTAPHARM S.P.A.Inventors: Antonio Giordani, Marco Lanza, Gianfranco Caselli, Stefano Mandelli, Simona Zanzola, Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20110086856Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: December 14, 2010Publication date: April 14, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Juliam M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Patent number: 7923450Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X and Y are as defined herein and to pharmaceutically active acid addition salts thereof. The compounds can be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.Type: GrantFiled: January 5, 2009Date of Patent: April 12, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers
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Publication number: 20110077233Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: October 25, 2010Publication date: March 31, 2011Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Publication number: 20110071144Abstract: The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group seleType: ApplicationFiled: April 23, 2010Publication date: March 24, 2011Inventors: Andrew Peter THOMAS, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Publication number: 20110070297Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 1, 2010Publication date: March 24, 2011Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company LimitedInventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
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Publication number: 20110064697Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20110055978Abstract: The present invention relates to synergistic mixtures comprising, as active components, an insecticidal compound I selected from the nicotinic receptor agonists/antagonists compounds and one or two further fungicidal compounds in synergistic effective amounts.Type: ApplicationFiled: February 4, 2009Publication date: March 3, 2011Applicant: BASF SEInventors: Laurent Jamet, Ralf Willi Gerhard, Dirk Voeste
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Publication number: 20110046148Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.Type: ApplicationFiled: February 5, 2009Publication date: February 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz
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Publication number: 20110039845Abstract: A 2-aminoquinazoline derivative represented by formula (I) {wherein R1 represents a hydrogen atom, or the like, R2 represents a hydrogen atom, R3 represents formula (II) [wherein A1 represents formula (III), or the like, R8 represents lower alkyl, or the like, and R9 represents optionally substituted aryl, or the like], R4 represents hydroxy, or the like, and R5 represents optionally substituted aryl, or the like}, or a pharmaceutically acceptable salt thereof is provided.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hajime Kashima, Tomoyuki Nishikawa, Yusuke Yamada, Toshihiro Seike, Yoshisuke Nakasato, Hiroshi Umehara
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Patent number: 7879867Abstract: Novel crystalline forms of (1R,2R)-7-chloro-3-[2-(2,4-difluorophenyl)-2 -hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]quinazolin-4(3H)-one, pharmaceutical compositions containing these crystalline forms, methods of using these crystalline forms for treating and/or preventing various microbial and/or fungal infections or disorders, and processes for obtaining these crystalline forms.Type: GrantFiled: August 6, 2007Date of Patent: February 1, 2011Assignees: Palau Pharma, S.A., Stiefel Laboratories, Inc.Inventors: Antonio Cánovas Paredes, Javier Bartroli Orpi, Elies Molins Grau, Anna Roig Serra, Kevin Meyer, Keith Lorimer
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Publication number: 20110021500Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as in the description, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.Type: ApplicationFiled: November 21, 2008Publication date: January 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Patent number: 7863282Abstract: A compound of formula Ia: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 15, 2006Date of Patent: January 4, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Publication number: 20100324029Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: ApplicationFiled: February 5, 2008Publication date: December 23, 2010Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
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Publication number: 20100317659Abstract: Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: February 26, 2010Publication date: December 16, 2010Inventors: Sunny Abraham, Qi Chao, Michael J. Hadd, Mark W. Holladay, Gang Liu, Eduardo Setti
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Publication number: 20100298359Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).Type: ApplicationFiled: December 4, 2008Publication date: November 25, 2010Inventors: Xianhai Huang, Anandan Palani, Jun Qin, Robert Aslanian, Zhaoning Zhu, William Greenlee
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Patent number: 7834000Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: GrantFiled: June 13, 2007Date of Patent: November 16, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Corey Gutierrez, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Daniele Bergeron, Sanghee Yoo, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar
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Publication number: 20100278835Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory syncytial virus (RSV).Type: ApplicationFiled: March 9, 2010Publication date: November 4, 2010Applicants: ASTRAZENECA UK LIMITED, ARROW THERAPEUTICS LIMITEDInventors: Helen Blade, Heather Marie Jackson, Gary Peter Tomkinson, Elisa Ann Carron, James Andrew Lumley, Christopher John Pilkington, Alexander James Floyd Thomas, Justin Warne
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Publication number: 20100261740Abstract: The invention relates to substituted 4-(tetrazol-5-yl)-quinazoline derivatives of the formula-I, or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted 4-(tetrazol-5-yl)-quinazoline derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti-proliferative effect in a warm-blooded animal such as man.Type: ApplicationFiled: October 28, 2008Publication date: October 14, 2010Applicant: Natco Pharma LimitedInventors: Durga Prasad Konkanchi, Subba Rao Pula, Lakshmi Anathaneni, Muddasani Pulla Reddy, Bhujanga Rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
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Publication number: 20100249146Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: ApplicationFiled: November 10, 2008Publication date: September 30, 2010Inventors: Tomoharu Iino, Akio Ohno, Norikazu Otake, Takuya Suga, Masanori Asia
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Publication number: 20100249159Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: ApplicationFiled: March 18, 2010Publication date: September 30, 2010Inventors: Dhanapalan Nagarathnam, Chunguang Wang
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Publication number: 20100221259Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Publication number: 20100222331Abstract: The present invention encompasses compounds of general Formula (1) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Bodo Betzemeier, Guido Boehmelt, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Daniel Kuhn, Jens Juergen Quant, Ulrich Reiser, Otmar Schaaf, Flavio Solca, Heinz Stadtmueller, Ulrike Tontsch-Grunt, Matthias Treu, Stephan Karl Zahn
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Publication number: 20100210709Abstract: Methods of preventing the development and reversing or partially reversing opioid tolerance in a subject are provided herein. Such methods include the step of administering to a subject in need thereof a therapeutically effective amount of a PDGFR modulator or EGFR modulator alone or together with an opiate analgesic. The methods can also be used for the treatment of refractory neuropathic pain, physical dependence or addiction.Type: ApplicationFiled: October 8, 2008Publication date: August 19, 2010Inventor: Gutstein B. Howard
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Publication number: 20100204226Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: February 10, 2010Publication date: August 12, 2010Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, JR., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Publication number: 20100184757Abstract: Active compound mixtures comprising ipconazole and at least one further fungicidally active compound are highly suitable for protecting industrial materials against colonization and destruction by microorganisms.Type: ApplicationFiled: January 22, 2010Publication date: July 22, 2010Applicant: LANXESS Deutschland GmbHInventors: Rainer Bruns, Martin Kugler, Thomas Jaetsch
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Publication number: 20100179152Abstract: The present invention is concerned with the use of PDE5 inhibitors in medicine.Type: ApplicationFiled: January 4, 2010Publication date: July 15, 2010Applicant: NYCOMED GmbHInventors: Torsten Dunkern, Christian Schudt, Friedrich Grimminger, Hossein Ardeschir Ghofrani, Manfred Kaps, Bernhard Rosengarten
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Publication number: 20100158863Abstract: A quinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof: formula (I) for use in treatment of prevention of a flaviviridae infection.Type: ApplicationFiled: January 11, 2007Publication date: June 24, 2010Applicant: ARROW THERAPEUTICS LIMITEDInventors: Neil Mathews, Alexander James Floyd Thomas, Keith Charles Spencer, Nathalie Tiberghien, Christopher John Pilkington, Lyn Jennens, Surinder Chana, Ian John Fraser
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Publication number: 20100144731Abstract: Novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided.Type: ApplicationFiled: September 3, 2009Publication date: June 10, 2010Applicant: Dr. Reddy's Laboratories Ltd.Inventors: Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti
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Publication number: 20100143299Abstract: This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR?R? and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-?/-oxide, a solvate or a pro-drug thereof.Type: ApplicationFiled: July 20, 2007Publication date: June 10, 2010Applicant: Gilead Sciences, Inc.Inventors: Ling-Jie Gao, Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
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Publication number: 20100144707Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: ApplicationFiled: March 27, 2006Publication date: June 10, 2010Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam
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Publication number: 20100137324Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: ApplicationFiled: February 2, 2010Publication date: June 3, 2010Inventors: Dhanaphalan Nagarathnam, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Uday Khire, Chunguang Wang, Barry Hart, Stephen Boyer, Olaf Weber, Mark Lynch
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Patent number: 7718663Abstract: An object of the present invention is to provide an antipruritic agent having a novel action mechanism. The present invention provides an antipruritic agent comprising a compound represented by the following general formula (1): wherein R1 represents a hydrogen atom or alkyl; the ring Q represents a cyclohexylene group or a phenylene group; A1 and A2 represent a single bond or an alkylene group; E represents —NHCO—; A3 represents a single bond or a divalent saturated or unsaturated aliphatic hydrocarbon group; R3 represents a non-cyclic aliphatic hydrocarbon group; and R4 and R5 are the same or different and each represents a hydrogen atom or alkyl, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: April 28, 2003Date of Patent: May 18, 2010Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiko Okano, Tatsuya Oyama
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Publication number: 20100099681Abstract: The present application relates to novel substituted 5-aminopyrazoles, methods of production thereof, use thereof alone or in combinations for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases.Type: ApplicationFiled: August 13, 2009Publication date: April 22, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lars Bärfacker, Raimund Kast, Nils Griebenow, Heinrich Meier, Peter Kolkhof, Barbara Albrecht-Küpper, Adam Nitsche, Nicole Teusch, Johannes-Peter Stasch, Dirk Schneider
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Patent number: 7691853Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: March 6, 2006Date of Patent: April 6, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M. C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert J. Davies, Pan Li, Marion W. Wannamaker, Cornelia J. Forster, Albert C. Pierce
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Patent number: 7687502Abstract: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 23, 2005Date of Patent: March 30, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Morihiro Mitsuya, Makoto Bamba, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki, Keisuke Arakawa
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Publication number: 20100069412Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: ApplicationFiled: April 28, 2009Publication date: March 18, 2010Applicant: ASTRAZENECA ABInventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri JUNG, Georges Rene PASQUET
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Publication number: 20100040575Abstract: Physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.Type: ApplicationFiled: July 21, 2009Publication date: February 18, 2010Applicant: PROBIODRUG AGInventors: Torsten Hoffmann, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
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Publication number: 20100022476Abstract: The invention provided a compound of formula: (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient.Type: ApplicationFiled: December 16, 2005Publication date: January 28, 2010Applicant: ASTRAZENECA ABInventor: Kevin Michael Foote
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Publication number: 20090318291Abstract: Fungicidal mixtures of 1-methylpyrazol-4-ylcarboxanilides and azolopyrimidinylamines Fungicidal mixtures comprising as active components: 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I ?in which the substituents are defined according to the description and 2) at least one azolopyrimidinylamine of the formula II ?in which the substituents are defined according to the description in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I and compound II and also the use of the compound I and the compound II for preparing such mixtures, and compositions comprising such mixtures.Type: ApplicationFiled: January 17, 2008Publication date: December 24, 2009Applicant: BASF SEInventors: Jochen Dietz, Ulrich Schöfl, Egon Haden
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Publication number: 20090306044Abstract: The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy.Type: ApplicationFiled: November 9, 2006Publication date: December 10, 2009Inventors: Flavio Solca, Andree Amelsberg, Gerd Stehle, Jacobus C.A. Van Meel, Anke Baum
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Publication number: 20090306073Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: ApplicationFiled: April 5, 2007Publication date: December 10, 2009Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Swapnil G. Yerande, Gajanan S. Inamdar, Jitendra C. Kaila, H. Padh Ahmedabad, Vasudevan Sudarsanam
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Patent number: 7625908Abstract: A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: GrantFiled: November 11, 2004Date of Patent: December 1, 2009Assignee: AstraZeneca ABInventors: Laurent Francois Andre Hennequin, Robert Hugh Bradbury, Jason Grant Kettle
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Patent number: 7625910Abstract: The present invention relates to a novel co-crystal of 2-{ethyl[3-({4-[(5-{2-[(3-fluorophenyl)amino]-2-oxoethyl}-1H-pyrazol-3-yl)amino]quinazolin-7-yl}oxy)propyl]amino}ethyl dihydrogen phosphate (AZD1152) which is an aurora kinase inhibitor that is useful in the treatment of hyperproliferative diseases such as cancer.Type: GrantFiled: May 15, 2007Date of Patent: December 1, 2009Assignee: AstraZeneca ABInventors: George Joseph Sependa, Richard Storey
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Publication number: 20090291940Abstract: Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.Type: ApplicationFiled: March 30, 2007Publication date: November 26, 2009Applicants: Taisho Pharmaceutical Co., Ltd., Nissan Chemical Industries, Ltd.Inventors: Taketoshi Okubo, Toshihito Kumagai, Takaaki Ishii, Toshio Nakamura, Kumi Abe, Yuri Amada, Tomoko Ishizaka, Xiang-Min Sun, Yoshinori Sekiguchi, Shigetada Sasako, Takanori Shimizu, Takayuki Nagatsuka
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Publication number: 20090291971Abstract: The present invention relates to processes for the preparation of heteroaryl ethers. In some embodiments, the processes relate to cross coupling reactions between triazol-1-yloxy and triazol-1-yl heterocycles with aryl boronic acids. In a further aspect, this invention also relates to compounds that are useful for the treatment of oncological diseases or disorders, and for the treatment of inflammation.Type: ApplicationFiled: October 30, 2008Publication date: November 26, 2009Applicant: WyethInventors: Tarek Suhayl Mansour, Sumrit Wacharasindhu, Zhao-Kui Wan, Sujata Bardhan