The Additional Hetero Ring Contains Nitrogen As The Only Ring Hetero Atom [e.g., N-(cyclopentylcarbonyl-l-histidyl)-pyrrolidine, Etc.] Patents (Class 548/314.7)
  • Publication number: 20110070197
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: September 10, 2010
    Publication date: March 24, 2011
    Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Ce Wang, Yao-Ling Qiu
  • Publication number: 20110064697
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: September 10, 2010
    Publication date: March 17, 2011
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20110064695
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: September 10, 2010
    Publication date: March 17, 2011
    Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
  • Patent number: 7906503
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
    Type: Grant
    Filed: October 21, 2008
    Date of Patent: March 15, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
  • Publication number: 20110046113
    Abstract: It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1): In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(?O) or NR11; and D is a group represented by the following general formula (4) or (6). In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). —(CR18R19)m3— Or —(CR20R21)m4-z-(CR22R23)m5??(7) z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26.
    Type: Application
    Filed: October 12, 2010
    Publication date: February 24, 2011
    Applicant: KUREHA CORPORATION
    Inventors: Toru YAMAZAKI, Shigeyuki KIKUMOTO, Masahiro ONO, Atsushi SAITOU, Haruka TAKAHASHI, Sei KUMAKURA, Kunitaka HIROSE, Mikiro YANAKA, Yoshiyuki TAKEMURA, Shigeru SUZUKI, Ryo MATSUI
  • Publication number: 20110046105
    Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
    Type: Application
    Filed: August 6, 2010
    Publication date: February 24, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard Jaehne, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
  • Publication number: 20110041261
    Abstract: The invention relates to the dyeing of keratinous fibres using azomethine direct dyes of formula (I) or reduced precursors of azomethine direct dyes of formula (II) obtained from 2-chloro-3-amino-6-methylphenol. A subject-matter of the invention is a dyeing composition comprising at least one chlorinated azomethine direct dye or one reduced precursor of a chlorinated azomethine direct dye, a method for dyeing keratinous fibres which employs the said composition and their uses in the dyeing of keratinous fibres. This composition makes it possible to obtain a particularly stable and consistent colouring.
    Type: Application
    Filed: December 9, 2008
    Publication date: February 24, 2011
    Inventors: Madeleine Leduc, Stéphane Sabelle, Eric Metais, Christophe Rondot
  • Publication number: 20110036975
    Abstract: Imidazolium-based dicationic liquid salts and methods of using such imidazolium-based dicationic liquid salts in techniques such as ESI-MS are provided.
    Type: Application
    Filed: February 17, 2009
    Publication date: February 17, 2011
    Applicant: SIGMA-ALDRICH CO.
    Inventor: Armstrong W. Daniel
  • Publication number: 20110028476
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof.
    Type: Application
    Filed: September 1, 2010
    Publication date: February 3, 2011
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20110021590
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein each of Ring A, Ring B, T, R2, R2?, and RA is as defined and described herein and methods for treating subjects or patients with a disease, disorder, or condition.
    Type: Application
    Filed: June 7, 2010
    Publication date: January 27, 2011
    Applicant: Link Medicine Corporation
    Inventor: Mark E. Duggan
  • Publication number: 20110003690
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.
    Type: Application
    Filed: January 29, 2009
    Publication date: January 6, 2011
    Applicant: BAY CROPSCIENCE AG
    Inventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
  • Publication number: 20110003825
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Application
    Filed: August 23, 2010
    Publication date: January 6, 2011
    Applicant: Schering Corporation
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • Patent number: 7838681
    Abstract: The invention relates to a method of synthesizing heterocyclic compounds. The invention is characterised in that it consists in opening a compound having formula (I), wherein: —X represents NH, O, S or a N-p group, p being a protective group, such as Boc or Troc; —Y represents N, O, S; —Z represents NH2 or NH-p; and —R1 represents a C1-C6 alkoxy radical, aryloxy, such as phenyloxy, or a pyrrolyl radical, said radicals being optionally substituted, or the salts thereof, and the isomers of the aforementioned compounds. Moreover, the above-mentioned opening step is performed in conditions such as to produce a heterocycle having formula (II), wherein: —X, Y and Z are as defined above; —R2 represents a —CH?CH—CH2—NH—COR1 or —CH?CH—CH2—NH—CO group; and R3 occupies one, two or three positions and represents a halogen. The invention can be used to synthesise natural products.
    Type: Grant
    Filed: April 30, 2004
    Date of Patent: November 23, 2010
    Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite de Paris Sud
    Inventors: Ali Al Mourabit, Nathalie Travert, Robert Abou-Jneid, Saïd Ghoulami
  • Publication number: 20100273849
    Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Application
    Filed: January 26, 2010
    Publication date: October 28, 2010
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenchöld, Pavol Zlatoidsky
  • Publication number: 20100267722
    Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 16, 2010
    Publication date: October 21, 2010
    Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Publication number: 20100261696
    Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (G1yT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (G1yT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 31, 2010
    Publication date: October 14, 2010
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
  • Publication number: 20100256192
    Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 29, 2009
    Publication date: October 7, 2010
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
  • Patent number: 7807844
    Abstract: A TGF-? gene expression inhibitor containing a pyrrole-imidazole polyamide having N-methylimidazole unit (hereinafter also referred to as Py), N-methylimidazole unit (hereinafter also referred to as Im) and ?-aminobutyrate unit which can be holded into an U-shaped conformation at the ?-aminobutyrate unit in the minor groove in a double helix region (hereinafter referred to as the target region) containing a complementary chain corresponding to the sequence at the ?557 to ?536 in the base sequence of a human transforming growth factor ?1 (hereinafter also referred to as hTGF-?1) promoter, either as a whole or a part thereof: TAAAGGAGAGCAATTCT-TACAG (SEQ ID NO: 1) wherein a Py/Im pair corresponds to a C-G base pair, an Im/Py pair corresponds to a G-C base pair, and Py/Py pairs correspond respectively to an A-A base pair and a T-A base pair.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: October 5, 2010
    Assignees: Nihon University, Gentier Biosystems, Inc.
    Inventors: Noboru Fukuda, Hirofumi Kishioka, Hiroshi Sugiyama
  • Publication number: 20100234374
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.
    Type: Application
    Filed: December 21, 2006
    Publication date: September 16, 2010
    Inventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Raffaele Ingenito, Carsten Schultz-Fademrecht
  • Publication number: 20100227855
    Abstract: Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.
    Type: Application
    Filed: March 16, 2010
    Publication date: September 9, 2010
    Applicant: ENDORECHERCHE, INC.
    Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, René Maltais
  • Patent number: 7790707
    Abstract: The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.
    Type: Grant
    Filed: March 21, 2007
    Date of Patent: September 7, 2010
    Assignee: EPIX Pharmaceuticals Inc.
    Inventors: Ashis Saha, Xiang Yu, Mercedes Lobera, Jian Lin, Srinivasa R. Cheruku, Oren Becker, Yael Marantz, Nili Schutz
  • Patent number: 7790710
    Abstract: The compounds of formula (I) in which R1, R11 and A have the meanings as given in the description are novel effective iNOS inhibitors.
    Type: Grant
    Filed: March 29, 2006
    Date of Patent: September 7, 2010
    Assignee: NYCOMED GmbH
    Inventors: Thomas Fuchss, Andreas Strub, Wolf-Rüdiger Ulrich, Christian Hesslinger, Martin Lehner, Raimund Külzer, Rainer Boer, Manfrid Eltze
  • Publication number: 20100216792
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: October 14, 2009
    Publication date: August 26, 2010
    Applicant: Bayer CropScience AG
    Inventors: Ulrich Görgens, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Publication number: 20100216806
    Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.
    Type: Application
    Filed: February 19, 2010
    Publication date: August 26, 2010
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
  • Publication number: 20100216813
    Abstract: The present invention relates to a compound represented by the following formula I or a pharmaceutically acceptable salt thereof; wherein R1, R2, and y are defined herein. The present invention further relates to compositions that include the compound of the present invention as well as a method of treating a patient from endometreosis or uterine fibroids.
    Type: Application
    Filed: November 29, 2006
    Publication date: August 26, 2010
    Inventor: James S. Frazee
  • Publication number: 20100184737
    Abstract: The present invention relates to compounds of Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of Formula I.
    Type: Application
    Filed: March 12, 2010
    Publication date: July 22, 2010
    Applicant: Pfizer Inc
    Inventors: Michael A. Brodney, Karen J. Coffman, Edward F. Kleinman, Brian T. O'Neill, Yuhpyng L. Chen
  • Publication number: 20100178246
    Abstract: A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.
    Type: Application
    Filed: December 4, 2009
    Publication date: July 15, 2010
    Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
  • Patent number: 7754750
    Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Grant
    Filed: May 6, 2008
    Date of Patent: July 13, 2010
    Assignee: AstraZeneca AB
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
  • Publication number: 20100173898
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.
    Type: Application
    Filed: March 15, 2010
    Publication date: July 8, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
  • Publication number: 20100168107
    Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.
    Type: Application
    Filed: March 12, 2010
    Publication date: July 1, 2010
    Applicant: Pfizer Inc
    Inventors: Michael A. Brodney, Karen J. Coffman
  • Publication number: 20100168088
    Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: October 2, 2009
    Publication date: July 1, 2010
    Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
  • Publication number: 20100168189
    Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.
    Type: Application
    Filed: February 8, 2008
    Publication date: July 1, 2010
    Inventors: David W. Old, Wha Bin Im, Vinh X. Ngo
  • Patent number: 7741347
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: June 22, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Lawrence G. Hamann, Clint A. James, David R. Langley, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Gan Wang, Fukang Yang
  • Publication number: 20100130446
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention has a glucokinase activity, and is useful as a medicament such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.
    Type: Application
    Filed: April 25, 2008
    Publication date: May 27, 2010
    Applicant: TAKEDA PHARMACEUTICAS COMPANY LIMITED
    Inventors: Tsuneo Yasuma, Kentaro Hashimoto, Masahiro Ito
  • Patent number: 7723307
    Abstract: Novel Amino Acid Derivatives and Pharmaceutical Uses Thereof Provided are novel compounds of Formula I: wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. Further provided are pharmaceutical formulations of the compounds and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally provided are methods, of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g.
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: May 25, 2010
    Assignee: Aston University
    Inventors: Martin Griffin, Ian G. Coutts, Robert E. Saint
  • Publication number: 20100121074
    Abstract: Disclosed is an ionic liquid which is stable over a wide potential range and exhibits a high ionic conductivity. The ionic liquid comprises a cyclic guanidine salt represented by the following formula (1): wherein R1 and R2 each is independently an alkyl group or an alkoxyalkyl group, X is a methylene group, an oxygen atom, a sulfur atom, or R3N; R3 is an alkyl group, an alkoxyalkyl group, or an acyl group; l, m, and n each is an integer in the range of 1-6; Y? is a monovalent anion such as (R4SO2)2N?, R4SO3?, R4COO?, BF4?, PF6?, NO3?, (CN)2N?, (CHO)2N?, NCS?, R4OSO3?, R4SO2S?, and a halogen ion. The ionic liquid is useful for a variety of electrolytes, particularly for electrolytes of electrochemical cells.
    Type: Application
    Filed: February 26, 2008
    Publication date: May 13, 2010
    Applicant: NIPPON STEEL CHEMICAL CO., LTD.
    Inventors: Atsushi Kawada, Aya Tashiro, Toshihiro Kumagai
  • Patent number: 7714013
    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: May 11, 2010
    Assignee: Transtech Pharma, Inc.
    Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi A. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
  • Publication number: 20100113549
    Abstract: The present invention relates to a process for the preparation of a pyrrolidone compound of the formula (I): where R1 is substituted or unsubstituted alkyl, alkenyl, or alkynyl, or an aromatic or non-aromatic cyclic or heterocyclic structure, R2 is substituted or unsubstituted alkyl or cycloalkyl, and each P is independently a protecting group.
    Type: Application
    Filed: December 6, 2005
    Publication date: May 6, 2010
    Applicant: ISIS INNOVATION LTD.
    Inventors: Timothy Block, Ben Davis, Timothy Chapman, Christopher Schofield
  • Patent number: 7683093
    Abstract: Novel compounds of the formula (I), in which R, R1, R2, R3 and R4 have the meaning indicated in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
    Type: Grant
    Filed: March 4, 2005
    Date of Patent: March 23, 2010
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz
  • Publication number: 20100056593
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: September 3, 2009
    Publication date: March 4, 2010
    Applicant: Ardea Biosciences
    Inventors: Esmir Gunic, Jean-Luc Girardet, David A. Paisner
  • Patent number: 7659270
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: August 8, 2007
    Date of Patent: February 9, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Publication number: 20090306047
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: June 8, 2009
    Publication date: December 10, 2009
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20090275591
    Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
    Type: Application
    Filed: August 29, 2006
    Publication date: November 5, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
  • Publication number: 20090269301
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently repre
    Type: Application
    Filed: November 8, 2007
    Publication date: October 29, 2009
    Applicant: PROBIODRUG AG
    Inventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
  • Patent number: 7601748
    Abstract: This invention relates to anti-androgenic N-[?-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.
    Type: Grant
    Filed: August 9, 2006
    Date of Patent: October 13, 2009
    Assignee: Bayer Schering Pharma AG
    Inventors: Arwed Cleve, Volker Schulze, Dieter Zopf, Jens Hoffmann, Andreas Reichel, Karsten Parczyk
  • Publication number: 20090239866
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Application
    Filed: July 28, 2006
    Publication date: September 24, 2009
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Jeffrey Michael Axten, Jesus R. Medina
  • Publication number: 20090233901
    Abstract: There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.
    Type: Application
    Filed: December 13, 2006
    Publication date: September 17, 2009
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
  • Patent number: 7582668
    Abstract: Provided are compounds of Formula I and pharmaceutically acceptable salts thereof which may be useful for the treatment of cancer or other proliferative disorders.
    Type: Grant
    Filed: November 8, 2006
    Date of Patent: September 1, 2009
    Assignees: Cytokinetics, Incorporated, SmithKline Beecham Corporation
    Inventors: Xiangping Qian, Luke W. Ashcraft, Jianchao Wang, Bing Yao, Hong Jiang, Gustave Bergnes, Bradley P. Morgan, David J. Morgans, Jr., Dashyant Dhanak, Steven D. Knight, Nicholas D. Adams, Cynthia A. Parrish, Kevin J. Duffy, Duke Fitch, Rosanna Tedesco
  • Publication number: 20090215795
    Abstract: A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.
    Type: Application
    Filed: July 17, 2008
    Publication date: August 27, 2009
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musha, Motoji Kogushi, Tsutomu Kawata, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
  • Publication number: 20090198056
    Abstract: The present invention relates to a compound of the formula (1): wherein R1 is group of the formula (2): (wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5 and R6 are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1 is single bond, etc., R2 is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3 is hydrogen atom, etc., L2 is single bond, etc., R4 is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.
    Type: Application
    Filed: August 31, 2006
    Publication date: August 6, 2009
    Inventors: Tsutomu Mimoto, Satoshi Nojima, Naoya Kinomura, Yoshiaki Kiso