Chalcogen Bonded Directly At The 2-position Of The Oxazole Ring Patents (Class 548/221)
  • Publication number: 20150111935
    Abstract: The present invention relates to a novel class of 1,3-benzoxazol-2(3H)-ones and their use as a medicament, preferably as a dermatologic agent, and as a cosmetic. These novel compounds are particularly useful in treating and/or preventing inflammation, irritation, itching, pruritus, pain, oedema and/or pro-allergic or allergic conditions in a patient. Usually they are topically applied to the skin or mucosa in the form of a pharmaceutical or cosmetic composition comprising the compound and a pharmaceutically and/or cosmetically acceptable carrier.
    Type: Application
    Filed: May 21, 2013
    Publication date: April 23, 2015
    Applicant: DR. AUGUST WOLFF GMBH & CO. KG ARZNEIMITTEL
    Inventors: Chrsitoph Abels, Ulrich Knie, Michael Soeberdt
  • Publication number: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Publication number: 20150045368
    Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 12, 2015
    Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
  • Publication number: 20150031685
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 29, 2015
    Applicant: Dr. Reeddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
  • Publication number: 20150011760
    Abstract: A reagent for carrying out a difluoromethylation reaction of unsaturated compounds and ring-nitrogen-containing aromatic compounds, a zinc difluoro-methanesulfinate, as well as a method for making the reagent and a method for its use are disclosed.
    Type: Application
    Filed: November 27, 2012
    Publication date: January 8, 2015
    Inventors: Phil S. Baran, Janice Akemi Dixon, Ryan Baxter, Yuta Fujiwara
  • Publication number: 20140378421
    Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Application
    Filed: November 9, 2012
    Publication date: December 25, 2014
    Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
  • Publication number: 20140378493
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Publication number: 20140315963
    Abstract: [Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.
    Type: Application
    Filed: April 18, 2014
    Publication date: October 23, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Ryota Shiraki, Takahiko Tobe, Shimpei Kawakami, Hiroyuki Moritomo, Makoto Ohmiya
  • Patent number: 8865623
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: October 21, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20140309427
    Abstract: Certain 3,6-disubstituted and 2, 4, 5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3, 6 and 2, 4, 5 pyrans are useful in probing the effects of their binding to monoamine transporter systems and the corresponding relationships to various afflictions affecting the CNS, or as a treatment for various CNS-related disorders in which the monoamine transport and related systems are implicated.
    Type: Application
    Filed: February 6, 2014
    Publication date: October 16, 2014
    Inventor: Aloke K. DUTTA
  • Publication number: 20140296238
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: June 10, 2014
    Publication date: October 2, 2014
    Inventors: Henry YU, Thomas E. RICHARDSON, Robert James FOGLESONG, Lizbeth Celeste DESELM, Andreas GOUTOPOULOS
  • Patent number: 8809402
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: August 19, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Patent number: 8791114
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
  • Publication number: 20140163079
    Abstract: The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 12, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Suzanne Walker Kahne, Jiaoyang Jiang, Michael Block Lazarus
  • Patent number: 8703963
    Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: April 22, 2014
    Assignee: University of South Florida
    Inventors: Edward Turos, Rajesh Kumar Mishra, Kevin Revell
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Publication number: 20140038943
    Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 6, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
  • Publication number: 20130345196
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.
    Type: Application
    Filed: May 24, 2012
    Publication date: December 26, 2013
    Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • Publication number: 20130316999
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: August 7, 2013
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
  • Publication number: 20130303541
    Abstract: The present invention discloses an aryloxy dihalopropenyl ether compound with the structure shown as general formula (I), of which the group definitions can be seen in the specification. The present invention also discloses the use of the compound with general formula (I) as an insecticide in the agricultural field and an insecticidal composition using the compound with general formula (I) as an active component.
    Type: Application
    Filed: March 28, 2012
    Publication date: November 14, 2013
    Applicants: Shenyang Research Institute Of Chemical Industry Co., Ltd., SINOCHEM CORPORATION
    Inventors: Changling Liu, Jichun Yang, Xiuhui Chang, Miao Li, KeKe Li, Qiao Wu, Yuquan Song
  • Publication number: 20130303525
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: July 19, 2011
    Publication date: November 14, 2013
    Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.
    Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
  • Patent number: 8569282
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: October 29, 2013
    Assignee: CytoPathfinder, Inc.
    Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
  • Patent number: 8501953
    Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: August 6, 2013
    Assignee: Agios Pharmaceuticals, Inc
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20130172335
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130172351
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: June 26, 2012
    Publication date: July 4, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
  • Patent number: 8450495
    Abstract: A method of preparing novel [11C]-labeled benzophenone/bezoxazole analogues is provided. The present invention also provides novel [11C]-labeled benzophenone/bezoxazole analogues prepared from the GMP synthesis method. Kit claims for preparing novel [11C]-labeled benzophenone/bezoxazole analogues and a method of use thereof are also provided.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: May 28, 2013
    Assignee: GE Healthcare Limited
    Inventors: Farhad Karimi, Bengt Langstrom
  • Patent number: 8450313
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Publication number: 20130123217
    Abstract: The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.
    Type: Application
    Filed: December 13, 2012
    Publication date: May 16, 2013
    Applicant: NEUMEDICS
    Inventor: Neumedics
  • Publication number: 20130109649
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: October 25, 2012
    Publication date: May 2, 2013
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Publication number: 20130079339
    Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.
    Type: Application
    Filed: December 22, 2010
    Publication date: March 28, 2013
    Applicant: PHARMESTE S.R.L.
    Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
  • Publication number: 20130079511
    Abstract: The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 28, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Jennifer SCHOMAKER, Luke BORALSKY, John HERSHBERGER, Jared RIGOLI, Christopher S. ADAMS
  • Publication number: 20130079374
    Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.
    Type: Application
    Filed: October 23, 2012
    Publication date: March 28, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventor: TAKEDA PHARMACEUTICAL COMPANY LIMITE
  • Publication number: 20130005984
    Abstract: A method of preparing novel [11C]-labeled benzophenone/bezoxazole analogues is provided. The present invention also provides novel [11C]-labeled benzophenone/bezoxazole analogues prepared from the GMP synthesis method. Kit claims for preparing novel [11C]-labeled benzophenone/bezoxazole analogues and a method of use thereof are also provided.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: FARHAD KARIMI, BENGT LANGSTROM
  • Publication number: 20120329775
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: June 4, 2012
    Publication date: December 27, 2012
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Patent number: 8329907
    Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: December 11, 2012
    Assignee: Merck Patent GmbH
    Inventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
  • Patent number: 8304553
    Abstract: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: November 6, 2012
    Assignee: Nanyang Technological University
    Inventors: Xuewei Liu, Jimei Ma
  • Patent number: 8293775
    Abstract: The present invention relates to benzoxazolone derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, in the treatment of movement disorders, in particular in Parkinson's disease.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: October 23, 2012
    Assignee: UCB Pharma, S.A.
    Inventors: Jean-Philippe Starck, Benoît Kenda
  • Patent number: 8293774
    Abstract: The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: October 23, 2012
    Assignee: Kyung Nong Corporation
    Inventors: Joo-kyung Kim, Dong-hoo Kim, Hyung-ho Kim, Kyung-hyun Kim, Cheol-su Yoon, In-cheon Hwang
  • Publication number: 20120232071
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • 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: 8188095
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: May 29, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
  • Publication number: 20120122849
    Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.
    Type: Application
    Filed: November 4, 2011
    Publication date: May 17, 2012
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20120095231
    Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: its pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen or the like, Y is a group of the formula: Z is —NR7- or the like, R1 is hydrogen or the like, R2 and R3 are each independently hydrogen or the like, n is 0 or 1, p is 0 to 6.
    Type: Application
    Filed: November 30, 2011
    Publication date: April 19, 2012
    Inventor: Toshisada YANO
  • Publication number: 20120053342
    Abstract: The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivatized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.
    Type: Application
    Filed: November 4, 2011
    Publication date: March 1, 2012
    Applicant: SABIC INNOVATIVE PLASTICS IP B.V.
    Inventors: Hatem Abdallah Belfadhel, Hans-Peter Brack, Ricardo Godoy-Lopez, Dennis James Patrick Maria Willemse
  • Publication number: 20120040960
    Abstract: The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: October 25, 2011
    Publication date: February 16, 2012
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui
  • Publication number: 20120040974
    Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
    Type: Application
    Filed: August 18, 2009
    Publication date: February 16, 2012
    Applicant: YALE UNIVERSITY
    Inventors: William L. Jorgensen, Richard J. Bucala
  • Publication number: 20120021907
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: January 6, 2010
    Publication date: January 26, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20120015976
    Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
    Type: Application
    Filed: March 9, 2010
    Publication date: January 19, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANK TER HAFTUNG
    Inventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
  • Publication number: 20120004227
    Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.
    Type: Application
    Filed: March 5, 2010
    Publication date: January 5, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya