Spiro Oxazine Patents (Class 544/71)
  • Patent number: 11767467
    Abstract: The present invention relates to a photochromic compound including a polyvalent residue on which at least one group having a photochromic moiety is substituted, and at least one long-chain group not containing a photochromic moiety and having a molecular weight of 300 or more is further substituted; and a curable composition containing the same. In accordance with the present invention, it is possible to provide a photochromic compound which has high solubility in a polymerizable compound serving as a matrix while retaining high photochromic characteristics and is hardly affected by the matrix; and a curable composition containing the same.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: September 26, 2023
    Assignee: TOKUYAMA CORPORATION
    Inventors: Takao Noguchi, Junji Takenaka, Junji Momoda, Takayoshi Kawasaki, Yasutomo Shimizu, Masayuki Miyazaki
  • Patent number: 11697636
    Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: November 12, 2020
    Date of Patent: July 11, 2023
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Katrin Groebke Zbinden, Roger Norcross, Phillippe Pfileger
  • Patent number: 11530218
    Abstract: Disclosed are spirocyclic compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and treating cancer, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.
    Type: Grant
    Filed: January 20, 2021
    Date of Patent: December 20, 2022
    Assignee: INCYTE CORPORATION
    Inventors: Le Zhao, Xiaozhao Wang, Wenyu Zhu, Haolin Yin, Liangxing Wu, Wenqing Yao
  • Patent number: 11091427
    Abstract: This invention relates to a method for producing an alkenyl 1-aminocyclopropane-1-carboxylic acid of Formula I wherein R1 is a protecting group, n is an integer between 1 and 10, and A and B are chiral centres such that when A is S, B is R and when A is R, B is S. The method comprises a stereoselective formation of the cyclopropane moiety by cycloaddition onto a double bond, in a molecule comprising a chiral template, Formula lc. Further provided is the use of Formula I in the production of stapled peptides.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: August 17, 2021
    Assignee: Agency for Science, Technology and Research
    Inventors: Tsz Ying Yuen, Charles William Johannes, Greg Verdine
  • Patent number: 10053453
    Abstract: The present application relates to compounds of formula (I), (Ia), or (Ib) and their pharmaceutical compositions/preparations. This application further relates to methods of treating or preventing A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia, including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.
    Type: Grant
    Filed: October 7, 2015
    Date of Patent: August 21, 2018
    Assignee: AstraZeneca AB
    Inventors: Roland Bürli, Mark E. Duggan, Jörg Holenz, Patrik Johansson, Karin Kolmodin, Philip Vellacott Thorne, Michael John McKenzie
  • Patent number: 9920070
    Abstract: The present invention relates to novel spiro-oxazine analogs of Formula-I and Indolinone compounds of Formula-II or positional isomers, or stereoisomers, or derivatives, or pharmaceutically acceptable salt thereof. Formula-I Formula-II Further the invention provides transition-metal free multicomponent reaction (MCR) process for the preparation of said compounds of Formula-I and II using aryne precursor, N-substituted isatin and N-heteroaromatic compound as the nucleophile, under mild condition leading to formation of desired complex of spiro-oxazine analogs (I) and indolinone analogs (II) in high yield and selectivity.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: March 20, 2018
    Assignee: Council of Scientific & Industrial Research
    Inventors: Biju Akkattu Thankappan, Anup Bhunia, Tony Roy
  • Patent number: 9604974
    Abstract: The present disclosure relates to compound of structural Formula I and a method for preparing said compounds. The disclosure further relates to a method of employing the Formula I compounds for modulation of Janus kinase-Signal Transducer and Activator of Transcription (JAK-STAT) pathway in cancer cells, and the corresponding use of compound of Formula I as anti-cancer agents.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: March 28, 2017
    Assignees: UNIVERSITY OF MYSORE, NATIONAL UNIVERSITY OF SINGPORE, BANGALORE UNIVERSITY, CAMBRIDGE ENTERPRISE LTD
    Inventors: Kanchugarakoppal Subbegowda Rangappa, Basappa, Chakrabhavi Dhananjaya Mohan, Shobith Rangappa, Hanumantharayappa Bharathkumar, Gautam Sethi, Andreas Bender, Peter Edward Lobie, Kam Man Hui, Alan Prem Kumar, Vijay Kumar Pandey, Julian Fuchs, Muthu Kumaraswamy Shanmugam, Krishna Bulusu, Xiaoyun Dai, Feng Li, Amudha Deivasigamani
  • Patent number: 9181273
    Abstract: The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: November 10, 2015
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Hayley Marie Binch, Michael Paul DeNinno, Lev Tyler Dewey Fanning, Bryan A. Frieman, Peter Diederik Jan Grootenhuis, Nicole Hilgraf, Pramod Joshi, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Alina Silina, Urvi Jagdishbhai Sheth, Dennis James Hurley, Vijayalaksmi Arumugam
  • Patent number: 9084794
    Abstract: This invention relates to spirocyclic piperidines according to Formula (I) and the use of spirocyclic piperidines for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: July 21, 2015
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Jonathan Michael Ghergurovich, Michael Lee Moore, Cynthia Ann Parrish, Lance Howard Ridgers, Hongyi Lu
  • Patent number: 9063358
    Abstract: A multi-functional photochromic chiral nematic liquid crystal window comprises at least a photochromic chiral nematic liquid crystal layer. The windows are able to not only to darken in color upon exposure to sunlight irradiation but also control the light and the heat passing through them, which can be used as the windows of buildings, vehicles, and the like.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: June 23, 2015
    Assignee: KENT STATE UNIVERSITY
    Inventors: Quan Li, Yannian Li, Ji Ma
  • 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
  • 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
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150079081
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Application
    Filed: October 27, 2014
    Publication date: March 19, 2015
    Applicant: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQuing Wei
  • Patent number: 8980877
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: March 17, 2015
    Assignee: DAC S.R.L.
    Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
  • Publication number: 20150051201
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 19, 2015
    Applicant: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Bryan K. Chan, Jennafer Dotson, Anthony Estrada, Timothy Heffron, Joseph Lyssikatos, Zachary Sweeney
  • 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: 20150025073
    Abstract: The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: August 7, 2014
    Publication date: January 22, 2015
    Inventors: Sara Sabina Hadida-Ruah, Hayley Marie Binch, Michael Paul DeNinno, Lev Tyler Dewey Fanning, Bryan A. Frieman, Peter Diederik Jan Grootenhuis, Nicole Hilgraf, Pramod Joshi, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Alina Silina, Urvi Jagdishbhai Sheth, Dennis James Hurley, Vijayalaksmi ARUMUGAM
  • 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: 8921363
    Abstract: The present invention relates to a compound represented by general formula I: or a stereoisomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt thereof, wherein A1, A2, A3, A4, A5, A6, R2, R7, W, X, Y and Z are defined within. These compounds are useful for the modulation of ?-secretase enzyme activity and for the treatment of ?-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions.
    Type: Grant
    Filed: August 4, 2011
    Date of Patent: December 30, 2014
    Assignee: Amgen Inc.
    Inventors: Ana Elena Minatti, Yuan Cheng, Wenge Zhong
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • 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: 20140364601
    Abstract: Processes for the preparation of the compound of formula (II) and intermediate compounds for use in the processes.
    Type: Application
    Filed: May 11, 2012
    Publication date: December 11, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Neil Barnwell, Philip Cornwall, Duncan Michael Gill, Gareth P. Howell, Rebecca Elizabeth Meadows, Andiappan Murugan, Philip O'Keefe, John Singleton, Jane Withnall, Eric Merifield, Christopher William Mitchell, Zakariya Mohamed Patel, James Barry Rose
  • Publication number: 20140350244
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventors: Richard V. Connors, Kang DAI, John EKSTEROWICZ, Pingchen FAN, Benjamin FISHER, Jiasheng FU, Kexue LI, Zhihong LI, Lawrence R. MCGEE, Rajiv SHARMA, Xiaodong WANG, Dustin L. MCMINN, Jeffrey T. MIHALIC, Jeffrey DEIGNAN
  • 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: 8883799
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: November 11, 2014
    Assignee: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQing Wei
  • 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: 8865741
    Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
    Type: Grant
    Filed: February 18, 2012
    Date of Patent: October 21, 2014
    Assignee: Asana Biosciences, LLC
    Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
  • Publication number: 20140309220
    Abstract: The invention relates to benzoxazines useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: November 2, 2012
    Publication date: October 16, 2014
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Corey Anderson, Joseph Pontillo, Edward Adam Kallel, Mehdi Michael Djamel Numa, Bryan A. Frieman, Jason McCartney, Jennings Franklin Worley, III, Vijayalaksmi Arumugam, Johnny Uy, Nicole Hilgraf, Brian Richard Bear
  • Publication number: 20140308282
    Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C?O, >S(?O), >S(?O)2, —O—C(?O)—, —C(?O)—O—, N(R2)—C(?O)—, or —C(?O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(?O)R2, —S(?O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 16, 2014
    Applicant: re: Viral Ltd
    Inventors: Stuart Cockerill, Christopher Pilkington, James Lumley, Richard Angell, Neil Mathews
  • Publication number: 20140296226
    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, L, 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: Application
    Filed: September 21, 2012
    Publication date: October 2, 2014
    Inventors: Ryan White, Yuan Cheng, Ana Elena Minatti, Bryant Yang, Xiao Mei Zheng, Patricia Lopez, Jason B. Human, Oleg Epstein, Ted Judd, Kelvin Sham, Qiufen Xue
  • Publication number: 20140275017
    Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20140275517
    Abstract: Methods and systems for the preparation of conditioned micronized active agents. Additionally, methods and systems for in-process conditioning of micronized active agent particles and compositions comprising conditioned micronized materials.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Pearl Therapeutics, Inc.
    Inventors: Ali Kazmi, David Lechuga, Herm Snyder, James Ivey, Reinhard Vehring, Jason H. Speck, Sarvajna Dwivedi
  • Patent number: 8822459
    Abstract: The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
    Type: Grant
    Filed: February 15, 2011
    Date of Patent: September 2, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaya Kokubo, Yoshikazu Takaoka, Shiro Shibayama
  • Patent number: 8801976
    Abstract: Photochromic dyes are disclosed. A photochromic dye can include a first photo-reactive group and a second photo-reactive group. A first photochromic reaction can be induced in the first photo-reactive group of the photochromic dye by radiation having a first wavelength, and a second photochromic reaction can be induced in the second photo-reactive group of the photochromic dye by radiation having a second wavelength.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: August 12, 2014
    Assignee: Korea University Research and Business Foundation
    Inventor: Dong Hoon Choi
  • Publication number: 20140191168
    Abstract: Photochromic dyes are disclosed. A photochromic dye can include a first photo-reactive group and a second photo-reactive group. A first photochromic reaction can be induced in the first photo-reactive group of the photochromic dye by radiation having a first wavelength, and a second photochromic reaction can be induced in the second photo-reactive group of the photochromic dye by radiation having a second wavelength.
    Type: Application
    Filed: September 28, 2012
    Publication date: July 10, 2014
    Applicant: KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION
    Inventor: KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION
  • Publication number: 20140194415
    Abstract: This invention relates to spirocyclic piperidines according to Formula (I) and the use of spirocyclic piperidines for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 10, 2014
    Applicant: GlaxoSmithKline Intellectual Property (No2) Limite
    Inventors: Jonathan Michael Ghergurovich, Michael Lee Moore, Cynthia Ann Parrish, Lance Howard Ridgers, Hongyi Lu
  • Patent number: 8772286
    Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fademrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
  • Publication number: 20140171427
    Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: November 25, 2013
    Publication date: June 19, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina HADIDA-RUAH, Edward Adam KALLEL, Mark Thomas MILLER, Joseph PONTILLO, Vijayalaksmi ARUMUGAM, Nicole HILGRAF, Jason McCARTNEY, Peter Diederik Jan GROOTENHUIS, Corey ANDERSON, Mehdi NUMA, Bryan A. Frieman, Brian Richard BEAR, Jason Philip JOHNSON, JR.
  • Patent number: 8754073
    Abstract: Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancers.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: June 17, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
  • Publication number: 20140113895
    Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 24, 2014
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Patent number: 8685965
    Abstract: Compounds of Formula (I), (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, L, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG, W, Y and Z are as described herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Donnette D. Staas, Ian M. Bell, Harold G. Selnick
  • Publication number: 20140080823
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 20, 2014
    Applicant: DAC S.R.L.
    Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
  • Patent number: 8658635
    Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: February 25, 2014
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Publication number: 20140045831
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Ildiko Maria Buck, Gianni Chessari, Steven Howard, David Charles Rees, Alison Jo-Anne Woolford
  • Publication number: 20140042377
    Abstract: A photochromic polymer comprising at least two photochromic moieties linked by a straight or branched chain polymer selected from the group consisting of poly(C2 to C4 alkylene oxide), poly[C1 to C10 alkoxy substituted (C2 to C4 alkylene oxide)] and poly[C1 to C-15 acyloxy substituted (C2 to C4 alkylene oxide)].
    Type: Application
    Filed: May 2, 2012
    Publication date: February 13, 2014
    Applicant: VIVIMED LABS EUROPE LTD
    Inventors: Richard Alexander Evans, Nino Malic
  • Publication number: 20140045828
    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: Application
    Filed: June 27, 2013
    Publication date: February 13, 2014
    Inventors: Jian CHEN, Wenge ZHONG, Bryant YANG, Wenyuan QIAN, Patricia LOPEZ, Ryan WHITE, Matthew WEISS, Tedd JUDD, Timothy POWERS, Yuan CHENG, Thomas DINEEN, Oleg EPSTEIN, Jason HUMAN, Jonathan D. LOW, Isaac E. MARX, Ana Elena MINATTI, Michele POTASHMAN, Nick A. PARAS, Qingyian LIU
  • Patent number: 8648070
    Abstract: This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: February 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Dieter Hamprecht, Barbara Kistler, Iain Lingard
  • Publication number: 20140027684
    Abstract: A photochromic polymer comprising at least two photochromic moieties linked by a straight or branched chain polymer selected from the group consisting of a homo-polyester, a co-polyester, and a co-polyester-polyether.
    Type: Application
    Filed: May 21, 2012
    Publication date: January 30, 2014
    Applicant: VIVIMED LABS EUROPE LTD
    Inventors: Richard Alexander Evans, Nino Malic, Ian John Dagley
  • Patent number: 8629271
    Abstract: The present invention relates to spirocyclic amide derivatives of the formula I, pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: January 14, 2014
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Nicholas David Kindon