Ring Oxygen In The Additional Hetero Ring Patents (Class 549/60)
  • Patent number: 8476309
    Abstract: Furanopyridine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: July 2, 2013
    Assignee: The University of Tennessee Research Foundation
    Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
  • Publication number: 20130153874
    Abstract: Provided are an organic electroluminescence device, which: shows high luminous efficiency; is free of any pixel defect; and has a long lifetime, and a material for an organic electroluminescence device for realizing the device. The material for an organic electroluminescence device is a compound of a specific structure having a ?-conjugated heteroacene skeleton crosslinked with a carbon atom, nitrogen atom, or oxygen atom. The organic electroluminescence device has one or more organic thin film layers including a light emitting layer between a cathode and an anode, and at least one layer of the organic thin film layers contains the material for an organic electroluminescence device.
    Type: Application
    Filed: February 5, 2013
    Publication date: June 20, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventor: IDEMITSU KOSAN CO., LTD.
  • Patent number: 8455497
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: June 4, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • Publication number: 20130136719
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: May 25, 2012
    Publication date: May 30, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson
  • Publication number: 20130123242
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 16, 2013
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
  • Patent number: 8436013
    Abstract: The invention features compositions and methods that are useful for treating or preventing AAT deficiency and associated conditions. In addition, the invention provides methods for identifying compounds useful for treatment of AAT deficiency and associated conditions.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: May 7, 2013
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Chen Liu, David A. Ostrov
  • Publication number: 20130096129
    Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
    Type: Application
    Filed: July 20, 2012
    Publication date: April 18, 2013
    Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
  • Patent number: 8420145
    Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: April 16, 2013
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Guy Servant
  • Patent number: 8410163
    Abstract: Substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carbonitriles and substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carboxamides and their salts are tubulin polymerization inhibitors, useful in the treatment of cancer.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: April 2, 2013
    Assignee: Telik, Inc.
    Inventors: Paul P. Beroza, Komath V. Damodaran, Stella Lui, Wenli Ma, Zhuo Wang, Hua Xu
  • Publication number: 20130079348
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: March 2, 2011
    Publication date: March 28, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130046072
    Abstract: Monomers having formula (I) and process for their synthesis which comprises the etherification reaction of a halogen-derivative (Z?Cl, Br, I) having formula (III) with the hydroxyl group of the glycerol derivative (IV), according to the following scheme:(Formula III, IV & I) (III) (IV) (I)
    Type: Application
    Filed: April 29, 2011
    Publication date: February 21, 2013
    Applicant: ENI S.p.A.
    Inventors: Giuliana Schimperna, Riccardo Po', Andrea Pellegrino, Maria Caldararo
  • Publication number: 20130039945
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: April 20, 2011
    Publication date: February 14, 2013
    Applicant: Kineta, Inc.
    Inventors: Shawn P. Iadonato, Kristin Bedard
  • Publication number: 20130035323
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: Abbott GmbH & Co. KG
    Inventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
  • 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
  • Patent number: 8357718
    Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.
    Type: Grant
    Filed: February 4, 2008
    Date of Patent: January 22, 2013
    Assignee: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Bettina Hamelin, Oswy Z. Pereira, Carl Poisson, Melanie Proulx, Thumkunta Jagadeeswar Reddy, Zhang Ming-Qiang
  • Publication number: 20130005767
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120316197
    Abstract: This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a pharmaceutical composition for the treatment of immune disease or allergy which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 22, 2011
    Publication date: December 13, 2012
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Kiyoshi Kanazawa, Kazuhiko Nonomura, Takako Okumura, Shinichi Koizumi
  • Patent number: 8329924
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: December 11, 2012
    Assignee: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
  • Publication number: 20120302752
    Abstract: Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Yigang Zhao, Victor A. Snieckus
  • Publication number: 20120301430
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: August 10, 2012
    Publication date: November 29, 2012
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson, Constantin G. Yannopoulos, Guy Falardeau, Louis Vaillancourt, Real Denis
  • Publication number: 20120302748
    Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.
    Type: Application
    Filed: February 28, 2012
    Publication date: November 29, 2012
    Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Patent number: 8318772
    Abstract: The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R1, R2 and n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: November 27, 2012
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Bohua Zhong, Youzhi Zhang, Yanping Zhang, Rui Xue, Xinhua He, Yunfeng Li, Hongxia Chen, Nan Zhao, Meiying Li
  • Publication number: 20120295966
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: February 12, 2010
    Publication date: November 22, 2012
    Applicant: N30 PHARMACEUTICALS, LLC
    Inventors: Xicheng Sun, Jian Qiu, Jan Wasley
  • Publication number: 20120289555
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: February 10, 2011
    Publication date: November 15, 2012
    Applicant: N30 PHARMACEUTICALS, LLC
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20120264736
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
    Type: Application
    Filed: October 6, 2011
    Publication date: October 18, 2012
    Applicant: Schering Corporation
    Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao
  • Patent number: 8288380
    Abstract: A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1—W2 represents CH—CH, or Y represents a single bond and W1—W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: October 16, 2012
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Publication number: 20120258965
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 11, 2012
    Applicants: The Johns Hopkins University, Cardioxyl Pharmaceuticals
    Inventors: John P. TOSCANO, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20120252995
    Abstract: Diels-Alder crosslinkable dendritic nonlinear optical chromophore compounds, films and crosslinked polymer composites formed from the chromophore compounds, methods for making and using the chromophore compounds, films, and crosslinked polymer composites, and electro-optic devices that include films and crosslinked polymer composites formed from the chromophore compounds.
    Type: Application
    Filed: May 3, 2012
    Publication date: October 4, 2012
    Applicant: UNIVERSITY OF WASHINGTON
    Inventors: Kwan-Yue Jen, Zhengwei Shi, Jingdong Luo, Su Huang, Xinghua Zhou
  • Publication number: 20120209005
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: October 22, 2010
    Publication date: August 16, 2012
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Patent number: 8242159
    Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: August 14, 2012
    Assignee: Dong-A Pharmaceutical. Co., Ltd
    Inventors: Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
  • Publication number: 20120202691
    Abstract: The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
    Type: Application
    Filed: July 29, 2010
    Publication date: August 9, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Stephane André Marie Jeanmart, Adrian Longstaff, Christopher John Mathews, Claire Janet Russel, Russell Colin Viner, Frances Kathryn Wood
  • Publication number: 20120178723
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 11, 2011
    Publication date: July 12, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20120172351
    Abstract: A compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof have a GPR40 receptor activation action and is useful as an insulin secretagogue or a prophylactic or therapeutic drug for diabetes and the like.
    Type: Application
    Filed: June 8, 2010
    Publication date: July 5, 2012
    Inventors: Nobuyuki Negoro, Yoshito Terao, Satoshi Mikami, Tomoya Yukawa
  • Publication number: 20120172345
    Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 11, 2011
    Publication date: July 5, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20120172599
    Abstract: Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a ?-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.
    Type: Application
    Filed: August 24, 2010
    Publication date: July 5, 2012
    Inventors: Akira Otomo, Isao Aoki, Hideki Miki, Hidehisa Tazawa, Shiyoshi Yokoyama
  • Publication number: 20120164103
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: March 9, 2012
    Publication date: June 28, 2012
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
  • Publication number: 20120156508
    Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles.
    Type: Application
    Filed: December 14, 2011
    Publication date: June 21, 2012
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Meng He, Darrin R. Dabideen, Sujit Mondal, Xiao-Man Dai, Ruisong Xu, Wenjing Xiao, Massimiliano Tomasulo, Huayun Yu, Anu Chopra, Anil Kumar
  • Publication number: 20120157677
    Abstract: The present invention relates to lactone compounds represented by the following Formulas I and II, and methods of making such lactone compounds. The present invention also relates to methods of making other materials from such lactone compounds, such as fused ring indenol compounds (e.g., indeno-fused naphthols), and fused ring indenopyran compounds (e.g., indeno-fused naphthopyrans).
    Type: Application
    Filed: December 7, 2011
    Publication date: June 21, 2012
    Applicant: TRANSITIONS OPTICAL INC.
    Inventors: Meng He, Darrin R. Dabideen, Ruisong Xu, Anil Kumar
  • Patent number: 8198271
    Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyle
    Type: Grant
    Filed: May 25, 2009
    Date of Patent: June 12, 2012
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Publication number: 20120142529
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: August 7, 2008
    Publication date: June 7, 2012
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Melloney Tyte, Stephane André Marie Jeanmart, Christopher John Mathews, Louisa Robinson
  • Publication number: 20120128640
    Abstract: An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells containing a compound represented by the formula (I) (wherein X, Y, Z, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.
    Type: Application
    Filed: June 4, 2010
    Publication date: May 24, 2012
    Applicant: NISSAN CHEMICAL INDUSTRIES LTD.
    Inventors: Taito Nishino, Shunsuke Iwamoto, Katsuaki Miyaji
  • Patent number: 8183262
    Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: May 22, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Publication number: 20120123125
    Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as a long-acting anticholinergic bronchodilator. Starting from oxalic acid derivative of formula III the invention describes preparation of a novel cyclic anhydride of formula II which is very efficient precursor in the synthesis of Tiotropium bromide (compound of formula I).
    Type: Application
    Filed: October 6, 2011
    Publication date: May 17, 2012
    Applicant: Drug Process Licensing Associates, LLC
    Inventor: Milan SOUKUP
  • Publication number: 20120123129
    Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R3, R9, R10, R11, R12 and G have the meanings given above as insecticides and/or acaricides and/or fungicides.
    Type: Application
    Filed: April 28, 2010
    Publication date: May 17, 2012
    Applicant: Bayer CropScience AG
    Inventor: Alfred ANGERMANN
  • Publication number: 20120116084
    Abstract: The invention relates to a method for manufacturing transistors. Said method involves using a molecule including at least two 2-dicyanomethylene-3-cyano-2,5-dihydrofuran groups. The invention can be implemented in particular in the field of electronics.
    Type: Application
    Filed: June 3, 2010
    Publication date: May 10, 2012
    Applicant: COMMISARIAT A L'ENERGIE ATOMIQUE ET AUX ENE ALT
    Inventors: Clément Suspene, Jean-Pierre Simonato
  • Publication number: 20120114765
    Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
    Type: Application
    Filed: March 31, 2010
    Publication date: May 10, 2012
    Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
  • Publication number: 20120108824
    Abstract: The present invention relates to a crystallisation procedure to obtain 1-(?-D- glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl] benzene hemihydrate crystals having a narrow particle size distribution and improved flowability, bulk and tap density properties.
    Type: Application
    Filed: July 8, 2010
    Publication date: May 3, 2012
    Inventors: Thomas Joachim Landewald Rammeloo, Ruben De Keyser, Gustaaf Jozef Petrus Schildermans
  • Publication number: 20120108636
    Abstract: The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 3, 2012
    Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
  • Publication number: 20120101286
    Abstract: Substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carbonitriles and substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carboxamides and their salts are tubulin polymerization inhibitors, useful in the treatment of cancer.
    Type: Application
    Filed: February 9, 2010
    Publication date: April 26, 2012
    Applicant: TELIK INC.
    Inventors: Paul P. Beroza, Komath V. Damodaran, Stella Lui, Wenli Ma, Zhuo Wang, Hua Xu
  • Publication number: 20120095012
    Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
    Type: Application
    Filed: December 30, 2009
    Publication date: April 19, 2012
    Applicant: Elara Pharmaceuticals GmbH
    Inventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen