At Least Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/236)
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Publication number: 20100324049Abstract: [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease. [Means for Solving Problems] The antagonist comprises, as an active ingredient, a compound represented by the formula (I) wherein R1a and R1b independently represent a hydrogen atom or a C1-6 alkyl group; R2a, R2b, R3a and R3b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Y represents H or —OH; Z represents —OR8, or the like; R8 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, or the like; R9a and R9b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Ar1 represents an aromatic carbon ring group, or an aromatic heteroring group; Ar2 represents a group produced by removing two hydrogen atoms from an aromatic carbon ring, or the like; and the ring group A represents an unsaturated heteroring group.Type: ApplicationFiled: September 26, 2008Publication date: December 23, 2010Inventors: Makoto Ando, Minoru Kameda, Hiroshi Miyazoe, Minoru Moriya, Etsuko Hirose, Takao Suzuki
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Publication number: 20100311757Abstract: Salarines and Tulearins isolated from Fascaplysinopsis sp. sponge and synthetic derivatives thereof are provided.Type: ApplicationFiled: September 25, 2008Publication date: December 9, 2010Applicants: RAMOT AT TEL-AVIV UNIVERSITY LTD., Université De La RéunionInventors: Yoel Kashman, Maurice Aknin, Amira Rudi, Ashgan Bishara, Drorit Neumann, Nathalie Ben Califa
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Publication number: 20100305070Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: December 2, 2010Applicant: The University Court of the University of DundeeInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20100305113Abstract: The invention relates to novel compounds of the formula I, as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.Type: ApplicationFiled: May 7, 2008Publication date: December 2, 2010Inventors: Hans-Georg Capraro, Patricia Imbach, Giorgio Caravatti, Pascal Furet
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Publication number: 20100297128Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula [Chemical formula should be inserted here as it appears on abstract in electronic form.] 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 9, 2008Publication date: November 25, 2010Inventors: Xianhai Huang, Anandan Palani, Robert G. Aslanian
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Publication number: 20100298315Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.Type: ApplicationFiled: January 26, 2010Publication date: November 25, 2010Applicant: sanofi-aventisInventors: Eva ALBERT, Eric BACQUE, Conception NEMECEK, Antonio UGOLINI, Sylvie WENTZLER
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Publication number: 20100298349Abstract: Compounds of formula (I) are A2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C1-C6alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-(C1-C6) -alkyl; or R?1 and R2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3 and R4 are independently selected from hydrogen, or optionally substituted C1-C6 alkyl, C1-C6 alkoxy-(C1-C6)-alkyl, C3-C8 cycloalkyl, aryl, heteroaryl, aryl-(C1-C6)-alkyl, or heteroaryl-C1-C6)-alkyl; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R5 and R6 are independently selected from hydrogen, C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl, —NHR7—N(—R8)—R9, —NH—(C?O)—R10, —(C?O)—NH—R11, —(C?O)—O—R12, or halo; and R7, R8, R9, R10, R?11, and R12 are independently selected from C1-C6 alkyl, aryl, aryl-(C1-C6)-alkyl and heteroaryl.Type: ApplicationFiled: September 19, 2008Publication date: November 25, 2010Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karinne Poullennec
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Publication number: 20100297097Abstract: The present invention relates to substituted triazole compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming A?42 peptide such as Alzheimer's disease and the like.Type: ApplicationFiled: November 7, 2008Publication date: November 25, 2010Inventors: Anne Marie Jeanne Bouillot, Alain Laroze
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Publication number: 20100292241Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: January 14, 2009Publication date: November 18, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
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Publication number: 20100292222Abstract: The invention concerns bicyclic compounds of Formula (I) wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.Type: ApplicationFiled: May 10, 2010Publication date: November 18, 2010Applicant: ASTRAZENECA ABInventors: Robert Hugh Bradbury, Alfred Arthur Rabow
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Publication number: 20100292238Abstract: Phenoxymethyl compounds that inhibit at least one phosphodiesterase 10 are described as are pharmaceutical compositions containing such compounds an methods for treating various CNS disorders by administering such compounds to a patient in need thereof.Type: ApplicationFiled: December 18, 2009Publication date: November 18, 2010Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20100292205Abstract: The invention pertains to pyrimidone compounds that serve as effective GSK-3 inhibitors. The invention further relates to pharmaceutical compositions and methods comprising such pyrimidone compounds; and the use of such compounds for treating certain disorders.Type: ApplicationFiled: August 13, 2007Publication date: November 18, 2010Applicant: PFIZER INC.Inventors: Bruce A. Lefker, Michael A. Brodney, Subas M. Sakya, Bruce A. Hay, Matthew D. Wessel, Edward L. Conn
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Publication number: 20100285145Abstract: Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.Type: ApplicationFiled: May 6, 2010Publication date: November 11, 2010Inventors: Etzer Darout, Michael P. DeNinno, Kentaro Futatsugi, Cristiano Guimaraes, Bruce A. Lefker, Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
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Publication number: 20100280007Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: ApplicationFiled: June 15, 2010Publication date: November 4, 2010Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Allison L. Zulli
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Publication number: 20100273788Abstract: The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.Type: ApplicationFiled: November 3, 2008Publication date: October 28, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nozomu SAKAI, Shinichi IMAMURA, Naoki MIYAMOTO, Takaharu HIRAYAMA
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Publication number: 20100273802Abstract: This invention provides 2-, 6, and 9-substituted purine derivatives, particularly 2(1-R hydroxymethylpropylamino)-6-benzylamino-9-isopropyl purine, having, in particular, antiproliferative properties, and suitable for use as pharmaceutical compositions and herbicidal compositions. Also provided are pharmaceutical compositions and herbicidal compositions comprising the 2-, 6, and 9-substituted purine derivatives, and methods of treatment using the 2-, 6, and 9-substituted purine derivatives.Type: ApplicationFiled: December 23, 2009Publication date: October 28, 2010Inventors: Laurent MEIJER, Emile BISAGNI, Michel LEGRAVEREND, Miroslav STRNAD
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Publication number: 20100273801Abstract: The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications.Type: ApplicationFiled: June 6, 2007Publication date: October 28, 2010Applicant: Valition teknillinen tutikimuskeskusInventors: Jari Yli-Kauhaluoma, Salme Koskimies, Sami Alakurtti, Taru Mäkelä, Päivi Tammela
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Publication number: 20100273775Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.Type: ApplicationFiled: December 10, 2008Publication date: October 28, 2010Applicant: E.I. Du pont de Nemours and CompanyInventors: John Joseph Bisaha, Alvin Donald Crews, JR., Michael Henry Howard, JR., Paula Louise Sharpe, Thomas Martin Stevenson, Andrew Edmund Taggi
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Patent number: 7820664Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: January 18, 2008Date of Patent: October 26, 2010Assignee: Bayer Schering Pharma AGInventors: Jean-Michel Vernier, Andreas Maderna, Yung-hyo Koh, Zhi Hong
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Patent number: 7820665Abstract: The present invention relates to imidazopyridazine compounds of Formula I, such as representative structure A, or a pharmaceutically acceptable salt thereof, that inhibit phosphoinositide 3-kinase; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds.Type: GrantFiled: December 18, 2008Date of Patent: October 26, 2010Assignee: Amgen Inc.Inventors: Shon Booker, Tae-Seong Kim, Hongyu Liao, Longbin Liu, Mark H. Norman, Emily Anne Peterson, Markian Stec, Nuria A. Tamayo
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Publication number: 20100267730Abstract: This invention relates to imidazopyridazine substituted piperidine derivatives and their use as pharmaceuticals.Type: ApplicationFiled: October 9, 2009Publication date: October 21, 2010Inventors: Giuseppe ALVARO, David Amantini, Sandro Belvedere
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Publication number: 20100267708Abstract: The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: December 22, 2008Publication date: October 21, 2010Applicant: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Sung Bae Lee, Seung Hyun Yoon, Mi Kyoung Cho, Kyoung Hee Kim, Heui Sul Park, Hyoung Jin Kim
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Publication number: 20100267699Abstract: The invention concerns bicyclic compounds of Formula I wherein , R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.Type: ApplicationFiled: February 9, 2010Publication date: October 21, 2010Inventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
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Patent number: 7816526Abstract: The present invention provides a compound represented by the formula: wherein Q represents a fused heterocyclic group, X and Y are the same or different and each represent an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, etc., or a salt thereof, as well as a herbicide comprising the compound or a salt thereof, which exhibits a significant effect for control of sulfonylurea herbicide-resistant weeds in paddy fields and can reduce the number of active ingredients in a combined preparation and a method of controlling sulfonylurea herbicide-resistant weeds which comprises using the same.Type: GrantFiled: January 15, 2003Date of Patent: October 19, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Yasushi Tanaka, Yukari Kajiwara, Makoto Noguchi, Takeshi Kajiwara, Takanori Tabuchi
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Patent number: 7816357Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I. including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R4, R5, m and n are described herein.Type: GrantFiled: December 17, 2004Date of Patent: October 19, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Guixue Yu, William R. Ewing, Amarendra B. Mikkilineni, Annapurna Pendri, Bruce A. Ellsworth, Philip M. Sher, Samuel Gerritz, Chongqing Sun, Natesan Murugesan, Ximao Wu
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Publication number: 20100261724Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: October 23, 2008Publication date: October 14, 2010Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
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Patent number: 7812158Abstract: The present invention is directed to compounds of the formula (I) and (II) or salts thereof or N-oxides and their use in peptide synthesis.Type: GrantFiled: November 1, 2004Date of Patent: October 12, 2010Assignee: University of MassachusettsInventors: Louis A. Carpino, Jusong Xia, Chongwu Zhang, Calin Dan Sferdean
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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: 20100240663Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: February 16, 2010Publication date: September 23, 2010Applicant: Icagen, Inc.Inventors: Thomas Eugene Christos, George S. Amato, Robert N. Atkinson, Maria Graciela Barolli, Lilli Ann Wolf-Gouveia, Mark J. Suto
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Publication number: 20100234348Abstract: The present invention provides compounds that potentiate the activity of antibiotic agents, particularly quinolones such as norflaxin. The invention further provides compositions, e.g., pharmaceutical compositions, comprising the inventive compounds. The invention also provides compositions comprising an antibiotic (e.g., a quinolone) and a compound that potentiates activity of the antibiotic. The invention further provides methods of treating a subject comprising administering any of the inventive compounds or compositions to the subject. The invention also provides screening methods to identify compounds that potentiate the activity of an antibiotic, e.g., a quinolone.Type: ApplicationFiled: August 2, 2007Publication date: September 16, 2010Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: Guillaume Cottarel, Timothy S. Gardner, Xiaoguang Lei, John Porco, Scott E. Schaus, Jamey Wierzbowski, Kollol Pal
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Publication number: 20100234597Abstract: A process for producing an imidazo[1,2-b]pyridazine compound represented by the formula (2): wherein R1, R2 and R3 are the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group which may be substituted with a halogen atom or atoms, an alkenyl group which may be substituted with a halogen atom or atoms, or an alkoxy group which may be substituted with a halogen atom or atoms, which comprises reacting a 2,3-dihydropyridazine compound represented by the formula (1): wherein R1, R2 and R3 are the same meanings as defined above, with a phosphorus oxyhalide in the presence of an organic base which is in an amount of 0.5 mole or more relative to 1 mole of the 2,3-dihydropyridazine compound and 1 mole or less relative to 1 mole of the phosphorus oxyhalide.Type: ApplicationFiled: August 22, 2006Publication date: September 16, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Ichiro Komoto, Kazuaki Sasaki, Tomohiko Gotou
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100222326Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 24, 2008Publication date: September 2, 2010Applicant: UCB PHARMA, S.A.Inventors: Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
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Publication number: 20100216768Abstract: The invention relates to N-substituted azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to N-substituted azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: June 11, 2008Publication date: August 26, 2010Inventors: Hazel Joan Dyke, Stephen Price, Karen Williams
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Publication number: 20100216798Abstract: There is provided fused heterocycles of imidazopyridazine or pyrazolopyrimidine derivative represented by the formula (I), which have excellent Lck inhibitory activity and are useful for a medicament particularly an immunosuppressive agent. [wherein one of Y and Z is C atom, and the other is N atom; —X— is —N(R1)— or the like, —R1 represents hydrogen or the like, -A- represents bond or the like, —R2 is cycloalkyl, aryl or the like, -E- is bond or the like, —R3 is aryl, aromatic heterocycle or the like, —R4, —R5 and —R6 are the same or different, each being hydrogen or the like.Type: ApplicationFiled: July 27, 2006Publication date: August 26, 2010Applicant: ASTELLAS PHARMA INCInventors: Kazuo Nakai, Fumie Takahashi, Kazuya Fujita, Yoshihiro Kozuki, Koichiro Mukoyoshi, Masamichi Inami, Norio Asai
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Publication number: 20100216799Abstract: The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.Type: ApplicationFiled: October 10, 2008Publication date: August 26, 2010Applicant: Glaxo Group LimitedInventors: Paul Martin Gore, Brian Edgar Looker, Panayiotis Alexandrou Procopiou, Sadie Vile
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Publication number: 20100210642Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.Type: ApplicationFiled: March 29, 2010Publication date: August 19, 2010Inventors: Silvia Gatti McArthur, Erwin Goetschi, Wylie Solang Palmer, Juergen Wichmann, Thomas Johannes Woltering
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Publication number: 20100210649Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.Type: ApplicationFiled: December 21, 2007Publication date: August 19, 2010Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
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Publication number: 20100209345Abstract: The invention provides fluorinated compounds of formula (I): The compounds may be used in diagnosis or treatment of a disorder in a mammal characterised by an abnormal density of peripheral benzodiazepine receptors.Type: ApplicationFiled: August 24, 2007Publication date: August 19, 2010Inventors: Andrew Katsifis, Christopher John Reginald Fookes, Tien Quoc Pham, Ivan Damir Greguric, Maria Filomena Pereira Soares Mattner
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Patent number: 7777035Abstract: Methods are provided for the synthesis of 1-[4-(substituted phenyl)-piperazin-1-yl ] -2- [3-(1H-imidazol-2-yl)-pyrazolo [3,4-b]pyridin-1-yl]-ethanone compounds via construction of the imidazole portion onto the corresponding aldehyde or nitrile compounds.Type: GrantFiled: May 22, 2007Date of Patent: August 17, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu, Mark M. Gleason, Yibin Zeng, Kevin Lloyd Greenman
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Publication number: 20100204212Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, Z is N, and R1, R2, R3, X and Y are as defined herein.Type: ApplicationFiled: April 8, 2010Publication date: August 12, 2010Inventors: Wayne Vaccaro, David R. Tortolani, Tram N. Huynh
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Publication number: 20100204235Abstract: Compounds of formula I in free or salt or solvate form, where R1, R2 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: July 24, 2008Publication date: August 12, 2010Inventors: Dimitrios Lizos, Sven Weiler, Nikolaus Johannes Stielf
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Publication number: 20100204470Abstract: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.Type: ApplicationFiled: June 25, 2007Publication date: August 12, 2010Inventors: Josef Wieser, Hannes Lengauer, Elfriede Klingler, Arthur Pichler, Hubert Sturm
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Patent number: 7772226Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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Publication number: 20100196357Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: January 21, 2010Publication date: August 5, 2010Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20100197912Abstract: The invention relates to novel polymorphic and hydrate forms and salts of 6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline, to methods for their preparation, to pharmaceutical compositions comprising at least one of said polymorphic or hydrate forms or salts, and to the therapeutic and/or prophylactic use of such compositions. The invention also provides new manners for preparing said compound.Type: ApplicationFiled: June 19, 2008Publication date: August 5, 2010Inventors: Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Carina Leys, Julius Walter Jozef Dickens, Sigrid Carl Maria Stokbroekx
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Publication number: 20100197682Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: ApplicationFiled: July 16, 2008Publication date: August 5, 2010Inventors: Ian Bruce, Darren Mark Legrand, James Dale, Thomas Anthony Hunt
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Patent number: 7767670Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: August 3, 2010Assignee: Ambit Biosciences CorporationInventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
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Publication number: 20100190774Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.Type: ApplicationFiled: April 8, 2010Publication date: July 29, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David J. Lauffer, Alexander Aronov, Pan Li, David D. Deininger, Kira McGinty, Dean Stamos, Jon H. Come, Michelle Stewart
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Publication number: 20100190795Abstract: The invention relates to betulin derivatives, and to the use thereof as agents against protozoa of the genus Leishmania and against leishmaniasis in applications of pharmaceutical industry.Type: ApplicationFiled: June 6, 2007Publication date: July 29, 2010Applicant: Valtion Teknillinen tutkimuskeskusInventors: Jari Yli-Kauhaluoma, Sami Alakurtti, Jaana Minkkinen, Nina Sarcerdoti-Sierra, Charles L. Jaffe, Tuomo Heiska