Chalcogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/312)
  • Patent number: 9233925
    Abstract: The present invention provides novel processes for the preparation of N-substituted benzamides having the formula VIc: In some embodiments, the invention provides a process for preparation of roflumilast and other pharmaceutically active species. Novel compounds, including intermediates for the synthesis of roflumilast, are also provided.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: January 12, 2016
    Assignee: ScinoPharm (Changshu) Pharmaceuticals, Ltd.
    Inventors: Yi-Jing Chen, Stanislaw Pikul, Shen-Chun Kuo, Guo-dong Chu
  • Publication number: 20150119362
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 30, 2015
    Inventors: Mark E. Gurney, Timothy J. Hagen, Joel R. Walker, Xuesheng Mo, A. Samuel Vellekoop, Robert Campbell, Lei Zhu, Donna L. Romero
  • Publication number: 20150099888
    Abstract: The present invention provides a compound of general formulae A useful as potential antitumor agents against human cancer cell lines and a process for the preparation thereof.
    Type: Application
    Filed: February 25, 2014
    Publication date: April 9, 2015
    Inventors: Ahmed Kamal, Mohammed Ashraf, Shaikh Faazil Bagwan, Yellamelli Valli Venkata Srikanth, Syed Mohammed Ali Hussaini, Adla Malla Reddy
  • Patent number: 8993258
    Abstract: A fluorinated voltage sensitive dye has the structure wherein p is 0, 1, or 2; Xq? is an anionic counterion having a charge, q, that is 1 or 2; n is 1 or 2; R1 is an optionally substituted C1-C12, alkyl; R2 is hydrogen, and R3 is hydrogen or fluorine; or R2 and R3 collectively form a divalent —CH?CH—CH?CH— group; R4 and each occurrence of R5 are each independently hydrogen or fluorine; R6 is hydrogen or fluorine or trifluoromethyl; and each occurrence of R7 is independently C1-C6 alkyl; provided that the dye comprises at least one fluorine atom. The dye is particularly useful for monitoring the dynamics of action potentials in axons and/or dendrites.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: March 31, 2015
    Assignee: The University of Connecticut
    Inventors: Ping Yan, Corey D. Acker, Leslie M. Loew
  • Publication number: 20150065517
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: March 5, 2015
    Applicant: NOVARTIS AG
    Inventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming LIU
  • Patent number: 8969577
    Abstract: The present invention relates to curable compositions comprising a thermolatent amidine base and an organic material which is polymerizable or crosslinkable with a basic or nucleophilic catalyst. In particular, the invention relates to curable coating compositions, especially powder coating compositions, and curable adhesive compositions, as well as to the use a thermolatent amidine base as a curing catalyst for thermally induced base-catalyzed polymerization or crosslinking reactions.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: March 3, 2015
    Assignee: BASF SE
    Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Ralf Knischka
  • Patent number: 8946437
    Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: February 3, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takashi Nakagawa, Makoto Sakamoto, Kazuya Yamaguchi, Yuki Terauchi, Masamichi Shirakura, Yasuo Harada, Yutaka Kojima, Takumi Sumida
  • Publication number: 20150025235
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: May 30, 2014
    Publication date: January 22, 2015
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
  • Publication number: 20150025246
    Abstract: The present invention provides novel processes for the preparation of N-substituted benzamides having the formula (VIc). In some embodiments, the invention provides a process for preparation of roflumilast and other pharmaceutically active species. Novel compounds, including intermediates for the synthesis of roflumilast, are also provided.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 22, 2015
    Applicant: Scinopharm (Changshu) Pharmaceuticals, Ltd.
    Inventors: Yi-Jing Chen, Stanislaw Pikul, Shen-Chun Kuo, Guo-dong Chu
  • Publication number: 20150011551
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Applicant: Sanford- Burnham Medical Reseach Institute
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
  • Publication number: 20140329674
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140323303
    Abstract: The present invention relates to a compound of formula (I): wherein: X is methyl or chlorine; R1 is methyl or chlorine; R2 is hydrogen, methyl, ethyl, n-propyl, cyclopropyl, vinyl, ethynyl, fluorine, chlorine, bromine, methoxy, ethoxy or fluoromethoxy; and G, R3, R4, R5 and R6 are as defined herein; wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.
    Type: Application
    Filed: November 30, 2012
    Publication date: October 30, 2014
    Applicants: Syngenta Participations AG, Syngenta Limited
    Inventors: Alaric James Avery, Mangala Mahadev Phadte, James Nicholas Scutt, John Benjamin Taylor, Russell Colin Viner, Jeffrey Steven Wailes
  • Publication number: 20140315878
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or a pharmaceutically acceptable salt thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes, and to methods of treatment, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert Ian Storer, Nigel Alan Swain, Robert McKenzie Owen
  • Patent number: 8865898
    Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: October 21, 2014
    Assignee: Japan Science and Technology Agency
    Inventor: Yoshihito Ueno
  • Patent number: 8859594
    Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: October 14, 2014
    Assignees: Tianjin Hemay Bio-Tech Co., Ltd., Tianjin Michele Sci-Tech Development Co., Ltd.
    Inventors: Hesheng Zhang, Xin Chen
  • Publication number: 20140303167
    Abstract: The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.
    Type: Application
    Filed: August 22, 2012
    Publication date: October 9, 2014
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Axel Choidas, Bert Klebl, Peter Habenberger, Jan Eickhoff, Roman Thomas, Johannes Heuckmann
  • Publication number: 20140296533
    Abstract: 4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a 3,3-dialkoxyprop-1-yne and a substituted methylene amine by a series of steps.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: James M. Renga, Gregory T. Whiteker, Peter L. Johnson, Christopher Galliford
  • Publication number: 20140296304
    Abstract: The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2012
    Publication date: October 2, 2014
    Applicants: LEAD DISCOVERY CENTER GMBH, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Gerd Rühter, Peter Nussbaumer, Axel Choidas, Carsten Schulz-Fademrecht, Bert Klebl, Jan Eickhoff
  • Patent number: 8846936
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Patent number: 8840866
    Abstract: 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: Grant
    Filed: January 7, 2013
    Date of Patent: September 23, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung
  • Publication number: 20140275536
    Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.
    Type: Application
    Filed: December 22, 2010
    Publication date: September 18, 2014
    Applicant: Galderma Research & Development
    Inventor: Cédric Poinsard
  • Patent number: 8829196
    Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: September 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Melissa Egbertson, Ahren Green, John C. Hartnett, Yiwei Li
  • Publication number: 20140221662
    Abstract: Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.
    Type: Application
    Filed: December 17, 2010
    Publication date: August 7, 2014
    Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES, LIANHE CHEMICAL TECHNOLOGY CO., LTD.
    Inventors: Dawei Ma, Shaolin Zhu, Shouyun Yu, You Wang, Qianghui Zhou
  • Publication number: 20140200225
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 17, 2014
    Applicant: ORION CORPORATION
    Inventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
  • Publication number: 20140171654
    Abstract: 4-Amino-3-chloro-6-(substituted)picolinates are prepared from difluoroacetic acid or trifluoroacetic acid, tritylamine or t-butylamine as a protecting group, a 3,3-dialkoxyprop-1-yne and a substituted methylene amine by a series of steps.
    Type: Application
    Filed: December 12, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Peter L. Johnson, James M. Renga, Natalie C. Giampietro, Gregory T. Whiteker, Christopher Galliford
  • Publication number: 20140171653
    Abstract: 4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a 3,3-dialkoxyprop-1-yne and a substituted methylene amine by a series of steps.
    Type: Application
    Filed: December 12, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: James M. Renga, Gregory T. Whiteker, Peter L. Johnson, Christopher Galliford
  • Patent number: 8722672
    Abstract: The present invention relates to pharmaceutical compositions of 2-Methyl-4?-trifluoromethoxy-biphenyl-3-carboxylic acid [6-(cis-2,6-dimethyl-morpholin-4-yl)-pyridin-3-yl]-amide, to the use of such compositions in therapeutic applications and to methods for manufacturing such compositions.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: May 13, 2014
    Assignee: Novartis AG
    Inventors: Andreas Fritze, Karine Corcelle, Melinda Eniko Grubesa
  • Publication number: 20140088105
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 27, 2014
    Applicant: NOVARTIS AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Publication number: 20140080768
    Abstract: The invention generally relates to Pro-Drugs of dihydroorotate dehydrogenase (DHODH) inhibitors and methods of use thereof. In certain embodiments, the invention provides a DHODH inhibitor compound including a cleavable functional group that increases bioavailability as compared to a form of the DHODH inhibitor without the functional group, rendering the former more suitable for therapeutic use.
    Type: Application
    Filed: September 19, 2012
    Publication date: March 20, 2014
    Inventors: Alan Palmer, Michael J. Hudson, Richard Todd, Patrick Camilleri
  • Publication number: 20140073789
    Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Inventor: Thomas Daly
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Publication number: 20140066410
    Abstract: This disclosure relates generally to compounds and compositions comprising one or more diphenylethylene, diphenylethylyne, and azobenzene analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory disease.
    Type: Application
    Filed: February 23, 2012
    Publication date: March 6, 2014
    Applicant: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
    Inventors: Ming-Ming Zhou, Michael Ohlmeyer, Shiraz Mujtaba, Alexander Plotnikov, David Kastrinsky, Guangtao Zhang
  • Publication number: 20140031348
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 30, 2014
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
  • Publication number: 20140024608
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 23, 2014
    Applicant: METHYLGENE INC.
    Inventors: Robert Deziel, Alain Ajamian
  • Publication number: 20140005212
    Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, R1b, R2a, R2b, R2c, A1, A2, and X are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 21, 2011
    Publication date: January 2, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou Ni, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark Youngman, Xiaoming Zhou
  • Publication number: 20140005178
    Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
    Type: Application
    Filed: August 12, 2013
    Publication date: January 2, 2014
    Applicant: Almirall, S.A.
    Inventors: Julio Cesar CASTRO PALOMINO LARIA, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Siliva Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
  • Patent number: 8614213
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Publication number: 20130327251
    Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
    Type: Application
    Filed: March 7, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF HOUSTON SYSTEM
    Inventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
  • Patent number: 8598213
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: December 3, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Patent number: 8586607
    Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: November 19, 2013
    Assignee: Syddansk Universitet
    Inventors: Trond Ulven, Elisabeth Christiansen
  • Publication number: 20130289076
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 31, 2013
    Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
  • Publication number: 20130267516
    Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: October 10, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
  • Patent number: 8530472
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, W, Y, R, R1, R2, R3 and R3? are as 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: September 10, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20130231342
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
    Type: Application
    Filed: July 27, 2011
    Publication date: September 5, 2013
    Applicant: Oryzon Fenomics S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
  • Publication number: 20130225596
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 29, 2013
    Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
  • Patent number: 8519142
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: August 27, 2013
    Assignee: Novartis AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Publication number: 20130217876
    Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.
    Type: Application
    Filed: August 21, 2012
    Publication date: August 22, 2013
    Applicant: ABBVIE INC.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 8501943
    Abstract: The present disclosure is directed to the sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid, pharmaceutically acceptable solvates thereof, pharmaceutical combinations thereof, and methods of treatment.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: August 6, 2013
    Assignee: Almirall, S.A.
    Inventors: Nuria Garcia Gonzalez, Francesc Carrera Carrera, Monserrat Julia Jane, Laurent Debethune, Xavier Serra Masia
  • Publication number: 20130196993
    Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: September 28, 2011
    Publication date: August 1, 2013
    Inventors: Michael Berger, Christopher Kern, Marko Eck
  • Publication number: 20130184315
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann