At Least Three Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 548/151)
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Publication number: 20110319425Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 12, 2010Publication date: December 29, 2011Inventors: Christelle Boléa, Sylvain Celanire
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Publication number: 20110319398Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.Type: ApplicationFiled: June 1, 2011Publication date: December 29, 2011Applicant: TUFTS UNIVERSITYInventor: Joan Mecsas
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Publication number: 20110294662Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.Type: ApplicationFiled: April 14, 2011Publication date: December 1, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Jürgen Benting, Ulrike Wachendorff-Neumann
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Publication number: 20110275677Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: January 3, 2011Publication date: November 10, 2011Applicant: ALLERGAN, INC.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Patent number: 7964623Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3Type: GrantFiled: November 17, 2009Date of Patent: June 21, 2011Assignee: Nissan Chemical Industries Ltd.Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
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Publication number: 20110135594Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: July 14, 2009Publication date: June 9, 2011Inventors: Michael Graupe, Chandrasekar Venkataramani
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Publication number: 20110112087Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X 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: April 20, 2010Publication date: May 12, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars VAN DER VEEN, Maria Impagnatiello, Darryl McConnell, Siegfried Schneider, Tobias Wunberg
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Publication number: 20110098327Abstract: This disclosure concerns novel compounds of Formula (I) or Formula (II) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: April 7, 2010Publication date: April 28, 2011Inventors: Rico Lavoie, John A. Bender, Carol Bachand, Edward H. Ruediger, John F. Kadow
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Publication number: 20110076291Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 27, 2010Publication date: March 31, 2011Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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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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Patent number: 7902183Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R5 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 5, 2007Date of Patent: March 8, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Bodo Betzemeier, Darryl McConnell, Thomas Gerstberger, Matthias Grauert, Matthias Hoffmann, Maria Impagnatiello, Lars van der Veen, Ulrike Weyer-Czernilofsky
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Publication number: 20110046132Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: April 28, 2009Publication date: February 24, 2011Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 7893160Abstract: Crosslinkable substituted fluorene compounds; oligomers and polymers prepared from such crosslinkable compounds; films and coatings; and multilayer electronic devices comprising such films are disclosed.Type: GrantFiled: October 25, 2004Date of Patent: February 22, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Michael Inbasekaran, Wanglin Yu
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Patent number: 7888336Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: GrantFiled: September 18, 2008Date of Patent: February 15, 2011Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Publication number: 20110031488Abstract: A compound for an organic thin film transistor having a structure shown by the following formula (1): X1-L-Ar-L-X2 ??(1) wherein L is —C?C—, or —CH?CH— in a trans configuration, X1 and X2 are independently an alkyl group having 2 to 30 carbon atoms or a haloalkyl group having 1 to 30 carbon atoms, and Ar is a substituted or unsubstituted aromatic hydrocarbon group having 14 to 60 ring carbon atoms which is a condensed ring of three or more rings, or a substituted or unsubstituted aromatic heterocyclic group having 11 to 60 ring atoms which is a condensed ring of three or more rings.Type: ApplicationFiled: April 2, 2009Publication date: February 10, 2011Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Masatoshi Saito, Yuki Nakano, Hiroaki Nakamura
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Patent number: 7879887Abstract: The present invention provides novel ?-amino acid derivatives of formula (1): (wherein, R1, R2, R3, R4, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have ?ARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.Type: GrantFiled: June 29, 2007Date of Patent: February 1, 2011Assignees: Nissan Chemical Industries, Ltd., Chugai Seiyaku Kabushiki KaishaInventors: Kazuhiko Ohrai, Michiaki Adachi, Koji Toyama, Takanori Shimizu, Keishi Hayashi, Masataka Minami, Yoshiyuki Suzuki, Masakazu Sugiyama, Masateru Ohta, Shojiro Kadono, Takuya Shiraishi, Haruhiko Sato, Yoshiaki Watanabe, Nobuya Ishii, Masahiro Sakaitani, Masami Hasegawa
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Patent number: 7875639Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 31, 2007Date of Patent: January 25, 2011Assignee: Abbott LaboratoriesInventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
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Publication number: 20110015201Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.Type: ApplicationFiled: February 12, 2009Publication date: January 20, 2011Inventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
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Publication number: 20110014250Abstract: Inhibitors of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), for example tetrazole, styrylpyrazole, phenylfuran, phenylthiophene, phenylpyrrazole, pyrazolecarboxamide, 2-thioacetamide and azo compounds, are useful for promoting or stimulating pigmentation of the skin and/or skin appendages and/or for preventing and/or for limiting depigmentation and/or whitening of the skin and/or skin appendages, notably for preventing and/or limiting canities.Type: ApplicationFiled: February 17, 2010Publication date: January 20, 2011Applicant: L'OREALInventors: JEAN-FRANCOIS MICHELET, STEPHANE COMMO
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Publication number: 20110006287Abstract: A copolymer comprising at least one donor monomer and at least one acceptor monomer is described. The polymer may optionally further comprise, consist or consist essentially of at least one additional comonomer. Various donor monomers, acceptor monomers and additional comonomers are also described. The polymer is useful in the manufacture of microelectronic devices such as optoelectronic devices.Type: ApplicationFiled: March 18, 2010Publication date: January 13, 2011Inventors: Wei You, Shengqiang Xiao
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Publication number: 20110003786Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: ApplicationFiled: July 2, 2010Publication date: January 6, 2011Inventors: Robin Alec FAIRHURST, Marc GERSPACHER, Robert MAH
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Publication number: 20100301314Abstract: According to the first invention group there are provided conjugated compounds having two or more groups represented by the following formula (I) or the following formula (II): wherein one of Ar and Ar? represents a C6 or greater divalent aromatic hydrocarbon group and the other represents a C4 or greater divalent heterocyclic group, wherein the groups each may have a substituent, with the proviso that the groups as a whole contain no fluorine atoms, R1 and R2 each independently represent a hydrogen atom, a halogen atom or a monovalent group, and Ar? represents a trivalent aromatic hydrocarbon or trivalent heterocyclic group; when the conjugated compound has two or more groups represented by formula (I), the portion excluding these groups contain no fluorine atoms.Type: ApplicationFiled: November 27, 2008Publication date: December 2, 2010Applicants: OSAKA UNIVERSITY, SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yoshio Aso, Yutaka Ie, Makoto Okabe, Masashi Nitani, Masato Ueda
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Publication number: 20100292232Abstract: Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs) of the formula Also disclosed are methods of making the NNRTIs, as well as compositions that include such NNRTIs and methods of their use for treating viral infections, in particular retroviral infections, such as HIV infection.Type: ApplicationFiled: November 5, 2008Publication date: November 18, 2010Inventors: Daniel Elleder, John A.T. Young, Thomas J. Baiga, Joseph P. Noel
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Publication number: 20100273839Abstract: The invention provides compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The compositions pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The compositions and pharmaceutical preparations of the invention may comprise one or more bithiazole-containing compounds of the invention, or an analog or derivative thereof.Type: ApplicationFiled: September 5, 2008Publication date: October 28, 2010Inventors: Mark J. Kurth, Alan S. Verkman
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Patent number: 7820657Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: March 16, 2007Date of Patent: October 26, 2010Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Publication number: 20100240614Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: September 18, 2008Publication date: September 23, 2010Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Publication number: 20100234609Abstract: Provided are a compound represented by Formula (I): wherein R1, R2, R3, and R4 are each independently selected from a hydrogen atom, a C1-6 alkyl group which may be substituted, a C7-14 aralkyl group which may be substituted and —C(?O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f). or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 27, 2007Publication date: September 16, 2010Inventors: Tsutomu Sato, Yoshihito Ohtake, Masahiro Nishimoto, Takashi Emura, Takamitsu Kobayashi, Marina Yamaguchi, Kyouko Takami
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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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Patent number: 7750160Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein derivatives of urea 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: July 6, 2010Assignee: Ambit Biosciences CorporationInventors: Zdravko V. Milanov, Hitesh K. Patel, Robert M. Grotzfeld, Shamal A. Mehta, Andiliy G. Lai, David J. Lockhart
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Publication number: 20100163813Abstract: The instant invention relates to novel benzotriazole UV-absorbers having a long wavelength shifted absorption spectrum with significant absorbance up to 410-420 nm. Further aspects of the invention are a process for their preparation, a UV stabilized composition containing the new UV-absorbers and the use of the new compounds as UV-light stabilizers for organic materials.Type: ApplicationFiled: June 18, 2007Publication date: July 1, 2010Inventors: Katharina Fritzsche, Markus Grob, Adalbert Braig, Iloan Marion Kienzle, Gérard Daniel Georges Vilain
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Publication number: 20100150833Abstract: The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus.Type: ApplicationFiled: February 17, 2010Publication date: June 17, 2010Inventors: Gilles D. Tamagnan, David Alagille, Herve Da Costa
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Publication number: 20100144778Abstract: The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: June 26, 2006Publication date: June 10, 2010Inventors: Subharekha Raghavan, Steven L. Colletti, Fa-Xiang Ding, Hong Shen, James R. Tata, Ashley Rouse Lins, Abigail Lee Smenton, Weichun Chen, Darby Rye Schmidt, George Scott Tria
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Publication number: 20100143253Abstract: The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Inventors: Gilles D. Tamagnan, David Alagille, Herve Da Costa
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Publication number: 20100113414Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.Type: ApplicationFiled: January 11, 2010Publication date: May 6, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Bodo BETZEMEIER, Trixi BRANDL, Steffen BREITFELDER, Ralph BRUECKNER, Thomas GERSTBERGER, Michael GMACHL, Matthias GRAUERT, Frank HILBERG, Christoph HOENKE, Matthias HOFFMANN, Maria IMPAGNATIELLO, Dirk KESSLER, Christian KLEIN, Bernd KRIST, Udo MAIER, Darryl McCONNELL, Charlotte REITHER, Stefan SCHEUERER, Andreas SCHOOP, Norbert SCHWEIFER, Oliver SIMON, Martin STEEGMAIER, Steffen STEURER, Irene WAIZENEGGER, Ulrike WEYER-CZERNILOFSKY, Andreas ZOEPHEL
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Publication number: 20100098634Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.Type: ApplicationFiled: July 24, 2009Publication date: April 22, 2010Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
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Patent number: 7691888Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.Type: GrantFiled: October 5, 2005Date of Patent: April 6, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Bodo Betzemeier, Trixi Brandl, Steffen Breitfelder, Ralph Brueckner, Thomas Gerstberger, Michael Gmachl, Matthias Grauert, Frank Hilberg, Christoph Hoenke, Matthias Hoffmann, Maria Impagnatiello, Dirk Kessler, Christian Klein, Bernd Krist, Udo Maier, Darryl McConnell, Charlotte Reither, Stefan Scheuerer, Andreas Schoop, Norbert Schweifer, Oliver Simon, Martin Steegmaier, Steffen Steurer, Irene Waizenegger, Ulrike Weyer-Czernilofsky, Andreas Zoephel
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Publication number: 20100069374Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3Type: ApplicationFiled: November 17, 2009Publication date: March 18, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
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Patent number: 7671078Abstract: The invention relates to isothiourea derivatives of formula I: wherein R1 is a residue of one of the following structures: where the variables are as defined in the claims of the invention, as well as processes for production of these compounds.Type: GrantFiled: February 25, 2005Date of Patent: March 2, 2010Assignee: Novartis AGInventors: Fraser Glickman, Markus Streiff, Gebhard Thoma, Hans-Günter Zerwes
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Publication number: 20090318513Abstract: A compound represented by the general formula (I): wherein R1 is a hydrogen atom, a halogen atom, or the like; R2, R3, and R4 are each independently a hydrogen atom, a halogen atom, C1-C15 alkyl optionally substituted with one or more C1-C12 alkyloxy or the like, or the like; R5 is a hydrogen atom or the like; R6 and R7 are a hydrogen atom or the like; R8 is C1-C3 alkyl or the like; R9 is a hydrogen atom or the like), a prodrug, a pharmaceutically acceptable salt, or solvate thereof.Type: ApplicationFiled: August 27, 2009Publication date: December 24, 2009Inventors: Masami Takayama, Yutaka Yoshida
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Publication number: 20090312352Abstract: The invention generally relates to compositions and methods for treatment of disease caused by Yersinia spp. infection. More specifically, the invention relates to protein tyrosine phosphatase inhibitors and derivatives and analogs thereof, pharmaceutical compositions containing the protein tyrosine phosphatase inhibitors and analogs, methods of making the protein tyrosine phosphatase inhibitors and analogs and methods of use thereof.Type: ApplicationFiled: October 19, 2005Publication date: December 17, 2009Inventors: Tomas Mikael Mustelin, Maurizio Pellecchia, Lutz Tautz
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Publication number: 20090275623Abstract: The present invention provides novel ?-amino acid derivatives of formula (1): (wherein, R1, R2, R3, R4, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have ?ARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.Type: ApplicationFiled: June 29, 2007Publication date: November 5, 2009Inventors: Kazuhiko Ohrai, Michiaki Adachi, Koji Toyama, Takanori Shimizu, Keishi Hayashi, Masataka Minami, Yoshiyuki Suzuki, Masakazu Sugiyama, Masateru Ohta, Shojiro Kadono, Takuya Shiraishi, Haruhiko Sato, Yoshiaki Watanabe, Nobuya Ishii, Masahiro Sakaitani, Masami Hasegawa
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Publication number: 20090258857Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: ApplicationFiled: June 13, 2007Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Patent number: 7601846Abstract: The present invention provides compounds that can protect mammalian cells from the damaging effects of chemotherapy, irradiation, or in other situations in which it is desirable to protect tissue from the consequences of clinical or environmental stress.Type: GrantFiled: November 10, 2005Date of Patent: October 13, 2009Assignee: The Regents of the University of CaliforniaInventors: Howard B. Cottam, Dennis A. Carson, Sylvie Barchechath
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Publication number: 20090247567Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: March 30, 2009Publication date: October 1, 2009Applicant: Genentech, Inc.Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
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Publication number: 20090156554Abstract: New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.Type: ApplicationFiled: February 5, 2009Publication date: June 18, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen BREITFELDER, Udo MAIER, Trixi BRANDL, Christoph HOENKE, Matthias GRAUERT, Alexander PAUTSCH, Matthias HOFFMANN, Frank KALKBRENNER, Anne T. JOERGENSEN, Gerhard SCHAENZLE, Stefan PETERS, Frank BUETTNER, Eckhart BAUER
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Publication number: 20090143376Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: March 3, 2006Publication date: June 4, 2009Applicant: Sitris Pharmaceuticals, Inc.Inventors: Michael Milburn, Jill Milne, Jean Bemis, Joseph J. Nunes, Roger Xie, Karl D. Nomington, Chi B. Vu
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Publication number: 20090108733Abstract: The present invention relates to a precursor of metallic complex for electroluminescent material, a luminescent material comprised of said precursor of metallic complex and metal, and an electroluminescent device containing a luminescent material comprised of said precursor and metal. The luminescent material comprised of the precursor according to the present invention and metal is advantageous in that it shows excellent electric conductivity and light emitting property of high efficiency.Type: ApplicationFiled: January 22, 2006Publication date: April 30, 2009Applicant: GRACEL DISPLAY INC.Inventors: Sung-Min Chin, Sang-Man Si, Keun-Hee Han, Kyung-Hoon Choi, Mi-Young Kwak, Bong-Ok Kim, Sung-Min Kim
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Patent number: 7517995Abstract: Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-cyclopentapyrazoles and the use thereof as pharmaceutical compositions.Type: GrantFiled: March 23, 2007Date of Patent: April 14, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Breitfelder, Udo Maier, Christoph Hoenke, Anne T. Joergensen, Alexander Pautsch, Trixi Brandl, Matthias Grauert, Matthias Hoffmann, Stefan Scheuerer, Klaus Erb, Michael Pieper, Ingo Pragst
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Publication number: 20090093474Abstract: The present invention relates to new thiazolyl-dihydro-indazoles of general formula (I) wherein the groups R1, R2 and R3 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-indazoles and the use thereof as pharmaceutical compositions.Type: ApplicationFiled: November 25, 2008Publication date: April 9, 2009Inventors: Matthias Grauert, Udo Maier, Matthias Hoffmann, Stefan Scheuerer, Anne T. Joergensen, Alexander Pautsch, Trixi Brandl, Christoph Hoenke, Steffen Breitfelder, Klaus Erb, Michael Pieper, Ingo Pragst
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Patent number: 7498327Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: June 22, 2005Date of Patent: March 3, 2009Assignee: WyethInventors: Youchu Wang, Chia-Cheng Shaw, Ronald Charles Bernotas, Chung-Chiee Paul Wang, Ping Cai, Zhi Wang