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: 20140094436
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 3, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
  • Publication number: 20140066425
    Abstract: Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.
    Type: Application
    Filed: March 8, 2012
    Publication date: March 6, 2014
    Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.
    Inventor: Youzhi Tong
  • Patent number: 8642628
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: February 4, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140031331
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
  • Publication number: 20140024680
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 23, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventor: Bayer Intellectual Property GmbH
  • Patent number: 8618152
    Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt, or mixtures thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: December 31, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc J. Farmer, Robert B. Perni, Govinda Rao Bhisetti, Keith P. Wilson
  • Patent number: 8618153
    Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: December 31, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Makonen Belema
  • Publication number: 20130303572
    Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 14, 2013
    Inventors: Péter Ferdinandy, Tamás Bálint Csont, Csaba Csonka, Krisztina Kedvesné Kupai, László Kovács, Attila Kis-Tamás, Ferenc Tamás Takács, Dénes Kónya, Gábor Medgyes, Sándor Cseh, István Hajdú, Zsolt Lõrincz, György Dormán, Anikó Görbe
  • Publication number: 20130296322
    Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 7, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
  • Publication number: 20130289086
    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: July 13, 2012
    Publication date: October 31, 2013
    Inventor: Mark E. Duggan
  • Patent number: 8552047
    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: January 30, 2012
    Date of Patent: October 8, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Omar D. Lopez, Gan Wang, Makonen Belema, John F. Kadow
  • Publication number: 20130253008
    Abstract: The present invention relates to novel azoles, novel antiviral active components of the general formulas 1A and 1B, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatitis C viruses (HCV). In general formulas 1A and 1B wherein: solid lines with accompanying dotted lines () represent ordinary bond or double bond, provided that one of them is an ordinary bond, the other one is double bond; X and Y accept various meanings, one of them is—nitrogen, the other—oxygen, sulfur or NH group; R1 and R2—optionally the same radicals selected from 2-(R)- and (S)-substituted N-acyl pyrrolidine derivatives; N-methyl-N-[2-(R) and (S)-substituted 2,2-disubstituted acetamides; methyl[2-(R) and (S)-substituted ((methyl)amino)-(1-oxobutan-2-yl)-2-(R)-] and (S)-iso-propyl)-carbamates.
    Type: Application
    Filed: November 28, 2011
    Publication date: September 26, 2013
    Applicant: Alla Chem LLC
    Inventors: Alexandre Vasilievich Ivachtchenko, Vadim Vasilievich Bichko, Oleg Dmitrievich Mitkin
  • Publication number: 20130237514
    Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.
    Type: Application
    Filed: October 5, 2012
    Publication date: September 12, 2013
    Applicant: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
  • Publication number: 20130230501
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
    Type: Application
    Filed: July 16, 2012
    Publication date: September 5, 2013
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
  • Publication number: 20130225644
    Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
    Type: Application
    Filed: April 1, 2013
    Publication date: August 29, 2013
    Applicant: Zealand Pharma A/S
    Inventor: Zealand Pharma A/S
  • Publication number: 20130210774
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 15, 2013
    Applicants: EMORY UNIVERSITY, RFS PHARMA, LLC
    Inventors: Steven J. Coats, Franck Amblard, Hongwang Zhang, Longhu Zhou, Richard Anthony Whitaker, Tamara Rosario McBrayer, Raymond F. Schinazi, Junxing Shi
  • Publication number: 20130196971
    Abstract: This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer.
    Type: Application
    Filed: September 15, 2011
    Publication date: August 1, 2013
    Inventors: Christopher Joseph Aquino, Dennis Heyer, Terence John Kiesow, David Lee Musso, Cynthia A. Parrish
  • Patent number: 8497289
    Abstract: In one aspect, the invention relates to compounds which are useful 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: Grant
    Filed: December 29, 2009
    Date of Patent: July 30, 2013
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
  • Publication number: 20130184238
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Patent number: 8476454
    Abstract: Compounds, compositions and methods for the treatment of malignancy are disclosed.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: July 2, 2013
    Assignee: Lankenau Institute for Medical Research
    Inventors: George C. Prendergast, Alexander J. Muller, James B. Duhadaway, William Malachowski
  • Patent number: 8470857
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: June 25, 2013
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20130152314
    Abstract: The invention relates to a composition for dyeing keratin materials, and in particular human keratin fibres such as the hair, comprising at least one 2-pyrrolidone functionalized in the 4 position with an ester or amide radical, and at least one hydrophobic direct dye or a pigment; a dyeing process using this composition. Similarly, the invention relates to the use of the said pyrrolidone combined with a direct dye or a pigment for dyeing keratin materials, and especially to the use of the said pyrrolidone for improving the colour uptake onto the fibres of direct dyes that are sparingly soluble or insoluble in aqueous-alcoholic supports. The invention also relates to novel pyrrolidone derivatives. The present invention makes it possible in particular to obtain direct dyeing on keratin materials that is fast, resistant to washing, chromatic and powerful.
    Type: Application
    Filed: June 8, 2011
    Publication date: June 20, 2013
    Applicant: L'OREAL
    Inventors: Stéphane Sabelle, Madeleine Leduc, Christian Blaise
  • Patent number: 8450478
    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: Grant
    Filed: January 25, 2012
    Date of Patent: May 28, 2013
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Atsushi Kawada, Aya Tashiro, Toshihiro Kumagai
  • Patent number: 8450304
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: May 28, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
  • Patent number: 8436034
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a? and I-A.a? in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: May 7, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Andreas Kling, Wilfried Hornberger, Helmut Mack, Achim Moeller, Volker Nimmrich, Dietmar Seeman, Wilfried Lubisch
  • Publication number: 20130090362
    Abstract: Polyamide compositions containing guanidinyl radicals, including tetramethylguanidinyl radicals, are described. These polyamides are useful for medical applications, for example, for treating human papilloma virus infections.
    Type: Application
    Filed: October 10, 2012
    Publication date: April 11, 2013
    Applicant: NANOVIR, LLC
    Inventor: NANOVIR, LLC
  • Publication number: 20130085147
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
    Type: Application
    Filed: November 7, 2012
    Publication date: April 4, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130040963
    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: June 4, 2012
    Publication date: February 14, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Esmir GUNIC, Jean-Luc GIRARDET, David A. PAISNER
  • Patent number: 8362003
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: January 29, 2013
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Publication number: 20130022587
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
    Type: Application
    Filed: July 16, 2012
    Publication date: January 24, 2013
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
  • Publication number: 20130017196
    Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
  • Patent number: 8354434
    Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: January 15, 2007
    Date of Patent: January 15, 2013
    Assignee: Purdue Pharma L.P.
    Inventor: Xiaoming Zhou
  • Publication number: 20120328565
    Abstract: The present invention discloses compounds of Formula I wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the treatment of HCV infection.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: John A. Brinkman, Andrew F. Donnell, Robert Francis Kester, Yimin Qian, Ramakanth Sarabu, Sung-Sau So
  • Publication number: 20120316170
    Abstract: To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): or the general formula (II): or an isotope thereof or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: Daiichi Sankyo Company Limited
    Inventors: Nobuo Machinaga, Jun Chiba, Fumihito Muro, Hiroshi Yuita, Jun Watanabe
  • Publication number: 20120316193
    Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.
    Type: Application
    Filed: May 10, 2012
    Publication date: December 13, 2012
    Inventors: Megan Foley, Bradley Tait, Matthew Cullen
  • Publication number: 20120302538
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/ and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Application
    Filed: May 29, 2012
    Publication date: November 29, 2012
    Applicant: ACHILLION PHARMACEUTICALS, INC
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Publication number: 20120295881
    Abstract: The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: July 11, 2012
    Publication date: November 22, 2012
    Applicant: Abbott GmbH & Co. KG
    Inventors: Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Frauke Pohlki, Charles W. Hutchins
  • Patent number: 8304410
    Abstract: The present invention relates to compounds having formula 3 as well as the synthesis, intermediates and methods of using the same.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: November 6, 2012
    Assignees: Università degli Studi di Roma “La Sapienza”, Università degli Studi di Siena
    Inventors: Mariangela Biava, Giulio Cesare Porretta, Raffaello Pompei, Maurizio Botta, Fabrizio Manetti, Alessandro De Logu
  • Publication number: 20120277217
    Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
    Type: Application
    Filed: October 27, 2010
    Publication date: November 1, 2012
    Applicant: NewLink Genetics Corporation
    Inventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
  • Patent number: 8288534
    Abstract: The invention relates to a novel process for the preparation of Ruthenium metathesis catalysts of the formula Ruthenium metathesis catalysts have been widely applied in the synthesis of macrocyclic drug compounds.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: October 16, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Angelino Doppiu, Ralf Karch, Kurt Puentener, Andreas Rivas-Nass, Michelangelo Scalone, Roland Winde, Eileen Woerner
  • Patent number: 8278307
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: May 8, 2007
    Date of Patent: October 2, 2012
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Mathew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi K. Sawyer, Jan Antoinette C. Romero
  • Patent number: 8268750
    Abstract: The invention relates to novel insecticidal active compound combinations comprising, firstly, compounds which act as insecticides on nicotinergic acetylcholine receptors as agonists and antagonists, and at least one active compound from the group of the anthranilamides, which combinations are suitable for protecting plants against attack by pests.
    Type: Grant
    Filed: October 30, 2004
    Date of Patent: September 18, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Christian Funke, Reiner Fischer, Rüdiger Fischer, Heike Hungenberg, Wolfram Andersch, Wolfgang Thielert, Anton Kraus
  • Patent number: 8252829
    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: Grant
    Filed: June 7, 2010
    Date of Patent: August 28, 2012
    Assignee: Link Medicine Corporation
    Inventor: Mark E. Duggan
  • Publication number: 20120196866
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 2, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
  • Publication number: 20120190700
    Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.
    Type: Application
    Filed: January 17, 2012
    Publication date: July 26, 2012
    Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
  • Publication number: 20120184580
    Abstract: Substituted di-arylhydantoin and di-arylthiohydantoins are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including CRPC and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: April 9, 2010
    Publication date: July 19, 2012
    Applicant: MEDIVATION PROSTATE THERAPEUTICS, INC.
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20120171125
    Abstract: A compound having an affinity to a SV2 protein for the treatment of a condition associated with enhancement or improvement of the cognitive ability or to counteract cognitive decline of a mammal. For example, a compound which is covered by formula (I) R1 is an halogen atom, preferably, a chlorine or a fluorine atom; n is equal to 1, 2 or 3; and R2 is cyano.
    Type: Application
    Filed: August 4, 2010
    Publication date: July 5, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoît Kenda, Alain Matagne
  • Patent number: 8211401
    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: Grant
    Filed: December 4, 2009
    Date of Patent: July 3, 2012
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
  • Patent number: 8207155
    Abstract: In one aspect, the invention relates to compounds which are useful 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: Grant
    Filed: March 31, 2010
    Date of Patent: June 26, 2012
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
  • Publication number: 20120149660
    Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R2, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.
    Type: Application
    Filed: December 9, 2011
    Publication date: June 14, 2012
    Inventors: Jin-Jun Liu, Tina Morgan Ross