Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., Maytansinoids, Etc.) Patents (Class 514/229.5)
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Patent number: 8598119Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.Type: GrantFiled: May 27, 2009Date of Patent: December 3, 2013Assignee: Intra-Cellular Therapies, Inc.Inventors: Sharon Mates, Allen Fienberg, Lawrence Wennogle
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Patent number: 8598164Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 6, 2011Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Vijayalaksmi Arumugam, Nicole Hilgraf, Jason McCartney, Peter Diederik Jan Grootenhuis, Corey Anderson, Mehdi Numa, Bryan A. Frieman, Brian Richard Bear, James Philip Johnson, Jr.
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Publication number: 20130302416Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.Type: ApplicationFiled: January 19, 2012Publication date: November 14, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
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Patent number: 8557806Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: March 13, 2012Date of Patent: October 15, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
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Patent number: 8546384Abstract: Naphthalimide compounds are used in tissue bonding and protein cross-linking applications. When activated by an activating agent, such as light in the 400-500 nm absorption range, the naphthalimide compounds form chemically-reactive species that cross-link proteins, bond connective tissues together, and bond tissues and other biomaterials together. A naphthalimide-labeled biomolecule, such as a naphthalimide-labeled chitosan, is also capable of bonding tissues without subsequent direct illumination of the contacted tissue area. The naphthalimide compounds may be used in tissue or arterial repair, stabilization of an expanded arterial wall after angioplasty, tethering pharmaceutical agents to tissue surfaces to provide local drug delivery, and for chemically bonding skin care products, sunscreens, and cosmetics to the skin.Type: GrantFiled: July 12, 2012Date of Patent: October 1, 2013Assignee: Alumend, LLCInventors: Ronald E. Utecht, Kaia L. Kloster, Millard M. Judy, Kevin J. Vaska, James L. Matthews
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Patent number: 8546383Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: May 25, 2012Date of Patent: October 1, 2013Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Patent number: 8536168Abstract: The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I:Type: GrantFiled: March 13, 2008Date of Patent: September 17, 2013Assignee: Novartis AGInventors: Miao Dai, Feng He, Rishi Kumar Jain, Rajesh Karki, Joseph Kelleher, III, John Lei, Luis Llamas, Michael A. Mcewan, Karen Miller-Moslin, Lawrence Bias Perez, Stefan Peukert, Naeem Yusuff
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Publication number: 20130225558Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 29, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130217672Abstract: A (+)-3-hydroxymorphinan-based polycycle derivative of formula (I) is effective as a neuroprotective agent for neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and ischemic stroke.Type: ApplicationFiled: May 13, 2011Publication date: August 22, 2013Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Jong Yup Kim, Jeongmin Kim, Kwang Woo Ahn
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Publication number: 20130210803Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 15, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Patent number: 8481529Abstract: Provided is a method for improving treatment of a neoplastic condition by combining a therapeutically effective amount of a polyADP-ribose polymerase inhibitor with a therapeutically effective amount of a compound which triggers the release of nucleolin from the G-quadruplexes in rDNA. As specifically exemplified, the compound which increases nucleolin binding is a substituted quinobenzoxazine analog, for example CX-3543.Type: GrantFiled: May 9, 2007Date of Patent: July 9, 2013Assignee: The Arizona Board of Regents on Behalf of the University of ArizonaInventors: Laurence H. Hurley, Mary Guzman
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Publication number: 20130123248Abstract: Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism.Type: ApplicationFiled: October 17, 2012Publication date: May 16, 2013Applicant: The Regents of the University of CaliforniaInventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
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Publication number: 20130039904Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.Type: ApplicationFiled: August 2, 2010Publication date: February 14, 2013Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.Inventor: Lifeng Xu
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Publication number: 20130029900Abstract: The invention relates to novel cell-binding agent-cytotoxic agent conjugate having a peptide linkers and more specifically to conjugates of formula (I). The invention also provides novel cytotoxic agents of formula (II), linker compounds represented by formula (III), and drug-linker compounds represented by formula (IV). The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.Type: ApplicationFiled: June 21, 2012Publication date: January 31, 2013Applicant: IMMUNOGEN, INC.Inventor: Wayne C. Widdison
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Publication number: 20130005720Abstract: This invention relates to a pharmaceutical composition for treating cancer, comprising an effective amount of a compound represented by formula (I): wherein R is —CCOCCOCC— or —CCOCCOCCOCC—; and a pharmaceutical acceptable carrier. This invention also relates to a method for treating cancer, comprising administering a therapeutically effective amount of said compound to a subject; and a method for stabilizing G4 structure of telomere by using this compound.Type: ApplicationFiled: June 30, 2011Publication date: January 3, 2013Applicant: Academia SinicaInventors: Ta-Chau CHANG, Zi-Fu Wang, Chih-Chien Cho, Wei-Chun Huang, Jen-Fei Chu
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Publication number: 20120329789Abstract: Pharmaceutical compositions for treating Alzheimer's disease are disclosed. The pharmaceutical compositions include a compound having the general formula: and a pharmaceutically acceptable carrier. Methods for treating Alzheimer's disease, inhibiting ATase I and/or ATase 2, reducing the activity of BACE1, reducing the level of amyloid ?-peptide (A?), and/or reducing the level of APP intracellular domain peptide (AICD) by administering such compositions are also disclosed.Type: ApplicationFiled: May 31, 2012Publication date: December 27, 2012Applicant: Wisconsin Alumni Research FoundationInventor: Luigi Puglielli
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Patent number: 8314093Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.Type: GrantFiled: December 18, 2009Date of Patent: November 20, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Jeffrey Wayne Clough, Somasekhar Bhamidipati, Rajinder Singh, Esteban Masuda, Haoran Zhao
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Publication number: 20120288533Abstract: The present invention provides protein (or peptide)-polysaccharide (or oligosaccharide) conjugates (PPC) as nanocapsular vehicles for nanoencapsulation of biologically active compounds, particularly nutraceuticals. The PPCs efficiently protect both hydrophobic (i.e., water insoluble) and hydrophilic (i.e., water soluble) nutraceuticals, to provide a composition which, when added to a beverage, disperses so as to provide a clear or transparent solution. In some embodiments, the PPCs are Maillard reaction based PPCs. Advantageously, the conjugates of the present invention protect the nutraceuticals from degradation, both during shelf life and upon gastric digestion.Type: ApplicationFiled: March 1, 2012Publication date: November 15, 2012Applicant: Technion Research and Development Foundation Ltd.Inventor: Yoav D. Livney
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Publication number: 20120289463Abstract: Compositions for antagonizing phosphorylation and subsequent degradation of glycogen synthase kinase 3 beta (GSK3?) in epidermal cells are disclosed. GSK3? phosphorylation antagonists include molecules that function to inhibit or reduce the binding activity or enzymatic activity of an upstream signaling molecule leading to GSK3? phosphorylation, or by downregulating the expression of one or more upstream signaling molecules involved in regulating GSK3? phosphorylation. Methods of using the GSK3? phosphorylation antagonists to inhibit or reduce the phosphorylation and degradation of GSK3? in epidermal cells are provided. The methods are useful to promote epithelialization and closure of wounds, such as chronic non-healing wounds.Type: ApplicationFiled: December 29, 2010Publication date: November 15, 2012Applicant: New York UniversityInventors: Marjana Tomic-Canic, Harold Brem
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Publication number: 20120283220Abstract: The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.Type: ApplicationFiled: September 22, 2010Publication date: November 8, 2012Inventors: Kuo-Hsiung Lee, Xiaoming Yang, Qian Shi, Kenneth F. Bastow, Che-Ming Teng, Tse-Ming Hong, Pan-Chyr Yang, Shuenn-Chen Yang
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Publication number: 20120276124Abstract: The invention relates to a compound of formula (I): wherein: ALK is a (C1-C6)alkylene group; X1 et X2 are each independently one of the following groups: —CH?CH—, —CO—, —CONR—, —NRCO—, —COO—, —OCO—, —OCONR—, —NRCOO—, —NRCONR?—, —NR—, —S(O)n (n=0, 1 or 2) or —O—; R and R? are independently H or a (C1-C6)alkyl group; i is an integer of from 1 to 40, preferably from 1 to 20, and more preferably from 1 to 10; j is an integer corresponding to 1 when X2 is —CH?CH— and 2 when X2 is not —CH?CH—; Zb is a simple bond, —O— or —NH— and Rb is H or a (C1-C6)alkyl, (C3-C7)cycloalkyl, aryl, heteroaryl or (C3-C7)heterocycloalkyl group; or Zb is a single bond and Rb is Hal.Type: ApplicationFiled: March 29, 2012Publication date: November 1, 2012Applicant: SANOFIInventors: Hervé BOUCHARD, Alain COMMERCON, Claudia FROMOND, Vincent MIKOL, Fabienne PARKER, Ingrid SASSOON, Daniel TAVARES
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Patent number: 8288374Abstract: Provided is a medicinal composition, in particular, a medicinal composition for treatment and/or prevention which has a high therapeutic effect on infection with a parasitic protozoa and a selective toxicity thereto and exhibits a life-prolonging effect and so on. A medicinal composition which contains as the active ingredient a benzo[a]phenoxazine compound represented by General formula (1) or a salt compound of the same, in particular, an agent for treating and/or preventing infection with a protozoa such as malaria, leishmaniasis, African trypanosomiasis, Chagas disease, toxoplasmosis, lymphatic filariasis, babesiosis or coccidium disease; and a novel compound which is contained therein as the active ingredient.Type: GrantFiled: March 11, 2009Date of Patent: October 16, 2012Assignees: Hoshi University, Synstar Japan Co., Ltd., Swiss Tropical and Public Health Institute, FUJIFILM CorporationInventors: Masataka Ihara, Jian-Feng Ge, Chika Arai, Nasser Saad Mohamed Ismail, Mei Yang, Isamu Itoh, Reto Brun
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Publication number: 20120232057Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: September 13, 2012Inventors: George W. GRIESGRABER, Tushar A. KSHIRSAGAR, Azim A. CELEBI, Sarah J. SLANIA, Michael E. DANIELSON, Michael J. RICE, Joshua R. WURST
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Patent number: 8242114Abstract: Naphthalimide compounds are used in tissue bonding and protein cross-linking applications. When activated by an activating agent, such as light in the 400-500 nm absorption range, the naphthalimide compounds form chemically-reactive species that cross-link proteins, bond connective tissues together, and bond tissues and other biomaterials together. A naphthalimide-labeled biomolecule, such as a naphthalimide-labeled chitosan, is also capable of bonding tissues without subsequent direct illumination of the contacted tissue area. The naphthalimide compounds may be used in tissue or arterial repair, stabilization of an expanded arterial wall after angioplasty, tethering pharmaceutical agents to tissue surfaces to provide local drug delivery, and for chemically bonding skin care products, sunscreens, and cosmetics to the skin.Type: GrantFiled: March 19, 2009Date of Patent: August 14, 2012Assignee: Alumend LLCInventors: Ronald E. Utecht, Kaia L. Kloster, Millard M. Judy, Kevin J. Vaska, James L. Matthews
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Publication number: 20120196852Abstract: The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.Type: ApplicationFiled: August 5, 2010Publication date: August 2, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun O. Liu, Omonike Arike Olaleye, Shridhar Bhat
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Publication number: 20120178747Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: July 12, 2012Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
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Patent number: 8207162Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: April 20, 2011Date of Patent: June 26, 2012Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Sarah J. Slania
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Publication number: 20120129775Abstract: Methods of inhibiting undesired angiogenesis are provided, which methods include administering to a subject a therapeutically effective amount of at least one of the compounds described herein, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 30, 2010Publication date: May 24, 2012Inventors: Enrique Zudaire, Marta Aparicio, Frank Cuttitta
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Publication number: 20120122804Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: ApplicationFiled: March 30, 2007Publication date: May 17, 2012Applicant: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terrance Moran
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Publication number: 20120115848Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: October 6, 2011Publication date: May 10, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Robert A. Galemmo, JR., Dean Richard Artis, I, Xiaocong Michael Ye, Danielle L. Aubele, Anh P. Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20120107317Abstract: The subject invention provides novel uses of cytoplasmic c-Myc for modulation of innate immune responses. The invention is based, at least in part, on the surprising discovery that cytoplasmic c-Myc, instead of nuclear c-Myc, modulates pro-inflammatory immune responses via its role as a positive feedback regulator. Specifically, the subject invention provides methods for treatment or amelioration of inflammatory diseases and/or immune disorders via inhibition c-Myc expression or its activity. Also provided are methods for the development of therapeutic agents for treating infection, inflammation, immune diseases and autoimmune diseases.Type: ApplicationFiled: October 26, 2011Publication date: May 3, 2012Applicant: The University of Hong KongInventors: ALLAN SIK YIN LAU, Howard Chi Ho Yim, Chun Bong Li, John Chi Him Pong
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Patent number: 8158621Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: January 21, 2010Date of Patent: April 17, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
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Patent number: 8148368Abstract: Surprising antiviral activity of 7-Nitro-2-(3-nitro phenyl)-4H-3,1-benzoxazin-4-one (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.Type: GrantFiled: September 7, 2010Date of Patent: April 3, 2012Inventors: Shaikh Riazuddin, Atta-ur Rehman, Usman Zafar, Iqbal Choudhary, Usman Ali Ashfaq, Khalid M. Khan, Tayyab Husnain, Zulfiqar Ali Khan, Javed Akram
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Publication number: 20120070409Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: February 3, 2011Publication date: March 22, 2012Applicant: Japan Tobacco Inc.Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
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Patent number: 8138179Abstract: Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R1?, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: GrantFiled: April 12, 2007Date of Patent: March 20, 2012Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Bibia Bennacer, Stefan Stutz
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Patent number: 8129377Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or the like; R3 represents a halogen or the like; q represents an integer of 1 to 7; R4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R5 represents a C6-C10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: September 29, 2005Date of Patent: March 6, 2012Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Kazutoshi Watanabe, Kenji Fukunaga, Toshiyuki Kohara, Fumiaki Uehara, Shinsuke Hiki, Satoshi Yokoshima
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Publication number: 20120046281Abstract: The invention features low-dosage rifalazil compositions and therapeutic regimens which are useful for the treatment of bacterial infections.Type: ApplicationFiled: October 31, 2011Publication date: February 23, 2012Applicant: ACTIVBIOTICS PHARMA, LLC.Inventors: Bernard E. Cabana, Arthur F. Michaelis, Gary P. Magnant, Chalom B. Sayada
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Publication number: 20120040930Abstract: The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.Type: ApplicationFiled: January 13, 2006Publication date: February 16, 2012Inventors: Catherine Guillou, Jean-Yves Lallemand, Thibault Sauvaítre, Jordi Molgo, Denyse Herlem, Daniel Guenard, Françoise Khuong-Huu
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Publication number: 20120004219Abstract: The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: The Governors of the University of AlbertaInventor: John Greer
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Patent number: 8088788Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: March 14, 2007Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Scott E. Langer, Philip D. Heppner
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Publication number: 20110306601Abstract: Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicant: The Regents of the University of CaliforniaInventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
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Publication number: 20110306607Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: May 6, 2011Publication date: December 15, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Vijayalaksmi Arumugam, Nicole Hilgraf, Jason McCartney, Peter Diederik Jan Grootenhuis, Corey Anderson, Mehdi Numa, Bryan A. Frieman, Brian Richard Bear, James Philip Johnson, JR.
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Patent number: 8067410Abstract: The present invention relates to novel phenolic and catecholic amines of Formula I, to processes for their preparation, pharmaceutical compositions containing them, to their use in therapy and to their use in radiolabeled form as PET- or SPECT ligands.Type: GrantFiled: June 24, 2009Date of Patent: November 29, 2011Assignee: H. Lundbeck A/SInventors: Ask Puschl, Morten Jorgensen, Benny Bang-Andersen
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Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel 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: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
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Patent number: 8039466Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3)alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: GrantFiled: November 23, 2007Date of Patent: October 18, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Philippe Panchaud, Jean-Luc Specklin
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Publication number: 20110245224Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: ApplicationFiled: October 13, 2009Publication date: October 6, 2011Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
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Publication number: 20110224201Abstract: Compounds of Formula (I), (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, L, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG, W, Y and Z are as described herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 CGRP receptors are involved.Type: ApplicationFiled: September 29, 2009Publication date: September 15, 2011Inventors: Donnette D. Staas, Ian M. Bell, Harold G. Selnick
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Publication number: 20110218195Abstract: The invention features methods and compostions for treating bacterial infections.Type: ApplicationFiled: August 31, 2010Publication date: September 8, 2011Applicant: ACTIVBIOTICS PHARMA, LLCInventor: Chalom B. Sayada
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Publication number: 20110207725Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: April 20, 2011Publication date: August 25, 2011Inventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sara J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Publication number: 20110207711Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.Type: ApplicationFiled: July 27, 2009Publication date: August 25, 2011Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito