Three Or More Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/236.2)
  • Patent number: 10336702
    Abstract: The invention is directed to compounds of general formula (I), and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: July 2, 2019
    Assignee: BerGenBio ASA
    Inventors: Jason John Shiers, John Paul Watts, Stuart Thomas Onions, Mohammed Abdul Quddus, Joseph William Wrigglesworth, Colin Peter Sambrook-Smith, Alan Naylor, Derek Londesbrough
  • Patent number: 10317417
    Abstract: Described herein are, inter alia, methods for diagnosing and treating arrhythmogenic cardiomyopathy (ACM) by detecting cardiac intercalated disk proteins, e.g., desmosomal proteins, mechanical and gap junction proteins, in buccal cells. Exemplary desmosomal and gap junction proteins that can be evaluated in the methods described herein include plakoglobin, plakophilin 1, desmoplakin, and Cx43. The methods can also include selecting and/or administering a treatment for ACM to the subject.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: June 11, 2019
    Assignee: Beth Israel Deaconess Medical Center, Inc.
    Inventors: Jeffrey E. Saffitz, Angeliki Asimaki
  • Patent number: 10251872
    Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: April 9, 2019
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
  • Patent number: 10227527
    Abstract: There are disclosed nanoemulsion optical materials, methods of making nanoemulsion optical materials and optical articles comprising nanoemulsion optical materials. A nanoemulsion optical material includes a polymer matrix and a plurality of nano-droplets, comprising an optically interactive material, directly dispersed within the polymer matrix.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: March 12, 2019
    Assignees: INDIZEN OPTICAL TECHNOLOGIES OF AMERICA, LLC, FUTURECHROMES S.L., CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS (CSIC), INSTITUT CATALA DE NANOCIENCIA I NANOTECHNOLOGIA (ICN2)
    Inventors: Claudio Roscini, Héctor Torres-Pierna, Daniel Ruiz-Molina
  • Patent number: 10159747
    Abstract: The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: December 25, 2018
    Assignee: Graybug Visioon, Inc.
    Inventors: Jeffrey L. Cleland, Ming Yang, John G. Bauman, Nu Hoang, Emmett Cunningham
  • Patent number: 9995756
    Abstract: Described herein are, inter alia, methods for diagnosing and treating arrhythmogenic cardiomyopathy (ACM) by detecting cardiac intercalated disk proteins, e.g., desmosomal proteins, mechanical and gap junction proteins, in buccal cells. Exemplary desmosomal and gap junction proteins that can be evaluated in the methods described herein include plakoglobin, plakophilin 1, desmoplakin, and Cx43. The methods can also include selecting and/or administering a treatment for ACM to the subject.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: June 12, 2018
    Assignee: Beth Israel Deaconess Medical Center, Inc.
    Inventors: Jeffrey E. Saffitz, Angeliki Asimaki
  • Patent number: 9914736
    Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: March 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Ping Liu, Dann Parker, Chun Sing Li, Qinghua Mao
  • Patent number: 9718790
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Ri are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstjtuted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: August 1, 2017
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Hiroyuki Kai, Tohru Horiguchi, Kentaro Asahi, Yasuhiko Fujii
  • Patent number: 9706776
    Abstract: Compounds of the formula (I) and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, including all stereoisomers and tautomeric forms, and wherein the substituents are as defined in claim 1, are useful for controlling animal pests and can be prepared in a manner known per se.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: July 18, 2017
    Assignee: Syngenta Participations AG
    Inventors: Michel Muehlebach, Andrew Edmunds, Andre Stoller, Natalie Anne Miller, Ottmar Franz Hueter
  • Patent number: 9687479
    Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: June 27, 2017
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
  • Patent number: 9642850
    Abstract: A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.
    Type: Grant
    Filed: November 15, 2016
    Date of Patent: May 9, 2017
    Assignee: PURDUE PHARMA L.P.
    Inventors: Robert F. Reder, Paul D. Goldenheim, Robert F. Kaiko
  • Patent number: 9635857
    Abstract: A tetrazolinone compound represented by formula (1): wherein R1 and R2 each represents a hydrogen atom, a halogen atom, or a C1-C3 alkyl group; R3 represents a C1-C3 alkyl group optionally having one or more halogen atoms; R4, R5, and R6 each represents a hydrogen atom or a halogen atom; R7 represents a C1-C3 alkyl group; Q represents a divalent group selected from Group P4; and A represents a C7-C18 aralkyloxy group optionally having one or more atoms or groups selected from Group P3, has excellent control activity against pests.
    Type: Grant
    Filed: October 23, 2014
    Date of Patent: May 2, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Takayuki Shioda, Yuya Yoshimoto
  • Patent number: 9540337
    Abstract: Compositions that are effective in inhibiting gamma-glutamyl transpeptidase are disclosed. Methods of producing and using these compositions are also disclosed.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: January 10, 2017
    Assignee: The Board of Regents of the University of Oklahoma
    Inventors: Marie H. Hanigan, Pui Kai Li
  • Patent number: 9533970
    Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: January 3, 2017
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
  • Patent number: 9403798
    Abstract: There is provided a novel triazinone compound that has an excellent T-type voltage-dependent calcium channel inhibitory activity and is specifically useful for treatment of pain. A compound of Formula (I), a tautomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof: where each substituent is defined in detail in the description or claims, for example R1 is H or C1-6 alkoxy, etc., each of L1 and L2 is independently a single bond or NR2, etc., L3 is C1-6 alkylene, etc., A is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc., B is C3-11 cycloalkylene, etc., D is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: August 2, 2016
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Noriko Saito, Jun Egi, Hiroshi Nagai, Megumi Ueno, Yusuke Shintani, Yusuke Inaba, Michiaki Adachi, Yuichi Hirai, Takeshi Kawazu, Koichi Yasutake, Daiki Takahashi
  • Patent number: 9393218
    Abstract: The subject of this application is the use of film-forming polyurethanes that are used in hair care agents or mixtures of these polyurethanes with other polymers in pharmaceutical preparations for dermal or transdermal administration of active ingredients, as well as patches and pharmaceutical preparations that contain these hair care polyurethanes.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: July 19, 2016
    Assignee: EPINAMICS GMBH
    Inventors: Ines Zurdo Schroeder, Patrick Franke, Stefan Bracht, Claus-Michael Lehr, Ulrich Schäfer
  • Patent number: 9346798
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: May 24, 2016
    Assignee: AMGEN INC.
    Inventors: Christiane Boezio, Alessandro Boezio, Howard Bregman, Nagasree Chakka, James R. Coats, Katrina Woodin Copeland, Erin F. Dimauro, Thomas Dineen, Hua Gao, Daniel La, Isaac E. Marx, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss
  • Patent number: 9328076
    Abstract: Disclosed herein is a compound having Formula I: or a salt thereof, in which R1, R2 and R3 are as defined herein. Also disclosed are processes to prepare compounds of Formula I and use of Formula I to prepare stable glassy phases.
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: May 3, 2016
    Assignee: HER MAJESTY IN THE RIGHT OF CANADA AS REPRESENTED BY THE MINISTER OF DEFENSE
    Inventor: Olivier Lebel
  • Patent number: 9161938
    Abstract: Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat one or more ocular conditions, such as an ocular vasculopathy or glaucoma, among others.
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: October 20, 2015
    Assignee: Allergan, Inc.
    Inventors: Glenn T. Huang, Brittany Jackson, James A. Burke, Ton Lin, Patrick M. Hughes, Larry A. Wheeler, Rosy Sheng Donn
  • Publication number: 20150148346
    Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Applicant: PTC Therapeutics Inc.
    Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
  • Publication number: 20150133411
    Abstract: Compounds, compositions and methods useful for treating ocular diseases are provided. In particular, antagonists of TRPV4, their synthesis, pharmaceutical compositions thereof and methods of treating ocular diseases such as glaucoma, are disclosed. Compounds of the invention include N-(3-(trifluoromethyl)phenyl)-2-methyl-1-(3-morpholinopropyl)-5-phenyl-1 H-pyrrole-3-carboxamide, as well as other 2-phenyl-pyrrole carboxamide derivates and indole carboxamide derivatives.
    Type: Application
    Filed: March 15, 2013
    Publication date: May 14, 2015
    Inventors: David Krizaj, Glenn D. Prestwich, Peter Barabas, Yong Xu, Daniel Ryskamp
  • Publication number: 20150133414
    Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.
    Type: Application
    Filed: April 22, 2013
    Publication date: May 14, 2015
    Applicant: University of Virginia Patent Foundation
    Inventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
  • Publication number: 20150126510
    Abstract: The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.
    Type: Application
    Filed: March 18, 2013
    Publication date: May 7, 2015
    Applicants: Universiteit Antwerpen, Shakturana CV
    Inventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi (deceased)
  • Publication number: 20150126499
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 9023846
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: May 5, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mark R Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel J. Parks, William J Parsons, Scott Ballentine, Shawn Branum
  • Publication number: 20150119395
    Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Patent number: 9018205
    Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: April 28, 2015
    Assignee: The Scripps Research Institute
    Inventors: Theodore Mark Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
  • Publication number: 20150111857
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Publication number: 20150111893
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
  • Publication number: 20150104491
    Abstract: The present invention provides a sustained release implant for intraocular use to treat elevated intraocular pressure, which implant is configured for intracameral or anterior vitreal administration to a patient with elevated intraocular pressure (IOP), said implant comprising a core of an antihypertensive agent surrounded by a polymer, which limits the rate of passage of the antihypertensive agent from the implant into the eye of said patient and said implant provides a linear rate of release of therapeutically effective amounts of said anti-hypertensive agent into the eye for a period of time of between 14 days and 365 days.
    Type: Application
    Filed: September 10, 2014
    Publication date: April 16, 2015
    Inventors: Ruiwen Shi, Patrick M. Hughes, James A. Burke, Michael R. Robinson, Hui Liu
  • Patent number: 9006228
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
  • Publication number: 20150099750
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: December 1, 2014
    Publication date: April 9, 2015
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
  • Publication number: 20150099004
    Abstract: A liquid pharmaceutical compositions comprising Aprepitant is preferably prepared as an oral suspension dosage form for the prevention and control of acute and delayed chemotherapy induced nausea and vomiting, and/or for prevention of postoperative nausea and vomiting.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 9, 2015
    Inventors: Udaya Toti, Shyamprasad Mukundan, Sasank Chaitanya Kunadharaju, Tushar Hingorani, Kumaresh Soppimath, Satish Pejaver, Navneet Puri
  • Patent number: 9000153
    Abstract: The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Publication number: 20150087646
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Application
    Filed: June 10, 2013
    Publication date: March 26, 2015
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20150086646
    Abstract: Embodiments of the invention relates to decreasing effects of local and/or regional anesthesia by administering to a patient in need thereof an agent selected from the group of agents consisting of reactive nitrogen species (RNS), reactive oxygen species (ROS) and/or an agent which induces formation of RNS and/or ROS. Exemplary agents which may be used include peroxynitrite and hydrogen peroxide.
    Type: Application
    Filed: April 7, 2013
    Publication date: March 26, 2015
    Inventors: Sagi Polani, Asher Polani, Roee Atlas
  • Publication number: 20150087647
    Abstract: Disclosed are pharmaceutical compositions comprising brimonidine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.
    Type: Application
    Filed: April 28, 2014
    Publication date: March 26, 2015
    Applicant: Allergan Sales, LLC
    Inventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Publication number: 20150072977
    Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: David Alexander LEARMONTH, Laszlo Erno KISS, Pedro Nuno LEAL PALMA, Humberto DOS SANTOS FERREIRA, Patricio Manuel Vieira ARAUJO SOARES DA SILVA
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8962574
    Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Paul Anthony Reilly
  • Publication number: 20150045365
    Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.
    Type: Application
    Filed: August 6, 2014
    Publication date: February 12, 2015
    Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
  • Publication number: 20150045347
    Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.
    Type: Application
    Filed: January 11, 2013
    Publication date: February 12, 2015
    Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
  • Publication number: 20150045359
    Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.
    Type: Application
    Filed: January 8, 2013
    Publication date: February 12, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
  • Patent number: 8951536
    Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: February 10, 2015
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Amy Takvorian, Wenyu Zhu, Richard B. Sparks
  • Patent number: 8940738
    Abstract: A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: January 27, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Daiki Sakai, Kazuki Nakayama, Kazutoshi Watanabe
  • Publication number: 20150025057
    Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 22, 2015
    Applicant: NOVARTIS AG
    Inventors: Oliver BARKER, Jonathan Mark BENTLY, Mark Gary BOCK, Thomas CAIN, Praful CHOVATIA, Jennifer Ruth DOD, Florence EUSTACHE, Laura GLEAVE, Jonathan HARGRAVE, Alexander HEIFETZ, Richard LAW, Ali RAOOF, David WILLOWS
  • Publication number: 20150018328
    Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 15, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
  • Publication number: 20150018344
    Abstract: Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R7, are useful as kinase modulators, including IRAK-4 modulation.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 15, 2015
    Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
  • Publication number: 20150018331
    Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 15, 2015
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson