Hetero Ring Is Six-membered And Includes At Least Nitrogen And Oxygen As Ring Hetero Atoms (e.g., Monocyclic 1,2- And 1,3-oxazines, Etc.) Patents (Class 514/228.8)
  • Patent number: 10213419
    Abstract: The present disclosure relates to compositions comprising impurities (e.g., carbamate and/or hydrolysis products) in a lomitapide sample and methods of detecting such impurities.
    Type: Grant
    Filed: May 2, 2016
    Date of Patent: February 26, 2019
    Assignee: Aegerion Pharmaceuticals, Inc.
    Inventor: Ann Gelormini
  • Patent number: 10207995
    Abstract: Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: February 19, 2019
    Assignee: Monsanto Technology LLC
    Inventors: Urszula Slomczynska, Matthew W. Dimmic, William P. Haakenson, Jr., Jennifer L. Bennett, Barry J. Shortt, Christina M. Taylor, Deryck Jeremy Williams
  • Patent number: 10017504
    Abstract: The present invention is directed to piperidine isoxazole and isothiazole orexin compounds which are antagonists of orexin receptors. Such compounds are of the general structural formula I: wherein the variables are defined herein. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: July 10, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel Liverton, Scott D. Kuduk, Douglas Beshore, Yunfu Luo, Na Meng, Tingting Yu
  • Patent number: 9861596
    Abstract: Provided are compounds for the treatment of neurological diseases or injuries, including neurodegenerative diseases, stroke, trauma, epilepsy, acute and chronic kidney injuries, diabetes mellitus, and/or seizures. In some embodiments, derivatives of vitamin K are provided.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: January 9, 2018
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: C. James Chou, Sherine S. Chan, Jennifer J. Rahn, Benjamin J. Josey
  • Patent number: 9758514
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: September 12, 2017
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop K. Vakkalanka
  • Patent number: 9650339
    Abstract: Compounds of the form In which Q is selected from —CH?NR12, —W, —CH2NHR13, —CH?O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
    Type: Grant
    Filed: February 26, 2014
    Date of Patent: May 16, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Marc Labelle, Thomas Boesen, Qasim Khan, Ramkrishna Reddy Vakiti, Utpal Sharma, Ying Yang, Mukund Mehrotra, Neerja Saraswat, Farman Ullah
  • Patent number: 9457031
    Abstract: Methods of treating bacterial infection by in a subject by administering a pharmaceutical composition including a celecoxib derivative are described. The compounds are particularly useful for treating infection by bacteria capable of growing inside macrophages, such as Myocobacteria tuberculosis.
    Type: Grant
    Filed: July 30, 2013
    Date of Patent: October 4, 2016
    Inventors: Ching-Shih Chen, Santosh Salunke, Larry Schlesinger, Abul K. Azad
  • Patent number: 9296734
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of R1 and R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: March 29, 2016
    Assignee: Amgen Inc.
    Inventors: Ana Elena Minatti, Jonathan D. Low, Jennifer R. Allen, Jian Chen, Ning Chen, Yuan Cheng, Ted Judd, Qingyian Liu, Patricia Lopez, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Nuria A. Tamayo, Qiufen Xue, Bryant Yang, Wenge Zhong
  • Patent number: 9221801
    Abstract: Compounds of the form In which Q is selected from —CH?NR12, —W, —CH2NHR13, —CH?O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: December 29, 2015
    Assignee: Epitherapeutics APS
    Inventors: Marc Labelle, Thomas Boesen, Qasim Khan, Ramkrishna Reddy Vakiti, Utpal Sharma, Ying Yang, Mukund Mehrotra, Neerja Saraswat, Farman Ullah
  • Patent number: 9163011
    Abstract: The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: October 20, 2015
    Assignee: NOVARTIS AG
    Inventors: Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Siem Jacob Veenstra
  • Patent number: 9115098
    Abstract: The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: August 25, 2015
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Hans Hilpert, Wolfgang Wostl
  • Patent number: 9079919
    Abstract: The present invention provides spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: July 14, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Robert Narquizian, Emmanuel Pinard, Wolfgang Wostl
  • Patent number: 9073909
    Abstract: The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes. The invention further provides a radio-labelled derivative thereof.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: July 7, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Edilio Boroni, Luca Gobbi, Hans Hilpert, Michael Honer, Dieter Murl, Robert Narquizian, Alessandra Polara
  • Patent number: 9067926
    Abstract: Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatement of, for example, Alzheimer's Disease.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: June 30, 2015
    Assignees: HOFFMANN-LA ROCHE INC., SIENA BIOTECH S.P.A.
    Inventors: Hans Hilpert, Roland Humm, Thomas Woltering
  • Publication number: 20150119375
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Pierre-Yves Coqueron, Mazen Es-Sayed, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Stephane Brunet, Helene Lachaise, Jean-Pierre Vors
  • Publication number: 20150111883
    Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).
    Type: Application
    Filed: October 21, 2014
    Publication date: April 23, 2015
    Inventors: Jaekyoo Lee, Jang-Sik Choi, Hae-Jun Hwang, Ho-Juhn Song, Jung-Ho Kim, Se-Won Kim, Jong Sung Koh, Jaesang Lee, Tae-Im Lee, Yung-Geun Choi, Sung-Ho Park, In Yong Lee, Byung-Chul Suh, Paresh Devidas Salgaonkar, Dong-Sik Jung
  • Patent number: 9012446
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: April 21, 2015
    Assignee: Amgen Inc.
    Inventors: Jian Chen, Wenge Zhong, Patricia Lopez, Ryan White, Matthew Weiss, Ted Judd, Timothy Powers, Yuan Cheng, Thomas Dineen, Jonathan D. Low, Isaac E. Marx, Ana Elena Minatti
  • Patent number: 8999980
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-? proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4a, R4b, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: April 7, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Moriyasu Masui, Akihiro Hori
  • Publication number: 20150094306
    Abstract: The present invention relates to pyrrolopyridinone 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: Application
    Filed: April 25, 2013
    Publication date: April 2, 2015
    Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
  • Patent number: 8987242
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: March 24, 2015
    Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceuticals Co., Ltd.
    Inventors: Samuel Chackalamannil, Tin-Yau Chan, Mariappan V. Chelliah, Martin C. Clasby, Michael Dwyer, William J. Greenlee, Tomokazu Hirabayashi, Santhosh Neelamkavil, Hidemitsu Nishida, Fumihiko Saitoh, Unmesh Shah, Yan Xia
  • Patent number: 8987255
    Abstract: The present invention provides compounds of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: March 24, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Thomas Woltering
  • Publication number: 20150080363
    Abstract: The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Application
    Filed: September 26, 2014
    Publication date: March 19, 2015
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Patent number: 8980884
    Abstract: 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: Grant
    Filed: May 31, 2012
    Date of Patent: March 17, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Luigi Puglielli
  • Patent number: 8969338
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20150057269
    Abstract: The present invention regards compositions and methods for the modulation of amidases capable of hydrolysing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH?CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.
    Type: Application
    Filed: February 17, 2012
    Publication date: February 26, 2015
    Applicant: Epitech Group S.r.l.
    Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Vincenzo Di Marzo, Salvatore Cuzzocrea
  • Publication number: 20150057262
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Patent number: 8952010
    Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom Ar1 represents a bicyclic heterocyclic group represented by the following formula: ?and Ar2 represents a bicyclic heterocyclic group represented by the following formulae:
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: February 10, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hiroaki Inagaki, Tetsunori Fujisawa, Masao Itoh, Aki Yokomizo, Toshifumi Tsuda, Saito Higuchi, Biswajit Das, Rita Katoch, Dilip J. Upadhyay
  • Publication number: 20150031690
    Abstract: The present invention provides a compound of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: January 23, 2013
    Publication date: January 29, 2015
    Applicants: F. Hoffmann-La Roche AG, Siena Biotech S.P.A
    Inventors: Hans Hilpert, Roland Humm, Thomas Woltering
  • Publication number: 20150025058
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
  • Publication number: 20150018338
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: July 7, 2014
    Publication date: January 15, 2015
    Applicant: NOVARTIS AG
    Inventors: Sangamesh BADIGER, Murali CHEBROLU, Mathias FREDERIKSEN, Philipp HOLZER, Konstanze HURTH, Rainer Martin LEUOEND, Rainer MACHAUER, Henrik MOEBITZ, Ulf NEUMANN, Rita RAMOS, Henrich RUEEGER, Michael SCHAEFER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
  • Publication number: 20150018347
    Abstract: The present application describes modulators of chemokine receptor activity of formula I or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Application
    Filed: October 1, 2014
    Publication date: January 15, 2015
    Inventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
  • Patent number: 8933072
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: January 13, 2015
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer-Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Patent number: 8927539
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Katerina Leftheris, Linghang Zhuang, Colin M. Tice, Suresh B. Singh, Yuanjie Ye
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Patent number: 8927540
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4?, have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: January 6, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Patent number: 8920793
    Abstract: The present invention relates to the preparation of poly(amino oxalate) (PAOX) using oxalyl chloride, 1,4-cyclohexanedimethanol, and piperazinediethanol, the preparation of biodegradable polymer particles using the PAOX, and the use of PAOX particles as a drug delivery vehicle. The PAOX according to the present invention is a polymer that has three characteristics of biodegradability, biocompatibility, and cationic properties at the same time with appropriate hydrophobicity and thus can be prepared as particles that allow rapid drug release. Moreover, the particles improve the delivery efficiency of a drug into cells and thus can be efficiently used as a drug delivery vehicle for the treatment of acute inflammatory diseases such as acute liver failure and acute lung injury.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: December 30, 2014
    Assignee: Industrial Cooperation Foundation Chonbuk National University
    Inventors: Dong Won Lee, Kyeong Yeol Seong, Han Sol Seo, Hyung Min Kim, Ye Rang Kim
  • Publication number: 20140371214
    Abstract: Compounds of the form In which Q is selected from —CH?NR12, —W, —CH2NHR13, —CH?O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Marc Labelle, Thomas Boesen, Qasim Khan, Ramkrishna Reddy Vakiti, Utpal Sharma, Ying Yang, Mukund Mehrotra, Neerja Saraswat, Farman Ullah
  • Publication number: 20140364428
    Abstract: The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Application
    Filed: December 4, 2012
    Publication date: December 11, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Henricus Jacobus Maria Gijsen, Sven Franciscus Anna Van Brandt
  • Patent number: 8906907
    Abstract: New compositions for and methods of treating ocular hypertension provide for effective treatment of ocular hypertension often using reduced concentrations of active components. Such compositions include a timolol component and a hypotensive lipid component. The present compositions and methods are relatively straightforward, can be easily produced, for example, using conventional manufacturing techniques, and can be easily and conveniently practiced, for example, using application or administration techniques or methodologies which are substantially similar to those employed with prior compositions used to treat ocular hypertension.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: December 9, 2014
    Assignee: Allergan, Inc.
    Inventors: June Chen, David F. Woodward, Alexander B. Kharlamb
  • Patent number: 8906852
    Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: December 9, 2014
    Assignee: MethylGene Inc.
    Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frédéric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Patent number: 8901115
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Patent number: 8895548
    Abstract: A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.
    Type: Grant
    Filed: November 1, 2013
    Date of Patent: November 25, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuuji Kooriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Publication number: 20140343048
    Abstract: The invention relates to novel 6-difluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Application
    Filed: December 4, 2012
    Publication date: November 20, 2014
    Inventors: Andrés Avelino Trabanco-Suárez, Henricus Jacobus Maria Gijsen, Michel Surkyn, Hana Prokopcová
  • Publication number: 20140336173
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(?O)—NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR2R10, —C(?O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 10, 2012
    Publication date: November 13, 2014
    Inventors: Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer
  • Publication number: 20140336158
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Patent number: 8883779
    Abstract: The present invention provides a compound of formula (I): wherein —X? is —CR7? or —N?, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: November 11, 2014
    Assignee: Shinogi & Co., Ltd.
    Inventors: Moriyasu Masui, Yasunori Mitsuoka, Syuhei Yoshida, Ken-ichi Kusakabe, Naohiro Onodera, Noriyuki Kurose
  • Patent number: 8883778
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: November 11, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao, Linghang Zhuang
  • Patent number: 8877749
    Abstract: The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: November 4, 2014
    Assignee: Bristol-Myers Squibbs Company
    Inventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
  • Patent number: 8871738
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha