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)
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Publication number: 20110070197Abstract: 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: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Ce Wang, Yao-Ling Qiu
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Publication number: 20110064697Abstract: 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: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20110064695Abstract: 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: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
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Patent number: 7906503Abstract: 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: GrantFiled: October 21, 2008Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
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Publication number: 20110046113Abstract: 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: ApplicationFiled: October 12, 2010Publication date: February 24, 2011Applicant: KUREHA CORPORATIONInventors: Toru YAMAZAKI, Shigeyuki KIKUMOTO, Masahiro ONO, Atsushi SAITOU, Haruka TAKAHASHI, Sei KUMAKURA, Kunitaka HIROSE, Mikiro YANAKA, Yoshiyuki TAKEMURA, Shigeru SUZUKI, Ryo MATSUI
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Publication number: 20110046105Abstract: 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: ApplicationFiled: August 6, 2010Publication date: February 24, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Jaehne, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
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Publication number: 20110041261Abstract: 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: ApplicationFiled: December 9, 2008Publication date: February 24, 2011Inventors: Madeleine Leduc, Stéphane Sabelle, Eric Metais, Christophe Rondot
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Publication number: 20110036975Abstract: Imidazolium-based dicationic liquid salts and methods of using such imidazolium-based dicationic liquid salts in techniques such as ESI-MS are provided.Type: ApplicationFiled: February 17, 2009Publication date: February 17, 2011Applicant: SIGMA-ALDRICH CO.Inventor: Armstrong W. Daniel
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Publication number: 20110028476Abstract: 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: ApplicationFiled: September 1, 2010Publication date: February 3, 2011Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Publication number: 20110021590Abstract: 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: ApplicationFiled: June 7, 2010Publication date: January 27, 2011Applicant: Link Medicine CorporationInventor: Mark E. Duggan
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Publication number: 20110003690Abstract: 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: ApplicationFiled: January 29, 2009Publication date: January 6, 2011Applicant: BAY CROPSCIENCE AGInventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
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Publication number: 20110003825Abstract: 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: ApplicationFiled: August 23, 2010Publication date: January 6, 2011Applicant: Schering CorporationInventors: Ying Huang, Guoqing Li, Andrew W. Stamford
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Patent number: 7838681Abstract: 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: GrantFiled: April 30, 2004Date of Patent: November 23, 2010Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite de Paris SudInventors: Ali Al Mourabit, Nathalie Travert, Robert Abou-Jneid, Saïd Ghoulami
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Publication number: 20100273849Abstract: 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: ApplicationFiled: January 26, 2010Publication date: October 28, 2010Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenchöld, Pavol Zlatoidsky
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Publication number: 20100267722Abstract: 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: ApplicationFiled: April 16, 2010Publication date: October 21, 2010Inventors: 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
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Publication number: 20100261696Abstract: 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: ApplicationFiled: March 31, 2010Publication date: October 14, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Publication number: 20100256192Abstract: 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: ApplicationFiled: December 29, 2009Publication date: October 7, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Patent number: 7807844Abstract: 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: GrantFiled: September 3, 2004Date of Patent: October 5, 2010Assignees: Nihon University, Gentier Biosystems, Inc.Inventors: Noboru Fukuda, Hirofumi Kishioka, Hiroshi Sugiyama
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Publication number: 20100234374Abstract: 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: ApplicationFiled: December 21, 2006Publication date: September 16, 2010Inventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Raffaele Ingenito, Carsten Schultz-Fademrecht
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Publication number: 20100227855Abstract: 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: ApplicationFiled: March 16, 2010Publication date: September 9, 2010Applicant: ENDORECHERCHE, INC.Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, René Maltais
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Patent number: 7790707Abstract: 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: GrantFiled: March 21, 2007Date of Patent: September 7, 2010Assignee: EPIX Pharmaceuticals Inc.Inventors: Ashis Saha, Xiang Yu, Mercedes Lobera, Jian Lin, Srinivasa R. Cheruku, Oren Becker, Yael Marantz, Nili Schutz
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Patent number: 7790710Abstract: 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: GrantFiled: March 29, 2006Date of Patent: September 7, 2010Assignee: NYCOMED GmbHInventors: Thomas Fuchss, Andreas Strub, Wolf-Rüdiger Ulrich, Christian Hesslinger, Martin Lehner, Raimund Külzer, Rainer Boer, Manfrid Eltze
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Publication number: 20100216792Abstract: 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: ApplicationFiled: October 14, 2009Publication date: August 26, 2010Applicant: Bayer CropScience AGInventors: 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
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Publication number: 20100216806Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
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Publication number: 20100216813Abstract: 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: ApplicationFiled: November 29, 2006Publication date: August 26, 2010Inventor: James S. Frazee
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Publication number: 20100184737Abstract: 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: ApplicationFiled: March 12, 2010Publication date: July 22, 2010Applicant: Pfizer IncInventors: Michael A. Brodney, Karen J. Coffman, Edward F. Kleinman, Brian T. O'Neill, Yuhpyng L. Chen
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Publication number: 20100178246Abstract: 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: ApplicationFiled: December 4, 2009Publication date: July 15, 2010Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Patent number: 7754750Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: GrantFiled: May 6, 2008Date of Patent: July 13, 2010Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
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Publication number: 20100173898Abstract: 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: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: SANOFI-AVENTISInventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
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Publication number: 20100168107Abstract: 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: ApplicationFiled: March 12, 2010Publication date: July 1, 2010Applicant: Pfizer IncInventors: Michael A. Brodney, Karen J. Coffman
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Publication number: 20100168088Abstract: 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: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20100168189Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.Type: ApplicationFiled: February 8, 2008Publication date: July 1, 2010Inventors: David W. Old, Wha Bin Im, Vinh X. Ngo
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Patent number: 7741347Abstract: 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: GrantFiled: May 14, 2008Date of Patent: June 22, 2010Assignee: Bristol-Myers Squibb CompanyInventors: 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
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Publication number: 20100130446Abstract: 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: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: TAKEDA PHARMACEUTICAS COMPANY LIMITEDInventors: Tsuneo Yasuma, Kentaro Hashimoto, Masahiro Ito
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Patent number: 7723307Abstract: 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: GrantFiled: June 16, 2004Date of Patent: May 25, 2010Assignee: Aston UniversityInventors: Martin Griffin, Ian G. Coutts, Robert E. Saint
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Publication number: 20100121074Abstract: 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: ApplicationFiled: February 26, 2008Publication date: May 13, 2010Applicant: NIPPON STEEL CHEMICAL CO., LTD.Inventors: Atsushi Kawada, Aya Tashiro, Toshihiro Kumagai
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Patent number: 7714013Abstract: 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: GrantFiled: August 28, 2006Date of Patent: May 11, 2010Assignee: 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
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Publication number: 20100113549Abstract: 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: ApplicationFiled: December 6, 2005Publication date: May 6, 2010Applicant: ISIS INNOVATION LTD.Inventors: Timothy Block, Ben Davis, Timothy Chapman, Christopher Schofield
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Patent number: 7683093Abstract: 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: GrantFiled: March 4, 2005Date of Patent: March 23, 2010Assignee: Merck Patent GmbHInventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz
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Publication number: 20100056593Abstract: 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: ApplicationFiled: September 3, 2009Publication date: March 4, 2010Applicant: Ardea BiosciencesInventors: Esmir Gunic, Jean-Luc Girardet, David A. Paisner
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Patent number: 7659270Abstract: 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: GrantFiled: August 8, 2007Date of Patent: February 9, 2010Assignee: Bristol-Myers Squibb CompanyInventors: 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
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Publication number: 20090306047Abstract: 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: ApplicationFiled: June 8, 2009Publication date: December 10, 2009Inventors: 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
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Publication number: 20090275591Abstract: 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: ApplicationFiled: August 29, 2006Publication date: November 5, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTEDInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
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Publication number: 20090269301Abstract: 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 repreType: ApplicationFiled: November 8, 2007Publication date: October 29, 2009Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Patent number: 7601748Abstract: 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: GrantFiled: August 9, 2006Date of Patent: October 13, 2009Assignee: Bayer Schering Pharma AGInventors: Arwed Cleve, Volker Schulze, Dieter Zopf, Jens Hoffmann, Andreas Reichel, Karsten Parczyk
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Publication number: 20090239866Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: July 28, 2006Publication date: September 24, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jeffrey Michael Axten, Jesus R. Medina
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Publication number: 20090233901Abstract: There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.Type: ApplicationFiled: December 13, 2006Publication date: September 17, 2009Applicant: Daiichi Sankyo Company, LimitedInventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
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Patent number: 7582668Abstract: 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: GrantFiled: November 8, 2006Date of Patent: September 1, 2009Assignees: Cytokinetics, Incorporated, SmithKline Beecham CorporationInventors: 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
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Publication number: 20090215795Abstract: 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: ApplicationFiled: July 17, 2008Publication date: August 27, 2009Applicant: 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
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Publication number: 20090198056Abstract: 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: ApplicationFiled: August 31, 2006Publication date: August 6, 2009Inventors: Tsutomu Mimoto, Satoshi Nojima, Naoya Kinomura, Yoshiaki Kiso