Boron Containing Doai Patents (Class 514/64)
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Patent number: 8461135Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: GrantFiled: September 19, 2011Date of Patent: June 11, 2013Assignee: Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert T. Jacobs, Daitao Chen, Michael Richard Kevin Alley
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Patent number: 8461364Abstract: This invention provides, among other things, polymorphs of the hydrochloride salt of (S)-3-aminomethyl-7-(3-hydroxy-propoxy)-3H-benzo[c][1,2]oxaborol-1-ol.Type: GrantFiled: December 17, 2009Date of Patent: June 11, 2013Assignees: GlaxoSmithKline LLC, Anacor Pharmaceuticals, Inc.Inventors: Conrad Wheeler, Dan Todd, Pingyun Chen, Beth A. Norton
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Publication number: 20130136794Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.Type: ApplicationFiled: April 21, 2011Publication date: May 30, 2013Applicant: PEKING UNIVERSITYInventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
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Publication number: 20130137629Abstract: Various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis can be treated with a compound selected from an incretin mimetic and a dipeptidyl peptidase IV inhibitor in combination with a Compound of Formula I or a pharmaceutically acceptable salt thereof Three of R1, R2, R3, R4 and R5 are hydrogen and the remainder are independently selected from the group consisting of hydrogen, halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; and m is 0, 2 or 4. R6 is hydrogen, O or hydroxy, and X is —OR7, wherein R7 is hydrogen or alkyl having from 1 to 3 carbon atoms; or R6 is hydrogen, and X is —NR8R9, wherein R8 is hydrogen or hydroxy and R9 is hydrogen, methyl or ethyl. When X is —NR8R9, hydroxy none of R1, R2, R3, R4 and R5 is hydroxy.Type: ApplicationFiled: January 24, 2013Publication date: May 30, 2013Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventor: WELLSTAT THERAPEUTICS CORPORATION
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Patent number: 8450301Abstract: The invention relates to the use of piperazine compounds of formula (I) or the agriculturally useful salts of piperazine compounds of formula (I) as herbicides, the variables in formula (I) being defined as cited in the claims and the description.Type: GrantFiled: December 29, 2006Date of Patent: May 28, 2013Assignee: BASF SEInventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kühn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Puhl, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt, Michael Rack
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Publication number: 20130131017Abstract: This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds.Type: ApplicationFiled: November 16, 2012Publication date: May 23, 2013Applicants: Anacor Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: Eli Lilly and Company, Anacor Pharmaceuticals, Inc.
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Publication number: 20130131016Abstract: This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds.Type: ApplicationFiled: November 16, 2012Publication date: May 23, 2013Applicants: Anacor Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: Eli Lilly and Company, Anacor Pharmaceuticals, Inc.
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Patent number: 8440642Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: GrantFiled: September 1, 2011Date of Patent: May 14, 2013Assignee: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
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Patent number: 8435968Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).Type: GrantFiled: September 18, 2009Date of Patent: May 7, 2013Assignee: PIMCO 2664 LimitedInventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
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Publication number: 20130108583Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:Type: ApplicationFiled: May 18, 2012Publication date: May 2, 2013Inventors: Alfredo C. Castro, Michael J. Grogan, William Matsui, Karen J. McGovern, Martin R. Tremblay
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Publication number: 20130108582Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:Type: ApplicationFiled: May 18, 2012Publication date: May 2, 2013Inventors: Alfredo C. Castro, Michael J. Grogan, William Matsui, Karen J. McGovern, Martin R. Tremblay
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Patent number: 8426387Abstract: Phenyl boric acid and its salts and substituent derivatives (e.g., substituted phenyl) effectively inhibit the growth of several cancer cell lines and offers utility in the treatment/prevention of cancer. The material may be applied or injected into affected areas or applied topically, especially for the treatment of cervical cancer.Type: GrantFiled: March 30, 2007Date of Patent: April 23, 2013Inventors: Stephen Carper, Susan Meacham
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Publication number: 20130096053Abstract: The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified ?-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties.Type: ApplicationFiled: June 24, 2011Publication date: April 18, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: Susan K. Heimbecher, David Monteith
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Publication number: 20130095100Abstract: This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by the inhibition of kinases including Src-kinase and Bcr-Abl kinase.Type: ApplicationFiled: December 6, 2012Publication date: April 18, 2013Applicant: Concert Pharmaceuticals, Inc.Inventor: Concert Pharmaceuticals, Inc.
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Publication number: 20130096068Abstract: A combination therapy is disclosed for treating cancer. The method comprises identifying a patient diagnosed of cancer and in need of treatment, administering to a cancer patient a therapeutically effective amount of a compound of Formula (I), and administering to said patient a therapeutically effective amount of a proteasome inhibitor.Type: ApplicationFiled: October 19, 2012Publication date: April 18, 2013Applicant: Niiki Pharma Inc.Inventor: Niiki Pharma Inc.
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Publication number: 20130096086Abstract: Methods described herein relate to mitochondria and their role in Human immunodeficiency virus type 1 (HIV-1) infection and cell-to-cell HIV-1 transmission and compositions and methods for modulating mitochondrial mediated cell-to-cell transmission of HIV-1. Methods for screening to identify inhibitors of mitochondrial mediated cell-to-cell transmission of HIV-1 are also envisioned herein.Type: ApplicationFiled: October 17, 2012Publication date: April 18, 2013Inventor: Sylvia Lee-Huang
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Publication number: 20130096085Abstract: Prochelator compounds of Formula (I) or Formula (II) are described, along with methods of using the same and pharmaceutical formulations or compositions containing the same.Type: ApplicationFiled: July 22, 2010Publication date: April 18, 2013Inventors: Katherine J. Franz, Marina G. D, Leed
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Publication number: 20130090309Abstract: The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: April 30, 2012Publication date: April 11, 2013Inventors: Eric Thomas Romeo, Michelle R. Machacek, Benjamin Wesley Trotter, Thomas Allen Miller, Brian Michael Andresen, Neville John Anthony, Brandon M. Taoka, Yuan Liu
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Patent number: 8415295Abstract: Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH3)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.Type: GrantFiled: January 22, 2010Date of Patent: April 9, 2013Assignee: Phenomix CorporationInventors: David Alan Campbell, David T. Winn, Juan Manuel Betancort
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Patent number: 8415327Abstract: Methods and compositions involving a class of boron-protected phenylphosphine agents having increased cell permeability and having improved chemical stability for treating or for preventing cell death-related diseases or conditions in a human or a non-human animal.Type: GrantFiled: February 22, 2010Date of Patent: April 9, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Leonard A. Levin, Yun Luo
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Patent number: 8415483Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: GrantFiled: December 20, 2011Date of Patent: April 9, 2013Assignee: AstraZeneca ABInventors: Gabor Csjernyik, Sofia Karlström, Annika Kers, Karin Kolmodin, Martin Nylöf, Liselotte Öhberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Söderman, Britt-Marie Swahn, Stefan Von Berg
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Patent number: 8415328Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.Type: GrantFiled: May 3, 2011Date of Patent: April 9, 2013Assignee: Pharmacyclics, IncInventors: Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader, Kieron Wesson
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Publication number: 20130084346Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: April 4, 2013Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
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Publication number: 20130079306Abstract: A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.Type: ApplicationFiled: July 1, 2011Publication date: March 28, 2013Inventors: Hiroshi Uchida, Akira Asagarasu, Teruaki Matsui
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Publication number: 20130079304Abstract: Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance.Type: ApplicationFiled: November 20, 2012Publication date: March 28, 2013Applicant: Novartis AGInventor: Novartis AG
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Publication number: 20130079305Abstract: 3-substituted vinylboronates and their use in the treatment of cancer such as colorectal cancer are disclosed. In some embodiments, the 3-substituted vinylboronates have the general Formula I: with the variables in the formula being as defined in the specification.Type: ApplicationFiled: May 31, 2011Publication date: March 28, 2013Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Morris Srebnik, Abed Al-Aziz Quntar, Alina Botvinik, Arie Dagan
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Publication number: 20130079303Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: November 19, 2012Publication date: March 28, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
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Publication number: 20130071323Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administering a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient; and administering at least one additional therapeutic agent.Type: ApplicationFiled: March 9, 2012Publication date: March 21, 2013Applicant: Gilead Calistoga LLCInventors: W. Michael Gallatin, Roger G. Ulrich, Neill A. Giese, Brian Lannutti, Langdon Miller, Thomas M. Jahn
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Publication number: 20130066264Abstract: Disclosed are a sugar-responsive gel and a medicine administering device having a pKa more suitable for use in a body environment and capable of administering medicine more autonomously than before. A sugar-responsive gel and an insulin administering device having a pKa more suitable for use in a body environment and capable of administering insulin more autonomously than before, wherein under a body condition of pKa of 7.4 or less and temperature of 35° C.-40° C., when the glucose concentration increases, insulin can be released from a gel body in response thereto, and when the glucose concentration decreases, insulin release from the gel body can be suppressed.Type: ApplicationFiled: May 24, 2011Publication date: March 14, 2013Applicant: NATIONAL INSTITUTE FOR MATERIALS SCIENCEInventors: Akira Matsumoto, Takehiko Ishii, Kazunori Kataoka, Yuji Miyahara
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Publication number: 20130059802Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: ApplicationFiled: September 7, 2012Publication date: March 7, 2013Applicant: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Michael Richard Kevin Alley, Stephen J. Benkovic, Michael DiPierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk R. Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zagar, Yong-Kang Zhang, Huchen Zhou
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Publication number: 20130059819Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.Type: ApplicationFiled: October 26, 2012Publication date: March 7, 2013Applicant: INFINITY PHARMACEUTICALS, INC.Inventor: INFINITY PHARMACEUTICALS, INC.
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Publication number: 20130059803Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: ApplicationFiled: September 7, 2012Publication date: March 7, 2013Applicant: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Michael Richard Kevin Alley, Stephen J. Benkovic, Michael DiPierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk R. Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zagar, Yong-Kang Zhang, Huchen Zhou
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Publication number: 20130053343Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.Type: ApplicationFiled: November 2, 2010Publication date: February 28, 2013Applicant: The Trustees of Columbia University in th City ofInventors: Donald Landry, Shi-Xian Deng
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Publication number: 20130052189Abstract: The present invention relates, in general, to a method of treating patients undergoing enzyme replacement therapy (ERT) or other therapy involving the administration of a proteinaceous therapeutic agent as well gene replacement therapy with non-viral or viral vectors, or other therapeutic modality or modalities, used alone or in combination, which involve the administration of exogenous substances for potential therapeutic benefit, including, but not limited to DNA vaccines, siRNA, splice-site switching oligomers (SSOs) as well as RNA-based nanoparticles (RNPs) and nanovaccines. The invention further relates to compounds and compositions suitable for use in such methods.Type: ApplicationFiled: May 6, 2011Publication date: February 28, 2013Inventors: Priya S. Kishnani, Suhrad G. Banugaria, Dwight D. Koeberl, Sean N. Prater
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Publication number: 20130045203Abstract: This disclosure relates to methods of treating or preventing cancer comprising administering a pharmaceutical composition comprising noscapine or noscapine derivatives to a subject diagnosed with a mutated adenomatous polyposis coli (APC) gene.Type: ApplicationFiled: February 25, 2011Publication date: February 21, 2013Applicant: EMORY UNIVERSITYInventors: Harish C. Joshi, Vincent Yang
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Publication number: 20130045949Abstract: Described herein are compounds that may be selectively activated to produce active anti-cancer agents in tumor cells. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds.Type: ApplicationFiled: July 1, 2012Publication date: February 21, 2013Applicant: UWM RESEARCH FOUNDATION, INC.Inventors: Xiaohua Peng, Yunyan Kuang, Sheng Cao, Wenbing Chen, Yibin Wang
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Publication number: 20130045264Abstract: There is provided an antifouling coating composition capable of forming an antifouling coating film which has stable coating film consumption degree on ships, underwater structures and the like and which exhibits excellent antifouling property over a long term. The antifouling coating composition includes a hydrolyzable copolymer (A) and an antifouling agent (B), wherein the hydrolyzable copolymer (A) is, e.g., a metal salt bond-containing copolymer having a component unit derived from a monomer (a21) represented by the general formula (II): CH2?C(R2)—COO-M-O—CO—C(R2)?CH2??(II) [In the formula (II), M is zinc or copper, and R2 is a hydrogen atom or a methyl group], and a component unit derived from other unsaturated monomer (a22) copolymerizable with the monomer (a21), and wherein the antifouling agent (B) includes at least medetomidine.Type: ApplicationFiled: March 18, 2011Publication date: February 21, 2013Applicant: CHUGOKU MARINE PAINTS, LTD.Inventors: Satoshi Masuda, Yusuke Hayashi, Yukio Kozono
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Patent number: 8378099Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.Type: GrantFiled: August 19, 2011Date of Patent: February 19, 2013Assignee: Millennium Pharmacueticals, Inc.Inventors: Julian Adams, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
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Publication number: 20130039906Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. 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: August 10, 2012Publication date: February 14, 2013Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
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Publication number: 20130040912Abstract: The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl-sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: UNIVERSITY OF BASELInventors: Vladimir Cmiljanovic, Natasa Cmiljanovic, Bernd Giese, Matthias Wymann
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Publication number: 20130035312Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: October 11, 2012Publication date: February 7, 2013Applicants: Axys Pharmaceuticals, Inc., Merck, Sharp & Dohme, Corp.Inventors: Merck, Sharp & Dohme, Corp., Axys Pharmaceuticals, Inc.
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Publication number: 20130035311Abstract: The present invention provides compounds of Formula I along with compositions containing the same and methods of use thereof in treating oxidative stress.Type: ApplicationFiled: August 1, 2012Publication date: February 7, 2013Inventors: Katherine J. Franz, Filip Kielar
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Publication number: 20130029927Abstract: The invention relates to a combination comprising the N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Inventors: Peter Wisdom Atadja, Wenlin Shao, Kapil N. Bhalla
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Publication number: 20130029928Abstract: There is provided compositions comprising perfluorooctanoic acid (PFOA) or a salt, derivative or variant thereof. There is also provided uses, methods therapeutic systems and combination therapies relating to PFOA.Type: ApplicationFiled: February 18, 2011Publication date: January 31, 2013Inventors: Clifford Roy Elcombe, Charles Roland Wolf, Anna Louise Westwood
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Patent number: 8362033Abstract: Disclosed is a novel composition and method for chemotherapy in leukemia. Activation of the calcium ion channel by tipifarnib increases intracellular calcium and triggers cell death in leukemia cell lines. Increasing the activity of this channel with 2-aminoethoxydiphenyl borate (2-APB) enhances both the intracellular calcium elevations and cell death, whereas decreasing the activity of the channel with gadolinium or lanthanum blocks the calcium increases and promotes cell survival. The protein target was able to overcome cell adhesion-mediated drug resistance, which often limits the usefulness of other targets. This protein is expressed in other immortalized cell lines, but has limited expression in normal native cell types in humans. Such limited expression would reduce the likelihood of adverse side effects associated with the targeting of this protein.Type: GrantFiled: September 4, 2009Date of Patent: January 29, 2013Assignee: University of South FloridaInventor: Javier Cuevas
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Publication number: 20130023494Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 5, 2011Publication date: January 24, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Sangdon Han, Daniel J. Buzard, Juerg Lehmann, Sanju Narayanan, Dawei Yue
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Publication number: 20130011459Abstract: A composite material formulated for slow release of a small molecule in seawater includes a porous inorganic oxide framework and micelles embedded within the pores of the framework. The micelles include a surfactant and a small molecule, the surfactant being present in the composite material at no more than 80 parts by weight per 100 parts by weight inorganic oxide, the composite material being stable in seawater for releasing the small molecule over at least 20 days.Type: ApplicationFiled: September 12, 2012Publication date: January 10, 2013Applicant: Naval Research LaboratoryInventors: Brian Melde, Michael A. Markowitz
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Patent number: 8349814Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.Type: GrantFiled: March 16, 2011Date of Patent: January 8, 2013Assignee: Infinity Pharmaceuticals, Inc.Inventors: Julian Adams, Mark L. Behnke, Alfredo C. Castro, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Tao Liu, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 8343944Abstract: This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.Type: GrantFiled: July 27, 2010Date of Patent: January 1, 2013Assignee: Anacor Pharmaceuticals, Inc.Inventors: Yi Xia, Michael Richard Kevin Alley, Yasheen Zhou, Rajeshwar Singh, Charles Ding, Kathy Cao, Jacob J. Plattner, Ligong Ou, Guofeng Jia, Neerja Saraswat, Sreekanth Ramachandran, Ding Zhou
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Publication number: 20120328610Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: November 17, 2010Publication date: December 27, 2012Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Ulf Bömer