At Least Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 548/218)
  • Patent number: 10836978
    Abstract: A detergent, cleaning, fabric softener or cosmetic composition comprising a compound based on 1-Aza-3,7-dioxabicyclo[3.3.0]octane (bicyclic oxazolidine derivative) substituted with 3,7-dimethyl-1,6-nonyldien represented by formula (I) is disclosed.
    Type: Grant
    Filed: September 25, 2018
    Date of Patent: November 17, 2020
    Assignee: Henkel AG & Co. KGaA
    Inventors: Andre Haetzelt, Andreas Bauer, Marc Weyhe, Andreas Gerigk, Manuela Materne, Hubert Smyrek, Isabelle Levert, Ralf Bunn
  • Patent number: 10829498
    Abstract: A detergent, cleaning, fabric softener or cosmetic composition comprising a compound based on 1-Aza-3,7-dioxabicyclo[3.3.0]octane (bicyclic oxazolidine derivative) substituted with 3,7-dimethyl-1,6-nonyldien represented by formula (I) is disclosed.
    Type: Grant
    Filed: September 25, 2018
    Date of Patent: November 10, 2020
    Assignee: Henkel AG & Co. KGaA
    Inventors: Andre Haetzelt, Andreas Bauer, Marc Weyhe, Andreas Gerigk, Manuela Materne, Hubert Smyrek, Isabelle Levert, Ralf Bunn
  • Patent number: 10586930
    Abstract: The present invention relates to organic light emitting elements, comprising thermally activated delayed fluorescence (TADF) emitters and/or hosts of formula which have a sufficiently small energy gap between S1 and T1 (?EST) to enable up-conversion of the triplet exciton from T1 to S1. The organic light emitting elements show high electroluminescent efficiency.
    Type: Grant
    Filed: May 11, 2015
    Date of Patent: March 10, 2020
    Assignee: UDC IRELAND LIMITED
    Inventors: Junichi Tanabe, Christian Lennartz
  • Patent number: 10377732
    Abstract: The present invention relates to a process for preparing 3-amino tetrahydropyrans and, more particularly, to an improved method for synthesizing a 2,3,5-substituted tetrahydropyran derivative, intermediate being used in the preparation of dipeptidyl peptidase-IV enzyme inhibitors (DPP-4 inhibitors).
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: August 13, 2019
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: Paolo Maragni, Massimo Verzini
  • Patent number: 10380388
    Abstract: Methods of marking paper products and marked paper products are provided. Some methods include irradiating the paper product to alter the functionalization of the paper.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: August 13, 2019
    Assignee: Xyleco, Inc.
    Inventor: Marshall Medoff
  • Patent number: 9481680
    Abstract: An improved process for the preparation of a key intermediate for the synthesis of the active ingredient Omarigliptin is provided. The key intermediate is a compound having the following formula (I) wherein R1 is propargyl or allyl group and P is an amine protecting group. The compound of formula (I) is prepared by converting a compound of formula (IV) by an amination reaction to a compound of formula (III), which is then protected to provide a compound of formula (II), which is then alkylated to provide the compound of formula (I).
    Type: Grant
    Filed: January 19, 2015
    Date of Patent: November 1, 2016
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A
    Inventors: Ottorino De Lucchi, Enrico Rosso, Simone Zaramella, Stefano Tartaggia
  • Publication number: 20150080583
    Abstract: The invention relates to a novel class of quaternary ammonium salts containing tetra-hydro[1,3]oxazolo[2,3-b][1,3]oxazol-4-ium moiety in the structure, in particular the new derivatives of 4-methyltetrahydro[1,3]oxazolo[2,3-b][1,3]oxazol-4-ium, 4-(2-oxoethyl)tetrahydro[1,3]oxazolo[2,3-6][1,3]oxazol-4-ium, bis{4-methyltetrahydro[1,3]oxazoio[2,3-6][1,3]oxazol-4-ium}, bis{4-(2-oxoethyl)tetrahydro[1,3]oxazolo[2,3-b][1,3]oxazol-4-ium} and tris{4-methyltetrahydro[1,3]oxazolo[2,3-b][1,3]oxazol-4-ium} salts, process for the preparation of a novel class of quaternary ammonium salts and applications thereof.
    Type: Application
    Filed: January 31, 2013
    Publication date: March 19, 2015
    Applicant: UNIWERSYTET MEDYCZNY IM. KAROLA MARCINKOWSKIEGO
    Inventors: Jakub Rózanski, Agnieszka Gielara-Korzanska, Stanislaw Sobiak, Marcelina Maria Kubicka, Helena Kukula
  • Publication number: 20150018388
    Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
    Type: Application
    Filed: December 11, 2013
    Publication date: January 15, 2015
    Inventors: Richard B. Silverman, Yinan Zhang
  • Patent number: 8853212
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: October 7, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20140243288
    Abstract: The present invention relates to a fused ring-containing oxazolidinone compound shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, A, B and C are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound for the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.
    Type: Application
    Filed: September 29, 2012
    Publication date: August 28, 2014
    Inventors: Hui Zhang, Aichen Wang
  • Patent number: 8785637
    Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: July 22, 2014
    Assignee: Atto-Tec GmbH
    Inventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Kemnitzer, Alexander Zilles
  • Patent number: 8710092
    Abstract: Provided herein are substituted indolo[4,3-fg]quinolines of Formula (I) and (II) where R1-R6 and R13 are as defined in the specification and pharmaceutical compositions thereof which are useful in treating, preventing, or ameliorating a variety of medical disorders such as, for example, migraine. In other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and or 5-HT1B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: April 29, 2014
    Assignee: Map Pharmaceuticals, Inc.
    Inventors: Jian Zhang, Robert O. Cook, Thomas A. Armer, Sergey Alexandrovich Kosarev, Dejian Xie
  • Publication number: 20140100248
    Abstract: The present invention relates to new heterocyclic compounds as modulators of sphingolipid signaling and uses thereof of as pharmaceutically active agents, suitable for treating proliferative, degenerative, infectious, and other diseases.
    Type: Application
    Filed: April 2, 2012
    Publication date: April 10, 2014
    Applicants: UNIVERSITÄT BERN, JOHANN WOLFGANG GOETHE-UNIVERSITÄT
    Inventors: Holger Stark, Aleksandra Zivkovic, Andrea Huwiler, Josef Pfeilschifter
  • Publication number: 20140073501
    Abstract: A species of Burkholderia sp with no known pathogenicity to vertebrates but with pesticidal activity (e.g., plants, insects, fungi, weeds and nematodes) is provided. Also provided are natural products derived from a culture of said species and methods of controlling pests using said natural products.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 13, 2014
    Inventors: Ratnakar Asolkar, Marja Koivunen, Pamela Marrone
  • Publication number: 20140027741
    Abstract: Heterocyclic compounds, synthetic methods for preparing the same, and organic light-emitting display devices comprising the same are described. The subject heterocyclic compounds may comprise an aromatic ring or a heteroaromatic ring fused with a carbazole, dibenzothiophene, or dibenzofurane derivative, the compounds featuring rigid backbone structures with high glass transition temperatures and high melting points. The subject heterocyclic compounds may exhibit high electrical stability, improved charge transport ability, high heat resistance and improved light-emitting properties when used in organic light-emitting devices. Organic light-emitting display devices prepared according to the present invention exhibit lower driving voltages, increased luminescent efficiencies and longer lifetimes.
    Type: Application
    Filed: June 17, 2013
    Publication date: January 30, 2014
    Inventors: Bum-Woo PARK, Yoon-Hyun KWAK, Sun-Young LEE, Jong-Won CHOI, Wha-Il CHOI, So-Yeon KIM, Ji-Youn LEE, Jin-Young YUN
  • Publication number: 20130345410
    Abstract: Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.
    Type: Application
    Filed: December 20, 2012
    Publication date: December 26, 2013
    Applicant: OPTIMER PHARMACEUTICALS, INC.
    Inventor: Optimer Pharmaceuticals, Inc.
  • Publication number: 20130320262
    Abstract: The present invention relates to a compound of a formula (I), (II) or (III), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I), (II) or (III). The invention furthermore relates to a process for the preparation of a compound of the formula (I), (II) or (III) and to a formulation comprising one or more compounds of the formula (I), (II) or (III).
    Type: Application
    Filed: January 18, 2012
    Publication date: December 5, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Irina Martynova, Amir Hossain Parham, Christof Pflumm
  • Patent number: 8546376
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: October 1, 2013
    Assignee: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Patent number: 8519149
    Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt 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: Grant
    Filed: October 28, 2011
    Date of Patent: August 27, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
  • Patent number: 8466294
    Abstract: 1-aza-3,7-dioxabicyclo[3.3.0]octane compounds, process for their preparation, their use as pro-fragrances, and washing and cleaning compositions, fabric softeners and cosmetics comprising them, and a process for prolonging the odor perception of such compositions.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: June 18, 2013
    Assignee: Henkel AG & Co. KGaA
    Inventors: Ursula Huchel, Silvia Sauf, Thomas Gerke
  • Publication number: 20130150347
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
  • Publication number: 20130078185
    Abstract: The present invention provides novel compounds useful in the treatment and diagnosis of mycobacterial infections. Compounds of the present invention have enhanced biological properties as compared to the related known compounds. The present invention also provides a precursor compound useful in the synthesis of certain compounds of the invention, and a method to obtain these compounds using said precursor compound. Methods of treatment and diagnosis in which the compounds of the invention fmd use are also provided.
    Type: Application
    Filed: May 31, 2011
    Publication date: March 28, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Vijaya Raj Kuniyil Kulangara, Chandan Ramaswamy Atreya
  • Publication number: 20130059845
    Abstract: The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I: wherein the variables are as described herein. Related compositions, formulations and methods for the preparation of compounds of formula I are also described.
    Type: Application
    Filed: August 24, 2012
    Publication date: March 7, 2013
    Inventors: Jiangao SONG, Phuongly Pham, Jingyuan Ma, Aaron Robert Novack, Imad Nashashibi, David W. G. Wone, Dong-Fang Shi, Xin Chen
  • Publication number: 20130030027
    Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.
    Type: Application
    Filed: July 23, 2010
    Publication date: January 31, 2013
    Applicants: The Regents of the University of California, The Trustes of The University of Pennsylvania
    Inventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
  • Publication number: 20130012720
    Abstract: The present application relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs that includes forming a compound of formula (VIII).
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: NEREUS PHAMACEUTICALS, INC.
    Inventors: Taotao Ling, Samuel Danishefsky
  • Patent number: 8318787
    Abstract: A prodrug that has a prodrug moiety that degrades into a compound having the general Formula I with R3 being an alcoholic moiety can be useful in therapies for neurodegenerative diseases as well as cancer. Accordingly, the prodrug compounds can have a structure of Formula I, analogs thereof, derivatives thereof, or salts thereof, wherein: A and B are sulfur or oxygen; R1 and R2, in para, meta, or ortho position, are independently halogen, alkyl, alkoxy, haloalkyl, where R1 and R2 independently are straight chain, branched, substituted or unsubstituted; and R3 is a prodrug moiety. As examples, the prodrug can have a structure of any of Formulas I-V, which as shown in the specification.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: November 27, 2012
    Assignee: University of Kansas
    Inventors: Roger A. Rajewski, Mehmet Tanol, Ingrid Gunda Georg, Michelle P. McIntosh
  • Publication number: 20120295942
    Abstract: There are described 4-difluoromethoxyphenyl pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Application
    Filed: January 28, 2011
    Publication date: November 22, 2012
    Inventors: Nicholas James Devereux, Jeffrey McKenna
  • Publication number: 20120276047
    Abstract: The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: November 23, 2010
    Publication date: November 1, 2012
    Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge
  • Publication number: 20120277240
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: February 17, 2011
    Publication date: November 1, 2012
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20120238541
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Application
    Filed: September 17, 2010
    Publication date: September 20, 2012
    Applicant: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Patent number: 8263632
    Abstract: The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is 0 or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H or OCH3; R10 is F or Cl; or a pharmaceutically acceptable salt or ester thereof
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: September 11, 2012
    Assignees: Vertex Pharmaceuticals Incoporated, MSD K.K.
    Inventors: Toshiharu Iwama, Nobuhiko Kawanishi, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
  • Patent number: 8262949
    Abstract: The instant invention relates to novel benzotriazole UV-absorbers having a long wavelength shifted absorption spectrum with significant absorbance up to 410-420 nm. Further aspects of the invention are a process for their preparation, a UV stabilized composition containing the new UV-absorbers and the use of the new compounds as UV-light stabilizers for organic materials.
    Type: Grant
    Filed: June 18, 2007
    Date of Patent: September 11, 2012
    Assignee: BASF SE
    Inventors: Katharina Fritzsche, Markus Grob, Adalbert Braig, Ilona Marion Kienzle, Gérard Daniel Georges Vilain
  • Publication number: 20120190862
    Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.
    Type: Application
    Filed: July 19, 2011
    Publication date: July 26, 2012
    Inventors: Gunnar HANSON, Charles CALDWELL, Patrick G. HARRAN, Susan HARRAN, Qi WEI, Ming ZHOU
  • Publication number: 20120157434
    Abstract: The present invention provides heterocyclic compounds of the following formula I: or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
    Type: Application
    Filed: February 29, 2008
    Publication date: June 21, 2012
    Inventors: Mikhail Fedorovich Gordeev, Zhengyu Yuan, Jinqian Liu
  • Patent number: 8178672
    Abstract: An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.
    Type: Grant
    Filed: October 19, 2005
    Date of Patent: May 15, 2012
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre
  • Patent number: 8168798
    Abstract: This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: May 1, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Steven Durrant, Jean-Damien Charrier, John Studley
  • Patent number: 8163785
    Abstract: There are described 4-difluoromethoxyphenyl pyrazolo[5.1-b]oxazole derivatives of Formula I: which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: April 24, 2012
    Assignee: Novartis AG
    Inventors: Nicholas James Devereux, Jeffrey McKenna
  • Patent number: 8163753
    Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: April 24, 2012
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
  • Patent number: 8097730
    Abstract: The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: January 17, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Zhihua Sui
  • Publication number: 20120004328
    Abstract: Due to toxicological concerns, it may be desirable to replace the fragrance compound lilial with less problematic compounds without losing the creative power and quality regarding perfumes. The present invention addresses this need by using selected oxazolidines described herein.
    Type: Application
    Filed: September 14, 2011
    Publication date: January 5, 2012
    Applicant: Henkel AG & Co. KGaA
    Inventors: Ursula Huchel, Ralf Bunn, Manuela Materne, Werner Faber, Hubert Smyrek, Theo ten Pierik, Frank Rittler, Andreas Bauer, Michael Dischmann, Silvia Sauf, Dagmar Preis-Amberger
  • Patent number: 8088928
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: August 4, 2006
    Date of Patent: January 3, 2012
    Assignee: Sirtris Pharmaceuticals, Inc.
    Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch, Thomas Salzmann, David Armistead
  • Publication number: 20110301160
    Abstract: In general, the present invention relates to compounds capable of inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.
    Type: Application
    Filed: December 3, 2010
    Publication date: December 8, 2011
    Applicant: ARQULE, INC.
    Inventors: Mark A. ASHWELL, Syed ALI, Jifeng LIU, Yanbin LIU, Peter LOHSE, Belew MEKONNEN, Robert SELLIAH, Manish TANDON, Woj WRONA, Valery ANTONENKO
  • Publication number: 20110269969
    Abstract: The present application relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs that includes forming a compound of formula (VIII).
    Type: Application
    Filed: July 15, 2011
    Publication date: November 3, 2011
    Applicant: NEREUS PHARMACEUTICALS, INC.
    Inventors: Taotao Ling, Samuel Danishefsky
  • Publication number: 20110251379
    Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
    Type: Application
    Filed: March 3, 2011
    Publication date: October 13, 2011
    Applicant: Satori Pharmaceuticals, Inc.
    Inventors: Brian Scott Bronk, Wesley Francis Austin, Steffen Phillip Creaser, Mark A. Findeis, Nathan Oliver Fuller, Jed Lee Hubbs, Jeffrey Lee Ives, Ruichao Shen
  • Publication number: 20110195986
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R4, R5, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.
    Type: Application
    Filed: October 8, 2009
    Publication date: August 11, 2011
    Inventors: Guohua Zhao, William N. Washburn, James J. Mignone
  • Patent number: 7994203
    Abstract: There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: August 9, 2011
    Assignee: Novartis AG
    Inventors: Ian Bruce, Andrew James Culshaw, Nicholas James Devereux, François Gessier, Jeffrey McKenna, James Neef, Helen Elizabeth Oakman
  • Publication number: 20110190360
    Abstract: There are described 4-difluoromethoxyphenyl pyrazolo[5.1-b]oxazole derivatives of Formula I: which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.
    Type: Application
    Filed: January 31, 2011
    Publication date: August 4, 2011
    Inventors: Nicholas James Devereux, Jeffrey McKenna
  • Publication number: 20110178308
    Abstract: The present invention relates to a method for the production of 2-halo-4-nitroimidazole and intermediates thereof. Further, the present invention relates to a production process of 1,4-dinitroimidazole comprising subjecting 4-nitroimidazole to nitration reaction. Furthermore, the present invention relates to a production process of 4-nitroimidazole comprising subjecting imidazole to nitration reaction.
    Type: Application
    Filed: August 21, 2009
    Publication date: July 21, 2011
    Inventors: Guido Wuellner, Franz-Willi Herkenrath, Alexander Juelich, Yoshinori Yamada, Shuji Kawabe
  • Publication number: 20110178117
    Abstract: The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: September 16, 2009
    Publication date: July 21, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Antonella Converso, Timothy John Hartingh, Sylwia Stachura
  • Patent number: 7977491
    Abstract: A dendron or dendrimer, which has, as a recurring unit of each branch, a structure of formula (I): wherein TC designates a linkage to a former generation in the direction to a focal point of the dendron or a core of the dendrimer; TT designates a linkage to a next generation in the direction to a terminal; X is a divalent group comprised of at least one heteroatom; L1 and L2 each are a divalent linking group; R is a hydrogen atom or a substituent; and a method of producing a dendron or a dendrimer; and a method of producing a thioacetal compound.
    Type: Grant
    Filed: March 28, 2005
    Date of Patent: July 12, 2011
    Assignee: Fujifilm Corporation
    Inventor: Koki Nakamura