Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/300)
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Patent number: 11484580Abstract: A composition of botulinum toxin is claimed which can penetrate into the ocular surface inclusive of a penetration through a conjunctiva, cornea, and other structures. This composition allows for a maximal penetration of a topical preparation of botulinum toxin which serves to reduce the need for frequent allergy drops for the treatment of ocular surface disease and other conditions causing ocular surface inflammation or deep ocular inflammation. No puncture of the needle is necessary for the administration. Herein describes a novel composition using several principles based on composition, method of application, which enhances the effectiveness of the penetration.Type: GrantFiled: February 26, 2018Date of Patent: November 1, 2022Assignee: Revance Therapeutics, Inc.Inventor: Gary E. Borodic
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Patent number: 10981861Abstract: The present disclosure provides a bromination method for m-diamide compounds comprising reacting a compound represented by formula I with a brominating reagent in the presence of an oxidant to obtain a brominated product represented by formula II. The method adopts a special design of brominating reagents and reaction conditions to introduce a bromine atom at a specific site of the m-diamide compound, with 87.9 to 99.5% yield of a brominated product obtained by the reaction and higher than 91.8% purity. Therefore, the bromination method has a simple route, mild reaction conditions, high efficiency, and does not require complicated and cumbersome post-treatment processes; furthermore, raw materials used for the bromination reaction are readily available, costs of the brominating reagent are low, and the brominated product finally obtained has high yield and high purity, thus the method is a novel one with a broad application prospect.Type: GrantFiled: April 7, 2020Date of Patent: April 20, 2021Assignee: Chang Sha Jia Qiao Biotech CO., LTD.Inventors: Jintao Zhu, Liang Lv, Chaoqun Huang, Liangming Luo, Rong Zhang
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Patent number: 10577308Abstract: The present disclosure relates generally to compounds having activity as voltage-gated sodium channel blockers and their use in the field of therapeutic treatment, including the therapy or management of conditions associated with excessive, unwanted, inadequate or otherwise undesirable sodium ion passage through cellular membranes via voltage-gated sodium channels. In some embodiments, the disclosure relates to aryloxy-substituted amines for use as sodium channel blockers or modulators. Methods for their manufacture and compositions containing the compounds are also disclosed.Type: GrantFiled: March 24, 2016Date of Patent: March 3, 2020Assignees: The Florey Institute, The University of MelbourneInventors: Spencer John Williams, Bevyn Jarrott
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Patent number: 10150759Abstract: The present invention relates to 1,4-pyridone bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: June 16, 2017Date of Patent: December 11, 2018Assignee: Epizyme, Inc.Inventors: Kevin W. Kuntz, John Emmerson Campbell
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Patent number: 9610299Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.Type: GrantFiled: March 16, 2015Date of Patent: April 4, 2017Assignee: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
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Patent number: 9353046Abstract: Provided is a method for producing an aromatic amide derivative represented by Formula (4), the method including a process in which an aromatic amide derivative represented by Formula (1) and a haloalkyl compound represented by Formula (3) are reacted with each other in the presence of a base and a metal or metal salt. In the formulae, each of X and Y represents a hydrogen atom, a halogen atom, or the like. A represents a hydrogen atom, an alkyl group, a group represented by Formula (2), or the like. Each of G1 and G2 represents an oxygen atom or the like. Q1 represents a phenyl group or the like. R1 represents a hydrogen atom, an alkyl group, or the like. Z1 represents a haloalkyl group or the like. Xa represents an iodine atom or the like. m represents a number of from 1 to 4, n1 represents a number from 1 to 5, and n2 represents a number of from 1 to 4.Type: GrantFiled: March 29, 2013Date of Patent: May 31, 2016Assignee: Mitsui Chemicals Agro, Inc.Inventor: Hironari Okura
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Patent number: 9029401Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: GrantFiled: February 14, 2012Date of Patent: May 12, 2015Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Publication number: 20150126591Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of Parkinson's disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be also used for the treatment of Huntington's disease, Alzheimer's disease, Multiple Sclerosis, Lateral Sclerosis, Neural Motor disorders.Type: ApplicationFiled: March 21, 2013Publication date: May 7, 2015Inventor: Mahesh Kandula
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Publication number: 20150126522Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.Type: ApplicationFiled: May 15, 2013Publication date: May 7, 2015Applicant: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Celine Duquenne, Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
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Publication number: 20150111885Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Michael John Bennett, Juan Manuel Betancort, Amogh Boloor, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
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Patent number: 9006242Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: October 15, 2013Date of Patent: April 14, 2015Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki
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Publication number: 20150087639Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.Type: ApplicationFiled: July 18, 2013Publication date: March 26, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
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Publication number: 20150080324Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.Type: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
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Patent number: 8981156Abstract: This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.Type: GrantFiled: May 30, 2011Date of Patent: March 17, 2015Assignee: Piramal Imaging SAInventors: Mathias Berndt, Matthias Friebe, Christina Hultsch, Fabrice Samson, Marianne Patt, Andreas Schildan, Christoph Smuda
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Publication number: 20150072396Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.Type: ApplicationFiled: March 1, 2012Publication date: March 12, 2015Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
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Publication number: 20150065721Abstract: Provided is a method for producing an aromatic amide derivative represented by Formula (4), the method including a process in which an aromatic amide derivative represented by Formula (1) and a haloalkyl compound represented by Formula (3) are reacted with each other in the presence of a base and a metal or metal salt. In the formulae, each of X and Y represents a hydrogen atom, a halogen atom, or the like. A represents a hydrogen atom, an alkyl group, a group represented by Formula (2), or the like. Each of G1 and G2 represents an oxygen atom or the like. Q1 represents a phenyl group or the like. R1 represents a hydrogen atom, an alkyl group, or the like. Z1 represents a haloalkyl group or the like. Xa represents an iodine atom or the like. m represents a number of from 1 to 4, n1 represents a number from 1 to 5, and n2 represents a number of from 1 to 4.Type: ApplicationFiled: March 29, 2013Publication date: March 5, 2015Applicant: Mitsui Chemicals Agro, Inc.Inventor: Hironari Okura
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Publication number: 20150065538Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: November 4, 2014Publication date: March 5, 2015Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
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Patent number: 8968701Abstract: The invention relates to a process for the production of radiotracers. In particular, this invention relates the isolation of radiotracers with containers filled with a stationary phase.Type: GrantFiled: July 6, 2010Date of Patent: March 3, 2015Assignee: Piramal Imaging SAInventors: Holger Siebeneicher, Keith Graham, Mathias Berndt
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Publication number: 20150045367Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: December 19, 2012Publication date: February 12, 2015Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
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Publication number: 20150045548Abstract: The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [18F]fluoride, wherein a [18F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [18F]fluoride or eluting a [18F]fluoride using a [18F]fluoride eluent with an adjusted pH, thereby stably obtaining a [18F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies.Type: ApplicationFiled: December 21, 2012Publication date: February 12, 2015Inventors: Sang Ju Lee, Seung Jun Oh, Dae Hyuk Moon, Jin Sook Ryu, Jae Seung Kim, Jong Jin Lee
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Patent number: 8952169Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: GrantFiled: May 21, 2013Date of Patent: February 10, 2015Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
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Patent number: 8952025Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: GrantFiled: April 2, 2013Date of Patent: February 10, 2015Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on Behalf of Arizona State UniversityInventors: Sidney Hecht, Omar Khdour, Jun Lu, Pablo Arce
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Patent number: 8946434Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: GrantFiled: July 8, 2011Date of Patent: February 3, 2015Assignee: N30 Pharmaceuticals, Inc.Inventors: Xicheng Sun, Jian Qiu
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Patent number: 8940902Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.Type: GrantFiled: July 20, 2012Date of Patent: January 27, 2015Assignee: AbbVie Inc.Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
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Publication number: 20150018341Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
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Publication number: 20150011773Abstract: This invention relates to novel compounds suitable for labeling by 18F and to the corresponding 18F labeled compounds themselves, 19F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by Positron Emission Tomography (PET).Type: ApplicationFiled: April 30, 2012Publication date: January 8, 2015Applicant: PIRAMAL IMAGING SAInventors: Mathias Berndt, Andre Muller, Heribert Schmitt-Willich, Timo Stellfeld, Georg Kettschau, Thomas Brumby, Keith Graham, Lutz Lehmann, Jorma Hassfeld, Martin Kruger
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Publication number: 20150005328Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.Type: ApplicationFiled: July 2, 2014Publication date: January 1, 2015Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
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Publication number: 20140357628Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.Type: ApplicationFiled: June 27, 2014Publication date: December 4, 2014Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
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Publication number: 20140336377Abstract: The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The 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 voltage gated sodium channels are involved.Type: ApplicationFiled: October 18, 2011Publication date: November 13, 2014Applicant: RAQUALIA PHARMA INC.Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Yoshimasa Arano, Mikio Morita
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Publication number: 20140323473Abstract: Organophosphate (OP) nerve agents and pesticides are potent inhibitors of acetylcholinesterase (AChE). Though oxime nucleophiles can reactivate an AChE-phosphyl adduct, the adduct can undergo a reaction called aging, leading to an aged-AChE adduct. The invention provides compounds and methods that can be used to reactivate an aged-AChE adduct. Such compounds and methods are useful to counteract organophosphorus poisoning.Type: ApplicationFiled: January 24, 2014Publication date: October 30, 2014Applicant: University of Iowa Research FoundationInventors: Daniel Quinn, Joseph John Topczewski
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Publication number: 20140323461Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.Type: ApplicationFiled: November 9, 2012Publication date: October 30, 2014Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
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Publication number: 20140315913Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.Type: ApplicationFiled: March 11, 2014Publication date: October 23, 2014Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
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Patent number: 8865908Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)Type: GrantFiled: July 30, 2010Date of Patent: October 21, 2014Assignee: Bayer Cropscience AGInventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
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Publication number: 20140303377Abstract: An object of the present invention is to provide insecticides having high effectiveness.Type: ApplicationFiled: June 24, 2014Publication date: October 9, 2014Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba, Atsuko Kawahara
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Publication number: 20140296303Abstract: Methods for treating and/or preventing at least one symptom of a disorder associated with oxidative stress, carbonyl stress, or combinations thereof in a subject. In some embodiments, the methods include administering to the subject an effective amount of pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods for treating or preventing a nephropathy, acute renal injury, acute renal failure, or combinations thereof in a subject, and formulations adapted for intravenous administration comprising pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing.Type: ApplicationFiled: June 12, 2014Publication date: October 2, 2014Inventors: Billy G. Hudson, Paul Vosiyan, Alp Ikizler
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Publication number: 20140288041Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: May 12, 2014Publication date: September 25, 2014Applicant: EPIZYME, INC.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
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Patent number: 8840866Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.Type: GrantFiled: January 7, 2013Date of Patent: September 23, 2014Assignee: The Trustees of the University of PennsylvaniaInventors: Hank F. Kung, Mei-Ping Kung
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Publication number: 20140275526Abstract: This disclosure relates to compounds containing a fluorophore covalently bonded to at least one protected sulfonate group of formula (I): in which X and R2-R5 are defined in the specification. This disclosure also relates to use of these compounds as dyes in an imaging methods, as well as intermediates that can be used to prepare these compounds.Type: ApplicationFiled: March 10, 2014Publication date: September 18, 2014Applicant: University of MassachusettsInventors: Stephen C. Miller, Steven M. Pauff, Adam Choi
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Publication number: 20140256748Abstract: 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaph-thalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels.Type: ApplicationFiled: October 2, 2012Publication date: September 11, 2014Inventors: Li-Tain Yeh, Barry D. Quart
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Publication number: 20140243362Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.Type: ApplicationFiled: September 25, 2012Publication date: August 28, 2014Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
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Publication number: 20140243533Abstract: This invention relates to improved methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.Type: ApplicationFiled: October 18, 2012Publication date: August 28, 2014Applicant: PIRAMAL IMAGING SAInventors: Franz Meier, Keith Graham
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Publication number: 20140243335Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
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Patent number: 8815917Abstract: Described herein is the DP2 antagonist [2?-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4?-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.Type: GrantFiled: July 29, 2010Date of Patent: August 26, 2014Assignee: Panmira Pharmaceuticals, LLCInventors: Jason Edward Brittain, Brian Andrew Stearns, Christopher David King, Kevin Ross Holme
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Publication number: 20140235637Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: InterMune, Inc.Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
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Patent number: 8802860Abstract: The present invention relates to a process for the preparation of substituted 3-(2-hydroxyethyl)-1-[4-nitrophenyl]pyridin-2(1H)-ones which serve as important intermediate compounds for producing drugs.Type: GrantFiled: April 26, 2011Date of Patent: August 12, 2014Assignee: Bayer Intellectual Property GmbHInventors: Joachim Krüger, Danja Groβbach, Holger Paulsen, Walter Kroh
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Patent number: 8791268Abstract: Vanilloid receptor ligand compounds corresponding to formula I: a process for producing such compounds, pharmaceutical compositions containing them, and the use of such compounds to treat pain and various other vanilloid receptor mediated conditions.Type: GrantFiled: March 31, 2011Date of Patent: July 29, 2014Assignee: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Michael Przewosny, Bernd Sundermann, Jeewoo Lee
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Patent number: 8791147Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.Type: GrantFiled: October 7, 2009Date of Patent: July 29, 2014Assignee: Amgen Inc.Inventors: Christopher Fotsch, Paul Harrington
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Patent number: 8779197Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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: October 10, 2008Date of Patent: July 15, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
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Patent number: 8771641Abstract: The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.Type: GrantFiled: December 16, 2010Date of Patent: July 8, 2014Assignee: GE Healthcare LimitedInventors: Harry John Wadsworth, Dennis O'Shea
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Publication number: 20140187539Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: ApplicationFiled: March 4, 2014Publication date: July 3, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger WAGNER, Elke LANGKOPF, Frank HIMMELSBACH, Rolf GOEGGEL, Birgit JUNG