At Least Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 548/218)
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Patent number: 10836978Abstract: 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: GrantFiled: September 25, 2018Date of Patent: November 17, 2020Assignee: Henkel AG & Co. KGaAInventors: Andre Haetzelt, Andreas Bauer, Marc Weyhe, Andreas Gerigk, Manuela Materne, Hubert Smyrek, Isabelle Levert, Ralf Bunn
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Patent number: 10829498Abstract: 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: GrantFiled: September 25, 2018Date of Patent: November 10, 2020Assignee: Henkel AG & Co. KGaAInventors: Andre Haetzelt, Andreas Bauer, Marc Weyhe, Andreas Gerigk, Manuela Materne, Hubert Smyrek, Isabelle Levert, Ralf Bunn
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Patent number: 10586930Abstract: 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: GrantFiled: May 11, 2015Date of Patent: March 10, 2020Assignee: UDC IRELAND LIMITEDInventors: Junichi Tanabe, Christian Lennartz
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Patent number: 10380388Abstract: 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: GrantFiled: July 27, 2018Date of Patent: August 13, 2019Assignee: Xyleco, Inc.Inventor: Marshall Medoff
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Patent number: 10377732Abstract: 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: GrantFiled: November 29, 2016Date of Patent: August 13, 2019Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.Inventors: Paolo Maragni, Massimo Verzini
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Patent number: 9481680Abstract: 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: GrantFiled: January 19, 2015Date of Patent: November 1, 2016Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.AInventors: Ottorino De Lucchi, Enrico Rosso, Simone Zaramella, Stefano Tartaggia
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Publication number: 20150080583Abstract: 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: ApplicationFiled: January 31, 2013Publication date: March 19, 2015Applicant: UNIWERSYTET MEDYCZNY IM. KAROLA MARCINKOWSKIEGOInventors: Jakub Rózanski, Agnieszka Gielara-Korzanska, Stanislaw Sobiak, Marcelina Maria Kubicka, Helena Kukula
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Publication number: 20150018388Abstract: 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: ApplicationFiled: December 11, 2013Publication date: January 15, 2015Inventors: Richard B. Silverman, Yinan Zhang
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Patent number: 8853212Abstract: 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: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20140243288Abstract: 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: ApplicationFiled: September 29, 2012Publication date: August 28, 2014Inventors: Hui Zhang, Aichen Wang
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Patent number: 8785637Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.Type: GrantFiled: August 8, 2013Date of Patent: July 22, 2014Assignee: Atto-Tec GmbHInventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Kemnitzer, Alexander Zilles
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Patent number: 8710092Abstract: 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: GrantFiled: December 23, 2010Date of Patent: April 29, 2014Assignee: Map Pharmaceuticals, Inc.Inventors: Jian Zhang, Robert O. Cook, Thomas A. Armer, Sergey Alexandrovich Kosarev, Dejian Xie
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Publication number: 20140100248Abstract: 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: ApplicationFiled: April 2, 2012Publication date: April 10, 2014Applicants: UNIVERSITÄT BERN, JOHANN WOLFGANG GOETHE-UNIVERSITÄTInventors: Holger Stark, Aleksandra Zivkovic, Andrea Huwiler, Josef Pfeilschifter
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Publication number: 20140073501Abstract: 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: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Inventors: Ratnakar Asolkar, Marja Koivunen, Pamela Marrone
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Publication number: 20140027741Abstract: 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: ApplicationFiled: June 17, 2013Publication date: January 30, 2014Inventors: Bum-Woo PARK, Yoon-Hyun KWAK, Sun-Young LEE, Jong-Won CHOI, Wha-Il CHOI, So-Yeon KIM, Ji-Youn LEE, Jin-Young YUN
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Publication number: 20130345410Abstract: 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: ApplicationFiled: December 20, 2012Publication date: December 26, 2013Applicant: OPTIMER PHARMACEUTICALS, INC.Inventor: Optimer Pharmaceuticals, Inc.
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Publication number: 20130320262Abstract: 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: ApplicationFiled: January 18, 2012Publication date: December 5, 2013Applicant: MERCK PATENT GMBHInventors: Irina Martynova, Amir Hossain Parham, Christof Pflumm
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Patent number: 8546376Abstract: 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: GrantFiled: September 17, 2010Date of Patent: October 1, 2013Assignee: Almac Discovery LimitedInventors: 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
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Patent number: 8519149Abstract: 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: GrantFiled: October 28, 2011Date of Patent: August 27, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
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Patent number: 8466294Abstract: 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: GrantFiled: July 17, 2008Date of Patent: June 18, 2013Assignee: Henkel AG & Co. KGaAInventors: Ursula Huchel, Silvia Sauf, Thomas Gerke
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Publication number: 20130150347Abstract: 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: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130078185Abstract: 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: ApplicationFiled: May 31, 2011Publication date: March 28, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Vijaya Raj Kuniyil Kulangara, Chandan Ramaswamy Atreya
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Publication number: 20130059845Abstract: 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: ApplicationFiled: August 24, 2012Publication date: March 7, 2013Inventors: Jiangao SONG, Phuongly Pham, Jingyuan Ma, Aaron Robert Novack, Imad Nashashibi, David W. G. Wone, Dong-Fang Shi, Xin Chen
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Publication number: 20130030027Abstract: 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: ApplicationFiled: July 23, 2010Publication date: January 31, 2013Applicants: The Regents of the University of California, The Trustes of The University of PennsylvaniaInventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
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Publication number: 20130012720Abstract: 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: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: NEREUS PHAMACEUTICALS, INC.Inventors: Taotao Ling, Samuel Danishefsky
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Patent number: 8318787Abstract: 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: GrantFiled: August 10, 2009Date of Patent: November 27, 2012Assignee: University of KansasInventors: Roger A. Rajewski, Mehmet Tanol, Ingrid Gunda Georg, Michelle P. McIntosh
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Publication number: 20120295942Abstract: There are described 4-difluoromethoxyphenyl pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.Type: ApplicationFiled: January 28, 2011Publication date: November 22, 2012Inventors: Nicholas James Devereux, Jeffrey McKenna
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Publication number: 20120277240Abstract: 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: ApplicationFiled: February 17, 2011Publication date: November 1, 2012Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20120276047Abstract: 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: ApplicationFiled: November 23, 2010Publication date: November 1, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20120238541Abstract: 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: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: 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
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Patent number: 8263632Abstract: 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 thereofType: GrantFiled: March 15, 2010Date of Patent: September 11, 2012Assignees: Vertex Pharmaceuticals Incoporated, MSD K.K.Inventors: Toshiharu Iwama, Nobuhiko Kawanishi, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
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Patent number: 8262949Abstract: 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: GrantFiled: June 18, 2007Date of Patent: September 11, 2012Assignee: BASF SEInventors: Katharina Fritzsche, Markus Grob, Adalbert Braig, Ilona Marion Kienzle, Gérard Daniel Georges Vilain
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Publication number: 20120190862Abstract: 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: ApplicationFiled: July 19, 2011Publication date: July 26, 2012Inventors: Gunnar HANSON, Charles CALDWELL, Patrick G. HARRAN, Susan HARRAN, Qi WEI, Ming ZHOU
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Publication number: 20120157434Abstract: 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: ApplicationFiled: February 29, 2008Publication date: June 21, 2012Inventors: Mikhail Fedorovich Gordeev, Zhengyu Yuan, Jinqian Liu
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Patent number: 8178672Abstract: 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: GrantFiled: October 19, 2005Date of Patent: May 15, 2012Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre
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Patent number: 8168798Abstract: 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: GrantFiled: December 17, 2010Date of Patent: May 1, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Patent number: 8163753Abstract: 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: GrantFiled: October 29, 2004Date of Patent: April 24, 2012Assignee: 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
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Patent number: 8163785Abstract: 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: GrantFiled: January 31, 2011Date of Patent: April 24, 2012Assignee: Novartis AGInventors: Nicholas James Devereux, Jeffrey McKenna
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Patent number: 8097730Abstract: 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: GrantFiled: October 15, 2009Date of Patent: January 17, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Zhihua Sui
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Publication number: 20120004328Abstract: 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: ApplicationFiled: September 14, 2011Publication date: January 5, 2012Applicant: Henkel AG & Co. KGaAInventors: Ursula Huchel, Ralf Bunn, Manuela Materne, Werner Faber, Hubert Smyrek, Theo ten Pierik, Frank Rittler, Andreas Bauer, Michael Dischmann, Silvia Sauf, Dagmar Preis-Amberger
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Patent number: 8088928Abstract: 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: GrantFiled: August 4, 2006Date of Patent: January 3, 2012Assignee: 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
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Publication number: 20110301160Abstract: 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: ApplicationFiled: December 3, 2010Publication date: December 8, 2011Applicant: ARQULE, INC.Inventors: Mark A. ASHWELL, Syed ALI, Jifeng LIU, Yanbin LIU, Peter LOHSE, Belew MEKONNEN, Robert SELLIAH, Manish TANDON, Woj WRONA, Valery ANTONENKO
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Publication number: 20110269969Abstract: 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: ApplicationFiled: July 15, 2011Publication date: November 3, 2011Applicant: NEREUS PHARMACEUTICALS, INC.Inventors: Taotao Ling, Samuel Danishefsky
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Publication number: 20110251379Abstract: 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: ApplicationFiled: March 3, 2011Publication date: October 13, 2011Applicant: 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
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Publication number: 20110195986Abstract: 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: ApplicationFiled: October 8, 2009Publication date: August 11, 2011Inventors: Guohua Zhao, William N. Washburn, James J. Mignone
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Patent number: 7994203Abstract: There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.Type: GrantFiled: August 3, 2009Date of Patent: August 9, 2011Assignee: Novartis AGInventors: Ian Bruce, Andrew James Culshaw, Nicholas James Devereux, François Gessier, Jeffrey McKenna, James Neef, Helen Elizabeth Oakman
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Publication number: 20110190360Abstract: 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: ApplicationFiled: January 31, 2011Publication date: August 4, 2011Inventors: Nicholas James Devereux, Jeffrey McKenna
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Publication number: 20110178117Abstract: 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: ApplicationFiled: September 16, 2009Publication date: July 21, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Antonella Converso, Timothy John Hartingh, Sylwia Stachura
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Publication number: 20110178308Abstract: 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: ApplicationFiled: August 21, 2009Publication date: July 21, 2011Inventors: Guido Wuellner, Franz-Willi Herkenrath, Alexander Juelich, Yoshinori Yamada, Shuji Kawabe
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Patent number: 7977491Abstract: 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: GrantFiled: March 28, 2005Date of Patent: July 12, 2011Assignee: Fujifilm CorporationInventor: Koki Nakamura