Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 546/121)
  • Patent number: 10307748
    Abstract: A highly pure optically active proton pump inhibitor compound can be produced safely and inexpensively in a high yield and enantioselectivity by a method of producing an optically active sulfoxide of Formula 2 or a salt thereof, comprising oxidizing a sulfide of Formula 1 or a salt thereof with hydrogen peroxide using an iron salt in the presence of a chiral ligand of Formula 3; wherein A is CH or N; R1 is hydrogen atom, an alkyl optionally substituted by halogen(s), or an alkoxy optionally substituted by halogen(s); one to three R2 may exist, and each of R2 is independently an alkyl, a dialkylamino, or an alkoxy optionally substituted by halogen(s) or alkoxy(s); each of R3 is independently hydrogen atom, a halogen, cyano or the like; R4 is a tertiary alkyl; and * and ** represent respectively R configuration or S configuration.
    Type: Grant
    Filed: December 25, 2015
    Date of Patent: June 4, 2019
    Assignee: THE UNIVERSITY OF TOKYO
    Inventors: Eiichi Nakamura, Laurean Ilies, Yoji Oderaotoshi, Takuhiro Izumi, Shigenobu Nishiguchi
  • Patent number: 10053460
    Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include interme-diates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1 ]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: August 21, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhijian Liu, Nobuyoshi Yasuda, Lu Yang, Artis Klapars, Kevin R. Campos, Mikhail Reibarkh
  • Patent number: 9980948
    Abstract: Disclosed is a compound which is useful as an AMPK activator.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: May 29, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yuusuke Tamura, Yu Hinata, Eiichi Kojima, Hiroki Ozasa
  • Patent number: 9908876
    Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo[1,2-a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.
    Type: Grant
    Filed: February 29, 2016
    Date of Patent: March 6, 2018
    Assignee: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Marvin J. Miller, Garrett C. Moraski, Lowell D. Markley, George E. Davis
  • Patent number: 9890159
    Abstract: The present invention relates to a process comprising converting a compound of formula (I) into a compound of formula (II) by reaction with an organolithium reagent, which compound can be further converted into duocarmycin analogs consisting of a DNA-alkylating and a DNA-binding part, and still further into corresponding antibody-drug conjugates.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: February 13, 2018
    Assignee: Synthon Biopharmaceuticals B.V.
    Inventors: Tijl Huijbregts, Ronald Christiaan Elgersma, Patrick Henry Beusker, Johannes Albertus Frederikus Joosten, Rudy Gerardus Elisabeth Coumans, Henri Johannes Spijker, Wiro Menge, Franciscus Marinus Hendrikus De Groot
  • Patent number: 9861620
    Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, Yonglian Zhang, Sherman Tim Waddell, Andrew Stamford, John S. Wai, Paul J. Coleman, John M. Sanders, Ronald Ferguson, Thomas H. Graham, Hong Li
  • Patent number: 9862716
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of 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: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi-Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Keith P. Moore, Ping Liu, Harold B. Wood, Chun Sing Li, Qinghua Mao, Douglas C. Beshore
  • Patent number: 9834557
    Abstract: A process for preparation of (2S, 5R)-7-oxo-6-sulphooxy-2-[((3R)-piperidine-3-carbonyl)-hydrazino carbonyl]-1,6-diaza-bicyclo[3.2.1]octane is disclosed.
    Type: Grant
    Filed: March 29, 2017
    Date of Patent: December 5, 2017
    Assignee: WOCKHARDT LIMITED
    Inventors: Sanjeev Joshi, Karuna Suresh Wankhede, Sunil Bhaginath Jadhav, Shivaji Sampatrao Pawar, Vinod Kashinath Ahirrao, Satish Bhawsar, Prasad Keshav Deshpande, Ravindra Dattatraya Yeole, Mahesh Vithalbhai Patel
  • Patent number: 9790223
    Abstract: A process for preparation of a compound of Formula (I) is disclosed.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: October 17, 2017
    Assignee: WOCKHARDT LIMITED
    Inventors: Vijay Prakash Chavan, Karuna Suresh Wankhede, Vikas Vithalrao Deshmukh, Satish Bhavsar, Kiran Ramchandra Patil, Ravindra Dattatraya Yeole, Prasad Keshav Deshpande, Mahesh Vithalbhai Patel
  • Patent number: 9688677
    Abstract: A process for preparation of a compound of Formula (I) is disclosed.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: June 27, 2017
    Assignee: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Mohammad Usman Shaikh, Mahesh Vithalbhai Patel
  • Patent number: 9676777
    Abstract: An optically active (2S,5R)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid compound defined by the following formula (F): wherein R1 represents CO2R, CO2M, or CONH2, wherein R represents an allyl group or a benzyl group, and M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.
    Type: Grant
    Filed: January 27, 2016
    Date of Patent: June 13, 2017
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
  • Patent number: 9670207
    Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: June 6, 2017
    Assignee: Dr. Reddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
  • Patent number: 9670201
    Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: June 6, 2017
    Assignee: Pfizer Inc.
    Inventors: Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Göran Mattias Wennerstål, Li Xing, Edouard Zamaratski, Liying Zhang
  • Patent number: 9670204
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: June 6, 2017
    Assignee: GALAPAGOS NV
    Inventors: Nicolas Desroy, Bertrand Heckmann, Reginald Christophe Xavier Brys, Agnès Marie Joncour, Christophe Peixoto, Xavier Marie Bock
  • Patent number: 9663518
    Abstract: A process for preparation of a compound of Formula (I) is disclosed.
    Type: Grant
    Filed: February 2, 2015
    Date of Patent: May 30, 2017
    Assignee: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Bharat Dond, Mahesh Vithalbhai Patel
  • Patent number: 9580424
    Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.
    Type: Grant
    Filed: May 13, 2015
    Date of Patent: February 28, 2017
    Assignee: Forest Laboratories Holdings Limited
    Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
  • Patent number: 9556174
    Abstract: A process for preparation of (2S, 5R)-Sulfuric acid mono-{[(4-aminopiperidin-4-yl) carbonyl]-7-oxo-1,6-diaza-bicyclo[3.2.1]-oct-6-yl} ester is disclosed which comprises reacting a compound of Formula (II) with a compound of Formula (III) to obtain a compound of Formula (IV).
    Type: Grant
    Filed: October 12, 2013
    Date of Patent: January 31, 2017
    Assignee: WOCKHARDT LIMITED
    Inventors: Karuna Suresh Wankhede, Mahesh Manikrao Surwase, Satish Bhawsar, Prasad Keshav Deshpande, Ravindra Dattatraya Yeole, Mahesh Vithalbhai Patel
  • Patent number: 9550772
    Abstract: The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.
    Type: Grant
    Filed: December 30, 2013
    Date of Patent: January 24, 2017
    Assignee: ORIBASE PHARMA
    Inventors: Gwénaël Cheve, Bénédicte Dayde-Cazals, Bénédicte Fauvel, Cédric Bories, Abdelaziz Yasri
  • Patent number: 9518040
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: December 13, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • Patent number: 9447093
    Abstract: The present invention discloses compositions of novel DYRK1A protein inhibitors based on a 3,5-diarylazaindole motif and their preparation and use as medications in the treatment of cognitive disorders associated with dysfunction of DYRK1A protein, with Down's syndrome and with Alzheimer's disease.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: September 20, 2016
    Assignees: Centre National De La Recherche Scientifique (CNRS), Universite de Reims Champagne-Ardenne, Universite Paris Diderot Paris 7
    Inventors: Robert Dobb, Kevin Cariou, Stephanie Gourdain, Jean Maurice Delabar, Nathalie Janel, Fernando Rodrigues Lima, Julien Dairou, Clement Denhez
  • Patent number: 9402833
    Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: August 2, 2016
    Assignee: Dr. Reddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
  • Patent number: 9403820
    Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3K activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3K activity, are described herein.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: August 2, 2016
    Assignees: Intellikine LLC, Sigma-Aldrich Company Limited
    Inventors: Pingda Ren, Michael Martin, Christopher Peter Worrall, Susanna del Rio Gancedo
  • Patent number: 9387204
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: July 12, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Swen Hölder, Armin Zülch, Thomas Bär, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
  • Patent number: 9340541
    Abstract: Disclosed is a method for preparing a compound of Formula 1 by coupling of intermediates of Formula 2 and Formula 3 in the presence of an aluminum reagent of Formula 4 wherein R1, R2a, R2b and R2c are defined in the disclosure.
    Type: Grant
    Filed: December 31, 2013
    Date of Patent: May 17, 2016
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: Ahmad El-Awa
  • Patent number: 9199984
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I) are inhibitors of neutrophil elastase.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: December 1, 2015
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Carmelida Capaldi, Robert Andrew Heald, Nicholas Charles Ray, Jonathan Mark Sutton
  • Patent number: 9199959
    Abstract: The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent. wherein, a broken line means the presence or absence of a bond; R1 is substituted or unsubstituted alkyl etc., R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is a substituted or unsubstituted aromatic carbocyclic group; R4 is a hydrogen atom etc.; R5 is a substituted or unsubstituted aromatic carbocyclic group etc.; Y is a single bond etc.; R6 is substituted or unsubstituted alkyl; R7 is —Z—R71 etc.; Z is —NR72—CO— etc.; R71 is substituted or unsubstituted alkyl etc.; R72 is a hydrogen atom etc.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: December 1, 2015
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Tsutomu Iwaki, Kenji Tomita
  • Patent number: 9173878
    Abstract: The present invention provides a pharmaceutical composition used in improving brain function including a compound of formula (I).
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: November 3, 2015
    Assignee: Tohoku University
    Inventor: Kohji Fukunaga
  • Patent number: 9145433
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: September 29, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • Patent number: 9120796
    Abstract: Provided herein are intermediates useful in the synthesis of ?-lactamase inhibitors, and methods of making said intermediates and ?-lactamase inhibitors.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: September 1, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Evan A. Hecker, Amy Baldwin
  • Patent number: 9108966
    Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: August 18, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
  • Patent number: 9085560
    Abstract: A method of inhibiting phosphatidyl inositol-3 kinase (PI3 kinase), comprising: contacting the PI3 kinase with an effective amount of a compound or pharmaceutically acceptable salt of the formula below, wherein the variables R1, R2, W1, W2, W3, W4, W5, are W6 are defined herein.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: July 21, 2015
    Assignee: INTELLIKINE, INC.
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
  • Patent number: 9045478
    Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: June 2, 2015
    Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Patent number: 9040554
    Abstract: Disclosed are solid forms of 8-chloro-N-[(2-chloro-5-methoxyphenyl)sulfonyl]-6-(trifluoromethyl)-imidazo[1,2-a]pyridine-2-carboxamide (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are nematocidal compositions comprising a nematocidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematicide, insecticide and/or fungicide are also disclosed. Also disclosed are methods for protecting a plant from nematodes comprising applying to the plant, or portion, or seed thereof, or to the growing medium of the plant, a nematocidally effective amount of Compound 1 comprising the polymorph Form A.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: May 26, 2015
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Christian Hoffmann, William J Marshall, Rafael Shapiro, Richard A Berger
  • Patent number: 9040706
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: May 26, 2015
    Assignee: GENENTECH, INC.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
  • Publication number: 20150141401
    Abstract: A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O?, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Seiichi Inamura, Akihiro Morinaka
  • Publication number: 20150141394
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 21, 2015
    Applicant: Wockhardt Ltd.
    Inventors: Vijaykumar Jagdishwar PATIL, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Publication number: 20150141399
    Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: February 5, 2015
    Publication date: May 21, 2015
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Patent number: 9029388
    Abstract: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: May 12, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Haruhi Kamisaki, Shinkichi Suzuki, Kasei Miura
  • Publication number: 20150118186
    Abstract: New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for theft preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: January 5, 2015
    Publication date: April 30, 2015
    Inventors: Jordi BACH TAÑA, Lluis Miquel PAGES SANTACANA, Joan TALTAVULL MOLL, Paul Robert EASTWOOD, Jacob GONZALEZ RODRIGUES, Victor GIULIO MATASSA
  • Patent number: 9018228
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; and R1, R2, R3, Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: April 28, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Renee Marie Lett, Brenton Todd Smith, Benjamin Kenneth Smith, Clarice Anne Tyler
  • Publication number: 20150112070
    Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
    Type: Application
    Filed: January 5, 2015
    Publication date: April 23, 2015
    Applicant: FOREST LABORATORIES HOLDINGS LTD.
    Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew Phillips, Mahendra G. Dedhiya
  • Publication number: 20150111864
    Abstract: This disclosure provides compositions containing solid forms of (2S,5R)-2-(5-(3-aminopropyl)-1,3,4-oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate, and methods of manufacturing and using these compositions.
    Type: Application
    Filed: October 2, 2014
    Publication date: April 23, 2015
    Inventors: Sudhakar Garad, Akash Jain, You Seok Hwang
  • Publication number: 20150111872
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 23, 2015
    Applicant: GALAPAGOS NV
    Inventors: Nicolas DESROY, Bertrand HECKMANN, Reginald Christophe Xavier BRYS, Agnès Marie JONCOUR, Christophe PEIXOTO, Xavier Marie BOCK
  • Patent number: 9012042
    Abstract: A condensed-cyclic compound represented by Formula 1 below, an organic light-emitting device including the same, and a flat panel display apparatus including the organic light-emitting device: X1, Ar1, Ar2, Ar3, Ar4, Ar5, Ar6, Ar7, Ar8, Ar9, Ar10, Ar11, and Ar12 being described in the detailed description of the invention. The organic light-emitting device including an organic layer including the compound above has low driving voltage and high emission efficiency.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: April 21, 2015
    Assignee: Samsung Display Co., Ltd.
    Inventors: Hee-Yeon Kim, Seung-Gak Yang, Jeoung-In Yi, Jae-Yong Lee
  • Patent number: 9012447
    Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: April 21, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
  • Patent number: 9012450
    Abstract: Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: April 21, 2015
    Assignees: Global Blood Therapeutics, Inc., Cytokinetics, Inc., The Regents of the University of California
    Inventors: Brian Metcalf, Chihyuan Chuang, Jeffrey Warrington, Kumar Paulvannan, Matthew P. Jacobson, Lan Hua, Bradley Morgan
  • 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
  • Patent number: 8999966
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr.