Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 544/250)
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Patent number: 8207180Abstract: The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.Type: GrantFiled: November 23, 2007Date of Patent: June 26, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
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Patent number: 8207181Abstract: The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I): wherein p, n, A, B, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.Type: GrantFiled: September 3, 2010Date of Patent: June 26, 2012Assignee: SanofiInventors: Raymond Walter Kosley, Jr., Rosy Sher
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Publication number: 20120157306Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.Type: ApplicationFiled: September 2, 2011Publication date: June 21, 2012Applicant: BAYER CROPSCIENCE AGInventors: Jens FRACKENPOHL, Hans-Joachim Zeiß, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
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Publication number: 20120157453Abstract: Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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: August 27, 2010Publication date: June 21, 2012Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Steven Mark Wenglowsky
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Publication number: 20120149688Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 10, 2011Publication date: June 14, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
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Publication number: 20120142911Abstract: The present invention relates to the synthesis of intermediates which are useful in TTX synthesis and to the preparation thereof.Type: ApplicationFiled: June 11, 2010Publication date: June 7, 2012Inventors: Pedro Noheda Marín, Luis Miguel Lozano Gordillo, Nuria Tabares Cantero, Raúl Benito Arenas, David Herrero
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Patent number: 8193178Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: September 12, 2008Date of Patent: June 5, 2012Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120128686Abstract: The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: ApplicationFiled: August 24, 2009Publication date: May 24, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Austen, Phillip Black, Wesley Blackaby, John Danilewicz, Ian Linney, Kay Schreiter, Martin Schneider
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Publication number: 20120129849Abstract: The present invention provides deuterated compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The deuterated compounds of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such deuterated compounds as therapeutic agents.Type: ApplicationFiled: September 23, 2011Publication date: May 24, 2012Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Mustapha HADDACH, David M. Ryckman
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Publication number: 20120129868Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: ApplicationFiled: July 29, 2010Publication date: May 24, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Anthony R. Gangloff, Andre A. Kiryanov
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Patent number: 8183250Abstract: The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs.Type: GrantFiled: June 2, 2009Date of Patent: May 22, 2012Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Sheela A. Thomas, Philip J. Hajduk, Daryl R. Sauer, Kathy Sarris, Vincent L. Giranda
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Publication number: 20120122889Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: December 23, 2009Publication date: May 17, 2012Applicant: President and Fellows of Harvard CollegeInventors: Junying Yuan, Emily S. Hsu
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Publication number: 20120108813Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Inventors: Prasada Rao V.S. LINGAM, Sachin Sundarlal CHAUDHARI, Abraham THOMAS, Neelima KHAIRATKAR-JOSHI, Vidya Ganapati KATTIGE
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Publication number: 20120094987Abstract: The invention relates to compounds of general formula (I); 1a, 1b, 1c and 1d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNF?-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.Type: ApplicationFiled: October 3, 2011Publication date: April 19, 2012Inventors: Claudia Reichelt, Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Siegfried Leistner, Andreas Krödel, Jochen Heinicke
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Publication number: 20120085997Abstract: Disclosed is an organic electroluminescent element which is characterized in that constituent layers including at least a phosphorescent light-emitting layer are provided between a pair of electrodes, and at least one of the constituent layers contains a compound represented by general formula (1). (In the formula, A1, A2 and A3 each represents a substituent; n1 and n2 each represents an integer of 0-3; X1 and X2 each represents an oxygen atom, a sulfur atom, an alkylene group, an imino group, a carbonyl group, a sulfoxide group or a sulfonyl group, or alternatively X2 represents a bonding hand; and Z1, Z2, Z3 and Z4 each represents an optionally substituted aromatic heterocyclic ring or an aromatic hydrocarbon ring, provided that all of the Z1, Z2, Z3 and Z4 are not aromatic hydrocarbon rings at the same time.Type: ApplicationFiled: April 28, 2010Publication date: April 12, 2012Applicant: KONICA MINOLTA HOLDINGS, INC.Inventors: Shuichi Sugita, Eisaku Katoh, Motoaki Sugino, Rie Katakura
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Patent number: 8148384Abstract: Compounds of formula I wherein A1, A2, and A3 are as defined herein are inhibitors of PIM kinase. The compounds of formula I are useful for the treatment of diseases such as cancer.Type: GrantFiled: December 6, 2007Date of Patent: April 3, 2012Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Lisa A. Hasvold, Laura A. Hexamer, Vincent L. Giranda, Nan-horng Lin, Zhi-Fu Tao, Le Wang
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Publication number: 20120077978Abstract: A compound is provided having the chemical structure: where R1 is H, CH3, a tert-butyl group, C(?O)-Glu, C(?O)-Asp, C(?O)-Gln, C(?O)-Asn, or R5 is C(?O)-Glu, C(?O)-Asp, C(?O)-Gln, or C(?O)-Asn; R2 comprises an organic chain that is 1 to 5 atoms in length; R3 is a tetrahedral moiety having a central atom and three terminal atoms, wherein the central atom is P, S, V, W, Se, or Te and wherein the terminal atoms are O and/or F; R4 is CH, N, or S; R5 is H, CH3; CH2C6H6, CH2CH2C6H6, OCH2C6H6, C(?O)-Phe, CH2C(?O)-Phe, C(?O)-Tyr, CH2C(?O)-Tyr, or a tert-butyl group; and R6 is H, OH, CH3, CH2OH, or a tert-butyl group.Type: ApplicationFiled: September 28, 2011Publication date: March 29, 2012Applicant: UNIVERSITY OF SOUTH CAROLINAInventors: Lukasz Lebioda, Lesa R. Celeste, Leslie L. Lovelace
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Patent number: 8143248Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: August 1, 2008Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
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Patent number: 8138194Abstract: Fused bicyclic pyrimidine compounds of formula (I): wherein R1, R3, R4, X1, X2, Y, Z, A, B, C, D, n, and the two bonds are defined herein. Also disclosed are a method for inhibiting Aurora kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: April 22, 2009Date of Patent: March 20, 2012Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Su-Ying Wu, Yu-Sheng Chao
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Patent number: 8133996Abstract: The invention relates to a process for the preparation of anagrelide, and for the preparation of intermediates for use in preparing anagrelide. The invention also relates to the intermediates per se, in particular compounds of Formula (V): where R constitutes a suitable leaving group, which may not be hydrogen. The R group may be selected from: (i) —SiR13, (ii) —CH2Ar, (iii) —COOR2, and (iv) sulfonates such as —SO2R3.Type: GrantFiled: February 6, 2008Date of Patent: March 13, 2012Assignee: CIPLA LimitedInventors: Srinivas Laxminarayan Pathi, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
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Patent number: 8134146Abstract: The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof to organic semiconductive materials and to electronic and optoelectronic components.Type: GrantFiled: March 20, 2007Date of Patent: March 13, 2012Assignee: Novaled AGInventors: Michael Limmert, Olaf Zeika, Martin Ammann, Horst Hartmann, Ansgar Werner
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Patent number: 8119647Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: GrantFiled: April 9, 2009Date of Patent: February 21, 2012Assignee: Glenmark Pharmaceuticals S.A.Inventors: Prasada Rao V. S. Lingam, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20120041197Abstract: The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such quinazolines.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Applicant: Novaled AGInventors: Josef Salbeck, Manfred Kussler, Andrea Lux
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Publication number: 20120040966Abstract: The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using percent cell viability as the end point.Type: ApplicationFiled: December 28, 2009Publication date: February 16, 2012Applicant: Southern Research Institute Office of Commercialization and Intellectual PropInventors: Joseph A. Maddry, Bill Severson, Colleen B. Jonsson, James W. Noah, Diana L. Noah, Xi Chen
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Publication number: 20120022045Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, ?3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: January 25, 2010Publication date: January 26, 2012Inventors: Shankar Venkatraman, John S. Wai, Wayne Thompson, Boyoung Kim, Richard C.A. Isaacs, H. Marie Loughran, Dai-Shi Su, John Lim, Mark W. Embrey, Peter D. Williams
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Publication number: 20120022251Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Publication number: 20120012794Abstract: The present invention relates to a compound according to formula: and an organic semiconducting material comprising that compound.Type: ApplicationFiled: December 2, 2009Publication date: January 19, 2012Applicant: NOVALED AGInventor: Omrane Fadhel
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Patent number: 8093246Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: GrantFiled: December 12, 2007Date of Patent: January 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu
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Publication number: 20110319394Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.Type: ApplicationFiled: June 22, 2011Publication date: December 29, 2011Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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Publication number: 20110301168Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: November 5, 2009Publication date: December 8, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong
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Publication number: 20110295002Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: ApplicationFiled: June 2, 2011Publication date: December 1, 2011Inventor: Aleem Gangjee
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Publication number: 20110288108Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: ApplicationFiled: June 2, 2011Publication date: November 24, 2011Inventor: Aleem Gangjee
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Publication number: 20110282056Abstract: Disclosed are compounds according to Formula I: wherein the variables are described herein.Type: ApplicationFiled: January 20, 2009Publication date: November 17, 2011Applicant: MERCK PATENT GMBHInventors: Benny C. Askew, Nadia Brugger, Ruoxi Lan, Amanda E. Sutton
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Patent number: 8053762Abstract: The present invention relates to a novel imidazoquinazoline derivative, a process for preparing the same, and an organic electronic device using the same. The imidazoquinazoline derivative according to the present invention serves as hole injecting, hole transporting, electron injecting, electron transporting, or a light emitting material in an organic electronic device including an organic light emitting device, and the device according to the present invention exhibits excellent characteristics in efficiency, operating voltage, and stability.Type: GrantFiled: December 12, 2006Date of Patent: November 8, 2011Assignee: LG Chem, Ltd.Inventors: Jae-Soon Bae, Dong-Hoon Lee, Dae-Woong Lee, Jun-Gi Jang, Sang-Young Jeon
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Publication number: 20110263850Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases. The process of the invention provides 6,7-dichloro-1,5- dihydroimidazo [2,1 -b] quinazolin 2 (3H)-one, more commonly known as anagrelide and its analogues in a clean and efficient manner.Type: ApplicationFiled: November 30, 2009Publication date: October 27, 2011Applicant: SHIRE LLCInventor: Bernard Golding
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Publication number: 20110263581Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: February 25, 2011Publication date: October 27, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Peter C. CHUA, Fabrice Pierre, Jeffrey P. Whitten
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Patent number: 8030321Abstract: Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: July 2, 2009Date of Patent: October 4, 2011Assignee: Janssen Pharmaceutica, NVInventors: Frank Chavez, Michael P. Curtis, James P. Edwards, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Brad M. Savall
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Patent number: 8026246Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.Type: GrantFiled: November 14, 2007Date of Patent: September 27, 2011Assignee: Millennium Pharmaceuticials, Inc.Inventors: Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
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Patent number: 8022078Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: May 19, 2009Date of Patent: September 20, 2011Assignee: University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
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Publication number: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
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Publication number: 20110224220Abstract: Compounds of formula (I): wherein: Z, R1, R2, R3, n, and m are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: ApplicationFiled: December 15, 2010Publication date: September 15, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Antonio Almario GARCIA, Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
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Patent number: 8017619Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: February 26, 2010Date of Patent: September 13, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
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Publication number: 20110212929Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: ApplicationFiled: March 18, 2011Publication date: September 1, 2011Inventors: Laurence H. Hurley, Daruka Mahadevan, Haiyong Han, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Ruben M. Munoz, Steven L. Warner, Kimiko Della Croce, Daniel D. Von Hoff, Cory L. Grand, James Welsh
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Publication number: 20110207757Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Applicant: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Publication number: 20110190281Abstract: This invention relates to novel sulfone 2I3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis mediated disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: January 13, 2009Publication date: August 4, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Martin Hentemann, William Scott, Jill Wood, Jeffrey Johnson, Aniko Redman, Ann-Marie Bullion, Leatte Guernon
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Publication number: 20110190325Abstract: Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).Type: ApplicationFiled: August 14, 2009Publication date: August 4, 2011Inventors: Gerald B. Hammond, Jose C. Aponte, Robert H. Gilman, Michel Henri Auguste Sauvain, Abraham Caisberg
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Patent number: 7989464Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.Type: GrantFiled: January 21, 2009Date of Patent: August 2, 2011Assignee: Schering CorporationInventors: Julius J. Matasi, Deen Tulshian, Duane A. Burnett, Wen-Lian Wu, Peter Korakas, Lisa S. Silverman, Thavalakulamgara K. Sasikumar, Li Qiang, Martin S. Domalski
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Publication number: 20110182882Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.Type: ApplicationFiled: July 7, 2009Publication date: July 28, 2011Applicant: Beta Pharma, Inc.Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
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Publication number: 20110182812Abstract: Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: February 25, 2011Publication date: July 28, 2011Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Anna Katrin Szardenings, Wei Zhang, Hartmuth C. Kolb, Daniel Kurt Cashion, Gang Chen, Dhanalakshmi Kasi, Changhui Liu, Anjana Sinha, Eric Wang, Chul Yu, Umesh B. Gangadharmath, Joseph C. Walsh
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Publication number: 20110178107Abstract: This invention relates to compounds of Formula (I), (II), or (III) shown in the specification. These compounds can be used to treat hepatitis C virus infection.Type: ApplicationFiled: January 19, 2011Publication date: July 21, 2011Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Ching-Cheng Wang, Chen-Fu Liu, Kuang-Yuan Lee, Mei-Chun Lin, Shu-Huei Wang, Chi-Feng Yen, Yu-Hsuan Wang, Chi-Hsin Richard King